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
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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-018fd0e1351f4fd09b20fcddd97b4c7a
ord-cb6871243aa046c0acd17a0fc444cdcb
C=C(C)CCl.CCCCCCCCCCCCCCO.O=C(OO)c1cccc(Cl)c1>>CCCCCCCCCCCCCCOCC1(C)CO1
C(CCCCCCCCCCCCC)O.[H-].[Na+].C(C(C)=C)Cl.ClC1=CC(=CC=C1)C(=O)OO>>O1CC1(COCCCCCCCCCCCCCC)C
Cl[CH2:16][C:17]([CH3:18])=[CH2:19].[CH3:1][CH2:2][CH2:3][CH2:4][CH2:5][CH2:6][CH2:7][CH2:8][CH2:9][CH2:10][CH2:11][CH2:12][CH2:13][CH2:14][OH:15].O=C(O[OH:20])c1cccc(Cl)c1>>[CH3:1][CH2:2][CH2:3][CH2:4][CH2:5][CH2:6][CH2:7][CH2:8][CH2:9][CH2:10][CH2:11][CH2:12][CH2:13][CH2:14][O:15][CH2:16][C:17]1([CH3:18])[CH2:19][O:2...
C=C(C)CCl.CCCCCCCCCCCCCCO.O=C(OO)c1cccc(Cl)c1
CCCCCCCCCCCCCCOCC1(C)CO1
null
null
CN(C=O)C.ClCCl.O
Heteroatom Alkylation and Arylation
OtherReaction
f67fee1378ff9e29a7ec8914e82defd9e3495ac250ed6031b1fd098a2ace357d
f33536a6cbdd7c0e99b2e1466416f23e4a04749846e1248994131907e4409a93
C1CO1
Cl-[CH2;D2;+0:1]-[C;H0;D3;+0:2](-[C;D1;H3:3])=[CH2;D1;+0:4].Cl-c1:c:c:c:c(-C(=O)-O-[OH;D1;+0:5]):c:1.[C:6]-[C:7]-[OH;D1;+0:8]>>[C:6]-[C:7]-[O;H0;D2;+0:8]-[CH2;D2;+0:1]-[C;H0;D4;+0:2]1(-[C;D1;H3:3])-[CH2;D2;+0:4]-[O;H0;D2;+0:5]-1
79.5
[{"value": 79.4, "product": "O1CC1(COCCCCCCCCCCCCCC)C", "details": "PERCENTYIELD", "is_desired": false}, {"value": 79.5, "product": "O1CC1(COCCCCCCCCCCCCCC)C", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
60
CELSIUS
15
HOUR
A 200-ml flask equipped with a stirrer was charged with 10 g (46.6 mmol) of tetradecanol, 50 ml of dimethylformamide, 2.86 g (71.5 mmol) of 60% NaH and 5.96 g (65.8 mmol) of methallyl chloride. The contents were stirred at 60° C. for 15 hours. After completion of the reaction, the reaction mixture was added with water ...
10.6084/m9.figshare.5104873.v1
null
Aromatic halide.Primary halide.Primary alcohol.Peroxide.Vinyl
Ether.Ether
c1ccccc1
C1CO1
C1CO1
HCl
CN(C=O)C.ClCCl.O
60
15
C=C(C)CCl.CCCCCCCCCCCCCCO.O=C(OO)c1cccc(Cl)c1>CN(C=O)C.ClCCl.O>CCCCCCCCCCCCCCOCC1(C)CO1
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-40839e5adad8417b8a69e675e27185ad
CCCCCCCCCCCCCCOCC1(C)CO1.NCCO>>CCCCCCCCCCCCCCOCC(C)(O)CNCCO
C(O)CN.O1CC1(COCCCCCCCCCCCCCC)C>>OCCNCC(COCCCCCCCCCCCCCC)(O)C
[CH3:1][CH2:2][CH2:3][CH2:4][CH2:5][CH2:6][CH2:7][CH2:8][CH2:9][CH2:10][CH2:11][CH2:12][CH2:13][CH2:14][O:15][CH2:16][C:17]1([CH3:18])[O:19][CH2:20]1.[NH2:21][CH2:22][CH2:23][OH:24]>>[CH3:1][CH2:2][CH2:3][CH2:4][CH2:5][CH2:6][CH2:7][CH2:8][CH2:9][CH2:10][CH2:11][CH2:12][CH2:13][CH2:14][O:15][CH2:16][C:17]([CH3:18])([OH...
CCCCCCCCCCCCCCOCC1(C)CO1.NCCO
CCCCCCCCCCCCCCOCC(C)(O)CNCCO
null
null
C(C)O
Heteroatom Alkylation and Arylation
OtherReaction
09dcc949ba57c1c8aa9b0ec8a5f2d0bd08582df941541cfb30cc229d76954460
981ed0456dddd8dd6daddb49af97a2d7d93f8ca3d6b01c65314714af406e7930
null
[C:1]-[C:2]-[NH2;D1;+0:3].[C:4]-[C:5]1(-[C;D1;H3:6])-[CH2;D2;+0:7]-[O;H0;D2;+0:8]-1>>[C:4]-[C:5](-[C;D1;H3:6])(-[OH;D1;+0:8])-[CH2;D2;+0:7]-[NH;D2;+0:3]-[C:2]-[C:1]
68
[{"value": 68.0, "product": "OCCNCC(COCCCCCCCCCCCCCC)(O)C", "details": "PERCENTYIELD", "is_desired": false}, {"value": 67.9, "product": "OCCNCC(COCCCCCCCCCCCCCC)(O)C", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
80
CELSIUS
null
null
A 100-ml flask equipped with a stirrer and dropping funnel was then charged with 16.8 g (280 mmol) of ethanolamine and 15 g of ethanol. While stirring the mixture at 80° C., an ethanol solution of 5.00 g (17.6 mmol) of 1,2-epoxy-2-methyl-3-tetradecyloxypropane was added dropwise over 3 hours. The contents were stirred ...
10.6084/m9.figshare.5104873.v1
null
Ether.Primary amine
Tertiary alcohol.Secondary amine
C1CO1
null
null
null
C(C)O
80
null
CCCCCCCCCCCCCCOCC1(C)CO1.NCCO>C(C)O>CCCCCCCCCCCCCCOCC(C)(O)CNCCO
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-b9a01b6c4e7348f3b4a477b1d53347a8
CCCCCCCCCCCCCCOCC1CO1.NCCCO>>CCCCCCCCCCCCCCOCC(O)CNCCCO
C(C1CO1)OCCCCCCCCCCCCCC.NCCCO>>OCCCNCC(COCCCCCCCCCCCCCC)O
[CH3:1][CH2:2][CH2:3][CH2:4][CH2:5][CH2:6][CH2:7][CH2:8][CH2:9][CH2:10][CH2:11][CH2:12][CH2:13][CH2:14][O:15][CH2:16][CH:17]1[O:18][CH2:19]1.[NH2:20][CH2:21][CH2:22][CH2:23][OH:24]>>[CH3:1][CH2:2][CH2:3][CH2:4][CH2:5][CH2:6][CH2:7][CH2:8][CH2:9][CH2:10][CH2:11][CH2:12][CH2:13][CH2:14][O:15][CH2:16][CH:17]([OH:18])[CH2:...
CCCCCCCCCCCCCCOCC1CO1.NCCCO
CCCCCCCCCCCCCCOCC(O)CNCCCO
null
null
C(C)O
Heteroatom Alkylation and Arylation
OtherReaction
f75f8fec78b0ee9c8e880101c8c57c2a3edaac070bc7ad0163a34826e2af8c65
04c78336d85647f6dca3040f384f77009d1b541aac7f8ccf33aa9798091ceab8
null
[C:1]-[C:2]-[NH2;D1;+0:3].[C:4]-[C:5]1-[CH2;D2;+0:6]-[O;H0;D2;+0:7]-1>>[C:4]-[C:5](-[OH;D1;+0:7])-[CH2;D2;+0:6]-[NH;D2;+0:3]-[C:2]-[C:1]
135
[{"value": 92.0, "product": "OCCCNCC(COCCCCCCCCCCCCCC)O", "details": "PERCENTYIELD", "is_desired": false}, {"value": 135.0, "product": "OCCCNCC(COCCCCCCCCCCCCCC)O", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
80
CELSIUS
null
null
A 300-ml two-necked flask equipped with a stirrer and a dropping funnel was charged with 25.1 g (0.33 mol) of 3-amino-1-propanol and 6.00 g of ethanol, and the contents were heated and stirred at 80° C. in a nitrogen atmosphere. After 9.00 g (33 mmol) of tetradecyl glycidyl ether were added dropwise over 2 hours, the r...
10.6084/m9.figshare.5104873.v1
null
Ether.Primary amine
Secondary alcohol.Secondary amine
C1CO1
null
null
null
C(C)O
80
null
CCCCCCCCCCCCCCOCC1CO1.NCCCO>C(C)O>CCCCCCCCCCCCCCOCC(O)CNCCCO
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-5d521726c64849569940c6f7bb84cf4f
CCCCCCCCCCCCCCOCC1CO1.CCO.NCC(=O)O>>CCCCCCCCCCCCOCC(C)(O)CCNCCO
C(C1CO1)OCCCCCCCCCCCCCC.C(C)O.NCC(=O)O.[OH-].[Na+].C(C)O.Cl>>OCCNCCC(COCCCCCCCCCCCC)(O)C
C(C[CH2:3][CH2:4][CH2:5][CH2:6][CH2:7][CH2:8][CH2:9][CH2:10][CH2:11][CH2:12][O:13][CH2:14][CH:15]1[O:17][CH2:18]1)[CH2:2][CH3:1].O[CH2:19][CH3:16].O=[C:22]([CH2:21][NH2:20])[OH:23]>>[CH3:1][CH2:2][CH2:3][CH2:4][CH2:5][CH2:6][CH2:7][CH2:8][CH2:9][CH2:10][CH2:11][CH2:12][O:13][CH2:14][C:15]([CH3:16])([OH:17])[CH2:18][CH2...
CCCCCCCCCCCCCCOCC1CO1.CCO.NCC(=O)O
CCCCCCCCCCCCOCC(C)(O)CCNCCO
null
null
null
Heteroatom Alkylation and Arylation
OtherReaction
6421f63ee64704188eacd859707a492b167f8b99570829447d4f950d0da28cc4
eb72a91262031d72ce374b3d0d4d73595d6a629341524b46dda84055f634c18f
null
O-[CH2;D2;+0:1]-[CH3;D1;+0:2].O=[C;H0;D3;+0:3](-[O;D1;H1:4])-[C:5]-[NH2;D1;+0:6].[#8:7]-[C:8]-[CH;D3;+0:9]1-[CH2;D2;+0:10]-[O;H0;D2;+0:11]-1.[C:12]-[C:13]-[CH2;D2;+0:14]-C-C-[CH2;D2;+0:15]-[C;D1;H3:16]>>[#8:7]-[C:8]-[C;H0;D4;+0:9](-[CH3;D1;+0:2])(-[OH;D1;+0:11])-[CH2;D2;+0:10]-[CH2;D2;+0:1]-[NH;D2;+0:6]-[C:5]-[CH2;D2;+...
30.7
[{"value": 30.7, "product": "OCCNCCC(COCCCCCCCCCCCC)(O)C", "details": "PERCENTYIELD", "is_desired": false}]
80
CELSIUS
null
null
A 300-ml two-necked flask equipped with a stirrer was charged with 7.51 g (0.1 mol) of glycine, 8.3 g (0.1 mol) of 48% NaOH and 200 ml of ethanol. While stirring the mixture at 80° C., an ethanol solution of 2.70 g (10 mmol) of tetradecyl glycidyl ether was added, and the resultant mixture was stirred for 3 hours. Afte...
10.6084/m9.figshare.5104873.v1
null
Carboxylic acid.Ether.Primary alcohol.Primary amine
Primary alcohol.Tertiary alcohol.Secondary amine
C1CO1
null
null
HO-
null
80
null
CCCCCCCCCCCCCCOCC1CO1.CCO.NCC(=O)O>>CCCCCCCCCCCCOCC(C)(O)CCNCCO
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-1c432984f9d54ac78349420a214a1024
CCCCCCCCCCCCCCOCC(O)CNCCO.O=P(O)(O)O>>CCCCCCCCCCCCCCOCC(O)CNCCOP(=O)([O-])O
C(C1CO1)OCCCCCCCCCCCCCC.C(O)CN.O1CCCC1.P(O)(O)(O)=O.O=P12OP3(=O)OP(=O)(O1)OP(=O)(O2)O3.OCCNCC(COCCCCCCCCCCCCCC)O.[OH-].[Na+].[Na]>>P(=O)(OCCNCC(COCCCCCCCCCCCCCC)O)([O-])O.[Na+]
[CH3:1][CH2:2][CH2:3][CH2:4][CH2:5][CH2:6][CH2:7][CH2:8][CH2:9][CH2:10][CH2:11][CH2:12][CH2:13][CH2:14][O:15][CH2:16][CH:17]([OH:18])[CH2:19][NH:20][CH2:21][CH2:22][OH:23].O[P:24](=[O:25])([OH:26])[OH:27]>>[CH3:1][CH2:2][CH2:3][CH2:4][CH2:5][CH2:6][CH2:7][CH2:8][CH2:9][CH2:10][CH2:11][CH2:12][CH2:13][CH2:14][O:15][CH2:...
CCCCCCCCCCCCCCOCC(O)CNCCO.O=P(O)(O)O
CCCCCCCCCCCCCCOCC(O)CNCCOP(=O)([O-])O
null
null
O
Functional Group Interconversion
OtherReaction
bbb792e2dbaac6137f4ab4b2ad2edf8b90c54de5f7db3b319a5444b78b4405dc
5700379a096deb40e2dc50b293f55a01cfe36aa58cf97bdfa006d0b7ff21038e
null
O-[P;H0;D4;+0:1](=[O;D1;H0:2])(-[O;D1;H1:3])-[OH;D1;+0:4].[C:5]-[C:6]-[OH;D1;+0:7]>>[C:5]-[C:6]-[O;H0;D2;+0:7]-[P;H0;D4;+0:1](-[O-;H0;D1:4])(=[O;D1;H0:2])-[O;D1;H1:3]
36.2
[{"value": 34.9, "product": "P(=O)(OCCNCC(COCCCCCCCCCCCCCC)O)([O-])O.[Na+]", "details": "PERCENTYIELD", "is_desired": false}, {"value": 36.2, "product": "P(=O)(OCCNCC(COCCCCCCCCCCCCCC)O)([O-])O.[Na+]", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
30
MINUTE
A 300-ml flask equipped with a stirrer was charged with 5.13 g (14.8 mmol) of 3-(2-hydroxyethylamino)-1-tetradecyloxy-2-propanol prepared from tetradecyl glycidyl ether and ethanolamine in the same manner as in Preparation Example 14, and 70 mol of tetrahydrofuran, 1.95 g (16.9 mmol) of 85% phosphoric acid and 3.54 g (...
10.6084/m9.figshare.5104873.v1
null
Primary alcohol
null
null
null
null
HO-
O
null
0.5
CCCCCCCCCCCCCCOCC(O)CNCCO.O=P(O)(O)O>O>CCCCCCCCCCCCCCOCC(O)CNCCOP(=O)([O-])O
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-540e2d8dfa8f4e3c817851023a8dc240
CBr.CCCCCCC(O)CCCCCCCCCCCCC(O)CN(C)CCO.CCCCCCC(O)CCCCCCCCCCCOCC1CO1>>CCCCCCC(O)CCCCCCCCCCCCC(O)C[N+](C)(C)CC(C)O.[Br-]
CN(CCO)CC(CCCCCCCCCCCCC(CCCCCC)O)O.C(C1CO1)OCCCCCCCCCCCC(CCCCCC)O.CNCCO.COCC(CN(C)CCO)O.CBr>>[Br-].OC(C[N+](CC(CCCCCCCCCCCCC(CCCCCC)O)O)(C)C)C
[CH3:26][Br:31].[CH3:1][CH2:2][CH2:3][CH2:4][CH2:5][CH2:6][CH:7]([OH:8])[CH2:9][CH2:10][CH2:11][CH2:12][CH2:13][CH2:14][CH2:15][CH2:16][CH2:17][CH2:18][CH2:19][CH2:20][CH:21]([OH:22])[CH2:23][N:24]([CH3:25])[CH2:27][CH2:28][OH:30].CCCCCCC(O)CCCCCCCCCCCOCC1O[CH2:29]1>>[CH3:1][CH2:2][CH2:3][CH2:4][CH2:5][CH2:6][CH:7]([OH...
CBr.CCCCCCC(O)CCCCCCCCCCCCC(O)CN(C)CCO.CCCCCCC(O)CCCCCCCCCCCOCC1CO1
CCCCCCC(O)CCCCCCCCCCCCC(O)C[N+](C)(C)CC(C)O.[Br-]
null
null
C(C)OCC
Heteroatom Alkylation and Arylation
OtherReaction
655d5e15669199b985c336dee1e41bbd5c253d27b8f38540e39e955cb16b7ff2
749391d1c8d87bf3231b7e96c58a053d5f8d292ffc23c83916e5cf24297c51a5
null
C-C-C-C-C-C-C(-O)-C-C-C-C-C-C-C-C-C-C-C-O-C-C1-O-[CH2;D2;+0:1]-1.[Br;H0;D1;+0:2]-[CH3;D1;+0:3].[C:4]-[C:5]-[N;H0;D3;+0:6](-[C;D1;H3:7])-[C:8]-[CH2;D2;+0:9]-[O;D1;H1:10]>>[Br-;H0;D0:2].[C:4]-[C:5]-[N+;H0;D4:6](-[C;D1;H3:7])(-[CH3;D1;+0:3])-[C:8]-[CH;D3;+0:9](-[CH3;D1;+0:1])-[O;D1;H1:10]
90
[{"value": 90.0, "product": "[Br-].OC(C[N+](CC(CCCCCCCCCCCCC(CCCCCC)O)O)(C)C)C", "details": "PERCENTYIELD", "is_desired": false}]
null
null
null
null
1-[N-Methyl-N-(2-hydroxyethyl)amino]-3-(12-hydroxyoctadecyl)-2-propanol was first prepared from 12-hydroxyoctadecyl glycidyl ether and N-methylethanolamine in the same manner as in the preparation of N-(3-methoxy-2-hydroxy-propyl)-N-methyl-2-hydroxyethylamine in Preparation Example 24. A 200-ml autoclave was charged wi...
10.6084/m9.figshare.5104873.v1
null
Ether.Ether.Primary alcohol.Secondary alcohol.Tertiary amine
Secondary alcohol
C1CO1
null
null
HO-
C(C)OCC
null
null
CBr.CCCCCCC(O)CCCCCCCCCCCCC(O)CN(C)CCO.CCCCCCC(O)CCCCCCCCCCCOCC1CO1>C(C)OCC>CCCCCCC(O)CCCCCCCCCCCCC(O)C[N+](C)(C)CC(C)O.[Br-]
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-80c2effe4d3141839b36b2e47237d5ac
CCCCCCCCCCCCCCCCC1CO1.NCCO>>CCCCCCCCCCCCCCCCC(O)CNCCO
C(O)CN.C(C)O.O1CC1CCCCCCCCCCCCCCCC>>OCCNCC(CCCCCCCCCCCCCCCC)O
[CH3:1][CH2:2][CH2:3][CH2:4][CH2:5][CH2:6][CH2:7][CH2:8][CH2:9][CH2:10][CH2:11][CH2:12][CH2:13][CH2:14][CH2:15][CH2:16][CH:17]1[O:18][CH2:19]1.[NH2:20][CH2:21][CH2:22][OH:23]>>[CH3:1][CH2:2][CH2:3][CH2:4][CH2:5][CH2:6][CH2:7][CH2:8][CH2:9][CH2:10][CH2:11][CH2:12][CH2:13][CH2:14][CH2:15][CH2:16][CH:17]([OH:18])[CH2:19][...
CCCCCCCCCCCCCCCCC1CO1.NCCO
CCCCCCCCCCCCCCCCC(O)CNCCO
null
null
O
Heteroatom Alkylation and Arylation
OtherReaction
f75f8fec78b0ee9c8e880101c8c57c2a3edaac070bc7ad0163a34826e2af8c65
04c78336d85647f6dca3040f384f77009d1b541aac7f8ccf33aa9798091ceab8
null
[C:1]-[C:2]-[NH2;D1;+0:3].[C:4]-[C:5]1-[CH2;D2;+0:6]-[O;H0;D2;+0:7]-1>>[C:4]-[C:5](-[OH;D1;+0:7])-[CH2;D2;+0:6]-[NH;D2;+0:3]-[C:2]-[C:1]
74.6
[{"value": 74.6, "product": "OCCNCC(CCCCCCCCCCCCCCCC)O", "details": "PERCENTYIELD", "is_desired": false}, {"value": 74.6, "product": "OCCNCC(CCCCCCCCCCCCCCCC)O", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
80
CELSIUS
null
null
A 300-ml flask equipped with a stirrer and a dropping funnel was charged with 45.8 g (0.75 mol) of ethanolamine and 9 g of ethanol. While stirring the mixture at 80° C., 13.4 g (50 mmol) of 1,2-epoxyoctadecane were added dropwise over 2 hours. Water was added to the resultant reaction mixture, and white crystals formed...
10.6084/m9.figshare.5104873.v1
null
Ether.Primary amine
Secondary alcohol.Secondary amine
C1CO1
null
null
null
O
80
null
CCCCCCCCCCCCCCCCC1CO1.NCCO>O>CCCCCCCCCCCCCCCCC(O)CNCCO
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-b816d25167cf4c2ca0b10e123324d743
CCCCCCCCCCCCCCCCC1CO1.CNCCO>>CCCCCCCCCCCCCCCCC(O)CN(C)CCO
O1CC1CCCCCCCCCCCCCCCC.CNCCO>>OCCN(C)CC(CCCCCCCCCCCCCCCC)O
[CH3:1][CH2:2][CH2:3][CH2:4][CH2:5][CH2:6][CH2:7][CH2:8][CH2:9][CH2:10][CH2:11][CH2:12][CH2:13][CH2:14][CH2:15][CH2:16][CH:17]1[O:18][CH2:19]1.[NH:20]([CH3:21])[CH2:22][CH2:23][OH:24]>>[CH3:1][CH2:2][CH2:3][CH2:4][CH2:5][CH2:6][CH2:7][CH2:8][CH2:9][CH2:10][CH2:11][CH2:12][CH2:13][CH2:14][CH2:15][CH2:16][CH:17]([OH:18])...
CCCCCCCCCCCCCCCCC1CO1.CNCCO
CCCCCCCCCCCCCCCCC(O)CN(C)CCO
null
null
C(C)O
Heteroatom Alkylation and Arylation
Ring opening of epoxide with amine
8b0e6adfb78f36f9ea38287644fe13d1ed2aa3ea65e10cc66a65b05c37e2e473
97e758d6c4c8255d25541eb6c6a6f62e7dc30829ea162ca3392731efabc98a65
null
[C:1]-[C:2]-[NH;D2;+0:3]-[C;D1;H3:4].[C:5]-[C:6]1-[CH2;D2;+0:7]-[O;H0;D2;+0:8]-1>>[C:5]-[C:6](-[OH;D1;+0:8])-[CH2;D2;+0:7]-[N;H0;D3;+0:3](-[C;D1;H3:4])-[C:2]-[C:1]
67
[{"value": 67.0, "product": "OCCN(C)CC(CCCCCCCCCCCCCCCC)O", "details": "PERCENTYIELD", "is_desired": false}, {"value": 66.9, "product": "OCCN(C)CC(CCCCCCCCCCCCCCCC)O", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
80
CELSIUS
18
HOUR
A 300-ml flask equipped with a stirrer was charged with 26.85 g (0.1 mol) of 1,2-epoxyoctadecane, 7.51 g (0.1 mol) of N-methylethanolamine and 50 ml of ethanol, and the contents were stirred at 80° C. for 18 hours. After the solvent was distilled off under reduced pressure, the resultant residue was purified by column ...
10.6084/m9.figshare.5104873.v1
null
Ether.Secondary amine
Secondary alcohol.Tertiary amine
C1CO1
null
null
null
C(C)O
80
18
CCCCCCCCCCCCCCCCC1CO1.CNCCO>C(C)O>CCCCCCCCCCCCCCCCC(O)CN(C)CCO
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-e403979772a141b9b46f8ea7de5203df
CCCCCCCCCCCCCCOCC1OC1(C)C.NCCO>>CCCCCCCCCCCCCCOCC(NCCO)C(C)(C)O
C(O)CN.C(CCCCCCCCCCCCC)OCC1C(C)(C)O1>>OCCNC(C(C)(O)C)COCCCCCCCCCCCCCC
[CH3:1][CH2:2][CH2:3][CH2:4][CH2:5][CH2:6][CH2:7][CH2:8][CH2:9][CH2:10][CH2:11][CH2:12][CH2:13][CH2:14][O:15][CH2:16][CH:17]1[C:22]([CH3:23])([CH3:24])[O:25]1.[NH2:18][CH2:19][CH2:20][OH:21]>>[CH3:1][CH2:2][CH2:3][CH2:4][CH2:5][CH2:6][CH2:7][CH2:8][CH2:9][CH2:10][CH2:11][CH2:12][CH2:13][CH2:14][O:15][CH2:16][CH:17]([NH...
CCCCCCCCCCCCCCOCC1OC1(C)C.NCCO
CCCCCCCCCCCCCCOCC(NCCO)C(C)(C)O
null
null
C(C)O
Heteroatom Alkylation and Arylation
OtherReaction
09dcc949ba57c1c8aa9b0ec8a5f2d0bd08582df941541cfb30cc229d76954460
981ed0456dddd8dd6daddb49af97a2d7d93f8ca3d6b01c65314714af406e7930
null
[#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].[C:8]-[C:9]-[NH2;D1;+0:10]>>[#8:1]-[C:2]-[CH;D3;+0:3](-[NH;D2;+0:10]-[C:9]-[C:8])-[C:5](-[C;D1;H3:6])(-[C;D1;H3:7])-[OH;D1;+0:4]
58
[{"value": 58.0, "product": "OCCNC(C(C)(O)C)COCCCCCCCCCCCCCC", "details": "PERCENTYIELD", "is_desired": false}, {"value": 57.8, "product": "OCCNC(C(C)(O)C)COCCCCCCCCCCCCCC", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
80
CELSIUS
null
null
A 100-ml two-necked flask equipped with a stirrer and a dropping funnel was charged with 15.3 g (16.7 mmol) of ethanolamine and 5.0 g of ethanol. While heating and stirring the mixture at 80° C. in a nitrogen atmosphere, an ethanol solution of 5.00 g (16.7 mmol) of 1-tetradecyloxy-3-methyl-2-butene oxide was added drop...
10.6084/m9.figshare.5104873.v1
null
Ether.Primary amine
Tertiary alcohol.Secondary amine
C1CO1
null
null
null
C(C)O
80
null
CCCCCCCCCCCCCCOCC1OC1(C)C.NCCO>C(C)O>CCCCCCCCCCCCCCOCC(NCCO)C(C)(C)O
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-70a4eebe93b24ba3bd4111e18405dbfa
CCCCCCCCC=CCCCCCCCC(=O)NCCO>>CCCCCCCCC=CCCCCCCCCNCCO
[OH-].[K+].C(CCCCCCCC=CCCCCCCCC)(=O)NCCO.[H-].[H-].[H-].[H-].[Li+].[Al+3].N#N>>C(CCCCCCCC=CCCCCCCCC)NCCO
O=[C:18]([CH2:17][CH2:16][CH2:15][CH2:14][CH2:13][CH2:12][CH2:11][CH:10]=[CH:9][CH2:8][CH2:7][CH2:6][CH2:5][CH2:4][CH2:3][CH2:2][CH3:1])[NH:19][CH2:20][CH2:21][OH:22]>>[CH3:1][CH2:2][CH2:3][CH2:4][CH2:5][CH2:6][CH2:7][CH2:8][CH:9]=[CH:10][CH2:11][CH2:12][CH2:13][CH2:14][CH2:15][CH2:16][CH2:17][CH2:18][NH:19][CH2:20][CH...
CCCCCCCCC=CCCCCCCCC(=O)NCCO
CCCCCCCCC=CCCCCCCCCNCCO
null
null
O1CCCC1
Reduction
Reduction of secondary amides to amines
85b757f1833edc9e5c6365ee6b904683f414e7b9a5f9bfcfd7addca401447058
ab40188eef2f825df7003af0ffae31d0ce53d126542122535627d3d354cbc9fe
null
O=[C;H0;D3;+0:1](-[#7:2]-[C:3])-[C:4]-[C:5]>>[C:5]-[C:4]-[CH2;D2;+0:1]-[#7:2]-[C:3]
65
[{"value": 65.0, "product": "C(CCCCCCCC=CCCCCCCCC)NCCO", "details": "PERCENTYIELD", "is_desired": false}, {"value": 60.2, "product": "C(CCCCCCCC=CCCCCCCCC)NCCO", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
60
CELSIUS
16
HOUR
A 100-ml eggplant type flask equipped with a stirrer was charged with 1.40 g (37.2 mmol) of LiAlH4 and 30 ml of tetrahydrofuran. While heating and stirring the contents at room temperature in an N2 atmosphere, a tetrahydrofuran solution of 1.67 g (5.12 mmol) of N-(9-octadecenoyl)ethanolamine was added dropwise over 10 ...
10.6084/m9.figshare.5104873.v1
null
Secondary amide
null
null
null
null
Other
O1CCCC1
60
16
CCCCCCCCC=CCCCCCCCC(=O)NCCO>O1CCCC1>CCCCCCCCC=CCCCCCCCCNCCO
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-9575b1a855c84db398427cd5e89360d1
CS(C)=O.O=CCCCCCCCCCCCCCCOC1CCCCO1>>C=CCCCCCCCCCCCCCCOC1CCCCO1
O1C(CCCC1)OCCCCCCCCCCCCCCC=O.CS(=O)C.N#N.[H-].[Na+].CS(=O)C.O>>O1C(CCCC1)OCCCCCCCCCCCCCCC=C
CS(=O)[CH3:1].O=[CH:2][CH2:3][CH2:4][CH2:5][CH2:6][CH2:7][CH2:8][CH2:9][CH2:10][CH2:11][CH2:12][CH2:13][CH2:14][CH2:15][CH2:16][O:17][CH:18]1[CH2:19][CH2:20][CH2:21][CH2:22][O:23]1>>[CH2:1]=[CH:2][CH2:3][CH2:4][CH2:5][CH2:6][CH2:7][CH2:8][CH2:9][CH2:10][CH2:11][CH2:12][CH2:13][CH2:14][CH2:15][CH2:16][O:17][CH:18]1[CH2:...
CS(C)=O.O=CCCCCCCCCCCCCCCOC1CCCCO1
C=CCCCCCCCCCCCCCCOC1CCCCO1
null
[Br-].C[P+](C1=CC=CC=C1)(C1=CC=CC=C1)C1=CC=CC=C1
C1CCOC1
C-C Coupling
OtherReaction
5cfb75c6bab693235daf0ac5fd1246c85d26339c8533fb46cd8a376b6da4a918
5aa2b06974507c8a8025fd53b24b8c1d2de573e1740ff1857bc2886b8646feca
C1CCOCC1
C-S(=O)-[CH3;D1;+0:1].O=[CH;D2;+0:2]-[C:3]-[C:4]>>[C:4]-[C:3]-[CH;D2;+0:2]=[CH2;D1;+0:1]
46
[{"value": 46.0, "product": "O1C(CCCC1)OCCCCCCCCCCCCCCC=C", "details": "PERCENTYIELD", "is_desired": false}]
null
null
30
MINUTE
A 300-ml three-necked flask equipped with a stirrer, dropping funnel and N2 inlet tube was charged with 40 ml of dimethyl sulfoxide and 1.2 g (30 mmol) of 60% sodium hydride. The contents were stirred at 75° C. for 1.5 hours in an N2 atmosphere and then cooled to room temperature. To this mixture, a solution of 8.93 g ...
10.6084/m9.figshare.5104873.v1
null
Aldehyde.Sulfoxide
Allyl
null
null
C1CCOCC1
Other
[Br-].C[P+](C1=CC=CC=C1)(C1=CC=CC=C1)C1=CC=CC=C1.C1CCOC1
null
0.5
CS(C)=O.O=CCCCCCCCCCCCCCCOC1CCCCO1>[Br-].C[P+](C1=CC=CC=C1)(C1=CC=CC=C1)C1=CC=CC=C1.C1CCOC1>C=CCCCCCCCCCCCCCCOC1CCCCO1
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-c54f235e113e4ef68f3a56e016403a66
NCCO.OCCCCCCCCCCCCCCC1CO1>>OCCCCCCCCCCCCCCC(O)CNCCO
O1CC1CCCCCCCCCCCCCCO.C(O)CN.N#N.C(O)CN>>OCCNCC(CCCCCCCCCCCCCCO)O
[NH2:19][CH2:20][CH2:21][OH:22].[OH:1][CH2:2][CH2:3][CH2:4][CH2:5][CH2:6][CH2:7][CH2:8][CH2:9][CH2:10][CH2:11][CH2:12][CH2:13][CH2:14][CH2:15][CH:16]1[O:17][CH2:18]1>>[OH:1][CH2:2][CH2:3][CH2:4][CH2:5][CH2:6][CH2:7][CH2:8][CH2:9][CH2:10][CH2:11][CH2:12][CH2:13][CH2:14][CH2:15][CH:16]([OH:17])[CH2:18][NH:19][CH2:20][CH2...
NCCO.OCCCCCCCCCCCCCCC1CO1
OCCCCCCCCCCCCCCC(O)CNCCO
null
null
C(C)O
Heteroatom Alkylation and Arylation
OtherReaction
f75f8fec78b0ee9c8e880101c8c57c2a3edaac070bc7ad0163a34826e2af8c65
04c78336d85647f6dca3040f384f77009d1b541aac7f8ccf33aa9798091ceab8
null
[C:1]-[C:2]-[NH2;D1;+0:3].[C:4]-[C:5]1-[CH2;D2;+0:6]-[O;H0;D2;+0:7]-1>>[C:4]-[C:5](-[OH;D1;+0:7])-[CH2;D2;+0:6]-[NH;D2;+0:3]-[C:2]-[C:1]
68
[{"value": 68.0, "product": "OCCNCC(CCCCCCCCCCCCCCO)O", "details": "PERCENTYIELD", "is_desired": false}, {"value": 66.7, "product": "OCCNCC(CCCCCCCCCCCCCCO)O", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
null
null
A 50-ml two-necked flask equipped with a stirrer, dropping funnel and N2 inlet tube was charged with 4.14 g (68 mmol) of ethanolamine and 0.8 g of ethanol. While heating and stirring the mixture at 80° C. in an N2 atmosphere, an ethanol solution of 0.87 g (3.4 mmol) of 1,2-epoxy-16-hexadecanol was added dropwise over 1...
10.6084/m9.figshare.5104873.v1
null
Ether.Primary amine
Secondary alcohol.Secondary amine
C1CO1
null
null
null
C(C)O
null
null
NCCO.OCCCCCCCCCCCCCCC1CO1>C(C)O>OCCCCCCCCCCCCCCC(O)CNCCO
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-314181a292b147ec995c4191958340db
O=C1CCCCCCCCCCCCCCCO1.OCCNCCO>>O=C(CCCCCCCCCCCCCCCO)N(CCO)CCO
N(CCO)CCO.C1CCCCCCCC(=O)OCCCCCCC1>>OCCN(C(CCCCCCCCCCCCCCCO)=O)CCO
[O:1]=[C:2]1[CH2:3][CH2:4][CH2:5][CH2:6][CH2:7][CH2:8][CH2:9][CH2:10][CH2:11][CH2:12][CH2:13][CH2:14][CH2:15][CH2:16][CH2:17][O:18]1.[NH:19]([CH2:20][CH2:21][OH:22])[CH2:23][CH2:24][OH:25]>>[O:1]=[C:2]([CH2:3][CH2:4][CH2:5][CH2:6][CH2:7][CH2:8][CH2:9][CH2:10][CH2:11][CH2:12][CH2:13][CH2:14][CH2:15][CH2:16][CH2:17][OH:1...
