dataset_id
large_stringclasses
414 values
reaction_id
large_stringlengths
36
36
reaction_smiles
large_stringlengths
4
873
rxn_insight_reaction
large_stringlengths
19
1.07k
mapped_reaction_smiles
large_stringlengths
14
3.37k
reactant_smiles
large_stringlengths
1
581
product_smiles
large_stringlengths
1
433
reagent_smiles
large_stringclasses
634 values
catalyst_smiles
large_stringlengths
1
683
solvent_smiles
large_stringlengths
1
245
rxn_insight_class
large_stringclasses
11 values
rxn_insight_name
large_stringclasses
346 values
rxn_insight_tag
large_stringlengths
64
64
rxn_insight_tag2
large_stringlengths
64
64
rxn_insight_scaffold
large_stringlengths
5
288
rxn_insight_template
large_stringlengths
24
2.64k
yield_percent
float64
-0.8
90,205,160,000B
yield_measurements
large_stringlengths
2
864
temperature_value
float64
-230
30.1k
temperature_units
large_stringclasses
3 values
reaction_time_value
float64
0
4k
time_units
large_stringclasses
4 values
procedure_details
large_stringlengths
1
23.6k
reference
large_stringclasses
96 values
doi
large_stringclasses
19 values
functional_groups_reactants
large_stringlengths
3
716
functional_groups_products
large_stringlengths
3
539
participating_rings_reactants
large_stringlengths
5
293
participating_rings_products
large_stringlengths
5
271
all_rings_products
large_stringlengths
5
271
byproduct_smiles
large_stringclasses
176 values
agent_smiles
large_stringlengths
1
712
temperature_c
float64
-230
30.1k
reaction_time_hours
float64
0
2.16k
reaction_smiles_with_agents
large_stringlengths
4
882
ord_dataset-c3a75813d0b24864aa4f7cd526efd6aa
ord-7b246f45fa6645ec92d12a7f69d24d40
CC(C)(O)C1=CC[C@H]2C3=CC=C4C[C@@H](O[Si](C)(C)C(C)(C)C)C[C@H](O[Si](C)(C)C(C)(C)C)[C@]4(C)[C@H]3CC[C@]12C.CC[Si](CC)(CC)OC(C)(C)C#CCBr>>CC[Si](CC)(CC)OC(C)(C)C#CCOC(C)(C)C1=CC[C@H]2C3=CC=C4C[C@@H](O[Si](C)(C)C(C)(C)C)C[C@H](O[Si](C)(C)C(C)(C)C)[C@]4(C)[C@H]3CC[C@]12C
[Si](C)(C)(C(C)(C)C)O[C@H]1C[C@@H](CC2=CC=C3[C@@H]4CC=C(C(C)(C)O)[C@]4(CC[C@@H]3[C@@]12C)C)O[Si](C)(C)C(C)(C)C.BrCC#CC(C)(C)O[Si](CC)(CC)CC.[H-].[Na+].C1COCCOCCOCCOCCO1>>[Si](C)(C)(C(C)(C)C)O[C@H]1C[C@@H](CC2=CC=C3[C@@H]4CC=C(C(C)(C)OCC#CC(C)(C)O[Si](CC)(CC)CC)[C@]4(CC[C@@H]3[C@@]12C)C)O[Si](C)(C)C(C)(C)C
[OH:15][C:16]([CH3:17])([CH3:18])[C:19]1=[CH:20][CH2:21][C@H:22]2[C:23]3=[CH:24][CH:25]=[C:26]4[CH2:27][C@@H:28]([O:29][Si:30]([CH3:31])([CH3:32])[C:33]([CH3:34])([CH3:35])[CH3:36])[CH2:37][C@H:38]([O:39][Si:40]([CH3:41])([CH3:42])[C:43]([CH3:44])([CH3:45])[CH3:46])[C@:47]4([CH3:48])[C@H:49]3[CH2:50][CH2:51][C@:52]12[C...
CC(C)(O)C1=CC[C@H]2C3=CC=C4C[C@@H](O[Si](C)(C)C(C)(C)C)C[C@H](O[Si](C)(C)C(C)(C)C)[C@]4(C)[C@H]3CC[C@]12C.CC[Si](CC)(CC)OC(C)(C)C#CCBr
CC[Si](CC)(CC)OC(C)(C)C#CCOC(C)(C)C1=CC[C@H]2C3=CC=C4C[C@@H](O[Si](C)(C)C(C)(C)C)C[C@H](O[Si](C)(C)C(C)(C)C)[C@]4(C)[C@H]3CC[C@]12C
null
null
O1CCCC1
Heteroatom Alkylation and Arylation
Williamson Ether Synthesis
9ef84a8c80411e848c10c5384ce78141e473ad5db44b97f46285876278d6d001
004868630acb495c3cf864467df50d8e3d3bf839809342ad5aeae72f8c34f6c8
C1=CC2CC[C@H]3C(=CC=C4CCCCC43)[C@@H]2C1
Br-[CH2;D2;+0:1]-[C:2]#[C:3]-[C:4].[C:5]-[C:6]=[C:7](-[C:8](-[C;D1;H3:9])(-[C;D1;H3:10])-[OH;D1;+0:11])-[C:12]>>[C:5]-[C:6]=[C:7](-[C:8](-[C;D1;H3:9])(-[C;D1;H3:10])-[O;H0;D2;+0:11]-[CH2;D2;+0:1]-[C:2]#[C:3]-[C:4])-[C:12]
62
[{"value": 62.0, "product": "[Si](C)(C)(C(C)(C)C)O[C@H]1C[C@@H](CC2=CC=C3[C@@H]4CC=C(C(C)(C)OCC#CC(C)(C)O[Si](CC)(CC)CC)[C@]4(CC[C@@H]3[C@@]12C)C)O[Si](C)(C)C(C)(C)C", "details": "PERCENTYIELD", "is_desired": false}, {"value": 62.0, "product": "[Si](C)(C)(C(C)(C)C)O[C@H]1C[C@@H](CC2=CC=C3[C@@H]4CC=C(C(C)(C)OCC#CC(C)(C)...
null
null
null
null
1α,3β-Bis(tert-Butyldimethylsilyloxy)-20-hydroxy-20-methylpregna-5,7,16-triene (100 mg, 0.175 mmol), 1-bromo-4-triethylsilyloxy-4-methyl-2-pentyne (203 mg, 0.697 mmol), sodium hydride (60% in oil, 42 mg, 1.05 mmol), 15-crown-5 (38 mg, 0.173 mmol) and tetrahydrofuran (3 ml) were reacted using a procedure similar to that...
10.6084/m9.figshare.5104873.v1
null
Primary halide.Tertiary alcohol
Ether
null
null
C1=C[C@H]2CC[C@H]3C(=CC=C4CCCC[C@@H]43)[C@@H]2C1
HBr
O1CCCC1
null
null
CC(C)(O)C1=CC[C@H]2C3=CC=C4C[C@@H](O[Si](C)(C)C(C)(C)C)C[C@H](O[Si](C)(C)C(C)(C)C)[C@]4(C)[C@H]3CC[C@]12C.CC[Si](CC)(CC)OC(C)(C)C#CCBr>O1CCCC1>CC[Si](CC)(CC)OC(C)(C)C#CCOC(C)(C)C1=CC[C@H]2C3=CC=C4C[C@@H](O[Si](C)(C)C(C)(C)C)C[C@H](O[Si](C)(C)C(C)(C)C)[C@]4(C)[C@H]3CC[C@]12C
ord_dataset-c3a75813d0b24864aa4f7cd526efd6aa
ord-e2a5237451924062ae26aea06949245a
CC(C)(O)C1=CC[C@H]2C3=CC=C4C[C@@H](O[Si](C)(C)C(C)(C)C)C[C@H](O[Si](C)(C)C(C)(C)C)[C@]4(C)[C@H]3CC[C@]12C.CC[Si](CC)(CC)OC(C)(C)C/C=C/Br>>CC[Si](CC)(CC)OC(C)(C)C/C=C/OC(C)(C)C1=CC[C@H]2C3=CC=C4C[C@@H](O[Si](C)(C)C(C)(C)C)C[C@H](O[Si](C)(C)C(C)(C)C)[C@]4(C)[C@H]3CC[C@]12C
[Si](C)(C)(C(C)(C)C)O[C@H]1C[C@@H](CC2=CC=C3[C@@H]4CC=C(C(C)(C)O)[C@]4(CC[C@@H]3[C@@]12C)C)O[Si](C)(C)C(C)(C)C.Br\C=C\CC(C)(C)O[Si](CC)(CC)CC.[H-].[Na+].C1COCCOCCOCCOCCO1>>[Si](C)(C)(C(C)(C)C)O[C@H]1C[C@@H](CC2=CC=C3[C@@H]4CC=C(C(C)(C)O\C=C\CC(C)(C)O[Si](CC)(CC)CC)[C@]4(CC[C@@H]3[C@@]12C)C)O[Si](C)(C)C(C)(C)C
[OH:15][C:16]([CH3:17])([CH3:18])[C:19]1=[CH:20][CH2:21][C@H:22]2[C:23]3=[CH:24][CH:25]=[C:26]4[CH2:27][C@@H:28]([O:29][Si:30]([CH3:31])([CH3:32])[C:33]([CH3:34])([CH3:35])[CH3:36])[CH2:37][C@H:38]([O:39][Si:40]([CH3:41])([CH3:42])[C:43]([CH3:44])([CH3:45])[CH3:46])[C@:47]4([CH3:48])[C@H:49]3[CH2:50][CH2:51][C@:52]12[C...
CC(C)(O)C1=CC[C@H]2C3=CC=C4C[C@@H](O[Si](C)(C)C(C)(C)C)C[C@H](O[Si](C)(C)C(C)(C)C)[C@]4(C)[C@H]3CC[C@]12C.CC[Si](CC)(CC)OC(C)(C)C/C=C/Br
CC[Si](CC)(CC)OC(C)(C)C/C=C/OC(C)(C)C1=CC[C@H]2C3=CC=C4C[C@@H](O[Si](C)(C)C(C)(C)C)C[C@H](O[Si](C)(C)C(C)(C)C)[C@]4(C)[C@H]3CC[C@]12C
null
null
O1CCCC1
Acylation
Williamson Ether Synthesis
3bebab49d1e73ccb378d80c964dd2eb3ac4ae759a028f210c53302497d420909
68002c25e6f3b076ffda77fb7b82207a1a988042aa4418cc4cd63986b874c804
C1=CC2CC[C@H]3C(=CC=C4CCCCC43)[C@@H]2C1
Br/[CH;D2;+0:1]=[C:2]/[C:3]-[C:4].[C:5]-[C:6]=[C:7](-[C:8](-[C;D1;H3:9])(-[C;D1;H3:10])-[OH;D1;+0:11])-[C:12]>>[C:5]-[C:6]=[C:7](-[C:8](-[C;D1;H3:9])(-[C;D1;H3:10])-[O;H0;D2;+0:11]/[CH;D2;+0:1]=[C:2]/[C:3]-[C:4])-[C:12]
99
[{"value": 99.0, "product": "[Si](C)(C)(C(C)(C)C)O[C@H]1C[C@@H](CC2=CC=C3[C@@H]4CC=C(C(C)(C)O\\C=C\\CC(C)(C)O[Si](CC)(CC)CC)[C@]4(CC[C@@H]3[C@@]12C)C)O[Si](C)(C)C(C)(C)C", "details": "PERCENTYIELD", "is_desired": false}, {"value": 99.0, "product": "[Si](C)(C)(C(C)(C)C)O[C@H]1C[C@@H](CC2=CC=C3[C@@H]4CC=C(C(C)(C)O\\C=C\\...
null
null
null
null
1α,3β-Bis(tert-butyldimethylsilyloxy)-20-hydroxy-20-methylpregna-5,7,16-triene (103 mg, 0.180 mmol), 1-bromo-4-triethylsilyloxy-4-methyl-(2E)-pentene (211 mg, 0.719 mmol), sodium hydride (60% in oil, 43 mg, 1.08 mmol), 15-crown-5 (40 mg, 0.182 mmol) and tetrahydrofuran (3 ml) were subjected to reaction using a procedur...
10.6084/m9.figshare.5104873.v1
null
Tertiary alcohol
Ether
null
null
C1=C[C@H]2CC[C@H]3C(=CC=C4CCCC[C@@H]43)[C@@H]2C1
HBr
O1CCCC1
null
null
CC(C)(O)C1=CC[C@H]2C3=CC=C4C[C@@H](O[Si](C)(C)C(C)(C)C)C[C@H](O[Si](C)(C)C(C)(C)C)[C@]4(C)[C@H]3CC[C@]12C.CC[Si](CC)(CC)OC(C)(C)C/C=C/Br>O1CCCC1>CC[Si](CC)(CC)OC(C)(C)C/C=C/OC(C)(C)C1=CC[C@H]2C3=CC=C4C[C@@H](O[Si](C)(C)C(C)(C)C)C[C@H](O[Si](C)(C)C(C)(C)C)[C@]4(C)[C@H]3CC[C@]12C
ord_dataset-c3a75813d0b24864aa4f7cd526efd6aa
ord-d3e80b1865d34207a9241eaeb472ffcb
CCC(C)(O)C1=CC[C@H]2C3=CC=C4C[C@@H](O[Si](C)(C)C(C)(C)C)C[C@H](O[Si](C)(C)C(C)(C)C)[C@]4(C)[C@H]3CC[C@]12C.CC[Si](CC)(CC)OC(C)(C)C/C=C\Br>>CCC(C)(O/C=C\CC(C)(C)O[Si](CC)(CC)CC)C1=CC[C@H]2C3=CC=C4C[C@@H](O[Si](C)(C)C(C)(C)C)C[C@H](O[Si](C)(C)C(C)(C)C)[C@]4(C)[C@H]3CC[C@]12C
[Si](C)(C)(C(C)(C)C)O[C@H]1C[C@@H](CC2=CC=C3[C@@H]4CC=C(C(C)(CC)O)[C@]4(CC[C@@H]3[C@@]12C)C)O[Si](C)(C)C(C)(C)C.Br\C=C/CC(C)(C)O[Si](CC)(CC)CC.[H-].[Na+].C1COCCOCCOCCOCCO1>>[Si](C)(C)(C(C)(C)C)O[C@H]1C[C@@H](CC2=CC=C3[C@@H]4CC=C(C(C)(CC)O\C=C/CC(C)(C)O[Si](CC)(CC)CC)[C@]4(CC[C@@H]3[C@@]12C)C)O[Si](C)(C)C(C)(C)C
[CH3:1][CH2:2][C:3]([CH3:4])([OH:5])[C:20]1=[CH:21][CH2:22][C@H:23]2[C:24]3=[CH:25][CH:26]=[C:27]4[CH2:28][C@@H:29]([O:30][Si:31]([CH3:32])([CH3:33])[C:34]([CH3:35])([CH3:36])[CH3:37])[CH2:38][C@H:39]([O:40][Si:41]([CH3:42])([CH3:43])[C:44]([CH3:45])([CH3:46])[CH3:47])[C@:48]4([CH3:49])[C@H:50]3[CH2:51][CH2:52][C@:53]1...
CCC(C)(O)C1=CC[C@H]2C3=CC=C4C[C@@H](O[Si](C)(C)C(C)(C)C)C[C@H](O[Si](C)(C)C(C)(C)C)[C@]4(C)[C@H]3CC[C@]12C.CC[Si](CC)(CC)OC(C)(C)C/C=C\Br
CCC(C)(O/C=C\CC(C)(C)O[Si](CC)(CC)CC)C1=CC[C@H]2C3=CC=C4C[C@@H](O[Si](C)(C)C(C)(C)C)C[C@H](O[Si](C)(C)C(C)(C)C)[C@]4(C)[C@H]3CC[C@]12C
null
null
O1CCCC1
Acylation
Williamson Ether Synthesis
3bebab49d1e73ccb378d80c964dd2eb3ac4ae759a028f210c53302497d420909
68002c25e6f3b076ffda77fb7b82207a1a988042aa4418cc4cd63986b874c804
C1=CC2CC[C@H]3C(=CC=C4CCCCC43)[C@@H]2C1
Br/[CH;D2;+0:1]=[C:2]\[C:3]-[C:4].[C:5]-[C:6]=[C:7](-[C:8](-[C:9])(-[C;D1;H3:10])-[OH;D1;+0:11])-[C:12]>>[C:5]-[C:6]=[C:7](-[C:8](-[C:9])(-[C;D1;H3:10])-[O;H0;D2;+0:11]/[CH;D2;+0:1]=[C:2]\[C:3]-[C:4])-[C:12]
100
[{"value": 100.0, "product": "[Si](C)(C)(C(C)(C)C)O[C@H]1C[C@@H](CC2=CC=C3[C@@H]4CC=C(C(C)(CC)O\\C=C/CC(C)(C)O[Si](CC)(CC)CC)[C@]4(CC[C@@H]3[C@@]12C)C)O[Si](C)(C)C(C)(C)C", "details": "PERCENTYIELD", "is_desired": false}, {"value": 98.0, "product": "[Si](C)(C)(C(C)(C)C)O[C@H]1C[C@@H](CC2=CC=C3[C@@H]4CC=C(C(C)(CC)O\\C=C...
null
null
null
null
1α,3β-Bis(tert-butyldimethylsilyloxy)-20-hydroxy-20-ethylpregna-5,7,16-triene (103 mg, 0.180 mmol), 1-bromo-4-triethylsilyloxy-4-methyl-(2Z)-pentene (211 mg, 0.719 mol), sodium hydride (60% in oil, 43 mg, 1.08 mmol), 15-crown-5 (40 mg, 0.182 mmol) and tetrahydrofuran (3 ml) were subjected to reaction using a procedure ...
10.6084/m9.figshare.5104873.v1
null
Tertiary alcohol
Ether
null
null
C1=C[C@H]2CC[C@H]3C(=CC=C4CCCC[C@@H]43)[C@@H]2C1
HBr
O1CCCC1
null
null
CCC(C)(O)C1=CC[C@H]2C3=CC=C4C[C@@H](O[Si](C)(C)C(C)(C)C)C[C@H](O[Si](C)(C)C(C)(C)C)[C@]4(C)[C@H]3CC[C@]12C.CC[Si](CC)(CC)OC(C)(C)C/C=C\Br>O1CCCC1>CCC(C)(O/C=C\CC(C)(C)O[Si](CC)(CC)CC)C1=CC[C@H]2C3=CC=C4C[C@@H](O[Si](C)(C)C(C)(C)C)C[C@H](O[Si](C)(C)C(C)(C)C)[C@]4(C)[C@H]3CC[C@]12C
ord_dataset-c3a75813d0b24864aa4f7cd526efd6aa
ord-4bbe192ac8e24825a0f792208891f093
CC(C)(O)C1=CC[C@H]2C3=CC=C4C[C@@H](O[Si](C)(C)C(C)(C)C)C[C@H](O[Si](C)(C)C(C)(C)C)[C@]4(C)[C@H]3CC[C@]12C.CCC(C#CCBr)(CC)O[Si](CC)(CC)CC>>CCC(C#CCOC(C)(C)C1=CC[C@H]2C3=CC=C4C[C@@H](O[Si](C)(C)C(C)(C)C)C[C@H](O[Si](C)(C)C(C)(C)C)[C@]4(C)[C@H]3CC[C@]12C)(CC)O[Si](CC)(CC)CC
[Si](C)(C)(C(C)(C)C)O[C@H]1C[C@@H](CC2=CC=C3[C@@H]4CC=C(C(C)(C)O)[C@]4(CC[C@@H]3[C@@]12C)C)O[Si](C)(C)C(C)(C)C.BrCC#CC(CC)(O[Si](CC)(CC)CC)CC.[H-].[Na+].C1COCCOCCOCCOCCO1>>[Si](C)(C)(C(C)(C)C)O[C@H]1C[C@@H](CC2=CC=C3[C@@H]4CC=C(C(C)(C)OCC#CC(CC)(O[Si](CC)(CC)CC)CC)[C@]4(CC[C@@H]3[C@@]12C)C)O[Si](C)(C)C(C)(C)C
[OH:7][C:8]([CH3:9])([CH3:10])[C:11]1=[CH:12][CH2:13][C@H:14]2[C:15]3=[CH:16][CH:17]=[C:18]4[CH2:19][C@@H:20]([O:21][Si:22]([CH3:23])([CH3:24])[C:25]([CH3:26])([CH3:27])[CH3:28])[CH2:29][C@H:30]([O:31][Si:32]([CH3:33])([CH3:34])[C:35]([CH3:36])([CH3:37])[CH3:38])[C@:39]4([CH3:40])[C@H:41]3[CH2:42][CH2:43][C@:44]12[CH3:...
CC(C)(O)C1=CC[C@H]2C3=CC=C4C[C@@H](O[Si](C)(C)C(C)(C)C)C[C@H](O[Si](C)(C)C(C)(C)C)[C@]4(C)[C@H]3CC[C@]12C.CCC(C#CCBr)(CC)O[Si](CC)(CC)CC
CCC(C#CCOC(C)(C)C1=CC[C@H]2C3=CC=C4C[C@@H](O[Si](C)(C)C(C)(C)C)C[C@H](O[Si](C)(C)C(C)(C)C)[C@]4(C)[C@H]3CC[C@]12C)(CC)O[Si](CC)(CC)CC
null
null
O1CCCC1
Heteroatom Alkylation and Arylation
Williamson Ether Synthesis
9ef84a8c80411e848c10c5384ce78141e473ad5db44b97f46285876278d6d001
004868630acb495c3cf864467df50d8e3d3bf839809342ad5aeae72f8c34f6c8
C1=CC2CC[C@H]3C(=CC=C4CCCCC43)[C@@H]2C1
Br-[CH2;D2;+0:1]-[C:2]#[C:3]-[C:4].[C:5]-[C:6]=[C:7](-[C:8](-[C;D1;H3:9])(-[C;D1;H3:10])-[OH;D1;+0:11])-[C:12]>>[C:5]-[C:6]=[C:7](-[C:8](-[C;D1;H3:9])(-[C;D1;H3:10])-[O;H0;D2;+0:11]-[CH2;D2;+0:1]-[C:2]#[C:3]-[C:4])-[C:12]
37.7
[{"value": 37.7, "product": "[Si](C)(C)(C(C)(C)C)O[C@H]1C[C@@H](CC2=CC=C3[C@@H]4CC=C(C(C)(C)OCC#CC(CC)(O[Si](CC)(CC)CC)CC)[C@]4(CC[C@@H]3[C@@]12C)C)O[Si](C)(C)C(C)(C)C", "details": "PERCENTYIELD", "is_desired": false}, {"value": 37.7, "product": "[Si](C)(C)(C(C)(C)C)O[C@H]1C[C@@H](CC2=CC=C3[C@@H]4CC=C(C(C)(C)OCC#CC(CC)...
null
null
null
null
1α,3β-Bis(tert-butyldimethylsilyloxy)-20-hydroxy-20-methylpregna-5,7,16-triene (100 mg, 0.17 mmol), 1-bromo-4-ethyl-4-triethylsilyloxy-2-hexyne (150 mg, 0.47 mmol), sodium hydride (60% in oil, 41 mg, 1.02 mmol), 15-crown-5 (37 mg, 0.17 mmol) and tetrahydrofuran (3 ml) were subjected to reaction using a procedure simila...
10.6084/m9.figshare.5104873.v1
null
Primary halide.Tertiary alcohol
Ether
null
null
C1=C[C@H]2CC[C@H]3C(=CC=C4CCCC[C@@H]43)[C@@H]2C1
HBr
O1CCCC1
null
null
CC(C)(O)C1=CC[C@H]2C3=CC=C4C[C@@H](O[Si](C)(C)C(C)(C)C)C[C@H](O[Si](C)(C)C(C)(C)C)[C@]4(C)[C@H]3CC[C@]12C.CCC(C#CCBr)(CC)O[Si](CC)(CC)CC>O1CCCC1>CCC(C#CCOC(C)(C)C1=CC[C@H]2C3=CC=C4C[C@@H](O[Si](C)(C)C(C)(C)C)C[C@H](O[Si](C)(C)C(C)(C)C)[C@]4(C)[C@H]3CC[C@]12C)(CC)O[Si](CC)(CC)CC
ord_dataset-c3a75813d0b24864aa4f7cd526efd6aa
ord-c180d7eb82f148dfb0d5d778d315e9db
CC(C)(O)C1=CC[C@H]2C3=CC=C4C[C@@H](O[Si](C)(C)C(C)(C)C)C[C@H](O[Si](C)(C)C(C)(C)C)[C@]4(C)[C@H]3CC[C@]12C.CCC(CC)(C/C=C\Br)O[Si](CC)(CC)CC>>CCC(CC)(C/C=C\OC(C)(C)C1=CC[C@H]2C3=CC=C4C[C@@H](O[Si](C)(C)C(C)(C)C)C[C@H](O[Si](C)(C)C(C)(C)C)[C@]4(C)[C@H]3CC[C@]12C)O[Si](CC)(CC)CC
[Si](C)(C)(C(C)(C)C)O[C@H]1C[C@@H](CC2=CC=C3[C@@H]4CC=C(C(C)(C)O)[C@]4(CC[C@@H]3[C@@]12C)C)O[Si](C)(C)C(C)(C)C.Br\C=C/CC(CC)(O[Si](CC)(CC)CC)CC.[H-].[Na+].C1COCCOCCOCCOCCO1>>[Si](C)(C)(C(C)(C)C)O[C@H]1C[C@@H](CC2=CC=C3[C@@H]4CC=C(C(C)(C)O\C=C/CC(CC)(O[Si](CC)(CC)CC)CC)[C@]4(CC[C@@H]3[C@@]12C)C)O[Si](C)(C)C(C)(C)C
[OH:9][C:10]([CH3:11])([CH3:12])[C:13]1=[CH:14][CH2:15][C@H:16]2[C:17]3=[CH:18][CH:19]=[C:20]4[CH2:21][C@@H:22]([O:23][Si:24]([CH3:25])([CH3:26])[C:27]([CH3:28])([CH3:29])[CH3:30])[CH2:31][C@H:32]([O:33][Si:34]([CH3:35])([CH3:36])[C:37]([CH3:38])([CH3:39])[CH3:40])[C@:41]4([CH3:42])[C@H:43]3[CH2:44][CH2:45][C@:46]12[CH...
CC(C)(O)C1=CC[C@H]2C3=CC=C4C[C@@H](O[Si](C)(C)C(C)(C)C)C[C@H](O[Si](C)(C)C(C)(C)C)[C@]4(C)[C@H]3CC[C@]12C.CCC(CC)(C/C=C\Br)O[Si](CC)(CC)CC
CCC(CC)(C/C=C\OC(C)(C)C1=CC[C@H]2C3=CC=C4C[C@@H](O[Si](C)(C)C(C)(C)C)C[C@H](O[Si](C)(C)C(C)(C)C)[C@]4(C)[C@H]3CC[C@]12C)O[Si](CC)(CC)CC
null
null
O1CCCC1
Acylation
Williamson Ether Synthesis
3bebab49d1e73ccb378d80c964dd2eb3ac4ae759a028f210c53302497d420909
68002c25e6f3b076ffda77fb7b82207a1a988042aa4418cc4cd63986b874c804
C1=CC2CC[C@H]3C(=CC=C4CCCCC43)[C@@H]2C1
Br/[CH;D2;+0:1]=[C:2]\[C:3]-[C:4].[C:5]-[C:6]=[C:7](-[C:8](-[C;D1;H3:9])(-[C;D1;H3:10])-[OH;D1;+0:11])-[C:12]>>[C:5]-[C:6]=[C:7](-[C:8](-[C;D1;H3:9])(-[C;D1;H3:10])-[O;H0;D2;+0:11]/[CH;D2;+0:1]=[C:2]\[C:3]-[C:4])-[C:12]
72
[{"value": 72.0, "product": "[Si](C)(C)(C(C)(C)C)O[C@H]1C[C@@H](CC2=CC=C3[C@@H]4CC=C(C(C)(C)O\\C=C/CC(CC)(O[Si](CC)(CC)CC)CC)[C@]4(CC[C@@H]3[C@@]12C)C)O[Si](C)(C)C(C)(C)C", "details": "PERCENTYIELD", "is_desired": false}, {"value": 71.7, "product": "[Si](C)(C)(C(C)(C)C)O[C@H]1C[C@@H](CC2=CC=C3[C@@H]4CC=C(C(C)(C)O\\C=C/...
null
null
null
null
1α,3β-Bis(tert-butyldimethylsilyloxy)-20-hydroxy-20-methylpregna-5,7,16-triene (100 mg, 0.175 mmol), 1-bromo-4-ethyl-4-triethylsilyloxy-(2Z)-hexene (224 mg, 0.697 mmol), sodium hydride (60% in oil, 42 mg, 1.05 mmol), 15-crown-5 (38 mg, 0.173 mmol) and tetrahydrofuran (3 ml) were subjected to reaction using a procedure ...
10.6084/m9.figshare.5104873.v1
null
Tertiary alcohol
Ether
null
null
C1=C[C@H]2CC[C@H]3C(=CC=C4CCCC[C@@H]43)[C@@H]2C1
HBr
O1CCCC1
null
null
CC(C)(O)C1=CC[C@H]2C3=CC=C4C[C@@H](O[Si](C)(C)C(C)(C)C)C[C@H](O[Si](C)(C)C(C)(C)C)[C@]4(C)[C@H]3CC[C@]12C.CCC(CC)(C/C=C\Br)O[Si](CC)(CC)CC>O1CCCC1>CCC(CC)(C/C=C\OC(C)(C)C1=CC[C@H]2C3=CC=C4C[C@@H](O[Si](C)(C)C(C)(C)C)C[C@H](O[Si](C)(C)C(C)(C)C)[C@]4(C)[C@H]3CC[C@]12C)O[Si](CC)(CC)CC
ord_dataset-c3a75813d0b24864aa4f7cd526efd6aa
ord-c425bee2d9844a92859ff71873587bbf
CC(C)(O)C1=CC[C@H]2C3=CC=C4C[C@@H](O[Si](C)(C)C(C)(C)C)C[C@H](O[Si](C)(C)C(C)(C)C)[C@]4(C)[C@H]3CC[C@]12C.CCC(CC)(C/C=C/Br)O[Si](CC)(CC)CC>>CCC(CC)(C/C=C/OC(C)(C)C1=CC[C@H]2C3=CC=C4C[C@@H](O[Si](C)(C)C(C)(C)C)C[C@H](O[Si](C)(C)C(C)(C)C)[C@]4(C)[C@H]3CC[C@]12C)O[Si](CC)(CC)CC
[Si](C)(C)(C(C)(C)C)O[C@H]1C[C@@H](CC2=CC=C3[C@@H]4CC=C(C(C)(C)O)[C@]4(CC[C@@H]3[C@@]12C)C)O[Si](C)(C)C(C)(C)C.Br\C=C\CC(CC)(O[Si](CC)(CC)CC)CC.[H-].[Na+].C1COCCOCCOCCOCCO1>>[Si](C)(C)(C(C)(C)C)O[C@H]1C[C@@H](CC2=CC=C3[C@@H]4CC=C(C(C)(C)O\C=C\CC(CC)(O[Si](CC)(CC)CC)CC)[C@]4(CC[C@@H]3[C@@]12C)C)O[Si](C)(C)C(C)(C)C
[OH:9][C:10]([CH3:11])([CH3:12])[C:13]1=[CH:14][CH2:15][C@H:16]2[C:17]3=[CH:18][CH:19]=[C:20]4[CH2:21][C@@H:22]([O:23][Si:24]([CH3:25])([CH3:26])[C:27]([CH3:28])([CH3:29])[CH3:30])[CH2:31][C@H:32]([O:33][Si:34]([CH3:35])([CH3:36])[C:37]([CH3:38])([CH3:39])[CH3:40])[C@:41]4([CH3:42])[C@H:43]3[CH2:44][CH2:45][C@:46]12[CH...
CC(C)(O)C1=CC[C@H]2C3=CC=C4C[C@@H](O[Si](C)(C)C(C)(C)C)C[C@H](O[Si](C)(C)C(C)(C)C)[C@]4(C)[C@H]3CC[C@]12C.CCC(CC)(C/C=C/Br)O[Si](CC)(CC)CC
CCC(CC)(C/C=C/OC(C)(C)C1=CC[C@H]2C3=CC=C4C[C@@H](O[Si](C)(C)C(C)(C)C)C[C@H](O[Si](C)(C)C(C)(C)C)[C@]4(C)[C@H]3CC[C@]12C)O[Si](CC)(CC)CC
null
null
O1CCCC1
Acylation
Williamson Ether Synthesis
3bebab49d1e73ccb378d80c964dd2eb3ac4ae759a028f210c53302497d420909
68002c25e6f3b076ffda77fb7b82207a1a988042aa4418cc4cd63986b874c804
C1=CC2CC[C@H]3C(=CC=C4CCCCC43)[C@@H]2C1
Br/[CH;D2;+0:1]=[C:2]/[C:3]-[C:4].[C:5]-[C:6]=[C:7](-[C:8](-[C;D1;H3:9])(-[C;D1;H3:10])-[OH;D1;+0:11])-[C:12]>>[C:5]-[C:6]=[C:7](-[C:8](-[C;D1;H3:9])(-[C;D1;H3:10])-[O;H0;D2;+0:11]/[CH;D2;+0:1]=[C:2]/[C:3]-[C:4])-[C:12]
62
[{"value": 62.0, "product": "[Si](C)(C)(C(C)(C)C)O[C@H]1C[C@@H](CC2=CC=C3[C@@H]4CC=C(C(C)(C)O\\C=C\\CC(CC)(O[Si](CC)(CC)CC)CC)[C@]4(CC[C@@H]3[C@@]12C)C)O[Si](C)(C)C(C)(C)C", "details": "PERCENTYIELD", "is_desired": false}, {"value": 61.6, "product": "[Si](C)(C)(C(C)(C)C)O[C@H]1C[C@@H](CC2=CC=C3[C@@H]4CC=C(C(C)(C)O\\C=C...
null
null
null
null
1α,3β-Bis(tert-butyldimethylsilyloxy)-20-hydroxy-20-methylpregna-5,7,16-triene (400 mg, 0.698 mmol), 1-bromo-4-ethyl-4-triethylsilyloxy-(2E)-hexene (0.897 g, 2.79 mmol), sodium hydride (60% in oil, 0.168 g, 4.188 mmol), 15-crown-5 (0.14 ml, 0.698 mmol) and tetrahydrofuran (12 ml) were subjected to reaction using a proc...
10.6084/m9.figshare.5104873.v1
null
Tertiary alcohol
Ether
null
null
C1=C[C@H]2CC[C@H]3C(=CC=C4CCCC[C@@H]43)[C@@H]2C1
HBr
O1CCCC1
null
null
CC(C)(O)C1=CC[C@H]2C3=CC=C4C[C@@H](O[Si](C)(C)C(C)(C)C)C[C@H](O[Si](C)(C)C(C)(C)C)[C@]4(C)[C@H]3CC[C@]12C.CCC(CC)(C/C=C/Br)O[Si](CC)(CC)CC>O1CCCC1>CCC(CC)(C/C=C/OC(C)(C)C1=CC[C@H]2C3=CC=C4C[C@@H](O[Si](C)(C)C(C)(C)C)C[C@H](O[Si](C)(C)C(C)(C)C)[C@]4(C)[C@H]3CC[C@]12C)O[Si](CC)(CC)CC
ord_dataset-c3a75813d0b24864aa4f7cd526efd6aa
ord-abf3dd53ffae4780b6342c0773508a49
CC(C)(O)COC(C)(C)C1=CC[C@H]2C3=CC=C4C[C@@H](O[Si](C)(C)C(C)(C)C)C[C@H](O[Si](C)(C)C(C)(C)C)[C@]4(C)[C@H]3CC[C@]12C>>CC(C)(O)COC(C)(C)C1=CC[C@H]2C3=CC=C4C[C@@H](O)C[C@H](O)[C@]4(C)[C@H]3CC[C@]12C
[Si](C)(C)(C(C)(C)C)O[C@H]1C[C@@H](CC2=CC=C3[C@@H]4CC=C(C(C)(C)OCC(C)(C)O)[C@]4(CC[C@@H]3[C@@]12C)C)O[Si](C)(C)C(C)(C)C.O1CCCC1.[F-].C(CCC)[N+](CCCC)(CCCC)CCCC>>O[C@H]1C[C@@H](CC2=CC=C3[C@@H]4CC=C(C(C)(C)OCC(C)(C)O)[C@]4(CC[C@@H]3[C@@]12C)C)O
CC(C)(C)[Si](C)(C)[O:20][C@@H:19]1[CH2:18][C:17]2=[CH:16][CH:15]=[C:14]3[C@@H:13]4[CH2:12][CH:11]=[C:10]([C:7]([O:6][CH2:5][C:2]([CH3:1])([CH3:3])[OH:4])([CH3:8])[CH3:9])[C@@:29]4([CH3:30])[CH2:28][CH2:27][C@@H:26]3[C@@:24]2([CH3:25])[C@@H:22]([O:23][Si](C)(C)C(C)(C)C)[CH2:21]1>>[CH3:1][C:2]([CH3:3])([OH:4])[CH2:5][O:6...
CC(C)(O)COC(C)(C)C1=CC[C@H]2C3=CC=C4C[C@@H](O[Si](C)(C)C(C)(C)C)C[C@H](O[Si](C)(C)C(C)(C)C)[C@]4(C)[C@H]3CC[C@]12C
CC(C)(O)COC(C)(C)C1=CC[C@H]2C3=CC=C4C[C@@H](O)C[C@H](O)[C@]4(C)[C@H]3CC[C@]12C
null
null
O1CCCC1
Deprotection
OtherReaction
3c4d3a3b788b4022df80488c890c930a0eff3addc93b825229adfe1b23285620
c96f1dab6a2ddd7b236398a198654bbc85e92a2fc2f6e88d092d4f9a3211cc52
C1=CC2CC[C@H]3C(=CC=C4CCCCC43)[C@@H]2C1
C-C(-C)(-C)-[Si](-C)(-C)-[O;H0;D2;+0:1]-[C:2]1-[C:3]-[C:4](=[C:5])-[C:6]-[C:7](-[O;H0;D2;+0:8]-[Si](-C)(-C)-C(-C)(-C)-C)-[C:9]-1>>[C:5]=[C:4]1-[C:3]-[C:2](-[OH;D1;+0:1])-[C:9]-[C:7](-[OH;D1;+0:8])-[C:6]-1
79
[{"value": 79.0, "product": "O[C@H]1C[C@@H](CC2=CC=C3[C@@H]4CC=C(C(C)(C)OCC(C)(C)O)[C@]4(CC[C@@H]3[C@@]12C)C)O", "details": "PERCENTYIELD", "is_desired": false}, {"value": 78.7, "product": "O[C@H]1C[C@@H](CC2=CC=C3[C@@H]4CC=C(C(C)(C)OCC(C)(C)O)[C@]4(CC[C@@H]3[C@@]12C)C)O", "details": "CALCULATEDPERCENTYIELD", "is_desir...
null
null
null
null
1α,3β-Bis(tert-butyldimethylsilyloxy)-20-(2-hydroxy-2-methylpropoxy)-20-methylpregna-5,7,16-triene (35.6 mg, 0.0552 mmol), a 1M tetra-n-butylammonium fluoride tetrahydrofuran solution (0.35 ml) and tetrahydrofuran (0.5 ml) were subjected to reaction using a procedure similar to that of Example 5(2) (reflux under heatin...
10.6084/m9.figshare.5104873.v1
null
TMS ether protective group.TMS ether protective group
Secondary alcohol.Secondary alcohol
null
null
C1=C[C@H]2CC[C@H]3C(=CC=C4CCCC[C@@H]43)[C@@H]2C1
Other
O1CCCC1
null
null
CC(C)(O)COC(C)(C)C1=CC[C@H]2C3=CC=C4C[C@@H](O[Si](C)(C)C(C)(C)C)C[C@H](O[Si](C)(C)C(C)(C)C)[C@]4(C)[C@H]3CC[C@]12C>O1CCCC1>CC(C)(O)COC(C)(C)C1=CC[C@H]2C3=CC=C4C[C@@H](O)C[C@H](O)[C@]4(C)[C@H]3CC[C@]12C
ord_dataset-c3a75813d0b24864aa4f7cd526efd6aa
ord-119241f1e30f4606852a9293fbdb4883
CCC(O)(CC)COC(C)(C)C1=CC[C@H]2C3=CC=C4C[C@@H](O[Si](C)(C)C(C)(C)C)C[C@H](O[Si](C)(C)C(C)(C)C)[C@]4(C)[C@H]3CC[C@]12C>>CCC(O)(CC)COC(C)(C)C1=CC[C@H]2C3=CC=C4C[C@@H](O)C[C@H](O)[C@]4(C)[C@H]3CC[C@]12C
[Si](C)(C)(C(C)(C)C)O[C@H]1C[C@@H](CC2=CC=C3[C@@H]4CC=C(C(C)(C)OCC(CC)(O)CC)[C@]4(CC[C@@H]3[C@@]12C)C)O[Si](C)(C)C(C)(C)C.O1CCCC1.[F-].C(CCC)[N+](CCCC)(CCCC)CCCC>>C(C)C(COC(C)(C1=CC[C@H]2C3=CC=C4C[C@H](C[C@@H]([C@]4(C)[C@H]3CC[C@]12C)O)O)C)(CC)O
CC(C)(C)[Si](C)(C)[O:22][C@@H:21]1[CH2:20][C:19]2=[CH:18][CH:17]=[C:16]3[C@@H:15]4[CH2:14][CH:13]=[C:12]([C:9]([O:8][CH2:7][C:3]([CH2:2][CH3:1])([OH:4])[CH2:5][CH3:6])([CH3:10])[CH3:11])[C@@:31]4([CH3:32])[CH2:30][CH2:29][C@@H:28]3[C@@:26]2([CH3:27])[C@@H:24]([O:25][Si](C)(C)C(C)(C)C)[CH2:23]1>>[CH3:1][CH2:2][C:3]([OH:...
CCC(O)(CC)COC(C)(C)C1=CC[C@H]2C3=CC=C4C[C@@H](O[Si](C)(C)C(C)(C)C)C[C@H](O[Si](C)(C)C(C)(C)C)[C@]4(C)[C@H]3CC[C@]12C
CCC(O)(CC)COC(C)(C)C1=CC[C@H]2C3=CC=C4C[C@@H](O)C[C@H](O)[C@]4(C)[C@H]3CC[C@]12C
null
null
O1CCCC1
Deprotection
OtherReaction
3c4d3a3b788b4022df80488c890c930a0eff3addc93b825229adfe1b23285620
c96f1dab6a2ddd7b236398a198654bbc85e92a2fc2f6e88d092d4f9a3211cc52
C1=CC2CC[C@H]3C(=CC=C4CCCCC43)[C@@H]2C1
C-C(-C)(-C)-[Si](-C)(-C)-[O;H0;D2;+0:1]-[C:2]1-[C:3]-[C:4](=[C:5])-[C:6]-[C:7](-[O;H0;D2;+0:8]-[Si](-C)(-C)-C(-C)(-C)-C)-[C:9]-1>>[C:5]=[C:4]1-[C:3]-[C:2](-[OH;D1;+0:1])-[C:9]-[C:7](-[OH;D1;+0:8])-[C:6]-1
94
[{"value": 94.0, "product": "C(C)C(COC(C)(C1=CC[C@H]2C3=CC=C4C[C@H](C[C@@H]([C@]4(C)[C@H]3CC[C@]12C)O)O)C)(CC)O", "details": "PERCENTYIELD", "is_desired": false}, {"value": 93.7, "product": "C(C)C(COC(C)(C1=CC[C@H]2C3=CC=C4C[C@H](C[C@@H]([C@]4(C)[C@H]3CC[C@]12C)O)O)C)(CC)O", "details": "CALCULATEDPERCENTYIELD", "is_des...
null
null
null
null
1α,3β-Bis(tert-butyldimethylsilyloxy)-20-(2-ethyl-2-hydroxybutoxy)-20-methylpregna-5,7,16-triene (32.0 mg, 0.0475 mmol), a 1M tetra-n-butylammonium fluoride tetrahydrofuran solution (0.3 ml, 0.3 mmol) and tetrahydrofuran (0.5 ml) were subjected to reaction using a procedure similar to that of Example 5(2) (reflux under...
10.6084/m9.figshare.5104873.v1
null
TMS ether protective group.TMS ether protective group
Secondary alcohol.Secondary alcohol
null
null
C1=C[C@H]2CC[C@H]3C(=CC=C4CCCC[C@@H]43)[C@@H]2C1
Other
O1CCCC1
null
null
CCC(O)(CC)COC(C)(C)C1=CC[C@H]2C3=CC=C4C[C@@H](O[Si](C)(C)C(C)(C)C)C[C@H](O[Si](C)(C)C(C)(C)C)[C@]4(C)[C@H]3CC[C@]12C>O1CCCC1>CCC(O)(CC)COC(C)(C)C1=CC[C@H]2C3=CC=C4C[C@@H](O)C[C@H](O)[C@]4(C)[C@H]3CC[C@]12C
ord_dataset-c3a75813d0b24864aa4f7cd526efd6aa
ord-805121a5f5d34460872e41c108db4b33
CC(C)(C)[Si](C)(C)O[C@@H]1CC2=CC=C3[C@H](CC[C@]4(C)C(CO)=CC[C@@H]34)[C@@]2(C)[C@@H](O[Si](C)(C)C(C)(C)C)C1.CC1(C)OC1CBr>>CC1(C)OC1COCC1=CC[C@H]2C3=CC=C4C[C@@H](O[Si](C)(C)C(C)(C)C)C[C@H](O[Si](C)(C)C(C)(C)C)[C@]4(C)[C@H]3CC[C@]12C
[Si](C)(C)(C(C)(C)C)O[C@H]1C[C@@H](CC2=CC=C3[C@@H]4CC=C([C@@]4(C)CC[C@@H]3[C@@]12C)CO)O[Si](C)(C)C(C)(C)C.[H-].[Na+].BrCC1C(C)(C)O1>>[Si](C)(C)(C(C)(C)C)O[C@H]1C[C@@H](CC2=CC=C3[C@@H]4CC=C([C@@]4(C)CC[C@@H]3[C@@]12C)COCC1C(C)(C)O1)O[Si](C)(C)C(C)(C)C
[OH:7][CH2:8][C:9]1=[CH:10][CH2:11][C@H:12]2[C:13]3=[CH:14][CH:15]=[C:16]4[CH2:17][C@@H:18]([O:19][Si:20]([CH3:21])([CH3:22])[C:23]([CH3:24])([CH3:25])[CH3:26])[CH2:27][C@H:28]([O:29][Si:30]([CH3:31])([CH3:32])[C:33]([CH3:34])([CH3:35])[CH3:36])[C@:37]4([CH3:38])[C@H:39]3[CH2:40][CH2:41][C@:42]12[CH3:43].Br[CH2:6][CH:5...
CC(C)(C)[Si](C)(C)O[C@@H]1CC2=CC=C3[C@H](CC[C@]4(C)C(CO)=CC[C@@H]34)[C@@]2(C)[C@@H](O[Si](C)(C)C(C)(C)C)C1.CC1(C)OC1CBr
CC1(C)OC1COCC1=CC[C@H]2C3=CC=C4C[C@@H](O[Si](C)(C)C(C)(C)C)C[C@H](O[Si](C)(C)C(C)(C)C)[C@]4(C)[C@H]3CC[C@]12C
null
null
O1CCCC1.C(C)(=O)OCC
Heteroatom Alkylation and Arylation
Williamson Ether Synthesis
dd3f9c60e1f90d961a7c01d970ae213561355ee1451f276a3b04696e4b6fae5c
46a6e883cf919b4006e69abfdfd883f458f55c08b3200960c6a5b57c4139fbca
C1=C(COCC2CO2)C2CC[C@H]3C(=CC=C4CCCCC43)[C@@H]2C1
Br-[CH2;D2;+0:1]-[C:2]1-[#8:3]-[C:4]-1.[C:5]-[C:6]=[C:7](-[C:8]-[OH;D1;+0:9])-[C:10]>>[C:5]-[C:6]=[C:7](-[C:8]-[O;H0;D2;+0:9]-[CH2;D2;+0:1]-[C:2]1-[#8:3]-[C:4]-1)-[C:10]
81.1
[{"value": 81.0, "product": "[Si](C)(C)(C(C)(C)C)O[C@H]1C[C@@H](CC2=CC=C3[C@@H]4CC=C([C@@]4(C)CC[C@@H]3[C@@]12C)COCC1C(C)(C)O1)O[Si](C)(C)C(C)(C)C", "details": "PERCENTYIELD", "is_desired": false}, {"value": 81.1, "product": "[Si](C)(C)(C(C)(C)C)O[C@H]1C[C@@H](CC2=CC=C3[C@@H]4CC=C([C@@]4(C)CC[C@@H]3[C@@]12C)COCC1C(C)(C...
null
null
null
null
A solution of 1α,3β-bis(tert-butyldimethylsilyloxy)-17-(hydroxymethyl)androsta-5,7,16-triene (51.6 mg, 0.0947 mmol), sodium hydride (95%, 21.1 mg, 0.879 mmol) and 1-bromo-2,3-epoxy-3-methylbutane (91.2 mg, 0.553 mmol) in tetrahydrofuran (1 ml) was stirred at room temperature for 20 min. and refluxed under heating for 2...
