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-02ee2261663048188cf6d85d2cc96e3f
ord-0ff8025e8c5444e9b4b310a7c0c96dda
Nc1nc(N)nc(N)n1>>Nc1nc(N)nc(N)n1
C=O.[OH-].[Na+].N1=C(N)N=C(N)N=C1N.[Na]>>C=O.N1=C(N)N=C(N)N=C1N
[NH2:3][c:4]1[n:5][c:6]([NH2:7])[n:8][c:9]([NH2:10])[n:11]1>>[NH2:3][c:4]1[n:5][c:6]([NH2:7])[n:8][c:9]([NH2:10])[n:11]1
Nc1nc(N)nc(N)n1
Nc1nc(N)nc(N)n1
null
null
O
Miscellaneous
OtherReaction
40ba59785861b8226ce5af6bdcbb9a37f0ff50a8c7ec7d4fc4c524cf906cc65c
56ebed4a8b3cebec83c37a71d68f0c87d1e404ab05a9ce792691e4e18a2379dd
c1ncncn1
null
null
[]
60
CELSIUS
30
MINUTE
50 parts of 20% liquor A (dispersion of aromatic isocyanate compound) and 100 parts of 30% liquor B (co-dispersion of imino compound-sensitizer) obtained in the above (1) were mixed with each other until a homogeneous mixture was obtained. 150 parts of the mixture of liquor A and liquor B was gradually added with 120 p...
10.6084/m9.figshare.5104873.v1
null
null
null
null
null
c1ncncn1
null
O
60
0.5
Nc1nc(N)nc(N)n1>O>Nc1nc(N)nc(N)n1
ord_dataset-02ee2261663048188cf6d85d2cc96e3f
ord-988a2c53241846448be5b0c88940992d
Nc1nc(N)nc(N)n1>>Nc1nc(N)nc(N)n1
[Na].C(=CC1=CC=CC=C1)/C/1=C/C(=O)OC1=O.N1=C(N)N=C(N)N=C1N.C=O.[OH-].[Na+]>>C=O.N1=C(N)N=C(N)N=C1N
[NH2:3][c:4]1[n:5][c:6]([NH2:7])[n:8][c:9]([NH2:10])[n:11]1>>[NH2:3][c:4]1[n:5][c:6]([NH2:7])[n:8][c:9]([NH2:10])[n:11]1
Nc1nc(N)nc(N)n1
Nc1nc(N)nc(N)n1
null
null
O
Miscellaneous
OtherReaction
40ba59785861b8226ce5af6bdcbb9a37f0ff50a8c7ec7d4fc4c524cf906cc65c
56ebed4a8b3cebec83c37a71d68f0c87d1e404ab05a9ce792691e4e18a2379dd
c1ncncn1
null
null
[]
60
CELSIUS
30
MINUTE
Previously, 50 parts of 20% liquor A (dispersion of aromatic isocyanate compound) and 50 parts of 40% liquor B (co-dispersion of imino compound-sensitizer) obtained by grinding and dispersing in the above (1) were mixed with each other until a homogeneous mixture was obtained. The resulting homogeneous mixture of liquo...
10.6084/m9.figshare.5104873.v1
null
null
null
null
null
c1ncncn1
null
O
60
0.5
Nc1nc(N)nc(N)n1>O>Nc1nc(N)nc(N)n1
ord_dataset-02ee2261663048188cf6d85d2cc96e3f
ord-532890acfa0c4878a648f53eab17e89c
Nc1nc(N)nc(N)n1>>Nc1nc(N)nc(N)n1
[Na].N1=C(N)N=C(N)N=C1N.C=O.N.[OH-].[Na+].N>>C=O.N1=C(N)N=C(N)N=C1N
[NH2:3][c:4]1[n:5][c:6]([NH2:7])[n:8][c:9]([NH2:10])[n:11]1>>[NH2:3][c:4]1[n:5][c:6]([NH2:7])[n:8][c:9]([NH2:10])[n:11]1
Nc1nc(N)nc(N)n1
Nc1nc(N)nc(N)n1
null
null
O
Miscellaneous
OtherReaction
40ba59785861b8226ce5af6bdcbb9a37f0ff50a8c7ec7d4fc4c524cf906cc65c
56ebed4a8b3cebec83c37a71d68f0c87d1e404ab05a9ce792691e4e18a2379dd
c1ncncn1
null
null
[]
60
CELSIUS
30
MINUTE
Previously, 50 parts of 20% liquor A (dispersion of aromatic isocyanate compound) and 100 parts of 30% liquor B (co-dispersion of imino compound-sensitizer) obtained by grinding and dispersing in the above (1) were mixed with each other until a homogeneous mixture was obtained. The resulting homogeneous mixture of liqu...
10.6084/m9.figshare.5104873.v1
null
null
null
null
null
c1ncncn1
null
O
60
0.5
Nc1nc(N)nc(N)n1>O>Nc1nc(N)nc(N)n1
ord_dataset-02ee2261663048188cf6d85d2cc96e3f
ord-ea88f85ac3924f1abb143061996c57cd
CC(C)(C)[C@@H](N)C(N)=O>>CC(C)(C)[C@H](N)C(N)=O
NC(C(C)(C)C)C(=O)N.N[C@@H](C(C)(C)C)C(=O)O.N[C@H](C(C)(C)C)C(=O)N>>N[C@@H](C(C)(C)C)C(=O)N
[CH3:1][C:2]([CH3:3])([CH3:4])[C@@H:5]([NH2:6])[C:7]([NH2:8])=[O:9]>>[CH3:1][C:2]([CH3:3])([CH3:4])[C@H:5]([NH2:6])[C:7]([NH2:8])=[O:9]
CC(C)(C)[C@@H](N)C(N)=O
CC(C)(C)[C@H](N)C(N)=O
null
null
null
Miscellaneous
OtherReaction
40ba59785861b8226ce5af6bdcbb9a37f0ff50a8c7ec7d4fc4c524cf906cc65c
56ebed4a8b3cebec83c37a71d68f0c87d1e404ab05a9ce792691e4e18a2379dd
null
null
null
[]
null
null
null
null
In the same way as in example VIII, an incubation was carried out with DL-tertiary leucine amide. Analysis of the remaining reaction mixture after 8 hours showed that both L-tertiary leucine and D-tertiary leucine amide with an e.e. of ≥99% were present in the reaction mixture. Conditions: See reaction.notes.procedure_...
10.6084/m9.figshare.5104873.v1
null
null
null
null
null
null
null
null
null
null
CC(C)(C)[C@@H](N)C(N)=O>>CC(C)(C)[C@H](N)C(N)=O
ord_dataset-02ee2261663048188cf6d85d2cc96e3f
ord-844e9b86e04349d6a419372f67937301
CO.O=C(O)C(O)c1ccc(Br)cc1>>COC(=O)C(O)c1ccc(Br)cc1
BrC1=CC=C(C=C1)C(C(=O)O)O.CO.S(O)(O)(=O)=O>>BrC1=CC=C(C=C1)C(C(=O)OC)O
[CH3:1][OH:2].O[C:3](=[O:4])[CH:5]([OH:6])[c:7]1[cH:8][cH:9][c:10]([Br:11])[cH:12][cH:13]1>>[CH3:1][O:2][C:3](=[O:4])[CH:5]([OH:6])[c:7]1[cH:8][cH:9][c:10]([Br:11])[cH:12][cH:13]1
CO.O=C(O)C(O)c1ccc(Br)cc1
COC(=O)C(O)c1ccc(Br)cc1
null
null
O
Protection
Esterification of Carboxylic Acids
9cecdbd189c6f9c3648521d17154d013842a5498de4e76e65efb1d842973340b
af0b8064f2e82ebe66c4c29d2391785ac1b993104265ccdc4d67ca79e36fa3c8
c1ccccc1
O-[C;H0;D3;+0:1](=[O;D1;H0:2])-[C:3](-[O;D1;H1:4])-[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](-[O;D1;H1:4])-[c:5]
92
[{"value": 92.0, "product": "BrC1=CC=C(C=C1)C(C(=O)OC)O", "details": "PERCENTYIELD", "is_desired": false}]
null
null
3
HOUR
A mixture of 20 g (87 mmol) of (±)-4-bromo-α-hydroxyphenylacetic acid, 200 ml of methanol and 2 ml of concentrated sulfuric acid was stirred for 3 hours at room temperature. To the mixture 50 ml of water was added. After the solution was extracted with ethyl acetate, the organic extract was washed with a saturated aque...
10.6084/m9.figshare.5104873.v1
null
Carboxylic acid.Methanol
Ester
null
null
c1ccccc1
HO-
O
null
3
CO.O=C(O)C(O)c1ccc(Br)cc1>O>COC(=O)C(O)c1ccc(Br)cc1
ord_dataset-02ee2261663048188cf6d85d2cc96e3f
ord-82e83c02b9134508a72b2b79ba90c519
CCCCCCCCOc1ccc(O)c(F)c1F.CCCCCCOc1ccc(C(=O)O)cc1>>CCCCCCCCOc1ccc(OC(=O)c2ccc(OCCCCCC)cc2)c(F)c1F
C(C)(C)(C)OO.C(CCC)[Li].C1(CCCCC1)N=C=NC1CCCCC1.C(CCCCC)OC1=CC=C(C(=O)O)C=C1.CN(C)C1=NC=CC=C1.FC1=C(C=CC(=C1F)OCCCCCCCC)O.FC(COC1=CC=CC=C1)C(CCCCC)F.C(C)(C)(C)OOC(C)(C)C.[Li]>>C(CCCCC)OC1=CC=C(C(=O)OC2=C(C(=C(C=C2)OCCCCCCCC)F)F)C=C1
[CH3:1][CH2:2][CH2:3][CH2:4][CH2:5][CH2:6][CH2:7][CH2:8][O:9][c:10]1[cH:11][cH:12][c:13]([OH:14])[c:30]([F:31])[c:32]1[F:33].O[C:15](=[O:16])[c:17]1[cH:18][cH:19][c:20]([O:21][CH2:22][CH2:23][CH2:24][CH2:25][CH2:26][CH3:27])[cH:28][cH:29]1>>[CH3:1][CH2:2][CH2:3][CH2:4][CH2:5][CH2:6][CH2:7][CH2:8][O:9][c:10]1[cH:11][cH:...
CCCCCCCCOc1ccc(O)c(F)c1F.CCCCCCOc1ccc(C(=O)O)cc1
CCCCCCCCOc1ccc(OC(=O)c2ccc(OCCCCCC)cc2)c(F)c1F
null
null
ClCCl.CCOCC
Acylation
Mitsunobu esterification
f18451ac648b00cb7c6684a3e64bee855b0320c7eb0f62b757b29d5fb6745560
1489fe0065c6531b60fda87a3857d7da1cd21873868856f058c20706f927fa08
O=C(Oc1ccccc1)c1ccccc1
O-[C;H0;D3;+0:1](=[O;D1;H0:2])-[c:3](:[c:4]):[c:5].[OH;D1;+0:6]-[c:7](:[c:8]):[c:9]>>[O;D1;H0:2]=[C;H0;D3;+0:1](-[O;H0;D2;+0:6]-[c:7](:[c:8]):[c:9])-[c:3](:[c:4]):[c:5]
null
[]
null
null
15
HOUR
0.1 mol of 4-hexyloxybenzoic acid, 0.01 mol of dimethylaminopyridine and 0.1 mol of 2,3-difluoro-4octyloxyphenol (preparable from 2,3-difluorooctyloxybenzene by lithiation at -70° to -80° and dropwise addition of a solution of lithium t-butylperoxide in ether prepared from 0.12 mol of t-butyl hydroperoxide and 0.12 mol...
10.6084/m9.figshare.5104873.v1
null
Carboxylic acid.Aromatic alcohol
Ester
null
null
c1ccccc1.c1ccccc1
HO-
ClCCl.CCOCC
null
15
CCCCCCCCOc1ccc(O)c(F)c1F.CCCCCCOc1ccc(C(=O)O)cc1>ClCCl.CCOCC>CCCCCCCCOc1ccc(OC(=O)c2ccc(OCCCCCC)cc2)c(F)c1F
ord_dataset-02ee2261663048188cf6d85d2cc96e3f
ord-709fc48404a84ef09737b5887db2472e
CCCCBr.CCCCC[C@@H]1CC[C@@H](COc2ccc(O)c(F)c2F)CC1>>CCCCC[C@@H]1CC[C@@H](COc2ccc(OCCCC)c(F)c2F)CC1
FC1=C(C=CC(=C1F)OC[C@@H]1CC[C@H](CC1)CCCCC)O.C(CCC)Br.C([O-])([O-])=O.[K+].[K+]>>C(CCC)OC1=C(C(=C(C=C1)OC[C@@H]1CC[C@H](CC1)CCCCC)F)F
Br[CH2:17][CH2:18][CH2:19][CH3:20].[CH3:1][CH2:2][CH2:3][CH2:4][CH2:5][C@H:6]1[CH2:7][CH2:8][C@H:9]([CH2:10][O:11][c:12]2[cH:13][cH:14][c:15]([OH:16])[c:21]([F:22])[c:23]2[F:24])[CH2:25][CH2:26]1>>[CH3:1][CH2:2][CH2:3][CH2:4][CH2:5][C@H:6]1[CH2:7][CH2:8][C@H:9]([CH2:10][O:11][c:12]2[cH:13][cH:14][c:15]([O:16][CH2:17][C...
CCCCBr.CCCCC[C@@H]1CC[C@@H](COc2ccc(O)c(F)c2F)CC1
CCCCC[C@@H]1CC[C@@H](COc2ccc(OCCCC)c(F)c2F)CC1
null
null
CN(C=O)C
Heteroatom Alkylation and Arylation
Williamson Ether Synthesis
7e1040116e3a4cf0e8ec5cc7865388d9cd0efabce6d320a1c25a36e411018d8b
d5f4610d46ccc0478471c5bc0fb862644eaf764bbc5d93badb39d54f6ec8e0a5
c1ccc(OCC2CCCCC2)cc1
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]
null
[]
null
null
null
null
0.1 mol of 2,3-difluoro-4-(trans-4-pentylcyclohexyl)methoxyphenol, 0.11 mol of butyl bromide and 0.11 mol of potassium carbonate are heated for 16 hours at 100° in 100 ml of dimethylformamide (DMF). After cooling, the inorganic salts are filtered off with suction, the filtrate is concentrated, and water is added. 1-but...
10.6084/m9.figshare.5104873.v1
null
Primary halide.Aromatic alcohol
Ether
null
null
C1CCCCC1.c1ccccc1
HBr
CN(C=O)C
null
null
CCCCBr.CCCCC[C@@H]1CC[C@@H](COc2ccc(O)c(F)c2F)CC1>CN(C=O)C>CCCCC[C@@H]1CC[C@@H](COc2ccc(OCCCC)c(F)c2F)CC1
ord_dataset-02ee2261663048188cf6d85d2cc96e3f
ord-32048f4b38654a34b265cba539771b47
Oc1cccc(F)c1F>>Oc1ccc(O)c(F)c1F
Cl.Cl.S(=O)([O-])[O-].[Na+].[Na+].[K].FC1=C(C=CC=C1F)O>>FC1=C(O)C=CC(=C1F)O
[OH:1][c:2]1[cH:3][cH:4][cH:5][c:7]([F:8])[c:9]1[F:10]>>[OH:1][c:2]1[cH:3][cH:4][c:5]([OH:6])[c:7]([F:8])[c:9]1[F:10]
Oc1cccc(F)c1F
Oc1ccc(O)c(F)c1F
null
null
[OH-].[Na+].C1(=CC=CC=C1)C
Oxidation
Aromatic hydroxylation
c7a66b348b8d881dd8ffccfacfb6192a695c6fe0c779e1e37631ad4085fe4603
ac85d33a723c7a3c15eece7d0a6d9fb901e902291e4984dab36fdac38eba9375
c1ccccc1
[F;D1;H0:1]-[c:2](:[c:3]):[cH;D2;+0:4]:[c:5]:[c:6]>>[F;D1;H0:1]-[c:2](:[c:3]):[c;H0;D3;+0:4](-[O;D1;H1:7]):[c:5]:[c:6]
null
[]
null
null
8
HOUR
1 mol of 2,3-difluorophenol is dissolved in 1 l of 10% sodium hydroxide solution, and a saturated aqueous solution of 1.1 mol of potassium peroxodisulphate is added dropwise over the course of 4 hours with ice cooling. During this addition, the temperature must not exceed 20o The mixture is stirred overnight at room te...
