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414 values
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large_stringlengths
36
36
reaction_smiles
large_stringlengths
4
873
rxn_insight_reaction
large_stringlengths
19
1.07k
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14
3.37k
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large_stringlengths
1
581
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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
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large_stringlengths
5
288
rxn_insight_template
large_stringlengths
24
2.64k
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float64
-0.8
90,205,160,000B
yield_measurements
large_stringlengths
2
864
temperature_value
float64
-230
30.1k
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large_stringclasses
3 values
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float64
0
4k
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large_stringclasses
4 values
procedure_details
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1
23.6k
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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-01dbb772c5e249108f0b191ed17a2c0c
ord-16aafcac545a4847bcf7a5fd0cf05ce5
CN1CC[C@H](O)C1.ClCCl.ClCCl.O=C(O)c1cccnc1Cl>>CN1C[C@H](CCCl)Oc2ncccc2C1=O.Cl
C(Cl)Cl.ClC1=C(C(=O)O)C=CC=N1.CN1C[C@H](CC1)O.[H-].[Na+].C1(=CC=CC=C1)P(C1=CC=CC=C1)C1=CC=CC=C1.CS(=O)(=O)O.C(Cl)Cl>>Cl.ClCC[C@@H]1OC2=C(C(N(C1)C)=O)C=CC=N2
[CH3:1][N:2]1[CH2:3][C@@H:4]([OH:8])[CH2:5][CH2:6]1.ClC[Cl:17].ClC[Cl:7].O[C:15]([c:14]1[c:9](Cl)[n:10][cH:11][cH:12][cH:13]1)=[O:16]>>[CH3:1][N:2]1[CH2:3][C@H:4]([CH2:5][CH2:6][Cl:7])[O:8][c:9]2[n:10][cH:11][cH:12][cH:13][c:14]2[C:15]1=[O:16].[ClH:17]
CN1CC[C@H](O)C1.ClCCl.ClCCl.O=C(O)c1cccnc1Cl
CN1C[C@H](CCCl)Oc2ncccc2C1=O.Cl
null
null
C(Cl)(Cl)(Cl)Cl.O1CCCC1.C(C)N(CC)CC
Acylation
OtherReaction
76bfdfbaa3a00bac267fc4db8894135b9ecdf739c038e44eea9f6d5231d11211
429fdccab5d11c54310b7d1ab555bf74ea09e30d5ff456a6396b038c56ef2638
O=C1NCCOc2ncccc21
Cl-C-[Cl;H0;D1;+0:1].Cl-C-[Cl;H0;D1;+0:2].Cl-[c;H0;D3;+0:3](:[#7;a:4]:[c:5]):[c:6](-[C;H0;D3;+0:7](-O)=[O;D1;H0:8]):[c:9].[C;D1;H3:10]-[N;H0;D3;+0:11]1-[C:12]-[C:13](-[OH;D1;+0:14])-[C:15]-[CH2;D2;+0:16]-1>>[C;D1;H3:10]-[N;H0;D3;+0:11]1-[C:12]-[C:13](-[C:15]-[CH2;D2;+0:16]-[Cl;H0;D1;+0:2])-[O;H0;D2;+0:14]-[c;H0;D3;+0:3...
null
[]
25
CELSIUS
null
null
A solution of 47.4 g (0.3 mole) of 2-chloronicotinic acid and 30 g (0.3 mole) of -(S)-1-methyl-3-pyrrolidinol in 400 ml of tetrahydrofuran was added over a period of 1 hr to a stirred suspension of 26.4 g (0.66 mole) of 60% sodium hydride)mineral oil in 500 ml of tetrahydrofuran at 50°-60° C. The mixture was stirred at...
10.6084/m9.figshare.5104873.v1
null
Aromatic halide.Primary halide.Primary halide.Primary halide.Primary halide.Carboxylic acid.Secondary alcohol.Tertiary amine
Primary halide.Ether.Tertiary amide
C1CC[NH]C1.c1ccncc1
c1cnc2c(c1)C[NH]CCO2
c1cnc2c(c1)C[NH]CCO2
HCl
C(Cl)(Cl)(Cl)Cl.O1CCCC1.C(C)N(CC)CC
25
null
CN1CC[C@H](O)C1.ClCCl.ClCCl.O=C(O)c1cccnc1Cl>C(Cl)(Cl)(Cl)Cl.O1CCCC1.C(C)N(CC)CC>CN1C[C@H](CCCl)Oc2ncccc2C1=O.Cl
ord_dataset-01dbb772c5e249108f0b191ed17a2c0c
ord-a017fe39f254422c88213d2d48dce469
CN1CC[C@@H](O)C1.ClCCl.ClCCl.O=C(O)c1cccnc1Cl>>CN1C[C@@H](CCCl)Oc2ncccc2C1=O.Cl
C(Cl)Cl.ClC1=C(C(=O)O)C=CC=N1.CN1C[C@@H](CC1)O.[H-].[Na+].C1(=CC=CC=C1)P(C1=CC=CC=C1)C1=CC=CC=C1.CS(=O)(=O)O.C(Cl)Cl>>Cl.ClCC[C@H]1OC2=C(C(N(C1)C)=O)C=CC=N2
[CH3:1][N:2]1[CH2:3][C@H:4]([OH:8])[CH2:5][CH2:6]1.ClC[Cl:17].ClC[Cl:7].O[C:15]([c:14]1[c:9](Cl)[n:10][cH:11][cH:12][cH:13]1)=[O:16]>>[CH3:1][N:2]1[CH2:3][C@@H:4]([CH2:5][CH2:6][Cl:7])[O:8][c:9]2[n:10][cH:11][cH:12][cH:13][c:14]2[C:15]1=[O:16].[ClH:17]
CN1CC[C@@H](O)C1.ClCCl.ClCCl.O=C(O)c1cccnc1Cl
CN1C[C@@H](CCCl)Oc2ncccc2C1=O.Cl
null
null
C(C)N(CC)CC.O1CCCC1.C(Cl)(Cl)(Cl)Cl
Acylation
OtherReaction
76bfdfbaa3a00bac267fc4db8894135b9ecdf739c038e44eea9f6d5231d11211
429fdccab5d11c54310b7d1ab555bf74ea09e30d5ff456a6396b038c56ef2638
O=C1NCCOc2ncccc21
Cl-C-[Cl;H0;D1;+0:1].Cl-C-[Cl;H0;D1;+0:2].Cl-[c;H0;D3;+0:3](:[#7;a:4]:[c:5]):[c:6](-[C;H0;D3;+0:7](-O)=[O;D1;H0:8]):[c:9].[C;D1;H3:10]-[N;H0;D3;+0:11]1-[C:12]-[C:13](-[OH;D1;+0:14])-[C:15]-[CH2;D2;+0:16]-1>>[C;D1;H3:10]-[N;H0;D3;+0:11]1-[C:12]-[C:13](-[C:15]-[CH2;D2;+0:16]-[Cl;H0;D1;+0:2])-[O;H0;D2;+0:14]-[c;H0;D3;+0:3...
null
[]
25
CELSIUS
null
null
A solution of 47.4 g (0.3 mole) of 2-chloronicotinic acid and 30 g (0.3 mole) of (R)-1-methyl-3-pyrrolidinol in 400 ml of tetrahydrofuran was added over a period of 1 hr to a stirred suspension of 26.4 g (0.66 mole) of 60% sodium hydride/mineral oil in 500 ml of tetrahydrofuran at 55°-60° C. The mixture was stirred at ...
10.6084/m9.figshare.5104873.v1
null
Aromatic halide.Primary halide.Primary halide.Primary halide.Primary halide.Carboxylic acid.Secondary alcohol.Tertiary amine
Primary halide.Ether.Tertiary amide
C1CC[NH]C1.c1ccncc1
c1cnc2c(c1)C[NH]CCO2
c1cnc2c(c1)C[NH]CCO2
HCl
C(C)N(CC)CC.O1CCCC1.C(Cl)(Cl)(Cl)Cl
25
null
CN1CC[C@@H](O)C1.ClCCl.ClCCl.O=C(O)c1cccnc1Cl>C(C)N(CC)CC.O1CCCC1.C(Cl)(Cl)(Cl)Cl>CN1C[C@@H](CCCl)Oc2ncccc2C1=O.Cl
ord_dataset-01dbb772c5e249108f0b191ed17a2c0c
ord-726005ffdfda42c1af28a0e408d3d24e
CN1CC(CCCl)Oc2ccc([N+](=O)[O-])cc2C1=O.S=P12SP3(=S)SP(=S)(S1)SP(=S)(S2)S3>>CN1CC(CCCl)Oc2ccc([N+](=O)[O-])cc2C1=S
P12(=S)SP3(=S)SP(=S)(S1)SP(=S)(S2)S3.ClCCC1OC2=C(C(N(C1)C)=O)C=C(C=C2)[N+](=O)[O-].P12(=S)SP3(=S)SP(=S)(S1)SP(=S)(S2)S3>>ClCCC1OC2=C(C(N(C1)C)=S)C=C(C=C2)[N+](=O)[O-]
O=[C:18]1[N:2]([CH3:1])[CH2:3][CH:4]([CH2:5][CH2:6][Cl:7])[O:8][c:9]2[cH:10][cH:11][c:12]([N+:13](=[O:14])[O-:15])[cH:16][c:17]21.S=P12SP3(=S)SP(=S)(S1)SP(=[S:19])(S2)S3>>[CH3:1][N:2]1[CH2:3][CH:4]([CH2:5][CH2:6][Cl:7])[O:8][c:9]2[cH:10][cH:11][c:12]([N+:13](=[O:14])[O-:15])[cH:16][c:17]2[C:18]1=[S:19]
CN1CC(CCCl)Oc2ccc([N+](=O)[O-])cc2C1=O.S=P12SP3(=S)SP(=S)(S1)SP(=S)(S2)S3
CN1CC(CCCl)Oc2ccc([N+](=O)[O-])cc2C1=S
null
null
C(C)#N.C1(=CC=CC=C1)C
Heteroatom Alkylation and Arylation
OtherReaction
43ac2affde81267970c96bfb182f28e85d876733ab6e6103821469d8ecc8ebf9
92373f703706fcd3b2fa077124e423e859506b3bebedf9bbb6de44eb68d5c891
S=C1NCCOc2ccccc21
O=[C;H0;D3;+0:1](-[#7:2](-[C;D1;H3:3])-[C:4])-[c:5](:[c:6]):[c:7]-[#8:8].S=P12-S-P3(=S)-S-P(=S)(-S-1)-S-P(=[S;H0;D1;+0:9])(-S-2)-S-3>>[#8:8]-[c:7]:[c:5](:[c:6])-[C;H0;D3;+0:1](=[S;H0;D1;+0:9])-[#7:2](-[C;D1;H3:3])-[C:4]
173.5
[{"value": 57.0, "product": "ClCCC1OC2=C(C(N(C1)C)=S)C=C(C=C2)[N+](=O)[O-]", "details": "PERCENTYIELD", "is_desired": false}, {"value": 173.5, "product": "ClCCC1OC2=C(C(N(C1)C)=S)C=C(C=C2)[N+](=O)[O-]", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
2
HOUR
To 2.0 g (0.007 mole) of 2-(2-chloroethyl)-2,3-dihydro-4-methyl-7-nitro-1,4-benzoxazepin-5(4H)-one in 35 ml of acetonitrile was added 1.0 g (0.0023 mole) of phosphorus pentasulfide and the mixture heated to reflux for 2 hr. Another 0.4 g (0.001 mole) of phosphorus pentasulfide was added and heating continued for 2 hr. ...
10.6084/m9.figshare.5104873.v1
null
Tertiary amide.Monosulfide.Monosulfide.Monosulfide.Monosulfide.Monosulfide.Monosulfide
Thioamide
c1ccc2c(c1)C[NH]CCO2.S1P2SP3SP1SP(S2)S3
c1ccc2c(c1)C[NH]CCO2
c1ccc2c(c1)C[NH]CCO2
Other
C(C)#N.C1(=CC=CC=C1)C
null
2
CN1CC(CCCl)Oc2ccc([N+](=O)[O-])cc2C1=O.S=P12SP3(=S)SP(=S)(S1)SP(=S)(S2)S3>C(C)#N.C1(=CC=CC=C1)C>CN1CC(CCCl)Oc2ccc([N+](=O)[O-])cc2C1=S
ord_dataset-01dbb772c5e249108f0b191ed17a2c0c
ord-76a12ce959eb4171b4a538b09030f1f9
CN1CC(CCCl)Oc2ccc(F)cc2C1=O.S=P12SP3(=S)SP(=S)(S1)SP(=S)(S2)S3>>CN1CC(CCCl)Oc2ccc(F)cc2C1=S
P12(=S)SP3(=S)SP(=S)(S1)SP(=S)(S2)S3.ClCCC1OC2=C(C(N(C1)C)=O)C=C(C=C2)F.P12(=S)SP3(=S)SP(=S)(S1)SP(=S)(S2)S3>>ClCCC1OC2=C(C(N(C1)C)=S)C=C(C=C2)F
O=[C:16]1[N:2]([CH3:1])[CH2:3][CH:4]([CH2:5][CH2:6][Cl:7])[O:8][c:9]2[cH:10][cH:11][c:12]([F:13])[cH:14][c:15]21.S=P12SP3(=S)SP(=S)(S1)SP(=[S:17])(S2)S3>>[CH3:1][N:2]1[CH2:3][CH:4]([CH2:5][CH2:6][Cl:7])[O:8][c:9]2[cH:10][cH:11][c:12]([F:13])[cH:14][c:15]2[C:16]1=[S:17]
CN1CC(CCCl)Oc2ccc(F)cc2C1=O.S=P12SP3(=S)SP(=S)(S1)SP(=S)(S2)S3
CN1CC(CCCl)Oc2ccc(F)cc2C1=S
null
null
C(C)#N.C1(=CC=CC=C1)C
Heteroatom Alkylation and Arylation
OtherReaction
43ac2affde81267970c96bfb182f28e85d876733ab6e6103821469d8ecc8ebf9
92373f703706fcd3b2fa077124e423e859506b3bebedf9bbb6de44eb68d5c891
S=C1NCCOc2ccccc21
O=[C;H0;D3;+0:1](-[#7:2](-[C;D1;H3:3])-[C:4])-[c:5](:[c:6]):[c:7]-[#8:8].S=P12-S-P3(=S)-S-P(=S)(-S-1)-S-P(=[S;H0;D1;+0:9])(-S-2)-S-3>>[#8:8]-[c:7]:[c:5](:[c:6])-[C;H0;D3;+0:1](=[S;H0;D1;+0:9])-[#7:2](-[C;D1;H3:3])-[C:4]
125.6
[{"value": 52.0, "product": "ClCCC1OC2=C(C(N(C1)C)=S)C=C(C=C2)F", "details": "PERCENTYIELD", "is_desired": false}, {"value": 125.6, "product": "ClCCC1OC2=C(C(N(C1)C)=S)C=C(C=C2)F", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
2
HOUR
To 1.0 g (0.0039 mole) of 2-(2-chloroethyl)-2,3-dihydro-7-fluoro-4-methyl-1,4-benzoxazepin-5(4H)-one in 30 ml of acetonitrile was added 0.7 g (0.0016 mole) of phosphorus pentasulfide and the reaction mixture heated to reflux. After 2 hr, another 0.4 g (0.009 mole) of phosphorus pentasulfide was added and heating contin...
10.6084/m9.figshare.5104873.v1
null
Tertiary amide.Monosulfide.Monosulfide.Monosulfide.Monosulfide.Monosulfide.Monosulfide
Thioamide
c1ccc2c(c1)C[NH]CCO2.S1P2SP3SP1SP(S2)S3
c1ccc2c(c1)C[NH]CCO2
c1ccc2c(c1)C[NH]CCO2
Other
C(C)#N.C1(=CC=CC=C1)C
null
2
CN1CC(CCCl)Oc2ccc(F)cc2C1=O.S=P12SP3(=S)SP(=S)(S1)SP(=S)(S2)S3>C(C)#N.C1(=CC=CC=C1)C>CN1CC(CCCl)Oc2ccc(F)cc2C1=S
ord_dataset-01dbb772c5e249108f0b191ed17a2c0c
ord-66c07ea6a9ef4116951cdf9662a6bd01
CN1CC(CCCl)Oc2ccccc2C1=O.CNC>>CN(C)CCC1CN(C)C(=O)c2ccccc2O1.Cl
CNC.ClCCC1OC2=C(C(N(C1)C)=O)C=CC=C2>>Cl.CN(CCC1OC2=C(C(N(C1)C)=O)C=CC=C2)C
[CH2:4]([CH2:5][CH:6]1[CH2:7][N:8]([CH3:9])[C:10](=[O:11])[c:12]2[cH:13][cH:14][cH:15][cH:16][c:17]2[O:18]1)[Cl:19].[CH3:1][NH:2][CH3:3]>>[CH3:1][N:2]([CH3:3])[CH2:4][CH2:5][CH:6]1[CH2:7][N:8]([CH3:9])[C:10](=[O:11])[c:12]2[cH:13][cH:14][cH:15][cH:16][c:17]2[O:18]1.[ClH:19]
CN1CC(CCCl)Oc2ccccc2C1=O.CNC
CN(C)CCC1CN(C)C(=O)c2ccccc2O1.Cl
null
null
C(C)O
Heteroatom Alkylation and Arylation
N-alkylation of secondary amines with alkyl halides
6d58cac08ccced0a33ed16fbca180bc12aa011288d6476106d98a7b2cbc3d709
523d37155b42c8dc851abeddadebb241cdd90bdf649ba750c35e13c8c752d7b0
O=C1NCCOc2ccccc21
[#8:1]-[C:2]-[C:3]-[CH2;D2;+0:4]-[Cl;H0;D1;+0:5].[C;D1;H3:6]-[NH;D2;+0:7]-[C;D1;H3:8]>>[#8:1]-[C:2]-[C:3]-[CH2;D2;+0:4]-[N;H0;D3;+0:7](-[C;D1;H3:6])-[C;D1;H3:8].[ClH;D0;+0:5]
null
[]
100
CELSIUS
null
null
A solution of 9 g (0.2 mole) of dimethylamine in 250 ml of ethanol was added to 24 g (0.1 mole) of 2-(2-chloroethyl)-2,3-dihydro-4-methyl-1,4-benzoxazepin-5(4H)one in a steel bomb. The mixture was heated at 100° C. for 18 hrs. The solution was concentrated in vacuo and the residue partitioned between ethyl acetate and ...
10.6084/m9.figshare.5104873.v1
null
Primary halide.Secondary amine
Tertiary amine
null
null
c1ccc2c(c1)C[NH]CCO2
null
C(C)O
100
null
CN1CC(CCCl)Oc2ccccc2C1=O.CNC>C(C)O>CN(C)CCC1CN(C)C(=O)c2ccccc2O1.Cl
ord_dataset-01dbb772c5e249108f0b191ed17a2c0c
ord-c7bfc234f1744f32ad7ffb0232bfef78
CNC.O=C1c2ccccc2OC(CCCl)CN1Cc1ccccc1>>CN(C)CCC1CN(Cc2ccccc2)C(=O)c2ccccc2O1.O
C(C1=CC=CC=C1)N1CC(OC2=C(C1=O)C=CC=C2)CCCl.CNC>>O.C(C1=CC=CC=C1)N1CC(OC2=C(C1=O)C=CC=C2)CCN(C)C
[CH3:1][NH:2][CH3:3].Cl[CH2:4][CH2:5][CH:6]1[CH2:7][N:8]([CH2:9][c:10]2[cH:11][cH:12][cH:13][cH:14][cH:15]2)[C:16](=[O:17])[c:18]2[cH:19][cH:20][cH:21][cH:22][c:23]2[O:24]1>>[CH3:1][N:2]([CH3:3])[CH2:4][CH2:5][CH:6]1[CH2:7][N:8]([CH2:9][c:10]2[cH:11][cH:12][cH:13][cH:14][cH:15]2)[C:16](=[O:17])[c:18]2[cH:19][cH:20][cH:...
CNC.O=C1c2ccccc2OC(CCCl)CN1Cc1ccccc1
CN(C)CCC1CN(Cc2ccccc2)C(=O)c2ccccc2O1.O
null
null
null
Functional Group Interconversion
N-alkylation of secondary amines with alkyl halides
105ac0dfe253fa64bb23e18afb1853920a6845d3c91bcb98534155cafd8aaf01
da87afc172ebd302d462893afe878066c210a24130312f3acba00f6d41a889fd
O=C1c2ccccc2OCCN1Cc1ccccc1
Cl-[CH2;D2;+0:1]-[C:2]-[C:3]-[#8:4].[C;D1;H3:5]-[NH;D2;+0:6]-[C;D1;H3:7]>>[#8:4]-[C:3]-[C:2]-[CH2;D2;+0:1]-[N;H0;D3;+0:6](-[C;D1;H3:5])-[C;D1;H3:7]
null
[]
null
null
null
null
Following the procedure of Example 1, 4-benzyl-2-(2-chloroethyl)-2,3-dihydro-1,4-benzoxazepin-5(4H)-one and dimethylamine were reacted and the free base of the title compound was obtained in the concentrated residue. Recrystallization from ethanol-water gave the product, m.p. 75°-77° C. Conditions: See reaction.notes.p...
10.6084/m9.figshare.5104873.v1
null
Primary halide.Secondary amine
Tertiary amine
null
null
c1ccccc1.c1ccc2c(c1)C[NH]CCO2
null
null
null
null
CNC.O=C1c2ccccc2OC(CCCl)CN1Cc1ccccc1>>CN(C)CCC1CN(Cc2ccccc2)C(=O)c2ccccc2O1.O
ord_dataset-01dbb772c5e249108f0b191ed17a2c0c
ord-b3d03018265147f9b16a7114a4128529
CN1CC(CCCl)Oc2ncccc2C1=S.CNC>>CN(C)CCC1CN(C)C(=S)c2cccnc2O1
C(\C=C\C(=O)O)(=O)O.CNC.C(C)O.ClCCC1OC2=C(C(N(C1)C)=S)C=CC=N2>>C(\C=C\C(=O)O)(=O)O.CN(CCC1OC2=C(C(N(C1)C)=S)C=CC=N2)C
Cl[CH2:4][CH2:5][CH:6]1[CH2:7][N:8]([CH3:9])[C:10](=[S:11])[c:12]2[cH:13][cH:14][cH:15][n:16][c:17]2[O:18]1.[CH3:1][NH:2][CH3:3]>>[CH3:1][N:2]([CH3:3])[CH2:4][CH2:5][CH:6]1[CH2:7][N:8]([CH3:9])[C:10](=[S:11])[c:12]2[cH:13][cH:14][cH:15][n:16][c:17]2[O:18]1
CN1CC(CCCl)Oc2ncccc2C1=S.CNC
CN(C)CCC1CN(C)C(=S)c2cccnc2O1
null
null
C(C)(C)O.CO.C(Cl)Cl
Heteroatom Alkylation and Arylation
N-alkylation of secondary amines with alkyl halides
6d58cac08ccced0a33ed16fbca180bc12aa011288d6476106d98a7b2cbc3d709
523d37155b42c8dc851abeddadebb241cdd90bdf649ba750c35e13c8c752d7b0
S=C1NCCOc2ncccc21
Cl-[CH2;D2;+0:1]-[C:2]-[C:3]-[#8:4].[C;D1;H3:5]-[NH;D2;+0:6]-[C;D1;H3:7]>>[#8:4]-[C:3]-[C:2]-[CH2;D2;+0:1]-[N;H0;D3;+0:6](-[C;D1;H3:5])-[C;D1;H3:7]
null
[]
100
CELSIUS
null
null
To a solution of 113 ml (1.0 mole) of 40% aqueous dimethylamine and 326 ml of ethanol in a steel bomb was added 48.4 g (0.189 mole) of 2-(2-chloroethyl)-2,3-dihydro-4-methylpyrido[3,2-f][1,4]-oxazepine-5(4H)-thione. The mixture was heated at 100° C. for 14 hr. The ethanol was removed in a rotary evaporator leaving some...
10.6084/m9.figshare.5104873.v1
null
Primary halide.Secondary amine
Tertiary amine
null
null
c1cnc2c(c1)C[NH]CCO2
HCl
C(C)(C)O.CO.C(Cl)Cl
100
null
CN1CC(CCCl)Oc2ncccc2C1=S.CNC>C(C)(C)O.CO.C(Cl)Cl>CN(C)CCC1CN(C)C(=S)c2cccnc2O1
ord_dataset-01dbb772c5e249108f0b191ed17a2c0c
ord-7f21215b778f48b0850df62ea6fcc93a
CN1CC(CCCl)Oc2cc(Cl)ccc2C1=S.CNC>>CN(C)CCC1CN(C)C(=S)c2ccc(Cl)cc2O1.Cl
ClC1=CC2=C(C(N(CC(O2)CCCl)C)=S)C=C1.CNC>>Cl.ClC1=CC2=C(C(N(CC(O2)CCN(C)C)C)=S)C=C1
[CH2:4]([CH2:5][CH:6]1[CH2:7][N:8]([CH3:9])[C:10](=[S:11])[c:12]2[cH:13][cH:14][c:15]([Cl:16])[cH:17][c:18]2[O:19]1)[Cl:20].[CH3:1][NH:2][CH3:3]>>[CH3:1][N:2]([CH3:3])[CH2:4][CH2:5][CH:6]1[CH2:7][N:8]([CH3:9])[C:10](=[S:11])[c:12]2[cH:13][cH:14][c:15]([Cl:16])[cH:17][c:18]2[O:19]1.[ClH:20]
CN1CC(CCCl)Oc2cc(Cl)ccc2C1=S.CNC
CN(C)CCC1CN(C)C(=S)c2ccc(Cl)cc2O1.Cl
null
null
C(C)O.Cl
Heteroatom Alkylation and Arylation
N-alkylation of secondary amines with alkyl halides
6d58cac08ccced0a33ed16fbca180bc12aa011288d6476106d98a7b2cbc3d709
523d37155b42c8dc851abeddadebb241cdd90bdf649ba750c35e13c8c752d7b0
S=C1NCCOc2ccccc21
[#8:1]-[C:2]-[C:3]-[CH2;D2;+0:4]-[Cl;H0;D1;+0:5].[C;D1;H3:6]-[NH;D2;+0:7]-[C;D1;H3:8]>>[#8:1]-[C:2]-[C:3]-[CH2;D2;+0:4]-[N;H0;D3;+0:7](-[C;D1;H3:6])-[C;D1;H3:8].[ClH;D0;+0:5]
null
[]
null
null
null
null
A solution of 9.8 g (0.04 mole) of 8-chloro-2-(2-chloroethyl)-2,3-dihydro-4-methyl-1,4-benzoxazepine-5 (4H)-thione in 50 ml of absolute ethanol and 10 ml of a 40% aqueous solution of dimethylamine were mixed and heated in a steel bomb at 100° C. for 16 hr. The ethanol was evaporated under reduced pressure and the resid...
10.6084/m9.figshare.5104873.v1
null
Primary halide.Secondary amine
Tertiary amine
null
null
c1ccc2c(c1)C[NH]CCO2
null
C(C)O.Cl
null
null
CN1CC(CCCl)Oc2cc(Cl)ccc2C1=S.CNC>C(C)O.Cl>CN(C)CCC1CN(C)C(=S)c2ccc(Cl)cc2O1.Cl
ord_dataset-01dbb772c5e249108f0b191ed17a2c0c
ord-9d16c145823b4fd287c4a6545f748c2d
CN1CC(CCCl)Oc2cnccc2C1=S.CNC>>CN(C)CCC1CN(C)C(=S)c2ccncc2O1.Cl
ClCCC1OC2=C(C(N(C1)C)=S)C=CN=C2.CNC>>Cl.CN(CCC1OC2=C(C(N(C1)C)=S)C=CN=C2)C
[CH2:4]([CH2:5][CH:6]1[CH2:7][N:8]([CH3:9])[C:10](=[S:11])[c:12]2[cH:13][cH:14][n:15][cH:16][c:17]2[O:18]1)[Cl:19].[CH3:1][NH:2][CH3:3]>>[CH3:1][N:2]([CH3:3])[CH2:4][CH2:5][CH:6]1[CH2:7][N:8]([CH3:9])[C:10](=[S:11])[c:12]2[cH:13][cH:14][n:15][cH:16][c:17]2[O:18]1.[ClH:19]
CN1CC(CCCl)Oc2cnccc2C1=S.CNC
CN(C)CCC1CN(C)C(=S)c2ccncc2O1.Cl
null
null
C(C)O
Heteroatom Alkylation and Arylation
N-alkylation of secondary amines with alkyl halides
6d58cac08ccced0a33ed16fbca180bc12aa011288d6476106d98a7b2cbc3d709
523d37155b42c8dc851abeddadebb241cdd90bdf649ba750c35e13c8c752d7b0
S=C1NCCOc2cnccc21
[#8:1]-[C:2]-[C:3]-[CH2;D2;+0:4]-[Cl;H0;D1;+0:5].[C;D1;H3:6]-[NH;D2;+0:7]-[C;D1;H3:8]>>[#8:1]-[C:2]-[C:3]-[CH2;D2;+0:4]-[N;H0;D3;+0:7](-[C;D1;H3:6])-[C;D1;H3:8].[ClH;D0;+0:5]
null
[]
null
null
null
null
To a solution of 0.5 g (0.002 mole) of 2-(2-chloroethyl)-2,3-dihydro-4-methylpyrido[4,3-f][1,4]-oxazepine-5(4H)-thione in 20 ml of ethyl alcohol was added 2 ml of 40% aqueous dimethylamine. The mixture was heated in a steel bomb to 100° C. for 14 hr. The resulting solution was filtered and concentrated. The residue was...
10.6084/m9.figshare.5104873.v1
null
Primary halide.Secondary amine
Tertiary amine
null
null
c1cc2c(cn1)OCC[NH]C2
null
C(C)O
null
null
CN1CC(CCCl)Oc2cnccc2C1=S.CNC>C(C)O>CN(C)CCC1CN(C)C(=S)c2ccncc2O1.Cl
ord_dataset-01dbb772c5e249108f0b191ed17a2c0c
ord-020326b1e4574d44986493bf5d683e46
CCNCC.CN1CC(CCCl)Oc2ncccc2C1=S>>CCN(CC)CCC1CN(C)C(=S)c2cccnc2O1
ClCCC1OC2=C(C(N(C1)C)=S)C=CC=N2.C(C)NCC>>C(C)N(CCC1OC2=C(C(N(C1)C)=S)C=CC=N2)CC
[CH3:1][CH2:2][NH:3][CH2:4][CH3:5].Cl[CH2:6][CH2:7][CH:8]1[CH2:9][N:10]([CH3:11])[C:12](=[S:13])[c:14]2[cH:15][cH:16][cH:17][n:18][c:19]2[O:20]1>>[CH3:1][CH2:2][N:3]([CH2:4][CH3:5])[CH2:6][CH2:7][CH:8]1[CH2:9][N:10]([CH3:11])[C:12](=[S:13])[c:14]2[cH:15][cH:16][cH:17][n:18][c:19]2[O:20]1
CCNCC.CN1CC(CCCl)Oc2ncccc2C1=S
CCN(CC)CCC1CN(C)C(=S)c2cccnc2O1
null
null
C(C)O
Heteroatom Alkylation and Arylation
N-alkylation of secondary amines with alkyl halides
6d58cac08ccced0a33ed16fbca180bc12aa011288d6476106d98a7b2cbc3d709
523d37155b42c8dc851abeddadebb241cdd90bdf649ba750c35e13c8c752d7b0
S=C1NCCOc2ncccc21
Cl-[CH2;D2;+0:1]-[C:2]-[C:3]-[#8:4].[C;D1;H3:5]-[C:6]-[NH;D2;+0:7]-[C:8]-[C;D1;H3:9]>>[#8:4]-[C:3]-[C:2]-[CH2;D2;+0:1]-[N;H0;D3;+0:7](-[C:6]-[C;D1;H3:5])-[C:8]-[C;D1;H3:9]
null
[]
null
null
null
null
2-(2-Chloroethyl)-2,3-dihydro-4-methylpyrido[3,2-f][1,4]-oxazepine-5(4H)-thione and diethylamine in ethanol are heated together to obtain the title compound. Conditions: See reaction.notes.procedure_details.
10.6084/m9.figshare.5104873.v1
null
Primary halide.Secondary amine
Tertiary amine
null
null
c1cnc2c(c1)C[NH]CCO2
HCl
C(C)O
null
null
CCNCC.CN1CC(CCCl)Oc2ncccc2C1=S>C(C)O>CCN(CC)CCC1CN(C)C(=S)c2cccnc2O1
ord_dataset-01dbb772c5e249108f0b191ed17a2c0c
ord-f2ced41ca80546fca5cc841a48e387ac
CN1CC(CCCl)Oc2ncccc2C1=O.CN1CC(CCl)Oc2ncccc2C1=O>>CN(C)CC1CN(C)C(=O)c2cccnc2O1
ClCC1OC2=C(C(N(C1)C)=O)C=CC=N2.ClCCC1OC2=C(C(N(C1)C)=O)C=CC=N2>>CN(C)CC1OC2=C(C(N(C1)C)=O)C=CC=N2
O=C1c2cccnc2OC(CCCl)[CH2:3][N:2]1[CH3:1].Cl[CH2:4][CH:5]1[CH2:6][N:7]([CH3:8])[C:9](=[O:10])[c:11]2[cH:12][cH:13][cH:14][n:15][c:16]2[O:17]1>>[CH3:1][N:2]([CH3:3])[CH2:4][CH:5]1[CH2:6][N:7]([CH3:8])[C:9](=[O:10])[c:11]2[cH:12][cH:13][cH:14][n:15][c:16]2[O:17]1
CN1CC(CCCl)Oc2ncccc2C1=O.CN1CC(CCl)Oc2ncccc2C1=O
CN(C)CC1CN(C)C(=O)c2cccnc2O1
null
null
null
Heteroatom Alkylation and Arylation
OtherReaction
cd18b0a1e34b5b148dbc523996cb1c11099777687f255297257557cddce67f0d
c3a337737fb112f6285f5fdfb311f31e44f8146f395929a52385b50ebe89346f
O=C1NCCOc2ncccc21
Cl-C-C-C1-O-c2:n:c:c:c:c:2-C(=O)-[N;H0;D3;+0:1](-[C;D1;H3:2])-[CH2;D2;+0:3]-1.Cl-[CH2;D2;+0:4]-[C:5](-[#8:6]-[c:7]:[#7;a:8])-[C:9]-[#7:10]>>[#7:10]-[C:9]-[C:5](-[CH2;D2;+0:4]-[N;H0;D3;+0:1](-[C;D1;H3:2])-[CH3;D1;+0:3])-[#8:6]-[c:7]:[#7;a:8]
null
[]
null
null
null
null
When in the procedure of Example 10, 2-chloromethyl-2,3-dihydro-4-methylpyrido[3,2-f][1,4]-oxazepin-5(4H)-one is substituted for 2-(2-chloroethyl)-2,3-dihydro-4-methylpyrido[3,2-f][1,4]-oxazepin-5(4H)-one, the title compound is prepared and is isolated if desired as a pharmaceutically acceptable salt. Conditions: See r...
10.6084/m9.figshare.5104873.v1
null
Primary halide.Primary halide.Ether.Tertiary amide
Tertiary amine
c1cnc2c(c1)C[NH]CCO2
null
c1cnc2c(c1)C[NH]CCO2
HCl
null
null
null
CN1CC(CCCl)Oc2ncccc2C1=O.CN1CC(CCl)Oc2ncccc2C1=O>>CN(C)CC1CN(C)C(=O)c2cccnc2O1
ord_dataset-01dbb772c5e249108f0b191ed17a2c0c
ord-2a5b54123d374a7f86084eaea7b0e18e
CN1CC(CCCl)Oc2c(ccc3ccccc23)C1=S.CNC>>CN(C)CCC1CN(C)C(=S)c2ccc3ccccc3c2O1.Cl
ClCCC1OC2=C(C(N(C1)C)=S)C=CC1=CC=CC=C12.CNC>>Cl.CN(CCC1OC2=C(C(N(C1)C)=S)C=CC1=CC=CC=C12)C
[CH2:4]([CH2:5][CH:6]1[CH2:7][N:8]([CH3:9])[C:10](=[S:11])[c:12]2[cH:13][cH:14][c:15]3[cH:16][cH:17][cH:18][cH:19][c:20]3[c:21]2[O:22]1)[Cl:23].[CH3:1][NH:2][CH3:3]>>[CH3:1][N:2]([CH3:3])[CH2:4][CH2:5][CH:6]1[CH2:7][N:8]([CH3:9])[C:10](=[S:11])[c:12]2[cH:13][cH:14][c:15]3[cH:16][cH:17][cH:18][cH:19][c:20]3[c:21]2[O:22]...
CN1CC(CCCl)Oc2c(ccc3ccccc23)C1=S.CNC
CN(C)CCC1CN(C)C(=S)c2ccc3ccccc3c2O1.Cl
null
null
C(C)O
Heteroatom Alkylation and Arylation
N-alkylation of secondary amines with alkyl halides
6d58cac08ccced0a33ed16fbca180bc12aa011288d6476106d98a7b2cbc3d709
523d37155b42c8dc851abeddadebb241cdd90bdf649ba750c35e13c8c752d7b0
S=C1NCCOc2c1ccc1ccccc21
[#8:1]-[C:2]-[C:3]-[CH2;D2;+0:4]-[Cl;H0;D1;+0:5].[C;D1;H3:6]-[NH;D2;+0:7]-[C;D1;H3:8]>>[#8:1]-[C:2]-[C:3]-[CH2;D2;+0:4]-[N;H0;D3;+0:7](-[C;D1;H3:6])-[C;D1;H3:8].[ClH;D0;+0:5]
20
[{"value": 20.0, "product": "Cl.CN(CCC1OC2=C(C(N(C1)C)=S)C=CC1=CC=CC=C12)C", "details": "PERCENTYIELD", "is_desired": false}]
null
null
null
null
To a solution of 15.0 g (0.05 mole) of 2-(2-chloroethyl)-2,3-dihydro-4-methylnaphth[2,1-f][1,4]-oxazepine-5(4H)-thione in 50 ml of absolute ethanol was added 10 g of a 40% aqueous solution of dimethylamine. The resulting solution was heated in a steel bomb at 100° C. for 40 hr and concentrated under reduced pressure. T...