O=C1CCCCCCCCCCCCCCCO1.OCCNCCO
O=C(CCCCCCCCCCCCCCCO)N(CCO)CCO
null
C[O-].[Na+]
O
Acylation
OtherReaction
d0669d32ff95853a71a1e4f52e404d304c90e5a3ad7f5c6454f90efa0c0695d9
ff1ec1760b35133bcda3889e4f778444bc5783bb8e80db6e68552e7362fe2c9f
null
[C:1]-[C:2]-[NH;D2;+0:3]-[C:4]-[C:5].[C:6]-[C:7]-[O;H0;D2;+0:8]-[C;H0;D3;+0:9](=[O;D1;H0:10])-[C:11]-[C:12]>>[C:1]-[C:2]-[N;H0;D3;+0:3](-[C:4]-[C:5])-[C;H0;D3;+0:9](=[O;D1;H0:10])-[C:11]-[C:12].[C:6]-[C:7]-[OH;D1;+0:8]
82
[{"value": 82.0, "product": "OCCN(C(CCCCCCCCCCCCCCCO)=O)CCO", "details": "PERCENTYIELD", "is_desired": false}, {"value": 82.0, "product": "OCCN(C(CCCCCCCCCCCCCCCO)=O)CCO", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
80
CELSIUS
18
HOUR
A 200-ml flask equipped with a stirrer was charged with 16.6 g (158 mmol) of diethanolamine and 20.1 g (79 mmol) of cyclohexadecanolide, to which 0.21 g (3.9 mmol) of sodium methoxide was added. The contents were stirred at 80° C. for 18 hours. After completion of the reaction, water was added, and solids deposited wer...
10.6084/m9.figshare.5104873.v1
null
Ester.Secondary amine
Tertiary amide.Primary alcohol
C1CCCCCCCCOCCCCCCC1
null
null
null
C[O-].[Na+].O
80
18
O=C1CCCCCCCCCCCCCCCO1.OCCNCCO>C[O-].[Na+].O>O=C(CCCCCCCCCCCCCCCO)N(CCO)CCO
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-f7c05078e24046a8887d238bff8b0c4f
O=C(CCCCCCCCCCCCCCCO)N(CCO)CCO>>OCCCCCCCCCCCCCCCCN(CCO)CCO
[OH-].[K+].N#N.OCCN(C(CCCCCCCCCCCCCCCO)=O)CCO.[H-].[H-].[H-].[H-].[Li+].[Al+3]>>OCCN(CCO)CCCCCCCCCCCCCCCCO
O=[C:17]([CH2:16][CH2:15][CH2:14][CH2:13][CH2:12][CH2:11][CH2:10][CH2:9][CH2:8][CH2:7][CH2:6][CH2:5][CH2:4][CH2:3][CH2:2][OH:1])[N:18]([CH2:19][CH2:20][OH:21])[CH2:22][CH2:23][OH:24]>>[OH:1][CH2:2][CH2:3][CH2:4][CH2:5][CH2:6][CH2:7][CH2:8][CH2:9][CH2:10][CH2:11][CH2:12][CH2:13][CH2:14][CH2:15][CH2:16][CH2:17][N:18]([CH...
O=C(CCCCCCCCCCCCCCCO)N(CCO)CCO
OCCCCCCCCCCCCCCCCN(CCO)CCO
null
null
O1CCCC1
Reduction
Reduction of tertiary amides to amines
f74c5a050b269ec4da3871c266f01344b7447381f47cda744f8b1e9c225ae62d
c8f3c617792f7a4fae96b8a97dc0ce23461ab85d8a738fe6caacff776ef51ffa
null
O=[C;H0;D3;+0:1](-[C:2]-[C:3])-[#7:4](-[C:5])-[C:6]>>[C:3]-[C:2]-[CH2;D2;+0:1]-[#7:4](-[C:5])-[C:6]
62
[{"value": 62.0, "product": "OCCN(CCO)CCCCCCCCCCCCCCCCO", "details": "PERCENTYIELD", "is_desired": false}, {"value": 62.0, "product": "OCCN(CCO)CCCCCCCCCCCCCCCCO", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
65
CELSIUS
18
HOUR
A 500-ml flask equipped with a stirrer and reflux condenser was charged with 3.01 g (79.3 mmol) of LiAlH4 and 200 ml of tetrahydrofuran. While stirring the mixture at room temperature in an N2 atmosphere, 5.00 g (13.9 mmol) of N,N-bis(2-hydroxyethyl)-16-hydroxyhexadecanamide were added, followed by stirring at 65° C. f...
10.6084/m9.figshare.5104873.v1
null
Tertiary amide
null
null
null
null
Other
O1CCCC1
65
18
O=C(CCCCCCCCCCCCCCCO)N(CCO)CCO>O1CCCC1>OCCCCCCCCCCCCCCCCN(CCO)CCO
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-1fba45c98c28483dbc24abfca08ff922
COC(=O)CCCCCCCCCCCCCCCOC1CCCCO1.OCCNCCO>>OCCNCCCCCCCCCCCCCCCCOC1CCCCO1
C1CCCCCCCC(=O)OCCCCCCC1.C(O)CN.O1C(CCCC1)OCCCCCCCCCCCCCCCC(=O)OC.N(CCO)CCO>>OCCNCCCCCCCCCCCCCCCCOC1OCCCC1
COC(=O)[CH2:6][CH2:7][CH2:8][CH2:9][CH2:10][CH2:11][CH2:12][CH2:13][CH2:14][CH2:15][CH2:16][CH2:17][CH2:18][CH2:19][CH2:20][O:21][CH:22]1[CH2:23][CH2:24][CH2:25][CH2:26][O:27]1.OC[CH2:5][NH:4][CH2:3][CH2:2][OH:1]>>[OH:1][CH2:2][CH2:3][NH:4][CH2:5][CH2:6][CH2:7][CH2:8][CH2:9][CH2:10][CH2:11][CH2:12][CH2:13][CH2:14][CH2:...
COC(=O)CCCCCCCCCCCCCCCOC1CCCCO1.OCCNCCO
OCCNCCCCCCCCCCCCCCCCOC1CCCCO1
null
null
null
C-C Coupling
OtherReaction
c6e6f8431a2f95e212ca1ff22e794af539e5b288412b6c9354d640c48d89ad58
28126b46b6bfdfc96be770904d9dbbbb023c790c30cc393f36b178a45fe2e52f
C1CCOCC1
C-O-C(=O)-[CH2;D2;+0:1]-[C:2]-[C:3].O-C-[CH2;D2;+0:4]-[#7:5]-[C:6]>>[C:6]-[#7:5]-[CH2;D2;+0:4]-[CH2;D2;+0:1]-[C:2]-[C:3]
null
[]
null
null
null
null
A reaction was conducted in the same manner as in Preparation Example 37 except that ethanolamine and methyl 16-(2-tetrahydropyranyloxy)hexadecanate were used in place of diethanolamine and cyclohexadecanolide, respectively, in Preparation Example 37, thereby obtaining the title compound (IId-4). Conditions: See reacti...
10.6084/m9.figshare.5104873.v1
null
Ester.Primary alcohol
null
null
null
C1CCOCC1
HO-
null
null
null
COC(=O)CCCCCCCCCCCCCCCOC1CCCCO1.OCCNCCO>>OCCNCCCCCCCCCCCCCCCCOC1CCCCO1
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-050e689426f84409ae62ef62ee510e60
CCCCCCCCCCCCCCSCC1CO1.NCCO>>CCCCCCCCCCCCCCSCC(O)CNCCO
C(O)CN.C(CCCCCCCCCCCCC)SCC1CO1>>OCCNCC(CSCCCCCCCCCCCCCC)O
[CH3:1][CH2:2][CH2:3][CH2:4][CH2:5][CH2:6][CH2:7][CH2:8][CH2:9][CH2:10][CH2:11][CH2:12][CH2:13][CH2:14][S:15][CH2:16][CH:17]1[O:18][CH2:19]1.[NH2:20][CH2:21][CH2:22][OH:23]>>[CH3:1][CH2:2][CH2:3][CH2:4][CH2:5][CH2:6][CH2:7][CH2:8][CH2:9][CH2:10][CH2:11][CH2:12][CH2:13][CH2:14][S:15][CH2:16][CH:17]([OH:18])[CH2:19][NH:2...
CCCCCCCCCCCCCCSCC1CO1.NCCO
CCCCCCCCCCCCCCSCC(O)CNCCO
null
null
C(C)O
Heteroatom Alkylation and Arylation
OtherReaction
f75f8fec78b0ee9c8e880101c8c57c2a3edaac070bc7ad0163a34826e2af8c65
04c78336d85647f6dca3040f384f77009d1b541aac7f8ccf33aa9798091ceab8
null
[C:1]-[C:2]-[NH2;D1;+0:3].[C:4]-[C:5]1-[CH2;D2;+0:6]-[O;H0;D2;+0:7]-1>>[C:4]-[C:5](-[OH;D1;+0:7])-[CH2;D2;+0:6]-[NH;D2;+0:3]-[C:2]-[C:1]
91
[{"value": 91.0, "product": "OCCNCC(CSCCCCCCCCCCCCCC)O", "details": "PERCENTYIELD", "is_desired": false}, {"value": 90.9, "product": "OCCNCC(CSCCCCCCCCCCCCCC)O", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
80
CELSIUS
null
null
A 300-ml flask equipped with a stirrer and dropping funnel was charged with 61.1 g (1 mol) of ethanolamine and 61 g of ethanol. While stirring the contents at 80° C., a solution of 14.3 g (50 mmol) of 1-tetradecylthio-2,3-epoxypropane in 30 g ethanol was added dropwise over 3 hours. After completion of the dropping, th...
10.6084/m9.figshare.5104873.v1
null
Ether.Primary amine
Secondary alcohol.Secondary amine
C1CO1
null
null
null
C(C)O
80
null
CCCCCCCCCCCCCCSCC1CO1.NCCO>C(C)O>CCCCCCCCCCCCCCSCC(O)CNCCO
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-a88b93c6dde7436aafafe69ae2775345
CCCCCCCCCCCCCC(=O)OCC1CO1.CNCCO>>CCCCCCCCCCCCCC(=O)OCC(O)CN(C)CCO
CNCCO.C(CCCCCCCCCCCCC)(=O)OCC1CO1>>C(CCCCCCCCCCCCC)(=O)OCC(CN(C)CCO)O
[CH3:1][CH2:2][CH2:3][CH2:4][CH2:5][CH2:6][CH2:7][CH2:8][CH2:9][CH2:10][CH2:11][CH2:12][CH2:13][C:14](=[O:15])[O:16][CH2:17][CH:18]1[O:19][CH2:20]1.[NH:21]([CH3:22])[CH2:23][CH2:24][OH:25]>>[CH3:1][CH2:2][CH2:3][CH2:4][CH2:5][CH2:6][CH2:7][CH2:8][CH2:9][CH2:10][CH2:11][CH2:12][CH2:13][C:14](=[O:15])[O:16][CH2:17][CH:18...
CCCCCCCCCCCCCC(=O)OCC1CO1.CNCCO
CCCCCCCCCCCCCC(=O)OCC(O)CN(C)CCO
null
null
C(C)O
Heteroatom Alkylation and Arylation
Ring opening of epoxide with amine
8b0e6adfb78f36f9ea38287644fe13d1ed2aa3ea65e10cc66a65b05c37e2e473
97e758d6c4c8255d25541eb6c6a6f62e7dc30829ea162ca3392731efabc98a65
null
[C:1]-[C:2]-[NH;D2;+0:3]-[C;D1;H3:4].[C:5]-[C:6]1-[CH2;D2;+0:7]-[O;H0;D2;+0:8]-1>>[C:5]-[C:6](-[OH;D1;+0:8])-[CH2;D2;+0:7]-[N;H0;D3;+0:3](-[C;D1;H3:4])-[C:2]-[C:1]
60.8
[{"value": 60.8, "product": "C(CCCCCCCCCCCCC)(=O)OCC(CN(C)CCO)O", "details": "PERCENTYIELD", "is_desired": false}, {"value": 60.8, "product": "C(CCCCCCCCCCCCC)(=O)OCC(CN(C)CCO)O", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
80
CELSIUS
2
HOUR
A 100-ml flask equipped with a stirrer and dropping funnel was charged with 6.01 g (80 mmol) of N-methylethanolamine, 50 ml of ethanol and 22.8 g (80 mmol) of glycidyl tetradecanate, and the contents were stirred at 80° C. for 2 hours. The resultant reaction mixture was concentrated under reduced pressure, and the resi...
10.6084/m9.figshare.5104873.v1
null
Ether.Secondary amine
Secondary alcohol.Tertiary amine
C1CO1
null
null
null
C(C)O
80
2
CCCCCCCCCCCCCC(=O)OCC1CO1.CNCCO>C(C)O>CCCCCCCCCCCCCC(=O)OCC(O)CN(C)CCO
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-4e7d6fabfea64e0cb15c31ea61de1db0
CC(O)NCCN.CCCCCCC(O)CCCCCCCCCCC(=O)OCC>>CCCCCCC(O)CCCCCCCCCCC(=O)NCCNCCO
OC(CCCCCCCCCCC(=O)OCC)CCCCCC.NCCNC(C)O.C[O-].[Na+].N#N>>OCCNCCNC(CCCCCCCCCCC(CCCCCC)O)=O
[NH2:21][CH2:22][CH2:23][NH:24][CH:25]([CH3:26])[OH:27].CCO[C:19]([CH2:18][CH2:17][CH2:16][CH2:15][CH2:14][CH2:13][CH2:12][CH2:11][CH2:10][CH2:9][CH:7]([CH2:6][CH2:5][CH2:4][CH2:3][CH2:2][CH3:1])[OH:8])=[O:20]>>[CH3:1][CH2:2][CH2:3][CH2:4][CH2:5][CH2:6][CH:7]([OH:8])[CH2:9][CH2:10][CH2:11][CH2:12][CH2:13][CH2:14][CH2:1...
CC(O)NCCN.CCCCCCC(O)CCCCCCCCCCC(=O)OCC
CCCCCCC(O)CCCCCCCCCCC(=O)NCCNCCO
null
null
C1CCOC1.O
Acylation
OtherReaction
077654e25b1463cc2f90add0637d4cfbbe7d9928abe034ea0ed574169e01e19c
e8f6313ae381d127459d5b4a3f52751700bf2be0d0c8db3d4e4c0ac77993682f
null
C-C-O-[C;H0;D3;+0:1](=[O;D1;H0:2])-[C:3]-[C:4].[CH3;D1;+0:5]-[CH;D3;+0:6](-[OH;D1;+0:7])-[#7:8]-[C:9]-[C:10]-[NH2;D1;+0:11]>>[C:4]-[C:3]-[C;H0;D3;+0:1](=[O;D1;H0:2])-[NH;D2;+0:11]-[C:10]-[C:9]-[#7:8]-[CH2;D2;+0:6]-[CH2;D2;+0:5]-[OH;D1;+0:7]
737.2
[{"value": 74.0, "product": "OCCNCCNC(CCCCCCCCCCC(CCCCCC)O)=O", "details": "PERCENTYIELD", "is_desired": false}, {"value": 737.2, "product": "OCCNCCNC(CCCCCCCCCCC(CCCCCC)O)=O", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
null
null
A 30-ml two-necked flask equipped with a stirrer and dropping funnel was charged with 2.08 g (20 mmol) of aminoethylaminoethanol and 0.054 g (1 mmol) of sodium methoxide. While heating and stirring the contents at 80° C. in an N2 atmosphere, a solution of 3.29 g (10 mmol) of ethyl 12-hydroxystearate in 10 ml of THF was...
10.6084/m9.figshare.5104873.v1
null
Ester.Secondary alcohol.Primary amine
Secondary amide.Primary alcohol
null
null
null
HO-
C1CCOC1.O
null
null
CC(O)NCCN.CCCCCCC(O)CCCCCCCCCCC(=O)OCC>C1CCOC1.O>CCCCCCC(O)CCCCCCCCCCC(=O)NCCNCCO
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-336388df5b80425486bbf74ea75cd7c9
C=CC(O)CCCCCCCCCC.O=C(OO)c1cccc(Cl)c1>>CCCCCCCCCCC(O)C1CO1
C=CC(CCCCCCCCCC)O.ClC1=CC(=CC=C1)C(=O)OO.C1=CC=CC=C1>>O1CC1C(CCCCCCCCCC)O
[CH3:1][CH2:2][CH2:3][CH2:4][CH2:5][CH2:6][CH2:7][CH2:8][CH2:9][CH2:10][CH:11]([OH:12])[CH:13]=[CH2:14].O=C(O[OH:15])c1cccc(Cl)c1>>[CH3:1][CH2:2][CH2:3][CH2:4][CH2:5][CH2:6][CH2:7][CH2:8][CH2:9][CH2:10][CH:11]([OH:12])[CH:13]1[CH2:14][O:15]1
C=CC(O)CCCCCCCCCC.O=C(OO)c1cccc(Cl)c1
CCCCCCCCCCC(O)C1CO1
null
null
CCCCCC
Heteroatom Alkylation and Arylation
OtherReaction
d136da1ba89cbec8282600d9bfdb623a2c13519ce4d37a4560f0218659f5ffb4
f75e65b0e5496a37782761dec7855d157e425ce81d4a868786f212e1339acdbf
C1CO1
Cl-c1:c:c:c:c(-C(=O)-O-[OH;D1;+0:1]):c:1.[C:2]-[C:3](-[O;D1;H1:4])-[CH;D2;+0:5]=[CH2;D1;+0:6]>>[C:2]-[C:3](-[O;D1;H1:4])-[CH;D3;+0:5]1-[CH2;D2;+0:6]-[O;H0;D2;+0:1]-1
74
[{"value": 74.0, "product": "O1CC1C(CCCCCCCCCC)O", "details": "PERCENTYIELD", "is_desired": false}, {"value": 73.9, "product": "O1CC1C(CCCCCCCCCC)O", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
48
HOUR
A 500-ml flask equipped with a stirrer was charged with 23.8 g (0.12 mol) of 1-tridecen-3-ol, 25.0 g (0.145 mol) of m-chloroperbenzoic acid and 250 ml of benzene, and the contents were stirred at room temperature for 48 hours. After completion of the reaction, 200 ml of hexane. Solids deposited were separated by filtra...
10.6084/m9.figshare.5104873.v1
null
Aromatic halide.Peroxide.Vinyl
Ether
c1ccccc1
C1CO1
C1CO1
HCl
CCCCCC
null
48
C=CC(O)CCCCCCCCCC.O=C(OO)c1cccc(Cl)c1>CCCCCC>CCCCCCCCCCC(O)C1CO1
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-5b031bc712c84f05b17662207d4f72dd
CCCCCCCCCCC(O)C1CO1.NCc1ccccc1>>CCCCCCCCCCC(O)C(O)CNCc1ccccc1
C(C1=CC=CC=C1)N.O1CC1C(CCCCCCCCCC)O>>C(C1=CC=CC=C1)NCC(C(CCCCCCCCCC)O)O
[CH3:1][CH2:2][CH2:3][CH2:4][CH2:5][CH2:6][CH2:7][CH2:8][CH2:9][CH2:10][CH:11]([OH:12])[CH:13]1[O:14][CH2:15]1.[NH2:16][CH2:17][c:18]1[cH:19][cH:20][cH:21][cH:22][cH:23]1>>[CH3:1][CH2:2][CH2:3][CH2:4][CH2:5][CH2:6][CH2:7][CH2:8][CH2:9][CH2:10][CH:11]([OH:12])[CH:13]([OH:14])[CH2:15][NH:16][CH2:17][c:18]1[cH:19][cH:20][...
CCCCCCCCCCC(O)C1CO1.NCc1ccccc1
CCCCCCCCCCC(O)C(O)CNCc1ccccc1
null
null
O1CCOCC1
Heteroatom Alkylation and Arylation
OtherReaction
f75f8fec78b0ee9c8e880101c8c57c2a3edaac070bc7ad0163a34826e2af8c65
04c78336d85647f6dca3040f384f77009d1b541aac7f8ccf33aa9798091ceab8
c1ccccc1
[C:1]-[C:2]1-[CH2;D2;+0:3]-[O;H0;D2;+0:4]-1.[NH2;D1;+0:5]-[C:6]-[c:7]>>[C:1]-[C:2](-[OH;D1;+0:4])-[CH2;D2;+0:3]-[NH;D2;+0:5]-[C:6]-[c:7]
72
[{"value": 72.0, "product": "C(C1=CC=CC=C1)NCC(C(CCCCCCCCCC)O)O", "details": "PERCENTYIELD", "is_desired": false}, {"value": 71.8, "product": "C(C1=CC=CC=C1)NCC(C(CCCCCCCCCC)O)O", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
12
HOUR
A 500-ml flask equipped with a stirrer was charged with 107 g (1 mol) of benzylamine, to which a solution of 5.2 g (71 mmol) of 1,2-epoxy-3-tridecanol in 170 ml of dioxane was added dropwise over 2 hours. After completion of the dropping, a reaction was conducted further for 12 hours at 80° C. Dioxane and excess benzyl...
10.6084/m9.figshare.5104873.v1
null
Ether.Primary amine
Secondary alcohol.Secondary amine
C1CO1
null
c1ccccc1
null
O1CCOCC1
null
12
CCCCCCCCCCC(O)C1CO1.NCc1ccccc1>O1CCOCC1>CCCCCCCCCCC(O)C(O)CNCc1ccccc1
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-6f171f3959e24ce6acc5b2cc1ccb94f6
CCCCCCCCCCCCCCCCC1CO1>>CCCCCCCCCCCCCCCCC(O)CN
C(C1=CC=CC=C1)N.O1CC1CCCCCCCCCCCCCCCC>>NCC(CCCCCCCCCCCCCCCC)O
[CH3:1][CH2:2][CH2:3][CH2:4][CH2:5][CH2:6][CH2:7][CH2:8][CH2:9][CH2:10][CH2:11][CH2:12][CH2:13][CH2:14][CH2:15][CH2:16][CH:17]1[O:18][CH2:19]1>>[CH3:1][CH2:2][CH2:3][CH2:4][CH2:5][CH2:6][CH2:7][CH2:8][CH2:9][CH2:10][CH2:11][CH2:12][CH2:13][CH2:14][CH2:15][CH2:16][CH:17]([OH:18])[CH2:19][NH2:20]
CCCCCCCCCCCCCCCCC1CO1
CCCCCCCCCCCCCCCCC(O)CN
null
null
null
Functional Group Addition
OtherReaction
e8f483baa1df50dc51ca71356091d0aab082bd6a57d18118803efcf9c9bd74a4
604c2cde89ba21cccea5848b25fc4ba515e46430643c268de3fdecd95de94a50
null
[C:1]-[C:2]1-[CH2;D2;+0:3]-[O;H0;D2;+0:4]-1>>[C:1]-[C:2](-[OH;D1;+0:4])-[CH2;D2;+0:3]-[N;D1;H2:5]
83.1
[{"value": 83.0, "product": "NCC(CCCCCCCCCCCCCCCC)O", "details": "PERCENTYIELD", "is_desired": false}, {"value": 83.1, "product": "NCC(CCCCCCCCCCCCCCCC)O", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
100
CELSIUS
12
HOUR
A 500-ml flask equipped with a stirrer was charged with 160 g (1.5 mol) of benzylamine, to which 29 g (0.11 mol) of 1,2-epoxyoctadecane were added dropwise over 3 hours while stirring at 100° C. Stirring was conducted further for 12 hours at 100° C. Benzyl alcohol was distilled off under reduced pressure, and the resid...
10.6084/m9.figshare.5104873.v1
null
Ether
Secondary alcohol.Primary amine
C1CO1
null
null
Other
null
100
12
CCCCCCCCCCCCCCCCC1CO1>>CCCCCCCCCCCCCCCCC(O)CN
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-cb7b361a66f24faab6f6db5494adcd1b
C1=COCCC1.CCCCCCCCCCCCCCCCC(O)CO>>CCCCCCCCCCCCCCCCC(O)COC1CCCCO1
C(=O)(O)[O-].[Na+].C(C(CCCCCCCCCCCCCCCC)O)O.C1(=CC=C(C=C1)S(=O)(=O)O)C.O1CCCC=C1>>O1C(CCCC1)OCC(CCCCCCCCCCCCCCCC)O
[CH:21]1=[CH:22][CH2:23][CH2:24][CH2:25][O:26]1.[CH3:1][CH2:2][CH2:3][CH2:4][CH2:5][CH2:6][CH2:7][CH2:8][CH2:9][CH2:10][CH2:11][CH2:12][CH2:13][CH2:14][CH2:15][CH2:16][CH:17]([OH:18])[CH2:19][OH:20]>>[CH3:1][CH2:2][CH2:3][CH2:4][CH2:5][CH2:6][CH2:7][CH2:8][CH2:9][CH2:10][CH2:11][CH2:12][CH2:13][CH2:14][CH2:15][CH2:16][...
C1=COCCC1.CCCCCCCCCCCCCCCCC(O)CO
CCCCCCCCCCCCCCCCC(O)COC1CCCCO1
null
null
ClCCl
Heteroatom Alkylation and Arylation
oxa-Michael addition
abdcab389770d0a73be3b825aa1d56cee234da38dbdf3510fe8104d481e7cf3f
c6a3efa2acb508a32cdf9fcedfcd9635cce0ecdcf12c094b743aa576ea01fd9a
C1CCOCC1
[#8:1]1-[C:2]-[C:3]-[C:4]-[CH;D2;+0:5]=[CH;D2;+0:6]-1.[C:7]-[C:8]-[OH;D1;+0:9]>>[C:7]-[C:8]-[O;H0;D2;+0:9]-[CH;D3;+0:6]1-[#8:1]-[C:2]-[C:3]-[C:4]-[CH2;D2;+0:5]-1
29
[{"value": 29.0, "product": "O1C(CCCC1)OCC(CCCCCCCCCCCCCCCC)O", "details": "PERCENTYIELD", "is_desired": false}, {"value": 28.9, "product": "O1C(CCCC1)OCC(CCCCCCCCCCCCCCCC)O", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
null
null
A 1-liter flask equipped with a stirrer and dropping funnel was charged with 20 g (70 mmol) of octadecane-1,2-diol, 0.7 g (3.5 mmol) of p-toluenesulfonic acid and 350 ml of dichloromethane. While stirring the contents at room temperature, 5.9 g (70 mmol) of dihydropyran were added dropwise. After stirring the mixture a...
10.6084/m9.figshare.5104873.v1
null
Ether.Primary alcohol
Ether.Ether
C1=COCCC1
C1CCOCC1
C1CCOCC1
null
ClCCl
null
null
C1=COCCC1.CCCCCCCCCCCCCCCCC(O)CO>ClCCl>CCCCCCCCCCCCCCCCC(O)COC1CCCCO1
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-c24607cade224f55921e8fa774f3f6f4
COC(=O)CCCCCCCCCCCO.NCC(O)CN>>NCC(O)CNC(=O)CCCCCCCCCCCO
OCCCCCCCCCCCC(=O)OC.NCC(CN)O.N#N>>NCC(CNC(CCCCCCCCCCCO)=O)O
CO[C:7](=[O:8])[CH2:9][CH2:10][CH2:11][CH2:12][CH2:13][CH2:14][CH2:15][CH2:16][CH2:17][CH2:18][CH2:19][OH:20].[NH2:1][CH2:2][CH:3]([OH:4])[CH2:5][NH2:6]>>[NH2:1][CH2:2][CH:3]([OH:4])[CH2:5][NH:6][C:7](=[O:8])[CH2:9][CH2:10][CH2:11][CH2:12][CH2:13][CH2:14][CH2:15][CH2:16][CH2:17][CH2:18][CH2:19][OH:20]
COC(=O)CCCCCCCCCCCO.NCC(O)CN
NCC(O)CNC(=O)CCCCCCCCCCCO
null
C[O-].[Na+]
C1CCOC1
Acylation
Aminolysis of esters
04c54ce22aa9bc0cea0de3d900446bcab51cf02bebeb606fa788a47dcd0e37ff
4335147c9ad02004b7c12428d7eac0b2e7e0e2017adc471d01c387239de8017d
null
C-O-[C;H0;D3;+0:1](=[O;D1;H0:2])-[C:3]-[C:4].[C:5]-[C:6]-[NH2;D1;+0:7]>>[C:4]-[C:3]-[C;H0;D3;+0:1](=[O;D1;H0:2])-[NH;D2;+0:7]-[C:6]-[C:5]
75.7
[{"value": 75.0, "product": "NCC(CNC(CCCCCCCCCCCO)=O)O", "details": "PERCENTYIELD", "is_desired": false}, {"value": 75.7, "product": "NCC(CNC(CCCCCCCCCCCO)=O)O", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
null
null
A 100-ml two-necked flask equipped with a stirrer and dropping funnel was charged with 9.39 g (104 mmol) of 1,3-diamino-2-propanol and 0.047 g (0.87 mmol) of sodium methoxide. While heating and stirring the contents at 80° C. in an N2 atmosphere, a THF solution of 4.00 g (17.4 mmol) of methyl 12-hydroxydodecanate was a...
10.6084/m9.figshare.5104873.v1
null
Ester.Primary amine
Secondary amide
null
null
null
HO-
C[O-].[Na+].C1CCOC1
null
null
COC(=O)CCCCCCCCCCCO.NCC(O)CN>C[O-].[Na+].C1CCOC1>NCC(O)CNC(=O)CCCCCCCCCCCO
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-5222a695140643c8a668e63555fad359
CC1(C)CCC(C)(C)c2cc3cc(Br)ccc3cc21.CCOC(=O)c1csc(Br)c1>>CCOC(=O)c1csc(-c2ccc3cc4c(cc3c2)C(C)(C)CCC4(C)C)c1
CC1(C=2C=C3C=CC(=CC3=CC2C(CC1)(C)C)Br)C.[Mg].BrC=1SC=C(C1)C(=O)OCC>>CC1(C=2C=C3C=CC(=CC3=CC2C(CC1)(C)C)C=1SC=C(C1)C(=O)OCC)C
Br[c:10]1[cH:11][cH:12][c:13]2[cH:14][c:15]3[c:16]([cH:17][c:18]2[cH:19]1)[C:20]([CH3:21])([CH3:22])[CH2:23][CH2:24][C:25]3([CH3:26])[CH3:27].Br[c:9]1[s:8][cH:7][c:6]([C:4]([O:3][CH2:2][CH3:1])=[O:5])[cH:28]1>>[CH3:1][CH2:2][O:3][C:4](=[O:5])[c:6]1[cH:7][s:8][c:9](-[c:10]2[cH:11][cH:12][c:13]3[cH:14][c:15]4[c:16]([cH:1...
CC1(C)CCC(C)(C)c2cc3cc(Br)ccc3cc21.CCOC(=O)c1csc(Br)c1
CCOC(=O)c1csc(-c2ccc3cc4c(cc3c2)C(C)(C)CCC4(C)C)c1
null
Cl[Ni]Cl.CCN(CC)CCOC=1C=CC(=CC1)CC=2C=CC=CC2.Cl.[Cl-].[Zn+2].[Cl-]
C1CCOC1
C-C Coupling
Negishi
f674f2dc28578b12b308e7cbd9921fcbada13b86e3e7229d39e6fd04933df713
a7a4ce9a92e2f8a62d28956a69a5cc384426ab72416e87d68c6a3feb23c22d66
c1csc(-c2ccc3cc4c(cc3c2)CCCC4)c1
Br-[c;H0;D3;+0:1](:[c:2]:[c:3]):[c:4]:[c:5].Br-[c;H0;D3;+0:6]1:[#16;a:7]:[c:8]:[c:9](-[C:10](-[#8:11])=[O;D1;H0:12]):[c:13]:1>>[#8:11]-[C:10](=[O;D1;H0:12])-[c:9]1:[c:13]:[c;H0;D3;+0:6](-[c;H0;D3;+0:1](:[c:2]:[c:3]):[c:4]:[c:5]):[#16;a:7]:[c:8]:1
null
[]
null
null
1
HOUR
A solution of 9.5 g (30 mmol) of 5,6,7,8-tetrahydro-5,5,8,8-tetramethyl-2-bromoanthracene was added dropwise to a suspension of 724 mg (30 mmol) of magnesium in 10 ml of THF. Once the addition was completed, the mixture was heated at reflux for one hour. At room temperature 4.1 g (30 mmol) of anhydrous zinc chloride we...
10.6084/m9.figshare.5104873.v1
null
Aromatic halide.Aromatic halide
null
c1ccc2cc3c(cc2c1)CCCC3.c1ccsc1
c1ccsc1.c1ccc2cc3c(cc2c1)CCCC3
c1ccsc1.c1ccc2cc3c(cc2c1)CCCC3
Br-
Cl[Ni]Cl.CCN(CC)CCOC=1C=CC(=CC1)CC=2C=CC=CC2.Cl.[Cl-].[Zn+2].[Cl-].C1CCOC1
null
1
CC1(C)CCC(C)(C)c2cc3cc(Br)ccc3cc21.CCOC(=O)c1csc(Br)c1>Cl[Ni]Cl.CCN(CC)CCOC=1C=CC(=CC1)CC=2C=CC=CC2.Cl.[Cl-].[Zn+2].[Cl-].C1CCOC1>CCOC(=O)c1csc(-c2ccc3cc4c(cc3c2)C(C)(C)CCC4(C)C)c1
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-66e0b8dbf3514265bd84740660b01c23
CCOC(=O)c1csc(-c2ccc3cc4c(cc3c2)C(C)(C)CCC4(C)C)c1>>CC1(C)CCC(C)(C)c2cc3cc(-c4cc(C(=O)O)cs4)ccc3cc21
CC1(C=2C=C3C=CC(=CC3=CC2C(CC1)(C)C)C=1SC=C(C1)C(=O)OCC)C.[OH-].[Na+]>>CC1(C=2C=C3C=CC(=CC3=CC2C(CC1)(C)C)C=1SC=C(C1)C(=O)O)C
CC[O:19][C:17]([c:16]1[cH:15][c:14](-[c:13]2[cH:12][c:11]3[cH:10][c:9]4[c:26]([cH:25][c:24]3[cH:23][cH:22]2)[C:2]([CH3:1])([CH3:3])[CH2:4][CH2:5][C:6]4([CH3:7])[CH3:8])[s:21][cH:20]1)=[O:18]>>[CH3:1][C:2]1([CH3:3])[CH2:4][CH2:5][C:6]([CH3:7])([CH3:8])[c:9]2[cH:10][c:11]3[cH:12][c:13](-[c:14]4[cH:15][c:16]([C:17](=[O:18...
CCOC(=O)c1csc(-c2ccc3cc4c(cc3c2)C(C)(C)CCC4(C)C)c1
CC1(C)CCC(C)(C)c2cc3cc(-c4cc(C(=O)O)cs4)ccc3cc21
null
null
null
Deprotection
Ester saponification (alkyl deprotection)
d872e08ad5c85a4add6cd04e6e987e73fead5f79b3f30ba61a81ba5029b29894
38ae1ee78433b9acfb0390501446149c80f88f23ac2d84c60b3369bdab75cec9
c1csc(-c2ccc3cc4c(cc3c2)CCCC4)c1
C-C-[O;H0;D2;+0:1]-[C:2](=[O;D1;H0:3])-[c:4]:[c:5]:[#16;a:6]>>[#16;a:6]:[c:5]:[c:4]-[C:2](=[O;D1;H0:3])-[OH;D1;+0:1]
null
[]
null
null
null
null
6.3 g (16 mmol) of the ester prepared in Example 1 and 100 ml of a 2N methanolic sodium hydroxide solution were introduced into a round-bottomed flask and the mixture was heated at reflux for one hour. The reaction medium was evaporated to dryness, the residue taken up in water, acidified to pH 1 with concentrated hydr...
10.6084/m9.figshare.5104873.v1
null
Ester
Carboxylic acid
null
null
c1ccc2cc3c(cc2c1)CCCC3.c1ccsc1
Other
null
null
null
CCOC(=O)c1csc(-c2ccc3cc4c(cc3c2)C(C)(C)CCC4(C)C)c1>>CC1(C)CCC(C)(C)c2cc3cc(-c4cc(C(=O)O)cs4)ccc3cc21
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-1c0764d0c4c24228988989f273084ebb
O=C(Cl)C(Cl)(Cl)Cl.c1cc[nH]c1>>O=C(c1ccc[nH]1)C(Cl)(Cl)Cl
C([O-])([O-])=O.[K+].[K+].ClC(C(=O)Cl)(Cl)Cl.N1C=CC=C1>>ClC(C(=O)C=1NC=CC1)(Cl)Cl
Cl[C:2](=[O:1])[C:8]([Cl:9])([Cl:10])[Cl:11].[cH:3]1[cH:4][cH:5][cH:6][nH:7]1>>[O:1]=[C:2]([c:3]1[cH:4][cH:5][cH:6][nH:7]1)[C:8]([Cl:9])([Cl:10])[Cl:11]
O=C(Cl)C(Cl)(Cl)Cl.c1cc[nH]c1
O=C(c1ccc[nH]1)C(Cl)(Cl)Cl
null
null
O.C(C)OCC
C-C Coupling
Friedel-Crafts acylation
701d21b652ce6d90463464dd21d4d87caf603bff2f60e1ad8fa59cfd59145f4f
fe2a4a0dfbb5b71b9a065e092364c64b22b4eb1ad4d6ba2a1e8edc9d31fce3e4
c1cc[nH]c1
Cl-[C;H0;D3;+0:1](=[O;D1;H0:2])-[C:3](-[Cl;D1;H0:4])(-[Cl;D1;H0:5])-[Cl;D1;H0:6].[#7;a:7]1:[c:8]:[c:9]:[c:10]:[cH;D2;+0:11]:1>>[Cl;D1;H0:4]-[C:3](-[Cl;D1;H0:5])(-[Cl;D1;H0:6])-[C;H0;D3;+0:1](=[O;D1;H0:2])-[c;H0;D3;+0:11]1:[#7;a:7]:[c:8]:[c:9]:[c:10]:1
null
[]
null
null
1
HOUR
45 g (247 mmol) of trichloroacetyl chloride and 100 ml of ethyl ether were introduced into a three-necked flask. A solution of 15.4 g (230 mmol) of pyrrole in 100 ml of ethyl ether was added dropwise and the mixture was stirred at room temperature for one hour, then a solution of 20 g of potassium carbonate in 60 ml of...
