dataset_id
large_stringclasses
414 values
reaction_id
large_stringlengths
36
36
reaction_smiles
large_stringlengths
4
873
rxn_insight_reaction
large_stringlengths
19
1.07k
mapped_reaction_smiles
large_stringlengths
14
3.37k
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large_stringlengths
1
581
product_smiles
large_stringlengths
1
433
reagent_smiles
large_stringclasses
634 values
catalyst_smiles
large_stringlengths
1
683
solvent_smiles
large_stringlengths
1
245
rxn_insight_class
large_stringclasses
11 values
rxn_insight_name
large_stringclasses
346 values
rxn_insight_tag
large_stringlengths
64
64
rxn_insight_tag2
large_stringlengths
64
64
rxn_insight_scaffold
large_stringlengths
5
288
rxn_insight_template
large_stringlengths
24
2.64k
yield_percent
float64
-0.8
90,205,160,000B
yield_measurements
large_stringlengths
2
864
temperature_value
float64
-230
30.1k
temperature_units
large_stringclasses
3 values
reaction_time_value
float64
0
4k
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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-02ee2261663048188cf6d85d2cc96e3f
ord-a62cae018b8c45d6b9035dabbb8fdbce
CO.COc1nc(Cl)cc(I)c1C=O>>COCc1c(I)cc(Cl)nc1OC
FC(C(=O)O)(F)F.ClC1=CC(=C(C(=N1)OC)C=O)I.C(C)[SiH](CC)CC.CO.C(=O)(O)[O-].[Na+]>>ClC1=NC(=C(C(=C1)I)COC)OC
O[CH3:1].[O:2]=[CH:3][c:4]1[c:5]([I:6])[cH:7][c:8]([Cl:9])[n:10][c:11]1[O:12][CH3:13]>>[CH3:1][O:2][CH2:3][c:4]1[c:5]([I:6])[cH:7][c:8]([Cl:9])[n:10][c:11]1[O:12][CH3:13]
CO.COc1nc(Cl)cc(I)c1C=O
COCc1c(I)cc(Cl)nc1OC
null
null
CCOCC
Heteroatom Alkylation and Arylation
OtherReaction
1d76918cc19966c7516bfe9a97a96abd1d20ff1b6b551b7a2a7721be5b12e885
a9e58bdb270b8602210135fa12a97050bf42474a87c9f2c3a2f396b5330373a5
c1ccncc1
O-[CH3;D1;+0:1].[#8:2]-[c:3](:[#7;a:4]:[c:5]):[c:6](-[CH;D2;+0:7]=[O;H0;D1;+0:8]):[c:9]>>[#8:2]-[c:3](:[#7;a:4]:[c:5]):[c:6](-[CH2;D2;+0:7]-[O;H0;D2;+0:8]-[CH3;D1;+0:1]):[c:9]
null
[]
25
CELSIUS
14
HOUR
To a mixture of 6-chloro-4-iodo-2-methoxy-3-pyridinecarboxaldehyde (1.07 g, 3.60 mmol), triethylsilane (0.86 mL, 5.40 mmol) and methanol (0.43 mL, 10.6 mmol) at 0° C. was added trifluoroacetic acid (2.2 mL, 28.6 mmol), and the resulting solution was stirred at 25° C. for 14 h. After dilution with ether (30 mL), saturat...
10.6084/m9.figshare.5104873.v1
null
Aldehyde.Methanol
Ether
null
null
c1ccncc1
Other
CCOCC
25
14
CO.COc1nc(Cl)cc(I)c1C=O>CCOCC>COCc1c(I)cc(Cl)nc1OC
ord_dataset-02ee2261663048188cf6d85d2cc96e3f
ord-bf42ea30b38f46aa809f3ee355b8012d
CN(C)C=O.Clc1ccc2ccccc2n1>>O=Cc1cc2ccccc2nc1Cl
CN(C=O)C.ClC1=NC2=CC=CC=C2C=C1.C(C)(C)NC(C)C.[Li]CCCC>>ClC1=NC2=CC=CC=C2C=C1C=O
CN(C)[CH:2]=[O:1].[cH:3]1[cH:4][c:5]2[cH:6][cH:7][cH:8][cH:9][c:10]2[n:11][c:12]1[Cl:13]>>[O:1]=[CH:2][c:3]1[cH:4][c:5]2[cH:6][cH:7][cH:8][cH:9][c:10]2[n:11][c:12]1[Cl:13]
CN(C)C=O.Clc1ccc2ccccc2n1
O=Cc1cc2ccccc2nc1Cl
null
null
C1CCOC1
C-C Coupling
OtherReaction
2fb6a63f37a90389382989ea42f8436574f9d339310d3a9ddc749d75d88d7d6b
f0bd75a0630092c31f21f61f4a015c77ae0dff14a0b742b4370d7a38fda490f7
c1ccc2ncccc2c1
C-N(-C)-[CH;D2;+0:1]=[O;D1;H0:2].[Cl;D1;H0:3]-[c:4]1:[#7;a:5]:[c:6]:[c:7]:[c:8]:[cH;D2;+0:9]:1>>[Cl;D1;H0:3]-[c:4]1:[#7;a:5]:[c:6]:[c:7]:[c:8]:[c;H0;D3;+0:9]:1-[CH;D2;+0:1]=[O;D1;H0:2]
92.2
[{"value": 92.0, "product": "ClC1=NC2=CC=CC=C2C=C1C=O", "details": "PERCENTYIELD", "is_desired": false}, {"value": 92.2, "product": "ClC1=NC2=CC=CC=C2C=C1C=O", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
-78
CELSIUS
30
MINUTE
To a solution of 0.46 mL (3.30 mmol) of diisopropylamine in 8 mL of THF at 0° C. was added 1.53 mL (3.30 mmol) of n-BuLi dropwise. After 20 min the solution was cooled to -78° C. and 2-chloroquinoline (491 mg, 3.0 mmol) was added neat. The mixture was stirred at -78° C. for 30 min, then dimethylformamide (0.39 mL, 5.04...
10.6084/m9.figshare.5104873.v1
null
Tertiary amide
Aldehyde
c1ccc2ncccc2c1
c1ccc2ncccc2c1
c1ccc2ncccc2c1
Other
C1CCOC1
-78
0.5
CN(C)C=O.Clc1ccc2ccccc2n1>C1CCOC1>O=Cc1cc2ccccc2nc1Cl
ord_dataset-02ee2261663048188cf6d85d2cc96e3f
ord-12269c99e5404be9b05d3835e65be89c
O=Cc1cc2ccccc2nc1I>>OCc1cc2ccccc2nc1I
IC1=NC2=CC=CC=C2C=C1C=O.[BH4-].[Na+]>>OCC=1C(=NC2=CC=CC=C2C1)I
[O:1]=[CH:2][c:3]1[cH:4][c:5]2[cH:6][cH:7][cH:8][cH:9][c:10]2[n:11][c:12]1[I:13]>>[OH:1][CH2:2][c:3]1[cH:4][c:5]2[cH:6][cH:7][cH:8][cH:9][c:10]2[n:11][c:12]1[I:13]
O=Cc1cc2ccccc2nc1I
OCc1cc2ccccc2nc1I
null
null
CO
Reduction
Reduction of aldehydes and ketones to alcohols
e7895795cd3f75445716c94697823c5929dcd4b5344525875fe75d36bca2f9d7
21bb81d5469aaaca71ab12c186bea4016451717fad8780cf288858a7d8fbc55a
c1ccc2ncccc2c1
[I;D1;H0:1]-[c:2](:[#7;a:3]:[c:4]):[c:5](-[CH;D2;+0:6]=[O;H0;D1;+0:7]):[c:8]>>[I;D1;H0:1]-[c:2](:[#7;a:3]:[c:4]):[c:5](-[CH2;D2;+0:6]-[OH;D1;+0:7]):[c:8]
84.4
[{"value": 84.0, "product": "OCC=1C(=NC2=CC=CC=C2C1)I", "details": "PERCENTYIELD", "is_desired": false}, {"value": 84.4, "product": "OCC=1C(=NC2=CC=CC=C2C1)I", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
0
CELSIUS
30
MINUTE
To a stirred solution of 2-iodo-3-quinolinecarboxaldehyde (595 mg, 2.10 mmol) in 40 mL of CH3OH at 0° C. was added NaBH4 (86 mg, 2.31 mmol), and the mixture was stirred at 0° C. for 30 min. After concentrating the mixture to approximately one-half of its original volume, water (30 mL) was added and the mixture was allo...
10.6084/m9.figshare.5104873.v1
null
Aldehyde
Primary alcohol
null
null
c1ccc2ncccc2c1
null
CO
0
0.5
O=Cc1cc2ccccc2nc1I>CO>OCc1cc2ccccc2nc1I
ord_dataset-02ee2261663048188cf6d85d2cc96e3f
ord-ec43efed8217448c8a53e867f44dee4e
O=C1CCC(=O)N1Cl.OCc1cc2ccccc2nc1I>>ClCc1cc2ccccc2nc1I
C(=O)(O)[O-].[Na+].OCC=1C(=NC2=CC=CC=C2C1)I.C1(=CC=CC=C1)P(C1=CC=CC=C1)C1=CC=CC=C1.ClN1C(CCC1=O)=O>>ClCC=1C(=NC2=CC=CC=C2C1)I
O=C1CCC(=O)N1[Cl:1].O[CH2:2][c:3]1[cH:4][c:5]2[cH:6][cH:7][cH:8][cH:9][c:10]2[n:11][c:12]1[I:13]>>[Cl:1][CH2:2][c:3]1[cH:4][c:5]2[cH:6][cH:7][cH:8][cH:9][c:10]2[n:11][c:12]1[I:13]
O=C1CCC(=O)N1Cl.OCc1cc2ccccc2nc1I
ClCc1cc2ccccc2nc1I
null
null
CN(C)C=O
Functional Group Interconversion
Alcohol to chloride_Other
f5aab884336f72e1370119b83151f1b95e31e5f052f259aee44382a5b9c14686
2aeb112456268e3e5dab065a03bb8fc4b6e8f1d07cae05ef26dce278613b654e
c1ccc2ncccc2c1
O-[CH2;D2;+0:1]-[c:2](:[c:3]):[c:4](-[I;D1;H0:5]):[#7;a:6]:[c:7].O=C1-C-C-C(=O)-N-1-[Cl;H0;D1;+0:8]>>[Cl;H0;D1;+0:8]-[CH2;D2;+0:1]-[c:2](:[c:3]):[c:4](-[I;D1;H0:5]):[#7;a:6]:[c:7]
84
[{"value": 84.0, "product": "ClCC=1C(=NC2=CC=CC=C2C1)I", "details": "PERCENTYIELD", "is_desired": false}]
-23
CELSIUS
1
HOUR
To a stirred mixture of 3-hydroxymethyl-2-iodoquinoline prepared in accordance with Example 10 above (350 mg, 1.23 mmol) and triphenylphosphine (483 mg, 1.84 mmol) in 10 mL of dry DMF at -23° C. was added N-chlorosuccinimide (246 mg, 1.84 mmol), and the mixture was stirred for 1 h at -23° C. After the addition of 40 mL...
10.6084/m9.figshare.5104873.v1
null
Tertiary amide.Tertiary amide.Primary alcohol
Primary halide
C1CCNC1
null
c1ccc2ncccc2c1
HO-
CN(C)C=O
-23
1
O=C1CCC(=O)N1Cl.OCc1cc2ccccc2nc1I>CN(C)C=O>ClCc1cc2ccccc2nc1I
ord_dataset-02ee2261663048188cf6d85d2cc96e3f
ord-86a11031d1d743c286db830c75a75df3
OCCCCCCCCO.[N-]=[N+]=[N-]>>[N-]=[N+]=NCCCCCCCCO
C1(=CC=C(C=C1)S(=O)(=O)Cl)C.C(CCCCCCCO)O.C(C)(=O)OCC.[N-]=[N+]=[N-].[Na+]>>N(=[N+]=[N-])CCCCCCCCO
O[CH2:4][CH2:5][CH2:6][CH2:7][CH2:8][CH2:9][CH2:10][CH2:11][OH:12].[N-:1]=[N+:2]=[N-:3]>>[N-:1]=[N+:2]=[N:3][CH2:4][CH2:5][CH2:6][CH2:7][CH2:8][CH2:9][CH2:10][CH2:11][OH:12]
OCCCCCCCCO.[N-]=[N+]=[N-]
[N-]=[N+]=NCCCCCCCCO
null
null
CN(C=O)C.N1=CC=CC=C1.C(Cl)Cl
Heteroatom Alkylation and Arylation
OtherReaction
b6ef7629d0f9b9d1438b20ee6805124558e67d10777a15184211800dd3e8b973
a446353c66aa2c48beeb0e3765234578855c107c1200bfc64cebc8b68d490616
null
O-[CH2;D2;+0:1]-[C:2]-[C:3].[N-;H0;D1:4]=[#7;+:5]=[N;-;D1;H0:6]>>[C:3]-[C:2]-[CH2;D2;+0:1]-[N;H0;D2;+0:4]=[#7;+:5]=[N;-;D1;H0:6]
null
[]
10
CELSIUS
null
null
14.65 g of 1,8-octanediol was dissolved in 80 g of pyridine, and cooled to 10° C. A solution of 19 g p-toluenesulfonyl chloride in 70 ml anhydrous methylene chloride was added dropwise thereto, and the mixture was heated gradually overnight for reaction. After water washing, the solvent was removed by distillation, to ...
10.6084/m9.figshare.5104873.v1
null
Primary alcohol
Azide
null
null
null
HO-
CN(C=O)C.N1=CC=CC=C1.C(Cl)Cl
10
null
OCCCCCCCCO.[N-]=[N+]=[N-]>CN(C=O)C.N1=CC=CC=C1.C(Cl)Cl>[N-]=[N+]=NCCCCCCCCO
ord_dataset-02ee2261663048188cf6d85d2cc96e3f
ord-dcadfe0e1eca4e47a8b88dad58fe8309
CCCCCCCCCCCCCCCC(=O)Cl.NCCO>>CCCCCCCCCCCCCCCC(=O)NCCO
NCCO.C(CCCCCCCCCCCCCCC)(=O)Cl>>C(CCCCCCCCCCCCCCC)(=O)NCCO
Cl[C:16]([CH2:15][CH2:14][CH2:13][CH2:12][CH2:11][CH2:10][CH2:9][CH2:8][CH2:7][CH2:6][CH2:5][CH2:4][CH2:3][CH2:2][CH3:1])=[O:17].[NH2:18][CH2:19][CH2:20][OH:21]>>[CH3:1][CH2:2][CH2:3][CH2:4][CH2:5][CH2:6][CH2:7][CH2:8][CH2:9][CH2:10][CH2:11][CH2:12][CH2:13][CH2:14][CH2:15][C:16](=[O:17])[NH:18][CH2:19][CH2:20][OH:21]
CCCCCCCCCCCCCCCC(=O)Cl.NCCO
CCCCCCCCCCCCCCCC(=O)NCCO
null
null
C(Cl)(Cl)Cl
Acylation
Acylation of Nitrogen Nucleophiles by Acyl/Thioacyl/Carbamoyl Halides and Analogs_OS
38143a4d536201990008fd6f2c68e6571a341d1c367481869fbbbe36cb038937
0e6ae078978e324f714e184b4f72826d4e3bf2d9ab22d6e9f73740af687be16f
null
Cl-[C;H0;D3;+0:1](=[O;D1;H0:2])-[C:3]-[C:4].[C:5]-[C:6]-[NH2;D1;+0:7]>>[C:4]-[C:3]-[C;H0;D3;+0:1](=[O;D1;H0:2])-[NH;D2;+0:7]-[C:6]-[C:5]
null
[]
null
null
null
null
2-Aminoethanol (13.76 g, 225.3 mmol) was dissolved in CHCl3 (750 ml). To the solution was added dropwise palmitoyl chloride (15.48 g, 56.3 mmol) with stirring under ice cooling. Thereafter, the mixture was stirred at room temperature for 19 hours. Conditions: See reaction.notes.procedure_details. Workup: Thereafter, th...
10.6084/m9.figshare.5104873.v1
null
Acyl halide.Primary amine
Secondary amide
null
null
null
HCl
C(Cl)(Cl)Cl
null
null
CCCCCCCCCCCCCCCC(=O)Cl.NCCO>C(Cl)(Cl)Cl>CCCCCCCCCCCCCCCC(=O)NCCO
ord_dataset-02ee2261663048188cf6d85d2cc96e3f
ord-146b31ec172a43eb9907724661a2a7f5
O=C(O)c1c(C(=O)O)c2ccccc2[nH]c1=O>>O=C1OC(=O)c2c1c(=O)[nH]c1ccccc21
C1=CC=C2C(=C1)C(=C(C(=O)N2)C(=O)O)C(=O)O.P(=O)(Cl)(Cl)Cl>>C1(OC(C=2C(NC=3C=CC=CC3C21)=O)=O)=O
O[C:2](=[O:1])[c:7]1[c:6]([C:4]([OH:3])=[O:5])[c:16]2[c:11]([nH:10][c:8]1=[O:9])[cH:12][cH:13][cH:14][cH:15]2>>[O:1]=[C:2]1[O:3][C:4](=[O:5])[c:6]2[c:7]1[c:8](=[O:9])[nH:10][c:11]1[cH:12][cH:13][cH:14][cH:15][c:16]21
O=C(O)c1c(C(=O)O)c2ccccc2[nH]c1=O
O=C1OC(=O)c2c1c(=O)[nH]c1ccccc21
null
null
C(Cl)(Cl)Cl
Miscellaneous
OtherReaction
6d51ecee017f321f8f64e74774842c818b7e862119463d0ba723ecec3dc0defe
22fb50577915472f1babb105381e408122dc09b3472eabb73e6e4daecfef90f6
O=C1OC(=O)c2c1c(=O)[nH]c1ccccc21
O-[C;H0;D3;+0:1](=[O;D1;H0:2])-[c:3](:[c:4]-[C:5](=[O;D1;H0:6])-[OH;D1;+0:7]):[c:8](=[O;D1;H0:9]):[#7;a:10]:[c:11]>>[O;D1;H0:2]=[C;H0;D3;+0:1]1-[O;H0;D2;+0:7]-[C:5](=[O;D1;H0:6])-[c:4]:[c:3]-1:[c:8](=[O;D1;H0:9]):[#7;a:10]:[c:11]
null
[]
null
null
null
null
A mixture of 2(1H)-Oxo-quinoline-3,4-dicarboxylic acid (2 g), phosphorous oxychloride (4 g) and dry chloroform (30 mL) was heated at reflux for 2 h. The solvent and excess reagents are removed in vacuo and the residue was treated with ice water to afford Furo[3,4-c]quinoline-1,3,4(5H)-trione as a yellow solid. Conditio...
10.6084/m9.figshare.5104873.v1
null
Carboxylic acid.Carboxylic acid
Anhydride
null
C1OCc2c1cnc1ccccc21
C1OCc2c1cnc1ccccc21
HO-
C(Cl)(Cl)Cl
null
null
O=C(O)c1c(C(=O)O)c2ccccc2[nH]c1=O>C(Cl)(Cl)Cl>O=C1OC(=O)c2c1c(=O)[nH]c1ccccc21
ord_dataset-02ee2261663048188cf6d85d2cc96e3f
ord-72ad1c3127de403cb4e6f9720380d252
O=C(O)c1c(C(=O)O)c2ccccc2[nH]c1=O.O=P(Cl)(Cl)Cl>>O=C1OC(=O)c2c1c(Cl)nc1ccccc21
C1=CC=C2C(=C1)C(=C(C(=O)N2)C(=O)O)C(=O)O.P(=O)(Cl)(Cl)Cl>>ClC1=NC=2C=CC=CC2C2=C1C(OC2=O)=O
O=[c:8]1[c:7]([C:2](O)=[O:1])[c:6]([C:4]([OH:3])=[O:5])[c:16]2[c:11]([nH:10]1)[cH:12][cH:13][cH:14][cH:15]2.O=P(Cl)(Cl)[Cl:9]>>[O:1]=[C:2]1[O:3][C:4](=[O:5])[c:6]2[c:7]1[c:8]([Cl:9])[n:10][c:11]1[cH:12][cH:13][cH:14][cH:15][c:16]21
O=C(O)c1c(C(=O)O)c2ccccc2[nH]c1=O.O=P(Cl)(Cl)Cl
O=C1OC(=O)c2c1c(Cl)nc1ccccc21
null
CN(C=O)C
null
Functional Group Interconversion
OtherReaction
88449996f48b41a26490a7b6400ea4cd93f48a4a70a9ba60fa3fe361b57838d0
91508a976437801004dea57b9103e0e1dbcc60fe3226a24e002cc00e886fc498
O=C1OC(=O)c2c1cnc1ccccc21
Cl-P(-Cl)(=O)-[Cl;H0;D1;+0:1].O-[C;H0;D3;+0:2](=[O;D1;H0:3])-[c:4]1:[c:5](-[C:6](=[O;D1;H0:7])-[OH;D1;+0:8]):[c:9]:[c:10](:[c:11]):[nH;D2;+0:12]:[c;H0;D3;+0:13]:1=O>>[Cl;H0;D1;+0:1]-[c;H0;D3;+0:13]1:[n;H0;D2;+0:12]:[c:10](:[c:11]):[c:9]:[c:5]2:[c:4]:1-[C;H0;D3;+0:2](=[O;D1;H0:3])-[O;H0;D2;+0:8]-[C:6]-2=[O;D1;H0:7]
null
[]
null
null
20
MINUTE
A mixture of 2(1H)-Oxo-quinoline-3,4-dicarboxylic acid (2.0 g), phosphorous oxychloride (10 mL) and 8 drops of dimethyl formamide was refluxed with stirring for 20 min. The reaction mixture was concentrated in vacuo and the residue treated with ice water to afford 4-Chloro-furo[3,4-c]quinoline-1,3-dione as a tan solid....
10.6084/m9.figshare.5104873.v1
null
Carboxylic acid.Carboxylic acid
Aromatic halide.Anhydride
c1cnc2ccccc2c1
c1ccc2c3c(cnc2c1)COC3
c1ccc2c3c(cnc2c1)COC3
HCl
CN(C=O)C
null
0.333333
O=C(O)c1c(C(=O)O)c2ccccc2[nH]c1=O.O=P(Cl)(Cl)Cl>CN(C=O)C>O=C1OC(=O)c2c1c(Cl)nc1ccccc21
ord_dataset-02ee2261663048188cf6d85d2cc96e3f
ord-fdab9219ef3743deb64f5cb01f5301ba
O=C1OC(=O)c2c1c(Cl)nc1ccccc21>>O=C1OCc2c(Cl)nc3ccccc3c21.O=C1OCc2c1c(Cl)nc1ccccc21
ClC1=NC=2C=CC=CC2C2=C1C(OC2=O)=O.[BH4-].[Na+]>>ClC1=NC=2C=CC=CC2C2=C1C(OC2)=O.ClC1=NC=2C=CC=CC2C2=C1COC2=O
[O:1]=[C:2]1[c:5]2[c:6]([Cl:7])[n:8][c:9]3[cH:10][cH:11][cH:12][cH:13][c:14]3[c:15]2[C:19](=[O:3])[O:18]1>>[O:1]=[C:2]1[O:3][CH2:4][c:5]2[c:6]([Cl:7])[n:8][c:9]3[cH:10][cH:11][cH:12][cH:13][c:14]3[c:15]21.[O:16]=[C:17]1[O:18][CH2:19][c:20]2[c:21]1[c:22]([Cl:23])[n:24][c:25]1[cH:26][cH:27][cH:28][cH:29][c:30]21
O=C1OC(=O)c2c1c(Cl)nc1ccccc21
O=C1OCc2c(Cl)nc3ccccc3c21.O=C1OCc2c1c(Cl)nc1ccccc21
null
null
O1CCCC1
Aromatic Heterocycle Formation
OtherReaction
a7d1bfb9ea6cea91c9519d869eed6cdf91b521b515ac8424e33152ff2a869fc9
5cea72f7edffe4fa1e3abc99f60e28cb4f6e73c6ce293be0fda0942048f6b571
O=C1OCc2c1cnc1ccccc21.O=C1OCc2cnc3ccccc3c21
[Cl;D1;H0:1]-[c:2]1:[#7;a:3]:[c:4](:[c:5]):[c:6](:[c:7]):[c;H0;D3;+0:8]2:[c;H0;D3;+0:9]:1-[C;H0;D3;+0:10](=[O;D1;H0:11])-[O;H0;D2;+0:12]-[C;H0;D3;+0:13]-2=[O;H0;D1;+0:14]>>[Cl;D1;H0:1]-[c:2]1:[#7;a:3]:[c:4](:[c:5]):[c:6](:[c:7]):[c;H0;D3;+0:8]2:[c;H0;D3;+0:9]:1-[C:15]-[O;H0;D2;+0:14]-[C;H0;D3;+0:10]-2=[O;D1;H0:11].[O;D...
null
[]
null
null
2
HOUR
To a well stirred mixture of 4-Chloro-furo[3,4-c]quinoline-1,3-dione (1.9 g) in tetrahydrofuran (10 mL) was added sodium borohydride (400 mg) at 0° C. and stirring was continued for 2 h. The reaction was then quenched with excess 6N HCl and water, and concentrated in vacuo to afford 4-Chloro-furo[3,4-c]quinolin-3(1H)-o...
10.6084/m9.figshare.5104873.v1
null
Anhydride.Ester.Ester
Aromatic halide.Ester.Ester
c1ccc2c3c(cnc2c1)COC3
c1ccc2c3c(cnc2c1)COC3.c1ccc2c3c(cnc2c1)COC3
c1ccc2c3c(cnc2c1)COC3.c1ccc2c3c(cnc2c1)COC3
Other
O1CCCC1
null
2
O=C1OC(=O)c2c1c(Cl)nc1ccccc21>O1CCCC1>O=C1OCc2c(Cl)nc3ccccc3c21.O=C1OCc2c1c(Cl)nc1ccccc21
ord_dataset-02ee2261663048188cf6d85d2cc96e3f
ord-3249a8af79024c0b8ff06a1dbe382196
O=C1OCc2c1c(Cl)nc1ccccc21>>O=C1OCc2c1cnc1ccccc21
ClC1=NC=2C=CC=CC2C2=C1C(OC2)=O.C(C)(=O)[O-].[Na+]>>C1OC(C=2C=NC=3C=CC=CC3C21)=O
Cl[c:7]1[c:6]2[c:5]([c:14]3[c:9]([n:8]1)[cH:10][cH:11][cH:12][cH:13]3)[CH2:4][O:3][C:2]2=[O:1]>>[O:1]=[C:2]1[O:3][CH2:4][c:5]2[c:6]1[cH:7][n:8][c:9]1[cH:10][cH:11][cH:12][cH:13][c:14]21
O=C1OCc2c1c(Cl)nc1ccccc21
O=C1OCc2c1cnc1ccccc21
null
[Pd]
C(C)(=O)O
Functional Group Interconversion
Aromatic dehalogenation
53dec7db27b62b5fafa395ddb5937d72a017015f1fcefa0c49887934c6f14472
56de34d4a44cb25d9380269ee5e138b0f24b40a3a0db22c5508049dc775a861f
O=C1OCc2c1cnc1ccccc21
Cl-[c;H0;D3;+0:1](:[#7;a:2]:[c:3]):[c:4]1:[c:5]-[C:6]-[#8:7]-[C:8]-1=[O;D1;H0:9]>>[O;D1;H0:9]=[C:8]1-[#8:7]-[C:6]-[c:5]:[c:4]-1:[cH;D2;+0:1]:[#7;a:2]:[c:3]
null
[]
null
null
2
HOUR
A mixture of 4-Chloro-furo[3,4-c]quinolin-3(1H)-one (500 mg), 10% Palladium on carbon (100 mg) and sodium acetate (500 mg) in 20 mL of acetic acid was hydrogenated at atmospheric pressure for 2 h. After filtration through celite, the solvent was removed in vacuo, and the residue was taken up in methylene chloride. Afte...
10.6084/m9.figshare.5104873.v1
null
Aromatic halide
null
c1ccc2c3c(cnc2c1)COC3
c1ccc2c3c(cnc2c1)COC3
c1ccc2c3c(cnc2c1)COC3
Other
[Pd].C(C)(=O)O
null
2
O=C1OCc2c1c(Cl)nc1ccccc21>[Pd].C(C)(=O)O>O=C1OCc2c1cnc1ccccc21
ord_dataset-02ee2261663048188cf6d85d2cc96e3f
ord-273c5eb135a04e95a9a37fa897521272
Nc1ccccc1.O=C1OCc2c1cnc1ccccc21>>O=C1c2cnc3ccccc3c2CN1c1ccccc1
C1OC(C=2C=NC=3C=CC=CC3C21)=O.NC1=CC=CC=C1>>C1(=CC=CC=C1)N1C(C=2C=NC=3C=CC=CC3C2C1)=O
[NH2:14][c:15]1[cH:16][cH:17][cH:18][cH:19][cH:20]1.O1[C:2](=[O:1])[c:3]2[cH:4][n:5][c:6]3[cH:7][cH:8][cH:9][cH:10][c:11]3[c:12]2[CH2:13]1>>[O:1]=[C:2]1[c:3]2[cH:4][n:5][c:6]3[cH:7][cH:8][cH:9][cH:10][c:11]3[c:12]2[CH2:13][N:14]1[c:15]1[cH:16][cH:17][cH:18][cH:19][cH:20]1
Nc1ccccc1.O=C1OCc2c1cnc1ccccc21
O=C1c2cnc3ccccc3c2CN1c1ccccc1
null
null
CCCCCC
Acylation
OtherReaction
71180cd65f60a07d8655a227fcf71b0eeb0e4fa552b6e708f78f901daefc935e
ab33057bb8fb2c9dad5b018a4f87637d8c1c3babde576dc33e825e140481b8d2
O=C1c2cnc3ccccc3c2CN1c1ccccc1
[NH2;D1;+0:1]-[c:2](:[c:3]):[c:4].[O;D1;H0:5]=[C;H0;D3;+0:6]1-O-[CH2;D2;+0:7]-[c:8]2:[c:9]:[c:10]:[#7;a:11]:[c:12]:[c:13]:2-1>>[O;D1;H0:5]=[C;H0;D3;+0:6]1-[N;H0;D3;+0:1](-[c:2](:[c:3]):[c:4])-[CH2;D2;+0:7]-[c:8]2:[c:9]:[c:10]:[#7;a:11]:[c:12]:[c:13]:2-1
null
[]
null
null
null
null
A mixture Furo[3,4-c]quinolin-3(1H)-one (100 mg) and aniline (2 mL) was heated at 180° C. for 5 min. After cooling to room temperature the mixture was slowly diluted with hexane and the resulting product was collected and washed with hexane to afford 2-Phenyl-pyrrolo[3,4-c]quinolin-3(1H)-one. Conditions: See reaction.n...
10.6084/m9.figshare.5104873.v1
null
Ester.Primary amine
Tertiary amide
c1ccc2c3c(cnc2c1)COC3
c1ccc2c3c(cnc2c1)C[NH]C3
c1ccc2c3c(cnc2c1)C[NH]C3.c1ccccc1
HO-
CCCCCC
null
null
Nc1ccccc1.O=C1OCc2c1cnc1ccccc21>CCCCCC>O=C1c2cnc3ccccc3c2CN1c1ccccc1
ord_dataset-02ee2261663048188cf6d85d2cc96e3f
ord-85ced26261244ccdada566c55d307030
O=C(OO)c1cccc(Cl)c1.O=C1c2cnc3ccccc3c2CN1c1ccccc1>>O=C1c2c(c3ccccc3[nH]c2=O)CN1c1ccccc1
C1(=CC=CC=C1)N1C(C=2C=NC=3C=CC=CC3C2C1)=O.ClC1=CC(=CC=C1)C(=O)OO>>C1(=CC=CC=C1)N1C(C=2C(NC=3C=CC=CC3C2C1)=O)=O
O=C(O[OH:13])c1cccc(Cl)c1.[O:1]=[C:2]1[c:3]2[c:4]([c:5]3[cH:6][cH:7][cH:8][cH:9][c:10]3[n:11][cH:12]2)[CH2:14][N:15]1[c:16]1[cH:17][cH:18][cH:19][cH:20][cH:21]1>>[O:1]=[C:2]1[c:3]2[c:4]([c:5]3[cH:6][cH:7][cH:8][cH:9][c:10]3[nH:11][c:12]2=[O:13])[CH2:14][N:15]1[c:16]1[cH:17][cH:18][cH:19][cH:20][cH:21]1
O=C(OO)c1cccc(Cl)c1.O=C1c2cnc3ccccc3c2CN1c1ccccc1
O=C1c2c(c3ccccc3[nH]c2=O)CN1c1ccccc1
null
null
C(Cl)Cl
Miscellaneous
OtherReaction
208fbd7481ea3db38e97849b66ab914150e3b853920943719393ba37740d2426
98b338a9d01476c0929fd5672e7509121bfe69600fd72e4d1cc6f1782e2d05d9
O=C1c2c(c3ccccc3[nH]c2=O)CN1c1ccccc1
Cl-c1:c:c:c:c(-C(=O)-O-[OH;D1;+0:1]):c:1.[O;D1;H0:2]=[C:3]1-[#7:4](-[c:5])-[C:6]-[c:7]2:[c:8]:[c:9](:[c:10]):[n;H0;D2;+0:11]:[cH;D2;+0:12]:[c:13]:2-1>>[O;D1;H0:2]=[C:3]1-[#7:4](-[c:5])-[C:6]-[c:7]2:[c:8]:[c:9](:[c:10]):[nH;D2;+0:11]:[c;H0;D3;+0:12](=[O;H0;D1;+0:1]):[c:13]:2-1
null
[]
50
CELSIUS
24
HOUR
A mixture of 2-Phenyl-pyrrolo[3,4-c]quinolin-3(1H)-one (60 mg), and m-chloroperbenzoic acid (105 mg) in 3 mL of methylene chloride was kept at room temperature for 24 h. The mixture was diluted with methylene chloride and washed with sodium carbonate solution. The organic layer was dried over magnesium sulfate and the ...