10.6084/m9.figshare.5104873.v1
null
null
Aromatic alcohol
c1ccccc1
c1ccccc1
c1ccccc1
Other
[OH-].[Na+].C1(=CC=CC=C1)C
null
8
Oc1cccc(F)c1F>[OH-].[Na+].C1(=CC=CC=C1)C>Oc1ccc(O)c(F)c1F
ord_dataset-02ee2261663048188cf6d85d2cc96e3f
ord-6ee06cc338d74b2ebea19761b8727ee9
COC(=O)CCCCC(=O)ON1C(=O)CCC1=O>>O=C(O)CCCCC(=O)ON1C(=O)CCC1=O
C(CCCCC(=O)ON1C(CCC1=O)=O)(=O)OC.Cl[Si](C)(C)C.[I-].[Na+]>>C1(CCC(N1OC(CCCCC(=O)O)=O)=O)=O
C[O:3][C:2](=[O:1])[CH2:4][CH2:5][CH2:6][CH2:7][C:8](=[O:9])[O:10][N:11]1[C:12](=[O:13])[CH2:14][CH2:15][C:16]1=[O:17]>>[O:1]=[C:2]([OH:3])[CH2:4][CH2:5][CH2:6][CH2:7][C:8](=[O:9])[O:10][N:11]1[C:12](=[O:13])[CH2:14][CH2:15][C:16]1=[O:17]
COC(=O)CCCCC(=O)ON1C(=O)CCC1=O
O=C(O)CCCCC(=O)ON1C(=O)CCC1=O
null
null
C(C)#N.C(C)(=O)OCC
Deprotection
Ester saponification (methyl deprotection)
d872e08ad5c85a4add6cd04e6e987e73fead5f79b3f30ba61a81ba5029b29894
38ae1ee78433b9acfb0390501446149c80f88f23ac2d84c60b3369bdab75cec9
O=C1CCC(=O)N1
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]
75.2
[{"value": 71.0, "product": "C1(CCC(N1OC(CCCCC(=O)O)=O)=O)=O", "details": "PERCENTYIELD", "is_desired": false}, {"value": 75.2, "product": "C1(CCC(N1OC(CCCCC(=O)O)=O)=O)=O", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
null
null
A solution of methyl succinimidyl adipate (4.5 g, 17.5 mmol), chlorotrimethylsilane (11.1 ml, 87.5 mmol) and sodium iodide (13.1 g, 87.5 mmol) in 10 ml of acetonitrile was heated at reflux for 12 hours. The mixture was then cooled to room temperature and diluted with ethyl acetate. The reaction mixture was washed repea...
10.6084/m9.figshare.5104873.v1
null
Ester
Carboxylic acid
null
null
C1CC[NH]C1
Other
C(C)#N.C(C)(=O)OCC
null
null
COC(=O)CCCCC(=O)ON1C(=O)CCC1=O>C(C)#N.C(C)(=O)OCC>O=C(O)CCCCC(=O)ON1C(=O)CCC1=O
ord_dataset-02ee2261663048188cf6d85d2cc96e3f
ord-1ed7b4f414b94a45a886575dff6a9247
O=C1CCC(=O)N1O.O=C1CCCC(=O)O1>>O=C(O)CCCC(=O)O.O=C1CCC(=O)N1O
Cl.C1(CCCC(=O)O1)=O.ON1C(CCC1=O)=O.C(C)N(CC)CC>>C(CCCC(=O)O)(=O)O.ON1C(CCC1=O)=O
[O:3]=[C:14]1[CH2:13][CH2:12][C:11](=[O:10])[N:16]1[OH:17].[O:1]=[C:2]1[CH2:4][CH2:5][CH2:6][C:7](=[O:8])[O:9]1>>[O:1]=[C:2]([OH:3])[CH2:4][CH2:5][CH2:6][C:7](=[O:8])[OH:9].[O:10]=[C:11]1[CH2:12][CH2:13][C:14](=[O:15])[N:16]1[OH:17]
O=C1CCC(=O)N1O.O=C1CCCC(=O)O1
O=C(O)CCCC(=O)O.O=C1CCC(=O)N1O
null
null
ClCCl
Functional Group Addition
OtherReaction
9788dff2a98060b369bf714f8584edc4415267d343a63106d8d813b535989e56
1376c454abf78648dfe038ea03fdaa7b24a002c84c34f33b09fae83b7b2b4302
O=C1CCC(=O)N1
[O;D1;H0:1]=[C;H0;D3;+0:2]1-[C:3]-[C:4]-[C:5]-[C:6](=[O;D1;H0:7])-[O;H0;D2;+0:8]-1.[O;D1;H0:9]=[C:10]1-[C:11]-[C:12]-[C;H0;D3;+0:13](=[O;H0;D1;+0:14])-[#7:15]-1-[O;D1;H1:16]>>[O;D1;H0:1]=[C;H0;D3;+0:2](-[OH;D1;+0:14])-[C:3]-[C:4]-[C:5]-[C:6](=[O;D1;H0:7])-[OH;D1;+0:8].[O;D1;H0:9]=[C:10]1-[C:11]-[C:12]-[C;H0;D3;+0:13](=...
null
[]
null
null
40
MINUTE
One mole of glutaric anhydride and one mole of N-hydroxysuccinimide were treated in dichloromethane with 1.2 equivalents of triethylamine. This reaction was stirred for 40 minutes, acidified by the addition of 0.5N hydrochloric acid (HCl) (aqueous), and then extracted with ethyl acetate to form mono N-hydroxysuccinimid...
10.6084/m9.figshare.5104873.v1
null
Anhydride.Tertiary amide
Carboxylic acid.Carboxylic acid.Tertiary amide
C1CC[NH]C1.C1CCOCC1
C1CC[NH]C1
C1CC[NH]C1
Other
ClCCl
null
0.666667
O=C1CCC(=O)N1O.O=C1CCCC(=O)O1>ClCCl>O=C(O)CCCC(=O)O.O=C1CCC(=O)N1O
ord_dataset-02ee2261663048188cf6d85d2cc96e3f
ord-e5f02821feab4e68bc5f37db01f810ce
O=P1(Oc2ccccc2)CCCC(CI)O1.[N-]=[N+]=[N-]>>[N-]=[N+]=NCC1CCCP(=O)(Oc2ccccc2)O1
[N-]=[N+]=[N-].[Na+].O(C1=CC=CC=C1)P1(OC(CCC1)CI)=O>>O(C1=CC=CC=C1)P1(OC(CCC1)CN=[N+]=[N-])=O
I[CH2:4][CH:5]1[CH2:6][CH2:7][CH2:8][P:9](=[O:10])([O:11][c:12]2[cH:13][cH:14][cH:15][cH:16][cH:17]2)[O:18]1.[N-:1]=[N+:2]=[N-:3]>>[N-:1]=[N+:2]=[N:3][CH2:4][CH:5]1[CH2:6][CH2:7][CH2:8][P:9](=[O:10])([O:11][c:12]2[cH:13][cH:14][cH:15][cH:16][cH:17]2)[O:18]1
O=P1(Oc2ccccc2)CCCC(CI)O1.[N-]=[N+]=[N-]
[N-]=[N+]=NCC1CCCP(=O)(Oc2ccccc2)O1
null
[Br-].C(CCC)[N+](CCCC)(CCCC)CCCC
C1=CC=CC=C1.CN(C)C=O
Heteroatom Alkylation and Arylation
OtherReaction
4b07a4c2a14d792a37e78a751619e60b15c60cbff0bebae1109754fb52d84cbb
2d41632f7225d65cdc2ad8562dfb28f3f5a017f92040ed4ccafbb8154954c8fe
O=P1(Oc2ccccc2)CCCCO1
I-[CH2;D2;+0:1]-[C:2](-[C:3])-[#8:4]-[#15:5].[N-;H0;D1:6]=[#7;+:7]=[N;-;D1;H0:8]>>[#15:5]-[#8:4]-[C:2](-[CH2;D2;+0:1]-[N;H0;D2;+0:6]=[#7;+:7]=[N;-;D1;H0:8])-[C:3]
96
[{"value": 96.0, "product": "O(C1=CC=CC=C1)P1(OC(CCC1)CN=[N+]=[N-])=O", "details": "PERCENTYIELD", "is_desired": false}]
null
null
null
null
A suspension containing two equivalents of sodium azide, one equivalent of the above-prepared iodonated oxaphosphorinane and a catalytic amount of about 0.1 equivalent of tetrabutylammonium bromide in benzene/DMF (1:1) was heated to 60-80 degrees C. for 16 hours to produce 2-phenoxy-2-oxo-6-(azidomethyl)-1,2-oxaphospho...
10.6084/m9.figshare.5104873.v1
null
Primary halide
Azide
null
null
C1CC[P]OC1.c1ccccc1
I-
[Br-].C(CCC)[N+](CCCC)(CCCC)CCCC.C1=CC=CC=C1.CN(C)C=O
null
null
O=P1(Oc2ccccc2)CCCC(CI)O1.[N-]=[N+]=[N-]>[Br-].C(CCC)[N+](CCCC)(CCCC)CCCC.C1=CC=CC=C1.CN(C)C=O>[N-]=[N+]=NCC1CCCP(=O)(Oc2ccccc2)O1
ord_dataset-02ee2261663048188cf6d85d2cc96e3f
ord-722703b0bdef43369d32d6d5d22467c1
CCOP(=O)(CCC(C)=O)OCC.Cn1cncn1>>CCOP(=O)(CCC(C)(O)c1ncnn1C)OCC
CN1N=CN=C1.O=C(CCP(OCC)(OCC)=O)C>>OC(CCP(OCC)(OCC)=O)(C1=NC=NN1C)C
[CH3:1][CH2:2][O:3][P:4](=[O:5])([CH2:6][CH2:7][C:8]([CH3:9])=[O:10])[O:17][CH2:18][CH3:19].[cH:11]1[n:12][cH:13][n:14][n:15]1[CH3:16]>>[CH3:1][CH2:2][O:3][P:4](=[O:5])([CH2:6][CH2:7][C:8]([CH3:9])([OH:10])[c:11]1[n:12][cH:13][n:14][n:15]1[CH3:16])[O:17][CH2:18][CH3:19]
CCOP(=O)(CCC(C)=O)OCC.Cn1cncn1
CCOP(=O)(CCC(C)(O)c1ncnn1C)OCC
null
null
O1CCCC1
C-C Coupling
OtherReaction
03bf5a0330805602a21b72eff83b38685dda6b1b4723d3339e24164dfe8e144b
454f67ba8644982dc9f605915a0f36178771eadaffb50d3f1e0f17f2b6fdeb10
c1nc[nH]n1
[C;D1;H3:1]-[#7;a:2]1:[#7;a:3]:[c:4]:[#7;a:5]:[cH;D2;+0:6]:1.[C:7]-[C:8]-[C;H0;D3;+0:9](-[C;D1;H3:10])=[O;H0;D1;+0:11]>>[C:7]-[C:8]-[C;H0;D4;+0:9](-[C;D1;H3:10])(-[OH;D1;+0:11])-[c;H0;D3;+0:6]1:[#7;a:5]:[c:4]:[#7;a:3]:[#7;a:2]:1-[C;D1;H3:1]
28.4
[{"value": 28.0, "product": "OC(CCP(OCC)(OCC)=O)(C1=NC=NN1C)C", "details": "PERCENTYIELD", "is_desired": false}, {"value": 28.4, "product": "OC(CCP(OCC)(OCC)=O)(C1=NC=NN1C)C", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
1
HOUR
To a solution of 1-methyl-1,2,4-triazole (3.0 g, 36.1 mmol) in tetrahydrofurane (60 ml) was added n-buthyllithium (43.3 mmol, 1.2 eq) at -78° C. under nitrogen. The mixture was stirred for 1 hour, then diethyl 3-oxo-butylphosphonate (8.3 g, 39.7 mmol, 1.1 eq) was added. The mixture was stirred for 2 hours and quenched ...
10.6084/m9.figshare.5104873.v1
null
Ketone
Tertiary alcohol
c1nnc[nH]1
c1nnc[nH]1
c1nnc[nH]1
null
O1CCCC1
null
1
CCOP(=O)(CCC(C)=O)OCC.Cn1cncn1>O1CCCC1>CCOP(=O)(CCC(C)(O)c1ncnn1C)OCC
ord_dataset-02ee2261663048188cf6d85d2cc96e3f
ord-3ce26230d98c428aa71701a3a4059bb1
CCOP(=O)(CCC(C)(O)c1ncnn1C)OCC>>Cn1ncnc1C(C)(O)CCP(=O)(O)O
CO.OC(CCP(OCC)(OCC)=O)(C1=NC=NN1C)C.C[Si](C)(C)Br.C1C(C)O1>>OC(CCP(O)(O)=O)(C1=NC=NN1C)C
CC[O:14][P:12]([CH2:11][CH2:10][C:7]([c:6]1[n:2]([CH3:1])[n:3][cH:4][n:5]1)([CH3:8])[OH:9])(=[O:13])[O:15]CC>>[CH3:1][n:2]1[n:3][cH:4][n:5][c:6]1[C:7]([CH3:8])([OH:9])[CH2:10][CH2:11][P:12](=[O:13])([OH:14])[OH:15]
CCOP(=O)(CCC(C)(O)c1ncnn1C)OCC
Cn1ncnc1C(C)(O)CCP(=O)(O)O
null
null
C(Cl)Cl.C(C)OCC
Deprotection
OtherReaction
eaaf8436ac19e7e26db9ff78e61eed5caf13b9167196c3230a9e1eb66b295f8b
30a26bc929988d0041b9998cdccd1d65eb125114a78065ed35d40f50c965c0a7
c1nc[nH]n1
C-C-[O;H0;D2;+0:1]-[#15:2](-[C:3])(=[O;D1;H0:4])-[O;H0;D2;+0:5]-C-C>>[C:3]-[#15:2](=[O;D1;H0:4])(-[OH;D1;+0:1])-[OH;D1;+0:5]
65
[{"value": 65.0, "product": null, "details": "PERCENTYIELD", "is_desired": false}]
null
null
16
HOUR
To a solution of diethyl 3-hydroxy-3-methyl-3-(1-methyl-1,2,4-triazol-5-yl)propylphosphonate (1.2 g, 4.12 mmol) in CH2Cl2 (24 ml) was added TMSBr (2.72 ml, 20.6 mmol, 5 eq) at room temperature under nitrogen. The reaction mixture was stirred for 16 hours. Then methanol (12 ml) was added to the mixture. After stirring f...
