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-018fd0e1351f4fd09b20fcddd97b4c7a
ord-889f87317a184fe882398292d773dda7
COC(=O)CCC(=O)OC.COC(=O)c1cccc(Cl)c1>>O=C(O)CCC(=O)c1cccc(Cl)c1
C(CCC(=O)OC)(=O)OC.[Na].C(C)O.ClC=1C=C(C(=O)OC)C=CC1.C(CCC(=O)OC)(=O)OC>>ClC=1C=C(C(=O)CCC(=O)O)C=CC1
COC(=O)[CH2:5][CH2:4][C:2](=[O:1])[O:3]C.CO[C:6](=[O:7])[c:8]1[cH:9][cH:10][cH:11][c:12]([Cl:13])[cH:14]1>>[O:1]=[C:2]([OH:3])[CH2:4][CH2:5][C:6](=[O:7])[c:8]1[cH:9][cH:10][cH:11][c:12]([Cl:13])[cH:14]1
COC(=O)CCC(=O)OC.COC(=O)c1cccc(Cl)c1
O=C(O)CCC(=O)c1cccc(Cl)c1
null
null
CCOCC
C-C Coupling
OtherReaction
6d482de2a0c1fffe47581cf2d6dc0eefca79628574252eec326be9292f335afe
1f69704fe402a3eb0e91a243a59f68f972592be61b4c787368515903d4c85726
c1ccccc1
C-O-C(=O)-[CH2;D2;+0:1]-[C:2]-[C:3](=[O;D1;H0:4])-[O;H0;D2;+0:5]-C.C-O-[C;H0;D3;+0:6](=[O;D1;H0:7])-[c:8](:[c:9]):[c:10]>>[O;D1;H0:4]=[C:3](-[OH;D1;+0:5])-[C:2]-[CH2;D2;+0:1]-[C;H0;D3;+0:6](=[O;D1;H0:7])-[c:8](:[c:9]):[c:10]
null
[]
null
null
null
null
Sodium (11 g, spheres) was added to 200 ml ethanol with stirring. When the gas evolution ceased, methyl 3-chlorobenzoate (10 g, 0.057 mole) and dimethyl succinate (9.0 g, 0.615 mole) were added rapidly and the mixture was stirred for 5 minutes at room temperature. The mixture was slowly concentrated on a rotary evapora...
10.6084/m9.figshare.5104873.v1
null
Ester.Ester.Ester
Carboxylic acid.Ketone
null
null
c1ccccc1
HO-
CCOCC
null
null
COC(=O)CCC(=O)OC.COC(=O)c1cccc(Cl)c1>CCOCC>O=C(O)CCC(=O)c1cccc(Cl)c1
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-4107cbb9265542ed86297db6dd6b41b9
Cc1ccc(C(=O)CCC(=O)O)cc1.ClCl>>Cc1c(Cl)cc(C(=O)CCC(=O)O)cc1Cl
CC1=CC=C(C(=O)CCC(=O)O)C=C1.[Cl-].[Al+3].[Cl-].[Cl-].ClCl>>ClC=1C=C(C(=O)CCC(=O)O)C=C(C1C)Cl
[CH3:1][c:2]1[cH:3][cH:5][c:6]([C:7](=[O:8])[CH2:9][CH2:10][C:11](=[O:12])[OH:13])[cH:14][cH:15]1.[Cl:4][Cl:16]>>[CH3:1][c:2]1[c:3]([Cl:4])[cH:5][c:6]([C:7](=[O:8])[CH2:9][CH2:10][C:11](=[O:12])[OH:13])[cH:14][c:15]1[Cl:16]
Cc1ccc(C(=O)CCC(=O)O)cc1.ClCl
Cc1c(Cl)cc(C(=O)CCC(=O)O)cc1Cl
null
null
C(Cl)Cl
Miscellaneous
OtherReaction
d2a751fe92dcfde720edd5e4971c1aa6cc149bff4a6d230cc6b5cac59ec9498c
861258def4b3bd7367f8a87cde43fe585d40dc3669ea29055dbcb9a2de101a4d
c1ccccc1
[C;D1;H3:1]-[c:2]1:[cH;D2;+0:3]:[c:4]:[c:5](-[C:6]=[O;D1;H0:7]):[c:8]:[cH;D2;+0:9]:1.[Cl;H0;D1;+0:10]-[Cl;H0;D1;+0:11]>>[C;D1;H3:1]-[c:2]1:[c;H0;D3;+0:3](-[Cl;H0;D1;+0:10]):[c:4]:[c:5](-[C:6]=[O;D1;H0:7]):[c:8]:[c;H0;D3;+0:9]:1-[Cl;H0;D1;+0:11]
44.2
[{"value": 44.2, "product": "ClC=1C=C(C(=O)CCC(=O)O)C=C(C1C)Cl", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
null
null
To a mixture of 3-(4-methylbenzoyl)propionic acid (7.5 g) and methylene chloride (250 ml) was added slowly portionwise aluminum chloride (15 g) at 0° C. After the addition was completed chlorine gas was bubbled in slowly at 0° C. After 6 hours the reaction mixture was poured into a mixture of hydrochloric acid and ice ...
10.6084/m9.figshare.5104873.v1
null
null
Aromatic halide.Aromatic halide
c1ccccc1
c1ccccc1
c1ccccc1
null
C(Cl)Cl
null
null
Cc1ccc(C(=O)CCC(=O)O)cc1.ClCl>C(Cl)Cl>Cc1c(Cl)cc(C(=O)CCC(=O)O)cc1Cl
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-5e3cc0d24c92424b96fce5ec22cba17e
C1=COCCC1.OCC#CCO>>OCC#CCOC1CCCCO1
C(C#CCO)O.O1CCCC=C1>>O1C(CCCC1)OCC#CCO
[CH:7]1=[CH:8][CH2:9][CH2:10][CH2:11][O:12]1.[OH:1][CH2:2][C:3]#[C:4][CH2:5][OH:6]>>[OH:1][CH2:2][C:3]#[C:4][CH2:5][O:6][CH:7]1[CH2:8][CH2:9][CH2:10][CH2:11][O:12]1
C1=COCCC1.OCC#CCO
OCC#CCOC1CCCCO1
null
null
CCOCC
Heteroatom Alkylation and Arylation
oxa-Michael addition
abdcab389770d0a73be3b825aa1d56cee234da38dbdf3510fe8104d481e7cf3f
c6a3efa2acb508a32cdf9fcedfcd9635cce0ecdcf12c094b743aa576ea01fd9a
C1CCOCC1
[#8:1]1-[C:2]-[C:3]-[C:4]-[CH;D2;+0:5]=[CH;D2;+0:6]-1.[C:7]-[C:8]#[C:9]-[C:10]-[OH;D1;+0:11]>>[C:7]-[C:8]#[C:9]-[C:10]-[O;H0;D2;+0:11]-[CH;D3;+0:6]1-[#8:1]-[C:2]-[C:3]-[C:4]-[CH2;D2;+0:5]-1
68.8
[{"value": 68.8, "product": "O1C(CCCC1)OCC#CCO", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
null
null
To a mixture of 5.0 g of 2-butyne-1,4-diol and 10 milligrams of p-toluenesulfonic add and 150 ml of dry ether there was added dropwise with stirring at room temperature 4.9 g of 3,4-dihydro-2H-pyran. After stirring overnight at ambient temperature the ether was evaporated and the residue was poured into 200 ml of water...
10.6084/m9.figshare.5104873.v1
null
Ether.Primary alcohol
Ether.Ether
C1=COCCC1
C1CCOCC1
C1CCOCC1
null
CCOCC
null
null
C1=COCCC1.OCC#CCO>CCOCC>OCC#CCOC1CCCCO1
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-ea2fb6c87de2423b8a84f6a9a4419031
C#CC1CCCCC1.C=O>>OCC#CC1CCCCC1
C1(CCCCC1)C#C.C=O.C=O>>C1(CCCCC1)C#CCO
[CH:3]#[C:4][CH:5]1[CH2:6][CH2:7][CH2:8][CH2:9][CH2:10]1.[O:1]=[CH2:2]>>[OH:1][CH2:2][C:3]#[C:4][CH:5]1[CH2:6][CH2:7][CH2:8][CH2:9][CH2:10]1
C#CC1CCCCC1.C=O
OCC#CC1CCCCC1
null
null
CCOCC
C-C Coupling
OtherReaction
b068d8bba9f864ba971dd324292d9b3526f0235b4ab7e3a9ce6aa76a39c4a1e7
22ebec2cc94dd24863aea8793d450cfe0691e1036be204d1a4c79c16effe90a4
C1CCCCC1
[CH2;D1;+0:1]=[O;H0;D1;+0:2].[C:3]-[C:4]#[CH;D1;+0:5]>>[C:3]-[C:4]#[C;H0;D2;+0:5]-[CH2;D2;+0:1]-[OH;D1;+0:2]
null
[]
null
null
null
null
To a solution of ethyl magesium bromide (prepared from 2.5 g of magnesium turning and 11.3 g of bromoethane) in ether was added dropwise a solution of 10.2 g of cyclohexylacetylene in ether and the reaction mixture was refluxed for 2 hours. The reaction mixture was cooled to ambient temperature and anhydrous formaldehy...
10.6084/m9.figshare.5104873.v1
null
Formaldehyde.Alkyne
Primary alcohol.Alkyne
null
null
C1CCCCC1
null
CCOCC
null
null
C#CC1CCCCC1.C=O>CCOCC>OCC#CC1CCCCC1
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-9050fa6258a9415bb85240ff78c07174
O=C1CCC(c2ccc(Cl)cc2)=NN1>>O=c1ccc(-c2ccc(Cl)cc2)n[nH]1
ClC1=CC=C(C=C1)C=1CCC(NN1)=O.C(C)(=O)O.BrBr>>ClC1=CC=C(C=C1)C=1C=CC(NN1)=O
[O:1]=[C:2]1[CH2:3][CH2:4][C:5]([c:6]2[cH:7][cH:8][c:9]([Cl:10])[cH:11][cH:12]2)=[N:13][NH:14]1>>[O:1]=[c:2]1[cH:3][cH:4][c:5](-[c:6]2[cH:7][cH:8][c:9]([Cl:10])[cH:11][cH:12]2)[n:13][nH:14]1
O=C1CCC(c2ccc(Cl)cc2)=NN1
O=c1ccc(-c2ccc(Cl)cc2)n[nH]1
null
null
O
Aromatic Heterocycle Formation
OtherReaction
73c80fbcc9dd7a9125aaf1059d9d4eab31b342d21fc860abf5e65fd78456864b
78b0616e5760c6d4dadfc1fac5c58c0254d0dc7b1bf102fea4bc1349928b0776
O=c1ccc(-c2ccccc2)n[nH]1
[O;D1;H0:1]=[C;H0;D3;+0:2]1-[CH2;D2;+0:3]-[CH2;D2;+0:4]-[C;H0;D3;+0:5](-[c;H0;D3;+0:6](:[c:7]:[c:8]):[c:9]:[c:10])=[N;H0;D2;+0:11]-[NH;D2;+0:12]-1>>[O;D1;H0:1]=[c;H0;D3;+0:2]1:[cH;D2;+0:3]:[cH;D2;+0:4]:[c;H0;D3;+0:5](-[c;H0;D3;+0:6](:[c:7]:[c:8]):[c:9]:[c:10]):[n;H0;D2;+0:11]:[nH;D2;+0:12]:1
93.1
[{"value": 89.0, "product": "ClC1=CC=C(C=C1)C=1C=CC(NN1)=O", "details": "PERCENTYIELD", "is_desired": false}, {"value": 93.1, "product": "ClC1=CC=C(C=C1)C=1C=CC(NN1)=O", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
null
null
To a solution of 6-(4-chlorophenyl)-4,5-dihydropyridazinone (11.75 g) and glacial acetic acid (100 ml) was added dropwise 3 ml of bromine and the mixture was heated at 60°-70° C. for 3 h. The resulting mixture was cooled and slowly poured into 400 ml of cold water. The resulting white solid was filtered and dried to yi...
10.6084/m9.figshare.5104873.v1
null
Hydrazone amide
null
C1=NNCCC1
c1cccnn1
c1cccnn1.c1ccccc1
null
O
null
null
O=C1CCC(c2ccc(Cl)cc2)=NN1>O>O=c1ccc(-c2ccc(Cl)cc2)n[nH]1
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-a068a289c1114a798edc84425ca9f594
FC1(F)CC(Cl)(Cl)C1(F)Cl>>FC1(F)C=C(Cl)C1(F)Cl
ClC1(C(C(C1)(F)F)(F)Cl)Cl.O.Cl>>ClC1(C(C=C1Cl)(F)F)F
Cl[C:5]1([Cl:6])[CH2:4][C:2]([F:1])([F:3])[C:7]1([F:8])[Cl:9]>>[F:1][C:2]1([F:3])[CH:4]=[C:5]([Cl:6])[C:7]1([F:8])[Cl:9]
FC1(F)CC(Cl)(Cl)C1(F)Cl
FC1(F)C=C(Cl)C1(F)Cl
null
null
CCOCC.C(C)N(CC)CC
Functional Group Interconversion
OtherReaction
0ca523bc88d44f4371960ac2ff9ed0bbb8882337b7061f7fba5b4787f1e02481
986b135105e7920109b424799136a4a8281fb4a0f49253ce1bf5d4426ed78637
C1=CCC1
Cl-[C;H0;D4;+0:1]1(-[Cl;D1;H0:2])-[CH2;D2;+0:3]-[C:4](-[F;D1;H0:5])(-[F;D1;H0:6])-[C:7]-1(-[Cl;D1;H0:8])-[F;D1;H0:9]>>[Cl;D1;H0:2]-[C;H0;D3;+0:1]1=[CH;D2;+0:3]-[C:4](-[F;D1;H0:5])(-[F;D1;H0:6])-[C:7]-1(-[Cl;D1;H0:8])-[F;D1;H0:9]
79
[{"value": 79.0, "product": "ClC1(C(C=C1Cl)(F)F)F", "details": "PERCENTYIELD", "is_desired": false}, {"value": 78.2, "product": "ClC1(C(C=C1Cl)(F)F)F", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
8
HOUR
To a solution of 1,1,2 trichloro-2,3,3-trifluorocyclobutane (55.5 g) in 100 ml of anhydrous ether, triethylamine (40 ml) was added dropwise over 30 min at room temperature, and the mixture was stirred overnight at ambient temperature. The mixture was then stirred with 120 ml H2O and 7.5 ml of concentrated HCl. The ethe...
10.6084/m9.figshare.5104873.v1
null
Tertiary halide.Tertiary halide
Alkenyl halide
C1CCC1
C1=CCC1
C1=CCC1
HCl
CCOCC.C(C)N(CC)CC
null
8
FC1(F)CC(Cl)(Cl)C1(F)Cl>CCOCC.C(C)N(CC)CC>FC1(F)C=C(Cl)C1(F)Cl
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-51c7ba5d9752485ca16303527dfa9966
O=C(O)C(F)(F)C(F)(Cl)C(=O)O>>O=C(O)C(F)C(F)(F)C(=O)O
ClC(C(C(=O)O)(F)F)(C(=O)O)F>>FC(C(=O)O)(C(C(=O)O)F)F
Cl[C:6]([C:4]([C:2](=[O:1])[OH:3])([F:5])[F:7])([F:8])[C:9](=[O:10])[OH:11]>>[O:1]=[C:2]([OH:3])[CH:4]([F:5])[C:6]([F:7])([F:8])[C:9](=[O:10])[OH:11]
O=C(O)C(F)(F)C(F)(Cl)C(=O)O
O=C(O)C(F)C(F)(F)C(=O)O
null
[Zn]
O1CCOCC1
Functional Group Addition
Dehalogenation
7f145230bfb0115349e969b2f2fa1359cfafe8c166e52b50a867192005e1f5bc
d6722b0df465660a9eeeaca5a8f5b3dbb2d1ebccb44917f2eca97a85bf850d06
null
Cl-[C;H0;D4;+0:1](-[F;D1;H0:2])(-[C:3](=[O;D1;H0:4])-[O;D1;H1:5])-[C;H0;D4;+0:6](-[F;D1;H0:7])(-[F;H0;D1;+0:8])-[C:9](=[O;D1;H0:10])-[O;D1;H1:11]>>[F;D1;H0:7]-[CH;D3;+0:6](-[C:9](=[O;D1;H0:10])-[O;D1;H1:11])-[C;H0;D4;+0:1](-[F;D1;H0:2])(-[F;H0;D1;+0:8])-[C:3](=[O;D1;H0:4])-[O;D1;H1:5]
40.7
[{"value": 32.0, "product": "FC(C(=O)O)(C(C(=O)O)F)F", "details": "PERCENTYIELD", "is_desired": false}, {"value": 40.7, "product": "FC(C(=O)O)(C(C(=O)O)F)F", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
10
HOUR
To a stirring solution of the chlorotrifluorosuccinic acid (part b) (24.5 g) in 200 ml dioxane was added portionwise zinc metal (85 g) and the mixture was stirred at ambient temperature for 10 hours to yield a viscous liquid which was decanted from the unreacted zinc. Most of the dioxane was evaporated in vacuo. The re...
10.6084/m9.figshare.5104873.v1
null
Tertiary halide.Tertiary halide.Tertiary halide.Tertiary halide
Tertiary halide.Tertiary halide.Secondary halide
null
null
null
Other
[Zn].O1CCOCC1
null
10
O=C(O)C(F)(F)C(F)(Cl)C(=O)O>[Zn].O1CCOCC1>O=C(O)C(F)C(F)(F)C(=O)O
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-9cda8deef8464fdbb84bc3f44d4fe1f5
O=C1CCC(=O)O1.c1ccc2ccccc2c1>>O=C(O)CCC(=O)c1cccc2ccccc12
Cl.[Cl-].[Cl-].[Cl-].[Al+3].C1=CC=CC2=CC=CC=C12.C1(CCC(=O)O1)=O>>C1(=CC=CC2=CC=CC=C12)C(=O)CCC(=O)O
[O:1]=[C:2]1[O:3][C:6](=[O:7])[CH2:5][CH2:4]1.[cH:8]1[cH:9][cH:10][cH:11][c:12]2[cH:13][cH:14][cH:15][cH:16][c:17]12>>[O:1]=[C:2]([OH:3])[CH2:4][CH2:5][C:6](=[O:7])[c:8]1[cH:9][cH:10][cH:11][c:12]2[cH:13][cH:14][cH:15][cH:16][c:17]12
O=C1CCC(=O)O1.c1ccc2ccccc2c1
O=C(O)CCC(=O)c1cccc2ccccc12
null
null
[N+](=O)([O-])C1=CC=CC=C1
C-C Coupling
OtherReaction
d1b47ca78c3ceb45955ddf79d2b2d22c1a0978cf9fa8ded4c5ee0a8331deac4e
4836357c99dfeeac9d5083fedc379181a858ae45ac77bd85eb46e7e1a9df36f0
c1ccc2ccccc2c1
[O;D1;H0:1]=[C:2]1-[C:3]-[C:4]-[C;H0;D3;+0:5](=[O;D1;H0:6])-[O;H0;D2;+0:7]-1.[c:8]:[c:9]:[cH;D2;+0:10]:[c:11](:[c:12]):[c:13]>>[O;D1;H0:1]=[C:2](-[OH;D1;+0:7])-[C:3]-[C:4]-[C;H0;D3;+0:5](=[O;D1;H0:6])-[c;H0;D3;+0:10](:[c:9]:[c:8]):[c:11](:[c:12]):[c:13]
null
[]
null
null
null
null
A mixture of naphthalene (40 g) and succinic anhydride (20 g) was added to a well stirred suspension of aluminum trichloride (55 g) in nitrobenzene (140 ml). The resulting mixture was stirred overnight at room temperature. The mixture was then poured slowly onto ice-water (600 g) and acidified with 6N-hydrochloric acid...
10.6084/m9.figshare.5104873.v1
null
Anhydride
Carboxylic acid.Ketone
C1CCOC1.c1ccc2ccccc2c1
c1ccc2ccccc2c1
c1ccc2ccccc2c1
null
[N+](=O)([O-])C1=CC=CC=C1
null
null
O=C1CCC(=O)O1.c1ccc2ccccc2c1>[N+](=O)([O-])C1=CC=CC=C1>O=C(O)CCC(=O)c1cccc2ccccc12
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-eff35b6820384eb2a5f2f60a585c840d
NN.O=C(O)CCCC(=O)c1ccccc1>>O=c1cccc(-c2ccccc2)nn1
C(C1=CC=CC=C1)(=O)CCCC(=O)O.NN.O>>C1(=CC=CC=C1)C1=CC=CC(N=N1)=O
[NH2:13][NH2:14].O=[C:6]([CH2:5][CH2:4][CH2:3][C:2](O)=[O:1])[c:7]1[cH:8][cH:9][cH:10][cH:11][cH:12]1>>[O:1]=[c:2]1[cH:3][cH:4][cH:5][c:6](-[c:7]2[cH:8][cH:9][cH:10][cH:11][cH:12]2)[n:13][n:14]1
NN.O=C(O)CCCC(=O)c1ccccc1
O=c1cccc(-c2ccccc2)nn1
null
null
C1(=CC=CC=C1)C.CCOCC
Aromatic Heterocycle Formation
OtherReaction
a31553d36b14882561a6dcdd04ef456bc0e14ea189c472490f94f02ebbe3ca3f
eadf9e657b4bde18ed656e299092aac7dd81eee1face1030775c3edd6ccba31c
O=c1cccc(-c2ccccc2)nn1
O-[C;H0;D3;+0:1](=[O;D1;H0:2])-[CH2;D2;+0:3]-[CH2;D2;+0:4]-[CH2;D2;+0:5]-[C;H0;D3;+0:6](=O)-[c;H0;D3;+0:7](:[c:8]:[c:9]):[c:10]:[c:11].[NH2;D1;+0:12]-[NH2;D1;+0:13]>>[O;D1;H0:2]=[c;H0;D3;+0:1]1:[cH;D2;+0:3]:[cH;D2;+0:4]:[cH;D2;+0:5]:[c;H0;D3;+0:6](-[c;H0;D3;+0:7](:[c:8]:[c:9]):[c:10]:[c:11]):[n;H0;D2;+0:12]:[n;H0;D2;+0...
39
[{"value": 39.0, "product": "C1(=CC=CC=C1)C1=CC=CC(N=N1)=O", "details": "PERCENTYIELD", "is_desired": false}]
null
null
null
null
To a mixture of 10g (0.052 mole) of 4-benzoylbutyric acid in 300 ml of toluene, hydrazine was added in one portion and the reaction was heated to reflux until all water had ceased to azeotrope. The reaction mixture was cooled and the toluene was stripped off in vacuo. The residue was dissolved in 200 ml Et2O and washed...
10.6084/m9.figshare.5104873.v1
null
Hydrazine.Carboxylic acid.Ketone
null
null
c1cccc[nH]n1
c1cccc[nH]n1.c1ccccc1
HO-
C1(=CC=CC=C1)C.CCOCC
null
null
NN.O=C(O)CCCC(=O)c1ccccc1>C1(=CC=CC=C1)C.CCOCC>O=c1cccc(-c2ccccc2)nn1
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-85c5b1a3dd694c5d823ad82e2974b06f
COC(=O)OC.O=C1CCc2cc(Cl)ccc21>>COC(=O)C1Cc2cc(Cl)ccc2C1=O
COC(OC)=O.[H-].[Na+].ClC=1C=C2CCC(C2=CC1)=O.[H][H]>>C(=O)(OC)C1C(C2=CC=C(C=C2C1)Cl)=O
CO[C:3]([O:2][CH3:1])=[O:4].[CH2:5]1[CH2:6][c:7]2[cH:8][c:9]([Cl:10])[cH:11][cH:12][c:13]2[C:14]1=[O:15]>>[CH3:1][O:2][C:3](=[O:4])[CH:5]1[CH2:6][c:7]2[cH:8][c:9]([Cl:10])[cH:11][cH:12][c:13]2[C:14]1=[O:15]
COC(=O)OC.O=C1CCc2cc(Cl)ccc21
COC(=O)C1Cc2cc(Cl)ccc2C1=O
null
null
C(OC)COC
C-C Coupling
OtherReaction
c2c31337dfb867d8c28bc65df0ad4496f817a712a58e176523b47d7fdb6e4f91
d76b6fc9d01d8258e5777a3b2326a8d78a9d9a55717b27736ba55600205f4ed0
O=C1CCc2ccccc21
C-O-[C;H0;D3;+0:1](=[O;D1;H0:2])-[#8:3]-[C;D1;H3:4].[O;D1;H0:5]=[C:6]1-[CH2;D2;+0:7]-[C:8]-[c:9]:[c:10]-1>>[C;D1;H3:4]-[#8:3]-[C;H0;D3;+0:1](=[O;D1;H0:2])-[CH;D3;+0:7]1-[C:8]-[c:9]:[c:10]-[C:6]-1=[O;D1;H0:5]
45
[{"value": 45.0, "product": "C(=O)(OC)C1C(C2=CC=C(C=C2C1)Cl)=O", "details": "PERCENTYIELD", "is_desired": false}, {"value": 44.5, "product": "C(=O)(OC)C1C(C2=CC=C(C=C2C1)Cl)=O", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
60
CELSIUS
null
null
To a mixture of sodium hydride (2.4 g, 60% in mineral oil, 0.06 mole) and 50 ml dry dimethoxyethane, 5-chloroindanone (50 g, 0.03 mole) in 50 ml dimethoxyethane was added dropwise at room temperature. The mixture was stirred at room temperature until hydrogen evolution ceased. Then dimethylcarbonate (27 g, 0.3 mole) wa...
10.6084/m9.figshare.5104873.v1
null
Carbonic Ester.Ketone
Ketone.Ester
c1ccc2c(c1)CCC2
c1ccc2c(c1)CCC2
c1ccc2c(c1)CCC2
HO-
C(OC)COC
60
null
COC(=O)OC.O=C1CCc2cc(Cl)ccc21>C(OC)COC>COC(=O)C1Cc2cc(Cl)ccc2C1=O
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-d54af9d4762649be9b45711704142f42
CN(C)C=O.O=C(O)Cc1ccc(Cl)cc1>>CN(C)C=C(C=O)c1ccc(Cl)cc1
C([O-])([O-])=O.[K+].[K+].P(=O)(Cl)(Cl)Cl.CN(C)C=O.ClC1=CC=C(C=C1)CC(=O)O>>ClC1=CC=C(C=C1)C(C=O)=CN(C)C
O=[CH:4][N:2]([CH3:1])[CH3:3].O=[C:6]([CH2:5][c:8]1[cH:9][cH:10][c:11]([Cl:12])[cH:13][cH:14]1)[OH:7]>>[CH3:1][N:2]([CH3:3])[CH:4]=[C:5]([CH:6]=[O:7])[c:8]1[cH:9][cH:10][c:11]([Cl:12])[cH:13][cH:14]1
CN(C)C=O.O=C(O)Cc1ccc(Cl)cc1
CN(C)C=C(C=O)c1ccc(Cl)cc1
null
null
C1(=CC=CC=C1)C
Acylation
OtherReaction
cbf378fe57a2b8d8304e623fb5ce9ee6fb9f6e90d9c6f965226d56b103180e6d
a9c635686380f13b6b5c45d80d4aef36b30fdab0aef140b81f04c277f7ba737d
c1ccccc1
O=[C;H0;D3;+0:1](-[OH;D1;+0:2])-[CH2;D2;+0:3]-[c:4](:[c:5]):[c:6].O=[CH;D2;+0:7]-[#7:8](-[C;D1;H3:9])-[C;D1;H3:10]>>[C;D1;H3:9]-[#7:8](-[C;D1;H3:10])-[CH;D2;+0:7]=[C;H0;D3;+0:3](-[CH;D2;+0:1]=[O;H0;D1;+0:2])-[c:4](:[c:5]):[c:6]
null
[]
null
null
8
HOUR
Phosphorus oxychloride (92 g) was added dropwise to stirred DMF (78 ml) between 10°-15° C. To the resulting slurry was added 4-chlorophenylacetic acid (34.12 g). The resulting mixture was stirred at room temperature for one half hour and then heated to 70°-80° C. during 5.5 hours, during which time the mixture became e...
10.6084/m9.figshare.5104873.v1
null
Carboxylic acid.Tertiary amide
Enamine.Aldehyde
null
null
c1ccccc1
HO-
C1(=CC=CC=C1)C
null
8
CN(C)C=O.O=C(O)Cc1ccc(Cl)cc1>C1(=CC=CC=C1)C>CN(C)C=C(C=O)c1ccc(Cl)cc1
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-3a2c011f1b3e4de5a080b95b7446e37f
CN(C)C=C(C=O)c1ccc(Cl)cc1.N#CCC(N)=O>>N#Cc1cc(-c2ccc(Cl)cc2)c[nH]c1=O
CC(=O)OCC1=C2C=CC=CC2=C(C3=CC=CC=C31)COC(=O)C.ClC1=CC=C(C=C1)C(C=O)=CN(C)C.C[O-].[Na+].C(#N)CC(=O)N>>C(#N)C=1C(NC=C(C1)C1=CC=C(C=C1)Cl)=O
CN(C)[CH:13]=[C:5]([CH:4]=O)[c:6]1[cH:7][cH:8][c:9]([Cl:10])[cH:11][cH:12]1.[N:1]#[C:2][CH2:3][C:15]([NH2:14])=[O:16]>>[N:1]#[C:2][c:3]1[cH:4][c:5](-[c:6]2[cH:7][cH:8][c:9]([Cl:10])[cH:11][cH:12]2)[cH:13][nH:14][c:15]1=[O:16]
CN(C)C=C(C=O)c1ccc(Cl)cc1.N#CCC(N)=O
N#Cc1cc(-c2ccc(Cl)cc2)c[nH]c1=O
null
null
CO.O
Aromatic Heterocycle Formation
OtherReaction
4fb69599b2ad512416349de44ee025f314a8ccdb2c8ad729cdf94ea75cf3109a
46cf335065eccd013987994a3f086665eb273ac87eb3153099a47e61dd329581
O=c1ccc(-c2ccccc2)c[nH]1
C-N(-C)-[CH;D2;+0:1]=[C;H0;D3;+0:2](-[CH;D2;+0:3]=O)-[c;H0;D3;+0:4](:[c:5]:[c:6]):[c:7]:[c:8].[N;D1;H0:9]#[C:10]-[CH2;D2;+0:11]-[C;H0;D3;+0:12](-[NH2;D1;+0:13])=[O;D1;H0:14]>>[N;D1;H0:9]#[C:10]-[c;H0;D3;+0:11]1:[cH;D2;+0:3]:[c;H0;D3;+0:2](-[c;H0;D3;+0:4](:[c:5]:[c:6]):[c:7]:[c:8]):[cH;D2;+0:1]:[nH;D2;+0:13]:[c;H0;D3;+0...
null
[]
null
null
null
null
To solution of sodium methoxide (7.52 g) in methanol (130 ml) was added cyanoacetamide (5.84 g) followed by 2-(4-chlorophenyl)-3-dimethylaminopropenal and the resulting suspension was refluxed overnight. During this time a yellow solid was formed. The mixture was cooled to room temperature and glacial acetic add (50 ml...
10.6084/m9.figshare.5104873.v1
null
Enamine.Aldehyde.Primary amide
null
null
c1cnccc1
c1cnccc1.c1ccccc1
HO-
CO.O
null
null
CN(C)C=C(C=O)c1ccc(Cl)cc1.N#CCC(N)=O>CO.O>N#Cc1cc(-c2ccc(Cl)cc2)c[nH]c1=O
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-045750bf97304072902ebfbcb4032b67
N#Cc1cc(-c2ccc(Cl)cc2)c[nH]c1=O>>O=c1ccc(-c2ccc(Cl)cc2)c[nH]1
C(#N)C=1C(NC=C(C1)C1=CC=C(C=C1)Cl)=O>>ClC1=CC=C(C=C1)C=1C=CC(NC1)=O
N#C[c:3]1[c:2](=[O:1])[nH:14][cH:13][c:5](-[c:6]2[cH:7][cH:8][c:9]([Cl:10])[cH:11][cH:12]2)[cH:4]1>>[O:1]=[c:2]1[cH:3][cH:4][c:5](-[c:6]2[cH:7][cH:8][c:9]([Cl:10])[cH:11][cH:12]2)[cH:13][nH:14]1
N#Cc1cc(-c2ccc(Cl)cc2)c[nH]c1=O
O=c1ccc(-c2ccc(Cl)cc2)c[nH]1
null
null
OP(=O)(O)O
Miscellaneous
OtherReaction
145adc421652def73603eb299eace1e2e3a197522b719b6949c0145a4308d11b
4f08c5adfb6d80fba1093598fc51ce38f180c76537f67052d397b642cb6f3b89
O=c1ccc(-c2ccccc2)c[nH]1
N#C-[c;H0;D3;+0:1]1:[c:2]:[c:3]:[c:4]:[#7;a:5]:[c:6]:1=[O;D1;H0:7]>>[O;D1;H0:7]=[c:6]1:[#7;a:5]:[c:4]:[c:3]:[c:2]:[cH;D2;+0:1]:1
75.6
[{"value": 75.6, "product": "ClC1=CC=C(C=C1)C=1C=CC(NC1)=O", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
null
null
A mixture of 3-cyano-5-(4-chlorophenyl)-2-pyridinone (4.6 g) and 85% H3PO4 (60 ml) was heated at reflux for 16 hours. The resulting mixture was cooled to room temperature, poured into ice/water and filtered yielding 3.1 g of 5-(4-chlorophenyl)-2-pyridinone as a yellow solid. Conditions: See reaction.notes.procedure_det...
10.6084/m9.figshare.5104873.v1
null
Nitrile
null
c1cnccc1
c1cccnc1
c1cccnc1.c1ccccc1
Other
OP(=O)(O)O
null
null
N#Cc1cc(-c2ccc(Cl)cc2)c[nH]c1=O>OP(=O)(O)O>O=c1ccc(-c2ccc(Cl)cc2)c[nH]1
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-b9509a42332a49fcbb34674de68bb37b
CCC#CCBr.CCCCCC.O=c1cccc[nH]1.[Cl-]>>CCC#CCn1cc(-c2ccc(Cl)cc2)ccc1=O
[Cl-].[NH4+].[H-].[Na+].N1C(C=CC=C1)=O.CCCCCC.C(C)(=O)OCC.BrCC#CCC>>ClC1=CC=C(C=C1)C=1C=CC(N(C1)CC#CCC)=O
Br[CH2:5][C:4]#[C:3][CH2:2][CH3:1].[CH2:9]([CH3:10])[CH2:15][CH2:14][CH2:12][CH3:11].[nH:6]1[cH:7][cH:8][cH:16][cH:17][c:18]1=[O:19].[Cl-:13]>>[CH3:1][CH2:2][C:3]#[C:4][CH2:5][n:6]1[cH:7][c:8](-[c:9]2[cH:10][cH:11][c:12]([Cl:13])[cH:14][cH:15]2)[cH:16][cH:17][c:18]1=[O:19]
CCC#CCBr.CCCCCC.O=c1cccc[nH]1.[Cl-]
CCC#CCn1cc(-c2ccc(Cl)cc2)ccc1=O
null
null
CN(C)C=O
Aromatic Heterocycle Formation
OtherReaction
c16e53991381708a0d74f5092b5e25b0353184189763eaae006dd565c1174ab9
f1e2d48aa3857a2357f3a371c35806794fc7180cbbfa20a78f207e36837e33dc
O=c1ccc(-c2ccccc2)c[nH]1
Br-[CH2;D2;+0:1]-[C:2]#[C:3]-[C:4].[CH3;D1;+0:5]-[CH2;D2;+0:6]-[CH2;D2;+0:7]-[CH2;D2;+0:8]-[CH2;D2;+0:9]-[CH3;D1;+0:10].[Cl-;H0;D0:11].[O;D1;H0:12]=[c:13]1:[c:14]:[c:15]:[cH;D2;+0:16]:[c:17]:[nH;D2;+0:18]:1>>[C:4]-[C:3]#[C:2]-[CH2;D2;+0:1]-[n;H0;D3;+0:18]1:[c:17]:[c;H0;D3;+0:16](-[c;H0;D3;+0:6]2:[cH;D2;+0:5]:[cH;D2;+0:...
null
[]
0
CELSIUS
null
null
To a suspension of NaH (60% in mineral oil, 200 mg) in dry DMF (50 ml) at 0° C. was added the preceding pyridinone and the mixture was stirred at 0° C. for one half hour. To the resulting suspension was added 1-bromo-2-pentyne dropwise. The resulting mixture was kept at 0° C. during one half hour and poured into satura...