10.6084/m9.figshare.5104873.v1
null
Primary halide.Secondary amine
Tertiary amine
null
null
c1ccc2c3c(ccc2c1)C[NH]CCO3
null
C(C)O
null
null
CN1CC(CCCl)Oc2c(ccc3ccccc23)C1=S.CNC>C(C)O>CN(C)CCC1CN(C)C(=S)c2ccc3ccccc3c2O1.Cl
ord_dataset-01dbb772c5e249108f0b191ed17a2c0c
ord-899dfc4eb3d343fca6a7503b6a131990
CN1CC(CCCl)Sc2ncccc2C1=O.CNC>>CN(C)CCC1CN(C)C(=O)c2cccnc2S1.Cl.Cl
CNC.ClCCC1SC2=C(C(N(C1)C)=O)C=CC=N2.CNC>>Cl.Cl.CN(CCC1SC2=C(C(N(C1)C)=O)C=CC=N2)C
[CH2:4]([CH2:5][CH:6]1[CH2:7][N:8]([CH3:9])[C:10](=[O:11])[c:12]2[cH:13][cH:14][cH:15][n:16][c:17]2[S:18]1)[Cl:19].[CH3:1][NH:2][CH3:3]>>[CH3:1][N:2]([CH3:3])[CH2:4][CH2:5][CH:6]1[CH2:7][N:8]([CH3:9])[C:10](=[O:11])[c:12]2[cH:13][cH:14][cH:15][n:16][c:17]2[S:18]1.[ClH:19].[ClH:20]
CN1CC(CCCl)Sc2ncccc2C1=O.CNC
CN(C)CCC1CN(C)C(=O)c2cccnc2S1.Cl.Cl
null
null
null
Functional Group Addition
N-alkylation of secondary amines with alkyl halides
6dc67fdaa84d3f88aea31bd6d36481dd1f7dd6caece2acc0ef2660765ea75733
44df6a34ed503be8d571d8a086699e2116e82b962d53e34ea90b7759e699f35c
O=C1NCCSc2ncccc21
[#16:1]-[C:2]-[C:3]-[CH2;D2;+0:4]-[Cl;H0;D1;+0:5].[C;D1;H3:6]-[NH;D2;+0:7]-[C;D1;H3:8]>>[#16:1]-[C:2]-[C:3]-[CH2;D2;+0:4]-[N;H0;D3;+0:7](-[C;D1;H3:6])-[C;D1;H3:8].[ClH;D0;+0:5]
null
[]
null
null
null
null
A solution of 1.5 g (0.0058 mole) of 2-(2-chloroethyl)-2,3-dihydro-4-methylpyrido[3,2-f][1,4]-thiazepin-5(4H)-one in 20 ml of dimethylamine was stirred at 25° C. in a sealed container for 72 hr. The excess dimethylamine was allowed to evaporate and the residue was partitioned between chloroform and dilute sodium hydrox...
10.6084/m9.figshare.5104873.v1
null
Primary halide.Secondary amine
Tertiary amine
null
null
c1cnc2c(c1)C[NH]CCS2
Other
null
null
null
CN1CC(CCCl)Sc2ncccc2C1=O.CNC>>CN(C)CCC1CN(C)C(=O)c2cccnc2S1.Cl.Cl
ord_dataset-01dbb772c5e249108f0b191ed17a2c0c
ord-86d68c4097fe4b1490aca906d3daf585
C1COCCN1.CN1CC(CCCl)Oc2ncccc2C1=O>>CN1CC(CCN2CCOCC2)Oc2ncccc2C1=O
C(C)(C)O.C(\C=C/C(=O)O)(=O)O.Cl.ClCCC1OC2=C(C(N(C1)C)=O)C=CC=N2.N1CCOCC1.[OH-].[Na+]>>C(\C=C/C(=O)O)(=O)O.CN1CC(OC2=C(C1=O)C=CC=N2)CCN2CCOCC2
[NH:7]1[CH2:8][CH2:9][O:10][CH2:11][CH2:12]1.Cl[CH2:6][CH2:5][CH:4]1[CH2:3][N:2]([CH3:1])[C:20](=[O:21])[c:19]2[c:14]([n:15][cH:16][cH:17][cH:18]2)[O:13]1>>[CH3:1][N:2]1[CH2:3][CH:4]([CH2:5][CH2:6][N:7]2[CH2:8][CH2:9][O:10][CH2:11][CH2:12]2)[O:13][c:14]2[n:15][cH:16][cH:17][cH:18][c:19]2[C:20]1=[O:21]
C1COCCN1.CN1CC(CCCl)Oc2ncccc2C1=O
CN1CC(CCN2CCOCC2)Oc2ncccc2C1=O
null
null
null
Heteroatom Alkylation and Arylation
N-alkylation of secondary amines with alkyl halides
2bad30dcdb0a20edb8ce877f072b133eedfd870621da393ec393128bfee00977
523d37155b42c8dc851abeddadebb241cdd90bdf649ba750c35e13c8c752d7b0
O=C1NCC(CCN2CCOCC2)Oc2ncccc21
Cl-[CH2;D2;+0:1]-[C:2]-[C:3]-[#8:4].[#8:5]1-[C:6]-[C:7]-[NH;D2;+0:8]-[C:9]-[C:10]-1>>[#8:4]-[C:3]-[C:2]-[CH2;D2;+0:1]-[N;H0;D3;+0:8]1-[C:7]-[C:6]-[#8:5]-[C:10]-[C:9]-1
null
[]
null
null
8
HOUR
2-(2-Chloroethyl)-2,3-dihydro-4-methylpyrido[3,2-f][1,4]oxazepin-5(4H)-one hydrochloride, 16 g (058 mole) was dissolved in morpholine (30 mL) and stirred overnight at room temperature. To the solution was added dilute sodium hydroxide solution (50 ml) and the resulting mixture extracted with chloroform (3×30 ml). The c...
10.6084/m9.figshare.5104873.v1
null
Primary halide.Secondary amine
Tertiary amine
C1COCCN1
C1COCC[NH]1
C1COCC[NH]1.c1cnc2c(c1)C[NH]CCO2
HCl
null
null
8
C1COCCN1.CN1CC(CCCl)Oc2ncccc2C1=O>>CN1CC(CCN2CCOCC2)Oc2ncccc2C1=O
ord_dataset-01dbb772c5e249108f0b191ed17a2c0c
ord-7df9808670ba4f2b81ba407bc9a2e80e
C1CCNC1.CN1CC(CCCl)Oc2ncccc2C1=O>>CN1CC(CCN2CCCC2)Oc2ncccc2C1=O
Cl.ClCCC1OC2=C(C(N(C1)C)=O)C=CC=N2.N1CCCC1.[OH-].[Na+].C(\C=C\C(=O)O)(=O)O>>C(\C=C\C(=O)O)(=O)O.CN1CC(OC2=C(C1=O)C=CC=N2)CCN2CCCC2
[NH:7]1[CH2:8][CH2:9][CH2:10][CH2:11]1.Cl[CH2:6][CH2:5][CH:4]1[CH2:3][N:2]([CH3:1])[C:19](=[O:20])[c:18]2[c:13]([n:14][cH:15][cH:16][cH:17]2)[O:12]1>>[CH3:1][N:2]1[CH2:3][CH:4]([CH2:5][CH2:6][N:7]2[CH2:8][CH2:9][CH2:10][CH2:11]2)[O:12][c:13]2[n:14][cH:15][cH:16][cH:17][c:18]2[C:19]1=[O:20]
C1CCNC1.CN1CC(CCCl)Oc2ncccc2C1=O
CN1CC(CCN2CCCC2)Oc2ncccc2C1=O
null
null
null
Heteroatom Alkylation and Arylation
N-alkylation of secondary amines with alkyl halides
19b442dc26882f89f7423416f5e0a16bdb8e48776df57991434a0634e21f0505
523d37155b42c8dc851abeddadebb241cdd90bdf649ba750c35e13c8c752d7b0
O=C1NCC(CCN2CCCC2)Oc2ncccc21
Cl-[CH2;D2;+0:1]-[C:2]-[C:3]-[#8:4].[C:5]1-[C:6]-[NH;D2;+0:7]-[C:8]-[C:9]-1>>[#8:4]-[C:3]-[C:2]-[CH2;D2;+0:1]-[N;H0;D3;+0:7]1-[C:6]-[C:5]-[C:9]-[C:8]-1
null
[]
80
CELSIUS
null
null
A sample of 2-(2-chloroethyl)-2,3-dihydro-4-methylpyrido[3,2-f][1,4]-oxazepine-5(4H)-one hydrochloride, 16 g (0.058 mole), was dissolved in 65 ml of pyrrolidine. The stirred solution was heated to 80° C. for 3 hr. The solution was cooled to room temperature and dilute sodium hydroxide solution (50 ml) was added. The re...
10.6084/m9.figshare.5104873.v1
null
Primary halide.Secondary amine
Tertiary amine
C1CCNC1
C1CC[NH]C1
C1CC[NH]C1.c1cnc2c(c1)C[NH]CCO2
HCl
null
80
null
C1CCNC1.CN1CC(CCCl)Oc2ncccc2C1=O>>CN1CC(CCN2CCCC2)Oc2ncccc2C1=O
ord_dataset-01dbb772c5e249108f0b191ed17a2c0c
ord-78147b45cdc7467d8d67941c2d646da8
CN1CC(CCCl)Oc2ncccc2C1=O.CNc1ccccc1>>CN1CC(CCN(C)c2ccccc2)Oc2ncccc2C1=O
Cl.ClCCC1OC2=C(C(N(C1)C)=O)C=CC=N2.CNC1=CC=CC=C1>>CN1CC(OC2=C(C1=O)C=CC=N2)CCN(C2=CC=CC=C2)C
Cl[CH2:6][CH2:5][CH:4]1[CH2:3][N:2]([CH3:1])[C:22](=[O:23])[c:21]2[c:16]([n:17][cH:18][cH:19][cH:20]2)[O:15]1.[NH:7]([CH3:8])[c:9]1[cH:10][cH:11][cH:12][cH:13][cH:14]1>>[CH3:1][N:2]1[CH2:3][CH:4]([CH2:5][CH2:6][N:7]([CH3:8])[c:9]2[cH:10][cH:11][cH:12][cH:13][cH:14]2)[O:15][c:16]2[n:17][cH:18][cH:19][cH:20][c:21]2[C:22]...
CN1CC(CCCl)Oc2ncccc2C1=O.CNc1ccccc1
CN1CC(CCN(C)c2ccccc2)Oc2ncccc2C1=O
null
null
null
Heteroatom Alkylation and Arylation
N-alkylation of secondary amines with alkyl halides
6d58cac08ccced0a33ed16fbca180bc12aa011288d6476106d98a7b2cbc3d709
523d37155b42c8dc851abeddadebb241cdd90bdf649ba750c35e13c8c752d7b0
O=C1NCC(CCNc2ccccc2)Oc2ncccc21
Cl-[CH2;D2;+0:1]-[C:2]-[C:3]-[#8:4].[C;D1;H3:5]-[NH;D2;+0:6]-[c:7](:[c:8]):[c:9]>>[#8:4]-[C:3]-[C:2]-[CH2;D2;+0:1]-[N;H0;D3;+0:6](-[C;D1;H3:5])-[c:7](:[c:8]):[c:9]
31
[{"value": 31.0, "product": "CN1CC(OC2=C(C1=O)C=CC=N2)CCN(C2=CC=CC=C2)C", "details": "PERCENTYIELD", "is_desired": false}]
95
CELSIUS
2
DAY
2-(2-Chloroethyl)-2,3-dihydro-4-methylpyrido[3,2-f][1,4]oxazepin-5(4H)-one hydrochloride, 4.00 g (0.015 mole) was dissolved in N-methylaniline (30 ml) and heated to 95° C. with stirring for 2 days. Excess N-methylaniline was removed by rotary evaporation (95° C., vacuum pump). The residue was taken up in chloroform (80...
10.6084/m9.figshare.5104873.v1
null
Primary halide.Secondary amine
Tertiary amine
null
null
c1ccccc1.c1cnc2c(c1)C[NH]CCO2
HCl
null
95
48
CN1CC(CCCl)Oc2ncccc2C1=O.CNc1ccccc1>>CN1CC(CCN(C)c2ccccc2)Oc2ncccc2C1=O
ord_dataset-01dbb772c5e249108f0b191ed17a2c0c
ord-d39ddbbc138844068577c6b89ab48ac7
CC1CCCN1.CN1CC(CCCl)Oc2ncccc2C1=O>>CC1CCCN1CCC1CN(C)C(=O)c2cccnc2O1
ClCCC1OC2=C(C(N(C1)C)=O)C=CC=N2.CC1NCCC1>>CN1CC(OC2=C(C1=O)C=CC=N2)CCN2C(CCC2)C
[CH3:1][CH:2]1[CH2:3][CH2:4][CH2:5][NH:6]1.Cl[CH2:7][CH2:8][CH:9]1[CH2:10][N:11]([CH3:12])[C:13](=[O:14])[c:15]2[cH:16][cH:17][cH:18][n:19][c:20]2[O:21]1>>[CH3:1][CH:2]1[CH2:3][CH2:4][CH2:5][N:6]1[CH2:7][CH2:8][CH:9]1[CH2:10][N:11]([CH3:12])[C:13](=[O:14])[c:15]2[cH:16][cH:17][cH:18][n:19][c:20]2[O:21]1
CC1CCCN1.CN1CC(CCCl)Oc2ncccc2C1=O
CC1CCCN1CCC1CN(C)C(=O)c2cccnc2O1
null
null
C(C)O
Heteroatom Alkylation and Arylation
N-alkylation of secondary amines with alkyl halides
19b442dc26882f89f7423416f5e0a16bdb8e48776df57991434a0634e21f0505
523d37155b42c8dc851abeddadebb241cdd90bdf649ba750c35e13c8c752d7b0
O=C1NCC(CCN2CCCC2)Oc2ncccc21
Cl-[CH2;D2;+0:1]-[C:2]-[C:3]-[#8:4].[C;D1;H3:5]-[C:6]1-[C:7]-[C:8]-[C:9]-[NH;D2;+0:10]-1>>[#8:4]-[C:3]-[C:2]-[CH2;D2;+0:1]-[N;H0;D3;+0:10]1-[C:9]-[C:8]-[C:7]-[C:6]-1-[C;D1;H3:5]
36.7
[{"value": 36.7, "product": "CN1CC(OC2=C(C1=O)C=CC=N2)CCN2C(CCC2)C", "details": "PERCENTYIELD", "is_desired": false}, {"value": 35.7, "product": "CN1CC(OC2=C(C1=O)C=CC=N2)CCN2C(CCC2)C", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
null
null
To a solution of 3.5 g (0.0145 mole) of 2-(2-chloroethyl)-2,3-dihydro-4-methylpyrido[3,2-f][1,4]oxazepine-5(4H)-one in ethanol (15 ml) was added 2-methyl pyrrolidine (5.0 g, 0.063 mole). The solution was heated to reflux for 3 hours with stirring. The ethanol was removed by rotary evaporation (water aspirator, 80° C.)....
10.6084/m9.figshare.5104873.v1
null
Primary halide.Secondary amine
Tertiary amine
C1CCNC1
C1CC[NH]C1
C1CC[NH]C1.c1cnc2c(c1)C[NH]CCO2
HCl
C(C)O
null
null
CC1CCCN1.CN1CC(CCCl)Oc2ncccc2C1=O>C(C)O>CC1CCCN1CCC1CN(C)C(=O)c2cccnc2O1
ord_dataset-01dbb772c5e249108f0b191ed17a2c0c
ord-f51221a6b41343b3ae0995547573df97
CN1CC(CCCl)Oc2ncccc2C1=O.c1cn[nH]c1>>CN1CC(CCn2cccn2)Oc2ncccc2C1=O
N1N=CC=C1.[H-].[Na+].N1N=CC=C1.N1N=CC=C1.ClCCC1OC2=C(C(N(C1)C)=O)C=CC=N2.[H-].[Na+]>>CN1CC(OC2=C(C1=O)C=CC=N2)CCN2N=CC=C2
Cl[CH2:6][CH2:5][CH:4]1[CH2:3][N:2]([CH3:1])[C:19](=[O:20])[c:18]2[c:13]([n:14][cH:15][cH:16][cH:17]2)[O:12]1.[nH:7]1[cH:8][cH:9][cH:10][n:11]1>>[CH3:1][N:2]1[CH2:3][CH:4]([CH2:5][CH2:6][n:7]2[cH:8][cH:9][cH:10][n:11]2)[O:12][c:13]2[n:14][cH:15][cH:16][cH:17][c:18]2[C:19]1=[O:20]
CN1CC(CCCl)Oc2ncccc2C1=O.c1cn[nH]c1
CN1CC(CCn2cccn2)Oc2ncccc2C1=O
null
null
CN(C=O)C
Heteroatom Alkylation and Arylation
N-alkylation of secondary amines with alkyl halides
31849359320dc3760d1a762ce95f120a544970fcb32b476aacf584ef81779a29
2e1e5fd9557b69cb528f6b2ffd179c67ef24ecb1a2c3994e1cdf0efe7ae19e9c
O=C1NCC(CCn2cccn2)Oc2ncccc21
Cl-[CH2;D2;+0:1]-[C:2]-[C:3]-[#8:4].[#7;a:5]1:[c:6]:[c:7]:[c:8]:[nH;D2;+0:9]:1>>[#8:4]-[C:3]-[C:2]-[CH2;D2;+0:1]-[n;H0;D3;+0:9]1:[#7;a:5]:[c:6]:[c:7]:[c:8]:1
null
[]
null
null
8
HOUR
To a suspension of sodium hydride (1.2 g active, 0.05 mole) in dimethylformamide (15 ml) was added dropwise a solution of pyrazole (3.10 g, 0.045 mole) in dimethylformamide (15 ml). The resulting solution was then added to a solution of 2-(2-chloroethyl)-2,3-dihydro-4-methylpyrido[3,2-f][1,4]oxazepine-5(4H)-one (9.12 g...
10.6084/m9.figshare.5104873.v1
null
Primary halide
null
c1cn[nH]c1
c1cn[nH]c1
c1cn[nH]c1.c1cnc2c(c1)C[NH]CCO2
HCl
CN(C=O)C
null
8
CN1CC(CCCl)Oc2ncccc2C1=O.c1cn[nH]c1>CN(C=O)C>CN1CC(CCn2cccn2)Oc2ncccc2C1=O
ord_dataset-01dbb772c5e249108f0b191ed17a2c0c
ord-db521c60394943f7aa9b07de7bbb410c
C1COCCN1.CN1CC(CCCl)Oc2ncccc2C1=S>>CN1CC(CCN2CCOCC2)Oc2ncccc2C1=S
ClCCC1OC2=C(C(N(C1)C)=S)C=CC=N2.N1CCOCC1>>CN1CC(OC2=C(C1=S)C=CC=N2)CCN2CCOCC2
[NH:7]1[CH2:8][CH2:9][O:10][CH2:11][CH2:12]1.Cl[CH2:6][CH2:5][CH:4]1[CH2:3][N:2]([CH3:1])[C:20](=[S:21])[c:19]2[c:14]([n:15][cH:16][cH:17][cH:18]2)[O:13]1>>[CH3:1][N:2]1[CH2:3][CH:4]([CH2:5][CH2:6][N:7]2[CH2:8][CH2:9][O:10][CH2:11][CH2:12]2)[O:13][c:14]2[n:15][cH:16][cH:17][cH:18][c:19]2[C:20]1=[S:21]
C1COCCN1.CN1CC(CCCl)Oc2ncccc2C1=S
CN1CC(CCN2CCOCC2)Oc2ncccc2C1=S
null
null
null
Heteroatom Alkylation and Arylation
N-alkylation of secondary amines with alkyl halides
2bad30dcdb0a20edb8ce877f072b133eedfd870621da393ec393128bfee00977
523d37155b42c8dc851abeddadebb241cdd90bdf649ba750c35e13c8c752d7b0
S=C1NCC(CCN2CCOCC2)Oc2ncccc21
Cl-[CH2;D2;+0:1]-[C:2]-[C:3]-[#8:4].[#8:5]1-[C:6]-[C:7]-[NH;D2;+0:8]-[C:9]-[C:10]-1>>[#8:4]-[C:3]-[C:2]-[CH2;D2;+0:1]-[N;H0;D3;+0:8]1-[C:7]-[C:6]-[#8:5]-[C:10]-[C:9]-1
null
[]
null
null
6
HOUR
2-(2-Chloroethyl)-2,3-dihydro-4-methylpyrido[3,2-f][1,4]oxazepine-5(4H)-thione, 4.5 g (0.018 mole) was dissolved in morpholine (30 ml). The solution was heated with stirring to 50°-60° C. for 6 hr. The morpholine was then removed by rotary evaporation (90° C., vacuum pump). The residue was taken up in chloroform (100 m...
10.6084/m9.figshare.5104873.v1
null
Primary halide.Secondary amine
Tertiary amine
C1COCCN1
C1COCC[NH]1
C1COCC[NH]1.c1cnc2c(c1)C[NH]CCO2
HCl
null
null
6
C1COCCN1.CN1CC(CCCl)Oc2ncccc2C1=S>>CN1CC(CCN2CCOCC2)Oc2ncccc2C1=S
ord_dataset-01dbb772c5e249108f0b191ed17a2c0c
ord-872233572f814beb868d5accde50c333
CCN1CC(CCCl)Oc2ncccc2C1=S.CNC>>CCN1CC(CCN(C)C)Oc2ncccc2C1=S
Cl.ClCCC1OC2=C(C(N(C1)CC)=S)C=CC=N2.CNC.CNC>>CN(CCC1OC2=C(C(N(C1)CC)=S)C=CC=N2)C
Cl[CH2:7][CH2:6][CH:5]1[CH2:4][N:3]([CH2:2][CH3:1])[C:18](=[S:19])[c:17]2[c:12]([n:13][cH:14][cH:15][cH:16]2)[O:11]1.[NH:8]([CH3:9])[CH3:10]>>[CH3:1][CH2:2][N:3]1[CH2:4][CH:5]([CH2:6][CH2:7][N:8]([CH3:9])[CH3:10])[O:11][c:12]2[n:13][cH:14][cH:15][cH:16][c:17]2[C:18]1=[S:19]
CCN1CC(CCCl)Oc2ncccc2C1=S.CNC
CCN1CC(CCN(C)C)Oc2ncccc2C1=S
null
null
null
Heteroatom Alkylation and Arylation
N-alkylation of secondary amines with alkyl halides
6d58cac08ccced0a33ed16fbca180bc12aa011288d6476106d98a7b2cbc3d709
523d37155b42c8dc851abeddadebb241cdd90bdf649ba750c35e13c8c752d7b0
S=C1NCCOc2ncccc21
Cl-[CH2;D2;+0:1]-[C:2]-[C:3]-[#8:4].[C;D1;H3:5]-[NH;D2;+0:6]-[C;D1;H3:7]>>[#8:4]-[C:3]-[C:2]-[CH2;D2;+0:1]-[N;H0;D3;+0:6](-[C;D1;H3:5])-[C;D1;H3:7]
null
[]
null
null
6
DAY
2-(2-Chloroethyl)-4-ethyl-2,3-dihydropyrido[3,2-f][1,4]oxazepin-5(4H)-thione hydrochloride, 5.00 g (0.016 mole) was added to 20 ml of anhydrous dimethylamine. The reaction flask was sealed tightly and stirred at room temperature for 6 days. The flask was opened after cooling to 0° C. and dimethylamine allowed to evapor...
10.6084/m9.figshare.5104873.v1
null
Primary halide.Secondary amine
Tertiary amine
null
null
c1cnc2c(c1)C[NH]CCO2
HCl
null
null
144
CCN1CC(CCCl)Oc2ncccc2C1=S.CNC>>CCN1CC(CCN(C)C)Oc2ncccc2C1=S
ord_dataset-01dbb772c5e249108f0b191ed17a2c0c
ord-9d782d8069744710b9a22aaa91c12169
CNC.O=C1c2cccnc2OC(CCl)CN1C1CCCCC1>>CN(C)CC1CN(C2CCCCC2)C(=O)c2cccnc2O1
ClCC1OC2=C(C(N(C1)C1CCCCC1)=O)C=CC=N2.ClCC1OC2=C(C(N(C1)C1CCCCC1)=O)C=CC=N2.CNC.C(C(=O)O)(=O)O>>C(C(=O)O)(=O)O.C1(CCCCC1)N1CC(OC2=C(C1=O)C=CC=N2)CN(C)C
[CH3:1][NH:2][CH3:3].Cl[CH2:4][CH:5]1[CH2:6][N:7]([CH:8]2[CH2:9][CH2:10][CH2:11][CH2:12][CH2:13]2)[C:14](=[O:15])[c:16]2[cH:17][cH:18][cH:19][n:20][c:21]2[O:22]1>>[CH3:1][N:2]([CH3:3])[CH2:4][CH:5]1[CH2:6][N:7]([CH:8]2[CH2:9][CH2:10][CH2:11][CH2:12][CH2:13]2)[C:14](=[O:15])[c:16]2[cH:17][cH:18][cH:19][n:20][c:21]2[O:22...
CNC.O=C1c2cccnc2OC(CCl)CN1C1CCCCC1
CN(C)CC1CN(C2CCCCC2)C(=O)c2cccnc2O1
null
null
C(C)(C)O
Heteroatom Alkylation and Arylation
N-alkylation of secondary amines with alkyl halides
6d58cac08ccced0a33ed16fbca180bc12aa011288d6476106d98a7b2cbc3d709
523d37155b42c8dc851abeddadebb241cdd90bdf649ba750c35e13c8c752d7b0
O=C1c2cccnc2OCCN1C1CCCCC1
Cl-[CH2;D2;+0:1]-[C:2](-[#8:3]-[c:4]:[#7;a:5])-[C:6]-[#7:7].[C;D1;H3:8]-[NH;D2;+0:9]-[C;D1;H3:10]>>[#7:7]-[C:6]-[C:2](-[CH2;D2;+0:1]-[N;H0;D3;+0:9](-[C;D1;H3:8])-[C;D1;H3:10])-[#8:3]-[c:4]:[#7;a:5]
null
[]
null
null
null
null
Utilizing the procedure of Example 10, 2-(chloromethyl-4-cyclohexyl-2,3-dihydropyrido[3,2-f][1,4]oxazepin-5(4H)-one (Intermediate 35) is reacted with 40% aqueous dimethylamine and reacted with oxalic acid in isopropyl alcohol. Conditions: See reaction.notes.procedure_details.
10.6084/m9.figshare.5104873.v1
null
Primary halide.Secondary amine
Tertiary amine
null
null
C1CCCCC1.c1cnc2c(c1)C[NH]CCO2
HCl
C(C)(C)O
null
null
CNC.O=C1c2cccnc2OC(CCl)CN1C1CCCCC1>C(C)(C)O>CN(C)CC1CN(C2CCCCC2)C(=O)c2cccnc2O1
ord_dataset-01dbb772c5e249108f0b191ed17a2c0c
ord-7051746fd05449e68d2d9950a4f789a1
CN(C)CCC1CN(Cc2ccccc2)C(=O)c2cccnc2O1>>CN(C)CCC1CNC(=O)c2cccnc2O1
[OH-].[Na+].C(C(=O)O)(=O)O.CN(C)CCC1OC2=C(C(N(C1)CC1=CC=CC=C1)=O)C=CC=N2.CN(C=O)C>>CN(CCC1OC2=C(C(NC1)=O)C=CC=N2)C
c1ccc(C[N:8]2[CH2:7][CH:6]([CH2:5][CH2:4][N:2]([CH3:1])[CH3:3])[O:17][c:16]3[c:11]([cH:12][cH:13][cH:14][n:15]3)[C:9]2=[O:10])cc1>>[CH3:1][N:2]([CH3:3])[CH2:4][CH2:5][CH:6]1[CH2:7][NH:8][C:9](=[O:10])[c:11]2[cH:12][cH:13][cH:14][n:15][c:16]2[O:17]1
CN(C)CCC1CN(Cc2ccccc2)C(=O)c2cccnc2O1
CN(C)CCC1CNC(=O)c2cccnc2O1
null
null
O
Deprotection
Hydrogenolysis of tertiary amines
b28a135fe3de6ff0ffbbf778b3863f5bc10e3bf8c4ba3b0b8ff8009777b68df1
34b1225b879c7cd6f415e82440353a2915ca55dd325d399a53ba925060397178
O=C1NCCOc2ncccc21
[#7;a:1]:[c:2]1:[c:3]-[C:4](=[O;D1;H0:5])-[N;H0;D3;+0:6](-C-c2:c:c:c:c:c:2)-[C:7]-[C:8]-[#8:9]-1>>[#7;a:1]:[c:2]1:[c:3]-[C:4](=[O;D1;H0:5])-[NH;D2;+0:6]-[C:7]-[C:8]-[#8:9]-1
null
[]
null
null
20
MINUTE
A solution of 3.0 g (0.006 mole) of 2-[2-(dimethylamino ethyl]-2,3-dihydro-4-phenylmethylpyrido[3,2-f][1,4]oxazepin-5(4H)-one oxalate [1:1.5]-hemihydrate in about 50 ml of water was made basic with dilute aqueous sodium hydroxide solution and then extracted with three 50 ml portions of benzene. The combined benzene ext...
10.6084/m9.figshare.5104873.v1
null
Tertiary amide
Secondary amide
c1ccccc1.c1cnc2c(c1)C[NH]CCO2
c1cnc2c(c1)CNCCO2
c1cnc2c(c1)CNCCO2
Other
O
null
0.333333
CN(C)CCC1CN(Cc2ccccc2)C(=O)c2cccnc2O1>O>CN(C)CCC1CNC(=O)c2cccnc2O1
ord_dataset-01dbb772c5e249108f0b191ed17a2c0c
ord-689206cad7fa430599e0f8db786a2e2d
CN1CC(CCCl)Oc2ncccc2C1=O.Fc1ccc(C(c2ccc(F)cc2)C2CCNCC2)cc1.[OH-]>>CN1CC(CCN2CCC(C(c3ccc(F)cc3)c3ccc(F)cc3)CC2)Oc2ncccc2C1=O.CN1CC(CCN2CCC(C(c3ccc(F)cc3)c3ccc(F)cc3)CC2)Oc2ncccc2C1=O.Cl.Cl.Cl.O
Cl.ClCCC1OC2=C(C(N(C1)C)=O)C=CC=N2.[OH-].[Na+].FC1=CC=C(C=C1)C(C1CCNCC1)C1=CC=C(C=C1)F>>O.Cl.Cl.FC1=CC=C(C=C1)C(C1CCN(CC1)CCC1OC2=C(C(N(C1)C)=O)C=CC=N2)C2=CC=C(C=C2)F.FC2=CC=C(C=C2)C(C2=CC=C(C=C2)F)C2CCN(CC2)CCC2OC1=C(C(N(C2)C)=O)C=CC=N1.Cl.Cl
[CH3:1][N:2]1[CH2:3][CH:4]([CH2:5][CH2:6][Cl:73])[O:28][c:29]2[n:30][cH:31][cH:32][cH:33][c:34]2[C:35]1=[O:36].[NH:7]1[CH2:8][CH2:9][CH:10]([CH:11]([c:12]2[cH:13][cH:14][c:15]([F:16])[cH:17][cH:18]2)[c:41]2[cH:25][cH:24][c:22]([F:23])[cH:19][cH:40]2)[CH2:26][CH2:27]1.[OH-:64]>>[CH3:1][N:2]1[CH2:3][CH:4]([CH2:5][CH2:6][...
CN1CC(CCCl)Oc2ncccc2C1=O.Fc1ccc(C(c2ccc(F)cc2)C2CCNCC2)cc1.[OH-]
CN1CC(CCN2CCC(C(c3ccc(F)cc3)c3ccc(F)cc3)CC2)Oc2ncccc2C1=O.CN1CC(CCN2CCC(C(c3ccc(F)cc3)c3ccc(F)cc3)CC2)Oc2ncccc2C1=O.Cl.Cl.Cl.O
null
null
C(Cl)(Cl)Cl
Aromatic Heterocycle Formation
OtherReaction
5a09a210a0153885747da70f67cf1f581cd83591f7c50fe484bcc919fa5fb333
f5c8bd4770c356b6e13d1a5ab63d3018ff9bf17614b67b80bcd2fa80c3297832
O=C1NCC(CCN2CCC(C(c3ccccc3)c3ccccc3)CC2)Oc2ncccc21.O=C1NCC(CCN2CCC(C(c3ccccc3)c3ccccc3)CC2)Oc2ncccc21
[#8:1]-[C:2]-[C:3]-[CH2;D2;+0:4]-[Cl;H0;D1;+0:5].[F;D1;H0:6]-[c;H0;D3;+0:7]1:[c:8]:[cH;D2;+0:9]:[c;H0;D3;+0:10](-[CH;D3;+0:11](-[C:12]2-[C:13]-[C:14]-[NH;D2;+0:15]-[C:16]-[C:17]-2)-[c:18](:[c:19]):[c:20]):[cH;D2;+0:21]:[cH;D2;+0:22]:1.[OH-;D0:23]>>[#7:24]-[C:25]-[CH;D3;+0:21](-[CH2;D2;+0:10]-[C:26]-[#7:27])-[O;H0;D2;+0...
null
[]
null
null
null
null
Ten grams (0.036 mole) of 2-(2-chloroethyl)-2,3-dihydro-4-methylpyrido[3,2-f]-1,4-oxazepin-5-(4H)-one hydrochloride were partitioned between dilute sodium hydroxide and chloroform. The chloroform was dried over sodium sulfate and concentrated on the rotary evaporator. The residue was dissolved in 50 ml of ethanol and 1...
10.6084/m9.figshare.5104873.v1
null
Aromatic halide.Primary halide.Secondary amine
Aromatic halide.Aromatic halide.Aromatic halide.Ether.Tertiary amide.Tertiary amine.Tertiary amine
C1CCNCC1.c1ccccc1
C1CC[NH]CC1.c1ccccc1.C1CC[NH]CC1.c1ccccc1.c1ccccc1.c1cnc2c(c1)C[NH]CCO2
C1CC[NH]CC1.c1ccccc1.c1ccccc1.c1cnc2c(c1)C[NH]CCO2.C1CC[NH]CC1.c1ccccc1.c1ccccc1.c1cnc2c(c1)C[NH]CCO2
null
C(Cl)(Cl)Cl
null
null
CN1CC(CCCl)Oc2ncccc2C1=O.Fc1ccc(C(c2ccc(F)cc2)C2CCNCC2)cc1.[OH-]>C(Cl)(Cl)Cl>CN1CC(CCN2CCC(C(c3ccc(F)cc3)c3ccc(F)cc3)CC2)Oc2ncccc2C1=O.CN1CC(CCN2CCC(C(c3ccc(F)cc3)c3ccc(F)cc3)CC2)Oc2ncccc2C1=O.Cl.Cl.Cl.O
ord_dataset-01dbb772c5e249108f0b191ed17a2c0c
ord-527d0d80a4d0427eaa7b5dca19829348
CN1CC(CCCl)Oc2ncccc2C1=S.CNc1ccccc1>>CN1CC(CCN(C)c2ccccc2)Oc2ncccc2C1=S
ClCCC1OC2=C(C(N(C1)C)=S)C=CC=N2.CNC1=CC=CC=C1.CNC1=CC=CC=C1>>CN1CC(OC2=C(C1=S)C=CC=N2)CCN(C2=CC=CC=C2)C
Cl[CH2:6][CH2:5][CH:4]1[CH2:3][N:2]([CH3:1])[C:22](=[S:23])[c:21]2[c:16]([n:17][cH:18][cH:19][cH:20]2)[O:15]1.[NH:7]([CH3:8])[c:9]1[cH:10][cH:11][cH:12][cH:13][cH:14]1>>[CH3:1][N:2]1[CH2:3][CH:4]([CH2:5][CH2:6][N:7]([CH3:8])[c:9]2[cH:10][cH:11][cH:12][cH:13][cH:14]2)[O:15][c:16]2[n:17][cH:18][cH:19][cH:20][c:21]2[C:22]...
CN1CC(CCCl)Oc2ncccc2C1=S.CNc1ccccc1
CN1CC(CCN(C)c2ccccc2)Oc2ncccc2C1=S
null
null
C1(=CC=CC=C1)C
Heteroatom Alkylation and Arylation
N-alkylation of secondary amines with alkyl halides
6d58cac08ccced0a33ed16fbca180bc12aa011288d6476106d98a7b2cbc3d709
523d37155b42c8dc851abeddadebb241cdd90bdf649ba750c35e13c8c752d7b0
S=C1NCC(CCNc2ccccc2)Oc2ncccc21
Cl-[CH2;D2;+0:1]-[C:2]-[C:3]-[#8:4].[C;D1;H3:5]-[NH;D2;+0:6]-[c:7](:[c:8]):[c:9]>>[#8:4]-[C:3]-[C:2]-[CH2;D2;+0:1]-[N;H0;D3;+0:6](-[C;D1;H3:5])-[c:7](:[c:8]):[c:9]
null
[]
null
null
2
DAY
To a suspension of 2-(2-chloroethyl)-2,3-dihydro-4-methylpyrido[3,2-f][1,4]oxazepine-5(4H)-thione in 100 ml of toluene was added 11.49 g (0.11 mole) N-methylaniline and the mixture heated to reflux with stirring for 2 days (after approx. 6 hr, 23.0 g (0.22 mole) additional N-methylaniline was added). Toluene was remove...
10.6084/m9.figshare.5104873.v1
null
Primary halide.Secondary amine
Tertiary amine
null
null
c1ccccc1.c1cnc2c(c1)C[NH]CCO2
HCl
C1(=CC=CC=C1)C
null
48
CN1CC(CCCl)Oc2ncccc2C1=S.CNc1ccccc1>C1(=CC=CC=C1)C>CN1CC(CCN(C)c2ccccc2)Oc2ncccc2C1=S
ord_dataset-01dbb772c5e249108f0b191ed17a2c0c
ord-ec03ce1100954ca0bec6d9b29d1c7ce8
CCO.CN1CC(CCCl)Oc2ncccc2C1=S.Fc1ccc(C(c2ccc(F)cc2)C2CCNCC2)cc1.O=C([O-])[O-]>>CN1CC(CCN2CCC(C(c3ccc(F)cc3)c3ccc(F)cc3)CC2)Oc2ncccc2C1=S.O.O=C(O)C(=O)O
ClCCC1OC2=C(C(N(C1)C)=S)C=CC=N2.FC1=CC=C(C=C1)C(C1CCNCC1)C1=CC=C(C=C1)F.C(C)O.C(=O)([O-])[O-].[K+].[K+]>>O.C(C(=O)O)(=O)O.FC1=CC=C(C=C1)C(C1CCN(CC1)CCC1OC2=C(C(N(C1)C)=S)C=CC=N2)C2=CC=C(C=C2)F
C([CH3:41])[OH:42].Cl[CH2:6][CH2:5][CH:4]1[CH2:3][N:2]([CH3:1])[C:35](=[S:36])[c:34]2[c:29]([n:30][cH:31][cH:32][cH:33]2)[O:28]1.[NH:7]1[CH2:8][CH2:9][CH:10]([CH:11]([c:12]2[cH:13][cH:14][c:15]([F:16])[cH:17][cH:18]2)[c:19]2[cH:20][cH:21][c:22]([F:23])[cH:24][cH:25]2)[CH2:26][CH2:27]1.[O-:37][C:39](=[O:38])[O-:40]>>[CH...
