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414 values
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36
36
reaction_smiles
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4
873
rxn_insight_reaction
large_stringlengths
19
1.07k
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14
3.37k
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1
581
product_smiles
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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
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large_stringclasses
4 values
procedure_details
large_stringlengths
1
23.6k
reference
large_stringclasses
96 values
doi
large_stringclasses
19 values
functional_groups_reactants
large_stringlengths
3
716
functional_groups_products
large_stringlengths
3
539
participating_rings_reactants
large_stringlengths
5
293
participating_rings_products
large_stringlengths
5
271
all_rings_products
large_stringlengths
5
271
byproduct_smiles
large_stringclasses
176 values
agent_smiles
large_stringlengths
1
712
temperature_c
float64
-230
30.1k
reaction_time_hours
float64
0
2.16k
reaction_smiles_with_agents
large_stringlengths
4
882
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-119328d4f6c144a381d29ff2f0cd48ad
CN(C)C=C(C=O)c1ccc(Cl)cc1.N#CCC(N)=O>>N#Cc1cc(-c2ccc(Cl)cc2)c[nH]c1=O
CC(=O)OCC1=C2C=CC=CC2=C(C3=CC=CC=C31)COC(=O)C.ClC1=CC=C(C=C1)C(C=O)=CN(C)C.C[O-].[Na+].C(#N)CC(=O)N>>C(#N)C=1C(NC=C(C1)C1=CC=C(C=C1)Cl)=O
CN(C)[CH:13]=[C:5]([CH:4]=O)[c:6]1[cH:7][cH:8][c:9]([Cl:10])[cH:11][cH:12]1.[N:1]#[C:2][CH2:3][C:15]([NH2:14])=[O:16]>>[N:1]#[C:2][c:3]1[cH:4][c:5](-[c:6]2[cH:7][cH:8][c:9]([Cl:10])[cH:11][cH:12]2)[cH:13][nH:14][c:15]1=[O:16]
CN(C)C=C(C=O)c1ccc(Cl)cc1.N#CCC(N)=O
N#Cc1cc(-c2ccc(Cl)cc2)c[nH]c1=O
null
null
CO.O
Aromatic Heterocycle Formation
OtherReaction
4fb69599b2ad512416349de44ee025f314a8ccdb2c8ad729cdf94ea75cf3109a
46cf335065eccd013987994a3f086665eb273ac87eb3153099a47e61dd329581
O=c1ccc(-c2ccccc2)c[nH]1
C-N(-C)-[CH;D2;+0:1]=[C;H0;D3;+0:2](-[CH;D2;+0:3]=O)-[c;H0;D3;+0:4](:[c:5]:[c:6]):[c:7]:[c:8].[N;D1;H0:9]#[C:10]-[CH2;D2;+0:11]-[C;H0;D3;+0:12](-[NH2;D1;+0:13])=[O;D1;H0:14]>>[N;D1;H0:9]#[C:10]-[c;H0;D3;+0:11]1:[cH;D2;+0:3]:[c;H0;D3;+0:2](-[c;H0;D3;+0:4](:[c:5]:[c:6]):[c:7]:[c:8]):[cH;D2;+0:1]:[nH;D2;+0:13]:[c;H0;D3;+0...
null
[]
null
null
null
null
To solution of sodium methoxide (7.52 g) in methanol (130 ml) was added cyanoacetamide (5.84 g) followed by 2-(4-chlorophenyl)-3-dimethylaminopropenal and the resulting suspension was refluxed overnight. During this time a yellow solid was formed. The mixture was cooled to room temperature and glacial acetic add (50 ml...
10.6084/m9.figshare.5104873.v1
null
Enamine.Aldehyde.Primary amide
null
null
c1cnccc1
c1cnccc1.c1ccccc1
HO-
CO.O
null
null
CN(C)C=C(C=O)c1ccc(Cl)cc1.N#CCC(N)=O>CO.O>N#Cc1cc(-c2ccc(Cl)cc2)c[nH]c1=O
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-79fe63c48e194c1993a6d88339084cf5
N#Cc1cc(-c2ccc(Cl)cc2)c[nH]c1=O>>O=c1ccc(-c2ccc(Cl)cc2)c[nH]1
C(#N)C=1C(NC=C(C1)C1=CC=C(C=C1)Cl)=O>>ClC1=CC=C(C=C1)C=1C=CC(NC1)=O
N#C[c:3]1[c:2](=[O:1])[nH:14][cH:13][c:5](-[c:6]2[cH:7][cH:8][c:9]([Cl:10])[cH:11][cH:12]2)[cH:4]1>>[O:1]=[c:2]1[cH:3][cH:4][c:5](-[c:6]2[cH:7][cH:8][c:9]([Cl:10])[cH:11][cH:12]2)[cH:13][nH:14]1
N#Cc1cc(-c2ccc(Cl)cc2)c[nH]c1=O
O=c1ccc(-c2ccc(Cl)cc2)c[nH]1
null
null
OP(=O)(O)O
Miscellaneous
OtherReaction
145adc421652def73603eb299eace1e2e3a197522b719b6949c0145a4308d11b
4f08c5adfb6d80fba1093598fc51ce38f180c76537f67052d397b642cb6f3b89
O=c1ccc(-c2ccccc2)c[nH]1
N#C-[c;H0;D3;+0:1]1:[c:2]:[c:3]:[c:4]:[#7;a:5]:[c:6]:1=[O;D1;H0:7]>>[O;D1;H0:7]=[c:6]1:[#7;a:5]:[c:4]:[c:3]:[c:2]:[cH;D2;+0:1]:1
75.6
[{"value": 75.6, "product": "ClC1=CC=C(C=C1)C=1C=CC(NC1)=O", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
null
null
A mixture of 3-cyano-5-(4-chlorophenyl)-2-pyridinone (4.6 g) and 85% H3PO4 (60 ml) was heated at reflux for 16 hours. The resulting mixture was cooled to room temperature, poured into ice/water and filtered yielding 3.1 g of 5-(4-chlorophenyl)-2-pyridinone as a yellow solid. Conditions: See reaction.notes.procedure_det...
10.6084/m9.figshare.5104873.v1
null
Nitrile
null
c1cnccc1
c1cccnc1
c1cccnc1.c1ccccc1
Other
OP(=O)(O)O
null
null
N#Cc1cc(-c2ccc(Cl)cc2)c[nH]c1=O>OP(=O)(O)O>O=c1ccc(-c2ccc(Cl)cc2)c[nH]1
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-c9ccf1c64cef45c9a38e8ebb2cfb10e4
CCC#CCBr.CCCCCC.O=c1cccc[nH]1.[Cl-]>>CCC#CCn1cc(-c2ccc(Cl)cc2)ccc1=O
[Cl-].[NH4+].[H-].[Na+].N1C(C=CC=C1)=O.CCCCCC.C(C)(=O)OCC.BrCC#CCC>>ClC1=CC=C(C=C1)C=1C=CC(N(C1)CC#CCC)=O
Br[CH2:5][C:4]#[C:3][CH2:2][CH3:1].[CH2:9]([CH3:10])[CH2:15][CH2:14][CH2:12][CH3:11].[nH:6]1[cH:7][cH:8][cH:16][cH:17][c:18]1=[O:19].[Cl-:13]>>[CH3:1][CH2:2][C:3]#[C:4][CH2:5][n:6]1[cH:7][c:8](-[c:9]2[cH:10][cH:11][c:12]([Cl:13])[cH:14][cH:15]2)[cH:16][cH:17][c:18]1=[O:19]
CCC#CCBr.CCCCCC.O=c1cccc[nH]1.[Cl-]
CCC#CCn1cc(-c2ccc(Cl)cc2)ccc1=O
null
null
CN(C)C=O
Aromatic Heterocycle Formation
OtherReaction
c16e53991381708a0d74f5092b5e25b0353184189763eaae006dd565c1174ab9
f1e2d48aa3857a2357f3a371c35806794fc7180cbbfa20a78f207e36837e33dc
O=c1ccc(-c2ccccc2)c[nH]1
Br-[CH2;D2;+0:1]-[C:2]#[C:3]-[C:4].[CH3;D1;+0:5]-[CH2;D2;+0:6]-[CH2;D2;+0:7]-[CH2;D2;+0:8]-[CH2;D2;+0:9]-[CH3;D1;+0:10].[Cl-;H0;D0:11].[O;D1;H0:12]=[c:13]1:[c:14]:[c:15]:[cH;D2;+0:16]:[c:17]:[nH;D2;+0:18]:1>>[C:4]-[C:3]#[C:2]-[CH2;D2;+0:1]-[n;H0;D3;+0:18]1:[c:17]:[c;H0;D3;+0:16](-[c;H0;D3;+0:6]2:[cH;D2;+0:5]:[cH;D2;+0:...
null
[]
0
CELSIUS
null
null
To a suspension of NaH (60% in mineral oil, 200 mg) in dry DMF (50 ml) at 0° C. was added the preceding pyridinone and the mixture was stirred at 0° C. for one half hour. To the resulting suspension was added 1-bromo-2-pentyne dropwise. The resulting mixture was kept at 0° C. during one half hour and poured into satura...
10.6084/m9.figshare.5104873.v1
null
Primary halide
Aromatic halide
c1ccccn1
c1ccncc1.c1ccccc1
c1ccncc1.c1ccccc1
HBr
CN(C)C=O
0
null
CCC#CCBr.CCCCCC.O=c1cccc[nH]1.[Cl-]>CN(C)C=O>CCC#CCn1cc(-c2ccc(Cl)cc2)ccc1=O
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-2125b916997c4e6d96420da536d3a807
O=C(C=Cc1ccccc1)Nc1ccc(Cl)cc1>>O=c1ccc2c(Cl)cccc2[nH]1
ClC1=CC=C(C=C1)NC(C=CC1=CC=CC=C1)=O.[Cl-].[Al+3].[Cl-].[Cl-]>>ClC1=C2C=CC(NC2=CC=C1)=O
c1ccc([CH:4]=[CH:3][C:2](=[O:1])[NH:12][c:11]2[cH:5][cH:8][c:6]([Cl:7])[cH:9][cH:10]2)cc1>>[O:1]=[c:2]1[cH:3][cH:4][c:5]2[c:6]([Cl:7])[cH:8][cH:9][cH:10][c:11]2[nH:12]1
O=C(C=Cc1ccccc1)Nc1ccc(Cl)cc1
O=c1ccc2c(Cl)cccc2[nH]1
null
null
ClC1=CC=CC=C1
Reduction
OtherReaction
ebe7e954f82f1e726cf9b7a8863216fec31733c3d8bfbb1cc71c49312cec65ac
10d6d5b071f1d84b20b253ce9eadaed211c373c6ee607356078792f13319351a
O=c1ccc2ccccc2[nH]1
[Cl;D1;H0:1]-[c;H0;D3;+0:2]1:[cH;D2;+0:3]:[cH;D2;+0:4]:[c:5](-[NH;D2;+0:6]-[C;H0;D3;+0:7](=[O;D1;H0:8])-[CH;D2;+0:9]=[CH;D2;+0:10]-c2:c:c:c:c:c:2):[c:11]:[cH;D2;+0:12]:1>>[Cl;D1;H0:1]-[c;H0;D3;+0:2]1:[cH;D2;+0:3]:[cH;D2;+0:12]:[c:11]:[c:5]2:[nH;D2;+0:6]:[c;H0;D3;+0:7](=[O;D1;H0:8]):[cH;D2;+0:9]:[cH;D2;+0:10]:[c;H0;D3;+...
null
[]
125
CELSIUS
3
HOUR
To a mixture of N-(4-chlorophenyl)cinnamamide (8.3 g), and chlorobenzene (60 ml) was added portionwise aluminum chloride (21.4 g) trader nitrogen at room temperature and the reaction mixture was slowly warmed up to 125° C. and kept at that temperature for 3 hours. The reaction mixture was cooled down and poured over 40...
10.6084/m9.figshare.5104873.v1
null
Aromatic halide.Secondary amide
Aromatic halide
c1ccccc1.c1ccccc1
c1ccc2ccccc2n1
c1ccc2ccccc2n1
Other
ClC1=CC=CC=C1
125
3
O=C(C=Cc1ccccc1)Nc1ccc(Cl)cc1>ClC1=CC=CC=C1>O=c1ccc2c(Cl)cccc2[nH]1
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-d9ff793142c547c8aee4d9d896a93b93
CCC#CCBr.O=c1ccc2ccccc2[nH]1.[Cl-]>>CCC#CCn1c(=O)ccc2c(Cl)cccc21
[Cl-].[NH4+].N1C(C=CC2=CC=CC=C12)=O.[H-].[Na+].BrCC#CCC>>ClC1=C2C=CC(N(C2=CC=C1)CC#CCC)=O
Br[CH2:5][C:4]#[C:3][CH2:2][CH3:1].[nH:6]1[c:7](=[O:8])[cH:9][cH:10][c:11]2[cH:12][cH:14][cH:15][cH:16][c:17]12.[Cl-:13]>>[CH3:1][CH2:2][C:3]#[C:4][CH2:5][n:6]1[c:7](=[O:8])[cH:9][cH:10][c:11]2[c:12]([Cl:13])[cH:14][cH:15][cH:16][c:17]12
CCC#CCBr.O=c1ccc2ccccc2[nH]1.[Cl-]
CCC#CCn1c(=O)ccc2c(Cl)cccc21
null
null
CN(C)C=O.CCCCCC
Heteroatom Alkylation and Arylation
OtherReaction
a61336fe7a89ec0981a525297b55629e44e830f13f91df56a44bf01390d8c69d
dbda6588fa29cbbc0e3c3f601e69924b300990bdcc56b8cec0535d1258039346
O=c1ccc2ccccc2[nH]1
Br-[CH2;D2;+0:1]-[C:2]#[C:3]-[C:4].[Cl-;H0;D0:5].[O;D1;H0:6]=[c:7]1:[c:8]:[c:9]:[c:10]2:[cH;D2;+0:11]:[c:12]:[c:13]:[c:14]:[c:15]:2:[nH;D2;+0:16]:1>>[C:4]-[C:3]#[C:2]-[CH2;D2;+0:1]-[n;H0;D3;+0:16]1:[c:15]2:[c:14]:[c:13]:[c:12]:[c;H0;D3;+0:11](-[Cl;H0;D1;+0:5]):[c:10]:2:[c:9]:[c:8]:[c:7]:1=[O;D1;H0:6]
null
[]
0
CELSIUS
null
null
To a suspension of NaH (60% in mineral oil, 700 mg) in dry DMF (100 ml) at 0° C. was added the preceding quinolinone (2.05 g) and the mixture was stirred at 0° C. for one half hour. To the resulting suspension was added 1-bromo-2-pentyne (1.6 g) dropwise. The resulting mixture was kept at 0° C. for one half hour and po...
10.6084/m9.figshare.5104873.v1
null
Primary halide
Aromatic halide
c1ccc2ccccc2n1
c1ccc2ncccc2c1
c1ccc2ncccc2c1
HBr
CN(C)C=O.CCCCCC
0
null
CCC#CCBr.O=c1ccc2ccccc2[nH]1.[Cl-]>CN(C)C=O.CCCCCC>CCC#CCn1c(=O)ccc2c(Cl)cccc21
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-ced4f53fd68e4069b40e335eb3df94b0
CN(C)C=C(C=O)c1ccc(Cl)cc1.NC(N)=O>>O=c1ncc(-c2ccc(Cl)cc2)c[nH]1
[Cl-].[NH4+].ClC1=CC=C(C=C1)C(C=O)=CN(C)C.NC(=O)N.Cl>>ClC1=CC=C(C=C1)C=1C=NC(NC1)=O
CN(C)[CH:4]=[C:5]([c:6]1[cH:7][cH:8][c:9]([Cl:10])[cH:11][cH:12]1)[CH:13]=O.[O:1]=[C:2]([NH2:3])[NH2:14]>>[O:1]=[c:2]1[n:3][cH:4][c:5](-[c:6]2[cH:7][cH:8][c:9]([Cl:10])[cH:11][cH:12]2)[cH:13][nH:14]1
CN(C)C=C(C=O)c1ccc(Cl)cc1.NC(N)=O
O=c1ncc(-c2ccc(Cl)cc2)c[nH]1
null
null
C(C)O.O
Aromatic Heterocycle Formation
OtherReaction
0e1bb7c6fc2fa2fbd0239b648ae136ef123b13ddeb9947c50b8f38d453d7d183
55a949c5abf218b0e7fd0015b81e86fb975fa441e5ac6bd395c3346bb38599f7
O=c1ncc(-c2ccccc2)c[nH]1
C-N(-C)-[CH;D2;+0:1]=[C;H0;D3;+0:2](-[CH;D2;+0:3]=O)-[c;H0;D3;+0:4](:[c:5]:[c:6]):[c:7]:[c:8].[NH2;D1;+0:9]-[C;H0;D3;+0:10](-[NH2;D1;+0:11])=[O;D1;H0:12]>>[O;D1;H0:12]=[c;H0;D3;+0:10]1:[n;H0;D2;+0:11]:[cH;D2;+0:1]:[c;H0;D3;+0:2](-[c;H0;D3;+0:4](:[c:5]:[c:6]):[c:7]:[c:8]):[cH;D2;+0:3]:[nH;D2;+0:9]:1
29.7
[{"value": 29.7, "product": "ClC1=CC=C(C=C1)C=1C=NC(NC1)=O", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
null
null
A mixture of 2-(4-chlorophenyl)dimethylaminopropenal (Example 145a) (5.13 g), urea (2.4 g), concentrated HCl (10 ml), water (4 ml) and ethanol (150 ml) was refluxed for 4 hours. After cooling to room temperature concentrated ammonium chloride was added until the pH was 7. The resulting yellow solid was filtered off and...
10.6084/m9.figshare.5104873.v1
null
Enamine.Aldehyde.Urea
null
null
c1cncnc1
c1cncnc1.c1ccccc1
HO-
C(C)O.O
null
null
CN(C)C=C(C=O)c1ccc(Cl)cc1.NC(N)=O>C(C)O.O>O=c1ncc(-c2ccc(Cl)cc2)c[nH]1
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-0cdfb3a6a39e4aada49cd2cfa61b5f7c
CCC#CCBr.CCCCCC.O=c1cccc[nH]1.[Cl-].[NH4+]>>CCC#CCn1cc(-c2ccc(Cl)cc2)cnc1=O
[Cl-].[NH4+].CCCCCC.[H-].[Na+].N1C(C=CC=C1)=O.BrCC#CCC>>ClC1=CC=C(C=C1)C=1C=NC(N(C1)CC#CCC)=O
Br[CH2:5][C:4]#[C:3][CH2:2][CH3:1].C[CH2:15][CH2:14][CH2:12][CH2:11][CH3:10].[nH:6]1[cH:7][cH:8][cH:16][cH:9][c:18]1=[O:19].[Cl-:13].[NH4+:17]>>[CH3:1][CH2:2][C:3]#[C:4][CH2:5][n:6]1[cH:7][c:8](-[c:9]2[cH:10][cH:11][c:12]([Cl:13])[cH:14][cH:15]2)[cH:16][n:17][c:18]1=[O:19]
CCC#CCBr.CCCCCC.O=c1cccc[nH]1.[Cl-].[NH4+]
CCC#CCn1cc(-c2ccc(Cl)cc2)cnc1=O
null
null
CN(C)C=O
Aromatic Heterocycle Formation
OtherReaction
b4467fdd65493649554b053844b88f7aedac75ecb5e83a2819a9163270cc6b1f
f1e2d48aa3857a2357f3a371c35806794fc7180cbbfa20a78f207e36837e33dc
O=c1ncc(-c2ccccc2)c[nH]1
Br-[CH2;D2;+0:1]-[C:2]#[C:3]-[C:4].C-[CH2;D2;+0:5]-[CH2;D2;+0:6]-[CH2;D2;+0:7]-[CH2;D2;+0:8]-[CH3;D1;+0:9].[Cl-;H0;D0:10].[NH4+;D0:11].[O;D1;H0:12]=[c;H0;D3;+0:13]1:[cH;D2;+0:14]:[cH;D2;+0:15]:[cH;D2;+0:16]:[c:17]:[nH;D2;+0:18]:1>>[C:4]-[C:3]#[C:2]-[CH2;D2;+0:1]-[n;H0;D3;+0:18]1:[c:17]:[c;H0;D3;+0:16](-[c;H0;D3;+0:14]2...
null
[]
0
CELSIUS
null
null
To a suspension of NaH (60% in mineral oil, 340 mg) in dry DMF (75 ml) at 0° C. was added the preceding pyridinone (1.0 g) and the mixture was stirred at 0° C. for one half hour. To the resulting suspension was added 1-bromo-2-pentyne (750 mg) dropwise. The resulting mixture was kept at 0° C. for one half hour and pour...
10.6084/m9.figshare.5104873.v1
null
Primary halide
Aromatic halide
c1ccccn1
c1cncnc1.c1ccccc1
c1cncnc1.c1ccccc1
HBr
CN(C)C=O
0
null
CCC#CCBr.CCCCCC.O=c1cccc[nH]1.[Cl-].[NH4+]>CN(C)C=O>CCC#CCn1cc(-c2ccc(Cl)cc2)cnc1=O
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-a068a7407087432ba77b2eb060642cca
O=c1ccc(-c2ccc(Cl)cc2)n[nH]1.S=P12SP3(=S)SP(=S)(S1)SP(=S)(S2)S3>>S=c1ccc(-c2ccc(Cl)cc2)n[nH]1
ClC1=CC=C(C=C1)C=1C=CC(NN1)=O.P12(=S)SP3(=S)SP(=S)(S1)SP(=S)(S2)S3>>ClC1=CC=C(C=C1)C=1C=CC(NN1)=S
O=[c:2]1[cH:3][cH:4][c:5](-[c:6]2[cH:7][cH:8][c:9]([Cl:10])[cH:11][cH:12]2)[n:13][nH:14]1.S=P12SP3(=S)SP(=S)(S1)SP(=[S:1])(S2)S3>>[S:1]=[c:2]1[cH:3][cH:4][c:5](-[c:6]2[cH:7][cH:8][c:9]([Cl:10])[cH:11][cH:12]2)[n:13][nH:14]1
O=c1ccc(-c2ccc(Cl)cc2)n[nH]1.S=P12SP3(=S)SP(=S)(S1)SP(=S)(S2)S3
S=c1ccc(-c2ccc(Cl)cc2)n[nH]1
null
null
N1=CC=CC=C1
Heteroatom Alkylation and Arylation
OtherReaction
e0da8be0c0e31372bc487fca4d998b8539b7ff5b84df07e1a6200efd3593e0bb
13be3f637e1e22872d741944f46b7fcc1954fe982a3a8a0f7825545d455ab147
S=c1ccc(-c2ccccc2)n[nH]1
O=[c;H0;D3;+0:1]1:[#7;a:2]:[#7;a:3]:[c:4]:[c:5]:[c:6]:1.S=P12-S-P3(=S)-S-P(=S)(-S-1)-S-P(=[S;H0;D1;+0:7])(-S-2)-S-3>>[S;H0;D1;+0:7]=[c;H0;D3;+0:1]1:[#7;a:2]:[#7;a:3]:[c:4]:[c:5]:[c:6]:1
187.1
[{"value": 187.1, "product": "ClC1=CC=C(C=C1)C=1C=CC(NN1)=S", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
null
null
A mixture of 3.0 g of 6-(4-chlorophenyl)-pyridazinone, 50 ml of dry pyridine and 3.2 g of phosphorus pentasulfide was refluxed for 1 hour, evaporated to dryness and extracted with 200 ml of ether. The ether extract was washed with water (3×100 ml), brine (100 ml), dried over magnesium sulfate and evaporated to yield 3....
10.6084/m9.figshare.5104873.v1
null
Monosulfide.Monosulfide.Monosulfide.Monosulfide.Monosulfide.Monosulfide
Thiocarbonyl
c1cccnn1.S1P2SP3SP1SP(S2)S3
c1cccnn1
c1cccnn1.c1ccccc1
Other
N1=CC=CC=C1
null
null
O=c1ccc(-c2ccc(Cl)cc2)n[nH]1.S=P12SP3(=S)SP(=S)(S1)SP(=S)(S2)S3>N1=CC=CC=C1>S=c1ccc(-c2ccc(Cl)cc2)n[nH]1
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-5b77163772334a28b4e039cda3410b19
NNC(=O)c1ccc(Cl)cc1.O=C(Cl)CCl>>O=C(CCl)NNC(=O)c1ccc(Cl)cc1
ClC1=CC=C(C(=O)NN)C=C1.ClCC(=O)Cl>>ClCC(=O)NNC(C1=CC=C(C=C1)Cl)=O
[NH2:5][NH:6][C:7](=[O:8])[c:9]1[cH:10][cH:11][c:12]([Cl:13])[cH:14][cH:15]1.Cl[C:2](=[O:1])[CH2:3][Cl:4]>>[O:1]=[C:2]([CH2:3][Cl:4])[NH:5][NH:6][C:7](=[O:8])[c:9]1[cH:10][cH:11][c:12]([Cl:13])[cH:14][cH:15]1
NNC(=O)c1ccc(Cl)cc1.O=C(Cl)CCl
O=C(CCl)NNC(=O)c1ccc(Cl)cc1
null
null
O1CCOCC1
Acylation
Acylation of Nitrogen Nucleophiles by Acyl/Thioacyl/Carbamoyl Halides and Analogs_OS
e9c0e57fff756e07b8f823de2eed1eeaae995a83400f2b5e18582349988c9a5f
384006bf8ba751654aef497f42d95dd6fc64342c355d6ce7d0ea9a3aaffeacc6
c1ccccc1
Cl-[C;H0;D3;+0:1](=[O;D1;H0:2])-[C:3]-[Cl;D1;H0:4].[NH2;D1;+0:5]-[#7:6]-[C:7](=[O;D1;H0:8])-[c:9]>>[Cl;D1;H0:4]-[C:3]-[C;H0;D3;+0:1](=[O;D1;H0:2])-[NH;D2;+0:5]-[#7:6]-[C:7](=[O;D1;H0:8])-[c:9]
null
[]
null
null
null
null
To a solution of p-chlorobenzoic hydrazide (11.2 g) in dioxane (100 ml) was added chloroacetyl chloride (6 ml). The resulting mixture was refluxed for three hours cooled to room temperature and filtered. The resulting solid was washed with ethyl ether and dried to yield N'-chloroacetyl-4-chlorobenzoic hydrazide as whit...
10.6084/m9.figshare.5104873.v1
null
Acyl halide.Acylhydrazine
Acylhydrazine.Acylhydrazine
null
null
c1ccccc1
HCl
O1CCOCC1
null
null
NNC(=O)c1ccc(Cl)cc1.O=C(Cl)CCl>O1CCOCC1>O=C(CCl)NNC(=O)c1ccc(Cl)cc1
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-3b6843caea374b8d88ee79ad8d8db495
COC(=S)NN.O=C(CBr)c1ccc(Cl)cc1>>O=C1NN=C(c2ccc(Cl)cc2)CS1
BrCC(=O)C1=CC=C(C=C1)Cl.COC(=S)NN>>ClC1=CC=C(C=C1)C1=NNC(SC1)=O
C[O:1][C:2]([NH:3][NH2:4])=[S:14].O=[C:5]([c:6]1[cH:7][cH:8][c:9]([Cl:10])[cH:11][cH:12]1)[CH2:13]Br>>[O:1]=[C:2]1[NH:3][N:4]=[C:5]([c:6]2[cH:7][cH:8][c:9]([Cl:10])[cH:11][cH:12]2)[CH2:13][S:14]1
COC(=S)NN.O=C(CBr)c1ccc(Cl)cc1
O=C1NN=C(c2ccc(Cl)cc2)CS1
null
null
C(C)#N
Acylation
OtherReaction
a0815ff887854434f061e02bb59e65917f2f792eefe3f407e6f67a241e834044
b7ddc8c969600ae9a9b2d12841c66a24307741bcbfc0810c56e58eb7d0e4892d
O=C1NN=C(c2ccccc2)CS1
Br-[CH2;D2;+0:1]-[C;H0;D3;+0:2](=O)-[c:3](:[c:4]):[c:5].C-[O;H0;D2;+0:6]-[C;H0;D3;+0:7](=[S;H0;D1;+0:8])-[#7:9]-[NH2;D1;+0:10]>>[O;H0;D1;+0:6]=[C;H0;D3;+0:7]1-[#7:9]-[N;H0;D2;+0:10]=[C;H0;D3;+0:2](-[c:3](:[c:4]):[c:5])-[CH2;D2;+0:1]-[S;H0;D2;+0:8]-1
48.4
[{"value": 48.4, "product": "ClC1=CC=C(C=C1)C1=NNC(SC1)=O", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
null
null
A mixture of 2-bromo-p-chloroacetophenone (9.16 g), methoxythiocarbonylhydrazine (13.0 g) and acetonitrile (75 ml) was refluxed overnight and then cooled and filtered. The light yellow solid was washed with hexane and dried yielding 5-(4-chlorophenyl)-3H,6H-1,3,4-thiadiazin-2-one (4.3 g). Conditions: See reaction.notes...
10.6084/m9.figshare.5104873.v1
null
Hydrazine.Primary halide.Ketone.Ether.Thioamide
Hydrazone amide.Monosulfide
null
C1=NNCSC1
C1=NNCSC1.c1ccccc1
HBr
C(C)#N
null
null
COC(=S)NN.O=C(CBr)c1ccc(Cl)cc1>C(C)#N>O=C1NN=C(c2ccc(Cl)cc2)CS1
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-d1123e2cb6514274b6960618c4f635b5
O=C(O)CCC(=O)c1cccc(Cl)c1>>O=C(O)CCCc1cccc(Cl)c1
ClC=1C=C(C(=O)CCC(=O)O)C=CC1.[OH-].[K+].NN>>ClC=1C=C(C=CC1)CCCC(=O)O
O=[C:6]([CH2:5][CH2:4][C:2](=[O:1])[OH:3])[c:7]1[cH:8][cH:9][cH:10][c:11]([Cl:12])[cH:13]1>>[O:1]=[C:2]([OH:3])[CH2:4][CH2:5][CH2:6][c:7]1[cH:8][cH:9][cH:10][c:11]([Cl:12])[cH:13]1
O=C(O)CCC(=O)c1cccc(Cl)c1
O=C(O)CCCc1cccc(Cl)c1
null
null
C(COCCO)O
Reduction
OtherReaction
bdac4f77103f4da1c5b42ea95e05b0b7b31176b78204db5f4144ffca7b3d54d5
f9ba67182f94acd5fbe41487f8f71e26bccf898b8fc8091ef46f4363de5628d4
c1ccccc1
O=[C;H0;D3;+0:1](-[C:2]-[C:3]-[C:4](=[O;D1;H0:5])-[O;D1;H1:6])-[c:7](:[c:8]):[c:9]>>[O;D1;H0:5]=[C:4](-[O;D1;H1:6])-[C:3]-[C:2]-[CH2;D2;+0:1]-[c:7](:[c:8]):[c:9]
90.8
[{"value": 90.8, "product": "ClC=1C=C(C=CC1)CCCC(=O)O", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
null
null
To a 300 ml round-bottomed flask equipped with magnetic stirrer and reflux condenser was charged 23.7 g of 87% potassium hydroxide and 150 ml of diethyleneglycol, With stirring, 23 g of 3-(3-chlorobenzoyl)-propionic acid was added followed by 24 g of 85% hydrazine. The mixture was heated to reflux for 2 hours when 50 m...
10.6084/m9.figshare.5104873.v1
null
Ketone
null
null
null
c1ccccc1
Other
C(COCCO)O
null
null
O=C(O)CCC(=O)c1cccc(Cl)c1>C(COCCO)O>O=C(O)CCCc1cccc(Cl)c1
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-0e26495fba2b4cde9bc3510578dfcbbf
CC(=O)CCC(=O)O.O=Cc1ccc(Cl)cc1>>O=C(O)CCC(=O)C=Cc1ccc(Cl)cc1
ClC1=CC=C(C=O)C=C1.C(CCC(=O)C)(=O)O.N1CCCCC1.C1(=CC=CC=C1)C>>ClC1=CC=C(C=CC(=O)CCC(=O)O)C=C1
[O:1]=[C:2]([OH:3])[CH2:4][CH2:5][C:6](=[O:7])[CH3:8].O=[CH:9][c:10]1[cH:11][cH:12][c:13]([Cl:14])[cH:15][cH:16]1>>[O:1]=[C:2]([OH:3])[CH2:4][CH2:5][C:6](=[O:7])[CH:8]=[CH:9][c:10]1[cH:11][cH:12][c:13]([Cl:14])[cH:15][cH:16]1
CC(=O)CCC(=O)O.O=Cc1ccc(Cl)cc1
O=C(O)CCC(=O)C=Cc1ccc(Cl)cc1
null
null
O
C-C Coupling
Aldehyde and ketone to alpha,beta-unsaturated carbonyl
df1bdbab1a06af9561d74fe6bc94ee8bda1d14faad9db1ada3a214bd64a24cf8
c93e93ada40f7f922a54fe24d38f540ecf5ff25d55d497f79f5f400f75d0c7ae
c1ccccc1
O=[CH;D2;+0:1]-[c:2](:[c:3]):[c:4].[C:5]-[C:6](-[CH3;D1;+0:7])=[O;D1;H0:8]>>[C:5]-[C:6](=[O;D1;H0:8])-[CH;D2;+0:7]=[CH;D2;+0:1]-[c:2](:[c:3]):[c:4]
44
[{"value": 44.0, "product": "ClC1=CC=C(C=CC(=O)CCC(=O)O)C=C1", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
null
null
To a dry 250 ml flask equipped with a magnetic stirrer, Dean-Stark trap, and reflux condenser was charged 15 g of 4-chlorobenzaldehyde, 12.4 g levulenic acid, 5.7 ml of piperidine, and 100 ml of toluene. The reaction was refluxed for 3 hours, after which no water was observed to azeotrope from the solution. The reactio...
10.6084/m9.figshare.5104873.v1
null
Aldehyde.Ketone
Ketone
null
null
c1ccccc1
HO-
O
null
null
CC(=O)CCC(=O)O.O=Cc1ccc(Cl)cc1>O>O=C(O)CCC(=O)C=Cc1ccc(Cl)cc1
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-275e8400c15942e28e2a52018fda7f14
COc1ccc(C(=O)[O-])c(C)c1[N+](=O)[O-]>>COc1ccc(C(=O)O)cc1[N+](=O)[O-]
[N+](=O)([O-])C=1C(=C(C(=O)[O-])C=CC1OC)C.[OH-].[K+]>>[N+](=O)([O-])C=1C=C(C(=O)O)C=CC1OC
C[c:10]1[c:6]([C:7](=[O:8])[O-:9])[cH:5][cH:4][c:3]([O:2][CH3:1])[c:11]1[N+:12](=[O:13])[O-:14]>>[CH3:1][O:2][c:3]1[cH:4][cH:5][c:6]([C:7](=[O:8])[OH:9])[cH:10][c:11]1[N+:12](=[O:13])[O-:14]
COc1ccc(C(=O)[O-])c(C)c1[N+](=O)[O-]
COc1ccc(C(=O)O)cc1[N+](=O)[O-]
null
null
O1CCCC1
Miscellaneous
OtherReaction
ec2bcf645eed3485ae21dd491bac7887e7ecc8e6727067de36c08c87eaa3e98c
d003579d88c8e6390ed4fac608b8ce68d334559ff02e2f3d9c9936750b60a874
c1ccccc1
C-[c;H0;D3;+0:1](:[c:2](-[#7;+:3]):[c:4]):[c:5](-[C:6](-[O-;H0;D1:7])=[O;D1;H0:8]):[c:9]>>[#7;+:3]-[c:2](:[c:4]):[cH;D2;+0:1]:[c:5](-[C:6](=[O;D1;H0:8])-[OH;D1;+0:7]):[c:9]
76.6
[{"value": 76.6, "product": "[N+](=O)([O-])C=1C=C(C(=O)O)C=CC1OC", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
12
HOUR
To a 500 ml erlenmeyer flask with magnetic stirrer was charged 10.3 g of 3-nitro-4-methoxy-methylbenzoate, 400 ml tetrahydrofuran, and 3.2 g of 86% potassium hydroxide. The reaction was stirred for 12 hours at ambient temperature, after which the resulting solid was collected by vacuum filtration and washed with 2×100 ...
