dataset_id
large_stringclasses
414 values
reaction_id
large_stringlengths
36
36
reaction_smiles
large_stringlengths
4
873
rxn_insight_reaction
large_stringlengths
19
1.07k
mapped_reaction_smiles
large_stringlengths
14
3.37k
reactant_smiles
large_stringlengths
1
581
product_smiles
large_stringlengths
1
433
reagent_smiles
large_stringclasses
634 values
catalyst_smiles
large_stringlengths
1
683
solvent_smiles
large_stringlengths
1
245
rxn_insight_class
large_stringclasses
11 values
rxn_insight_name
large_stringclasses
346 values
rxn_insight_tag
large_stringlengths
64
64
rxn_insight_tag2
large_stringlengths
64
64
rxn_insight_scaffold
large_stringlengths
5
288
rxn_insight_template
large_stringlengths
24
2.64k
yield_percent
float64
-0.8
90,205,160,000B
yield_measurements
large_stringlengths
2
864
temperature_value
float64
-230
30.1k
temperature_units
large_stringclasses
3 values
reaction_time_value
float64
0
4k
time_units
large_stringclasses
4 values
procedure_details
large_stringlengths
1
23.6k
reference
large_stringclasses
96 values
doi
large_stringclasses
19 values
functional_groups_reactants
large_stringlengths
3
716
functional_groups_products
large_stringlengths
3
539
participating_rings_reactants
large_stringlengths
5
293
participating_rings_products
large_stringlengths
5
271
all_rings_products
large_stringlengths
5
271
byproduct_smiles
large_stringclasses
176 values
agent_smiles
large_stringlengths
1
712
temperature_c
float64
-230
30.1k
reaction_time_hours
float64
0
2.16k
reaction_smiles_with_agents
large_stringlengths
4
882
ord_dataset-c2ad1656a3ca4d08888ffb6e3f3a2742
ord-e87e8b45cb4e463291e44ca41c4cfad3
Cc1ccc(F)cc1Cl>>Cc1cc([N+](=O)[O-])c(F)cc1Cl
ClC1=C(C=CC(=C1)F)C.[N+](=O)([O-])[O-].[K+]>>ClC1=C(C=C(C(=C1)F)[N+](=O)[O-])C
[CH3:1][c:2]1[cH:3][cH:4][c:8]([F:9])[cH:10][c:11]1[Cl:12]>>[CH3:1][c:2]1[cH:3][c:4]([N+:5](=[O:6])[O-:7])[c:8]([F:9])[cH:10][c:11]1[Cl:12]
Cc1ccc(F)cc1Cl
Cc1cc([N+](=O)[O-])c(F)cc1Cl
null
null
OS(=O)(=O)O
Functional Group Addition
OtherReaction
6862453966ade01f48ad6e78fdee5c31f5f3bef2a50d1592f73a35f3caf6154f
22f3183026a2d99c91ec0c53f0059a15c8421016bd62c8ab45281362b96dc686
c1ccccc1
[F;D1;H0:1]-[c:2](:[c:3]):[cH;D2;+0:4]:[c:5]:[c:6]>>[F;D1;H0:1]-[c:2](:[c:3]):[c;H0;D3;+0:4](-[#7;+:7](-[O;-;D1;H0:8])=[O;D1;H0:9]):[c:5]:[c:6]
795.3
[{"value": 80.0, "product": "ClC1=C(C=C(C(=C1)F)[N+](=O)[O-])C", "details": "PERCENTYIELD", "is_desired": false}, {"value": 795.3, "product": "ClC1=C(C=C(C(=C1)F)[N+](=O)[O-])C", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
28
CELSIUS
8
HOUR
To a stirred solution of 2-chloro-4-fluorotoluene (2.000 g, 1.383 mmol, Aldrich, used as received) in conc. H2SO4 (15.0 mL) at 0° C., KNO3 (1.400 g, 1.385 mmol) was added in one lot. The resulting pale yellow solution was allowed to warm to 28° C. and stirred overnight at 28° C. It was then poured into ice (100 g) and ...
10.6084/m9.figshare.5104873.v1
null
null
Nitro group
c1ccccc1
c1ccccc1
c1ccccc1
Other
OS(=O)(=O)O
28
8
Cc1ccc(F)cc1Cl>OS(=O)(=O)O>Cc1cc([N+](=O)[O-])c(F)cc1Cl
ord_dataset-c2ad1656a3ca4d08888ffb6e3f3a2742
ord-ad3a05284c3544a09486d2295e29d42a
Cc1cc([N+](=O)[O-])c(F)cc1Cl.NCC(=O)[O-]>>Cc1cc([N+](=O)[O-])c(NCC(=O)[O-])cc1Cl
ClC1=C(C=C(C(=C1)F)[N+](=O)[O-])C.NCC(=O)[O-].[Na+]>>[Na+].ClC=1C(=CC(=C(C1)NCC(=O)[O-])[N+](=O)[O-])C
F[c:8]1[c:4]([N+:5](=[O:6])[O-:7])[cH:3][c:2]([CH3:1])[c:15]([Cl:16])[cH:14]1.[NH2:9][CH2:10][C:11](=[O:12])[O-:13]>>[CH3:1][c:2]1[cH:3][c:4]([N+:5](=[O:6])[O-:7])[c:8]([NH:9][CH2:10][C:11](=[O:12])[O-:13])[cH:14][c:15]1[Cl:16]
Cc1cc([N+](=O)[O-])c(F)cc1Cl.NCC(=O)[O-]
Cc1cc([N+](=O)[O-])c(NCC(=O)[O-])cc1Cl
null
null
O.CN(C)C=O
Heteroatom Alkylation and Arylation
Buchwald-Hartwig/Ullmann-Goldberg/N-arylation primary amine
da9dae6a655c4bd18887b692f91621e77027436294d6e1fc7be7295afb364796
71a04ae650defc5edd86a92f43c304e981a05f07ff76248da8d4155f3905a29d
c1ccccc1
F-[c;H0;D3;+0:1](:[c:2]:[c:3]):[c:4](-[#7;+:5]):[c:6].[NH2;D1;+0:7]-[C:8]-[C:9](-[O;-;D1;H0:10])=[O;D1;H0:11]>>[#7;+:5]-[c:4](:[c:6]):[c;H0;D3;+0:1](-[NH;D2;+0:7]-[C:8]-[C:9](-[O;-;D1;H0:10])=[O;D1;H0:11]):[c:2]:[c:3]
null
[]
70
CELSIUS
8
HOUR
To a stirred solution of 2-chloro-4-fluoro-5-nitrotoluene (2.080 g, 10.97 mmol, as prepared above) in DMF (11.0 mL) at 70° C., was added dropwise, a solution of sodium glycinate (1.065 g, 10.97 mmol, Aldrich, used as received) in water (11.0 mL). The resulting suspension was stirred overnight at 70° C., cooled to room ...
10.6084/m9.figshare.5104873.v1
null
Aromatic halide.Primary amine
Secondary amine
c1ccccc1
c1ccccc1
c1ccccc1
HF
O.CN(C)C=O
70
8
Cc1cc([N+](=O)[O-])c(F)cc1Cl.NCC(=O)[O-]>O.CN(C)C=O>Cc1cc([N+](=O)[O-])c(NCC(=O)[O-])cc1Cl
ord_dataset-c2ad1656a3ca4d08888ffb6e3f3a2742
ord-320d60f9a6d0463695a7580e7e302485
Cc1cc([N+](=O)[O-])c(NCC(=O)O)cc1Cl>>Cc1cc2c(cc1Cl)NCC(=O)N2
ClC=1C(=CC(=C(C1)NCC(=O)O)[N+](=O)[O-])C.O.O.[Sn](Cl)Cl>>ClC=1C=C2NCC(NC2=CC1C)=O
O=[N+:13]([O-])[c:4]1[cH:3][c:2]([CH3:1])[c:7]([Cl:8])[cH:6][c:5]1[NH:9][CH2:10][C:11](O)=[O:12]>>[CH3:1][c:2]1[cH:3][c:4]2[c:5]([cH:6][c:7]1[Cl:8])[NH:9][CH2:10][C:11](=[O:12])[NH:13]2
Cc1cc([N+](=O)[O-])c(NCC(=O)O)cc1Cl
Cc1cc2c(cc1Cl)NCC(=O)N2
null
null
C(C)O
Functional Group Interconversion
OtherReaction
248a0ced66d35d5637fd333df7859a163df67de7a5eafc38f3d14fb913b635e3
98c112fcc8dd821704dc378798368c2081a2acc574356674c70af3e59954ee0d
O=C1CNc2ccccc2N1
O-[C;H0;D3;+0:1](=[O;D1;H0:2])-[C:3]-[#7:4]-[c:5]:[c:6](-[N+;H0;D3:7](=O)-[O-]):[c:8]>>[O;D1;H0:2]=[C;H0;D3;+0:1]1-[C:3]-[#7:4]-[c:5]:[c:6](:[c:8])-[NH;D2;+0:7]-1
31.2
[{"value": 31.0, "product": "ClC=1C=C2NCC(NC2=CC1C)=O", "details": "PERCENTYIELD", "is_desired": false}, {"value": 31.2, "product": "ClC=1C=C2NCC(NC2=CC1C)=O", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
null
null
A solution of N-(5'-chloro-4'-methyl-2'-nitrophenyl)glycine (1.000 g, 4.088 mmol, as prepared above) and tin (II) chloride dihydrate (2.767 g, 12.26 mmol, Aldrich, used as received) in ethanol (20.0 mL) was refluxed for 30 min. It was then cooled to room temperature and the precipitated solid was filtered, washed with ...
10.6084/m9.figshare.5104873.v1
null
Carboxylic acid.Nitro group
Secondary amide
null
c1ccc2c(c1)NCCN2
c1ccc2c(c1)NCCN2
Other
C(C)O
null
null
Cc1cc([N+](=O)[O-])c(NCC(=O)O)cc1Cl>C(C)O>Cc1cc2c(cc1Cl)NCC(=O)N2
ord_dataset-c2ad1656a3ca4d08888ffb6e3f3a2742
ord-542fdfd736c04d64ac3410cac1f60bbe
Cc1cc(F)ccc1Cl>>Cc1cc(F)c([N+](=O)[O-])cc1Cl
ClC1=C(C=C(C=C1)F)C.[N+](=O)([O-])[O-].[K+]>>ClC1=C(C=C(C(=C1)[N+](=O)[O-])F)C
[CH3:1][c:2]1[cH:3][c:4]([F:5])[cH:6][cH:10][c:11]1[Cl:12]>>[CH3:1][c:2]1[cH:3][c:4]([F:5])[c:6]([N+:7](=[O:8])[O-:9])[cH:10][c:11]1[Cl:12]
Cc1cc(F)ccc1Cl
Cc1cc(F)c([N+](=O)[O-])cc1Cl
null
null
OS(=O)(=O)O
Functional Group Addition
OtherReaction
6862453966ade01f48ad6e78fdee5c31f5f3bef2a50d1592f73a35f3caf6154f
22f3183026a2d99c91ec0c53f0059a15c8421016bd62c8ab45281362b96dc686
c1ccccc1
[F;D1;H0:1]-[c:2](:[c:3]):[cH;D2;+0:4]:[c:5]:[c:6]>>[F;D1;H0:1]-[c:2](:[c:3]):[c;H0;D3;+0:4](-[#7;+:7](-[O;-;D1;H0:8])=[O;D1;H0:9]):[c:5]:[c:6]
94
[{"value": 94.0, "product": "ClC1=C(C=C(C(=C1)[N+](=O)[O-])F)C", "details": "PERCENTYIELD", "is_desired": false}, {"value": 93.9, "product": "ClC1=C(C=C(C(=C1)[N+](=O)[O-])F)C", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
28
CELSIUS
8
HOUR
To a stirred solution of 2-chloro-5-fluorotoluene (0.500 g, 3.46 mmol, Lancaster, used as received) in conc. H2SO4 (5.0 mL) at 0° C., KNO3 (0.350 g, 3.46 mmol) was added in one lot. The resulting pale yellow solution was allowed to warm to 28° C. and stirred overnight at 28° C. It was then poured into ice (50 g) and ex...
10.6084/m9.figshare.5104873.v1
null
null
Nitro group
c1ccccc1
c1ccccc1
c1ccccc1
Other
OS(=O)(=O)O
28
8
Cc1cc(F)ccc1Cl>OS(=O)(=O)O>Cc1cc(F)c([N+](=O)[O-])cc1Cl
ord_dataset-c2ad1656a3ca4d08888ffb6e3f3a2742
ord-6f15bb650df74b71ae3950aa217798c8
Cc1cc(F)c([N+](=O)[O-])cc1Cl.NCC(=O)[O-]>>Cc1cc(NCC(=O)[O-])c([N+](=O)[O-])cc1Cl
ClC1=C(C=C(C(=C1)[N+](=O)[O-])F)C.NCC(=O)[O-].[Na+]>>[Na+].ClC1=CC(=C(C=C1C)NCC(=O)[O-])[N+](=O)[O-]
F[c:4]1[cH:3][c:2]([CH3:1])[c:15]([Cl:16])[cH:14][c:10]1[N+:11](=[O:12])[O-:13].[NH2:5][CH2:6][C:7](=[O:8])[O-:9]>>[CH3:1][c:2]1[cH:3][c:4]([NH:5][CH2:6][C:7](=[O:8])[O-:9])[c:10]([N+:11](=[O:12])[O-:13])[cH:14][c:15]1[Cl:16]
Cc1cc(F)c([N+](=O)[O-])cc1Cl.NCC(=O)[O-]
Cc1cc(NCC(=O)[O-])c([N+](=O)[O-])cc1Cl
null
null
O.CN(C)C=O
Heteroatom Alkylation and Arylation
Buchwald-Hartwig/Ullmann-Goldberg/N-arylation primary amine
da9dae6a655c4bd18887b692f91621e77027436294d6e1fc7be7295afb364796
71a04ae650defc5edd86a92f43c304e981a05f07ff76248da8d4155f3905a29d
c1ccccc1
F-[c;H0;D3;+0:1](:[c:2]:[c:3]):[c:4](-[#7;+:5]):[c:6].[NH2;D1;+0:7]-[C:8]-[C:9](-[O;-;D1;H0:10])=[O;D1;H0:11]>>[#7;+:5]-[c:4](:[c:6]):[c;H0;D3;+0:1](-[NH;D2;+0:7]-[C:8]-[C:9](-[O;-;D1;H0:10])=[O;D1;H0:11]):[c:2]:[c:3]
null
[]
70
CELSIUS
8
HOUR
To a stirred solution of 2-chloro-5-fluoro-4-nitrotoluene (0.605 g, 3.19 mmol, as prepared above) in DMF (3.0 mL) at 70° C., was added dropwise, a solution of sodium glycinate (0.310 g, 3.19 mmol, Aldrich, used as received) in water (3.0 mL). The resulting suspension was stirred overnight at 70° C. The suspension was c...
10.6084/m9.figshare.5104873.v1
null
Aromatic halide.Primary amine
Secondary amine
c1ccccc1
c1ccccc1
c1ccccc1
HF
O.CN(C)C=O
70
8
Cc1cc(F)c([N+](=O)[O-])cc1Cl.NCC(=O)[O-]>O.CN(C)C=O>Cc1cc(NCC(=O)[O-])c([N+](=O)[O-])cc1Cl
ord_dataset-c2ad1656a3ca4d08888ffb6e3f3a2742
ord-cddbda38d6b149dc93731d7fe0f4c254
Cc1cc(NCC(=O)[O-])c([N+](=O)[O-])cc1Cl>>Cc1cc2c(cc1Cl)NC(=O)CN2
[Na+].ClC1=CC(=C(C=C1C)NCC(=O)[O-])[N+](=O)[O-].O.O.[Sn](Cl)Cl>>ClC1=C(C=C2NCC(NC2=C1)=O)C
O=[N+:9]([O-])[c:5]1[c:4]([NH:13][CH2:12][C:10]([O-])=[O:11])[cH:3][c:2]([CH3:1])[c:7]([Cl:8])[cH:6]1>>[CH3:1][c:2]1[cH:3][c:4]2[c:5]([cH:6][c:7]1[Cl:8])[NH:9][C:10](=[O:11])[CH2:12][NH:13]2
Cc1cc(NCC(=O)[O-])c([N+](=O)[O-])cc1Cl
Cc1cc2c(cc1Cl)NC(=O)CN2
null
null
C(C)O
Functional Group Interconversion
OtherReaction
183261da32373f3dc4dd237e8a75ee7d967e6598ba6a325e2c313518785e8076
013ea010a5fc8551154a976160b11b17bb85fae400bd37b37532ea17a3df22d8
O=C1CNc2ccccc2N1
O=[N+;H0;D3:1](-[O-])-[c:2](:[c:3]):[c:4]-[#7:5]-[C:6]-[C;H0;D3;+0:7](-[O-])=[O;D1;H0:8]>>[O;D1;H0:8]=[C;H0;D3;+0:7]1-[C:6]-[#7:5]-[c:4]:[c:2](:[c:3])-[NH;D2;+0:1]-1
66.2
[{"value": 66.0, "product": "ClC1=C(C=C2NCC(NC2=C1)=O)C", "details": "PERCENTYIELD", "is_desired": false}, {"value": 66.2, "product": "ClC1=C(C=C2NCC(NC2=C1)=O)C", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
null
null
A solution of N-(4'-chloro-5'-methyl-2'-nitrophenyl)glycine sodium salt (0.300 g, 1.23 mmol, as prepared above) and tin (II) chloride dihydrate (0.830 g, 3.68 mmol, Aldrich, used as received) in ethanol (4.0 mL) was refluxed for 30 min. It was then cooled to room temperature and the precipitated solid was filtered, was...
10.6084/m9.figshare.5104873.v1
null
Nitro group
Secondary amide
null
c1ccc2c(c1)NCCN2
c1ccc2c(c1)NCCN2
Other
C(C)O
null
null
Cc1cc(NCC(=O)[O-])c([N+](=O)[O-])cc1Cl>C(C)O>Cc1cc2c(cc1Cl)NC(=O)CN2
ord_dataset-c2ad1656a3ca4d08888ffb6e3f3a2742
ord-20edf21ec70840f0a6212c3319d100fd
Clc1ccc(Cl)c(Br)c1.O=[N+]([O-])O>>O=[N+]([O-])c1cc(Cl)c(Br)cc1Cl
BrC1=C(C=CC(=C1)Cl)Cl.[N+](=O)(O)[O-]>>ClC1=C(C=C(C(=C1)[N+](=O)[O-])Cl)Br
[cH:4]1[cH:5][c:6]([Cl:7])[c:8]([Br:9])[cH:10][c:11]1[Cl:12].O[N+:2](=[O:1])[O-:3]>>[O:1]=[N+:2]([O-:3])[c:4]1[cH:5][c:6]([Cl:7])[c:8]([Br:9])[cH:10][c:11]1[Cl:12]
Clc1ccc(Cl)c(Br)c1.O=[N+]([O-])O
O=[N+]([O-])c1cc(Cl)c(Br)cc1Cl
null
null
null
Functional Group Addition
Aromatic nitration with HNO3
53848b8b2bb4e867226e49db2e60519b24be9379900e3ad7c56af54fe8fde7a5
ddce49825c02b8965f10c8d99e3c841d26e1f136da6037b417c09313e6d73097
c1ccccc1
O-[N+;H0;D3:1](-[O;-;D1;H0:2])=[O;D1;H0:3].[Cl;D1;H0:4]-[c:5](:[c:6]):[cH;D2;+0:7]:[c:8]:[c:9]>>[Cl;D1;H0:4]-[c:5](:[c:6]):[c;H0;D3;+0:7](-[N+;H0;D3:1](-[O;-;D1;H0:2])=[O;D1;H0:3]):[c:8]:[c:9]
null
[]
null
null
null
null
A solution of 2-bromo-1,4-dichlorobenzene (1.000 g, 4.443 mmol, Aldrich, used as received) in fuming HNO3 (7.0 mL) was stirred at 50° C. for 1.5 h and poured into ice (80 g). Yellowish white solid was filtered, washed with water (10 mL), and dried under vacuum to obtain 1.14 g (95%) of pure (1H NMR) title compound as a...
10.6084/m9.figshare.5104873.v1
null
Nitrate
Nitro group
c1ccccc1
c1ccccc1
c1ccccc1
HO-
null
null
null
Clc1ccc(Cl)c(Br)c1.O=[N+]([O-])O>>O=[N+]([O-])c1cc(Cl)c(Br)cc1Cl
ord_dataset-c2ad1656a3ca4d08888ffb6e3f3a2742
ord-0b069435ba774dba9ff2497ddd53fbd5
NCC(=O)O.O=[N+]([O-])c1cc(Cl)c(Br)cc1Cl>>O=C([O-])CNc1cc(Br)c(Cl)cc1[N+](=O)[O-]
ClC1=C(C=C(C(=C1)[N+](=O)[O-])Cl)Br.C(=O)(O)[O-].[Na+].NCC(=O)O>>[Na+].BrC=1C(=CC(=C(C1)NCC(=O)[O-])[N+](=O)[O-])Cl
[O:1]=[C:2]([OH:3])[CH2:4][NH2:5].Cl[c:6]1[cH:7][c:8]([Br:9])[c:10]([Cl:11])[cH:12][c:13]1[N+:14](=[O:15])[O-:16]>>[O:1]=[C:2]([O-:3])[CH2:4][NH:5][c:6]1[cH:7][c:8]([Br:9])[c:10]([Cl:11])[cH:12][c:13]1[N+:14](=[O:15])[O-:16]
NCC(=O)O.O=[N+]([O-])c1cc(Cl)c(Br)cc1Cl
O=C([O-])CNc1cc(Br)c(Cl)cc1[N+](=O)[O-]
null
null
O.CN(C)C=O
Functional Group Interconversion
OtherReaction
a2430459d1d806b76ea5929617ab6a3b4b60e59fbb7c728918866c9a46a4773e
ebd1e2e92d10853bf82065836c155b592d0f6786d464f94a738662626a68c1ab
c1ccccc1
Cl-[c;H0;D3;+0:1](:[c:2]:[c:3]):[c:4](-[#7;+:5]):[c:6].[NH2;D1;+0:7]-[C:8]-[C:9](=[O;D1;H0:10])-[OH;D1;+0:11]>>[#7;+:5]-[c:4](:[c:6]):[c;H0;D3;+0:1](-[NH;D2;+0:7]-[C:8]-[C:9](-[O-;H0;D1:11])=[O;D1;H0:10]):[c:2]:[c:3]
null
[]
65
CELSIUS
65
HOUR
To a stirred solution of 2,5-dichloro-4-nitrobromobenzene (1.000 g, 3.691 mmol, as prepared above) in DMF (10.0 mL) at 65° C., was added, dropwise, a solution of NaHCO3 (0.316 g, 3.76 mmol) and glycine (0.280 g, 3.73 mmol, Aldrich, used as received) in water (3.8 mL). The resulting suspension was stirred at 65° C. for ...
10.6084/m9.figshare.5104873.v1
null
Aromatic halide.Carboxylic acid.Primary amine
Secondary amine
c1ccccc1
c1ccccc1
c1ccccc1
HCl
O.CN(C)C=O
65
65
NCC(=O)O.O=[N+]([O-])c1cc(Cl)c(Br)cc1Cl>O.CN(C)C=O>O=C([O-])CNc1cc(Br)c(Cl)cc1[N+](=O)[O-]
ord_dataset-c2ad1656a3ca4d08888ffb6e3f3a2742
ord-ca172412065f4dc89cc0ba64cadecc2a
O=C([O-])CNc1cc(Br)c(Cl)cc1[N+](=O)[O-]>>O=C1CNc2cc(Br)c(Cl)cc2N1
[Na+].BrC=1C(=CC(=C(C1)NCC(=O)[O-])[N+](=O)[O-])Cl.O.O.[Sn](Cl)Cl>>BrC=1C=C2NCC(NC2=CC1Cl)=O
O=[N+:13]([O-])[c:12]1[c:5]([NH:4][CH2:3][C:2]([O-])=[O:1])[cH:6][c:7]([Br:8])[c:9]([Cl:10])[cH:11]1>>[O:1]=[C:2]1[CH2:3][NH:4][c:5]2[cH:6][c:7]([Br:8])[c:9]([Cl:10])[cH:11][c:12]2[NH:13]1
O=C([O-])CNc1cc(Br)c(Cl)cc1[N+](=O)[O-]
O=C1CNc2cc(Br)c(Cl)cc2N1
null
null
C(C)O
Functional Group Interconversion
OtherReaction
183261da32373f3dc4dd237e8a75ee7d967e6598ba6a325e2c313518785e8076
013ea010a5fc8551154a976160b11b17bb85fae400bd37b37532ea17a3df22d8
O=C1CNc2ccccc2N1
O=[N+;H0;D3:1](-[O-])-[c:2](:[c:3]):[c:4]-[#7:5]-[C:6]-[C;H0;D3;+0:7](-[O-])=[O;D1;H0:8]>>[O;D1;H0:8]=[C;H0;D3;+0:7]1-[C:6]-[#7:5]-[c:4]:[c:2](:[c:3])-[NH;D2;+0:1]-1
86
[{"value": 86.0, "product": "BrC=1C=C2NCC(NC2=CC1Cl)=O", "details": "PERCENTYIELD", "is_desired": false}]
null
null
8
HOUR
A solution of N-(5'-bromo-4'-chloro-2'-nitrophenyl)glycine sodium salt (0.255 g, 0.824 mmol, as prepared above) and tin (II) chloride dihydrate (0.560 g, 2.48 mmol, Aldrich, used as received) in ethanol (6 mL) was refluxed for 3 h. It was then cooled to room temperature and allowed to stand overnight at room temperatur...
10.6084/m9.figshare.5104873.v1
null
Nitro group
Secondary amide
null
c1ccc2c(c1)NCCN2
c1ccc2c(c1)NCCN2
Other
C(C)O
null
8
O=C([O-])CNc1cc(Br)c(Cl)cc1[N+](=O)[O-]>C(C)O>O=C1CNc2cc(Br)c(Cl)cc2N1
ord_dataset-c2ad1656a3ca4d08888ffb6e3f3a2742
ord-334f56af14ba41f48cdc5075bfda0fb6
O=C1CNc2cc(Br)c(Cl)cc2N1.O=[N+]([O-])O>>O=c1cnc2c([N+](=O)[O-])c(Br)c(Cl)cc2[nH]1
BrC=1C=C2NCC(NC2=CC1Cl)=O.[N+](=O)(O)[O-]>>BrC=1C(=C2N=CC(NC2=CC1Cl)=O)[N+](=O)[O-]
[O:1]=[C:2]1[CH2:3][NH:4][c:5]2[cH:6][c:10]([Br:11])[c:12]([Cl:13])[cH:14][c:15]2[NH:16]1.O[N+:7](=[O:8])[O-:9]>>[O:1]=[c:2]1[cH:3][n:4][c:5]2[c:6]([N+:7](=[O:8])[O-:9])[c:10]([Br:11])[c:12]([Cl:13])[cH:14][c:15]2[nH:16]1
O=C1CNc2cc(Br)c(Cl)cc2N1.O=[N+]([O-])O
O=c1cnc2c([N+](=O)[O-])c(Br)c(Cl)cc2[nH]1
null
null
C(=O)(C(F)(F)F)O
Functional Group Addition
OtherReaction
e6922c8d1ed2e684d16228320675145012a12d1c7c6f08012225825ad76b19cd
92db0dea6f4127973fddae387509b31c8597671f173224c34b8f168e75366373
O=c1cnc2ccccc2[nH]1
O-[N+;H0;D3:1](-[O;-;D1;H0:2])=[O;D1;H0:3].[Br;D1;H0:4]-[c:5]1:[c:6]:[c:7]:[c:8]2:[c:9](:[cH;D2;+0:10]:1)-[NH;D2;+0:11]-[CH2;D2;+0:12]-[C;H0;D3;+0:13](=[O;D1;H0:14])-[NH;D2;+0:15]-2>>[Br;D1;H0:4]-[c:5]1:[c:6]:[c:7]:[c:8]2:[nH;D2;+0:15]:[c;H0;D3;+0:13](=[O;D1;H0:14]):[cH;D2;+0:12]:[n;H0;D2;+0:11]:[c:9]:2:[c;H0;D3;+0:10]...
70
[{"value": 70.0, "product": "BrC=1C(=C2N=CC(NC2=CC1Cl)=O)[N+](=O)[O-]", "details": "PERCENTYIELD", "is_desired": false}, {"value": 70.0, "product": "BrC=1C(=C2N=CC(NC2=CC1Cl)=O)[N+](=O)[O-]", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
8
HOUR
To a stirred suspension of 6-bromo-7-chloro-3,4-dihydroquinoxaline-2(1H)-one (0.06 g, 0.23 mmol, as obtained above) in CF3COOH (0.5 mL) was added fuming HNO3 (0.02 mL, 0.46 mmol) and the resulting reddish yellow suspension was stirred at room temperature overnight. The cream colored suspension so obtained was poured in...
10.6084/m9.figshare.5104873.v1
null
Nitrate.Secondary amide.Secondary amine
Nitro group
c1ccc2c(c1)NCCN2
c1ccc2nccnc2c1
c1ccc2nccnc2c1
HO-
C(=O)(C(F)(F)F)O
null
8
O=C1CNc2cc(Br)c(Cl)cc2N1.O=[N+]([O-])O>C(=O)(C(F)(F)F)O>O=c1cnc2c([N+](=O)[O-])c(Br)c(Cl)cc2[nH]1
ord_dataset-c2ad1656a3ca4d08888ffb6e3f3a2742
ord-94d496ef03ff467399e1d332ac63af12
O=c1cnc2c([N+](=O)[O-])c(Br)c(Cl)cc2[nH]1>>O=c1[nH]c2cc(Cl)c(Br)c([N+](=O)[O-])c2[nH]c1=O
BrC=1C(=C2N=CC(NC2=CC1Cl)=O)[N+](=O)[O-].[N+](=O)([O-])[O-].[K+]>>BrC=1C(=C2NC(C(NC2=CC1Cl)=O)=O)[N+](=O)[O-]
[O:1]=[c:2]1[nH:3][c:4]2[cH:5][c:6]([Cl:7])[c:8]([Br:9])[c:10]([N+:11](=[O:12])[O-:13])[c:14]2[n:15][cH:16]1>>[O:1]=[c:2]1[nH:3][c:4]2[cH:5][c:6]([Cl:7])[c:8]([Br:9])[c:10]([N+:11](=[O:12])[O-:13])[c:14]2[nH:15][c:16]1=[O:17]
O=c1cnc2c([N+](=O)[O-])c(Br)c(Cl)cc2[nH]1
O=c1[nH]c2cc(Cl)c(Br)c([N+](=O)[O-])c2[nH]c1=O
null
null
OS(=O)(=O)O
Oxidation
OtherReaction
96c202f6e3cb7e50a66333c2dba6347f7ff3c54edf2c49e23e682f9d93af3dd2
82a3692de44364afcfd8cc4460435180e0752c31812bf6008d75e02664a32947
O=c1[nH]c2ccccc2[nH]c1=O
[O;D1;H0:1]=[c:2]1:[#7;a:3]:[c:4](:[c:5]):[c:6](:[c:7]):[n;H0;D2;+0:8]:[cH;D2;+0:9]:1>>[O;D1;H0:10]=[c;H0;D3;+0:9]1:[nH;D2;+0:8]:[c:6](:[c:7]):[c:4](:[c:5]):[#7;a:3]:[c:2]:1=[O;D1;H0:1]
null
[]
null
null
65
HOUR
To a stirred solution of 6-bromo-7-chloro-5-nitroquinoxaline-2(1H)-one (0.025 g, 0.082 mmol, as prepared above) in conc. H2SO4 (0.5 mL) was added KNO3 (0.011 g, 0.11 mmol) and the resulting dark red solution was stirred at room temperature for 65 h. The solution was then cooled in an ice-bath and diluted with ice to a ...
10.6084/m9.figshare.5104873.v1
null
null
null
c1ccc2nccnc2c1
C1=CNc2ccccc2N1
C1=CNc2ccccc2N1
Other
OS(=O)(=O)O
null
65
O=c1cnc2c([N+](=O)[O-])c(Br)c(Cl)cc2[nH]1>OS(=O)(=O)O>O=c1[nH]c2cc(Cl)c(Br)c([N+](=O)[O-])c2[nH]c1=O
ord_dataset-c2ad1656a3ca4d08888ffb6e3f3a2742
ord-b5dd336517fb420bb79c1a6528361ef7
Fc1ccc(F)c(Br)c1>>O=[N+]([O-])c1cc(F)c(Br)cc1F
BrC1=C(C=CC(=C1)F)F.[N+](=O)([O-])[O-].[K+]>>BrC1=C(C=C(C(=C1)F)[N+](=O)[O-])F
[cH:4]1[cH:5][c:6]([F:7])[c:8]([Br:9])[cH:10][c:11]1[F:12]>>[O:1]=[N+:2]([O-:3])[c:4]1[cH:5][c:6]([F:7])[c:8]([Br:9])[cH:10][c:11]1[F:12]
Fc1ccc(F)c(Br)c1
O=[N+]([O-])c1cc(F)c(Br)cc1F
null
null
OS(=O)(=O)O
Functional Group Addition
OtherReaction
6862453966ade01f48ad6e78fdee5c31f5f3bef2a50d1592f73a35f3caf6154f
22f3183026a2d99c91ec0c53f0059a15c8421016bd62c8ab45281362b96dc686
c1ccccc1
[F;D1;H0:1]-[c:2](:[c:3]):[cH;D2;+0:4]:[c:5]:[c:6]>>[F;D1;H0:1]-[c:2](:[c:3]):[c;H0;D3;+0:4](-[#7;+:7](-[O;-;D1;H0:8])=[O;D1;H0:9]):[c:5]:[c:6]
89.4
[{"value": 89.0, "product": "BrC1=C(C=C(C(=C1)F)[N+](=O)[O-])F", "details": "PERCENTYIELD", "is_desired": false}, {"value": 89.4, "product": "BrC1=C(C=C(C(=C1)F)[N+](=O)[O-])F", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
28
CELSIUS
8
HOUR
To a stirred solution of 1-bromo-2,5-difluorobenzene (1.000 g, 5.181 mmol, Aldrich, used as received) in conc. H2SO4 (8.0 mL) at 0° C., KNO3 (0.525 g, 5.19 mmol) was added in one lot. The resulting yellow solution was allowed to warm to 28° C. and stirred at 28° C. overnight. It was then poured into ice (80 g) and extr...