10.6084/m9.figshare.5104873.v1
null
null
null
null
null
c1ncn[nH]1
Other
C(Cl)Cl.C(C)OCC
null
16
CCOP(=O)(CCC(C)(O)c1ncnn1C)OCC>C(Cl)Cl.C(C)OCC>Cn1ncnc1C(C)(O)CCP(=O)(O)O
ord_dataset-02ee2261663048188cf6d85d2cc96e3f
ord-52a1540eb16c4bf9bce3f0fea0589617
COCCOCOc1c(C(C)(C)C)nc(CC(O)c2cccnc2)nc1C(C)(C)C>>CC(C)(C)c1nc(C=Cc2cccnc2)nc(C(C)(C)C)c1O
CC(C)(C)C1=NC(=NC(=C1OCOCCOC)C(C)(C)C)CC(O)C=1C=NC=CC1.C(C)(=O)[O-].[Na+].C(C)(=O)OC(C)=O>>CC(C)(C)C1=NC(=NC(=C1O)C(C)(C)C)C=CC=1C=NC=CC1
COCCOC[O:23][c:22]1[c:5]([C:2]([CH3:1])([CH3:3])[CH3:4])[n:6][c:7]([CH2:8][CH:9](O)[c:10]2[cH:11][cH:12][cH:13][n:14][cH:15]2)[n:16][c:17]1[C:18]([CH3:19])([CH3:20])[CH3:21]>>[CH3:1][C:2]([CH3:3])([CH3:4])[c:5]1[n:6][c:7]([CH:8]=[CH:9][c:10]2[cH:11][cH:12][cH:13][n:14][cH:15]2)[n:16][c:17]([C:18]([CH3:19])([CH3:20])[CH...
COCCOCOc1c(C(C)(C)C)nc(CC(O)c2cccnc2)nc1C(C)(C)C
CC(C)(C)c1nc(C=Cc2cccnc2)nc(C(C)(C)C)c1O
null
null
C1(=CC=CC=C1)C
Functional Group Interconversion
OtherReaction
3ccc784524ce127fa6d3f650df3c3c4b6f3f837eae77b44298f6abb14acc1f54
c8923c733b00c09c1c92f840cc716f59d71fd45875244f4527080cb33a30e6d8
C(=Cc1ncccn1)c1cccnc1
C-O-C-C-O-C-[O;H0;D2;+0:1]-[c:2]1:[c:3](-[C:4]):[#7;a:5]:[c:6](-[CH2;D2;+0:7]-[CH;D3;+0:8](-O)-[c:9](:[c:10]):[c:11]:[#7;a:12]:[c:13]):[#7;a:14]:[c:15]:1-[C:16]>>[C:4]-[c:3]1:[#7;a:5]:[c:6](-[CH;D2;+0:7]=[CH;D2;+0:8]-[c:9](:[c:10]):[c:11]:[#7;a:12]:[c:13]):[#7;a:14]:[c:15](-[C:16]):[c:2]:1-[OH;D1;+0:1]
49.8
[{"value": 40.0, "product": "CC(C)(C)C1=NC(=NC(=C1O)C(C)(C)C)C=CC=1C=NC=CC1", "details": "PERCENTYIELD", "is_desired": false}, {"value": 49.8, "product": "CC(C)(C)C1=NC(=NC(=C1O)C(C)(C)C)C=CC=1C=NC=CC1", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
190
CELSIUS
null
null
A mixture of 4,6-bis(1,1-dimethylethyl)-5-[(2-methoxyethoxy)methoxy]-α-(3 -pyridinyl)-2-pyrimidineethanol (350 mg), sodium acetate (10 g) and acetic anhydride (7 mL) in toluene (100 mL) is heated at reflux for 8 hours. The reaction mixture is cooled and the solvent is evaporated. Dichlorobenzene (30 mL) is added and th...
10.6084/m9.figshare.5104873.v1
null
Ether.Ether.Ether.Secondary alcohol
Aromatic alcohol
null
null
c1cncnc1.c1ccncc1
HO-
C1(=CC=CC=C1)C
190
null
COCCOCOc1c(C(C)(C)C)nc(CC(O)c2cccnc2)nc1C(C)(C)C>C1(=CC=CC=C1)C>CC(C)(C)c1nc(C=Cc2cccnc2)nc(C(C)(C)C)c1O
ord_dataset-02ee2261663048188cf6d85d2cc96e3f
ord-edc7f325608347ef9c24c27f7f1bcf0b
CC(=O)OC(C(=O)C(C)(C)C)C(=O)C(C)(C)C.[NH4+]>>Cc1nc(C(C)(C)C)c(C(=O)C(C)(C)C)o1
C(C)(=O)OC(C(C(C)(C)C)=O)C(C(C)(C)C)=O.C(C)(=O)[O-].[NH4+]>>CC(C)(C)C=1N=C(OC1C(C(C)(C)C)=O)C
O=[C:2]([CH3:1])[O:16][CH:9]([C:4](=O)[C:5]([CH3:6])([CH3:7])[CH3:8])[C:10](=[O:11])[C:12]([CH3:13])([CH3:14])[CH3:15].[NH4+:3]>>[CH3:1][c:2]1[n:3][c:4]([C:5]([CH3:6])([CH3:7])[CH3:8])[c:9]([C:10](=[O:11])[C:12]([CH3:13])([CH3:14])[CH3:15])[o:16]1
CC(=O)OC(C(=O)C(C)(C)C)C(=O)C(C)(C)C.[NH4+]
Cc1nc(C(C)(C)C)c(C(=O)C(C)(C)C)o1
null
null
C(C)(=O)O.[OH-].[Na+].O
Aromatic Heterocycle Formation
OtherReaction
513d6dc05be315534012c4ee040873e6fa4aee581b54c11940793fd4174b356e
d0e9f772275cfdec8d5b1c1cabb0557f331ce07d5a2ae2cab05542daef89be5d
c1cocn1
O=[C;H0;D3;+0:1](-[C;D1;H3:2])-[O;H0;D2;+0:3]-[CH;D3;+0:4](-[C:5](-[C:6])=[O;D1;H0:7])-[C;H0;D3;+0:8](=O)-[C:9](-[C;D1;H3:10])(-[C;D1;H3:11])-[C;D1;H3:12].[NH4+;D0:13]>>[C:6]-[C:5](=[O;D1;H0:7])-[c;H0;D3;+0:4]1:[o;H0;D2;+0:3]:[c;H0;D3;+0:1](-[C;D1;H3:2]):[n;H0;D2;+0:13]:[c;H0;D3;+0:8]:1-[C:9](-[C;D1;H3:10])(-[C;D1;H3:1...
92.5
[{"value": 91.0, "product": "CC(C)(C)C=1N=C(OC1C(C(C)(C)C)=O)C", "details": "PERCENTYIELD", "is_desired": false}, {"value": 92.5, "product": "CC(C)(C)C=1N=C(OC1C(C(C)(C)C)=O)C", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
null
null
A solution of 4-(acetyloxy)-2,2,6,6-tetramethyl 3,5 heptanedione (22 g, 0.09 mol) in acetic acid (100 mL) is treated with ammonium acetate (44 g). The reaction mixture is heated at reflux overnight. The reaction mixture is diluted with water and neutralized (to pH 5) by the addition of aqueous sodium hydroxide. The pro...
10.6084/m9.figshare.5104873.v1
null
Ketone.Ketone.Ester
Ketone
null
c1cocn1
c1cocn1
HO-
C(C)(=O)O.[OH-].[Na+].O
null
null
CC(=O)OC(C(=O)C(C)(C)C)C(=O)C(C)(C)C.[NH4+]>C(C)(=O)O.[OH-].[Na+].O>Cc1nc(C(C)(C)C)c(C(=O)C(C)(C)C)o1
ord_dataset-02ee2261663048188cf6d85d2cc96e3f
ord-c60e5ad8c697434fa67dd662437ae58d
Cc1nc(C(C)(C)C)c(C(=O)C(C)(C)C)o1.[NH4+]>>Cc1nc(C(C)(C)C)c(O)c(C(C)(C)C)n1
CC(C)(C)C=1N=C(OC1C(C(C)(C)C)=O)C.[OH-].[NH4+]>>CC(C)(C)C1=NC(=NC(=C1O)C(C)(C)C)C
O=[C:11]([c:9]1[c:4]([C:5]([CH3:6])([CH3:7])[CH3:8])[n:16][c:2]([CH3:1])[o:10]1)[C:12]([CH3:13])([CH3:14])[CH3:15].[NH4+:3]>>[CH3:1][c:2]1[n:3][c:4]([C:5]([CH3:6])([CH3:7])[CH3:8])[c:9]([OH:10])[c:11]([C:12]([CH3:13])([CH3:14])[CH3:15])[n:16]1
Cc1nc(C(C)(C)C)c(C(=O)C(C)(C)C)o1.[NH4+]
Cc1nc(C(C)(C)C)c(O)c(C(C)(C)C)n1
null
null
null
Functional Group Interconversion
OtherReaction
2de4a4cfe89cbfa88f952fe89cdb000b1990949ca6496c79a95865617e4875da
f0f6c0aea42e131fa87fd5383e2df959f9ded0709f604973ae337694df8652bd
c1cncnc1
O=[C;H0;D3;+0:1](-[c:2]1:[o;H0;D2;+0:3]:[c;H0;D3;+0:4](-[C;D1;H3:5]):[n;H0;D2;+0:6]:[c;H0;D3;+0:7]:1-[C:8](-[C;D1;H3:9])(-[C;D1;H3:10])-[C;D1;H3:11])-[C:12](-[C;D1;H3:13])(-[C;D1;H3:14])-[C;D1;H3:15].[NH4+;D0:16]>>[C;D1;H3:13]-[C:12](-[C;D1;H3:14])(-[C;D1;H3:15])-[c;H0;D3;+0:1]1:[n;H0;D2;+0:6]:[c;H0;D3;+0:4](-[C;D1;H3:...
75
[{"value": 75.0, "product": "CC(C)(C)C1=NC(=NC(=C1O)C(C)(C)C)C", "details": "PERCENTYIELD", "is_desired": false}]
null
null
null
null
A mixture of 1-[4-(1,1-dimethylethyl)-2 methyl-5-oxazolyl]-2,2-dimethyl-1 propanone (8.5 g, 38 mmol) and concentrated ammonium hydroxide (100 mL) is heated at 180° C. for 36 hours in a steel bomb. The reaction mixture is cooled and the excess ammonia is evaporated on the rotovap. The pH of the resulting mixture is adju...
10.6084/m9.figshare.5104873.v1
null
Ketone
Aromatic alcohol
c1cocn1
c1cncnc1
c1cncnc1
HO-
null
null
null
Cc1nc(C(C)(C)C)c(C(=O)C(C)(C)C)o1.[NH4+]>>Cc1nc(C(C)(C)C)c(O)c(C(C)(C)C)n1
ord_dataset-02ee2261663048188cf6d85d2cc96e3f
ord-9502ecdb7f4d41659d2e170dd6a9e06b
COCCOCCl.Cc1nc(C(C)(C)C)c(O)c(C(C)(C)C)n1>>COCCOCOc1c(C(C)(C)C)nc(C)nc1C(C)(C)C
CC(C)(C)C1=NC(=NC(=C1O)C(C)(C)C)C.[H-].[Na+].COCCOCCl>>CC(C)(C)C1=NC(=NC(=C1OCOCCOC)C(C)(C)C)C
Cl[CH2:6][O:5][CH2:4][CH2:3][O:2][CH3:1].[OH:7][c:8]1[c:9]([C:10]([CH3:11])([CH3:12])[CH3:13])[n:14][c:15]([CH3:16])[n:17][c:18]1[C:19]([CH3:20])([CH3:21])[CH3:22]>>[CH3:1][O:2][CH2:3][CH2:4][O:5][CH2:6][O:7][c:8]1[c:9]([C:10]([CH3:11])([CH3:12])[CH3:13])[n:14][c:15]([CH3:16])[n:17][c:18]1[C:19]([CH3:20])([CH3:21])[CH3...
COCCOCCl.Cc1nc(C(C)(C)C)c(O)c(C(C)(C)C)n1
COCCOCOc1c(C(C)(C)C)nc(C)nc1C(C)(C)C
null
null
C1CCOC1.O1CCCC1
Heteroatom Alkylation and Arylation
Williamson Ether Synthesis
6e90ffbf0683e1a3ee55c5e3ea453aefc5ddd369c0150ed0150f9546d7e47f4f
efd670663709b79afcad1306da9f69b33a0147cfa3639ca4c0b54b35ef4b1852
c1cncnc1
Cl-[CH2;D2;+0:1]-[#8:2]-[C:3].[C:4]-[c:5]1:[#7;a:6]:[c:7]:[#7;a:8]:[c:9](-[C:10]):[c:11]:1-[OH;D1;+0:12]>>[C:4]-[c:5]1:[#7;a:6]:[c:7]:[#7;a:8]:[c:9](-[C:10]):[c:11]:1-[O;H0;D2;+0:12]-[CH2;D2;+0:1]-[#8:2]-[C:3]
null
[]
null
null
4
HOUR
4,6-Bis(1,1-dimethylethyl) 5 hydroxy-2-methyl pyrimidine (9.8 g, 44.1 mmoles) is dissolved in 100 mL of tetrahydrofuran and added dropwise to a suspension of sodium hydride (1.2 g, 48.5 mmoles) in THF (50 mL) at 0° C. The reaction mixture is warmed to room temperature over 15 minutes. 2-Methoxyethoxymethyl chloride (7....
10.6084/m9.figshare.5104873.v1
null
Primary halide.Ether.Aromatic alcohol
Ether.Ether
null
null
c1cncnc1
HCl
C1CCOC1.O1CCCC1
null
4
COCCOCCl.Cc1nc(C(C)(C)C)c(O)c(C(C)(C)C)n1>C1CCOC1.O1CCCC1>COCCOCOc1c(C(C)(C)C)nc(C)nc1C(C)(C)C
ord_dataset-02ee2261663048188cf6d85d2cc96e3f
ord-f8b7c078c1f34c738ce919fd25bc8ca3
COCCOCOc1c(C(C)(C)C)nc(C)nc1C(C)(C)C.O=Cc1cccnc1>>COCCOCOc1c(C(C)(C)C)nc(CC(O)c2cccnc2)nc1C(C)(C)C
N1=CC(=CC=C1)C=O.C(CCC)[Li].CC(C)(C)C1=NC(=NC(=C1OCOCCOC)C(C)(C)C)C>>CC(C)(C)C1=NC(=NC(=C1OCOCCOC)C(C)(C)C)CC(O)C=1C=NC=CC1
[CH3:1][O:2][CH2:3][CH2:4][O:5][CH2:6][O:7][c:8]1[c:9]([C:10]([CH3:11])([CH3:12])[CH3:13])[n:14][c:15]([CH3:16])[n:25][c:26]1[C:27]([CH3:28])([CH3:29])[CH3:30].[CH:17](=[O:18])[c:19]1[cH:20][cH:21][cH:22][n:23][cH:24]1>>[CH3:1][O:2][CH2:3][CH2:4][O:5][CH2:6][O:7][c:8]1[c:9]([C:10]([CH3:11])([CH3:12])[CH3:13])[n:14][c:1...