10.6084/m9.figshare.5104873.v1
null
Aromatic halide.Peroxide
null
c1ccccc1.c1ccc2c3c(cnc2c1)C[NH]C3
C1NCc2c1cnc1ccccc21
C1NCc2c1cnc1ccccc21.c1ccccc1
HCl
C(Cl)Cl
50
24
O=C(OO)c1cccc(Cl)c1.O=C1c2cnc3ccccc3c2CN1c1ccccc1>C(Cl)Cl>O=C1c2c(c3ccccc3[nH]c2=O)CN1c1ccccc1
ord_dataset-02ee2261663048188cf6d85d2cc96e3f
ord-bff13585dd6045868860fbe58d6d87e2
C=O.CC1(C)OC(=O)CC(=O)O1.c1ccncc1>>CC1(C)OC(=O)C(C[n+]2ccccc2)=C(O)O1.[OH-]
CC1(OC(=O)CC(=O)O1)C.N1=CC=CC=C1.C=O>>[OH-].OC1=C(C(OC(O1)(C)C)=O)C[N+]1=CC=CC=C1
[CH2:8]=[O:18].[CH3:1][C:2]1([CH3:3])[O:4][C:5](=[O:6])[CH2:7][C:15](=[O:16])[O:17]1.[n:9]1[cH:10][cH:11][cH:12][cH:13][cH:14]1>>[CH3:1][C:2]1([CH3:3])[O:4][C:5](=[O:6])[C:7]([CH2:8][n+:9]2[cH:10][cH:11][cH:12][cH:13][cH:14]2)=[C:15]([OH:16])[O:17]1.[OH-:18]
C=O.CC1(C)OC(=O)CC(=O)O1.c1ccncc1
CC1(C)OC(=O)C(C[n+]2ccccc2)=C(O)O1.[OH-]
null
null
null
Heteroatom Alkylation and Arylation
OtherReaction
46efea35d93f5283d05aaf0b002fc1811445bc3deb29e1ea43f74a2419383191
2b876f2a10baccbae056058d76912619de176012ba4b118b915592ac5ebf1bc3
O=C1OCOC=C1C[n+]1ccccc1
[CH2;D1;+0:1]=[O;H0;D1;+0:2].[O;D1;H0:3]=[C:4]1-[#8:5]-[C:6]-[#8:7]-[C;H0;D3;+0:8](=[O;H0;D1;+0:9])-[CH2;D2;+0:10]-1.[c:11]:[c:12]:[n;H0;D2;+0:13]:[c:14]:[c:15]>>[O;D1;H0:3]=[C:4]1-[#8:5]-[C:6]-[#8:7]-[C;H0;D3;+0:8](-[OH;D1;+0:9])=[C;H0;D3;+0:10]-1-[CH2;D2;+0:1]-[n+;H0;D3:13](:[c:12]:[c:11]):[c:14]:[c:15].[OH-;D0:2]
91.6
[{"value": 91.6, "product": "[OH-].OC1=C(C(OC(O1)(C)C)=O)C[N+]1=CC=CC=C1", "details": "PERCENTYIELD", "is_desired": false}]
null
null
1
HOUR
Meldrum's acid (20 g, 0.139 mol) was dissolved in 50 ml of pyridine. The solution immediately turned yellow and was somewhat exothermic. After dissolution was complete, a 37% aqueous solution of formaldehyde (10.4 ml, 0.139 mol) was added in one portion. The reaction mixture was allowed to stir for one hour under argon...
10.6084/m9.figshare.5104873.v1
null
Formaldehyde.Ester.Ester
Ester.Ether.Enol
C1COCOC1.c1ccncc1
C1=COCOC1.C1=CC=[NH+]C=C1
C1=COCOC1.C1=CC=[NH+]C=C1
null
null
null
1
C=O.CC1(C)OC(=O)CC(=O)O1.c1ccncc1>>CC1(C)OC(=O)C(C[n+]2ccccc2)=C(O)O1.[OH-]
ord_dataset-02ee2261663048188cf6d85d2cc96e3f
ord-e195c176d6b849b682dd3bfd3a2e2e17
O=[N+]([O-])c1ccc2nc(S)sc2c1>>Nc1ccc2nc(S)sc2c1
S.[Na].[N+](=O)([O-])C1=CC2=C(N=C(S2)S)C=C1>>NC1=CC2=C(N=C(S2)S)C=C1
O=[N+:1]([O-])[c:2]1[cH:3][cH:4][c:5]2[n:6][c:7]([SH:8])[s:9][c:10]2[cH:11]1>>[NH2:1][c:2]1[cH:3][cH:4][c:5]2[n:6][c:7]([SH:8])[s:9][c:10]2[cH:11]1
O=[N+]([O-])c1ccc2nc(S)sc2c1
Nc1ccc2nc(S)sc2c1
null
null
O
Reduction
Reduction of nitro groups to amines
bbc242b150a51e69d3ad1caaa391f4422710431b398dcb880555f476706790be
7b0317532ea57a4fcedc1efc3e3c22eb5238d1c8330da53d4f9801fc2391f567
c1ccc2scnc2c1
O=[N+;H0;D3:1](-[O-])-[c:2](:[c:3]):[c:4]:[c:5]:[#16;a:6]>>[#16;a:6]:[c:5]:[c:4]:[c:2](-[NH2;D1;+0:1]):[c:3]
null
[]
20
CELSIUS
4
HOUR
132 Parts of sodium hydrogen sulphide was dissolved in 400 parts of water, and stirred at 20° C. 53 Parts of 6-nitro-2-mercaptobenzothiazole, prepared as described previously herein, was added over 10 minutes; the reaction mixture was then heated to 110° C., and stirred whilst boiling the mixture under reflux condition...
10.6084/m9.figshare.5104873.v1
null
Nitro group
Primary amine
null
null
c1ccc2scnc2c1
Other
O
20
4
O=[N+]([O-])c1ccc2nc(S)sc2c1>O>Nc1ccc2nc(S)sc2c1
ord_dataset-02ee2261663048188cf6d85d2cc96e3f
ord-8d7febe7112045ef956a7488caf062d7
CCCCCC=CCC=CCCCCCCCC(=O)Cl>>CCCCCCCCC=CCCCCCCCC(=O)Cl
C(CCCCCCCC=CCC=CCCCCC)(=O)Cl.C(CCCCCCCC=CCCCCCCCC)(=O)O>>C(CCCCCCCC=CCCCCCCCC)(=O)Cl
[CH3:1][CH2:2][CH2:3][CH2:4][CH2:5][CH:6]=[CH:7][CH2:8][CH:9]=[CH:10][CH2:11][CH2:12][CH2:13][CH2:14][CH2:15][CH2:16][CH2:17][C:18](=[O:19])[Cl:20]>>[CH3:1][CH2:2][CH2:3][CH2:4][CH2:5][CH2:6][CH2:7][CH2:8][CH:9]=[CH:10][CH2:11][CH2:12][CH2:13][CH2:14][CH2:15][CH2:16][CH2:17][C:18](=[O:19])[Cl:20]
CCCCCC=CCC=CCCCCCCCC(=O)Cl
CCCCCCCCC=CCCCCCCCC(=O)Cl
null
null
null
Reduction
Hydrogenation (double to single)
0bc3968b35f0839c230afb4215314da278abd4e1f10e42ec3012c5512de49ea5
312e9350dcad67590617294c0eb017edf0b9fbfe6133c06a3f393b871a889092
null
[C:1]-[C:2]=[C:3]-[C:4]-[CH;D2;+0:5]=[CH;D2;+0:6]-[C:7]-[C:8]>>[C:1]-[C:2]=[C:3]-[C:4]-[CH2;D2;+0:5]-[CH2;D2;+0:6]-[C:7]-[C:8]
85
[{"value": 85.0, "product": "C(CCCCCCCC=CCCCCCCCC)(=O)Cl", "details": "PERCENTYIELD", "is_desired": false}]
null
null
null
null
Octadec-9-enoyl chloride (25.5 parts, boiling point 160°-180° C. at 0.12 Torr, 85% yield) was prepared from 28.1 parts of octadec-9-enoic acid using the procedure described in part A of Example 3 for the preparation of octadec-9,12-dienoyl chloride. Conditions: See reaction.notes.procedure_details.
10.6084/m9.figshare.5104873.v1
null
null
null
null
null
null
null
null
null
null
CCCCCC=CCC=CCCCCCCCC(=O)Cl>>CCCCCCCCC=CCCCCCCCC(=O)Cl
ord_dataset-02ee2261663048188cf6d85d2cc96e3f
ord-e42ee508cabb475f98ffdb624b16f4b6
NS(=O)(=O)c1ccccc1.c1ccncc1.c1ccncc1>>O=S1N=C(S(=O)(=O)c2ccccc2)c2ccccc21
C1(=CC=CC=C1)S(=O)(=O)N.N1=CC=CC=C1.N1=CC=CC=C1.C(Cl)(Cl)(Cl)Cl.Cl>>C1(=CC=CC=C1)S(=O)(=O)C1=NS(C2=C1C=CC=C2)=O
[O:1]=[S:2]([NH2:3])(=[O:7])[c:8]1[cH:9][cH:10][cH:11][cH:12][cH:13]1.c1c[cH:4][cH:14][cH:19]n1.c1n[cH:15][cH:16][cH:17][cH:18]1>>[O:1]=[S:2]1[N:3]=[C:4]([S:5](=[O:6])(=[O:7])[c:8]2[cH:9][cH:10][cH:11][cH:12][cH:13]2)[c:14]2[cH:15][cH:16][cH:17][cH:18][c:19]21
NS(=O)(=O)c1ccccc1.c1ccncc1.c1ccncc1
O=S1N=C(S(=O)(=O)c2ccccc2)c2ccccc21
null
null
C(C)(=O)O.CO
Functional Group Interconversion
OtherReaction
eda97579b08027eca375e0a357e16f3fb2bb4c16016c7597519e65665f0d76d1
3e2c31b10cef57bda3459f8766fa5304a52d531571e8ab0c8709da1016e8804b
O=S1N=C(S(=O)(=O)c2ccccc2)c2ccccc21
[NH2;D1;+0:1]-[S;H0;D4;+0:2](=[O;D1;H0:3])(=[O;H0;D1;+0:4])-[c;H0;D3;+0:5](:[c:6]:[c:7]):[c:8]:[c:9].[cH;D2;+0:10]1:[cH;D2;+0:11]:n:c:c:[cH;D2;+0:12]:1.[c:13]1:[c:14]:[cH;D2;+0:15]:c:n:[cH;D2;+0:16]:1>>[O;D1;H0:3]=[S;H0;D3;+0:2]1-[N;H0;D2;+0:1]=[C;H0;D3;+0:12](-[#16:17](=[O;D1;H0:18])(=[O;H0;D1;+0:4])-[c;H0;D3;+0:5](:[...
null
[]
null
null
45
MINUTE
31.44 G. (0.2 mole) of benzenesulfonamide was dissolved in 80 ml. of dry pyridine to obtain a clear, straw-colored solution, which was placed in a cold water bath. To this pyridine solution was added the carbon tetrachloride solution produced in Part B above. An exothermic reaction ensued with formation of a white slur...
10.6084/m9.figshare.5104873.v1
null
Sulfonamide
Sulfone
c1ccccc1.c1ccncc1.c1ccncc1
c1ccccc1.c1ccc2sncc2c1
c1ccccc1.c1ccc2sncc2c1
Other
C(C)(=O)O.CO
null
0.75
NS(=O)(=O)c1ccccc1.c1ccncc1.c1ccncc1>C(C)(=O)O.CO>O=S1N=C(S(=O)(=O)c2ccccc2)c2ccccc21
ord_dataset-02ee2261663048188cf6d85d2cc96e3f
ord-832f1035ccee4e16b54fec29013e82eb
CCOC(=O)C1CCN(C(=O)C2CC2)CC1>>O=C(C1CC1)N1CCC(CO)CC1
[BH4-].[Li+].C1(CC1)C(=O)N1CCC(CC1)C(=O)OCC.B(OC)(OC)OC>>C1(CC1)C(=O)N1CCC(CC1)CO
CCO[C:10]([CH:9]1[CH2:8][CH2:7][N:6]([C:2](=[O:1])[CH:3]2[CH2:4][CH2:5]2)[CH2:13][CH2:12]1)=[O:11]>>[O:1]=[C:2]([CH:3]1[CH2:4][CH2:5]1)[N:6]1[CH2:7][CH2:8][CH:9]([CH2:10][OH:11])[CH2:12][CH2:13]1
CCOC(=O)C1CCN(C(=O)C2CC2)CC1
O=C(C1CC1)N1CCC(CO)CC1
null
null
O.O1CCCC1
Reduction
Reduction of ester to primary alcohol
21d61543c6ec8a8cebe1b3ef55ef3dd20acbf79a4f1c12a7fb51e32be7a3248a
1fbcd628a0426673c5d10aa49a977cd2d1ae02a8cdf57bbb10d94aa03a94e937
O=C(C1CC1)N1CCCCC1
C-C-O-[C;H0;D3;+0:1](=[O;H0;D1;+0:2])-[C:3](-[C:4])-[C:5]>>[C:4]-[C:3](-[CH2;D2;+0:1]-[OH;D1;+0:2])-[C:5]
63.7
[{"value": 63.7, "product": "C1(CC1)C(=O)N1CCC(CC1)CO", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
48
HOUR
A solution of 1-(cyclopropylcarbonyl)-4-carboethoxy piperidine (35 g, 156 mmol) in anhydrous tetrahydrofuran (350 mL) was stirred at ambient temperature under a nitrogen atmosphere. A solution of lithium borohydride in tetrahydrofuran (2M, 78 mL, 156 mmol) was added dropwise. Trimethyl borate (1.77 mL, 15.7 mmol) was a...
10.6084/m9.figshare.5104873.v1
null
Ester
Primary alcohol
null
null
C1CC1.C1CC[NH]CC1
HO-
O.O1CCCC1
null
48
CCOC(=O)C1CCN(C(=O)C2CC2)CC1>O.O1CCCC1>O=C(C1CC1)N1CCC(CO)CC1
ord_dataset-02ee2261663048188cf6d85d2cc96e3f
ord-4a3dc28a00854038bc8f00c5c9d2d330
O=C(CC1CCN(CC2CC2)CC1)c1ccc(F)cc1.[Br][Mg][c]1ccccc1>>OC(CC1CCN(CC2CC2)CC1)(c1ccccc1)c1ccc(F)cc1
[NH4+].[Cl-].C1(=CC=CC=C1)[Mg]Br.CCOCC.C1(CC1)CN1CCC(CC1)CC(=O)C1=CC=C(C=C1)F>>C1(CC1)CN1CCC(CC1)CC(O)(C1=CC=CC=C1)C1=CC=C(C=C1)F
[O:1]=[C:2]([CH2:3][CH:4]1[CH2:5][CH2:6][N:7]([CH2:8][CH:9]2[CH2:10][CH2:11]2)[CH2:12][CH2:13]1)[c:20]1[cH:21][cH:22][c:23]([F:24])[cH:25][cH:26]1.[Br][Mg][c:14]1[cH:15][cH:16][cH:17][cH:18][cH:19]1>>[OH:1][C:2]([CH2:3][CH:4]1[CH2:5][CH2:6][N:7]([CH2:8][CH:9]2[CH2:10][CH2:11]2)[CH2:12][CH2:13]1)([c:14]1[cH:15][cH:16][c...
O=C(CC1CCN(CC2CC2)CC1)c1ccc(F)cc1.[Br][Mg][c]1ccccc1
OC(CC1CCN(CC2CC2)CC1)(c1ccccc1)c1ccc(F)cc1
null
null
O1CCCC1
C-C Coupling
Grignard from ketone to alcohol
181fdd58eba73242b2de454099edbf422e18f2a0a3f78d67208494cf1d83905c
5854166cd4ea706bc07d74dc79eb8f4a990bc6c5eacbf0ca947d88ee86e78fdf
c1ccc(C(CC2CCN(CC3CC3)CC2)c2ccccc2)cc1
[Br]-[Mg]-[c;H0;D3;+0:1](:[c:2]:[c:3]):[c:4]:[c:5].[C:6]-[C:7]-[C;H0;D3;+0:8](=[O;H0;D1;+0:9])-[c:10](:[c:11]):[c:12]>>[C:6]-[C:7]-[C;H0;D4;+0:8](-[OH;D1;+0:9])(-[c:10](:[c:11]):[c:12])-[c;H0;D3;+0:1](:[c:2]:[c:3]):[c:4]:[c:5]
null
[]
null
null
null
null
1-(Cyclopropylmethyl)-4-(2'-(4"-fluorophenyl)-2'-oxoethyl)piperidine (Example 429, 1.0 g, 3.6 mmol) was mixed with dry tetrahydrofuran (10 mL). A solution of phenyl magnesium bromide in ether (3.0M, 3 mL, 9 mmol) was added with stirring. The reaction mixture was stirred for 24 h; poured onto a saturated NH4Cl solution ...
10.6084/m9.figshare.5104873.v1
null
Magnesium halide.Ketone
Tertiary alcohol
c1ccccc1
c1ccccc1
C1CC[NH]CC1.C1CC1.c1ccccc1.c1ccccc1
Br-.Mg
O1CCCC1
null
null
O=C(CC1CCN(CC2CC2)CC1)c1ccc(F)cc1.[Br][Mg][c]1ccccc1>O1CCCC1>OC(CC1CCN(CC2CC2)CC1)(c1ccccc1)c1ccc(F)cc1
ord_dataset-02ee2261663048188cf6d85d2cc96e3f
ord-a1afae4c809643d59843e94bfd9a4e3d
Fc1cc[c]([Mg][Br])cc1.Fc1ccc(OCC2CCN(CC3CC3)CC2)cc1>>OC(CC1CCN(CC2CC2)CC1)(c1ccc(F)cc1)c1ccc(F)cc1
C1(CC1)CN1CCC(CC1)COC1=CC=C(C=C1)F.FC1=CC=C(C=C1)[Mg]Br.O1CCCC1>>C1(CC1)CN1CCC(CC1)CC(O)(C1=CC=C(C=C1)F)C1=CC=C(C=C1)F
[Br][Mg][c:21]1[cH:22][cH:23][c:24]([F:25])[cH:26][cH:27]1.[O:1]([c:2]1[cH:15][cH:16][c:17]([F:18])[cH:19][cH:20]1)[CH2:3][CH:4]1[CH2:5][CH2:6][N:7]([CH2:8][CH:9]2[CH2:10][CH2:11]2)[CH2:12][CH2:13]1>>[OH:1][C:2]([CH2:3][CH:4]1[CH2:5][CH2:6][N:7]([CH2:8][CH:9]2[CH2:10][CH2:11]2)[CH2:12][CH2:13]1)([c:14]1[cH:15][cH:16][c...
Fc1cc[c]([Mg][Br])cc1.Fc1ccc(OCC2CCN(CC3CC3)CC2)cc1
OC(CC1CCN(CC2CC2)CC1)(c1ccc(F)cc1)c1ccc(F)cc1
null
null
null
C-C Coupling
OtherReaction
a75c9d378418ce52c555e34277b111f09bd2b02a0be0a5d1bbdee04e0640cc07
25f603babd45839717eb7b0e561ce156c6a60169be5fa25d8aaf6c4c8ba84b37
c1ccc(C(CC2CCN(CC3CC3)CC2)c2ccccc2)cc1
[Br]-[Mg]-[c;H0;D3;+0:1](:[c:2]:[c:3]):[c:4]:[c:5].[C:6]-[C:7](-[CH2;D2;+0:8]-[O;H0;D2;+0:9]-[c;H0;D3;+0:10]1:[cH;D2;+0:11]:[c:12]:[c:13]:[c:14]:[cH;D2;+0:15]:1)-[C:16]>>[C:6]-[C:7](-[CH2;D2;+0:8]-[C;H0;D4;+0:10](-[OH;D1;+0:9])(-[c:17]1:[cH;D2;+0:11]:[c:12]:[c:13]:[c:14]:[cH;D2;+0:15]:1)-[c;H0;D3;+0:1](:[c:2]:[c:3]):[c...
null
[]
null
null
null
null
Following the procedure described for Example 547, the compound of Example 429 (1.0 g, 3.6 mmol) was reacted a solution of 4-fluorophenylmagnesium bromide in tetrahydrofuran (1.0M, 9 mL, 9 mmol) to give the title compound, a solid (1.1 g): mp 119°-121° C.; Anal.: Calcd for C23H27F2NO.0.5H2O: C, 72.60, H, 7.41, N, 3.68,...
10.6084/m9.figshare.5104873.v1
null
Magnesium halide.Ether
Tertiary alcohol
c1ccccc1.c1ccccc1
c1ccccc1.c1ccccc1
C1CC[NH]CC1.C1CC1.c1ccccc1.c1ccccc1
Br-.Mg
null
null
null
Fc1cc[c]([Mg][Br])cc1.Fc1ccc(OCC2CCN(CC3CC3)CC2)cc1>>OC(CC1CCN(CC2CC2)CC1)(c1ccc(F)cc1)c1ccc(F)cc1
ord_dataset-02ee2261663048188cf6d85d2cc96e3f
ord-4a783f44e5724f2c918ab22504b47e95
CCOC(=O)c1ccc(Br)cc1.Fc1ccc(Br)cc1>>CCOC(=O)c1ccc(-c2ccc(F)cc2)cc1
BrC1=CC=C(C=C1)F.BrC1=CC=C(C(=O)OCC)C=C1>>C(C)OC(C1=CC=C(C=C1)C1=CC=C(C=C1)F)=O
Br[c:9]1[cH:8][cH:7][c:6]([C:4]([O:3][CH2:2][CH3:1])=[O:5])[cH:18][cH:17]1.Br[c:10]1[cH:11][cH:12][c:13]([F:14])[cH:15][cH:16]1>>[CH3:1][CH2:2][O:3][C:4](=[O:5])[c:6]1[cH:7][cH:8][c:9](-[c:10]2[cH:11][cH:12][c:13]([F:14])[cH:15][cH:16]2)[cH:17][cH:18]1
CCOC(=O)c1ccc(Br)cc1.Fc1ccc(Br)cc1
CCOC(=O)c1ccc(-c2ccc(F)cc2)cc1
null
null
null
C-C Coupling
Negishi
c762f793fad28f910ecef7baabecb58fd3905901ac0af2c73542eba7e0faa33e
a7a4ce9a92e2f8a62d28956a69a5cc384426ab72416e87d68c6a3feb23c22d66
c1ccc(-c2ccccc2)cc1
Br-[c;H0;D3;+0:1](:[c:2]:[c:3]):[c:4]:[c:5].Br-[c;H0;D3;+0:6](:[c:7]:[c:8]):[c:9]:[c:10]>>[c:8]:[c:7]:[c;H0;D3;+0:6](-[c;H0;D3;+0:1](:[c:2]:[c:3]):[c:4]:[c:5]):[c:9]:[c:10]
null
[]
null
null
null
null
Using the procedure described for Example 551, 4-bromofluorobenzene (1.75 g, 10 mmol) was metallated and coupled with ethyl 4-bromobenzoate (2.28 g, 10 mmol) to give the title compound after chromatography (ethyl acetate-hexanes (1:9) (0.7 g)): 1H-NMR (CDCl3, 300 MHz): 8.1 (d, 2H, J=8), 7.65-7.5 (m, 4H), 7.15 (t, 2H, J...
10.6084/m9.figshare.5104873.v1
null
Aromatic halide.Aromatic halide
null
c1ccccc1.c1ccccc1
c1ccccc1.c1ccccc1
c1ccccc1.c1ccccc1
Br-
null
null
null
CCOC(=O)c1ccc(Br)cc1.Fc1ccc(Br)cc1>>CCOC(=O)c1ccc(-c2ccc(F)cc2)cc1
ord_dataset-02ee2261663048188cf6d85d2cc96e3f
ord-29553a4becdf4d34adb98b5354444849
CC(C)(C)[C@@]1(O)CCN2C[C@@H]3c4ccccc4CCc4cccc(c43)[C@H]2C1.NC(CO)(CO)CO.O=C(CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1)c1ccc(F)cc1>>NCCc1ccc(O)c(O)c1
C1CN(CCC12C(=O)NCN2C3=CC=CC=C3)CCCC(=O)C4=CC=C(C=C4)F.CC(C)(C)[C@]1(CCN2C[C@@H]3C=4C=CC=CC4CCC5=C3C(=CC=C5)[C@H]2C1)O.C(C(CO)(CO)N)O.Cl.[Na+].[Cl-].[Mg+2].[Cl-].[Cl-]>>NCCC1=CC(O)=C(O)C=C1
CC(C)(C)[C@@]1([OH:8])CCN2C[C@@H]3c4ccccc4CCc4cccc(c43)[C@H]2C1.OCC(CO)(C[OH:10])[NH2:1].O=C1NCN(c2ccccc2)C12CCN(C[CH2:2]C[C:3](=O)[c:4]1[cH:5][cH:6][c:7](F)[cH:9][cH:11]1)CC2>>[NH2:1][CH2:2][CH2:3][c:4]1[cH:5][cH:6][c:7]([OH:8])[c:9]([OH:10])[cH:11]1
CC(C)(C)[C@@]1(O)CCN2C[C@@H]3c4ccccc4CCc4cccc(c43)[C@H]2C1.NC(CO)(CO)CO.O=C(CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1)c1ccc(F)cc1
NCCc1ccc(O)c(O)c1
null
null
null
Heteroatom Alkylation and Arylation
OtherReaction
955cea429a112d006f45729daa4c51fb4b3bbd7e792f3382a8f0f119928ce8dd
509e1d9aee36ecf6808e5844cd4b578cf1f67efac6379dd129f5b1e3ddd51fb2
c1ccccc1
C-C(-C)(-C)-[C@@]1(-[OH;D1;+0:1])-C-C-N2-C-[C@H]3-c4:c:c:c:c:c:4-C-C-c4:c:c:c:c(:c:4-3)-[C@@H]-2-C-1.F-[c;H0;D3;+0:2]1:[c:3]:[c:4]:[c:5](-[C;H0;D3;+0:6](=O)-C-[CH2;D2;+0:7]-C-N2-C-C-C3(-C-C-2)-C(=O)-N-C-N-3-c2:c:c:c:c:c:2):[c:8]:[cH;D2;+0:9]:1.O-C-C(-[NH2;D1;+0:10])(-C-O)-C-[OH;D1;+0:11]>>[NH2;D1;+0:10]-[CH2;D2;+0:7]-[...
null
[]
null
null
15
MINUTE
0.5 mL aliquots of the membrane preparation were incubated with unlabeled drugs, and 0.15 nM [3H]spiperone in a final volume of 1 mL containing 50 mM Tris HCl, 120 mM NaCl and 1 mM MgCl2 (pH 7.7). Nonspecific binding was measured in the presence of 100 nM (+)-butaclamol. After 15 minutes of incubation at 37° C., sample...
10.6084/m9.figshare.5104873.v1
null
Aromatic halide.Ketone.Secondary amide.Primary alcohol.Primary alcohol.Primary alcohol.Tertiary alcohol.Primary amine.Tertiary amine.Tertiary amine.Tertiary amine
Aromatic alcohol.Aromatic alcohol.Primary amine
c1ccc2c(c1)CCc1cccc3c1[C@@H]2CN1CCCC[C@H]31.c1ccccc1.C1CC2(CCN1)CNCN2.c1ccccc1
c1ccccc1
c1ccccc1
HF
null
null
0.25
CC(C)(C)[C@@]1(O)CCN2C[C@@H]3c4ccccc4CCc4cccc(c43)[C@H]2C1.NC(CO)(CO)CO.O=C(CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1)c1ccc(F)cc1>>NCCc1ccc(O)c(O)c1
ord_dataset-02ee2261663048188cf6d85d2cc96e3f
ord-9334216d98874a0aa0f332578a5d0309
CC(=O)OC[C@H]1O[C@@H](n2cnc(C(=O)O)c2N)[C@H](OC(C)=O)[C@@H]1OC(C)=O.[N-]=[N+]=C(c1ccccc1)c1ccccc1>>CC(=O)OC[C@H]1O[C@@H](n2cnc(C(=O)OC(c3ccccc3)c3ccccc3)c2N)[C@H](OC(C)=O)[C@@H]1OC(C)=O
C1(=CC=CC=C1)C(=[N+]=[N-])C1=CC=CC=C1.NC1=C(N=CN1[C@H]1[C@H](OC(C)=O)[C@H](OC(C)=O)[C@H](O1)COC(C)=O)C(=O)O>>C1(=CC=CC=C1)C(C1=CC=CC=C1)OC(=O)C=1N=CN(C1N)[C@H]1[C@H](OC(C)=O)[C@H](OC(C)=O)[C@H](O1)COC(C)=O
[CH3:1][C:2](=[O:3])[O:4][CH2:5][C@H:6]1[O:7][C@@H:8]([n:9]2[cH:10][n:11][c:12]([C:13](=[O:14])[OH:15])[c:29]2[NH2:30])[C@H:31]([O:32][C:33]([CH3:34])=[O:35])[C@@H:36]1[O:37][C:38]([CH3:39])=[O:40].[N-]=[N+]=[C:16]([c:17]1[cH:18][cH:19][cH:20][cH:21][cH:22]1)[c:23]1[cH:24][cH:25][cH:26][cH:27][cH:28]1>>[CH3:1][C:2](=[O...
CC(=O)OC[C@H]1O[C@@H](n2cnc(C(=O)O)c2N)[C@H](OC(C)=O)[C@@H]1OC(C)=O.[N-]=[N+]=C(c1ccccc1)c1ccccc1
CC(=O)OC[C@H]1O[C@@H](n2cnc(C(=O)OC(c3ccccc3)c3ccccc3)c2N)[C@H](OC(C)=O)[C@@H]1OC(C)=O
null
null
C(Cl)Cl
Heteroatom Alkylation and Arylation
O-alkylation of carboxylic acids with diazo compounds
8531b6eb3abfd6846ce0cb8d79abac610072134e0cc0be40cc269196cd4eea5b
d6eab3abd961fdb019332f17e55277b8a7c7f7a1f79c71be7a6248f0a0e6a15e
O=C(OC(c1ccccc1)c1ccccc1)c1cn([C@H]2CCCO2)cn1
[#7;a:1]:[c:2](-[C:3](=[O;D1;H0:4])-[OH;D1;+0:5]):[c:6]:[#7;a:7].[N-]=[N+]=[C;H0;D3;+0:8](-[c:9](:[c:10]):[c:11])-[c:12](:[c:13]):[c:14]>>[#7;a:1]:[c:2](-[C:3](=[O;D1;H0:4])-[O;H0;D2;+0:5]-[CH;D3;+0:8](-[c:9](:[c:10]):[c:11])-[c:12](:[c:13]):[c:14]):[c:6]:[#7;a:7]
88
[{"value": 88.0, "product": "C1(=CC=CC=C1)C(C1=CC=CC=C1)OC(=O)C=1N=CN(C1N)[C@H]1[C@H](OC(C)=O)[C@H](OC(C)=O)[C@H](O1)COC(C)=O", "details": "PERCENTYIELD", "is_desired": false}]
null
null
16
HOUR
Diphenyldiazomethane (2.0 g, 10.3 mmol) was added to the suspension of 5-amino-1-(2,3,5-tris-O-acetyl-β-D-ribofuranosyl)-1H-imidazole-4-carboxylic acid (3.86 g, 10 mmol) in CH2Cl2 (50 mL). The mixture was stirred at room temperature for 16 h, by which time all the reactants had dissolved. The reaction mixture was poure...
10.6084/m9.figshare.5104873.v1
null
Carboxylic acid.Diazo
Ester
null
null
C1CCOC1.c1c[nH]cn1.c1ccccc1.c1ccccc1
Other
C(Cl)Cl
null
16
CC(=O)OC[C@H]1O[C@@H](n2cnc(C(=O)O)c2N)[C@H](OC(C)=O)[C@@H]1OC(C)=O.[N-]=[N+]=C(c1ccccc1)c1ccccc1>C(Cl)Cl>CC(=O)OC[C@H]1O[C@@H](n2cnc(C(=O)OC(c3ccccc3)c3ccccc3)c2N)[C@H](OC(C)=O)[C@@H]1OC(C)=O
ord_dataset-02ee2261663048188cf6d85d2cc96e3f
ord-36b73a24973348ec866f55e0fe8d820d
O=C(Nc1nc2c(c(=O)o1)NCN2[C@@H]1O[C@H](CO)[C@@H](O)[C@H]1O)OCc1ccccc1>>Nc1nc2c(ncn2[C@@H]2O[C@H](CO)[C@@H](O)[C@H]2O)c(=O)o1
C1(=CC=CC=C1)COC(=O)NC=1OC(C2=C(N1)N(CN2)[C@H]2[C@H](O)[C@H](O)[C@H](O2)CO)=O>>C1=NC2=C(N1[C@H]3[C@@H]([C@@H]([C@H](O3)CO)O)O)N=C(OC2=O)N
O=C(OCc1ccccc1)[NH:1][c:2]1[n:3][c:4]2[c:5]([c:18](=[O:19])[o:20]1)[NH:6][CH2:7][N:8]2[C@@H:9]1[O:10][C@H:11]([CH2:12][OH:13])[C@@H:14]([OH:15])[C@H:16]1[OH:17]>>[NH2:1][c:2]1[n:3][c:4]2[c:5]([n:6][cH:7][n:8]2[C@@H:9]2[O:10][C@H:11]([CH2:12][OH:13])[C@@H:14]([OH:15])[C@H:16]2[OH:17])[c:18](=[O:19])[o:20]1
O=C(Nc1nc2c(c(=O)o1)NCN2[C@@H]1O[C@H](CO)[C@@H](O)[C@H]1O)OCc1ccccc1
Nc1nc2c(ncn2[C@@H]2O[C@H](CO)[C@@H](O)[C@H]2O)c(=O)o1
null
[Pd]
CN(C)C=O
Functional Group Interconversion
OtherReaction
fc2498df57d0b68601c8b0128483aec1185030e8f2a21873dd28fb10e9c48464
2035eb5d20d0a6c1999bd2ad7c2c4c43934ccc29852a60019e95d400e45d9192
O=c1ocnc2c1ncn2[C@H]1CCCO1
O=C(-O-C-c1:c:c:c:c:c:1)-[NH;D2;+0:1]-[c:2]1:[#7;a:3]:[c:4]2:[c:5](:[c:6](=[O;D1;H0:7]):[#8;a:8]:1)-[NH;D2;+0:9]-[CH2;D2;+0:10]-[N;H0;D3;+0:11]-2-[C:12](-[C:13])-[#8:14]-[C:15]>>[C:15]-[#8:14]-[C:12](-[n;H0;D3;+0:11]1:[cH;D2;+0:10]:[n;H0;D2;+0:9]:[c:5]2:[c:6](=[O;D1;H0:7]):[#8;a:8]:[c:2](-[NH2;D1;+0:1]):[#7;a:3]:[c:4]:...
null
[]
null
null
4
HOUR
10% Palladium on charcoal (172 mg) was added to a solution of 5-[[(phenylmethoxy)carbonyl]amino]-3-(β-D-ribofuranosyl)imidazo[4,5-d][1,3]oxazin-7(1H)-one (172 mg, 0.41 mmol) in DMF (7 mL) and the mixture was stirred at room temperature under a hydrogen atmosphere for 4 h. The mixture was filtered through prewashed Celi...
10.6084/m9.figshare.5104873.v1
null
Carbamic ester.Ether.Secondary amine.Tertiary amine
Primary amine
c1ccccc1.c1nc2c(co1)NCN2
c1nc2cocnc2n1
c1nc2cocnc2n1.C1CCOC1
HO-
[Pd].CN(C)C=O
null
4
O=C(Nc1nc2c(c(=O)o1)NCN2[C@@H]1O[C@H](CO)[C@@H](O)[C@H]1O)OCc1ccccc1>[Pd].CN(C)C=O>Nc1nc2c(ncn2[C@@H]2O[C@H](CO)[C@@H](O)[C@H]2O)c(=O)o1
ord_dataset-02ee2261663048188cf6d85d2cc96e3f
ord-ff74fda1878941da9ad64d6ce412d08d
O=C(NC(=O)OCc1ccccc1)Nc1c(C(=O)OC(c2ccccc2)c2ccccc2)ncn1[C@@H]1O[C@H](CO)[C@@H](O)[C@H]1O>>NC(=O)Nc1c(C(=O)O)ncn1[C@@H]1O[C@H](CO)[C@@H](O)[C@H]1O
C1(=CC=CC=C1)C(C1=CC=CC=C1)OC(=O)C=1N=CN(C1NC(=O)NC(=O)OCC1=CC=CC=C1)[C@H]1[C@H](O)[C@H](O)[C@H](O1)CO>>NC(=O)NC1=C(N=CN1[C@H]1[C@H](O)[C@H](O)[C@H](O1)CO)C(=O)O
O=C(OCc1ccccc1)[NH:1][C:2](=[O:3])[NH:4][c:5]1[c:6]([C:7](=[O:8])[O:9]C(c2ccccc2)c2ccccc2)[n:10][cH:11][n:12]1[C@@H:13]1[O:14][C@H:15]([CH2:16][OH:17])[C@@H:18]([OH:19])[C@H:20]1[OH:21]>>[NH2:1][C:2](=[O:3])[NH:4][c:5]1[c:6]([C:7](=[O:8])[OH:9])[n:10][cH:11][n:12]1[C@@H:13]1[O:14][C@H:15]([CH2:16][OH:17])[C@@H:18]([OH:...