10.6084/m9.figshare.5104873.v1
null
Primary halide.Primary alcohol
Ether
null
null
C1CO1.C1=C[C@H]2CC[C@H]3C(=CC=C4CCCC[C@@H]43)[C@@H]2C1
HBr
O1CCCC1.C(C)(=O)OCC
null
null
CC(C)(C)[Si](C)(C)O[C@@H]1CC2=CC=C3[C@H](CC[C@]4(C)C(CO)=CC[C@@H]34)[C@@]2(C)[C@@H](O[Si](C)(C)C(C)(C)C)C1.CC1(C)OC1CBr>O1CCCC1.C(C)(=O)OCC>CC1(C)OC1COCC1=CC[C@H]2C3=CC=C4C[C@@H](O[Si](C)(C)C(C)(C)C)C[C@H](O[Si](C)(C)C(C)(C)C)[C@]4(C)[C@H]3CC[C@]12C
ord_dataset-c3a75813d0b24864aa4f7cd526efd6aa
ord-c7fd4f7d8e38425ba62bc91da9c29ed4
CC1(C)OC1COCC1=CC[C@H]2C3=CC=C4C[C@@H](O[Si](C)(C)C(C)(C)C)C[C@H](O[Si](C)(C)C(C)(C)C)[C@]4(C)[C@H]3CC[C@]12C>>CC(C)(O)CCOCC1=CC[C@H]2C3=CC=C4C[C@@H](O[Si](C)(C)C(C)(C)C)C[C@H](O[Si](C)(C)C(C)(C)C)[C@]4(C)[C@H]3CC[C@]12C
CCC([BH-](C(CC)C)C(CC)C)C.[Li+].[Si](C)(C)(C(C)(C)C)O[C@H]1C[C@@H](CC2=CC=C3[C@@H]4CC=C([C@@]4(C)CC[C@@H]3[C@@]12C)COCC1C(C)(C)O1)O[Si](C)(C)C(C)(C)C.CCC([BH-](C(CC)C)C(CC)C)C.[Li+].[OH-].[Na+].OO>>[Si](C)(C)(C(C)(C)C)O[C@H]1C[C@@H](CC2=CC=C3[C@@H]4CC=C([C@@]4(C)CC[C@@H]3[C@@]12C)COCCC(C)(C)O)O[Si](C)(C)C(C)(C)C
[CH3:1][C:2]1([CH3:3])[O:4][CH:5]1[CH2:6][O:7][CH2:8][C:9]1=[CH:10][CH2:11][C@H:12]2[C:13]3=[CH:14][CH:15]=[C:16]4[CH2:17][C@@H:18]([O:19][Si:20]([CH3:21])([CH3:22])[C:23]([CH3:24])([CH3:25])[CH3:26])[CH2:27][C@H:28]([O:29][Si:30]([CH3:31])([CH3:32])[C:33]([CH3:34])([CH3:35])[CH3:36])[C@:37]4([CH3:38])[C@H:39]3[CH2:40]...
CC1(C)OC1COCC1=CC[C@H]2C3=CC=C4C[C@@H](O[Si](C)(C)C(C)(C)C)C[C@H](O[Si](C)(C)C(C)(C)C)[C@]4(C)[C@H]3CC[C@]12C
CC(C)(O)CCOCC1=CC[C@H]2C3=CC=C4C[C@@H](O[Si](C)(C)C(C)(C)C)C[C@H](O[Si](C)(C)C(C)(C)C)[C@]4(C)[C@H]3CC[C@]12C
null
null
O1CCCC1.C(C)(=O)OCC
Reduction
OtherReaction
fb68e1f7e7aa0012b71755c2e659c5ca3af240790d29315ee068c102a1263dc2
ac77f1c31bbb4f9df2f7d9b876f6243f6ca37479f36d1e779ab0e1e90922def4
C1=CC2CC[C@H]3C(=CC=C4CCCCC43)[C@@H]2C1
[#8:1]-[C:2]-[CH;D3;+0:3]1-[O;H0;D2;+0:4]-[C:5]-1(-[C;D1;H3:6])-[C;D1;H3:7]>>[#8:1]-[C:2]-[CH2;D2;+0:3]-[C:5](-[C;D1;H3:6])(-[C;D1;H3:7])-[OH;D1;+0:4]
87
[{"value": 87.0, "product": "[Si](C)(C)(C(C)(C)C)O[C@H]1C[C@@H](CC2=CC=C3[C@@H]4CC=C([C@@]4(C)CC[C@@H]3[C@@]12C)COCCC(C)(C)O)O[Si](C)(C)C(C)(C)C", "details": "PERCENTYIELD", "is_desired": false}, {"value": 86.7, "product": "[Si](C)(C)(C(C)(C)C)O[C@H]1C[C@@H](CC2=CC=C3[C@@H]4CC=C([C@@]4(C)CC[C@@H]3[C@@]12C)COCCC(C)(C)O)...
null
null
1
HOUR
At room temperature, a solution of 1.0M L-SELECTRIDE in tetrahydrofuran (0.25 ml, 0.25 mmol) was added to a solution of 1α,3β-bis(tert-butyldimethylsilyloxy)-17-(2,3-epoxy-3-methylbutoxymethyl)androsta-5,7,16-triene (48.3 mg, 0.0768 mmol) in tetrahydrofuran (2 ml) and stirred at the same temperature for 1 hour. To the ...
10.6084/m9.figshare.5104873.v1
null
Ether
Tertiary alcohol
C1CO1
null
C1=C[C@H]2CC[C@H]3C(=CC=C4CCCC[C@@H]43)[C@@H]2C1
null
O1CCCC1.C(C)(=O)OCC
null
1
CC1(C)OC1COCC1=CC[C@H]2C3=CC=C4C[C@@H](O[Si](C)(C)C(C)(C)C)C[C@H](O[Si](C)(C)C(C)(C)C)[C@]4(C)[C@H]3CC[C@]12C>O1CCCC1.C(C)(=O)OCC>CC(C)(O)CCOCC1=CC[C@H]2C3=CC=C4C[C@@H](O[Si](C)(C)C(C)(C)C)C[C@H](O[Si](C)(C)C(C)(C)C)[C@]4(C)[C@H]3CC[C@]12C
ord_dataset-c3a75813d0b24864aa4f7cd526efd6aa
ord-d8d9b3d9d69d439b898cc3da5dad74d8
CC(C)(O)CCOCC1=CC[C@H]2C3=CC=C4C[C@@H](O[Si](C)(C)C(C)(C)C)C[C@H](O[Si](C)(C)C(C)(C)C)[C@]4(C)[C@H]3CC[C@]12C>>CC(C)(O)CCOCC1=CC[C@H]2C3=CC=C4C[C@@H](O)C[C@H](O)[C@]4(C)[C@H]3CC[C@]12C
[Si](C)(C)(C(C)(C)C)O[C@H]1C[C@@H](CC2=CC=C3[C@@H]4CC=C([C@@]4(C)CC[C@@H]3[C@@]12C)COCCC(C)(C)O)O[Si](C)(C)C(C)(C)C.O1CCCC1.[F-].C(CCC)[N+](CCCC)(CCCC)CCCC>>O[C@H]1C[C@@H](CC2=CC=C3[C@@H]4CC=C([C@@]4(C)CC[C@@H]3[C@@]12C)COCCC(C)(C)O)O
CC(C)(C)[Si](C)(C)[O:19][C@@H:18]1[CH2:17][C:16]2=[CH:15][CH:14]=[C:13]3[C@@H:12]4[CH2:11][CH:10]=[C:9]([CH2:8][O:7][CH2:6][CH2:5][C:2]([CH3:1])([CH3:3])[OH:4])[C@@:28]4([CH3:29])[CH2:27][CH2:26][C@@H:25]3[C@@:23]2([CH3:24])[C@@H:21]([O:22][Si](C)(C)C(C)(C)C)[CH2:20]1>>[CH3:1][C:2]([CH3:3])([OH:4])[CH2:5][CH2:6][O:7][C...
CC(C)(O)CCOCC1=CC[C@H]2C3=CC=C4C[C@@H](O[Si](C)(C)C(C)(C)C)C[C@H](O[Si](C)(C)C(C)(C)C)[C@]4(C)[C@H]3CC[C@]12C
CC(C)(O)CCOCC1=CC[C@H]2C3=CC=C4C[C@@H](O)C[C@H](O)[C@]4(C)[C@H]3CC[C@]12C
null
null
null
Deprotection
OtherReaction
3c4d3a3b788b4022df80488c890c930a0eff3addc93b825229adfe1b23285620
c96f1dab6a2ddd7b236398a198654bbc85e92a2fc2f6e88d092d4f9a3211cc52
C1=CC2CC[C@H]3C(=CC=C4CCCCC43)[C@@H]2C1
C-C(-C)(-C)-[Si](-C)(-C)-[O;H0;D2;+0:1]-[C:2]1-[C:3]-[C:4](=[C:5])-[C:6]-[C:7](-[O;H0;D2;+0:8]-[Si](-C)(-C)-C(-C)(-C)-C)-[C:9]-1>>[C:5]=[C:4]1-[C:3]-[C:2](-[OH;D1;+0:1])-[C:9]-[C:7](-[OH;D1;+0:8])-[C:6]-1
82
[{"value": 82.0, "product": "O[C@H]1C[C@@H](CC2=CC=C3[C@@H]4CC=C([C@@]4(C)CC[C@@H]3[C@@]12C)COCCC(C)(C)O)O", "details": "PERCENTYIELD", "is_desired": false}, {"value": 81.9, "product": "O[C@H]1C[C@@H](CC2=CC=C3[C@@H]4CC=C([C@@]4(C)CC[C@@H]3[C@@]12C)COCCC(C)(C)O)O", "details": "CALCULATEDPERCENTYIELD", "is_desired": fal...
null
null
null
null
1α,3β-Bis(tert-butyldimethylsilyloxy)-17-(3-hydroxy-3-methylbutoxymethyl)androsta-5,7,16-triene (40.0 mg, 0.0634 mmol) and a 1M tetra-n-butylammonium fluoride tetrahydrofuran solution (0.4 ml, 0.4 mmol) were subjected to reaction using a procedure similar to that of Example 5(2) (reflux under heating for 1 hour), worke...
10.6084/m9.figshare.5104873.v1
null
TMS ether protective group.TMS ether protective group
Secondary alcohol.Secondary alcohol
null
null
C1=C[C@H]2CC[C@H]3C(=CC=C4CCCC[C@@H]43)[C@@H]2C1
Other
null
null
null
CC(C)(O)CCOCC1=CC[C@H]2C3=CC=C4C[C@@H](O[Si](C)(C)C(C)(C)C)C[C@H](O[Si](C)(C)C(C)(C)C)[C@]4(C)[C@H]3CC[C@]12C>>CC(C)(O)CCOCC1=CC[C@H]2C3=CC=C4C[C@@H](O)C[C@H](O)[C@]4(C)[C@H]3CC[C@]12C
ord_dataset-c3a75813d0b24864aa4f7cd526efd6aa
ord-fcbac95b81c24dac8b57a9b0f6fda1a1
CC(C)(O)C1=CC[C@H]2C3=CC=C4C[C@@H](O[Si](C)(C)C(C)(C)C)C[C@H](O[Si](C)(C)C(C)(C)C)[C@]4(C)[C@H]3CC[C@]12C.CC1(C)OC1CBr>>CC(C)(O)CCOC(C)(C)C1=CC[C@H]2C3=CC=C4C[C@@H](O[Si](C)(C)C(C)(C)C)C[C@H](O[Si](C)(C)C(C)(C)C)[C@]4(C)[C@H]3CC[C@]12C
CCC([BH-](C(CC)C)C(CC)C)C.[Li+].O1CCCC1.[Si](C)(C)(C(C)(C)C)O[C@H]1C[C@@H](CC2=CC=C3[C@@H]4CC=C(C(C)(C)O)[C@]4(CC[C@@H]3[C@@]12C)C)O[Si](C)(C)C(C)(C)C.[H-].[Na+].BrCC1C(C)(C)O1.[OH-].[Na+].OO>>[Si](C)(C)(C(C)(C)C)O[C@H]1C[C@@H](CC2=CC=C3[C@@H]4CC=C(C(C)(C)OCCC(C)(C)O)[C@]4(CC[C@@H]3[C@@]12C)C)O[Si](C)(C)C(C)(C)C
[OH:7][C:8]([CH3:9])([CH3:10])[C:11]1=[CH:12][CH2:13][C@H:14]2[C:15]3=[CH:16][CH:17]=[C:18]4[CH2:19][C@@H:20]([O:21][Si:22]([CH3:23])([CH3:24])[C:25]([CH3:26])([CH3:27])[CH3:28])[CH2:29][C@H:30]([O:31][Si:32]([CH3:33])([CH3:34])[C:35]([CH3:36])([CH3:37])[CH3:38])[C@:39]4([CH3:40])[C@H:41]3[CH2:42][CH2:43][C@:44]12[CH3:...
CC(C)(O)C1=CC[C@H]2C3=CC=C4C[C@@H](O[Si](C)(C)C(C)(C)C)C[C@H](O[Si](C)(C)C(C)(C)C)[C@]4(C)[C@H]3CC[C@]12C.CC1(C)OC1CBr
CC(C)(O)CCOC(C)(C)C1=CC[C@H]2C3=CC=C4C[C@@H](O[Si](C)(C)C(C)(C)C)C[C@H](O[Si](C)(C)C(C)(C)C)[C@]4(C)[C@H]3CC[C@]12C
null
null
O1CCCC1.C(C)(=O)OCC
Heteroatom Alkylation and Arylation
OtherReaction
582d7d0e2791030ab802c70e7bf642b8dfc7e3c25a708cf942edeab4e0e6f0ef
826d1333eb2b345d0c50f458d857543fab5b748885fcae047c31a1171432bf9d
C1=CC2CC[C@H]3C(=CC=C4CCCCC43)[C@@H]2C1
Br-[CH2;D2;+0:1]-[CH;D3;+0:2]1-[O;H0;D2;+0:3]-[C:4]-1(-[C;D1;H3:5])-[C;D1;H3:6].[C:7]-[C:8]=[C:9](-[C:10](-[C;D1;H3:11])(-[C;D1;H3:12])-[OH;D1;+0:13])-[C:14]>>[C:7]-[C:8]=[C:9](-[C:10](-[C;D1;H3:11])(-[C;D1;H3:12])-[O;H0;D2;+0:13]-[CH2;D2;+0:1]-[CH2;D2;+0:2]-[C:4](-[C;D1;H3:5])(-[C;D1;H3:6])-[OH;D1;+0:3])-[C:14]
93.2
[{"value": 93.0, "product": "[Si](C)(C)(C(C)(C)C)O[C@H]1C[C@@H](CC2=CC=C3[C@@H]4CC=C(C(C)(C)OCCC(C)(C)O)[C@]4(CC[C@@H]3[C@@]12C)C)O[Si](C)(C)C(C)(C)C", "details": "PERCENTYIELD", "is_desired": false}, {"value": 93.2, "product": "[Si](C)(C)(C(C)(C)C)O[C@H]1C[C@@H](CC2=CC=C3[C@@H]4CC=C(C(C)(C)OCCC(C)(C)O)[C@]4(CC[C@@H]3[...
null
null
12
HOUR
A solution of 1α,3β-bis(tert-butyldimethylsilyloxy)-20-hydroxy-20-methylpregna-5,7,16-triene (67.7 mg, 0.118 mmol), sodium hydride (60% in oil, 40.0 mg, 1.00 mmol) and 1-bromo-2,3-epoxy-3-methylbutane (100 mg, 0.606 mmol) in tetrahydrofuran (1 ml) was refluxed under heating for 1.5 hours. To the thus obtained reaction ...
10.6084/m9.figshare.5104873.v1
null
Primary halide.Ether.Tertiary alcohol
Ether.Tertiary alcohol
C1CO1
null
C1=C[C@H]2CC[C@H]3C(=CC=C4CCCC[C@@H]43)[C@@H]2C1
Br-
O1CCCC1.C(C)(=O)OCC
null
12
CC(C)(O)C1=CC[C@H]2C3=CC=C4C[C@@H](O[Si](C)(C)C(C)(C)C)C[C@H](O[Si](C)(C)C(C)(C)C)[C@]4(C)[C@H]3CC[C@]12C.CC1(C)OC1CBr>O1CCCC1.C(C)(=O)OCC>CC(C)(O)CCOC(C)(C)C1=CC[C@H]2C3=CC=C4C[C@@H](O[Si](C)(C)C(C)(C)C)C[C@H](O[Si](C)(C)C(C)(C)C)[C@]4(C)[C@H]3CC[C@]12C
ord_dataset-c3a75813d0b24864aa4f7cd526efd6aa
ord-535b11fdc0c14b828a6d5ca418dab416
C=CC(=O)N(C)C.CC(C)(C)[Si](C)(C)O[C@@H]1CC2=CC=C3[C@H](CC[C@]4(C)C(CO)=CC[C@@H]34)[C@@]2(C)[C@@H](O[Si](C)(C)C(C)(C)C)C1>>CN(C)C(=O)CCOCC1=CC[C@H]2C3=CC=C4C[C@@H](O[Si](C)(C)C(C)(C)C)C[C@H](O[Si](C)(C)C(C)(C)C)[C@]4(C)[C@H]3CC[C@]12C
[Cl-].[NH4+].CN(C(C=C)=O)C.[Si](C)(C)(C(C)(C)C)O[C@H]1C[C@@H](CC2=CC=C3[C@@H]4CC=C([C@@]4(C)CC[C@@H]3[C@@]12C)CO)O[Si](C)(C)C(C)(C)C.[H-].[Na+]>>[Si](C)(C)(C(C)(C)C)O[C@H]1C[C@@H](CC2=CC=C3[C@@H]4CC=C([C@@]4(C)CC[C@@H]3[C@@]12C)COCCC(=O)N(C)C)O[Si](C)(C)C(C)(C)C
[CH3:1][N:2]([CH3:3])[C:4](=[O:5])[CH:6]=[CH2:7].[OH:8][CH2:9][C:10]1=[CH:11][CH2:12][C@H:13]2[C:14]3=[CH:15][CH:16]=[C:17]4[CH2:18][C@@H:19]([O:20][Si:21]([CH3:22])([CH3:23])[C:24]([CH3:25])([CH3:26])[CH3:27])[CH2:28][C@H:29]([O:30][Si:31]([CH3:32])([CH3:33])[C:34]([CH3:35])([CH3:36])[CH3:37])[C@:38]4([CH3:39])[C@H:40...
C=CC(=O)N(C)C.CC(C)(C)[Si](C)(C)O[C@@H]1CC2=CC=C3[C@H](CC[C@]4(C)C(CO)=CC[C@@H]34)[C@@]2(C)[C@@H](O[Si](C)(C)C(C)(C)C)C1
CN(C)C(=O)CCOCC1=CC[C@H]2C3=CC=C4C[C@@H](O[Si](C)(C)C(C)(C)C)C[C@H](O[Si](C)(C)C(C)(C)C)[C@]4(C)[C@H]3CC[C@]12C
null
null
O1CCCC1
Heteroatom Alkylation and Arylation
oxa-Michael addition
f7c7da7c78eb65b9b2c8f63d0f16c4d5887e45e01ac1a9ea608f777c535e8cd7
d7c87de309863ac8797e1e336d1d5992291f9ca863376e68ebcf1e8fd5f0e442
C1=CC2CC[C@H]3C(=CC=C4CCCCC43)[C@@H]2C1
[C;D1;H3:1]-[#7:2](-[C;D1;H3:3])-[C:4](=[O;D1;H0:5])-[CH;D2;+0:6]=[CH2;D1;+0:7].[C:8]-[C:9]=[C:10](-[C:11]-[OH;D1;+0:12])-[C:13]>>[C:8]-[C:9]=[C:10](-[C:11]-[O;H0;D2;+0:12]-[CH2;D2;+0:7]-[CH2;D2;+0:6]-[C:4](=[O;D1;H0:5])-[#7:2](-[C;D1;H3:1])-[C;D1;H3:3])-[C:13]
93.2
[{"value": 92.7, "product": "[Si](C)(C)(C(C)(C)C)O[C@H]1C[C@@H](CC2=CC=C3[C@@H]4CC=C([C@@]4(C)CC[C@@H]3[C@@]12C)COCCC(=O)N(C)C)O[Si](C)(C)C(C)(C)C", "details": "PERCENTYIELD", "is_desired": false}, {"value": 93.2, "product": "[Si](C)(C)(C(C)(C)C)O[C@H]1C[C@@H](CC2=CC=C3[C@@H]4CC=C([C@@]4(C)CC[C@@H]3[C@@]12C)COCCC(=O)N(...
null
null
30
MINUTE
To a solution of 1α,3β-bis(tert-butyldimethylsilyloxy)-17-hydroxymethylandrosta-5,7,16-triene (951 mg, 1.75 mmol) in tetrahydrofuran (17.5 ml), was added sodium hydride (60% in oil, 105 mg, 2.62 mmol), followed by stirring under nitrogen stream at room temperature for 30 min. After adding N,N-dimethylacrylamide (540 mg...
10.6084/m9.figshare.5104873.v1
null
Primary alcohol.Vinyl
Ether
null
null
C1=C[C@H]2CC[C@H]3C(=CC=C4CCCC[C@@H]43)[C@@H]2C1
null
O1CCCC1
null
0.5
C=CC(=O)N(C)C.CC(C)(C)[Si](C)(C)O[C@@H]1CC2=CC=C3[C@H](CC[C@]4(C)C(CO)=CC[C@@H]34)[C@@]2(C)[C@@H](O[Si](C)(C)C(C)(C)C)C1>O1CCCC1>CN(C)C(=O)CCOCC1=CC[C@H]2C3=CC=C4C[C@@H](O[Si](C)(C)C(C)(C)C)C[C@H](O[Si](C)(C)C(C)(C)C)[C@]4(C)[C@H]3CC[C@]12C
ord_dataset-c3a75813d0b24864aa4f7cd526efd6aa
ord-aa466e4402f844efbbd164d3cf1c23bb
CN(C)C(=O)CCOCC1=CC[C@H]2C3=CC=C4C[C@@H](O[Si](C)(C)C(C)(C)C)C[C@H](O[Si](C)(C)C(C)(C)C)[C@]4(C)[C@H]3CC[C@]12C>>CCC(O)(CC)CCOCC1=CC[C@H]2C3=CC=C4C[C@@H](O[Si](C)(C)C(C)(C)C)C[C@H](O[Si](C)(C)C(C)(C)C)[C@]4(C)[C@H]3CC[C@]12C
[Cl-].[NH4+].Cl[Ce](Cl)Cl.O1CCCC1.C(C)[Mg]Br.[Si](C)(C)(C(C)(C)C)O[C@H]1C[C@@H](CC2=CC=C3[C@@H]4CC=C([C@@]4(C)CC[C@@H]3[C@@]12C)COCCC(=O)N(C)C)O[Si](C)(C)C(C)(C)C.O1CCCC1>>[Si](C)(C)(C(C)(C)C)O[C@H]1C[C@@H](CC2=CC=C3[C@@H]4CC=C([C@@]4(C)CC[C@@H]3[C@@]12C)COCCC(CC)(O)CC)O[Si](C)(C)C(C)(C)C
CN([C:3](=[O:4])[CH2:7][CH2:8][O:9][CH2:10][C:11]1=[CH:12][CH2:13][C@H:14]2[C:15]3=[CH:16][CH:17]=[C:18]4[CH2:19][C@@H:20]([O:21][Si:22]([CH3:23])([CH3:24])[C:25]([CH3:26])([CH3:27])[CH3:28])[CH2:29][C@H:30]([O:31][Si:32]([CH3:33])([CH3:34])[C:35]([CH3:36])([CH3:37])[CH3:38])[C@:39]4([CH3:40])[C@H:41]3[CH2:42][CH2:43][...
CN(C)C(=O)CCOCC1=CC[C@H]2C3=CC=C4C[C@@H](O[Si](C)(C)C(C)(C)C)C[C@H](O[Si](C)(C)C(C)(C)C)[C@]4(C)[C@H]3CC[C@]12C
CCC(O)(CC)CCOCC1=CC[C@H]2C3=CC=C4C[C@@H](O[Si](C)(C)C(C)(C)C)C[C@H](O[Si](C)(C)C(C)(C)C)[C@]4(C)[C@H]3CC[C@]12C
null
null
null
Functional Group Interconversion
OtherReaction
4e89bd3b6f1dae16ca265385a8e13d357db2ec6b1542aa318708859fb61ad9eb
4d5323d9e013bb3a490067f70b6ce5c7da5f30c3fdbeb30b2d6862dc3cd4bb84
C1=CC2CC[C@H]3C(=CC=C4CCCCC43)[C@@H]2C1
C-N(-[CH3;D1;+0:1])-[C;H0;D3;+0:2](=[O;H0;D1;+0:3])-[C:4]-[C:5]>>[C:5]-[C:4]-[C;H0;D4;+0:2](-[OH;D1;+0:3])(-[C:6]-[C;D1;H3:7])-[C:8]-[CH3;D1;+0:1]
56
[{"value": 56.0, "product": "[Si](C)(C)(C(C)(C)C)O[C@H]1C[C@@H](CC2=CC=C3[C@@H]4CC=C([C@@]4(C)CC[C@@H]3[C@@]12C)COCCC(CC)(O)CC)O[Si](C)(C)C(C)(C)C", "details": "PERCENTYIELD", "is_desired": false}]
null
null
30
MINUTE
Tetrahydrofuran (11 ml) was mixed with anhydrous cerous (III) chloride (2.33 g, 9.46 mmol), stirred under nitrogen stream at room temperature for 30 min., cooled with ice, mixed with ethylmagnesium bromide (0.96 mol/l, 9.0 ml, 8.6 mmol) and stirred for 30 min. The reaction solution was mixed with a solution of 1α,3β-bi...
10.6084/m9.figshare.5104873.v1
null
Tertiary amide
Tertiary alcohol
null
null
C1=C[C@H]2CC[C@H]3C(=CC=C4CCCC[C@@H]43)[C@@H]2C1
null
null
null
0.5
CN(C)C(=O)CCOCC1=CC[C@H]2C3=CC=C4C[C@@H](O[Si](C)(C)C(C)(C)C)C[C@H](O[Si](C)(C)C(C)(C)C)[C@]4(C)[C@H]3CC[C@]12C>>CCC(O)(CC)CCOCC1=CC[C@H]2C3=CC=C4C[C@@H](O[Si](C)(C)C(C)(C)C)C[C@H](O[Si](C)(C)C(C)(C)C)[C@]4(C)[C@H]3CC[C@]12C
ord_dataset-c3a75813d0b24864aa4f7cd526efd6aa
ord-57fc10183ae24c289d5d5e52fdec0be2
C=CC(=O)N(C)C.CC(C)(O)C1=CC[C@H]2C3=CC=C4C[C@@H](O[Si](C)(C)C(C)(C)C)C[C@H](O[Si](C)(C)C(C)(C)C)[C@]4(C)[C@H]3CC[C@]12C>>CN(C)C(=O)CCOC(C)(C)C1=CC[C@H]2C3=CC=C4C[C@@H](O[Si](C)(C)C(C)(C)C)C[C@H](O[Si](C)(C)C(C)(C)C)[C@]4(C)[C@H]3CC[C@]12C
[Si](C)(C)(C(C)(C)C)O[C@H]1C[C@@H](CC2=CC=C3[C@@H]4CC=C(C(C)(C)O)[C@]4(CC[C@@H]3[C@@]12C)C)O[Si](C)(C)C(C)(C)C.CN(C(C=C)=O)C.[H-].[Na+]>>[Si](C)(C)(C(C)(C)C)O[C@H]1C[C@@H](CC2=CC=C3[C@@H]4CC=C(C(C)(C)OCCC(=O)N(C)C)[C@]4(CC[C@@H]3[C@@]12C)C)O[Si](C)(C)C(C)(C)C
[CH3:1][N:2]([CH3:3])[C:4](=[O:5])[CH:6]=[CH2:7].[OH:8][C:9]([CH3:10])([CH3:11])[C:12]1=[CH:13][CH2:14][C@H:15]2[C:16]3=[CH:17][CH:18]=[C:19]4[CH2:20][C@@H:21]([O:22][Si:23]([CH3:24])([CH3:25])[C:26]([CH3:27])([CH3:28])[CH3:29])[CH2:30][C@H:31]([O:32][Si:33]([CH3:34])([CH3:35])[C:36]([CH3:37])([CH3:38])[CH3:39])[C@:40]...
C=CC(=O)N(C)C.CC(C)(O)C1=CC[C@H]2C3=CC=C4C[C@@H](O[Si](C)(C)C(C)(C)C)C[C@H](O[Si](C)(C)C(C)(C)C)[C@]4(C)[C@H]3CC[C@]12C
CN(C)C(=O)CCOC(C)(C)C1=CC[C@H]2C3=CC=C4C[C@@H](O[Si](C)(C)C(C)(C)C)C[C@H](O[Si](C)(C)C(C)(C)C)[C@]4(C)[C@H]3CC[C@]12C
null
null
O1CCCC1
Heteroatom Alkylation and Arylation
oxa-Michael addition
714eaa0e6de1d85d58a88133b4d5e95857344ec278e90cde0496674a55b79739
ea8641c928da9fe5f2bca5bb859dbb223e9e99eefdf70a15450fd2e768112e0a
C1=CC2CC[C@H]3C(=CC=C4CCCCC43)[C@@H]2C1
[C;D1;H3:1]-[#7:2](-[C;D1;H3:3])-[C:4](=[O;D1;H0:5])-[CH;D2;+0:6]=[CH2;D1;+0:7].[C:8]-[C:9]=[C:10](-[C:11](-[C;D1;H3:12])(-[C;D1;H3:13])-[OH;D1;+0:14])-[C:15]>>[C:8]-[C:9]=[C:10](-[C:11](-[C;D1;H3:12])(-[C;D1;H3:13])-[O;H0;D2;+0:14]-[CH2;D2;+0:7]-[CH2;D2;+0:6]-[C:4](=[O;D1;H0:5])-[#7:2](-[C;D1;H3:1])-[C;D1;H3:3])-[C:15...
47.1
[{"value": 47.1, "product": "[Si](C)(C)(C(C)(C)C)O[C@H]1C[C@@H](CC2=CC=C3[C@@H]4CC=C(C(C)(C)OCCC(=O)N(C)C)[C@]4(CC[C@@H]3[C@@]12C)C)O[Si](C)(C)C(C)(C)C", "details": "PERCENTYIELD", "is_desired": false}, {"value": 47.1, "product": "[Si](C)(C)(C(C)(C)C)O[C@H]1C[C@@H](CC2=CC=C3[C@@H]4CC=C(C(C)(C)OCCC(=O)N(C)C)[C@]4(CC[C@@...
null
null
null
null
1α,3β-Bis(tert-butyldimethylsilyloxy)-20-hydroxy-20-methylpregna-5,7,16-triene (200 mg, 0.36 mmol), N,N-dimethylacrylamide (107 mg, 1.08 mmol), sodium hydride (60% in oil, 23 mg, 0.56 mmol) and tetrahydrofuran (4 ml) were subjected to reaction using a procedure similar to that of Example 25(1) (17 hours at room tempera...
10.6084/m9.figshare.5104873.v1
null
Tertiary alcohol.Vinyl
Ether
null
null
C1=C[C@H]2CC[C@H]3C(=CC=C4CCCC[C@@H]43)[C@@H]2C1
null
O1CCCC1
null
null
C=CC(=O)N(C)C.CC(C)(O)C1=CC[C@H]2C3=CC=C4C[C@@H](O[Si](C)(C)C(C)(C)C)C[C@H](O[Si](C)(C)C(C)(C)C)[C@]4(C)[C@H]3CC[C@]12C>O1CCCC1>CN(C)C(=O)CCOC(C)(C)C1=CC[C@H]2C3=CC=C4C[C@@H](O[Si](C)(C)C(C)(C)C)C[C@H](O[Si](C)(C)C(C)(C)C)[C@]4(C)[C@H]3CC[C@]12C
ord_dataset-c3a75813d0b24864aa4f7cd526efd6aa
ord-f76a56a7c1944a91b3e37927785e3331
CN(C)C(=O)CCOC(C)(C)C1=CC[C@H]2C3=CC=C4C[C@@H](O[Si](C)(C)C(C)(C)C)C[C@H](O[Si](C)(C)C(C)(C)C)[C@]4(C)[C@H]3CC[C@]12C>>CCC(O)(CC)CCOC(C)(C)C1=CC[C@H]2C3=CC=C4C[C@@H](O[Si](C)(C)C(C)(C)C)C[C@H](O[Si](C)(C)C(C)(C)C)[C@]4(C)[C@H]3CC[C@]12C
[Si](C)(C)(C(C)(C)C)O[C@H]1C[C@@H](CC2=CC=C3[C@@H]4CC=C(C(C)(C)OCCC(=O)N(C)C)[C@]4(CC[C@@H]3[C@@]12C)C)O[Si](C)(C)C(C)(C)C.Cl[Ce](Cl)Cl.C(C)[Mg]Br.O1CCCC1>>[Si](C)(C)(C(C)(C)C)O[C@H]1C[C@@H](CC2=CC=C3[C@@H]4CC=C(C(C)(C)OCCC(CC)(O)CC)[C@]4(CC[C@@H]3[C@@]12C)C)O[Si](C)(C)C(C)(C)C
N([C:3](=[O:4])[CH2:7][CH2:8][O:9][C:10]([CH3:11])([CH3:12])[C:13]1=[CH:14][CH2:15][C@H:16]2[C:17]3=[CH:18][CH:19]=[C:20]4[CH2:21][C@@H:22]([O:23][Si:24]([CH3:25])([CH3:26])[C:27]([CH3:28])([CH3:29])[CH3:30])[CH2:31][C@H:32]([O:33][Si:34]([CH3:35])([CH3:36])[C:37]([CH3:38])([CH3:39])[CH3:40])[C@:41]4([CH3:42])[C@H:43]3...
CN(C)C(=O)CCOC(C)(C)C1=CC[C@H]2C3=CC=C4C[C@@H](O[Si](C)(C)C(C)(C)C)C[C@H](O[Si](C)(C)C(C)(C)C)[C@]4(C)[C@H]3CC[C@]12C
CCC(O)(CC)CCOC(C)(C)C1=CC[C@H]2C3=CC=C4C[C@@H](O[Si](C)(C)C(C)(C)C)C[C@H](O[Si](C)(C)C(C)(C)C)[C@]4(C)[C@H]3CC[C@]12C
null
null
null
Miscellaneous
OtherReaction
73a53c3699641f342e1262e87a7f18e7e1a58b3ae6a2bb965100bc5ca5aa8072
874533d67f572a036e87d660456c519859ccdb0867854a53cf4201fd273afc22
C1=CC2CC[C@H]3C(=CC=C4CCCCC43)[C@@H]2C1
[C:1]-[C:2]-[C;H0;D3;+0:3](=[O;H0;D1;+0:4])-N(-[CH3;D1;+0:5])-[CH3;D1;+0:6]>>[C:1]-[C:2]-[C;H0;D4;+0:3](-[OH;D1;+0:4])(-[C:7]-[C;D1;H3:8])-[CH2;D2;+0:5]-[CH3;D1;+0:6]
51.7
[{"value": 51.7, "product": "[Si](C)(C)(C(C)(C)C)O[C@H]1C[C@@H](CC2=CC=C3[C@@H]4CC=C(C(C)(C)OCCC(CC)(O)CC)[C@]4(CC[C@@H]3[C@@]12C)C)O[Si](C)(C)C(C)(C)C", "details": "PERCENTYIELD", "is_desired": false}]
null
null
null
null
1α,3β-Bis(tert-butyldimethylsilyloxy)-20-(N,N-dimethylaminocarbonylethoxy)-20-methylpregna-5,7,16-triene (133 mg, 0.20 mmol), anhydrous cerous (III) chloride (2.17 g, 8.8 mmol), ethylmagnesium bromide (8.3 ml, 8.0 mmol) and tetrahydrofuran (10 ml) were subjected to reaction using a procedure similar to that of Example ...
10.6084/m9.figshare.5104873.v1
null
Tertiary amide
Tertiary alcohol
null
null
C1=C[C@H]2CC[C@H]3C(=CC=C4CCCC[C@@H]43)[C@@H]2C1
null
null
null
null
CN(C)C(=O)CCOC(C)(C)C1=CC[C@H]2C3=CC=C4C[C@@H](O[Si](C)(C)C(C)(C)C)C[C@H](O[Si](C)(C)C(C)(C)C)[C@]4(C)[C@H]3CC[C@]12C>>CCC(O)(CC)CCOC(C)(C)C1=CC[C@H]2C3=CC=C4C[C@@H](O[Si](C)(C)C(C)(C)C)C[C@H](O[Si](C)(C)C(C)(C)C)[C@]4(C)[C@H]3CC[C@]12C
ord_dataset-c3a75813d0b24864aa4f7cd526efd6aa
ord-4f1ca6185ce24e27b5c2376a8ade2ba8
CCC(O)(CC)CCOC(C)(C)C1=CC[C@H]2C3=CC=C4C[C@@H](O[Si](C)(C)C(C)(C)C)C[C@H](O[Si](C)(C)C(C)(C)C)[C@]4(C)[C@H]3CC[C@]12C>>CCC(O)(CC)CCOC(C)(C)C1=CC[C@H]2C3=CC=C4C[C@@H](O)C[C@H](O)[C@]4(C)[C@H]3CC[C@]12C
[Si](C)(C)(C(C)(C)C)O[C@H]1C[C@@H](CC2=CC=C3[C@@H]4CC=C(C(C)(C)OCCC(CC)(O)CC)[C@]4(CC[C@@H]3[C@@]12C)C)O[Si](C)(C)C(C)(C)C.O1CCCC1.[F-].C(CCC)[N+](CCCC)(CCCC)CCCC>>O[C@H]1C[C@@H](CC2=CC=C3[C@@H]4CC=C(C(C)(C)OCCC(CC)(O)CC)[C@]4(CC[C@@H]3[C@@]12C)C)O
CC(C)(C)[Si](C)(C)[O:23][C@@H:22]1[CH2:21][C:20]2=[CH:19][CH:18]=[C:17]3[C@@H:16]4[CH2:15][CH:14]=[C:13]([C:10]([O:9][CH2:8][CH2:7][C:3]([CH2:2][CH3:1])([OH:4])[CH2:5][CH3:6])([CH3:11])[CH3:12])[C@@:32]4([CH3:33])[CH2:31][CH2:30][C@@H:29]3[C@@:27]2([CH3:28])[C@@H:25]([O:26][Si](C)(C)C(C)(C)C)[CH2:24]1>>[CH3:1][CH2:2][C...
CCC(O)(CC)CCOC(C)(C)C1=CC[C@H]2C3=CC=C4C[C@@H](O[Si](C)(C)C(C)(C)C)C[C@H](O[Si](C)(C)C(C)(C)C)[C@]4(C)[C@H]3CC[C@]12C
CCC(O)(CC)CCOC(C)(C)C1=CC[C@H]2C3=CC=C4C[C@@H](O)C[C@H](O)[C@]4(C)[C@H]3CC[C@]12C
null
null
O1CCCC1
Deprotection
OtherReaction
3c4d3a3b788b4022df80488c890c930a0eff3addc93b825229adfe1b23285620
c96f1dab6a2ddd7b236398a198654bbc85e92a2fc2f6e88d092d4f9a3211cc52
C1=CC2CC[C@H]3C(=CC=C4CCCCC43)[C@@H]2C1
C-C(-C)(-C)-[Si](-C)(-C)-[O;H0;D2;+0:1]-[C:2]1-[C:3]-[C:4](=[C:5])-[C:6]-[C:7](-[O;H0;D2;+0:8]-[Si](-C)(-C)-C(-C)(-C)-C)-[C:9]-1>>[C:5]=[C:4]1-[C:3]-[C:2](-[OH;D1;+0:1])-[C:9]-[C:7](-[OH;D1;+0:8])-[C:6]-1
100
[{"value": 100.0, "product": "O[C@H]1C[C@@H](CC2=CC=C3[C@@H]4CC=C(C(C)(C)OCCC(CC)(O)CC)[C@]4(CC[C@@H]3[C@@]12C)C)O", "details": "PERCENTYIELD", "is_desired": false}, {"value": 99.9, "product": "O[C@H]1C[C@@H](CC2=CC=C3[C@@H]4CC=C(C(C)(C)OCCC(CC)(O)CC)[C@]4(CC[C@@H]3[C@@]12C)C)O", "details": "CALCULATEDPERCENTYIELD", "i...
null
null
null
null
1α,3β-Bis(tert-butyldimethylsilyloxy)-20-(3-ethyl-3-hydroxypentyloxy)-20-methylpregna-5,7,16-triene (85 mg, 0.12 mmol), a 1M tetra-n-butylammonium fluoride tetrahydrofuran solution (1.2 ml) and tetrahydrofuran (4.6 ml) were subjected to reaction using a procedure similar to that of Example 5(2) (3 hours), worked up and...
10.6084/m9.figshare.5104873.v1
null
TMS ether protective group.TMS ether protective group
Secondary alcohol.Secondary alcohol
null
null
C1=C[C@H]2CC[C@H]3C(=CC=C4CCCC[C@@H]43)[C@@H]2C1
Other
O1CCCC1
null
null
CCC(O)(CC)CCOC(C)(C)C1=CC[C@H]2C3=CC=C4C[C@@H](O[Si](C)(C)C(C)(C)C)C[C@H](O[Si](C)(C)C(C)(C)C)[C@]4(C)[C@H]3CC[C@]12C>O1CCCC1>CCC(O)(CC)CCOC(C)(C)C1=CC[C@H]2C3=CC=C4C[C@@H](O)C[C@H](O)[C@]4(C)[C@H]3CC[C@]12C
ord_dataset-c3a75813d0b24864aa4f7cd526efd6aa
ord-8eca95401ac24e66a48eeaee52e9b4de
CC(C)(C)OC(=O)CBr.CC(C)(C)[Si](C)(C)O[C@@H]1CC2=CC=C3[C@H](CC[C@]4(C)C(CO)=CC[C@@H]34)[C@@]2(C)[C@@H](O[Si](C)(C)C(C)(C)C)C1>>CC(C)(C)OC(=O)COCC1=CC[C@H]2C3=CC=C4C[C@@H](O[Si](C)(C)C(C)(C)C)C[C@H](O[Si](C)(C)C(C)(C)C)[C@]4(C)[C@H]3CC[C@]12C
[Si](C)(C)(C(C)(C)C)O[C@H]1C[C@@H](CC2=CC=C3[C@@H]4CC=C([C@@]4(C)CC[C@@H]3[C@@]12C)CO)O[Si](C)(C)C(C)(C)C.[H-].[Na+].C1COCCOCCOCCOCCO1.BrCC(=O)OC(C)(C)C>>[Si](C)(C)(C(C)(C)C)O[C@H]1C[C@@H](CC2=CC=C3[C@@H]4CC=C([C@@]4(C)CC[C@@H]3[C@@]12C)COCC(=O)OC(C)(C)C)O[Si](C)(C)C(C)(C)C
Br[CH2:8][C:6]([O:5][C:2]([CH3:1])([CH3:3])[CH3:4])=[O:7].[OH:9][CH2:10][C:11]1=[CH:12][CH2:13][C@H:14]2[C:15]3=[CH:16][CH:17]=[C:18]4[CH2:19][C@@H:20]([O:21][Si:22]([CH3:23])([CH3:24])[C:25]([CH3:26])([CH3:27])[CH3:28])[CH2:29][C@H:30]([O:31][Si:32]([CH3:33])([CH3:34])[C:35]([CH3:36])([CH3:37])[CH3:38])[C@:39]4([CH3:4...
CC(C)(C)OC(=O)CBr.CC(C)(C)[Si](C)(C)O[C@@H]1CC2=CC=C3[C@H](CC[C@]4(C)C(CO)=CC[C@@H]34)[C@@]2(C)[C@@H](O[Si](C)(C)C(C)(C)C)C1
CC(C)(C)OC(=O)COCC1=CC[C@H]2C3=CC=C4C[C@@H](O[Si](C)(C)C(C)(C)C)C[C@H](O[Si](C)(C)C(C)(C)C)[C@]4(C)[C@H]3CC[C@]12C
null
null
O1CCCC1.C(C)(=O)OCC
Heteroatom Alkylation and Arylation
Williamson Ether Synthesis
4541d644834c1bca555c4310180b1edadd2271c26488a32c314314a2e4f9c76f
1858e49e1dc71f5ec31a1f9e719a3d52cdbfbbd98e3e0f8a48e0f56789173453
C1=CC2CC[C@H]3C(=CC=C4CCCCC43)[C@@H]2C1
Br-[CH2;D2;+0:1]-[C:2](=[O;D1;H0:3])-[#8:4]-[C:5](-[C;D1;H3:6])(-[C;D1;H3:7])-[C;D1;H3:8].[C:9]-[C:10]=[C:11](-[C:12]-[OH;D1;+0:13])-[C:14]>>[C:9]-[C:10]=[C:11](-[C:12]-[O;H0;D2;+0:13]-[CH2;D2;+0:1]-[C:2](=[O;D1;H0:3])-[#8:4]-[C:5](-[C;D1;H3:6])(-[C;D1;H3:7])-[C;D1;H3:8])-[C:14]
78.1
[{"value": 78.0, "product": "[Si](C)(C)(C(C)(C)C)O[C@H]1C[C@@H](CC2=CC=C3[C@@H]4CC=C([C@@]4(C)CC[C@@H]3[C@@]12C)COCC(=O)OC(C)(C)C)O[Si](C)(C)C(C)(C)C", "details": "PERCENTYIELD", "is_desired": false}, {"value": 78.1, "product": "[Si](C)(C)(C(C)(C)C)O[C@H]1C[C@@H](CC2=CC=C3[C@@H]4CC=C([C@@]4(C)CC[C@@H]3[C@@]12C)COCC(=O)...
null
null
null
null
A solution of 1α,3β-bis(tert-butyldimethylsilyloxy)-17-(hydroxymethyl)androsta-5,7,16-triene (1.0 g, 1.84 mmol), sodium hydride (60% in oil, 220 mg, 5.50 mmol), 15-crown-5 (400 mg, 1.82 mmol) and t-butyl bromoacetate (0.55 ml, 3.69 mmol) in tetrahydrofuran (20 ml) was refluxed under heating for 1 hour and 15 min. The r...
10.6084/m9.figshare.5104873.v1
null
Primary halide.Ester.Primary alcohol
Ester.Ether
null
null
C1=C[C@H]2CC[C@H]3C(=CC=C4CCCC[C@@H]43)[C@@H]2C1
HBr
O1CCCC1.C(C)(=O)OCC
null
null
CC(C)(C)OC(=O)CBr.CC(C)(C)[Si](C)(C)O[C@@H]1CC2=CC=C3[C@H](CC[C@]4(C)C(CO)=CC[C@@H]34)[C@@]2(C)[C@@H](O[Si](C)(C)C(C)(C)C)C1>O1CCCC1.C(C)(=O)OCC>CC(C)(C)OC(=O)COCC1=CC[C@H]2C3=CC=C4C[C@@H](O[Si](C)(C)C(C)(C)C)C[C@H](O[Si](C)(C)C(C)(C)C)[C@]4(C)[C@H]3CC[C@]12C
ord_dataset-c3a75813d0b24864aa4f7cd526efd6aa
ord-09f817b1421040bf81adda1049ebfd49
CC(C)(C)OC(=O)COCC1=CC[C@H]2C3=CC=C4C[C@@H](O[Si](C)(C)C(C)(C)C)C[C@H](O[Si](C)(C)C(C)(C)C)[C@]4(C)[C@H]3CC[C@]12C>>CC(C)(O)COCC1=CC[C@H]2C3=CC=C4C[C@@H](O[Si](C)(C)C(C)(C)C)C[C@H](O[Si](C)(C)C(C)(C)C)[C@]4(C)[C@H]3CC[C@]12C
O.[Cl-].[NH4+].[Si](C)(C)(C(C)(C)C)O[C@H]1C[C@@H](CC2=CC=C3[C@@H]4CC=C([C@@]4(C)CC[C@@H]3[C@@]12C)COCC(=O)OC(C)(C)C)O[Si](C)(C)C(C)(C)C.C[Mg]Br.O1CCCC1>>[Si](C)(C)(C(C)(C)C)O[C@H]1C[C@@H](CC2=CC=C3[C@@H]4CC=C([C@@]4(C)CC[C@@H]3[C@@]12C)COCC(C)(C)O)O[Si](C)(C)C(C)(C)C
CC(C)([CH3:3])[O:4][C:2](=O)[CH2:5][O:6][CH2:7][C:8]1=[CH:9][CH2:10][C@H:11]2[C:12]3=[CH:13][CH:14]=[C:15]4[CH2:16][C@@H:17]([O:18][Si:19]([CH3:20])([CH3:21])[C:22]([CH3:23])([CH3:24])[CH3:25])[CH2:26][C@H:27]([O:28][Si:29]([CH3:30])([CH3:31])[C:32]([CH3:33])([CH3:34])[CH3:35])[C@:36]4([CH3:37])[C@H:38]3[CH2:39][CH2:40...
CC(C)(C)OC(=O)COCC1=CC[C@H]2C3=CC=C4C[C@@H](O[Si](C)(C)C(C)(C)C)C[C@H](O[Si](C)(C)C(C)(C)C)[C@]4(C)[C@H]3CC[C@]12C
CC(C)(O)COCC1=CC[C@H]2C3=CC=C4C[C@@H](O[Si](C)(C)C(C)(C)C)C[C@H](O[Si](C)(C)C(C)(C)C)[C@]4(C)[C@H]3CC[C@]12C
null
null
O1CCCC1
Functional Group Interconversion
OtherReaction
0b851953c6b990603b6c2ce705013e806d0e3ec15190715f96b2920bbd66bf77
b84ab3aa125fecf72904a057d293902a2500c7c549137a262c925c1887e56d13
C1=CC2CC[C@H]3C(=CC=C4CCCCC43)[C@@H]2C1
C-C(-C)(-[CH3;D1;+0:1])-[O;H0;D2;+0:2]-[C;H0;D3;+0:3](=O)-[C:4]-[#8:5]>>[#8:5]-[C:4]-[C;H0;D4;+0:3](-[C;D1;H3:6])(-[CH3;D1;+0:1])-[OH;D1;+0:2]
70.2
[{"value": 70.0, "product": "[Si](C)(C)(C(C)(C)C)O[C@H]1C[C@@H](CC2=CC=C3[C@@H]4CC=C([C@@]4(C)CC[C@@H]3[C@@]12C)COCC(C)(C)O)O[Si](C)(C)C(C)(C)C", "details": "PERCENTYIELD", "is_desired": false}, {"value": 70.2, "product": "[Si](C)(C)(C(C)(C)C)O[C@H]1C[C@@H](CC2=CC=C3[C@@H]4CC=C([C@@]4(C)CC[C@@H]3[C@@]12C)COCC(C)(C)O)O[...
null
null
30
MINUTE
To a solution of 1α,3β-bis(tert-butyldimethylsilyloxy)-17-(tert-butoxycarbonylmethoxymethyl)androsta-5,7,16-triene (175 mg, 0.266 mmol) in tetrahydrofuran (4 ml), was added dropwise a 0.93M methylmagnesium bromide/tetrahydrofuran solution (3 ml, 2.79 mmol) at external temperature of −30° C., followed by stirring at the...