COCCOCOc1c(C(C)(C)C)nc(C)nc1C(C)(C)C.O=Cc1cccnc1
COCCOCOc1c(C(C)(C)C)nc(CC(O)c2cccnc2)nc1C(C)(C)C
null
null
C1CCOC1
C-C Coupling
OtherReaction
995c7a5cbf37230035b00de18cd91aae550f6b3916b2678b4c13427cfa9d9370
a7cae52d902b2812376f5459a7a8b7ead54e8ef31fd78982d2e99bec532613ba
c1cnc(CCc2cccnc2)nc1
[CH3;D1;+0:1]-[c:2](:[#7;a:3]:[c:4]):[#7;a:5]:[c:6].[O;H0;D1;+0:7]=[CH;D2;+0:8]-[c:9](:[c:10]):[c:11]:[#7;a:12]:[c:13]>>[OH;D1;+0:7]-[CH;D3;+0:8](-[CH2;D2;+0:1]-[c:2](:[#7;a:3]:[c:4]):[#7;a:5]:[c:6])-[c:9](:[c:10]):[c:11]:[#7;a:12]:[c:13]
50
[{"value": 50.0, "product": "CC(C)(C)C1=NC(=NC(=C1OCOCCOC)C(C)(C)C)CC(O)C=1C=NC=CC1", "details": "PERCENTYIELD", "is_desired": false}, {"value": 49.9, "product": "CC(C)(C)C1=NC(=NC(=C1OCOCCOC)C(C)(C)C)CC(O)C=1C=NC=CC1", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
30
MINUTE
n-Butyllithium (1.5 mL of 1.6M solution in hexane, 2.4 mmol) is added dropwise to a solution of 4,6-bis(1,1-dimethylethyl)-5-[(2-methoxyethoxy)methoxy]-2-methylpyrimidine (750 mg, 2.4 mmol) in dry THF (12 mL) at 0° C. under an atmosphere of dry nitrogen. The reaction mixture is stirred at room temperature for 30 minute...
10.6084/m9.figshare.5104873.v1
null
Aldehyde
Secondary alcohol
null
null
c1cncnc1.c1ccncc1
null
C1CCOC1
null
0.5
COCCOCOc1c(C(C)(C)C)nc(C)nc1C(C)(C)C.O=Cc1cccnc1>C1CCOC1>COCCOCOc1c(C(C)(C)C)nc(CC(O)c2cccnc2)nc1C(C)(C)C
ord_dataset-02ee2261663048188cf6d85d2cc96e3f
ord-5e13a4705a5441f1b9a49bbde17a9f3c
Br.Nc1nc2cc(Cl)c(Cl)cc2[nH]1>>Clc1cc2nc(Br)[nH]c2cc1Cl
NC=1NC2=C(N1)C=C(C(=C2)Cl)Cl.Br.N(=O)[O-].[Na+]>>BrC=1NC2=C(N1)C=C(C(=C2)Cl)Cl
[BrH:7].N[c:6]1[n:5][c:4]2[cH:3][c:2]([Cl:1])[c:11]([Cl:12])[cH:10][c:9]2[nH:8]1>>[Cl:1][c:2]1[cH:3][c:4]2[n:5][c:6]([Br:7])[nH:8][c:9]2[cH:10][c:11]1[Cl:12]
Br.Nc1nc2cc(Cl)c(Cl)cc2[nH]1
Clc1cc2nc(Br)[nH]c2cc1Cl
null
null
O
Miscellaneous
OtherReaction
857c8f1e64ccd27863105cbe22e92e556631542f0a4a501417bddd8e9b7bc616
1129c10513c603d2647e51dd9713063aaf10bd8a364ed275b9b93c32624e3ba4
c1ccc2[nH]cnc2c1
N-[c;H0;D3;+0:1]1:[#7;a:2]:[c:3]:[c:4]:[#7;a:5]:1.[BrH;D0;+0:6]>>[Br;H0;D1;+0:6]-[c;H0;D3;+0:1]1:[#7;a:2]:[c:3]:[c:4]:[#7;a:5]:1
26
[{"value": 26.0, "product": "BrC=1NC2=C(N1)C=C(C(=C2)Cl)Cl", "details": "PERCENTYIELD", "is_desired": false}]
null
null
1
HOUR
2-Amino-5,6-dichlorobenzimidazole (3 g, 16 mmole) was suspended in 150 ml of water and brought into solution with 2 ml of HBr. Sodium nitrite (3.3 g, 55 mmole) was then added and the mixture was stirred at room temperature for 1 hr. Excess CuBr2 was then added and the mixture was heated on a steam bath for 1 hr. The aq...
10.6084/m9.figshare.5104873.v1
null
Primary amine
Aromatic halide
c1ccc2[nH]cnc2c1
c1ccc2[nH]cnc2c1
c1ccc2[nH]cnc2c1
Other
O
null
1
Br.Nc1nc2cc(Cl)c(Cl)cc2[nH]1>O>Clc1cc2nc(Br)[nH]c2cc1Cl
ord_dataset-02ee2261663048188cf6d85d2cc96e3f
ord-2ecad7da38b24e3d9a065c9be68c87c0
CC(=O)O[C@@H]1O[C@H](COC(=O)c2ccccc2)[C@@H](OC(=O)c2ccccc2)[C@H]1OC(=O)c1ccccc1.Clc1nc2cc(Cl)c(Cl)cc2[nH]1>>OC[C@H]1O[C@@H](n2c(Cl)nc3cc(Cl)c(Cl)cc32)[C@H](O)[C@@H]1O
FC(C(O[Si](C)(C)C)=N[Si](C)(C)C)(F)F.ClC=1NC2=C(N1)C=C(C(=C2)Cl)Cl.[Si](C)(C)(C)S(=O)(=O)C(F)(F)F.C(C)(=O)O[C@H]1[C@H](OC(C2=CC=CC=C2)=O)[C@H](OC(C2=CC=CC=C2)=O)[C@H](O1)COC(C1=CC=CC=C1)=O>>ClC1=NC2=C(N1[C@H]1[C@H](O)[C@H](O)[C@H](O1)CO)C=C(C(=C2)Cl)Cl
CC(=O)O[C@@H:5]1[O:4][C@H:3]([CH2:2][O:1]C(=O)c2ccccc2)[C@@H:20]([O:21]C(=O)c2ccccc2)[C@H:18]1[O:19]C(=O)c1ccccc1.[nH:6]1[c:7]([Cl:8])[n:9][c:10]2[cH:11][c:12]([Cl:13])[c:14]([Cl:15])[cH:16][c:17]12>>[OH:1][CH2:2][C@H:3]1[O:4][C@@H:5]([n:6]2[c:7]([Cl:8])[n:9][c:10]3[cH:11][c:12]([Cl:13])[c:14]([Cl:15])[cH:16][c:17]23)[...
CC(=O)O[C@@H]1O[C@H](COC(=O)c2ccccc2)[C@@H](OC(=O)c2ccccc2)[C@H]1OC(=O)c1ccccc1.Clc1nc2cc(Cl)c(Cl)cc2[nH]1
OC[C@H]1O[C@@H](n2c(Cl)nc3cc(Cl)c(Cl)cc32)[C@H](O)[C@@H]1O
null
null
C(C)#N
Heteroatom Alkylation and Arylation
OtherReaction
c642901dd79f8e49f810fd25b8a46c1aaa649572bdb579ffd97b77f2c228f59e
21d64cf2032d78ffc90699b40c7d706de3ba73747db98398625e977d93d000d4
c1ccc2c(c1)ncn2[C@H]1CCCO1
C-C(=O)-O-[C@@H;D3;+0:1]1-[#8:2]-[C:3](-[C:4]-[O;H0;D2;+0:5]-C(=O)-c2:c:c:c:c:c:2)-[C:6](-[O;H0;D2;+0:7]-C(=O)-c2:c:c:c:c:c:2)-[C:8]-1-[O;H0;D2;+0:9]-C(=O)-c1:c:c:c:c:c:1.[Cl;D1;H0:10]-[c:11]1:[#7;a:12]:[c:13](:[c:14]):[c:15](:[c:16]):[nH;D2;+0:17]:1>>[Cl;D1;H0:10]-[c:11]1:[#7;a:12]:[c:13](:[c:14]):[c:15](:[c:16]):[n;H...
null
[]
75
CELSIUS
45
MINUTE
2,5,6-Trichlorobenzimidazole (700 mg, 0.0032 moles) was dissolved in acetonitrile and BSTFA (1 ml, 0.0038 moles) was added. The mixture was heated at 75° C. for 20 minutes. TMSTf (1 ml, 0.0051 moles) and 1-O-acetyl-2,3,5-tri-O-benzoyl-β-D-ribofuranose (1.9 g, 0.0038 moles) were added while heating was continued for 45 ...
10.6084/m9.figshare.5104873.v1
null
Ester.Ester.Ester.Ester.Ether
Ether.Primary alcohol.Secondary alcohol.Secondary alcohol
C1CCOC1.c1ccccc1.c1ccccc1.c1ccccc1.c1ccc2[nH]cnc2c1
C1CCOC1.c1ccc2[nH]cnc2c1
C1CCOC1.c1ccc2[nH]cnc2c1
HO-
C(C)#N
75
0.75
CC(=O)O[C@@H]1O[C@H](COC(=O)c2ccccc2)[C@@H](OC(=O)c2ccccc2)[C@H]1OC(=O)c1ccccc1.Clc1nc2cc(Cl)c(Cl)cc2[nH]1>C(C)#N>OC[C@H]1O[C@@H](n2c(Cl)nc3cc(Cl)c(Cl)cc32)[C@H](O)[C@@H]1O
ord_dataset-02ee2261663048188cf6d85d2cc96e3f
ord-2985c0e734b84302990b58baa671a5d0
ClC1O[C@H](COCc2ccccc2)[C@@H](OCc2ccccc2)[C@H]1OCc1ccccc1.O=[N+]([O-])c1cc2nc(Cl)[nH]c2cc1[N+](=O)[O-]>>O=[N+]([O-])c1cc2nc(Cl)n([C@@H]3O[C@H](COCc4ccccc4)[C@@H](OCc4ccccc4)[C@H]3OCc3ccccc3)c2cc1[N+](=O)[O-]
ClC=1NC2=C(N1)C=C(C(=C2)[N+](=O)[O-])[N+](=O)[O-].C(C1=CC=CC=C1)O[C@H]1C(O[C@@H]([C@H]1OCC1=CC=CC=C1)COCC1=CC=CC=C1)Cl.[Si](C)(C)(C)OS(=O)(=O)C(F)(F)F>>ClC1=NC2=C(N1[C@H]1[C@H](OCC3=CC=CC=C3)[C@H](OCC3=CC=CC=C3)[C@H](O1)COCC1=CC=CC=C1)C=C(C(=C2)[N+](=O)[O-])[N+](=O)[O-]
Cl[CH:11]1[O:12][C@H:13]([CH2:14][O:15][CH2:16][c:17]2[cH:18][cH:19][cH:20][cH:21][cH:22]2)[C@@H:23]([O:24][CH2:25][c:26]2[cH:27][cH:28][cH:29][cH:30][cH:31]2)[C@H:32]1[O:33][CH2:34][c:35]1[cH:36][cH:37][cH:38][cH:39][cH:40]1.[O:1]=[N+:2]([O-:3])[c:4]1[cH:5][c:6]2[n:7][c:8]([Cl:9])[nH:10][c:41]2[cH:42][c:43]1[N+:44](=[...
ClC1O[C@H](COCc2ccccc2)[C@@H](OCc2ccccc2)[C@H]1OCc1ccccc1.O=[N+]([O-])c1cc2nc(Cl)[nH]c2cc1[N+](=O)[O-]
O=[N+]([O-])c1cc2nc(Cl)n([C@@H]3O[C@H](COCc4ccccc4)[C@@H](OCc4ccccc4)[C@H]3OCc3ccccc3)c2cc1[N+](=O)[O-]
null
null
CC#N.CCOC(=O)C
Heteroatom Alkylation and Arylation
N-alkylation of secondary amines with alkyl halides
6c291171bb6e4032d543e33eca92380ebcd07cbb2d3668ca761f05e7d5702513
dfebb98912d1cf9ca9bea5f0eb687cda9773eb2f7ac7378282049e4233a1d769
c1ccc(COC[C@H]2O[C@@H](n3cnc4ccccc43)[C@H](OCc3ccccc3)[C@@H]2OCc2ccccc2)cc1
Cl-[CH;D3;+0:1]1-[#8:2]-[C:3]-[C:4]-[C:5]-1-[#8:6].[Cl;D1;H0:7]-[c:8]1:[#7;a:9]:[c:10](:[c:11]):[c:12](:[c:13]):[nH;D2;+0:14]:1>>[#8:6]-[C:5]1-[C:4]-[C:3]-[#8:2]-[C@H;D3;+0:1]-1-[n;H0;D3;+0:14]1:[c:12](:[c:13]):[c:10](:[c:11]):[#7;a:9]:[c:8]:1-[Cl;D1;H0:7]
35
[{"value": 35.0, "product": "ClC1=NC2=C(N1[C@H]1[C@H](OCC3=CC=CC=C3)[C@H](OCC3=CC=CC=C3)[C@H](O1)COCC1=CC=CC=C1)C=C(C(=C2)[N+](=O)[O-])[N+](=O)[O-]", "details": "PERCENTYIELD", "is_desired": false}]
75
CELSIUS
15
MINUTE
To a mixture of 0.541 g (2.23 mmol) of 2-chloro-5,6-dinitrobenzimidazole in 12 mL of MeCN, was added 0.558 mL (2.23 mmol) of BSA. The reaction mixture was stirred at 75° C. for 15 min to give a clear solution. This solution was treated with the above MeCN solution of 2,3,5-tri-O-benzyl-D-ribofuranosyl chloride and 0.56...
10.6084/m9.figshare.5104873.v1
null
Secondary halide.Ether
Ether
C1CCOC1.c1ccc2[nH]cnc2c1
c1ccc2[nH]cnc2c1.C1CCOC1
c1ccc2[nH]cnc2c1.C1CCOC1.c1ccccc1.c1ccccc1.c1ccccc1
HCl
CC#N.CCOC(=O)C
75
0.25
ClC1O[C@H](COCc2ccccc2)[C@@H](OCc2ccccc2)[C@H]1OCc1ccccc1.O=[N+]([O-])c1cc2nc(Cl)[nH]c2cc1[N+](=O)[O-]>CC#N.CCOC(=O)C>O=[N+]([O-])c1cc2nc(Cl)n([C@@H]3O[C@H](COCc4ccccc4)[C@@H](OCc4ccccc4)[C@H]3OCc3ccccc3)c2cc1[N+](=O)[O-]
ord_dataset-02ee2261663048188cf6d85d2cc96e3f
ord-888777079fb14ca3a86b3b24b2f9e593
O=[N+]([O-])c1cc2nc(Cl)n([C@@H]3O[C@H](COCc4ccccc4)[C@@H](OCc4ccccc4)[C@H]3OCc3ccccc3)c2cc1[N+](=O)[O-]>>O=[N+]([O-])c1cc2nc(Cl)n([C@@H]3O[C@H](CO)[C@@H](O)[C@H]3O)c2cc1[N+](=O)[O-]
CO.ClC1=NC2=C(N1[C@H]1[C@H](OCC3=CC=CC=C3)[C@H](OCC3=CC=CC=C3)[C@H](O1)COCC1=CC=CC=C1)C=C(C(=C2)[N+](=O)[O-])[N+](=O)[O-].B(Cl)(Cl)Cl>>ClC1=NC2=C(N1[C@H]1[C@H](O)[C@H](O)[C@H](O1)CO)C=C(C(=C2)[N+](=O)[O-])[N+](=O)[O-]
c1ccc(C[O:15][CH2:14][C@H:13]2[O:12][C@@H:11]([n:10]3[c:8]([Cl:9])[n:7][c:6]4[cH:5][c:4]([N+:2](=[O:1])[O-:3])[c:22]([N+:23](=[O:24])[O-:25])[cH:21][c:20]43)[C@H:18]([O:19]Cc3ccccc3)[C@@H:16]2[O:17]Cc2ccccc2)cc1>>[O:1]=[N+:2]([O-:3])[c:4]1[cH:5][c:6]2[n:7][c:8]([Cl:9])[n:10]([C@@H:11]3[O:12][C@H:13]([CH2:14][OH:15])[C@...