10.6084/m9.figshare.5104873.v1
null
null
Nitro group
c1ccccc1
c1ccccc1
c1ccccc1
Other
OS(=O)(=O)O
28
8
Fc1ccc(F)c(Br)c1>OS(=O)(=O)O>O=[N+]([O-])c1cc(F)c(Br)cc1F
ord_dataset-c2ad1656a3ca4d08888ffb6e3f3a2742
ord-1bdba27d99f44e589e147105b04a762a
NCC(=O)[O-].O=[N+]([O-])c1cc(F)c(Br)cc1F>>O=C([O-])CNc1cc(Br)c(F)cc1[N+](=O)[O-]
BrC1=C(C=C(C(=C1)F)[N+](=O)[O-])F.NCC(=O)[O-].[Na+]>>[Na+].BrC=1C(=CC(=C(C1)NCC(=O)[O-])[N+](=O)[O-])F
[O:1]=[C:2]([O-:3])[CH2:4][NH2:5].F[c:6]1[cH:7][c:8]([Br:9])[c:10]([F:11])[cH:12][c:13]1[N+:14](=[O:15])[O-:16]>>[O:1]=[C:2]([O-:3])[CH2:4][NH:5][c:6]1[cH:7][c:8]([Br:9])[c:10]([F:11])[cH:12][c:13]1[N+:14](=[O:15])[O-:16]
NCC(=O)[O-].O=[N+]([O-])c1cc(F)c(Br)cc1F
O=C([O-])CNc1cc(Br)c(F)cc1[N+](=O)[O-]
null
null
O.CN(C)C=O
Heteroatom Alkylation and Arylation
Buchwald-Hartwig/Ullmann-Goldberg/N-arylation primary amine
da9dae6a655c4bd18887b692f91621e77027436294d6e1fc7be7295afb364796
71a04ae650defc5edd86a92f43c304e981a05f07ff76248da8d4155f3905a29d
c1ccccc1
F-[c;H0;D3;+0:1](:[c:2]:[c:3]):[c:4](-[#7;+:5]):[c:6].[NH2;D1;+0:7]-[C:8]-[C:9](-[O;-;D1;H0:10])=[O;D1;H0:11]>>[#7;+:5]-[c:4](:[c:6]):[c;H0;D3;+0:1](-[NH;D2;+0:7]-[C:8]-[C:9](-[O;-;D1;H0:10])=[O;D1;H0:11]):[c:2]:[c:3]
35
[{"value": 35.0, "product": "[Na+].BrC=1C(=CC(=C(C1)NCC(=O)[O-])[N+](=O)[O-])F", "details": "PERCENTYIELD", "is_desired": false}, {"value": 32.2, "product": "[Na+].BrC=1C(=CC(=C(C1)NCC(=O)[O-])[N+](=O)[O-])F", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
70
CELSIUS
8
HOUR
To a stirred solution of 1-bromo-2,5-difluoro-4-nitrobenzene (1.100 g, 4.622 mmol, as prepared above) in DMF (11.0 mL) at 70° C., was added, dropwise, a solution of sodium glycinate (0.451 g, 4.65 mmol, Aldrich, used as received) in water (5.0 mL). The resulting solution was stirred overnight at 70° C. The solution was...
10.6084/m9.figshare.5104873.v1
null
Aromatic halide.Primary amine
Secondary amine
c1ccccc1
c1ccccc1
c1ccccc1
HF
O.CN(C)C=O
70
8
NCC(=O)[O-].O=[N+]([O-])c1cc(F)c(Br)cc1F>O.CN(C)C=O>O=C([O-])CNc1cc(Br)c(F)cc1[N+](=O)[O-]
ord_dataset-c2ad1656a3ca4d08888ffb6e3f3a2742
ord-15e37d10d88148d9bb4bb35e4f153e2c
O=C([O-])CNc1cc(Br)c(F)cc1[N+](=O)[O-]>>O=C1CNc2cc(Br)c(F)cc2N1
[Na+].BrC=1C(=CC(=C(C1)NCC(=O)[O-])[N+](=O)[O-])F.O.O.[Sn](Cl)Cl>>BrC=1C=C2NCC(NC2=CC1F)=O
O=[N+:13]([O-])[c:12]1[c:5]([NH:4][CH2:3][C:2]([O-])=[O:1])[cH:6][c:7]([Br:8])[c:9]([F:10])[cH:11]1>>[O:1]=[C:2]1[CH2:3][NH:4][c:5]2[cH:6][c:7]([Br:8])[c:9]([F:10])[cH:11][c:12]2[NH:13]1
O=C([O-])CNc1cc(Br)c(F)cc1[N+](=O)[O-]
O=C1CNc2cc(Br)c(F)cc2N1
null
null
C(C)O
Functional Group Interconversion
OtherReaction
183261da32373f3dc4dd237e8a75ee7d967e6598ba6a325e2c313518785e8076
013ea010a5fc8551154a976160b11b17bb85fae400bd37b37532ea17a3df22d8
O=C1CNc2ccccc2N1
O=[N+;H0;D3:1](-[O-])-[c:2](:[c:3]):[c:4]-[#7:5]-[C:6]-[C;H0;D3;+0:7](-[O-])=[O;D1;H0:8]>>[O;D1;H0:8]=[C;H0;D3;+0:7]1-[C:6]-[#7:5]-[c:4]:[c:2](:[c:3])-[NH;D2;+0:1]-1
64
[{"value": 64.0, "product": "BrC=1C=C2NCC(NC2=CC1F)=O", "details": "PERCENTYIELD", "is_desired": false}, {"value": 63.9, "product": "BrC=1C=C2NCC(NC2=CC1F)=O", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
null
null
N-(5'-bromo-4'-fluoro-2'-nitrophenyl)glycine sodium salt (0.450 g, 1.54 mmol, as prepared above) and tin (II) chloride dihydrate (1.039 g, 4.605 mmol, Aldrich, used as received) in ethanol (7.0 mL) was refluxed for 30 min. It was then cooled to room temperature and solvent was removed under vacuum. The residue was dilu...
10.6084/m9.figshare.5104873.v1
null
Nitro group
Secondary amide
null
c1ccc2c(c1)NCCN2
c1ccc2c(c1)NCCN2
Other
C(C)O
null
null
O=C([O-])CNc1cc(Br)c(F)cc1[N+](=O)[O-]>C(C)O>O=C1CNc2cc(Br)c(F)cc2N1
ord_dataset-c2ad1656a3ca4d08888ffb6e3f3a2742
ord-8e5fea2bcbfc49a781474b90155555c6
Fc1ccc(Br)c(F)c1>>O=[N+]([O-])c1cc(Br)c(F)cc1F
BrC1=C(C=C(C=C1)F)F.[N+](=O)([O-])[O-].[K+]>>BrC1=C(C=C(C(=C1)[N+](=O)[O-])F)F
[cH:4]1[cH:5][c:6]([Br:7])[c:8]([F:9])[cH:10][c:11]1[F:12]>>[O:1]=[N+:2]([O-:3])[c:4]1[cH:5][c:6]([Br:7])[c:8]([F:9])[cH:10][c:11]1[F:12]
Fc1ccc(Br)c(F)c1
O=[N+]([O-])c1cc(Br)c(F)cc1F
null
null
OS(=O)(=O)O
Functional Group Addition
OtherReaction
6862453966ade01f48ad6e78fdee5c31f5f3bef2a50d1592f73a35f3caf6154f
22f3183026a2d99c91ec0c53f0059a15c8421016bd62c8ab45281362b96dc686
c1ccccc1
[F;D1;H0:1]-[c:2](:[c:3]):[cH;D2;+0:4]:[c:5]:[c:6]>>[F;D1;H0:1]-[c:2](:[c:3]):[c;H0;D3;+0:4](-[#7;+:7](-[O;-;D1;H0:8])=[O;D1;H0:9]):[c:5]:[c:6]
null
[]
28
CELSIUS
8
HOUR
To a stirred solution of 1-bromo-2,4-difluorobenzene (0.512 g, 2.65 mmol, Aldrich, used as received) in conc. H2SO4 (5.0 mL) at 0° C., KNO3 (0.275 g, 2.72 mmol) was added in one lot. The resulting solution was allowed to warm to 28° C. and stirred at that temperature overnight. It was then poured into ice (50 g) and ex...
10.6084/m9.figshare.5104873.v1
null
null
Nitro group
c1ccccc1
c1ccccc1
c1ccccc1
Other
OS(=O)(=O)O
28
8
Fc1ccc(Br)c(F)c1>OS(=O)(=O)O>O=[N+]([O-])c1cc(Br)c(F)cc1F
ord_dataset-c2ad1656a3ca4d08888ffb6e3f3a2742
ord-3b2d4eb0ed2e4dee9788780360db7fee
O=C(O)CNc1cc(F)c(Br)cc1[N+](=O)[O-]>>O=C1CNc2cc(F)c(Br)cc2N1
BrC1=CC(=C(C=C1F)NCC(=O)O)[N+](=O)[O-].BrC1=C(C=C(C(=C1)[N+](=O)[O-])F)NCC(=O)O.O.O.[Sn](Cl)Cl>>BrC1=C(C=C2NCC(NC2=C1)=O)F
O=[N+:13]([O-])[c:12]1[c:5]([NH:4][CH2:3][C:2](O)=[O:1])[cH:6][c:7]([F:8])[c:9]([Br:10])[cH:11]1>>[O:1]=[C:2]1[CH2:3][NH:4][c:5]2[cH:6][c:7]([F:8])[c:9]([Br:10])[cH:11][c:12]2[NH:13]1
O=C(O)CNc1cc(F)c(Br)cc1[N+](=O)[O-]
O=C1CNc2cc(F)c(Br)cc2N1
null
null
C(C)O
Functional Group Interconversion
OtherReaction
248a0ced66d35d5637fd333df7859a163df67de7a5eafc38f3d14fb913b635e3
98c112fcc8dd821704dc378798368c2081a2acc574356674c70af3e59954ee0d
O=C1CNc2ccccc2N1
O-[C;H0;D3;+0:1](=[O;D1;H0:2])-[C:3]-[#7:4]-[c:5]:[c:6](-[N+;H0;D3:7](=O)-[O-]):[c:8]>>[O;D1;H0:2]=[C;H0;D3;+0:1]1-[C:3]-[#7:4]-[c:5]:[c:6](:[c:8])-[NH;D2;+0:7]-1
null
[]
null
null
null
null
A solution of a mixture of N-(4'-bromo-5'-fluoro-2'-nitrophenyl)glycine and N-(2'-bromo-5'-fluoro-4'-nitrophenyl)glycine (0.150 g, 0.512 mmol, as prepared above) and tin (II) chloride dihydrate (0.346 g, 1.53 mmol, Aldrich, used as received) in ethanol (3.0 mL) was refluxed for 30 min. It was then cooled to room temper...
10.6084/m9.figshare.5104873.v1
null
Carboxylic acid.Nitro group
Secondary amide
null
c1ccc2c(c1)NCCN2
c1ccc2c(c1)NCCN2
Other
C(C)O
null
null
O=C(O)CNc1cc(F)c(Br)cc1[N+](=O)[O-]>C(C)O>O=C1CNc2cc(F)c(Br)cc2N1
ord_dataset-c2ad1656a3ca4d08888ffb6e3f3a2742
ord-df080efb7627478b95dffad12a254006
Cc1cc(F)ccc1Br>>Cc1cc(F)c([N+](=O)[O-])cc1Br
BrC1=C(C=C(C=C1)F)C.[N+](=O)([O-])[O-].[K+]>>BrC1=C(C=C(C(=C1)[N+](=O)[O-])F)C
[CH3:1][c:2]1[cH:3][c:4]([F:5])[cH:6][cH:10][c:11]1[Br:12]>>[CH3:1][c:2]1[cH:3][c:4]([F:5])[c:6]([N+:7](=[O:8])[O-:9])[cH:10][c:11]1[Br:12]
Cc1cc(F)ccc1Br
Cc1cc(F)c([N+](=O)[O-])cc1Br
null
null
OS(=O)(=O)O
Functional Group Addition
OtherReaction
6862453966ade01f48ad6e78fdee5c31f5f3bef2a50d1592f73a35f3caf6154f
22f3183026a2d99c91ec0c53f0059a15c8421016bd62c8ab45281362b96dc686
c1ccccc1
[F;D1;H0:1]-[c:2](:[c:3]):[cH;D2;+0:4]:[c:5]:[c:6]>>[F;D1;H0:1]-[c:2](:[c:3]):[c;H0;D3;+0:4](-[#7;+:7](-[O;-;D1;H0:8])=[O;D1;H0:9]):[c:5]:[c:6]
99
[{"value": 98.0, "product": "BrC1=C(C=C(C(=C1)[N+](=O)[O-])F)C", "details": "PERCENTYIELD", "is_desired": false}, {"value": 99.0, "product": "BrC1=C(C=C(C(=C1)[N+](=O)[O-])F)C", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
28
CELSIUS
8
HOUR
To a stirred solution of 2-bromo-5-fluorotoluene (1.495 g, 7.909 mmol, Aldrich, used as received) in conc. H2SO4 (10.0 mL) at 0° C., KNO3 (0.800 g, 7.91 mmol) was added in one lot. The resulting pale yellow solution was warmed to 28° C. and stirred overnight at 28° C. It was then poured into ice (50 g) and extracted wi...
10.6084/m9.figshare.5104873.v1
null
null
Nitro group
c1ccccc1
c1ccccc1
c1ccccc1
Other
OS(=O)(=O)O
28
8
Cc1cc(F)ccc1Br>OS(=O)(=O)O>Cc1cc(F)c([N+](=O)[O-])cc1Br
ord_dataset-c2ad1656a3ca4d08888ffb6e3f3a2742
ord-1be67ca729984837a23c9cd02623e794
Cc1cc(F)c([N+](=O)[O-])cc1Br.NCC(=O)[O-]>>Cc1cc(NCC(=O)[O-])c([N+](=O)[O-])cc1Br
BrC1=C(C=C(C(=C1)[N+](=O)[O-])F)C.NCC(=O)[O-].[Na+]>>[Na+].BrC1=CC(=C(C=C1C)NCC(=O)[O-])[N+](=O)[O-]
F[c:4]1[cH:3][c:2]([CH3:1])[c:15]([Br:16])[cH:14][c:10]1[N+:11](=[O:12])[O-:13].[NH2:5][CH2:6][C:7](=[O:8])[O-:9]>>[CH3:1][c:2]1[cH:3][c:4]([NH:5][CH2:6][C:7](=[O:8])[O-:9])[c:10]([N+:11](=[O:12])[O-:13])[cH:14][c:15]1[Br:16]
Cc1cc(F)c([N+](=O)[O-])cc1Br.NCC(=O)[O-]
Cc1cc(NCC(=O)[O-])c([N+](=O)[O-])cc1Br
null
null
O.CN(C)C=O
Heteroatom Alkylation and Arylation
Buchwald-Hartwig/Ullmann-Goldberg/N-arylation primary amine
da9dae6a655c4bd18887b692f91621e77027436294d6e1fc7be7295afb364796
71a04ae650defc5edd86a92f43c304e981a05f07ff76248da8d4155f3905a29d
c1ccccc1
F-[c;H0;D3;+0:1](:[c:2]:[c:3]):[c:4](-[#7;+:5]):[c:6].[NH2;D1;+0:7]-[C:8]-[C:9](-[O;-;D1;H0:10])=[O;D1;H0:11]>>[#7;+:5]-[c:4](:[c:6]):[c;H0;D3;+0:1](-[NH;D2;+0:7]-[C:8]-[C:9](-[O;-;D1;H0:10])=[O;D1;H0:11]):[c:2]:[c:3]
null
[]
70
CELSIUS
8
HOUR
To a stirred solution of 2-bromo-5-fluoro-4-nitrotoluene (1.662 g, 7.102 mmol, as prepared above) in DMF (7.0 mL) at 70° C., was added, dropwise, a solution of sodium glycinate (0.690 g, 7.11 mmol, Aldrich, used as received) in water (7.0 mL). The resulting suspension was stirred overnight at 70° C. The suspension was ...
10.6084/m9.figshare.5104873.v1
null
Aromatic halide.Primary amine
Secondary amine
c1ccccc1
c1ccccc1
c1ccccc1
HF
O.CN(C)C=O
70
8
Cc1cc(F)c([N+](=O)[O-])cc1Br.NCC(=O)[O-]>O.CN(C)C=O>Cc1cc(NCC(=O)[O-])c([N+](=O)[O-])cc1Br
ord_dataset-c2ad1656a3ca4d08888ffb6e3f3a2742
ord-170bfe4b83bd411a95c389639b5e87c3
Cc1cc(NCC(=O)[O-])c([N+](=O)[O-])cc1Br>>Cc1cc2c(cc1Br)NC(=O)CN2
[Na+].BrC1=CC(=C(C=C1C)NCC(=O)[O-])[N+](=O)[O-].O.O.[Sn](Cl)Cl>>BrC1=C(C=C2NCC(NC2=C1)=O)C
O=[N+:9]([O-])[c:5]1[c:4]([NH:13][CH2:12][C:10]([O-])=[O:11])[cH:3][c:2]([CH3:1])[c:7]([Br:8])[cH:6]1>>[CH3:1][c:2]1[cH:3][c:4]2[c:5]([cH:6][c:7]1[Br:8])[NH:9][C:10](=[O:11])[CH2:12][NH:13]2
Cc1cc(NCC(=O)[O-])c([N+](=O)[O-])cc1Br
Cc1cc2c(cc1Br)NC(=O)CN2
null
null
C(C)O
Functional Group Interconversion
OtherReaction
183261da32373f3dc4dd237e8a75ee7d967e6598ba6a325e2c313518785e8076
013ea010a5fc8551154a976160b11b17bb85fae400bd37b37532ea17a3df22d8
O=C1CNc2ccccc2N1
O=[N+;H0;D3:1](-[O-])-[c:2](:[c:3]):[c:4]-[#7:5]-[C:6]-[C;H0;D3;+0:7](-[O-])=[O;D1;H0:8]>>[O;D1;H0:8]=[C;H0;D3;+0:7]1-[C:6]-[#7:5]-[c:4]:[c:2](:[c:3])-[NH;D2;+0:1]-1
38.4
[{"value": 38.0, "product": "BrC1=C(C=C2NCC(NC2=C1)=O)C", "details": "PERCENTYIELD", "is_desired": false}, {"value": 38.4, "product": "BrC1=C(C=C2NCC(NC2=C1)=O)C", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
null
null
A solution of N-(4'-bromo-5'-methyl-2'-nitrophenyl)glycine sodium salt (0.200 g, 0.692 mmol, as prepared above) and tin (II) chloride dihydrate (0.468 g, 2.07 mmol, Aldrich, used as received) in ethanol (2.0 mL) was refluxed for 30 min. It was then cooled to room temperature. The precipitated solid was filtered and dri...
10.6084/m9.figshare.5104873.v1
null
Nitro group
Secondary amide
null
c1ccc2c(c1)NCCN2
c1ccc2c(c1)NCCN2
Other
C(C)O
null
null
Cc1cc(NCC(=O)[O-])c([N+](=O)[O-])cc1Br>C(C)O>Cc1cc2c(cc1Br)NC(=O)CN2
ord_dataset-c2ad1656a3ca4d08888ffb6e3f3a2742
ord-3d9b42a8b7534529b0009aa51e2fe56a
Fc1ccc(Cl)c(F)c1>>O=[N+]([O-])c1cc(Cl)c(F)cc1F
ClC1=C(C=C(C=C1)F)F.[N+](=O)([O-])[O-].[K+]>>ClC1=C(C=C(C(=C1)[N+](=O)[O-])F)F
[cH:4]1[cH:5][c:6]([Cl:7])[c:8]([F:9])[cH:10][c:11]1[F:12]>>[O:1]=[N+:2]([O-:3])[c:4]1[cH:5][c:6]([Cl:7])[c:8]([F:9])[cH:10][c:11]1[F:12]
Fc1ccc(Cl)c(F)c1
O=[N+]([O-])c1cc(Cl)c(F)cc1F
null
null
OS(=O)(=O)O
Functional Group Addition
OtherReaction
6862453966ade01f48ad6e78fdee5c31f5f3bef2a50d1592f73a35f3caf6154f
22f3183026a2d99c91ec0c53f0059a15c8421016bd62c8ab45281362b96dc686
c1ccccc1
[F;D1;H0:1]-[c:2](:[c:3]):[cH;D2;+0:4]:[c:5]:[c:6]>>[F;D1;H0:1]-[c:2](:[c:3]):[c;H0;D3;+0:4](-[#7;+:7](-[O;-;D1;H0:8])=[O;D1;H0:9]):[c:5]:[c:6]
null
[]
28
CELSIUS
8
HOUR
To a stirred solution of 1-chloro-2,4-difluorobenzene (0.829 g, 5.58 mmol, Aldrich, used as received) in conc. H2SO4 (8.0 mL) at 0° C., KNO3 (0.565 g, 5.59 mmol) was added in one lot. The resulting solution was allowed to warm to 28° C. and stirred overnight at 28° C. It was then poured into ice (80 g) and extracted wi...
10.6084/m9.figshare.5104873.v1
null
null
Nitro group
c1ccccc1
c1ccccc1
c1ccccc1
Other
OS(=O)(=O)O
28
8
Fc1ccc(Cl)c(F)c1>OS(=O)(=O)O>O=[N+]([O-])c1cc(Cl)c(F)cc1F
ord_dataset-c2ad1656a3ca4d08888ffb6e3f3a2742
ord-b0b95af2a07c4e2ba77f3872c698d610
O=C([O-])CNc1cc(F)c(Cl)cc1[N+](=O)[O-]>>O=C1CNc2cc(F)c(Cl)cc2N1
[Na+].ClC1=CC(=C(C=C1F)NCC(=O)[O-])[N+](=O)[O-].[Na+].ClC1=C(C=C(C(=C1)[N+](=O)[O-])F)NCC(=O)[O-].O.O.[Sn](Cl)Cl>>ClC1=C(C=C2NCC(NC2=C1)=O)F
O=[N+:13]([O-])[c:12]1[c:5]([NH:4][CH2:3][C:2]([O-])=[O:1])[cH:6][c:7]([F:8])[c:9]([Cl:10])[cH:11]1>>[O:1]=[C:2]1[CH2:3][NH:4][c:5]2[cH:6][c:7]([F:8])[c:9]([Cl:10])[cH:11][c:12]2[NH:13]1
O=C([O-])CNc1cc(F)c(Cl)cc1[N+](=O)[O-]
O=C1CNc2cc(F)c(Cl)cc2N1
null
null
C(C)O
Functional Group Interconversion
OtherReaction
183261da32373f3dc4dd237e8a75ee7d967e6598ba6a325e2c313518785e8076
013ea010a5fc8551154a976160b11b17bb85fae400bd37b37532ea17a3df22d8
O=C1CNc2ccccc2N1
O=[N+;H0;D3:1](-[O-])-[c:2](:[c:3]):[c:4]-[#7:5]-[C:6]-[C;H0;D3;+0:7](-[O-])=[O;D1;H0:8]>>[O;D1;H0:8]=[C;H0;D3;+0:7]1-[C:6]-[#7:5]-[c:4]:[c:2](:[c:3])-[NH;D2;+0:1]-1
null
[]
null
null
null
null
A solution of a mixture of N-(4'-chloro-5'-fluoro-2'-nitrophenyl)glycine sodium salt and N-(2'-chloro-5'-fluoro-4'-nitrophenyl)glycine sodium salt (0.175 g, 0.704 mmol, as prepared above) and tin (II) chloride dihydrate (0.475 g, 2.11 mmol, Aldrich, used as received) in ethanol (3.5 mL) was refluxed for 30 min. It was ...
10.6084/m9.figshare.5104873.v1
null
Nitro group
Secondary amide
null
c1ccc2c(c1)NCCN2
c1ccc2c(c1)NCCN2
Other
C(C)O
null
null
O=C([O-])CNc1cc(F)c(Cl)cc1[N+](=O)[O-]>C(C)O>O=C1CNc2cc(F)c(Cl)cc2N1
ord_dataset-c2ad1656a3ca4d08888ffb6e3f3a2742
ord-a5ae1c95958b469682aaea64e7a91558
O=c1[nH]c2cc(F)c(F)c([N+](=O)[O-])c2[nH]c1=O.[NH4+]>>Nc1c(F)cc2[nH]c(=O)c(=O)[nH]c2c1[N+](=O)[O-]
FC=1C(=C2NC(C(NC2=CC1F)=O)=O)[N+](=O)[O-].[OH-].[NH4+].Cl>>NC=1C(=C2NC(C(NC2=CC1F)=O)=O)[N+](=O)[O-]
F[c:2]1[c:3]([F:4])[cH:5][c:6]2[nH:7][c:8](=[O:9])[c:10](=[O:11])[nH:12][c:13]2[c:14]1[N+:15](=[O:16])[O-:17].[NH4+:1]>>[NH2:1][c:2]1[c:3]([F:4])[cH:5][c:6]2[nH:7][c:8](=[O:9])[c:10](=[O:11])[nH:12][c:13]2[c:14]1[N+:15](=[O:16])[O-:17]
O=c1[nH]c2cc(F)c(F)c([N+](=O)[O-])c2[nH]c1=O.[NH4+]
Nc1c(F)cc2[nH]c(=O)c(=O)[nH]c2c1[N+](=O)[O-]
null
[OH-].[NH4+]
O
Functional Group Interconversion
OtherReaction
8f4f69ff4fc6f6debd38e640de53e6bbf37fe0ffa13d22b66fd2d77e6c98fc57
560c85d40afb1a57d77cf3258abf3be5bba829f35224f8687bf9a1d4c1f94bd9
O=c1[nH]c2ccccc2[nH]c1=O
F-[c;H0;D3;+0:1]1:[c:2](-[#7;+:3]):[c:4]2:[#7;a:5]:[c:6]:[c:7]:[#7;a:8]:[c:9]:2:[c:10]:[c:11]:1-[F;D1;H0:12].[NH4+;D0:13]>>[#7;+:3]-[c:2]1:[c:4]2:[#7;a:5]:[c:6]:[c:7]:[#7;a:8]:[c:9]:2:[c:10]:[c:11](-[F;D1;H0:12]):[c;H0;D3;+0:1]:1-[NH2;D1;+0:13]
76
[{"value": 76.0, "product": "NC=1C(=C2NC(C(NC2=CC1F)=O)=O)[N+](=O)[O-]", "details": "PERCENTYIELD", "is_desired": false}]
80
CELSIUS
null
null
To a solution of 20 mg (0.082 mmol) of 6,7-difluoro-5-nitro-1,4-dihydroquinoxaline-2,3-dione in 0.5 mL of DMSO-d6 was added 2 drops of 30% ammonium hydroxide and the solution was heated at 80° C. for 24 h. To the mixture was added one more drop of 30% ammonium hydroxide and it was heated at 80° C. for 10 h. The mixture...
10.6084/m9.figshare.5104873.v1
null
Aromatic halide
Primary amine
C1=CNc2ccccc2N1
C1=CNc2ccccc2N1
C1=CNc2ccccc2N1
HF
[OH-].[NH4+].O
80
null
O=c1[nH]c2cc(F)c(F)c([N+](=O)[O-])c2[nH]c1=O.[NH4+]>[OH-].[NH4+].O>Nc1c(F)cc2[nH]c(=O)c(=O)[nH]c2c1[N+](=O)[O-]
ord_dataset-c2ad1656a3ca4d08888ffb6e3f3a2742
ord-4ac1b182a1b047c9bcfb08ee4bb87260
C[O-].O=c1[nH]c2cc(F)c(F)c([N+](=O)[O-])c2[nH]c1=O>>COc1c(F)cc2[nH]c(=O)c(=O)[nH]c2c1[N+](=O)[O-]
FC=1C(=C2NC(C(NC2=CC1F)=O)=O)[N+](=O)[O-].C[O-].[Na+].Cl>>FC1=C(C(=C2NC(C(NC2=C1)=O)=O)[N+](=O)[O-])OC
[CH3:1][O-:2].F[c:3]1[c:4]([F:5])[cH:6][c:7]2[nH:8][c:9](=[O:10])[c:11](=[O:12])[nH:13][c:14]2[c:15]1[N+:16](=[O:17])[O-:18]>>[CH3:1][O:2][c:3]1[c:4]([F:5])[cH:6][c:7]2[nH:8][c:9](=[O:10])[c:11](=[O:12])[nH:13][c:14]2[c:15]1[N+:16](=[O:17])[O-:18]
C[O-].O=c1[nH]c2cc(F)c(F)c([N+](=O)[O-])c2[nH]c1=O
COc1c(F)cc2[nH]c(=O)c(=O)[nH]c2c1[N+](=O)[O-]
null
null
O
Heteroatom Alkylation and Arylation
OtherReaction
8f5da7fe2bfdb6898cabd699e332b74d553c190b8b21b1599bb1f70cc864c524
51fd03eb6a688046e417b9ed09ea0e72062396d005af1318b9b5f376a97da959
O=c1[nH]c2ccccc2[nH]c1=O
F-[c;H0;D3;+0:1]1:[c:2](-[#7;+:3]):[c:4]2:[#7;a:5]:[c:6]:[c:7]:[#7;a:8]:[c:9]:2:[c:10]:[c:11]:1-[F;D1;H0:12].[C;D1;H3:13]-[O-;H0;D1:14]>>[#7;+:3]-[c:2]1:[c:4]2:[#7;a:5]:[c:6]:[c:7]:[#7;a:8]:[c:9]:2:[c:10]:[c:11](-[F;D1;H0:12]):[c;H0;D3;+0:1]:1-[O;H0;D2;+0:14]-[C;D1;H3:13]
77.5
[{"value": 77.0, "product": "FC1=C(C(=C2NC(C(NC2=C1)=O)=O)[N+](=O)[O-])OC", "details": "PERCENTYIELD", "is_desired": false}, {"value": 77.5, "product": "FC1=C(C(=C2NC(C(NC2=C1)=O)=O)[N+](=O)[O-])OC", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
10
SECOND
To a solution of 21 mg (0.086 mmol) of 6,7-difluoro-5-nitro-1,4-dihydroquinoxaline-2,3-dione in 0.5 mL of DMSO-d6 was added 16 mg (0.29 mmol) of sodium methoxide. The solution was shaken in a vortex for 10 s and kept at room temperature for 3 h. It was then added to 3 mL of water and acidified with 2N HCl to pH=4. The ...
10.6084/m9.figshare.5104873.v1
null
Aromatic halide
Ether
C1=CNc2ccccc2N1
C1=CNc2ccccc2N1
C1=CNc2ccccc2N1
Other
O
null
0.002778
C[O-].O=c1[nH]c2cc(F)c(F)c([N+](=O)[O-])c2[nH]c1=O>O>COc1c(F)cc2[nH]c(=O)c(=O)[nH]c2c1[N+](=O)[O-]
ord_dataset-c2ad1656a3ca4d08888ffb6e3f3a2742
ord-e8c46cbae4c34f099d61289b32e13ed2
CC[O-].O=c1[nH]c2cc(F)c(F)c([N+](=O)[O-])c2[nH]c1=O>>CCOc1c(F)cc2[nH]c(=O)c(=O)[nH]c2c1[N+](=O)[O-]
FC=1C(=C2NC(C(NC2=CC1F)=O)=O)[N+](=O)[O-].[O-]CC.[Na+].Cl>>FC1=C(C(=C2NC(C(NC2=C1)=O)=O)[N+](=O)[O-])OCC
[CH3:1][CH2:2][O-:3].F[c:4]1[c:5]([F:6])[cH:7][c:8]2[nH:9][c:10](=[O:11])[c:12](=[O:13])[nH:14][c:15]2[c:16]1[N+:17](=[O:18])[O-:19]>>[CH3:1][CH2:2][O:3][c:4]1[c:5]([F:6])[cH:7][c:8]2[nH:9][c:10](=[O:11])[c:12](=[O:13])[nH:14][c:15]2[c:16]1[N+:17](=[O:18])[O-:19]
CC[O-].O=c1[nH]c2cc(F)c(F)c([N+](=O)[O-])c2[nH]c1=O
CCOc1c(F)cc2[nH]c(=O)c(=O)[nH]c2c1[N+](=O)[O-]
null
null
O
Heteroatom Alkylation and Arylation
OtherReaction
8f5da7fe2bfdb6898cabd699e332b74d553c190b8b21b1599bb1f70cc864c524
51fd03eb6a688046e417b9ed09ea0e72062396d005af1318b9b5f376a97da959
O=c1[nH]c2ccccc2[nH]c1=O
F-[c;H0;D3;+0:1]1:[c:2](-[#7;+:3]):[c:4]2:[#7;a:5]:[c:6]:[c:7]:[#7;a:8]:[c:9]:2:[c:10]:[c:11]:1-[F;D1;H0:12].[C;D1;H3:13]-[C:14]-[O-;H0;D1:15]>>[#7;+:3]-[c:2]1:[c:4]2:[#7;a:5]:[c:6]:[c:7]:[#7;a:8]:[c:9]:2:[c:10]:[c:11](-[F;D1;H0:12]):[c;H0;D3;+0:1]:1-[O;H0;D2;+0:15]-[C:14]-[C;D1;H3:13]
91
[{"value": 91.0, "product": "FC1=C(C(=C2NC(C(NC2=C1)=O)=O)[N+](=O)[O-])OCC", "details": "PERCENTYIELD", "is_desired": false}, {"value": 91.0, "product": "FC1=C(C(=C2NC(C(NC2=C1)=O)=O)[N+](=O)[O-])OCC", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
null
null
A solution of 24 mg (0.098 mmol) of 6,7-difluoro-5-nitro-1,4-dihydroquinoxaline-2,3-dione and 24 mg (0.33 mmol) of sodium ethoxide (96%) in 0.5 mL of DMSO-d6 was kept at room temperature for 5 h. The red solution was added to 3 mL of water and acidified with 2N HCl to pH=4. The precipitate was filtered, washed with wat...
10.6084/m9.figshare.5104873.v1
null
Aromatic halide
Ether
C1=CNc2ccccc2N1
C1=CNc2ccccc2N1
C1=CNc2ccccc2N1
Other
O
null
null
CC[O-].O=c1[nH]c2cc(F)c(F)c([N+](=O)[O-])c2[nH]c1=O>O>CCOc1c(F)cc2[nH]c(=O)c(=O)[nH]c2c1[N+](=O)[O-]
ord_dataset-c2ad1656a3ca4d08888ffb6e3f3a2742
ord-d70cdbc2c5ed458ba2904ae61b20a51d
O=c1[nH]c2cc(F)c(F)c([N+](=O)[O-])c2[nH]c1=O.[OH-]>>O=c1[nH]c2cc(F)c(O)c([N+](=O)[O-])c2[nH]c1=O
FC=1C(=C2NC(C(NC2=CC1F)=O)=O)[N+](=O)[O-].[OH-].[Na+].Cl>>FC1=C(C(=C2NC(C(NC2=C1)=O)=O)[N+](=O)[O-])O
F[c:8]1[c:6]([F:7])[cH:5][c:4]2[nH:3][c:2](=[O:1])[c:16](=[O:17])[nH:15][c:14]2[c:10]1[N+:11](=[O:12])[O-:13].[OH-:9]>>[O:1]=[c:2]1[nH:3][c:4]2[cH:5][c:6]([F:7])[c:8]([OH:9])[c:10]([N+:11](=[O:12])[O-:13])[c:14]2[nH:15][c:16]1=[O:17]
O=c1[nH]c2cc(F)c(F)c([N+](=O)[O-])c2[nH]c1=O.[OH-]
O=c1[nH]c2cc(F)c(O)c([N+](=O)[O-])c2[nH]c1=O
null
null
O
Heteroatom Alkylation and Arylation
OtherReaction
8f69e382ad3e3b305956707d493f91d1500fa55eff550db7ecd715f8d3799832
05ba928edd770174a8e0738270a5c99182284743586e41e52e6183b77c44ac41
O=c1[nH]c2ccccc2[nH]c1=O
F-[c;H0;D3;+0:1]1:[c:2](-[#7;+:3]):[c:4]2:[#7;a:5]:[c:6]:[c:7]:[#7;a:8]:[c:9]:2:[c:10]:[c:11]:1-[F;D1;H0:12].[OH-;D0:13]>>[#7;+:3]-[c:2]1:[c:4]2:[#7;a:5]:[c:6]:[c:7]:[#7;a:8]:[c:9]:2:[c:10]:[c:11](-[F;D1;H0:12]):[c;H0;D3;+0:1]:1-[OH;D1;+0:13]
80.4
[{"value": 80.0, "product": "FC1=C(C(=C2NC(C(NC2=C1)=O)=O)[N+](=O)[O-])O", "details": "PERCENTYIELD", "is_desired": false}, {"value": 80.4, "product": "FC1=C(C(=C2NC(C(NC2=C1)=O)=O)[N+](=O)[O-])O", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
105
CELSIUS
null
null
A mixture of 24 mg (0.098 mmol) of 6,7-difluoro-5-nitro-1,4-dihydroquinoxaline-2,3-dione and 19 mg (0.47 mmol) of sodium hydroxide in 0.6 mL of D2O was heated at 105° C. for 24 h. The mixture was added to 2 mL of water and acidified with 2N HCl to pH=1. The precipitate was filtered, washed with water, and dried to leav...