10.6084/m9.figshare.5104873.v1
null
null
Carboxylic acid
c1ccccc1
c1ccccc1
c1ccccc1
Other
O1CCCC1
null
12
COc1ccc(C(=O)[O-])c(C)c1[N+](=O)[O-]>O1CCCC1>COc1ccc(C(=O)O)cc1[N+](=O)[O-]
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-eb63de3fd8b24647933622c8df3a84d0
O=[N+]([O-])c1cccc(S(=O)(=O)OC[C@@H]2CO2)c1.Oc1ccccc1OCc1ccccc1>>Oc1cccc(C[C@H]2CO2)c1OCc1ccccc1
C(C1=CC=CC=C1)OC1=C(C=CC=C1)O.C([O-])([O-])=O.[K+].[K+].C([C@@H]1CO1)OS(=O)(=O)C1=CC(=CC=C1)[N+](=O)[O-]>>C([C@H]1CO1)C=1C(=C(C=CC1)O)OCC1=CC=CC=C1
O=[N+]([O-])c1cccc(S(=O)(=O)O[CH2:7][C@@H:8]2[CH2:9][O:10]2)c1.[OH:1][c:2]1[cH:3][cH:4][cH:5][cH:6][c:11]1[O:12][CH2:13][c:14]1[cH:15][cH:16][cH:17][cH:18][cH:19]1>>[OH:1][c:2]1[cH:3][cH:4][cH:5][c:6]([CH2:7][C@H:8]2[CH2:9][O:10]2)[c:11]1[O:12][CH2:13][c:14]1[cH:15][cH:16][cH:17][cH:18][cH:19]1
O=[N+]([O-])c1cccc(S(=O)(=O)OC[C@@H]2CO2)c1.Oc1ccccc1OCc1ccccc1
Oc1cccc(C[C@H]2CO2)c1OCc1ccccc1
null
null
CC(=O)C
Functional Group Interconversion
OtherReaction
d85bd53c3531f4545f1b83e87e40f622e30342624aa88fd54162f4caae93acc5
5502ac73153b92df99e08d1f611cc54b4d1dc79aa8af4606001f3dd91f190740
c1ccc(COc2ccccc2C[C@H]2CO2)cc1
O=[N+](-[O-])-c1:c:c:c:c(-S(=O)(=O)-O-[CH2;D2;+0:1]-[C:2]2-[#8:3]-[C:4]-2):c:1.[#8:5]-[c:6](:[c:7]):[cH;D2;+0:8]:[c:9]:[c:10]>>[#8:5]-[c:6](:[c:7]):[c;H0;D3;+0:8](-[CH2;D2;+0:1]-[C:2]1-[#8:3]-[C:4]-1):[c:9]:[c:10]
null
[]
null
null
null
null
A mixture of 2-benzyloxyphenol (900 mg, 4.5 mMol) and potassium carbonate (1.87 g, 13.5 mMol) in acetone (45 ml) was heated under reflux for 15 mins. (S)-Glycidyl-3-nitrobenzenesulphonate (1.0 g, 4.5 mMol) was added and the reaction mixture was heated under reflux for 23 hours. After cooling, the reaction mixture was f...
10.6084/m9.figshare.5104873.v1
null
Nitro group.Sulfonate
null
c1ccccc1.c1ccccc1
c1ccccc1
c1ccccc1.C1CO1.c1ccccc1
HO-
CC(=O)C
null
null
O=[N+]([O-])c1cccc(S(=O)(=O)OC[C@@H]2CO2)c1.Oc1ccccc1OCc1ccccc1>CC(=O)C>Oc1cccc(C[C@H]2CO2)c1OCc1ccccc1
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-7a6d0a34d26147ccbbd1b4a703979302
O=[N+]([O-])c1cccc(S(=O)(=O)OC[C@@H]2CO2)c1.Oc1cccc(OCc2ccccc2)c1>>Oc1cccc(OCc2ccccc2)c1C[C@H]1CO1
C(C1=CC=CC=C1)OC=1C=C(C=CC1)O.C([O-])([O-])=O.[K+].[K+].C([C@@H]1CO1)OS(=O)(=O)C1=CC(=CC=C1)[N+](=O)[O-]>>C([C@H]1CO1)C1=C(C=CC=C1OCC1=CC=CC=C1)O
O=[N+]([O-])c1cccc(S(=O)(=O)O[CH2:16][C@@H:17]2[CH2:18][O:19]2)c1.[OH:1][c:2]1[cH:3][cH:4][cH:5][c:6]([O:7][CH2:8][c:9]2[cH:10][cH:11][cH:12][cH:13][cH:14]2)[cH:15]1>>[OH:1][c:2]1[cH:3][cH:4][cH:5][c:6]([O:7][CH2:8][c:9]2[cH:10][cH:11][cH:12][cH:13][cH:14]2)[c:15]1[CH2:16][C@H:17]1[CH2:18][O:19]1
O=[N+]([O-])c1cccc(S(=O)(=O)OC[C@@H]2CO2)c1.Oc1cccc(OCc2ccccc2)c1
Oc1cccc(OCc2ccccc2)c1C[C@H]1CO1
null
null
CC(=O)C
Functional Group Interconversion
OtherReaction
d85bd53c3531f4545f1b83e87e40f622e30342624aa88fd54162f4caae93acc5
5502ac73153b92df99e08d1f611cc54b4d1dc79aa8af4606001f3dd91f190740
c1ccc(COc2ccccc2C[C@H]2CO2)cc1
O=[N+](-[O-])-c1:c:c:c:c(-S(=O)(=O)-O-[CH2;D2;+0:1]-[C:2]2-[#8:3]-[C:4]-2):c:1.[#8:5]-[c:6](:[c:7]):[cH;D2;+0:8]:[c:9](-[O;D1;H1:10]):[c:11]>>[#8:5]-[c:6](:[c:7]):[c;H0;D3;+0:8](-[CH2;D2;+0:1]-[C:2]1-[#8:3]-[C:4]-1):[c:9](-[O;D1;H1:10]):[c:11]
null
[]
null
null
null
null
A mixture of 3-benzyloxyphenol (900 mg, 4.5 mMol) and potassium carbonate (1.87 g, 13.5 mMol) in acetone (45 ml) was heated under reflux for 15 mins. (S)-Glycidyl-3-nitrobenzenesulphonate (1.0 g, 4.5 mMol) was added and the reaction mixture was heated under reflux for 23 hours. After cooling the reaction mixture was fi...
10.6084/m9.figshare.5104873.v1
null
Nitro group.Sulfonate
null
c1ccccc1.c1ccccc1
c1ccccc1
c1ccccc1.c1ccccc1.C1CO1
HO-
CC(=O)C
null
null
O=[N+]([O-])c1cccc(S(=O)(=O)OC[C@@H]2CO2)c1.Oc1cccc(OCc2ccccc2)c1>CC(=O)C>Oc1cccc(OCc2ccccc2)c1C[C@H]1CO1
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-f128083fd7554ead9f40eeecd8845c28
O=[N+]([O-])c1cccc(S(=O)(=O)OC[C@@H]2CO2)c1.Oc1ccc(OCc2ccccc2)cc1>>Oc1ccc(OCc2ccccc2)cc1C[C@H]1CO1
C(C1=CC=CC=C1)OC1=CC=C(C=C1)O.C([O-])([O-])=O.[K+].[K+].C([C@@H]1CO1)OS(=O)(=O)C1=CC(=CC=C1)[N+](=O)[O-]>>C([C@H]1CO1)C1=C(C=CC(=C1)OCC1=CC=CC=C1)O
O=[N+]([O-])c1cccc(S(=O)(=O)O[CH2:16][C@@H:17]2[CH2:18][O:19]2)c1.[OH:1][c:2]1[cH:3][cH:4][c:5]([O:6][CH2:7][c:8]2[cH:9][cH:10][cH:11][cH:12][cH:13]2)[cH:14][cH:15]1>>[OH:1][c:2]1[cH:3][cH:4][c:5]([O:6][CH2:7][c:8]2[cH:9][cH:10][cH:11][cH:12][cH:13]2)[cH:14][c:15]1[CH2:16][C@H:17]1[CH2:18][O:19]1
O=[N+]([O-])c1cccc(S(=O)(=O)OC[C@@H]2CO2)c1.Oc1ccc(OCc2ccccc2)cc1
Oc1ccc(OCc2ccccc2)cc1C[C@H]1CO1
null
null
CC(=O)C
Functional Group Interconversion
OtherReaction
d85bd53c3531f4545f1b83e87e40f622e30342624aa88fd54162f4caae93acc5
5502ac73153b92df99e08d1f611cc54b4d1dc79aa8af4606001f3dd91f190740
c1ccc(COc2cccc(C[C@H]3CO3)c2)cc1
O=[N+](-[O-])-c1:c:c:c:c(-S(=O)(=O)-O-[CH2;D2;+0:1]-[C:2]2-[#8:3]-[C:4]-2):c:1.[O;D1;H1:5]-[c:6](:[c:7]):[cH;D2;+0:8]:[c:9]:[c:10]>>[O;D1;H1:5]-[c:6](:[c:7]):[c;H0;D3;+0:8](-[CH2;D2;+0:1]-[C:2]1-[#8:3]-[C:4]-1):[c:9]:[c:10]
null
[]
null
null
null
null
A mixture of 4-benzyloxyphenol (2.0 g, 10 mMol) and potassium carbonate (4.14 g, 30 mMol) in acetone (50 ml) was heated under reflux for 15 mins. (S)-Glycidyl-3-nitrobenzenesulphonate (2.23 g, 10 mMol) was added and the reaction mixture was heated under reflux for 18 hours. After cooling, the reaction mixture was filte...
10.6084/m9.figshare.5104873.v1
null
Nitro group.Sulfonate
null
c1ccccc1.c1ccccc1
c1ccccc1
c1ccccc1.c1ccccc1.C1CO1
HO-
CC(=O)C
null
null
O=[N+]([O-])c1cccc(S(=O)(=O)OC[C@@H]2CO2)c1.Oc1ccc(OCc2ccccc2)cc1>CC(=O)C>Oc1ccc(OCc2ccccc2)cc1C[C@H]1CO1
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-d01bdcbca7ae4670b375df3584280165
COC(=O)c1cc(OCc2ccccc2)ccc1O>>OCc1cc(OCc2ccccc2)ccc1O
[H-].[Al+3].[Li+].[H-].[H-].[H-].COC(C1=C(C=CC(=C1)OCC1=CC=CC=C1)O)=O>>C(C1=CC=CC=C1)OC1=CC(=C(C=C1)O)CO
CO[C:2](=[O:1])[c:3]1[cH:4][c:5]([O:6][CH2:7][c:8]2[cH:9][cH:10][cH:11][cH:12][cH:13]2)[cH:14][cH:15][c:16]1[OH:17]>>[OH:1][CH2:2][c:3]1[cH:4][c:5]([O:6][CH2:7][c:8]2[cH:9][cH:10][cH:11][cH:12][cH:13]2)[cH:14][cH:15][c:16]1[OH:17]
COC(=O)c1cc(OCc2ccccc2)ccc1O
OCc1cc(OCc2ccccc2)ccc1O
null
null
O1CCCC1
Reduction
Reduction of ester to primary alcohol
21d61543c6ec8a8cebe1b3ef55ef3dd20acbf79a4f1c12a7fb51e32be7a3248a
1fbcd628a0426673c5d10aa49a977cd2d1ae02a8cdf57bbb10d94aa03a94e937
c1ccc(COc2ccccc2)cc1
C-O-[C;H0;D3;+0:1](=[O;H0;D1;+0:2])-[c:3](:[c:4]):[c:5]>>[OH;D1;+0:2]-[CH2;D2;+0:1]-[c:3](:[c:4]):[c:5]
null
[]
0
CELSIUS
20
MINUTE
Lithium aluminium hydride (0.235 g, 6.2 mMol) was suspended in tetrahydrofuran (25 ml) and cooled to 0° C. 5-Benzyloxy-2-hydroxy benzoic acid methyl ester (2 g, 7.75 mMol) in tetrahydrofuran (10 ml) was added dropwise, via cannula. The mixture was warmed to room temperature and stirred for 20 minutes. The reaction was ...
10.6084/m9.figshare.5104873.v1
null
Ester
Primary alcohol
null
null
c1ccccc1.c1ccccc1
Other
O1CCCC1
0
0.333333
COC(=O)c1cc(OCc2ccccc2)ccc1O>O1CCCC1>OCc1cc(OCc2ccccc2)ccc1O
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-86f5e49c8e57407dadc506848462b455
COC(=O)COc1ccc(C[C@@H](C)N)cc1.c1ccc(COc2ccc(OC[C@@H]3CO3)cc2OCc2ccccc2)cc1>>COC(=O)COc1ccc(CC(C)NCC(O)COc2ccc(OCc3ccccc3)c(OCc3ccccc3)c2)cc1
C(C1=CC=CC=C1)OC=1C=C(OC[C@@H]2CO2)C=CC1OCC1=CC=CC=C1.COC(COC1=CC=C(C=C1)C[C@@H](C)N)=O>>C(C1=CC=CC=C1)OC=1C=C(OCC(CNC(CC2=CC=C(OCC(=O)OC)C=C2)C)O)C=CC1OCC1=CC=CC=C1
[CH3:1][O:2][C:3](=[O:4])[CH2:5][O:6][c:7]1[cH:8][cH:9][c:10]([CH2:11][C@@H:12]([CH3:13])[NH2:14])[cH:42][cH:43]1.[CH2:15]1[C@@H:16]([CH2:18][O:19][c:20]2[cH:21][cH:22][c:23]([O:24][CH2:25][c:26]3[cH:27][cH:28][cH:29][cH:30][cH:31]3)[c:32]([O:33][CH2:34][c:35]3[cH:36][cH:37][cH:38][cH:39][cH:40]3)[cH:41]2)[O:17]1>>[CH3...
COC(=O)COc1ccc(C[C@@H](C)N)cc1.c1ccc(COc2ccc(OC[C@@H]3CO3)cc2OCc2ccccc2)cc1
COC(=O)COc1ccc(CC(C)NCC(O)COc2ccc(OCc3ccccc3)c(OCc3ccccc3)c2)cc1
null
null
null
Heteroatom Alkylation and Arylation
OtherReaction
f75f8fec78b0ee9c8e880101c8c57c2a3edaac070bc7ad0163a34826e2af8c65
04c78336d85647f6dca3040f384f77009d1b541aac7f8ccf33aa9798091ceab8
c1ccc(CCNCCCOc2ccc(OCc3ccccc3)c(OCc3ccccc3)c2)cc1
[#8:1]-[C:2]-[C@@H;D3;+0:3]1-[CH2;D2;+0:4]-[O;H0;D2;+0:5]-1.[C;D1;H3:6]-[C@@H;D3;+0:7](-[NH2;D1;+0:8])-[C:9]-[c:10]>>[#8:1]-[C:2]-[CH;D3;+0:3](-[OH;D1;+0:5])-[CH2;D2;+0:4]-[NH;D2;+0:8]-[CH;D3;+0:7](-[C;D1;H3:6])-[C:9]-[c:10]
null
[]
null
null
null
null
The title compound was prepared from (S)-3-(3,4-dibenzyloxyphenoxy)-1,2-epoxypropane and (R)-4-(2-aminopropyl)phenoxyacetic acid methyl ester according to the method described in Procedure 13. Conditions: See reaction.notes.procedure_details.
10.6084/m9.figshare.5104873.v1
null
Ether.Primary amine
Secondary alcohol.Secondary amine
C1CO1
null
c1ccccc1.c1ccccc1.c1ccccc1.c1ccccc1
null
null
null
null
COC(=O)COc1ccc(C[C@@H](C)N)cc1.c1ccc(COc2ccc(OC[C@@H]3CO3)cc2OCc2ccccc2)cc1>>COC(=O)COc1ccc(CC(C)NCC(O)COc2ccc(OCc3ccccc3)c(OCc3ccccc3)c2)cc1
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-a3c93df638364213adea34d2adfb06d5
COc1ccc(C[C@@H](C)N)cc1OC>>C[C@@H](N)Cc1ccc(O)c(O)c1
COC=1C=C(C=CC1OC)C[C@@H](C)N.Br>>Br.OC=1C=C(C=CC1O)C[C@@H](C)N
C[O:10][c:9]1[cH:8][cH:7][c:6]([CH2:5][C@@H:3]([CH3:2])[NH2:4])[cH:13][c:11]1[O:12]C>>[CH3:2][C@@H:3]([NH2:4])[CH2:5][c:6]1[cH:7][cH:8][c:9]([OH:10])[c:11]([OH:12])[cH:13]1
COc1ccc(C[C@@H](C)N)cc1OC
C[C@@H](N)Cc1ccc(O)c(O)c1
null
null
null
Deprotection
OtherReaction
a0f05885bbc65ae2846cad0ac34029941211b2ef3a426958b0c8aa83bb16fe86
9df751cd682ad9d54ed75d7313aaead6a019c5d37ede15c4672866d319b900ff
c1ccccc1
C-[O;H0;D2;+0:1]-[c:2](:[c:3]):[c:4](-[O;H0;D2;+0:5]-C):[c:6]>>[OH;D1;+0:1]-[c:2](:[c:3]):[c:4](-[OH;D1;+0:5]):[c:6]
null
[]
null
null
null
null
A solution of (R)-3-(3,4-dimethoxyphenyl)-2-propylamine hydrochloride1 (500 mg, 2.15 mMol) in hydrogen bromide (48%, 5 ml) was stirred at 100° C. under an argon atmosphere for 20 hours. After cooling, the solvent was evaporated and the residue was dried giving the title compound. Conditions: See reaction.notes.procedur...
10.6084/m9.figshare.5104873.v1
null
Ether.Ether
Aromatic alcohol.Aromatic alcohol
null
null
c1ccccc1
Other
null
null
null
COc1ccc(C[C@@H](C)N)cc1OC>>C[C@@H](N)Cc1ccc(O)c(O)c1
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-15507b7830194c87ab4d8306a193e36d
CCOC(=O)C(Br)(Br)C(=O)OCC.C[C@@H](CNC(=O)OC(C)(C)C)c1ccc(O)c(O)c1>>CCOC(=O)C1(C(=O)OCC)Oc2ccc(C[C@@H](C)NC(=O)OC(C)(C)C)cc2O1
C([O-])([O-])=O.[K+].[K+].BrC(C(=O)OCC)(C(=O)OCC)Br.OC=1C=C(C=CC1O)[C@H](CNC(OC(C)(C)C)=O)C>>C(C)(C)(C)OC(=O)N[C@@H](CC1=CC2=C(OC(O2)(C(=O)OCC)C(=O)OCC)C=C1)C
Br[C:6](Br)([C:4]([O:3][CH2:2][CH3:1])=[O:5])[C:7](=[O:8])[O:9][CH2:10][CH3:11].[OH:12][c:13]1[cH:14][cH:15][c:16]([C@H:18]([CH2:17][NH:20][C:21](=[O:22])[O:23][C:24]([CH3:25])([CH3:26])[CH3:27])[CH3:19])[cH:28][c:29]1[OH:30]>>[CH3:1][CH2:2][O:3][C:4](=[O:5])[C:6]1([C:7](=[O:8])[O:9][CH2:10][CH3:11])[O:12][c:13]2[cH:14...
CCOC(=O)C(Br)(Br)C(=O)OCC.C[C@@H](CNC(=O)OC(C)(C)C)c1ccc(O)c(O)c1
CCOC(=O)C1(C(=O)OCC)Oc2ccc(C[C@@H](C)NC(=O)OC(C)(C)C)cc2O1
null
null
CC(=O)C
Heteroatom Alkylation and Arylation
OtherReaction
de476b63dc919a8f3e80de3a61a89ffd2470b06a92be1eaaaddf4be8e0f44b66
a86729b0879fcb1fe9a0b2a5ed2b34c3c74bcee429454486f23c56ed9ecb94bf
c1ccc2c(c1)OCO2
Br-[C;H0;D4;+0:1](-Br)(-[C:2](=[O;D1;H0:3])-[#8:4]-[C:5])-[C:6](=[O;D1;H0:7])-[#8:8]-[C:9].[C;D1;H3:10]-[C@@H;D3;+0:11](-[CH2;D2;+0:12]-[NH;D2;+0:13]-[C:14](=[O;D1;H0:15])-[#8:16]-[C:17](-[C;D1;H3:18])(-[C;D1;H3:19])-[C;D1;H3:20])-[c;H0;D3;+0:21]1:[c:22]:[c:23]:[c:24](-[OH;D1;+0:25]):[c:26](-[OH;D1;+0:27]):[c:28]:1>>[C...
null
[]
60
CELSIUS
1
HOUR
A solution of (R)-2-(3,4-dihydroxyphenyl)propylcarbamic acid, t-butyl ester. (1.07 g, 4 mMol) in acetone (25 ml) containing potassium carbonate (3 equiv, 1.66 g, 12 mMol) was stirred at 60° C. under an argon atmosphere for 1 hour. After cooling to ambient temperature, a solution of diethyl dibromomalonate (1.27 g, 4 mM...
10.6084/m9.figshare.5104873.v1
null
Tertiary halide.Tertiary halide.Carbamic ester.Ester.Ester.Aromatic alcohol.Aromatic alcohol
Carbamic ester.Ester.Ester.Ether.Ether
c1ccccc1
c1ccc2c(c1)OCO2
c1ccc2c(c1)OCO2
HBr
CC(=O)C
60
1
CCOC(=O)C(Br)(Br)C(=O)OCC.C[C@@H](CNC(=O)OC(C)(C)C)c1ccc(O)c(O)c1>CC(=O)C>CCOC(=O)C1(C(=O)OCC)Oc2ccc(C[C@@H](C)NC(=O)OC(C)(C)C)cc2O1
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-bd1ea3526e084bb093238986ab53097a
CCOC(=O)C1(C(=O)OCC)Oc2ccc(C[C@@H](C)NC(=O)OC(C)(C)C)cc2O1>>CCOC(=O)C1(C(=O)OCC)Oc2ccc(C[C@@H](C)N)cc2O1
C(C)OC(=O)C1(OC2=C(O1)C=CC(=C2)C[C@@H](C)NC(=O)OC(C)(C)C)C(=O)OCC.C(C)OCC.Cl>>Cl.N[C@@H](CC1=CC2=C(OC(O2)(C(=O)OCC)C(=O)OCC)C=C1)C
CC(C)(C)OC(=O)[NH:20][C@@H:18]([CH2:17][c:16]1[cH:15][cH:14][c:13]2[c:22]([cH:21]1)[O:23][C:6]([C:4]([O:3][CH2:2][CH3:1])=[O:5])([C:7](=[O:8])[O:9][CH2:10][CH3:11])[O:12]2)[CH3:19]>>[CH3:1][CH2:2][O:3][C:4](=[O:5])[C:6]1([C:7](=[O:8])[O:9][CH2:10][CH3:11])[O:12][c:13]2[cH:14][cH:15][c:16]([CH2:17][C@@H:18]([CH3:19])[NH...
CCOC(=O)C1(C(=O)OCC)Oc2ccc(C[C@@H](C)NC(=O)OC(C)(C)C)cc2O1
CCOC(=O)C1(C(=O)OCC)Oc2ccc(C[C@@H](C)N)cc2O1
null
null
C(C)(=O)OCC
Reduction
Hydrogenolysis of amides/imides/carbamates
3c33dd2a2d355ee5ba0287367e209aa147a39aa00607f0c95fb2bf1ade45d014
c5b5dffe7dd8beebdc1baa8b5b05300a9f7079e65dcfd42ade6f8a77ff09537d
c1ccc2c(c1)OCO2
C-C(-C)(-C)-O-C(=O)-[NH;D2;+0:1]-[C:2](-[C:3])-[C;D1;H3:4]>>[C:3]-[C:2](-[C;D1;H3:4])-[NH2;D1;+0:1]
null
[]
null
null
null
null
A solution of (R)-5-[N-(t-butyloxycarbonyl)-2-aminopropyl]-1,3-benzodioxole-2,2-dicarboxylic acid diethyl ester (3.0 g, 7 mMol) in ethyl acetate (40 ml) and hydrogen chloride solution in diethyl ether (1M, 56 ml, 56 mMol) was stirred at ambient temperature under an argon atmosphere for 48 hours. The solvent was evapora...
10.6084/m9.figshare.5104873.v1
null
Carbamic ester.Ether.Boc
Primary amine
null
null
c1ccc2c(c1)OCO2
HO-
C(C)(=O)OCC
null
null
CCOC(=O)C1(C(=O)OCC)Oc2ccc(C[C@@H](C)NC(=O)OC(C)(C)C)cc2O1>C(C)(=O)OCC>CCOC(=O)C1(C(=O)OCC)Oc2ccc(C[C@@H](C)N)cc2O1
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-5e96551488e842a0ae7a5944f04ecff0
CCOP(=O)(COS(=O)(=O)c1ccc(Cl)cc1)OCC.O=C(O)NCCc1ccc(O)cc1>>CCOP(=O)(COc1ccc(CCNC(=O)OC(C)(C)C)cc1)OCC
C(C)OP(OCC)(=O)COS(=O)(=O)C1=CC=C(C=C1)Cl.[H-].[Na+].OC1=CC=C(C=C1)CCNC(O)=O.O>>C(C)(C)(C)OC(=O)NCCC1=CC=C(OCP(OCC)(OCC)=O)C=C1
O=S(=O)(O[CH2:6][P:4]([O:3][CH2:2][CH3:1])(=[O:5])[O:24][CH2:25][CH3:26])c1c[cH:19][c:18](Cl)[cH:20][cH:21]1.[OH:7][c:8]1[cH:9][cH:10][c:11]([CH2:12][CH2:13][NH:14][C:15](=[O:16])[OH:17])[cH:22][cH:23]1>>[CH3:1][CH2:2][O:3][P:4](=[O:5])([CH2:6][O:7][c:8]1[cH:9][cH:10][c:11]([CH2:12][CH2:13][NH:14][C:15](=[O:16])[O:17][...
CCOP(=O)(COS(=O)(=O)c1ccc(Cl)cc1)OCC.O=C(O)NCCc1ccc(O)cc1
CCOP(=O)(COc1ccc(CCNC(=O)OC(C)(C)C)cc1)OCC
null
null
CS(=O)C
Heteroatom Alkylation and Arylation
OtherReaction
7fbeef5523bed283442829ff1014a5b4867a48e8acae5f082f9dcee58e2d0312
ce8f0489d71ba4094431209bdeaacc87eb9195031b5a70c3e3935924bafae50e
c1ccccc1
Cl-[c;H0;D3;+0:1]1:[cH;D2;+0:2]:c:c(-S(=O)(=O)-O-[CH2;D2;+0:3]-[#15:4](-[#8:5])(-[#8:6])=[O;D1;H0:7]):[cH;D2;+0:8]:[cH;D2;+0:9]:1.[C:10]-[#7:11]-[C:12](=[O;D1;H0:13])-[OH;D1;+0:14].[OH;D1;+0:15]-[c:16](:[c:17]):[c:18]>>[#8:5]-[#15:4](-[#8:6])(=[O;D1;H0:7])-[CH2;D2;+0:3]-[O;H0;D2;+0:15]-[c:16](:[c:17]):[c:18].[C:10]-[#7...
null
[]
null
null
null
null
A solution of 2-(4-hydroxyphenyl)ethylcarbamic acid, t-butyl ester1 (4.0 g, 16.9 mMol) in dry DMSO (37.5 ml) was cooled in an ice-bath and treated with sodium hydride (80% in mineral oil 0.557 g, 1.1 equiv) with stirring under argon according to the method described by Cornforth2. When effervescence ceased a solution o...
10.6084/m9.figshare.5104873.v1
null
Aromatic halide.Carbamic acid.Aromatic alcohol.Sulfonate
Carbamic ester.Ether.Ether.Boc
c1ccccc1
null
c1ccccc1
Other
CS(=O)C
null
null
CCOP(=O)(COS(=O)(=O)c1ccc(Cl)cc1)OCC.O=C(O)NCCc1ccc(O)cc1>CS(=O)C>CCOP(=O)(COc1ccc(CCNC(=O)OC(C)(C)C)cc1)OCC
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-37aef411031a48079180fe910acb60fa
CCOP(=O)(COc1ccc(CCNC(=O)OC(C)(C)C)cc1)OCC>>CCOP(=O)(COc1ccc(CCN)cc1)OCC
C(C)(C)(C)OC(=O)NCCC1=CC=C(OCP(OCC)(OCC)=O)C=C1>>NCCC1=CC=C(OCP(OCC)(OCC)=O)C=C1
CC(C)(C)OC(=O)[NH:14][CH2:13][CH2:12][c:11]1[cH:10][cH:9][c:8]([O:7][CH2:6][P:4]([O:3][CH2:2][CH3:1])(=[O:5])[O:17][CH2:18][CH3:19])[cH:16][cH:15]1>>[CH3:1][CH2:2][O:3][P:4](=[O:5])([CH2:6][O:7][c:8]1[cH:9][cH:10][c:11]([CH2:12][CH2:13][NH2:14])[cH:15][cH:16]1)[O:17][CH2:18][CH3:19]
CCOP(=O)(COc1ccc(CCNC(=O)OC(C)(C)C)cc1)OCC
CCOP(=O)(COc1ccc(CCN)cc1)OCC
null
null
C(Cl)Cl.FC(C(=O)O)(F)F
Reduction
Hydrogenolysis of amides/imides/carbamates
3c33dd2a2d355ee5ba0287367e209aa147a39aa00607f0c95fb2bf1ade45d014
c5b5dffe7dd8beebdc1baa8b5b05300a9f7079e65dcfd42ade6f8a77ff09537d
c1ccccc1
C-C(-C)(-C)-O-C(=O)-[NH;D2;+0:1]-[C:2]-[C:3]>>[C:3]-[C:2]-[NH2;D1;+0:1]
null
[]
null
null
null
null
4-(2-t-Butoxycarbonylaminoethyl)phenoxymethylphosphonic acid, diethyl ester (2.856 g, 9.95 mMol) in methylene chloride (300 ml) and trifluoracetic acid (16 ml) was stirred at room temperature for 5 h. The solution was concentrated under reduced pressure and product dried under in vacuo. The trifluoacetic acid salt was ...
10.6084/m9.figshare.5104873.v1
null
Carbamic ester.Ether.Boc
Primary amine
null
null
c1ccccc1
HO-
C(Cl)Cl.FC(C(=O)O)(F)F
null
null
CCOP(=O)(COc1ccc(CCNC(=O)OC(C)(C)C)cc1)OCC>C(Cl)Cl.FC(C(=O)O)(F)F>CCOP(=O)(COc1ccc(CCN)cc1)OCC
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-1f90df0f79374e948d81d55edfef11d9
COC(=O)CBr.C[C@H](Cc1ccc(O)cc1)NC(=O)OC(C)(C)C>>COC(=O)COc1ccc(C[C@@H](C)NC(=O)OC(C)(C)C)cc1
C([O-])([O-])=O.[K+].[K+].OC1=CC=C(C=C1)C[C@@H](C)NC(OC(C)(C)C)=O.BrCC(=O)OC>>C(C)(C)(C)OC(=O)N[C@@H](CC1=CC=C(OCC(=O)OC)C=C1)C
Br[CH2:5][C:3]([O:2][CH3:1])=[O:4].[OH:6][c:7]1[cH:8][cH:9][c:10]([CH2:11][C@@H:12]([CH3:13])[NH:14][C:15](=[O:16])[O:17][C:18]([CH3:19])([CH3:20])[CH3:21])[cH:22][cH:23]1>>[CH3:1][O:2][C:3](=[O:4])[CH2:5][O:6][c:7]1[cH:8][cH:9][c:10]([CH2:11][C@@H:12]([CH3:13])[NH:14][C:15](=[O:16])[O:17][C:18]([CH3:19])([CH3:20])[CH3...
COC(=O)CBr.C[C@H](Cc1ccc(O)cc1)NC(=O)OC(C)(C)C
COC(=O)COc1ccc(C[C@@H](C)NC(=O)OC(C)(C)C)cc1
null
null
CC(=O)C
Heteroatom Alkylation and Arylation
Williamson Ether Synthesis
50d675b335c583a6ce22e1164b27a78b18b9ca447d45137820c344bcb6369217
0865de4e1853c59ac25437e36fd18b03329566cb9eff4b4f0ce70d5714692fd3
c1ccccc1
Br-[CH2;D2;+0:1]-[C:2](=[O;D1;H0:3])-[#8:4]-[C;D1;H3:5].[OH;D1;+0:6]-[c:7](:[c:8]):[c:9]>>[C;D1;H3:5]-[#8:4]-[C:2](=[O;D1;H0:3])-[CH2;D2;+0:1]-[O;H0;D2;+0:6]-[c:7](:[c:8]):[c:9]
null
[]
null
null
null
null
Potassium carbonate (1.95 g, 14.2 mMol) was added to a solution of (R)-2-(4-hydroxyphenyl)-1-methylethylcarbamic acid, t-butyl ester (2.96 g, 11.8 mMol) in acetone (50 ml) at room temperature under argon. Methyl bromoacetate (1.81 g, 11.8 mMol) was added dropwise and the reaction mixture was heated at reflux for 3 hour...
10.6084/m9.figshare.5104873.v1
null
Primary halide.Ester.Aromatic alcohol
Ester.Ether
null
null
c1ccccc1
HBr
CC(=O)C
null
null
COC(=O)CBr.C[C@H](Cc1ccc(O)cc1)NC(=O)OC(C)(C)C>CC(=O)C>COC(=O)COc1ccc(C[C@@H](C)NC(=O)OC(C)(C)C)cc1
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-925d657bfda44fcdaa2c7275376e5fb5
C=CCOCc1ccccc1.O=[PH2]O>>O=[PH](O)CCCOCc1ccccc1
C(C=C)OCC1=CC=CC=C1.[PH2](O)=O>>C(C1=CC=CC=C1)OCCCP(O)=O
[CH2:4]=[CH:5][CH2:6][O:7][CH2:8][c:9]1[cH:10][cH:11][cH:12][cH:13][cH:14]1.[O:1]=[PH2:2][OH:3]>>[O:1]=[PH:2]([OH:3])[CH2:4][CH2:5][CH2:6][O:7][CH2:8][c:9]1[cH:10][cH:11][cH:12][cH:13][cH:14]1
C=CCOCc1ccccc1.O=[PH2]O
O=[PH](O)CCCOCc1ccccc1
null
null
null
Miscellaneous
OtherReaction
57a64b6b42d462fe8276aa79a48b5b98ebab75830adad1905b3795c71ea65b06
b53d8f361e43dc967c3023dcafe218466acf623d0cf729a1557a2a80217926eb
c1ccccc1
[#8:1]-[C:2]-[CH;D2;+0:3]=[CH2;D1;+0:4].[O;D1;H0:5]=[PH2;D2;+0:6]-[O;D1;H1:7]>>[#8:1]-[C:2]-[CH2;D2;+0:3]-[CH2;D2;+0:4]-[PH;D3;+0:6](=[O;D1;H0:5])-[O;D1;H1:7]
null
[]
null
null
null
null
The title compound was prepared from allylbenzyl ether and 50% aqueous phosphinic acid by an analogous procedure to that described in J. Inorg. Nucl. Chem., 1965, 27, 697. Conditions: See reaction.notes.procedure_details.