10.6084/m9.figshare.5104873.v1
null
Acyl halide
Ketone
c1cc[nH]c1
c1cc[nH]c1
c1cc[nH]c1
HCl
O.C(C)OCC
null
1
O=C(Cl)C(Cl)(Cl)Cl.c1cc[nH]c1>O.C(C)OCC>O=C(c1ccc[nH]1)C(Cl)(Cl)Cl
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-2f9353d568ba495d9d6fa8a66d2c0875
CO.O=C(c1cc(I)c[nH]1)C(Cl)(Cl)Cl>>COC(=O)c1cc(I)c[nH]1
IC=1C=C(NC1)C(C(Cl)(Cl)Cl)=O.CO.C[O-].[Na+]>>IC=1C=C(NC1)C(=O)OC
[CH3:1][OH:2].ClC(Cl)(Cl)[C:3](=[O:4])[c:5]1[cH:6][c:7]([I:8])[cH:9][nH:10]1>>[CH3:1][O:2][C:3](=[O:4])[c:5]1[cH:6][c:7]([I:8])[cH:9][nH:10]1
CO.O=C(c1cc(I)c[nH]1)C(Cl)(Cl)Cl
COC(=O)c1cc(I)c[nH]1
null
null
O.C(C)OCC
Acylation
OtherReaction
bb2341d143935ccc8065bdd4084fedbad20e7f48b8013bb1e9d80700631fc60c
23a2adf82de85a40ec60d39fbe3e80820c3a8dd06055de3d3c5fde7651211013
c1cc[nH]c1
Cl-C(-Cl)(-Cl)-[C;H0;D3;+0:1](=[O;D1;H0:2])-[c:3](:[c:4]):[#7;a:5]:[c:6].[C;D1;H3:7]-[OH;D1;+0:8]>>[C;D1;H3:7]-[O;H0;D2;+0:8]-[C;H0;D3;+0:1](=[O;D1;H0:2])-[c:3](:[c:4]):[#7;a:5]:[c:6]
null
[]
null
null
4
HOUR
8.2 g (24 mmol) of 4-iodo-2-trichloroacetylpyrrole and 100 ml of methanol were introduced into a round-bottomed flask and 2 g (36 mmol) of sodium methoxide were added. The mixture was stirred at room temperature for four hours, the reaction medium evaporated to dryness, and the residue obtained taken up in water and et...
10.6084/m9.figshare.5104873.v1
null
Trichloro group.Ketone.Methanol
Ester
null
null
c1cc[nH]c1
HCl
O.C(C)OCC
null
4
CO.O=C(c1cc(I)c[nH]1)C(Cl)(Cl)Cl>O.C(C)OCC>COC(=O)c1cc(I)c[nH]1
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-8254c501c8dc491b8f88eae119f49eae
CI.COC(=O)c1cc(I)c[nH]1>>COC(=O)c1cc(I)cn1C
O.[H-].[Na+].IC=1C=C(NC1)C(=O)OC.IC>>CN1C(=CC(=C1)I)C(=O)OC
I[CH3:11].[CH3:1][O:2][C:3](=[O:4])[c:5]1[cH:6][c:7]([I:8])[cH:9][nH:10]1>>[CH3:1][O:2][C:3](=[O:4])[c:5]1[cH:6][c:7]([I:8])[cH:9][n:10]1[CH3:11]
CI.COC(=O)c1cc(I)c[nH]1
COC(=O)c1cc(I)cn1C
null
null
CN(C)C=O
Heteroatom Alkylation and Arylation
N-alkylation of secondary amines with alkyl halides
9ead09c93a8a9d57f887a48202e25076c1ec25be9e5b61e0648504d88c26cda6
7a358c636daddc97c1fb4c29f378044d7eac3f01815d9966e599841f642d631a
c1cc[nH]c1
I-[CH3;D1;+0:1].[C;D1;H3:2]-[#8:3]-[C:4](=[O;D1;H0:5])-[c:6]1:[c:7]:[c:8]:[c:9]:[nH;D2;+0:10]:1>>[C;D1;H3:2]-[#8:3]-[C:4](=[O;D1;H0:5])-[c:6]1:[c:7]:[c:8]:[c:9]:[n;H0;D3;+0:10]:1-[CH3;D1;+0:1]
null
[]
null
null
null
null
780 mg (25.9 mmol) of sodium hydride (80% in oil) and 20 ml of DMF were introduced into a three-necked flask, a solution of 6.5 g (25.9 mmol) of methyl 4-iodo-2-pyrrolecarboxylate in 50 ml of DMF was added dropwise and the mixture was stirred until gaseous emission ceased. 2.1 ml (33.6 mmol) of iodomethane were then ad...
10.6084/m9.figshare.5104873.v1
null
null
null
c1cc[nH]c1
c1cc[nH]c1
c1cc[nH]c1
HI
CN(C)C=O
null
null
CI.COC(=O)c1cc(I)c[nH]1>CN(C)C=O>COC(=O)c1cc(I)cn1C
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-205c29c6463642c4a3ef2726db5ff6fc
CC1(C)CCC(C)(C)c2cc3cc(B(O)O)ccc3cc21.COC(=O)c1cc(I)cn1C>>COC(=O)c1cc(-c2ccc3cc4c(cc3c2)C(C)(C)CCC4(C)C)cn1C
CC1(C=2C=C3C=CC(=CC3=CC2C(CC1)(C)C)B(O)O)C.C([O-])([O-])=O.[K+].[K+].CN1C(=CC(=C1)I)C(=O)OC>>CN1C(=CC(=C1)C1=CC2=CC=3C(CCC(C3C=C2C=C1)(C)C)(C)C)C(=O)OC
OB(O)[c:8]1[cH:9][cH:10][c:11]2[cH:12][c:13]3[c:14]([cH:15][c:16]2[cH:17]1)[C:18]([CH3:19])([CH3:20])[CH2:21][CH2:22][C:23]3([CH3:24])[CH3:25].I[c:7]1[cH:6][c:5]([C:3]([O:2][CH3:1])=[O:4])[n:27]([CH3:28])[cH:26]1>>[CH3:1][O:2][C:3](=[O:4])[c:5]1[cH:6][c:7](-[c:8]2[cH:9][cH:10][c:11]3[cH:12][c:13]4[c:14]([cH:15][c:16]3[...
CC1(C)CCC(C)(C)c2cc3cc(B(O)O)ccc3cc21.COC(=O)c1cc(I)cn1C
COC(=O)c1cc(-c2ccc3cc4c(cc3c2)C(C)(C)CCC4(C)C)cn1C
null
null
C1(=CC=CC=C1)C
C-C Coupling
Suzuki coupling with boronic acids
1ae6c8ac07df41724f89d3a167e7b6589b8a63a41abe6b2b281e91283bac64b7
08d2969413ef1a2cd5b43667268ba178160c7b55545bf48018e31f2b019632ec
c1cc(-c2ccc3cc4c(cc3c2)CCCC4)c[nH]1
I-[c;H0;D3;+0:1]1:[c:2]:[#7;a:3](-[C;D1;H3:4]):[c:5](-[C:6](-[#8:7])=[O;D1;H0:8]):[c:9]:1.O-B(-O)-[c;H0;D3;+0:10](:[c:11]:[c:12]):[c:13]:[c:14]>>[#8:7]-[C:6](=[O;D1;H0:8])-[c:5]1:[c:9]:[c;H0;D3;+0:1](-[c;H0;D3;+0:10](:[c:11]:[c:12]):[c:13]:[c:14]):[c:2]:[#7;a:3]:1-[C;D1;H3:4]
47
[{"value": 47.0, "product": "CN1C(=CC(=C1)C1=CC2=CC=3C(CCC(C3C=C2C=C1)(C)C)(C)C)C(=O)OC", "details": "PERCENTYIELD", "is_desired": false}, {"value": 33.9, "product": "CN1C(=CC(=C1)C1=CC2=CC=3C(CCC(C3C=C2C=C1)(C)C)(C)C)C(=O)OC", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
20
MINUTE
231 mg (0.2 mml) of tetrakis-(triphenylphosphine)palladium (0), 50 ml of toluene and 1.75 g (6.6 mmol) of methyl N-methyl-4-iodo-2-pyrrolecarboxylate were introduced into a three-necked flask and under a nitrogen stream and the mixture was stirred at room temperature for 20 minutes. 2.8 g (10 mmol) of 5,6,7,8-tetrahydr...
10.6084/m9.figshare.5104873.v1
null
Aromatic halide.Boronic acid
null
c1ccc2cc3c(cc2c1)CCCC3.c1cc[nH]c1
c1cc[nH]c1.c1ccc2cc3c(cc2c1)CCCC3
c1cc[nH]c1.c1ccc2cc3c(cc2c1)CCCC3
HI.B
C1(=CC=CC=C1)C
null
0.333333
CC1(C)CCC(C)(C)c2cc3cc(B(O)O)ccc3cc21.COC(=O)c1cc(I)cn1C>C1(=CC=CC=C1)C>COC(=O)c1cc(-c2ccc3cc4c(cc3c2)C(C)(C)CCC4(C)C)cn1C
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-d9af6adb5c534d1a86a82222f63dd4ec
CI.COC(=O)c1ccc(-c2ccc3cc4c(cc3c2)C(C)(C)CCC4(C)C)cc1O>>COC(=O)c1ccc(-c2ccc3cc4c(cc3c2)C(C)(C)CCC4(C)C)cc1OC
O.[H-].[Na+].OC1=C(C(=O)OC)C=CC(=C1)C1=CC2=CC=3C(CCC(C3C=C2C=C1)(C)C)(C)C.IC>>COC1=C(C(=O)OC)C=CC(=C1)C1=CC2=CC=3C(CCC(C3C=C2C=C1)(C)C)(C)C
I[CH3:30].[CH3:1][O:2][C:3](=[O:4])[c:5]1[cH:6][cH:7][c:8](-[c:9]2[cH:10][cH:11][c:12]3[cH:13][c:14]4[c:15]([cH:16][c:17]3[cH:18]2)[C:19]([CH3:20])([CH3:21])[CH2:22][CH2:23][C:24]4([CH3:25])[CH3:26])[cH:27][c:28]1[OH:29]>>[CH3:1][O:2][C:3](=[O:4])[c:5]1[cH:6][cH:7][c:8](-[c:9]2[cH:10][cH:11][c:12]3[cH:13][c:14]4[c:15](...
CI.COC(=O)c1ccc(-c2ccc3cc4c(cc3c2)C(C)(C)CCC4(C)C)cc1O
COC(=O)c1ccc(-c2ccc3cc4c(cc3c2)C(C)(C)CCC4(C)C)cc1OC
null
null
CN(C)C=O
Heteroatom Alkylation and Arylation
Williamson Ether Synthesis
b8b041187bac58376aae824630608e7deb49a01db3d652291f8b379c10d4e434
0f0966e3597a58033417ecee71659f4d0c082f95d46b1e52c95541e6e4a59086
c1ccc(-c2ccc3cc4c(cc3c2)CCCC4)cc1
I-[CH3;D1;+0:1].[#8:2]-[C:3](=[O;D1;H0:4])-[c:5]:[c:6](-[OH;D1;+0:7]):[c:8]>>[#8:2]-[C:3](=[O;D1;H0:4])-[c:5]:[c:6](-[O;H0;D2;+0:7]-[CH3;D1;+0:1]):[c:8]
null
[]
null
null
null
null
130 mg (4.2 mmol) of sodium hydride (80% in oil) and 20 ml of DMF were introduced into a three-necked flask, a solution of 1.6 g (4.2 mmol) of methyl 2-hydroxy-4-(5,6,7,8-tetrahydro-5,5,8,8-tetramethyl-2-anthryl)benzoate in 50 ml of DMF was added dropwise and the mixture was stirred until gaseous emission ceased. 340 μ...
10.6084/m9.figshare.5104873.v1
null
Aromatic alcohol
Ether
null
null
c1ccccc1.c1ccc2cc3c(cc2c1)CCCC3
HI
CN(C)C=O
null
null
CI.COC(=O)c1ccc(-c2ccc3cc4c(cc3c2)C(C)(C)CCC4(C)C)cc1O>CN(C)C=O>COC(=O)c1ccc(-c2ccc3cc4c(cc3c2)C(C)(C)CCC4(C)C)cc1OC
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-b7fc3759f58e4209a7cf0781050443b3
BrCc1ccccc1.Oc1cc2ccc(Br)cc2cc1C12CC3CC(CC(C3)C1)C2>>Brc1ccc2cc(OCc3ccccc3)c(C34CC5CC(CC(C5)C3)C4)cc2c1
C12(CC3CC(CC(C1)C3)C2)C2=C(C=C3C=CC(=CC3=C2)Br)O.C(C1=CC=CC=C1)Br>>C12(CC3CC(CC(C1)C3)C2)C2=C(C=C3C=CC(=CC3=C2)Br)OCC2=CC=CC=C2
Br[CH2:9][c:10]1[cH:11][cH:12][cH:13][cH:14][cH:15]1.[Br:1][c:2]1[cH:3][cH:4][c:5]2[cH:6][c:7]([OH:8])[c:16]([C:17]34[CH2:18][CH:19]5[CH2:20][CH:21]([CH2:22][CH:23]([CH2:24]5)[CH2:25]3)[CH2:26]4)[cH:27][c:28]2[cH:29]1>>[Br:1][c:2]1[cH:3][cH:4][c:5]2[cH:6][c:7]([O:8][CH2:9][c:10]3[cH:11][cH:12][cH:13][cH:14][cH:15]3)[c:...
BrCc1ccccc1.Oc1cc2ccc(Br)cc2cc1C12CC3CC(CC(C3)C1)C2
Brc1ccc2cc(OCc3ccccc3)c(C34CC5CC(CC(C5)C3)C4)cc2c1
null
null
null
Heteroatom Alkylation and Arylation
Williamson Ether Synthesis
7e1040116e3a4cf0e8ec5cc7865388d9cd0efabce6d320a1c25a36e411018d8b
d5f4610d46ccc0478471c5bc0fb862644eaf764bbc5d93badb39d54f6ec8e0a5
c1ccc(COc2cc3ccccc3cc2C23CC4CC(CC(C4)C2)C3)cc1
Br-[CH2;D2;+0:1]-[c:2](:[c:3]):[c:4].[OH;D1;+0:5]-[c:6](:[c:7]):[c:8]>>[c:3]:[c:2](-[CH2;D2;+0:1]-[O;H0;D2;+0:5]-[c:6](:[c:7]):[c:8]):[c:4]
80
[{"value": 80.0, "product": "C12(CC3CC(CC(C1)C3)C2)C2=C(C=C3C=CC(=CC3=C2)Br)OCC2=CC=CC=C2", "details": "PERCENTYIELD", "is_desired": false}, {"value": 79.8, "product": "C12(CC3CC(CC(C1)C3)C2)C2=C(C=C3C=CC(=CC3=C2)Br)OCC2=CC=CC=C2", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
null
null
Following the basic procedure of Example 11, by reacting 12.5 g (35 mmol) of 7-(1-adamantyl)-6-hydroxy-2-bromonaphthalene with 5 ml (42 mmol) of benzyl bromide, 12.5 g (80%) of the expected compound of melting point 150°-151° C. were obtained. Conditions: See reaction.notes.procedure_details.
10.6084/m9.figshare.5104873.v1
null
Primary halide.Aromatic alcohol
Ether
null
null
c1ccc2ccccc2c1.c1ccccc1.C1C2CC3CC1CC(C2)C3
HBr
null
null
null
BrCc1ccccc1.Oc1cc2ccc(Br)cc2cc1C12CC3CC(CC(C3)C1)C2>>Brc1ccc2cc(OCc3ccccc3)c(C34CC5CC(CC(C5)C3)C4)cc2c1
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-0bc171163cc04932b98554480b9c571f
COC(=O)c1ccc(I)cc1O.OB(O)c1ccc2cc(OCc3ccccc3)c(C34CC5CC(CC(C5)C3)C4)cc2c1>>COC(=O)c1ccc(-c2ccc3cc(OCc4ccccc4)c(C45CC6CC(CC(C6)C4)C5)cc3c2)cc1O
C12(CC3CC(CC(C1)C3)C2)C2=C(C=C3C=CC(=CC3=C2)B(O)O)OCC2=CC=CC=C2.OC1=C(C(=O)OC)C=CC(=C1)I>>OC1=C(C(=O)OC)C=CC(=C1)C1=CC2=CC(=C(C=C2C=C1)OCC1=CC=CC=C1)C12CC3CC(CC(C1)C3)C2
I[c:8]1[cH:7][cH:6][c:5]([C:3]([O:2][CH3:1])=[O:4])[c:38]([OH:39])[cH:37]1.OB(O)[c:9]1[cH:10][cH:11][c:12]2[cH:13][c:14]([O:15][CH2:16][c:17]3[cH:18][cH:19][cH:20][cH:21][cH:22]3)[c:23]([C:24]34[CH2:25][CH:26]5[CH2:27][CH:28]([CH2:29][CH:30]([CH2:31]5)[CH2:32]3)[CH2:33]4)[cH:34][c:35]2[cH:36]1>>[CH3:1][O:2][C:3](=[O:4]...
COC(=O)c1ccc(I)cc1O.OB(O)c1ccc2cc(OCc3ccccc3)c(C34CC5CC(CC(C5)C3)C4)cc2c1
COC(=O)c1ccc(-c2ccc3cc(OCc4ccccc4)c(C45CC6CC(CC(C6)C4)C5)cc3c2)cc1O
null
null
null
C-C Coupling
Suzuki coupling with boronic acids
44300e12668e13575bd83146e75f4d99efe4beab23be02dbe4dd7587e7e6a7cd
08d2969413ef1a2cd5b43667268ba178160c7b55545bf48018e31f2b019632ec
c1ccc(COc2cc3ccc(-c4ccccc4)cc3cc2C23CC4CC(CC(C4)C2)C3)cc1
I-[c;H0;D3;+0:1](:[c:2]:[c:3]):[c:4]:[c:5].O-B(-O)-[c;H0;D3;+0:6](:[c:7]:[c:8]):[c:9]:[c:10]>>[c:8]:[c:7]:[c;H0;D3;+0:6](-[c;H0;D3;+0:1](:[c:2]:[c:3]):[c:4]:[c:5]):[c:9]:[c:10]
36.2
[{"value": 36.0, "product": "OC1=C(C(=O)OC)C=CC(=C1)C1=CC2=CC(=C(C=C2C=C1)OCC1=CC=CC=C1)C12CC3CC(CC(C1)C3)C2", "details": "PERCENTYIELD", "is_desired": false}, {"value": 36.2, "product": "OC1=C(C(=O)OC)C=CC(=C1)C1=CC2=CC(=C(C=C2C=C1)OCC1=CC=CC=C1)C12CC3CC(CC(C1)C3)C2", "details": "CALCULATEDPERCENTYIELD", "is_desired":...
null
null
null
null
Following the basic procedure of Example 7(f), by reacting 5.52 g (13.4 mmol) of 7-(1-adamantyl)-6-benzyloxy-2-naphthylboronic acid with 2.46 g (8.8 mmol) of methyl 2-hydroxy-4-iodobenzoate, 1.65 g (36%) of the expected compound was obtained. Conditions: See reaction.notes.procedure_details.
10.6084/m9.figshare.5104873.v1
null
Aromatic halide.Boronic acid
null
c1ccccc1.c1ccc2ccccc2c1
c1ccccc1.c1ccc2ccccc2c1
c1ccccc1.c1ccc2ccccc2c1.c1ccccc1.C1C2CC3CC1CC(C2)C3
HI.B
null
null
null
COC(=O)c1ccc(I)cc1O.OB(O)c1ccc2cc(OCc3ccccc3)c(C34CC5CC(CC(C5)C3)C4)cc2c1>>COC(=O)c1ccc(-c2ccc3cc(OCc4ccccc4)c(C45CC6CC(CC(C6)C4)C5)cc3c2)cc1O
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-dbade7089fdb4aeda06e0dbd6d0e1ec8
CCCCCCI.COC(=O)c1ccc(-c2ccc3cc(O)c(C45CC6CC(CC(C6)C4)C5)cc3c2)cc1O>>CCCCCCOc1cc2ccc(-c3ccc(C(=O)OC)c(O)c3)cc2cc1C12CC3CC(CC(C3)C1)C2
OC1=C(C(=O)OC)C=CC(=C1)C1=CC2=CC(=C(C=C2C=C1)O)C12CC3CC(CC(C1)C3)C2.ICCCCCC>>OC1=C(C(=O)OC)C=CC(=C1)C1=CC2=CC(=C(C=C2C=C1)OCCCCCC)C12CC3CC(CC(C1)C3)C2
I[CH2:6][CH2:5][CH2:4][CH2:3][CH2:2][CH3:1].[OH:7][c:8]1[cH:9][c:10]2[cH:11][cH:12][c:13](-[c:14]3[cH:15][cH:16][c:17]([C:18](=[O:19])[O:20][CH3:21])[c:22]([OH:23])[cH:24]3)[cH:25][c:26]2[cH:27][c:28]1[C:29]12[CH2:30][CH:31]3[CH2:32][CH:33]([CH2:34][CH:35]([CH2:36]3)[CH2:37]1)[CH2:38]2>>[CH3:1][CH2:2][CH2:3][CH2:4][CH2...
CCCCCCI.COC(=O)c1ccc(-c2ccc3cc(O)c(C45CC6CC(CC(C6)C4)C5)cc3c2)cc1O
CCCCCCOc1cc2ccc(-c3ccc(C(=O)OC)c(O)c3)cc2cc1C12CC3CC(CC(C3)C1)C2
null
null
null
Heteroatom Alkylation and Arylation
Williamson Ether Synthesis
7e1040116e3a4cf0e8ec5cc7865388d9cd0efabce6d320a1c25a36e411018d8b
d5f4610d46ccc0478471c5bc0fb862644eaf764bbc5d93badb39d54f6ec8e0a5
c1ccc(-c2ccc3ccc(C45CC6CC(CC(C6)C4)C5)cc3c2)cc1
I-[CH2;D2;+0:1]-[C:2]-[C:3].[OH;D1;+0:4]-[c:5](:[c:6]):[c:7]>>[C:3]-[C:2]-[CH2;D2;+0:1]-[O;H0;D2;+0:4]-[c:5](:[c:6]):[c:7]
55
[{"value": 55.0, "product": "OC1=C(C(=O)OC)C=CC(=C1)C1=CC2=CC(=C(C=C2C=C1)OCCCCCC)C12CC3CC(CC(C1)C3)C2", "details": "PERCENTYIELD", "is_desired": false}, {"value": 54.6, "product": "OC1=C(C(=O)OC)C=CC(=C1)C1=CC2=CC(=C(C=C2C=C1)OCCCCCC)C12CC3CC(CC(C1)C3)C2", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
null
null
Following the basic procedure of Example 11, by reacting 430 mg (1 mmol) of methyl 2-hydroxy-4-[7-(1-adamantyl)-6-hydroxy-2-naphthyl]benzoate with 180 μl (1.2 mmol) of 6-iodohexane, 280 mg (55%) of methyl 2-hydroxy-4-[7-(1-adamantyl)-6-hexyloxy-2-naphthyl]benzoate were obtained. Conditions: See reaction.notes.procedure...
10.6084/m9.figshare.5104873.v1
null
Primary halide.Aromatic alcohol
Ether
null
null
c1ccc2ccccc2c1.c1ccccc1.C1C2CC3CC1CC(C2)C3
HI
null
null
null
CCCCCCI.COC(=O)c1ccc(-c2ccc3cc(O)c(C45CC6CC(CC(C6)C4)C5)cc3c2)cc1O>>CCCCCCOc1cc2ccc(-c3ccc(C(=O)OC)c(O)c3)cc2cc1C12CC3CC(CC(C3)C1)C2
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-9a85735f44d44b4dad4458afbbf407f8
COC(=O)c1ccc(-c2ccc3cc(O)c(C45CC6CC(CC(C6)C4)C5)cc3c2)cc1.COCCOCCl>>COCCOCOc1cc2ccc(-c3ccc(C(=O)OC)cc3)cc2cc1C12CC3CC(CC(C3)C1)C2
C12(CC3CC(CC(C1)C3)C2)C2=C(C=C3C=CC(=CC3=C2)C2=CC=C(C(=O)OC)C=C2)O.COCCOCCl>>C12(CC3CC(CC(C1)C3)C2)C2=C(C=C3C=CC(=CC3=C2)C2=CC=C(C(=O)OC)C=C2)OCOCCOC
[OH:7][c:8]1[cH:9][c:10]2[cH:11][cH:12][c:13](-[c:14]3[cH:15][cH:16][c:17]([C:18](=[O:19])[O:20][CH3:21])[cH:22][cH:23]3)[cH:24][c:25]2[cH:26][c:27]1[C:28]12[CH2:29][CH:30]3[CH2:31][CH:32]([CH2:33][CH:34]([CH2:35]3)[CH2:36]1)[CH2:37]2.Cl[CH2:6][O:5][CH2:4][CH2:3][O:2][CH3:1]>>[CH3:1][O:2][CH2:3][CH2:4][O:5][CH2:6][O:7]...
COC(=O)c1ccc(-c2ccc3cc(O)c(C45CC6CC(CC(C6)C4)C5)cc3c2)cc1.COCCOCCl
COCCOCOc1cc2ccc(-c3ccc(C(=O)OC)cc3)cc2cc1C12CC3CC(CC(C3)C1)C2
null
null
null
Heteroatom Alkylation and Arylation
Williamson Ether Synthesis
6e90ffbf0683e1a3ee55c5e3ea453aefc5ddd369c0150ed0150f9546d7e47f4f
efd670663709b79afcad1306da9f69b33a0147cfa3639ca4c0b54b35ef4b1852
c1ccc(-c2ccc3ccc(C45CC6CC(CC(C6)C4)C5)cc3c2)cc1
Cl-[CH2;D2;+0:1]-[#8:2]-[C:3].[OH;D1;+0:4]-[c:5](:[c:6]):[c:7]>>[C:3]-[#8:2]-[CH2;D2;+0:1]-[O;H0;D2;+0:4]-[c:5](:[c:6]):[c:7]
55
[{"value": 55.0, "product": "C12(CC3CC(CC(C1)C3)C2)C2=C(C=C3C=CC(=CC3=C2)C2=CC=C(C(=O)OC)C=C2)OCOCCOC", "details": "PERCENTYIELD", "is_desired": false}, {"value": 54.1, "product": "C12(CC3CC(CC(C1)C3)C2)C2=C(C=C3C=CC(=CC3=C2)C2=CC=C(C(=O)OC)C=C2)OCOCCOC", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
null
null
Following the basic procedure of Example 12, by reacting 980 mg (2.4 mmol) of methyl 4-[7-(1-adamantyl)-6-hydroxy-2-naphthyl]benzoate with 330 μl (28.6 mmol) of methoxyethoxymethyl chloride, 650 mg (55%) of the expected compound were obtained in the form of an oil. Conditions: See reaction.notes.procedure_details.
10.6084/m9.figshare.5104873.v1
null
Primary halide.Ether.Aromatic alcohol
Ether.Ether
null
null
c1ccc2ccccc2c1.c1ccccc1.C1C2CC3CC1CC(C2)C3
HCl
null
null
null
COC(=O)c1ccc(-c2ccc3cc(O)c(C45CC6CC(CC(C6)C4)C5)cc3c2)cc1.COCCOCCl>>COCCOCOc1cc2ccc(-c3ccc(C(=O)OC)cc3)cc2cc1C12CC3CC(CC(C3)C1)C2
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-af764768aabb4d659aa7d8d3f6f94944
Cc1cc(C(=O)O)ccc1N.[I-]>>Cc1cc(C(=O)O)ccc1I
[I-].[K+].S(O)(O)(=O)=O.N(=O)[O-].[Na+].CC=1C=C(C(=O)O)C=CC1N.S(O)(O)(=O)=O>>CC=1C=C(C(=O)O)C=CC1I
N[c:10]1[c:2]([CH3:1])[cH:3][c:4]([C:5](=[O:6])[OH:7])[cH:8][cH:9]1.[I-:11]>>[CH3:1][c:2]1[cH:3][c:4]([C:5](=[O:6])[OH:7])[cH:8][cH:9][c:10]1[I:11]
Cc1cc(C(=O)O)ccc1N.[I-]
Cc1cc(C(=O)O)ccc1I
null
[Cu](I)I
O.C(C)(=O)OCC
Functional Group Interconversion
OtherReaction
f4fea6a3c7b007f3829d29d893f3499a4094808c0f3b2211f4c3483919a690d8
9c224743a26d9e1c3135e4817dd611aec414d8ea156f02200a3aef865be78b01
c1ccccc1
N-[c;H0;D3;+0:1](:[c:2]:[c:3]):[c:4](-[C;D1;H3:5]):[c:6].[I-;H0;D0:7]>>[C;D1;H3:5]-[c:4](:[c:6]):[c;H0;D3;+0:1](-[I;H0;D1;+0:7]):[c:2]:[c:3]
null
[]
null
null
2
HOUR
20 g (0.132 mol) of 3-methyl-4-aminobenzoic acid and 175 ml of sulfuric acid (20%) were introduced into a three-necked flask. At -10° C., a solution of 11.9 g (0.172 mol) of sodium nitrite in 50 ml of water was added dropwise and the mixture was stirred for two hours. This solution was introduced dropwise via a droppin...
10.6084/m9.figshare.5104873.v1
null
Primary amine
Aromatic halide
c1ccccc1
c1ccccc1
c1ccccc1
Other
[Cu](I)I.O.C(C)(=O)OCC
null
2
Cc1cc(C(=O)O)ccc1N.[I-]>[Cu](I)I.O.C(C)(=O)OCC>Cc1cc(C(=O)O)ccc1I
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-9664b54f4f6141978a503b896b8ef7fd
CO.Cc1cc(C(=O)O)ccc1I>>COC(=O)c1ccc(I)c(C)c1
CC=1C=C(C(=O)O)C=CC1I.CO.S(O)(O)(=O)=O>>CC=1C=C(C(=O)OC)C=CC1I
[CH3:1][OH:2].O[C:3](=[O:4])[c:5]1[cH:6][cH:7][c:8]([I:9])[c:10]([CH3:11])[cH:12]1>>[CH3:1][O:2][C:3](=[O:4])[c:5]1[cH:6][cH:7][c:8]([I:9])[c:10]([CH3:11])[cH:12]1
CO.Cc1cc(C(=O)O)ccc1I
COC(=O)c1ccc(I)c(C)c1
null
null
null
Protection
Esterification of Carboxylic Acids
9cecdbd189c6f9c3648521d17154d013842a5498de4e76e65efb1d842973340b
af0b8064f2e82ebe66c4c29d2391785ac1b993104265ccdc4d67ca79e36fa3c8
c1ccccc1
O-[C;H0;D3;+0:1](=[O;D1;H0:2])-[c:3](:[c:4]):[c:5].[C;D1;H3:6]-[OH;D1;+0:7]>>[C;D1;H3:6]-[O;H0;D2;+0:7]-[C;H0;D3;+0:1](=[O;D1;H0:2])-[c:3](:[c:4]):[c:5]
null
[]
null
null
null
null
24.4 g (0.093 mol) of 3-methyl-4-iodobenzoic acid and 250 ml of methanol were introduced into a round-bottomed flask and 2.5 ml of concentrated sulfuric acid were added dropwise. The mixture was heated at reflux for twelve hours, the reaction medium evaporated, taken up in ethyl acetate and water, the organic phase dec...
10.6084/m9.figshare.5104873.v1
null
Carboxylic acid.Methanol
Ester
null
null
c1ccccc1
HO-
null
null
null
CO.Cc1cc(C(=O)O)ccc1I>>COC(=O)c1ccc(I)c(C)c1
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-7949d567ab7542a8990b7bcf17a467de
CC1(C)CCC(C)(C)c2cc3cc(B(O)O)ccc3cc21.COC(=O)c1ccc(I)c(C)c1>>COC(=O)c1ccc(-c2ccc3cc4c(cc3c2)C(C)(C)CCC4(C)C)c(C)c1
CC1(C=2C=C3C=CC(=CC3=CC2C(CC1)(C)C)B(O)O)C.CC=1C=C(C(=O)OC)C=CC1I>>CC=1C=C(C(=O)OC)C=CC1C1=CC2=CC=3C(CCC(C3C=C2C=C1)(C)C)(C)C
OB(O)[c:9]1[cH:10][cH:11][c:12]2[cH:13][c:14]3[c:15]([cH:16][c:17]2[cH:18]1)[C:19]([CH3:20])([CH3:21])[CH2:22][CH2:23][C:24]3([CH3:25])[CH3:26].I[c:8]1[cH:7][cH:6][c:5]([C:3]([O:2][CH3:1])=[O:4])[cH:29][c:27]1[CH3:28]>>[CH3:1][O:2][C:3](=[O:4])[c:5]1[cH:6][cH:7][c:8](-[c:9]2[cH:10][cH:11][c:12]3[cH:13][c:14]4[c:15]([cH...
CC1(C)CCC(C)(C)c2cc3cc(B(O)O)ccc3cc21.COC(=O)c1ccc(I)c(C)c1
COC(=O)c1ccc(-c2ccc3cc4c(cc3c2)C(C)(C)CCC4(C)C)c(C)c1
null
null
null
C-C Coupling
Suzuki coupling with boronic acids
bf3685ce01b232e2a6a72cf78778682668414933f5a01822d81318d82da577bf
08d2969413ef1a2cd5b43667268ba178160c7b55545bf48018e31f2b019632ec
c1ccc(-c2ccc3cc4c(cc3c2)CCCC4)cc1
I-[c;H0;D3;+0:1](:[c:2]:[c:3]):[c:4](-[C;D1;H3:5]):[c:6].O-B(-O)-[c;H0;D3;+0:7](:[c:8]:[c:9]):[c:10]:[c:11]>>[C;D1;H3:5]-[c:4](:[c:6]):[c;H0;D3;+0:1](-[c;H0;D3;+0:7](:[c:8]:[c:9]):[c:10]:[c:11]):[c:2]:[c:3]
53
[{"value": 53.0, "product": "CC=1C=C(C(=O)OC)C=CC1C1=CC2=CC=3C(CCC(C3C=C2C=C1)(C)C)(C)C", "details": "PERCENTYIELD", "is_desired": false}, {"value": 52.9, "product": "CC=1C=C(C(=O)OC)C=CC1C1=CC2=CC=3C(CCC(C3C=C2C=C1)(C)C)(C)C", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
null
null
Following the basic procedure of Example 7(f), by reacting 2.8 g (10 mmol) of 5,6,7,8-tetrahydro-5,5,8,8-tetramethyl-2-anthrylboronic acid with 1.84 g (6.7 mmol) of methyl 3-methyl-4-iodobenzoate, 1.37 g (53%) of methyl 3-methyl-4-(5,6,7,8-tetrahydro-5,5,8,8-tetramethyl-2-anthryl)benzoate was obtained in the form of a ...
10.6084/m9.figshare.5104873.v1
null
Aromatic halide.Boronic acid
null
c1ccc2cc3c(cc2c1)CCCC3.c1ccccc1
c1ccccc1.c1ccc2cc3c(cc2c1)CCCC3
c1ccccc1.c1ccc2cc3c(cc2c1)CCCC3
HI.B
null
null
null
CC1(C)CCC(C)(C)c2cc3cc(B(O)O)ccc3cc21.COC(=O)c1ccc(I)c(C)c1>>COC(=O)c1ccc(-c2ccc3cc4c(cc3c2)C(C)(C)CCC4(C)C)c(C)c1
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-5fa351dbe3ea452bbf01e7f31dec9368
CCCI.COC(=O)c1cc(I)c[nH]1>>CCCn1cc(I)cc1C(=O)OC
IC=1C=C(NC1)C(=O)OC.ICCC>>C(CC)N1C(=CC(=C1)I)C(=O)OC
I[CH2:3][CH2:2][CH3:1].[nH:4]1[cH:5][c:6]([I:7])[cH:8][c:9]1[C:10](=[O:11])[O:12][CH3:13]>>[CH3:1][CH2:2][CH2:3][n:4]1[cH:5][c:6]([I:7])[cH:8][c:9]1[C:10](=[O:11])[O:12][CH3:13]
CCCI.COC(=O)c1cc(I)c[nH]1
CCCn1cc(I)cc1C(=O)OC
null
null
null
Heteroatom Alkylation and Arylation
N-alkylation of secondary amines with alkyl halides
ed81cee7c9cb1b5c2931f1dacbfdcf63d83b311ec7685759e6b229eee13149ed
2e1e5fd9557b69cb528f6b2ffd179c67ef24ecb1a2c3994e1cdf0efe7ae19e9c
c1cc[nH]c1
I-[CH2;D2;+0:1]-[C:2]-[C;D1;H3:3].[C;D1;H3:4]-[#8:5]-[C:6](=[O;D1;H0:7])-[c:8]1:[c:9]:[c:10]:[c:11]:[nH;D2;+0:12]:1>>[C;D1;H3:4]-[#8:5]-[C:6](=[O;D1;H0:7])-[c:8]1:[c:9]:[c:10]:[c:11]:[n;H0;D3;+0:12]:1-[CH2;D2;+0:1]-[C:2]-[C;D1;H3:3]
64.7
[{"value": 64.0, "product": "C(CC)N1C(=CC(=C1)I)C(=O)OC", "details": "PERCENTYIELD", "is_desired": false}, {"value": 64.7, "product": "C(CC)N1C(=CC(=C1)I)C(=O)OC", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
null
null
Following the basic procedure of Example 7(d), by reacting 1.96 g (7.8 mmol) of methyl 4-iodo-2-pyrrolecarboxylate with 940 μl (9.6 mmol) of 3-iodopropane, 1.48 g (64%) of methyl N-propyl-4-iodo-2-pyrrolecarboxylate was obtained in the form of a slightly yellow oil. Conditions: See reaction.notes.procedure_details.