10.6084/m9.figshare.5104873.v1
null
Aromatic halide
Aromatic alcohol
C1=CNc2ccccc2N1
C1=CNc2ccccc2N1
C1=CNc2ccccc2N1
Other
O
105
null
O=c1[nH]c2cc(F)c(F)c([N+](=O)[O-])c2[nH]c1=O.[OH-]>O>O=c1[nH]c2cc(F)c(O)c([N+](=O)[O-])c2[nH]c1=O
ord_dataset-c2ad1656a3ca4d08888ffb6e3f3a2742
ord-624cebb798804d829738a81171efb650
Cc1cc(N)c(N)cc1C.O=C(O)C(=O)O>>Cc1cc2[nH]c(=O)c(=O)[nH]c2cc1C
CC1=CC(=C(C=C1C)N)N.C(C(=O)O)(=O)O>>CC=1C=C2NC(C(NC2=CC1C)=O)=O
[CH3:1][c:2]1[cH:3][c:4]([NH2:5])[c:11]([NH2:10])[cH:12][c:13]1[CH3:14].O[C:6](=[O:7])[C:8](O)=[O:9]>>[CH3:1][c:2]1[cH:3][c:4]2[nH:5][c:6](=[O:7])[c:8](=[O:9])[nH:10][c:11]2[cH:12][c:13]1[CH3:14]
Cc1cc(N)c(N)cc1C.O=C(O)C(=O)O
Cc1cc2[nH]c(=O)c(=O)[nH]c2cc1C
null
null
Cl.O
Aromatic Heterocycle Formation
OtherReaction
c86e58e5de9d81a144b6b41f680eb7659186c7868f08e5aac1617724bf77eb2d
7638e82fa21608897e39fce0230ec3ea8d25eb3dc2c5eca945d0fbdce3af493b
O=c1[nH]c2ccccc2[nH]c1=O
O-[C;H0;D3;+0:1](=[O;D1;H0:2])-[C;H0;D3;+0:3](-O)=[O;D1;H0:4].[NH2;D1;+0:5]-[c:6](:[c:7]):[c:8](-[NH2;D1;+0:9]):[c:10]>>[O;D1;H0:2]=[c;H0;D3;+0:1]1:[nH;D2;+0:9]:[c:8](:[c:10]):[c:6](:[c:7]):[nH;D2;+0:5]:[c;H0;D3;+0:3]:1=[O;D1;H0:4]
938.5
[{"value": 94.0, "product": "CC=1C=C2NC(C(NC2=CC1C)=O)=O", "details": "PERCENTYIELD", "is_desired": false}, {"value": 938.5, "product": "CC=1C=C2NC(C(NC2=CC1C)=O)=O", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
null
null
A mixture of 2.72 g (2.0 mmol) of 4,5-dimethyl-1,2-phenylenediamine and 1.92 g (21.3 mmol) of oxalic acid in 30 mL of 2N HCl was refluxed for 2.5 h and cooled to room temperature. The mixture was diluted with 20 mL of H2O, filtered, washed with water, and dried to leave a pale-brown solid 3.57 g (94%); mp>250° C.; 1H N...
10.6084/m9.figshare.5104873.v1
null
Carboxylic acid.Carboxylic acid.Primary amine.Primary amine
null
c1ccccc1
C1=CNc2ccccc2N1
C1=CNc2ccccc2N1
HO-
Cl.O
null
null
Cc1cc(N)c(N)cc1C.O=C(O)C(=O)O>Cl.O>Cc1cc2[nH]c(=O)c(=O)[nH]c2cc1C
ord_dataset-c2ad1656a3ca4d08888ffb6e3f3a2742
ord-b9209e1cd3964563a3a61efb57e33278
Cc1cc2[nH]c(=O)c(=O)[nH]c2cc1C.O=[N+]([O-])O>>Cc1cc2[nH]c(=O)c(=O)[nH]c2c([N+](=O)[O-])c1C
CC=1C=C2NC(C(NC2=CC1C)=O)=O.[N+](=O)(O)[O-]>>CC=1C(=C2NC(C(NC2=CC1C)=O)=O)[N+](=O)[O-]
[CH3:1][c:2]1[cH:3][c:4]2[nH:5][c:6](=[O:7])[c:8](=[O:9])[nH:10][c:11]2[cH:12][c:16]1[CH3:17].O[N+:13](=[O:14])[O-:15]>>[CH3:1][c:2]1[cH:3][c:4]2[nH:5][c:6](=[O:7])[c:8](=[O:9])[nH:10][c:11]2[c:12]([N+:13](=[O:14])[O-:15])[c:16]1[CH3:17]
Cc1cc2[nH]c(=O)c(=O)[nH]c2cc1C.O=[N+]([O-])O
Cc1cc2[nH]c(=O)c(=O)[nH]c2c([N+](=O)[O-])c1C
null
null
OS(=O)(=O)O
Functional Group Addition
Aromatic nitration with HNO3
f306af00a66ff7115c5c95beb4c7becbc44efd79c2b514bddcddde59dc0f2d08
ddce49825c02b8965f10c8d99e3c841d26e1f136da6037b417c09313e6d73097
O=c1[nH]c2ccccc2[nH]c1=O
O-[N+;H0;D3:1](-[O;-;D1;H0:2])=[O;D1;H0:3].[C;D1;H3:4]-[c:5]1:[c:6]:[c:7]:[c:8]2:[#7;a:9]:[c:10]:[c:11]:[#7;a:12]:[c:13]:2:[cH;D2;+0:14]:1>>[C;D1;H3:4]-[c:5]1:[c:6]:[c:7]:[c:8]2:[#7;a:9]:[c:10]:[c:11]:[#7;a:12]:[c:13]:2:[c;H0;D3;+0:14]:1-[N+;H0;D3:1](-[O;-;D1;H0:2])=[O;D1;H0:3]
60
[{"value": 60.0, "product": "CC=1C(=C2NC(C(NC2=CC1C)=O)=O)[N+](=O)[O-]", "details": "PERCENTYIELD", "is_desired": false}]
null
null
48
HOUR
To a solution of 1.90 g (10.0 mmol) of 6,7-dimethyl-1,4-dihydroquinoxaline-2,3-dione in 25 mL of H2SO4 (97%) kept in an ice bath was added dropwise 1.2 mL of HNO3 (69-70%) and the solution was stirred at room temperature for 48 h. It was poured into 300 mL of ice-water and stirred for 10 min. The mixture was filtered, ...
10.6084/m9.figshare.5104873.v1
null
Nitrate
Nitro group
C1=CNc2ccccc2N1
C1=CNc2ccccc2N1
C1=CNc2ccccc2N1
HO-
OS(=O)(=O)O
null
48
Cc1cc2[nH]c(=O)c(=O)[nH]c2cc1C.O=[N+]([O-])O>OS(=O)(=O)O>Cc1cc2[nH]c(=O)c(=O)[nH]c2c([N+](=O)[O-])c1C
ord_dataset-c2ad1656a3ca4d08888ffb6e3f3a2742
ord-3a7276f51d6f4504a3428b3e11e65497
CCc1cc(Br)cc(N)c1N.O=C(O)C(=O)O>>CCc1cc(Br)cc2[nH]c(=O)c(=O)[nH]c12
NC1=C(C=C(C=C1CC)Br)N.O.O.C(C(=O)O)(=O)O>>BrC1=CC(=C2NC(C(NC2=C1)=O)=O)CC
[CH3:1][CH2:2][c:3]1[cH:4][c:5]([Br:6])[cH:7][c:8]([NH2:9])[c:15]1[NH2:14].O=[C:12]([C:10](O)=[O:11])[OH:13]>>[CH3:1][CH2:2][c:3]1[cH:4][c:5]([Br:6])[cH:7][c:8]2[nH:9][c:10](=[O:11])[c:12](=[O:13])[nH:14][c:15]12
CCc1cc(Br)cc(N)c1N.O=C(O)C(=O)O
CCc1cc(Br)cc2[nH]c(=O)c(=O)[nH]c12
null
null
Cl.[OH-].[Na+]
Aromatic Heterocycle Formation
OtherReaction
c86e58e5de9d81a144b6b41f680eb7659186c7868f08e5aac1617724bf77eb2d
7638e82fa21608897e39fce0230ec3ea8d25eb3dc2c5eca945d0fbdce3af493b
O=c1[nH]c2ccccc2[nH]c1=O
O-[C;H0;D3;+0:1](=[O;D1;H0:2])-[C;H0;D3;+0:3](=O)-[OH;D1;+0:4].[NH2;D1;+0:5]-[c:6](:[c:7]):[c:8](-[NH2;D1;+0:9]):[c:10]>>[O;D1;H0:2]=[c;H0;D3;+0:1]1:[nH;D2;+0:9]:[c:8](:[c:10]):[c:6](:[c:7]):[nH;D2;+0:5]:[c;H0;D3;+0:3]:1=[O;H0;D1;+0:4]
31.9
[{"value": 31.9, "product": "BrC1=CC(=C2NC(C(NC2=C1)=O)=O)CC", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
null
null
A mixture of 1,2-diamino-4-bromo-6-ethylbenzene (40 mg, 0.14 mmol) and oxalic acid dihydrate (25 mg, 0.20 mmol, used as received) in 4N HCl (1.5 mL) was refluxed at 120°-5° C. for 3 h, then cooled to room temperature. The mixture was centrifuged and the liquid layer was removed. The yellow solid was washed with cold wa...
10.6084/m9.figshare.5104873.v1
null
Carboxylic acid.Carboxylic acid.Primary amine.Primary amine
null
c1ccccc1
C1=CNc2ccccc2N1
C1=CNc2ccccc2N1
HO-
Cl.[OH-].[Na+]
null
null
CCc1cc(Br)cc(N)c1N.O=C(O)C(=O)O>Cl.[OH-].[Na+]>CCc1cc(Br)cc2[nH]c(=O)c(=O)[nH]c12
ord_dataset-c2ad1656a3ca4d08888ffb6e3f3a2742
ord-101ba999a0e442b7a1ebad51b3339ed1
Cc1cc(C)c(N)c([N+](=O)[O-])c1>>Cc1cc(N)c(N)cc1C
CC1=CC(=C(N)C(=C1)C)[N+](=O)[O-].C(C)O>>NC1=C(C=C(C(=C1)C)C)N
O=[N+:5]([O-])[c:4]1[cH:3][c:2]([CH3:1])[cH:8][c:9]([CH3:10])[c:6]1[NH2:7]>>[CH3:1][c:2]1[cH:3][c:4]([NH2:5])[c:6]([NH2:7])[cH:8][c:9]1[CH3:10]
Cc1cc(C)c(N)c([N+](=O)[O-])c1
Cc1cc(N)c(N)cc1C
null
[Pd]
null
Functional Group Interconversion
OtherReaction
1613b5fba4e86adb9547d5bf6e370cff331bfa463637841d4b06138778df9f24
10b8579fd1662beac4350d758bc16e1f45ee6ea295ff9572db62110c9e2a77db
c1ccccc1
O=[N+;H0;D3:1](-[O-])-[c:2]1:[c:3]:[c;H0;D3;+0:4](-[C;D1;H3:5]):[cH;D2;+0:6]:[c;H0;D3;+0:7](-[C;D1;H3:8]):[c;H0;D3;+0:9]:1-[N;D1;H2:10]>>[C;D1;H3:8]-[c;H0;D3;+0:7]1:[cH;D2;+0:6]:[c;H0;D3;+0:9](-[N;D1;H2:10]):[c:2](-[NH2;D1;+0:1]):[c:3]:[c;H0;D3;+0:4]:1-[C;D1;H3:5]
96
[{"value": 96.0, "product": "NC1=C(C=C(C(=C1)C)C)N", "details": "PERCENTYIELD", "is_desired": false}]
null
null
2
HOUR
A mixture of 4,6-dimethyl-2-nitroaniline (1.66 g, 10.0 mmole) and 10% Pd/C (200 mg) in ethanol (35 mL) was hydrogenated for 2 h at room temperature under 25 psi H2. The catalyst was removed by filtration with celite and the solvent was removed by rota-evaporation to give 1.300 g (96%) of 1,2-diamino-4,5-dimethylbenzene...
10.6084/m9.figshare.5104873.v1
null
Nitro group
Primary amine
c1ccccc1
c1ccccc1
c1ccccc1
Other
[Pd]
null
2
Cc1cc(C)c(N)c([N+](=O)[O-])c1>[Pd]>Cc1cc(N)c(N)cc1C
ord_dataset-c2ad1656a3ca4d08888ffb6e3f3a2742
ord-43fa774a4335414e86153f409864b47c
Cc1cc(C)c(N)c(N)c1.O=C(O)C(=O)O>>Cc1cc(C)c2[nH]c(=O)c(=O)[nH]c2c1
NC1=C(C=C(C=C1C)C)N.O.O.C(C(=O)O)(=O)O>>CC1=C2NC(C(NC2=CC(=C1)C)=O)=O
[CH3:1][c:2]1[cH:3][c:4]([CH3:5])[c:6]([NH2:7])[c:13]([NH2:12])[cH:14]1.O=[C:10]([C:8](O)=[O:9])[OH:11]>>[CH3:1][c:2]1[cH:3][c:4]([CH3:5])[c:6]2[nH:7][c:8](=[O:9])[c:10](=[O:11])[nH:12][c:13]2[cH:14]1
Cc1cc(C)c(N)c(N)c1.O=C(O)C(=O)O
Cc1cc(C)c2[nH]c(=O)c(=O)[nH]c2c1
null
null
Cl
Aromatic Heterocycle Formation
OtherReaction
c86e58e5de9d81a144b6b41f680eb7659186c7868f08e5aac1617724bf77eb2d
7638e82fa21608897e39fce0230ec3ea8d25eb3dc2c5eca945d0fbdce3af493b
O=c1[nH]c2ccccc2[nH]c1=O
O-[C;H0;D3;+0:1](=[O;D1;H0:2])-[C;H0;D3;+0:3](=O)-[OH;D1;+0:4].[NH2;D1;+0:5]-[c:6](:[c:7]):[c:8](-[NH2;D1;+0:9]):[c:10]>>[O;D1;H0:2]=[c;H0;D3;+0:1]1:[nH;D2;+0:9]:[c:8](:[c:10]):[c:6](:[c:7]):[nH;D2;+0:5]:[c;H0;D3;+0:3]:1=[O;H0;D1;+0:4]
87.2
[{"value": 87.0, "product": "CC1=C2NC(C(NC2=CC(=C1)C)=O)=O", "details": "PERCENTYIELD", "is_desired": false}, {"value": 87.2, "product": "CC1=C2NC(C(NC2=CC(=C1)C)=O)=O", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
null
null
A mixture of 1,2-diamino-4,6-dimethylbenzene (424 mg, 3.11 mmole) and oxalic acid dihydrate (432 mg, 3.43 mmole, used as received) in 4N HCl (20 mL) was refluxed at 120°-5° C. for 3 h, then cooled to room temperature. The mixture was centrifuged and the supernatant was removed. The yellow solid was washed with cold wat...
10.6084/m9.figshare.5104873.v1
null
Carboxylic acid.Carboxylic acid.Primary amine.Primary amine
null
c1ccccc1
C1=CNc2ccccc2N1
C1=CNc2ccccc2N1
HO-
Cl
null
null
Cc1cc(C)c(N)c(N)c1.O=C(O)C(=O)O>Cl>Cc1cc(C)c2[nH]c(=O)c(=O)[nH]c2c1
ord_dataset-c2ad1656a3ca4d08888ffb6e3f3a2742
ord-63aacc9beb9f47a3a479f15e7d73ef6a
Nc1cc2ccccc2cc1N.O=C(O)C(=O)O>>O=c1[nH]c2cc3ccccc3cc2[nH]c1=O
C1=C(C(=CC2=CC=CC=C12)N)N.C(C(=O)O)(=O)O>>N1C(C(NC=2C=C3C(=CC12)C=CC=C3)=O)=O
[NH2:3][c:4]1[cH:5][c:6]2[cH:7][cH:8][cH:9][cH:10][c:11]2[cH:12][c:13]1[NH2:14].O[C:2](=[O:1])[C:15](O)=[O:16]>>[O:1]=[c:2]1[nH:3][c:4]2[cH:5][c:6]3[cH:7][cH:8][cH:9][cH:10][c:11]3[cH:12][c:13]2[nH:14][c:15]1=[O:16]
Nc1cc2ccccc2cc1N.O=C(O)C(=O)O
O=c1[nH]c2cc3ccccc3cc2[nH]c1=O
null
null
Cl
Aromatic Heterocycle Formation
OtherReaction
f1fe36c6b10ba58e3cd86b5b0cd5c869c8ba039404150d34422ea91f8af3fc56
7638e82fa21608897e39fce0230ec3ea8d25eb3dc2c5eca945d0fbdce3af493b
O=c1[nH]c2cc3ccccc3cc2[nH]c1=O
O-[C;H0;D3;+0:1](=[O;D1;H0:2])-[C;H0;D3;+0:3](-O)=[O;D1;H0:4].[NH2;D1;+0:5]-[c:6](:[c:7]):[c:8](-[NH2;D1;+0:9]):[c:10]>>[O;D1;H0:2]=[c;H0;D3;+0:1]1:[nH;D2;+0:5]:[c:6](:[c:7]):[c:8](:[c:10]):[nH;D2;+0:9]:[c;H0;D3;+0:3]:1=[O;D1;H0:4]
99.3
[{"value": 99.0, "product": "N1C(C(NC=2C=C3C(=CC12)C=CC=C3)=O)=O", "details": "PERCENTYIELD", "is_desired": false}, {"value": 99.3, "product": "N1C(C(NC=2C=C3C(=CC12)C=CC=C3)=O)=O", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
null
null
A mixture of 603 mg (3.81 mmol) of 2,3-naphthalenediamine and 382 mg (4.24 mmol) of oxalic acid in 5 mL of 2N HCl was refluxed for 3 h and cooled to room temperature. The mixture was filtered, washed with water, and dried to leave a brown solid 803 mg (99%); mp>250° C.; 1H NMR (DMSO-d6), 7.382 (dd, 2, J=3.16, 6.17), 7....
10.6084/m9.figshare.5104873.v1
null
Carboxylic acid.Carboxylic acid.Primary amine.Primary amine
null
c1ccc2ccccc2c1
C1=CNc2cc3ccccc3cc2N1
C1=CNc2cc3ccccc3cc2N1
HO-
Cl
null
null
Nc1cc2ccccc2cc1N.O=C(O)C(=O)O>Cl>O=c1[nH]c2cc3ccccc3cc2[nH]c1=O
ord_dataset-c2ad1656a3ca4d08888ffb6e3f3a2742
ord-b25ce42331c840ea8602ce53d0963993
Cc1cccc(N)c1N.O=C(O)C(=O)O>>Cc1cccc2[nH]c(=O)c(=O)[nH]c12
[OH-].[Na+].NC1=C(C=CC=C1N)C.Cl.O.O.C(C(=O)O)(=O)O.Cl>>CC1=C2NC(C(NC2=CC=C1)=O)=O
[CH3:1][c:2]1[cH:3][cH:4][cH:5][c:6]([NH2:7])[c:13]1[NH2:12].O=[C:8]([OH:9])[C:10](O)=[O:11]>>[CH3:1][c:2]1[cH:3][cH:4][cH:5][c:6]2[nH:7][c:8](=[O:9])[c:10](=[O:11])[nH:12][c:13]12
Cc1cccc(N)c1N.O=C(O)C(=O)O
Cc1cccc2[nH]c(=O)c(=O)[nH]c12
null
null
null
Aromatic Heterocycle Formation
OtherReaction
c86e58e5de9d81a144b6b41f680eb7659186c7868f08e5aac1617724bf77eb2d
7638e82fa21608897e39fce0230ec3ea8d25eb3dc2c5eca945d0fbdce3af493b
O=c1[nH]c2ccccc2[nH]c1=O
O-[C;H0;D3;+0:1](=[O;D1;H0:2])-[C;H0;D3;+0:3](=O)-[OH;D1;+0:4].[NH2;D1;+0:5]-[c:6](:[c:7]):[c:8](-[NH2;D1;+0:9]):[c:10]>>[O;D1;H0:2]=[c;H0;D3;+0:1]1:[nH;D2;+0:5]:[c:6](:[c:7]):[c:8](:[c:10]):[nH;D2;+0:9]:[c;H0;D3;+0:3]:1=[O;H0;D1;+0:4]
768.5
[{"value": 64.0, "product": "CC1=C2NC(C(NC2=CC=C1)=O)=O", "details": "PERCENTYIELD", "is_desired": false}, {"value": 768.5, "product": "CC1=C2NC(C(NC2=CC=C1)=O)=O", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
25
CELSIUS
null
null
To a stirred solution of 2,3-diaminotoluene (0.498 g, 0.407 mmol, Aldrich) in 2N HCl (6 mL, 12 mmol), oxalic acid dihydrate (0.520 g, 0.412 mmol, Fisher) was added in one portion. The resulting deep purple solution was refluxed for 13 h, to give a purple suspension. This was cooled to 25° C., filtered, washed with wate...
10.6084/m9.figshare.5104873.v1
null
Carboxylic acid.Carboxylic acid.Primary amine.Primary amine
null
c1ccccc1
C1=CNc2ccccc2N1
C1=CNc2ccccc2N1
HO-
null
25
null
Cc1cccc(N)c1N.O=C(O)C(=O)O>>Cc1cccc2[nH]c(=O)c(=O)[nH]c12
ord_dataset-c2ad1656a3ca4d08888ffb6e3f3a2742
ord-12fa4b7545e24913ba70142a23da9b9f
Cc1ccc(N)c(N)c1.O=C(O)C(=O)O>>Cc1ccc2[nH]c(=O)c(=O)[nH]c2c1
[OH-].[Na+].NC=1C=C(C=CC1N)C.Cl.O.O.C(C(=O)O)(=O)O.Cl>>CC=1C=C2NC(C(NC2=CC1)=O)=O
[CH3:1][c:2]1[cH:3][cH:4][c:5]([NH2:6])[c:12]([NH2:11])[cH:13]1.O[C:7](=[O:8])[C:9](O)=[O:10]>>[CH3:1][c:2]1[cH:3][cH:4][c:5]2[nH:6][c:7](=[O:8])[c:9](=[O:10])[nH:11][c:12]2[cH:13]1
Cc1ccc(N)c(N)c1.O=C(O)C(=O)O
Cc1ccc2[nH]c(=O)c(=O)[nH]c2c1
null
null
null
Aromatic Heterocycle Formation
OtherReaction
c86e58e5de9d81a144b6b41f680eb7659186c7868f08e5aac1617724bf77eb2d
7638e82fa21608897e39fce0230ec3ea8d25eb3dc2c5eca945d0fbdce3af493b
O=c1[nH]c2ccccc2[nH]c1=O
O-[C;H0;D3;+0:1](=[O;D1;H0:2])-[C;H0;D3;+0:3](-O)=[O;D1;H0:4].[NH2;D1;+0:5]-[c:6](:[c:7]):[c:8](-[NH2;D1;+0:9]):[c:10]>>[O;D1;H0:4]=[c;H0;D3;+0:3]1:[nH;D2;+0:5]:[c:6](:[c:7]):[c:8](:[c:10]):[nH;D2;+0:9]:[c;H0;D3;+0:1]:1=[O;D1;H0:2]
518.2
[{"value": 43.0, "product": "CC=1C=C2NC(C(NC2=CC1)=O)=O", "details": "PERCENTYIELD", "is_desired": false}, {"value": 518.2, "product": "CC=1C=C2NC(C(NC2=CC1)=O)=O", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
25
CELSIUS
null
null
To a stirred solution of 3,4-diaminotoluene (0.302 g, 0.247 mmol, Aldrich) in 2N HCl (4 mL, 8 mmol), oxalic acid dihydrate (0.330 g, 0.261 mmol, Fisher) was added in one portion. The resulting deep purple solution was refluxed for 13 h, to give a purple suspension. This was cooled to 25° C., filtered, washed with water...
10.6084/m9.figshare.5104873.v1
null
Carboxylic acid.Carboxylic acid.Primary amine.Primary amine
null
c1ccccc1
C1=CNc2ccccc2N1
C1=CNc2ccccc2N1
HO-
null
25
null
Cc1ccc(N)c(N)c1.O=C(O)C(=O)O>>Cc1ccc2[nH]c(=O)c(=O)[nH]c2c1
ord_dataset-c2ad1656a3ca4d08888ffb6e3f3a2742
ord-cb4d580f1a1646c0b4045ba962cee035
Cc1cc([N+](=O)[O-])c(N)c([N+](=O)[O-])c1>>Cc1cc(N)c(N)c([N+](=O)[O-])c1
CC1=CC(=C(N)C(=C1)[N+](=O)[O-])[N+](=O)[O-]>>CC=1C=C(C(=C(C1)N)N)[N+](=O)[O-]
O=[N+:5]([O-])[c:4]1[cH:3][c:2]([CH3:1])[cH:12][c:8]([N+:9](=[O:10])[O-:11])[c:6]1[NH2:7]>>[CH3:1][c:2]1[cH:3][c:4]([NH2:5])[c:6]([NH2:7])[c:8]([N+:9](=[O:10])[O-:11])[cH:12]1
Cc1cc([N+](=O)[O-])c(N)c([N+](=O)[O-])c1
Cc1cc(N)c(N)c([N+](=O)[O-])c1
null
null
O.C(C)O
Functional Group Interconversion
Reduction of nitro groups to amines
5c1ea979989295c14f1f65f49e58974d5c524451abca65fc2e6cec44e3d0784f
10b8579fd1662beac4350d758bc16e1f45ee6ea295ff9572db62110c9e2a77db
c1ccccc1
O=[N+;H0;D3:1](-[O-])-[c:2](:[c:3]):[c:4]>>[NH2;D1;+0:1]-[c:2](:[c:3]):[c:4]
85
[{"value": 85.0, "product": "CC=1C=C(C(=C(C1)N)N)[N+](=O)[O-]", "details": "PERCENTYIELD", "is_desired": false}, {"value": 76.8, "product": "CC=1C=C(C(=C(C1)N)N)[N+](=O)[O-]", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
28
CELSIUS
null
null
The procedure of Gillespie et al., J. Org. Chem. 25:942 (1960) was adopted as follows. A dark black solution of 4-methyl-2,6-dinitroaniline (0.100 g, 0.561 mmol, Aldrich, used as received) in 6.66% aq. (NH4)2S (3.3 mL, prepared from 20% aq.(NH4)2S solution supplied by Aldrich) and ethanol (3.5 mL) was refluxed for 45 m...
10.6084/m9.figshare.5104873.v1
null
Nitro group
Primary amine
null
null
c1ccccc1
Other
O.C(C)O
28
null
Cc1cc([N+](=O)[O-])c(N)c([N+](=O)[O-])c1>O.C(C)O>Cc1cc(N)c(N)c([N+](=O)[O-])c1
ord_dataset-c2ad1656a3ca4d08888ffb6e3f3a2742
ord-c070473595ab44adbb5b496789489738
Cc1cc(F)ccc1F>>Cc1cc(F)c([N+](=O)[O-])cc1F
FC1=C(C=C(C=C1)F)C.[N+](=O)([O-])[O-].[K+]>>FC1=C(C=C(C(=C1)[N+](=O)[O-])F)C
[CH3:1][c:2]1[cH:3][c:4]([F:5])[cH:6][cH:10][c:11]1[F:12]>>[CH3:1][c:2]1[cH:3][c:4]([F:5])[c:6]([N+:7](=[O:8])[O-:9])[cH:10][c:11]1[F:12]
Cc1cc(F)ccc1F
Cc1cc(F)c([N+](=O)[O-])cc1F
null
null
OS(=O)(=O)O
Functional Group Addition
OtherReaction
6862453966ade01f48ad6e78fdee5c31f5f3bef2a50d1592f73a35f3caf6154f
22f3183026a2d99c91ec0c53f0059a15c8421016bd62c8ab45281362b96dc686
c1ccccc1
[F;D1;H0:1]-[c:2](:[c:3]):[cH;D2;+0:4]:[c:5]:[c:6]>>[F;D1;H0:1]-[c:2](:[c:3]):[c;H0;D3;+0:4](-[#7;+:7](-[O;-;D1;H0:8])=[O;D1;H0:9]):[c:5]:[c:6]
91
[{"value": 91.0, "product": "FC1=C(C=C(C(=C1)[N+](=O)[O-])F)C", "details": "PERCENTYIELD", "is_desired": false}, {"value": 75.4, "product": "FC1=C(C=C(C(=C1)[N+](=O)[O-])F)C", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
28
CELSIUS
8
HOUR
To a stirred solution of 2,5-difluorotoluene (0.544 g, 4.25 mmol, Aldrich, used as received) in conc. H2SO4 (5.0 mL) at 0° C., KNO3 (0.430 g, 4.25 mmol) was added in one portion. The resulting pale yellow solution was warmed to 28° C. and stirred at that temperature overnight. It was then poured into ice (25 g) and ext...
10.6084/m9.figshare.5104873.v1
null
null
Nitro group
c1ccccc1
c1ccccc1
c1ccccc1
Other
OS(=O)(=O)O
28
8
Cc1cc(F)ccc1F>OS(=O)(=O)O>Cc1cc(F)c([N+](=O)[O-])cc1F
ord_dataset-c2ad1656a3ca4d08888ffb6e3f3a2742
ord-b1c07f4bc15f4967bc2ba5f088db89a5
Cc1cc(F)c([N+](=O)[O-])cc1F.NCC(=O)[O-]>>Cc1cc(NCC(=O)[O-])c([N+](=O)[O-])cc1F
FC1=C(C=C(C(=C1)[N+](=O)[O-])F)C.NCC(=O)[O-].[Na+]>>[Na+].FC1=CC(=C(C=C1C)NCC(=O)[O-])[N+](=O)[O-]
F[c:4]1[cH:3][c:2]([CH3:1])[c:15]([F:16])[cH:14][c:10]1[N+:11](=[O:12])[O-:13].[NH2:5][CH2:6][C:7](=[O:8])[O-:9]>>[CH3:1][c:2]1[cH:3][c:4]([NH:5][CH2:6][C:7](=[O:8])[O-:9])[c:10]([N+:11](=[O:12])[O-:13])[cH:14][c:15]1[F:16]
Cc1cc(F)c([N+](=O)[O-])cc1F.NCC(=O)[O-]
Cc1cc(NCC(=O)[O-])c([N+](=O)[O-])cc1F
null
null
O.CN(C)C=O
Heteroatom Alkylation and Arylation
Buchwald-Hartwig/Ullmann-Goldberg/N-arylation primary amine
da9dae6a655c4bd18887b692f91621e77027436294d6e1fc7be7295afb364796
71a04ae650defc5edd86a92f43c304e981a05f07ff76248da8d4155f3905a29d
c1ccccc1
F-[c;H0;D3;+0:1](:[c:2]:[c:3]):[c:4](-[#7;+:5]):[c:6].[NH2;D1;+0:7]-[C:8]-[C:9](-[O;-;D1;H0:10])=[O;D1;H0:11]>>[#7;+:5]-[c:4](:[c:6]):[c;H0;D3;+0:1](-[NH;D2;+0:7]-[C:8]-[C:9](-[O;-;D1;H0:10])=[O;D1;H0:11]):[c:2]:[c:3]
null
[]
28
CELSIUS
8
HOUR
To a stirred solution of 2,5-difluoro-4-nitrotoluene (0.550 g. 3.18 mmol) in DMF (5.0 mL) was added dropwise a solution of sodium glycinate (0.308 g, 3.18 mmol, Aldrich, used as received) in water (1.0 mL). The resulting suspension was stirred at 28° C. overnight. The solid was filtered and dried under vacuum to give 0...
10.6084/m9.figshare.5104873.v1
null
Aromatic halide.Primary amine
Secondary amine
c1ccccc1
c1ccccc1
c1ccccc1
HF
O.CN(C)C=O
28
8
Cc1cc(F)c([N+](=O)[O-])cc1F.NCC(=O)[O-]>O.CN(C)C=O>Cc1cc(NCC(=O)[O-])c([N+](=O)[O-])cc1F
ord_dataset-c2ad1656a3ca4d08888ffb6e3f3a2742
ord-12229507d5aa4380966ce63e12a8945b
Cc1cc(NCC(=O)[O-])c([N+](=O)[O-])cc1F>>Cc1cc2c(cc1F)NC(=O)CN2
[Na+].FC1=CC(=C(C=C1C)NCC(=O)[O-])[N+](=O)[O-].O.O.[Sn](Cl)Cl>>FC1=C(C=C2NCC(NC2=C1)=O)C
O=[N+:9]([O-])[c:5]1[c:4]([NH:13][CH2:12][C:10]([O-])=[O:11])[cH:3][c:2]([CH3:1])[c:7]([F:8])[cH:6]1>>[CH3:1][c:2]1[cH:3][c:4]2[c:5]([cH:6][c:7]1[F:8])[NH:9][C:10](=[O:11])[CH2:12][NH:13]2
Cc1cc(NCC(=O)[O-])c([N+](=O)[O-])cc1F
Cc1cc2c(cc1F)NC(=O)CN2
null
null
C(C)O
Functional Group Interconversion
OtherReaction
183261da32373f3dc4dd237e8a75ee7d967e6598ba6a325e2c313518785e8076
013ea010a5fc8551154a976160b11b17bb85fae400bd37b37532ea17a3df22d8
O=C1CNc2ccccc2N1
O=[N+;H0;D3:1](-[O-])-[c:2](:[c:3]):[c:4]-[#7:5]-[C:6]-[C;H0;D3;+0:7](-[O-])=[O;D1;H0:8]>>[O;D1;H0:8]=[C;H0;D3;+0:7]1-[C:6]-[#7:5]-[c:4]:[c:2](:[c:3])-[NH;D2;+0:1]-1
32.4
[{"value": 32.4, "product": "FC1=C(C=C2NCC(NC2=C1)=O)C", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
null
null
A mixture of N-(4-fluoro-5-methyl-2-nitrophenyl)glycine sodium salt (0.125 g, 0.548 mmol) and tin (II) chloride dihydrate (0.370 g, 1.64 mmol, Aldrich, used as received) in ethanol (3.0 mL) was refluxed for 30 min. It was then cooled to room temperature and the solvent was removed under vacuum. The residue was diluted ...