10.6084/m9.figshare.5104873.v1
null
Allyl
null
null
null
c1ccccc1
null
null
null
null
C=CCOCc1ccccc1.O=[PH2]O>>O=[PH](O)CCCOCc1ccccc1
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-5e782fbe5d444dfdbc8456bc63b99809
C=O.CCCCO[PH](=O)CCCOCc1ccccc1>>CCCCOP(=O)(CO)CCCOCc1ccccc1
C(CCC)OP(=O)CCCOCC1=CC=CC=C1.C=O>>C(C1=CC=CC=C1)OCCCP(OCCCC)(=O)CO
[CH2:8]=[O:9].[CH3:1][CH2:2][CH2:3][CH2:4][O:5][PH:6](=[O:7])[CH2:10][CH2:11][CH2:12][O:13][CH2:14][c:15]1[cH:16][cH:17][cH:18][cH:19][cH:20]1>>[CH3:1][CH2:2][CH2:3][CH2:4][O:5][P:6](=[O:7])([CH2:8][OH:9])[CH2:10][CH2:11][CH2:12][O:13][CH2:14][c:15]1[cH:16][cH:17][cH:18][cH:19][cH:20]1
C=O.CCCCO[PH](=O)CCCOCc1ccccc1
CCCCOP(=O)(CO)CCCOCc1ccccc1
null
null
null
Miscellaneous
OtherReaction
ff9e019412f5fb147910daaf4ee10ff7abac3966a22d93efa93ff9552cbbbf9e
a07b6e0bbdb5ea0627df192b2885de7d34cb5e55531d8d5102717495a910d9a6
c1ccccc1
[CH2;D1;+0:1]=[O;H0;D1;+0:2].[C:3]-[C:4]-[PH;D3;+0:5](=[O;D1;H0:6])-[#8:7]-[C:8]>>[C:3]-[C:4]-[P;H0;D4;+0:5](=[O;D1;H0:6])(-[#8:7]-[C:8])-[CH2;D2;+0:1]-[OH;D1;+0:2]
null
[]
null
null
null
null
The title compound was prepared from 3-benzyloxypropylphosphinic acid n-butyl ester and paraformaldehyde according to the method described in Procedure 31. Purification by chromatography, eluting with dichloromethane containing 5% methanol, gave an oil. Conditions: See reaction.notes.procedure_details. Workup: Purifica...
10.6084/m9.figshare.5104873.v1
null
Formaldehyde
Primary alcohol
null
null
c1ccccc1
null
null
null
null
C=O.CCCCO[PH](=O)CCCOCc1ccccc1>>CCCCOP(=O)(CO)CCCOCc1ccccc1
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-d7fbc646e6f24341bd3baed08edf1bc8
CC(C)(C)OC(=O)NCCc1ccc(O)cc1.CCCCOP(=O)(CCCOCc1ccccc1)COS(=O)(=O)c1ccc(Cl)cc1>>CCCCOP(=O)(CCCOCc1ccccc1)COc1ccc(CCNC(=O)OC(C)(C)C)cc1
C(C1=CC=CC=C1)OCCCP(OCCCC)(=O)COS(=O)(=O)C1=CC=C(C=C1)Cl.OC1=CC=C(C=C1)CCNC(OC(C)(C)C)=O>>C(C)(C)(C)OC(=O)NCCC1=CC=C(OCP(OCCCC)(=O)CCCOCC2=CC=CC=C2)C=C1
[OH:20][c:21]1[cH:22][cH:23][c:24]([CH2:25][CH2:26][NH:27][C:28](=[O:29])[O:30][C:31]([CH3:32])([CH3:33])[CH3:34])[cH:35][cH:36]1.O=S(=O)(O[CH2:19][P:6]([O:5][CH2:4][CH2:3][CH2:2][CH3:1])(=[O:7])[CH2:8][CH2:9][CH2:10][O:11][CH2:12][c:13]1[cH:14][cH:15][cH:16][cH:17][cH:18]1)c1ccc(Cl)cc1>>[CH3:1][CH2:2][CH2:3][CH2:4][O:...
CC(C)(C)OC(=O)NCCc1ccc(O)cc1.CCCCOP(=O)(CCCOCc1ccccc1)COS(=O)(=O)c1ccc(Cl)cc1
CCCCOP(=O)(CCCOCc1ccccc1)COc1ccc(CCNC(=O)OC(C)(C)C)cc1
null
null
null
Heteroatom Alkylation and Arylation
OtherReaction
4a0fabf60c721d09151620f81fa665b80305ceb254e48798548a02ab5f5e8fbd
950dec716ae7be3d224d7e6483bf59e5d7854c2812a5092d632124a3b7567300
O=[PH](CCCOCc1ccccc1)COc1ccccc1
Cl-c1:c:c:c(-S(=O)(=O)-O-[CH2;D2;+0:1]-[#15:2](-[#8:3])(-[C:4])=[O;D1;H0:5]):c:c:1.[OH;D1;+0:6]-[c:7](:[c:8]):[c:9]>>[#8:3]-[#15:2](-[C:4])(=[O;D1;H0:5])-[CH2;D2;+0:1]-[O;H0;D2;+0:6]-[c:7](:[c:8]):[c:9]
null
[]
null
null
null
null
The title compound was prepared from 3-benzyloxypropyl-(4-chlorobenzenesulfonyloxymethyl)phosphinic acid, n-butyl ester and 2-(4-hydroxyphenyl)ethylcarbamic acid, t-butyl ester according to the procedure described in Procedure 24. The crude product was purified by chromatography, eluting with dichloromethane containing...
10.6084/m9.figshare.5104873.v1
null
Aromatic halide.Aromatic alcohol.Sulfonate
Ether
c1ccccc1
null
c1ccccc1.c1ccccc1
HCl
null
null
null
CC(C)(C)OC(=O)NCCc1ccc(O)cc1.CCCCOP(=O)(CCCOCc1ccccc1)COS(=O)(=O)c1ccc(Cl)cc1>>CCCCOP(=O)(CCCOCc1ccccc1)COc1ccc(CCNC(=O)OC(C)(C)C)cc1
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-dc474815e92e4518a4bce138d4d23348
CCCCOP(=O)(CCCOCc1ccccc1)COS(=O)(=O)c1ccc(Cl)cc1.C[C@H](Cc1ccc(O)cc1)NC(=O)OC(C)(C)C>>CCCCO[P@](=O)(CCCOCc1ccccc1)COc1ccc(CC(C)NC(=O)OC(C)(C)C)cc1
C(C1=CC=CC=C1)OCCCP(OCCCC)(=O)COS(=O)(=O)C1=CC=C(C=C1)Cl.OC1=CC=C(C=C1)C[C@@H](C)NC(OC(C)(C)C)=O>>C(C)(C)(C)OC(=O)NC(CC1=CC=C(OC[P@@](OCCCC)(=O)CCCOCC2=CC=CC=C2)C=C1)C
O=S(=O)(O[CH2:19][P:6]([O:5][CH2:4][CH2:3][CH2:2][CH3:1])(=[O:7])[CH2:8][CH2:9][CH2:10][O:11][CH2:12][c:13]1[cH:14][cH:15][cH:16][cH:17][cH:18]1)c1ccc(Cl)cc1.[OH:20][c:21]1[cH:22][cH:23][c:24]([CH2:25][C@@H:26]([CH3:27])[NH:28][C:29](=[O:30])[O:31][C:32]([CH3:33])([CH3:34])[CH3:35])[cH:36][cH:37]1>>[CH3:1][CH2:2][CH2:3...
CCCCOP(=O)(CCCOCc1ccccc1)COS(=O)(=O)c1ccc(Cl)cc1.C[C@H](Cc1ccc(O)cc1)NC(=O)OC(C)(C)C
CCCCO[P@](=O)(CCCOCc1ccccc1)COc1ccc(CC(C)NC(=O)OC(C)(C)C)cc1
null
null
null
Heteroatom Alkylation and Arylation
OtherReaction
4a0fabf60c721d09151620f81fa665b80305ceb254e48798548a02ab5f5e8fbd
950dec716ae7be3d224d7e6483bf59e5d7854c2812a5092d632124a3b7567300
O=[PH](CCCOCc1ccccc1)COc1ccccc1
Cl-c1:c:c:c(-S(=O)(=O)-O-[CH2;D2;+0:1]-[P;H0;D4;+0:2](=[O;D1;H0:3])(-[#8:4]-[C:5])-[C:6]-[C:7]):c:c:1.[OH;D1;+0:8]-[c:9](:[c:10]):[c:11]>>[C:5]-[#8:4]-[P@;H0;D4;+0:2](=[O;D1;H0:3])(-[C:6]-[C:7])-[CH2;D2;+0:1]-[O;H0;D2;+0:8]-[c:9](:[c:10]):[c:11]
null
[]
null
null
null
null
The title compound was prepared from 3-benzyloxypropyl-(4-chlorobenzenesulfonyloxymethyl)phosphinic acid, n-butyl ester and (R)-2-(4-hydroxyphenyl)-1-methylethylcarbamic acid, t-butyl ester according to the method described in Procedure 24. The crude product was purified by chromatography, eluting with dichloromethane ...
10.6084/m9.figshare.5104873.v1
null
Aromatic halide.Aromatic alcohol.Sulfonate
Ether
c1ccccc1
null
c1ccccc1.c1ccccc1
HCl
null
null
null
CCCCOP(=O)(CCCOCc1ccccc1)COS(=O)(=O)c1ccc(Cl)cc1.C[C@H](Cc1ccc(O)cc1)NC(=O)OC(C)(C)C>>CCCCO[P@](=O)(CCCOCc1ccccc1)COc1ccc(CC(C)NC(=O)OC(C)(C)C)cc1
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-7f531c27f471483498c3ba9ea0b700cd
O=[PH](O)C1CCCCC1>>CCCCO[PH](=O)C1CCCCC1
C1(CCCCC1)P(O)=O>>C1(CCCCC1)P(OCCCC)=O
[CH2:1]1[CH2:9][CH:8]([PH:6]([OH:5])=[O:7])[CH2:13][CH2:12][CH2:11]1>>[CH3:1][CH2:2][CH2:3][CH2:4][O:5][PH:6](=[O:7])[CH:8]1[CH2:9][CH2:10][CH2:11][CH2:12][CH2:13]1
O=[PH](O)C1CCCCC1
CCCCO[PH](=O)C1CCCCC1
null
null
C(CCC)O
Miscellaneous
OtherReaction
497ed6fa2fecc89bd99211bb234d91811e03f385203fb438fe023970267815cc
56ebed4a8b3cebec83c37a71d68f0c87d1e404ab05a9ce792691e4e18a2379dd
C1CCCCC1
[O;D1;H0:1]=[#15:2](-[OH;D1;+0:3])-[C:4]1-[C:5]-[C:6]-[CH2;D2;+0:7]-[CH2;D2;+0:8]-[CH2;D2;+0:9]-1>>[CH3;D1;+0:8]-[C:10]-[C:11]-[C:12]-[O;H0;D2;+0:3]-[#15:2](=[O;D1;H0:1])-[C:4]1-[C:5]-[C:6]-[CH2;D2;+0:7]-[C:13]-[CH2;D2;+0:9]-1
null
[]
null
null
null
null
The title compound was prepared from cyclohexylphosphinic acid and n-butanol according the the method described in Procedure 43. The compound was used without further purification. Conditions: See reaction.notes.procedure_details. Workup: The compound was used without further purification
10.6084/m9.figshare.5104873.v1
null
null
null
C1CCCCC1
C1CCCCC1
C1CCCCC1
Other
C(CCC)O
null
null
O=[PH](O)C1CCCCC1>C(CCC)O>CCCCO[PH](=O)C1CCCCC1
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-8779dd64d7dd4ab6a8cba54d39669391
C=O.CCCCO[PH](=O)C1CCCCC1>>CCCCOP(=O)(CO)C1CCCCC1
C1(CCCCC1)P(OCCCC)=O.C=O>>C1(CCCCC1)P(OCCCC)(=O)CO
[CH2:8]=[O:9].[CH3:1][CH2:2][CH2:3][CH2:4][O:5][PH:6](=[O:7])[CH:10]1[CH2:11][CH2:12][CH2:13][CH2:14][CH2:15]1>>[CH3:1][CH2:2][CH2:3][CH2:4][O:5][P:6](=[O:7])([CH2:8][OH:9])[CH:10]1[CH2:11][CH2:12][CH2:13][CH2:14][CH2:15]1
C=O.CCCCO[PH](=O)C1CCCCC1
CCCCOP(=O)(CO)C1CCCCC1
null
null
null
Miscellaneous
OtherReaction
ff9e019412f5fb147910daaf4ee10ff7abac3966a22d93efa93ff9552cbbbf9e
a07b6e0bbdb5ea0627df192b2885de7d34cb5e55531d8d5102717495a910d9a6
C1CCCCC1
[CH2;D1;+0:1]=[O;H0;D1;+0:2].[C:3]-[C:4](-[PH;D3;+0:5](=[O;D1;H0:6])-[#8:7]-[C:8])-[C:9]>>[C:3]-[C:4](-[P;H0;D4;+0:5](=[O;D1;H0:6])(-[#8:7]-[C:8])-[CH2;D2;+0:1]-[OH;D1;+0:2])-[C:9]
null
[]
null
null
null
null
The title compound was prepared from cyclohexylphosphinic acid, n-butyl ester and paraformaldehyde according to the method described in Procedure 31. Purification by chromatography, eluting with dichloromethane containing 5% methanol, gave an oil. Conditions: See reaction.notes.procedure_details. Workup: Purification b...
10.6084/m9.figshare.5104873.v1
null
Formaldehyde
Primary alcohol
null
null
C1CCCCC1
null
null
null
null
C=O.CCCCO[PH](=O)C1CCCCC1>>CCCCOP(=O)(CO)C1CCCCC1
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-d63aff1397e8480b8c2a33699be1bede
CCCCOP(=O)(COc1ccccc1)C1CCC(CCN)CC1.c1ccc(COc2ccc(OC[C@@H]3CO3)cc2)cc1>>CCCCO[P@](=O)(COc1ccccc1)C1CCC(CCNCC(O)COc2ccc(OCc3ccccc3)cc2)CC1
NCCC1CCC(CC1)P(OCCCC)(=O)COC1=CC=CC=C1.C(C1=CC=CC=C1)OC1=CC=C(OC[C@H]2OC2)C=C1>>C(C1=CC=CC=C1)OC1=CC=C(OCC(CNCCC2CCC(CC2)[P@@](OCCCC)(=O)COC2=CC=CC=C2)O)C=C1
[CH3:1][CH2:2][CH2:3][CH2:4][O:5][P:6](=[O:7])([CH2:8][O:9][c:10]1[cH:11][cH:12][cH:13][cH:14][cH:15]1)[CH:16]1[CH2:17][CH2:18][CH:19]([CH2:20][CH2:21][NH2:22])[CH2:42][CH2:43]1.[CH2:23]1[C@@H:24]([CH2:26][O:27][c:28]2[cH:29][cH:30][c:31]([O:32][CH2:33][c:34]3[cH:35][cH:36][cH:37][cH:38][cH:39]3)[cH:40][cH:41]2)[O:25]1...
CCCCOP(=O)(COc1ccccc1)C1CCC(CCN)CC1.c1ccc(COc2ccc(OC[C@@H]3CO3)cc2)cc1
CCCCO[P@](=O)(COc1ccccc1)C1CCC(CCNCC(O)COc2ccc(OCc3ccccc3)cc2)CC1
null
null
null
Heteroatom Alkylation and Arylation
OtherReaction
f75f8fec78b0ee9c8e880101c8c57c2a3edaac070bc7ad0163a34826e2af8c65
04c78336d85647f6dca3040f384f77009d1b541aac7f8ccf33aa9798091ceab8
O=[PH](COc1ccccc1)C1CCC(CCNCCCOc2ccc(OCc3ccccc3)cc2)CC1
[#8:1]-[C:2]-[C@@H;D3;+0:3]1-[CH2;D2;+0:4]-[O;H0;D2;+0:5]-1.[C:6]-[C:7]-[NH2;D1;+0:8]>>[#8:1]-[C:2]-[CH;D3;+0:3](-[OH;D1;+0:5])-[CH2;D2;+0:4]-[NH;D2;+0:8]-[C:7]-[C:6]
null
[]
null
null
null
null
The title compound was prepared from 4-(2-aminoethyl)phenoxy methylcyclohexylphosphinic acid, n-butyl ester and (S)-2-(4-benzyloxyphenoxymethyl)oxirane according to the method described in Procedure 13. Conditions: See reaction.notes.procedure_details.
10.6084/m9.figshare.5104873.v1
null
Ether.Primary amine
Secondary alcohol.Secondary amine
C1CO1
null
c1ccccc1.C1CCCCC1.c1ccccc1.c1ccccc1
null
null
null
null
CCCCOP(=O)(COc1ccccc1)C1CCC(CCN)CC1.c1ccc(COc2ccc(OC[C@@H]3CO3)cc2)cc1>>CCCCO[P@](=O)(COc1ccccc1)C1CCC(CCNCC(O)COc2ccc(OCc3ccccc3)cc2)CC1
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-7f98044a2f33492ab975abc63fa26522
C=CCCCC.O=[PH2]O>>CCCCCC[PH](=O)O
C=CCCCC.[PH2](O)=O>>C(CCCCC)P(O)=O
[CH3:1][CH2:2][CH2:3][CH2:4][CH:5]=[CH2:6].[PH2:7](=[O:8])[OH:9]>>[CH3:1][CH2:2][CH2:3][CH2:4][CH2:5][CH2:6][PH:7](=[O:8])[OH:9]
C=CCCCC.O=[PH2]O
CCCCCC[PH](=O)O
null
null
null
Miscellaneous
OtherReaction
57a64b6b42d462fe8276aa79a48b5b98ebab75830adad1905b3795c71ea65b06
b53d8f361e43dc967c3023dcafe218466acf623d0cf729a1557a2a80217926eb
null
[C:1]-[C:2]-[CH;D2;+0:3]=[CH2;D1;+0:4].[O;D1;H0:5]=[PH2;D2;+0:6]-[O;D1;H1:7]>>[C:1]-[C:2]-[CH2;D2;+0:3]-[CH2;D2;+0:4]-[PH;D3;+0:6](=[O;D1;H0:5])-[O;D1;H1:7]
null
[]
null
null
null
null
The title compound was prepared from n-hexene and 50% aqueous phosphinic acid by an analogous procedure to that described in J. Inorg. Nucl. Chem., 1965, 27, 697. Conditions: See reaction.notes.procedure_details.
10.6084/m9.figshare.5104873.v1
null
Allyl
null
null
null
null
null
null
null
null
C=CCCCC.O=[PH2]O>>CCCCCC[PH](=O)O
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-f16851ac82164be198238393b2929fcf
CCCCCC[PH](=O)O>>CCCCCC[PH](=O)OCCCC
C(CCCCC)P(O)=O>>C(CCCCC)P(OCCCC)=O
[CH3:1][CH2:2][CH2:3][CH2:4][CH2:5][CH2:6][PH:7](=[O:8])[OH:9]>>[CH3:1][CH2:2][CH2:3][CH2:4][CH2:5][CH2:6][PH:7](=[O:8])[O:9][CH2:10][CH2:11][CH2:12][CH3:13]
CCCCCC[PH](=O)O
CCCCCC[PH](=O)OCCCC
null
null
C(CCC)O
Miscellaneous
OtherReaction
40ba59785861b8226ce5af6bdcbb9a37f0ff50a8c7ec7d4fc4c524cf906cc65c
56ebed4a8b3cebec83c37a71d68f0c87d1e404ab05a9ce792691e4e18a2379dd
null
[C:1]-[#15:2](=[O;D1;H0:3])-[OH;D1;+0:4]>>[C:5]-[C:6]-[O;H0;D2;+0:4]-[#15:2](-[C:1])=[O;D1;H0:3]
null
[]
null
null
null
null
The title compound was prepared from n-hexylphosphinic acid and n-butanol according the the method described in Procedure 43. The compound was used without further purification. Conditions: See reaction.notes.procedure_details. Workup: The compound was used without further purification
10.6084/m9.figshare.5104873.v1
null
null
null
null
null
null
Other
C(CCC)O
null
null
CCCCCC[PH](=O)O>C(CCC)O>CCCCCC[PH](=O)OCCCC
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-8ac817860d9d44d4acd7988671266af2
C=O.CCCCCC[PH](=O)OCCCC>>CCCCCCP(=O)(CO)OCCCC
C(CCCCC)P(OCCCC)=O.C=O>>C(CCCCC)P(OCCCC)(=O)CO
[CH2:9]=[O:10].[CH3:1][CH2:2][CH2:3][CH2:4][CH2:5][CH2:6][PH:7](=[O:8])[O:11][CH2:12][CH2:13][CH2:14][CH3:15]>>[CH3:1][CH2:2][CH2:3][CH2:4][CH2:5][CH2:6][P:7](=[O:8])([CH2:9][OH:10])[O:11][CH2:12][CH2:13][CH2:14][CH3:15]
C=O.CCCCCC[PH](=O)OCCCC
CCCCCCP(=O)(CO)OCCCC
null
null
null
Miscellaneous
OtherReaction
ff9e019412f5fb147910daaf4ee10ff7abac3966a22d93efa93ff9552cbbbf9e
a07b6e0bbdb5ea0627df192b2885de7d34cb5e55531d8d5102717495a910d9a6
null
[CH2;D1;+0:1]=[O;H0;D1;+0:2].[C:3]-[#8:4]-[PH;D3;+0:5](=[O;D1;H0:6])-[C:7]-[C:8]>>[C:3]-[#8:4]-[P;H0;D4;+0:5](=[O;D1;H0:6])(-[C:7]-[C:8])-[CH2;D2;+0:1]-[OH;D1;+0:2]
null
[]
null
null
null
null
The title compound was prepared from n-hexylphosphinic acid, n-butyl ester and paraformaldehyde according to the method described in Procedure 31. Purification by chromatography, eluting with dichloromethane containing 5% methanol, gave an oil. Conditions: See reaction.notes.procedure_details. Workup: Purification by c...
10.6084/m9.figshare.5104873.v1
null
Formaldehyde
Primary alcohol
null
null
null
null
null
null
null
C=O.CCCCCC[PH](=O)OCCCC>>CCCCCCP(=O)(CO)OCCCC
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-21a512275c5740b8a6d9a02b334da1ec
NCCc1ccc(O)cc1.c1ccc(COc2ccc(OC[C@@H]3CO3)cc2)cc1>>Oc1ccc(CCNC[C@H](O)COc2ccc(OCc3ccccc3)cc2)cc1
NCCC1=CC=C(C=C1)O.C(C1=CC=CC=C1)OC1=CC=C(OC[C@H]2OC2)C=C1>>C(C1=CC=CC=C1)OC1=CC=C(OC[C@H](CNCCC2=CC=C(C=C2)O)O)C=C1
[OH:1][c:2]1[cH:3][cH:4][c:5]([CH2:6][CH2:7][NH2:8])[cH:28][cH:29]1.[CH2:9]1[C@@H:10]([CH2:12][O:13][c:14]2[cH:15][cH:16][c:17]([O:18][CH2:19][c:20]3[cH:21][cH:22][cH:23][cH:24][cH:25]3)[cH:26][cH:27]2)[O:11]1>>[OH:1][c:2]1[cH:3][cH:4][c:5]([CH2:6][CH2:7][NH:8][CH2:9][C@H:10]([OH:11])[CH2:12][O:13][c:14]2[cH:15][cH:16]...
NCCc1ccc(O)cc1.c1ccc(COc2ccc(OC[C@@H]3CO3)cc2)cc1
Oc1ccc(CCNC[C@H](O)COc2ccc(OCc3ccccc3)cc2)cc1
null
null
null
Heteroatom Alkylation and Arylation
OtherReaction
f75f8fec78b0ee9c8e880101c8c57c2a3edaac070bc7ad0163a34826e2af8c65
04c78336d85647f6dca3040f384f77009d1b541aac7f8ccf33aa9798091ceab8
c1ccc(CCNCCCOc2ccc(OCc3ccccc3)cc2)cc1
[#8:1]-[C:2]-[C@@H;D3;+0:3]1-[CH2;D2;+0:4]-[O;H0;D2;+0:5]-1.[C:6]-[C:7]-[NH2;D1;+0:8]>>[#8:1]-[C:2]-[C@@H;D3;+0:3](-[OH;D1;+0:5])-[CH2;D2;+0:4]-[NH;D2;+0:8]-[C:7]-[C:6]
null
[]
null
null
null
null
The title compound was prepared from tyramine and (S)-2-(4-benzyloxyphenoxymethyl)oxirane according to the method described in Procedure 13. Conditions: See reaction.notes.procedure_details.
10.6084/m9.figshare.5104873.v1
null
Ether.Primary amine
Secondary alcohol.Secondary amine
C1CO1
null
c1ccccc1.c1ccccc1.c1ccccc1
null
null
null
null
NCCc1ccc(O)cc1.c1ccc(COc2ccc(OC[C@@H]3CO3)cc2)cc1>>Oc1ccc(CCNC[C@H](O)COc2ccc(OCc3ccccc3)cc2)cc1
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-c88884b2244548bda021d31a20f133fd
BrCc1ccccc1.Oc1ccc(CCNC[C@H](O)COc2ccc(OCc3ccccc3)cc2)cc1>>Oc1ccc(CCN(Cc2ccccc2)C[C@H](O)COc2ccc(OCc3ccccc3)cc2)cc1
C(C1=CC=CC=C1)OC1=CC=C(OC[C@H](CNCCC2=CC=C(C=C2)O)O)C=C1.C(C1=CC=CC=C1)Br.C([O-])([O-])=O.[Na+].[Na+]>>C(C1=CC=CC=C1)N(CCC1=CC=C(C=C1)O)C[C@@H](COC1=CC=C(C=C1)OCC1=CC=CC=C1)O
Br[CH2:9][c:10]1[cH:11][cH:12][cH:13][cH:14][cH:15]1.[OH:1][c:2]1[cH:3][cH:4][c:5]([CH2:6][CH2:7][NH:8][CH2:16][C@H:17]([OH:18])[CH2:19][O:20][c:21]2[cH:22][cH:23][c:24]([O:25][CH2:26][c:27]3[cH:28][cH:29][cH:30][cH:31][cH:32]3)[cH:33][cH:34]2)[cH:35][cH:36]1>>[OH:1][c:2]1[cH:3][cH:4][c:5]([CH2:6][CH2:7][N:8]([CH2:9][c...
BrCc1ccccc1.Oc1ccc(CCNC[C@H](O)COc2ccc(OCc3ccccc3)cc2)cc1
Oc1ccc(CCN(Cc2ccccc2)C[C@H](O)COc2ccc(OCc3ccccc3)cc2)cc1
null
null
CN(C=O)C
Heteroatom Alkylation and Arylation
N-alkylation of secondary amines with alkyl halides
6d58cac08ccced0a33ed16fbca180bc12aa011288d6476106d98a7b2cbc3d709
523d37155b42c8dc851abeddadebb241cdd90bdf649ba750c35e13c8c752d7b0
c1ccc(CCN(CCCOc2ccc(OCc3ccccc3)cc2)Cc2ccccc2)cc1
Br-[CH2;D2;+0:1]-[c:2](:[c:3]):[c:4].[C:5]-[C:6]-[NH;D2;+0:7]-[C:8]-[C:9]>>[C:5]-[C:6]-[N;H0;D3;+0:7](-[C:8]-[C:9])-[CH2;D2;+0:1]-[c:2](:[c:3]):[c:4]
null
[]
null
null
18
HOUR
A solution of (S)-1-(4-benzyloxyphenoxy)-3-[N-2-(4-hydroxyphenyl)ethylamino]propan-2-ol (1.9 g, 4.8 mMol) and benzyl bromide (0.57 ml, 4.8 mMol) in dimethylformamide (10 ml) containing sodium carbonate (770 mg, 7.2 mMol) was stirred at room temperature for 18 hours. The mixture was filtered and the residue was washed w...
10.6084/m9.figshare.5104873.v1
null
Primary halide.Secondary amine
Tertiary amine
null
null
c1ccccc1.c1ccccc1.c1ccccc1.c1ccccc1
HBr
CN(C=O)C
null
18
BrCc1ccccc1.Oc1ccc(CCNC[C@H](O)COc2ccc(OCc3ccccc3)cc2)cc1>CN(C=O)C>Oc1ccc(CCN(Cc2ccccc2)C[C@H](O)COc2ccc(OCc3ccccc3)cc2)cc1
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-fbb7b4f2d98e40cc842d6d8dc54f1727
C[Si](C)(C)N[Si](C)(C)C.ClCc1ccccc1.O=[PH2][O-]>>CCCCO[PH](=O)Cc1ccccc1
[PH2]([O-])=O.[NH4+].C[Si](N[Si](C)(C)C)(C)C.C(C1=CC=CC=C1)Cl>>C(C1=CC=CC=C1)P(OCCCC)=O
C[Si](N[Si](C)([CH3:1])[CH3:4])([CH3:2])[CH3:3].Cl[CH2:8][c:9]1[cH:10][cH:11][cH:12][cH:13][cH:14]1.[O-:5][PH2:6]=[O:7]>>[CH3:1][CH2:2][CH2:3][CH2:4][O:5][PH:6](=[O:7])[CH2:8][c:9]1[cH:10][cH:11][cH:12][cH:13][cH:14]1
C[Si](C)(C)N[Si](C)(C)C.ClCc1ccccc1.O=[PH2][O-]
CCCCO[PH](=O)Cc1ccccc1
null
null
ClCCl
Heteroatom Alkylation and Arylation
OtherReaction
896e526c4cf7b73f9e61941ba9abeea264ce8bddded81bccc6872aa9369bde62
21c2d6ad627e0d89816de17f4010107ca25a77225bb725f813a79c7150b158e4
c1ccccc1
C-[Si](-[CH3;D1;+0:1])(-[CH3;D1;+0:2])-N-[Si](-C)(-[CH3;D1;+0:3])-[CH3;D1;+0:4].Cl-[CH2;D2;+0:5]-[c:6](:[c:7]):[c:8].[O-;H0;D1:9]-[PH2;D2;+0:10]=[O;D1;H0:11]>>[CH3;D1;+0:3]-[CH2;D2;+0:1]-[CH2;D2;+0:2]-[CH2;D2;+0:4]-[O;H0;D2;+0:9]-[PH;D3;+0:10](=[O;D1;H0:11])-[CH2;D2;+0:5]-[c:6](:[c:7]):[c:8]
null
[]
110
CELSIUS
18
HOUR
A mixture of ammonium phosphinate (9.18 g) and hexamethyldisilazane (25 mL) was heated at 110° C. for 2 hours. The mixture was cooled in ice, dissolved in dry dichloromethane (120 mL), benzyl chloride (20 g; 14 mL) was added and the mixture allowed to warm to room temperature and stirred 18 hours. The solution was filt...
10.6084/m9.figshare.5104873.v1
null
Primary halide.Secondary amine.Silyl protective group.Silyl protective group
null
null
null
c1ccccc1
HCl
ClCCl
110
18
C[Si](C)(C)N[Si](C)(C)C.ClCc1ccccc1.O=[PH2][O-]>ClCCl>CCCCO[PH](=O)Cc1ccccc1
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-b4965ae0e45f4361b45b7c919bb59755
C=O.CCCCO[PH](=O)Cc1ccccc1>>CCCCOP(=O)(CO)Cc1ccccc1
C(C1=CC=CC=C1)P(OCCCC)=O.C=O>>C(C1=CC=CC=C1)P(OCCCC)(=O)CO
[CH2:8]=[O:9].[CH3:1][CH2:2][CH2:3][CH2:4][O:5][PH:6](=[O:7])[CH2:10][c:11]1[cH:12][cH:13][cH:14][cH:15][cH:16]1>>[CH3:1][CH2:2][CH2:3][CH2:4][O:5][P:6](=[O:7])([CH2:8][OH:9])[CH2:10][c:11]1[cH:12][cH:13][cH:14][cH:15][cH:16]1
C=O.CCCCO[PH](=O)Cc1ccccc1
CCCCOP(=O)(CO)Cc1ccccc1
null
null
null
Miscellaneous
OtherReaction
ff9e019412f5fb147910daaf4ee10ff7abac3966a22d93efa93ff9552cbbbf9e
a07b6e0bbdb5ea0627df192b2885de7d34cb5e55531d8d5102717495a910d9a6
c1ccccc1
[CH2;D1;+0:1]=[O;H0;D1;+0:2].[C:3]-[#8:4]-[PH;D3;+0:5](=[O;D1;H0:6])-[C:7]-[c:8]>>[C:3]-[#8:4]-[P;H0;D4;+0:5](=[O;D1;H0:6])(-[C:7]-[c:8])-[CH2;D2;+0:1]-[OH;D1;+0:2]
null
[]
null
null
null
null
The title compound was prepared from benzylphosphinic acid, n-butyl ester and paraformaldehyde according to the method described in Procedure 31. Conditions: See reaction.notes.procedure_details.
10.6084/m9.figshare.5104873.v1
null
Formaldehyde
Primary alcohol
null
null
c1ccccc1
null
null
null
null
C=O.CCCCO[PH](=O)Cc1ccccc1>>CCCCOP(=O)(CO)Cc1ccccc1
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-1b2ca7107578479d93f1b4ae6d8fd313
CCCCOP(=O)(CO)Cc1ccccc1.O=S(=O)(Cl)c1ccc(Cl)cc1>>CCCCOP(=O)(COS(=O)(=O)c1ccc(Cl)cc1)Cc1ccccc1
C(C1=CC=CC=C1)P(OCCCC)(=O)CO.ClC1=CC=C(C=C1)S(=O)(=O)Cl>>C(C1=CC=CC=C1)P(OCCCC)(=O)COS(=O)(=O)C1=CC=C(C=C1)Cl
[CH3:1][CH2:2][CH2:3][CH2:4][O:5][P:6](=[O:7])([CH2:8][OH:9])[CH2:20][c:21]1[cH:22][cH:23][cH:24][cH:25][cH:26]1.Cl[S:10](=[O:11])(=[O:12])[c:13]1[cH:14][cH:15][c:16]([Cl:17])[cH:18][cH:19]1>>[CH3:1][CH2:2][CH2:3][CH2:4][O:5][P:6](=[O:7])([CH2:8][O:9][S:10](=[O:11])(=[O:12])[c:13]1[cH:14][cH:15][c:16]([Cl:17])[cH:18][c...