10.6084/m9.figshare.5104873.v1
null
Primary halide
null
c1cc[nH]c1
c1cc[nH]c1
c1cc[nH]c1
HI
null
null
null
CCCI.COC(=O)c1cc(I)c[nH]1>>CCCn1cc(I)cc1C(=O)OC
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-00a204d0f65b435cab8a71dca632e9c7
CC1(C)CCC(C)(C)c2cc3cc(B(O)O)ccc3cc21.CCCn1cc(I)cc1C(=O)OC>>CCCn1cc(-c2ccc3cc4c(cc3c2)C(C)(C)CCC4(C)C)cc1C(=O)OC
CC1(C=2C=C3C=CC(=CC3=CC2C(CC1)(C)C)B(O)O)C.C(CC)N1C(=CC(=C1)I)C(=O)OC>>C(CC)N1C(=CC(=C1)C1=CC2=CC=3C(CCC(C3C=C2C=C1)(C)C)(C)C)C(=O)OC
OB(O)[c:7]1[cH:8][cH:9][c:10]2[cH:11][c:12]3[c:13]([cH:14][c:15]2[cH:16]1)[C:17]([CH3:18])([CH3:19])[CH2:20][CH2:21][C:22]3([CH3:23])[CH3:24].I[c:6]1[cH:5][n:4]([CH2:3][CH2:2][CH3:1])[c:26]([C:27](=[O:28])[O:29][CH3:30])[cH:25]1>>[CH3:1][CH2:2][CH2:3][n:4]1[cH:5][c:6](-[c:7]2[cH:8][cH:9][c:10]3[cH:11][c:12]4[c:13]([cH:...
CC1(C)CCC(C)(C)c2cc3cc(B(O)O)ccc3cc21.CCCn1cc(I)cc1C(=O)OC
CCCn1cc(-c2ccc3cc4c(cc3c2)C(C)(C)CCC4(C)C)cc1C(=O)OC
null
null
null
C-C Coupling
Suzuki coupling with boronic acids
1ae6c8ac07df41724f89d3a167e7b6589b8a63a41abe6b2b281e91283bac64b7
08d2969413ef1a2cd5b43667268ba178160c7b55545bf48018e31f2b019632ec
c1cc(-c2ccc3cc4c(cc3c2)CCCC4)c[nH]1
I-[c;H0;D3;+0:1]1:[c:2]:[c:3](-[C:4](-[#8:5])=[O;D1;H0:6]):[#7;a:7](-[C:8]):[c:9]:1.O-B(-O)-[c;H0;D3;+0:10](:[c:11]:[c:12]):[c:13]:[c:14]>>[#8:5]-[C:4](=[O;D1;H0:6])-[c:3]1:[c:2]:[c;H0;D3;+0:1](-[c;H0;D3;+0:10](:[c:11]:[c:12]):[c:13]:[c:14]):[c:9]:[#7;a:7]:1-[C:8]
22.3
[{"value": 22.0, "product": "C(CC)N1C(=CC(=C1)C1=CC2=CC=3C(CCC(C3C=C2C=C1)(C)C)(C)C)C(=O)OC", "details": "PERCENTYIELD", "is_desired": false}, {"value": 22.3, "product": "C(CC)N1C(=CC(=C1)C1=CC2=CC=3C(CCC(C3C=C2C=C1)(C)C)(C)C)C(=O)OC", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
null
null
Following the basic procedure of Example 7(f), by reacting 1.7 g (6 mmol) of 5,6,7,8-tetrahydro-5,5,8,8-tetramethyl-2-anthrylboronic acid with 1.47 g (5 mmol) of methyl N-propyl-4-iodo-2-pyrrolecarboxylate, 450 mg (22%) of methyl N-propyl-4-(5,6,7,8-tetrahydro-5,5,8,8-tetramethyl-2-anthryl)-2-pyrrolecarboxylate were ob...
10.6084/m9.figshare.5104873.v1
null
Aromatic halide.Boronic acid
null
c1ccc2cc3c(cc2c1)CCCC3.c1cc[nH]c1
c1cc[nH]c1.c1ccc2cc3c(cc2c1)CCCC3
c1cc[nH]c1.c1ccc2cc3c(cc2c1)CCCC3
HI.B
null
null
null
CC1(C)CCC(C)(C)c2cc3cc(B(O)O)ccc3cc21.CCCn1cc(I)cc1C(=O)OC>>CCCn1cc(-c2ccc3cc4c(cc3c2)C(C)(C)CCC4(C)C)cc1C(=O)OC
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-02728028cd2a48e7adeea22530388872
CCCI.COC(=O)c1ccc(-c2ccc3cc4c(cc3c2)C(C)(C)CCC4(C)C)cc1O>>CCCOc1cc(-c2ccc3cc4c(cc3c2)C(C)(C)CCC4(C)C)ccc1C(=O)OC
OC1=C(C(=O)OC)C=CC(=C1)C1=CC2=CC=3C(CCC(C3C=C2C=C1)(C)C)(C)C.ICCC>>C(CC)OC1=C(C(=O)OC)C=CC(=C1)C1=CC2=CC=3C(CCC(C3C=C2C=C1)(C)C)(C)C
I[CH2:3][CH2:2][CH3:1].[OH:4][c:5]1[cH:6][c:7](-[c:8]2[cH:9][cH:10][c:11]3[cH:12][c:13]4[c:14]([cH:15][c:16]3[cH:17]2)[C:18]([CH3:19])([CH3:20])[CH2:21][CH2:22][C:23]4([CH3:24])[CH3:25])[cH:26][cH:27][c:28]1[C:29](=[O:30])[O:31][CH3:32]>>[CH3:1][CH2:2][CH2:3][O:4][c:5]1[cH:6][c:7](-[c:8]2[cH:9][cH:10][c:11]3[cH:12][c:1...
CCCI.COC(=O)c1ccc(-c2ccc3cc4c(cc3c2)C(C)(C)CCC4(C)C)cc1O
CCCOc1cc(-c2ccc3cc4c(cc3c2)C(C)(C)CCC4(C)C)ccc1C(=O)OC
null
null
null
Heteroatom Alkylation and Arylation
Williamson Ether Synthesis
7e1040116e3a4cf0e8ec5cc7865388d9cd0efabce6d320a1c25a36e411018d8b
d5f4610d46ccc0478471c5bc0fb862644eaf764bbc5d93badb39d54f6ec8e0a5
c1ccc(-c2ccc3cc4c(cc3c2)CCCC4)cc1
I-[CH2;D2;+0:1]-[C:2]-[C;D1;H3:3].[#8:4]-[C:5](=[O;D1;H0:6])-[c:7]:[c:8](-[OH;D1;+0:9]):[c:10]>>[#8:4]-[C:5](=[O;D1;H0:6])-[c:7]:[c:8](-[O;H0;D2;+0:9]-[CH2;D2;+0:1]-[C:2]-[C;D1;H3:3]):[c:10]
54
[{"value": 54.0, "product": "C(CC)OC1=C(C(=O)OC)C=CC(=C1)C1=CC2=CC=3C(CCC(C3C=C2C=C1)(C)C)(C)C", "details": "PERCENTYIELD", "is_desired": false}, {"value": 52.8, "product": "C(CC)OC1=C(C(=O)OC)C=CC(=C1)C1=CC2=CC=3C(CCC(C3C=C2C=C1)(C)C)(C)C", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
null
null
Following the basic procedure of Example 12, by reacting 2 g (5.1 mmol) of methyl 2-hydroxy-4-(5,6,7,8-tetrahydro-5,5,8,8-tetramethyl-2-anthryl)benzoate with 600 μl (6.1 mmol) of 3-iodopropane, 1.16 g (54%) of methyl 2-propyloxy-4-(5,6,7,8-tetrahydro-5,5,8,8-tetramethyl-2-anthryl)benzoate was obtained. Conditions: See ...
10.6084/m9.figshare.5104873.v1
null
Primary halide.Aromatic alcohol
Ether
null
null
c1ccccc1.c1ccc2cc3c(cc2c1)CCCC3
HI
null
null
null
CCCI.COC(=O)c1ccc(-c2ccc3cc4c(cc3c2)C(C)(C)CCC4(C)C)cc1O>>CCCOc1cc(-c2ccc3cc4c(cc3c2)C(C)(C)CCC4(C)C)ccc1C(=O)OC
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-f03bd0e627354ee4a55f5536f5f04cf4
Fc1ccc(CBr)cc1.Oc1cc2ccc(Br)cc2cc1C12CC3CC(CC(C3)C1)C2>>Fc1ccc(COc2cc3ccc(Br)cc3cc2C23CC4CC(CC(C4)C2)C3)cc1
C12(CC3CC(CC(C1)C3)C2)C2=C(C=C3C=CC(=CC3=C2)Br)O.FC1=CC=C(CBr)C=C1>>C12(CC3CC(CC(C1)C3)C2)C2=C(C=C3C=CC(=CC3=C2)Br)OCC2=CC=C(C=C2)F
Br[CH2:6][c:5]1[cH:4][cH:3][c:2]([F:1])[cH:30][cH:29]1.[OH:7][c:8]1[cH:9][c:10]2[cH:11][cH:12][c:13]([Br:14])[cH:15][c:16]2[cH:17][c:18]1[C:19]12[CH2:20][CH:21]3[CH2:22][CH:23]([CH2:24][CH:25]([CH2:26]3)[CH2:27]1)[CH2:28]2>>[F:1][c:2]1[cH:3][cH:4][c:5]([CH2:6][O:7][c:8]2[cH:9][c:10]3[cH:11][cH:12][c:13]([Br:14])[cH:15]...
Fc1ccc(CBr)cc1.Oc1cc2ccc(Br)cc2cc1C12CC3CC(CC(C3)C1)C2
Fc1ccc(COc2cc3ccc(Br)cc3cc2C23CC4CC(CC(C4)C2)C3)cc1
null
null
null
Heteroatom Alkylation and Arylation
Williamson Ether Synthesis
7e1040116e3a4cf0e8ec5cc7865388d9cd0efabce6d320a1c25a36e411018d8b
d5f4610d46ccc0478471c5bc0fb862644eaf764bbc5d93badb39d54f6ec8e0a5
c1ccc(COc2cc3ccccc3cc2C23CC4CC(CC(C4)C2)C3)cc1
Br-[CH2;D2;+0:1]-[c:2](:[c:3]):[c:4].[OH;D1;+0:5]-[c:6](:[c:7]):[c:8]>>[c:7]:[c:6](-[O;H0;D2;+0:5]-[CH2;D2;+0:1]-[c:2](:[c:3]):[c:4]):[c:8]
86
[{"value": 86.0, "product": "C12(CC3CC(CC(C1)C3)C2)C2=C(C=C3C=CC(=CC3=C2)Br)OCC2=CC=C(C=C2)F", "details": "PERCENTYIELD", "is_desired": false}, {"value": 85.9, "product": "C12(CC3CC(CC(C1)C3)C2)C2=C(C=C3C=CC(=CC3=C2)Br)OCC2=CC=C(C=C2)F", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
null
null
Following the basic procedure of Example 11, by reacting 1.1 g (3 mmol) of 7-(1-adamantyl)-6-hydroxy-2-bromonaphthalene with 420 μl (3,3 mmol) of 4-fluorobenzyl bromide, 1.2 g (86%) of the expected compound was obtained in the form of a colorless oil. Conditions: See reaction.notes.procedure_details.
10.6084/m9.figshare.5104873.v1
null
Primary halide.Aromatic alcohol
Ether
null
null
c1ccccc1.c1ccc2ccccc2c1.C1C2CC3CC1CC(C2)C3
HBr
null
null
null
Fc1ccc(CBr)cc1.Oc1cc2ccc(Br)cc2cc1C12CC3CC(CC(C3)C1)C2>>Fc1ccc(COc2cc3ccc(Br)cc3cc2C23CC4CC(CC(C4)C2)C3)cc1
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-a18ffbdb8f6b474a86827045ded0ce46
CC(C)(C)[Si](C)(C)Cl.Oc1cc2ccc(Br)cc2cc1C12CC3CC(CC(C3)C1)C2>>CC(C)(C)[Si](C)(C)Oc1cc2ccc(Br)cc2cc1C12CC3CC(CC(C3)C1)C2
[Si](C)(C)(C(C)(C)C)Cl.C12(CC3CC(CC(C1)C3)C2)C2=C(C=C3C=CC(=CC3=C2)Br)O.CN(C)C=O.C(C)N(CC)CC>>C12(CC3CC(CC(C1)C3)C2)C2=C(C=C3C=CC(=CC3=C2)Br)O[Si](C)(C)C(C)(C)C
Cl[Si:5]([C:2]([CH3:1])([CH3:3])[CH3:4])([CH3:6])[CH3:7].[OH:8][c:9]1[cH:10][c:11]2[cH:12][cH:13][c:14]([Br:15])[cH:16][c:17]2[cH:18][c:19]1[C:20]12[CH2:21][CH:22]3[CH2:23][CH:24]([CH2:25][CH:26]([CH2:27]3)[CH2:28]1)[CH2:29]2>>[CH3:1][C:2]([CH3:3])([CH3:4])[Si:5]([CH3:6])([CH3:7])[O:8][c:9]1[cH:10][c:11]2[cH:12][cH:13]...
CC(C)(C)[Si](C)(C)Cl.Oc1cc2ccc(Br)cc2cc1C12CC3CC(CC(C3)C1)C2
CC(C)(C)[Si](C)(C)Oc1cc2ccc(Br)cc2cc1C12CC3CC(CC(C3)C1)C2
null
CN(C1=CC=NC=C1)C
O
Protection
Alcohol protection with silyl ethers
91043baed1393f1ecd2302d7d0b31c01cf171d3977dd7c70afa1da52fa298c73
4a917c959d011f885a1269fa3c1f022ee5e09144996246d24e42e65634a451ac
c1ccc2cc(C34CC5CC(CC(C5)C3)C4)ccc2c1
Cl-[Si;H0;D4;+0:1](-[C;D1;H3:2])(-[C;D1;H3:3])-[C:4](-[C;D1;H3:5])(-[C;D1;H3:6])-[C;D1;H3:7].[OH;D1;+0:8]-[c:9](:[c:10]):[c:11]>>[C;D1;H3:5]-[C:4](-[C;D1;H3:6])(-[C;D1;H3:7])-[Si;H0;D4;+0:1](-[C;D1;H3:2])(-[C;D1;H3:3])-[O;H0;D2;+0:8]-[c:9](:[c:10]):[c:11]
null
[]
null
null
12
HOUR
11.9 g (33.3 mmol) of 7-(1-adamantyl)-6-hydroxy-2-bromonaphthalene, 120 ml of DMF, 5.1 ml (36.6 mmol) of triethylamine and 203 mg of 4-dimethylaminopyridine were introduced successively into a three-necked flask. A solution of 5.52 g (36.6 mmol) of tert-butyldimethylsilyl chloride was added dropwise and the mixture was...
10.6084/m9.figshare.5104873.v1
null
Aromatic alcohol.Silyl protective group
TMS ether protective group
null
null
c1ccc2ccccc2c1.C1C2CC3CC1CC(C2)C3
HCl
CN(C1=CC=NC=C1)C.O
null
12
CC(C)(C)[Si](C)(C)Cl.Oc1cc2ccc(Br)cc2cc1C12CC3CC(CC(C3)C1)C2>CN(C1=CC=NC=C1)C.O>CC(C)(C)[Si](C)(C)Oc1cc2ccc(Br)cc2cc1C12CC3CC(CC(C3)C1)C2
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-3150c5b19251400f94abae6bc2510c0b
CC(C)(C)[Si](C)(C)Oc1cc2ccc(Br)cc2cc1C12CC3CC(CC(C3)C1)C2.OBO>>CC(C)(C)[Si](C)(C)Oc1cc2ccc(B(O)O)cc2cc1C12CC3CC(CC(C3)C1)C2
C12(CC3CC(CC(C1)C3)C2)C2=C(C=C3C=CC(=CC3=C2)Br)O[Si](C)(C)C(C)(C)C.B(O)O>>C12(CC3CC(CC(C1)C3)C2)C2=C(C=C3C=CC(=CC3=C2)B(O)O)O[Si](C)(C)C(C)(C)C
Br[c:14]1[cH:13][cH:12][c:11]2[cH:10][c:9]([O:8][Si:5]([C:2]([CH3:1])([CH3:3])[CH3:4])([CH3:6])[CH3:7])[c:21]([C:22]34[CH2:23][CH:24]5[CH2:25][CH:26]([CH2:27][CH:28]([CH2:29]5)[CH2:30]3)[CH2:31]4)[cH:20][c:19]2[cH:18]1.[BH:15]([OH:16])[OH:17]>>[CH3:1][C:2]([CH3:3])([CH3:4])[Si:5]([CH3:6])([CH3:7])[O:8][c:9]1[cH:10][c:1...
CC(C)(C)[Si](C)(C)Oc1cc2ccc(Br)cc2cc1C12CC3CC(CC(C3)C1)C2.OBO
CC(C)(C)[Si](C)(C)Oc1cc2ccc(B(O)O)cc2cc1C12CC3CC(CC(C3)C1)C2
null
null
null
Miscellaneous
OtherReaction
5e14c0418b5489193c2f9cab37a1ee7bed4f0fe7e58c5c9713c9fa95392c1e02
dafd25fbe01879c365f8c874026e570f49824f4bb82016b29d0c5d21aeb58ca3
c1ccc2cc(C34CC5CC(CC(C5)C3)C4)ccc2c1
Br-[c;H0;D3;+0:1](:[c:2]:[c:3]):[c:4]:[c:5].[O;D1;H1:6]-[BH;D2;+0:7]-[O;D1;H1:8]>>[O;D1;H1:6]-[B;H0;D3;+0:7](-[O;D1;H1:8])-[c;H0;D3;+0:1](:[c:2]:[c:3]):[c:4]:[c:5]
null
[]
null
null
null
null
Following the basic procedure of Example 7(e), beginning with 11.9 g (25.4 mmol) of 7-(1-adamantyl)-6-tert-butyldimethylsilyloxy-2-bromonaphthalene, 8.37 g (75%) of the expected boronic acid of melting point 221°-222° C. were obtained. Conditions: See reaction.notes.procedure_details. Workup: were obtained
10.6084/m9.figshare.5104873.v1
null
Aromatic halide
Boronic acid
c1ccc2ccccc2c1
c1ccc2ccccc2c1
c1ccc2ccccc2c1.C1C2CC3CC1CC(C2)C3
HBr
null
null
null
CC(C)(C)[Si](C)(C)Oc1cc2ccc(Br)cc2cc1C12CC3CC(CC(C3)C1)C2.OBO>>CC(C)(C)[Si](C)(C)Oc1cc2ccc(B(O)O)cc2cc1C12CC3CC(CC(C3)C1)C2
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-dd8eb0b6bec94543a29935506ffa1165
CCOC(=O)c1csc(-c2ccc3cc(O[Si](C)(C)C(C)(C)C)c(C45CC6CC(CC(C6)C4)C5)cc3c2)c1>>CCOC(=O)c1csc(-c2ccc3cc(O)c(C45CC6CC(CC(C6)C4)C5)cc3c2)c1
C12(CC3CC(CC(C1)C3)C2)C2=C(C=C3C=CC(=CC3=C2)C=2SC=C(C2)C(=O)OCC)O[Si](C)(C)C(C)(C)C.[F-].C(CCC)[N+](CCCC)(CCCC)CCCC.O>>C12(CC3CC(CC(C1)C3)C2)C2=C(C=C3C=CC(=CC3=C2)C=2SC=C(C2)C(=O)OCC)O
CC(C)(C)[Si](C)(C)[O:16][c:15]1[cH:14][c:13]2[cH:12][cH:11][c:10](-[c:9]3[s:8][cH:7][c:6]([C:4]([O:3][CH2:2][CH3:1])=[O:5])[cH:31]3)[cH:30][c:29]2[cH:28][c:17]1[C:18]12[CH2:19][CH:20]3[CH2:21][CH:22]([CH2:23][CH:24]([CH2:25]3)[CH2:26]1)[CH2:27]2>>[CH3:1][CH2:2][O:3][C:4](=[O:5])[c:6]1[cH:7][s:8][c:9](-[c:10]2[cH:11][cH...
CCOC(=O)c1csc(-c2ccc3cc(O[Si](C)(C)C(C)(C)C)c(C45CC6CC(CC(C6)C4)C5)cc3c2)c1
CCOC(=O)c1csc(-c2ccc3cc(O)c(C45CC6CC(CC(C6)C4)C5)cc3c2)c1
null
null
C1CCOC1
Deprotection
Alcohol deprotection from silyl ethers
e70131badc7d7d580ed75b2dfb3ce6df2a5f496b2119611cf5354e1267babe73
b09ece7bccc3ff762f4ff5407ad846fffba6d6a63735853c86a86d29904f54ed
c1csc(-c2ccc3ccc(C45CC6CC(CC(C6)C4)C5)cc3c2)c1
C-C(-C)(-C)-[Si](-C)(-C)-[O;H0;D2;+0:1]-[c:2](:[c:3]):[c:4]>>[OH;D1;+0:1]-[c:2](:[c:3]):[c:4]
null
[]
null
null
2
HOUR
8.29 g (15.2 mmol) of ethyl 2-[7-(1-adamantyl)-6-tert-butyldimethylsilyloxy-2-naphthyl]-4-thiophenecarboxylate and 60 ml of THF were introduced into a round-bottomed flask. A solution of 15.2 ml (16.6 mmol) of tetrabutylammonium fluoride in THF (1.1N) was added dropwise and the mixture was stirred at room temperature f...
10.6084/m9.figshare.5104873.v1
null
TMS ether protective group
Aromatic alcohol
null
null
c1ccsc1.c1ccc2ccccc2c1.C1C2CC3CC1CC(C2)C3
Other
C1CCOC1
null
2
CCOC(=O)c1csc(-c2ccc3cc(O[Si](C)(C)C(C)(C)C)c(C45CC6CC(CC(C6)C4)C5)cc3c2)c1>C1CCOC1>CCOC(=O)c1csc(-c2ccc3cc(O)c(C45CC6CC(CC(C6)C4)C5)cc3c2)c1
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-20b7c42ff39d4f27aff2e357d5541bd7
CC(=O)Oc1cc(OC(C)=O)cc(C(=O)O)c1.CCC(N)C(N)=O>>CCC(O)c1cc(O)cc(O)c1
C(C)(=O)OC=1C=C(C(=O)O)C=C(C1)OC(C)=O.OCC(C)(CO)CO.C(=C)[Si](C=C)(C=C)C=C.OC1=CC=C(C=C1)C(C)(C1=CC=C(C=C1)O)C1=CC=C(C=C1)O.C(CN)N.N=O.OCC(CO)(CO)CO.NC(C(=O)N)CC>>OC=1C=C(C(CC)O)C=C(C1)O
CC(=O)[O:8][c:7]1[cH:6][c:5](C(=O)[OH:4])[cH:12][c:10]([O:11]C(C)=O)[cH:9]1.NC(=O)[CH:3](N)[CH2:2][CH3:1]>>[CH3:1][CH2:2][CH:3]([OH:4])[c:5]1[cH:6][c:7]([OH:8])[cH:9][c:10]([OH:11])[cH:12]1
CC(=O)Oc1cc(OC(C)=O)cc(C(=O)O)c1.CCC(N)C(N)=O
CCC(O)c1cc(O)cc(O)c1
null
null
null
Heteroatom Alkylation and Arylation
OtherReaction
2c2d1c8b68ffa1b974d0bfc3253fc7eccb45d9de1ab9e2c57e4e8b38819e81d8
68f8d4f234bd8dc2e62e327d389484b226fe14658d99e9cae7ce55e67399ce26
c1ccccc1
C-C(=O)-[O;H0;D2;+0:1]-[c:2]1:[c:3]:[c;H0;D3;+0:4](-C(=O)-[OH;D1;+0:5]):[c:6]:[c:7](-[O;H0;D2;+0:8]-C(-C)=O):[c:9]:1.N-C(=O)-[CH;D3;+0:10](-N)-[C:11]-[C;D1;H3:12]>>[C;D1;H3:12]-[C:11]-[CH;D3;+0:10](-[OH;D1;+0:5])-[c;H0;D3;+0:4]1:[c:3]:[c:2](-[OH;D1;+0:1]):[c:9]:[c:7](-[OH;D1;+0:8]):[c:6]:1
null
[]
null
null
null
null
The dendrimers of the present invention can be selected as toner additives, for example, as illustrated in the documents mentioned herein. Dendrimers are known, and can be considered radially symmetrical molecules of a STARBURST™ topology comprised of an initiator core, such as nitrogen, ethylenediimine, silicon, and t...
10.6084/m9.figshare.5104873.v1
null
Carboxylic acid.Ester.Ester.Primary amide.Primary amine
Secondary alcohol.Aromatic alcohol.Aromatic alcohol
c1ccccc1
c1ccccc1
c1ccccc1
HO-
null
null
null
CC(=O)Oc1cc(OC(C)=O)cc(C(=O)O)c1.CCC(N)C(N)=O>>CCC(O)c1cc(O)cc(O)c1
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-d0e79d3004cd4cb5a98d3c999a726a05
N#CCc1ccc(F)cc1.O=[N+]([O-])c1ccccc1>>Fc1ccc(-c2onc3ccccc23)cc1
FC1=CC=C(C=C1)CC#N.[OH-].[Na+].[N+](=O)([O-])C1=CC=CC=C1>>FC1=CC=C(C=C1)C=1ON=C2C1C=CC=C2
N#C[CH2:6][c:5]1[cH:4][cH:3][c:2]([F:1])[cH:16][cH:15]1.O=[N+:8]([O-:7])[c:9]1[cH:10][cH:11][cH:12][cH:13][cH:14]1>>[F:1][c:2]1[cH:3][cH:4][c:5](-[c:6]2[o:7][n:8][c:9]3[cH:10][cH:11][cH:12][cH:13][c:14]23)[cH:15][cH:16]1
N#CCc1ccc(F)cc1.O=[N+]([O-])c1ccccc1
Fc1ccc(-c2onc3ccccc23)cc1
null
null
CO
Aromatic Heterocycle Formation
OtherReaction
0f22d84b2a4c2a0e4579a9b5d1adb0e1a3a85c6a163e0b5818a361e01201e52a
b0095d38e0fbba4b05f88363393446922ef1c66394cfc608f7c1cd4fc808583a
c1ccc(-c2onc3ccccc23)cc1
N#C-[CH2;D2;+0:1]-[c;H0;D3;+0:2](:[c:3]:[c:4]):[c:5]:[c:6].O=[N+;H0;D3:7](-[O-;H0;D1:8])-[c:9](:[c:10]):[cH;D2;+0:11]:[c:12]:[c:13]>>[c:10]:[c:9]1:[n;H0;D2;+0:7]:[o;H0;D2;+0:8]:[c;H0;D3;+0:1](-[c;H0;D3;+0:2](:[c:3]:[c:4]):[c:5]:[c:6]):[c;H0;D3;+0:11]:1:[c:12]:[c:13]
null
[]
null
null
9
HOUR
A total of 50.7 g (0.375 mol) of 4-fluorophenyl-acetonitrile is slowly added to a vigorously stirred, room-temperature solution of 150 g (3.75 mol) of sodium hydroxide in 750 ml of absolute methanol. After solution is complete, 46 g (0.374 mol) of nitrobenzene is slowly added. The resulting solution is warmed to 65°-70...
10.6084/m9.figshare.5104873.v1
null
Nitrile.Nitro group
null
c1ccccc1
c1ccc2nocc2c1
c1ccccc1.c1ccc2nocc2c1
HO-
CO
null
9
N#CCc1ccc(F)cc1.O=[N+]([O-])c1ccccc1>CO>Fc1ccc(-c2onc3ccccc23)cc1
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-92bc8cb4ed55424491eb833aaed1c16a
Fc1ccc(-c2onc3ccccc23)cc1>>Nc1ccccc1C(=O)c1ccc(F)cc1
FC1=CC=C(C=C1)C=1ON=C2C1C=CC=C2>>NC1=C(C(=O)C2=CC=C(C=C2)F)C=CC=C1
[n:1]1[c:2]2[cH:3][cH:4][cH:5][cH:6][c:7]2[c:8](-[c:10]2[cH:11][cH:12][c:13]([F:14])[cH:15][cH:16]2)[o:9]1>>[NH2:1][c:2]1[cH:3][cH:4][cH:5][cH:6][c:7]1[C:8](=[O:9])[c:10]1[cH:11][cH:12][c:13]([F:14])[cH:15][cH:16]1
Fc1ccc(-c2onc3ccccc23)cc1
Nc1ccccc1C(=O)c1ccc(F)cc1
null
[Pd]
O1CCCC1.C(C)N(CC)CC
Miscellaneous
OtherReaction
63dfc430e67d3a7ada3c7e8f6e094ee16a92b905651085a196381d3119990ee1
2e99338cc955e46b2c0e811178d7128dca9a68ef9fbb467724eba7220efe12b0
O=C(c1ccccc1)c1ccccc1
[c:1]:[c:2]:[c;H0;D3;+0:3](-[c;H0;D3;+0:4]1:[o;H0;D2;+0:5]:[n;H0;D2;+0:6]:[c:7](:[c:8]):[c:9]:1:[c:10]):[c:11]:[c:12]>>[NH2;D1;+0:6]-[c:7](:[c:8]):[c:9](-[C;H0;D3;+0:4](=[O;H0;D1;+0:5])-[c;H0;D3;+0:3](:[c:2]:[c:1]):[c:11]:[c:12]):[c:10]
null
[]
null
null
null
null
To a suspension of (16) (42.6 g, 0.2 mol) in 750 ml of dry tetrahydrofuran (THF) and 20 ml of triethylamine is added 5% palladium on charcoal (6 g). The vigorously stirred suspension is flushed with hydrogen gas and stirred at room temperature under a hydrogen atmosphere until absorption of hydrogen ceases (approximate...
10.6084/m9.figshare.5104873.v1
null
null
Ketone.Primary amine
c1ccc2nocc2c1
c1ccccc1
c1ccccc1.c1ccccc1
null
[Pd].O1CCCC1.C(C)N(CC)CC
null
null
Fc1ccc(-c2onc3ccccc23)cc1>[Pd].O1CCCC1.C(C)N(CC)CC>Nc1ccccc1C(=O)c1ccc(F)cc1
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-505bc94ed0b24d42b247b9173702273a
CC(=O)c1ccc(F)cc1.Nc1ccccc1C(=O)c1ccc(F)cc1>>Fc1ccc(-c2cc(-c3ccc(F)cc3)c3ccccc3n2)cc1
NC1=C(C(=O)C2=CC=C(C=C2)F)C=CC=C1.CC(=O)C1=CC=C(C=C1)F.O.C=1(C(=CC=CC1)S(=O)(=O)O)C>>FC1=CC=C(C=C1)C1=NC2=CC=CC=C2C(=C1)C1=CC=C(C=C1)F
O=[C:6]([c:5]1[cH:4][cH:3][c:2]([F:1])[cH:24][cH:23]1)[CH3:7].O=[C:8]([c:9]1[cH:10][cH:11][c:12]([F:13])[cH:14][cH:15]1)[c:16]1[cH:17][cH:18][cH:19][cH:20][c:21]1[NH2:22]>>[F:1][c:2]1[cH:3][cH:4][c:5](-[c:6]2[cH:7][c:8](-[c:9]3[cH:10][cH:11][c:12]([F:13])[cH:14][cH:15]3)[c:16]3[cH:17][cH:18][cH:19][cH:20][c:21]3[n:22]2...
CC(=O)c1ccc(F)cc1.Nc1ccccc1C(=O)c1ccc(F)cc1
Fc1ccc(-c2cc(-c3ccc(F)cc3)c3ccccc3n2)cc1
null
null
O
Aromatic Heterocycle Formation
OtherReaction
ef62a17cf5af6b6a9400c0546d94e169af6c90ed68e6730786f9942d0bd5f3dc
e8142154ce82c2e242e52c937b939f3fefdc51b29f1e30581e6f69472c9bf693
c1ccc(-c2cc(-c3ccccc3)c3ccccc3n2)cc1
O=[C;H0;D3;+0:1](-[CH3;D1;+0:2])-[c;H0;D3;+0:3](:[c:4]:[c:5]):[c:6]:[c:7].O=[C;H0;D3;+0:8](-[c:9](:[c:10]):[c:11](-[NH2;D1;+0:12]):[c:13])-[c;H0;D3;+0:14](:[c:15]:[c:16]):[c:17]:[c:18]>>[c:16]:[c:15]:[c;H0;D3;+0:14](-[c;H0;D3;+0:8]1:[cH;D2;+0:2]:[c;H0;D3;+0:1](-[c;H0;D3;+0:3](:[c:4]:[c:5]):[c:6]:[c:7]):[n;H0;D2;+0:12]:...
null
[]
200
CELSIUS
null
null
A flask is loaded with (17) (21.5 g, 0.1 mol), 4-fluoroacetophenone (13.8 g, 0.1 mol), and toluene sulfonic acid monohydrate (3.8 g, 0.02 mol). The flask is heated to 200° C. and the water of condensation removed. After water evolution ceased, the mixture is cooled and the crude solid product is crushed and washed with...
10.6084/m9.figshare.5104873.v1
null
Ketone.Ketone.Primary amine
null
c1ccccc1
c1ccc2ncccc2c1
c1ccccc1.c1ccccc1.c1ccc2ncccc2c1
HO-
O
200
null
CC(=O)c1ccc(F)cc1.Nc1ccccc1C(=O)c1ccc(F)cc1>O>Fc1ccc(-c2cc(-c3ccc(F)cc3)c3ccccc3n2)cc1
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-48ed68423d4a4e7fb6e576167938191c
Cl.Cl>>ClCCl.N
N1=CC=CC=C1.CC(C)(C)[Si](C)(C)Cl.N[C@@H](CC1=CNC=N1)CO.[H-].[Na+].Cl.Cl.N[C@@H](CC1=CNC=N1)CO>>N.C(Cl)Cl.N[C@@H](CC1=CNC=N1)CO
[ClH:1].[ClH:3]>>[Cl:1][CH2:2][Cl:3].[NH3:4]
Cl.Cl
ClCCl.N
null
null
CN(C)C=O.CCCCCC
Functional Group Addition
OtherReaction
41523ea8a56e473f35c21479a8332be3a39833fcdb7794bb86c8a0176356dde0
ffcace6ec62222cc441f032155f7c26a7f18918e26f8fa19eef390df174a1801
null
[ClH;D0;+0:1].[ClH;D0;+0:2]>>[Cl;H0;D1;+0:1]-[C:3]-[Cl;H0;D1;+0:2]
null
[]
null
null
1.5
HOUR
TBDMS protected histidinol 14--To a stirred solution of 205 mg (5.1 mmol) of NaH washed 3× with hexane, under argon, in 3.0 mL DMF was added in portions 500 mg (2.3 mmol) of histidinol dihydrochloride, resulting in moderate gas evolution. The solution was stirred for 1.5 h, then 1.8 mL (23 mmol) of anhydrous pyridine a...