O=C(NC(=O)OCc1ccccc1)Nc1c(C(=O)OC(c2ccccc2)c2ccccc2)ncn1[C@@H]1O[C@H](CO)[C@@H](O)[C@H]1O
NC(=O)Nc1c(C(=O)O)ncn1[C@@H]1O[C@H](CO)[C@@H](O)[C@H]1O
null
[Pd]
CN(C)C=O.C1CCOC1.C(C)O
Reduction
OtherReaction
6e1486eafbcea8442192eba866515d318abd7924f55a61ba62dacae9c5b4ae62
ff61d05c19231ae2eed2fc2d917cf58f7517ebb4b75f8fcb793d18e13a839cdf
c1cn([C@H]2CCCO2)cn1
O=C(-O-C-c1:c:c:c:c:c:1)-[NH;D2;+0:1]-[C:2](=[O;D1;H0:3])-[#7:4]-[c:5](:[#7;a:6]):[c:7](-[C:8](=[O;D1;H0:9])-[O;H0;D2;+0:10]-C(-c1:c:c:c:c:c:1)-c1:c:c:c:c:c:1):[#7;a:11]>>[#7;a:11]:[c:7](-[C:8](=[O;D1;H0:9])-[OH;D1;+0:10]):[c:5](-[#7:4]-[C:2](-[NH2;D1;+0:1])=[O;D1;H0:3]):[#7;a:6]
null
[]
null
null
2
HOUR
5-[[[[(phenylmethoxy)carbonyl]amino]carbonyl]amino]-1-(β-D-ribofuranosyl)-1H-imidazole-4-carboxylic acid diphenylmethyl ester (1.76 g, 2.9 mmol) was dissolved in the mixture of DMF (50 mL), THF (20 mL) and ethanol (30 mL) and mixed with 10% palladium on charcoal. The mixture was hydrogenated at 50 psig pressure for 2 h...
10.6084/m9.figshare.5104873.v1
null
Carbamic ester.Ester.Ether.Urea
Carboxylic acid.Urea
c1ccccc1.c1ccccc1.c1ccccc1
null
c1c[nH]cn1.C1CCOC1
HO-
[Pd].CN(C)C=O.C1CCOC1.C(C)O
null
2
O=C(NC(=O)OCc1ccccc1)Nc1c(C(=O)OC(c2ccccc2)c2ccccc2)ncn1[C@@H]1O[C@H](CO)[C@@H](O)[C@H]1O>[Pd].CN(C)C=O.C1CCOC1.C(C)O>NC(=O)Nc1c(C(=O)O)ncn1[C@@H]1O[C@H](CO)[C@@H](O)[C@H]1O
ord_dataset-02ee2261663048188cf6d85d2cc96e3f
ord-b09968f7a78948329b0580e276d90a67
NC(=O)Nc1nc(C(=O)O)cn1[C@@H]1O[C@H](CO)[C@@H](O)[C@H]1O>>Nc1nc2c(ncn2[C@@H]2O[C@H](CO)[C@@H](O)[C@H]2O)c(=O)o1
Cl.CN(CCCN=C=NCC)C.NC(=O)NC=1N(C=C(N1)C(=O)O)[C@H]1[C@H](O)[C@H](O)[C@H](O1)CO>>C1=NC2=C(N1[C@H]3[C@@H]([C@@H]([C@H](O3)CO)O)O)N=C(OC2=O)N
O[C:18]([c:5]1[cH:4][n:8]([C@@H:9]2[O:10][C@H:11]([CH2:12][OH:13])[C@@H:14]([OH:15])[C@H:16]2[OH:17])[c:7]([NH:3][C:2]([NH2:1])=[O:20])[n:6]1)=[O:19]>>[NH2:1][c:2]1[n:3][c:4]2[c:5]([n:6][cH:7][n:8]2[C@@H:9]2[O:10][C@H:11]([CH2:12][OH:13])[C@@H:14]([OH:15])[C@H:16]2[OH:17])[c:18](=[O:19])[o:20]1
NC(=O)Nc1nc(C(=O)O)cn1[C@@H]1O[C@H](CO)[C@@H](O)[C@H]1O
Nc1nc2c(ncn2[C@@H]2O[C@H](CO)[C@@H](O)[C@H]2O)c(=O)o1
null
null
CO.O
Aromatic Heterocycle Formation
OtherReaction
cd6bc30d58c0b8a63a359140a705be31656f97d3a88e5b712198a607b7f4cb74
fadb2580f49ac438d8998fc783c5f4fbb063a52cd630276446cea9d6cf60b2de
O=c1ocnc2c1ncn2[C@H]1CCCO1
O-[C;H0;D3;+0:1](=[O;D1;H0:2])-[c:3]1:[#7;a:4]:[c;H0;D3;+0:5](-[NH;D2;+0:6]-[C;H0;D3;+0:7](-[N;D1;H2:8])=[O;H0;D1;+0:9]):[#7;a:10](-[C:11]-[#8:12]):[cH;D2;+0:13]:1>>[#8:12]-[C:11]-[#7;a:10]1:[cH;D2;+0:5]:[#7;a:4]:[c:3]2:[c;H0;D3;+0:1](=[O;D1;H0:2]):[o;H0;D2;+0:9]:[c;H0;D3;+0:7](-[N;D1;H2:8]):[n;H0;D2;+0:6]:[c;H0;D3;+0:...
null
[]
null
null
8
HOUR
1-(3-Dimethylaminopropyl)-3-ethylcarbodiimide hydrochloride (78 mg, 0.41 mmol) was added to a solution of 5-[[(amino)carbonyl]amino-1-(β-D-ribofuranosyl)-1H-imidazole-4-carboxylic acid (19 mg, 0.063 mmol) in water (2 mL) and CH3OH (5 mL) and the mixture was stirred at room temperature overnight. The reaction was quench...
10.6084/m9.figshare.5104873.v1
null
Carboxylic acid.Urea
null
c1c[nH]cn1
c1nc2cocnc2n1
c1nc2cocnc2n1.C1CCOC1
HO-
CO.O
null
8
NC(=O)Nc1nc(C(=O)O)cn1[C@@H]1O[C@H](CO)[C@@H](O)[C@H]1O>CO.O>Nc1nc2c(ncn2[C@@H]2O[C@H](CO)[C@@H](O)[C@H]2O)c(=O)o1
ord_dataset-02ee2261663048188cf6d85d2cc96e3f
ord-099b2ab360d147c7b305025fdc1c5d3f
CC(=O)OC[C@H]1O[C@@H](n2cnc(C(=O)OC(c3ccccc3)c3ccccc3)c2N)[C@H](OC(C)=O)[C@@H]1OC(C)=O.O=C(N=C=S)OCc1ccccc1>>CC(=O)OC[C@H]1O[C@@H](n2cnc(C(=O)OC(c3ccccc3)c3ccccc3)c2NC(=S)NC(=O)OCc2ccccc2)[C@H](OC(C)=O)[C@@H]1OC(C)=O
C(C1=CC=CC=C1)OC(=O)N=C=S.C1(=CC=CC=C1)C(C1=CC=CC=C1)OC(=O)C=1N=CN(C1N)[C@H]1[C@H](OC(C)=O)[C@H](OC(C)=O)[C@H](O1)COC(C)=O.C(C1=CC=CC=C1)OC(=O)N=C=S>>C1(=CC=CC=C1)C(C1=CC=CC=C1)OC(=O)C=1N=CN(C1NC(=S)NC(=O)OCC1=CC=CC=C1)[C@H]1[C@H](OC(C)=O)[C@H](OC(C)=O)[C@H](O1)COC(C)=O
[CH3:1][C:2](=[O:3])[O:4][CH2:5][C@H:6]1[O:7][C@@H:8]([n:9]2[cH:10][n:11][c:12]([C:13](=[O:14])[O:15][CH:16]([c:17]3[cH:18][cH:19][cH:20][cH:21][cH:22]3)[c:23]3[cH:24][cH:25][cH:26][cH:27][cH:28]3)[c:29]2[NH2:30])[C@H:44]([O:45][C:46]([CH3:47])=[O:48])[C@@H:49]1[O:50][C:51]([CH3:52])=[O:53].[C:31](=[S:32])=[N:33][C:34]...
CC(=O)OC[C@H]1O[C@@H](n2cnc(C(=O)OC(c3ccccc3)c3ccccc3)c2N)[C@H](OC(C)=O)[C@@H]1OC(C)=O.O=C(N=C=S)OCc1ccccc1
CC(=O)OC[C@H]1O[C@@H](n2cnc(C(=O)OC(c3ccccc3)c3ccccc3)c2NC(=S)NC(=O)OCc2ccccc2)[C@H](OC(C)=O)[C@@H]1OC(C)=O
null
null
C(Cl)Cl
Heteroatom Alkylation and Arylation
thiourea
d196f428325df478b289a71c7a1a97a24db09ae9600571f1068a75b9c1a64923
d5d2ed8b9b1ac1023c3c8e0c0be1b8fb1cb57874c436f1471dd4bc0b489dd07a
O=C(NC(=S)Nc1c(C(=O)OC(c2ccccc2)c2ccccc2)ncn1[C@H]1CCCO1)OCc1ccccc1
[#8:1]-[C:2](=[O;D1;H0:3])-[c:4]1:[#7;a:5]:[c:6]:[#7;a:7](-[C:8]-[#8:9]):[c:10]:1-[NH2;D1;+0:11].[C:12]-[#8:13]-[C:14](=[O;D1;H0:15])-[N;H0;D2;+0:16]=[C;H0;D2;+0:17]=[S;D1;H0:18]>>[#8:1]-[C:2](=[O;D1;H0:3])-[c:4]1:[#7;a:5]:[c:6]:[#7;a:7](-[C:8]-[#8:9]):[c:10]:1-[NH;D2;+0:11]-[C;H0;D3;+0:17](=[S;D1;H0:18])-[NH;D2;+0:16]...
98
[{"value": 98.0, "product": "C1(=CC=CC=C1)C(C1=CC=CC=C1)OC(=O)C=1N=CN(C1NC(=S)NC(=O)OCC1=CC=CC=C1)[C@H]1[C@H](OC(C)=O)[C@H](OC(C)=O)[C@H](O1)COC(C)=O", "details": "PERCENTYIELD", "is_desired": false}]
null
null
46
HOUR
Four portions of benzyloxycarbonyl isothiocyanate (Caution: stench, handle in a well ventilated hood only, crude, 2.0 g each, total 41 mmol) were added to a solution of 5-amino-1-(2,3,5-tris-O-acetyl-β-D-ribofuranosyl)-1H-imidazole-4-carboxylic acid diphenylmethyl ester (1.1 g, 2 mmol) in CH2Cl2 (10 mL) at 0 h, 6 h, 22...
10.6084/m9.figshare.5104873.v1
null
Primary amine.Isothiocyanate
Carbamic ester.Thiourea
null
null
C1CCOC1.c1c[nH]cn1.c1ccccc1.c1ccccc1.c1ccccc1
null
C(Cl)Cl
null
46
CC(=O)OC[C@H]1O[C@@H](n2cnc(C(=O)OC(c3ccccc3)c3ccccc3)c2N)[C@H](OC(C)=O)[C@@H]1OC(C)=O.O=C(N=C=S)OCc1ccccc1>C(Cl)Cl>CC(=O)OC[C@H]1O[C@@H](n2cnc(C(=O)OC(c3ccccc3)c3ccccc3)c2NC(=S)NC(=O)OCc2ccccc2)[C@H](OC(C)=O)[C@@H]1OC(C)=O
ord_dataset-02ee2261663048188cf6d85d2cc96e3f
ord-55af28a305474a509ca9db96966a0640
O=C(Nc1nc2c(ncn2[C@@H]2O[C@H](CO)[C@@H](O)[C@H]2O)c(=O)s1)OCc1ccccc1>>Nc1nc2c(ncn2[C@@H]2O[C@H](CO)[C@@H](O)[C@H]2O)c(=O)s1
C1(=CC=CC=C1)COC(NC=1SC(C2=C(N1)N(C=N2)[C@H]2[C@H](O)[C@H](O)[C@H](O2)CO)=O)=O>>[C@@H]1([C@H](O)[C@H](O)[C@@H](CO)O1)N1C=NC=2C(=O)SC(N)=NC12
O=C(OCc1ccccc1)[NH:1][c:2]1[n:3][c:4]2[c:5]([n:6][cH:7][n:8]2[C@@H:9]2[O:10][C@H:11]([CH2:12][OH:13])[C@@H:14]([OH:15])[C@H:16]2[OH:17])[c:18](=[O:19])[s:20]1>>[NH2:1][c:2]1[n:3][c:4]2[c:5]([n:6][cH:7][n:8]2[C@@H:9]2[O:10][C@H:11]([CH2:12][OH:13])[C@@H:14]([OH:15])[C@H:16]2[OH:17])[c:18](=[O:19])[s:20]1
O=C(Nc1nc2c(ncn2[C@@H]2O[C@H](CO)[C@@H](O)[C@H]2O)c(=O)s1)OCc1ccccc1
Nc1nc2c(ncn2[C@@H]2O[C@H](CO)[C@@H](O)[C@H]2O)c(=O)s1
null
[Pd]
CN(C)C=O
Reduction
Hydrogenolysis of amides/imides/carbamates
087b6600ba91d3df931fe6979f2445c192cbfd59e04fd2d8a10f7c7573ac669f
4e549866ec1acadec4c84aaf8495992a28ec78d8ea5ef1b9f44dd843b0dcb7d4
O=c1scnc2c1ncn2[C@H]1CCCO1
O=C(-O-C-c1:c:c:c:c:c:1)-[NH;D2;+0:1]-[c:2]1:[#16;a:3]:[c:4]:[c:5](:[#7;a:6]):[c:7](:[#7;a:8]):[#7;a:9]:1>>[#7;a:6]:[c:5]1:[c:4]:[#16;a:3]:[c:2](-[NH2;D1;+0:1]):[#7;a:9]:[c:7]:1:[#7;a:8]
null
[]
null
null
6
HOUR
A solution of [3,7-dihydro-7-oxo-3-(β-D-ribofuranosyl)imidazo[4,5-d][1,3]thiazin-5-yl]carbamic acid phenylmethyl ester (170 mg, 0.39 mmol) in dry DMF (10 mL) was hydrogenated in the presence of 10% palladium on charcoal (200 mg) at room temperature and 50 psig for 6 h. Additional catalyst (200 mg) was added and hydroge...
10.6084/m9.figshare.5104873.v1
null
Carbamic ester.Ether
Primary amine
c1ccccc1
null
c1nc2cscnc2n1.C1CCOC1
HO-
[Pd].CN(C)C=O
null
6
O=C(Nc1nc2c(ncn2[C@@H]2O[C@H](CO)[C@@H](O)[C@H]2O)c(=O)s1)OCc1ccccc1>[Pd].CN(C)C=O>Nc1nc2c(ncn2[C@@H]2O[C@H](CO)[C@@H](O)[C@H]2O)c(=O)s1
ord_dataset-02ee2261663048188cf6d85d2cc96e3f
ord-1c5d6f3e9f13411cab9d4d7d0306d9c2
CN(C=O)c1ccccc1.Nc1nccs1>>CN(C=Nc1nccs1)c1ccccc1
P(=O)(Cl)(Cl)Cl.NC=1SC=CN1.CN(C1=CC=CC=C1)C=O>>S1C(=NC=C1)N=CN(C1=CC=CC=C1)C
O=[CH:3][N:2]([CH3:1])[c:10]1[cH:11][cH:12][cH:13][cH:14][cH:15]1.[NH2:4][c:5]1[n:6][cH:7][cH:8][s:9]1>>[CH3:1][N:2]([CH:3]=[N:4][c:5]1[n:6][cH:7][cH:8][s:9]1)[c:10]1[cH:11][cH:12][cH:13][cH:14][cH:15]1
CN(C=O)c1ccccc1.Nc1nccs1
CN(C=Nc1nccs1)c1ccccc1
null
NC=1SC=CN1
C1(=CC=CC=C1)C
Heteroatom Alkylation and Arylation
OtherReaction
d548d780574a6e8bf4728bd7c36e74e2f78572af917149e7c38580ae970e40c3
b9d219f0674c4c56492b0e55f3afda0e6dc263a5614af120d7a27809c687708b
C(=Nc1nccs1)Nc1ccccc1
O=[CH;D2;+0:1]-[#7:2](-[C;D1;H3:3])-[c:4].[NH2;D1;+0:5]-[c:6]1:[#16;a:7]:[c:8]:[c:9]:[#7;a:10]:1>>[C;D1;H3:3]-[#7:2](-[c:4])-[CH;D2;+0:1]=[N;H0;D2;+0:5]-[c:6]1:[#16;a:7]:[c:8]:[c:9]:[#7;a:10]:1
94.2
[{"value": 94.2, "product": "S1C(=NC=C1)N=CN(C1=CC=CC=C1)C", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
10
MINUTE
To a stirred suspension of N-methylformanilide (67.6 g; 0.50 mole), toluene (25 g) and 2-aminothiazole (2.0 g; 0.02 mole) was added phosphorus oxychloride (45.8 mL; 0.50 mole) over 15 minutes. The temperature was maintained below 45° C. during this addition. Stirring was continued for 10 minutes, after which time a hot...
10.6084/m9.figshare.5104873.v1
null
Tertiary amide.Primary amine
null
null
null
c1cscn1.c1ccccc1
HO-
NC=1SC=CN1.C1(=CC=CC=C1)C
null
0.166667
CN(C=O)c1ccccc1.Nc1nccs1>NC=1SC=CN1.C1(=CC=CC=C1)C>CN(C=Nc1nccs1)c1ccccc1
ord_dataset-02ee2261663048188cf6d85d2cc96e3f
ord-94e0b41df81646abb6a98f85deb9681f
CN(C=O)c1ccccc1.Nc1ccccn1>>CN(C=Nc1ccccn1)c1ccccc1
CN(C1=CC=CC=C1)C=O.NC1=NC=CC=C1>>N1=C(C=CC=C1)N=CN(C1=CC=CC=C1)C
O=[CH:3][N:2]([CH3:1])[c:11]1[cH:12][cH:13][cH:14][cH:15][cH:16]1.[NH2:4][c:5]1[cH:6][cH:7][cH:8][cH:9][n:10]1>>[CH3:1][N:2]([CH:3]=[N:4][c:5]1[cH:6][cH:7][cH:8][cH:9][n:10]1)[c:11]1[cH:12][cH:13][cH:14][cH:15][cH:16]1
CN(C=O)c1ccccc1.Nc1ccccn1
CN(C=Nc1ccccn1)c1ccccc1
null
null
null
Heteroatom Alkylation and Arylation
OtherReaction
d548d780574a6e8bf4728bd7c36e74e2f78572af917149e7c38580ae970e40c3
b9d219f0674c4c56492b0e55f3afda0e6dc263a5614af120d7a27809c687708b
C(=Nc1ccccn1)Nc1ccccc1
O=[CH;D2;+0:1]-[#7:2](-[C;D1;H3:3])-[c:4].[NH2;D1;+0:5]-[c:6](:[c:7]):[#7;a:8]:[c:9]>>[C;D1;H3:3]-[#7:2](-[c:4])-[CH;D2;+0:1]=[N;H0;D2;+0:5]-[c:6](:[c:7]):[#7;a:8]:[c:9]
null
[]
null
null
null
null
Prepared following the procedure of Example 1 from N-methylformanilide and 2-aminopyridine. Vacuum distillation of the crude product gave pure 3 as a pale yellow oil: bp 164°-165° C. @ 0.5 mm Hg. 1H-NMR (CDCl3) 8.94 (S, 1H), 8.30 (d, 1H, J=5 Hz), 7.6-6.9 (m,8H), 3.52 (S, 3H); IR(neat) 3045, 1620, 1580, 1555, 1500, 1460...
10.6084/m9.figshare.5104873.v1
null
Tertiary amide.Primary amine
null
null
null
c1ccncc1.c1ccccc1
HO-
null
null
null
CN(C=O)c1ccccc1.Nc1ccccn1>>CN(C=Nc1ccccn1)c1ccccc1
ord_dataset-02ee2261663048188cf6d85d2cc96e3f
ord-21c43fd9d87e46ca92b874799634794d
CCN(C=O)c1ccccc1.Nc1ccccn1>>CCN(C=Nc1ccccn1)c1ccccc1
C(C)N(C1=CC=CC=C1)C=O.NC1=NC=CC=C1>>N1=C(C=CC=C1)N=CN(C1=CC=CC=C1)CC
O=[CH:4][N:3]([CH2:2][CH3:1])[c:12]1[cH:13][cH:14][cH:15][cH:16][cH:17]1.[NH2:5][c:6]1[cH:7][cH:8][cH:9][cH:10][n:11]1>>[CH3:1][CH2:2][N:3]([CH:4]=[N:5][c:6]1[cH:7][cH:8][cH:9][cH:10][n:11]1)[c:12]1[cH:13][cH:14][cH:15][cH:16][cH:17]1
CCN(C=O)c1ccccc1.Nc1ccccn1
CCN(C=Nc1ccccn1)c1ccccc1
null
null
null
Heteroatom Alkylation and Arylation
OtherReaction
d548d780574a6e8bf4728bd7c36e74e2f78572af917149e7c38580ae970e40c3
b9d219f0674c4c56492b0e55f3afda0e6dc263a5614af120d7a27809c687708b
C(=Nc1ccccn1)Nc1ccccc1
O=[CH;D2;+0:1]-[#7:2](-[C:3])-[c:4].[NH2;D1;+0:5]-[c:6](:[c:7]):[#7;a:8]:[c:9]>>[C:3]-[#7:2](-[c:4])-[CH;D2;+0:1]=[N;H0;D2;+0:5]-[c:6](:[c:7]):[#7;a:8]:[c:9]
null
[]
null
null
null
null
Prepared following the procedure of Example 1 from N-ethylformanilide and 2-aminopyridine. Vacuum distillation of the crude product gave pure 4 as a pale yellow oil: bp 164° C. @ 0.5 mm Hg. 1H-NMR (CDCl3) 8.83 (S, 1H), 8.30 (m,1H), 7.5-6.9 (m, 8H), 4.09 (q, 2H, J=7 Hz) 1.26 (t, 3H, J=7 Hz); IR(neat) 2990, 1620, 1570, 1...
10.6084/m9.figshare.5104873.v1
null
Tertiary amide.Primary amine
null
null
null
c1ccncc1.c1ccccc1
HO-
null
null
null
CCN(C=O)c1ccccc1.Nc1ccccn1>>CCN(C=Nc1ccccn1)c1ccccc1
ord_dataset-02ee2261663048188cf6d85d2cc96e3f
ord-ef6d53c2edb44bcfb521c55fd592d6aa
OC(CCl)C(O)CCl>>ClCC1OCOC1CCl
S(O)(O)(=O)=O.ClCC(C(CCl)O)O.O1OOCCC1.ClCC(C(CCl)O)O>>ClCC1OCOC1CCl
O[CH:7]([CH:3]([CH2:2][Cl:1])[OH:4])[CH2:8][Cl:9]>>[Cl:1][CH2:2][CH:3]1[O:4][CH2:5][O:6][CH:7]1[CH2:8][Cl:9]
OC(CCl)C(O)CCl
ClCC1OCOC1CCl
null
null
ClCCCl
Heteroatom Alkylation and Arylation
Diol acetalization
dffe56556f707e5f943e2e6a5abded5aa25faea622ba5aaefbcc99107066ab83
4c2b5746d777df4b3850be8bb940817bfc292176b756747eedaf24277a4ed5e4
C1COCO1
O-[CH;D3;+0:1](-[C:2]-[Cl;D1;H0:3])-[C:4](-[C:5])-[OH;D1;+0:6]>>[C:5]-[C:4]1-[O;H0;D2;+0:6]-[C:7]-[#8:8]-[CH;D3;+0:1]-1-[C:2]-[Cl;D1;H0:3]
89.5
[{"value": 89.5, "product": "ClCC1OCOC1CCl", "details": "PERCENTYIELD", "is_desired": false}]
null
null
8
HOUR
A three-neck 500-mL flask equipped with a thermometer, a mechanical stirrer, an addition funnel, a condenser, and a positive nitrogen atmosphere was charged with 1,4-dichloro-2,3-butanediol (50.0 g, 0.314 mole), trioxane (9.43 g, 0.314 mole), and 1,2-dichloroethane (EDC) (300 mL). The 1,4-dichloro-2,3-butanediol was no...
10.6084/m9.figshare.5104873.v1
null
Secondary alcohol.Secondary alcohol
Ether.Ether
null
C1COCO1
C1COCO1
null
ClCCCl
null
8
OC(CCl)C(O)CCl>ClCCCl>ClCC1OCOC1CCl
ord_dataset-02ee2261663048188cf6d85d2cc96e3f
ord-235b5db98cd94164b1a080341731bb8b
CCOC(=O)NC(CO)C(O)c1ccc(SC)cc1>>CSc1ccc(C2OC(=O)NC2CO)cc1
OC(C(CO)NC(=O)OCC)C1=CC=C(C=C1)SC>>CSC1=CC=C(C=C1)C1C(NC(O1)=O)CO
CCO[C:9](=[O:10])[NH:11][CH:12]([CH:7]([c:6]1[cH:5][cH:4][c:3]([S:2][CH3:1])[cH:16][cH:15]1)[OH:8])[CH2:13][OH:14]>>[CH3:1][S:2][c:3]1[cH:4][cH:5][c:6]([CH:7]2[O:8][C:9](=[O:10])[NH:11][CH:12]2[CH2:13][OH:14])[cH:15][cH:16]1
CCOC(=O)NC(CO)C(O)c1ccc(SC)cc1
CSc1ccc(C2OC(=O)NC2CO)cc1
null
null
C1(=CC=CC=C1)C
Miscellaneous
Intramolecular transesterification/Lactone formation
63623eac8f0b8aa138cf2addcfba157dc0d2343ba1e0308780e210c976c64df4
9e80c4ff7ba95f533a858930199d9a906feab625690374862e4109792e682b92
O=C1NCC(c2ccccc2)O1
C-C-O-[C;H0;D3;+0:1](=[O;D1;H0:2])-[#7:3]-[C:4]-[C:5](-[OH;D1;+0:6])-[c:7]>>[O;D1;H0:2]=[C;H0;D3;+0:1]1-[#7:3]-[C:4]-[C:5](-[c:7])-[O;H0;D2;+0:6]-1
null
[]
null
null
null
null
Compound (H) (5 g; 17.5 mmols) has been dissolved in warm toluene (25 ml). To this solution, an equimolar amount of potassium tert. butylate has been added and the reaction mixture has been refluxed for 3 hours. Afterwards, almost all of the solvent has been evaporated; water and ice have been added to the residue and ...
10.6084/m9.figshare.5104873.v1
null
Carbamic ester.Ether.Secondary alcohol
Carbamic ester
null
C1COCN1
c1ccccc1.C1COCN1
HO-
C1(=CC=CC=C1)C
null
null
CCOC(=O)NC(CO)C(O)c1ccc(SC)cc1>C1(=CC=CC=C1)C>CSc1ccc(C2OC(=O)NC2CO)cc1
ord_dataset-02ee2261663048188cf6d85d2cc96e3f
ord-d496dfe999fb47a1b259625feaebd9e5
ClCCCOc1ccc(Cl)c(Cl)c1.OC1(c2ccc(Cl)c(Cl)c2)CCNCC1>>OC1(c2ccc(Cl)c(Cl)c2)CCN(CCCOc2ccc(Cl)c(Cl)c2)CC1
ClC=1C=C(OCCCCl)C=CC1Cl.OC1(CCNCC1)C1=CC(=C(C=C1)Cl)Cl>>ClC=1C=C(OCCCN2CCC(CC2)(C2=CC(=C(C=C2)Cl)Cl)O)C=CC1Cl
Cl[CH2:14][CH2:15][CH2:16][O:17][c:18]1[cH:19][cH:20][c:21]([Cl:22])[c:23]([Cl:24])[cH:25]1.[OH:1][C:2]1([c:3]2[cH:4][cH:5][c:6]([Cl:7])[c:8]([Cl:9])[cH:10]2)[CH2:11][CH2:12][NH:13][CH2:26][CH2:27]1>>[OH:1][C:2]1([c:3]2[cH:4][cH:5][c:6]([Cl:7])[c:8]([Cl:9])[cH:10]2)[CH2:11][CH2:12][N:13]([CH2:14][CH2:15][CH2:16][O:17][...
ClCCCOc1ccc(Cl)c(Cl)c1.OC1(c2ccc(Cl)c(Cl)c2)CCNCC1
OC1(c2ccc(Cl)c(Cl)c2)CCN(CCCOc2ccc(Cl)c(Cl)c2)CC1
null
null
null
Heteroatom Alkylation and Arylation
N-alkylation of secondary amines with alkyl halides
0240b8450ff2c489d02f5f0d90bc953079d7a3ab239d35a03f26392fc248b4ef
523d37155b42c8dc851abeddadebb241cdd90bdf649ba750c35e13c8c752d7b0
c1ccc(OCCCN2CCC(c3ccccc3)CC2)cc1
Cl-[CH2;D2;+0:1]-[C:2]-[C:3].[C:4]-[C:5]-[NH;D2;+0:6]-[C:7]-[C:8]>>[C:4]-[C:5]-[N;H0;D3;+0:6](-[CH2;D2;+0:1]-[C:2]-[C:3])-[C:7]-[C:8]
97.5
[{"value": 97.5, "product": "ClC=1C=C(OCCCN2CCC(CC2)(C2=CC(=C(C=C2)Cl)Cl)O)C=CC1Cl", "details": "PERCENTYIELD", "is_desired": false}, {"value": 97.4, "product": "ClC=1C=C(OCCCN2CCC(CC2)(C2=CC(=C(C=C2)Cl)Cl)O)C=CC1Cl", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
null
null
3-(3,4-dichlorophenoxy)propylchloride 1.38 g and 4-hydroxy-4-(3,4-dichlorophenyl)piperidine 1.35 g are reacted in the same manner as Example 109 (1) to prepare 2.40 g (Yield: 97.5%) of 1-{3-(3,4-dichlorophenoxy)propyl}-4-hydroxy-4-(3,4-dichlorophenyl) piperidine (III-66). mp. 118.0°-118.5° C. Conditions: See reaction.n...
10.6084/m9.figshare.5104873.v1
null
Primary halide.Secondary amine
Tertiary amine
C1CCNCC1
C1CC[NH]CC1
c1ccccc1.C1CC[NH]CC1.c1ccccc1
HCl
null
null
null
ClCCCOc1ccc(Cl)c(Cl)c1.OC1(c2ccc(Cl)c(Cl)c2)CCNCC1>>OC1(c2ccc(Cl)c(Cl)c2)CCN(CCCOc2ccc(Cl)c(Cl)c2)CC1
ord_dataset-02ee2261663048188cf6d85d2cc96e3f
ord-0d60770bcb50476997f7e87cec0a58de
CCOC(=O)N1CCC(O)(c2ccc(Cl)c(Cl)c2)CC1>>OC1(c2ccc(Cl)c(Cl)c2)CCNCC1
C(C)OC(=O)N1CCC(CC1)(C1=CC(=C(C=C1)Cl)Cl)O.[OH-].[K+]>>OC1(CCNCC1)C1=CC(=C(C=C1)Cl)Cl
CCOC(=O)[N:13]1[CH2:12][CH2:11][C:2]([OH:1])([c:3]2[cH:4][cH:5][c:6]([Cl:7])[c:8]([Cl:9])[cH:10]2)[CH2:15][CH2:14]1>>[OH:1][C:2]1([c:3]2[cH:4][cH:5][c:6]([Cl:7])[c:8]([Cl:9])[cH:10]2)[CH2:11][CH2:12][NH:13][CH2:14][CH2:15]1
CCOC(=O)N1CCC(O)(c2ccc(Cl)c(Cl)c2)CC1
OC1(c2ccc(Cl)c(Cl)c2)CCNCC1
null
null
C(CCC)O
Reduction
Hydrogenolysis of tertiary amines
6dc5c07be2bf2a2ccc4ff166fd44281ea50e6dda805f74758334dcde1ad7a582
20c36f41eeb07c3ba4437b51ba72e8ff3c22d0b27e7197b0e9af3127f331149f
c1ccc(C2CCNCC2)cc1
C-C-O-C(=O)-[N;H0;D3;+0:1](-[C:2]-[C:3])-[C:4]-[C:5]>>[C:3]-[C:2]-[NH;D2;+0:1]-[C:4]-[C:5]
90
[{"value": 90.0, "product": "OC1(CCNCC1)C1=CC(=C(C=C1)Cl)Cl", "details": "PERCENTYIELD", "is_desired": false}, {"value": 90.0, "product": "OC1(CCNCC1)C1=CC(=C(C=C1)Cl)Cl", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
null
null
A mixture of 64.2 g of 1-ethoxycarbonyl-4-hydroxy-4-(3,4-dichlorophenyl)piperidine (X-1) and a solution of 72.4 g of KOH in 700 ml of nBuOH is refluxed for 2 hours and evaporated. The reaction mixture is concentrated under reduced pressure and extracted with ethyl acetate. The organic layer is washed with water, dried ...
10.6084/m9.figshare.5104873.v1
null
Carbamic ester.Ether
Secondary amine
C1CC[NH]CC1
C1CCNCC1
c1ccccc1.C1CCNCC1
HO-
C(CCC)O
null
null
CCOC(=O)N1CCC(O)(c2ccc(Cl)c(Cl)c2)CC1>C(CCC)O>OC1(c2ccc(Cl)c(Cl)c2)CCNCC1
ord_dataset-02ee2261663048188cf6d85d2cc96e3f
ord-1550a2c42379468ab53a6c235e7abb7c
CON=C(C(=O)O)c1csc(NC(c2ccccc2)(c2ccccc2)c2ccccc2)n1.CSCC1=C(C(=O)O)N2C(=O)C(N)[C@H]2SC1>>CON=C(C(=O)NC1C(=O)N2C(C(=O)O)=C(CSC)CS[C@H]12)c1csc(NC(c2ccccc2)(c2ccccc2)c2ccccc2)n1
CSCC=1CS[C@H]2N(C1C(=O)O)C(C2N)=O.C(Cl)Cl.C(C1=CC=CC=C1)(C1=CC=CC=C1)(C1=CC=CC=C1)NC=1SC=C(N1)C(C(=O)O)=NOC>>CSCC=1CS[C@H]2N(C1C(=O)O)C(C2NC(C(=NOC)C=2N=C(SC2)NC(C2=CC=CC=C2)(C2=CC=CC=C2)C2=CC=CC=C2)=O)=O
O[C:5]([C:4](=[N:3][O:2][CH3:1])[c:23]1[cH:24][s:25][c:26]([NH:27][C:28]([c:29]2[cH:30][cH:31][cH:32][cH:33][cH:34]2)([c:35]2[cH:36][cH:37][cH:38][cH:39][cH:40]2)[c:41]2[cH:42][cH:43][cH:44][cH:45][cH:46]2)[n:47]1)=[O:6].[NH2:7][CH:8]1[C:9](=[O:10])[N:11]2[C:12]([C:13](=[O:14])[OH:15])=[C:16]([CH2:17][S:18][CH3:19])[CH...