CCCCOP(=O)(CO)Cc1ccccc1.O=S(=O)(Cl)c1ccc(Cl)cc1
CCCCOP(=O)(COS(=O)(=O)c1ccc(Cl)cc1)Cc1ccccc1
null
null
null
Acylation
Formation of Sulfonic Esters
76a2f1ce13fb019af608455a0d79fe83b29c455d623b278b739d67e5b567ea89
e7708aa65b3d8696add9aec26cae169160bb027d6d2772db2030dd9c0b07b540
O=[PH](COS(=O)(=O)c1ccccc1)Cc1ccccc1
Cl-[S;H0;D4;+0:1](=[O;D1;H0:2])(=[O;D1;H0:3])-[c:4](:[c:5]):[c:6].[#15:7]-[C:8]-[OH;D1;+0:9]>>[#15:7]-[C:8]-[O;H0;D2;+0:9]-[S;H0;D4;+0:1](=[O;D1;H0:2])(=[O;D1;H0:3])-[c:4](:[c:5]):[c:6]
null
[]
null
null
null
null
The title compound was prepared from benzylhydroxymethylphosphinic acid, n-butyl ester and 4-chlorobenzenesulfonyl chloride according to the method described in Procedure 32. The resulting white solid (mp 87°-88° C.) was used in the next stage without further purification. Conditions: See reaction.notes.procedure_detai...
10.6084/m9.figshare.5104873.v1
null
Primary alcohol.Sulfonyl halide
Sulfonate
null
null
c1ccccc1.c1ccccc1
HCl
null
null
null
CCCCOP(=O)(CO)Cc1ccccc1.O=S(=O)(Cl)c1ccc(Cl)cc1>>CCCCOP(=O)(COS(=O)(=O)c1ccc(Cl)cc1)Cc1ccccc1
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-bcd59e6d31334fa7a06760faa96f245d
COC(=O)COc1ccc(CC(C)NCC(O)COc2ccc(O)c(O)c2)cc1>>CC(Cc1ccc(OCC(=O)O)cc1)NCC(O)COc1ccc(O)c(O)c1
Cl.OC(CNC(CC1=CC=C(OCC(=O)OC)C=C1)C)COC1=CC(=C(C=C1)O)O.Cl>>Cl.OC=1C=C(OCC(CNC(CC2=CC=C(OCC(=O)O)C=C2)C)O)C=CC1O
C[O:12][C:10]([CH2:9][O:8][c:7]1[cH:6][cH:5][c:4]([CH2:3][CH:2]([CH3:1])[NH:15][CH2:16][CH:17]([OH:18])[CH2:19][O:20][c:21]2[cH:22][cH:23][c:24]([OH:25])[c:26]([OH:27])[cH:28]2)[cH:14][cH:13]1)=[O:11]>>[CH3:1][CH:2]([CH2:3][c:4]1[cH:5][cH:6][c:7]([O:8][CH2:9][C:10](=[O:11])[OH:12])[cH:13][cH:14]1)[NH:15][CH2:16][CH:17]...
COC(=O)COc1ccc(CC(C)NCC(O)COc2ccc(O)c(O)c2)cc1
CC(Cc1ccc(OCC(=O)O)cc1)NCC(O)COc1ccc(O)c(O)c1
null
null
O
Deprotection
Ester saponification (methyl deprotection)
d872e08ad5c85a4add6cd04e6e987e73fead5f79b3f30ba61a81ba5029b29894
38ae1ee78433b9acfb0390501446149c80f88f23ac2d84c60b3369bdab75cec9
c1ccc(CCNCCCOc2ccccc2)cc1
C-[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
[]
100
CELSIUS
null
null
A solution of (SR)-4-{2-[2-hydroxy-3-(3,4-dihydroxyphenoxy)propylamino]propyl}phenoxyacetic acid, methyl ester, hydrochloride (78 mg, 0.17 mMol) in water (2 ml) containing hydrochloric acid (1M, 0.5 ml, 0.51 mMol) was heated at 100° C. under argon for 3 hours. After cooling to room temperature the solution was freeze d...
10.6084/m9.figshare.5104873.v1
null
Ester
Carboxylic acid
null
null
c1ccccc1.c1ccccc1
Other
O
100
null
COC(=O)COc1ccc(CC(C)NCC(O)COc2ccc(O)c(O)c2)cc1>O>CC(Cc1ccc(OCC(=O)O)cc1)NCC(O)COc1ccc(O)c(O)c1
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-8e4211f4f8714a32ba4f81b5ab11c25a
CCCCO[P@@](=O)(CCCOCc1ccccc1)COc1ccc(CCNCC(O)COc2ccc(O)c(CO)c2)cc1>>O=P(O)(CCCOCc1ccccc1)COc1ccc(CCNC[C@H](O)COc2ccc(O)c(CO)c2)cc1
OC(CNCCC1=CC=C(OC[P@](OCCCC)(=O)CCCOCC2=CC=CC=C2)C=C1)COC1=CC(=C(C=C1)O)CO.Cl>>O[C@@H](CNCCC1=CC=C(OCP(O)(=O)CCCOCC2=CC=CC=C2)C=C1)COC1=CC(=C(C=C1)O)CO
CCCC[O:3][P@@:2](=[O:1])([CH2:4][CH2:5][CH2:6][O:7][CH2:8][c:9]1[cH:10][cH:11][cH:12][cH:13][cH:14]1)[CH2:15][O:16][c:17]1[cH:18][cH:19][c:20]([CH2:21][CH2:22][NH:23][CH2:24][CH:25]([OH:26])[CH2:27][O:28][c:29]2[cH:30][cH:31][c:32]([OH:33])[c:34]([CH2:35][OH:36])[cH:37]2)[cH:38][cH:39]1>>[O:1]=[P:2]([OH:3])([CH2:4][CH2...
CCCCO[P@@](=O)(CCCOCc1ccccc1)COc1ccc(CCNCC(O)COc2ccc(O)c(CO)c2)cc1
O=P(O)(CCCOCc1ccccc1)COc1ccc(CCNC[C@H](O)COc2ccc(O)c(CO)c2)cc1
null
null
null
Deprotection
OtherReaction
eaaf8436ac19e7e26db9ff78e61eed5caf13b9167196c3230a9e1eb66b295f8b
30a26bc929988d0041b9998cdccd1d65eb125114a78065ed35d40f50c965c0a7
O=[PH](CCCOCc1ccccc1)COc1ccc(CCNCCCOc2ccccc2)cc1
C-C-C-C-[O;H0;D2;+0:1]-[P@;H0;D4;+0:2](=[O;D1;H0:3])(-[C:4]-[#8:5])-[C:6]-[C:7]>>[#8:5]-[C:4]-[P;H0;D4;+0:2](=[O;D1;H0:3])(-[OH;D1;+0:1])-[C:6]-[C:7]
null
[]
null
null
null
null
The title compound was prepared from (S)-4-{2-[2-hydroxy-3-(4-hydroxy-3-hydroxymethyl-phenoxy)propylamino]ethyl}phenoxymethyl-(3-benzyloxypropyl)phosphinic acid, n-butyl ester according to a modification of the procedure described in Example 5. Acidification to pH 3.5 with 1M hydrochloric acid followed by C18 reverse p...
10.6084/m9.figshare.5104873.v1
null
null
null
null
null
c1ccccc1.c1ccccc1.c1ccccc1
Other
null
null
null
CCCCO[P@@](=O)(CCCOCc1ccccc1)COc1ccc(CCNCC(O)COc2ccc(O)c(CO)c2)cc1>>O=P(O)(CCCOCc1ccccc1)COc1ccc(CCNC[C@H](O)COc2ccc(O)c(CO)c2)cc1
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-53f0eba6f5424c5d8afd83daf49ced93
CCCCOP(=O)(CCCOCc1ccccc1)COc1ccc(CC(C)NCC(O)COc2ccc(O)c(CO)c2)cc1>>CC(Cc1ccc(OCP(=O)(O)CCCOCc2ccccc2)cc1)NCC(O)COc1ccc(O)c(CO)c1
OC(CNC(CC1=CC=C(OCP(OCCCC)(=O)CCCOCC2=CC=CC=C2)C=C1)C)COC1=CC(=C(C=C1)O)CO.Cl>>Cl.OC(CNC(CC1=CC=C(OCP(O)(=O)CCCOCC2=CC=CC=C2)C=C1)C)COC1=CC(=C(C=C1)O)CO
CCCC[O:12][P:10]([CH2:9][O:8][c:7]1[cH:6][cH:5][c:4]([CH2:3][CH:2]([CH3:1])[NH:26][CH2:27][CH:28]([OH:29])[CH2:30][O:31][c:32]2[cH:33][cH:34][c:35]([OH:36])[c:37]([CH2:38][OH:39])[cH:40]2)[cH:25][cH:24]1)(=[O:11])[CH2:13][CH2:14][CH2:15][O:16][CH2:17][c:18]1[cH:19][cH:20][cH:21][cH:22][cH:23]1>>[CH3:1][CH:2]([CH2:3][c:...
CCCCOP(=O)(CCCOCc1ccccc1)COc1ccc(CC(C)NCC(O)COc2ccc(O)c(CO)c2)cc1
CC(Cc1ccc(OCP(=O)(O)CCCOCc2ccccc2)cc1)NCC(O)COc1ccc(O)c(CO)c1
null
null
null
Deprotection
OtherReaction
eaaf8436ac19e7e26db9ff78e61eed5caf13b9167196c3230a9e1eb66b295f8b
30a26bc929988d0041b9998cdccd1d65eb125114a78065ed35d40f50c965c0a7
O=[PH](CCCOCc1ccccc1)COc1ccc(CCNCCCOc2ccccc2)cc1
C-C-C-C-[O;H0;D2;+0:1]-[#15:2](-[C:3])(-[C:4])=[O;D1;H0:5]>>[C:3]-[#15:2](-[C:4])(=[O;D1;H0:5])-[OH;D1;+0:1]
null
[]
null
null
null
null
The title compound was prepared from (SR)-4-{2-[2-hydroxy-3-(4-hydroxy-3-hydroxymethylphenoxy)propylamino]propyl}phenoxymethyl(3-benzyloxypropyl)phosphinic acid, n-butyl ester according to a modification of the procedure described in Example 5. Acidification to pH 3.5 with 1M hydrochloric acid followed by C18 reverse p...
10.6084/m9.figshare.5104873.v1
null
null
null
null
null
c1ccccc1.c1ccccc1.c1ccccc1
Other
null
null
null
CCCCOP(=O)(CCCOCc1ccccc1)COc1ccc(CC(C)NCC(O)COc2ccc(O)c(CO)c2)cc1>>CC(Cc1ccc(OCP(=O)(O)CCCOCc2ccccc2)cc1)NCC(O)COc1ccc(O)c(CO)c1
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-722dbda67fac4d1c8121beafd45c9dbf
CCCCO[P@](=O)(COc1ccccc1)C1CCC(CCNCC(O)COc2ccc(OCc3ccccc3)cc2)CC1>>CCCCO[P@](=O)(COc1ccccc1)C1CCC(CCNCC(O)COc2ccc(O)cc2)CC1
OC(CNCCC1CCC(CC1)[P@@](OCCCC)(=O)COC1=CC=CC=C1)COC1=CC=C(C=C1)OCC1=CC=CC=C1>>OC(CNCCC1CCC(CC1)[P@@](OCCCC)(=O)COC1=CC=CC=C1)COC1=CC=C(C=C1)O
c1ccc(C[O:32][c:31]2[cH:30][cH:29][c:28]([O:27][CH2:26][CH:24]([CH2:23][NH:22][CH2:21][CH2:20][CH:19]3[CH2:18][CH2:17][CH:16]([P@@:6]([O:5][CH2:4][CH2:3][CH2:2][CH3:1])(=[O:7])[CH2:8][O:9][c:10]4[cH:11][cH:12][cH:13][cH:14][cH:15]4)[CH2:36][CH2:35]3)[OH:25])[cH:34][cH:33]2)cc1>>[CH3:1][CH2:2][CH2:3][CH2:4][O:5][P@:6](=...
CCCCO[P@](=O)(COc1ccccc1)C1CCC(CCNCC(O)COc2ccc(OCc3ccccc3)cc2)CC1
CCCCO[P@](=O)(COc1ccccc1)C1CCC(CCNCC(O)COc2ccc(O)cc2)CC1
null
[Pd]
CO
Deprotection
Hydroxyl benzyl deprotection
36869d1fe85185a14d9eb30bf05178c600a9b6eca277ffaf3803578c30e0bf5d
26a36596df80ec137b0e8087297418351c93c32819177f680675220622f215d4
O=[PH](COc1ccccc1)C1CCC(CCNCCCOc2ccccc2)CC1
[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]
null
[]
null
null
24
HOUR
A solution of (S)-4-{2-[2-hydroxy-3-(4-benzyloxyphenoxy)propylamino]ethyl}phenoxymethylcyclohexylphosphinic acid, n-butyl ester (1.00 g, 1.64 mMol) in methanol (100 ml) containing 10% palladium on charcoal (50 mg) was hydrogenated at 40° C. and 40 p.s.i. for 24 hours. After cooling to room temperature the suspension wa...
10.6084/m9.figshare.5104873.v1
null
Ether
Aromatic alcohol
c1ccccc1
null
c1ccccc1.C1CCCCC1.c1ccccc1
Other
[Pd].CO
null
24
CCCCO[P@](=O)(COc1ccccc1)C1CCC(CCNCC(O)COc2ccc(OCc3ccccc3)cc2)CC1>[Pd].CO>CCCCO[P@](=O)(COc1ccccc1)C1CCC(CCNCC(O)COc2ccc(O)cc2)CC1
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-f306d8cee34644e195747dc14d730ec8
CCCCO[P@@](=O)(CCCC(CC)CCNCC(O)COc1ccc(O)cc1)COc1ccccc1>>CC[C@@H](CCCP(=O)(O)COc1ccccc1)CCNCC(O)COc1ccc(O)cc1
OC(CNCCC(CCC[P@@](OCCCC)(=O)COC1=CC=CC=C1)CC)COC1=CC=C(C=C1)O.Cl>>OC(CNCC[C@H](CCCP(O)(=O)COC1=CC=CC=C1)CC)COC1=CC=C(C=C1)O
CCCC[O:9][P@:7]([CH2:6][CH2:5][CH2:4][CH:3]([CH2:2][CH3:1])[CH2:18][CH2:19][NH:20][CH2:21][CH:22]([OH:23])[CH2:24][O:25][c:26]1[cH:27][cH:28][c:29]([OH:30])[cH:31][cH:32]1)(=[O:8])[CH2:10][O:11][c:12]1[cH:13][cH:14][cH:15][cH:16][cH:17]1>>[CH3:1][CH2:2][C@@H:3]([CH2:4][CH2:5][CH2:6][P:7](=[O:8])([OH:9])[CH2:10][O:11][c...
CCCCO[P@@](=O)(CCCC(CC)CCNCC(O)COc1ccc(O)cc1)COc1ccccc1
CC[C@@H](CCCP(=O)(O)COc1ccccc1)CCNCC(O)COc1ccc(O)cc1
null
null
null
Deprotection
OtherReaction
eaaf8436ac19e7e26db9ff78e61eed5caf13b9167196c3230a9e1eb66b295f8b
30a26bc929988d0041b9998cdccd1d65eb125114a78065ed35d40f50c965c0a7
O=[PH](CCCCCCNCCCOc1ccccc1)COc1ccccc1
C-C-C-C-[O;H0;D2;+0:1]-[P@;H0;D4;+0:2](=[O;D1;H0:3])(-[C:4]-[#8:5])-[C:6]-[C:7]>>[#8:5]-[C:4]-[P;H0;D4;+0:2](=[O;D1;H0:3])(-[OH;D1;+0:1])-[C:6]-[C:7]
null
[]
null
null
null
null
The title compound was prepared from (S)-4-{2-[2-hydroxy-3-(4-hydroxyphenoxy)propylamino]ethyl}phenoxymethyl-n-hexyl phosphinic acid, n-butyl ester according a modification of the procedure described in Example 25. Acidification to pH 6 with 1M hydrochloric acid followed by C18 reverse phase chromatography and freeze d...
10.6084/m9.figshare.5104873.v1
null
null
null
null
null
c1ccccc1.c1ccccc1
Other
null
null
null
CCCCO[P@@](=O)(CCCC(CC)CCNCC(O)COc1ccc(O)cc1)COc1ccccc1>>CC[C@@H](CCCP(=O)(O)COc1ccccc1)CCNCC(O)COc1ccc(O)cc1
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-7dcfc77b6fae44dabea5f16d26269c62
CCCCOP(=O)(COc1ccccc1)Cc1ccc(CC(C)NCC(O)COc2ccc(O)c(CO)c2)cc1>>CC(Cc1ccc(CP(=O)(O)COc2ccccc2)cc1)NCC(O)COc1ccc(O)c(CO)c1
Cl.OC(CNC(CC1=CC=C(CP(OCCCC)(=O)COC2=CC=CC=C2)C=C1)C)COC1=CC(=C(C=C1)O)CO>>OC(CNC(CC1=CC=C(CP(O)(=O)COC2=CC=CC=C2)C=C1)C)COC1=CC(=C(C=C1)O)CO
CCCC[O:11][P:9]([CH2:8][c:7]1[cH:6][cH:5][c:4]([CH2:3][CH:2]([CH3:1])[NH:22][CH2:23][CH:24]([OH:25])[CH2:26][O:27][c:28]2[cH:29][cH:30][c:31]([OH:32])[c:33]([CH2:34][OH:35])[cH:36]2)[cH:21][cH:20]1)(=[O:10])[CH2:12][O:13][c:14]1[cH:15][cH:16][cH:17][cH:18][cH:19]1>>[CH3:1][CH:2]([CH2:3][c:4]1[cH:5][cH:6][c:7]([CH2:8][P...
CCCCOP(=O)(COc1ccccc1)Cc1ccc(CC(C)NCC(O)COc2ccc(O)c(CO)c2)cc1
CC(Cc1ccc(CP(=O)(O)COc2ccccc2)cc1)NCC(O)COc1ccc(O)c(CO)c1
null
null
null
Deprotection
OtherReaction
eaaf8436ac19e7e26db9ff78e61eed5caf13b9167196c3230a9e1eb66b295f8b
30a26bc929988d0041b9998cdccd1d65eb125114a78065ed35d40f50c965c0a7
O=[PH](COc1ccccc1)Cc1ccc(CCNCCCOc2ccccc2)cc1
C-C-C-C-[O;H0;D2;+0:1]-[#15:2](-[C:3])(-[C:4])=[O;D1;H0:5]>>[C:3]-[#15:2](-[C:4])(=[O;D1;H0:5])-[OH;D1;+0:1]
null
[]
null
null
null
null
The title compound was prepared from (SR)-4-{2-[2-hydroxy-3-(4-hydroxy-3-hydroxymethyl-phenoxy)propylamino]propyl}phenoxymethylbenzylphosphinic acid, n-butyl ester according to the method described in Example 5 followed by acidification to pH 3.5 with 1M hydrochloric acid, as a solid (mp 180°-183° C.) following chromat...
10.6084/m9.figshare.5104873.v1
null
null
null
null
null
c1ccccc1.c1ccccc1.c1ccccc1
Other
null
null
null
CCCCOP(=O)(COc1ccccc1)Cc1ccc(CC(C)NCC(O)COc2ccc(O)c(CO)c2)cc1>>CC(Cc1ccc(CP(=O)(O)COc2ccccc2)cc1)NCC(O)COc1ccc(O)c(CO)c1
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-32e98db4036848ce8b8264c0ec0c3131
CCC(CC)OP(=O)(O)O.CCOC(C)=O.Cc1cn(COCOC(=O)c2ccccc2)c(=O)[nH]c1=O>>CCOP(=O)(COCOCn1cc(C)c(=O)[nH]c1=O)OCC
C(C)(=O)OCC.C(C1=CC=CC=C1)(=O)OCOCN1C(=O)NC(=O)C(C)=C1.C(C)C(OP(=O)(O)O)CC.FC(S(=O)(=O)O[Si](C)(C)C)(F)F>>C(C)OP(=O)(OCC)COCOCN1C(=O)NC(=O)C(C)=C1
CCC(O[P:4](O)(=[O:5])[OH:20])[CH2:21][CH3:22].CC(=O)[O:3][CH2:2][CH3:1].O=[C:6](c1ccccc1)[O:7][CH2:8][O:9][CH2:10][n:11]1[cH:12][c:13]([CH3:14])[c:15](=[O:16])[nH:17][c:18]1=[O:19]>>[CH3:1][CH2:2][O:3][P:4](=[O:5])([CH2:6][O:7][CH2:8][O:9][CH2:10][n:11]1[cH:12][c:13]([CH3:14])[c:15](=[O:16])[nH:17][c:18]1=[O:19])[O:20]...
CCC(CC)OP(=O)(O)O.CCOC(C)=O.Cc1cn(COCOC(=O)c2ccccc2)c(=O)[nH]c1=O
CCOP(=O)(COCOCn1cc(C)c(=O)[nH]c1=O)OCC
null
null
C1=CC=CC=C1
Heteroatom Alkylation and Arylation
OtherReaction
0011ab4c5e0e8d6ec22b1403e9fa2cfd5f1c5f5ed345a8324698dd0f9a332eea
5a67587bdd06f11f80d02c1bbacae855575e59f72bbbfb0c1648772d5a52e271
O=c1cc[nH]c(=O)[nH]1
C-C(=O)-[O;H0;D2;+0:1]-[C:2]-[C;D1;H3:3].C-C-C(-O-[P;H0;D4;+0:4](-O)(=[O;D1;H0:5])-[OH;D1;+0:6])-[CH2;D2;+0:7]-[C;D1;H3:8].O=[C;H0;D3;+0:9](-[#8:10]-[C:11])-c1:c:c:c:c:c:1>>[C:11]-[#8:10]-[CH2;D2;+0:9]-[P;H0;D4;+0:4](=[O;D1;H0:5])(-[O;H0;D2;+0:6]-[CH2;D2;+0:7]-[C;D1;H3:8])-[O;H0;D2;+0:1]-[C:2]-[C;D1;H3:3]
null
[]
85
CELSIUS
null
null
To a solution of 1-[(benzoyloxy)methoxymethyl]thymine (2.9 g, 10 mmol) and diethyl phosphonomethanol (1.85 g, 11 mmol) in benzene (180 mL) was added trimethylsilyl trifluoromethanesulfonate (0.05 mL) via a syringe under nitrogen. The solution was heated at 85° C. for 20 min. After cooling to room temperature, ethyl ace...
10.6084/m9.figshare.5104873.v1
null
Ester.Ester.Phosphate ester
Ether
c1ccccc1
null
c1cncnc1
HO-
C1=CC=CC=C1
85
null
CCC(CC)OP(=O)(O)O.CCOC(C)=O.Cc1cn(COCOC(=O)c2ccccc2)c(=O)[nH]c1=O>C1=CC=CC=C1>CCOP(=O)(COCOCn1cc(C)c(=O)[nH]c1=O)OCC
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-77276d898fd0423db0141ad034a6f470
CCOP(=O)(COCOCCl)OCC.Nc1nc(Cl)c2[nH]cnc2n1>>CCOP(=O)(COCOCn1cnc2c(Cl)nc(N)nc21)OCC
[H-].[Na+].ClCOCOCP(=O)(OCC)OCC.NC1=NC(=C2NC=NC2=N1)Cl>>NC1=NC(=C2N=CN(C2=N1)COCOCP(=O)(OCC)OCC)Cl
Cl[CH2:10][O:9][CH2:8][O:7][CH2:6][P:4]([O:3][CH2:2][CH3:1])(=[O:5])[O:22][CH2:23][CH3:24].[nH:11]1[cH:12][n:13][c:14]2[n:20][c:18]([NH2:19])[n:17][c:15]([Cl:16])[c:21]12>>[CH3:1][CH2:2][O:3][P:4](=[O:5])([CH2:6][O:7][CH2:8][O:9][CH2:10][n:11]1[cH:12][n:13][c:14]2[c:15]([Cl:16])[n:17][c:18]([NH2:19])[n:20][c:21]12)[O:2...
CCOP(=O)(COCOCCl)OCC.Nc1nc(Cl)c2[nH]cnc2n1
CCOP(=O)(COCOCn1cnc2c(Cl)nc(N)nc21)OCC
null
null
CN(C)C=O
Heteroatom Alkylation and Arylation
OtherReaction
216f1d1b2e599190b2de244995a4e132e5cff1104483d70bd1d02c3a4261d102
a0a01b3cbff93f3bdd38266e6735d54f714324d4b50ebf14fee21f956ddad209
c1ncc2nc[nH]c2n1
Cl-[CH2;D2;+0:1]-[#8:2]-[C:3].[Cl;D1;H0:4]-[c;H0;D3;+0:5]1:[#7;a:6]:[c:7](-[N;D1;H2:8]):[n;H0;D2;+0:9]:[c;H0;D3;+0:10]2:[#7;a:11]:[c:12]:[nH;D2;+0:13]:[c;H0;D3;+0:14]:2:1>>[C:3]-[#8:2]-[CH2;D2;+0:1]-[n;H0;D3;+0:13]1:[c:12]:[#7;a:11]:[c;H0;D3;+0:10]2:[c;H0;D3;+0:5](-[Cl;D1;H0:4]):[#7;a:6]:[c:7](-[N;D1;H2:8]):[n;H0;D2;+0...
null
[]
25
CELSIUS
1
HOUR
To a suspension of 60% sodium hydride in mineral oil (1.4 g, 34.5 mmol) in DMF (100 mL) was added 2-amino-6-chloropurine (5.78 g, 34.2 mmol) and the mixture was stirred for 1 hr at 25° C. To the resulting yellow solution was added dropwise a solution of above chloromethoxy(diethylphosphonomethoxy)methane in DMF (20 mL)...
10.6084/m9.figshare.5104873.v1
null
Aromatic halide.Primary halide.Ether
Aromatic halide.Ether
c1ncc2[nH]cnc2n1
c1ncc2nc[nH]c2n1
c1ncc2nc[nH]c2n1
HCl
CN(C)C=O
25
1
CCOP(=O)(COCOCCl)OCC.Nc1nc(Cl)c2[nH]cnc2n1>CN(C)C=O>CCOP(=O)(COCOCn1cnc2c(Cl)nc(N)nc21)OCC
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-93d03e24b2e64b579f6821175b3c99c2
CCOP(COCOCCl)OCC.Nc1ncnc2nc[nH]c12>>CCOP(=O)(COCOCn1cnc2c(N)ncnc21)OCC
ClCOCOCP(OCC)OCC.[H-].[Na+].C(C)OP(=O)(OCC)[O-].ClCOCOCCl.N1=CN=C2N=CNC2=C1N>>C(C)OP(=O)(OCC)COCOCN1C2=NC=NC(=C2N=C1)N
Cl[CH2:10][O:9][CH2:8][O:7][CH2:6][P:4]([O:3][CH2:2][CH3:1])[O:21][CH2:22][CH3:23].[n:11]1[cH:12][nH:13][c:14]2[c:15]([NH2:16])[n:17][cH:18][n:19][c:20]12>>[CH3:1][CH2:2][O:3][P:4](=[O:5])([CH2:6][O:7][CH2:8][O:9][CH2:10][n:11]1[cH:12][n:13][c:14]2[c:15]([NH2:16])[n:17][cH:18][n:19][c:20]12)[O:21][CH2:22][CH3:23]
CCOP(COCOCCl)OCC.Nc1ncnc2nc[nH]c12
CCOP(=O)(COCOCn1cnc2c(N)ncnc21)OCC
null
null
CN(C)C=O
Functional Group Interconversion
OtherReaction
9abd68eff6abfb54236fe246d2ef743ebf10d5f42c95aac86e158e6fcd485fec
42c71821dc42e0c1902cec868cf7d0abd0a4511b0313126f4c5eb9aac58d5cad
c1ncc2nc[nH]c2n1
Cl-[CH2;D2;+0:1]-[#8:2]-[C:3]-[#8:4]-[C:5]-[P;H0;D3;+0:6](-[#8:7]-[C:8])-[#8:9]-[C:10].[N;D1;H2:11]-[c:12]1:[#7;a:13]:[c:14]:[#7;a:15]:[c:16]2:[n;H0;D2;+0:17]:[c:18]:[nH;D2;+0:19]:[c:20]:1:2>>[C:8]-[#8:7]-[P;H0;D4;+0:6](=[O;D1;H0:21])(-[#8:9]-[C:10])-[C:5]-[#8:4]-[C:3]-[#8:2]-[CH2;D2;+0:1]-[n;H0;D3;+0:17]1:[c:18]:[n;H0...
null
[]
80
CELSIUS
1
HOUR
To a suspension of 60% sodium hydride in mineral oil (1.4 g, 34.5 mmol) in DMF (100 mL) was added adenine (4.7 g, 34.5 mmol) and the mixture was stirred at 80° C. for 1 hr. To the resulting yellow solution was added dropwise a solution of chloromethoxy(diethoxyphosphinomethoxy)methane [(prepared from diethylphosphate (...
10.6084/m9.figshare.5104873.v1
null
Primary halide.Ether
Ether
c1ncc2nc[nH]c2n1
c1ncnc2[nH]cnc12
c1ncnc2[nH]cnc12
null
CN(C)C=O
80
1
CCOP(COCOCCl)OCC.Nc1ncnc2nc[nH]c12>CN(C)C=O>CCOP(=O)(COCOCn1cnc2c(N)ncnc21)OCC
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-56bf9eb6e7e746298f149b2bbd996b66
CCOP(=O)(COCOCCl)OCC.Nc1cc[nH]c(=O)n1>>CCOP(=O)(COCOCn1ccc(N)nc1=O)OCC
[H-].[Na+].ClCOCOCP(=O)(OCC)OCC.N1C(=O)N=C(N)C=C1>>C(C)OP(=O)(OCC)COCOCN1C(=O)N=C(N)C=C1
Cl[CH2:10][O:9][CH2:8][O:7][CH2:6][P:4]([O:3][CH2:2][CH3:1])(=[O:5])[O:19][CH2:20][CH3:21].[nH:11]1[cH:12][cH:13][c:14]([NH2:15])[n:16][c:17]1=[O:18]>>[CH3:1][CH2:2][O:3][P:4](=[O:5])([CH2:6][O:7][CH2:8][O:9][CH2:10][n:11]1[cH:12][cH:13][c:14]([NH2:15])[n:16][c:17]1=[O:18])[O:19][CH2:20][CH3:21]
CCOP(=O)(COCOCCl)OCC.Nc1cc[nH]c(=O)n1
CCOP(=O)(COCOCn1ccc(N)nc1=O)OCC
null
null
CN(C)C=O
Heteroatom Alkylation and Arylation
N-alkylation of secondary amines with alkyl halides
06dfed3106c428c0f55338752b8abbb17bab6785f3cc392db7055710fc6495af
969a4609e178674696657c590a647839ca01abd1f90b8f0c9e475b1d6507651b
O=c1nccc[nH]1
Cl-[CH2;D2;+0:1]-[#8:2]-[C:3].[O;D1;H0:4]=[c:5]1:[#7;a:6]:[c:7]:[c:8]:[c:9]:[nH;D2;+0:10]:1>>[C:3]-[#8:2]-[CH2;D2;+0:1]-[n;H0;D3;+0:10]1:[c:9]:[c:8]:[c:7]:[#7;a:6]:[c:5]:1=[O;D1;H0:4]
null
[]
80
CELSIUS
15
HOUR
To a suspension of 60% sodium hydride in mineral oil (700 mg, 17 mmol) in DMF (50 mL) was added cytosine (1.9 g, 17 mmol) and the mixture was heated at 80° C. for 2 hr under nitrogen. To the resulting yellow solution was added dropwise a solution of chloromethoxy(diethylphosphonomethoxy)methane [prepared from diethylph...
10.6084/m9.figshare.5104873.v1
null
Primary halide.Ether
Ether
c1ccncn1
c1cncnc1
c1cncnc1
HCl
CN(C)C=O
80
15
CCOP(=O)(COCOCCl)OCC.Nc1cc[nH]c(=O)n1>CN(C)C=O>CCOP(=O)(COCOCn1ccc(N)nc1=O)OCC
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-e7425b3ba2444f079944b9d7bd609176
C=O.ClCCl.OCC[Se]c1ccccc1>>ClCOCC[Se]c1ccccc1
C1(=CC=CC=C1)[Se]CCO.C=O.C(Cl)Cl>>C1(=CC=CC=C1)[Se]CCOCCl
O=[CH2:2].ClC[Cl:1].[OH:3][CH2:4][CH2:5][Se:6][c:7]1[cH:8][cH:9][cH:10][cH:11][cH:12]1>>[Cl:1][CH2:2][O:3][CH2:4][CH2:5][Se:6][c:7]1[cH:8][cH:9][cH:10][cH:11][cH:12]1
C=O.ClCCl.OCC[Se]c1ccccc1
ClCOCC[Se]c1ccccc1
null
null
null
Heteroatom Alkylation and Arylation
OtherReaction
2f66a7b791ce8e51834c825fa4b4a8e80b5ba150d2e0f9b01c3670ab1489df68
c22f3e3cfb808b8fb5dc9e224a4962596d53a693fe06c73a918a5d25fa10d01c
c1ccccc1
Cl-C-[Cl;H0;D1;+0:1].O=[CH2;D1;+0:2].[C:3]-[C:4]-[OH;D1;+0:5]>>[C:3]-[C:4]-[O;H0;D2;+0:5]-[CH2;D2;+0:2]-[Cl;H0;D1;+0:1]
null
[]
null
null
null
null
To a solution of 2-(phenylselenyl)ethanol (4.0 g, 20 mmol) [prepared according to the literature procedure: P. Rollin, V. V. Bencomo, P. Sinay, Synthesis, 13 (1984)] in CH2Cl2 (15 mL) was added paraformaldehyde (620 mg, 20 mmol). HCl gas was then bubbled into the solution at 5° C. for 2 hr. The solution was dried (MgSO...