10.6084/m9.figshare.5104873.v1
null
Primary halide
Aromatic halide
c1ccccn1
c1ccncc1.c1ccccc1
c1ccncc1.c1ccccc1
HBr
CN(C)C=O
0
null
CCC#CCBr.CCCCCC.O=c1cccc[nH]1.[Cl-]>CN(C)C=O>CCC#CCn1cc(-c2ccc(Cl)cc2)ccc1=O
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-c8099fc1e3494ad8923c576fec19c417
Nc1ccc(Cl)cc1.O=C(Cl)C=Cc1ccccc1>>O=C(C=Cc1ccccc1)Nc1ccc(Cl)cc1
C(C)(=O)OCC.ClC1=CC=C(N)C=C1.N1=CC=CC=C1.C(C=CC1=CC=CC=C1)(=O)Cl>>ClC1=CC=C(C=C1)NC(C=CC1=CC=CC=C1)=O
[NH2:11][c:12]1[cH:13][cH:14][c:15]([Cl:16])[cH:17][cH:18]1.Cl[C:2](=[O:1])[CH:3]=[CH:4][c:5]1[cH:6][cH:7][cH:8][cH:9][cH:10]1>>[O:1]=[C:2]([CH:3]=[CH:4][c:5]1[cH:6][cH:7][cH:8][cH:9][cH:10]1)[NH:11][c:12]1[cH:13][cH:14][c:15]([Cl:16])[cH:17][cH:18]1
Nc1ccc(Cl)cc1.O=C(Cl)C=Cc1ccccc1
O=C(C=Cc1ccccc1)Nc1ccc(Cl)cc1
null
null
C1(=CC=CC=C1)C.O
Acylation
Acylation of Nitrogen Nucleophiles by Acyl/Thioacyl/Carbamoyl Halides and Analogs_OS
38143a4d536201990008fd6f2c68e6571a341d1c367481869fbbbe36cb038937
0e6ae078978e324f714e184b4f72826d4e3bf2d9ab22d6e9f73740af687be16f
O=C(C=Cc1ccccc1)Nc1ccccc1
Cl-[C;H0;D3;+0:1](=[O;D1;H0:2])-[C:3]=[C:4]-[c:5].[NH2;D1;+0:6]-[c:7](:[c:8]):[c:9]>>[O;D1;H0:2]=[C;H0;D3;+0:1](-[C:3]=[C:4]-[c:5])-[NH;D2;+0:6]-[c:7](:[c:8]):[c:9]
null
[]
0
CELSIUS
15
MINUTE
To a mixture of 4-chloroaniline (16.2 g), toluene (120 ml), and pyridine (11 ml) at 0° C., cinnamoyl chloride (20.0 g) in 120 ml of toluene was added dropwise. After stirring 15 minutes at 0° C. the reaction mixture was poured into a mixture of ethyl acetate: water (250 ml:250 ml). The organic layer was separated and e...
10.6084/m9.figshare.5104873.v1
null
Acyl halide.Primary amine
Secondary amide
null
null
c1ccccc1.c1ccccc1
HCl
C1(=CC=CC=C1)C.O
0
0.25
Nc1ccc(Cl)cc1.O=C(Cl)C=Cc1ccccc1>C1(=CC=CC=C1)C.O>O=C(C=Cc1ccccc1)Nc1ccc(Cl)cc1
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-771487d5281b4f96990cdc8a7a9c2bb2
O=C(C=Cc1ccccc1)Nc1ccc(Cl)cc1>>O=c1ccc2c(Cl)cccc2[nH]1
ClC1=CC=C(C=C1)NC(C=CC1=CC=CC=C1)=O.[Cl-].[Al+3].[Cl-].[Cl-]>>ClC1=C2C=CC(NC2=CC=C1)=O
c1ccc([CH:4]=[CH:3][C:2](=[O:1])[NH:12][c:11]2[cH:5][cH:8][c:6]([Cl:7])[cH:9][cH:10]2)cc1>>[O:1]=[c:2]1[cH:3][cH:4][c:5]2[c:6]([Cl:7])[cH:8][cH:9][cH:10][c:11]2[nH:12]1
O=C(C=Cc1ccccc1)Nc1ccc(Cl)cc1
O=c1ccc2c(Cl)cccc2[nH]1
null
null
ClC1=CC=CC=C1
Reduction
OtherReaction
ebe7e954f82f1e726cf9b7a8863216fec31733c3d8bfbb1cc71c49312cec65ac
10d6d5b071f1d84b20b253ce9eadaed211c373c6ee607356078792f13319351a
O=c1ccc2ccccc2[nH]1
[Cl;D1;H0:1]-[c;H0;D3;+0:2]1:[cH;D2;+0:3]:[cH;D2;+0:4]:[c:5](-[NH;D2;+0:6]-[C;H0;D3;+0:7](=[O;D1;H0:8])-[CH;D2;+0:9]=[CH;D2;+0:10]-c2:c:c:c:c:c:2):[c:11]:[cH;D2;+0:12]:1>>[Cl;D1;H0:1]-[c;H0;D3;+0:2]1:[cH;D2;+0:3]:[cH;D2;+0:12]:[c:11]:[c:5]2:[nH;D2;+0:6]:[c;H0;D3;+0:7](=[O;D1;H0:8]):[cH;D2;+0:9]:[cH;D2;+0:10]:[c;H0;D3;+...
null
[]
125
CELSIUS
3
HOUR
To a mixture of N-(4-chlorophenyl)cinnamamide (8.3 g), and chlorobenzene (60 ml) was added portionwise aluminum chloride (21.4 g) under nitrogen at room temperature and the reaction mixture was slowly warmed up to 125° C. and kept at that temperature for 3 hours. The reaction mixture was cooled down and poured over 400...
10.6084/m9.figshare.5104873.v1
null
Aromatic halide.Secondary amide
Aromatic halide
c1ccccc1.c1ccccc1
c1ccc2ccccc2n1
c1ccc2ccccc2n1
Other
ClC1=CC=CC=C1
125
3
O=C(C=Cc1ccccc1)Nc1ccc(Cl)cc1>ClC1=CC=CC=C1>O=c1ccc2c(Cl)cccc2[nH]1
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-3d045ba7bb254c15a155333d94ac21c7
CCC#CCBr.O=c1ccc2ccccc2[nH]1.[Cl-]>>CCC#CCn1c(=O)ccc2c(Cl)cccc21
[Cl-].[NH4+].N1C(C=CC2=CC=CC=C12)=O.[H-].[Na+].BrCC#CCC>>ClC1=C2C=CC(N(C2=CC=C1)CC#CCC)=O
Br[CH2:5][C:4]#[C:3][CH2:2][CH3:1].[nH:6]1[c:7](=[O:8])[cH:9][cH:10][c:11]2[cH:12][cH:14][cH:15][cH:16][c:17]12.[Cl-:13]>>[CH3:1][CH2:2][C:3]#[C:4][CH2:5][n:6]1[c:7](=[O:8])[cH:9][cH:10][c:11]2[c:12]([Cl:13])[cH:14][cH:15][cH:16][c:17]12
CCC#CCBr.O=c1ccc2ccccc2[nH]1.[Cl-]
CCC#CCn1c(=O)ccc2c(Cl)cccc21
null
null
CN(C)C=O.CCCCCC
Heteroatom Alkylation and Arylation
OtherReaction
a61336fe7a89ec0981a525297b55629e44e830f13f91df56a44bf01390d8c69d
dbda6588fa29cbbc0e3c3f601e69924b300990bdcc56b8cec0535d1258039346
O=c1ccc2ccccc2[nH]1
Br-[CH2;D2;+0:1]-[C:2]#[C:3]-[C:4].[Cl-;H0;D0:5].[O;D1;H0:6]=[c:7]1:[c:8]:[c:9]:[c:10]2:[cH;D2;+0:11]:[c:12]:[c:13]:[c:14]:[c:15]:2:[nH;D2;+0:16]:1>>[C:4]-[C:3]#[C:2]-[CH2;D2;+0:1]-[n;H0;D3;+0:16]1:[c:15]2:[c:14]:[c:13]:[c:12]:[c;H0;D3;+0:11](-[Cl;H0;D1;+0:5]):[c:10]:2:[c:9]:[c:8]:[c:7]:1=[O;D1;H0:6]
null
[]
0
CELSIUS
null
null
To a suspension of NaH (60% in mineral oil, 700 mg) in dry DMF (100 ml) at 0° C. was added the preceding quinolinone (2.05 g) and the mixture was stirred at 0° C. for one half hour. To the resulting suspension was added 1-bromo-2-pentyne (1.6 g) dropwise. The resulting mixture was kept at 0° C. for one half hour and po...
10.6084/m9.figshare.5104873.v1
null
Primary halide
Aromatic halide
c1ccc2ccccc2n1
c1ccc2ncccc2c1
c1ccc2ncccc2c1
HBr
CN(C)C=O.CCCCCC
0
null
CCC#CCBr.O=c1ccc2ccccc2[nH]1.[Cl-]>CN(C)C=O.CCCCCC>CCC#CCn1c(=O)ccc2c(Cl)cccc21
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-682083a1fe1b4917a49c1da58af0cb59
CN(C)C=C(C=O)c1ccc(Cl)cc1.NC(N)=O>>O=c1ncc(-c2ccc(Cl)cc2)c[nH]1
[Cl-].[NH4+].ClC1=CC=C(C=C1)C(C=O)=CN(C)C.NC(=O)N.Cl>>ClC1=CC=C(C=C1)C=1C=NC(NC1)=O
CN(C)[CH:4]=[C:5]([c:6]1[cH:7][cH:8][c:9]([Cl:10])[cH:11][cH:12]1)[CH:13]=O.[O:1]=[C:2]([NH2:3])[NH2:14]>>[O:1]=[c:2]1[n:3][cH:4][c:5](-[c:6]2[cH:7][cH:8][c:9]([Cl:10])[cH:11][cH:12]2)[cH:13][nH:14]1
CN(C)C=C(C=O)c1ccc(Cl)cc1.NC(N)=O
O=c1ncc(-c2ccc(Cl)cc2)c[nH]1
null
null
C(C)O.O
Aromatic Heterocycle Formation
OtherReaction
0e1bb7c6fc2fa2fbd0239b648ae136ef123b13ddeb9947c50b8f38d453d7d183
55a949c5abf218b0e7fd0015b81e86fb975fa441e5ac6bd395c3346bb38599f7
O=c1ncc(-c2ccccc2)c[nH]1
C-N(-C)-[CH;D2;+0:1]=[C;H0;D3;+0:2](-[CH;D2;+0:3]=O)-[c;H0;D3;+0:4](:[c:5]:[c:6]):[c:7]:[c:8].[NH2;D1;+0:9]-[C;H0;D3;+0:10](-[NH2;D1;+0:11])=[O;D1;H0:12]>>[O;D1;H0:12]=[c;H0;D3;+0:10]1:[n;H0;D2;+0:11]:[cH;D2;+0:1]:[c;H0;D3;+0:2](-[c;H0;D3;+0:4](:[c:5]:[c:6]):[c:7]:[c:8]):[cH;D2;+0:3]:[nH;D2;+0:9]:1
29.7
[{"value": 29.7, "product": "ClC1=CC=C(C=C1)C=1C=NC(NC1)=O", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
null
null
A mixture of 2-(4-chlorophenyl)dimethylaminopropenal (Example 145a) (5.13 g), urea (2.4 g), concentrated HCl (10 ml), water (4 ml) and ethanol (150 ml) was refluxed for 4 hours. After cooling to room temperature concentrated ammonium chloride was added until the pH was 7. The resulting yellow solid was filtered off and...
10.6084/m9.figshare.5104873.v1
null
Enamine.Aldehyde.Urea
null
null
c1cncnc1
c1cncnc1.c1ccccc1
HO-
C(C)O.O
null
null
CN(C)C=C(C=O)c1ccc(Cl)cc1.NC(N)=O>C(C)O.O>O=c1ncc(-c2ccc(Cl)cc2)c[nH]1
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-b6e9c38f760d411e813e29218db44408
CCC#CCBr.CCCCCC.O=c1cccc[nH]1.[Cl-].[NH4+]>>CCC#CCn1cc(-c2ccc(Cl)cc2)cnc1=O
[Cl-].[NH4+].CCCCCC.[H-].[Na+].N1C(C=CC=C1)=O.BrCC#CCC>>ClC1=CC=C(C=C1)C=1C=NC(N(C1)CC#CCC)=O
Br[CH2:5][C:4]#[C:3][CH2:2][CH3:1].C[CH2:15][CH2:14][CH2:12][CH2:11][CH3:10].[nH:6]1[cH:7][cH:8][cH:16][cH:9][c:18]1=[O:19].[Cl-:13].[NH4+:17]>>[CH3:1][CH2:2][C:3]#[C:4][CH2:5][n:6]1[cH:7][c:8](-[c:9]2[cH:10][cH:11][c:12]([Cl:13])[cH:14][cH:15]2)[cH:16][n:17][c:18]1=[O:19]
CCC#CCBr.CCCCCC.O=c1cccc[nH]1.[Cl-].[NH4+]
CCC#CCn1cc(-c2ccc(Cl)cc2)cnc1=O
null
null
CN(C)C=O
Aromatic Heterocycle Formation
OtherReaction
b4467fdd65493649554b053844b88f7aedac75ecb5e83a2819a9163270cc6b1f
f1e2d48aa3857a2357f3a371c35806794fc7180cbbfa20a78f207e36837e33dc
O=c1ncc(-c2ccccc2)c[nH]1
Br-[CH2;D2;+0:1]-[C:2]#[C:3]-[C:4].C-[CH2;D2;+0:5]-[CH2;D2;+0:6]-[CH2;D2;+0:7]-[CH2;D2;+0:8]-[CH3;D1;+0:9].[Cl-;H0;D0:10].[NH4+;D0:11].[O;D1;H0:12]=[c;H0;D3;+0:13]1:[cH;D2;+0:14]:[cH;D2;+0:15]:[cH;D2;+0:16]:[c:17]:[nH;D2;+0:18]:1>>[C:4]-[C:3]#[C:2]-[CH2;D2;+0:1]-[n;H0;D3;+0:18]1:[c:17]:[c;H0;D3;+0:16](-[c;H0;D3;+0:14]2...
null
[]
0
CELSIUS
null
null
To a suspension of NaH (60% in mineral oil, 340 mg) in dry DMF (75 ml) at 0° C. was added the preceding pyridinone (1.0 g) and the mixture was stirred at 0° C. for one half hour. To the resulting suspension was added 1-bromo-2-pentyne (750 mg) dropwise. The resulting mixture was kept at 0° C. for one half hour and pour...
10.6084/m9.figshare.5104873.v1
null
Primary halide
Aromatic halide
c1ccccn1
c1cncnc1.c1ccccc1
c1cncnc1.c1ccccc1
HBr
CN(C)C=O
0
null
CCC#CCBr.CCCCCC.O=c1cccc[nH]1.[Cl-].[NH4+]>CN(C)C=O>CCC#CCn1cc(-c2ccc(Cl)cc2)cnc1=O
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-3601c190422e4f1099ec81cc9afbdad4
O=c1ccc(-c2ccc(Cl)cc2)n[nH]1.S=P12SP3(=S)SP(=S)(S1)SP(=S)(S2)S3>>S=c1ccc(-c2ccc(Cl)cc2)n[nH]1
ClC1=CC=C(C=C1)C=1C=CC(NN1)=O.P12(=S)SP3(=S)SP(=S)(S1)SP(=S)(S2)S3>>ClC1=CC=C(C=C1)C=1C=CC(NN1)=S
O=[c:2]1[cH:3][cH:4][c:5](-[c:6]2[cH:7][cH:8][c:9]([Cl:10])[cH:11][cH:12]2)[n:13][nH:14]1.S=P12SP3(=S)SP(=S)(S1)SP(=[S:1])(S2)S3>>[S:1]=[c:2]1[cH:3][cH:4][c:5](-[c:6]2[cH:7][cH:8][c:9]([Cl:10])[cH:11][cH:12]2)[n:13][nH:14]1
O=c1ccc(-c2ccc(Cl)cc2)n[nH]1.S=P12SP3(=S)SP(=S)(S1)SP(=S)(S2)S3
S=c1ccc(-c2ccc(Cl)cc2)n[nH]1
null
null
N1=CC=CC=C1
Heteroatom Alkylation and Arylation
OtherReaction
e0da8be0c0e31372bc487fca4d998b8539b7ff5b84df07e1a6200efd3593e0bb
13be3f637e1e22872d741944f46b7fcc1954fe982a3a8a0f7825545d455ab147
S=c1ccc(-c2ccccc2)n[nH]1
O=[c;H0;D3;+0:1]1:[#7;a:2]:[#7;a:3]:[c:4]:[c:5]:[c:6]:1.S=P12-S-P3(=S)-S-P(=S)(-S-1)-S-P(=[S;H0;D1;+0:7])(-S-2)-S-3>>[S;H0;D1;+0:7]=[c;H0;D3;+0:1]1:[#7;a:2]:[#7;a:3]:[c:4]:[c:5]:[c:6]:1
187.1
[{"value": 187.1, "product": "ClC1=CC=C(C=C1)C=1C=CC(NN1)=S", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
null
null
A mixture of 3.0 g of 6-(4-chlorophenyl)-pyridazinone, 50 ml of dry pyridine and 3.2 g of phosphorus pentasulfide was refluxed for 1 hour, evaporated to dryness and extracted with 200 ml of ether. The ether extract was washed with water (3×100 ml), brine (100 ml), dried over magnesium sulfate and evaporated to yield 3....
10.6084/m9.figshare.5104873.v1
null
Monosulfide.Monosulfide.Monosulfide.Monosulfide.Monosulfide.Monosulfide
Thiocarbonyl
c1cccnn1.S1P2SP3SP1SP(S2)S3
c1cccnn1
c1cccnn1.c1ccccc1
Other
N1=CC=CC=C1
null
null
O=c1ccc(-c2ccc(Cl)cc2)n[nH]1.S=P12SP3(=S)SP(=S)(S1)SP(=S)(S2)S3>N1=CC=CC=C1>S=c1ccc(-c2ccc(Cl)cc2)n[nH]1
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-9444014702f243e4a6c2da6f4e2518a1
NNC(=O)c1ccc(Cl)cc1.O=C(Cl)CCl>>O=C(CCl)NNC(=O)c1ccc(Cl)cc1
ClC1=CC=C(C(=O)NN)C=C1.ClCC(=O)Cl>>ClCC(=O)NNC(C1=CC=C(C=C1)Cl)=O
[NH2:5][NH:6][C:7](=[O:8])[c:9]1[cH:10][cH:11][c:12]([Cl:13])[cH:14][cH:15]1.Cl[C:2](=[O:1])[CH2:3][Cl:4]>>[O:1]=[C:2]([CH2:3][Cl:4])[NH:5][NH:6][C:7](=[O:8])[c:9]1[cH:10][cH:11][c:12]([Cl:13])[cH:14][cH:15]1
NNC(=O)c1ccc(Cl)cc1.O=C(Cl)CCl
O=C(CCl)NNC(=O)c1ccc(Cl)cc1
null
null
O1CCOCC1
Acylation
Acylation of Nitrogen Nucleophiles by Acyl/Thioacyl/Carbamoyl Halides and Analogs_OS
e9c0e57fff756e07b8f823de2eed1eeaae995a83400f2b5e18582349988c9a5f
384006bf8ba751654aef497f42d95dd6fc64342c355d6ce7d0ea9a3aaffeacc6
c1ccccc1
Cl-[C;H0;D3;+0:1](=[O;D1;H0:2])-[C:3]-[Cl;D1;H0:4].[NH2;D1;+0:5]-[#7:6]-[C:7](=[O;D1;H0:8])-[c:9]>>[Cl;D1;H0:4]-[C:3]-[C;H0;D3;+0:1](=[O;D1;H0:2])-[NH;D2;+0:5]-[#7:6]-[C:7](=[O;D1;H0:8])-[c:9]
null
[]
null
null
null
null
To a solution of p-chlorobenzoic hydrazide (11.2 g) in dioxane (100 ml) was added chloroacetyl chloride (6 ml). The resulting mixture was refluxed for three hours, cooled to room temperature and filtered. The resulting solid was washed with ethyl ether and dried to yield N'-chloroacetyl-4-chlorobenzoic hydrazide as whi...
10.6084/m9.figshare.5104873.v1
null
Acyl halide.Acylhydrazine
Acylhydrazine.Acylhydrazine
null
null
c1ccccc1
HCl
O1CCOCC1
null
null
NNC(=O)c1ccc(Cl)cc1.O=C(Cl)CCl>O1CCOCC1>O=C(CCl)NNC(=O)c1ccc(Cl)cc1
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-a3d67c3bad7c44c29b9bc8727026575d
COC(=S)NN.O=C(CBr)c1ccc(Cl)cc1>>O=C1NN=C(c2ccc(Cl)cc2)CS1
BrCC(=O)C1=CC=C(C=C1)Cl.COC(=S)NN>>ClC1=CC=C(C=C1)C1=NNC(SC1)=O
C[O:1][C:2]([NH:3][NH2:4])=[S:14].O=[C:5]([c:6]1[cH:7][cH:8][c:9]([Cl:10])[cH:11][cH:12]1)[CH2:13]Br>>[O:1]=[C:2]1[NH:3][N:4]=[C:5]([c:6]2[cH:7][cH:8][c:9]([Cl:10])[cH:11][cH:12]2)[CH2:13][S:14]1
COC(=S)NN.O=C(CBr)c1ccc(Cl)cc1
O=C1NN=C(c2ccc(Cl)cc2)CS1
null
null
C(C)#N
Acylation
OtherReaction
a0815ff887854434f061e02bb59e65917f2f792eefe3f407e6f67a241e834044
b7ddc8c969600ae9a9b2d12841c66a24307741bcbfc0810c56e58eb7d0e4892d
O=C1NN=C(c2ccccc2)CS1
Br-[CH2;D2;+0:1]-[C;H0;D3;+0:2](=O)-[c:3](:[c:4]):[c:5].C-[O;H0;D2;+0:6]-[C;H0;D3;+0:7](=[S;H0;D1;+0:8])-[#7:9]-[NH2;D1;+0:10]>>[O;H0;D1;+0:6]=[C;H0;D3;+0:7]1-[#7:9]-[N;H0;D2;+0:10]=[C;H0;D3;+0:2](-[c:3](:[c:4]):[c:5])-[CH2;D2;+0:1]-[S;H0;D2;+0:8]-1
48.4
[{"value": 48.4, "product": "ClC1=CC=C(C=C1)C1=NNC(SC1)=O", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
null
null
A mixture of 2-bromo-p-chloroacetophenone (9.16 g), methoxythiocarbonylhydrazine (13.0 g) and acetonitrile (75 ml) was refluxed overnight and then cooled and filtered. The light yellow solid was washed with hexane and dried yielding 5-(4-chlorophenyl)-3H,6H-1,3,4-thiadiazin-2-one (4.3 g). Conditions: See reaction.notes...
10.6084/m9.figshare.5104873.v1
null
Hydrazine.Primary halide.Ketone.Ether.Thioamide
Hydrazone amide.Monosulfide
null
C1=NNCSC1
C1=NNCSC1.c1ccccc1
HBr
C(C)#N
null
null
COC(=S)NN.O=C(CBr)c1ccc(Cl)cc1>C(C)#N>O=C1NN=C(c2ccc(Cl)cc2)CS1
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-9f7ecc08ca4a459c8bd54d42b7e2aa72
O=C(O)CCC(=O)c1cccc(Cl)c1>>O=C(O)CCCc1cccc(Cl)c1
ClC=1C=C(C(=O)CCC(=O)O)C=CC1.[OH-].[K+].NN>>ClC=1C=C(C=CC1)CCCC(=O)O
O=[C:6]([CH2:5][CH2:4][C:2](=[O:1])[OH:3])[c:7]1[cH:8][cH:9][cH:10][c:11]([Cl:12])[cH:13]1>>[O:1]=[C:2]([OH:3])[CH2:4][CH2:5][CH2:6][c:7]1[cH:8][cH:9][cH:10][c:11]([Cl:12])[cH:13]1
O=C(O)CCC(=O)c1cccc(Cl)c1
O=C(O)CCCc1cccc(Cl)c1
null
null
C(COCCO)O
Reduction
OtherReaction
bdac4f77103f4da1c5b42ea95e05b0b7b31176b78204db5f4144ffca7b3d54d5
f9ba67182f94acd5fbe41487f8f71e26bccf898b8fc8091ef46f4363de5628d4
c1ccccc1
O=[C;H0;D3;+0:1](-[C:2]-[C:3]-[C:4](=[O;D1;H0:5])-[O;D1;H1:6])-[c:7](:[c:8]):[c:9]>>[O;D1;H0:5]=[C:4](-[O;D1;H1:6])-[C:3]-[C:2]-[CH2;D2;+0:1]-[c:7](:[c:8]):[c:9]
90.8
[{"value": 90.8, "product": "ClC=1C=C(C=CC1)CCCC(=O)O", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
null
null
To a 300 ml round-bottomed flask equipped with magnetic stirrer and reflux condenser was charged 23.7 g of 87% potassium hydroxide and 150 ml of diethyleneglycol, With stirring, 23 g of 3-(3-chlorobenzoyl)propionic acid was added followed by 24 g of 85% hydrazine. The mixture was heated to reflux for 2 hours when 50 ml...
10.6084/m9.figshare.5104873.v1
null
Ketone
null
null
null
c1ccccc1
Other
C(COCCO)O
null
null
O=C(O)CCC(=O)c1cccc(Cl)c1>C(COCCO)O>O=C(O)CCCc1cccc(Cl)c1
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-ce1f4e690dcc46599c10634baebf9087
CNN.O=C(O)CCC(=O)c1ccc(Cl)cc1>>CN1N=C(c2ccc(Cl)cc2)CCC1=O
ClC1=CC=C(C(=O)CCC(=O)O)C=C1.CNN>>ClC1=CC=C(C=C1)C=1CCC(N(N1)C)=O
[CH3:1][NH:2][NH2:3].O=[C:4]([c:5]1[cH:6][cH:7][c:8]([Cl:9])[cH:10][cH:11]1)[CH2:12][CH2:13][C:14](O)=[O:15]>>[CH3:1][N:2]1[N:3]=[C:4]([c:5]2[cH:6][cH:7][c:8]([Cl:9])[cH:10][cH:11]2)[CH2:12][CH2:13][C:14]1=[O:15]
CNN.O=C(O)CCC(=O)c1ccc(Cl)cc1
CN1N=C(c2ccc(Cl)cc2)CCC1=O
null
null
C(C)O
Acylation
OtherReaction
4e477d09c29dc9649665c2a512a7ab66ed0db9837b745e511eba3c76a3cc18d7
30de68c4dde17a0553a43eee47b1b865b8390bb08557512a59e6e71e0ed0ad51
O=C1CCC(c2ccccc2)=NN1
O-[C;H0;D3;+0:1](=[O;D1;H0:2])-[C:3]-[C:4]-[C;H0;D3;+0:5](=O)-[c:6](:[c:7]):[c:8].[C;D1;H3:9]-[NH;D2;+0:10]-[NH2;D1;+0:11]>>[C;D1;H3:9]-[N;H0;D3;+0:10]1-[N;H0;D2;+0:11]=[C;H0;D3;+0:5](-[c:6](:[c:7]):[c:8])-[C:4]-[C:3]-[C;H0;D3;+0:1]-1=[O;D1;H0:2]
null
[]
null
null
null
null
To a 250 ml flask equipped with magnetic stirrer and reflux condenser was charged 10 g of 3-(4-chlorobenzoyl)-propionic acid, 250 ml of absolute ethanol, and 2.5 ml of methyl hydrazine. The reaction was refluxed for 3 hours and cooled to yield a solid which was collected by vacuum filtration, washed with 50 ml of hexan...
10.6084/m9.figshare.5104873.v1
null
Hydrazine.Carboxylic acid.Ketone
Hydrazone amide
null
C1=N[NH]CCC1
C1=N[NH]CCC1.c1ccccc1
HO-
C(C)O
null
null
CNN.O=C(O)CCC(=O)c1ccc(Cl)cc1>C(C)O>CN1N=C(c2ccc(Cl)cc2)CCC1=O
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-41e667fc94ef4b21b0e687948a96209d
CC(=O)CCC(=O)O.O=Cc1ccc(Cl)cc1>>O=C(O)CCC(=O)C=Cc1ccc(Cl)cc1
ClC1=CC=C(C=O)C=C1.C(CCC(=O)C)(=O)O.N1CCCCC1.C1(=CC=CC=C1)C>>ClC1=CC=C(C=CC(=O)CCC(=O)O)C=C1
[O:1]=[C:2]([OH:3])[CH2:4][CH2:5][C:6](=[O:7])[CH3:8].O=[CH:9][c:10]1[cH:11][cH:12][c:13]([Cl:14])[cH:15][cH:16]1>>[O:1]=[C:2]([OH:3])[CH2:4][CH2:5][C:6](=[O:7])[CH:8]=[CH:9][c:10]1[cH:11][cH:12][c:13]([Cl:14])[cH:15][cH:16]1
CC(=O)CCC(=O)O.O=Cc1ccc(Cl)cc1
O=C(O)CCC(=O)C=Cc1ccc(Cl)cc1
null
null
O
C-C Coupling
Aldehyde and ketone to alpha,beta-unsaturated carbonyl
df1bdbab1a06af9561d74fe6bc94ee8bda1d14faad9db1ada3a214bd64a24cf8
c93e93ada40f7f922a54fe24d38f540ecf5ff25d55d497f79f5f400f75d0c7ae
c1ccccc1
O=[CH;D2;+0:1]-[c:2](:[c:3]):[c:4].[C:5]-[C:6](-[CH3;D1;+0:7])=[O;D1;H0:8]>>[C:5]-[C:6](=[O;D1;H0:8])-[CH;D2;+0:7]=[CH;D2;+0:1]-[c:2](:[c:3]):[c:4]
44
[{"value": 44.0, "product": "ClC1=CC=C(C=CC(=O)CCC(=O)O)C=C1", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
null
null
To a dry 250 ml flask equipped with a magnetic stirrer, Dean-Stark trap, and reflux condenser was charged 15 g of 4-chlorobenzaldehyde, 12.4 g levulenic acid, 5.7 ml of piperidine, and 100 ml of toluene. The reaction was refluxed for 3 hours, after which no water was observed to azeotrope from the solution. The reactio...
10.6084/m9.figshare.5104873.v1
null
Aldehyde.Ketone
Ketone
null
null
c1ccccc1
HO-
O
null
null
CC(=O)CCC(=O)O.O=Cc1ccc(Cl)cc1>O>O=C(O)CCC(=O)C=Cc1ccc(Cl)cc1
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-4f03ae878f504b23bfedb43e4307c94e
COc1ccc(C(=O)[O-])c(C)c1[N+](=O)[O-]>>COc1ccc(C(=O)O)cc1[N+](=O)[O-]
[N+](=O)([O-])C=1C(=C(C(=O)[O-])C=CC1OC)C.[OH-].[K+]>>[N+](=O)([O-])C=1C=C(C(=O)O)C=CC1OC
C[c:10]1[c:6]([C:7](=[O:8])[O-:9])[cH:5][cH:4][c:3]([O:2][CH3:1])[c:11]1[N+:12](=[O:13])[O-:14]>>[CH3:1][O:2][c:3]1[cH:4][cH:5][c:6]([C:7](=[O:8])[OH:9])[cH:10][c:11]1[N+:12](=[O:13])[O-:14]
COc1ccc(C(=O)[O-])c(C)c1[N+](=O)[O-]
COc1ccc(C(=O)O)cc1[N+](=O)[O-]
null
null
O1CCCC1
Miscellaneous
OtherReaction
ec2bcf645eed3485ae21dd491bac7887e7ecc8e6727067de36c08c87eaa3e98c
d003579d88c8e6390ed4fac608b8ce68d334559ff02e2f3d9c9936750b60a874
c1ccccc1
C-[c;H0;D3;+0:1](:[c:2](-[#7;+:3]):[c:4]):[c:5](-[C:6](-[O-;H0;D1:7])=[O;D1;H0:8]):[c:9]>>[#7;+:3]-[c:2](:[c:4]):[cH;D2;+0:1]:[c:5](-[C:6](=[O;D1;H0:8])-[OH;D1;+0:7]):[c:9]
76.6
[{"value": 76.6, "product": "[N+](=O)([O-])C=1C=C(C(=O)O)C=CC1OC", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
12
HOUR
To a 500 ml erlenmeyer flask with magnetic stirrer was charged 10.3 g of 3-nitro-4-methoxy-methylbenzoate, 400 ml tetrahydrofuran, and 3.2 g of 86% potassium hydroxide. The reaction was stirred for 12 hours at ambient temperature, after which the resulting solid was collected by vacuum filtration and washed with 2×100 ...
10.6084/m9.figshare.5104873.v1
null
null
Carboxylic acid
c1ccccc1
c1ccccc1
c1ccccc1
Other
O1CCCC1
null
12
COc1ccc(C(=O)[O-])c(C)c1[N+](=O)[O-]>O1CCCC1>COc1ccc(C(=O)O)cc1[N+](=O)[O-]
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-07e514fe010d477b830fbb79e7963a40
Cc1ccccc1.Cc1cccnc1C#N.O=S(=O)(O)O>>Cc1cccnc1C(=O)NC(C)(C)C
C1(=CC=CC=C1)C.C(#N)C1=NC=CC=C1C.N.OS(=O)(=O)O>>CC(C)(C)NC(=O)C1=NC=CC=C1C
c1c[cH:12][c:11]([CH3:14])[cH:13]c1.[CH3:1][c:2]1[cH:3][cH:4][cH:5][n:6][c:7]1[C:8]#[N:10].O=S(=O)(O)[OH:9]>>[CH3:1][c:2]1[cH:3][cH:4][cH:5][n:6][c:7]1[C:8](=[O:9])[NH:10][C:11]([CH3:12])([CH3:13])[CH3:14]
Cc1ccccc1.Cc1cccnc1C#N.O=S(=O)(O)O
Cc1cccnc1C(=O)NC(C)(C)C
null
null
O.C(C)(C)(C)O
Heteroatom Alkylation and Arylation
OtherReaction
780c5bd372645be2428cf4f314e6765c167cb2cb84e2e593d576e2f8633a9926
aaa659fb1f3b655f5022532af787efa2716aa193a615252f400a1fe3a0f40998
c1ccncc1
O-S(=O)(=O)-[OH;D1;+0:1].[C;D1;H3:2]-[c;H0;D3;+0:3]1:[cH;D2;+0:4]:c:c:c:[cH;D2;+0:5]:1.[N;H0;D1;+0:6]#[C;H0;D2;+0:7]-[c:8](:[c:9]):[#7;a:10]:[c:11]>>[C;D1;H3:2]-[C;H0;D4;+0:3](-[CH3;D1;+0:4])(-[CH3;D1;+0:5])-[NH;D2;+0:6]-[C;H0;D3;+0:7](=[O;H0;D1;+0:1])-[c:8](:[c:9]):[#7;a:10]:[c:11]
97
[{"value": 97.0, "product": "CC(C)(C)NC(=O)C1=NC=CC=C1C", "details": "PERCENTYIELD", "is_desired": false}]
70
CELSIUS
30
MINUTE
Suspend 2-cyano-3-methyl pyridine (400 g) in t-butanol (800 mL) and heat to 70° C. Add concentrated H2SO4 (400 mL) dropwise over 45 minutes. Maintain the temperature at 75° C., until the reaction is complete, and for an additional 30 minutes. Dilute the mixture with water (400 mL), charge with toluene (600 mL) and brin...