10.6084/m9.figshare.5104873.v1
null
Nitro group
Secondary amide
null
c1ccc2c(c1)NCCN2
c1ccc2c(c1)NCCN2
Other
C(C)O
null
null
Cc1cc(NCC(=O)[O-])c([N+](=O)[O-])cc1F>C(C)O>Cc1cc2c(cc1F)NC(=O)CN2
ord_dataset-c2ad1656a3ca4d08888ffb6e3f3a2742
ord-b037678c36524cf9b3abf748abca8e64
N#Cc1c(Cl)c([N+](=O)[O-])cc2[nH]c(=O)c(=O)[nH]c12>>N#Cc1c(Cl)c(N)cc2[nH]c(=O)c(=O)[nH]c12
ClC=1C(=C2NC(C(NC2=CC1[N+](=O)[O-])=O)=O)C#N.O.O.[Sn](Cl)Cl>>NC1=C(C(=C2NC(C(NC2=C1)=O)=O)C#N)Cl
O=[N+:7]([O-])[c:6]1[c:4]([Cl:5])[c:3]([C:2]#[N:1])[c:16]2[c:9]([cH:8]1)[nH:10][c:11](=[O:12])[c:13](=[O:14])[nH:15]2>>[N:1]#[C:2][c:3]1[c:4]([Cl:5])[c:6]([NH2:7])[cH:8][c:9]2[nH:10][c:11](=[O:12])[c:13](=[O:14])[nH:15][c:16]12
N#Cc1c(Cl)c([N+](=O)[O-])cc2[nH]c(=O)c(=O)[nH]c12
N#Cc1c(Cl)c(N)cc2[nH]c(=O)c(=O)[nH]c12
null
null
C(C)O
Reduction
Reduction of nitro groups to amines
bbc242b150a51e69d3ad1caaa391f4422710431b398dcb880555f476706790be
7b0317532ea57a4fcedc1efc3e3c22eb5238d1c8330da53d4f9801fc2391f567
O=c1[nH]c2ccccc2[nH]c1=O
O=[N+;H0;D3:1](-[O-])-[c:2](:[c:3]):[c:4]:[c:5]:[#7;a:6]>>[#7;a:6]:[c:5]:[c:4]:[c:2](-[NH2;D1;+0:1]):[c:3]
88
[{"value": 88.0, "product": "NC1=C(C(=C2NC(C(NC2=C1)=O)=O)C#N)Cl", "details": "PERCENTYIELD", "is_desired": false}, {"value": 86.7, "product": "NC1=C(C(=C2NC(C(NC2=C1)=O)=O)C#N)Cl", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
null
null
A suspension of 6-chloro-5-cyano-7-nitroquinoxaline-2(1H),3(4H)-dione (0.100 g, 0.38 mmol, as prepared above) and tin (II) chloride dihydrate (0.508 g, 2.25 mmol, Aldrich) in ethanol (4.0 mL) was refluxed for 24 h. The resulting suspension was then cooled to room temperature and the yellow solid was filtered, washed wi...
10.6084/m9.figshare.5104873.v1
null
Nitro group
Primary amine
null
null
C1=CNc2ccccc2N1
Other
C(C)O
null
null
N#Cc1c(Cl)c([N+](=O)[O-])cc2[nH]c(=O)c(=O)[nH]c12>C(C)O>N#Cc1c(Cl)c(N)cc2[nH]c(=O)c(=O)[nH]c12
ord_dataset-c2ad1656a3ca4d08888ffb6e3f3a2742
ord-1a433fa6d1f2405e8e1c8446180bc673
Cl.N#Cc1c(Cl)c(N)cc2[nH]c(=O)c(=O)[nH]c12>>N#Cc1c(Cl)c(Cl)cc2[nH]c(=O)c(=O)[nH]c12
NC1=C(C(=C2NC(C(NC2=C1)=O)=O)C#N)Cl.N(=O)[O-].[Na+].Cl.Cl.N#N>>C(#N)C1=C2NC(C(NC2=CC(=C1Cl)Cl)=O)=O
[ClH:7].N[c:6]1[c:4]([Cl:5])[c:3]([C:2]#[N:1])[c:16]2[c:9]([cH:8]1)[nH:10][c:11](=[O:12])[c:13](=[O:14])[nH:15]2>>[N:1]#[C:2][c:3]1[c:4]([Cl:5])[c:6]([Cl:7])[cH:8][c:9]2[nH:10][c:11](=[O:12])[c:13](=[O:14])[nH:15][c:16]12
Cl.N#Cc1c(Cl)c(N)cc2[nH]c(=O)c(=O)[nH]c12
N#Cc1c(Cl)c(Cl)cc2[nH]c(=O)c(=O)[nH]c12
null
Cl[Cu]
O
Miscellaneous
OtherReaction
023dfe963532b1779b3f5c5b05a8c601e35822f2a486d4ab398d090042dccad7
1129c10513c603d2647e51dd9713063aaf10bd8a364ed275b9b93c32624e3ba4
O=c1[nH]c2ccccc2[nH]c1=O
N-[c;H0;D3;+0:1]1:[c:2]:[c:3]2:[#7;a:4]:[c:5]:[c:6]:[#7;a:7]:[c:8]:2:[c:9]:[c:10]:1-[Cl;D1;H0:11].[ClH;D0;+0:12]>>[Cl;D1;H0:11]-[c:10]1:[c:9]:[c:8]2:[#7;a:7]:[c:6]:[c:5]:[#7;a:4]:[c:3]:2:[c:2]:[c;H0;D3;+0:1]:1-[Cl;H0;D1;+0:12]
77
[{"value": 77.0, "product": "C(#N)C1=C2NC(C(NC2=CC(=C1Cl)Cl)=O)=O", "details": "PERCENTYIELD", "is_desired": false}]
null
null
2
HOUR
To a stirred solution of 7-amino-6-chloro-5-cyanoquinoxaline-2(1H),3(4H)-dione (0.035 g, 0.15 mmol, as prepared above) in concentrated HCl (1.5 mL) at 0° C., an aqueous solution of NaNO2 (0.060 g, 0.87 mmol) in water (0.20 mL) was added and the resulting turbid solution was stirred in an ice bath for 2 h. A solution of...
10.6084/m9.figshare.5104873.v1
null
Primary amine
Aromatic halide
C1=CNc2ccccc2N1
C1=CNc2ccccc2N1
C1=CNc2ccccc2N1
Other
Cl[Cu].O
null
2
Cl.N#Cc1c(Cl)c(N)cc2[nH]c(=O)c(=O)[nH]c12>Cl[Cu].O>N#Cc1c(Cl)c(Cl)cc2[nH]c(=O)c(=O)[nH]c12
ord_dataset-c2ad1656a3ca4d08888ffb6e3f3a2742
ord-bdab480f98884bfcb8fb5bb903a163a5
C[O-].O=c1[nH]c2cc(Cl)c(F)c([N+](=O)[O-])c2[nH]c1=O>>COc1c(Cl)cc2[nH]c(=O)c(=O)[nH]c2c1[N+](=O)[O-]
ClC1=C(C(=C2NC(C(NC2=C1)=O)=O)[N+](=O)[O-])F.C[O-].[Na+]>>ClC1=C(C(=C2NC(C(NC2=C1)=O)=O)[N+](=O)[O-])OC
[CH3:1][O-:2].F[c:3]1[c:4]([Cl:5])[cH:6][c:7]2[nH:8][c:9](=[O:10])[c:11](=[O:12])[nH:13][c:14]2[c:15]1[N+:16](=[O:17])[O-:18]>>[CH3:1][O:2][c:3]1[c:4]([Cl:5])[cH:6][c:7]2[nH:8][c:9](=[O:10])[c:11](=[O:12])[nH:13][c:14]2[c:15]1[N+:16](=[O:17])[O-:18]
C[O-].O=c1[nH]c2cc(Cl)c(F)c([N+](=O)[O-])c2[nH]c1=O
COc1c(Cl)cc2[nH]c(=O)c(=O)[nH]c2c1[N+](=O)[O-]
null
Cl
O.CS(=O)C
Heteroatom Alkylation and Arylation
OtherReaction
8f5da7fe2bfdb6898cabd699e332b74d553c190b8b21b1599bb1f70cc864c524
51fd03eb6a688046e417b9ed09ea0e72062396d005af1318b9b5f376a97da959
O=c1[nH]c2ccccc2[nH]c1=O
F-[c;H0;D3;+0:1]1:[c:2](-[#7;+:3]):[c:4]2:[#7;a:5]:[c:6]:[c:7]:[#7;a:8]:[c:9]:2:[c:10]:[c:11]:1-[Cl;D1;H0:12].[C;D1;H3:13]-[O-;H0;D1:14]>>[#7;+:3]-[c:2]1:[c:4]2:[#7;a:5]:[c:6]:[c:7]:[#7;a:8]:[c:9]:2:[c:10]:[c:11](-[Cl;D1;H0:12]):[c;H0;D3;+0:1]:1-[O;H0;D2;+0:14]-[C;D1;H3:13]
null
[]
null
null
8
HOUR
To a stirred solution of 7-Chloro-6-fluoro-5-nitroquinoxaline-2(1H),3(4H)-dione (0.100 g, 0.385 mmol, as prepared above) in DMSO (1.0 mL) at room temperature, sodium methoxide (0.125 g, 2.31 mmol, Mallinckrodt) was added in one portion. The resulting dark red solution was stirred overnight at room temperature. It was t...
10.6084/m9.figshare.5104873.v1
null
Aromatic halide
Ether
C1=CNc2ccccc2N1
C1=CNc2ccccc2N1
C1=CNc2ccccc2N1
Other
Cl.O.CS(=O)C
null
8
C[O-].O=c1[nH]c2cc(Cl)c(F)c([N+](=O)[O-])c2[nH]c1=O>Cl.O.CS(=O)C>COc1c(Cl)cc2[nH]c(=O)c(=O)[nH]c2c1[N+](=O)[O-]
ord_dataset-c2ad1656a3ca4d08888ffb6e3f3a2742
ord-b8d301c6f54d46f7a3a3c206fb56c3c7
CCc1ccc([N+](=O)[O-])cc1CC.CCc1cccc([N+](=O)[O-])c1CC>>CCc1ccc(N)cc1CC.CCc1cccc(N)c1CC
C(C)C1=C(C=C(C=C1)[N+](=O)[O-])CC.C(C)C1=C(C(=CC=C1)[N+](=O)[O-])CC>>C(C)C=1C=C(N)C=CC1CC.C(C)C1=C(N)C=CC=C1CC
O=[N+:7]([O-])[c:6]1[cH:5][cH:4][c:3]([CH2:2][CH3:1])[c:9]([CH2:10][CH3:11])[cH:8]1.O=[N+:19]([O-])[c:18]1[cH:17][cH:16][cH:15][c:14]([CH2:13][CH3:12])[c:20]1[CH2:21][CH3:22]>>[CH3:1][CH2:2][c:3]1[cH:4][cH:5][c:6]([NH2:7])[cH:8][c:9]1[CH2:10][CH3:11].[CH3:12][CH2:13][c:14]1[cH:15][cH:16][cH:17][c:18]([NH2:19])[c:20]1[C...
CCc1ccc([N+](=O)[O-])cc1CC.CCc1cccc([N+](=O)[O-])c1CC
CCc1ccc(N)cc1CC.CCc1cccc(N)c1CC
null
null
C(C)(=O)OCC
Functional Group Interconversion
OtherReaction
f469aaae1e88945b257afa41cebe21597b9a3f326d9f2ab1d5670c64dd831541
86e032c8ebc9cbcd13a880d0d66c541ff63611af16d12657aad958d17abf4587
c1ccccc1.c1ccccc1
O=[N+;H0;D3:1](-[O-])-[c:2](:[c:3]):[c:4].O=[N+;H0;D3:5](-[O-])-[c:6](:[c:7]):[c:8]>>[NH2;D1;+0:1]-[c:2](:[c:3]):[c:4].[NH2;D1;+0:5]-[c:6](:[c:7]):[c:8]
71
[{"value": 71.0, "product": "C(C)C=1C=C(N)C=CC1CC", "details": "PERCENTYIELD", "is_desired": false}, {"value": 19.0, "product": "C(C)C1=C(N)C=CC=C1CC", "details": "PERCENTYIELD", "is_desired": false}]
null
null
10
HOUR
A mixture of 1,2-diethyl-4-nitrobenzene (16) and 1,2-diethyl-3-nitrobenzene (17) (1.4 g, 7.82 mmol) was dissolved in ethyl acetate (20 mL). To this solution was added 10% Pd--C (350 mg, 20%; Aldrich). The mixture was agitated at room temperature under a pressure of 35 psi (H2) for 10 h. The catalyst was removed through...
10.6084/m9.figshare.5104873.v1
null
Nitro group.Nitro group
Primary amine.Primary amine
null
null
c1ccccc1.c1ccccc1
Other
C(C)(=O)OCC
null
10
CCc1ccc([N+](=O)[O-])cc1CC.CCc1cccc([N+](=O)[O-])c1CC>C(C)(=O)OCC>CCc1ccc(N)cc1CC.CCc1cccc(N)c1CC
ord_dataset-c2ad1656a3ca4d08888ffb6e3f3a2742
ord-88a736fe9b214bc981472e81f31e1d7b
CCc1cc(N)c([N+](=O)[O-])cc1CC>>CCc1cc(N)c(N)cc1CC
C(C)C1=CC(=C(N)C=C1CC)[N+](=O)[O-]>>C(C)C1=CC(=C(C=C1CC)N)N
O=[N+:8]([O-])[c:7]1[c:5]([NH2:6])[cH:4][c:3]([CH2:2][CH3:1])[c:10]([CH2:11][CH3:12])[cH:9]1>>[CH3:1][CH2:2][c:3]1[cH:4][c:5]([NH2:6])[c:7]([NH2:8])[cH:9][c:10]1[CH2:11][CH3:12]
CCc1cc(N)c([N+](=O)[O-])cc1CC
CCc1cc(N)c(N)cc1CC
null
null
C(C)(=O)OCC
Reduction
Reduction of nitro groups to amines
bbc242b150a51e69d3ad1caaa391f4422710431b398dcb880555f476706790be
7b0317532ea57a4fcedc1efc3e3c22eb5238d1c8330da53d4f9801fc2391f567
c1ccccc1
O=[N+;H0;D3:1](-[O-])-[c:2](:[c:3]):[c:4]>>[NH2;D1;+0:1]-[c:2](:[c:3]):[c:4]
96
[{"value": 96.0, "product": "C(C)C1=CC(=C(C=C1CC)N)N", "details": "PERCENTYIELD", "is_desired": false}, {"value": 95.7, "product": "C(C)C1=CC(=C(C=C1CC)N)N", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
5
HOUR
4,5-Diethyl-2-nitroaniline (23) (567 mg, 2.92 mmol) was dissolved in ethyl acetate (20 mL). To this solution was added 10% Pd--C (142 mg, 20%; Aldrich). The mixture was agitated at room temperature under a pressure of 35 psi (H2) for 5 h. The catalyst was removed through a column of Celite (5 g) and washed with ethyl a...
10.6084/m9.figshare.5104873.v1
null
Nitro group
Primary amine
null
null
c1ccccc1
Other
C(C)(=O)OCC
null
5
CCc1cc(N)c([N+](=O)[O-])cc1CC>C(C)(=O)OCC>CCc1cc(N)c(N)cc1CC
ord_dataset-c2ad1656a3ca4d08888ffb6e3f3a2742
ord-d5dec3f0abf64b4793c94bbca73a6396
CCc1cc(N)c(N)cc1CC.O=C(O)C(=O)O>>CCc1cc2[nH]c(=O)c(=O)[nH]c2cc1CC
C(C)C1=CC(=C(C=C1CC)N)N.O.O.C(C(=O)O)(=O)O>>C(C)C=1C=C2NC(C(NC2=CC1CC)=O)=O
[CH3:1][CH2:2][c:3]1[cH:4][c:5]([NH2:6])[c:12]([NH2:11])[cH:13][c:14]1[CH2:15][CH3:16].O=[C:9]([C:7](O)=[O:8])[OH:10]>>[CH3:1][CH2:2][c:3]1[cH:4][c:5]2[nH:6][c:7](=[O:8])[c:9](=[O:10])[nH:11][c:12]2[cH:13][c:14]1[CH2:15][CH3:16]
CCc1cc(N)c(N)cc1CC.O=C(O)C(=O)O
CCc1cc2[nH]c(=O)c(=O)[nH]c2cc1CC
null
null
Cl
Aromatic Heterocycle Formation
OtherReaction
c86e58e5de9d81a144b6b41f680eb7659186c7868f08e5aac1617724bf77eb2d
7638e82fa21608897e39fce0230ec3ea8d25eb3dc2c5eca945d0fbdce3af493b
O=c1[nH]c2ccccc2[nH]c1=O
O-[C;H0;D3;+0:1](=[O;D1;H0:2])-[C;H0;D3;+0:3](=O)-[OH;D1;+0:4].[NH2;D1;+0:5]-[c:6](:[c:7]):[c:8](-[NH2;D1;+0:9]):[c:10]>>[O;D1;H0:2]=[c;H0;D3;+0:1]1:[nH;D2;+0:9]:[c:8](:[c:10]):[c:6](:[c:7]):[nH;D2;+0:5]:[c;H0;D3;+0:3]:1=[O;H0;D1;+0:4]
88
[{"value": 88.0, "product": "C(C)C=1C=C2NC(C(NC2=CC1CC)=O)=O", "details": "PERCENTYIELD", "is_desired": false}, {"value": 88.0, "product": "C(C)C=1C=C2NC(C(NC2=CC1CC)=O)=O", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
null
null
4,5-Diethyl-1,2-diaminobenzene 24 (459 mg, 2.80 mmol) was dissolved in 4N hydrochloric acid (12 mL) at 90° C. Oxalic acid dihydrate (983 mg, 6.47 mmoL) was added to this solution in one portion with stirring under N2. The mixture was refluxed at 130°-5° C. (oil bath) for 3 h. A yellow solid precipitated, which was coll...
10.6084/m9.figshare.5104873.v1
null
Carboxylic acid.Carboxylic acid.Primary amine.Primary amine
null
c1ccccc1
C1=CNc2ccccc2N1
C1=CNc2ccccc2N1
HO-
Cl
null
null
CCc1cc(N)c(N)cc1CC.O=C(O)C(=O)O>Cl>CCc1cc2[nH]c(=O)c(=O)[nH]c2cc1CC
ord_dataset-c2ad1656a3ca4d08888ffb6e3f3a2742
ord-aa96ed4539a240bb91e84eed224faea7
CCc1cc2[nH]c(=O)c(=O)[nH]c2cc1CC.O=[N+]([O-])[O-]>>CCc1cc2[nH]c(=O)c(=O)[nH]c2c([N+](=O)[O-])c1CC
C(C)C=1C=C2NC(C(NC2=CC1CC)=O)=O.FC(C(=O)O)(F)F.[N+](=O)([O-])[O-].[K+]>>[N+](=O)([O-])C1=C2NC(C(NC2=CC(=C1CC)CC)=O)=O
[CH3:1][CH2:2][c:3]1[cH:4][c:5]2[nH:6][c:7](=[O:8])[c:9](=[O:10])[nH:11][c:12]2[cH:13][c:17]1[CH2:18][CH3:19].[O-][N+:14](=[O:15])[O-:16]>>[CH3:1][CH2:2][c:3]1[cH:4][c:5]2[nH:6][c:7](=[O:8])[c:9](=[O:10])[nH:11][c:12]2[c:13]([N+:14](=[O:15])[O-:16])[c:17]1[CH2:18][CH3:19]
CCc1cc2[nH]c(=O)c(=O)[nH]c2cc1CC.O=[N+]([O-])[O-]
CCc1cc2[nH]c(=O)c(=O)[nH]c2c([N+](=O)[O-])c1CC
null
null
O
Functional Group Addition
Aromatic nitration with NO3 salt
f306af00a66ff7115c5c95beb4c7becbc44efd79c2b514bddcddde59dc0f2d08
ddce49825c02b8965f10c8d99e3c841d26e1f136da6037b417c09313e6d73097
O=c1[nH]c2ccccc2[nH]c1=O
[C:1]-[c:2]1:[c:3]:[c:4]:[c:5]2:[#7;a:6]:[c:7]:[c:8]:[#7;a:9]:[c:10]:2:[cH;D2;+0:11]:1.[O-]-[N+;H0;D3:12](-[O;-;D1;H0:13])=[O;D1;H0:14]>>[C:1]-[c:2]1:[c:3]:[c:4]:[c:5]2:[#7;a:6]:[c:7]:[c:8]:[#7;a:9]:[c:10]:2:[c;H0;D3;+0:11]:1-[N+;H0;D3:12](-[O;-;D1;H0:13])=[O;D1;H0:14]
69.1
[{"value": 69.0, "product": "[N+](=O)([O-])C1=C2NC(C(NC2=CC(=C1CC)CC)=O)=O", "details": "PERCENTYIELD", "is_desired": false}, {"value": 69.1, "product": "[N+](=O)([O-])C1=C2NC(C(NC2=CC(=C1CC)CC)=O)=O", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
null
null
6,7-Diethyl-2,3-quinoxalinedione 25 (218 mg, 1.0 mmol) was added to trifluoroacetic acid (8 mL; Sigma). To this suspension was added potassium nitrate (121.2 mg, 1.2 mmol; Baker) in one portion with stirring under N2. The reaction was stirred at room temperature for 48 h. Trifluoroacetic acid was evaporated in vacuo to...
10.6084/m9.figshare.5104873.v1
null
Nitrate
Nitro group
C1=CNc2ccccc2N1
C1=CNc2ccccc2N1
C1=CNc2ccccc2N1
HO-
O
null
null
CCc1cc2[nH]c(=O)c(=O)[nH]c2cc1CC.O=[N+]([O-])[O-]>O>CCc1cc2[nH]c(=O)c(=O)[nH]c2c([N+](=O)[O-])c1CC
ord_dataset-c2ad1656a3ca4d08888ffb6e3f3a2742
ord-45212a821f1e4ebfacc57678d2b28b19
CC(=O)OC(C)=O.Nc1ccc2c(c1)CCC2>>CC(=O)Nc1ccc2c(c1)CCC2
NC=1C=C2CCCC2=CC1.C(C)(=O)OC(C)=O>>C(C)(=O)NC=1C=C2CCCC2=CC1
CC(=O)O[C:2]([CH3:1])=[O:3].[NH2:4][c:5]1[cH:6][cH:7][c:8]2[c:9]([cH:10]1)[CH2:11][CH2:12][CH2:13]2>>[CH3:1][C:2](=[O:3])[NH:4][c:5]1[cH:6][cH:7][c:8]2[c:9]([cH:10]1)[CH2:11][CH2:12][CH2:13]2
CC(=O)OC(C)=O.Nc1ccc2c(c1)CCC2
CC(=O)Nc1ccc2c(c1)CCC2
null
null
O1CCOCC1.O
Acylation
Aminolysis of esters
87d35e51b477fc9a658a6f307eb56d84c8879182772c9dd3a42ec0d584fd2684
627cbc0550c9f51ad0105d9fcf46677e8c93bed87ee95bfe69292a82550c95b7
c1ccc2c(c1)CCC2
C-C(=O)-O-[C;H0;D3;+0:1](-[C;D1;H3:2])=[O;D1;H0:3].[NH2;D1;+0:4]-[c:5](:[c:6]):[c:7]>>[C;D1;H3:2]-[C;H0;D3;+0:1](=[O;D1;H0:3])-[NH;D2;+0:4]-[c:5](:[c:6]):[c:7]
91
[{"value": 91.0, "product": "C(C)(=O)NC=1C=C2CCCC2=CC1", "details": "PERCENTYIELD", "is_desired": false}, {"value": 90.9, "product": "C(C)(=O)NC=1C=C2CCCC2=CC1", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
16
HOUR
To a solution of 5.2 g (39 mmol) of 5-aminoindan in 15 mL of dioxane kept in an ice-bath was added dropwise 8 mL (8.6 g, 84 mmol) of acetic anhydride. The solution was stirred at room temperature for 16 h. It was diluted with 70 mL of water. The mixture was filtered, washed with water, and dried to leave a gray solid 6...
10.6084/m9.figshare.5104873.v1
null
Anhydride.Primary amine
Secondary amide
null
null
c1ccc2c(c1)CCC2
HO-
O1CCOCC1.O
null
16
CC(=O)OC(C)=O.Nc1ccc2c(c1)CCC2>O1CCOCC1.O>CC(=O)Nc1ccc2c(c1)CCC2
ord_dataset-c2ad1656a3ca4d08888ffb6e3f3a2742
ord-6422effaf4d74f519eb3d457fcdf3521
CC(=O)Nc1ccc2c(c1)CCC2.O=[N+]([O-])[O-]>>CC(=O)Nc1cc2c(cc1[N+](=O)[O-])CCC2
[N+](=O)([O-])[O-].[K+].C(C)(=O)NC=1C=C2CCCC2=CC1>>C(C)(=O)NC=1C=C2CCCC2=CC1[N+](=O)[O-]
[CH3:1][C:2](=[O:3])[NH:4][c:5]1[cH:6][c:7]2[c:8]([cH:9][cH:10]1)[CH2:14][CH2:15][CH2:16]2.[O-][N+:11](=[O:12])[O-:13]>>[CH3:1][C:2](=[O:3])[NH:4][c:5]1[cH:6][c:7]2[c:8]([cH:9][c:10]1[N+:11](=[O:12])[O-:13])[CH2:14][CH2:15][CH2:16]2
CC(=O)Nc1ccc2c(c1)CCC2.O=[N+]([O-])[O-]
CC(=O)Nc1cc2c(cc1[N+](=O)[O-])CCC2
null
null
OS(=O)(=O)O
Functional Group Addition
Aromatic nitration with NO3 salt
cfd75387f50e1142b60c8213f482ef40b605d13135e71d44588a632fab28010f
ddce49825c02b8965f10c8d99e3c841d26e1f136da6037b417c09313e6d73097
c1ccc2c(c1)CCC2
[C;D1;H3:1]-[C:2](=[O;D1;H0:3])-[#7:4]-[c:5](:[c:6]):[cH;D2;+0:7]:[c:8]:[c:9].[O-]-[N+;H0;D3:10](-[O;-;D1;H0:11])=[O;D1;H0:12]>>[C;D1;H3:1]-[C:2](=[O;D1;H0:3])-[#7:4]-[c:5](:[c:6]):[c;H0;D3;+0:7](-[N+;H0;D3:10](-[O;-;D1;H0:11])=[O;D1;H0:12]):[c:8]:[c:9]
15.1
[{"value": 15.0, "product": "C(C)(=O)NC=1C=C2CCCC2=CC1[N+](=O)[O-]", "details": "PERCENTYIELD", "is_desired": false}, {"value": 15.1, "product": "C(C)(=O)NC=1C=C2CCCC2=CC1[N+](=O)[O-]", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
1
HOUR
To a solution of 5.59 g (31.9 mmol) of 5-acetamidoindan in 55 mL of H2SO4 kept in an ice-bath was added portionwise 3.62 g of KNO3 (35.8 mmol). The solution was stirred in the ice-bath for 2 h and at room temperature overnight. It was added to 500 mL of ice-water and stirred for 1 h. The precipitate was filtered, washe...
10.6084/m9.figshare.5104873.v1
null
Nitrate
Nitro group
c1ccc2c(c1)CCC2
c1ccc2c(c1)CCC2
c1ccc2c(c1)CCC2
HO-
OS(=O)(=O)O
null
1
CC(=O)Nc1ccc2c(c1)CCC2.O=[N+]([O-])[O-]>OS(=O)(=O)O>CC(=O)Nc1cc2c(cc1[N+](=O)[O-])CCC2
ord_dataset-c2ad1656a3ca4d08888ffb6e3f3a2742
ord-c56d610317f54b7aa67c4261f2a9a716
CC(=O)Nc1cc2c(cc1[N+](=O)[O-])CCC2>>Nc1cc2c(cc1[N+](=O)[O-])CCC2
C(C)(=O)NC=1C=C2CCCC2=CC1[N+](=O)[O-]>>NC=1C=C2CCCC2=CC1[N+](=O)[O-]
CC(=O)[NH:1][c:2]1[cH:3][c:4]2[c:5]([cH:6][c:7]1[N+:8](=[O:9])[O-:10])[CH2:11][CH2:12][CH2:13]2>>[NH2:1][c:2]1[cH:3][c:4]2[c:5]([cH:6][c:7]1[N+:8](=[O:9])[O-:10])[CH2:11][CH2:12][CH2:13]2
CC(=O)Nc1cc2c(cc1[N+](=O)[O-])CCC2
Nc1cc2c(cc1[N+](=O)[O-])CCC2
null
null
Cl
Reduction
Hydrogenolysis of amides/imides/carbamates
755df58c254dea764fdda078ffd678ec540bba057c83683be04c253f1270ac7b
025f7cefe51e71668ad5d09fca32df168e9b538347403e4d5c1748073e538adc
c1ccc2c(c1)CCC2
C-C(=O)-[NH;D2;+0:1]-[c:2](:[c:3]):[c:4]>>[NH2;D1;+0:1]-[c:2](:[c:3]):[c:4]
97.2
[{"value": 97.0, "product": "NC=1C=C2CCCC2=CC1[N+](=O)[O-]", "details": "PERCENTYIELD", "is_desired": false}, {"value": 97.2, "product": "NC=1C=C2CCCC2=CC1[N+](=O)[O-]", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
85
CELSIUS
null
null
A mixture of 259 mg (1.16 mmol) of 5-acetamido-6-nitroindan in 4 mL of 2N HCl was heated at 85° C. for 9 h and cooled to room temperature. The solid precipitate was filtered, washed with water, and dried to leave 201 mg (97%) of a crystalline yellow solid. 1H NMR (CDCl3), 2.068 (m, 2), 2.843 (m, 4), 6.00 (sb, 2), 6.650...
10.6084/m9.figshare.5104873.v1
null
Secondary amide
Primary amine
null
null
c1ccc2c(c1)CCC2
HO-
Cl
85
null
CC(=O)Nc1cc2c(cc1[N+](=O)[O-])CCC2>Cl>Nc1cc2c(cc1[N+](=O)[O-])CCC2
ord_dataset-c2ad1656a3ca4d08888ffb6e3f3a2742
ord-a086c150e15a42718188fdd2ed774274
Nc1cc2c(cc1[N+](=O)[O-])CCC2>>Nc1cc2c(cc1N)CCC2
NC=1C=C2CCCC2=CC1[N+](=O)[O-].Cl[Sn]Cl>>NC=1C=C2CCCC2=CC1N
O=[N+:8]([O-])[c:7]1[c:2]([NH2:1])[cH:3][c:4]2[c:5]([cH:6]1)[CH2:9][CH2:10][CH2:11]2>>[NH2:1][c:2]1[cH:3][c:4]2[c:5]([cH:6][c:7]1[NH2:8])[CH2:9][CH2:10][CH2:11]2
Nc1cc2c(cc1[N+](=O)[O-])CCC2
Nc1cc2c(cc1N)CCC2
null
null
C(C)O
Reduction
Reduction of nitro groups to amines
bbc242b150a51e69d3ad1caaa391f4422710431b398dcb880555f476706790be
7b0317532ea57a4fcedc1efc3e3c22eb5238d1c8330da53d4f9801fc2391f567
c1ccc2c(c1)CCC2
O=[N+;H0;D3:1](-[O-])-[c:2](:[c:3]):[c:4]>>[NH2;D1;+0:1]-[c:2](:[c:3]):[c:4]
97.6
[{"value": 97.0, "product": "NC=1C=C2CCCC2=CC1N", "details": "PERCENTYIELD", "is_desired": false}, {"value": 97.6, "product": "NC=1C=C2CCCC2=CC1N", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
null
null
A solution of 200 mg (1.12 mmol) of 5-amino-6-nitroindan and 1.14 g (6.01 mmol) of SnCl2 in 8 mL of ethanol was heated at 70° C. for 2 h. It was evaporated to remove the ethanol. The residue was treated with 40% aqueous NaOH to pH=12. The mixture was diluted with 4 mL of water and extracted with CHCl3 (3×10 mL). The ex...
10.6084/m9.figshare.5104873.v1
null
Nitro group
Primary amine
null
null
c1ccc2c(c1)CCC2
Other
C(C)O
null
null
Nc1cc2c(cc1[N+](=O)[O-])CCC2>C(C)O>Nc1cc2c(cc1N)CCC2
ord_dataset-c2ad1656a3ca4d08888ffb6e3f3a2742
ord-1f41145c35d14389a62208c891c594b4
CCc1ccc([N+](=O)[O-])cc1Cl>>CCc1ccc(N)cc1Cl
ClC=1C=C(C=CC1CC)[N+](=O)[O-].O.O.Cl[Sn]Cl>>ClC=1C=C(N)C=CC1CC
O=[N+:7]([O-])[c:6]1[cH:5][cH:4][c:3]([CH2:2][CH3:1])[c:9]([Cl:10])[cH:8]1>>[CH3:1][CH2:2][c:3]1[cH:4][cH:5][c:6]([NH2:7])[cH:8][c:9]1[Cl:10]
CCc1ccc([N+](=O)[O-])cc1Cl
CCc1ccc(N)cc1Cl
null
null
null
Reduction
Reduction of nitro groups to amines
bbc242b150a51e69d3ad1caaa391f4422710431b398dcb880555f476706790be
7b0317532ea57a4fcedc1efc3e3c22eb5238d1c8330da53d4f9801fc2391f567
c1ccccc1
O=[N+;H0;D3:1](-[O-])-[c:2](:[c:3]):[c:4]>>[NH2;D1;+0:1]-[c:2](:[c:3]):[c:4]
98
[{"value": 98.0, "product": "ClC=1C=C(N)C=CC1CC", "details": "PERCENTYIELD", "is_desired": false}, {"value": 97.9, "product": "ClC=1C=C(N)C=CC1CC", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
null
null
A solution of 8.9 g (48 mmol) of 31 and 54.6 g (241 mmol) of SnCl2.2H2O in 100 mL of absolute alcohol was refluxed for 1 h. It was evaporated to remove most of the solvent and the residue was treated with 2N NaOH to pH=9. The mixture was filtered and the solid was washed with methanol (10 mL) and ethyl acetate (200 mL)...
10.6084/m9.figshare.5104873.v1
null
Nitro group
Primary amine
null
null
c1ccccc1
Other
null
null
null
CCc1ccc([N+](=O)[O-])cc1Cl>>CCc1ccc(N)cc1Cl
ord_dataset-c2ad1656a3ca4d08888ffb6e3f3a2742
ord-7dce83d20adb454489999b231737edc2
CCc1cc2c(cc1Cl)NCC(=O)N2.O=[N+]([O-])O.O=c1[nH]c2cc3c(cc2[nH]c1=O)OCO3>>CCc1cc2[nH]c(=O)c(=O)[nH]c2c([N+](=O)[O-])c1Cl
C1OC=2C=C3NC(C(NC3=CC2O1)=O)=O.C1OC=2C=C3NC(C(NC3=CC2O1)=O)=O.C(C)C1=C(N)C=CC=C1CC.[N+](=O)(O)[O-].ClC=1C=C2NCC(NC2=CC1CC)=O>>ClC=1C(=C2NC(C(NC2=CC1CC)=O)=O)[N+](=O)[O-]
[CH3:1][CH2:2][c:3]1[cH:4][c:5]2[c:12]([cH:13][c:17]1[Cl:18])[NH:11][CH2:9][C:7](=[O:8])[NH:6]2.O[N+:14](=[O:15])[O-:16].O=c1[nH]c2cc3c(cc2[nH]c1=[O:10])OCO3>>[CH3:1][CH2:2][c:3]1[cH:4][c:5]2[nH:6][c:7](=[O:8])[c:9](=[O:10])[nH:11][c:12]2[c:13]([N+:14](=[O:15])[O-:16])[c:17]1[Cl:18]
CCc1cc2c(cc1Cl)NCC(=O)N2.O=[N+]([O-])O.O=c1[nH]c2cc3c(cc2[nH]c1=O)OCO3
CCc1cc2[nH]c(=O)c(=O)[nH]c2c([N+](=O)[O-])c1Cl
null
null
C(F)(F)(F)C(=O)O
Protection
OtherReaction
668f49ce01915eb3f34d13ad94594d109e41c1b3034302953862f472217f0d55
a459b17178d2549680121fc0f4a13d6f42b44a6ec99534453738493ce17d41a2
O=c1[nH]c2ccccc2[nH]c1=O
O-[N+;H0;D3:1](-[O;-;D1;H0:2])=[O;D1;H0:3].O=c1:[nH]:c2:c:c3:c(:c:c:2:[nH]:c:1=[O;H0;D1;+0:4])-O-C-O-3.[Cl;D1;H0:5]-[c:6]1:[c:7]:[c:8]:[c:9]2:[c:10](:[cH;D2;+0:11]:1)-[NH;D2;+0:12]-[CH2;D2;+0:13]-[C;H0;D3;+0:14](=[O;D1;H0:15])-[NH;D2;+0:16]-2>>[Cl;D1;H0:5]-[c:6]1:[c:7]:[c:8]:[c:9]2:[nH;D2;+0:16]:[c;H0;D3;+0:14](=[O;D1;...
null
[]
null
null
10
MINUTE
To a solution of 137 mg (0.65 mmol) of 36 in 4 mL of CF3CO2H kept in an ice bath was added dropwise 0.4 mL of fuming HNO3. The solution was stirred in the ice bath for 1 h and at room temperature overnight. It was evaporated and the residue was treated with 6 mL of water and stirred for 10 min. The mixture was filtered...