CON=C(C(=O)O)c1csc(NC(c2ccccc2)(c2ccccc2)c2ccccc2)n1.CSCC1=C(C(=O)O)N2C(=O)C(N)[C@H]2SC1
CON=C(C(=O)NC1C(=O)N2C(C(=O)O)=C(CSC)CS[C@H]12)c1csc(NC(c2ccccc2)(c2ccccc2)c2ccccc2)n1
null
null
C(C)(=O)O.CC(=O)C.C(C)N(CC)CC
Acylation
Carboxylic acid with primary amine to amide
37494d655fc476b499cf056f6435518833ae87795aab58744c3c61cc6e2d35e8
1acc31e468ee9ff2d6601bea2d2eb10c464508bb7150073479303b3753dd92b4
N=C(C(=O)NC1C(=O)N2C=CCS[C@H]12)c1csc(NC(c2ccccc2)(c2ccccc2)c2ccccc2)n1
O-[C;H0;D3;+0:1](=[O;D1;H0:2])-[C:3](=[#7:4]-[#8:5])-[c:6](:[#7;a:7]):[c:8]:[#16;a:9].[#16:10]-[C:11]1-[#7:12](-[C:13](-[C:14](=[O;D1;H0:15])-[O;D1;H1:16])=[C:17])-[C:18](=[O;D1;H0:19])-[C:20]-1-[NH2;D1;+0:21]>>[#16:10]-[C:11]1-[#7:12](-[C:13](-[C:14](=[O;D1;H0:15])-[O;D1;H1:16])=[C:17])-[C:18](=[O;D1;H0:19])-[C:20]-1-...
null
[]
20
CELSIUS
null
null
A mixture of 2.6 g of 3-methylthiomethyl-7-amino-ceph -3-eme-4-carboxylic acid, 26 ml of methylene chloride and 3 ml of triethylamine was stirred at 20° C. under an inert atmosphere and after cooling the mixture to -20° C., an acetone suspension of the mixed anhydride of Example 3 prepared from 6 g of the triethylamine...
10.6084/m9.figshare.5104873.v1
null
Carboxylic acid.Primary amine
Secondary amide
null
null
C1=CN2CC[C@H]2SC1.c1cscn1.c1ccccc1.c1ccccc1.c1ccccc1
HO-
C(C)(=O)O.CC(=O)C.C(C)N(CC)CC
20
null
CON=C(C(=O)O)c1csc(NC(c2ccccc2)(c2ccccc2)c2ccccc2)n1.CSCC1=C(C(=O)O)N2C(=O)C(N)[C@H]2SC1>C(C)(=O)O.CC(=O)C.C(C)N(CC)CC>CON=C(C(=O)NC1C(=O)N2C(C(=O)O)=C(CSC)CS[C@H]12)c1csc(NC(c2ccccc2)(c2ccccc2)c2ccccc2)n1
ord_dataset-02ee2261663048188cf6d85d2cc96e3f
ord-add39cef9add4eb09014846177ec4042
CON=C(C(=O)NC1C(=O)N2C(C(=O)O)=C(CSC)CS[C@H]12)c1csc(NC(c2ccccc2)(c2ccccc2)c2ccccc2)n1>>CON=C(C(=O)NC1C(=O)N2C(C(=O)O)=C(CSC)CS[C@H]12)c1csc(N)n1
CSCC=1CS[C@H]2N(C1C(=O)O)C(C2NC(C(=NOC)C=2N=C(SC2)NC(C2=CC=CC=C2)(C2=CC=CC=C2)C2=CC=CC=C2)=O)=O.FC(C(=O)O)(F)F>>CSCC=1CS[C@H]2N(C1C(=O)O)C(C2NC(C(=NOC)C=2N=C(SC2)N)=O)=O
c1ccc(C(c2ccccc2)(c2ccccc2)[NH:27][c:26]2[s:25][cH:24][c:23]([C:4](=[N:3][O:2][CH3:1])[C:5](=[O:6])[NH:7][CH:8]3[C:9](=[O:10])[N:11]4[C:12]([C:13](=[O:14])[OH:15])=[C:16]([CH2:17][S:18][CH3:19])[CH2:20][S:21][C@H:22]34)[n:28]2)cc1>>[CH3:1][O:2][N:3]=[C:4]([C:5](=[O:6])[NH:7][CH:8]1[C:9](=[O:10])[N:11]2[C:12]([C:13](=[O...
CON=C(C(=O)NC1C(=O)N2C(C(=O)O)=C(CSC)CS[C@H]12)c1csc(NC(c2ccccc2)(c2ccccc2)c2ccccc2)n1
CON=C(C(=O)NC1C(=O)N2C(C(=O)O)=C(CSC)CS[C@H]12)c1csc(N)n1
null
null
null
Deprotection
OtherReaction
7c27519660e9b0607fb80b9d32b9bfde8e19f5eec1a916a21370255e79658eb1
f6571fb5b7780a2b467937abfba91ba7d787f19d503265f299ff4a25a08963bd
N=C(C(=O)NC1C(=O)N2C=CCS[C@H]12)c1cscn1
[#16;a:1]1:[c:2]:[c:3]:[#7;a:4]:[c:5]:1-[NH;D2;+0:6]-C(-c1:c:c:c:c:c:1)(-c1:c:c:c:c:c:1)-c1:c:c:c:c:c:1>>[NH2;D1;+0:6]-[c:5]1:[#16;a:1]:[c:2]:[c:3]:[#7;a:4]:1
null
[]
20
CELSIUS
20
MINUTE
A mixture of 6.15 g of the product of Step A and 61 ml of trifluoroacetic acid was stirred at 20° C. for 20 minutes and the mixture was evaporated under reduced pressure at 30° C. to a volume of 15 ml. 150 ml of ispropyl ether were added at 10° C. to the mixture which was then stirred at 20° C. for 15 minutes and was v...
10.6084/m9.figshare.5104873.v1
null
Secondary amine
Primary amine
c1ccccc1.c1ccccc1.c1ccccc1
null
C1=CN2CC[C@H]2SC1.c1cscn1
Other
null
20
0.333333
CON=C(C(=O)NC1C(=O)N2C(C(=O)O)=C(CSC)CS[C@H]12)c1csc(NC(c2ccccc2)(c2ccccc2)c2ccccc2)n1>>CON=C(C(=O)NC1C(=O)N2C(C(=O)O)=C(CSC)CS[C@H]12)c1csc(N)n1
ord_dataset-02ee2261663048188cf6d85d2cc96e3f
ord-dcaa90fa626041689c210e2969f0e25b
C=CCO.CC(=O)OCC1=C(C(=O)O)N2C(=O)[C@@H](N)[C@H]2SC1>>C=CCOCC1=C(C(=O)O)N2C(=O)C(N)[C@H]2SC1
CC(=O)OCC1=C(N2[C@@H]([C@@H](C2=O)N)SC1)C(=O)O.B(F)(F)F.C(C=C)O>>C(C=C)OCC=1CS[C@H]2N(C1C(=O)O)C(C2N)=O
[CH2:1]=[CH:2][CH2:3][OH:4].CC(=O)O[CH2:5][C:6]1=[C:7]([C:8](=[O:9])[OH:10])[N:11]2[C:12](=[O:13])[C@@H:14]([NH2:15])[C@H:16]2[S:17][CH2:18]1>>[CH2:1]=[CH:2][CH2:3][O:4][CH2:5][C:6]1=[C:7]([C:8](=[O:9])[OH:10])[N:11]2[C:12](=[O:13])[CH:14]([NH2:15])[C@H:16]2[S:17][CH2:18]1
C=CCO.CC(=O)OCC1=C(C(=O)O)N2C(=O)[C@@H](N)[C@H]2SC1
C=CCOCC1=C(C(=O)O)N2C(=O)C(N)[C@H]2SC1
null
null
C(C)N(CC)CC
Heteroatom Alkylation and Arylation
OtherReaction
4252ee116e29ffa2b694d6e7ecc32c5cf1dbb2ee9625404732e0de7be874bedb
250047d74ba3e9a91b4a9d25ecfcf45e8445a0f7cdc18c5b9e40c2e06683e003
O=C1C[C@H]2SCC=CN12
C-C(=O)-O-[CH2;D2;+0:1]-[C:2](=[C:3](-[C:4](=[O;D1;H0:5])-[O;D1;H1:6])-[#7:7]-[C:8]=[O;D1;H0:9])-[C:10]-[#16:11].[C;D1;H2:12]=[C:13]-[C:14]-[OH;D1;+0:15]>>[#16:11]-[C:10]-[C:2](-[CH2;D2;+0:1]-[O;H0;D2;+0:15]-[C:14]-[C:13]=[C;D1;H2:12])=[C:3](-[C:4](=[O;D1;H0:5])-[O;D1;H1:6])-[#7:7]-[C:8]=[O;D1;H0:9]
null
[]
null
null
null
null
Using the procedure of Step A of Example 8, 27.2 g of 7-amino-cephalosporanic acid, 170 ml of the etherate of boron trifluoride, 136 ml of allyl alcohol and 115 ml of triethylamine were reacted and the 9 g of raw product was purified successively twice with hot hydrochloric acid and ammonium hydroxide to obtain 4.72 g ...
10.6084/m9.figshare.5104873.v1
null
Ester.Primary alcohol
Ether
null
null
C1=CN2CC[C@H]2SC1
HO-
C(C)N(CC)CC
null
null
C=CCO.CC(=O)OCC1=C(C(=O)O)N2C(=O)[C@@H](N)[C@H]2SC1>C(C)N(CC)CC>C=CCOCC1=C(C(=O)O)N2C(=O)C(N)[C@H]2SC1
ord_dataset-02ee2261663048188cf6d85d2cc96e3f
ord-332c42f9e23541eaa37b1a643ef16125
CC(=O)OCC1=C(C(=O)O)N2C(=O)[C@@H](N)[C@H]2SC1.CCCO>>CCCOCC1=C(C(=O)O)N2C(=O)C(N)[C@H]2SC1
CC(=O)OCC1=C(N2[C@@H]([C@@H](C2=O)N)SC1)C(=O)O.B(F)(F)F.C(CC)O>>C(CC)OCC=1CS[C@H]2N(C1C(=O)O)C(C2N)=O
CC(=O)[O:4][CH2:5][C:6]1=[C:7]([C:8](=[O:9])[OH:10])[N:11]2[C:12](=[O:13])[C@@H:14]([NH2:15])[C@H:16]2[S:17][CH2:18]1.O[CH2:3][CH2:2][CH3:1]>>[CH3:1][CH2:2][CH2:3][O:4][CH2:5][C:6]1=[C:7]([C:8](=[O:9])[OH:10])[N:11]2[C:12](=[O:13])[CH:14]([NH2:15])[C@H:16]2[S:17][CH2:18]1
CC(=O)OCC1=C(C(=O)O)N2C(=O)[C@@H](N)[C@H]2SC1.CCCO
CCCOCC1=C(C(=O)O)N2C(=O)C(N)[C@H]2SC1
null
null
C(C)N(CC)CC
Heteroatom Alkylation and Arylation
OtherReaction
4252ee116e29ffa2b694d6e7ecc32c5cf1dbb2ee9625404732e0de7be874bedb
250047d74ba3e9a91b4a9d25ecfcf45e8445a0f7cdc18c5b9e40c2e06683e003
O=C1C[C@H]2SCC=CN12
C-C(=O)-[O;H0;D2;+0:1]-[C:2]-[C:3](=[C:4](-[C:5](=[O;D1;H0:6])-[O;D1;H1:7])-[#7:8]-[C:9]=[O;D1;H0:10])-[C:11]-[#16:12].O-[CH2;D2;+0:13]-[C:14]-[C;D1;H3:15]>>[#16:12]-[C:11]-[C:3](-[C:2]-[O;H0;D2;+0:1]-[CH2;D2;+0:13]-[C:14]-[C;D1;H3:15])=[C:4](-[C:5](=[O;D1;H0:6])-[O;D1;H1:7])-[#7:8]-[C:9]=[O;D1;H0:10]
null
[]
null
null
null
null
Using the procedure of Step A of Example 8, 27.2 g of 7-amino-cephalosporanic acid, 170 ml of the etherate of of boron trifluoride, 131 ml of propanol and 128 ml of triethylamine were reacted to obtain 17.4 g of raw product which was purified with hot hydrochloric acid and ammonium hydroxide to obtain 7.45 g of 3-propo...
10.6084/m9.figshare.5104873.v1
null
Ester.Primary alcohol
Ether
null
null
C1=CN2CC[C@H]2SC1
HO-
C(C)N(CC)CC
null
null
CC(=O)OCC1=C(C(=O)O)N2C(=O)[C@@H](N)[C@H]2SC1.CCCO>C(C)N(CC)CC>CCCOCC1=C(C(=O)O)N2C(=O)C(N)[C@H]2SC1
ord_dataset-02ee2261663048188cf6d85d2cc96e3f
ord-563744f14f8d4c1594cf03c6eaa41a0e
CC(=O)OCC1=C(C(=O)O)N2C(=O)[C@@H](N)[C@H]2SC1.CC(C)O>>CC(C)OCC1=C(C(=O)O)N2C(=O)C(N)[C@H]2SC1
CC(=O)OCC1=C(N2[C@@H]([C@@H](C2=O)N)SC1)C(=O)O.B(F)(F)F.C(C)(C)O>>C(C)(C)OCC=1CS[C@H]2N(C1C(=O)O)C(C2N)=O
O=[C:2]([CH3:1])[O:4][CH2:5][C:6]1=[C:7]([C:8](=[O:9])[OH:10])[N:11]2[C:12](=[O:13])[C@@H:14]([NH2:15])[C@H:16]2[S:17][CH2:18]1.CC(O)[CH3:3]>>[CH3:1][CH:2]([CH3:3])[O:4][CH2:5][C:6]1=[C:7]([C:8](=[O:9])[OH:10])[N:11]2[C:12](=[O:13])[CH:14]([NH2:15])[C@H:16]2[S:17][CH2:18]1
CC(=O)OCC1=C(C(=O)O)N2C(=O)[C@@H](N)[C@H]2SC1.CC(C)O
CC(C)OCC1=C(C(=O)O)N2C(=O)C(N)[C@H]2SC1
null
null
C(C)N(CC)CC
C-C Coupling
OtherReaction
4b37754320a3a4e9fa7d05a7c8560982c3763f26a82f39c0cd8c8f3cbc557ca8
3344fa8ba720230c95001ed564e60a6abd4a907139323d3507fc29876e94fca3
O=C1C[C@H]2SCC=CN12
C-C(-O)-[CH3;D1;+0:1].O=[C;H0;D3;+0:2](-[C;D1;H3:3])-[#8:4]-[C:5]-[C:6]=[C:7]>>[C:7]=[C:6]-[C:5]-[#8:4]-[CH;D3;+0:2](-[C;D1;H3:3])-[CH3;D1;+0:1]
null
[]
null
null
null
null
Using the procedure of Step A of Example 8, 27.2 g of 7-amino-cephalosporanic acid, 170 ml of the etherate of boron trifluoride, 134 ml of isopropanol and 125 ml of triethylamine were reacted to obtain 16.25 g of raw product which was purified by two successive treatments with hot hydrochloric acid and ammonium hydroxi...
10.6084/m9.figshare.5104873.v1
null
Ester.Secondary alcohol
Ether
null
null
C1=CN2CC[C@H]2SC1
HO-
C(C)N(CC)CC
null
null
CC(=O)OCC1=C(C(=O)O)N2C(=O)[C@@H](N)[C@H]2SC1.CC(C)O>C(C)N(CC)CC>CC(C)OCC1=C(C(=O)O)N2C(=O)C(N)[C@H]2SC1
ord_dataset-02ee2261663048188cf6d85d2cc96e3f
ord-80f62c1c46ba4eb9a6ba6a91577ca2ab
CC(=O)OCC1=C(C(=O)O)N2C(=O)[C@@H](N)[C@H]2SC1.OCc1ccccc1>>NC1C(=O)N2C(C(=O)O)=C(OCc3ccccc3)CS[C@H]12
B(F)(F)F.CC(=O)OCC1=C(N2[C@@H]([C@@H](C2=O)N)SC1)C(=O)O.C(C1=CC=CC=C1)O.[OH-].[NH4+].B(F)(F)F>>C(C1=CC=CC=C1)OC=1CS[C@H]2N(C1C(=O)O)C(C2N)=O
CC(=O)OC[C:10]1=[C:6]([C:7](=[O:8])[OH:9])[N:5]2[C:3](=[O:4])[C@@H:2]([NH2:1])[C@H:21]2[S:20][CH2:19]1.[OH:11][CH2:12][c:13]1[cH:14][cH:15][cH:16][cH:17][cH:18]1>>[NH2:1][CH:2]1[C:3](=[O:4])[N:5]2[C:6]([C:7](=[O:8])[OH:9])=[C:10]([O:11][CH2:12][c:13]3[cH:14][cH:15][cH:16][cH:17][cH:18]3)[CH2:19][S:20][C@H:21]12
CC(=O)OCC1=C(C(=O)O)N2C(=O)[C@@H](N)[C@H]2SC1.OCc1ccccc1
NC1C(=O)N2C(C(=O)O)=C(OCc3ccccc3)CS[C@H]12
null
null
C(C)(=O)O.Cl.C(C)N(CC)CC
Acylation
OtherReaction
d48ee1196e65f97a301708ef8ff641ddb01af021a1e09c53eb7629c897f78fb1
ea7fec9b87f263517f6d6d5ea567ba191e6eeb412002bf8de9a1b87edd81c107
O=C1C[C@H]2SCC(OCc3ccccc3)=CN12
C-C(=O)-O-C-[C;H0;D3;+0:1]1=[C:2](-[C:3](=[O;D1;H0:4])-[O;D1;H1:5])-[#7:6](-[C:7]-[#16:8]-[C:9]-1)-[C:10]=[O;D1;H0:11].[OH;D1;+0:12]-[C:13]-[c:14]>>[O;D1;H0:11]=[C:10]-[#7:6]1-[C:7]-[#16:8]-[C:9]-[C;H0;D3;+0:1](-[O;H0;D2;+0:12]-[C:13]-[c:14])=[C:2]-1-[C:3](=[O;D1;H0:4])-[O;D1;H1:5]
null
[]
null
null
null
null
Using the procedure of Step A of Example 8, 27.2 g of 7-amino-cephalosporanic acid, 128 ml of the etherate of boron trifluoride, 126 ml of benzyl alcohol and 90 ml of triethylamine were reacted to obtain 27.1 g of raw product. 25 g of the said product and 250 ml of acetic acid were added to 25 ml of the etherate of bor...
10.6084/m9.figshare.5104873.v1
null
Enamine.Ester.Primary alcohol
Enamine.Ether
C1=CN2CC[C@H]2SC1
C1=CN2CC[C@H]2SC1
C1=CN2CC[C@H]2SC1.c1ccccc1
HO-
C(C)(=O)O.Cl.C(C)N(CC)CC
null
null
CC(=O)OCC1=C(C(=O)O)N2C(=O)[C@@H](N)[C@H]2SC1.OCc1ccccc1>C(C)(=O)O.Cl.C(C)N(CC)CC>NC1C(=O)N2C(C(=O)O)=C(OCc3ccccc3)CS[C@H]12
ord_dataset-02ee2261663048188cf6d85d2cc96e3f
ord-15135c6a32ce4d6eb19033f97ae48811
CSCC1=C(C(=O)O)N2C(=O)C(NC(=O)C(=NO)c3csc(N)n3)[C@H]2SC1>>CSCC1=C(C(=O)[O-])N2C(=O)C(NC(=O)C(=NO)c3csc(N)n3)[C@H]2SC1
C(C)(=O)[O-].[Na+].C(C)O.CSCC=1CS[C@H]2N(C1C(=O)O)C(C2NC(C(=NO)C=2N=C(SC2)N)=O)=O>>CSCC=1CS[C@H]2N(C1C(=O)[O-])C(C2NC(C(=NO)C=2N=C(SC2)N)=O)=O.[Na+]
[CH3:1][S:2][CH2:3][C:4]1=[C:5]([C:6](=[O:7])[OH:8])[N:9]2[C:10](=[O:11])[CH:12]([NH:13][C:14](=[O:15])[C:16](=[N:17][OH:18])[c:19]3[cH:20][s:21][c:22]([NH2:23])[n:24]3)[C@H:25]2[S:26][CH2:27]1>>[CH3:1][S:2][CH2:3][C:4]1=[C:5]([C:6](=[O:7])[O-:8])[N:9]2[C:10](=[O:11])[CH:12]([NH:13][C:14](=[O:15])[C:16](=[N:17][OH:18])...
CSCC1=C(C(=O)O)N2C(=O)C(NC(=O)C(=NO)c3csc(N)n3)[C@H]2SC1
CSCC1=C(C(=O)[O-])N2C(=O)C(NC(=O)C(=NO)c3csc(N)n3)[C@H]2SC1
null
null
CN(C=O)C
Oxidation
Carboxylic acid to carboxylate
af9382a4a3fca177895c8a400271aa22025197fc08b983f9d71150044c1e6777
b3097057beeca787f1d4960a7ee432572ee7aecad541233195b0dbbc0f674e9c
N=C(C(=O)NC1C(=O)N2C=CCS[C@H]12)c1cscn1
[#16:1]-[C:2]-[C:3](-[C:4])=[C:5](-[C:6](=[O;D1;H0:7])-[OH;D1;+0:8])-[#7:9]-[C:10]=[O;D1;H0:11]>>[#16:1]-[C:2]-[C:3](-[C:4])=[C:5](-[C:6](-[O-;H0;D1:8])=[O;D1;H0:7])-[#7:9]-[C:10]=[O;D1;H0:11]
null
[]
null
null
null
null
3.5 ml of a methanolic solution of sodium acetate and 30 ml of ethanol were added to a solution of 1 g of the syn isomer of 3-methylthiomethyl-7-[2-(2-amino-4-thiazolyl)-2-hydroxyimino-acetamido]-ceph-3-eme-4-carboxylic acid in 2 ml of dimethylformamide and the mixture was vacuum filtered. The product was rinsed with e...
10.6084/m9.figshare.5104873.v1
null
Carboxylic acid
null
null
null
C1=CN2CC[C@H]2SC1.c1cscn1
null
CN(C=O)C
null
null
CSCC1=C(C(=O)O)N2C(=O)C(NC(=O)C(=NO)c3csc(N)n3)[C@H]2SC1>CN(C=O)C>CSCC1=C(C(=O)[O-])N2C(=O)C(NC(=O)C(=NO)c3csc(N)n3)[C@H]2SC1
ord_dataset-02ee2261663048188cf6d85d2cc96e3f
ord-259cdfd8194a46da8519bc2b1b2c0ec8
C=CCOCCCCCCCCCCI.COC(=O)c1ccc(O)cc1>>C=CCOCCCCCCCCCCOc1ccc(C(=O)O)cc1
[OH-].[K+].C(C=C)OCCCCCCCCCCI.COC(=O)C=1C=CC(=CC1)O.C([O-])([O-])=O.[K+].[K+].Cl>>C(C=C)OCCCCCCCCCCOC1=CC=C(C(=O)O)C=C1
I[CH2:14][CH2:13][CH2:12][CH2:11][CH2:10][CH2:9][CH2:8][CH2:7][CH2:6][CH2:5][O:4][CH2:3][CH:2]=[CH2:1].C[O:22][C:20]([c:19]1[cH:18][cH:17][c:16]([OH:15])[cH:24][cH:23]1)=[O:21]>>[CH2:1]=[CH:2][CH2:3][O:4][CH2:5][CH2:6][CH2:7][CH2:8][CH2:9][CH2:10][CH2:11][CH2:12][CH2:13][CH2:14][O:15][c:16]1[cH:17][cH:18][c:19]([C:20](...
C=CCOCCCCCCCCCCI.COC(=O)c1ccc(O)cc1
C=CCOCCCCCCCCCCOc1ccc(C(=O)O)cc1
null
null
C(C)O
Heteroatom Alkylation and Arylation
OtherReaction
c47049bacd28cc701f2e77df376a2fcefecd5392e081f9a62473cff265d23a8c
017337a0828c32d10d28543003ae15a8b492b5e2f69019c65a4461eabc617d95
c1ccccc1
C-[O;H0;D2;+0:1]-[C:2](=[O;D1;H0:3])-[c:4].[OH;D1;+0:5]-[c:6](:[c:7]):[c:8].I-[CH2;D2;+0:9]-[C:10]-[C:11]>>[C:11]-[C:10]-[CH2;D2;+0:9]-[O;H0;D2;+0:5]-[c:6](:[c:7]):[c:8].[O;D1;H0:3]=[C:2](-[OH;D1;+0:1])-[c:4]
80
[{"value": 80.0, "product": "C(C=C)OCCCCCCCCCCOC1=CC=C(C(=O)O)C=C1", "details": "PERCENTYIELD", "is_desired": false}, {"value": 79.9, "product": "C(C=C)OCCCCCCCCCCOC1=CC=C(C(=O)O)C=C1", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
80
CELSIUS
null
null
70 mmol (22.7 g) of 10-iododecyl allyl ether, 70 mmol (10.6 g) of methyl p-hydroxybenzoate, and 70 mmol (9.6 g) of potassium carbonate were refluxed in absolute ethanol for 15 hours. After addition of an aqueous potassium hydroxide solution (containing 4.0 g of potassium hydroxide) into the reaction solution, the resul...
10.6084/m9.figshare.5104873.v1
null
Primary halide.Ester.Aromatic alcohol
Carboxylic acid.Ether
null
null
c1ccccc1
HI
C(C)O
80
null
C=CCOCCCCCCCCCCI.COC(=O)c1ccc(O)cc1>C(C)O>C=CCOCCCCCCCCCCOc1ccc(C(=O)O)cc1
ord_dataset-02ee2261663048188cf6d85d2cc96e3f
ord-ef2495e77e554402bda2035c66f5f24f
CCOC(OCC)P(=O)(CCC#N)OCC>>CCOC(OCC)P(=O)(CCCN)OCC
[H][H].C(#N)CCP(OCC)(=O)C(OCC)OCC.N>>NCCCP(OCC)(=O)C(OCC)OCC
[CH3:1][CH2:2][O:3][CH:4]([O:5][CH2:6][CH3:7])[P:8](=[O:9])([CH2:10][CH2:11][C:12]#[N:13])[O:14][CH2:15][CH3:16]>>[CH3:1][CH2:2][O:3][CH:4]([O:5][CH2:6][CH3:7])[P:8](=[O:9])([CH2:10][CH2:11][CH2:12][NH2:13])[O:14][CH2:15][CH3:16]
CCOC(OCC)P(=O)(CCC#N)OCC
CCOC(OCC)P(=O)(CCCN)OCC
null
[Ni]
C(C)O
Reduction
Reduction of nitrile to amine
65bec2d9f430701d30dc9fcbe1c5418f3dfa174d67be035c50edfc71895dc9c7
e8d1bc928b94bd4f5bf4b23363ce8f88b1ce7d146ba93829e7b8ad8dbe0007a7
null
[C:1]-[C:2]-[C;H0;D2;+0:3]#[N;H0;D1;+0:4]>>[C:1]-[C:2]-[CH2;D2;+0:3]-[NH2;D1;+0:4]
null
[]
null
null
null
null
A solution of 9.6 g of ethyl 2-cyanoethyl(diethoxymethyl)phosphinate in 450 ml of ethanol is added to 82 g of an 8% solution of ammonia in ethanol. To this is added 5 ml of Raney Nickel and the resulting mixture is hydrogenated at 1 bar until the theoretical amount of hydrogen has been taken up. The mixture is then fil...
10.6084/m9.figshare.5104873.v1
null
Nitrile
Primary amine
null
null
null
null
[Ni].C(C)O
null
null
CCOC(OCC)P(=O)(CCC#N)OCC>[Ni].C(C)O>CCOC(OCC)P(=O)(CCCN)OCC
ord_dataset-02ee2261663048188cf6d85d2cc96e3f
ord-b947884471ff43dea42884fb63629a10
C/C=C/C#N.CCOC(OCC)P([O-])OCC>>CCOC(OCC)P(=O)(OCC)C(C)CC#N
C(C)(=O)O.C(C)OC(OCC)P(OCC)[O-].C(\C=C\C)#N.[H-].[Na+]>>C(#N)CC(C)P(OCC)(=O)C(OCC)OCC
[CH:13](\[CH3:14])=[CH:15]/[C:16]#[N:17].[CH3:1][CH2:2][O:3][CH:4]([O:5][CH2:6][CH3:7])[P:8]([O-:9])[O:10][CH2:11][CH3:12]>>[CH3:1][CH2:2][O:3][CH:4]([O:5][CH2:6][CH3:7])[P:8](=[O:9])([O:10][CH2:11][CH3:12])[CH:13]([CH3:14])[CH2:15][C:16]#[N:17]
C/C=C/C#N.CCOC(OCC)P([O-])OCC
CCOC(OCC)P(=O)(OCC)C(C)CC#N
null
null
C(C)O
Miscellaneous
OtherReaction
40ba59785861b8226ce5af6bdcbb9a37f0ff50a8c7ec7d4fc4c524cf906cc65c
56ebed4a8b3cebec83c37a71d68f0c87d1e404ab05a9ce792691e4e18a2379dd
null
[#8:1]-[C:2](-[#8:3])-[P;H0;D3;+0:4](-[O-;H0;D1:5])-[#8:6]-[C:7].[C;D1;H3:8]/[CH;D2;+0:9]=[CH;D2;+0:10]/[C:11]#[N;D1;H0:12]>>[#8:1]-[C:2](-[#8:3])-[P;H0;D4;+0:4](=[O;H0;D1;+0:5])(-[#8:6]-[C:7])-[CH;D3;+0:9](-[C;D1;H3:8])-[CH2;D2;+0:10]-[C:11]#[N;D1;H0:12]
null
[]
null
null
4
HOUR
A solution of 23.5 g of ethyl (diethoxymethyl)phosphonite and 6.7 g of crotononitrile in 30 ml of dry ethanol is added to a stirred mixture of 1.2 g of sodium hydride (50% dispersion in oil) in 30 ml of ethanol at 0° C. under an atmosphere of nitrogen. The reaction mixture is allowed to warm to room temperature and sti...
10.6084/m9.figshare.5104873.v1
null
null
null
null
null
null
null
C(C)O
null
4
C/C=C/C#N.CCOC(OCC)P([O-])OCC>C(C)O>CCOC(OCC)P(=O)(OCC)C(C)CC#N
ord_dataset-02ee2261663048188cf6d85d2cc96e3f
ord-8451bd41350741798488ec1da4264c87
CCOC(OCC)P(=O)(OCC)C(C)CC#N>>CCOC(OCC)P(=O)(OCC)C(C)CCN
[H][H].CC(CC#N)P(OCC)(=O)C(OCC)OCC.N>>NCCC(C)P(OCC)(=O)C(OCC)OCC
[CH3:1][CH2:2][O:3][CH:4]([O:5][CH2:6][CH3:7])[P:8](=[O:9])([O:10][CH2:11][CH3:12])[CH:13]([CH3:14])[CH2:15][C:16]#[N:17]>>[CH3:1][CH2:2][O:3][CH:4]([O:5][CH2:6][CH3:7])[P:8](=[O:9])([O:10][CH2:11][CH3:12])[CH:13]([CH3:14])[CH2:15][CH2:16][NH2:17]
CCOC(OCC)P(=O)(OCC)C(C)CC#N
CCOC(OCC)P(=O)(OCC)C(C)CCN
null
[Ni]
C(C)O
Reduction
Reduction of nitrile to amine
65bec2d9f430701d30dc9fcbe1c5418f3dfa174d67be035c50edfc71895dc9c7
e8d1bc928b94bd4f5bf4b23363ce8f88b1ce7d146ba93829e7b8ad8dbe0007a7
null
[C:1]-[C:2]-[C;H0;D2;+0:3]#[N;H0;D1;+0:4]>>[C:1]-[C:2]-[CH2;D2;+0:3]-[NH2;D1;+0:4]
null
[]
null
null
null
null
A solution of 17.0 g of ethyl 1-methyl-2-cyanoethyl(diethoxymethyl)phosphinate in 150 ml of ethanol is added to 155.0 g of an 8% solution of ammonia in ethanol. To this are added 10 ml of Raney Nickel and the resulting mixture is hydrogenated at 1 bar until the theoretical amount of hydrogen has been taken up. The mixt...
10.6084/m9.figshare.5104873.v1
null
Nitrile
Primary amine
null
null
null
null
[Ni].C(C)O
null
null
CCOC(OCC)P(=O)(OCC)C(C)CC#N>[Ni].C(C)O>CCOC(OCC)P(=O)(OCC)C(C)CCN
ord_dataset-02ee2261663048188cf6d85d2cc96e3f
ord-1ae62f932ea54514b4d903d6fdb8d064
CCOC(OCC)P(=O)(CC(C)CN)OCC>>CC(CN)CP(O)O.O
NCC(CP(OCC)(=O)C(OCC)OCC)C>>O.NCC(CP(O)O)C
CCOC([P:6]([CH2:5][CH:2]([CH3:1])[CH2:3][NH2:4])([O:7]CC)=[O:8])[O:9]CC>>[CH3:1][CH:2]([CH2:3][NH2:4])[CH2:5][P:6]([OH:7])[OH:8].[OH2:9]
CCOC(OCC)P(=O)(CC(C)CN)OCC
CC(CN)CP(O)O.O
null
null
Cl
Miscellaneous
OtherReaction
27a7ce5124ce9df58d78a5aef67d94157caa3dd464298a2201254c2545b8416a
79a17d37832f2717ceac93b17ac3ad97b0bc0d876910e15be3eeb8366cf301c1
null
C-C-O-C(-[O;H0;D2;+0:1]-C-C)-[P;H0;D4;+0:2](=[O;H0;D1;+0:3])(-[C:4]-[C:5])-[O;H0;D2;+0:6]-C-C>>[C:5]-[C:4]-[P;H0;D3;+0:2](-[OH;D1;+0:6])-[OH;D1;+0:3].[OH2;D0;+0:1]
null
[]
null
null
null
null
A solution of 6.0 g of ethyl 3-amino-2-methylpropyl(diethoxymethyl)phosphinate in 30 ml of 36% aqueous hydrochloric acid is heated to reflux for a period of 7 hours. The reaction mixture is then allowed to cool to room temperature, concentrated under reduced pressure and co-evaporated twice with 10 ml of water under re...