10.6084/m9.figshare.5104873.v1
null
Ester.Boc
Tertiary alcohol
null
null
C1=C[C@H]2CC[C@H]3C(=CC=C4CCCC[C@@H]43)[C@@H]2C1
HO-
O1CCCC1
null
0.5
CC(C)(C)OC(=O)COCC1=CC[C@H]2C3=CC=C4C[C@@H](O[Si](C)(C)C(C)(C)C)C[C@H](O[Si](C)(C)C(C)(C)C)[C@]4(C)[C@H]3CC[C@]12C>O1CCCC1>CC(C)(O)COCC1=CC[C@H]2C3=CC=C4C[C@@H](O[Si](C)(C)C(C)(C)C)C[C@H](O[Si](C)(C)C(C)(C)C)[C@]4(C)[C@H]3CC[C@]12C
ord_dataset-c3a75813d0b24864aa4f7cd526efd6aa
ord-6c03d50094e243f4919677055cf73518
CC(C)(C)OC(=O)COCC1=CC[C@H]2C3=CC=C4C[C@@H](O[Si](C)(C)C(C)(C)C)C[C@H](O[Si](C)(C)C(C)(C)C)[C@]4(C)[C@H]3CC[C@]12C>>CCC(O)(CC)COCC1=CC[C@H]2C3=CC=C4C[C@@H](O[Si](C)(C)C(C)(C)C)C[C@H](O[Si](C)(C)C(C)(C)C)[C@]4(C)[C@H]3CC[C@]12C
[Si](C)(C)(C(C)(C)C)O[C@H]1C[C@@H](CC2=CC=C3[C@@H]4CC=C([C@@]4(C)CC[C@@H]3[C@@]12C)COCC(=O)OC(C)(C)C)O[Si](C)(C)C(C)(C)C.C(C)[Mg]Br.O1CCCC1>>[Si](C)(C)(C(C)(C)C)O[C@H]1C[C@@H](CC2=CC=C3[C@@H]4CC=C([C@@]4(C)CC[C@@H]3[C@@]12C)COCC(CC)(O)CC)O[Si](C)(C)C(C)(C)C
CC(C)(C)O[C:3](=[O:4])[CH2:7][O:8][CH2:9][C:10]1=[CH:11][CH2:12][C@H:13]2[C:14]3=[CH:15][CH:16]=[C:17]4[CH2:18][C@@H:19]([O:20][Si:21]([CH3:22])([CH3:23])[C:24]([CH3:25])([CH3:26])[CH3:27])[CH2:28][C@H:29]([O:30][Si:31]([CH3:32])([CH3:33])[C:34]([CH3:35])([CH3:36])[CH3:37])[C@:38]4([CH3:39])[C@H:40]3[CH2:41][CH2:42][C@...
CC(C)(C)OC(=O)COCC1=CC[C@H]2C3=CC=C4C[C@@H](O[Si](C)(C)C(C)(C)C)C[C@H](O[Si](C)(C)C(C)(C)C)[C@]4(C)[C@H]3CC[C@]12C
CCC(O)(CC)COCC1=CC[C@H]2C3=CC=C4C[C@@H](O[Si](C)(C)C(C)(C)C)C[C@H](O[Si](C)(C)C(C)(C)C)[C@]4(C)[C@H]3CC[C@]12C
null
null
O1CCCC1
Functional Group Interconversion
OtherReaction
0b851953c6b990603b6c2ce705013e806d0e3ec15190715f96b2920bbd66bf77
b84ab3aa125fecf72904a057d293902a2500c7c549137a262c925c1887e56d13
C1=CC2CC[C@H]3C(=CC=C4CCCCC43)[C@@H]2C1
C-C(-C)(-C)-O-[C;H0;D3;+0:1](=[O;H0;D1;+0:2])-[C:3]-[#8:4]>>[#8:4]-[C:3]-[C;H0;D4;+0:1](-[OH;D1;+0:2])(-[C:5]-[C;D1;H3:6])-[C:7]-[C;D1;H3:8]
81.3
[{"value": 81.0, "product": "[Si](C)(C)(C(C)(C)C)O[C@H]1C[C@@H](CC2=CC=C3[C@@H]4CC=C([C@@]4(C)CC[C@@H]3[C@@]12C)COCC(CC)(O)CC)O[Si](C)(C)C(C)(C)C", "details": "PERCENTYIELD", "is_desired": false}, {"value": 81.3, "product": "[Si](C)(C)(C(C)(C)C)O[C@H]1C[C@@H](CC2=CC=C3[C@@H]4CC=C([C@@]4(C)CC[C@@H]3[C@@]12C)COCC(CC)(O)C...
null
null
null
null
A solution of 1α,3β-bis(tert-butyldimethylsilyloxy)-17-(tert-butoxycarbonylmethoxymethyl)androsta-5,7,16-triene (175 mg, 0.266 mmol) in tetrahydrofuran (4 ml) was subjected to reaction with a 0.96M ethylmagnesium bromide/tetrahydrofuran solution (3 ml, 2.88 mmol) using a procedure similar to that of Example 27(2) (exte...
10.6084/m9.figshare.5104873.v1
null
Ester.Boc
Tertiary alcohol
null
null
C1=C[C@H]2CC[C@H]3C(=CC=C4CCCC[C@@H]43)[C@@H]2C1
Other
O1CCCC1
null
null
CC(C)(C)OC(=O)COCC1=CC[C@H]2C3=CC=C4C[C@@H](O[Si](C)(C)C(C)(C)C)C[C@H](O[Si](C)(C)C(C)(C)C)[C@]4(C)[C@H]3CC[C@]12C>O1CCCC1>CCC(O)(CC)COCC1=CC[C@H]2C3=CC=C4C[C@@H](O[Si](C)(C)C(C)(C)C)C[C@H](O[Si](C)(C)C(C)(C)C)[C@]4(C)[C@H]3CC[C@]12C
ord_dataset-c3a75813d0b24864aa4f7cd526efd6aa
ord-a773ccc2032d4a18904f46db6e89d973
CCC(O)(CC)COCC1=CC[C@H]2C3=CC=C4C[C@@H](O[Si](C)(C)C(C)(C)C)C[C@H](O[Si](C)(C)C(C)(C)C)[C@]4(C)[C@H]3CC[C@]12C>>CCC(O)(CC)COCC1=CC[C@H]2C3=CC=C4C[C@@H](O)C[C@H](O)[C@]4(C)[C@H]3CC[C@]12C
[Si](C)(C)(C(C)(C)C)O[C@H]1C[C@@H](CC2=CC=C3[C@@H]4CC=C([C@@]4(C)CC[C@@H]3[C@@]12C)COCC(CC)(O)CC)O[Si](C)(C)C(C)(C)C.O1CCCC1.[F-].C(CCC)[N+](CCCC)(CCCC)CCCC>>C(C)C(COCC=1[C@]2(C)[C@@H](CC1)C1=CC=C3C[C@H](C[C@@H]([C@]3(C)[C@H]1CC2)O)O)(CC)O
CC(C)(C)[Si](C)(C)[O:20][C@@H:19]1[CH2:18][C:17]2=[CH:16][CH:15]=[C:14]3[C@@H:13]4[CH2:12][CH:11]=[C:10]([CH2:9][O:8][CH2:7][C:3]([CH2:2][CH3:1])([OH:4])[CH2:5][CH3:6])[C@@:29]4([CH3:30])[CH2:28][CH2:27][C@@H:26]3[C@@:24]2([CH3:25])[C@@H:22]([O:23][Si](C)(C)C(C)(C)C)[CH2:21]1>>[CH3:1][CH2:2][C:3]([OH:4])([CH2:5][CH3:6]...
CCC(O)(CC)COCC1=CC[C@H]2C3=CC=C4C[C@@H](O[Si](C)(C)C(C)(C)C)C[C@H](O[Si](C)(C)C(C)(C)C)[C@]4(C)[C@H]3CC[C@]12C
CCC(O)(CC)COCC1=CC[C@H]2C3=CC=C4C[C@@H](O)C[C@H](O)[C@]4(C)[C@H]3CC[C@]12C
null
null
O1CCCC1
Deprotection
OtherReaction
3c4d3a3b788b4022df80488c890c930a0eff3addc93b825229adfe1b23285620
c96f1dab6a2ddd7b236398a198654bbc85e92a2fc2f6e88d092d4f9a3211cc52
C1=CC2CC[C@H]3C(=CC=C4CCCCC43)[C@@H]2C1
C-C(-C)(-C)-[Si](-C)(-C)-[O;H0;D2;+0:1]-[C:2]1-[C:3]-[C:4](=[C:5])-[C:6]-[C:7](-[O;H0;D2;+0:8]-[Si](-C)(-C)-C(-C)(-C)-C)-[C:9]-1>>[C:5]=[C:4]1-[C:3]-[C:2](-[OH;D1;+0:1])-[C:9]-[C:7](-[OH;D1;+0:8])-[C:6]-1
72
[{"value": 72.0, "product": "C(C)C(COCC=1[C@]2(C)[C@@H](CC1)C1=CC=C3C[C@H](C[C@@H]([C@]3(C)[C@H]1CC2)O)O)(CC)O", "details": "PERCENTYIELD", "is_desired": false}, {"value": 71.6, "product": "C(C)C(COCC=1[C@]2(C)[C@@H](CC1)C1=CC=C3C[C@H](C[C@@H]([C@]3(C)[C@H]1CC2)O)O)(CC)O", "details": "CALCULATEDPERCENTYIELD", "is_desir...
null
null
null
null
1α,3β-Bis(tert-butyldimethylsilyloxy)-17-{2-ethyl-2-hydroxybutoxymethyl}androsta-5,7,16-triene (139 mg, 0.216 mmol), a 1M tetra-n-butylammonium fluoride tetrahydrofuran solution (1.3 ml, 1.3 mmol) and tetrahydrofuran (3 ml) were subjected to reaction using a procedure similar to that of Example 5(2) (4 hours), worked u...
10.6084/m9.figshare.5104873.v1
null
TMS ether protective group.TMS ether protective group
Secondary alcohol.Secondary alcohol
null
null
C1=C[C@H]2CC[C@H]3C(=CC=C4CCCC[C@@H]43)[C@@H]2C1
Other
O1CCCC1
null
null
CCC(O)(CC)COCC1=CC[C@H]2C3=CC=C4C[C@@H](O[Si](C)(C)C(C)(C)C)C[C@H](O[Si](C)(C)C(C)(C)C)[C@]4(C)[C@H]3CC[C@]12C>O1CCCC1>CCC(O)(CC)COCC1=CC[C@H]2C3=CC=C4C[C@@H](O)C[C@H](O)[C@]4(C)[C@H]3CC[C@]12C
ord_dataset-c3a75813d0b24864aa4f7cd526efd6aa
ord-e66355c7f5344561854354458ec36a7e
CC(C)(O)C#CCOCC1=CC[C@H]2C3=CC=C4C[C@@H](O)C[C@H](O)[C@]4(C)[C@H]3CC[C@]12C>>CC(C)(O)C/C=C\OCC1=CC[C@H]2C3=CC=C4C[C@@H](O)C[C@H](O)[C@]4(C)[C@H]3CC[C@]12C
O[C@H]1C[C@@H](CC2=CC=C3[C@@H]4CC=C([C@@]4(C)CC[C@@H]3[C@@]12C)COCC#CC(C)(C)O)O.N1=CC=CC2=CC=CC=C12>>O[C@H]1C[C@@H](CC2=CC=C3[C@@H]4CC=C([C@@]4(C)CC[C@@H]3[C@@]12C)CO\C=C/CC(C)(C)O)O
[CH3:1][C:2]([CH3:3])([OH:4])[C:5]#[C:6][CH2:7][O:8][CH2:9][C:10]1=[CH:11][CH2:12][C@H:13]2[C:14]3=[CH:15][CH:16]=[C:17]4[CH2:18][C@@H:19]([OH:20])[CH2:21][C@H:22]([OH:23])[C@:24]4([CH3:25])[C@H:26]3[CH2:27][CH2:28][C@:29]12[CH3:30]>>[CH3:1][C:2]([CH3:3])([OH:4])[CH2:5]/[CH:6]=[CH:7]\[O:8][CH2:9][C:10]1=[CH:11][CH2:12]...
CC(C)(O)C#CCOCC1=CC[C@H]2C3=CC=C4C[C@@H](O)C[C@H](O)[C@]4(C)[C@H]3CC[C@]12C
CC(C)(O)C/C=C\OCC1=CC[C@H]2C3=CC=C4C[C@@H](O)C[C@H](O)[C@]4(C)[C@H]3CC[C@]12C
null
[Pd]
CO
Miscellaneous
OtherReaction
2cb46d90d4ce375341220560e877f5d7e4c63abc1c248ae9e08e17759b4c1c9a
ab900cf836def760791838ce6e44f66c180fd21fe805999101fd878f395b1783
C1=CC2CC[C@H]3C(=CC=C4CCCCC43)[C@@H]2C1
[C:1]=[C:2]-[C:3]-[#8:4]-[CH2;D2;+0:5]-[C;H0;D2;+0:6]#[C;H0;D2;+0:7]-[C:8](-[C;D1;H3:9])(-[C;D1;H3:10])-[O;D1;H1:11]>>[C:1]=[C:2]-[C:3]-[#8:4]/[CH;D2;+0:5]=[CH;D2;+0:6]\[CH2;D2;+0:7]-[C:8](-[C;D1;H3:9])(-[C;D1;H3:10])-[O;D1;H1:11]
78
[{"value": 78.0, "product": "O[C@H]1C[C@@H](CC2=CC=C3[C@@H]4CC=C([C@@]4(C)CC[C@@H]3[C@@]12C)CO\\C=C/CC(C)(C)O)O", "details": "PERCENTYIELD", "is_desired": false}, {"value": 77.9, "product": "O[C@H]1C[C@@H](CC2=CC=C3[C@@H]4CC=C([C@@]4(C)CC[C@@H]3[C@@]12C)CO\\C=C/CC(C)(C)O)O", "details": "CALCULATEDPERCENTYIELD", "is_des...
null
null
null
null
1α,3β-Dihydroxy-17-(4-hydroxy-4-methyl-2-pentynyloxymethyl)androsta-5,7,16-triene (78 mg, 0.189 mmol), quinoline (12.3 mg, 0.0952 mmol), 5% palladium/barium sulfate (16 mg) and methanol (5 ml) were stirred at room temperature for 2 hours under a hydrogen atmosphere. The reaction mixture was filtered, evaporated for rem...
10.6084/m9.figshare.5104873.v1
null
Ether.Alkyne
Ether
null
null
C1=C[C@H]2CC[C@H]3C(=CC=C4CCCC[C@@H]43)[C@@H]2C1
null
[Pd].CO
null
null
CC(C)(O)C#CCOCC1=CC[C@H]2C3=CC=C4C[C@@H](O)C[C@H](O)[C@]4(C)[C@H]3CC[C@]12C>[Pd].CO>CC(C)(O)C/C=C\OCC1=CC[C@H]2C3=CC=C4C[C@@H](O)C[C@H](O)[C@]4(C)[C@H]3CC[C@]12C
ord_dataset-c3a75813d0b24864aa4f7cd526efd6aa
ord-9953d635993c4e47977430099ff37e58
CCC(O)(C#CCOCC1=CC[C@H]2C3=CC=C4C[C@@H](O)C[C@H](O)[C@]4(C)[C@H]3CC[C@]12C)CC>>CCC(O)(CC)C/C=C\OCC1=CC[C@H]2C3=CC=C4C[C@@H](O)C[C@H](O)[C@]4(C)[C@H]3CC[C@]12C
C(C)C(C#CCOCC=1[C@]2(C)[C@@H](CC1)C1=CC=C3C[C@H](C[C@@H]([C@]3(C)[C@H]1CC2)O)O)(CC)O.N1=CC=CC2=CC=CC=C12>>C(C)C(C\C=C/OCC=1[C@]2(C)[C@@H](CC1)C1=CC=C3C[C@H](C[C@@H]([C@]3(C)[C@H]1CC2)O)O)(CC)O
[CH3:1][CH2:2][C:3]([OH:4])([CH2:5][CH3:6])[C:7]#[C:8][CH2:9][O:10][CH2:11][C:12]1=[CH:13][CH2:14][C@H:15]2[C:16]3=[CH:17][CH:18]=[C:19]4[CH2:20][C@@H:21]([OH:22])[CH2:23][C@H:24]([OH:25])[C@:26]4([CH3:27])[C@H:28]3[CH2:29][CH2:30][C@:31]12[CH3:32]>>[CH3:1][CH2:2][C:3]([OH:4])([CH2:5][CH3:6])[CH2:7]/[CH:8]=[CH:9]\[O:10...
CCC(O)(C#CCOCC1=CC[C@H]2C3=CC=C4C[C@@H](O)C[C@H](O)[C@]4(C)[C@H]3CC[C@]12C)CC
CCC(O)(CC)C/C=C\OCC1=CC[C@H]2C3=CC=C4C[C@@H](O)C[C@H](O)[C@]4(C)[C@H]3CC[C@]12C
null
[Pd]
CO
Miscellaneous
OtherReaction
2cb46d90d4ce375341220560e877f5d7e4c63abc1c248ae9e08e17759b4c1c9a
ab900cf836def760791838ce6e44f66c180fd21fe805999101fd878f395b1783
C1=CC2CC[C@H]3C(=CC=C4CCCCC43)[C@@H]2C1
[C:1]=[C:2]-[C:3]-[#8:4]-[CH2;D2;+0:5]-[C;H0;D2;+0:6]#[C;H0;D2;+0:7]-[C:8](-[C:9])(-[C:10])-[O;D1;H1:11]>>[C:1]=[C:2]-[C:3]-[#8:4]/[CH;D2;+0:5]=[CH;D2;+0:6]\[CH2;D2;+0:7]-[C:8](-[C:9])(-[C:10])-[O;D1;H1:11]
null
[]
null
null
null
null
The fraction (0.3 g) containing 17-(4-ethyl-4-hydroxy-2-hexynyloxymethyl)-1α,3β-dihydroxyandrosta-5,7,16-triene obtained in Example 11 (2), 5% palladium/barium sulfate (0.3 g), quinoline (0.03 ml, 0.2538 mmol) and methanol (6.8 ml) were subjected to reaction using a procedure similar to that of Example 29(1) (4 hours) ...
10.6084/m9.figshare.5104873.v1
null
Ether.Alkyne
Ether
null
null
C1=C[C@H]2CC[C@H]3C(=CC=C4CCCC[C@@H]43)[C@@H]2C1
null
[Pd].CO
null
null
CCC(O)(C#CCOCC1=CC[C@H]2C3=CC=C4C[C@@H](O)C[C@H](O)[C@]4(C)[C@H]3CC[C@]12C)CC>[Pd].CO>CCC(O)(CC)C/C=C\OCC1=CC[C@H]2C3=CC=C4C[C@@H](O)C[C@H](O)[C@]4(C)[C@H]3CC[C@]12C
ord_dataset-c3a75813d0b24864aa4f7cd526efd6aa
ord-7d6a628d7eb941198bff4b0c0a9ab257
CC(=O)SCC1=CC[C@H]2C3=CC=C4C[C@@H](O[Si](C)(C)C(C)(C)C)C[C@H](O[Si](C)(C)C(C)(C)C)[C@]4(C)[C@H]3CC[C@]12C.CCC(CC)(CCCBr)O[Si](CC)(CC)CC>>CCC(CC)(CCCSCC1=CC[C@H]2C3=CC=C4C[C@@H](O[Si](C)(C)C(C)(C)C)C[C@H](O[Si](C)(C)C(C)(C)C)[C@]4(C)[C@H]3CC[C@]12C)O[Si](CC)(CC)CC
C(C)(=O)SCC=1[C@]2(C)[C@@H](CC1)C1=CC=C3C[C@H](C[C@@H]([C@]3(C)[C@H]1CC2)O[Si](C)(C)C(C)(C)C)O[Si](C)(C)C(C)(C)C.BrCCCC(CC)(O[Si](CC)(CC)CC)CC.CO.[OH-].[K+]>>[Si](C)(C)(C(C)(C)C)O[C@H]1C[C@@H](CC2=CC=C3[C@@H]4CC=C([C@@]4(C)CC[C@@H]3[C@@]12C)CSCCCC(CC)(O[Si](CC)(CC)CC)CC)O[Si](C)(C)C(C)(C)C
CC(=O)[S:9][CH2:10][C:11]1=[CH:12][CH2:13][C@H:14]2[C:15]3=[CH:16][CH:17]=[C:18]4[CH2:19][C@@H:20]([O:21][Si:22]([CH3:23])([CH3:24])[C:25]([CH3:26])([CH3:27])[CH3:28])[CH2:29][C@H:30]([O:31][Si:32]([CH3:33])([CH3:34])[C:35]([CH3:36])([CH3:37])[CH3:38])[C@:39]4([CH3:40])[C@H:41]3[CH2:42][CH2:43][C@:44]12[CH3:45].Br[CH2:...
CC(=O)SCC1=CC[C@H]2C3=CC=C4C[C@@H](O[Si](C)(C)C(C)(C)C)C[C@H](O[Si](C)(C)C(C)(C)C)[C@]4(C)[C@H]3CC[C@]12C.CCC(CC)(CCCBr)O[Si](CC)(CC)CC
CCC(CC)(CCCSCC1=CC[C@H]2C3=CC=C4C[C@@H](O[Si](C)(C)C(C)(C)C)C[C@H](O[Si](C)(C)C(C)(C)C)[C@]4(C)[C@H]3CC[C@]12C)O[Si](CC)(CC)CC
null
null
O1CCCC1
Heteroatom Alkylation and Arylation
OtherReaction
ac55b1813a50f413501bd3cd7115530e7b82e267a203d71b1e207485ab027747
2e4a9869295789d93ad40520a43348bbebd282f62196fc6899c2f5df92cb929d
C1=CC2CC[C@H]3C(=CC=C4CCCCC43)[C@@H]2C1
Br-[CH2;D2;+0:1]-[C:2]-[C:3].C-C(=O)-[S;H0;D2;+0:4]-[C:5]-[C:6](=[C:7]-[C:8])-[C:9]>>[C:8]-[C:7]=[C:6](-[C:5]-[S;H0;D2;+0:4]-[CH2;D2;+0:1]-[C:2]-[C:3])-[C:9]
91.3
[{"value": 91.0, "product": "[Si](C)(C)(C(C)(C)C)O[C@H]1C[C@@H](CC2=CC=C3[C@@H]4CC=C([C@@]4(C)CC[C@@H]3[C@@]12C)CSCCCC(CC)(O[Si](CC)(CC)CC)CC)O[Si](C)(C)C(C)(C)C", "details": "PERCENTYIELD", "is_desired": false}, {"value": 91.3, "product": "[Si](C)(C)(C(C)(C)C)O[C@H]1C[C@@H](CC2=CC=C3[C@@H]4CC=C([C@@]4(C)CC[C@@H]3[C@@]...
null
null
5
MINUTE
To a solution of 17-acetylthiomethyl-1α,3β-bis(tert-butyldimethylsilyloxy)androsta-5,7,16-triene (274 mg, 0.454 mmol) and 1-bromo-4-ethyl-4-(triethylsilyloxy)hexane (294 mg, 0.909 mmol) in tetrahydrofuran (2 ml), was added a 1M potassium hydroxide methanol solution (3 ml) under a nitrogen atmosphere, followed by stirri...
10.6084/m9.figshare.5104873.v1
null
Primary halide.Carbo-thioester
Monosulfide
null
null
C1=C[C@H]2CC[C@H]3C(=CC=C4CCCC[C@@H]43)[C@@H]2C1
HBr
O1CCCC1
null
0.083333
CC(=O)SCC1=CC[C@H]2C3=CC=C4C[C@@H](O[Si](C)(C)C(C)(C)C)C[C@H](O[Si](C)(C)C(C)(C)C)[C@]4(C)[C@H]3CC[C@]12C.CCC(CC)(CCCBr)O[Si](CC)(CC)CC>O1CCCC1>CCC(CC)(CCCSCC1=CC[C@H]2C3=CC=C4C[C@@H](O[Si](C)(C)C(C)(C)C)C[C@H](O[Si](C)(C)C(C)(C)C)[C@]4(C)[C@H]3CC[C@]12C)O[Si](CC)(CC)CC
ord_dataset-c3a75813d0b24864aa4f7cd526efd6aa
ord-e6735f5f88fa44dda823410e416ee3fd
CC(=O)SCC1=CC[C@H]2C3=CC=C4C[C@@H](O[Si](C)(C)C(C)(C)C)C[C@H](O[Si](C)(C)C(C)(C)C)[C@]4(C)[C@H]3CC[C@]12C.CC[Si](CC)(CC)OC(C)(C)CCCCBr>>CC[Si](CC)(CC)OC(C)(C)CCCCSCC1=CC[C@H]2C3=CC=C4C[C@@H](O[Si](C)(C)C(C)(C)C)C[C@H](O[Si](C)(C)C(C)(C)C)[C@]4(C)[C@H]3CC[C@]12C
C(C)(=O)SCC=1[C@]2(C)[C@@H](CC1)C1=CC=C3C[C@H](C[C@@H]([C@]3(C)[C@H]1CC2)O[Si](C)(C)C(C)(C)C)O[Si](C)(C)C(C)(C)C.BrCCCCC(C)(C)O[Si](CC)(CC)CC.CO.[OH-].[K+]>>[Si](C)(C)(C(C)(C)C)O[C@H]1C[C@@H](CC2=CC=C3[C@@H]4CC=C([C@@]4(C)CC[C@@H]3[C@@]12C)CSCCCCC(C)(C)O[Si](CC)(CC)CC)O[Si](C)(C)C(C)(C)C
CC(=O)[S:16][CH2:17][C:18]1=[CH:19][CH2:20][C@H:21]2[C:22]3=[CH:23][CH:24]=[C:25]4[CH2:26][C@@H:27]([O:28][Si:29]([CH3:30])([CH3:31])[C:32]([CH3:33])([CH3:34])[CH3:35])[CH2:36][C@H:37]([O:38][Si:39]([CH3:40])([CH3:41])[C:42]([CH3:43])([CH3:44])[CH3:45])[C@:46]4([CH3:47])[C@H:48]3[CH2:49][CH2:50][C@:51]12[CH3:52].Br[CH2...
CC(=O)SCC1=CC[C@H]2C3=CC=C4C[C@@H](O[Si](C)(C)C(C)(C)C)C[C@H](O[Si](C)(C)C(C)(C)C)[C@]4(C)[C@H]3CC[C@]12C.CC[Si](CC)(CC)OC(C)(C)CCCCBr
CC[Si](CC)(CC)OC(C)(C)CCCCSCC1=CC[C@H]2C3=CC=C4C[C@@H](O[Si](C)(C)C(C)(C)C)C[C@H](O[Si](C)(C)C(C)(C)C)[C@]4(C)[C@H]3CC[C@]12C
null
null
O1CCCC1
Heteroatom Alkylation and Arylation
OtherReaction
ac55b1813a50f413501bd3cd7115530e7b82e267a203d71b1e207485ab027747
2e4a9869295789d93ad40520a43348bbebd282f62196fc6899c2f5df92cb929d
C1=CC2CC[C@H]3C(=CC=C4CCCCC43)[C@@H]2C1
Br-[CH2;D2;+0:1]-[C:2]-[C:3].C-C(=O)-[S;H0;D2;+0:4]-[C:5]-[C:6](=[C:7]-[C:8])-[C:9]>>[C:3]-[C:2]-[CH2;D2;+0:1]-[S;H0;D2;+0:4]-[C:5]-[C:6](=[C:7]-[C:8])-[C:9]
93.4
[{"value": 93.0, "product": "[Si](C)(C)(C(C)(C)C)O[C@H]1C[C@@H](CC2=CC=C3[C@@H]4CC=C([C@@]4(C)CC[C@@H]3[C@@]12C)CSCCCCC(C)(C)O[Si](CC)(CC)CC)O[Si](C)(C)C(C)(C)C", "details": "PERCENTYIELD", "is_desired": false}, {"value": 93.4, "product": "[Si](C)(C)(C(C)(C)C)O[C@H]1C[C@@H](CC2=CC=C3[C@@H]4CC=C([C@@]4(C)CC[C@@H]3[C@@]1...
null
null
null
null
17-Acetylthiomethyl-1α,3β-bis(tert-butyldimethylsilyloxy)androsta-5,7,16-triene (262 mg, 0.434 mmol), 1-bromo-5-triethylsilyloxy-5-methylhexane (266 mg, 0.860 mmol), a 1M potassium hydroxide methanol solution (3 ml) and tetrahydrofuran (2 ml) were subjected to reaction using a procedure similar to that of Example 31(1)...
10.6084/m9.figshare.5104873.v1
null
Primary halide.Carbo-thioester
Monosulfide
null
null
C1=C[C@H]2CC[C@H]3C(=CC=C4CCCC[C@@H]43)[C@@H]2C1
HBr
O1CCCC1
null
null
CC(=O)SCC1=CC[C@H]2C3=CC=C4C[C@@H](O[Si](C)(C)C(C)(C)C)C[C@H](O[Si](C)(C)C(C)(C)C)[C@]4(C)[C@H]3CC[C@]12C.CC[Si](CC)(CC)OC(C)(C)CCCCBr>O1CCCC1>CC[Si](CC)(CC)OC(C)(C)CCCCSCC1=CC[C@H]2C3=CC=C4C[C@@H](O[Si](C)(C)C(C)(C)C)C[C@H](O[Si](C)(C)C(C)(C)C)[C@]4(C)[C@H]3CC[C@]12C
ord_dataset-c3a75813d0b24864aa4f7cd526efd6aa
ord-3aa0f12e1abf4c07b006015c14a90f4e
CC(=O)SCC1=CC[C@H]2C3=CC=C4C[C@@H](O[Si](C)(C)C(C)(C)C)C[C@H](O[Si](C)(C)C(C)(C)C)[C@]4(C)[C@H]3CC[C@]12C.CC[Si](CC)(CC)OC(C)(C)C/C=C/Br>>CC[Si](CC)(CC)OC(C)(C)C/C=C/SCC1=CC[C@H]2C3=CC=C4C[C@@H](O[Si](C)(C)C(C)(C)C)C[C@H](O[Si](C)(C)C(C)(C)C)[C@]4(C)[C@H]3CC[C@]12C
C(C)(=O)SCC=1[C@]2(C)[C@@H](CC1)C1=CC=C3C[C@H](C[C@@H]([C@]3(C)[C@H]1CC2)O[Si](C)(C)C(C)(C)C)O[Si](C)(C)C(C)(C)C.Br\C=C\CC(C)(C)O[Si](CC)(CC)CC.CO.[OH-].[K+]>>[Si](C)(C)(C(C)(C)C)O[C@H]1C[C@@H](CC2=CC=C3[C@@H]4CC=C([C@@]4(C)CC[C@@H]3[C@@]12C)CS\C=C\CC(C)(C)O[Si](CC)(CC)CC)O[Si](C)(C)C(C)(C)C
CC(=O)[S:15][CH2:16][C:17]1=[CH:18][CH2:19][C@H:20]2[C:21]3=[CH:22][CH:23]=[C:24]4[CH2:25][C@@H:26]([O:27][Si:28]([CH3:29])([CH3:30])[C:31]([CH3:32])([CH3:33])[CH3:34])[CH2:35][C@H:36]([O:37][Si:38]([CH3:39])([CH3:40])[C:41]([CH3:42])([CH3:43])[CH3:44])[C@:45]4([CH3:46])[C@H:47]3[CH2:48][CH2:49][C@:50]12[CH3:51].Br/[CH...
CC(=O)SCC1=CC[C@H]2C3=CC=C4C[C@@H](O[Si](C)(C)C(C)(C)C)C[C@H](O[Si](C)(C)C(C)(C)C)[C@]4(C)[C@H]3CC[C@]12C.CC[Si](CC)(CC)OC(C)(C)C/C=C/Br
CC[Si](CC)(CC)OC(C)(C)C/C=C/SCC1=CC[C@H]2C3=CC=C4C[C@@H](O[Si](C)(C)C(C)(C)C)C[C@H](O[Si](C)(C)C(C)(C)C)[C@]4(C)[C@H]3CC[C@]12C
null
null
O1CCCC1
Heteroatom Alkylation and Arylation
OtherReaction
414ef9d7284b3a3a3ca4f3037df8885fc317c70df763f998bdece1a30f85b3fd
950082924a0524bfc0063f92485d7f4b587dbc9668e1d8f834d8cda3a56bc402
C1=CC2CC[C@H]3C(=CC=C4CCCCC43)[C@@H]2C1
Br/[CH;D2;+0:1]=[C:2]/[C:3]-[C:4].C-C(=O)-[S;H0;D2;+0:5]-[C:6]-[C:7](=[C:8]-[C:9])-[C:10]>>[C:9]-[C:8]=[C:7](-[C:6]-[S;H0;D2;+0:5]/[CH;D2;+0:1]=[C:2]/[C:3]-[C:4])-[C:10]
90
[{"value": 90.0, "product": "[Si](C)(C)(C(C)(C)C)O[C@H]1C[C@@H](CC2=CC=C3[C@@H]4CC=C([C@@]4(C)CC[C@@H]3[C@@]12C)CS\\C=C\\CC(C)(C)O[Si](CC)(CC)CC)O[Si](C)(C)C(C)(C)C", "details": "PERCENTYIELD", "is_desired": false}, {"value": 90.0, "product": "[Si](C)(C)(C(C)(C)C)O[C@H]1C[C@@H](CC2=CC=C3[C@@H]4CC=C([C@@]4(C)CC[C@@H]3[C...
null
null
null
null
17-Acetylthiomethyl-1α,3β-bis(tert-butyldimethylsilyloxy)androsta-5,7,16-triene (304 mg, 0.504 mmol), 1-bromo-4-triethylsilyloxy-4-methyl-(2E)-pentene (296 mg, 1.01 mmol), a 1M potassium hydroxide methanol solution (3 ml) and tetrahydrofuran (2 ml) were subjected to reaction using a procedure similar to that of Example...
10.6084/m9.figshare.5104873.v1
null
Carbo-thioester
Monosulfide
null
null
C1=C[C@H]2CC[C@H]3C(=CC=C4CCCC[C@@H]43)[C@@H]2C1
HBr
O1CCCC1
null
null
CC(=O)SCC1=CC[C@H]2C3=CC=C4C[C@@H](O[Si](C)(C)C(C)(C)C)C[C@H](O[Si](C)(C)C(C)(C)C)[C@]4(C)[C@H]3CC[C@]12C.CC[Si](CC)(CC)OC(C)(C)C/C=C/Br>O1CCCC1>CC[Si](CC)(CC)OC(C)(C)C/C=C/SCC1=CC[C@H]2C3=CC=C4C[C@@H](O[Si](C)(C)C(C)(C)C)C[C@H](O[Si](C)(C)C(C)(C)C)[C@]4(C)[C@H]3CC[C@]12C
ord_dataset-c3a75813d0b24864aa4f7cd526efd6aa
ord-b40612350df64afcb83face9bc2e6092
CC(=O)SCC1=CC[C@H]2C3=CC=C4C[C@@H](O[Si](C)(C)C(C)(C)C)C[C@H](O[Si](C)(C)C(C)(C)C)[C@]4(C)[C@H]3CC[C@]12C.CC(C)(O)CCBr>>CC(C)(O)CCSCC1=CC[C@H]2C3=CC=C4C[C@@H](O[Si](C)(C)C(C)(C)C)C[C@H](O[Si](C)(C)C(C)(C)C)[C@]4(C)[C@H]3CC[C@]12C
C(C)(=O)SCC=1[C@]2(C)[C@@H](CC1)C1=CC=C3C[C@H](C[C@@H]([C@]3(C)[C@H]1CC2)O[Si](C)(C)C(C)(C)C)O[Si](C)(C)C(C)(C)C.BrCCC(C)(C)O.CO.[OH-].[K+]>>[Si](C)(C)(C(C)(C)C)O[C@H]1C[C@@H](CC2=CC=C3[C@@H]4CC=C([C@@]4(C)CC[C@@H]3[C@@]12C)CSCCC(C)(C)O)O[Si](C)(C)C(C)(C)C
CC(=O)[S:7][CH2:8][C:9]1=[CH:10][CH2:11][C@H:12]2[C:13]3=[CH:14][CH:15]=[C:16]4[CH2:17][C@@H:18]([O:19][Si:20]([CH3:21])([CH3:22])[C:23]([CH3:24])([CH3:25])[CH3:26])[CH2:27][C@H:28]([O:29][Si:30]([CH3:31])([CH3:32])[C:33]([CH3:34])([CH3:35])[CH3:36])[C@:37]4([CH3:38])[C@H:39]3[CH2:40][CH2:41][C@:42]12[CH3:43].Br[CH2:6]...
CC(=O)SCC1=CC[C@H]2C3=CC=C4C[C@@H](O[Si](C)(C)C(C)(C)C)C[C@H](O[Si](C)(C)C(C)(C)C)[C@]4(C)[C@H]3CC[C@]12C.CC(C)(O)CCBr
CC(C)(O)CCSCC1=CC[C@H]2C3=CC=C4C[C@@H](O[Si](C)(C)C(C)(C)C)C[C@H](O[Si](C)(C)C(C)(C)C)[C@]4(C)[C@H]3CC[C@]12C
null
null
O1CCCC1
Heteroatom Alkylation and Arylation
OtherReaction
ac55b1813a50f413501bd3cd7115530e7b82e267a203d71b1e207485ab027747
2e4a9869295789d93ad40520a43348bbebd282f62196fc6899c2f5df92cb929d
C1=CC2CC[C@H]3C(=CC=C4CCCCC43)[C@@H]2C1
Br-[CH2;D2;+0:1]-[C:2]-[C:3].C-C(=O)-[S;H0;D2;+0:4]-[C:5]-[C:6](=[C:7]-[C:8])-[C:9]>>[C:8]-[C:7]=[C:6](-[C:5]-[S;H0;D2;+0:4]-[CH2;D2;+0:1]-[C:2]-[C:3])-[C:9]
93
[{"value": 93.0, "product": "[Si](C)(C)(C(C)(C)C)O[C@H]1C[C@@H](CC2=CC=C3[C@@H]4CC=C([C@@]4(C)CC[C@@H]3[C@@]12C)CSCCC(C)(C)O)O[Si](C)(C)C(C)(C)C", "details": "PERCENTYIELD", "is_desired": false}, {"value": 93.0, "product": "[Si](C)(C)(C(C)(C)C)O[C@H]1C[C@@H](CC2=CC=C3[C@@H]4CC=C([C@@]4(C)CC[C@@H]3[C@@]12C)CSCCC(C)(C)O)...
null
null
null
null
17-Acetylthiomethyl-1α,3β-bis(tert-butyldimethylsilyloxy)androsta-5,7,16-triene (67.7 mg, 0.112 mmol), 1-bromo-3-hydroxy-3-methylbutane (93.5 mg, 0.560 mmol), 1M potassium hydroxide methanol solution (1 ml) and tetrahydrofuran (1 ml) were subjected to reaction using a procedure similar to that of Example 31(1) (at room...
10.6084/m9.figshare.5104873.v1
null
Primary halide.Carbo-thioester
Monosulfide
null
null
C1=C[C@H]2CC[C@H]3C(=CC=C4CCCC[C@@H]43)[C@@H]2C1
HBr
O1CCCC1
null
null
CC(=O)SCC1=CC[C@H]2C3=CC=C4C[C@@H](O[Si](C)(C)C(C)(C)C)C[C@H](O[Si](C)(C)C(C)(C)C)[C@]4(C)[C@H]3CC[C@]12C.CC(C)(O)CCBr>O1CCCC1>CC(C)(O)CCSCC1=CC[C@H]2C3=CC=C4C[C@@H](O[Si](C)(C)C(C)(C)C)C[C@H](O[Si](C)(C)C(C)(C)C)[C@]4(C)[C@H]3CC[C@]12C
ord_dataset-c3a75813d0b24864aa4f7cd526efd6aa
ord-5ee07af8e70c4954abdedabfc16b7f64
CC(C)(O)CCSCC1=CC[C@H]2C3=CC=C4C[C@@H](O[Si](C)(C)C(C)(C)C)C[C@H](O[Si](C)(C)C(C)(C)C)[C@]4(C)[C@H]3CC[C@]12C>>CC(C)(O)CCSCC1=CC[C@H]2C3=CC=C4C[C@@H](O)C[C@H](O)[C@]4(C)[C@H]3CC[C@]12C
[Si](C)(C)(C(C)(C)C)O[C@H]1C[C@@H](CC2=CC=C3[C@@H]4CC=C([C@@]4(C)CC[C@@H]3[C@@]12C)CSCCC(C)(C)O)O[Si](C)(C)C(C)(C)C.O1CCCC1.[F-].C(CCC)[N+](CCCC)(CCCC)CCCC>>O[C@H]1C[C@@H](CC2=CC=C3[C@@H]4CC=C([C@@]4(C)CC[C@@H]3[C@@]12C)CSCCC(C)(C)O)O
CC(C)(C)[Si](C)(C)[O:19][C@@H:18]1[CH2:17][C:16]2=[CH:15][CH:14]=[C:13]3[C@@H:12]4[CH2:11][CH:10]=[C:9]([CH2:8][S:7][CH2:6][CH2:5][C:2]([CH3:1])([CH3:3])[OH:4])[C@@:28]4([CH3:29])[CH2:27][CH2:26][C@@H:25]3[C@@:23]2([CH3:24])[C@@H:21]([O:22][Si](C)(C)C(C)(C)C)[CH2:20]1>>[CH3:1][C:2]([CH3:3])([OH:4])[CH2:5][CH2:6][S:7][C...
CC(C)(O)CCSCC1=CC[C@H]2C3=CC=C4C[C@@H](O[Si](C)(C)C(C)(C)C)C[C@H](O[Si](C)(C)C(C)(C)C)[C@]4(C)[C@H]3CC[C@]12C
CC(C)(O)CCSCC1=CC[C@H]2C3=CC=C4C[C@@H](O)C[C@H](O)[C@]4(C)[C@H]3CC[C@]12C
null
null
O1CCCC1
Deprotection
OtherReaction
3c4d3a3b788b4022df80488c890c930a0eff3addc93b825229adfe1b23285620
c96f1dab6a2ddd7b236398a198654bbc85e92a2fc2f6e88d092d4f9a3211cc52
C1=CC2CC[C@H]3C(=CC=C4CCCCC43)[C@@H]2C1
C-C(-C)(-C)-[Si](-C)(-C)-[O;H0;D2;+0:1]-[C:2]1-[C:3]-[C:4](=[C:5])-[C:6]-[C:7](-[O;H0;D2;+0:8]-[Si](-C)(-C)-C(-C)(-C)-C)-[C:9]-1>>[C:5]=[C:4]1-[C:3]-[C:2](-[OH;D1;+0:1])-[C:9]-[C:7](-[OH;D1;+0:8])-[C:6]-1
95.5
[{"value": 95.0, "product": "O[C@H]1C[C@@H](CC2=CC=C3[C@@H]4CC=C([C@@]4(C)CC[C@@H]3[C@@]12C)CSCCC(C)(C)O)O", "details": "PERCENTYIELD", "is_desired": false}, {"value": 95.5, "product": "O[C@H]1C[C@@H](CC2=CC=C3[C@@H]4CC=C([C@@]4(C)CC[C@@H]3[C@@]12C)CSCCC(C)(C)O)O", "details": "CALCULATEDPERCENTYIELD", "is_desired": fal...
null
null
null
null
1α,3β-Bis(tert-butyldimethylsilyloxy)-17-(3-hydroxy-3-methylbutylthiomethyl)androsta-5,7,16-triene (63.5 mg, 0.0981 mmol), a 1M tetra-n-butylammonium fluoride tetrahydrofuran solution (1 ml) and tetrahydrofuran (1 ml) were subjected to reaction using a procedure similar to that of Example 5(2) (reflux under heating for...
10.6084/m9.figshare.5104873.v1
null
TMS ether protective group.TMS ether protective group
Secondary alcohol.Secondary alcohol
null
null
C1=C[C@H]2CC[C@H]3C(=CC=C4CCCC[C@@H]43)[C@@H]2C1
Other
O1CCCC1
null
null
CC(C)(O)CCSCC1=CC[C@H]2C3=CC=C4C[C@@H](O[Si](C)(C)C(C)(C)C)C[C@H](O[Si](C)(C)C(C)(C)C)[C@]4(C)[C@H]3CC[C@]12C>O1CCCC1>CC(C)(O)CCSCC1=CC[C@H]2C3=CC=C4C[C@@H](O)C[C@H](O)[C@]4(C)[C@H]3CC[C@]12C
ord_dataset-c3a75813d0b24864aa4f7cd526efd6aa
ord-cf7db74464e144219f9c73c4d6f70138
CC(C)(C)[Si](C)(C)O[C@@H]1CC2=CC[C@H]3[C@@H]4CCC[C@@]4(C)CC[C@@H]3[C@@]2(C)[C@@H](O[Si](C)(C)C(C)(C)C)C1>>C=C1CC[C@H]2[C@@H]3CC=C4C[C@@H](O[Si](C)(C)C(C)(C)C)C[C@H](O[Si](C)(C)C(C)(C)C)[C@]4(C)[C@H]3CC[C@]12C
[Si](C)(C)(C(C)(C)C)O[C@H]1C[C@@H](CC2=CC[C@H]3[C@@H]4CCC[C@@]4(C)CC[C@@H]3[C@@]12C)O[Si](C)(C)C(C)(C)C.O1CCCC1.O1CCCC1.CC(C)([O-])C.[K+]>>[Si](C)(C)(C(C)(C)C)O[C@H]1C[C@@H](CC2=CC[C@H]3[C@@H]4CCC([C@@]4(C)CC[C@@H]3[C@@]12C)=C)O[Si](C)(C)C(C)(C)C
[CH2:2]1[CH2:3][CH2:4][C@H:5]2[C@@H:6]3[CH2:7][CH:8]=[C:9]4[CH2:10][C@@H:11]([O:12][Si:13]([CH3:14])([CH3:15])[C:16]([CH3:17])([CH3:18])[CH3:19])[CH2:20][C@H:21]([O:22][Si:23]([CH3:24])([CH3:25])[C:26]([CH3:27])([CH3:28])[CH3:29])[C@:30]4([CH3:31])[C@H:32]3[CH2:33][CH2:34][C@:35]12[CH3:36]>>[CH2:1]=[C:2]1[CH2:3][CH2:4]...
CC(C)(C)[Si](C)(C)O[C@@H]1CC2=CC[C@H]3[C@@H]4CCC[C@@]4(C)CC[C@@H]3[C@@]2(C)[C@@H](O[Si](C)(C)C(C)(C)C)C1
C=C1CC[C@H]2[C@@H]3CC=C4C[C@@H](O[Si](C)(C)C(C)(C)C)C[C@H](O[Si](C)(C)C(C)(C)C)[C@]4(C)[C@H]3CC[C@]12C
null
[Br-].C[P+](C1=CC=CC=C1)(C1=CC=CC=C1)C1=CC=CC=C1
O.CCCCCC.CC(=O)C.CO
Miscellaneous
OtherReaction
7c25aa6c39004c295ea8e39669430c4214ce17cd1d210263e8fa8499e631cdcc
4741489b7ce48b1006256d06e81c9d9d68657901282cd304500858c7d1cda546
C=C1CC[C@@H]2C1CC[C@@H]1C3CCCCC3=CC[C@@H]21
[C:1]-[C:2]1(-[C;D1;H3:3])-[C:4]-[C:5]-[C:6]-[CH2;D2;+0:7]-1>>[C:1]-[C:2]1(-[C;D1;H3:3])-[C:4]-[C:5]-[C:6]-[C;H0;D3;+0:7]-1=[C;D1;H2:8]
null
[]
60
CELSIUS
2
HOUR
A mixture of tetrahydrofuran (70 ml), methyltriphenylphosphonium bromide (50 g) and potassium t-butoxide (13.9 g) were stirred at 60° C. for 2 hours, while under suspension. To this suspension, was added 1α,3β-bis(tert-butyldimethylsilyloxy)androst-5-ene (18.7 g) and tetrahydrofuran (60 ml), followed by reaction for 2 ...