10.6084/m9.figshare.5104873.v1
null
Ether.Ether.Nitrate.Secondary amide.Secondary amine
Nitro group
c1ccc2c(c1)NCCN2.C1=CNc2cc3c(cc2N1)OCO3
C1=CNc2ccccc2N1
C1=CNc2ccccc2N1
HO-
C(F)(F)(F)C(=O)O
null
0.166667
CCc1cc2c(cc1Cl)NCC(=O)N2.O=[N+]([O-])O.O=c1[nH]c2cc3c(cc2[nH]c1=O)OCO3>C(F)(F)(F)C(=O)O>CCc1cc2[nH]c(=O)c(=O)[nH]c2c([N+](=O)[O-])c1Cl
ord_dataset-c2ad1656a3ca4d08888ffb6e3f3a2742
ord-7be7b329106841c5a1cdf0b795ef6837
CCc1cc([N+](=O)[O-])c(N)cc1Cl>>CCc1cc(N)c(N)cc1Cl
ClC=1C=C(N)C(=CC1CC)[N+](=O)[O-].O.O.Cl[Sn]Cl>>NC1=C(C=C(C(=C1)CC)Cl)N
O=[N+:6]([O-])[c:5]1[cH:4][c:3]([CH2:2][CH3:1])[c:10]([Cl:11])[cH:9][c:7]1[NH2:8]>>[CH3:1][CH2:2][c:3]1[cH:4][c:5]([NH2:6])[c:7]([NH2:8])[cH:9][c:10]1[Cl:11]
CCc1cc([N+](=O)[O-])c(N)cc1Cl
CCc1cc(N)c(N)cc1Cl
null
null
null
Reduction
Reduction of nitro groups to amines
bbc242b150a51e69d3ad1caaa391f4422710431b398dcb880555f476706790be
7b0317532ea57a4fcedc1efc3e3c22eb5238d1c8330da53d4f9801fc2391f567
c1ccccc1
O=[N+;H0;D3:1](-[O-])-[c:2](:[c:3]):[c:4]>>[NH2;D1;+0:1]-[c:2](:[c:3]):[c:4]
99.4
[{"value": 99.0, "product": "NC1=C(C=C(C(=C1)CC)Cl)N", "details": "PERCENTYIELD", "is_desired": false}, {"value": 99.4, "product": "NC1=C(C=C(C(=C1)CC)Cl)N", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
null
null
A solution of 271 mg (1.35 mmol) of 34 and 1.24 g (5.49 mmol) of SnCl2.2H2O, in 5 mL of absolute alcohol was refluxed for 2 h. It was evaporated and the residue was treated with 1N NaOH to pH=10. The mixture was extracted with CH2Cl2 (3×10 mL). The extract was dried (MgSO4) and evaporated to leave 229 mg (99%) of a yel...
10.6084/m9.figshare.5104873.v1
null
Nitro group
Primary amine
null
null
c1ccccc1
Other
null
null
null
CCc1cc([N+](=O)[O-])c(N)cc1Cl>>CCc1cc(N)c(N)cc1Cl
ord_dataset-c2ad1656a3ca4d08888ffb6e3f3a2742
ord-65de9c754ef24117815da28fff8b8ea2
CCc1cc(N)c(N)cc1Cl.O=C(O)C(=O)O>>CCc1cc2[nH]c(=O)c(=O)[nH]c2cc1Cl
NC1=C(C=C(C(=C1)CC)Cl)N.C(C(=O)O)(=O)O.Cl>>ClC=1C=C2NC(C(NC2=CC1CC)=O)=O
[CH3:1][CH2:2][c:3]1[cH:4][c:5]([NH2:6])[c:12]([NH2:11])[cH:13][c:14]1[Cl:15].O[C:7](=[O:8])[C:9](O)=[O:10]>>[CH3:1][CH2:2][c:3]1[cH:4][c:5]2[nH:6][c:7](=[O:8])[c:9](=[O:10])[nH:11][c:12]2[cH:13][c:14]1[Cl:15]
CCc1cc(N)c(N)cc1Cl.O=C(O)C(=O)O
CCc1cc2[nH]c(=O)c(=O)[nH]c2cc1Cl
null
null
null
Aromatic Heterocycle Formation
OtherReaction
c86e58e5de9d81a144b6b41f680eb7659186c7868f08e5aac1617724bf77eb2d
7638e82fa21608897e39fce0230ec3ea8d25eb3dc2c5eca945d0fbdce3af493b
O=c1[nH]c2ccccc2[nH]c1=O
O-[C;H0;D3;+0:1](=[O;D1;H0:2])-[C;H0;D3;+0:3](-O)=[O;D1;H0:4].[NH2;D1;+0:5]-[c:6](:[c:7]):[c:8](-[NH2;D1;+0:9]):[c:10]>>[O;D1;H0:4]=[c;H0;D3;+0:3]1:[nH;D2;+0:5]:[c:6](:[c:7]):[c:8](:[c:10]):[nH;D2;+0:9]:[c;H0;D3;+0:1]:1=[O;D1;H0:2]
92
[{"value": 92.0, "product": "ClC=1C=C2NC(C(NC2=CC1CC)=O)=O", "details": "PERCENTYIELD", "is_desired": false}, {"value": 92.0, "product": "ClC=1C=C2NC(C(NC2=CC1CC)=O)=O", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
null
null
A mixture of 228 mg (1.33 mmol) of 38 and 124 mg (1.38 mmol) of oxalic acid in 4 mL of aqueous 2N HCl was refluxed for 4 h. It was cooled to room temperature, filtered, and dried to leave 275 mg (92%) of a brown solid; mp>400° C.; 1H NMR (DMSO-d6), 1.134 (t, 3, J=7.4), 2.635 (q, 2, J=7.4), 7.026 (s, 1), 7.107 (s, 1), 1...
10.6084/m9.figshare.5104873.v1
null
Carboxylic acid.Carboxylic acid.Primary amine.Primary amine
null
c1ccccc1
C1=CNc2ccccc2N1
C1=CNc2ccccc2N1
HO-
null
null
null
CCc1cc(N)c(N)cc1Cl.O=C(O)C(=O)O>>CCc1cc2[nH]c(=O)c(=O)[nH]c2cc1Cl
ord_dataset-c2ad1656a3ca4d08888ffb6e3f3a2742
ord-824e083e88e1451d809db0bda97f1706
COc1cc2c(cc1OC)=NC(=O)C(=O)N=2>>O=C1N=c2cc(O)c(O)cc2=NC1=O
Cl.B(Br)(Br)Br.[OH-].[Na+].COC1=CC2=NC(C(N=C2C=C1OC)=O)=O>>OC1=CC2=NC(C(N=C2C=C1O)=O)=O
C[O:7][c:6]1[cH:5][c:4]2[c:11]([cH:10][c:8]1[O:9]C)=[N:12][C:13](=[O:14])[C:2](=[O:1])[N:3]=2>>[O:1]=[C:2]1[N:3]=[c:4]2[cH:5][c:6]([OH:7])[c:8]([OH:9])[cH:10][c:11]2=[N:12][C:13]1=[O:14]
COc1cc2c(cc1OC)=NC(=O)C(=O)N=2
O=C1N=c2cc(O)c(O)cc2=NC1=O
null
null
C(Cl)Cl
Deprotection
OtherReaction
a0f05885bbc65ae2846cad0ac34029941211b2ef3a426958b0c8aa83bb16fe86
9df751cd682ad9d54ed75d7313aaead6a019c5d37ede15c4672866d319b900ff
O=C1N=c2ccccc2=NC1=O
C-[O;H0;D2;+0:1]-[c:2](:[c:3]):[c:4](-[O;H0;D2;+0:5]-C):[c:6]>>[OH;D1;+0:1]-[c:2](:[c:3]):[c:4](-[OH;D1;+0:5]):[c:6]
88.5
[{"value": 88.0, "product": "OC1=CC2=NC(C(N=C2C=C1O)=O)=O", "details": "PERCENTYIELD", "is_desired": false}, {"value": 88.5, "product": "OC1=CC2=NC(C(N=C2C=C1O)=O)=O", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
24
HOUR
To a suspension of 6,7-dimethoxy-2,3-quinoxalinedione (45) (222 mg, 1.0 mmol) in 2 mL of methylene dichloride was added 5 mL of a solution of boron tribromide in methylene dichloride (1M, Aldrich). The resulting mixture was stirred at room temperature for 24 hr. The mixture was then poured into ice-water (10 g) to form...
10.6084/m9.figshare.5104873.v1
null
Ether.Ether
Aromatic alcohol.Aromatic alcohol
null
null
c1ccc2c(c1)=NCCN=2
Other
C(Cl)Cl
null
24
COc1cc2c(cc1OC)=NC(=O)C(=O)N=2>C(Cl)Cl>O=C1N=c2cc(O)c(O)cc2=NC1=O
ord_dataset-c2ad1656a3ca4d08888ffb6e3f3a2742
ord-965407359eb34b6c9c540882c628652f
CC(=O)O.COc1cc2c(cc1OC)=NC(=O)C(=O)N=2>>COc1cc2c(c(OC(C)=O)c1OC)=NC(=O)C(=O)N=2
COC1=CC2=NC(C(N=C2C=C1OC)=O)=O.C(C)(=O)O.[N+](=O)(O)[O-]>>C(C)(=O)OC=1C2=NC(C(N=C2C=C(C1OC)OC)=O)=O
[OH:8][C:9]([CH3:10])=[O:11].[CH3:1][O:2][c:3]1[cH:4][c:5]2[c:6]([cH:7][c:12]1[O:13][CH3:14])=[N:15][C:16](=[O:17])[C:18](=[O:19])[N:20]=2>>[CH3:1][O:2][c:3]1[cH:4][c:5]2[c:6]([c:7]([O:8][C:9]([CH3:10])=[O:11])[c:12]1[O:13][CH3:14])=[N:15][C:16](=[O:17])[C:18](=[O:19])[N:20]=2
CC(=O)O.COc1cc2c(cc1OC)=NC(=O)C(=O)N=2
COc1cc2c(c(OC(C)=O)c1OC)=NC(=O)C(=O)N=2
null
null
null
Heteroatom Alkylation and Arylation
OtherReaction
d165d1f90abcf4cf4c04ce8b0f0f275eeebb9a3a990c7710c17dc6ce017987f3
badd4f82161bb0ee7acffd023ea4caae5d036bce7065c10ab0a06e83a6a6f119
O=C1N=c2ccccc2=NC1=O
[#8:1]-[c:2](:[c:3]):[cH;D2;+0:4]:[c:5]1:[c:6]=[#7:7]-[C:8](=[O;D1;H0:9])-[C:10](=[O;D1;H0:11])-[#7:12]=1.[C;D1;H3:13]-[C:14](=[O;D1;H0:15])-[OH;D1;+0:16]>>[#8:1]-[c:2](:[c:3]):[c;H0;D3;+0:4](-[O;H0;D2;+0:16]-[C:14](-[C;D1;H3:13])=[O;D1;H0:15]):[c:5]1:[c:6]=[#7:7]-[C:8](=[O;D1;H0:9])-[C:10](=[O;D1;H0:11])-[#7:12]=1
54
[{"value": 54.0, "product": "C(C)(=O)OC=1C2=NC(C(N=C2C=C(C1OC)OC)=O)=O", "details": "PERCENTYIELD", "is_desired": false}]
null
null
24
HOUR
6,7-Dimethoxy-2,3-quinoxalinedione (45) (222 mg, 1.0 mmol) was dissolved in glacial acetic acid (10 mL) at 100° C. (oil bath). The oil bath was removed and fuming nitric acid (53 μL, 1.2 mmol; Baker) was added dropwise to the solution. The reaction mixture was then stirred at room temperature for 24 h. The mixture was ...
10.6084/m9.figshare.5104873.v1
null
Carboxylic acid
Ester
c1ccc2c(c1)=NCCN=2
c1ccc2c(c1)=NCCN=2
c1ccc2c(c1)=NCCN=2
null
null
null
24
CC(=O)O.COc1cc2c(cc1OC)=NC(=O)C(=O)N=2>>COc1cc2c(c(OC(C)=O)c1OC)=NC(=O)C(=O)N=2
ord_dataset-c2ad1656a3ca4d08888ffb6e3f3a2742
ord-d3fd1de3a9bf4946b30dced194907e14
COc1cc2c(c(OC(C)=O)c1OC)=NC(=O)C(=O)N=2>>COc1cc2c(c(O)c1OC)=NC(=O)C(=O)N=2
C(C)(=O)OC=1C2=NC(C(N=C2C=C(C1OC)OC)=O)=O.[OH-].[Na+].Cl>>OC=1C2=NC(C(N=C2C=C(C1OC)OC)=O)=O
CC(=O)[O:8][c:7]1[c:6]2[c:5]([cH:4][c:3]([O:2][CH3:1])[c:9]1[O:10][CH3:11])=[N:17][C:15](=[O:16])[C:13](=[O:14])[N:12]=2>>[CH3:1][O:2][c:3]1[cH:4][c:5]2[c:6]([c:7]([OH:8])[c:9]1[O:10][CH3:11])=[N:12][C:13](=[O:14])[C:15](=[O:16])[N:17]=2
COc1cc2c(c(OC(C)=O)c1OC)=NC(=O)C(=O)N=2
COc1cc2c(c(O)c1OC)=NC(=O)C(=O)N=2
null
null
O
Reduction
Hydrolysis or Hydrogenolysis of Carboxylic Esters or Thioesters
db7d50f1ad65e3456617ab9bc6ab5b9ede0e069a6dd971d117a653e2a40b05de
efe1c37482b229370967d04d1a68db10ee663983a92b84fa0f009f5bb178597f
O=C1N=c2ccccc2=NC1=O
C-C(=O)-[O;H0;D2;+0:1]-[c:2](:[c:3]):[c:4]=[#7:5]>>[#7:5]=[c:4]:[c:2](-[OH;D1;+0:1]):[c:3]
91
[{"value": 86.0, "product": "OC=1C2=NC(C(N=C2C=C(C1OC)OC)=O)=O", "details": "PERCENTYIELD", "is_desired": false}, {"value": 91.0, "product": "OC=1C2=NC(C(N=C2C=C(C1OC)OC)=O)=O", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
null
null
5-Acetyloxy-6,7-dimethoxy-2,3-quinoxalinedione (47) (30 mg, 0.107 mmol) was added to a single-necked 15-mL flask. Sodium hydroxide aqueous solution (2N, 1 mL) was added to the flask under nitrogen with stirring. The solution was then stirred at room temperature for 24 h. The solution was diluted with water (3 mL) and t...
10.6084/m9.figshare.5104873.v1
null
Ester
Aromatic alcohol
null
null
c1ccc2c(c1)=NCCN=2
HO-
O
null
null
COc1cc2c(c(OC(C)=O)c1OC)=NC(=O)C(=O)N=2>O>COc1cc2c(c(O)c1OC)=NC(=O)C(=O)N=2
ord_dataset-c2ad1656a3ca4d08888ffb6e3f3a2742
ord-34c2a14bc7e5483fa0ea763baa2fd8c7
COc1cc2c(c(O)c1OC)=NC(=O)C(=O)N=2>>O=C1N=c2cc(O)c(O)c(O)c2=NC1=O
Cl.[B].[OH-].[Na+].OC=1C2=NC(C(N=C2C=C(C1OC)OC)=O)=O>>OC=1C2=NC(C(N=C2C=C(C1O)O)=O)=O
C[O:7][c:6]1[cH:5][c:4]2[c:12]([c:10]([OH:11])[c:8]1[O:9]C)=[N:13][C:14](=[O:15])[C:2](=[O:1])[N:3]=2>>[O:1]=[C:2]1[N:3]=[c:4]2[cH:5][c:6]([OH:7])[c:8]([OH:9])[c:10]([OH:11])[c:12]2=[N:13][C:14]1=[O:15]
COc1cc2c(c(O)c1OC)=NC(=O)C(=O)N=2
O=C1N=c2cc(O)c(O)c(O)c2=NC1=O
null
null
C(Cl)Cl
Deprotection
OtherReaction
a0f05885bbc65ae2846cad0ac34029941211b2ef3a426958b0c8aa83bb16fe86
9df751cd682ad9d54ed75d7313aaead6a019c5d37ede15c4672866d319b900ff
O=C1N=c2ccccc2=NC1=O
C-[O;H0;D2;+0:1]-[c:2](:[c:3]):[c:4](-[O;H0;D2;+0:5]-C):[c:6]>>[OH;D1;+0:1]-[c:2](:[c:3]):[c:4](-[OH;D1;+0:5]):[c:6]
80.8
[{"value": 80.0, "product": "OC=1C2=NC(C(N=C2C=C(C1O)O)=O)=O", "details": "PERCENTYIELD", "is_desired": false}, {"value": 80.8, "product": "OC=1C2=NC(C(N=C2C=C(C1O)O)=O)=O", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
12
HOUR
To a suspension of 5-hydroxy-6,7-dimethoxy-2,3-quinoxalinedione (48) (50 mg, 0.22 mmol) in 2 mL of methylene dichloride was added 2 mL of a solution of boron tribomide in methylene dichloride (1M, Aldrich). The resulting mixture was stirred at room temperature for 12 hr. The mixture was poured into ice-water (5 g) to f...
10.6084/m9.figshare.5104873.v1
null
Ether.Ether
Aromatic alcohol.Aromatic alcohol
null
null
c1ccc2c(c1)=NCCN=2
Other
C(Cl)Cl
null
12
COc1cc2c(c(O)c1OC)=NC(=O)C(=O)N=2>C(Cl)Cl>O=C1N=c2cc(O)c(O)c(O)c2=NC1=O
ord_dataset-c2ad1656a3ca4d08888ffb6e3f3a2742
ord-f001a64fe8f24ef6a5090cd755cd65c4
COc1cc2c(c(O)c1OC)=NC(=O)C(=O)N=2.O=C(Cl)Cc1ccccc1>>COc1cc2c(c(OC(=O)Cc3ccccc3)c1OC)=NC(=O)C(=O)N=2
C(C)N(CC)CC.C1(=CC=CC=C1)CC(=O)Cl.OC=1C2=NC(C(N=C2C=C(C1OC)OC)=O)=O>>C1(=CC=CC=C1)CC(=O)OC=1C2=NC(C(N=C2C=C(C1OC)OC)=O)=O
[CH3:1][O:2][c:3]1[cH:4][c:5]2[c:6]([c:7]([OH:8])[c:18]1[O:19][CH3:20])=[N:21][C:22](=[O:23])[C:24](=[O:25])[N:26]=2.Cl[C:9](=[O:10])[CH2:11][c:12]1[cH:13][cH:14][cH:15][cH:16][cH:17]1>>[CH3:1][O:2][c:3]1[cH:4][c:5]2[c:6]([c:7]([O:8][C:9](=[O:10])[CH2:11][c:12]3[cH:13][cH:14][cH:15][cH:16][cH:17]3)[c:18]1[O:19][CH3:20]...
COc1cc2c(c(O)c1OC)=NC(=O)C(=O)N=2.O=C(Cl)Cc1ccccc1
COc1cc2c(c(OC(=O)Cc3ccccc3)c1OC)=NC(=O)C(=O)N=2
null
null
C(Cl)Cl
Acylation
Schotten-Baumann to ester
1cda078f55e64d9385e544d1067595d5e7672bbd1eff542e7a341817a2d8c4d5
6439fc27f97ee9ed7c11ef9b5032d9493d05f28a7bbb50d256a2d54d035fbfb2
O=C(Cc1ccccc1)Oc1cccc2c1=NC(=O)C(=O)N=2
Cl-[C;H0;D3;+0:1](=[O;D1;H0:2])-[C:3]-[c:4].[#7:5]=[c:6]:[c:7](-[OH;D1;+0:8]):[c:9]>>[#7:5]=[c:6]:[c:7](-[O;H0;D2;+0:8]-[C;H0;D3;+0:1](=[O;D1;H0:2])-[C:3]-[c:4]):[c:9]
77
[{"value": 77.0, "product": "C1(=CC=CC=C1)CC(=O)OC=1C2=NC(C(N=C2C=C(C1OC)OC)=O)=O", "details": "PERCENTYIELD", "is_desired": false}, {"value": 77.0, "product": "C1(=CC=CC=C1)CC(=O)OC=1C2=NC(C(N=C2C=C(C1OC)OC)=O)=O", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
12
HOUR
To a suspension of 5-hydroxy-6,7-dimethoxy-2,3-quinoxalinedione (48) (50 mg, 0.22 mmol) in 3 mL of methylene dichloride was added 0.14 mL of triethylamine and phenylacetyl chloride (77.5 mg, 0.5 mmol, Aldrich) at 0° C. The resulting mixture was stirred at room temperature for 12 hr. The reaction mixture was then poured...
10.6084/m9.figshare.5104873.v1
null
Acyl halide.Aromatic alcohol
Ester
null
null
c1ccccc1.c1ccc2c(c1)=NCCN=2
HCl
C(Cl)Cl
null
12
COc1cc2c(c(O)c1OC)=NC(=O)C(=O)N=2.O=C(Cl)Cc1ccccc1>C(Cl)Cl>COc1cc2c(c(OC(=O)Cc3ccccc3)c1OC)=NC(=O)C(=O)N=2
ord_dataset-c2ad1656a3ca4d08888ffb6e3f3a2742
ord-e5efc9f8d1154f20a3bdc405582e0e1b
Fc1ccc(F)c(Cl)c1>>O=[N+]([O-])c1cc(F)c(Cl)cc1F
ClC1=C(C=CC(=C1)F)F.[N+](=O)([O-])[O-].[K+]>>ClC1=C(C=C(C(=C1)F)[N+](=O)[O-])F
[cH:4]1[cH:5][c:6]([F:7])[c:8]([Cl:9])[cH:10][c:11]1[F:12]>>[O:1]=[N+:2]([O-:3])[c:4]1[cH:5][c:6]([F:7])[c:8]([Cl:9])[cH:10][c:11]1[F:12]
Fc1ccc(F)c(Cl)c1
O=[N+]([O-])c1cc(F)c(Cl)cc1F
null
null
OS(=O)(=O)O
Functional Group Addition
OtherReaction
6862453966ade01f48ad6e78fdee5c31f5f3bef2a50d1592f73a35f3caf6154f
22f3183026a2d99c91ec0c53f0059a15c8421016bd62c8ab45281362b96dc686
c1ccccc1
[F;D1;H0:1]-[c:2](:[c:3]):[cH;D2;+0:4]:[c:5]:[c:6]>>[F;D1;H0:1]-[c:2](:[c:3]):[c;H0;D3;+0:4](-[#7;+:7](-[O;-;D1;H0:8])=[O;D1;H0:9]):[c:5]:[c:6]
85
[{"value": 85.0, "product": "ClC1=C(C=C(C(=C1)F)[N+](=O)[O-])F", "details": "PERCENTYIELD", "is_desired": false}, {"value": 84.3, "product": "ClC1=C(C=C(C(=C1)F)[N+](=O)[O-])F", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
8
HOUR
To a stirred solution of 1-chloro-2,5-difluorobenzene (0.770 g, 5.18 mmol) in concd H2SO4 (8.0 mL) at 0° C., KNO3 (0.525 g, 5.19 mmol) was added in one lot. The resulting yellow solution was allowed to warm to room temperature and stirred overnight at room temperature. It was then poured into ice (80 g) and extracted w...
10.6084/m9.figshare.5104873.v1
null
null
Nitro group
c1ccccc1
c1ccccc1
c1ccccc1
Other
OS(=O)(=O)O
null
8
Fc1ccc(F)c(Cl)c1>OS(=O)(=O)O>O=[N+]([O-])c1cc(F)c(Cl)cc1F
ord_dataset-c2ad1656a3ca4d08888ffb6e3f3a2742
ord-6af7050892d54175aa064b56c9f69106
NCC(=O)[O-].O=[N+]([O-])c1cc(F)c(Cl)cc1F>>O=C([O-])CNc1cc(Cl)c(F)cc1[N+](=O)[O-]
ClC1=C(C=C(C(=C1)F)[N+](=O)[O-])F.NCC(=O)[O-].[Na+]>>[Na+].ClC=1C(=CC(=C(C1)NCC(=O)[O-])[N+](=O)[O-])F
[O:1]=[C:2]([O-:3])[CH2:4][NH2:5].F[c:6]1[cH:7][c:8]([Cl:9])[c:10]([F:11])[cH:12][c:13]1[N+:14](=[O:15])[O-:16]>>[O:1]=[C:2]([O-:3])[CH2:4][NH:5][c:6]1[cH:7][c:8]([Cl:9])[c:10]([F:11])[cH:12][c:13]1[N+:14](=[O:15])[O-:16]
NCC(=O)[O-].O=[N+]([O-])c1cc(F)c(Cl)cc1F
O=C([O-])CNc1cc(Cl)c(F)cc1[N+](=O)[O-]
null
null
O.C(C)O
Heteroatom Alkylation and Arylation
Buchwald-Hartwig/Ullmann-Goldberg/N-arylation primary amine
da9dae6a655c4bd18887b692f91621e77027436294d6e1fc7be7295afb364796
71a04ae650defc5edd86a92f43c304e981a05f07ff76248da8d4155f3905a29d
c1ccccc1
F-[c;H0;D3;+0:1](:[c:2]:[c:3]):[c:4](-[#7;+:5]):[c:6].[NH2;D1;+0:7]-[C:8]-[C:9](-[O;-;D1;H0:10])=[O;D1;H0:11]>>[#7;+:5]-[c:4](:[c:6]):[c;H0;D3;+0:1](-[NH;D2;+0:7]-[C:8]-[C:9](-[O;-;D1;H0:10])=[O;D1;H0:11]):[c:2]:[c:3]
64
[{"value": 64.0, "product": "[Na+].ClC=1C(=CC(=C(C1)NCC(=O)[O-])[N+](=O)[O-])F", "details": "PERCENTYIELD", "is_desired": false}, {"value": 58.4, "product": "[Na+].ClC=1C(=CC(=C(C1)NCC(=O)[O-])[N+](=O)[O-])F", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
null
null
To a stirred solution of 1-chloro-2,5-difluoro-4-nitrobenzene (0.825 g, 4.26 mmol) in ethanol (8.0 mL), was added a solution of sodium glycinate (0.415 g, 4.27 mmol) in water (1.5 mL). The resulting suspension was refluxed for 60 h. The solution was cooled to room temperature and the precipitated bright orange solid wa...
10.6084/m9.figshare.5104873.v1
null
Aromatic halide.Primary amine
Secondary amine
c1ccccc1
c1ccccc1
c1ccccc1
HF
O.C(C)O
null
null
NCC(=O)[O-].O=[N+]([O-])c1cc(F)c(Cl)cc1F>O.C(C)O>O=C([O-])CNc1cc(Cl)c(F)cc1[N+](=O)[O-]
ord_dataset-c2ad1656a3ca4d08888ffb6e3f3a2742
ord-453ac216b75e4661a8e649ffaaf4878f
O=C([O-])CNc1cc(Cl)c(F)cc1[N+](=O)[O-]>>O=C1CNc2cc(Cl)c(F)cc2N1
[Na+].ClC=1C(=CC(=C(C1)NCC(=O)[O-])[N+](=O)[O-])F.O.O.[Sn](Cl)Cl>>ClC=1C=C2NCC(NC2=CC1F)=O
O=[N+:13]([O-])[c:12]1[c:5]([NH:4][CH2:3][C:2]([O-])=[O:1])[cH:6][c:7]([Cl:8])[c:9]([F:10])[cH:11]1>>[O:1]=[C:2]1[CH2:3][NH:4][c:5]2[cH:6][c:7]([Cl:8])[c:9]([F:10])[cH:11][c:12]2[NH:13]1
O=C([O-])CNc1cc(Cl)c(F)cc1[N+](=O)[O-]
O=C1CNc2cc(Cl)c(F)cc2N1
null
null
C(C)O
Functional Group Interconversion
OtherReaction
183261da32373f3dc4dd237e8a75ee7d967e6598ba6a325e2c313518785e8076
013ea010a5fc8551154a976160b11b17bb85fae400bd37b37532ea17a3df22d8
O=C1CNc2ccccc2N1
O=[N+;H0;D3:1](-[O-])-[c:2](:[c:3]):[c:4]-[#7:5]-[C:6]-[C;H0;D3;+0:7](-[O-])=[O;D1;H0:8]>>[O;D1;H0:8]=[C;H0;D3;+0:7]1-[C:6]-[#7:5]-[c:4]:[c:2](:[c:3])-[NH;D2;+0:1]-1
59.4
[{"value": 59.0, "product": "ClC=1C=C2NCC(NC2=CC1F)=O", "details": "PERCENTYIELD", "is_desired": false}, {"value": 59.4, "product": "ClC=1C=C2NCC(NC2=CC1F)=O", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
null
null
A suspension of N-(5'-chloro-4'-fluoro-2'-nitrophenyl)glycine sodium salt (0.650 g, 2.61 mmol) and tin (II) chloride dihydrate (1.770 g, 7.845 mmol) in ethanol (10.5 mL) was refluxed for 1 h. It was then cooled to room temperature and ~5 mL ethanol was removed under vacuum. The precipitated solid was collected by filtr...
10.6084/m9.figshare.5104873.v1
null
Nitro group
Secondary amide
null
c1ccc2c(c1)NCCN2
c1ccc2c(c1)NCCN2
Other
C(C)O
null
null
O=C([O-])CNc1cc(Cl)c(F)cc1[N+](=O)[O-]>C(C)O>O=C1CNc2cc(Cl)c(F)cc2N1
ord_dataset-c2ad1656a3ca4d08888ffb6e3f3a2742
ord-542ed5268d7d4c67afd4a6169b794c6b
CC(=O)c1cc(Cl)ccc1Cl>>CCc1cc(Cl)ccc1Cl
ClC1=C(C=C(C=C1)Cl)C(C)=O>>ClC1=C(C=C(C=C1)Cl)CC
O=[C:2]([CH3:1])[c:3]1[cH:4][c:5]([Cl:6])[cH:7][cH:8][c:9]1[Cl:10]>>[CH3:1][CH2:2][c:3]1[cH:4][c:5]([Cl:6])[cH:7][cH:8][c:9]1[Cl:10]
CC(=O)c1cc(Cl)ccc1Cl
CCc1cc(Cl)ccc1Cl
null
[Zn]
Cl.O
Reduction
OtherReaction
bdac4f77103f4da1c5b42ea95e05b0b7b31176b78204db5f4144ffca7b3d54d5
f9ba67182f94acd5fbe41487f8f71e26bccf898b8fc8091ef46f4363de5628d4
c1ccccc1
O=[C;H0;D3;+0:1](-[C;D1;H3:2])-[c:3](:[c:4]):[c:5]>>[C;D1;H3:2]-[CH2;D2;+0:1]-[c:3](:[c:4]):[c:5]
null
[]
null
null
null
null
A suspension of mossy zinc (10 g) and mercuric chloride (0.5 g) in concd HCl (0.5 mL) and water (5 mL) was shaken for ~5 min. The aqueous layer was then decanted. To the residue was added concd HCl (7.5 mL) and water (7.5 mL) followed by 2',5'-dichloroacetophenone (3.106 g, 16.43 mmol) and the suspension was refluxed f...
10.6084/m9.figshare.5104873.v1
null
Ketone
null
null
null
c1ccccc1
Other
[Zn].Cl.O
null
null
CC(=O)c1cc(Cl)ccc1Cl>[Zn].Cl.O>CCc1cc(Cl)ccc1Cl
ord_dataset-c2ad1656a3ca4d08888ffb6e3f3a2742
ord-ba407004792444bbb4dd640a7211cba6
CCc1cc(Cl)ccc1Cl.O=[N+]([O-])[O-]>>CCc1cc(Cl)c([N+](=O)[O-])cc1Cl
ClC1=C(C=C(C=C1)Cl)CC.[N+](=O)([O-])[O-].[K+]>>ClC1=C(C=C(C(=C1)CC)Cl)[N+](=O)[O-]
[CH3:1][CH2:2][c:3]1[cH:4][c:5]([Cl:6])[cH:7][cH:11][c:12]1[Cl:13].[O-][N+:8](=[O:9])[O-:10]>>[CH3:1][CH2:2][c:3]1[cH:4][c:5]([Cl:6])[c:7]([N+:8](=[O:9])[O-:10])[cH:11][c:12]1[Cl:13]
CCc1cc(Cl)ccc1Cl.O=[N+]([O-])[O-]
CCc1cc(Cl)c([N+](=O)[O-])cc1Cl
null
null
OS(=O)(=O)O
Functional Group Addition
Aromatic nitration with NO3 salt
53848b8b2bb4e867226e49db2e60519b24be9379900e3ad7c56af54fe8fde7a5
ddce49825c02b8965f10c8d99e3c841d26e1f136da6037b417c09313e6d73097
c1ccccc1
[Cl;D1;H0:1]-[c:2](:[c:3]):[cH;D2;+0:4]:[c:5]:[c:6].[O-]-[N+;H0;D3:7](-[O;-;D1;H0:8])=[O;D1;H0:9]>>[Cl;D1;H0:1]-[c:2](:[c:3]):[c;H0;D3;+0:4](-[N+;H0;D3:7](-[O;-;D1;H0:8])=[O;D1;H0:9]):[c:5]:[c:6]
92
[{"value": 92.0, "product": "ClC1=C(C=C(C(=C1)CC)Cl)[N+](=O)[O-]", "details": "PERCENTYIELD", "is_desired": false}, {"value": 91.6, "product": "ClC1=C(C=C(C(=C1)CC)Cl)[N+](=O)[O-]", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
8
HOUR
To a stirred solution of 2,5-dichloro-1-ethylbenzene (0.795 g, 4.68 mmol) in concd H2SO4 (4.5 mL) at 0° C., KNO3 (0.473 g, 4.68 mmol) was added in one portion. The resulting pale yellow solution was allowed to warm to room temperature and was stirred overnight at room temperature. It was then poured into ice (80 g) and...