10.6084/m9.figshare.5104873.v1
null
Primary halide.Primary halide.Formaldehyde.Primary alcohol
Primary halide.Ether
null
null
c1ccccc1
HCl
null
null
null
C=O.ClCCl.OCC[Se]c1ccccc1>>ClCOCC[Se]c1ccccc1
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-eb7c577d427641d3b098b5304ce0b096
COC1CCC(OC)O1.Cc1c[nH]c(=O)[nH]c1=O>>COC1CCC(n2cc(C)c(=O)[nH]c2=O)O1
COC1OC(CC1)OC.[Sn](Cl)(Cl)(Cl)Cl.S(=O)(=O)([O-])[O-].[NH4+].[NH4+].Cl[Si](C)(C)C.N1C(=O)NC(=O)C(C)=C1>>COC1CCC(O1)N1C(=O)NC(=O)C(C)=C1
CO[CH:6]1[CH2:5][CH2:4][CH:3]([O:2][CH3:1])[O:16]1.[nH:7]1[cH:8][c:9]([CH3:10])[c:11](=[O:12])[nH:13][c:14]1=[O:15]>>[CH3:1][O:2][CH:3]1[CH2:4][CH2:5][CH:6]([n:7]2[cH:8][c:9]([CH3:10])[c:11](=[O:12])[nH:13][c:14]2=[O:15])[O:16]1
COC1CCC(OC)O1.Cc1c[nH]c(=O)[nH]c1=O
COC1CCC(n2cc(C)c(=O)[nH]c2=O)O1
null
null
C[Si](N[Si](C)(C)C)(C)C.C(C)(=O)OCC.ClC(C)Cl
Heteroatom Alkylation and Arylation
OtherReaction
9b598d3fa89a3273540ae795a39c8396c116d041fc8f58b6aa756468b2271686
ccc058ecd89f692c39a92bd6db91fb86578428d38b5955a659e0a2343eccf0fd
O=c1ccn(C2CCCO2)c(=O)[nH]1
C-O-[CH;D3;+0:1]1-[#8:2]-[C:3]-[C:4]-[C:5]-1.[O;D1;H0:6]=[c:7]1:[#7;a:8]:[c:9]:[c:10]:[c:11]:[nH;D2;+0:12]:1>>[O;D1;H0:6]=[c:7]1:[#7;a:8]:[c:9]:[c:10]:[c:11]:[n;H0;D3;+0:12]:1-[CH;D3;+0:1]1-[#8:2]-[C:3]-[C:4]-[C:5]-1
null
[]
145
CELSIUS
null
null
To a suspension of thymine (2.5 g, 20 mmol) in hexamethyldisilazane (30 mL) was added ammonium sulfate (50 mg) and chlorotrimethylsilane (0.5 mL) and the mixture was heated at 145° C. for 4 hr under nitrogen. The excess hexamethyldisilazane was removed at reduced pressure, and the residual oil was dissolved in xylene a...
10.6084/m9.figshare.5104873.v1
null
Ether.Ether
Ether
C1CCOC1.c1cncnc1
C1CCOC1.c1cncnc1
C1CCOC1.c1cncnc1
HO-
C[Si](N[Si](C)(C)C)(C)C.C(C)(=O)OCC.ClC(C)Cl
145
null
COC1CCC(OC)O1.Cc1c[nH]c(=O)[nH]c1=O>C[Si](N[Si](C)(C)C)(C)C.C(C)(=O)OCC.ClC(C)Cl>COC1CCC(n2cc(C)c(=O)[nH]c2=O)O1
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-560dc193ecc34b789acc357ab3f450a5
CC(=O)Nc1nc(C(=O)N(c2ccccc2)c2ccccc2)c2ncn(COCC[Se]c3ccccc3)c2n1>>C=COCn1cnc2c(C(=O)N(c3ccccc3)c3ccccc3)nc(NC(C)=O)nc21
C(C)(C)N(CC)C(C)C.C(C)(=O)NC1=NC(=C2N=CN(C2=N1)COCC[Se]C1=CC=CC=C1)C(N(C1=CC=CC=C1)C1=CC=CC=C1)=O.OO.C([O-])(O)=O.[Na+]>>C(C)(=O)NC1=NC(=C2N=CN(C2=N1)COC=C)C(N(C1=CC=CC=C1)C1=CC=CC=C1)=O
c1ccc([Se][CH2:1][CH2:2][O:3][CH2:4][n:5]2[cH:6][n:7][c:8]3[c:9]([C:10](=[O:11])[N:12]([c:13]4[cH:14][cH:15][cH:16][cH:17][cH:18]4)[c:19]4[cH:20][cH:21][cH:22][cH:23][cH:24]4)[n:25][c:26]([NH:27][C:28]([CH3:29])=[O:30])[n:31][c:32]23)cc1>>[CH2:1]=[CH:2][O:3][CH2:4][n:5]1[cH:6][n:7][c:8]2[c:9]([C:10](=[O:11])[N:12]([c:1...
CC(=O)Nc1nc(C(=O)N(c2ccccc2)c2ccccc2)c2ncn(COCC[Se]c3ccccc3)c2n1
C=COCn1cnc2c(C(=O)N(c3ccccc3)c3ccccc3)nc(NC(C)=O)nc21
null
null
O1CCOCC1
Functional Group Interconversion
OtherReaction
f0f1a26b0ed9935583cab47eabbbc5114ef7eea7864650856d5594f762522cc3
258173fc649f8a796b89cbbce487cd2ae8fd8b5c210e0d7885f99df8ff5c9f48
O=C(c1ncnc2[nH]cnc12)N(c1ccccc1)c1ccccc1
[C:1]-[#8:2]-[CH2;D2;+0:3]-[CH2;D2;+0:4]-[Se]-c1:c:c:c:c:c:1>>[C:1]-[#8:2]-[CH;D2;+0:3]=[CH2;D1;+0:4]
null
[]
60
CELSIUS
null
null
To a solution of 2-acetamido-6-diphenylcarbamoyl-9-[2-(phenylselenyl)ethoxymethyl]purine (4.92 g, 8.16 mmol) in dioxane (80 mL) was added 30% H2O2 (4 mL, 35 mmol) and sodium bicarbonate (2.1 g, 24.5 mmol). The mixture was heated at 60° C. for 20 min. The reaction was then concentrated to about 10 mL, diluted with ethyl...
10.6084/m9.figshare.5104873.v1
null
Ether
Ether.Vinyl
c1ccccc1
null
c1ccccc1.c1ccccc1.c1ncc2nc[nH]c2n1
Se
O1CCOCC1
60
null
CC(=O)Nc1nc(C(=O)N(c2ccccc2)c2ccccc2)c2ncn(COCC[Se]c3ccccc3)c2n1>O1CCOCC1>C=COCn1cnc2c(C(=O)N(c3ccccc3)c3ccccc3)nc(NC(C)=O)nc21
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-a66c33e4b2254f71b2ba86198e200a69
CC(C)(C)C(=O)Cl.Nc1ncnc2c1ncn2[C@H]1CC=CO1>>CC(C)(C)C(=O)Nc1ncnc2c1ncn2[C@H]1CC=CO1
CO.O1[C@H](CC=C1)N1C2=NC=NC(=C2N=C1)N.CC(C(=O)Cl)(C)C.C(Cl)Cl.CO>>O1[C@H](CC=C1)N1C2=NC=NC(=C2N=C1)NC(C(C)(C)C)=O
Cl[C:5]([C:2]([CH3:1])([CH3:3])[CH3:4])=[O:6].[NH2:7][c:8]1[n:9][cH:10][n:11][c:12]2[c:13]1[n:14][cH:15][n:16]2[C@H:17]1[CH2:18][CH:19]=[CH:20][O:21]1>>[CH3:1][C:2]([CH3:3])([CH3:4])[C:5](=[O:6])[NH:7][c:8]1[n:9][cH:10][n:11][c:12]2[c:13]1[n:14][cH:15][n:16]2[C@H:17]1[CH2:18][CH:19]=[CH:20][O:21]1
CC(C)(C)C(=O)Cl.Nc1ncnc2c1ncn2[C@H]1CC=CO1
CC(C)(C)C(=O)Nc1ncnc2c1ncn2[C@H]1CC=CO1
null
CN(C1=CC=NC=C1)C
N1=CC=CC=C1
Acylation
Acylation of Nitrogen Nucleophiles by Acyl/Thioacyl/Carbamoyl Halides and Analogs_OS
38143a4d536201990008fd6f2c68e6571a341d1c367481869fbbbe36cb038937
0e6ae078978e324f714e184b4f72826d4e3bf2d9ab22d6e9f73740af687be16f
C1=CO[C@@H](n2cnc3cncnc32)C1
Cl-[C;H0;D3;+0:1](=[O;D1;H0:2])-[C:3](-[C;D1;H3:4])(-[C;D1;H3:5])-[C;D1;H3:6].[NH2;D1;+0:7]-[c:8]1:[#7;a:9]:[c:10]:[#7;a:11]:[c:12]2:[#7;a:13]:[c:14]:[#7;a:15]:[c:16]:2:1>>[C;D1;H3:4]-[C:3](-[C;D1;H3:5])(-[C;D1;H3:6])-[C;H0;D3;+0:1](=[O;D1;H0:2])-[NH;D2;+0:7]-[c:8]1:[#7;a:9]:[c:10]:[#7;a:11]:[c:12]2:[#7;a:13]:[c:14]:[#...
94
[{"value": 94.0, "product": "O1[C@H](CC=C1)N1C2=NC=NC(=C2N=C1)NC(C(C)(C)C)=O", "details": "PERCENTYIELD", "is_desired": false}]
55
CELSIUS
30
MINUTE
To a suspension of the product of Step C (196 g, 0.97 mole), 4-dimethylaminopyridine (5.9 g, 0.048 mole) in dry pyridine (970 mL) at 26° C. was added dropwise over 1 hr trimethylacetylchloride (145 mL, 142.1 g, 1.18 mole, 1.2 equiv.). A slight 3° C. exotherm was noted. The reaction mixture was then heated to 55° C. for...
10.6084/m9.figshare.5104873.v1
null
Acyl halide.Primary amine
Secondary amide
null
null
c1ncnc2nc[nH]c12.C1=COCC1
HCl
CN(C1=CC=NC=C1)C.N1=CC=CC=C1
55
0.5
CC(C)(C)C(=O)Cl.Nc1ncnc2c1ncn2[C@H]1CC=CO1>CN(C1=CC=NC=C1)C.N1=CC=CC=C1>CC(C)(C)C(=O)Nc1ncnc2c1ncn2[C@H]1CC=CO1
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-f026b66c93374e7dacf2ff70e1bdeab8
NN.O=C(O)CCC(=O)c1ccc(Cl)cc1>>O=C1CCC(c2ccc(Cl)cc2)=NN1
ClC1=CC=C(C(=O)CCC(=O)O)C=C1.O.NN>>ClC1=CC=C(C=C1)C=1CCC(NN1)=O
[NH2:13][NH2:14].O=[C:5]([CH2:4][CH2:3][C:2](O)=[O:1])[c:6]1[cH:7][cH:8][c:9]([Cl:10])[cH:11][cH:12]1>>[O:1]=[C:2]1[CH2:3][CH2:4][C:5]([c:6]2[cH:7][cH:8][c:9]([Cl:10])[cH:11][cH:12]2)=[N:13][NH:14]1
NN.O=C(O)CCC(=O)c1ccc(Cl)cc1
O=C1CCC(c2ccc(Cl)cc2)=NN1
null
null
C(C)O
Acylation
OtherReaction
16e715242dd5e92f711d46176c552652cef6c6f4fed9bc9a09a311d5b0b86cea
30de68c4dde17a0553a43eee47b1b865b8390bb08557512a59e6e71e0ed0ad51
O=C1CCC(c2ccccc2)=NN1
O-[C;H0;D3;+0:1](=[O;D1;H0:2])-[C:3]-[C:4]-[C;H0;D3;+0:5](=O)-[c:6](:[c:7]):[c:8].[NH2;D1;+0:9]-[NH2;D1;+0:10]>>[O;D1;H0:2]=[C;H0;D3;+0:1]1-[C:3]-[C:4]-[C;H0;D3;+0:5](-[c:6](:[c:7]):[c:8])=[N;H0;D2;+0:9]-[NH;D2;+0:10]-1
81.5
[{"value": 80.0, "product": "ClC1=CC=C(C=C1)C=1CCC(NN1)=O", "details": "PERCENTYIELD", "is_desired": false}, {"value": 81.5, "product": "ClC1=CC=C(C=C1)C=1CCC(NN1)=O", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
null
null
To a solution of 3-(4-chlorobenzoyl)propionic acid (20 g) in absolute ethanol (200 ml) was added 5 g of hydrazine monohydrate. A thick solid was formed which dissolved after heating. The resulting solution was refluxed for 3 h, cooled and the solid formed filtered and dried to yield 16 g (80%) of 6-(4-chlorophenyl)-4,5...
10.6084/m9.figshare.5104873.v1
null
Hydrazine.Carboxylic acid.Ketone
Hydrazone amide
null
C1=NNCCC1
C1=NNCCC1.c1ccccc1
HO-
C(C)O
null
null
NN.O=C(O)CCC(=O)c1ccc(Cl)cc1>C(C)O>O=C1CCC(c2ccc(Cl)cc2)=NN1
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-d1cec5adaec74900a26ae5c2339bc4da
CC(C(=O)O)C(=O)c1ccc(Cl)cc1.CC(C)(C)NN>>CC(C)(C)N1N=C(c2ccc(Cl)cc2)CCC1=O
ClC1=CC=C(C(=O)C(C(=O)O)C)C=C1.C(C)(=O)[O-].[Na+].Cl.C(C)(C)(C)NN>>ClC1=CC=C(C=C1)C=1CCC(N(N1)C(C)(C)C)=O
O=[C:7]([c:8]1[cH:9][cH:10][c:11]([Cl:12])[cH:13][cH:14]1)[CH:15]([CH3:16])[C:17](O)=[O:18].[CH3:1][C:2]([CH3:3])([CH3:4])[NH:5][NH2:6]>>[CH3:1][C:2]([CH3:3])([CH3:4])[N:5]1[N:6]=[C:7]([c:8]2[cH:9][cH:10][c:11]([Cl:12])[cH:13][cH:14]2)[CH2:15][CH2:16][C:17]1=[O:18]
CC(C(=O)O)C(=O)c1ccc(Cl)cc1.CC(C)(C)NN
CC(C)(C)N1N=C(c2ccc(Cl)cc2)CCC1=O
null
null
C(CCC)O
Acylation
OtherReaction
4e477d09c29dc9649665c2a512a7ab66ed0db9837b745e511eba3c76a3cc18d7
30de68c4dde17a0553a43eee47b1b865b8390bb08557512a59e6e71e0ed0ad51
O=C1CCC(c2ccccc2)=NN1
O-[C;H0;D3;+0:1](=[O;D1;H0:2])-[CH;D3;+0:3](-[CH3;D1;+0:4])-[C;H0;D3;+0:5](=O)-[c:6](:[c:7]):[c:8].[C;D1;H3:9]-[C:10](-[C;D1;H3:11])(-[C;D1;H3:12])-[NH;D2;+0:13]-[NH2;D1;+0:14]>>[C;D1;H3:9]-[C:10](-[C;D1;H3:11])(-[C;D1;H3:12])-[N;H0;D3;+0:13]1-[N;H0;D2;+0:14]=[C;H0;D3;+0:5](-[c:6](:[c:7]):[c:8])-[CH2;D2;+0:3]-[CH2;D2;+...
34.4
[{"value": 34.4, "product": "ClC1=CC=C(C=C1)C=1CCC(N(N1)C(C)(C)C)=O", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
null
null
To a solution of 4-chlorobenzoylpropionic acid (4.24 g) in n-butanol (150 ml) was added anhydrous sodium acetate (1.54 g) and t-butylhydrazine hydrochloride (2.75 g) portionwise at room temperature. The resulting mixture was refluxed for 9 hours distilling off 65 ml of n-butanol during that time. The resulting mixture ...
10.6084/m9.figshare.5104873.v1
null
Hydrazine.Carboxylic acid.Ketone
Hydrazone amide
null
C1=N[NH]CCC1
C1=N[NH]CCC1.c1ccccc1
HO-
C(CCC)O
null
null
CC(C(=O)O)C(=O)c1ccc(Cl)cc1.CC(C)(C)NN>C(CCC)O>CC(C)(C)N1N=C(c2ccc(Cl)cc2)CCC1=O
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-4180ca501a3f4f4d860ac5334c81ecf5
COC(=O)CCC(=O)OC.COC(=O)c1cccc(Cl)c1>>O=C(O)CCC(=O)c1cccc(Cl)c1
C(CCC(=O)OC)(=O)OC.[Na].C(C)O.ClC=1C=C(C(=O)OC)C=CC1.C(CCC(=O)OC)(=O)OC>>ClC=1C=C(C(=O)CCC(=O)O)C=CC1
COC(=O)[CH2:5][CH2:4][C:2](=[O:1])[O:3]C.CO[C:6](=[O:7])[c:8]1[cH:9][cH:10][cH:11][c:12]([Cl:13])[cH:14]1>>[O:1]=[C:2]([OH:3])[CH2:4][CH2:5][C:6](=[O:7])[c:8]1[cH:9][cH:10][cH:11][c:12]([Cl:13])[cH:14]1
COC(=O)CCC(=O)OC.COC(=O)c1cccc(Cl)c1
O=C(O)CCC(=O)c1cccc(Cl)c1
null
null
CCOCC
C-C Coupling
OtherReaction
6d482de2a0c1fffe47581cf2d6dc0eefca79628574252eec326be9292f335afe
1f69704fe402a3eb0e91a243a59f68f972592be61b4c787368515903d4c85726
c1ccccc1
C-O-C(=O)-[CH2;D2;+0:1]-[C:2]-[C:3](=[O;D1;H0:4])-[O;H0;D2;+0:5]-C.C-O-[C;H0;D3;+0:6](=[O;D1;H0:7])-[c:8](:[c:9]):[c:10]>>[O;D1;H0:4]=[C:3](-[OH;D1;+0:5])-[C:2]-[CH2;D2;+0:1]-[C;H0;D3;+0:6](=[O;D1;H0:7])-[c:8](:[c:9]):[c:10]
null
[]
null
null
null
null
Sodium (11 g, spheres) was added to 200 ml ethanol with stirring. When the gas evolution ceased, methyl 3-chlorobenzoate (10 g, 0.057 mole) and dimethyl succinate (9.0 g, 0.615 mole) were added rapidly and the mixture was stirred for 5 minutes at room temperature. The mixture was slowly concentrated on a rotary evapora...
10.6084/m9.figshare.5104873.v1
null
Ester.Ester.Ester
Carboxylic acid.Ketone
null
null
c1ccccc1
HO-
CCOCC
null
null
COC(=O)CCC(=O)OC.COC(=O)c1cccc(Cl)c1>CCOCC>O=C(O)CCC(=O)c1cccc(Cl)c1
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-6293fd2e9db947d781cf392334ab42c8
Cc1ccc(C(=O)CCC(=O)O)cc1.ClCl>>Cc1c(Cl)cc(C(=O)CCC(=O)O)cc1Cl
CC1=CC=C(C(=O)CCC(=O)O)C=C1.[Cl-].[Al+3].[Cl-].[Cl-].ClCl>>ClC=1C=C(C(=O)CCC(=O)O)C=C(C1C)Cl
[CH3:1][c:2]1[cH:3][cH:5][c:6]([C:7](=[O:8])[CH2:9][CH2:10][C:11](=[O:12])[OH:13])[cH:14][cH:15]1.[Cl:4][Cl:16]>>[CH3:1][c:2]1[c:3]([Cl:4])[cH:5][c:6]([C:7](=[O:8])[CH2:9][CH2:10][C:11](=[O:12])[OH:13])[cH:14][c:15]1[Cl:16]
Cc1ccc(C(=O)CCC(=O)O)cc1.ClCl
Cc1c(Cl)cc(C(=O)CCC(=O)O)cc1Cl
null
null
C(Cl)Cl
Miscellaneous
OtherReaction
d2a751fe92dcfde720edd5e4971c1aa6cc149bff4a6d230cc6b5cac59ec9498c
861258def4b3bd7367f8a87cde43fe585d40dc3669ea29055dbcb9a2de101a4d
c1ccccc1
[C;D1;H3:1]-[c:2]1:[cH;D2;+0:3]:[c:4]:[c:5](-[C:6]=[O;D1;H0:7]):[c:8]:[cH;D2;+0:9]:1.[Cl;H0;D1;+0:10]-[Cl;H0;D1;+0:11]>>[C;D1;H3:1]-[c:2]1:[c;H0;D3;+0:3](-[Cl;H0;D1;+0:10]):[c:4]:[c:5](-[C:6]=[O;D1;H0:7]):[c:8]:[c;H0;D3;+0:9]:1-[Cl;H0;D1;+0:11]
44.2
[{"value": 44.2, "product": "ClC=1C=C(C(=O)CCC(=O)O)C=C(C1C)Cl", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
null
null
To a mixture of 3-(4-methylbenzoyl)propionic acid (7.5 g) and methylene chloride (250 ml) was added slowly portionwise aluminum chloride (15 g) at 0° C. After the addition was completed chlorine gas was bubbled in slowly at 0° C. After 6 hours the reaction mixture was poured into a mixture of hydrochloric acid and ice ...
10.6084/m9.figshare.5104873.v1
null
null
Aromatic halide.Aromatic halide
c1ccccc1
c1ccccc1
c1ccccc1
null
C(Cl)Cl
null
null
Cc1ccc(C(=O)CCC(=O)O)cc1.ClCl>C(Cl)Cl>Cc1c(Cl)cc(C(=O)CCC(=O)O)cc1Cl
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-fc69e41020da42a2a18c5933d3ff4b1f
C1=COCCC1.OCC#CCO>>OCC#CCOC1CCCCO1
C(C#CCO)O.O1CCCC=C1>>O1C(CCCC1)OCC#CCO
[CH:7]1=[CH:8][CH2:9][CH2:10][CH2:11][O:12]1.[OH:1][CH2:2][C:3]#[C:4][CH2:5][OH:6]>>[OH:1][CH2:2][C:3]#[C:4][CH2:5][O:6][CH:7]1[CH2:8][CH2:9][CH2:10][CH2:11][O:12]1
C1=COCCC1.OCC#CCO
OCC#CCOC1CCCCO1
null
C1(=CC=C(C=C1)S(=O)(=O)O)C
CCOCC
Heteroatom Alkylation and Arylation
oxa-Michael addition
abdcab389770d0a73be3b825aa1d56cee234da38dbdf3510fe8104d481e7cf3f
c6a3efa2acb508a32cdf9fcedfcd9635cce0ecdcf12c094b743aa576ea01fd9a
C1CCOCC1
[#8:1]1-[C:2]-[C:3]-[C:4]-[CH;D2;+0:5]=[CH;D2;+0:6]-1.[C:7]-[C:8]#[C:9]-[C:10]-[OH;D1;+0:11]>>[C:7]-[C:8]#[C:9]-[C:10]-[O;H0;D2;+0:11]-[CH;D3;+0:6]1-[#8:1]-[C:2]-[C:3]-[C:4]-[CH2;D2;+0:5]-1
68.8
[{"value": 68.8, "product": "O1C(CCCC1)OCC#CCO", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
null
null
To a mixture of 5.0 g of 2-butyne-1,4-diol and 10 milligrams of p-toluenesulfonic acid and 150 ml of dry ether there was added dropwise with stirring at room temperature 4.9 g of 3,4-dihydro-2H-pyran. After stirring overnight at ambient temperature the ether was evaporated and the residue was poured into 200 ml of wate...
10.6084/m9.figshare.5104873.v1
null
Ether.Primary alcohol
Ether.Ether
C1=COCCC1
C1CCOCC1
C1CCOCC1
null
C1(=CC=C(C=C1)S(=O)(=O)O)C.CCOCC
null
null
C1=COCCC1.OCC#CCO>C1(=CC=C(C=C1)S(=O)(=O)O)C.CCOCC>OCC#CCOC1CCCCO1
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-a87607fbb9ca412d85516fecfc51ea39
C#CC1CCCCC1.C=O>>OCC#CC1CCCCC1
C1(CCCCC1)C#C.C=O.C=O>>C1(CCCCC1)C#CCO
[CH:3]#[C:4][CH:5]1[CH2:6][CH2:7][CH2:8][CH2:9][CH2:10]1.[O:1]=[CH2:2]>>[OH:1][CH2:2][C:3]#[C:4][CH:5]1[CH2:6][CH2:7][CH2:8][CH2:9][CH2:10]1
C#CC1CCCCC1.C=O
OCC#CC1CCCCC1
null
null
CCOCC
C-C Coupling
OtherReaction
b068d8bba9f864ba971dd324292d9b3526f0235b4ab7e3a9ce6aa76a39c4a1e7
22ebec2cc94dd24863aea8793d450cfe0691e1036be204d1a4c79c16effe90a4
C1CCCCC1
[CH2;D1;+0:1]=[O;H0;D1;+0:2].[C:3]-[C:4]#[CH;D1;+0:5]>>[C:3]-[C:4]#[C;H0;D2;+0:5]-[CH2;D2;+0:1]-[OH;D1;+0:2]
null
[]
null
null
null
null
To a solution of ethyl magesium bromide (prepared from 2.5 g of magnesium turning and 11.3 g of bromoethane) in ether was added dropwise a solution of 10.2 g of cyclohexylacetylene in ether and the reaction mixture was refluxed for 2 hours. The reaction mixture was cooled to ambient temperature and anhydrous formaldehy...
10.6084/m9.figshare.5104873.v1
null
Formaldehyde.Alkyne
Primary alcohol.Alkyne
null
null
C1CCCCC1
null
CCOCC
null
null
C#CC1CCCCC1.C=O>CCOCC>OCC#CC1CCCCC1
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-a01b2f9c7fd648488efd533de927a930
O=C1CCC(c2ccc(Cl)cc2)=NN1>>O=c1ccc(-c2ccc(Cl)cc2)n[nH]1
ClC1=CC=C(C=C1)C=1CCC(NN1)=O.C(C)(=O)O.BrBr>>ClC1=CC=C(C=C1)C=1C=CC(NN1)=O
[O:1]=[C:2]1[CH2:3][CH2:4][C:5]([c:6]2[cH:7][cH:8][c:9]([Cl:10])[cH:11][cH:12]2)=[N:13][NH:14]1>>[O:1]=[c:2]1[cH:3][cH:4][c:5](-[c:6]2[cH:7][cH:8][c:9]([Cl:10])[cH:11][cH:12]2)[n:13][nH:14]1
O=C1CCC(c2ccc(Cl)cc2)=NN1
O=c1ccc(-c2ccc(Cl)cc2)n[nH]1
null
null
O
Aromatic Heterocycle Formation
OtherReaction
73c80fbcc9dd7a9125aaf1059d9d4eab31b342d21fc860abf5e65fd78456864b
78b0616e5760c6d4dadfc1fac5c58c0254d0dc7b1bf102fea4bc1349928b0776
O=c1ccc(-c2ccccc2)n[nH]1
[O;D1;H0:1]=[C;H0;D3;+0:2]1-[CH2;D2;+0:3]-[CH2;D2;+0:4]-[C;H0;D3;+0:5](-[c;H0;D3;+0:6](:[c:7]:[c:8]):[c:9]:[c:10])=[N;H0;D2;+0:11]-[NH;D2;+0:12]-1>>[O;D1;H0:1]=[c;H0;D3;+0:2]1:[cH;D2;+0:3]:[cH;D2;+0:4]:[c;H0;D3;+0:5](-[c;H0;D3;+0:6](:[c:7]:[c:8]):[c:9]:[c:10]):[n;H0;D2;+0:11]:[nH;D2;+0:12]:1
93.1
[{"value": 89.0, "product": "ClC1=CC=C(C=C1)C=1C=CC(NN1)=O", "details": "PERCENTYIELD", "is_desired": false}, {"value": 93.1, "product": "ClC1=CC=C(C=C1)C=1C=CC(NN1)=O", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
null
null
To a solution of 6-(4-chlorophenyl)-4,5-dihydropyridazinone (11.75 g) and glacial acetic acid (100 ml) was added dropwise 3 ml of bromine and the mixture was heated at 60°-70° C. for 3 h. The resulting mixture was cooled and slowly poured into 400 ml of cold water. The resulting white solid was filtered and dried to yi...
10.6084/m9.figshare.5104873.v1
null
Hydrazone amide
null
C1=NNCCC1
c1cccnn1
c1cccnn1.c1ccccc1
null
O
null
null
O=C1CCC(c2ccc(Cl)cc2)=NN1>O>O=c1ccc(-c2ccc(Cl)cc2)n[nH]1
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-07f806809672440ba2c325ca90047b96
FC1(F)CC(Cl)(Cl)C1(F)Cl>>FC1(F)C=C(Cl)C1(F)Cl
ClC1(C(C(C1)(F)F)(F)Cl)Cl.O.Cl>>ClC1(C(C=C1Cl)(F)F)F
Cl[C:5]1([Cl:6])[CH2:4][C:2]([F:1])([F:3])[C:7]1([F:8])[Cl:9]>>[F:1][C:2]1([F:3])[CH:4]=[C:5]([Cl:6])[C:7]1([F:8])[Cl:9]
FC1(F)CC(Cl)(Cl)C1(F)Cl
FC1(F)C=C(Cl)C1(F)Cl
null
null
CCOCC.C(C)N(CC)CC
Functional Group Interconversion
OtherReaction
0ca523bc88d44f4371960ac2ff9ed0bbb8882337b7061f7fba5b4787f1e02481
986b135105e7920109b424799136a4a8281fb4a0f49253ce1bf5d4426ed78637
C1=CCC1
Cl-[C;H0;D4;+0:1]1(-[Cl;D1;H0:2])-[CH2;D2;+0:3]-[C:4](-[F;D1;H0:5])(-[F;D1;H0:6])-[C:7]-1(-[Cl;D1;H0:8])-[F;D1;H0:9]>>[Cl;D1;H0:2]-[C;H0;D3;+0:1]1=[CH;D2;+0:3]-[C:4](-[F;D1;H0:5])(-[F;D1;H0:6])-[C:7]-1(-[Cl;D1;H0:8])-[F;D1;H0:9]
79
[{"value": 79.0, "product": "ClC1(C(C=C1Cl)(F)F)F", "details": "PERCENTYIELD", "is_desired": false}, {"value": 78.2, "product": "ClC1(C(C=C1Cl)(F)F)F", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
8
HOUR
To a solution of 1,1,2 trichloro-2,3,3-trifluorocyclobutane (55.5 g) in 100 ml of anhydrous ether, triethylamine (40 ml) was added dropwise over 30 min at room temperature, and the mixture was stirred overnight at ambient temperature. The mixture was then stirred with 120 ml H2O and 7.5 ml of concentrated HCl. The ethe...
10.6084/m9.figshare.5104873.v1
null
Tertiary halide.Tertiary halide
Alkenyl halide
C1CCC1
C1=CCC1
C1=CCC1
HCl
CCOCC.C(C)N(CC)CC
null
8
FC1(F)CC(Cl)(Cl)C1(F)Cl>CCOCC.C(C)N(CC)CC>FC1(F)C=C(Cl)C1(F)Cl
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-12d76bd288204ab9895441c0ad284664
O=C(O)C(F)(F)C(F)(Cl)C(=O)O>>O=C(O)C(F)C(F)(F)C(=O)O
ClC(C(C(=O)O)(F)F)(C(=O)O)F>>FC(C(=O)O)(C(C(=O)O)F)F
Cl[C:6]([C:4]([C:2](=[O:1])[OH:3])([F:5])[F:7])([F:8])[C:9](=[O:10])[OH:11]>>[O:1]=[C:2]([OH:3])[CH:4]([F:5])[C:6]([F:7])([F:8])[C:9](=[O:10])[OH:11]
O=C(O)C(F)(F)C(F)(Cl)C(=O)O
O=C(O)C(F)C(F)(F)C(=O)O
null
[Zn]
O1CCOCC1
Functional Group Addition
Dehalogenation
7f145230bfb0115349e969b2f2fa1359cfafe8c166e52b50a867192005e1f5bc
d6722b0df465660a9eeeaca5a8f5b3dbb2d1ebccb44917f2eca97a85bf850d06
null
Cl-[C;H0;D4;+0:1](-[F;D1;H0:2])(-[C:3](=[O;D1;H0:4])-[O;D1;H1:5])-[C;H0;D4;+0:6](-[F;D1;H0:7])(-[F;H0;D1;+0:8])-[C:9](=[O;D1;H0:10])-[O;D1;H1:11]>>[F;D1;H0:7]-[CH;D3;+0:6](-[C:9](=[O;D1;H0:10])-[O;D1;H1:11])-[C;H0;D4;+0:1](-[F;D1;H0:2])(-[F;H0;D1;+0:8])-[C:3](=[O;D1;H0:4])-[O;D1;H1:5]
40.7
[{"value": 32.0, "product": "FC(C(=O)O)(C(C(=O)O)F)F", "details": "PERCENTYIELD", "is_desired": false}, {"value": 40.7, "product": "FC(C(=O)O)(C(C(=O)O)F)F", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
10
HOUR
To a stirring solution of the chlorotrifluorosuccinic acid (part b) (24.5 g) in 200 ml dioxane was added portionwise zinc metal (85 g) and the mixture was stirred at ambient temperature for 10 hours to yield a viscous liquid which was decanted from the unreacted zinc. Most of the dioxane was evaporated in vacuo. The re...
10.6084/m9.figshare.5104873.v1
null
Tertiary halide.Tertiary halide.Tertiary halide.Tertiary halide
Tertiary halide.Tertiary halide.Secondary halide
null
null
null
Other
[Zn].O1CCOCC1
null
10
O=C(O)C(F)(F)C(F)(Cl)C(=O)O>[Zn].O1CCOCC1>O=C(O)C(F)C(F)(F)C(=O)O
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-406ab0cccf234491959e2eb53d45aa2c
O=C1CCC(=O)O1.c1ccc2ccccc2c1>>O=C(O)CCC(=O)c1cccc2ccccc12
Cl.[Cl-].[Cl-].[Cl-].[Al+3].C1=CC=CC2=CC=CC=C12.C1(CCC(=O)O1)=O>>C1(=CC=CC2=CC=CC=C12)C(=O)CCC(=O)O
[O:1]=[C:2]1[O:3][C:6](=[O:7])[CH2:5][CH2:4]1.[cH:8]1[cH:9][cH:10][cH:11][c:12]2[cH:13][cH:14][cH:15][cH:16][c:17]12>>[O:1]=[C:2]([OH:3])[CH2:4][CH2:5][C:6](=[O:7])[c:8]1[cH:9][cH:10][cH:11][c:12]2[cH:13][cH:14][cH:15][cH:16][c:17]12
O=C1CCC(=O)O1.c1ccc2ccccc2c1
O=C(O)CCC(=O)c1cccc2ccccc12
null
null
[N+](=O)([O-])C1=CC=CC=C1
C-C Coupling
OtherReaction
d1b47ca78c3ceb45955ddf79d2b2d22c1a0978cf9fa8ded4c5ee0a8331deac4e
4836357c99dfeeac9d5083fedc379181a858ae45ac77bd85eb46e7e1a9df36f0
c1ccc2ccccc2c1
[O;D1;H0:1]=[C:2]1-[C:3]-[C:4]-[C;H0;D3;+0:5](=[O;D1;H0:6])-[O;H0;D2;+0:7]-1.[c:8]:[c:9]:[cH;D2;+0:10]:[c:11](:[c:12]):[c:13]>>[O;D1;H0:1]=[C:2](-[OH;D1;+0:7])-[C:3]-[C:4]-[C;H0;D3;+0:5](=[O;D1;H0:6])-[c;H0;D3;+0:10](:[c:9]:[c:8]):[c:11](:[c:12]):[c:13]
null
[]
null
null
null
null
A mixture of naphthalene (40 g) and succinic anhydride (20 g) was added to a well stirred suspension of aluminum trichloride (55 g) in nitrobenzene (140 ml). The resulting mixture was stirred overnight at room temperature. The mixture was then poured slowly onto ice-water (600 g) and acidified with 6N-hydrochloric acid...
