dataset_id
large_stringclasses
414 values
reaction_id
large_stringlengths
36
36
reaction_smiles
large_stringlengths
4
873
rxn_insight_reaction
large_stringlengths
19
1.07k
mapped_reaction_smiles
large_stringlengths
14
3.37k
reactant_smiles
large_stringlengths
1
581
product_smiles
large_stringlengths
1
433
reagent_smiles
large_stringclasses
634 values
catalyst_smiles
large_stringlengths
1
683
solvent_smiles
large_stringlengths
1
245
rxn_insight_class
large_stringclasses
11 values
rxn_insight_name
large_stringclasses
346 values
rxn_insight_tag
large_stringlengths
64
64
rxn_insight_tag2
large_stringlengths
64
64
rxn_insight_scaffold
large_stringlengths
5
288
rxn_insight_template
large_stringlengths
24
2.64k
yield_percent
float64
-0.8
90,205,160,000B
yield_measurements
large_stringlengths
2
864
temperature_value
float64
-230
30.1k
temperature_units
large_stringclasses
3 values
reaction_time_value
float64
0
4k
time_units
large_stringclasses
4 values
procedure_details
large_stringlengths
1
23.6k
reference
large_stringclasses
96 values
doi
large_stringclasses
19 values
functional_groups_reactants
large_stringlengths
3
716
functional_groups_products
large_stringlengths
3
539
participating_rings_reactants
large_stringlengths
5
293
participating_rings_products
large_stringlengths
5
271
all_rings_products
large_stringlengths
5
271
byproduct_smiles
large_stringclasses
176 values
agent_smiles
large_stringlengths
1
712
temperature_c
float64
-230
30.1k
reaction_time_hours
float64
0
2.16k
reaction_smiles_with_agents
large_stringlengths
4
882
ord_dataset-c2ad1656a3ca4d08888ffb6e3f3a2742
ord-a7f27325a7db463097aa4e14db1b2c3d
O=Cc1ccccc1Br.O=Cc1ccccn1.[Li][CH2]CCC>>CCCCC(O)C1=CC=CCC1(O)Cc1ccccn1
N1=C(C=CC=C1)C=O.C(CCC)[Li].BrC1=C(C=O)C=CC=C1.CCOCC.C(CCC)[Li].[Cl-].[NH4+]>>OC1(CC2=NC=CC=C2)CC=CC=C1C(CCCC)O
Br[c:12]1[c:7]([CH:5]=[O:6])[cH:8][cH:9][cH:10][cH:11]1.[O:13]=[CH:14][c:15]1[cH:16][cH:17][cH:18][cH:19][n:20]1.[Li][CH2:4][CH2:3][CH2:2][CH3:1]>>[CH3:1][CH2:2][CH2:3][CH2:4][CH:5]([OH:6])[C:7]1=[CH:8][CH:9]=[CH:10][CH2:11][C:12]1([OH:13])[CH2:14][c:15]1[cH:16][cH:17][cH:18][cH:19][n:20]1
O=Cc1ccccc1Br.O=Cc1ccccn1.[Li][CH2]CCC
CCCCC(O)C1=CC=CCC1(O)Cc1ccccn1
null
null
CCCCCC
Heteroatom Alkylation and Arylation
OtherReaction
e031a0f480b28d7406c9fbcd18b24b11407fff24d3f8282fb50539c418e7ad54
a92b097469f48c59253e44991e52c5ed7691955dc06e514e3062f5db527f870d
C1=CCC(Cc2ccccn2)C=C1
Br-[c;H0;D3;+0:1]1:[cH;D2;+0:2]:[cH;D2;+0:3]:[cH;D2;+0:4]:[cH;D2;+0:5]:[c;H0;D3;+0:6]:1-[CH;D2;+0:7]=[O;H0;D1;+0:8].[C:9]-[C:10]-[CH2;D2;+0:11]-[Li].[O;H0;D1;+0:12]=[CH;D2;+0:13]-[c:14](:[c:15]):[#7;a:16]:[c:17]>>[C:9]-[C:10]-[CH2;D2;+0:11]-[CH;D3;+0:7](-[OH;D1;+0:8])-[C;H0;D3;+0:6]1=[CH;D2;+0:5]-[CH;D2;+0:4]=[CH;D2;+0...
83.2
[{"value": 83.2, "product": "OC1(CC2=NC=CC=C2)CC=CC=C1C(CCCC)O", "details": "PERCENTYIELD", "is_desired": false}]
-45
CELSIUS
0.5
HOUR
To a mixture of 10 mL (85.6 mmol) of 2-bromobenzaldehyde in 300 mL of ether cooled to -45° C. was added in portions 8.56 mL (85.6 mmol) of 10M n-butyllithium in hexane over a 20 min period, and the reaction mixture was stirred at -20 for 1/2 h. To the above reaction mixture cooled to -20° C., was added 8.98 mL (88.9 mm...
10.6084/m9.figshare.5104873.v1
null
Aromatic halide.Aldehyde.Aldehyde.Alkyl lithium
Secondary alcohol.Tertiary alcohol.Conjugated diene
c1ccccc1
C1=CCCC=C1
C1=CCCC=C1.c1ccncc1
Br-.Li
CCCCCC
-45
0.5
O=Cc1ccccc1Br.O=Cc1ccccn1.[Li][CH2]CCC>CCCCCC>CCCCC(O)C1=CC=CCC1(O)Cc1ccccn1
ord_dataset-c2ad1656a3ca4d08888ffb6e3f3a2742
ord-6f930ecb5bb04d1aa44f812c6ea43e74
CCCCC(O)C1=CC=CCC1(O)Cc1ccccn1>>CCCCc1c2ccccc2cc2cccc[n+]12
Cl(=O)(=O)(=O)[O-].[Na+].OC1(CC2=NC=CC=C2)CC=CC=C1C(CCCC)O.S(=O)(=O)(C(F)(F)F)OS(=O)(=O)C(F)(F)F>>Cl(=O)(=O)(=O)[O-].C(CCC)C1=C2C(=CC=3C=CC=C[N+]13)C=CC=C2
O[CH:5]([CH2:4][CH2:3][CH2:2][CH3:1])[C:6]1=[CH:7][CH:8]=[CH:9][CH2:10][C:11]1(O)[CH2:12][c:13]1[cH:14][cH:15][cH:16][cH:17][n:18]1>>[CH3:1][CH2:2][CH2:3][CH2:4][c:5]1[c:6]2[cH:7][cH:8][cH:9][cH:10][c:11]2[cH:12][c:13]2[cH:14][cH:15][cH:16][cH:17][n+:18]12
CCCCC(O)C1=CC=CCC1(O)Cc1ccccn1
CCCCc1c2ccccc2cc2cccc[n+]12
null
null
C1=CC=CC=C1
Aromatic Heterocycle Formation
OtherReaction
c84f3868e0c6722589014de7c60aedba9f98be30a9ca3e55abd0ea909c901521
f51c0a0ae7a8de0b25d6d01f96a75e2856b70c8fe670dfe67c4bca77de7114cf
c1ccc2c[n+]3ccccc3cc2c1
O-[CH;D3;+0:1](-[C:2]-[C:3])-[C;H0;D3;+0:4]1=[CH;D2;+0:5]-[CH;D2;+0:6]=[CH;D2;+0:7]-[CH2;D2;+0:8]-[C;H0;D4;+0:9]-1(-O)-[CH2;D2;+0:10]-[c:11](:[c:12]):[n;H0;D2;+0:13]:[c:14]:[c:15]>>[C:3]-[C:2]-[c;H0;D3;+0:1]1:[c;H0;D3;+0:4]2:[cH;D2;+0:5]:[cH;D2;+0:6]:[cH;D2;+0:7]:[cH;D2;+0:8]:[c;H0;D3;+0:9]:2:[cH;D2;+0:10]:[c:11](:[c:1...
11
[{"value": 11.0, "product": "Cl(=O)(=O)(=O)[O-].C(CCC)C1=C2C(=CC=3C=CC=C[N+]13)C=CC=C2", "details": "PERCENTYIELD", "is_desired": false}]
null
null
null
null
To a refluxing solution of 11.1 g (0.04 mol) of 2-[1-hydroxy-6'-(1-hydroxypentyl)-benzyl]pyridine in 250 mL of benzene was added 23.9 mL (0.14 mol) of triflic anhydride in 5 min, the mixture was heated for 65 min and then cooled. The reaction mixture was concentrated in vacuo, the residual oil was triturated in ether a...
10.6084/m9.figshare.5104873.v1
null
Secondary alcohol.Tertiary alcohol.Conjugated diene
null
C1=CCCC=C1.c1ccncc1
c1ccc2c[n+]3ccccc3cc2c1
c1ccc2c[n+]3ccccc3cc2c1
HO-
C1=CC=CC=C1
null
null
CCCCC(O)C1=CC=CCC1(O)Cc1ccccn1>C1=CC=CC=C1>CCCCc1c2ccccc2cc2cccc[n+]12
ord_dataset-c2ad1656a3ca4d08888ffb6e3f3a2742
ord-f95fa9e3ced54384ab73c44eda5cce01
O=Cc1ccccn1.OCCO>>c1ccc(C2OCCO2)nc1
O.N1=C(C=CC=C1)C=O.C(CO)O.C1(=CC=C(C=C1)S(=O)(=O)O)C>>O1C(OCC1)C1=NC=CC=C1
[cH:1]1[cH:2][cH:3][c:4]([CH:5]=[O:6])[n:10][cH:11]1.O[CH2:7][CH2:8][OH:9]>>[cH:1]1[cH:2][cH:3][c:4]([CH:5]2[O:6][CH2:7][CH2:8][O:9]2)[n:10][cH:11]1
O=Cc1ccccn1.OCCO
c1ccc(C2OCCO2)nc1
null
null
C1(=CC=CC=C1)C
Heteroatom Alkylation and Arylation
OtherReaction
fe0fbb45a87f24c1e456c6b4e41101562cd8f0af3ec376bb6115e7c1555d997b
7ac65b5a5f576337ce8e86e0130eb9b4757ca21b2419a0e82bbdfd5def30ee73
c1ccc(C2OCCO2)nc1
O-[CH2;D2;+0:1]-[C:2]-[OH;D1;+0:3].[O;H0;D1;+0:4]=[CH;D2;+0:5]-[c:6](:[c:7]):[#7;a:8]:[c:9]>>[c:9]:[#7;a:8]:[c:6](-[CH;D3;+0:5]1-[O;H0;D2;+0:4]-[CH2;D2;+0:1]-[C:2]-[O;H0;D2;+0:3]-1):[c:7]
29.3
[{"value": 29.3, "product": "O1C(OCC1)C1=NC=CC=C1", "details": "PERCENTYIELD", "is_desired": false}, {"value": 29.0, "product": "O1C(OCC1)C1=NC=CC=C1", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
null
null
A mixture of 2-pyridinecarboxaldehyde (2678, 2.5 mol), ethylene glycol (310.35 g, 5 mol), and 118.8 g (0.62 mol) of p-toluenesulfonic acid in 1.5 L of toluene placed in a 3 L flask fined with a Dean Stark trap was allowed to reflux until the removal of water was complete. The mixture was concentrated in vacuo and the r...
10.6084/m9.figshare.5104873.v1
null
Aldehyde.Primary alcohol.Primary alcohol
Ether.Ether
null
C1COCO1
c1ccncc1.C1COCO1
HO-
C1(=CC=CC=C1)C
null
null
O=Cc1ccccn1.OCCO>C1(=CC=CC=C1)C>c1ccc(C2OCCO2)nc1
ord_dataset-c2ad1656a3ca4d08888ffb6e3f3a2742
ord-97e68516a7b54210978c6375755505c7
Cc1cc(Br)ccc1Br.O=C1CCC(=O)N1Br>>BrCc1cc(Br)ccc1Br
BrC1=C(C=C(C=C1)Br)C.C1CC(=O)N(C1=O)Br>>BrC1=C(CBr)C=C(C=C1)Br
[CH3:2][c:3]1[cH:4][c:5]([Br:6])[cH:7][cH:8][c:9]1[Br:10].O=C1CCC(=O)N1[Br:1]>>[Br:1][CH2:2][c:3]1[cH:4][c:5]([Br:6])[cH:7][cH:8][c:9]1[Br:10]
Cc1cc(Br)ccc1Br.O=C1CCC(=O)N1Br
BrCc1cc(Br)ccc1Br
null
C(C1=CC=CC=C1)OOCC1=CC=CC=C1
C(Cl)(Cl)(Cl)Cl
Functional Group Interconversion
Wohl-Ziegler bromination benzyl primary
45c0aca0d63a96f0092e6dded9c888827eaf6379dac179e1cefc99293896300a
08f5e7e34d3f321cce3e85421b38226d6240cca0939494ae61032d4f8405cf22
c1ccccc1
O=C1-C-C-C(=O)-N-1-[Br;H0;D1;+0:1].[CH3;D1;+0:2]-[c:3](:[c:4]):[c:5]>>[Br;H0;D1;+0:1]-[CH2;D2;+0:2]-[c:3](:[c:4]):[c:5]
55.7
[{"value": 55.7, "product": "BrC1=C(CBr)C=C(C=C1)Br", "details": "PERCENTYIELD", "is_desired": false}, {"value": 55.2, "product": "BrC1=C(CBr)C=C(C=C1)Br", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
24
HOUR
To a solution of 75 g (0.3 mol) of 2,5-dibromotoluene in 1 L of carbon tetrachloride was added 58.73 g (0.33 mol) of NBS and 50 mg of benzyl peroxide, and the resulting mixture was refluxed with stirring for 24 h. The mixture was cooled, and concentrated in vacuo. The residue was crystallized from hot methanol and wash...
10.6084/m9.figshare.5104873.v1
null
Tertiary amide.Tertiary amide
Primary halide
C1CCNC1
null
c1ccccc1
HO-
C(C1=CC=CC=C1)OOCC1=CC=CC=C1.C(Cl)(Cl)(Cl)Cl
null
24
Cc1cc(Br)ccc1Br.O=C1CCC(=O)N1Br>C(C1=CC=CC=C1)OOCC1=CC=CC=C1.C(Cl)(Cl)(Cl)Cl>BrCc1cc(Br)ccc1Br
ord_dataset-c2ad1656a3ca4d08888ffb6e3f3a2742
ord-cc9a8b29702e4dc4a1ee1ef714409b7f
BrCc1cc(Br)ccc1Br.c1ccc(C2OCCO2)nc1>>Brc1ccc(Br)c(C[n+]2ccccc2C2OCCO2)c1.[Br-]
O1C(OCC1)C1=NC=CC=C1.BrC1=C(CBr)C=C(C=C1)Br>>[Br-].BrC1=C(C[N+]2=C(C=CC=C2)C2OCCO2)C=C(C=C1)Br
[Br:1][c:2]1[cH:3][cH:4][c:5]([Br:6])[c:7]([CH2:8][Br:21])[cH:20]1.[n:9]1[cH:10][cH:11][cH:12][cH:13][c:14]1[CH:15]1[O:16][CH2:17][CH2:18][O:19]1>>[Br:1][c:2]1[cH:3][cH:4][c:5]([Br:6])[c:7]([CH2:8][n+:9]2[cH:10][cH:11][cH:12][cH:13][c:14]2[CH:15]2[O:16][CH2:17][CH2:18][O:19]2)[cH:20]1.[Br-:21]
BrCc1cc(Br)ccc1Br.c1ccc(C2OCCO2)nc1
Brc1ccc(Br)c(C[n+]2ccccc2C2OCCO2)c1.[Br-]
null
null
S1(=O)(=O)CCCC1.C(C)(=O)OCC
Functional Group Interconversion
OtherReaction
e56fd11791c067861416b6f318bdb2898b5c0e8f298d85abbe02936af387902e
47a659f5704a5b7ca1b92ff731f18f109c6bde1d45152a3a393eefbd10265508
c1ccc(C[n+]2ccccc2C2OCCO2)cc1
[#8:1]-[C:2](-[c:3](:[c:4]):[n;H0;D2;+0:5]:[c:6]:[c:7])-[#8:8].[Br;H0;D1;+0:9]-[CH2;D2;+0:10]-[c:11](:[c:12]):[c:13]>>[#8:1]-[C:2](-[c:3](:[c:4]):[n+;H0;D3:5](-[CH2;D2;+0:10]-[c:11](:[c:12]):[c:13]):[c:6]:[c:7])-[#8:8].[Br-;H0;D0:9]
79
[{"value": 79.0, "product": "[Br-].BrC1=C(C[N+]2=C(C=CC=C2)C2OCCO2)C=C(C=C1)Br", "details": "PERCENTYIELD", "is_desired": false}, {"value": 78.6, "product": "[Br-].BrC1=C(C[N+]2=C(C=CC=C2)C2OCCO2)C=C(C=C1)Br", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
null
null
A mixture of 25.03 g (0.165 mol) of 2-(1,3-dioxolan-2-yl)-pyridine and 2,5-dibromobenzyl bromide (54 g, 0,165 mol) in 60 mL of sulfolane was heated on a steam-bath for 6 h. The mixture was diluted with 600 mL of ethyl acetate, cooled, and the resulting solid product was isolated by filtration. The above solid was tritu...
10.6084/m9.figshare.5104873.v1
null
Primary halide
null
c1ccncc1
C1=CC=[NH+]C=C1
c1ccccc1.C1=CC=[NH+]C=C1.C1COCO1
null
S1(=O)(=O)CCCC1.C(C)(=O)OCC
null
null
BrCc1cc(Br)ccc1Br.c1ccc(C2OCCO2)nc1>S1(=O)(=O)CCCC1.C(C)(=O)OCC>Brc1ccc(Br)c(C[n+]2ccccc2C2OCCO2)c1.[Br-]
ord_dataset-c2ad1656a3ca4d08888ffb6e3f3a2742
ord-7efa731e8f694dbfb068dab0ee90d921
c1ccc2c[n+]3ccccc3cc2c1>>c1ccc2c(c1)Cc1cccc[n+]1C2
Cl(=O)(=O)(=O)[O-].C1=CC=C[N+]=2C=C3C(=CC12)C=CC=C3.COC1=CC=C(CN2N=C(C=C2)C(=C)C2=NN(C=C2)CC2=CC=C(C=C2)OC)C=C1>>Cl(=O)(=O)(=O)[O-].C1=CC=C[N+]=2CC3=C(CC12)C=CC=C3
[cH:6]1[cH:7][cH:8][c:9]2[c:10]([cH:11]1)[cH:12][c:13]1[cH:14][cH:15][cH:16][cH:17][n+:18]1[cH:19]2>>[cH:6]1[cH:7][cH:8][c:9]2[c:10]([cH:11]1)[CH2:12][c:13]1[cH:14][cH:15][cH:16][cH:17][n+:18]1[CH2:19]2
c1ccc2c[n+]3ccccc3cc2c1
c1ccc2c(c1)Cc1cccc[n+]1C2
null
null
[N+](=O)([O-])C
Reduction
OtherReaction
7cdb7aaca538fff6a3dac1c2ddd900795b832d55bb2ce8c0d156d768f2ba1c03
312e9350dcad67590617294c0eb017edf0b9fbfe6133c06a3f393b871a889092
c1ccc2c(c1)Cc1cccc[n+]1C2
[c:1]:[c:2]1:[cH;D2;+0:3]:[c:4](:[c:5]):[#7;a;+:6](:[c:7]):[cH;D2;+0:8]:[c:9]:1:[c:10]>>[c:1]:[c:2]1:[c:9](:[c:10])-[CH2;D2;+0:8]-[#7;a;+:6](:[c:7]):[c:4](:[c:5])-[CH2;D2;+0:3]-1
null
[]
null
null
null
null
A reaction mixture containing benzo[b]quinolizinium perchlorate (9.5 g; 6.8 mmol) and 1,1-di-[(1-p-methoxybenzyl)-pyrazol-3-yl)ethylene (14.9 g; 0.034 mol) in 300 mL of nitromethane was refluxed for 16 h under nitrogen. The reaction mixture was concentrated in vacuo, the residue was triturated with 400 mL of methanol, ...
10.6084/m9.figshare.5104873.v1
null
null
null
c1ccc2c[n+]3ccccc3cc2c1
c1ccc2c(c1)Cc1cccc[n+]1C2
c1ccc2c(c1)Cc1cccc[n+]1C2
null
[N+](=O)([O-])C
null
null
c1ccc2c[n+]3ccccc3cc2c1>[N+](=O)([O-])C>c1ccc2c(c1)Cc1cccc[n+]1C2
ord_dataset-c2ad1656a3ca4d08888ffb6e3f3a2742
ord-890b521151d148d6ac87282c67673b5a
CC(Br)Br.CCOC(=O)c1ccoc1>>CC=C(OCC)c1ccoc1
C([O-])([O-])=O.[K+].[K+].CN(C)CCN(C)C.O1C=C(C=C1)C(=O)OCC.BrC(C)Br>>O1C=C(C=C1)C(=CC)OCC
Br[CH:2](Br)[CH3:1].O=[C:3]([O:4][CH2:5][CH3:6])[c:7]1[cH:8][cH:9][o:10][cH:11]1>>[CH3:1][CH:2]=[C:3]([O:4][CH2:5][CH3:6])[c:7]1[cH:8][cH:9][o:10][cH:11]1
CC(Br)Br.CCOC(=O)c1ccoc1
CC=C(OCC)c1ccoc1
null
[Zn].Cl[Ti](Cl)(Cl)Cl
C(Cl)Cl.C1CCOC1
C-C Coupling
OtherReaction
b75b3bce30a6373d339e9987c31d379a4f3d2ed45ea21c78854e952e43da1243
5330b04385989beb765aabd8bd463ff2d23c2650a9c6675c8c17037535e79bca
c1ccoc1
Br-[CH;D3;+0:1](-Br)-[C;D1;H3:2].O=[C;H0;D3;+0:3](-[#8:4]-[C:5])-[c:6]1:[c:7]:[#8;a:8]:[c:9]:[c:10]:1>>[C:5]-[#8:4]-[C;H0;D3;+0:3](=[CH;D2;+0:1]-[C;D1;H3:2])-[c:6]1:[c:7]:[#8;a:8]:[c:9]:[c:10]:1
54.3
[{"value": 54.3, "product": "O1C=C(C=C1)C(=CC)OCC", "details": "PERCENTYIELD", "is_desired": false}, {"value": 54.3, "product": "O1C=C(C=C1)C(=CC)OCC", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
10
MINUTE
To 300 mL of THF was added with cooling (ice-bath) 300 mL (0.3 mol) of 1M TiCl4 in methylene chloride and the mixture was stirred for 10 min. To the above mixture was added at room temperature 90.5 mL (0.6 mol) of TMEDA, the mixture was stirred for 10 min, and then 44.12 g (0.675 mol) of Zn dust was added with cooling ...
10.6084/m9.figshare.5104873.v1
null
Secondary halide.Secondary halide.Ester
Ether
null
null
c1ccoc1
Br-
[Zn].Cl[Ti](Cl)(Cl)Cl.C(Cl)Cl.C1CCOC1
null
0.166667
CC(Br)Br.CCOC(=O)c1ccoc1>[Zn].Cl[Ti](Cl)(Cl)Cl.C(Cl)Cl.C1CCOC1>CC=C(OCC)c1ccoc1
ord_dataset-c2ad1656a3ca4d08888ffb6e3f3a2742
ord-4b6d8583ad144aa1990c4ddd9ecf4d80
CNOC.O=C(O)c1ccoc1>>CON(C)C(=O)c1ccoc1
O1C=C(C=C1)C(=O)O.C(C(=O)Cl)(=O)Cl.Cl.CNOC.C(Cl)Cl>>CN(C(=O)C1=COC=C1)OC
[CH3:1][O:2][NH:3][CH3:4].O[C:5](=[O:6])[c:7]1[cH:8][cH:9][o:10][cH:11]1>>[CH3:1][O:2][N:3]([CH3:4])[C:5](=[O:6])[c:7]1[cH:8][cH:9][o:10][cH:11]1
CNOC.O=C(O)c1ccoc1
CON(C)C(=O)c1ccoc1
null
N1=CC=CC=C1.CN(C1=CC=NC=C1)C
N1=CC=CC=C1.C1(=CC=CC=C1)C
Acylation
Acylation of Nitrogen Nucleophiles by Carboxylic Acids
ac72df6259d5d7baee7abdbd4706ef4b4627f86ead9dc94f0cefcfcb37c21def
c5e4172490b2731ba9322b68af56376edadc31ce0bb9a3dfdea23a1817a852fd
c1ccoc1
O-[C;H0;D3;+0:1](=[O;D1;H0:2])-[c:3]1:[c:4]:[#8;a:5]:[c:6]:[c:7]:1.[C;D1;H3:8]-[#8:9]-[NH;D2;+0:10]-[C;D1;H3:11]>>[C;D1;H3:8]-[#8:9]-[N;H0;D3;+0:10](-[C;D1;H3:11])-[C;H0;D3;+0:1](=[O;D1;H0:2])-[c:3]1:[c:4]:[#8;a:5]:[c:6]:[c:7]:1
88.7
[{"value": 88.7, "product": "CN(C(=O)C1=COC=C1)OC", "details": "PERCENTYIELD", "is_desired": false}, {"value": 88.6, "product": "CN(C(=O)C1=COC=C1)OC", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
2
HOUR
To a solution of furan-3-carboxylic acid (36 g, 0.32 mol) in 250 mL of toluene was added 49 mL (0.385 mol) of oxalyl chloride and 1 drop of pyridine and the mixture was heated at 80°-90° C. for 1.5 h. The mixture was cooled to room temperature, N,O-dimethylhydroxylamine hydrochloride (35 g, 0.36 mol), 4-dimethylaminopy...
10.6084/m9.figshare.5104873.v1
null
Carboxylic acid.Secondary amine
Tertiary amide
null
null
c1ccoc1
HO-
N1=CC=CC=C1.CN(C1=CC=NC=C1)C.N1=CC=CC=C1.C1(=CC=CC=C1)C
null
2
CNOC.O=C(O)c1ccoc1>N1=CC=CC=C1.CN(C1=CC=NC=C1)C.N1=CC=CC=C1.C1(=CC=CC=C1)C>CON(C)C(=O)c1ccoc1
ord_dataset-c2ad1656a3ca4d08888ffb6e3f3a2742
ord-b81f6bbadd364fcabd341cb169b90406
Brc1ccoc1.CON(C)C(=O)c1ccoc1>>O=C(c1ccoc1)c1ccoc1
C(CCC)[Li].BrC1=COC=C1.CN(C(=O)C1=COC=C1)OC>>O1C=C(C=C1)C(=O)C1=COC=C1
Br[c:3]1[cH:4][cH:5][o:6][cH:7]1.CON(C)[C:2](=[O:1])[c:8]1[cH:9][cH:10][o:11][cH:12]1>>[O:1]=[C:2]([c:3]1[cH:4][cH:5][o:6][cH:7]1)[c:8]1[cH:9][cH:10][o:11][cH:12]1
Brc1ccoc1.CON(C)C(=O)c1ccoc1
O=C(c1ccoc1)c1ccoc1
null
null
CCOCC
C-C Coupling
OtherReaction
b6253f5511204f961138e67901e3464478ba474fec97457ac8b7f18ef0d3225e
7d9aa59f8ecc532475d910f9ab122332ecbb7f9444a37371b7c1bac80798d342
O=C(c1ccoc1)c1ccoc1
Br-[c;H0;D3;+0:1]1:[c:2]:[c:3]:[#8;a:4]:[c:5]:1.C-O-N(-C)-[C;H0;D3;+0:6](=[O;D1;H0:7])-[c:8]1:[c:9]:[#8;a:10]:[c:11]:[c:12]:1>>[O;D1;H0:7]=[C;H0;D3;+0:6](-[c:8]1:[c:9]:[#8;a:10]:[c:11]:[c:12]:1)-[c;H0;D3;+0:1]1:[c:2]:[c:3]:[#8;a:4]:[c:5]:1
78.4
[{"value": 78.3, "product": "O1C=C(C=C1)C(=O)C1=COC=C1", "details": "PERCENTYIELD", "is_desired": false}, {"value": 78.4, "product": "O1C=C(C=C1)C(=O)C1=COC=C1", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
-78
CELSIUS
20
MINUTE
To a solution of n-butyllithium (2.5M, 28 mL, 0.07 mol) in 150 mL of ether at -78° C. was added a solution of 3-bromofuran (10 g, 0.0628 mol) in 30 mL of ether over a 20 min period and the mixture was stirred at -78° C. for 20 min. To the above mixture was added 3-(N-methyl-N-methoxycarbamoyl)furan (9.16 g, 0.059 mol) ...
10.6084/m9.figshare.5104873.v1
null
Aromatic halide.Tertiary amide
Ketone
c1ccoc1
c1ccoc1
c1ccoc1.c1ccoc1
HBr
CCOCC
-78
0.333333
Brc1ccoc1.CON(C)C(=O)c1ccoc1>CCOCC>O=C(c1ccoc1)c1ccoc1
ord_dataset-c2ad1656a3ca4d08888ffb6e3f3a2742
ord-aa8346898c194446b65096a59802d62f
COc1ccc(CCl)cc1.c1c[nH]nn1>>COc1ccc(Cn2ccnn2)cc1
[H-].[Na+].N1N=NC=C1.COC1=CC=C(CCl)C=C1>>COC1=CC=C(CN2N=NC=C2)C=C1
Cl[CH2:7][c:6]1[cH:5][cH:4][c:3]([O:2][CH3:1])[cH:14][cH:13]1.[nH:8]1[cH:9][cH:10][n:11][n:12]1>>[CH3:1][O:2][c:3]1[cH:4][cH:5][c:6]([CH2:7][n:8]2[cH:9][cH:10][n:11][n:12]2)[cH:13][cH:14]1
COc1ccc(CCl)cc1.c1c[nH]nn1
COc1ccc(Cn2ccnn2)cc1
null
null
CN(C)C=O
Heteroatom Alkylation and Arylation
N-alkylation of secondary amines with alkyl halides
05c339ca377d2bd6d40ca68d986302f474aa669d3b7616e451ee2557764f991a
2e1e5fd9557b69cb528f6b2ffd179c67ef24ecb1a2c3994e1cdf0efe7ae19e9c
c1ccc(Cn2ccnn2)cc1
Cl-[CH2;D2;+0:1]-[c:2](:[c:3]):[c:4].[#7;a:5]1:[#7;a:6]:[nH;D2;+0:7]:[c:8]:[c:9]:1>>[c:3]:[c:2](-[CH2;D2;+0:1]-[n;H0;D3;+0:7]1:[#7;a:6]:[#7;a:5]:[c:9]:[c:8]:1):[c:4]
64.5
[{"value": 64.5, "product": "COC1=CC=C(CN2N=NC=C2)C=C1", "details": "PERCENTYIELD", "is_desired": false}, {"value": 64.3, "product": "COC1=CC=C(CN2N=NC=C2)C=C1", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
1
HOUR
To a suspension of 3.5 g (0.139 mol) of sodium hydride in 120 mL of DMF at 0° C. was added 8 g (0.115 mol) of 1,2,3-triazole in 50 mL of DMF dropwise, and the mixture was allowed to warm to room temperature and stirred for 1 h. The above mixture was cooled to 0° C., and 21.8 g (0.139 mol) of p-methoxybenzyl chloride wa...
10.6084/m9.figshare.5104873.v1
null
Primary halide
null
c1c[nH]nn1
c1c[nH]nn1
c1ccccc1.c1c[nH]nn1
HCl
CN(C)C=O
null
1
COc1ccc(CCl)cc1.c1c[nH]nn1>CN(C)C=O>COc1ccc(Cn2ccnn2)cc1
ord_dataset-c2ad1656a3ca4d08888ffb6e3f3a2742
ord-3f54e9fca67143dcba827aa0a2909574
CC(C)[Si](C(C)C)(C(C)C)n1cccc1.NC(=O)CCC(=O)NBr>>CC(C)[Si](C(C)C)(C(C)C)n1ccc(Br)c1
C(C)(C)[Si](N1C=CC=C1)(C(C)C)C(C)C.BrNC(CCC(=O)N)=O>>BrC1=CN(C=C1)[Si](C(C)C)(C(C)C)C(C)C
[CH3:1][CH:2]([CH3:3])[Si:4]([CH:5]([CH3:6])[CH3:7])([CH:8]([CH3:9])[CH3:10])[n:11]1[cH:12][cH:13][cH:14][cH:16]1.NC(=O)CCC(=O)N[Br:15]>>[CH3:1][CH:2]([CH3:3])[Si:4]([CH:5]([CH3:6])[CH3:7])([CH:8]([CH3:9])[CH3:10])[n:11]1[cH:12][cH:13][c:14]([Br:15])[cH:16]1
CC(C)[Si](C(C)C)(C(C)C)n1cccc1.NC(=O)CCC(=O)NBr
CC(C)[Si](C(C)C)(C(C)C)n1ccc(Br)c1
null
null
C1CCOC1
Functional Group Interconversion
Bromination
f3f8a432f8a8ea08a5ceb07de68b0f44caf8ff6de6fbb318e6fe4b30105676a4
f0c47cfd4d5d7957b01579ba4ffee0b3c64b05d7411e52b95a7ea89b926af55c
c1cc[nH]c1
N-C(=O)-C-C-C(=O)-N-[Br;H0;D1;+0:1].[C:2]-[#14:3](-[C:4])(-[C:5])-[#7;a:6]1:[c:7]:[c:8]:[cH;D2;+0:9]:[c:10]:1>>[Br;H0;D1;+0:1]-[c;H0;D3;+0:9]1:[c:8]:[c:7]:[#7;a:6](-[#14:3](-[C:2])(-[C:4])-[C:5]):[c:10]:1
58.6
[{"value": 58.4, "product": "BrC1=CN(C=C1)[Si](C(C)C)(C(C)C)C(C)C", "details": "PERCENTYIELD", "is_desired": false}, {"value": 58.6, "product": "BrC1=CN(C=C1)[Si](C(C)C)(C(C)C)C(C)C", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
-78
CELSIUS
3
HOUR
To a solution of 1-triisoproylsilyl-pyrrole (13.2 g, 0.059 mol) in 250 mL of THF at -78° C. was added 10.45 g (0.0587 mol) of N-bromosuccinamide (NBS), and the mixture was stirred at -78° C. for 3 h. The reaction mixture was warmed to room temperature and concentrated in vacuo, and the resulting residue in hexane was s...
10.6084/m9.figshare.5104873.v1
null
Primary amide.Secondary amide
Aromatic halide
c1cc[nH]c1
c1cc[nH]c1
c1cc[nH]c1
HO-
C1CCOC1
-78
3
CC(C)[Si](C(C)C)(C(C)C)n1cccc1.NC(=O)CCC(=O)NBr>C1CCOC1>CC(C)[Si](C(C)C)(C(C)C)n1ccc(Br)c1
ord_dataset-c2ad1656a3ca4d08888ffb6e3f3a2742
ord-a24df7fa58b844ecb0722793a52c4932
O=Cc1ccoc1>>C#CC(O)c1ccoc1
[Cl-].[NH4+].O1C=C(C=C1)C=O.C(#C)[Mg]Br>>O1C=C(C=C1)C(C#C)O
[CH:3](=[O:4])[c:5]1[cH:6][cH:7][o:8][cH:9]1>>[CH:1]#[C:2][CH:3]([OH:4])[c:5]1[cH:6][cH:7][o:8][cH:9]1
O=Cc1ccoc1
C#CC(O)c1ccoc1
null
null
C1CCOC1
Miscellaneous
OtherReaction
eceee5816c0f9c145051e60fc30c4aeafbf642f1679c2474e31812706dbe581d
ce9a178c225fe56fa06be88a01a759294be5f00e5e9f9de154a8b5b2a2cf9c70
c1ccoc1
[O;H0;D1;+0:1]=[CH;D2;+0:2]-[c:3]1:[c:4]:[c:5]:[#8;a:6]:[c:7]:1>>[C;D1;H1:8]#[C:9]-[CH;D3;+0:2](-[OH;D1;+0:1])-[c:3]1:[c:4]:[c:5]:[#8;a:6]:[c:7]:1
null
[]
null
null
1
HOUR
To 3-furaldehyde (25.0 g, 0.26 mol) in THF (250 mL) at 78° C. was added ethynylmagnesium bromide (572 mL, 0.286, 0.5M THF) at the rate of 10 mL per min. The mixture was slowly warmed to room temperature, stirred for 1 h and then poured into a cooled ammonium chloride solution. The mixture was extracted with ethyl aceta...
10.6084/m9.figshare.5104873.v1
null
Aldehyde
Secondary alcohol.Alkyne
null
null
c1ccoc1
Other
C1CCOC1
null
1
O=Cc1ccoc1>C1CCOC1>C#CC(O)c1ccoc1
ord_dataset-c2ad1656a3ca4d08888ffb6e3f3a2742
ord-491a1b04b1054004b4485eb8facf8717
C1CCOC1.CCCCCC.CCOS(=O)(=O)OCC>>C#CC(OCC)c1ccoc1
C(C)OS(=O)(=O)OCC.CCCCCC.C1CCOC1.[OH-].[Na+]>>O1C=C(C=C1)C(C#C)OCC
[CH2:7]1[CH2:8][CH2:9][O:10][CH2:11]1.CCC[CH2:3][CH2:2][CH3:1].CCOS(=O)(=O)[O:4][CH2:5][CH3:6]>>[CH:1]#[C:2][CH:3]([O:4][CH2:5][CH3:6])[c:7]1[cH:8][cH:9][o:10][cH:11]1
C1CCOC1.CCCCCC.CCOS(=O)(=O)OCC
C#CC(OCC)c1ccoc1
null
[Br-].C(CCC)[N+](CCCC)(CCCC)CCCC
null
Aromatic Heterocycle Formation
OtherReaction
3f873826f4654ad7aaf5a2c17f25114a588aa81b94e0ea75700c5f54fda569d5
f41dbc21054001785f284181f5c75e4b473563ff691cf0c69f61571efe4b4c56
c1ccoc1
C-C-C-[CH2;D2;+0:1]-[CH2;D2;+0:2]-[CH3;D1;+0:3].C-C-O-S(=O)(=O)-[O;H0;D2;+0:4]-[C:5]-[C;D1;H3:6].[CH2;D2;+0:7]1-[CH2;D2;+0:8]-[CH2;D2;+0:9]-[CH2;D2;+0:10]-[O;H0;D2;+0:11]-1>>[C;D1;H3:6]-[C:5]-[O;H0;D2;+0:4]-[CH;D3;+0:1](-[C;H0;D2;+0:2]#[CH;D1;+0:3])-[c;H0;D3;+0:8]1:[cH;D2;+0:7]:[o;H0;D2;+0:11]:[cH;D2;+0:10]:[cH;D2;+0:9...
null
[]
null
null
3
HOUR
To a mixture of 1-(3-furyl)-1-hydroxy-2-propane (20.0 g, 0.163 mol), hexane (200 mL) and THF (25 mL) was added tetrabutylammonium bromide (1.05 g, 0.0032 mol), 50% NaOH (150 mL) and then diethylsulfate (30.0g, 0.195 mol) at 0° C. The mixture was stirred for 3 h at room temperature, poured into ice, and extracted with e...