10.6084/m9.figshare.5104873.v1
null
Nitrate
Nitro group
c1ccccc1
c1ccccc1
c1ccccc1
HO-
OS(=O)(=O)O
null
8
CCc1cc(Cl)ccc1Cl.O=[N+]([O-])[O-]>OS(=O)(=O)O>CCc1cc(Cl)c([N+](=O)[O-])cc1Cl
ord_dataset-c2ad1656a3ca4d08888ffb6e3f3a2742
ord-4c819dd84db14c9db991f43604900434
CCc1cc(NCC(=O)[O-])c([N+](=O)[O-])cc1Cl>>CCc1cc2c(cc1Cl)NC(=O)CN2
[Na+].ClC1=CC(=C(C=C1CC)NCC(=O)[O-])[N+](=O)[O-].O.O.[Sn](Cl)Cl>>ClC1=C(C=C2NCC(NC2=C1)=O)CC
O=[N+:10]([O-])[c:6]1[c:5]([NH:14][CH2:13][C:11]([O-])=[O:12])[cH:4][c:3]([CH2:2][CH3:1])[c:8]([Cl:9])[cH:7]1>>[CH3:1][CH2:2][c:3]1[cH:4][c:5]2[c:6]([cH:7][c:8]1[Cl:9])[NH:10][C:11](=[O:12])[CH2:13][NH:14]2
CCc1cc(NCC(=O)[O-])c([N+](=O)[O-])cc1Cl
CCc1cc2c(cc1Cl)NC(=O)CN2
null
null
C(C)O
Functional Group Interconversion
OtherReaction
183261da32373f3dc4dd237e8a75ee7d967e6598ba6a325e2c313518785e8076
013ea010a5fc8551154a976160b11b17bb85fae400bd37b37532ea17a3df22d8
O=C1CNc2ccccc2N1
O=[N+;H0;D3:1](-[O-])-[c:2](:[c:3]):[c:4]-[#7:5]-[C:6]-[C;H0;D3;+0:7](-[O-])=[O;D1;H0:8]>>[O;D1;H0:8]=[C;H0;D3;+0:7]1-[C:6]-[#7:5]-[c:4]:[c:2](:[c:3])-[NH;D2;+0:1]-1
null
[]
null
null
null
null
A suspension of N-(4'-Chloro-5'-ethyl-2'-nitrophenyl)glycine sodium salt (0.082 g, 0.31 mmol) and tin (II) chloride dihydrate (0.215 g, 0.953 mmol) in ethanol (1.0 mL) was refluxed for 45 min. It was then cooled to room temperature and the precipitated solid was filtered, washed with ethanol (1.0 mL), and dried under v...
10.6084/m9.figshare.5104873.v1
null
Nitro group
Secondary amide
null
c1ccc2c(c1)NCCN2
c1ccc2c(c1)NCCN2
Other
C(C)O
null
null
CCc1cc(NCC(=O)[O-])c([N+](=O)[O-])cc1Cl>C(C)O>CCc1cc2c(cc1Cl)NC(=O)CN2
ord_dataset-c2ad1656a3ca4d08888ffb6e3f3a2742
ord-745046916d634bcd956d4328d02e4632
Cc1cc2c(cc1Cl)NC(=O)CN2.O=C(O)C(F)(F)F.O=[N+]([O-])O>>Cc1c(Cl)cc2[nH]c(=O)c(=O)[nH]c2c1[N+](=O)[O-]
ClC1=C(C=C2NCC(NC2=C1)=O)C.[N+](=O)(O)[O-].C(=O)(C(F)(F)F)O>>ClC1=C(C(=C2NC(C(NC2=C1)=O)=O)[N+](=O)[O-])C
[CH3:1][c:2]1[c:3]([Cl:4])[cH:5][c:6]2[c:13]([cH:14]1)[NH:12][CH2:10][C:8](=[O:9])[NH:7]2.OC(C(F)(F)F)=[O:11].O[N+:15](=[O:16])[O-:17]>>[CH3:1][c:2]1[c:3]([Cl:4])[cH:5][c:6]2[nH:7][c:8](=[O:9])[c:10](=[O:11])[nH:12][c:13]2[c:14]1[N+:15](=[O:16])[O-:17]
Cc1cc2c(cc1Cl)NC(=O)CN2.O=C(O)C(F)(F)F.O=[N+]([O-])O
Cc1c(Cl)cc2[nH]c(=O)c(=O)[nH]c2c1[N+](=O)[O-]
null
null
null
Protection
OtherReaction
80c677eaf05c9e3260cc2c36d32955f1a198302f695a8f6f7fdc8245e989ad9f
c3f6f8522c120ea155981de10cc58aa2ca6e015b56fcea863d9ab5f778379b6c
O=c1[nH]c2ccccc2[nH]c1=O
F-C(-F)(-F)-C(-O)=[O;H0;D1;+0:1].O-[N+;H0;D3:2](-[O;-;D1;H0:3])=[O;D1;H0:4].[C;D1;H3:5]-[c:6]1:[c:7]:[c:8]:[c:9]2:[c:10](:[cH;D2;+0:11]:1)-[NH;D2;+0:12]-[CH2;D2;+0:13]-[C;H0;D3;+0:14](=[O;D1;H0:15])-[NH;D2;+0:16]-2>>[C;D1;H3:5]-[c:6]1:[c:7]:[c:8]:[c:9]2:[nH;D2;+0:16]:[c;H0;D3;+0:14](=[O;D1;H0:15]):[c;H0;D3;+0:13](=[O;H...
null
[]
null
null
8
HOUR
To a stirred suspension of 7-chloro-3,4-Dihydro-6-methyl-quinoxaline-2(1H)-one (0.100 g, 0.51 mmol) in TFA (3.0 mL) prepared as in Example 8, excess fuming HNO3 (0.30 mL) was added and the resulting red solution was stirred overnight at room temperature. The solvent was removed under vacuum and the residue diluted with...
10.6084/m9.figshare.5104873.v1
null
Trifluoro group.Carboxylic acid.Nitrate.Secondary amide.Secondary amine
Nitro group
c1ccc2c(c1)NCCN2
C1=CNc2ccccc2N1
C1=CNc2ccccc2N1
HF
null
null
8
Cc1cc2c(cc1Cl)NC(=O)CN2.O=C(O)C(F)(F)F.O=[N+]([O-])O>>Cc1c(Cl)cc2[nH]c(=O)c(=O)[nH]c2c1[N+](=O)[O-]
ord_dataset-c2ad1656a3ca4d08888ffb6e3f3a2742
ord-c5c0bc97f38849c2b37ca0ba4d8a916b
Cc1c(Cl)cc2[nH]c(=O)c(=O)[nH]c2c1[N+](=O)[O-]>>Cc1c(Cl)cc2[nH]c(=O)c(=O)[nH]c2c1N
ClC1=C(C(=C2NC(C(NC2=C1)=O)=O)[N+](=O)[O-])C.O.O.[Sn](Cl)Cl>>NC1=C2NC(C(NC2=CC(=C1C)Cl)=O)=O
O=[N+:15]([O-])[c:14]1[c:2]([CH3:1])[c:3]([Cl:4])[cH:5][c:6]2[nH:7][c:8](=[O:9])[c:10](=[O:11])[nH:12][c:13]21>>[CH3:1][c:2]1[c:3]([Cl:4])[cH:5][c:6]2[nH:7][c:8](=[O:9])[c:10](=[O:11])[nH:12][c:13]2[c:14]1[NH2:15]
Cc1c(Cl)cc2[nH]c(=O)c(=O)[nH]c2c1[N+](=O)[O-]
Cc1c(Cl)cc2[nH]c(=O)c(=O)[nH]c2c1N
null
null
C(C)O
Reduction
Reduction of nitro groups to amines
bbc242b150a51e69d3ad1caaa391f4422710431b398dcb880555f476706790be
7b0317532ea57a4fcedc1efc3e3c22eb5238d1c8330da53d4f9801fc2391f567
O=c1[nH]c2ccccc2[nH]c1=O
O=[N+;H0;D3:1](-[O-])-[c:2](:[c:3]):[c:4]1:[#7;a:5]:[c:6]:[c:7]:[#7;a:8]:[c:9]:1>>[NH2;D1;+0:1]-[c:2](:[c:3]):[c:4]1:[#7;a:5]:[c:6]:[c:7]:[#7;a:8]:[c:9]:1
null
[]
null
null
null
null
A suspension of 7-chloro-1,4-dihydro-6-methyl-5-nitroquinoxaline-2,3-dione (0.050 g, 0.20 mmol) and tin (II) chloride dihydrate (0.133 g, 0.60 mmol) in ethanol (1.0 mL) was refluxed for 6 h. The suspension was then cooled to room temperature and the solid was collected by vacuum filtration, washed with ethanol (1 mL), ...
10.6084/m9.figshare.5104873.v1
null
Nitro group
Primary amine
null
null
C1=CNc2ccccc2N1
Other
C(C)O
null
null
Cc1c(Cl)cc2[nH]c(=O)c(=O)[nH]c2c1[N+](=O)[O-]>C(C)O>Cc1c(Cl)cc2[nH]c(=O)c(=O)[nH]c2c1N
ord_dataset-c2ad1656a3ca4d08888ffb6e3f3a2742
ord-e7df90c36ae44d7eb540bd7f7071a5b1
Fc1ccc(Cl)c(F)c1>>O=[N+]([O-])c1cc(Cl)c(F)cc1F
ClC1=C(C=C(C=C1)F)F.[N+](=O)([O-])[O-].[K+]>>ClC1=C(C=C(C(=C1)[N+](=O)[O-])F)F
[cH:4]1[cH:5][c:6]([Cl:7])[c:8]([F:9])[cH:10][c:11]1[F:12]>>[O:1]=[N+:2]([O-:3])[c:4]1[cH:5][c:6]([Cl:7])[c:8]([F:9])[cH:10][c:11]1[F:12]
Fc1ccc(Cl)c(F)c1
O=[N+]([O-])c1cc(Cl)c(F)cc1F
null
null
OS(=O)(=O)O
Functional Group Addition
OtherReaction
6862453966ade01f48ad6e78fdee5c31f5f3bef2a50d1592f73a35f3caf6154f
22f3183026a2d99c91ec0c53f0059a15c8421016bd62c8ab45281362b96dc686
c1ccccc1
[F;D1;H0:1]-[c:2](:[c:3]):[cH;D2;+0:4]:[c:5]:[c:6]>>[F;D1;H0:1]-[c:2](:[c:3]):[c;H0;D3;+0:4](-[#7;+:7](-[O;-;D1;H0:8])=[O;D1;H0:9]):[c:5]:[c:6]
null
[]
null
null
8
HOUR
To a stirred solution of 1-chloro-2,4-difluorobenzene (0.829 g, 5.58 mmol) in concd H2SO4 (8.0 mL) at 0° C., KNO3 (0.565 g, 5.59 mmol) was added in one portion. The resulting solution was allowed to warm to room temperature and stirred overnight at room temperature. It was then poured into ice (80 g) and extracted with...
10.6084/m9.figshare.5104873.v1
null
null
Nitro group
c1ccccc1
c1ccccc1
c1ccccc1
Other
OS(=O)(=O)O
null
8
Fc1ccc(Cl)c(F)c1>OS(=O)(=O)O>O=[N+]([O-])c1cc(Cl)c(F)cc1F
ord_dataset-c2ad1656a3ca4d08888ffb6e3f3a2742
ord-ad05905abd7d40db96cb11b9e5771e2e
O=C([O-])CNc1cc(F)c(Cl)cc1[N+](=O)[O-]>>O=C1CNc2cc(F)c(Cl)cc2N1
[Na+].ClC1=CC(=C(C=C1F)NCC(=O)[O-])[N+](=O)[O-].[Na+].ClC1=C(C=C(C(=C1)[N+](=O)[O-])F)NCC(=O)[O-].O.O.[Sn](Cl)Cl>>ClC1=C(C=C2NCC(NC2=C1)=O)F
O=[N+:13]([O-])[c:12]1[c:5]([NH:4][CH2:3][C:2]([O-])=[O:1])[cH:6][c:7]([F:8])[c:9]([Cl:10])[cH:11]1>>[O:1]=[C:2]1[CH2:3][NH:4][c:5]2[cH:6][c:7]([F:8])[c:9]([Cl:10])[cH:11][c:12]2[NH:13]1
O=C([O-])CNc1cc(F)c(Cl)cc1[N+](=O)[O-]
O=C1CNc2cc(F)c(Cl)cc2N1
null
null
C(C)O
Functional Group Interconversion
OtherReaction
183261da32373f3dc4dd237e8a75ee7d967e6598ba6a325e2c313518785e8076
013ea010a5fc8551154a976160b11b17bb85fae400bd37b37532ea17a3df22d8
O=C1CNc2ccccc2N1
O=[N+;H0;D3:1](-[O-])-[c:2](:[c:3]):[c:4]-[#7:5]-[C:6]-[C;H0;D3;+0:7](-[O-])=[O;D1;H0:8]>>[O;D1;H0:8]=[C;H0;D3;+0:7]1-[C:6]-[#7:5]-[c:4]:[c:2](:[c:3])-[NH;D2;+0:1]-1
null
[]
null
null
null
null
A suspension of N-(4'-chloro-5'-fluoro-2'-nitrophenyl)glycine sodium salt and N-(2'-chloro-5'-fluoro-4'-nitrophenyl)glycine sodium salt (0.175 g, 0.704 mmol) and tin (II) chloride dihydrate (0.475 g, 2.11 mmol) in ethanol (3.5 mL) was refluxed for 30 min. It was then cooled to room temperature and the solvent was remov...
10.6084/m9.figshare.5104873.v1
null
Nitro group
Secondary amide
null
c1ccc2c(c1)NCCN2
c1ccc2c(c1)NCCN2
Other
C(C)O
null
null
O=C([O-])CNc1cc(F)c(Cl)cc1[N+](=O)[O-]>C(C)O>O=C1CNc2cc(F)c(Cl)cc2N1
ord_dataset-c2ad1656a3ca4d08888ffb6e3f3a2742
ord-8b969f968a774a71a47db4d035adaf78
CCS.O=c1[nH]c2cc(Cl)c(F)c([N+](=O)[O-])c2[nH]c1=O>>CCSc1c(Cl)cc2[nH]c(=O)c(=O)[nH]c2c1[N+](=O)[O-]
ClC1=C(C(=C2NC(C(NC2=C1)=O)=O)[N+](=O)[O-])F.C(C)S.[Na]>>ClC1=C(C(=C2NC(C(NC2=C1)=O)=O)[N+](=O)[O-])SCC
[CH3:1][CH2:2][SH:3].F[c:4]1[c:5]([Cl:6])[cH:7][c:8]2[nH:9][c:10](=[O:11])[c:12](=[O:13])[nH:14][c:15]2[c:16]1[N+:17](=[O:18])[O-:19]>>[CH3:1][CH2:2][S:3][c:4]1[c:5]([Cl:6])[cH:7][c:8]2[nH:9][c:10](=[O:11])[c:12](=[O:13])[nH:14][c:15]2[c:16]1[N+:17](=[O:18])[O-:19]
CCS.O=c1[nH]c2cc(Cl)c(F)c([N+](=O)[O-])c2[nH]c1=O
CCSc1c(Cl)cc2[nH]c(=O)c(=O)[nH]c2c1[N+](=O)[O-]
null
Cl
O.CS(=O)C
Heteroatom Alkylation and Arylation
thioether_nucl_sub
37d6a583faeeb606077eb6008f8ae442049fb9481db2190565bab57b55926369
b7fe376f7aad2517725eef26ab981e4baa6c31c5f38fdf89e7c52a4a2c6cc1d2
O=c1[nH]c2ccccc2[nH]c1=O
F-[c;H0;D3;+0:1]1:[c:2](-[#7;+:3]):[c:4]2:[#7;a:5]:[c:6]:[c:7]:[#7;a:8]:[c:9]:2:[c:10]:[c:11]:1-[Cl;D1;H0:12].[C;D1;H3:13]-[C:14]-[SH;D1;+0:15]>>[#7;+:3]-[c:2]1:[c:4]2:[#7;a:5]:[c:6]:[c:7]:[#7;a:8]:[c:9]:2:[c:10]:[c:11](-[Cl;D1;H0:12]):[c;H0;D3;+0:1]:1-[S;H0;D2;+0:15]-[C:14]-[C;D1;H3:13]
null
[]
null
null
null
null
A solution of 7-Chloro-1,4-dihydro-6-fluoro-5-nitroquinoxaline-2,3-dione (0.100 g, 0.385 mmol) and ethanethiol, sodium salt (0.130 g, 1.55 mmol) in DMSO (1.0 mL) was stirred at room temperature for 24 h. The resulting solution was diluted with water (5 mL) and acidified with concd HCl (4-5 drops) to pH ~5. The precipit...
10.6084/m9.figshare.5104873.v1
null
Aromatic halide.Aliphatic thiol
Monosulfide
C1=CNc2ccccc2N1
C1=CNc2ccccc2N1
C1=CNc2ccccc2N1
HF
Cl.O.CS(=O)C
null
null
CCS.O=c1[nH]c2cc(Cl)c(F)c([N+](=O)[O-])c2[nH]c1=O>Cl.O.CS(=O)C>CCSc1c(Cl)cc2[nH]c(=O)c(=O)[nH]c2c1[N+](=O)[O-]
ord_dataset-c2ad1656a3ca4d08888ffb6e3f3a2742
ord-1a076efc56904834b8e30dd331d929ed
Cc1cc(F)ccc1Cl>>Cc1cc(F)c([N+](=O)[O-])cc1Cl
ClC1=C(C=C(C=C1)F)C.[N+](=O)([O-])[O-].[K+]>>ClC1=C(C=C(C(=C1)[N+](=O)[O-])F)C
[CH3:1][c:2]1[cH:3][c:4]([F:5])[cH:6][cH:10][c:11]1[Cl:12]>>[CH3:1][c:2]1[cH:3][c:4]([F:5])[c:6]([N+:7](=[O:8])[O-:9])[cH:10][c:11]1[Cl:12]
Cc1cc(F)ccc1Cl
Cc1cc(F)c([N+](=O)[O-])cc1Cl
null
null
OS(=O)(=O)O
Functional Group Addition
OtherReaction
6862453966ade01f48ad6e78fdee5c31f5f3bef2a50d1592f73a35f3caf6154f
22f3183026a2d99c91ec0c53f0059a15c8421016bd62c8ab45281362b96dc686
c1ccccc1
[F;D1;H0:1]-[c:2](:[c:3]):[cH;D2;+0:4]:[c:5]:[c:6]>>[F;D1;H0:1]-[c:2](:[c:3]):[c;H0;D3;+0:4](-[#7;+:7](-[O;-;D1;H0:8])=[O;D1;H0:9]):[c:5]:[c:6]
90.4
[{"value": 90.0, "product": "ClC1=C(C=C(C(=C1)[N+](=O)[O-])F)C", "details": "PERCENTYIELD", "is_desired": false}, {"value": 90.4, "product": "ClC1=C(C=C(C(=C1)[N+](=O)[O-])F)C", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
8
HOUR
To a stirred solution of 2-chloro-5-fluorotoluene (10.356 g, 71.628 mmol, Lancaster, used as received) in conc. H2SO4 (70 mL) at 0° C., KNO3 (7.252 g, 71.72 mmol) was added in four equal portions. The resulting pale yellow solution was allowed to warm to room temperature and was stirred overnight at room temperature. I...
10.6084/m9.figshare.5104873.v1
null
null
Nitro group
c1ccccc1
c1ccccc1
c1ccccc1
Other
OS(=O)(=O)O
null
8
Cc1cc(F)ccc1Cl>OS(=O)(=O)O>Cc1cc(F)c([N+](=O)[O-])cc1Cl
ord_dataset-c2ad1656a3ca4d08888ffb6e3f3a2742
ord-6defbbfc6e5a4b3791bf13861c906a5e
Cc1cc(NCC(=O)[O-])c([N+](=O)[O-])cc1Cl>>Cc1cc2c(cc1Cl)NC(=O)CN2
[K+].ClC1=CC(=C(C=C1C)NCC(=O)[O-])[N+](=O)[O-].S(=O)([O-])S(=O)[O-].[Na+].[Na+]>>ClC1=C(C=C2NCC(NC2=C1)=O)C
O=[N+:9]([O-])[c:5]1[c:4]([NH:13][CH2:12][C:10]([O-])=[O:11])[cH:3][c:2]([CH3:1])[c:7]([Cl:8])[cH:6]1>>[CH3:1][c:2]1[cH:3][c:4]2[c:5]([cH:6][c:7]1[Cl:8])[NH:9][C:10](=[O:11])[CH2:12][NH:13]2
Cc1cc(NCC(=O)[O-])c([N+](=O)[O-])cc1Cl
Cc1cc2c(cc1Cl)NC(=O)CN2
null
null
O
Functional Group Interconversion
OtherReaction
183261da32373f3dc4dd237e8a75ee7d967e6598ba6a325e2c313518785e8076
013ea010a5fc8551154a976160b11b17bb85fae400bd37b37532ea17a3df22d8
O=C1CNc2ccccc2N1
O=[N+;H0;D3:1](-[O-])-[c:2](:[c:3]):[c:4]-[#7:5]-[C:6]-[C;H0;D3;+0:7](-[O-])=[O;D1;H0:8]>>[O;D1;H0:8]=[C;H0;D3;+0:7]1-[C:6]-[#7:5]-[c:4]:[c:2](:[c:3])-[NH;D2;+0:1]-1
87.6
[{"value": 86.0, "product": "ClC1=C(C=C2NCC(NC2=C1)=O)C", "details": "PERCENTYIELD", "is_desired": false}, {"value": 87.6, "product": "ClC1=C(C=C2NCC(NC2=C1)=O)C", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
80
CELSIUS
1
HOUR
To a stirred bright orange solution of N-(4'-chloro-5'-methyl-2'-nitrophenyl)glycine potassium salt (0.097 g, 0.36 mmol) in water (5.0 mL) at 80° C., sodium dithionite (0.500 g, 2.87 mmol) was added in two equal portions. It instantly formed a white suspension, which was stirred at 80° C. for 1 h. It was then cooled at...
10.6084/m9.figshare.5104873.v1
null
Nitro group
Secondary amide
null
c1ccc2c(c1)NCCN2
c1ccc2c(c1)NCCN2
Other
O
80
1
Cc1cc(NCC(=O)[O-])c([N+](=O)[O-])cc1Cl>O>Cc1cc2c(cc1Cl)NC(=O)CN2
ord_dataset-c2ad1656a3ca4d08888ffb6e3f3a2742
ord-8dc8ca74650e49239a9ba862a47071df
N#Cc1n[nH]c(NC(=O)C(F)(F)F)c1SC(F)(F)F>>N#Cc1n[nH]c(N)c1SC(F)(F)F
C(#N)C1=NNC(=C1SC(F)(F)F)NC(C(F)(F)F)=O.[OH-].[NH4+].Cl>>C(#N)C1=NNC(=C1SC(F)(F)F)N
O=C(C(F)(F)F)[NH:7][c:6]1[nH:5][n:4][c:3]([C:2]#[N:1])[c:8]1[S:9][C:10]([F:11])([F:12])[F:13]>>[N:1]#[C:2][c:3]1[n:4][nH:5][c:6]([NH2:7])[c:8]1[S:9][C:10]([F:11])([F:12])[F:13]
N#Cc1n[nH]c(NC(=O)C(F)(F)F)c1SC(F)(F)F
N#Cc1n[nH]c(N)c1SC(F)(F)F
null
null
CO.C(C)(=O)OCC
Reduction
Hydrogenolysis of amides/imides/carbamates
44b36597c7daf0608965c52c8db8a9220c21d9447ce54e0af375898475f3493f
caaeb83af2cb178156ae90fe7f610a106cd4bb5397d23f56d37a7fe11e2668ed
c1cn[nH]c1
F-C(-F)(-F)-C(=O)-[NH;D2;+0:1]-[c:2]1:[#7;a:3]:[#7;a:4]:[c:5]:[c:6]:1>>[NH2;D1;+0:1]-[c:2]1:[#7;a:3]:[#7;a:4]:[c:5]:[c:6]:1
87.6
[{"value": 87.6, "product": "C(#N)C1=NNC(=C1SC(F)(F)F)N", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
15
HOUR
The product of Step E (55 g, 181 mmoles) was dissolved in methanol. 100 ml of ammonium hydroxide were added, the solution was refluxed for 3 hours and then stirred at room temperature for 15 hours. The methanolic solution was brought to pH7 using concentrated aqueous hydrochloric acid and diluted with ethyl acetate. Th...
10.6084/m9.figshare.5104873.v1
null
Trifluoro group.Secondary amide
Primary amine
null
null
c1cn[nH]c1
Other
CO.C(C)(=O)OCC
null
15
N#Cc1n[nH]c(NC(=O)C(F)(F)F)c1SC(F)(F)F>CO.C(C)(=O)OCC>N#Cc1n[nH]c(N)c1SC(F)(F)F
ord_dataset-c2ad1656a3ca4d08888ffb6e3f3a2742
ord-d35c5951d44f43e7878bff135ef2e886
O=C(N[C@H](CO)Cc1ccccc1)OCc1ccccc1>>O=C[C@H](Cc1ccccc1)NC(=O)OCc1ccccc1
C(CC(O)(C(=O)O)CC(=O)O)(=O)O.C(CC(O)(C(=O)O)CC(=O)O)(=O)O.CS(=O)C.C(C(=O)Cl)(=O)Cl.C(C1=CC=CC=C1)OC(=O)N[C@@H](CC1=CC=CC=C1)CO>>C(C1=CC=CC=C1)OC(=O)N[C@@H](CC1=CC=CC=C1)C=O
[OH:1][CH2:2][C@H:3]([CH2:4][c:5]1[cH:6][cH:7][cH:8][cH:9][cH:10]1)[NH:11][C:12](=[O:13])[O:14][CH2:15][c:16]1[cH:17][cH:18][cH:19][cH:20][cH:21]1>>[O:1]=[CH:2][C@H:3]([CH2:4][c:5]1[cH:6][cH:7][cH:8][cH:9][cH:10]1)[NH:11][C:12](=[O:13])[O:14][CH2:15][c:16]1[cH:17][cH:18][cH:19][cH:20][cH:21]1
O=C(N[C@H](CO)Cc1ccccc1)OCc1ccccc1
O=C[C@H](Cc1ccccc1)NC(=O)OCc1ccccc1
null
null
ClCCl.CCOCC.C(C)N(CC)CC
Oxidation
Oxidation or Dehydrogenation of Alcohols to Aldehydes and Ketones
41bfa9deea81b465c88ad21fdfb64a2e1ba29490558cf430df132cb98b4a538b
0a03c6724c1862e8f86d4a463afda55b8e067dc6cb42597b472eb7cabc03eda3
O=C(NCCc1ccccc1)OCc1ccccc1
[C:1]-[C:2](-[#7:3]-[C:4]=[O;D1;H0:5])-[CH2;D2;+0:6]-[OH;D1;+0:7]>>[C:1]-[C:2](-[#7:3]-[C:4]=[O;D1;H0:5])-[CH;D2;+0:6]=[O;H0;D1;+0:7]
103.2
[{"value": 103.2, "product": "C(C1=CC=CC=C1)OC(=O)N[C@@H](CC1=CC=CC=C1)C=O", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
-78
CELSIUS
10
MINUTE
To a solution of 1.8 ml of dimethyl sulfoxide in 20 ml of dichloromethane cooled to -78° C. was added slowly 1.65 ml of oxalyl chloride. The solution was stirred for 10 min at -78° C. and a solution of 3.6 g (0.012 mol) of N-((benzyloxy)carbonyl)-L-phenylalaninol in 45 ml of dichloromethane was added slowly. The result...
10.6084/m9.figshare.5104873.v1
null
Primary alcohol
Aldehyde
null
null
c1ccccc1.c1ccccc1
null
ClCCl.CCOCC.C(C)N(CC)CC
-78
0.166667
O=C(N[C@H](CO)Cc1ccccc1)OCc1ccccc1>ClCCl.CCOCC.C(C)N(CC)CC>O=C[C@H](Cc1ccccc1)NC(=O)OCc1ccccc1
ord_dataset-c2ad1656a3ca4d08888ffb6e3f3a2742
ord-08c659d86451420eab107de0c01f7ba3
COC(=O)[C@](N)(N=C=O)C(C)C.OCc1ccccn1>>COC(=O)[C@@H](NC(=O)OCc1ccccn1)C(C)C
COC([C@@](N)(C(C)C)N=C=O)=O.N1=C(C=CC=C1)CO>>COC([C@@H](NC(=O)OCC1=NC=CC=C1)C(C)C)=O
N[C@@:5]([C:3]([O:2][CH3:1])=[O:4])([N:6]=[C:7]=[O:8])[CH:17]([CH3:18])[CH3:19].[OH:9][CH2:10][c:11]1[cH:12][cH:13][cH:14][cH:15][n:16]1>>[CH3:1][O:2][C:3](=[O:4])[C@@H:5]([NH:6][C:7](=[O:8])[O:9][CH2:10][c:11]1[cH:12][cH:13][cH:14][cH:15][n:16]1)[CH:17]([CH3:18])[CH3:19]
COC(=O)[C@](N)(N=C=O)C(C)C.OCc1ccccn1
COC(=O)[C@@H](NC(=O)OCc1ccccn1)C(C)C
null
null
C1(=CC=CC=C1)C
Functional Group Interconversion
OtherReaction
a23be472936c50c173c2dd2734289c9dfae50efca7ef50b8a0cb8898e49c8803
594e835804772a869b7a162be980a733776c00b82a87e4b097f0a7da7fddd8e1
c1ccncc1
N-[C@@;H0;D4;+0:1](-[N;H0;D2;+0:2]=[C;H0;D2;+0:3]=[O;D1;H0:4])(-[C:5](-[C;D1;H3:6])-[C;D1;H3:7])-[C:8](=[O;D1;H0:9])-[#8:10]-[C;D1;H3:11].[#7;a:12]:[c:13]-[C:14]-[OH;D1;+0:15]>>[#7;a:12]:[c:13]-[C:14]-[O;H0;D2;+0:15]-[C;H0;D3;+0:3](=[O;D1;H0:4])-[NH;D2;+0:2]-[C@@H;D3;+0:1](-[C:5](-[C;D1;H3:6])-[C;D1;H3:7])-[C:8](=[O;D1...
54.1
[{"value": 54.0, "product": "COC([C@@H](NC(=O)OCC1=NC=CC=C1)C(C)C)=O", "details": "PERCENTYIELD", "is_desired": false}, {"value": 54.1, "product": "COC([C@@H](NC(=O)OCC1=NC=CC=C1)C(C)C)=O", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
null
null
A solution of 0.78 g (5.0 mmol) of α-isocyanato-valine methyl ester and 0.55 ml (5.7 mmol) of pyridine-2-methanol in 30 mL of toluene was heated at reflux under N2 atmosphere for 4 h. The solvent was removed in vacuo, and the residue was purified by silica gel chromatography using 2% methanol in chloroform to give 0.72...
10.6084/m9.figshare.5104873.v1
null
Ester.Isocyanate.Primary alcohol.Primary amine
Carbamic ester.Ester
null
null
c1ccncc1
Other
C1(=CC=CC=C1)C
null
null
COC(=O)[C@](N)(N=C=O)C(C)C.OCc1ccccn1>C1(=CC=CC=C1)C>COC(=O)[C@@H](NC(=O)OCc1ccccn1)C(C)C
ord_dataset-c2ad1656a3ca4d08888ffb6e3f3a2742
ord-26eb608ac2fb46d293186deb92007f42
CC(C)(C)OC(=O)NCc1ccccn1.CI>>CN(Cc1ccccn1)C(=O)OC(C)(C)C
C(C)(C)(C)OC(=O)NCC1=NC=CC=C1.[H-].[Na+].CI>>C(C)(C)(C)OC(=O)N(C)CC1=NC=CC=C1
[NH:2]([CH2:3][c:4]1[cH:5][cH:6][cH:7][cH:8][n:9]1)[C:10](=[O:11])[O:12][C:13]([CH3:14])([CH3:15])[CH3:16].I[CH3:1]>>[CH3:1][N:2]([CH2:3][c:4]1[cH:5][cH:6][cH:7][cH:8][n:9]1)[C:10](=[O:11])[O:12][C:13]([CH3:14])([CH3:15])[CH3:16]
CC(C)(C)OC(=O)NCc1ccccn1.CI
CN(Cc1ccccn1)C(=O)OC(C)(C)C
null
null
O1CCCC1
Heteroatom Alkylation and Arylation
N-alkylation of secondary amines with alkyl halides
29c841ae076cb6ee785aad2a4e3ce1a9b47357d7ad25657b8d9991b1347f5721
c485eddcb40c5a0d396ffdb624041effa09ee4f5ca2ecce3fe13077cf65004ed
c1ccncc1
I-[CH3;D1;+0:1].[#7;a:2]:[c:3]-[C:4]-[NH;D2;+0:5]-[C:6](=[O;D1;H0:7])-[#8:8]-[C:9](-[C;D1;H3:10])(-[C;D1;H3:11])-[C;D1;H3:12]>>[#7;a:2]:[c:3]-[C:4]-[N;H0;D3;+0:5](-[CH3;D1;+0:1])-[C:6](=[O;D1;H0:7])-[#8:8]-[C:9](-[C;D1;H3:10])(-[C;D1;H3:11])-[C;D1;H3:12]
70.6
[{"value": 70.0, "product": "C(C)(C)(C)OC(=O)N(C)CC1=NC=CC=C1", "details": "PERCENTYIELD", "is_desired": false}, {"value": 70.6, "product": "C(C)(C)(C)OC(=O)N(C)CC1=NC=CC=C1", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
15
MINUTE
A solution of 19.8 g (95 mmol) of 2-(N-(t-butyloxycarbonyl)aminomethyl)pyridine in anhydrous tetrahydrofuran was cooled under N2 atmosphere to 0° C. and treated with 4.95 g (124 mmol) of sodium hydride (60% dispersion in oil). The solution was stirred for 15 min, treated dropwise with 7.1 ml (114 mmol) of methyl iodide...
10.6084/m9.figshare.5104873.v1
null
Carbamic ester
Carbamic ester
null
null
c1ccncc1
HI
O1CCCC1
null
0.25
CC(C)(C)OC(=O)NCc1ccccn1.CI>O1CCCC1>CN(Cc1ccccn1)C(=O)OC(C)(C)C
ord_dataset-c2ad1656a3ca4d08888ffb6e3f3a2742
ord-e93e26de6b054b1f97fa7352b742e53d
CN1CCOCC1.COC(=O)[C@](N)(N=C=O)C(C)C.c1ccncc1>>COC(=O)[C@@H](NC(=O)N(C)Cc1ccccn1)C(C)C
Cl.Cl.N1=CC=CC=C1.COC([C@@](N)(C(C)C)N=C=O)=O.CN1CCOCC1>>COC([C@@H](NC(=O)N(CC1=NC=CC=C1)C)C(C)C)=O
C1C[N:9]([CH3:10])[CH2:11]CO1.N[C@@:5]([C:3]([O:2][CH3:1])=[O:4])([N:6]=[C:7]=[O:8])[CH:18]([CH3:19])[CH3:20].[cH:12]1[cH:13][cH:15][cH:14][cH:16][n:17]1>>[CH3:1][O:2][C:3](=[O:4])[C@@H:5]([NH:6][C:7](=[O:8])[N:9]([CH3:10])[CH2:11][c:12]1[cH:13][cH:14][cH:15][cH:16][n:17]1)[CH:18]([CH3:19])[CH3:20]
CN1CCOCC1.COC(=O)[C@](N)(N=C=O)C(C)C.c1ccncc1
COC(=O)[C@@H](NC(=O)N(C)Cc1ccccn1)C(C)C
null
null
ClCCl
Acylation
OtherReaction
5f78e7a9317bbf5d5ac00daeea29dec8bf69abe7d4911d6308ca83fdb03a70d6
2effd315014811dadf8dba713f272b199ed3e0d3d89636a6a85d466106a03f82
c1ccncc1
N-[C@@;H0;D4;+0:1](-[N;H0;D2;+0:2]=[C;H0;D2;+0:3]=[O;D1;H0:4])(-[C:5](-[C;D1;H3:6])-[C;D1;H3:7])-[C:8](=[O;D1;H0:9])-[#8:10]-[C;D1;H3:11].[#7;a: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;H3:18]-[N;H0;D3;+0:19]1-C-C-O-C-[CH2;D2;+0:20]-1>>[C;D1;H3:18]-[N;H0;D3;+0:19](-[CH2;D2;+0:20...
null
[]
null
null
2
HOUR
A mixture of 1.61 g (7.2 mmol) of 2-(N-methylamino)methyl)pyridine dihydrochloride and 1.14 g (7.2 mmol) of α-isocyanato-valine methyl ester in 40 ml of dichloromethane was treated with 2 ml (18 mmol) of 4-methylmorpholine. After being stirred for 2 h, the solution was partitioned between dichloromethane and water, dri...