O=[N+]([O-])c1cc2nc(Cl)n([C@@H]3O[C@H](COCc4ccccc4)[C@@H](OCc4ccccc4)[C@H]3OCc3ccccc3)c2cc1[N+](=O)[O-]
O=[N+]([O-])c1cc2nc(Cl)n([C@@H]3O[C@H](CO)[C@@H](O)[C@H]3O)c2cc1[N+](=O)[O-]
null
null
C(Cl)Cl.CCOC(=O)C
Deprotection
OtherReaction
a2ffff3fbeceaaf24517526a2c17f5b86a650947c9a6af47e884fd6d27207539
e242dbd29e2c64f486ea1ce31c428d361e20176899376328dc1f9a6880949e31
c1ccc2c(c1)ncn2[C@H]1CCCO1
C(-[O;H0;D2;+0:1]-[C:2]-[C:3]1-[#8:4]-[C:5]-[C:6](-[O;H0;D2;+0:7]-C-c2:c:c:c:c:c:2)-[C:8]-1-[O;H0;D2;+0:9]-C-c1:c:c:c:c:c:1)-c1:c:c:c:c:c:1>>[OH;D1;+0:1]-[C:2]-[C:3]1-[#8:4]-[C:5]-[C:6](-[OH;D1;+0:7])-[C:8]-1-[OH;D1;+0:9]
77.6
[{"value": 77.6, "product": "ClC1=NC2=C(N1[C@H]1[C@H](O)[C@H](O)[C@H](O1)CO)C=C(C(=C2)[N+](=O)[O-])[N+](=O)[O-]", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
-78
CELSIUS
2
HOUR
To a solution of 0.464 g (0.719 mmol) of 60 in 12 mL of CH2Cl2, was added dropwise 8.4 mL of 1M BCl3 at -78° C. The reaction mixture was stirred at -78° C. for 2 h and then at -40° C. for 2 h. MeOH (5 mL) was added and stirring was continued at -40° C. for 10 min. The reaction mixture was diluted with EtOAc (75 mL). Th...
10.6084/m9.figshare.5104873.v1
null
Ether.Ether.Ether
Primary alcohol.Secondary alcohol.Secondary alcohol
c1ccccc1.c1ccccc1.c1ccccc1
null
c1ccc2[nH]cnc2c1.C1CCOC1
Other
C(Cl)Cl.CCOC(=O)C
-78
2
O=[N+]([O-])c1cc2nc(Cl)n([C@@H]3O[C@H](COCc4ccccc4)[C@@H](OCc4ccccc4)[C@H]3OCc3ccccc3)c2cc1[N+](=O)[O-]>C(Cl)Cl.CCOC(=O)C>O=[N+]([O-])c1cc2nc(Cl)n([C@@H]3O[C@H](CO)[C@@H](O)[C@H]3O)c2cc1[N+](=O)[O-]
ord_dataset-02ee2261663048188cf6d85d2cc96e3f
ord-9fe5815b9f6446a0bb918644fe3631c0
CC(=O)OC[C@H]1O[C@@H](OC(C)=O)[C@H](OC(C)=O)[C@@H]1OC(C)=O.Clc1cc(Cl)c2[nH]c(Cl)nc2c1>>CC(=O)OC[C@H]1O[C@@H](n2c(Cl)nc3c(Cl)cc(Cl)cc32)[C@H](OC(C)=O)[C@@H]1OC(C)=O
ClC=1NC2=C(N1)C=C(C=C2Cl)Cl.C(C)(=O)O[C@H]1[C@H](OC(C)=O)[C@H](OC(C)=O)[C@H](O1)COC(C)=O.[Si](C)(C)(C)OS(=O)(=O)C(F)(F)F>>C(C)(=O)O[C@H]1[C@@H](O[C@@H]([C@H]1OC(C)=O)COC(C)=O)N1C(=NC2=C1C=C(C=C2Cl)Cl)Cl
CC(=O)O[C@@H:8]1[O:7][C@H:6]([CH2:5][O:4][C:2]([CH3:1])=[O:3])[C@@H:26]([O:27][C:28]([CH3:29])=[O:30])[C@H:21]1[O:22][C:23]([CH3:24])=[O:25].[nH:9]1[c:10]([Cl:11])[n:12][c:13]2[cH:19][c:17]([Cl:18])[cH:16][c:14]([Cl:15])[c:20]12>>[CH3:1][C:2](=[O:3])[O:4][CH2:5][C@H:6]1[O:7][C@@H:8]([n:9]2[c:10]([Cl:11])[n:12][c:13]3[c...
CC(=O)OC[C@H]1O[C@@H](OC(C)=O)[C@H](OC(C)=O)[C@@H]1OC(C)=O.Clc1cc(Cl)c2[nH]c(Cl)nc2c1
CC(=O)OC[C@H]1O[C@@H](n2c(Cl)nc3c(Cl)cc(Cl)cc32)[C@H](OC(C)=O)[C@@H]1OC(C)=O
null
null
CC#N.CCOC(=O)C
Heteroatom Alkylation and Arylation
OtherReaction
808be96b2b3729670d01959e9d8dd2b734689aada507d6de2ba46319ea398d03
ae9dd19f446bf9c0f4758602be629bf1e647ce5bccda6016d39f2be87aad806d
c1ccc2c(c1)ncn2[C@H]1CCCO1
C-C(=O)-O-[C@@H;D3;+0:1]1-[#8:2]-[C:3]-[C:4]-[C:5]-1-[#8:6]-[C:7](-[C;D1;H3:8])=[O;D1;H0:9].[Cl;D1;H0:10]-[c:11]1:[#7;a:12]:[c;H0;D3;+0:13]2:[cH;D2;+0:14]:[c:15](-[Cl;D1;H0:16]):[c:17]:[c;H0;D3;+0:18](-[Cl;D1;H0:19]):[c;H0;D3;+0:20]:2:[nH;D2;+0:21]:1>>[C;D1;H3:8]-[C:7](=[O;D1;H0:9])-[#8:6]-[C:5]1-[C:4]-[C:3]-[#8:2]-[C@...
71.3
[{"value": 71.3, "product": "C(C)(=O)O[C@H]1[C@@H](O[C@@H]([C@H]1OC(C)=O)COC(C)=O)N1C(=NC2=C1C=C(C=C2Cl)Cl)Cl", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
80
CELSIUS
15
MINUTE
To a suspension of 1.362 g (6.15 mmol) of 2,4,6-trichlorobenzimidazole in 31 mL of MeCN, was added 1.52 mL (6.15 mmol) of BSA. The reaction mixture was stirred at 80° C. for 15 min to give a clear solution. This solution was treated with 2.153 g (6.675 mmol) of 1,2,3,5-tetra-O-acetyl-β-D-ribofuranose and 1.426 mL (7.38...
10.6084/m9.figshare.5104873.v1
null
Aromatic halide.Ester.Ether
Aromatic halide.Ether
C1CCOC1.c1ccc2[nH]cnc2c1
C1CCOC1.c1ccc2nc[nH]c2c1
C1CCOC1.c1ccc2nc[nH]c2c1
HO-
CC#N.CCOC(=O)C
80
0.25
CC(=O)OC[C@H]1O[C@@H](OC(C)=O)[C@H](OC(C)=O)[C@@H]1OC(C)=O.Clc1cc(Cl)c2[nH]c(Cl)nc2c1>CC#N.CCOC(=O)C>CC(=O)OC[C@H]1O[C@@H](n2c(Cl)nc3c(Cl)cc(Cl)cc32)[C@H](OC(C)=O)[C@@H]1OC(C)=O
ord_dataset-02ee2261663048188cf6d85d2cc96e3f
ord-6b415f062b484284bdb4a8dfbb581067
CC(=O)OC[C@H]1O[C@@H](n2c(Cl)nc3c(Br)c(Br)ccc32)[C@H](OC(C)=O)[C@@H]1OC(C)=O>>OC[C@H]1O[C@@H](n2c(Cl)nc3c(Br)c(Br)ccc32)[C@H](O)[C@@H]1O
ClC1=NC2=C(N1[C@H]1[C@H](OC(C)=O)[C@H](OC(C)=O)[C@H](O1)COC(C)=O)C=CC(=C2Br)Br>>ClC1=NC2=C(N1[C@H]1[C@H](O)[C@H](O)[C@H](O1)CO)C=CC(=C2Br)Br
CC(=O)[O:1][CH2:2][C@H:3]1[O:4][C@@H:5]([n:6]2[c:7]([Cl:8])[n:9][c:10]3[c:11]([Br:12])[c:13]([Br:14])[cH:15][cH:16][c:17]23)[C@H:18]([O:19]C(C)=O)[C@@H:20]1[O:21]C(C)=O>>[OH:1][CH2:2][C@H:3]1[O:4][C@@H:5]([n:6]2[c:7]([Cl:8])[n:9][c:10]3[c:11]([Br:12])[c:13]([Br:14])[cH:15][cH:16][c:17]23)[C@H:18]([OH:19])[C@@H:20]1[OH:...
CC(=O)OC[C@H]1O[C@@H](n2c(Cl)nc3c(Br)c(Br)ccc32)[C@H](OC(C)=O)[C@@H]1OC(C)=O
OC[C@H]1O[C@@H](n2c(Cl)nc3c(Br)c(Br)ccc32)[C@H](O)[C@@H]1O
null
null
N.CO
Reduction
OtherReaction
b1205f31a625dd524c4abcf6ea407c1a38966308677d8535d59411f69b7afe49
53784a05a6c1858c11deb702d4a1392e7852c783da9a57d4771755f87682c932
c1ccc2c(c1)ncn2[C@H]1CCCO1
C-C(=O)-[O;H0;D2;+0:1]-[C:2]1-[C:3]-[#8:4]-[C:5](-[C:6]-[O;H0;D2;+0:7]-C(-C)=O)-[C:8]-1-[O;H0;D2;+0:9]-C(-C)=O>>[OH;D1;+0:1]-[C:2]1-[C:3]-[#8:4]-[C:5](-[C:6]-[OH;D1;+0:7])-[C:8]-1-[OH;D1;+0:9]
null
[]
null
null
null
null
A solution of 0.529 g (0.930 mmol) of 84 in 25 mL of NH3 /MeOH was stirred in a pressure bottle at room temperature for 5 h. Volatile materials were removed by evaporation and coevaporation with MeOH (3 x, bath temperature<40° C.). The resulting solid was recrystallized from MeOH/H2O to give 0.316 g (2 crops, 77%) of 8...
10.6084/m9.figshare.5104873.v1
null
Ester.Ester.Ester
Primary alcohol.Secondary alcohol.Secondary alcohol
null
null
C1CCOC1.c1cc2nc[nH]c2cc1
HO-
N.CO
null
null
CC(=O)OC[C@H]1O[C@@H](n2c(Cl)nc3c(Br)c(Br)ccc32)[C@H](OC(C)=O)[C@@H]1OC(C)=O>N.CO>OC[C@H]1O[C@@H](n2c(Cl)nc3c(Br)c(Br)ccc32)[C@H](O)[C@@H]1O
ord_dataset-02ee2261663048188cf6d85d2cc96e3f
ord-970b971bcff641f38c1bdbadc4189929
BrBr.OC[C@H]1O[C@@H](n2c(Cl)nc3ccc(Cl)cc32)[C@H](O)[C@@H]1O>>OC[C@H]1O[C@@H](n2c(Cl)nc3cc(Br)c(Cl)cc32)[C@H](O)[C@@H]1O
ClC1=NC2=C(N1[C@H]1[C@H](O)[C@H](O)[C@H](O1)CO)C=C(C=C2)Cl.BrBr.O>>BrC1=CC2=C(N(C(=N2)Cl)[C@H]2[C@H](O)[C@H](O)[C@H](O2)CO)C=C1Cl
Br[Br:13].[OH:1][CH2:2][C@H:3]1[O:4][C@@H:5]([n:6]2[c:7]([Cl:8])[n:9][c:10]3[cH:11][cH:12][c:14]([Cl:15])[cH:16][c:17]23)[C@H:18]([OH:19])[C@@H:20]1[OH:21]>>[OH:1][CH2:2][C@H:3]1[O:4][C@@H:5]([n:6]2[c:7]([Cl:8])[n:9][c:10]3[cH:11][c:12]([Br:13])[c:14]([Cl:15])[cH:16][c:17]23)[C@H:18]([OH:19])[C@@H:20]1[OH:21]
BrBr.OC[C@H]1O[C@@H](n2c(Cl)nc3ccc(Cl)cc32)[C@H](O)[C@@H]1O
OC[C@H]1O[C@@H](n2c(Cl)nc3cc(Br)c(Cl)cc32)[C@H](O)[C@@H]1O
null
null
O
Functional Group Interconversion
Bromination
85478af56c963644b81844bf5b7a011f7757bd89cb89f72df54391190362ce77
3c4065ab4a8681675e06a527dcad54d701c7bfdcac9f73f87773b05034108934
c1ccc2c(c1)ncn2[C@H]1CCCO1
Br-[Br;H0;D1;+0:1].[Cl;D1;H0:2]-[c:3]1:[c:4]:[c:5]2:[#7;a:6]:[c:7]:[#7;a:8]:[c:9]:2:[c:10]:[cH;D2;+0:11]:1>>[Br;H0;D1;+0:1]-[c;H0;D3;+0:11]1:[c:10]:[c:9]2:[#7;a:8]:[c:7]:[#7;a:6]:[c:5]:2:[c:4]:[c:3]:1-[Cl;D1;H0:2]
null
[]
null
null
3
HOUR
To a suspension of 0.319 g (1.0 mmol) of 2,6-dichloro-1-β-D-ribofuranosylbenzimidazole in 10 mL of H2O, was added dropwise a sat. solution of Br2 /H2O at room temperature. After the addition has been completed, stirring was continued for 3 h. The reaction mixture was filtered and the solid was washed with portions of H...