CCO.CN1CC(CCCl)Oc2ncccc2C1=S.Fc1ccc(C(c2ccc(F)cc2)C2CCNCC2)cc1.O=C([O-])[O-]
CN1CC(CCN2CCC(C(c3ccc(F)cc3)c3ccc(F)cc3)CC2)Oc2ncccc2C1=S.O.O=C(O)C(=O)O
null
null
null
Acylation
OtherReaction
2002116e767ae1e26b92e45d2c1e2d70fd1b71f5fd55b011d52b4f2b624197f7
1657da22b930a2f8cb24a0cf8f110142ca1524ba96790fa23a24272ddc03aeda
S=C1NCC(CCN2CCC(C(c3ccccc3)c3ccccc3)CC2)Oc2ncccc21
Cl-[CH2;D2;+0:1]-[C:2]-[C:3]-[#8:4].[CH3;D1;+0:5]-C-[OH;D1;+0:6].[C:7]-[C:8]-[NH;D2;+0:9]-[C:10]-[C:11].[O-;H0;D1:12]-[C;H0;D3;+0:13](-[O-;H0;D1:14])=[O;D1;H0:15]>>[#8:4]-[C:3]-[C:2]-[CH2;D2;+0:1]-[N;H0;D3;+0:9](-[C:8]-[C:7])-[C:10]-[C:11].[O;D1;H0:15]=[C;H0;D3;+0:13](-[OH;D1;+0:14])-[C;H0;D3;+0:5](-[O;D1;H1:16])=[O;H0...
null
[]
null
null
null
null
A solution of 4 g (0.016 mole) of 2-(2-chloroethyl)-2,3-dihydro-4-methylpyrido[3,2-f][1,4]-oxazepine-5(4H)-thione and 4.5 g (0.016 mole) of 4-[bis(4-fluorophenyl)methyl]piperidine in 100 ml of ethanol was refluxed for 48 hr. One gram of K2CO3 was added and this mixture stirred at reflux for 144 hr. The mixture was conc...
10.6084/m9.figshare.5104873.v1
null
Primary halide.Primary alcohol.Secondary amine
Carboxylic acid.Carboxylic acid.Tertiary amine
C1CCNCC1
C1CC[NH]CC1
C1CC[NH]CC1.c1ccccc1.c1ccccc1.c1cnc2c(c1)C[NH]CCO2
HCl
null
null
null
CCO.CN1CC(CCCl)Oc2ncccc2C1=S.Fc1ccc(C(c2ccc(F)cc2)C2CCNCC2)cc1.O=C([O-])[O-]>>CN1CC(CCN2CCC(C(c3ccc(F)cc3)c3ccc(F)cc3)CC2)Oc2ncccc2C1=S.O.O=C(O)C(=O)O
ord_dataset-01dbb772c5e249108f0b191ed17a2c0c
ord-6d86f383aca44f438845b19594bf30af
CN1CC(CCCl)Oc2ncccc2C1=S.c1cn[nH]c1>>CN1CC(CCn2cccn2)Oc2ncccc2C1=S
ClCCC1OC2=C(C(N(C1)C)=S)C=CC=N2.[H-].[Na+].N1N=CC=C1.[H][H]>>CN1CC(OC2=C(C1=S)C=CC=N2)CCN2N=CC=C2
Cl[CH2:6][CH2:5][CH:4]1[CH2:3][N:2]([CH3:1])[C:19](=[S:20])[c:18]2[c:13]([n:14][cH:15][cH:16][cH:17]2)[O:12]1.[nH:7]1[cH:8][cH:9][cH:10][n:11]1>>[CH3:1][N:2]1[CH2:3][CH:4]([CH2:5][CH2:6][n:7]2[cH:8][cH:9][cH:10][n:11]2)[O:12][c:13]2[n:14][cH:15][cH:16][cH:17][c:18]2[C:19]1=[S:20]
CN1CC(CCCl)Oc2ncccc2C1=S.c1cn[nH]c1
CN1CC(CCn2cccn2)Oc2ncccc2C1=S
null
null
CN(C=O)C
Heteroatom Alkylation and Arylation
N-alkylation of secondary amines with alkyl halides
31849359320dc3760d1a762ce95f120a544970fcb32b476aacf584ef81779a29
2e1e5fd9557b69cb528f6b2ffd179c67ef24ecb1a2c3994e1cdf0efe7ae19e9c
S=C1NCC(CCn2cccn2)Oc2ncccc21
Cl-[CH2;D2;+0:1]-[C:2]-[C:3]-[#8:4].[#7;a:5]1:[c:6]:[c:7]:[c:8]:[nH;D2;+0:9]:1>>[#8:4]-[C:3]-[C:2]-[CH2;D2;+0:1]-[n;H0;D3;+0:9]1:[#7;a:5]:[c:6]:[c:7]:[c:8]:1
null
[]
null
null
8
HOUR
To a suspension of 2.16 g (0.054 mole) of sodium hydride in 20 ml of dimethylformamide was added dropwise a solution of 2.92 g (0.043 mole) of pyrazole in 10 ml of dimethylformamide. There was a slight exotherm at this point with some evolution of hydrogen gas. The resulting solution was then added dropwise to a soluti...
10.6084/m9.figshare.5104873.v1
null
Primary halide
null
c1cn[nH]c1
c1cn[nH]c1
c1cn[nH]c1.c1cnc2c(c1)C[NH]CCO2
HCl
CN(C=O)C
null
8
CN1CC(CCCl)Oc2ncccc2C1=S.c1cn[nH]c1>CN(C=O)C>CN1CC(CCn2cccn2)Oc2ncccc2C1=S
ord_dataset-01dbb772c5e249108f0b191ed17a2c0c
ord-a175c2df01544d719c07426ac8bda4f5
CN1CC(C)(CCCl)Oc2ncccc2C1=O.CNC>>CN(C)CCC1(C)CN(C)C(=O)c2cccnc2O1.Cl
Cl.ClCCC1(OC2=C(C(N(C1)C)=O)C=CC=N2)C.CNC>>Cl.Cl.CN(CCC1(OC2=C(C(N(C1)C)=O)C=CC=N2)C)C
[CH2:4]([CH2:5][C:6]1([CH3:7])[CH2:8][N:9]([CH3:10])[C:11](=[O:12])[c:13]2[cH:14][cH:15][cH:16][n:17][c:18]2[O:19]1)[Cl:21].[CH3:1][NH:2][CH3:3]>>[CH3:1][N:2]([CH3:3])[CH2:4][CH2:5][C:6]1([CH3:7])[CH2:8][N:9]([CH3:10])[C:11](=[O:12])[c:13]2[cH:14][cH:15][cH:16][n:17][c:18]2[O:19]1.[ClH:21]
CN1CC(C)(CCCl)Oc2ncccc2C1=O.CNC
CN(C)CCC1(C)CN(C)C(=O)c2cccnc2O1.Cl
null
null
CO
Heteroatom Alkylation and Arylation
N-alkylation of secondary amines with alkyl halides
6d58cac08ccced0a33ed16fbca180bc12aa011288d6476106d98a7b2cbc3d709
523d37155b42c8dc851abeddadebb241cdd90bdf649ba750c35e13c8c752d7b0
O=C1NCCOc2ncccc21
[#8:1]-[C:2]-[C:3]-[CH2;D2;+0:4]-[Cl;H0;D1;+0:5].[C;D1;H3:6]-[NH;D2;+0:7]-[C;D1;H3:8]>>[#8:1]-[C:2]-[C:3]-[CH2;D2;+0:4]-[N;H0;D3;+0:7](-[C;D1;H3:6])-[C;D1;H3:8].[ClH;D0;+0:5]
67
[{"value": 67.0, "product": "Cl.Cl.CN(CCC1(OC2=C(C(N(C1)C)=O)C=CC=N2)C)C", "details": "PERCENTYIELD", "is_desired": false}]
null
null
8
DAY
To 4.5 g (0.015 mole) of 2-(2-chloroethyl)-2,3-dihydro-2,4-dimethylpyrido[3,2-f]-1,4-oxazepin-5(4H)-one hydrochloride in 15 ml of methanol was added 40 ml of dimethylamine. The flask was sealed tightly and left standing at room temperature for 8 days. The methanol and dimethylamine were removed by rotary evaporation (7...
10.6084/m9.figshare.5104873.v1
null
Primary halide.Secondary amine
Tertiary amine
null
null
c1cnc2c(c1)C[NH]CCO2
null
CO
null
192
CN1CC(C)(CCCl)Oc2ncccc2C1=O.CNC>CO>CN(C)CCC1(C)CN(C)C(=O)c2cccnc2O1.Cl
ord_dataset-01dbb772c5e249108f0b191ed17a2c0c
ord-08923e8e29984bf08578bf990ca8b9ae
CN1CC(C)(CCCl)Oc2ncccc2C1=S.CNC>>CN(C)CCC1(C)CN(C)C(=S)c2cccnc2O1.Cl
ClCCC1(OC2=C(C(N(C1)C)=S)C=CC=N2)C.CNC>>Cl.CN(CCC1(OC2=C(C(N(C1)C)=S)C=CC=N2)C)C
[CH2:4]([CH2:5][C:6]1([CH3:7])[CH2:8][N:9]([CH3:10])[C:11](=[S:12])[c:13]2[cH:14][cH:15][cH:16][n:17][c:18]2[O:19]1)[Cl:20].[CH3:1][NH:2][CH3:3]>>[CH3:1][N:2]([CH3:3])[CH2:4][CH2:5][C:6]1([CH3:7])[CH2:8][N:9]([CH3:10])[C:11](=[S:12])[c:13]2[cH:14][cH:15][cH:16][n:17][c:18]2[O:19]1.[ClH:20]
CN1CC(C)(CCCl)Oc2ncccc2C1=S.CNC
CN(C)CCC1(C)CN(C)C(=S)c2cccnc2O1.Cl
null
null
CO
Heteroatom Alkylation and Arylation
N-alkylation of secondary amines with alkyl halides
6d58cac08ccced0a33ed16fbca180bc12aa011288d6476106d98a7b2cbc3d709
523d37155b42c8dc851abeddadebb241cdd90bdf649ba750c35e13c8c752d7b0
S=C1NCCOc2ncccc21
[#8:1]-[C:2]-[C:3]-[CH2;D2;+0:4]-[Cl;H0;D1;+0:5].[C;D1;H3:6]-[NH;D2;+0:7]-[C;D1;H3:8]>>[#8:1]-[C:2]-[C:3]-[CH2;D2;+0:4]-[N;H0;D3;+0:7](-[C;D1;H3:6])-[C;D1;H3:8].[ClH;D0;+0:5]
76
[{"value": 76.0, "product": "Cl.CN(CCC1(OC2=C(C(N(C1)C)=S)C=CC=N2)C)C", "details": "PERCENTYIELD", "is_desired": false}]
null
null
10
DAY
To a suspension of 4.5 g (0.017 mole) of 2-(2-chloroethyl)-2,3-dihydro-2,4-dimethylpyrido[3,2-f]-1,4-oxazepine-5(4H)-thione in 20 ml of methanol, cooled in an ice bath, was added 40 ml of dimethylamine. The flask was sealed tightly and left standing at room temperature for 10 days. The dimethylamine and methanol were r...
10.6084/m9.figshare.5104873.v1
null
Primary halide.Secondary amine
Tertiary amine
null
null
c1cnc2c(c1)C[NH]CCO2
null
CO
null
240
CN1CC(C)(CCCl)Oc2ncccc2C1=S.CNC>CO>CN(C)CCC1(C)CN(C)C(=S)c2cccnc2O1.Cl
ord_dataset-01dbb772c5e249108f0b191ed17a2c0c
ord-d72b57dfc95c4cd685ec1dc1014cf8f3
CC(Cl)CC1CN(C)C(=O)c2cccnc2O1.CNC>>CC(CC1CN(C)C(=O)c2cccnc2O1)N(C)C.Cl.Cl
CNC.[I-].[Na+].ClC(CC1OC2=C(C(N(C1)C)=O)C=CC=N2)C>>Cl.Cl.CN(C(CC1OC2=C(C(N(C1)C)=O)C=CC=N2)C)C
[CH3:1][CH:2]([CH2:3][CH:4]1[CH2:5][N:6]([CH3:7])[C:8](=[O:9])[c:10]2[cH:11][cH:12][cH:13][n:14][c:15]2[O:16]1)[Cl:20].[NH:17]([CH3:18])[CH3:19]>>[CH3:1][CH:2]([CH2:3][CH:4]1[CH2:5][N:6]([CH3:7])[C:8](=[O:9])[c:10]2[cH:11][cH:12][cH:13][n:14][c:15]2[O:16]1)[N:17]([CH3:18])[CH3:19].[ClH:20].[ClH:21]
CC(Cl)CC1CN(C)C(=O)c2cccnc2O1.CNC
CC(CC1CN(C)C(=O)c2cccnc2O1)N(C)C.Cl.Cl
null
null
null
Functional Group Addition
N-alkylation of secondary amines with alkyl halides
6354b1816e35679ba45812db9d6cf0e2801e934ad90352b72a8e10c741b582a5
de9d9c3ab30a40b38f20c962f47fd1d829290070ee492aec7c48aef2c08786f2
O=C1NCCOc2ncccc21
[#8:1]-[C:2]-[C:3]-[CH;D3;+0:4](-[C;D1;H3:5])-[Cl;H0;D1;+0:6].[C;D1;H3:7]-[NH;D2;+0:8]-[C;D1;H3:9]>>[#8:1]-[C:2]-[C:3]-[CH;D3;+0:4](-[C;D1;H3:5])-[N;H0;D3;+0:8](-[C;D1;H3:7])-[C;D1;H3:9].[ClH;D0;+0:6]
null
[]
null
null
7
DAY
Into a stainless steel bomb was placed 1.0 g sodium iodide, 5.0 g (0.017 mole) of 2-(2-chloropropyl)-2,3-dihydro-4-methylpyrido[3,2-f][1,4]oxazepin-5(4H)-one and 40 ml of dimethylamine. The bomb was sealed tightly, placed in the oven at 60° C. and rolled continuously for 7 days. The bomb was allowed to stand at room te...
10.6084/m9.figshare.5104873.v1
null
Secondary halide.Secondary amine
Tertiary amine
null
null
c1cnc2c(c1)C[NH]CCO2
Other
null
null
168
CC(Cl)CC1CN(C)C(=O)c2cccnc2O1.CNC>>CC(CC1CN(C)C(=O)c2cccnc2O1)N(C)C.Cl.Cl
ord_dataset-01dbb772c5e249108f0b191ed17a2c0c
ord-f80487ff4d8a47d2b5d758272f0f2d59
CC1CCCN1.CN1CC(CCCl)Oc2ncccc2C1=S>>CC(C)O.CC1CCCN1CCC1CN(C)C(=S)c2cccnc2O1
C(\C=C\C(=O)O)(=O)O.CC1NCCC1.ClCCC1OC2=C(C(N(C1)C)=S)C=CC=N2.C([O-])([O-])=O.[K+].[K+]>>CC(C)O.C(\C=C\C(=O)O)(=O)O.CN1CC(OC2=C(C1=S)C=CC=N2)CCN2C(CCC2)C
[CH3:5][CH:6]1[CH2:7][CH2:8][CH2:9][NH:10]1.Cl[CH2:11][CH2:12][CH:13]1[CH2:14][N:15]([CH3:16])[C:17](=[S:18])[c:19]2[cH:20][cH:21][cH:22][n:23][c:24]2[O:25]1>>[CH3:1][CH:2]([CH3:3])[OH:4].[CH3:5][CH:6]1[CH2:7][CH2:8][CH2:9][N:10]1[CH2:11][CH2:12][CH:13]1[CH2:14][N:15]([CH3:16])[C:17](=[S:18])[c:19]2[cH:20][cH:21][cH:22...
CC1CCCN1.CN1CC(CCCl)Oc2ncccc2C1=S
CC(C)O.CC1CCCN1CCC1CN(C)C(=S)c2cccnc2O1
null
null
C(C)O
Heteroatom Alkylation and Arylation
N-alkylation of secondary amines with alkyl halides
da1dbf66ee826e6a6dceaca1e2898a33db23975104e256522dd31d3cfd809487
02e69e7344fdc40630a38a963004019f41856704aa70b506ccd14ac03983aa03
S=C1NCC(CCN2CCCC2)Oc2ncccc21
Cl-[CH2;D2;+0:1]-[C:2]-[C:3]-[#8:4].[C;D1;H3:5]-[C:6]1-[C:7]-[C:8]-[C:9]-[NH;D2;+0:10]-1>>[#8:4]-[C:3]-[C:2]-[CH2;D2;+0:1]-[N;H0;D3;+0:10]1-[C:9]-[C:8]-[C:7]-[C:6]-1-[C;D1;H3:5]
32.8
[{"value": 16.4, "product": "CC(C)O.C(\\C=C\\C(=O)O)(=O)O.CN1CC(OC2=C(C1=S)C=CC=N2)CCN2C(CCC2)C", "details": "PERCENTYIELD", "is_desired": false}, {"value": 32.8, "product": "CC(C)O.C(\\C=C\\C(=O)O)(=O)O.CN1CC(OC2=C(C1=S)C=CC=N2)CCN2C(CCC2)C", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
8
HOUR
To a suspension of 5.0 g (0.019 mole) of 2-(chloroethyl)-2,3-dihydro-4-methylpyrido[3,2-f]-1,4-oxazepine-5(4H)-thione in 25 ml of absolute ethanol was added 3.5 g (0.04 mole) of 2-methylpyrrolidine. The mixture was heated to reflux for 6.5 hr and left standing at room temperature overnight. Mass spec and TLC showed pre...
10.6084/m9.figshare.5104873.v1
null
Primary halide.Secondary amine
Secondary alcohol.Tertiary amine
C1CCNC1
C1CC[NH]C1
C1CC[NH]C1.c1cnc2c(c1)C[NH]CCO2
null
C(C)O
null
8
CC1CCCN1.CN1CC(CCCl)Oc2ncccc2C1=S>C(C)O>CC(C)O.CC1CCCN1CCC1CN(C)C(=S)c2cccnc2O1
ord_dataset-01dbb772c5e249108f0b191ed17a2c0c
ord-89054f1c59674f65a50d35bff9d091ac
C1COCCN1.CCN1CC(CCCl)N(C)c2ccccc2C1=O>>CCN1CC(CCN2CCOCC2)N(C)c2ccccc2C1=O
ClCCC1N(C2=C(C(N(C1)CC)=O)C=CC=C2)C.N1CCOCC1>>C(C)N1CC(N(C2=C(C1=O)C=CC=C2)C)CCN2CCOCC2
[NH:8]1[CH2:9][CH2:10][O:11][CH2:12][CH2:13]1.Cl[CH2:7][CH2:6][CH:5]1[CH2:4][N:3]([CH2:2][CH3:1])[C:22](=[O:23])[c:21]2[c:16]([cH:17][cH:18][cH:19][cH:20]2)[N:14]1[CH3:15]>>[CH3:1][CH2:2][N:3]1[CH2:4][CH:5]([CH2:6][CH2:7][N:8]2[CH2:9][CH2:10][O:11][CH2:12][CH2:13]2)[N:14]([CH3:15])[c:16]2[cH:17][cH:18][cH:19][cH:20][c:...
C1COCCN1.CCN1CC(CCCl)N(C)c2ccccc2C1=O
CCN1CC(CCN2CCOCC2)N(C)c2ccccc2C1=O
null
null
null
Heteroatom Alkylation and Arylation
N-alkylation of secondary amines with alkyl halides
2bad30dcdb0a20edb8ce877f072b133eedfd870621da393ec393128bfee00977
523d37155b42c8dc851abeddadebb241cdd90bdf649ba750c35e13c8c752d7b0
O=C1NCC(CCN2CCOCC2)Nc2ccccc21
Cl-[CH2;D2;+0:1]-[C:2]-[C:3]-[#7:4].[#8:5]1-[C:6]-[C:7]-[NH;D2;+0:8]-[C:9]-[C:10]-1>>[#7:4]-[C:3]-[C:2]-[CH2;D2;+0:1]-[N;H0;D3;+0:8]1-[C:9]-[C:10]-[#8:5]-[C:6]-[C:7]-1
61
[{"value": 61.0, "product": "C(C)N1CC(N(C2=C(C1=O)C=CC=C2)C)CCN2CCOCC2", "details": "PERCENTYIELD", "is_desired": false}]
null
null
null
null
A solution of 30 g (0.112 mole) of 2-(2-chloroethyl)-4-ethyl-1-methyl-1,2,3,4-tetrahydro-5H-1,4-benzodiazepin-5-one in 70 ml of morpholine was refluxed for 3 hrs, concentrated on the rotary evaporator and the residue partitioned between chloroform and dilute sodium hydroxide. The chloroform was dried over anhydrous sod...
10.6084/m9.figshare.5104873.v1
null
Primary halide.Secondary amine
Tertiary amine
C1COCCN1
C1COCC[NH]1
C1COCC[NH]1.c1ccc2c(c1)C[NH]CC[NH]2
HCl
null
null
null
C1COCCN1.CCN1CC(CCCl)N(C)c2ccccc2C1=O>>CCN1CC(CCN2CCOCC2)N(C)c2ccccc2C1=O
ord_dataset-01dbb772c5e249108f0b191ed17a2c0c
ord-a24b688b91924da2b3f0df85caa2c0e1
CC(C)N1CC(CCl)N(C)c2ccccc2C1=O.CNC>>CC(C)N1CC(CN(C)C)N(C)c2ccccc2C1=O
ClCC1N(C2=C(C(N(C1)C(C)C)=O)C=CC=C2)C.CNC>>CN1C(CN(C(C2=C1C=CC=C2)=O)C(C)C)CN(C)C
Cl[CH2:7][CH:6]1[CH2:5][N:4]([CH:2]([CH3:1])[CH3:3])[C:19](=[O:20])[c:18]2[c:13]([cH:14][cH:15][cH:16][cH:17]2)[N:11]1[CH3:12].[NH:8]([CH3:9])[CH3:10]>>[CH3:1][CH:2]([CH3:3])[N:4]1[CH2:5][CH:6]([CH2:7][N:8]([CH3:9])[CH3:10])[N:11]([CH3:12])[c:13]2[cH:14][cH:15][cH:16][cH:17][c:18]2[C:19]1=[O:20]
CC(C)N1CC(CCl)N(C)c2ccccc2C1=O.CNC
CC(C)N1CC(CN(C)C)N(C)c2ccccc2C1=O
null
null
CO
Heteroatom Alkylation and Arylation
N-alkylation of secondary amines with alkyl halides
6d58cac08ccced0a33ed16fbca180bc12aa011288d6476106d98a7b2cbc3d709
523d37155b42c8dc851abeddadebb241cdd90bdf649ba750c35e13c8c752d7b0
O=C1NCCNc2ccccc21
Cl-[CH2;D2;+0:1]-[C:2](-[C:3]-[#7:4])-[#7:5](-[C;D1;H3:6])-[c:7].[C;D1;H3:8]-[NH;D2;+0:9]-[C;D1;H3:10]>>[#7:4]-[C:3]-[C:2](-[CH2;D2;+0:1]-[N;H0;D3;+0:9](-[C;D1;H3:8])-[C;D1;H3:10])-[#7:5](-[C;D1;H3:6])-[c:7]
null
[]
100
CELSIUS
15
HOUR
A mixture of 5.0 g (0.02 mole) of 2-chloromethyl-1,2,3,4-tetrahydro-1-methyl-4-(1-methylethyl)-5H-1,4-benzodiazepin-5-one, and 15.0 g (0.45 mole) of dimethylamine, and 200 ml of methanol were placed in a steel bomb and heated and stirred at 100° C. for 15 hr. After concentrating in vacuo, the residue partitioned betwee...
10.6084/m9.figshare.5104873.v1
null
Primary halide.Secondary amine
Tertiary amine
null
null
c1ccc2c(c1)C[NH]CC[NH]2
HCl
CO
100
15
CC(C)N1CC(CCl)N(C)c2ccccc2C1=O.CNC>CO>CC(C)N1CC(CN(C)C)N(C)c2ccccc2C1=O
ord_dataset-01dbb772c5e249108f0b191ed17a2c0c
ord-3f6dd8deeda549f8aafb1ee422df00da
CN.CNC.ClCC1CO1>>CNCC(O)CN(C)C.Cl
CNC.C(Cl)C1CO1.CN>>Cl.CN(CC(CNC)O)C
[CH3:1][NH2:2].[NH:7]([CH3:8])[CH3:9].[CH2:3]([CH:4]1[O:5][CH2:6]1)[Cl:10]>>[CH3:1][NH:2][CH2:3][CH:4]([OH:5])[CH2:6][N:7]([CH3:8])[CH3:9].[ClH:10]
CN.CNC.ClCC1CO1
CNCC(O)CN(C)C.Cl
null
null
CO
Heteroatom Alkylation and Arylation
OtherReaction
d22195cf4e7b9d5acfa6177d95cd3d6abea14a34c18d0a0dcafc33355b257996
a7cbd855026b2ff6bc2fa326904381ca9eec04c82500bb354c2a8f9ee9c38c46
null
[C;D1;H3:1]-[NH2;D1;+0:2].[C;D1;H3:3]-[NH;D2;+0:4]-[C;D1;H3:5].[Cl;H0;D1;+0:6]-[CH2;D2;+0:7]-[C:8]1-[CH2;D2;+0:9]-[O;H0;D2;+0:10]-1>>[C;D1;H3:1]-[NH;D2;+0:2]-[CH2;D2;+0:7]-[C:8](-[OH;D1;+0:10])-[CH2;D2;+0:9]-[N;H0;D3;+0:4](-[C;D1;H3:3])-[C;D1;H3:5].[ClH;D0;+0:6]
84
[{"value": 84.0, "product": "Cl.CN(CC(CNC)O)C", "details": "PERCENTYIELD", "is_desired": false}]
null
null
1.5
HOUR
Dimethylamine 22.6 g, 40% solution (0.2 mole) was added dropwise to a solution of 16 ml of epichlorohydrin (0.2 mole) in 100 ml of methanol at 5° C. stirring in an ice bath. After two hours at 5° C. a chilled solution of 86 ml methylamine of 40% solution (1 mole) was poured into the reaction mixture. Stirring was conti...
10.6084/m9.figshare.5104873.v1
null
Primary halide.Ether.Primary amine.Secondary amine
Secondary alcohol.Secondary amine.Tertiary amine
C1CO1
null
null
null
CO
null
1.5
CN.CNC.ClCC1CO1>CO>CNCC(O)CN(C)C.Cl
ord_dataset-01dbb772c5e249108f0b191ed17a2c0c
ord-5bc77dfd9e3c45db8eebc1805fbfa2fb
CN1CC(CCCl)Oc2c(ccc3cnccc23)C1=S.CNC>>CN(C)CCC1CN(C)C(=S)c2ccc3cnccc3c2O1.Cl
ClCCC1OC2=C3C=CN=CC3=CC=C2C(N(C1)C)=S.CNC>>Cl.CN(CCC1OC2=C3C=CN=CC3=CC=C2C(N(C1)C)=S)C
[CH2:4]([CH2:5][CH:6]1[CH2:7][N:8]([CH3:9])[C:10](=[S:11])[c:12]2[cH:13][cH:14][c:15]3[cH:16][n:17][cH:18][cH:19][c:20]3[c:21]2[O:22]1)[Cl:23].[CH3:1][NH:2][CH3:3]>>[CH3:1][N:2]([CH3:3])[CH2:4][CH2:5][CH:6]1[CH2:7][N:8]([CH3:9])[C:10](=[S:11])[c:12]2[cH:13][cH:14][c:15]3[cH:16][n:17][cH:18][cH:19][c:20]3[c:21]2[O:22]1....
CN1CC(CCCl)Oc2c(ccc3cnccc23)C1=S.CNC
CN(C)CCC1CN(C)C(=S)c2ccc3cnccc3c2O1.Cl
null
null
null
Heteroatom Alkylation and Arylation
N-alkylation of secondary amines with alkyl halides
6d58cac08ccced0a33ed16fbca180bc12aa011288d6476106d98a7b2cbc3d709
523d37155b42c8dc851abeddadebb241cdd90bdf649ba750c35e13c8c752d7b0
S=C1NCCOc2c1ccc1cnccc21
[#8:1]-[C:2]-[C:3]-[CH2;D2;+0:4]-[Cl;H0;D1;+0:5].[C;D1;H3:6]-[NH;D2;+0:7]-[C;D1;H3:8]>>[#8:1]-[C:2]-[C:3]-[CH2;D2;+0:4]-[N;H0;D3;+0:7](-[C;D1;H3:6])-[C;D1;H3:8].[ClH;D0;+0:5]
null
[]
null
null
null
null
Following the procedure of Example 31, 2-(2-chloroethyl)-2,3-dihydro-4-methyl-1,4-oxazepino[7,6-f]isoquinoline-5(4H)-thione is reacted with dimethylamine to give the title compound. Conditions: See reaction.notes.procedure_details.
10.6084/m9.figshare.5104873.v1
null
Primary halide.Secondary amine
Tertiary amine
null
null
c1cc2c3c(ccc2cn1)C[NH]CCO3
null
null
null
null
CN1CC(CCCl)Oc2c(ccc3cnccc23)C1=S.CNC>>CN(C)CCC1CN(C)C(=S)c2ccc3cnccc3c2O1.Cl
ord_dataset-01dbb772c5e249108f0b191ed17a2c0c
ord-efef61e1c72e49098ec79ee2158eaa42
CNC.Cc1cc2c(c3ncccc13)OC(CCCl)CN(C)C2=S>>Cc1cc2c(c3ncccc13)OC(CCN(C)C)CN(C)C2=S.Cl
ClCCC1OC2=C(C=C(C=3C=CC=NC23)C)C(N(C1)C)=S.CNC>>Cl.CN(CCC1OC2=C(C=C(C=3C=CC=NC23)C)C(N(C1)C)=S)C
[NH:16]([CH3:17])[CH3:18].[CH3:1][c:2]1[cH:3][c:4]2[c:5]([c:6]3[n:7][cH:8][cH:9][cH:10][c:11]13)[O:12][CH:13]([CH2:14][CH2:15][Cl:24])[CH2:19][N:20]([CH3:21])[C:22]2=[S:23]>>[CH3:1][c:2]1[cH:3][c:4]2[c:5]([c:6]3[n:7][cH:8][cH:9][cH:10][c:11]13)[O:12][CH:13]([CH2:14][CH2:15][N:16]([CH3:17])[CH3:18])[CH2:19][N:20]([CH3:2...
CNC.Cc1cc2c(c3ncccc13)OC(CCCl)CN(C)C2=S
Cc1cc2c(c3ncccc13)OC(CCN(C)C)CN(C)C2=S.Cl
null
null
null
Heteroatom Alkylation and Arylation
N-alkylation of secondary amines with alkyl halides
6d58cac08ccced0a33ed16fbca180bc12aa011288d6476106d98a7b2cbc3d709
523d37155b42c8dc851abeddadebb241cdd90bdf649ba750c35e13c8c752d7b0
S=C1NCCOc2c1ccc1cccnc21
[#8:1]-[C:2]-[C:3]-[CH2;D2;+0:4]-[Cl;H0;D1;+0:5].[C;D1;H3:6]-[NH;D2;+0:7]-[C;D1;H3:8]>>[#8:1]-[C:2]-[C:3]-[CH2;D2;+0:4]-[N;H0;D3;+0:7](-[C;D1;H3:6])-[C;D1;H3:8].[ClH;D0;+0:5]
null
[]
null
null
null
null
Following the procedure of Example 31, 2-(2-chloroethyl)-2,3-dihydro-4,7-dimethyl-1,4-oxazepino[6,7-h]quinoline-5(4H)-thione is reacted with dimethylamine to give the title compound. Conditions: See reaction.notes.procedure_details.
10.6084/m9.figshare.5104873.v1
null
Primary halide.Secondary amine
Tertiary amine
null
null
c1cnc2c3c(ccc2c1)C[NH]CCO3
null
null
null
null
CNC.Cc1cc2c(c3ncccc13)OC(CCCl)CN(C)C2=S>>Cc1cc2c(c3ncccc13)OC(CCN(C)C)CN(C)C2=S.Cl
ord_dataset-01dbb772c5e249108f0b191ed17a2c0c
ord-b5c30907b10f4115832fbf4e0039c599
CNC.Cc1ccc2ccc3c(c2n1)OC(CCCl)CN(C)C3=S>>Cc1ccc2ccc3c(c2n1)OC(CCN(C)C)CN(C)C3=S.Cl
ClCCC1OC2=C(C=CC=3C=CC(=NC23)C)C(N(C1)C)=S.CNC>>Cl.CN(CCC1OC2=C(C=CC=3C=CC(=NC23)C)C(N(C1)C)=S)C
[NH:16]([CH3:17])[CH3:18].[CH3:1][c:2]1[cH:3][cH:4][c:5]2[cH:6][cH:7][c:8]3[c:9]([c:10]2[n:11]1)[O:12][CH:13]([CH2:14][CH2:15][Cl:24])[CH2:19][N:20]([CH3:21])[C:22]3=[S:23]>>[CH3:1][c:2]1[cH:3][cH:4][c:5]2[cH:6][cH:7][c:8]3[c:9]([c:10]2[n:11]1)[O:12][CH:13]([CH2:14][CH2:15][N:16]([CH3:17])[CH3:18])[CH2:19][N:20]([CH3:2...
CNC.Cc1ccc2ccc3c(c2n1)OC(CCCl)CN(C)C3=S
Cc1ccc2ccc3c(c2n1)OC(CCN(C)C)CN(C)C3=S.Cl
null
null
null
Heteroatom Alkylation and Arylation
N-alkylation of secondary amines with alkyl halides
6d58cac08ccced0a33ed16fbca180bc12aa011288d6476106d98a7b2cbc3d709
523d37155b42c8dc851abeddadebb241cdd90bdf649ba750c35e13c8c752d7b0
S=C1NCCOc2c1ccc1cccnc21
[#8:1]-[C:2]-[C:3]-[CH2;D2;+0:4]-[Cl;H0;D1;+0:5].[C;D1;H3:6]-[NH;D2;+0:7]-[C;D1;H3:8]>>[#8:1]-[C:2]-[C:3]-[CH2;D2;+0:4]-[N;H0;D3;+0:7](-[C;D1;H3:6])-[C;D1;H3:8].[ClH;D0;+0:5]
null
[]
null
null
null
null
Following the procedure of Example 31, 2-(2-chloroethyl)-2,3-dihydro-4,10-dimethyl-1,4-oxazepino[6,7-h)quinoline-5(4H)-thione is reacted with dimethylamine to give the title compound. Conditions: See reaction.notes.procedure_details.
10.6084/m9.figshare.5104873.v1
null
Primary halide.Secondary amine
Tertiary amine
null
null
c1cnc2c3c(ccc2c1)C[NH]CCO3
null
null
null
null
CNC.Cc1ccc2ccc3c(c2n1)OC(CCCl)CN(C)C3=S>>Cc1ccc2ccc3c(c2n1)OC(CCN(C)C)CN(C)C3=S.Cl
ord_dataset-01dbb772c5e249108f0b191ed17a2c0c
ord-1e3095902341438cbca43e09b1024cfd
CN1CC(CCCl)Oc2ccc3ncccc3c2C1=S.CNC>>CN(C)CCC1CN(C)C(=S)c2c(ccc3ncccc23)O1.Cl
ClCCC1OC=2C(=C3C=CC=NC3=CC2)C(N(C1)C)=S.CNC>>Cl.CN(CCC1OC=2C(=C3C=CC=NC3=CC2)C(N(C1)C)=S)C
[CH2:4]([CH2:5][CH:6]1[CH2:7][N:8]([CH3:9])[C:10](=[S:11])[c:12]2[c:13]([cH:14][cH:15][c:16]3[n:17][cH:18][cH:19][cH:20][c:21]23)[O:22]1)[Cl:23].[CH3:1][NH:2][CH3:3]>>[CH3:1][N:2]([CH3:3])[CH2:4][CH2:5][CH:6]1[CH2:7][N:8]([CH3:9])[C:10](=[S:11])[c:12]2[c:13]([cH:14][cH:15][c:16]3[n:17][cH:18][cH:19][cH:20][c:21]23)[O:2...
CN1CC(CCCl)Oc2ccc3ncccc3c2C1=S.CNC
CN(C)CCC1CN(C)C(=S)c2c(ccc3ncccc23)O1.Cl
null
null
null
Heteroatom Alkylation and Arylation
N-alkylation of secondary amines with alkyl halides
6d58cac08ccced0a33ed16fbca180bc12aa011288d6476106d98a7b2cbc3d709
523d37155b42c8dc851abeddadebb241cdd90bdf649ba750c35e13c8c752d7b0
S=C1NCCOc2ccc3ncccc3c21
[#8:1]-[C:2]-[C:3]-[CH2;D2;+0:4]-[Cl;H0;D1;+0:5].[C;D1;H3:6]-[NH;D2;+0:7]-[C;D1;H3:8]>>[#8:1]-[C:2]-[C:3]-[CH2;D2;+0:4]-[N;H0;D3;+0:7](-[C;D1;H3:6])-[C;D1;H3:8].[ClH;D0;+0:5]
null
[]
null
null
null
null
Following the procedure of Example 31, 4-(2-chloroethyl)-3,4-dihydro-2-methyl-[1,4]-oxazepino[6,7-f]quinoline-1(2H )-thione is reacted with dimethylamine to give the title compound. Conditions: See reaction.notes.procedure_details.
10.6084/m9.figshare.5104873.v1
null
Primary halide.Secondary amine
Tertiary amine
null
null
c1cnc2ccc3c(c2c1)C[NH]CCO3
null
null
null
null
CN1CC(CCCl)Oc2ccc3ncccc3c2C1=S.CNC>>CN(C)CCC1CN(C)C(=S)c2c(ccc3ncccc23)O1.Cl
ord_dataset-01dbb772c5e249108f0b191ed17a2c0c
ord-c507885de2b74b8cbebd94b7d36d5089
CN1CC(CCCl)Oc2c(ccc3cccnc23)C1=S.CNC>>CN(C)CCC1CN(C)C(=S)c2ccc3cccnc3c2O1.Cl
ClCCC1OC2=C(C=CC=3C=CC=NC23)C(N(C1)C)=S.CNC>>Cl.CN(CCC1OC2=C(C=CC=3C=CC=NC23)C(N(C1)C)=S)C
[CH2:4]([CH2:5][CH:6]1[CH2:7][N:8]([CH3:9])[C:10](=[S:11])[c:12]2[cH:13][cH:14][c:15]3[cH:16][cH:17][cH:18][n:19][c:20]3[c:21]2[O:22]1)[Cl:23].[CH3:1][NH:2][CH3:3]>>[CH3:1][N:2]([CH3:3])[CH2:4][CH2:5][CH:6]1[CH2:7][N:8]([CH3:9])[C:10](=[S:11])[c:12]2[cH:13][cH:14][c:15]3[cH:16][cH:17][cH:18][n:19][c:20]3[c:21]2[O:22]1....
CN1CC(CCCl)Oc2c(ccc3cccnc23)C1=S.CNC
CN(C)CCC1CN(C)C(=S)c2ccc3cccnc3c2O1.Cl
null
null
null
Heteroatom Alkylation and Arylation
N-alkylation of secondary amines with alkyl halides
6d58cac08ccced0a33ed16fbca180bc12aa011288d6476106d98a7b2cbc3d709
523d37155b42c8dc851abeddadebb241cdd90bdf649ba750c35e13c8c752d7b0
S=C1NCCOc2c1ccc1cccnc21
[#8:1]-[C:2]-[C:3]-[CH2;D2;+0:4]-[Cl;H0;D1;+0:5].[C;D1;H3:6]-[NH;D2;+0:7]-[C;D1;H3:8]>>[#8:1]-[C:2]-[C:3]-[CH2;D2;+0:4]-[N;H0;D3;+0:7](-[C;D1;H3:6])-[C;D1;H3:8].[ClH;D0;+0:5]
null
[]
null
null
null
null
Following the procedure of Example 31, 2-(2-chloroethyl)-2,3-dihydro-4-methyl-1,4-oxazepino[6,7-h]quinoline-5(4H)-thione is reacted with dimethylamine to give the title compound. Conditions: See reaction.notes.procedure_details.