10.6084/m9.figshare.5104873.v1
null
Ester.Ether.Isocyanate.Primary amine.Tertiary amine
Ester.Urea
C1COCC[NH]1.c1ccncc1
c1ccncc1
c1ccncc1
HO-
ClCCl
null
2
CN1CCOCC1.COC(=O)[C@](N)(N=C=O)C(C)C.c1ccncc1>ClCCl>COC(=O)[C@@H](NC(=O)N(C)Cc1ccccn1)C(C)C
ord_dataset-c2ad1656a3ca4d08888ffb6e3f3a2742
ord-724f26f9de804657823e0d6bd96a4e01
COC(=O)[C@@H](NC(=O)N(C)Cc1ccccn1)C(C)C>>CC(C)[C@H](NC(=O)N(C)Cc1ccccn1)C(=O)O
COC([C@@H](NC(=O)N(CC1=NC=CC=C1)C)C(C)C)=O.[OH-].[Li+]>>CN(CC1=NC=CC=C1)C(=O)N[C@@H](C(C)C)C(=O)O
C[O:19][C:17]([C@H:4]([CH:2]([CH3:1])[CH3:3])[NH:5][C:6](=[O:7])[N:8]([CH3:9])[CH2:10][c:11]1[cH:12][cH:13][cH:14][cH:15][n:16]1)=[O:18]>>[CH3:1][CH:2]([CH3:3])[C@H:4]([NH:5][C:6](=[O:7])[N:8]([CH3:9])[CH2:10][c:11]1[cH:12][cH:13][cH:14][cH:15][n:16]1)[C:17](=[O:18])[OH:19]
COC(=O)[C@@H](NC(=O)N(C)Cc1ccccn1)C(C)C
CC(C)[C@H](NC(=O)N(C)Cc1ccccn1)C(=O)O
null
null
O1CCOCC1
Deprotection
Ester saponification (methyl deprotection)
d872e08ad5c85a4add6cd04e6e987e73fead5f79b3f30ba61a81ba5029b29894
38ae1ee78433b9acfb0390501446149c80f88f23ac2d84c60b3369bdab75cec9
c1ccncc1
C-[O;H0;D2;+0:1]-[C:2](-[C:3])=[O;D1;H0:4]>>[C:3]-[C:2](=[O;D1;H0:4])-[OH;D1;+0:1]
85
[{"value": 85.0, "product": "CN(CC1=NC=CC=C1)C(=O)N[C@@H](C(C)C)C(=O)O", "details": "PERCENTYIELD", "is_desired": false}, {"value": 85.0, "product": "CN(CC1=NC=CC=C1)C(=O)N[C@@H](C(C)C)C(=O)O", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
1
HOUR
A solution of 4.47 g (16 mmol) of N-((N-methyl-N-((2-pyridinyl)methyl)amino)carbonyl)valine methyl ester in 65 ml of dioxane was treated with 65 ml of 0.5M aqueous lithium hydroxide. After being stirred at ambient temperature for 1 h, the resulting solution was concentrated in vacuo to a small volume (ca. 5 ml), neutra...
10.6084/m9.figshare.5104873.v1
null
Ester
Carboxylic acid
null
null
c1ccncc1
Other
O1CCOCC1
null
1
COC(=O)[C@@H](NC(=O)N(C)Cc1ccccn1)C(C)C>O1CCOCC1>CC(C)[C@H](NC(=O)N(C)Cc1ccccn1)C(=O)O
ord_dataset-c2ad1656a3ca4d08888ffb6e3f3a2742
ord-b33e4cc98aef4ab5917079a082a85979
CC(C)C(N)=S.O=C(CCl)CCl>>CC(C)c1nc(CCl)cs1.Cl
CC(C(N)=S)C.ClCC(=O)CCl.[O-]S(=O)(=O)[O-].[Mg+2]>>Cl.ClCC=1N=C(SC1)C(C)C
[CH3:1][CH:2]([CH3:3])[C:4]([NH2:5])=[S:10].O=[C:6]([CH2:7][Cl:8])[CH2:9][Cl:11]>>[CH3:1][CH:2]([CH3:3])[c:4]1[n:5][c:6]([CH2:7][Cl:8])[cH:9][s:10]1.[ClH:11]
CC(C)C(N)=S.O=C(CCl)CCl
CC(C)c1nc(CCl)cs1.Cl
null
null
CC(=O)C
Aromatic Heterocycle Formation
OtherReaction
21eb8c7cda3c7fc14309a0c556334226f1a9147c334386d33bc70341830a82ec
9f145257a80f08f1a7a6ee36c84cd4115965bd63128f36de61c7ed688ad2603c
c1cscn1
O=[C;H0;D3;+0:1](-[C:2]-[Cl;D1;H0:3])-[CH2;D2;+0:4]-[Cl;H0;D1;+0:5].[C;D1;H3:6]-[C:7](-[C;D1;H3:8])-[C;H0;D3;+0:9](-[NH2;D1;+0:10])=[S;H0;D1;+0:11]>>[C;D1;H3:6]-[C:7](-[C;D1;H3:8])-[c;H0;D3;+0:9]1:[n;H0;D2;+0:10]:[c;H0;D3;+0:1](-[C:2]-[Cl;D1;H0:3]):[cH;D2;+0:4]:[s;H0;D2;+0:11]:1.[ClH;D0;+0:5]
null
[]
null
null
null
null
A mixture of 94.0 g (0.91 mol) of 2-methylpropaneothioamide, 115.7 g (0.91 mol) of 1,3-dichloroacetone, and 109.7 g (0.91 mol) of MgSO4 in 1.6 liters of acetone was heated at reflux for 3.5 h. The resulting mixture was allowed to cool, filtered, and the solvent was removed in vacuo to provide the crude desired compound...
10.6084/m9.figshare.5104873.v1
null
Primary halide.Ketone.Thioamide
null
null
c1cscn1
c1cscn1
HO-
CC(=O)C
null
null
CC(C)C(N)=S.O=C(CCl)CCl>CC(=O)C>CC(C)c1nc(CCl)cs1.Cl
ord_dataset-c2ad1656a3ca4d08888ffb6e3f3a2742
ord-ad3df19240ba47bfa890ccd0addad581
CC(C)c1nc(CCl)cs1.CN>>CNCc1csc(C(C)C)n1
Cl.ClCC=1N=C(SC1)C(C)C.CN>>C(C)(C)C=1SC=C(N1)CNC
Cl[CH2:3][c:4]1[cH:5][s:6][c:7]([CH:8]([CH3:9])[CH3:10])[n:11]1.[CH3:1][NH2:2]>>[CH3:1][NH:2][CH2:3][c:4]1[cH:5][s:6][c:7]([CH:8]([CH3:9])[CH3:10])[n:11]1
CC(C)c1nc(CCl)cs1.CN
CNCc1csc(C(C)C)n1
null
null
O
Heteroatom Alkylation and Arylation
N-alkylation of primary amines with alkyl halides
fc19a1445ff204e66e51735d0191465bda3c6691fd233624a54742c9d4828411
0b1d32f56ad00f1e5bdae9390f9227bbea012fa2f8203aac34726b8a6761cc7c
c1cscn1
Cl-[CH2;D2;+0:1]-[c:2]1:[#7;a:3]:[c:4]:[#16;a:5]:[c:6]:1.[C;D1;H3:7]-[NH2;D1;+0:8]>>[C;D1;H3:7]-[NH;D2;+0:8]-[CH2;D2;+0:1]-[c:2]1:[#7;a:3]:[c:4]:[#16;a:5]:[c:6]:1
55
[{"value": 55.0, "product": "C(C)(C)C=1SC=C(N1)CNC", "details": "PERCENTYIELD", "is_desired": false}]
null
null
1
HOUR
A solution of 40 g of 4-(chloromethyl)-2-isopropylthiazole hydrochloride in 100 ml of water was added dropwise with stirring to 400 ml of 40% aqueous methylamine. The resulting solution was stirred for 1 h, then concentrated in vacuo. The residue was taken up in chloroform, dried over Na2SO4, and concentrated in vacuo....
10.6084/m9.figshare.5104873.v1
null
Primary halide.Primary amine
Secondary amine
null
null
c1cscn1
HCl
O
null
1
CC(C)c1nc(CCl)cs1.CN>O>CNCc1csc(C(C)C)n1
ord_dataset-c2ad1656a3ca4d08888ffb6e3f3a2742
ord-d0e8b0d3ed0b4d9ea6bc70ffabf5049e
COC(=O)[C@@H](N)C(C)C.O=C(Cl)Oc1ccc([N+](=O)[O-])cc1>>COC(=O)[C@@H](NC(=O)Oc1ccc([N+](=O)[O-])cc1)C(C)C
ClC(=O)OC1=CC=C(C=C1)[N+](=O)[O-].Cl.COC([C@@H](N)C(C)C)=O.CN1CCOCC1>>COC([C@@H](NC(=O)OC1=CC=C(C=C1)[N+](=O)[O-])C(C)C)=O
[CH3:1][O:2][C:3](=[O:4])[C@@H:5]([NH2:6])[CH:19]([CH3:20])[CH3:21].Cl[C:7](=[O:8])[O:9][c:10]1[cH:11][cH:12][c:13]([N+:14](=[O:15])[O-:16])[cH:17][cH:18]1>>[CH3:1][O:2][C:3](=[O:4])[C@@H:5]([NH:6][C:7](=[O:8])[O:9][c:10]1[cH:11][cH:12][c:13]([N+:14](=[O:15])[O-:16])[cH:17][cH:18]1)[CH:19]([CH3:20])[CH3:21]
COC(=O)[C@@H](N)C(C)C.O=C(Cl)Oc1ccc([N+](=O)[O-])cc1
COC(=O)[C@@H](NC(=O)Oc1ccc([N+](=O)[O-])cc1)C(C)C
null
null
C(Cl)Cl
Protection
Acylation of Nitrogen Nucleophiles by Acyl/Thioacyl/Carbamoyl Halides and Analogs_OS
038720aa61a7efa0f2a9ee6f2e0adf63a9ffdc2be4697c11a6215baef34f97b2
205f353513ce9506ab61831799da8fb73ec2ef5cfa927664496d3ce72c438860
c1ccccc1
Cl-[C;H0;D3;+0:1](=[O;D1;H0:2])-[#8:3]-[c:4].[C:5]-[C:6](-[NH2;D1;+0:7])-[C:8](=[O;D1;H0:9])-[#8:10]-[C;D1;H3:11]>>[C:5]-[C:6](-[NH;D2;+0:7]-[C;H0;D3;+0:1](=[O;D1;H0:2])-[#8:3]-[c:4])-[C:8](=[O;D1;H0:9])-[#8:10]-[C;D1;H3:11]
null
[]
null
null
8
HOUR
A solution of 66.1 g (0.328 mol) of 4-nitrophenyl chloroformate in 1.2 liters of CH2Cl2 was cooled to 0° C. and treated with L-valine methyl ester hydrochloride. The resulting mixture was treated slowly, with stirring, with 68.9 ml (0.626 mol) of 4-methylmorpholine. The resulting solution was allowed to slowly warm to ...
10.6084/m9.figshare.5104873.v1
null
Acyl halide.Ether.Primary amine
Carbamic ester
null
null
c1ccccc1
HCl
C(Cl)Cl
null
8
COC(=O)[C@@H](N)C(C)C.O=C(Cl)Oc1ccc([N+](=O)[O-])cc1>C(Cl)Cl>COC(=O)[C@@H](NC(=O)Oc1ccc([N+](=O)[O-])cc1)C(C)C
ord_dataset-c2ad1656a3ca4d08888ffb6e3f3a2742
ord-6d7205b94b6f456d88a89c4c418a3c7b
CNCc1csc(C(C)C)n1.COC(=O)[C@@H](NC(=O)Oc1ccc([N+](=O)[O-])cc1)C(C)C>>COC(=O)[C@@H](NC(=O)N(C)Cc1csc(C(C)C)n1)C(C)C
C(C)N(CC)CC.C(C)(C)C=1SC=C(N1)CNC.COC([C@@H](NC(=O)OC1=CC=C(C=C1)[N+](=O)[O-])C(C)C)=O>>COC([C@@H](NC(=O)N(CC=1N=C(SC1)C(C)C)C)C(C)C)=O
[NH:9]([CH3:10])[CH2:11][c:12]1[cH:13][s:14][c:15]([CH:16]([CH3:17])[CH3:18])[n:19]1.O=[N+]([O-])c1ccc(O[C:7]([NH:6][C@H:5]([C:3]([O:2][CH3:1])=[O:4])[CH:20]([CH3:21])[CH3:22])=[O:8])cc1>>[CH3:1][O:2][C:3](=[O:4])[C@@H:5]([NH:6][C:7](=[O:8])[N:9]([CH3:10])[CH2:11][c:12]1[cH:13][s:14][c:15]([CH:16]([CH3:17])[CH3:18])[n:...
CNCc1csc(C(C)C)n1.COC(=O)[C@@H](NC(=O)Oc1ccc([N+](=O)[O-])cc1)C(C)C
COC(=O)[C@@H](NC(=O)N(C)Cc1csc(C(C)C)n1)C(C)C
null
CN(C1=CC=NC=C1)C
C1CCOC1
Acylation
OtherReaction
e2d977a702ed644c57a3c6a03e066457d8dc73a51640ae48afb0cf24b6adf835
fc4b793bbeca2541e0488e7b2269d1dcbab20357be7785ff606aacdf4ebd8736
c1cscn1
O=[N+](-[O-])-c1:c:c:c(-O-[C;H0;D3;+0:1](=[O;D1;H0:2])-[#7:3]-[C:4]-[C:5](-[#8:6])=[O;D1;H0:7]):c:c:1.[#16;a:8]:[c:9]:[c:10](-[C:11]-[NH;D2;+0:12]-[C;D1;H3:13]):[#7;a:14]>>[#16;a:8]:[c:9]:[c:10](-[C:11]-[N;H0;D3;+0:12](-[C;D1;H3:13])-[C;H0;D3;+0:1](=[O;D1;H0:2])-[#7:3]-[C:4]-[C:5](-[#8:6])=[O;D1;H0:7]):[#7;a:14]
72.1
[{"value": 54.0, "product": "COC([C@@H](NC(=O)N(CC=1N=C(SC1)C(C)C)C)C(C)C)=O", "details": "PERCENTYIELD", "is_desired": false}, {"value": 72.1, "product": "COC([C@@H](NC(=O)N(CC=1N=C(SC1)C(C)C)C)C(C)C)=O", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
null
null
A solution of 15.7 g (92 mmol) of 2-isopropyl-4-(((N-methyl)amino)methyl)thiazole in 200 ml of THF was combined with a solution of 20.5 g (69 mmol) of N-(((4-nitrophenyl)oxy)carbonyl)-L-valine methyl ester. The resulting solution was treated with 1.6 g of 4-dimethylaminopyridine and 12.9 ml (92 mmol) of triethylamine, ...
10.6084/m9.figshare.5104873.v1
null
Carbamic ester.Ether.Nitro group.Secondary amine
Urea
c1ccccc1
null
c1cscn1
HO-
CN(C1=CC=NC=C1)C.C1CCOC1
null
null
CNCc1csc(C(C)C)n1.COC(=O)[C@@H](NC(=O)Oc1ccc([N+](=O)[O-])cc1)C(C)C>CN(C1=CC=NC=C1)C.C1CCOC1>COC(=O)[C@@H](NC(=O)N(C)Cc1csc(C(C)C)n1)C(C)C
ord_dataset-c2ad1656a3ca4d08888ffb6e3f3a2742
ord-5eae13859e80465a8960583cb560c9e2
COC(=O)[C@@H](NC(=O)N(C)Cc1csc(C(C)C)n1)C(C)C>>CC(C)c1nc(CN(C)C(=O)N[C@H](C(=O)O)C(C)C)cs1
Cl.COC([C@@H](NC(=O)N(CC=1N=C(SC1)C(C)C)C)C(C)C)=O.[Li+].[OH-]>>CN(CC=1N=C(SC1)C(C)C)C(=O)N[C@@H](C(C)C)C(=O)O
C[O:16][C:14]([C@@H:13]([NH:12][C:10]([N:8]([CH2:7][c:6]1[n:5][c:4]([CH:2]([CH3:1])[CH3:3])[s:21][cH:20]1)[CH3:9])=[O:11])[CH:17]([CH3:18])[CH3:19])=[O:15]>>[CH3:1][CH:2]([CH3:3])[c:4]1[n:5][c:6]([CH2:7][N:8]([CH3:9])[C:10](=[O:11])[NH:12][C@H:13]([C:14](=[O:15])[OH:16])[CH:17]([CH3:18])[CH3:19])[cH:20][s:21]1
COC(=O)[C@@H](NC(=O)N(C)Cc1csc(C(C)C)n1)C(C)C
CC(C)c1nc(CN(C)C(=O)N[C@H](C(=O)O)C(C)C)cs1
null
null
O1CCOCC1
Deprotection
Ester saponification (methyl deprotection)
d872e08ad5c85a4add6cd04e6e987e73fead5f79b3f30ba61a81ba5029b29894
38ae1ee78433b9acfb0390501446149c80f88f23ac2d84c60b3369bdab75cec9
c1cscn1
C-[O;H0;D2;+0:1]-[C:2](-[C:3])=[O;D1;H0:4]>>[C:3]-[C:2](=[O;D1;H0:4])-[OH;D1;+0:1]
81.6
[{"value": 81.0, "product": "CN(CC=1N=C(SC1)C(C)C)C(=O)N[C@@H](C(C)C)C(=O)O", "details": "PERCENTYIELD", "is_desired": false}, {"value": 81.6, "product": "CN(CC=1N=C(SC1)C(C)C)C(=O)N[C@@H](C(C)C)C(=O)O", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
30
MINUTE
A solution of 1.42 g (4.3 mmol) N-((N-methyl-N-((2-isopropyl-4-thiazolyl)methyl)amino)carbonyl)-L-valine methyl ester in 17 ml of dioxane was treated with 17.3 ml of 0.50M aqueous LiOH. The resulting solution was stirred at ambient temperature for 30 min, treated with 8.7 ml of 1M HCl, and concentrated in vacuo. The re...
10.6084/m9.figshare.5104873.v1
null
Ester
Carboxylic acid
null
null
c1cscn1
Other
O1CCOCC1
null
0.5
COC(=O)[C@@H](NC(=O)N(C)Cc1csc(C(C)C)n1)C(C)C>O1CCOCC1>CC(C)c1nc(CN(C)C(=O)N[C@H](C(=O)O)C(C)C)cs1
ord_dataset-c2ad1656a3ca4d08888ffb6e3f3a2742
ord-09967249e5c54fa28770a501c9324417
CCOC(=O)CCl.CCOC=O>>CCOC(=O)C(Cl)C=O
CC(C)([O-])C.[K+].ClCC(=O)OCC.C(=O)OCC.Cl>>ClC(C(=O)OCC)C=O
[CH3:1][CH2:2][O:3][C:4](=[O:5])[CH2:6][Cl:7].CCO[CH:8]=[O:9]>>[CH3:1][CH2:2][O:3][C:4](=[O:5])[CH:6]([Cl:7])[CH:8]=[O:9]
CCOC(=O)CCl.CCOC=O
CCOC(=O)C(Cl)C=O
null
null
C(C)OCC.C1CCOC1
C-C Coupling
OtherReaction
3fc0b57ea3d3da606fb4d103c3a7d45c1f7249c90fa5736c3093ee79b9f9e4ef
5f6d2dec246ebbf9bd8ff555f8e6b948874f1d470f439cfed67b1d917f8c57cb
null
C-C-O-[CH;D2;+0:1]=[O;D1;H0:2].[C:3]-[#8:4]-[C:5](=[O;D1;H0:6])-[CH2;D2;+0:7]-[Cl;D1;H0:8]>>[C:3]-[#8:4]-[C:5](=[O;D1;H0:6])-[CH;D3;+0:7](-[Cl;D1;H0:8])-[CH;D2;+0:1]=[O;D1;H0:2]
null
[]
0
CELSIUS
1
HOUR
To a three neck 2 L round bottom flask charged with potassium t-butoxide (0.5 mol, 500 mL of a 1M solution in THF) and 500 mL of dry THF cooled to 0° C. was added dropwise from an addition funnel a solution of ethyl chloroacetate (0.5 mol, 53.5 mL) and ethyl formate (0.5 mol, 40.4 mL), in 200 mL of THF over 3 hours. Af...
10.6084/m9.figshare.5104873.v1
null
Primary halide.Ester.Ether
Secondary halide.Aldehyde
null
null
null
HO-
C(C)OCC.C1CCOC1
0
1
CCOC(=O)CCl.CCOC=O>C(C)OCC.C1CCOC1>CCOC(=O)C(Cl)C=O
ord_dataset-c2ad1656a3ca4d08888ffb6e3f3a2742
ord-9ad27e36ea8a4245a799e896435ce5b9
CCOC(=O)C(Cl)C=O.NC=S>>CCOC(=O)c1cncs1
C(=S)N.ClC(C(=O)OCC)C=O>>S1C=NC=C1C(=O)OCC
O=[CH:7][CH:6](Cl)[C:4]([O:3][CH2:2][CH3:1])=[O:5].[NH2:8][CH:9]=[S:10]>>[CH3:1][CH2:2][O:3][C:4](=[O:5])[c:6]1[cH:7][n:8][cH:9][s:10]1
CCOC(=O)C(Cl)C=O.NC=S
CCOC(=O)c1cncs1
null
null
CC(=O)C
Aromatic Heterocycle Formation
OtherReaction
ca1a491634351402ba53e022aaddc0a4c7ec0639045153b7668e78d316c6754f
b332eb5ea501618d8dbac38c7e3242fcefa783e31f17b6ca5d4aaeb74530fc69
c1cscn1
Cl-[CH;D3;+0:1](-[CH;D2;+0:2]=O)-[C:3](=[O;D1;H0:4])-[#8:5]-[C:6].[NH2;D1;+0:7]-[CH;D2;+0:8]=[S;H0;D1;+0:9]>>[C:6]-[#8:5]-[C:3](=[O;D1;H0:4])-[c;H0;D3;+0:1]1:[cH;D2;+0:2]:[n;H0;D2;+0:7]:[cH;D2;+0:8]:[s;H0;D2;+0:9]:1
60
[{"value": 60.0, "product": "S1C=NC=C1C(=O)OCC", "details": "PERCENTYIELD", "is_desired": false}, {"value": 60.0, "product": "S1C=NC=C1C(=O)OCC", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
null
null
To a round bottom flask was added 250 mL of dry acetone, 7.5 g (0.123 mol) of thioformamide, and 18.54 g (0.123 mol) of ethyl 2-chloro-2-formylacetate. The reaction was heated at reflux for 2 hours. The solvent was removed in vacuo, and the residue was purified by chromatography (SiO2, 6 cm o.d. column, 100% CHCl3, Rf ...
10.6084/m9.figshare.5104873.v1
null
Secondary halide.Aldehyde.Ester.Thioamide
Ester
null
c1cscn1
c1cscn1
HCl
CC(=O)C
null
null
CCOC(=O)C(Cl)C=O.NC=S>CC(=O)C>CCOC(=O)c1cncs1
ord_dataset-c2ad1656a3ca4d08888ffb6e3f3a2742
ord-62b01f02baa24502b500f023bdca3e5a
O=C(Cl)Oc1ccc([N+](=O)[O-])cc1.OCc1cncs1>>O=C(OCc1cncs1)Oc1ccc([N+](=O)[O-])cc1
OCC1=CN=CS1.ClC(=O)OC1=CC=C(C=C1)[N+](=O)[O-]>>C1=CC(=CC=C1[N+](=O)[O-])OC(=O)OCC2=CN=CS2
Cl[C:2](=[O:1])[O:10][c:11]1[cH:12][cH:13][c:14]([N+:15](=[O:16])[O-:17])[cH:18][cH:19]1.[OH:3][CH2:4][c:5]1[cH:6][n:7][cH:8][s:9]1>>[O:1]=[C:2]([O:3][CH2:4][c:5]1[cH:6][n:7][cH:8][s:9]1)[O:10][c:11]1[cH:12][cH:13][c:14]([N+:15](=[O:16])[O-:17])[cH:18][cH:19]1
O=C(Cl)Oc1ccc([N+](=O)[O-])cc1.OCc1cncs1
O=C(OCc1cncs1)Oc1ccc([N+](=O)[O-])cc1
null
null
C(Cl)(Cl)Cl.C(Cl)Cl
Acylation
Schotten-Baumann to ester
c7a3e8873fc25f3519e40d98cf7a48f9e19cf51f2928c1b7217b087e636631b6
025f705bf83a5228860243b04919f20e0b9a7bfb249341effd2e1aa6465736d3
O=C(OCc1cncs1)Oc1ccccc1
Cl-[C;H0;D3;+0:1](=[O;D1;H0:2])-[#8:3]-[c:4].[#16;a:5]:[c:6](-[C:7]-[OH;D1;+0:8]):[c:9]:[#7;a:10]>>[#16;a:5]:[c:6](-[C:7]-[O;H0;D2;+0:8]-[C;H0;D3;+0:1](=[O;D1;H0:2])-[#8:3]-[c:4]):[c:9]:[#7;a:10]
78
[{"value": 78.0, "product": "C1=CC(=CC=C1[N+](=O)[O-])OC(=O)OCC2=CN=CS2", "details": "PERCENTYIELD", "is_desired": false}, {"value": 78.0, "product": "C1=CC(=CC=C1[N+](=O)[O-])OC(=O)OCC2=CN=CS2", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
1
HOUR
A solution of 3.11 g (27 mmol) of 5-(hydroxymethyl)thiazole and excess N-methyl morphcline in 100 ml of methylene chloride was cooled to 0° C. and treated with 8.2 g (41 mmol) of 4-nitrophenyl chloroformate. After being stirred for 1 h, the reaction mixture was diluted with CHCl3, washed successively with 1N HCl, satur...
10.6084/m9.figshare.5104873.v1
null
Acyl halide.Ether.Primary alcohol
Ether.Ether
null
null
c1cscn1.c1ccccc1
HCl
C(Cl)(Cl)Cl.C(Cl)Cl
null
1
O=C(Cl)Oc1ccc([N+](=O)[O-])cc1.OCc1cncs1>C(Cl)(Cl)Cl.C(Cl)Cl>O=C(OCc1cncs1)Oc1ccc([N+](=O)[O-])cc1
ord_dataset-c2ad1656a3ca4d08888ffb6e3f3a2742
ord-c32fd0fc0a484c6db081584442ac1344
CC(C)C(N)=O.O=C(CCl)CCl>>CC(C)C1=NC(O)(CCl)CO1
C(C(C)C)(=O)N.ClCC(=O)CCl.C(=O)(O)[O-].[Na+].[O-]S(=O)(=O)[O-].[Mg+2]>>ClCC1(N=C(OC1)C(C)C)O
[CH3:1][CH:2]([CH3:3])[C:4]([NH2:5])=[O:11].Cl[CH2:10][C:6](=[O:7])[CH2:8][Cl:9]>>[CH3:1][CH:2]([CH3:3])[C:4]1=[N:5][C:6]([OH:7])([CH2:8][Cl:9])[CH2:10][O:11]1
CC(C)C(N)=O.O=C(CCl)CCl
CC(C)C1=NC(O)(CCl)CO1
null
null
CC(=O)C
Acylation
OtherReaction
96b0c9b531b7ecf0c959da8409be7baafbdac9aad9b452ba4d5e43082e96ac79
8599b7dd32c3600e36d583ed13bb88d0962a835190be95a3561b48ff733289d8
C1=NCCO1
Cl-[CH2;D2;+0:1]-[C;H0;D3;+0:2](=[O;H0;D1;+0:3])-[C:4]-[Cl;D1;H0:5].[C;D1;H3:6]-[C:7](-[C;D1;H3:8])-[C;H0;D3;+0:9](-[NH2;D1;+0:10])=[O;H0;D1;+0:11]>>[C;D1;H3:6]-[C:7](-[C;D1;H3:8])-[C;H0;D3;+0:9]1=[N;H0;D2;+0:10]-[C;H0;D4;+0:2](-[OH;D1;+0:3])(-[C:4]-[Cl;D1;H0:5])-[CH2;D2;+0:1]-[O;H0;D2;+0:11]-1
46
[{"value": 46.0, "product": "ClCC1(N=C(OC1)C(C)C)O", "details": "PERCENTYIELD", "is_desired": false}, {"value": 45.6, "product": "ClCC1(N=C(OC1)C(C)C)O", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
null
null
To a solution of isobutyramide (9.876 g, 0.1122 mol)in acetone (130 mL) was added 1,3-dichloroacetone (10.0 g, 0.0748 mol), NaHCO3 (9.429 g, 0.1122 mol), and MgSO4 (18.01 g, 0.1496 mol). The mixture was heated at reflux under argon for 63 hrs, then cooled to room temperature, vacuum filtered, and concentrated in vacuo ...
10.6084/m9.figshare.5104873.v1
null
Primary halide.Ketone.Primary amide
Ether.Tertiary alcohol
null
C1=NCCO1
C1=NCCO1
HCl
CC(=O)C
null
null
CC(C)C(N)=O.O=C(CCl)CCl>CC(=O)C>CC(C)C1=NC(O)(CCl)CO1
ord_dataset-c2ad1656a3ca4d08888ffb6e3f3a2742
ord-5001dcc3f1c448c29ea30547f19ae029
CC(C)C1=NC(O)(CCl)CO1>>CC(C)c1nc(CCl)co1
ClCC1(N=C(OC1)C(C)C)O.O=S(Cl)Cl>>ClCC=1N=C(OC1)C(C)C
O[C:6]1([CH2:7][Cl:8])[N:5]=[C:4]([CH:2]([CH3:1])[CH3:3])[O:10][CH2:9]1>>[CH3:1][CH:2]([CH3:3])[c:4]1[n:5][c:6]([CH2:7][Cl:8])[cH:9][o:10]1
CC(C)C1=NC(O)(CCl)CO1
CC(C)c1nc(CCl)co1
null
null
ClCCCl
Aromatic Heterocycle Formation
OtherReaction
64419d6c7f4b17ce247ad9efaef19b4bef1aa2589b0263151d7cc8c07ae834f9
0058add5abc280cb9af66d568cb9bdb323ac1e806a9b79b330bb4ffe7b3d08f3
c1cocn1
O-[C;H0;D4;+0:1]1(-[C:2]-[Cl;D1;H0:3])-[CH2;D2;+0:4]-[O;H0;D2;+0:5]-[C;H0;D3;+0:6](-[C:7](-[C;D1;H3:8])-[C;D1;H3:9])=[N;H0;D2;+0:10]-1>>[C;D1;H3:8]-[C:7](-[C;D1;H3:9])-[c;H0;D3;+0:6]1:[n;H0;D2;+0:10]:[c;H0;D3;+0:1](-[C:2]-[Cl;D1;H0:3]):[cH;D2;+0:4]:[o;H0;D2;+0:5]:1
96
[{"value": 96.0, "product": "ClCC=1N=C(OC1)C(C)C", "details": "PERCENTYIELD", "is_desired": false}, {"value": 95.6, "product": "ClCC=1N=C(OC1)C(C)C", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
70
CELSIUS
15
MINUTE
A solution of 4-chloromethyl-4-hydroxy-2-isopropyloxazoline (4.88 g, 0.0275 mol) in 1,2-dichloroethane (20 mL) was added to a solution of SOCl2 (2.40 mL, 0.0329 mol) in 1,2-dichloroethane (80 mL) at 0° C. under argon, and the solution was heated to 70° C. After 15 min at 70° C., the reaction was cooled to room temperat...
10.6084/m9.figshare.5104873.v1
null
Ether.Tertiary alcohol
null
C1=NCCO1
c1cocn1
c1cocn1
HO-
ClCCCl
70
0.25
CC(C)C1=NC(O)(CCl)CO1>ClCCCl>CC(C)c1nc(CCl)co1
ord_dataset-c2ad1656a3ca4d08888ffb6e3f3a2742
ord-c0a1ae4aeb9043d29ee930653e08aad8
CC(C)c1nc(CCl)co1.CN>>CNCc1coc(C(C)C)n1
CN.ClCC=1N=C(OC1)C(C)C>>C(C)(C)C=1OC=C(N1)CNC
Cl[CH2:3][c:4]1[cH:5][o:6][c:7]([CH:8]([CH3:9])[CH3:10])[n:11]1.[CH3:1][NH2:2]>>[CH3:1][NH:2][CH2:3][c:4]1[cH:5][o:6][c:7]([CH:8]([CH3:9])[CH3:10])[n:11]1
CC(C)c1nc(CCl)co1.CN
CNCc1coc(C(C)C)n1
null
null
O1CCOCC1.O
Heteroatom Alkylation and Arylation
N-alkylation of primary amines with alkyl halides
fc19a1445ff204e66e51735d0191465bda3c6691fd233624a54742c9d4828411
0b1d32f56ad00f1e5bdae9390f9227bbea012fa2f8203aac34726b8a6761cc7c
c1cocn1
Cl-[CH2;D2;+0:1]-[c:2]1:[#7;a:3]:[c:4]:[#8;a:5]:[c:6]:1.[C;D1;H3:7]-[NH2;D1;+0:8]>>[C;D1;H3:7]-[NH;D2;+0:8]-[CH2;D2;+0:1]-[c:2]1:[#7;a:3]:[c:4]:[#8;a:5]:[c:6]:1
71
[{"value": 71.0, "product": "C(C)(C)C=1OC=C(N1)CNC", "details": "PERCENTYIELD", "is_desired": false}]
null
null
45
MINUTE
To 40% aqueous methylamine (100 mL) was added dropwise a suspension of 4-chloromethyl-2-isopropyloxazole (4.20 g, 0.0263 mol) in p-dioxane/H2O (1:1 (v/v), 20 mL) over a 25 min period. After stirring for 45 min at ambient temperature, the volume was reduced to ca. 50 mL by rotary evaporation in vacuo, and NaCl was added...
10.6084/m9.figshare.5104873.v1
null
Primary halide.Primary amine
Secondary amine
null
null
c1cocn1
HCl
O1CCOCC1.O
null
0.75
CC(C)c1nc(CCl)co1.CN>O1CCOCC1.O>CNCc1coc(C(C)C)n1
ord_dataset-c2ad1656a3ca4d08888ffb6e3f3a2742
ord-3e31ff1c1629400b83005281e5fe567b
CNCc1coc(C(C)C)n1.COC(=O)[C@@H](NC(=O)Oc1ccc([N+](=O)[O-])cc1)C(C)C>>COC(=O)[C@@H](NC(=O)N(C)Cc1coc(C(C)C)n1)C(C)C
COC([C@@H](NC(=O)OC1=CC=C(C=C1)[N+](=O)[O-])C(C)C)=O.C(C)(C)C=1OC=C(N1)CNC>>COC([C@@H](NC(=O)N(CC=1N=C(OC1)C(C)C)C)C(C)C)=O
[NH:9]([CH3:10])[CH2:11][c:12]1[cH:13][o:14][c:15]([CH:16]([CH3:17])[CH3:18])[n:19]1.O=[N+]([O-])c1ccc(O[C:7]([NH:6][C@H:5]([C:3]([O:2][CH3:1])=[O:4])[CH:20]([CH3:21])[CH3:22])=[O:8])cc1>>[CH3:1][O:2][C:3](=[O:4])[C@@H:5]([NH:6][C:7](=[O:8])[N:9]([CH3:10])[CH2:11][c:12]1[cH:13][o:14][c:15]([CH:16]([CH3:17])[CH3:18])[n:...