10.6084/m9.figshare.5104873.v1
null
null
Primary halide.Primary halide
null
null
null
Other
CN(C)C=O.CCCCCC
null
1.5
Cl.Cl>CN(C)C=O.CCCCCC>ClCCl.N
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-58e35fa5d3104b07bb1cd637b9c2a80b
CC(CN)(CN)CN.O=C1CCCO1>>CC1(CN)CN=C2CCCN2C1
C1(CCCO1)=O.[Cl-].[NH4+].NCC(C)(CN)CN>>NCC1(CN=C2N(C1)CCC2)C
[CH3:1][C:2]([CH2:3][NH2:4])([CH2:5][NH2:6])[CH2:12][NH2:11].O=[C:7]1O[CH2:10][CH2:9][CH2:8]1>>[CH3:1][C:2]1([CH2:3][NH2:4])[CH2:5][N:6]=[C:7]2[CH2:8][CH2:9][CH2:10][N:11]2[CH2:12]1
CC(CN)(CN)CN.O=C1CCCO1
CC1(CN)CN=C2CCCN2C1
null
null
O
Heteroatom Alkylation and Arylation
OtherReaction
1d8e04e574d96100d365a352017d9cbd9eb21df9423d7eccd6549a60899f558c
278cd8e31d8f48c7f944b77ce78ef7ba21405ad243ad2b6be0edc47e13497c28
C1CN=C2CCCN2C1
O=[C;H0;D3;+0:1]1-O-[CH2;D2;+0:2]-[C:3]-[C:4]-1.[NH2;D1;+0:5]-[C:6]-[C:7]-[C:8]-[NH2;D1;+0:9]>>[C:6]1-[C:7]-[C:8]-[N;H0;D2;+0:9]=[C;H0;D3;+0:1]2-[C:4]-[C:3]-[CH2;D2;+0:2]-[N;H0;D3;+0:5]-1-2
null
[]
250
CELSIUS
1.5
HOUR
A mixture of 21.03 g (0.24 mol) of γ-butyrolactone and 1.31 g (24 mmol) of ammonium chloride in 114.5 g (0.98 mol) of 1,1,1-tris(aminomethyl)ethane was heated at 250° C. in an autoclave. After 1.5 h, the mixture was cooled and the excess amine and the water formed were removed by distillation. The residue was distilled...
10.6084/m9.figshare.5104873.v1
null
Ester.Primary amine.Primary amine
Tertiary amine
C1CCOC1
C1CN=C2CCCN2C1
C1CN=C2CCCN2C1
HO-
O
250
1.5
CC(CN)(CN)CN.O=C1CCCO1>O>CC1(CN)CN=C2CCCN2C1
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-54fc6a8a376c4fd9a41d798a9116e90e
CC(=O)c1c(C)cc(C)cc1C.CCOC(=O)C(=O)OCC>>CCOC(=O)C(=O)CC(=O)c1c(C)cc(C)cc1C
CC1=C(C(=CC(=C1)C)C)C(C)=O.C(C(=O)OCC)(=O)OCC.[H-].[Na+]>>O=C(C(=O)OCC)CC(C1=C(C=C(C=C1C)C)C)=O
[CH3:8][C:9](=[O:10])[c:11]1[c:12]([CH3:13])[cH:14][c:15]([CH3:16])[cH:17][c:18]1[CH3:19].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]([CH3:13])[cH:14][c:15]([CH3:16])[cH:17][c:18]1[CH3:19]
CC(=O)c1c(C)cc(C)cc1C.CCOC(=O)C(=O)OCC
CCOC(=O)C(=O)CC(=O)c1c(C)cc(C)cc1C
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]
66.7
[{"value": 66.7, "product": "O=C(C(=O)OCC)CC(C1=C(C=C(C=C1C)C)C)=O", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
null
null
To a solution of 2', 4', 6'-trimethylacetophenone (15 g, 92.6 mmol) and diethyl oxalate (20 g, 139 mmol) in 500 mL of anhydrous toluene was cautiously added 7.4 g of NaH (60% dispersion in mineral oil). The reaction mixture was slowly heated to reflux under N2. It was refluxed for about 20 minutes, then cooled, poured ...
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(C)cc(C)cc1C.CCOC(=O)C(=O)OCC>C1(=CC=CC=C1)C>CCOC(=O)C(=O)CC(=O)c1c(C)cc(C)cc1C
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-d9ea025a9a0a4f688e80e240ea0b34ac
CCOC(=O)C(=O)CC(=O)c1c(C)cc(C)cc1C.O=N[O-]>>CCOC(=O)C(=O)C(=NO)C(=O)c1c(C)cc(C)cc1C
O=C(C(=O)OCC)CC(C1=C(C=C(C=C1C)C)C)=O.Cl.N(=O)[O-].[Na+]>>O=C(C(=O)OCC)C(C(C1=C(C=C(C=C1C)C)C)=O)=NO
[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]([CH3:15])[cH:16][c:17]([CH3:18])[cH:19][c:20]1[CH3:21].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]([CH3:15])[cH:16][c:17]([CH3:18])[cH:19][c:20]1[CH3:21]
CCOC(=O)C(=O)CC(=O)c1c(C)cc(C)cc1C.O=N[O-]
CCOC(=O)C(=O)C(=NO)C(=O)c1c(C)cc(C)cc1C
null
null
C(C)O
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
N2O3 gas was slowly passed into a stirred solution of the product of step A (16.2 g) in 300 mL of ethanol until the disappearance of starting material was confirmed by TLC. N2O3 gas was generated by the dropwise addition of 12N aqueous HCl solution into an aqueous slurry of NaNO2. The solvent was removed from the mixtu...
10.6084/m9.figshare.5104873.v1
null
Ketone.Ketone.Nitroso
Ketone.Ketone.Oxime
null
null
c1ccccc1
HO-
C(C)O
null
null
CCOC(=O)C(=O)CC(=O)c1c(C)cc(C)cc1C.O=N[O-]>C(C)O>CCOC(=O)C(=O)C(=NO)C(=O)c1c(C)cc(C)cc1C
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-75a3caa0644f40ee90d13cb00258ca5f
CCOC(=O)C(=O)C(=NO)C(=O)c1c(C)cc(C)cc1C.CNN>>CCOC(=O)c1nn(C)c(-c2c(C)cc(C)cc2C)c1N
O=C(C(=O)OCC)C(C(C1=C(C=C(C=C1C)C)C)=O)=NO.Cl.CNN>>NC=1C(=NN(C1C1=C(C=C(C=C1C)C)C)C)C(=O)OCC
O=[C:6]([C:4]([O:3][CH2:2][CH3:1])=[O:5])[C:20]([C:10](=O)[c:11]1[c:12]([CH3:13])[cH:14][c:15]([CH3:16])[cH:17][c:18]1[CH3:19])=[N:21]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]([CH3:13])[cH:14][c:15]([CH3:16])[cH:17][c:18]2[CH3:19])[c:20]1[NH2:21]
CCOC(=O)C(=O)C(=NO)C(=O)c1c(C)cc(C)cc1C.CNN
CCOC(=O)c1nn(C)c(-c2c(C)cc(C)cc2C)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](-[C;D1;H3:6]):[c:7]):[c:8](-[C;D1;H3:9]):[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;H3:1...
78.9
[{"value": 78.9, "product": "NC=1C(=NN(C1C1=C(C=C(C=C1C)C)C)C)C(=O)OCC", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
4
HOUR
To a solution of the product of step B (4.0 g, 13.8 mmol) and 1.6 mL of 12N hydrochloric acid in 100 mL of methanol was added dropwise 0.63 g of methyl hydrazine at 0° C. The reaction mixture was stirred at room temperature 4 hours, and then concentrated. The resulting residue was partitioned between water and ethyl ac...
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
4
CCOC(=O)C(=O)C(=NO)C(=O)c1c(C)cc(C)cc1C.CNN>CO>CCOC(=O)c1nn(C)c(-c2c(C)cc(C)cc2C)c1N
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-c0a66d17f4434d27b82b139747ba9e7b
CCCBr.CCCNc1nc(C)nc2c(-c3c(C)cc(C)cc3C)n(C)nc12>>CCCN(CCC)c1nc(C)nc2c(-c3c(C)cc(C)cc3C)n(C)nc12
C(CC)NC=1C=2C(N=C(N1)C)=C(N(N2)C)C2=C(C=C(C=C2C)C)C.[OH-].[K+].BrCCC>>C(CC)N(C=1C=2C(N=C(N1)C)=C(N(N2)C)C2=C(C=C(C=C2C)C)C)CCC
Br[CH2:5][CH2:6][CH3:7].[CH3:1][CH2:2][CH2:3][NH:4][c:8]1[n:9][c:10]([CH3:11])[n:12][c:13]2[c:14](-[c:15]3[c:16]([CH3:17])[cH:18][c:19]([CH3:20])[cH:21][c:22]3[CH3:23])[n:24]([CH3:25])[n:26][c:27]12>>[CH3:1][CH2:2][CH2:3][N:4]([CH2:5][CH2:6][CH3:7])[c:8]1[n:9][c:10]([CH3:11])[n:12][c:13]2[c:14](-[c:15]3[c:16]([CH3:17])...
CCCBr.CCCNc1nc(C)nc2c(-c3c(C)cc(C)cc3C)n(C)nc12
CCCN(CCC)c1nc(C)nc2c(-c3c(C)cc(C)cc3C)n(C)nc12
null
null
CS(=O)C
Heteroatom Alkylation and Arylation
N-alkylation of secondary amines with alkyl halides
6d58cac08ccced0a33ed16fbca180bc12aa011288d6476106d98a7b2cbc3d709
523d37155b42c8dc851abeddadebb241cdd90bdf649ba750c35e13c8c752d7b0
c1ccc(-c2[nH]nc3cncnc23)cc1
Br-[CH2;D2;+0:1]-[C:2]-[C;D1;H3:3].[C:4]-[C:5]-[NH;D2;+0:6]-[c:7]1:[#7;a:8]:[c:9]:[#7;a:10]:[c:11]2:[c:12]:[#7;a:13]:[#7;a:14]:[c:15]:2:1>>[C:4]-[C:5]-[N;H0;D3;+0:6](-[CH2;D2;+0:1]-[C:2]-[C;D1;H3:3])-[c:7]1:[#7;a:8]:[c:9]:[#7;a:10]:[c:11]2:[c:12]:[#7;a:13]:[#7;a:14]:[c:15]:2:1
null
[]
60
CELSIUS
null
null
A mixture of the product of step F (400 mg, 1.2 mmol), powder KOH (1.0 g) and 1-bromopropane (1 mL) in 2 mL of DMSO was heated at 60° C. for 8 hours. The excess bromopropane was then evaporated. The mixture was partitioned between water and ether. The aqueous layer was separated and extracted with ether. The combined e...
10.6084/m9.figshare.5104873.v1
null
Primary halide.Secondary amine
Tertiary amine
null
null
c1ccccc1.c1ncc2n[nH]cc2n1
HBr
CS(=O)C
60
null
CCCBr.CCCNc1nc(C)nc2c(-c3c(C)cc(C)cc3C)n(C)nc12>CS(=O)C>CCCN(CCC)c1nc(C)nc2c(-c3c(C)cc(C)cc3C)n(C)nc12
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-564b28fa70ee43db9e87ffa6d6c4d4e6
CC1(NC(=O)OC(C)(C)C)CCN(c2nccc(Cl)n2)CC1>>CC1(N)CCN(c2nccc(Cl)n2)CC1
C1(=CC=CC=C1)OC.FC(C(=O)O)(F)F.C(C)(C)(C)OC(=O)NC1(CCN(CC1)C1=NC=CC(=N1)Cl)C.[OH-].[Na+]>>NC1(CCN(CC1)C1=NC=CC(=N1)Cl)C
CC(C)(C)OC(=O)[NH:3][C:2]1([CH3:1])[CH2:4][CH2:5][N:6]([c:7]2[n:8][cH:9][cH:10][c:11]([Cl:12])[n:13]2)[CH2:14][CH2:15]1>>[CH3:1][C:2]1([NH2:3])[CH2:4][CH2:5][N:6]([c:7]2[n:8][cH:9][cH:10][c:11]([Cl:12])[n:13]2)[CH2:14][CH2:15]1
CC1(NC(=O)OC(C)(C)C)CCN(c2nccc(Cl)n2)CC1
CC1(N)CCN(c2nccc(Cl)n2)CC1
null
null
C(Cl)Cl
Reduction
Hydrogenolysis of amides/imides/carbamates
3c33dd2a2d355ee5ba0287367e209aa147a39aa00607f0c95fb2bf1ade45d014
c5b5dffe7dd8beebdc1baa8b5b05300a9f7079e65dcfd42ade6f8a77ff09537d
c1cnc(N2CCCCC2)nc1
C-C(-C)(-C)-O-C(=O)-[NH;D2;+0:1]-[C:2](-[C;D1;H3:3])(-[C:4])-[C:5]>>[C:4]-[C:2](-[C;D1;H3:3])(-[NH2;D1;+0:1])-[C:5]
null
[]
null
null
1
HOUR
A solution of 2.22 g (0.0068 mol) of 4-t-butoxycarbonylamino-1-(4-chloropyrimidin-2-yl)-4-methylpiperidine (step c) in 25 ml of anhydrous methylene chloride is cooled under a nitrogen atmosphere and 5 ml of anisole and 25 ml of trifluoroacetic acid are added slowly. The mixture is stirred for 1 hour at room temperature...
10.6084/m9.figshare.5104873.v1
null
Carbamic ester.Ether.Boc
Primary amine
null
null
C1CC[NH]CC1.c1cncnc1
HO-
C(Cl)Cl
null
1
CC1(NC(=O)OC(C)(C)C)CCN(c2nccc(Cl)n2)CC1>C(Cl)Cl>CC1(N)CCN(c2nccc(Cl)n2)CC1
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-b6be6f155af94436ba0e8bfe5bd8a6cd
CC1(NC(=O)OC(C)(C)C)CCN(c2ccnc(Cl)n2)CC1>>CC1(N)CCN(c2ccnc(Cl)n2)CC1
C1(=CC=CC=C1)OC.FC(C(=O)O)(F)F.C(C)(C)(C)OC(=O)NC1(CCN(CC1)C1=NC(=NC=C1)Cl)C.[OH-].[Na+]>>NC1(CCN(CC1)C1=NC(=NC=C1)Cl)C
CC(C)(C)OC(=O)[NH:3][C:2]1([CH3:1])[CH2:4][CH2:5][N:6]([c:7]2[cH:8][cH:9][n:10][c:11]([Cl:12])[n:13]2)[CH2:14][CH2:15]1>>[CH3:1][C:2]1([NH2:3])[CH2:4][CH2:5][N:6]([c:7]2[cH:8][cH:9][n:10][c:11]([Cl:12])[n:13]2)[CH2:14][CH2:15]1
CC1(NC(=O)OC(C)(C)C)CCN(c2ccnc(Cl)n2)CC1
CC1(N)CCN(c2ccnc(Cl)n2)CC1
null
null
C(Cl)Cl
Reduction
Hydrogenolysis of amides/imides/carbamates
3c33dd2a2d355ee5ba0287367e209aa147a39aa00607f0c95fb2bf1ade45d014
c5b5dffe7dd8beebdc1baa8b5b05300a9f7079e65dcfd42ade6f8a77ff09537d
c1cc(N2CCCCC2)ncn1
C-C(-C)(-C)-O-C(=O)-[NH;D2;+0:1]-[C:2](-[C;D1;H3:3])(-[C:4])-[C:5]>>[C:4]-[C:2](-[C;D1;H3:3])(-[NH2;D1;+0:1])-[C:5]
null
[]
null
null
1
HOUR
The procedure described in Example 2 is followed up to the end of step (c). A solution of 6.81 g (0.021 mol) of 4-t-butoxycarbonylamino-1-(2-chloropyrimidin-4-yl)-4-methylpiperidine (step c) in 80 ml of anhydrous methylene chloride is cooled under a nitrogen atmosphere and 16.4 ml of anisole and 83 ml of trifluoroaceti...
10.6084/m9.figshare.5104873.v1
null
Carbamic ester.Ether.Boc
Primary amine
null
null
C1CC[NH]CC1.c1cncnc1
HO-
C(Cl)Cl
null
1
CC1(NC(=O)OC(C)(C)C)CCN(c2ccnc(Cl)n2)CC1>C(Cl)Cl>CC1(N)CCN(c2ccnc(Cl)n2)CC1
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-4c3ca7fee7ca4cb68a75ae1c5be3919e
Cc1ccc(C(=O)O)cc1.O=S(Cl)Cl>>Cc1ccc(C(=O)Cl)cc1
CC1=CC=C(C(=O)O)C=C1.S(=O)(Cl)Cl>>CC1=CC=C(C(=O)Cl)C=C1
O[C:6]([c:5]1[cH:4][cH:3][c:2]([CH3:1])[cH:10][cH:9]1)=[O:7].O=S(Cl)[Cl:8]>>[CH3:1][c:2]1[cH:3][cH:4][c:5]([C:6](=[O:7])[Cl:8])[cH:9][cH:10]1
Cc1ccc(C(=O)O)cc1.O=S(Cl)Cl
Cc1ccc(C(=O)Cl)cc1
null
null
null
Functional Group Interconversion
Alcohol to chloride_SOCl2
c301c14a9dcd0670d52e8b77396cbe7fd8edeedd757bc43f4162ade1fc52fc93
787f545db5dc0b29dde55b5fbed7db8625b8055f49327f97ed4d83cc47c3af1d
c1ccccc1
Cl-S(=O)-[Cl;H0;D1;+0:1].O-[C;H0;D3;+0:2](=[O;D1;H0:3])-[c:4](:[c:5]):[c:6]>>[Cl;H0;D1;+0:1]-[C;H0;D3;+0:2](=[O;D1;H0:3])-[c:4](:[c:5]):[c:6]
null
[]
null
null
null
null
4-Methylbenzoyl chloride was prepared in a conventional manner from 4-methylbenzoic acid and thionyl chloride and after excess thionyl chloride was distilled off, was used as the crude product in the side chain chlorination. Conditions: See reaction.notes.procedure_details. Workup: after excess thionyl chloride was dis...
10.6084/m9.figshare.5104873.v1
null
Carboxylic acid
Acyl halide
null
null
c1ccccc1
HCl
null
null
null
Cc1ccc(C(=O)O)cc1.O=S(Cl)Cl>>Cc1ccc(C(=O)Cl)cc1
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-b9c7d389a33241bbb79d7412a80e13bc
CCCCCCCCCCOc1cnc(-c2ccc(C=CCCO)cc2)nc1>>CCCCCCCCCCOc1cnc(-c2ccc(CCCCO)cc2)nc1
OCCC=CC1=CC=C(C=C1)C1=NC=C(C=N1)OCCCCCCCCCC.[H][H].[H][H]>>OCCCCC1=CC=C(C=C1)C1=NC=C(C=N1)OCCCCCCCCCC
[CH3:1][CH2:2][CH2:3][CH2:4][CH2:5][CH2:6][CH2:7][CH2:8][CH2:9][CH2:10][O:11][c:12]1[cH:13][n:14][c:15](-[c:16]2[cH:17][cH:18][c:19]([CH:20]=[CH:21][CH2:22][CH2:23][OH:24])[cH:25][cH:26]2)[n:27][cH:28]1>>[CH3:1][CH2:2][CH2:3][CH2:4][CH2:5][CH2:6][CH2:7][CH2:8][CH2:9][CH2:10][O:11][c:12]1[cH:13][n:14][c:15](-[c:16]2[cH:...
CCCCCCCCCCOc1cnc(-c2ccc(C=CCCO)cc2)nc1
CCCCCCCCCCOc1cnc(-c2ccc(CCCCO)cc2)nc1
null
[Pd]
O1CCCC1
Reduction
Hydrogenation (double to single)
0bc3968b35f0839c230afb4215314da278abd4e1f10e42ec3012c5512de49ea5
312e9350dcad67590617294c0eb017edf0b9fbfe6133c06a3f393b871a889092
c1ccc(-c2ncccn2)cc1
[C:1]-[C:2]-[CH;D2;+0:3]=[CH;D2;+0:4]-[c:5](:[c:6]):[c:7]>>[C:1]-[C:2]-[CH2;D2;+0:3]-[CH2;D2;+0:4]-[c:5](:[c:6]):[c:7]
99
[{"value": 99.0, "product": "OCCCCC1=CC=C(C=C1)C1=NC=C(C=N1)OCCCCCCCCCC", "details": "PERCENTYIELD", "is_desired": false}]
null
null
null
null
0.38 g (1 mmol) of the thus obtained 2-(4-(4-hydroxy-1-butenyl) phenyl)-5-decyloxypyrimidine was dissolved in 20 ml of tetrahydrofuran, added with 0.05 g of 10% Pd/C and subjected to a hydrogenation reaction in a hydrogen atmosphere under normal pressure. The reaction was stopped when about 25 ml of hydrogen was consum...
10.6084/m9.figshare.5104873.v1
null
null
null
null
null
c1cncnc1.c1ccccc1
null
[Pd].O1CCCC1
null
null
CCCCCCCCCCOc1cnc(-c2ccc(C=CCCO)cc2)nc1>[Pd].O1CCCC1>CCCCCCCCCCOc1cnc(-c2ccc(CCCCO)cc2)nc1
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-8266c5cd4a68414b8c3137da7bc01eef
CCCCCCCCCCOc1cnc(-c2ccc(C(C)=O)cc2)nc1>>CCCCCCCCCCOc1cnc(-c2ccc(C(C)O)cc2)nc1
[BH4-].[Na+].C(C)(=O)C1=CC=C(C=C1)C1=NC=C(C=N1)OCCCCCCCCCC.C(C)O.C(Cl)(Cl)Cl>>OC(C)C1=CC=C(C=C1)C1=NC=C(C=N1)OCCCCCCCCCC
[CH3:1][CH2:2][CH2:3][CH2:4][CH2:5][CH2:6][CH2:7][CH2:8][CH2:9][CH2:10][O:11][c:12]1[cH:13][n:14][c:15](-[c:16]2[cH:17][cH:18][c:19]([C:20]([CH3:21])=[O:22])[cH:23][cH:24]2)[n:25][cH:26]1>>[CH3:1][CH2:2][CH2:3][CH2:4][CH2:5][CH2:6][CH2:7][CH2:8][CH2:9][CH2:10][O:11][c:12]1[cH:13][n:14][c:15](-[c:16]2[cH:17][cH:18][c:19...
CCCCCCCCCCOc1cnc(-c2ccc(C(C)=O)cc2)nc1
CCCCCCCCCCOc1cnc(-c2ccc(C(C)O)cc2)nc1
null
null
O
Reduction
Reduction of ketone to secondary alcohol
02790ac194d8bf7ccb13d6247c59412024d87f77d2c906ef7804f021f57d5070
1bd3cd74b454139c0a0068ac0135836499926b274bff569df163210c6c944a89
c1ccc(-c2ncccn2)cc1
[C;D1;H3:1]-[C;H0;D3;+0:2](=[O;H0;D1;+0:3])-[c:4](:[c:5]):[c:6]>>[C;D1;H3:1]-[CH;D3;+0:2](-[OH;D1;+0:3])-[c:4](:[c:5]):[c:6]
100.3
[{"value": 100.0, "product": "OC(C)C1=CC=C(C=C1)C1=NC=C(C=N1)OCCCCCCCCCC", "details": "PERCENTYIELD", "is_desired": false}, {"value": 100.3, "product": "OC(C)C1=CC=C(C=C1)C1=NC=C(C=N1)OCCCCCCCCCC", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
4
HOUR
35.5 g (0.1 mo1) of 2-(4-acetylphenyl)-5-decyloxypyrimidine, 300 ml of ethanol and 300 ml of chloroform were supplied into a four-necked flask equipped with a stirrer and a thermometer. Then 2.8 g (0.075 mol) of sodium borohydride was added at 30°-40° C. and the mixture was stirred at the same temperature for 4 hours. ...
10.6084/m9.figshare.5104873.v1
null
Ketone
Secondary alcohol
null
null
c1cncnc1.c1ccccc1
null
O
null
4
CCCCCCCCCCOc1cnc(-c2ccc(C(C)=O)cc2)nc1>O>CCCCCCCCCCOc1cnc(-c2ccc(C(C)O)cc2)nc1
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-01a269bda00c4ee495d089d890ae2b6c
CCCCCCCCCCOc1cnc(-c2ccc(C(C)OC(C)=O)cc2)nc1>>CCCCCCCCCCOc1cnc(-c2ccc(C(C)O)cc2)nc1
C(C)(=O)OC(C)C1=CC=C(C=C1)C1=NC=C(C=N1)OCCCCCCCCCC>>OC(C)C1=CC=C(C=C1)C1=NC=C(C=N1)OCCCCCCCCCC
CC(=O)[O:22][CH:20]([c:19]1[cH:18][cH:17][c:16](-[c:15]2[n:14][cH:13][c:12]([O:11][CH2:10][CH2:9][CH2:8][CH2:7][CH2:6][CH2:5][CH2:4][CH2:3][CH2:2][CH3:1])[cH:26][n:25]2)[cH:24][cH:23]1)[CH3:21]>>[CH3:1][CH2:2][CH2:3][CH2:4][CH2:5][CH2:6][CH2:7][CH2:8][CH2:9][CH2:10][O:11][c:12]1[cH:13][n:14][c:15](-[c:16]2[cH:17][cH:18...
CCCCCCCCCCOc1cnc(-c2ccc(C(C)OC(C)=O)cc2)nc1
CCCCCCCCCCOc1cnc(-c2ccc(C(C)O)cc2)nc1
null
null
[OH-].[Na+].CO
Reduction
Hydrolysis or Hydrogenolysis of Carboxylic Esters or Thioesters
d7acfb2397f2b5b2a83b3bebf3698d6d984dd716982297f62a944222c79ce234
19dd58e0f83625e74b4b1375d88cb4c813ee60f593d812516d14eafc4ab68dc7
c1ccc(-c2ncccn2)cc1
C-C(=O)-[O;H0;D2;+0:1]-[C:2](-[C;D1;H3:3])-[c:4]>>[C;D1;H3:3]-[C:2](-[OH;D1;+0:1])-[c:4]
null
[]
30
CELSIUS
2
HOUR
4 g of the above product (-)-(4-(1-acetoxyethyl) phenyl)-5-decyloxypyrimidine was dissolved in a mixture of 50 ml of methanol and 10 ml of a 20% sodium hydroxide solution, stirred at 30° C. for 2 hours and hydrolyzed, and the resulting reaction solution was extracted by adding 200 ml of water and 200 ml of toluene, fol...
10.6084/m9.figshare.5104873.v1
null
Ester
Secondary alcohol
null
null
c1cncnc1.c1ccccc1
HO-
[OH-].[Na+].CO
30
2
CCCCCCCCCCOc1cnc(-c2ccc(C(C)OC(C)=O)cc2)nc1>[OH-].[Na+].CO>CCCCCCCCCCOc1cnc(-c2ccc(C(C)O)cc2)nc1
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-aa775880ee5b480896f2619381c4dc7e
CCCCCCCCCCOc1cnc(-c2ccc(C=CC(O)C(F)(F)F)cc2)nc1>>CCCCCCCCCCOc1cnc(-c2ccc(C=CC(OCCCC)C(F)(F)F)cc2)nc1
OC(C=CC1=CC=C(C=C1)C1=NC=C(C=N1)OCCCCCCCCCC)C(F)(F)F>>C(CCC)OC(C=CC1=CC=C(C=C1)C1=NC=C(C=N1)OCCCCCCCCCC)C(F)(F)F
[CH3:1][CH2:2][CH2:3][CH2:4][CH2:5][CH2:6][CH2:7][CH2:8][CH2:9][CH2:10][O:11][c:12]1[cH:13][n:14][c:15](-[c:16]2[cH:17][cH:18][c:19]([CH:20]=[CH:21][CH:22]([OH:23])[C:28]([F:29])([F:30])[F:31])[cH:32][cH:33]2)[n:34][cH:24]1>>[CH3:1][CH2:2][CH2:3][CH2:4][CH2:5][CH2:6][CH2:7][CH2:8][CH2:9][CH2:10][O:11][c:12]1[cH:13][n:1...
CCCCCCCCCCOc1cnc(-c2ccc(C=CC(O)C(F)(F)F)cc2)nc1
CCCCCCCCCCOc1cnc(-c2ccc(C=CC(OCCCC)C(F)(F)F)cc2)nc1
null
[Ag]=O
C(CCC)I
Functional Group Interconversion
OtherReaction
1f8b4f749d7b68e358abf6dadca641af7be42cbed7d6129cc817b66a2815d76b
1986048cb9f2a7cc7e0c9d12b7a8bd2e76fdd82b5837c7e5982a2b2c413cbea0
c1ccc(-c2ncccn2)cc1
[C:1]-[#8:2]-[c;H0;D3;+0:3]1:[c:4]:[#7;a:5]:[c:6](-[c:7]):[n;H0;D2;+0:8]:[cH;D2;+0:9]:1.[F;D1;H0:10]-[C:11](-[F;D1;H0:12])(-[F;D1;H0:13])-[C:14](-[OH;D1;+0:15])-[C:16]=[C:17]-[c:18]>>[C:1]-[#8:2]-[c;H0;D3;+0:3]1:[c:4]:[#7;a:5]:[c:6](-[c:7]):[n;H0;D2;+0:8]:[c:19]:1.[C:20]-[C:21]-[CH2;D2;+0:9]-[O;H0;D2;+0:15]-[C:14](-[C:...
173.7
[{"value": 173.7, "product": "C(CCC)OC(C=CC1=CC=C(C=C1)C1=NC=C(C=N1)OCCCCCCCCCC)C(F)(F)F", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
4
DAY
1.0 g of (-)-2-(4-(3-hydroxy-4,4,4-trifluoro-1-butenyl) phenyl)-5-decyloxypyrimidine was dissolved in 5 ml of butyl iodide. The solution was added with 3 g of silver oxide and stirred at 25°-30° C. for 4 days. The reaction mixture was cleared of silver oxide by filtration and concentrated under reduced pressure, and th...
10.6084/m9.figshare.5104873.v1
null
Ether.Secondary alcohol
Ether.Ether
c1cncnc1
c1cncnc1
c1cncnc1.c1ccccc1
Other
[Ag]=O.C(CCC)I
null
96
CCCCCCCCCCOc1cnc(-c2ccc(C=CC(O)C(F)(F)F)cc2)nc1>[Ag]=O.C(CCC)I>CCCCCCCCCCOc1cnc(-c2ccc(C=CC(OCCCC)C(F)(F)F)cc2)nc1
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-a527bf234aeb411088cf0a7588b93b15
CCCC(=O)Cl.CCCCCCCCCCOc1cnc(-c2ccc(C=CC(O)C(F)(F)F)cc2)nc1>>CCCCCCCCCCOc1cnc(-c2ccc(C=CC(OC(=O)CCC)C(F)(F)F)cc2)nc1
OC(C=CC1=CC=C(C=C1)C1=NC=C(C=N1)OCCCCCCCCCC)C(F)(F)F.C(CCC)(=O)Cl>>C(CCC)(=O)OC(C=CC1=CC=C(C=C1)C1=NC=C(C=N1)OCCCCCCCCCC)C(F)(F)F
Cl[C:24](=[O:25])[CH2:26][CH2:27][CH3:28].[CH3:1][CH2:2][CH2:3][CH2:4][CH2:5][CH2:6][CH2:7][CH2:8][CH2:9][CH2:10][O:11][c:12]1[cH:13][n:14][c:15](-[c:16]2[cH:17][cH:18][c:19]([CH:20]=[CH:21][CH:22]([OH:23])[C:29]([F:30])([F:31])[F:32])[cH:33][cH:34]2)[n:35][cH:36]1>>[CH3:1][CH2:2][CH2:3][CH2:4][CH2:5][CH2:6][CH2:7][CH2...
CCCC(=O)Cl.CCCCCCCCCCOc1cnc(-c2ccc(C=CC(O)C(F)(F)F)cc2)nc1
CCCCCCCCCCOc1cnc(-c2ccc(C=CC(OC(=O)CCC)C(F)(F)F)cc2)nc1
null
null
C1(=CC=CC=C1)C.N1=CC=CC=C1
Acylation
Schotten-Baumann to ester
27b76e29491fa7db5375755e15223de884a194f57a493147db0b5495ea981908
d47ab90ace9b5dcd818151c10aae400dcf599f5a3476072b8dfedc474e97c335
c1ccc(-c2ncccn2)cc1
Cl-[C;H0;D3;+0:1](=[O;D1;H0:2])-[C:3]-[C:4].[F;D1;H0:5]-[C:6](-[F;D1;H0:7])(-[F;D1;H0:8])-[C:9](-[OH;D1;+0:10])-[C:11]=[C:12]-[c:13]>>[C:4]-[C:3]-[C;H0;D3;+0:1](=[O;D1;H0:2])-[O;H0;D2;+0:10]-[C:9](-[C:11]=[C:12]-[c:13])-[C:6](-[F;D1;H0:5])(-[F;D1;H0:7])-[F;D1;H0:8]
93.1
[{"value": 93.1, "product": "C(CCC)(=O)OC(C=CC1=CC=C(C=C1)C1=NC=C(C=N1)OCCCCCCCCCC)C(F)(F)F", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
4
HOUR
1.0 g of (-)-2-(4-(3-hydroxy-4,4,4-trifluoro-1-butenyl) phenyl)-5-decyloxypyrimidine was dissolved in 20 ml of pyridine. The solution was added with 0.5 g of butyryl chloride and stirred at 25°-30° C. for 4 hours. The reaction mixture was diluted with 100 ml of toluene and washed with 4N hydrochloric acid, water, a 5% ...
10.6084/m9.figshare.5104873.v1
null
Acyl halide.Secondary alcohol
Ester
null
null
c1cncnc1.c1ccccc1
HCl
C1(=CC=CC=C1)C.N1=CC=CC=C1
null
4
CCCC(=O)Cl.CCCCCCCCCCOc1cnc(-c2ccc(C=CC(O)C(F)(F)F)cc2)nc1>C1(=CC=CC=C1)C.N1=CC=CC=C1>CCCCCCCCCCOc1cnc(-c2ccc(C=CC(OC(=O)CCC)C(F)(F)F)cc2)nc1
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-5085d0f6c9584e6a85f4d46b48c68abb
CCCCCCCCC(=O)Cl.CCCCCCCCCCOc1cnc(-c2ccc(CCCC(O)C(F)(F)F)cc2)nc1>>CCCCCCCCCCOc1cnc(-c2ccc(CCCC(OC(=O)CCCCCCCC)C(F)(F)F)cc2)nc1
OC(CCCC1=CC=C(C=C1)C1=NC=C(C=N1)OCCCCCCCCCC)C(F)(F)F.C(CCCCCCCC)(=O)Cl>>C(CCCCCCCC)(=O)OC(CCCC1=CC=C(C=C1)C1=NC=C(C=N1)OCCCCCCCCCC)C(F)(F)F
Cl[C:25](=[O:26])[CH2:27][CH2:28][CH2:29][CH2:30][CH2:31][CH2:32][CH2:33][CH3:34].[CH3:1][CH2:2][CH2:3][CH2:4][CH2:5][CH2:6][CH2:7][CH2:8][CH2:9][CH2:10][O:11][c:12]1[cH:13][n:14][c:15](-[c:16]2[cH:17][cH:18][c:19]([CH2:20][CH2:21][CH2:22][CH:23]([OH:24])[C:35]([F:36])([F:37])[F:38])[cH:39][cH:40]2)[n:41][cH:42]1>>[CH3...
CCCCCCCCC(=O)Cl.CCCCCCCCCCOc1cnc(-c2ccc(CCCC(O)C(F)(F)F)cc2)nc1
CCCCCCCCCCOc1cnc(-c2ccc(CCCC(OC(=O)CCCCCCCC)C(F)(F)F)cc2)nc1
null
null
C1(=CC=CC=C1)C.N1=CC=CC=C1
Acylation
Schotten-Baumann to ester
27b76e29491fa7db5375755e15223de884a194f57a493147db0b5495ea981908
d47ab90ace9b5dcd818151c10aae400dcf599f5a3476072b8dfedc474e97c335
c1ccc(-c2ncccn2)cc1
Cl-[C;H0;D3;+0:1](=[O;D1;H0:2])-[C:3]-[C:4].[C:5]-[C:6](-[OH;D1;+0:7])-[C:8](-[F;D1;H0:9])(-[F;D1;H0:10])-[F;D1;H0:11]>>[C:5]-[C:6](-[O;H0;D2;+0:7]-[C;H0;D3;+0:1](=[O;D1;H0:2])-[C:3]-[C:4])-[C:8](-[F;D1;H0:9])(-[F;D1;H0:10])-[F;D1;H0:11]
null
[]
null
null
null
null
1.1 g (2.5 mmol) of (-)-2-(4-(4-hydroxy-5,5,5-trifluoro-1-pentyl)phenyl)-5-decyloxypyrimidine was dissolved in 10 ml of pyridine, followed by addition of 0.53 g (3 mmol) of nonanoyl chloride and 2-hour reaction at 20°-30° C. The reaction mixture was diluted with 100 ml of toluene, and the toluene layer was washed with ...