10.6084/m9.figshare.5104873.v1
null
Ether.Ether
null
null
null
null
HO-
Cl
null
null
CCOC(OCC)P(=O)(CC(C)CN)OCC>Cl>CC(CN)CP(O)O.O
ord_dataset-02ee2261663048188cf6d85d2cc96e3f
ord-eef10675c57b4433ad24a46cb58f9591
C=C(C)C#N.CCOC(OCC)P([O-])OCC>>CCOC(OCC)P(=O)(CC(C)C#N)OCC
C(C)(=O)O.C(C)OC(OCC)P(OCC)[O-].C(C(=C)C)#N.[H-].[Na+]>>C(C)OP(=O)(C(OCC)OCC)CC(C)C#N
[CH2:10]=[C:11]([CH3:12])[C:13]#[N:14].[CH3:1][CH2:2][O:3][CH:4]([O:5][CH2:6][CH3:7])[P:8]([O-:9])[O:15][CH2:16][CH3:17]>>[CH3:1][CH2:2][O:3][CH:4]([O:5][CH2:6][CH3:7])[P:8](=[O:9])([CH2:10][CH:11]([CH3:12])[C:13]#[N:14])[O:15][CH2:16][CH3:17]
C=C(C)C#N.CCOC(OCC)P([O-])OCC
CCOC(OCC)P(=O)(CC(C)C#N)OCC
null
null
C(C)O
Miscellaneous
OtherReaction
6e18384a4cb428c82c20d31730f2ac142cfbf9a333fe90e3d93fcc2d02070c0d
62104ffcb4d4ab6482284e0c7ae124bc1d1d4f4befe80d570c6848ac4dc98f52
null
[#8:1]-[C:2](-[#8:3])-[P;H0;D3;+0:4](-[O-;H0;D1:5])-[#8:6]-[C:7].[C;D1;H3:8]-[C;H0;D3;+0:9](=[CH2;D1;+0:10])-[C:11]#[N;D1;H0:12]>>[#8:1]-[C:2](-[#8:3])-[P;H0;D4;+0:4](=[O;H0;D1;+0:5])(-[#8:6]-[C:7])-[CH2;D2;+0:10]-[CH;D3;+0:9](-[C;D1;H3:8])-[C:11]#[N;D1;H0:12]
null
[]
null
null
4
HOUR
A solution of 23.5 g of ethyl (diethoxymethyl)phosphonite and 6.7 g of methacrylonitrile in 30 ml of ethanol is added dropwise to a stirred mixture of 1.2 g of sodium hydride (50% dispersion in oil) in 30 ml of ethanol at 0° C. under an atmosphere of nitrogen. The reaction mixture is allowed to warm to room temperature...
10.6084/m9.figshare.5104873.v1
null
Vinyl
null
null
null
null
null
C(C)O
null
4
C=C(C)C#N.CCOC(OCC)P([O-])OCC>C(C)O>CCOC(OCC)P(=O)(CC(C)C#N)OCC
ord_dataset-02ee2261663048188cf6d85d2cc96e3f
ord-bd87fbc37fc84c7d8ac7af5c2a634c49
CCOC(OCC)P(=O)(CC(C)C#N)OCC>>CCOC(OCC)P(=O)(CC(C)CN)OCC
[H][H].C(#N)C(CP(OCC)(=O)C(OCC)OCC)C.N>>NCC(CP(OCC)(=O)C(OCC)OCC)C
[CH3:1][CH2:2][O:3][CH:4]([O:5][CH2:6][CH3:7])[P:8](=[O:9])([CH2:10][CH:11]([CH3:12])[C:13]#[N:14])[O:15][CH2:16][CH3:17]>>[CH3:1][CH2:2][O:3][CH:4]([O:5][CH2:6][CH3:7])[P:8](=[O:9])([CH2:10][CH:11]([CH3:12])[CH2:13][NH2:14])[O:15][CH2:16][CH3:17]
CCOC(OCC)P(=O)(CC(C)C#N)OCC
CCOC(OCC)P(=O)(CC(C)CN)OCC
null
[Ni]
C(C)O
Reduction
Reduction of nitrile to amine
65bec2d9f430701d30dc9fcbe1c5418f3dfa174d67be035c50edfc71895dc9c7
e8d1bc928b94bd4f5bf4b23363ce8f88b1ce7d146ba93829e7b8ad8dbe0007a7
null
[C:1]-[C:2](-[C;D1;H3:3])-[C;H0;D2;+0:4]#[N;H0;D1;+0:5]>>[C:1]-[C:2](-[C;D1;H3:3])-[CH2;D2;+0:4]-[NH2;D1;+0:5]
null
[]
null
null
null
null
A solution of 17.0 g of ethyl 2-cyanopropyl(diethoxymethyl)phosphinate in 150 ml of ethanol is added to 155 g of an 8% solution of ammonia in ethanol. To this are added 10 ml of Raney Nickel and the resulting mixture is hydrogenated at 1 bar until the theoretical amount of hydrogen has been taken up. The mixture is the...
10.6084/m9.figshare.5104873.v1
null
Nitrile
Primary amine
null
null
null
null
[Ni].C(C)O
null
null
CCOC(OCC)P(=O)(CC(C)C#N)OCC>[Ni].C(C)O>CCOC(OCC)P(=O)(CC(C)CN)OCC
ord_dataset-02ee2261663048188cf6d85d2cc96e3f
ord-30eae213606d47d0a395349b420efeef
C=CC(C)=O.CCOC(OCC)[PH]([O-])(OCC)[Si](C)(C)C>>CCOC(OCC)P(=O)(CCC(C)=O)OCC
C[Si](C)(C)P(OCC)([O-])C(OCC)OCC.C(=C)C(=O)C.C(Cl)(Cl)Cl>>O=C(CCP(OCC)(=O)C(OCC)OCC)C
[CH2:10]=[CH:11][C:12]([CH3:13])=[O:14].C[Si](C)(C)[PH:8]([CH:4]([O:3][CH2:2][CH3:1])[O:5][CH2:6][CH3:7])([O-:9])[O:15][CH2:16][CH3:17]>>[CH3:1][CH2:2][O:3][CH:4]([O:5][CH2:6][CH3:7])[P:8](=[O:9])([CH2:10][CH2:11][C:12]([CH3:13])=[O:14])[O:15][CH2:16][CH3:17]
C=CC(C)=O.CCOC(OCC)[PH]([O-])(OCC)[Si](C)(C)C
CCOC(OCC)P(=O)(CCC(C)=O)OCC
null
null
O
Miscellaneous
OtherReaction
7d7e0fb375dd2c5cfc37764f94acfc8098223f35039f3d05eac8e8d72fdb3708
5caae0ad5d16d18fc5881c6147ddf5ea7b358c9624a0ebbc0fc9d7ba66c36201
null
C-[Si](-C)(-C)-[PH;D4;+0:1](-[O-;H0;D1:2])(-[#8:3]-[C:4])-[C:5](-[#8:6])-[#8:7].[C;D1;H3:8]-[C:9](=[O;D1;H0:10])-[CH;D2;+0:11]=[CH2;D1;+0:12]>>[#8:6]-[C:5](-[#8:7])-[P;H0;D4;+0:1](=[O;H0;D1;+0:2])(-[#8:3]-[C:4])-[CH2;D2;+0:12]-[CH2;D2;+0:11]-[C:9](-[C;D1;H3:8])=[O;D1;H0:10]
null
[]
50
CELSIUS
0.5
HOUR
15.0 g of ethyl trimethylsilyl(diethoxymethyl)phosphonite are added dropwise to a stirred solution of 3.9 g of methyl vinyl ketone under an atmosphere of nitrogen at room temperature. The mixture is then heated to 50° C. for a period of 1 hour. The mixture is then allowed to cool to room temperature, 25 ml of chlorofor...
10.6084/m9.figshare.5104873.v1
null
Ketone.Vinyl.Silyl protective group
Ketone
null
null
null
Other
O
50
0.5
C=CC(C)=O.CCOC(OCC)[PH]([O-])(OCC)[Si](C)(C)C>O>CCOC(OCC)P(=O)(CCC(C)=O)OCC
ord_dataset-02ee2261663048188cf6d85d2cc96e3f
ord-88ebe0a4089a43fc83a6dd6a91de9f79
CCOC(OCC)P(=O)(CCC(C)=O)OCC.[NH4+]>>CCOC(OCC)P(=O)(CCC(C)N)OCC
Cl.O=C(CCP(OCC)(=O)C(OCC)OCC)C.C(C)(=O)[O-].[NH4+].C(#N)[BH3-].[Na+]>>NC(CCP(OCC)(=O)C(OCC)OCC)C
O=[C:12]([CH2:11][CH2:10][P:8]([CH:4]([O:3][CH2:2][CH3:1])[O:5][CH2:6][CH3:7])(=[O:9])[O:15][CH2:16][CH3:17])[CH3:13].[NH4+:14]>>[CH3:1][CH2:2][O:3][CH:4]([O:5][CH2:6][CH3:7])[P:8](=[O:9])([CH2:10][CH2:11][CH:12]([CH3:13])[NH2:14])[O:15][CH2:16][CH3:17]
CCOC(OCC)P(=O)(CCC(C)=O)OCC.[NH4+]
CCOC(OCC)P(=O)(CCC(C)N)OCC
null
null
CO
Functional Group Interconversion
OtherReaction
14af499c4b742b1ab2135a986a4f7f4e6dda0ad50987736be8cf00d531c63192
2ef9e3e9915394571ec6196ff6ea06bca9f3dff8c6f6f43c81edc876014a94a5
null
O=[C;H0;D3;+0:1](-[C;D1;H3:2])-[C:3]-[C:4].[NH4+;D0:5]>>[C:4]-[C:3]-[CH;D3;+0:1](-[C;D1;H3:2])-[NH2;D1;+0:5]
null
[]
null
null
2.5
HOUR
To a solution of 8.0 g of ethyl 3-oxobutyl(diethoxymethyl)phosphinate in 100 ml of methanol is added 22.8 g of ammonium acetate and 1.3 g of sodium cyanoborohydride. The mixture is stirred under an atmosphere of nitrogen at room temperature for a period of 2.5 h, and then left to stand overnight. The mixture is then ac...
10.6084/m9.figshare.5104873.v1
null
Ketone
Primary amine
null
null
null
HO-
CO
null
2.5
CCOC(OCC)P(=O)(CCC(C)=O)OCC.[NH4+]>CO>CCOC(OCC)P(=O)(CCC(C)N)OCC
ord_dataset-02ee2261663048188cf6d85d2cc96e3f
ord-2d1131dab45645f4ab0bcc2a3bb89e9f
CCOC(OCC)P(=O)(OCC)C(CCN)c1ccc(Cl)cc1>>NCCC(c1ccc(Cl)cc1)P(O)O
NCCC(C1=CC=C(C=C1)Cl)P(OCC)(=O)C(OCC)OCC>>NCCC(C1=CC=C(C=C1)Cl)P(O)O
CCOC(OCC)[P:12]([CH:4]([CH2:3][CH2:2][NH2:1])[c:5]1[cH:6][cH:7][c:8]([Cl:9])[cH:10][cH:11]1)(=[O:13])[O:14]CC>>[NH2:1][CH2:2][CH2:3][CH:4]([c:5]1[cH:6][cH:7][c:8]([Cl:9])[cH:10][cH:11]1)[P:12]([OH:13])[OH:14]
CCOC(OCC)P(=O)(OCC)C(CCN)c1ccc(Cl)cc1
NCCC(c1ccc(Cl)cc1)P(O)O
null
null
Cl
Miscellaneous
OtherReaction
27a7ce5124ce9df58d78a5aef67d94157caa3dd464298a2201254c2545b8416a
79a17d37832f2717ceac93b17ac3ad97b0bc0d876910e15be3eeb8366cf301c1
c1ccccc1
C-C-O-C(-O-C-C)-[P;H0;D4;+0:1](=[O;H0;D1;+0:2])(-[O;H0;D2;+0:3]-C-C)-[C:4](-[C:5])-[c:6]>>[C:5]-[C:4](-[c:6])-[P;H0;D3;+0:1](-[OH;D1;+0:2])-[OH;D1;+0:3]
null
[]
null
null
null
null
A solution of 17.9 g of ethyl 3-amino-1-(4-chlorophenyl)propyl(diethoxymethyl)phosphinate in 200 ml of 36% aqueous hydrochloric acid is heated to reflux for a period of 6 hours. The reaction mixture is then allowed to cool to room temperature, concentrated under reduced pressure and co-evaporated twice with 50 ml of wa...
10.6084/m9.figshare.5104873.v1
null
Ether.Ether
null
null
null
c1ccccc1
HO-
Cl
null
null
CCOC(OCC)P(=O)(OCC)C(CCN)c1ccc(Cl)cc1>Cl>NCCC(c1ccc(Cl)cc1)P(O)O
ord_dataset-02ee2261663048188cf6d85d2cc96e3f
ord-c9b492f8af154b9a8a86074c4ebadc12
CCOC(OCC)P([O-])OCC.N#CC=Cc1ccc(Cl)cc1>>CCOC(OCC)P(=O)(OCC)C(CC#N)c1ccc(Cl)cc1
C(C)(=O)O.C(C)OC(OCC)P(OCC)[O-].ClC1=CC=C(C=CC#N)C=C1.[H-].[Na+]>>ClC1=CC=C(C=C1)C(CC#N)P(OCC)(=O)C(OCC)OCC
[CH3:1][CH2:2][O:3][CH:4]([O:5][CH2:6][CH3:7])[P:8]([O-:9])[O:10][CH2:11][CH3:12].[CH:13](=[CH:14][C:15]#[N:16])[c:17]1[cH:18][cH:19][c:20]([Cl:21])[cH:22][cH:23]1>>[CH3:1][CH2:2][O:3][CH:4]([O:5][CH2:6][CH3:7])[P:8](=[O:9])([O:10][CH2:11][CH3:12])[CH:13]([CH2:14][C:15]#[N:16])[c:17]1[cH:18][cH:19][c:20]([Cl:21])[cH:22...
CCOC(OCC)P([O-])OCC.N#CC=Cc1ccc(Cl)cc1
CCOC(OCC)P(=O)(OCC)C(CC#N)c1ccc(Cl)cc1
null
null
C(C)O
Miscellaneous
OtherReaction
40ba59785861b8226ce5af6bdcbb9a37f0ff50a8c7ec7d4fc4c524cf906cc65c
56ebed4a8b3cebec83c37a71d68f0c87d1e404ab05a9ce792691e4e18a2379dd
c1ccccc1
[#8:1]-[C:2](-[#8:3])-[P;H0;D3;+0:4](-[O-;H0;D1:5])-[#8:6]-[C:7].[N;D1;H0:8]#[C:9]-[CH;D2;+0:10]=[CH;D2;+0:11]-[c:12](:[c:13]):[c:14]>>[#8:1]-[C:2](-[#8:3])-[P;H0;D4;+0:4](=[O;H0;D1;+0:5])(-[#8:6]-[C:7])-[CH;D3;+0:11](-[CH2;D2;+0:10]-[C:9]#[N;D1;H0:8])-[c:12](:[c:13]):[c:14]
null
[]
null
null
4
HOUR
A solution of 25.8 g of ethyl (diethoxymethyl)phosphonite and 18.0 g of 4-chlorocinnamonitrile in 100 ml of ethanol is added to a stirred mixture of 1.2 g of sodium hydride (50% dispersion in oil) in 30 ml of ethanol at 0° C. under an atmosphere of nitrogen. The reaction mixture is allowed to warm to room temperature a...
10.6084/m9.figshare.5104873.v1
null
null
null
null
null
c1ccccc1
null
C(C)O
null
4
CCOC(OCC)P([O-])OCC.N#CC=Cc1ccc(Cl)cc1>C(C)O>CCOC(OCC)P(=O)(OCC)C(CC#N)c1ccc(Cl)cc1
ord_dataset-02ee2261663048188cf6d85d2cc96e3f
ord-ccb1ee78f6554d898be6494680e71a61
CCOC(OCC)P(=O)(OCC)C(CC#N)c1ccc(Cl)cc1>>CCOC(OCC)P(=O)(OCC)C(CCN)c1ccc(Cl)cc1
[H][H].ClC1=CC=C(C=C1)C(CC#N)P(OCC)(=O)C(OCC)OCC.N>>NCCC(C1=CC=C(C=C1)Cl)P(OCC)(=O)C(OCC)OCC
[CH3:1][CH2:2][O:3][CH:4]([O:5][CH2:6][CH3:7])[P:8](=[O:9])([O:10][CH2:11][CH3:12])[CH:13]([CH2:14][C:15]#[N:16])[c:17]1[cH:18][cH:19][c:20]([Cl:21])[cH:22][cH:23]1>>[CH3:1][CH2:2][O:3][CH:4]([O:5][CH2:6][CH3:7])[P:8](=[O:9])([O:10][CH2:11][CH3:12])[CH:13]([CH2:14][CH2:15][NH2:16])[c:17]1[cH:18][cH:19][c:20]([Cl:21])[c...
CCOC(OCC)P(=O)(OCC)C(CC#N)c1ccc(Cl)cc1
CCOC(OCC)P(=O)(OCC)C(CCN)c1ccc(Cl)cc1
null
[Ni]
C(C)O
Reduction
Reduction of nitrile to amine
65bec2d9f430701d30dc9fcbe1c5418f3dfa174d67be035c50edfc71895dc9c7
e8d1bc928b94bd4f5bf4b23363ce8f88b1ce7d146ba93829e7b8ad8dbe0007a7
c1ccccc1
[C:1]-[C:2]-[C;H0;D2;+0:3]#[N;H0;D1;+0:4]>>[C:1]-[C:2]-[CH2;D2;+0:3]-[NH2;D1;+0:4]
null
[]
null
null
null
null
A solution of 20 g of ethyl 1-(4-chlorophenyl)-2-cyanoethyl(diethoxymethyl)phosphinate in 85 ml of ethanol is added to 131 g of an 8% solution of ammonia in ethanol. To this are added 8.5 ml of Raney Nickel and the resulting mixture is hydrogenated at 1 bar until the theoretical amount of hydrogen has been taken up. Th...
10.6084/m9.figshare.5104873.v1
null
Nitrile
Primary amine
null
null
c1ccccc1
null
[Ni].C(C)O
null
null
CCOC(OCC)P(=O)(OCC)C(CC#N)c1ccc(Cl)cc1>[Ni].C(C)O>CCOC(OCC)P(=O)(OCC)C(CCN)c1ccc(Cl)cc1
ord_dataset-02ee2261663048188cf6d85d2cc96e3f
ord-55868750e6b040479bb094ca25ef81c9
CCOC(OCC)P(=O)(CCC(N)c1ccc(Cl)cc1)OCC>>NC(CCP(O)O)c1ccc(Cl)cc1
NC(CCP(OCC)(=O)C(OCC)OCC)C1=CC=C(C=C1)Cl>>NC(CCP(O)O)C1=CC=C(C=C1)Cl
CCOC(OCC)[P:5]([CH2:4][CH2:3][CH:2]([NH2:1])[c:8]1[cH:9][cH:10][c:11]([Cl:12])[cH:13][cH:14]1)([O:6]CC)=[O:7]>>[NH2:1][CH:2]([CH2:3][CH2:4][P:5]([OH:6])[OH:7])[c:8]1[cH:9][cH:10][c:11]([Cl:12])[cH:13][cH:14]1
CCOC(OCC)P(=O)(CCC(N)c1ccc(Cl)cc1)OCC
NC(CCP(O)O)c1ccc(Cl)cc1
null
null
Cl
Miscellaneous
OtherReaction
27a7ce5124ce9df58d78a5aef67d94157caa3dd464298a2201254c2545b8416a
79a17d37832f2717ceac93b17ac3ad97b0bc0d876910e15be3eeb8366cf301c1
c1ccccc1
C-C-O-C(-O-C-C)-[P;H0;D4;+0:1](=[O;H0;D1;+0:2])(-[C:3]-[C:4])-[O;H0;D2;+0:5]-C-C>>[C:4]-[C:3]-[P;H0;D3;+0:1](-[OH;D1;+0:5])-[OH;D1;+0:2]
null
[]
null
null
null
null
A solution of 10.5 g of ethyl 3-amino-3-(4-chlorophenyl)propyl(diethoxymethyl)phosphinate in 100 ml of 36% aqueous hydrochloric acid is heated to reflux for a period of 2 hours. The reaction mixture is then allowed to cool to room temperature, concentrated under reduced pressure, and co-evaporated twice with 25 ml of w...
10.6084/m9.figshare.5104873.v1
null
Ether.Ether
null
null
null
c1ccccc1
HO-
Cl
null
null
CCOC(OCC)P(=O)(CCC(N)c1ccc(Cl)cc1)OCC>Cl>NC(CCP(O)O)c1ccc(Cl)cc1
ord_dataset-02ee2261663048188cf6d85d2cc96e3f
ord-8b74142270b4473b95606c08d755bcbc
C=CC(=O)c1ccc(Cl)cc1.CCOC(OCC)[PH]([O-])(OCC)[Si](C)(C)C>>CCOC(OCC)P(=O)(CCC(=O)c1ccc(Cl)cc1)OCC
C[Si](C)(C)P(OCC)([O-])C(OCC)OCC.C(=C)C(=O)C1=CC=C(C=C1)Cl.C(Cl)(Cl)Cl>>ClC1=CC=C(C(=O)CCP(OCC)(=O)C(OCC)OCC)C=C1
[CH2:10]=[CH:11][C:12](=[O:13])[c:14]1[cH:15][cH:16][c:17]([Cl:18])[cH:19][cH:20]1.C[Si](C)(C)[PH:8]([CH:4]([O:3][CH2:2][CH3:1])[O:5][CH2:6][CH3:7])([O-:9])[O:21][CH2:22][CH3:23]>>[CH3:1][CH2:2][O:3][CH:4]([O:5][CH2:6][CH3:7])[P:8](=[O:9])([CH2:10][CH2:11][C:12](=[O:13])[c:14]1[cH:15][cH:16][c:17]([Cl:18])[cH:19][cH:20...
C=CC(=O)c1ccc(Cl)cc1.CCOC(OCC)[PH]([O-])(OCC)[Si](C)(C)C
CCOC(OCC)P(=O)(CCC(=O)c1ccc(Cl)cc1)OCC
null
null
O
Miscellaneous
OtherReaction
7d7e0fb375dd2c5cfc37764f94acfc8098223f35039f3d05eac8e8d72fdb3708
5caae0ad5d16d18fc5881c6147ddf5ea7b358c9624a0ebbc0fc9d7ba66c36201
c1ccccc1
C-[Si](-C)(-C)-[PH;D4;+0:1](-[O-;H0;D1:2])(-[#8:3]-[C:4])-[C:5](-[#8:6])-[#8:7].[CH2;D1;+0:8]=[CH;D2;+0:9]-[C:10](=[O;D1;H0:11])-[c:12]>>[#8:6]-[C:5](-[#8:7])-[P;H0;D4;+0:1](=[O;H0;D1;+0:2])(-[#8:3]-[C:4])-[CH2;D2;+0:8]-[CH2;D2;+0:9]-[C:10](=[O;D1;H0:11])-[c:12]
null
[]
null
null
1
HOUR
17.7 g of ethyl trimethylsilyl(diethoxymethyl)phosphonite is added dropwise to a stirred solution of 11.7 g of 4-chlorophenyl vinyl ketone under an atmosphere of nitrogen, at room temperature. The reaction mixture is stirred for a period of 1 hour, 25 ml of chloroform is added followed by 10 ml of water and this mixtur...
10.6084/m9.figshare.5104873.v1
null
Ketone.Vinyl.Silyl protective group
Ketone
null
null
c1ccccc1
Other
O
null
1
C=CC(=O)c1ccc(Cl)cc1.CCOC(OCC)[PH]([O-])(OCC)[Si](C)(C)C>O>CCOC(OCC)P(=O)(CCC(=O)c1ccc(Cl)cc1)OCC
ord_dataset-02ee2261663048188cf6d85d2cc96e3f
ord-289773cedfb2422f9ae710bf263f973b
CCOC(OCC)P(=O)(CCC(=O)c1ccc(Cl)cc1)OCC.[NH4+]>>CCOC(OCC)P(=O)(CCC(N)c1ccc(Cl)cc1)OCC
Cl.ClC1=CC=C(C(=O)CCP(OCC)(=O)C(OCC)OCC)C=C1.C(C)(=O)[O-].[NH4+].C(#N)[BH3-].[Na+]>>NC(CCP(OCC)(=O)C(OCC)OCC)C1=CC=C(C=C1)Cl
O=[C:12]([CH2:11][CH2:10][P:8]([CH:4]([O:3][CH2:2][CH3:1])[O:5][CH2:6][CH3:7])(=[O:9])[O:21][CH2:22][CH3:23])[c:14]1[cH:15][cH:16][c:17]([Cl:18])[cH:19][cH:20]1.[NH4+:13]>>[CH3:1][CH2:2][O:3][CH:4]([O:5][CH2:6][CH3:7])[P:8](=[O:9])([CH2:10][CH2:11][CH:12]([NH2:13])[c:14]1[cH:15][cH:16][c:17]([Cl:18])[cH:19][cH:20]1)[O:...
CCOC(OCC)P(=O)(CCC(=O)c1ccc(Cl)cc1)OCC.[NH4+]
CCOC(OCC)P(=O)(CCC(N)c1ccc(Cl)cc1)OCC
null
null
CO
Functional Group Interconversion
OtherReaction
14af499c4b742b1ab2135a986a4f7f4e6dda0ad50987736be8cf00d531c63192
2ef9e3e9915394571ec6196ff6ea06bca9f3dff8c6f6f43c81edc876014a94a5
c1ccccc1
O=[C;H0;D3;+0:1](-[C:2]-[C:3])-[c:4](:[c:5]):[c:6].[NH4+;D0:7]>>[C:3]-[C:2]-[CH;D3;+0:1](-[NH2;D1;+0:7])-[c:4](:[c:5]):[c:6]
null
[]
null
null
3
DAY
To a solution of 25.4 g of ethyl 2-(4-chlorobenzoyl)ethyl(diethoxymethyl)phosphinate in 200 ml of methanol is added 52 g of ammonium acetate and 4.23 g of sodium cyanoborohydride. The mixture is stirred under an atmosphere of nitrogen at room temperature for a period of 3 days. The mixture is then acidified to pH 2 wit...
10.6084/m9.figshare.5104873.v1
null
Ketone
Primary amine
null
null
c1ccccc1
HO-
CO
null
72
CCOC(OCC)P(=O)(CCC(=O)c1ccc(Cl)cc1)OCC.[NH4+]>CO>CCOC(OCC)P(=O)(CCC(N)c1ccc(Cl)cc1)OCC
ord_dataset-02ee2261663048188cf6d85d2cc96e3f
ord-5d3d5e2e87004cd9903c0e82a10c90bf
CCOC(OCC)P(=O)(CC(CN)c1ccc(Cl)cc1)OCC>>NCC(CP(O)O)c1ccc(Cl)cc1
NCC(CP(OCC)(=O)C(OCC)OCC)C1=CC=C(C=C1)Cl>>NCC(CP(O)O)C1=CC=C(C=C1)Cl
CCOC(OCC)[P:5]([CH2:4][CH:3]([CH2:2][NH2:1])[c:8]1[cH:9][cH:10][c:11]([Cl:12])[cH:13][cH:14]1)([O:6]CC)=[O:7]>>[NH2:1][CH2:2][CH:3]([CH2:4][P:5]([OH:6])[OH:7])[c:8]1[cH:9][cH:10][c:11]([Cl:12])[cH:13][cH:14]1
CCOC(OCC)P(=O)(CC(CN)c1ccc(Cl)cc1)OCC
NCC(CP(O)O)c1ccc(Cl)cc1
null
null
Cl
Miscellaneous
OtherReaction
27a7ce5124ce9df58d78a5aef67d94157caa3dd464298a2201254c2545b8416a
79a17d37832f2717ceac93b17ac3ad97b0bc0d876910e15be3eeb8366cf301c1
c1ccccc1
C-C-O-C(-O-C-C)-[P;H0;D4;+0:1](=[O;H0;D1;+0:2])(-[C:3]-[C:4])-[O;H0;D2;+0:5]-C-C>>[C:4]-[C:3]-[P;H0;D3;+0:1](-[OH;D1;+0:5])-[OH;D1;+0:2]
null
[]
null
null
null
null
A solution of 5.0 g of ethyl 3-amino-2-(4-chlorophenyl)propyl(diethoxymethyl)phosphinate in 60 ml of 36% aqueous hydrochloric acid is heated to reflux for a period of 1 h. The reaction mixture is then allowed to cool to room temperature, concentrated under reduced pressure and co-evaporated twice with 20 ml of water un...
10.6084/m9.figshare.5104873.v1
null
Ether.Ether
null
null
null
c1ccccc1
HO-
Cl
null
null
CCOC(OCC)P(=O)(CC(CN)c1ccc(Cl)cc1)OCC>Cl>NCC(CP(O)O)c1ccc(Cl)cc1
ord_dataset-02ee2261663048188cf6d85d2cc96e3f
ord-5452f2a370614bcb8a2b00ea97ee9967
CCOC(OCC)P(C)(=O)OCC.O=[N+]([O-])C=Cc1ccc(Cl)cc1>>CCOC(OCC)P(=O)(CC(C[N+](=O)[O-])c1ccc(Cl)cc1)OCC
ClC1=CC=C(C=C[N+](=O)[O-])C=C1.C(C)OC(OCC)P(OCC)(=O)C.[Cl-].[NH4+].C(C)(C)NC(C)C.C(CCC)[Li]>>ClC1=CC=C(C=C1)C(CP(OCC)(=O)C(OCC)OCC)C[N+](=O)[O-]
[CH3:1][CH2:2][O:3][CH:4]([O:5][CH2:6][CH3:7])[P:8](=[O:9])([CH3:10])[O:23][CH2:24][CH3:25].[CH:11](=[CH:12][N+:13](=[O:14])[O-:15])[c:16]1[cH:17][cH:18][c:19]([Cl:20])[cH:21][cH:22]1>>[CH3:1][CH2:2][O:3][CH:4]([O:5][CH2:6][CH3:7])[P:8](=[O:9])([CH2:10][CH:11]([CH2:12][N+:13](=[O:14])[O-:15])[c:16]1[cH:17][cH:18][c:19]...
CCOC(OCC)P(C)(=O)OCC.O=[N+]([O-])C=Cc1ccc(Cl)cc1
CCOC(OCC)P(=O)(CC(C[N+](=O)[O-])c1ccc(Cl)cc1)OCC
null
null
CCCCCC.O1CCCC1
C-C Coupling
Michael addition methyl
4792ab23977aa8f2d8848039e3cf8e0149eb8bcd2b5b236e5f3910f20c70f1a9
62f7b8b1b06d8abe0a7458fcdb08bc1ff61c22493460bb08abd465e204dda1f5
c1ccccc1
[#8:1]-[#15:2](-[C:3])(-[CH3;D1;+0:4])=[O;D1;H0:5].[O;-;D1;H0:6]-[#7;+:7](=[O;D1;H0:8])-[CH;D2;+0:9]=[CH;D2;+0:10]-[c:11](:[c:12]):[c:13]>>[#8:1]-[#15:2](-[C:3])(=[O;D1;H0:5])-[CH2;D2;+0:4]-[CH;D3;+0:10](-[CH2;D2;+0:9]-[#7;+:7](-[O;-;D1;H0:6])=[O;D1;H0:8])-[c:11](:[c:12]):[c:13]
null
[]
null
null
10
MINUTE
To a solution of 1.16 g of diisopropylamine in 40 ml of tetrahydrofuran at -78° C. under an atmosphere of nitrogen are added 7.2 ml of a 1.6M solution of n-butyllithium in hexane. This solution is then stirred for a period of 10 minutes at this temperature, after which time a solution of 2.0 g of ethyl (diethoxymethyl)...
10.6084/m9.figshare.5104873.v1
null
Enamine
Nitro group
null
null
c1ccccc1
null
CCCCCC.O1CCCC1
null
0.166667
CCOC(OCC)P(C)(=O)OCC.O=[N+]([O-])C=Cc1ccc(Cl)cc1>CCCCCC.O1CCCC1>CCOC(OCC)P(=O)(CC(C[N+](=O)[O-])c1ccc(Cl)cc1)OCC
ord_dataset-02ee2261663048188cf6d85d2cc96e3f
ord-c5a1a84c29f44ee782fe93c28e070f30
CCOC(OCC)P(=O)(CC(CN)C1CCCCC1)OCC>>NCC(CP(O)O)C1CCCCC1
NCC(CP(OCC)(=O)C(OCC)OCC)C1CCCCC1>>NCC(CP(O)O)C1CCCCC1
CCOC(OCC)[P:5]([CH2:4][CH:3]([CH2:2][NH2:1])[CH:8]1[CH2:9][CH2:10][CH2:11][CH2:12][CH2:13]1)(=[O:6])[O:7]CC>>[NH2:1][CH2:2][CH:3]([CH2:4][P:5]([OH:6])[OH:7])[CH:8]1[CH2:9][CH2:10][CH2:11][CH2:12][CH2:13]1
CCOC(OCC)P(=O)(CC(CN)C1CCCCC1)OCC
NCC(CP(O)O)C1CCCCC1
null
null
Cl
Miscellaneous
OtherReaction
27a7ce5124ce9df58d78a5aef67d94157caa3dd464298a2201254c2545b8416a
79a17d37832f2717ceac93b17ac3ad97b0bc0d876910e15be3eeb8366cf301c1
C1CCCCC1
C-C-O-C(-O-C-C)-[P;H0;D4;+0:1](=[O;H0;D1;+0:2])(-[C:3]-[C:4])-[O;H0;D2;+0:5]-C-C>>[C:4]-[C:3]-[P;H0;D3;+0:1](-[OH;D1;+0:2])-[OH;D1;+0:5]
null
[]
null
null
null
null
A solution of 1.4 g of ethyl 3-amino-2-cyclohexylpropyl(diethoxymethyl)phosphinate in 30 ml of 36% aqueous hydrochloric acid is heated to reflux for a period of 1 hour. The reaction mixture is then allowed to cool to room temperature, concentrated under reduced pressure and co-evaporated twice with 10 ml of water under...
10.6084/m9.figshare.5104873.v1
null
Ether.Ether
null
null
null
C1CCCCC1
HO-
Cl
null
null
CCOC(OCC)P(=O)(CC(CN)C1CCCCC1)OCC>Cl>NCC(CP(O)O)C1CCCCC1
ord_dataset-02ee2261663048188cf6d85d2cc96e3f
ord-8eac40f644db47c7bd864d7aafcf3b39
CCOC(OCC)P(C)(=O)OCC.O=[N+]([O-])C=Cc1ccccc1>>CCOC(OCC)P(=O)(CC(C[N+](=O)[O-])c1ccccc1)OCC
[N+](=O)([O-])C=CC1=CC=CC=C1.C(C)OC(OCC)P(OCC)(=O)C.[Cl-].[NH4+].C(C)(C)NC(C)C.C(CCC)[Li]>>[N+](=O)([O-])CC(CP(OCC)(=O)C(OCC)OCC)C1=CC=CC=C1
[CH3:1][CH2:2][O:3][CH:4]([O:5][CH2:6][CH3:7])[P:8](=[O:9])([CH3:10])[O:22][CH2:23][CH3:24].[CH:11](=[CH:12][N+:13](=[O:14])[O-:15])[c:16]1[cH:17][cH:18][cH:19][cH:20][cH:21]1>>[CH3:1][CH2:2][O:3][CH:4]([O:5][CH2:6][CH3:7])[P:8](=[O:9])([CH2:10][CH:11]([CH2:12][N+:13](=[O:14])[O-:15])[c:16]1[cH:17][cH:18][cH:19][cH:20]...