10.6084/m9.figshare.5104873.v1
null
Nitrile
Secondary amide
c1ccccc1
null
c1ccncc1
Other
O.C(C)(C)(C)O
70
0.5
Cc1ccccc1.Cc1cccnc1C#N.O=S(=O)(O)O>O.C(C)(C)(C)O>Cc1cccnc1C(=O)NC(C)(C)C
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-b713158f99fb4e31b927599348f3f54c
N#Cc1ccc(CBr)cc1.O=C1NCCN1>>N#Cc1ccc(CN2CCN(Cc3ccc(C#N)cc3)C2=O)cc1
O.BrCC1=CC=C(C#N)C=C1.[H-].[Na+].N1C(NCC1)=O>>O=C1N(CCN1CC1=CC=C(C#N)C=C1)CC1=CC=C(C#N)C=C1
Br[CH2:7][c:6]1[cH:5][cH:4][c:3]([C:2]#[N:1])[cH:24][cH:23]1.[NH:8]1[CH2:9][CH2:15][NH:11][C:21]1=[O:22]>>[N:1]#[C:2][c:3]1[cH:4][cH:5][c:6]([CH2:7][N:8]2[CH2:9][CH2:10][N:11]([CH2:12][c:13]3[cH:14][cH:15][c:16]([C:17]#[N:18])[cH:19][cH:20]3)[C:21]2=[O:22])[cH:23][cH:24]1
N#Cc1ccc(CBr)cc1.O=C1NCCN1
N#Cc1ccc(CN2CCN(Cc3ccc(C#N)cc3)C2=O)cc1
null
null
CN(C=O)C
Aromatic Heterocycle Formation
OtherReaction
39571f641692bae0ab2e4fb7e56baf0a046bbe68e5d15065d8f936b61702d85c
04064b000c1f037cb6379c4a9b891971302bcd094d2302ea56061b3b37327222
O=C1N(Cc2ccccc2)CCN1Cc1ccccc1
Br-[CH2;D2;+0:1]-[c:2](:[c:3]):[c:4].[O;D1;H0:5]=[C:6]1-[NH;D2;+0:7]-[CH2;D2;+0:8]-[CH2;D2;+0:9]-[NH;D2;+0:10]-1>>[C:11]-[c:12](:[c:13]):[cH;D2;+0:8]:[c:14]:[c:15]-[C:16]-[N;H0;D3;+0:7]1-[C:17]-[CH2;D2;+0:9]-[N;H0;D3;+0:10](-[CH2;D2;+0:1]-[c:2](:[c:3]):[c:4])-[C:6]-1=[O;D1;H0:5]
null
[]
null
null
1
HOUR
To sodium hydride (2.4 g, 60 mmol) in dimethylformamide (50 mL) at 0° C. was added imidazolin-2-one (2.6 g, 30 mmol). After stirring for 20 minutes 4-(bromomethyl)benzonitrile (13 g, 66 mmol) was added and the mixture was warmed to ambient temperature. After stirring for 1 hour the reaction was poured into water and a ...
10.6084/m9.figshare.5104873.v1
null
Primary halide.Urea
Urea.Nitrile
C1CNCN1
C1C[NH]C[NH]1.c1ccccc1
c1ccccc1.C1C[NH]C[NH]1.c1ccccc1
Br-
CN(C=O)C
null
1
N#Cc1ccc(CBr)cc1.O=C1NCCN1>CN(C=O)C>N#Cc1ccc(CN2CCN(Cc3ccc(C#N)cc3)C2=O)cc1
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-e289c3d74b254a4196a9c35ea0894330
CN(C)c1ccc(C(O)C(=O)c2ccccc2)cc1.NC(N)=O>>CN(C)c1ccc(-c2[nH]c(=O)[nH]c2-c2ccccc2)cc1
NC(=O)N.CN(C1=CC=C(C=C1)C(C(=O)C1=CC=CC=C1)O)C>>CN(C1=CC=C(C=C1)C=1NC(NC1C1=CC=CC=C1)=O)C
O=[C:13]([CH:8](O)[c:7]1[cH:6][cH:5][c:4]([N:2]([CH3:1])[CH3:3])[cH:21][cH:20]1)[c:14]1[cH:15][cH:16][cH:17][cH:18][cH:19]1.[NH2:9][C:10](=[O:11])[NH2:12]>>[CH3:1][N:2]([CH3:3])[c:4]1[cH:5][cH:6][c:7](-[c:8]2[nH:9][c:10](=[O:11])[nH:12][c:13]2-[c:14]2[cH:15][cH:16][cH:17][cH:18][cH:19]2)[cH:20][cH:21]1
CN(C)c1ccc(C(O)C(=O)c2ccccc2)cc1.NC(N)=O
CN(C)c1ccc(-c2[nH]c(=O)[nH]c2-c2ccccc2)cc1
null
null
C(C)(=O)O
Aromatic Heterocycle Formation
OtherReaction
7a04490902783a9d1d6099ad78b95538301d0ef7b8b6cc364284d393dbdf37cd
19da97726e6dc44d537eff971a50046c3e80ca62fdecca0b64533a3c10927d47
O=c1[nH]c(-c2ccccc2)c(-c2ccccc2)[nH]1
O-[CH;D3;+0:1](-[C;H0;D3;+0:2](=O)-[c;H0;D3;+0:3](:[c:4]:[c:5]):[c:6]:[c:7])-[c;H0;D3;+0:8](:[c:9]:[c:10]):[c:11]:[c:12].[NH2;D1;+0:13]-[C;H0;D3;+0:14](-[NH2;D1;+0:15])=[O;D1;H0:16]>>[O;D1;H0:16]=[c;H0;D3;+0:14]1:[nH;D2;+0:13]:[c;H0;D3;+0:2](-[c;H0;D3;+0:3](:[c:4]:[c:5]):[c:6]:[c:7]):[c;H0;D3;+0:1](-[c;H0;D3;+0:8](:[c:...
null
[]
120
CELSIUS
2
HOUR
To acetic acid (2 mL) was added urea (0.6 g, 10 mmol) and 2-(4-dimethylaminophenyl)-2-hydroxy-1-phenylethanone (2.6 g, 10 mmol). After stirring for 2 hours at 120° C., the reaction was cooled to ambient temperature. The resulting solid was filtered, washed with ether, and dried in vacuo to give 4-(4-dimethylaminophenyl...
10.6084/m9.figshare.5104873.v1
null
Ketone.Urea.Secondary alcohol
null
null
c1c[nH]cn1
c1ccccc1.c1c[nH]cn1.c1ccccc1
HO-
C(C)(=O)O
120
2
CN(C)c1ccc(C(O)C(=O)c2ccccc2)cc1.NC(N)=O>C(C)(=O)O>CN(C)c1ccc(-c2[nH]c(=O)[nH]c2-c2ccccc2)cc1
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-aad224480b7f4172a95830c33af130b0
N#Cc1cccc(CBr)c1.O=c1[nH]c(-c2ccccc2)c(-c2ccccc2)[nH]1>>N#Cc1cccc(Cn2c(-c3ccccc3)c(-c3ccccc3)[nH]c2=O)c1
C1(=CC=CC=C1)C=1NC(NC1C1=CC=CC=C1)=O.BrCC=1C=C(C#N)C=CC1.[H-].[Na+]>>C1(=CC=CC=C1)C=1NC(N(C1C1=CC=CC=C1)CC=1C=C(C#N)C=CC1)=O
Br[CH2:8][c:7]1[cH:6][cH:5][cH:4][c:3]([C:2]#[N:1])[cH:27]1.[nH:9]1[c:10](-[c:11]2[cH:12][cH:13][cH:14][cH:15][cH:16]2)[c:17](-[c:18]2[cH:19][cH:20][cH:21][cH:22][cH:23]2)[nH:24][c:25]1=[O:26]>>[N:1]#[C:2][c:3]1[cH:4][cH:5][cH:6][c:7]([CH2:8][n:9]2[c:10](-[c:11]3[cH:12][cH:13][cH:14][cH:15][cH:16]3)[c:17](-[c:18]3[cH:1...
N#Cc1cccc(CBr)c1.O=c1[nH]c(-c2ccccc2)c(-c2ccccc2)[nH]1
N#Cc1cccc(Cn2c(-c3ccccc3)c(-c3ccccc3)[nH]c2=O)c1
null
null
CN(C=O)C
Heteroatom Alkylation and Arylation
N-alkylation of secondary amines with alkyl halides
b9d84e1ee028da6e8c5d8924d45fbf8f3755d9adc2caf0035bd5ed7f30f5ee03
2e1e5fd9557b69cb528f6b2ffd179c67ef24ecb1a2c3994e1cdf0efe7ae19e9c
O=c1[nH]c(-c2ccccc2)c(-c2ccccc2)n1Cc1ccccc1
Br-[CH2;D2;+0:1]-[c:2](:[c:3]):[c:4].[O;D1;H0:5]=[c:6]1:[#7;a:7]:[c:8](-[c:9]):[c:10](-[c:11]):[nH;D2;+0:12]:1>>[O;D1;H0:5]=[c:6]1:[#7;a:7]:[c:8](-[c:9]):[c:10](-[c:11]):[n;H0;D3;+0:12]:1-[CH2;D2;+0:1]-[c:2](:[c:3]):[c:4]
null
[]
null
null
null
null
In a manner similar to Preparation 1 above, 2,3-dihydro-4,5-diphenyl-1H-imidazol-2-one (1.2 g, 5 mmol) was reacted with 3-(bromomethyl)benzonitrile (0.39 g, mmol) and sodium hydride (0.18 g, 5 mmol) in dimethylformamide (20 mL) to give 3-[(2,3-dihydro-4,5-diphenyl-2-oxo-1H-imidazol-1-yl)methyl]benzonitrile after chroma...
10.6084/m9.figshare.5104873.v1
null
Primary halide
null
c1c[nH]cn1
c1c[nH]cn1
c1ccccc1.c1ccccc1.c1ccccc1.c1c[nH]cn1
HBr
CN(C=O)C
null
null
N#Cc1cccc(CBr)c1.O=c1[nH]c(-c2ccccc2)c(-c2ccccc2)[nH]1>CN(C=O)C>N#Cc1cccc(Cn2c(-c3ccccc3)c(-c3ccccc3)[nH]c2=O)c1
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-06bbfeb3be78487fb44540ecbac09d5f
COC(=O)c1cccc(CBr)c1.O=c1[nH]c(-c2ccccc2)c(-c2ccccc2)[nH]1>>COC(=O)c1cccc(Cn2c(-c3ccccc3)c(-c3ccccc3)[nH]c2=O)c1
C1(=CC=CC=C1)C=1NC(NC1C1=CC=CC=C1)=O.BrCC=1C=C(C(=O)OC)C=CC1.Cl>>COC(=O)C=1C=C(C=CC1)CN1C(NC(=C1C1=CC=CC=C1)C1=CC=CC=C1)=O
Br[CH2:10][c:9]1[cH:8][cH:7][cH:6][c:5]([C:3]([O:2][CH3:1])=[O:4])[cH:29]1.[nH:11]1[c:12](-[c:13]2[cH:14][cH:15][cH:16][cH:17][cH:18]2)[c:19](-[c:20]2[cH:21][cH:22][cH:23][cH:24][cH:25]2)[nH:26][c:27]1=[O:28]>>[CH3:1][O:2][C:3](=[O:4])[c:5]1[cH:6][cH:7][cH:8][c:9]([CH2:10][n:11]2[c:12](-[c:13]3[cH:14][cH:15][cH:16][cH:...
COC(=O)c1cccc(CBr)c1.O=c1[nH]c(-c2ccccc2)c(-c2ccccc2)[nH]1
COC(=O)c1cccc(Cn2c(-c3ccccc3)c(-c3ccccc3)[nH]c2=O)c1
null
null
CN(C)C=O
Heteroatom Alkylation and Arylation
N-alkylation of secondary amines with alkyl halides
b9d84e1ee028da6e8c5d8924d45fbf8f3755d9adc2caf0035bd5ed7f30f5ee03
2e1e5fd9557b69cb528f6b2ffd179c67ef24ecb1a2c3994e1cdf0efe7ae19e9c
O=c1[nH]c(-c2ccccc2)c(-c2ccccc2)n1Cc1ccccc1
Br-[CH2;D2;+0:1]-[c:2](:[c:3]):[c:4].[O;D1;H0:5]=[c:6]1:[#7;a:7]:[c:8](-[c:9]):[c:10](-[c:11]):[nH;D2;+0:12]:1>>[O;D1;H0:5]=[c:6]1:[#7;a:7]:[c:8](-[c:9]):[c:10](-[c:11]):[n;H0;D3;+0:12]:1-[CH2;D2;+0:1]-[c:2](:[c:3]):[c:4]
25
[{"value": 25.0, "product": "COC(=O)C=1C=C(C=CC1)CN1C(NC(=C1C1=CC=CC=C1)C1=CC=CC=C1)=O", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
50
CELSIUS
30
MINUTE
To 2,3-dihydro-4,5-diphenyl-1H-imidazol-2-one (4.76 g, 20 mmol) in 50 mL DMF was added to a suspension of Nail (0.8 g, 20 mmol) in 25 mL DMF. The suspension was stirred at ambient temperatures for 30 minutes, then heated to 50° C. for 30 minutes. A solution of methyl 3-bromomethylbenzoate (2.86 g, 12.5 mmol) in 20 mL D...
10.6084/m9.figshare.5104873.v1
null
Primary halide
null
c1c[nH]cn1
c1c[nH]cn1
c1ccccc1.c1ccccc1.c1ccccc1.c1c[nH]cn1
HBr
CN(C)C=O
50
0.5
COC(=O)c1cccc(CBr)c1.O=c1[nH]c(-c2ccccc2)c(-c2ccccc2)[nH]1>CN(C)C=O>COC(=O)c1cccc(Cn2c(-c3ccccc3)c(-c3ccccc3)[nH]c2=O)c1
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-fd90658687c84716b19eb33da57e2759
N#Cc1ccc2ccc(CBr)cc2c1.N#Cc1cccc(Cn2c(-c3ccccc3)c(-c3ccccc3)[nH]c2=O)c1>>N#Cc1cccc(Cn2c(-c3ccccc3)c(-c3ccccc3)n(Cc3ccc4ccc(C#N)cc4c3)c2=O)c1
C1(=CC=CC=C1)C=1NC(N(C1C1=CC=CC=C1)CC=1C=C(C#N)C=CC1)=O.BrCC1=CC=C2C=CC(=CC2=C1)C#N>>C(#N)C=1C=C(C=CC1)CN1C(N(C(=C1C1=CC=CC=C1)C1=CC=CC=C1)CC1=CC=C2C=CC(=CC2=C1)C#N)=O
Br[CH2:25][c:26]1[cH:27][cH:28][c:29]2[cH:30][cH:31][c:32]([C:33]#[N:34])[cH:35][c:36]2[cH:37]1.[N:1]#[C:2][c:3]1[cH:4][cH:5][cH:6][c:7]([CH2:8][n:9]2[c:10](-[c:11]3[cH:12][cH:13][cH:14][cH:15][cH:16]3)[c:17](-[c:18]3[cH:19][cH:20][cH:21][cH:22][cH:23]3)[nH:24][c:38]2=[O:39])[cH:40]1>>[N:1]#[C:2][c:3]1[cH:4][cH:5][cH:6...
N#Cc1ccc2ccc(CBr)cc2c1.N#Cc1cccc(Cn2c(-c3ccccc3)c(-c3ccccc3)[nH]c2=O)c1
N#Cc1cccc(Cn2c(-c3ccccc3)c(-c3ccccc3)n(Cc3ccc4ccc(C#N)cc4c3)c2=O)c1
null
null
null
Heteroatom Alkylation and Arylation
N-alkylation of secondary amines with alkyl halides
b9d84e1ee028da6e8c5d8924d45fbf8f3755d9adc2caf0035bd5ed7f30f5ee03
2e1e5fd9557b69cb528f6b2ffd179c67ef24ecb1a2c3994e1cdf0efe7ae19e9c
O=c1n(Cc2ccccc2)c(-c2ccccc2)c(-c2ccccc2)n1Cc1ccc2ccccc2c1
Br-[CH2;D2;+0:1]-[c:2](:[c:3]):[c:4].[C:5]-[#7;a:6]1:[c:7](-[c:8]):[c:9](-[c:10]):[nH;D2;+0:11]:[c:12]:1=[O;D1;H0:13]>>[C:5]-[#7;a:6]1:[c:7](-[c:8]):[c:9](-[c:10]):[n;H0;D3;+0:11](-[CH2;D2;+0:1]-[c:2](:[c:3]):[c:4]):[c:12]:1=[O;D1;H0:13]
null
[]
null
null
null
null
In a manner similar to Preparation 2 above, 3-[(2,3-dihydro-4,5-diphenyl-2-oxo-1H-imidazol-1-yl) methyl]benzonitrile was reacted with 7-(bromomethyl)-naphthalene-2-carbonitrile to give 7-[[3-(3-cyanophenyl)methyl-2,3-dihydro-4,5-diphenyl-2-oxo-1H-imidazol-1-yl]methyl]naphthalene-2-carbonitrile; NMR (CDCl3) 8.05 (s,1), ...
10.6084/m9.figshare.5104873.v1
null
Primary halide
null
c1c[nH]cn1
c1c[nH]cn1
c1ccccc1.c1ccccc1.c1ccccc1.c1ccc2ccccc2c1.c1c[nH]cn1
HBr
null
null
null
N#Cc1ccc2ccc(CBr)cc2c1.N#Cc1cccc(Cn2c(-c3ccccc3)c(-c3ccccc3)[nH]c2=O)c1>>N#Cc1cccc(Cn2c(-c3ccccc3)c(-c3ccccc3)n(Cc3ccc4ccc(C#N)cc4c3)c2=O)c1
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-f942832a149344ee8ae24b50f8c14966
CO.O=C(O)C1Cc2ccccc2CN1>>COC(=O)C1Cc2ccccc2CN1
C(C)(=O)Cl.CO.C1NC(CC2=CC=CC=C12)C(=O)O>>COC(=O)C1NCC2=CC=CC=C2C1
O[CH3:1].[OH:2][C:3](=[O:4])[CH:5]1[CH2:6][c:7]2[cH:8][cH:9][cH:10][cH:11][c:12]2[CH2:13][NH:14]1>>[CH3:1][O:2][C:3](=[O:4])[CH:5]1[CH2:6][c:7]2[cH:8][cH:9][cH:10][cH:11][c:12]2[CH2:13][NH:14]1
CO.O=C(O)C1Cc2ccccc2CN1
COC(=O)C1Cc2ccccc2CN1
null
null
CN(C)C=O
Heteroatom Alkylation and Arylation
Esterification of Carboxylic Acids
961bfcd5802efbb4a2d5a1e38cbfb6654b5b78f769c3570df49b858a6f105ab6
0a622556a49b258b9020bd3a5bdd1fa9237e7093cf9b09de3a6b575ffe935dcd
c1ccc2c(c1)CCNC2
O-[CH3;D1;+0:1].[#7:2]-[C:3]-[C:4](=[O;D1;H0:5])-[OH;D1;+0:6]>>[#7:2]-[C:3]-[C:4](=[O;D1;H0:5])-[O;H0;D2;+0:6]-[CH3;D1;+0:1]
46.6
[{"value": 46.6, "product": "COC(=O)C1NCC2=CC=CC=C2C1", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
0
CELSIUS
10
MINUTE
Acetyl chloride (0.88 g) was added to methanol (100 ml) with stirring at 0° C. After 10 minutes, 1,2,3,4-tetrahydroisoquinoline-3-carboxylic acid (J. Am. Chem. Soc., 1962, 48, 4487-4494) (2.0 g) was added; the reaction was allowed to warm to room temperature and stirred overnight. DMF (1 ml) was then added and stirring...
10.6084/m9.figshare.5104873.v1
null
Carboxylic acid.Methanol
Ester
null
null
c1ccc2c(c1)CCNC2
HO-
CN(C)C=O
0
0.166667
CO.O=C(O)C1Cc2ccccc2CN1>CN(C)C=O>COC(=O)C1Cc2ccccc2CN1
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-0c015ee7e7924c23b9f14267ea629a04
CS(=O)(=O)OCOc1ccccc1.O=S(=O)(O)Cl>>COc1ccc(S(=O)(=O)Cl)cc1OS(C)(=O)=O
ClS(=O)(=O)O.CS(=O)(=O)OCOC1=CC=CC=C1.C(C(=O)Cl)(=O)Cl.C1(=CC=CC=C1)C.C(C(=O)Cl)(=O)Cl>>CS(=O)(=O)OC=1C=C(C=CC1OC)S(=O)(=O)Cl
[CH2:1]([O:2][c:3]1[cH:4][cH:5][cH:6][cH:11][cH:12]1)[O:13][S:14]([CH3:15])(=[O:16])=[O:17].O=[S:7]([OH:8])(=[O:9])[Cl:10]>>[CH3:1][O:2][c:3]1[cH:4][cH:5][c:6]([S:7](=[O:8])(=[O:9])[Cl:10])[cH:11][c:12]1[O:13][S:14]([CH3:15])(=[O:16])=[O:17]
CS(=O)(=O)OCOc1ccccc1.O=S(=O)(O)Cl
COc1ccc(S(=O)(=O)Cl)cc1OS(C)(=O)=O
null
CN(C)C=O
ClCCl
Functional Group Interconversion
OtherReaction
4f315fa4b3128c51c380de69526b2c215346c70fd2b64d262976c5395499ed83
0e61b0140d418f3a714817b5060773e18c160606500a286b714ae0a828923f0e
c1ccccc1
O=[S;H0;D4;+0:1](-[Cl;D1;H0:2])(=[O;D1;H0:3])-[OH;D1;+0:4].[C;D1;H3:5]-[#16:6](=[O;D1;H0:7])(=[O;D1;H0:8])-[O;H0;D2;+0:9]-[CH2;D2;+0:10]-[#8:11]-[c:12]1:[c:13]:[c:14]:[cH;D2;+0:15]:[c:16]:[cH;D2;+0:17]:1>>[C;D1;H3:5]-[#16:6](=[O;D1;H0:7])(=[O;D1;H0:8])-[O;H0;D2;+0:9]-[c;H0;D3;+0:17]1:[c:16]:[c;H0;D3;+0:15](-[S;H0;D4;+0...
null
[]
-10
CELSIUS
4
HOUR
A solution of 2-(methanesulphonyloxy)methoxybenzene (0.822 g) in dichloromethane (15 ml) was stirred and cooled to -10° C. under a nitrogen atmosphere. A solution of chlorosulphonic acid (0.27 ml) in dichloromethane (5 ml) was then added dropwise over a period of 1 hour, maintaining the temperature below 0° C. The mixt...
10.6084/m9.figshare.5104873.v1
null
Mesylate.Ether
Mesylate.Ether.Sulfonyl halide
c1ccccc1
c1ccccc1
c1ccccc1
HO-
CN(C)C=O.ClCCl
-10
4
CS(=O)(=O)OCOc1ccccc1.O=S(=O)(O)Cl>CN(C)C=O.ClCCl>COc1ccc(S(=O)(=O)Cl)cc1OS(C)(=O)=O
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-ff57e297cfdc46e5b5870e456c42198a
COc1ccc(S(=O)(=O)N2CCc3ccccc32)cc1OS(C)(=O)=O>>COc1ccc(S(=O)(=O)N2CCc3ccccc32)cc1O
CS(=O)(=O)OC=1C=C(C=CC1OC)S(=O)(=O)N1CCC2=CC=CC=C12.[OH-].[Na+]>>OC=1C=C(C=CC1OC)S(=O)(=O)N1CCC2=CC=CC=C12
CS(=O)(=O)[O:21][c:20]1[c:3]([O:2][CH3:1])[cH:4][cH:5][c:6]([S:7](=[O:8])(=[O:9])[N:10]2[CH2:11][CH2:12][c:13]3[cH:14][cH:15][cH:16][cH:17][c:18]32)[cH:19]1>>[CH3:1][O:2][c:3]1[cH:4][cH:5][c:6]([S:7](=[O:8])(=[O:9])[N:10]2[CH2:11][CH2:12][c:13]3[cH:14][cH:15][cH:16][cH:17][c:18]32)[cH:19][c:20]1[OH:21]
COc1ccc(S(=O)(=O)N2CCc3ccccc32)cc1OS(C)(=O)=O
COc1ccc(S(=O)(=O)N2CCc3ccccc32)cc1O
null
null
null
Functional Group Interconversion
OtherReaction
ee3aaebba994f49df1ba424e944fca44eeafa016a3e36bf167dd8b29195eaed8
01728c3d642b2daee982c52b87a87c062dbb984fb985d3f341f8d76fc5df3eb8
O=S(=O)(c1ccccc1)N1CCc2ccccc21
C-S(=O)(=O)-[O;H0;D2;+0:1]-[c:2](:[c:3]):[c:4]>>[OH;D1;+0:1]-[c:2](:[c:3]):[c:4]
100.5
[{"value": 100.5, "product": "OC=1C=C(C=CC1OC)S(=O)(=O)N1CCC2=CC=CC=C12", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
null
null
A solution of N-(3-methanesulphonyloxy-4-methoxybenzenesulphonyl)-1,2-dihydroindole (1 g) and saturated aqueous sodium hydroxide solution (2 ml) was heated at 85°-90° C. for 2 hours. The solvent was removed in vacuo and the residue partitioned between ethyl acetate (5 ml) and water (10 ml). The aqueous phase was acidif...
10.6084/m9.figshare.5104873.v1
null
Mesylate
Aromatic alcohol
null
null
c1ccccc1.c1ccc2c(c1)CC[NH]2
HO-
null
null
null
COc1ccc(S(=O)(=O)N2CCc3ccccc32)cc1OS(C)(=O)=O>>COc1ccc(S(=O)(=O)N2CCc3ccccc32)cc1O
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-80b4d3c6a338477cbce6e4a97e49acd8
COc1ccc(S(=O)(=O)Cl)cc1OC.c1ccc2c(c1)CCCN2>>COc1ccc(S(=O)(=O)N2CCCc3ccccc32)cc1OC
N1CCCC2=CC=CC=C12.COC=1C=C(C=CC1OC)S(=O)(=O)Cl.C(C)N(CC)CC>>COC=1C=C(C=CC1OC)S(=O)(=O)N1CCCC2=CC=CC=C12
Cl[S:7]([c:6]1[cH:5][cH:4][c:3]([O:2][CH3:1])[c:21]([O:22][CH3:23])[cH:20]1)(=[O:8])=[O:9].[NH:10]1[CH2:11][CH2:12][CH2:13][c:14]2[cH:15][cH:16][cH:17][cH:18][c:19]21>>[CH3:1][O:2][c:3]1[cH:4][cH:5][c:6]([S:7](=[O:8])(=[O:9])[N:10]2[CH2:11][CH2:12][CH2:13][c:14]3[cH:15][cH:16][cH:17][cH:18][c:19]32)[cH:20][c:21]1[O:22]...
COc1ccc(S(=O)(=O)Cl)cc1OC.c1ccc2c(c1)CCCN2
COc1ccc(S(=O)(=O)N2CCCc3ccccc32)cc1OC
null
null
ClCCl
Acylation
Sulfonamide synthesis (Schotten-Baumann) secondary amine
bdce99988baba5b5a8e112b2aa8881a4125937433bf8ddee5495587b5e0d21b3
b7aca5a5d690b0846685a854bc946849e1041bfc3965161290b5ffb2821af09e
O=S(=O)(c1ccccc1)N1CCCc2ccccc21
Cl-[S;H0;D4;+0:1](=[O;D1;H0:2])(=[O;D1;H0:3])-[c:4](:[c:5]):[c:6].[C:7]-[C:8]-[NH;D2;+0:9]-[c:10](:[c:11]):[c:12]>>[C:7]-[C:8]-[N;H0;D3;+0:9](-[S;H0;D4;+0:1](=[O;D1;H0:2])(=[O;D1;H0:3])-[c:4](:[c:5]):[c:6])-[c:10](:[c:11]):[c:12]
null
[]
null
null
24
HOUR
1,2,3,4-Tetrahydroquinoline (0.29 ml) was added to a suspension of 3,4-dimethoxybenzene sulphonyl chloride (0.50 g) in dichloromethane (15 ml) at room temperature. Triethylamine (0.44 ml) was added and the resulting mixture stirred for 24 hours at room temperature. The reaction mixture was then diluted with dichloromet...
10.6084/m9.figshare.5104873.v1
null
Secondary amine.Sulfonyl halide
Tertiary amine
c1ccc2c(c1)CCCN2
c1ccc2c(c1)CCC[NH]2
c1ccccc1.c1ccc2c(c1)CCC[NH]2
HCl
ClCCl
null
24
COc1ccc(S(=O)(=O)Cl)cc1OC.c1ccc2c(c1)CCCN2>ClCCl>COc1ccc(S(=O)(=O)N2CCCc3ccccc32)cc1OC
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-44bcaad266d04c4ebb5e17cd00e7e878
BrCCCOc1ccccc1.COc1ccc(S(=O)(=O)N2CCc3ccccc32)cc1O>>COc1ccc(S(=O)(=O)N2CCc3ccccc32)cc1OCCCOc1ccccc1
OC=1C=C(C=CC1OC)S(=O)(=O)N1CCC2=CC=CC=C12.O(C1=CC=CC=C1)CCCBr.C([O-])([O-])=O.[Cs+].[Cs+]>>O(C1=CC=CC=C1)CCCOC=1C=C(C=CC1OC)S(=O)(=O)N1CCC2=CC=CC=C12
Br[CH2:22][CH2:23][CH2:24][O:25][c:26]1[cH:27][cH:28][cH:29][cH:30][cH:31]1.[CH3:1][O:2][c:3]1[cH:4][cH:5][c:6]([S:7](=[O:8])(=[O:9])[N:10]2[CH2:11][CH2:12][c:13]3[cH:14][cH:15][cH:16][cH:17][c:18]32)[cH:19][c:20]1[OH:21]>>[CH3:1][O:2][c:3]1[cH:4][cH:5][c:6]([S:7](=[O:8])(=[O:9])[N:10]2[CH2:11][CH2:12][c:13]3[cH:14][cH...
BrCCCOc1ccccc1.COc1ccc(S(=O)(=O)N2CCc3ccccc32)cc1O
COc1ccc(S(=O)(=O)N2CCc3ccccc32)cc1OCCCOc1ccccc1
null
null
CN(C=O)C
Heteroatom Alkylation and Arylation
Williamson Ether Synthesis
7e1040116e3a4cf0e8ec5cc7865388d9cd0efabce6d320a1c25a36e411018d8b
d5f4610d46ccc0478471c5bc0fb862644eaf764bbc5d93badb39d54f6ec8e0a5
O=S(=O)(c1cccc(OCCCOc2ccccc2)c1)N1CCc2ccccc21
Br-[CH2;D2;+0:1]-[C:2]-[C:3].[OH;D1;+0:4]-[c:5](:[c:6]):[c:7]>>[C:3]-[C:2]-[CH2;D2;+0:1]-[O;H0;D2;+0:4]-[c:5](:[c:6]):[c:7]
86.8
[{"value": 86.8, "product": "O(C1=CC=CC=C1)CCCOC=1C=C(C=CC1OC)S(=O)(=O)N1CCC2=CC=CC=C12", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
75
CELSIUS
null
null
A solution of N-(3-hydroxy-4-methoxybenzenesulphonyl)- 1,2-dihydroindole (0.2 g) and 3-phenoxypropylbromide (0.15 g) in N,N-dimethylformamide (20 ml) was treated with cesium carbonate (0.3 g) and heated at 75° C. overnight. The solvent was removed in vacuo and the residue partitioned between dichloromethane (30 ml) and...
10.6084/m9.figshare.5104873.v1
null
Primary halide.Aromatic alcohol
Ether
null
null
c1ccccc1.c1ccc2c(c1)CC[NH]2.c1ccccc1
HBr
CN(C=O)C
75
null
BrCCCOc1ccccc1.COc1ccc(S(=O)(=O)N2CCc3ccccc32)cc1O>CN(C=O)C>COc1ccc(S(=O)(=O)N2CCc3ccccc32)cc1OCCCOc1ccccc1
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-1251e1d4efb04be2a0db094b4b863a07
COc1ccc(S(=O)(=O)Cl)cc1OC.O=c1[nH]c(-c2ccccc2)cc2ccccc12>>COc1ccc(S(=O)(=O)n2c(-c3ccccc3)cc3ccccc3c2=O)cc1OC
C1(=CC=CC=C1)C=1NC(=O)C2=CC=CC=C2C1.[H-].[Na+].COC=1C=C(C=CC1OC)S(=O)(=O)Cl>>COC=1C=C(C=CC1OC)S(=O)(=O)N1C(=O)C2=CC=CC=C2C=C1C1=CC=CC=C1
Cl[S:7]([c:6]1[cH:5][cH:4][c:3]([O:2][CH3:1])[c:28]([O:29][CH3:30])[cH:27]1)(=[O:8])=[O:9].[nH:10]1[c:11](-[c:12]2[cH:13][cH:14][cH:15][cH:16][cH:17]2)[cH:18][c:19]2[cH:20][cH:21][cH:22][cH:23][c:24]2[c:25]1=[O:26]>>[CH3:1][O:2][c:3]1[cH:4][cH:5][c:6]([S:7](=[O:8])(=[O:9])[n:10]2[c:11](-[c:12]3[cH:13][cH:14][cH:15][cH:...
COc1ccc(S(=O)(=O)Cl)cc1OC.O=c1[nH]c(-c2ccccc2)cc2ccccc12
COc1ccc(S(=O)(=O)n2c(-c3ccccc3)cc3ccccc3c2=O)cc1OC
null
null
CN(C=O)C
Acylation
OtherReaction
c3c33c450ee7d635baa794cb37e7b92a990cfc48b9c0e915d3035acd3b32cd77
97f7469015d28c17dd04331dd6d96add6c8052624259a8aad52811d647e364c7
O=c1c2ccccc2cc(-c2ccccc2)n1S(=O)(=O)c1ccccc1
Cl-[S;H0;D4;+0:1](=[O;D1;H0:2])(=[O;D1;H0:3])-[c:4](:[c:5]):[c:6].[O;D1;H0:7]=[c:8](:[c:9]):[nH;D2;+0:10]:[c:11](-[c:12]):[c:13]>>[O;D1;H0:7]=[c:8](:[c:9]):[n;H0;D3;+0:10](-[S;H0;D4;+0:1](=[O;D1;H0:2])(=[O;D1;H0:3])-[c:4](:[c:5]):[c:6]):[c:11](-[c:12]):[c:13]
46.7
[{"value": 46.7, "product": "COC=1C=C(C=CC1OC)S(=O)(=O)N1C(=O)C2=CC=CC=C2C=C1C1=CC=CC=C1", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
0
CELSIUS
5
MINUTE
A solution of 3-phenylisocarbostyril (0.1 g) in N,N-dimethylformamide (2 ml) was cooled to 0° C. under an inert atmosphere. Sodium hydride (0.019 g) was added and the resulting mixture stirred at 0° C. for 5 minutes. 3,4-Dimethoxybenzenesulphonylchloride (0.107 g) was added over a 3 minute period, with continued stirri...
10.6084/m9.figshare.5104873.v1
null
Sulfonyl halide
null
c1cc2ccccc2cn1
c1ccc2cnccc2c1
c1ccccc1.c1ccccc1.c1ccc2cnccc2c1
HCl
CN(C=O)C
0
0.083333
COc1ccc(S(=O)(=O)Cl)cc1OC.O=c1[nH]c(-c2ccccc2)cc2ccccc12>CN(C=O)C>COc1ccc(S(=O)(=O)n2c(-c3ccccc3)cc3ccccc3c2=O)cc1OC
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-48f858c335dc420faf30089f06b9929d
COC(=O)C1Cc2ccccc2CN1S(=O)(=O)c1ccc(OC)c(OC)c1>>COc1ccc(S(=O)(=O)N2Cc3ccccc3CC2C(=O)O)cc1OC
COC=1C=C(C=CC1OC)S(=O)(=O)N1CC2=CC=CC=C2CC1C(=O)OC.[OH-].[Li+]>>COC=1C=C(C=CC1OC)S(=O)(=O)N1CC2=CC=CC=C2CC1C(=O)O
C[O:22][C:20]([CH:19]1[N:10]([S:7]([c:6]2[cH:5][cH:4][c:3]([O:2][CH3:1])[c:24]([O:25][CH3:26])[cH:23]2)(=[O:8])=[O:9])[CH2:11][c:12]2[cH:13][cH:14][cH:15][cH:16][c:17]2[CH2:18]1)=[O:21]>>[CH3:1][O:2][c:3]1[cH:4][cH:5][c:6]([S:7](=[O:8])(=[O:9])[N:10]2[CH2:11][c:12]3[cH:13][cH:14][cH:15][cH:16][c:17]3[CH2:18][CH:19]2[C:...