10.6084/m9.figshare.5104873.v1
null
Acyl halide.Secondary alcohol
Ester
null
null
c1cncnc1.c1ccccc1
HCl
C1(=CC=CC=C1)C.N1=CC=CC=C1
null
null
CCCCCCCCC(=O)Cl.CCCCCCCCCCOc1cnc(-c2ccc(CCCC(O)C(F)(F)F)cc2)nc1>C1(=CC=CC=C1)C.N1=CC=CC=C1>CCCCCCCCCCOc1cnc(-c2ccc(CCCC(OC(=O)CCCCCCCC)C(F)(F)F)cc2)nc1
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-9b515fcf22a54464836bc78f7d1d5c2e
CCCC(=O)Cl.CCCCCCCCCCOc1cnc(-c2ccc(C=CC(C)O)cc2)nc1>>CCCCCCCCCCOc1cnc(-c2ccc(C=CC(C)OC(=O)CCC)cc2)nc1
OC(C=CC1=CC=C(C=C1)C1=NC=C(C=N1)OCCCCCCCCCC)C.C(CCC)(=O)Cl>>C(CCC)(=O)OC(C=CC1=CC=C(C=C1)C1=NC=C(C=N1)OCCCCCCCCCC)C
Cl[C:25](=[O:26])[CH2:27][CH2:28][CH3:29].[CH3:1][CH2:2][CH2:3][CH2:4][CH2:5][CH2:6][CH2:7][CH2:8][CH2:9][CH2:10][O:11][c:12]1[cH:13][n:14][c:15](-[c:16]2[cH:17][cH:18][c:19]([CH:20]=[CH:21][CH:22]([CH3:23])[OH:24])[cH:30][cH:31]2)[n:32][cH:33]1>>[CH3:1][CH2:2][CH2:3][CH2:4][CH2:5][CH2:6][CH2:7][CH2:8][CH2:9][CH2:10][O...
CCCC(=O)Cl.CCCCCCCCCCOc1cnc(-c2ccc(C=CC(C)O)cc2)nc1
CCCCCCCCCCOc1cnc(-c2ccc(C=CC(C)OC(=O)CCC)cc2)nc1
null
null
C1(=CC=CC=C1)C.N1=CC=CC=C1
Acylation
Schotten-Baumann to ester
27b76e29491fa7db5375755e15223de884a194f57a493147db0b5495ea981908
d47ab90ace9b5dcd818151c10aae400dcf599f5a3476072b8dfedc474e97c335
c1ccc(-c2ncccn2)cc1
Cl-[C;H0;D3;+0:1](=[O;D1;H0:2])-[C:3]-[C:4].[C;D1;H3:5]-[C:6](-[OH;D1;+0:7])-[C:8]=[C:9]-[c:10]>>[C:4]-[C:3]-[C;H0;D3;+0:1](=[O;D1;H0:2])-[O;H0;D2;+0:7]-[C:6](-[C;D1;H3:5])-[C:8]=[C:9]-[c:10]
88.7
[{"value": 88.7, "product": "C(CCC)(=O)OC(C=CC1=CC=C(C=C1)C1=NC=C(C=N1)OCCCCCCCCCC)C", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
4
HOUR
1.0 g of (-)-2-(4-(3-hydroxy-1-butenyl)phenyl)-5-decyloxypyrimidine was dissolved in 20 ml of pyridine, added with 0.5 g of butyryl chloride and stirred at 25°-30° C. for 4 hours. The reaction mixture was diluted with 100 ml of toluene and washed with 4N hydrochloric acid, water, a 5% sodium bicarbonate solution and wa...
10.6084/m9.figshare.5104873.v1
null
Acyl halide.Secondary alcohol
Ester
null
null
c1cncnc1.c1ccccc1
HCl
C1(=CC=CC=C1)C.N1=CC=CC=C1
null
4
CCCC(=O)Cl.CCCCCCCCCCOc1cnc(-c2ccc(C=CC(C)O)cc2)nc1>C1(=CC=CC=C1)C.N1=CC=CC=C1>CCCCCCCCCCOc1cnc(-c2ccc(C=CC(C)OC(=O)CCC)cc2)nc1
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-db70288e9ca54cb89358931186bc5974
N#[N+]c1ccc(Cl)cc1.Nc1cc(Cl)nc(N)n1>>Nc1nc(N)c(N=Nc2ccc(Cl)cc2)c(Cl)n1
ClC1=NC(=NC(=C1)N)N.C(C)(=O)[O-].[Na+].[Cl-].ClC1=CC=C(C=C1)[N+]#N>>ClC1=C(C(=NC(=N1)N)N)N=NC1=CC=C(C=C1)Cl
[N:7]#[N+:8][c:9]1[cH:10][cH:11][c:12]([Cl:13])[cH:14][cH:15]1.[NH2:1][c:2]1[n:3][c:4]([NH2:5])[cH:6][c:16]([Cl:17])[n:18]1>>[NH2:1][c:2]1[n:3][c:4]([NH2:5])[c:6]([N:7]=[N:8][c:9]2[cH:10][cH:11][c:12]([Cl:13])[cH:14][cH:15]2)[c:16]([Cl:17])[n:18]1
N#[N+]c1ccc(Cl)cc1.Nc1cc(Cl)nc(N)n1
Nc1nc(N)c(N=Nc2ccc(Cl)cc2)c(Cl)n1
null
null
C(C)(=O)O.O
Functional Group Addition
OtherReaction
59dbef215a5e5b8c943f9f2b2cb274bbf73bcb989858c51965027a5e963c218e
2c6cd95d4efa78d9d3de76e13585ebc8f102df9229b31c028b4deed5aad0dd25
c1ccc(N=Nc2cncnc2)cc1
[Cl;D1;H0:1]-[c:2]1:[#7;a:3]:[c:4]:[#7;a:5]:[c:6](-[N;D1;H2:7]):[cH;D2;+0:8]:1.[N;H0;D1;+0:9]#[N+;H0;D2:10]-[c:11](:[c:12]):[c:13]>>[Cl;D1;H0:1]-[c:2]1:[#7;a:3]:[c:4]:[#7;a:5]:[c:6](-[N;D1;H2:7]):[c;H0;D3;+0:8]:1-[N;H0;D2;+0:9]=[N;H0;D2;+0:10]-[c:11](:[c:12]):[c:13]
41.4
[{"value": 41.4, "product": "ClC1=C(C(=NC(=N1)N)N)N=NC1=CC=C(C=C1)Cl", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
20
MINUTE
To a suspension of 4-chloro-2,6-diaminopyrimidine (21.68 g, 0.150 mol) in water (750 ml) and acetic acid (750 ml) was added sodium acetate (300 g). Solution occurred after stirring for 20 minutes, and then the solution of 4-chlorobenzenediazonium chloride (0.166 mol) was added with cooling over 30 minutes at a rate tha...
10.6084/m9.figshare.5104873.v1
null
null
Diazene
c1cncnc1
c1cncnc1
c1cncnc1.c1ccccc1
null
C(C)(=O)O.O
null
0.333333
N#[N+]c1ccc(Cl)cc1.Nc1cc(Cl)nc(N)n1>C(C)(=O)O.O>Nc1nc(N)c(N=Nc2ccc(Cl)cc2)c(Cl)n1
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-63652823dab044f195e03b0122ca1c8d
Nc1nc(N)c(N=Nc2ccc(Cl)cc2)c(Cl)n1>>Nc1nc(N)c(N)c(Cl)n1
ClC1=C(C(=NC(=N1)N)N)N=NC1=CC=C(C=C1)Cl>>ClC1=C(C(=NC(=N1)N)N)N
Clc1ccc(N=[N:7][c:6]2[c:4]([NH2:5])[n:3][c:2]([NH2:1])[n:10][c:8]2[Cl:9])cc1>>[NH2:1][c:2]1[n:3][c:4]([NH2:5])[c:6]([NH2:7])[c:8]([Cl:9])[n:10]1
Nc1nc(N)c(N=Nc2ccc(Cl)cc2)c(Cl)n1
Nc1nc(N)c(N)c(Cl)n1
null
[Zn]
C(C)(=O)O.C(C)O.O
Deprotection
OtherReaction
0722c3cf3c652bcadbf2fd556ba1691a180af92ae74607c0f7d0965c24b92a49
16b76cc963cfd15c080c900b77fa1174c8de86c98ea02220734eaeb14bc96073
c1cncnc1
Cl-c1:c:c:c(-N=[N;H0;D2;+0:1]-[c:2]2:[c:3](-[N;D1;H2:4]):[#7;a:5]:[c:6]:[#7;a:7]:[c:8]:2-[Cl;D1;H0:9]):c:c:1>>[Cl;D1;H0:9]-[c:8]1:[#7;a:7]:[c:6]:[#7;a:5]:[c:3](-[N;D1;H2:4]):[c:2]:1-[NH2;D1;+0:1]
75.7
[{"value": 75.7, "product": "ClC1=C(C(=NC(=N1)N)N)N", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
3
DAY
A suspension of 6-chloro-5-[(4-chlorophenyl)azo]-2,4-pyrimidinediamine (24.55 g, 0.0906 mol) in ethanol (640 ml), water (640 ml) and acetic acid (64 ml) was heated to 70° under nitrogen. Zinc dust (75 g) was added slowly over 1 hour, and then the reaction was stirred an additional hour at 70°. Then the reaction was coo...
10.6084/m9.figshare.5104873.v1
null
Aromatic halide.Diazene
Primary amine
c1ccccc1
null
c1cncnc1
HCl
[Zn].C(C)(=O)O.C(C)O.O
null
72
Nc1nc(N)c(N=Nc2ccc(Cl)cc2)c(Cl)n1>[Zn].C(C)(=O)O.C(C)O.O>Nc1nc(N)c(N)c(Cl)n1
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-b26f3f6bab4540adb2aaf83c30a9a560
N#Cc1ccc2[nH]cc(CCCCCl)c2c1.NC(=O)c1cc2cc(N3CCNCC3)ccc2o1>>N#Cc1ccc2[nH]cc(CCCCN3CCN(c4ccc5oc(C(N)=O)cc5c4)CC3)c2c1
N1(CCNCC1)C=1C=CC2=C(C=C(O2)C(=O)N)C1.ClCCCCC1=CNC2=CC=C(C=C12)C#N>>C(#N)C=1C=C2C(=CNC2=CC1)CCCCN1CCN(CC1)C=1C=CC2=C(C=C(O2)C(N)=O)C1
Cl[CH2:13][CH2:12][CH2:11][CH2:10][c:9]1[cH:8][nH:7][c:6]2[cH:5][cH:4][c:3]([C:2]#[N:1])[cH:33][c:32]21.[NH:14]1[CH2:15][CH2:16][N:17]([c:18]2[cH:19][cH:20][c:21]3[o:22][c:23]([C:24]([NH2:25])=[O:26])[cH:27][c:28]3[cH:29]2)[CH2:30][CH2:31]1>>[N:1]#[C:2][c:3]1[cH:4][cH:5][c:6]2[nH:7][cH:8][c:9]([CH2:10][CH2:11][CH2:12][...
N#Cc1ccc2[nH]cc(CCCCCl)c2c1.NC(=O)c1cc2cc(N3CCNCC3)ccc2o1
N#Cc1ccc2[nH]cc(CCCCN3CCN(c4ccc5oc(C(N)=O)cc5c4)CC3)c2c1
null
null
null
Heteroatom Alkylation and Arylation
N-alkylation of secondary amines with alkyl halides
bad6b7d8e43c3debef0c262d60564e43415b41bcee72e526419c8c16be18fec1
523d37155b42c8dc851abeddadebb241cdd90bdf649ba750c35e13c8c752d7b0
c1ccc2c(CCCCN3CCN(c4ccc5occc5c4)CC3)c[nH]c2c1
Cl-[CH2;D2;+0:1]-[C:2]-[C:3].[#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
null
[]
null
null
null
null
5-(1-piperazinyl)benzofuran-2-carboxamide or a corresponding salt is reacted with 3-(4-chlorobutyl)-5-cyanoindole to give 1-[4-(5-cyanoindol-3-yl)butyl]-4-(2-carbamoylbenzofuran-5-yl)piperazine and optionally then converted into its acid addition salt. Conditions: See reaction.notes.procedure_details.
10.6084/m9.figshare.5104873.v1
null
Primary halide.Secondary amine
Tertiary amine
C1CNCC[NH]1
C1C[NH]CC[NH]1
c1ccc2[nH]ccc2c1.C1C[NH]CC[NH]1.c1ccc2occc2c1
HCl
null
null
null
N#Cc1ccc2[nH]cc(CCCCCl)c2c1.NC(=O)c1cc2cc(N3CCNCC3)ccc2o1>>N#Cc1ccc2[nH]cc(CCCCN3CCN(c4ccc5oc(C(N)=O)cc5c4)CC3)c2c1
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-fb1ddf8127a44d35bcac2a8bffbfe5d1
CCOC(=O)c1cc2cc([N+](=O)[O-])ccc2o1>>CCOC(=O)c1cc2cc(N)ccc2o1
[N+](=O)([O-])C=1C=CC2=C(C=C(O2)C(=O)OCC)C1>>NC=1C=CC2=C(C=C(O2)C(=O)OCC)C1
O=[N+:11]([O-])[c:10]1[cH:9][c:8]2[cH:7][c:6]([C:4]([O:3][CH2:2][CH3:1])=[O:5])[o:15][c:14]2[cH:13][cH:12]1>>[CH3:1][CH2:2][O:3][C:4](=[O:5])[c:6]1[cH:7][c:8]2[cH:9][c:10]([NH2:11])[cH:12][cH:13][c:14]2[o:15]1
CCOC(=O)c1cc2cc([N+](=O)[O-])ccc2o1
CCOC(=O)c1cc2cc(N)ccc2o1
null
[Ni]
CO
Reduction
Reduction of nitro groups to amines
bbc242b150a51e69d3ad1caaa391f4422710431b398dcb880555f476706790be
7b0317532ea57a4fcedc1efc3e3c22eb5238d1c8330da53d4f9801fc2391f567
c1ccc2occc2c1
O=[N+;H0;D3:1](-[O-])-[c:2](:[c:3]):[c:4]>>[NH2;D1;+0:1]-[c:2](:[c:3]):[c:4]
null
[]
null
null
null
null
A solution of 2.3 g of ethyl 5-nitrobenzofuran-2-carboxylate in 60 ml of methanol is hydrogenated in the presence of Raney nickel. The catalyst is filtered off and the solution is concentrated. After customary working up, ethyl 5-aminobenzofuran-2-carboxylate, Rf 0.1 (dichloromethane/ethanol 9.5:0.5) obtained; hydrochl...
10.6084/m9.figshare.5104873.v1
null
Nitro group
Primary amine
null
null
c1ccc2occc2c1
Other
[Ni].CO
null
null
CCOC(=O)c1cc2cc([N+](=O)[O-])ccc2o1>[Ni].CO>CCOC(=O)c1cc2cc(N)ccc2o1
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-7d431b55cb724be5bee26d49a4283c0c
CCOC(=O)c1cc2cc(N3CCN(C(=O)OC(C)(C)C)CC3)ccc2o1.NC=O>>CC(C)(C)OC(=O)N1CCN(c2ccc3oc(C(N)=O)cc3c2)CC1
C(C)(C)(C)OC(=O)N1CCN(CC1)C=1C=CC2=C(C=C(O2)C(=O)OCC)C1.C(=O)N>>C(C)(C)(C)OC(=O)N1CCN(CC1)C=1C=CC2=C(C=C(O2)C(=O)N)C1
CCO[C:18]([c:17]1[o:16][c:15]2[cH:14][cH:13][c:12]([N:11]3[CH2:10][CH2:9][N:8]([C:6]([O:5][C:2]([CH3:1])([CH3:3])[CH3:4])=[O:7])[CH2:25][CH2:24]3)[cH:23][c:22]2[cH:21]1)=[O:20].O=C[NH2:19]>>[CH3:1][C:2]([CH3:3])([CH3:4])[O:5][C:6](=[O:7])[N:8]1[CH2:9][CH2:10][N:11]([c:12]2[cH:13][cH:14][c:15]3[o:16][c:17]([C:18]([NH2:1...
CCOC(=O)c1cc2cc(N3CCN(C(=O)OC(C)(C)C)CC3)ccc2o1.NC=O
CC(C)(C)OC(=O)N1CCN(c2ccc3oc(C(N)=O)cc3c2)CC1
null
null
CN1C(CCC1)=O
Acylation
OtherReaction
8485ff0c27805637c203a0305c6b23f92c4eeb142cc0b7710a60928ccd98fb24
6966630ca7488e58a1b66dece4d4906c351d42d1615b3e81f8c9466448df6023
c1cc2cc(N3CCNCC3)ccc2o1
C-C-O-[C;H0;D3;+0:1](=[O;D1;H0:2])-[c:3](:[c:4]):[#8;a:5]:[c:6].O=C-[NH2;D1;+0:7]>>[NH2;D1;+0:7]-[C;H0;D3;+0:1](=[O;D1;H0:2])-[c:3](:[c:4]):[#8;a:5]:[c:6]
null
[]
null
null
null
null
A solution of 3 g of ethyl 5-(4-tert-butoxycarbonyl-1-piperazinyl)benzofuran-2-carboxylate in 100 ml of N-methylpyrrolidone is stirred for 5 hours with 1 g of formamide and 3 g of sodium alkoxide. After customary working up, 5-(4-tert-butoxycarbonyl-1-piperazinyl)benzofuran-2-carboxamide, m.p. 198°-200°, is obtained. C...
10.6084/m9.figshare.5104873.v1
null
Ester.Primary amide
Primary amide
null
null
C1C[NH]CC[NH]1.c1ccc2occc2c1
HO-
CN1C(CCC1)=O
null
null
CCOC(=O)c1cc2cc(N3CCN(C(=O)OC(C)(C)C)CC3)ccc2o1.NC=O>CN1C(CCC1)=O>CC(C)(C)OC(=O)N1CCN(c2ccc3oc(C(N)=O)cc3c2)CC1
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-9767918db3564609a907b285260c24dc
CCOC(=O)c1cc2cc(N3CCNCC3)ccc2o1.ClCc1ccccc1>>CCOC(=O)c1cc2cc(N3CCN(Cc4ccccc4)CC3)ccc2o1
N1(CCNCC1)C=1C=CC2=C(C=C(O2)C(=O)OCC)C1.C(C1=CC=CC=C1)Cl>>C(C1=CC=CC=C1)N1CCN(CC1)C=1C=CC2=C(C=C(O2)C(=O)OCC)C1
[CH3:1][CH2:2][O:3][C:4](=[O:5])[c:6]1[cH:7][c:8]2[cH:9][c:10]([N:11]3[CH2:12][CH2:13][NH:14][CH2:22][CH2:23]3)[cH:24][cH:25][c:26]2[o:27]1.Cl[CH2:15][c:16]1[cH:17][cH:18][cH:19][cH:20][cH:21]1>>[CH3:1][CH2:2][O:3][C:4](=[O:5])[c:6]1[cH:7][c:8]2[cH:9][c:10]([N:11]3[CH2:12][CH2:13][N:14]([CH2:15][c:16]4[cH:17][cH:18][cH...
CCOC(=O)c1cc2cc(N3CCNCC3)ccc2o1.ClCc1ccccc1
CCOC(=O)c1cc2cc(N3CCN(Cc4ccccc4)CC3)ccc2o1
null
null
ClCCl
Heteroatom Alkylation and Arylation
N-alkylation of secondary amines with alkyl halides
b703623ddc3b029d4716c15f5414f41773434bcc7e3f3853faf62273596bed77
523d37155b42c8dc851abeddadebb241cdd90bdf649ba750c35e13c8c752d7b0
c1ccc(CN2CCN(c3ccc4occc4c3)CC2)cc1
Cl-[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:7]-[C:6]-[#7:5]-[C:10]-[C:9]-1):[c:4]
null
[]
null
null
2
HOUR
A solution of 1 g of ethyl 5-(1-piperazinyl)-benzofuran-2-carboxylate in 50 ml of dichloromethane is treated with 1 g of benzyl chloride and stirred for 2 hours. After customary working up, ethyl 5-(4-benzyl-1-piperazinyl)benzofuran-2-carboxylate, m.p. 219°-222°, is obtained. Conditions: See reaction.notes.procedure_de...
10.6084/m9.figshare.5104873.v1
null
Primary halide.Secondary amine
Tertiary amine
C1C[NH]CCN1
C1C[NH]CC[NH]1
c1ccc2occc2c1.C1C[NH]CC[NH]1.c1ccccc1
HCl
ClCCl
null
2
CCOC(=O)c1cc2cc(N3CCNCC3)ccc2o1.ClCc1ccccc1>ClCCl>CCOC(=O)c1cc2cc(N3CCN(Cc4ccccc4)CC3)ccc2o1
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-b5c1249063ad41ecb9a886e640b8e144
CC(C)(C)OC(=O)N1CCN(c2ccc3oc(C(N)=O)cc3c2)CC1>>NC(=O)c1cc2cc(N3CCNCC3)ccc2o1
C(C)(C)(C)OC(=O)N1CCN(CC1)C=1C=CC2=C(C=C(O2)C(=O)N)C1>>N1(CCNCC1)C=1C=CC2=C(C=C(O2)C(=O)N)C1
CC(C)(C)OC(=O)[N:12]1[CH2:11][CH2:10][N:9]([c:8]2[cH:7][c:6]3[cH:5][c:4]([C:2]([NH2:1])=[O:3])[o:18][c:17]3[cH:16][cH:15]2)[CH2:14][CH2:13]1>>[NH2:1][C:2](=[O:3])[c:4]1[cH:5][c:6]2[cH:7][c:8]([N:9]3[CH2:10][CH2:11][NH:12][CH2:13][CH2:14]3)[cH:15][cH:16][c:17]2[o:18]1
CC(C)(C)OC(=O)N1CCN(c2ccc3oc(C(N)=O)cc3c2)CC1
NC(=O)c1cc2cc(N3CCNCC3)ccc2o1
null
null
Cl
Reduction
Boc amine deprotection
2c25e19aee181a3c5131cfdfda27035fd54d4379a11d745dfb75d386bacfd500
a94b29c7264c852156fc1cdd4a0951a4fc26c06d0edc9e50c743825dbf79e3fd
c1cc2cc(N3CCNCC3)ccc2o1
C-C(-C)(-C)-O-C(=O)-[N;H0;D3;+0:1]1-[C:2]-[C:3]-[#7:4]-[C:5]-[C:6]-1>>[#7:4]1-[C:3]-[C:2]-[NH;D2;+0:1]-[C:6]-[C:5]-1
null
[]
null
null
null
null
1 g of 5-(4-tert-butoxycarbonyl-1-piperazinyl)-benzofuran-2-carboxamide is dissolved in 50 ml of methanolic HCl and stirred for I hour. After customary working up, 5-(1-piperazinyl)benzofuran-2-carboxamide, m.p. 252°-255°, is obtained. Conditions: See reaction.notes.procedure_details.
10.6084/m9.figshare.5104873.v1
null
Carbamic ester.Ether.Boc
Secondary amine
C1C[NH]CC[NH]1
C1C[NH]CCN1
c1ccc2occc2c1.C1C[NH]CCN1
HO-
Cl
null
null
CC(C)(C)OC(=O)N1CCN(c2ccc3oc(C(N)=O)cc3c2)CC1>Cl>NC(=O)c1cc2cc(N3CCNCC3)ccc2o1
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-185abfaba55a4edabda0c165062f3325
COc1ccc(Cc2nccc3cc(OC)c(OC)cc23)cc1OC.O=C(CBr)c1ccccc1>>Br.c1ccc2c(c1)ccn1cccc21
COC=1C=CC(=CC1OC)CC2=C3C=C(C(=CC3=CC=N2)OC)OC.Cl.COC=1C=CC(=CC1OC)CC2=C3C=C(C(=CC3=CC=N2)OC)OC.C(C(=O)C1=CC=CC=C1)Br>>C=1C=CN2C1C1=CC=CC=C1C=C2.COC=1C=CC(=CC1OC)CC2=C3C=C(C(=CC3=CC=N2)OC)OC.Br
COc1ccc(C[c:36]2c3cc(OC)c(OC)c[c:31]3[cH:33][cH:34][n:35]2)cc1OC.O=[C:38]([CH2:37][Br:1])[c:39]1[cH:30][cH:29][cH:28][cH:27][cH:32]1>>[BrH:1].[cH:27]1[cH:28][cH:29][c:30]2[c:31]([cH:32]1)[cH:33][cH:34][n:35]1[cH:36][cH:37][cH:38][c:39]21
COc1ccc(Cc2nccc3cc(OC)c(OC)cc23)cc1OC.O=C(CBr)c1ccccc1
Br.c1ccc2c(c1)ccn1cccc21
null
null
CC(=O)C
Miscellaneous
OtherReaction
5b1557426c466a1800a826fc8905b45ce8b0bd3b7b5a14fabf8103068e10bab9
7619af0a64bd8308938008ca62032f343612f5b288c90b81bdc8a457a3d66263
c1ccc2c(c1)ccn1cccc21
C-O-c1:c:c:c(-C-[c;H0;D3;+0:1]2:[n;H0;D2;+0:2]:[c:3]:[c:4]:[c;H0;D3;+0:5]3:c:c(-O-C):c(-O-C):c:c:3:2):c:c:1-O-C.O=[C;H0;D3;+0:6](-[CH2;D2;+0:7]-[Br;H0;D1;+0:8])-[c;H0;D3;+0:9]1:[cH;D2;+0:10]:[c:11]:[c:12]:[c:13]:[cH;D2;+0:14]:1>>[BrH;D0;+0:8].[c:13]1:[c:12]:[c:11]:[c;H0;D3;+0:10]2:[c;H0;D3;+0:5](:[c:4]:[c:3]:[n;H0;D3;+...
97
[{"value": 97.0, "product": "C=1C=CN2C1C1=CC=CC=C1C=C2", "details": "PERCENTYIELD", "is_desired": false}]
null
null
null
null
A series of novel pyrrolo[2,1-a]isoquinoline dyes was prepared from readily available starting materials via a simple synthetic pathway. One such starting material is papaverine, a naturally occurring alkaloid that is relatively inexpensive and commercially available as its hydrochloride salt. Papaverine hydrochloride ...
10.6084/m9.figshare.5104873.v1
null
Primary halide.Ketone.Ether.Ether.Ether.Ether
null
c1ccccc1.c1ccc2cnccc2c1.c1ccccc1
c1ccc2c(c1)ccn1cccc21
c1ccc2c(c1)ccn1cccc21
HO-
CC(=O)C
null
null
COc1ccc(Cc2nccc3cc(OC)c(OC)cc23)cc1OC.O=C(CBr)c1ccccc1>CC(=O)C>Br.c1ccc2c(c1)ccn1cccc21
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-138236e224a34c72b9402d81270c32cc
CC(=O)OC(C)(C)C.NCCCC[C@H](NC(=O)OCc1ccccc1)C(=O)O>>CC(C)(C)OC(=O)[C@H](CCCCN)NC(=O)OCc1ccccc1
[OH-].[Na+].C(=O)(OCC1=CC=CC=C1)N[C@@H](CCCCN)C(=O)O.C(C)(=O)OC(C)(C)C.Cl(=O)(=O)(=O)O>>C(=O)(OCC1=CC=CC=C1)N[C@@H](CCCCN)C(=O)OC(C)(C)C
CC(=O)O[C:2]([CH3:1])([CH3:3])[CH3:4].[OH:5][C:6](=[O:7])[C@H:8]([CH2:9][CH2:10][CH2:11][CH2:12][NH2:13])[NH:14][C:15](=[O:16])[O:17][CH2:18][c:19]1[cH:20][cH:21][cH:22][cH:23][cH:24]1>>[CH3:1][C:2]([CH3:3])([CH3:4])[O:5][C:6](=[O:7])[C@H:8]([CH2:9][CH2:10][CH2:11][CH2:12][NH2:13])[NH:14][C:15](=[O:16])[O:17][CH2:18][c...
CC(=O)OC(C)(C)C.NCCCC[C@H](NC(=O)OCc1ccccc1)C(=O)O
CC(C)(C)OC(=O)[C@H](CCCCN)NC(=O)OCc1ccccc1
null
null
O.C(C)(=O)OCC
Heteroatom Alkylation and Arylation
OtherReaction
5d0917103c940f1e5ac32fa703bc10c45f3a69de0aac06714163499c8044ed5e
55fd932a5ab5c250a820c8abdb02fe030ad2f5c333e3caf54ef6d66281c0b519
c1ccccc1
C-C(=O)-O-[C;H0;D4;+0:1](-[C;D1;H3:2])(-[C;D1;H3:3])-[C;D1;H3:4].[C:5]-[C:6](=[O;D1;H0:7])-[OH;D1;+0:8]>>[C:5]-[C:6](=[O;D1;H0:7])-[O;H0;D2;+0:8]-[C;H0;D4;+0:1](-[C;D1;H3:2])(-[C;D1;H3:3])-[C;D1;H3:4]
null
[]
null
null
8
HOUR
A mixture of 25 g of Nα-CBZ-L-lysine from Sigma, where CBZ is benzyloxycarbonyl, 250 mL of t-butyl acetate and 14 mL of 70% perchloric acid was vigorously mixed until all solids were dissolved. After stirring overnight, 375 mL of ethyl acetate was added followed by 250 mL of water. The pH of the aqueous layer was raise...
10.6084/m9.figshare.5104873.v1
null
Carboxylic acid.Ester
Ester
null
null
c1ccccc1
HO-
O.C(C)(=O)OCC
null
8
CC(=O)OC(C)(C)C.NCCCC[C@H](NC(=O)OCc1ccccc1)C(=O)O>O.C(C)(=O)OCC>CC(C)(C)OC(=O)[C@H](CCCCN)NC(=O)OCc1ccccc1
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-fcbfd11331bc48daad13c3d9090822ab
C=O.CC(C)(C)OC(=O)[C@H](CCCCN)NC(=O)OCc1ccccc1>>CN(C)NCCCC[C@H](NC(=O)OCc1ccccc1)C(=O)OC(C)(C)C
C=O.C(=O)(OCC1=CC=CC=C1)N[C@@H](CCCCN)C(=O)OC(C)(C)C.[BH3-]C#N.[Na+]>>CN(NCCCC[C@H](NC(=O)OCC1=CC=CC=C1)C(=O)OC(C)(C)C)C
O=[CH2:1].[NH2:4][CH2:5][CH2:6][CH2:7][CH2:8][C@H:9]([NH:10][C:11](=[O:12])[O:13][CH2:14][c:15]1[cH:16][cH:17][cH:18][cH:19][cH:20]1)[C:21](=[O:22])[O:23][C:24]([CH3:25])([CH3:26])[CH3:27]>>[CH3:1][N:2]([CH3:3])[NH:4][CH2:5][CH2:6][CH2:7][CH2:8][C@H:9]([NH:10][C:11](=[O:12])[O:13][CH2:14][c:15]1[cH:16][cH:17][cH:18][cH...
C=O.CC(C)(C)OC(=O)[C@H](CCCCN)NC(=O)OCc1ccccc1
CN(C)NCCCC[C@H](NC(=O)OCc1ccccc1)C(=O)OC(C)(C)C
null
[Cl-].[Cl-].[Zn+2]
CO
Functional Group Interconversion
OtherReaction
027108093d66f25b96db02c2a96d84c4d6959ed84baaa7e0f661b3cbc1d5d2a6
470057d9808f6000905d55406490a6d808be0a7d893d79207ff5fea327996f07
c1ccccc1
O=[CH2;D1;+0:1].[C:2]-[C:3]-[NH2;D1;+0:4]>>[C:2]-[C:3]-[NH;D2;+0:4]-[#7:5](-[C;D1;H3:6])-[CH3;D1;+0:1]
null
[]
null
null
1
HOUR
A mixture consisting of 3.7 (27.2 mmol) of ZnCl2, 3.2 g (53 mmol) of NaCNBH3 and 60 mL of methanol was prepared to which was added a solution of 18 g (51.7 mmol) of the amine 1 in 180 mL of methanol. After cooling to 10°-15° C. 12.4 mL of 37% formaldehyde (165 mmol) was added dropwise over a 2-3 minute period. The reac...
10.6084/m9.figshare.5104873.v1
null
Formaldehyde.Primary amine
Hydrazine
null
null
c1ccccc1
null
[Cl-].[Cl-].[Zn+2].CO
null
1
C=O.CC(C)(C)OC(=O)[C@H](CCCCN)NC(=O)OCc1ccccc1>[Cl-].[Cl-].[Zn+2].CO>CN(C)NCCCC[C@H](NC(=O)OCc1ccccc1)C(=O)OC(C)(C)C
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-2d46e70de5c24d3e972efa60da2d0c9b
CN(C)NCCCC[C@H](NC(=O)OCc1ccccc1)C(=O)OC(C)(C)C.OO>>CN(C)NCCCC[C@@H](C(=O)OC(C)(C)C)[NH+]([O-])C(=O)OCc1ccccc1
CN(NCCCC[C@H](NC(=O)OCC1=CC=CC=C1)C(=O)OC(C)(C)C)C.OO.OO>>CN(NCCCC[C@H]([NH+](C(=O)OCC1=CC=CC=C1)[O-])C(=O)OC(C)(C)C)C
[CH3:1][N:2]([CH3:3])[NH:4][CH2:5][CH2:6][CH2:7][CH2:8][C@@H:9]([C:10](=[O:11])[O:12][C:13]([CH3:14])([CH3:15])[CH3:16])[NH:17][C:19](=[O:20])[O:21][CH2:22][c:23]1[cH:24][cH:25][cH:26][cH:27][cH:28]1.O[OH:18]>>[CH3:1][N:2]([CH3:3])[NH:4][CH2:5][CH2:6][CH2:7][CH2:8][C@@H:9]([C:10](=[O:11])[O:12][C:13]([CH3:14])([CH3:15]...
CN(C)NCCCC[C@H](NC(=O)OCc1ccccc1)C(=O)OC(C)(C)C.OO
CN(C)NCCCC[C@@H](C(=O)OC(C)(C)C)[NH+]([O-])C(=O)OCc1ccccc1
null
null
CO
Functional Group Interconversion
OtherReaction
ffa3c246ed1677fbed02d8b0540bad4c5b5bb5053711032730364292798a0d94
783c90bfee8f176c85f19a00da30e47da456c4a5f1236b20aa29c1dddcde7e75
c1ccccc1
O-[OH;D1;+0:1].[C:2]-[#8:3]-[C:4](=[O;D1;H0:5])-[NH;D2;+0:6]-[C:7](-[C:8])-[C:9](=[O;D1;H0:10])-[#8:11]-[C:12](-[C;D1;H3:13])(-[C;D1;H3:14])-[C;D1;H3:15]>>[C:2]-[#8:3]-[C:4](=[O;D1;H0:5])-[NH+;D3:6](-[O-;H0;D1:1])-[C:7](-[C:8])-[C:9](=[O;D1;H0:10])-[#8:11]-[C:12](-[C;D1;H3:13])(-[C;D1;H3:14])-[C;D1;H3:15]
null
[]
60
CELSIUS
48
HOUR
A solution of 25.3 g of dimethylamine 2, 7.9 mL of 30% hydrogen peroxide and 150 mL of methanol was stirred for 5 h after which an additional 7.9 g of 30% hydrogen peroxide was added. The reaction was allowed to stir for 48 h and monitored by silica gel TLC, eluting with solvent A. A 1 mL aqueous slurry of approximatel...
10.6084/m9.figshare.5104873.v1
null
Carbamic ester.Peroxide
null
null
null
c1ccccc1
HO-
CO
60
48
CN(C)NCCCC[C@H](NC(=O)OCc1ccccc1)C(=O)OC(C)(C)C.OO>CO>CN(C)NCCCC[C@@H](C(=O)OC(C)(C)C)[NH+]([O-])C(=O)OCc1ccccc1
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-1c6890bb15744174b710f1c89858ac54
CCCCOC(=O)C(CCc1c[n+](CCCCC(NC(=O)OCc2ccccc2)C(=O)OC(C)(C)C)cc(O)c1CC(NC(=O)OCc1ccccc1)C(=O)OC(C)(C)C)NC(=O)OCc1ccccc1>>N[C@H](CCCC[n+]1cc(O)c(C[C@H](N)C(=O)O)c(CC[C@H](N)C(=O)O)c1)C(=O)[O-]
OC=1C=[N+](C=C(C1CC(C(=O)OC(C)(C)C)NC(=O)OCC1=CC=CC=C1)CCC(C(=O)OCCCC)NC(=O)OCC1=CC=CC=C1)CCCCC(C(=O)OC(C)(C)C)NC(=O)OCC1=CC=CC=C1.Br>>C1=C(C(=C(C=[N+]1CCCC[C@H](C(=O)[O-])N)O)C[C@@H](C(=O)O)N)CC[C@@H](C(=O)O)N
CCCC[O:25][C:23]([CH:21]([CH2:20][CH2:19][c:18]1[c:11]([CH2:12][CH:13]([NH:14]C(=O)OCc2ccccc2)[C:15](=[O:16])[O:17]C(C)(C)C)[c:9]([OH:10])[cH:8][n+:7]([CH2:6][CH2:5][CH2:4][CH2:3][CH:2]([NH:1]C(=O)OCc2ccccc2)[C:27](=[O:28])[O:29]C(C)(C)C)[cH:26]1)[NH:22]C(=O)OCc1ccccc1)=[O:24]>>[NH2:1][C@H:2]([CH2:3][CH2:4][CH2:5][CH2:...