10.6084/m9.figshare.5104873.v1
null
null
Aromatic halide
c1ccc2nc[nH]c2c1
c1ccc2[nH]cnc2c1
C1CCOC1.c1ccc2[nH]cnc2c1
HBr
O
null
3
BrBr.OC[C@H]1O[C@@H](n2c(Cl)nc3ccc(Cl)cc32)[C@H](O)[C@@H]1O>O>OC[C@H]1O[C@@H](n2c(Cl)nc3cc(Br)c(Cl)cc32)[C@H](O)[C@@H]1O
ord_dataset-02ee2261663048188cf6d85d2cc96e3f
ord-2a691585e35b4638beb7daeb4f74ee31
BrBr.OC[C@H]1O[C@@H](n2c(Cl)nc3cc(Cl)ccc32)[C@H](O)[C@@H]1O>>OC[C@H]1O[C@@H](n2c(Cl)nc3cc(Cl)c(Br)cc32)[C@H](O)[C@@H]1O
ClC1=NC2=C(N1[C@H]1[C@H](O)[C@H](O)[C@H](O1)CO)C=CC(=C2)Cl.BrBr.O>>BrC=1C(=CC2=C(N(C(=N2)Cl)[C@H]2[C@H](O)[C@H](O)[C@H](O2)CO)C1)Cl
Br[Br:15].[OH:1][CH2:2][C@H:3]1[O:4][C@@H:5]([n:6]2[c:7]([Cl:8])[n:9][c:10]3[cH:11][c:12]([Cl:13])[cH:14][cH:16][c:17]23)[C@H:18]([OH:19])[C@@H:20]1[OH:21]>>[OH:1][CH2:2][C@H:3]1[O:4][C@@H:5]([n:6]2[c:7]([Cl:8])[n:9][c:10]3[cH:11][c:12]([Cl:13])[c:14]([Br:15])[cH:16][c:17]23)[C@H:18]([OH:19])[C@@H:20]1[OH:21]
BrBr.OC[C@H]1O[C@@H](n2c(Cl)nc3cc(Cl)ccc32)[C@H](O)[C@@H]1O
OC[C@H]1O[C@@H](n2c(Cl)nc3cc(Cl)c(Br)cc32)[C@H](O)[C@@H]1O
null
null
O
Functional Group Interconversion
Bromination
e4bd10f799acb6c33603007dd6dc4250314cca1654097931bb81aab38c07d1cb
3c4065ab4a8681675e06a527dcad54d701c7bfdcac9f73f87773b05034108934
c1ccc2c(c1)ncn2[C@H]1CCCO1
Br-[Br;H0;D1;+0:1].[#8:2]-[C:3]-[#7;a:4]1:[c:5]:[#7;a:6]:[c:7]2:[c:8]:[c:9](-[Cl;D1;H0:10]):[cH;D2;+0:11]:[c:12]:[c:13]:1:2>>[#8:2]-[C:3]-[#7;a:4]1:[c:5]:[#7;a:6]:[c:7]2:[c:8]:[c:9](-[Cl;D1;H0:10]):[c;H0;D3;+0:11](-[Br;H0;D1;+0:1]):[c:12]:[c:13]:1:2
null
[]
null
null
6
HOUR
To a suspension of 0.110 g (0.313 mmol, as C12H12Cl2N2O4MeOH) of 2,5-dichloro-1-β-D-ribofuranosylbenzimidazole in 3 mL of H2O was added dropwise 10 mL of a sat. solution of Br2 /H2O at room temperature. After the addition has been completed, stirring was continued for 6 h. The reaction mixture was filtered and the soli...
10.6084/m9.figshare.5104873.v1
null
null
Aromatic halide
c1ccc2[nH]cnc2c1
c1ccc2[nH]cnc2c1
C1CCOC1.c1ccc2[nH]cnc2c1
HBr
O
null
6
BrBr.OC[C@H]1O[C@@H](n2c(Cl)nc3cc(Cl)ccc32)[C@H](O)[C@@H]1O>O>OC[C@H]1O[C@@H](n2c(Cl)nc3cc(Cl)c(Br)cc32)[C@H](O)[C@@H]1O
ord_dataset-02ee2261663048188cf6d85d2cc96e3f
ord-54ee79e104304afe86e6fd203bcf0aac
CC(=O)c1ccc(N)cc1.O=[N+]([O-])c1cnccc1Cl>>CC(=O)c1ccc(Nc2ccncc2[N+](=O)[O-])cc1
Cl.ClC1=C(C=NC=C1)[N+](=O)[O-].NC1=CC=C(C=C1)C(C)=O>>Cl.C(C)(=O)C1=CC=C(C=C1)NC1=C(C=NC=C1)[N+](=O)[O-]
[CH3:1][C:2](=[O:3])[c:4]1[cH:5][cH:6][c:7]([NH2:8])[cH:18][cH:19]1.Cl[c:9]1[cH:10][cH:11][n:12][cH:13][c:14]1[N+:15](=[O:16])[O-:17]>>[CH3:1][C:2](=[O:3])[c:4]1[cH:5][cH:6][c:7]([NH:8][c:9]2[cH:10][cH:11][n:12][cH:13][c:14]2[N+:15](=[O:16])[O-:17])[cH:18][cH:19]1
CC(=O)c1ccc(N)cc1.O=[N+]([O-])c1cnccc1Cl
CC(=O)c1ccc(Nc2ccncc2[N+](=O)[O-])cc1
null
null
C(C)O
Heteroatom Alkylation and Arylation
Goldberg coupling aryl amine-aryl chloride
c026a7bf7aba66b20cf21a13c528689aaaa1c05901524d62b36ca0c3b0572cef
71a04ae650defc5edd86a92f43c304e981a05f07ff76248da8d4155f3905a29d
c1ccc(Nc2ccncc2)cc1
Cl-[c;H0;D3;+0:1]1:[c:2]:[c:3]:[#7;a:4]:[c:5]:[c:6]:1-[#7;+:7].[NH2;D1;+0:8]-[c:9](:[c:10]):[c:11]>>[#7;+:7]-[c:6]1:[c:5]:[#7;a:4]:[c:3]:[c:2]:[c;H0;D3;+0:1]:1-[NH;D2;+0:8]-[c:9](:[c:10]):[c:11]
null
[]
null
null
8
HOUR
A solution of 4-chloro-3-nitropyridine hydrochloride (9.75 g, 50 mmol) in ethanol (40 ml) was added to a slurry of p-aminoacetophenone (6.76 g, 50 ml) in ethanol (25 ml), and the mixture was stirred at room temperature overnight. The mixture was chilled in ice, and the yellow solid filtered off and dried in vacuo. Yiel...
10.6084/m9.figshare.5104873.v1
null
Aromatic halide.Primary amine
Secondary amine
c1ccncc1
c1ccncc1
c1ccccc1.c1ccncc1
HCl
C(C)O
null
8
CC(=O)c1ccc(N)cc1.O=[N+]([O-])c1cnccc1Cl>C(C)O>CC(=O)c1ccc(Nc2ccncc2[N+](=O)[O-])cc1
ord_dataset-02ee2261663048188cf6d85d2cc96e3f
ord-8a022d8b3e334c6db46c27f865df462d
CC(=O)c1ccc(Nc2ccncc2[N+](=O)[O-])cc1>>CC(=O)c1ccc(Nc2ccncc2N)cc1
Cl.C(C)(=O)C1=CC=C(C=C1)NC1=C(C=NC=C1)[N+](=O)[O-].[OH-].[Na+].ClCCl>>C(C)(=O)C1=CC=C(C=C1)NC1=C(C=NC=C1)N
O=[N+:15]([O-])[c:14]1[c:9]([NH:8][c:7]2[cH:6][cH:5][c:4]([C:2]([CH3:1])=[O:3])[cH:17][cH:16]2)[cH:10][cH:11][n:12][cH:13]1>>[CH3:1][C:2](=[O:3])[c:4]1[cH:5][cH:6][c:7]([NH:8][c:9]2[cH:10][cH:11][n:12][cH:13][c:14]2[NH2:15])[cH:16][cH:17]1
CC(=O)c1ccc(Nc2ccncc2[N+](=O)[O-])cc1
CC(=O)c1ccc(Nc2ccncc2N)cc1
null
[Pd]
C(C)O
Reduction
Reduction of nitro groups to amines
bbc242b150a51e69d3ad1caaa391f4422710431b398dcb880555f476706790be
7b0317532ea57a4fcedc1efc3e3c22eb5238d1c8330da53d4f9801fc2391f567
c1ccc(Nc2ccncc2)cc1
O=[N+;H0;D3:1](-[O-])-[c:2](:[c:3]):[c:4]:[#7;a:5]:[c:6]>>[NH2;D1;+0:1]-[c:2](:[c:3]):[c:4]:[#7;a:5]:[c:6]
null
[]
null
null
3.5
HOUR
4-(4-Acetylphenyl)amino-3-nitropyridine hydrochloride (2.0 g, 71.8 mmol) was partitioned between aqueous sodium hydroxide and dichloromethane (3×20 ml). The combined organic phases were washed with water (20 ml) and concentrated under reduced pressure to give a solid. Ethanol (20 ml) was added, and the solution was hyd...
10.6084/m9.figshare.5104873.v1
null
Nitro group
Primary amine
null
null
c1ccccc1.c1ccncc1
Other
[Pd].C(C)O
null
3.5
CC(=O)c1ccc(Nc2ccncc2[N+](=O)[O-])cc1>[Pd].C(C)O>CC(=O)c1ccc(Nc2ccncc2N)cc1
ord_dataset-02ee2261663048188cf6d85d2cc96e3f
ord-c0a37bba41f04afd9a67999b126b0e4c
CCO.Cc1nc2cnccc2n1-c1ccc(C#N)cc1.[OH-]>>Cc1nc2cnccc2n1-c1ccc(C(=O)O)cc1
C(#N)C1=CC=C(C=C1)N1C(=NC=2C=NC=CC21)C.[OH-].[Na+].C(C)O>>CC=1N(C2=C(C=NC=C2)N1)C1=CC=C(C(=O)O)C=C1
CC[OH:17].N#[C:15][c:14]1[cH:13][cH:12][c:11](-[n:10]2[c:2]([CH3:1])[n:3][c:4]3[cH:5][n:6][cH:7][cH:8][c:9]32)[cH:19][cH:18]1.[OH-:16]>>[CH3:1][c:2]1[n:3][c:4]2[cH:5][n:6][cH:7][cH:8][c:9]2[n:10]1-[c:11]1[cH:12][cH:13][c:14]([C:15](=[O:16])[OH:17])[cH:18][cH:19]1
CCO.Cc1nc2cnccc2n1-c1ccc(C#N)cc1.[OH-]
Cc1nc2cnccc2n1-c1ccc(C(=O)O)cc1
null
null
null
Acylation
OtherReaction
e41cdaf6ecb9257286a05c8e01433d124042c5939fb4d758964487a1f4637b56
e38d1b350c527156572f58ef95bb65354ed43ce776b83f166b6fd042d5d9aca9
c1ccc(-n2cnc3cnccc32)cc1
C-C-[OH;D1;+0:1].N#[C;H0;D2;+0:2]-[c:3](:[c:4]):[c:5].[OH-;D0:6]>>[O;H0;D1;+0:6]=[C;H0;D3;+0:2](-[OH;D1;+0:1])-[c:3](:[c:4]):[c:5]
null
[]
0
CELSIUS
null
null
A mixture of 1-(4-cyanophenyl)-2-methylimidazo[4,5-c]pyridine (12.0 g, 51.3 mmol) and 40% aqueous sodium hydroxide (55 ml) in absolute ethanol (55 ml) was heated at reflux for 11/2 hours. The solvent was removed under reduced pressure, and the brown residue was dissolved in water. The solution was chilled to 0° C. by t...
10.6084/m9.figshare.5104873.v1
null
Nitrile.Primary alcohol
Carboxylic acid
null
null
c1nc2ccncc2[nH]1.c1ccccc1
Other
null
0
null
CCO.Cc1nc2cnccc2n1-c1ccc(C#N)cc1.[OH-]>>Cc1nc2cnccc2n1-c1ccc(C(=O)O)cc1
ord_dataset-02ee2261663048188cf6d85d2cc96e3f
ord-2bc83680343e4dc3bafc2ceb0ba1db4f
N#Cc1ccc(N)cc1.O=[N+]([O-])c1cnccc1Cl>>N#Cc1ccc(N2C=CC(N)=C([N+](=O)[O-])C2)cc1
C(#N)C1=CC=C(N)C=C1.ClC1=C(C=NC=C1)[N+](=O)[O-].C(C)O>>C(#N)C1=CC=C(C=C1)N1CC(=C(C=C1)N)[N+](=O)[O-]
[N:1]#[C:2][c:3]1[cH:4][cH:5][c:6]([NH2:11])[cH:17][cH:18]1.Cl[c:10]1[cH:9][cH:8][n:7][cH:16][c:12]1[N+:13](=[O:14])[O-:15]>>[N:1]#[C:2][c:3]1[cH:4][cH:5][c:6]([N:7]2[CH:8]=[CH:9][C:10]([NH2:11])=[C:12]([N+:13](=[O:14])[O-:15])[CH2:16]2)[cH:17][cH:18]1
N#Cc1ccc(N)cc1.O=[N+]([O-])c1cnccc1Cl
N#Cc1ccc(N2C=CC(N)=C([N+](=O)[O-])C2)cc1
null
null
null
Heteroatom Alkylation and Arylation
OtherReaction
f4972f1f841e9ba0e8e5b05ae7c079f1d0ec4fa3257eef450b530a4701a53eef
7f5cb3bfcd0ac63af84eb2f0127a859aff886d9e3621027b9cba876ef76e284f
C1=CCN(c2ccccc2)C=C1
Cl-[c;H0;D3;+0:1]1:[cH;D2;+0:2]:[cH;D2;+0:3]:[n;H0;D2;+0:4]:[cH;D2;+0:5]:[c;H0;D3;+0:6]:1-[#7;+:7](-[O;-;D1;H0:8])=[O;D1;H0:9].[NH2;D1;+0:10]-[c;H0;D3;+0:11](:[c:12]:[c:13]):[c:14]:[c:15]>>[NH2;D1;+0:10]-[C;H0;D3;+0:1]1=[C;H0;D3;+0:6](-[#7;+:7](-[O;-;D1;H0:8])=[O;D1;H0:9])-[CH2;D2;+0:5]-[N;H0;D3;+0:4](-[c;H0;D3;+0:11](...
null
[]
null
null
18
HOUR
According to the method of J. C. S. Perkin Trans. I, 1979, 135, p-cyanoaniline (6.894 g, 58.4 mmol) was added to a solution of 4-chloro-3-nitropyridine (9.26 g, 58.4 mmol) in ethanol (200 ml) and the mixture was stirred at room temperature for 18 hours. The resulting yellow suspension was poured into 500 ml of ice-cold...
10.6084/m9.figshare.5104873.v1
null
Aromatic halide.Nitro group.Primary amine
Enamine.Enamine.Enamine
c1ccccc1.c1ccncc1
c1ccccc1.C1=CC[NH]C=C1
c1ccccc1.C1=CC[NH]C=C1
Other
null
null
18
N#Cc1ccc(N)cc1.O=[N+]([O-])c1cnccc1Cl>>N#Cc1ccc(N2C=CC(N)=C([N+](=O)[O-])C2)cc1
ord_dataset-02ee2261663048188cf6d85d2cc96e3f
ord-bfb37d5ede1743f48bb523d01f9a756e
N#Cc1ccc(N2C=CC(N)=C([N+](=O)[O-])C2)cc1>>N#Cc1ccc(Nc2ccncc2N)cc1
O.O.[Sn](Cl)Cl.C(#N)C1=CC=C(C=C1)N1CC(=C(C=C1)N)[N+](=O)[O-].C(C)O>>NC=1C=NC=CC1NC1=CC=C(C=C1)C#N
O=[N+:14]([O-])[C:13]1=[C:12]([NH2:11])[CH:9]=[CH:10][N:7]([c:6]2[cH:5][cH:4][c:3]([C:2]#[N:1])[cH:16][cH:15]2)[CH2:8]1>>[N:1]#[C:2][c:3]1[cH:4][cH:5][c:6]([NH:7][c:8]2[cH:9][cH:10][n:11][cH:12][c:13]2[NH2:14])[cH:15][cH:16]1
N#Cc1ccc(N2C=CC(N)=C([N+](=O)[O-])C2)cc1
N#Cc1ccc(Nc2ccncc2N)cc1
null
null
Cl.O
Aromatic Heterocycle Formation
OtherReaction
85fffbdc141f9269fd47c5c8c23470804b907d6e82687e1e8a45dc48bdd8e240
337a1a814f17d27a4b29bfe4c3705248b8640b97c12cd64cb063871ed264acd9
c1ccc(Nc2ccncc2)cc1
O=[N+;H0;D3:1](-[O-])-[C;H0;D3;+0:2]1=[C;H0;D3;+0:3](-[NH2;D1;+0:4])-[CH;D2;+0:5]=[CH;D2;+0:6]-[N;H0;D3;+0:7](-[c:8](:[c:9]):[c:10])-[CH2;D2;+0:11]-1>>[NH2;D1;+0:1]-[c;H0;D3;+0:2]1:[cH;D2;+0:3]:[n;H0;D2;+0:4]:[cH;D2;+0:6]:[cH;D2;+0:5]:[c;H0;D3;+0:11]:1-[NH;D2;+0:7]-[c:8](:[c:9]):[c:10]
null
[]
null
null
null
null
According to a modification of the method of Pharm. Helv. Acta, 1975, 50, 188., tin dichloride dihydrate (56.4 g, 250 mmol) was added to a suspension of N-(4-cyanophenyl)-4-amino-3-nitropyridine (12.0 g, 50 mmol) in 2N aqueous hydrochloric acid (35 ml), water (150 ml) and ethanol (75 ml) and the resulting mixture was h...