10.6084/m9.figshare.5104873.v1
null
Ether
Ether.Alkyne
C1CCOC1
c1ccoc1
c1ccoc1
HO-
[Br-].C(CCC)[N+](CCCC)(CCCC)CCCC
null
3
C1CCOC1.CCCCCC.CCOS(=O)(=O)OCC>[Br-].C(CCC)[N+](CCCC)(CCCC)CCCC>C#CC(OCC)c1ccoc1
ord_dataset-c2ad1656a3ca4d08888ffb6e3f3a2742
ord-03291b9b47684e2b99540819df771aca
CC(=O)Oc1cccc2c[n+]3ccccc3cc12>>CCCCc1c2ccccc2cc2cccc[n+]12
Cl(=O)(=O)(=O)[O-].C(C)(=O)OC1=CC=CC=2C1=CC=1C=CC=C[N+]1C2>>Cl(=O)(=O)(=O)[O-].C(CCC)C1=C2C(=CC=3C=CC=C[N+]13)C=CC=C2
O=[C:2](O[c:10]1[cH:9][cH:8][cH:7][c:6]2[cH:5][n+:18]3[c:13]([cH:12][c:11]21)[cH:14][cH:15][cH:16][cH:17]3)[CH3:1]>>[CH3:1][CH2:2][CH2:3][CH2:4][c:5]1[c:6]2[cH:7][cH:8][cH:9][cH:10][c:11]2[cH:12][c:13]2[cH:14][cH:15][cH:16][cH:17][n+:18]12
CC(=O)Oc1cccc2c[n+]3ccccc3cc12
CCCCc1c2ccccc2cc2cccc[n+]12
null
null
O
Miscellaneous
OtherReaction
99f2775fabdbc5e65bbf6f300dc24c948c9657949e71ca195b75c7b06498ea71
28fae2c895dcf8b3c21a52bf83b0739e0fc2e8531ad352ab3d887795d8ac1e21
c1ccc2c[n+]3ccccc3cc2c1
O=[C;H0;D3;+0:1](-[C;D1;H3:2])-O-[c;H0;D3;+0:3]1:[c:4]:[c:5]:[c:6]:[c:7]2:[cH;D2;+0:8]:[#7;a;+:9](:[c:10]):[c:11]:[c:12]:[c:13]:2:1>>[C;D1;H3:2]-[CH2;D2;+0:1]-[C:14]-[C:15]-[c;H0;D3;+0:8]1:[#7;a;+:9](:[c:10]):[c:11]:[c:12]:[c:13]2:[cH;D2;+0:3]:[c:4]:[c:5]:[c:6]:[c:7]:2:1
115.8
[{"value": 115.8, "product": "Cl(=O)(=O)(=O)[O-].C(CCC)C1=C2C(=CC=3C=CC=C[N+]13)C=CC=C2", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
null
null
The above 10-acetoxybenzo[b]quinolizinium perchlorate (3.3 g) was dissolved in 500 mL of water, the solution was boiled, and filtered. To the filtrate was added 100 mL of 30% sodium perchlorate solution and the mixture was chilled. The precipitated solid was isolated by filtration and dried in vacuo to afford 1.9 g of ...
10.6084/m9.figshare.5104873.v1
null
Ester
null
c1ccc2c[n+]3ccccc3cc2c1
c1ccc2c[n+]3ccccc3cc2c1
c1ccc2c[n+]3ccccc3cc2c1
null
O
null
null
CC(=O)Oc1cccc2c[n+]3ccccc3cc12>O>CCCCc1c2ccccc2cc2cccc[n+]12
ord_dataset-c2ad1656a3ca4d08888ffb6e3f3a2742
ord-6384099966cc470f9da8fd1817c1ceaf
COc1ccc(CCl)cc1.c1nc[nH]n1>>COc1ccc(Cn2cncn2)cc1
[H-].[Na+].N1N=CN=C1.COC1=CC=C(CCl)C=C1>>COC1=CC=C(CN2N=CN=C2)C=C1
Cl[CH2:7][c:6]1[cH:5][cH:4][c:3]([O:2][CH3:1])[cH:14][cH:13]1.[nH:8]1[cH:9][n:10][cH:11][n:12]1>>[CH3:1][O:2][c:3]1[cH:4][cH:5][c:6]([CH2:7][n:8]2[cH:9][n:10][cH:11][n:12]2)[cH:13][cH:14]1
COc1ccc(CCl)cc1.c1nc[nH]n1
COc1ccc(Cn2cncn2)cc1
null
null
CN(C)C=O
Heteroatom Alkylation and Arylation
N-alkylation of secondary amines with alkyl halides
9f47013937e839adceb07b7e24945feef9d8519d2c1c97fb8023b4a65c36ed06
2e1e5fd9557b69cb528f6b2ffd179c67ef24ecb1a2c3994e1cdf0efe7ae19e9c
c1ccc(Cn2cncn2)cc1
Cl-[CH2;D2;+0:1]-[c:2](:[c:3]):[c:4].[#7;a:5]1:[c:6]:[#7;a:7]:[nH;D2;+0:8]:[c:9]:1>>[c:3]:[c:2](-[CH2;D2;+0:1]-[n;H0;D3;+0:8]1:[#7;a:7]:[c:6]:[#7;a:5]:[c:9]:1):[c:4]
79.8
[{"value": 64.5, "product": "COC1=CC=C(CN2N=CN=C2)C=C1", "details": "PERCENTYIELD", "is_desired": false}, {"value": 79.8, "product": "COC1=CC=C(CN2N=CN=C2)C=C1", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
1
HOUR
To a suspension of 4 g (0.16 mol) of sodium hydride in 200 ml of DMF 20 at 0° C. was added 10 g (0.145 mol) of 1,2,4-triazole in 75 ml of DMF dropwise over a period of 30 minutes, and the mixture was allowed to warm to room temperature and stirred for 1 h. The above mixture was cooled to 0° C., 25 g (0.16 mol) of p-met...
10.6084/m9.figshare.5104873.v1
null
Primary halide
null
c1nc[nH]n1
c1nc[nH]n1
c1ccccc1.c1nc[nH]n1
HCl
CN(C)C=O
null
1
COc1ccc(CCl)cc1.c1nc[nH]n1>CN(C)C=O>COc1ccc(Cn2cncn2)cc1
ord_dataset-c2ad1656a3ca4d08888ffb6e3f3a2742
ord-6ce3346cf8114cf58cd9e465b5199dfe
Brc1ccoc1.C#CCO>>OCC#Cc1ccoc1
BrC1=COC=C1.C(C#C)O>>O1C=C(C=C1)C#CCO
Br[c:5]1[cH:6][cH:7][o:8][cH:9]1.[OH:1][CH2:2][C:3]#[CH:4]>>[OH:1][CH2:2][C:3]#[C:4][c:5]1[cH:6][cH:7][o:8][cH:9]1
Brc1ccoc1.C#CCO
OCC#Cc1ccoc1
null
[Cu]I
null
C-C Coupling
Sonogashira alkyne_aryl halide
85c427816ae28bd4dbb19650a00c34ca6489eaef6ce7658febdd08dde476e105
305eca0fd2975da49e7f69e4edfb9dc1cbce82513954bc5a73be3289e70e5f76
c1ccoc1
Br-[c;H0;D3;+0:1]1:[c:2]:[c:3]:[#8;a:4]:[c:5]:1.[C:6]-[C:7]#[CH;D1;+0:8]>>[C:6]-[C:7]#[C;H0;D2;+0:8]-[c;H0;D3;+0:1]1:[c:2]:[c:3]:[#8;a:4]:[c:5]:1
null
[]
null
null
null
null
To a mixture of 3-bromofuran (10 g, 0.068 mol) and propargyl alcohol (4.3 ml, 0.074 mol) in 200 ml of TEA was added under argon, CuI (0.26 g, 1.4 mmol) and [(C6H5)3P]2PdCl2 (1.05 g, 1.4 mmol) and the mixture was stirred at 0° C. for 2 hours and at room temperature for 72 hours. The reaction mixture was cooled, decanted...
10.6084/m9.figshare.5104873.v1
null
Aromatic halide.Alkyne
Alkyne
c1ccoc1
c1ccoc1
c1ccoc1
HBr
[Cu]I
null
null
Brc1ccoc1.C#CCO>[Cu]I>OCC#Cc1ccoc1
ord_dataset-c2ad1656a3ca4d08888ffb6e3f3a2742
ord-fda4a291a31f49d1ad96851e7bc4285b
CC(=O)OC(C)=O.OCC#Cc1ccoc1>>CC(=O)OCC#Cc1ccoc1
Cl.O1C=C(C=C1)C#CCO.C(C)(=O)OC(C)=O>>C(C)(=O)OCC#CC1=COC=C1
CC(=O)O[C:2]([CH3:1])=[O:3].[OH:4][CH2:5][C:6]#[C:7][c:8]1[cH:9][cH:10][o:11][cH:12]1>>[CH3:1][C:2](=[O:3])[O:4][CH2:5][C:6]#[C:7][c:8]1[cH:9][cH:10][o:11][cH:12]1
CC(=O)OC(C)=O.OCC#Cc1ccoc1
CC(=O)OCC#Cc1ccoc1
null
CN(C)C=1C=CN=CC1
C(Cl)Cl
Acylation
Transesterification
f81e513b7b512b10157c16426844efd8d88e34c97987c1347c6ba8a688351205
fc27d67c790d5fb520ba5d49de1490661fa5b822b714863734ce7e3029dfa84f
c1ccoc1
C-C(=O)-O-[C;H0;D3;+0:1](-[C;D1;H3:2])=[O;D1;H0:3].[#8;a:4]:[c:5]:[c:6]-[C:7]#[C:8]-[C:9]-[OH;D1;+0:10]>>[#8;a:4]:[c:5]:[c:6]-[C:7]#[C:8]-[C:9]-[O;H0;D2;+0:10]-[C;H0;D3;+0:1](-[C;D1;H3:2])=[O;D1;H0:3]
74.3
[{"value": 57.5, "product": "C(C)(=O)OCC#CC1=COC=C1", "details": "PERCENTYIELD", "is_desired": false}, {"value": 74.3, "product": "C(C)(=O)OCC#CC1=COC=C1", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
1
HOUR
A mixture of 3-(3-furyl)-2-propynyl alcohol (1.45 g, 0.0118 mol), DMAP (1 mg), TEA (2.46 ml, 0.017 mol), and acetic anhydride (1.6 ml, 0.017 mol) in 25 ml of methylene chloride was stirred for 1 hour and the mixture was poured into cold 1 N HCl solution. The mixture was extracted with ether (3×50 ml), the organic layer...
10.6084/m9.figshare.5104873.v1
null
Anhydride.Primary alcohol
Ester
null
null
c1ccoc1
HO-
CN(C)C=1C=CN=CC1.C(Cl)Cl
null
1
CC(=O)OC(C)=O.OCC#Cc1ccoc1>CN(C)C=1C=CN=CC1.C(Cl)Cl>CC(=O)OCC#Cc1ccoc1
ord_dataset-c2ad1656a3ca4d08888ffb6e3f3a2742
ord-026656cf16884d9aa661211bb77daa46
COc1ccc[n+]2cc3ccccc3cc12>>CCCCc1c2ccccc2cc2cccc[n+]12
Cl(=O)(=O)(=O)[O-].COC1=CC=C[N+]=2C=C3C(=CC12)C=CC=C3.O.Cl(=O)(=O)(=O)[O-].[Na+]>>Cl(=O)(=O)(=O)[O-].C(CCC)C1=C2C(=CC=3C=CC=C[N+]13)C=CC=C2
O([CH3:1])[c:14]1[c:13]2[cH:12][c:11]3[c:6]([cH:5][n+:18]2[cH:17][cH:16][cH:15]1)[cH:7][cH:8][cH:9][cH:10]3>>[CH3:1][CH2:2][CH2:3][CH2:4][c:5]1[c:6]2[cH:7][cH:8][cH:9][cH:10][c:11]2[cH:12][c:13]2[cH:14][cH:15][cH:16][cH:17][n+:18]12
COc1ccc[n+]2cc3ccccc3cc12
CCCCc1c2ccccc2cc2cccc[n+]12
null
null
Br
Miscellaneous
OtherReaction
ebc5d9875058df04f1ba3f72cc8cb765df1dbb969f047be989d32342f3f8bc2c
291cad8b6dfbbd2c823b5c9d45efc37a166dc3454a9f151ac48cb357f4bc155f
c1ccc2c[n+]3ccccc3cc2c1
[CH3;D1;+0:1]-O-[c;H0;D3;+0:2]1:[c:3]:[c:4]:[c:5]:[#7;a;+:6]2:[cH;D2;+0:7]:[c:8](:[c:9]):[c:10]:[c:11]:[c:12]:2:1>>[CH3;D1;+0:1]-[C:13]-[C:14]-[C:15]-[c;H0;D3;+0:7]1:[#7;a;+:6]2:[c:5]:[c:4]:[c:3]:[cH;D2;+0:2]:[c:12]:2:[c:11]:[c:10]:[c:8]:1:[c:9]
156.2
[{"value": 88.8, "product": "Cl(=O)(=O)(=O)[O-].C(CCC)C1=C2C(=CC=3C=CC=C[N+]13)C=CC=C2", "details": "PERCENTYIELD", "is_desired": false}, {"value": 156.2, "product": "Cl(=O)(=O)(=O)[O-].C(CCC)C1=C2C(=CC=3C=CC=C[N+]13)C=CC=C2", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
100
CELSIUS
null
null
A mixture of 1-methoxybenzo[b]quinolizinium perchlorate (1.4 g; 6.1 mmol) in 30 ml of 48% HBr was heated at 100° C. for 16 hour. The reaction mixture was poured into 100 ml of water and 50 ml of sodium perchlorate was added with stirring. The resulting solid was filtered and dried to afford 1.6 g (88.8%) of 1-hydroxybe...
10.6084/m9.figshare.5104873.v1
null
Ether
null
c1ccc2c[n+]3ccccc3cc2c1
c1ccc2c[n+]3ccccc3cc2c1
c1ccc2c[n+]3ccccc3cc2c1
null
Br
100
null
COc1ccc[n+]2cc3ccccc3cc12>Br>CCCCc1c2ccccc2cc2cccc[n+]12
ord_dataset-c2ad1656a3ca4d08888ffb6e3f3a2742
ord-a996c746ecb54471ac6df38e30d8d3e1
[C-]#N.c1ccc2c[n+]3ccccc3cc2c1>>CCCCc1c2ccccc2cc2cccc[n+]12
[C-]#N.[K+].[Br-].C1=CC=C[N+]=2C=C3C(=CC12)C=CC=C3.Cl(=O)(=O)(=O)[O-].[Na+]>>Cl(=O)(=O)(=O)[O-].C(CCC)C1=C2C(=CC=3C=CC=C[N+]13)C=CC=C2
N#[C-:1].[cH:5]1[c:6]2[cH:7][cH:8][cH:9][cH:10][c:11]2[cH:12][c:13]2[cH:14][cH:15][cH:16][cH:17][n+:18]12>>[CH3:1][CH2:2][CH2:3][CH2:4][c:5]1[c:6]2[cH:7][cH:8][cH:9][cH:10][c:11]2[cH:12][c:13]2[cH:14][cH:15][cH:16][cH:17][n+:18]12
[C-]#N.c1ccc2c[n+]3ccccc3cc2c1
CCCCc1c2ccccc2cc2cccc[n+]12
null
null
O.C(C)O.O
C-C Coupling
OtherReaction
3285131ee597b0d4582360034ea620b84ea2ebf0f2e14aef2ac87fe5ca21ada5
410ec9b1cc243569e4ff568c248f0b402403802e002b4018f576af3f6960507b
c1ccc2c[n+]3ccccc3cc2c1
N#[C-;H0;D1:1].[c:2]:[c:3](:[c:4]):[cH;D2;+0:5]:[#7;a;+:6](:[c:7]):[c:8]>>[CH3;D1;+0:1]-[C:9]-[C:10]-[C:11]-[c;H0;D3;+0:5](:[#7;a;+:6](:[c:7]):[c:8]):[c:3](:[c:2]):[c:4]
null
[]
null
null
null
null
A solution of KCN (3g, 0.046 mol) in a minimum of water was added to a solution of benzo[b]quinolizinium bromide (10 g; 0.0385 mol) in 200 ml water. The resulting solid was extracted with an equal volume of methylene chloride. The above organic layer was heated and a solution of bromine (6.4 g) in methylene chloride wa...
10.6084/m9.figshare.5104873.v1
null
null
null
c1ccc2c[n+]3ccccc3cc2c1
c1ccc2c[n+]3ccccc3cc2c1
c1ccc2c[n+]3ccccc3cc2c1
null
O.C(C)O.O
null
null
[C-]#N.c1ccc2c[n+]3ccccc3cc2c1>O.C(C)O.O>CCCCc1c2ccccc2cc2cccc[n+]12
ord_dataset-c2ad1656a3ca4d08888ffb6e3f3a2742
ord-8b317ef19c874f57b5a89bc35fd2943f
CCOC(=O)C(C)(C)CC(=O)O.O=S(Cl)Cl>>CCOC(=O)C(C)(C)CC(=O)Cl
C(C)OC(=O)C(CC(=O)O)(C)C.S(=O)(Cl)Cl>>C(C)OC(=O)C(CC(=O)Cl)(C)C
O[C:10]([CH2:9][C:6]([C:4]([O:3][CH2:2][CH3:1])=[O:5])([CH3:7])[CH3:8])=[O:11].O=S(Cl)[Cl:12]>>[CH3:1][CH2:2][O:3][C:4](=[O:5])[C:6]([CH3:7])([CH3:8])[CH2:9][C:10](=[O:11])[Cl:12]
CCOC(=O)C(C)(C)CC(=O)O.O=S(Cl)Cl
CCOC(=O)C(C)(C)CC(=O)Cl
null
null
null
Functional Group Interconversion
Alcohol to chloride_SOCl2
c301c14a9dcd0670d52e8b77396cbe7fd8edeedd757bc43f4162ade1fc52fc93
787f545db5dc0b29dde55b5fbed7db8625b8055f49327f97ed4d83cc47c3af1d
null
Cl-S(=O)-[Cl;H0;D1;+0:1].O-[C;H0;D3;+0:2](=[O;D1;H0:3])-[C:4]-[C:5]-[C:6](-[#8:7])=[O;D1;H0:8]>>[#8:7]-[C:6](=[O;D1;H0:8])-[C:5]-[C:4]-[C;H0;D3;+0:2](-[Cl;H0;D1;+0:1])=[O;D1;H0:3]
null
[]
null
null
20
HOUR
A mixture of 3-ethoxycarbonyl-3,3-dimethylpropionic acid (1 g) and 3 ml of thionyl chloride was stirred at room temperature for 20 hours. The excess thionyl chloride was removed in vacuo to afford 1,1 g of 3-ethoxycarbonyl-3,3-dimethylpropionyl chloride. Conditions: See reaction.notes.procedure_details. Workup: The exc...
10.6084/m9.figshare.5104873.v1
null
Carboxylic acid
Acyl halide
null
null
null
HCl
null
null
20
CCOC(=O)C(C)(C)CC(=O)O.O=S(Cl)Cl>>CCOC(=O)C(C)(C)CC(=O)Cl
ord_dataset-c2ad1656a3ca4d08888ffb6e3f3a2742
ord-a06452d4ab3e4671a5bd9c4e53382385
CO.O=C(O)c1nccc2ccccc12>>COC(=O)c1nccc2ccccc12
C1(=NC=CC2=CC=CC=C12)C(=O)O.CO>>COC(=O)C1=NC=CC2=CC=CC=C12
[CH3:1][OH:2].O[C:3](=[O:4])[c:5]1[n:6][cH:7][cH:8][c:9]2[cH:10][cH:11][cH:12][cH:13][c:14]12>>[CH3:1][O:2][C:3](=[O:4])[c:5]1[n:6][cH:7][cH:8][c:9]2[cH:10][cH:11][cH:12][cH:13][c:14]12
CO.O=C(O)c1nccc2ccccc12
COC(=O)c1nccc2ccccc12
null
null
null
Protection
Esterification of Carboxylic Acids
9cecdbd189c6f9c3648521d17154d013842a5498de4e76e65efb1d842973340b
af0b8064f2e82ebe66c4c29d2391785ac1b993104265ccdc4d67ca79e36fa3c8
c1ccc2cnccc2c1
O-[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]
50
[{"value": 50.0, "product": "COC(=O)C1=NC=CC2=CC=CC=C12", "details": "PERCENTYIELD", "is_desired": false}]
null
null
null
null
A mixture of 1-isoquinolinecarboxylic acid (25 g.0.14 mol), 25 g of AMBERLYST®-15 (H+), and 300 ml of methanol was refluxed for 3 days. The reaction mixture was cooled, filtered, and the filtrate was concentrated in vacuo to afford 13.6 g (50%) of 1-isoquinolinecarboxylic acid methyl ester. Conditions: See reaction.not...
10.6084/m9.figshare.5104873.v1
null
Carboxylic acid.Methanol
Ester
null
null
c1ccc2cnccc2c1
HO-
null
null
null
CO.O=C(O)c1nccc2ccccc12>>COC(=O)c1nccc2ccccc12
ord_dataset-c2ad1656a3ca4d08888ffb6e3f3a2742
ord-1ad88c5ca76c4d329b8bf085bdb1345f
COC(=O)c1nccc2ccccc12>>O=Cc1nccc2ccccc12
COC(=O)C1=NC=CC2=CC=CC=C12.[H-].[H-].[H-].[H-].[Li+].[Al+3]>>C1(=NC=CC2=CC=CC=C12)C=O
CO[C:2](=[O:1])[c:3]1[n:4][cH:5][cH:6][c:7]2[cH:8][cH:9][cH:10][cH:11][c:12]12>>[O:1]=[CH:2][c:3]1[n:4][cH:5][cH:6][c:7]2[cH:8][cH:9][cH:10][cH:11][c:12]12
COC(=O)c1nccc2ccccc12
O=Cc1nccc2ccccc12
null
null
C1CCOC1
Reduction
OtherReaction
ec1c6c64dd9be73981e5a6c952ab740869d298b20e87e097e88e1179cc5bc6dc
33ddc7b9457742ba0a376f08a972e4f33779267f6f1fe15e3be786427ae9f4ec
c1ccc2cnccc2c1
C-O-[C;H0;D3;+0:1](=[O;D1;H0:2])-[c:3](:[c:4]):[#7;a:5]:[c:6]>>[O;D1;H0:2]=[CH;D2;+0:1]-[c:3](:[c:4]):[#7;a:5]:[c:6]
64
[{"value": 64.0, "product": "C1(=NC=CC2=CC=CC=C12)C=O", "details": "PERCENTYIELD", "is_desired": false}, {"value": 63.6, "product": "C1(=NC=CC2=CC=CC=C12)C=O", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
null
null
1-Isoquinolinecarboxaldehyde (7.3 g, 64 %) was prepared from 1-isoquinolinecarboxylic acid methyl ester (13.6 g, 0.073 mol) and 1M LAH (36.6 ml in THF) in 300 ml of dry THF (J. Org. Chem., vol 28, p 1898, 1963) to afford 7.3 g (64%) of 1-isoquinolinecarboxaldehyde. Conditions: See reaction.notes.procedure_details.
10.6084/m9.figshare.5104873.v1
null
Ester
Aldehyde
null
null
c1ccc2cnccc2c1
HO-
C1CCOC1
null
null
COC(=O)c1nccc2ccccc12>C1CCOC1>O=Cc1nccc2ccccc12
ord_dataset-c2ad1656a3ca4d08888ffb6e3f3a2742
ord-e72d322566874e22b4fe3d4c4cb4dd39
O=Cc1nccc2ccccc12.OCCO>>c1ccc2c(C3OCCO3)nccc2c1
C1(=NC=CC2=CC=CC=C12)C=O.C(CO)O.C1(=CC=C(C=C1)S(=O)(=O)O)C>>O1C(OCC1)C1=NC=CC2=CC=CC=C12
[cH:1]1[cH:2][cH:3][c:4]2[c:5]([CH:6]=[O:7])[n:11][cH:12][cH:13][c:14]2[cH:15]1.O[CH2:8][CH2:9][OH:10]>>[cH:1]1[cH:2][cH:3][c:4]2[c:5]([CH:6]3[O:7][CH2:8][CH2:9][O:10]3)[n:11][cH:12][cH:13][c:14]2[cH:15]1
O=Cc1nccc2ccccc12.OCCO
c1ccc2c(C3OCCO3)nccc2c1
null
null
C1(=CC=CC=C1)C
Heteroatom Alkylation and Arylation
OtherReaction
fe0fbb45a87f24c1e456c6b4e41101562cd8f0af3ec376bb6115e7c1555d997b
7ac65b5a5f576337ce8e86e0130eb9b4757ca21b2419a0e82bbdfd5def30ee73
c1ccc2c(C3OCCO3)nccc2c1
O-[CH2;D2;+0:1]-[C:2]-[OH;D1;+0:3].[O;H0;D1;+0:4]=[CH;D2;+0:5]-[c:6](:[c:7]):[#7;a:8]:[c:9]>>[c:9]:[#7;a:8]:[c:6](-[CH;D3;+0:5]1-[O;H0;D2;+0:3]-[C:2]-[CH2;D2;+0:1]-[O;H0;D2;+0:4]-1):[c:7]
100.5
[{"value": 100.5, "product": "O1C(OCC1)C1=NC=CC2=CC=CC=C12", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
null
null
A mixture of 1-isoquinolinecarboxaldehyde (7.2 g, 46 mmol), 5.7 g (92 mmol) of ethylene glycol, 200 ml of toluene and 2.3 g (12 mmol) of p-toluenesulfonic acid under argon in a 3 neck-flask equipped with a Dean-Stark Trap was refluxed for 6 h separating the water. The mixture was cooled to room temperature, and poured ...
10.6084/m9.figshare.5104873.v1
null
Aldehyde.Primary alcohol.Primary alcohol
Ether.Ether
null
C1COCO1
C1COCO1.c1ccc2cnccc2c1
HO-
C1(=CC=CC=C1)C
null
null
O=Cc1nccc2ccccc12.OCCO>C1(=CC=CC=C1)C>c1ccc2c(C3OCCO3)nccc2c1
ord_dataset-c2ad1656a3ca4d08888ffb6e3f3a2742
ord-d817cdb898dc4c4791fd3470bd46b871
Brc1c(COC2CCCCO2)cccc1COC1CCCCO1.O=Cc1ccccn1>>OC(c1ccccn1)c1c(COC2CCCCO2)cccc1COC1CCCCO1
C1=CC=NC(=C1)C=O.CN(C)CCN(C)C.O1C(CCCC1)OCC1=C(C(=CC=C1)COC1OCCCC1)Br.[Li]CCCC>>N1=C(C=CC=C1)C(O)C1=C(C=CC=C1COC1OCCCC1)COC1OCCCC1
Br[c:9]1[c:10]([CH2:11][O:12][CH:13]2[CH2:14][CH2:15][CH2:16][CH2:17][O:18]2)[cH:19][cH:20][cH:21][c:22]1[CH2:23][O:24][CH:25]1[CH2:26][CH2:27][CH2:28][CH2:29][O:30]1.[O:1]=[CH:2][c:3]1[cH:4][cH:5][cH:6][cH:7][n:8]1>>[OH:1][CH:2]([c:3]1[cH:4][cH:5][cH:6][cH:7][n:8]1)[c:9]1[c:10]([CH2:11][O:12][CH:13]2[CH2:14][CH2:15][C...
Brc1c(COC2CCCCO2)cccc1COC1CCCCO1.O=Cc1ccccn1
OC(c1ccccn1)c1c(COC2CCCCO2)cccc1COC1CCCCO1
null
null
CCOCC
C-C Coupling
Grignard_alcohol
0c8bc0f755f4d9a2cfce93ae43a9a9a531fa8ad86ff120aed0a18ba03c84e4d7
1c0bd0afc1d5e370e3c8193faf738f03752295e40fa0eb99c756011e9a4be26b
c1ccc(Cc2c(COC3CCCCO3)cccc2COC2CCCCO2)nc1
Br-[c;H0;D3;+0:1](:[c:2](-[C:3]):[c:4]):[c:5](-[C:6]):[c:7].[O;H0;D1;+0:8]=[CH;D2;+0:9]-[c:10](:[c:11]):[#7;a:12]:[c:13]>>[C:3]-[c:2](:[c:4]):[c;H0;D3;+0:1](-[CH;D3;+0:9](-[OH;D1;+0:8])-[c:10](:[c:11]):[#7;a:12]:[c:13]):[c:5](-[C:6]):[c:7]
73
[{"value": 73.0, "product": "N1=C(C=CC=C1)C(O)C1=C(C=CC=C1COC1OCCCC1)COC1OCCCC1", "details": "PERCENTYIELD", "is_desired": false}, {"value": 72.6, "product": "N1=C(C=CC=C1)C(O)C1=C(C=CC=C1COC1OCCCC1)COC1OCCCC1", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
1.5
HOUR
To a solution of 2,6-di(tetrahydro-2H-2-pyranyloxymethyl)-phenyl bromide (15.5 g, 39 mmol) in ether at -30° C. was added n-BuLi (2.5M, 16.4 ml, 41 mmol) and the mixture was allowed to warm to room temperature and stirred for 1.5 hours. The mixture was cooled to 0° C., and TMEDA (4.56 g, 37 mmol) was added, and the resu...
10.6084/m9.figshare.5104873.v1
null
Aromatic halide.Aldehyde
Secondary alcohol
c1ccccc1
c1ccccc1
c1ccncc1.C1CCOCC1.c1ccccc1.C1CCOCC1
Br-
CCOCC
null
1.5
Brc1c(COC2CCCCO2)cccc1COC1CCCCO1.O=Cc1ccccn1>CCOCC>OC(c1ccccn1)c1c(COC2CCCCO2)cccc1COC1CCCCO1
ord_dataset-c2ad1656a3ca4d08888ffb6e3f3a2742
ord-387c94b08c6e47d38076a85d28b4897a
OC(c1ccccn1)c1c(COC2CCCCO2)cccc1COC1CCCCO1>>OCc1cccc(CO)c1C(O)c1ccccn1
N1=C(C=CC=C1)C(O)C1=C(C=CC=C1COC1OCCCC1)COC1OCCCC1>>N1=C(C=CC=C1)C(O)C1=C(C=CC=C1CO)CO
C1CCC([O:1][CH2:2][c:3]2[cH:4][cH:5][cH:6][c:7]([CH2:8][O:9]C3CCCCO3)[c:10]2[CH:11]([OH:12])[c:13]2[cH:14][cH:15][cH:16][cH:17][n:18]2)OC1>>[OH:1][CH2:2][c:3]1[cH:4][cH:5][cH:6][c:7]([CH2:8][OH:9])[c:10]1[CH:11]([OH:12])[c:13]1[cH:14][cH:15][cH:16][cH:17][n:18]1
OC(c1ccccn1)c1c(COC2CCCCO2)cccc1COC1CCCCO1
OCc1cccc(CO)c1C(O)c1ccccn1
null
null
C(C)(=O)O.C1CCOC1.O
Reduction
OtherReaction
d55354815d6f7a64ea8a1f850bd51ba9e291163ec84af74464989e21ec3f9d66
12369fed9e6b5d76484a682f4ff2019230b866ab4384925c750ef80e8cdac252
c1ccc(Cc2ccccn2)cc1
[c:1]-[C:2]-[O;H0;D2;+0:3]-C1-C-C-C-C-O-1.[c:4]-[C:5]-[O;H0;D2;+0:6]-C1-C-C-C-C-O-1>>[OH;D1;+0:3]-[C:2]-[c:1].[OH;D1;+0:6]-[C:5]-[c:4]
43.8
[{"value": 43.8, "product": "N1=C(C=CC=C1)C(O)C1=C(C=CC=C1CO)CO", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
null
null
A solution of 1 g (2.42 mmol) of 1-(2-pyridyl)-1-[2,6-di(tetrahydro-2H-2-pyranyloxymethyl)phenyl]-methanol in 14 ml of acetic acid/THF/water (4:2:1) was heated at 100° C. under nitrogen for 6 hours. The mixture was concentrated in vacuo, the residue was dissolved in ethyl acetate and concentrated in vacuo. The residual...
10.6084/m9.figshare.5104873.v1
null
Ether.Ether.Ether.Ether
Primary alcohol.Primary alcohol
C1CCOCC1.C1CCOCC1
null
c1ccccc1.c1ccncc1
HO-
C(C)(=O)O.C1CCOC1.O
null
null
OC(c1ccccn1)c1c(COC2CCCCO2)cccc1COC1CCCCO1>C(C)(=O)O.C1CCOC1.O>OCc1cccc(CO)c1C(O)c1ccccn1
ord_dataset-c2ad1656a3ca4d08888ffb6e3f3a2742
ord-e24046e8b4f849598eae1352c2006e5b
OCc1cccc(CO)c1C(O)c1ccccn1>>CCCCc1c2ccccc2cc2cccc[n+]12
N1=C(C=CC=C1)C(O)C1=C(C=CC=C1CO)CO.Cl(=O)(=O)(=O)[O-].[Na+]>>Cl(=O)(=O)(=O)[O-].C(CCC)C1=C2C(=CC=3C=CC=C[N+]13)C=CC=C2
O[CH2:1][c:7]1[c:6]([CH:12](O)[c:13]2[cH:14][cH:15][cH:16][cH:17][n:18]2)[c:11]([CH2:3]O)[cH:10][cH:9][cH:8]1>>[CH3:1][CH2:2][CH2:3][CH2:4][c:5]1[c:6]2[cH:7][cH:8][cH:9][cH:10][c:11]2[cH:12][c:13]2[cH:14][cH:15][cH:16][cH:17][n+:18]12
OCc1cccc(CO)c1C(O)c1ccccn1
CCCCc1c2ccccc2cc2cccc[n+]12
null
null
O=P(Cl)(Cl)Cl
Aromatic Heterocycle Formation
OtherReaction
de93c16343d29e4aa02c02125e95aa1dd3391dde60191777f8eedf76e75d8202
6c98e5a80f1c9efa595117e788b54eeaca48c0fac195062be92a50c6d4ed9ee5
c1ccc2c[n+]3ccccc3cc2c1
O-[CH2;D2;+0:1]-[c;H0;D3;+0:2]1:[c:3]:[c:4]:[c:5]:[c;H0;D3;+0:6](-[CH2;D2;+0:7]-O):[c;H0;D3;+0:8]:1-[CH;D3;+0:9](-O)-[c:10](:[c:11]):[n;H0;D2;+0:12]:[c:13]:[c:14]>>[CH3;D1;+0:1]-[C:15]-[CH2;D2;+0:7]-[C:16]-[c:17]1:[c;H0;D3;+0:8]2:[cH;D2;+0:2]:[c:3]:[c:4]:[c:5]:[c;H0;D3;+0:6]:2:[cH;D2;+0:9]:[c:10](:[c:11]):[n+;H0;D3:12]...
null
[]
null
null
null
null
A mixture of 0.6 g (2.5 mmol) of 1-(2-pyridyl)-1-[2,6-di(hydroxymethyl)-phenyl]methanol and 10 ml of POCl3 was refluxed with 30 stirring for 4 hours. The mixture was cooled, poured onto ice, stirred and treated with a 20% sodium perchlorate solution. The resulting mixture was filtered, the resulting solid was washed wi...
10.6084/m9.figshare.5104873.v1
null
Primary alcohol.Primary alcohol.Secondary alcohol
null
c1ccccc1.c1ccncc1
c1ccc2c[n+]3ccccc3cc2c1
c1ccc2c[n+]3ccccc3cc2c1
null
O=P(Cl)(Cl)Cl
null
null
OCc1cccc(CO)c1C(O)c1ccccn1>O=P(Cl)(Cl)Cl>CCCCc1c2ccccc2cc2cccc[n+]12
ord_dataset-c2ad1656a3ca4d08888ffb6e3f3a2742
ord-fee2b76fa72f4ff9b4a4d85aa6743379
COC(=O)c1ccc(C)c(N)c1>>COC(=O)c1ccc2cn[nH]c2c1
COC(C1=CC(=C(C=C1)C)N)=O.N(=O)[O-].[Na+]>>N1N=CC2=CC=C(C=C12)C(=O)OC
[CH3:1][O:2][C:3](=[O:4])[c:5]1[cH:6][cH:7][c:8]([CH3:9])[c:12]([NH2:11])[cH:13]1>>[CH3:1][O:2][C:3](=[O:4])[c:5]1[cH:6][cH:7][c:8]2[cH:9][n:10][nH:11][c:12]2[cH:13]1
COC(=O)c1ccc(C)c(N)c1
COC(=O)c1ccc2cn[nH]c2c1
null
null
O.C(C)(=O)O
Aromatic Heterocycle Formation
OtherReaction
9194288567782b9a53b0fcc5af5659b26356b37141f27aaae557b9a5c0e3b9e0
0c2e6cfe0bdb8f8cd78303a7637b3ef339f807f5bc27c4a22ad516ce20b37476
c1ccc2[nH]ncc2c1
[CH3;D1;+0:1]-[c:2](:[c:3]):[c:4](-[NH2;D1;+0:5]):[c:6]>>[c:6]:[c:4]1:[nH;D2;+0:5]:[#7;a:7]:[cH;D2;+0:1]:[c:2]:1:[c:3]
71.9
[{"value": 71.6, "product": "N1N=CC2=CC=C(C=C12)C(=O)OC", "details": "PERCENTYIELD", "is_desired": false}, {"value": 71.9, "product": "N1N=CC2=CC=C(C=C12)C(=O)OC", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
4
HOUR
To a solution of 3-amino-4-methylbenzoic acid methyl ester (25 g, 0.15 mol) in 1 L of acetic acid cooled to 0° C. was added a solution of NaNO2 (12.5 g, 0.182 mol) in 50 ml of water and the mixture was warmed to room temperature with stirring over 4 hours. The solution was concentrated in vacuo, the residue was tritura...