COC(=O)C1Cc2ccccc2CN1S(=O)(=O)c1ccc(OC)c(OC)c1
COc1ccc(S(=O)(=O)N2Cc3ccccc3CC2C(=O)O)cc1OC
null
null
C1CCOC1
Deprotection
Ester saponification (methyl deprotection)
d872e08ad5c85a4add6cd04e6e987e73fead5f79b3f30ba61a81ba5029b29894
38ae1ee78433b9acfb0390501446149c80f88f23ac2d84c60b3369bdab75cec9
O=S(=O)(c1ccccc1)N1CCc2ccccc2C1
C-[O;H0;D2;+0:1]-[C:2](=[O;D1;H0:3])-[C:4]-[#7:5]>>[#7:5]-[C:4]-[C:2](=[O;D1;H0:3])-[OH;D1;+0:1]
null
[]
null
null
8
HOUR
A solution of N-(3,4-dimethoxybenzenesulphonyl)-3-methoxycarbonyl-1,2,3,4-tetrahydro-isoquinoline(0.5 g) in THF (30 ml) was treated with a saturated aqueous solution of lithium hydroxide (3 ml) at room temperature. After stirring overnight, the solvent was removed in vacuo. The residue was diluted with water (10 ml), w...
10.6084/m9.figshare.5104873.v1
null
Ester
Carboxylic acid
null
null
c1ccccc1.c1ccc2c(c1)CC[NH]C2
Other
C1CCOC1
null
8
COC(=O)C1Cc2ccccc2CN1S(=O)(=O)c1ccc(OC)c(OC)c1>C1CCOC1>COc1ccc(S(=O)(=O)N2Cc3ccccc3CC2C(=O)O)cc1OC
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-1fbe8bec2d7a4b37b8e811f839c2b36c
C#Cc1ccccn1.COc1ccc(S(=O)(=O)N2Cc3cccc(Br)c3C2)cc1OC>>COc1ccc(S(=O)(=O)N2Cc3cccc(C#Cc4ccccn4)c3C2)cc1OC
COC=1C=C(C=CC1OC)S(=O)(=O)N1CC2=CC=CC(=C2C1)Br.C(C)N(CC)CC.C(#C)C1=NC=CC=C1.C(#C)C1=NC=CC=C1>>COC=1C=C(C=CC1OC)S(=O)(=O)N1CC2=CC=CC(=C2C1)C#CC1=NC=CC=C1
[CH:17]#[C:18][c:19]1[cH:20][cH:21][cH:22][cH:23][n:24]1.Br[c:16]1[cH:15][cH:14][cH:13][c:12]2[c:25]1[CH2:26][N:10]([S:7]([c:6]1[cH:5][cH:4][c:3]([O:2][CH3:1])[c:28]([O:29][CH3:30])[cH:27]1)(=[O:8])=[O:9])[CH2:11]2>>[CH3:1][O:2][c:3]1[cH:4][cH:5][c:6]([S:7](=[O:8])(=[O:9])[N:10]2[CH2:11][c:12]3[cH:13][cH:14][cH:15][c:1...
C#Cc1ccccn1.COc1ccc(S(=O)(=O)N2Cc3cccc(Br)c3C2)cc1OC
COc1ccc(S(=O)(=O)N2Cc3cccc(C#Cc4ccccn4)c3C2)cc1OC
null
C1=CC=C(C=C1)P(C2=CC=CC=C2)C3=CC=CC=C3.C1=CC=C(C=C1)P(C2=CC=CC=C2)C3=CC=CC=C3.Cl[Pd]Cl.[Pd]
CN(C=O)C.C(C)(=O)OCC
C-C Coupling
Sonogashira alkyne_aryl halide
f06f27dcb2a41374466bd91bd48dd25e8c6394917ee727f9b0b274433d7f9627
305eca0fd2975da49e7f69e4edfb9dc1cbce82513954bc5a73be3289e70e5f76
O=S(=O)(c1ccccc1)N1Cc2cccc(C#Cc3ccccn3)c2C1
Br-[c;H0;D3;+0:1](:[c:2]:[c:3]):[c:4](:[c:5])-[C:6]-[#7:7].[#7;a:8]:[c:9]-[C:10]#[CH;D1;+0:11]>>[#7:7]-[C:6]-[c:4](:[c:5]):[c;H0;D3;+0:1](-[C;H0;D2;+0:11]#[C:10]-[c:9]:[#7;a:8]):[c:2]:[c:3]
12.5
[{"value": 12.5, "product": "COC=1C=C(C=CC1OC)S(=O)(=O)N1CC2=CC=CC(=C2C1)C#CC1=NC=CC=C1", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
90
CELSIUS
3
DAY
2-(3,4-Dimethoxybenzenesulphonyl)-4-bromoisoindoline (0.19 g), triethylamine (0.10 ml), 2-ethynylpyridine(0.06 g) and bis (triphenylphosphine)palladium(II)chloride (10%) in anhydrous N,N-dimethylformamide(2 ml) were stirred together under an inert atmosphere and heated to 90° C. After 20 hours further 2-ethynylpyridine...
10.6084/m9.figshare.5104873.v1
null
Aromatic halide.Alkyne
Alkyne
c1ccc2c(c1)C[NH]C2
c1ccc2c(c1)C[NH]C2
c1ccccc1.c1ccc2c(c1)C[NH]C2.c1ccncc1
HBr
C1=CC=C(C=C1)P(C2=CC=CC=C2)C3=CC=CC=C3.C1=CC=C(C=C1)P(C2=CC=CC=C2)C3=CC=CC=C3.Cl[Pd]Cl.[Pd].CN(C=O)C.C(C)(=O)OCC
90
72
C#Cc1ccccn1.COc1ccc(S(=O)(=O)N2Cc3cccc(Br)c3C2)cc1OC>C1=CC=C(C=C1)P(C2=CC=CC=C2)C3=CC=CC=C3.C1=CC=C(C=C1)P(C2=CC=CC=C2)C3=CC=CC=C3.Cl[Pd]Cl.[Pd].CN(C=O)C.C(C)(=O)OCC>COc1ccc(S(=O)(=O)N2Cc3cccc(C#Cc4ccccn4)c3C2)cc1OC
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-ff129fa8213d45ca8f4648e29b01c951
CO[C@H]1C[C@@H]2CC[C@@H](C)[C@@](O)(O2)C(=O)C(=O)N2CCCC[C@H]2C(=O)O[C@H]([C@H](C)C[C@@H]2CC[C@@H](O)[C@H](OC)C2)CC(=O)[C@H](C)/C=C(\C)[C@@H](O)[C@@H](OC)C(=O)[C@H](C)C[C@H](C)/C=C/C=C/C=C/1C>>CO[C@@H]1C[C@H](C[C@@H](C)[C@@H]2CC(=O)[C@H](C)/C=C(\C)[C@@H](O)[C@@H](OC)C(=O)[C@H](C)C[C@H](C)/C=C\C=CC=C(C)C(=O)C[C@@H]3CC[C@...
C(#N)C1=C(C(=O)C(=C(C1=O)Cl)Cl)C#N.C[C@@H]1CC[C@H]2C[C@@H](/C(=C/C=C/C=C/[C@H](C[C@H](C(=O)[C@@H]([C@@H](/C(=C/[C@H](C(=O)C[C@H](OC(=O)[C@@H]3CCCCN3C(=O)C(=O)[C@@]1(O2)O)[C@H](C)C[C@@H]4CC[C@H]([C@@H](C4)OC)O)C)/C)O)OC)C)C)/C)OC.O>>C[C@@H]1CC[C@H]2CC(=O)C(=CC=C/C=C\[C@H](C[C@H](C(=O)[C@@H]([C@@H](/C(=C/[C@H](C(=O)C[C@H...
C[O:38][C@@H:37]1/[C:35]([CH3:36])=[CH:34]/[CH:33]=[CH:32]/[CH:31]=[CH:30]/[C@@H:28]([CH3:29])[CH2:27][C@@H:25]([CH3:26])[C:23](=[O:24])[C@H:20]([O:21][CH3:22])[C@H:18]([OH:19])/[C:16]([CH3:17])=[CH:15]/[C@@H:13]([CH3:14])[C:11](=[O:12])[CH2:10][C@@H:9]([C@@H:7]([CH2:6][C@H:5]2[CH2:4][C@@H:3]([O:2][CH3:1])[C@H:63]([OH:...
CO[C@H]1C[C@@H]2CC[C@@H](C)[C@@](O)(O2)C(=O)C(=O)N2CCCC[C@H]2C(=O)O[C@H]([C@H](C)C[C@@H]2CC[C@@H](O)[C@H](OC)C2)CC(=O)[C@H](C)/C=C(\C)[C@@H](O)[C@@H](OC)C(=O)[C@H](C)C[C@H](C)/C=C/C=C/C=C/1C
CO[C@@H]1C[C@H](C[C@@H](C)[C@@H]2CC(=O)[C@H](C)/C=C(\C)[C@@H](O)[C@@H](OC)C(=O)[C@H](C)C[C@H](C)/C=C\C=CC=C(C)C(=O)C[C@@H]3CC[C@@H](C)[C@@](O)(O3)C(=O)C(=O)N3CCCC[C@H]3C(=O)O2)CC[C@H]1O
null
null
ClCCl
Miscellaneous
OtherReaction
4ad29d9a9f8fa62d26ac0b34d9c9d494139463612a562b91246c4663134b934c
06ee4e636755478860a38bbf5b67d3037b3b941f1ee50aea08d8ea3a7f23e056
O=C1C=CC=C/C=C\CCCC(=O)CCC=CCC(=O)C[C@@H](CCC2CCCCC2)OC(=O)[C@@H]2CCCCN2C(=O)C(=O)C2CCC[C@@H](C1)O2
C-[O;H0;D2;+0:1]-[C@@H;D3;+0:2](-[C:3]-[C:4]-[#8:5])/[C:6](-[C;D1;H3:7])=[C:8]/[C:9]=[C:10]/[C:11]=[C:12]>>[#8:5]-[C:4]-[C:3]-[C;H0;D3;+0:2](=[O;H0;D1;+0:1])-[C:6](-[C;D1;H3:7])=[C:8]-[C:9]=[C:10]/[C:11]=[C:12]
null
[]
null
null
45
MINUTE
To a solution of rapamycin (5 mg, 0.055 mmol) in dichloromethane (0.1 mL) was added water (0.02 mL) followed by DDQ (2.4 mg, 0.011 mmol), and the resulting dark brown suspension was stirred at room temperature for 45 min. The mixture was filtered through celite and then partitioned between dichloromethane and brine; th...
10.6084/m9.figshare.5104873.v1
null
Ether
Ketone
C1=C/C=C/CC[C@@H]2CCC[C@H](CCN3CCCC[C@H]3COCCCC/C=C/CCCCCC/C=C/1)O2
C1=C/C=C\CCCCCCC=CCCCCOC[C@@H]2CCCCN2CC[C@H]2CCC[C@@H](CCC=C1)O2
C1CCCCC1.C1=C/C=C\CCCCCCC=CCCCCOC[C@@H]2CCCCN2CC[C@H]2CCC[C@@H](CCC=C1)O2
Other
ClCCl
null
0.75
CO[C@H]1C[C@@H]2CC[C@@H](C)[C@@](O)(O2)C(=O)C(=O)N2CCCC[C@H]2C(=O)O[C@H]([C@H](C)C[C@@H]2CC[C@@H](O)[C@H](OC)C2)CC(=O)[C@H](C)/C=C(\C)[C@@H](O)[C@@H](OC)C(=O)[C@H](C)C[C@H](C)/C=C/C=C/C=C/1C>ClCCl>CO[C@@H]1C[C@H](C[C@@H](C)[C@@H]2CC(=O)[C@H](C)/C=C(\C)[C@@H](O)[C@@H](OC)C(=O)[C@H](C)C[C@H](C)/C=C\C=CC=C(C)C(=O)C[C@@H]3...
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-45b51dfa48a4401f8cc762580c573748
CCOC(=O)/N=N/C(=O)OCC.Cn1c(C=Cc2ccccc2O)cc2ccccc21>>COC(=O)[C@H](C)Oc1ccccc1C=Cc1cc2ccccc2n1C
OC1=C(C=CC=C1)C=CC=1N(C2=CC=CC=C2C1)C.C1(=CC=CC=C1)P(C1=CC=CC=C1)C1=CC=CC=C1.CCOC(=O)/N=N/C(=O)OCC.C1CCOC1>>COC(=O)[C@H](C)OC1=C(C=CC=C1)C=CC=1N(C2=CC=CC=C2C1)C
C[CH2:1][O:2][C:3](/N=N/C(=O)O[CH2:5][CH3:6])=[O:4].[OH:7][c:8]1[cH:9][cH:10][cH:11][cH:12][c:13]1[CH:14]=[CH:15][c:16]1[cH:17][c:18]2[cH:19][cH:20][cH:21][cH:22][c:23]2[n:24]1[CH3:25]>>[CH3:1][O:2][C:3](=[O:4])[C@H:5]([CH3:6])[O:7][c:8]1[cH:9][cH:10][cH:11][cH:12][c:13]1[CH:14]=[CH:15][c:16]1[cH:17][c:18]2[cH:19][cH:2...
CCOC(=O)/N=N/C(=O)OCC.Cn1c(C=Cc2ccccc2O)cc2ccccc21
COC(=O)[C@H](C)Oc1ccccc1C=Cc1cc2ccccc2n1C
null
null
[Cl-].[Na+].O
C-C Coupling
OtherReaction
0f7daa1e28b94fa56e93d642499403664434ff60aef02861826759334413479d
e12cd616c68daa01974b9e799eaff061e9c3515771499b426b7524dd69fcfada
C(=Cc1cc2ccccc2[nH]1)c1ccccc1
C-[CH2;D2;+0:1]-[#8:2]-[C;H0;D3;+0:3](=[O;D1;H0:4])/N=N/C(=O)-O-[CH2;D2;+0:5]-[C;D1;H3:6].[C:7]=[C:8]-[c:9]:[c:10](-[OH;D1;+0:11]):[c:12]>>[C:7]=[C:8]-[c:9]:[c:10](-[O;H0;D2;+0:11]-[C@@H;D3;+0:5](-[C;D1;H3:6])-[C;H0;D3;+0:3](=[O;D1;H0:4])-[#8:2]-[CH3;D1;+0:1]):[c:12]
90
[{"value": 90.0, "product": "COC(=O)[C@H](C)OC1=C(C=CC=C1)C=CC=1N(C2=CC=CC=C2C1)C", "details": "PERCENTYIELD", "is_desired": false}]
null
null
2
HOUR
To a solution of 1.50 g (6.02 mmol) of 2-[2-(2-hydroxyphenyl)vinyl]-1-methylindole, 1.89 g (7.21 mmol) of triphenylphosphine and 0.69 ml (7.22 mmol) of R-(+)-methyl lactate in 15 ml of THF was added 1.14 ml (7.24 mmol) of diethylazodicarboxylate under an ice-cooled condition, followed by stirring at room temperature fo...
10.6084/m9.figshare.5104873.v1
null
Ether.Ether.Diazene.Aromatic alcohol
Ester.Ether
null
null
c1ccccc1.c1cc2ccccc2[nH]1
HO-
[Cl-].[Na+].O
null
2
CCOC(=O)/N=N/C(=O)OCC.Cn1c(C=Cc2ccccc2O)cc2ccccc21>[Cl-].[Na+].O>COC(=O)[C@H](C)Oc1ccccc1C=Cc1cc2ccccc2n1C
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-dc610c599a6a47cbbab5dcc6ac8c553a
COC(=O)CBr.c1ccc2c(Nc3ccncc3)noc2c1>>Br.COC(=O)Cn1ccc(=Nc2noc3ccccc23)cc1
N1=CC=C(C=C1)NC1=NOC2=C1C=CC=C2.BrCC(=O)OC>>Br.COC(CN1C=CC(C=C1)=NC1=NOC2=C1C=CC=C2)=O
[Br:1][CH2:6][C:4]([O:3][CH3:2])=[O:5].[n:7]1[cH:8][cH:9][c:10]([NH:11][c:12]2[n:13][o:14][c:15]3[cH:16][cH:17][cH:18][cH:19][c:20]23)[cH:21][cH:22]1>>[BrH:1].[CH3:2][O:3][C:4](=[O:5])[CH2:6][n:7]1[cH:8][cH:9][c:10](=[N:11][c:12]2[n:13][o:14][c:15]3[cH:16][cH:17][cH:18][cH:19][c:20]23)[cH:21][cH:22]1
COC(=O)CBr.c1ccc2c(Nc3ccncc3)noc2c1
Br.COC(=O)Cn1ccc(=Nc2noc3ccccc23)cc1
null
null
C(C)#N
Heteroatom Alkylation and Arylation
OtherReaction
a05baa0d189a78d43c66bc7586e891af508d8c2523abdfecef022b9457bc51ad
350896f2b21b02a4330179c771d63e7fba34621d26da5f19b2e6779a93051bdb
c1ccc2c(N=c3cc[nH]cc3)noc2c1
[#7;a:1]1:[#8;a:2]:[c:3]:[c:4]:[c:5]:1-[NH;D2;+0:6]-[c;H0;D3;+0:7]1:[c:8]:[c:9]:[n;H0;D2;+0:10]:[c:11]:[c:12]:1.[Br;H0;D1;+0:13]-[CH2;D2;+0:14]-[C:15](=[O;D1;H0:16])-[#8:17]-[C;D1;H3:18]>>[BrH;D0;+0:13].[C;D1;H3:18]-[#8:17]-[C:15](=[O;D1;H0:16])-[CH2;D2;+0:14]-[n;H0;D3;+0:10]1:[c:9]:[c:8]:[c;H0;D3;+0:7](=[N;H0;D2;+0:6]...
70
[{"value": 70.0, "product": "Br.COC(CN1C=CC(C=C1)=NC1=NOC2=C1C=CC=C2)=O", "details": "PERCENTYIELD", "is_desired": false}]
null
null
null
null
A mixture of 3-(4-pyridinylamino)-1,2-benzisoxazole (0.9 g, 4.3 mmol) and methyl bromoacetate (0.44 mL, 1.1 eq) in acetonitrile (25 mL) was heated at reflux for one hour. The mixture was then allowed to cool to room temperature and the precipitated product was collected by filtration. The white solid was washed with di...
10.6084/m9.figshare.5104873.v1
null
Primary halide.Ester.Secondary amine
Ester
c1ccncc1
c1ccncc1
c1ccncc1.c1ccc2oncc2c1
null
C(C)#N
null
null
COC(=O)CBr.c1ccc2c(Nc3ccncc3)noc2c1>C(C)#N>Br.COC(=O)Cn1ccc(=Nc2noc3ccccc23)cc1
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-f35791fc5d9c4277b1f7f4b9129278c8
FC(F)(F)c1cccc(Nc2nccc(-c3ccnc(Cl)c3)n2)c1.NCCCO>>OCCCNc1cc(-c2ccnc(Nc3cccc(C(F)(F)F)c3)n2)ccn1
FC(C=1C=C(C=CC1)NC1=NC=CC(=N1)C1=CC(=NC=C1)Cl)(F)F.NCCCO>>FC(C=1C=C(C=CC1)NC1=NC=CC(=N1)C1=CC(=NC=C1)NCCCO)(F)F
Cl[c:6]1[cH:7][c:8](-[c:9]2[cH:10][cH:11][n:12][c:13]([NH:14][c:15]3[cH:16][cH:17][cH:18][c:19]([C:20]([F:21])([F:22])[F:23])[cH:24]3)[n:25]2)[cH:26][cH:27][n:28]1.[OH:1][CH2:2][CH2:3][CH2:4][NH2:5]>>[OH:1][CH2:2][CH2:3][CH2:4][NH:5][c:6]1[cH:7][c:8](-[c:9]2[cH:10][cH:11][n:12][c:13]([NH:14][c:15]3[cH:16][cH:17][cH:18]...
FC(F)(F)c1cccc(Nc2nccc(-c3ccnc(Cl)c3)n2)c1.NCCCO
OCCCNc1cc(-c2ccnc(Nc3cccc(C(F)(F)F)c3)n2)ccn1
null
null
null
Heteroatom Alkylation and Arylation
N-arylation (Buchwald-Hartwig/Ullmann-Goldberg)
c026a7bf7aba66b20cf21a13c528689aaaa1c05901524d62b36ca0c3b0572cef
71a04ae650defc5edd86a92f43c304e981a05f07ff76248da8d4155f3905a29d
c1ccc(Nc2nccc(-c3ccncc3)n2)cc1
Cl-[c;H0;D3;+0:1](:[#7;a:2]:[c:3]):[c:4]:[c:5].[C:6]-[C:7]-[NH2;D1;+0:8]>>[C:6]-[C:7]-[NH;D2;+0:8]-[c;H0;D3;+0:1](:[#7;a:2]:[c:3]):[c:4]:[c:5]
null
[]
null
null
null
null
50 mg (0.143 mmol) of N-(3-trifluoromethyl-phenyl)-4-(2-chloro4-pyridyl)-2-pyrimidineamine are stirred for 44 h at 100° in 1 ml of 3-amino-1-propanol. Concentration by evaporation and chromatography (methylene chloride:methanol=9:1) give N-(3-trifluoromethyl-phenyl)-4-[2-(3-hydroxy-propyl-amino)-4-pyridyl]-2-pyrimidine...
10.6084/m9.figshare.5104873.v1
null
Aromatic halide.Primary amine
Secondary amine
c1ccncc1
c1ccncc1
c1ccncc1.c1cncnc1.c1ccccc1
HCl
null
null
null
FC(F)(F)c1cccc(Nc2nccc(-c3ccnc(Cl)c3)n2)c1.NCCCO>>OCCCNc1cc(-c2ccnc(Nc3cccc(C(F)(F)F)c3)n2)ccn1
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-160c9a75cc8c48d189fa78e2f7af0bda
N#Cc1ccnc(Cl)c1>>CC(=O)c1ccnc(Cl)c1
ClC1=NC=CC(=C1)C#N.C[Mg]Cl.Cl.C(C)OCC>>C(C)(=O)C1=CC(=NC=C1)Cl
N#[C:2][c:4]1[cH:5][cH:6][n:7][c:8]([Cl:9])[cH:10]1>>[CH3:1][C:2](=[O:3])[c:4]1[cH:5][cH:6][n:7][c:8]([Cl:9])[cH:10]1
N#Cc1ccnc(Cl)c1
CC(=O)c1ccnc(Cl)c1
null
null
null
Miscellaneous
OtherReaction
54622de249eb9a5622e28710a02d261b08e09c3ee957106ef84a0e4751ccb30f
957d5e0aaa82a4f5b73d699040cb2acd7f615417c9e400cbb7a63fa4c133449a
c1ccncc1
N#[C;H0;D2;+0:1]-[c:2]1:[c:3]:[c:4]:[#7;a:5]:[c:6]:[c:7]:1>>[C;D1;H3:8]-[C;H0;D3;+0:1](=[O;D1;H0:9])-[c:2]1:[c:3]:[c:4]:[#7;a:5]:[c:6]:[c:7]:1
null
[]
null
null
40
HOUR
24.61 g (177.62 mmol) of 2-chloro-4-cyano-pyridine are placed in 1.25 litres of diethyl ether under nitrogen, and 120 ml (22% in tetrahydrofuran, 353 mmol) of methyl-magnesium chloride are added. The red suspension is stirred for 40 h at RT, poured onto 1.25 litres of ice/water and 250 ml of 6N HCl and stirred for 14 h...
10.6084/m9.figshare.5104873.v1
null
Nitrile
Ketone
null
null
c1ccncc1
null
null
null
40
N#Cc1ccnc(Cl)c1>>CC(=O)c1ccnc(Cl)c1
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-6eee014e31484dc4a5b6680a1edc957c
CC(=O)c1cc[n+]([O-])cc1.O=P(Cl)(Cl)Cl>>CC(=O)c1ccnc(Cl)c1
C(C)(=O)C1=CC=[N+](C=C1)[O-].P(=O)(Cl)(Cl)Cl.[OH-].[Na+]>>C(C)(=O)C1=CC(=NC=C1)Cl
[O-][n+:7]1[cH:6][cH:5][c:4]([C:2]([CH3:1])=[O:3])[cH:10][cH:8]1.O=P(Cl)(Cl)[Cl:9]>>[CH3:1][C:2](=[O:3])[c:4]1[cH:5][cH:6][n:7][c:8]([Cl:9])[cH:10]1
CC(=O)c1cc[n+]([O-])cc1.O=P(Cl)(Cl)Cl
CC(=O)c1ccnc(Cl)c1
null
null
C1(=CC=CC=C1)C
Miscellaneous
OtherReaction
a7e4b874c7a18ec6b4305e16cc93c9103d77bfb4ce559ead41b2d45f56dcb90f
a48150e9dff88baab32dd83daf5ab089c597626e3c583c33a5868d8e1353c1ea
c1ccncc1
Cl-P(-Cl)(=O)-[Cl;H0;D1;+0:1].[C;D1;H3:2]-[C:3](=[O;D1;H0:4])-[c:5]1:[c:6]:[cH;D2;+0:7]:[n+;H0;D3:8](-[O-]):[c:9]:[c:10]:1>>[C;D1;H3:2]-[C:3](=[O;D1;H0:4])-[c:5]1:[c:6]:[c;H0;D3;+0:7](-[Cl;H0;D1;+0:1]):[n;H0;D2;+0:8]:[c:9]:[c:10]:1
null
[]
null
null
null
null
5.0 g (36.5 mmol) of 4-acetyl-pyridine N-oxide and 6.64 ml (73 mmol) of phosphorus oxychloride are stirred in 50 ml of toluene for 2 h at 100°. The reaction mixture is stirred at 50° into 500 ml of 10N sodium hydroxide solution, extracted with ethyl acetate and treated with Tonsil (Fluka; bentonite--colloidal aqueous a...
10.6084/m9.figshare.5104873.v1
null
null
Aromatic halide
C1=CC=[NH+]C=C1
c1ccncc1
c1ccncc1
HCl
C1(=CC=CC=C1)C
null
null
CC(=O)c1cc[n+]([O-])cc1.O=P(Cl)(Cl)Cl>C1(=CC=CC=C1)C>CC(=O)c1ccnc(Cl)c1
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-c9d27f69137047ca85c77482a3084a76
CC(=O)c1ccncc1>>CC(=O)c1cc[n+]([O-])cc1
C(C)(=O)C1=CC=NC=C1.ClC1=CC(=CC=C1)C(=O)OO>>C(C)(=O)C1=CC=[N+](C=C1)[O-]
[CH3:1][C:2](=[O:3])[c:4]1[cH:5][cH:6][n:7][cH:9][cH:10]1>>[CH3:1][C:2](=[O:3])[c:4]1[cH:5][cH:6][n+:7]([O-:8])[cH:9][cH:10]1
CC(=O)c1ccncc1
CC(=O)c1cc[n+]([O-])cc1
null
null
C(Cl)Cl
Functional Group Interconversion
OtherReaction
54415aed4bb61f76efee9ed140374352608210a9fed7c372975c12eb7023cea2
f1bbf9aa3c82f5e49be9f6d53533b6bb152f359232b6d32090c168949766aa71
c1cc[nH+]cc1
[c:1]:[c:2]:[n;H0;D2;+0:3]:[c:4]:[c:5]>>[O;-;D1;H0:6]-[n+;H0;D3:3](:[c:4]:[c:5]):[c:2]:[c:1]
null
[]
null
null
null
null
The 4-acetyl-pyridine N-oxide used is prepared in the following manner: 11.0 ml (100 mmol) of 4-acetyl-pyridine and 31.3 g (100 mmol) of 55% m-chloro-perbenzoic acid are boiled under RF for 16 h in 200 ml of methylene chloride. Precipitation with 200 ml of diethyl ether gives 4-acetyl-pyridine N-oxide; m.p. 132°-133°. ...
10.6084/m9.figshare.5104873.v1
null
null
null
c1ccncc1
C1=CC=[NH+]C=C1
C1=CC=[NH+]C=C1
null
C(Cl)Cl
null
null
CC(=O)c1ccncc1>C(Cl)Cl>CC(=O)c1cc[n+]([O-])cc1
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-17f4a6bed6804e1a87ae17bb1cfb5ad3
CC(=O)c1ccnc(Cl)c1.CCOC(OCC)N(C)C>>CN(C)C=CC(=O)c1ccnc(Cl)c1
C(C)(=O)C1=CC(=NC=C1)Cl.C(C)OC(N(C)C)OCC>>CN(C=CC(=O)C1=CC(=NC=C1)Cl)C
[CH3:5][C:6](=[O:7])[c:8]1[cH:9][cH:10][n:11][c:12]([Cl:13])[cH:14]1.CCO[CH:4](OCC)[N:2]([CH3:1])[CH3:3]>>[CH3:1][N:2]([CH3:3])[CH:4]=[CH:5][C:6](=[O:7])[c:8]1[cH:9][cH:10][n:11][c:12]([Cl:13])[cH:14]1
CC(=O)c1ccnc(Cl)c1.CCOC(OCC)N(C)C
CN(C)C=CC(=O)c1ccnc(Cl)c1
null
null
null
C-C Coupling
OtherReaction
57f48fac7254684faf48980af66a0d538cb8dee0ab05f049059285d4840b8be4
49ae3600e90e05c7cda8811d9438748b91211f407b3eab7b1bcb51e798f4d85a
c1ccncc1
C-C-O-[CH;D3;+0:1](-O-C-C)-[#7:2](-[C;D1;H3:3])-[C;D1;H3:4].[CH3;D1;+0:5]-[C:6](=[O;D1;H0:7])-[c:8]>>[C;D1;H3:3]-[#7:2](-[C;D1;H3:4])-[CH;D2;+0:1]=[CH;D2;+0:5]-[C:6](=[O;D1;H0:7])-[c:8]
null
[]
null
null
null
null
16.2 g (104.2 mmol) of 4-acetyl-2-chloro-pyridine are stirred at 110° with 116 ml of dimethylformamide diethylacetal for 1 h. Cooling to 0°, filtering and drying at 60° under HV give 3-dimethylamino-1-(2-chloro-4-pyridyl)-2-propen-1-one; 1H-NMR (dimethyl sulfoxide): 2.98 (3H,s), 3.2 (3H,s), 5.9 (1H,d), 7.8 (3H,m), 8.5 ...
10.6084/m9.figshare.5104873.v1
null
Ketone.Ether.Ether
Enamine
null
null
c1ccncc1
HO-
null
null
null
CC(=O)c1ccnc(Cl)c1.CCOC(OCC)N(C)C>>CN(C)C=CC(=O)c1ccnc(Cl)c1
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-dd9f79aff70f4e008da6da583aa08a55
N#CN.Nc1cccc(C(F)(F)F)c1>>N=C(N)Nc1cccc(C(F)(F)F)c1
N#CN.FC(C=1C=C(N)C=CC1)(F)F.[N+](=O)(O)[O-]>>[N+](=O)(O)[O-].FC(C=1C=C(C=CC1)NC(=N)N)(F)F
[N:1]#[C:2][NH2:3].[NH2:4][c:5]1[cH:6][cH:7][cH:8][c:9]([C:10]([F:11])([F:12])[F:13])[cH:14]1>>[NH:1]=[C:2]([NH2:3])[NH:4][c:5]1[cH:6][cH:7][cH:8][c:9]([C:10]([F:11])([F:12])[F:13])[cH:14]1
N#CN.Nc1cccc(C(F)(F)F)c1
N=C(N)Nc1cccc(C(F)(F)F)c1
null
null
C(C)O
Heteroatom Alkylation and Arylation
OtherReaction
a0cbddf5d7d81fe92104447f1edef14329807abeadc66f8268b3c04bddc38ea2
9b168a0be416143e92b99e2902110a4569d3f9f31721e83b72aa42867628c64d
c1ccccc1
[N;D1;H2:1]-[C;H0;D2;+0:2]#[N;H0;D1;+0:3].[NH2;D1;+0:4]-[c:5](:[c:6]):[c:7]>>[N;D1;H2:1]-[C;H0;D3;+0:2](=[NH;D1;+0:3])-[NH;D2;+0:4]-[c:5](:[c:6]):[c:7]
null
[]
null
null
null
null
6.3 g (150 mmol) of cyanamide (50% in water) are added to a suspension of 16.1 g (100 mmol) of 3-trifluoromethyl-aniline in 35 ml of ethanol. 7.0 ml of nitric acid (65%, 0.1 mol) are then added to the brown solution and the reaction mixture is heated for 20 h under RF. It is then cooled to 0° and filtered, and the mate...
10.6084/m9.figshare.5104873.v1
null
Cyanamide.Primary amine
Secondary amine
null
null
c1ccccc1
null
C(C)O
null
null
N#CN.Nc1cccc(C(F)(F)F)c1>C(C)O>N=C(N)Nc1cccc(C(F)(F)F)c1
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-80c466f42a2f4da1817b28cc4a125e1c
CN(C)C=CC(=O)c1ccnc(Cl)c1.N=C(N)Nc1cccc(C(F)(F)F)c1>>FC(F)(F)c1cccc(Nc2nccc(-c3ccnc(Cl)c3)n2)c1
CN(C=CC(=O)C1=CC(=NC=C1)Cl)C.[N+](=O)(O)[O-].FC(C=1C=C(C=CC1)NC(=N)N)(F)F.[OH-].[Na+]>>FC(C=1C=C(C=CC1)NC1=NC=CC(=N1)C1=CC(=NC=C1)Cl)(F)F
CN(C)[CH:13]=[CH:14][C:15](=O)[c:16]1[cH:17][cH:18][n:19][c:20]([Cl:21])[cH:22]1.[F:1][C:2]([F:3])([F:4])[c:5]1[cH:6][cH:7][cH:8][c:9]([NH:10][C:11](=[NH:12])[NH2:23])[cH:24]1>>[F:1][C:2]([F:3])([F:4])[c:5]1[cH:6][cH:7][cH:8][c:9]([NH:10][c:11]2[n:12][cH:13][cH:14][c:15](-[c:16]3[cH:17][cH:18][n:19][c:20]([Cl:21])[cH:2...
CN(C)C=CC(=O)c1ccnc(Cl)c1.N=C(N)Nc1cccc(C(F)(F)F)c1
FC(F)(F)c1cccc(Nc2nccc(-c3ccnc(Cl)c3)n2)c1
null
null
CC(C)O
Aromatic Heterocycle Formation
OtherReaction
78274536798da2b99a51ce47d0994df99b4d5455af910301779a9ae5938608b5
11da551d0a7bf93f6d300d0e461ec1d4a2060497908163f95323146dc93cd499
c1ccc(Nc2nccc(-c3ccncc3)n2)cc1
C-N(-C)-[CH;D2;+0:1]=[CH;D2;+0:2]-[C;H0;D3;+0:3](=O)-[c;H0;D3;+0:4]1:[c:5]:[c:6]:[#7;a:7]:[c:8](-[Cl;D1;H0:9]):[c:10]:1.[NH2;D1;+0:11]-[C;H0;D3;+0:12](=[NH;D1;+0:13])-[#7:14]-[c:15]>>[Cl;D1;H0:9]-[c:8]1:[#7;a:7]:[c:6]:[c:5]:[c;H0;D3;+0:4](-[c;H0;D3;+0:3]2:[cH;D2;+0:2]:[cH;D2;+0:1]:[n;H0;D2;+0:13]:[c;H0;D3;+0:12](-[#7:1...
null
[]
null
null
18
HOUR
150 mg (0.71 mmol) of 3-dimethylamino-1-(2-chloro-4-pyridyl)-2-propen-1-one are suspended in 1.5 ml of 2-propanol. 190 mg (0.712 mmol) of 3-trifluoromethylphenyl-guanidine nitrate and 31 mg (0.783 mmol) of sodium hydroxide are added and the reaction mixture is stirred for 18 h under RF. It is then cooled to RT and filt...