CCCCOC(=O)C(CCc1c[n+](CCCCC(NC(=O)OCc2ccccc2)C(=O)OC(C)(C)C)cc(O)c1CC(NC(=O)OCc1ccccc1)C(=O)OC(C)(C)C)NC(=O)OCc1ccccc1
N[C@H](CCCC[n+]1cc(O)c(C[C@H](N)C(=O)O)c(CC[C@H](N)C(=O)O)c1)C(=O)[O-]
null
null
null
Miscellaneous
OtherReaction
75990981b45ceb497d1737383df43bfbb9cf97e893baf9d9696871101496658c
b71332cca5f7165c9a25a4c1883c32cfb1bcc76f89d47889d4ed1d741b4da989
c1cc[nH+]cc1
C-C(-C)(-C)-[O;H0;D2;+0:1]-[C:2](=[O;D1;H0:3])-[CH;D3;+0:4](-[C:5]-[C:6])-[NH;D2;+0:7]-C(=O)-O-C-c1:c:c:c:c:c:1.C-C(-C)(-C)-[O;H0;D2;+0:8]-[C:9](=[O;D1;H0:10])-[CH;D3;+0:11](-[C:12]-[c:13])-[NH;D2;+0:14]-C(=O)-O-C-c1:c:c:c:c:c:1.C-C-C-C-[O;H0;D2;+0:15]-[C:16](=[O;D1;H0:17])-[CH;D3;+0:18](-[C:19]-[C:20])-[NH;D2;+0:21]-C...
null
[]
null
null
null
null
reacting the pyridinium salt prepared in step (c) with HBr in an appropriate solvent to provide deoxypyridinoline. Conditions: See reaction.notes.procedure_details.
10.6084/m9.figshare.5104873.v1
null
Carbamic ester.Carbamic ester.Carbamic ester.Ester.Ester.Ester.Ether.Ether.Ether.Boc.Boc
Carboxylic acid.Carboxylic acid.Primary amine.Primary amine.Primary amine
c1ccccc1.c1ccccc1.c1ccccc1
null
C1=CC=[NH+]C=C1
HO-
null
null
null
CCCCOC(=O)C(CCc1c[n+](CCCCC(NC(=O)OCc2ccccc2)C(=O)OC(C)(C)C)cc(O)c1CC(NC(=O)OCc1ccccc1)C(=O)OC(C)(C)C)NC(=O)OCc1ccccc1>>N[C@H](CCCC[n+]1cc(O)c(C[C@H](N)C(=O)O)c(CC[C@H](N)C(=O)O)c1)C(=O)[O-]
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-5cabef20e3d4416cbf3328a8863028c7
CC#N.c1ccc2c(c1)CC1OC21>>N[C@@H]1c2ccccc2C[C@@H]1O
C(C)#N.CS(=O)(=O)O.C12C(CC3=CC=CC=C13)O2.O>>N[C@H]1[C@H](CC2=CC=CC=C12)O
CC#[N:1].[CH:2]12[c:3]3[cH:4][cH:5][cH:6][cH:7][c:8]3[CH2:9][CH:10]1[O:11]2>>[NH2:1][C@@H:2]1[c:3]2[cH:4][cH:5][cH:6][cH:7][c:8]2[CH2:9][C@@H:10]1[OH:11]
CC#N.c1ccc2c(c1)CC1OC21
N[C@@H]1c2ccccc2C[C@@H]1O
null
null
C(Cl)Cl
Heteroatom Alkylation and Arylation
OtherReaction
c326310fbe6c4c9ff3a0833bf4c39adac3f31aec1ac88f4c5a37342c4ef31146
133fdcfd54a50b782beb091526e7c313f29970d3e8558cf65178b1c05b908815
c1ccc2c(c1)CCC2
C-C#[N;H0;D1;+0:1].[c:2]:[c:3]1:[c:4]-[C:5]-[CH;D3;+0:6]2-[O;H0;D2;+0:7]-[CH;D3;+0:8]-2-1>>[NH2;D1;+0:1]-[C@H;D3;+0:8]1-[C@@H;D3;+0:6](-[OH;D1;+0:7])-[C:5]-[c:4]:[c:3]-1:[c:2]
null
[]
-20
CELSIUS
null
null
Indene oxide (117 g) diluted to a total volume of 600 mL in methylene chloride was diluted with acetonitrile (600 mL) and cooled to -20° C. Methanesulfonic acid (114 mL) was then added. The mixture was warmed to 25° C. and aged for 2 h. Water (600 mL) was added and the mixture heated at 45° C. for 5 h. The organic phas...
10.6084/m9.figshare.5104873.v1
null
Ether.Nitrile
Secondary alcohol.Primary amine
c1ccc2c(c1)CC1OC21
c1ccc2c(c1)CCC2
c1ccc2c(c1)CCC2
Other
C(Cl)Cl
-20
null
CC#N.c1ccc2c(c1)CC1OC21>C(Cl)Cl>N[C@@H]1c2ccccc2C[C@@H]1O
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-0d0c32a5746a47be8dab7284d54a01f0
CC#N.O[C@@H]1Cc2ccccc2[C@H]1O>>N[C@@H]1c2ccccc2C[C@@H]1O
[OH-].[Na+].S(O)(O)(=O)=O.[C@@H]1([C@@H](CC2=CC=CC=C12)O)O.C(C)#N.C(C)#N.O>>N[C@H]1[C@H](CC2=CC=CC=C12)O
CC#[N:1].O[C@@H:2]1[c:3]2[cH:4][cH:5][cH:6][cH:7][c:8]2[CH2:9][C@H:10]1[OH:11]>>[NH2:1][C@@H:2]1[c:3]2[cH:4][cH:5][cH:6][cH:7][c:8]2[CH2:9][C@@H:10]1[OH:11]
CC#N.O[C@@H]1Cc2ccccc2[C@H]1O
N[C@@H]1c2ccccc2C[C@@H]1O
null
null
null
Heteroatom Alkylation and Arylation
OtherReaction
d881d6d5d211f65d417c36b0d4968906c9ad252517a54e2b64bea808b0ba8aac
67fd49cf09a1a174c541805acde8e33a68a7d1aea9b7b149523a970b84a1b277
c1ccc2c(c1)CCC2
C-C#[N;H0;D1;+0:1].O-[C@H;D3;+0:2]1-[C:3](-[O;D1;H1:4])-[C:5]-[c:6]:[c:7]-1:[c:8]>>[NH2;D1;+0:1]-[C@H;D3;+0:2]1-[C:3](-[O;D1;H1:4])-[C:5]-[c:6]:[c:7]-1:[c:8]
63
[{"value": 63.0, "product": "N[C@H]1[C@H](CC2=CC=CC=C12)O", "details": "PERCENTYIELD", "is_desired": false}]
0
CELSIUS
null
null
Trans-1,2-indandiol (1.5 g) was dissolved in acetonitrile (25 mL) cooled to 0° C., and concentrated sulfuric acid (1.1 mL) was added. The mixture was gradually warmed to 20° C. and aged to 3 hours. Water (2 mL) was added and the mixture heated to reflux. Concentrated aqueous sodium hydroxide was added to adjust the pH ...
10.6084/m9.figshare.5104873.v1
null
Nitrile.Secondary alcohol
Primary amine
c1ccc2c(c1)CCC2
c1ccc2c(c1)CCC2
c1ccc2c(c1)CCC2
HO-
null
0
null
CC#N.O[C@@H]1Cc2ccccc2[C@H]1O>>N[C@@H]1c2ccccc2C[C@@H]1O
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-bb4572950e154c0d8d7ae87ec0fb230d
CC#N.O[C@@H]1c2ccccc2C[C@@H]1O>>N[C@@H]1c2ccccc2C[C@@H]1O
[C@@H]1([C@H](CC2=CC=CC=C12)O)O.C(C)#N.S(O)(O)(=O)=O.O>>N[C@H]1[C@H](CC2=CC=CC=C12)O
CC#[N:1].O[C@@H:2]1[c:3]2[cH:4][cH:5][cH:6][cH:7][c:8]2[CH2:9][C@@H:10]1[OH:11]>>[NH2:1][C@@H:2]1[c:3]2[cH:4][cH:5][cH:6][cH:7][c:8]2[CH2:9][C@@H:10]1[OH:11]
CC#N.O[C@@H]1c2ccccc2C[C@@H]1O
N[C@@H]1c2ccccc2C[C@@H]1O
null
null
null
Heteroatom Alkylation and Arylation
OtherReaction
d881d6d5d211f65d417c36b0d4968906c9ad252517a54e2b64bea808b0ba8aac
67fd49cf09a1a174c541805acde8e33a68a7d1aea9b7b149523a970b84a1b277
c1ccc2c(c1)CCC2
C-C#[N;H0;D1;+0:1].O-[C@H;D3;+0:2]1-[C:3](-[O;D1;H1:4])-[C:5]-[c:6]:[c:7]-1:[c:8]>>[NH2;D1;+0:1]-[C@H;D3;+0:2]1-[C:3](-[O;D1;H1:4])-[C:5]-[c:6]:[c:7]-1:[c:8]
null
[]
-40
CELSIUS
1
HOUR
Cis-1,2-indandiol (1.0 g) was dissolved in acetonitrile (20 mL), cooled to -40° C., and fuming sulfuric acid (21% SO3, 0.8 mL) was added. The mixture was aged for 1 hour with gradual warming to 0° C. Water was added and the mixture heated to 80° C. for 1 hour to provide an aqueous solution of cis-1-amino-2-indanol. Con...
10.6084/m9.figshare.5104873.v1
null
Nitrile.Secondary alcohol
Primary amine
c1ccc2c(c1)CCC2
c1ccc2c(c1)CCC2
c1ccc2c(c1)CCC2
HO-
null
-40
1
CC#N.O[C@@H]1c2ccccc2C[C@@H]1O>>N[C@@H]1c2ccccc2C[C@@H]1O
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-f5c19c1716b641f7a3721e4238a2fc65
CCCC1CCC(c2ccc([Si](OC)(OC)OC)cc2)CC1.Fc1ccc(Br)cc1F>>CCCC1CCC(c2ccc(-c3ccc(F)c(F)c3)cc2)CC1
FC=1C=C(C=CC1F)Br.O.C(CC)C1CCC(CC1)C1=CC=C(C=C1)[Si](OC)(OC)OC.CCCC[N+](CCCC)(CCCC)CCCC.[F-]>>C(CC)C1CCC(CC1)C1=CC=C(C=C1)C1=CC(=C(C=C1)F)F
CO[Si](OC)(OC)[c:11]1[cH:10][cH:9][c:8]([CH:7]2[CH2:6][CH2:5][CH:4]([CH2:3][CH2:2][CH3:1])[CH2:23][CH2:22]2)[cH:21][cH:20]1.Br[c:12]1[cH:13][cH:14][c:15]([F:16])[c:17]([F:18])[cH:19]1>>[CH3:1][CH2:2][CH2:3][CH:4]1[CH2:5][CH2:6][CH:7]([c:8]2[cH:9][cH:10][c:11](-[c:12]3[cH:13][cH:14][c:15]([F:16])[c:17]([F:18])[cH:19]3)[...
CCCC1CCC(c2ccc([Si](OC)(OC)OC)cc2)CC1.Fc1ccc(Br)cc1F
CCCC1CCC(c2ccc(-c3ccc(F)c(F)c3)cc2)CC1
null
C=1C=CC(=CC1)[P](C=2C=CC=CC2)(C=3C=CC=CC3)[Pd]([P](C=4C=CC=CC4)(C=5C=CC=CC5)C=6C=CC=CC6)([P](C=7C=CC=CC7)(C=8C=CC=CC8)C=9C=CC=CC9)[P](C=1C=CC=CC1)(C=1C=CC=CC1)C=1C=CC=CC1
C1(=CC=CC=C1)C
C-C Coupling
OtherReaction
6c7e46f037db2db13a9d5119176e5c1599bfbcc866048f620c21387f17020f61
2856e130876f022e74efbbf6704a31362bbcc6a09b5f3423754264b3ad894840
c1ccc(-c2ccc(C3CCCCC3)cc2)cc1
Br-[c;H0;D3;+0:1](:[c:2]:[c:3]):[c:4]:[c:5].C-O-[Si](-O-C)(-O-C)-[c;H0;D3;+0:6](:[c:7]:[c:8]):[c:9]:[c:10]>>[c:3]:[c:2]:[c;H0;D3;+0:1](-[c;H0;D3;+0:6](:[c:7]:[c:8]):[c:9]:[c:10]):[c:4]:[c:5]
94.5
[{"value": 40.0, "product": "C(CC)C1CCC(CC1)C1=CC=C(C=C1)C1=CC(=C(C=C1)F)F", "details": "PERCENTYIELD", "is_desired": false}, {"value": 94.5, "product": "C(CC)C1CCC(CC1)C1=CC=C(C=C1)C1=CC(=C(C=C1)F)F", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
30
MINUTE
To 0.645 g (2 mmol) of 4-(4-propylcyclohexyl)-phenyltrimethoxysilane (Ih) was added 2.1 ml of TBAF (2.1 mmol, 1M in THF) under nitrogen, and the mixture was stirred at room temperature for 30 minutes. After the solvent was removed under reduced pressure, a solution of 3,4-difluorobromobenzene (0.463 g, 2.4 mmol) in tol...
10.6084/m9.figshare.5104873.v1
null
Aromatic halide.Silyl protective group
null
c1ccccc1.c1ccccc1
c1ccccc1.c1ccccc1
C1CCCCC1.c1ccccc1.c1ccccc1
HBr
C=1C=CC(=CC1)[P](C=2C=CC=CC2)(C=3C=CC=CC3)[Pd]([P](C=4C=CC=CC4)(C=5C=CC=CC5)C=6C=CC=CC6)([P](C=7C=CC=CC7)(C=8C=CC=CC8)C=9C=CC=CC9)[P](C=1C=CC=CC1)(C=1C=CC=CC1)C=1C=CC=CC1.C1(=CC=CC=C1)C
null
0.5
CCCC1CCC(c2ccc([Si](OC)(OC)OC)cc2)CC1.Fc1ccc(Br)cc1F>C=1C=CC(=CC1)[P](C=2C=CC=CC2)(C=3C=CC=CC3)[Pd]([P](C=4C=CC=CC4)(C=5C=CC=CC5)C=6C=CC=CC6)([P](C=7C=CC=CC7)(C=8C=CC=CC8)C=9C=CC=CC9)[P](C=1C=CC=CC1)(C=1C=CC=CC1)C=1C=CC=CC1.C1(=CC=CC=C1)C>CCCC1CCC(c2ccc(-c3ccc(F)c(F)c3)cc2)CC1
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-605c87dbb48f48b79511bcb4086ebb7c
FC(F)=C(F)C(F)(F)F.O=S(=O)=O>>O=S1(=O)OC(F)(F)C1(F)C(F)(F)F
OS(=O)(=O)O.O=S(=O)=O.FC(C(=C(F)F)F)(F)F>>C1(C(OS1(=O)=O)(F)F)(C(F)(F)F)F
[C:5]([F:6])([F:7])=[C:8]([F:9])[C:10]([F:11])([F:12])[F:13].[O:1]=[S:2](=[O:3])=[O:4]>>[O:1]=[S:2]1(=[O:3])[O:4][C:5]([F:6])([F:7])[C:8]1([F:9])[C:10]([F:11])([F:12])[F:13]
FC(F)=C(F)C(F)(F)F.O=S(=O)=O
O=S1(=O)OC(F)(F)C1(F)C(F)(F)F
null
null
null
Heteroatom Alkylation and Arylation
OtherReaction
fc11a660dfe158b2f097d9ced0e7160496bf1a7a654f488480d20094b26f97c9
d984d1e98d50ababc2f79015fe04137f1ee62396665577d69700bd725f0b5290
O=S1(=O)CCO1
[F;D1;H0:1]-[C:2](-[F;D1;H0:3])(-[F;D1;H0:4])-[C;H0;D3;+0:5](-[F;D1;H0:6])=[C;H0;D3;+0:7](-[F;D1;H0:8])-[F;D1;H0:9].[O;D1;H0:10]=[S;H0;D3;+0:11](=[O;D1;H0:12])=[O;H0;D1;+0:13]>>[F;D1;H0:1]-[C:2](-[F;D1;H0:3])(-[F;D1;H0:4])-[C;H0;D4;+0:5]1(-[F;D1;H0:6])-[C;H0;D4;+0:7](-[F;D1;H0:8])(-[F;D1;H0:9])-[O;H0;D2;+0:13]-[S;H0;D4...
66
[{"value": 66.0, "product": "C1(C(OS1(=O)=O)(F)F)(C(F)(F)F)F", "details": "PERCENTYIELD", "is_desired": false}]
-45
CELSIUS
9
MINUTE
A 100 mL Parr™ reactor was charged with 63.8 g of 65% oleum (0.52 mole SO3), cooled to -45° C., evacuated, and then charged with 62 grams (0.44 mole) liquid hexafluoropropene from a cold trap (-78° C.). The reaction mixture was allowed to warm to room temperature. At 20° C. a slight exotherm was observed which increase...
10.6084/m9.figshare.5104873.v1
null
Alkenyl halide.Alkenyl halide.Alkenyl halide
Tertiary halide.Tertiary halide.Tertiary halide.Sulfonate
null
C1CSO1
C1CSO1
null
null
-45
0.15
FC(F)=C(F)C(F)(F)F.O=S(=O)=O>>O=S1(=O)OC(F)(F)C1(F)C(F)(F)F
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-88d4144d85e8491ea90668f6b8fef2a3
FC(F)=C(F)C(F)(F)F.O=S(=O)=O>>O=S1(=O)OC(F)(F)C1(F)C(F)(F)F
OS(=O)(=O)O.O=S(=O)=O.FC(C(=C(F)F)F)(F)F.FC(C(=C(F)F)F)(F)F>>C1(C(OS1(=O)=O)(F)F)(C(F)(F)F)F
[C:5]([F:6])([F:7])=[C:8]([F:9])[C:10]([F:11])([F:12])[F:13].[O:1]=[S:2](=[O:3])=[O:4]>>[O:1]=[S:2]1(=[O:3])[O:4][C:5]([F:6])([F:7])[C:8]1([F:9])[C:10]([F:11])([F:12])[F:13]
FC(F)=C(F)C(F)(F)F.O=S(=O)=O
O=S1(=O)OC(F)(F)C1(F)C(F)(F)F
null
null
null
Heteroatom Alkylation and Arylation
OtherReaction
fc11a660dfe158b2f097d9ced0e7160496bf1a7a654f488480d20094b26f97c9
d984d1e98d50ababc2f79015fe04137f1ee62396665577d69700bd725f0b5290
O=S1(=O)CCO1
[F;D1;H0:1]-[C:2](-[F;D1;H0:3])(-[F;D1;H0:4])-[C;H0;D3;+0:5](-[F;D1;H0:6])=[C;H0;D3;+0:7](-[F;D1;H0:8])-[F;D1;H0:9].[O;D1;H0:10]=[S;H0;D3;+0:11](=[O;D1;H0:12])=[O;H0;D1;+0:13]>>[F;D1;H0:1]-[C:2](-[F;D1;H0:3])(-[F;D1;H0:4])-[C;H0;D4;+0:5]1(-[F;D1;H0:6])-[C;H0;D4;+0:7](-[F;D1;H0:8])(-[F;D1;H0:9])-[O;H0;D2;+0:13]-[S;H0;D4...
62
[{"value": 62.0, "product": "C1(C(OS1(=O)=O)(F)F)(C(F)(F)F)F", "details": "PERCENTYIELD", "is_desired": false}, {"value": 61.8, "product": "C1(C(OS1(=O)=O)(F)F)(C(F)(F)F)F", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
43
CELSIUS
null
null
Using essentially the procedure of Example 1, the reactor was charged with 33.8 g of 67 wt. % oleum (0.28 mole SO3) and 58.0 g hexafluoropropene. After the initial exotherm (max. pressure 896 kPa at 39° C.) the mixture was heated for 13 hours at 43° C. The reactor was vented of excess hexafluoropropene (16.0 g recovere...
10.6084/m9.figshare.5104873.v1
null
Alkenyl halide.Alkenyl halide.Alkenyl halide
Tertiary halide.Tertiary halide.Tertiary halide.Sulfonate
null
C1CSO1
C1CSO1
null
null
43
null
FC(F)=C(F)C(F)(F)F.O=S(=O)=O>>O=S1(=O)OC(F)(F)C1(F)C(F)(F)F
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-42930046cadb48d6957e758ac989945a
FC(F)=C(F)C(F)(F)F.O=S(=O)=O>>O=S1(=O)OC(F)(F)C1(F)C(F)(F)F
FC(C(=C(F)F)F)(F)F.OS(=O)(=O)O.O=S(=O)=O>>C1(C(OS1(=O)=O)(F)F)(C(F)(F)F)F
[C:5]([F:6])([F:7])=[C:8]([F:9])[C:10]([F:11])([F:12])[F:13].[O:1]=[S:2](=[O:3])=[O:4]>>[O:1]=[S:2]1(=[O:3])[O:4][C:5]([F:6])([F:7])[C:8]1([F:9])[C:10]([F:11])([F:12])[F:13]
FC(F)=C(F)C(F)(F)F.O=S(=O)=O
O=S1(=O)OC(F)(F)C1(F)C(F)(F)F
null
null
null
Heteroatom Alkylation and Arylation
OtherReaction
fc11a660dfe158b2f097d9ced0e7160496bf1a7a654f488480d20094b26f97c9
d984d1e98d50ababc2f79015fe04137f1ee62396665577d69700bd725f0b5290
O=S1(=O)CCO1
[F;D1;H0:1]-[C:2](-[F;D1;H0:3])(-[F;D1;H0:4])-[C;H0;D3;+0:5](-[F;D1;H0:6])=[C;H0;D3;+0:7](-[F;D1;H0:8])-[F;D1;H0:9].[O;D1;H0:10]=[S;H0;D3;+0:11](=[O;D1;H0:12])=[O;H0;D1;+0:13]>>[F;D1;H0:1]-[C:2](-[F;D1;H0:3])(-[F;D1;H0:4])-[C;H0;D4;+0:5]1(-[F;D1;H0:6])-[C;H0;D4;+0:7](-[F;D1;H0:8])(-[F;D1;H0:9])-[O;H0;D2;+0:13]-[S;H0;D4...
65
[{"value": 65.0, "product": "C1(C(OS1(=O)=O)(F)F)(C(F)(F)F)F", "details": "PERCENTYIELD", "is_desired": false}]
50
CELSIUS
null
null
Using essentially the procedure of Example 1, the reactor was charged with 44.7 g hexafluoropropene, 45.9 g of 67 wt. % oleum and 41.5 g Fluorinert FC-77™. The reaction mixture was heated at 50° C. for 6 hours. The reactor was vented of excess HFP and the sultone layer (95.0 g) was separated and distilled to provide th...
10.6084/m9.figshare.5104873.v1
null
Alkenyl halide.Alkenyl halide.Alkenyl halide
Tertiary halide.Tertiary halide.Tertiary halide.Sulfonate
null
C1CSO1
C1CSO1
null
null
50
null
FC(F)=C(F)C(F)(F)F.O=S(=O)=O>>O=S1(=O)OC(F)(F)C1(F)C(F)(F)F
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-66f1b1423ff84fd0aecb09103bf3af98
CCCC(=O)CC(=O)OCC.Oc1cc(O)cc(O)c1>>CCCc1cc(=O)oc2cc(O)cc(O)c12
C1(O)=CC(O)=CC(O)=C1.C(CCC)(=O)CC(=O)OCC.FC(S(=O)(=O)O)(F)F>>OC1=C2C(=CC(OC2=CC(=C1)O)=O)CCC
CCO[C:6]([CH2:5][C:4](=O)[CH2:3][CH2:2][CH3:1])=[O:7].[OH:8][c:9]1[cH:10][c:11]([OH:12])[cH:13][c:14]([OH:15])[cH:16]1>>[CH3:1][CH2:2][CH2:3][c:4]1[cH:5][c:6](=[O:7])[o:8][c:9]2[cH:10][c:11]([OH:12])[cH:13][c:14]([OH:15])[c:16]12
CCCC(=O)CC(=O)OCC.Oc1cc(O)cc(O)c1
CCCc1cc(=O)oc2cc(O)cc(O)c12
null
null
O
Aromatic Heterocycle Formation
OtherReaction
73bb7365a8a6e9bc003da4fff3edbd064895960a48b91098cfd38bf6af202cd2
89a9e45776dbe9070f40025f4f55f2a7b9907ff5b9cebad1727718d85938e303
O=c1ccc2ccccc2o1
C-C-O-[C;H0;D3;+0:1](=[O;D1;H0:2])-[CH2;D2;+0:3]-[C;H0;D3;+0:4](=O)-[C:5]-[C:6].[O;D1;H1:7]-[c:8](:[c:9]):[cH;D2;+0:10]:[c:11](-[OH;D1;+0:12]):[c:13]>>[C:6]-[C:5]-[c;H0;D3;+0:4]1:[cH;D2;+0:3]:[c;H0;D3;+0:1](=[O;D1;H0:2]):[o;H0;D2;+0:12]:[c:11](:[c:13]):[c;H0;D3;+0:10]:1:[c:8](-[O;D1;H1:7]):[c:9]
99.1
[{"value": 99.0, "product": "OC1=C2C(=CC(OC2=CC(=C1)O)=O)CCC", "details": "PERCENTYIELD", "is_desired": false}, {"value": 99.1, "product": "OC1=C2C(=CC(OC2=CC(=C1)O)=O)CCC", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
null
null
A suspension of anhydrous phloroglucinol (20.0 g, 0.159 mol) in ethyl butrylacetate (26.3 g; 0.167 mol) was added over 30 min to 50 g of constantly stirred trifluoromethanesulfonic acid cooled in an ice bath. A drying tube was then fined to the reaction vessel and the mixture was stirred for 16h at 25° C., after which ...
10.6084/m9.figshare.5104873.v1
null
Ketone.Ester.Aromatic alcohol
null
c1ccccc1
c1ccc2cccoc2c1
c1ccc2cccoc2c1
HO-
O
null
null
CCCC(=O)CC(=O)OCC.Oc1cc(O)cc(O)c1>O>CCCc1cc(=O)oc2cc(O)cc(O)c12
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-6edcc2e8e3744c608ae582a2c614eb39
CCOC(=O)CN1Cc2ccccc2C[C@H](N2C(=O)c3ccccc3C2=O)C1=O.O=C(Cl)OCc1ccccc1>>CCOC(=O)CN1Cc2ccccc2C[C@H](NC(=O)OCc2ccccc2)C1=O
C(C)N(CC)CC.C(C1=CC=CC=C1)OC(=O)Cl.C1(C=2C(C(N1[C@@H]1C(N(CC3=C(C1)C=CC=C3)CC(=O)OCC)=O)=O)=CC=CC2)=O.C(C)O>>C1(=CC=CC=C1)COC(=O)N[C@@H]1C(N(CC2=C(C1)C=CC=C2)CC(=O)OCC)=O
O=C1c2ccccc2C(=O)[N:17]1[C@H:16]1[CH2:15][c:14]2[c:9]([cH:10][cH:11][cH:12][cH:13]2)[CH2:8][N:7]([CH2:6][C:4]([O:3][CH2:2][CH3:1])=[O:5])[C:28]1=[O:29].Cl[C:18](=[O:19])[O:20][CH2:21][c:22]1[cH:23][cH:24][cH:25][cH:26][cH:27]1>>[CH3:1][CH2:2][O:3][C:4](=[O:5])[CH2:6][N:7]1[CH2:8][c:9]2[cH:10][cH:11][cH:12][cH:13][c:14]...
CCOC(=O)CN1Cc2ccccc2C[C@H](N2C(=O)c3ccccc3C2=O)C1=O.O=C(Cl)OCc1ccccc1
CCOC(=O)CN1Cc2ccccc2C[C@H](NC(=O)OCc2ccccc2)C1=O
null
null
C1(=CC=CC=C1)C.C(C)(=O)OCC.O.NN
Protection
OtherReaction
fe3102b6b408f3d3825eb2b8e397463241cc48fe0961b1edbc9ae90e981158d6
1040b538a38b728279e7919c87da3a9c1d00e9f692e311a76ca8b5e574dd287d
O=C(N[C@H]1Cc2ccccc2CNC1=O)OCc1ccccc1
Cl-[C;H0;D3;+0:1](=[O;D1;H0:2])-[#8:3]-[C:4].O=C1-[N;H0;D3;+0:5](-[C:6](-[C:7])-[C:8](=[O;D1;H0:9])-[#7:10](-[C:11]-[C:12](-[#8:13])=[O;D1;H0:14])-[C:15])-C(=O)-c2:c:c:c:c:c:2-1>>[#8:13]-[C:12](=[O;D1;H0:14])-[C:11]-[#7:10](-[C:15])-[C:8](=[O;D1;H0:9])-[C:6](-[NH;D2;+0:5]-[C;H0;D3;+0:1](=[O;D1;H0:2])-[#8:3]-[C:4])-[C:7...
null
[]
0
CELSIUS
2
HOUR
A solution of (S)-1,3,4,5-tetrahydro-4-phthalimido-3-oxo-2H-2-benzazepine-2-acetic acid, ethyl ester (1.67 g., 4.26 mmol.) in 1.0M hydrazine hydrate in ethanol (9.0 ml., 9.0 mmol.) was stirred at room temperature under argon for 36 hours. The mixture was diluted with an equal volume of ethyl acetate, filtered and filtr...
10.6084/m9.figshare.5104873.v1
null
Acyl halide.Ether.Substituted dicarboximide
Carbamic ester
c1ccc2c(c1)C[NH]C2
null
c1ccc2c(c1)CCC[NH]C2.c1ccccc1
HCl
C1(=CC=CC=C1)C.C(C)(=O)OCC.O.NN
0
2
CCOC(=O)CN1Cc2ccccc2C[C@H](N2C(=O)c3ccccc3C2=O)C1=O.O=C(Cl)OCc1ccccc1>C1(=CC=CC=C1)C.C(C)(=O)OCC.O.NN>CCOC(=O)CN1Cc2ccccc2C[C@H](NC(=O)OCc2ccccc2)C1=O
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-c2956910e6964c68a222931d19fd2abc
CC(C)(C)OC(=O)N[C@@H](CO)C(=O)O.O=[N+]([O-])c1ccccc1F>>CC(C)(C)OC(=O)N[C@@H](COc1ccccc1[N+](=O)[O-])C(=O)O
[H-].[Na+].FC1=C(C=CC=C1)[N+](=O)[O-].C(Cl)Cl.CC(C)(OC(=O)N[C@@H](CO)C(=O)O)C>>CC(C)(OC(=O)N[C@@H](COC1=C(C=CC=C1)[N+](=O)[O-])C(=O)O)C
[CH3:1][C:2]([CH3:3])([CH3:4])[O:5][C:6](=[O:7])[NH:8][C@@H:9]([CH2:10][OH:11])[C:21](=[O:22])[OH:23].F[c:12]1[cH:13][cH:14][cH:15][cH:16][c:17]1[N+:18](=[O:19])[O-:20]>>[CH3:1][C:2]([CH3:3])([CH3:4])[O:5][C:6](=[O:7])[NH:8][C@@H:9]([CH2:10][O:11][c:12]1[cH:13][cH:14][cH:15][cH:16][c:17]1[N+:18](=[O:19])[O-:20])[C:21](...
CC(C)(C)OC(=O)N[C@@H](CO)C(=O)O.O=[N+]([O-])c1ccccc1F
CC(C)(C)OC(=O)N[C@@H](COc1ccccc1[N+](=O)[O-])C(=O)O
null
null
CN(C=O)C.CO.C(C)(=O)O
Heteroatom Alkylation and Arylation
Williamson Ether Synthesis
4821d6d7238522ee9ef4538c00647e855becf4de3d9c939c0cec2b01c1e5e915
a4cafa7bcd156e21cca6eaac1b32e28ec8540642a31181122e6957f3d7559631
c1ccccc1
F-[c;H0;D3;+0:1](:[c:2]:[c:3]):[c:4](-[#7;+:5]):[c:6].[O;D1;H0:7]=[C:8](-[O;D1;H1:9])-[C:10]-[C:11]-[OH;D1;+0:12]>>[#7;+:5]-[c:4](:[c:6]):[c;H0;D3;+0:1](-[O;H0;D2;+0:12]-[C:11]-[C:10]-[C:8](=[O;D1;H0:7])-[O;D1;H1:9]):[c:2]:[c:3]
null
[]
null
null
null
null
A solution of N-[(1,1-dimethylethoxy)carbonyl]-L-serine (24.3 g., 0.118 mole) in dry dimethylformamide (25 ml.) was added dropwise over a period of 1.0 hour to a cooled (0°, ice-salt bath) suspension of 60% sodium hydride (10.1 g., 0.25 mole) in dry dimethylformamide (200 ml.) and stirring was continued at 0° until the...
10.6084/m9.figshare.5104873.v1
null
Aromatic halide.Primary alcohol
Ether
c1ccccc1
c1ccccc1
c1ccccc1
HF
CN(C=O)C.CO.C(C)(=O)O
null
null
CC(C)(C)OC(=O)N[C@@H](CO)C(=O)O.O=[N+]([O-])c1ccccc1F>CN(C=O)C.CO.C(C)(=O)O>CC(C)(C)OC(=O)N[C@@H](COc1ccccc1[N+](=O)[O-])C(=O)O
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-34f0afde778d417c9ab448469c03bc23
CCOC(=O)CBr.O=C(N[C@H]1CSC[C@@H](c2ccccc2)NC1=O)OCc1ccccc1>>CCOC(=O)CN1C(=O)[C@@H](NC(=O)OCc2ccccc2)CSC[C@H]1c1ccccc1
[OH-].[K+].BrCC(=O)OCC.BrCC(=O)OCC.C1(=CC=CC=C1)[C@@H]1CSC[C@@H](C(N1)=O)NC(=O)OCC1=CC=CC=C1>>O=C1N([C@@H](CSC[C@@H]1NC(=O)OCC1=CC=CC=C1)C1=CC=CC=C1)CC(=O)OCC
Br[CH2:6][C:4]([O:3][CH2:2][CH3:1])=[O:5].[NH:7]1[C:8](=[O:9])[C@@H:10]([NH:11][C:12](=[O:13])[O:14][CH2:15][c:16]2[cH:17][cH:18][cH:19][cH:20][cH:21]2)[CH2:22][S:23][CH2:24][C@H:25]1[c:26]1[cH:27][cH:28][cH:29][cH:30][cH:31]1>>[CH3:1][CH2:2][O:3][C:4](=[O:5])[CH2:6][N:7]1[C:8](=[O:9])[C@@H:10]([NH:11][C:12](=[O:13])[O...
CCOC(=O)CBr.O=C(N[C@H]1CSC[C@@H](c2ccccc2)NC1=O)OCc1ccccc1
CCOC(=O)CN1C(=O)[C@@H](NC(=O)OCc2ccccc2)CSC[C@H]1c1ccccc1
null
[Br-].C(CCC)[N+](CCCC)(CCCC)CCCC
C(C)(=O)OCC.O1CCCC1.S(=O)(=O)([O-])[O-].[Mg+2]
Heteroatom Alkylation and Arylation
N-alkylation of secondary amines with alkyl halides
448d2a9bdfd31665de19d5d708bf0615b1c0dce8080afe65ff0e19354a21937a
933a6f1013d44497c9c5902b73c24fbdc7813d20b886bdbc4c670d5b43ca2182
O=C(N[C@H]1CSC[C@@H](c2ccccc2)NC1=O)OCc1ccccc1
Br-[CH2;D2;+0:1]-[C:2](=[O;D1;H0:3])-[#8:4]-[C:5].[#16:6]-[C:7]-[C:8](-[c:9])-[NH;D2;+0:10]-[C:11](=[O;D1;H0:12])-[C:13]>>[#16:6]-[C:7]-[C:8](-[c:9])-[N;H0;D3;+0:10](-[CH2;D2;+0:1]-[C:2](=[O;D1;H0:3])-[#8:4]-[C:5])-[C:11](=[O;D1;H0:12])-[C:13]
null
[]
null
null
null
null
A solution of (3R-cis)-tetrahydro-3-phenyl-6-[[(phenylmethoxy)carbonyl]amino]-1,4-thiazepin-5(4H)-one (1.16 g., 3.25 mmol) [prepared as described by Yanagisawa et al., J. Med. Chem., Vol. 30, p. 1984-1991 (1987)] in distilled tetrahydrofuran (30 ml.), under an atmosphere of argon, was cooled to 0° C. and treated with p...