10.6084/m9.figshare.5104873.v1
null
Primary amine
null
c1ccccc1
c1ccc2n[nH]cc2c1
c1ccc2n[nH]cc2c1
Other
O.C(C)(=O)O
null
4
COC(=O)c1ccc(C)c(N)c1>O.C(C)(=O)O>COC(=O)c1ccc2cn[nH]c2c1
ord_dataset-c2ad1656a3ca4d08888ffb6e3f3a2742
ord-0aea872a6936492d87a04dfedfb85e49
CI.Cc1ccc(Cl)c(O)c1>>COc1cc(C)ccc1Cl
OC=1C=C(C=CC1Cl)C.C([O-])([O-])=O.[K+].[K+].CI>>COC=1C=C(C=CC1Cl)C
I[CH3:1].[OH:2][c:3]1[cH:4][c:5]([CH3:6])[cH:7][cH:8][c:9]1[Cl:10]>>[CH3:1][O:2][c:3]1[cH:4][c:5]([CH3:6])[cH:7][cH:8][c:9]1[Cl:10]
CI.Cc1ccc(Cl)c(O)c1
COc1cc(C)ccc1Cl
null
null
CC(=O)C
Heteroatom Alkylation and Arylation
Williamson Ether Synthesis
b8b041187bac58376aae824630608e7deb49a01db3d652291f8b379c10d4e434
0f0966e3597a58033417ecee71659f4d0c082f95d46b1e52c95541e6e4a59086
c1ccccc1
I-[CH3;D1;+0:1].[OH;D1;+0:2]-[c:3](:[c:4]):[c:5]>>[CH3;D1;+0:1]-[O;H0;D2;+0:2]-[c:3](:[c:4]):[c:5]
93.4
[{"value": 93.4, "product": "COC=1C=C(C=CC1Cl)C", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
16
HOUR
To a solution of 3-hydroxy-4-chlorotoluene (25 g, 0.175 mol) in 400 ml of acetone was added 30.11 g (0.22 mol) of milled potassium carbonate and 31.22 g (0.22 mol) of methyl iodide, and the mixture was refluxed with stirring for 16 hours. The mixture was cooled, filtered, and the filtrate was concentrated in vacuo. The...
10.6084/m9.figshare.5104873.v1
null
Aromatic alcohol
Ether
null
null
c1ccccc1
HI
CC(=O)C
null
16
CI.Cc1ccc(Cl)c(O)c1>CC(=O)C>COc1cc(C)ccc1Cl
ord_dataset-c2ad1656a3ca4d08888ffb6e3f3a2742
ord-2be1e6306c5d4e08a0d4bf6dc738737d
COc1cc(C(=O)O)ccc1Cl>>COc1cc(CO)ccc1Cl
B.C1CCOC1.COC=1C=C(C(=O)O)C=CC1Cl>>COC=1C=C(C=CC1Cl)CO
O=[C:6]([c:5]1[cH:4][c:3]([O:2][CH3:1])[c:10]([Cl:11])[cH:9][cH:8]1)[OH:7]>>[CH3:1][O:2][c:3]1[cH:4][c:5]([CH2:6][OH:7])[cH:8][cH:9][c:10]1[Cl:11]
COc1cc(C(=O)O)ccc1Cl
COc1cc(CO)ccc1Cl
null
null
C1CCOC1
Reduction
Reduction of carboxylic acid to primary alcohol
0db83a5ebe1e318b78b55461cf7eb8f7c004eef0f9e3b6666d3df4c96b5f665e
93b4621647b04d2ad2f2825215b1567f171ba61fe10d136b5db6ea0470aa4932
c1ccccc1
O=[C;H0;D3;+0:1](-[O;D1;H1:2])-[c:3](:[c:4]):[c:5]>>[O;D1;H1:2]-[CH2;D2;+0:1]-[c:3](:[c:4]):[c:5]
91.1
[{"value": 90.0, "product": "COC=1C=C(C=CC1Cl)CO", "details": "PERCENTYIELD", "is_desired": false}, {"value": 91.1, "product": "COC=1C=C(C=CC1Cl)CO", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
3
HOUR
To 30.6 ml of BH3.THF was added a solution of 3-methoxy-4-chlorobenzoic acid (35 g, 0.187 mol) in 450 ml of THF, and the mixture was refluxed with stirring under argon for 3 hours. The mixture was quenched 25 with THF/water (1:1,300 ml), concentrated in vacuo, and the residue was partitioned between methylene chloride/...
10.6084/m9.figshare.5104873.v1
null
Carboxylic acid
Primary alcohol
null
null
c1ccccc1
Other
C1CCOC1
null
3
COc1cc(C(=O)O)ccc1Cl>C1CCOC1>COc1cc(CO)ccc1Cl
ord_dataset-c2ad1656a3ca4d08888ffb6e3f3a2742
ord-424594ac1c044b53938437c9aaf9f4c4
COc1c(Cl)ccc2c[n+]3ccccc3cc12>>CCCCc1c2ccccc2cc2cccc[n+]12
Cl(=O)(=O)(=O)[O-].ClC=1C=CC=2C(=CC=3C=CC=C[N+]3C2)C1OC>>Cl(=O)(=O)(=O)[O-].C(CCC)C1=C2C(=CC=3C=CC=C[N+]13)C=CC=C2
Cl[c:9]1[c:2](O[CH3:1])[c:11]2[c:6]([cH:5][n+:18]3[c:13]([cH:12]2)[cH:14][cH:15][cH:16][cH:17]3)[cH:7][cH:8]1>>[CH3:1][CH2:2][CH2:3][CH2:4][c:5]1[c:6]2[cH:7][cH:8][cH:9][cH:10][c:11]2[cH:12][c:13]2[cH:14][cH:15][cH:16][cH:17][n+:18]12
COc1c(Cl)ccc2c[n+]3ccccc3cc12
CCCCc1c2ccccc2cc2cccc[n+]12
null
null
Br
Miscellaneous
OtherReaction
3177d18575f824db6a18db7ccac580de1b41fb8334f450736d0cd46e792b9b34
80083ded544d02db894571ce654dd57555ca45a58f858fdf0ed3a262453c36e3
c1ccc2c[n+]3ccccc3cc2c1
Cl-[c;H0;D3;+0:1]1:[c:2]:[c:3]:[c:4]2:[cH;D2;+0:5]:[#7;a;+:6](:[c:7]):[c:8](:[c:9]):[c:10]:[c;H0;D3;+0:11]:2:[c;H0;D3;+0:12]:1-O-[CH3;D1;+0:13]>>[CH3;D1;+0:13]-[CH2;D2;+0:12]-[C:14]-[C:15]-[c;H0;D3;+0:5]1:[#7;a;+:6](:[c:7]):[c:8](:[c:9]):[c:10]:[c;H0;D3;+0:11]2:[c:16]:[cH;D2;+0:1]:[c:2]:[c:3]:[c:4]:2:1
152.6
[{"value": 79.0, "product": "Cl(=O)(=O)(=O)[O-].C(CCC)C1=C2C(=CC=3C=CC=C[N+]13)C=CC=C2", "details": "PERCENTYIELD", "is_desired": false}, {"value": 152.6, "product": "Cl(=O)(=O)(=O)[O-].C(CCC)C1=C2C(=CC=3C=CC=C[N+]13)C=CC=C2", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
18
HOUR
A reaction mixture containing 9-chloro-10-methoxybenzo[b]quinolizinium perchlorate (5 g; 14.83 mmol) and 48% HBr (50 ml) was refluxed with stirring for 18 hours. The mixture was concentrated in vacuo, the residue was redissolved in water, filtered, and the filtrate was treated with a sodium perchlorate solution with st...
10.6084/m9.figshare.5104873.v1
null
Aromatic halide.Ether
null
c1ccc2c[n+]3ccccc3cc2c1
c1ccc2c[n+]3ccccc3cc2c1
c1ccc2c[n+]3ccccc3cc2c1
null
Br
null
18
COc1c(Cl)ccc2c[n+]3ccccc3cc12>Br>CCCCc1c2ccccc2cc2cccc[n+]12
ord_dataset-c2ad1656a3ca4d08888ffb6e3f3a2742
ord-d5f647c0f6554e4d83d12e046e00e776
Oc1cc2cc3cccc[n+]3cc2cc1Cl>>c1cc[n+]2ccccc2c1
Cl(=O)(=O)(=O)[O-].ClC1=CC=2C(=CC=3C=CC=C[N+]3C2)C=C1O.O1C=C(C=C1)C(=C)C1=COC=C1>>Cl(=O)(=O)(=O)[O-].C1=CC=C[N+]2=CC=CC=C12
Oc1c[c:12]2[c:11](cc1Cl)[cH:10][n+:9]1[cH:8][cH:7][cH:6][cH:15][c:14]1[cH:13]2>>[cH:6]1[cH:7][cH:8][n+:9]2[cH:10][cH:11][cH:12][cH:13][c:14]2[cH:15]1
Oc1cc2cc3cccc[n+]3cc2cc1Cl
c1cc[n+]2ccccc2c1
null
null
C(C)#N
Reduction
OtherReaction
4a490ae2d40c8a22c4fbd0dfcd99c73ac62674f1773cc3df9de17c12d26c6f71
00acf62c1ee6c127a512fc4aef1d1ace4643d23c07024023ca84c70c1c95b724
c1cc[n+]2ccccc2c1
Cl-c1:c:[c;H0;D3;+0:1]2:[c:2]:[#7;a;+:3](:[c:4]):[c:5](:[c:6]):[c:7]:[c;H0;D3;+0:8]:2:c:c:1-O>>[c:6]:[c:5]1:[c:7]:[cH;D2;+0:8]:[cH;D2;+0:1]:[c:2]:[#7;a;+:3]:1:[c:4]
null
[]
null
null
6
HOUR
A reaction mixture containing 8-chloro-9-hydroxybenzo[b]quinolizinium perchlorate (3.3 g; 10 mmol) and 1,1-di(3-furyl)ethylene (1.76 g, 11 mmol) in 50 ml of acetonitrile was allowed to reflux under nitrogen with stirring for 6 hours. The reaction mixture was concentrated in vacuo and the residue was crystallized from m...
10.6084/m9.figshare.5104873.v1
null
Aromatic halide.Aromatic alcohol
null
c1ccc2c[n+]3ccccc3cc2c1
c1cc[n+]2ccccc2c1
c1cc[n+]2ccccc2c1
HCl
C(C)#N
null
6
Oc1cc2cc3cccc[n+]3cc2cc1Cl>C(C)#N>c1cc[n+]2ccccc2c1
ord_dataset-c2ad1656a3ca4d08888ffb6e3f3a2742
ord-1864db37366949a8ae45eeee9714f568
COC(=O)c1cc2ccccc2cn1>>O=Cc1cc2ccccc2cn1
COC(=O)C=1N=CC2=CC=CC=C2C1.[H-].[H-].[H-].[H-].[Li+].[Al+3]>>C1=NC(=CC2=CC=CC=C12)C=O
CO[C:2](=[O:1])[c:3]1[cH:4][c:5]2[cH:6][cH:7][cH:8][cH:9][c:10]2[cH:11][n:12]1>>[O:1]=[CH:2][c:3]1[cH:4][c:5]2[cH:6][cH:7][cH:8][cH:9][c:10]2[cH:11][n:12]1
COC(=O)c1cc2ccccc2cn1
O=Cc1cc2ccccc2cn1
null
null
C1CCOC1
Reduction
OtherReaction
ec1c6c64dd9be73981e5a6c952ab740869d298b20e87e097e88e1179cc5bc6dc
33ddc7b9457742ba0a376f08a972e4f33779267f6f1fe15e3be786427ae9f4ec
c1ccc2cnccc2c1
C-O-[C;H0;D3;+0:1](=[O;D1;H0:2])-[c:3](:[c:4]):[#7;a:5]:[c:6]>>[O;D1;H0:2]=[CH;D2;+0:1]-[c:3](:[c:4]):[#7;a:5]:[c:6]
85.7
[{"value": 84.0, "product": "C1=NC(=CC2=CC=CC=C12)C=O", "details": "PERCENTYIELD", "is_desired": false}, {"value": 85.7, "product": "C1=NC(=CC2=CC=CC=C12)C=O", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
null
null
3-Isoquinolinecarboxaldehyde (7 g, 84%) was prepared by reduction of 3-isoquinolinecarboxylic acid methyl ester (10 g, 52 mmol) with 1M LAH (27 ml in THF,27 mmol) in 300 ml of dry THF at -78° C. for 30 minutes. The mixture was quenched with 7 ml of acetic acid, concentrated in vacuo, and the residue was purified by sil...
10.6084/m9.figshare.5104873.v1
null
Ester
Aldehyde
null
null
c1ccc2cnccc2c1
HO-
C1CCOC1
null
null
COC(=O)c1cc2ccccc2cn1>C1CCOC1>O=Cc1cc2ccccc2cn1
ord_dataset-c2ad1656a3ca4d08888ffb6e3f3a2742
ord-ba96baec63e2477e9126cc3d3a5c07f5
O=Cc1cc2ccccc2cn1.OCCO>>c1ccc2cc(C3OCCO3)ncc2c1
C1=NC(=CC2=CC=CC=C12)C=O.C(CO)O.C1(=CC=C(C=C1)S(=O)(=O)O)C>>O1C(OCC1)C=1N=CC2=CC=CC=C2C1
[cH:1]1[cH:2][cH:3][c:4]2[cH:5][c:6]([CH:7]=[O:8])[n:12][cH:13][c:14]2[cH:15]1.O[CH2:9][CH2:10][OH:11]>>[cH:1]1[cH:2][cH:3][c:4]2[cH:5][c:6]([CH:7]3[O:8][CH2:9][CH2:10][O:11]3)[n:12][cH:13][c:14]2[cH:15]1
O=Cc1cc2ccccc2cn1.OCCO
c1ccc2cc(C3OCCO3)ncc2c1
null
null
C1(=CC=CC=C1)C
Heteroatom Alkylation and Arylation
OtherReaction
fe0fbb45a87f24c1e456c6b4e41101562cd8f0af3ec376bb6115e7c1555d997b
7ac65b5a5f576337ce8e86e0130eb9b4757ca21b2419a0e82bbdfd5def30ee73
c1ccc2cc(C3OCCO3)ncc2c1
O-[CH2;D2;+0:1]-[C:2]-[OH;D1;+0:3].[O;H0;D1;+0:4]=[CH;D2;+0:5]-[c:6](:[c:7]):[#7;a:8]:[c:9]>>[c:9]:[#7;a:8]:[c:6](-[CH;D3;+0:5]1-[O;H0;D2;+0:3]-[C:2]-[CH2;D2;+0:1]-[O;H0;D2;+0:4]-1):[c:7]
89.9
[{"value": 89.9, "product": "O1C(OCC1)C=1N=CC2=CC=CC=C2C1", "details": "PERCENTYIELD", "is_desired": false}, {"value": 89.3, "product": "O1C(OCC1)C=1N=CC2=CC=CC=C2C1", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
null
null
A mixture of 3-isoquinolinecarboxaldehyde (7 g, 44.5 mmol), 5.5 g (88 mmol) of ethylene glycol, 400 ml of toluene and 1.1 g (4.4 mmol) of p-toluenesulfonic acid was refluxed for 16 h while separating the water formed. The mixture was cooled to room temperature and washed with sodium bicarbonate solution, water, and bri...
10.6084/m9.figshare.5104873.v1
null
Aldehyde.Primary alcohol.Primary alcohol
Ether.Ether
null
C1COCO1
c1ccc2cnccc2c1.C1COCO1
HO-
C1(=CC=CC=C1)C
null
null
O=Cc1cc2ccccc2cn1.OCCO>C1(=CC=CC=C1)C>c1ccc2cc(C3OCCO3)ncc2c1
ord_dataset-c2ad1656a3ca4d08888ffb6e3f3a2742
ord-0757477bf28d448db4c5e894a5ea97c1
CCCCCCCCO.O=C(Br)CBr>>CCCCCCCCOC(=O)CBr
BrCC(=O)Br.C(CCCCCCC)O.N1=CC=CC=C1>>BrCC(=O)OCCCCCCCC
[CH3:1][CH2:2][CH2:3][CH2:4][CH2:5][CH2:6][CH2:7][CH2:8][OH:9].Br[C:10](=[O:11])[CH2:12][Br:13]>>[CH3:1][CH2:2][CH2:3][CH2:4][CH2:5][CH2:6][CH2:7][CH2:8][O:9][C:10](=[O:11])[CH2:12][Br:13]
CCCCCCCCO.O=C(Br)CBr
CCCCCCCCOC(=O)CBr
null
null
C(Cl)Cl
Acylation
Schotten-Baumann to ester
6cefe709828c5bd4655f254e75d5dff9e8876e192e7dd47256c1bc0067bc5291
d8a7643b81ed07a6f633aa99465180dfa0565e61ae25aef36338ebb9837c9cef
null
Br-[C;H0;D3;+0:1](=[O;D1;H0:2])-[C:3]-[Br;D1;H0:4].[C:5]-[C:6]-[OH;D1;+0:7]>>[Br;D1;H0:4]-[C:3]-[C;H0;D3;+0:1](=[O;D1;H0:2])-[O;H0;D2;+0:7]-[C:6]-[C:5]
24.1
[{"value": 24.1, "product": "BrCC(=O)OCCCCCCCC", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
10
MINUTE
Bromoacetyl bromide (20 g, 99.1 mmol) was added to a solution of 1-octanol (12.9 g, 99.1 mmol) and 10 ml of pyridine in 100 ml of methylene chloride at 0° C. After 10 minutes, the mixture was quenched with 100 ml of ice/water, and the aqueous layer was extracted with methylene chloride, and the combined organic layer w...
10.6084/m9.figshare.5104873.v1
null
Acyl halide.Primary alcohol
Ester
null
null
null
HBr
C(Cl)Cl
null
0.166667
CCCCCCCCO.O=C(Br)CBr>C(Cl)Cl>CCCCCCCCOC(=O)CBr
ord_dataset-c2ad1656a3ca4d08888ffb6e3f3a2742
ord-792d9e5904e149f68154f932fa6d2ce2
CC(C)C(=O)O.CCCCCCCCOC(=O)CBr.CN(C)P(=O)(N(C)C)N(C)C>>CCCCCCCCOC(=O)C(C)C(C)(C)C(=O)O
C(C(C)C)(=O)O.C(C)(C)[N-]C(C)C.[Li+].C(C)(C)NC(C)C.[Li]CCCC.BrCC(=O)OCCCCCCCC.CN(C)P(=O)(N(C)C)N(C)C>>C(CCCCCCC)OC(=O)C(C(C(=O)O)(C)C)C
[CH:14]([CH3:15])([CH3:16])[C:17](=[O:18])[OH:19].Br[CH2:12][C:10]([O:9][CH2:8][CH2:7][CH2:6][CH2:5][CH2:4][CH2:3][CH2:2][CH3:1])=[O:11].CN(C)P(=O)(N(C)C)N(C)[CH3:13]>>[CH3:1][CH2:2][CH2:3][CH2:4][CH2:5][CH2:6][CH2:7][CH2:8][O:9][C:10](=[O:11])[CH:12]([CH3:13])[C:14]([CH3:15])([CH3:16])[C:17](=[O:18])[OH:19]
CC(C)C(=O)O.CCCCCCCCOC(=O)CBr.CN(C)P(=O)(N(C)C)N(C)C
CCCCCCCCOC(=O)C(C)C(C)(C)C(=O)O
null
null
C1CCOC1
C-C Coupling
OtherReaction
d841351e32f03fa351b4752ba248e792eea3b05d10b194e1f2052626c1dc4283
c8d0ace6c092b333e4fa699bb753afeb889070a86fd0de61e6d5288d99558a57
null
Br-[CH2;D2;+0:1]-[C:2](=[O;D1;H0:3])-[#8:4]-[C:5].C-N(-C)-P(=O)(-N(-C)-C)-N(-C)-[CH3;D1;+0:6].[C;D1;H3:7]-[CH;D3;+0:8](-[C;D1;H3:9])-[C:10](=[O;D1;H0:11])-[O;D1;H1:12]>>[C:5]-[#8:4]-[C:2](=[O;D1;H0:3])-[CH;D3;+0:1](-[CH3;D1;+0:6])-[C;H0;D4;+0:8](-[C;D1;H3:7])(-[C;D1;H3:9])-[C:10](=[O;D1;H0:11])-[O;D1;H1:12]
12.3
[{"value": 12.3, "product": "C(CCCCCCC)OC(=O)C(C(C(=O)O)(C)C)C", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
45
CELSIUS
null
null
To a mixture of lithium diisopropylamide (prepared from 4.8 g, (47.8 mmol) of diisopropylamine and 19.1 ml, (2.5M, 47.8 mmol) of n-BuLi) in 50 ml of THF was added isobutyric acid (2.2 ml, 23.9 mmol) at 0° C. and the mixture was allowed to warm to 45° C. with stirring. To the mixture cooled to -78° C., was added 4.3 g (...
10.6084/m9.figshare.5104873.v1
null
Primary halide.Ester.Tertiary amine.Tertiary amine.Tertiary amine
Ester
null
null
null
HBr
C1CCOC1
45
null
CC(C)C(=O)O.CCCCCCCCOC(=O)CBr.CN(C)P(=O)(N(C)C)N(C)C>C1CCOC1>CCCCCCCCOC(=O)C(C)C(C)(C)C(=O)O
ord_dataset-c2ad1656a3ca4d08888ffb6e3f3a2742
ord-6956540df8cc4043ada703c4bf8c5ec1
CCCCCCCCOC(=O)C(C)C(C)(C)C(=O)O.O=S(Cl)Cl>>CCCCCCCCOC(=O)C(C)C(C)(C)C(=O)Cl
C(CCCCCCC)OC(=O)C(C(C(=O)O)(C)C)C.S(=O)(Cl)Cl>>C(CCCCCCC)OC(=O)C(C(C(=O)Cl)(C)C)C
O[C:17]([C:14]([CH:12]([C:10]([O:9][CH2:8][CH2:7][CH2:6][CH2:5][CH2:4][CH2:3][CH2:2][CH3:1])=[O:11])[CH3:13])([CH3:15])[CH3:16])=[O:18].O=S(Cl)[Cl:19]>>[CH3:1][CH2:2][CH2:3][CH2:4][CH2:5][CH2:6][CH2:7][CH2:8][O:9][C:10](=[O:11])[CH:12]([CH3:13])[C:14]([CH3:15])([CH3:16])[C:17](=[O:18])[Cl:19]
CCCCCCCCOC(=O)C(C)C(C)(C)C(=O)O.O=S(Cl)Cl
CCCCCCCCOC(=O)C(C)C(C)(C)C(=O)Cl
null
null
null
Functional Group Interconversion
Alcohol to chloride_SOCl2
c301c14a9dcd0670d52e8b77396cbe7fd8edeedd757bc43f4162ade1fc52fc93
787f545db5dc0b29dde55b5fbed7db8625b8055f49327f97ed4d83cc47c3af1d
null
Cl-S(=O)-[Cl;H0;D1;+0:1].O-[C;H0;D3;+0:2](=[O;D1;H0:3])-[C:4](-[C;D1;H3:5])(-[C;D1;H3:6])-[C:7]-[C:8](-[#8:9])=[O;D1;H0:10]>>[#8:9]-[C:8](=[O;D1;H0:10])-[C:7]-[C:4](-[C;D1;H3:5])(-[C;D1;H3:6])-[C;H0;D3;+0:2](-[Cl;H0;D1;+0:1])=[O;D1;H0:3]
null
[]
null
null
null
null
3-(1-Octyloxycarbonyl)-2,2-dimethylbutyric acid (0.4 g) was treated with thionyl chloride (20 ml) and the excess thionyl chloride was removed in vacuo to afford 0.33 g of 3-(1-octyloxycarbonyl)-2,2-dimethylbutyric acid chloride. Conditions: See reaction.notes.procedure_details. Workup: the excess thionyl chloride was r...
10.6084/m9.figshare.5104873.v1
null
Carboxylic acid
Acyl halide
null
null
null
HCl
null
null
null
CCCCCCCCOC(=O)C(C)C(C)(C)C(=O)O.O=S(Cl)Cl>>CCCCCCCCOC(=O)C(C)C(C)(C)C(=O)Cl
ord_dataset-c2ad1656a3ca4d08888ffb6e3f3a2742
ord-f04b1eaf04fb4dce92f8799d2cdb1db8
CC(=O)CCc1ccc(OCc2ccccc2)cc1.Cl.N>>CC([NH3+])CCc1ccc(OCc2ccccc2)cc1.[Cl-]
C(C1=CC=CC=C1)OC1=CC=C(C=C1)CCC(=O)C.N.Cl>>[Cl-].CC(CCC1=CC=C(C=C1)OCC1=CC=CC=C1)[NH3+]
O=[C:2]([CH3:1])[CH2:4][CH2:5][c:6]1[cH:7][cH:8][c:9]([O:10][CH2:11][c:12]2[cH:13][cH:14][cH:15][cH:16][cH:17]2)[cH:18][cH:19]1.[ClH:20].[NH3:3]>>[CH3:1][CH:2]([NH3+:3])[CH2:4][CH2:5][c:6]1[cH:7][cH:8][c:9]([O:10][CH2:11][c:12]2[cH:13][cH:14][cH:15][cH:16][cH:17]2)[cH:18][cH:19]1.[Cl-:20]
CC(=O)CCc1ccc(OCc2ccccc2)cc1.Cl.N
CC([NH3+])CCc1ccc(OCc2ccccc2)cc1.[Cl-]
null
[Ni]
C(C)O
Heteroatom Alkylation and Arylation
OtherReaction
0e565144b759285fc4001485318c08d7fdafb328470199718d930bb43326e691
150a254dd88f1deb9794fe82c75c17a8f7dc6e37ef5fe402d4d271ea53a55f02
c1ccc(COc2ccccc2)cc1
O=[C;H0;D3;+0:1](-[C;D1;H3:2])-[C:3]-[C:4].[ClH;D0;+0:5].[NH3;D0;+0:6]>>[C:4]-[C:3]-[CH;D3;+0:1](-[C;D1;H3:2])-[NH3+;D1:6].[Cl-;H0;D0:5]
null
[]
null
null
2
HOUR
A solution of 40.0 g of methyl 2-(4-benzyloxyphenyl)ethyl ketone and 160 ml of anhydrous ammonia in 300 ml of ethanol was heated at 75° C. and stirred for two hours. After cooling the reaction mixture to room temperature, 4.0 g of Raney nickel was added in one portion, and the reaction mixture then was stirred at 25° C...
10.6084/m9.figshare.5104873.v1
null
Ketone
null
null
null
c1ccccc1.c1ccccc1
Other
[Ni].C(C)O
null
2
CC(=O)CCc1ccc(OCc2ccccc2)cc1.Cl.N>[Ni].C(C)O>CC([NH3+])CCc1ccc(OCc2ccccc2)cc1.[Cl-]
ord_dataset-c2ad1656a3ca4d08888ffb6e3f3a2742
ord-cbb806ea98e64dc89b3cf63cd5aec498
CC(N)CCc1ccc(OCc2ccccc2)cc1.O=C(Oc1ccc(C(O)C(=O)O)cc1)c1ccccc1>>CC(CCc1ccc(OCc2ccccc2)cc1)NC(=O)C(O)c1ccc(OCc2ccccc2)cc1
C(C1=CC=CC=C1)(=O)OC1=CC=C(C(C(=O)O)O)C=C1.CC(CCC1=CC=C(C=C1)OCC1=CC=CC=C1)N.C1CCC(CC1)N=C=NC2CCCCC2>>C(C1=CC=CC=C1)OC1=CC=C(C=C1)C(C(NC(CCC1=CC=C(C=C1)OCC1=CC=CC=C1)C)=O)O
[CH3:1][CH:2]([CH2:3][CH2:4][c:5]1[cH:6][cH:7][c:8]([O:9][CH2:10][c:11]2[cH:12][cH:13][cH:14][cH:15][cH:16]2)[cH:17][cH:18]1)[NH2:19].O=[C:29]([O:28][c:27]1[cH:26][cH:25][c:24]([CH:22]([C:20](O)=[O:21])[OH:23])[cH:37][cH:36]1)[c:30]1[cH:31][cH:32][cH:33][cH:34][cH:35]1>>[CH3:1][CH:2]([CH2:3][CH2:4][c:5]1[cH:6][cH:7][c:...
CC(N)CCc1ccc(OCc2ccccc2)cc1.O=C(Oc1ccc(C(O)C(=O)O)cc1)c1ccccc1
CC(CCc1ccc(OCc2ccccc2)cc1)NC(=O)C(O)c1ccc(OCc2ccccc2)cc1
null
null
null
Acylation
OtherReaction
344cb8682157e909550dc80a6959e17d802e8a262d79ed544925031a997fda5c
cfaed6d41dcaf720ed77c4966e5a454532fca2474a59d27ec50e08496706380a
O=C(Cc1ccc(OCc2ccccc2)cc1)NCCCc1ccc(OCc2ccccc2)cc1
O-[C;H0;D3;+0:1](=[O;D1;H0:2])-[C:3](-[O;D1;H1:4])-[c:5].O=[C;H0;D3;+0:6](-[#8:7]-[c:8])-[c:9](:[c:10]):[c:11].[C:12]-[C:13](-[C;D1;H3:14])-[NH2;D1;+0:15]>>[C:12]-[C:13](-[C;D1;H3:14])-[NH;D2;+0:15]-[C;H0;D3;+0:1](=[O;D1;H0:2])-[C:3](-[O;D1;H1:4])-[c:5].[c:8]-[#8:7]-[CH2;D2;+0:6]-[c:9](:[c:10]):[c:11]
null
[]
null
null
null
null
As pointed out above, a preferred embodiment of this invention employs a mixture of all four optica isomers of the compound of Example 7. This racemic mixture can be prepared by the method described above by reaction of dl-4-(benzoyloxy)mandelic acid with dl-1-methyl-3-(4-benzyloxyphenyl)propylamine in the presence of ...
10.6084/m9.figshare.5104873.v1
null
Carboxylic acid.Ester.Primary amine
Ether.Secondary amide
null
null
c1ccccc1.c1ccccc1.c1ccccc1.c1ccccc1
Other
null
null
null
CC(N)CCc1ccc(OCc2ccccc2)cc1.O=C(Oc1ccc(C(O)C(=O)O)cc1)c1ccccc1>>CC(CCc1ccc(OCc2ccccc2)cc1)NC(=O)C(O)c1ccc(OCc2ccccc2)cc1
ord_dataset-c2ad1656a3ca4d08888ffb6e3f3a2742
ord-662ab25bd1194f68a20d32f2372b72ac
[Na+]>>[Na+]
[Na+].COC1=CC=C(OC(C(=O)[O-])C)C=C1.N[C@@H](CCC(=O)O)C(=O)[O-].[K+]>>N[C@@H](CCC(=O)O)C(=O)[O-].[Na+]
[Na+:11]>>[Na+:11]
[Na+]
[Na+]
null
null
null
Miscellaneous
OtherReaction
40ba59785861b8226ce5af6bdcbb9a37f0ff50a8c7ec7d4fc4c524cf906cc65c
56ebed4a8b3cebec83c37a71d68f0c87d1e404ab05a9ce792691e4e18a2379dd
null
null
null
[]
null
null
null
null
Addition of 0.5% by weight of (-)-2-(4-methoxyphenoxy)propionic acid sodium salt to monopotassium glutamate produced a flavor almost identical to monosodium glutamate. Virtually no bitter taste was detectable. Conditions: See reaction.notes.procedure_details.
10.6084/m9.figshare.5104873.v1
null
null
null
null
null
null
null
null
null
null
[Na+]>>[Na+]
ord_dataset-c2ad1656a3ca4d08888ffb6e3f3a2742
ord-b5fb1dd9ab56411ebfb21a50f3743df7
[Na+]>>[Na+]
[Na+].COC1=CC=C(OC(C(=O)[O-])C)C=C1.N[C@@H](CCC(=O)O)C(=O)[O-].[K+]>>N[C@@H](CCC(=O)O)C(=O)[O-].[Na+]
[Na+:11]>>[Na+:11]
[Na+]
[Na+]
null
null
null
Miscellaneous
OtherReaction
40ba59785861b8226ce5af6bdcbb9a37f0ff50a8c7ec7d4fc4c524cf906cc65c
56ebed4a8b3cebec83c37a71d68f0c87d1e404ab05a9ce792691e4e18a2379dd
null
null
null
[]
null
null
null
null
Addition of 0.5% by weight of (-)-2-(4-methoxyphenoxy)propionic acid sodium salt to monopotassium glutamate produced a flavor almost identical to monosodium glutamate. Virtually no bitter taste was detectable. Conditions: See reaction.notes.procedure_details.
10.6084/m9.figshare.5104873.v1
null
null
null
null
null
null
null
null
null
null
[Na+]>>[Na+]
ord_dataset-c2ad1656a3ca4d08888ffb6e3f3a2742
ord-74576cc0cdeb45d39886fb8cdd6bf5f5
[Na+]>>[Na+]
[Na+].COC1=CC=C(OC(C(=O)[O-])C)C=C1.N[C@@H](CCC(=O)O)C(=O)[O-].[K+]>>N[C@@H](CCC(=O)O)C(=O)[O-].[Na+]
[Na+:11]>>[Na+:11]
[Na+]
[Na+]
null
null
null
Miscellaneous
OtherReaction
40ba59785861b8226ce5af6bdcbb9a37f0ff50a8c7ec7d4fc4c524cf906cc65c
56ebed4a8b3cebec83c37a71d68f0c87d1e404ab05a9ce792691e4e18a2379dd
null
null
null
[]
null
null
null
null
Addition of 0.5% by weight of (-)-2-(4-methoxyphenoxy)propionic acid sodium salt to monopotassium glutamate produced a flavor almost identical to monosodium glutamate. Virtually no bitter taste was detectable. Conditions: See reaction.notes.procedure_details.
10.6084/m9.figshare.5104873.v1
null
null
null
null
null
null
null
null
null
null
[Na+]>>[Na+]
ord_dataset-c2ad1656a3ca4d08888ffb6e3f3a2742
ord-90959db5947a4258a73a1e63948f6255
COC(=O)c1cccc(O)c1.O=C1C2CC3CC(C2)CC1C3>>Oc1cccc(COC=C2C3CC4CC(C3)CC2C4)c1
OC=1C=C(C(=O)OC)C=CC1.C12C(C3CC(CC(C1)C3)C2)=O.[H-].[H-].[H-].[H-].[Li+].[Al+3].C(C)N(CC)CC>>OC=1C=C(C=CC1)COC=C1C2CC3CC(CC1C3)C2
O=[C:7]([c:6]1[cH:5][cH:4][cH:3][c:2]([OH:1])[cH:20]1)[O:8][CH3:9].O=[C:10]1[CH:11]2[CH2:12][CH:13]3[CH2:14][CH:15]([CH2:16]2)[CH2:17][CH:18]1[CH2:19]3>>[OH:1][c:2]1[cH:3][cH:4][cH:5][c:6]([CH2:7][O:8][CH:9]=[C:10]2[CH:11]3[CH2:12][CH:13]4[CH2:14][CH:15]([CH2:16]3)[CH2:17][CH:18]2[CH2:19]4)[cH:20]1
COC(=O)c1cccc(O)c1.O=C1C2CC3CC(C2)CC1C3
Oc1cccc(COC=C2C3CC4CC(C3)CC2C4)c1
null
null
O.C1CCOC1
C-C Coupling
OtherReaction
389106083e04f8e6df8f0c9260f1407d6bf5c54e09b67603de76eae196869798
52f6d3ebf2f24b4710cebf4125f6a3882be46cd0b71cef8accd7c6ff101eaf88
C(OCc1ccccc1)=C1C2CC3CC(C2)CC1C3
O=[C;H0;D3;+0:1](-[#8:2]-[CH3;D1;+0:3])-[c:4](:[c:5]):[c:6].O=[C;H0;D3;+0:7](-[C:8](-[C:9])-[C:10])-[C:11](-[C:12])-[C:13]>>[C:9]-[C:8](-[C:10])-[C;H0;D3;+0:7](=[CH;D2;+0:3]-[#8:2]-[CH2;D2;+0:1]-[c:4](:[c:5]):[c:6])-[C:11](-[C:12])-[C:13]
89
[{"value": 89.0, "product": "OC=1C=C(C=CC1)COC=C1C2CC3CC(CC1C3)C2", "details": "PERCENTYIELD", "is_desired": false}, {"value": 88.8, "product": "OC=1C=C(C=CC1)COC=C1C2CC3CC(CC1C3)C2", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
15
MINUTE
[(3-Hydroxyphenyl)methoxymethylene]adamantane (1a) was prepared as described in my previous application Serial No. 224,681, filed Jul. 27, 1988. A 500-mL flask was fitted with a reflux condenser, a 125-mL addition funnel, and nitrogen line. The apparatus was dried by means of a hot air gun and nitrogen purging. Dry THF...