10.6084/m9.figshare.5104873.v1
null
Enamine.Ketone.Primary amine
null
null
c1cncnc1
c1ccccc1.c1cncnc1.c1ccncc1
HO-
CC(C)O
null
18
CN(C)C=CC(=O)c1ccnc(Cl)c1.N=C(N)Nc1cccc(C(F)(F)F)c1>CC(C)O>FC(F)(F)c1cccc(Nc2nccc(-c3ccnc(Cl)c3)n2)c1
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-d187a558f2cb415e8f8f2e8cc58499db
O=P(Cl)(Cl)Cl.[O-][n+]1ccc(-c2ccnc(Nc3cccc(Cl)c3)n2)cc1>>Clc1cccc(Nc2nccc(-c3ccnc(Cl)c3)n2)c1
ClC=1C=C(C=CC1)NC1=NC=CC(=N1)C1=CC=[N+](C=C1)[O-].P(=O)(Cl)(Cl)Cl.[OH-].[Na+]>>ClC=1C=C(C=CC1)NC1=NC=CC(=N1)C1=CC(=NC=C1)Cl
O=P(Cl)(Cl)[Cl:18].[O-][n+:16]1[cH:15][cH:14][c:13](-[c:12]2[cH:11][cH:10][n:9][c:8]([NH:7][c:6]3[cH:5][cH:4][cH:3][c:2]([Cl:1])[cH:21]3)[n:20]2)[cH:19][cH:17]1>>[Cl:1][c:2]1[cH:3][cH:4][cH:5][c:6]([NH:7][c:8]2[n:9][cH:10][cH:11][c:12](-[c:13]3[cH:14][cH:15][n:16][c:17]([Cl:18])[cH:19]3)[n:20]2)[cH:21]1
O=P(Cl)(Cl)Cl.[O-][n+]1ccc(-c2ccnc(Nc3cccc(Cl)c3)n2)cc1
Clc1cccc(Nc2nccc(-c3ccnc(Cl)c3)n2)c1
null
null
null
Miscellaneous
OtherReaction
a7e4b874c7a18ec6b4305e16cc93c9103d77bfb4ce559ead41b2d45f56dcb90f
a48150e9dff88baab32dd83daf5ab089c597626e3c583c33a5868d8e1353c1ea
c1ccc(Nc2nccc(-c3ccncc3)n2)cc1
Cl-P(-Cl)(=O)-[Cl;H0;D1;+0:1].[O-]-[n+;H0;D3:2]1:[c:3]:[c:4]:[c:5]:[c:6]:[cH;D2;+0:7]:1>>[Cl;H0;D1;+0:1]-[c;H0;D3;+0:7]1:[c:6]:[c:5]:[c:4]:[c:3]:[n;H0;D2;+0:2]:1
null
[]
null
null
null
null
10.0 g (32 mmol) of N-(3-chloro-phenyl)-4-(N-oxido-4-pyridyl)-2-pyrimidineamine are stirred for 24 h in 100 ml of phosphorus oxychloride at 110°. The reaction mixture is stirred at 50° into 2N sodium hydroxide solution and extracted with tetrahydrofuran. Concentration and crystallisation (tetrahydrofuran/ethanol) of th...
10.6084/m9.figshare.5104873.v1
null
null
Aromatic halide
C1=CC=[NH+]C=C1
c1ccncc1
c1ccccc1.c1cncnc1.c1ccncc1
HCl
null
null
null
O=P(Cl)(Cl)Cl.[O-][n+]1ccc(-c2ccnc(Nc3cccc(Cl)c3)n2)cc1>>Clc1cccc(Nc2nccc(-c3ccnc(Cl)c3)n2)c1
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-a39fc3b67bbd45ff88d29b84e47f577f
Clc1cccc(Nc2nccc(-c3ccncc3)n2)c1>>[O-][n+]1ccc(-c2ccnc(Nc3cccc(Cl)c3)n2)cc1
ClC=1C=C(C=CC1)NC1=NC=CC(=N1)C1=CC=NC=C1.ClC1=CC(=CC=C1)C(=O)OO>>ClC=1C=C(C=CC1)NC1=NC=CC(=N1)C1=CC=[N+](C=C1)[O-]
[n:2]1[cH:3][cH:4][c:5](-[c:6]2[cH:7][cH:8][n:9][c:10]([NH:11][c:12]3[cH:13][cH:14][cH:15][c:16]([Cl:17])[cH:18]3)[n:19]2)[cH:20][cH:21]1>>[O-:1][n+:2]1[cH:3][cH:4][c:5](-[c:6]2[cH:7][cH:8][n:9][c:10]([NH:11][c:12]3[cH:13][cH:14][cH:15][c:16]([Cl:17])[cH:18]3)[n:19]2)[cH:20][cH:21]1
Clc1cccc(Nc2nccc(-c3ccncc3)n2)c1
[O-][n+]1ccc(-c2ccnc(Nc3cccc(Cl)c3)n2)cc1
null
null
C(Cl)Cl
Functional Group Interconversion
OtherReaction
54415aed4bb61f76efee9ed140374352608210a9fed7c372975c12eb7023cea2
f1bbf9aa3c82f5e49be9f6d53533b6bb152f359232b6d32090c168949766aa71
c1ccc(Nc2nccc(-c3cc[nH+]cc3)n2)cc1
[c:1]:[c:2]:[n;H0;D2;+0:3]:[c:4]:[c:5]>>[O;-;D1;H0:6]-[n+;H0;D3:3](:[c:2]:[c:1]):[c:4]:[c:5]
null
[]
null
null
null
null
10 g (35.4 mmol) of N-(3-chloro-phenyl)-4-(4-pyridyl)-2-pyrimidineamine and 11.1 g (35.4 mmol) of m-chloroperbenzoic acid are stirred for 5 h at RT in 500 ml of methylene chloride. Concentration and crystallisation (acetic acid) of the residue give N-(3-chloro-phenyl)-4-(N-oxido4-pyridyl)-2-pyrimidineamine; m.p. 274°-2...
10.6084/m9.figshare.5104873.v1
null
null
null
c1ccncc1
C1=CC=[NH+]C=C1
C1=CC=[NH+]C=C1.c1cncnc1.c1ccccc1
null
C(Cl)Cl
null
null
Clc1cccc(Nc2nccc(-c3ccncc3)n2)c1>C(Cl)Cl>[O-][n+]1ccc(-c2ccnc(Nc3cccc(Cl)c3)n2)cc1
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-69f537074c164129a11f9fadfb9978d6
Clc1cccc(Nc2nccc(-c3ccnc(Cl)c3)n2)c1.NCCN>>NCCNc1cc(-c2ccnc(Nc3cccc(Cl)c3)n2)ccn1
ClC=1C=C(C=CC1)NC1=NC=CC(=N1)C1=CC(=NC=C1)Cl.C(CN)N>>ClC=1C=C(C=CC1)NC1=NC=CC(=N1)C1=CC(=NC=C1)NCCN
Cl[c:5]1[cH:6][c:7](-[c:8]2[cH:9][cH:10][n:11][c:12]([NH:13][c:14]3[cH:15][cH:16][cH:17][c:18]([Cl:19])[cH:20]3)[n:21]2)[cH:22][cH:23][n:24]1.[NH2:1][CH2:2][CH2:3][NH2:4]>>[NH2:1][CH2:2][CH2:3][NH:4][c:5]1[cH:6][c:7](-[c:8]2[cH:9][cH:10][n:11][c:12]([NH:13][c:14]3[cH:15][cH:16][cH:17][c:18]([Cl:19])[cH:20]3)[n:21]2)[cH...
Clc1cccc(Nc2nccc(-c3ccnc(Cl)c3)n2)c1.NCCN
NCCNc1cc(-c2ccnc(Nc3cccc(Cl)c3)n2)ccn1
null
null
null
Heteroatom Alkylation and Arylation
N-arylation (Buchwald-Hartwig/Ullmann-Goldberg)
c026a7bf7aba66b20cf21a13c528689aaaa1c05901524d62b36ca0c3b0572cef
71a04ae650defc5edd86a92f43c304e981a05f07ff76248da8d4155f3905a29d
c1ccc(Nc2nccc(-c3ccncc3)n2)cc1
Cl-[c;H0;D3;+0:1](:[#7;a:2]:[c:3]):[c:4]:[c:5].[C:6]-[C:7]-[NH2;D1;+0:8]>>[C:6]-[C:7]-[NH;D2;+0:8]-[c;H0;D3;+0:1](:[#7;a:2]:[c:3]):[c:4]:[c:5]
null
[]
null
null
null
null
20 mg (0.063 mmol) of N-(3-chloro-phenyl)-4-(2-chloro-4-pyridyl)-2-pyrimidineamine are stirred for 26 h at 110° with 1 ml of ethylenediamine. Concentration and chromatography (methylene chloride:methanol:conc. ammonia solution=80:20: 1) give N-(3-chloro-phenyl)-4-[2-(2-amino-ethyl-amino)-4-pyridyl]-2-pyrimidineamine; R...
10.6084/m9.figshare.5104873.v1
null
Aromatic halide.Primary amine
Secondary amine
c1ccncc1
c1ccncc1
c1ccncc1.c1cncnc1.c1ccccc1
HCl
null
null
null
Clc1cccc(Nc2nccc(-c3ccnc(Cl)c3)n2)c1.NCCN>>NCCNc1cc(-c2ccnc(Nc3cccc(Cl)c3)n2)ccn1
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-b2c40033208b4111b3cb9a725ae2825c
NCCN.O=C(O)c1cc(-c2ccnc(Nc3cccc(Cl)c3)n2)ccn1>>NCCNC(=O)c1cc(-c2ccnc(Nc3cccc(Cl)c3)n2)ccn1
ClC=1C=C(C=CC1)NC1=NC=CC(=N1)C1=CC(=NC=C1)C(=O)O.Cl.C(C)N=C=NCCCN(C)C.ON1C(CCC1=O)=O.C(CN)N>>Cl.ClC=1C=C(C=CC1)NC1=NC=CC(=N1)C1=CC(=NC=C1)C(=O)NCCN
[NH2:2][CH2:3][CH2:4][NH2:5].O[C:6](=[O:7])[c:8]1[cH:9][c:10](-[c:11]2[cH:12][cH:13][n:14][c:15]([NH:16][c:17]3[cH:18][cH:19][cH:20][c:21]([Cl:22])[cH:23]3)[n:24]2)[cH:25][cH:26][n:27]1>>[NH2:2][CH2:3][CH2:4][NH:5][C:6](=[O:7])[c:8]1[cH:9][c:10](-[c:11]2[cH:12][cH:13][n:14][c:15]([NH:16][c:17]3[cH:18][cH:19][cH:20][c:2...
NCCN.O=C(O)c1cc(-c2ccnc(Nc3cccc(Cl)c3)n2)ccn1
NCCNC(=O)c1cc(-c2ccnc(Nc3cccc(Cl)c3)n2)ccn1
null
null
CN(C=O)C.CN(C)C=O.C(C)(=O)OCC
Acylation
Carboxylic acid with primary amine to amide
37494d655fc476b499cf056f6435518833ae87795aab58744c3c61cc6e2d35e8
1acc31e468ee9ff2d6601bea2d2eb10c464508bb7150073479303b3753dd92b4
c1ccc(Nc2nccc(-c3ccncc3)n2)cc1
O-[C;H0;D3;+0:1](=[O;D1;H0:2])-[c:3](:[c:4]):[#7;a:5]:[c:6].[C:7]-[C:8]-[NH2;D1;+0:9]>>[C:7]-[C:8]-[NH;D2;+0:9]-[C;H0;D3;+0:1](=[O;D1;H0:2])-[c:3](:[c:4]):[#7;a:5]:[c:6]
null
[]
null
null
2.5
HOUR
80 mg (0.24 mmol) of N-[3-chloro-phenyl]-4-(2-carboxy-4-pyridyl)-2-pyrimidineamine, 70.8 mg (0.36 mmol) of N-ethyl-N'-(3-dimethylaminopropyl)-carbodiimide hydrochloride and 42 mg (0.36 mmol) of N-hydroxysuccinimide are dissolved in 3 ml of dimethylformamide and stirred for 2.5 h at RT. The reaction mixture is then adde...
10.6084/m9.figshare.5104873.v1
null
Carboxylic acid.Primary amine
Secondary amide
null
null
c1ccncc1.c1cncnc1.c1ccccc1
HO-
CN(C=O)C.CN(C)C=O.C(C)(=O)OCC
null
2.5
NCCN.O=C(O)c1cc(-c2ccnc(Nc3cccc(Cl)c3)n2)ccn1>CN(C=O)C.CN(C)C=O.C(C)(=O)OCC>NCCNC(=O)c1cc(-c2ccnc(Nc3cccc(Cl)c3)n2)ccn1
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-4d75cb7565874f338140d42a8ca396c2
CO.O=C(O)c1cccc(Nc2nccc(-c3ccnc(NCCCO)c3)n2)c1>>COC(=O)c1cccc(Nc2nccc(-c3ccnc(NCCCO)c3)n2)c1
C(=O)(O)C=1C=C(C=CC1)NC1=NC=CC(=N1)C1=CC(=NC=C1)NCCCO.S(O)(O)(=O)=O.CO>>COC(=O)C=1C=C(C=CC1)NC1=NC=CC(=N1)C1=CC(=NC=C1)NCCCO
[CH3:1][OH:2].O[C:3](=[O:4])[c:5]1[cH:6][cH:7][cH:8][c:9]([NH:10][c:11]2[n:12][cH:13][cH:14][c:15](-[c:16]3[cH:17][cH:18][n:19][c:20]([NH:21][CH2:22][CH2:23][CH2:24][OH:25])[cH:26]3)[n:27]2)[cH:28]1>>[CH3:1][O:2][C:3](=[O:4])[c:5]1[cH:6][cH:7][cH:8][c:9]([NH:10][c:11]2[n:12][cH:13][cH:14][c:15](-[c:16]3[cH:17][cH:18][n...
CO.O=C(O)c1cccc(Nc2nccc(-c3ccnc(NCCCO)c3)n2)c1
COC(=O)c1cccc(Nc2nccc(-c3ccnc(NCCCO)c3)n2)c1
null
null
null
Protection
Esterification of Carboxylic Acids
9cecdbd189c6f9c3648521d17154d013842a5498de4e76e65efb1d842973340b
af0b8064f2e82ebe66c4c29d2391785ac1b993104265ccdc4d67ca79e36fa3c8
c1ccc(Nc2nccc(-c3ccncc3)n2)cc1
O-[C;H0;D3;+0:1](=[O;D1;H0:2])-[c:3](:[c:4]):[c:5].[C;D1;H3:6]-[OH;D1;+0:7]>>[C;D1;H3:6]-[O;H0;D2;+0:7]-[C;H0;D3;+0:1](=[O;D1;H0:2])-[c:3](:[c:4]):[c:5]
null
[]
null
null
null
null
2.0 g (5.4 mmol) of N-[3-carboxy-phenyl]-4-(2-(3-hydroxy-propyl-amino)-4-pyridyl)-2-pyrimidineamine and 0.28 ml (5.4 mmol) of conc. sulfuric acid are boiled under RF in 150 ml of methanol for 24 h. After cooling to RT, the reaction mixture is concentrated to half the volume, diluted with 100 ml of ethyl acetate and ext...
10.6084/m9.figshare.5104873.v1
null
Carboxylic acid.Methanol
Ester
null
null
c1ccccc1.c1cncnc1.c1ccncc1
HO-
null
null
null
CO.O=C(O)c1cccc(Nc2nccc(-c3ccnc(NCCCO)c3)n2)c1>>COC(=O)c1cccc(Nc2nccc(-c3ccnc(NCCCO)c3)n2)c1
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-e95dea12efcf46abb4f2455c2c2c6569
COC(=O)c1cccc(Nc2nccc(-c3ccnc(NCCCO)c3)n2)c1.NCCCN>>NCCCNC(=O)c1cccc(Nc2nccc(-c3ccnc(NCCCO)c3)n2)c1
COC(=O)C=1C=C(C=CC1)NC1=NC=CC(=N1)C1=CC(=NC=C1)NCCCO.NCCCN>>NCCCNC(=O)C=1C=C(C=CC1)NC1=NC=CC(=N1)C1=CC(=NC=C1)NCCCO
CO[C:6](=[O:7])[c:8]1[cH:9][cH:10][cH:11][c:12]([NH:13][c:14]2[n:15][cH:16][cH:17][c:18](-[c:19]3[cH:20][cH:21][n:22][c:23]([NH:24][CH2:25][CH2:26][CH2:27][OH:28])[cH:29]3)[n:30]2)[cH:31]1.[NH2:1][CH2:2][CH2:3][CH2:4][NH2:5]>>[NH2:1][CH2:2][CH2:3][CH2:4][NH:5][C:6](=[O:7])[c:8]1[cH:9][cH:10][cH:11][c:12]([NH:13][c:14]2...
COC(=O)c1cccc(Nc2nccc(-c3ccnc(NCCCO)c3)n2)c1.NCCCN
NCCCNC(=O)c1cccc(Nc2nccc(-c3ccnc(NCCCO)c3)n2)c1
null
null
C(C)(=O)OCC
Acylation
Aminolysis of esters
04c54ce22aa9bc0cea0de3d900446bcab51cf02bebeb606fa788a47dcd0e37ff
4335147c9ad02004b7c12428d7eac0b2e7e0e2017adc471d01c387239de8017d
c1ccc(Nc2nccc(-c3ccncc3)n2)cc1
C-O-[C;H0;D3;+0:1](=[O;D1;H0:2])-[c:3](:[c:4]):[c:5].[C:6]-[C:7]-[NH2;D1;+0:8]>>[C:6]-[C:7]-[NH;D2;+0:8]-[C;H0;D3;+0:1](=[O;D1;H0:2])-[c:3](:[c:4]):[c:5]
null
[]
null
null
null
null
100 mg (0.26 mmol) of N-[3-methoxycarbonyl-phenyl]-4-[2-(3-hydroxy-propyl-amino)-4-pyridyl]-2-pyrimidineamine and 0.5 ml of 1,3-diamino-propane are stirred for 24 h at 90° and then diluted with 20 ml of ethyl acetate and extracted with 2×10 ml of sodium chloride solution. The organic phase is dried, concentrated and cr...
10.6084/m9.figshare.5104873.v1
null
Ester.Primary amine
Secondary amide
null
null
c1ccccc1.c1cncnc1.c1ccncc1
HO-
C(C)(=O)OCC
null
null
COC(=O)c1cccc(Nc2nccc(-c3ccnc(NCCCO)c3)n2)c1.NCCCN>C(C)(=O)OCC>NCCCNC(=O)c1cccc(Nc2nccc(-c3ccnc(NCCCO)c3)n2)c1
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-8b8f64beacb447798a17fed01f8b02fc
ClCCl.Clc1cccc(Nc2nccc(-c3ccnc(N4CCNCC4)c3)n2)c1>>C1CNCCN1.Clc1cccc(Nc2nccc(-c3ccnc(Cl)c3)n2)c1
C(Cl)Cl.ClC=1C=C(C=CC1)NC1=NC=CC(=N1)C1=CC(=NC=C1)N1CCNCC1>>ClC=1C=C(C=CC1)NC1=NC=CC(=N1)C1=CC(=NC=C1)Cl.N1CCNCC1
ClC[Cl:24].[CH2:1]1[CH2:2][NH:3][CH2:4][CH2:5][N:6]1[c:23]1[n:22][cH:21][cH:20][c:19](-[c:18]2[cH:17][cH:16][n:15][c:14]([NH:13][c:12]3[cH:11][cH:10][cH:9][c:8]([Cl:7])[cH:27]3)[n:26]2)[cH:25]1>>[CH2:1]1[CH2:2][NH:3][CH2:4][CH2:5][NH:6]1.[Cl:7][c:8]1[cH:9][cH:10][cH:11][c:12]([NH:13][c:14]2[n:15][cH:16][cH:17][c:18](-[...
ClCCl.Clc1cccc(Nc2nccc(-c3ccnc(N4CCNCC4)c3)n2)c1
C1CNCCN1.Clc1cccc(Nc2nccc(-c3ccnc(Cl)c3)n2)c1
null
null
CO
Functional Group Interconversion
OtherReaction
accb083ee8fd7641a677dca692d5f564b73dc543c66b542e44a7304924f0d3b4
b03e6f5e6e8d8a1bd25b5055e831596b4284cf0e900bac020435f2faffd27024
C1CNCCN1.c1ccc(Nc2nccc(-c3ccncc3)n2)cc1
Cl-C-[Cl;H0;D1;+0:1].[c:2]:[c:3]:[c;H0;D3;+0:4](-[N;H0;D3;+0:5]1-[C:6]-[C:7]-[#7:8]-[C:9]-[C:10]-1):[#7;a:11]:[c:12]>>[#7:8]1-[C:7]-[C:6]-[NH;D2;+0:5]-[C:10]-[C:9]-1.[Cl;H0;D1;+0:1]-[c;H0;D3;+0:4](:[#7;a:11]:[c:12]):[c:3]:[c:2]
null
[]
null
null
null
null
Analogously to Example 1, there is obtained from 100 mg (0.31 mmol) of N-[3-chloro-phenyl]-4-(2-chloro-4-pyridyl)-2-pyrimidineamine and 500 mg (5.63 mmol) of piperazine, from the melt after chromatography (methylene chloride:methanol=95:5), N-[3-chloro-phenyl]-4-[2-(1-piperazinyl)-4-pyridyl]-2-pyrimidineamine; Conditio...
10.6084/m9.figshare.5104873.v1
null
Primary halide.Primary halide.Tertiary amine
Aromatic halide.Secondary amine
C1C[NH]CCN1.c1ccncc1
C1CNCCN1.c1ccncc1
C1CNCCN1.c1ccccc1.c1cncnc1.c1ccncc1
HCl
CO
null
null
ClCCl.Clc1cccc(Nc2nccc(-c3ccnc(N4CCNCC4)c3)n2)c1>CO>C1CNCCN1.Clc1cccc(Nc2nccc(-c3ccnc(Cl)c3)n2)c1
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-6188ee3573314f55babc64ae624ba785
CC(=O)OC(C)=O.N[C@@H](CC(=O)OCc1ccccc1)C(=O)O>>CC(=O)NC(CC(=O)OCc1ccccc1)C(C)=O
C1=CC=C(C=C1)COC(=O)C[C@@H](C(=O)O)N.C(C)N(CC)CC.[OH-].[K+].C(C)(=O)OC(C)=O>>C(C)(=O)NC(CC(=O)OCC1=CC=CC=C1)C(C)=O
O=C(O[C:2]([CH3:1])=[O:3])[CH3:18].O[C:17]([C@@H:5]([NH2:4])[CH2:6][C:7](=[O:8])[O:9][CH2:10][c:11]1[cH:12][cH:13][cH:14][cH:15][cH:16]1)=[O:19]>>[CH3:1][C:2](=[O:3])[NH:4][CH:5]([CH2:6][C:7](=[O:8])[O:9][CH2:10][c:11]1[cH:12][cH:13][cH:14][cH:15][cH:16]1)[C:17]([CH3:18])=[O:19]
CC(=O)OC(C)=O.N[C@@H](CC(=O)OCc1ccccc1)C(=O)O
CC(=O)NC(CC(=O)OCc1ccccc1)C(C)=O
null
CN(C1=CC=NC=C1)C
O
C-C Coupling
OtherReaction
b802459ff5eb68424777810c52e09960d8b0c0aeb6f75b59978e8d896c3dd42e
a9679e805e0145be1fc9e7c455e6b352598a150489d618752043f7ed3d22039c
c1ccccc1
O-[C;H0;D3;+0:1](=[O;D1;H0:2])-[C@@H;D3;+0:3](-[NH2;D1;+0:4])-[C:5]-[C:6](=[O;D1;H0:7])-[#8:8]-[C:9].O=C(-[CH3;D1;+0:10])-O-[C;H0;D3;+0:11](-[C;D1;H3:12])=[O;D1;H0:13]>>[C:9]-[#8:8]-[C:6](=[O;D1;H0:7])-[C:5]-[CH;D3;+0:3](-[NH;D2;+0:4]-[C;H0;D3;+0:11](-[C;D1;H3:12])=[O;D1;H0:13])-[C;H0;D3;+0:1](-[CH3;D1;+0:10])=[O;D1;H0...
82.8
[{"value": 82.8, "product": "C(C)(=O)NC(CC(=O)OCC1=CC=CC=C1)C(C)=O", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
null
null
β-Benzyl L-aspartate (400 g, 1.79 mol) was suspended in triethylamine (748 ml, 5.37 mol) and acetic anhydride (676 ml, 7.16 mol) was dropwise added at 0° C. with stirring. After stirring for 30 minutes, 4-dimethylaminopyridine (20.0 g, 0.16 mol) was portionwise added under ice-cooling. The mixture was stirred overnight...
10.6084/m9.figshare.5104873.v1
null
Anhydride.Carboxylic acid.Primary amine
Ketone.Secondary amide
null
null
c1ccccc1
HO-
CN(C1=CC=NC=C1)C.O
null
null
CC(=O)OC(C)=O.N[C@@H](CC(=O)OCc1ccccc1)C(=O)O>CN(C1=CC=NC=C1)C.O>CC(=O)NC(CC(=O)OCc1ccccc1)C(C)=O
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-0b86b7517ec945ca8eeab9a8c1598395
NN.O=C(O)CCC(=O)c1ccc(Cl)cc1>>O=C1CCC(c2ccc(Cl)cc2)=NN1
ClC1=CC=C(C(=O)CCC(=O)O)C=C1.O.NN>>ClC1=CC=C(C=C1)C=1CCC(NN1)=O
[NH2:13][NH2:14].O=[C:5]([CH2:4][CH2:3][C:2](O)=[O:1])[c:6]1[cH:7][cH:8][c:9]([Cl:10])[cH:11][cH:12]1>>[O:1]=[C:2]1[CH2:3][CH2:4][C:5]([c:6]2[cH:7][cH:8][c:9]([Cl:10])[cH:11][cH:12]2)=[N:13][NH:14]1
NN.O=C(O)CCC(=O)c1ccc(Cl)cc1
O=C1CCC(c2ccc(Cl)cc2)=NN1
null
null
C(C)O
Acylation
OtherReaction
16e715242dd5e92f711d46176c552652cef6c6f4fed9bc9a09a311d5b0b86cea
30de68c4dde17a0553a43eee47b1b865b8390bb08557512a59e6e71e0ed0ad51
O=C1CCC(c2ccccc2)=NN1
O-[C;H0;D3;+0:1](=[O;D1;H0:2])-[C:3]-[C:4]-[C;H0;D3;+0:5](=O)-[c:6](:[c:7]):[c:8].[NH2;D1;+0:9]-[NH2;D1;+0:10]>>[O;D1;H0:2]=[C;H0;D3;+0:1]1-[C:3]-[C:4]-[C;H0;D3;+0:5](-[c:6](:[c:7]):[c:8])=[N;H0;D2;+0:9]-[NH;D2;+0:10]-1
81.5
[{"value": 80.0, "product": "ClC1=CC=C(C=C1)C=1CCC(NN1)=O", "details": "PERCENTYIELD", "is_desired": false}, {"value": 81.5, "product": "ClC1=CC=C(C=C1)C=1CCC(NN1)=O", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
null
null
To a solution of 3-(4-chlorobenzoyl)propionic acid (20 g) in absolute ethanol (200 ml) was added 5 g of hydrazine monohydrate. A thick solid was formed which dissolved after heating. The resulting solution was refluxed for 3 h, cooled and the solid formed filtered and dried to yield 16 g (80%) of 6-(4-chlorophenyl)-4,5...
10.6084/m9.figshare.5104873.v1
null
Hydrazine.Carboxylic acid.Ketone
Hydrazone amide
null
C1=NNCCC1
C1=NNCCC1.c1ccccc1
HO-
C(C)O
null
null
NN.O=C(O)CCC(=O)c1ccc(Cl)cc1>C(C)O>O=C1CCC(c2ccc(Cl)cc2)=NN1
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-676eee09ab9444cfbed62b0de2f1342d
COC(=O)CCC(=O)OC.COC(=O)c1cccc(Cl)c1>>O=C(O)CCC(=O)c1cccc(Cl)c1
C(CCC(=O)OC)(=O)OC.[Na].C(C)O.ClC=1C=C(C(=O)OC)C=CC1.C(CCC(=O)OC)(=O)OC>>ClC=1C=C(C(=O)CCC(=O)O)C=CC1
COC(=O)[CH2:5][CH2:4][C:2](=[O:1])[O:3]C.CO[C:6](=[O:7])[c:8]1[cH:9][cH:10][cH:11][c:12]([Cl:13])[cH:14]1>>[O:1]=[C:2]([OH:3])[CH2:4][CH2:5][C:6](=[O:7])[c:8]1[cH:9][cH:10][cH:11][c:12]([Cl:13])[cH:14]1
COC(=O)CCC(=O)OC.COC(=O)c1cccc(Cl)c1
O=C(O)CCC(=O)c1cccc(Cl)c1
null
null
CCOCC
C-C Coupling
OtherReaction
6d482de2a0c1fffe47581cf2d6dc0eefca79628574252eec326be9292f335afe
1f69704fe402a3eb0e91a243a59f68f972592be61b4c787368515903d4c85726
c1ccccc1
C-O-C(=O)-[CH2;D2;+0:1]-[C:2]-[C:3](=[O;D1;H0:4])-[O;H0;D2;+0:5]-C.C-O-[C;H0;D3;+0:6](=[O;D1;H0:7])-[c:8](:[c:9]):[c:10]>>[O;D1;H0:4]=[C:3](-[OH;D1;+0:5])-[C:2]-[CH2;D2;+0:1]-[C;H0;D3;+0:6](=[O;D1;H0:7])-[c:8](:[c:9]):[c:10]
null
[]
null
null
null
null
Sodium (11 g, spheres) was added to 200 ml ethanol with stirring. When the gas evolution ceased, methyl 3-chlorobenzoate (10 g, 0.057 mole) and dimethyl succinate (9.0 g, 0.615 mole) were added rapidly and the mixture was stirred for 5 minutes at room temperature. The mixture was slowly concentrated on a rotary evapora...
10.6084/m9.figshare.5104873.v1
null
Ester.Ester.Ester
Carboxylic acid.Ketone
null
null
c1ccccc1
HO-
CCOCC
null
null
COC(=O)CCC(=O)OC.COC(=O)c1cccc(Cl)c1>CCOCC>O=C(O)CCC(=O)c1cccc(Cl)c1
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-4c442c2d85c24feebbe8e0084018a86b
CC(C(=O)O)C(=O)c1ccc(Cl)cc1.O=[N+]([O-])O>>CC(C(=O)O)C(=O)c1ccc(Cl)c([N+](=O)[O-])c1
ClC1=CC=C(C(=O)C(C(=O)O)C)C=C1.[N+](=O)(O)[O-]>>ClC1=C(C=C(C(=O)C(C(=O)O)C)C=C1)[N+](=O)[O-]
[CH3:1][CH:2]([C:3](=[O:4])[OH:5])[C:6](=[O:7])[c:8]1[cH:9][cH:10][c:11]([Cl:12])[cH:13][cH:17]1.O[N+:14](=[O:15])[O-:16]>>[CH3:1][CH:2]([C:3](=[O:4])[OH:5])[C:6](=[O:7])[c:8]1[cH:9][cH:10][c:11]([Cl:12])[c:13]([N+:14](=[O:15])[O-:16])[cH:17]1
CC(C(=O)O)C(=O)c1ccc(Cl)cc1.O=[N+]([O-])O
CC(C(=O)O)C(=O)c1ccc(Cl)c([N+](=O)[O-])c1
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]-[C:10]=[O;D1;H0:11]>>[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]-[C:10]=[O;D1;H0:11]
null
[]
0
CELSIUS
30
MINUTE
To fuming nitric acid (150 ml) was added p-chlorobenzoylpropionic acid (20.0 g), slowly portionwise at 0° C. After the addition was completed the resulting mixture was stirred at 0° C. for 30 minutes and the resulting white solid was suction filtered and washed with water until the pH of the washing liquids was neutral...
10.6084/m9.figshare.5104873.v1
null
Nitrate
Nitro group
c1ccccc1
c1ccccc1
c1ccccc1
HO-
null
0
0.5
CC(C(=O)O)C(=O)c1ccc(Cl)cc1.O=[N+]([O-])O>>CC(C(=O)O)C(=O)c1ccc(Cl)c([N+](=O)[O-])c1
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-64ad41c7f6d34083816470ce8e3c45fd
C1=COCCC1.OCC#CCO>>OCC#CCOC1CCCCO1
C(C#CCO)O.O1CCCC=C1>>O1C(CCCC1)OCC#CCO
[CH:7]1=[CH:8][CH2:9][CH2:10][CH2:11][O:12]1.[OH:1][CH2:2][C:3]#[C:4][CH2:5][OH:6]>>[OH:1][CH2:2][C:3]#[C:4][CH2:5][O:6][CH:7]1[CH2:8][CH2:9][CH2:10][CH2:11][O:12]1
C1=COCCC1.OCC#CCO
OCC#CCOC1CCCCO1
null
C1(=CC=C(C=C1)S(=O)(=O)O)C
CCOCC
Heteroatom Alkylation and Arylation
oxa-Michael addition
abdcab389770d0a73be3b825aa1d56cee234da38dbdf3510fe8104d481e7cf3f
c6a3efa2acb508a32cdf9fcedfcd9635cce0ecdcf12c094b743aa576ea01fd9a
C1CCOCC1
[#8:1]1-[C:2]-[C:3]-[C:4]-[CH;D2;+0:5]=[CH;D2;+0:6]-1.[C:7]-[C:8]#[C:9]-[C:10]-[OH;D1;+0:11]>>[C:7]-[C:8]#[C:9]-[C:10]-[O;H0;D2;+0:11]-[CH;D3;+0:6]1-[#8:1]-[C:2]-[C:3]-[C:4]-[CH2;D2;+0:5]-1
68.8
[{"value": 68.8, "product": "O1C(CCCC1)OCC#CCO", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
null
null
To a mixture of 5.0 g of 2-butyne-1,4-diol and 10 milligrams of p-toluenesulfonic acid and 150 ml of dry ether there was added dropwise with stirring at room temperature 4.9 g of 3,4-dihydro-2H-pyran. After stirring overnight at ambient temperature the ether was evaporated and the residue was poured into 200 ml of wate...
10.6084/m9.figshare.5104873.v1
null
Ether.Primary alcohol
Ether.Ether
C1=COCCC1
C1CCOCC1
C1CCOCC1
null
C1(=CC=C(C=C1)S(=O)(=O)O)C.CCOCC
null
null
C1=COCCC1.OCC#CCO>C1(=CC=C(C=C1)S(=O)(=O)O)C.CCOCC>OCC#CCOC1CCCCO1
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-b7fb0104fad94bc0b378012d50f6c0c8
C#CC1CCCCC1.C=O>>OCC#CC1CCCCC1
C1(CCCCC1)C#C.C=O.C=O>>C1(CCCCC1)C#CCO
[CH:3]#[C:4][CH:5]1[CH2:6][CH2:7][CH2:8][CH2:9][CH2:10]1.[O:1]=[CH2:2]>>[OH:1][CH2:2][C:3]#[C:4][CH:5]1[CH2:6][CH2:7][CH2:8][CH2:9][CH2:10]1
C#CC1CCCCC1.C=O
OCC#CC1CCCCC1
null
null
CCOCC
C-C Coupling
OtherReaction
b068d8bba9f864ba971dd324292d9b3526f0235b4ab7e3a9ce6aa76a39c4a1e7
22ebec2cc94dd24863aea8793d450cfe0691e1036be204d1a4c79c16effe90a4
C1CCCCC1
[CH2;D1;+0:1]=[O;H0;D1;+0:2].[C:3]-[C:4]#[CH;D1;+0:5]>>[C:3]-[C:4]#[C;H0;D2;+0:5]-[CH2;D2;+0:1]-[OH;D1;+0:2]
null
[]
null
null
null
null
To a solution of ethyl magesium bromide (prepared from 2.5 g of magnesium turning and 11.3 g of bromoethane) in ether was added dropwise a solution of 10.2 g of cyclohexylacetylene in ether and the reaction mixture was refluxed for 2 hours. The reaction mixture was cooled to ambient temperature and anhydrous formaldehy...