10.6084/m9.figshare.5104873.v1
null
null
Vinyl
C1=C2CCCC[C@@H]2[C@H]2CC[C@@H]3CCC[C@H]3[C@@H]2C1
C1=C2CCCC[C@@H]2[C@H]2CC[C@@H]3CCC[C@H]3[C@@H]2C1
C1=C2CCCC[C@@H]2[C@H]2CC[C@@H]3CCC[C@H]3[C@@H]2C1
Other
[Br-].C[P+](C1=CC=CC=C1)(C1=CC=CC=C1)C1=CC=CC=C1.O.CCCCCC.CC(=O)C.CO
60
2
CC(C)(C)[Si](C)(C)O[C@@H]1CC2=CC[C@H]3[C@@H]4CCC[C@@]4(C)CC[C@@H]3[C@@]2(C)[C@@H](O[Si](C)(C)C(C)(C)C)C1>[Br-].C[P+](C1=CC=CC=C1)(C1=CC=CC=C1)C1=CC=CC=C1.O.CCCCCC.CC(=O)C.CO>C=C1CC[C@H]2[C@@H]3CC=C4C[C@@H](O[Si](C)(C)C(C)(C)C)C[C@H](O[Si](C)(C)C(C)(C)C)[C@]4(C)[C@H]3CC[C@]12C
ord_dataset-c3a75813d0b24864aa4f7cd526efd6aa
ord-72031b92e7964eb6b128206455f66ab4
C=C1CC[C@H]2[C@@H]3CC=C4C[C@@H](O[Si](C)(C)C(C)(C)C)C[C@H](O[Si](C)(C)C(C)(C)C)[C@]4(C)[C@H]3CC[C@]12C.OO>>CC(C)(C)[Si](C)(C)O[C@@H]1CC2=CC[C@H]3[C@@H]4CC[C@H](CO)[C@@]4(C)CC[C@@H]3[C@@]2(C)[C@@H](O[Si](C)(C)C(C)(C)C)C1
[Si](C)(C)(C(C)(C)C)O[C@H]1C[C@@H](CC2=CC[C@H]3[C@@H]4CCC([C@@]4(C)CC[C@@H]3[C@@]12C)=C)O[Si](C)(C)C(C)(C)C.C12CCCC(CCC1)B2.[OH-].[Na+].OO>>[Si](C)(C)(C(C)(C)C)O[C@H]1C[C@@H](CC2=CC[C@H]3[C@@H]4CC[C@@H]([C@@]4(C)CC[C@@H]3[C@@]12C)CO)O[Si](C)(C)C(C)(C)C
[CH3:1][C:2]([CH3:3])([CH3:4])[Si:5]([CH3:6])([CH3:7])[O:8][C@@H:9]1[CH2:10][C:11]2=[CH:12][CH2:13][C@H:14]3[C@@H:15]4[CH2:16][CH2:17][C:18](=[CH2:19])[C@@:21]4([CH3:22])[CH2:23][CH2:24][C@@H:25]3[C@@:26]2([CH3:27])[C@@H:28]([O:29][Si:30]([CH3:31])([CH3:32])[C:33]([CH3:34])([CH3:35])[CH3:36])[CH2:37]1.O[OH:20]>>[CH3:1]...
C=C1CC[C@H]2[C@@H]3CC=C4C[C@@H](O[Si](C)(C)C(C)(C)C)C[C@H](O[Si](C)(C)C(C)(C)C)[C@]4(C)[C@H]3CC[C@]12C.OO
CC(C)(C)[Si](C)(C)O[C@@H]1CC2=CC[C@H]3[C@@H]4CC[C@H](CO)[C@@]4(C)CC[C@@H]3[C@@]2(C)[C@@H](O[Si](C)(C)C(C)(C)C)C1
null
null
CO
Heteroatom Alkylation and Arylation
OtherReaction
14323edfe0584e2510a42abdde4fbf731fb650ba7151b53acb5cab26e269514a
4ceb30033bcfd57c382fe05e353b68e7f657859dbacaaa785451a244b2657476
C1=C2CCCCC2[C@H]2CCC3CCC[C@H]3[C@@H]2C1
O-[OH;D1;+0:1].[C:2]-[C:3]1(-[C;D1;H3:4])-[C:5]-[C:6]-[C:7]-[C;H0;D3;+0:8]-1=[CH2;D1;+0:9]>>[C:2]-[C:3]1(-[C;D1;H3:4])-[C:5]-[C:6]-[C:7]-[C@@H;D3;+0:8]-1-[CH2;D2;+0:9]-[OH;D1;+0:1]
null
[]
null
null
4
HOUR
To 1α,3β-bis(tert-butyldimethylsilyloxy)-17-methyleneandrost-5-ene (30.3 g), was added 9-borabicyclo[3,3,1]nonane (0.5M solution in tetrahydrofuran, 228 ml) and reacted by stirring at room temperature for 4 hours. Under cooling with ice, a 3M sodium hydroxide solution (150 ml) and then a 30% hydrogen peroxide solution ...
10.6084/m9.figshare.5104873.v1
null
Peroxide.Vinyl
Primary alcohol
C1=C2CCCC[C@@H]2[C@H]2CC[C@@H]3CCC[C@H]3[C@@H]2C1
C1=C2CCCC[C@@H]2[C@H]2CC[C@@H]3CCC[C@H]3[C@@H]2C1
C1=C2CCCC[C@@H]2[C@H]2CC[C@@H]3CCC[C@H]3[C@@H]2C1
Other
CO
null
4
C=C1CC[C@H]2[C@@H]3CC=C4C[C@@H](O[Si](C)(C)C(C)(C)C)C[C@H](O[Si](C)(C)C(C)(C)C)[C@]4(C)[C@H]3CC[C@]12C.OO>CO>CC(C)(C)[Si](C)(C)O[C@@H]1CC2=CC[C@H]3[C@@H]4CC[C@H](CO)[C@@]4(C)CC[C@@H]3[C@@]2(C)[C@@H](O[Si](C)(C)C(C)(C)C)C1
ord_dataset-c3a75813d0b24864aa4f7cd526efd6aa
ord-4b555da856334d37b2959f11092ad220
C=CC(=O)N(C)C.CC(C)(C)[Si](C)(C)OC1CC2=CC[C@H]3[C@@H]4CC[C@H](CO)[C@@]4(C)CC[C@@H]3[C@@]2(C)[C@@H](O[Si](C)(C)C(C)(C)C)C1>>CN(C)C(=O)CCOC[C@H]1CC[C@H]2[C@@H]3CC=C4C[C@@H](O[Si](C)(C)C(C)(C)C)C[C@H](O[Si](C)(C)C(C)(C)C)[C@]4(C)[C@H]3CC[C@]12C
[Si](C)(C)(C(C)(C)C)O[C@H]1CC(CC2=CC[C@H]3[C@@H]4CC[C@@H]([C@@]4(C)CC[C@@H]3[C@@]12C)CO)O[Si](C)(C)C(C)(C)C.CN(C(C=C)=O)C.[H-].[Na+].C1COCCOCCOCCOCCO1.[Cl-].[NH4+]>>[Si](C)(C)(C(C)(C)C)O[C@H]1C[C@@H](CC2=CC[C@H]3[C@@H]4CC[C@@H]([C@@]4(C)CC[C@@H]3[C@@]12C)COCCC(=O)N(C)C)O[Si](C)(C)C(C)(C)C
[CH3:1][N:2]([CH3:3])[C:4](=[O:5])[CH:6]=[CH2:7].[OH:8][CH2:9][C@H:10]1[CH2:11][CH2:12][C@H:13]2[C@@H:14]3[CH2:15][CH:16]=[C:17]4[CH2:18][CH:19]([O:20][Si:21]([CH3:22])([CH3:23])[C:24]([CH3:25])([CH3:26])[CH3:27])[CH2:28][C@H:29]([O:30][Si:31]([CH3:32])([CH3:33])[C:34]([CH3:35])([CH3:36])[CH3:37])[C@:38]4([CH3:39])[C@H...
C=CC(=O)N(C)C.CC(C)(C)[Si](C)(C)OC1CC2=CC[C@H]3[C@@H]4CC[C@H](CO)[C@@]4(C)CC[C@@H]3[C@@]2(C)[C@@H](O[Si](C)(C)C(C)(C)C)C1
CN(C)C(=O)CCOC[C@H]1CC[C@H]2[C@@H]3CC=C4C[C@@H](O[Si](C)(C)C(C)(C)C)C[C@H](O[Si](C)(C)C(C)(C)C)[C@]4(C)[C@H]3CC[C@]12C
null
null
O1CCCC1
Heteroatom Alkylation and Arylation
oxa-Michael addition
f7c7da7c78eb65b9b2c8f63d0f16c4d5887e45e01ac1a9ea608f777c535e8cd7
d7c87de309863ac8797e1e336d1d5992291f9ca863376e68ebcf1e8fd5f0e442
C1=C2CCCCC2[C@H]2CCC3CCC[C@H]3[C@@H]2C1
[C;D1;H3:1]-[#7:2](-[C;D1;H3:3])-[C:4](=[O;D1;H0:5])-[CH;D2;+0:6]=[CH2;D1;+0:7].[C:8]-[C:9]-[OH;D1;+0:10]>>[C:8]-[C:9]-[O;H0;D2;+0:10]-[CH2;D2;+0:7]-[CH2;D2;+0:6]-[C:4](=[O;D1;H0:5])-[#7:2](-[C;D1;H3:1])-[C;D1;H3:3]
60.8
[{"value": 60.8, "product": "[Si](C)(C)(C(C)(C)C)O[C@H]1C[C@@H](CC2=CC[C@H]3[C@@H]4CC[C@@H]([C@@]4(C)CC[C@@H]3[C@@]12C)COCCC(=O)N(C)C)O[Si](C)(C)C(C)(C)C", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
null
null
To 1α,3-bis(tert-butyldimethylsilyloxy)-17β-(hydroxymethyl)androst-5-ene (18.4 g), was added N,N-dimethylacrylamide (9.95 g), sodium hydride (60% in oil, 2.0 g), 15-crown-5 (2.2 g) and tetrahydrofuran (73.5 ml), followed by reaction at 0° C. for 8 hours. After stopping the reaction by adding a saturated aqueous ammoniu...
10.6084/m9.figshare.5104873.v1
null
Primary alcohol.Vinyl
Ether
null
null
C1=C2CCCC[C@@H]2[C@H]2CC[C@@H]3CCC[C@H]3[C@@H]2C1
null
O1CCCC1
null
null
C=CC(=O)N(C)C.CC(C)(C)[Si](C)(C)OC1CC2=CC[C@H]3[C@@H]4CC[C@H](CO)[C@@]4(C)CC[C@@H]3[C@@]2(C)[C@@H](O[Si](C)(C)C(C)(C)C)C1>O1CCCC1>CN(C)C(=O)CCOC[C@H]1CC[C@H]2[C@@H]3CC=C4C[C@@H](O[Si](C)(C)C(C)(C)C)C[C@H](O[Si](C)(C)C(C)(C)C)[C@]4(C)[C@H]3CC[C@]12C
ord_dataset-c3a75813d0b24864aa4f7cd526efd6aa
ord-679f47ec92954ed5999bb1baa4b6b5fd
CC(C)(C#N)N=NC(C)(C)C#N.CCCCCC.CN(C)C(=O)CCOC[C@H]1CC[C@H]2[C@@H]3CC=C4C[C@@H](O[Si](C)(C)C(C)(C)C)C[C@H](O[Si](C)(C)C(C)(C)C)[C@]4(C)[C@H]3CC[C@]12C.O=C1CCC(=O)N1Br>>CN(C)C(=O)CCOC[C@H]1CC[C@H]2C3=CC=C4C[C@@H](O[Si](C)(C)C(C)(C)C)C[C@H](O[Si](C)(C)C(C)(C)C)[C@]4(C)[C@H]3CC[C@]12C.O=C1N=NC(=O)N1c1ccccc1
[Si](C)(C)(C(C)(C)C)O[C@H]1C[C@@H](CC2=CC[C@H]3[C@@H]4CC[C@@H]([C@@]4(C)CC[C@@H]3[C@@]12C)COCCC(=O)N(C)C)O[Si](C)(C)C(C)(C)C.BrN1C(CCC1=O)=O.N(=NC(C#N)(C)C)C(C#N)(C)C.CCCCCC>>C1(=CC=CC=C1)N1C(N=NC1=O)=O.[Si](C)(C)(C(C)(C)C)O[C@H]1C[C@@H](CC2=CC=C3[C@@H]4CC[C@@H]([C@@]4(C)CC[C@@H]3[C@@]12C)COCCC(=O)N(C)C)O[Si](C)(C)C(C)...
CC(C)(C#N)[N:47]=[N:48]C(C)(C)C#N.[CH3:52][CH2:57][CH2:56][CH2:55][CH2:54][CH3:53].[CH3:1][N:2]([CH3:3])[C:4](=[O:5])[CH2:6][CH2:7][O:8][CH2:9][C@H:10]1[CH2:11][CH2:12][C@H:13]2[C@@H:14]3[CH2:15][CH:16]=[C:17]4[CH2:18][C@@H:19]([O:20][Si:21]([CH3:22])([CH3:23])[C:24]([CH3:25])([CH3:26])[CH3:27])[CH2:28][C@H:29]([O:30][...
CC(C)(C#N)N=NC(C)(C)C#N.CCCCCC.CN(C)C(=O)CCOC[C@H]1CC[C@H]2[C@@H]3CC=C4C[C@@H](O[Si](C)(C)C(C)(C)C)C[C@H](O[Si](C)(C)C(C)(C)C)[C@]4(C)[C@H]3CC[C@]12C.O=C1CCC(=O)N1Br
CN(C)C(=O)CCOC[C@H]1CC[C@H]2C3=CC=C4C[C@@H](O[Si](C)(C)C(C)(C)C)C[C@H](O[Si](C)(C)C(C)(C)C)[C@]4(C)[C@H]3CC[C@]12C.O=C1N=NC(=O)N1c1ccccc1
null
null
O1CCCC1
Aromatic Heterocycle Formation
OtherReaction
83057f1ad2c8f1f7a09b95693a904e8d2b903f3ff7c23fef5e808847f97a5652
bc22e3b1b2c63e1c9de6e4cce4e1e3342dd819aa8074d8f4b543ef014f34b736
C1=C2CCCCC2[C@H]2CCC3CCC[C@H]3C2=C1.O=C1N=NC(=O)N1c1ccccc1
Br-[N;H0;D3;+0:1]1-[C;H0;D3;+0:2](=[O;D1;H0:3])-C-C-[C;H0;D3;+0:4]-1=[O;D1;H0:5].C-C(-C)(-C#N)-[N;H0;D2;+0:6]=[N;H0;D2;+0:7]-C(-C)(-C)-C#N.[CH3;D1;+0:8]-[CH2;D2;+0:9]-[CH2;D2;+0:10]-[CH2;D2;+0:11]-[CH2;D2;+0:12]-[CH3;D1;+0:13].[C:14]-[C:15](-[C:16])-[C@@H;D3;+0:17]1-[CH2;D2;+0:18]-[C:19]=[C:20](-[C:21])-[C:22]-[C:23]-1...
140.2
[{"value": 140.2, "product": "C1(=CC=CC=C1)N1C(N=NC1=O)=O.[Si](C)(C)(C(C)(C)C)O[C@H]1C[C@@H](CC2=CC=C3[C@@H]4CC[C@@H]([C@@]4(C)CC[C@@H]3[C@@]12C)COCCC(=O)N(C)C)O[Si](C)(C)C(C)(C)C", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
null
null
To 1α,3β-bis(tert-butyldimethylsilyloxy)-17β-(N,N-dimethylaminocarbonylethoxymethyl)androst-5-ene (15 g), were added N-bromosuccinimide (5.36 g), 2,2′-azobis isobutyronitrile (1.06 g), hexane (120 ml) and tetrahydrofuran (30 ml), followed by reflux under heating for 15 min. After cooling to room temperature, the mixtur...
10.6084/m9.figshare.5104873.v1
null
Diazene.Nitrile.Nitrile.Tertiary amide.Tertiary amide
Diazene.Substituted dicarboximide.Conjugated diene
C1=C2CCCC[C@@H]2[C@H]2CC[C@@H]3CCC[C@H]3[C@@H]2C1.C1CC[NH]C1
C1=C2CCCC[C@@H]2[C@H]2CC[C@@H]3CCC[C@H]3C2=C1.C1N=NC[NH]1.c1ccccc1
C1=C2CCCC[C@@H]2[C@H]2CC[C@@H]3CCC[C@H]3C2=C1.C1N=NC[NH]1.c1ccccc1
HBr
O1CCCC1
null
null
CC(C)(C#N)N=NC(C)(C)C#N.CCCCCC.CN(C)C(=O)CCOC[C@H]1CC[C@H]2[C@@H]3CC=C4C[C@@H](O[Si](C)(C)C(C)(C)C)C[C@H](O[Si](C)(C)C(C)(C)C)[C@]4(C)[C@H]3CC[C@]12C.O=C1CCC(=O)N1Br>O1CCCC1>CN(C)C(=O)CCOC[C@H]1CC[C@H]2C3=CC=C4C[C@@H](O[Si](C)(C)C(C)(C)C)C[C@H](O[Si](C)(C)C(C)(C)C)[C@]4(C)[C@H]3CC[C@]12C.O=C1N=NC(=O)N1c1ccccc1
ord_dataset-c3a75813d0b24864aa4f7cd526efd6aa
ord-5385123b715d4c92b06b49dff910a28e
CN(C)C(=O)CCOC[C@H]1CC[C@H]2C3=CC=C4C[C@@H](O[Si](C)(C)C(C)(C)C)C[C@H](O[Si](C)(C)C(C)(C)C)[C@]4(C)[C@H]3CC[C@]12C>>CC(C)(C)[Si](C)(C)O[C@@H]1CC2=CC=C3[C@@H]4CC[C@H](CO)[C@@]4(C)CC[C@@H]3[C@@]2(C)[C@@H](O[Si](C)(C)C(C)(C)C)C1
C1(=CC=CC=C1)N1C(N=NC1=O)=O.[Si](C)(C)(C(C)(C)C)O[C@H]1C[C@@H](CC2=CC=C3[C@@H]4CC[C@@H]([C@@]4(C)CC[C@@H]3[C@@]12C)COCCC(=O)N(C)C)O[Si](C)(C)C(C)(C)C.O1CCCC1.CC(C)([O-])C.[K+]>>C1(=CC=CC=C1)N1C(N=NC1=O)=O.[Si](C)(C)(C(C)(C)C)O[C@H]1C[C@@H](CC2=CC=C3[C@@H]4CC[C@@H]([C@@]4(C)CC[C@@H]3[C@@]12C)CO)O[Si](C)(C)C(C)(C)C
CN(C)C(=O)CC[O:20][CH2:19][C@H:18]1[CH2:17][CH2:16][C@H:15]2[C:14]3=[CH:13][CH:12]=[C:11]4[CH2:10][C@@H:9]([O:8][Si:5]([C:2]([CH3:1])([CH3:3])[CH3:4])([CH3:6])[CH3:7])[CH2:37][C@H:28]([O:29][Si:30]([CH3:31])([CH3:32])[C:33]([CH3:34])([CH3:35])[CH3:36])[C@:26]4([CH3:27])[C@H:25]3[CH2:24][CH2:23][C@@:21]21[CH3:22]>>[CH3:...
CN(C)C(=O)CCOC[C@H]1CC[C@H]2C3=CC=C4C[C@@H](O[Si](C)(C)C(C)(C)C)C[C@H](O[Si](C)(C)C(C)(C)C)[C@]4(C)[C@H]3CC[C@]12C
CC(C)(C)[Si](C)(C)O[C@@H]1CC2=CC=C3[C@@H]4CC[C@H](CO)[C@@]4(C)CC[C@@H]3[C@@]2(C)[C@@H](O[Si](C)(C)C(C)(C)C)C1
null
null
[Cl-].[Na+].O
Reduction
Cleavage of alkoxy ethers to alcohols
60ac9a93d999cff681f127f66d1aed73076ddbd2f72a568d7688aea508340e75
ed5b96494aea9c4ef78dc6eafcbfb0f1e3b4b57ea3d84f02d5723a8aad400f9f
C1=C2CCCCC2[C@H]2CCC3CCC[C@H]3C2=C1
C-N(-C)-C(=O)-C-C-[O;H0;D2;+0:1]-[C:2]-[C:3]>>[C:3]-[C:2]-[OH;D1;+0:1]
80.1
[{"value": 80.1, "product": "C1(=CC=CC=C1)N1C(N=NC1=O)=O.[Si](C)(C)(C(C)(C)C)O[C@H]1C[C@@H](CC2=CC=C3[C@@H]4CC[C@@H]([C@@]4(C)CC[C@@H]3[C@@]12C)CO)O[Si](C)(C)C(C)(C)C", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
null
null
To 1α,3β-bis(tert-butyldimethylsilyloxy)-17β-(N,N-dimethylaminocarbonylethoxymethyl)androsta-5,7-diene 4-phenyl-1,2,4-triazoline-3,5-dione adduct (9 g), were added tetrahydrofuran (90 ml) and then potassium t-butoxide (10.5 g), followed by reaction at room temperature for 10 min. After stopping the reaction by adding s...
10.6084/m9.figshare.5104873.v1
null
Ether.Tertiary amide
Primary alcohol
null
null
C1=C2CCCC[C@@H]2[C@H]2CC[C@@H]3CCC[C@H]3C2=C1
HO-
[Cl-].[Na+].O
null
null
CN(C)C(=O)CCOC[C@H]1CC[C@H]2C3=CC=C4C[C@@H](O[Si](C)(C)C(C)(C)C)C[C@H](O[Si](C)(C)C(C)(C)C)[C@]4(C)[C@H]3CC[C@]12C>[Cl-].[Na+].O>CC(C)(C)[Si](C)(C)O[C@@H]1CC2=CC=C3[C@@H]4CC[C@H](CO)[C@@]4(C)CC[C@@H]3[C@@]2(C)[C@@H](O[Si](C)(C)C(C)(C)C)C1
ord_dataset-c3a75813d0b24864aa4f7cd526efd6aa
ord-d4ff8f2783c34484a23ef81f6b6b95cc
CC(C)(C)[Si](C)(C)O[C@@H]1CC2=CC=C3[C@@H]4CC[C@H](CO)[C@@]4(C)CC[C@@H]3[C@@]2(C)[C@@H](O[Si](C)(C)C(C)(C)C)C1>>C[C@]12CC[C@H]3C(=CC=C4C[C@@H](O)C[C@H](O)[C@@]43C)[C@@H]1CC[C@@H]2CO
[Si](C)(C)(C(C)(C)C)O[C@H]1C[C@@H](CC2=CC=C3[C@@H]4CC[C@@H]([C@@]4(C)CC[C@@H]3[C@@]12C)CO)O[Si](C)(C)C(C)(C)C.O1CCCC1.[F-].C(CCC)[N+](CCCC)(CCCC)CCCC>>O[C@H]1C[C@@H](CC2=CC=C3[C@@H]4CC[C@@H]([C@@]4(C)CC[C@@H]3[C@@]12C)CO)O
CC(C)(C)[Si](C)(C)[O:12][C@@H:11]1[CH2:10][C:9]2=[CH:8][CH:7]=[C:6]3[C@H:5]([CH2:4][CH2:3][C@@:2]4([CH3:1])[C@H:18]3[CH2:19][CH2:20][C@@H:21]4[CH2:22][OH:23])[C@@:16]2([CH3:17])[C@@H:14]([O:15][Si](C)(C)C(C)(C)C)[CH2:13]1>>[CH3:1][C@:2]12[CH2:3][CH2:4][C@H:5]3[C:6](=[CH:7][CH:8]=[C:9]4[CH2:10][C@@H:11]([OH:12])[CH2:13]...
CC(C)(C)[Si](C)(C)O[C@@H]1CC2=CC=C3[C@@H]4CC[C@H](CO)[C@@]4(C)CC[C@@H]3[C@@]2(C)[C@@H](O[Si](C)(C)C(C)(C)C)C1
C[C@]12CC[C@H]3C(=CC=C4C[C@@H](O)C[C@H](O)[C@@]43C)[C@@H]1CC[C@@H]2CO
null
null
C(C)(=O)OCC
Deprotection
OtherReaction
3c4d3a3b788b4022df80488c890c930a0eff3addc93b825229adfe1b23285620
c96f1dab6a2ddd7b236398a198654bbc85e92a2fc2f6e88d092d4f9a3211cc52
C1=C2CCCCC2[C@H]2CCC3CCC[C@H]3C2=C1
C-C(-C)(-C)-[Si](-C)(-C)-[O;H0;D2;+0:1]-[C:2]1-[C:3]-[C:4](=[C:5])-[C:6]-[C:7](-[O;H0;D2;+0:8]-[Si](-C)(-C)-C(-C)(-C)-C)-[C:9]-1>>[C:5]=[C:4]1-[C:3]-[C:2](-[OH;D1;+0:1])-[C:9]-[C:7](-[OH;D1;+0:8])-[C:6]-1
96.2
[{"value": 96.2, "product": "O[C@H]1C[C@@H](CC2=CC=C3[C@@H]4CC[C@@H]([C@@]4(C)CC[C@@H]3[C@@]12C)CO)O", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
null
null
To 1α,3β-bis(tert-butyldimethylsilyloxy)-17β-(hydroxymethyl)androsta-5,7-diene (1.0 g), was added a 1M tetra-n-butylammonium fluoride tetrahydrofuran solution (11 ml), followed by reflux for 6 hours. After adding ethyl acetate, the reaction mixture was washed with saturated brine, a saturated aqueous sodium bicarbonate...
10.6084/m9.figshare.5104873.v1
null
TMS ether protective group.TMS ether protective group
Secondary alcohol.Secondary alcohol
null
null
C1=C2CCCC[C@@H]2[C@H]2CC[C@H]3CCC[C@H]3C2=C1
Other
C(C)(=O)OCC
null
null
CC(C)(C)[Si](C)(C)O[C@@H]1CC2=CC=C3[C@@H]4CC[C@H](CO)[C@@]4(C)CC[C@@H]3[C@@]2(C)[C@@H](O[Si](C)(C)C(C)(C)C)C1>C(C)(=O)OCC>C[C@]12CC[C@H]3C(=CC=C4C[C@@H](O)C[C@H](O)[C@@]43C)[C@@H]1CC[C@@H]2CO
ord_dataset-c3a75813d0b24864aa4f7cd526efd6aa
ord-851c9b370e384106b3146c8a63abe960
CC(C)(C)[Si](C)(C)O[C@@H]1CC2=CC[C@H]3[C@@H]4CC[C@H](CO)[C@@]4(C)CC[C@@H]3[C@@]2(C)[C@@H](O[Si](C)(C)C(C)(C)C)C1.CCC(CC)(CCCBr)O[Si](CC)(CC)CC>>CCC(CC)(CCCOC[C@H]1CC[C@H]2[C@@H]3CC=C4C[C@@H](O[Si](C)(C)C(C)(C)C)C[C@H](O[Si](C)(C)C(C)(C)C)[C@]4(C)[C@H]3CC[C@]12C)O[Si](CC)(CC)CC
BrCCCC(CC)(O[Si](CC)(CC)CC)CC.[H-].[K+].C1COCCOCCOCCOCCOCCO1.[Si](C)(C)(C(C)(C)C)O[C@H]1C[C@@H](CC2=CC[C@H]3[C@@H]4CC[C@@H]([C@@]4(C)CC[C@@H]3[C@@]12C)CO)O[Si](C)(C)C(C)(C)C.[Cl-].[NH4+]>>[Si](C)(C)(C(C)(C)C)O[C@H]1C[C@@H](CC2=CC[C@H]3[C@@H]4CC[C@@H]([C@@]4(C)CC[C@@H]3[C@@]12C)COCCCC(CC)(O[Si](CC)(CC)CC)CC)O[Si](C)(C)C...
[OH:9][CH2:10][C@H:11]1[CH2:12][CH2:13][C@H:14]2[C@@H:15]3[CH2:16][CH:17]=[C:18]4[CH2:19][C@@H:20]([O:21][Si:22]([CH3:23])([CH3:24])[C:25]([CH3:26])([CH3:27])[CH3:28])[CH2:29][C@H:30]([O:31][Si:32]([CH3:33])([CH3:34])[C:35]([CH3:36])([CH3:37])[CH3:38])[C@:39]4([CH3:40])[C@H:41]3[CH2:42][CH2:43][C@:44]12[CH3:45].Br[CH2:...
CC(C)(C)[Si](C)(C)O[C@@H]1CC2=CC[C@H]3[C@@H]4CC[C@H](CO)[C@@]4(C)CC[C@@H]3[C@@]2(C)[C@@H](O[Si](C)(C)C(C)(C)C)C1.CCC(CC)(CCCBr)O[Si](CC)(CC)CC
CCC(CC)(CCCOC[C@H]1CC[C@H]2[C@@H]3CC=C4C[C@@H](O[Si](C)(C)C(C)(C)C)C[C@H](O[Si](C)(C)C(C)(C)C)[C@]4(C)[C@H]3CC[C@]12C)O[Si](CC)(CC)CC
null
null
O1CCCC1
Heteroatom Alkylation and Arylation
Williamson Ether Synthesis
dd3f9c60e1f90d961a7c01d970ae213561355ee1451f276a3b04696e4b6fae5c
46a6e883cf919b4006e69abfdfd883f458f55c08b3200960c6a5b57c4139fbca
C1=C2CCCCC2[C@H]2CCC3CCC[C@H]3[C@@H]2C1
Br-[CH2;D2;+0:1]-[C:2]-[C:3].[C:4]-[C:5]-[OH;D1;+0:6]>>[C:4]-[C:5]-[O;H0;D2;+0:6]-[CH2;D2;+0:1]-[C:2]-[C:3]
99.6
[{"value": 99.6, "product": "[Si](C)(C)(C(C)(C)C)O[C@H]1C[C@@H](CC2=CC[C@H]3[C@@H]4CC[C@@H]([C@@]4(C)CC[C@@H]3[C@@]12C)COCCCC(CC)(O[Si](CC)(CC)CC)CC)O[Si](C)(C)C(C)(C)C", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
5
MINUTE
1α,3β-Bis(tert-butyldimethylsilyloxy)-17β-(hydroxymethyl)androst-5-ene (11.0 g) was dissolved in tetrahydrofuran. Under cooling with ice, potassium hydride (30% in oil, 200.3 g) and 18-crown-6 (2.64 g) were added to the solution, which was then stirred for 5 min. 1-Bromo-4-ethyl-4-(triethylsilyloxy)hexane (25.91 g) was...
10.6084/m9.figshare.5104873.v1
null
Primary halide.Primary alcohol
Ether
null
null
C1=C2CCCC[C@@H]2[C@H]2CC[C@@H]3CCC[C@H]3[C@@H]2C1
HBr
O1CCCC1
null
0.083333
CC(C)(C)[Si](C)(C)O[C@@H]1CC2=CC[C@H]3[C@@H]4CC[C@H](CO)[C@@]4(C)CC[C@@H]3[C@@]2(C)[C@@H](O[Si](C)(C)C(C)(C)C)C1.CCC(CC)(CCCBr)O[Si](CC)(CC)CC>O1CCCC1>CCC(CC)(CCCOC[C@H]1CC[C@H]2[C@@H]3CC=C4C[C@@H](O[Si](C)(C)C(C)(C)C)C[C@H](O[Si](C)(C)C(C)(C)C)[C@]4(C)[C@H]3CC[C@]12C)O[Si](CC)(CC)CC
ord_dataset-c3a75813d0b24864aa4f7cd526efd6aa
ord-d995151a34f5417984c86604a34de416
CCC(CC)(CCCOC[C@H]1CC[C@H]2[C@@H]3CC=C4C[C@@H](O[Si](C)(C)C(C)(C)C)C[C@H](O[Si](C)(C)C(C)(C)C)[C@]4(C)[C@H]3CC[C@]12C)O[Si](CC)(CC)CC>>CCC(CC)(CCCOC[C@H]1CC[C@H]2C3=CC=C4C[C@@H](O[Si](C)(C)C(C)(C)C)C[C@H](O[Si](C)(C)C(C)(C)C)[C@]4(C)[C@H]3CC[C@]12C)O[Si](CC)(CC)CC
C1(=CC=CC=C1)N1C(N=NC1=O)=O.N(=NC(C#N)(C)C)C(C#N)(C)C.[Si](C)(C)(C(C)(C)C)O[C@H]1C[C@@H](CC2=CC[C@H]3[C@@H]4CC[C@@H]([C@@]4(C)CC[C@@H]3[C@@]12C)COCCCC(CC)(O[Si](CC)(CC)CC)CC)O[Si](C)(C)C(C)(C)C.BrN1C(CCC1=O)=O>>C1(=CC=CC=C1)N1C(N=NC1=O)=O.[Si](C)(C)(C(C)(C)C)O[C@H]1C[C@@H](CC2=CC=C3[C@@H]4CC[C@@H]([C@@]4(C)CC[C@@H]3[C@...
[CH3:1][CH2:2][C:3]([CH2:4][CH3:5])([CH2:6][CH2:7][CH2:8][O:9][CH2:10][C@H:11]1[CH2:12][CH2:13][C@H:14]2[C@@H:15]3[CH2:16][CH:17]=[C:18]4[CH2:19][C@@H:20]([O:21][Si:22]([CH3:23])([CH3:24])[C:25]([CH3:26])([CH3:27])[CH3:28])[CH2:29][C@H:30]([O:31][Si:32]([CH3:33])([CH3:34])[C:35]([CH3:36])([CH3:37])[CH3:38])[C@:39]4([CH...
CCC(CC)(CCCOC[C@H]1CC[C@H]2[C@@H]3CC=C4C[C@@H](O[Si](C)(C)C(C)(C)C)C[C@H](O[Si](C)(C)C(C)(C)C)[C@]4(C)[C@H]3CC[C@]12C)O[Si](CC)(CC)CC
CCC(CC)(CCCOC[C@H]1CC[C@H]2C3=CC=C4C[C@@H](O[Si](C)(C)C(C)(C)C)C[C@H](O[Si](C)(C)C(C)(C)C)[C@]4(C)[C@H]3CC[C@]12C)O[Si](CC)(CC)CC
null
null
CCCCCC
Oxidation
OtherReaction
59e599993b7b3b967c8da247b1e66f54ad495c7a1835473b960fabbca47978b2
0b9fdf82b0e2b620f0b6676b9714eb5a5219404b4adc877f914530378ab5be4a
C1=C2CCCCC2[C@H]2CCC3CCC[C@H]3C2=C1
[C:1]-[C:2](-[C:3])-[C@@H;D3;+0:4]1-[CH2;D2;+0:5]-[C:6]=[C:7](-[C:8])-[C:9]-[C:10]-1-[C:11]>>[C:1]-[C:2](-[C:3])-[C;H0;D3;+0:4]1=[CH;D2;+0:5]-[C:6]=[C:7](-[C:8])-[C:9]-[C:10]-1-[C:11]
null
[]
null
null
null
null
To 1α,3β-bis(tert-butyldimethylsilyloxy)-17β-{4-ethyl-4-(triethylsilyloxy)hexyloxymethyl}androst-5-ene (1.0 g), were added hexane (15 ml), N-bromosuccinimide (336.4 mg) and then 2,2′-azobis isobutyronitrile (77.6 mg), followed by reaction under reflux for 30 min. After cooling with ice, the mixture was filtered to remo...
10.6084/m9.figshare.5104873.v1
null
null
Conjugated diene
C1=C2CCCC[C@@H]2[C@H]2CC[C@@H]3CCC[C@H]3[C@@H]2C1
C1=C2CCCC[C@@H]2[C@H]2CC[C@@H]3CCC[C@H]3C2=C1
C1=C2CCCC[C@@H]2[C@H]2CC[C@@H]3CCC[C@H]3C2=C1
null
CCCCCC
null
null
CCC(CC)(CCCOC[C@H]1CC[C@H]2[C@@H]3CC=C4C[C@@H](O[Si](C)(C)C(C)(C)C)C[C@H](O[Si](C)(C)C(C)(C)C)[C@]4(C)[C@H]3CC[C@]12C)O[Si](CC)(CC)CC>CCCCCC>CCC(CC)(CCCOC[C@H]1CC[C@H]2C3=CC=C4C[C@@H](O[Si](C)(C)C(C)(C)C)C[C@H](O[Si](C)(C)C(C)(C)C)[C@]4(C)[C@H]3CC[C@]12C)O[Si](CC)(CC)CC
ord_dataset-c3a75813d0b24864aa4f7cd526efd6aa
ord-a9a7ef79a04e4412a1b1f87986ec6afe
CC(C)(O)CCOC[C@H]1CC[C@H]2C3=CC=C4C[C@@H](O[Si](C)(C)C(C)(C)C)C[C@H](O[Si](C)(C)C(C)(C)C)[C@]4(C)[C@H]3CC[C@]12C>>CC(C)(O)CCOC[C@H]1CC[C@H]2C3=CC=C4C[C@@H](O)C[C@H](O)[C@]4(C)[C@H]3CC[C@]12C
[Si](C)(C)(C(C)(C)C)O[C@H]1C[C@@H](CC2=CC=C3[C@@H]4CC[C@@H]([C@@]4(C)CC[C@@H]3[C@@]12C)COCCC(C)(C)O)O[Si](C)(C)C(C)(C)C.O1CCCC1.[F-].C(CCC)[N+](CCCC)(CCCC)CCCC>>O[C@H]1C[C@@H](CC2=CC=C3[C@@H]4CC[C@@H]([C@@]4(C)CC[C@@H]3[C@@]12C)COCCC(C)(C)O)O
CC(C)(C)[Si](C)(C)[O:19][C@@H:18]1[CH2:17][C:16]2=[CH:15][CH:14]=[C:13]3[C@@H:12]4[CH2:11][CH2:10][C@H:9]([CH2:8][O:7][CH2:6][CH2:5][C:2]([CH3:1])([CH3:3])[OH:4])[C@@:28]4([CH3:29])[CH2:27][CH2:26][C@@H:25]3[C@@:23]2([CH3:24])[C@@H:21]([O:22][Si](C)(C)C(C)(C)C)[CH2:20]1>>[CH3:1][C:2]([CH3:3])([OH:4])[CH2:5][CH2:6][O:7]...
CC(C)(O)CCOC[C@H]1CC[C@H]2C3=CC=C4C[C@@H](O[Si](C)(C)C(C)(C)C)C[C@H](O[Si](C)(C)C(C)(C)C)[C@]4(C)[C@H]3CC[C@]12C
CC(C)(O)CCOC[C@H]1CC[C@H]2C3=CC=C4C[C@@H](O)C[C@H](O)[C@]4(C)[C@H]3CC[C@]12C
null
null
C(C)(=O)OCC
Deprotection
OtherReaction
3c4d3a3b788b4022df80488c890c930a0eff3addc93b825229adfe1b23285620
c96f1dab6a2ddd7b236398a198654bbc85e92a2fc2f6e88d092d4f9a3211cc52
C1=C2CCCCC2[C@H]2CCC3CCC[C@H]3C2=C1
C-C(-C)(-C)-[Si](-C)(-C)-[O;H0;D2;+0:1]-[C:2]1-[C:3]-[C:4](=[C:5])-[C:6]-[C:7](-[O;H0;D2;+0:8]-[Si](-C)(-C)-C(-C)(-C)-C)-[C:9]-1>>[C:5]=[C:4]1-[C:3]-[C:2](-[OH;D1;+0:1])-[C:9]-[C:7](-[OH;D1;+0:8])-[C:6]-1
91.7
[{"value": 91.7, "product": "O[C@H]1C[C@@H](CC2=CC=C3[C@@H]4CC[C@@H]([C@@]4(C)CC[C@@H]3[C@@]12C)COCCC(C)(C)O)O", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
null
null
To 1α,3β-bis(tert-butyldimethylsilyloxy)-17β-(3-hydroxy-3-methylbutoxymethyl)androsta-5,7-diene (700 mg), was added a 1M tetra-n-butylammonium fluoride tetrahydrofuran solution (20 ml), followed by reaction for 6 hours. After adding ethyl acetate, the reaction mixture was washed with saturated brine, a saturated aqueou...
10.6084/m9.figshare.5104873.v1
null
TMS ether protective group.TMS ether protective group
Secondary alcohol.Secondary alcohol
null
null
C1=C2CCCC[C@@H]2[C@H]2CC[C@@H]3CCC[C@H]3C2=C1
Other
C(C)(=O)OCC
null
null
CC(C)(O)CCOC[C@H]1CC[C@H]2C3=CC=C4C[C@@H](O[Si](C)(C)C(C)(C)C)C[C@H](O[Si](C)(C)C(C)(C)C)[C@]4(C)[C@H]3CC[C@]12C>C(C)(=O)OCC>CC(C)(O)CCOC[C@H]1CC[C@H]2C3=CC=C4C[C@@H](O)C[C@H](O)[C@]4(C)[C@H]3CC[C@]12C
ord_dataset-c3a75813d0b24864aa4f7cd526efd6aa
ord-4b7011ffb0c84fa6b7126d0ffa4f7f41
CC(C)(C)[Si](C)(C)O[C@@H]1CC2=CC=C3[C@@H]4CC[C@H](CO)[C@@]4(C)CC[C@@H]3[C@@]2(C)[C@@H](O[Si](C)(C)C(C)(C)C)C1.CS(=O)(=O)Cl>>CC(C)(C)[Si](C)(C)O[C@@H]1CC2=CC=C3[C@@H]4CC[C@H](COS(C)(=O)=O)[C@@]4(C)CC[C@@H]3[C@@]2(C)[C@@H](O[Si](C)(C)C(C)(C)C)C1
[Si](C)(C)(C(C)(C)C)O[C@H]1C[C@@H](CC2=CC=C3[C@@H]4CC[C@@H]([C@@]4(C)CC[C@@H]3[C@@]12C)CO)O[Si](C)(C)C(C)(C)C.C(C)N(CC)CC.CS(=O)(=O)Cl>>[Si](C)(C)(C(C)(C)C)O[C@H]1C[C@@H](CC2=CC=C3[C@@H]4CC[C@@H]([C@@]4(C)CC[C@@H]3[C@@]12C)COS(=O)(=O)C)O[Si](C)(C)C(C)(C)C
[CH3:1][C:2]([CH3:3])([CH3:4])[Si:5]([CH3:6])([CH3:7])[O:8][C@@H:9]1[CH2:10][C:11]2=[CH:12][CH:13]=[C:14]3[C@@H:15]4[CH2:16][CH2:17][C@H:18]([CH2:19][OH:20])[C@@:25]4([CH3:26])[CH2:27][CH2:28][C@@H:29]3[C@@:30]2([CH3:31])[C@@H:32]([O:33][Si:34]([CH3:35])([CH3:36])[C:37]([CH3:38])([CH3:39])[CH3:40])[CH2:41]1.Cl[S:21]([C...
CC(C)(C)[Si](C)(C)O[C@@H]1CC2=CC=C3[C@@H]4CC[C@H](CO)[C@@]4(C)CC[C@@H]3[C@@]2(C)[C@@H](O[Si](C)(C)C(C)(C)C)C1.CS(=O)(=O)Cl
CC(C)(C)[Si](C)(C)O[C@@H]1CC2=CC=C3[C@@H]4CC[C@H](COS(C)(=O)=O)[C@@]4(C)CC[C@@H]3[C@@]2(C)[C@@H](O[Si](C)(C)C(C)(C)C)C1
null
null
O1CCCC1.CCCCCC
Acylation
Formation of Sulfonic Esters
2fa969eb2c954bb96793348a1b2335ec63fbd290dadec6e3e02295e1768e64cf
cb77b899e4adf980b1def97230ef2861660fd7f9602260ec64747d9afd3a795a
C1=C2CCCCC2[C@H]2CCC3CCC[C@H]3C2=C1
Cl-[S;H0;D4;+0:1](-[C;D1;H3:2])(=[O;D1;H0:3])=[O;D1;H0:4].[C:5]-[C:6]-[OH;D1;+0:7]>>[C:5]-[C:6]-[O;H0;D2;+0:7]-[S;H0;D4;+0:1](-[C;D1;H3:2])(=[O;D1;H0:3])=[O;D1;H0:4]
91
[{"value": 91.0, "product": "[Si](C)(C)(C(C)(C)C)O[C@H]1C[C@@H](CC2=CC=C3[C@@H]4CC[C@@H]([C@@]4(C)CC[C@@H]3[C@@]12C)COS(=O)(=O)C)O[Si](C)(C)C(C)(C)C", "details": "PERCENTYIELD", "is_desired": false}, {"value": 90.5, "product": "[Si](C)(C)(C(C)(C)C)O[C@H]1C[C@@H](CC2=CC=C3[C@@H]4CC[C@@H]([C@@]4(C)CC[C@@H]3[C@@]12C)COS(=...
0
CELSIUS
1
HOUR
A solution of 1α,3β-bis(tert-butyldimethylsilyloxy)-17β-(hydroxymethyl)androsta-5,7-diene (150 mg, 0.274 mmol) and triethylamine (0.153 ml, 1.10 mmol) in tetrahydrofuran (2.3 ml) was cooled to 0° C., followed by the addition of methanesulfonyl chloride (63 μl, 0.814 mmol) and stirring at 0° C. for 1 hour. The reaction ...
10.6084/m9.figshare.5104873.v1
null
Primary alcohol.Sulfonyl halide
Mesylate
null
null
C1=C2CCCC[C@@H]2[C@H]2CC[C@@H]3CCC[C@H]3C2=C1
HCl
O1CCCC1.CCCCCC
0
1
CC(C)(C)[Si](C)(C)O[C@@H]1CC2=CC=C3[C@@H]4CC[C@H](CO)[C@@]4(C)CC[C@@H]3[C@@]2(C)[C@@H](O[Si](C)(C)C(C)(C)C)C1.CS(=O)(=O)Cl>O1CCCC1.CCCCCC>CC(C)(C)[Si](C)(C)O[C@@H]1CC2=CC=C3[C@@H]4CC[C@H](COS(C)(=O)=O)[C@@]4(C)CC[C@@H]3[C@@]2(C)[C@@H](O[Si](C)(C)C(C)(C)C)C1
ord_dataset-c3a75813d0b24864aa4f7cd526efd6aa
ord-bde3da8b39744ff283da6cf2d0b42318
CC(=O)SC[C@H]1CC[C@H]2C3=CC=C4C[C@@H](O[Si](C)(C)C(C)(C)C)C[C@H](O[Si](C)(C)C(C)(C)C)[C@]4(C)[C@H]3CC[C@]12C.CC(C)(O)CCBr>>CC(C)(O)CCSC[C@H]1CC[C@H]2C3=CC=C4C[C@@H](O[Si](C)(C)C(C)(C)C)C[C@H](O[Si](C)(C)C(C)(C)C)[C@]4(C)[C@H]3CC[C@]12C
[Si](C)(C)(C(C)(C)C)O[C@H]1C[C@@H](CC2=CC=C3[C@@H]4CC[C@@H]([C@@]4(C)CC[C@@H]3[C@@]12C)CSC(C)=O)O[Si](C)(C)C(C)(C)C.BrCCC(C)(O)C.CO.[OH-].[K+]>>[Si](C)(C)(C(C)(C)C)O[C@H]1C[C@@H](CC2=CC=C3[C@@H]4CC[C@@H]([C@@]4(C)CC[C@@H]3[C@@]12C)CSCCC(C)(C)O)O[Si](C)(C)C(C)(C)C
CC(=O)[S:7][CH2:8][C@H:9]1[CH2:10][CH2:11][C@H:12]2[C:13]3=[CH:14][CH:15]=[C:16]4[CH2:17][C@@H:18]([O:19][Si:20]([CH3:21])([CH3:22])[C:23]([CH3:24])([CH3:25])[CH3:26])[CH2:27][C@H:28]([O:29][Si:30]([CH3:31])([CH3:32])[C:33]([CH3:34])([CH3:35])[CH3:36])[C@:37]4([CH3:38])[C@H:39]3[CH2:40][CH2:41][C@:42]12[CH3:43].Br[CH2:...
CC(=O)SC[C@H]1CC[C@H]2C3=CC=C4C[C@@H](O[Si](C)(C)C(C)(C)C)C[C@H](O[Si](C)(C)C(C)(C)C)[C@]4(C)[C@H]3CC[C@]12C.CC(C)(O)CCBr
CC(C)(O)CCSC[C@H]1CC[C@H]2C3=CC=C4C[C@@H](O[Si](C)(C)C(C)(C)C)C[C@H](O[Si](C)(C)C(C)(C)C)[C@]4(C)[C@H]3CC[C@]12C
null
null
O1CCCC1
Heteroatom Alkylation and Arylation
OtherReaction
ac55b1813a50f413501bd3cd7115530e7b82e267a203d71b1e207485ab027747
2e4a9869295789d93ad40520a43348bbebd282f62196fc6899c2f5df92cb929d
C1=C2CCCCC2[C@H]2CCC3CCC[C@H]3C2=C1
Br-[CH2;D2;+0:1]-[C:2]-[C:3].C-C(=O)-[S;H0;D2;+0:4]-[C:5]-[C:6]>>[C:3]-[C:2]-[CH2;D2;+0:1]-[S;H0;D2;+0:4]-[C:5]-[C:6]
90.5
[{"value": 90.0, "product": "[Si](C)(C)(C(C)(C)C)O[C@H]1C[C@@H](CC2=CC=C3[C@@H]4CC[C@@H]([C@@]4(C)CC[C@@H]3[C@@]12C)CSCCC(C)(C)O)O[Si](C)(C)C(C)(C)C", "details": "PERCENTYIELD", "is_desired": false}, {"value": 90.5, "product": "[Si](C)(C)(C(C)(C)C)O[C@H]1C[C@@H](CC2=CC=C3[C@@H]4CC[C@@H]([C@@]4(C)CC[C@@H]3[C@@]12C)CSCCC...
null
null
1
HOUR
To a solution of 1α,3β-bis(tert-butyldimethylsilyloxy)-17β-(acetylthiomethyl)androsta-5,7-diene (135 mg, 0.223 mmol) and 4-bromo-2-methylbutan-2-ol (186 mg, 1.12 mmol) in tetrahydrofuran (1.5 ml), was added a 1M potassium hydroxide methanol solution (1.5 ml), followed by stirring at room temperature for 1 hour. The rea...