10.6084/m9.figshare.5104873.v1
null
Ketone.Ester
Ether
C1C2CC3CC1CC(C2)C3
C1C2CC3CC1CC(C2)C3
c1ccccc1.C1C2CC3CC1CC(C2)C3
Other
O.C1CCOC1
null
0.25
COC(=O)c1cccc(O)c1.O=C1C2CC3CC(C2)CC1C3>O.C1CCOC1>Oc1cccc(COC=C2C3CC4CC(C3)CC2C4)c1
ord_dataset-c2ad1656a3ca4d08888ffb6e3f3a2742
ord-7fa72a964a72422f852d7a22402421fe
CCCCCCCCCCCCCCCCC(OC(C)=O)C(=O)N[C@@H](CO)[C@H](O)[C@H](O)CCCCCCCCCCCCCC>>CCCCCCCCCCCCCCCCC(O)C(=O)N[C@@H](CO)[C@H](O)[C@H](O)CCCCCCCCCCCCCC
[OH-].[Na+].C(C)(=O)OC(C(=O)N[C@@H](CO)[C@H](O)[C@H](O)CCCCCCCCCCCCCC)CCCCCCCCCCCCCCCC.[OH-].[Na+]>>OC(C(=O)N[C@@H](CO)[C@H](O)[C@H](O)CCCCCCCCCCCCCC)CCCCCCCCCCCCCCCC
CC(=O)[O:18][CH: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][CH3:1])[C:19](=[O:20])[NH:21][C@@H:22]([CH2:23][OH:24])[C@H:25]([OH:26])[C@H:27]([OH:28])[CH2:29][CH2:30][CH2:31][CH2:32][CH2:33][CH2:34][CH2:35][CH2:36][CH2:37][CH2:38][CH2:39][CH2:40][C...
CCCCCCCCCCCCCCCCC(OC(C)=O)C(=O)N[C@@H](CO)[C@H](O)[C@H](O)CCCCCCCCCCCCCC
CCCCCCCCCCCCCCCCC(O)C(=O)N[C@@H](CO)[C@H](O)[C@H](O)CCCCCCCCCCCCCC
null
null
C(C)O
Reduction
Hydrolysis or Hydrogenolysis of Carboxylic Esters or Thioesters
d7acfb2397f2b5b2a83b3bebf3698d6d984dd716982297f62a944222c79ce234
19dd58e0f83625e74b4b1375d88cb4c813ee60f593d812516d14eafc4ab68dc7
null
C-C(=O)-[O;H0;D2;+0:1]-[C:2](-[C:3])-[C:4](=[O;D1;H0:5])-[#7:6]-[C:7]>>[C:3]-[C:2](-[OH;D1;+0:1])-[C:4](=[O;D1;H0:5])-[#7:6]-[C:7]
null
[]
null
null
1.5
HOUR
A mixture of 35.62 grams (55.4 mmoles) of N-(2-acetoxy-octadecanoyl) phytosphingosine, 250 ml of 96% ethanol and 20 ml of 6.18M sodium hydroxide is stirred for 1.5 hours. An additional 5 ml of 6.18M sodium hydroxide is added and the stirring continued for 1 hour. Conditions: See reaction.notes.procedure_details. Workup...
10.6084/m9.figshare.5104873.v1
null
Ester
Secondary alcohol
null
null
null
HO-
C(C)O
null
1.5
CCCCCCCCCCCCCCCCC(OC(C)=O)C(=O)N[C@@H](CO)[C@H](O)[C@H](O)CCCCCCCCCCCCCC>C(C)O>CCCCCCCCCCCCCCCCC(O)C(=O)N[C@@H](CO)[C@H](O)[C@H](O)CCCCCCCCCCCCCC
ord_dataset-c2ad1656a3ca4d08888ffb6e3f3a2742
ord-5e431815bfc34fb79e4253adb29aeeb3
CCCCCCCCCCCCCCCCCCCCCCC(N[C@@H](CO)[C@H](O)[C@H](O)CCCCCCCCCCCCCC)C(=O)OC(C)=O>>CCCCCCCCCCCCCCCCCCCCCCC(N[C@@H](CO)[C@H](O)[C@H](O)CCCCCCCCCCCCCC)C(=O)O
[OH-].[Na+].C(C)(=O)OC(C(CCCCCCCCCCCCCCCCCCCCCC)N[C@@H](CO)[C@H](O)[C@H](O)CCCCCCCCCCCCCC)=O.[OH-].[Na+]>>OC(C(CCCCCCCCCCCCCCCCCCCCCC)N[C@@H](CO)[C@H](O)[C@H](O)CCCCCCCCCCCCCC)=O
CC(=O)[O:48][C:46]([CH:23]([CH2:22][CH2:21][CH2:20][CH2:19][CH2:18][CH2:17][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][CH3:1])[NH:24][C@@H:25]([CH2:26][OH:27])[C@H:28]([OH:29])[C@H:30]([OH:31])[CH2:32][CH2:33][CH2:34][CH2:35][CH2:36][CH2:37][CH2:38][C...
CCCCCCCCCCCCCCCCCCCCCCC(N[C@@H](CO)[C@H](O)[C@H](O)CCCCCCCCCCCCCC)C(=O)OC(C)=O
CCCCCCCCCCCCCCCCCCCCCCC(N[C@@H](CO)[C@H](O)[C@H](O)CCCCCCCCCCCCCC)C(=O)O
null
null
C(C)O
Reduction
Hydrolysis or Hydrogenolysis of Carboxylic Esters or Thioesters
18e1e61321ff01ec602ee6e196a485c543be50cc909a3dcf6656e78df2b0c8a3
142e3062b491bdf723a1cbf11092ef8608063f50d7ab4a919f898a356546f037
null
C-C(=O)-[O;H0;D2;+0:1]-[C:2](-[C:3])=[O;D1;H0:4]>>[C:3]-[C:2](=[O;D1;H0:4])-[OH;D1;+0:1]
null
[]
null
null
1.5
HOUR
Sodium hydroxide (0.08 ml, 6.18M) is added to a stirred solution of 58 mg of N-(α-acetoxy-tetracosanoyl) phytosphingosine in 3 ml of 96% ethanol. After 1.5 hours, additional 6.18M sodium hydroxide (0.05 ml) is added and stirring is continued for 0.5 hour. Conditions: See reaction.notes.procedure_details. Workup: is con...
10.6084/m9.figshare.5104873.v1
null
Anhydride
Carboxylic acid
null
null
null
HO-
C(C)O
null
1.5
CCCCCCCCCCCCCCCCCCCCCCC(N[C@@H](CO)[C@H](O)[C@H](O)CCCCCCCCCCCCCC)C(=O)OC(C)=O>C(C)O>CCCCCCCCCCCCCCCCCCCCCCC(N[C@@H](CO)[C@H](O)[C@H](O)CCCCCCCCCCCCCC)C(=O)O
ord_dataset-c2ad1656a3ca4d08888ffb6e3f3a2742
ord-6b6e2b7980b642d68dd1b77edd6c47e4
O=C(O)c1ccc(B(O)O)cc1.O=C1CCC(=O)N1O>>O=C(ON1C(=O)CCC1=O)c1ccc(B(O)O)cc1
C1(CCCCC1)N=C=NC1CCCCC1.C(=O)(O)C1=CC=C(C=C1)B(O)O.ON1C(CCC1=O)=O.ClCCl>>C1(CCC(N1OC(=O)C1=CC=C(C=C1)B(O)O)=O)=O
O[C:2](=[O:1])[c:11]1[cH:12][cH:13][c:14]([B:15]([OH:16])[OH:17])[cH:18][cH:19]1.[OH:3][N:4]1[C:5](=[O:6])[CH2:7][CH2:8][C:9]1=[O:10]>>[O:1]=[C:2]([O:3][N:4]1[C:5](=[O:6])[CH2:7][CH2:8][C:9]1=[O:10])[c:11]1[cH:12][cH:13][c:14]([B:15]([OH:16])[OH:17])[cH:18][cH:19]1
O=C(O)c1ccc(B(O)O)cc1.O=C1CCC(=O)N1O
O=C(ON1C(=O)CCC1=O)c1ccc(B(O)O)cc1
null
null
CN(C)C=O
Protection
OtherReaction
a1b3ee4184fc00a0730e4c14eca3a5fbe87fccb44744074c13ef1bfbfabde8ad
e66168e1cfeb6611d93ee4c49193aae81e56c700a9fe46743dc42eed291ed0f9
O=C(ON1C(=O)CCC1=O)c1ccccc1
O-[C;H0;D3;+0:1](=[O;D1;H0:2])-[c:3](:[c:4]):[c:5].[O;D1;H0:6]=[C:7]1-[C:8]-[C:9]-[C:10](=[O;D1;H0:11])-[#7:12]-1-[OH;D1;+0:13]>>[O;D1;H0:6]=[C:7]1-[C:8]-[C:9]-[C:10](=[O;D1;H0:11])-[#7:12]-1-[O;H0;D2;+0:13]-[C;H0;D3;+0:1](=[O;D1;H0:2])-[c:3](:[c:4]):[c:5]
null
[]
null
null
10
MINUTE
4-Carboxyphenyl-boronic acid (CPBA, Example 1, 0.25 g, 1.51 mmol) and N-hydroxysuccinimide (0.26 g, 2.26 mmol) were dissolved in 8.5 ml DMF using a magnetic stirrer. 20 ml of dichloromethane (CH2Cl2) was then added, and the solution was stirred for 10 minutes. N,N'-dicyclohexyl-carbodiimide (DCC, 0.93 g, 4.52 mmol) in ...
10.6084/m9.figshare.5104873.v1
null
Carboxylic acid
null
null
null
C1CC[NH]C1.c1ccccc1
HO-
CN(C)C=O
null
0.166667
O=C(O)c1ccc(B(O)O)cc1.O=C1CCC(=O)N1O>CN(C)C=O>O=C(ON1C(=O)CCC1=O)c1ccc(B(O)O)cc1
ord_dataset-c2ad1656a3ca4d08888ffb6e3f3a2742
ord-07f496de1bd0491e8be710dd1d24e21a
COc1ccc(N)cc1.c1ccc2c(c1)Nc1ccccc1S2>>COc1ccc(NC2C=CC3=Nc4ccccc4SC3=C2)cc1
C1=CC=CC=2SC3=CC=CC=C3NC12.C1=CC=CC=2SC3=CC=CC=C3NC12.COC1=CC=C(C=C1)N.I(=O)(=O)(=O)O.O>>COC1=CC=C(C=C1)NC1C=CC2=NC3=CC=CC=C3SC2=C1
[CH3:1][O:2][c:3]1[cH:4][cH:5][c:6]([NH2:7])[cH:22][cH:23]1.[cH:8]1[cH:9][cH:10][c:11]2[c:20]([cH:21]1)[S:19][c:18]1[c:13]([cH:14][cH:15][cH:16][cH:17]1)[NH:12]2>>[CH3:1][O:2][c:3]1[cH:4][cH:5][c:6]([NH:7][CH:8]2[CH:9]=[CH:10][C:11]3=[N:12][c:13]4[cH:14][cH:15][cH:16][cH:17][c:18]4[S:19][C:20]3=[CH:21]2)[cH:22][cH:23]1
COc1ccc(N)cc1.c1ccc2c(c1)Nc1ccccc1S2
COc1ccc(NC2C=CC3=Nc4ccccc4SC3=C2)cc1
null
null
CO
Heteroatom Alkylation and Arylation
OtherReaction
6930dee6fed16270a98a17affa303d48c6d1a23c1b7ce83a8f96734b9c689844
135d6726372d55ea8e2468fa41946626334f79bb40cbea88b6316de909b8cb14
C1=CC(Nc2ccccc2)C=C2Sc3ccccc3N=C12
[NH2;D1;+0:1]-[c:2](:[c:3]):[c:4].[c:5]:[c:6]1:[c:7]-[#16:8]-[c;H0;D3;+0:9]2:[cH;D2;+0:10]:[cH;D2;+0:11]:[cH;D2;+0:12]:[cH;D2;+0:13]:[c;H0;D3;+0:14]:2-[NH;D2;+0:15]-1>>[c:5]:[c:6]1:[c:7]-[#16:8]-[C;H0;D3;+0:9]2=[CH;D2;+0:10]-[CH;D3;+0:11](-[NH;D2;+0:1]-[c:2](:[c:3]):[c:4])-[CH;D2;+0:12]=[CH;D2;+0:13]-[C;H0;D3;+0:14]-2=...
null
[]
null
null
null
null
Phenothiazine, 0.5 g/0.0025M, and p-anisidine, 0.307 g/0.0025M, were dissolved in 50 ml of methanol and stirred at ambient temperature. Periodic acid, 3.4 g/0.015M, was dissolved in 40 ml of methanol and the solution added in one portion to the stirring phenothiazine mixture. The reaction mixture was stirred for 20 min...
10.6084/m9.figshare.5104873.v1
null
Primary amine.Secondary amine.Monosulfide
Substituted imine.Secondary amine.Monosulfide
c1ccc2c(c1)Nc1ccccc1S2
C1=CC2=Nc3ccccc3SC2=CC1
c1ccccc1.C1=CC2=Nc3ccccc3SC2=CC1
null
CO
null
null
COc1ccc(N)cc1.c1ccc2c(c1)Nc1ccccc1S2>CO>COc1ccc(NC2C=CC3=Nc4ccccc4SC3=C2)cc1
ord_dataset-c2ad1656a3ca4d08888ffb6e3f3a2742
ord-84944dda715e4fbebd2a94e48004d0ca
O=C(CN1CCN(Cc2ccccc2)CCN(Cc2ccccc2)CCN(Cc2ccccc2)CC1)NCCOCCOCCNC(=O)CN1CCN(Cc2ccccc2)CCN(Cc2ccccc2)CCN(Cc2ccccc2)CC1>>O=C(CN1CCNCCNCCNCC1)NCCOCCOCCNC(=O)CN1CCNCCNCCNCC1
C(C1=CC=CC=C1)N1CCN(CCN(CCN(CC1)CC1=CC=CC=C1)CC1=CC=CC=C1)CC(NCCOCCOCCNC(CN1CCN(CCN(CCN(CC1)CC1=CC=CC=C1)CC1=CC=CC=C1)CC1=CC=CC=C1)=O)=O.[H][H]>>N1(CCNCCNCCNCC1)CC(NCCOCCOCCNC(CN1CCNCCNCCNCC1)=O)=O
c1ccc(C[N:7]2[CH2:6][CH2:5][N:4]([CH2:3][C:2](=[O:1])[NH:16][CH2:17][CH2:18][O:19][CH2:20][CH2:21][O:22][CH2:23][CH2:24][NH:25][C:26](=[O:27])[CH2:28][N:29]3[CH2:30][CH2:31][N:32](Cc4ccccc4)[CH2:33][CH2:34][N:35](Cc4ccccc4)[CH2:36][CH2:37][N:38](Cc4ccccc4)[CH2:39][CH2:40]3)[CH2:15][CH2:14][N:13](Cc3ccccc3)[CH2:12][CH2:...
O=C(CN1CCN(Cc2ccccc2)CCN(Cc2ccccc2)CCN(Cc2ccccc2)CC1)NCCOCCOCCNC(=O)CN1CCN(Cc2ccccc2)CCN(Cc2ccccc2)CCN(Cc2ccccc2)CC1
O=C(CN1CCNCCNCCNCC1)NCCOCCOCCNC(=O)CN1CCNCCNCCNCC1
null
[Pd]
C(C)O
Deprotection
OtherReaction
b3ef448f3c072b860503888ac4ae403973cda377756245b9bc84361b4ec206d0
705d8456c685cb47958fd61d15282eb479dd11776543e6bc5df803aca4cd9d81
O=C(CN1CCNCCNCCNCC1)NCCOCCOCCNC(=O)CN1CCNCCNCCNCC1
C(-[N;H0;D3;+0:1]1-[C:2]-[C:3]-[#7:4]-[C:5]-[C:6]-[N;H0;D3;+0:7](-C-c2:c:c:c:c:c:2)-[C:8]-[C:9]-[N;H0;D3;+0:10](-C-c2:c:c:c:c:c:2)-[C:11]-[C:12]-1)-c1:c:c:c:c:c:1.C(-[N;H0;D3;+0:13]1-[C:14]-[C:15]-[N;H0;D3;+0:16](-C-c2:c:c:c:c:c:2)-[C:17]-[C:18]-[#7:19]-[C:20]-[C:21]-[N;H0;D3;+0:22](-C-c2:c:c:c:c:c:2)-[C:23]-[C:24]-1)-...
null
[]
null
null
null
null
A 100 mL Autoclave pressure reactor was charged with 9.2 g (8.3 mmol) of 8, 50 mL of ethanol and 3 g of 10% Pd/C. The reactor was pressurized to 220 psig with hydrogen for 3 hours at 80° C. The mixture was filtered and the filtrate was concentrated to a slightly yellow oil. 1H NMR, 13C NMR, and mass spectroscopy data w...
10.6084/m9.figshare.5104873.v1
null
Tertiary amine.Tertiary amine.Tertiary amine.Tertiary amine.Tertiary amine.Tertiary amine
Secondary amine.Secondary amine.Secondary amine.Secondary amine.Secondary amine.Secondary amine
c1ccccc1.C1C[NH]CC[NH]CC[NH]CC[NH]1.C1C[NH]CC[NH]CC[NH]CC[NH]1.c1ccccc1.c1ccccc1.c1ccccc1.c1ccccc1.c1ccccc1
C1CNCC[NH]CCNCCN1.C1CNCC[NH]CCNCCN1
C1CNCC[NH]CCNCCN1.C1CNCC[NH]CCNCCN1
Other
[Pd].C(C)O
null
null
O=C(CN1CCN(Cc2ccccc2)CCN(Cc2ccccc2)CCN(Cc2ccccc2)CC1)NCCOCCOCCNC(=O)CN1CCN(Cc2ccccc2)CCN(Cc2ccccc2)CCN(Cc2ccccc2)CC1>[Pd].C(C)O>O=C(CN1CCNCCNCCNCC1)NCCOCCOCCNC(=O)CN1CCNCCNCCNCC1
ord_dataset-c2ad1656a3ca4d08888ffb6e3f3a2742
ord-de6058ab8e8a475cb7537815b0489c23
CC1CO1.O=C(O)CN1CCNCCN(CC(=O)O)CCN(CC(=O)O)CC1>>CC(O)CN1CCN(CC(=O)O)CCN(CC(=O)O)CCN(CC(=O)O)CC1
C1C(C)O1.C(=O)(O)CN1CCN(CCN(CCNCC1)CC(=O)O)CC(=O)O.[OH-].[Na+]>>C(=O)(O)CN1CCN(CCN(CCN(CC1)CC(C)O)CC(=O)O)CC(=O)O
[CH3:1][CH:2]1[O:3][CH2:4]1.[N:5]1([CH2:9][C:10](=[O:11])[OH:12])[CH2:6][CH2:7][NH:8][CH2:13][CH2:14][N:15]([CH2:16][C:17](=[O:18])[OH:19])[CH2:20][CH2:21][N:22]([CH2:23][C:24](=[O:25])[OH:26])[CH2:27][CH2:28]1>>[CH3:1][CH:2]([OH:3])[CH2:4][N:5]1[CH2:6][CH2:7][N:8]([CH2:9][C:10](=[O:11])[OH:12])[CH2:13][CH2:14][N:15]([...
CC1CO1.O=C(O)CN1CCNCCN(CC(=O)O)CCN(CC(=O)O)CC1
CC(O)CN1CCN(CC(=O)O)CCN(CC(=O)O)CCN(CC(=O)O)CC1
null
null
O
Heteroatom Alkylation and Arylation
Ring opening of epoxide with amine
21c25a0a59c5eb9f0cfa1bff61bf24a37379bbb493ae62bd16e9525054d02154
463dd67c902792183527d1ff0fe86cd8bdfb6ac2b856921305dee39e0d05e1a4
C1CNCCNCCNCCN1
[#7:1]-[C:2]-[C:3]-[NH;D2;+0:4]-[C:5]-[C:6]-[N;H0;D3;+0:7](-[CH2;D2;+0:8]-[C:9](=[O;D1;H0:10])-[O;D1;H1:11])-[C:12]-[C:13]-[#7:14].[C;D1;H3:15]-[C:16]1-[CH2;D2;+0:17]-[O;H0;D2;+0:18]-1>>[#7:1]-[C:2]-[C:3]-[N;H0;D3;+0:4](-[CH2;D2;+0:8]-[C:9](=[O;D1;H0:10])-[O;D1;H1:11])-[C:5]-[C:6]-[N;H0;D3;+0:7](-[CH2;D2;+0:17]-[C:16](...
96
[{"value": 96.0, "product": "C(=O)(O)CN1CCN(CCN(CCN(CC1)CC(C)O)CC(=O)O)CC(=O)O", "details": "PERCENTYIELD", "is_desired": false}]
null
null
null
null
To a solution of 194.0 g (0.56 mol) of 15 in 450 mL of water is added sufficient NaOH to adjust the pH to 12.0 to 12.5 (the temperature is maintained below 30° C. during the addition). Propylene oxide (65 g, 1.12 mols) is added to the basic solution. After 6 hours at ambient temperature the excess propylene oxide and s...
10.6084/m9.figshare.5104873.v1
null
Ether.Secondary amine.Tertiary amine
Secondary alcohol.Tertiary amine.Tertiary amine
C1CO1.C1CNCC[NH]CC[NH]CC[NH]1
C1C[NH]CC[NH]CC[NH]CC[NH]1
C1C[NH]CC[NH]CC[NH]CC[NH]1
null
O
null
null
CC1CO1.O=C(O)CN1CCNCCN(CC(=O)O)CCN(CC(=O)O)CC1>O>CC(O)CN1CCN(CC(=O)O)CCN(CC(=O)O)CCN(CC(=O)O)CC1
ord_dataset-c2ad1656a3ca4d08888ffb6e3f3a2742
ord-a60415cbb95e437fb80f71d2bf6155d2
O=P(O)(O)O>>O=P([O-])([O-])[O-]
C(CCCCCCC)S(=O)(=O)[O-].[Na+].P(O)(O)(O)=O.[OH-].[Na+].Cl.N1(CCCCC1)CCOC1=CC=C(C(=O)O)C=C1>>P(=O)([O-])([O-])[O-].C(CCCCCCC)S(=O)(=O)[O-]
[O:13]=[P:14]([OH:15])([OH:16])[OH:17]>>[O:13]=[P:14]([O-:15])([O-:16])[O-:17]
O=P(O)(O)O
O=P([O-])([O-])[O-]
null
null
C(C)#N.O
Oxidation
OtherReaction
8411f9fce1f185c5c08a89a741e7494817f2d5e55ac6ad2b663e4ffb9ef8fbab
82a3692de44364afcfd8cc4460435180e0752c31812bf6008d75e02664a32947
null
[O;D1;H0:1]=[#15:2](-[OH;D1;+0:3])(-[OH;D1;+0:4])-[OH;D1;+0:5]>>[O-;H0;D1:3]-[#15:2](-[O-;H0;D1:4])(-[O-;H0;D1:5])=[O;D1;H0:1]
null
[]
null
null
5
MINUTE
HPLC analysis indicated substantially pure 4-(2-piperidinoethoxy)benzoic acid, hydrochloride with only minor amounts of the methyl ester. The HPLC analysis was conducted as follows: A Zorbax C8 column was used (length: 25 cm; diameter: 4.6 mm; particle size: 5 microns). A weak eluent (60 mM phosphate and 10 mM octane s...
10.6084/m9.figshare.5104873.v1
null
null
null
null
null
null
null
C(C)#N.O
null
0.083333
O=P(O)(O)O>C(C)#N.O>O=P([O-])([O-])[O-]
ord_dataset-c2ad1656a3ca4d08888ffb6e3f3a2742
ord-d12c63c36e004bc2bf7eed9db4fbf3fa
COC(=O)c1ccc(O)cc1.ClCCN1CCCCC1>>O=C(O)c1ccc(OCCN2CCCCC2)cc1
C([O-])([O-])=O.[K+].[K+].OC1=CC=C(C(=O)OC)C=C1.C(C)(=O)OC(C)C.Cl.ClCCN1CCCCC1>>Cl.N1(CCCCC1)CCOC1=CC=C(C(=O)O)C=C1
C[O:4][C:3](=[O:2])[c:5]1[cH:6][cH:7][c:8]([OH:9])[cH:18][cH:19]1.Cl[CH2:10][CH2:11][N:12]1[CH2:13][CH2:14][CH2:15][CH2:16][CH2:17]1>>[O:2]=[C:3]([OH:4])[c:5]1[cH:6][cH:7][c:8]([O:9][CH2:10][CH2:11][N:12]2[CH2:13][CH2:14][CH2:15][CH2:16][CH2:17]2)[cH:18][cH:19]1
COC(=O)c1ccc(O)cc1.ClCCN1CCCCC1
O=C(O)c1ccc(OCCN2CCCCC2)cc1
null
null
O
Heteroatom Alkylation and Arylation
OtherReaction
c47049bacd28cc701f2e77df376a2fcefecd5392e081f9a62473cff265d23a8c
017337a0828c32d10d28543003ae15a8b492b5e2f69019c65a4461eabc617d95
c1ccc(OCCN2CCCCC2)cc1
C-[O;H0;D2;+0:1]-[C:2](=[O;D1;H0:3])-[c:4].[OH;D1;+0:5]-[c:6](:[c:7]):[c:8].Cl-[CH2;D2;+0:9]-[C:10]-[#7:11]>>[#7:11]-[C:10]-[CH2;D2;+0:9]-[O;H0;D2;+0:5]-[c:6](:[c:7]):[c:8].[O;D1;H0:3]=[C:2](-[OH;D1;+0:1])-[c:4]
null
[]
80
CELSIUS
5
HOUR
To a 250 mL 3 neck flask equipped with mechanical stirring, condenser, and heating apparatus consisting of a RTD probe hooked via a temperature controller to a heating mantle and under nitrogen atmosphere, the following were added: 7.61 g methyl 4-hydroxybenzoate, 11.05 g β-chloroethylpiperidine hydrochloride, 16.59 g ...
10.6084/m9.figshare.5104873.v1
null
Primary halide.Ester.Aromatic alcohol
Carboxylic acid.Ether
null
null
c1ccccc1.C1CC[NH]CC1
HCl
O
80
5
COC(=O)c1ccc(O)cc1.ClCCN1CCCCC1>O>O=C(O)c1ccc(OCCN2CCCCC2)cc1
ord_dataset-c2ad1656a3ca4d08888ffb6e3f3a2742
ord-48ae4b85295345399e5e9c5cdc2a4dea
COC(=O)c1ccc(O)cc1.ClCCN1CCCCC1>>O=C(O)c1ccc(OCCN2CCCCC2)cc1
C([O-])([O-])=O.[K+].[K+].OC1=CC=C(C(=O)OC)C=C1.C(C)(=O)OCCCCC.Cl.ClCCN1CCCCC1>>Cl.N1(CCCCC1)CCOC1=CC=C(C(=O)O)C=C1
C[O:4][C:3](=[O:2])[c:5]1[cH:6][cH:7][c:8]([OH:9])[cH:18][cH:19]1.Cl[CH2:10][CH2:11][N:12]1[CH2:13][CH2:14][CH2:15][CH2:16][CH2:17]1>>[O:2]=[C:3]([OH:4])[c:5]1[cH:6][cH:7][c:8]([O:9][CH2:10][CH2:11][N:12]2[CH2:13][CH2:14][CH2:15][CH2:16][CH2:17]2)[cH:18][cH:19]1
COC(=O)c1ccc(O)cc1.ClCCN1CCCCC1
O=C(O)c1ccc(OCCN2CCCCC2)cc1
null
null
O
Heteroatom Alkylation and Arylation
OtherReaction
c47049bacd28cc701f2e77df376a2fcefecd5392e081f9a62473cff265d23a8c
017337a0828c32d10d28543003ae15a8b492b5e2f69019c65a4461eabc617d95
c1ccc(OCCN2CCCCC2)cc1
C-[O;H0;D2;+0:1]-[C:2](=[O;D1;H0:3])-[c:4].[OH;D1;+0:5]-[c:6](:[c:7]):[c:8].Cl-[CH2;D2;+0:9]-[C:10]-[#7:11]>>[#7:11]-[C:10]-[CH2;D2;+0:9]-[O;H0;D2;+0:5]-[c:6](:[c:7]):[c:8].[O;D1;H0:3]=[C:2](-[OH;D1;+0:1])-[c:4]
null
[]
null
null
null
null
To a 125 mL 3 neck flask with mechanical stirring, condenser, and a heating apparatus consisting of an RTD probe hooked via a temperature controller to a heating mantle, the following were added: 7.61 g methyl 4-hydroxybenzoate, 11.05 g β-chloroethylpiperidine hydrochloride, 16.59 g powdered potassium carbonate, and 60...
10.6084/m9.figshare.5104873.v1
null
Primary halide.Ester.Aromatic alcohol
Carboxylic acid.Ether
null
null
c1ccccc1.C1CC[NH]CC1
HCl
O
null
null
COC(=O)c1ccc(O)cc1.ClCCN1CCCCC1>O>O=C(O)c1ccc(OCCN2CCCCC2)cc1
ord_dataset-c2ad1656a3ca4d08888ffb6e3f3a2742
ord-21f24d67043b4692bc3cf3a299646270
COC(=O)c1ccc(O)cc1.ClCCN1CCCCC1>>O=C(O)c1ccc(OCCN2CCCCC2)cc1
C([O-])([O-])=O.[K+].[K+].OC1=CC=C(C(=O)OC)C=C1.C(C)(=O)OCCCCC.Cl.ClCCN1CCCCC1>>Cl.N1(CCCCC1)CCOC1=CC=C(C(=O)O)C=C1
C[O:4][C:3](=[O:2])[c:5]1[cH:6][cH:7][c:8]([OH:9])[cH:18][cH:19]1.Cl[CH2:10][CH2:11][N:12]1[CH2:13][CH2:14][CH2:15][CH2:16][CH2:17]1>>[O:2]=[C:3]([OH:4])[c:5]1[cH:6][cH:7][c:8]([O:9][CH2:10][CH2:11][N:12]2[CH2:13][CH2:14][CH2:15][CH2:16][CH2:17]2)[cH:18][cH:19]1
COC(=O)c1ccc(O)cc1.ClCCN1CCCCC1
O=C(O)c1ccc(OCCN2CCCCC2)cc1
null
null
O
Heteroatom Alkylation and Arylation
OtherReaction
c47049bacd28cc701f2e77df376a2fcefecd5392e081f9a62473cff265d23a8c
017337a0828c32d10d28543003ae15a8b492b5e2f69019c65a4461eabc617d95
c1ccc(OCCN2CCCCC2)cc1
C-[O;H0;D2;+0:1]-[C:2](=[O;D1;H0:3])-[c:4].[OH;D1;+0:5]-[c:6](:[c:7]):[c:8].Cl-[CH2;D2;+0:9]-[C:10]-[#7:11]>>[#7:11]-[C:10]-[CH2;D2;+0:9]-[O;H0;D2;+0:5]-[c:6](:[c:7]):[c:8].[O;D1;H0:3]=[C:2](-[OH;D1;+0:1])-[c:4]
null
[]
97
CELSIUS
8
HOUR
To a 125 mL 3 neck flask with mechanical stirring, condensers, and a heating apparatus consisting of an RTD probe in the flask hooked via a temperature controller to a heating mantle, the following were added: 7.61 g methyl 4-hydroxybenzoate, 11.05 g -chloroethylpiperidine hydrochloride, 16.59 g powdered potassium carb...
10.6084/m9.figshare.5104873.v1
null
Primary halide.Ester.Aromatic alcohol
Carboxylic acid.Ether
null
null
c1ccccc1.C1CC[NH]CC1
HCl
O
97
8
COC(=O)c1ccc(O)cc1.ClCCN1CCCCC1>O>O=C(O)c1ccc(OCCN2CCCCC2)cc1
ord_dataset-c2ad1656a3ca4d08888ffb6e3f3a2742
ord-0b3314315e2f4a7d9cfeba4d69f24baf
COC(=O)c1ccc(O)cc1.ClCCN1CCCCC1>>O=C(O)c1ccc(OCCN2CCCCC2)cc1
C([O-])([O-])=O.[K+].[K+].OC1=CC=C(C(=O)OC)C=C1.Cl.ClCCN1CCCCC1>>Cl.N1(CCCCC1)CCOC1=CC=C(C(=O)O)C=C1
C[O:4][C:3](=[O:2])[c:5]1[cH:6][cH:7][c:8]([OH:9])[cH:18][cH:19]1.Cl[CH2:10][CH2:11][N:12]1[CH2:13][CH2:14][CH2:15][CH2:16][CH2:17]1>>[O:2]=[C:3]([OH:4])[c:5]1[cH:6][cH:7][c:8]([O:9][CH2:10][CH2:11][N:12]2[CH2:13][CH2:14][CH2:15][CH2:16][CH2:17]2)[cH:18][cH:19]1
COC(=O)c1ccc(O)cc1.ClCCN1CCCCC1
O=C(O)c1ccc(OCCN2CCCCC2)cc1
null
null
C(C)(=O)OCCCCC
Heteroatom Alkylation and Arylation
OtherReaction
c47049bacd28cc701f2e77df376a2fcefecd5392e081f9a62473cff265d23a8c
017337a0828c32d10d28543003ae15a8b492b5e2f69019c65a4461eabc617d95
c1ccc(OCCN2CCCCC2)cc1
C-[O;H0;D2;+0:1]-[C:2](=[O;D1;H0:3])-[c:4].[OH;D1;+0:5]-[c:6](:[c:7]):[c:8].Cl-[CH2;D2;+0:9]-[C:10]-[#7:11]>>[#7:11]-[C:10]-[CH2;D2;+0:9]-[O;H0;D2;+0:5]-[c:6](:[c:7]):[c:8].[O;D1;H0:3]=[C:2](-[OH;D1;+0:1])-[c:4]
null
[]
125
CELSIUS
null
null
To a 125 mL 3 neck flask with mechanical stirring, condenser, and a heating apparatus consisting of an RTD probe in the flask hooked via a temperature controller to a heating mantle, the following were added: 7.61 g methyl 4-hydroxybenzoate, 11.05 g β-chloroethylpiperidine hydrochloride, 16.59 g powdered potassium carb...
10.6084/m9.figshare.5104873.v1
null
Primary halide.Ester.Aromatic alcohol
Carboxylic acid.Ether
null
null
c1ccccc1.C1CC[NH]CC1
HCl
C(C)(=O)OCCCCC
125
null
COC(=O)c1ccc(O)cc1.ClCCN1CCCCC1>C(C)(=O)OCCCCC>O=C(O)c1ccc(OCCN2CCCCC2)cc1
ord_dataset-c2ad1656a3ca4d08888ffb6e3f3a2742
ord-eb82cfb403a14a159e26a2010c1cf21e
COC(=O)c1ccc(O)cc1.ClCCN1CCCCC1>>O=C(O)c1ccc(OCCN2CCCCC2)cc1
C([O-])([O-])=O.[K+].[K+].OC1=CC=C(C(=O)OC)C=C1.C(C)(=O)OCC.Cl.ClCCN1CCCCC1>>Cl.N1(CCCCC1)CCOC1=CC=C(C(=O)O)C=C1
C[O:4][C:3](=[O:2])[c:5]1[cH:6][cH:7][c:8]([OH:9])[cH:18][cH:19]1.Cl[CH2:10][CH2:11][N:12]1[CH2:13][CH2:14][CH2:15][CH2:16][CH2:17]1>>[O:2]=[C:3]([OH:4])[c:5]1[cH:6][cH:7][c:8]([O:9][CH2:10][CH2:11][N:12]2[CH2:13][CH2:14][CH2:15][CH2:16][CH2:17]2)[cH:18][cH:19]1
COC(=O)c1ccc(O)cc1.ClCCN1CCCCC1
O=C(O)c1ccc(OCCN2CCCCC2)cc1
null
null
O
Heteroatom Alkylation and Arylation
OtherReaction
c47049bacd28cc701f2e77df376a2fcefecd5392e081f9a62473cff265d23a8c
017337a0828c32d10d28543003ae15a8b492b5e2f69019c65a4461eabc617d95
c1ccc(OCCN2CCCCC2)cc1
C-[O;H0;D2;+0:1]-[C:2](=[O;D1;H0:3])-[c:4].[OH;D1;+0:5]-[c:6](:[c:7]):[c:8].Cl-[CH2;D2;+0:9]-[C:10]-[#7:11]>>[#7:11]-[C:10]-[CH2;D2;+0:9]-[O;H0;D2;+0:5]-[c:6](:[c:7]):[c:8].[O;D1;H0:3]=[C:2](-[OH;D1;+0:1])-[c:4]
null
[]
null
null
4
HOUR
To a 250 mL 3 neck flask with mechanical stirring and condenser, and a heating apparatus consisting of an RTD probe in the flask hooked via a temperature controller to a heating mantle and under nitrogen atmosphere, the following was added: 7.61 g of methyl 4-hydroxybenzoate, 11.05 g of β-chloroethylpiperidine hydrochl...