10.6084/m9.figshare.5104873.v1
null
Enamine.Enamine.Enamine
Primary amine.Secondary amine
C1=CC[NH]C=C1
c1ccncc1
c1ccccc1.c1ccncc1
Other
Cl.O
null
null
N#Cc1ccc(N2C=CC(N)=C([N+](=O)[O-])C2)cc1>Cl.O>N#Cc1ccc(Nc2ccncc2N)cc1
ord_dataset-02ee2261663048188cf6d85d2cc96e3f
ord-1881b69a76034b96a687673d2018cfa2
CCC(CC)(CC)C([O-])([O-])[O-].N#Cc1ccc(Nc2ccncc2N)cc1>>Cc1nc2cnccc2n1-c1ccc(C#N)cc1
NC=1C=NC=CC1NC1=CC=C(C=C1)C#N.C(C)C(C([O-])([O-])[O-])(CC)CC>>C(#N)C1=CC=C(C=C1)N1C(=NC=2C=NC=CC21)C
CC[C:1](CC)(CC)[C:2]([O-])([O-])[O-].[NH2:3][c:4]1[cH:5][n:6][cH:7][cH:8][c:9]1[NH:10][c:11]1[cH:12][cH:13][c:14]([C:15]#[N:16])[cH:17][cH:18]1>>[CH3:1][c:2]1[n:3][c:4]2[cH:5][n:6][cH:7][cH:8][c:9]2[n:10]1-[c:11]1[cH:12][cH:13][c:14]([C:15]#[N:16])[cH:17][cH:18]1
CCC(CC)(CC)C([O-])([O-])[O-].N#Cc1ccc(Nc2ccncc2N)cc1
Cc1nc2cnccc2n1-c1ccc(C#N)cc1
null
null
C(C)(=O)OC(C)=O
Aromatic Heterocycle Formation
OtherReaction
99d7c43dad96eb181154231219720884f174b11d7b53ea87c0579a92d92b6894
c12bf4e666f812d0e692aca3756678364265d1c8b3469e9563c84f9ed1df94d2
c1ccc(-n2cnc3cnccc32)cc1
C-C-[C;H0;D4;+0:1](-C-C)(-C-C)-[C;H0;D4;+0:2](-[O-])(-[O-])-[O-].[NH2;D1;+0:3]-[c:4]1:[c:5]:[#7;a:6]:[c:7]:[c:8]:[c:9]:1-[NH;D2;+0:10]-[c;H0;D3;+0:11](:[c:12]:[c:13]):[c:14]:[c:15]>>[CH3;D1;+0:1]-[c;H0;D3;+0:2]1:[n;H0;D2;+0:3]:[c:4]2:[c:5]:[#7;a:6]:[c:7]:[c:8]:[c:9]:2:[n;H0;D3;+0:10]:1-[c;H0;D3;+0:11](:[c:12]:[c:13]):[...
null
[]
null
null
null
null
A mixture of 3-amino-4-(4'-cyanophenyl)aminopyridine (9.31 g, 44.3 mmol), triethyl-orthoacetate (40 ml) and acetic anhydride (30 ml) was heated at reflux for 2 hours under nitrogen, cooled, then concentrated under reduced pressure. The brown residue was dissolved in 1M hydrochloric acid and washed with ethyl acetate (2...
10.6084/m9.figshare.5104873.v1
null
Primary amine.Secondary amine
null
c1ccncc1
c1nc2ccncc2[nH]1
c1nc2ccncc2[nH]1.c1ccccc1
HO-
C(C)(=O)OC(C)=O
null
null
CCC(CC)(CC)C([O-])([O-])[O-].N#Cc1ccc(Nc2ccncc2N)cc1>C(C)(=O)OC(C)=O>Cc1nc2cnccc2n1-c1ccc(C#N)cc1
ord_dataset-02ee2261663048188cf6d85d2cc96e3f
ord-0b7ac1002a9c48df9ec7bd4af81498e1
CCCCOC(=O)c1cc(=O)n(CCCC)c2ccccc12>>CCCCn1c(=O)cc(C(=O)O)c2ccccc21
C(CCC)N1C(C=C(C2=CC=CC=C12)C(=O)OCCCC)=O.[OH-].[Na+].O>>C(CCC)N1C(C=C(C2=CC=CC=C12)C(=O)O)=O
CCCC[O:12][C:10]([c:9]1[cH:8][c:6](=[O:7])[n:5]([CH2:4][CH2:3][CH2:2][CH3:1])[c:18]2[c:13]1[cH:14][cH:15][cH:16][cH:17]2)=[O:11]>>[CH3:1][CH2:2][CH2:3][CH2:4][n:5]1[c:6](=[O:7])[cH:8][c:9]([C:10](=[O:11])[OH:12])[c:13]2[cH:14][cH:15][cH:16][cH:17][c:18]12
CCCCOC(=O)c1cc(=O)n(CCCC)c2ccccc12
CCCCn1c(=O)cc(C(=O)O)c2ccccc21
null
null
O1CCOCC1
Deprotection
Ester saponification (alkyl deprotection)
d872e08ad5c85a4add6cd04e6e987e73fead5f79b3f30ba61a81ba5029b29894
38ae1ee78433b9acfb0390501446149c80f88f23ac2d84c60b3369bdab75cec9
O=c1ccc2ccccc2[nH]1
C-C-C-C-[O;H0;D2;+0:1]-[C:2](=[O;D1;H0:3])-[c:4]>>[O;D1;H0:3]=[C:2](-[OH;D1;+0:1])-[c:4]
87
[{"value": 87.0, "product": "C(CCC)N1C(C=C(C2=CC=CC=C12)C(=O)O)=O", "details": "PERCENTYIELD", "is_desired": false}, {"value": 86.7, "product": "C(CCC)N1C(C=C(C2=CC=CC=C12)C(=O)O)=O", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
30
MINUTE
A mixture of 2.04 g (6.77 mmols) of Compound b, 0.54 g of sodium hydroxide, 40 ml of water and 40 mt of dioxane was stirred at room temperature for 30 minutes. After concentration under reduced pressure, the residue was purified by silica gel column chromatography (eluting solvent: chloroform/methanol=5/1) to give 1.44...
10.6084/m9.figshare.5104873.v1
null
Ester
Carboxylic acid
null
null
c1ccc2ncccc2c1
Other
O1CCOCC1
null
0.5
CCCCOC(=O)c1cc(=O)n(CCCC)c2ccccc12>O1CCOCC1>CCCCn1c(=O)cc(C(=O)O)c2ccccc21
ord_dataset-02ee2261663048188cf6d85d2cc96e3f
ord-b0cbbbccef144c919960c98519e95613
CC(=O)OC(C)=O.Cc1ccc2c(c1)C(=O)C(=O)N2>>CC(=O)N1C(=O)C(=O)c2cc(C)ccc21
C([O-])(O)=O.[Na+].CC=1C=C2C(C(NC2=CC1)=O)=O.[H-].[Na+].C(C)(=O)OC(C)=O>>C(C)(=O)N1C(=O)C(=O)C2=CC(=CC=C12)C
CC(=O)O[C:2]([CH3:1])=[O:3].[NH:4]1[C:5](=[O:6])[C:7](=[O:8])[c:9]2[cH:10][c:11]([CH3:12])[cH:13][cH:14][c:15]21>>[CH3:1][C:2](=[O:3])[N:4]1[C:5](=[O:6])[C:7](=[O:8])[c:9]2[cH:10][c:11]([CH3:12])[cH:13][cH:14][c:15]21
CC(=O)OC(C)=O.Cc1ccc2c(c1)C(=O)C(=O)N2
CC(=O)N1C(=O)C(=O)c2cc(C)ccc21
null
null
C1(=CC=CC=C1)C
Acylation
Aminolysis of esters
4a0f25f96b85e6dba36941728b4336dc91b0f1a4d810a1dfde51aa5c4671f3af
6ade37977f95c6b33058b518e7f2719ed63964406d89a7d8f0d2f46ad042f783
O=C1Nc2ccccc2C1=O
C-C(=O)-O-[C;H0;D3;+0:1](-[C;D1;H3:2])=[O;D1;H0:3].[O;D1;H0:4]=[C:5]1-[NH;D2;+0:6]-[c:7](:[c:8]):[c:9]-[C:10]-1=[O;D1;H0:11]>>[C;D1;H3:2]-[C;H0;D3;+0:1](=[O;D1;H0:3])-[N;H0;D3;+0:6]1-[C:5](=[O;D1;H0:4])-[C:10](=[O;D1;H0:11])-[c:9]:[c:7]-1:[c:8]
47.6
[{"value": 47.0, "product": "C(C)(=O)N1C(=O)C(=O)C2=CC(=CC=C12)C", "details": "PERCENTYIELD", "is_desired": false}, {"value": 47.6, "product": "C(C)(=O)N1C(=O)C(=O)C2=CC(=CC=C12)C", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
0
CELSIUS
null
null
With stirring at 0° C., 8.06 g (50.0 mmols) of 5-methylisatin was added by small portions to a solution of 2.00 g (50.0 mmols) of sodium hydride in toluene. While stirring under ice cooling, 4.7 ml (50.0 mmols) of acetic anhydride was dropwise added to the mixture followed by heating at 80° C. for further an hour with ...
10.6084/m9.figshare.5104873.v1
null
Anhydride.Secondary amide
Substituted dicarboximide
c1ccc2c(c1)CCN2
c1ccc2c(c1)CC[NH]2
c1ccc2c(c1)CC[NH]2
HO-
C1(=CC=CC=C1)C
0
null
CC(=O)OC(C)=O.Cc1ccc2c(c1)C(=O)C(=O)N2>C1(=CC=CC=C1)C>CC(=O)N1C(=O)C(=O)c2cc(C)ccc21
ord_dataset-02ee2261663048188cf6d85d2cc96e3f
ord-8e967b2fdeb8454a83c24e9d3bcde951
CC1(C)CC(=O)CC(=O)C1.O=C(Cl)c1cccc2nnsc12>>CC1(C)CC(=O)C=C(OC(=O)c2cccc3nnsc23)C1
CC1(CC(CC(C1)=O)=O)C.C(C)N(CC)CC.S1N=NC2=C1C(=CC=C2)C(=O)Cl>>S1N=NC2=C1C(=CC=C2)C(=O)OC2=CC(CC(C2)(C)C)=O
[CH3:1][C:2]1([CH3:3])[CH2:4][C:5](=[O:6])[CH2:7][C:8](=[O:9])[CH2:21]1.Cl[C:10](=[O:11])[c:12]1[cH:13][cH:14][cH:15][c:16]2[n:17][n:18][s:19][c:20]12>>[CH3:1][C:2]1([CH3:3])[CH2:4][C:5](=[O:6])[CH:7]=[C:8]([O:9][C:10](=[O:11])[c:12]2[cH:13][cH:14][cH:15][c:16]3[n:17][n:18][s:19][c:20]23)[CH2:21]1
CC1(C)CC(=O)CC(=O)C1.O=C(Cl)c1cccc2nnsc12
CC1(C)CC(=O)C=C(OC(=O)c2cccc3nnsc23)C1
null
null
C(C)(=O)OCC
Acylation
OtherReaction
6735d7ed13afeda04dc34e9d73db8318d3ee19ff8f52c74cf58af2674d2467cd
7a1f26add480aea147c3ac5da9749e601111e151dc22e68815c1439775d80e22
O=C1C=C(OC(=O)c2cccc3nnsc23)CCC1
Cl-[C;H0;D3;+0:1](=[O;D1;H0:2])-[c:3](:[c:4]):[c:5]1:[#16;a:6]:[#7;a:7]:[#7;a:8]:[c:9]:1.[O;D1;H0:10]=[C:11]1-[C:12]-[C:13]-[C:14]-[C;H0;D3;+0:15](=[O;H0;D1;+0:16])-[CH2;D2;+0:17]-1>>[O;D1;H0:2]=[C;H0;D3;+0:1](-[O;H0;D2;+0:16]-[C;H0;D3;+0:15]1=[CH;D2;+0:17]-[C:11](=[O;D1;H0:10])-[C:12]-[C:13]-[C:14]-1)-[c:3](:[c:4]):[c...
87.5
[{"value": 87.5, "product": "S1N=NC2=C1C(=CC=C2)C(=O)OC2=CC(CC(C2)(C)C)=O", "details": "PERCENTYIELD", "is_desired": false}, {"value": 86.8, "product": "S1N=NC2=C1C(=CC=C2)C(=O)OC2=CC(CC(C2)(C)C)=O", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
8
HOUR
5.6 g (0.04 mol) of 5,5-dimethyl-1,3-cyclohexanedione are dissolved in a mixture of 4.4 g (0.044 mol) of triethylamine and 120 ml of ethyl acetate. 8.7 g (0.044 mol) of benzothiadiazole-7-carboxylic acid chloride are added dropwise at 15° to 20° C., and the mixture is subsequently stirred overnight at room temperature....