10.6084/m9.figshare.5104873.v1
null
Primary halide.Carbo-thioester
Monosulfide
null
null
C1=C2CCCC[C@@H]2[C@H]2CC[C@@H]3CCC[C@H]3C2=C1
HBr
O1CCCC1
null
1
CC(=O)SC[C@H]1CC[C@H]2C3=CC=C4C[C@@H](O[Si](C)(C)C(C)(C)C)C[C@H](O[Si](C)(C)C(C)(C)C)[C@]4(C)[C@H]3CC[C@]12C.CC(C)(O)CCBr>O1CCCC1>CC(C)(O)CCSC[C@H]1CC[C@H]2C3=CC=C4C[C@@H](O[Si](C)(C)C(C)(C)C)C[C@H](O[Si](C)(C)C(C)(C)C)[C@]4(C)[C@H]3CC[C@]12C
ord_dataset-c3a75813d0b24864aa4f7cd526efd6aa
ord-1a56bf1980954911b5d4f2db94f288e4
CC(C)(O)CCSC[C@H]1CC[C@H]2C3=CC=C4C[C@@H](O[Si](C)(C)C(C)(C)C)C[C@H](O[Si](C)(C)C(C)(C)C)[C@]4(C)[C@H]3CC[C@]12C>>CC(C)(O)CCSC[C@H]1CC[C@H]2C3=CC=C4C[C@@H](O)C[C@H](O)[C@]4(C)[C@H]3CC[C@]12C
[Si](C)(C)(C(C)(C)C)O[C@H]1C[C@@H](CC2=CC=C3[C@@H]4CC[C@@H]([C@@]4(C)CC[C@@H]3[C@@]12C)CSCCC(C)(C)O)O[Si](C)(C)C(C)(C)C.O1CCCC1.[F-].C(CCC)[N+](CCCC)(CCCC)CCCC>>O[C@H]1C[C@@H](CC2=CC=C3[C@@H]4CC[C@@H]([C@@]4(C)CC[C@@H]3[C@@]12C)CSCCC(C)(C)O)O
CC(C)(C)[Si](C)(C)[O:19][C@@H:18]1[CH2:17][C:16]2=[CH:15][CH:14]=[C:13]3[C@@H:12]4[CH2:11][CH2:10][C@H:9]([CH2:8][S:7][CH2:6][CH2:5][C:2]([CH3:1])([CH3:3])[OH:4])[C@@:28]4([CH3:29])[CH2:27][CH2:26][C@@H:25]3[C@@:23]2([CH3:24])[C@@H:21]([O:22][Si](C)(C)C(C)(C)C)[CH2:20]1>>[CH3:1][C:2]([CH3:3])([OH:4])[CH2:5][CH2:6][S:7]...
CC(C)(O)CCSC[C@H]1CC[C@H]2C3=CC=C4C[C@@H](O[Si](C)(C)C(C)(C)C)C[C@H](O[Si](C)(C)C(C)(C)C)[C@]4(C)[C@H]3CC[C@]12C
CC(C)(O)CCSC[C@H]1CC[C@H]2C3=CC=C4C[C@@H](O)C[C@H](O)[C@]4(C)[C@H]3CC[C@]12C
null
null
O1CCCC1.C(C)(=O)OCC
Deprotection
OtherReaction
3c4d3a3b788b4022df80488c890c930a0eff3addc93b825229adfe1b23285620
c96f1dab6a2ddd7b236398a198654bbc85e92a2fc2f6e88d092d4f9a3211cc52
C1=C2CCCCC2[C@H]2CCC3CCC[C@H]3C2=C1
C-C(-C)(-C)-[Si](-C)(-C)-[O;H0;D2;+0:1]-[C:2]1-[C:3]-[C:4](=[C:5])-[C:6]-[C:7](-[O;H0;D2;+0:8]-[Si](-C)(-C)-C(-C)(-C)-C)-[C:9]-1>>[C:5]=[C:4]1-[C:3]-[C:2](-[OH;D1;+0:1])-[C:9]-[C:7](-[OH;D1;+0:8])-[C:6]-1
84
[{"value": 84.0, "product": "O[C@H]1C[C@@H](CC2=CC=C3[C@@H]4CC[C@@H]([C@@]4(C)CC[C@@H]3[C@@]12C)CSCCC(C)(C)O)O", "details": "PERCENTYIELD", "is_desired": false}, {"value": 83.9, "product": "O[C@H]1C[C@@H](CC2=CC=C3[C@@H]4CC[C@@H]([C@@]4(C)CC[C@@H]3[C@@]12C)CSCCC(C)(C)O)O", "details": "CALCULATEDPERCENTYIELD", "is_desir...
null
null
null
null
To a solution of 1α,3β-bis(tert-butyldimethylsilyloxy)-17β-(3-hydroxy-3-methylbutylthiomethyl)androsta-5,7-diene (130 mg, 0.215 mmol) in tetrahydrofuran (1 ml), was added a 1M tetra-n-butylammonium fluoride tetrahydrofuran solution (2.15 ml, 2.15 mmol), followed by reflux under heating for 5 hours. The reaction mixture...
10.6084/m9.figshare.5104873.v1
null
TMS ether protective group.TMS ether protective group
Secondary alcohol.Secondary alcohol
null
null
C1=C2CCCC[C@@H]2[C@H]2CC[C@@H]3CCC[C@H]3C2=C1
Other
O1CCCC1.C(C)(=O)OCC
null
null
CC(C)(O)CCSC[C@H]1CC[C@H]2C3=CC=C4C[C@@H](O[Si](C)(C)C(C)(C)C)C[C@H](O[Si](C)(C)C(C)(C)C)[C@]4(C)[C@H]3CC[C@]12C>O1CCCC1.C(C)(=O)OCC>CC(C)(O)CCSC[C@H]1CC[C@H]2C3=CC=C4C[C@@H](O)C[C@H](O)[C@]4(C)[C@H]3CC[C@]12C
ord_dataset-c3a75813d0b24864aa4f7cd526efd6aa
ord-917ca00bfa7848439af464b8b18dd5bb
CNN.COc1ccc(OC)c(C(=O)O)c1.COc1ccc(P2(=S)SP(=S)(c3ccc(OC)cc3)S2)cc1>>COc1ccc(OC)c(C(=S)N(C)N)c1
C1CCC(CC1)N=C=NC2CCCCC2.COC1=C(C(=O)O)C=C(C=C1)OC.CNN.COC=1C=CC(=CC1)P2(=S)SP(=S)(S2)C=3C=CC(=CC3)OC>>CN(N)C(C1=C(C=CC(=C1)OC)OC)=S
[NH:12]([CH3:13])[NH2:14].O=[C:10](O)[c:9]1[c:6]([O:7][CH3:8])[cH:5][cH:4][c:3]([O:2][CH3:1])[cH:15]1.COc1ccc(P2(=S)SP(c3ccc(OC)cc3)(=[S:11])S2)cc1>>[CH3:1][O:2][c:3]1[cH:4][cH:5][c:6]([O:7][CH3:8])[c:9]([C:10](=[S:11])[N:12]([CH3:13])[NH2:14])[cH:15]1
CNN.COc1ccc(OC)c(C(=O)O)c1.COc1ccc(P2(=S)SP(=S)(c3ccc(OC)cc3)S2)cc1
COc1ccc(OC)c(C(=S)N(C)N)c1
null
CN(C)C=1C=CN=CC1
C(Cl)Cl.C(C)(=O)OCC
Heteroatom Alkylation and Arylation
OtherReaction
47d7c2005d1e7811627afd45f1badff9791a2fb612e24bc6785162cdb2f64974
bfbc8035f907b8a9898ad994e28561387663bddd432650d77e24e3cb196c5bc2
c1ccccc1
C-O-c1:c:c:c(-P2(=S)-S-P(=[S;H0;D1;+0:1])(-c3:c:c:c(-O-C):c:c:3)-S-2):c:c:1.O-[C;H0;D3;+0:2](=O)-[c:3](:[c:4]):[c:5].[C;D1;H3:6]-[NH;D2;+0:7]-[N;D1;H2:8]>>[C;D1;H3:6]-[N;H0;D3;+0:7](-[N;D1;H2:8])-[C;H0;D3;+0:2](=[S;H0;D1;+0:1])-[c:3](:[c:4]):[c:5]
116.8
[{"value": 82.0, "product": "CN(N)C(C1=C(C=CC(=C1)OC)OC)=S", "details": "PERCENTYIELD", "is_desired": false}, {"value": 116.8, "product": "CN(N)C(C1=C(C=CC(=C1)OC)OC)=S", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
8
HOUR
DCC (4.5 g, 21.8 mmol) was added in one portion to a solution of 2,5-dimethoxybenzoic acid (3.6 g, 20 mol), methylhydrazine (1.2 ml, 23 mmol) and DMAP (30 mg, cat.) in CH2Cl2(60 ml) cooled in an ice bath. The reaction mixture was stirred overnight at room temperature. The slurry was cooled at −20° C. for 1 h and filter...
10.6084/m9.figshare.5104873.v1
null
Hydrazine.Carboxylic acid.Ether.Ether.Monosulfide.Monosulfide
Hydrazine.Thioamide
c1ccccc1.P1SPS1.c1ccccc1
null
c1ccccc1
Other
CN(C)C=1C=CN=CC1.C(Cl)Cl.C(C)(=O)OCC
null
8
CNN.COc1ccc(OC)c(C(=O)O)c1.COc1ccc(P2(=S)SP(=S)(c3ccc(OC)cc3)S2)cc1>CN(C)C=1C=CN=CC1.C(Cl)Cl.C(C)(=O)OCC>COc1ccc(OC)c(C(=S)N(C)N)c1
ord_dataset-c3a75813d0b24864aa4f7cd526efd6aa
ord-16183485148f4b48b77ba0ac5d33f916
NN>>c1ccnnc1
NN.N[C@@H](CCC(N)=O)C(=O)O>>N1=NC=CC=C1.N[C@@H](CCC(N)=O)C(=O)O
[NH2:14][NH2:15]>>[cH:11]1[cH:12][cH:13][n:14][n:15][cH:16]1
NN
c1ccnnc1
null
null
null
Aromatic Heterocycle Formation
OtherReaction
3cc0159d461fee0fd6cc80b5d78917c7ffe2a593cffe4d961936985f7fad1d5f
ee3fba3c00b79a80c27ae38af6a02a8b0939483a226bcd6fe6c12c9f7aba8e28
c1ccnnc1
[NH2;D1;+0:1]-[NH2;D1;+0:2]>>[c:3]1:[c:4]:[c:5]:[n;H0;D2;+0:1]:[n;H0;D2;+0:2]:[c:6]:1
5
[{"value": 5.0, "product": "N1=NC=CC=C1", "details": "PERCENTYIELD", "is_desired": false}]
null
null
null
null
FIG. 2 depicts a schematic diagram 200 depicting the treatment of hydrazine waste to glutamine or a derivative thereof, in accordance with a preferred embodiment of the present invention. The hydrogenization of pyridazine using 5% Pd/C can provide glutamine in a 45% yield. Although this pyridazine is not easily biodegr...
10.6084/m9.figshare.5104873.v1
null
Hydrazine
null
null
c1ccnnc1
c1ccnnc1
Other
null
null
null
NN>>c1ccnnc1
ord_dataset-c3a75813d0b24864aa4f7cd526efd6aa
ord-74e87f9a12ac48378338e6e65b39ebfc
CCC(C)=O.CCCC=O.CCCCC(C=O)CC>>CCCC(=O)CCC.CCCC=CC(C)=O.CCCCCC(=O)CC.CCCCCC(C)=O
C(C)C(C=O)CCCC.C(CCC)=O.C(C)C(=O)C>>C(CCCC)C(=O)C.C(CCC)=CC(C)=O.C(CC)C(=O)CCC.CCC(CCCCC)=O
[CH3:21][C:22](=[O:23])[CH2:24][CH3:25].[CH3:9][CH2:10][CH2:11][CH:12]=[O:16].[CH:1]([CH:4]([CH2:6][CH3:7])[CH2:30][CH2:29][CH2:28][CH3:17])=[O:5]>>[CH3:1][CH2:2][CH2:3][C:4](=[O:5])[CH2:6][CH2:7][CH3:8].[CH3:9][CH2:10][CH2:11][CH:12]=[CH:13][C:14]([CH3:15])=[O:16].[CH3:17][CH2:18][CH2:19][CH2:20][CH2:21][C:22](=[O:23]...
CCC(C)=O.CCCC=O.CCCCC(C=O)CC
CCCC(=O)CCC.CCCC=CC(C)=O.CCCCCC(=O)CC.CCCCCC(C)=O
null
null
C(C(C)C)C(=O)C
C-C Coupling
OtherReaction
c863ff4502a4872a6e4a37d5c6a5043afe51243a70baf7fc6f67034ac154a1ef
ae04af4f751dea9f079b0e8a3c2680e7045a9ae69ebb7a0d2e3b92543677c2db
null
[CH3;D1;+0:1]-[CH2;D2;+0:2]-[C:3]-[CH2;D2;+0:4]-[CH;D3;+0:5](-[C:6]-[CH3;D1;+0:7])-[CH;D2;+0:8]=[O;H0;D1;+0:9].[C:10]-[C:11](-[CH3;D1;+0:12])=[O;D1;H0:13].[C:14]-[C:15]-[CH;D2;+0:16]=[O;H0;D1;+0:17]>>[C;D1;H3:18]-[CH2;D2;+0:7]-[C:6]-[C;H0;D3;+0:5](=[O;H0;D1;+0:9])-[C:19]-[C:20]-[CH3;D1;+0:8].[C;D1;H3:21]-[C:22]-[CH2;D2...
null
[]
null
null
null
null
U.S. Pat. No. 2,088,018 describes the preparation of secondary alcohols by simple aldol condensation of aldehydes, namely 2-ethylhexaldehyde and butyraldehyde, onto ketones, namely methyl ethyl ketone, methyl amyl ketone, methyl isobutyl ketone, butylideneacetone, dipropyl ketone and methylheptanone, and the subsequent...
10.6084/m9.figshare.5104873.v1
null
Aldehyde.Aldehyde.Ketone
Ketone.Ketone.Ketone.Ketone
null
null
null
Other
C(C(C)C)C(=O)C
null
null
CCC(C)=O.CCCC=O.CCCCC(C=O)CC>C(C(C)C)C(=O)C>CCCC(=O)CCC.CCCC=CC(C)=O.CCCCCC(=O)CC.CCCCCC(C)=O
ord_dataset-c3a75813d0b24864aa4f7cd526efd6aa
ord-385a60180831478591c2e7f190c4b233
C=COCCCCCCOC=C.OCCCCCCO>>C=COCCCCCCO
C([O-])([O-])=O.[Na+].[Na+].C(CCCCCO)O.C(C)(=O)OC=C.C(=C)OCCCCCCOC=C>>C(=C)OCCCCCCO
C=COCCCCCCO[CH:2]=[CH2:1].[OH:3][CH2:4][CH2:5][CH2:6][CH2:7][CH2:8][CH2:9][OH:10]>>[CH2:1]=[CH:2][O:3][CH2:4][CH2:5][CH2:6][CH2:7][CH2:8][CH2:9][OH:10]
C=COCCCCCCOC=C.OCCCCCCO
C=COCCCCCCO
null
null
C1(=CC=CC=C1)C
Acylation
OtherReaction
84ff68ba5901d637da9c9d96551f0a1d17ca7657a982fa1072af8fd2b0b32d3b
509a7a4b565cd49ff866c9f0586bc0ffa851a5f12533282130d9eeb123692a41
null
C=C-O-C-C-C-C-C-C-O-[CH;D2;+0:1]=[C;D1;H2:2].[C:3]-[C:4]-[OH;D1;+0:5]>>[C:3]-[C:4]-[O;H0;D2;+0:5]-[CH;D2;+0:1]=[C;D1;H2:2]
null
[]
100
CELSIUS
6
HOUR
To a mixture of di-μ-chlorobis(1,5-cyclooctadiene)diiridium(I) [Ir(cod)Cl]2 (6.7 mg, 0.01 mmol) and sodium carbonate (64 mg, 0.6 mmol) in toluene (1.0 ml), 1,6-hexanediol (118 mg, 1 mmol) and vinyl acetate (344 mg, 4 mmol) were added, followed by stirring at 100° C. in an atmosphere of argon gas for 6 hours. The reacti...
10.6084/m9.figshare.5104873.v1
null
Ether.Ether.Primary alcohol.Vinyl.Vinyl
Ether
null
null
null
HO-
C1(=CC=CC=C1)C
100
6
C=COCCCCCCOC=C.OCCCCCCO>C1(=CC=CC=C1)C>C=COCCCCCCO
ord_dataset-c3a75813d0b24864aa4f7cd526efd6aa
ord-c6dfb5bc8847406e9ee7580fa7097c57
C=COC12CC3CC(C1)CC(OC=C)(C3)C2.OC12CC3CC(C1)CC(O)(C3)C2>>C=COC12CC3CC(CC(O)(C3)C1)C2
C([O-])([O-])=O.[Na+].[Na+].C12(CC3(CC(CC(C1)C3)C2)O)O.C(C)(=O)OC=C.C(=C)OC12CC3(CC(CC(C1)C3)C2)OC=C>>C(=C)OC12CC3(CC(CC(C1)C3)C2)O
C=COC12CC3CC(C1)CC(O[CH:2]=[CH2:1])(C3)C2.[OH:3][C:4]12[CH2:5][CH:6]3[CH2:7][CH:8]([CH2:9][C:10]([OH:11])([CH2:12]3)[CH2:13]1)[CH2:14]2>>[CH2:1]=[CH:2][O:3][C:4]12[CH2:5][CH:6]3[CH2:7][CH:8]([CH2:9][C:10]([OH:11])([CH2:12]3)[CH2:13]1)[CH2:14]2
C=COC12CC3CC(C1)CC(OC=C)(C3)C2.OC12CC3CC(C1)CC(O)(C3)C2
C=COC12CC3CC(CC(O)(C3)C1)C2
null
null
C1(=CC=CC=C1)C
Acylation
OtherReaction
5411ddf257e28c4fcac9f3bbf029b667684799b45386358bb0a46d43aed6f2f0
3d4b98bfc4b1b8d1e4c33891a182aafedfecac35089df3e0715a245c9efed478
C1C2CC3CC1CC(C2)C3
C=C-O-C12-C-C3-C-C(-C-1)-C-C(-O-[CH;D2;+0:1]=[C;D1;H2:2])(-C-3)-C-2.[C:3]-[C:4](-[OH;D1;+0:5])(-[C:6])-[C:7]>>[C:3]-[C:4](-[O;H0;D2;+0:5]-[CH;D2;+0:1]=[C;D1;H2:2])(-[C:6])-[C:7]
null
[]
100
CELSIUS
5
HOUR
To a mixture of di-μ-chlorobis(1,5-cyclooctadiene)diiridium(I) [Ir(cod)Cl]2 (6.7 mg, 0.01 mmol) and sodium carbonate (64 mg, 0.6 mmol) in toluene (1.0 ml), 1,3-adamantanediol (1 mmol) and vinyl acetate (6 mmol) were added, followed by stirring at 100° C. in an atmosphere of argon gas for 5 hours. The reaction mixture w...
10.6084/m9.figshare.5104873.v1
null
Ether.Ether.Tertiary alcohol.Vinyl.Vinyl
Ether
C1C2CC3CC1CC(C2)C3
null
C1C2CC3CC1CC(C2)C3
HO-
C1(=CC=CC=C1)C
100
5
C=COC12CC3CC(C1)CC(OC=C)(C3)C2.OC12CC3CC(C1)CC(O)(C3)C2>C1(=CC=CC=C1)C>C=COC12CC3CC(CC(O)(C3)C1)C2
ord_dataset-c3a75813d0b24864aa4f7cd526efd6aa
ord-504342d31d0a441d9ce7df3f5695b57d
C=COC12CC3CC(O)(C1)CC(OC=C)(C3)C2.OC12CC3CC(O)(C1)CC(O)(C3)C2>>C=COC12CC3CC(O)(CC(O)(C3)C1)C2
C([O-])([O-])=O.[Na+].[Na+].C12(CC3(CC(CC(C1)C3)(C2)O)O)O.C(C)(=O)OC=C.C(=C)OC12CC3(CC(CC(C1)(C3)OC=C)C2)O.C(=C)OC12CC3(CC(CC(C1)C3)(C2)OC=C)OC=C>>C(=C)OC12CC3(CC(CC(C1)C3)(C2)O)O
C=COC12CC3CC(O)(C1)CC(O[CH:2]=[CH2:1])(C3)C2.[OH:3][C:4]12[CH2:5][CH:6]3[CH2:7][C:8]([OH:9])([CH2:10][C:11]([OH:12])([CH2:13]3)[CH2:14]1)[CH2:15]2>>[CH2:1]=[CH:2][O:3][C:4]12[CH2:5][CH:6]3[CH2:7][C:8]([OH:9])([CH2:10][C:11]([OH:12])([CH2:13]3)[CH2:14]1)[CH2:15]2
C=COC12CC3CC(O)(C1)CC(OC=C)(C3)C2.OC12CC3CC(O)(C1)CC(O)(C3)C2
C=COC12CC3CC(O)(CC(O)(C3)C1)C2
null
null
C1(=CC=CC=C1)C
Acylation
OtherReaction
5e2557d8390ce5e5031ff4061978a5df7a5894ecb5b1c87aa0ac5f6af1da458c
a7f89e1882cdb2909dd701fc44e8118d7023049a5b1500a5a5aabb84f2aa72bc
C1C2CC3CC1CC(C2)C3
C=C-O-C12-C-C3-C-C(-O)(-C-1)-C-C(-O-[CH;D2;+0:1]=[C;D1;H2:2])(-C-3)-C-2.[C:3]-[C:4](-[OH;D1;+0:5])(-[C:6])-[C:7]>>[C:3]-[C:4](-[O;H0;D2;+0:5]-[CH;D2;+0:1]=[C;D1;H2:2])(-[C:6])-[C:7]
null
[]
100
CELSIUS
5
HOUR
To a mixture of di-μ-chlorobis(1,5-cyclooctadiene)diiridium(I) [Ir(cod)Cl]2 (6.7 mg, 0.01 mmol) and sodium carbonate (64 mg, 0.6 mmol) in toluene (1.0 ml), 1,3,5-adamantanetriol (1 mmol) and vinyl acetate (9 mmol) were added, followed by stirring at 100° C. in an atmosphere of argon gas for 5 hours. The reaction mixtur...
10.6084/m9.figshare.5104873.v1
null
Ether.Ether.Tertiary alcohol.Tertiary alcohol.Vinyl.Vinyl
Ether
C1C2CC3CC1CC(C2)C3
null
C1C2CC3CC1CC(C2)C3
HO-
C1(=CC=CC=C1)C
100
5
C=COC12CC3CC(O)(C1)CC(OC=C)(C3)C2.OC12CC3CC(O)(C1)CC(O)(C3)C2>C1(=CC=CC=C1)C>C=COC12CC3CC(O)(CC(O)(C3)C1)C2
ord_dataset-c3a75813d0b24864aa4f7cd526efd6aa
ord-b42039f3bdaf413c95f8ecda28d765ed
C=C(C)OCCCCCCCC.CCCCCCCCO>>CCCCCCCCOC(C)=O
C([O-])([O-])=O.[Na+].[Na+].C(CCCCCCC)O.C(C)(=O)OC(=C)C.C(CCCCCCC)OC(C)(C)OCCCCCCCC.C(=C)(C)OCCCCCCCC>>C(C)(=O)OCCCCCCCC
CCCCCCCC[O:12][C:10](C)=[CH2:11].[CH3:1][CH2:2][CH2:3][CH2:4][CH2:5][CH2:6][CH2:7][CH2:8][OH:9]>>[CH3:1][CH2:2][CH2:3][CH2:4][CH2:5][CH2:6][CH2:7][CH2:8][O:9][C:10]([CH3:11])=[O:12]
C=C(C)OCCCCCCCC.CCCCCCCCO
CCCCCCCCOC(C)=O
null
null
C1(=CC=CC=C1)C
Acylation
OtherReaction
12ba798a7bffce408863524d31eb3a42a39322f073effb080907c6d58029487b
6e85e98260bc6172724d060165d0fcfc69391dedb179e5c21597d647017827cb
null
C-C-C-C-C-C-C-C-[O;H0;D2;+0:1]-[C;H0;D3;+0:2](-C)=[CH2;D1;+0:3].[C:4]-[C:5]-[OH;D1;+0:6]>>[C:4]-[C:5]-[O;H0;D2;+0:6]-[C;H0;D3;+0:2](-[CH3;D1;+0:3])=[O;H0;D1;+0:1]
null
[]
100
CELSIUS
15
HOUR
To a mixture of di-μ-chlorobis(1,5-cyclooctadiene)diiridium(I) [Ir(cod)Cl]2 (0.01 mmol) and sodium carbonate (0.03 mmol) in toluene (1.0 ml), 1-octanol (130 mg, 1 mmol) and isopropenyl acetate (5 mmol) were added, followed by stirring at 100° C. in an atmosphere of argon gas for 15 hours. The reaction mixture was analy...
10.6084/m9.figshare.5104873.v1
null
Ether.Primary alcohol.Vinyl
Ester
null
null
null
Other
C1(=CC=CC=C1)C
100
15
C=C(C)OCCCCCCCC.CCCCCCCCO>C1(=CC=CC=C1)C>CCCCCCCCOC(C)=O
ord_dataset-c3a75813d0b24864aa4f7cd526efd6aa
ord-bb0ae9e5c0614e48b91c03afdb979d47
C=C(C)OCCCCCCCC.CCCCCCCCO>>CCCCCCCCOC(C)=O
C(=C)(C)OCCCCCCCC.C(CCCCCCC)OC(C)(C)OCCCCCCCC.F[B-](F)(F)F.C([O-])([O-])=O.[Na+].[Na+].C(CCCCCCC)O.C(C)(=O)OC(=C)C>>C(C)(=O)OCCCCCCCC
CCCCCCCC[O:12][C:10](C)=[CH2:11].[CH3:1][CH2:2][CH2:3][CH2:4][CH2:5][CH2:6][CH2:7][CH2:8][OH:9]>>[CH3:1][CH2:2][CH2:3][CH2:4][CH2:5][CH2:6][CH2:7][CH2:8][O:9][C:10]([CH3:11])=[O:12]
C=C(C)OCCCCCCCC.CCCCCCCCO
CCCCCCCCOC(C)=O
null
null
C1(=CC=CC=C1)C
Acylation
OtherReaction
12ba798a7bffce408863524d31eb3a42a39322f073effb080907c6d58029487b
6e85e98260bc6172724d060165d0fcfc69391dedb179e5c21597d647017827cb
null
C-C-C-C-C-C-C-C-[O;H0;D2;+0:1]-[C;H0;D3;+0:2](-C)=[CH2;D1;+0:3].[C:4]-[C:5]-[OH;D1;+0:6]>>[C:4]-[C:5]-[O;H0;D2;+0:6]-[C;H0;D3;+0:2](-[CH3;D1;+0:3])=[O;H0;D1;+0:1]
null
[]
100
CELSIUS
15
HOUR
To a mixture of bis(1,5-cyclooctadiene)iridium tetrafluoroborate [Ir(cod)2]+BF4− (0.01 mmol) and sodium carbonate (0.03 mmol) in toluene (1.0 ml), 1-octanol (130 mg, 1 mmol) and isopropenyl acetate (5 mmol) were added, followed by stirring at 100° C. in an atmosphere of argon gas for 15 hours. The reaction mixture was ...
10.6084/m9.figshare.5104873.v1
null
Ether.Primary alcohol.Vinyl
Ester
null
null
null
Other
C1(=CC=CC=C1)C
100
15
C=C(C)OCCCCCCCC.CCCCCCCCO>C1(=CC=CC=C1)C>CCCCCCCCOC(C)=O
ord_dataset-c3a75813d0b24864aa4f7cd526efd6aa
ord-ac5dce3512a44a70a5b765db9973a4c7
CCCCCCCCO.CCCCCCCCOC(C)=O>>CCCCCCCCOC(C)OC(C)=O
C([O-])([O-])=O.[Na+].[Na+].C(CCCCCCC)O.C(C)(=O)OC=C.C(C)(=O)OCCCCCCCC.C(=C)OCCCCCCCC>>C(C)(=O)OC(C)OCCCCCCCC
[CH3:1][CH2:2][CH2:3][CH2:4][CH2:5][CH2:6][CH2:7][CH2:8][OH:9].CCCCCC[CH2:11][CH2:10][O:12][C:13]([CH3:14])=[O:15]>>[CH3:1][CH2:2][CH2:3][CH2:4][CH2:5][CH2:6][CH2:7][CH2:8][O:9][CH:10]([CH3:11])[O:12][C:13]([CH3:14])=[O:15]
CCCCCCCCO.CCCCCCCCOC(C)=O
CCCCCCCCOC(C)OC(C)=O
null
null
C1(=CC=CC=C1)C
Heteroatom Alkylation and Arylation
OtherReaction
979b8325f6c86bd7f54883d4339d8941e9012bd27a51cce50286476d3a7986f1
9dc366785c78d3f697d5ebd42f23b786ef7a373defee7e9fd1a94b3dd2d792cb
null
C-C-C-C-C-C-[CH2;D2;+0:1]-[CH2;D2;+0:2]-[#8:3]-[C:4](-[C;D1;H3:5])=[O;D1;H0:6].[C:7]-[C:8]-[OH;D1;+0:9]>>[C:7]-[C:8]-[O;H0;D2;+0:9]-[CH;D3;+0:2](-[CH3;D1;+0:1])-[#8:3]-[C:4](-[C;D1;H3:5])=[O;D1;H0:6]
null
[]
100
CELSIUS
2
HOUR
To a mixture of di-μ-chlorobis(1,5-cyclooctadiene)diiridium(I) [Ir(cod)Cl]2 (0.01 mmol) and sodium carbonate (0.1 mmol) in toluene (1.0 ml), 1-octanol (130 mg, 1 mmol) and vinyl acetate (5 mmol) were added, followed by stirring at 100° C. in an atmosphere of argon gas for 2 hours. The reaction mixture was analyzed by g...
10.6084/m9.figshare.5104873.v1
null
Ester.Primary alcohol
Ester.Ether
null
null
null
Other
C1(=CC=CC=C1)C
100
2
CCCCCCCCO.CCCCCCCCOC(C)=O>C1(=CC=CC=C1)C>CCCCCCCCOC(C)OC(C)=O
ord_dataset-c3a75813d0b24864aa4f7cd526efd6aa
ord-780852031da347f0a2c25019e1f5cc01
C=COC(C)=O.CCCCCCCCO>>CCCCCCCCOC(C)=O
C(O)([O-])=O.[Na+].C(CCCCCCC)O.C(C)(=O)OC=C.C(=C)OCCCCCCCC>>C(C)(=O)OCCCCCCCC
C=C[O:9][C:10]([CH3:11])=[O:12].O[CH2:8][CH2:7][CH2:6][CH2:5][CH2:4][CH2:3][CH2:2][CH3:1]>>[CH3:1][CH2:2][CH2:3][CH2:4][CH2:5][CH2:6][CH2:7][CH2:8][O:9][C:10]([CH3:11])=[O:12]
C=COC(C)=O.CCCCCCCCO
CCCCCCCCOC(C)=O
null
null
C1(=CC=CC=C1)C
Heteroatom Alkylation and Arylation
Transesterification
1f62a48d697c8d05270b2586da78dd3983b9960afc30c6a9d1ec3949e81d4234
89037c7729098ddd0eec149343f13d88dc823f0d1194aa0a012d1107ef8d2f4e
null
C=C-[O;H0;D2;+0:1]-[C:2](-[C;D1;H3:3])=[O;D1;H0:4].O-[CH2;D2;+0:5]-[C:6]-[C:7]>>[C:7]-[C:6]-[CH2;D2;+0:5]-[O;H0;D2;+0:1]-[C:2](-[C;D1;H3:3])=[O;D1;H0:4]
null
[]
100
CELSIUS
2
HOUR
To a mixture of di-μ-chlorobis(1,5-cyclooctadiene)diiridium(I) [Ir(cod)Cl]2 (0.01 mmol) and sodium hydrogencarbonate (1.2 mmol) in toluene (1.0 ml), 1-octanol (130 mg, 1 mmol) and vinyl acetate (2 mmol) were added, followed by stirring at 100° C. in an atmosphere of argon gas for 2 hours. The reaction mixture was analy...
10.6084/m9.figshare.5104873.v1
null
Ester.Primary alcohol.Vinyl
Ester
null
null
null
HO-
C1(=CC=CC=C1)C
100
2
C=COC(C)=O.CCCCCCCCO>C1(=CC=CC=C1)C>CCCCCCCCOC(C)=O
ord_dataset-c3a75813d0b24864aa4f7cd526efd6aa
ord-13e0412b39c54058b57aa132f24b8794
C=COC(C)=O.CCCCCCCCO>>CCCCCCCCOC(C)=O
C(=C)OCCCCCCCC.F[B-](F)(F)F.C([O-])([O-])=O.[Na+].[Na+].C(CCCCCCC)O.C(C)(=O)OC=C>>C(C)(=O)OCCCCCCCC
C=C[O:9][C:10]([CH3:11])=[O:12].O[CH2:8][CH2:7][CH2:6][CH2:5][CH2:4][CH2:3][CH2:2][CH3:1]>>[CH3:1][CH2:2][CH2:3][CH2:4][CH2:5][CH2:6][CH2:7][CH2:8][O:9][C:10]([CH3:11])=[O:12]
C=COC(C)=O.CCCCCCCCO
CCCCCCCCOC(C)=O
null
null
C1(=CC=CC=C1)C
Heteroatom Alkylation and Arylation
Transesterification
1f62a48d697c8d05270b2586da78dd3983b9960afc30c6a9d1ec3949e81d4234
89037c7729098ddd0eec149343f13d88dc823f0d1194aa0a012d1107ef8d2f4e
null
C=C-[O;H0;D2;+0:1]-[C:2](-[C;D1;H3:3])=[O;D1;H0:4].O-[CH2;D2;+0:5]-[C:6]-[C:7]>>[C:7]-[C:6]-[CH2;D2;+0:5]-[O;H0;D2;+0:1]-[C:2](-[C;D1;H3:3])=[O;D1;H0:4]
null
[]
100
CELSIUS
2
HOUR
To a mixture of bis(1,5-cyclooctadiene)iridium tetrafluoroborate [Ir(cod)2]+BF4− (0.01 mmol) and sodium carbonate (0.6 mmol) in toluene (1.0 ml), 1-octanol (130 mg, 1 mmol) and vinyl acetate (2 mmol) were added, followed by stirring at 100° C. in an atmosphere of argon gas for 2 hours. The reaction mixture was analyzed...
10.6084/m9.figshare.5104873.v1
null
Ester.Primary alcohol.Vinyl
Ester
null
null
null
HO-
C1(=CC=CC=C1)C
100
2
C=COC(C)=O.CCCCCCCCO>C1(=CC=CC=C1)C>CCCCCCCCOC(C)=O
ord_dataset-c3a75813d0b24864aa4f7cd526efd6aa
ord-aa8ea40883fd4d5a90129da3c6e88bf3
C=COC(C)=O.CCCCCCCCO>>CCCCCCCCOC(C)=O
C(CCCCCCC)O.C(C)(=O)OC=C.C(=C)OCCCCCCCC>>C(C)(=O)OCCCCCCCC
C=C[O:9][C:10]([CH3:11])=[O:12].O[CH2:8][CH2:7][CH2:6][CH2:5][CH2:4][CH2:3][CH2:2][CH3:1]>>[CH3:1][CH2:2][CH2:3][CH2:4][CH2:5][CH2:6][CH2:7][CH2:8][O:9][C:10]([CH3:11])=[O:12]
C=COC(C)=O.CCCCCCCCO
CCCCCCCCOC(C)=O
null
null
C1(=CC=CC=C1)C
Heteroatom Alkylation and Arylation
Transesterification
1f62a48d697c8d05270b2586da78dd3983b9960afc30c6a9d1ec3949e81d4234
89037c7729098ddd0eec149343f13d88dc823f0d1194aa0a012d1107ef8d2f4e
null
C=C-[O;H0;D2;+0:1]-[C:2](-[C;D1;H3:3])=[O;D1;H0:4].O-[CH2;D2;+0:5]-[C:6]-[C:7]>>[C:7]-[C:6]-[CH2;D2;+0:5]-[O;H0;D2;+0:1]-[C:2](-[C;D1;H3:3])=[O;D1;H0:4]
null
[]
100
CELSIUS
2
HOUR
To a mixture of di-μ-chlorobis(1,5-cyclooctadiene)diiridium(I) [Ir(cod)Cl]2 (0.01 mmol) and 4MgCO3-Mg(OH)2-5H2O (0.6 mmol) in toluene (1.0 ml), 1-octanol (130 mg, 1 mmol) and vinyl acetate (2 mmol) were added, followed by stirring at 100° C. in an atmosphere of argon gas for 2 hours. The reaction mixture was analyzed b...
10.6084/m9.figshare.5104873.v1
null
Ester.Primary alcohol.Vinyl
Ester
null
null
null
HO-
C1(=CC=CC=C1)C
100
2
C=COC(C)=O.CCCCCCCCO>C1(=CC=CC=C1)C>CCCCCCCCOC(C)=O
ord_dataset-c3a75813d0b24864aa4f7cd526efd6aa
ord-a0d8f2c0bcb84cc8bc7bda50ca92ca8c
C=COC(C)=O.CCCCCCCCO>>CCCCCCCCOC(C)=O
C(C)N(CC)CC.C(CCCCCCC)O.C(C)(=O)OC=C.C(=C)OCCCCCCCC>>C(C)(=O)OCCCCCCCC
C=C[O:9][C:10]([CH3:11])=[O:12].O[CH2:8][CH2:7][CH2:6][CH2:5][CH2:4][CH2:3][CH2:2][CH3:1]>>[CH3:1][CH2:2][CH2:3][CH2:4][CH2:5][CH2:6][CH2:7][CH2:8][O:9][C:10]([CH3:11])=[O:12]
C=COC(C)=O.CCCCCCCCO
CCCCCCCCOC(C)=O
null
null
C1(=CC=CC=C1)C
Heteroatom Alkylation and Arylation
Transesterification
1f62a48d697c8d05270b2586da78dd3983b9960afc30c6a9d1ec3949e81d4234
89037c7729098ddd0eec149343f13d88dc823f0d1194aa0a012d1107ef8d2f4e
null
C=C-[O;H0;D2;+0:1]-[C:2](-[C;D1;H3:3])=[O;D1;H0:4].O-[CH2;D2;+0:5]-[C:6]-[C:7]>>[C:7]-[C:6]-[CH2;D2;+0:5]-[O;H0;D2;+0:1]-[C:2](-[C;D1;H3:3])=[O;D1;H0:4]
null
[]
100
CELSIUS
2
HOUR
To a mixture of di-μ-chlorobis(1,5-cyclooctadiene)diiridium(I) [Ir(cod)Cl]2 (0.01 mmol) and triethylamine (0.6 mmol) in toluene (1.0 ml), 1-octanol (130 mg, 1 mmol) and vinyl acetate (2 mmol) were added, followed by stirring at 100° C. in an atmosphere of argon gas for 2 hours. The reaction mixture was analyzed by gas ...
10.6084/m9.figshare.5104873.v1
null
Ester.Primary alcohol.Vinyl
Ester
null
null
null
HO-
C1(=CC=CC=C1)C
100
2
C=COC(C)=O.CCCCCCCCO>C1(=CC=CC=C1)C>CCCCCCCCOC(C)=O
ord_dataset-c3a75813d0b24864aa4f7cd526efd6aa
ord-9348e9232724437a8b3011be6c2796dc
C=COC(C)=O.CCCCCCCCO>>CCCCCCCCOC(C)=O
C(=C)OCCCCCCCC.F[B-](F)(F)F.C([O-])([O-])=O.[Na+].[Na+].C(CCCCCCC)O.C(C)(=O)OC=C>>C(C)(=O)OCCCCCCCC
C=C[O:9][C:10]([CH3:11])=[O:12].O[CH2:8][CH2:7][CH2:6][CH2:5][CH2:4][CH2:3][CH2:2][CH3:1]>>[CH3:1][CH2:2][CH2:3][CH2:4][CH2:5][CH2:6][CH2:7][CH2:8][O:9][C:10]([CH3:11])=[O:12]
C=COC(C)=O.CCCCCCCCO
CCCCCCCCOC(C)=O
null
null
C1(=CC=CC=C1)C
Heteroatom Alkylation and Arylation
Transesterification
1f62a48d697c8d05270b2586da78dd3983b9960afc30c6a9d1ec3949e81d4234
89037c7729098ddd0eec149343f13d88dc823f0d1194aa0a012d1107ef8d2f4e
null
C=C-[O;H0;D2;+0:1]-[C:2](-[C;D1;H3:3])=[O;D1;H0:4].O-[CH2;D2;+0:5]-[C:6]-[C:7]>>[C:7]-[C:6]-[CH2;D2;+0:5]-[O;H0;D2;+0:1]-[C:2](-[C;D1;H3:3])=[O;D1;H0:4]
null
[]
100
CELSIUS
2
HOUR
To a mixture of (1,5-cyclooctadiene)(acetonitrile)iridium tetrafluoroborate [Ir(cod) (CH3CN)]+BF4− (0.01 mmol) and sodium carbonate (0.6 mmol) in toluene (1.0 ml), 1-octanol (130 mg, 1 mmol) and vinyl acetate (2 mmol) were added, followed by stirring at 100° C. in an atmosphere of argon gas for 2 hours. The reaction mi...
10.6084/m9.figshare.5104873.v1
null
Ester.Primary alcohol.Vinyl
Ester
null
null
null
HO-
C1(=CC=CC=C1)C
100
2
C=COC(C)=O.CCCCCCCCO>C1(=CC=CC=C1)C>CCCCCCCCOC(C)=O
ord_dataset-c3a75813d0b24864aa4f7cd526efd6aa
ord-23d6d4ffa44348848a0b664c32a65c64
C=COC(C)=O.C=COCCOCCOCCOC=C>>C=COCCOCCOCCOC(C)=O
C(C)(=O)[O-].[Na+].C(COCCOCCO)O.C(C)(=O)OC=C.C(=C)OCCOCCOCCO.C(=C)OCCOCCOCCOC=C>>C(C)(=O)OCCOCCOCCOC=C
C=C[O:12][C:13]([CH3:14])=[O:15].C=CO[CH2:11][CH2:10][O:9][CH2:8][CH2:7][O:6][CH2:5][CH2:4][O:3][CH:2]=[CH2:1]>>[CH2:1]=[CH:2][O:3][CH2:4][CH2:5][O:6][CH2:7][CH2:8][O:9][CH2:10][CH2:11][O:12][C:13]([CH3:14])=[O:15]
C=COC(C)=O.C=COCCOCCOCCOC=C
C=COCCOCCOCCOC(C)=O
null
null
C1(=CC=CC=C1)C
Heteroatom Alkylation and Arylation
OtherReaction
702a5c0357c1cd0d935ea1bb3ff21417ad2b347673544c22573bc5f20dde36f1
76a119fe11a2760904d23496e6a03c8ef2943f7f0eca5c1e59b734558929b11b
null
C=C-O-[CH2;D2;+0:1]-[C:2]-[#8:3].C=C-[O;H0;D2;+0:4]-[C:5](-[C;D1;H3:6])=[O;D1;H0:7]>>[#8:3]-[C:2]-[CH2;D2;+0:1]-[O;H0;D2;+0:4]-[C:5](-[C;D1;H3:6])=[O;D1;H0:7]
null
[]
100
CELSIUS
6
HOUR
To a mixture of di-μ-chlorobis(1,5-cyclooctadiene)diiridium(I) [Ir(cod)Cl]2 (0.01 mmol) and sodium acetate (1.2 mmol) in toluene (2.0 ml),triethylene glycol (1 mmol) and vinyl acetate (4 mmol) were added, followed by stirring at 100° C. in an atmosphere of argon gas for 6 hours. The reaction mixture was analyzed by gas...
10.6084/m9.figshare.5104873.v1
null
Ester.Ether.Vinyl.Vinyl
Ester
null
null
null
HO-
C1(=CC=CC=C1)C
100
6
C=COC(C)=O.C=COCCOCCOCCOC=C>C1(=CC=CC=C1)C>C=COCCOCCOCCOC(C)=O
ord_dataset-c3a75813d0b24864aa4f7cd526efd6aa
ord-9fd399b1e47447c491fc9dd0e5816314
Brc1ccccn1.Cc1cc(C)c(CC#N)c(C)c1>>Cc1cc(C)c(C(C#N)c2ccccn2)c(C)c1
[NH4+].[Cl-].CC1=C(C(=CC(=C1)C)C)CC#N.BrC1=NC=CC=C1.CC(C)([O-])C.[K+]>>N1=C(C=CC=C1)C(C#N)C1=C(C=C(C=C1C)C)C
Br[c:10]1[cH:11][cH:12][cH:13][cH:14][n:15]1.[CH3:1][c:2]1[cH:3][c:4]([CH3:5])[c:6]([CH2:7][C:8]#[N:9])[c:16]([CH3:17])[cH:18]1>>[CH3:1][c:2]1[cH:3][c:4]([CH3:5])[c:6]([CH:7]([C:8]#[N:9])[c:10]2[cH:11][cH:12][cH:13][cH:14][n:15]2)[c:16]([CH3:17])[cH:18]1
Brc1ccccn1.Cc1cc(C)c(CC#N)c(C)c1
Cc1cc(C)c(C(C#N)c2ccccn2)c(C)c1
null
null
CS(=O)C
C-C Coupling
Hurtley reaction
8f95a6a4dbf65d683dbaed1144079febc7be23de24a7c40bb0b3588067e89135
48892094855745f5c51f8910c27ce7c101e08ad3f9da2a58d5512e3d9c1b432f
c1ccc(Cc2ccccn2)cc1
Br-[c;H0;D3;+0:1](:[#7;a:2]:[c:3]):[c:4]:[c:5].[N;D1;H0:6]#[C:7]-[CH2;D2;+0:8]-[c:9](:[c:10]):[c:11]>>[N;D1;H0:6]#[C:7]-[CH;D3;+0:8](-[c:9](:[c:10]):[c:11])-[c;H0;D3;+0:1](:[#7;a:2]:[c:3]):[c:4]:[c:5]
null
[]
null
null
4
HOUR
Add dropwise over a 1-hour period a mixed solution of 2-(2,4,6-trimethylphenyl)ethanenitrile (20 g; 0.126 mol) and 2-bromopyridine (35 g; 0.22 mol) in DMSO (25 mL) to a solution of potassium t-butoxide (35 g; 0.31 mol) dissolved in DMSO (125 mL). After the addition, stir the mixture for 4 h at ambient temperature and s...
10.6084/m9.figshare.5104873.v1
null
Aromatic halide
null
c1ccncc1
c1ccncc1
c1ccccc1.c1ccncc1
HBr
CS(=O)C
null
4
Brc1ccccn1.Cc1cc(C)c(CC#N)c(C)c1>CS(=O)C>Cc1cc(C)c(C(C#N)c2ccccn2)c(C)c1
ord_dataset-c3a75813d0b24864aa4f7cd526efd6aa
ord-950f94b2156b4e3ba6cbaf232186d86d
CCOC(=O)CBr.Cc1cc(C)c(C(C#N)c2ccccn2)c(C)c1>>CCOC(=O)c1c(N)c(-c2c(C)cc(C)cc2C)c2ccccn12
CC(C)([O-])C.[K+].BrCC(=O)OCC.N1=C(C=CC=C1)C(C#N)C1=C(C=C(C=C1C)C)C.C([O-])([O-])=O.[K+].[K+]>>NC=1C(=C2C=CC=CN2C1C(=O)OCC)C1=C(C=C(C=C1C)C)C
Br[CH2:6][C:4]([O:3][CH2:2][CH3:1])=[O:5].[C:7](#[N:8])[CH:9]([c:10]1[c:11]([CH3:12])[cH:13][c:14]([CH3:15])[cH:16][c:17]1[CH3:18])[c:19]1[cH:20][cH:21][cH:22][cH:23][n:24]1>>[CH3:1][CH2:2][O:3][C:4](=[O:5])[c:6]1[c:7]([NH2:8])[c:9](-[c:10]2[c:11]([CH3:12])[cH:13][c:14]([CH3:15])[cH:16][c:17]2[CH3:18])[c:19]2[cH:20][cH...
CCOC(=O)CBr.Cc1cc(C)c(C(C#N)c2ccccn2)c(C)c1
CCOC(=O)c1c(N)c(-c2c(C)cc(C)cc2C)c2ccccn12
null
null
CS(=O)C.[NH4+].[Cl-]
Aromatic Heterocycle Formation
OtherReaction
02387becbb0a0174e67eb86acd80dfe071e3507fb464bb83cb9adde301540e54
dbe50c1f4efdf7f701346d96862c76be1bb037ffd95658422881cd1a6cf8422f
c1ccc(-c2ccn3ccccc23)cc1
Br-[CH2;D2;+0:1]-[C:2](=[O;D1;H0:3])-[#8:4]-[C:5].[C;D1;H3:6]-[c:7](:[c:8]):[c;H0;D3;+0:9](-[CH;D3;+0:10](-[C;H0;D2;+0:11]#[N;H0;D1;+0:12])-[c:13](:[c:14]):[n;H0;D2;+0:15]:[c:16]:[c:17]):[c:18](-[C;D1;H3:19]):[c:20]>>[C:5]-[#8:4]-[C:2](=[O;D1;H0:3])-[c;H0;D3;+0:1]1:[c;H0;D3;+0:11](-[NH2;D1;+0:12]):[c;H0;D3;+0:10](-[c;H...
null
[]
0
CELSIUS
1
DAY
Slowly add dropwise ethyl bromoacetate (23 mL; 0.21 mol) over a 3-hour period to a mixture of 2-(2-pyridinyl)-2-(2,4,6-trimethylphenyl)-ethanenitrile (22.3 g; 0.094 mol) and potassium carbonate (78 g; 0.57 mol) suspended in DMSO (100 mL). Stir the mixture for 1 day, pour into an aqueous NH4Cl solution (ca. 1 L), and ex...