10.6084/m9.figshare.5104873.v1
null
Primary halide.Ester.Aromatic alcohol
Carboxylic acid.Ether
null
null
c1ccccc1.C1CC[NH]CC1
HCl
O
null
4
COC(=O)c1ccc(O)cc1.ClCCN1CCCCC1>O>O=C(O)c1ccc(OCCN2CCCCC2)cc1
ord_dataset-c2ad1656a3ca4d08888ffb6e3f3a2742
ord-8927131f18e74190aa3f19ad25d8e14b
COC(=O)c1ccc(O)cc1.ClCCN1CCCCC1>>O=C(O)c1ccc(OCCN2CCCCC2)cc1
C(C)(=O)OCCCCC.Cl.ClCCN1CCCCC1.C([O-])([O-])=O.[K+].[K+].OC1=CC=C(C(=O)OC)C=C1.OC1=CC=C(C(=O)OC)C=C1>>Cl.N1(CCCCC1)CCOC1=CC=C(C(=O)O)C=C1
C[O:4][C:3](=[O:2])[c:5]1[cH:6][cH:7][c:8]([OH:9])[cH:18][cH:19]1.Cl[CH2:10][CH2:11][N:12]1[CH2:13][CH2:14][CH2:15][CH2:16][CH2:17]1>>[O:2]=[C:3]([OH:4])[c:5]1[cH:6][cH:7][c:8]([O:9][CH2:10][CH2:11][N:12]2[CH2:13][CH2:14][CH2:15][CH2:16][CH2:17]2)[cH:18][cH:19]1
COC(=O)c1ccc(O)cc1.ClCCN1CCCCC1
O=C(O)c1ccc(OCCN2CCCCC2)cc1
null
null
O.CC(=O)C
Heteroatom Alkylation and Arylation
OtherReaction
c47049bacd28cc701f2e77df376a2fcefecd5392e081f9a62473cff265d23a8c
017337a0828c32d10d28543003ae15a8b492b5e2f69019c65a4461eabc617d95
c1ccc(OCCN2CCCCC2)cc1
C-[O;H0;D2;+0:1]-[C:2](=[O;D1;H0:3])-[c:4].[OH;D1;+0:5]-[c:6](:[c:7]):[c:8].Cl-[CH2;D2;+0:9]-[C:10]-[#7:11]>>[#7:11]-[C:10]-[CH2;D2;+0:9]-[O;H0;D2;+0:5]-[c:6](:[c:7]):[c:8].[O;D1;H0:3]=[C:2](-[OH;D1;+0:1])-[c:4]
null
[]
95
CELSIUS
null
null
To two 125 mL 3 neck flasks with mechanical stirring, condensers, and a heating apparatus consisting of an RTD probe in the flask hooked via a temperature controller to a heating mantle the following were added: 7.61 g of methyl 4-hydroxybenzoate, 11.05 g of β-chloroethylpiperidine hydrochloride, 16.59 g of powdered po...
10.6084/m9.figshare.5104873.v1
null
Primary halide.Ester.Aromatic alcohol
Carboxylic acid.Ether
null
null
c1ccccc1.C1CC[NH]CC1
HCl
O.CC(=O)C
95
null
COC(=O)c1ccc(O)cc1.ClCCN1CCCCC1>O.CC(=O)C>O=C(O)c1ccc(OCCN2CCCCC2)cc1
ord_dataset-c2ad1656a3ca4d08888ffb6e3f3a2742
ord-b190f2bf04fc450e98f6452e9e676dfb
COC(=O)c1ccc(O)cc1.ClCCN1CCCCC1>>O=C(O)c1ccc(OCCN2CCCCC2)cc1
OC1=CC=C(C(=O)OC)C=C1.C([O-])([O-])=O.[K+].[K+].Cl.ClCCN1CCCCC1>>Cl.N1(CCCCC1)CCOC1=CC=C(C(=O)O)C=C1
C[O:4][C:3](=[O:2])[c:5]1[cH:6][cH:7][c:8]([OH:9])[cH:18][cH:19]1.Cl[CH2:10][CH2:11][N:12]1[CH2:13][CH2:14][CH2:15][CH2:16][CH2:17]1>>[O:2]=[C:3]([OH:4])[c:5]1[cH:6][cH:7][c:8]([O:9][CH2:10][CH2:11][N:12]2[CH2:13][CH2:14][CH2:15][CH2:16][CH2:17]2)[cH:18][cH:19]1
COC(=O)c1ccc(O)cc1.ClCCN1CCCCC1
O=C(O)c1ccc(OCCN2CCCCC2)cc1
null
null
C(C)(=O)OCCCCC
Heteroatom Alkylation and Arylation
OtherReaction
c47049bacd28cc701f2e77df376a2fcefecd5392e081f9a62473cff265d23a8c
017337a0828c32d10d28543003ae15a8b492b5e2f69019c65a4461eabc617d95
c1ccc(OCCN2CCCCC2)cc1
C-[O;H0;D2;+0:1]-[C:2](=[O;D1;H0:3])-[c:4].[OH;D1;+0:5]-[c:6](:[c:7]):[c:8].Cl-[CH2;D2;+0:9]-[C:10]-[#7:11]>>[#7:11]-[C:10]-[CH2;D2;+0:9]-[O;H0;D2;+0:5]-[c:6](:[c:7]):[c:8].[O;D1;H0:3]=[C:2](-[OH;D1;+0:1])-[c:4]
91
[{"value": 91.0, "product": "Cl.N1(CCCCC1)CCOC1=CC=C(C(=O)O)C=C1", "details": "PERCENTYIELD", "is_desired": false}]
null
null
1
HOUR
To a 2000 gallon tank were added: 1320 L of amyl acetate, 167.42 kg of methyl 4-hydroxybenzoate, 408.6 kg of potassium carbonate, and 283.5 kg of β-chloroethylpiperidine hydrochloride. The mixture was heated to 120° C.-125° C. for 5 hours, at which time HPLC analysis indicated complete consumption of the methyl 4-hydro...
10.6084/m9.figshare.5104873.v1
null
Primary halide.Ester.Aromatic alcohol
Carboxylic acid.Ether
null
null
c1ccccc1.C1CC[NH]CC1
HCl
C(C)(=O)OCCCCC
null
1
COC(=O)c1ccc(O)cc1.ClCCN1CCCCC1>C(C)(=O)OCCCCC>O=C(O)c1ccc(OCCN2CCCCC2)cc1
ord_dataset-c2ad1656a3ca4d08888ffb6e3f3a2742
ord-8c764efa47ef4b9b8b9f366061dd03f4
CC(C)=O.COC(=O)c1ccco1>>CC(=O)CC(=O)c1ccco1
Cl.O1C(=CC=C1)C(=O)OC.[H-].[Na+].CC(=O)C>>O1C(=CC=C1)C(=O)CC(C)=O
[CH3:1][C:2](=[O:3])[CH3:4].CO[C:5](=[O:6])[c:7]1[cH:8][cH:9][cH:10][o:11]1>>[CH3:1][C:2](=[O:3])[CH2:4][C:5](=[O:6])[c:7]1[cH:8][cH:9][cH:10][o:11]1
CC(C)=O.COC(=O)c1ccco1
CC(=O)CC(=O)c1ccco1
null
null
C(C)OCC
C-C Coupling
OtherReaction
32688b2be78fcb1623f924ded4f1da30562c8a1cc17a29844013a0b12a85add5
da4745a356290ddd7ef0372302b86253afded9b0422422979166627a7dfa5740
c1ccoc1
C-O-[C;H0;D3;+0:1](=[O;D1;H0:2])-[c:3](:[c:4]):[#8;a:5]:[c:6].[C;D1;H3:7]-[C:8](-[CH3;D1;+0:9])=[O;D1;H0:10]>>[C;D1;H3:7]-[C:8](=[O;D1;H0:10])-[CH2;D2;+0:9]-[C;H0;D3;+0:1](=[O;D1;H0:2])-[c:3](:[c:4]):[#8;a:5]:[c:6]
99.6
[{"value": 99.0, "product": "O1C(=CC=C1)C(=O)CC(C)=O", "details": "PERCENTYIELD", "is_desired": false}, {"value": 99.6, "product": "O1C(=CC=C1)C(=O)CC(C)=O", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
null
null
4.27 ml (5.04 g, 40 mmol) methyl 2-furoate was added to a suspension of NaH (made from 3.83 g commercial NaH slurry by removal of the mineral oil with pentane) in 30 ml anhydrous diethyl ether. To this was added, so as to maintain the temperature below 30° C., 5.87 ml (4.64 g, 80 mmol) acetone (dried over CaCl2). This ...
10.6084/m9.figshare.5104873.v1
null
Ketone.Ester
Ketone.Ketone
null
null
c1ccoc1
HO-
C(C)OCC
null
null
CC(C)=O.COC(=O)c1ccco1>C(C)OCC>CC(=O)CC(=O)c1ccco1
ord_dataset-c2ad1656a3ca4d08888ffb6e3f3a2742
ord-0c22f013146b4803aae89fe7bf0b0ee4
CC(=O)CC(=O)c1ccco1.Cc1ccc(Nc2ccccc2C=O)cc1>>Cc1nc2ccccc2cc1C(=O)c1ccco1
C1(=CC=C(C=C1)NC1=C(C=O)C=CC=C1)C.O1C(=CC=C1)C(=O)CC(C)=O.N1CCCCC1>>O1C(=CC=C1)C(=O)C=1C(=NC2=CC=CC=C2C1)C
O=[C:2]([CH3:1])[CH2:11][C:12](=[O:13])[c:14]1[cH:15][cH:16][cH:17][o:18]1.Cc1ccc([NH:3][c:4]2[cH:5][cH:6][cH:7][cH:8][c:9]2[CH:10]=O)cc1>>[CH3:1][c:2]1[n:3][c:4]2[cH:5][cH:6][cH:7][cH:8][c:9]2[cH:10][c:11]1[C:12](=[O:13])[c:14]1[cH:15][cH:16][cH:17][o:18]1
CC(=O)CC(=O)c1ccco1.Cc1ccc(Nc2ccccc2C=O)cc1
Cc1nc2ccccc2cc1C(=O)c1ccco1
null
null
C(C)O
Miscellaneous
OtherReaction
2416acfd09007c1ea10369ce459296e913e809b309d191a5ebdcba6e94949c3d
70cdb026039ea0aa79cd465265ab660cd4e8b5ed67c3f66b3411348cb42687eb
O=C(c1cnc2ccccc2c1)c1ccco1
C-c1:c:c:c(-[NH;D2;+0:1]-[c:2](:[c:3]):[c:4](-[CH;D2;+0:5]=O):[c:6]):c:c:1.O=[C;H0;D3;+0:7](-[C;D1;H3:8])-[CH2;D2;+0:9]-[C:10](=[O;D1;H0:11])-[c:12]:[#8;a:13]>>[#8;a:13]:[c:12]-[C:10](=[O;D1;H0:11])-[c;H0;D3;+0:9]1:[cH;D2;+0:5]:[c:4](:[c:6]):[c:2](:[c:3]):[n;H0;D2;+0:1]:[c;H0;D3;+0:7]:1-[C;D1;H3:8]
77
[{"value": 77.0, "product": "O1C(=CC=C1)C(=O)C=1C(=NC2=CC=CC=C2C1)C", "details": "PERCENTYIELD", "is_desired": false}]
null
null
null
null
A solution of 410 mg (1.95 mmol) N-(p-tolyl)-o-aminobenzaldehyde 326 mg (2.15 mmol), (2-furoyl)acetone and 50 mg piperidine in 4 ml 95% ethanol was heated overnight under reflux. Removal of he volatile materials left a black, gummy oil which was taken up in dichloromethane and, after being washed with 3M NaOH, brine, a...
10.6084/m9.figshare.5104873.v1
null
Aldehyde.Ketone.Ketone.Secondary amine
Ketone
c1ccccc1.c1ccccc1
c1ccc2ncccc2c1
c1ccc2ncccc2c1.c1ccoc1
HO-
C(C)O
null
null
CC(=O)CC(=O)c1ccco1.Cc1ccc(Nc2ccccc2C=O)cc1>C(C)O>Cc1nc2ccccc2cc1C(=O)c1ccco1
ord_dataset-c2ad1656a3ca4d08888ffb6e3f3a2742
ord-9c207d102f3d43a682f5738fec76f3e0
COc1ccccc1C1(O)C(O)CC(c2ccccc2)(c2ccccc2)C2CN(Cc3ccccc3)CC21>>COc1ccccc1C1(O)C(O)CC(c2ccccc2)(c2ccccc2)C2CNCC21
C(C1=CC=CC=C1)N1CC2C(CC(C(C2C1)(O)C1=C(C=CC=C1)OC)O)(C1=CC=CC=C1)C1=CC=CC=C1>>C1(=CC=CC=C1)C1(CC(C(C2CNCC12)(O)C1=C(C=CC=C1)OC)O)C1=CC=CC=C1
c1ccc(C[N:29]2[CH2:28][CH:27]3[C:14]([c:15]4[cH:16][cH:17][cH:18][cH:19][cH:20]4)([c:21]4[cH:22][cH:23][cH:24][cH:25][cH:26]4)[CH2:13][CH:11]([OH:12])[C:9]([c:8]4[c:3]([O:2][CH3:1])[cH:4][cH:5][cH:6][cH:7]4)([OH:10])[CH:31]3[CH2:30]2)cc1>>[CH3:1][O:2][c:3]1[cH:4][cH:5][cH:6][cH:7][c:8]1[C:9]1([OH:10])[CH:11]([OH:12])[C...
COc1ccccc1C1(O)C(O)CC(c2ccccc2)(c2ccccc2)C2CN(Cc3ccccc3)CC21
COc1ccccc1C1(O)C(O)CC(c2ccccc2)(c2ccccc2)C2CNCC21
null
[OH-].[OH-].[Pd+2]
C(C)O
Deprotection
Hydrogenolysis of tertiary amines
253182af9e6c4683f8e32255be69a71cb32bcb9cb5d661b565d49a4d2de9a8bd
1c99dd446c0bf4ae872cd8df8de34955be195747c234e9f3c49f46d1de614f66
c1ccc(C2CCC(c3ccccc3)(c3ccccc3)C3CNCC23)cc1
C(-[N;H0;D3;+0:1]1-[C:2]-[C:3]-[C:4]-[C:5]-1)-c1:c:c:c:c:c:1>>[C:3]1-[C:2]-[NH;D2;+0:1]-[C:5]-[C:4]-1
null
[]
65
CELSIUS
null
null
A mixture of 2 g of (3aRS, 4RS, 5RS, 7aRS)-2-benzyl-7,7-diphenyl-4-(2-methoxyphenyl)perhydro-4,5-isoindolediol and 50 cm3 of ethanol is heated to 65° C. with stirring; 0.65 g of 20% palladium hydroxide on charcoal is added, and the reaction mixture is then hydrogenated, with stirring, at a temperature of 65° C. and at ...
10.6084/m9.figshare.5104873.v1
null
Tertiary amine
Secondary amine
c1ccccc1.C1CCC2C[NH]CC2C1
C1CCC2CNCC2C1
c1ccccc1.c1ccccc1.c1ccccc1.C1CCC2CNCC2C1
Other
[OH-].[OH-].[Pd+2].C(C)O
65
null
COc1ccccc1C1(O)C(O)CC(c2ccccc2)(c2ccccc2)C2CN(Cc3ccccc3)CC21>[OH-].[OH-].[Pd+2].C(C)O>COc1ccccc1C1(O)C(O)CC(c2ccccc2)(c2ccccc2)C2CNCC21
ord_dataset-c2ad1656a3ca4d08888ffb6e3f3a2742
ord-eedc028c8bdc4146bb046986c7c5d7a6
CC(=O)OC1CC(c2ccccc2)(c2ccccc2)C2CN(Cc3ccccc3)CC2C1=O.COc1cccc[c]1[Mg][Br]>>COc1ccccc1C1(O)C(O)CC(c2ccccc2)(c2ccccc2)C2CN(Cc3ccccc3)CC21
C(C)OCC.COC1=C(C=CC=C1)[Mg]Br.C(C)(=O)OC1C(C2CN(CC2C(C1)(C1=CC=CC=C1)C1=CC=CC=C1)CC1=CC=CC=C1)=O.[Cl-].[NH4+]>>C(C1=CC=CC=C1)N1CC2C(CC(C(C2C1)(O)C1=C(C=CC=C1)OC)O)(C1=CC=CC=C1)C1=CC=CC=C1
CC(=O)[O:12][CH:11]1[C:9](=[O:10])[CH:38]2[CH:27]([C:14]([c:15]3[cH:16][cH:17][cH:18][cH:19][cH:20]3)([c:21]3[cH:22][cH:23][cH:24][cH:25][cH:26]3)[CH2:13]1)[CH2:28][N:29]([CH2:30][c:31]1[cH:32][cH:33][cH:34][cH:35][cH:36]1)[CH2:37]2.[Br][Mg][c:8]1[c:3]([O:2][CH3:1])[cH:4][cH:5][cH:6][cH:7]1>>[CH3:1][O:2][c:3]1[cH:4][cH...
CC(=O)OC1CC(c2ccccc2)(c2ccccc2)C2CN(Cc3ccccc3)CC2C1=O.COc1cccc[c]1[Mg][Br]
COc1ccccc1C1(O)C(O)CC(c2ccccc2)(c2ccccc2)C2CN(Cc3ccccc3)CC21
null
null
O1CCCC1
C-C Coupling
OtherReaction
e498e00f826f84469c7f4f604736d37b54465d21893a5c4123d12c7de05ed650
f7598ae3e9675ec604d2c92cc3bb7b70ef88fca2d39aac1c01617ae9a7c5c226
c1ccc(CN2CC3C(c4ccccc4)CCC(c4ccccc4)(c4ccccc4)C3C2)cc1
C-C(=O)-[O;H0;D2;+0:1]-[C:2](-[C:3])-[C;H0;D3;+0:4](=[O;H0;D1;+0:5])-[C:6](-[C:7])-[C:8]-[#7:9].[#8:10]-[c:11](:[c:12]):[c;H0;D3;+0:13](-[Mg]-[Br]):[c:14]:[c:15]>>[#7:9]-[C:8]-[C:6](-[C:7])-[C;H0;D4;+0:4](-[OH;D1;+0:5])(-[c;H0;D3;+0:13](:[c:14]:[c:15]):[c:11](-[#8:10]):[c:12])-[C:2](-[OH;D1;+0:1])-[C:3]
64.8
[{"value": 64.8, "product": "C(C1=CC=CC=C1)N1CC2C(CC(C(C2C1)(O)C1=C(C=CC=C1)OC)O)(C1=CC=CC=C1)C1=CC=CC=C1", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
null
null
To a suspension of 84.4 g of 2-methoxyphenylmagnesium bromide in 1000 cm3 of tetrahydrofuran is added dropwise, at room temperature and with stirring, a solution of 22 g of (3aRS,5RS,7aRS)-5-acetoxy-2-benzyl-7,7-diphenylperhydro-4-isoindolone in 220 cm3 of tetrahydrofuran. The reaction mixture is stirred at room temper...
10.6084/m9.figshare.5104873.v1
null
Magnesium halide.Ketone.Ester
Secondary alcohol.Tertiary alcohol
C1CCC2C[NH]CC2C1.c1ccccc1
c1ccccc1.C1CCC2C[NH]CC2C1
c1ccccc1.c1ccccc1.c1ccccc1.C1CCC2C[NH]CC2C1.c1ccccc1
HBr.Mg
O1CCCC1
null
null
CC(=O)OC1CC(c2ccccc2)(c2ccccc2)C2CN(Cc3ccccc3)CC2C1=O.COc1cccc[c]1[Mg][Br]>O1CCCC1>COc1ccccc1C1(O)C(O)CC(c2ccccc2)(c2ccccc2)C2CN(Cc3ccccc3)CC21
ord_dataset-c2ad1656a3ca4d08888ffb6e3f3a2742
ord-913a6feed96a437ebd28023f775cac77
CC(=O)OC1CC(c2ccccc2)(c2ccccc2)C=CC1=O.CCCCOCN(Cc1ccccc1)C[Si](C)(C)C>>CC(=O)OC1CC(c2ccccc2)(c2ccccc2)C2CN(Cc3ccccc3)CC2C1=O
C(C)(=O)OC1CC(C=CC1=O)(C1=CC=CC=C1)C1=CC=CC=C1.C(CCC)OCN(C[Si](C)(C)C)CC1=CC=CC=C1.C([O-])([O-])=O.[Na+].[Na+]>>C(C)(=O)OC1C(C2CN(CC2C(C1)(C1=CC=CC=C1)C1=CC=CC=C1)CC1=CC=CC=C1)=O
[CH3:1][C:2](=[O:3])[O:4][CH:5]1[CH2:6][C:7]([c:8]2[cH:9][cH:10][cH:11][cH:12][cH:13]2)([c:14]2[cH:15][cH:16][cH:17][cH:18][cH:19]2)[CH:20]=[CH:31][C:32]1=[O:33].CCCCO[CH2:21][N:22]([CH2:23][c:24]1[cH:25][cH:26][cH:27][cH:28][cH:29]1)[CH2:30][Si](C)(C)C>>[CH3:1][C:2](=[O:3])[O:4][CH:5]1[CH2:6][C:7]([c:8]2[cH:9][cH:10][...
CC(=O)OC1CC(c2ccccc2)(c2ccccc2)C=CC1=O.CCCCOCN(Cc1ccccc1)C[Si](C)(C)C
CC(=O)OC1CC(c2ccccc2)(c2ccccc2)C2CN(Cc3ccccc3)CC2C1=O
null
FC(C(=O)O)(F)F
ClCCl
C-C Coupling
OtherReaction
afb1d7242d6e74cef85c96aa325bc405021655089e3bf824675e454b68d53365
03644a3196585e0d3367d533cc1c6d9c16aa98260b7b1ea5bb3a4b4e00da1fbe
O=C1CCC(c2ccccc2)(c2ccccc2)C2CN(Cc3ccccc3)CC12
C-C-C-C-O-[CH2;D2;+0:1]-[#7:2](-[C:3])-[CH2;D2;+0:4]-[Si](-C)(-C)-C.[O;D1;H0:5]=[C:6]1-[C:7]-[C:8]-[C:9](-[c:10])(-[c:11])-[CH;D2;+0:12]=[CH;D2;+0:13]-1>>[C:3]-[#7:2]1-[CH2;D2;+0:1]-[CH;D3;+0:12]2-[CH;D3;+0:13](-[CH2;D2;+0:4]-1)-[C:6](=[O;D1;H0:5])-[C:7]-[C:8]-[C:9]-2(-[c:10])-[c:11]
null
[]
null
null
15
HOUR
To a solution of 86 g of 6-acetoxy-4,4-diphenyl-2-cyclohexenone and 96 cm3 of N-butoxymethyl-N-(trimethylsilylmethyl)benzylamine in 1000 cm3 of dichloromethane are added 15 drops of trifluoroacetic acid. The reaction mixture is stirred at room temperature for 15 hours, followed by addition of 2 g of sodium carbonate an...
10.6084/m9.figshare.5104873.v1
null
Ketone.Ether.Silyl protective group
Ketone
C1=CCCCC1
C1CCC2C[NH]CC2C1
c1ccccc1.c1ccccc1.C1CCC2C[NH]CC2C1.c1ccccc1
HO-
FC(C(=O)O)(F)F.ClCCl
null
15
CC(=O)OC1CC(c2ccccc2)(c2ccccc2)C=CC1=O.CCCCOCN(Cc1ccccc1)C[Si](C)(C)C>FC(C(=O)O)(F)F.ClCCl>CC(=O)OC1CC(c2ccccc2)(c2ccccc2)C2CN(Cc3ccccc3)CC2C1=O
ord_dataset-c2ad1656a3ca4d08888ffb6e3f3a2742
ord-f85f73c50d104dee8e88300abae7d75d
CI.COc1ccccc1CC(=O)N1C(=O)O[C@@H](c2ccccc2)[C@@H]1C>>COc1ccccc1[C@H](C)C(=O)N1C(=O)O[C@@H](c2ccccc2)[C@@H]1C
C[C@@H]1N(C(O[C@H]1C1=CC=CC=C1)=O)C(CC1=C(C=CC=C1)OC)=O.CI>>C[C@@H]1N(C(O[C@H]1C1=CC=CC=C1)=O)C([C@@H](C)C1=C(C=CC=C1)OC)=O
I[CH3:10].[CH3:1][O:2][c:3]1[cH:4][cH:5][cH:6][cH:7][c:8]1[CH2:9][C:11](=[O:12])[N:13]1[C:14](=[O:15])[O:16][C@@H:17]([c:18]2[cH:19][cH:20][cH:21][cH:22][cH:23]2)[C@@H:24]1[CH3:25]>>[CH3:1][O:2][c:3]1[cH:4][cH:5][cH:6][cH:7][c:8]1[C@H:9]([CH3:10])[C:11](=[O:12])[N:13]1[C:14](=[O:15])[O:16][C@@H:17]([c:18]2[cH:19][cH:20...
CI.COc1ccccc1CC(=O)N1C(=O)O[C@@H](c2ccccc2)[C@@H]1C
COc1ccccc1[C@H](C)C(=O)N1C(=O)O[C@@H](c2ccccc2)[C@@H]1C
null
null
O1CCCC1.C(C)(=O)OCC
C-C Coupling
Methylation with MeI_secondary
0e09d968095a587418cca2841b1e4f096e8103de8fbb60e833faf1fb3df36a41
410ec9b1cc243569e4ff568c248f0b402403802e002b4018f576af3f6960507b
O=C(Cc1ccccc1)N1C[C@H](c2ccccc2)OC1=O
I-[CH3;D1;+0:1].[#8:2]-[C:3](=[O;D1;H0:4])-[#7:5](-[C:6](=[O;D1;H0:7])-[CH2;D2;+0:8]-[c:9](:[c:10]):[c:11])-[C:12]>>[#8:2]-[C:3](=[O;D1;H0:4])-[#7:5](-[C:6](=[O;D1;H0:7])-[C@@H;D3;+0:8](-[CH3;D1;+0:1])-[c:9](:[c:10]):[c:11])-[C:12]
null
[]
null
null
45
MINUTE
To a solution, cooled to -50° C., of 10 g of (4S,5S)-4-methyl-5-phenyl-3-[(2-methoxyphenyl)acetyl]-2-oxazolidinone in 150 cm3 of tetrahydrofuran are added 19.1 g of sodium 1,1,1,3,3,3-hexamethyldisilazide, and the mixture is stirred for 45 minutes at this temperature, followed by addition of 7.72 cm3 of methyl iodide. ...
10.6084/m9.figshare.5104873.v1
null
null
null
null
null
c1ccccc1.C1COC[NH]1.c1ccccc1
HI
O1CCCC1.C(C)(=O)OCC
null
0.75
CI.COc1ccccc1CC(=O)N1C(=O)O[C@@H](c2ccccc2)[C@@H]1C>O1CCCC1.C(C)(=O)OCC>COc1ccccc1[C@H](C)C(=O)N1C(=O)O[C@@H](c2ccccc2)[C@@H]1C
ord_dataset-c2ad1656a3ca4d08888ffb6e3f3a2742
ord-7f84790e52974f32a2309d5505a0da5c
COc1ccccc1CC(=O)O.C[C@@H]1NC(=O)O[C@H]1c1ccccc1>>COc1ccccc1CC(=O)N1C(=O)O[C@@H](c2ccccc2)[C@@H]1C
C(CCC)[Li].C[C@@H]1NC(O[C@H]1C1=CC=CC=C1)=O.CC(C)(C)C(=O)Cl.[Cl-].[NH4+].COC1=C(C=CC=C1)CC(=O)O.[H-].[Na+]>>C[C@@H]1N(C(O[C@H]1C1=CC=CC=C1)=O)C(CC1=C(C=CC=C1)OC)=O
O[C:10]([CH2:9][c:8]1[c:3]([O:2][CH3:1])[cH:4][cH:5][cH:6][cH:7]1)=[O:11].[NH:12]1[C:13](=[O:14])[O:15][C@@H:16]([c:17]2[cH:18][cH:19][cH:20][cH:21][cH:22]2)[C@@H:23]1[CH3:24]>>[CH3:1][O:2][c:3]1[cH:4][cH:5][cH:6][cH:7][c:8]1[CH2:9][C:10](=[O:11])[N:12]1[C:13](=[O:14])[O:15][C@@H:16]([c:17]2[cH:18][cH:19][cH:20][cH:21]...
COc1ccccc1CC(=O)O.C[C@@H]1NC(=O)O[C@H]1c1ccccc1
COc1ccccc1CC(=O)N1C(=O)O[C@@H](c2ccccc2)[C@@H]1C
null
null
O1CCCC1.CCCCCC.C(C)(=O)OCC
Protection
Acylation of Nitrogen Nucleophiles by Carboxylic Acids
e6b8877cb13581e7e20b3470e89734487d9fd6d7ab7fd08c61d6e2df594633e1
921ca845ddbf5a24a35d32f527510f05b226860d95f601c94808547d4fe20ceb
O=C(Cc1ccccc1)N1C[C@H](c2ccccc2)OC1=O
O-[C;H0;D3;+0:1](=[O;D1;H0:2])-[C:3]-[c:4].[C;D1;H3:5]-[C:6]1-[C:7]-[#8:8]-[C:9](=[O;D1;H0:10])-[NH;D2;+0:11]-1>>[C;D1;H3:5]-[C:6]1-[C:7]-[#8:8]-[C:9](=[O;D1;H0:10])-[N;H0;D3;+0:11]-1-[C;H0;D3;+0:1](=[O;D1;H0:2])-[C:3]-[c:4]
74.1
[{"value": 74.1, "product": "C[C@@H]1N(C(O[C@H]1C1=CC=CC=C1)=O)C(CC1=C(C=CC=C1)OC)=O", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
-30
CELSIUS
45
MINUTE
To a suspension of 1.89 g of sodium hydride (80% dispersion in petroleum jelly) in 200 cm3 of dry tetrahydrofuran are added at room temperature 9.38 g of 2-methoxyphenylacetic acid. This suspension is cooled to -30° C. and 7.77 cm3 of pivalolyl chloride are added, finally followed by addition of a solution cooled to -7...
10.6084/m9.figshare.5104873.v1
null
Carbamic ester.Carboxylic acid
Carbamic ester.Substituted dicarboximide
C1COCN1
C1COC[NH]1
c1ccccc1.C1COC[NH]1.c1ccccc1
HO-
O1CCCC1.CCCCCC.C(C)(=O)OCC
-30
0.75
COc1ccccc1CC(=O)O.C[C@@H]1NC(=O)O[C@H]1c1ccccc1>O1CCCC1.CCCCCC.C(C)(=O)OCC>COc1ccccc1CC(=O)N1C(=O)O[C@@H](c2ccccc2)[C@@H]1C
ord_dataset-c2ad1656a3ca4d08888ffb6e3f3a2742
ord-71e76fe394b94ca08d51895d1070f820
COc1ccccc1[C@@H](C)C(=O)O.COc1ccccc1[C@@]1(O)[C@H](O)CC(c2ccccc2)(c2ccccc2)[C@@H]2CNC[C@@H]21>>COc1ccccc1[C@@H](C)C(=O)N1C[C@@H]2[C@H](C1)[C@@](O)(c1ccccc1OC)[C@H](O)CC2(c1ccccc1)c1ccccc1
C1(=CC=CC=C1)C1(C[C@H]([C@]([C@H]2CNC[C@@H]12)(O)C1=C(C=CC=C1)OC)O)C1=CC=CC=C1.COC1=C(C=CC=C1)[C@H](C(=O)O)C>>C1(=CC=CC=C1)C1(C[C@H]([C@]([C@H]2CN(C[C@@H]12)C([C@H](C)C1=C(C=CC=C1)OC)=O)(O)C1=C(C=CC=C1)OC)O)C1=CC=CC=C1
O[C:11]([C@@H:9]([c:8]1[c:3]([O:2][CH3:1])[cH:4][cH:5][cH:6][cH:7]1)[CH3:10])=[O:12].[NH:13]1[CH2:14][C@@H:15]2[C@H:16]([CH2:17]1)[C@@:18]([OH:19])([c:20]1[cH:21][cH:22][cH:23][cH:24][c:25]1[O:26][CH3:27])[C@H:28]([OH:29])[CH2:30][C:31]2([c:32]1[cH:33][cH:34][cH:35][cH:36][cH:37]1)[c:38]1[cH:39][cH:40][cH:41][cH:42][cH...
COc1ccccc1[C@@H](C)C(=O)O.COc1ccccc1[C@@]1(O)[C@H](O)CC(c2ccccc2)(c2ccccc2)[C@@H]2CNC[C@@H]21
COc1ccccc1[C@@H](C)C(=O)N1C[C@@H]2[C@H](C1)[C@@](O)(c1ccccc1OC)[C@H](O)CC2(c1ccccc1)c1ccccc1
null
null
null
Acylation
Acylation of Nitrogen Nucleophiles by Carboxylic Acids
f47032714243d00bafcf35beb26606675da0e4fc72a54d2453dc571b1b03d871
c5e4172490b2731ba9322b68af56376edadc31ce0bb9a3dfdea23a1817a852fd
O=C(Cc1ccccc1)N1C[C@@H]2C(c3ccccc3)CCC(c3ccccc3)(c3ccccc3)[C@@H]2C1
O-[C;H0;D3;+0:1](=[O;D1;H0:2])-[C:3](-[C;D1;H3:4])-[c:5].[C:6]1-[C:7]-[C:8]-[C:9]-[NH;D2;+0:10]-1>>[C;D1;H3:4]-[C:3](-[c:5])-[C;H0;D3;+0:1](=[O;D1;H0:2])-[N;H0;D3;+0:10]1-[C:6]-[C:7]-[C:8]-[C:9]-1
43.2
[{"value": 43.2, "product": "C1(=CC=CC=C1)C1(C[C@H]([C@]([C@H]2CN(C[C@@H]12)C([C@H](C)C1=C(C=CC=C1)OC)=O)(O)C1=C(C=CC=C1)OC)O)C1=CC=CC=C1", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
null
null
By working according to the procedure of Example 1, starting from 0.2 g of (3aR,4R,5R,7aR)-7,7-diphenyl-4-(2-methoxyphenyl)perhydro-4,5-isoindolediol and 0.11 g of (R)-2-(2-methoxyphenyl) propionic acid, 0.12 g of (3aR,4R,5R,7aR)-7,7-diphenyl-4-(2-methoxyphenyl)-2-[(R)-2-(2-methoxyphenyl) propionyl]perhydro-4,5-isoindo...
10.6084/m9.figshare.5104873.v1
null
Carboxylic acid.Secondary amine
Tertiary amide
C1CC[C@H]2CNC[C@H]2C1
C1CC[C@H]2C[NH]C[C@H]2C1
c1ccccc1.c1ccccc1.C1CC[C@H]2C[NH]C[C@H]2C1.c1ccccc1.c1ccccc1
HO-
null
null
null
COc1ccccc1[C@@H](C)C(=O)O.COc1ccccc1[C@@]1(O)[C@H](O)CC(c2ccccc2)(c2ccccc2)[C@@H]2CNC[C@@H]21>>COc1ccccc1[C@@H](C)C(=O)N1C[C@@H]2[C@H](C1)[C@@](O)(c1ccccc1OC)[C@H](O)CC2(c1ccccc1)c1ccccc1
ord_dataset-c2ad1656a3ca4d08888ffb6e3f3a2742
ord-333a9cb6f4c44addbf85a8788cba6880
COc1ccccc1[C@@H](C)C(=O)N1C(=O)O[C@H](c2ccccc2)[C@H]1C.OO>>COc1ccccc1[C@@H](C)C(=O)O
S(=O)([O-])[O-].[Na+].[Na+].C[C@H]1N(C(O[C@@H]1C1=CC=CC=C1)=O)C([C@H](C)C1=C(C=CC=C1)OC)=O.[OH-].[Li+].OO>>COC1=C(C=CC=C1)[C@H](C(=O)O)C
C[C@@H]1[C@@H](c2ccccc2)OC(=O)N1[C:11]([C@@H:9]([c:8]1[c:3]([O:2][CH3:1])[cH:4][cH:5][cH:6][cH:7]1)[CH3:10])=[O:12].O[OH:13]>>[CH3:1][O:2][c:3]1[cH:4][cH:5][cH:6][cH:7][c:8]1[C@@H:9]([CH3:10])[C:11](=[O:12])[OH:13]
COc1ccccc1[C@@H](C)C(=O)N1C(=O)O[C@H](c2ccccc2)[C@H]1C.OO
COc1ccccc1[C@@H](C)C(=O)O
null
null
O1CCCC1.O
Acylation
OtherReaction
7fefc4011edcbe1dffc93611e6aa33ad6e04d8cda971cf8f87e37d90bd4136c7
e2c678181571c92a15078448ccb62575ef30480d579a3bf1599e99419fa7b1b3
c1ccccc1
C-[C@H]1-N(-[C;H0;D3;+0:1](=[O;D1;H0:2])-[C:3](-[C;D1;H3:4])-[c:5])-C(=O)-O-[C@@H]-1-c1:c:c:c:c:c:1.O-[OH;D1;+0:6]>>[C;D1;H3:4]-[C:3](-[c:5])-[C;H0;D3;+0:1](=[O;D1;H0:2])-[OH;D1;+0:6]
null
[]
null
null
3
HOUR
To a solution, cooled to +5° C., of 10.88 g of (4R, 5R)-4-methyl-5-phenyl-3-[(R)-2-(2-methoxyphenyl)propionyl]-2-oxazolidinone in 300 cm3 of tetrahydrofuran and 100 cm3 of water are added 2.71 g of lithium hydroxide and 13 cm3 of aqueous 30% hydrogen peroxide solution. The reaction mixture is stirred for 3 hours at thi...
10.6084/m9.figshare.5104873.v1
null
Carbamic ester.Ether.Substituted dicarboximide.Peroxide
Carboxylic acid
C1COCN1.c1ccccc1
null
c1ccccc1
HO-
O1CCCC1.O
null
3
COc1ccccc1[C@@H](C)C(=O)N1C(=O)O[C@H](c2ccccc2)[C@H]1C.OO>O1CCCC1.O>COc1ccccc1[C@@H](C)C(=O)O
ord_dataset-c2ad1656a3ca4d08888ffb6e3f3a2742
ord-4bd13a1ef22b4a92a19593e562a1264a
CI.COc1ccccc1CC(=O)N1C(=O)O[C@H](c2ccccc2)[C@H]1C>>COc1ccccc1[C@@H](C)C(=O)N1C(=O)O[C@H](c2ccccc2)[C@H]1C
C(C)(=O)O.C[C@H]1N(C(O[C@@H]1C1=CC=CC=C1)=O)C(CC1=C(C=CC=C1)OC)=O.CI>>C[C@H]1N(C(O[C@@H]1C1=CC=CC=C1)=O)C([C@H](C)C1=C(C=CC=C1)OC)=O
I[CH3:10].[CH3:1][O:2][c:3]1[cH:4][cH:5][cH:6][cH:7][c:8]1[CH2:9][C:11](=[O:12])[N:13]1[C:14](=[O:15])[O:16][C@H:17]([c:18]2[cH:19][cH:20][cH:21][cH:22][cH:23]2)[C@H:24]1[CH3:25]>>[CH3:1][O:2][c:3]1[cH:4][cH:5][cH:6][cH:7][c:8]1[C@@H:9]([CH3:10])[C:11](=[O:12])[N:13]1[C:14](=[O:15])[O:16][C@H:17]([c:18]2[cH:19][cH:20][...