10.6084/m9.figshare.5104873.v1
null
Formaldehyde.Alkyne
Primary alcohol.Alkyne
null
null
C1CCCCC1
null
CCOCC
null
null
C#CC1CCCCC1.C=O>CCOCC>OCC#CC1CCCCC1
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-836c8b6682c54c8ab49aa69cf992817b
O=C1CCC(c2ccc(Cl)cc2)=NN1>>O=c1ccc(-c2ccc(Cl)cc2)n[nH]1
ClC1=CC=C(C=C1)C=1CCC(NN1)=O.C(C)(=O)O.BrBr>>ClC1=CC=C(C=C1)C=1C=CC(NN1)=O
[O:1]=[C:2]1[CH2:3][CH2:4][C:5]([c:6]2[cH:7][cH:8][c:9]([Cl:10])[cH:11][cH:12]2)=[N:13][NH:14]1>>[O:1]=[c:2]1[cH:3][cH:4][c:5](-[c:6]2[cH:7][cH:8][c:9]([Cl:10])[cH:11][cH:12]2)[n:13][nH:14]1
O=C1CCC(c2ccc(Cl)cc2)=NN1
O=c1ccc(-c2ccc(Cl)cc2)n[nH]1
null
null
O
Aromatic Heterocycle Formation
OtherReaction
73c80fbcc9dd7a9125aaf1059d9d4eab31b342d21fc860abf5e65fd78456864b
78b0616e5760c6d4dadfc1fac5c58c0254d0dc7b1bf102fea4bc1349928b0776
O=c1ccc(-c2ccccc2)n[nH]1
[O;D1;H0:1]=[C;H0;D3;+0:2]1-[CH2;D2;+0:3]-[CH2;D2;+0:4]-[C;H0;D3;+0:5](-[c;H0;D3;+0:6](:[c:7]:[c:8]):[c:9]:[c:10])=[N;H0;D2;+0:11]-[NH;D2;+0:12]-1>>[O;D1;H0:1]=[c;H0;D3;+0:2]1:[cH;D2;+0:3]:[cH;D2;+0:4]:[c;H0;D3;+0:5](-[c;H0;D3;+0:6](:[c:7]:[c:8]):[c:9]:[c:10]):[n;H0;D2;+0:11]:[nH;D2;+0:12]:1
93.1
[{"value": 89.0, "product": "ClC1=CC=C(C=C1)C=1C=CC(NN1)=O", "details": "PERCENTYIELD", "is_desired": false}, {"value": 93.1, "product": "ClC1=CC=C(C=C1)C=1C=CC(NN1)=O", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
null
null
To a solution of 6-(4-chlorophenyl)-4,5-dihydropyridazinone (11.75 g) and glacial acetic acid (100 ml) was added dropwise 3 ml of bromine and the mixture was heated at 60°-70° C. for 3 h. The resulting mixture was cooled and slowly poured into 400 ml of cold water. The resulting white solid was filtered and dried to yi...
10.6084/m9.figshare.5104873.v1
null
Hydrazone amide
null
C1=NNCCC1
c1cccnn1
c1cccnn1.c1ccccc1
null
O
null
null
O=C1CCC(c2ccc(Cl)cc2)=NN1>O>O=c1ccc(-c2ccc(Cl)cc2)n[nH]1
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-a6ba3063855543d494bab226d66b41f6
FC1(F)CC(Cl)(Cl)C1(F)Cl>>FC1(F)C=C(Cl)C1(F)Cl
ClC1(C(C(C1)(F)F)(F)Cl)Cl.O.Cl>>ClC1(C(C=C1Cl)(F)F)F
Cl[C:5]1([Cl:6])[CH2:4][C:2]([F:1])([F:3])[C:7]1([F:8])[Cl:9]>>[F:1][C:2]1([F:3])[CH:4]=[C:5]([Cl:6])[C:7]1([F:8])[Cl:9]
FC1(F)CC(Cl)(Cl)C1(F)Cl
FC1(F)C=C(Cl)C1(F)Cl
null
null
CCOCC.C(C)N(CC)CC
Functional Group Interconversion
OtherReaction
0ca523bc88d44f4371960ac2ff9ed0bbb8882337b7061f7fba5b4787f1e02481
986b135105e7920109b424799136a4a8281fb4a0f49253ce1bf5d4426ed78637
C1=CCC1
Cl-[C;H0;D4;+0:1]1(-[Cl;D1;H0:2])-[CH2;D2;+0:3]-[C:4](-[F;D1;H0:5])(-[F;D1;H0:6])-[C:7]-1(-[Cl;D1;H0:8])-[F;D1;H0:9]>>[Cl;D1;H0:2]-[C;H0;D3;+0:1]1=[CH;D2;+0:3]-[C:4](-[F;D1;H0:5])(-[F;D1;H0:6])-[C:7]-1(-[Cl;D1;H0:8])-[F;D1;H0:9]
79
[{"value": 79.0, "product": "ClC1(C(C=C1Cl)(F)F)F", "details": "PERCENTYIELD", "is_desired": false}, {"value": 78.2, "product": "ClC1(C(C=C1Cl)(F)F)F", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
8
HOUR
To a solution of 1,1,2 trichloro-2,3,3-trifluorocyclobutane (55.5 g) in 100 ml of anhydrous ether, triethylamine (40 ml) was added dropwise over 30 min at room temperature, and the mixture was stirred overnight at ambient temperature. The mixture was then stirred with 120 ml H2O and 7.5 ml of concentrated HCl. The ethe...
10.6084/m9.figshare.5104873.v1
null
Tertiary halide.Tertiary halide
Alkenyl halide
C1CCC1
C1=CCC1
C1=CCC1
HCl
CCOCC.C(C)N(CC)CC
null
8
FC1(F)CC(Cl)(Cl)C1(F)Cl>CCOCC.C(C)N(CC)CC>FC1(F)C=C(Cl)C1(F)Cl
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-b94b41efbd25422b9fc00f014be629d5
O=C(O)C(F)(F)C(F)(Cl)C(=O)O>>O=C(O)C(F)C(F)(F)C(=O)O
ClC(C(C(=O)O)(F)F)(C(=O)O)F>>FC(C(=O)O)(C(C(=O)O)F)F
Cl[C:6]([C:4]([C:2](=[O:1])[OH:3])([F:5])[F:7])([F:8])[C:9](=[O:10])[OH:11]>>[O:1]=[C:2]([OH:3])[CH:4]([F:5])[C:6]([F:7])([F:8])[C:9](=[O:10])[OH:11]
O=C(O)C(F)(F)C(F)(Cl)C(=O)O
O=C(O)C(F)C(F)(F)C(=O)O
null
[Zn]
O1CCOCC1
Functional Group Addition
Dehalogenation
7f145230bfb0115349e969b2f2fa1359cfafe8c166e52b50a867192005e1f5bc
d6722b0df465660a9eeeaca5a8f5b3dbb2d1ebccb44917f2eca97a85bf850d06
null
Cl-[C;H0;D4;+0:1](-[F;D1;H0:2])(-[C:3](=[O;D1;H0:4])-[O;D1;H1:5])-[C;H0;D4;+0:6](-[F;D1;H0:7])(-[F;H0;D1;+0:8])-[C:9](=[O;D1;H0:10])-[O;D1;H1:11]>>[F;D1;H0:7]-[CH;D3;+0:6](-[C:9](=[O;D1;H0:10])-[O;D1;H1:11])-[C;H0;D4;+0:1](-[F;D1;H0:2])(-[F;H0;D1;+0:8])-[C:3](=[O;D1;H0:4])-[O;D1;H1:5]
40.7
[{"value": 32.0, "product": "FC(C(=O)O)(C(C(=O)O)F)F", "details": "PERCENTYIELD", "is_desired": false}, {"value": 40.7, "product": "FC(C(=O)O)(C(C(=O)O)F)F", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
10
HOUR
To a stirring solution of the chlorotrifluorosuccinic acid (part b) (24.5 g) in 200 ml dioxane was added portionwise zinc metal (85 g) and the mixture was stirred at ambient temperature for 10 hours to yield a viscous liquid which was decanted from the unreacted zinc. Most of the dioxane was evaporated in vacuo. The re...
10.6084/m9.figshare.5104873.v1
null
Tertiary halide.Tertiary halide.Tertiary halide.Tertiary halide
Tertiary halide.Tertiary halide.Secondary halide
null
null
null
Other
[Zn].O1CCOCC1
null
10
O=C(O)C(F)(F)C(F)(Cl)C(=O)O>[Zn].O1CCOCC1>O=C(O)C(F)C(F)(F)C(=O)O
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-09da337c3a844b5cb26234c0ea51edee
NN.O=C(O)CCCC(=O)c1ccccc1>>O=c1cccc(-c2ccccc2)nn1
C(C1=CC=CC=C1)(=O)CCCC(=O)O.NN.O>>C1(=CC=CC=C1)C1=CC=CC(N=N1)=O
[NH2:13][NH2:14].O=[C:6]([CH2:5][CH2:4][CH2:3][C:2](O)=[O:1])[c:7]1[cH:8][cH:9][cH:10][cH:11][cH:12]1>>[O:1]=[c:2]1[cH:3][cH:4][cH:5][c:6](-[c:7]2[cH:8][cH:9][cH:10][cH:11][cH:12]2)[n:13][n:14]1
NN.O=C(O)CCCC(=O)c1ccccc1
O=c1cccc(-c2ccccc2)nn1
null
null
C1(=CC=CC=C1)C.CCOCC
Aromatic Heterocycle Formation
OtherReaction
a31553d36b14882561a6dcdd04ef456bc0e14ea189c472490f94f02ebbe3ca3f
eadf9e657b4bde18ed656e299092aac7dd81eee1face1030775c3edd6ccba31c
O=c1cccc(-c2ccccc2)nn1
O-[C;H0;D3;+0:1](=[O;D1;H0:2])-[CH2;D2;+0:3]-[CH2;D2;+0:4]-[CH2;D2;+0:5]-[C;H0;D3;+0:6](=O)-[c;H0;D3;+0:7](:[c:8]:[c:9]):[c:10]:[c:11].[NH2;D1;+0:12]-[NH2;D1;+0:13]>>[O;D1;H0:2]=[c;H0;D3;+0:1]1:[cH;D2;+0:3]:[cH;D2;+0:4]:[cH;D2;+0:5]:[c;H0;D3;+0:6](-[c;H0;D3;+0:7](:[c:8]:[c:9]):[c:10]:[c:11]):[n;H0;D2;+0:12]:[n;H0;D2;+0...
39
[{"value": 39.0, "product": "C1(=CC=CC=C1)C1=CC=CC(N=N1)=O", "details": "PERCENTYIELD", "is_desired": false}]
null
null
null
null
To a mixture of 10 g (0.052 mole) of 4-benzoylbutyric acid in 300 ml of toluene, hydrazine was added in one portion and the reaction was heated to reflux until all water had ceased to azeotrope. The reaction mixture was cooled and the toluene was stripped off in vacuo. The residue was dissolved in 200 ml Et2O and washe...
10.6084/m9.figshare.5104873.v1
null
Hydrazine.Carboxylic acid.Ketone
null
null
c1cccc[nH]n1
c1cccc[nH]n1.c1ccccc1
HO-
C1(=CC=CC=C1)C.CCOCC
null
null
NN.O=C(O)CCCC(=O)c1ccccc1>C1(=CC=CC=C1)C.CCOCC>O=c1cccc(-c2ccccc2)nn1
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-3cf41a524c8b40e093b3d619340e8c02
COC(=O)OC.O=C1CCc2cc(Cl)ccc21>>COC(=O)C1Cc2cc(Cl)ccc2C1=O
COC(OC)=O.[H-].[Na+].ClC=1C=C2CCC(C2=CC1)=O.[H][H]>>C(=O)(OC)C1C(C2=CC=C(C=C2C1)Cl)=O
CO[C:3]([O:2][CH3:1])=[O:4].[CH2:5]1[CH2:6][c:7]2[cH:8][c:9]([Cl:10])[cH:11][cH:12][c:13]2[C:14]1=[O:15]>>[CH3:1][O:2][C:3](=[O:4])[CH:5]1[CH2:6][c:7]2[cH:8][c:9]([Cl:10])[cH:11][cH:12][c:13]2[C:14]1=[O:15]
COC(=O)OC.O=C1CCc2cc(Cl)ccc21
COC(=O)C1Cc2cc(Cl)ccc2C1=O
null
null
C(OC)COC
C-C Coupling
OtherReaction
c2c31337dfb867d8c28bc65df0ad4496f817a712a58e176523b47d7fdb6e4f91
d76b6fc9d01d8258e5777a3b2326a8d78a9d9a55717b27736ba55600205f4ed0
O=C1CCc2ccccc21
C-O-[C;H0;D3;+0:1](=[O;D1;H0:2])-[#8:3]-[C;D1;H3:4].[O;D1;H0:5]=[C:6]1-[CH2;D2;+0:7]-[C:8]-[c:9]:[c:10]-1>>[C;D1;H3:4]-[#8:3]-[C;H0;D3;+0:1](=[O;D1;H0:2])-[CH;D3;+0:7]1-[C:8]-[c:9]:[c:10]-[C:6]-1=[O;D1;H0:5]
45
[{"value": 45.0, "product": "C(=O)(OC)C1C(C2=CC=C(C=C2C1)Cl)=O", "details": "PERCENTYIELD", "is_desired": false}, {"value": 44.5, "product": "C(=O)(OC)C1C(C2=CC=C(C=C2C1)Cl)=O", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
60
CELSIUS
null
null
To a mixture of sodium hydride (2.4 g, 60% in mineral oil, 0.06. mole) and 50 ml dry dimethoxyethane, 5-chloroindanone (50 g, 0.03 mole) in 50 ml dimethoxyethane was added dropwise at room temperature. The mixture was stirred at room temperature until hydrogen evolution ceased. Then dimethylcarbonate (27 g, 0.3 mole) w...
10.6084/m9.figshare.5104873.v1
null
Carbonic Ester.Ketone
Ketone.Ester
c1ccc2c(c1)CCC2
c1ccc2c(c1)CCC2
c1ccc2c(c1)CCC2
HO-
C(OC)COC
60
null
COC(=O)OC.O=C1CCc2cc(Cl)ccc21>C(OC)COC>COC(=O)C1Cc2cc(Cl)ccc2C1=O
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-351246f0dd44448ebbd806606156bbea
CN(C)C=O.O=C(O)Cc1ccc(Cl)cc1>>CN(C)C=C(C=O)c1ccc(Cl)cc1
C([O-])([O-])=O.[K+].[K+].P(=O)(Cl)(Cl)Cl.CN(C)C=O.ClC1=CC=C(C=C1)CC(=O)O>>ClC1=CC=C(C=C1)C(C=O)=CN(C)C
O=[CH:4][N:2]([CH3:1])[CH3:3].O=[C:6]([CH2:5][c:8]1[cH:9][cH:10][c:11]([Cl:12])[cH:13][cH:14]1)[OH:7]>>[CH3:1][N:2]([CH3:3])[CH:4]=[C:5]([CH:6]=[O:7])[c:8]1[cH:9][cH:10][c:11]([Cl:12])[cH:13][cH:14]1
CN(C)C=O.O=C(O)Cc1ccc(Cl)cc1
CN(C)C=C(C=O)c1ccc(Cl)cc1
null
null
C1(=CC=CC=C1)C
Acylation
OtherReaction
cbf378fe57a2b8d8304e623fb5ce9ee6fb9f6e90d9c6f965226d56b103180e6d
a9c635686380f13b6b5c45d80d4aef36b30fdab0aef140b81f04c277f7ba737d
c1ccccc1
O=[C;H0;D3;+0:1](-[OH;D1;+0:2])-[CH2;D2;+0:3]-[c:4](:[c:5]):[c:6].O=[CH;D2;+0:7]-[#7:8](-[C;D1;H3:9])-[C;D1;H3:10]>>[C;D1;H3:9]-[#7:8](-[C;D1;H3:10])-[CH;D2;+0:7]=[C;H0;D3;+0:3](-[CH;D2;+0:1]=[O;H0;D1;+0:2])-[c:4](:[c:5]):[c:6]
null
[]
null
null
8
HOUR
Phosphorus oxychloride (92 g) was added dropwise to stirred DMF (78 ml) between 10°-15° C. To the resulting slurry was added 4-chlorophenylacetic acid (34.12 g). The resulting mixture was stirred at room temperature for one half hour and then heated to 70°-80° C. during 5.5 hours, during which time the mixture became e...
10.6084/m9.figshare.5104873.v1
null
Carboxylic acid.Tertiary amide
Enamine.Aldehyde
null
null
c1ccccc1
HO-
C1(=CC=CC=C1)C
null
8
CN(C)C=O.O=C(O)Cc1ccc(Cl)cc1>C1(=CC=CC=C1)C>CN(C)C=C(C=O)c1ccc(Cl)cc1
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-0e60e058e5c041cbbf3f3bd73811d422
CN(C)C=C(C=O)c1ccc(Cl)cc1.N#CCC(N)=O>>N#Cc1cc(-c2ccc(Cl)cc2)c[nH]c1=O
C(C)(=O)O.ClC1=CC=C(C=C1)C(C=O)=CN(C)C.C[O-].[Na+].C(#N)CC(=O)N>>C(#N)C=1C(NC=C(C1)C1=CC=C(C=C1)Cl)=O
CN(C)[CH:13]=[C:5]([CH:4]=O)[c:6]1[cH:7][cH:8][c:9]([Cl:10])[cH:11][cH:12]1.[N:1]#[C:2][CH2:3][C:15]([NH2:14])=[O:16]>>[N:1]#[C:2][c:3]1[cH:4][c:5](-[c:6]2[cH:7][cH:8][c:9]([Cl:10])[cH:11][cH:12]2)[cH:13][nH:14][c:15]1=[O:16]
CN(C)C=C(C=O)c1ccc(Cl)cc1.N#CCC(N)=O
N#Cc1cc(-c2ccc(Cl)cc2)c[nH]c1=O
null
null
CO.O
Aromatic Heterocycle Formation
OtherReaction
4fb69599b2ad512416349de44ee025f314a8ccdb2c8ad729cdf94ea75cf3109a
46cf335065eccd013987994a3f086665eb273ac87eb3153099a47e61dd329581
O=c1ccc(-c2ccccc2)c[nH]1
C-N(-C)-[CH;D2;+0:1]=[C;H0;D3;+0:2](-[CH;D2;+0:3]=O)-[c;H0;D3;+0:4](:[c:5]:[c:6]):[c:7]:[c:8].[N;D1;H0:9]#[C:10]-[CH2;D2;+0:11]-[C;H0;D3;+0:12](-[NH2;D1;+0:13])=[O;D1;H0:14]>>[N;D1;H0:9]#[C:10]-[c;H0;D3;+0:11]1:[cH;D2;+0:3]:[c;H0;D3;+0:2](-[c;H0;D3;+0:4](:[c:5]:[c:6]):[c:7]:[c:8]):[cH;D2;+0:1]:[nH;D2;+0:13]:[c;H0;D3;+0...
null
[]
null
null
null
null
To solution of sodium methoxide (7.52 g) in methanol (130 ml) was added cyanoacetamide (5.84 g) followed by 2-(4-chlorophenyl)-3-dimethylaminopropenal and the resulting suspension was refluxed overnight. During this time a yellow solid was formed. The mixture was cooled to room temperature and glacial acetic acid (50 m...
10.6084/m9.figshare.5104873.v1
null
Enamine.Aldehyde.Primary amide
null
null
c1cnccc1
c1cnccc1.c1ccccc1
HO-
CO.O
null
null
CN(C)C=C(C=O)c1ccc(Cl)cc1.N#CCC(N)=O>CO.O>N#Cc1cc(-c2ccc(Cl)cc2)c[nH]c1=O
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-354b2e3cf6af4b84a2f7d3ebed5eb64d
N#Cc1cc(-c2ccc(Cl)cc2)c[nH]c1=O>>O=c1ccc(-c2ccc(Cl)cc2)c[nH]1
C(#N)C=1C(NC=C(C1)C1=CC=C(C=C1)Cl)=O>>ClC1=CC=C(C=C1)C=1C=CC(NC1)=O
N#C[c:3]1[c:2](=[O:1])[nH:14][cH:13][c:5](-[c:6]2[cH:7][cH:8][c:9]([Cl:10])[cH:11][cH:12]2)[cH:4]1>>[O:1]=[c:2]1[cH:3][cH:4][c:5](-[c:6]2[cH:7][cH:8][c:9]([Cl:10])[cH:11][cH:12]2)[cH:13][nH:14]1
N#Cc1cc(-c2ccc(Cl)cc2)c[nH]c1=O
O=c1ccc(-c2ccc(Cl)cc2)c[nH]1
null
null
OP(=O)(O)O
Miscellaneous
OtherReaction
145adc421652def73603eb299eace1e2e3a197522b719b6949c0145a4308d11b
4f08c5adfb6d80fba1093598fc51ce38f180c76537f67052d397b642cb6f3b89
O=c1ccc(-c2ccccc2)c[nH]1
N#C-[c;H0;D3;+0:1]1:[c:2]:[c:3]:[c:4]:[#7;a:5]:[c:6]:1=[O;D1;H0:7]>>[O;D1;H0:7]=[c:6]1:[#7;a:5]:[c:4]:[c:3]:[c:2]:[cH;D2;+0:1]:1
75.6
[{"value": 75.6, "product": "ClC1=CC=C(C=C1)C=1C=CC(NC1)=O", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
null
null
A mixture of 3-cyano-5-(4-chlorophenyl)-2-pyridinone (4.6 g) and 85% H3PO4 (60 ml) was heated at reflux for 16 hours. The resulting mixture was cooled to room temperature, poured into ice/water and filtered yielding 3.1 g of 5-(4-chlorophenyl)-2-pyridinone as a yellow solid. Conditions: See reaction.notes.procedure_det...
10.6084/m9.figshare.5104873.v1
null
Nitrile
null
c1cnccc1
c1cccnc1
c1cccnc1.c1ccccc1
Other
OP(=O)(O)O
null
null
N#Cc1cc(-c2ccc(Cl)cc2)c[nH]c1=O>OP(=O)(O)O>O=c1ccc(-c2ccc(Cl)cc2)c[nH]1
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-abf8a35446cd49678e6b7fb0a5cfdc74
CCC#CCBr.CCCCCC.O=c1cccc[nH]1.[Cl-]>>CCC#CCn1cc(-c2ccc(Cl)cc2)ccc1=O
[Cl-].[NH4+].[H-].[Na+].N1C(C=CC=C1)=O.CCCCCC.C(C)(=O)OCC.BrCC#CCC>>ClC1=CC=C(C=C1)C=1C=CC(N(C1)CC#CCC)=O
Br[CH2:5][C:4]#[C:3][CH2:2][CH3:1].[CH2:9]([CH3:10])[CH2:15][CH2:14][CH2:12][CH3:11].[nH:6]1[cH:7][cH:8][cH:16][cH:17][c:18]1=[O:19].[Cl-:13]>>[CH3:1][CH2:2][C:3]#[C:4][CH2:5][n:6]1[cH:7][c:8](-[c:9]2[cH:10][cH:11][c:12]([Cl:13])[cH:14][cH:15]2)[cH:16][cH:17][c:18]1=[O:19]
CCC#CCBr.CCCCCC.O=c1cccc[nH]1.[Cl-]
CCC#CCn1cc(-c2ccc(Cl)cc2)ccc1=O
null
null
CN(C)C=O
Aromatic Heterocycle Formation
OtherReaction
c16e53991381708a0d74f5092b5e25b0353184189763eaae006dd565c1174ab9
f1e2d48aa3857a2357f3a371c35806794fc7180cbbfa20a78f207e36837e33dc
O=c1ccc(-c2ccccc2)c[nH]1
Br-[CH2;D2;+0:1]-[C:2]#[C:3]-[C:4].[CH3;D1;+0:5]-[CH2;D2;+0:6]-[CH2;D2;+0:7]-[CH2;D2;+0:8]-[CH2;D2;+0:9]-[CH3;D1;+0:10].[Cl-;H0;D0:11].[O;D1;H0:12]=[c:13]1:[c:14]:[c:15]:[cH;D2;+0:16]:[c:17]:[nH;D2;+0:18]:1>>[C:4]-[C:3]#[C:2]-[CH2;D2;+0:1]-[n;H0;D3;+0:18]1:[c:17]:[c;H0;D3;+0:16](-[c;H0;D3;+0:6]2:[cH;D2;+0:5]:[cH;D2;+0:...
null
[]
0
CELSIUS
null
null
To a suspension of NaH (60% in mineral oil, 200 mg) in dry DMF (50 ml) at 0° C. was added the preceding pyridinone and the mixture was stirred at 0° C. for one half hour. To the resulting suspension was added 1-bromo-2-pentyne dropwise. The resulting mixture was kept at 0° C. during one half hour and poured into satura...
10.6084/m9.figshare.5104873.v1
null
Primary halide
Aromatic halide
c1ccccn1
c1ccncc1.c1ccccc1
c1ccncc1.c1ccccc1
HBr
CN(C)C=O
0
null
CCC#CCBr.CCCCCC.O=c1cccc[nH]1.[Cl-]>CN(C)C=O>CCC#CCn1cc(-c2ccc(Cl)cc2)ccc1=O
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-d0e6fc6e604f42b1aaa518cbc9b8ffed
Nc1ccc(Cl)cc1.O=C(Cl)C=Cc1ccccc1>>O=C(C=Cc1ccccc1)Nc1ccc(Cl)cc1
C(C)(=O)OCC.ClC1=CC=C(N)C=C1.N1=CC=CC=C1.C(C=CC1=CC=CC=C1)(=O)Cl>>ClC1=CC=C(C=C1)NC(C=CC1=CC=CC=C1)=O
[NH2:11][c:12]1[cH:13][cH:14][c:15]([Cl:16])[cH:17][cH:18]1.Cl[C:2](=[O:1])[CH:3]=[CH:4][c:5]1[cH:6][cH:7][cH:8][cH:9][cH:10]1>>[O:1]=[C:2]([CH:3]=[CH:4][c:5]1[cH:6][cH:7][cH:8][cH:9][cH:10]1)[NH:11][c:12]1[cH:13][cH:14][c:15]([Cl:16])[cH:17][cH:18]1
Nc1ccc(Cl)cc1.O=C(Cl)C=Cc1ccccc1
O=C(C=Cc1ccccc1)Nc1ccc(Cl)cc1
null
null
C1(=CC=CC=C1)C.O
Acylation
Acylation of Nitrogen Nucleophiles by Acyl/Thioacyl/Carbamoyl Halides and Analogs_OS
38143a4d536201990008fd6f2c68e6571a341d1c367481869fbbbe36cb038937
0e6ae078978e324f714e184b4f72826d4e3bf2d9ab22d6e9f73740af687be16f
O=C(C=Cc1ccccc1)Nc1ccccc1
Cl-[C;H0;D3;+0:1](=[O;D1;H0:2])-[C:3]=[C:4]-[c:5].[NH2;D1;+0:6]-[c:7](:[c:8]):[c:9]>>[O;D1;H0:2]=[C;H0;D3;+0:1](-[C:3]=[C:4]-[c:5])-[NH;D2;+0:6]-[c:7](:[c:8]):[c:9]
null
[]
0
CELSIUS
15
MINUTE
To a mixture of 4-chloroaniline (16.2 g), toluene (120 ml), and pyridine (11 ml) at 0° C., cinnamoyl chloride (20.0 g) in 120 ml of toluene was added dropwise. After stirring 15 minutes at 0° C. the reaction mixture was poured into a mixture of ethyl acetate: water (250 ml:250 ml). The organic layer was separated and e...
10.6084/m9.figshare.5104873.v1
null
Acyl halide.Primary amine
Secondary amide
null
null
c1ccccc1.c1ccccc1
HCl
C1(=CC=CC=C1)C.O
0
0.25
Nc1ccc(Cl)cc1.O=C(Cl)C=Cc1ccccc1>C1(=CC=CC=C1)C.O>O=C(C=Cc1ccccc1)Nc1ccc(Cl)cc1
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-9b1470facdae4b2f84c618a3f6010aa4
O=C(C=Cc1ccccc1)Nc1ccc(Cl)cc1>>O=c1ccc2c(Cl)cccc2[nH]1
ClC1=CC=C(C=C1)NC(C=CC1=CC=CC=C1)=O.[Cl-].[Al+3].[Cl-].[Cl-]>>ClC1=C2C=CC(NC2=CC=C1)=O
c1ccc([CH:4]=[CH:3][C:2](=[O:1])[NH:12][c:11]2[cH:5][cH:8][c:6]([Cl:7])[cH:9][cH:10]2)cc1>>[O:1]=[c:2]1[cH:3][cH:4][c:5]2[c:6]([Cl:7])[cH:8][cH:9][cH:10][c:11]2[nH:12]1
O=C(C=Cc1ccccc1)Nc1ccc(Cl)cc1
O=c1ccc2c(Cl)cccc2[nH]1
null
null
ClC1=CC=CC=C1
Reduction
OtherReaction
ebe7e954f82f1e726cf9b7a8863216fec31733c3d8bfbb1cc71c49312cec65ac
10d6d5b071f1d84b20b253ce9eadaed211c373c6ee607356078792f13319351a
O=c1ccc2ccccc2[nH]1
[Cl;D1;H0:1]-[c;H0;D3;+0:2]1:[cH;D2;+0:3]:[cH;D2;+0:4]:[c:5](-[NH;D2;+0:6]-[C;H0;D3;+0:7](=[O;D1;H0:8])-[CH;D2;+0:9]=[CH;D2;+0:10]-c2:c:c:c:c:c:2):[c:11]:[cH;D2;+0:12]:1>>[Cl;D1;H0:1]-[c;H0;D3;+0:2]1:[cH;D2;+0:3]:[cH;D2;+0:12]:[c:11]:[c:5]2:[nH;D2;+0:6]:[c;H0;D3;+0:7](=[O;D1;H0:8]):[cH;D2;+0:9]:[cH;D2;+0:10]:[c;H0;D3;+...
null
[]
125
CELSIUS
3
HOUR
To a mixture of N-(4-chlorophenyl)cinnamamide (8.3 g), and chlorobenzene (60 ml) was added portionwise aluminum chloride (21.4 g) under nitrogen at room temperature and the reaction mixture was slowly warmed up to 125° C. and kept at that temperature for 3 hours. The reaction mixture was cooled down and poured over 400...
10.6084/m9.figshare.5104873.v1
null
Aromatic halide.Secondary amide
Aromatic halide
c1ccccc1.c1ccccc1
c1ccc2ccccc2n1
c1ccc2ccccc2n1
Other
ClC1=CC=CC=C1
125
3
O=C(C=Cc1ccccc1)Nc1ccc(Cl)cc1>ClC1=CC=CC=C1>O=c1ccc2c(Cl)cccc2[nH]1
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-437fb7fada4948e496f111fd7c9c5c2e
CCC#CCBr.O=c1ccc2ccccc2[nH]1.[Cl-]>>CCC#CCn1c(=O)ccc2c(Cl)cccc21
[Cl-].[NH4+].N1C(C=CC2=CC=CC=C12)=O.[H-].[Na+].BrCC#CCC>>ClC1=C2C=CC(N(C2=CC=C1)CC#CCC)=O
Br[CH2:5][C:4]#[C:3][CH2:2][CH3:1].[nH:6]1[c:7](=[O:8])[cH:9][cH:10][c:11]2[cH:12][cH:14][cH:15][cH:16][c:17]12.[Cl-:13]>>[CH3:1][CH2:2][C:3]#[C:4][CH2:5][n:6]1[c:7](=[O:8])[cH:9][cH:10][c:11]2[c:12]([Cl:13])[cH:14][cH:15][cH:16][c:17]12
CCC#CCBr.O=c1ccc2ccccc2[nH]1.[Cl-]
CCC#CCn1c(=O)ccc2c(Cl)cccc21
null
null
CN(C)C=O.CCCCCC
Heteroatom Alkylation and Arylation
OtherReaction
a61336fe7a89ec0981a525297b55629e44e830f13f91df56a44bf01390d8c69d
dbda6588fa29cbbc0e3c3f601e69924b300990bdcc56b8cec0535d1258039346
O=c1ccc2ccccc2[nH]1
Br-[CH2;D2;+0:1]-[C:2]#[C:3]-[C:4].[Cl-;H0;D0:5].[O;D1;H0:6]=[c:7]1:[c:8]:[c:9]:[c:10]2:[cH;D2;+0:11]:[c:12]:[c:13]:[c:14]:[c:15]:2:[nH;D2;+0:16]:1>>[C:4]-[C:3]#[C:2]-[CH2;D2;+0:1]-[n;H0;D3;+0:16]1:[c:15]2:[c:14]:[c:13]:[c:12]:[c;H0;D3;+0:11](-[Cl;H0;D1;+0:5]):[c:10]:2:[c:9]:[c:8]:[c:7]:1=[O;D1;H0:6]
null
[]
0
CELSIUS
null
null
To a suspension of NaH (60% in mineral oil, 700 mg) in dry DMF (100 ml) at 0° C. was added the preceding quinolinone (2.05 g) and the mixture was stirred at 0° C. for one half hour. To the resulting suspension was added 1-bromo-2-pentyne (1.6 g) dropwise. The resulting mixture was kept at 0° C. for one half hour and po...
10.6084/m9.figshare.5104873.v1
null
Primary halide
Aromatic halide
c1ccc2ccccc2n1
c1ccc2ncccc2c1
c1ccc2ncccc2c1
HBr
CN(C)C=O.CCCCCC
0
null
CCC#CCBr.O=c1ccc2ccccc2[nH]1.[Cl-]>CN(C)C=O.CCCCCC>CCC#CCn1c(=O)ccc2c(Cl)cccc21
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-a8ade6c521814efe8e95d3631964bfae
CN(C)C=C(C=O)c1ccc(Cl)cc1.NC(N)=O>>O=c1ncc(-c2ccc(Cl)cc2)c[nH]1
[Cl-].[NH4+].ClC1=CC=C(C=C1)C(C=O)=CN(C)C.NC(=O)N.Cl>>ClC1=CC=C(C=C1)C=1C=NC(NC1)=O
CN(C)[CH:4]=[C:5]([c:6]1[cH:7][cH:8][c:9]([Cl:10])[cH:11][cH:12]1)[CH:13]=O.[O:1]=[C:2]([NH2:3])[NH2:14]>>[O:1]=[c:2]1[n:3][cH:4][c:5](-[c:6]2[cH:7][cH:8][c:9]([Cl:10])[cH:11][cH:12]2)[cH:13][nH:14]1
CN(C)C=C(C=O)c1ccc(Cl)cc1.NC(N)=O
O=c1ncc(-c2ccc(Cl)cc2)c[nH]1
null
null
C(C)O.O
Aromatic Heterocycle Formation
OtherReaction
0e1bb7c6fc2fa2fbd0239b648ae136ef123b13ddeb9947c50b8f38d453d7d183
55a949c5abf218b0e7fd0015b81e86fb975fa441e5ac6bd395c3346bb38599f7
O=c1ncc(-c2ccccc2)c[nH]1
C-N(-C)-[CH;D2;+0:1]=[C;H0;D3;+0:2](-[CH;D2;+0:3]=O)-[c;H0;D3;+0:4](:[c:5]:[c:6]):[c:7]:[c:8].[NH2;D1;+0:9]-[C;H0;D3;+0:10](-[NH2;D1;+0:11])=[O;D1;H0:12]>>[O;D1;H0:12]=[c;H0;D3;+0:10]1:[n;H0;D2;+0:11]:[cH;D2;+0:1]:[c;H0;D3;+0:2](-[c;H0;D3;+0:4](:[c:5]:[c:6]):[c:7]:[c:8]):[cH;D2;+0:3]:[nH;D2;+0:9]:1
29.7
[{"value": 29.7, "product": "ClC1=CC=C(C=C1)C=1C=NC(NC1)=O", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
null
null
A mixture of 2-(4-chlorophenyl)dimethylaminopropenal (Example 145a) (5.13 g), urea (2.4 g), concentrated HCl (10 ml), water (4 ml) and ethanol (150 ml) was refluxed for 4 hours. After cooling to room temperature concentrated ammonium chloride was added until the pH was 7. The resulting yellow solid was filtered off and...