10.6084/m9.figshare.5104873.v1
null
Primary halide.Ester.Nitrile
Ester.Primary amine
c1ccncc1
c1ccn2cccc2c1
c1ccccc1.c1ccn2cccc2c1
HBr
CS(=O)C.[NH4+].[Cl-]
0
24
CCOC(=O)CBr.Cc1cc(C)c(C(C#N)c2ccccn2)c(C)c1>CS(=O)C.[NH4+].[Cl-]>CCOC(=O)c1c(N)c(-c2c(C)cc(C)cc2C)c2ccccn12
ord_dataset-c3a75813d0b24864aa4f7cd526efd6aa
ord-44429aaa5f9c4912afa90daad3429515
CC1(C)C2CCC1(CS(=O)(=O)O)C(=O)C2.CCOC(=O)c1c(N)c(-c2c(C)cc(C)cc2C)c2ccccn12>>Cc1cc(C)c(-c2cccn3c2cc2nc(C)cc(O)c23)c(C)c1
NC=1C(=C2C=CC=CN2C1C(=O)OCC)C1=C(C=C(C=C1C)C)C.CC1(C2CCC1(C(=O)C2)CS(=O)(=O)O)C.COC(C)(C)OC.C[Si](C)(C)[N-][Si](C)(C)C.[K+].C1(=CC=CC=C1)C>>CC=1C=C(C2=C(C=C3C(=CC=CN23)C2=C(C=C(C=C2C)C)C)N1)O
CC1([CH3:17])C2CC(=O)C1(CS(=O)(=O)O)[CH2:12][CH2:13]2.CCO[C:19]([c:18]1[n:11]2[cH:10][cH:9][cH:8][cH:14][c:21]2[c:7](-[c:6]2[c:4]([CH3:5])[cH:3][c:2]([CH3:1])[cH:24][c:22]2[CH3:23])[c:16]1[NH2:15])=[O:20]>>[CH3:1][c:2]1[cH:3][c:4]([CH3:5])[c:6](-[c:7]2[cH:8][cH:9][cH:10][n:11]3[c:12]2[cH:13][c:14]2[n:15][c:16]([CH3:17]...
CC1(C)C2CCC1(CS(=O)(=O)O)C(=O)C2.CCOC(=O)c1c(N)c(-c2c(C)cc(C)cc2C)c2ccccn12
Cc1cc(C)c(-c2cccn3c2cc2nc(C)cc(O)c23)c(C)c1
null
null
null
C-C Coupling
OtherReaction
adee181db23e8f608a48d2c5ef58b9961d9c9d17bb6a2928e4d7bedb66dd5be0
5d1c49fd3b82c2013b6db54c337ac490521c2e95f871f3869fc30e0aec8dd54e
c1ccc(-c2cccn3c2cc2ncccc23)cc1
C-C-O-[C;H0;D3;+0:1](=[O;H0;D1;+0:2])-[c;H0;D3;+0:3]1:[c;H0;D3;+0:4](-[NH2;D1;+0:5]):[c;H0;D3;+0:6](-[c:7](:[c:8]):[c:9]):[c;H0;D3;+0:10]2:[cH;D2;+0:11]:[cH;D2;+0:12]:[c:13]:[c:14]:[n;H0;D3;+0:15]:1:2.C-C1(-[CH3;D1;+0:16])-C2-C-C(=O)-C-1(-C-S(-O)(=O)=O)-[CH2;D2;+0:17]-[CH2;D2;+0:18]-2>>[CH3;D1;+0:16]-[c;H0;D3;+0:4]1:[c...
null
[]
null
null
null
null
To a solution of 2-ethyl 2-amino-1-(2,4,6-trimethylphenyl)indolizine-3-carboxylate (19.2 g; 59.6 mmol) in 2,2-dimethoxypropane (100 mL), add dl-camphorsulfonic acid (0.2 g). Stir the mixture at reflux for 30 min and then distill slowly to remove ca. 60 mL of volatiles over a 30-minute period. Cool the solution to ambie...
10.6084/m9.figshare.5104873.v1
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Ketone.Ester.Primary amine.Sulfonic acid
Aromatic alcohol
C1CC2CCC1C2.c1ccn2cccc2c1
c1ccn2c(c1)cc1ncccc12
c1ccccc1.c1ccn2c(c1)cc1ncccc12
HO-
null
null
null
CC1(C)C2CCC1(CS(=O)(=O)O)C(=O)C2.CCOC(=O)c1c(N)c(-c2c(C)cc(C)cc2C)c2ccccn12>>Cc1cc(C)c(-c2cccn3c2cc2nc(C)cc(O)c23)c(C)c1
ord_dataset-c3a75813d0b24864aa4f7cd526efd6aa
ord-448b30c85c3f44b9b5daf07c67a8ae6c
Cc1cc(C)c(-c2cccn3c2cc2nc(C)cc(O)c23)c(C)c1.O=P(Cl)(Cl)Cl>>Cc1cc(C)c(-c2cccn3c2cc2nc(C)cc(Cl)c23)c(C)c1
CC=1C=C(C2=C(C=C3C(=CC=CN23)C2=C(C=C(C=C2C)C)C)N1)O.OC1=CC(=NC=2C(=C3C=CC=CN3C21)C2=C(C=C(C=C2C)C)C)C.P(=O)(Cl)(Cl)Cl>>ClC1=CC(=NC=2C=C3C(=CC=CN3C21)C2=C(C=C(C=C2C)C)C)C
O[c:19]1[cH:18][c:16]([CH3:17])[n:15][c:14]2[cH:13][c:12]3[c:7](-[c:6]4[c:4]([CH3:5])[cH:3][c:2]([CH3:1])[cH:24][c:22]4[CH3:23])[cH:8][cH:9][cH:10][n:11]3[c:21]21.O=P(Cl)(Cl)[Cl:20]>>[CH3:1][c:2]1[cH:3][c:4]([CH3:5])[c:6](-[c:7]2[cH:8][cH:9][cH:10][n:11]3[c:12]2[cH:13][c:14]2[n:15][c:16]([CH3:17])[cH:18][c:19]([Cl:20])...
Cc1cc(C)c(-c2cccn3c2cc2nc(C)cc(O)c23)c(C)c1.O=P(Cl)(Cl)Cl
Cc1cc(C)c(-c2cccn3c2cc2nc(C)cc(Cl)c23)c(C)c1
null
null
null
Functional Group Interconversion
Alcohol to chloride_POCl3_para
11a2af47b57335970e56251de17e6ee61937240e53ea068e5b5ae61ecd817d06
e71580a8ffadb7b2717ecd7d68c1d3c0ca161ba5e6a787a49dad5a1359adc993
c1ccc(-c2cccn3c2cc2ncccc23)cc1
Cl-P(-Cl)(=O)-[Cl;H0;D1;+0:1].O-[c;H0;D3;+0:2]1:[c:3]:[c:4](-[C;D1;H3:5]):[#7;a:6]:[c:7]2:[c:8]:[c:9]:[#7;a:10](:[c:11]):[c:12]:2:1>>[C;D1;H3:5]-[c:4]1:[#7;a:6]:[c:7]2:[c:8]:[c:9]:[#7;a:10](:[c:11]):[c:12]:2:[c;H0;D3;+0:2](-[Cl;H0;D1;+0:1]):[c:3]:1
null
[]
null
null
null
null
Heat at 100° C. for 1 h a solution of 4-hydroxy-2-methyl-10-(2,4,6-trimethylphenyl)pyridino-[2,3-b]indolizine 2-methyl-9-(2,4,6-trimethylphenyl)pyrido[2,3-b]-indolizin-4-ol (10.1 g; 32 mmol) in phosphorus oxychloride (60 mL), cool to ambient temperature, and concentrate in vacuo. Partition the residue into ice water an...
10.6084/m9.figshare.5104873.v1
null
Aromatic alcohol
Aromatic halide
c1ccn2c(c1)cc1ncccc12
c1ccn2c(c1)cc1ncccc12
c1ccccc1.c1ccn2c(c1)cc1ncccc12
HCl
null
null
null
Cc1cc(C)c(-c2cccn3c2cc2nc(C)cc(O)c23)c(C)c1.O=P(Cl)(Cl)Cl>>Cc1cc(C)c(-c2cccn3c2cc2nc(C)cc(Cl)c23)c(C)c1
ord_dataset-c3a75813d0b24864aa4f7cd526efd6aa
ord-2b444a23c00341c5a009ee678e673ced
Cc1cc(C)c(-c2cccn3c2cc2nc(C)cc(Cl)c23)c(C)c1.NCCN>>Cc1cc(C)c(-c2cccn3c2cc2nc(C)cc(NCCN)c23)c(C)c1
ClC1=CC(=NC=2C=C3C(=CC=CN3C21)C2=C(C=C(C=C2C)C)C)C.C(CN)N>>NCCNC1=CC(=NC=2C=C3C(=CC=CN3C21)C2=C(C=C(C=C2C)C)C)C
Cl[c:19]1[cH:18][c:16]([CH3:17])[n:15][c:14]2[cH:13][c:12]3[c:7](-[c:6]4[c:4]([CH3:5])[cH:3][c:2]([CH3:1])[cH:27][c:25]4[CH3:26])[cH:8][cH:9][cH:10][n:11]3[c:24]21.[NH2:20][CH2:21][CH2:22][NH2:23]>>[CH3:1][c:2]1[cH:3][c:4]([CH3:5])[c:6](-[c:7]2[cH:8][cH:9][cH:10][n:11]3[c:12]2[cH:13][c:14]2[n:15][c:16]([CH3:17])[cH:18]...
Cc1cc(C)c(-c2cccn3c2cc2nc(C)cc(Cl)c23)c(C)c1.NCCN
Cc1cc(C)c(-c2cccn3c2cc2nc(C)cc(NCCN)c23)c(C)c1
null
null
CN1CCCC1=O
Heteroatom Alkylation and Arylation
N-arylation (Buchwald-Hartwig/Ullmann-Goldberg)
f25174d3f1cf7e2df5fcfaa6b1cf490b9776a217f28eb2d399728d8149e2491f
71a04ae650defc5edd86a92f43c304e981a05f07ff76248da8d4155f3905a29d
c1ccc(-c2cccn3c2cc2ncccc23)cc1
Cl-[c;H0;D3;+0:1]1:[c:2]:[c:3](-[C;D1;H3:4]):[#7;a:5]:[c:6]2:[c:7]:[c:8]:[#7;a:9](:[c:10]):[c:11]:2:1.[C:12]-[C:13]-[NH2;D1;+0:14]>>[C:12]-[C:13]-[NH;D2;+0:14]-[c;H0;D3;+0:1]1:[c:2]:[c:3](-[C;D1;H3:4]):[#7;a:5]:[c:6]2:[c:7]:[c:8]:[#7;a:9](:[c:10]):[c:11]:2:1
null
[]
null
null
null
null
Heat a solution of 4-chloro-2-methyl-9-(2,4,6-trimethylphenyl)pyridino[2,3-b]-indolizine (0.35 g, 1.04 mmol), and ethylene diamine (0.32 g, 1.04 mmol) in dry NMP (3 mL) at 100° C. for 5 h. Pour the cooled mixture onto water (30 mL) and extract twice with EtOAc (30 mL). Wash the combined extract with brine (30 mL), dry,...
10.6084/m9.figshare.5104873.v1
null
Aromatic halide.Primary amine
Secondary amine
c1ccn2c(c1)cc1ncccc12
c1ccn2c(c1)cc1ncccc12
c1ccccc1.c1ccn2c(c1)cc1ncccc12
HCl
CN1CCCC1=O
null
null
Cc1cc(C)c(-c2cccn3c2cc2nc(C)cc(Cl)c23)c(C)c1.NCCN>CN1CCCC1=O>Cc1cc(C)c(-c2cccn3c2cc2nc(C)cc(NCCN)c23)c(C)c1
ord_dataset-c3a75813d0b24864aa4f7cd526efd6aa
ord-1d79be6d72524b4e94ffad33aa9b2707
CCOc1ccc(CC(=O)NCCNc2cc(C)nc3cc4c(-c5c(C)cc(C)cc5C)cccn4c23)cc1OC>>CCOc1ccc(CCNCCNc2cc(C)nc3cc4c(-c5c(C)cc(C)cc5C)cccn4c23)cc1OC
N(C)(C)CC.C(C)OC1=C(C=C(C=C1)CC(=O)NCCNC1=CC(=NC=2C=C3C(=CC=CN3C21)C2=C(C=C(C=C2C)C)C)C)OC.[AlH3]>>C(C)OC1=C(C=C(C=C1)CCNCCNC1=CC(=NC=2C=C3C(=CC=CN3C21)C2=C(C=C(C=C2C)C)C)C)OC
O=[C:9]([CH2:8][c:7]1[cH:6][cH:5][c:4]([O:3][CH2:2][CH3:1])[c:38]([O:39][CH3:40])[cH:37]1)[NH:10][CH2:11][CH2:12][NH:13][c:14]1[cH:15][c:16]([CH3:17])[n:18][c:19]2[cH:20][c:21]3[c:22](-[c:23]4[c:24]([CH3:25])[cH:26][c:27]([CH3:28])[cH:29][c:30]4[CH3:31])[cH:32][cH:33][cH:34][n:35]3[c:36]12>>[CH3:1][CH2:2][O:3][c:4]1[cH...
CCOc1ccc(CC(=O)NCCNc2cc(C)nc3cc4c(-c5c(C)cc(C)cc5C)cccn4c23)cc1OC
CCOc1ccc(CCNCCNc2cc(C)nc3cc4c(-c5c(C)cc(C)cc5C)cccn4c23)cc1OC
null
null
C1CCOC1
Reduction
Reduction of secondary amides to amines
85b757f1833edc9e5c6365ee6b904683f414e7b9a5f9bfcfd7addca401447058
ab40188eef2f825df7003af0ffae31d0ce53d126542122535627d3d354cbc9fe
c1ccc(CCNCCNc2ccnc3cc4c(-c5ccccc5)cccn4c23)cc1
O=[C;H0;D3;+0:1](-[#7:2]-[C:3])-[C:4]-[c:5]>>[C:3]-[#7:2]-[CH2;D2;+0:1]-[C:4]-[c:5]
null
[]
null
null
15
MINUTE
Treat a solution of 2-(4-ethoxy-3-methoxy-phenyl)-N-{2-[2-methyl-9-(2,4,6-trimethyl-phenyl)-pyridino[2,3-b]indolizin-4-ylamino]-ethyl}-acetamide (0.08 g, 0.145 mmol) in THF (5 mL) with AlH3.NMe2Et (3 mL, 1.45 mmol) and heat to reflux for 14 h. Cool the resulting mixture to ambient temperature, quench with Na2CO3.10H2O ...
10.6084/m9.figshare.5104873.v1
null
Secondary amide
null
null
null
c1ccccc1.c1ccccc1.c1ccn2c(c1)cc1ncccc12
Other
C1CCOC1
null
0.25
CCOc1ccc(CC(=O)NCCNc2cc(C)nc3cc4c(-c5c(C)cc(C)cc5C)cccn4c23)cc1OC>C1CCOC1>CCOc1ccc(CCNCCNc2cc(C)nc3cc4c(-c5c(C)cc(C)cc5C)cccn4c23)cc1OC
ord_dataset-c3a75813d0b24864aa4f7cd526efd6aa
ord-4395eea2939440faae29dd616f8797af
Cc1cc(C)c(-c2cccn3c2cc2nc(C)nc(O)c23)c(C)c1.O=P(Cl)(Cl)Cl>>Cc1cc(C)c(-c2cccn3c2cc2nc(C)nc(Cl)c23)c(C)c1
CC=1N=C(C2=C(C=C3C(=CC=CN23)C2=C(C=C(C=C2C)C)C)N1)O.P(=O)(Cl)(Cl)Cl>>ClC1=NC(=NC=2C=C3C(=CC=CN3C21)C2=C(C=C(C=C2C)C)C)C
O[c:19]1[n:18][c:16]([CH3:17])[n:15][c:14]2[cH:13][c:12]3[c:7](-[c:6]4[c:4]([CH3:5])[cH:3][c:2]([CH3:1])[cH:24][c:22]4[CH3:23])[cH:8][cH:9][cH:10][n:11]3[c:21]21.O=P(Cl)(Cl)[Cl:20]>>[CH3:1][c:2]1[cH:3][c:4]([CH3:5])[c:6](-[c:7]2[cH:8][cH:9][cH:10][n:11]3[c:12]2[cH:13][c:14]2[n:15][c:16]([CH3:17])[n:18][c:19]([Cl:20])[c...
Cc1cc(C)c(-c2cccn3c2cc2nc(C)nc(O)c23)c(C)c1.O=P(Cl)(Cl)Cl
Cc1cc(C)c(-c2cccn3c2cc2nc(C)nc(Cl)c23)c(C)c1
null
null
null
Functional Group Interconversion
Alcohol to chloride_POCl3_ortho
011132c403ee0a5007ec254ed22d995bfd8c53aaea0928f360354c85698fcdc2
e71580a8ffadb7b2717ecd7d68c1d3c0ca161ba5e6a787a49dad5a1359adc993
c1ccc(-c2cccn3c2cc2ncncc23)cc1
Cl-P(-Cl)(=O)-[Cl;H0;D1;+0:1].O-[c;H0;D3;+0:2]1:[#7;a:3]:[c:4]:[#7;a:5]:[c:6]2:[c:7]:[c:8]:[#7;a:9](:[c:10]):[c:11]:2:1>>[Cl;H0;D1;+0:1]-[c;H0;D3;+0:2]1:[#7;a:3]:[c:4]:[#7;a:5]:[c:6]2:[c:7]:[c:8]:[#7;a:9](:[c:10]):[c:11]:2:1
null
[]
null
null
null
null
Heat at 100° C. for 2 h a solution of 2-methyl-9-(2,4,6-trimethylphenyl)pyrimidino[4,5-b]indolizin-4-ol (120 mg) in phosphorus oxychloride (2 mL), cool to ambient temperature, and concentrate in vacuo. Partition the residue into ice water and CH2Cl2. Extract the aqueous phase twice with CH2Cl2 and wash the combined org...
10.6084/m9.figshare.5104873.v1
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Aromatic alcohol
Aromatic halide
c1ccn2c(c1)cc1ncncc12
c1ccn2c(c1)cc1ncncc12
c1ccccc1.c1ccn2c(c1)cc1ncncc12
HCl
null
null
null
Cc1cc(C)c(-c2cccn3c2cc2nc(C)nc(O)c23)c(C)c1.O=P(Cl)(Cl)Cl>>Cc1cc(C)c(-c2cccn3c2cc2nc(C)nc(Cl)c23)c(C)c1
ord_dataset-c3a75813d0b24864aa4f7cd526efd6aa
ord-9b776e6a19444b638cd2ea1c6264dace
Cc1cc(C)c(-c2cccn3c2cc2nc(C)nc(Cl)c23)c(C)c1.NCCN>>Cc1cc(C)c(-c2cccn3c2cc2nc(C)nc(NCCN)c23)c(C)c1
ClC1=NC(=NC=2C=C3C(=CC=CN3C21)C2=C(C=C(C=C2C)C)C)C.C(CN)N.CCOC(=O)C>>NCCNC1=NC(=NC=2C=C3C(=CC=CN3C21)C2=C(C=C(C=C2C)C)C)C
Cl[c:19]1[n:18][c:16]([CH3:17])[n:15][c:14]2[cH:13][c:12]3[c:7](-[c:6]4[c:4]([CH3:5])[cH:3][c:2]([CH3:1])[cH:27][c:25]4[CH3:26])[cH:8][cH:9][cH:10][n:11]3[c:24]21.[NH2:20][CH2:21][CH2:22][NH2:23]>>[CH3:1][c:2]1[cH:3][c:4]([CH3:5])[c:6](-[c:7]2[cH:8][cH:9][cH:10][n:11]3[c:12]2[cH:13][c:14]2[n:15][c:16]([CH3:17])[n:18][c...
Cc1cc(C)c(-c2cccn3c2cc2nc(C)nc(Cl)c23)c(C)c1.NCCN
Cc1cc(C)c(-c2cccn3c2cc2nc(C)nc(NCCN)c23)c(C)c1
null
null
CN1CCCC1=O
Heteroatom Alkylation and Arylation
N-arylation (Buchwald-Hartwig/Ullmann-Goldberg)
62f88a9d5fc18db0c9f152c03e9572f705ab74d8c34a818f2de56fdd152c9027
71a04ae650defc5edd86a92f43c304e981a05f07ff76248da8d4155f3905a29d
c1ccc(-c2cccn3c2cc2ncncc23)cc1
Cl-[c;H0;D3;+0:1]1:[#7;a:2]:[c:3]:[#7;a:4]:[c:5]2:[c:6]:[c:7]:[#7;a:8](:[c:9]):[c:10]:2:1.[C:11]-[C:12]-[NH2;D1;+0:13]>>[C:11]-[C:12]-[NH;D2;+0:13]-[c;H0;D3;+0:1]1:[#7;a:2]:[c:3]:[#7;a:4]:[c:5]2:[c:6]:[c:7]:[#7;a:8](:[c:9]):[c:10]:2:1
null
[]
null
null
null
null
Heat a solution of 4-chloro-2-methyl-9-(2,4,6-trimethylphenyl)pyrimidino[4,5-b]indolizine (0.3 g, 0.89 mmol), and ethylene diamine (0.6 mL, 8.93 mmol) in dry NMP (3 mL) at 100° C. for 14 h. Pour the cooled mixture onto water (30 mL) and extracte twice with EtOAc (30 mL). Wash the combined extracts with brine (30 mL), d...
10.6084/m9.figshare.5104873.v1
null
Aromatic halide.Primary amine
Secondary amine
c1ccn2c(c1)cc1ncncc12
c1ccn2c(c1)cc1ncncc12
c1ccccc1.c1ccn2c(c1)cc1ncncc12
HCl
CN1CCCC1=O
null
null
Cc1cc(C)c(-c2cccn3c2cc2nc(C)nc(Cl)c23)c(C)c1.NCCN>CN1CCCC1=O>Cc1cc(C)c(-c2cccn3c2cc2nc(C)nc(NCCN)c23)c(C)c1
ord_dataset-c3a75813d0b24864aa4f7cd526efd6aa
ord-b280c7e4cd58488ab2913354e1aa71a7
Cc1cc(C)c(-c2cccn3c2cc2nc(C)nc(NCCN)c23)c(C)c1.O=C1CCCC1>>Cc1cc(C)c(-c2cccn3c2cc2nc(C)nc(NCCNC4CCCC4)c23)c(C)c1
NCCNC1=NC(=NC=2C=C3C(=CC=CN3C21)C2=C(C=C(C=C2C)C)C)C.C1(CCCC1)=O.C(C)(=O)O.C(C)(=O)O[BH-](OC(C)=O)OC(C)=O.[Na+]>>C1(CCCC1)NCCNC1=NC(=NC=2C=C3C(=CC=CN3C21)C2=C(C=C(C=C2C)C)C)C
[CH3:1][c:2]1[cH:3][c:4]([CH3:5])[c:6](-[c:7]2[cH:8][cH:9][cH:10][n:11]3[c:12]2[cH:13][c:14]2[n:15][c:16]([CH3:17])[n:18][c:19]([NH:20][CH2:21][CH2:22][NH2:23])[c:29]32)[c:30]([CH3:31])[cH:32]1.O=[C:24]1[CH2:25][CH2:26][CH2:27][CH2:28]1>>[CH3:1][c:2]1[cH:3][c:4]([CH3:5])[c:6](-[c:7]2[cH:8][cH:9][cH:10][n:11]3[c:12]2[cH...
Cc1cc(C)c(-c2cccn3c2cc2nc(C)nc(NCCN)c23)c(C)c1.O=C1CCCC1
Cc1cc(C)c(-c2cccn3c2cc2nc(C)nc(NCCNC4CCCC4)c23)c(C)c1
null
null
ClC(C)Cl.C(Cl)Cl
Heteroatom Alkylation and Arylation
Reductive amination with ketone
b85679fed5f5625b57908374666b40667904d1ae7fb913f5564f84f7e4e3c6f0
07faf85ffe990e88a1de7fd04a339bf226f78d8bfae9712ea59eebd76bb54b9f
c1ccc(-c2cccn3c2cc2ncnc(NCCNC4CCCC4)c23)cc1
O=[C;H0;D3;+0:1]1-[C:2]-[C:3]-[C:4]-[C:5]-1.[C:6]-[C:7]-[NH2;D1;+0:8]>>[C:6]-[C:7]-[NH;D2;+0:8]-[CH;D3;+0:1]1-[C:2]-[C:3]-[C:4]-[C:5]-1
null
[]
null
null
14
HOUR
Treat a solution of (2-aminoethyl)[2-methyl-9-(2,4,6-trimethylphenyl)pyrimidino[4,5-b]indolizin-4-yl]amine (0.07 g, 0.19 mmol), cyclopentanone (0.02 mL, 0.19 mmol) and acetic acid (0.01 mL, 0.19 mmol) in dry dichloroethane (3 mL) with sodium triacetoxyborohydride (0.06 g, 0.27 mmol) and stir at ambient temperature for ...
10.6084/m9.figshare.5104873.v1
null
Ketone.Primary amine
Secondary amine
C1CCCC1
C1CCCC1
c1ccccc1.c1ccn2c(c1)cc1ncncc12.C1CCCC1
Other
ClC(C)Cl.C(Cl)Cl
null
14
Cc1cc(C)c(-c2cccn3c2cc2nc(C)nc(NCCN)c23)c(C)c1.O=C1CCCC1>ClC(C)Cl.C(Cl)Cl>Cc1cc(C)c(-c2cccn3c2cc2nc(C)nc(NCCNC4CCCC4)c23)c(C)c1
ord_dataset-c3a75813d0b24864aa4f7cd526efd6aa
ord-f807ff24e2804cd888c618644e5b2c6f
CCOc1ccc(CC(=O)NCCN)cc1OC>>CCOc1ccc(CCNCCN)cc1OC
N(C)(C)CC.NCCNC(CC1=CC(=C(C=C1)OCC)OC)=O.[AlH3]>>C(C)OC1=C(C=C(CCNCCN)C=C1)OC
O=[C:9]([CH2:8][c:7]1[cH:6][cH:5][c:4]([O:3][CH2:2][CH3:1])[c:15]([O:16][CH3:17])[cH:14]1)[NH:10][CH2:11][CH2:12][NH2:13]>>[CH3:1][CH2:2][O:3][c:4]1[cH:5][cH:6][c:7]([CH2:8][CH2:9][NH:10][CH2:11][CH2:12][NH2:13])[cH:14][c:15]1[O:16][CH3:17]
CCOc1ccc(CC(=O)NCCN)cc1OC
CCOc1ccc(CCNCCN)cc1OC
null
null
C1CCOC1
Reduction
Reduction of secondary amides to amines
85b757f1833edc9e5c6365ee6b904683f414e7b9a5f9bfcfd7addca401447058
ab40188eef2f825df7003af0ffae31d0ce53d126542122535627d3d354cbc9fe
c1ccccc1
O=[C;H0;D3;+0:1](-[#7:2]-[C:3])-[C:4]-[c:5]>>[C:3]-[#7:2]-[CH2;D2;+0:1]-[C:4]-[c:5]
null
[]
null
null
15
MINUTE
Treat a solution of N-(2-amino-ethyl)-2-(4-ethoxy-3-methoxy-phenyl)acetamide (0.7 g, 2.77 mmol) in THF (10 mL) with AlH3.NMe2Et (55 mL, 27.74 mmol) and heat to reflux for 14 h. Cool the resulting mixture to ambient temperature, quench with Na2CO3.10H2O (0.5 g) and stir at ambient temperature for 15 min. Filter the solu...
10.6084/m9.figshare.5104873.v1
null
Secondary amide
null
null
null
c1ccccc1
Other
C1CCOC1
null
0.25
CCOc1ccc(CC(=O)NCCN)cc1OC>C1CCOC1>CCOc1ccc(CCNCCN)cc1OC
ord_dataset-c3a75813d0b24864aa4f7cd526efd6aa
ord-0e7d3d12db8c48dab2f087c8ed44a567
COc1cc(C)c(-c2cn(C)c3c(Cl)nc(C)nc23)c(C)c1.COc1ccc(CC(=O)NCCN)cc1>>COc1ccc(CC(=O)NCCNc2nc(C)nc3c(-c4c(C)cc(OC)cc4C)cn(C)c23)cc1
ClC=1C2=C(N=C(N1)C)C(=CN2C)C2=C(C=C(C=C2C)OC)C.NCCNC(CC1=CC=C(C=C1)OC)=O.O>>COC1=CC=C(C=C1)CC(=O)NCCNC1=NC(=NC2=C1N(C=C2C2=C(C=C(C=C2C)OC)C)C)C
Cl[c:14]1[n:15][c:16]([CH3:17])[n:18][c:19]2[c:20](-[c:21]3[c:22]([CH3:23])[cH:24][c:25]([O:26][CH3:27])[cH:28][c:29]3[CH3:30])[cH:31][n:32]([CH3:33])[c:34]12.[CH3:1][O:2][c:3]1[cH:4][cH:5][c:6]([CH2:7][C:8](=[O:9])[NH:10][CH2:11][CH2:12][NH2:13])[cH:35][cH:36]1>>[CH3:1][O:2][c:3]1[cH:4][cH:5][c:6]([CH2:7][C:8](=[O:9])...
COc1cc(C)c(-c2cn(C)c3c(Cl)nc(C)nc23)c(C)c1.COc1ccc(CC(=O)NCCN)cc1
COc1ccc(CC(=O)NCCNc2nc(C)nc3c(-c4c(C)cc(OC)cc4C)cn(C)c23)cc1
null
null
CN1CCCC1=O
Heteroatom Alkylation and Arylation
N-arylation (Buchwald-Hartwig/Ullmann-Goldberg)
4e9376aae532abc2c3c92cfa1996ed64a03a89441cc1d43f64dc118dec94ec57
71a04ae650defc5edd86a92f43c304e981a05f07ff76248da8d4155f3905a29d
O=C(Cc1ccccc1)NCCNc1ncnc2c(-c3ccccc3)c[nH]c12
Cl-[c;H0;D3;+0:1]1:[#7;a:2]:[c:3]:[#7;a:4]:[c:5]2:[c:6]:[c:7]:[#7;a:8](-[C;D1;H3:9]):[c:10]:2:1.[C:11]-[C:12]-[NH2;D1;+0:13]>>[C:11]-[C:12]-[NH;D2;+0:13]-[c;H0;D3;+0:1]1:[#7;a:2]:[c:3]:[#7;a:4]:[c:5]2:[c:6]:[c:7]:[#7;a:8](-[C;D1;H3:9]):[c:10]:2:1
null
[]
null
null
null
null
Heat a solution of 4-chloro-7-(4-methoxy-2,6-dimethyl-phenyl)-2,5-dimethyl-5H-pyrrolo[3,2-d]pyrimidine (120 mg, 0.38 mmol) and N-(2-amino-ethyl)-2-(4-methoxyphenyl)-acetamide (125 mg) in NMP (2 mL) for 14 h at 130° C. Pour into water (5 mL) and extract with EtOAc (2×10 mL). Dry the combined organic extracts over Na2SO4...
10.6084/m9.figshare.5104873.v1
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Aromatic halide.Primary amine
Secondary amine
c1ncc2[nH]ccc2n1
c1ncc2[nH]ccc2n1
c1ccccc1.c1ccccc1.c1ncc2[nH]ccc2n1
HCl
CN1CCCC1=O
null
null
COc1cc(C)c(-c2cn(C)c3c(Cl)nc(C)nc23)c(C)c1.COc1ccc(CC(=O)NCCN)cc1>CN1CCCC1=O>COc1ccc(CC(=O)NCCNc2nc(C)nc3c(-c4c(C)cc(OC)cc4C)cn(C)c23)cc1
ord_dataset-c3a75813d0b24864aa4f7cd526efd6aa
ord-d153384e7cbd4e5eaba1412a6dbe40b4
Cc1cc(Cl)c([N+](=O)[O-])c(O)n1.NCc1ccccc1>>Cc1cc(NCc2ccccc2)c([N+](=O)[O-])c(O)n1
ClC1=C(C(=NC(=C1)C)O)[N+](=O)[O-].C(C1=CC=CC=C1)N>>C(C1=CC=CC=C1)NC1=C(C(=NC(=C1)C)O)[N+](=O)[O-]
Cl[c:4]1[cH:3][c:2]([CH3:1])[n:19][c:17]([OH:18])[c:13]1[N+:14](=[O:15])[O-:16].[NH2:5][CH2:6][c:7]1[cH:8][cH:9][cH:10][cH:11][cH:12]1>>[CH3:1][c:2]1[cH:3][c:4]([NH:5][CH2:6][c:7]2[cH:8][cH:9][cH:10][cH:11][cH:12]2)[c:13]([N+:14](=[O:15])[O-:16])[c:17]([OH:18])[n:19]1
Cc1cc(Cl)c([N+](=O)[O-])c(O)n1.NCc1ccccc1
Cc1cc(NCc2ccccc2)c([N+](=O)[O-])c(O)n1
null
null
CCO
Heteroatom Alkylation and Arylation
N-arylation (Buchwald-Hartwig/Ullmann-Goldberg)
c026a7bf7aba66b20cf21a13c528689aaaa1c05901524d62b36ca0c3b0572cef
71a04ae650defc5edd86a92f43c304e981a05f07ff76248da8d4155f3905a29d
c1ccc(CNc2ccncc2)cc1
Cl-[c;H0;D3;+0:1]1:[c:2]:[c:3](-[C;D1;H3:4]):[#7;a:5]:[c:6](-[O;D1;H1:7]):[c:8]:1-[#7;+:9].[NH2;D1;+0:10]-[C:11]-[c:12]>>[#7;+:9]-[c:8]1:[c:6](-[O;D1;H1:7]):[#7;a:5]:[c:3](-[C;D1;H3:4]):[c:2]:[c;H0;D3;+0:1]:1-[NH;D2;+0:10]-[C:11]-[c:12]
null
[]
null
null
null
null
Stir a solution of 4-chloro-6-methyl-3-nitro-pyridin-2-ol (10.0 g, 53.0 mmol) and benzyl amine (17.3 g, 159 mmol) in EtOH (30 mL) at ambient temperature for 12 h, then concentrate in vacuo. Pour the resulting residue into water, acidify to pH 3 with 1N HCl and filter. Wash the precipitate several times with water to ob...
10.6084/m9.figshare.5104873.v1
null
Aromatic halide.Primary amine
Secondary amine
c1ccncc1
c1ccncc1
c1ccncc1.c1ccccc1
HCl
CCO
null
null
Cc1cc(Cl)c([N+](=O)[O-])c(O)n1.NCc1ccccc1>CCO>Cc1cc(NCc2ccccc2)c([N+](=O)[O-])c(O)n1
ord_dataset-c3a75813d0b24864aa4f7cd526efd6aa
ord-ba0681111f0441e59ee860871cbd6cb3
Cc1cc(NCc2ccccc2)c([N+](=O)[O-])c(O)n1.O=P(Cl)(Cl)Cl>>Cc1cc(NCc2ccccc2)c([N+](=O)[O-])c(Cl)n1
C(C1=CC=CC=C1)NC1=C(C(=NC(=C1)C)O)[N+](=O)[O-].P(=O)(Cl)(Cl)Cl>>C(C1=CC=CC=C1)NC1=C(C(=NC(=C1)C)Cl)[N+](=O)[O-]
O[c:17]1[c:13]([N+:14](=[O:15])[O-:16])[c:4]([NH:5][CH2:6][c:7]2[cH:8][cH:9][cH:10][cH:11][cH:12]2)[cH:3][c:2]([CH3:1])[n:19]1.O=P(Cl)(Cl)[Cl:18]>>[CH3:1][c:2]1[cH:3][c:4]([NH:5][CH2:6][c:7]2[cH:8][cH:9][cH:10][cH:11][cH:12]2)[c:13]([N+:14](=[O:15])[O-:16])[c:17]([Cl:18])[n:19]1
Cc1cc(NCc2ccccc2)c([N+](=O)[O-])c(O)n1.O=P(Cl)(Cl)Cl
Cc1cc(NCc2ccccc2)c([N+](=O)[O-])c(Cl)n1
null
[Cl-].C[N+](C)(C)C
null
Functional Group Interconversion
Alcohol to chloride_POCl3_ortho
ab85b19a1f19bdb0596b983dc6471067aedf5e7b894e737e6d16cd077bd81b42
e71580a8ffadb7b2717ecd7d68c1d3c0ca161ba5e6a787a49dad5a1359adc993
c1ccc(CNc2ccncc2)cc1
Cl-P(-Cl)(=O)-[Cl;H0;D1;+0:1].O-[c;H0;D3;+0:2](:[#7;a:3]:[c:4]):[c:5](-[#7;+:6]):[c:7]>>[#7;+:6]-[c:5](:[c:7]):[c;H0;D3;+0:2](-[Cl;H0;D1;+0:1]):[#7;a:3]:[c:4]
null
[]
null
null
null
null
Heat a solution of 4-benzylamino-6-methyl-3-nitro-pyridin-2-ol (13.70 g, 52.8 mmol) and tetramethylammonium chloride (6.0 g, 52.8 mmol) to reflux in phosphorus oxychloride (15 mL) for 5 h. After cooling, remove the excess phosphorus oxychloride in vacuo. Triturate the residue in ice-water (400 mL) to obtain the title c...
10.6084/m9.figshare.5104873.v1
null
Aromatic alcohol
Aromatic halide
c1ccncc1
c1ccncc1
c1ccncc1.c1ccccc1
HCl
[Cl-].C[N+](C)(C)C
null
null
Cc1cc(NCc2ccccc2)c([N+](=O)[O-])c(O)n1.O=P(Cl)(Cl)Cl>[Cl-].C[N+](C)(C)C>Cc1cc(NCc2ccccc2)c([N+](=O)[O-])c(Cl)n1
ord_dataset-c3a75813d0b24864aa4f7cd526efd6aa
ord-93a0e0392bfb41d1a4ce35af9bec7f30
CC1=C([N+](=O)[O-])C(C)(NCc2ccccc2)CC(C)(C)C1Nc1ccccn1>>CC1=C(N)C(C)(NCc2ccccc2)CC(C)(C)C1Nc1ccccn1
CC1(CC(C(=C(C1NC1=NC=CC=C1)C)[N+](=O)[O-])(C)NCC1=CC=CC=C1)C>>NC1=C(C(C(CC1(C)NCC1=CC=CC=C1)(C)C)NC1=NC=CC=C1)C
O=[N+:4]([O-])[C:3]1=[C:2]([CH3:1])[CH:19]([NH:20][c:21]2[cH:22][cH:23][cH:24][cH:25][n:26]2)[C:16]([CH3:17])([CH3:18])[CH2:15][C:5]1([CH3:6])[NH:7][CH2:8][c:9]1[cH:10][cH:11][cH:12][cH:13][cH:14]1>>[CH3:1][C:2]1=[C:3]([NH2:4])[C:5]([CH3:6])([NH:7][CH2:8][c:9]2[cH:10][cH:11][cH:12][cH:13][cH:14]2)[CH2:15][C:16]([CH3:17...
CC1=C([N+](=O)[O-])C(C)(NCc2ccccc2)CC(C)(C)C1Nc1ccccn1
CC1=C(N)C(C)(NCc2ccccc2)CC(C)(C)C1Nc1ccccn1
null
[Fe]
C(C)(=O)O.CO
Reduction
Reduction of nitro groups to amines
af6c5b301491be261a262616a03eb9b7e8465cf4d54efa20d6e4ba026dae1843
932aeb69032745ef767518b2869fbe1b80680a98af29f5f41fa577be193d71ee
C1=CC(Nc2ccccn2)CCC1NCc1ccccc1
O=[N+;H0;D3:1](-[O-])-[C:2](=[C:3](-[C;D1;H3:4])-[C:5])-[C:6]>>[C:5]-[C:3](-[C;D1;H3:4])=[C:2](-[NH2;D1;+0:1])-[C:6]
null
[]
70
CELSIUS
null
null
Add iron powder (7.0 g) to a solution of 6-methyl-3-nitro-4-[benzylamino](2-pyridyl)(2,4,6-trimethylphenyl)amine (8.75 g, 23.2 mmol) in acetic acid (14 mL) and MeOH (70 mL). Heat the resulting mixture at 70° C. for 1 h, cool to ambient temperature, and filter through a pad of celite. Evaporate the filtrate to dryness u...
10.6084/m9.figshare.5104873.v1
null
Enamine
Enamine
null
null
C1=CCCCC1.c1ccccc1.c1ccncc1
Other
[Fe].C(C)(=O)O.CO
70
null
CC1=C([N+](=O)[O-])C(C)(NCc2ccccc2)CC(C)(C)C1Nc1ccccn1>[Fe].C(C)(=O)O.CO>CC1=C(N)C(C)(NCc2ccccc2)CC(C)(C)C1Nc1ccccn1
ord_dataset-c3a75813d0b24864aa4f7cd526efd6aa
ord-ed258c7e10b54f8bb28c48f09d702f3d
Cc1cc(C)c(-n2c(C)nc3c(NCc4ccccc4)cc(C)nc32)c(C)c1>>Cc1cc(C)c(-n2cnc3c(N)cc(C)nc32)c(C)c1
CC=1N(C2=NC(=CC(=C2N1)NCC1=CC=CC=C1)C)C1=C(C=C(C=C1C)C)C>>CC1=CC(=C2C(=N1)N(C=N2)C2=C(C=C(C=C2C)C)C)N
C[c:8]1[n:7](-[c:6]2[c:4]([CH3:5])[cH:3][c:2]([CH3:1])[cH:20][c:18]2[CH3:19])[c:17]2[c:10]([n:9]1)[c:11]([NH:12]Cc1ccccc1)[cH:13][c:14]([CH3:15])[n:16]2>>[CH3:1][c:2]1[cH:3][c:4]([CH3:5])[c:6](-[n:7]2[cH:8][n:9][c:10]3[c:11]([NH2:12])[cH:13][c:14]([CH3:15])[n:16][c:17]23)[c:18]([CH3:19])[cH:20]1
Cc1cc(C)c(-n2c(C)nc3c(NCc4ccccc4)cc(C)nc32)c(C)c1
Cc1cc(C)c(-n2cnc3c(N)cc(C)nc32)c(C)c1
null
[OH-].[Pd+2].[OH-]
C(C)(=O)O
Deprotection
OtherReaction
a8cfbee1f0bfb6466a347fd6c1b5d43b8b332ef3673c8f86756b7c7c72e838f8
f6571fb5b7780a2b467937abfba91ba7d787f19d503265f299ff4a25a08963bd
c1ccc(-n2cnc3cccnc32)cc1
C-[c;H0;D3;+0:1]1:[#7;a:2]:[c:3]2:[c:4](-[NH;D2;+0:5]-C-c3:c:c:c:c:c:3):[c:6]:[c:7]:[#7;a:8]:[c:9]:2:[#7;a:10]:1-[c:11]>>[NH2;D1;+0:5]-[c:4]1:[c:6]:[c:7]:[#7;a:8]:[c:9]2:[#7;a:10](-[c:11]):[cH;D2;+0:1]:[#7;a:2]:[c:3]:1:2
null
[]
null
null
20
HOUR
Add palladium hydroxide (0.05 g) to a solution of [2,5-dimethyl-3-(2,4,6-trimethylphenyl)imidazolo[5,4-b]pyridin-7-yl]benzylamine (0.15 g, 0.42 mmol) in acetic acid (10 mL). Hydrogenate the mixture at a pressure of 50 psi for 20 hr. Filter the reaction mixture through celite, evaporate to dryness under reduced pressure...
10.6084/m9.figshare.5104873.v1
null
Secondary amine
Primary amine
c1ccccc1.c1ccc2nc[nH]c2n1
c1ccc2nc[nH]c2n1
c1ccccc1.c1ccc2nc[nH]c2n1
Other
[OH-].[Pd+2].[OH-].C(C)(=O)O
null
20
Cc1cc(C)c(-n2c(C)nc3c(NCc4ccccc4)cc(C)nc32)c(C)c1>[OH-].[Pd+2].[OH-].C(C)(=O)O>Cc1cc(C)c(-n2cnc3c(N)cc(C)nc32)c(C)c1
ord_dataset-c3a75813d0b24864aa4f7cd526efd6aa
ord-742e002137e348309f2ac695e2683299
Cc1cc(C)c(-n2cnc3c(N)cc(C)nc32)c(C)c1.O=C(Cl)CCl>>Cc1cc(C)c(-n2cnc3c(NC(=O)CCl)cc(C)nc32)c(C)c1
C([O-])([O-])=O.[K+].[K+].CC1=CC(=C2C(=N1)N(C=N2)C2=C(C=C(C=C2C)C)C)N.C(C)(C)N(C(C)C)CC.ClCC(=O)Cl>>CC1=CC(=C2C(=N1)N(C=N2)C2=C(C=C(C=C2C)C)C)NC(CCl)=O
[CH3:1][c:2]1[cH:3][c:4]([CH3:5])[c:6](-[n:7]2[cH:8][n:9][c:10]3[c:11]([NH2:12])[cH:17][c:18]([CH3:19])[n:20][c:21]23)[c:22]([CH3:23])[cH:24]1.Cl[C:13](=[O:14])[CH2:15][Cl:16]>>[CH3:1][c:2]1[cH:3][c:4]([CH3:5])[c:6](-[n:7]2[cH:8][n:9][c:10]3[c:11]([NH:12][C:13](=[O:14])[CH2:15][Cl:16])[cH:17][c:18]([CH3:19])[n:20][c:21...
Cc1cc(C)c(-n2cnc3c(N)cc(C)nc32)c(C)c1.O=C(Cl)CCl
Cc1cc(C)c(-n2cnc3c(NC(=O)CCl)cc(C)nc32)c(C)c1
null
null
ClCCCl
Acylation
Acylation of Nitrogen Nucleophiles by Acyl/Thioacyl/Carbamoyl Halides and Analogs_OS
38143a4d536201990008fd6f2c68e6571a341d1c367481869fbbbe36cb038937
0e6ae078978e324f714e184b4f72826d4e3bf2d9ab22d6e9f73740af687be16f
c1ccc(-n2cnc3cccnc32)cc1
Cl-[C;H0;D3;+0:1](=[O;D1;H0:2])-[C:3]-[Cl;D1;H0:4].[NH2;D1;+0:5]-[c:6]1:[c:7]:[c:8]:[#7;a:9]:[c:10]2:[#7;a:11]:[c:12]:[#7;a:13]:[c:14]:1:2>>[Cl;D1;H0:4]-[C:3]-[C;H0;D3;+0:1](=[O;D1;H0:2])-[NH;D2;+0:5]-[c:6]1:[c:7]:[c:8]:[#7;a:9]:[c:10]2:[#7;a:11]:[c:12]:[#7;a:13]:[c:14]:1:2
null
[]
null
null
null
null
Treat a solution of 5-methyl-3-(2,4,6-trimethylphenyl)imidazolo[5,4-b]pyridin-7-ylamine (0.05 g, 1.9 mmol), and N,N-diisopropylethylamine, (0.04 mL, 0.21 mmol) in 1,2-dichloroethane (5 mL) with chloroacetyl chloride (0.017 mL, 0.21 mmol). Heat the solution to reflux for 3 h, cool to ambient temperature, and pour into a...
10.6084/m9.figshare.5104873.v1
null
Acyl halide.Primary amine
Secondary amide
null
null
c1ccccc1.c1ccc2nc[nH]c2n1
HCl
ClCCCl
null
null
Cc1cc(C)c(-n2cnc3c(N)cc(C)nc32)c(C)c1.O=C(Cl)CCl>ClCCCl>Cc1cc(C)c(-n2cnc3c(NC(=O)CCl)cc(C)nc32)c(C)c1
ord_dataset-c3a75813d0b24864aa4f7cd526efd6aa
ord-ce05fb09294841c38a6645dcd2a972b8
Cc1cc(C)c(-n2cnc3c(NC(=O)CCl)cc(C)nc32)c(C)c1>>Cc1cc(C)c(-n2cnc3c(NCCCl)cc(C)nc32)c(C)c1
CC1=CC(=C2C(=N1)N(C=N2)C2=C(C=C(C=C2C)C)C)NC(CCl)=O>>ClCCNC1=C2C(=NC(=C1)C)N(C=N2)C2=C(C=C(C=C2C)C)C
O=[C:13]([NH:12][c:11]1[c:10]2[n:9][cH:8][n:7](-[c:6]3[c:4]([CH3:5])[cH:3][c:2]([CH3:1])[cH:23][c:21]3[CH3:22])[c:20]2[n:19][c:17]([CH3:18])[cH:16]1)[CH2:14][Cl:15]>>[CH3:1][c:2]1[cH:3][c:4]([CH3:5])[c:6](-[n:7]2[cH:8][n:9][c:10]3[c:11]([NH:12][CH2:13][CH2:14][Cl:15])[cH:16][c:17]([CH3:18])[n:19][c:20]23)[c:21]([CH3:22...
Cc1cc(C)c(-n2cnc3c(NC(=O)CCl)cc(C)nc32)c(C)c1
Cc1cc(C)c(-n2cnc3c(NCCCl)cc(C)nc32)c(C)c1
null
null
C1CCOC1
Reduction
Reduction of secondary amides to amines
85b757f1833edc9e5c6365ee6b904683f414e7b9a5f9bfcfd7addca401447058
ab40188eef2f825df7003af0ffae31d0ce53d126542122535627d3d354cbc9fe
c1ccc(-n2cnc3cccnc32)cc1
O=[C;H0;D3;+0:1](-[#7:2]-[c:3]:[c:4]:[#7;a:5])-[C:6]-[Cl;D1;H0:7]>>[#7;a:5]:[c:4]:[c:3]-[#7:2]-[CH2;D2;+0:1]-[C:6]-[Cl;D1;H0:7]
null
[]
null
null
null
null
Treat a solution of N-[5-methyl-3-(2,4,6-trimethylphenyl)imidazolo[5,4-b]pyridin-7-yl]-2-chloroacetamide (0.04 g, 0.10 mmol) in THF (5 mL) with borane-methyl sulfide complex (0.03 mL, 0.30 mmol). Heat the mixture to reflux for 8 h and quench at ambient temperature with a large excess of MeOH, followed by 6 N HCl (2 mL)...