10.6084/m9.figshare.5104873.v1
null
Primary halide.Secondary amine
Tertiary amine
null
null
c1cnc2c3c(ccc2c1)C[NH]CCO3
null
null
null
null
CN1CC(CCCl)Oc2c(ccc3cccnc23)C1=S.CNC>>CN(C)CCC1CN(C)C(=S)c2ccc3cccnc3c2O1.Cl
ord_dataset-01dbb772c5e249108f0b191ed17a2c0c
ord-f1088ee455db457fb16d426fb9f3ae0f
C1CNC1.CN1CC(CCCl)Oc2ncccc2C1=O.CS(C)=O.O=C([O-])[O-]>>CN1CC(CCN2CCC2)Oc2ncccc2C1=O.O.O=C(O)C(=O)O
N1CCC1.N1CCC1.C([O-])([O-])=O.[K+].[K+].N1CCC1.ClCCC1OC2=C(C(N(C1)C)=O)C=CC=N2.CS(=O)C>>O.C(C(=O)O)(=O)O.N1(CCC1)CCC1OC2=C(C(N(C1)C)=O)C=CC=N2
[NH:7]1[CH2:8][CH2:9][CH2:10]1.Cl[CH2:6][CH2:5][CH:4]1[CH2:3][N:2]([CH3:1])[C:18](=[O:19])[c:17]2[c:12]([n:13][cH:14][cH:15][cH:16]2)[O:11]1.CS([CH3:24])=[O:25].[O-:20][C:22](=[O:21])[O-:23]>>[CH3:1][N:2]1[CH2:3][CH:4]([CH2:5][CH2:6][N:7]2[CH2:8][CH2:9][CH2:10]2)[O:11][c:12]2[n:13][cH:14][cH:15][cH:16][c:17]2[C:18]1=[O...
C1CNC1.CN1CC(CCCl)Oc2ncccc2C1=O.CS(C)=O.O=C([O-])[O-]
CN1CC(CCN2CCC2)Oc2ncccc2C1=O.O.O=C(O)C(=O)O
null
null
null
Acylation
OtherReaction
77dbd28e1d288692e8933194a5fd7d4e881a291f523fe1b9f24a40a476a01050
f282cae9af8040819d24c5fbca643165e020d58516afba86aaf6fb6ad76c90bd
O=C1NCC(CCN2CCC2)Oc2ncccc21
C-S(-[CH3;D1;+0:1])=[O;H0;D1;+0:2].Cl-[CH2;D2;+0:3]-[C:4]-[C:5]-[#8:6].[C:7]1-[C:8]-[C:9]-[NH;D2;+0:10]-1.[O-;H0;D1:11]-[C;H0;D3;+0:12](-[O-;H0;D1:13])=[O;D1;H0:14]>>[#8:6]-[C:5]-[C:4]-[CH2;D2;+0:3]-[N;H0;D3;+0:10]1-[C:7]-[C:8]-[C:9]-1.[O;D1;H0:14]=[C;H0;D3;+0:12](-[OH;D1;+0:13])-[C;H0;D3;+0:1](-[O;D1;H1:15])=[O;H0;D1;...
null
[]
null
null
4
DAY
To a solution of 5.0 g (0.021 mole) of 2-(2-chloroethyl)-2,3-dihydro-4-methylpyrido[3,2-f]-1,4-oxazepin-5(4H)-one dissolved in 40 ml of dimethylsulfoxide was added 8.7 g (0.063 mole) of potassium carbonate followed by 1.40 g (0.025 mole) of azetidine. The mixture was stirred for 4 days at room temperature*. Another 0.5...
10.6084/m9.figshare.5104873.v1
null
Primary halide.Secondary amine.Sulfoxide
Carboxylic acid.Carboxylic acid.Tertiary amine
C1CNC1
C1C[NH]C1
C1C[NH]C1.c1cnc2c(c1)C[NH]CCO2
HCl
null
null
96
C1CNC1.CN1CC(CCCl)Oc2ncccc2C1=O.CS(C)=O.O=C([O-])[O-]>>CN1CC(CCN2CCC2)Oc2ncccc2C1=O.O.O=C(O)C(=O)O
ord_dataset-01dbb772c5e249108f0b191ed17a2c0c
ord-cad802f8607b497e826f6484b8b5dd8e
C1CNC1.C1CNC1.CN1CC(CCCl)Oc2ncccc2C1=S.CS(C)=O.O=C([O-])[O-]>>CN1CC(CCN2CCC2)Oc2ncccc2C1=S.O=C(O)/C=C/C(=O)O
N1CCC1.C([O-])([O-])=O.[K+].[K+].N1CCC1.ClCCC1OC2=C(C(N(C1)C)=S)C=CC=N2.CS(=O)C.N1CCC1>>C(\C=C\C(=O)O)(=O)O.N1(CCC1)CCC1OC2=C(C(N(C1)C)=S)C=CC=N2
[NH:7]1[CH2:8][CH2:9][CH2:10]1.C1NC[CH2:24]1.Cl[CH2:6][CH2:5][CH:4]1[CH2:3][N:2]([CH3:1])[C:18](=[S:19])[c:17]2[c:12]([n:13][cH:14][cH:15][cH:16]2)[O:11]1.S(=[O:20])([CH3:21])[CH3:23].[O-:22][C:25](=[O:26])[O-:27]>>[CH3:1][N:2]1[CH2:3][CH:4]([CH2:5][CH2:6][N:7]2[CH2:8][CH2:9][CH2:10]2)[O:11][c:12]2[n:13][cH:14][cH:15][...
C1CNC1.C1CNC1.CN1CC(CCCl)Oc2ncccc2C1=S.CS(C)=O.O=C([O-])[O-]
CN1CC(CCN2CCC2)Oc2ncccc2C1=S.O=C(O)/C=C/C(=O)O
null
null
null
C-C Coupling
OtherReaction
e6d9413339adaed3fb86a9b94839ebff98c94748362bf95d66420eca04c8c043
6716722ac7a12289371f78fe0a6508251281db471213d1dc2f1737480cf9e159
S=C1NCC(CCN2CCC2)Oc2ncccc21
C1-N-C-[CH2;D2;+0:1]-1.Cl-[CH2;D2;+0:2]-[C:3]-[C:4]-[#8:5].[CH3;D1;+0:6]-S(-[CH3;D1;+0:7])=[O;H0;D1;+0:8].[C:9]1-[C:10]-[C:11]-[NH;D2;+0:12]-1.[O-;H0;D1:13]-[C;H0;D3;+0:14](-[O-;H0;D1:15])=[O;D1;H0:16]>>[#8:5]-[C:4]-[C:3]-[CH2;D2;+0:2]-[N;H0;D3;+0:12]1-[C:9]-[C:10]-[C:11]-1.[O;D1;H0:16]=[C;H0;D3;+0:14](-[OH;D1;+0:15])/...
31
[{"value": 31.0, "product": "C(\\C=C\\C(=O)O)(=O)O.N1(CCC1)CCC1OC2=C(C(N(C1)C)=S)C=CC=N2", "details": "PERCENTYIELD", "is_desired": false}]
null
null
8
HOUR
To 5.0 g (0.0914 mole) of 2-(2-chloroethyl)-2,5-dihydro-4-methylpyrido[3,2-f]-1,4-oxazepine-5(4H)-thione dissolved in 50 ml of dimethylsulfoxide was added 8.04 g (0.058 mole) of potassium carbonate and 1.21 g (0.021 mole) of azetidine. The reaction mixture was stirred at room temperature for 8 hr after which was added ...
10.6084/m9.figshare.5104873.v1
null
Primary halide.Secondary amine.Secondary amine.Sulfoxide
Carboxylic acid.Carboxylic acid.Tertiary amine
C1CNC1.C1CNC1
C1C[NH]C1
C1C[NH]C1.c1cnc2c(c1)C[NH]CCO2
HCl
null
null
8
C1CNC1.C1CNC1.CN1CC(CCCl)Oc2ncccc2C1=S.CS(C)=O.O=C([O-])[O-]>>CN1CC(CCN2CCC2)Oc2ncccc2C1=S.O=C(O)/C=C/C(=O)O
ord_dataset-01dbb772c5e249108f0b191ed17a2c0c
ord-f16fdd29c044474da886cbfb04a2815b
CCNCC.CCOC(C)=O.CN1CC(CCCl)Oc2ncc(Cl)cc2C1=O.CO.[OH-]>>CCN(CC)CCC1CN(C)C(=O)c2cc(Cl)cnc2O1.O=C(O)C(=O)O
C(C)OC(C)=O.CO.C(C)NCC.C(C)NCC.C(C)NCC.[OH-].[NH4+].ClC1=CC=2C(N(CC(OC2N=C1)CCCl)C)=O>>C(C(=O)O)(=O)O.ClC1=CC=2C(N(CC(OC2N=C1)CCN(CC)CC)C)=O
[CH3:1][CH2:2][NH:3][CH2:4][CH3:5].CC[O:27][C:25]([CH3:23])=[O:26].Cl[CH2:6][CH2:7][CH:8]1[CH2:9][N:10]([CH3:11])[C:12](=[O:13])[c:14]2[cH:15][c:16]([Cl:17])[cH:18][n:19][c:20]2[O:21]1.C[OH:22].[OH-:24]>>[CH3:1][CH2:2][N:3]([CH2:4][CH3:5])[CH2:6][CH2:7][CH:8]1[CH2:9][N:10]([CH3:11])[C:12](=[O:13])[c:14]2[cH:15][c:16]([...
CCNCC.CCOC(C)=O.CN1CC(CCCl)Oc2ncc(Cl)cc2C1=O.CO.[OH-]
CCN(CC)CCC1CN(C)C(=O)c2cc(Cl)cnc2O1.O=C(O)C(=O)O
null
null
C(C)O
Acylation
OtherReaction
348c2faf84980bee9a4ac0d2546d922eeb25e7f323783ef33bbdb080267b5569
8c7a5897958746e817096e691bd5a0eaed0fcdfc28d5444735c68f8fbc5b17f6
O=C1NCCOc2ncccc21
C-C-[O;H0;D2;+0:1]-[C:2](-[CH3;D1;+0:3])=[O;D1;H0:4].C-[OH;D1;+0:5].Cl-[CH2;D2;+0:6]-[C:7]-[C:8]-[#8:9].[C;D1;H3:10]-[C:11]-[NH;D2;+0:12]-[C:13]-[C;D1;H3:14].[OH-;D0:15]>>[#8:9]-[C:8]-[C:7]-[CH2;D2;+0:6]-[N;H0;D3;+0:12](-[C:11]-[C;D1;H3:10])-[C:13]-[C;D1;H3:14].[O;D1;H0:4]=[C:2](-[OH;D1;+0:1])-[C;H0;D3;+0:3](=[O;H0;D1;...
76
[{"value": 76.0, "product": "C(C(=O)O)(=O)O.ClC1=CC=2C(N(CC(OC2N=C1)CCN(CC)CC)C)=O", "details": "PERCENTYIELD", "is_desired": false}]
null
null
1
HOUR
To a suspension of 7-chloro-2-(2-chloroethyl)-2,3-dihydro-4-methylpyrido[3,2-f][1,4]oxazepine-5(4H)-one in 50 ml of absolute ethanol was added 2.26 ml (0.022 mole) of diethylamine and the mixture heated to reflux. (Complete dissolution occurred). After 1 hr, another 2.26 ml (0.022 mole) of diethylamine was added follow...
10.6084/m9.figshare.5104873.v1
null
Primary halide.Ester.Secondary amine.Methanol
Carboxylic acid.Carboxylic acid.Tertiary amine
null
null
c1cnc2c(c1)C[NH]CCO2
HCl
C(C)O
null
1
CCNCC.CCOC(C)=O.CN1CC(CCCl)Oc2ncc(Cl)cc2C1=O.CO.[OH-]>C(C)O>CCN(CC)CCC1CN(C)C(=O)c2cc(Cl)cnc2O1.O=C(O)C(=O)O
ord_dataset-01dbb772c5e249108f0b191ed17a2c0c
ord-c8d4455c6b164a84bffaf46314b5819e
C1CNC1.C1CNC1.CN1CC(CCCl)Oc2ncc(Cl)cc2C1=O.O=C([O-])[O-].[OH-]>>CN1CC(CCN2CCC2)Oc2ncc(Cl)cc2C1=O.O=C(O)C(=O)O
N1CCC1.[OH-].[NH4+].N1CCC1.ClC1=CC=2C(N(CC(OC2N=C1)CCCl)C)=O.C([O-])([O-])=O.[K+].[K+].N1CCC1>>C(C(=O)O)(=O)O.N1(CCC1)CCC1OC2=C(C(N(C1)C)=O)C=C(C=N2)Cl
[NH:7]1[CH2:8][CH2:9][CH2:10]1.C1NC[CH2:22]1.Cl[CH2:6][CH2:5][CH:4]1[CH2:3][N:2]([CH3:1])[C:19](=[O:20])[c:18]2[c:12]([n:13][cH:14][c:15]([Cl:16])[cH:17]2)[O:11]1.[O-:21][C:24](=[O:25])[O-:26].[OH-:23]>>[CH3:1][N:2]1[CH2:3][CH:4]([CH2:5][CH2:6][N:7]2[CH2:8][CH2:9][CH2:10]2)[O:11][c:12]2[n:13][cH:14][c:15]([Cl:16])[cH:1...
C1CNC1.C1CNC1.CN1CC(CCCl)Oc2ncc(Cl)cc2C1=O.O=C([O-])[O-].[OH-]
CN1CC(CCN2CCC2)Oc2ncc(Cl)cc2C1=O.O=C(O)C(=O)O
null
null
CS(=O)C.CO.O.C(C)(=O)OCC
Acylation
OtherReaction
d65171afcf06fb0b281bb4e97894cbaf6fd8db7060487fd5c137c059ce31ba9c
c1d2c5ce311472318c38226bdf9a6dc42cc459acce751b23151f36da42111bd5
O=C1NCC(CCN2CCC2)Oc2ncccc21
C1-N-C-[CH2;D2;+0:1]-1.Cl-[CH2;D2;+0:2]-[C:3]-[C:4]-[#8:5].[C:6]1-[C:7]-[C:8]-[NH;D2;+0:9]-1.[O-;H0;D1:10]-[C;H0;D3;+0:11](-[O-;H0;D1:12])=[O;D1;H0:13].[OH-;D0:14]>>[#8:5]-[C:4]-[C:3]-[CH2;D2;+0:2]-[N;H0;D3;+0:9]1-[C:6]-[C:7]-[C:8]-1.[O;D1;H0:13]=[C;H0;D3;+0:11](-[OH;D1;+0:12])-[C;H0;D3;+0:1](=[O;H0;D1;+0:10])-[OH;D1;+...
null
[]
null
null
24
HOUR
To a solution of 6 g (0.022 mole) of 7-chloro-2-(2-chloroethyl)-2,3-dihydro-4-methylpyrido[3,2-f][1,4]-oxazepine-5(4H)-one in 40 ml of dimethyl sulfoxide was added 8.0 g of crushed potassium carbonate and 1.5 g (0.026 mole) of azetidine. The reaction was stirred at room temperature for 24 hr. After checking ty TLC [7:2...
10.6084/m9.figshare.5104873.v1
null
Primary halide.Secondary amine.Secondary amine
Carboxylic acid.Carboxylic acid.Tertiary amine
C1CNC1.C1CNC1
C1C[NH]C1
C1C[NH]C1.c1cnc2c(c1)C[NH]CCO2
HCl
CS(=O)C.CO.O.C(C)(=O)OCC
null
24
C1CNC1.C1CNC1.CN1CC(CCCl)Oc2ncc(Cl)cc2C1=O.O=C([O-])[O-].[OH-]>CS(=O)C.CO.O.C(C)(=O)OCC>CN1CC(CCN2CCC2)Oc2ncc(Cl)cc2C1=O.O=C(O)C(=O)O
ord_dataset-01dbb772c5e249108f0b191ed17a2c0c
ord-c3bc64bc129e484f957dfe469d616691
CN1CC(CCCl)Oc2ncc(Cl)cc2C1=O.NCCc1ccccc1.NCCc1ccccc1>>Cc1ccccc1CNC1CN(C)C(=O)c2cc(Cl)cnc2O1
C(C1=CC=CC=C1)CN.C(C(=O)O)(=O)O.ClC1=CC=2C(N(CC(OC2N=C1)CCCl)C)=O.C(C1=CC=CC=C1)CN>>C(C(=O)O)(=O)O.ClC1=CC=2C(N(CC(OC2N=C1)NCC1=C(C=CC=C1)C)C)=O
ClCC[CH:10]1[CH2:11][N:12]([CH3:13])[C:14](=[O:15])[c:16]2[cH:17][c:18]([Cl:19])[cH:20][n:21][c:22]2[O:23]1.NC[CH2:8][c:7]1[cH:2][cH:3][cH:4][cH:5][cH:6]1.c1ccc([CH2:1]C[NH2:9])cc1>>[CH3:1][c:2]1[cH:3][cH:4][cH:5][cH:6][c:7]1[CH2:8][NH:9][CH:10]1[CH2:11][N:12]([CH3:13])[C:14](=[O:15])[c:16]2[cH:17][c:18]([Cl:19])[cH:20...
CN1CC(CCCl)Oc2ncc(Cl)cc2C1=O.NCCc1ccccc1.NCCc1ccccc1
Cc1ccccc1CNC1CN(C)C(=O)c2cc(Cl)cnc2O1
null
null
C(C)O.C(C)(C)O
Heteroatom Alkylation and Arylation
OtherReaction
f4b44215ead1d0438d2bf11d21ce9c6f45fc759030e2e06357806e7c7da491fc
0ee453ae46d68daf31d23066ef30b155c941f69bce1acdf87c9465ca7ffc7607
O=C1NCC(NCc2ccccc2)Oc2ncccc21
Cl-C-C-[CH;D3;+0:1](-[#8:2]-[c:3]:[#7;a:4])-[C:5]-[#7:6](-[C;D1;H3:7])-[C:8]=[O;D1;H0:9].N-C-[CH2;D2;+0:10]-[c:11](:[c:12]):[cH;D2;+0:13]:[c:14]:[c:15].[NH2;D1;+0:16]-C-[CH2;D2;+0:17]-c1:c:c:c:c:c:1>>[#7;a:4]:[c:3]-[#8:2]-[CH;D3;+0:1](-[NH;D2;+0:16]-[CH2;D2;+0:10]-[c:11](:[c:12]):[c;H0;D3;+0:13](-[CH3;D1;+0:17]):[c:14]...
47.9
[{"value": 47.9, "product": "C(C(=O)O)(=O)O.ClC1=CC=2C(N(CC(OC2N=C1)NCC1=C(C=CC=C1)C)C)=O", "details": "PERCENTYIELD", "is_desired": false}]
null
null
null
null
To a solution of 6.0 g (0.022 mole) of 7-chloro-2-(2-chloroethyl)-2,3-dihydro-4-methylpyrido[3,2-f][1,4]-oxazepine-5(4H)-one in 50 ml of absolute ethanol was added 5.3 g (0.044 mole) of benzylmethylamine and the mixture heated to reflux for three days. The solvent was removed by rotary evaporation, and the residue was ...
10.6084/m9.figshare.5104873.v1
null
Primary halide.Ether.Primary amine.Primary amine
Ether.Secondary amine
c1cnc2c(c1)C[NH]CCO2.c1ccccc1.c1ccccc1
c1ccccc1.c1cnc2c(c1)C[NH]CCO2
c1ccccc1.c1cnc2c(c1)C[NH]CCO2
HCl
C(C)O.C(C)(C)O
null
null
CN1CC(CCCl)Oc2ncc(Cl)cc2C1=O.NCCc1ccccc1.NCCc1ccccc1>C(C)O.C(C)(C)O>Cc1ccccc1CNC1CN(C)C(=O)c2cc(Cl)cnc2O1
ord_dataset-01dbb772c5e249108f0b191ed17a2c0c
ord-708edbb82c3846ab9c16f701e9c84890
C1CNC1.CN1CC(CCCl)Oc2ncc(Cl)cc2C1=S.CS(C)=O.O=C([O-])[O-]>>CN1CC(CCN2CCC2)Oc2ncc(Cl)cc2C1=S.O=C(O)C(=O)O
N1CCC1.N1CCC1.ClC1=CC=2C(N(CC(OC2N=C1)CCCl)C)=S.C([O-])([O-])=O.[K+].[K+].N1CCC1.CS(=O)C>>C(C(=O)O)(=O)O.N1(CCC1)CCC1OC2=C(C(N(C1)C)=S)C=C(C=N2)Cl
[NH:7]1[CH2:8][CH2:9][CH2:10]1.Cl[CH2:6][CH2:5][CH:4]1[CH2:3][N:2]([CH3:1])[C:19](=[S:20])[c:18]2[c:12]([n:13][cH:14][c:15]([Cl:16])[cH:17]2)[O:11]1.CS([CH3:24])=[O:25].[O:21]=[C:22]([O-:23])[O-:26]>>[CH3:1][N:2]1[CH2:3][CH:4]([CH2:5][CH2:6][N:7]2[CH2:8][CH2:9][CH2:10]2)[O:11][c:12]2[n:13][cH:14][c:15]([Cl:16])[cH:17][...
C1CNC1.CN1CC(CCCl)Oc2ncc(Cl)cc2C1=S.CS(C)=O.O=C([O-])[O-]
CN1CC(CCN2CCC2)Oc2ncc(Cl)cc2C1=S.O=C(O)C(=O)O
null
null
O
Acylation
OtherReaction
77dbd28e1d288692e8933194a5fd7d4e881a291f523fe1b9f24a40a476a01050
f282cae9af8040819d24c5fbca643165e020d58516afba86aaf6fb6ad76c90bd
S=C1NCC(CCN2CCC2)Oc2ncccc21
C-S(-[CH3;D1;+0:1])=[O;H0;D1;+0:2].Cl-[CH2;D2;+0:3]-[C:4]-[C:5]-[#8:6].[C:7]1-[C:8]-[C:9]-[NH;D2;+0:10]-1.[O-;H0;D1:11]-[C;H0;D3;+0:12](-[O-;H0;D1:13])=[O;D1;H0:14]>>[#8:6]-[C:5]-[C:4]-[CH2;D2;+0:3]-[N;H0;D3;+0:10]1-[C:7]-[C:8]-[C:9]-1.[O;D1;H0:14]=[C;H0;D3;+0:12](-[OH;D1;+0:11])-[C;H0;D3;+0:1](=[O;H0;D1;+0:2])-[OH;D1;...
82
[{"value": 82.0, "product": "C(C(=O)O)(=O)O.N1(CCC1)CCC1OC2=C(C(N(C1)C)=S)C=C(C=N2)Cl", "details": "PERCENTYIELD", "is_desired": false}]
null
null
24
HOUR
To a solution of 4.75 g (0.0164 mole) of 7-chloro-2-(2-chloroethyl)-2,3-dihydro-4-methylpyrido[3,2-f]-1,4-oxazepine-5(4H)-thione in 40 ml of dimethyl sulfoxide was added 8.0 g of crushed potassium carbonate and 1.4 g (0.0246 mole) of azetidine. The flask was sealed and stirred at room temperature for 24 hr after which ...
10.6084/m9.figshare.5104873.v1
null
Primary halide.Secondary amine.Sulfoxide
Carboxylic acid.Carboxylic acid.Tertiary amine
C1CNC1
C1C[NH]C1
C1C[NH]C1.c1cnc2c(c1)C[NH]CCO2
HCl
O
null
24
C1CNC1.CN1CC(CCCl)Oc2ncc(Cl)cc2C1=S.CS(C)=O.O=C([O-])[O-]>O>CN1CC(CCN2CCC2)Oc2ncc(Cl)cc2C1=S.O=C(O)C(=O)O
ord_dataset-01dbb772c5e249108f0b191ed17a2c0c
ord-ba780da7ad95459898e6dbacd6e9e38a
CNC.Cc1ccc2c(n1)OC(CCCl)CN(C)C2=O>>Cc1ccc2c(n1)OC(CCN(C)C)CN(C)C2=O
CNC.O.ClCCC1OC2=C(C(N(C1)C)=O)C=CC(=N2)C.C(\C=C\C(=O)O)(=O)O>>C(\C=C\C(=O)O)(=O)O.CN(CCC1OC2=C(C(N(C1)C)=O)C=CC(=N2)C)C
[NH:12]([CH3:13])[CH3:14].Cl[CH2:11][CH2:10][CH:9]1[O:8][c:6]2[c:5]([cH:4][cH:3][c:2]([CH3:1])[n:7]2)[C:18](=[O:19])[N:16]([CH3:17])[CH2:15]1>>[CH3:1][c:2]1[cH:3][cH:4][c:5]2[c:6]([n:7]1)[O:8][CH:9]([CH2:10][CH2:11][N:12]([CH3:13])[CH3:14])[CH2:15][N:16]([CH3:17])[C:18]2=[O:19]
CNC.Cc1ccc2c(n1)OC(CCCl)CN(C)C2=O
Cc1ccc2c(n1)OC(CCN(C)C)CN(C)C2=O
null
null
C(C)(C)O
Heteroatom Alkylation and Arylation
N-alkylation of secondary amines with alkyl halides
6d58cac08ccced0a33ed16fbca180bc12aa011288d6476106d98a7b2cbc3d709
523d37155b42c8dc851abeddadebb241cdd90bdf649ba750c35e13c8c752d7b0
O=C1NCCOc2ncccc21
Cl-[CH2;D2;+0:1]-[C:2]-[C:3]-[#8:4].[C;D1;H3:5]-[NH;D2;+0:6]-[C;D1;H3:7]>>[#8:4]-[C:3]-[C:2]-[CH2;D2;+0:1]-[N;H0;D3;+0:6](-[C;D1;H3:5])-[C;D1;H3:7]
null
[]
null
null
3
DAY
To 50 ml of freshly collected dimethylamine was added 5.0 g (0.020 mole) of 2-(2-chloroethyl)-2,3-dihydro-4,8-dimethylpyrido[3,2-f]-1,4-oxazepin-5(4H)-one hydrate [1:1]. The reaction flask was sealed tightly and left standing at room temperature for 3 days. The dimethylamine was evaporated in a stream of air. The resid...
10.6084/m9.figshare.5104873.v1
null
Primary halide.Secondary amine
Tertiary amine
null
null
c1cnc2c(c1)C[NH]CCO2
HCl
C(C)(C)O
null
72
CNC.Cc1ccc2c(n1)OC(CCCl)CN(C)C2=O>C(C)(C)O>Cc1ccc2c(n1)OC(CCN(C)C)CN(C)C2=O
ord_dataset-01dbb772c5e249108f0b191ed17a2c0c
ord-f1df6ffd3002451e8e3a249fd7ae56eb
CN1CC(CCCl)Oc2ccc([N+](=O)[O-])cc2C1=S.CNC>>CN(C)CCC1CN(C)C(=S)c2cc([N+](=O)[O-])ccc2O1
CNC.ClCCC1OC2=C(C(N(C1)C)=S)C=C(C=C2)[N+](=O)[O-]>>CN(CCC1OC2=C(C(N(C1)C)=S)C=C(C=C2)[N+](=O)[O-])C
Cl[CH2:4][CH2:5][CH:6]1[CH2:7][N:8]([CH3:9])[C:10](=[S:11])[c:12]2[cH:13][c:14]([N+:15](=[O:16])[O-:17])[cH:18][cH:19][c:20]2[O:21]1.[CH3:1][NH:2][CH3:3]>>[CH3:1][N:2]([CH3:3])[CH2:4][CH2:5][CH:6]1[CH2:7][N:8]([CH3:9])[C:10](=[S:11])[c:12]2[cH:13][c:14]([N+:15](=[O:16])[O-:17])[cH:18][cH:19][c:20]2[O:21]1
CN1CC(CCCl)Oc2ccc([N+](=O)[O-])cc2C1=S.CNC
CN(C)CCC1CN(C)C(=S)c2cc([N+](=O)[O-])ccc2O1
null
null
null
Heteroatom Alkylation and Arylation
N-alkylation of secondary amines with alkyl halides
6d58cac08ccced0a33ed16fbca180bc12aa011288d6476106d98a7b2cbc3d709
523d37155b42c8dc851abeddadebb241cdd90bdf649ba750c35e13c8c752d7b0
S=C1NCCOc2ccccc21
Cl-[CH2;D2;+0:1]-[C:2]-[C:3]-[#8:4].[C;D1;H3:5]-[NH;D2;+0:6]-[C;D1;H3:7]>>[#8:4]-[C:3]-[C:2]-[CH2;D2;+0:1]-[N;H0;D3;+0:6](-[C;D1;H3:5])-[C;D1;H3:7]
null
[]
null
null
6
DAY
To 50 ml of freshly collected dimethylamine was added 4.25 g (0.014 mole) of 2-(2-chloroethyl)-2,3-dihydro-4-methyl-7-nitro-1,4-benzoxazepine-5(4H)-thione. The reaction flask was sealed tightly and allowed to stand at room temperature for 6 days. The dimethylamine was evaporated at room temperature. The solid residue w...
10.6084/m9.figshare.5104873.v1
null
Primary halide.Secondary amine
Tertiary amine
null
null
c1ccc2c(c1)C[NH]CCO2
HCl
null
null
144
CN1CC(CCCl)Oc2ccc([N+](=O)[O-])cc2C1=S.CNC>>CN(C)CCC1CN(C)C(=S)c2cc([N+](=O)[O-])ccc2O1
ord_dataset-02ee2261663048188cf6d85d2cc96e3f
ord-e7162987fc5047f0bed022391e7a5186
O=S(=O)=O>>O=S(=O)=O
S(=O)(=O)=O.S(O)(O)(=O)=O>>OS(=O)(=O)O.O=S(=O)=O
[O:6]=[S:7](=[O:8])=[O:9]>>[O:6]=[S:7](=[O:8])=[O:9]
O=S(=O)=O
O=S(=O)=O
null
null
null
Miscellaneous
OtherReaction
40ba59785861b8226ce5af6bdcbb9a37f0ff50a8c7ec7d4fc4c524cf906cc65c
56ebed4a8b3cebec83c37a71d68f0c87d1e404ab05a9ce792691e4e18a2379dd
null
null
null
[]
null
null
null
null
FIG. 7 depicts a subunit for sulfuric acid. Liquid sulfur dioxide is supplied by a cylinder 121 to a fractionating column 122 and then to a membrane filter 123. The purified sulfur dioxide gas is then fed to a catalytic oxidizer 124 where it is combined with purified air 125 over a platinum or other suitable catalyst t...
10.6084/m9.figshare.5104873.v1
null
null
null
null
null
null
null
null
null
null
O=S(=O)=O>>O=S(=O)=O
ord_dataset-02ee2261663048188cf6d85d2cc96e3f
ord-be3efbcf3dc141dc81dfa55a22b25b70
O=C([O-])C1=NN(c2ccc(S(=O)(=O)[O-])cc2)C(=O)C1N=Nc1ccc(S(=O)(=O)[O-])cc1>>O=C1CCCN1C1CCCCC1
C1=CC(=CC=C1N=NC2C(=NN(C2=O)C3=CC=C(C=C3)S(=O)(=O)[O-])C(=O)[O-])S(=O)(=O)[O-].[Na+].[Na+].[Na+]>>C1(CCCCC1)N1C(CCC1)=O
O=S(=O)([O-])c1ccc(N=N[CH:3]2[C:2](=[O:1])[N:6]([c:7]3[cH:8][cH:9][c:10](S(=O)(=O)[O-])[cH:11][cH:12]3)N=[C:4]2[C:5](=O)[O-])cc1>>[O:1]=[C:2]1[CH2:3][CH2:4][CH2:5][N:6]1[CH:7]1[CH2:8][CH2:9][CH2:10][CH2:11][CH2:12]1
O=C([O-])C1=NN(c2ccc(S(=O)(=O)[O-])cc2)C(=O)C1N=Nc1ccc(S(=O)(=O)[O-])cc1
O=C1CCCN1C1CCCCC1
null
null
O
Miscellaneous
OtherReaction
48fd1a31d28002a4a8a1da1390fdad3f28d5625ad662f2c858b26fe70ce4c78e
0b540714ee81d30a708af2c8e77ca9cf57ebbc61ca67680c6d13b9905ab53e84
O=C1CCCN1C1CCCCC1
O=[C;H0;D3;+0:1](-[O-])-[C;H0;D3;+0:2]1=N-[N;H0;D3;+0:3](-[c;H0;D3;+0:4]2:[cH;D2;+0:5]:[cH;D2;+0:6]:[c;H0;D3;+0:7](-S(=O)(=O)-[O-]):[cH;D2;+0:8]:[cH;D2;+0:9]:2)-[C:10](=[O;D1;H0:11])-[CH;D3;+0:12]-1-N=N-c1:c:c:c(-S(=O)(=O)-[O-]):c:c:1>>[O;D1;H0:11]=[C:10]1-[CH2;D2;+0:12]-[CH2;D2;+0:2]-[CH2;D2;+0:1]-[N;H0;D3;+0:3]-1-[CH...
null
[]
null
null
null
null
An ink composition comprising 2.5 percent by weight of Tartrazine FD&C Yellow #5, a yellow dye obtained from Buffalo Color, West Patterson, N.Y., 15 percent by weight of cyclohexyl pyrrolidone (obtained from GAF Corporation, Wayne, N.J.), and 82.5 percent by weight of deionized water was prepared by mixing together the...
10.6084/m9.figshare.5104873.v1
null
Hydrazone amide.Diazene.Sulfonic acid.Sulfonic acid
Tertiary amide
c1ccccc1.C1=N[NH]CC1.c1ccccc1
C1CC[NH]C1.C1CCCCC1
C1CC[NH]C1.C1CCCCC1
Other
O
null
null
O=C([O-])C1=NN(c2ccc(S(=O)(=O)[O-])cc2)C(=O)C1N=Nc1ccc(S(=O)(=O)[O-])cc1>O>O=C1CCCN1C1CCCCC1
ord_dataset-02ee2261663048188cf6d85d2cc96e3f
ord-b1f4a5001bb04225b37898725e06c20d
CC(C)CC(C)O.Cc1ccccc1.OB(O)O>>CC(C)CC(C)OB(OC(C)CC(C)C)OC(C)CC(C)C
CC(CC(C)O)C.C1(=CC=CC=C1)C.B(O)(O)O>>B(OC(C)CC(C)C)(OC(C)CC(C)C)OC(C)CC(C)C
[CH3:12][CH:13]([CH3:15])[CH2:19][CH:17]([OH:16])[CH3:18].[cH:1]1[cH:6][cH:5][cH:4][cH:2][c:10]1[CH3:11].O[B:8]([OH:7])[OH:9]>>[CH3:1][CH:2]([CH3:3])[CH2:4][CH:5]([CH3:6])[O:7][B:8]([O:9][CH:10]([CH3:11])[CH2:12][CH:13]([CH3:14])[CH3:15])[O:16][CH:17]([CH3:18])[CH2:19][CH:20]([CH3:21])[CH3:22]
CC(C)CC(C)O.Cc1ccccc1.OB(O)O
CC(C)CC(C)OB(OC(C)CC(C)C)OC(C)CC(C)C
null
null
O
C-C Coupling
OtherReaction
b0a8c44e3cf48ea1069e1a9c1beb6ed937cd51bf99523fdf580607d9cbf59326
7ccf8a4ec454d6cc03ce1e3efafa301b3c51d9e9635279e99312f4bc816939b8
null
O-[B;H0;D3;+0:1](-[OH;D1;+0:2])-[OH;D1;+0:3].[C;D1;H3:4]-[CH;D3;+0:5](-[CH3;D1;+0:6])-[CH2;D2;+0:7]-[C:8](-[C;D1;H3:9])-[OH;D1;+0:10].[C;D1;H3:11]-[c;H0;D3;+0:12]1:[cH;D2;+0:13]:[cH;D2;+0:14]:[cH;D2;+0:15]:[cH;D2;+0:16]:[cH;D2;+0:17]:1>>[C;D1;H3:11]-[CH;D3;+0:12](-[CH2;D2;+0:6]-[CH;D3;+0:5](-[C;D1;H3:18])-[C;D1;H3:4])-...
null
[]
null
null
null
null
Approximately 306 grams of 4-methyl-2-pentanol, 100 grams of toluene, and 62 grams of boric acid were charged to a 2-liter glass reactor having an inert nitrogen atmosphere and equipped with heater, agitator, and Dean-Stark tube with condenser. The reactants were heated up to about 155° C. for a period of about 5 hours...
10.6084/m9.figshare.5104873.v1
null
Secondary alcohol
null
c1ccccc1
null
null
null
O
null
null
CC(C)CC(C)O.Cc1ccccc1.OB(O)O>O>CC(C)CC(C)OB(OC(C)CC(C)C)OC(C)CC(C)C
ord_dataset-02ee2261663048188cf6d85d2cc96e3f
ord-c1c07a48db7345b6a7f46b1de4eb0229
CCCCCCC(O)CCCCCCCCCCC(=O)O>>CCCCCCCCCCCCCCCCC(O)C(=O)[O-]
OC(CCCCCCCCCCC(=O)O)CCCCCC.[P].[S].[OH-].[Li+]>>OC(C(=O)[O-])CCCCCCCCCCCCCCCC.[Li+]
[CH3:1][CH2:2][CH2:3][CH2:4][CH2:5][CH2:6][CH:7]([CH2:8][CH2:9][CH2:10][CH2:11][CH2:12][CH2:13][CH2:14][CH2:15][CH2:16][CH2:17][C:19](=[O:20])[OH:21])[OH:18]>>[CH3:1][CH2:2][CH2:3][CH2:4][CH2:5][CH2:6][CH2:7][CH2:8][CH2:9][CH2:10][CH2:11][CH2:12][CH2:13][CH2:14][CH2:15][CH2:16][CH:17]([OH:18])[C:19](=[O:20])[O-:21]
CCCCCCC(O)CCCCCCCCCCC(=O)O
CCCCCCCCCCCCCCCCC(O)C(=O)[O-]
null
null
null
Functional Group Interconversion
OtherReaction
9902cbf33697a1170a2502a73f5637431b7f1ab9f5d17966da97f339e3fc8c0d
54cb95a546ba1fa58e84d50759a385f2264699bea86ea1ae67a3fdfe781ce107
null
[C:1]-[C:2]-[CH2;D2;+0:3]-[C:4](=[O;D1;H0:5])-[OH;D1;+0:6].[C:7]-[C:8]-[CH;D3;+0:9](-[OH;D1;+0:10])-[C:11]-[C:12]>>[C:7]-[C:8]-[CH2;D2;+0:9]-[C:11]-[C:12].[C:1]-[C:2]-[CH;D3;+0:3](-[OH;D1;+0:10])-[C:4](-[O-;H0;D1:6])=[O;D1;H0:5]
null
[]
null
null
null
null
A lithium hydroxystearate grease thickener was prepared by saponification of a mixture containing 12-hydroxystearic acid (50%) and the tri-glyceride thereof (25%) and 25% of C22 fatty acids containing no OH groups with lithium hydroxide in a mineral oil vehicle (ISO 150 viscosity grade of a 70/30 mixture of naphthenic ...