CCOC(OCC)P(C)(=O)OCC.O=[N+]([O-])C=Cc1ccccc1
CCOC(OCC)P(=O)(CC(C[N+](=O)[O-])c1ccccc1)OCC
null
null
CCCCCC.O1CCCC1
C-C Coupling
Michael addition methyl
4792ab23977aa8f2d8848039e3cf8e0149eb8bcd2b5b236e5f3910f20c70f1a9
62f7b8b1b06d8abe0a7458fcdb08bc1ff61c22493460bb08abd465e204dda1f5
c1ccccc1
[#8:1]-[#15:2](-[C:3])(-[CH3;D1;+0:4])=[O;D1;H0:5].[O;-;D1;H0:6]-[#7;+:7](=[O;D1;H0:8])-[CH;D2;+0:9]=[CH;D2;+0:10]-[c:11](:[c:12]):[c:13]>>[#8:1]-[#15:2](-[C:3])(=[O;D1;H0:5])-[CH2;D2;+0:4]-[CH;D3;+0:10](-[CH2;D2;+0:9]-[#7;+:7](-[O;-;D1;H0:6])=[O;D1;H0:8])-[c:11](:[c:12]):[c:13]
null
[]
null
null
10
MINUTE
To a solution of 5.8 g of diisopropylamine in 40 ml of tetrahydrofuran at -78° C. under an atmosphere of nitrogen are added 35.7 ml of a 1.6M solution of n-butyllithium in hexane. This solution is then stirred for a period of 10 minutes at this temperature, after which time a solution of 10.0 g of ethyl (diethoxymethyl...
10.6084/m9.figshare.5104873.v1
null
Enamine
Nitro group
null
null
c1ccccc1
null
CCCCCC.O1CCCC1
null
0.166667
CCOC(OCC)P(C)(=O)OCC.O=[N+]([O-])C=Cc1ccccc1>CCCCCC.O1CCCC1>CCOC(OCC)P(=O)(CC(C[N+](=O)[O-])c1ccccc1)OCC
ord_dataset-02ee2261663048188cf6d85d2cc96e3f
ord-c56a0fae75ff4778b92cc4966c5ef390
CCOC(OCC)P(=O)(CC(C[N+](=O)[O-])c1ccccc1)OCC>>CCOC(OCC)P(=O)(CC(CN)c1ccccc1)OCC
[H][H].[N+](=O)([O-])CC(CP(OCC)(=O)C(OCC)OCC)C1=CC=CC=C1.N>>NCC(CP(OCC)(=O)C(OCC)OCC)C1=CC=CC=C1
O=[N+:13]([O-])[CH2:12][CH:11]([CH2:10][P:8]([CH:4]([O:3][CH2:2][CH3:1])[O:5][CH2:6][CH3:7])(=[O:9])[O:20][CH2:21][CH3:22])[c:14]1[cH:15][cH:16][cH:17][cH:18][cH:19]1>>[CH3:1][CH2:2][O:3][CH:4]([O:5][CH2:6][CH3:7])[P:8](=[O:9])([CH2:10][CH:11]([CH2:12][NH2:13])[c:14]1[cH:15][cH:16][cH:17][cH:18][cH:19]1)[O:20][CH2:21][...
CCOC(OCC)P(=O)(CC(C[N+](=O)[O-])c1ccccc1)OCC
CCOC(OCC)P(=O)(CC(CN)c1ccccc1)OCC
null
[Ni]
C(C)O
Reduction
Reduction of nitro groups to amines
bbc242b150a51e69d3ad1caaa391f4422710431b398dcb880555f476706790be
7b0317532ea57a4fcedc1efc3e3c22eb5238d1c8330da53d4f9801fc2391f567
c1ccccc1
O=[N+;H0;D3:1](-[O-])-[C:2]-[C:3]>>[C:3]-[C:2]-[NH2;D1;+0:1]
null
[]
null
null
null
null
A solution of 1.0 g of ethyl 3-nitro-2-phenylpropyl(diethoxymethyl)phosphinate in 25 ml of ethanol is added to 25 g of an 8% solution of ammonia in ethanol. To this are added 0.5 ml of Raney Nickel and the resulting mixture hydrogenated at 1 bar until the theoretical amount of hydrogen has been taken up. The mixture is...
10.6084/m9.figshare.5104873.v1
null
Nitro group
Primary amine
null
null
c1ccccc1
Other
[Ni].C(C)O
null
null
CCOC(OCC)P(=O)(CC(C[N+](=O)[O-])c1ccccc1)OCC>[Ni].C(C)O>CCOC(OCC)P(=O)(CC(CN)c1ccccc1)OCC
ord_dataset-02ee2261663048188cf6d85d2cc96e3f
ord-a5f9fd3310074c17a1faf12c0f5dc92c
CCOC(OCC)P(=O)(CC(CN)c1ccccc1)OCC>>CCOC(OCC)P(=O)(CC(CN)C1CCCCC1)OCC
NCC(CP(OCC)(=O)C(OCC)OCC)C1=CC=CC=C1>>NCC(CP(OCC)(=O)C(OCC)OCC)C1CCCCC1
[CH3:1][CH2:2][O:3][CH:4]([O:5][CH2:6][CH3:7])[P:8](=[O:9])([CH2:10][CH:11]([CH2:12][NH2:13])[c:14]1[cH:15][cH:16][cH:17][cH:18][cH:19]1)[O:20][CH2:21][CH3:22]>>[CH3:1][CH2:2][O:3][CH:4]([O:5][CH2:6][CH3:7])[P:8](=[O:9])([CH2:10][CH:11]([CH2:12][NH2:13])[CH:14]1[CH2:15][CH2:16][CH2:17][CH2:18][CH2:19]1)[O:20][CH2:21][C...
CCOC(OCC)P(=O)(CC(CN)c1ccccc1)OCC
CCOC(OCC)P(=O)(CC(CN)C1CCCCC1)OCC
null
[Rh]
C(C)(C)(C)O
Reduction
Arene hydrogenation
cfd1f3b98f7cd3ca3735c14f302dc0acdc6f0d4501cd6920cbb5c1a3d892ff3a
312e9350dcad67590617294c0eb017edf0b9fbfe6133c06a3f393b871a889092
C1CCCCC1
[C:1]-[C:2](-[C:3])-[c;H0;D3;+0:4]1:[cH;D2;+0:5]:[cH;D2;+0:6]:[cH;D2;+0:7]:[cH;D2;+0:8]:[cH;D2;+0:9]:1>>[C:1]-[C:2](-[C:3])-[CH;D3;+0:4]1-[CH2;D2;+0:5]-[CH2;D2;+0:6]-[CH2;D2;+0:7]-[CH2;D2;+0:8]-[CH2;D2;+0:9]-1
null
[]
null
null
20
HOUR
A solution of 3.45 g of ethyl 3-amino-2-phenylpropyl(diethoxymethyl)phosphinate in 25 ml of tertiary butanol is added to 2.0 g of 5% rhodium in alumina, suspended in 25 ml of tertiary butanol. The resulting mixture is hydrogenated at an atmosphere of 150 bar and temperature of 100° C. for a period of 20 hours. The mixt...
10.6084/m9.figshare.5104873.v1
null
null
null
c1ccccc1
C1CCCCC1
C1CCCCC1
null
[Rh].C(C)(C)(C)O
null
20
CCOC(OCC)P(=O)(CC(CN)c1ccccc1)OCC>[Rh].C(C)(C)(C)O>CCOC(OCC)P(=O)(CC(CN)C1CCCCC1)OCC
ord_dataset-02ee2261663048188cf6d85d2cc96e3f
ord-0233c2129abb4c02a5960c402417b8d8
CCOC(OCC)P(=O)(CC(CN)Cc1ccccc1)OCC>>NCC(Cc1ccccc1)CP(O)O
NCC(CP(OCC)(=O)C(OCC)OCC)CC1=CC=CC=C1>>NCC(CP(O)O)CC1=CC=CC=C1
CCOC(OCC)[P:12]([CH2:11][CH:3]([CH2:2][NH2:1])[CH2:4][c:5]1[cH:6][cH:7][cH:8][cH:9][cH:10]1)(=[O:13])[O:14]CC>>[NH2:1][CH2:2][CH:3]([CH2:4][c:5]1[cH:6][cH:7][cH:8][cH:9][cH:10]1)[CH2:11][P:12]([OH:13])[OH:14]
CCOC(OCC)P(=O)(CC(CN)Cc1ccccc1)OCC
NCC(Cc1ccccc1)CP(O)O
null
null
Cl
Miscellaneous
OtherReaction
27a7ce5124ce9df58d78a5aef67d94157caa3dd464298a2201254c2545b8416a
79a17d37832f2717ceac93b17ac3ad97b0bc0d876910e15be3eeb8366cf301c1
c1ccccc1
C-C-O-C(-O-C-C)-[P;H0;D4;+0:1](=[O;H0;D1;+0:2])(-[C:3]-[C:4])-[O;H0;D2;+0:5]-C-C>>[C:4]-[C:3]-[P;H0;D3;+0:1](-[OH;D1;+0:2])-[OH;D1;+0:5]
null
[]
null
null
null
null
A solution of 3.5 g of ethyl 3-amino-2-benzylpropyl(diethoxymethyl)phosphinate in 35 ml of 36% aqueous hydrochloric acid is heated to reflux for a period of 3 hours. The reaction mixture is then allowed to cool to room temperature, concentrated under reduced pressure and co-evaporated twice with 20 ml of water under re...
10.6084/m9.figshare.5104873.v1
null
Ether.Ether
null
null
null
c1ccccc1
HO-
Cl
null
null
CCOC(OCC)P(=O)(CC(CN)Cc1ccccc1)OCC>Cl>NCC(Cc1ccccc1)CP(O)O
ord_dataset-02ee2261663048188cf6d85d2cc96e3f
ord-856eab2a0560410681b793d4b1b773fd
BrCc1ccccc1.CCOC(OCC)P(=O)(CCC#N)OCC>>CCOC(OCC)P(=O)(CC(C#N)Cc1ccccc1)OCC
C(C1=CC=CC=C1)Br.C(#N)CCP(OCC)(=O)C(OCC)OCC.[Cl-].[NH4+].C(C)(C)NC(C)C.C(CCC)[Li]>>C(C1=CC=CC=C1)C(CP(OCC)(=O)C(OCC)OCC)C#N
Br[CH2:14][c:15]1[cH:16][cH:17][cH:18][cH:19][cH:20]1.[CH3:1][CH2:2][O:3][CH:4]([O:5][CH2:6][CH3:7])[P:8](=[O:9])([CH2:10][CH2:11][C:12]#[N:13])[O:21][CH2:22][CH3:23]>>[CH3:1][CH2:2][O:3][CH:4]([O:5][CH2:6][CH3:7])[P:8](=[O:9])([CH2:10][CH:11]([C:12]#[N:13])[CH2:14][c:15]1[cH:16][cH:17][cH:18][cH:19][cH:20]1)[O:21][CH2...
BrCc1ccccc1.CCOC(OCC)P(=O)(CCC#N)OCC
CCOC(OCC)P(=O)(CC(C#N)Cc1ccccc1)OCC
null
null
CCCCCC.O1CCCC1
C-C Coupling
OtherReaction
15973705e8ad8fc52aace4e951dc2397c95f8af8fb2361e425388262f1895099
f5e5e22797736d188bba28deb76a4cee8e4fee4dca04fe24f733d2ee68a23361
c1ccccc1
Br-[CH2;D2;+0:1]-[c:2](:[c:3]):[c:4].[#15:5]-[C:6]-[CH2;D2;+0:7]-[C:8]#[N;D1;H0:9]>>[#15:5]-[C:6]-[CH;D3;+0:7](-[C:8]#[N;D1;H0:9])-[CH2;D2;+0:1]-[c:2](:[c:3]):[c:4]
null
[]
null
null
10
MINUTE
To a solution of 0.97 g of diisopropylamine in 40 ml of tetrahydrofuran at -78° C. under an atmosphere of nitrogen are added 6.0 ml of a 1.6M solution of n-butyllithium in hexane. This solution is then stirred for a period of 10 minutes at this temperature, after which time a solution of 2.0 g of ethyl 2-cyanoethyl(die...
10.6084/m9.figshare.5104873.v1
null
Primary halide
null
null
null
c1ccccc1
HBr
CCCCCC.O1CCCC1
null
0.166667
BrCc1ccccc1.CCOC(OCC)P(=O)(CCC#N)OCC>CCCCCC.O1CCCC1>CCOC(OCC)P(=O)(CC(C#N)Cc1ccccc1)OCC
ord_dataset-02ee2261663048188cf6d85d2cc96e3f
ord-37b50643042144889ddbf8ea19fd8458
CCOC(OCC)P(=O)(CC(C#N)Cc1ccccc1)OCC>>CCOC(OCC)P(=O)(CC(CN)Cc1ccccc1)OCC
[H][H].C(C1=CC=CC=C1)C(CP(OCC)(=O)C(OCC)OCC)C#N.N>>NCC(CP(OCC)(=O)C(OCC)OCC)CC1=CC=CC=C1
[CH3:1][CH2:2][O:3][CH:4]([O:5][CH2:6][CH3:7])[P:8](=[O:9])([CH2:10][CH:11]([C:12]#[N:13])[CH2:14][c:15]1[cH:16][cH:17][cH:18][cH:19][cH:20]1)[O:21][CH2:22][CH3:23]>>[CH3:1][CH2:2][O:3][CH:4]([O:5][CH2:6][CH3:7])[P:8](=[O:9])([CH2:10][CH:11]([CH2:12][NH2:13])[CH2:14][c:15]1[cH:16][cH:17][cH:18][cH:19][cH:20]1)[O:21][CH...
CCOC(OCC)P(=O)(CC(C#N)Cc1ccccc1)OCC
CCOC(OCC)P(=O)(CC(CN)Cc1ccccc1)OCC
null
[Ni]
C(C)O
Reduction
Reduction of nitrile to amine
65bec2d9f430701d30dc9fcbe1c5418f3dfa174d67be035c50edfc71895dc9c7
e8d1bc928b94bd4f5bf4b23363ce8f88b1ce7d146ba93829e7b8ad8dbe0007a7
c1ccccc1
[C:1]-[C:2](-[C:3])-[C;H0;D2;+0:4]#[N;H0;D1;+0:5]>>[C:1]-[C:2](-[C:3])-[CH2;D2;+0:4]-[NH2;D1;+0:5]
null
[]
null
null
null
null
A solution of 3.5 g of ethyl 2-benzyl-2-cyanoethyl(diethoxymethyl)phosphinate in 50 ml of ethanol is added to 25 g of an 8% solution of ammonia in ethanol. To this are added 2 ml of Raney Nickel and the resulting mixture is hydrogenated at 1 bar until the theoretical amount of hydrogen has been taken up. The mixture is...
10.6084/m9.figshare.5104873.v1
null
Nitrile
Primary amine
null
null
c1ccccc1
null
[Ni].C(C)O
null
null
CCOC(OCC)P(=O)(CC(C#N)Cc1ccccc1)OCC>[Ni].C(C)O>CCOC(OCC)P(=O)(CC(CN)Cc1ccccc1)OCC
ord_dataset-02ee2261663048188cf6d85d2cc96e3f
ord-19a9b1f0815341adbd64aa967ff7b15f
CCOC(OCC)P(=O)(CC(CN)c1ccc(Cl)cc1)OCC>>Cl.NCC(CP(O)O)c1ccc(Cl)cc1
NCC(CP(OCC)(=O)C(OCC)OCC)C1=CC=C(C=C1)Cl>>Cl.NCC(CP(O)O)C1=CC=C(C=C1)Cl
CCOC(OCC)[P:6]([CH2:5][CH:4]([CH2:3][NH2:2])[c:9]1[cH:10][cH:11][c:12]([Cl:1])[cH:14][cH:15]1)(=[O:7])[O:8]CC>>[ClH:1].[NH2:2][CH2:3][CH:4]([CH2:5][P:6]([OH:7])[OH:8])[c:9]1[cH:10][cH:11][c:12]([Cl:13])[cH:14][cH:15]1
CCOC(OCC)P(=O)(CC(CN)c1ccc(Cl)cc1)OCC
Cl.NCC(CP(O)O)c1ccc(Cl)cc1
null
null
Cl
Miscellaneous
OtherReaction
a1a8c8915d84e005416c9f23b64d1565b30cfa9a9f9a8c6c76d7f39da21921b3
1c6f68af3a00735409b48f113e6c8647fe15c8e43c4864833ee19c70c719047c
c1ccccc1
C-C-O-C(-O-C-C)-[P;H0;D4;+0:1](=[O;H0;D1;+0:2])(-[C:3]-[C:4])-[O;H0;D2;+0:5]-C-C.[Cl;H0;D1;+0:6]-[c;H0;D3;+0:7](:[c:8]:[c:9]):[c:10]:[c:11]>>[C:4]-[C:3]-[P;H0;D3;+0:1](-[OH;D1;+0:2])-[OH;D1;+0:5].[Cl;D1;H0:12]-[c;H0;D3;+0:7](:[c:8]:[c:9]):[c:10]:[c:11].[ClH;D0;+0:6]
null
[]
null
null
null
null
A solution of 5.0 g of ethyl 3-amino-2-(4-chlorophenyl)propyl(diethoxymethyl)phosphinate in 60 ml of 36% aqueous hydrochloric acid is heated to reflux for a period of 1 hour. The reaction mixture is then allowed to cool to room temperature, concentrated under reduced pressure, and co-evaporated three times with 20 ml o...
10.6084/m9.figshare.5104873.v1
null
Aromatic halide.Ether.Ether
Aromatic halide
c1ccccc1
c1ccccc1
c1ccccc1
HO-
Cl
null
null
CCOC(OCC)P(=O)(CC(CN)c1ccc(Cl)cc1)OCC>Cl>Cl.NCC(CP(O)O)c1ccc(Cl)cc1
ord_dataset-02ee2261663048188cf6d85d2cc96e3f
ord-a76616da146e429fbd1b8adac259000a
NCC(CP(O)O)c1ccc(Cl)cc1>>NCC(C[PH](=O)[O-])c1ccc(Cl)cc1
NCC(CP(O)O)C1=CC=C(C=C1)Cl.[OH-].[Na+]>>NCC(CP([O-])=O)C1=CC=C(C=C1)Cl.[Na+]
[NH2:1][CH2:2][CH:3]([CH2:4][P:5]([OH:6])[OH:7])[c:8]1[cH:9][cH:10][c:11]([Cl:12])[cH:13][cH:14]1>>[NH2:1][CH2:2][CH:3]([CH2:4][PH:5](=[O:6])[O-:7])[c:8]1[cH:9][cH:10][c:11]([Cl:12])[cH:13][cH:14]1
NCC(CP(O)O)c1ccc(Cl)cc1
NCC(C[PH](=O)[O-])c1ccc(Cl)cc1
null
null
null
Functional Group Interconversion
OtherReaction
42af6cdfb86a130c92365e01a31b50705eea7bdf12f67dc370bf24402f7ceedc
f1bbf9aa3c82f5e49be9f6d53533b6bb152f359232b6d32090c168949766aa71
c1ccccc1
[C:1]-[C:2]-[P;H0;D3;+0:3](-[OH;D1;+0:4])-[OH;D1;+0:5]>>[C:1]-[C:2]-[PH;D3;+0:3](-[O-;H0;D1:5])=[O;H0;D1;+0:4]
null
[]
null
null
null
null
A solution of 0.25 g of 3-amino-2-(4-chlorophenyl)propylphosphonous acid in 10 ml of 0.1M sodium hydroxide solution is stirred at room temperature for a period of 1 hour, and then concentrated under reduced pressure to give sodium 3-amino-2-(4-chlorophenyl)propylphosphinate as a hygroscopic solid, 31 p=+26.0 ppm (D2O)....
10.6084/m9.figshare.5104873.v1
null
null
null
null
null
c1ccccc1
null
null
null
null
NCC(CP(O)O)c1ccc(Cl)cc1>>NCC(C[PH](=O)[O-])c1ccc(Cl)cc1
ord_dataset-02ee2261663048188cf6d85d2cc96e3f
ord-2bbc92e2ff0d431487501fe1aa3d360f
CCOC(OCC)P(=O)(CC(CN)c1ccccc1)OCC>>NCC(CP(O)O)c1ccccc1
NCC(CP(OCC)(=O)C(OCC)OCC)C1=CC=CC=C1>>NCC(CP(O)O)C1=CC=CC=C1
CCOC(OCC)[P:5]([CH2:4][CH:3]([CH2:2][NH2:1])[c:8]1[cH:9][cH:10][cH:11][cH:12][cH:13]1)(=[O:6])[O:7]CC>>[NH2:1][CH2:2][CH:3]([CH2:4][P:5]([OH:6])[OH:7])[c:8]1[cH:9][cH:10][cH:11][cH:12][cH:13]1
CCOC(OCC)P(=O)(CC(CN)c1ccccc1)OCC
NCC(CP(O)O)c1ccccc1
null
null
Cl
Miscellaneous
OtherReaction
27a7ce5124ce9df58d78a5aef67d94157caa3dd464298a2201254c2545b8416a
79a17d37832f2717ceac93b17ac3ad97b0bc0d876910e15be3eeb8366cf301c1
c1ccccc1
C-C-O-C(-O-C-C)-[P;H0;D4;+0:1](=[O;H0;D1;+0:2])(-[C:3]-[C:4])-[O;H0;D2;+0:5]-C-C>>[C:4]-[C:3]-[P;H0;D3;+0:1](-[OH;D1;+0:2])-[OH;D1;+0:5]
null
[]
null
null
null
null
A solution of 4.0 g of ethyl 3-amino-2-phenylpropyl(diethoxymethyl)phosphinate in 40 ml of 36% aqueous hydrochloric acid is heated to reflux for a period of 2 h. The reaction mixture is then allowed to cool to room temperature, concentrated under reduced pressure and co-evaporated twice with 20 ml of water under reduce...
10.6084/m9.figshare.5104873.v1
null
Ether.Ether
null
null
null
c1ccccc1
HO-
Cl
null
null
CCOC(OCC)P(=O)(CC(CN)c1ccccc1)OCC>Cl>NCC(CP(O)O)c1ccccc1
ord_dataset-02ee2261663048188cf6d85d2cc96e3f
ord-5336d52842114646b59fecae49e4dd9d
CCOC(OCC)P(C)(=O)OCC.O=[N+]([O-])C=Cc1ccccc1>>CCOC(OCC)P(=O)(CC(C[N+](=O)[O-])c1ccccc1)OCC
[N+](=O)([O-])C=CC1=CC=CC=C1.C(C)OC(OCC)P(OCC)(=O)C.[Cl-].[NH4+].C(C)(C)NC(C)C.C(CCC)[Li]>>[N+](=O)([O-])CC(CP(OCC)(=O)C(OCC)OCC)C1=CC=CC=C1
[CH3:1][CH2:2][O:3][CH:4]([O:5][CH2:6][CH3:7])[P:8](=[O:9])([CH3:10])[O:22][CH2:23][CH3:24].[CH:11](=[CH:12][N+:13](=[O:14])[O-:15])[c:16]1[cH:17][cH:18][cH:19][cH:20][cH:21]1>>[CH3:1][CH2:2][O:3][CH:4]([O:5][CH2:6][CH3:7])[P:8](=[O:9])([CH2:10][CH:11]([CH2:12][N+:13](=[O:14])[O-:15])[c:16]1[cH:17][cH:18][cH:19][cH:20]...
CCOC(OCC)P(C)(=O)OCC.O=[N+]([O-])C=Cc1ccccc1
CCOC(OCC)P(=O)(CC(C[N+](=O)[O-])c1ccccc1)OCC
null
null
CCCCCC.O1CCCC1
C-C Coupling
Michael addition methyl
4792ab23977aa8f2d8848039e3cf8e0149eb8bcd2b5b236e5f3910f20c70f1a9
62f7b8b1b06d8abe0a7458fcdb08bc1ff61c22493460bb08abd465e204dda1f5
c1ccccc1
[#8:1]-[#15:2](-[C:3])(-[CH3;D1;+0:4])=[O;D1;H0:5].[O;-;D1;H0:6]-[#7;+:7](=[O;D1;H0:8])-[CH;D2;+0:9]=[CH;D2;+0:10]-[c:11](:[c:12]):[c:13]>>[#8:1]-[#15:2](-[C:3])(=[O;D1;H0:5])-[CH2;D2;+0:4]-[CH;D3;+0:10](-[CH2;D2;+0:9]-[#7;+:7](-[O;-;D1;H0:6])=[O;D1;H0:8])-[c:11](:[c:12]):[c:13]
null
[]
null
null
10
MINUTE
To a solution of 5.8 g of diisopropylamine in 40 ml of tetrahydrofuran at -78° C. under an atmosphere of nitrogen are added 35.7 ml of a 1.6M solution of n-butyllithium in hexane. This solution is then stirred for a period of 10 minutes at this temperature, after which time a solution of 10.0 g of ethyl (diethoxymethyl...
10.6084/m9.figshare.5104873.v1
null
Enamine
Nitro group
null
null
c1ccccc1
null
CCCCCC.O1CCCC1
null
0.166667
CCOC(OCC)P(C)(=O)OCC.O=[N+]([O-])C=Cc1ccccc1>CCCCCC.O1CCCC1>CCOC(OCC)P(=O)(CC(C[N+](=O)[O-])c1ccccc1)OCC
ord_dataset-02ee2261663048188cf6d85d2cc96e3f
ord-7dc71600b17042d78234f99e2162c0fb
CCOC(OCC)P(=O)(CC(C[N+](=O)[O-])c1ccccc1)OCC>>CCOC(OCC)P(=O)(CC(CN)c1ccccc1)OCC
[H][H].[N+](=O)([O-])CC(CP(OCC)(=O)C(OCC)OCC)C1=CC=CC=C1.N>>NCC(CP(OCC)(=O)C(OCC)OCC)C1=CC=CC=C1
O=[N+:13]([O-])[CH2:12][CH:11]([CH2:10][P:8]([CH:4]([O:3][CH2:2][CH3:1])[O:5][CH2:6][CH3:7])(=[O:9])[O:20][CH2:21][CH3:22])[c:14]1[cH:15][cH:16][cH:17][cH:18][cH:19]1>>[CH3:1][CH2:2][O:3][CH:4]([O:5][CH2:6][CH3:7])[P:8](=[O:9])([CH2:10][CH:11]([CH2:12][NH2:13])[c:14]1[cH:15][cH:16][cH:17][cH:18][cH:19]1)[O:20][CH2:21][...
CCOC(OCC)P(=O)(CC(C[N+](=O)[O-])c1ccccc1)OCC
CCOC(OCC)P(=O)(CC(CN)c1ccccc1)OCC
null
[Ni]
C(C)O
Reduction
Reduction of nitro groups to amines
bbc242b150a51e69d3ad1caaa391f4422710431b398dcb880555f476706790be
7b0317532ea57a4fcedc1efc3e3c22eb5238d1c8330da53d4f9801fc2391f567
c1ccccc1
O=[N+;H0;D3:1](-[O-])-[C:2]-[C:3]>>[C:3]-[C:2]-[NH2;D1;+0:1]
null
[]
null
null
null
null
A solution of 5.7 g of ethyl 3-nitro-2-phenylpropyl(diethoxymethyl)phosphinate in 60 ml of ethanol is added to 50 g of an 8% solution of ammonia in ethanol. To this are added 9 ml of Raney Nickel and the resulting mixture is hydrogenated at 1 bar until the theoretical amount of hydrogen has been taken up. The mixture i...
10.6084/m9.figshare.5104873.v1
null
Nitro group
Primary amine
null
null
c1ccccc1
Other
[Ni].C(C)O
null
null
CCOC(OCC)P(=O)(CC(C[N+](=O)[O-])c1ccccc1)OCC>[Ni].C(C)O>CCOC(OCC)P(=O)(CC(CN)c1ccccc1)OCC
ord_dataset-02ee2261663048188cf6d85d2cc96e3f
ord-a1d96c615d30475b87d289bd7824e029
CCOC(OCC)P(=O)(CC(CN)c1ccc(F)cc1)OCC>>NCC(CP(O)O)c1ccc(F)cc1
NCC(CP(OCC)(=O)C(OCC)OCC)C1=CC=C(C=C1)F>>NCC(CP(O)O)C1=CC=C(C=C1)F
CCOC(OCC)[P:5]([CH2:4][CH:3]([CH2:2][NH2:1])[c:8]1[cH:9][cH:10][c:11]([F:12])[cH:13][cH:14]1)([O:6]CC)=[O:7]>>[NH2:1][CH2:2][CH:3]([CH2:4][P:5]([OH:6])[OH:7])[c:8]1[cH:9][cH:10][c:11]([F:12])[cH:13][cH:14]1
CCOC(OCC)P(=O)(CC(CN)c1ccc(F)cc1)OCC
NCC(CP(O)O)c1ccc(F)cc1
null
null
Cl
Miscellaneous
OtherReaction
27a7ce5124ce9df58d78a5aef67d94157caa3dd464298a2201254c2545b8416a
79a17d37832f2717ceac93b17ac3ad97b0bc0d876910e15be3eeb8366cf301c1
c1ccccc1
C-C-O-C(-O-C-C)-[P;H0;D4;+0:1](=[O;H0;D1;+0:2])(-[C:3]-[C:4])-[O;H0;D2;+0:5]-C-C>>[C:4]-[C:3]-[P;H0;D3;+0:1](-[OH;D1;+0:5])-[OH;D1;+0:2]
null
[]
null
null
null
null
A solution of 4.4 g of ethyl 3-amino-2-(4-fluorophenyl)propyl(diethoxymethyl)phosphinate in 40 ml of 36% aqueous hydrochloric acid is heated to reflux for a period of 2 h. The reaction mixture is then allowed to cool to room temperature, concentrated under reduced pressure and co-evaporated twice with 20 ml of water un...
10.6084/m9.figshare.5104873.v1
null
Ether.Ether
null
null
null
c1ccccc1
HO-
Cl
null
null
CCOC(OCC)P(=O)(CC(CN)c1ccc(F)cc1)OCC>Cl>NCC(CP(O)O)c1ccc(F)cc1
ord_dataset-02ee2261663048188cf6d85d2cc96e3f
ord-ccb81927c486466b913958dd34a1a9b4
CCOC(OCC)P(C)(=O)OCC.O=[N+]([O-])C=Cc1ccc(F)cc1>>CCOC(OCC)P(=O)(CC(C[N+](=O)[O-])c1ccc(F)cc1)OCC
FC1=CC=C(C=C[N+](=O)[O-])C=C1.C(C)OP(=O)(C)C(OCC)OCC.[Cl-].[NH4+].C(C)(C)NC(C)C.C(CCC)[Li]>>FC1=CC=C(C=C1)C(CP(OCC)(=O)C(OCC)OCC)C[N+](=O)[O-]
[CH3:1][CH2:2][O:3][CH:4]([O:5][CH2:6][CH3:7])[P:8](=[O:9])([CH3:10])[O:23][CH2:24][CH3:25].[CH:11](=[CH:12][N+:13](=[O:14])[O-:15])[c:16]1[cH:17][cH:18][c:19]([F:20])[cH:21][cH:22]1>>[CH3:1][CH2:2][O:3][CH:4]([O:5][CH2:6][CH3:7])[P:8](=[O:9])([CH2:10][CH:11]([CH2:12][N+:13](=[O:14])[O-:15])[c:16]1[cH:17][cH:18][c:19](...
CCOC(OCC)P(C)(=O)OCC.O=[N+]([O-])C=Cc1ccc(F)cc1
CCOC(OCC)P(=O)(CC(C[N+](=O)[O-])c1ccc(F)cc1)OCC
null
null
CCCCCC.O1CCCC1
C-C Coupling
Michael addition methyl
4792ab23977aa8f2d8848039e3cf8e0149eb8bcd2b5b236e5f3910f20c70f1a9
62f7b8b1b06d8abe0a7458fcdb08bc1ff61c22493460bb08abd465e204dda1f5
c1ccccc1
[#8:1]-[#15:2](-[C:3])(-[CH3;D1;+0:4])=[O;D1;H0:5].[O;-;D1;H0:6]-[#7;+:7](=[O;D1;H0:8])-[CH;D2;+0:9]=[CH;D2;+0:10]-[c:11](:[c:12]):[c:13]>>[#8:1]-[#15:2](-[C:3])(=[O;D1;H0:5])-[CH2;D2;+0:4]-[CH;D3;+0:10](-[CH2;D2;+0:9]-[#7;+:7](-[O;-;D1;H0:6])=[O;D1;H0:8])-[c:11](:[c:12]):[c:13]
null
[]
null
null
10
MINUTE
To a solution of 5.8 g of diisopropylamine in 40 ml of tetrahydrofuran at -78° C. under an atmosphere of nitrogen are added 35.7 ml of a 1.6M solution of n-butyllithium in hexane. This solution is then stirred for a period of 10 minutes at this temperature, after which time a solution of 10.0 g of ethyl(diethoxymethyl)...
10.6084/m9.figshare.5104873.v1
null
Enamine
Nitro group
null
null
c1ccccc1
null
CCCCCC.O1CCCC1
null
0.166667
CCOC(OCC)P(C)(=O)OCC.O=[N+]([O-])C=Cc1ccc(F)cc1>CCCCCC.O1CCCC1>CCOC(OCC)P(=O)(CC(C[N+](=O)[O-])c1ccc(F)cc1)OCC
ord_dataset-02ee2261663048188cf6d85d2cc96e3f
ord-6ea9919d85d9467ea82fcb08f059f9d8
CCOC(OCC)P(=O)(CC(C[N+](=O)[O-])c1ccc(F)cc1)OCC>>CCOC(OCC)P(=O)(CC(CN)c1ccc(F)cc1)OCC
[H][H].FC1=CC=C(C=C1)C(CP(OCC)(=O)C(OCC)OCC)C[N+](=O)[O-].N>>NCC(CP(OCC)(=O)C(OCC)OCC)C1=CC=C(C=C1)F
O=[N+:13]([O-])[CH2:12][CH:11]([CH2:10][P:8]([CH:4]([O:3][CH2:2][CH3:1])[O:5][CH2:6][CH3:7])(=[O:9])[O:21][CH2:22][CH3:23])[c:14]1[cH:15][cH:16][c:17]([F:18])[cH:19][cH:20]1>>[CH3:1][CH2:2][O:3][CH:4]([O:5][CH2:6][CH3:7])[P:8](=[O:9])([CH2:10][CH:11]([CH2:12][NH2:13])[c:14]1[cH:15][cH:16][c:17]([F:18])[cH:19][cH:20]1)[...
CCOC(OCC)P(=O)(CC(C[N+](=O)[O-])c1ccc(F)cc1)OCC
CCOC(OCC)P(=O)(CC(CN)c1ccc(F)cc1)OCC
null
[Ni]
C(C)O
Reduction
Reduction of nitro groups to amines
bbc242b150a51e69d3ad1caaa391f4422710431b398dcb880555f476706790be
7b0317532ea57a4fcedc1efc3e3c22eb5238d1c8330da53d4f9801fc2391f567
c1ccccc1
O=[N+;H0;D3:1](-[O-])-[C:2]-[C:3]>>[C:3]-[C:2]-[NH2;D1;+0:1]
null
[]
null
null
null
null
A solution of 5.0 g of ethyl 2-(4-fluorophenyl)-3-nitropropyl(diethoxymethyl)phosphinate in 50 ml of ethanol is added to 40 g of an 8% solution of ammonia in ethanol. To this are added 7 ml of Raney Nickel and the resulting mixture is hydrogenated at 1 bar until the theoretical amount of hydrogen has been taken up. The...