10.6084/m9.figshare.5104873.v1
null
Secondary amide
null
null
null
c1ccccc1.c1ccc2nc[nH]c2n1
Other
C1CCOC1
null
null
Cc1cc(C)c(-n2cnc3c(NC(=O)CCl)cc(C)nc32)c(C)c1>C1CCOC1>Cc1cc(C)c(-n2cnc3c(NCCCl)cc(C)nc32)c(C)c1
ord_dataset-c3a75813d0b24864aa4f7cd526efd6aa
ord-e1c295b6c13a4b0693de6ccd9488b432
CCOc1ccc(CCN)cc1OC.Cc1cc(C)c(-n2cnc3c(NCCCl)cc(C)nc32)c(C)c1>>CCOc1ccc(CCNCCNc2cc(C)nc3c2ncn3-c2c(C)cc(C)cc2C)cc1OC
ClCCNC1=C2C(=NC(=C1)C)N(C=N2)C2=C(C=C(C=C2C)C)C.C(C)OC1=C(C=C(CCN)C=C1)OC>>C(C)OC1=C(C=C(C=C1)CCNCCNC1=C2C(=NC(=C1)C)N(C=N2)C2=C(C=C(C=C2C)C)C)OC
[CH3:1][CH2:2][O:3][c:4]1[cH:5][cH:6][c:7]([CH2:8][CH2:9][NH2:10])[cH:33][c:34]1[O:35][CH3:36].Cl[CH2:11][CH2:12][NH:13][c:14]1[cH:15][c:16]([CH3:17])[n:18][c:19]2[c:20]1[n:21][cH:22][n:23]2-[c:24]1[c:25]([CH3:26])[cH:27][c:28]([CH3:29])[cH:30][c:31]1[CH3:32]>>[CH3:1][CH2:2][O:3][c:4]1[cH:5][cH:6][c:7]([CH2:8][CH2:9][N...
CCOc1ccc(CCN)cc1OC.Cc1cc(C)c(-n2cnc3c(NCCCl)cc(C)nc32)c(C)c1
CCOc1ccc(CCNCCNc2cc(C)nc3c2ncn3-c2c(C)cc(C)cc2C)cc1OC
null
null
CN1CCCC1=O
Heteroatom Alkylation and Arylation
N-alkylation of primary amines with alkyl halides
fc19a1445ff204e66e51735d0191465bda3c6691fd233624a54742c9d4828411
0b1d32f56ad00f1e5bdae9390f9227bbea012fa2f8203aac34726b8a6761cc7c
c1ccc(CCNCCNc2ccnc3c2ncn3-c2ccccc2)cc1
Cl-[CH2;D2;+0:1]-[C:2]-[#7:3].[C:4]-[C:5]-[NH2;D1;+0:6]>>[#7:3]-[C:2]-[CH2;D2;+0:1]-[NH;D2;+0:6]-[C:5]-[C:4]
null
[]
null
null
null
null
Heat a solution of (2-chloroethyl)[5-methyl-3-(2,4,6-trimethylphenyl)imidazolo[5,4-b]pyridin-7-yl]-amine (0.030 g, 0.09 mmol) and 4-ethoxy-3-methoxy phenethylamine (0.10 g, 0.55 mmol) in dry NMP (2 mL) at 110° C. for 16 h. Pour the cooled mixture onto water (20 mL) and extract twice with EtOAc (20 mL). Wash the combine...
10.6084/m9.figshare.5104873.v1
null
Primary halide.Primary amine
Secondary amine
null
null
c1ccccc1.c1ccc2[nH]cnc2n1.c1ccccc1
HCl
CN1CCCC1=O
null
null
CCOc1ccc(CCN)cc1OC.Cc1cc(C)c(-n2cnc3c(NCCCl)cc(C)nc32)c(C)c1>CN1CCCC1=O>CCOc1ccc(CCNCCNc2cc(C)nc3c2ncn3-c2c(C)cc(C)cc2C)cc1OC
ord_dataset-c3a75813d0b24864aa4f7cd526efd6aa
ord-c9c5398839e8430bb7f6e5356ef0486f
Cc1cc(C)c(-n2c(C)nc3c(NCc4ccccc4)cc(C)nc32)c(C)c1>>Cc1cc(C)c(-n2c(C)nc3c(N)cc(C)nc32)c(C)c1
CC=1N(C2=NC(=CC(=C2N1)NCC1=CC=CC=C1)C)C1=C(C=C(C=C1C)C)C>>CC=1N(C2=NC(=CC(=C2N1)N)C)C1=C(C=C(C=C1C)C)C
c1ccc(C[NH:13][c:12]2[c:11]3[n:10][c:8]([CH3:9])[n:7](-[c:6]4[c:4]([CH3:5])[cH:3][c:2]([CH3:1])[cH:21][c:19]4[CH3:20])[c:18]3[n:17][c:15]([CH3:16])[cH:14]2)cc1>>[CH3:1][c:2]1[cH:3][c:4]([CH3:5])[c:6](-[n:7]2[c:8]([CH3:9])[n:10][c:11]3[c:12]([NH2:13])[cH:14][c:15]([CH3:16])[n:17][c:18]23)[c:19]([CH3:20])[cH:21]1
Cc1cc(C)c(-n2c(C)nc3c(NCc4ccccc4)cc(C)nc32)c(C)c1
Cc1cc(C)c(-n2c(C)nc3c(N)cc(C)nc32)c(C)c1
null
[OH-].[Pd+2].[OH-]
C(C)(=O)O
Deprotection
OtherReaction
93c46c2f9981b731115295839d7158a8a73faedd00707b7604ace2fa5f580cbc
f6571fb5b7780a2b467937abfba91ba7d787f19d503265f299ff4a25a08963bd
c1ccc(-n2cnc3cccnc32)cc1
C(-[NH;D2;+0:1]-[c:2]1:[c:3]:[c:4]:[#7;a:5]:[c:6]2:[#7;a:7]:[c:8]:[#7;a:9]:[c:10]:1:2)-c1:c:c:c:c:c:1>>[NH2;D1;+0:1]-[c:2]1:[c:3]:[c:4]:[#7;a:5]:[c:6]2:[#7;a:7]:[c:8]:[#7;a:9]:[c:10]:1:2
null
[]
null
null
20
HOUR
Add palladium hydroxide (2.0 g) to a solution of [2,5-dimethyl-3-(2,4,6-trimethylphenyl)imidazolo[5,4-b]pyridin-7-yl]benzylamine (1.50 g, 4.05 mmol) in acetic acid (10 mL). Hydrogenate the mixture at a pressure of 40 psi for 20 hr. Filter the reaction mixture through celite, evaporate to dryness under reduced pressure,...
10.6084/m9.figshare.5104873.v1
null
Secondary amine
Primary amine
c1ccccc1
null
c1ccccc1.c1ccc2nc[nH]c2n1
Other
[OH-].[Pd+2].[OH-].C(C)(=O)O
null
20
Cc1cc(C)c(-n2c(C)nc3c(NCc4ccccc4)cc(C)nc32)c(C)c1>[OH-].[Pd+2].[OH-].C(C)(=O)O>Cc1cc(C)c(-n2c(C)nc3c(N)cc(C)nc32)c(C)c1
ord_dataset-c3a75813d0b24864aa4f7cd526efd6aa
ord-bd9ebd31ce7044ed8c20fc1c6accae44
Cc1cc(C)c(-n2c(C)nc3c(N)cc(C)nc32)c(C)c1.O=C(Cl)CCl>>Cc1cc(C)c(-n2c(C)nc3c(NC(=O)CCl)cc(C)nc32)c(C)c1
C([O-])([O-])=O.[K+].[K+].CC=1N(C2=NC(=CC(=C2N1)N)C)C1=C(C=C(C=C1C)C)C.C(C)(C)N(C(C)C)CC.ClCC(=O)Cl>>CC=1N(C2=NC(=CC(=C2N1)NC(CCl)=O)C)C1=C(C=C(C=C1C)C)C
[CH3:1][c:2]1[cH:3][c:4]([CH3:5])[c:6](-[n:7]2[c:8]([CH3:9])[n:10][c:11]3[c:12]([NH2:13])[cH:18][c:19]([CH3:20])[n:21][c:22]23)[c:23]([CH3:24])[cH:25]1.Cl[C:14](=[O:15])[CH2:16][Cl:17]>>[CH3:1][c:2]1[cH:3][c:4]([CH3:5])[c:6](-[n:7]2[c:8]([CH3:9])[n:10][c:11]3[c:12]([NH:13][C:14](=[O:15])[CH2:16][Cl:17])[cH:18][c:19]([C...
Cc1cc(C)c(-n2c(C)nc3c(N)cc(C)nc32)c(C)c1.O=C(Cl)CCl
Cc1cc(C)c(-n2c(C)nc3c(NC(=O)CCl)cc(C)nc32)c(C)c1
null
null
ClCCCl
Acylation
Acylation of Nitrogen Nucleophiles by Acyl/Thioacyl/Carbamoyl Halides and Analogs_OS
38143a4d536201990008fd6f2c68e6571a341d1c367481869fbbbe36cb038937
0e6ae078978e324f714e184b4f72826d4e3bf2d9ab22d6e9f73740af687be16f
c1ccc(-n2cnc3cccnc32)cc1
Cl-[C;H0;D3;+0:1](=[O;D1;H0:2])-[C:3]-[Cl;D1;H0:4].[NH2;D1;+0:5]-[c:6]1:[c:7]:[c:8]:[#7;a:9]:[c:10]2:[#7;a:11]:[c:12]:[#7;a:13]:[c:14]:1:2>>[Cl;D1;H0:4]-[C:3]-[C;H0;D3;+0:1](=[O;D1;H0:2])-[NH;D2;+0:5]-[c:6]1:[c:7]:[c:8]:[#7;a:9]:[c:10]2:[#7;a:11]:[c:12]:[#7;a:13]:[c:14]:1:2
null
[]
null
null
null
null
Treat a solution of 2,5-dimethyl-3-(2,4,6-trimethylphenyl)imidazolo[5,4-b]pyridine-7-ylamine (0.8 g, 2.85 mmol), and N,N-diisopropylethylamine, (0.54 mL, 3.13 mmol) in 1,2-dichloroethane (10 mL) with chloroacetyl chloride (0.25 mL, 3.13 mmol). Heat the solution to reflux for 5 h, cool to ambient temperature, and pour i...
10.6084/m9.figshare.5104873.v1
null
Acyl halide.Primary amine
Secondary amide
null
null
c1ccccc1.c1ccc2nc[nH]c2n1
HCl
ClCCCl
null
null
Cc1cc(C)c(-n2c(C)nc3c(N)cc(C)nc32)c(C)c1.O=C(Cl)CCl>ClCCCl>Cc1cc(C)c(-n2c(C)nc3c(NC(=O)CCl)cc(C)nc32)c(C)c1
ord_dataset-c3a75813d0b24864aa4f7cd526efd6aa
ord-cc91cab80c8644bc95cc5487d3e22d00
Cc1cc(C)c(-n2c(C)nc3c(NC(=O)CCl)cc(C)nc32)c(C)c1>>Cc1cc(C)c(-n2c(C)nc3c(NCCCl)cc(C)nc32)c(C)c1
CC=1N(C2=NC(=CC(=C2N1)NC(CCl)=O)C)C1=C(C=C(C=C1C)C)C>>CC=1N(C2=NC(=CC(=C2N1)NCCCl)C)C1=C(C=C(C=C1C)C)C
O=[C:14]([NH:13][c:12]1[c:11]2[n:10][c:8]([CH3:9])[n:7](-[c:6]3[c:4]([CH3:5])[cH:3][c:2]([CH3:1])[cH:24][c:22]3[CH3:23])[c:21]2[n:20][c:18]([CH3:19])[cH:17]1)[CH2:15][Cl:16]>>[CH3:1][c:2]1[cH:3][c:4]([CH3:5])[c:6](-[n:7]2[c:8]([CH3:9])[n:10][c:11]3[c:12]([NH:13][CH2:14][CH2:15][Cl:16])[cH:17][c:18]([CH3:19])[n:20][c:21...
Cc1cc(C)c(-n2c(C)nc3c(NC(=O)CCl)cc(C)nc32)c(C)c1
Cc1cc(C)c(-n2c(C)nc3c(NCCCl)cc(C)nc32)c(C)c1
null
null
C1CCOC1
Reduction
Reduction of secondary amides to amines
85b757f1833edc9e5c6365ee6b904683f414e7b9a5f9bfcfd7addca401447058
ab40188eef2f825df7003af0ffae31d0ce53d126542122535627d3d354cbc9fe
c1ccc(-n2cnc3cccnc32)cc1
O=[C;H0;D3;+0:1](-[#7:2]-[c:3]:[c:4]:[#7;a:5])-[C:6]-[Cl;D1;H0:7]>>[#7;a:5]:[c:4]:[c:3]-[#7:2]-[CH2;D2;+0:1]-[C:6]-[Cl;D1;H0:7]
null
[]
null
null
null
null
Treat a solution of N-[2,5-dimethyl-3-(2,4,6-trimethylphenyl)imidazolo[5,4-b]pyridin-7-yl]-2-chloroacetamide (0.91 g, 2.55 mmol) in THF (5 mL) with borane-methyl sulfide complex (0.8 mL, 7.65 mmol). Heat the mixture to reflux for 18 h and quench at ambient temperature with a large excess of MeOH, followed by 6N HCl (5 ...
10.6084/m9.figshare.5104873.v1
null
Secondary amide
null
null
null
c1ccccc1.c1ccc2nc[nH]c2n1
Other
C1CCOC1
null
null
Cc1cc(C)c(-n2c(C)nc3c(NC(=O)CCl)cc(C)nc32)c(C)c1>C1CCOC1>Cc1cc(C)c(-n2c(C)nc3c(NCCCl)cc(C)nc32)c(C)c1
ord_dataset-c3a75813d0b24864aa4f7cd526efd6aa
ord-51435ab0d0544cf9ae8e09c96b30e6c1
Cc1cc(C)c(-n2c(C)nc3c(NCCCl)cc(C)nc32)c(C)c1.NC1CCCCC1>>Cc1cc(C)c(-n2c(C)nc3c(NCCNC4CCCCC4)cc(C)nc32)c(C)c1
CC=1N(C2=NC(=CC(=C2N1)NCCCl)C)C1=C(C=C(C=C1C)C)C.C1(CCCCC1)N>>CC=1N(C2=NC(=CC(=C2N1)NCCNC1CCCCC1)C)C1=C(C=C(C=C1C)C)C
Cl[CH2:15][CH2:14][NH:13][c:12]1[c:11]2[n:10][c:8]([CH3:9])[n:7](-[c:6]3[c:4]([CH3:5])[cH:3][c:2]([CH3:1])[cH:30][c:28]3[CH3:29])[c:27]2[n:26][c:24]([CH3:25])[cH:23]1.[NH2:16][CH:17]1[CH2:18][CH2:19][CH2:20][CH2:21][CH2:22]1>>[CH3:1][c:2]1[cH:3][c:4]([CH3:5])[c:6](-[n:7]2[c:8]([CH3:9])[n:10][c:11]3[c:12]([NH:13][CH2:14...
Cc1cc(C)c(-n2c(C)nc3c(NCCCl)cc(C)nc32)c(C)c1.NC1CCCCC1
Cc1cc(C)c(-n2c(C)nc3c(NCCNC4CCCCC4)cc(C)nc32)c(C)c1
null
null
CN1CCCC1=O
Heteroatom Alkylation and Arylation
N-alkylation of primary amines with alkyl halides
fc19a1445ff204e66e51735d0191465bda3c6691fd233624a54742c9d4828411
0b1d32f56ad00f1e5bdae9390f9227bbea012fa2f8203aac34726b8a6761cc7c
c1ccc(-n2cnc3c(NCCNC4CCCCC4)ccnc32)cc1
Cl-[CH2;D2;+0:1]-[C:2]-[#7:3].[C:4]-[C:5](-[NH2;D1;+0:6])-[C:7]>>[#7:3]-[C:2]-[CH2;D2;+0:1]-[NH;D2;+0:6]-[C:5](-[C:4])-[C:7]
null
[]
null
null
null
null
Heat a solution of [2,5-dimethyl-3-(2,4,6-trimethylphenyl)imidazolo[5,4-b]pyridin-7-yl](2-chloroethyl)amine (0.04 g, 0.12 mmol), and cyclohexyl amine (0.13 mL g, 1.16 mmol) in dry NMP (2 mL) at 80° C. for 20 h. Pour the cooled mixture onto water (20 mL) and extract twice with ethyl acetate (20 mL). Wash the combined ex...
10.6084/m9.figshare.5104873.v1
null
Primary halide.Primary amine
Secondary amine
null
null
c1ccccc1.C1CCCCC1.c1ccc2nc[nH]c2n1
HCl
CN1CCCC1=O
null
null
Cc1cc(C)c(-n2c(C)nc3c(NCCCl)cc(C)nc32)c(C)c1.NC1CCCCC1>CN1CCCC1=O>Cc1cc(C)c(-n2c(C)nc3c(NCCNC4CCCCC4)cc(C)nc32)c(C)c1
ord_dataset-c3a75813d0b24864aa4f7cd526efd6aa
ord-d65f2cf901554667a889a13c32f7fb06
COc1ccc(CNc2cc(C)nc3c2nc(C)n3-c2ccc(Cl)cc2Cl)cc1>>Cc1cc(N)c2nc(C)n(-c3ccc(Cl)cc3Cl)c2n1
ClC1=C(C=CC(=C1)Cl)N1C(=NC=2C1=NC(=CC2NCC2=CC=C(C=C2)OC)C)C.C1(=CC=CC=C1)OC.FC(C(=O)O)(F)F.S(O)(O)(=O)=O>>ClC1=C(C=CC(=C1)Cl)N1C(=NC=2C1=NC(=CC2N)C)C
COc1ccc(C[NH:5][c:4]2[cH:3][c:2]([CH3:1])[n:20][c:19]3[c:6]2[n:7][c:8]([CH3:9])[n:10]3-[c:11]2[cH:12][cH:13][c:14]([Cl:15])[cH:16][c:17]2[Cl:18])cc1>>[CH3:1][c:2]1[cH:3][c:4]([NH2:5])[c:6]2[n:7][c:8]([CH3:9])[n:10](-[c:11]3[cH:12][cH:13][c:14]([Cl:15])[cH:16][c:17]3[Cl:18])[c:19]2[n:20]1
COc1ccc(CNc2cc(C)nc3c2nc(C)n3-c2ccc(Cl)cc2Cl)cc1
Cc1cc(N)c2nc(C)n(-c3ccc(Cl)cc3Cl)c2n1
null
null
C(=O)(O)[O-].[Na+]
Reduction
OtherReaction
bd6cc2ddd30b209c36eb43f9e2d163a4da40f8a48bda8b578aa13caf5d4fe5dd
79272555d5bd71219cf9e8b42c4ac12a30bbf383c58cfbccf49a5a990e3653c1
c1ccc(-n2cnc3cccnc32)cc1
C-O-c1:c:c:c(-C-[NH;D2;+0:1]-[c:2]2:[c:3]:[c:4]:[#7;a:5]:[c:6]3:[#7;a:7]:[c:8]:[#7;a:9]:[c:10]:3:2):c:c:1>>[NH2;D1;+0:1]-[c:2]1:[c:3]:[c:4]:[#7;a:5]:[c:6]2:[#7;a:7]:[c:8]:[#7;a:9]:[c:10]:2:1
null
[]
null
null
null
null
Stir a solution of [3-(2,4-dichlorophenyl)-2,5-dimethylimidazolo[5,4-b]pyridin-7-yl](4-methoxybenzyl)amine (4.23 g, 10 mmol), anisole (3.2 mL, 29.6 mmol), trifluoroacetic acid (80 mL), and concentrated sulfuric acid (2 mL) at ambient temperature for 14 h. Add the resulting mixture dropwise to ice-water and dilute with ...
10.6084/m9.figshare.5104873.v1
null
Ether.Secondary amine
Primary amine
c1ccccc1
null
c1ccc2[nH]cnc2n1.c1ccccc1
HO-
C(=O)(O)[O-].[Na+]
null
null
COc1ccc(CNc2cc(C)nc3c2nc(C)n3-c2ccc(Cl)cc2Cl)cc1>C(=O)(O)[O-].[Na+]>Cc1cc(N)c2nc(C)n(-c3ccc(Cl)cc3Cl)c2n1
ord_dataset-c3a75813d0b24864aa4f7cd526efd6aa
ord-fdfd86257a8f43f7bfd2fa8ca41ff73e
Cc1cc(N)c2nc(C)n(-c3ccc(Cl)cc3Cl)c2n1.O=C(Cl)CCl>>Cc1cc(NC(=O)CCl)c2nc(C)n(-c3ccc(Cl)cc3Cl)c2n1
C([O-])([O-])=O.[K+].[K+].ClC1=C(C=CC(=C1)Cl)N1C(=NC=2C1=NC(=CC2N)C)C.C(C)(C)N(C(C)C)CC.ClCC(=O)Cl>>ClC1=C(C=CC(=C1)Cl)N1C(=NC=2C1=NC(=CC2NC(CCl)=O)C)C
[CH3:1][c:2]1[cH:3][c:4]([NH2:5])[c:10]2[n:11][c:12]([CH3:13])[n:14](-[c:15]3[cH:16][cH:17][c:18]([Cl:19])[cH:20][c:21]3[Cl:22])[c:23]2[n:24]1.Cl[C:6](=[O:7])[CH2:8][Cl:9]>>[CH3:1][c:2]1[cH:3][c:4]([NH:5][C:6](=[O:7])[CH2:8][Cl:9])[c:10]2[n:11][c:12]([CH3:13])[n:14](-[c:15]3[cH:16][cH:17][c:18]([Cl:19])[cH:20][c:21]3[C...
Cc1cc(N)c2nc(C)n(-c3ccc(Cl)cc3Cl)c2n1.O=C(Cl)CCl
Cc1cc(NC(=O)CCl)c2nc(C)n(-c3ccc(Cl)cc3Cl)c2n1
null
null
ClCCCl
Acylation
Acylation of Nitrogen Nucleophiles by Acyl/Thioacyl/Carbamoyl Halides and Analogs_OS
38143a4d536201990008fd6f2c68e6571a341d1c367481869fbbbe36cb038937
0e6ae078978e324f714e184b4f72826d4e3bf2d9ab22d6e9f73740af687be16f
c1ccc(-n2cnc3cccnc32)cc1
Cl-[C;H0;D3;+0:1](=[O;D1;H0:2])-[C:3]-[Cl;D1;H0:4].[NH2;D1;+0:5]-[c:6]1:[c:7]:[c:8]:[#7;a:9]:[c:10]2:[#7;a:11]:[c:12]:[#7;a:13]:[c:14]:2:1>>[Cl;D1;H0:4]-[C:3]-[C;H0;D3;+0:1](=[O;D1;H0:2])-[NH;D2;+0:5]-[c:6]1:[c:7]:[c:8]:[#7;a:9]:[c:10]2:[#7;a:11]:[c:12]:[#7;a:13]:[c:14]:2:1
null
[]
null
null
null
null
Treat a solution of 3-(2,4-dichlorophenyl)-2,5-dimethylimidazolo[5,4-b]pyridin-7-ylamine (0.2 g, 0.65 mmol), and N,N-diisopropylethylamine, (0.12 mL, 0.72 mmol) in 1,2-dichloroethane (10 mL) with chloroacetyl chloride (0.06 mL, 30.72 mmol). Heat the solution to reflux for 2 h, cool to ambient temperature, and pour into...
10.6084/m9.figshare.5104873.v1
null
Acyl halide.Primary amine
Secondary amide
null
null
c1ccc2[nH]cnc2n1.c1ccccc1
HCl
ClCCCl
null
null
Cc1cc(N)c2nc(C)n(-c3ccc(Cl)cc3Cl)c2n1.O=C(Cl)CCl>ClCCCl>Cc1cc(NC(=O)CCl)c2nc(C)n(-c3ccc(Cl)cc3Cl)c2n1
ord_dataset-c3a75813d0b24864aa4f7cd526efd6aa
ord-6b4d01944ca74127aa34c6e0d30c2413
Cc1cc(NC(=O)CCl)c2nc(C)n(-c3ccc(Cl)cc3Cl)c2n1>>Cc1cc(NCCCl)c2nc(C)n(-c3ccc(Cl)cc3Cl)c2n1
ClC1=C(C=CC(=C1)Cl)N1C(=NC=2C1=NC(=CC2NC(CCl)=O)C)C>>ClC1=C(C=CC(=C1)Cl)N1C(=NC=2C1=NC(=CC2NCCCl)C)C
O=[C:6]([NH:5][c:4]1[cH:3][c:2]([CH3:1])[n:23][c:22]2[c:9]1[n:10][c:11]([CH3:12])[n:13]2-[c:14]1[cH:15][cH:16][c:17]([Cl:18])[cH:19][c:20]1[Cl:21])[CH2:7][Cl:8]>>[CH3:1][c:2]1[cH:3][c:4]([NH:5][CH2:6][CH2:7][Cl:8])[c:9]2[n:10][c:11]([CH3:12])[n:13](-[c:14]3[cH:15][cH:16][c:17]([Cl:18])[cH:19][c:20]3[Cl:21])[c:22]2[n:23...
Cc1cc(NC(=O)CCl)c2nc(C)n(-c3ccc(Cl)cc3Cl)c2n1
Cc1cc(NCCCl)c2nc(C)n(-c3ccc(Cl)cc3Cl)c2n1
null
null
C1CCOC1
Reduction
Reduction of secondary amides to amines
85b757f1833edc9e5c6365ee6b904683f414e7b9a5f9bfcfd7addca401447058
ab40188eef2f825df7003af0ffae31d0ce53d126542122535627d3d354cbc9fe
c1ccc(-n2cnc3cccnc32)cc1
O=[C;H0;D3;+0:1](-[#7:2]-[c:3]:[c:4]:[#7;a:5])-[C:6]-[Cl;D1;H0:7]>>[#7;a:5]:[c:4]:[c:3]-[#7:2]-[CH2;D2;+0:1]-[C:6]-[Cl;D1;H0:7]
null
[]
null
null
null
null
Treat a solution of N-[3-(2,4-dichlorophenyl)-2,5-dimethylimidazolo[5,4-b]pyridin-7-yl]-2-chloroacetamide (1.0 g, 2.6 mmol) in THF (5 mL) with borane-methyl sulfide complex (0.8 mL, 7.8 mmol). Heat the mixture to reflux for 3 h and quench at ambient temperature with a large excess of MeOH followed by 5 N HCl (2 mL). Re...
10.6084/m9.figshare.5104873.v1
null
Secondary amide
null
null
null
c1ccc2[nH]cnc2n1.c1ccccc1
Other
C1CCOC1
null
null
Cc1cc(NC(=O)CCl)c2nc(C)n(-c3ccc(Cl)cc3Cl)c2n1>C1CCOC1>Cc1cc(NCCCl)c2nc(C)n(-c3ccc(Cl)cc3Cl)c2n1
ord_dataset-c3a75813d0b24864aa4f7cd526efd6aa
ord-1f94f7901d2048a4838a642508af10ca
Cc1cc(NCCCl)c2nc(C)n(-c3ccc(Cl)cc3Cl)c2n1.NC1CCCC1>>Cc1cc(NCCNC2CCCC2)c2nc(C)n(-c3ccc(Cl)cc3Cl)c2n1
ClC1=C(C=CC(=C1)Cl)N1C(=NC=2C1=NC(=CC2NCCCl)C)C.C1(CCCC1)N>>ClC1=C(C=CC(=C1)Cl)N1C(=NC=2C1=NC(=CC2NCCNC2CCCC2)C)C
Cl[CH2:7][CH2:6][NH:5][c:4]1[cH:3][c:2]([CH3:1])[n:28][c:27]2[c:14]1[n:15][c:16]([CH3:17])[n:18]2-[c:19]1[cH:20][cH:21][c:22]([Cl:23])[cH:24][c:25]1[Cl:26].[NH2:8][CH:9]1[CH2:10][CH2:11][CH2:12][CH2:13]1>>[CH3:1][c:2]1[cH:3][c:4]([NH:5][CH2:6][CH2:7][NH:8][CH:9]2[CH2:10][CH2:11][CH2:12][CH2:13]2)[c:14]2[n:15][c:16]([CH...
Cc1cc(NCCCl)c2nc(C)n(-c3ccc(Cl)cc3Cl)c2n1.NC1CCCC1
Cc1cc(NCCNC2CCCC2)c2nc(C)n(-c3ccc(Cl)cc3Cl)c2n1
null
null
CN1CCCC1=O
Heteroatom Alkylation and Arylation
N-alkylation of primary amines with alkyl halides
fc19a1445ff204e66e51735d0191465bda3c6691fd233624a54742c9d4828411
0b1d32f56ad00f1e5bdae9390f9227bbea012fa2f8203aac34726b8a6761cc7c
c1ccc(-n2cnc3c(NCCNC4CCCC4)ccnc32)cc1
Cl-[CH2;D2;+0:1]-[C:2]-[#7:3].[C:4]-[C:5](-[NH2;D1;+0:6])-[C:7]>>[#7:3]-[C:2]-[CH2;D2;+0:1]-[NH;D2;+0:6]-[C:5](-[C:4])-[C:7]
null
[]
null
null
null
null
Heat a solution of [3-(2,4-dichlorophenyl)-2,5-dimethylimidazolo[5,4-b]pyridin-7-yl](2-chloroethyl)amine (0.08 g, 0.22 mmol), and cyclopentyl amine (0.2 mL g, 0.22 mmol) in dry NMP (3 mL) at 80° C. for 20 h. Pour the cooled mixture onto water (30 mL) and extract twice with EtOAc (50 mL). Wash the combined extracts with...
10.6084/m9.figshare.5104873.v1
null
Primary halide.Primary amine
Secondary amine
null
null
C1CCCC1.c1ccc2[nH]cnc2n1.c1ccccc1
HCl
CN1CCCC1=O
null
null
Cc1cc(NCCCl)c2nc(C)n(-c3ccc(Cl)cc3Cl)c2n1.NC1CCCC1>CN1CCCC1=O>Cc1cc(NCCNC2CCCC2)c2nc(C)n(-c3ccc(Cl)cc3Cl)c2n1
ord_dataset-c3a75813d0b24864aa4f7cd526efd6aa
ord-863e557edd7e499d827a0df1bcec0c60
CC(=O)c1c(Cl)cccc1Cl.CCOC(=O)C(=O)OCC>>CCOC(=O)C(=O)CC(=O)c1c(Cl)cccc1Cl
ClC1=C(C(=CC=C1)Cl)C(C)=O.C(C(=O)OCC)(=O)OCC.[H-].[Na+]>>ClC1=C(C(=CC=C1)Cl)C(CC(C(=O)OCC)=O)=O
[CH3:8][C:9](=[O:10])[c:11]1[c:12]([Cl:13])[cH:14][cH:15][cH:16][c:17]1[Cl:18].CCO[C:6]([C:4]([O:3][CH2:2][CH3:1])=[O:5])=[O:7]>>[CH3:1][CH2:2][O:3][C:4](=[O:5])[C:6](=[O:7])[CH2:8][C:9](=[O:10])[c:11]1[c:12]([Cl:13])[cH:14][cH:15][cH:16][c:17]1[Cl:18]
CC(=O)c1c(Cl)cccc1Cl.CCOC(=O)C(=O)OCC
CCOC(=O)C(=O)CC(=O)c1c(Cl)cccc1Cl
null
null
C1(=CC=CC=C1)C
C-C Coupling
OtherReaction
75e47111412c372865b4b8c2556a24f38f2daf372ab5522938a6e976b4732185
907e247f98c28f5bcc369b20fadcc26c24574c2b68d4b59762f1e8515d373c02
c1ccccc1
C-C-O-[C;H0;D3;+0:1](=[O;D1;H0:2])-[C:3](=[O;D1;H0:4])-[#8:5]-[C:6].[CH3;D1;+0:7]-[C:8](=[O;D1;H0:9])-[c:10]>>[C:6]-[#8:5]-[C:3](=[O;D1;H0:4])-[C;H0;D3;+0:1](=[O;D1;H0:2])-[CH2;D2;+0:7]-[C:8](=[O;D1;H0:9])-[c:10]
null
[]
null
null
null
null
To a solution of 2′,6′-dichloroacetophenone (12.5 g, 66 mmol) and diethyl oxalate (14.6 g, 100 mmol) in 450 mL of anhydrous toluene, cautiously add sodium hydride (60% dispersion in mineral oil, 2.8 g, 70 mmol). Cautiously heat the reaction mixture to reflux under N2 for 1 h, cool to ambient temperature and pour onto i...
10.6084/m9.figshare.5104873.v1
null
Ketone.Ester.Ester
Ketone.Ketone
null
null
c1ccccc1
HO-
C1(=CC=CC=C1)C
null
null
CC(=O)c1c(Cl)cccc1Cl.CCOC(=O)C(=O)OCC>C1(=CC=CC=C1)C>CCOC(=O)C(=O)CC(=O)c1c(Cl)cccc1Cl
ord_dataset-c3a75813d0b24864aa4f7cd526efd6aa
ord-2f1f42acdc234f729f366de830183706
CCOC(=O)C(=O)CC(=O)c1c(Cl)cccc1Cl.O=N[O-]>>CCOC(=O)C(=O)C(=NO)C(=O)c1c(Cl)cccc1Cl
Cl.N(=O)[O-].[Na+].ClC1=C(C(=CC=C1)Cl)C(CC(C(=O)OCC)=O)=O>>ClC1=C(C(=CC=C1)Cl)C(C(C(C(=O)OCC)=O)=NO)=O
[CH3:1][CH2:2][O:3][C:4](=[O:5])[C:6](=[O:7])[CH2:8][C:11](=[O:12])[c:13]1[c:14]([Cl:15])[cH:16][cH:17][cH:18][c:19]1[Cl:20].O=[N:9][O-:10]>>[CH3:1][CH2:2][O:3][C:4](=[O:5])[C:6](=[O:7])[C:8](=[N:9][OH:10])[C:11](=[O:12])[c:13]1[c:14]([Cl:15])[cH:16][cH:17][cH:18][c:19]1[Cl:20]
CCOC(=O)C(=O)CC(=O)c1c(Cl)cccc1Cl.O=N[O-]
CCOC(=O)C(=O)C(=NO)C(=O)c1c(Cl)cccc1Cl
null
null
CCO
Heteroatom Alkylation and Arylation
OtherReaction
9638fdacd8d405b0a44d1ce6aba3da753854cff65501b5a57f0aafc95fc4c4f0
d3bd726ddd957b1a2366e6bbf86ce90af8c1a91be2fc86e65360edda049ba84b
c1ccccc1
O=[N;H0;D2;+0:1]-[O-;H0;D1:2].[C:3]-[#8:4]-[C:5](=[O;D1;H0:6])-[C:7](=[O;D1;H0:8])-[CH2;D2;+0:9]-[C:10](=[O;D1;H0:11])-[c:12]>>[C:3]-[#8:4]-[C:5](=[O;D1;H0:6])-[C:7](=[O;D1;H0:8])-[C;H0;D3;+0:9](=[N;H0;D2;+0:1]-[OH;D1;+0:2])-[C:10](=[O;D1;H0:11])-[c:12]
null
[]
null
null
null
null
Slowly bubble N2O3 gas (generated by the dropwise addition of concentrated HCl into an aqueous solution of sodium nitrite) into a stirred solution of ethyl 4-(2,6-dichlorophenyl)-2,4-dioxobutanoate (14.4 g, 50 mmol) in EtOH (300 mL) until the reaction is complete (as determined by TLC). Remove the EtOH by evaporation u...
10.6084/m9.figshare.5104873.v1
null
Ketone.Ketone.Nitroso
Ketone.Ketone.Oxime
null
null
c1ccccc1
HO-
CCO
null
null
CCOC(=O)C(=O)CC(=O)c1c(Cl)cccc1Cl.O=N[O-]>CCO>CCOC(=O)C(=O)C(=NO)C(=O)c1c(Cl)cccc1Cl
ord_dataset-c3a75813d0b24864aa4f7cd526efd6aa
ord-ee8a7298a6884a1f828e5aabb66ebe39
CCOC(=O)C(=O)C(=NO)C(=O)c1c(Cl)cccc1Cl.CNN>>CCOC(=O)c1nn(C)c(-c2c(Cl)cccc2Cl)c1N
CNN.ClC1=C(C(=CC=C1)Cl)C(C(C(C(=O)OCC)=O)=NO)=O.Cl>>NC=1C(=NN(C1C1=C(C=CC=C1Cl)Cl)C)C(=O)OCC
O=[C:6]([C:4]([O:3][CH2:2][CH3:1])=[O:5])[C:19]([C:10](=O)[c:11]1[c:12]([Cl:13])[cH:14][cH:15][cH:16][c:17]1[Cl:18])=[N:20]O.[NH2:7][NH:8][CH3:9]>>[CH3:1][CH2:2][O:3][C:4](=[O:5])[c:6]1[n:7][n:8]([CH3:9])[c:10](-[c:11]2[c:12]([Cl:13])[cH:14][cH:15][cH:16][c:17]2[Cl:18])[c:19]1[NH2:20]
CCOC(=O)C(=O)C(=NO)C(=O)c1c(Cl)cccc1Cl.CNN
CCOC(=O)c1nn(C)c(-c2c(Cl)cccc2Cl)c1N
null
null
CO
Aromatic Heterocycle Formation
OtherReaction
e4c6ec0e05e1c203106a5b5aa997e8a1ccd7f76a640bd7c557c3b58ce08a8ce3
5d820015a1c4befea2445c7bdac96cc1fe907ff48e6873810c167772c5bb36e5
c1ccc(-c2ccn[nH]2)cc1
O-[N;H0;D2;+0:1]=[C;H0;D3;+0:2](-[C;H0;D3;+0:3](=O)-[c;H0;D3;+0:4](:[c:5](-[Cl;D1;H0:6]):[c:7]):[c:8](-[Cl;D1;H0:9]):[c:10])-[C;H0;D3;+0:11](=O)-[C:12](=[O;D1;H0:13])-[#8:14]-[C:15].[C;D1;H3:16]-[NH;D2;+0:17]-[NH2;D1;+0:18]>>[C:15]-[#8:14]-[C:12](=[O;D1;H0:13])-[c;H0;D3;+0:11]1:[n;H0;D2;+0:18]:[n;H0;D3;+0:17](-[C;D1;H3...
null
[]
null
null
8
HOUR
To a solution of ethyl 4-(2,6-dichlorophenyl)-3-(hydroxyimino)-2,4-dioxobutanoate (14 g, 44 mmol) in MeOH (400 mL) at 0° C., add dropwise-concentrated HCl (10 mL) followed by methyl hydrazine (2.02 g, 44 mmol). Stir the reaction mixture at ambient temperature for 8 h and concentrate in vacuo. Partition the residue betw...
10.6084/m9.figshare.5104873.v1
null
Hydrazine.Ketone.Ketone.Ester.Oxime
Ester.Primary amine
null
c1cn[nH]c1
c1cn[nH]c1.c1ccccc1
HO-
CO
null
8
CCOC(=O)C(=O)C(=NO)C(=O)c1c(Cl)cccc1Cl.CNN>CO>CCOC(=O)c1nn(C)c(-c2c(Cl)cccc2Cl)c1N
ord_dataset-c3a75813d0b24864aa4f7cd526efd6aa
ord-54c31ae7d8f345268fd8807691204861
Cc1nc(Cl)c2nn(C)c(-c3c(Cl)cccc3Cl)c2n1.NCCN>>Cc1nc(NCCN)c2nn(C)c(-c3c(Cl)cccc3Cl)c2n1
ClC1=C(C(=CC=C1)Cl)C=1N(N=C2C1N=C(N=C2Cl)C)C.C(CN)N>>NCCNC1=NC(=NC=2C1=NN(C2C2=C(C=CC=C2Cl)Cl)C)C
Cl[c:4]1[n:3][c:2]([CH3:1])[n:23][c:22]2[c:9]1[n:10][n:11]([CH3:12])[c:13]2-[c:14]1[c:15]([Cl:16])[cH:17][cH:18][cH:19][c:20]1[Cl:21].[NH2:5][CH2:6][CH2:7][NH2:8]>>[CH3:1][c:2]1[n:3][c:4]([NH:5][CH2:6][CH2:7][NH2:8])[c:9]2[n:10][n:11]([CH3:12])[c:13](-[c:14]3[c:15]([Cl:16])[cH:17][cH:18][cH:19][c:20]3[Cl:21])[c:22]2[n:...
Cc1nc(Cl)c2nn(C)c(-c3c(Cl)cccc3Cl)c2n1.NCCN
Cc1nc(NCCN)c2nn(C)c(-c3c(Cl)cccc3Cl)c2n1
null
null
C(C)#N
Heteroatom Alkylation and Arylation
N-arylation (Buchwald-Hartwig/Ullmann-Goldberg)
90788f58b1dab3f5c9d9dae91bbc2ea7662e25e823d106feb56d7b4d01eeed0b
71a04ae650defc5edd86a92f43c304e981a05f07ff76248da8d4155f3905a29d
c1ccc(-c2[nH]nc3cncnc23)cc1
Cl-[c;H0;D3;+0:1]1:[#7;a:2]:[c:3]:[#7;a:4]:[c:5]2:[c:6]:[#7;a:7](-[C;D1;H3:8]):[#7;a:9]:[c:10]:2:1.[C:11]-[C:12]-[NH2;D1;+0:13]>>[C:11]-[C:12]-[NH;D2;+0:13]-[c;H0;D3;+0:1]1:[#7;a:2]:[c:3]:[#7;a:4]:[c:5]2:[c:6]:[#7;a:7](-[C;D1;H3:8]):[#7;a:9]:[c:10]:2:1
null
[]
null
null
null
null
To a stirred solution of 3-(2,6-dichlorophenyl)-7-chloro-2,5-dimethylpyrazolo[4,3-d]pyrimidine (652 mg, 2.0 mmol) in acetonitrile (50 mL) at 50° C., add ethylene diamine (2.4 g, 40 mmol) in one portion. Maintain the reaction at 50° C. for 2 h, cool to ambient temperature and remove the volatiles by evaporation. Partiti...
10.6084/m9.figshare.5104873.v1
null
Aromatic halide.Primary amine
Secondary amine
c1ncc2[nH]ncc2n1
c1ncc2[nH]ncc2n1
c1ncc2[nH]ncc2n1.c1ccccc1
HCl
C(C)#N
null
null
Cc1nc(Cl)c2nn(C)c(-c3c(Cl)cccc3Cl)c2n1.NCCN>C(C)#N>Cc1nc(NCCN)c2nn(C)c(-c3c(Cl)cccc3Cl)c2n1
ord_dataset-c3a75813d0b24864aa4f7cd526efd6aa
ord-1b888f0018af40c7a2290f4c72bf12da
CCOc1ccc(CC(=O)O)cc1OC.Cc1nc(NCCN)c2nn(C)c(-c3c(Cl)cccc3Cl)c2n1>>CCOc1ccc(C(Nc2nc(C)nc3c(-c4c(Cl)cccc4Cl)n(C)nc23)C(N)=O)cc1OC
NCCNC1=NC(=NC=2C1=NN(C2C2=C(C=CC=C2Cl)Cl)C)C.CN1CCOCC1.C(C)OC1=C(C=C(C=C1)CC(=O)O)OC.O=C1OCCN1P(=O)(N1C(OCC1)=O)Cl>>ClC1=C(C(=CC=C1)Cl)C=1N(N=C2C(=NC(=NC21)C)NC(C(=O)N)C2=CC(=C(C=C2)OCC)OC)C
O[C:29]([CH2:8][c:7]1[cH:6][cH:5][c:4]([O:3][CH2:2][CH3:1])[c:33]([O:34][CH3:35])[cH:32]1)=[O:31].C(C[NH2:30])[NH:9][c:10]1[n:11][c:12]([CH3:13])[n:14][c:15]2[c:16](-[c:17]3[c:18]([Cl:19])[cH:20][cH:21][cH:22][c:23]3[Cl:24])[n:25]([CH3:26])[n:27][c:28]12>>[CH3:1][CH2:2][O:3][c:4]1[cH:5][cH:6][c:7]([CH:8]([NH:9][c:10]2[...
CCOc1ccc(CC(=O)O)cc1OC.Cc1nc(NCCN)c2nn(C)c(-c3c(Cl)cccc3Cl)c2n1
CCOc1ccc(C(Nc2nc(C)nc3c(-c4c(Cl)cccc4Cl)n(C)nc23)C(N)=O)cc1OC
null
null
CN(C(C)=O)C.CCOC(=O)C
Acylation
OtherReaction
7fd04dea0988f7e8650366ae1e798c3a521907e16b31c0690d4a8ad7bb63ddcf
96ca7822a3bd0940a911422d3c93a7753d1a74d2e8ab35b13ac09ac85eb42ae5
c1ccc(CNc2ncnc3c(-c4ccccc4)[nH]nc23)cc1
O-[C;H0;D3;+0:1](=[O;D1;H0:2])-[CH2;D2;+0:3]-[c:4](:[c:5]):[c:6].[NH2;D1;+0:7]-C-C-[NH;D2;+0:8]-[c:9]1:[#7;a:10]:[c:11]:[#7;a:12]:[c:13]2:[c:14]:[#7;a:15]:[#7;a:16]:[c:17]:1:2>>[NH2;D1;+0:7]-[C;H0;D3;+0:1](=[O;D1;H0:2])-[CH;D3;+0:3](-[NH;D2;+0:8]-[c:9]1:[#7;a:10]:[c:11]:[#7;a:12]:[c:13]2:[c:14]:[#7;a:15]:[#7;a:16]:[c:1...
null
[]
null
null
14
HOUR
To a stirred solution of (2-aminoethyl)[3-(2,6-dichlorophenyl)-2,5-dimethylpyrazolo[3,4-e]pyrimidin-7-yl]amine (175 mg, 0.5 mmol) in N,N-dimethylacetamide (5 mL), add 4-methylmorpholine (101 mg, 1.0 mmol), 2-(4-ethoxy-3-methoxyphenyl)acetic acid (115 mg, 0.55 mmol) and bis(2-oxo-3-oxazolidinyl)phosphinic chloride (331 ...
10.6084/m9.figshare.5104873.v1
null
Carboxylic acid.Primary amine.Secondary amine
Primary amide.Secondary amine
null
null
c1ccccc1.c1ccccc1.c1ncc2n[nH]cc2n1
HO-
CN(C(C)=O)C.CCOC(=O)C
null
14
CCOc1ccc(CC(=O)O)cc1OC.Cc1nc(NCCN)c2nn(C)c(-c3c(Cl)cccc3Cl)c2n1>CN(C(C)=O)C.CCOC(=O)C>CCOc1ccc(C(Nc2nc(C)nc3c(-c4c(Cl)cccc4Cl)n(C)nc23)C(N)=O)cc1OC
ord_dataset-c3a75813d0b24864aa4f7cd526efd6aa
ord-a8e838d24581408dac1aacea7fd8421f
Cc1nc(Cl)c([N+](=O)[O-])c(Cl)n1>>Cc1nc(Cl)c(N)c(Cl)n1
ClC1=NC(=NC(=C1[N+](=O)[O-])Cl)C>>ClC1=NC(=NC(=C1N)Cl)C
O=[N+:7]([O-])[c:6]1[c:4]([Cl:5])[n:3][c:2]([CH3:1])[n:10][c:8]1[Cl:9]>>[CH3:1][c:2]1[n:3][c:4]([Cl:5])[c:6]([NH2:7])[c:8]([Cl:9])[n:10]1
Cc1nc(Cl)c([N+](=O)[O-])c(Cl)n1
Cc1nc(Cl)c(N)c(Cl)n1
null
[Fe]
C(C)(=O)O.CO
Reduction
Reduction of nitro groups to amines
bbc242b150a51e69d3ad1caaa391f4422710431b398dcb880555f476706790be
7b0317532ea57a4fcedc1efc3e3c22eb5238d1c8330da53d4f9801fc2391f567
c1cncnc1
O=[N+;H0;D3:1](-[O-])-[c:2]1:[c:3](-[Cl;D1;H0:4]):[#7;a:5]:[c:6]:[#7;a:7]:[c:8]:1-[Cl;D1;H0:9]>>[Cl;D1;H0:4]-[c:3]1:[#7;a:5]:[c:6]:[#7;a:7]:[c:8](-[Cl;D1;H0:9]):[c:2]:1-[NH2;D1;+0:1]
null
[]
65
CELSIUS
null
null
Add iron powder (6.0 g) to a solution of 4,6 dichloro-2-methyl-5-nitro-pyrimidine (6.50 g, 31 mmol) in acetic acid (11 mL) and MeOH (50 mL). Heat the resulting mixture at 65° C. for 1 h. After cooling, to ambient temperature, filter the mixture through a pad of celite, and evaporate the filtrate to dryness under reduce...
10.6084/m9.figshare.5104873.v1
null
Nitro group
Primary amine
null
null
c1cncnc1
Other
[Fe].C(C)(=O)O.CO
65
null
Cc1nc(Cl)c([N+](=O)[O-])c(Cl)n1>[Fe].C(C)(=O)O.CO>Cc1nc(Cl)c(N)c(Cl)n1
ord_dataset-c3a75813d0b24864aa4f7cd526efd6aa
ord-ee748f942cea4117896b641bc673b6a5
Cc1cc(C)c(-c2cccc3c(Br)cc(C)nc23)c(C)c1.NCCN>>Cc1cc(C)c(-c2cccc3c(NCCN)cc(C)nc23)c(C)c1
BrC1=CC(=NC2=C(C=CC=C12)C1=C(C=C(C=C1C)C)C)C.C(CN)N>>NCCNC1=CC(=NC2=C(C=CC=C12)C1=C(C=C(C=C1C)C)C)C
Br[c:12]1[c:11]2[cH:10][cH:9][cH:8][c:7](-[c:6]3[c:4]([CH3:5])[cH:3][c:2]([CH3:1])[cH:24][c:22]3[CH3:23])[c:21]2[n:20][c:18]([CH3:19])[cH:17]1.[NH2:13][CH2:14][CH2:15][NH2:16]>>[CH3:1][c:2]1[cH:3][c:4]([CH3:5])[c:6](-[c:7]2[cH:8][cH:9][cH:10][c:11]3[c:12]([NH:13][CH2:14][CH2:15][NH2:16])[cH:17][c:18]([CH3:19])[n:20][c:...