10.6084/m9.figshare.5104873.v1
null
Carboxylic acid.Secondary alcohol
Secondary alcohol
null
null
null
null
null
null
null
CCCCCCC(O)CCCCCCCCCCC(=O)O>>CCCCCCCCCCCCCCCCC(O)C(=O)[O-]
ord_dataset-02ee2261663048188cf6d85d2cc96e3f
ord-c11e140ba9cd45de8bbf75d1cbd64d0a
C#Cc1ccc(OCC)cc1.Fc1ccc(I)cc1F>>CCOc1ccc(C#Cc2ccc(F)c(F)c2)cc1
C(C)OC1=CC=C(C=C1)C#C.FC=1C=C(C=CC1F)I.C(C)N(CC)CC>>FC=1C=C(C=CC1F)C#CC1=CC=C(C=C1)OCC
[CH3:1][CH2:2][O:3][c:4]1[cH:5][cH:6][c:7]([C:8]#[CH:9])[cH:18][cH:19]1.I[c:10]1[cH:11][cH:12][c:13]([F:14])[c:15]([F:16])[cH:17]1>>[CH3:1][CH2:2][O:3][c:4]1[cH:5][cH:6][c:7]([C:8]#[C:9][c:10]2[cH:11][cH:12][c:13]([F:14])[c:15]([F:16])[cH:17]2)[cH:18][cH:19]1
C#Cc1ccc(OCC)cc1.Fc1ccc(I)cc1F
CCOc1ccc(C#Cc2ccc(F)c(F)c2)cc1
null
Cl[Pd]([P](C1=CC=CC=C1)(C2=CC=CC=C2)C3=CC=CC=C3)([P](C4=CC=CC=C4)(C5=CC=CC=C5)C6=CC=CC=C6)Cl.[Cu]I
C(C)(C)(C)OC
C-C Coupling
Sonogashira alkyne_aryl halide
15c08902746c61a960c314898ce6bb5fcc5e189f9e057388c59dba9ec9d0c81c
305eca0fd2975da49e7f69e4edfb9dc1cbce82513954bc5a73be3289e70e5f76
C(#Cc1ccccc1)c1ccccc1
I-[c;H0;D3;+0:1](:[c:2]:[c:3]):[c:4]:[c:5].[CH;D1;+0:6]#[C:7]-[c:8]>>[c:3]:[c:2]:[c;H0;D3;+0:1](-[C;H0;D2;+0:6]#[C:7]-[c:8]):[c:4]:[c:5]
null
[]
null
null
2
HOUR
0.4 mmol of bis(triphenylphosphine)palladium(II) chloride and 0.2 mmol of CuI are added at room temperature to a mixture of 0.02 m of 4-ethoxyphenylacetylene, 0.02 m of 3,4-difluoroiodobenzene and 50 ml of triethylamine. The reaction mixture is stirred at room temperature for 2 hours, diluted with 100 ml of methyl tert...
10.6084/m9.figshare.5104873.v1
null
Aromatic halide.Alkyne
Alkyne
c1ccccc1
c1ccccc1
c1ccccc1.c1ccccc1
HI
Cl[Pd]([P](C1=CC=CC=C1)(C2=CC=CC=C2)C3=CC=CC=C3)([P](C4=CC=CC=C4)(C5=CC=CC=C5)C6=CC=CC=C6)Cl.[Cu]I.C(C)(C)(C)OC
null
2
C#Cc1ccc(OCC)cc1.Fc1ccc(I)cc1F>Cl[Pd]([P](C1=CC=CC=C1)(C2=CC=CC=C2)C3=CC=CC=C3)([P](C4=CC=CC=C4)(C5=CC=CC=C5)C6=CC=CC=C6)Cl.[Cu]I.C(C)(C)(C)OC>CCOc1ccc(C#Cc2ccc(F)c(F)c2)cc1
ord_dataset-02ee2261663048188cf6d85d2cc96e3f
ord-f7a7c59d4cda43ec8f4e943cd1b919d7
C#Cc1ccc(OCCCC)cc1.Fc1cc(Br)cc(F)c1F>>CCCCOc1ccc(C#Cc2cc(F)c(F)c(F)c2)cc1
C(CCC)OC1=CC=C(C=C1)C#C.FC=1C=C(C=C(C1F)F)Br.C(C)N(CC)CC>>FC=1C=C(C=C(C1F)F)C#CC1=CC=C(C=C1)OCCCC
[CH3:1][CH2:2][CH2:3][CH2:4][O:5][c:6]1[cH:7][cH:8][c:9]([C:10]#[CH:11])[cH:21][cH:22]1.Br[c:12]1[cH:13][c:14]([F:15])[c:16]([F:17])[c:18]([F:19])[cH:20]1>>[CH3:1][CH2:2][CH2:3][CH2:4][O:5][c:6]1[cH:7][cH:8][c:9]([C:10]#[C:11][c:12]2[cH:13][c:14]([F:15])[c:16]([F:17])[c:18]([F:19])[cH:20]2)[cH:21][cH:22]1
C#Cc1ccc(OCCCC)cc1.Fc1cc(Br)cc(F)c1F
CCCCOc1ccc(C#Cc2cc(F)c(F)c(F)c2)cc1
null
Cl[Pd]([P](C1=CC=CC=C1)(C2=CC=CC=C2)C3=CC=CC=C3)([P](C4=CC=CC=C4)(C5=CC=CC=C5)C6=CC=CC=C6)Cl.[Cu]I
C(C)(C)(C)OC
C-C Coupling
Sonogashira alkyne_aryl halide
15c08902746c61a960c314898ce6bb5fcc5e189f9e057388c59dba9ec9d0c81c
305eca0fd2975da49e7f69e4edfb9dc1cbce82513954bc5a73be3289e70e5f76
C(#Cc1ccccc1)c1ccccc1
Br-[c;H0;D3;+0:1](:[c:2]:[c:3]):[c:4]:[c:5].[CH;D1;+0:6]#[C:7]-[c:8]>>[c:3]:[c:2]:[c;H0;D3;+0:1](-[C;H0;D2;+0:6]#[C:7]-[c:8]):[c:4]:[c:5]
null
[]
null
null
2
HOUR
0.4 mmol of bis(triphenylphosphine)palladium(II) chloride and 0.2 mmol of CuI are added at room temperature to a mixture of 0.02 m of 4-butoxyphenylacetylene, 0.02 m of 3,4,5-trifluorobromobenzene and 50 ml of triethylamine. The reaction mixture is stirred at room temperature for 2 hours, diluted with methyl tert.-buty...
10.6084/m9.figshare.5104873.v1
null
Aromatic halide.Alkyne
Alkyne
c1ccccc1
c1ccccc1
c1ccccc1.c1ccccc1
HBr
Cl[Pd]([P](C1=CC=CC=C1)(C2=CC=CC=C2)C3=CC=CC=C3)([P](C4=CC=CC=C4)(C5=CC=CC=C5)C6=CC=CC=C6)Cl.[Cu]I.C(C)(C)(C)OC
null
2
C#Cc1ccc(OCCCC)cc1.Fc1cc(Br)cc(F)c1F>Cl[Pd]([P](C1=CC=CC=C1)(C2=CC=CC=C2)C3=CC=CC=C3)([P](C4=CC=CC=C4)(C5=CC=CC=C5)C6=CC=CC=C6)Cl.[Cu]I.C(C)(C)(C)OC>CCCCOc1ccc(C#Cc2cc(F)c(F)c(F)c2)cc1
ord_dataset-02ee2261663048188cf6d85d2cc96e3f
ord-f5389a0b5ac54c3387a6aa94190a6c9c
COC[P+](c1ccccc1)(c1ccccc1)c1ccccc1.N#Cc1ccc(C=O)cc1>>COC=Cc1ccc(C#N)cc1
C(#N)C1=CC=C(C=O)C=C1.[Cl-].COC[P+](C1=CC=CC=C1)(C1=CC=CC=C1)C1=CC=CC=C1>>COC=CC1=CC=C(C#N)C=C1
c1ccc([P+](c2ccccc2)(c2ccccc2)[CH2:3][O:2][CH3:1])cc1.O=[CH:4][c:5]1[cH:6][cH:7][c:8]([C:9]#[N:10])[cH:11][cH:12]1>>[CH3:1][O:2][CH:3]=[CH:4][c:5]1[cH:6][cH:7][c:8]([C:9]#[N:10])[cH:11][cH:12]1
COC[P+](c1ccccc1)(c1ccccc1)c1ccccc1.N#Cc1ccc(C=O)cc1
COC=Cc1ccc(C#N)cc1
null
null
COC(C)(C)C
C-C Coupling
Wittig with Phosphonium
1b762435fe6b580b808a6e9f0dae00ddd254c0b88d607d21a223e11776d2e3a4
bf4569804906d66c98adaac7df334e96eee508d45c26c621eb5069c3e4f1df77
c1ccccc1
O=[CH;D2;+0:1]-[c:2](:[c:3]):[c:4].[C;D1;H3:5]-[#8:6]-[CH2;D2;+0:7]-[P+](-c1:c:c:c:c:c:1)(-c1:c:c:c:c:c:1)-c1:c:c:c:c:c:1>>[C;D1;H3:5]-[#8:6]-[CH;D2;+0:7]=[CH;D2;+0:1]-[c:2](:[c:3]):[c:4]
null
[]
null
null
1
HOUR
A suspension of 37.2 g of methoxymethyl-triphenylphosphonium chloride in 250 ml of t-butyl methyl ether is treated at room temperature while gassing with argon with 13.4 g of potassium t-butylate and stirred for 1 hour. Subsequently, the reaction mixture is treated at about 20° C. with a mixture of 9.49 g of 4-cyanoben...
10.6084/m9.figshare.5104873.v1
null
Aldehyde.Ether
Ether
c1ccccc1.c1ccccc1.c1ccccc1
null
c1ccccc1
HO-
COC(C)(C)C
null
1
COC[P+](c1ccccc1)(c1ccccc1)c1ccccc1.N#Cc1ccc(C=O)cc1>COC(C)(C)C>COC=Cc1ccc(C#N)cc1
ord_dataset-02ee2261663048188cf6d85d2cc96e3f
ord-cad7b00ba5724d598c933c5d285d2c46
COC=C(C=O)c1ccc(C#N)cc1.N=C(N)c1ccc(C(N)=O)cc1>>N#Cc1ccc(-c2cnc(-c3ccc(C(N)=O)cc3)nc2)cc1
Cl.C(N)(=N)C1=CC=C(C(=O)N)C=C1.[Na].C(#N)C1=CC=C(C=C1)C(C=O)=COC>>C(#N)C1=CC=C(C=C1)C=1C=NC(=NC1)C1=CC=C(C(=O)N)C=C1
CO[CH:21]=[C:7]([c:6]1[cH:5][cH:4][c:3]([C:2]#[N:1])[cH:23][cH:22]1)[CH:8]=O.[NH2:9][C:10]([c:11]1[cH:12][cH:13][c:14]([C:15]([NH2:16])=[O:17])[cH:18][cH:19]1)=[NH:20]>>[N:1]#[C:2][c:3]1[cH:4][cH:5][c:6](-[c:7]2[cH:8][n:9][c:10](-[c:11]3[cH:12][cH:13][c:14]([C:15]([NH2:16])=[O:17])[cH:18][cH:19]3)[n:20][cH:21]2)[cH:22]...
COC=C(C=O)c1ccc(C#N)cc1.N=C(N)c1ccc(C(N)=O)cc1
N#Cc1ccc(-c2cnc(-c3ccc(C(N)=O)cc3)nc2)cc1
null
null
CO
Aromatic Heterocycle Formation
OtherReaction
7ff619bc6b8105d6a50f08652202021c7036772b44111654e9ca09f6e0092ca4
5e1c8e4021bf83ca9a2cb1d1e6032536755277517375e5fd4bee10b9e4aead67
c1ccc(-c2cnc(-c3ccccc3)nc2)cc1
C-O-[CH;D2;+0:1]=[C;H0;D3;+0:2](-[CH;D2;+0:3]=O)-[c;H0;D3;+0:4](:[c:5]:[c:6]):[c:7]:[c:8].[NH2;D1;+0:9]-[C;H0;D3;+0:10](=[NH;D1;+0:11])-[c;H0;D3;+0:12](:[c:13]:[c:14]):[c:15]:[c:16]>>[c:14]:[c:13]:[c;H0;D3;+0:12](-[c;H0;D3;+0:10]1:[n;H0;D2;+0:11]:[cH;D2;+0:1]:[c;H0;D3;+0:2](-[c;H0;D3;+0:4](:[c:5]:[c:6]):[c:7]:[c:8]):[c...
null
[]
null
null
2
HOUR
247 mg of sodium are treated at room temperature with 10 ml of methanol. After 15 minutes the solution obtained is treated at room temperature with 1.58 g of 4-amidinobenzamide hydrochloride. A white suspension forms and this is treated dropwise at room temperature within 10 minutes with a solution of 1.42 g of 2-(4-cy...
10.6084/m9.figshare.5104873.v1
null
Aldehyde.Ether.Primary amine
null
null
c1cncnc1
c1ccccc1.c1cncnc1.c1ccccc1
HO-
CO
null
2
COC=C(C=O)c1ccc(C#N)cc1.N=C(N)c1ccc(C(N)=O)cc1>CO>N#Cc1ccc(-c2cnc(-c3ccc(C(N)=O)cc3)nc2)cc1
ord_dataset-02ee2261663048188cf6d85d2cc96e3f
ord-66dbc3d515fb4644a721ff89c761de7f
[Ag+]>>[Ag]
[N+](=O)([O-])[O-].[Ag+].N.N1N=NC2=C1C=CC=C2>>N1N=NC2=C1C=CC=C2.[Ag]
[Ag+:1]>>[Ag:1]
[Ag+]
[Ag]
null
null
null
Miscellaneous
OtherReaction
40ba59785861b8226ce5af6bdcbb9a37f0ff50a8c7ec7d4fc4c524cf906cc65c
56ebed4a8b3cebec83c37a71d68f0c87d1e404ab05a9ce792691e4e18a2379dd
null
[Ag+;H0;D0:1]>>[Ag;H0;D0;+0:1]
null
[]
null
null
null
null
Prepared by mixing simultaneously an ammoniacal silver nitrate aqueous solution and bendotriazole (containing 0.2 mol % of aqueous ammonia per mol benzotriazole) into a 10%-aqueous solution of phenylcarbamoyl gelatin of 50° C. After completing the addition, the pH was reduced and then flocculation and desalting were ca...
10.6084/m9.figshare.5104873.v1
null
null
null
null
null
null
null
null
null
null
[Ag+]>>[Ag]
ord_dataset-02ee2261663048188cf6d85d2cc96e3f
ord-1552f7df163c4dd28c6db945c2a62da2
CCC(C)(C)c1ccc(OCC(CNC(=O)c2cc(C(=O)NCC(COc3ccc(C(C)(C)CC)cc3)C(C)(C)CC)cc(S(=O)(=O)Cl)c2)C(C)(C)CC)cc1>>CCC(C)(C)c1ccc(OCC(CNC(=O)c2cc(C(=O)NCC(COc3ccc(C(C)(C)CC)cc3)C(C)(C)CC)cc(S(=O)[O-])c2)C(C)(C)CC)cc1
C(C)(C)(CC)C(CNC(=O)C=1C=C(C=C(C1)C(NCC(COC1=CC=C(C=C1)C(C)(C)CC)C(C)(C)CC)=O)S(=O)(=O)Cl)COC1=CC=C(C=C1)C(C)(C)CC.S(=O)([O-])[O-].[Na+].[Na+].C(O)([O-])=O.[Na+].O>>C(C)(C)(CC)C(CNC(=O)C=1C=C(C=C(C1)C(NCC(COC1=CC=C(C=C1)C(C)(C)CC)C(C)(C)CC)=O)S(=O)[O-])COC1=CC=C(C=C1)C(C)(C)CC.[Na+]
Cl[S:45]([c:44]1[cH:43][c:19]([C:20](=[O:21])[NH:22][CH2:23][CH:24]([CH2:25][O:26][c:27]2[cH:28][cH:29][c:30]([C:31]([CH3:32])([CH3:33])[CH2:34][CH3:35])[cH:36][cH:37]2)[C:38]([CH3:39])([CH3:40])[CH2:41][CH3:42])[cH:18][c:17]([C:15]([NH:14][CH2:13][CH:12]([CH2:11][O:10][c:9]2[cH:8][cH:7][c:6]([C:3]([CH2:2][CH3:1])([CH3...
CCC(C)(C)c1ccc(OCC(CNC(=O)c2cc(C(=O)NCC(COc3ccc(C(C)(C)CC)cc3)C(C)(C)CC)cc(S(=O)(=O)Cl)c2)C(C)(C)CC)cc1
CCC(C)(C)c1ccc(OCC(CNC(=O)c2cc(C(=O)NCC(COc3ccc(C(C)(C)CC)cc3)C(C)(C)CC)cc(S(=O)[O-])c2)C(C)(C)CC)cc1
null
null
C(C)#N
Miscellaneous
OtherReaction
65bd520d46095381b97cf2b1c808b198594dded087e2637f2dbe5add6a47838a
5f0d826ff827e7d94d07bc9ee74d0a88c79bcf75bb024f05043486e1cbe294bd
O=C(NCCCOc1ccccc1)c1cccc(C(=O)NCCCOc2ccccc2)c1
Cl-[S;H0;D4;+0:1](=[O;D1;H0:2])(=[O;H0;D1;+0:3])-[c:4](:[c:5]):[c:6]>>[O-;H0;D1:3]-[S;H0;D3;+0:1](=[O;D1;H0:2])-[c:4](:[c:5]):[c:6]
82.8
[{"value": 82.8, "product": "C(C)(C)(CC)C(CNC(=O)C=1C=C(C=C(C1)C(NCC(COC1=CC=C(C=C1)C(C)(C)CC)C(C)(C)CC)=O)S(=O)[O-])COC1=CC=C(C=C1)C(C)(C)CC.[Na+]", "details": "PERCENTYIELD", "is_desired": false}, {"value": 82.8, "product": "C(C)(C)(CC)C(CNC(=O)C=1C=C(C=C(C1)C(NCC(COC1=CC=C(C=C1)C(C)(C)CC)C(C)(C)CC)=O)S(=O)[O-])COC1=...
30
CELSIUS
null
null
To 2 g (0.016 mol) of sodium sulfite and 2.4 g (0.029 mol) of sodium hydrogen carbonate were added 100 ml of water and 20 ml of acetonitrile and the mixture was stirred at 30° C. To the mixture was added dropwise a solution of 10.5 g (0.013 mol) of 3,5-di-(2,4-di-tert-amylphenoxypropylcarbamoyl)benzenesulfonyl chloride...
10.6084/m9.figshare.5104873.v1
null
Sulfonyl halide
null
null
null
c1ccccc1.c1ccccc1.c1ccccc1
Other
C(C)#N
30
null
CCC(C)(C)c1ccc(OCC(CNC(=O)c2cc(C(=O)NCC(COc3ccc(C(C)(C)CC)cc3)C(C)(C)CC)cc(S(=O)(=O)Cl)c2)C(C)(C)CC)cc1>C(C)#N>CCC(C)(C)c1ccc(OCC(CNC(=O)c2cc(C(=O)NCC(COc3ccc(C(C)(C)CC)cc3)C(C)(C)CC)cc(S(=O)[O-])c2)C(C)(C)CC)cc1
ord_dataset-02ee2261663048188cf6d85d2cc96e3f
ord-1d5819da44804bb79114f5102ded9ad5
CCCCCCCCCCCCCCCCOC(=O)c1cc(C(=O)OCCCCCCCCCCCCCCCC)cc(S(=O)(=O)Cl)c1.O>>CCCCCCCCCCCCCCCCOC(=O)c1cc(C(=O)OCCCCCCCCCCCCCCCC)cc(S(=O)(=O)O)c1
C(CCCCCCCCCCCCCCC)OC(=O)C=1C=C(C=C(C1)C(=O)OCCCCCCCCCCCCCCCC)S(=O)(=O)Cl.O.Cl>>C(CCCCCCCCCCCCCCC)OC(=O)C=1C=C(C=C(C1)C(=O)OCCCCCCCCCCCCCCCC)S(=O)(=O)O
Cl[S:44]([c:43]1[cH:42][c:22]([C:23](=[O:24])[O:25][CH2:26][CH2:27][CH2:28][CH2:29][CH2:30][CH2:31][CH2:32][CH2:33][CH2:34][CH2:35][CH2:36][CH2:37][CH2:38][CH2:39][CH2:40][CH3:41])[cH:21][c:20]([C:18]([O:17][CH2:16][CH2:15][CH2:14][CH2:13][CH2:12][CH2:11][CH2:10][CH2:9][CH2:8][CH2:7][CH2:6][CH2:5][CH2:4][CH2:3][CH2:2][...
CCCCCCCCCCCCCCCCOC(=O)c1cc(C(=O)OCCCCCCCCCCCCCCCC)cc(S(=O)(=O)Cl)c1.O
CCCCCCCCCCCCCCCCOC(=O)c1cc(C(=O)OCCCCCCCCCCCCCCCC)cc(S(=O)(=O)O)c1
null
[Zn]
C(Cl)(Cl)Cl
Acylation
OtherReaction
1eafc1aae6c14d9972cab5f3920901c9514a0be256331ee344fa90a3f3cbb637
0a58714a63276a8fe8849940eeb9a2ea532cac0a306d322fd1d3946a4729fe01
c1ccccc1
Cl-[S;H0;D4;+0:1](=[O;D1;H0:2])(=[O;D1;H0:3])-[c:4](:[c:5]):[c:6].[OH2;D0;+0:7]>>[O;D1;H0:2]=[S;H0;D4;+0:1](=[O;D1;H0:3])(-[OH;D1;+0:7])-[c:4](:[c:5]):[c:6]
null
[]
null
null
30
MINUTE
87 ml of water and 18.2 ml (0.218 mol) of 12N-HCl were added to the solution of 87 ml of chloroform and 8.65 g (0.0121 mol) of the white solid containing 3,5-dihexadecyloxycarbonylbenzenesulfonyl chloride, and then 7.93 g of zinc was added thereto at 5° C. followed by stirring for 4 hours and 30 minutes. After the inso...
10.6084/m9.figshare.5104873.v1
null
Sulfonyl halide
Sulfonic acid
null
null
c1ccccc1
HCl
[Zn].C(Cl)(Cl)Cl
null
0.5
CCCCCCCCCCCCCCCCOC(=O)c1cc(C(=O)OCCCCCCCCCCCCCCCC)cc(S(=O)(=O)Cl)c1.O>[Zn].C(Cl)(Cl)Cl>CCCCCCCCCCCCCCCCOC(=O)c1cc(C(=O)OCCCCCCCCCCCCCCCC)cc(S(=O)(=O)O)c1
ord_dataset-02ee2261663048188cf6d85d2cc96e3f
ord-0efa13a49ba14cf48bbde9a169b7b718
CCCCCCCCCCCCc1ccc(O)cc1O.O=Nc1ccc(O)cc1O>>CCCCCCCCCCCCc1cc2nc3ccc(O)cc3oc-2cc1=O
C(CCCCCCCCCCC)C1=C(C=C(O)C=C1)O.N(=O)C1=C(C=C(O)C=C1)O>>C(CCCCCCCCCCC)C1=CC2=NC3=CC=C(C=C3OC2=CC1=O)O
O[c:25]1[cH:15][cH:14][c:13]([CH2:12][CH2:11][CH2:10][CH2:9][CH2:8][CH2:7][CH2:6][CH2:5][CH2:4][CH2:3][CH2:2][CH3:1])[c:27]([OH:28])[cH:26]1.O=[N:16][c:17]1[cH:18][cH:19][c:20]([OH:21])[cH:22][c:23]1[OH:24]>>[CH3:1][CH2:2][CH2:3][CH2:4][CH2:5][CH2:6][CH2:7][CH2:8][CH2:9][CH2:10][CH2:11][CH2:12][c:13]1[cH:14][c:15]2[n:1...
CCCCCCCCCCCCc1ccc(O)cc1O.O=Nc1ccc(O)cc1O
CCCCCCCCCCCCc1cc2nc3ccc(O)cc3oc-2cc1=O
null
null
S(O)(O)(=O)=O
Aromatic Heterocycle Formation
OtherReaction
feeaff925a6fe0f956d6a39e6fb8aff7991b05d71d2117702fc196a2ef8c74c6
5f9d020af144bb530e68224e7a66d6a00fa1eddb8435fb4807edcffd80f1584a
O=c1ccc2nc3ccccc3oc-2c1
O-[c;H0;D3;+0:1]1:[c:2]:[c;H0;D3;+0:3](-[OH;D1;+0:4]):[c:5](-[C:6]):[c:7]:[cH;D2;+0:8]:1.O=[N;H0;D2;+0:9]-[c:10](:[c:11]):[c:12](-[OH;D1;+0:13]):[c:14]>>[C:6]-[c:5]1:[c:7]:[c;H0;D3;+0:8]2:[n;H0;D2;+0:9]:[c:10](:[c:11]):[c:12](:[c:14]):[o;H0;D2;+0:13]:[c;H0;D3;+0:1]-2:[c:2]:[c;H0;D3;+0:3]:1=[O;H0;D1;+0:4]
47.9
[{"value": 47.9, "product": "C(CCCCCCCCCCC)C1=CC2=NC3=CC=C(C=C3OC2=CC1=O)O", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
5
HOUR
A solution of 4-dodecylresorcinol (8.5 g, 30.53 mmole) (Aldrich Chemical Company) and 4-nitrosoresorcinol (5.0 g, 35.9 mmole) (Aldrich) in concentrated sulfuric acid (100 mL) is heated to 67° C. with stirring for 5 hours. The reaction mixture is allowed to cool to room temperature, poured into ice-water (1800 mL) and f...
10.6084/m9.figshare.5104873.v1
null
Nitroso.Aromatic alcohol.Aromatic alcohol.Aromatic alcohol
null
c1ccccc1.c1ccccc1
c1ccc2oc3ccccc3nc2c1
c1ccc2oc3ccccc3nc2c1
HO-
S(O)(O)(=O)=O
null
5
CCCCCCCCCCCCc1ccc(O)cc1O.O=Nc1ccc(O)cc1O>S(O)(O)(=O)=O>CCCCCCCCCCCCc1cc2nc3ccc(O)cc3oc-2cc1=O
ord_dataset-02ee2261663048188cf6d85d2cc96e3f
ord-524d531152204c2e8e6ceed8643f94a1
CC(=O)OCC1O[C@H](Br)C(OC(C)=O)[C@@H](OC(C)=O)[C@H]1OC(C)=O.CCCCCCCCCCCCCCCCCCc1cc2nc3ccc(O)cc3oc-2cc1=O>>CCCCCCCCCCCCCCCCCCc1cc2nc3ccc(O[C@@H]4O[C@H](COC(C)=O)[C@H](OC(C)=O)[C@H](OC(C)=O)[C@H]4OC(C)=O)cc3oc-2cc1=O
OC=1C=C2OC3=CC(C(=CC3=NC2=CC1)CCCCCCCCCCCCCCCCCC)=O.CC1=CC(=NC(=C1)C)C.CC(=O)OCC1[C@@H]([C@@H](C([C@H](O1)Br)OC(=O)C)OC(=O)C)OC(=O)C>>C(CCCCCCCCCCCCCCCCC)C1=CC2=NC3=CC=C(C=C3OC2=CC1=O)O[C@H]1[C@H](OC(C)=O)[C@@H](OC(C)=O)[C@@H](OC(C)=O)[C@H](O1)COC(C)=O
Br[C@H:28]1[O:29][CH:30]([CH2:31][O:32][C:33]([CH3:34])=[O:35])[C@H:36]([O:37][C:38]([CH3:39])=[O:40])[C@H:41]([O:42][C:43]([CH3:44])=[O:45])[CH:46]1[O:47][C:48]([CH3:49])=[O:50].[CH3:1][CH2:2][CH2:3][CH2:4][CH2:5][CH2:6][CH2:7][CH2:8][CH2:9][CH2:10][CH2:11][CH2:12][CH2:13][CH2:14][CH2:15][CH2:16][CH2:17][CH2:18][c:19]...
CC(=O)OCC1O[C@H](Br)C(OC(C)=O)[C@@H](OC(C)=O)[C@H]1OC(C)=O.CCCCCCCCCCCCCCCCCCc1cc2nc3ccc(O)cc3oc-2cc1=O
CCCCCCCCCCCCCCCCCCc1cc2nc3ccc(O[C@@H]4O[C@H](COC(C)=O)[C@H](OC(C)=O)[C@H](OC(C)=O)[C@H]4OC(C)=O)cc3oc-2cc1=O
null
C([O-])([O-])=O.[Ag+2]
ClCCl
Heteroatom Alkylation and Arylation
Williamson Ether Synthesis
10bc97c5591dffc70f58b8342cb03eebbb174e9f252bf00557248c38c5c8d459
55080db572a904fc27b88d797c7a6e2b661ffe3650c92412a40a3b49e5a4d963
O=c1ccc2nc3ccc(O[C@H]4CCCCO4)cc3oc-2c1
Br-[C@H;D3;+0:1]1-[#8:2]-[C:3]-[C:4]-[C:5](-[#8:6]-[C:7](-[C;D1;H3:8])=[O;D1;H0:9])-[CH;D3;+0:10]-1-[#8:11]-[C:12](-[C;D1;H3:13])=[O;D1;H0:14].[#8;a:15]:[c:16]:[c:17]:[c:18](-[OH;D1;+0:19]):[c:20]>>[#8;a:15]:[c:16]:[c:17]:[c:18](-[O;H0;D2;+0:19]-[C@@H;D3;+0:1]1-[#8:2]-[C:3]-[C:4]-[C:5](-[#8:6]-[C:7](-[C;D1;H3:8])=[O;D1...
null
[]
null
null
1
HOUR
A mixture of 7-hydroxy-2-octadecyl-3H-phenoxazine-3-one ("octadecylresorufin) (220 mg, 0.47 mmole), powdered, activated 4Å molecular sieves (0.5 g), sym-collidine (125 μL, 0.95 mmole), and silver carbonate (155 mg, 0.56 mmole) in dry dichloromethane (20 mL) is allowed to stir at room temperature, under an atmosphere of...
10.6084/m9.figshare.5104873.v1
null
Secondary halide.Ether.Aromatic alcohol
Ether.Ether
C1CCOCC1
C1CCOCC1
c1ccc2oc3ccccc3nc2c1.C1CCOCC1
HBr
C([O-])([O-])=O.[Ag+2].ClCCl
null
1
CC(=O)OCC1O[C@H](Br)C(OC(C)=O)[C@@H](OC(C)=O)[C@H]1OC(C)=O.CCCCCCCCCCCCCCCCCCc1cc2nc3ccc(O)cc3oc-2cc1=O>C([O-])([O-])=O.[Ag+2].ClCCl>CCCCCCCCCCCCCCCCCCc1cc2nc3ccc(O[C@@H]4O[C@H](COC(C)=O)[C@H](OC(C)=O)[C@H](OC(C)=O)[C@H]4OC(C)=O)cc3oc-2cc1=O
ord_dataset-02ee2261663048188cf6d85d2cc96e3f
ord-24c840048e664bd5a56761d42d4b423b
O=C1CCC(=O)O1.Oc1cccc(O)c1>>O=C(O)CC=C1c2ccc(O)cc2Oc2cc(O)ccc21
C1(O)=CC(O)=CC=C1.C1(CCC(=O)O1)=O>>C(=O)(O)CC=C1C2=CC=C(C=C2OC=2C=C(C=CC12)O)O
[O:1]=[C:2]1[O:3][C:10](=[O:11])[CH2:9][CH2:4]1.[cH:7]1[c:13]([OH:14])[cH:12][c:17]([OH:18])[cH:19][cH:20]1>>[O:1]=[C:2]([OH:3])[CH2:4][CH:5]=[C:6]1[c:7]2[cH:8][cH:9][c:10]([OH:11])[cH:12][c:13]2[O:14][c:15]2[cH:16][c:17]([OH:18])[cH:19][cH:20][c:21]21
O=C1CCC(=O)O1.Oc1cccc(O)c1
O=C(O)CC=C1c2ccc(O)cc2Oc2cc(O)ccc21
null
null
null
Aromatic Heterocycle Formation
OtherReaction
4925f2a5eef4e9804a3612d2dae70eada4948017ed12fefbe63397580ba4f239
4c5e42ba40f03a268dd3324423389cf0e89fa2dfb6bd8dd2bc3e76b5039fdcf7
[CH]=C1c2ccccc2Oc2ccccc21
[O;D1;H0:1]=[C:2]1-[CH2;D2;+0:3]-[CH2;D2;+0:4]-[C;H0;D3;+0:5](=[O;H0;D1;+0:6])-[O;H0;D2;+0:7]-1.[O;D1;H1:8]-[c;H0;D3;+0:9]1:[c:10]:[cH;D2;+0:11]:[cH;D2;+0:12]:[c:13](-[OH;D1;+0:14]):[cH;D2;+0:15]:1>>[O;D1;H0:1]=[C:2](-[OH;D1;+0:7])-[CH2;D2;+0:3]-[C:16]=[C:17]1-[c:18]2:[cH;D2;+0:11]:[c:10]:[c;H0;D3;+0:9](-[O;D1;H1:8]):[...
88.4
[{"value": 88.0, "product": "C(=O)(O)CC=C1C2=CC=C(C=C2OC=2C=C(C=CC12)O)O", "details": "PERCENTYIELD", "is_desired": false}, {"value": 88.4, "product": "C(=O)(O)CC=C1C2=CC=C(C=C2OC=2C=C(C=CC12)O)O", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
65
CELSIUS
2
HOUR
Resorcinol (33.0 g, 0.300 mol) and succinic anhydride (30.0 g, 0.300 mol) were placed in a round bottomed flask and purged with nitrogen. Methanesulfonic acid (150 mL) was added and the solution was stirred at 65° C. for 2 hours under an atmosphere of nitrogen. The reaction mixture was added dropwise to rapidly stirred...
10.6084/m9.figshare.5104873.v1
null
Anhydride.Aromatic alcohol.Aromatic alcohol
Carboxylic acid.Ether.Aromatic alcohol.Aromatic alcohol
C1CCOC1.c1ccccc1
c1ccc2c(c1)Cc1ccccc1O2
c1ccc2c(c1)Cc1ccccc1O2
Other
null
65
2
O=C1CCC(=O)O1.Oc1cccc(O)c1>>O=C(O)CC=C1c2ccc(O)cc2Oc2cc(O)ccc21
ord_dataset-02ee2261663048188cf6d85d2cc96e3f
ord-237c45c77bf1482fa8552c921abf2dea
O=Cc1ccc(O)cc1O>>Cc1ccc(O)cc1O
[H][H].P(O)(O)(O)=O.OC1=C(C=O)C=CC(=C1)O.[H][H]>>CC1=C(C=C(O)C=C1)O
O=[CH:1][c:2]1[cH:3][cH:4][c:5]([OH:6])[cH:7][c:8]1[OH:9]>>[CH3:1][c:2]1[cH:3][cH:4][c:5]([OH:6])[cH:7][c:8]1[OH:9]
O=Cc1ccc(O)cc1O
Cc1ccc(O)cc1O
null
[Pd]
CC(C)O
Reduction
OtherReaction
80164d08698e723aff741c2b428f9ebe7e14faf51ad55ff412ac682536758b9f
9b627af1c37cea795d25b24c8b755865edc79a56af73aa7fa1348903b24aee3f
c1ccccc1
O=[CH;D2;+0:1]-[c:2](:[c:3]):[c:4]>>[CH3;D1;+0:1]-[c:2](:[c:3]):[c:4]
98.1
[{"value": 98.0, "product": "CC1=C(C=C(O)C=C1)O", "details": "PERCENTYIELD", "is_desired": false}, {"value": 98.1, "product": "CC1=C(C=C(O)C=C1)O", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
null
null
2,4-Dihyroxybenzaldehyde (33.97 gm, 0.246 mol) (recrystallized from toluene) was dissolved in spectroscopic grade 2-propanol (3 L) in a round bottom flask fitted with a gas inlet and a bubbler outlet. 10% Palladium on carbon (1.35 gm) was added followed by phosphoric acid (3mL) and the mixture was sparaged with nitroge...
10.6084/m9.figshare.5104873.v1
null
Aldehyde
null
null
null
c1ccccc1
Other
[Pd].CC(C)O
null
null
O=Cc1ccc(O)cc1O>[Pd].CC(C)O>Cc1ccc(O)cc1O
ord_dataset-02ee2261663048188cf6d85d2cc96e3f
ord-97f438e7ffbd4764b1ee7bf05860487d
Cc1ccc(O)cc1O.O=C1CCC(=O)O1>>Cc1cc2c(cc1O)Oc1cc(O)c(C)cc1C2=CCC(=O)O
CC1=C(C=C(O)C=C1)O.C1(CCC(=O)O1)=O>>C(=O)(O)CC=C1C2=CC(=C(C=C2OC=2C=C(C(=CC12)C)O)O)C
[CH3:1][c:2]1[cH:3][cH:4][c:5]([OH:9])[cH:6][c:7]1[OH:8].[CH2:10]1[C:12](=[O:13])[O:23][C:21](=[O:22])[CH2:20]1>>[CH3:1][c:2]1[cH:3][c:4]2[c:5]([cH:6][c:7]1[OH:8])[O:9][c:10]1[cH:11][c:12]([OH:13])[c:14]([CH3:15])[cH:16][c:17]1[C:18]2=[CH:19][CH2:20][C:21](=[O:22])[OH:23]
Cc1ccc(O)cc1O.O=C1CCC(=O)O1
Cc1cc2c(cc1O)Oc1cc(O)c(C)cc1C2=CCC(=O)O
null
null
null
Aromatic Heterocycle Formation
OtherReaction
8e7ce8e5ab260605c6335916ab57b07e358f90acd2e31915711746a6f7c02794
2af0d7052e250fcc0027d675556884856e46081e4d1bd17dfc6a2818e78b4b0b
[CH]=C1c2ccccc2Oc2ccccc21
[O;D1;H0:1]=[C:2]1-[CH2;D2;+0:3]-[CH2;D2;+0:4]-[C;H0;D3;+0:5](=[O;H0;D1;+0:6])-[O;H0;D2;+0:7]-1.[OH;D1;+0:8]-[c:9](:[c:10]):[cH;D2;+0:11]:[c:12]:[c:13]>>[C;D1;H3:14]-[c:15]1:[c:16]:[c:17]2:[c;H0;D3;+0:4](:[c:18]:[c;H0;D3;+0:5]:1-[OH;D1;+0:6])-[O;H0;D2;+0:8]-[c:9](:[c:10]):[c;H0;D3;+0:11](:[c:12]:[c:13])-[C:19]-2=[C:20]...