10.6084/m9.figshare.5104873.v1
null
Enamine.Aldehyde.Urea
null
null
c1cncnc1
c1cncnc1.c1ccccc1
HO-
C(C)O.O
null
null
CN(C)C=C(C=O)c1ccc(Cl)cc1.NC(N)=O>C(C)O.O>O=c1ncc(-c2ccc(Cl)cc2)c[nH]1
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-d8693bdeb39847fdbe0763c20bb31a87
CCC#CCBr.CCCCCC.O=c1cccc[nH]1.[Cl-].[NH4+]>>CCC#CCn1cc(-c2ccc(Cl)cc2)cnc1=O
[Cl-].[NH4+].CCCCCC.[H-].[Na+].N1C(C=CC=C1)=O.BrCC#CCC>>ClC1=CC=C(C=C1)C=1C=NC(N(C1)CC#CCC)=O
Br[CH2:5][C:4]#[C:3][CH2:2][CH3:1].C[CH2:15][CH2:14][CH2:12][CH2:11][CH3:10].[nH:6]1[cH:7][cH:8][cH:16][cH:9][c:18]1=[O:19].[Cl-:13].[NH4+:17]>>[CH3:1][CH2:2][C:3]#[C:4][CH2:5][n:6]1[cH:7][c:8](-[c:9]2[cH:10][cH:11][c:12]([Cl:13])[cH:14][cH:15]2)[cH:16][n:17][c:18]1=[O:19]
CCC#CCBr.CCCCCC.O=c1cccc[nH]1.[Cl-].[NH4+]
CCC#CCn1cc(-c2ccc(Cl)cc2)cnc1=O
null
null
CN(C)C=O
Aromatic Heterocycle Formation
OtherReaction
b4467fdd65493649554b053844b88f7aedac75ecb5e83a2819a9163270cc6b1f
f1e2d48aa3857a2357f3a371c35806794fc7180cbbfa20a78f207e36837e33dc
O=c1ncc(-c2ccccc2)c[nH]1
Br-[CH2;D2;+0:1]-[C:2]#[C:3]-[C:4].C-[CH2;D2;+0:5]-[CH2;D2;+0:6]-[CH2;D2;+0:7]-[CH2;D2;+0:8]-[CH3;D1;+0:9].[Cl-;H0;D0:10].[NH4+;D0:11].[O;D1;H0:12]=[c;H0;D3;+0:13]1:[cH;D2;+0:14]:[cH;D2;+0:15]:[cH;D2;+0:16]:[c:17]:[nH;D2;+0:18]:1>>[C:4]-[C:3]#[C:2]-[CH2;D2;+0:1]-[n;H0;D3;+0:18]1:[c:17]:[c;H0;D3;+0:16](-[c;H0;D3;+0:14]2...
null
[]
0
CELSIUS
null
null
To a suspension of NaH (60% in mineral oil, 340 mg) in dry DMF (75 ml) at 0° C. was added the preceding pyridinone (1.0 g) and the mixture was stirred at 0° C. for one half hour. To the resulting suspension was added 1-bromo-2-pentyne (750 mg) dropwise. The resulting mixture was kept at 0° C. for one half hour and pour...
10.6084/m9.figshare.5104873.v1
null
Primary halide
Aromatic halide
c1ccccn1
c1cncnc1.c1ccccc1
c1cncnc1.c1ccccc1
HBr
CN(C)C=O
0
null
CCC#CCBr.CCCCCC.O=c1cccc[nH]1.[Cl-].[NH4+]>CN(C)C=O>CCC#CCn1cc(-c2ccc(Cl)cc2)cnc1=O
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-6599866d48314986a02151e7cded27be
O=c1ccc(-c2ccc(Cl)cc2)n[nH]1.S=P12SP3(=S)SP(=S)(S1)SP(=S)(S2)S3>>S=c1ccc(-c2ccc(Cl)cc2)n[nH]1
ClC1=CC=C(C=C1)C=1C=CC(NN1)=O.P12(=S)SP3(=S)SP(=S)(S1)SP(=S)(S2)S3>>ClC1=CC=C(C=C1)C=1C=CC(NN1)=S
O=[c:2]1[cH:3][cH:4][c:5](-[c:6]2[cH:7][cH:8][c:9]([Cl:10])[cH:11][cH:12]2)[n:13][nH:14]1.S=P12SP3(=S)SP(=S)(S1)SP(=[S:1])(S2)S3>>[S:1]=[c:2]1[cH:3][cH:4][c:5](-[c:6]2[cH:7][cH:8][c:9]([Cl:10])[cH:11][cH:12]2)[n:13][nH:14]1
O=c1ccc(-c2ccc(Cl)cc2)n[nH]1.S=P12SP3(=S)SP(=S)(S1)SP(=S)(S2)S3
S=c1ccc(-c2ccc(Cl)cc2)n[nH]1
null
null
N1=CC=CC=C1
Heteroatom Alkylation and Arylation
OtherReaction
e0da8be0c0e31372bc487fca4d998b8539b7ff5b84df07e1a6200efd3593e0bb
13be3f637e1e22872d741944f46b7fcc1954fe982a3a8a0f7825545d455ab147
S=c1ccc(-c2ccccc2)n[nH]1
O=[c;H0;D3;+0:1]1:[#7;a:2]:[#7;a:3]:[c:4]:[c:5]:[c:6]:1.S=P12-S-P3(=S)-S-P(=S)(-S-1)-S-P(=[S;H0;D1;+0:7])(-S-2)-S-3>>[S;H0;D1;+0:7]=[c;H0;D3;+0:1]1:[#7;a:2]:[#7;a:3]:[c:4]:[c:5]:[c:6]:1
187.1
[{"value": 187.1, "product": "ClC1=CC=C(C=C1)C=1C=CC(NN1)=S", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
null
null
A mixture of 3.0 g of 6-(4-chlorophenyl)-pyridazinone, 50 ml of dry pyridine and 3.2 g of phosphorus pentasulfide was refluxed for 1 hour, evaporated to dryness and extracted with 200 ml of ether. The ether extract was washed with water (3×100 ml), brine (100 ml), dried over magnesium sulfate and evaporated to yield 3....
10.6084/m9.figshare.5104873.v1
null
Monosulfide.Monosulfide.Monosulfide.Monosulfide.Monosulfide.Monosulfide
Thiocarbonyl
c1cccnn1.S1P2SP3SP1SP(S2)S3
c1cccnn1
c1cccnn1.c1ccccc1
Other
N1=CC=CC=C1
null
null
O=c1ccc(-c2ccc(Cl)cc2)n[nH]1.S=P12SP3(=S)SP(=S)(S1)SP(=S)(S2)S3>N1=CC=CC=C1>S=c1ccc(-c2ccc(Cl)cc2)n[nH]1
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-d38b7b009446439cb95143c67e49b8ed
NNC(=O)c1ccc(Cl)cc1.O=C(Cl)CCl>>O=C(CCl)NNC(=O)c1ccc(Cl)cc1
ClC1=CC=C(C(=O)NN)C=C1.ClCC(=O)Cl>>ClCC(=O)NNC(C1=CC=C(C=C1)Cl)=O
[NH2:5][NH:6][C:7](=[O:8])[c:9]1[cH:10][cH:11][c:12]([Cl:13])[cH:14][cH:15]1.Cl[C:2](=[O:1])[CH2:3][Cl:4]>>[O:1]=[C:2]([CH2:3][Cl:4])[NH:5][NH:6][C:7](=[O:8])[c:9]1[cH:10][cH:11][c:12]([Cl:13])[cH:14][cH:15]1
NNC(=O)c1ccc(Cl)cc1.O=C(Cl)CCl
O=C(CCl)NNC(=O)c1ccc(Cl)cc1
null
null
O1CCOCC1
Acylation
Acylation of Nitrogen Nucleophiles by Acyl/Thioacyl/Carbamoyl Halides and Analogs_OS
e9c0e57fff756e07b8f823de2eed1eeaae995a83400f2b5e18582349988c9a5f
384006bf8ba751654aef497f42d95dd6fc64342c355d6ce7d0ea9a3aaffeacc6
c1ccccc1
Cl-[C;H0;D3;+0:1](=[O;D1;H0:2])-[C:3]-[Cl;D1;H0:4].[NH2;D1;+0:5]-[#7:6]-[C:7](=[O;D1;H0:8])-[c:9]>>[Cl;D1;H0:4]-[C:3]-[C;H0;D3;+0:1](=[O;D1;H0:2])-[NH;D2;+0:5]-[#7:6]-[C:7](=[O;D1;H0:8])-[c:9]
null
[]
null
null
null
null
To a solution of p-chlorobenzoic hydrazide (11.2 g) in dioxane (100 ml) was added chloroacetyl chloride (6 ml). The resulting mixture was refluxed for three hours, cooled to room temperature and filtered. The resulting solid was washed with ethyl ether and dried to yield N'-chloroacetyl-4-chlorobenzoic hydrazide as whi...
10.6084/m9.figshare.5104873.v1
null
Acyl halide.Acylhydrazine
Acylhydrazine.Acylhydrazine
null
null
c1ccccc1
HCl
O1CCOCC1
null
null
NNC(=O)c1ccc(Cl)cc1.O=C(Cl)CCl>O1CCOCC1>O=C(CCl)NNC(=O)c1ccc(Cl)cc1
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-78ffab45f98b4d54bbf0b4abd3bad247
COC(=S)NN.O=C(CBr)c1ccc(Cl)cc1>>O=C1NN=C(c2ccc(Cl)cc2)CS1
BrCC(=O)C1=CC=C(C=C1)Cl.COC(=S)NN>>ClC1=CC=C(C=C1)C1=NNC(SC1)=O
C[O:1][C:2]([NH:3][NH2:4])=[S:14].O=[C:5]([c:6]1[cH:7][cH:8][c:9]([Cl:10])[cH:11][cH:12]1)[CH2:13]Br>>[O:1]=[C:2]1[NH:3][N:4]=[C:5]([c:6]2[cH:7][cH:8][c:9]([Cl:10])[cH:11][cH:12]2)[CH2:13][S:14]1
COC(=S)NN.O=C(CBr)c1ccc(Cl)cc1
O=C1NN=C(c2ccc(Cl)cc2)CS1
null
null
C(C)#N
Acylation
OtherReaction
a0815ff887854434f061e02bb59e65917f2f792eefe3f407e6f67a241e834044
b7ddc8c969600ae9a9b2d12841c66a24307741bcbfc0810c56e58eb7d0e4892d
O=C1NN=C(c2ccccc2)CS1
Br-[CH2;D2;+0:1]-[C;H0;D3;+0:2](=O)-[c:3](:[c:4]):[c:5].C-[O;H0;D2;+0:6]-[C;H0;D3;+0:7](=[S;H0;D1;+0:8])-[#7:9]-[NH2;D1;+0:10]>>[O;H0;D1;+0:6]=[C;H0;D3;+0:7]1-[#7:9]-[N;H0;D2;+0:10]=[C;H0;D3;+0:2](-[c:3](:[c:4]):[c:5])-[CH2;D2;+0:1]-[S;H0;D2;+0:8]-1
48.4
[{"value": 48.4, "product": "ClC1=CC=C(C=C1)C1=NNC(SC1)=O", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
null
null
A mixture of 2-bromo-p-chloroacetophenone (9.16 g), methoxythiocarbonylhydrazine (13.0 g) and acetonitrile (75 ml) was refluxed overnight and then cooled and filtered. The light yellow solid was washed with hexane and dried yielding 5-(4-chlorophenyl)-3H,6H-1,3,4-thiadiazin-2-one (4.3 g). Conditions: See reaction.notes...
10.6084/m9.figshare.5104873.v1
null
Hydrazine.Primary halide.Ketone.Ether.Thioamide
Hydrazone amide.Monosulfide
null
C1=NNCSC1
C1=NNCSC1.c1ccccc1
HBr
C(C)#N
null
null
COC(=S)NN.O=C(CBr)c1ccc(Cl)cc1>C(C)#N>O=C1NN=C(c2ccc(Cl)cc2)CS1
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-071020b2a4f5457396b9e1aa29ee7de2
O=C(O)CCC(=O)c1cccc(Cl)c1>>O=C(O)CCCc1cccc(Cl)c1
ClC=1C=C(C(=O)CCC(=O)O)C=CC1.[OH-].[K+].NN>>ClC=1C=C(C=CC1)CCCC(=O)O
O=[C:6]([CH2:5][CH2:4][C:2](=[O:1])[OH:3])[c:7]1[cH:8][cH:9][cH:10][c:11]([Cl:12])[cH:13]1>>[O:1]=[C:2]([OH:3])[CH2:4][CH2:5][CH2:6][c:7]1[cH:8][cH:9][cH:10][c:11]([Cl:12])[cH:13]1
O=C(O)CCC(=O)c1cccc(Cl)c1
O=C(O)CCCc1cccc(Cl)c1
null
null
C(COCCO)O
Reduction
OtherReaction
bdac4f77103f4da1c5b42ea95e05b0b7b31176b78204db5f4144ffca7b3d54d5
f9ba67182f94acd5fbe41487f8f71e26bccf898b8fc8091ef46f4363de5628d4
c1ccccc1
O=[C;H0;D3;+0:1](-[C:2]-[C:3]-[C:4](=[O;D1;H0:5])-[O;D1;H1:6])-[c:7](:[c:8]):[c:9]>>[O;D1;H0:5]=[C:4](-[O;D1;H1:6])-[C:3]-[C:2]-[CH2;D2;+0:1]-[c:7](:[c:8]):[c:9]
90.8
[{"value": 90.8, "product": "ClC=1C=C(C=CC1)CCCC(=O)O", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
null
null
To a 300 ml round-bottomed flask equipped with magnetic stirrer and reflux condenser was charged 23.7 g of 87% potassium hydroxide and 150 ml of diethyleneglycol, with stirring, 23 g of 3-(3-chlorobenzoyl)propionic acid was added followed by 24 g of 85% hydrazine. The mixture was heated to reflux for 2 hours when 50 ml...
10.6084/m9.figshare.5104873.v1
null
Ketone
null
null
null
c1ccccc1
Other
C(COCCO)O
null
null
O=C(O)CCC(=O)c1cccc(Cl)c1>C(COCCO)O>O=C(O)CCCc1cccc(Cl)c1
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-ced7355b22f246b584e1e59141387906
CNN.O=C(O)CCC(=O)c1ccc(Cl)cc1>>CN1N=C(c2ccc(Cl)cc2)CCC1=O
ClC1=CC=C(C(=O)CCC(=O)O)C=C1.CNN>>ClC1=CC=C(C=C1)C=1CCC(N(N1)C)=O
[CH3:1][NH:2][NH2:3].O=[C:4]([c:5]1[cH:6][cH:7][c:8]([Cl:9])[cH:10][cH:11]1)[CH2:12][CH2:13][C:14](O)=[O:15]>>[CH3:1][N:2]1[N:3]=[C:4]([c:5]2[cH:6][cH:7][c:8]([Cl:9])[cH:10][cH:11]2)[CH2:12][CH2:13][C:14]1=[O:15]
CNN.O=C(O)CCC(=O)c1ccc(Cl)cc1
CN1N=C(c2ccc(Cl)cc2)CCC1=O
null
null
C(C)O
Acylation
OtherReaction
4e477d09c29dc9649665c2a512a7ab66ed0db9837b745e511eba3c76a3cc18d7
30de68c4dde17a0553a43eee47b1b865b8390bb08557512a59e6e71e0ed0ad51
O=C1CCC(c2ccccc2)=NN1
O-[C;H0;D3;+0:1](=[O;D1;H0:2])-[C:3]-[C:4]-[C;H0;D3;+0:5](=O)-[c:6](:[c:7]):[c:8].[C;D1;H3:9]-[NH;D2;+0:10]-[NH2;D1;+0:11]>>[C;D1;H3:9]-[N;H0;D3;+0:10]1-[N;H0;D2;+0:11]=[C;H0;D3;+0:5](-[c:6](:[c:7]):[c:8])-[C:4]-[C:3]-[C;H0;D3;+0:1]-1=[O;D1;H0:2]
null
[]
null
null
null
null
To a 250 ml flask equipped with magnetic stirrer and reflux condenser was charged 10 g of 3-(4-chlorobenzoyl)-propionic acid, 250 ml of absolute ethanol, and 2.5 ml of methyl hydrazine. The reaction was refluxed for 3 hours and cooled to yield a solid which was collected by vacuum filtration, washed with 50 ml of hexan...
10.6084/m9.figshare.5104873.v1
null
Hydrazine.Carboxylic acid.Ketone
Hydrazone amide
null
C1=N[NH]CCC1
C1=N[NH]CCC1.c1ccccc1
HO-
C(C)O
null
null
CNN.O=C(O)CCC(=O)c1ccc(Cl)cc1>C(C)O>CN1N=C(c2ccc(Cl)cc2)CCC1=O
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-429297c02798479a94358463bcef7999
CC(=O)CCC(=O)O.O=Cc1ccc(Cl)cc1>>O=C(O)CCC(=O)C=Cc1ccc(Cl)cc1
ClC1=CC=C(C=O)C=C1.C(CCC(=O)C)(=O)O.N1CCCCC1.C1(=CC=CC=C1)C>>ClC1=CC=C(C=CC(=O)CCC(=O)O)C=C1
[O:1]=[C:2]([OH:3])[CH2:4][CH2:5][C:6](=[O:7])[CH3:8].O=[CH:9][c:10]1[cH:11][cH:12][c:13]([Cl:14])[cH:15][cH:16]1>>[O:1]=[C:2]([OH:3])[CH2:4][CH2:5][C:6](=[O:7])[CH:8]=[CH:9][c:10]1[cH:11][cH:12][c:13]([Cl:14])[cH:15][cH:16]1
CC(=O)CCC(=O)O.O=Cc1ccc(Cl)cc1
O=C(O)CCC(=O)C=Cc1ccc(Cl)cc1
null
null
O
C-C Coupling
Aldehyde and ketone to alpha,beta-unsaturated carbonyl
df1bdbab1a06af9561d74fe6bc94ee8bda1d14faad9db1ada3a214bd64a24cf8
c93e93ada40f7f922a54fe24d38f540ecf5ff25d55d497f79f5f400f75d0c7ae
c1ccccc1
O=[CH;D2;+0:1]-[c:2](:[c:3]):[c:4].[C:5]-[C:6](-[CH3;D1;+0:7])=[O;D1;H0:8]>>[C:5]-[C:6](=[O;D1;H0:8])-[CH;D2;+0:7]=[CH;D2;+0:1]-[c:2](:[c:3]):[c:4]
44
[{"value": 44.0, "product": "ClC1=CC=C(C=CC(=O)CCC(=O)O)C=C1", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
null
null
To a dry 250 ml flask equipped with a magnetic stirrer, Dean-Stark trap, and reflux condenser was charged 15 g of 4-chlorobenzaldehyde, 12.4 g levulenic acid, 5.7 ml of piperidine, and 100 ml of toluene. The reaction was refluxed for 3 hours, after which no water was observed to azeotrope from the solution. The reactio...
10.6084/m9.figshare.5104873.v1
null
Aldehyde.Ketone
Ketone
null
null
c1ccccc1
HO-
O
null
null
CC(=O)CCC(=O)O.O=Cc1ccc(Cl)cc1>O>O=C(O)CCC(=O)C=Cc1ccc(Cl)cc1
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-5fafd6034f39415a9b2fc5112a7c5611
COc1ccc(C(=O)[O-])c(C)c1[N+](=O)[O-]>>COc1ccc(C(=O)O)cc1[N+](=O)[O-]
[N+](=O)([O-])C=1C(=C(C(=O)[O-])C=CC1OC)C.[OH-].[K+]>>[N+](=O)([O-])C=1C=C(C(=O)O)C=CC1OC
C[c:10]1[c:6]([C:7](=[O:8])[O-:9])[cH:5][cH:4][c:3]([O:2][CH3:1])[c:11]1[N+:12](=[O:13])[O-:14]>>[CH3:1][O:2][c:3]1[cH:4][cH:5][c:6]([C:7](=[O:8])[OH:9])[cH:10][c:11]1[N+:12](=[O:13])[O-:14]
COc1ccc(C(=O)[O-])c(C)c1[N+](=O)[O-]
COc1ccc(C(=O)O)cc1[N+](=O)[O-]
null
null
O1CCCC1
Miscellaneous
OtherReaction
ec2bcf645eed3485ae21dd491bac7887e7ecc8e6727067de36c08c87eaa3e98c
d003579d88c8e6390ed4fac608b8ce68d334559ff02e2f3d9c9936750b60a874
c1ccccc1
C-[c;H0;D3;+0:1](:[c:2](-[#7;+:3]):[c:4]):[c:5](-[C:6](-[O-;H0;D1:7])=[O;D1;H0:8]):[c:9]>>[#7;+:3]-[c:2](:[c:4]):[cH;D2;+0:1]:[c:5](-[C:6](=[O;D1;H0:8])-[OH;D1;+0:7]):[c:9]
76.6
[{"value": 76.6, "product": "[N+](=O)([O-])C=1C=C(C(=O)O)C=CC1OC", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
12
HOUR
To a 500 ml erlenmeyer flask with magnetic stirrer was charged 10.3 g of 3-nitro-4-methoxy-methylbenzoate, 400 ml tetrahydrofuran, and 3.2 g of 86% potassium hydroxide. The reaction was stirred for 12 hours at ambient temperature, after which the resulting solid was collected by vacuum filtration and washed with 2×100 ...
10.6084/m9.figshare.5104873.v1
null
null
Carboxylic acid
c1ccccc1
c1ccccc1
c1ccccc1
Other
O1CCCC1
null
12
COc1ccc(C(=O)[O-])c(C)c1[N+](=O)[O-]>O1CCCC1>COc1ccc(C(=O)O)cc1[N+](=O)[O-]
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-a1b8d0e577394df0ad9547d14447018b
COc1ccc2c(C(=O)c3ccc(OCCN4CCCCC4)cc3)c(N(C)C)sc2c1.[Br][Mg][c]1cccc2ccccc12>>COc1ccc2c(C(=O)c3ccc(OCCN4CCCCC4)cc3)c(-c3cccc4ccccc34)sc2c1
C1(=CC=CC2=CC=CC=C12)[Mg]Br.CN(C=1SC2=C(C1C(=O)C1=CC=C(C=C1)OCCN1CCCCC1)C=CC(=C2)OC)C>>C1(=CC=CC2=CC=CC=C12)C=1SC2=C(C1C(=O)C1=CC=C(C=C1)OCCN1CCCCC1)C=CC(=C2)OC
CN(C)[c:25]1[c:7]([C:8](=[O:9])[c:10]2[cH:11][cH:12][c:13]([O:14][CH2:15][CH2:16][N:17]3[CH2:18][CH2:19][CH2:20][CH2:21][CH2:22]3)[cH:23][cH:24]2)[c:6]2[cH:5][cH:4][c:3]([O:2][CH3:1])[cH:38][c:37]2[s:36]1.[Br][Mg][c:26]1[cH:27][cH:28][cH:29][c:30]2[cH:31][cH:32][cH:33][cH:34][c:35]12>>[CH3:1][O:2][c:3]1[cH:4][cH:5][c:6...
COc1ccc2c(C(=O)c3ccc(OCCN4CCCCC4)cc3)c(N(C)C)sc2c1.[Br][Mg][c]1cccc2ccccc12
COc1ccc2c(C(=O)c3ccc(OCCN4CCCCC4)cc3)c(-c3cccc4ccccc34)sc2c1
null
null
O1CCCC1
C-C Coupling
OtherReaction
1c8033480f43bfecb0046def01a62092035a5425c88b1aeef0ec98f9dc67e298
87044ac4bcbffcaa9a599921042d9edfcfa91aa179fb824aef73cbceb7ea02f9
O=C(c1ccc(OCCN2CCCCC2)cc1)c1c(-c2cccc3ccccc23)sc2ccccc12
C-N(-C)-[c;H0;D3;+0:1]1:[#16;a:2]:[c:3]:[c:4]:[c:5]:1-[C:6](=[O;D1;H0:7])-[c:8].[Br]-[Mg]-[c;H0;D3;+0:9](:[c:10]:[c:11]):[c:12](:[c:13]):[c:14]>>[O;D1;H0:7]=[C:6](-[c:8])-[c:5]1:[c:4]:[c:3]:[#16;a:2]:[c;H0;D3;+0:1]:1-[c;H0;D3;+0:9](:[c:10]:[c:11]):[c:12](:[c:13]):[c:14]
58
[{"value": 58.0, "product": "C1(=CC=CC2=CC=CC=C12)C=1SC2=C(C1C(=O)C1=CC=C(C=C1)OCCN1CCCCC1)C=CC(=C2)OC", "details": "PERCENTYIELD", "is_desired": false}, {"value": 57.5, "product": "C1(=CC=CC2=CC=CC=C12)C=1SC2=C(C1C(=O)C1=CC=C(C=C1)OCCN1CCCCC1)C=CC(=C2)OC", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
null
null
A solution of [2-dimethylamino-6-methoxybenzothien-3-yl][4-[2-(1-piperdinyl)ethoxy]phenyl]methanone (1.58 g, 3.6 mmol) (see U.S. Pat. No. 5,420,349) in tetrahydrofuran (THF, 12 mL) was cooled to 0° C. and treated with a 0.65M THF solution of 1-naphthylmagnesium bromide (20.0 mL, 13 mmol) (prepared from 1-bromonaphthale...
10.6084/m9.figshare.5104873.v1
null
Magnesium halide.Tertiary amine
null
c1ccc2sccc2c1.c1ccc2ccccc2c1
c1ccc2ccccc2c1.c1ccc2sccc2c1
c1ccccc1.C1CC[NH]CC1.c1ccc2ccccc2c1.c1ccc2sccc2c1
HBr.Mg
O1CCCC1
null
null
COc1ccc2c(C(=O)c3ccc(OCCN4CCCCC4)cc3)c(N(C)C)sc2c1.[Br][Mg][c]1cccc2ccccc12>O1CCCC1>COc1ccc2c(C(=O)c3ccc(OCCN4CCCCC4)cc3)c(-c3cccc4ccccc34)sc2c1
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-acaaec7f0b624f78bd5144946ae675b0
COc1ccc2c(C(=O)c3ccc(OCCN4CCCCC4)cc3)c(-c3cccc4ccccc34)sc2c1>>O=C(c1ccc(OCCN2CCCCC2)cc1)c1c(-c2cccc3ccccc23)sc2cc(O)ccc12
C1(=CC=CC2=CC=CC=C12)C=1SC2=C(C1C(=O)C1=CC=C(C=C1)OCCN1CCCCC1)C=CC(=C2)OC.C(C)S.[Cl-].[Al+3].[Cl-].[Cl-]>>C1(=CC=CC2=CC=CC=C12)C=1SC2=C(C1C(=O)C1=CC=C(C=C1)OCCN1CCCCC1)C=CC(=C2)O
C[O:34][c:33]1[cH:32][c:31]2[s:30][c:19](-[c:20]3[cH:21][cH:22][cH:23][c:24]4[cH:25][cH:26][cH:27][cH:28][c:29]34)[c:18]([C:2](=[O:1])[c:3]3[cH:4][cH:5][c:6]([O:7][CH2:8][CH2:9][N:10]4[CH2:11][CH2:12][CH2:13][CH2:14][CH2:15]4)[cH:16][cH:17]3)[c:37]2[cH:36][cH:35]1>>[O:1]=[C:2]([c:3]1[cH:4][cH:5][c:6]([O:7][CH2:8][CH2:9...
COc1ccc2c(C(=O)c3ccc(OCCN4CCCCC4)cc3)c(-c3cccc4ccccc34)sc2c1
O=C(c1ccc(OCCN2CCCCC2)cc1)c1c(-c2cccc3ccccc23)sc2cc(O)ccc12
null
null
C(Cl)Cl
Deprotection
Cleavage of methoxy ethers to alcohols
c5320c7dfa4f544d4900efcae9b3262bf0d5286bcf39c86109232351f35b23d5
26a36596df80ec137b0e8087297418351c93c32819177f680675220622f215d4
O=C(c1ccc(OCCN2CCCCC2)cc1)c1c(-c2cccc3ccccc23)sc2ccccc12
C-[O;H0;D2;+0:1]-[c:2](:[c:3]):[c:4]:[c:5]:[#16;a:6]>>[#16;a:6]:[c:5]:[c:4]:[c:2](-[OH;D1;+0:1]):[c:3]
53.4
[{"value": 53.0, "product": "C1(=CC=CC2=CC=CC=C12)C=1SC2=C(C1C(=O)C1=CC=C(C=C1)OCCN1CCCCC1)C=CC(=C2)O", "details": "PERCENTYIELD", "is_desired": false}, {"value": 53.4, "product": "C1(=CC=CC2=CC=CC=C12)C=1SC2=C(C1C(=O)C1=CC=C(C=C1)OCCN1CCCCC1)C=CC(=C2)O", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
null
null
A solution of the product of Example 1 (1.00 g, 1.92 mmol), ethanethiol (0.45 mL, 6.18 mmol), and aluminum chloride (1.54 g, 11.55 mmol) in anhydrous methylene chloride (40 mL) was stirred for 3.5 hours. The mixture was quenched with saturated potassium sodium tartrate (also known as Rochelle's salt) and extracted with...
10.6084/m9.figshare.5104873.v1
null
Ether
Aromatic alcohol
null
null
c1ccccc1.C1CC[NH]CC1.c1ccc2ccccc2c1.c1ccc2sccc2c1
Other
C(Cl)Cl
null
null
COc1ccc2c(C(=O)c3ccc(OCCN4CCCCC4)cc3)c(-c3cccc4ccccc34)sc2c1>C(Cl)Cl>O=C(c1ccc(OCCN2CCCCC2)cc1)c1c(-c2cccc3ccccc23)sc2cc(O)ccc12
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-091c17ec47894388ba59fc099d21a39b
COc1ccc2c(C(=O)c3ccc(OCCN4CCCCC4)cc3)c(N(C)C)sc2c1.[Br][Mg][c]1ccc2ccccc2c1>>COc1ccc2c(C(=O)c3ccc(OCCN4CCCCC4)cc3)c(-c3ccc4ccccc4c3)sc2c1
C1=C(C=CC2=CC=CC=C12)[Mg]Br.CN(C=1SC2=C(C1C(=O)C1=CC=C(C=C1)OCCN1CCCCC1)C=CC(=C2)OC)C.CO>>C1=C(C=CC2=CC=CC=C12)C=1SC2=C(C1C(=O)C1=CC=C(C=C1)OCCN1CCCCC1)C=CC(=C2)OC
CN(C)[c:25]1[c:7]([C:8](=[O:9])[c:10]2[cH:11][cH:12][c:13]([O:14][CH2:15][CH2:16][N:17]3[CH2:18][CH2:19][CH2:20][CH2:21][CH2:22]3)[cH:23][cH:24]2)[c:6]2[cH:5][cH:4][c:3]([O:2][CH3:1])[cH:38][c:37]2[s:36]1.[Br][Mg][c:26]1[cH:27][cH:28][c:29]2[cH:30][cH:31][cH:32][cH:33][c:34]2[cH:35]1>>[CH3:1][O:2][c:3]1[cH:4][cH:5][c:6...
COc1ccc2c(C(=O)c3ccc(OCCN4CCCCC4)cc3)c(N(C)C)sc2c1.[Br][Mg][c]1ccc2ccccc2c1
COc1ccc2c(C(=O)c3ccc(OCCN4CCCCC4)cc3)c(-c3ccc4ccccc4c3)sc2c1
null
null
C1CCOC1.C(Cl)Cl
C-C Coupling
OtherReaction
1c8033480f43bfecb0046def01a62092035a5425c88b1aeef0ec98f9dc67e298
87044ac4bcbffcaa9a599921042d9edfcfa91aa179fb824aef73cbceb7ea02f9
O=C(c1ccc(OCCN2CCCCC2)cc1)c1c(-c2ccc3ccccc3c2)sc2ccccc12
C-N(-C)-[c;H0;D3;+0:1]1:[#16;a:2]:[c:3]:[c:4]:[c:5]:1-[C:6](=[O;D1;H0:7])-[c:8].[Br]-[Mg]-[c;H0;D3;+0:9](:[c:10]:[c:11]):[c:12]:[c:13]>>[O;D1;H0:7]=[C:6](-[c:8])-[c:5]1:[c:4]:[c:3]:[#16;a:2]:[c;H0;D3;+0:1]:1-[c;H0;D3;+0:9](:[c:10]:[c:11]):[c:12]:[c:13]
75.1
[{"value": 75.0, "product": "C1=C(C=CC2=CC=CC=C12)C=1SC2=C(C1C(=O)C1=CC=C(C=C1)OCCN1CCCCC1)C=CC(=C2)OC", "details": "PERCENTYIELD", "is_desired": false}, {"value": 75.1, "product": "C1=C(C=CC2=CC=CC=C12)C=1SC2=C(C1C(=O)C1=CC=C(C=C1)OCCN1CCCCC1)C=CC(=C2)OC", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
null
null
By the method described in Example 1, [2-dimethylamino-6-methoxybenzothien-3-yl][4-[2-(1-piperdinyl)ethoxy]phenyl]methanone (1.58 g, 3.6 mmol) in THF (12 mL) was reacted with a 0.65M THF solution of 2-naphthylmagnesium bromide (15 mL, 9.8 mmol) to provide, after chromatography (silica gel, 5% methanol in methylene chlo...
10.6084/m9.figshare.5104873.v1
null
Magnesium halide.Tertiary amine
null
c1ccc2sccc2c1.c1ccc2ccccc2c1
c1ccc2ccccc2c1.c1ccc2sccc2c1
c1ccccc1.C1CC[NH]CC1.c1ccc2ccccc2c1.c1ccc2sccc2c1
HBr.Mg
C1CCOC1.C(Cl)Cl
null
null
COc1ccc2c(C(=O)c3ccc(OCCN4CCCCC4)cc3)c(N(C)C)sc2c1.[Br][Mg][c]1ccc2ccccc2c1>C1CCOC1.C(Cl)Cl>COc1ccc2c(C(=O)c3ccc(OCCN4CCCCC4)cc3)c(-c3ccc4ccccc4c3)sc2c1
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-c366215603d74e8f80c204c070b5fd26
COc1ccc2c(C(=O)c3ccc(OCCN4CCCCC4)cc3)c(-c3ccc4ccccc4c3)sc2c1>>O=C(c1ccc(OCCN2CCCCC2)cc1)c1c(-c2ccc3ccccc3c2)sc2cc(O)ccc12
CO.C1=C(C=CC2=CC=CC=C12)C=1SC2=C(C1C(=O)C1=CC=C(C=C1)OCCN1CCCCC1)C=CC(=C2)OC.C(C)S.[Cl-].[Al+3].[Cl-].[Cl-]>>C1=C(C=CC2=CC=CC=C12)C=1SC2=C(C1C(=O)C1=CC=C(C=C1)OCCN1CCCCC1)C=CC(=C2)O
C[O:34][c:33]1[cH:32][c:31]2[s:30][c:19](-[c:20]3[cH:21][cH:22][c:23]4[cH:24][cH:25][cH:26][cH:27][c:28]4[cH:29]3)[c:18]([C:2](=[O:1])[c:3]3[cH:4][cH:5][c:6]([O:7][CH2:8][CH2:9][N:10]4[CH2:11][CH2:12][CH2:13][CH2:14][CH2:15]4)[cH:16][cH:17]3)[c:37]2[cH:36][cH:35]1>>[O:1]=[C:2]([c:3]1[cH:4][cH:5][c:6]([O:7][CH2:8][CH2:9...
COc1ccc2c(C(=O)c3ccc(OCCN4CCCCC4)cc3)c(-c3ccc4ccccc4c3)sc2c1
O=C(c1ccc(OCCN2CCCCC2)cc1)c1c(-c2ccc3ccccc3c2)sc2cc(O)ccc12
null
null
C(Cl)Cl
Deprotection
Cleavage of methoxy ethers to alcohols
c5320c7dfa4f544d4900efcae9b3262bf0d5286bcf39c86109232351f35b23d5
26a36596df80ec137b0e8087297418351c93c32819177f680675220622f215d4
O=C(c1ccc(OCCN2CCCCC2)cc1)c1c(-c2ccc3ccccc3c2)sc2ccccc12
C-[O;H0;D2;+0:1]-[c:2](:[c:3]):[c:4]:[c:5]:[#16;a:6]>>[#16;a:6]:[c:5]:[c:4]:[c:2](-[OH;D1;+0:1]):[c:3]
98.1
[{"value": 98.0, "product": "C1=C(C=CC2=CC=CC=C12)C=1SC2=C(C1C(=O)C1=CC=C(C=C1)OCCN1CCCCC1)C=CC(=C2)O", "details": "PERCENTYIELD", "is_desired": false}, {"value": 98.1, "product": "C1=C(C=CC2=CC=CC=C12)C=1SC2=C(C1C(=O)C1=CC=C(C=C1)OCCN1CCCCC1)C=CC(=C2)O", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
null
null
By the method described in Example 2, the product of Example 3 (1.35 g, 2.59 mmol), ethanethiol (0.56 mL, 7.69 mmol), and aluminum chloride (2.07 g, 15.52 mmol) were reacted in anhydrous methylene chloride (50 mL) to give, after chromatography (silica gel, 5% methanol in methylene chloride) 1.29 g (98%) of the title pr...