CI.COc1ccccc1CC(=O)N1C(=O)O[C@H](c2ccccc2)[C@H]1C
COc1ccccc1[C@@H](C)C(=O)N1C(=O)O[C@H](c2ccccc2)[C@H]1C
null
null
O1CCCC1.C(C)(=O)OCC
C-C Coupling
Methylation with MeI_secondary
0e09d968095a587418cca2841b1e4f096e8103de8fbb60e833faf1fb3df36a41
410ec9b1cc243569e4ff568c248f0b402403802e002b4018f576af3f6960507b
O=C(Cc1ccccc1)N1C[C@@H](c2ccccc2)OC1=O
I-[CH3;D1;+0:1].[#8:2]-[C:3](=[O;D1;H0:4])-[#7:5](-[C:6](=[O;D1;H0:7])-[CH2;D2;+0:8]-[c:9](:[c:10]):[c:11])-[C:12]>>[#8:2]-[C:3](=[O;D1;H0:4])-[#7:5](-[C:6](=[O;D1;H0:7])-[C@H;D3;+0:8](-[CH3;D1;+0:1])-[c:9](:[c:10]):[c:11])-[C:12]
null
[]
null
null
45
MINUTE
To a solution, cooled to -50° C., of 22.82 g of (4R, 5R)-4-methyl-5-phenyl-3-[(2-methoxyphenyl)acetyl]-2-oxazolidinone in 190 cm3 of tetrahydrofuran are added 19.31 g of sodium 1,1,1,3,3,3-hexamethyldisilazide, and the mixture is stirred for 45 minutes at this temperature, followed by addition of 8.82 cm3 of methyl iod...
10.6084/m9.figshare.5104873.v1
null
null
null
null
null
c1ccccc1.C1COC[NH]1.c1ccccc1
HI
O1CCCC1.C(C)(=O)OCC
null
0.75
CI.COc1ccccc1CC(=O)N1C(=O)O[C@H](c2ccccc2)[C@H]1C>O1CCCC1.C(C)(=O)OCC>COc1ccccc1[C@@H](C)C(=O)N1C(=O)O[C@H](c2ccccc2)[C@H]1C
ord_dataset-c2ad1656a3ca4d08888ffb6e3f3a2742
ord-305680a96b9241db832c63f34167b873
COc1ccccc1CC(=O)O.C[C@H]1NC(=O)O[C@@H]1c1ccccc1>>COc1ccccc1CC(=O)N1C(=O)O[C@H](c2ccccc2)[C@H]1C
C[C@H]1NC(O[C@@H]1C1=CC=CC=C1)=O.[Cl-].[NH4+].C(CCC)[Li].COC1=C(C=CC=C1)CC(=O)O>>C[C@H]1N(C(O[C@@H]1C1=CC=CC=C1)=O)C(CC1=C(C=CC=C1)OC)=O
O[C:10]([CH2:9][c:8]1[c:3]([O:2][CH3:1])[cH:4][cH:5][cH:6][cH:7]1)=[O:11].[NH:12]1[C:13](=[O:14])[O:15][C@H:16]([c:17]2[cH:18][cH:19][cH:20][cH:21][cH:22]2)[C@H:23]1[CH3:24]>>[CH3:1][O:2][c:3]1[cH:4][cH:5][cH:6][cH:7][c:8]1[CH2:9][C:10](=[O:11])[N:12]1[C:13](=[O:14])[O:15][C@H:16]([c:17]2[cH:18][cH:19][cH:20][cH:21][cH...
COc1ccccc1CC(=O)O.C[C@H]1NC(=O)O[C@@H]1c1ccccc1
COc1ccccc1CC(=O)N1C(=O)O[C@H](c2ccccc2)[C@H]1C
null
null
O1CCCC1.CCCCCC.C(C)(=O)OCC
Protection
Acylation of Nitrogen Nucleophiles by Carboxylic Acids
e6b8877cb13581e7e20b3470e89734487d9fd6d7ab7fd08c61d6e2df594633e1
921ca845ddbf5a24a35d32f527510f05b226860d95f601c94808547d4fe20ceb
O=C(Cc1ccccc1)N1C[C@@H](c2ccccc2)OC1=O
O-[C;H0;D3;+0:1](=[O;D1;H0:2])-[C:3]-[c:4].[C;D1;H3:5]-[C:6]1-[C:7]-[#8:8]-[C:9](=[O;D1;H0:10])-[NH;D2;+0:11]-1>>[C;D1;H3:5]-[C:6]1-[C:7]-[#8:8]-[C:9](=[O;D1;H0:10])-[N;H0;D3;+0:11]-1-[C;H0;D3;+0:1](=[O;D1;H0:2])-[C:3]-[c:4]
null
[]
null
null
30
MINUTE
To a solution of 27.4 g of (4R,5R)-4-methyl-5-phenyl-2-oxazolidinone in 200 cm3 of dry tetrahydrofuran are added, at -78° C., 100 cm3 of a 1.6M butyllithium solution in hexane, followed by addition of 33.12 g of a solution of 2-methoxyphenylacetic acid in 30 cm3 of tetrahydrofuran. The mixture is stirred for 30 minutes...
10.6084/m9.figshare.5104873.v1
null
Carbamic ester.Carboxylic acid
Carbamic ester.Substituted dicarboximide
C1COCN1
C1COC[NH]1
c1ccccc1.C1COC[NH]1.c1ccccc1
HO-
O1CCCC1.CCCCCC.C(C)(=O)OCC
null
0.5
COc1ccccc1CC(=O)O.C[C@H]1NC(=O)O[C@@H]1c1ccccc1>O1CCCC1.CCCCCC.C(C)(=O)OCC>COc1ccccc1CC(=O)N1C(=O)O[C@H](c2ccccc2)[C@H]1C
ord_dataset-c2ad1656a3ca4d08888ffb6e3f3a2742
ord-50951ff0bd514fd4ae9a987c41fc417e
COc1ccccc1[C@@]1(O)C(O)CC(c2ccccc2)(c2ccccc2)[C@@H]2CN(C(=O)Cc3ccccc3OCc3ccccc3)C[C@@H]21>>COc1ccccc1[C@@]1(O)[C@H](O)CC(c2ccccc2)(c2ccccc2)[C@@H]2CN(C(=O)Cc3ccccc3O)C[C@@H]21
C1(=CC=CC=C1)C1(CC([C@]([C@H]2CN(C[C@@H]12)C(CC1=C(C=CC=C1)OCC1=CC=CC=C1)=O)(O)C1=C(C=CC=C1)OC)O)C1=CC=CC=C1>>C1(=CC=CC=C1)C1(C[C@H]([C@]([C@H]2CN(C[C@@H]12)C(CC1=C(C=CC=C1)O)=O)(O)C1=C(C=CC=C1)OC)O)C1=CC=CC=C1
c1ccc(C[O:39][c:38]2[c:33]([CH2:32][C:30]([N:29]3[CH2:28][C@H:27]4[C:14]([c:15]5[cH:16][cH:17][cH:18][cH:19][cH:20]5)([c:21]5[cH:22][cH:23][cH:24][cH:25][cH:26]5)[CH2:13][CH:11]([OH:12])[C@@:9]([c:8]5[c:3]([O:2][CH3:1])[cH:4][cH:5][cH:6][cH:7]5)([OH:10])[C@H:41]4[CH2:40]3)=[O:31])[cH:34][cH:35][cH:36][cH:37]2)cc1>>[CH3...
COc1ccccc1[C@@]1(O)C(O)CC(c2ccccc2)(c2ccccc2)[C@@H]2CN(C(=O)Cc3ccccc3OCc3ccccc3)C[C@@H]21
COc1ccccc1[C@@]1(O)[C@H](O)CC(c2ccccc2)(c2ccccc2)[C@@H]2CN(C(=O)Cc3ccccc3O)C[C@@H]21
null
[OH-].[OH-].[Pd+2]
C(C)O
Deprotection
Hydroxyl benzyl deprotection
36869d1fe85185a14d9eb30bf05178c600a9b6eca277ffaf3803578c30e0bf5d
26a36596df80ec137b0e8087297418351c93c32819177f680675220622f215d4
O=C(Cc1ccccc1)N1C[C@@H]2C(c3ccccc3)CCC(c3ccccc3)(c3ccccc3)[C@@H]2C1
[c:1]:[c:2](-[O;H0;D2;+0:3]-C-c1:c:c:c:c:c:1):[c:4]>>[OH;D1;+0:3]-[c:2](:[c:1]):[c:4]
84.6
[{"value": 84.6, "product": "C1(=CC=CC=C1)C1(C[C@H]([C@]([C@H]2CN(C[C@@H]12)C(CC1=C(C=CC=C1)O)=O)(O)C1=C(C=CC=C1)OC)O)C1=CC=CC=C1", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
60
CELSIUS
null
null
A mixture of 1.5 g of (3aR,4R, SR,7aR)-7,7-diphenyl-4-(2-methoxyphenyl)-2-[(2-benzyloxyphenyl)acetyl]perhydro-4,5-isoindolediol and 50 cm3 of ethanol is heated to 60° C. with stirring; 0.5 g of 20% palladium hydroxide on charcoal is added and the reaction mixture is then hydrogenated, with stirring, at a temperature of...
10.6084/m9.figshare.5104873.v1
null
Ether
Aromatic alcohol
c1ccccc1
null
c1ccccc1.c1ccccc1.c1ccccc1.C1CC[C@H]2C[NH]C[C@H]2C1.c1ccccc1
Other
[OH-].[OH-].[Pd+2].C(C)O
60
null
COc1ccccc1[C@@]1(O)C(O)CC(c2ccccc2)(c2ccccc2)[C@@H]2CN(C(=O)Cc3ccccc3OCc3ccccc3)C[C@@H]21>[OH-].[OH-].[Pd+2].C(C)O>COc1ccccc1[C@@]1(O)[C@H](O)CC(c2ccccc2)(c2ccccc2)[C@@H]2CN(C(=O)Cc3ccccc3O)C[C@@H]21
ord_dataset-c2ad1656a3ca4d08888ffb6e3f3a2742
ord-fb44ceafc3a5487c9f4702671fd25908
COc1ccccc1C1(O)C(O)CC(c2ccccc2)(c2ccccc2)C2CNCC21.O=C(Cl)Cc1ccc2ccccc2c1>>COc1ccccc1C1(O)C(O)CC(c2ccccc2)(c2ccccc2)C2CN(C(=O)Cc3ccc4ccccc4c3)CC21
O.C1=C(C=CC2=CC=CC=C12)CC(=O)Cl.C1(=CC=CC=C1)C1(CC(C(C2CNCC12)(O)C1=C(C=CC=C1)OC)O)C1=CC=CC=C1.C(C)(C)N(CC)C(C)C>>C1(=CC=CC=C1)C1(CC(C(C2CN(CC12)C(CC1=CC2=CC=CC=C2C=C1)=O)(O)C1=C(C=CC=C1)OC)O)C1=CC=CC=C1
[CH3:1][O:2][c:3]1[cH:4][cH:5][cH:6][cH:7][c:8]1[C:9]1([OH:10])[CH:11]([OH:12])[CH2:13][C:14]([c:15]2[cH:16][cH:17][cH:18][cH:19][cH:20]2)([c:21]2[cH:22][cH:23][cH:24][cH:25][cH:26]2)[CH:27]2[CH2:28][NH:29][CH2:43][CH:44]12.Cl[C:30](=[O:31])[CH2:32][c:33]1[cH:34][cH:35][c:36]2[cH:37][cH:38][cH:39][cH:40][c:41]2[cH:42]1...
COc1ccccc1C1(O)C(O)CC(c2ccccc2)(c2ccccc2)C2CNCC21.O=C(Cl)Cc1ccc2ccccc2c1
COc1ccccc1C1(O)C(O)CC(c2ccccc2)(c2ccccc2)C2CN(C(=O)Cc3ccc4ccccc4c3)CC21
null
null
ClCCl
Acylation
N-alkylation of secondary amines with alkyl halides
75017718c2fd505eefc84a6034d3d2fb46ceb0888a163173531a82534493cc96
96cb0a2fed10552c5770a45a2d6523b47ac3e38928b4a9c698d8577451182dcd
O=C(Cc1ccc2ccccc2c1)N1CC2C(c3ccccc3)CCC(c3ccccc3)(c3ccccc3)C2C1
Cl-[C;H0;D3;+0:1](=[O;D1;H0:2])-[C:3]-[c:4].[C:5]1-[C:6]-[NH;D2;+0:7]-[C:8]-[C:9]-1>>[O;D1;H0:2]=[C;H0;D3;+0:1](-[C:3]-[c:4])-[N;H0;D3;+0:7]1-[C:6]-[C:5]-[C:9]-[C:8]-1
50.8
[{"value": 50.8, "product": "C1(=CC=CC=C1)C1(CC(C(C2CN(CC12)C(CC1=CC2=CC=CC=C2C=C1)=O)(O)C1=C(C=CC=C1)OC)O)C1=CC=CC=C1", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
1
HOUR
To a solution of 0.42 g of (3aRS,4RS,5RS,7aRS)-7,7-diphenyl-4-(2-methoxyphenyl)perhydro-4,5-isoindolediol in 10 cm3 of dichloromethane is added 0.21 cm3 of diisopropylethylamine, followed by 0.23 g of 2-naphthylacetyl chloride in 5.5 cm3 of dichloromethane. After stirring at room temperature for 1 hour, 25 cm3 of water...
10.6084/m9.figshare.5104873.v1
null
Acyl halide.Secondary amine
Tertiary amide
C1CCC2CNCC2C1
C1CCC2C[NH]CC2C1
c1ccccc1.c1ccccc1.c1ccccc1.C1CCC2C[NH]CC2C1.c1ccc2ccccc2c1
HCl
ClCCl
null
1
COc1ccccc1C1(O)C(O)CC(c2ccccc2)(c2ccccc2)C2CNCC21.O=C(Cl)Cc1ccc2ccccc2c1>ClCCl>COc1ccccc1C1(O)C(O)CC(c2ccccc2)(c2ccccc2)C2CN(C(=O)Cc3ccc4ccccc4c3)CC21
ord_dataset-c2ad1656a3ca4d08888ffb6e3f3a2742
ord-f702a20ae3d74a158601fb61cb6aa32b
COc1ccccc1C1(O)C(O)CC(c2ccccc2)(c2ccccc2)C2CNCC21.O=C(Cl)Cc1cccc2ccccc12>>COc1ccccc1C1(O)C(O)CC(c2ccccc2)(c2ccccc2)C2CN(C(=O)Cc3cccc4ccccc34)CC21
C1(=CC=CC=C1)C1(CC(C(C2CNCC12)(O)C1=C(C=CC=C1)OC)O)C1=CC=CC=C1.C1(=CC=CC2=CC=CC=C12)CC(=O)Cl>>C1(=CC=CC=C1)C1(CC(C(C2CN(CC12)C(CC1=CC=CC2=CC=CC=C12)=O)(O)C1=C(C=CC=C1)OC)O)C1=CC=CC=C1
[CH3:1][O:2][c:3]1[cH:4][cH:5][cH:6][cH:7][c:8]1[C:9]1([OH:10])[CH:11]([OH:12])[CH2:13][C:14]([c:15]2[cH:16][cH:17][cH:18][cH:19][cH:20]2)([c:21]2[cH:22][cH:23][cH:24][cH:25][cH:26]2)[CH:27]2[CH2:28][NH:29][CH2:43][CH:44]12.Cl[C:30](=[O:31])[CH2:32][c:33]1[cH:34][cH:35][cH:36][c:37]2[cH:38][cH:39][cH:40][cH:41][c:42]12...
COc1ccccc1C1(O)C(O)CC(c2ccccc2)(c2ccccc2)C2CNCC21.O=C(Cl)Cc1cccc2ccccc12
COc1ccccc1C1(O)C(O)CC(c2ccccc2)(c2ccccc2)C2CN(C(=O)Cc3cccc4ccccc34)CC21
null
null
null
Acylation
N-alkylation of secondary amines with alkyl halides
75017718c2fd505eefc84a6034d3d2fb46ceb0888a163173531a82534493cc96
96cb0a2fed10552c5770a45a2d6523b47ac3e38928b4a9c698d8577451182dcd
O=C(Cc1cccc2ccccc12)N1CC2C(c3ccccc3)CCC(c3ccccc3)(c3ccccc3)C2C1
Cl-[C;H0;D3;+0:1](=[O;D1;H0:2])-[C:3]-[c:4].[C:5]1-[C:6]-[NH;D2;+0:7]-[C:8]-[C:9]-1>>[O;D1;H0:2]=[C;H0;D3;+0:1](-[C:3]-[c:4])-[N;H0;D3;+0:7]1-[C:6]-[C:5]-[C:9]-[C:8]-1
45.9
[{"value": 45.9, "product": "C1(=CC=CC=C1)C1(CC(C(C2CN(CC12)C(CC1=CC=CC2=CC=CC=C12)=O)(O)C1=C(C=CC=C1)OC)O)C1=CC=CC=C1", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
null
null
By working according to the procedure of Example A, starting from 0.62 g of (3aRS,4RS,5RS,7aRS)-7,7-diphenyl-4-(2-methoxyphenyl)perhydro-4,5-isoindolediol and 0.35 g of 1-naphthylacetyl chloride, 0.4 g of (3aRS,4RS,5RS,7aRS)-7,7-diphenyl-4-(2methoxyphenyl)-2-[(1-naphthyl)acetyl]perhydro-4,5-isoindolediol is obtained, m...
10.6084/m9.figshare.5104873.v1
null
Acyl halide.Secondary amine
Tertiary amide
C1CCC2CNCC2C1
C1CCC2C[NH]CC2C1
c1ccccc1.c1ccccc1.c1ccccc1.C1CCC2C[NH]CC2C1.c1ccc2ccccc2c1
HCl
null
null
null
COc1ccccc1C1(O)C(O)CC(c2ccccc2)(c2ccccc2)C2CNCC21.O=C(Cl)Cc1cccc2ccccc12>>COc1ccccc1C1(O)C(O)CC(c2ccccc2)(c2ccccc2)C2CN(C(=O)Cc3cccc4ccccc34)CC21
ord_dataset-c2ad1656a3ca4d08888ffb6e3f3a2742
ord-3a7d3fcf84904af89b0162e8dcc4e243
COc1ccccc1C1(O)C(O)CC(c2ccccc2)(c2ccccc2)C2CNCC21.COc1ccccc1CC(=O)O>>COc1ccccc1CC(=O)C1NCC2C1C(c1ccccc1)(c1ccccc1)CC(O)C2(O)c1ccccc1OC
Cl.C1(=CC=CC=C1)C1(CC(C(C2CNCC12)(O)C1=C(C=CC=C1)OC)O)C1=CC=CC=C1.C(C)N(CC)CC.COC1=C(C=CC=C1)CC(=O)O>>C1(=CC=CC=C1)C1(CC(C(C2CNC(C12)C(CC1=C(C=CC=C1)OC)=O)(O)C1=C(C=CC=C1)OC)O)C1=CC=CC=C1
[CH2:12]1[NH:13][CH2:14][CH:15]2[CH:16]1[C:17]([c:18]1[cH:19][cH:20][cH:21][cH:22][cH:23]1)([c:24]1[cH:25][cH:26][cH:27][cH:28][cH:29]1)[CH2:30][CH:31]([OH:32])[C:33]2([OH:34])[c:35]1[cH:36][cH:37][cH:38][cH:39][c:40]1[O:41][CH3:42].O[C:10]([CH2:9][c:8]1[c:3]([O:2][CH3:1])[cH:4][cH:5][cH:6][cH:7]1)=[O:11]>>[CH3:1][O:2]...
COc1ccccc1C1(O)C(O)CC(c2ccccc2)(c2ccccc2)C2CNCC21.COc1ccccc1CC(=O)O
COc1ccccc1CC(=O)C1NCC2C1C(c1ccccc1)(c1ccccc1)CC(O)C2(O)c1ccccc1OC
null
null
ClCCl
C-C Coupling
OtherReaction
348f28eb1206b1d8c46913f3c2a9e136a52e67dd0c5f883196b7d72ab51b799d
a49756d2995b35bf1c4b6840928f031562470ef5bd676447fb43ce2575147daa
O=C(Cc1ccccc1)C1NCC2C(c3ccccc3)CCC(c3ccccc3)(c3ccccc3)C12
O-[C;H0;D3;+0:1](=[O;D1;H0:2])-[C:3]-[c:4].[C:5]-[C:6]1-[C:7]-[C:8]-[#7:9]-[CH2;D2;+0:10]-1>>[C:5]-[C:6]1-[C:7]-[C:8]-[#7:9]-[CH;D3;+0:10]-1-[C;H0;D3;+0:1](=[O;D1;H0:2])-[C:3]-[c:4]
77.5
[{"value": 77.5, "product": "C1(=CC=CC=C1)C1(CC(C(C2CNC(C12)C(CC1=C(C=CC=C1)OC)=O)(O)C1=C(C=CC=C1)OC)O)C1=CC=CC=C1", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
90
MINUTE
To a solution of 4.5 g of (3aRS,4RS,5RS,7aRS)-7,7-diphenyl-4-(2-methoxyphenyl)perhydro-4,5-isoindolediol hydrochloride in 100 cm3 of dichloromethane, cooled to 0° C., are added 4.2 cm3 of triethylamine, followed by 2.4 g of (2-methoxyphenyl)acetic acid in 50 cm3 of dichloromethane. Stirring is carried out at room tempe...
10.6084/m9.figshare.5104873.v1
null
Carboxylic acid
Ketone
C1CCC2CNCC2C1
C1CCC2CNCC2C1
c1ccccc1.c1ccccc1.c1ccccc1.C1CCC2CNCC2C1.c1ccccc1
HO-
ClCCl
null
1.5
COc1ccccc1C1(O)C(O)CC(c2ccccc2)(c2ccccc2)C2CNCC21.COc1ccccc1CC(=O)O>ClCCl>COc1ccccc1CC(=O)C1NCC2C1C(c1ccccc1)(c1ccccc1)CC(O)C2(O)c1ccccc1OC
ord_dataset-c2ad1656a3ca4d08888ffb6e3f3a2742
ord-cd22a7b3952a4e9c87a905c978cab9b6
COc1ccccc1C1(O)C(O)CC(c2ccccc2)(c2ccccc2)C2CNCC21.O=C(O)Cc1ccccc1N1CCCC1>>COc1ccccc1C1(O)C(O)CC(c2ccccc2)(c2ccccc2)C2CN(C(=O)Cc3ccccc3N3CCCC3)CC21
C1(=CC=CC=C1)C1(CC(C(C2CNCC12)(O)C1=C(C=CC=C1)OC)O)C1=CC=CC=C1.N1(CCCC1)C1=C(C=CC=C1)CC(=O)O>>C1(=CC=CC=C1)C1(CC(C(C2CN(CC12)C(CC1=C(C=CC=C1)N1CCCC1)=O)(O)C1=C(C=CC=C1)OC)O)C1=CC=CC=C1
[CH3:1][O:2][c:3]1[cH:4][cH:5][cH:6][cH:7][c:8]1[C:9]1([OH:10])[CH:11]([OH:12])[CH2:13][C:14]([c:15]2[cH:16][cH:17][cH:18][cH:19][cH:20]2)([c:21]2[cH:22][cH:23][cH:24][cH:25][cH:26]2)[CH:27]2[CH2:28][NH:29][CH2:44][CH:45]12.O[C:30](=[O:31])[CH2:32][c:33]1[cH:34][cH:35][cH:36][cH:37][c:38]1[N:39]1[CH2:40][CH2:41][CH2:42...
COc1ccccc1C1(O)C(O)CC(c2ccccc2)(c2ccccc2)C2CNCC21.O=C(O)Cc1ccccc1N1CCCC1
COc1ccccc1C1(O)C(O)CC(c2ccccc2)(c2ccccc2)C2CN(C(=O)Cc3ccccc3N3CCCC3)CC21
null
null
null
Acylation
Acylation of Nitrogen Nucleophiles by Carboxylic Acids
2457854ffd9a54613a67a643011206ed6317d3a06f087c446877d03b7cda3988
c5e4172490b2731ba9322b68af56376edadc31ce0bb9a3dfdea23a1817a852fd
O=C(Cc1ccccc1N1CCCC1)N1CC2C(c3ccccc3)CCC(c3ccccc3)(c3ccccc3)C2C1
O-[C;H0;D3;+0:1](=[O;D1;H0:2])-[C:3]-[c:4].[C:5]1-[C:6]-[NH;D2;+0:7]-[C:8]-[C:9]-1>>[O;D1;H0:2]=[C;H0;D3;+0:1](-[C:3]-[c:4])-[N;H0;D3;+0:7]1-[C:6]-[C:5]-[C:9]-[C:8]-1
77.8
[{"value": 77.8, "product": "C1(=CC=CC=C1)C1(CC(C(C2CN(CC12)C(CC1=C(C=CC=C1)N1CCCC1)=O)(O)C1=C(C=CC=C1)OC)O)C1=CC=CC=C1", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
null
null
By working according to the procedure of Example 1, starting from 0.62 g of (3aRS,4RS,5RS,7aRS)-7,7-diphenyl-4-(2-methoxyphenyl)perhydro-4,5-isoindolediol and 0.40 g of 2-(1-pyrrolidinyl)phenylacetic acid, 0.70 g of (3aRS,4RS,5RS,7aRS)-7,7-diphenyl-4-(2-methoxyphenyl)-2-[(2-(1-pyrrolidinyl)phenyl)acetyl]perhydro-4,5-is...
10.6084/m9.figshare.5104873.v1
null
Carboxylic acid.Secondary amine
Tertiary amide
C1CCC2CNCC2C1
C1CCC2C[NH]CC2C1
c1ccccc1.c1ccccc1.c1ccccc1.C1CCC2C[NH]CC2C1.c1ccccc1.C1CC[NH]C1
HO-
null
null
null
COc1ccccc1C1(O)C(O)CC(c2ccccc2)(c2ccccc2)C2CNCC21.O=C(O)Cc1ccccc1N1CCCC1>>COc1ccccc1C1(O)C(O)CC(c2ccccc2)(c2ccccc2)C2CN(C(=O)Cc3ccccc3N3CCCC3)CC21
ord_dataset-c2ad1656a3ca4d08888ffb6e3f3a2742
ord-ebb6dfc4c437444cbe1e002b13554768
COc1ccccc1C1(O)C(O)CC(c2ccccc2)(c2ccccc2)C2CN(C(=O)Cc3ccc([N+](=O)[O-])cc3)CC21>>COc1ccccc1C1(O)C(O)CC(c2ccccc2)(c2ccccc2)C2CN(C(=O)Cc3ccc(N)cc3)CC21
O.[Cl-].[NH4+].C1(=CC=CC=C1)C1(CC(C(C2CN(CC12)C(CC1=CC=C(C=C1)[N+](=O)[O-])=O)(O)C1=C(C=CC=C1)OC)O)C1=CC=CC=C1>>C1(=CC=CC=C1)C1(CC(C(C2CN(CC12)C(CC1=CC=C(C=C1)N)=O)(O)C1=C(C=CC=C1)OC)O)C1=CC=CC=C1
O=[N+:37]([O-])[c:36]1[cH:35][cH:34][c:33]([CH2:32][C:30]([N:29]2[CH2:28][CH:27]3[C:14]([c:15]4[cH:16][cH:17][cH:18][cH:19][cH:20]4)([c:21]4[cH:22][cH:23][cH:24][cH:25][cH:26]4)[CH2:13][CH:11]([OH:12])[C:9]([c:8]4[c:3]([O:2][CH3:1])[cH:4][cH:5][cH:6][cH:7]4)([OH:10])[CH:41]3[CH2:40]2)=[O:31])[cH:39][cH:38]1>>[CH3:1][O:...
COc1ccccc1C1(O)C(O)CC(c2ccccc2)(c2ccccc2)C2CN(C(=O)Cc3ccc([N+](=O)[O-])cc3)CC21
COc1ccccc1C1(O)C(O)CC(c2ccccc2)(c2ccccc2)C2CN(C(=O)Cc3ccc(N)cc3)CC21
null
[Zn]
CO
Reduction
Reduction of nitro groups to amines
bbc242b150a51e69d3ad1caaa391f4422710431b398dcb880555f476706790be
7b0317532ea57a4fcedc1efc3e3c22eb5238d1c8330da53d4f9801fc2391f567
O=C(Cc1ccccc1)N1CC2C(c3ccccc3)CCC(c3ccccc3)(c3ccccc3)C2C1
O=[N+;H0;D3:1](-[O-])-[c:2](:[c:3]):[c:4]>>[NH2;D1;+0:1]-[c:2](:[c:3]):[c:4]
74.9
[{"value": 74.9, "product": "C1(=CC=CC=C1)C1(CC(C(C2CN(CC12)C(CC1=CC=C(C=C1)N)=O)(O)C1=C(C=CC=C1)OC)O)C1=CC=CC=C1", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
null
null
To a solution of 1 g of (3aRS,4RS,5RS,7aRS)-7,7-diphenyl-4-(2-methoxyphenyl)-2-[(4-nitrophenyl)acetyl]perhydro-4,5-isoindolediol in 3.3 cm3 of methanol, maintained at a temperature of 50° C., are added 33 cm3 of water, 4.6 g of ammonium chloride and 2.2 g of zinc powder. The reaction mixture is brought to reflux for 30...
10.6084/m9.figshare.5104873.v1
null
Nitro group
Primary amine
null
null
c1ccccc1.c1ccccc1.c1ccccc1.C1CCC2C[NH]CC2C1.c1ccccc1
Other
[Zn].CO
null
null
COc1ccccc1C1(O)C(O)CC(c2ccccc2)(c2ccccc2)C2CN(C(=O)Cc3ccc([N+](=O)[O-])cc3)CC21>[Zn].CO>COc1ccccc1C1(O)C(O)CC(c2ccccc2)(c2ccccc2)C2CN(C(=O)Cc3ccc(N)cc3)CC21
ord_dataset-c2ad1656a3ca4d08888ffb6e3f3a2742
ord-7b3d35f9eec5401abafe481d8cf02aaf
C=C(Cl)C#N.N#CC(NC(=O)C(F)(F)F)c1ccc(Cl)cc1>>N#Cc1cc(C(F)(F)F)[nH]c1-c1ccc(Cl)cc1
ClC(C#N)=C.ClC1=CC=C(C=C1)C(NC(C(F)(F)F)=O)C#N.CS(=O)(=O)O.C(C)(=O)Cl.C(C)N(CC)CC>>ClC1=CC=C(C=C1)C=1NC(=CC1C#N)C(F)(F)F
ClC([C:2]#[N:1])=[CH2:4].N#[C:3][CH:11]([NH:10][C:5](=O)[C:6]([F:7])([F:8])[F:9])[c:12]1[cH:13][cH:14][c:15]([Cl:16])[cH:17][cH:18]1>>[N:1]#[C:2][c:3]1[cH:4][c:5]([C:6]([F:7])([F:8])[F:9])[nH:10][c:11]1-[c:12]1[cH:13][cH:14][c:15]([Cl:16])[cH:17][cH:18]1
C=C(Cl)C#N.N#CC(NC(=O)C(F)(F)F)c1ccc(Cl)cc1
N#Cc1cc(C(F)(F)F)[nH]c1-c1ccc(Cl)cc1
null
null
O.C(C)#N.C1(=CC=CC=C1)C.C(C)(=O)OCC.CCCCCCC
Aromatic Heterocycle Formation
OtherReaction
3f91c15dbdc300705d913ba177e9f6eca4eba8456c9598dba9bdbaa28bf4c731
bce0d127b06909f028c7567105178a809c3b4d2897dafeb4ba99dcbf1cc5f33f
c1ccc(-c2ccc[nH]2)cc1
Cl-C(=[CH2;D1;+0:1])-[C;H0;D2;+0:2]#[N;D1;H0:3].N#[C;H0;D2;+0:4]-[CH;D3;+0:5](-[NH;D2;+0:6]-[C;H0;D3;+0:7](=O)-[C:8](-[F;D1;H0:9])(-[F;D1;H0:10])-[F;D1;H0:11])-[c;H0;D3;+0:12](:[c:13]:[c:14]):[c:15]:[c:16]>>[F;D1;H0:9]-[C:8](-[F;D1;H0:10])(-[F;D1;H0:11])-[c;H0;D3;+0:7]1:[cH;D2;+0:1]:[c;H0;D3;+0:4](-[C;H0;D2;+0:2]#[N;D1...
null
[]
80
CELSIUS
null
null
A slurry of N-[(p-chlorophenyl)cyanomethyl]-2,2,2-trifluoroacetamide (13.1 g, 0.05 mol) in toluene is treated sequentially with methanesulfonic acid (2.4 g, 0.025 mol) and acetyl chloride (4.32 g, 0.055 mol), at room temperature, heated at 80° C. for 2 hours, cooled to room temperature, diluted with acetonitrile, treat...
10.6084/m9.figshare.5104873.v1
null
Alkenyl halide.Nitrile.Nitrile.Secondary amide.Vinyl
Nitrile
null
c1cc[nH]c1
c1cc[nH]c1.c1ccccc1
HCl
O.C(C)#N.C1(=CC=CC=C1)C.C(C)(=O)OCC.CCCCCCC
80
null
C=C(Cl)C#N.N#CC(NC(=O)C(F)(F)F)c1ccc(Cl)cc1>O.C(C)#N.C1(=CC=CC=C1)C.C(C)(=O)OCC.CCCCCCC>N#Cc1cc(C(F)(F)F)[nH]c1-c1ccc(Cl)cc1
ord_dataset-c2ad1656a3ca4d08888ffb6e3f3a2742
ord-cda2074a6391416591e32f8f1d0e302b
CN(C)[NH+]=CCl.CO/N=C(\C(=O)Cl)c1csc(N)n1>>CO/N=C(\C(=O)Cl)c1csc(N=CN(C)C)n1
[Cl-].CN(C)[NH+]=CCl.O1CCCC1.Cl.NC=1SC=C(N1)/C(/C(=O)Cl)=N/OC>>CN(C)C=NC=1SC=C(N1)/C(/C(=O)Cl)=N/OC.Cl
Cl[CH:13]=[NH+:14]N([CH3:15])[CH3:16].[CH3:1][O:2]/[N:3]=[C:4](\[C:5](=[O:6])[Cl:7])[c:8]1[cH:9][s:10][c:11]([NH2:12])[n:17]1>>[CH3:1][O:2]/[N:3]=[C:4](\[C:5](=[O:6])[Cl:7])[c:8]1[cH:9][s:10][c:11]([N:12]=[CH:13][N:14]([CH3:15])[CH3:16])[n:17]1
CN(C)[NH+]=CCl.CO/N=C(\C(=O)Cl)c1csc(N)n1
CO/N=C(\C(=O)Cl)c1csc(N=CN(C)C)n1
null
null
null
Functional Group Interconversion
OtherReaction
edca639bc5aaef9daccd9d92f10fe8ab1d1d4efb5b9878178998522894b2e63d
5de7b66aa3e43f62e2731183e10e8dc9c78ad8588054e17fa7602a7444dcae43
c1cscn1
Cl-[CH;D2;+0:1]=[NH+;D2:2]-N(-[CH3;D1;+0:3])-[CH3;D1;+0:4].[NH2;D1;+0:5]-[c:6]1:[#16;a:7]:[c:8]:[c:9]:[#7;a:10]:1>>[CH3;D1;+0:3]-[N;H0;D3;+0:2](-[CH3;D1;+0:4])-[CH;D2;+0:1]=[N;H0;D2;+0:5]-[c:6]1:[#16;a:7]:[c:8]:[c:9]:[#7;a:10]:1
47
[{"value": 47.0, "product": "CN(C)C=NC=1SC=C(N1)/C(/C(=O)Cl)=N/OC.Cl", "details": "PERCENTYIELD", "is_desired": false}]
-10
CELSIUS
40
MINUTE
Dimethylaminochloromethyleneammonium chloride (496 mg, 3.87 mmol) was dissolved in 10 ml of tetrahydrofuran, followed by cooling to -10° C. Added to the solution were 870 mg (3.4 mmol) of (Z)-2-(2-aminothiazol-4-yl)-2-methoxyiminoacetyl chloride hydrochloride and the resulting mixture was stirred for 40 minutes. The re...
10.6084/m9.figshare.5104873.v1
null
Hydrazine.Primary amine
Tertiary amine
null
null
c1cscn1
HCl
null
-10
0.666667
CN(C)[NH+]=CCl.CO/N=C(\C(=O)Cl)c1csc(N)n1>>CO/N=C(\C(=O)Cl)c1csc(N=CN(C)C)n1
ord_dataset-c2ad1656a3ca4d08888ffb6e3f3a2742
ord-94207a37d3ee491990b588d121f42aa9
CN(C)[NH+]=CCl.CO/N=C(\C(=O)O)c1csc(N)n1.[Cl-]>>CO/N=C(\C(=O)Cl)c1csc(N=CN(C)C)n1.Cl
[Cl-].CN(C)[NH+]=CCl.NC=1SC=C(N1)/C(/C(=O)O)=N/OC.C(C)(C)OC(C)C>>CN(C)C=NC=1SC=C(N1)/C(/C(=O)Cl)=N/OC.Cl
N([NH+:14]=[CH:13][Cl:7])([CH3:15])[CH3:16].O[C:5](/[C:4](=[N:3]\[O:2][CH3:1])[c:8]1[cH:9][s:10][c:11]([NH2:12])[n:17]1)=[O:6].[Cl-:18]>>[CH3:1][O:2]/[N:3]=[C:4](\[C:5](=[O:6])[Cl:7])[c:8]1[cH:9][s:10][c:11]([N:12]=[CH:13][N:14]([CH3:15])[CH3:16])[n:17]1.[ClH:18]
CN(C)[NH+]=CCl.CO/N=C(\C(=O)O)c1csc(N)n1.[Cl-]
CO/N=C(\C(=O)Cl)c1csc(N=CN(C)C)n1.Cl
null
null
O1CCCC1
Functional Group Interconversion
OtherReaction
4123e9b2fd562f23844f2df5587e5f936a112b292e018473b3637589a0b28ed7
a52ac2539d6757599153d533a8fbe84d7ef8a9f7d469b2a81399b2c50c0e1b35
c1cscn1
O-[C;H0;D3;+0:1](=[O;D1;H0:2])/[C:3](=[#7:4]\[#8:5])-[c:6]1:[#7;a:7]:[c:8](-[NH2;D1;+0:9]):[#16;a:10]:[c:11]:1.[CH3;D1;+0:12]-N(-[CH3;D1;+0:13])-[NH+;D2:14]=[CH;D2;+0:15]-[Cl;H0;D1;+0:16].[Cl-;H0;D0:17]>>[#8:5]/[#7:4]=[C:3](\[C;H0;D3;+0:1](-[Cl;H0;D1;+0:16])=[O;D1;H0:2])-[c:6]1:[#7;a:7]:[c:8](-[N;H0;D2;+0:9]=[CH;D2;+0:...