74.2
[{"value": 74.0, "product": "C(=O)(O)CC=C1C2=CC(=C(C=C2OC=2C=C(C(=CC12)C)O)O)C", "details": "PERCENTYIELD", "is_desired": false}, {"value": 74.2, "product": "C(=O)(O)CC=C1C2=CC(=C(C=C2OC=2C=C(C(=CC12)C)O)O)C", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
65
CELSIUS
null
null
4-Methylresorcinol (25.8 g, 0.208 mol) and succinic anhydride (20.8 g, 0.208 g) were placed in a round bottom flask and the flask was purged with nitrogen. Methanesulfonic acid (150 mL) was added and the solution heated under nitrogen to 65° C. for 2 hours. The solution was added dropwise to 1 L of rapidly stirred, ice...
10.6084/m9.figshare.5104873.v1
null
Anhydride.Aromatic alcohol
Carboxylic acid.Ether.Aromatic alcohol
c1ccccc1.C1CCOC1
c1ccc2c(c1)Cc1ccccc1O2
c1ccc2c(c1)Cc1ccccc1O2
Other
null
65
null
Cc1ccc(O)cc1O.O=C1CCC(=O)O1>>Cc1cc2c(cc1O)Oc1cc(O)c(C)cc1C2=CCC(=O)O
ord_dataset-02ee2261663048188cf6d85d2cc96e3f
ord-69d326a15330467090d94484b9ed6312
CN(C=O)c1ccccc1.Cc1c(O)cccc1O>>Cc1c(O)ccc(C=O)c1O
P(=O)(Cl)(Cl)Cl.CN(C1=CC=CC=C1)C=O.CC1=C(O)C=CC=C1O>>OC1=C(C=O)C=CC(=C1C)O
CN(c1ccccc1)[CH:8]=[O:9].[CH3:1][c:2]1[c:3]([OH:4])[cH:5][cH:6][cH:7][c:10]1[OH:11]>>[CH3:1][c:2]1[c:3]([OH:4])[cH:5][cH:6][c:7]([CH:8]=[O:9])[c:10]1[OH:11]
CN(C=O)c1ccccc1.Cc1c(O)cccc1O
Cc1c(O)ccc(C=O)c1O
null
null
CCOCC
C-C Coupling
OtherReaction
285803636db9e45ff0b980aa9c160ed6302cad8a21b5d872b908f4e4658d903e
f0bd75a0630092c31f21f61f4a015c77ae0dff14a0b742b4370d7a38fda490f7
c1ccccc1
C-N(-[CH;D2;+0:1]=[O;D1;H0:2])-c1:c:c:c:c:c:1.[O;D1;H1:3]-[c:4](:[c:5]):[cH;D2;+0:6]:[c:7]:[c:8]>>[O;D1;H0:2]=[CH;D2;+0:1]-[c;H0;D3;+0:6](:[c:7]:[c:8]):[c:4](-[O;D1;H1:3]):[c:5]
57
[{"value": 57.0, "product": "OC1=C(C=O)C=CC(=C1C)O", "details": "PERCENTYIELD", "is_desired": false}, {"value": 56.8, "product": "OC1=C(C=O)C=CC(=C1C)O", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
1
HOUR
Phosphorus oxychloride (80 mL, 0.86 mol) was added to a stirred mixture of N-methylformanilide (102 mL, 0.82 mol) in ether (250 mL). The mixture was stirred for 1 hour at room temperature and then cooled in ice. 2-Methyl resorcinol (Aldrich, 100 g, 0.81 mol) was added and the mixture was allowed to warm to room tempera...
10.6084/m9.figshare.5104873.v1
null
Tertiary amide
Aldehyde
c1ccccc1.c1ccccc1
c1ccccc1
c1ccccc1
Other
CCOCC
null
1
CN(C=O)c1ccccc1.Cc1c(O)cccc1O>CCOCC>Cc1c(O)ccc(C=O)c1O
ord_dataset-02ee2261663048188cf6d85d2cc96e3f
ord-acac41327ddf4baf83b59f70db7ade15
Cc1c(O)ccc(C=O)c1O>>Cc1ccc(O)c(C)c1O
OC1=C(C=O)C=CC(=C1C)O.P(O)(O)(O)=O>>CC1=C(O)C=CC(=C1O)C
O=[CH:1][c:2]1[cH:3][cH:4][c:5]([OH:6])[c:7]([CH3:8])[c:9]1[OH:10]>>[CH3:1][c:2]1[cH:3][cH:4][c:5]([OH:6])[c:7]([CH3:8])[c:9]1[OH:10]
Cc1c(O)ccc(C=O)c1O
Cc1ccc(O)c(C)c1O
null
[Pd]
C(C)(C)O
Reduction
OtherReaction
80164d08698e723aff741c2b428f9ebe7e14faf51ad55ff412ac682536758b9f
9b627af1c37cea795d25b24c8b755865edc79a56af73aa7fa1348903b24aee3f
c1ccccc1
O=[CH;D2;+0:1]-[c:2](:[c:3]):[c:4]>>[CH3;D1;+0:1]-[c:2](:[c:3]):[c:4]
72
[{"value": 72.0, "product": "CC1=C(O)C=CC(=C1O)C", "details": "PERCENTYIELD", "is_desired": false}, {"value": 72.0, "product": "CC1=C(O)C=CC(=C1O)C", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
null
null
A solution of 2,4-dihydroxy-3-methylbenzaldehyde (30.0 g, 197 mmol) with isopropanol (3 L) was ice-cooled in a 5 L 3-neck flask fitted with a magnetic stirrer. Phosphoric acid (4 mL) and d10% palladium on carbon were added and the solution was sparged with nitrogen, then hydrogen. When uptake was judged to be complete ...
10.6084/m9.figshare.5104873.v1
null
Aldehyde
null
null
null
c1ccccc1
Other
[Pd].C(C)(C)O
null
null
Cc1c(O)ccc(C=O)c1O>[Pd].C(C)(C)O>Cc1ccc(O)c(C)c1O
ord_dataset-02ee2261663048188cf6d85d2cc96e3f
ord-88e1e4ec780f4191be8409df6b2f61b1
II.Nc1ccn([C@H]2CC[C@@H](CO)O2)c(=O)n1>>Nc1nc(=O)n([C@H]2CC[C@@H](CO)O2)cc1I
[C@@H]1(CC[C@@H](CO)O1)N1C(=O)N=C(N)C=C1.II>>IC=1C(=NC(N([C@H]2CC[C@@H](CO)O2)C1)=O)N
I[I:16].[NH2:1][c:2]1[n:3][c:4](=[O:5])[n:6]([C@H:7]2[CH2:8][CH2:9][C@@H:10]([CH2:11][OH:12])[O:13]2)[cH:14][cH:15]1>>[NH2:1][c:2]1[n:3][c:4](=[O:5])[n:6]([C@H:7]2[CH2:8][CH2:9][C@@H:10]([CH2:11][OH:12])[O:13]2)[cH:14][c:15]1[I:16]
II.Nc1ccn([C@H]2CC[C@@H](CO)O2)c(=O)n1
Nc1nc(=O)n([C@H]2CC[C@@H](CO)O2)cc1I
null
null
ClCCl.CO
Functional Group Interconversion
OtherReaction
b0bb6940bdaa4f483f95617a9ee5e6563c160ea710db3fde10ee056459a3fce1
3c4065ab4a8681675e06a527dcad54d701c7bfdcac9f73f87773b05034108934
O=c1ncccn1[C@H]1CCCO1
I-[I;H0;D1;+0:1].[#8:2]-[C:3]-[#7;a:4]1:[c:5]:[cH;D2;+0:6]:[c:7](-[N;D1;H2:8]):[#7;a:9]:[c:10]:1>>[#8:2]-[C:3]-[#7;a:4]1:[c:5]:[c;H0;D3;+0:6](-[I;H0;D1;+0:1]):[c:7](-[N;D1;H2:8]):[#7;a:9]:[c:10]:1
83
[{"value": 83.0, "product": "IC=1C(=NC(N([C@H]2CC[C@@H](CO)O2)C1)=O)N", "details": "PERCENTYIELD", "is_desired": false}, {"value": 82.8, "product": "IC=1C(=NC(N([C@H]2CC[C@@H](CO)O2)C1)=O)N", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
4
HOUR
A solution of 2', 3'-dideoxycytidine (2.11 g, 10 mmol, Raylo) and mercuric acetate (3.35 g, 10.5 mmol, Fisher) in 50 mL of methanol was refluxed for 19 hours. The resulting white suspension was diluted with methanol (50 mL) and dichloromethane (100 mL). Iodine (3.05 g, 12 mmol) was added and the suspension was stirred ...
10.6084/m9.figshare.5104873.v1
null
null
Aromatic halide
c1cncnc1
c1cncnc1
c1cncnc1.C1CCOC1
HI
ClCCl.CO
null
4
II.Nc1ccn([C@H]2CC[C@@H](CO)O2)c(=O)n1>ClCCl.CO>Nc1nc(=O)n([C@H]2CC[C@@H](CO)O2)cc1I
ord_dataset-02ee2261663048188cf6d85d2cc96e3f
ord-dae2fd2549ce4bb2a6b66fb56721b9fb
CCCCN(CCCC)CCCC.O=P([O-])([O-])OP(=O)([O-])[O-].c1ccncc1>>CCCC[NH+](CCCC)CCCC.CCCC[NH+](CCCC)CCCC.CCCC[NH+](CCCC)CCCC.O=P([O-])([O-])OP(=O)([O-])O
N1=CC=CC=C1.O.O.O.O.O.O.O.O.O.O.[O-]P([O-])(=O)OP(=O)([O-])[O-].[Na+].[Na+].[Na+].[Na+].C(CCC)N(CCCC)CCCC>>[O-]P([O-])(=O)OP(=O)([O-])O.C(CCC)[NH+](CCCC)CCCC.C(CCC)[NH+](CCCC)CCCC.C(CCC)[NH+](CCCC)CCCC
[CH3:1][CH2:2][CH2:3][CH2:4][N:18]([CH2:23][CH2:24][CH2:25][CH3:26])[CH2:36][CH2:37][CH2:38][CH3:39].[O:40]=[P:41]([O-:42])([O-:43])[O:44][P:45](=[O:46])([O-:47])[O-:48].[n:5]1[cH:6][cH:7][cH:8][cH:20][cH:10]1>>[CH3:1][CH2:2][CH2:3][CH2:4][NH+:5]([CH2:6][CH2:7][CH2:8][CH3:9])[CH2:10][CH2:11][CH2:12][CH3:13].[CH3:14][CH...
CCCCN(CCCC)CCCC.O=P([O-])([O-])OP(=O)([O-])[O-].c1ccncc1
CCCC[NH+](CCCC)CCCC.CCCC[NH+](CCCC)CCCC.CCCC[NH+](CCCC)CCCC.O=P([O-])([O-])OP(=O)([O-])O
null
null
CN(C=O)C.O
Heteroatom Alkylation and Arylation
OtherReaction
7b212c0c068f7c0a0dcdcb2565ee613e3020cb41766d4f4424178d3ecf789f7e
7c33147a6170e63e1fbe1110c4ce069481be57a96b70c4a5a6d7e8253f321bd2
null
[#8:1]-[#15:2](-[O-;H0;D1:3])(-[O;-;D1;H0:4])=[O;D1;H0:5].[C:6]-[C:7]-[N;H0;D3;+0:8](-[CH2;D2;+0:9]-[C:10]-[C:11])-[CH2;D2;+0:12]-[C:13]-[C:14].[cH;D2;+0:15]1:[cH;D2;+0:16]:[cH;D2;+0:17]:[cH;D2;+0:18]:[cH;D2;+0:19]:[n;H0;D2;+0:20]:1>>[#8:1]-[#15:2](-[O;-;D1;H0:4])(=[O;D1;H0:5])-[OH;D1;+0:3].[C:21]-[#7;+:22](-[C:23])-[C...
null
[]
null
null
null
null
Tetrasodium pyrophosphate decahydrate (4.46 g, 10 mmol) was dissolved in the minimum amount of water (about 50 mL) and passed through a column of AG50W X8 (100-200 mesh, 4×10 cm bed) poured in water. The column was eluted with water and the eluent was collected in an ice-cooled flask until pH of the eluent approached n...
10.6084/m9.figshare.5104873.v1
null
Tertiary amine
null
c1ccncc1
null
null
null
CN(C=O)C.O
null
null
CCCCN(CCCC)CCCC.O=P([O-])([O-])OP(=O)([O-])[O-].c1ccncc1>CN(C=O)C.O>CCCC[NH+](CCCC)CCCC.CCCC[NH+](CCCC)CCCC.CCCC[NH+](CCCC)CCCC.O=P([O-])([O-])OP(=O)([O-])O
ord_dataset-02ee2261663048188cf6d85d2cc96e3f
ord-2754db0450694fd5addb217d80c7651c
ClI.O=c1ccn([C@H]2CC[C@@H](CO)O2)c(=O)[nH]1>>O=c1[nH]c(=O)n([C@H]2CC[C@@H](CO)O2)cc1I
[C@@H]1(CC[C@@H](CO)O1)N1C(=O)NC(=O)C=C1.ICl>>IC=1C(NC(N([C@H]2CC[C@@H](CO)O2)C1)=O)=O
Cl[I:16].[O:1]=[c:2]1[nH:3][c:4](=[O:5])[n:6]([C@H:7]2[CH2:8][CH2:9][C@@H:10]([CH2:11][OH:12])[O:13]2)[cH:14][cH:15]1>>[O:1]=[c:2]1[nH:3][c:4](=[O:5])[n:6]([C@H:7]2[CH2:8][CH2:9][C@@H:10]([CH2:11][OH:12])[O:13]2)[cH:14][c:15]1[I:16]
ClI.O=c1ccn([C@H]2CC[C@@H](CO)O2)c(=O)[nH]1
O=c1[nH]c(=O)n([C@H]2CC[C@@H](CO)O2)cc1I
null
null
CO
Functional Group Interconversion
OtherReaction
ab990d4cf4e29f4bfc1eed19f85a157586116cba28cf7e047e67e704b97886a0
3c4065ab4a8681675e06a527dcad54d701c7bfdcac9f73f87773b05034108934
O=c1ccn([C@H]2CCCO2)c(=O)[nH]1
Cl-[I;H0;D1;+0:1].[#8:2]-[C:3]-[#7;a:4]1:[c:5]:[cH;D2;+0:6]:[c:7](=[O;D1;H0:8]):[#7;a:9]:[c:10]:1>>[#8:2]-[C:3]-[#7;a:4]1:[c:5]:[c;H0;D3;+0:6](-[I;H0;D1;+0:1]):[c:7](=[O;D1;H0:8]):[#7;a:9]:[c:10]:1
66
[{"value": 66.0, "product": "IC=1C(NC(N([C@H]2CC[C@@H](CO)O2)C1)=O)=O", "details": "PERCENTYIELD", "is_desired": false}, {"value": 66.0, "product": "IC=1C(NC(N([C@H]2CC[C@@H](CO)O2)C1)=O)=O", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
165
MINUTE
Dideoxyuridine (2.122 g, 10.0 mmol) was dissolved in 30 mL of warm methanol and, after cooling to 25°, iodine monochloride (4.06 g, 25 mmol, 2.5 eq, Fisher) in methanol (20 mL) was added over 5 minutes. The dark purple reaction mixture was heated in a 50° bath under nitrogen for 20 minutes and then immediately cooled i...
10.6084/m9.figshare.5104873.v1
null
null
Aromatic halide
c1ccncn1
c1cncnc1
c1cncnc1.C1CCOC1
HCl
CO
null
2.75
ClI.O=c1ccn([C@H]2CC[C@@H](CO)O2)c(=O)[nH]1>CO>O=c1[nH]c(=O)n([C@H]2CC[C@@H](CO)O2)cc1I
ord_dataset-02ee2261663048188cf6d85d2cc96e3f
ord-f862215dba7846cf8cae5bec600dc198
C#CCNC(=O)C(F)(F)F.O=c1ccn([C@]2(I)O[C@H](CO)[C@@H](O)[C@H]2O)c(=O)[nH]1>>O=C(NCC#Cc1cn([C@H]2CC[C@@H](CO)O2)c(=O)[nH]c1=O)C(F)(F)F
I[C@@]1([C@H](O)[C@H](O)[C@@H](CO)O1)N1C(=O)NC(=O)C=C1.C(C#C)NC(C(F)(F)F)=O.CO>>FC(C(=O)NCC#CC=1C(NC(N([C@H]2CC[C@@H](CO)O2)C1)=O)=O)(F)F
[O:1]=[C:2]([NH:3][CH2:4][C:5]#[CH:6])[C:22]([F:23])([F:24])[F:25].O[C@H:11]1[C@:10](I)([n:9]2[cH:8][cH:7][c:20](=[O:21])[nH:19][c:17]2=[O:18])[O:16][C@H:13]([CH2:14][OH:15])[C@H:12]1O>>[O:1]=[C:2]([NH:3][CH2:4][C:5]#[C:6][c:7]1[cH:8][n:9]([C@H:10]2[CH2:11][CH2:12][C@@H:13]([CH2:14][OH:15])[O:16]2)[c:17](=[O:18])[nH:19...
C#CCNC(=O)C(F)(F)F.O=c1ccn([C@]2(I)O[C@H](CO)[C@@H](O)[C@H]2O)c(=O)[nH]1
O=C(NCC#Cc1cn([C@H]2CC[C@@H](CO)O2)c(=O)[nH]c1=O)C(F)(F)F
null
null
ClCCl
C-C Coupling
OtherReaction
79020e65c8a73c14d651f6b591a1daf884e17a3b0d82391b8a8ea303aeeec2d7
feec4c80e84523492497dfe04bfed80862cb3ade02d554790cab7099c3d3dac5
O=c1ccn([C@H]2CCCO2)c(=O)[nH]1
I-[C@@;H0;D4;+0:1]1(-[#7;a:2]2:[c:3]:[#7;a:4]:[c:5](=[O;D1;H0:6]):[cH;D2;+0:7]:[c:8]:2)-[#8:9]-[C:10](-[C:11])-[C@@H;D3;+0:12](-O)-[C@H;D3;+0:13]-1-O.[C:14]-[C:15]#[CH;D1;+0:16]>>[C:11]-[C:10]1-[#8:9]-[C@@H;D3;+0:1](-[#7;a:2]2:[c:3]:[#7;a:4]:[c:5](=[O;D1;H0:6]):[c;H0;D3;+0:7](-[C;H0;D2;+0:16]#[C:15]-[C:14]):[c:8]:2)-[C...
null
[]
null
null
null
null
Iodouridine 21 was coupled for 3 hours to N-propargyltrifluoroacetamide following the general method given in Example 5C. Chromatography with a 0-5% methanol in dichloromethane gradient afforded material which was homogeneous by TLC, but which was difficult to dry. After co-evaporating the chromatographed product sever...
10.6084/m9.figshare.5104873.v1
null
Tertiary halide.Ether.Secondary alcohol.Secondary alcohol.Alkyne
Ether.Alkyne
C1CCOC1.c1ccncn1
c1cncnc1.C1CCOC1
c1cncnc1.C1CCOC1
HI
ClCCl
null
null
C#CCNC(=O)C(F)(F)F.O=c1ccn([C@]2(I)O[C@H](CO)[C@@H](O)[C@H]2O)c(=O)[nH]1>ClCCl>O=C(NCC#Cc1cn([C@H]2CC[C@@H](CO)O2)c(=O)[nH]c1=O)C(F)(F)F
ord_dataset-02ee2261663048188cf6d85d2cc96e3f
ord-f62f81003c6c41a6ac6db8897b3efe07
O=C(NCC#Cc1cn([C@H]2CC[C@@H](CO)O2)c(=O)[nH]c1=O)C(F)(F)F.O=P([O-])([O-])OP(=O)([O-])OP(=O)([O-])[O-]>>NCC#Cc1cn([C@H]2CC[C@@H](COP(=O)(O)OP(=O)(O)OP(=O)(O)O)O2)c(=O)[nH]c1=O
FC(C(=O)NCC#CC=1C(NC(N([C@H]2CC[C@@H](CO)O2)C1)=O)=O)(F)F.[O-]P([O-])(=O)OP(=O)([O-])OP(=O)([O-])[O-]>>P(O)(=O)(OP(=O)(O)OP(=O)(O)O)OC[C@@H]1CC[C@@H](O1)N1C(=O)NC(=O)C(=C1)C#CCN
O=C(C(F)(F)F)[NH:1][CH2:2][C:3]#[C:4][c:5]1[cH:6][n:7]([C@H:8]2[CH2:9][CH2:10][C@@H:11]([CH2:12][OH:13])[O:26]2)[c:27](=[O:28])[nH:29][c:30]1=[O:31].[O-][P:14](=[O:15])([O-:16])[O:17][P:18](=[O:19])([O-:20])[O:21][P:22](=[O:23])([O-:24])[O-:25]>>[NH2:1][CH2:2][C:3]#[C:4][c:5]1[cH:6][n:7]([C@H:8]2[CH2:9][CH2:10][C@@H:11...
O=C(NCC#Cc1cn([C@H]2CC[C@@H](CO)O2)c(=O)[nH]c1=O)C(F)(F)F.O=P([O-])([O-])OP(=O)([O-])OP(=O)([O-])[O-]
NCC#Cc1cn([C@H]2CC[C@@H](COP(=O)(O)OP(=O)(O)OP(=O)(O)O)O2)c(=O)[nH]c1=O
null
null
null
Miscellaneous
OtherReaction
202bfe9d4cc39183f8a334ff356e45e02f54d921ebf09363277273dabb646529
46156dbef801c93696b95c5685005862403542a82af6e01a304bedb700f59b74
O=c1ccn([C@H]2CCCO2)c(=O)[nH]1
F-C(-F)(-F)-C(=O)-[NH;D2;+0:1]-[C:2]-[C:3]#[C:4]-[c:5](:[c:6]:[#7;a:7]):[c:8]:[#7;a:9].[#8:10]-[C:11]-[C:12]-[OH;D1;+0:13].[O-;H0;D1:14]-[P;H0;D4;+0:15](-[O-])(=[O;D1;H0:16])-[#8:17]-[#15:18](-[O-;H0;D1:19])(=[O;D1;H0:20])-[#8:21]-[#15:22](-[O-;H0;D1:23])(-[O-;H0;D1:24])=[O;D1;H0:25]>>[#7;a:7]:[c:6]:[c:5](-[C:4]#[C:3]-...
null
[]
null
null
210
MINUTE
Alkynylamino nucleoside 22 (0.30 mmol) was converted to the corresponding triphosphate and its trifluoroacetyl group was removed following the general procedure given in Example 5E. After addition of the second aliquot of phosphorus oxychloride, phosphorylation was allowed to proceed for 210 minutes. Assuming an absorp...
10.6084/m9.figshare.5104873.v1
null
Trifluoro group.Secondary amide.Primary alcohol
Primary amine.Phosphate ester
null
null
c1cncnc1.C1CCOC1
Other
null
null
3.5
O=C(NCC#Cc1cn([C@H]2CC[C@@H](CO)O2)c(=O)[nH]c1=O)C(F)(F)F.O=P([O-])([O-])OP(=O)([O-])OP(=O)([O-])[O-]>>NCC#Cc1cn([C@H]2CC[C@@H](COP(=O)(O)OP(=O)(O)OP(=O)(O)O)O2)c(=O)[nH]c1=O
ord_dataset-02ee2261663048188cf6d85d2cc96e3f
ord-4087f7af24ab478188b0f20324748df5
CN.Cc1ccc(S(=O)(=O)OC[C@H]2O[C@@H](n3cc(C)c(=O)[nH]c3=O)C[C@@H]2O)cc1>>CNC[C@H]1O[C@@H](n2cc(C)c(=O)[nH]c2=O)C[C@@H]1O
[K+].[Br-].C1(=CC=C(C=C1)S(=O)(=O)OC[C@@H]1[C@H](C[C@@H](O1)N1C(=O)NC(=O)C(C)=C1)O)C.CN.CN>>CNC[C@@H]1[C@H](C[C@@H](O1)N1C(=O)NC(=O)C(C)=C1)O
[CH3:1][NH2:2].Cc1ccc(S(=O)(=O)O[CH2:3][C@H:4]2[O:5][C@@H:6]([n:7]3[cH:8][c:9]([CH3:10])[c:11](=[O:12])[nH:13][c:14]3=[O:15])[CH2:16][C@@H:17]2[OH:18])cc1>>[CH3:1][NH:2][CH2:3][C@H:4]1[O:5][C@@H:6]([n:7]2[cH:8][c:9]([CH3:10])[c:11](=[O:12])[nH:13][c:14]2=[O:15])[CH2:16][C@@H:17]1[OH:18]
CN.Cc1ccc(S(=O)(=O)OC[C@H]2O[C@@H](n3cc(C)c(=O)[nH]c3=O)C[C@@H]2O)cc1
CNC[C@H]1O[C@@H](n2cc(C)c(=O)[nH]c2=O)C[C@@H]1O
null
null
O
Heteroatom Alkylation and Arylation
OtherReaction
638d8ac0818bc5201610866a65ae9dacec8e97cdcf8f64754391fee0b8c67d26
5fc01bd280a9fcb20b84d795bd8ba6fa3b8702870fcffd0b390748ae9cc9cc09
O=c1ccn([C@H]2CCCO2)c(=O)[nH]1
C-c1:c:c:c(-S(=O)(=O)-O-[CH2;D2;+0:1]-[C:2](-[C:3])-[#8:4]-[C:5]):c:c:1.[C;D1;H3:6]-[NH2;D1;+0:7]>>[C:3]-[C:2](-[CH2;D2;+0:1]-[NH;D2;+0:7]-[C;D1;H3:6])-[#8:4]-[C:5]
null
[]
null
null
3
DAY
5'-O-(p-toluenesulfonyl)thymidine (19.8 g, 50 mmol) was placed in a pressure vessel into which monomethylamine (250 g) was condensed. The vessel was sealed and allowed to stand at room temperature for 3 days. The vessel was cooled, opened, and the monomethylamine allowed to evaporate. The remaining contents of the vess...
10.6084/m9.figshare.5104873.v1
null
Tosylate.Primary amine
Secondary amine
c1ccccc1
null
C1CCOC1.c1cncnc1
TsOH.HO-
O
null
72
CN.Cc1ccc(S(=O)(=O)OC[C@H]2O[C@@H](n3cc(C)c(=O)[nH]c3=O)C[C@@H]2O)cc1>O>CNC[C@H]1O[C@@H](n2cc(C)c(=O)[nH]c2=O)C[C@@H]1O
ord_dataset-02ee2261663048188cf6d85d2cc96e3f
ord-fef06120f7244b028a882a59eab365e0
Cn1c(=O)c2[nH]c(CCCN)nc2n(C)c1=O>>Cn1c(=O)c2[nH]cnc2n(C)c1=O
NCCCC1=NC=2N(C(N(C)C(C2N1)=O)=O)C>>N1(C)C(=O)N(C)C=2N=CNC2C1=O
NCCC[c:7]1[nH:6][c:5]2[c:3](=[O:4])[n:2]([CH3:1])[c:12](=[O:13])[n:10]([CH3:11])[c:9]2[n:8]1>>[CH3:1][n:2]1[c:3](=[O:4])[c:5]2[nH:6][cH:7][n:8][c:9]2[n:10]([CH3:11])[c:12]1=[O:13]
Cn1c(=O)c2[nH]c(CCCN)nc2n(C)c1=O
Cn1c(=O)c2[nH]cnc2n(C)c1=O
null
null
C([O-])([O-])=O
Deprotection
OtherReaction
999929fb35c459640fe6677f54719c0eee39b2af4c6b530442e3859eabba5dc8
5a39875410f78de0778907c5ec963354b592c2b209b9049b152e5c90fc9aa424
O=c1[nH]c(=O)c2[nH]cnc2[nH]1
N-C-C-C-[c;H0;D3;+0:1]1:[#7;a:2]:[c:3]2:[c:4]:[#7;a:5]:[c:6]:[#7;a:7](-[C;D1;H3:8]):[c:9]:2:[#7;a:10]:1>>[C;D1;H3:8]-[#7;a:7]1:[c:6]:[#7;a:5]:[c:4]:[c:3]2:[#7;a:2]:[cH;D2;+0:1]:[#7;a:10]:[c:9]:1:2
null
[]
null
null
null
null
A solution of 5 mM 8-(3-aminopropyl)-theophylline (R.C. Boguslaski et al., 1980) in 0.1 M carbonate buffer, pH 8.0, was incubated with an N-hydroxysuccinimide ester activated dextran surface (according to Example I.3.2) overnight at 25° C., whereupon the surface was washed with water. Conditions: See reaction.notes.pro...
10.6084/m9.figshare.5104873.v1
null
Primary amine
null
c1ncc2[nH]cnc2n1
c1ncc2[nH]cnc2n1
c1ncc2[nH]cnc2n1
Other
C([O-])([O-])=O
null
null
Cn1c(=O)c2[nH]c(CCCN)nc2n(C)c1=O>C([O-])([O-])=O>Cn1c(=O)c2[nH]cnc2n(C)c1=O
ord_dataset-02ee2261663048188cf6d85d2cc96e3f
ord-3e5a74dd499d489bad82923a415203e2
C=CC(Cl)c1ccccc1.C=CC(Cl)c1ccccc1.CC(=O)/C=C(/C)[O-]>>C=Cc1cccc(CC(C(C)=O)C(C)=O)c1
C(=C)C(C1=CC=CC=C1)Cl.C/C(=C/C(=O)C)/[O-].[Na+].[I-].[Na+].C(=C)C(C1=CC=CC=C1)Cl.CC(=O)C.CC(=O)C>>C(=C)C=1C=C(CC(C(C)=O)C(C)=O)C=CC1
C=C[CH:8](Cl)[c:7]1cccc[cH:16]1.C=[CH:1][CH:2](Cl)[c:3]1cc[cH:6][cH:5][cH:4]1.[CH:9](\[C:10]([CH3:11])=[O:12])=[C:13](/[CH3:14])[O-:15]>>[CH2:1]=[CH:2][c:3]1[cH:4][cH:5][cH:6][c:7]([CH2:8][CH:9]([C:10]([CH3:11])=[O:12])[C:13]([CH3:14])=[O:15])[cH:16]1
C=CC(Cl)c1ccccc1.C=CC(Cl)c1ccccc1.CC(=O)/C=C(/C)[O-]
C=Cc1cccc(CC(C(C)=O)C(C)=O)c1
null
null
null
Acylation
OtherReaction
31127f4c33519efa8cacb9513f536f97f4a15745b0e64b22f5c4a87d89e6e123
75acb20a8c8c10d0c404e241869ac0c4b23d8748eee1f1cc1d2051ea4e5952da
c1ccccc1
C=C-[CH;D3;+0:1](-Cl)-[c;H0;D3;+0:2]1:[cH;D2;+0:3]:c:c:c:c:1.C=[CH;D2;+0:4]-[CH;D3;+0:5](-Cl)-[c;H0;D3;+0:6]1:[c:7]:[c:8]:[cH;D2;+0:9]:c:c:1.[C;D1;H3:10]-[C:11](=[O;D1;H0:12])/[CH;D2;+0:13]=[C;H0;D3;+0:14](/[C;D1;H3:15])-[O-;H0;D1:16]>>[C;D1;H3:10]-[C:11](=[O;D1;H0:12])-[CH;D3;+0:13](-[CH2;D2;+0:1]-[c;H0;D3;+0:2]1:[cH;...
null
[]
null
null
null
null
To 308 g of sodium acetylacetonate and 30 g of sodium iodide in 100 mL acetone (dried over 3A molecular sieves) was added dropwise 282 ml vinylbenzyl chloride (70% Meta, 30% Para), in 600 ml acetone. An ice bath was used to keep the pot temperature below 50° during the addition. The solution was maintained at 45°-50° C...
10.6084/m9.figshare.5104873.v1
null
Secondary halide.Secondary halide.Ketone.Vinyl.Vinyl
Ketone.Ketone.Vinyl
c1ccccc1.c1ccccc1
c1ccccc1
c1ccccc1
HCl
null
null
null
C=CC(Cl)c1ccccc1.C=CC(Cl)c1ccccc1.CC(=O)/C=C(/C)[O-]>>C=Cc1cccc(CC(C(C)=O)C(C)=O)c1
ord_dataset-02ee2261663048188cf6d85d2cc96e3f
ord-404ac2a782b04285b1b2dc05ed2a47c8
C=C(C)C(=O)OC.c1ccc2c(c1)Nc1ccccc1S2>>C=C(C)C(=O)OCCCC
C(C(=C)C)(=O)OC.C1=CC=CC=2SC3=CC=CC=C3NC12>>C(C(=C)C)(=O)OCCCC
[CH2:1]=[C:2]([CH3:3])[C:4](=[O:5])[O:6][CH3:7].c1ccc2c(c1)Nc1c[cH:10][cH:8][cH:9]c1S2>>[CH2:1]=[C:2]([CH3:3])[C:4](=[O:5])[O:6][CH2:7][CH2:8][CH2:9][CH3:10]
C=C(C)C(=O)OC.c1ccc2c(c1)Nc1ccccc1S2
C=C(C)C(=O)OCCCC
null
null
C(CCC)O
C-C Coupling
OtherReaction
b29de4aae1a731855e0dbf3b55e482ef9401c13e3f76bf07e7b3578e1662373e
eaa3d0330089f8b63f71d1899090b3847cce744f5ae028d6d671f21ac4689a5e
null
N1-c2:c:[cH;D2;+0:1]:[cH;D2;+0:2]:[cH;D2;+0:3]:c:2-S-c2:c:c:c:c:c:2-1.[C;D1;H2:4]=[C:5]-[C:6](=[O;D1;H0:7])-[#8:8]-[CH3;D1;+0:9]>>[C;D1;H2:4]=[C:5]-[C:6](=[O;D1;H0:7])-[#8:8]-[CH2;D2;+0:9]-[CH2;D2;+0:2]-[CH2;D2;+0:3]-[CH3;D1;+0:1]
null
[]
null
null
6
HOUR
Two hundred six grams of a reaction mix containing a 5:1 mole ratio of methyl methacrylate, 1-butanol, and 100 ppm phenothiazine as inhibitor were added to a 500 ml flask equipped with an agitatior, thermocouple, and a 10-tray Oldershaw fractional distillation column. Thirty grams of the heterogeneous zirconium vinylbe...
10.6084/m9.figshare.5104873.v1
null
Ester.Secondary amine.Monosulfide
Ester
c1ccc2c(c1)Nc1ccccc1S2
null
null
Other
C(CCC)O
null
6
C=C(C)C(=O)OC.c1ccc2c(c1)Nc1ccccc1S2>C(CCC)O>C=C(C)C(=O)OCCCC
ord_dataset-02ee2261663048188cf6d85d2cc96e3f
ord-bff539d21f0449efa90cb66fd5b38883
C=C(C)C(=O)OC.CCCCCCCCCCCCO>>C=C(C)C(=O)OCCCCCCCCCCCC
C(C(=C)C)(=O)OC.C(CCCCCCCCCCC)O.C1=CC=CC=2SC3=CC=CC=C3NC12>>C(C(=C)C)(=O)OCCCCCCCCCCCC
CO[C:4]([C:2](=[CH2:1])[CH3:3])=[O:5].[OH:6][CH2:7][CH2:8][CH2:9][CH2:10][CH2:11][CH2:12][CH2:13][CH2:14][CH2:15][CH2:16][CH2:17][CH3:18]>>[CH2:1]=[C:2]([CH3:3])[C:4](=[O:5])[O:6][CH2:7][CH2:8][CH2:9][CH2:10][CH2:11][CH2:12][CH2:13][CH2:14][CH2:15][CH2:16][CH2:17][CH3:18]
C=C(C)C(=O)OC.CCCCCCCCCCCCO
C=C(C)C(=O)OCCCCCCCCCCCC
null
null
null
Protection
Transesterification
1adccd25c595429871da3756142c075aac7032d22473ca1588e41d51e1a19040
a6c84db4df003bced50681f216baba6e759c1d4451f21f814c7bb7ee782a7375
null
C-O-[C;H0;D3;+0:1](=[O;D1;H0:2])-[C:3](=[C;D1;H2:4])-[C;D1;H3:5].[C:6]-[C:7]-[OH;D1;+0:8]>>[C:6]-[C:7]-[O;H0;D2;+0:8]-[C;H0;D3;+0:1](=[O;D1;H0:2])-[C:3](=[C;D1;H2:4])-[C;D1;H3:5]
null
[]
null
null
6
HOUR
Two hundred six grams of a reaction mix containing a 5:1 mole ratio of methyl methacrylate, 1-dodecanol, and 100 ppm phenothiazine as inhibitor were added to a 500 ml flask equipped with an agitatior, thermocouple, and a 10-tray Oldershaw fractional distillation column. Thirty grams of the heterogeneous zirconium vinyl...
10.6084/m9.figshare.5104873.v1
null
Ester.Primary alcohol
Ester
null
null
null
HO-
null
null
6
C=C(C)C(=O)OC.CCCCCCCCCCCCO>>C=C(C)C(=O)OCCCCCCCCCCCC
ord_dataset-02ee2261663048188cf6d85d2cc96e3f
ord-78085214e0d5496ab614bdad6a715709
C=CCc1noc(CCl)n1.Oc1ccc(F)cc1Cl>>C=CCc1noc(COc2ccc(F)cc2Cl)n1
ClC1=C(C=CC(=C1)F)O.C(C=C)C1=NOC(=N1)CCl.C([O-])([O-])=O.[K+].[K+]>>C(C=C)C1=NOC(=N1)COC1=C(C=C(C=C1)F)Cl
Cl[CH2:8][c:7]1[o:6][n:5][c:4]([CH2:3][CH:2]=[CH2:1])[n:18]1.[OH:9][c:10]1[cH:11][cH:12][c:13]([F:14])[cH:15][c:16]1[Cl:17]>>[CH2:1]=[CH:2][CH2:3][c:4]1[n:5][o:6][c:7]([CH2:8][O:9][c:10]2[cH:11][cH:12][c:13]([F:14])[cH:15][c:16]2[Cl:17])[n:18]1
C=CCc1noc(CCl)n1.Oc1ccc(F)cc1Cl
C=CCc1noc(COc2ccc(F)cc2Cl)n1
null
null
CC(=O)C
Heteroatom Alkylation and Arylation
Williamson Ether Synthesis
7e1040116e3a4cf0e8ec5cc7865388d9cd0efabce6d320a1c25a36e411018d8b
d5f4610d46ccc0478471c5bc0fb862644eaf764bbc5d93badb39d54f6ec8e0a5
c1ccc(OCc2ncno2)cc1
Cl-[CH2;D2;+0:1]-[c:2]1:[#7;a:3]:[c:4]:[#7;a:5]:[#8;a:6]:1.[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]1:[#7;a:3]:[c:4]:[#7;a:5]:[#8;a:6]:1):[c:10]
80.8
[{"value": 80.8, "product": "C(C=C)C1=NOC(=N1)COC1=C(C=C(C=C1)F)Cl", "details": "PERCENTYIELD", "is_desired": false}, {"value": 80.7, "product": "C(C=C)C1=NOC(=N1)COC1=C(C=C(C=C1)F)Cl", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
null
null
0.71 g of 2-chloro-4-fluorophenol, 0.77 g of 3-allyl-5-chloromethyl-1,2,4-oxadiazole and 0.83 of potassium carbonate were added to 20 ml of acetone. After completion of the reaction, the resulting precipitates were filtered out from the mixture and then acetone was removed by distillation, and the residue was purified ...