10.6084/m9.figshare.5104873.v1
null
Ether
Aromatic alcohol
null
null
c1ccccc1.C1CC[NH]CC1.c1ccc2ccccc2c1.c1ccc2sccc2c1
Other
C(Cl)Cl
null
null
COc1ccc2c(C(=O)c3ccc(OCCN4CCCCC4)cc3)c(-c3ccc4ccccc4c3)sc2c1>C(Cl)Cl>O=C(c1ccc(OCCN2CCCCC2)cc1)c1c(-c2ccc3ccccc3c2)sc2cc(O)ccc12
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-dee584427df84216a8609fe44f49a665
COc1ccc2c(C(=O)c3ccc(OCCN4CCCCC4)cc3)c(N(C)C)sc2c1.[Br][Mg][c]1cccs1>>COc1ccc2c(C(=O)c3ccc(OCCN4CCCCC4)cc3)c(-c3cccs3)sc2c1
S1C(=CC=C1)[Mg]Br.CN(C=1SC2=C(C1C(=O)C1=CC=C(C=C1)OCCN1CCCCC1)C=CC(=C2)OC)C>>S1C(=CC=C1)C=1SC2=C(C1C(=O)C1=CC=C(C=C1)OCCN1CCCCC1)C=CC(=C2)OC
CN(C)[c:25]1[c:7]([C:8](=[O:9])[c:10]2[cH:11][cH:12][c:13]([O:14][CH2:15][CH2:16][N:17]3[CH2:18][CH2:19][CH2:20][CH2:21][CH2:22]3)[cH:23][cH:24]2)[c:6]2[cH:5][cH:4][c:3]([O:2][CH3:1])[cH:33][c:32]2[s:31]1.[Br][Mg][c:26]1[cH:27][cH:28][cH:29][s:30]1>>[CH3:1][O:2][c:3]1[cH:4][cH:5][c:6]2[c:7]([C:8](=[O:9])[c:10]3[cH:11][...
COc1ccc2c(C(=O)c3ccc(OCCN4CCCCC4)cc3)c(N(C)C)sc2c1.[Br][Mg][c]1cccs1
COc1ccc2c(C(=O)c3ccc(OCCN4CCCCC4)cc3)c(-c3cccs3)sc2c1
null
null
C1CCOC1
C-C Coupling
OtherReaction
326d35adb6a1c10eb3af749bc3d574a7fea24f35eecef701ce7ed69d3577388e
87044ac4bcbffcaa9a599921042d9edfcfa91aa179fb824aef73cbceb7ea02f9
O=C(c1ccc(OCCN2CCCCC2)cc1)c1c(-c2cccs2)sc2ccccc12
C-N(-C)-[c;H0;D3;+0:1]1:[#16;a:2]:[c:3]:[c:4]:[c:5]:1-[C:6](=[O;D1;H0:7])-[c:8].[Br]-[Mg]-[c;H0;D3;+0:9]1:[#16;a:10]:[c:11]:[c:12]:[c:13]:1>>[O;D1;H0:7]=[C:6](-[c:8])-[c:5]1:[c:4]:[c:3]:[#16;a:2]:[c;H0;D3;+0:1]:1-[c;H0;D3;+0:9]1:[#16;a:10]:[c:11]:[c:12]:[c:13]:1
72.1
[{"value": 72.0, "product": "S1C(=CC=C1)C=1SC2=C(C1C(=O)C1=CC=C(C=C1)OCCN1CCCCC1)C=CC(=C2)OC", "details": "PERCENTYIELD", "is_desired": false}, {"value": 72.1, "product": "S1C(=CC=C1)C=1SC2=C(C1C(=O)C1=CC=C(C=C1)OCCN1CCCCC1)C=CC(=C2)OC", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
null
null
By the method described in Example 1, [2-dimethylamino-6-methoxybenzothien-3-yl][4-[2-(1-piperdinyl)ethoxy]phenyl]methanone (1.97 g, 4.5 mmol) in THF (15 mL) was reacted with a 0.60M THF solution of 2-thienylmagnesium bromide (31.8 mL, 13.5 mmol) (prepared from 2-bromothiophene, n-butyllithium, and magnesium bromide in...
10.6084/m9.figshare.5104873.v1
null
Magnesium halide.Tertiary amine
null
c1ccc2sccc2c1.c1ccsc1
c1ccsc1.c1ccc2sccc2c1
c1ccccc1.C1CC[NH]CC1.c1ccsc1.c1ccc2sccc2c1
HBr.Mg
C1CCOC1
null
null
COc1ccc2c(C(=O)c3ccc(OCCN4CCCCC4)cc3)c(N(C)C)sc2c1.[Br][Mg][c]1cccs1>C1CCOC1>COc1ccc2c(C(=O)c3ccc(OCCN4CCCCC4)cc3)c(-c3cccs3)sc2c1
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-fd1d646105624c93a6051c2970a32067
COc1ccc([CH2][Mg][Br])cc1.COc1ccc2c(C(=O)c3ccc(OCCN4CCCCC4)cc3)c(N(C)C)sc2c1>>COc1ccc(Cc2sc3cc(OC)ccc3c2C(=O)c2ccc(OCCN3CCCCC3)cc2)cc1
COC1=CC=C(C[Mg]Br)C=C1.CN(C=1SC2=C(C1C(=O)C1=CC=C(C=C1)OCCN1CCCCC1)C=CC(=C2)OC)C>>COC1=CC=C(C=C1)CC=1SC2=C(C1C(=O)C1=CC=C(C=C1)OCCN1CCCCC1)C=CC(=C2)OC
[Br][Mg][CH2:7][c:6]1[cH:5][cH:4][c:3]([O:2][CH3:1])[cH:37][cH:36]1.CN(C)[c:8]1[s:9][c:10]2[cH:11][c:12]([O:13][CH3:14])[cH:15][cH:16][c:17]2[c:18]1[C:19](=[O:20])[c:21]1[cH:22][cH:23][c:24]([O:25][CH2:26][CH2:27][N:28]2[CH2:29][CH2:30][CH2:31][CH2:32][CH2:33]2)[cH:34][cH:35]1>>[CH3:1][O:2][c:3]1[cH:4][cH:5][c:6]([CH2:...
COc1ccc([CH2][Mg][Br])cc1.COc1ccc2c(C(=O)c3ccc(OCCN4CCCCC4)cc3)c(N(C)C)sc2c1
COc1ccc(Cc2sc3cc(OC)ccc3c2C(=O)c2ccc(OCCN3CCCCC3)cc2)cc1
null
null
C1CCOC1
C-C Coupling
OtherReaction
4161a3f4e8978f6ed4d0727517bcf2ac9c3fb21b97d2835a8002b5dd124b6103
87044ac4bcbffcaa9a599921042d9edfcfa91aa179fb824aef73cbceb7ea02f9
O=C(c1ccc(OCCN2CCCCC2)cc1)c1c(Cc2ccccc2)sc2ccccc12
C-N(-C)-[c;H0;D3;+0:1]1:[#16;a:2]:[c:3]:[c:4]:[c:5]:1-[C:6](=[O;D1;H0:7])-[c:8].[Br]-[Mg]-[CH2;D2;+0:9]-[c:10](:[c:11]):[c:12]>>[O;D1;H0:7]=[C:6](-[c:8])-[c:5]1:[c:4]:[c:3]:[#16;a:2]:[c;H0;D3;+0:1]:1-[CH2;D2;+0:9]-[c:10](:[c:11]):[c:12]
29.4
[{"value": 29.0, "product": "COC1=CC=C(C=C1)CC=1SC2=C(C1C(=O)C1=CC=C(C=C1)OCCN1CCCCC1)C=CC(=C2)OC", "details": "PERCENTYIELD", "is_desired": false}, {"value": 29.4, "product": "COC1=CC=C(C=C1)CC=1SC2=C(C1C(=O)C1=CC=C(C=C1)OCCN1CCCCC1)C=CC(=C2)OC", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
null
null
By the method described in Example 1, [2-dimethylamino-6-methoxybenzothien-3-yl][4-[2-(1-piperdinyl)ethoxy]phenyl]-methanone (6.0 g, 13.7 mmol) in THF (51 mL) was reacted with a 0.83M THF solution of 4-methoxybenzylmagnesium bromide (19.8 mL, 16.4 mmol) (prepared from 4-methoxybenzylchloride and magnesium turnings in T...
10.6084/m9.figshare.5104873.v1
null
Magnesium halide.Tertiary amine
null
c1ccc2sccc2c1
c1ccc2sccc2c1
c1ccccc1.c1ccc2sccc2c1.c1ccccc1.C1CC[NH]CC1
HBr.Mg
C1CCOC1
null
null
COc1ccc([CH2][Mg][Br])cc1.COc1ccc2c(C(=O)c3ccc(OCCN4CCCCC4)cc3)c(N(C)C)sc2c1>C1CCOC1>COc1ccc(Cc2sc3cc(OC)ccc3c2C(=O)c2ccc(OCCN3CCCCC3)cc2)cc1
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-137bd4435e364643b101a1a71a0e2096
CCOC(=S)CC.CCOc1ccc(N)cc1>>CCOc1ccc2c(c1)CC(=O)N2
C(C)N(CC)CC.C(C)OC1=CC=C(N)C=C1.CCC(=S)OCC.ClCl>>C(C)OC=1C=C2CC(NC2=CC1)=O
CC[O:12][C:11](=S)[CH2:10]C.[CH3:1][CH2:2][O:3][c:4]1[cH:5][cH:6][c:7]([NH2:13])[cH:8][cH:9]1>>[CH3:1][CH2:2][O:3][c:4]1[cH:5][cH:6][c:7]2[c:8]([cH:9]1)[CH2:10][C:11](=[O:12])[NH:13]2
CCOC(=S)CC.CCOc1ccc(N)cc1
CCOc1ccc2c(c1)CC(=O)N2
null
null
C(Cl)Cl.O
Acylation
OtherReaction
a2a74f97cf7b487de6b223d2dc53dd6aa5e8f47b1840b7ace2677d5fc1e0131e
7ad4bf7309306986e6cc349c7bc628011e853b7eb203cf188a8de27e64e52865
O=C1Cc2ccccc2N1
C-C-[O;H0;D2;+0:1]-[C;H0;D3;+0:2](=S)-[CH2;D2;+0:3]-C.[NH2;D1;+0:4]-[c:5](:[c:6]):[cH;D2;+0:7]:[c:8]:[c:9]>>[O;H0;D1;+0:1]=[C;H0;D3;+0:2]1-[CH2;D2;+0:3]-[c;H0;D3;+0:7](:[c:8]:[c:9]):[c:5](:[c:6])-[NH;D2;+0:4]-1
null
[]
null
null
5
MINUTE
23.6 g of ethyl methylthioacetate in 60 ml of DCM are added to a solution, cooled to about -70° C., of 12.5 g of chlorine in 400 ml of DCM. After stirring for 5 minutes at the same temperature, a solution of 4-ethoxyaniline (48.3 g) in 120 ml of DCM is added. The mixture is stirred for one hour at about -70° C., 39.3 m...
10.6084/m9.figshare.5104873.v1
null
Ether.Primary amine.Thiocarbonyl
Secondary amide
c1ccccc1
c1ccc2c(c1)CCN2
c1ccc2c(c1)CCN2
Other
C(Cl)Cl.O
null
0.083333
CCOC(=S)CC.CCOc1ccc(N)cc1>C(Cl)Cl.O>CCOc1ccc2c(c1)CC(=O)N2
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-6ff5774731954061858d03160b92b6f9
O=C1Nc2ccc(Cl)cc2C1=O.c1ccccc1>>O=C1Nc2ccc(Cl)cc2C1(c1ccccc1)c1ccccc1
ClC=1C=C2C(C(NC2=CC1)=O)=O.[Cl-].[Al+3].[Cl-].[Cl-].C1=CC=CC=C1>>ClC=1C=C2C(C(NC2=CC1)=O)(C1=CC=CC=C1)C1=CC=CC=C1
O=[C:11]1[C:2](=[O:1])[NH:3][c:4]2[cH:5][cH:6][c:7]([Cl:8])[cH:9][c:10]21.[cH:12]1[cH:19][cH:20][cH:21][cH:22][cH:23]1>>[O:1]=[C:2]1[NH:3][c:4]2[cH:5][cH:6][c:7]([Cl:8])[cH:9][c:10]2[C:11]1([c:12]1[cH:13][cH:14][cH:15][cH:16][cH:17]1)[c:18]1[cH:19][cH:20][cH:21][cH:22][cH:23]1
O=C1Nc2ccc(Cl)cc2C1=O.c1ccccc1
O=C1Nc2ccc(Cl)cc2C1(c1ccccc1)c1ccccc1
null
null
null
C-C Coupling
OtherReaction
dba4da327e7262cdcc29a8207cdf08b13f4d7581c1f62dc179c070e46d100989
06a42e352cf517302d592bf38a2fd11b220014e39071074dc7becb6ee0bee4b2
O=C1Nc2ccccc2C1(c1ccccc1)c1ccccc1
O=[C;H0;D3;+0:1]1-[C:2](=[O;D1;H0:3])-[#7:4]-[c:5]:[c:6]-1:[c:7].[c:8]1:[c:9]:[c:10]:[cH;D2;+0:11]:[cH;D2;+0:12]:[cH;D2;+0:13]:1>>[O;D1;H0:3]=[C:2]1-[#7:4]-[c:5]:[c:6](:[c:7])-[C;H0;D4;+0:1]-1(-[c:14]1:[cH;D2;+0:13]:[c:8]:[c:9]:[c:10]:[cH;D2;+0:11]:1)-[c;H0;D3;+0:12](:[c:15]:[c:16]):[c:17]:[c:18]
null
[]
null
null
null
null
This compound is prepared by the method described in Helv. Chim. Acta, 1946, 29, 415-431, by the reaction of benzene with 5-chloroisatin in the presence of aluminum chloride. M.p.=281° C. Conditions: See reaction.notes.procedure_details. Workup: This compound is prepared by the method
10.6084/m9.figshare.5104873.v1
null
Ketone
null
c1ccc2c(c1)CCN2.c1ccccc1
c1ccc2c(c1)CCN2.c1ccccc1.c1ccccc1
c1ccc2c(c1)CCN2.c1ccccc1.c1ccccc1
null
null
null
null
O=C1Nc2ccc(Cl)cc2C1=O.c1ccccc1>>O=C1Nc2ccc(Cl)cc2C1(c1ccccc1)c1ccccc1
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-43d95d9c07ef43d581eb72b8af369b67
CCO.O=C(Cl)c1ccc(F)cc1>>CCOC(=O)c1ccc(F)cc1
FC1=CC=C(C(=O)Cl)C=C1.C(C)O>>FC1=CC=C(C(=O)OCC)C=C1
[CH3:1][CH2:2][OH:3].Cl[C:4](=[O:5])[c:6]1[cH:7][cH:8][c:9]([F:10])[cH:11][cH:12]1>>[CH3:1][CH2:2][O:3][C:4](=[O:5])[c:6]1[cH:7][cH:8][c:9]([F:10])[cH:11][cH:12]1
CCO.O=C(Cl)c1ccc(F)cc1
CCOC(=O)c1ccc(F)cc1
null
null
null
Acylation
Schotten-Baumann to ester
6cefe709828c5bd4655f254e75d5dff9e8876e192e7dd47256c1bc0067bc5291
d8a7643b81ed07a6f633aa99465180dfa0565e61ae25aef36338ebb9837c9cef
c1ccccc1
Cl-[C;H0;D3;+0:1](=[O;D1;H0:2])-[c:3](:[c:4]):[c:5].[C;D1;H3:6]-[C:7]-[OH;D1;+0:8]>>[C;D1;H3:6]-[C:7]-[O;H0;D2;+0:8]-[C;H0;D3;+0:1](=[O;D1;H0:2])-[c:3](:[c:4]):[c:5]
null
[]
null
null
null
null
A mixture containing 35 g of 4-fluorobenzoyl chloride in 50 ml of 100% ethanol is refluxed for 15 minutes. 35 g of the ethyl 4-fluorobenzoate obtained are mixed with 22 g of imidazole and 61 g of potassium carbonate in 35 ml of DMSO. The mixture is heated for 18 hours at 120°-130° C. and 500 ml of iced water are then a...
10.6084/m9.figshare.5104873.v1
null
Acyl halide.Primary alcohol
Ester
null
null
c1ccccc1
HCl
null
null
null
CCO.O=C(Cl)c1ccc(F)cc1>>CCOC(=O)c1ccc(F)cc1
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-60883984e0a345f69557d95970310d78
COC(=O)COc1ccc(C(=O)CBr)cc1.c1cc(N2CCNCC2)ccn1>>COC(=O)COc1ccc(C(=O)CN2CCN(c3ccncc3)CC2)cc1
BrCC(=O)C1=CC=C(OCC(=O)OC)C=C1.N1=CC=C(C=C1)N1CCNCC1>>N1=CC=C(C=C1)N1CCN(CC1)CC(=O)C1=CC=C(OCC(=O)OC)C=C1
Br[CH2:13][C:11]([c:10]1[cH:9][cH:8][c:7]([O:6][CH2:5][C:3]([O:2][CH3:1])=[O:4])[cH:27][cH:26]1)=[O:12].[NH:14]1[CH2:15][CH2:16][N:17]([c:18]2[cH:19][cH:20][n:21][cH:22][cH:23]2)[CH2:24][CH2:25]1>>[CH3:1][O:2][C:3](=[O:4])[CH2:5][O:6][c:7]1[cH:8][cH:9][c:10]([C:11](=[O:12])[CH2:13][N:14]2[CH2:15][CH2:16][N:17]([c:18]3[...
COC(=O)COc1ccc(C(=O)CBr)cc1.c1cc(N2CCNCC2)ccn1
COC(=O)COc1ccc(C(=O)CN2CCN(c3ccncc3)CC2)cc1
null
null
C(C)#N
Heteroatom Alkylation and Arylation
N-alkylation of secondary amines with alkyl halides
f26d51e2c774d81a020fc5d8715a5a6f6b06297cf3257cffbe63e8f82c8c4256
98b92c1800516dd6f2e7ad31e751bba9f02d8a8062f38a8945939bbe90ecca84
O=C(CN1CCN(c2ccncc2)CC1)c1ccccc1
Br-[CH2;D2;+0:1]-[C:2](=[O;D1;H0:3])-[c:4].[#7:5]1-[C:6]-[C:7]-[NH;D2;+0:8]-[C:9]-[C:10]-1>>[O;D1;H0:3]=[C:2](-[c:4])-[CH2;D2;+0:1]-[N;H0;D3;+0:8]1-[C:7]-[C:6]-[#7:5]-[C:10]-[C:9]-1
null
[]
null
null
1.5
HOUR
A solution of methyl 4-bromoacetylphenoxyacetate (4.3 g) in acetonitrile (50 ml) was added dropwise over 40 minutes to a stirred solution of 1-(4-pyridyl)piperazine (4.9 g) in acetonitrile (100 ml). Stirring was continued for a further 1.5 hours, then the solution was filtered and the filtrate evaporated in vacuo. The ...
10.6084/m9.figshare.5104873.v1
null
Primary halide.Ketone.Secondary amine
Ketone.Tertiary amine
C1CNCC[NH]1
C1C[NH]CC[NH]1
c1ccccc1.C1C[NH]CC[NH]1.c1ccncc1
HBr
C(C)#N
null
1.5
COC(=O)COc1ccc(C(=O)CBr)cc1.c1cc(N2CCNCC2)ccn1>C(C)#N>COC(=O)COc1ccc(C(=O)CN2CCN(c3ccncc3)CC2)cc1
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-369459ec0ce24604a44164b3a522b96e
COC(=O)COc1ccc(C(=O)CN2CCN(c3ccncc3)CC2)cc1>>O=C(O)COc1ccc(C(=O)CN2CCN(c3ccncc3)CC2)cc1
N1=CC=C(C=C1)N1CCN(CC1)CC(=O)C1=CC=C(OCC(=O)OC)C=C1.[OH-].[Na+]>>N1=CC=C(C=C1)N1CCN(CC1)CC(=O)C1=CC=C(OCC(=O)O)C=C1
C[O:3][C:2](=[O:1])[CH2:4][O:5][c:6]1[cH:7][cH:8][c:9]([C:10](=[O:11])[CH2:12][N:13]2[CH2:14][CH2:15][N:16]([c:17]3[cH:18][cH:19][n:20][cH:21][cH:22]3)[CH2:23][CH2:24]2)[cH:25][cH:26]1>>[O:1]=[C:2]([OH:3])[CH2:4][O:5][c:6]1[cH:7][cH:8][c:9]([C:10](=[O:11])[CH2:12][N:13]2[CH2:14][CH2:15][N:16]([c:17]3[cH:18][cH:19][n:20...
COC(=O)COc1ccc(C(=O)CN2CCN(c3ccncc3)CC2)cc1
O=C(O)COc1ccc(C(=O)CN2CCN(c3ccncc3)CC2)cc1
null
null
CO.O
Deprotection
Ester saponification (methyl deprotection)
d872e08ad5c85a4add6cd04e6e987e73fead5f79b3f30ba61a81ba5029b29894
38ae1ee78433b9acfb0390501446149c80f88f23ac2d84c60b3369bdab75cec9
O=C(CN1CCN(c2ccncc2)CC1)c1ccccc1
C-[O;H0;D2;+0:1]-[C:2](-[C:3])=[O;D1;H0:4]>>[C:3]-[C:2](=[O;D1;H0:4])-[OH;D1;+0:1]
null
[]
4
CELSIUS
2
HOUR
A stirred solution of the product of Example 1 (550 mg) in methanol (10 ml) was treated with a M sodium hydroxide solution (1.65 ml) and stirring continued for a further 2 hours. The mixture was diluted with water (10 ml) and the resulting solution concentrated in vacuo. Water (20 ml) was added and then a M hydrochlori...
10.6084/m9.figshare.5104873.v1
null
Ester
Carboxylic acid
null
null
c1ccccc1.C1C[NH]CC[NH]1.c1ccncc1
Other
CO.O
4
2
COC(=O)COc1ccc(C(=O)CN2CCN(c3ccncc3)CC2)cc1>CO.O>O=C(O)COc1ccc(C(=O)CN2CCN(c3ccncc3)CC2)cc1
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-2900eeef6bee4f96854b610d5c6665dc
COC(=O)COc1ccc(C(=O)CN2CCN(c3ccncc3)CC2)cc1OC>>COc1cc(C(=O)CN2CCN(c3ccncc3)CC2)ccc1OCC(=O)O
N1=CC=C(C=C1)N1CCN(CC1)CC(=O)C1=CC(=C(OCC(=O)OC)C=C1)OC>>N1=CC=C(C=C1)N1CCN(CC1)CC(=O)C1=CC(=C(OCC(=O)O)C=C1)OC
C[O:28][C:26]([CH2:25][O:24][c:23]1[c:3]([O:2][CH3:1])[cH:4][c:5]([C:6](=[O:7])[CH2:8][N:9]2[CH2:10][CH2:11][N:12]([c:13]3[cH:14][cH:15][n:16][cH:17][cH:18]3)[CH2:19][CH2:20]2)[cH:21][cH:22]1)=[O:27]>>[CH3:1][O:2][c:3]1[cH:4][c:5]([C:6](=[O:7])[CH2:8][N:9]2[CH2:10][CH2:11][N:12]([c:13]3[cH:14][cH:15][n:16][cH:17][cH:18...
COC(=O)COc1ccc(C(=O)CN2CCN(c3ccncc3)CC2)cc1OC
COc1cc(C(=O)CN2CCN(c3ccncc3)CC2)ccc1OCC(=O)O
null
null
O
Deprotection
Ester saponification (methyl deprotection)
d872e08ad5c85a4add6cd04e6e987e73fead5f79b3f30ba61a81ba5029b29894
38ae1ee78433b9acfb0390501446149c80f88f23ac2d84c60b3369bdab75cec9
O=C(CN1CCN(c2ccncc2)CC1)c1ccccc1
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]
47
[{"value": 47.0, "product": "N1=CC=C(C=C1)N1CCN(CC1)CC(=O)C1=CC(=C(OCC(=O)O)C=C1)OC", "details": "PERCENTYIELD", "is_desired": false}]
null
null
null
null
In a similar manner to Example 2, but starting from the product of Example 5, the title compound was prepared in 47% yield: m.p. 218°-224° C.; NMR(d6DMSO) δ 8.16(2H,d), 7.65(1H,dd), 7.53(1H,d), 6.92(1H,d), 6.85(2H,d), 4.73(2H,s), 3.86(2H,s), 3.82(3H,s), 3.36(4H,t), 2.63(4H,t); m/e 386(M+H)+ ; calculated for C20H23N3O5....
10.6084/m9.figshare.5104873.v1
null
Ester
Carboxylic acid
null
null
c1ccccc1.C1C[NH]CC[NH]1.c1ccncc1
Other
O
null
null
COC(=O)COc1ccc(C(=O)CN2CCN(c3ccncc3)CC2)cc1OC>O>COc1cc(C(=O)CN2CCN(c3ccncc3)CC2)ccc1OCC(=O)O
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-4789241e5b8e4d179a6429cc6ce17888
COC(=O)COc1ccccc1.O=C(Cl)CCCl>>COC(=O)COc1ccc(C(=O)CCCl)cc1
O(C1=CC=CC=C1)CC(=O)OC.ClCCC(=O)Cl.[Cl-].[Al+3].[Cl-].[Cl-]>>ClCCC(=O)C1=CC=C(OCC(=O)OC)C=C1
[CH3:1][O:2][C:3](=[O:4])[CH2:5][O:6][c:7]1[cH:8][cH:9][cH:10][cH:16][cH:17]1.Cl[C:11](=[O:12])[CH2:13][CH2:14][Cl:15]>>[CH3:1][O:2][C:3](=[O:4])[CH2:5][O:6][c:7]1[cH:8][cH:9][c:10]([C:11](=[O:12])[CH2:13][CH2:14][Cl:15])[cH:16][cH:17]1
COC(=O)COc1ccccc1.O=C(Cl)CCCl
COC(=O)COc1ccc(C(=O)CCCl)cc1
null
null
ClCCl
C-C Coupling
Friedel-Crafts acylation
55541449ad4f182ef3dc0497085b282b1dcb76e0fb5ed140dc4eab4973eacb28
fe2a4a0dfbb5b71b9a065e092364c64b22b4eb1ad4d6ba2a1e8edc9d31fce3e4
c1ccccc1
Cl-[C;H0;D3;+0:1](=[O;D1;H0:2])-[C:3]-[C:4].[c:5]:[c:6]:[cH;D2;+0:7]:[c:8]:[c:9]>>[C:4]-[C:3]-[C;H0;D3;+0:1](=[O;D1;H0:2])-[c;H0;D3;+0:7](:[c:6]:[c:5]):[c:8]:[c:9]
null
[]
null
null
1
HOUR
Aluminium chloride (33.35 g) was added portionwise to a stirred cooled (<0° C.) solution of methyl phenoxyacetate (14.46 ml) and 3-chloropropionyl chloride (9.55 ml) in dichloromethane (500 ml). After the addition the ice-bath was removed and the mixture stirred for 1 hour when it was poured into ice-water (500 ml). Th...
10.6084/m9.figshare.5104873.v1
null
Acyl halide
Ketone
c1ccccc1
c1ccccc1
c1ccccc1
HCl
ClCCl
null
1
COC(=O)COc1ccccc1.O=C(Cl)CCCl>ClCCl>COC(=O)COc1ccc(C(=O)CCCl)cc1
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-dec26e4a500a423b998283ba15ea943b
COC(=O)Cc1ccc(C(=O)CCl)cc1.c1cc(N2CCNCC2)ccn1>>COC(=O)Cc1ccc(C(=O)CN2CCN(c3ccncc3)CC2)cc1
ClCC(=O)C1=CC=C(C=C1)CC(=O)OC.N1=CC=C(C=C1)N1CCNCC1>>N1=CC=C(C=C1)N1CCN(CC1)CC(=O)C1=CC=C(C=C1)CC(=O)OC
Cl[CH2:12][C:10]([c:9]1[cH:8][cH:7][c:6]([CH2:5][C:3]([O:2][CH3:1])=[O:4])[cH:26][cH:25]1)=[O:11].[NH:13]1[CH2:14][CH2:15][N:16]([c:17]2[cH:18][cH:19][n:20][cH:21][cH:22]2)[CH2:23][CH2:24]1>>[CH3:1][O:2][C:3](=[O:4])[CH2:5][c:6]1[cH:7][cH:8][c:9]([C:10](=[O:11])[CH2:12][N:13]2[CH2:14][CH2:15][N:16]([c:17]3[cH:18][cH:19...
COC(=O)Cc1ccc(C(=O)CCl)cc1.c1cc(N2CCNCC2)ccn1
COC(=O)Cc1ccc(C(=O)CN2CCN(c3ccncc3)CC2)cc1
null
null
C(C)#N
Heteroatom Alkylation and Arylation
N-alkylation of secondary amines with alkyl halides
f26d51e2c774d81a020fc5d8715a5a6f6b06297cf3257cffbe63e8f82c8c4256
98b92c1800516dd6f2e7ad31e751bba9f02d8a8062f38a8945939bbe90ecca84
O=C(CN1CCN(c2ccncc2)CC1)c1ccccc1
Cl-[CH2;D2;+0:1]-[C:2](=[O;D1;H0:3])-[c:4].[#7:5]1-[C:6]-[C:7]-[NH;D2;+0:8]-[C:9]-[C:10]-1>>[O;D1;H0:3]=[C:2](-[c:4])-[CH2;D2;+0:1]-[N;H0;D3;+0:8]1-[C:7]-[C:6]-[#7:5]-[C:10]-[C:9]-1
null
[]
null
null
8
HOUR
A solution of methyl 4-chloroacetylphenylacetate (260 mg) in acetonitrile (4 ml) was added dropwise over 15 minutes to a stirred solution of 1-(4-pyridyl)piperazine (375 mg) in acetonitrile (10 ml) and the mixture stirred overnight. The supernatent was decanted from the solid formed, concentrated in vacuo and purified ...
10.6084/m9.figshare.5104873.v1
null
Primary halide.Ketone.Secondary amine
Ketone.Tertiary amine
C1CNCC[NH]1
C1C[NH]CC[NH]1
c1ccccc1.C1C[NH]CC[NH]1.c1ccncc1
HCl
C(C)#N
null
8
COC(=O)Cc1ccc(C(=O)CCl)cc1.c1cc(N2CCNCC2)ccn1>C(C)#N>COC(=O)Cc1ccc(C(=O)CN2CCN(c3ccncc3)CC2)cc1
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-77e50f1da1444b07b851d442f07f91b1
CCC(=O)c1ccc(OCC(=O)OC)cc1.c1cc(N2CCNCC2)ccn1>>COC(=O)COc1ccc(C(=O)C(C)N2CCN(c3ccncc3)CC2)cc1
CCC(=O)C1=CC=C(OCC(=O)OC)C=C1.N1=CC=C(C=C1)N1CCNCC1>>N1=CC=C(C=C1)N1CCN(CC1)C(C(=O)C1=CC=C(OCC(=O)OC)C=C1)C
[CH3:1][O:2][C:3](=[O:4])[CH2:5][O:6][c:7]1[cH:8][cH:9][c:10]([C:11](=[O:12])[CH2:13][CH3:14])[cH:27][cH:28]1.[NH:15]1[CH2:16][CH2:17][N:18]([c:19]2[cH:20][cH:21][n:22][cH:23][cH:24]2)[CH2:25][CH2:26]1>>[CH3:1][O:2][C:3](=[O:4])[CH2:5][O:6][c:7]1[cH:8][cH:9][c:10]([C:11](=[O:12])[CH:13]([CH3:14])[N:15]2[CH2:16][CH2:17]...
CCC(=O)c1ccc(OCC(=O)OC)cc1.c1cc(N2CCNCC2)ccn1
COC(=O)COc1ccc(C(=O)C(C)N2CCN(c3ccncc3)CC2)cc1
null
null
C(C)#N
Heteroatom Alkylation and Arylation
OtherReaction
3a3ed397381e44670ce2e8342acad8222d2432ca85ece7a4615c2b6be4971f24
35f76118ef70465dec1f1daab296204894422630ea976731c8b4f0c910a4773f
O=C(CN1CCN(c2ccncc2)CC1)c1ccccc1
[#7:1]1-[C:2]-[C:3]-[NH;D2;+0:4]-[C:5]-[C:6]-1.[C;D1;H3:7]-[CH2;D2;+0:8]-[C:9](=[O;D1;H0:10])-[c:11]>>[C;D1;H3:7]-[CH;D3;+0:8](-[C:9](=[O;D1;H0:10])-[c:11])-[N;H0;D3;+0:4]1-[C:3]-[C:2]-[#7:1]-[C:6]-[C:5]-1
null
[]
null
null
8
HOUR
A solution of RS methyl 4-(2-methylacetyl)phenoxyacetate (1.2 g) in acetonitrile (10 ml) was added dropwise over 30 minutes to a stirred solution of 1-(4-pyridyl)piperazine (1.3 g) in acetonitrile (30 ml) and the mixture stirred overnight. The mixture was then filtered and the filtrate evaporated to give an oil. Purifi...
10.6084/m9.figshare.5104873.v1
null
Ketone.Secondary amine
Ketone.Tertiary amine
C1CNCC[NH]1
C1C[NH]CC[NH]1
c1ccccc1.C1C[NH]CC[NH]1.c1ccncc1
null
C(C)#N
null
8
CCC(=O)c1ccc(OCC(=O)OC)cc1.c1cc(N2CCNCC2)ccn1>C(C)#N>COC(=O)COc1ccc(C(=O)C(C)N2CCN(c3ccncc3)CC2)cc1
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-9af742574ebf4d4aa094524fbbb466cc
CCOC(=O)CCCBr.Oc1ccc(N2CCN(c3ccncc3)CC2)cc1>>CCOC(=O)CCCOc1ccc(N2CCN(c3ccncc3)CC2)cc1
N1=CC=C(C=C1)N1CCN(CC1)C1=CC=C(C=C1)O.[H-].[Na+].BrCCCC(=O)OCC>>N1=CC=C(C=C1)N1CCN(CC1)C1=CC=C(OCCCC(=O)OCC)C=C1
Br[CH2:8][CH2:7][CH2:6][C:4]([O:3][CH2:2][CH3:1])=[O:5].[OH:9][c:10]1[cH:11][cH:12][c:13]([N:14]2[CH2:15][CH2:16][N:17]([c:18]3[cH:19][cH:20][n:21][cH:22][cH:23]3)[CH2:24][CH2:25]2)[cH:26][cH:27]1>>[CH3:1][CH2:2][O:3][C:4](=[O:5])[CH2:6][CH2:7][CH2:8][O:9][c:10]1[cH:11][cH:12][c:13]([N:14]2[CH2:15][CH2:16][N:17]([c:18]...
CCOC(=O)CCCBr.Oc1ccc(N2CCN(c3ccncc3)CC2)cc1
CCOC(=O)CCCOc1ccc(N2CCN(c3ccncc3)CC2)cc1
null
null
CN(C)C=O
Heteroatom Alkylation and Arylation
Williamson Ether Synthesis
7e1040116e3a4cf0e8ec5cc7865388d9cd0efabce6d320a1c25a36e411018d8b
d5f4610d46ccc0478471c5bc0fb862644eaf764bbc5d93badb39d54f6ec8e0a5
c1ccc(N2CCN(c3ccncc3)CC2)cc1
Br-[CH2;D2;+0:1]-[C:2]-[C:3]-[C:4](-[#8:5])=[O;D1;H0:6].[OH;D1;+0:7]-[c:8](:[c:9]):[c:10]>>[#8:5]-[C:4](=[O;D1;H0:6])-[C:3]-[C:2]-[CH2;D2;+0:1]-[O;H0;D2;+0:7]-[c:8](:[c:9]):[c:10]
null
[]
null
null
1
HOUR
A stirred suspension of 4-(4-(4-pyridyl)piperazin-1-yl)-phenol (1.34 g) in dry DMF (20 ml) was treated with sodium hydride (60% dispersion in mineral oil, 0.21 g) and the mixture stirred for 1 hour. To the resulting solution was added ethyl 4-bromobutyrate and the mixture was stirred for 16 hours. Solvent was evaporate...
10.6084/m9.figshare.5104873.v1
null
Primary halide.Aromatic alcohol
Ether
null
null
c1ccccc1.C1C[NH]CC[NH]1.c1ccncc1
HBr
CN(C)C=O
null
1
CCOC(=O)CCCBr.Oc1ccc(N2CCN(c3ccncc3)CC2)cc1>CN(C)C=O>CCOC(=O)CCCOc1ccc(N2CCN(c3ccncc3)CC2)cc1