10.6084/m9.figshare.5104873.v1
null
Anhydride
Carboxylic acid.Ketone
C1CCOC1.c1ccc2ccccc2c1
c1ccc2ccccc2c1
c1ccc2ccccc2c1
null
[N+](=O)([O-])C1=CC=CC=C1
null
null
O=C1CCC(=O)O1.c1ccc2ccccc2c1>[N+](=O)([O-])C1=CC=CC=C1>O=C(O)CCC(=O)c1cccc2ccccc12
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-f007d2f3c0154a719f2dd1d49dbba9b3
NN.O=C(O)CCCC(=O)c1ccccc1>>O=c1cccc(-c2ccccc2)nn1
C(C1=CC=CC=C1)(=O)CCCC(=O)O.NN.O>>C1(=CC=CC=C1)C1=CC=CC(N=N1)=O
[NH2:13][NH2:14].O=[C:6]([CH2:5][CH2:4][CH2:3][C:2](O)=[O:1])[c:7]1[cH:8][cH:9][cH:10][cH:11][cH:12]1>>[O:1]=[c:2]1[cH:3][cH:4][cH:5][c:6](-[c:7]2[cH:8][cH:9][cH:10][cH:11][cH:12]2)[n:13][n:14]1
NN.O=C(O)CCCC(=O)c1ccccc1
O=c1cccc(-c2ccccc2)nn1
null
null
C1(=CC=CC=C1)C.CCOCC
Aromatic Heterocycle Formation
OtherReaction
a31553d36b14882561a6dcdd04ef456bc0e14ea189c472490f94f02ebbe3ca3f
eadf9e657b4bde18ed656e299092aac7dd81eee1face1030775c3edd6ccba31c
O=c1cccc(-c2ccccc2)nn1
O-[C;H0;D3;+0:1](=[O;D1;H0:2])-[CH2;D2;+0:3]-[CH2;D2;+0:4]-[CH2;D2;+0:5]-[C;H0;D3;+0:6](=O)-[c;H0;D3;+0:7](:[c:8]:[c:9]):[c:10]:[c:11].[NH2;D1;+0:12]-[NH2;D1;+0:13]>>[O;D1;H0:2]=[c;H0;D3;+0:1]1:[cH;D2;+0:3]:[cH;D2;+0:4]:[cH;D2;+0:5]:[c;H0;D3;+0:6](-[c;H0;D3;+0:7](:[c:8]:[c:9]):[c:10]:[c:11]):[n;H0;D2;+0:12]:[n;H0;D2;+0...
39
[{"value": 39.0, "product": "C1(=CC=CC=C1)C1=CC=CC(N=N1)=O", "details": "PERCENTYIELD", "is_desired": false}]
null
null
null
null
To a mixture of 10 g (0.052 mole) of 4-benzoylbutyric acid in 300 ml of toluene, hydrazine was added in one portion and the reaction was heated to reflux until all water had ceased to azeotrope. The reaction mixture was cooled and the toluene was stripped off in vacuo. The residue was dissolved in 200 ml Et2O and washe...
10.6084/m9.figshare.5104873.v1
null
Hydrazine.Carboxylic acid.Ketone
null
null
c1cccc[nH]n1
c1cccc[nH]n1.c1ccccc1
HO-
C1(=CC=CC=C1)C.CCOCC
null
null
NN.O=C(O)CCCC(=O)c1ccccc1>C1(=CC=CC=C1)C.CCOCC>O=c1cccc(-c2ccccc2)nn1
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-38cbb1529cc84ed082175760bc576022
COC(=O)OC.O=C1CCc2cc(Cl)ccc21>>COC(=O)C1Cc2cc(Cl)ccc2C1=O
COC(OC)=O.[H-].[Na+].ClC=1C=C2CCC(C2=CC1)=O.[H][H]>>C(=O)(OC)C1C(C2=CC=C(C=C2C1)Cl)=O
CO[C:3]([O:2][CH3:1])=[O:4].[CH2:5]1[CH2:6][c:7]2[cH:8][c:9]([Cl:10])[cH:11][cH:12][c:13]2[C:14]1=[O:15]>>[CH3:1][O:2][C:3](=[O:4])[CH:5]1[CH2:6][c:7]2[cH:8][c:9]([Cl:10])[cH:11][cH:12][c:13]2[C:14]1=[O:15]
COC(=O)OC.O=C1CCc2cc(Cl)ccc21
COC(=O)C1Cc2cc(Cl)ccc2C1=O
null
null
C(OC)COC
C-C Coupling
OtherReaction
c2c31337dfb867d8c28bc65df0ad4496f817a712a58e176523b47d7fdb6e4f91
d76b6fc9d01d8258e5777a3b2326a8d78a9d9a55717b27736ba55600205f4ed0
O=C1CCc2ccccc21
C-O-[C;H0;D3;+0:1](=[O;D1;H0:2])-[#8:3]-[C;D1;H3:4].[O;D1;H0:5]=[C:6]1-[CH2;D2;+0:7]-[C:8]-[c:9]:[c:10]-1>>[C;D1;H3:4]-[#8:3]-[C;H0;D3;+0:1](=[O;D1;H0:2])-[CH;D3;+0:7]1-[C:8]-[c:9]:[c:10]-[C:6]-1=[O;D1;H0:5]
45
[{"value": 45.0, "product": "C(=O)(OC)C1C(C2=CC=C(C=C2C1)Cl)=O", "details": "PERCENTYIELD", "is_desired": false}, {"value": 44.5, "product": "C(=O)(OC)C1C(C2=CC=C(C=C2C1)Cl)=O", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
60
CELSIUS
null
null
To a mixture of sodium hydride (2.4 g, 60% in mineral oil, 0.06 mole) and 50 ml dry dimethoxyethane, 5-chloroindanone (50 g, 0.03 mole) in 50 ml dimethoxyethane was added dropwise at room temperature. The mixture was stirred at room temperature until hydrogen evolution ceased. Then dimethylcarbonate (27 g, 0.3 mole) wa...
10.6084/m9.figshare.5104873.v1
null
Carbonic Ester.Ketone
Ketone.Ester
c1ccc2c(c1)CCC2
c1ccc2c(c1)CCC2
c1ccc2c(c1)CCC2
HO-
C(OC)COC
60
null
COC(=O)OC.O=C1CCc2cc(Cl)ccc21>C(OC)COC>COC(=O)C1Cc2cc(Cl)ccc2C1=O
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-247e413f02fe4dc189d56235735a1bdb
CN(C)C=O.O=C(O)Cc1ccc(Cl)cc1>>CN(C)C=C(C=O)c1ccc(Cl)cc1
C([O-])([O-])=O.[K+].[K+].P(=O)(Cl)(Cl)Cl.CN(C)C=O.ClC1=CC=C(C=C1)CC(=O)O>>ClC1=CC=C(C=C1)C(C=O)=CN(C)C
O=[CH:4][N:2]([CH3:1])[CH3:3].O=[C:6]([CH2:5][c:8]1[cH:9][cH:10][c:11]([Cl:12])[cH:13][cH:14]1)[OH:7]>>[CH3:1][N:2]([CH3:3])[CH:4]=[C:5]([CH:6]=[O:7])[c:8]1[cH:9][cH:10][c:11]([Cl:12])[cH:13][cH:14]1
CN(C)C=O.O=C(O)Cc1ccc(Cl)cc1
CN(C)C=C(C=O)c1ccc(Cl)cc1
null
null
C1(=CC=CC=C1)C
Acylation
OtherReaction
cbf378fe57a2b8d8304e623fb5ce9ee6fb9f6e90d9c6f965226d56b103180e6d
a9c635686380f13b6b5c45d80d4aef36b30fdab0aef140b81f04c277f7ba737d
c1ccccc1
O=[C;H0;D3;+0:1](-[OH;D1;+0:2])-[CH2;D2;+0:3]-[c:4](:[c:5]):[c:6].O=[CH;D2;+0:7]-[#7:8](-[C;D1;H3:9])-[C;D1;H3:10]>>[C;D1;H3:9]-[#7:8](-[C;D1;H3:10])-[CH;D2;+0:7]=[C;H0;D3;+0:3](-[CH;D2;+0:1]=[O;H0;D1;+0:2])-[c:4](:[c:5]):[c:6]
null
[]
null
null
8
HOUR
Phosphorus oxychloride (92 g) was added dropwise to stirred DMF (78 ml) between 10°-15° C. To the resulting slurry was added 4-chlorophenylacetic acid (34.12 g). The resulting mixture was stirred at room temperature for one half hour and then heated to 70°-80° C. during 5.5 hours, during which time the mixture became e...
10.6084/m9.figshare.5104873.v1
null
Carboxylic acid.Tertiary amide
Enamine.Aldehyde
null
null
c1ccccc1
HO-
C1(=CC=CC=C1)C
null
8
CN(C)C=O.O=C(O)Cc1ccc(Cl)cc1>C1(=CC=CC=C1)C>CN(C)C=C(C=O)c1ccc(Cl)cc1
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-506fcc7b31c241b1b92a78d6c6e2a5ef
CN(C)C=C(C=O)c1ccc(Cl)cc1.N#CCC(N)=O>>N#Cc1cc(-c2ccc(Cl)cc2)c[nH]c1=O
C(C)(=O)O.ClC1=CC=C(C=C1)C(C=O)=CN(C)C.C[O-].[Na+].C(#N)CC(=O)N>>C(#N)C=1C(NC=C(C1)C1=CC=C(C=C1)Cl)=O
CN(C)[CH:13]=[C:5]([CH:4]=O)[c:6]1[cH:7][cH:8][c:9]([Cl:10])[cH:11][cH:12]1.[N:1]#[C:2][CH2:3][C:15]([NH2:14])=[O:16]>>[N:1]#[C:2][c:3]1[cH:4][c:5](-[c:6]2[cH:7][cH:8][c:9]([Cl:10])[cH:11][cH:12]2)[cH:13][nH:14][c:15]1=[O:16]
CN(C)C=C(C=O)c1ccc(Cl)cc1.N#CCC(N)=O
N#Cc1cc(-c2ccc(Cl)cc2)c[nH]c1=O
null
null
CO.O
Aromatic Heterocycle Formation
OtherReaction
4fb69599b2ad512416349de44ee025f314a8ccdb2c8ad729cdf94ea75cf3109a
46cf335065eccd013987994a3f086665eb273ac87eb3153099a47e61dd329581
O=c1ccc(-c2ccccc2)c[nH]1
C-N(-C)-[CH;D2;+0:1]=[C;H0;D3;+0:2](-[CH;D2;+0:3]=O)-[c;H0;D3;+0:4](:[c:5]:[c:6]):[c:7]:[c:8].[N;D1;H0:9]#[C:10]-[CH2;D2;+0:11]-[C;H0;D3;+0:12](-[NH2;D1;+0:13])=[O;D1;H0:14]>>[N;D1;H0:9]#[C:10]-[c;H0;D3;+0:11]1:[cH;D2;+0:3]:[c;H0;D3;+0:2](-[c;H0;D3;+0:4](:[c:5]:[c:6]):[c:7]:[c:8]):[cH;D2;+0:1]:[nH;D2;+0:13]:[c;H0;D3;+0...
null
[]
null
null
null
null
To solution of sodium methoxide (7.52 g) in methanol (130 ml) was added cyanoacetamide (5.84 g) followed by 2-(4-chlorophenyl)-3-dimethylaminopropenal and the resulting suspension was refluxed overnight. During this time a yellow solid was formed. The mixture was cooled to room temperature and glacial acetic acid (50 m...
10.6084/m9.figshare.5104873.v1
null
Enamine.Aldehyde.Primary amide
null
null
c1cnccc1
c1cnccc1.c1ccccc1
HO-
CO.O
null
null
CN(C)C=C(C=O)c1ccc(Cl)cc1.N#CCC(N)=O>CO.O>N#Cc1cc(-c2ccc(Cl)cc2)c[nH]c1=O
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-1a4f37788b1a484282d9cf4c25552db7
N#Cc1cc(-c2ccc(Cl)cc2)c[nH]c1=O>>O=c1ccc(-c2ccc(Cl)cc2)c[nH]1
C(#N)C=1C(NC=C(C1)C1=CC=C(C=C1)Cl)=O>>ClC1=CC=C(C=C1)C=1C=CC(NC1)=O
N#C[c:3]1[c:2](=[O:1])[nH:14][cH:13][c:5](-[c:6]2[cH:7][cH:8][c:9]([Cl:10])[cH:11][cH:12]2)[cH:4]1>>[O:1]=[c:2]1[cH:3][cH:4][c:5](-[c:6]2[cH:7][cH:8][c:9]([Cl:10])[cH:11][cH:12]2)[cH:13][nH:14]1
N#Cc1cc(-c2ccc(Cl)cc2)c[nH]c1=O
O=c1ccc(-c2ccc(Cl)cc2)c[nH]1
null
null
OP(=O)(O)O
Miscellaneous
OtherReaction
145adc421652def73603eb299eace1e2e3a197522b719b6949c0145a4308d11b
4f08c5adfb6d80fba1093598fc51ce38f180c76537f67052d397b642cb6f3b89
O=c1ccc(-c2ccccc2)c[nH]1
N#C-[c;H0;D3;+0:1]1:[c:2]:[c:3]:[c:4]:[#7;a:5]:[c:6]:1=[O;D1;H0:7]>>[O;D1;H0:7]=[c:6]1:[#7;a:5]:[c:4]:[c:3]:[c:2]:[cH;D2;+0:1]:1
75.6
[{"value": 75.6, "product": "ClC1=CC=C(C=C1)C=1C=CC(NC1)=O", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
null
null
A mixture of 3-cyano-5-(4-chlorophenyl)-2-pyridinone (4.6 g) and 85% H3PO4 (60 ml) was heated at reflux for 16 hours. The resulting mixture was cooled to room temperature, poured into ice/water and filtered yielding 3.1 g of 5-(4-chlorophenyl)-2-pyridinone as a yellow solid. Conditions: See reaction.notes.procedure_det...
10.6084/m9.figshare.5104873.v1
null
Nitrile
null
c1cnccc1
c1cccnc1
c1cccnc1.c1ccccc1
Other
OP(=O)(O)O
null
null
N#Cc1cc(-c2ccc(Cl)cc2)c[nH]c1=O>OP(=O)(O)O>O=c1ccc(-c2ccc(Cl)cc2)c[nH]1
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-3aaa2f0964b0473a962a140eaa35f34c
CCC#CCBr.CCCCCC.O=c1cccc[nH]1.[Cl-]>>CCC#CCn1cc(-c2ccc(Cl)cc2)ccc1=O
[Cl-].[NH4+].[H-].[Na+].N1C(C=CC=C1)=O.CCCCCC.C(C)(=O)OCC.BrCC#CCC>>ClC1=CC=C(C=C1)C=1C=CC(N(C1)CC#CCC)=O
Br[CH2:5][C:4]#[C:3][CH2:2][CH3:1].[CH2:9]([CH3:10])[CH2:15][CH2:14][CH2:12][CH3:11].[nH:6]1[cH:7][cH:8][cH:16][cH:17][c:18]1=[O:19].[Cl-:13]>>[CH3:1][CH2:2][C:3]#[C:4][CH2:5][n:6]1[cH:7][c:8](-[c:9]2[cH:10][cH:11][c:12]([Cl:13])[cH:14][cH:15]2)[cH:16][cH:17][c:18]1=[O:19]
CCC#CCBr.CCCCCC.O=c1cccc[nH]1.[Cl-]
CCC#CCn1cc(-c2ccc(Cl)cc2)ccc1=O
null
null
CN(C)C=O
Aromatic Heterocycle Formation
OtherReaction
c16e53991381708a0d74f5092b5e25b0353184189763eaae006dd565c1174ab9
f1e2d48aa3857a2357f3a371c35806794fc7180cbbfa20a78f207e36837e33dc
O=c1ccc(-c2ccccc2)c[nH]1
Br-[CH2;D2;+0:1]-[C:2]#[C:3]-[C:4].[CH3;D1;+0:5]-[CH2;D2;+0:6]-[CH2;D2;+0:7]-[CH2;D2;+0:8]-[CH2;D2;+0:9]-[CH3;D1;+0:10].[Cl-;H0;D0:11].[O;D1;H0:12]=[c:13]1:[c:14]:[c:15]:[cH;D2;+0:16]:[c:17]:[nH;D2;+0:18]:1>>[C:4]-[C:3]#[C:2]-[CH2;D2;+0:1]-[n;H0;D3;+0:18]1:[c:17]:[c;H0;D3;+0:16](-[c;H0;D3;+0:6]2:[cH;D2;+0:5]:[cH;D2;+0:...
null
[]
0
CELSIUS
null
null
To a suspension of NaH (60% in mineral oil, 200 mg) in dry DMF (50 ml) at 0° C. was added the preceding pyridinone and the mixture was stirred at 0° C. for one half hour. To the resulting suspension was added 1-bromo-2-pentyne dropwise. The resulting mixture was kept at 0° C. during one half hour and poured into satura...
10.6084/m9.figshare.5104873.v1
null
Primary halide
Aromatic halide
c1ccccn1
c1ccncc1.c1ccccc1
c1ccncc1.c1ccccc1
HBr
CN(C)C=O
0
null
CCC#CCBr.CCCCCC.O=c1cccc[nH]1.[Cl-]>CN(C)C=O>CCC#CCn1cc(-c2ccc(Cl)cc2)ccc1=O
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-0ed0a908d15a48e6b829b90b094e3f19
Nc1ccc(Cl)cc1.O=C(Cl)C=Cc1ccccc1>>O=C(C=Cc1ccccc1)Nc1ccc(Cl)cc1
C(C)(=O)OCC.ClC1=CC=C(N)C=C1.N1=CC=CC=C1.C(C=CC1=CC=CC=C1)(=O)Cl>>ClC1=CC=C(C=C1)NC(C=CC1=CC=CC=C1)=O
[NH2:11][c:12]1[cH:13][cH:14][c:15]([Cl:16])[cH:17][cH:18]1.Cl[C:2](=[O:1])[CH:3]=[CH:4][c:5]1[cH:6][cH:7][cH:8][cH:9][cH:10]1>>[O:1]=[C:2]([CH:3]=[CH:4][c:5]1[cH:6][cH:7][cH:8][cH:9][cH:10]1)[NH:11][c:12]1[cH:13][cH:14][c:15]([Cl:16])[cH:17][cH:18]1
Nc1ccc(Cl)cc1.O=C(Cl)C=Cc1ccccc1
O=C(C=Cc1ccccc1)Nc1ccc(Cl)cc1
null
null
C1(=CC=CC=C1)C.O
Acylation
Acylation of Nitrogen Nucleophiles by Acyl/Thioacyl/Carbamoyl Halides and Analogs_OS
38143a4d536201990008fd6f2c68e6571a341d1c367481869fbbbe36cb038937
0e6ae078978e324f714e184b4f72826d4e3bf2d9ab22d6e9f73740af687be16f
O=C(C=Cc1ccccc1)Nc1ccccc1
Cl-[C;H0;D3;+0:1](=[O;D1;H0:2])-[C:3]=[C:4]-[c:5].[NH2;D1;+0:6]-[c:7](:[c:8]):[c:9]>>[O;D1;H0:2]=[C;H0;D3;+0:1](-[C:3]=[C:4]-[c:5])-[NH;D2;+0:6]-[c:7](:[c:8]):[c:9]
null
[]
0
CELSIUS
15
MINUTE
To a mixture of 4-chloroaniline (16.2 g), toluene (120 ml), and pyridine (11 ml) at 0° C., cinnamoyl chloride (20.0 g) in 120 ml of toluene was added dropwise. After stirring 15 minutes at 0° C. the reaction mixture was poured into a mixture of ethyl acetate: water (250 ml:250 ml). The organic layer was separated and e...
10.6084/m9.figshare.5104873.v1
null
Acyl halide.Primary amine
Secondary amide
null
null
c1ccccc1.c1ccccc1
HCl
C1(=CC=CC=C1)C.O
0
0.25
Nc1ccc(Cl)cc1.O=C(Cl)C=Cc1ccccc1>C1(=CC=CC=C1)C.O>O=C(C=Cc1ccccc1)Nc1ccc(Cl)cc1
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-326a0eacbf2f4832bc99567ea0fb9504
O=C(C=Cc1ccccc1)Nc1ccc(Cl)cc1>>O=c1ccc2c(Cl)cccc2[nH]1
ClC1=CC=C(C=C1)NC(C=CC1=CC=CC=C1)=O.[Cl-].[Al+3].[Cl-].[Cl-]>>ClC1=C2C=CC(NC2=CC=C1)=O
c1ccc([CH:4]=[CH:3][C:2](=[O:1])[NH:12][c:11]2[cH:5][cH:8][c:6]([Cl:7])[cH:9][cH:10]2)cc1>>[O:1]=[c:2]1[cH:3][cH:4][c:5]2[c:6]([Cl:7])[cH:8][cH:9][cH:10][c:11]2[nH:12]1
O=C(C=Cc1ccccc1)Nc1ccc(Cl)cc1
O=c1ccc2c(Cl)cccc2[nH]1
null
null
ClC1=CC=CC=C1
Reduction
OtherReaction
ebe7e954f82f1e726cf9b7a8863216fec31733c3d8bfbb1cc71c49312cec65ac
10d6d5b071f1d84b20b253ce9eadaed211c373c6ee607356078792f13319351a
O=c1ccc2ccccc2[nH]1
[Cl;D1;H0:1]-[c;H0;D3;+0:2]1:[cH;D2;+0:3]:[cH;D2;+0:4]:[c:5](-[NH;D2;+0:6]-[C;H0;D3;+0:7](=[O;D1;H0:8])-[CH;D2;+0:9]=[CH;D2;+0:10]-c2:c:c:c:c:c:2):[c:11]:[cH;D2;+0:12]:1>>[Cl;D1;H0:1]-[c;H0;D3;+0:2]1:[cH;D2;+0:3]:[cH;D2;+0:12]:[c:11]:[c:5]2:[nH;D2;+0:6]:[c;H0;D3;+0:7](=[O;D1;H0:8]):[cH;D2;+0:9]:[cH;D2;+0:10]:[c;H0;D3;+...
null
[]
125
CELSIUS
3
HOUR
To a mixture of N-(4-chlorophenyl)cinnamamide (8.3 g), and chlorobenzene (60 ml) was added portionwise aluminum chloride (21.4 g) under nitrogen at room temperature and the reaction mixture was slowly warmed up to 125° C. and kept at that temperature for 3 hours. The reaction mixture was cooled down and poured over 400...
10.6084/m9.figshare.5104873.v1
null
Aromatic halide.Secondary amide
Aromatic halide
c1ccccc1.c1ccccc1
c1ccc2ccccc2n1
c1ccc2ccccc2n1
Other
ClC1=CC=CC=C1
125
3
O=C(C=Cc1ccccc1)Nc1ccc(Cl)cc1>ClC1=CC=CC=C1>O=c1ccc2c(Cl)cccc2[nH]1
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-bb2d977cc5f147c5ab274afa7d1d2d39
CCC#CCBr.O=c1ccc2ccccc2[nH]1.[Cl-]>>CCC#CCn1c(=O)ccc2c(Cl)cccc21
[Cl-].[NH4+].N1C(C=CC2=CC=CC=C12)=O.[H-].[Na+].BrCC#CCC>>ClC1=C2C=CC(N(C2=CC=C1)CC#CCC)=O
Br[CH2:5][C:4]#[C:3][CH2:2][CH3:1].[nH:6]1[c:7](=[O:8])[cH:9][cH:10][c:11]2[cH:12][cH:14][cH:15][cH:16][c:17]12.[Cl-:13]>>[CH3:1][CH2:2][C:3]#[C:4][CH2:5][n:6]1[c:7](=[O:8])[cH:9][cH:10][c:11]2[c:12]([Cl:13])[cH:14][cH:15][cH:16][c:17]12
CCC#CCBr.O=c1ccc2ccccc2[nH]1.[Cl-]
CCC#CCn1c(=O)ccc2c(Cl)cccc21
null
null
CN(C)C=O.CCCCCC
Heteroatom Alkylation and Arylation
OtherReaction
a61336fe7a89ec0981a525297b55629e44e830f13f91df56a44bf01390d8c69d
dbda6588fa29cbbc0e3c3f601e69924b300990bdcc56b8cec0535d1258039346
O=c1ccc2ccccc2[nH]1
Br-[CH2;D2;+0:1]-[C:2]#[C:3]-[C:4].[Cl-;H0;D0:5].[O;D1;H0:6]=[c:7]1:[c:8]:[c:9]:[c:10]2:[cH;D2;+0:11]:[c:12]:[c:13]:[c:14]:[c:15]:2:[nH;D2;+0:16]:1>>[C:4]-[C:3]#[C:2]-[CH2;D2;+0:1]-[n;H0;D3;+0:16]1:[c:15]2:[c:14]:[c:13]:[c:12]:[c;H0;D3;+0:11](-[Cl;H0;D1;+0:5]):[c:10]:2:[c:9]:[c:8]:[c:7]:1=[O;D1;H0:6]
null
[]
0
CELSIUS
null
null
To a suspension of NaH (60% in mineral oil, 700 mg) in dry DMF (100 ml) at 0° C. was added the preceding quinolinone (2.05 g) and the mixture was stirred at 0° C. for one half hour. To the resulting suspension was added 1-bromo-2-pentyne (1.6 g) dropwise. The resulting mixture was kept at 0° C. for one half hour and po...
10.6084/m9.figshare.5104873.v1
null
Primary halide
Aromatic halide
c1ccc2ccccc2n1
c1ccc2ncccc2c1
c1ccc2ncccc2c1
HBr
CN(C)C=O.CCCCCC
0
null
CCC#CCBr.O=c1ccc2ccccc2[nH]1.[Cl-]>CN(C)C=O.CCCCCC>CCC#CCn1c(=O)ccc2c(Cl)cccc21
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-50a47b176604482395560ff8f1a4f880
CN(C)C=C(C=O)c1ccc(Cl)cc1.NC(N)=O>>O=c1ncc(-c2ccc(Cl)cc2)c[nH]1
[Cl-].[NH4+].ClC1=CC=C(C=C1)C(C=O)=CN(C)C.NC(=O)N.Cl>>ClC1=CC=C(C=C1)C=1C=NC(NC1)=O
CN(C)[CH:4]=[C:5]([c:6]1[cH:7][cH:8][c:9]([Cl:10])[cH:11][cH:12]1)[CH:13]=O.[O:1]=[C:2]([NH2:3])[NH2:14]>>[O:1]=[c:2]1[n:3][cH:4][c:5](-[c:6]2[cH:7][cH:8][c:9]([Cl:10])[cH:11][cH:12]2)[cH:13][nH:14]1
CN(C)C=C(C=O)c1ccc(Cl)cc1.NC(N)=O
O=c1ncc(-c2ccc(Cl)cc2)c[nH]1
null
null
C(C)O.O
Aromatic Heterocycle Formation
OtherReaction
0e1bb7c6fc2fa2fbd0239b648ae136ef123b13ddeb9947c50b8f38d453d7d183
55a949c5abf218b0e7fd0015b81e86fb975fa441e5ac6bd395c3346bb38599f7
O=c1ncc(-c2ccccc2)c[nH]1
C-N(-C)-[CH;D2;+0:1]=[C;H0;D3;+0:2](-[CH;D2;+0:3]=O)-[c;H0;D3;+0:4](:[c:5]:[c:6]):[c:7]:[c:8].[NH2;D1;+0:9]-[C;H0;D3;+0:10](-[NH2;D1;+0:11])=[O;D1;H0:12]>>[O;D1;H0:12]=[c;H0;D3;+0:10]1:[n;H0;D2;+0:11]:[cH;D2;+0:1]:[c;H0;D3;+0:2](-[c;H0;D3;+0:4](:[c:5]:[c:6]):[c:7]:[c:8]):[cH;D2;+0:3]:[nH;D2;+0:9]:1
29.7
[{"value": 29.7, "product": "ClC1=CC=C(C=C1)C=1C=NC(NC1)=O", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
null
null
A mixture of 2-(4-chlorophenyl)dimethylaminopropenal (Example 145a) (5.13 g), urea (2.4 g), concentrated HCl (10 ml), water (4 ml) and ethanol (150 ml) was refluxed for 4 hours. After cooling to room temperature concentrated ammonium chloride was added until the pH was 7. The resulting yellow solid was filtered off and...
10.6084/m9.figshare.5104873.v1
null
Enamine.Aldehyde.Urea
null
null
c1cncnc1
c1cncnc1.c1ccccc1
HO-
C(C)O.O
null
null
CN(C)C=C(C=O)c1ccc(Cl)cc1.NC(N)=O>C(C)O.O>O=c1ncc(-c2ccc(Cl)cc2)c[nH]1
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-4cc12f6af27449db870b9f2027866d61
CCC#CCBr.CCCCCC.O=c1cccc[nH]1.[Cl-].[NH4+]>>CCC#CCn1cc(-c2ccc(Cl)cc2)cnc1=O
[Cl-].[NH4+].CCCCCC.[H-].[Na+].N1C(C=CC=C1)=O.BrCC#CCC>>ClC1=CC=C(C=C1)C=1C=NC(N(C1)CC#CCC)=O
Br[CH2:5][C:4]#[C:3][CH2:2][CH3:1].C[CH2:15][CH2:14][CH2:12][CH2:11][CH3:10].[nH:6]1[cH:7][cH:8][cH:16][cH:9][c:18]1=[O:19].[Cl-:13].[NH4+:17]>>[CH3:1][CH2:2][C:3]#[C:4][CH2:5][n:6]1[cH:7][c:8](-[c:9]2[cH:10][cH:11][c:12]([Cl:13])[cH:14][cH:15]2)[cH:16][n:17][c:18]1=[O:19]
CCC#CCBr.CCCCCC.O=c1cccc[nH]1.[Cl-].[NH4+]
CCC#CCn1cc(-c2ccc(Cl)cc2)cnc1=O
null
null
CN(C)C=O
Aromatic Heterocycle Formation
OtherReaction
b4467fdd65493649554b053844b88f7aedac75ecb5e83a2819a9163270cc6b1f
f1e2d48aa3857a2357f3a371c35806794fc7180cbbfa20a78f207e36837e33dc
O=c1ncc(-c2ccccc2)c[nH]1
Br-[CH2;D2;+0:1]-[C:2]#[C:3]-[C:4].C-[CH2;D2;+0:5]-[CH2;D2;+0:6]-[CH2;D2;+0:7]-[CH2;D2;+0:8]-[CH3;D1;+0:9].[Cl-;H0;D0:10].[NH4+;D0:11].[O;D1;H0:12]=[c;H0;D3;+0:13]1:[cH;D2;+0:14]:[cH;D2;+0:15]:[cH;D2;+0:16]:[c:17]:[nH;D2;+0:18]:1>>[C:4]-[C:3]#[C:2]-[CH2;D2;+0:1]-[n;H0;D3;+0:18]1:[c:17]:[c;H0;D3;+0:16](-[c;H0;D3;+0:14]2...
null
[]
0
CELSIUS
null
null
To a suspension of NaH (60% in mineral oil, 340 mg) in dry DMF (75 ml) at 0° C. was added the preceding pyridinone (1.0 g) and the mixture was stirred at 0° C. for one half hour. To the resulting suspension was added 1-bromo-2-pentyne (750 mg) dropwise. The resulting mixture was kept at 0° C. for one half hour and pour...
10.6084/m9.figshare.5104873.v1
null
Primary halide
Aromatic halide
c1ccccn1
c1cncnc1.c1ccccc1
c1cncnc1.c1ccccc1
HBr
CN(C)C=O
0
null
CCC#CCBr.CCCCCC.O=c1cccc[nH]1.[Cl-].[NH4+]>CN(C)C=O>CCC#CCn1cc(-c2ccc(Cl)cc2)cnc1=O
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-e530c7df16024f4aae4797b4613d3ced
O=c1ccc(-c2ccc(Cl)cc2)n[nH]1.S=P12SP3(=S)SP(=S)(S1)SP(=S)(S2)S3>>S=c1ccc(-c2ccc(Cl)cc2)n[nH]1
ClC1=CC=C(C=C1)C=1C=CC(NN1)=O.P12(=S)SP3(=S)SP(=S)(S1)SP(=S)(S2)S3>>ClC1=CC=C(C=C1)C=1C=CC(NN1)=S
O=[c:2]1[cH:3][cH:4][c:5](-[c:6]2[cH:7][cH:8][c:9]([Cl:10])[cH:11][cH:12]2)[n:13][nH:14]1.S=P12SP3(=S)SP(=S)(S1)SP(=[S:1])(S2)S3>>[S:1]=[c:2]1[cH:3][cH:4][c:5](-[c:6]2[cH:7][cH:8][c:9]([Cl:10])[cH:11][cH:12]2)[n:13][nH:14]1
O=c1ccc(-c2ccc(Cl)cc2)n[nH]1.S=P12SP3(=S)SP(=S)(S1)SP(=S)(S2)S3
S=c1ccc(-c2ccc(Cl)cc2)n[nH]1
null
null
N1=CC=CC=C1
Heteroatom Alkylation and Arylation
OtherReaction
e0da8be0c0e31372bc487fca4d998b8539b7ff5b84df07e1a6200efd3593e0bb
13be3f637e1e22872d741944f46b7fcc1954fe982a3a8a0f7825545d455ab147
S=c1ccc(-c2ccccc2)n[nH]1
O=[c;H0;D3;+0:1]1:[#7;a:2]:[#7;a:3]:[c:4]:[c:5]:[c:6]:1.S=P12-S-P3(=S)-S-P(=S)(-S-1)-S-P(=[S;H0;D1;+0:7])(-S-2)-S-3>>[S;H0;D1;+0:7]=[c;H0;D3;+0:1]1:[#7;a:2]:[#7;a:3]:[c:4]:[c:5]:[c:6]:1
187.1
[{"value": 187.1, "product": "ClC1=CC=C(C=C1)C=1C=CC(NN1)=S", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
null
null
A mixture of 3.0 g of 6-(4-chlorophenyl)-pyridazinone, 50 ml of dry pyridine and 3.2 g of phosphorus pentasulfide was refluxed for 1 hour, evaporated to dryness and extracted with 200 ml of ether. The ether extract was washed with water (3×100 ml), brine (100 ml), dried over magnesium sulfate and evaporated to yield 3....
10.6084/m9.figshare.5104873.v1
null
Monosulfide.Monosulfide.Monosulfide.Monosulfide.Monosulfide.Monosulfide
Thiocarbonyl
c1cccnn1.S1P2SP3SP1SP(S2)S3
c1cccnn1
c1cccnn1.c1ccccc1
Other
N1=CC=CC=C1
null
null
O=c1ccc(-c2ccc(Cl)cc2)n[nH]1.S=P12SP3(=S)SP(=S)(S1)SP(=S)(S2)S3>N1=CC=CC=C1>S=c1ccc(-c2ccc(Cl)cc2)n[nH]1
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-7d8de4f9f5ac412ebeca703ef49f3390
NNC(=O)c1ccc(Cl)cc1.O=C(Cl)CCl>>O=C(CCl)NNC(=O)c1ccc(Cl)cc1
ClC1=CC=C(C(=O)NN)C=C1.ClCC(=O)Cl>>ClCC(=O)NNC(C1=CC=C(C=C1)Cl)=O
[NH2:5][NH:6][C:7](=[O:8])[c:9]1[cH:10][cH:11][c:12]([Cl:13])[cH:14][cH:15]1.Cl[C:2](=[O:1])[CH2:3][Cl:4]>>[O:1]=[C:2]([CH2:3][Cl:4])[NH:5][NH:6][C:7](=[O:8])[c:9]1[cH:10][cH:11][c:12]([Cl:13])[cH:14][cH:15]1
NNC(=O)c1ccc(Cl)cc1.O=C(Cl)CCl
O=C(CCl)NNC(=O)c1ccc(Cl)cc1
null
null
O1CCOCC1
Acylation
Acylation of Nitrogen Nucleophiles by Acyl/Thioacyl/Carbamoyl Halides and Analogs_OS
e9c0e57fff756e07b8f823de2eed1eeaae995a83400f2b5e18582349988c9a5f
384006bf8ba751654aef497f42d95dd6fc64342c355d6ce7d0ea9a3aaffeacc6
c1ccccc1
Cl-[C;H0;D3;+0:1](=[O;D1;H0:2])-[C:3]-[Cl;D1;H0:4].[NH2;D1;+0:5]-[#7:6]-[C:7](=[O;D1;H0:8])-[c:9]>>[Cl;D1;H0:4]-[C:3]-[C;H0;D3;+0:1](=[O;D1;H0:2])-[NH;D2;+0:5]-[#7:6]-[C:7](=[O;D1;H0:8])-[c:9]
null
[]
null
null
null
null
To a solution of p-chlorobenzoic hydrazide (11.2 g) in dioxane (100 ml) was added chloroacetyl chloride (6 ml). The resulting mixture was refluxed for three hours, cooled to room temperature and filtered. The resulting solid was washed with ethyl ether and dried to yield N'-chloroacetyl-4-chlorobenzoic hydrazide as whi...