10.6084/m9.figshare.5104873.v1
null
Primary halide.Aromatic alcohol
Ether
null
null
c1ncon1.c1ccccc1
HCl
CC(=O)C
null
null
C=CCc1noc(CCl)n1.Oc1ccc(F)cc1Cl>CC(=O)C>C=CCc1noc(COc2ccc(F)cc2Cl)n1
ord_dataset-02ee2261663048188cf6d85d2cc96e3f
ord-e5bfa70b33c24bb5b62e1dfb336704c5
CCOC(=O)c1noc(COc2ccc(Cl)cc2Cl)n1>>CCC(=O)c1noc(COc2ccc(Cl)cc2Cl)n1
C(C)OC(=O)C1=NOC(=N1)COC1=C(C=C(C=C1)Cl)Cl.C(C)[Mg]Br.Cl>>C(C)C(=O)C1=NOC(=N1)COC1=C(C=C(C=C1)Cl)Cl
CCO[C:3](=[O:4])[c:5]1[n:6][o:7][c:8]([CH2:9][O:10][c:11]2[cH:12][cH:13][c:14]([Cl:15])[cH:16][c:17]2[Cl:18])[n:19]1>>[CH3:1][CH2:2][C:3](=[O:4])[c:5]1[n:6][o:7][c:8]([CH2:9][O:10][c:11]2[cH:12][cH:13][c:14]([Cl:15])[cH:16][c:17]2[Cl:18])[n:19]1
CCOC(=O)c1noc(COc2ccc(Cl)cc2Cl)n1
CCC(=O)c1noc(COc2ccc(Cl)cc2Cl)n1
null
null
O1CCCC1
Functional Group Interconversion
OtherReaction
600d91131af1bb1ee8c20c567e56234839eb0602aa06d3adc0666216769f9a6a
ebe855e3c62a5d82c9c1d005e3b3e8a9e3b63aca37bc8a601a136cf86007489d
c1ccc(OCc2ncno2)cc1
C-C-O-[C;H0;D3;+0:1](=[O;D1;H0:2])-[c:3]1:[#7;a:4]:[c:5]:[#8;a:6]:[#7;a:7]:1>>[C;D1;H3:8]-[C:9]-[C;H0;D3;+0:1](=[O;D1;H0:2])-[c:3]1:[#7;a:4]:[c:5]:[#8;a:6]:[#7;a:7]:1
83
[{"value": 83.0, "product": "C(C)C(=O)C1=NOC(=N1)COC1=C(C=C(C=C1)Cl)Cl", "details": "PERCENTYIELD", "is_desired": false}]
-78
CELSIUS
1
HOUR
0.95 g of 3-ethoxycarbonyl-5-[(2,4-dichlorophenoxy)methyl]-1,2,4-oxadiazole was added to 30 ml of tetrahydrofuran. The mixture was cooled to -78° C., and then 3 ml of ethylmagnesium bromide (2M solution) was added dropwise. After the mixture was stirred at -78° C. for 1 hour, it was poured into cold aqueous 5% HCl solu...
10.6084/m9.figshare.5104873.v1
null
Ester
Ketone
null
null
c1ncon1.c1ccccc1
Other
O1CCCC1
-78
1
CCOC(=O)c1noc(COc2ccc(Cl)cc2Cl)n1>O1CCCC1>CCC(=O)c1noc(COc2ccc(Cl)cc2Cl)n1
ord_dataset-02ee2261663048188cf6d85d2cc96e3f
ord-ee847813e8e14c88ba9cb5b8597ec847
CCC(=O)c1noc(COc2ccc(Cl)cc2Cl)n1.NO>>CCC(=NO)c1noc(COc2ccc(Cl)cc2Cl)n1
C(C)C(=O)C1=NOC(=N1)COC1=C(C=C(C=C1)Cl)Cl.Cl.ON>>ON=C(CC)C1=NOC(=N1)COC1=C(C=C(C=C1)Cl)Cl
O=[C:3]([CH2:2][CH3:1])[c:6]1[n:7][o:8][c:9]([CH2:10][O:11][c:12]2[cH:13][cH:14][c:15]([Cl:16])[cH:17][c:18]2[Cl:19])[n:20]1.[NH2:4][OH:5]>>[CH3:1][CH2:2][C:3](=[N:4][OH:5])[c:6]1[n:7][o:8][c:9]([CH2:10][O:11][c:12]2[cH:13][cH:14][c:15]([Cl:16])[cH:17][c:18]2[Cl:19])[n:20]1
CCC(=O)c1noc(COc2ccc(Cl)cc2Cl)n1.NO
CCC(=NO)c1noc(COc2ccc(Cl)cc2Cl)n1
null
null
CO
Heteroatom Alkylation and Arylation
OtherReaction
b5fd91d879f097d0ef2e8e2d3ef7d2ef0195968870a9602a47b8324c601790b9
1a0ef15294bdb221fb8888b5d4c7fcf00473b11e53da288791d32747daa48d23
c1ccc(OCc2ncno2)cc1
O=[C;H0;D3;+0:1](-[C:2]-[C;D1;H3:3])-[c:4]1:[#7;a:5]:[c:6]:[#8;a:7]:[#7;a:8]:1.[NH2;D1;+0:9]-[O;D1;H1:10]>>[C;D1;H3:3]-[C:2]-[C;H0;D3;+0:1](=[N;H0;D2;+0:9]-[O;D1;H1:10])-[c:4]1:[#7;a:5]:[c:6]:[#8;a:7]:[#7;a:8]:1
85
[{"value": 85.0, "product": "ON=C(CC)C1=NOC(=N1)COC1=C(C=C(C=C1)Cl)Cl", "details": "PERCENTYIELD", "is_desired": false}, {"value": 84.7, "product": "ON=C(CC)C1=NOC(=N1)COC1=C(C=C(C=C1)Cl)Cl", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
null
null
0.9 g of 3-ethylcarbonyl-5-[(2,4-dichlorophenoxy)methyl]-1,2,4-oxadiazole and 0.21 g of hydroxyamine hydrochloride were added to 10 ml of methanol. The mixture was heated to reflux for 4 hours. After evaporation of methanol, water was added to the residue. The aqueous solution was extracted with ethylacetate. After eva...
10.6084/m9.figshare.5104873.v1
null
Ketone.Primary amine
Oxime
null
null
c1ncon1.c1ccccc1
HO-
CO
null
null
CCC(=O)c1noc(COc2ccc(Cl)cc2Cl)n1.NO>CO>CCC(=NO)c1noc(COc2ccc(Cl)cc2Cl)n1
ord_dataset-02ee2261663048188cf6d85d2cc96e3f
ord-71d372ee817748b9b806f8449f71356b
CCCC(=O)c1noc(COc2ccc(Cl)cc2Cl)n1>>CCCC(O)c1noc(COc2ccc(Cl)cc2Cl)n1
C(CC)C(=O)C1=NOC(=N1)COC1=C(C=C(C=C1)Cl)Cl.CC([O-])C.[Al+3].CC([O-])C.CC([O-])C>>OC(CCC)C1=NOC(=N1)COC1=C(C=C(C=C1)Cl)Cl
[CH3:1][CH2:2][CH2:3][C:4](=[O:5])[c:6]1[n:7][o:8][c:9]([CH2:10][O:11][c:12]2[cH:13][cH:14][c:15]([Cl:16])[cH:17][c:18]2[Cl:19])[n:20]1>>[CH3:1][CH2:2][CH2:3][CH:4]([OH:5])[c:6]1[n:7][o:8][c:9]([CH2:10][O:11][c:12]2[cH:13][cH:14][c:15]([Cl:16])[cH:17][c:18]2[Cl:19])[n:20]1
CCCC(=O)c1noc(COc2ccc(Cl)cc2Cl)n1
CCCC(O)c1noc(COc2ccc(Cl)cc2Cl)n1
null
null
C(C)(C)O
Reduction
Reduction of ketone to secondary alcohol
02790ac194d8bf7ccb13d6247c59412024d87f77d2c906ef7804f021f57d5070
1bd3cd74b454139c0a0068ac0135836499926b274bff569df163210c6c944a89
c1ccc(OCc2ncno2)cc1
[C:1]-[C:2]-[C;H0;D3;+0:3](=[O;H0;D1;+0:4])-[c:5]1:[#7;a:6]:[c:7]:[#8;a:8]:[#7;a:9]:1>>[C:1]-[C:2]-[CH;D3;+0:3](-[OH;D1;+0:4])-[c:5]1:[#7;a:6]:[c:7]:[#8;a:8]:[#7;a:9]:1
54
[{"value": 54.0, "product": "OC(CCC)C1=NOC(=N1)COC1=C(C=C(C=C1)Cl)Cl", "details": "PERCENTYIELD", "is_desired": false}, {"value": 53.5, "product": "OC(CCC)C1=NOC(=N1)COC1=C(C=C(C=C1)Cl)Cl", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
null
null
0.316 g of 3-propylcarbonyl-5-[(2,4-dichlorophenoxy)methyl]-1,2,4-oxadiazole and 0.20 g of aluminum isopropoxide were added to 10 ml of isopropanol. The mixture was heated to reflux for 48 hours. After evaporation of isopropanol, water was added to the residue. The aqueous solution was extracted with ethylacetate. Afte...
10.6084/m9.figshare.5104873.v1
null
Ketone
Secondary alcohol
null
null
c1ncon1.c1ccccc1
null
C(C)(C)O
null
null
CCCC(=O)c1noc(COc2ccc(Cl)cc2Cl)n1>C(C)(C)O>CCCC(O)c1noc(COc2ccc(Cl)cc2Cl)n1
ord_dataset-02ee2261663048188cf6d85d2cc96e3f
ord-f7f78b9b17294d74a78dab97f5765fd7
CO.Clc1ccc(OCc2nc(C(Cl)(Cl)Cl)no2)c(Cl)c1.N>>N=COCc1noc(COc2ccc(Cl)cc2Cl)n1
ClC(C1=NOC(=N1)COC1=C(C=C(C=C1)Cl)Cl)(Cl)Cl.CO.N>>N=COCC1=NOC(=N1)COC1=C(C=C(C=C1)Cl)Cl
[CH3:2][OH:3].Cl[C:4](Cl)(Cl)[c:5]1[n:6][o:7][c:8]([CH2:9][O:10][c:11]2[cH:12][cH:13][c:14]([Cl:15])[cH:16][c:17]2[Cl:18])[n:19]1.[NH3:1]>>[NH:1]=[CH:2][O:3][CH2:4][c:5]1[n:6][o:7][c:8]([CH2:9][O:10][c:11]2[cH:12][cH:13][c:14]([Cl:15])[cH:16][c:17]2[Cl:18])[n:19]1
CO.Clc1ccc(OCc2nc(C(Cl)(Cl)Cl)no2)c(Cl)c1.N
N=COCc1noc(COc2ccc(Cl)cc2Cl)n1
null
null
null
Heteroatom Alkylation and Arylation
OtherReaction
3165328e1df447a7b4dd544a286cfa722eec7f2e0dcc6edb1d8edee130bac9d1
d4b362c6db8558ccca20b721b79cf14321d12ee6b3f0a59f0c6ad4b2ff912dd6
c1ccc(OCc2ncno2)cc1
Cl-[C;H0;D4;+0:1](-Cl)(-Cl)-[c:2]1:[#7;a:3]:[c:4]:[#8;a:5]:[#7;a:6]:1.[CH3;D1;+0:7]-[OH;D1;+0:8].[NH3;D0;+0:9]>>[NH;D1;+0:9]=[CH;D2;+0:7]-[O;H0;D2;+0:8]-[CH2;D2;+0:1]-[c:2]1:[#7;a:3]:[c:4]:[#8;a:5]:[#7;a:6]:1
50.9
[{"value": 50.9, "product": "N=COCC1=NOC(=N1)COC1=C(C=C(C=C1)Cl)Cl", "details": "PERCENTYIELD", "is_desired": false}]
null
null
4
HOUR
2.17 g of 3-(trichloromethyl)-5-[(2,4-dichlorophenoxy)methyl]-1,2,4-oxadiazole was added to 50 ml of methanol. An excess of ammonia gas was added with formation of bubble at 0° C. and then the mixture was stirred at room temperature for 4 hours. After evaporation of methanol, water was added to the residue. The aqueous...
10.6084/m9.figshare.5104873.v1
null
Trichloro group.Methanol
Ether
null
null
c1ncon1.c1ccccc1
HCl
null
null
4
CO.Clc1ccc(OCc2nc(C(Cl)(Cl)Cl)no2)c(Cl)c1.N>>N=COCc1noc(COc2ccc(Cl)cc2Cl)n1
ord_dataset-02ee2261663048188cf6d85d2cc96e3f
ord-0486b163d93d4c4098549fecca2a4eab
CC1=C(C)C(=O)OC1=O.Nc1ccc(Cl)c(S(N)(=O)=O)c1>>CC1=C(C)C(=O)N(c2ccc(Cl)c(S(N)(=O)=O)c2)C1=O
NC=1C=CC(=C(C1)S(=O)(=O)N)Cl.C/C=1/C(=O)OC(\C1\C)=O>>ClC1=C(C=C(C=C1)N1C(C(=C(C1=O)C)C)=O)S(=O)(=O)N
O1[C:5](=[O:6])[C:3]([CH3:4])=[C:2]([CH3:1])[C:19]1=[O:20].[NH2:7][c:8]1[cH:9][cH:10][c:11]([Cl:12])[c:13]([S:14]([NH2:15])(=[O:16])=[O:17])[cH:18]1>>[CH3:1][C:2]1=[C:3]([CH3:4])[C:5](=[O:6])[N:7]([c:8]2[cH:9][cH:10][c:11]([Cl:12])[c:13]([S:14]([NH2:15])(=[O:16])=[O:17])[cH:18]2)[C:19]1=[O:20]
CC1=C(C)C(=O)OC1=O.Nc1ccc(Cl)c(S(N)(=O)=O)c1
CC1=C(C)C(=O)N(c2ccc(Cl)c(S(N)(=O)=O)c2)C1=O
null
null
N1=CC=CC=C1
Acylation
OtherReaction
cab1acd179957d4f5c27ba23f314ee257f7d508deff2838c7964b1019063e651
2a4a20e639c386292668b0b265a8e1b50d707d5f0576437dc5ade3e7fd444d29
O=C1C=CC(=O)N1c1ccccc1
[C;D1;H3:1]-[C:2]1=[C:3](-[C;D1;H3:4])-[C;H0;D3;+0:5](=[O;D1;H0:6])-O-[C;H0;D3;+0:7]-1=[O;D1;H0:8].[NH2;D1;+0:9]-[c:10](:[c:11]):[c:12]>>[C;D1;H3:1]-[C:2]1=[C:3](-[C;D1;H3:4])-[C;H0;D3;+0:5](=[O;D1;H0:6])-[N;H0;D3;+0:9](-[c:10](:[c:11]):[c:12])-[C;H0;D3;+0:7]-1=[O;D1;H0:8]
93
[{"value": 93.0, "product": "ClC1=C(C=C(C=C1)N1C(C(=C(C1=O)C)C)=O)S(=O)(=O)N", "details": "PERCENTYIELD", "is_desired": false}]
null
null
20
MINUTE
In 3 ml of pyridine, 1 mmol of 5-amino-2-chlorobenzenesulfonamide and 1.05 mmol of 2,3-dimethylmaleic anhydride were stirred at 90-100° C. for 9 hours. Pyridine was then distilled off from the reaction mixture, followed by the addition of 20 ml of ice water and 0.1 ml of 35% hydrochloric acid to the solid residue. Afte...
10.6084/m9.figshare.5104873.v1
null
Anhydride.Primary amine
Substituted dicarboximide
C1=CCOC1
C1=CC[NH]C1
C1=CC[NH]C1.c1ccccc1
HO-
N1=CC=CC=C1
null
0.333333
CC1=C(C)C(=O)OC1=O.Nc1ccc(Cl)c(S(N)(=O)=O)c1>N1=CC=CC=C1>CC1=C(C)C(=O)N(c2ccc(Cl)c(S(N)(=O)=O)c2)C1=O
ord_dataset-02ee2261663048188cf6d85d2cc96e3f
ord-b9ac6e1cabe64925a2abe6ef104073ff
CC1=C(C)C(=O)OC1=O.COC(=O)c1ccc(N)cc1S(N)(=O)=O>>COC(=O)c1ccc(N2C(=O)C(C)=C(C)C2=O)cc1S(N)(=O)=O
NC1=CC(=C(C(=O)OC)C=C1)S(=O)(=O)N.C/C=1/C(=O)OC(\C1\C)=O>>NS(=O)(=O)C1=C(C(=O)OC)C=CC(=C1)N1C(C(=C(C1=O)C)C)=O
O1[C:10](=[O:11])[C:12]([CH3:13])=[C:14]([CH3:15])[C:16]1=[O:17].[CH3:1][O:2][C:3](=[O:4])[c:5]1[cH:6][cH:7][c:8]([NH2:9])[cH:18][c:19]1[S:20]([NH2:21])(=[O:22])=[O:23]>>[CH3:1][O:2][C:3](=[O:4])[c:5]1[cH:6][cH:7][c:8]([N:9]2[C:10](=[O:11])[C:12]([CH3:13])=[C:14]([CH3:15])[C:16]2=[O:17])[cH:18][c:19]1[S:20]([NH2:21])(=...
CC1=C(C)C(=O)OC1=O.COC(=O)c1ccc(N)cc1S(N)(=O)=O
COC(=O)c1ccc(N2C(=O)C(C)=C(C)C2=O)cc1S(N)(=O)=O
null
null
C(C)(=O)O
Acylation
OtherReaction
cab1acd179957d4f5c27ba23f314ee257f7d508deff2838c7964b1019063e651
2a4a20e639c386292668b0b265a8e1b50d707d5f0576437dc5ade3e7fd444d29
O=C1C=CC(=O)N1c1ccccc1
[C;D1;H3:1]-[C:2]1=[C:3](-[C;D1;H3:4])-[C;H0;D3;+0:5](=[O;D1;H0:6])-O-[C;H0;D3;+0:7]-1=[O;D1;H0:8].[NH2;D1;+0:9]-[c:10](:[c:11]):[c:12]>>[C;D1;H3:1]-[C:2]1=[C:3](-[C;D1;H3:4])-[C;H0;D3;+0:5](=[O;D1;H0:6])-[N;H0;D3;+0:9](-[c:10](:[c:11]):[c:12])-[C;H0;D3;+0:7]-1=[O;D1;H0:8]
43
[{"value": 43.0, "product": "NS(=O)(=O)C1=C(C(=O)OC)C=CC(=C1)N1C(C(=C(C1=O)C)C)=O", "details": "PERCENTYIELD", "is_desired": false}]
null
null
2
HOUR
In 3 ml of acetic acid, 1 mmol of methyl 4-amino-2-(aminosulfonyl)benzoate and 1.05 mmol of 2,3-dimethylmaleic anhydride were stirred at 80° C. for 40 hours. Acetic acid was then distilled off from the reaction mixture, followed by the addition of 20 ml of ice water to the oily residue. After the mixture thus formed wa...
10.6084/m9.figshare.5104873.v1
null
Anhydride.Primary amine
Substituted dicarboximide
C1=CCOC1
C1=CC[NH]C1
c1ccccc1.C1=CC[NH]C1
HO-
C(C)(=O)O
null
2
CC1=C(C)C(=O)OC1=O.COC(=O)c1ccc(N)cc1S(N)(=O)=O>C(C)(=O)O>COC(=O)c1ccc(N2C(=O)C(C)=C(C)C2=O)cc1S(N)(=O)=O
ord_dataset-02ee2261663048188cf6d85d2cc96e3f
ord-a7a4e504e0e84b019b4a1e1fa710be55
COC(=O)c1c(Sc2nc(OC)cc(OC)n2)cccc1C(C)=O.CON>>CON=C(C)c1cccc(Sc2nc(OC)cc(OC)n2)c1C(=O)OC
C([O-])([O-])=O.[K+].[K+].COC1=NC(=NC(=C1)OC)SC1=C(C(=O)OC)C(=CC=C1)C(C)=O.Cl.CON.O>>COC1=NC(=NC(=C1)OC)SC1=C(C(=O)OC)C(=CC=C1)C(C)=NOC
O=[C:4]([CH3:5])[c:6]1[cH:7][cH:8][cH:9][c:10]([S:11][c:12]2[n:13][c:14]([O:15][CH3:16])[cH:17][c:18]([O:19][CH3:20])[n:21]2)[c:22]1[C:23](=[O:24])[O:25][CH3:26].[CH3:1][O:2][NH2:3]>>[CH3:1][O:2][N:3]=[C:4]([CH3:5])[c:6]1[cH:7][cH:8][cH:9][c:10]([S:11][c:12]2[n:13][c:14]([O:15][CH3:16])[cH:17][c:18]([O:19][CH3:20])[n:2...
COC(=O)c1c(Sc2nc(OC)cc(OC)n2)cccc1C(C)=O.CON
CON=C(C)c1cccc(Sc2nc(OC)cc(OC)n2)c1C(=O)OC
null
null
CO
Heteroatom Alkylation and Arylation
OtherReaction
3d7a74a3d1c5abb5292963d4a3067f1fb8a89aead752dc9bb1d63522c4c0bd5c
6b0edeaa66853687109d0d530554f76edf36b01a8ec084e7ae9c709f0949a6b9
c1ccc(Sc2ncccn2)cc1
O=[C;H0;D3;+0:1](-[C;D1;H3:2])-[c:3](:[c:4]):[c:5]-[C:6](-[#8:7])=[O;D1;H0:8].[C;D1;H3:9]-[#8:10]-[NH2;D1;+0:11]>>[#8:7]-[C:6](=[O;D1;H0:8])-[c:5]:[c:3](-[C;H0;D3;+0:1](-[C;D1;H3:2])=[N;H0;D2;+0:11]-[#8:10]-[C;D1;H3:9]):[c:4]
60
[{"value": 59.0, "product": "COC1=NC(=NC(=C1)OC)SC1=C(C(=O)OC)C(=CC=C1)C(C)=NOC", "details": "PERCENTYIELD", "is_desired": false}, {"value": 60.0, "product": "COC1=NC(=NC(=C1)OC)SC1=C(C(=O)OC)C(=CC=C1)C(C)=NOC", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
null
null
1.0 g of methyl 2-[(4,6-dimethoxypyrimidin-2-yl)thio]-6-acetylbenzoate and 0.5 g of methoxyamine hydrochloride were dissolved in 6 ml of methanol, and the resultant solution was refluxed for 15 minutes. After cooling the mixed liquor to room temperature, 0.8 g of potassium carbonate was added to this liquor and the res...
10.6084/m9.figshare.5104873.v1
null
Ketone.Primary amine
null
null
null
c1ccccc1.c1cncnc1
HO-
CO
null
null
COC(=O)c1c(Sc2nc(OC)cc(OC)n2)cccc1C(C)=O.CON>CO>CON=C(C)c1cccc(Sc2nc(OC)cc(OC)n2)c1C(=O)OC
ord_dataset-02ee2261663048188cf6d85d2cc96e3f
ord-bef430985b434ffd803e950af8b3d2e0
COC(=O)c1c(O)cccc1C=O.COc1cc(OC)nc(S(C)(=O)=O)n1>>COC(=O)c1c(C=O)cccc1Oc1nc(OC)cc(OC)n1
C(=O)C1=C(C(=O)OC)C(=CC=C1)O.COC1=NC(=NC(=C1)OC)S(=O)(=O)C.C([O-])([O-])=O.[K+].[K+]>>COC1=NC(=NC(=C1)OC)OC1=C(C(=O)OC)C(=CC=C1)C=O
[CH3:1][O:2][C:3](=[O:4])[c:5]1[c:6]([CH:7]=[O:8])[cH:9][cH:10][cH:11][c:12]1[OH:13].CS(=O)(=O)[c:14]1[n:15][c:16]([O:17][CH3:18])[cH:19][c:20]([O:21][CH3:22])[n:23]1>>[CH3:1][O:2][C:3](=[O:4])[c:5]1[c:6]([CH:7]=[O:8])[cH:9][cH:10][cH:11][c:12]1[O:13][c:14]1[n:15][c:16]([O:17][CH3:18])[cH:19][c:20]([O:21][CH3:22])[n:23...
COC(=O)c1c(O)cccc1C=O.COc1cc(OC)nc(S(C)(=O)=O)n1
COC(=O)c1c(C=O)cccc1Oc1nc(OC)cc(OC)n1
null
null
CN(C)C=O
Heteroatom Alkylation and Arylation
OtherReaction
1c345af4a3df0f977c6c030350153f590996fc7a2b6ceaf9fe6cff27648ed228
5df75ac15caf6173d8206dd70d45a57321a6ccb2169690bfa04f02c58252d4f1
c1ccc(Oc2ncccn2)cc1
C-S(=O)(=O)-[c;H0;D3;+0:1](:[#7;a:2]:[c:3]):[#7;a:4]:[c:5].[#8:6]-[C:7](=[O;D1;H0:8])-[c:9]:[c:10](-[OH;D1;+0:11]):[c:12]>>[#8:6]-[C:7](=[O;D1;H0:8])-[c:9]:[c:10](-[O;H0;D2;+0:11]-[c;H0;D3;+0:1](:[#7;a:2]:[c:3]):[#7;a:4]:[c:5]):[c:12]
56.1
[{"value": 52.0, "product": "COC1=NC(=NC(=C1)OC)OC1=C(C(=O)OC)C(=CC=C1)C=O", "details": "PERCENTYIELD", "is_desired": false}, {"value": 56.1, "product": "COC1=NC(=NC(=C1)OC)OC1=C(C(=O)OC)C(=CC=C1)C=O", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
null
null
13.8 g of potassium carbonate and 50 ml of DMF were placed in a 200 ml eggplant type flask, and 11.1 g of methyl 2-formyl-6-hydroxybenzoate and 14.6 g of 4,6-dimethoxy-2-methanesulfonylpyrimidine were added thereto with stirring. The mixture was stirred at 80° C. for 1 hour, and the resultant liquor was poured into an ...
10.6084/m9.figshare.5104873.v1
null
Aromatic alcohol.Sulfone
Ether
c1cncnc1
c1cncnc1
c1ccccc1.c1cncnc1
HO-
CN(C)C=O
null
null
COC(=O)c1c(O)cccc1C=O.COc1cc(OC)nc(S(C)(=O)=O)n1>CN(C)C=O>COC(=O)c1c(C=O)cccc1Oc1nc(OC)cc(OC)n1
ord_dataset-02ee2261663048188cf6d85d2cc96e3f
ord-e77e497ab65949148fe18d9b14c87ef9
COC(=O)c1c(C=O)cccc1Oc1nc(OC)cc(OC)n1.NO>>COC(=O)c1c(C=NO)cccc1Oc1nc(OC)cc(OC)n1
COC1=NC(=NC(=C1)OC)OC1=C(C(=O)OC)C(=CC=C1)C=O.Cl.ON.C(C)(=O)[O-].[K+]>>COC1=NC(=NC(=C1)OC)OC1=C(C(=O)OC)C(=CC=C1)C=NO
O=[CH:7][c:6]1[c:5]([C:3]([O:2][CH3:1])=[O:4])[c:13]([O:14][c:15]2[n:16][c:17]([O:18][CH3:19])[cH:20][c:21]([O:22][CH3:23])[n:24]2)[cH:12][cH:11][cH:10]1.[NH2:8][OH:9]>>[CH3:1][O:2][C:3](=[O:4])[c:5]1[c:6]([CH:7]=[N:8][OH:9])[cH:10][cH:11][cH:12][c:13]1[O:14][c:15]1[n:16][c:17]([O:18][CH3:19])[cH:20][c:21]([O:22][CH3:2...
COC(=O)c1c(C=O)cccc1Oc1nc(OC)cc(OC)n1.NO
COC(=O)c1c(C=NO)cccc1Oc1nc(OC)cc(OC)n1
null
null
CO
Heteroatom Alkylation and Arylation
OtherReaction
26f32c058bcc6b69b34e9c38433bccb165270e0a55ab24439c783c1aee9d8dac
3593c4a8dedbac5f92a1a749cef37ecd686935362f91b9154f0c9930a5edea38
c1ccc(Oc2ncccn2)cc1
O=[CH;D2;+0:1]-[c:2](:[c:3]):[c:4]-[C:5](-[#8:6])=[O;D1;H0:7].[NH2;D1;+0:8]-[O;D1;H1:9]>>[#8:6]-[C:5](=[O;D1;H0:7])-[c:4]:[c:2](-[CH;D2;+0:1]=[N;H0;D2;+0:8]-[O;D1;H1:9]):[c:3]
72
[{"value": 72.0, "product": "COC1=NC(=NC(=C1)OC)OC1=C(C(=O)OC)C(=CC=C1)C=NO", "details": "PERCENTYIELD", "is_desired": false}, {"value": 71.6, "product": "COC1=NC(=NC(=C1)OC)OC1=C(C(=O)OC)C(=CC=C1)C=NO", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
10
MINUTE
2.0 g of methyl 2-[(4,6-dimethoxypyrimidin-2-yl)oxy]-6-formylbenzoate, 0.8 g of hydroxyamine hydrochloride, 1.1 g of potassium acetate and 10 ml of methanol were placed in a 50 ml eggplant type flask, and were stirred for 10 minutes at room temperature. Methanol was distilled off under reduced pressure, and the residue...
10.6084/m9.figshare.5104873.v1
null
Aldehyde.Primary amine
Oxime
null
null
c1ccccc1.c1cncnc1
HO-
CO
null
0.166667
COC(=O)c1c(C=O)cccc1Oc1nc(OC)cc(OC)n1.NO>CO>COC(=O)c1c(C=NO)cccc1Oc1nc(OC)cc(OC)n1
ord_dataset-02ee2261663048188cf6d85d2cc96e3f
ord-58d146d694ce48609c737e896ac57533
CCOC(=O)C(C)Br.COC(=O)c1c(C=NO)cccc1Oc1nc(OC)cc(OC)n1>>CCOC(=O)C(C)ON=Cc1cccc(Oc2nc(OC)cc(OC)n2)c1C(=O)OC
COC1=NC(=NC(=C1)OC)OC1=C(C(=O)OC)C(=CC=C1)C=NO.BrC(C(=O)OCC)C>>COC1=NC(=NC(=C1)OC)OC1=C(C(=O)OC)C(=CC=C1)C=NOC(C)C(=O)OCC
Br[CH:6]([C:4]([O:3][CH2:2][CH3:1])=[O:5])[CH3:7].[OH:8][N:9]=[CH:10][c:11]1[cH:12][cH:13][cH:14][c:15]([O:16][c:17]2[n:18][c:19]([O:20][CH3:21])[cH:22][c:23]([O:24][CH3:25])[n:26]2)[c:27]1[C:28](=[O:29])[O:30][CH3:31]>>[CH3:1][CH2:2][O:3][C:4](=[O:5])[CH:6]([CH3:7])[O:8][N:9]=[CH:10][c:11]1[cH:12][cH:13][cH:14][c:15](...
CCOC(=O)C(C)Br.COC(=O)c1c(C=NO)cccc1Oc1nc(OC)cc(OC)n1
CCOC(=O)C(C)ON=Cc1cccc(Oc2nc(OC)cc(OC)n2)c1C(=O)OC
null
[Ag]=O
CC(=O)C
Heteroatom Alkylation and Arylation
OtherReaction
5b3220c592c1ff8e56030890b9220853f42f069aeea0537edf1f26ba44e3a466
eaa3d712fa7ce293731d22b792157600787d0e3bec44c5b4827bc124713fbe82
c1ccc(Oc2ncccn2)cc1
Br-[CH;D3;+0:1](-[C;D1;H3:2])-[C:3](=[O;D1;H0:4])-[#8:5]-[C:6].[OH;D1;+0:7]-[#7:8]=[C:9]-[c:10]>>[C:6]-[#8:5]-[C:3](=[O;D1;H0:4])-[CH;D3;+0:1](-[C;D1;H3:2])-[O;H0;D2;+0:7]-[#7:8]=[C:9]-[c:10]
27
[{"value": 27.0, "product": "COC1=NC(=NC(=C1)OC)OC1=C(C(=O)OC)C(=CC=C1)C=NOC(C)C(=O)OCC", "details": "PERCENTYIELD", "is_desired": false}]
null
null
null
null
2.0 g of methyl 2-[(4,6-dimethoxypyrimidin-2-yl)oxy]-6-hydroxyiminomethylbenzoate, 3 ml of ethyl 2-bromopropionate and 0.9 g of silver oxide (I) were place in a 50 ml eggplant type flask, and were allowed to stand for one night at room temperature. 10 ml of acetone and 10 g of silica gel were added to the resultant rea...
10.6084/m9.figshare.5104873.v1
null
Secondary halide.Ester.Oxime
Ester
null
null
c1ccccc1.c1cncnc1
HBr
[Ag]=O.CC(=O)C
null
null
CCOC(=O)C(C)Br.COC(=O)c1c(C=NO)cccc1Oc1nc(OC)cc(OC)n1>[Ag]=O.CC(=O)C>CCOC(=O)C(C)ON=Cc1cccc(Oc2nc(OC)cc(OC)n2)c1C(=O)OC
ord_dataset-02ee2261663048188cf6d85d2cc96e3f
ord-d4e0e0fd7a664fc7b02425517796a68b
COC(=O)c1c(O)cccc1C(C)=O.COC1=CC(OC)=NN(Cl)N1>>COC(=O)c1c(ON2N=C(OC)C=C(OC)N2)cccc1C(C)=O
C(C)(=O)C=1C=CC=C(C1C(=O)OC)O.[H-].[Na+].C1=CC=CC=C1.ClN1NC(=CC(=N1)OC)OC>>C(C)(=O)C1=C(C(=O)OC)C(=CC=C1)ON1NC(=CC(=N1)OC)OC
[CH3:1][O:2][C:3](=[O:4])[c:5]1[c:6]([OH:7])[cH:18][cH:19][cH:20][c:21]1[C:22]([CH3:23])=[O:24].Cl[N:8]1[N:9]=[C:10]([O:11][CH3:12])[CH:13]=[C:14]([O:15][CH3:16])[NH:17]1>>[CH3:1][O:2][C:3](=[O:4])[c:5]1[c:6]([O:7][N:8]2[N:9]=[C:10]([O:11][CH3:12])[CH:13]=[C:14]([O:15][CH3:16])[NH:17]2)[cH:18][cH:19][cH:20][c:21]1[C:22...
COC(=O)c1c(O)cccc1C(C)=O.COC1=CC(OC)=NN(Cl)N1
COC(=O)c1c(ON2N=C(OC)C=C(OC)N2)cccc1C(C)=O
null
null
O
Miscellaneous
OtherReaction
59ca52d02f18f6f1cf694bf6135fe35f5ebb54812490bc5f05c6acbea73cb85f
353e49c7be80af9aebc634afb2cd1a6a6f10d92d32a4386b7fb0f5327d26735f
C1=CNN(Oc2ccccc2)N=C1
Cl-[N;H0;D3;+0:1]1-[#7:2]-[C:3](-[#8:4])=[C:5]-[C:6](-[#8:7])=[#7:8]-1.[#8:9]-[C:10](=[O;D1;H0:11])-[c:12]:[c:13](-[OH;D1;+0:14]):[c:15]>>[#8:7]-[C:6]1=[#7:8]-[N;H0;D3;+0:1](-[O;H0;D2;+0:14]-[c:13](:[c:15]):[c:12]-[C:10](-[#8:9])=[O;D1;H0:11])-[#7:2]-[C:3](-[#8:4])=[C:5]-1
67
[{"value": 67.0, "product": "C(C)(=O)C1=C(C(=O)OC)C(=CC=C1)ON1NC(=CC(=N1)OC)OC", "details": "PERCENTYIELD", "is_desired": false}, {"value": 66.6, "product": "C(C)(=O)C1=C(C(=O)OC)C(=CC=C1)ON1NC(=CC(=N1)OC)OC", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
1
DAY
1.0 g of methyl 6-acetylsalicylate was added to a suspension solution of 0.23 g of sodium hydride and 30 ml of benzene, and the resultant mixture was stirred for 10 minutes at room temperature. 0.95 g of 2-chloro-4,6-dimethoxytriazine was added to the resultant mixture, and the mixture was stirred for one day and one n...
10.6084/m9.figshare.5104873.v1
null
Hydrazine.Hydrazone.Aromatic alcohol
Hydrazine.Hydrazone
C1=CN[NH]N=C1
C1=CN[NH]N=C1
c1ccccc1.C1=CN[NH]N=C1
HCl
O
null
24
COC(=O)c1c(O)cccc1C(C)=O.COC1=CC(OC)=NN(Cl)N1>O>COC(=O)c1c(ON2N=C(OC)C=C(OC)N2)cccc1C(C)=O
ord_dataset-02ee2261663048188cf6d85d2cc96e3f
ord-9caf7f2af9b04e69903afed00c9e43d0
COC(=O)c1c(ON2N=C(OC)C=C(OC)N2)cccc1C(C)=O.CON>>CON=C(C)c1cccc(ON2N=C(OC)C=C(OC)N2)c1C(=O)OC
C(C)(=O)C1=C(C(=O)OC)C(=CC=C1)ON1NC(=CC(=N1)OC)OC.Cl.CON.C(C)(=O)[O-].[K+].CO>>COC1=NN(NC(=C1)OC)OC1=C(C(=O)OC)C(=CC=C1)C(C)=NOC
O=[C:4]([CH3:5])[c:6]1[cH:7][cH:8][cH:9][c:10]([O:11][N:12]2[N:13]=[C:14]([O:15][CH3:16])[CH:17]=[C:18]([O:19][CH3:20])[NH:21]2)[c:22]1[C:23](=[O:24])[O:25][CH3:26].[CH3:1][O:2][NH2:3]>>[CH3:1][O:2][N:3]=[C:4]([CH3:5])[c:6]1[cH:7][cH:8][cH:9][c:10]([O:11][N:12]2[N:13]=[C:14]([O:15][CH3:16])[CH:17]=[C:18]([O:19][CH3:20]...
COC(=O)c1c(ON2N=C(OC)C=C(OC)N2)cccc1C(C)=O.CON
CON=C(C)c1cccc(ON2N=C(OC)C=C(OC)N2)c1C(=O)OC
null
null
O
Heteroatom Alkylation and Arylation
OtherReaction
3d7a74a3d1c5abb5292963d4a3067f1fb8a89aead752dc9bb1d63522c4c0bd5c
6b0edeaa66853687109d0d530554f76edf36b01a8ec084e7ae9c709f0949a6b9
C1=CNN(Oc2ccccc2)N=C1
O=[C;H0;D3;+0:1](-[C;D1;H3:2])-[c:3](:[c:4]):[c:5]-[C:6](-[#8:7])=[O;D1;H0:8].[C;D1;H3:9]-[#8:10]-[NH2;D1;+0:11]>>[#8:7]-[C:6](=[O;D1;H0:8])-[c:5]:[c:3](-[C;H0;D3;+0:1](-[C;D1;H3:2])=[N;H0;D2;+0:11]-[#8:10]-[C;D1;H3:9]):[c:4]
48
[{"value": 48.0, "product": "COC1=NN(NC(=C1)OC)OC1=C(C(=O)OC)C(=CC=C1)C(C)=NOC", "details": "PERCENTYIELD", "is_desired": false}]
null
null
null
null
0.9 of methyl 2-acetyl-6-[(4,6-dimethoxytriazin-2-yl)oxy]benzoate, 0.68 g of methoxyamine hydrochloride and 0.80 g of potassium acetate were added to 30 ml of methanol, and the resultant mixture was stirred for one day and one night at room temperature. The resultant reaction liquor was poured into water, and was extra...