96.9
[{"value": 96.9, "product": "CN(C)C=NC=1SC=C(N1)/C(/C(=O)Cl)=N/OC.Cl", "details": "PERCENTYIELD", "is_desired": false}]
-12
CELSIUS
40
MINUTE
Dimethylaminochloromethyleneammonium chloride (1.52 g, 12.0 mmol) was dissolved in 7 ml of tetrahydrofuran, followed by cooling to -12° C. Added to the solution were 1.10 g (5.5 mmol) of (Z)-2-(2-aminothiazol-4-yl)-2-methoxyiminoacetic acid and the resulting mixture was stirred for 40 minutes. Isopropyl ether (16 ml) w...
10.6084/m9.figshare.5104873.v1
null
Hydrazine.Carboxylic acid.Primary amine
Acyl halide.Tertiary amine
null
null
c1cscn1
HO-
O1CCCC1
-12
0.666667
CN(C)[NH+]=CCl.CO/N=C(\C(=O)O)c1csc(N)n1.[Cl-]>O1CCCC1>CO/N=C(\C(=O)Cl)c1csc(N=CN(C)C)n1.Cl
ord_dataset-c2ad1656a3ca4d08888ffb6e3f3a2742
ord-9959aa0b4e7344f4bd7a706d9a088565
CN(C)C=O.CO/N=C(\C(=O)O)c1csc(N)n1.O=C(Cl)C(=O)Cl>>CO/N=C(\C(=O)Cl)c1csc(N=CN(C)C)n1.Cl
NC=1SC=C(N1)/C(/C(=O)O)=N/OC.CN(C=O)C.C(C(=O)Cl)(=O)Cl>>CN(C)C=NC=1SC=C(N1)/C(/C(=O)Cl)=N/OC.Cl
O=[CH:13][N:14]([CH3:15])[CH3:16].O[C:5](/[C:4](=[N:3]\[O:2][CH3:1])[c:8]1[cH:9][s:10][c:11]([NH2:12])[n:17]1)=[O:6].O=C(C(=O)[Cl:18])[Cl:7]>>[CH3:1][O:2]/[N:3]=[C:4](\[C:5](=[O:6])[Cl:7])[c:8]1[cH:9][s:10][c:11]([N:12]=[CH:13][N:14]([CH3:15])[CH3:16])[n:17]1.[ClH:18]
CN(C)C=O.CO/N=C(\C(=O)O)c1csc(N)n1.O=C(Cl)C(=O)Cl
CO/N=C(\C(=O)Cl)c1csc(N=CN(C)C)n1.Cl
null
null
O1CCCC1
Miscellaneous
OtherReaction
c1fd11cc7b768c67699cde9de4369b36d9319360ddd6d5b5b2074076a00a8c49
c7899aa0f0dc139674ae89005ef4b2ef1c28749aa960b8e5456d4ec85191bb72
c1cscn1
O-[C;H0;D3;+0:1](=[O;D1;H0:2])/[C:3](=[#7:4]\[#8:5])-[c:6]1:[#7;a:7]:[c:8](-[NH2;D1;+0:9]):[#16;a:10]:[c:11]:1.O=C(-[Cl;H0;D1;+0:12])-C(=O)-[Cl;H0;D1;+0:13].O=[CH;D2;+0:14]-[#7:15](-[C;D1;H3:16])-[C;D1;H3:17]>>[#8:5]/[#7:4]=[C:3](\[C;H0;D3;+0:1](-[Cl;H0;D1;+0:13])=[O;D1;H0:2])-[c:6]1:[#7;a:7]:[c:8](-[N;H0;D2;+0:9]=[CH;...
43
[{"value": 43.0, "product": "CN(C)C=NC=1SC=C(N1)/C(/C(=O)Cl)=N/OC.Cl", "details": "PERCENTYIELD", "is_desired": false}, {"value": 42.4, "product": "CN(C)C=NC=1SC=C(N1)/C(/C(=O)Cl)=N/OC.Cl", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
-15
CELSIUS
10
MINUTE
Dimethylformamide (1.6 g, 22 mmol) and 10 ml of tetrahydrofuran were mixed, to which 3.06 g (24 mmol) of oxalyl chloride were added dropwise under ice-cooling. After completion of the dropwise addition, the resulting mixture was stirred for further 10 minutes and was then cooled to -15° C. To the mixture so obtained, w...
10.6084/m9.figshare.5104873.v1
null
Acyl halide.Acyl halide.Carboxylic acid.Tertiary amide.Primary amine
Acyl halide
null
null
c1cscn1
HO-
O1CCCC1
-15
0.166667
CN(C)C=O.CO/N=C(\C(=O)O)c1csc(N)n1.O=C(Cl)C(=O)Cl>O1CCCC1>CO/N=C(\C(=O)Cl)c1csc(N=CN(C)C)n1.Cl
ord_dataset-c2ad1656a3ca4d08888ffb6e3f3a2742
ord-40fa5bfaa01d48d18c4efaa85968461c
CN(C)C=O.CO/N=C(\C(=O)O)c1csc(N)n1.O=C(Cl)OC(Cl)(Cl)Cl>>CO/N=C(\C(=O)Cl)c1csc(N=CN(C)C)n1.Cl
C(C)(=O)OC(C)C.ClC(=O)OC(Cl)(Cl)Cl.CN(C=O)C.NC=1SC=C(N1)/C(/C(=O)O)=N/OC>>CN(C)C=NC=1SC=C(N1)/C(/C(=O)Cl)=N/OC.Cl
O=[CH:13][N:14]([CH3:15])[CH3:16].O[C:5](/[C:4](=[N:3]\[O:2][CH3:1])[c:8]1[cH:9][s:10][c:11]([NH2:12])[n:17]1)=[O:6].O=C(OC(Cl)(Cl)[Cl:18])[Cl:7]>>[CH3:1][O:2]/[N:3]=[C:4](\[C:5](=[O:6])[Cl:7])[c:8]1[cH:9][s:10][c:11]([N:12]=[CH:13][N:14]([CH3:15])[CH3:16])[n:17]1.[ClH:18]
CN(C)C=O.CO/N=C(\C(=O)O)c1csc(N)n1.O=C(Cl)OC(Cl)(Cl)Cl
CO/N=C(\C(=O)Cl)c1csc(N=CN(C)C)n1.Cl
null
null
O1CCCC1
Miscellaneous
OtherReaction
eaea42979679f589b5c838d189e8bcdbc0f11e2bb8facc5306b0359763adaced
ce7fd3fb70154b1296c89587dc416e49acfde049e0a380446ef38465c9572215
c1cscn1
Cl-C(-Cl)(-[Cl;H0;D1;+0:1])-O-C(=O)-[Cl;H0;D1;+0:2].O-[C;H0;D3;+0:3](=[O;D1;H0:4])/[C:5](=[#7:6]\[#8:7])-[c:8]1:[#7;a:9]:[c:10](-[NH2;D1;+0:11]):[#16;a:12]:[c:13]:1.O=[CH;D2;+0:14]-[#7:15](-[C;D1;H3:16])-[C;D1;H3:17]>>[#8:7]/[#7:6]=[C:5](\[C;H0;D3;+0:3](-[Cl;H0;D1;+0:2])=[O;D1;H0:4])-[c:8]1:[#7;a:9]:[c:10](-[N;H0;D2;+0...
94
[{"value": 94.0, "product": "CN(C)C=NC=1SC=C(N1)/C(/C(=O)Cl)=N/OC.Cl", "details": "PERCENTYIELD", "is_desired": false}]
null
null
30
MINUTE
Dimethylformamide (0.8 g, 11 mmol) was added to 9 ml of tetrahydrofuran, followed by ice-cooling. To the resulting mixture, 0.6 ml of trichloromethyl chloroformate was added dropwise under ice-cooling. After stirring the resulting mixture for 30 minutes, the mixture was cooled to -10° C. (Z)-2-(2-Amino-thiazol-4-yl)-2-...
10.6084/m9.figshare.5104873.v1
null
Acyl halide.Trichloro group.Carboxylic acid.Ether.Tertiary amide.Primary amine
Acyl halide
null
null
c1cscn1
HCl
O1CCCC1
null
0.5
CN(C)C=O.CO/N=C(\C(=O)O)c1csc(N)n1.O=C(Cl)OC(Cl)(Cl)Cl>O1CCCC1>CO/N=C(\C(=O)Cl)c1csc(N=CN(C)C)n1.Cl
ord_dataset-c2ad1656a3ca4d08888ffb6e3f3a2742
ord-44c097f4597f45aaa8e470701df07836
CN(C)C=O.CO/N=C(\C(=O)O)c1csc(N)n1>>CO/N=C(\C(=O)OC)c1csc(N=CN(C)C)n1
NC=1SC=C(N1)/C(/C(=O)O)=N/OC.O1CCCC1.CN(C=O)C.[OH-].[Na+].P(=O)(Cl)(Cl)Cl>>CN(C)C=NC=1SC=C(N1)/C(/C(=O)OC)=N/OC
O=[CH:14][N:15]([CH3:8])[CH3:17].[CH3:1][O:2]/[N:3]=[C:4](\[C:5](=[O:6])[OH:7])[c:9]1[cH:10][s:11][c:12]([NH2:13])[n:18]1>>[CH3:1][O:2]/[N:3]=[C:4](\[C:5](=[O:6])[O:7][CH3:8])[c:9]1[cH:10][s:11][c:12]([N:13]=[CH:14][N:15]([CH3:16])[CH3:17])[n:18]1
CN(C)C=O.CO/N=C(\C(=O)O)c1csc(N)n1
CO/N=C(\C(=O)OC)c1csc(N=CN(C)C)n1
null
null
CO
Heteroatom Alkylation and Arylation
OtherReaction
d70a286ad904b1503497cdcff8261707546da8ca90f4a12730593efb811ff04d
9bbed73db60f00920df17e3dd909bd56740044f6820b270937aa116b0a5812c9
c1cscn1
O=[CH;D2;+0:1]-[N;H0;D3;+0:2](-[C;D1;H3:3])-[CH3;D1;+0:4].[#7:5]=[C:6](\[C:7](=[O;D1;H0:8])-[OH;D1;+0:9])-[c:10]1:[#7;a:11]:[c:12](-[NH2;D1;+0:13]):[#16;a:14]:[c:15]:1>>[#7:5]=[C:6](\[C:7](=[O;D1;H0:8])-[O;H0;D2;+0:9]-[CH3;D1;+0:4])-[c:10]1:[#7;a:11]:[c:12](-[N;H0;D2;+0:13]=[CH;D2;+0:1]-[N;H0;D3;+0:2](-[C;D1;H3:16])-[C...
94
[{"value": 94.0, "product": "CN(C)C=NC=1SC=C(N1)/C(/C(=O)OC)=N/OC", "details": "PERCENTYIELD", "is_desired": false}]
5
CELSIUS
3
HOUR
(Z)-2-(2-aminothiazol-4-yl)-2-methoxyiminoacetic acid (0.5 g, 2.5 mmol) was dissolved in 20 ml of tetrahydrofuran. Subsequent to the addition of 0.72 g (9.9 mmol) of dimethylformamide, the resulting solution was cooled to 5° C. The solution was added with 1.52 g (9.9 mmol) of phosphorus oxychloride and the resulting mi...
10.6084/m9.figshare.5104873.v1
null
Carboxylic acid.Tertiary amide.Primary amine
Ester.Tertiary amine
null
null
c1cscn1
null
CO
5
3
CN(C)C=O.CO/N=C(\C(=O)O)c1csc(N)n1>CO>CO/N=C(\C(=O)OC)c1csc(N=CN(C)C)n1
ord_dataset-c2ad1656a3ca4d08888ffb6e3f3a2742
ord-c46fb7910fca43abbd53bbc36327201c
CN(C)[NH+]=CCl.CO.CO/N=C(\C(=O)O)c1csc(N)n1>>CO/N=C(\C(=O)OC)c1csc(N=CN(C)C)n1
[Cl-].CN(C)[NH+]=CCl.O1CCCC1.NC=1SC=C(N1)/C(/C(=O)O)=N/OC.C(O)([O-])=O.[Na+].CO>>CN(C)C=NC=1SC=C(N1)/C(/C(=O)OC)=N/OC
Cl[CH:14]=[NH+:15]N([CH3:16])[CH3:17].O[CH3:8].[CH3:1][O:2]/[N:3]=[C:4](\[C:5](=[O:6])[OH:7])[c:9]1[cH:10][s:11][c:12]([NH2:13])[n:18]1>>[CH3:1][O:2]/[N:3]=[C:4](\[C:5](=[O:6])[O:7][CH3:8])[c:9]1[cH:10][s:11][c:12]([N:13]=[CH:14][N:15]([CH3:16])[CH3:17])[n:18]1
CN(C)[NH+]=CCl.CO.CO/N=C(\C(=O)O)c1csc(N)n1
CO/N=C(\C(=O)OC)c1csc(N=CN(C)C)n1
null
null
null
Functional Group Interconversion
OtherReaction
3456d0573b2da524291a0f1b61970c154474fb5ccafd90e0e9271cd005bd60f0
c47988b2c9d3d9360562c6f39c2436905f74fa093bcb3b817d9ec26f5479a58c
c1cscn1
Cl-[CH;D2;+0:1]=[NH+;D2:2]-N(-[CH3;D1;+0:3])-[CH3;D1;+0:4].O-[CH3;D1;+0:5].[#7:6]=[C:7](\[C:8](=[O;D1;H0:9])-[OH;D1;+0:10])-[c:11]1:[#7;a:12]:[c:13](-[NH2;D1;+0:14]):[#16;a:15]:[c:16]:1>>[#7:6]=[C:7](\[C:8](=[O;D1;H0:9])-[O;H0;D2;+0:10]-[CH3;D1;+0:5])-[c:11]1:[#7;a:12]:[c:13](-[N;H0;D2;+0:14]=[CH;D2;+0:1]-[N;H0;D3;+0:2...
95
[{"value": 95.0, "product": "CN(C)C=NC=1SC=C(N1)/C(/C(=O)OC)=N/OC", "details": "PERCENTYIELD", "is_desired": false}]
-3
CELSIUS
40
MINUTE
Dimethylaminochloromethyleneammonium chloride (400 mg, 3.1 mmol) was dissolved in 10 ml of tetrahydrofuran, followed by cooling to -3° C. The solution was added with 300 mg (1.5 mmol) of (Z)-2-(2-aminothiazol-4-yl)-2-methoxyiminoacetic acid and the mixture so obtained was stirred for 40 minutes. After the resulting mix...
10.6084/m9.figshare.5104873.v1
null
Hydrazine.Carboxylic acid.Primary amine.Methanol
Ester.Tertiary amine
null
null
c1cscn1
HCl
null
-3
0.666667
CN(C)[NH+]=CCl.CO.CO/N=C(\C(=O)O)c1csc(N)n1>>CO/N=C(\C(=O)OC)c1csc(N=CN(C)C)n1
ord_dataset-c2ad1656a3ca4d08888ffb6e3f3a2742
ord-189585ea02bc4713a78b924966961140
CN(C)[NH+]=CCl.CO.CO/N=C(\C(=O)O)c1csc(N)n1>>CO/N=C(/C(=O)OC)c1csc(N=CN(C)C)n1
[Cl-].CN(C)[NH+]=CCl.O1CCCC1.NC=1SC=C(N1)/C(/C(=O)O)=N/OC.C(O)([O-])=O.[Na+].CO>>CN(C)C=NC=1SC=C(N1)\C(\C(=O)OC)=N/OC
Cl[CH:14]=[NH+:15]N([CH3:16])[CH3:17].O[CH3:8].[CH3:1][O:2]/[N:3]=[C:4](\[C:5](=[O:6])[OH:7])[c:9]1[cH:10][s:11][c:12]([NH2:13])[n:18]1>>[CH3:1][O:2]/[N:3]=[C:4](/[C:5](=[O:6])[O:7][CH3:8])[c:9]1[cH:10][s:11][c:12]([N:13]=[CH:14][N:15]([CH3:16])[CH3:17])[n:18]1
CN(C)[NH+]=CCl.CO.CO/N=C(\C(=O)O)c1csc(N)n1
CO/N=C(/C(=O)OC)c1csc(N=CN(C)C)n1
null
null
null
Functional Group Interconversion
OtherReaction
3456d0573b2da524291a0f1b61970c154474fb5ccafd90e0e9271cd005bd60f0
c47988b2c9d3d9360562c6f39c2436905f74fa093bcb3b817d9ec26f5479a58c
c1cscn1
Cl-[CH;D2;+0:1]=[NH+;D2:2]-N(-[CH3;D1;+0:3])-[CH3;D1;+0:4].O-[CH3;D1;+0:5].[#7:6]=[C:7](\[C:8](=[O;D1;H0:9])-[OH;D1;+0:10])-[c:11]1:[#7;a:12]:[c:13](-[NH2;D1;+0:14]):[#16;a:15]:[c:16]:1>>[#7:6]=[C:7](/[C:8](=[O;D1;H0:9])-[O;H0;D2;+0:10]-[CH3;D1;+0:5])-[c:11]1:[#7;a:12]:[c:13](-[N;H0;D2;+0:14]=[CH;D2;+0:1]-[N;H0;D3;+0:2...
72
[{"value": 72.0, "product": "CN(C)C=NC=1SC=C(N1)\\C(\\C(=O)OC)=N/OC", "details": "PERCENTYIELD", "is_desired": false}]
null
null
16
HOUR
Dimethylaminochloromethyleneammonium chloride (400 mg, 3.1 mmol) was dissolved in 10 ml of tetrahydrofuran, Added to the resulting solution were 300 mg of (Z)-2-(2-aminothiazol-4-yl)-2-methoxyimino-acetic acid, followed by stirring at room temperature for 16 hours. Methanol (10 ml) was added thereto. The mixture so obt...
10.6084/m9.figshare.5104873.v1
null
Hydrazine.Carboxylic acid.Primary amine.Methanol
Ester.Tertiary amine
null
null
c1cscn1
HCl
null
null
16
CN(C)[NH+]=CCl.CO.CO/N=C(\C(=O)O)c1csc(N)n1>>CO/N=C(/C(=O)OC)c1csc(N=CN(C)C)n1
ord_dataset-c2ad1656a3ca4d08888ffb6e3f3a2742
ord-8f24189601874b8dbcf6802f3355fe98
CC/C=C(\C(=O)O)c1csc(N)n1.CN(C)[NH+]=CCl.CO>>CC/C=C(\C(=O)OC)c1csc(N=CN(C)C)n1
C(O)([O-])=O.[Na+].CO.[Cl-].CN(C)[NH+]=CCl.O1CCCC1.NC=1SC=C(N1)/C(/C(=O)O)=C/CC>>CN(C)C=NC=1SC=C(N1)/C(/C(=O)OC)=C/CC
[CH3:1][CH2:2]/[CH:3]=[C:4](\[C:5](=[O:6])[OH:7])[c:9]1[cH:10][s:11][c:12]([NH2:13])[n:18]1.Cl[CH:14]=[NH+][N:15]([CH3:16])[CH3:17].O[CH3:8]>>[CH3:1][CH2:2]/[CH:3]=[C:4](\[C:5](=[O:6])[O:7][CH3:8])[c:9]1[cH:10][s:11][c:12]([N:13]=[CH:14][N:15]([CH3:16])[CH3:17])[n:18]1
CC/C=C(\C(=O)O)c1csc(N)n1.CN(C)[NH+]=CCl.CO
CC/C=C(\C(=O)OC)c1csc(N=CN(C)C)n1
null
null
null
Heteroatom Alkylation and Arylation
OtherReaction
cc868f42fc4ea4486b68a23a4a842774e8dec1dace7529177ac927f86d56cca8
c9485ed1774eb17e96eafc224e6fcdfff31a74bf9276a9087acc5464567f3272
c1cscn1
Cl-[CH;D2;+0:1]=[NH+]-[N;H0;D3;+0:2](-[C;D1;H3:3])-[C;D1;H3:4].O-[CH3;D1;+0:5].[C:6]/[C:7]=[C:8](\[C:9](=[O;D1;H0:10])-[OH;D1;+0:11])-[c:12]1:[#7;a:13]:[c:14](-[NH2;D1;+0:15]):[#16;a:16]:[c:17]:1>>[C:6]/[C:7]=[C:8](\[C:9](=[O;D1;H0:10])-[O;H0;D2;+0:11]-[CH3;D1;+0:5])-[c:12]1:[#7;a:13]:[c:14](-[N;H0;D2;+0:15]=[CH;D2;+0:...
67
[{"value": 67.0, "product": "CN(C)C=NC=1SC=C(N1)/C(/C(=O)OC)=C/CC", "details": "PERCENTYIELD", "is_desired": false}]
null
null
1
HOUR
Dimethylaminochloromethyleneammonium chloride (830 mg, 6.5 mmol) was added to 12 ml of tetrahydrofuran, and the resulting mixture was ice-cooled. Added to the mixture were 196 mg (0.99 mmol) of (Z)-2-(2-aminothiazol-4-yl)-2-pentenoic acid, followed by stirring for 1 hour. Methanol (10 ml) was added thereto. The mixture...
10.6084/m9.figshare.5104873.v1
null
Hydrazine.Carboxylic acid.Primary amine.Methanol
Ester.Tertiary amine
null
null
c1cscn1
HCl
null
null
1
CC/C=C(\C(=O)O)c1csc(N)n1.CN(C)[NH+]=CCl.CO>>CC/C=C(\C(=O)OC)c1csc(N=CN(C)C)n1
ord_dataset-c2ad1656a3ca4d08888ffb6e3f3a2742
ord-d6dd7437a4df4e30817c1c6d65d25c7d
CO/N=C(\C(=O)NCCc1ccccc1)c1csc(N=CN(C)C)n1>>CO/N=C(\C(=O)NCCc1ccccc1)c1csc(N)n1
C(O)([O-])=O.[Na+].C(C)(=O)OCC.C1(=CC=CC=C1)CCNC(\C(=N/OC)\C=1N=C(SC1)N=CN(C)C)=O.S(O)(O)(=O)=O>>C1(=CC=CC=C1)CCNC(\C(=N/OC)\C=1N=C(SC1)N)=O
CN(C)C=[N:20][c:19]1[s:18][cH:17][c:16](/[C:4](=[N:3]/[O:2][CH3:1])[C:5](=[O:6])[NH:7][CH2:8][CH2:9][c:10]2[cH:11][cH:12][cH:13][cH:14][cH:15]2)[n:21]1>>[CH3:1][O:2]/[N:3]=[C:4](\[C:5](=[O:6])[NH:7][CH2:8][CH2:9][c:10]1[cH:11][cH:12][cH:13][cH:14][cH:15]1)[c:16]1[cH:17][s:18][c:19]([NH2:20])[n:21]1
CO/N=C(\C(=O)NCCc1ccccc1)c1csc(N=CN(C)C)n1
CO/N=C(\C(=O)NCCc1ccccc1)c1csc(N)n1
null
null
CO
Deprotection
OtherReaction
33bcd42056000f3bc2d5907a85ff371ecf8a91697366ae3c95c7cdc536f4e4f7
09463156f8971f4e8007d84d8ed410eed1d618bdb6ba7dd05b4970ff2019f62b
N=C(C(=O)NCCc1ccccc1)c1cscn1
C-N(-C)-C=[N;H0;D2;+0:1]-[c:2]1:[#16;a:3]:[c:4]:[c:5]:[#7;a:6]:1>>[NH2;D1;+0:1]-[c:2]1:[#16;a:3]:[c:4]:[c:5]:[#7;a:6]:1
95.8
[{"value": 95.0, "product": "C1(=CC=CC=C1)CCNC(\\C(=N/OC)\\C=1N=C(SC1)N)=O", "details": "PERCENTYIELD", "is_desired": false}, {"value": 95.8, "product": "C1(=CC=CC=C1)CCNC(\\C(=N/OC)\\C=1N=C(SC1)N)=O", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
3
DAY
(Z)-N-(2-phenylethyl)-2-(2-dimethylaminomethylidenaminothiazol-4-yl)-2-methoxyiminoacetamide (130 mg, 0.36 mmol) was dissolved in 4 ml of methanol, followed by the addition of 0.5 ml of 1.8N sulfuric acid. The mixture so obtained was stirred for 3 days at room temperature. The reaction mixture was then added with 20 ml...
10.6084/m9.figshare.5104873.v1
null
Tertiary amine
Primary amine
null
null
c1ccccc1.c1cscn1
Other
CO
null
72
CO/N=C(\C(=O)NCCc1ccccc1)c1csc(N=CN(C)C)n1>CO>CO/N=C(\C(=O)NCCc1ccccc1)c1csc(N)n1
ord_dataset-c2ad1656a3ca4d08888ffb6e3f3a2742
ord-8963643bac2048a9a944f4a1f3c4252e
CO/N=C(\C(=O)NCCc1ccccc1)c1csc(N=CN(C)C)n1>>CO/N=C(\C(=O)NCCc1ccccc1)c1csc(N)n1
C(O)([O-])=O.[Na+].C(C)(=O)OCC.C1(=CC=CC=C1)CCNC(\C(=N/OC)\C=1N=C(SC1)N=CN(C)C)=O.Cl>>C1(=CC=CC=C1)CCNC(\C(=N/OC)\C=1N=C(SC1)N)=O
CN(C)C=[N:20][c:19]1[s:18][cH:17][c:16](/[C:4](=[N:3]/[O:2][CH3:1])[C:5](=[O:6])[NH:7][CH2:8][CH2:9][c:10]2[cH:11][cH:12][cH:13][cH:14][cH:15]2)[n:21]1>>[CH3:1][O:2]/[N:3]=[C:4](\[C:5](=[O:6])[NH:7][CH2:8][CH2:9][c:10]1[cH:11][cH:12][cH:13][cH:14][cH:15]1)[c:16]1[cH:17][s:18][c:19]([NH2:20])[n:21]1
CO/N=C(\C(=O)NCCc1ccccc1)c1csc(N=CN(C)C)n1
CO/N=C(\C(=O)NCCc1ccccc1)c1csc(N)n1
null
null
CO
Deprotection
OtherReaction
33bcd42056000f3bc2d5907a85ff371ecf8a91697366ae3c95c7cdc536f4e4f7
09463156f8971f4e8007d84d8ed410eed1d618bdb6ba7dd05b4970ff2019f62b
N=C(C(=O)NCCc1ccccc1)c1cscn1
C-N(-C)-C=[N;H0;D2;+0:1]-[c:2]1:[#16;a:3]:[c:4]:[c:5]:[#7;a:6]:1>>[NH2;D1;+0:1]-[c:2]1:[#16;a:3]:[c:4]:[c:5]:[#7;a:6]:1
97.7
[{"value": 97.5, "product": "C1(=CC=CC=C1)CCNC(\\C(=N/OC)\\C=1N=C(SC1)N)=O", "details": "PERCENTYIELD", "is_desired": false}, {"value": 97.7, "product": "C1(=CC=CC=C1)CCNC(\\C(=N/OC)\\C=1N=C(SC1)N)=O", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
60
CELSIUS
30
MINUTE
(Z)-N-(2-Phenylethyl)-2-(2-dimethylaminomethylidenaminothiazol-4-yl)-2-methoxyiminoacetamide (130 mg, 0.36 mmol) was dissolved in 4 ml of methanol, followed by the addition of 1 ml of 2 N hydrochloric acid. The mixture so obtained was stirred at 60° C. for 3 hours and 30 minutes. The reaction mixture was then added wit...
10.6084/m9.figshare.5104873.v1
null
Tertiary amine
Primary amine
null
null
c1ccccc1.c1cscn1
Other
CO
60
0.5
CO/N=C(\C(=O)NCCc1ccccc1)c1csc(N=CN(C)C)n1>CO>CO/N=C(\C(=O)NCCc1ccccc1)c1csc(N)n1
ord_dataset-c2ad1656a3ca4d08888ffb6e3f3a2742
ord-bccf734719ee4e03a13a60243dc65238
CO/N=C(\C(=O)NCCc1ccccc1)c1csc(N=CN(C)C)n1>>CO/N=C(\C(=O)NCCc1ccccc1)c1csc(N)n1
C(=O)O.O.C1(=CC=CC=C1)CCNC(\C(=N/OC)\C=1N=C(SC1)N=CN(C)C)=O.C(O)([O-])=O.[Na+]>>C1(=CC=CC=C1)CCNC(\C(=N/OC)\C=1N=C(SC1)N)=O
CN(C)C=[N:20][c:19]1[s:18][cH:17][c:16](/[C:4](=[N:3]/[O:2][CH3:1])[C:5](=[O:6])[NH:7][CH2:8][CH2:9][c:10]2[cH:11][cH:12][cH:13][cH:14][cH:15]2)[n:21]1>>[CH3:1][O:2]/[N:3]=[C:4](\[C:5](=[O:6])[NH:7][CH2:8][CH2:9][c:10]1[cH:11][cH:12][cH:13][cH:14][cH:15]1)[c:16]1[cH:17][s:18][c:19]([NH2:20])[n:21]1
CO/N=C(\C(=O)NCCc1ccccc1)c1csc(N=CN(C)C)n1
CO/N=C(\C(=O)NCCc1ccccc1)c1csc(N)n1
null
null
CO.C(C)(=O)OCC
Deprotection
OtherReaction
33bcd42056000f3bc2d5907a85ff371ecf8a91697366ae3c95c7cdc536f4e4f7
09463156f8971f4e8007d84d8ed410eed1d618bdb6ba7dd05b4970ff2019f62b
N=C(C(=O)NCCc1ccccc1)c1cscn1
C-N(-C)-C=[N;H0;D2;+0:1]-[c:2]1:[#16;a:3]:[c:4]:[c:5]:[#7;a:6]:1>>[NH2;D1;+0:1]-[c:2]1:[#16;a:3]:[c:4]:[c:5]:[#7;a:6]:1
57.9
[{"value": 57.9, "product": "C1(=CC=CC=C1)CCNC(\\C(=N/OC)\\C=1N=C(SC1)N)=O", "details": "PERCENTYIELD", "is_desired": false}, {"value": 57.5, "product": "C1(=CC=CC=C1)CCNC(\\C(=N/OC)\\C=1N=C(SC1)N)=O", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
60
CELSIUS
30
MINUTE
(Z)-N-(2-Phenylethyl)-2-(2-dimethylaminomethylidenaminothiazol-4-yl)-2-methoxyiminoacetamide (130 mg, 0.36 mmol) was dissolved in 4 ml of methanol, followed by the addition of 0.5 ml of formic acid and 1 ml of water. The mixture so obtained was stirred at 60° C. for 3 hours and 30 minutes. The reaction mixture was then...
10.6084/m9.figshare.5104873.v1
null
Tertiary amine
Primary amine
null
null
c1ccccc1.c1cscn1
Other
CO.C(C)(=O)OCC
60
0.5
CO/N=C(\C(=O)NCCc1ccccc1)c1csc(N=CN(C)C)n1>CO.C(C)(=O)OCC>CO/N=C(\C(=O)NCCc1ccccc1)c1csc(N)n1
ord_dataset-c2ad1656a3ca4d08888ffb6e3f3a2742
ord-4094125384014bf38c8f542f3d52bf4f
CO/N=C(\C(=O)NCCc1ccccc1)c1csc(N=CN(C)C)n1>>CO/N=C(\C(=O)NCCc1ccccc1)c1csc(N)n1
[Cl-].[NH4+].C(Cl)Cl.[OH-].[Na+].C1(=CC=CC=C1)CCNC(\C(=N/OC)\C=1N=C(SC1)N=CN(C)C)=O>>C1(=CC=CC=C1)CCNC(\C(=N/OC)\C=1N=C(SC1)N)=O
CN(C)C=[N:20][c:19]1[s:18][cH:17][c:16](/[C:4](=[N:3]/[O:2][CH3:1])[C:5](=[O:6])[NH:7][CH2:8][CH2:9][c:10]2[cH:11][cH:12][cH:13][cH:14][cH:15]2)[n:21]1>>[CH3:1][O:2]/[N:3]=[C:4](\[C:5](=[O:6])[NH:7][CH2:8][CH2:9][c:10]1[cH:11][cH:12][cH:13][cH:14][cH:15]1)[c:16]1[cH:17][s:18][c:19]([NH2:20])[n:21]1
CO/N=C(\C(=O)NCCc1ccccc1)c1csc(N=CN(C)C)n1
CO/N=C(\C(=O)NCCc1ccccc1)c1csc(N)n1
null
null
CO
Deprotection
OtherReaction
33bcd42056000f3bc2d5907a85ff371ecf8a91697366ae3c95c7cdc536f4e4f7
09463156f8971f4e8007d84d8ed410eed1d618bdb6ba7dd05b4970ff2019f62b
N=C(C(=O)NCCc1ccccc1)c1cscn1
C-N(-C)-C=[N;H0;D2;+0:1]-[c:2]1:[#16;a:3]:[c:4]:[c:5]:[#7;a:6]:1>>[NH2;D1;+0:1]-[c:2]1:[#16;a:3]:[c:4]:[c:5]:[#7;a:6]:1
82.1
[{"value": 81.8, "product": "C1(=CC=CC=C1)CCNC(\\C(=N/OC)\\C=1N=C(SC1)N)=O", "details": "PERCENTYIELD", "is_desired": false}, {"value": 82.1, "product": "C1(=CC=CC=C1)CCNC(\\C(=N/OC)\\C=1N=C(SC1)N)=O", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
2
DAY
(Z)-N-(2-Phenylethyl)-2-(2-dimethylaminomethylidenaminothiazol-4-yl)-2-methoxyiminoacetamide (130 mg, 0.36 mmol) was dissolved in 4 ml of methanol, followed by the addition of 1 ml of a 1N aqueous solution of sodium hydroxide. The mixture so obtained was stirred at room temperature for 2 days. The reaction mixture was ...
10.6084/m9.figshare.5104873.v1
null
Tertiary amine
Primary amine
null
null
c1ccccc1.c1cscn1
Other
CO
null
48
CO/N=C(\C(=O)NCCc1ccccc1)c1csc(N=CN(C)C)n1>CO>CO/N=C(\C(=O)NCCc1ccccc1)c1csc(N)n1
ord_dataset-c2ad1656a3ca4d08888ffb6e3f3a2742
ord-69960a002bb1481596e42a63ec2dd704
COc1cc(N)c(N)cc1OC.O=C(O)C(=O)O>>COc1cc2[nH]c(=O)c(=O)[nH]c2cc1OC
NC1=C(C=C(C(=C1)OC)OC)N.C(C(=O)O)(=O)O>>COC=1C=C2NC(C(NC2=CC1OC)=O)=O
[CH3:1][O:2][c:3]1[cH:4][c:5]([NH2:6])[c:12]([NH2:11])[cH:13][c:14]1[O:15][CH3:16].O[C:7](=[O:8])[C:9](O)=[O:10]>>[CH3:1][O:2][c:3]1[cH:4][c:5]2[nH:6][c:7](=[O:8])[c:9](=[O:10])[nH:11][c:12]2[cH:13][c:14]1[O:15][CH3:16]
COc1cc(N)c(N)cc1OC.O=C(O)C(=O)O
COc1cc2[nH]c(=O)c(=O)[nH]c2cc1OC
null
null
null
Aromatic Heterocycle Formation
OtherReaction
c86e58e5de9d81a144b6b41f680eb7659186c7868f08e5aac1617724bf77eb2d
7638e82fa21608897e39fce0230ec3ea8d25eb3dc2c5eca945d0fbdce3af493b
O=c1[nH]c2ccccc2[nH]c1=O
O-[C;H0;D3;+0:1](=[O;D1;H0:2])-[C;H0;D3;+0:3](-O)=[O;D1;H0:4].[NH2;D1;+0:5]-[c:6](:[c:7]):[c:8](-[NH2;D1;+0:9]):[c:10]>>[O;D1;H0:4]=[c;H0;D3;+0:3]1:[nH;D2;+0:5]:[c:6](:[c:7]):[c:8](:[c:10]):[nH;D2;+0:9]:[c;H0;D3;+0:1]:1=[O;D1;H0:2]
null
[]
null
null
null
null
6,7-Dimethoxy-1,4-dihydroquinoxaline-2,3-dione was prepared from 1,2-dimethoxybenzene. Nitration of 1,2-dimethoxybenzene gave 1,2-dimethoxy-4,5-dinitrobenzene, which was reduced to 1,2-diamino-4,5-dimethoxybenzene. Condensation of the diamine with oxalic acid gave 6,7-dimethoxy-1,4-dihydroquinoxaline-2,3-dione. ##STR31...