10.6084/m9.figshare.5104873.v1
null
Primary halide.Ester.Secondary amide
Ester.Tertiary amide
C1CNCCSC1
C1C[NH]CCSC1
C1C[NH]CCSC1.c1ccccc1.c1ccccc1
HBr
[Br-].C(CCC)[N+](CCCC)(CCCC)CCCC.C(C)(=O)OCC.O1CCCC1.S(=O)(=O)([O-])[O-].[Mg+2]
null
null
CCOC(=O)CBr.O=C(N[C@H]1CSC[C@@H](c2ccccc2)NC1=O)OCc1ccccc1>[Br-].C(CCC)[N+](CCCC)(CCCC)CCCC.C(C)(=O)OCC.O1CCCC1.S(=O)(=O)([O-])[O-].[Mg+2]>CCOC(=O)CN1C(=O)[C@@H](NC(=O)OCc2ccccc2)CSC[C@H]1c1ccccc1
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-89c19946194d4a158a9cbb1375586293
N[C@@H](Cc1ccccc1)C(=O)O.[Br-]>>O=C(O)[C@@H](Br)Cc1ccccc1
N(=O)[O-].[Na+].C1(=CC=CC=C1)C.N[C@@H](CC1=CC=CC=C1)C(=O)O.[Br-].[K+]>>Br[C@H](C(=O)O)CC1=CC=CC=C1
N[C@H:4]([C:2](=[O:1])[OH:3])[CH2:6][c:7]1[cH:8][cH:9][cH:10][cH:11][cH:12]1.[Br-:5]>>[O:1]=[C:2]([OH:3])[C@@H:4]([Br:5])[CH2:6][c:7]1[cH:8][cH:9][cH:10][cH:11][cH:12]1
N[C@@H](Cc1ccccc1)C(=O)O.[Br-]
O=C(O)[C@@H](Br)Cc1ccccc1
null
null
C(C)(=O)O.S(O)(O)(=O)=O
Functional Group Interconversion
OtherReaction
117344ae409beae3589a30d5997369184f62edb887830bd6b795e8dfdf82920d
9544d3c5449a12cdcbad58c02e82937c94837ec7c67e3baf5ab21c8ae3b17e42
c1ccccc1
N-[C@@H;D3;+0:1](-[C:2]-[c:3])-[C:4](=[O;D1;H0:5])-[O;D1;H1:6].[Br-;H0;D0:7]>>[Br;H0;D1;+0:7]-[C@@H;D3;+0:1](-[C:2]-[c:3])-[C:4](=[O;D1;H0:5])-[O;D1;H1:6]
null
[]
null
null
1
HOUR
A solution of L-phenylalanine (30.0 g., 0.175 mole) and potassium bromide (73.5 g., 0.618 mole) in 2.5N sulfuric acid (365 ml.) was cooled down to 0° (ice-salt bath) and treated portionwise with sodium nitrite (19.3 g., 0.28 mole) over a period of 1.0 hour. Stirring was continued for 1.0 hour at 0° and at room temperat...
10.6084/m9.figshare.5104873.v1
null
Primary amine
Secondary halide
null
null
c1ccccc1
Other
C(C)(=O)O.S(O)(O)(=O)=O
null
1
N[C@@H](Cc1ccccc1)C(=O)O.[Br-]>C(C)(=O)O.S(O)(O)(=O)=O>O=C(O)[C@@H](Br)Cc1ccccc1
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-d26e1da8640f4b3bb9f977d4faa64c80
C[C@@H](O)[C@H](NC(=O)OC(C)(C)C)C(=O)O.O=[N+]([O-])c1ccccc1F>>C[C@@H](Oc1ccccc1[N+](=O)[O-])[C@H](NC(=O)OC(C)(C)C)C(=O)O
CC(C)(OC(=O)N[C@@H]([C@H](O)C)C(=O)O)C.[H-].[Na+].FC1=C(C=CC=C1)[N+](=O)[O-]>>CC(C)(OC(=O)N[C@@H]([C@H](OC1=C(C=CC=C1)[N+](=O)[O-])C)C(=O)O)C
[CH3:1][C@@H:2]([OH:3])[C@H:13]([NH:14][C:15](=[O:16])[O:17][C:18]([CH3:19])([CH3:20])[CH3:21])[C:22](=[O:23])[OH:24].F[c:4]1[cH:5][cH:6][cH:7][cH:8][c:9]1[N+:10](=[O:11])[O-:12]>>[CH3:1][C@@H:2]([O:3][c:4]1[cH:5][cH:6][cH:7][cH:8][c:9]1[N+:10](=[O:11])[O-:12])[C@H:13]([NH:14][C:15](=[O:16])[O:17][C:18]([CH3:19])([CH3:...
C[C@@H](O)[C@H](NC(=O)OC(C)(C)C)C(=O)O.O=[N+]([O-])c1ccccc1F
C[C@@H](Oc1ccccc1[N+](=O)[O-])[C@H](NC(=O)OC(C)(C)C)C(=O)O
null
null
CN(C=O)C
Heteroatom Alkylation and Arylation
Williamson Ether Synthesis
fc6e1b465ae75176f3fa192a660d0d622bdf538cea285b0e2b9dc00b273004b2
1f70dbbaebc288b3a5d3f37803812d9d22b151831cd4b8351080508554b19875
c1ccccc1
F-[c;H0;D3;+0:1](:[c:2]:[c:3]):[c:4](-[#7;+:5]):[c:6].[C;D1;H3:7]-[C:8](-[OH;D1;+0:9])-[C:10]-[C:11](=[O;D1;H0:12])-[O;D1;H1:13]>>[#7;+:5]-[c:4](:[c:6]):[c;H0;D3;+0:1](-[O;H0;D2;+0:9]-[C:8](-[C;D1;H3:7])-[C:10]-[C:11](=[O;D1;H0:12])-[O;D1;H1:13]):[c:2]:[c:3]
null
[]
0
CELSIUS
null
null
A solution of N-[(1,1-dimethylethoxy)carbonyl]-L-threonine (5.02 g., 22.9 mmol.) in dry dimethylformamide (10 ml.) was added dropwise over a period of 30 minutes to a cooled (0° C.) suspension of 60% sodium hydride (1.93 g., 48.25 mmol., 2.11 eq.) in dry dimethylformamide (40 ml.). The reaction was stirred at 0° C. unt...
10.6084/m9.figshare.5104873.v1
null
Aromatic halide.Secondary alcohol
Ether
c1ccccc1
c1ccccc1
c1ccccc1
HF
CN(C=O)C
0
null
C[C@@H](O)[C@H](NC(=O)OC(C)(C)C)C(=O)O.O=[N+]([O-])c1ccccc1F>CN(C=O)C>C[C@@H](Oc1ccccc1[N+](=O)[O-])[C@H](NC(=O)OC(C)(C)C)C(=O)O
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-e9bbf79d4ce94d02ab717ad740996fe9
CO.N[C@@H](CCCCO)C(=O)O>>COC(=O)[C@@H](N)CCCCO
N[C@H](C(=O)O)CCCCO.Cl.CO>>Cl.N[C@H](C(=O)OC)CCCCO
[CH3:1][OH:2].O[C:3](=[O:4])[C@@H:5]([NH2:6])[CH2:7][CH2:8][CH2:9][CH2:10][OH:11]>>[CH3:1][O:2][C:3](=[O:4])[C@@H:5]([NH2:6])[CH2:7][CH2:8][CH2:9][CH2:10][OH:11]
CO.N[C@@H](CCCCO)C(=O)O
COC(=O)[C@@H](N)CCCCO
null
null
null
Protection
Esterification of Carboxylic Acids
9cecdbd189c6f9c3648521d17154d013842a5498de4e76e65efb1d842973340b
af0b8064f2e82ebe66c4c29d2391785ac1b993104265ccdc4d67ca79e36fa3c8
null
O-[C;H0;D3;+0:1](=[O;D1;H0:2])-[C:3](-[C:4])-[N;D1;H2:5].[C;D1;H3:6]-[OH;D1;+0:7]>>[C:4]-[C:3](-[N;D1;H2:5])-[C;H0;D3;+0:1](=[O;D1;H0:2])-[O;H0;D2;+0:7]-[C;D1;H3:6]
null
[]
null
null
2.5
HOUR
A slurry of (S)-2-amino-6-hydroxyhexanoic acid (2.42 g., 16.4 mmole) in dry methanol (60 ml.) was treated with gaseous hydrogen chloride until the mixture began to reflux. The homogeneous solution was then stirred at room temperature for 2.5 hours. The solvent was stripped and the residue azeotroped three times with to...
10.6084/m9.figshare.5104873.v1
null
Carboxylic acid.Methanol
Ester
null
null
null
HO-
null
null
2.5
CO.N[C@@H](CCCCO)C(=O)O>>COC(=O)[C@@H](N)CCCCO
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-64ae065485524aae852fadf8328767e1
CCOC(=O)CN.O=C(O)[C@H](CCCCO)N1C(=O)c2ccccc2C1=O>>CCCC[C@@H](C(=O)NCC(=O)OCC)N1C(=O)c2ccccc2C1=O
Cl.NCC(=O)OCC.CN1CCOCC1.C1(C=2C(C(N1[C@H](C(=O)O)CCCCO)=O)=CC=CC2)=O.OC1=CC=CC=2NN=NC21>>C1(C=2C(C(N1[C@H](C(=O)NCC(=O)OCC)CCCC)=O)=CC=CC2)=O
[NH2:8][CH2:9][C:10](=[O:11])[O:12][CH2:13][CH3:14].O[CH2:1][CH2:2][CH2:3][CH2:4][C@@H:5]([C:6](O)=[O:7])[N:15]1[C:16](=[O:17])[c:18]2[cH:19][cH:20][cH:21][cH:22][c:23]2[C:24]1=[O:25]>>[CH3:1][CH2:2][CH2:3][CH2:4][C@@H:5]([C:6](=[O:7])[NH:8][CH2:9][C:10](=[O:11])[O:12][CH2:13][CH3:14])[N:15]1[C:16](=[O:17])[c:18]2[cH:1...
CCOC(=O)CN.O=C(O)[C@H](CCCCO)N1C(=O)c2ccccc2C1=O
CCCC[C@@H](C(=O)NCC(=O)OCC)N1C(=O)c2ccccc2C1=O
null
null
CN(C=O)C
Acylation
OtherReaction
0417a24920227ec1bd95566b2c81b0ce9679eff3bca069621b0123bac13830c8
a1b92777bbff0323f68374ba2bb35d2b7447e9327d1247846bdecf2f4bf4b05b
O=C1NC(=O)c2ccccc21
O-[CH2;D2;+0:1]-[C:2]-[C:3]-[C:4]-[C:5](-[#7:6](-[C:7]=[O;D1;H0:8])-[C:9]=[O;D1;H0:10])-[C;H0;D3;+0:11](-O)=[O;D1;H0:12].[C:13]-[#8:14]-[C:15](=[O;D1;H0:16])-[C:17]-[NH2;D1;+0:18]>>[C:13]-[#8:14]-[C:15](=[O;D1;H0:16])-[C:17]-[NH;D2;+0:18]-[C;H0;D3;+0:11](=[O;D1;H0:12])-[C:5](-[C:4]-[C:3]-[C:2]-[CH3;D1;+0:1])-[#7:6](-[C...
null
[]
null
null
5
MINUTE
A slurry of glycine, ethyl ester, hydrochloride salt (2.718 g, 19.5 mmol.) in dimethylformamide (36 ml.) was treated with 4-methyl morpholine (2.60 ml., 2.39 g., 23.6 mmol.) and stirred at room temperature for 5 minutes. The mixture was then treated with (S)-2-phthalimido-6-hydroxyhexanoic acid (4.50 g., 16.2 mmol.) an...
10.6084/m9.figshare.5104873.v1
null
Carboxylic acid.Primary alcohol.Primary amine
Secondary amide
null
null
c1ccc2c(c1)C[NH]C2
HO-
CN(C=O)C
null
0.083333
CCOC(=O)CN.O=C(O)[C@H](CCCCO)N1C(=O)c2ccccc2C1=O>CN(C=O)C>CCCC[C@@H](C(=O)NCC(=O)OCC)N1C(=O)c2ccccc2C1=O
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-1a4951c4532f4cb2bdd53951628d0ded
C=CC(=O)OCC.[N-]=[N+]=NC1CCc2ccccc2NC1=O>>CCOC(=O)CCN1C(=O)C(N=[N+]=[N-])CCc2ccccc21
N(=[N+]=[N-])C1C(NC2=C(CC1)C=CC=C2)=O.C(C=C)(=O)OCC.C(C)(C)(C)O.[K]>>N(=[N+]=[N-])C1C(N(C2=C(CC1)C=CC=C2)CCC(=O)OCC)=O
[CH3:1][CH2:2][O:3][C:4](=[O:5])[CH:6]=[CH2:7].[NH:8]1[C:9](=[O:10])[CH:11]([N:12]=[N+:13]=[N-:14])[CH2:15][CH2:16][c:17]2[cH:18][cH:19][cH:20][cH:21][c:22]21>>[CH3:1][CH2:2][O:3][C:4](=[O:5])[CH2:6][CH2:7][N:8]1[C:9](=[O:10])[CH:11]([N:12]=[N+:13]=[N-:14])[CH2:15][CH2:16][c:17]2[cH:18][cH:19][cH:20][cH:21][c:22]21
C=CC(=O)OCC.[N-]=[N+]=NC1CCc2ccccc2NC1=O
CCOC(=O)CCN1C(=O)C(N=[N+]=[N-])CCc2ccccc21
null
null
O1CCCC1.C(C)(C)(C)O.O1CCCC1
Heteroatom Alkylation and Arylation
aza-Michael addition secondary
ba7c4bd71d9dac9254c12d0209ebbe315a4f74699e256502917bd8de51885203
91e54cd6e65f2c08b5c1a8b4338c7ceefc90d4eb91eb55b2313d1887e8793e60
O=C1CCCc2ccccc2N1
[C:1]-[#8:2]-[C:3](=[O;D1;H0:4])-[CH;D2;+0:5]=[CH2;D1;+0:6].[C:7]-[C:8](=[O;D1;H0:9])-[NH;D2;+0:10]-[c:11](:[c:12]):[c:13]>>[C:7]-[C:8](=[O;D1;H0:9])-[N;H0;D3;+0:10](-[CH2;D2;+0:6]-[CH2;D2;+0:5]-[C:3](=[O;D1;H0:4])-[#8:2]-[C:1])-[c:11](:[c:12]):[c:13]
null
[]
null
null
null
null
A solution of 3-azido-1,3,4,5-tetrahydro-2H-1-benzazepin-2-one [prepared as described by Watthey et al., J. Med. Chem., 28, p. 1511-15156 (1985)] in tetrahydrofuran/tert-butanol was cooled to 0° C. and treated with ethyl acrylate and 1N tert-butanol, potassium salt/tetrahydrofuran according to the procedure of Example ...
10.6084/m9.figshare.5104873.v1
null
Ester.Secondary amide.Vinyl
Ester.Tertiary amide
c1ccc2c(c1)CCCCN2
c1ccc2c(c1)CCCC[NH]2
c1ccc2c(c1)CCCC[NH]2
null
O1CCCC1.C(C)(C)(C)O.O1CCCC1
null
null
C=CC(=O)OCC.[N-]=[N+]=NC1CCc2ccccc2NC1=O>O1CCCC1.C(C)(C)(C)O.O1CCCC1>CCOC(=O)CCN1C(=O)C(N=[N+]=[N-])CCc2ccccc21
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-d269152a14054777a8d6f6accb67dec8
CC(C)(C)OC(=O)NN.CCOC(=O)CBr>>CCOC(=O)CNNC(=O)OC(C)(C)C
C(C)N(CC)CC.C(C)N(CC)CC.BrCC(=O)OCC.C(C)N(CC)CC.N(N)C(=O)OC(C)(C)C.BrCC(=O)OCC.BrCC(=O)OCC>>CC(C)(OC(=O)NNCC(=O)OCC)C
[NH2:7][NH:8][C:9](=[O:10])[O:11][C:12]([CH3:13])([CH3:14])[CH3:15].Br[CH2:6][C:4]([O:3][CH2:2][CH3:1])=[O:5]>>[CH3:1][CH2:2][O:3][C:4](=[O:5])[CH2:6][NH:7][NH:8][C:9](=[O:10])[O:11][C:12]([CH3:13])([CH3:14])[CH3:15]
CC(C)(C)OC(=O)NN.CCOC(=O)CBr
CCOC(=O)CNNC(=O)OC(C)(C)C
null
null
C1=CC=CC=C1
Heteroatom Alkylation and Arylation
N-alkylation of primary amines with alkyl halides
a10280ad95ed368c75fdf1d65f9c7b02199bd814b62740ab81803f6da82dc483
150ef5d6000fad15b6e5d9a7d488fe3ba905820f4205bfb36d0ee312b4df76ec
null
Br-[CH2;D2;+0:1]-[C:2](=[O;D1;H0:3])-[#8:4]-[C:5].[C;D1;H3:6]-[C:7](-[C;D1;H3:8])(-[C;D1;H3:9])-[#8:10]-[C:11](=[O;D1;H0:12])-[#7:13]-[NH2;D1;+0:14]>>[C:5]-[#8:4]-[C:2](=[O;D1;H0:3])-[CH2;D2;+0:1]-[NH;D2;+0:14]-[#7:13]-[C:11](=[O;D1;H0:12])-[#8:10]-[C:7](-[C;D1;H3:6])(-[C;D1;H3:8])-[C;D1;H3:9]
null
[]
null
null
null
null
Triethylamine (13.94 ml., 0.1 mol.) was added to a solution of hydrazine carboxylic acid, 1,1-dimethylethyl ester (13.216 g., 0.1 mole) in benzene (100 ml.), followed by the addition of ethyl bromoacetate (11.09 ml., 0.1 mol.). The reaction mixture was refluxed (oil bath, 95°-100° C.) for 14 hours, after which triethyl...
10.6084/m9.figshare.5104873.v1
null
Acylhydrazine.Primary halide
Acylhydrazine.Ester
null
null
null
HBr
C1=CC=CC=C1
null
null
CC(C)(C)OC(=O)NN.CCOC(=O)CBr>C1=CC=CC=C1>CCOC(=O)CNNC(=O)OC(C)(C)C
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-fcdfc14041c342599ff1c5287314bf6b
CCCC[C@@H](N)C(=O)O.[Br-]>>CCCC[C@H](Br)C(=O)O
[Br-].[K+].N[C@H](CCCC)C(=O)O.N(=O)[O-].[Na+]>>Br[C@H](C(=O)O)CCCC
N[C@H:5]([CH2:4][CH2:3][CH2:2][CH3:1])[C:7](=[O:8])[OH:9].[Br-:6]>>[CH3:1][CH2:2][CH2:3][CH2:4][C@H:5]([Br:6])[C:7](=[O:8])[OH:9]
CCCC[C@@H](N)C(=O)O.[Br-]
CCCC[C@H](Br)C(=O)O
null
null
S(O)(O)(=O)=O
Functional Group Interconversion
OtherReaction
117344ae409beae3589a30d5997369184f62edb887830bd6b795e8dfdf82920d
9544d3c5449a12cdcbad58c02e82937c94837ec7c67e3baf5ab21c8ae3b17e42
null
N-[C@H;D3;+0:1](-[C:2]-[C:3])-[C:4](=[O;D1;H0:5])-[O;D1;H1:6].[Br-;H0;D0:7]>>[Br;H0;D1;+0:7]-[C@@H;D3;+0:1](-[C:2]-[C:3])-[C:4](=[O;D1;H0:5])-[O;D1;H1:6]
null
[]
-10
CELSIUS
1
HOUR
Potassium bromide (15.9 g., .133 mmol.) was added to a stirred solution of D-norleucine (5.0 g., 38 mmol.) in 2.5N sulfuric acid (77 ml.) at room temperature. The reaction mixture was cooled to -10° C. and solid sodium nitrite (3.94 g., 57 mmol.) was added portionwise, maintaining the temperature between -10° and -5° C...
10.6084/m9.figshare.5104873.v1
null
Primary amine
Secondary halide
null
null
null
Other
S(O)(O)(=O)=O
-10
1
CCCC[C@@H](N)C(=O)O.[Br-]>S(O)(O)(=O)=O>CCCC[C@H](Br)C(=O)O
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-2dd08204e1ab4e3cac55386d2d7fb4fa
CC(=Cc1ccccc1)C(=O)O>>CC(Cc1ccccc1)C(=O)O
CC(C(=O)O)=CC1=CC=CC=C1>>CC(C(=O)O)CC1=CC=CC=C1
[CH3:1][C:2](=[CH:3][c:4]1[cH:5][cH:6][cH:7][cH:8][cH:9]1)[C:10](=[O:11])[OH:12]>>[CH3:1][CH:2]([CH2:3][c:4]1[cH:5][cH:6][cH:7][cH:8][cH:9]1)[C:10](=[O:11])[OH:12]
CC(=Cc1ccccc1)C(=O)O
CC(Cc1ccccc1)C(=O)O
null
[Pd]
CO
Reduction
Hydrogenation (double to single)
0bc3968b35f0839c230afb4215314da278abd4e1f10e42ec3012c5512de49ea5
312e9350dcad67590617294c0eb017edf0b9fbfe6133c06a3f393b871a889092
c1ccccc1
[C;D1;H3:1]-[C;H0;D3;+0:2](=[CH;D2;+0:3]-[c:4](:[c:5]):[c:6])-[C:7](=[O;D1;H0:8])-[O;D1;H1:9]>>[C;D1;H3:1]-[CH;D3;+0:2](-[CH2;D2;+0:3]-[c:4](:[c:5]):[c:6])-[C:7](=[O;D1;H0:8])-[O;D1;H1:9]
null
[]
null
null
null
null
A solution of α-methyl cinnamic acid (10.0 g., 61.7 mmol.) in dry methanol (250 ml.) was treated with 10% palladium on carbon and hydrogenated (balloon used) at room temperature for 16 hours. The reaction mixture was diluted with methanol (250 ml.), filtered through a Celite pad in a millipore unit, washing the pad wel...
10.6084/m9.figshare.5104873.v1
null
null
null
null
null
c1ccccc1
null
[Pd].CO
null
null
CC(=Cc1ccccc1)C(=O)O>[Pd].CO>CC(Cc1ccccc1)C(=O)O
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-b0ab2ffb190f41a3906168de2e0367c1
BrCc1ccccc1.O=C(O)[C@H](CCCCO)N1C(=O)c2ccccc2C1=O>>O=C(OCc1ccccc1)[C@H](CCCCO)N1C(=O)c2ccccc2C1=O
C([O-])([O-])=O.[Cs+].[Cs+].C1(C=2C(C(N1[C@H](C(=O)O)CCCCO)=O)=CC=CC2)=O.C(C1=CC=CC=C1)Br>>C1(C=2C(C(N1[C@H](C(=O)OCC1=CC=CC=C1)CCCCO)=O)=CC=CC2)=O
Br[CH2:4][c:5]1[cH:6][cH:7][cH:8][cH:9][cH:10]1.[O:1]=[C:2]([OH:3])[C@H:11]([CH2:12][CH2:13][CH2:14][CH2:15][OH:16])[N:17]1[C:18](=[O:19])[c:20]2[cH:21][cH:22][cH:23][cH:24][c:25]2[C:26]1=[O:27]>>[O:1]=[C:2]([O:3][CH2:4][c:5]1[cH:6][cH:7][cH:8][cH:9][cH:10]1)[C@H:11]([CH2:12][CH2:13][CH2:14][CH2:15][OH:16])[N:17]1[C:18...
BrCc1ccccc1.O=C(O)[C@H](CCCCO)N1C(=O)c2ccccc2C1=O
O=C(OCc1ccccc1)[C@H](CCCCO)N1C(=O)c2ccccc2C1=O
null
null
CN(C=O)C
Heteroatom Alkylation and Arylation
Williamson Ether Synthesis
06c4f868ad4646eea8208ecb83f54ca035dd62d04f0d8101641a4f487f2c695c
8446834f0edd1e71a2dcaffc09b80c7367abf3407263a8998354a2d20c1766bb
O=C(CN1C(=O)c2ccccc2C1=O)OCc1ccccc1
Br-[CH2;D2;+0:1]-[c:2](:[c:3]):[c:4].[C:5]-[C:6](=[O;D1;H0:7])-[OH;D1;+0:8]>>[C:5]-[C:6](=[O;D1;H0:7])-[O;H0;D2;+0:8]-[CH2;D2;+0:1]-[c:2](:[c:3]):[c:4]
null
[]
null
null
2
HOUR
A slurry of cesium carbonate (3.819 g, 11.7 mmol.) and (S)-2-phthalimido-6-hydroxyhexanoic acid (6.00 g, 21.6 mmol.) in dimethylformamide (60 ml.) was treated with benzyl bromide (3.30 ml., 4.75 g., 27.7 mmol.). After stirring at room temperature for 2 hours, the mixture was partitioned between ethyl acetate and water....
10.6084/m9.figshare.5104873.v1
null
Primary halide.Carboxylic acid
Ester
null
null
c1ccccc1.c1ccc2c(c1)C[NH]C2
HBr
CN(C=O)C
null
2
BrCc1ccccc1.O=C(O)[C@H](CCCCO)N1C(=O)c2ccccc2C1=O>CN(C=O)C>O=C(OCc1ccccc1)[C@H](CCCCO)N1C(=O)c2ccccc2C1=O
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-efe923230555472e8f595617781b5290
CI.O=C(O)[C@H](CCCCO)N1C(=O)c2ccccc2C1=O>>COC(=O)[C@H](CCCCO)N1C(=O)c2ccccc2C1=O
C1(C=2C(C(N1[C@H](C(=O)O)CCCCO)=O)=CC=CC2)=O.C([O-])([O-])=O.[Cs+].[Cs+].CI>>C1(C=2C(C(N1[C@H](C(=O)OC)CCCCO)=O)=CC=CC2)=O
I[CH3:1].[OH:2][C:3](=[O:4])[C@H:5]([CH2:6][CH2:7][CH2:8][CH2:9][OH:10])[N:11]1[C:12](=[O:13])[c:14]2[cH:15][cH:16][cH:17][cH:18][c:19]2[C:20]1=[O:21]>>[CH3:1][O:2][C:3](=[O:4])[C@H:5]([CH2:6][CH2:7][CH2:8][CH2:9][OH:10])[N:11]1[C:12](=[O:13])[c:14]2[cH:15][cH:16][cH:17][cH:18][c:19]2[C:20]1=[O:21]
CI.O=C(O)[C@H](CCCCO)N1C(=O)c2ccccc2C1=O
COC(=O)[C@H](CCCCO)N1C(=O)c2ccccc2C1=O
null
null
CN(C=O)C.C(C)(=O)OCC
Heteroatom Alkylation and Arylation
Williamson Ether Synthesis
9474aa79a2adc7353c0c02444ca598a6f486ecdd7ed5edb9ae0645721ee50389
badd4f82161bb0ee7acffd023ea4caae5d036bce7065c10ab0a06e83a6a6f119
O=C1NC(=O)c2ccccc21
I-[CH3;D1;+0:1].[C:2]-[C:3](=[O;D1;H0:4])-[OH;D1;+0:5]>>[C:2]-[C:3](=[O;D1;H0:4])-[O;H0;D2;+0:5]-[CH3;D1;+0:1]
196
[{"value": 196.0, "product": "C1(C=2C(C(N1[C@H](C(=O)OC)CCCCO)=O)=CC=CC2)=O", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
2
HOUR
A slurry of (S)-2-phthalimido-6-hydroxyhexanoic acid (3.752 g., 13.5 mmol.) and cesium carbonate (2.178 g., 6.7 mmol.) in dimethylformamide (44 ml.) was treated with methyl iodide (3.0 ml., 6.84 g., 48.2 mmol.). After stirring at room temperature for 2 hours, the mixture was diluted with ethyl acetate and washed succes...
10.6084/m9.figshare.5104873.v1
null
Carboxylic acid
Ester
null
null
c1ccc2c(c1)C[NH]C2
HI
CN(C=O)C.C(C)(=O)OCC
null
2
CI.O=C(O)[C@H](CCCCO)N1C(=O)c2ccccc2C1=O>CN(C=O)C.C(C)(=O)OCC>COC(=O)[C@H](CCCCO)N1C(=O)c2ccccc2C1=O
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-276860cf665e4f20bd9d6fbcfc7e8c12
CCOC(=O)CBr.C[C@@H]1CCC[C@H](NC(=O)OC(C)(C)C)C(=O)N1>>CCOC(=O)CN1C(=O)[C@@H](NC(=O)OC(C)(C)C)CCC[C@H]1C
CC(C)(OC(=O)N[C@@H]1C(N[C@@H](CCC1)C)=O)C.C[Si](C)(C)[N-][Si](C)(C)C.[Li+].BrCC(=O)OCC>>CC(C)(OC(=O)N[C@@H]1C(N([C@@H](CCC1)C)CC(=O)OCC)=O)C
Br[CH2:6][C:4]([O:3][CH2:2][CH3:1])=[O:5].[NH:7]1[C:8](=[O:9])[C@@H:10]([NH:11][C:12](=[O:13])[O:14][C:15]([CH3:16])([CH3:17])[CH3:18])[CH2:19][CH2:20][CH2:21][C@H:22]1[CH3:23]>>[CH3:1][CH2:2][O:3][C:4](=[O:5])[CH2:6][N:7]1[C:8](=[O:9])[C@@H:10]([NH:11][C:12](=[O:13])[O:14][C:15]([CH3:16])([CH3:17])[CH3:18])[CH2:19][CH...
CCOC(=O)CBr.C[C@@H]1CCC[C@H](NC(=O)OC(C)(C)C)C(=O)N1
CCOC(=O)CN1C(=O)[C@@H](NC(=O)OC(C)(C)C)CCC[C@H]1C
null
null
O1CCCC1
Heteroatom Alkylation and Arylation
N-alkylation of secondary amines with alkyl halides
21efda898581b4e7e1b0a01b07328527522c0c899fbfe8483d7f4fdc1f9e273c
933a6f1013d44497c9c5902b73c24fbdc7813d20b886bdbc4c670d5b43ca2182
O=C1CCCCCN1
Br-[CH2;D2;+0:1]-[C:2](=[O;D1;H0:3])-[#8:4]-[C:5].[C:6]-[C:7](=[O;D1;H0:8])-[NH;D2;+0:9]-[C:10](-[C;D1;H3:11])-[C:12]>>[C:6]-[C:7](=[O;D1;H0:8])-[N;H0;D3;+0:9](-[CH2;D2;+0:1]-[C:2](=[O;D1;H0:3])-[#8:4]-[C:5])-[C:10](-[C;D1;H3:11])-[C:12]
null
[]
null
null
30
MINUTE
A solution of (3S-cis)-hexahydro-3-[[(1,1-dimethylethoxy)carbonyl]amino]-7-methyl-2H-azepin-2-one [prepared as described in Example 64(f), 500 mg., 2.06 mmol.] in tetrahydrofuran (13 ml.) at room temperature under argon was treated dropwise with 1.0M lithium bis(trimethylsilyl)amide in tetrahydrofuran (2.7 ml., 2.7 mmo...
10.6084/m9.figshare.5104873.v1
null
Primary halide.Ester.Secondary amide
Ester.Tertiary amide
C1CCCNCC1
C1CCC[NH]CC1
C1CCC[NH]CC1
HBr
O1CCCC1
null
0.5
CCOC(=O)CBr.C[C@@H]1CCC[C@H](NC(=O)OC(C)(C)C)C(=O)N1>O1CCCC1>CCOC(=O)CN1C(=O)[C@@H](NC(=O)OC(C)(C)C)CCC[C@H]1C
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-6701048b9aed462d813326f7541d1d53
CC(C)NC(C)C.ClCCCCBr.O=C(O)C1CCCC1>>CC(C)[N-]C(C)C.O=C(O)C1(CCCCCl)CCCC1.[Li+]
BrCCCCCl.C1(CCCC1)C(=O)O.C(C)(C)NC(C)C.C(CCC)[Li]>>C(C)(C)[N-]C(C)C.[Li+].ClCCCCC1(CCCC1)C(=O)O
[CH3:1][CH:2]([CH3:3])[NH:4][CH:5]([CH3:6])[CH3:7].Br[CH2:12][CH2:13][CH2:14][CH2:15][Cl:16].[O:8]=[C:9]([OH:10])[CH:11]1[CH2:17][CH2:18][CH2:19][CH2:20]1>>[CH3:1][CH:2]([CH3:3])[N-:4][CH:5]([CH3:6])[CH3:7].[O:8]=[C:9]([OH:10])[C:11]1([CH2:12][CH2:13][CH2:14][CH2:15][Cl:16])[CH2:17][CH2:18][CH2:19][CH2:20]1.[Li+:21]
CC(C)NC(C)C.ClCCCCBr.O=C(O)C1CCCC1
CC(C)[N-]C(C)C.O=C(O)C1(CCCCCl)CCCC1.[Li+]
null
null
O1CCCC1
C-C Coupling
OtherReaction
77153b7242f8754879e3f0b886657cd5957a50555e81a521ab32e496bf739211
9ba1e0467902f373f7806da8e18ec7a85760b64f74aa649da2579d00e73d9ca4
C1CCCC1
Br-[CH2;D2;+0:1]-[C:2]-[C:3].[C;D1;H3:4]-[C:5](-[C;D1;H3:6])-[NH;D2;+0:7]-[C:8](-[C;D1;H3:9])-[C;D1;H3:10].[O;D1;H0:11]=[C:12](-[O;D1;H1:13])-[CH;D3;+0:14]1-[C:15]-[C:16]-[C:17]-[C:18]-1>>[C;D1;H3:4]-[C:5](-[C;D1;H3:6])-[N-;H0;D2:7]-[C:8](-[C;D1;H3:9])-[C;D1;H3:10].[C:3]-[C:2]-[CH2;D2;+0:1]-[C;H0;D4;+0:14]1(-[C:12](=[O...
null
[]
-74
CELSIUS
15
MINUTE
A solution of lithium diisopropylamide was prepared under nitrogen from diisopropylamine (31.0 ml., 220 mmol.) and n-butyl lithium (1.5M in hexane, 88.0 ml., 220 mmol.) in tetrahydrofuran (80 ml.), maintaining the temperature between -3° C. -1° C. After stirring 15 minutes, cyclopentanecarboxylic acid (11.4 g., 100 mmo...
10.6084/m9.figshare.5104873.v1
null
Primary halide.Secondary amine
null
C1CCCC1
C1CCCC1
C1CCCC1
null
O1CCCC1
-74
0.25
CC(C)NC(C)C.ClCCCCBr.O=C(O)C1CCCC1>O1CCCC1>CC(C)[N-]C(C)C.O=C(O)C1(CCCCCl)CCCC1.[Li+]
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-765f7e8377cb44718d3884bdc87dc102
CCCCC.CCOCC.CCOCC>>O=C1CCCCCC12CCCC2
C(C)(C)(C)[Li].CCOCC.CCOCC.CCCCC>>C1CCCC12C(CCCCC2)=O
[CH3:8][CH2:12][CH2:11][CH2:10][CH3:9].C([O:1][CH2:2][CH3:3])[CH3:5].CCO[CH2:7][CH3:6]>>[O:1]=[C:2]1[CH2:3][CH2:4][CH2:5][CH2:6][CH2:7][C:8]12[CH2:9][CH2:10][CH2:11][CH2:12]2
CCCCC.CCOCC.CCOCC
O=C1CCCCCC12CCCC2
null
null
null
Acylation
OtherReaction
7f9c56080232237cb2af9c91b9ac11dba4e3d417835241b7fb2a95600fe5c061
71cd9ffc2461c2b8f2c58f8e59f7f0e3e5cc0afbee292adb82f64bbd7fde8e75
O=C1CCCCCC12CCCC2
C-C-O-[CH2;D2;+0:1]-[CH3;D1;+0:2].[CH3;D1;+0:3]-[CH2;D2;+0:4]-[O;H0;D2;+0:5]-C-[CH3;D1;+0:6].[CH3;D1;+0:7]-[C:8]-[C:9]-[C:10]-[CH3;D1;+0:11]>>[O;H0;D1;+0:5]=[C;H0;D3;+0:4]1-[CH2;D2;+0:3]-[C:12]-[CH2;D2;+0:6]-[CH2;D2;+0:2]-[CH2;D2;+0:1]-[C;H0;D4;+0:7]-12-[C:8]-[C:9]-[C:10]-[CH2;D2;+0:11]-2
null
[]
-100
CELSIUS
null
null
t-Butyl lithium (1.7M in pentane, 20.0 ml., 34 mmol.) was slowly added to ether (38 ml.) at -20° C. as the reaction was further cooled to -100° C. in a methanol/dry ice/liquid nitrogen bath. To this -100° C. solution was added the product from part (c) (5.0 g., 16.1 mmol.) in 2:1 ether/pentane (3 ml.) over 35 minutes, ...
10.6084/m9.figshare.5104873.v1
null
Ether.Ether
Ketone
null
C1CCCC2(CC1)CCCC2
C1CCCC2(CC1)CCCC2
HO-
null
-100
null
CCCCC.CCOCC.CCOCC>>O=C1CCCCCC12CCCC2