CNCc1coc(C(C)C)n1.COC(=O)[C@@H](NC(=O)Oc1ccc([N+](=O)[O-])cc1)C(C)C
COC(=O)[C@@H](NC(=O)N(C)Cc1coc(C(C)C)n1)C(C)C
null
null
CN(C)C=O
Acylation
OtherReaction
e2d977a702ed644c57a3c6a03e066457d8dc73a51640ae48afb0cf24b6adf835
fc4b793bbeca2541e0488e7b2269d1dcbab20357be7785ff606aacdf4ebd8736
c1cocn1
O=[N+](-[O-])-c1:c:c:c(-O-[C;H0;D3;+0:1](=[O;D1;H0:2])-[#7:3]-[C:4]-[C:5](-[#8:6])=[O;D1;H0:7]):c:c:1.[#7;a:8]:[c:9](-[C:10]-[NH;D2;+0:11]-[C;D1;H3:12]):[c:13]:[#8;a:14]>>[#7;a:8]:[c:9](-[C:10]-[N;H0;D3;+0:11](-[C;D1;H3:12])-[C;H0;D3;+0:1](=[O;D1;H0:2])-[#7:3]-[C:4]-[C:5](-[#8:6])=[O;D1;H0:7]):[c:13]:[#8;a:14]
54.1
[{"value": 54.0, "product": "COC([C@@H](NC(=O)N(CC=1N=C(OC1)C(C)C)C)C(C)C)=O", "details": "PERCENTYIELD", "is_desired": false}, {"value": 54.1, "product": "COC([C@@H](NC(=O)N(CC=1N=C(OC1)C(C)C)C)C(C)C)=O", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
30
MINUTE
A solution of N-(((4-nitrophenyl)oxy)carbonyl)-L-valine methyl ester (0.903 g, 0.00305 mol) in anhydrous DMF (6 mL) was added to a solution of 2-isopropyl-4-(((N-methyl)amino)methyl)oxazole (9, 0.470 g, 0.00305 mol) in anhydrous DMF (6 mL) under argon, and the yellow solution was stirred at room temperature for 30 min....
10.6084/m9.figshare.5104873.v1
null
Carbamic ester.Ether.Nitro group.Secondary amine
Urea
c1ccccc1
null
c1cocn1
HO-
CN(C)C=O
null
0.5
CNCc1coc(C(C)C)n1.COC(=O)[C@@H](NC(=O)Oc1ccc([N+](=O)[O-])cc1)C(C)C>CN(C)C=O>COC(=O)[C@@H](NC(=O)N(C)Cc1coc(C(C)C)n1)C(C)C
ord_dataset-c2ad1656a3ca4d08888ffb6e3f3a2742
ord-176ef9d7d5934107b54d7ee963182235
COC(=O)[C@@H](NC(=O)N(C)Cc1coc(C(C)C)n1)C(C)C>>CC(C)c1nc(CN(C)C(=O)N[C@H](C(=O)O)C(C)C)co1
COC([C@@H](NC(=O)N(CC=1N=C(OC1)C(C)C)C)C(C)C)=O>>CN(CC=1N=C(OC1)C(C)C)C(=O)N[C@@H](C(C)C)C(=O)O
C[O:16][C:14]([C@@H:13]([NH:12][C:10]([N:8]([CH2:7][c:6]1[n:5][c:4]([CH:2]([CH3:1])[CH3:3])[o:21][cH:20]1)[CH3:9])=[O:11])[CH:17]([CH3:18])[CH3:19])=[O:15]>>[CH3:1][CH:2]([CH3:3])[c:4]1[n:5][c:6]([CH2:7][N:8]([CH3:9])[C:10](=[O:11])[NH:12][C@H:13]([C:14](=[O:15])[OH:16])[CH:17]([CH3:18])[CH3:19])[cH:20][o:21]1
COC(=O)[C@@H](NC(=O)N(C)Cc1coc(C(C)C)n1)C(C)C
CC(C)c1nc(CN(C)C(=O)N[C@H](C(=O)O)C(C)C)co1
null
null
O1CCOCC1.O
Deprotection
Ester saponification (methyl deprotection)
d872e08ad5c85a4add6cd04e6e987e73fead5f79b3f30ba61a81ba5029b29894
38ae1ee78433b9acfb0390501446149c80f88f23ac2d84c60b3369bdab75cec9
c1cocn1
C-[O;H0;D2;+0:1]-[C:2](-[C:3])=[O;D1;H0:4]>>[C:3]-[C:2](=[O;D1;H0:4])-[OH;D1;+0:1]
98.2
[{"value": 98.0, "product": "CN(CC=1N=C(OC1)C(C)C)C(=O)N[C@@H](C(C)C)C(=O)O", "details": "PERCENTYIELD", "is_desired": false}, {"value": 98.2, "product": "CN(CC=1N=C(OC1)C(C)C)C(=O)N[C@@H](C(C)C)C(=O)O", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
1
HOUR
To a solution of N-((N-methyl-N-((2-isopropyl-4-oxazolyl)methyl)amino)carbonyl)-L-valine methyl ester 10 (0.511 g, 0.00164 mol) in p-dioxane (10 mL) and H2O (5 mL) was added LiOH monohydrate (0.103 g, 0.00246 mol). After stirring at room temperature for 1 hr, the p-dioxane was removed by rotary evaporation in vacuo, an...
10.6084/m9.figshare.5104873.v1
null
Ester
Carboxylic acid
null
null
c1cocn1
Other
O1CCOCC1.O
null
1
COC(=O)[C@@H](NC(=O)N(C)Cc1coc(C(C)C)n1)C(C)C>O1CCOCC1.O>CC(C)c1nc(CN(C)C(=O)N[C@H](C(=O)O)C(C)C)co1
ord_dataset-c2ad1656a3ca4d08888ffb6e3f3a2742
ord-58ee2bd126c54f2e9bb64ba134fc048c
C=CCC(O)CC.CCOC(=O)/C(Cl)=N\O>>CCOC(=O)C1=NOC(CCC(C)O)C1
C(C)N(CC)CC.C(C)OCC.OC(CC)CC=C.CCOC(=O)/C(=N\O)/Cl.C(C)OCC>>C(=O)(OCC)C1=NOC(C1)CCC(C)O
[CH2:9]=[CH:10][CH2:11][CH:12]([CH2:13][CH3:15])[OH:14].Cl/[C:6]([C:4]([O:3][CH2:2][CH3:1])=[O:5])=[N:7]/[OH:8]>>[CH3:1][CH2:2][O:3][C:4](=[O:5])[C:6]1=[N:7][O:8][CH:9]([CH2:10][CH2:11][CH:12]([CH3:13])[OH:14])[CH2:15]1
C=CCC(O)CC.CCOC(=O)/C(Cl)=N\O
CCOC(=O)C1=NOC(CCC(C)O)C1
null
null
null
Heteroatom Alkylation and Arylation
OtherReaction
5b6dad6070799c6f29fb7bc03432e54a0604aa32650a519a56da49e571e1dd2e
22f69b79f1e698a66982b9d19d867aa041819fe03d3879a2be18cee17c0b9833
C1=NOCC1
Cl/[C;H0;D3;+0:1](=[#7:2]/[OH;D1;+0:3])-[C:4](=[O;D1;H0:5])-[#8:6]-[C:7].[CH2;D1;+0:8]=[CH;D2;+0:9]-[C:10]-[C:11](-[O;D1;H1:12])-[CH2;D2;+0:13]-[CH3;D1;+0:14]>>[C:7]-[#8:6]-[C:4](=[O;D1;H0:5])-[C;H0;D3;+0:1]1=[#7:2]-[O;H0;D2;+0:3]-[CH;D3;+0:8](-[CH2;D2;+0:9]-[C:10]-[C:11](-[CH3;D1;+0:13])-[O;D1;H1:12])-[CH2;D2;+0:14]-1
null
[]
0
CELSIUS
null
null
To a solution of 6 g of 3-hydroxy-5-hexene in 150 ml of diethyl ether was added 18.1 g of ethyl chlorooximidoacetate. The solution was cooled to 0° C., and a solution of 21 ml of triethylamine in 210 ml of diethyl ether was added over 2.5 h. The amine hydrochloride salt was filtered and the residue was purified by sili...
10.6084/m9.figshare.5104873.v1
null
Alkenyl halide.Ester.Allyl.Oxime
Ester
null
C1=NOCC1
C1=NOCC1
HCl
null
0
null
C=CCC(O)CC.CCOC(=O)/C(Cl)=N\O>>CCOC(=O)C1=NOC(CCC(C)O)C1
ord_dataset-c2ad1656a3ca4d08888ffb6e3f3a2742
ord-a8c916b78d1346f5a0cda6c31c21aa14
C#CCOC1CCCCO1.CCOC(OCC)OCC>>CCOC(C#CCOC1CCCCO1)OCC
C(C)[Mg]Br.C1CCOC1.C(C#C)OC1OCCCC1.C(C)OC(OCC)OCC>>C(C)OC(C#CCOC1OCCCC1)OCC
[CH:5]#[C:6][CH2:7][O:8][CH:9]1[CH2:10][CH2:11][CH2:12][CH2:13][O:14]1.CCO[CH:4]([O:3][CH2:2][CH3:1])[O:15][CH2:16][CH3:17]>>[CH3:1][CH2:2][O:3][CH:4]([C:5]#[C:6][CH2:7][O:8][CH:9]1[CH2:10][CH2:11][CH2:12][CH2:13][O:14]1)[O:15][CH2:16][CH3:17]
C#CCOC1CCCCO1.CCOC(OCC)OCC
CCOC(C#CCOC1CCCCO1)OCC
null
null
C1(=CC=CC=C1)C
C-C Coupling
OtherReaction
5c785d27c44a43526fd7fdd77cfc98b0f959dd7c7f379a09a381a32824fc27db
6edbaa6dd32bc7980574a42cae4193d6efda2e147efbdfba916ce27407251dd7
C1CCOCC1
C-C-O-[CH;D3;+0:1](-[#8:2]-[C:3])-[#8:4]-[C:5].[C:6]-[C:7]#[CH;D1;+0:8]>>[C:3]-[#8:2]-[CH;D3;+0:1](-[#8:4]-[C:5])-[C;H0;D2;+0:8]#[C:7]-[C:6]
79
[{"value": 79.0, "product": "C(C)OC(C#CCOC1OCCCC1)OCC", "details": "PERCENTYIELD", "is_desired": false}]
null
null
4
HOUR
A 1M solution of ethylmagnesium bromide in THF (200 ml, 0.2 mol) was treated with 29 ml (0.2 mol) of a solution of 3,4,5,6-tetrahydro-2-(2-propynyloxy)-2H-pyran in toluene, while maintaining ambient temperature through use of a cool water bath. The resulting solution was stirred for 4 h and treated with 47 ml (0.28 mol...
10.6084/m9.figshare.5104873.v1
null
Ether.Ether.Ether.Alkyne
Ether.Ether.Alkyne
null
null
C1CCOCC1
HO-
C1(=CC=CC=C1)C
null
4
C#CCOC1CCCCO1.CCOC(OCC)OCC>C1(=CC=CC=C1)C>CCOC(C#CCOC1CCCCO1)OCC
ord_dataset-c2ad1656a3ca4d08888ffb6e3f3a2742
ord-94131f34c83b4b5ea02e7dfd9ab76786
CN(C)C(N)=S.O=C(CCl)CCl>>CN(C)c1nc(CCl)cs1
ClCC(=O)CCl.CN(C(=S)N)C.[O-]S(=O)(=O)[O-].[Mg+2]>>ClCC=1N=C(SC1)N(C)C
[CH3:1][N:2]([CH3:3])[C:4]([NH2:5])=[S:10].O=[C:6]([CH2:7][Cl:8])[CH2:9]Cl>>[CH3:1][N:2]([CH3:3])[c:4]1[n:5][c:6]([CH2:7][Cl:8])[cH:9][s:10]1
CN(C)C(N)=S.O=C(CCl)CCl
CN(C)c1nc(CCl)cs1
null
null
CC(=O)C
Aromatic Heterocycle Formation
OtherReaction
bef473efef1d9ea696235ac9e0e73338149dac4bc5d824d8ecb15263a8e3a4b0
39fbe568f79251ca2d63e869c3b1ee705fef7458c6d99863e8f91d4da02df595
c1cscn1
Cl-[CH2;D2;+0:1]-[C;H0;D3;+0:2](=O)-[C:3]-[Cl;D1;H0:4].[C;D1;H3:5]-[#7:6](-[C;D1;H3:7])-[C;H0;D3;+0:8](-[NH2;D1;+0:9])=[S;H0;D1;+0:10]>>[C;D1;H3:5]-[#7:6](-[C;D1;H3:7])-[c;H0;D3;+0:8]1:[n;H0;D2;+0:9]:[c;H0;D3;+0:2](-[C:3]-[Cl;D1;H0:4]):[cH;D2;+0:1]:[s;H0;D2;+0:10]:1
70
[{"value": 70.0, "product": "ClCC=1N=C(SC1)N(C)C", "details": "PERCENTYIELD", "is_desired": false}, {"value": 55.0, "product": "ClCC=1N=C(SC1)N(C)C", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
null
null
A mixture of 15 g (144 mmol) of N,N-dimethylthiourea and excess MgSO4 in 350 ml of acetone was heated to reflux and treated dropwise with a solution of 18.3 g (144 mmol) of 1,3-dichloroacetone in 35 ml of acetone. The resulting mixture was heated at reflux for 1.5 h, allowed to cool, filtered, and concentrated in vacuo...
10.6084/m9.figshare.5104873.v1
null
Primary halide.Ketone.Thiourea
null
null
c1cscn1
c1cscn1
HCl
CC(=O)C
null
null
CN(C)C(N)=S.O=C(CCl)CCl>CC(=O)C>CN(C)c1nc(CCl)cs1
ord_dataset-c2ad1656a3ca4d08888ffb6e3f3a2742
ord-ebd74e6522cb40efa3214dae18c5b7b6
CN(C)c1nc(CCl)cs1.O>>CN(C)c1nc(CO)cs1
C1CCOC1.O.ClCC=1N=C(SC1)N(C)C.C1CCOC1.O>>CN(C)C=1SC=C(N1)CO
Cl[CH2:7][c:6]1[n:5][c:4]([N:2]([CH3:1])[CH3:3])[s:10][cH:9]1.[OH2:8]>>[CH3:1][N:2]([CH3:3])[c:4]1[n:5][c:6]([CH2:7][OH:8])[cH:9][s:10]1
CN(C)c1nc(CCl)cs1.O
CN(C)c1nc(CO)cs1
null
F[B-](F)(F)F.[Ag+]
null
Heteroatom Alkylation and Arylation
OtherReaction
231253c55c0f42174a17340b823c6702155eb165c3d2f7b555bb09f54b91b1a3
e7141d94960d4874394ef66bcefdd72176a955fa44e71bb38bf7656b1bd4e11a
c1cscn1
Cl-[CH2;D2;+0:1]-[c:2]1:[#7;a:3]:[c:4]:[#16;a:5]:[c:6]:1.[OH2;D0;+0:7]>>[OH;D1;+0:7]-[CH2;D2;+0:1]-[c:2]1:[#7;a:3]:[c:4]:[#16;a:5]:[c:6]:1
null
[]
null
null
1
HOUR
A solution of 5.186 g (29 mmol) of 4-(chloromethyl)-2-(dimethylamino)thiazole in 100 ml of 1:1 THF/H2O was cooled to 0° C. and treated dropwise with a solution of 5.73 g (29 mmol) of silver tetrafluoroborate in 50 ml of 1:1 THF/H2O. After being stirred for 1 h, the mixture was filtered, the solid mass was washed with e...
10.6084/m9.figshare.5104873.v1
null
Primary halide
Primary alcohol
null
null
c1cscn1
HCl
F[B-](F)(F)F.[Ag+]
null
1
CN(C)c1nc(CCl)cs1.O>F[B-](F)(F)F.[Ag+]>CN(C)c1nc(CO)cs1
ord_dataset-c2ad1656a3ca4d08888ffb6e3f3a2742
ord-00a13d5c9a94459f9f294cd9c829351b
CN(C)c1nc(CO)cs1.COC(=O)[C@](N)(N=C=O)C(C)C>>COC(=O)[C@@H](NC(=O)OCc1csc(N(C)C)n1)C(C)C
CN(C)C=1SC=C(N1)CO.COC([C@@](N)(C(C)C)N=C=O)=O>>COC([C@@H](NC(=O)OCC=1N=C(SC1)N(C)C)C(C)C)=O
[OH:9][CH2:10][c:11]1[cH:12][s:13][c:14]([N:15]([CH3:16])[CH3:17])[n:18]1.N[C@@:5]([C:3]([O:2][CH3:1])=[O:4])([N:6]=[C:7]=[O:8])[CH:19]([CH3:20])[CH3:21]>>[CH3:1][O:2][C:3](=[O:4])[C@@H:5]([NH:6][C:7](=[O:8])[O:9][CH2:10][c:11]1[cH:12][s:13][c:14]([N:15]([CH3:16])[CH3:17])[n:18]1)[CH:19]([CH3:20])[CH3:21]
CN(C)c1nc(CO)cs1.COC(=O)[C@](N)(N=C=O)C(C)C
COC(=O)[C@@H](NC(=O)OCc1csc(N(C)C)n1)C(C)C
null
CN(C1=CC=NC=C1)C
ClCCl
Functional Group Interconversion
OtherReaction
a23be472936c50c173c2dd2734289c9dfae50efca7ef50b8a0cb8898e49c8803
594e835804772a869b7a162be980a733776c00b82a87e4b097f0a7da7fddd8e1
c1cscn1
N-[C@@;H0;D4;+0:1](-[N;H0;D2;+0:2]=[C;H0;D2;+0:3]=[O;D1;H0:4])(-[C:5](-[C;D1;H3:6])-[C;D1;H3:7])-[C:8](=[O;D1;H0:9])-[#8:10]-[C;D1;H3:11].[#16;a:12]:[c:13]:[c:14](-[C:15]-[OH;D1;+0:16]):[#7;a:17]>>[#16;a:12]:[c:13]:[c:14](-[C:15]-[O;H0;D2;+0:16]-[C;H0;D3;+0:3](=[O;D1;H0:4])-[NH;D2;+0:2]-[C@@H;D3;+0:1](-[C:5](-[C;D1;H3:...
95
[{"value": 95.0, "product": "COC([C@@H](NC(=O)OCC=1N=C(SC1)N(C)C)C(C)C)=O", "details": "PERCENTYIELD", "is_desired": false}, {"value": 94.4, "product": "COC([C@@H](NC(=O)OCC=1N=C(SC1)N(C)C)C(C)C)=O", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
null
null
A solution of 505 mg (3.19 mmol) of 2-(N,N-dimethylamino)-4-(hydroxymethyl)thiazole, 3.19 mmol of α-isocyanato-L-valine methyl ester, and 100 mg of 4-dimethylaminopyridine in 30 ml of dichloromethane was heated at reflux for 3 h. The resulting solution was allowed to cool, diluted with dichloromethane, washed sequentia...
10.6084/m9.figshare.5104873.v1
null
Ester.Isocyanate.Primary alcohol.Primary amine
Carbamic ester.Ester
null
null
c1cscn1
Other
CN(C1=CC=NC=C1)C.ClCCl
null
null
CN(C)c1nc(CO)cs1.COC(=O)[C@](N)(N=C=O)C(C)C>CN(C1=CC=NC=C1)C.ClCCl>COC(=O)[C@@H](NC(=O)OCc1csc(N(C)C)n1)C(C)C
ord_dataset-c2ad1656a3ca4d08888ffb6e3f3a2742
ord-bb97273c68bf445e929cb09da7acb2ff
CCOC(=O)C(=O)CBr.NC(=S)N1CCOCC1>>CCOC(=O)c1csc(N2CCOCC2)n1
NC(=S)N1CCOCC1.BrCC(C(=O)OCC)=O.[O-]S(=O)(=O)[O-].[Mg+2]>>N1(CCOCC1)C=1SC=C(N1)C(=O)OCC
O=[C:6]([C:4]([O:3][CH2:2][CH3:1])=[O:5])[CH2:7]Br.[S:8]=[C:9]([N:10]1[CH2:11][CH2:12][O:13][CH2:14][CH2:15]1)[NH2:16]>>[CH3:1][CH2:2][O:3][C:4](=[O:5])[c:6]1[cH:7][s:8][c:9]([N:10]2[CH2:11][CH2:12][O:13][CH2:14][CH2:15]2)[n:16]1
CCOC(=O)C(=O)CBr.NC(=S)N1CCOCC1
CCOC(=O)c1csc(N2CCOCC2)n1
null
null
CC(=O)C
Aromatic Heterocycle Formation
OtherReaction
2acf8b62928feda0eec79ae390961e4e289c4aabc8d6caf6e6ddc0eda363b75d
86bbdfdfc5fa521b3981982705c3355aa8731992aa62c549aa1ec0eef245e5b9
c1csc(N2CCOCC2)n1
Br-[CH2;D2;+0:1]-[C;H0;D3;+0:2](=O)-[C:3](=[O;D1;H0:4])-[#8:5]-[C:6].[C:7]-[#7:8](-[C;H0;D3;+0:9](-[NH2;D1;+0:10])=[S;H0;D1;+0:11])-[C:12]>>[C:7]-[#7:8](-[c;H0;D3;+0:9]1:[n;H0;D2;+0:10]:[c;H0;D3;+0:2](-[C:3](=[O;D1;H0:4])-[#8:5]-[C:6]):[cH;D2;+0:1]:[s;H0;D2;+0:11]:1)-[C:12]
55.2
[{"value": 55.0, "product": "N1(CCOCC1)C=1SC=C(N1)C(=O)OCC", "details": "PERCENTYIELD", "is_desired": false}, {"value": 55.2, "product": "N1(CCOCC1)C=1SC=C(N1)C(=O)OCC", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
null
null
A mixture of 1.85 g (12.7 mmol) of 4-((amino)thiocarbonyl)morpholine, 1.59 ml (12.7 mmol) of ethyl bromopyruvate, and excess MgSO4 in 50 ml of acetone was heated at reflux for 2 h. The resulting mixture was allowed to cool, filtered, and concentrated in vacuo. The residue was taken up in chloroform, washed with aqueous...
10.6084/m9.figshare.5104873.v1
null
Primary halide.Ketone.Ester.Thiourea
Ester
null
c1cscn1
c1cscn1.C1COCC[NH]1
HBr
CC(=O)C
null
null
CCOC(=O)C(=O)CBr.NC(=S)N1CCOCC1>CC(=O)C>CCOC(=O)c1csc(N2CCOCC2)n1
ord_dataset-c2ad1656a3ca4d08888ffb6e3f3a2742
ord-7d854e66a30d4598ba3f260d83acb5fa
CCOC(=O)c1csc(N2CCOCC2)n1>>OCc1csc(N2CCOCC2)n1
[H-].[Al+3].[Li+].[H-].[H-].[H-].N1(CCOCC1)C=1SC=C(N1)C(=O)OCC>>N1(CCOCC1)C=1SC=C(N1)CO
CCO[C:2](=[O:1])[c:3]1[cH:4][s:5][c:6]([N:7]2[CH2:8][CH2:9][O:10][CH2:11][CH2:12]2)[n:13]1>>[OH:1][CH2:2][c:3]1[cH:4][s:5][c:6]([N:7]2[CH2:8][CH2:9][O:10][CH2:11][CH2:12]2)[n:13]1
CCOC(=O)c1csc(N2CCOCC2)n1
OCc1csc(N2CCOCC2)n1
null
null
C1(=CC=CC=C1)C.C1CCOC1
Reduction
Reduction of ester to primary alcohol
21d61543c6ec8a8cebe1b3ef55ef3dd20acbf79a4f1c12a7fb51e32be7a3248a
1fbcd628a0426673c5d10aa49a977cd2d1ae02a8cdf57bbb10d94aa03a94e937
c1csc(N2CCOCC2)n1
C-C-O-[C;H0;D3;+0:1](=[O;H0;D1;+0:2])-[c:3]1:[#7;a:4]:[c:5]:[#16;a:6]:[c:7]:1>>[OH;D1;+0:2]-[CH2;D2;+0:1]-[c:3]1:[#7;a:4]:[c:5]:[#16;a:6]:[c:7]:1
61.1
[{"value": 61.0, "product": "N1(CCOCC1)C=1SC=C(N1)CO", "details": "PERCENTYIELD", "is_desired": false}, {"value": 61.1, "product": "N1(CCOCC1)C=1SC=C(N1)CO", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
0
CELSIUS
1
HOUR
A solution of 7.0 ml (7.0 mmol) of lithium aluminum hydride in toluene was diluted with 10 ml of THF, cooled to 0° C., and treated with a solution of 1.7 g (7.0 mmol) of ethyl 2-(4-morpholinyl)thiazole-4-carboxylate in 25 ml of THF. The resulting solution was stirred for 1 h, quenched cautiously with aqueous Rochelle's...
10.6084/m9.figshare.5104873.v1
null
Ester
Primary alcohol
null
null
c1cscn1.C1COCC[NH]1
HO-
C1(=CC=CC=C1)C.C1CCOC1
0
1
CCOC(=O)c1csc(N2CCOCC2)n1>C1(=CC=CC=C1)C.C1CCOC1>OCc1csc(N2CCOCC2)n1
ord_dataset-c2ad1656a3ca4d08888ffb6e3f3a2742
ord-4fd6ba6668b04b55b557b83207267fa9
CCOC(=O)c1csc(N2CCCC2)n1>>OCc1csc(N2CCCC2)n1
N1(CCCC1)C=1SC=C(N1)C(=O)OCC.CO>>N1(CCCC1)C=1SC=C(N1)CO
CCO[C:2](=[O:1])[c:3]1[cH:4][s:5][c:6]([N:7]2[CH2:8][CH2:9][CH2:10][CH2:11]2)[n:12]1>>[OH:1][CH2:2][c:3]1[cH:4][s:5][c:6]([N:7]2[CH2:8][CH2:9][CH2:10][CH2:11]2)[n:12]1
CCOC(=O)c1csc(N2CCCC2)n1
OCc1csc(N2CCCC2)n1
null
null
C(Cl)(Cl)Cl
Reduction
Reduction of ester to primary alcohol
21d61543c6ec8a8cebe1b3ef55ef3dd20acbf79a4f1c12a7fb51e32be7a3248a
1fbcd628a0426673c5d10aa49a977cd2d1ae02a8cdf57bbb10d94aa03a94e937
c1csc(N2CCCC2)n1
C-C-O-[C;H0;D3;+0:1](=[O;H0;D1;+0:2])-[c:3]1:[#7;a:4]:[c:5]:[#16;a:6]:[c:7]:1>>[OH;D1;+0:2]-[CH2;D2;+0:1]-[c:3]1:[#7;a:4]:[c:5]:[#16;a:6]:[c:7]:1
4
[{"value": 4.0, "product": "N1(CCCC1)C=1SC=C(N1)CO", "details": "PERCENTYIELD", "is_desired": false}]
null
null
null
null
Using the procedure of Example 23C but replacing ethyl 2-(4-morpholinyl)thiazole-4-carboxylate with ethyl 2-(1-pyrrolidinyl)thiazole-4-carboxylate provided, after silica gel chromatography using 2-4% methanol in chloroform, the desired compound (Rf 0.26, 4% methanol in chloroform) in 53% yield. 1H NMR (CDCl3) δ2.04 (m,...
10.6084/m9.figshare.5104873.v1
null
Ester
Primary alcohol
null
null
c1cscn1.C1CC[NH]C1
HO-
C(Cl)(Cl)Cl
null
null
CCOC(=O)c1csc(N2CCCC2)n1>C(Cl)(Cl)Cl>OCc1csc(N2CCCC2)n1
ord_dataset-c2ad1656a3ca4d08888ffb6e3f3a2742
ord-b61ac108471143a1be239e5bce7d401e
CC(C)[C@@](N)(N=C=O)C(=O)O.CNCc1csc(N(C)C)n1>>COC(=O)[C@@H](NC(=O)N(C)Cc1csc(N(C)C)n1)C(C)C
N(=C=O)[C@](N)(C(C)C)C(=O)O.CN(C)C=1SC=C(N1)CNC.ClCCl.ClCCl>>COC([C@@H](NC(=O)N(CC=1N=C(SC1)N(C)C)C)C(C)C)=O
N[C@@:5]([C:3]([OH:2])=[O:4])([N:6]=[C:7]=[O:8])[CH:20]([CH3:21])[CH3:22].[NH:9]([CH3:10])[CH2:11][c:12]1[cH:13][s:14][c:15]([N:16]([CH3:17])[CH3:18])[n:19]1>>[CH3:1][O:2][C:3](=[O:4])[C@@H:5]([NH:6][C:7](=[O:8])[N:9]([CH3:10])[CH2:11][c:12]1[cH:13][s:14][c:15]([N:16]([CH3:17])[CH3:18])[n:19]1)[CH:20]([CH3:21])[CH3:22]
CC(C)[C@@](N)(N=C=O)C(=O)O.CNCc1csc(N(C)C)n1
COC(=O)[C@@H](NC(=O)N(C)Cc1csc(N(C)C)n1)C(C)C
null
null
null
Functional Group Interconversion
OtherReaction
c380c012b5fe53dd6cd702dc61e4967ea3c8f8e7c8428aa9fc563de56876cc9c
91a4ee2356b16742374f8224db1dc3afc61c8fe99d0b1285b4d7465b0deb162f
c1cscn1
N-[C@@;H0;D4;+0:1](-[N;H0;D2;+0:2]=[C;H0;D2;+0:3]=[O;D1;H0:4])(-[C:5](-[C;D1;H3:6])-[C;D1;H3:7])-[C:8](=[O;D1;H0:9])-[OH;D1;+0:10].[#16;a:11]:[c:12]:[c:13](-[C:14]-[NH;D2;+0:15]-[C;D1;H3:16]):[#7;a:17]>>[#16;a:11]:[c:12]:[c:13](-[C:14]-[N;H0;D3;+0:15](-[C;D1;H3:16])-[C;H0;D3;+0:3](=[O;D1;H0:4])-[NH;D2;+0:2]-[C@@H;D3;+0...
34
[{"value": 34.0, "product": "COC([C@@H](NC(=O)N(CC=1N=C(SC1)N(C)C)C)C(C)C)=O", "details": "PERCENTYIELD", "is_desired": false}]
null
null
16
HOUR
A solution of 741 mg (4.42 mmol) of α-isocyanato-L-valine in in 5 ml of dichloromethane was added to a solution of 720 mg (4.21 mmol) of 2-(N,N-dimethylamino)-4-(((N-methyl)amino)methyl)thiazole in 25 ml of dichloromethane. The resulting solution was stirred at ambient temperature for 16 h, partitioned between chlorofo...
10.6084/m9.figshare.5104873.v1
null
Carboxylic acid.Isocyanate.Primary amine.Secondary amine
Ester.Urea
null
null
c1cscn1
null
null
null
16
CC(C)[C@@](N)(N=C=O)C(=O)O.CNCc1csc(N(C)C)n1>>COC(=O)[C@@H](NC(=O)N(C)Cc1csc(N(C)C)n1)C(C)C
ord_dataset-c2ad1656a3ca4d08888ffb6e3f3a2742
ord-f7583450d6ad4da3b8ea9914bcf7f117
C#CCOC1CCCCO1.CC(C)C(=O)Cl>>CC(C)C(=O)C#CCOC1CCCCO1
C(C(C)C)(=O)Cl.C(C#C)OC1OCCCC1>>CC(C(C#CCOC1OCCCC1)=O)C
[CH:6]#[C:7][CH2:8][O:9][CH:10]1[CH2:11][CH2:12][CH2:13][CH2:14][O:15]1.Cl[C:4]([CH:2]([CH3:1])[CH3:3])=[O:5]>>[CH3:1][CH:2]([CH3:3])[C:4](=[O:5])[C:6]#[C:7][CH2:8][O:9][CH:10]1[CH2:11][CH2:12][CH2:13][CH2:14][O:15]1
C#CCOC1CCCCO1.CC(C)C(=O)Cl
CC(C)C(=O)C#CCOC1CCCCO1
null
null
null
C-C Coupling
OtherReaction
a6f0b2b4226aa44d92013aea18c387b08c35f5add226dac668d88084e9d68d79
8ba6b48924727c95ba5477874811455682753922dd7cd313d89aad2a979363dd
C1CCOCC1
Cl-[C;H0;D3;+0:1](=[O;D1;H0:2])-[C:3](-[C;D1;H3:4])-[C;D1;H3:5].[C:6]-[C:7]#[CH;D1;+0:8]>>[C:6]-[C:7]#[C;H0;D2;+0:8]-[C;H0;D3;+0:1](=[O;D1;H0:2])-[C:3](-[C;D1;H3:4])-[C;D1;H3:5]
null
[]
null
null
null
null
The desired compound was prepared from isobutyryl chloride and 3,4,5,6-tetrahydro-2-(2-propynyloxy)-2H-pyran by analogy to the procedure of Tohda, et. al. (Synthesis, 777 (1977)). Conditions: See reaction.notes.procedure_details.
10.6084/m9.figshare.5104873.v1
null
Acyl halide.Alkyne
Ketone
null
null
C1CCOCC1
HCl
null
null
null
C#CCOC1CCCCO1.CC(C)C(=O)Cl>>CC(C)C(=O)C#CCOC1CCCCO1
ord_dataset-c2ad1656a3ca4d08888ffb6e3f3a2742
ord-387912939de7416b9e56f5247a2569aa
CC(=O)OC(C)=O.CC1(C)C=CC=CC1CCO>>CC(=O)OCCC1C=CC=CC1(C)C
CC1(C(CCO)C=CC=C1)C.C(C)(=O)OC(C)=O>>C(C)(=O)OCCC1C(C=CC=C1)(C)C
CC(=O)O[C:2]([CH3:1])=[O:3].[OH:4][CH2:5][CH2:6][CH:7]1[CH:8]=[CH:9][CH:10]=[CH:11][C:12]1([CH3:13])[CH3:14]>>[CH3:1][C:2](=[O:3])[O:4][CH2:5][CH2:6][CH:7]1[CH:8]=[CH:9][CH:10]=[CH:11][C:12]1([CH3:13])[CH3:14]
CC(=O)OC(C)=O.CC1(C)C=CC=CC1CCO
CC(=O)OCCC1C=CC=CC1(C)C
null
null
N1=CC=CC=C1
Acylation
Transesterification
f81e513b7b512b10157c16426844efd8d88e34c97987c1347c6ba8a688351205
fc27d67c790d5fb520ba5d49de1490661fa5b822b714863734ce7e3029dfa84f
C1=CCCC=C1
C-C(=O)-O-[C;H0;D3;+0:1](-[C;D1;H3:2])=[O;D1;H0:3].[C:4]-[C:5]-[OH;D1;+0:6]>>[C:4]-[C:5]-[O;H0;D2;+0:6]-[C;H0;D3;+0:1](-[C;D1;H3:2])=[O;D1;H0:3]
null
[]
null
null
8
HOUR
Dissolve 2,2-dimethylphenethyl alcohol (118.0 g, 0.786 mol) in pyridine (700 mL). Add, by dropwise addition, acetic anhydride (222 mL, 240.7 g, 2.358 mol) and stir overnight at room temperature. Evaporate the solvent in vacuo and purify by distillation to give the title compound as a clear colorless oil; bp 75° C. @ 0....
10.6084/m9.figshare.5104873.v1
null
Anhydride.Primary alcohol
Ester
null
null
C1=CCCC=C1
HO-
N1=CC=CC=C1
null
8
CC(=O)OC(C)=O.CC1(C)C=CC=CC1CCO>N1=CC=CC=C1>CC(=O)OCCC1C=CC=CC1(C)C