10.6084/m9.figshare.5104873.v1
null
Acyl halide.Acylhydrazine
Acylhydrazine.Acylhydrazine
null
null
c1ccccc1
HCl
O1CCOCC1
null
null
NNC(=O)c1ccc(Cl)cc1.O=C(Cl)CCl>O1CCOCC1>O=C(CCl)NNC(=O)c1ccc(Cl)cc1
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-10c1b8c1d0dd44818ead6ca91a1dbfb1
COC(=S)NN.O=C(CBr)c1ccc(Cl)cc1>>O=C1NN=C(c2ccc(Cl)cc2)CS1
BrCC(=O)C1=CC=C(C=C1)Cl.COC(=S)NN>>ClC1=CC=C(C=C1)C1=NNC(SC1)=O
C[O:1][C:2]([NH:3][NH2:4])=[S:14].O=[C:5]([c:6]1[cH:7][cH:8][c:9]([Cl:10])[cH:11][cH:12]1)[CH2:13]Br>>[O:1]=[C:2]1[NH:3][N:4]=[C:5]([c:6]2[cH:7][cH:8][c:9]([Cl:10])[cH:11][cH:12]2)[CH2:13][S:14]1
COC(=S)NN.O=C(CBr)c1ccc(Cl)cc1
O=C1NN=C(c2ccc(Cl)cc2)CS1
null
null
C(C)#N
Acylation
OtherReaction
a0815ff887854434f061e02bb59e65917f2f792eefe3f407e6f67a241e834044
b7ddc8c969600ae9a9b2d12841c66a24307741bcbfc0810c56e58eb7d0e4892d
O=C1NN=C(c2ccccc2)CS1
Br-[CH2;D2;+0:1]-[C;H0;D3;+0:2](=O)-[c:3](:[c:4]):[c:5].C-[O;H0;D2;+0:6]-[C;H0;D3;+0:7](=[S;H0;D1;+0:8])-[#7:9]-[NH2;D1;+0:10]>>[O;H0;D1;+0:6]=[C;H0;D3;+0:7]1-[#7:9]-[N;H0;D2;+0:10]=[C;H0;D3;+0:2](-[c:3](:[c:4]):[c:5])-[CH2;D2;+0:1]-[S;H0;D2;+0:8]-1
48.4
[{"value": 48.4, "product": "ClC1=CC=C(C=C1)C1=NNC(SC1)=O", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
null
null
A mixture of 2-bromo-p-chloroacetophenone (9.16 g), methoxythiocarbonylhydrazine (13.0 g) and acetonitrile (75 ml) was refluxed overnight and then cooled and filtered. The light yellow solid was washed with hexane and dried yielding 5-(4-chlorophenyl)-3H,6H-1,3,4-thiadiazin-2-one (4.3 g). Conditions: See reaction.notes...
10.6084/m9.figshare.5104873.v1
null
Hydrazine.Primary halide.Ketone.Ether.Thioamide
Hydrazone amide.Monosulfide
null
C1=NNCSC1
C1=NNCSC1.c1ccccc1
HBr
C(C)#N
null
null
COC(=S)NN.O=C(CBr)c1ccc(Cl)cc1>C(C)#N>O=C1NN=C(c2ccc(Cl)cc2)CS1
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-93c4153772314fe5b6357b0fc7b230aa
O=C(O)CCC(=O)c1cccc(Cl)c1>>O=C(O)CCCc1cccc(Cl)c1
ClC=1C=C(C(=O)CCC(=O)O)C=CC1.[OH-].[K+].NN>>ClC=1C=C(C=CC1)CCCC(=O)O
O=[C:6]([CH2:5][CH2:4][C:2](=[O:1])[OH:3])[c:7]1[cH:8][cH:9][cH:10][c:11]([Cl:12])[cH:13]1>>[O:1]=[C:2]([OH:3])[CH2:4][CH2:5][CH2:6][c:7]1[cH:8][cH:9][cH:10][c:11]([Cl:12])[cH:13]1
O=C(O)CCC(=O)c1cccc(Cl)c1
O=C(O)CCCc1cccc(Cl)c1
null
null
C(COCCO)O
Reduction
OtherReaction
bdac4f77103f4da1c5b42ea95e05b0b7b31176b78204db5f4144ffca7b3d54d5
f9ba67182f94acd5fbe41487f8f71e26bccf898b8fc8091ef46f4363de5628d4
c1ccccc1
O=[C;H0;D3;+0:1](-[C:2]-[C:3]-[C:4](=[O;D1;H0:5])-[O;D1;H1:6])-[c:7](:[c:8]):[c:9]>>[O;D1;H0:5]=[C:4](-[O;D1;H1:6])-[C:3]-[C:2]-[CH2;D2;+0:1]-[c:7](:[c:8]):[c:9]
90.8
[{"value": 90.8, "product": "ClC=1C=C(C=CC1)CCCC(=O)O", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
null
null
To a 300 ml round-bottomed flask equipped with magnetic stirrer and reflux condenser was charged 23.7 g of 87% potassium hydroxide and 150 ml of diethyleneglycol, With stirring, 23 g of 3-(3-chlorobenzoyl)propionic acid was added followed by 24 g of 85% hydrazine. The mixture was heated to reflux for 2 hours when 50 ml...
10.6084/m9.figshare.5104873.v1
null
Ketone
null
null
null
c1ccccc1
Other
C(COCCO)O
null
null
O=C(O)CCC(=O)c1cccc(Cl)c1>C(COCCO)O>O=C(O)CCCc1cccc(Cl)c1
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-b13d649eb0e543419a54c9aec5175c91
CNN.O=C(O)CCC(=O)c1ccc(Cl)cc1>>CN1N=C(c2ccc(Cl)cc2)CCC1=O
ClC1=CC=C(C(=O)CCC(=O)O)C=C1.CNN>>ClC1=CC=C(C=C1)C=1CCC(N(N1)C)=O
[CH3:1][NH:2][NH2:3].O=[C:4]([c:5]1[cH:6][cH:7][c:8]([Cl:9])[cH:10][cH:11]1)[CH2:12][CH2:13][C:14](O)=[O:15]>>[CH3:1][N:2]1[N:3]=[C:4]([c:5]2[cH:6][cH:7][c:8]([Cl:9])[cH:10][cH:11]2)[CH2:12][CH2:13][C:14]1=[O:15]
CNN.O=C(O)CCC(=O)c1ccc(Cl)cc1
CN1N=C(c2ccc(Cl)cc2)CCC1=O
null
null
C(C)O
Acylation
OtherReaction
4e477d09c29dc9649665c2a512a7ab66ed0db9837b745e511eba3c76a3cc18d7
30de68c4dde17a0553a43eee47b1b865b8390bb08557512a59e6e71e0ed0ad51
O=C1CCC(c2ccccc2)=NN1
O-[C;H0;D3;+0:1](=[O;D1;H0:2])-[C:3]-[C:4]-[C;H0;D3;+0:5](=O)-[c:6](:[c:7]):[c:8].[C;D1;H3:9]-[NH;D2;+0:10]-[NH2;D1;+0:11]>>[C;D1;H3:9]-[N;H0;D3;+0:10]1-[N;H0;D2;+0:11]=[C;H0;D3;+0:5](-[c:6](:[c:7]):[c:8])-[C:4]-[C:3]-[C;H0;D3;+0:1]-1=[O;D1;H0:2]
null
[]
null
null
null
null
To a 250 ml flask equipped with magnetic stirrer and reflux condenser was charged 10 g of 3-(4-chlorobenzoyl)-propionic acid, 250 ml. of absolute ethanol, and 2.5 ml of methyl hydrazine. The reaction was refluxed for 3 hours and cooled to yield a solid which was collected by vacuum filtration, washed with 50 ml of hexa...
10.6084/m9.figshare.5104873.v1
null
Hydrazine.Carboxylic acid.Ketone
Hydrazone amide
null
C1=N[NH]CCC1
C1=N[NH]CCC1.c1ccccc1
HO-
C(C)O
null
null
CNN.O=C(O)CCC(=O)c1ccc(Cl)cc1>C(C)O>CN1N=C(c2ccc(Cl)cc2)CCC1=O
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-71f9c60234da4ab48aa5084c5a174dbb
CC(=O)CCC(=O)O.O=Cc1ccc(Cl)cc1>>O=C(O)CCC(=O)C=Cc1ccc(Cl)cc1
ClC1=CC=C(C=O)C=C1.C(CCC(=O)C)(=O)O.N1CCCCC1.C1(=CC=CC=C1)C>>ClC1=CC=C(C=CC(=O)CCC(=O)O)C=C1
[O:1]=[C:2]([OH:3])[CH2:4][CH2:5][C:6](=[O:7])[CH3:8].O=[CH:9][c:10]1[cH:11][cH:12][c:13]([Cl:14])[cH:15][cH:16]1>>[O:1]=[C:2]([OH:3])[CH2:4][CH2:5][C:6](=[O:7])[CH:8]=[CH:9][c:10]1[cH:11][cH:12][c:13]([Cl:14])[cH:15][cH:16]1
CC(=O)CCC(=O)O.O=Cc1ccc(Cl)cc1
O=C(O)CCC(=O)C=Cc1ccc(Cl)cc1
null
null
O
C-C Coupling
Aldehyde and ketone to alpha,beta-unsaturated carbonyl
df1bdbab1a06af9561d74fe6bc94ee8bda1d14faad9db1ada3a214bd64a24cf8
c93e93ada40f7f922a54fe24d38f540ecf5ff25d55d497f79f5f400f75d0c7ae
c1ccccc1
O=[CH;D2;+0:1]-[c:2](:[c:3]):[c:4].[C:5]-[C:6](-[CH3;D1;+0:7])=[O;D1;H0:8]>>[C:5]-[C:6](=[O;D1;H0:8])-[CH;D2;+0:7]=[CH;D2;+0:1]-[c:2](:[c:3]):[c:4]
44
[{"value": 44.0, "product": "ClC1=CC=C(C=CC(=O)CCC(=O)O)C=C1", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
null
null
To a dry 250 ml flask equipped with a magnetic stirrer, Dean-Stark trap, and reflux condenser was charged 15 g of 4-chlorobenzaldehyde, 12.4 g levulenic acid, 5.7 ml of piperidine, and 100 ml of toluene. The reaction was refluxed for 3 hours, after which no water was observed to azeotrope from the solution. The reactio...
10.6084/m9.figshare.5104873.v1
null
Aldehyde.Ketone
Ketone
null
null
c1ccccc1
HO-
O
null
null
CC(=O)CCC(=O)O.O=Cc1ccc(Cl)cc1>O>O=C(O)CCC(=O)C=Cc1ccc(Cl)cc1
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-7eeb6357d2624e32bcc06f1bb1a4e975
COc1ccc(C(=O)[O-])c(C)c1[N+](=O)[O-]>>COc1ccc(C(=O)O)cc1[N+](=O)[O-]
[N+](=O)([O-])C=1C(=C(C(=O)[O-])C=CC1OC)C.[OH-].[K+]>>[N+](=O)([O-])C=1C=C(C(=O)O)C=CC1OC
C[c:10]1[c:6]([C:7](=[O:8])[O-:9])[cH:5][cH:4][c:3]([O:2][CH3:1])[c:11]1[N+:12](=[O:13])[O-:14]>>[CH3:1][O:2][c:3]1[cH:4][cH:5][c:6]([C:7](=[O:8])[OH:9])[cH:10][c:11]1[N+:12](=[O:13])[O-:14]
COc1ccc(C(=O)[O-])c(C)c1[N+](=O)[O-]
COc1ccc(C(=O)O)cc1[N+](=O)[O-]
null
null
O1CCCC1
Miscellaneous
OtherReaction
ec2bcf645eed3485ae21dd491bac7887e7ecc8e6727067de36c08c87eaa3e98c
d003579d88c8e6390ed4fac608b8ce68d334559ff02e2f3d9c9936750b60a874
c1ccccc1
C-[c;H0;D3;+0:1](:[c:2](-[#7;+:3]):[c:4]):[c:5](-[C:6](-[O-;H0;D1:7])=[O;D1;H0:8]):[c:9]>>[#7;+:3]-[c:2](:[c:4]):[cH;D2;+0:1]:[c:5](-[C:6](=[O;D1;H0:8])-[OH;D1;+0:7]):[c:9]
76.6
[{"value": 76.6, "product": "[N+](=O)([O-])C=1C=C(C(=O)O)C=CC1OC", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
12
HOUR
To a 500 ml erlenmeyer flask with magnetic stirrer was charged 10.3 g of 3-nitro-4-methoxy-methylbenzoate, 400 ml tetrahydrofuran, and 3.2 g of 86% potassium hydroxide. The reaction was stirred for 12 hours at ambient temperature, after which the resulting solid was collected by vacuum filtration and washed with 2×100 ...
10.6084/m9.figshare.5104873.v1
null
null
Carboxylic acid
c1ccccc1
c1ccccc1
c1ccccc1
Other
O1CCCC1
null
12
COc1ccc(C(=O)[O-])c(C)c1[N+](=O)[O-]>O1CCCC1>COc1ccc(C(=O)O)cc1[N+](=O)[O-]
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-eff2bc0de6514ad8b023fb68fc66d9c2
CC(C)(C)OC(=O)N[C@H](Cc1ccccc1)C(=O)N1CCC[C@H]1C(=O)OCc1ccccc1>>N[C@H](Cc1ccccc1)C(=O)N1CCC[C@H]1C(=O)OCc1ccccc1
FC(C(=O)O)(F)F.N([C@H](CC1=CC=CC=C1)C(=O)N1[C@H](C(=O)OCC2=CC=CC=C2)CCC1)C(=O)OC(C)(C)C.C1(=CC=CC=C1)OC>>N[C@H](CC1=CC=CC=C1)C(=O)N1[C@H](C(=O)OCC2=CC=CC=C2)CCC1.FC(F)(F)C(=O)O
CC(C)(C)OC(=O)[NH:1][C@H:2]([CH2:3][c:4]1[cH:5][cH:6][cH:7][cH:8][cH:9]1)[C:10](=[O:11])[N:12]1[CH2:13][CH2:14][CH2:15][C@H:16]1[C:17](=[O:18])[O:19][CH2:20][c:21]1[cH:22][cH:23][cH:24][cH:25][cH:26]1>>[NH2:1][C@H:2]([CH2:3][c:4]1[cH:5][cH:6][cH:7][cH:8][cH:9]1)[C:10](=[O:11])[N:12]1[CH2:13][CH2:14][CH2:15][C@H:16]1[C:...
CC(C)(C)OC(=O)N[C@H](Cc1ccccc1)C(=O)N1CCC[C@H]1C(=O)OCc1ccccc1
N[C@H](Cc1ccccc1)C(=O)N1CCC[C@H]1C(=O)OCc1ccccc1
null
null
ClCCl
Reduction
Hydrogenolysis of amides/imides/carbamates
3c33dd2a2d355ee5ba0287367e209aa147a39aa00607f0c95fb2bf1ade45d014
c5b5dffe7dd8beebdc1baa8b5b05300a9f7079e65dcfd42ade6f8a77ff09537d
O=C(OCc1ccccc1)[C@@H]1CCCN1C(=O)CCc1ccccc1
C-C(-C)(-C)-O-C(=O)-[NH;D2;+0:1]-[C:2](-[C:3])-[C:4](=[O;D1;H0:5])-[#7:6](-[C:7])-[C:8]-[C:9](-[#8:10])=[O;D1;H0:11]>>[#8:10]-[C:9](=[O;D1;H0:11])-[C:8]-[#7:6](-[C:4](=[O;D1;H0:5])-[C:2](-[C:3])-[NH2;D1;+0:1])-[C:7]
85
[{"value": 85.0, "product": "N[C@H](CC1=CC=CC=C1)C(=O)N1[C@H](C(=O)OCC2=CC=CC=C2)CCC1.FC(F)(F)C(=O)O", "details": "PERCENTYIELD", "is_desired": false}]
null
null
3
HOUR
To a stirring solution of Boc-D-Phe-Pro-OBn (68 g, 150 mmol) in dichloromethane (50 mL) at 0° C., was added anisole (20 mL) followed by trifluoroacetic acid (400 mL). After stirring for 3 hours, the solvents were evaporated in vacuo and the thick oily residue was dissolved in diethyl ether (1.5 L) and refrigerated (72 ...
10.6084/m9.figshare.5104873.v1
null
Carbamic ester.Ether.Boc
Primary amine
null
null
c1ccccc1.C1CC[NH]C1.c1ccccc1
HO-
ClCCl
null
3
CC(C)(C)OC(=O)N[C@H](Cc1ccccc1)C(=O)N1CCC[C@H]1C(=O)OCc1ccccc1>ClCCl>N[C@H](Cc1ccccc1)C(=O)N1CCC[C@H]1C(=O)OCc1ccccc1
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-75f289d130c7444bbf7348c68b3481f5
O=C(O)[C@@H]1CCCN1.O=C(O)[C@H]1CCCCN1C(=O)OCc1ccccc1>>O=C(O)[C@@H]1CCCN1C(=O)[C@H]1CCCCN1C(=O)OCc1ccccc1
N1([C@@H](C(=O)O)CCCC1)C(=O)OCC1=CC=CC=C1.ClC1=C(C=C(C(=C1)Cl)Cl)O.N1[C@H](C(=O)O)CCC1.C(C)N(CC)CC.C1(CCCCC1)N=C=NC1CCCCC1>>N1([C@@H](C(=O)N2[C@H](C(=O)O)CCC2)CCCC1)C(=O)OCC1=CC=CC=C1
[O:1]=[C:2]([OH:3])[C@@H:4]1[CH2:5][CH2:6][CH2:7][NH:8]1.O[C:9](=[O:10])[C@H:11]1[CH2:12][CH2:13][CH2:14][CH2:15][N:16]1[C:17](=[O:18])[O:19][CH2:20][c:21]1[cH:22][cH:23][cH:24][cH:25][cH:26]1>>[O:1]=[C:2]([OH:3])[C@@H:4]1[CH2:5][CH2:6][CH2:7][N:8]1[C:9](=[O:10])[C@H:11]1[CH2:12][CH2:13][CH2:14][CH2:15][N:16]1[C:17](=[...
O=C(O)[C@@H]1CCCN1.O=C(O)[C@H]1CCCCN1C(=O)OCc1ccccc1
O=C(O)[C@@H]1CCCN1C(=O)[C@H]1CCCCN1C(=O)OCc1ccccc1
null
null
C(C)(=O)OCC
Acylation
Acylation of Nitrogen Nucleophiles by Carboxylic Acids
a590d96426a2fbaed42913d9daf8a16471a16de4978200f1d35a30a10009ebe7
c5e4172490b2731ba9322b68af56376edadc31ce0bb9a3dfdea23a1817a852fd
O=C([C@H]1CCCCN1C(=O)OCc1ccccc1)N1CCCC1
O-[C;H0;D3;+0:1](=[O;D1;H0:2])-[C:3](-[C:4])-[#7:5](-[C:6](-[#8:7])=[O;D1;H0:8])-[C:9].[O;D1;H0:10]=[C:11](-[O;D1;H1:12])-[C:13]1-[C:14]-[C:15]-[C:16]-[NH;D2;+0:17]-1>>[#8:7]-[C:6](=[O;D1;H0:8])-[#7:5](-[C:9])-[C:3](-[C;H0;D3;+0:1](=[O;D1;H0:2])-[N;H0;D3;+0:17]1-[C:16]-[C:15]-[C:14]-[C:13]-1-[C:11](=[O;D1;H0:10])-[O;D1...
null
[]
0
CELSIUS
1
HOUR
Cbz-D-hPro-OH (9.5 g, 36 mmol) was dissolved in ethyl acetate (100 mL) and the solution cooled to 0° C. Added to the solution was 2,4,5-trichlorophenol (7.1 g, 36 mmol) and 1,3-dicyclohexylcarbodiimide (7.4 g, 36 mmol). The reaction was stirred for 1 hour at 0° C. and 1 hour at room temperature. The precipitate was fil...
10.6084/m9.figshare.5104873.v1
null
Carboxylic acid.Secondary amine
Tertiary amide
C1CCNC1
C1CC[NH]C1
C1CC[NH]C1.C1CC[NH]CC1.c1ccccc1
HO-
C(C)(=O)OCC
0
1
O=C(O)[C@@H]1CCCN1.O=C(O)[C@H]1CCCCN1C(=O)OCc1ccccc1>C(C)(=O)OCC>O=C(O)[C@@H]1CCCN1C(=O)[C@H]1CCCCN1C(=O)OCc1ccccc1
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-e27f2076ea2944b58cddfe057fe8345b
O=C(O)c1nccc2ccccc12>>O=C(O)C1NCCC2CCCCC21
C1(=NC=CC2=CC=CC=C12)C(=O)O.[H][H]>>C1(NCCC2CCCCC12)C(=O)O
[O:1]=[C:2]([OH:3])[c:4]1[n:5][cH:6][cH:7][c:8]2[cH:9][cH:10][cH:11][cH:12][c:13]12>>[O:1]=[C:2]([OH:3])[CH:4]1[NH:5][CH2:6][CH2:7][CH:8]2[CH2:9][CH2:10][CH2:11][CH2:12][CH:13]12
O=C(O)c1nccc2ccccc12
O=C(O)C1NCCC2CCCCC21
null
[Rh]
Cl.CCO
Reduction
OtherReaction
9d4ceb2330349e47c2f1e6d3fa94e6f87fe5387baf3dc326c222e39cbecb1d6e
2b7f370a519e29b4dede190aa36b37f30822496e32f2c8bfa9736e631bde52e2
C1CCC2CNCCC2C1
[O;D1;H0:1]=[C:2](-[O;D1;H1:3])-[c;H0;D3;+0:4]1:[n;H0;D2;+0:5]:[cH;D2;+0:6]:[cH;D2;+0:7]:[c;H0;D3;+0:8]2:[cH;D2;+0:9]:[cH;D2;+0:10]:[cH;D2;+0:11]:[cH;D2;+0:12]:[c;H0;D3;+0:13]:1:2>>[O;D1;H0:1]=[C:2](-[O;D1;H1:3])-[CH;D3;+0:4]1-[NH;D2;+0:5]-[CH2;D2;+0:6]-[CH2;D2;+0:7]-[CH;D3;+0:8]2-[CH2;D2;+0:9]-[CH2;D2;+0:10]-[CH2;D2;+...
56.8
[{"value": 48.0, "product": "C1(NCCC2CCCCC12)C(=O)O", "details": "PERCENTYIELD", "is_desired": false}, {"value": 56.8, "product": "C1(NCCC2CCCCC12)C(=O)O", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
null
null
A solution of 1-isoquinolinecarboxylic acid (50 g, 0.288 mol) in EtOH (150 mL) and 60 mL of 5N HCl was reduced over 5% Rh/Al2O3 (14 g) at 52 bar (750 psi) of hydrogen in a high pressure apparatus at 50° C. for 17 hours. The reaction mixture was filtered through a pad of diatomaceous earth, and the filtrate was concentr...
10.6084/m9.figshare.5104873.v1
null
null
Secondary amine
c1ccc2cnccc2c1
C1CCC2CNCCC2C1
C1CCC2CNCCC2C1
null
[Rh].Cl.CCO
null
null
O=C(O)c1nccc2ccccc12>[Rh].Cl.CCO>O=C(O)C1NCCC2CCCCC21
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-d52eb0d907f4438189c898a207603691
CCO.O=C(O)[C@@H]1Cc2ccccc2N1>>CCOC(=O)[C@@H]1Cc2ccccc2N1
Cl.N1[C@@H](CC2=CC=CC=C12)C(=O)O.C(C)O>>C(C)OC(=O)[C@H]1NC2=CC=CC=C2C1
[CH3:1][CH2:2][OH:3].O[C:4](=[O:5])[C@@H:6]1[CH2:7][c:8]2[cH:9][cH:10][cH:11][cH:12][c:13]2[NH:14]1>>[CH3:1][CH2:2][O:3][C:4](=[O:5])[C@@H:6]1[CH2:7][c:8]2[cH:9][cH:10][cH:11][cH:12][c:13]2[NH:14]1
CCO.O=C(O)[C@@H]1Cc2ccccc2N1
CCOC(=O)[C@@H]1Cc2ccccc2N1
null
null
null
Protection
Esterification of Carboxylic Acids
070670f68a20c1021da94fabee54def4688122fb721af5f52cd5a03630845d0e
0d8a72b7375d91aa7263e766e03a3cb7c4fa91e27abcd590409ff03b98eed690
c1ccc2c(c1)CCN2
O-[C;H0;D3;+0:1](=[O;D1;H0:2])-[C:3](-[C:4])-[#7:5]-[c:6].[C;D1;H3:7]-[C:8]-[OH;D1;+0:9]>>[C:4]-[C:3](-[C;H0;D3;+0:1](=[O;D1;H0:2])-[O;H0;D2;+0:9]-[C:8]-[C;D1;H3:7])-[#7:5]-[c:6]
null
[]
null
null
16
HOUR
HCl gas was bubbled through a stirring suspension of (S)-indoline-2-carboxylic acid (20 g, 110 mmol) in ethanol (500 mL). When the acid was completely dissolved, the solution was brought to reflux. After 16 hours, the solution was cooled and the solvent removed in vacuo. The residue was triturated with diethyl ether an...
10.6084/m9.figshare.5104873.v1
null
Carboxylic acid.Primary alcohol
Ester
null
null
c1ccc2c(c1)CCN2
HO-
null
null
16
CCO.O=C(O)[C@@H]1Cc2ccccc2N1>>CCOC(=O)[C@@H]1Cc2ccccc2N1
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-6423112fc5f740f1b81f8bc3b9883d73
COC(=O)/C=C/c1ccc(C#N)cc1>>COC(=O)CCc1ccc(C#N)cc1
C(#N)C1=CC=C(/C=C/C(=O)OC)C=C1>>C(#N)C1=CC=C(CCC(=O)OC)C=C1
[CH3:1][O:2][C:3](=[O:4])/[CH:5]=[CH:6]/[c:7]1[cH:8][cH:9][c:10]([C:11]#[N:12])[cH:13][cH:14]1>>[CH3:1][O:2][C:3](=[O:4])[CH2:5][CH2:6][c:7]1[cH:8][cH:9][c:10]([C:11]#[N:12])[cH:13][cH:14]1
COC(=O)/C=C/c1ccc(C#N)cc1
COC(=O)CCc1ccc(C#N)cc1
null
[Pd].[O-]S(=O)(=O)[O-].[Ba+2]
C1(=CC=CC=C1)C
Reduction
Hydrogenation (double to single)
c04c38f95d7b746e5bdb99c368a7a33956c97b95b54c7ad89be2a85526386ec9
9a50abf8d2e4cd9195d7a0cadbe97483a261a81cf70b653cfddd5ecf76d383a6
c1ccccc1
[C;D1;H3:1]-[#8:2]-[C:3](=[O;D1;H0:4])/[CH;D2;+0:5]=[CH;D2;+0:6]/[c:7](:[c:8]):[c:9]>>[C;D1;H3:1]-[#8:2]-[C:3](=[O;D1;H0:4])-[CH2;D2;+0:5]-[CH2;D2;+0:6]-[c:7](:[c:8]):[c:9]
77
[{"value": 77.0, "product": "C(#N)C1=CC=C(CCC(=O)OC)C=C1", "details": "PERCENTYIELD", "is_desired": false}, {"value": 76.7, "product": "C(#N)C1=CC=C(CCC(=O)OC)C=C1", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
9
HOUR
To a solution of methyl p-cyano-trans-cinnamate (13.6 g, 73 mmol) in toluene (485 mL) was added 5% Pd/BaSO4 (2.7 g). After 9 hours under hydrogen gas at 4 bar (60 psi), the solution was filtered, concentrated in vacuo and chromatographed over silica gel, eluting with a step gradient of hexanes through 30% ethyl acetate...
10.6084/m9.figshare.5104873.v1
null
Ester
Ester
null
null
c1ccccc1
null
[Pd].[O-]S(=O)(=O)[O-].[Ba+2].C1(=CC=CC=C1)C
null
9
COC(=O)/C=C/c1ccc(C#N)cc1>[Pd].[O-]S(=O)(=O)[O-].[Ba+2].C1(=CC=CC=C1)C>COC(=O)CCc1ccc(C#N)cc1
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-83a8bb81a8d64ea092985f3237412bba
CC(C)(C)OC(=O)NCc1ccc([N+](=O)[O-])cc1>>CC(C)(C)OC(=O)NCc1ccc(N)cc1
[BH4-].[Na+].C(=O)(OC(C)(C)C)NCC1=CC=C(C=C1)[N+](=O)[O-].[BH4-].[Na+]>>C(=O)(OC(C)(C)C)NCC1=CC=C(C=C1)N
O=[N+:14]([O-])[c:13]1[cH:12][cH:11][c:10]([CH2:9][NH:8][C:6]([O:5][C:2]([CH3:1])([CH3:3])[CH3:4])=[O:7])[cH:16][cH:15]1>>[CH3:1][C:2]([CH3:3])([CH3:4])[O:5][C:6](=[O:7])[NH:8][CH2:9][c:10]1[cH:11][cH:12][c:13]([NH2:14])[cH:15][cH:16]1
CC(C)(C)OC(=O)NCc1ccc([N+](=O)[O-])cc1
CC(C)(C)OC(=O)NCc1ccc(N)cc1
null
null
CO
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]
97
[{"value": 97.0, "product": "C(=O)(OC(C)(C)C)NCC1=CC=C(C=C1)N", "details": "PERCENTYIELD", "is_desired": false}, {"value": 96.9, "product": "C(=O)(OC(C)(C)C)NCC1=CC=C(C=C1)N", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
null
null
To a stirring solution of p-BocNHCH2C6H4NO2 (7.5 g, 29.7 mmol) and NiCl2.6H2O (17.7 g, 74.3 mmol) in methanol (150 mL) at 0° C. was added NaBH4 (5.6 g, 149 mmol) in small portions over 30 min. After complete addition of NaBH4 and 15 min, the solvent was evaporated in vacuo and the residue was dissolved in conc. ammoniu...
10.6084/m9.figshare.5104873.v1
null
Nitro group
Primary amine
null
null
c1ccccc1
Other
CO
null
null
CC(C)(C)OC(=O)NCc1ccc([N+](=O)[O-])cc1>CO>CC(C)(C)OC(=O)NCc1ccc(N)cc1
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-bbd17ea5df144cd0a50c633bd92af129
COC(=O)Cl.NCCc1ccccc1>>COC(=O)NCCc1ccccc1
Cl.C(CC1=CC=CC=C1)N.C(C)N(CC)CC.ClC(=O)OC>>COC(=O)NCCC1=CC=CC=C1
Cl[C:3]([O:2][CH3:1])=[O:4].[NH2:5][CH2:6][CH2:7][c:8]1[cH:9][cH:10][cH:11][cH:12][cH:13]1>>[CH3:1][O:2][C:3](=[O:4])[NH:5][CH2:6][CH2:7][c:8]1[cH:9][cH:10][cH:11][cH:12][cH:13]1
COC(=O)Cl.NCCc1ccccc1
COC(=O)NCCc1ccccc1
null
null
C1CCOC1.C(C)OCC
Protection
Acylation of Nitrogen Nucleophiles by Acyl/Thioacyl/Carbamoyl Halides and Analogs_OS
038720aa61a7efa0f2a9ee6f2e0adf63a9ffdc2be4697c11a6215baef34f97b2
205f353513ce9506ab61831799da8fb73ec2ef5cfa927664496d3ce72c438860
c1ccccc1
Cl-[C;H0;D3;+0:1](=[O;D1;H0:2])-[#8:3]-[C;D1;H3:4].[C:5]-[C:6]-[NH2;D1;+0:7]>>[C:5]-[C:6]-[NH;D2;+0:7]-[C;H0;D3;+0:1](=[O;D1;H0:2])-[#8:3]-[C;D1;H3:4]
95
[{"value": 95.0, "product": "COC(=O)NCCC1=CC=CC=C1", "details": "PERCENTYIELD", "is_desired": false}, {"value": 94.9, "product": "COC(=O)NCCC1=CC=CC=C1", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
1
HOUR
To a stirred solution of phenethylamine (75.2 mL, 0.6 mol) and triethylamine (83 mL, 0.6 mol) in THF (500 mL) was added slowly methyl chloroformate 46.2 mL, 0.6 mol) dissolved in THF (50 mL). After the reaction was stirred for an additional 1 h at room temperature, diethyl ether (2 L) and 1N HCl (800 mL) were added. Th...
10.6084/m9.figshare.5104873.v1
null
Acyl halide.Ether.Primary amine
Carbamic ester
null
null
c1ccccc1
HCl
C1CCOC1.C(C)OCC
null
1
COC(=O)Cl.NCCc1ccccc1>C1CCOC1.C(C)OCC>COC(=O)NCCc1ccccc1
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-270d72865aa54cd2959c3b0657ef5d22
CC[O-].COC(=O)N1CCC2CCCCC2C1C(=O)OC(C)(C)C>>CCOC(=O)C1C2CCCCC2CCN1C(=O)OC
C(C)(C)(C)OC(=O)C1N(CCC2CCCCC12)C(=O)OC.[O-]CC.[Na+]>>C(C)OC(=O)C1N(CCC2CCCCC12)C(=O)OC
[CH3:1][CH2:2][O-:3].CC(C)(C)O[C:4](=[O:5])[CH:6]1[CH:7]2[CH2:8][CH2:9][CH2:10][CH2:11][CH:12]2[CH2:13][CH2:14][N:15]1[C:16](=[O:17])[O:18][CH3:19]>>[CH3:1][CH2:2][O:3][C:4](=[O:5])[CH:6]1[CH:7]2[CH2:8][CH2:9][CH2:10][CH2:11][CH:12]2[CH2:13][CH2:14][N:15]1[C:16](=[O:17])[O:18][CH3:19]
CC[O-].COC(=O)N1CCC2CCCCC2C1C(=O)OC(C)(C)C
CCOC(=O)C1C2CCCCC2CCN1C(=O)OC
null
null
CCO
Acylation
OtherReaction
3cc7d733b384e9ba94618e0e6dfcbd720d0785c06391bc57e0b5b74973c7cb95
42b1bb1596c614df074e57dead0e958643c9c7a196d5946ef0b85c6ac72e94d6
C1CCC2CNCCC2C1
C-C(-C)(-C)-O-[C;H0;D3;+0:1](=[O;D1;H0:2])-[C:3](-[C:4])-[#7:5](-[C:6](-[#8:7])=[O;D1;H0:8])-[C:9].[C;D1;H3:10]-[C:11]-[O-;H0;D1:12]>>[#8:7]-[C:6](=[O;D1;H0:8])-[#7:5](-[C:9])-[C:3](-[C;H0;D3;+0:1](=[O;D1;H0:2])-[O;H0;D2;+0:12]-[C:11]-[C;D1;H3:10])-[C:4]
95.2
[{"value": 0.95, "product": "C(C)OC(=O)C1N(CCC2CCCCC12)C(=O)OC", "details": "PERCENTYIELD", "is_desired": false}, {"value": 95.2, "product": "C(C)OC(=O)C1N(CCC2CCCCC12)C(=O)OC", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
null
null
To a solution of 2-methoxycarbonyl-(1RS,4aSR,8aSR)-perhydoisoquinoline-1-carboxylic acid t-butyl ester (81.2 g, 273 mmol) in EtOH (500 mL) was added sodium ethoxide (21% in ethanol) (88.4 mL, 273 mmol) and the reaction mixture was refluxed (24 h). The organic solvent was evaporated in vacuo, ethyl acetate (400 mL) and ...