Cc1cc(C)c(-c2cccc3c(Br)cc(C)nc23)c(C)c1.NCCN
Cc1cc(C)c(-c2cccc3c(NCCN)cc(C)nc23)c(C)c1
null
null
C(CO)O
Heteroatom Alkylation and Arylation
N-arylation (Buchwald-Hartwig/Ullmann-Goldberg)
45e8470a78418ade39424f40732aa5ecf6717a7e5d47830a67429c5970ebd551
71a04ae650defc5edd86a92f43c304e981a05f07ff76248da8d4155f3905a29d
c1ccc(-c2cccc3cccnc23)cc1
Br-[c;H0;D3;+0:1]1:[c:2]:[c:3](-[C;D1;H3:4]):[#7;a:5]:[c:6](:[c:7]):[c:8]:1:[c:9].[C:10]-[C:11]-[NH2;D1;+0:12]>>[C:10]-[C:11]-[NH;D2;+0:12]-[c;H0;D3;+0:1]1:[c:2]:[c:3](-[C;D1;H3:4]):[#7;a:5]:[c:6](:[c:7]):[c:8]:1:[c:9]
null
[]
null
null
4
HOUR
In a sealed tube, heat 4-bromo-2-methyl-8-(2,4,6-trimethyl-phenyl)-quinoline (100 mg, 0.29 mmol) at 140° C. in a mixture of ethylene glycol (1 mL) and ethylene diamine (0.3 mL). After 4 h, cool the reaction mixture and partition between saturated aqueous NaHCO3 and chloroform. Dry the combined organic extracts on Na2SO...
10.6084/m9.figshare.5104873.v1
null
Aromatic halide.Primary amine
Secondary amine
c1ccc2ncccc2c1
c1ccc2ncccc2c1
c1ccccc1.c1ccc2ncccc2c1
HBr
C(CO)O
null
4
Cc1cc(C)c(-c2cccc3c(Br)cc(C)nc23)c(C)c1.NCCN>C(CO)O>Cc1cc(C)c(-c2cccc3c(NCCN)cc(C)nc23)c(C)c1
ord_dataset-c3a75813d0b24864aa4f7cd526efd6aa
ord-f213b349498040b1b9d7ad3b03a50bd3
CNCCNc1cc(C)nc(Oc2c(C)cc(C)cc2C)c1C.COc1ccc(CC(=O)O)cc1OC>>COc1ccc(CC(=O)NCCNc2cc(C)nc(Oc3c(C)cc(C)cc3C)c2C)cc1OC
CC=1C(=NC(=CC1NCCNC)C)OC1=C(C=C(C=C1C)C)C.COC=1C=C(C=CC1OC)CC(=O)O.C(CCl)Cl.C=1C=CC2=C(C1)N=NN2O>>COC=1C=C(C=CC1OC)CC(=O)NCCNC1=C(C(=NC(=C1)C)OC1=C(C=C(C=C1C)C)C)C
C[NH:10][CH2:11][CH2:12][NH:13][c:14]1[cH:15][c:16]([CH3:17])[n:18][c:19]([O:20][c:21]2[c:22]([CH3:23])[cH:24][c:25]([CH3:26])[cH:27][c:28]2[CH3:29])[c:30]1[CH3:31].O[C:8]([CH2:7][c:6]1[cH:5][cH:4][c:3]([O:2][CH3:1])[c:33]([O:34][CH3:35])[cH:32]1)=[O:9]>>[CH3:1][O:2][c:3]1[cH:4][cH:5][c:6]([CH2:7][C:8](=[O:9])[NH:10][C...
CNCCNc1cc(C)nc(Oc2c(C)cc(C)cc2C)c1C.COc1ccc(CC(=O)O)cc1OC
COc1ccc(CC(=O)NCCNc2cc(C)nc(Oc3c(C)cc(C)cc3C)c2C)cc1OC
null
null
CN(C)C=O.CCOC(=O)C
Acylation
OtherReaction
5a5ff76e01d051a03a2c77088c884912413ce09f49ca50e186c0fb9c62ad0bd2
9b702924f2df230008ea1edd297d6a4305f6e78d7804dff7e838c4286e010bf9
O=C(Cc1ccccc1)NCCNc1ccnc(Oc2ccccc2)c1
C-[NH;D2;+0:1]-[C:2]-[C:3].O-[C;H0;D3;+0:4](=[O;D1;H0:5])-[C:6]-[c:7]>>[C:3]-[C:2]-[NH;D2;+0:1]-[C;H0;D3;+0:4](=[O;D1;H0:5])-[C:6]-[c:7]
null
[]
null
null
null
null
Stir a solution of [3,6-dimethyl-2-(2,4,6-trimethyl-phenoxy)-4-pyridyl][2-(methylamino)ethyl]amine (68 mg, 0.23 mmol), 3,4-dimethoxyphenylacetic acid (59 mg, 0.3 mmol), EDC (59 mg, 0.3 mmol) and HOBT (41 mg, 0.3 mmol) in DMF (1.0 mL) for 12 h. Dilute the reaction mixture with EtOAc (10 mL) and wash with saturated aq Na...
10.6084/m9.figshare.5104873.v1
null
Carboxylic acid.Secondary amine
Secondary amide
null
null
c1ccccc1.c1ccncc1.c1ccccc1
HO-
CN(C)C=O.CCOC(=O)C
null
null
CNCCNc1cc(C)nc(Oc2c(C)cc(C)cc2C)c1C.COc1ccc(CC(=O)O)cc1OC>CN(C)C=O.CCOC(=O)C>COc1ccc(CC(=O)NCCNc2cc(C)nc(Oc3c(C)cc(C)cc3C)c2C)cc1OC
ord_dataset-c3a75813d0b24864aa4f7cd526efd6aa
ord-6f046879ca3246f4b57f746bea94b86f
COc1ccc(CC(=O)NCCNc2cc(C)nc(Oc3c(C)cc(C)cc3C)c2C)cc1OC>>COc1ccc(CCNCCNc2cc(C)nc(Oc3c(C)cc(C)cc3C)c2C)cc1OC
COC=1C=C(C=CC1OC)CC(=O)NCCNC1=C(C(=NC(=C1)C)OC1=C(C=C(C=C1C)C)C)C>>COC=1C=C(C=CC1OC)CCNCCNC1=C(C(=NC(=C1)C)OC1=C(C=C(C=C1C)C)C)C
O=[C:8]([CH2:7][c:6]1[cH:5][cH:4][c:3]([O:2][CH3:1])[c:32]([O:33][CH3:34])[cH:31]1)[NH:9][CH2:10][CH2:11][NH:12][c:13]1[cH:14][c:15]([CH3:16])[n:17][c:18]([O:19][c:20]2[c:21]([CH3:22])[cH:23][c:24]([CH3:25])[cH:26][c:27]2[CH3:28])[c:29]1[CH3:30]>>[CH3:1][O:2][c:3]1[cH:4][cH:5][c:6]([CH2:7][CH2:8][NH:9][CH2:10][CH2:11][...
COc1ccc(CC(=O)NCCNc2cc(C)nc(Oc3c(C)cc(C)cc3C)c2C)cc1OC
COc1ccc(CCNCCNc2cc(C)nc(Oc3c(C)cc(C)cc3C)c2C)cc1OC
null
null
C(Cl)(Cl)Cl.CO.C1CCOC1
Reduction
Reduction of secondary amides to amines
85b757f1833edc9e5c6365ee6b904683f414e7b9a5f9bfcfd7addca401447058
ab40188eef2f825df7003af0ffae31d0ce53d126542122535627d3d354cbc9fe
c1ccc(CCNCCNc2ccnc(Oc3ccccc3)c2)cc1
O=[C;H0;D3;+0:1](-[#7:2]-[C:3])-[C:4]-[c:5]>>[C:3]-[#7:2]-[CH2;D2;+0:1]-[C:4]-[c:5]
null
[]
null
null
null
null
Add BH3 in THF (1 M solution, 0.3 mmol, 0.3 mL) to a solution of the crude 2-(3,4-dimethoxyphenyl)-N-(2-{[3,6-dimethyl-2-(2,4,6-trimethylphenoxy)(4-pyridyl)]amino}ethyl) acetamide in THF (2.0 mL) at ambient temperature. Heat the reaction mixture under reflux for 15 h, dilute with a solution of 10% aq HCV/MeOH (1:1, 2 m...
10.6084/m9.figshare.5104873.v1
null
Secondary amide
null
null
null
c1ccccc1.c1ccncc1.c1ccccc1
Other
C(Cl)(Cl)Cl.CO.C1CCOC1
null
null
COc1ccc(CC(=O)NCCNc2cc(C)nc(Oc3c(C)cc(C)cc3C)c2C)cc1OC>C(Cl)(Cl)Cl.CO.C1CCOC1>COc1ccc(CCNCCNc2cc(C)nc(Oc3c(C)cc(C)cc3C)c2C)cc1OC
ord_dataset-c3a75813d0b24864aa4f7cd526efd6aa
ord-1703578e8f0548f3b5fb59ecb4a819e6
CCOc1ccc(CCN)cc1OC.CN(C)[P+](On1nnc2ccccc21)(N(C)C)N(C)C.Cc1cc(C)c(Nc2cc(NCCN)nc(C)n2)c(C)c1>>CCOc1ccc(CC(=O)NCCNc2cc(Nc3c(C)cc(C)cc3C)nc(C)n2)cc1OC
NCCNC1=NC(=NC(=C1)NC1=C(C=C(C=C1C)C)C)C.C(C)OC1=C(C=C(CCN)C=C1)OC.C(C)(C)N(C(C)C)CC.F[P-](F)(F)(F)(F)F.N1(N=NC2=C1C=CC=C2)O[P+](N(C)C)(N(C)C)N(C)C>>C(C)OC1=C(C=C(C=C1)CC(=O)NCCNC1=NC(=NC(=C1)NC1=C(C=C(C=C1C)C)C)C)OC
N[CH2:9][CH2:8][c:7]1[cH:6][cH:5][c:4]([O:3][CH2:2][CH3:1])[c:33]([O:34][CH3:35])[cH:32]1.CN(C)[P+](N(C)C)(N(C)C)[O:10]n1nnc2ccccc21.[NH2:11][CH2:12][CH2:13][NH:14][c:15]1[cH:16][c:17]([NH:18][c:19]2[c:20]([CH3:21])[cH:22][c:23]([CH3:24])[cH:25][c:26]2[CH3:27])[n:28][c:29]([CH3:30])[n:31]1>>[CH3:1][CH2:2][O:3][c:4]1[cH...
CCOc1ccc(CCN)cc1OC.CN(C)[P+](On1nnc2ccccc21)(N(C)C)N(C)C.Cc1cc(C)c(Nc2cc(NCCN)nc(C)n2)c(C)c1
CCOc1ccc(CC(=O)NCCNc2cc(Nc3c(C)cc(C)cc3C)nc(C)n2)cc1OC
null
null
C(Cl)Cl
Acylation
OtherReaction
cfa0c8edd50211f798565f1f3ee293d20dceaf8bf7f85f12f401d7e690fe524c
bf4cc782380223a2c801d48a0a69f6e4dea018cf7baecf2e6477eb9dab060c74
O=C(Cc1ccccc1)NCCNc1cc(Nc2ccccc2)ncn1
C-N(-C)-[P+](-[O;H0;D2;+0:1]-n1:n:n:c2:c:c:c:c:c:2:1)(-N(-C)-C)-N(-C)-C.N-[CH2;D2;+0:2]-[C:3]-[c:4].[C:5]-[C:6]-[NH2;D1;+0:7]>>[C:5]-[C:6]-[NH;D2;+0:7]-[C;H0;D3;+0:2](=[O;H0;D1;+0:1])-[C:3]-[c:4]
null
[]
null
null
14
HOUR
To a solution of (2-aminoethyl){2-methyl-6-[(2,4,6-trimethylphenyl)amino]pyrimidin-4-yl}amine (0.36 g, 1.26 mmol), 4-ethoxy-3-methoxyphenethylamine (0.26 g, 1.26 mmol)) and N,N diisopropylethyl amine (0.24 ml, 1.38 mmol in CH2Cl2 (5 mL), add benzotriazol-1-yloxytris-(dimethylamino)phosphonium hexafluorophosphate (0.61 ...
10.6084/m9.figshare.5104873.v1
null
Primary amine.Primary amine.Tertiary amine.Tertiary amine.Tertiary amine
Secondary amide
c1ccc2[nH]nnc2c1
null
c1ccccc1.c1cncnc1.c1ccccc1
Other
C(Cl)Cl
null
14
CCOc1ccc(CCN)cc1OC.CN(C)[P+](On1nnc2ccccc21)(N(C)C)N(C)C.Cc1cc(C)c(Nc2cc(NCCN)nc(C)n2)c(C)c1>C(Cl)Cl>CCOc1ccc(CC(=O)NCCNc2cc(Nc3c(C)cc(C)cc3C)nc(C)n2)cc1OC
ord_dataset-c3a75813d0b24864aa4f7cd526efd6aa
ord-f2635e5060ee4ca2a9981737d112e6cd
CCOc1ccc(CC(=O)NCCNc2cc(Nc3c(C)cc(C)cc3C)nc(C)n2)cc1OC>>CCOc1ccc(CCNCCNc2cc(Nc3c(C)cc(C)cc3C)nc(C)n2)cc1OC
N(C)(C)CC.C(C)OC1=C(C=C(C=C1)CC(=O)NCCNC1=NC(=NC(=C1)NC1=C(C=C(C=C1C)C)C)C)OC.[AlH3]>>C(C)OC1=C(C=C(C=C1)CCNCCNC1=NC(=NC(=C1)NC1=C(C=C(C=C1C)C)C)C)OC
O=[C:9]([CH2:8][c:7]1[cH:6][cH:5][c:4]([O:3][CH2:2][CH3:1])[c:32]([O:33][CH3:34])[cH:31]1)[NH:10][CH2:11][CH2:12][NH:13][c:14]1[cH:15][c:16]([NH:17][c:18]2[c:19]([CH3:20])[cH:21][c:22]([CH3:23])[cH:24][c:25]2[CH3:26])[n:27][c:28]([CH3:29])[n:30]1>>[CH3:1][CH2:2][O:3][c:4]1[cH:5][cH:6][c:7]([CH2:8][CH2:9][NH:10][CH2:11]...
CCOc1ccc(CC(=O)NCCNc2cc(Nc3c(C)cc(C)cc3C)nc(C)n2)cc1OC
CCOc1ccc(CCNCCNc2cc(Nc3c(C)cc(C)cc3C)nc(C)n2)cc1OC
null
null
C1CCOC1
Reduction
Reduction of secondary amides to amines
85b757f1833edc9e5c6365ee6b904683f414e7b9a5f9bfcfd7addca401447058
ab40188eef2f825df7003af0ffae31d0ce53d126542122535627d3d354cbc9fe
c1ccc(CCNCCNc2cc(Nc3ccccc3)ncn2)cc1
O=[C;H0;D3;+0:1](-[#7:2]-[C:3])-[C:4]-[c:5]>>[C:3]-[#7:2]-[CH2;D2;+0:1]-[C:4]-[c:5]
null
[]
null
null
15
MINUTE
Heat a solution of 2-(4-ethoxy-3-methoxy-phenyl)-N-{2-[2-methyl-6-(2,4,6-trimethyl-phenylamino)-pyrimidin-4-ylamino]ethyl}-acetamide (0.324 g, 0.68 mmol) in THF (10 mL) with AlH3.NMe2Et (14 mL, 6.78 mmol) to reflux for 14 h. Cool the resulting mixture to ambient temperature, quench with Na2CO3.10H2O (1.0 g) and stir at...
10.6084/m9.figshare.5104873.v1
null
Secondary amide
null
null
null
c1ccccc1.c1cncnc1.c1ccccc1
Other
C1CCOC1
null
0.25
CCOc1ccc(CC(=O)NCCNc2cc(Nc3c(C)cc(C)cc3C)nc(C)n2)cc1OC>C1CCOC1>CCOc1ccc(CCNCCNc2cc(Nc3c(C)cc(C)cc3C)nc(C)n2)cc1OC
ord_dataset-c3a75813d0b24864aa4f7cd526efd6aa
ord-eb6b609ad68141eda11b3cb0a92c7fe2
C1CNCCN1.COCOc1ccc(C2(C)COc3cc(OCOC)ccc3C2CCCCCCCCCOS(=O)(=O)c2ccc(C)cc2)cc1>>COCOc1ccc(C2(C)COc3cc(OCOC)ccc3C2CCCCCCCCCN2CCNCC2)cc1
CC1=CC=C(C=C1)S(=O)(=O)OCCCCCCCCCC1C(COC2=CC(=CC=C12)OCOC)(C)C1=CC=C(C=C1)OCOC.N1CCNCC1.[OH-].[Na+]>>COCOC1=CC=C2C(C(COC2=C1)(C)C1=CC=C(C=C1)OCOC)CCCCCCCCCN1CCNCC1
[NH:33]1[CH2:34][CH2:35][NH:36][CH2:37][CH2:38]1.Cc1ccc(S(=O)(=O)O[CH2:32][CH2:31][CH2:30][CH2:29][CH2:28][CH2:27][CH2:26][CH2:25][CH2:24][CH:23]2[C:9]([c:8]3[cH:7][cH:6][c:5]([O:4][CH2:3][O:2][CH3:1])[cH:40][cH:39]3)([CH3:10])[CH2:11][O:12][c:13]3[cH:14][c:15]([O:16][CH2:17][O:18][CH3:19])[cH:20][cH:21][c:22]32)cc1>>[...
C1CNCCN1.COCOc1ccc(C2(C)COc3cc(OCOC)ccc3C2CCCCCCCCCOS(=O)(=O)c2ccc(C)cc2)cc1
COCOc1ccc(C2(C)COc3cc(OCOC)ccc3C2CCCCCCCCCN2CCNCC2)cc1
null
null
O1CCOCC1
Heteroatom Alkylation and Arylation
OtherReaction
3012dc60c14310d621abae8cd9ce102b1b72363f5aa91786df5d66245515072b
71b4ac4449ece5e0df64e56caf0f1cbac76e83f802a92104cfb6c6c861b6a71c
c1ccc(C2COc3ccccc3C2CCCCCCCCCN2CCNCC2)cc1
C-c1:c:c:c(-S(=O)(=O)-O-[CH2;D2;+0:1]-[C:2]-[C:3]):c:c:1.[#7:4]1-[C:5]-[C:6]-[NH;D2;+0:7]-[C:8]-[C:9]-1>>[C:3]-[C:2]-[CH2;D2;+0:1]-[N;H0;D3;+0:7]1-[C:6]-[C:5]-[#7:4]-[C:9]-[C:8]-1
81
[{"value": 81.0, "product": "COCOC1=CC=C2C(C(COC2=C1)(C)C1=CC=C(C=C1)OCOC)CCCCCCCCCN1CCNCC1", "details": "PERCENTYIELD", "is_desired": false}]
null
null
null
null
9-{7-(Methoxymethoxy)-3-[4-(methoxymethoxy)phenyl]-3-methylchroman-4-yl}nonyl 4-methylbenzenesulfonate (540 mg, 0.843 mmol) and piperazine (2.2 g, 25.5 mmol) were dissolved in dioxane and then the mixture was refluxed for 2 hours. The mixture was cooled down to room temperature, basified to pH 13 using 5N-NaOH, and the...
10.6084/m9.figshare.5104873.v1
null
Tosylate.Secondary amine
Tertiary amine
C1CNCCN1.c1ccccc1
C1C[NH]CCN1
c1ccccc1.c1ccc2c(c1)CCCO2.C1C[NH]CCN1
TsOH.HO-
O1CCOCC1
null
null
C1CNCCN1.COCOc1ccc(C2(C)COc3cc(OCOC)ccc3C2CCCCCCCCCOS(=O)(=O)c2ccc(C)cc2)cc1>O1CCOCC1>COCOc1ccc(C2(C)COc3cc(OCOC)ccc3C2CCCCCCCCCN2CCNCC2)cc1
ord_dataset-c3a75813d0b24864aa4f7cd526efd6aa
ord-b65e146e05a14a1a8dfc125bbb52583a
COCOc1ccc(C2(C)COc3cc(OCOC)ccc3C2CCCCCCCCCN2CCNCC2)cc1.Cc1ccc(S(=O)(=O)OCCCC(F)(F)C(F)(F)F)cc1>>COCOc1ccc(C2(C)COc3cc(OCOC)ccc3C2CCCCCCCCCN2CCN(CCCC(F)(F)C(F)(F)F)CC2)cc1
COCOC1=CC=C2C(C(COC2=C1)(C)C1=CC=C(C=C1)OCOC)CCCCCCCCCN1CCNCC1.C(=O)([O-])[O-].[K+].[K+].FC(CCCOS(=O)(=O)C1=CC=C(C=C1)C)(C(F)(F)F)F>>COCOC1=CC=C2C(C(COC2=C1)(C)C1=CC=C(C=C1)OCOC)CCCCCCCCCN1CCN(CC1)CCCC(C(F)(F)F)(F)F
[CH3:1][O:2][CH2:3][O:4][c:5]1[cH:6][cH:7][c:8]([C:9]2([CH3:10])[CH2:11][O:12][c:13]3[cH:14][c:15]([O:16][CH2:17][O:18][CH3:19])[cH:20][cH:21][c:22]3[CH:23]2[CH2:24][CH2:25][CH2:26][CH2:27][CH2:28][CH2:29][CH2:30][CH2:31][CH2:32][N:33]2[CH2:34][CH2:35][NH:36][CH2:47][CH2:48]2)[cH:49][cH:50]1.Cc1ccc(S(=O)(=O)O[CH2:37][C...
COCOc1ccc(C2(C)COc3cc(OCOC)ccc3C2CCCCCCCCCN2CCNCC2)cc1.Cc1ccc(S(=O)(=O)OCCCC(F)(F)C(F)(F)F)cc1
COCOc1ccc(C2(C)COc3cc(OCOC)ccc3C2CCCCCCCCCN2CCN(CCCC(F)(F)C(F)(F)F)CC2)cc1
null
null
O
Heteroatom Alkylation and Arylation
OtherReaction
9d271698b0c48162ad18ec9c479844bc505434e9294038bc9af6d1140123fb4f
71b4ac4449ece5e0df64e56caf0f1cbac76e83f802a92104cfb6c6c861b6a71c
c1ccc(C2COc3ccccc3C2CCCCCCCCCN2CCNCC2)cc1
C-c1:c:c:c(-S(=O)(=O)-O-[CH2;D2;+0:1]-[C:2]-[C:3]):c:c:1.[#7:4]1-[C:5]-[C:6]-[NH;D2;+0:7]-[C:8]-[C:9]-1>>[C:3]-[C:2]-[CH2;D2;+0:1]-[N;H0;D3;+0:7]1-[C:6]-[C:5]-[#7:4]-[C:9]-[C:8]-1
48.6
[{"value": 48.0, "product": "COCOC1=CC=C2C(C(COC2=C1)(C)C1=CC=C(C=C1)OCOC)CCCCCCCCCN1CCN(CC1)CCCC(C(F)(F)F)(F)F", "details": "PERCENTYIELD", "is_desired": false}, {"value": 48.6, "product": "COCOC1=CC=C2C(C(COC2=C1)(C)C1=CC=C(C=C1)OCOC)CCCCCCCCCN1CCN(CC1)CCCC(C(F)(F)F)(F)F", "details": "CALCULATEDPERCENTYIELD", "is_des...
null
null
null
null
7-(Methoxymethoxy)-3-(4-methoxymethoxyphenyl)-4-(9-piperazinylnonyl)-3-methylchroman (380 mg, 0.685 mmol), K2CO3 (190 mg, 1.375 mmol) and 4,4,5,5,5-pentafluoropentyl-4-methylbenzenesulfonate (460 mg, 1.384 mmol) were refluxed under acetone for 15 hours. After the mixture was cooled down to room temperature, water was a...
10.6084/m9.figshare.5104873.v1
null
Tosylate.Secondary amine
Tertiary amine
C1C[NH]CCN1.c1ccccc1
C1C[NH]CC[NH]1
c1ccccc1.c1ccc2c(c1)CCCO2.C1C[NH]CC[NH]1
TsOH.HO-
O
null
null
COCOc1ccc(C2(C)COc3cc(OCOC)ccc3C2CCCCCCCCCN2CCNCC2)cc1.Cc1ccc(S(=O)(=O)OCCCC(F)(F)C(F)(F)F)cc1>O>COCOc1ccc(C2(C)COc3cc(OCOC)ccc3C2CCCCCCCCCN2CCN(CCCC(F)(F)C(F)(F)F)CC2)cc1
ord_dataset-c3a75813d0b24864aa4f7cd526efd6aa
ord-502f9fd81a9f4c6b8b752215ee2a5228
COCOc1ccc(C2(C)COc3cc(OCOC)ccc3C2CCCCCCCCCN2CCN(CCCC(F)(F)C(F)(F)F)CC2)cc1>>CC1(c2ccc(O)cc2)COc2cc(O)ccc2C1CCCCCCCCCN1CCN(CCCC(F)(F)C(F)(F)F)CC1
COCOC1=CC=C2C(C(COC2=C1)(C)C1=CC=C(C=C1)OCOC)CCCCCCCCCN1CCN(CC1)CCCC(C(F)(F)F)(F)F>>OC1=CC=C2C(C(COC2=C1)(C)C1=CC=C(C=C1)O)CCCCCCCCCN1CCN(CC1)CCCC(C(F)(F)F)(F)F
COC[O:7][c:6]1[cH:5][cH:4][c:3]([C:2]2([CH3:1])[CH2:10][O:11][c:12]3[cH:13][c:14]([O:15]COC)[cH:16][cH:17][c:18]3[CH:19]2[CH2:20][CH2:21][CH2:22][CH2:23][CH2:24][CH2:25][CH2:26][CH2:27][CH2:28][N:29]2[CH2:30][CH2:31][N:32]([CH2:33][CH2:34][CH2:35][C:36]([F:37])([F:38])[C:39]([F:40])([F:41])[F:42])[CH2:43][CH2:44]2)[cH:...
COCOc1ccc(C2(C)COc3cc(OCOC)ccc3C2CCCCCCCCCN2CCN(CCCC(F)(F)C(F)(F)F)CC2)cc1
CC1(c2ccc(O)cc2)COc2cc(O)ccc2C1CCCCCCCCCN1CCN(CCCC(F)(F)C(F)(F)F)CC1
null
null
Cl.CO
Reduction
OtherReaction
ca434a15af04bd105d14de328e5decdefa40fa872c8bf2d8a06e38dd9d786610
9290d799ef03b273f5a33508bad8fca1206e009b9df18f946351c38e7647a04c
c1ccc(C2COc3ccccc3C2CCCCCCCCCN2CCNCC2)cc1
C-O-C-[O;H0;D2;+0:1]-[c:2](:[c:3]):[c:4].C-O-C-[O;H0;D2;+0:5]-[c:6](:[c:7]):[c:8]>>[OH;D1;+0:1]-[c:2](:[c:3]):[c:4].[OH;D1;+0:5]-[c:6](:[c:7]):[c:8]
88
[{"value": 88.0, "product": "OC1=CC=C2C(C(COC2=C1)(C)C1=CC=C(C=C1)O)CCCCCCCCCN1CCN(CC1)CCCC(C(F)(F)F)(F)F", "details": "PERCENTYIELD", "is_desired": false}]
50
CELSIUS
1
HOUR
7-(Methoxymethoxy)-3-(4-methoxymethoxyphenyl)-4-{9-[4-(4,4,5,5,5-pentafluoropentyl)piperazinyl]nonyl}-3-methylchroman (210 mg, 0.294 mmol) was dissolved in 2N-HCl solution in methanol, and the mixture was stirred at 50° C. for 1 hour. The mixture was cooled down to room temperature, adjusted to pH=9 using aqueous NaHCO...
10.6084/m9.figshare.5104873.v1
null
Ether.Ether.Ether.Ether
Aromatic alcohol.Aromatic alcohol
null
null
c1ccccc1.c1ccc2c(c1)CCCO2.C1C[NH]CC[NH]1
HO-
Cl.CO
50
1
COCOc1ccc(C2(C)COc3cc(OCOC)ccc3C2CCCCCCCCCN2CCN(CCCC(F)(F)C(F)(F)F)CC2)cc1>Cl.CO>CC1(c2ccc(O)cc2)COc2cc(O)ccc2C1CCCCCCCCCN1CCN(CCCC(F)(F)C(F)(F)F)CC1
ord_dataset-c3a75813d0b24864aa4f7cd526efd6aa
ord-590bd6cc73ae45b885ec4d481e80acdd
Cc1cc(C(C)(C)C)cc(C(C)(C)C)c1.O=C1CCC(=O)N1Br>>CC(C)(C)c1cc(CBr)cc(C(C)(C)C)c1
C(C)(C)(C)C=1C=C(C=C(C1)C(C)(C)C)C.BrN1C(CCC1=O)=O>>C(C)(C)(C)C=1C=C(C=C(C1)C(C)(C)C)CBr
[CH3:1][C:2]([CH3:3])([CH3:4])[c:5]1[cH:6][c:7]([CH3:8])[cH:10][c:11]([C:12]([CH3:13])([CH3:14])[CH3:15])[cH:16]1.O=C1CCC(=O)N1[Br:9]>>[CH3:1][C:2]([CH3:3])([CH3:4])[c:5]1[cH:6][c:7]([CH2:8][Br:9])[cH:10][c:11]([C:12]([CH3:13])([CH3:14])[CH3:15])[cH:16]1
Cc1cc(C(C)(C)C)cc(C(C)(C)C)c1.O=C1CCC(=O)N1Br
CC(C)(C)c1cc(CBr)cc(C(C)(C)C)c1
null
CC(C)(C#N)N=NC(C)(C)C#N
C(Cl)(Cl)(Cl)Cl
Functional Group Interconversion
Wohl-Ziegler bromination benzyl primary
45c0aca0d63a96f0092e6dded9c888827eaf6379dac179e1cefc99293896300a
08f5e7e34d3f321cce3e85421b38226d6240cca0939494ae61032d4f8405cf22
c1ccccc1
O=C1-C-C-C(=O)-N-1-[Br;H0;D1;+0:1].[CH3;D1;+0:2]-[c:3](:[c:4]):[c:5]>>[Br;H0;D1;+0:1]-[CH2;D2;+0:2]-[c:3](:[c:4]):[c:5]
61.2
[{"value": 61.0, "product": "C(C)(C)(C)C=1C=C(C=C(C1)C(C)(C)C)CBr", "details": "PERCENTYIELD", "is_desired": false}, {"value": 61.2, "product": "C(C)(C)(C)C=1C=C(C=C(C1)C(C)(C)C)CBr", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
5
HOUR
3,5-Bis(t-butyl)-1-methylbenzene (200 mg, 0.98 mmol) was dissolved in carbon tetrachloride (4 ml), and then N-bromosuccinimide (192 mg, 1.08 mmol) and AIBN (α,α′-azabisisobutyronitrile) (2 mg) were added thereto. The mixture was heated under reflux and stirred for 5 hours. The filtrate obtained from the filtration of t...
10.6084/m9.figshare.5104873.v1
null
Tertiary amide.Tertiary amide
Primary halide
C1CCNC1
null
c1ccccc1
HO-
CC(C)(C#N)N=NC(C)(C)C#N.C(Cl)(Cl)(Cl)Cl
null
5
Cc1cc(C(C)(C)C)cc(C(C)(C)C)c1.O=C1CCC(=O)N1Br>CC(C)(C#N)N=NC(C)(C)C#N.C(Cl)(Cl)(Cl)Cl>CC(C)(C)c1cc(CBr)cc(C(C)(C)C)c1
ord_dataset-c3a75813d0b24864aa4f7cd526efd6aa
ord-0c4bcea7fa9f4f4fbae5be5b7622ef17
CC(C)(C)OC(=O)N1CCNCC1.CC(C)(C)c1cc(CBr)cc(C(C)(C)C)c1>>CC(C)(C)OC(=O)N1CCN(Cc2cc(C(C)(C)C)cc(C(C)(C)C)c2)CC1
C(C)(C)(C)C=1C=C(C=C(C1)C(C)(C)C)CBr.N1(CCNCC1)C(=O)OC(C)(C)C.C([O-])([O-])=O.[K+].[K+]>>C(C)(C)(C)C=1C=C(C=C(C1)C(C)(C)C)CN1CCN(CC1)C(=O)OC(C)(C)C
[CH3:1][C:2]([CH3:3])([CH3:4])[O:5][C:6](=[O:7])[N:8]1[CH2:9][CH2:10][NH:11][CH2:27][CH2:28]1.Br[CH2:12][c:13]1[cH:14][c:15]([C:16]([CH3:17])([CH3:18])[CH3:19])[cH:20][c:21]([C:22]([CH3:23])([CH3:24])[CH3:25])[cH:26]1>>[CH3:1][C:2]([CH3:3])([CH3:4])[O:5][C:6](=[O:7])[N:8]1[CH2:9][CH2:10][N:11]([CH2:12][c:13]2[cH:14][c:...
CC(C)(C)OC(=O)N1CCNCC1.CC(C)(C)c1cc(CBr)cc(C(C)(C)C)c1
CC(C)(C)OC(=O)N1CCN(Cc2cc(C(C)(C)C)cc(C(C)(C)C)c2)CC1
null
null
CC(=O)C.CN(C)C=O
Heteroatom Alkylation and Arylation
N-alkylation of secondary amines with alkyl halides
b703623ddc3b029d4716c15f5414f41773434bcc7e3f3853faf62273596bed77
523d37155b42c8dc851abeddadebb241cdd90bdf649ba750c35e13c8c752d7b0
c1ccc(CN2CCNCC2)cc1
Br-[CH2;D2;+0:1]-[c:2](:[c:3]):[c:4].[#7:5]1-[C:6]-[C:7]-[NH;D2;+0:8]-[C:9]-[C:10]-1>>[c:3]:[c:2](-[CH2;D2;+0:1]-[N;H0;D3;+0:8]1-[C:9]-[C:10]-[#7:5]-[C:6]-[C:7]-1):[c:4]
56.1
[{"value": 56.0, "product": "C(C)(C)(C)C=1C=C(C=C(C1)C(C)(C)C)CN1CCN(CC1)C(=O)OC(C)(C)C", "details": "PERCENTYIELD", "is_desired": false}, {"value": 56.1, "product": "C(C)(C)(C)C=1C=C(C=C(C1)C(C)(C)C)CN1CCN(CC1)C(=O)OC(C)(C)C", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
8
HOUR
3,5-Bis(t-butyl)-1-(bromomethyl)benzene (170 mg, 0.60 mmol), t-butyl piperazine carboxylate (102 mg, 0.55 mmol) and potassium carbonate (151 mg, 1.10 mmol) were dissolved in a solvent mixture of acetone (2 ml) and DMF (0.2 ml), and the mixture was stirred overnight while heated under reflux. The reaction mixture was ex...
10.6084/m9.figshare.5104873.v1
null
Primary halide.Secondary amine
Tertiary amine
C1C[NH]CCN1
C1C[NH]CC[NH]1
C1C[NH]CC[NH]1.c1ccccc1
HBr
CC(=O)C.CN(C)C=O
null
8
CC(C)(C)OC(=O)N1CCNCC1.CC(C)(C)c1cc(CBr)cc(C(C)(C)C)c1>CC(=O)C.CN(C)C=O>CC(C)(C)OC(=O)N1CCN(Cc2cc(C(C)(C)C)cc(C(C)(C)C)c2)CC1
ord_dataset-c3a75813d0b24864aa4f7cd526efd6aa
ord-4b404b72e8764ac39f42611c05e23403
CC(C)(C)c1cc(CN2CCNCC2)cc(C(C)(C)C)c1.COCOc1ccc(C2(C)COc3cc(OCOC)ccc3C2c2ccc(OCCCl)cc2)cc1>>COCOc1ccc(C2(C)COc3cc(OCOC)ccc3C2c2ccc(OCCN3CCN(Cc4cc(C(C)(C)C)cc(C(C)(C)C)c4)CC3)cc2)cc1
CCCCCC.ClCCOC1=CC=C(C=C1)C1C(COC2=CC(=CC=C12)OCOC)(C)C1=CC=C(C=C1)OCOC.C(C)(C)(C)C=1C=C(C=C(C1)C(C)(C)C)CN1CCNCC1.C([O-])([O-])=O.[K+].[K+]>>C(C)(C)(C)C=1C=C(C=C(C1)C(C)(C)C)CN1CCN(CC1)CCOC1=CC=C(C=C1)C1C(COC2=CC(=CC=C12)OCOC)(C)C1=CC=C(C=C1)OCOC
[NH:31]1[CH2:32][CH2:33][N:34]([CH2:35][c:36]2[cH:37][c:38]([C:39]([CH3:40])([CH3:41])[CH3:42])[cH:43][c:44]([C:45]([CH3:46])([CH3:47])[CH3:48])[cH:49]2)[CH2:50][CH2:51]1.Cl[CH2:30][CH2:29][O:28][c:27]1[cH:26][cH:25][c:24]([CH:23]2[C:9]([c:8]3[cH:7][cH:6][c:5]([O:4][CH2:3][O:2][CH3:1])[cH:55][cH:54]3)([CH3:10])[CH2:11]...
CC(C)(C)c1cc(CN2CCNCC2)cc(C(C)(C)C)c1.COCOc1ccc(C2(C)COc3cc(OCOC)ccc3C2c2ccc(OCCCl)cc2)cc1
COCOc1ccc(C2(C)COc3cc(OCOC)ccc3C2c2ccc(OCCN3CCN(Cc4cc(C(C)(C)C)cc(C(C)(C)C)c4)CC3)cc2)cc1
null
[I-].C(CCC)[N+](CCCC)(CCCC)CCCC
CC(=O)C.CN(C)C=O.C(C)(=O)OCC
Heteroatom Alkylation and Arylation
N-alkylation of secondary amines with alkyl halides
bad6b7d8e43c3debef0c262d60564e43415b41bcee72e526419c8c16be18fec1
523d37155b42c8dc851abeddadebb241cdd90bdf649ba750c35e13c8c752d7b0
c1ccc(CN2CCN(CCOc3ccc(C4c5ccccc5OCC4c4ccccc4)cc3)CC2)cc1
Cl-[CH2;D2;+0:1]-[C:2]-[#8:3].[#7:4]1-[C:5]-[C:6]-[NH;D2;+0:7]-[C:8]-[C:9]-1>>[#8:3]-[C:2]-[CH2;D2;+0:1]-[N;H0;D3;+0:7]1-[C:6]-[C:5]-[#7:4]-[C:9]-[C:8]-1
51
[{"value": 51.0, "product": "C(C)(C)(C)C=1C=C(C=C(C1)C(C)(C)C)CN1CCN(CC1)CCOC1=CC=C(C=C1)C1C(COC2=CC(=CC=C12)OCOC)(C)C1=CC=C(C=C1)OCOC", "details": "PERCENTYIELD", "is_desired": false}, {"value": 50.7, "product": "C(C)(C)(C)C=1C=C(C=C(C1)C(C)(C)C)CN1CCN(CC1)CCOC1=CC=C(C=C1)C1C(COC2=CC(=CC=C12)OCOC)(C)C1=CC=C(C=C1)OCOC"...
null
null
null
null
(3RS,4SR)-4-[4-(2-Chloroethoxy)phenyl]-7-(methoxymethoxy)-3-[4-(methoxymethoxy)phenyl]-3-methylchroman (210 mg, 0.42 mmol) and {(3,5-bis(t-butyl)phenyl]methyl}piperazine (243 mg, 0.84 mmol) were dissolved in a solvent mixture of acetone (4 ml) and DMF (0.4 ml). To the mixture potassium carbonate (116 mg, 0.84 mmol) and...
10.6084/m9.figshare.5104873.v1
null
Primary halide.Secondary amine
Tertiary amine
C1CNCC[NH]1
C1C[NH]CC[NH]1
c1ccccc1.c1ccc2c(c1)CCCO2.c1ccccc1.C1C[NH]CC[NH]1.c1ccccc1
HCl
[I-].C(CCC)[N+](CCCC)(CCCC)CCCC.CC(=O)C.CN(C)C=O.C(C)(=O)OCC
null
null
CC(C)(C)c1cc(CN2CCNCC2)cc(C(C)(C)C)c1.COCOc1ccc(C2(C)COc3cc(OCOC)ccc3C2c2ccc(OCCCl)cc2)cc1>[I-].C(CCC)[N+](CCCC)(CCCC)CCCC.CC(=O)C.CN(C)C=O.C(C)(=O)OCC>COCOc1ccc(C2(C)COc3cc(OCOC)ccc3C2c2ccc(OCCN3CCN(Cc4cc(C(C)(C)C)cc(C(C)(C)C)c4)CC3)cc2)cc1
ord_dataset-c3a75813d0b24864aa4f7cd526efd6aa
ord-9084cee2c4444cc081748c35eeb32eb2
COCOc1ccc(C2(C)COc3cc(OCOC)ccc3C2c2ccc(OCCN3CCN(Cc4cc(C(C)(C)C)cc(C(C)(C)C)c4)CC3)cc2)cc1>>CC(C)(C)c1cc(CN2CCN(CCOc3ccc(C4c5ccc(O)cc5OCC4(C)c4ccc(O)cc4)cc3)CC2)cc(C(C)(C)C)c1
C(C)(C)(C)C=1C=C(C=C(C1)C(C)(C)C)CN1CCN(CC1)CCOC1=CC=C(C=C1)C1C(COC2=CC(=CC=C12)OCOC)(C)C1=CC=C(C=C1)OCOC.Cl.C([O-])(O)=O.[Na+]>>C(C)(C)(C)C=1C=C(C=C(C1)C(C)(C)C)CN1CCN(CC1)CCOC1=CC=C(C=C1)C1C(COC2=CC(=CC=C12)O)(C)C1=CC=C(C=C1)O
COC[O:25][c:24]1[cH:23][cH:22][c:21]2[c:27]([cH:26]1)[O:28][CH2:29][C:30]([CH3:31])([c:32]1[cH:33][cH:34][c:35]([O:36]COC)[cH:37][cH:38]1)[CH:20]2[c:19]1[cH:18][cH:17][c:16]([O:15][CH2:14][CH2:13][N:12]2[CH2:11][CH2:10][N:9]([CH2:8][c:7]3[cH:6][c:5]([C:2]([CH3:1])([CH3:3])[CH3:4])[cH:49][c:44]([C:45]([CH3:46])([CH3:47]...
COCOc1ccc(C2(C)COc3cc(OCOC)ccc3C2c2ccc(OCCN3CCN(Cc4cc(C(C)(C)C)cc(C(C)(C)C)c4)CC3)cc2)cc1
CC(C)(C)c1cc(CN2CCN(CCOc3ccc(C4c5ccc(O)cc5OCC4(C)c4ccc(O)cc4)cc3)CC2)cc(C(C)(C)C)c1
null
null
ClCCl.CO
Reduction
OtherReaction
ca434a15af04bd105d14de328e5decdefa40fa872c8bf2d8a06e38dd9d786610
9290d799ef03b273f5a33508bad8fca1206e009b9df18f946351c38e7647a04c
c1ccc(CN2CCN(CCOc3ccc(C4c5ccccc5OCC4c4ccccc4)cc3)CC2)cc1
C-O-C-[O;H0;D2;+0:1]-[c:2](:[c:3]):[c:4].C-O-C-[O;H0;D2;+0:5]-[c:6](:[c:7]):[c:8]>>[OH;D1;+0:1]-[c:2](:[c:3]):[c:4].[OH;D1;+0:5]-[c:6](:[c:7]):[c:8]
54
[{"value": 54.0, "product": "C(C)(C)(C)C=1C=C(C=C(C1)C(C)(C)C)CN1CCN(CC1)CCOC1=CC=C(C=C1)C1C(COC2=CC(=CC=C12)O)(C)C1=CC=C(C=C1)O", "details": "PERCENTYIELD", "is_desired": false}, {"value": 53.9, "product": "C(C)(C)(C)C=1C=C(C=C(C1)C(C)(C)C)CN1CCN(CC1)CCOC1=CC=C(C=C1)C1C(COC2=CC(=CC=C12)O)(C)C1=CC=C(C=C1)O", "details":...
null
null
2
HOUR
(3RS,4SR)-4-{4-{2-{4-{[3,5-Bis(t-butyl)phenyl]methyl}piperazinyl}ethoxy}phenyl}-7-(methoxymethoxy)-3-[4-(methoxymethoxy)phenyl]-3-methylchroman (150 mg, 0.21 mmol) was dissolved in methanol (1.5 ml), 6N-HCl (2 ml) was added portionwise thereto, and the mixture was stirred at 50–60° C. for 2 hours. The reaction solution...
10.6084/m9.figshare.5104873.v1
null
Ether.Ether.Ether.Ether
Aromatic alcohol.Aromatic alcohol
null
null
c1ccccc1.C1C[NH]CC[NH]1.c1ccccc1.c1ccc2c(c1)CCCO2.c1ccccc1
HO-
ClCCl.CO
null
2
COCOc1ccc(C2(C)COc3cc(OCOC)ccc3C2c2ccc(OCCN3CCN(Cc4cc(C(C)(C)C)cc(C(C)(C)C)c4)CC3)cc2)cc1>ClCCl.CO>CC(C)(C)c1cc(CN2CCN(CCOc3ccc(C4c5ccc(O)cc5OCC4(C)c4ccc(O)cc4)cc3)CC2)cc(C(C)(C)C)c1
ord_dataset-c3a75813d0b24864aa4f7cd526efd6aa
ord-088a750a1a0243b2a737763c3b29f920
COc1ccc(C2(C)COc3cc(OC)ccc3C2CCCCCO)cc1.Cc1ccc(S(=O)(=O)Cl)cc1>>COc1ccc(C2(C)COc3cc(OC)ccc3C2CCCCCOS(=O)(=O)c2ccc(C)cc2)cc1
OCCCCCC1C(COC2=CC(=CC=C12)OC)(C)C1=CC=C(C=C1)OC.C1(=CC=C(C=C1)S(=O)(=O)Cl)C.O>>COC1=CC=C2C(C(COC2=C1)(C)C1=CC=C(C=C1)OC)CCCCCOS(=O)(=O)C1=CC=C(C=C1)C
[CH3:1][O:2][c:3]1[cH:4][cH:5][c:6]([C:7]2([CH3:8])[CH2:9][O:10][c:11]3[cH:12][c:13]([O:14][CH3:15])[cH:16][cH:17][c:18]3[CH:19]2[CH2:20][CH2:21][CH2:22][CH2:23][CH2:24][OH:25])[cH:36][cH:37]1.Cl[S:26](=[O:27])(=[O:28])[c:29]1[cH:30][cH:31][c:32]([CH3:33])[cH:34][cH:35]1>>[CH3:1][O:2][c:3]1[cH:4][cH:5][c:6]([C:7]2([CH3...
COc1ccc(C2(C)COc3cc(OC)ccc3C2CCCCCO)cc1.Cc1ccc(S(=O)(=O)Cl)cc1
COc1ccc(C2(C)COc3cc(OC)ccc3C2CCCCCOS(=O)(=O)c2ccc(C)cc2)cc1
null
null
N1=CC=CC=C1.ClCCl
Acylation
Formation of Sulfonic Esters
d05d91207659f8fa672c205a316a670adfe2b92492fc9adad2ee3f241e574fb9
a7748b0f3b0eba3868d0cf03ae67721db046202accaaea9cadb4edbc96ec8768
O=S(=O)(OCCCCCC1c2ccccc2OCC1c1ccccc1)c1ccccc1
Cl-[S;H0;D4;+0:1](=[O;D1;H0:2])(=[O;D1;H0:3])-[c:4](:[c:5]):[c:6].[C:7]-[C:8]-[OH;D1;+0:9]>>[C:7]-[C:8]-[O;H0;D2;+0:9]-[S;H0;D4;+0:1](=[O;D1;H0:2])(=[O;D1;H0:3])-[c:4](:[c:5]):[c:6]
53
[{"value": 53.0, "product": "COC1=CC=C2C(C(COC2=C1)(C)C1=CC=C(C=C1)OC)CCCCCOS(=O)(=O)C1=CC=C(C=C1)C", "details": "PERCENTYIELD", "is_desired": false}, {"value": 50.0, "product": "COC1=CC=C2C(C(COC2=C1)(C)C1=CC=C(C=C1)OC)CCCCCOS(=O)(=O)C1=CC=C(C=C1)C", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
3
HOUR
(3RS,4RS)-4-(5-Hydroxypentyl)-7-methoxy-3-(4-methoxyphenyl)-3-methylchroman (430 mg, 1.2 mmol) was dissolved in a solvent mixture of pyridine (12 ml) and dichloromethane (4 ml), which was then cooled down to 0° C. p-Toluenesulfonylchloride (460 mg, 2.3 mmol) was added dropwise thereto, and the mixture was stirred at ro...
10.6084/m9.figshare.5104873.v1
null
Tosylate.Primary alcohol.Sulfonyl halide
Tosylate
null
null
c1ccccc1.c1ccc2c(c1)CCCO2.c1ccccc1
HCl
N1=CC=CC=C1.ClCCl
null
3
COc1ccc(C2(C)COc3cc(OC)ccc3C2CCCCCO)cc1.Cc1ccc(S(=O)(=O)Cl)cc1>N1=CC=CC=C1.ClCCl>COc1ccc(C2(C)COc3cc(OC)ccc3C2CCCCCOS(=O)(=O)c2ccc(C)cc2)cc1