10.6084/m9.figshare.5104873.v1
null
Nitro group
Primary amine
null
null
c1ccccc1
Other
[Ni].C(C)O
null
null
CCOC(OCC)P(=O)(CC(C[N+](=O)[O-])c1ccc(F)cc1)OCC>[Ni].C(C)O>CCOC(OCC)P(=O)(CC(CN)c1ccc(F)cc1)OCC
ord_dataset-02ee2261663048188cf6d85d2cc96e3f
ord-2727d84160a24d0ca7d4fd9ff1eb90d8
CCOC(OCC)P(=O)(CC(CN)c1ccc(C)cc1)OCC>>Cc1ccc(C(CN)CP(O)O)cc1
NCC(CP(OCC)(=O)C(OCC)OCC)C1=CC=C(C=C1)C>>NCC(CP(O)O)C1=CC=C(C=C1)C
CCOC(OCC)[P:10]([CH2:9][CH:6]([c:5]1[cH:4][cH:3][c:2]([CH3:1])[cH:14][cH:13]1)[CH2:7][NH2:8])(=[O:11])[O:12]CC>>[CH3:1][c:2]1[cH:3][cH:4][c:5]([CH:6]([CH2:7][NH2:8])[CH2:9][P:10]([OH:11])[OH:12])[cH:13][cH:14]1
CCOC(OCC)P(=O)(CC(CN)c1ccc(C)cc1)OCC
Cc1ccc(C(CN)CP(O)O)cc1
null
null
Cl
Miscellaneous
OtherReaction
27a7ce5124ce9df58d78a5aef67d94157caa3dd464298a2201254c2545b8416a
79a17d37832f2717ceac93b17ac3ad97b0bc0d876910e15be3eeb8366cf301c1
c1ccccc1
C-C-O-C(-O-C-C)-[P;H0;D4;+0:1](=[O;H0;D1;+0:2])(-[C:3]-[C:4])-[O;H0;D2;+0:5]-C-C>>[C:4]-[C:3]-[P;H0;D3;+0:1](-[OH;D1;+0:2])-[OH;D1;+0:5]
null
[]
null
null
null
null
A solution of 3.7 g of ethyl 3-amino-2-(4-methylphenyl)propyl(diethoxymethyl)phosphinate in 40 ml of 36% aqueous hydrochloric acid is heated to reflux for a period of 1 h. The reaction mixture is then allowed to cool to room temperature, concentrated under reduced pressure and co-evaporated twice with 20 ml of water un...
10.6084/m9.figshare.5104873.v1
null
Ether.Ether
null
null
null
c1ccccc1
HO-
Cl
null
null
CCOC(OCC)P(=O)(CC(CN)c1ccc(C)cc1)OCC>Cl>Cc1ccc(C(CN)CP(O)O)cc1
ord_dataset-02ee2261663048188cf6d85d2cc96e3f
ord-789e38ffe1424cb886e603ae877f3048
CCOC(OCC)P(C)(=O)OCC.Cc1ccc(C=C[N+](=O)[O-])cc1>>CCOC(OCC)P(=O)(CC(C[N+](=O)[O-])c1ccc(C)cc1)OCC
CC1=CC=C(C=C[N+](=O)[O-])C=C1.C(C)OP(=O)(C)C(OCC)OCC.[Cl-].[NH4+].C(C)(C)NC(C)C.C(CCC)[Li]>>CC1=CC=C(C=C1)C(CP(OCC)(=O)C(OCC)OCC)C[N+](=O)[O-]
[CH3:1][CH2:2][O:3][CH:4]([O:5][CH2:6][CH3:7])[P:8](=[O:9])([CH3:10])[O:23][CH2:24][CH3:25].[CH:11](=[CH:12][N+:13](=[O:14])[O-:15])[c:16]1[cH:17][cH:18][c:19]([CH3:20])[cH:21][cH:22]1>>[CH3:1][CH2:2][O:3][CH:4]([O:5][CH2:6][CH3:7])[P:8](=[O:9])([CH2:10][CH:11]([CH2:12][N+:13](=[O:14])[O-:15])[c:16]1[cH:17][cH:18][c:19...
CCOC(OCC)P(C)(=O)OCC.Cc1ccc(C=C[N+](=O)[O-])cc1
CCOC(OCC)P(=O)(CC(C[N+](=O)[O-])c1ccc(C)cc1)OCC
null
null
CCCCCC.O1CCCC1
C-C Coupling
Michael addition methyl
4792ab23977aa8f2d8848039e3cf8e0149eb8bcd2b5b236e5f3910f20c70f1a9
62f7b8b1b06d8abe0a7458fcdb08bc1ff61c22493460bb08abd465e204dda1f5
c1ccccc1
[#8:1]-[#15:2](-[C:3])(-[CH3;D1;+0:4])=[O;D1;H0:5].[O;-;D1;H0:6]-[#7;+:7](=[O;D1;H0:8])-[CH;D2;+0:9]=[CH;D2;+0:10]-[c:11](:[c:12]):[c:13]>>[#8:1]-[#15:2](-[C:3])(=[O;D1;H0:5])-[CH2;D2;+0:4]-[CH;D3;+0:10](-[CH2;D2;+0:9]-[#7;+:7](-[O;-;D1;H0:6])=[O;D1;H0:8])-[c:11](:[c:12]):[c:13]
null
[]
null
null
10
MINUTE
To a solution of 8.7 g of diisopropylamine in 40 ml of tetrahydrofuran at -78° C. under an atmosphere of nitrogen are added 53.6 ml of a 1.6M solution of n-butyllithium in hexane. This solution is then stirred for a period of 10 minutes at this temperature, after which time a solution of 15.0 g of ethyl(diethoxymethyl)...
10.6084/m9.figshare.5104873.v1
null
Enamine
Nitro group
null
null
c1ccccc1
null
CCCCCC.O1CCCC1
null
0.166667
CCOC(OCC)P(C)(=O)OCC.Cc1ccc(C=C[N+](=O)[O-])cc1>CCCCCC.O1CCCC1>CCOC(OCC)P(=O)(CC(C[N+](=O)[O-])c1ccc(C)cc1)OCC
ord_dataset-02ee2261663048188cf6d85d2cc96e3f
ord-7b87461ecdde45988aceaf88c872f80d
CCOC(OCC)P(=O)(CC(C[N+](=O)[O-])c1ccc(C)cc1)OCC>>CCOC(OCC)P(=O)(CC(CN)c1ccc(C)cc1)OCC
[H][H].CC1=CC=C(C=C1)C(CP(OCC)(=O)C(OCC)OCC)C[N+](=O)[O-].N>>NCC(CP(OCC)(=O)C(OCC)OCC)C1=CC=C(C=C1)C
O=[N+:13]([O-])[CH2:12][CH:11]([CH2:10][P:8]([CH:4]([O:3][CH2:2][CH3:1])[O:5][CH2:6][CH3:7])(=[O:9])[O:21][CH2:22][CH3:23])[c:14]1[cH:15][cH:16][c:17]([CH3:18])[cH:19][cH:20]1>>[CH3:1][CH2:2][O:3][CH:4]([O:5][CH2:6][CH3:7])[P:8](=[O:9])([CH2:10][CH:11]([CH2:12][NH2:13])[c:14]1[cH:15][cH:16][c:17]([CH3:18])[cH:19][cH:20...
CCOC(OCC)P(=O)(CC(C[N+](=O)[O-])c1ccc(C)cc1)OCC
CCOC(OCC)P(=O)(CC(CN)c1ccc(C)cc1)OCC
null
[Ni]
C(C)O
Reduction
Reduction of nitro groups to amines
bbc242b150a51e69d3ad1caaa391f4422710431b398dcb880555f476706790be
7b0317532ea57a4fcedc1efc3e3c22eb5238d1c8330da53d4f9801fc2391f567
c1ccccc1
O=[N+;H0;D3:1](-[O-])-[C:2]-[C:3]>>[C:3]-[C:2]-[NH2;D1;+0:1]
null
[]
null
null
null
null
A solution of 6.5 g of ethyl 2-(4-methylphenyl)-3-nitropropyl(diethoxymethyl)phosphinate in 60 ml of ethanol is added to 52 g of an 8% solution of ammonia in ethanol. To this are added 8 ml of Raney Nickel and the resulting mixture is hydrogenated at 1 bar until the theoretical amount of hydrogen has been taken up. The...
10.6084/m9.figshare.5104873.v1
null
Nitro group
Primary amine
null
null
c1ccccc1
Other
[Ni].C(C)O
null
null
CCOC(OCC)P(=O)(CC(C[N+](=O)[O-])c1ccc(C)cc1)OCC>[Ni].C(C)O>CCOC(OCC)P(=O)(CC(CN)c1ccc(C)cc1)OCC
ord_dataset-02ee2261663048188cf6d85d2cc96e3f
ord-3dbe2fa47a034bca8062cd9450dbb32c
CCOC(OCC)P(=O)(CC(CN)c1ccc(OC)cc1)OCC>>COc1ccc(C(CN)CP(O)O)cc1
NCC(CP(OCC)(=O)C(OCC)OCC)C1=CC=C(C=C1)OC>>NCC(CP(O)O)C1=CC=C(C=C1)OC
CCOC(OCC)[P:11]([CH2:10][CH:7]([c:6]1[cH:5][cH:4][c:3]([O:2][CH3:1])[cH:15][cH:14]1)[CH2:8][NH2:9])([O:12]CC)=[O:13]>>[CH3:1][O:2][c:3]1[cH:4][cH:5][c:6]([CH:7]([CH2:8][NH2:9])[CH2:10][P:11]([OH:12])[OH:13])[cH:14][cH:15]1
CCOC(OCC)P(=O)(CC(CN)c1ccc(OC)cc1)OCC
COc1ccc(C(CN)CP(O)O)cc1
null
null
Cl
Miscellaneous
OtherReaction
27a7ce5124ce9df58d78a5aef67d94157caa3dd464298a2201254c2545b8416a
79a17d37832f2717ceac93b17ac3ad97b0bc0d876910e15be3eeb8366cf301c1
c1ccccc1
C-C-O-C(-O-C-C)-[P;H0;D4;+0:1](=[O;H0;D1;+0:2])(-[C:3]-[C:4])-[O;H0;D2;+0:5]-C-C>>[C:4]-[C:3]-[P;H0;D3;+0:1](-[OH;D1;+0:5])-[OH;D1;+0:2]
null
[]
null
null
null
null
A solution of 4.6 g of ethyl 3-amino-2-(4-methoxyphenyl)propyl(diethoxymethyl)phosphinate in 30 ml of 36% aqueous hydrochloric acid is heated to reflux for a period of 1 hour. The reaction mixture is then allowed to cool to room temperature, concentrated under reduced pressure and co-evaporated twice with 20 ml of wate...
10.6084/m9.figshare.5104873.v1
null
Ether.Ether
null
null
null
c1ccccc1
HO-
Cl
null
null
CCOC(OCC)P(=O)(CC(CN)c1ccc(OC)cc1)OCC>Cl>COc1ccc(C(CN)CP(O)O)cc1
ord_dataset-02ee2261663048188cf6d85d2cc96e3f
ord-052fc1659f244dcba4296a66d0377419
CCOC(OCC)P(C)(=O)OCC.COc1ccc(C=C[N+](=O)[O-])cc1>>CCOC(OCC)P(=O)(CC(C[N+](=O)[O-])c1ccc(OC)cc1)OCC
COC1=CC=C(C=C[N+](=O)[O-])C=C1.C(C)OC(OCC)P(OCC)(=O)C.[Cl-].[NH4+].C(C)(C)NC(C)C.C(CCC)[Li]>>COC1=CC=C(C=C1)C(CP(OCC)(=O)C(OCC)OCC)C[N+](=O)[O-]
[CH3:1][CH2:2][O:3][CH:4]([O:5][CH2:6][CH3:7])[P:8](=[O:9])([CH3:10])[O:24][CH2:25][CH3:26].[CH:11](=[CH:12][N+:13](=[O:14])[O-:15])[c:16]1[cH:17][cH:18][c:19]([O:20][CH3:21])[cH:22][cH:23]1>>[CH3:1][CH2:2][O:3][CH:4]([O:5][CH2:6][CH3:7])[P:8](=[O:9])([CH2:10][CH:11]([CH2:12][N+:13](=[O:14])[O-:15])[c:16]1[cH:17][cH:18...
CCOC(OCC)P(C)(=O)OCC.COc1ccc(C=C[N+](=O)[O-])cc1
CCOC(OCC)P(=O)(CC(C[N+](=O)[O-])c1ccc(OC)cc1)OCC
null
null
CCCCCC.O1CCCC1
C-C Coupling
Michael addition methyl
4792ab23977aa8f2d8848039e3cf8e0149eb8bcd2b5b236e5f3910f20c70f1a9
62f7b8b1b06d8abe0a7458fcdb08bc1ff61c22493460bb08abd465e204dda1f5
c1ccccc1
[#8:1]-[#15:2](-[C:3])(-[CH3;D1;+0:4])=[O;D1;H0:5].[O;-;D1;H0:6]-[#7;+:7](=[O;D1;H0:8])-[CH;D2;+0:9]=[CH;D2;+0:10]-[c:11](:[c:12]):[c:13]>>[#8:1]-[#15:2](-[C:3])(=[O;D1;H0:5])-[CH2;D2;+0:4]-[CH;D3;+0:10](-[CH2;D2;+0:9]-[#7;+:7](-[O;-;D1;H0:6])=[O;D1;H0:8])-[c:11](:[c:12]):[c:13]
null
[]
null
null
10
MINUTE
To a solution of 8.7 g of diisopropylamine in 40 ml of tetrahydrofuran at -78° C. under an atmosphere of nitrogen are added 53.6 ml of a 1.6M solution of n-butyllithium in hexane. This solution is then stirred for a period of 10 minutes at this temperature, after which time a solution of 15.0 g of ethyl (diethoxymethyl...
10.6084/m9.figshare.5104873.v1
null
Enamine
Nitro group
null
null
c1ccccc1
null
CCCCCC.O1CCCC1
null
0.166667
CCOC(OCC)P(C)(=O)OCC.COc1ccc(C=C[N+](=O)[O-])cc1>CCCCCC.O1CCCC1>CCOC(OCC)P(=O)(CC(C[N+](=O)[O-])c1ccc(OC)cc1)OCC
ord_dataset-02ee2261663048188cf6d85d2cc96e3f
ord-c7d3f848b65b4035934634d4b5b9371c
CCOC(OCC)P(=O)(CC(C[N+](=O)[O-])c1ccc(OC)cc1)OCC>>CCOC(OCC)P(=O)(CC(CN)c1ccc(OC)cc1)OCC
[H][H].COC1=CC=C(C=C1)C(CP(OCC)(=O)C(OCC)OCC)C[N+](=O)[O-].N>>NCC(CP(OCC)(=O)C(OCC)OCC)C1=CC=C(C=C1)OC
O=[N+:13]([O-])[CH2:12][CH:11]([CH2:10][P:8]([CH:4]([O:3][CH2:2][CH3:1])[O:5][CH2:6][CH3:7])(=[O:9])[O:22][CH2:23][CH3:24])[c:14]1[cH:15][cH:16][c:17]([O:18][CH3:19])[cH:20][cH:21]1>>[CH3:1][CH2:2][O:3][CH:4]([O:5][CH2:6][CH3:7])[P:8](=[O:9])([CH2:10][CH:11]([CH2:12][NH2:13])[c:14]1[cH:15][cH:16][c:17]([O:18][CH3:19])[...
CCOC(OCC)P(=O)(CC(C[N+](=O)[O-])c1ccc(OC)cc1)OCC
CCOC(OCC)P(=O)(CC(CN)c1ccc(OC)cc1)OCC
null
[Ni]
C(C)O
Reduction
Reduction of nitro groups to amines
bbc242b150a51e69d3ad1caaa391f4422710431b398dcb880555f476706790be
7b0317532ea57a4fcedc1efc3e3c22eb5238d1c8330da53d4f9801fc2391f567
c1ccccc1
O=[N+;H0;D3:1](-[O-])-[C:2]-[C:3]>>[C:3]-[C:2]-[NH2;D1;+0:1]
null
[]
null
null
null
null
A solution of 6.6 g of ethyl 2-(4-methoxyphenyl)-3-nitropropyl(diethoxymethyl)phosphinate in 50 ml of ethanol is added to 52 g of an 8% solution of ammonia in ethanol. To this are added 8 ml of Raney Nickel and the resulting mixture is hydrogenated at 1 bar until the theoretical amount of hydrogen has been taken up. Th...
10.6084/m9.figshare.5104873.v1
null
Nitro group
Primary amine
null
null
c1ccccc1
Other
[Ni].C(C)O
null
null
CCOC(OCC)P(=O)(CC(C[N+](=O)[O-])c1ccc(OC)cc1)OCC>[Ni].C(C)O>CCOC(OCC)P(=O)(CC(CN)c1ccc(OC)cc1)OCC
ord_dataset-02ee2261663048188cf6d85d2cc96e3f
ord-765eee938f5f4e1793095537f302f9ea
CC(=O)CC(=O)[O-].N=C(N)NN>>CC(CC(=O)O)=NNC(=N)N
C(CC(=O)C)(=O)[O-].[Li+].C(=N)(N)NN.Cl.C(C)O>>C(N)(=N)NN=C(CC(=O)O)C
O=[C:2]([CH3:1])[CH2:3][C:4](=[O:5])[O-:6].[NH2:7][NH:8][C:9](=[NH:10])[NH2:11]>>[CH3:1][C:2]([CH2:3][C:4](=[O:5])[OH:6])=[N:7][NH:8][C:9](=[NH:10])[NH2:11]
CC(=O)CC(=O)[O-].N=C(N)NN
CC(CC(=O)O)=NNC(=N)N
null
null
O
Heteroatom Alkylation and Arylation
OtherReaction
88005d6d8085d6ee296ad8005c0568792897129ef26cedaae52e63e5012734c7
348380d82fd877efc76db31f1a616d192c30557986be45e68c3952f08c73a05b
null
O=[C;H0;D3;+0:1](-[C;D1;H3:2])-[C:3]-[C:4](-[O-;H0;D1:5])=[O;D1;H0:6].[N;D1;H1:7]=[C:8]-[#7:9]-[NH2;D1;+0:10]>>[C;D1;H3:2]-[C;H0;D3;+0:1](-[C:3]-[C:4](=[O;D1;H0:6])-[OH;D1;+0:5])=[N;H0;D2;+0:10]-[#7:9]-[C:8]=[N;D1;H1:7]
54.9
[{"value": 54.9, "product": "C(N)(=N)NN=C(CC(=O)O)C", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
24
HOUR
Lithium acetoacetate (0.655 g) in 2 ml water treated with 0.665 g aminoguanidine HCl in 1.33 ml water. The solution was heated to reflux over 30 minutes and then allowed to cool. Ethanol (10 ml) was added and the mixture was stored at -20° C. for 24 hrs., then at 4° C. for 24 hrs. The mixture was allowed to reach room ...
10.6084/m9.figshare.5104873.v1
null
Hydrazine.Ketone
Hydrazone.Carboxylic acid
null
null
null
HO-
O
null
24
CC(=O)CC(=O)[O-].N=C(N)NN>O>CC(CC(=O)O)=NNC(=N)N
ord_dataset-02ee2261663048188cf6d85d2cc96e3f
ord-a9a5f08948ef490a8633b44f5ca2f366
C=CC(=O)O.COCCCCCCO>>C=CC(=O)OCCCCCCOC
C1(=CC=C(C=C1)S(=O)(=O)O)C.COC.COCCCCCCO.C(C=C)(=O)O>>C(C=C)(=O)OCCCCCCOC
O[C:3]([CH:2]=[CH2:1])=[O:4].[OH:5][CH2:6][CH2:7][CH2:8][CH2:9][CH2:10][CH2:11][O:12][CH3:13]>>[CH2:1]=[CH:2][C:3](=[O:4])[O:5][CH2:6][CH2:7][CH2:8][CH2:9][CH2:10][CH2:11][O:12][CH3:13]
C=CC(=O)O.COCCCCCCO
C=CC(=O)OCCCCCCOC
null
null
C1(=CC=CC=C1)C.O
Protection
Esterification of Carboxylic Acids
070670f68a20c1021da94fabee54def4688122fb721af5f52cd5a03630845d0e
0d8a72b7375d91aa7263e766e03a3cb7c4fa91e27abcd590409ff03b98eed690
null
O-[C;H0;D3;+0:1](=[O;D1;H0:2])-[C:3]=[C;D1;H2:4].[C:5]-[C:6]-[OH;D1;+0:7]>>[C:5]-[C:6]-[O;H0;D2;+0:7]-[C;H0;D3;+0:1](=[O;D1;H0:2])-[C:3]=[C;D1;H2:4]
null
[]
null
null
null
null
803.6 grams of the monomethyl ether described in Part (A) above were azeotropically esterified with 629.8 grams acrylic acid in 254.6 grams toluene in the presence of 24 grams p-toluenesulfonic acid and inhibitors until no more water was collected. Conditions were 95°-98° C., nitrogen sparge in vacuo. On completion, th...
10.6084/m9.figshare.5104873.v1
null
Carboxylic acid.Primary alcohol
Ester
null
null
null
HO-
C1(=CC=CC=C1)C.O
null
null
C=CC(=O)O.COCCCCCCO>C1(=CC=CC=C1)C.O>C=CC(=O)OCCCCCCOC
ord_dataset-02ee2261663048188cf6d85d2cc96e3f
ord-0490a3c74fb84af38fee37a9f0e79743
COCCOCCO.O>>COC(O)COCCO
O.COCCOCCO.C(C=C)(=O)O.C1(=CC=C(C=C1)S(=O)(=O)O)C>>C(C=C)(=O)O.COC(COCCO)O
[CH3:6][O:7][CH2:8][CH2:10][O:11][CH2:12][CH2:13][OH:14].[OH2:9]>>[CH3:6][O:7][CH:8]([OH:9])[CH2:10][O:11][CH2:12][CH2:13][OH:14]
COCCOCCO.O
COC(O)COCCO
null
null
C1(=CC=CC=C1)C
Heteroatom Alkylation and Arylation
OtherReaction
e436aa388eea9f8fec2004301a7209b67f19650883978f247ad90d876368643d
c5b0d75b63e227d521baa73581cf28339228a50fdabb8eebf3697b67f34937a0
null
[#8:1]-[C:2]-[CH2;D2;+0:3]-[#8:4]-[C;D1;H3:5].[OH2;D0;+0:6]>>[#8:1]-[C:2]-[CH;D3;+0:3](-[OH;D1;+0:6])-[#8:4]-[C;D1;H3:5]
null
[]
null
null
null
null
682 grams Methyl Carbitol (diethylene glycol monomethyl ether, Union Carbide) were azeotropically esterified with 598.9 grams acrylic acid in 272 grams toluene in the presence of 22.8 grams p-toluenesulfonic acid and inhibitors until no more water was collected. Conditions were 95°-98° C., nitrogen sparge in vacuo. On ...
10.6084/m9.figshare.5104873.v1
null
Ether
Ether.Secondary alcohol
null
null
null
null
C1(=CC=CC=C1)C
null
null
COCCOCCO.O>C1(=CC=CC=C1)C>COC(O)COCCO
ord_dataset-02ee2261663048188cf6d85d2cc96e3f
ord-da7e98e9ee854ef08afec3f05f935e77
ClCc1ccc(Cl)nc1.Oc1ccc(Oc2ccccc2)cc1Cl>>Clc1ccc(COc2ccc(Oc3ccccc3)cc2Cl)cn1
[H-].[Na+].ClC1=C(C=CC(=C1)OC1=CC=CC=C1)O.ClC1=NC=C(C=C1)CCl>>ClC1=NC=C(C=C1)COC1=C(C=C(C=C1)OC1=CC=CC=C1)Cl
Cl[CH2:6][c:5]1[cH:4][cH:3][c:2]([Cl:1])[n:23][cH:22]1.[OH:7][c:8]1[cH:9][cH:10][c:11]([O:12][c:13]2[cH:14][cH:15][cH:16][cH:17][cH:18]2)[cH:19][c:20]1[Cl:21]>>[Cl:1][c:2]1[cH:3][cH:4][c:5]([CH2:6][O:7][c:8]2[cH:9][cH:10][c:11]([O:12][c:13]3[cH:14][cH:15][cH:16][cH:17][cH:18]3)[cH:19][c:20]2[Cl:21])[cH:22][n:23]1
ClCc1ccc(Cl)nc1.Oc1ccc(Oc2ccccc2)cc1Cl
Clc1ccc(COc2ccc(Oc3ccccc3)cc2Cl)cn1
null
null
CN(C=O)C
Heteroatom Alkylation and Arylation
Williamson Ether Synthesis
7e1040116e3a4cf0e8ec5cc7865388d9cd0efabce6d320a1c25a36e411018d8b
d5f4610d46ccc0478471c5bc0fb862644eaf764bbc5d93badb39d54f6ec8e0a5
c1ccc(Oc2ccc(OCc3cccnc3)cc2)cc1
Cl-[CH2;D2;+0:1]-[c:2](:[c:3]):[c:4]:[#7;a:5]:[c:6].[OH;D1;+0:7]-[c:8](:[c:9]):[c:10]>>[c:9]:[c:8](-[O;H0;D2;+0:7]-[CH2;D2;+0:1]-[c:2](:[c:3]):[c:4]:[#7;a:5]:[c:6]):[c:10]
70.8
[{"value": 70.8, "product": "ClC1=NC=C(C=C1)COC1=C(C=C(C=C1)OC1=CC=CC=C1)Cl", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
30
MINUTE
To a solution of 0.09 g of sodium hydride (60% oil dispersion) in 10 ml of N,N-dimethylformamide, there was added dropwise a solution of 0.45 g of 2-chloro-4-phenoxyphenol in 3 ml of N,N-dimethylformamide with stirring and ice-cooling. After 30 minutes, a solution of 0.34 g of 2-chloro-5-chloromethylpyridine in 5 ml of...
10.6084/m9.figshare.5104873.v1
null
Primary halide.Aromatic alcohol
Ether
null
null
c1ccncc1.c1ccccc1.c1ccccc1
HCl
CN(C=O)C
null
0.5
ClCc1ccc(Cl)nc1.Oc1ccc(Oc2ccccc2)cc1Cl>CN(C=O)C>Clc1ccc(COc2ccc(Oc3ccccc3)cc2Cl)cn1
ord_dataset-02ee2261663048188cf6d85d2cc96e3f
ord-cfef7c7616f74cf4b1c7989b7ccd6e17
ClCc1ccc(Cl)nc1.Oc1ccc(Oc2cccc(C(F)(F)F)c2)cc1Cl>>FC(F)(F)c1cccc(Oc2ccc(OCc3ccc(Cl)nc3)c(Cl)c2)c1
[H-].[Na+].ClC1=C(C=CC(=C1)OC1=CC(=CC=C1)C(F)(F)F)O.ClC1=NC=C(C=C1)CCl>>ClC1=NC=C(C=C1)COC1=C(C=C(C=C1)OC1=CC(=CC=C1)C(F)(F)F)Cl
Cl[CH2:16][c:17]1[cH:18][cH:19][c:20]([Cl:21])[n:22][cH:23]1.[F:1][C:2]([F:3])([F:4])[c:5]1[cH:6][cH:7][cH:8][c:9]([O:10][c:11]2[cH:12][cH:13][c:14]([OH:15])[c:24]([Cl:25])[cH:26]2)[cH:27]1>>[F:1][C:2]([F:3])([F:4])[c:5]1[cH:6][cH:7][cH:8][c:9]([O:10][c:11]2[cH:12][cH:13][c:14]([O:15][CH2:16][c:17]3[cH:18][cH:19][c:20]...
ClCc1ccc(Cl)nc1.Oc1ccc(Oc2cccc(C(F)(F)F)c2)cc1Cl
FC(F)(F)c1cccc(Oc2ccc(OCc3ccc(Cl)nc3)c(Cl)c2)c1
null
null
CN(C=O)C
Heteroatom Alkylation and Arylation
Williamson Ether Synthesis
7e1040116e3a4cf0e8ec5cc7865388d9cd0efabce6d320a1c25a36e411018d8b
d5f4610d46ccc0478471c5bc0fb862644eaf764bbc5d93badb39d54f6ec8e0a5
c1ccc(Oc2ccc(OCc3cccnc3)cc2)cc1
Cl-[CH2;D2;+0:1]-[c:2](:[c:3]):[c:4]:[#7;a:5]:[c:6].[OH;D1;+0:7]-[c:8](:[c:9]):[c:10]>>[c:9]:[c:8](-[O;H0;D2;+0:7]-[CH2;D2;+0:1]-[c:2](:[c:3]):[c:4]:[#7;a:5]:[c:6]):[c:10]
null
[]
null
null
30
MINUTE
To a solution 0.07 g of sodium hydride (60% oil dispersion) in 10 ml of N,N-dimethylformamide, there was added dropwise a solution of 0.50 g of 2-chloro-4-(3-trifluoromethylphenoxy)phenol in 3 ml of N,N-dimethylformamide with stirring and ice-cooling. After 30 minutes, a solution of 0.28 g of 2-chloro-5-chloromethylpyr...
10.6084/m9.figshare.5104873.v1
null
Primary halide.Aromatic alcohol
Ether
null
null
c1ccccc1.c1ccccc1.c1ccncc1
HCl
CN(C=O)C
null
0.5
ClCc1ccc(Cl)nc1.Oc1ccc(Oc2cccc(C(F)(F)F)c2)cc1Cl>CN(C=O)C>FC(F)(F)c1cccc(Oc2ccc(OCc3ccc(Cl)nc3)c(Cl)c2)c1
ord_dataset-02ee2261663048188cf6d85d2cc96e3f
ord-1b4f35597bfc40f99c6612fc401f6e22
ClCc1ccc(Cl)nc1.Oc1ccc(Oc2cccc(Br)c2)cc1Cl>>Clc1ccc(COc2ccc(Oc3cccc(Br)c3)cc2Cl)cn1
[H-].[Na+].ClC1=C(C=CC(=C1)OC1=CC(=CC=C1)Br)O.ClC1=NC=C(C=C1)CCl>>ClC1=NC=C(C=C1)COC1=C(C=C(C=C1)OC1=CC(=CC=C1)Br)Cl
Cl[CH2:6][c:5]1[cH:4][cH:3][c:2]([Cl:1])[n:24][cH:23]1.[OH:7][c:8]1[cH:9][cH:10][c:11]([O:12][c:13]2[cH:14][cH:15][cH:16][c:17]([Br:18])[cH:19]2)[cH:20][c:21]1[Cl:22]>>[Cl:1][c:2]1[cH:3][cH:4][c:5]([CH2:6][O:7][c:8]2[cH:9][cH:10][c:11]([O:12][c:13]3[cH:14][cH:15][cH:16][c:17]([Br:18])[cH:19]3)[cH:20][c:21]2[Cl:22])[cH:...
ClCc1ccc(Cl)nc1.Oc1ccc(Oc2cccc(Br)c2)cc1Cl
Clc1ccc(COc2ccc(Oc3cccc(Br)c3)cc2Cl)cn1
null
null
CN(C=O)C
Heteroatom Alkylation and Arylation
Williamson Ether Synthesis
7e1040116e3a4cf0e8ec5cc7865388d9cd0efabce6d320a1c25a36e411018d8b
d5f4610d46ccc0478471c5bc0fb862644eaf764bbc5d93badb39d54f6ec8e0a5
c1ccc(Oc2ccc(OCc3cccnc3)cc2)cc1
Cl-[CH2;D2;+0:1]-[c:2](:[c:3]):[c:4]:[#7;a:5]:[c:6].[OH;D1;+0:7]-[c:8](:[c:9]):[c:10]>>[c:9]:[c:8](-[O;H0;D2;+0:7]-[CH2;D2;+0:1]-[c:2](:[c:3]):[c:4]:[#7;a:5]:[c:6]):[c:10]
null
[]
null
null
30
MINUTE
To a solution of 0.07 g of sodium hydride (60% oil dispersion) in 10 ml of N,N-dimethylformamide, there is added dropwise a solution of 0.50 g of 2-chloro-4-(3-bromophenoxy)phenol in 3 ml of N,N-dimethylformamide with stirring and ice-cooling. After 30 minutes, a solution of 0.27 g of 2-chloro-5-chloromethylpyridine in...
10.6084/m9.figshare.5104873.v1
null
Primary halide.Aromatic alcohol
Ether
null
null
c1ccncc1.c1ccccc1.c1ccccc1
HCl
CN(C=O)C
null
0.5
ClCc1ccc(Cl)nc1.Oc1ccc(Oc2cccc(Br)c2)cc1Cl>CN(C=O)C>Clc1ccc(COc2ccc(Oc3cccc(Br)c3)cc2Cl)cn1
ord_dataset-02ee2261663048188cf6d85d2cc96e3f
ord-11045075c0464d549a020ace23fc45e9
Oc1ccc(Oc2cc(F)cc(F)c2)cc1>>Oc1ccc(Oc2cc(F)cc(F)c2)cc1Cl
FC=1C=C(OC2=CC=C(C=C2)O)C=C(C1)F>>ClC1=C(C=CC(=C1)OC1=CC(=CC(=C1)F)F)O
[OH:1][c:2]1[cH:3][cH:4][c:5]([O:6][c:7]2[cH:8][c:9]([F:10])[cH:11][c:12]([F:13])[cH:14]2)[cH:15][cH:16]1>>[OH:1][c:2]1[cH:3][cH:4][c:5]([O:6][c:7]2[cH:8][c:9]([F:10])[cH:11][c:12]([F:13])[cH:14]2)[cH:15][c:16]1[Cl:17]
Oc1ccc(Oc2cc(F)cc(F)c2)cc1
Oc1ccc(Oc2cc(F)cc(F)c2)cc1Cl
null
null
C(Cl)(Cl)(Cl)Cl
Functional Group Addition
Aromatic chlorination
2e63a9b91d60f82a8e59b7c72ed55b9aec048f26be2f5eb9ca65b1b73867743c
0a2f22058f27970cef4a98a778644dbe9c44e91f66c74cd24db321993177608a
c1ccc(Oc2ccccc2)cc1
[O;D1;H1:1]-[c:2](:[c:3]):[cH;D2;+0:4]:[c:5]:[c:6]>>[Cl;D1;H0:7]-[c;H0;D3;+0:4](:[c:5]:[c:6]):[c:2](-[O;D1;H1:1]):[c:3]
null
[]
null
null
5
HOUR
To a solution of 5.0 g p-(3,5-difluorophenoxy)phenol in 50 mg of carbon tetrachloride, there were added dropwise 2.45 of tert-butylhypochlorous acid with stirring and ice-cooling, and stirring was continued at room temperature for 5 hours. The reaction mixture was concentrated and extracted with 200 ml of ethyl acetate...