10.6084/m9.figshare.5104873.v1
null
Ester.Boc
Ester
null
null
C1CCC2C[NH]CCC2C1
HO-
CCO
null
null
CC[O-].COC(=O)N1CCC2CCCCC2C1C(=O)OC(C)(C)C>CCO>CCOC(=O)C1C2CCCCC2CCN1C(=O)OC
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-38e1d602a0364020bf23b6b6c882b7cf
N#Cc1cccs1.O=C=O>>N#Cc1ccc(C=O)s1
CN(C=O)C.C(CCC)[Li].C(CC(O)(C(=O)O)CC(=O)O)(=O)O.S1C(=CC=C1)C#N.C(=O)=O.CC(=O)C.C(C)(C)NC(C)C>>C(#N)C=1SC(=CC1)C=O
[N:1]#[C:2][c:3]1[cH:4][cH:5][cH:6][s:9]1.O=[C:7]=[O:8]>>[N:1]#[C:2][c:3]1[cH:4][cH:5][c:6]([CH:7]=[O:8])[s:9]1
N#Cc1cccs1.O=C=O
N#Cc1ccc(C=O)s1
null
null
C1CCOC1.O
C-C Coupling
OtherReaction
05aa40df6ec4f7da1e5627875219c10c948fc22ad67059603c674615270a006e
3c6b0d8e5d1da1ba2dcb896a8f9334c1841604d7035e307445ba5ecf475b5051
c1ccsc1
O=[C;H0;D2;+0:1]=[O;D1;H0:2].[#16;a:3]1:[c:4]:[c:5]:[c:6]:[cH;D2;+0:7]:1>>[O;D1;H0:2]=[CH;D2;+0:1]-[c;H0;D3;+0:7]1:[#16;a:3]:[c:4]:[c:5]:[c:6]:1
84
[{"value": 84.0, "product": "C(#N)C=1SC(=CC1)C=O", "details": "PERCENTYIELD", "is_desired": false}]
null
null
5
MINUTE
To a flame-dried 3 neck 1 L round bottom flask was added diisopropylamine (9 mL, 66 mmol) and THF (150 mL) under a nitrogen atmosphere. The flask was cooled to an internal temperature of -78° C. (dry ice/acetone). To this stirring solution was added n-butyllithium (1.6M in hexanes, 41.3 mL, 66.1 mmol) via syringe and t...
10.6084/m9.figshare.5104873.v1
null
Carbon dioxide
Aldehyde
c1ccsc1
c1ccsc1
c1ccsc1
Other
C1CCOC1.O
null
0.083333
N#Cc1cccs1.O=C=O>C1CCOC1.O>N#Cc1ccc(C=O)s1
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-a1b67cc5004d4967b21c8097f4c0e66d
N#Cc1ccc(C=O)s1>>N#Cc1ccc(CO)s1
C(#N)C=1SC(=CC1)C=O.[BH4-].[Na+]>>C(#N)C=1SC(=CC1)CO
[N:1]#[C:2][c:3]1[cH:4][cH:5][c:6]([CH:7]=[O:8])[s:9]1>>[N:1]#[C:2][c:3]1[cH:4][cH:5][c:6]([CH2:7][OH:8])[s:9]1
N#Cc1ccc(C=O)s1
N#Cc1ccc(CO)s1
null
null
CCO
Reduction
Reduction of aldehydes and ketones to alcohols
e7895795cd3f75445716c94697823c5929dcd4b5344525875fe75d36bca2f9d7
21bb81d5469aaaca71ab12c186bea4016451717fad8780cf288858a7d8fbc55a
c1ccsc1
[O;H0;D1;+0:1]=[CH;D2;+0:2]-[c:3](:[c:4]):[#16;a:5]:[c:6]>>[OH;D1;+0:1]-[CH2;D2;+0:2]-[c:3](:[c:4]):[#16;a:5]:[c:6]
88
[{"value": 88.0, "product": "C(#N)C=1SC(=CC1)CO", "details": "PERCENTYIELD", "is_desired": false}, {"value": 87.7, "product": "C(#N)C=1SC(=CC1)CO", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
5
MINUTE
To a solution of 2-cyano-5-formyl-thiophene (6.9 g, 50 mmol) in EtOH (100 mL) was added sodium borohydride (1.9 g, 50 mmol) in portions. After 5 min of stirring, the solvent was removed in vacuo and the residue was partitioned between ethyl acetate and brine. The layers were separated and the organic phase was washed o...
10.6084/m9.figshare.5104873.v1
null
Aldehyde
Primary alcohol
null
null
c1ccsc1
null
CCO
null
0.083333
N#Cc1ccc(C=O)s1>CCO>N#Cc1ccc(CO)s1
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-69104add2a2849aba17decff43b8a344
BrC(Br)(Br)Br.N#Cc1ccc(CO)s1>>N#Cc1ccc(CBr)s1
C(#N)C=1SC(=CC1)CO.C1(=CC=CC=C1)P(C1=CC=CC=C1)C1=CC=CC=C1.C(Br)(Br)(Br)Br>>C(#N)C=1SC(=CC1)CBr
BrC(Br)(Br)[Br:8].O[CH2:7][c:6]1[cH:5][cH:4][c:3]([C:2]#[N:1])[s:9]1>>[N:1]#[C:2][c:3]1[cH:4][cH:5][c:6]([CH2:7][Br:8])[s:9]1
BrC(Br)(Br)Br.N#Cc1ccc(CO)s1
N#Cc1ccc(CBr)s1
null
null
C1CCOC1
Functional Group Interconversion
Appel reaction
752e1807cd47d8316010cc3f92eab16c5a89ffb844d9514fcae469ba993c78dd
2c6b51fb1e17cb2c93d565e0423c75825df2c8e11c870e0c98b278f20ba9f3ad
c1ccsc1
Br-C(-Br)(-Br)-[Br;H0;D1;+0:1].O-[CH2;D2;+0:2]-[c:3](:[c:4]):[#16;a:5]:[c:6]>>[Br;H0;D1;+0:1]-[CH2;D2;+0:2]-[c:3](:[c:4]):[#16;a:5]:[c:6]
75
[{"value": 75.0, "product": "C(#N)C=1SC(=CC1)CBr", "details": "PERCENTYIELD", "is_desired": false}, {"value": 74.8, "product": "C(#N)C=1SC(=CC1)CBr", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
8
HOUR
To a solution of 2-cyano-5-(hydroxymethyl)thiophene (6.0 g, 43 mmol) in THF (50 mL) was added triphenylphosphine (15.7 g, 47 mmol) and carbon tetrabromide (12.3 g, 47 mmol). After stirring overnight under nitrogen atmosphere at room temperature, the solvent was removed in vacuo and the residue was dissolved in chlorofo...
10.6084/m9.figshare.5104873.v1
null
Tertiary halide.Tertiary halide.Tertiary halide.Tertiary halide.Primary alcohol
Primary halide
null
null
c1ccsc1
HBr
C1CCOC1
null
8
BrC(Br)(Br)Br.N#Cc1ccc(CO)s1>C1CCOC1>N#Cc1ccc(CBr)s1
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-47a44d0423b048a0ba771f9e6b7956a7
CC#CCO.O=C(O)C1CN=CNC1>>CC#CCOC(=O)C1CN=CNC1
Cl.N1C=NCC(C1)C(=O)O.C(C(=O)Cl)(=O)Cl.C(C#CC)O>>C(C#CC)OC(=O)C1CN=CNC1
[CH3:1][C:2]#[C:3][CH2:4][OH:5].O[C:6](=[O:7])[CH:8]1[CH2:9][N:10]=[CH:11][NH:12][CH2:13]1>>[CH3:1][C:2]#[C:3][CH2:4][O:5][C:6](=[O:7])[CH:8]1[CH2:9][N:10]=[CH:11][NH:12][CH2:13]1
CC#CCO.O=C(O)C1CN=CNC1
CC#CCOC(=O)C1CN=CNC1
null
null
C1=CC=CC=C1.O
Protection
Esterification of Carboxylic Acids
070670f68a20c1021da94fabee54def4688122fb721af5f52cd5a03630845d0e
0d8a72b7375d91aa7263e766e03a3cb7c4fa91e27abcd590409ff03b98eed690
C1=NCCCN1
O-[C;H0;D3;+0:1](=[O;D1;H0:2])-[C:3](-[C:4]-[#7:5])-[C:6]-[#7:7].[C;D1;H3:8]-[C:9]#[C:10]-[C:11]-[OH;D1;+0:12]>>[#7:7]-[C:6]-[C:3](-[C;H0;D3;+0:1](=[O;D1;H0:2])-[O;H0;D2;+0:12]-[C:11]-[C:10]#[C:9]-[C;D1;H3:8])-[C:4]-[#7:5]
61
[{"value": 61.0, "product": "C(C#CC)OC(=O)C1CN=CNC1", "details": "PERCENTYIELD", "is_desired": false}]
null
null
null
null
1,4,5,6-tetrahydropyrimidine-5-carboxylic acid hydrochloride (1 g, 6 mmol) was suspended in a solution of oxalyl chloride (1.5 mL, 17 mmol) in benzene (10 mL), heated with stirring under reflux for 2.5 h, and then evaporated to dryness in vacuo after cooling, to give an orange-yellow residue. A mixture of the acid chlo...
10.6084/m9.figshare.5104873.v1
null
Carboxylic acid.Primary alcohol
Ester
null
null
C1=NCCCN1
HO-
C1=CC=CC=C1.O
null
null
CC#CCO.O=C(O)C1CN=CNC1>C1=CC=CC=C1.O>CC#CCOC(=O)C1CN=CNC1
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-f8b34ec462304b808abfb14a00d8380b
N#Cc1ccc(CBr)cc1.O=C1NCCN1>>N#Cc1ccc(CN2CCN(Cc3ccc(C#N)cc3)C2=O)cc1
O.BrCC1=CC=C(C#N)C=C1.[H-].[Na+].N1C(NCC1)=O>>O=C1N(CCN1CC1=CC=C(C#N)C=C1)CC1=CC=C(C#N)C=C1
Br[CH2:7][c:6]1[cH:5][cH:4][c:3]([C:2]#[N:1])[cH:24][cH:23]1.[NH:8]1[CH2:9][CH2:15][NH:11][C:21]1=[O:22]>>[N:1]#[C:2][c:3]1[cH:4][cH:5][c:6]([CH2:7][N:8]2[CH2:9][CH2:10][N:11]([CH2:12][c:13]3[cH:14][cH:15][c:16]([C:17]#[N:18])[cH:19][cH:20]3)[C:21]2=[O:22])[cH:23][cH:24]1
N#Cc1ccc(CBr)cc1.O=C1NCCN1
N#Cc1ccc(CN2CCN(Cc3ccc(C#N)cc3)C2=O)cc1
null
null
CN(C=O)C
Aromatic Heterocycle Formation
OtherReaction
39571f641692bae0ab2e4fb7e56baf0a046bbe68e5d15065d8f936b61702d85c
04064b000c1f037cb6379c4a9b891971302bcd094d2302ea56061b3b37327222
O=C1N(Cc2ccccc2)CCN1Cc1ccccc1
Br-[CH2;D2;+0:1]-[c:2](:[c:3]):[c:4].[O;D1;H0:5]=[C:6]1-[NH;D2;+0:7]-[CH2;D2;+0:8]-[CH2;D2;+0:9]-[NH;D2;+0:10]-1>>[C:11]-[c:12](:[c:13]):[cH;D2;+0:8]:[c:14]:[c:15]-[C:16]-[N;H0;D3;+0:7]1-[C:17]-[CH2;D2;+0:9]-[N;H0;D3;+0:10](-[CH2;D2;+0:1]-[c:2](:[c:3]):[c:4])-[C:6]-1=[O;D1;H0:5]
null
[]
null
null
1
HOUR
To sodium hydride (2.4 g, 60 mmol) in dimethylformamide (50 mL) at 0° C. was added imidazolin-2-one (2.6 g, 30 mmol). After stirring for 20 minutes 4-(bromomethyl)benzonitrile (13 g, 66 mmol) was added and the mixture was warmed to ambient temperature. After stirring for 1 hour the reaction was poured into water and a ...
10.6084/m9.figshare.5104873.v1
null
Primary halide.Urea
Urea.Nitrile
C1CNCN1
C1C[NH]C[NH]1.c1ccccc1
c1ccccc1.C1C[NH]C[NH]1.c1ccccc1
Br-
CN(C=O)C
null
1
N#Cc1ccc(CBr)cc1.O=C1NCCN1>CN(C=O)C>N#Cc1ccc(CN2CCN(Cc3ccc(C#N)cc3)C2=O)cc1
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-e3fd8b3d0bbc4562bc1152c1b8ade224
N#Cc1cccc(CBr)c1.O=c1[nH]c(-c2ccccc2)c(-c2ccccc2)[nH]1>>N#Cc1cccc(Cn2c(-c3ccccc3)c(-c3ccccc3)[nH]c2=O)c1
C1(=CC=CC=C1)C=1NC(NC1C1=CC=CC=C1)=O.BrCC=1C=C(C#N)C=CC1.[H-].[Na+]>>C1(=CC=CC=C1)C=1NC(N(C1C1=CC=CC=C1)CC=1C=C(C#N)C=CC1)=O
Br[CH2:8][c:7]1[cH:6][cH:5][cH:4][c:3]([C:2]#[N:1])[cH:27]1.[nH:9]1[c:10](-[c:11]2[cH:12][cH:13][cH:14][cH:15][cH:16]2)[c:17](-[c:18]2[cH:19][cH:20][cH:21][cH:22][cH:23]2)[nH:24][c:25]1=[O:26]>>[N:1]#[C:2][c:3]1[cH:4][cH:5][cH:6][c:7]([CH2:8][n:9]2[c:10](-[c:11]3[cH:12][cH:13][cH:14][cH:15][cH:16]3)[c:17](-[c:18]3[cH:1...
N#Cc1cccc(CBr)c1.O=c1[nH]c(-c2ccccc2)c(-c2ccccc2)[nH]1
N#Cc1cccc(Cn2c(-c3ccccc3)c(-c3ccccc3)[nH]c2=O)c1
null
null
CN(C=O)C
Heteroatom Alkylation and Arylation
N-alkylation of secondary amines with alkyl halides
b9d84e1ee028da6e8c5d8924d45fbf8f3755d9adc2caf0035bd5ed7f30f5ee03
2e1e5fd9557b69cb528f6b2ffd179c67ef24ecb1a2c3994e1cdf0efe7ae19e9c
O=c1[nH]c(-c2ccccc2)c(-c2ccccc2)n1Cc1ccccc1
Br-[CH2;D2;+0:1]-[c:2](:[c:3]):[c:4].[O;D1;H0:5]=[c:6]1:[#7;a:7]:[c:8](-[c:9]):[c:10](-[c:11]):[nH;D2;+0:12]:1>>[O;D1;H0:5]=[c:6]1:[#7;a:7]:[c:8](-[c:9]):[c:10](-[c:11]):[n;H0;D3;+0:12]:1-[CH2;D2;+0:1]-[c:2](:[c:3]):[c:4]
null
[]
null
null
null
null
In a manner similar to Preparation 1 above, 2,3-dihydro-4,5-diphenyl-1H-imidazol-2-one (1.2 g, 5 mmol) was reacted with 3-(bromomethyl)benzonitrile (0.39 g, 2 mmol) and sodium hydride (0.18 g, 5 mmol) in dimethylformamide (20 mL) to give 3-[(2,3-dihydro-4,5-diphenyl-2-oxo-1H-imidazol-1-yl)methyl]benzonitrile after chro...
10.6084/m9.figshare.5104873.v1
null
Primary halide
null
c1c[nH]cn1
c1c[nH]cn1
c1ccccc1.c1ccccc1.c1ccccc1.c1c[nH]cn1
HBr
CN(C=O)C
null
null
N#Cc1cccc(CBr)c1.O=c1[nH]c(-c2ccccc2)c(-c2ccccc2)[nH]1>CN(C=O)C>N#Cc1cccc(Cn2c(-c3ccccc3)c(-c3ccccc3)[nH]c2=O)c1
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-72c771861dac4179880db9f695399653
COC(=O)c1cccc(CBr)c1.O=c1[nH]c(-c2ccccc2)c(-c2ccccc2)[nH]1>>COC(=O)c1cccc(Cn2c(-c3ccccc3)c(-c3ccccc3)[nH]c2=O)c1
Cl.C1(=CC=CC=C1)C=1NC(NC1C1=CC=CC=C1)=O.[H-].[Na+].BrCC=1C=C(C(=O)OC)C=CC1>>COC(=O)C=1C=C(C=CC1)CN1C(NC(=C1C1=CC=CC=C1)C1=CC=CC=C1)=O
Br[CH2:10][c:9]1[cH:8][cH:7][cH:6][c:5]([C:3]([O:2][CH3:1])=[O:4])[cH:29]1.[nH:11]1[c:12](-[c:13]2[cH:14][cH:15][cH:16][cH:17][cH:18]2)[c:19](-[c:20]2[cH:21][cH:22][cH:23][cH:24][cH:25]2)[nH:26][c:27]1=[O:28]>>[CH3:1][O:2][C:3](=[O:4])[c:5]1[cH:6][cH:7][cH:8][c:9]([CH2:10][n:11]2[c:12](-[c:13]3[cH:14][cH:15][cH:16][cH:...
COC(=O)c1cccc(CBr)c1.O=c1[nH]c(-c2ccccc2)c(-c2ccccc2)[nH]1
COC(=O)c1cccc(Cn2c(-c3ccccc3)c(-c3ccccc3)[nH]c2=O)c1
null
null
CN(C)C=O
Heteroatom Alkylation and Arylation
N-alkylation of secondary amines with alkyl halides
b9d84e1ee028da6e8c5d8924d45fbf8f3755d9adc2caf0035bd5ed7f30f5ee03
2e1e5fd9557b69cb528f6b2ffd179c67ef24ecb1a2c3994e1cdf0efe7ae19e9c
O=c1[nH]c(-c2ccccc2)c(-c2ccccc2)n1Cc1ccccc1
Br-[CH2;D2;+0:1]-[c:2](:[c:3]):[c:4].[O;D1;H0:5]=[c:6]1:[#7;a:7]:[c:8](-[c:9]):[c:10](-[c:11]):[nH;D2;+0:12]:1>>[O;D1;H0:5]=[c:6]1:[#7;a:7]:[c:8](-[c:9]):[c:10](-[c:11]):[n;H0;D3;+0:12]:1-[CH2;D2;+0:1]-[c:2](:[c:3]):[c:4]
25
[{"value": 25.0, "product": "COC(=O)C=1C=C(C=CC1)CN1C(NC(=C1C1=CC=CC=C1)C1=CC=CC=C1)=O", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
50
CELSIUS
30
MINUTE
To 2,3-dihydro-4,5-diphenyl-1H-imidazol-2-one (4.76 g, 20 mmol) in 50 mL DMF was added to a suspension of NaH (0.8 g, 20 mmol) in 25 mL DMF. The suspension was stirred at ambient temperatures for 30 minutes, then heated to 50° C. for 30 minutes. A solution of methyl 3-bromomethylbenzoate (2.86 g, 12.5 mmol) in 20 mL DM...
10.6084/m9.figshare.5104873.v1
null
Primary halide
null
c1c[nH]cn1
c1c[nH]cn1
c1ccccc1.c1ccccc1.c1ccccc1.c1c[nH]cn1
HBr
CN(C)C=O
50
0.5
COC(=O)c1cccc(CBr)c1.O=c1[nH]c(-c2ccccc2)c(-c2ccccc2)[nH]1>CN(C)C=O>COC(=O)c1cccc(Cn2c(-c3ccccc3)c(-c3ccccc3)[nH]c2=O)c1
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-d584948385474449aadf00017badca74
N#Cc1ccc2ccc(CBr)cc2c1.N#Cc1cccc(Cn2c(-c3ccccc3)c(-c3ccccc3)[nH]c2=O)c1>>N#Cc1cccc(Cn2c(-c3ccccc3)c(-c3ccccc3)n(Cc3ccc4ccc(C#N)cc4c3)c2=O)c1
C1(=CC=CC=C1)C=1NC(N(C1C1=CC=CC=C1)CC=1C=C(C#N)C=CC1)=O.BrCC1=CC=C2C=CC(=CC2=C1)C#N>>C(#N)C=1C=C(C=CC1)CN1C(N(C(=C1C1=CC=CC=C1)C1=CC=CC=C1)CC1=CC=C2C=CC(=CC2=C1)C#N)=O
Br[CH2:25][c:26]1[cH:27][cH:28][c:29]2[cH:30][cH:31][c:32]([C:33]#[N:34])[cH:35][c:36]2[cH:37]1.[N:1]#[C:2][c:3]1[cH:4][cH:5][cH:6][c:7]([CH2:8][n:9]2[c:10](-[c:11]3[cH:12][cH:13][cH:14][cH:15][cH:16]3)[c:17](-[c:18]3[cH:19][cH:20][cH:21][cH:22][cH:23]3)[nH:24][c:38]2=[O:39])[cH:40]1>>[N:1]#[C:2][c:3]1[cH:4][cH:5][cH:6...
N#Cc1ccc2ccc(CBr)cc2c1.N#Cc1cccc(Cn2c(-c3ccccc3)c(-c3ccccc3)[nH]c2=O)c1
N#Cc1cccc(Cn2c(-c3ccccc3)c(-c3ccccc3)n(Cc3ccc4ccc(C#N)cc4c3)c2=O)c1
null
null
null
Heteroatom Alkylation and Arylation
N-alkylation of secondary amines with alkyl halides
b9d84e1ee028da6e8c5d8924d45fbf8f3755d9adc2caf0035bd5ed7f30f5ee03
2e1e5fd9557b69cb528f6b2ffd179c67ef24ecb1a2c3994e1cdf0efe7ae19e9c
O=c1n(Cc2ccccc2)c(-c2ccccc2)c(-c2ccccc2)n1Cc1ccc2ccccc2c1
Br-[CH2;D2;+0:1]-[c:2](:[c:3]):[c:4].[C:5]-[#7;a:6]1:[c:7](-[c:8]):[c:9](-[c:10]):[nH;D2;+0:11]:[c:12]:1=[O;D1;H0:13]>>[C:5]-[#7;a:6]1:[c:7](-[c:8]):[c:9](-[c:10]):[n;H0;D3;+0:11](-[CH2;D2;+0:1]-[c:2](:[c:3]):[c:4]):[c:12]:1=[O;D1;H0:13]
null
[]
null
null
null
null
In a manner similar to Preparation 2 above, 3-[(2,3-dihydro4,5-diphenyl-2-oxo-1H-imidazol-1-yl)methyl]benzonitrile was reacted with 7-(bromomethyl)-naphthalene-2-carbonitrile to give 7-[[3-(3-cyanophenyl)methyl-2,3-dihydro-4,5-diphenyl-2-oxo-1H-imidazol-1-yl]methyl]naphthalene-2-carbonitrile; NMR (CDCl3)8.05 (s,1), 7.9...
10.6084/m9.figshare.5104873.v1
null
Primary halide
null
c1c[nH]cn1
c1c[nH]cn1
c1ccccc1.c1ccccc1.c1ccccc1.c1ccc2ccccc2c1.c1c[nH]cn1
HBr
null
null
null
N#Cc1ccc2ccc(CBr)cc2c1.N#Cc1cccc(Cn2c(-c3ccccc3)c(-c3ccccc3)[nH]c2=O)c1>>N#Cc1cccc(Cn2c(-c3ccccc3)c(-c3ccccc3)n(Cc3ccc4ccc(C#N)cc4c3)c2=O)c1
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-d0f3e38e8aab4374bc8286880e180242
CCOC(=O)c1cn(C2Cc3ccccc3C2=O)c(C(=O)OCC)n1.[NH4+]>>CCOC(=O)c1cn2c3c([nH]c(=O)c2n1)-c1ccccc1C3
C(C)(=O)[O-].[NH4+].O=C1C(CC2=CC=CC=C12)N1C(=NC(=C1)C(=O)OCC)C(=O)OCC>>O=C1C=2N(C3=C(N1)C=1C=CC=CC1C3)C=C(N2)C(=O)OCC
CCO[C:12](=[O:13])[c:14]1[n:8]([CH:9]2[C:10](=O)[c:16]3[cH:17][cH:18][cH:19][cH:20][c:21]3[CH2:22]2)[cH:7][c:6]([C:4]([O:3][CH2:2][CH3:1])=[O:5])[n:15]1.[NH4+:11]>>[CH3:1][CH2:2][O:3][C:4](=[O:5])[c:6]1[cH:7][n:8]2[c:9]3[c:10]([nH:11][c:12](=[O:13])[c:14]2[n:15]1)-[c:16]1[cH:17][cH:18][cH:19][cH:20][c:21]1[CH2:22]3
CCOC(=O)c1cn(C2Cc3ccccc3C2=O)c(C(=O)OCC)n1.[NH4+]
CCOC(=O)c1cn2c3c([nH]c(=O)c2n1)-c1ccccc1C3
null
null
C(C)(=O)O
Aromatic Heterocycle Formation
OtherReaction
81592ab7f3ddbb1f56ea7a979fdc4c2449d437c2d54c1a03e34c3c798f871052
90d91da8fe4a4df48cab6f211982834fddab85bdecacddc95412489737467fb5
O=c1[nH]c2c(n3ccnc13)Cc1ccccc1-2
C-C-O-[C;H0;D3;+0:1](=[O;D1;H0:2])-[c:3]1:[#7;a:4]:[c:5](-[C:6](-[#8:7])=[O;D1;H0:8]):[c:9]:[#7;a:10]:1-[CH;D3;+0:11]1-[C:12]-[c:13](:[c:14]):[c;H0;D3;+0:15](:[c:16]:[c:17])-[C;H0;D3;+0:18]-1=O.[NH4+;D0:19]>>[#8:7]-[C:6](=[O;D1;H0:8])-[c:5]1:[#7;a:4]:[c:3]2:[#7;a:10](:[c:9]:1):[c;H0;D3;+0:11]1:[c;H0;D3;+0:18](:[nH;D2;+...
37.7
[{"value": 37.7, "product": "O=C1C=2N(C3=C(N1)C=1C=CC=CC1C3)C=C(N2)C(=O)OCC", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
null
null
51.2 g of ammonium acetate are added in small portions to a solution of 2 g of diethyl 1-(1-oxoindan-2-yl)imidazole-2,4-dicarboxylate in 80 ml of acetic acid and the mixture is heated to reflux for 2 hours. After cooling to a temperature close to 20° C. the precipitate formed is filtered off and rinsed with distilled w...
10.6084/m9.figshare.5104873.v1
null
Ketone.Ester
null
c1c[nH]cn1.c1ccc2c(c1)CCC2
c1cn2c3c(ncc2n1)c1ccccc1C3
c1cn2c3c(ncc2n1)c1ccccc1C3
HO-
C(C)(=O)O
null
null
CCOC(=O)c1cn(C2Cc3ccccc3C2=O)c(C(=O)OCC)n1.[NH4+]>C(C)(=O)O>CCOC(=O)c1cn2c3c([nH]c(=O)c2n1)-c1ccccc1C3
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-285176e937a841c4943a04d3364e6c62
CCOC(=O)c1cn2c3c([nH]c(=O)c2n1)-c1ccc(N)cc1C3.CN=C=O>>CCOC(=O)c1cn2c3c([nH]c(=O)c2n1)-c1ccc(NC(=O)NC)cc1C3
CN=C=O.NC1=CC=2CC3=C(NC(C=4N3C=C(N4)C(=O)OCC)=O)C2C=C1>>CNC(NC1=CC=2CC3=C(NC(C=4N3C=C(N4)C(=O)OCC)=O)C2C=C1)=O
[CH3:1][CH2:2][O:3][C:4](=[O:5])[c:6]1[cH:7][n:8]2[c:9]3[c:10]([nH:11][c:12](=[O:13])[c:14]2[n:15]1)-[c:16]1[cH:17][cH:18][c:19]([NH2:20])[cH:25][c:26]1[CH2:27]3.[C:21](=[O:22])=[N:23][CH3:24]>>[CH3:1][CH2:2][O:3][C:4](=[O:5])[c:6]1[cH:7][n:8]2[c:9]3[c:10]([nH:11][c:12](=[O:13])[c:14]2[n:15]1)-[c:16]1[cH:17][cH:18][c:1...
CCOC(=O)c1cn2c3c([nH]c(=O)c2n1)-c1ccc(N)cc1C3.CN=C=O
CCOC(=O)c1cn2c3c([nH]c(=O)c2n1)-c1ccc(NC(=O)NC)cc1C3
null
null
CN(C=O)C
Acylation
Urea synthesis via isocyanate and primary amine
d39cd7dc52a79bb265ff8ef61ef7bf9dc7f7b5fb0150fcb4881bdfb18ab9c380
a5dc801930c765d2a435a0a2973e50163c305ba8e7641d6adbcc1550b7b96de7
O=c1[nH]c2c(n3ccnc13)Cc1ccccc1-2
[C;D1;H3:1]-[N;H0;D2;+0:2]=[C;H0;D2;+0:3]=[O;D1;H0:4].[NH2;D1;+0:5]-[c:6](:[c:7]):[c:8]>>[C;D1;H3:1]-[NH;D2;+0:2]-[C;H0;D3;+0:3](=[O;D1;H0:4])-[NH;D2;+0:5]-[c:6](:[c:7]):[c:8]
null
[]
null
null
12
HOUR
0.44 ml of methyl isocyanate is added dropwise with stirring to a suspension of 580 mg of ethyl 8-amino-4,5-dihydro-4-oxo-10H-imidazo[1,2-a]indeno[1,2-e]pyrazine-2-carboxylate in 10 ml of dimethylformamide and stirring is continued for 12 hours at a temperature close to 20° C. The reaction mixture is then filtered, rin...
10.6084/m9.figshare.5104873.v1
null
Isocyanate.Primary amine
Urea
null
null
c1ccc2c(c1)Cc1c2ncc2nccn12
null
CN(C=O)C
null
12
CCOC(=O)c1cn2c3c([nH]c(=O)c2n1)-c1ccc(N)cc1C3.CN=C=O>CN(C=O)C>CCOC(=O)c1cn2c3c([nH]c(=O)c2n1)-c1ccc(NC(=O)NC)cc1C3
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-e4f280544c164e7781c5e91559bf59d4
CCOC(=O)c1cn(C2Cc3ccc(Cl)cc3C2=O)c(C(=O)OCC)n1.[NH4+]>>CCOC(=O)c1cn2c3c([nH]c(=O)c2n1)-c1cc(Cl)ccc1C3
ClC1=CC=C2CC(C(C2=C1)=O)N1C(=NC(=C1)C(=O)OCC)C(=O)OCC.C(C)(=O)[O-].[NH4+].C(C)(=O)O>>ClC=1C=CC=2CC3=C(NC(C=4N3C=C(N4)C(=O)OCC)=O)C2C1
CCO[C:12](=[O:13])[c:14]1[n:8]([CH:9]2[C:10](=O)[c:16]3[cH:17][c:18]([Cl:19])[cH:20][cH:21][c:22]3[CH2:23]2)[cH:7][c:6]([C:4]([O:3][CH2:2][CH3:1])=[O:5])[n:15]1.[NH4+:11]>>[CH3:1][CH2:2][O:3][C:4](=[O:5])[c:6]1[cH:7][n:8]2[c:9]3[c:10]([nH:11][c:12](=[O:13])[c:14]2[n:15]1)-[c:16]1[cH:17][c:18]([Cl:19])[cH:20][cH:21][c:2...
CCOC(=O)c1cn(C2Cc3ccc(Cl)cc3C2=O)c(C(=O)OCC)n1.[NH4+]
CCOC(=O)c1cn2c3c([nH]c(=O)c2n1)-c1cc(Cl)ccc1C3
null
null
C(C)#N.CO.CC(=O)C
Aromatic Heterocycle Formation
OtherReaction
61c7ec55b0cda76461d1bc06479dacee3533b147a8fd30112bef8bce93ad32d8
90d91da8fe4a4df48cab6f211982834fddab85bdecacddc95412489737467fb5
O=c1[nH]c2c(n3ccnc13)Cc1ccccc1-2
C-C-O-[C;H0;D3;+0:1](=[O;D1;H0:2])-[c:3]1:[#7;a:4]:[c:5](-[C:6](-[#8:7])=[O;D1;H0:8]):[c:9]:[#7;a:10]:1-[CH;D3;+0:11]1-[C:12]-[c:13](:[c:14]):[c;H0;D3;+0:15](:[c:16]:[c:17])-[C;H0;D3;+0:18]-1=O.[NH4+;D0:19]>>[#8:7]-[C:6](=[O;D1;H0:8])-[c:5]1:[#7;a:4]:[c:3]2:[#7;a:10](:[c:9]:1):[c;H0;D3;+0:11]1:[c;H0;D3;+0:18](:[nH;D2;+...
61.7
[{"value": 61.7, "product": "ClC=1C=CC=2CC3=C(NC(C=4N3C=C(N4)C(=O)OCC)=O)C2C1", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
null
null
The procedure is as in Example 1 but starting from 5 g of diethyl 1-(6-chloro-1-oxoindan-2-yl)imidazole-2,4-dicarboxylate, 118 g of ammonium acetate and 190 ml of acetic acid. After washing the precipitate with water and then with methyl ethyl ketone, the solid obtained is first of all ground in acetonitrile and then i...
10.6084/m9.figshare.5104873.v1
null
Ketone.Ester
null
c1c[nH]cn1.c1ccc2c(c1)CCC2
c1ccc2c(c1)c1ncc3nccn3c1C2
c1ccc2c(c1)c1ncc3nccn3c1C2
HO-
C(C)#N.CO.CC(=O)C
null
null
CCOC(=O)c1cn(C2Cc3ccc(Cl)cc3C2=O)c(C(=O)OCC)n1.[NH4+]>C(C)#N.CO.CC(=O)C>CCOC(=O)c1cn2c3c([nH]c(=O)c2n1)-c1cc(Cl)ccc1C3