10.6084/m9.figshare.5104873.v1
null
Ketone.Primary amine
null
null
null
c1ccccc1.C1=CN[NH]N=C1
HO-
O
null
null
COC(=O)c1c(ON2N=C(OC)C=C(OC)N2)cccc1C(C)=O.CON>O>CON=C(C)c1cccc(ON2N=C(OC)C=C(OC)N2)c1C(=O)OC
ord_dataset-02ee2261663048188cf6d85d2cc96e3f
ord-f731ed3622dd4070b9453e090fd140d9
C=CCON.COC(=O)c1c(Oc2nc(OC)cc(OC)n2)cccc1C(C)=O>>C=CCON=C(C)c1cccc(Oc2nc(OC)cc(OC)n2)c1C(=O)OC
C(C)(=O)C1=C(C(=O)OC)C(=CC=C1)OC1=NC(=CC(=N1)OC)OC.Cl.C(C=C)ON.C(C)(=O)[O-].[K+].CO>>C(C=C)ON=C(C)C1=C(C(=O)OC)C(=CC=C1)OC1=NC(=CC(=N1)OC)OC
[CH2:1]=[CH:2][CH2:3][O:4][NH2:5].O=[C:6]([CH3:7])[c:8]1[cH:9][cH:10][cH:11][c:12]([O:13][c:14]2[n:15][c:16]([O:17][CH3:18])[cH:19][c:20]([O:21][CH3:22])[n:23]2)[c:24]1[C:25](=[O:26])[O:27][CH3:28]>>[CH2:1]=[CH:2][CH2:3][O:4][N:5]=[C:6]([CH3:7])[c:8]1[cH:9][cH:10][cH:11][c:12]([O:13][c:14]2[n:15][c:16]([O:17][CH3:18])[...
C=CCON.COC(=O)c1c(Oc2nc(OC)cc(OC)n2)cccc1C(C)=O
C=CCON=C(C)c1cccc(Oc2nc(OC)cc(OC)n2)c1C(=O)OC
null
null
O
Heteroatom Alkylation and Arylation
OtherReaction
3d7a74a3d1c5abb5292963d4a3067f1fb8a89aead752dc9bb1d63522c4c0bd5c
6b0edeaa66853687109d0d530554f76edf36b01a8ec084e7ae9c709f0949a6b9
c1ccc(Oc2ncccn2)cc1
O=[C;H0;D3;+0:1](-[C;D1;H3:2])-[c:3](:[c:4]):[c:5]-[C:6](-[#8:7])=[O;D1;H0:8].[C;D1;H2:9]=[C:10]-[C:11]-[#8:12]-[NH2;D1;+0:13]>>[#8:7]-[C:6](=[O;D1;H0:8])-[c:5]:[c:3](-[C;H0;D3;+0:1](-[C;D1;H3:2])=[N;H0;D2;+0:13]-[#8:12]-[C:11]-[C:10]=[C;D1;H2:9]):[c:4]
46.3
[{"value": 46.0, "product": "C(C=C)ON=C(C)C1=C(C(=O)OC)C(=CC=C1)OC1=NC(=CC(=N1)OC)OC", "details": "PERCENTYIELD", "is_desired": false}, {"value": 46.3, "product": "C(C=C)ON=C(C)C1=C(C(=O)OC)C(=CC=C1)OC1=NC(=CC(=N1)OC)OC", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
5
HOUR
1.0 g of methyl 2-acetyl-6-[(4,6-dimethoxypyrimidin-2-yl)oxy]benzoate, 1.0 g of allyloxyamine hydrochloride and 0.9 g of potassium acetate were added to 30 ml of methanol, and were refluxed with stirring for 5 hours. The reaction mixture was then poured into a cold water, and was extracted with ethyl acetate. The organ...
10.6084/m9.figshare.5104873.v1
null
Ketone.Primary amine
null
null
null
c1ccccc1.c1cncnc1
HO-
O
null
5
C=CCON.COC(=O)c1c(Oc2nc(OC)cc(OC)n2)cccc1C(C)=O>O>C=CCON=C(C)c1cccc(Oc2nc(OC)cc(OC)n2)c1C(=O)OC
ord_dataset-02ee2261663048188cf6d85d2cc96e3f
ord-5f68bfe24502413aa07932d4095cc464
BrCc1cccc(Br)c1.CCOP(OCC)OCC>>CCOP(=O)(Cc1cccc(Br)c1)OCC
BrC=1C=C(CBr)C=CC1.P(OCC)(OCC)OCC.C(C)Br>>BrC=1C=C(CP(OCC)(OCC)=O)C=CC1
Br[CH2:6][c:7]1[cH:8][cH:9][cH:10][c:11]([Br:12])[cH:13]1.CC[O:5][P:4]([O:3][CH2:2][CH3:1])[O:14][CH2:15][CH3:16]>>[CH3:1][CH2:2][O:3][P:4](=[O:5])([CH2:6][c:7]1[cH:8][cH:9][cH:10][c:11]([Br:12])[cH:13]1)[O:14][CH2:15][CH3:16]
BrCc1cccc(Br)c1.CCOP(OCC)OCC
CCOP(=O)(Cc1cccc(Br)c1)OCC
null
null
null
Miscellaneous
OtherReaction
0cee6f48ecb82f0bf47fd5d9d42e2dd8fcb51b36e7641d6549e2ebcac266a3bf
60e0209a3e01281b77ea7e07e181a846736713b5a4a90ae8d47a0480f9ce79e5
c1ccccc1
Br-[CH2;D2;+0:1]-[c:2](:[c:3]):[c:4].C-C-[O;H0;D2;+0:5]-[P;H0;D3;+0:6](-[#8:7]-[C:8])-[#8:9]-[C:10]>>[C:8]-[#8:7]-[P;H0;D4;+0:6](=[O;H0;D1;+0:5])(-[#8:9]-[C:10])-[CH2;D2;+0:1]-[c:2](:[c:3]):[c:4]
null
[]
null
null
null
null
50 g (0.2 mol) of 3-bromobenzyl bromide and 33.2 g (0.2 mol) of triethyl phosphite were heated at 140° C. for 2 hours, during which ethyl bromide was distilled off. The product was distilled over a 30 cm Vigreux column. Conditions: See reaction.notes.procedure_details. Workup: was distilled off; The product was distill...
10.6084/m9.figshare.5104873.v1
null
Primary halide
null
null
null
c1ccccc1
HBr
null
null
null
BrCc1cccc(Br)c1.CCOP(OCC)OCC>>CCOP(=O)(Cc1cccc(Br)c1)OCC
ord_dataset-02ee2261663048188cf6d85d2cc96e3f
ord-9bbd528effc4400bb7abc75186c3da13
CC(C)OP(OC(C)C)OC(C)C.Cc1ccccc1CBr>>Cc1ccccc1CP(=O)(OC(C)C)OC(C)C
CC1=C(CBr)C=CC=C1.P(OC(C)C)(OC(C)C)OC(C)C>>CC1=C(CP(OC(C)C)(OC(C)C)=O)C=CC=C1
CC(C)[O:10][P:9]([O:11][CH:12]([CH3:13])[CH3:14])[O:15][CH:16]([CH3:17])[CH3:18].Br[CH2:8][c:7]1[c:2]([CH3:1])[cH:3][cH:4][cH:5][cH:6]1>>[CH3:1][c:2]1[cH:3][cH:4][cH:5][cH:6][c:7]1[CH2:8][P:9](=[O:10])([O:11][CH:12]([CH3:13])[CH3:14])[O:15][CH:16]([CH3:17])[CH3:18]
CC(C)OP(OC(C)C)OC(C)C.Cc1ccccc1CBr
Cc1ccccc1CP(=O)(OC(C)C)OC(C)C
null
null
null
Miscellaneous
OtherReaction
0cee6f48ecb82f0bf47fd5d9d42e2dd8fcb51b36e7641d6549e2ebcac266a3bf
60e0209a3e01281b77ea7e07e181a846736713b5a4a90ae8d47a0480f9ce79e5
c1ccccc1
Br-[CH2;D2;+0:1]-[c:2](:[c:3]):[c:4].C-C(-C)-[O;H0;D2;+0:5]-[P;H0;D3;+0:6](-[#8:7]-[C:8])-[#8:9]-[C:10]>>[C:8]-[#8:7]-[P;H0;D4;+0:6](=[O;H0;D1;+0:5])(-[#8:9]-[C:10])-[CH2;D2;+0:1]-[c:2](:[c:3]):[c:4]
null
[]
null
null
null
null
34.5 g (0.19 mol) of 2-methylbenzyl bromide and 39 g (0.19 mol) of triisopropyl phosphite were heated at 150° C. for 2 hours. During this procedure, i-propyl bromide distilled off. The product was distilled through a 30 cm Vigreux column. Conditions: See reaction.notes.procedure_details. Workup: During this procedure, ...
10.6084/m9.figshare.5104873.v1
null
Primary halide
null
null
null
c1ccccc1
HBr
null
null
null
CC(C)OP(OC(C)C)OC(C)C.Cc1ccccc1CBr>>Cc1ccccc1CP(=O)(OC(C)C)OC(C)C
ord_dataset-02ee2261663048188cf6d85d2cc96e3f
ord-72cd4b260c0043e8aa2503a92dce1f5e
COC(=O)c1cccc(C)c1.O=C1CCC(=O)N1Br>>COC(=O)c1cccc(CBr)c1
C1(=CC(=CC=C1)C(=O)OC)C.C1CC(=O)N(C1=O)Br.CC(C)(C#N)N=NC(C)(C)C#N>>BrCC=1C=C(C(=O)OC)C=CC1
[CH3:1][O:2][C:3](=[O:4])[c:5]1[cH:6][cH:7][cH:8][c:9]([CH3:10])[cH:12]1.O=C1CCC(=O)N1[Br:11]>>[CH3:1][O:2][C:3](=[O:4])[c:5]1[cH:6][cH:7][cH:8][c:9]([CH2:10][Br:11])[cH:12]1
COC(=O)c1cccc(C)c1.O=C1CCC(=O)N1Br
COC(=O)c1cccc(CBr)c1
null
null
null
Functional Group Interconversion
Wohl-Ziegler bromination benzyl primary
45c0aca0d63a96f0092e6dded9c888827eaf6379dac179e1cefc99293896300a
08f5e7e34d3f321cce3e85421b38226d6240cca0939494ae61032d4f8405cf22
c1ccccc1
O=C1-C-C-C(=O)-N-1-[Br;H0;D1;+0:1].[CH3;D1;+0:2]-[c:3](:[c:4]):[c:5]>>[Br;H0;D1;+0:1]-[CH2;D2;+0:2]-[c:3](:[c:4]):[c:5]
null
[]
null
null
null
null
Methyl m-toluate was brominated with NBS and AIBN as described in Example 21 to give methyl m-bromomethylbenzoate, and this was further reacted with triethyl phosphite as described in Example 2 without further purification. Conditions: See reaction.notes.procedure_details.
10.6084/m9.figshare.5104873.v1
null
Tertiary amide.Tertiary amide
Primary halide
C1CCNC1
null
c1ccccc1
HO-
null
null
null
COC(=O)c1cccc(C)c1.O=C1CCC(=O)N1Br>>COC(=O)c1cccc(CBr)c1
ord_dataset-02ee2261663048188cf6d85d2cc96e3f
ord-67807ba4f6aa49a6bfa5666d55bc49c7
Cc1ccccc1CC(=O)O.O=C1CCC(=O)N1Br>>CCOC(=O)Cc1ccccc1CBr
C1(=C(C=CC=C1)CC(=O)O)C.C1CC(=O)N(C1=O)Br.CC(C)(C#N)N=NC(C)(C)C#N>>BrCC1=C(C=CC=C1)CC(=O)OCC
[OH:3][C:4](=[O:5])[CH2:6][c:7]1[cH:8][cH:9][cH:10][cH:11][c:12]1[CH3:13].O=C1C[CH2:1][C:2](=O)N1[Br:14]>>[CH3:1][CH2:2][O:3][C:4](=[O:5])[CH2:6][c:7]1[cH:8][cH:9][cH:10][cH:11][c:12]1[CH2:13][Br:14]
Cc1ccccc1CC(=O)O.O=C1CCC(=O)N1Br
CCOC(=O)Cc1ccccc1CBr
null
null
null
Functional Group Interconversion
OtherReaction
1362608f413d4bb6c464b165a96e5b3a887bb1d9ae8ab376765975b118a4d0c6
5765430870c89e3aab339fb3a79e6267a09f7a7000a9527aaa43f7b6538477a8
c1ccccc1
O=C1-C-[CH2;D2;+0:1]-[C;H0;D3;+0:2](=O)-N-1-[Br;H0;D1;+0:3].[CH3;D1;+0:4]-[c:5](:[c:6]):[c:7]-[C:8]-[C:9](=[O;D1;H0:10])-[OH;D1;+0:11]>>[Br;H0;D1;+0:3]-[CH2;D2;+0:4]-[c:5](:[c:6]):[c:7]-[C:8]-[C:9](=[O;D1;H0:10])-[O;H0;D2;+0:11]-[CH2;D2;+0:2]-[CH3;D1;+0:1]
null
[]
null
null
null
null
o-Tolylacetic acid was brominated with NBS and AIBN as described in Example 21 to give ethyl o-bromomethylphenylacetate, and this was reacted with triethyl phosphite as described in Example 2. Conditions: See reaction.notes.procedure_details.
10.6084/m9.figshare.5104873.v1
null
Carboxylic acid.Tertiary amide.Tertiary amide
Primary halide.Ester
C1CCNC1
null
c1ccccc1
HO-
null
null
null
Cc1ccccc1CC(=O)O.O=C1CCC(=O)N1Br>>CCOC(=O)Cc1ccccc1CBr
ord_dataset-02ee2261663048188cf6d85d2cc96e3f
ord-1599d97756fc4192b03e40c6513b40d3
CCOP(OCC)OCC.COc1ccc(CCl)cc1>>CCOP(=O)(Cc1ccc(OC)cc1)OCC
COC1=CC=C(CCl)C=C1.P(OCC)(OCC)OCC>>COC1=CC=C(CP(OCC)(OCC)=O)C=C1
CC[O:5][P:4]([O:3][CH2:2][CH3:1])[O:15][CH2:16][CH3:17].Cl[CH2:6][c:7]1[cH:8][cH:9][c:10]([O:11][CH3:12])[cH:13][cH:14]1>>[CH3:1][CH2:2][O:3][P:4](=[O:5])([CH2:6][c:7]1[cH:8][cH:9][c:10]([O:11][CH3:12])[cH:13][cH:14]1)[O:15][CH2:16][CH3:17]
CCOP(OCC)OCC.COc1ccc(CCl)cc1
CCOP(=O)(Cc1ccc(OC)cc1)OCC
null
null
null
Miscellaneous
OtherReaction
0cee6f48ecb82f0bf47fd5d9d42e2dd8fcb51b36e7641d6549e2ebcac266a3bf
60e0209a3e01281b77ea7e07e181a846736713b5a4a90ae8d47a0480f9ce79e5
c1ccccc1
C-C-[O;H0;D2;+0:1]-[P;H0;D3;+0:2](-[#8:3]-[C:4])-[#8:5]-[C:6].Cl-[CH2;D2;+0:7]-[c:8](:[c:9]):[c:10]>>[C:4]-[#8:3]-[P;H0;D4;+0:2](=[O;H0;D1;+0:1])(-[#8:5]-[C:6])-[CH2;D2;+0:7]-[c:8](:[c:9]):[c:10]
null
[]
null
null
null
null
p-Methoxybenzyl chloride was reacted with triethyl phosphite as described in Example 2. Conditions: See reaction.notes.procedure_details.
10.6084/m9.figshare.5104873.v1
null
Primary halide
null
null
null
c1ccccc1
HCl
null
null
null
CCOP(OCC)OCC.COc1ccc(CCl)cc1>>CCOP(=O)(Cc1ccc(OC)cc1)OCC
ord_dataset-02ee2261663048188cf6d85d2cc96e3f
ord-d600937ba404454f851cb18c5c96b0b1
BrBr.CCOP(=O)(Cc1ccccc1C)OCC>>CCOP(=O)(Cc1ccc(Br)cc1C)OCC
CC1=C(CP(OCC)(OCC)=O)C=CC=C1.BrBr>>CC1=C(CP(OCC)(OCC)=O)C=CC(=C1)Br
Br[Br:11].[CH3:1][CH2:2][O:3][P:4](=[O:5])([CH2:6][c:7]1[cH:8][cH:9][cH:10][cH:12][c:13]1[CH3:14])[O:15][CH2:16][CH3:17]>>[CH3:1][CH2:2][O:3][P:4](=[O:5])([CH2:6][c:7]1[cH:8][cH:9][c:10]([Br:11])[cH:12][c:13]1[CH3:14])[O:15][CH2:16][CH3:17]
BrBr.CCOP(=O)(Cc1ccccc1C)OCC
CCOP(=O)(Cc1ccc(Br)cc1C)OCC
null
null
P(=O)(OC)(OC)OC.O
Functional Group Interconversion
Bromination
f6effe61353895b318215d8bd9b6bb1105cafbf7be8c217d748df587260b32c3
3c4065ab4a8681675e06a527dcad54d701c7bfdcac9f73f87773b05034108934
c1ccccc1
Br-[Br;H0;D1;+0:1].[c:2]:[c:3]:[cH;D2;+0:4]:[c:5]:[c:6]>>[Br;H0;D1;+0:1]-[c;H0;D3;+0:4](:[c:3]:[c:2]):[c:5]:[c:6]
null
[]
null
null
null
null
10 g (42 mmol) of diethyl 2-methylbenzylphosphonate were dissolved in 60 ml of trimethyl phosphate and the solution was introduced into a flask protected from light and moisture. 16 g (0.05 mol) of Br2 were added dropwise, while stirring. The mixture was stirred at 90° C. for 15 hours and, after cooling, was diluted wi...
10.6084/m9.figshare.5104873.v1
null
null
Aromatic halide
c1ccccc1
c1ccccc1
c1ccccc1
HBr
P(=O)(OC)(OC)OC.O
null
null
BrBr.CCOP(=O)(Cc1ccccc1C)OCC>P(=O)(OC)(OC)OC.O>CCOP(=O)(Cc1ccc(Br)cc1C)OCC
ord_dataset-02ee2261663048188cf6d85d2cc96e3f
ord-3b1908a01a5143ef967011e4244289b7
CCOP(=O)(Cc1ccccc1C)OCC.[O]=[Mn](=[O])(=[O])[O-]>>CCOP(=O)(Cc1ccccc1C(=O)O)OCC
OS(=O)(=O)O.CC1=C(CP(OCC)(OCC)=O)C=CC=C1.[O-][Mn](=O)(=O)=O.[K+].C(=O)([O-])[O-].[Na+].[Na+]>>C(=O)(O)C1=C(CP(OCC)(OCC)=O)C=CC=C1
[CH3:1][CH2:2][O:3][P:4](=[O:5])([CH2:6][c:7]1[cH:8][cH:9][cH:10][cH:11][c:12]1[CH3:13])[O:16][CH2:17][CH3:18].[O]=[Mn](=[O])(=[O])[O-:15]>>[CH3:1][CH2:2][O:3][P:4](=[O:5])([CH2:6][c:7]1[cH:8][cH:9][cH:10][cH:11][c:12]1[C:13](=[O:14])[OH:15])[O:16][CH2:17][CH3:18]
CCOP(=O)(Cc1ccccc1C)OCC.[O]=[Mn](=[O])(=[O])[O-]
CCOP(=O)(Cc1ccccc1C(=O)O)OCC
null
null
O
Acylation
OtherReaction
7769a4cd09a67e270ac2d1d32df6b7a59b468ff590f9c59723b72ba3c8deb342
903e48d04e4504a4fe6977f5e5582144adff237d0488a4542a1907161cf0134c
c1ccccc1
[CH3;D1;+0:1]-[c:2](:[c:3]):[c:4].[O-;H0;D1:5]-[Mn](=[O])(=[O])=[O]>>[O;D1;H0:6]=[C;H0;D3;+0:1](-[OH;D1;+0:5])-[c:2](:[c:3]):[c:4]
null
[]
null
null
null
null
4 g of diethyl 2-methylbenzylphosphonate were added to a solution of 12 g of KMnO4 and 4 g of Na2CO3 in 300 ml of water and the mixture was boiled under reflux for 24 hours. It was acidified with 15 ml of concentrated H2SO4 and extracted five times with 300 ml of ether each time. The organic phase was dried over MgSO4,...
10.6084/m9.figshare.5104873.v1
null
null
Carboxylic acid
null
null
c1ccccc1
HO-
O
null
null
CCOP(=O)(Cc1ccccc1C)OCC.[O]=[Mn](=[O])(=[O])[O-]>O>CCOP(=O)(Cc1ccccc1C(=O)O)OCC
ord_dataset-02ee2261663048188cf6d85d2cc96e3f
ord-88cb2fb8067f482b8c767b3656f1557f
CC12CCC(C(=O)OC1=O)C2(C)C.NCCCCN1CCN(c2ncccn2)CC1>>CC12CCC(C(=O)N(CCCCN3CCN(c4ncccn4)CC3)C1=O)C2(C)C
NCCCCN1CCN(CC1)C1=NC=CC=N1.CC1(C2CCC1(C(=O)OC2=O)C)C>>N1=C(N=CC=C1)N1CCN(CC1)CCCCN1C(C2(CCC(C1=O)C2(C)C)C)=O
O1[C:6](=[O:7])[CH:5]2[CH2:4][CH2:3][C:2]([CH3:1])([C:25]1=[O:26])[C:27]2([CH3:28])[CH3:29].[NH2:8][CH2:9][CH2:10][CH2:11][CH2:12][N:13]1[CH2:14][CH2:15][N:16]([c:17]2[n:18][cH:19][cH:20][cH:21][n:22]2)[CH2:23][CH2:24]1>>[CH3:1][C:2]12[CH2:3][CH2:4][CH:5]([C:6](=[O:7])[N:8]([CH2:9][CH2:10][CH2:11][CH2:12][N:13]3[CH2:14...
CC12CCC(C(=O)OC1=O)C2(C)C.NCCCCN1CCN(c2ncccn2)CC1
CC12CCC(C(=O)N(CCCCN3CCN(c4ncccn4)CC3)C1=O)C2(C)C
null
null
null
Acylation
OtherReaction
b2dab778bbababe3728f59be0984a9052d84b3f07c1a6627953660a5bd6e03d0
2a4a20e639c386292668b0b265a8e1b50d707d5f0576437dc5ade3e7fd444d29
O=C1C2CCC(C2)C(=O)N1CCCCN1CCN(c2ncccn2)CC1
[C;D1;H3:1]-[C:2]12-[C:3]-[C:4](-[C:5]-[C:6]-1)-[C;H0;D3;+0:7](=[O;D1;H0:8])-O-[C;H0;D3;+0:9]-2=[O;D1;H0:10].[C:11]-[C:12]-[NH2;D1;+0:13]>>[C:11]-[C:12]-[N;H0;D3;+0:13]1-[C;H0;D3;+0:9](=[O;D1;H0:10])-[C:2]2(-[C;D1;H3:1])-[C:3]-[C:4](-[C:5]-[C:6]-2)-[C;H0;D3;+0:7]-1=[O;D1;H0:8]
17
[{"value": 17.0, "product": "N1=C(N=CC=C1)N1CCN(CC1)CCCCN1C(C2(CCC(C1=O)C2(C)C)C)=O", "details": "PERCENTYIELD", "is_desired": false}]
null
null
null
null
The title compound was prepared from 2.47 g (10.4 mmol) of 1-(4-aminobutyl)-4-(2-pyrimidinyl)piperazine and 1.89 g (10.3 mmol) of dl-camphoric anhydride, substantially according to the procedure of Example 1. This afforded 0.7 g of product, mp 94°-97° C. (17% yield). Conditions: See reaction.notes.procedure_details.
10.6084/m9.figshare.5104873.v1
null
Anhydride.Primary amine
Substituted dicarboximide
C1CC2COCC1C2
C1CC2C[NH]CC1C2
C1CC2C[NH]CC1C2.C1C[NH]CC[NH]1.c1cncnc1
HO-
null
null
null
CC12CCC(C(=O)OC1=O)C2(C)C.NCCCCN1CCN(c2ncccn2)CC1>>CC12CCC(C(=O)N(CCCCN3CCN(c4ncccn4)CC3)C1=O)C2(C)C
ord_dataset-02ee2261663048188cf6d85d2cc96e3f
ord-ff612c52e1a04b8e97b7f6d47d01eb91
NCCCCN1CCN(c2ncccn2)CC1.O=C1OC(=O)C2CCC1C2>>O=C1C2CCC(C2)C(=O)N1CCCCN1CCN(c2ncccn2)CC1
NCCCCN1CCN(CC1)C1=NC=CC=N1.C12C(OC(C(CC1)C2)=O)=O>>N1=C(N=CC=C1)N1CCN(CC1)CCCCN1C(C2CCC(C1=O)C2)=O
[NH2:10][CH2:11][CH2:12][CH2:13][CH2:14][N:15]1[CH2:16][CH2:17][N:18]([c:19]2[n:20][cH:21][cH:22][cH:23][n:24]2)[CH2:25][CH2:26]1.O1[C:2](=[O:1])[CH:3]2[CH2:4][CH2:5][CH:6]([CH2:7]2)[C:8]1=[O:9]>>[O:1]=[C:2]1[CH:3]2[CH2:4][CH2:5][CH:6]([CH2:7]2)[C:8](=[O:9])[N:10]1[CH2:11][CH2:12][CH2:13][CH2:14][N:15]1[CH2:16][CH2:17]...
NCCCCN1CCN(c2ncccn2)CC1.O=C1OC(=O)C2CCC1C2
O=C1C2CCC(C2)C(=O)N1CCCCN1CCN(c2ncccn2)CC1
null
null
null
Acylation
OtherReaction
b2dab778bbababe3728f59be0984a9052d84b3f07c1a6627953660a5bd6e03d0
2a4a20e639c386292668b0b265a8e1b50d707d5f0576437dc5ade3e7fd444d29
O=C1C2CCC(C2)C(=O)N1CCCCN1CCN(c2ncccn2)CC1
[C:1]-[C:2]-[NH2;D1;+0:3].[O;D1;H0:4]=[C;H0;D3;+0:5]1-O-[C;H0;D3;+0:6](=[O;D1;H0:7])-[C:8]2-[C:9]-[C:10]-[C:11]-1-[C:12]-2>>[C:1]-[C:2]-[N;H0;D3;+0:3]1-[C;H0;D3;+0:5](=[O;D1;H0:4])-[C:11]2-[C:10]-[C:9]-[C:8](-[C:12]-2)-[C;H0;D3;+0:6]-1=[O;D1;H0:7]
34
[{"value": 34.0, "product": "N1=C(N=CC=C1)N1CCN(CC1)CCCCN1C(C2CCC(C1=O)C2)=O", "details": "PERCENTYIELD", "is_desired": false}]
null
null
null
null
The title compound was prepared from 1.92 g (8.2 mmol) of 1-(4-aminobutyl)-4-(2-pyrimidinyl)piperazine and 1.14 g (8.14 mmol) of 3-oxabicyclo[3.2.1]octan-2,4-dione, substantially following the procedure of Example 1. Yield: 1.0 g (34% yield). Conditions: See reaction.notes.procedure_details.
10.6084/m9.figshare.5104873.v1
null
Anhydride.Primary amine
Substituted dicarboximide
C1CC2COCC1C2
C1CC2C[NH]CC1C2
C1CC2C[NH]CC1C2.C1C[NH]CC[NH]1.c1cncnc1
HO-
null
null
null
NCCCCN1CCN(c2ncccn2)CC1.O=C1OC(=O)C2CCC1C2>>O=C1C2CCC(C2)C(=O)N1CCCCN1CCN(c2ncccn2)CC1
ord_dataset-02ee2261663048188cf6d85d2cc96e3f
ord-443f179a2fda400bab688522515184dd
NCCCCN1CCN(c2ncccn2)CC1.O=C1OC(=O)C2CCCC1C2>>O=C1C2CCCC(C2)C(=O)N1CCCCN1CCN(c2ncccn2)CC1
NCCCCN1CCN(CC1)C1=NC=CC=N1.C12C(OC(C(CCC1)C2)=O)=O>>N1=C(N=CC=C1)N1CCN(CC1)CCCCN1C(C2CCCC(C1=O)C2)=O
[NH2:11][CH2:12][CH2:13][CH2:14][CH2:15][N:16]1[CH2:17][CH2:18][N:19]([c:20]2[n:21][cH:22][cH:23][cH:24][n:25]2)[CH2:26][CH2:27]1.O1[C:2](=[O:1])[CH:3]2[CH2:4][CH2:5][CH2:6][CH:7]([CH2:8]2)[C:9]1=[O:10]>>[O:1]=[C:2]1[CH:3]2[CH2:4][CH2:5][CH2:6][CH:7]([CH2:8]2)[C:9](=[O:10])[N:11]1[CH2:12][CH2:13][CH2:14][CH2:15][N:16]1...
NCCCCN1CCN(c2ncccn2)CC1.O=C1OC(=O)C2CCCC1C2
O=C1C2CCCC(C2)C(=O)N1CCCCN1CCN(c2ncccn2)CC1
null
null
null
Acylation
OtherReaction
6db7e0bce5132044bb5be71dd65c16d70e74c9d48d6d82239559f39783148260
2a4a20e639c386292668b0b265a8e1b50d707d5f0576437dc5ade3e7fd444d29
O=C1C2CCCC(C2)C(=O)N1CCCCN1CCN(c2ncccn2)CC1
[C:1]-[C:2]-[NH2;D1;+0:3].[C:4]-[C:5]1-[C:6]-[C:7](-[C:8])-[C;H0;D3;+0:9](=[O;D1;H0:10])-O-[C;H0;D3;+0:11]-1=[O;D1;H0:12]>>[C:1]-[C:2]-[N;H0;D3;+0:3]1-[C;H0;D3;+0:11](=[O;D1;H0:12])-[C:5](-[C:4])-[C:6]-[C:7](-[C:8])-[C;H0;D3;+0:9]-1=[O;D1;H0:10]
47
[{"value": 47.0, "product": "N1=C(N=CC=C1)N1CCN(CC1)CCCCN1C(C2CCCC(C1=O)C2)=O", "details": "PERCENTYIELD", "is_desired": false}, {"value": 46.5, "product": "N1=C(N=CC=C1)N1CCN(CC1)CCCCN1C(C2CCCC(C1=O)C2)=O", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
null
null
Following substantially the procedure of Example 1, 2.78 g (11.8 mmol) of 1-(4-aminobutyl)-4-(2-pyrimidinyl) piperazine was reacted with 1.88 g (12.2 mmol) of 3-oxabicyclo[3.3.1]nonan-2,4-dione. The product was chromatographed on silica gel, eluting with dichloromethane/methanol (90:10), to give 2.04 g (47% yield) of t...
10.6084/m9.figshare.5104873.v1
null
Anhydride.Primary amine
Substituted dicarboximide
C1CC2COCC(C1)C2
C1CC2C[NH]CC(C1)C2
C1CC2C[NH]CC(C1)C2.C1C[NH]CC[NH]1.c1cncnc1
HO-
null
null
null
NCCCCN1CCN(c2ncccn2)CC1.O=C1OC(=O)C2CCCC1C2>>O=C1C2CCCC(C2)C(=O)N1CCCCN1CCN(c2ncccn2)CC1
ord_dataset-02ee2261663048188cf6d85d2cc96e3f
ord-1790a349503649588a9f0cb35a4defe4
CC1(C)C2CCC1C(=O)OC2=O.NCCCCN1CCN(c2ncccn2)CC1>>CC1(C)C2CCC1C(=O)N(CCCCN1CCN(c3ncccn3)CC1)C2=O
NCCCCN1CCN(CC1)C1=NC=CC=N1.CC1(C2C(OC(C1CC2)=O)=O)C>>N1=C(N=CC=C1)N1CCN(CC1)CCCCN1C(C2CCC(C1=O)C2(C)C)=O
O1[C:8](=[O:9])[CH:7]2[C:2]([CH3:1])([CH3:3])[CH:4]([CH2:5][CH2:6]2)[C:27]1=[O:28].[NH2:10][CH2:11][CH2:12][CH2:13][CH2:14][N:15]1[CH2:16][CH2:17][N:18]([c:19]2[n:20][cH:21][cH:22][cH:23][n:24]2)[CH2:25][CH2:26]1>>[CH3:1][C:2]1([CH3:3])[CH:4]2[CH2:5][CH2:6][CH:7]1[C:8](=[O:9])[N:10]([CH2:11][CH2:12][CH2:13][CH2:14][N:1...
CC1(C)C2CCC1C(=O)OC2=O.NCCCCN1CCN(c2ncccn2)CC1
CC1(C)C2CCC1C(=O)N(CCCCN1CCN(c3ncccn3)CC1)C2=O
null
null
null
Acylation
OtherReaction
b2dab778bbababe3728f59be0984a9052d84b3f07c1a6627953660a5bd6e03d0
2a4a20e639c386292668b0b265a8e1b50d707d5f0576437dc5ade3e7fd444d29
O=C1C2CCC(C2)C(=O)N1CCCCN1CCN(c2ncccn2)CC1
[C:1]-[C:2]-[NH2;D1;+0:3].[O;D1;H0:4]=[C;H0;D3;+0:5]1-O-[C;H0;D3;+0:6](=[O;D1;H0:7])-[C:8]2-[C:9]-[C:10]-1-[C:11]-[C:12]-2>>[C:1]-[C:2]-[N;H0;D3;+0:3]1-[C;H0;D3;+0:5](=[O;D1;H0:4])-[C:10]2-[C:9]-[C:8](-[C:12]-[C:11]-2)-[C;H0;D3;+0:6]-1=[O;D1;H0:7]
32
[{"value": 32.0, "product": "N1=C(N=CC=C1)N1CCN(CC1)CCCCN1C(C2CCC(C1=O)C2(C)C)=O", "details": "PERCENTYIELD", "is_desired": false}, {"value": 30.3, "product": "N1=C(N=CC=C1)N1CCN(CC1)CCCCN1C(C2CCC(C1=O)C2(C)C)=O", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
null
null
Following substantially the procedure of Example 1, 0.54 g (2.34 mmol) of 1-(4-aminobutyl)-4-(2-pyrimidinyl) piperazine was reacted with 0.36 g (2.14 mmol) of 8,8-dimethyl-3-oxabicyclo[3.2.1]octan-2,4-dione. The product was chromatographed on silica gel, eluting with dichloromethane/methanol (96:4), to give 0.25 g (32%...
10.6084/m9.figshare.5104873.v1
null
Anhydride.Primary amine
Substituted dicarboximide
C1CC2COCC1C2
C1CC2C[NH]CC1C2
C1CC2C[NH]CC1C2.C1C[NH]CC[NH]1.c1cncnc1
HO-
null
null
null
CC1(C)C2CCC1C(=O)OC2=O.NCCCCN1CCN(c2ncccn2)CC1>>CC1(C)C2CCC1C(=O)N(CCCCN1CCN(c3ncccn3)CC1)C2=O
ord_dataset-02ee2261663048188cf6d85d2cc96e3f
ord-e56e486a103f4058a11eaf6d3e707e63
CC12CCC(C)(C1)C(=O)OC2=O.NCCCCN1CCN(c2ncccn2)CC1>>CC12CCC(C)(C1)C(=O)N(CCCCN1CCN(c3ncccn3)CC1)C2=O
NCCCCN1CCN(CC1)C1=NC=CC=N1.CC12C(OC(C(CC1)(C2)C)=O)=O>>N1=C(N=CC=C1)N1CCN(CC1)CCCCN1C(C2(CCC(C1=O)(C2)C)C)=O
O1[C:8](=[O:9])[C:5]2([CH3:6])[CH2:4][CH2:3][C:2]([CH3:1])([CH2:7]2)[C:27]1=[O:28].[NH2:10][CH2:11][CH2:12][CH2:13][CH2:14][N:15]1[CH2:16][CH2:17][N:18]([c:19]2[n:20][cH:21][cH:22][cH:23][n:24]2)[CH2:25][CH2:26]1>>[CH3:1][C:2]12[CH2:3][CH2:4][C:5]([CH3:6])([CH2:7]1)[C:8](=[O:9])[N:10]([CH2:11][CH2:12][CH2:13][CH2:14][N...
CC12CCC(C)(C1)C(=O)OC2=O.NCCCCN1CCN(c2ncccn2)CC1
CC12CCC(C)(C1)C(=O)N(CCCCN1CCN(c3ncccn3)CC1)C2=O
null
null
null
Acylation
OtherReaction
b2dab778bbababe3728f59be0984a9052d84b3f07c1a6627953660a5bd6e03d0
2a4a20e639c386292668b0b265a8e1b50d707d5f0576437dc5ade3e7fd444d29
O=C1C2CCC(C2)C(=O)N1CCCCN1CCN(c2ncccn2)CC1
[C;D1;H3:1]-[C:2]12-[C:3]-[C:4]-[C:5](-[C;D1;H3:6])(-[C:7]-1)-[C;H0;D3;+0:8](=[O;D1;H0:9])-O-[C;H0;D3;+0:10]-2=[O;D1;H0:11].[C:12]-[C:13]-[NH2;D1;+0:14]>>[C:12]-[C:13]-[N;H0;D3;+0:14]1-[C;H0;D3;+0:10](=[O;D1;H0:11])-[C:2]2(-[C;D1;H3:1])-[C:3]-[C:4]-[C:5](-[C;D1;H3:6])(-[C:7]-2)-[C;H0;D3;+0:8]-1=[O;D1;H0:9]
21
[{"value": 21.0, "product": "N1=C(N=CC=C1)N1CCN(CC1)CCCCN1C(C2(CCC(C1=O)(C2)C)C)=O", "details": "PERCENTYIELD", "is_desired": false}, {"value": 20.4, "product": "N1=C(N=CC=C1)N1CCN(CC1)CCCCN1C(C2(CCC(C1=O)(C2)C)C)=O", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
null
null
Following substantially the procedure of Example 1, 4.2 g (17.8 mmol) of 1-(4-aminobutyl)-4-(2-pyrimidinyl) piperazine was reacted with 2.99 g (17.8 mmol) of 1,5-dimethyl-3-oxabicyclo[3.2.1]octan-2,4-dione. The product was chromatographed on silica gel, eluting with dichloromethane/methanol (96:4), to give 1.4 g (21% y...
10.6084/m9.figshare.5104873.v1
null
Anhydride.Primary amine
Substituted dicarboximide
C1CC2COCC1C2
C1CC2C[NH]CC1C2
C1CC2C[NH]CC1C2.C1C[NH]CC[NH]1.c1cncnc1
HO-
null
null
null
CC12CCC(C)(C1)C(=O)OC2=O.NCCCCN1CCN(c2ncccn2)CC1>>CC12CCC(C)(C1)C(=O)N(CCCCN1CCN(c3ncccn3)CC1)C2=O