10.6084/m9.figshare.5104873.v1
null
Carboxylic acid.Carboxylic acid.Primary amine.Primary amine
null
c1ccccc1
C1=CNc2ccccc2N1
C1=CNc2ccccc2N1
HO-
null
null
null
COc1cc(N)c(N)cc1OC.O=C(O)C(=O)O>>COc1cc2[nH]c(=O)c(=O)[nH]c2cc1OC
ord_dataset-c2ad1656a3ca4d08888ffb6e3f3a2742
ord-b8a253bdb1e143b2ae6d02ae88447cf5
C[O-].O=c1[nH]c2cc(Cl)c(F)c([N+](=O)[O-])c2[nH]c1=O>>COc1c(Cl)cc2c(c1[N+](=O)[O-])=NC(=O)C(=O)N=2
ClC1=C(C(=C2NC(C(NC2=C1)=O)=O)[N+](=O)[O-])F.C[O-].[Na+]>>ClC=1C(=C(C2=NC(C(N=C2C1)=O)=O)[N+](=O)[O-])OC
[CH3:1][O-:2].F[c:3]1[c:4]([Cl:5])[cH:6][c:7]2[c:8]([c:9]1[N+:10](=[O:11])[O-:12])[nH:13][c:14](=[O:15])[c:16](=[O:17])[nH:18]2>>[CH3:1][O:2][c:3]1[c:4]([Cl:5])[cH:6][c:7]2[c:8]([c:9]1[N+:10](=[O:11])[O-:12])=[N:13][C:14](=[O:15])[C:16](=[O:17])[N:18]=2
C[O-].O=c1[nH]c2cc(Cl)c(F)c([N+](=O)[O-])c2[nH]c1=O
COc1c(Cl)cc2c(c1[N+](=O)[O-])=NC(=O)C(=O)N=2
null
null
null
Protection
OtherReaction
a7d76c2a6bfdd138babfd395a211f1e275b9bcf1d4bcb24c8cd20882f7161f6c
29fc5779163b01c4d317ea64bb5a1fa8b0f020fb7a365acf4aa351c7d5296f72
O=C1N=c2ccccc2=NC1=O
F-[c;H0;D3;+0:1]1:[c:2](-[Cl;D1;H0:3]):[c:4]:[c;H0;D3;+0:5]2:[nH;D2;+0:6]:[c;H0;D3;+0:7](=[O;D1;H0:8]):[c;H0;D3;+0:9](=[O;D1;H0:10]):[nH;D2;+0:11]:[c;H0;D3;+0:12]:2:[c:13]:1-[#7;+:14].[C;D1;H3:15]-[O-;H0;D1:16]>>[#7;+:14]-[c:13]1:[c;H0;D3;+0:1](-[O;H0;D2;+0:16]-[C;D1;H3:15]):[c:2](-[Cl;D1;H0:3]):[c:4]:[c;H0;D3;+0:5]2:[...
null
[]
null
null
null
null
Similarly, the reaction of 7-chloro-6-fluoro-5-nitro-1,4-dihydroquinoxaline-2,3-dione with sodium methoxide gave 7-chloro-6-methoxy-5-nitroquinoxaline-2,3-dione, and with ethanethiol gave 7-chloro-6-ethylthio-5-nitroquinoxaline-2,3-dione. Conditions: See reaction.notes.procedure_details.
10.6084/m9.figshare.5104873.v1
null
Aromatic halide
Ether
C1=CNc2ccccc2N1
c1ccc2c(c1)=NCCN=2
c1ccc2c(c1)=NCCN=2
HF
null
null
null
C[O-].O=c1[nH]c2cc(Cl)c(F)c([N+](=O)[O-])c2[nH]c1=O>>COc1c(Cl)cc2c(c1[N+](=O)[O-])=NC(=O)C(=O)N=2
ord_dataset-c2ad1656a3ca4d08888ffb6e3f3a2742
ord-3cc03fd3884c4b61ab9530f4f144bf4b
Nc1cc(F)c(F)cc1[N+](=O)[O-]>>Nc1cc(F)c(F)cc1N
FC1=CC(=C(C=C1)N)N.FC1=CC(=C(C=C1)N)N.[Cl-].[Cl-].[Ca+2].FC1=CC(=C(N)C=C1F)[N+](=O)[O-]>>FC1=CC(=C(C=C1F)N)N
O=[N+:10]([O-])[c:9]1[c:2]([NH2:1])[cH:3][c:4]([F:5])[c:6]([F:7])[cH:8]1>>[NH2:1][c:2]1[cH:3][c:4]([F:5])[c:6]([F:7])[cH:8][c:9]1[NH2:10]
Nc1cc(F)c(F)cc1[N+](=O)[O-]
Nc1cc(F)c(F)cc1N
null
[Zn]
O.CCO
Reduction
Reduction of nitro groups to amines
bbc242b150a51e69d3ad1caaa391f4422710431b398dcb880555f476706790be
7b0317532ea57a4fcedc1efc3e3c22eb5238d1c8330da53d4f9801fc2391f567
c1ccccc1
O=[N+;H0;D3:1](-[O-])-[c:2](:[c:3]):[c:4]>>[NH2;D1;+0:1]-[c:2](:[c:3]):[c:4]
67.3
[{"value": 67.3, "product": null, "details": "PERCENTYIELD", "is_desired": false}]
null
null
null
null
4,5-Difluoro-1,2-diaminobenzene was prepared using an adaptation of the method of Tsuji et al., (Tsuji, Y. et al., J. Org. Chem. 55:580 (1990)). Zn powder (942 mg, 14.4 mmol), CaCl2 (94.4 mg), H2O (1.0 mL) and 4.0 mL EtOH were combined and brought to reflux as described for 4-fluoro-1,2-diaminobenzene (see Example 11) ...
10.6084/m9.figshare.5104873.v1
null
Nitro group
Primary amine
null
null
c1ccccc1
Other
[Zn].O.CCO
null
null
Nc1cc(F)c(F)cc1[N+](=O)[O-]>[Zn].O.CCO>Nc1cc(F)c(F)cc1N
ord_dataset-c2ad1656a3ca4d08888ffb6e3f3a2742
ord-86b392d03e2846528aa1fa65dbd1be47
CCOC(=O)C(=O)OCC.Nc1cc(F)c(F)cc1N>>O=c1[nH]c2cc(F)c(F)cc2[nH]c1=O
C(C(=O)OCC)(=O)OCC.FC1=CC(=C(C=C1F)N)N>>FC=1C=C2NC(C(NC2=CC1F)=O)=O
CCO[C:2](=[O:1])[C:13](OCC)=[O:14].[NH2:3][c:4]1[cH:5][c:6]([F:7])[c:8]([F:9])[cH:10][c:11]1[NH2:12]>>[O:1]=[c:2]1[nH:3][c:4]2[cH:5][c:6]([F:7])[c:8]([F:9])[cH:10][c:11]2[nH:12][c:13]1=[O:14]
CCOC(=O)C(=O)OCC.Nc1cc(F)c(F)cc1N
O=c1[nH]c2cc(F)c(F)cc2[nH]c1=O
null
null
null
Aromatic Heterocycle Formation
OtherReaction
97e21139ecefaa04a2e379ed0dfebec189c2701deff8c9503bbfc28454aa8630
c8ccb70449d522f01766cc73ad4a0b9615cb3862df314fa00223145fc838cd64
O=c1[nH]c2ccccc2[nH]c1=O
C-C-O-[C;H0;D3;+0:1](=[O;D1;H0:2])-[C;H0;D3;+0:3](=[O;D1;H0:4])-O-C-C.[NH2;D1;+0:5]-[c:6](:[c:7]):[c:8](-[NH2;D1;+0:9]):[c:10]>>[O;D1;H0:2]=[c;H0;D3;+0:1]1:[nH;D2;+0:5]:[c:6](:[c:7]):[c:8](:[c:10]):[nH;D2;+0:9]:[c;H0;D3;+0:3]:1=[O;D1;H0:4]
null
[]
null
null
null
null
The title compound (Sarges, R. et al., J. Med. Chem. 33:2240 (1990)) was prepared using an adaptation of the method of Cheeseman. (Cheeseman, G. W. H. J. Chem. Soc. 1171 (1962)). A mixture of diethyl oxalate (1.11 g, 7.63 mmol and 4,5-difluoro-1,2-diaminobenzene (110 mg, 0.763 mmol) was heated to reflux under N2 for 2 ...
10.6084/m9.figshare.5104873.v1
null
Ester.Ester.Primary amine.Primary amine
null
c1ccccc1
C1=CNc2ccccc2N1
C1=CNc2ccccc2N1
HO-
null
null
null
CCOC(=O)C(=O)OCC.Nc1cc(F)c(F)cc1N>>O=c1[nH]c2cc(F)c(F)cc2[nH]c1=O
ord_dataset-c2ad1656a3ca4d08888ffb6e3f3a2742
ord-3a55073e62434c55a2982297e6aefec4
Nc1cc(F)c(F)c(F)c1N.O=C(O)C(=O)O>>O=c1[nH]c2cc(F)c(F)c(F)c2[nH]c1=O
C(C)O.FC=1C(=C(C=C(C1F)F)N)N.C(C(=O)O)(=O)O>>FC1=C2NC(C(NC2=CC(=C1F)F)=O)=O
[NH2:3][c:4]1[cH:5][c:6]([F:7])[c:8]([F:9])[c:10]([F:11])[c:12]1[NH2:13].O[C:2](=[O:1])[C:14](O)=[O:15]>>[O:1]=[c:2]1[nH:3][c:4]2[cH:5][c:6]([F:7])[c:8]([F:9])[c:10]([F:11])[c:12]2[nH:13][c:14]1=[O:15]
Nc1cc(F)c(F)c(F)c1N.O=C(O)C(=O)O
O=c1[nH]c2cc(F)c(F)c(F)c2[nH]c1=O
null
null
Cl
Aromatic Heterocycle Formation
OtherReaction
c86e58e5de9d81a144b6b41f680eb7659186c7868f08e5aac1617724bf77eb2d
7638e82fa21608897e39fce0230ec3ea8d25eb3dc2c5eca945d0fbdce3af493b
O=c1[nH]c2ccccc2[nH]c1=O
O-[C;H0;D3;+0:1](=[O;D1;H0:2])-[C;H0;D3;+0:3](-O)=[O;D1;H0:4].[NH2;D1;+0:5]-[c:6](:[c:7]):[c:8](-[NH2;D1;+0:9]):[c:10]>>[O;D1;H0:2]=[c;H0;D3;+0:1]1:[nH;D2;+0:5]:[c:6](:[c:7]):[c:8](:[c:10]):[nH;D2;+0:9]:[c;H0;D3;+0:3]:1=[O;D1;H0:4]
36
[{"value": 36.0, "product": "FC1=C2NC(C(NC2=CC(=C1F)F)=O)=O", "details": "PERCENTYIELD", "is_desired": false}, {"value": 4.0, "product": "FC1=C2NC(C(NC2=CC(=C1F)F)=O)=O", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
8
HOUR
To a brown solution of 3,4,5-trifluoro-1,2-phenylenediamine (285 mg, 1.75 mmol) in aqueous 2N HCl (10 mL) is added oxalic acid (221 mg, 1.75 mmol). The brown mixture is brought to reflux and stirred under N2 overnight. The mixture is filtered to yield 139 mg (37%) of crude title compound. An analytical sample is prepar...
10.6084/m9.figshare.5104873.v1
null
Carboxylic acid.Carboxylic acid.Primary amine.Primary amine
null
c1ccccc1
C1=CNc2ccccc2N1
C1=CNc2ccccc2N1
HO-
Cl
null
8
Nc1cc(F)c(F)c(F)c1N.O=C(O)C(=O)O>Cl>O=c1[nH]c2cc(F)c(F)c(F)c2[nH]c1=O
ord_dataset-c2ad1656a3ca4d08888ffb6e3f3a2742
ord-25c1c2e595e141d09b33471fe1808e8d
O=[N+]([O-])[O-].O=c1[nH]c2cc(F)c(F)c(F)c2[nH]c1=O>>O=c1[nH]c2c(F)c(F)c(F)c([N+](=O)[O-])c2[nH]c1=O
FC1=C2NC(C(NC2=CC(=C1F)F)=O)=O.S(O)(O)(=O)=O.[N+](=O)([O-])[O-].[K+]>>[N+](=O)([O-])C1=C2NC(C(NC2=C(C(=C1F)F)F)=O)=O
[O-][N+:12](=[O:13])[O-:14].[O:1]=[c:2]1[nH:3][c:4]2[cH:5][c:7]([F:8])[c:9]([F:10])[c:11]([F:6])[c:15]2[nH:16][c:17]1=[O:18]>>[O:1]=[c:2]1[nH:3][c:4]2[c:5]([F:6])[c:7]([F:8])[c:9]([F:10])[c:11]([N+:12](=[O:13])[O-:14])[c:15]2[nH:16][c:17]1=[O:18]
O=[N+]([O-])[O-].O=c1[nH]c2cc(F)c(F)c(F)c2[nH]c1=O
O=c1[nH]c2c(F)c(F)c(F)c([N+](=O)[O-])c2[nH]c1=O
null
null
null
Functional Group Interconversion
Aromatic nitration with NO3 salt
9b381d098dcad5196b132a57d8e96dee6d17d216c4112b0363cc96bfbd7d28da
0ce6037a9929cfde4fb0319b5ea6c7a5e61c11a2cadf28ca4b1b99abfaf70590
O=c1[nH]c2ccccc2[nH]c1=O
[F;D1;H0:1]-[c:2]1:[c:3](-[F;D1;H0:4]):[cH;D2;+0:5]:[c:6]2:[#7;a:7]:[c:8]:[c:9]:[#7;a:10]:[c:11]:2:[c;H0;D3;+0:12]:1-[F;H0;D1;+0:13].[O-]-[N+;H0;D3:14](-[O;-;D1;H0:15])=[O;D1;H0:16]>>[F;D1;H0:1]-[c:2]1:[c:3](-[F;D1;H0:4]):[c;H0;D3;+0:5](-[F;H0;D1;+0:13]):[c:6]2:[#7;a:7]:[c:8]:[c:9]:[#7;a:10]:[c:11]:2:[c;H0;D3;+0:12]:1-...
null
[]
null
null
8
HOUR
To 5,6,7-trifluoro-1,4-dihydro-2,3-quinoxalinedione (93 mg, 0.43 mmol) is added concentrated sulfuric acid (0.5 mL). While the flask is in an ice bath, KNO3 is slowly added, giving a brown mixture, which is stirred overnight. The reaction mixture, now dark red, is then added to ice water (5 mL), instantly giving an ora...
10.6084/m9.figshare.5104873.v1
null
Aromatic halide.Nitrate
Aromatic halide.Nitro group
C1=CNc2ccccc2N1
C1=CNc2ccccc2N1
C1=CNc2ccccc2N1
HO-
null
null
8
O=[N+]([O-])[O-].O=c1[nH]c2cc(F)c(F)c(F)c2[nH]c1=O>>O=c1[nH]c2c(F)c(F)c(F)c([N+](=O)[O-])c2[nH]c1=O
ord_dataset-c2ad1656a3ca4d08888ffb6e3f3a2742
ord-80600a2229cb427eb0740b402c5fba7d
O=C(Nc1ccc(F)c(Cl)c1F)C(F)(F)F.O=[N+]([O-])O>>O=C(Nc1c([N+](=O)[O-])cc(F)c(Cl)c1F)C(F)(F)F
[N+](=O)(O)[O-].ClC=1C(=C(C=CC1F)NC(C(F)(F)F)=O)F.[N+](=O)(O)[O-]>>ClC=1C(=C(C(=CC1F)[N+](=O)[O-])NC(C(F)(F)F)=O)F
[O:1]=[C:2]([NH:3][c:4]1[cH:5][cH:9][c:10]([F:11])[c:12]([Cl:13])[c:14]1[F:15])[C:16]([F:17])([F:18])[F:19].O[N+:6](=[O:7])[O-:8]>>[O:1]=[C:2]([NH:3][c:4]1[c:5]([N+:6](=[O:7])[O-:8])[cH:9][c:10]([F:11])[c:12]([Cl:13])[c:14]1[F:15])[C:16]([F:17])([F:18])[F:19]
O=C(Nc1ccc(F)c(Cl)c1F)C(F)(F)F.O=[N+]([O-])O
O=C(Nc1c([N+](=O)[O-])cc(F)c(Cl)c1F)C(F)(F)F
null
null
OS(=O)(=O)O
Functional Group Addition
Aromatic nitration with HNO3
53848b8b2bb4e867226e49db2e60519b24be9379900e3ad7c56af54fe8fde7a5
ddce49825c02b8965f10c8d99e3c841d26e1f136da6037b417c09313e6d73097
c1ccccc1
O-[N+;H0;D3:1](-[O;-;D1;H0:2])=[O;D1;H0:3].[O;D1;H0:4]=[C:5]-[#7:6]-[c:7](:[c:8]):[cH;D2;+0:9]:[c:10]:[c:11]>>[O;-;D1;H0:2]-[N+;H0;D3:1](=[O;D1;H0:3])-[c;H0;D3;+0:9](:[c:10]:[c:11]):[c:7](-[#7:6]-[C:5]=[O;D1;H0:4]):[c:8]
95
[{"value": 95.0, "product": "ClC=1C(=C(C(=CC1F)[N+](=O)[O-])NC(C(F)(F)F)=O)F", "details": "PERCENTYIELD", "is_desired": false}]
null
null
4
HOUR
To a solution of 15.1 g (58.1 mmol) of 3-chloro-2,4-difluoro-(trifluoroacetamido)benzene in 80 mL of H2SO4 kept in an ice-bath was added dropwise 10 mL of HNO3. Solid precipitate was observed during addition of HNO3. The mixture was stirred in an ice-bath for 4 h, then added to 600 mL of ice-water. The precipitate was ...
10.6084/m9.figshare.5104873.v1
null
Nitrate
Nitro group
c1ccccc1
c1ccccc1
c1ccccc1
HO-
OS(=O)(=O)O
null
4
O=C(Nc1ccc(F)c(Cl)c1F)C(F)(F)F.O=[N+]([O-])O>OS(=O)(=O)O>O=C(Nc1c([N+](=O)[O-])cc(F)c(Cl)c1F)C(F)(F)F
ord_dataset-c2ad1656a3ca4d08888ffb6e3f3a2742
ord-c0b2172acf044bee8060c3836fd1650a
O=C(Nc1c([N+](=O)[O-])cc(F)c(Cl)c1F)C(F)(F)F>>Nc1c([N+](=O)[O-])cc(F)c(Cl)c1F
ClC=1C(=C(C(=CC1F)[N+](=O)[O-])NC(C(F)(F)F)=O)F>>ClC=1C(=C(N)C(=CC1F)[N+](=O)[O-])F
O=C(C(F)(F)F)[NH:1][c:2]1[c:3]([N+:4](=[O:5])[O-:6])[cH:7][c:8]([F:9])[c:10]([Cl:11])[c:12]1[F:13]>>[NH2:1][c:2]1[c:3]([N+:4](=[O:5])[O-:6])[cH:7][c:8]([F:9])[c:10]([Cl:11])[c:12]1[F:13]
O=C(Nc1c([N+](=O)[O-])cc(F)c(Cl)c1F)C(F)(F)F
Nc1c([N+](=O)[O-])cc(F)c(Cl)c1F
null
null
C(=O)([O-])[O-].[K+].[K+].CO.O
Reduction
Hydrogenolysis of amides/imides/carbamates
44b36597c7daf0608965c52c8db8a9220c21d9447ce54e0af375898475f3493f
caaeb83af2cb178156ae90fe7f610a106cd4bb5397d23f56d37a7fe11e2668ed
c1ccccc1
F-C(-F)(-F)-C(=O)-[NH;D2;+0:1]-[c:2](:[c:3]):[c:4]>>[NH2;D1;+0:1]-[c:2](:[c:3]):[c:4]
6.9
[{"value": 6.9, "product": "ClC=1C(=C(N)C(=CC1F)[N+](=O)[O-])F", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
null
null
A solution of 6.35 g (20.8 mmol) of 3-chloro-2,4-difluoro-6-nitro-(trifluoroacetamido)benzene in 60 mL of 7% K2CO3 methanol/water (3:2) was stirred at 25° C. for 4 h. The solution was evaporated to remove the methanol. Solid was observed in the residue. It was filtered, washed with water, and dried to leave 301 mg of a...
10.6084/m9.figshare.5104873.v1
null
Trifluoro group.Secondary amide
Primary amine
null
null
c1ccccc1
Other
C(=O)([O-])[O-].[K+].[K+].CO.O
null
null
O=C(Nc1c([N+](=O)[O-])cc(F)c(Cl)c1F)C(F)(F)F>C(=O)([O-])[O-].[K+].[K+].CO.O>Nc1c([N+](=O)[O-])cc(F)c(Cl)c1F
ord_dataset-c2ad1656a3ca4d08888ffb6e3f3a2742
ord-3cada9c9acb74b5d838041f2015ca3bb
Nc1c([N+](=O)[O-])cc(F)c(Cl)c1F>>Nc1cc(F)c(Cl)c(F)c1N
ClC=1C(=C(N)C(=CC1F)[N+](=O)[O-])F.Cl[Sn]Cl>>ClC1=C(C(=C(C=C1F)N)N)F
O=[N+:1]([O-])[c:2]1[cH:3][c:4]([F:5])[c:6]([Cl:7])[c:8]([F:9])[c:10]1[NH2:11]>>[NH2:1][c:2]1[cH:3][c:4]([F:5])[c:6]([Cl:7])[c:8]([F:9])[c:10]1[NH2:11]
Nc1c([N+](=O)[O-])cc(F)c(Cl)c1F
Nc1cc(F)c(Cl)c(F)c1N
null
null
C(C)O
Reduction
Reduction of nitro groups to amines
bbc242b150a51e69d3ad1caaa391f4422710431b398dcb880555f476706790be
7b0317532ea57a4fcedc1efc3e3c22eb5238d1c8330da53d4f9801fc2391f567
c1ccccc1
O=[N+;H0;D3:1](-[O-])-[c:2](:[c:3]):[c:4]>>[NH2;D1;+0:1]-[c:2](:[c:3]):[c:4]
95.6
[{"value": 95.0, "product": "ClC1=C(C(=C(C=C1F)N)N)F", "details": "PERCENTYIELD", "is_desired": false}, {"value": 95.6, "product": "ClC1=C(C(=C(C=C1F)N)N)F", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
null
null
A solution of 348 mg (1.67 mmol) of 3-chloro-2,4-difluoro-6-nitroaniline and 1.57 g (8.28 mmol) of SnCl2 in 8 mL of ethanol was heated at 70° C. for 2 h. The solution was evaporated to remove the ethanol. The residue was treated with 2N NaOH to pH=13. White precipitate was observed. The mixture was extracted with CHCl3...
10.6084/m9.figshare.5104873.v1
null
Nitro group
Primary amine
null
null
c1ccccc1
Other
C(C)O
null
null
Nc1c([N+](=O)[O-])cc(F)c(Cl)c1F>C(C)O>Nc1cc(F)c(Cl)c(F)c1N
ord_dataset-c2ad1656a3ca4d08888ffb6e3f3a2742
ord-c565455ebe624ff695bd4f3f0a89e4d7
Nc1cc(F)c(Cl)c(F)c1N.O=C(O)C(=O)O>>O=c1[nH]c2cc(F)c(Cl)c(F)c2[nH]c1=O
ClC1=C(C(=C(C=C1F)N)N)F.C(C(=O)O)(=O)O>>ClC=1C(=C2NC(C(NC2=CC1F)=O)=O)F
[NH2:3][c:4]1[cH:5][c:6]([F:7])[c:8]([Cl:9])[c:10]([F:11])[c:12]1[NH2:13].O[C:2](=[O:1])[C:14](O)=[O:15]>>[O:1]=[c:2]1[nH:3][c:4]2[cH:5][c:6]([F:7])[c:8]([Cl:9])[c:10]([F:11])[c:12]2[nH:13][c:14]1=[O:15]
Nc1cc(F)c(Cl)c(F)c1N.O=C(O)C(=O)O
O=c1[nH]c2cc(F)c(Cl)c(F)c2[nH]c1=O
null
null
Cl
Aromatic Heterocycle Formation
OtherReaction
c86e58e5de9d81a144b6b41f680eb7659186c7868f08e5aac1617724bf77eb2d
7638e82fa21608897e39fce0230ec3ea8d25eb3dc2c5eca945d0fbdce3af493b
O=c1[nH]c2ccccc2[nH]c1=O
O-[C;H0;D3;+0:1](=[O;D1;H0:2])-[C;H0;D3;+0:3](-O)=[O;D1;H0:4].[NH2;D1;+0:5]-[c:6](:[c:7]):[c:8](-[NH2;D1;+0:9]):[c:10]>>[O;D1;H0:2]=[c;H0;D3;+0:1]1:[nH;D2;+0:5]:[c:6](:[c:7]):[c:8](:[c:10]):[nH;D2;+0:9]:[c;H0;D3;+0:3]:1=[O;D1;H0:4]
82
[{"value": 82.0, "product": "ClC=1C(=C2NC(C(NC2=CC1F)=O)=O)F", "details": "PERCENTYIELD", "is_desired": false}, {"value": 81.7, "product": "ClC=1C(=C2NC(C(NC2=CC1F)=O)=O)F", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
null
null
A mixture of 230 mg (1.29 mmol) of 4-chloro-3,5-difluoro-1,2-phenylenediamine and 125 mg (1.38 mmol) of oxalic acid in 4 mL of 2N HCl was refluxed for 3 h and cooled to room temperature. The mixture was filtered, washed with water, and dried to leave a brown solid (245 mg, 82%); mp>250° C.; 1H NMR (DMSO-d6), 6.921 (d, ...
10.6084/m9.figshare.5104873.v1
null
Carboxylic acid.Carboxylic acid.Primary amine.Primary amine
null
c1ccccc1
C1=CNc2ccccc2N1
C1=CNc2ccccc2N1
HO-
Cl
null
null
Nc1cc(F)c(Cl)c(F)c1N.O=C(O)C(=O)O>Cl>O=c1[nH]c2cc(F)c(Cl)c(F)c2[nH]c1=O
ord_dataset-c2ad1656a3ca4d08888ffb6e3f3a2742
ord-8da99543e0364674abc4d6f1dbd12299
O=[N+]([O-])[O-].O=c1[nH]c2cc(F)c(Cl)c(F)c2[nH]c1=O>>O=c1[nH]c2c(F)c(Cl)c(F)c([N+](=O)[O-])c2[nH]c1=O
ClC=1C(=C2NC(C(NC2=CC1F)=O)=O)F.[N+](=O)([O-])[O-].[K+].[N+](=O)([O-])[O-].[K+]>>ClC1=C(C(=C2NC(C(NC2=C1F)=O)=O)[N+](=O)[O-])F
[O-][N+:12](=[O:13])[O-:14].[O:1]=[c:2]1[nH:3][c:4]2[cH:5][c:9]([F:10])[c:7]([Cl:8])[c:11]([F:6])[c:15]2[nH:16][c:17]1=[O:18]>>[O:1]=[c:2]1[nH:3][c:4]2[c:5]([F:6])[c:7]([Cl:8])[c:9]([F:10])[c:11]([N+:12](=[O:13])[O-:14])[c:15]2[nH:16][c:17]1=[O:18]
O=[N+]([O-])[O-].O=c1[nH]c2cc(F)c(Cl)c(F)c2[nH]c1=O
O=c1[nH]c2c(F)c(Cl)c(F)c([N+](=O)[O-])c2[nH]c1=O
null
null
OS(=O)(=O)O
Functional Group Interconversion
Aromatic nitration with NO3 salt
bdc7586a693070879fbbcb7ac36c4ca1147950a00c707c57a6b53f196453fef2
a6e75bd3b480911aeca325a734424f30acd0183ae8bf9859f205a30a2d946dc4
O=c1[nH]c2ccccc2[nH]c1=O
[Cl;D1;H0:1]-[c;H0;D3;+0:2]1:[c;H0;D3;+0:3](-[F;H0;D1;+0:4]):[c:5]2:[#7;a:6]:[c:7]:[c:8]:[#7;a:9]:[c:10]:2:[cH;D2;+0:11]:[c;H0;D3;+0:12]:1-[F;D1;H0:13].[O-]-[N+;H0;D3:14](-[O;-;D1;H0:15])=[O;D1;H0:16]>>[Cl;D1;H0:1]-[c;H0;D3;+0:2]1:[c;H0;D3;+0:11](-[F;H0;D1;+0:4]):[c:10]2:[#7;a:9]:[c:8]:[c:7]:[#7;a:6]:[c:5]:2:[c;H0;D3;+...
65
[{"value": 65.0, "product": "ClC1=C(C(=C2NC(C(NC2=C1F)=O)=O)[N+](=O)[O-])F", "details": "PERCENTYIELD", "is_desired": false}, {"value": 57.4, "product": "ClC1=C(C(=C2NC(C(NC2=C1F)=O)=O)[N+](=O)[O-])F", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
14
HOUR
To a solution of 120 mg (5.16 mmol) of 6-chloro-5,7-difluoro-1,4-dihydroquinoxaline-2,3-dione in 1 mL of H2SO4 (97%) kept in an ice bath was added portionwise 60 mg (0.59 mmol) of KNO3. The solution was stirred at room temperature for 14 h and 60 mg of KNO3 was added. It was stirred at room temperature for 24 h, then d...
10.6084/m9.figshare.5104873.v1
null
Aromatic halide.Aromatic halide.Aromatic halide.Nitrate
Aromatic halide.Aromatic halide.Aromatic halide.Nitro group
C1=CNc2ccccc2N1
C1=CNc2ccccc2N1
C1=CNc2ccccc2N1
HO-
OS(=O)(=O)O
null
14
O=[N+]([O-])[O-].O=c1[nH]c2cc(F)c(Cl)c(F)c2[nH]c1=O>OS(=O)(=O)O>O=c1[nH]c2c(F)c(Cl)c(F)c([N+](=O)[O-])c2[nH]c1=O
ord_dataset-c2ad1656a3ca4d08888ffb6e3f3a2742
ord-2af234bdce2f49bd88878ea3885cee0f
O=C(Nc1c([N+](=O)[O-])cc(F)cc1[N+](=O)[O-])C(F)(F)F>>Nc1c([N+](=O)[O-])cc(F)cc1[N+](=O)[O-]
FC1=CC(=C(C(=C1)[N+](=O)[O-])NC(C(F)(F)F)=O)[N+](=O)[O-]>>FC1=CC(=C(N)C(=C1)[N+](=O)[O-])[N+](=O)[O-]
O=C(C(F)(F)F)[NH:1][c:2]1[c:3]([N+:4](=[O:5])[O-:6])[cH:7][c:8]([F:9])[cH:10][c:11]1[N+:12](=[O:13])[O-:14]>>[NH2:1][c:2]1[c:3]([N+:4](=[O:5])[O-:6])[cH:7][c:8]([F:9])[cH:10][c:11]1[N+:12](=[O:13])[O-:14]
O=C(Nc1c([N+](=O)[O-])cc(F)cc1[N+](=O)[O-])C(F)(F)F
Nc1c([N+](=O)[O-])cc(F)cc1[N+](=O)[O-]
null
null
C(=O)([O-])[O-].[K+].[K+]
Reduction
Hydrogenolysis of amides/imides/carbamates
44b36597c7daf0608965c52c8db8a9220c21d9447ce54e0af375898475f3493f
caaeb83af2cb178156ae90fe7f610a106cd4bb5397d23f56d37a7fe11e2668ed
c1ccccc1
F-C(-F)(-F)-C(=O)-[NH;D2;+0:1]-[c:2](:[c:3]):[c:4]>>[NH2;D1;+0:1]-[c:2](:[c:3]):[c:4]
52.2
[{"value": 52.0, "product": "FC1=CC(=C(N)C(=C1)[N+](=O)[O-])[N+](=O)[O-]", "details": "PERCENTYIELD", "is_desired": false}, {"value": 52.2, "product": "FC1=CC(=C(N)C(=C1)[N+](=O)[O-])[N+](=O)[O-]", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
null
null
A solution of 4-fluoro-2,6-dinitro-(trifluoroacetamido)benzene (297 mg, 1.00 mmol) in 10% K2CO3 (10 mL) was refluxed for 1 h, then cooled to room temperature to give yellow crystals. It was filtered and washed with cold water (2×1 mL), affording 105 mg (52%) of the title compound. 1H NMR (DMSO-d6): δ8.254 (s, 2H), 8.46...
10.6084/m9.figshare.5104873.v1
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Trifluoro group.Secondary amide
Primary amine
null
null
c1ccccc1
Other
C(=O)([O-])[O-].[K+].[K+]
null
null
O=C(Nc1c([N+](=O)[O-])cc(F)cc1[N+](=O)[O-])C(F)(F)F>C(=O)([O-])[O-].[K+].[K+]>Nc1c([N+](=O)[O-])cc(F)cc1[N+](=O)[O-]
ord_dataset-c2ad1656a3ca4d08888ffb6e3f3a2742
ord-5f0ef1fe42bf4089bfdb32856a06d1da
Nc1c([N+](=O)[O-])cc(F)cc1[N+](=O)[O-]>>Nc1cc(F)cc([N+](=O)[O-])c1N
FC1=CC(=C(N)C(=C1)[N+](=O)[O-])[N+](=O)[O-].CCO>>NC1=C(C=C(C=C1[N+](=O)[O-])F)N
O=[N+:1]([O-])[c:2]1[cH:3][c:4]([F:5])[cH:6][c:7]([N+:8](=[O:9])[O-:10])[c:11]1[NH2:12]>>[NH2:1][c:2]1[cH:3][c:4]([F:5])[cH:6][c:7]([N+:8](=[O:9])[O-:10])[c:11]1[NH2:12]
Nc1c([N+](=O)[O-])cc(F)cc1[N+](=O)[O-]
Nc1cc(F)cc([N+](=O)[O-])c1N
null
null
O
Functional Group Interconversion
Reduction of nitro groups to amines
5c1ea979989295c14f1f65f49e58974d5c524451abca65fc2e6cec44e3d0784f
10b8579fd1662beac4350d758bc16e1f45ee6ea295ff9572db62110c9e2a77db
c1ccccc1
O=[N+;H0;D3:1](-[O-])-[c:2](:[c:3]):[c:4]>>[NH2;D1;+0:1]-[c:2](:[c:3]):[c:4]
50
[{"value": 50.0, "product": "NC1=C(C=C(C=C1[N+](=O)[O-])F)N", "details": "PERCENTYIELD", "is_desired": false}, {"value": 50.0, "product": "NC1=C(C=C(C=C1[N+](=O)[O-])F)N", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
null
null
A solution of 4-fluoro-2,6-dinitroaniline (125 mg, 0.62 mmole) in freshly prepared 6% (NH4)2S (5 mL) and EtOH (5 mL) was refluxed for 30 min, diluted with water (10 mL) and kept at 4° C. for several hours. The precipitate was collected and washed with cold water (2×1 mL), affording 53 mg (50%) of 1,2-diamino-4-fluoro-6...
10.6084/m9.figshare.5104873.v1
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Nitro group
Primary amine
null
null
c1ccccc1
Other
O
null
null
Nc1c([N+](=O)[O-])cc(F)cc1[N+](=O)[O-]>O>Nc1cc(F)cc([N+](=O)[O-])c1N
ord_dataset-c2ad1656a3ca4d08888ffb6e3f3a2742
ord-5f3c86c86c224a99bae8cd6ed4600e41
Nc1cc(F)cc([N+](=O)[O-])c1N.O=C(O)C(=O)O>>O=c1[nH]c2cc(F)cc([N+](=O)[O-])c2[nH]c1=O
NC1=C(C=C(C=C1[N+](=O)[O-])F)N.O.O.C(C(=O)O)(=O)O>>FC1=CC(=C2NC(C(NC2=C1)=O)=O)[N+](=O)[O-]
[NH2:3][c:4]1[cH:5][c:6]([F:7])[cH:8][c:9]([N+:10](=[O:11])[O-:12])[c:13]1[NH2:14].O[C:2](=[O:1])[C:15](O)=[O:16]>>[O:1]=[c:2]1[nH:3][c:4]2[cH:5][c:6]([F:7])[cH:8][c:9]([N+:10](=[O:11])[O-:12])[c:13]2[nH:14][c:15]1=[O:16]
Nc1cc(F)cc([N+](=O)[O-])c1N.O=C(O)C(=O)O
O=c1[nH]c2cc(F)cc([N+](=O)[O-])c2[nH]c1=O
null
null
Cl
Aromatic Heterocycle Formation
OtherReaction
c86e58e5de9d81a144b6b41f680eb7659186c7868f08e5aac1617724bf77eb2d
7638e82fa21608897e39fce0230ec3ea8d25eb3dc2c5eca945d0fbdce3af493b
O=c1[nH]c2ccccc2[nH]c1=O
O-[C;H0;D3;+0:1](=[O;D1;H0:2])-[C;H0;D3;+0:3](-O)=[O;D1;H0:4].[NH2;D1;+0:5]-[c:6](:[c:7]):[c:8](-[NH2;D1;+0:9]):[c:10]>>[O;D1;H0:2]=[c;H0;D3;+0:1]1:[nH;D2;+0:5]:[c:6](:[c:7]):[c:8](:[c:10]):[nH;D2;+0:9]:[c;H0;D3;+0:3]:1=[O;D1;H0:4]
43.5
[{"value": 42.0, "product": "FC1=CC(=C2NC(C(NC2=C1)=O)=O)[N+](=O)[O-]", "details": "PERCENTYIELD", "is_desired": false}, {"value": 43.5, "product": "FC1=CC(=C2NC(C(NC2=C1)=O)=O)[N+](=O)[O-]", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
null
null
A mixture of 1,2-diamino-4-fluoro-6-nitrobenzene (80 mg, 0.46 mmole) and oxalic acid dihydrate (70 mg, 0.56 mmole, used as received) in 4N HCl (4 mL) was refluxed at 120°-5° C. for 3 h, then cooled to room temperature. The mixture was centrifuged and the supernatant was removed. The yellow solid was washed with cold wa...
10.6084/m9.figshare.5104873.v1
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Carboxylic acid.Carboxylic acid.Primary amine.Primary amine
null
c1ccccc1
C1=CNc2ccccc2N1
C1=CNc2ccccc2N1
HO-
Cl
null
null
Nc1cc(F)cc([N+](=O)[O-])c1N.O=C(O)C(=O)O>Cl>O=c1[nH]c2cc(F)cc([N+](=O)[O-])c2[nH]c1=O