10.6084/m9.figshare.5104873.v1
null
null
Aromatic halide
c1ccccc1
c1ccccc1
c1ccccc1.c1ccccc1
Other
C(Cl)(Cl)(Cl)Cl
null
5
Oc1ccc(Oc2cc(F)cc(F)c2)cc1>C(Cl)(Cl)(Cl)Cl>Oc1ccc(Oc2cc(F)cc(F)c2)cc1Cl
ord_dataset-02ee2261663048188cf6d85d2cc96e3f
ord-7cea9b0826894985a9e86e4b858b5be2
BrCCCCCCBr.OCCc1ccccc1>>BrCCCCCCOCCc1ccccc1
C(CC1=CC=CC=C1)O.BrCCCCCCBr.[OH-].[Na+]>>BrCCCCCCOCCC1=CC=CC=C1
Br[CH2:7][CH2:6][CH2:5][CH2:4][CH2:3][CH2:2][Br:1].[OH:8][CH2:9][CH2:10][c:11]1[cH:12][cH:13][cH:14][cH:15][cH:16]1>>[Br:1][CH2:2][CH2:3][CH2:4][CH2:5][CH2:6][CH2:7][O:8][CH2:9][CH2:10][c:11]1[cH:12][cH:13][cH:14][cH:15][cH:16]1
BrCCCCCCBr.OCCc1ccccc1
BrCCCCCCOCCc1ccccc1
null
S([O-])(O)(=O)=O.C(CCC)[N+](CCCC)(CCCC)CCCC
O
Heteroatom Alkylation and Arylation
Williamson Ether Synthesis
dd3f9c60e1f90d961a7c01d970ae213561355ee1451f276a3b04696e4b6fae5c
46a6e883cf919b4006e69abfdfd883f458f55c08b3200960c6a5b57c4139fbca
c1ccccc1
Br-[CH2;D2;+0:1]-[C:2]-[C:3].[C:4]-[C:5]-[OH;D1;+0:6]>>[C:4]-[C:5]-[O;H0;D2;+0:6]-[CH2;D2;+0:1]-[C:2]-[C:3]
55.7
[{"value": 55.7, "product": "BrCCCCCCOCCC1=CC=CC=C1", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
null
null
A mixture of phenethyl alcohol (20 g), 1,6-dibromohexane (195 g) and tetrabutylammonium bisulphate (3.0 g) in 50% w/v NaOH solution (100 ml) was heated at 65-70° for 4h. The cooled reaction mixture was poured into H2O (400 ml) and extracted with CX (2×300 ml). The dried extracts were evaporated in vacuo to give a yello...
10.6084/m9.figshare.5104873.v1
null
Primary halide.Primary alcohol
Ether
null
null
c1ccccc1
HBr
S([O-])(O)(=O)=O.C(CCC)[N+](CCCC)(CCCC)CCCC.O
null
null
BrCCCCCCBr.OCCc1ccccc1>S([O-])(O)(=O)=O.C(CCC)[N+](CCCC)(CCCC)CCCC.O>BrCCCCCCOCCc1ccccc1
ord_dataset-02ee2261663048188cf6d85d2cc96e3f
ord-17aed5b9702b46f69ddfc58fdccf4fd4
BrCCCCCCBr.OCCCCc1ccccc1>>BrCCCCCCOCCCCc1ccccc1
O.[H-].[Na+].C1(=CC=CC=C1)CCCCO.BrCCCCCCBr>>BrCCCCCCOCCCCC1=CC=CC=C1
Br[CH2:7][CH2:6][CH2:5][CH2:4][CH2:3][CH2:2][Br:1].[OH:8][CH2:9][CH2:10][CH2:11][CH2:12][c:13]1[cH:14][cH:15][cH:16][cH:17][cH:18]1>>[Br:1][CH2:2][CH2:3][CH2:4][CH2:5][CH2:6][CH2:7][O:8][CH2:9][CH2:10][CH2:11][CH2:12][c:13]1[cH:14][cH:15][cH:16][cH:17][cH:18]1
BrCCCCCCBr.OCCCCc1ccccc1
BrCCCCCCOCCCCc1ccccc1
null
null
C1CCOC1
Heteroatom Alkylation and Arylation
Williamson Ether Synthesis
dd3f9c60e1f90d961a7c01d970ae213561355ee1451f276a3b04696e4b6fae5c
46a6e883cf919b4006e69abfdfd883f458f55c08b3200960c6a5b57c4139fbca
c1ccccc1
Br-[CH2;D2;+0:1]-[C:2]-[C:3].[C:4]-[C:5]-[OH;D1;+0:6]>>[C:4]-[C:5]-[O;H0;D2;+0:6]-[CH2;D2;+0:1]-[C:2]-[C:3]
48
[{"value": 48.0, "product": "BrCCCCCCOCCCCC1=CC=CC=C1", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
null
null
NaH (46% dispersion in oil; 6.5 g) was added portionwise to a solution of 4-phenyl-1-butanol (15.0 g) and 1,6-dibromohexane (48.8 g) in THF (200 ml) under nitrogen. The resulting suspension was refluxed for 27 h and treated with H2O (80 ml). The mixture was extracted with ER (2×200 ml) and the dried extract was evapora...
10.6084/m9.figshare.5104873.v1
null
Primary halide.Primary alcohol
Ether
null
null
c1ccccc1
HBr
C1CCOC1
null
null
BrCCCCCCBr.OCCCCc1ccccc1>C1CCOC1>BrCCCCCCOCCCCc1ccccc1
ord_dataset-02ee2261663048188cf6d85d2cc96e3f
ord-c168fac950b8444d8d024b6f43774ded
C=C(C)OC.O=C(CBr)c1ccc(O)c(CO)c1>>CC1(C)OCc2cc(C(=O)CBr)ccc2O1
COC(=C)C.BrCC(=O)C1=CC(=C(C=C1)O)CO.C1(=CC=C(C=C1)S(=O)(=O)O)C>>BrCC(=O)C1=CC2=C(OC(OC2)(C)C)C=C1
CO[C:2](=[CH2:1])[CH3:3].[OH:4][CH2:5][c:6]1[cH:7][c:8]([C:9](=[O:10])[CH2:11][Br:12])[cH:13][cH:14][c:15]1[OH:16]>>[CH3:1][C:2]1([CH3:3])[O:4][CH2:5][c:6]2[cH:7][c:8]([C:9](=[O:10])[CH2:11][Br:12])[cH:13][cH:14][c:15]2[O:16]1
C=C(C)OC.O=C(CBr)c1ccc(O)c(CO)c1
CC1(C)OCc2cc(C(=O)CBr)ccc2O1
null
null
C(Cl)Cl
Heteroatom Alkylation and Arylation
OtherReaction
0f672d215e527014d9141e70d05d5718fa217fdfa248c8eb2528a90aa9055ba8
8119ee9e00187f1c0b478e3c1dce92c3b914153c12cfed038c7de8671ef37557
c1ccc2c(c1)COCO2
C-O-[C;H0;D3;+0:1](-[C;D1;H3:2])=[CH2;D1;+0:3].[OH;D1;+0:4]-[c:5](:[c:6]):[c:7]-[C:8]-[OH;D1;+0:9]>>[C;D1;H3:2]-[C;H0;D4;+0:1]1(-[CH3;D1;+0:3])-[O;H0;D2;+0:4]-[c:5](:[c:6]):[c:7]-[C:8]-[O;H0;D2;+0:9]-1
82.5
[{"value": 82.5, "product": "BrCC(=O)C1=CC2=C(OC(OC2)(C)C)C=C1", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
null
null
2-Methoxypropene (10 g) was added over 15 min to a stirred solution of 2-bromo-1-[4-hydroxy-3-(hydroxymethyl)phenyl]ethanone (5 g) and toluene-4-sulphonic acid (0.5 g) in CH2Cl2 (100 ml) at 23°. The mixture was stirred for 3h, filtered through a wad of triethylamine-deactivated silica and evaporated to give an oil. Pur...
10.6084/m9.figshare.5104873.v1
null
Ether.Primary alcohol.Aromatic alcohol.Vinyl
Ether.Ether
null
c1ccc2c(c1)COCO2
c1ccc2c(c1)COCO2
HO-
C(Cl)Cl
null
null
C=C(C)OC.O=C(CBr)c1ccc(O)c(CO)c1>C(Cl)Cl>CC1(C)OCc2cc(C(=O)CBr)ccc2O1
ord_dataset-02ee2261663048188cf6d85d2cc96e3f
ord-b0c4d599e3284cc39dfd6ae880a00517
BrCCCCCCBr.OCCCc1ccccc1>>BrCCCCCCOCCCc1ccccc1
C1(=CC=CC=C1)CCCO.S(=O)(=O)(O)O.BrCCCCCCBr.[OH-].[Na+]>>BrCCCCCCOCCCC=1C=CC=CC1
Br[CH2:7][CH2:6][CH2:5][CH2:4][CH2:3][CH2:2][Br:1].[OH:8][CH2:9][CH2:10][CH2:11][c:12]1[cH:13][cH:14][cH:15][cH:16][cH:17]1>>[Br:1][CH2:2][CH2:3][CH2:4][CH2:5][CH2:6][CH2:7][O:8][CH2:9][CH2:10][CH2:11][c:12]1[cH:13][cH:14][cH:15][cH:16][cH:17]1
BrCCCCCCBr.OCCCc1ccccc1
BrCCCCCCOCCCc1ccccc1
null
null
O
Heteroatom Alkylation and Arylation
Williamson Ether Synthesis
dd3f9c60e1f90d961a7c01d970ae213561355ee1451f276a3b04696e4b6fae5c
46a6e883cf919b4006e69abfdfd883f458f55c08b3200960c6a5b57c4139fbca
c1ccccc1
Br-[CH2;D2;+0:1]-[C:2]-[C:3].[C:4]-[C:5]-[OH;D1;+0:6]>>[C:4]-[C:5]-[O;H0;D2;+0:6]-[CH2;D2;+0:1]-[C:2]-[C:3]
1,223
[{"value": 1223.0, "product": "BrCCCCCCOCCCC=1C=CC=CC1", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
null
null
3-Phenylpropanol (3.00 g) and 1,6-dibromohexane hydrogen sulphate (0.5 g) and 12.5 M aqueous NaOH (16 ml) for 30 h. The mixture was diluted with H2O (80 ml), extracted with ER (3×100 ml), and the combined organic extracts were washed consecutively with H2O (80 ml) and BR (80 ml). The dried extracts were evaporated and ...
10.6084/m9.figshare.5104873.v1
null
Primary halide.Primary alcohol
Ether
null
null
c1ccccc1
HBr
O
null
null
BrCCCCCCBr.OCCCc1ccccc1>O>BrCCCCCCOCCCc1ccccc1
ord_dataset-02ee2261663048188cf6d85d2cc96e3f
ord-ac03c135aa2e493cb63eaf76ba6c32fa
BrCCCCCCBr.COc1ccccc1CCCCO>>COc1ccccc1CCCCOCCCCCCBr
O.[H-].[Na+].COC1=C(C=CC=C1)CCCCO.BrCCCCCCBr>>BrCCCCCCOCCCCC1=C(C=CC=C1)OC
Br[CH2:14][CH2:15][CH2:16][CH2:17][CH2:18][CH2:19][Br:20].[CH3:1][O:2][c:3]1[cH:4][cH:5][cH:6][cH:7][c:8]1[CH2:9][CH2:10][CH2:11][CH2:12][OH:13]>>[CH3:1][O:2][c:3]1[cH:4][cH:5][cH:6][cH:7][c:8]1[CH2:9][CH2:10][CH2:11][CH2:12][O:13][CH2:14][CH2:15][CH2:16][CH2:17][CH2:18][CH2:19][Br:20]
BrCCCCCCBr.COc1ccccc1CCCCO
COc1ccccc1CCCCOCCCCCCBr
null
null
C1CCOC1
Heteroatom Alkylation and Arylation
Williamson Ether Synthesis
dd3f9c60e1f90d961a7c01d970ae213561355ee1451f276a3b04696e4b6fae5c
46a6e883cf919b4006e69abfdfd883f458f55c08b3200960c6a5b57c4139fbca
c1ccccc1
Br-[CH2;D2;+0:1]-[C:2]-[C:3].[C:4]-[C:5]-[OH;D1;+0:6]>>[C:4]-[C:5]-[O;H0;D2;+0:6]-[CH2;D2;+0:1]-[C:2]-[C:3]
58.8
[{"value": 58.8, "product": "BrCCCCCCOCCCCC1=C(C=CC=C1)OC", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
null
null
NaH (46% dispersion in oil; 1.36 g) was added portionwise to a solution of 2-methoxybenzenebutanol (5.0 g) and 1,6-dibromohexane (13.8 g) in THF (50 ml). The suspension was refluxed for 20 h and was treated cautiously with H2O (20 ml). The resulting emulsion was extracted with ER (2×50 ml) and the dried extract was eva...
10.6084/m9.figshare.5104873.v1
null
Primary halide.Primary alcohol
Ether
null
null
c1ccccc1
HBr
C1CCOC1
null
null
BrCCCCCCBr.COc1ccccc1CCCCO>C1CCOC1>COc1ccccc1CCCCOCCCCCCBr
ord_dataset-02ee2261663048188cf6d85d2cc96e3f
ord-5c394360b9934f6ea34c45ca866ffcda
BrCCCc1ccccc1.C1COC1>>OCCCCCCc1ccccc1
BrCCCC1=CC=CC=C1.[Mg].[NH4+].[Cl-].O1CCC1>>C1(=CC=CC=C1)CCCCCCO
Br[CH2:5][CH2:6][CH2:7][c:8]1[cH:9][cH:10][cH:11][cH:12][cH:13]1.[O:1]1[CH2:2][CH2:3][CH2:4]1>>[OH:1][CH2:2][CH2:3][CH2:4][CH2:5][CH2:6][CH2:7][c:8]1[cH:9][cH:10][cH:11][cH:12][cH:13]1
BrCCCc1ccccc1.C1COC1
OCCCCCCc1ccccc1
null
null
C1CCOC1
C-C Coupling
OtherReaction
637c455f8adb2e182e9efd933b19dd0e74f5dc12d12c6269b2293bb0d517dc42
30e13948c8786a09f1276ae1d49b379da946c0f461d188344ec892c684344fba
c1ccccc1
Br-[CH2;D2;+0:1]-[C:2]-[C:3].[C:4]1-[C:5]-[CH2;D2;+0:6]-[O;H0;D2;+0:7]-1>>[C:3]-[C:2]-[CH2;D2;+0:1]-[CH2;D2;+0:6]-[C:5]-[C:4]-[OH;D1;+0:7]
33.8
[{"value": 33.8, "product": "C1(=CC=CC=C1)CCCCCCO", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
2
HOUR
(3-Bromopropyl)benzene (20 g) in THF (75 ml) was added dropwise to magnesium (2.43 g) at a rate to maintain gentle reflux. The mixture was stirred for 2 h at RT and oxetane (10 g) was added dropwise. The resulting suspension was stirred at RT for 2h and at reflux for 16 h and poured into saturated aqueous NH4Cl (100 ml...
10.6084/m9.figshare.5104873.v1
null
Primary halide.Ether
Primary alcohol
C1COC1
null
c1ccccc1
Br-
C1CCOC1
null
2
BrCCCc1ccccc1.C1COC1>C1CCOC1>OCCCCCCc1ccccc1
ord_dataset-02ee2261663048188cf6d85d2cc96e3f
ord-8d888550453845d89f366f2eeaefe39f
C1=COCCC1.OCCCCCl>>ClCCCCOC1CCCCO1
O1CCCC=C1.ClCCCCO>>ClCCCCOC1OCCCC1
[CH:7]1=[CH:8][CH2:9][CH2:10][CH2:11][O:12]1.[Cl:1][CH2:2][CH2:3][CH2:4][CH2:5][OH:6]>>[Cl:1][CH2:2][CH2:3][CH2:4][CH2:5][O:6][CH:7]1[CH2:8][CH2:9][CH2:10][CH2:11][O:12]1
C1=COCCC1.OCCCCCl
ClCCCCOC1CCCCO1
null
Cl
null
Heteroatom Alkylation and Arylation
oxa-Michael addition
abdcab389770d0a73be3b825aa1d56cee234da38dbdf3510fe8104d481e7cf3f
c6a3efa2acb508a32cdf9fcedfcd9635cce0ecdcf12c094b743aa576ea01fd9a
C1CCOCC1
[#8:1]1-[C:2]-[C:3]-[C:4]-[CH;D2;+0:5]=[CH;D2;+0:6]-1.[C:7]-[C:8]-[OH;D1;+0:9]>>[C:7]-[C:8]-[O;H0;D2;+0:9]-[CH;D3;+0:6]1-[#8:1]-[C:2]-[C:3]-[C:4]-[CH2;D2;+0:5]-1
89.9
[{"value": 89.9, "product": "ClCCCCOC1OCCCC1", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
30
MINUTE
Dihydropyran (15.5 g) was added dropwise to a mixture of 4-chlorobutanol (20 g) and hydrochloric acid (18 M, 1 drop) at RT. The mixture was stirred for 30 min and washed with H2O (100 ml), aqueous NaHCO3 (1 M, 50 ml) and BR (50 ml). The dried liquid was heated under reduced pressure to leave the title compound as a col...
10.6084/m9.figshare.5104873.v1
null
Ether.Primary alcohol
Ether.Ether
C1=COCCC1
C1CCOCC1
C1CCOCC1
null
Cl
null
0.5
C1=COCCC1.OCCCCCl>Cl>ClCCCCOC1CCCCO1
ord_dataset-02ee2261663048188cf6d85d2cc96e3f
ord-acc0d0ac996740c1aa636be541a52c57
BrCCCCCCBr.Cc1cccc(C)c1CCO>>Cc1cccc(C)c1CCOCCCCCCBr
[H-].[Na+].CC1=C(C(=CC=C1)C)CCO.BrCCCCCCBr.O>>BrCCCCCCOCCC1=C(C=CC=C1C)C
Br[CH2:12][CH2:13][CH2:14][CH2:15][CH2:16][CH2:17][Br:18].[CH3:1][c:2]1[cH:3][cH:4][cH:5][c:6]([CH3:7])[c:8]1[CH2:9][CH2:10][OH:11]>>[CH3:1][c:2]1[cH:3][cH:4][cH:5][c:6]([CH3:7])[c:8]1[CH2:9][CH2:10][O:11][CH2:12][CH2:13][CH2:14][CH2:15][CH2:16][CH2:17][Br:18]
BrCCCCCCBr.Cc1cccc(C)c1CCO
Cc1cccc(C)c1CCOCCCCCCBr
null
null
C1CCOC1
Heteroatom Alkylation and Arylation
Williamson Ether Synthesis
dd3f9c60e1f90d961a7c01d970ae213561355ee1451f276a3b04696e4b6fae5c
46a6e883cf919b4006e69abfdfd883f458f55c08b3200960c6a5b57c4139fbca
c1ccccc1
Br-[CH2;D2;+0:1]-[C:2]-[C:3].[C:4]-[C:5]-[OH;D1;+0:6]>>[C:3]-[C:2]-[CH2;D2;+0:1]-[O;H0;D2;+0:6]-[C:5]-[C:4]
52.7
[{"value": 52.7, "product": "BrCCCCCCOCCC1=C(C=CC=C1C)C", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
null
null
NaH (46% dispersion in oil; 4.2 g) was added portionwise to a solution f 2,6-dimethylbenzenethanol (6.0 g) and 1,6-dibromohexane (19.52 g) in THF (50 ml) under nitrogen. The mixture was refluxed for 18 h and treated cautiously with H2O (20 ml). The resulting emulsion was extracted with ER (3×100 ml) and the dried extra...
10.6084/m9.figshare.5104873.v1
null
Primary halide.Primary alcohol
Ether
null
null
c1ccccc1
HBr
C1CCOC1
null
null
BrCCCCCCBr.Cc1cccc(C)c1CCO>C1CCOC1>Cc1cccc(C)c1CCOCCCCCCBr
ord_dataset-02ee2261663048188cf6d85d2cc96e3f
ord-818d644ce64a41d8816409c37119191b
C1COC1.Fc1ccc(Br)cc1>>OCCCc1ccc(F)cc1
II.O1CCC1.[NH4+].[Cl-].BrC1=CC=C(C=C1)F.[Mg]>>FC1=CC=C(C=C1)CCCO
[O:1]1[CH2:2][CH2:4][CH2:3]1.Br[c:5]1[cH:6][cH:7][c:8]([F:9])[cH:10][cH:11]1>>[OH:1][CH2:2][CH2:3][CH2:4][c:5]1[cH:6][cH:7][c:8]([F:9])[cH:10][cH:11]1
C1COC1.Fc1ccc(Br)cc1
OCCCc1ccc(F)cc1
null
null
C1CCOC1
C-C Coupling
OtherReaction
ab402a405392853d5b7c6e8072d47a43f8468f3d0c950058e1f959f41ce09a3a
104534dc5f965e596cd2f673f5d9f6169287a1e8ccc931bc81d74b3081323966
c1ccccc1
Br-[c;H0;D3;+0:1](:[c:2]:[c:3]):[c:4]:[c:5].[CH2;D2;+0:6]1-[CH2;D2;+0:7]-[CH2;D2;+0:8]-[O;H0;D2;+0:9]-1>>[OH;D1;+0:9]-[CH2;D2;+0:6]-[CH2;D2;+0:8]-[CH2;D2;+0:7]-[c;H0;D3;+0:1](:[c:2]:[c:3]):[c:4]:[c:5]
51.6
[{"value": 51.6, "product": "FC1=CC=C(C=C1)CCCO", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
null
null
A Grignard reagent was prepared from 4-bromo-1-fluorobenzene (8.0 g)., magnesium turnings (1.10 g), and iodine (one small crystal) in THF (40 ml). Oxetane (2.3 g) in THF (10 ml) was added at RT and the reaction mixture was heated at reflux overnight. The cooled solution was poured into aqueous saturated NH4Cl (100 ml),...
10.6084/m9.figshare.5104873.v1
null
Aromatic halide.Ether
Primary alcohol
C1COC1.c1ccccc1
c1ccccc1
c1ccccc1
Br-
C1CCOC1
null
null
C1COC1.Fc1ccc(Br)cc1>C1CCOC1>OCCCc1ccc(F)cc1
ord_dataset-02ee2261663048188cf6d85d2cc96e3f
ord-b66b5c858c9f4603b5c7693801f728e2
BrCCCCCCBr.COc1ccc(CCO)cc1>>COc1ccc(CCOCCCCCCBr)cc1
COC1=CC=C(C=C1)CCO.BrCCCCCCBr.[OH-].[Na+]>>BrCCCCCCOCCC1=CC=C(C=C1)OC
Br[CH2:10][CH2:11][CH2:12][CH2:13][CH2:14][CH2:15][Br:16].[CH3:1][O:2][c:3]1[cH:4][cH:5][c:6]([CH2:7][CH2:8][OH:9])[cH:17][cH:18]1>>[CH3:1][O:2][c:3]1[cH:4][cH:5][c:6]([CH2:7][CH2:8][O:9][CH2:10][CH2:11][CH2:12][CH2:13][CH2:14][CH2:15][Br:16])[cH:17][cH:18]1
BrCCCCCCBr.COc1ccc(CCO)cc1
COc1ccc(CCOCCCCCCBr)cc1
null
S([O-])(O)(=O)=O.C(CCC)[N+](CCCC)(CCCC)CCCC
O
Heteroatom Alkylation and Arylation
Williamson Ether Synthesis
dd3f9c60e1f90d961a7c01d970ae213561355ee1451f276a3b04696e4b6fae5c
46a6e883cf919b4006e69abfdfd883f458f55c08b3200960c6a5b57c4139fbca
c1ccccc1
Br-[CH2;D2;+0:1]-[C:2]-[C:3].[C:4]-[C:5]-[OH;D1;+0:6]>>[C:3]-[C:2]-[CH2;D2;+0:1]-[O;H0;D2;+0:6]-[C:5]-[C:4]
237.5
[{"value": 237.5, "product": "BrCCCCCCOCCC1=CC=C(C=C1)OC", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
null
null
4-Methoxybenzeneethanol (5.0 g) and 1,6-dibromohexane (23.7 g) were stirred rapidly at RT with tetra-n-butyl ammonium bisulphate (0.94 g) and 12.5 M aqueous NaOH (30 ml) for 16 h. The mixture was diluted with H2O (125 ml), extracted with ER (3×150 ml) and the combined organic extracts were washed consecutively with H2O...
10.6084/m9.figshare.5104873.v1
null
Primary halide.Primary alcohol
Ether
null
null
c1ccccc1
HBr
S([O-])(O)(=O)=O.C(CCC)[N+](CCCC)(CCCC)CCCC.O
null
null
BrCCCCCCBr.COc1ccc(CCO)cc1>S([O-])(O)(=O)=O.C(CCC)[N+](CCCC)(CCCC)CCCC.O>COc1ccc(CCOCCCCCCBr)cc1
ord_dataset-02ee2261663048188cf6d85d2cc96e3f
ord-e69fe70ae7ca4200a4a1976a61404a61
BrCCCCCBr.OCCc1ccc(F)cc1>>Fc1ccc(CCOCCCCCBr)cc1
FC1=CC=C(C=C1)CCO.BrCCCCCBr.[OH-].[Na+]>>BrCCCCCOCCC1=CC=C(C=C1)F
Br[CH2:9][CH2:10][CH2:11][CH2:12][CH2:13][Br:14].[F:1][c:2]1[cH:3][cH:4][c:5]([CH2:6][CH2:7][OH:8])[cH:15][cH:16]1>>[F:1][c:2]1[cH:3][cH:4][c:5]([CH2:6][CH2:7][O:8][CH2:9][CH2:10][CH2:11][CH2:12][CH2:13][Br:14])[cH:15][cH:16]1
BrCCCCCBr.OCCc1ccc(F)cc1
Fc1ccc(CCOCCCCCBr)cc1
null
S(=O)(=O)(O)[O-].C(CCC)[N+](CCCC)(CCCC)CCCC
O
Heteroatom Alkylation and Arylation
Williamson Ether Synthesis
dd3f9c60e1f90d961a7c01d970ae213561355ee1451f276a3b04696e4b6fae5c
46a6e883cf919b4006e69abfdfd883f458f55c08b3200960c6a5b57c4139fbca
c1ccccc1
Br-[CH2;D2;+0:1]-[C:2]-[C:3].[C:4]-[C:5]-[OH;D1;+0:6]>>[C:3]-[C:2]-[CH2;D2;+0:1]-[O;H0;D2;+0:6]-[C:5]-[C:4]
null
[]
null
null
null
null
4-Fluorobenzeneethanol (10.0 g), 1,5-dibromopentane (29 ml), tetra-n-butylammonium hydrogen sulphate (3.2 g, 9 mmol), and aqueous 12.5 M NaOH (109 ml) were stirred vigorously at RT overnight. The mixture was diluted with H2O (400 ml), extracted with ER (3×200 ml), and the combined organic extracts were evaporated. The ...
10.6084/m9.figshare.5104873.v1
null
Primary halide.Primary alcohol
Ether
null
null
c1ccccc1
HBr
S(=O)(=O)(O)[O-].C(CCC)[N+](CCCC)(CCCC)CCCC.O
null
null
BrCCCCCBr.OCCc1ccc(F)cc1>S(=O)(=O)(O)[O-].C(CCC)[N+](CCCC)(CCCC)CCCC.O>Fc1ccc(CCOCCCCCBr)cc1
ord_dataset-02ee2261663048188cf6d85d2cc96e3f
ord-b8644227ad934494a702894e391ecfb3
BrCCCCCBr.COc1ccc(CCCO)cc1>>COc1ccc(CCCOCCCCCBr)cc1
COC1=CC=C(C=C1)CCCO.BrCCCCCBr.[OH-].[Na+]>>BrCCCCCOCCCC1=CC=C(C=C1)OC
Br[CH2:11][CH2:12][CH2:13][CH2:14][CH2:15][Br:16].[CH3:1][O:2][c:3]1[cH:4][cH:5][c:6]([CH2:7][CH2:8][CH2:9][OH:10])[cH:17][cH:18]1>>[CH3:1][O:2][c:3]1[cH:4][cH:5][c:6]([CH2:7][CH2:8][CH2:9][O:10][CH2:11][CH2:12][CH2:13][CH2:14][CH2:15][Br:16])[cH:17][cH:18]1
BrCCCCCBr.COc1ccc(CCCO)cc1
COc1ccc(CCCOCCCCCBr)cc1
null
S([O-])(O)(=O)=O.C(CCC)[N+](CCCC)(CCCC)CCCC
O
Heteroatom Alkylation and Arylation
Williamson Ether Synthesis
dd3f9c60e1f90d961a7c01d970ae213561355ee1451f276a3b04696e4b6fae5c
46a6e883cf919b4006e69abfdfd883f458f55c08b3200960c6a5b57c4139fbca
c1ccccc1
Br-[CH2;D2;+0:1]-[C:2]-[C:3].[C:4]-[C:5]-[OH;D1;+0:6]>>[C:3]-[C:2]-[CH2;D2;+0:1]-[O;H0;D2;+0:6]-[C:5]-[C:4]
244.6
[{"value": 244.6, "product": "BrCCCCCOCCCC1=CC=C(C=C1)OC", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
null
null
4-Methoxybenzenepropanol (7.5 g) and 1,5 dibromopentane (30.5 g) were stirred rapidly at RT with tetra-n-butylammonium bisulphate (1.02 g) and 12.5 M aqueous NaOH (36 ml) for 16 h. The mixture was diluted with H2O (170 ml), extracted with ER (3×20 ml) and the combined organic extracts were washed consecutively with H2O...
10.6084/m9.figshare.5104873.v1
null
Primary halide.Primary alcohol
Ether
null
null
c1ccccc1
HBr
S([O-])(O)(=O)=O.C(CCC)[N+](CCCC)(CCCC)CCCC.O
null
null
BrCCCCCBr.COc1ccc(CCCO)cc1>S([O-])(O)(=O)=O.C(CCC)[N+](CCCC)(CCCC)CCCC.O>COc1ccc(CCCOCCCCCBr)cc1
ord_dataset-02ee2261663048188cf6d85d2cc96e3f
ord-514bf848f79a4968bbf480ff0bb655b9
BrCCOCCCc1ccccc1.C#CC(C)(C)N>>CC(C)(N)C#CCCOCCCc1ccccc1
CC(C)(C#C)N.[Li+].[NH2-].BrCCOCCCC1=CC=CC=C1>>CC(C#CCCOCCCC1=CC=CC=C1)(N)C
Br[CH2:7][CH2:8][O:9][CH2:10][CH2:11][CH2:12][c:13]1[cH:14][cH:15][cH:16][cH:17][cH:18]1.[CH3:1][C:2]([CH3:3])([NH2:4])[C:5]#[CH:6]>>[CH3:1][C:2]([CH3:3])([NH2:4])[C:5]#[C:6][CH2:7][CH2:8][O:9][CH2:10][CH2:11][CH2:12][c:13]1[cH:14][cH:15][cH:16][cH:17][cH:18]1
BrCCOCCCc1ccccc1.C#CC(C)(C)N
CC(C)(N)C#CCCOCCCc1ccccc1
null
null
N
C-C Coupling
OtherReaction
a2902088eeffba8af7cde0e465024f8c5b6cd6239687cb7ab88d93a01519cd51
65c5c213019f4e08c3c32f7e1ced539ac3ff1efc4a39855e6d21bd16502eefc5
c1ccccc1
Br-[CH2;D2;+0:1]-[C:2]-[#8:3].[C:4]-[C:5]#[CH;D1;+0:6]>>[#8:3]-[C:2]-[CH2;D2;+0:1]-[C;H0;D2;+0:6]#[C:5]-[C:4]
13.8
[{"value": 13.8, "product": "CC(C#CCCOCCCC1=CC=CC=C1)(N)C", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
90
MINUTE
1,1-Dimethylpropargylamine (8.5 g) was added dropwise to a suspension of lithamide [from lithium (1.7 g)] in liquid ammonia (100 ml) at -33°. The mixture was stirred for 90 min and a solution of [3-(2-bromoethoxy)propyl]benzene (21.5 g) in ER (30 ml) was added dropwise. The suspension was stirred at 4 h and ammonia was...
10.6084/m9.figshare.5104873.v1
null
Primary halide.Alkyne
Alkyne
null
null
c1ccccc1
HBr
N
null
1.5
BrCCOCCCc1ccccc1.C#CC(C)(C)N>N>CC(C)(N)C#CCCOCCCc1ccccc1
ord_dataset-02ee2261663048188cf6d85d2cc96e3f
ord-cea66657c1d54213bd0be73281450b4e
CNC.COC(=O)c1cc(C(=O)CBr)ccc1OCc1ccccc1>>COC(=O)c1cc(C(O)CN(C)C)ccc1OCc1ccccc1
CNC.BrCC(=O)C=1C=CC(=C(C(=O)OC)C1)OCC1=CC=CC=C1.[BH4-].[Na+]>>CN(CC(O)C=1C=CC(=C(C(=O)OC)C1)OCC1=CC=CC=C1)C
[NH:11]([CH3:12])[CH3:13].Br[CH2:10][C:8]([c:7]1[cH:6][c:5]([C:3]([O:2][CH3:1])=[O:4])[c:16]([O:17][CH2:18][c:19]2[cH:20][cH:21][cH:22][cH:23][cH:24]2)[cH:15][cH:14]1)=[O:9]>>[CH3:1][O:2][C:3](=[O:4])[c:5]1[cH:6][c:7]([CH:8]([OH:9])[CH2:10][N:11]([CH3:12])[CH3:13])[cH:14][cH:15][c:16]1[O:17][CH2:18][c:19]1[cH:20][cH:21...
CNC.COC(=O)c1cc(C(=O)CBr)ccc1OCc1ccccc1
COC(=O)c1cc(C(O)CN(C)C)ccc1OCc1ccccc1
null
null
C(C)O.C1CCOC1
Heteroatom Alkylation and Arylation
OtherReaction
a65602a3b96095e5dbb2f138d3f287ce56a941015a66cef48c8137cee7280ea1
45a6cc47e2b15c343ede1c801f826eabfff338b5dc3020746051ac4edcfff0cc
c1ccc(COc2ccccc2)cc1
Br-[CH2;D2;+0:1]-[C;H0;D3;+0:2](=[O;H0;D1;+0:3])-[c:4](:[c:5]):[c:6].[C;D1;H3:7]-[NH;D2;+0:8]-[C;D1;H3:9]>>[C;D1;H3:7]-[N;H0;D3;+0:8](-[C;D1;H3:9])-[CH2;D2;+0:1]-[CH;D3;+0:2](-[OH;D1;+0:3])-[c:4](:[c:5]):[c:6]
null
[]
null
null
2
HOUR
Dimethylamine (33% in ethanol, 156 ml) was added to a stirred suspension of methyl 5-(bromoacetyl)-2-(phenylmethoxy)benzoate (105.8 g) in absolute ethanol (1l) and THF (1l). The resulting solution was stirred at RT for 2 h, treated with NaBH4 (25 g) and stirred at RT overnight. The solvent was removed in vacuo and H2O ...
10.6084/m9.figshare.5104873.v1
null
Primary halide.Ketone.Secondary amine
Secondary alcohol.Tertiary amine
null
null
c1ccccc1.c1ccccc1
Br-
C(C)O.C1CCOC1
null
2
CNC.COC(=O)c1cc(C(=O)CBr)ccc1OCc1ccccc1>C(C)O.C1CCOC1>COC(=O)c1cc(C(O)CN(C)C)ccc1OCc1ccccc1