10.6084/m9.figshare.5104873.v1
null
Acyl halide.Ketone.Ketone
Ketone.Ester
C1CCCCC1
C1=CCCCC1
C1=CCCCC1.c1ccc2snnc2c1
HCl
C(C)(=O)OCC
null
8
CC1(C)CC(=O)CC(=O)C1.O=C(Cl)c1cccc2nnsc12>C(C)(=O)OCC>CC1(C)CC(=O)C=C(OC(=O)c2cccc3nnsc23)C1
ord_dataset-02ee2261663048188cf6d85d2cc96e3f
ord-48b492e5913b4918978d9c22b2beb223
CCN(CC)CC.O=C(Cl)c1cccc2nnsc12.O=C([O-])CC(=O)[O-]>>CC1(C)OC(=O)C(c2cccc3nnsc23)C(=O)O1
S1N=NC2=C1C(=CC=C2)C(=O)Cl.O1CCCC1.C(CC(=O)[O-])(=O)[O-].C(C)N(CC)CC>>S1N=NC2=C1C(=CC=C2)C2C(OC(OC2=O)(C)C)=O
CCN(CC)C[CH3:3].O=C(Cl)[c:8]1[cH:9][cH:10][cH:11][c:12]2[n:13][n:14][s:15][c:16]12.[O-:4][C:5](=[O:6])[CH2:7][C:17](=[O:18])[O-:19]>>[CH3:1][C:2]1([CH3:3])[O:4][C:5](=[O:6])[CH:7]([c:8]2[cH:9][cH:10][cH:11][c:12]3[n:13][n:14][s:15][c:16]23)[C:17](=[O:18])[O:19]1
CCN(CC)CC.O=C(Cl)c1cccc2nnsc12.O=C([O-])CC(=O)[O-]
CC1(C)OC(=O)C(c2cccc3nnsc23)C(=O)O1
null
CN(C1=CC=NC=C1)C
ClCCl
Heteroatom Alkylation and Arylation
OtherReaction
ae8949bd5389917d799d143b0271a3658b49bede264839d5632bbefb7933ab20
d720e928948097b7f6c113ab62778b4f27788a4832f75effd2f635294ccbe152
O=C1OCOC(=O)C1c1cccc2nnsc12
C-C-N(-C-C)-C-[CH3;D1;+0:1].Cl-C(=O)-[c;H0;D3;+0:2]1:[c:3]:[c:4]:[c:5]:[c:6]2:[#7;a:7]:[#7;a:8]:[#16;a:9]:[c:10]:2:1.[O-;H0;D1:11]-[C:12](=[O;D1;H0:13])-[CH2;D2;+0:14]-[C:15](-[O-;H0;D1:16])=[O;D1;H0:17]>>[C;D1;H3:18]-[C:19]1(-[CH3;D1;+0:1])-[O;H0;D2;+0:11]-[C:12](=[O;D1;H0:13])-[CH;D3;+0:14](-[c;H0;D3;+0:2]2:[c:3]:[c:...
null
[]
0
CELSIUS
2
HOUR
5.5 g of benzo-1,2,3-thiadiazole-7-carboxylic acid chloride in 10 ml of tetrahydrofuran are added dropwise to a solution, stirred at 0° C., of 3.6 g of cycloisopropylidene malonate, 7.6 ml of triethylamine and 2.0 g of 4-dimethylaminopyridine in 25 ml of dichloromethane. The reaction mixture is stirred for 2 hours at 0...
10.6084/m9.figshare.5104873.v1
null
Acyl halide.Tertiary amine
Ester.Ester
c1ccc2snnc2c1
C1COCOC1.c1ccc2snnc2c1
C1COCOC1.c1ccc2snnc2c1
HCl
CN(C1=CC=NC=C1)C.ClCCl
0
2
CCN(CC)CC.O=C(Cl)c1cccc2nnsc12.O=C([O-])CC(=O)[O-]>CN(C1=CC=NC=C1)C.ClCCl>CC1(C)OC(=O)C(c2cccc3nnsc23)C(=O)O1
ord_dataset-02ee2261663048188cf6d85d2cc96e3f
ord-ac19de6fdddf43cb807f1b8ce12dad02
CCOC(=O)CC(=O)OCC.O=C(Cl)c1cccc2nnsc12>>CCOC(=O)C(C(=O)OCC)c1cccc2nnsc12
Cl.S1N=NC2=C1C(=CC=C2)C(=O)Cl.[Cl-].[Mg+2].[Cl-].C(CC(=O)OCC)(=O)OCC>>S1N=NC2=C1C(=CC=C2)C(C(=O)OCC)C(=O)OCC
[CH3:1][CH2:2][O:3][C:4](=[O:5])[CH2:6][C:7](=[O:8])[O:9][CH2:10][CH3:11].O=C(Cl)[c:12]1[cH:13][cH:14][cH:15][c:16]2[n:17][n:18][s:19][c:20]12>>[CH3:1][CH2:2][O:3][C:4](=[O:5])[CH:6]([C:7](=[O:8])[O:9][CH2:10][CH3:11])[c:12]1[cH:13][cH:14][cH:15][c:16]2[n:17][n:18][s:19][c:20]12
CCOC(=O)CC(=O)OCC.O=C(Cl)c1cccc2nnsc12
CCOC(=O)C(C(=O)OCC)c1cccc2nnsc12
null
null
C(C)#N.C(C)N(CC)CC
C-C Coupling
OtherReaction
1827c9723f069e808d178933fb2dc8d05c44677163aabec504aa40d27d6c1785
e28ec79096f04aff39f08a42e1f41a13d940f698d541817c5a1398a9c16c1710
c1ccc2snnc2c1
Cl-C(=O)-[c;H0;D3;+0:1]1:[c:2]:[c:3]:[c:4]:[c:5]2:[#7;a:6]:[#7;a:7]:[#16;a:8]:[c:9]:2:1.[C:10]-[#8:11]-[C:12](=[O;D1;H0:13])-[CH2;D2;+0:14]-[C:15](=[O;D1;H0:16])-[#8:17]-[C:18]>>[C:10]-[#8:11]-[C:12](=[O;D1;H0:13])-[CH;D3;+0:14](-[C:15](=[O;D1;H0:16])-[#8:17]-[C:18])-[c;H0;D3;+0:1]1:[c:2]:[c:3]:[c:4]:[c:5]2:[#7;a:6]:[#...
83.2
[{"value": 83.2, "product": "S1N=NC2=C1C(=CC=C2)C(C(=O)OCC)C(=O)OCC", "details": "PERCENTYIELD", "is_desired": false}]
0
CELSIUS
null
null
4.8 g of magnesium chloride in 50 ml of acetonitrile are treated with 7.6 ml of diethyl malonate and 14 ml of triethylamine, with ice-cooling and stirring. The mixture is stirred for 20 minutes and then treated at 0°-5° C. with portions of a suspension of 9.6 g of benzo-1,2,3-thiadiazole-7-carboxylic acid chloride in 5...
10.6084/m9.figshare.5104873.v1
null
Acyl halide.Ester.Ester
Ester.Ester
c1ccc2snnc2c1
c1ccc2snnc2c1
c1ccc2snnc2c1
HCl
C(C)#N.C(C)N(CC)CC
0
null
CCOC(=O)CC(=O)OCC.O=C(Cl)c1cccc2nnsc12>C(C)#N.C(C)N(CC)CC>CCOC(=O)C(C(=O)OCC)c1cccc2nnsc12
ord_dataset-02ee2261663048188cf6d85d2cc96e3f
ord-8551d82337ad4e2ca282f87e462a018c
CON=C(C(N)=O)c1ccccc1Oc1ccccc1>>CON=C(C#N)c1ccccc1Oc1ccccc1
O(C1=CC=CC=C1)C1=C(C=CC=C1)C(C(=O)N)=NOC.FC(C(=O)OC(C(F)(F)F)=O)(F)F>>O(C1=CC=CC=C1)C1=C(C=CC=C1)C(C#N)=NOC
O=[C:5]([C:4](=[N:3][O:2][CH3:1])[c:7]1[cH:8][cH:9][cH:10][cH:11][c:12]1[O:13][c:14]1[cH:15][cH:16][cH:17][cH:18][cH:19]1)[NH2:6]>>[CH3:1][O:2][N:3]=[C:4]([C:5]#[N:6])[c:7]1[cH:8][cH:9][cH:10][cH:11][c:12]1[O:13][c:14]1[cH:15][cH:16][cH:17][cH:18][cH:19]1
CON=C(C(N)=O)c1ccccc1Oc1ccccc1
CON=C(C#N)c1ccccc1Oc1ccccc1
null
null
Cl.N1=CC=CC=C1
Miscellaneous
OtherReaction
5094e9d814705bbdc421edbf7e9198e499e70e93916e2cec6eefbc82d1ba5440
32b9893bcb5223559a9d02852f8392cf6473aacfb044a52ba4e9cb9c29edb170
c1ccc(Oc2ccccc2)cc1
O=[C;H0;D3;+0:1](-[NH2;D1;+0:2])-[C:3](-[c:4])=[#7:5]-[#8:6]>>[#8:6]-[#7:5]=[C:3](-[c:4])-[C;H0;D2;+0:1]#[N;H0;D1;+0:2]
96.9
[{"value": 96.9, "product": "O(C1=CC=CC=C1)C1=C(C=CC=C1)C(C#N)=NOC", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
0
CELSIUS
2
HOUR
2-(2-Phenoxyphenyl)-2-methoxyiminoacetamide (3.77 g) was dissolved in pyridine (5.53 g). The solution was cooled to 0° C. Trifluoroacetic anhydride (4.40 g) was added dropwise. The mixture was stirred for 2 hours at 0° C., and then diluted with dil. hydrochloric acid and extracted with ethyl acetate. The extract was dr...
10.6084/m9.figshare.5104873.v1
null
Primary amide
Nitrile
null
null
c1ccccc1.c1ccccc1
HO-
Cl.N1=CC=CC=C1
0
2
CON=C(C(N)=O)c1ccccc1Oc1ccccc1>Cl.N1=CC=CC=C1>CON=C(C#N)c1ccccc1Oc1ccccc1
ord_dataset-02ee2261663048188cf6d85d2cc96e3f
ord-e555e7dc8bc3456baab94c706ef1c2ed
O=C(Br)CBr.O=C(c1ccccc1)c1cccc2c1NCCO2>>O=C(c1ccccc1)c1cccc2c1N(C(=O)CBr)CCO2
C(C1=CC=CC=C1)(=O)C1=CC=CC2=C1NCCO2.N1=CC=CC=C1.BrCC(=O)Br.O>>BrCC(=O)N1CCOC2=C1C(=CC=C2)C(C2=CC=CC=C2)=O
Br[C:16](=[O:17])[CH2:18][Br:19].[O:1]=[C:2]([c:3]1[cH:4][cH:5][cH:6][cH:7][cH:8]1)[c:9]1[cH:10][cH:11][cH:12][c:13]2[c:14]1[NH:15][CH2:20][CH2:21][O:22]2>>[O:1]=[C:2]([c:3]1[cH:4][cH:5][cH:6][cH:7][cH:8]1)[c:9]1[cH:10][cH:11][cH:12][c:13]2[c:14]1[N:15]([C:16](=[O:17])[CH2:18][Br:19])[CH2:20][CH2:21][O:22]2
O=C(Br)CBr.O=C(c1ccccc1)c1cccc2c1NCCO2
O=C(c1ccccc1)c1cccc2c1N(C(=O)CBr)CCO2
null
null
C(Cl)Cl
Acylation
N-alkylation of secondary amines with alkyl halides
01ebb2cf1a1c967cd091832d838545262f7647265a4fa9f17181e6a0858005ad
96cb0a2fed10552c5770a45a2d6523b47ac3e38928b4a9c698d8577451182dcd
O=C(c1ccccc1)c1cccc2c1NCCO2
Br-[C;H0;D3;+0:1](=[O;D1;H0:2])-[C:3]-[Br;D1;H0:4].[O;D1;H0:5]=[C:6]-[c:7]:[c:8]1:[c:9]-[#8:10]-[C:11]-[C:12]-[NH;D2;+0:13]-1>>[Br;D1;H0:4]-[C:3]-[C;H0;D3;+0:1](=[O;D1;H0:2])-[N;H0;D3;+0:13]1-[C:12]-[C:11]-[#8:10]-[c:9]:[c:8]-1:[c:7]-[C:6]=[O;D1;H0:5]
69.4
[{"value": 69.4, "product": "BrCC(=O)N1CCOC2=C1C(=CC=C2)C(C2=CC=CC=C2)=O", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
null
null
To a solution of 5-benzoyl-3,4-dihydro-2H-1,4-benzoxazine (5.74 g), pyridine (1.9 g) and methylene chloride (100 ml) was dropwise added a solution of bromoacetyl bromide (5.82 g) in methylene chloride (5 ml) at room temperature. After the mixture was stirred for 1.0 hour at the same temperature, water (100 ml) was adde...
10.6084/m9.figshare.5104873.v1
null
Acyl halide.Secondary amine
Tertiary amide
c1ccc2c(c1)NCCO2
c1ccc2c(c1)[NH]CCO2
c1ccccc1.c1ccc2c(c1)[NH]CCO2
HBr
C(Cl)Cl
null
null
O=C(Br)CBr.O=C(c1ccccc1)c1cccc2c1NCCO2>C(Cl)Cl>O=C(c1ccccc1)c1cccc2c1N(C(=O)CBr)CCO2
ord_dataset-02ee2261663048188cf6d85d2cc96e3f
ord-e8a77560b32d4c18a9b1ab844404ff19
N#Cc1cccc2c1NCC2.O=S(=O)(O)O.[OH-]>>O=C(O)c1cccc2c1NCC2
C(#N)C=1C=CC=C2CCNC12.S(O)(O)(=O)=O.[OH-].[Na+]>>N1CCC2=CC=CC(=C12)C(=O)O
N#[C:2][c:4]1[cH:5][cH:6][cH:7][c:8]2[c:9]1[NH:10][CH2:11][CH2:12]2.O=S(=O)(O)[OH:1].[OH-:3]>>[O:1]=[C:2]([OH:3])[c:4]1[cH:5][cH:6][cH:7][c:8]2[c:9]1[NH:10][CH2:11][CH2:12]2
N#Cc1cccc2c1NCC2.O=S(=O)(O)O.[OH-]
O=C(O)c1cccc2c1NCC2
null
null
null
Acylation
OtherReaction
e05c34ebe51fe654c61f91bb118ee544dcd0a035df9f073c07f2e1b77a1f299a
e722778fc7d66899e0f2f256942c8c213a77617f32bb1410d97747833c62e260
c1ccc2c(c1)CCN2
N#[C;H0;D2;+0:1]-[c:2](:[c:3]):[c:4]-[#7:5].O-S(=O)(=O)-[OH;D1;+0:6].[OH-;D0:7]>>[#7:5]-[c:4]:[c:2](-[C;H0;D3;+0:1](=[O;H0;D1;+0:6])-[OH;D1;+0:7]):[c:3]
null
[]
5
CELSIUS
5.5
HOUR
A mixture of 7-cyanoindoline (4.32 g) and 50% aqueous sulfuric acid (40 ml) was stirred at 110°-120° C. for 5.5 hours, cooled to 5° C. and adjusted to pH 7-8 with 24% aqueous sodium hydroxide. The mixture was washed with ethyl acetate and the aqueous layer was adjusted to pH 2.5-3.0 with 6N hydrochloric acid. The preci...
10.6084/m9.figshare.5104873.v1
null
Nitrile
Carboxylic acid
null
null
c1ccc2c(c1)CCN2
HO-
null
5
5.5
N#Cc1cccc2c1NCC2.O=S(=O)(O)O.[OH-]>>O=C(O)c1cccc2c1NCC2
ord_dataset-02ee2261663048188cf6d85d2cc96e3f
ord-9cac606d071b4395a00aaae08346ef5c
COC(=O)/C=C/c1ccccc1NCc1c[nH]cn1>>Cl.O=C(O)/C=C/c1ccccc1NCc1c[nH]cn1
Cl.N1C=NC(=C1)CNC1=C(C=CC=C1)/C=C/C(=O)OC.[OH-].[Na+]>>Cl.Cl.N1C=NC(=C1)CNC1=C(C=CC=C1)/C=C/C(=O)O
C[O:5][C:4](=[O:3])/[CH:6]=[CH:7]/[c:8]1[cH:9][cH:10][cH:11][cH:12][c:13]1[NH:14][CH2:15][c:16]1[cH:17][nH:18][cH:19][n:20]1>>[ClH:2].[O:3]=[C:4]([OH:5])/[CH:6]=[CH:7]/[c:8]1[cH:9][cH:10][cH:11][cH:12][c:13]1[NH:14][CH2:15][c:16]1[cH:17][nH:18][cH:19][n:20]1
COC(=O)/C=C/c1ccccc1NCc1c[nH]cn1
Cl.O=C(O)/C=C/c1ccccc1NCc1c[nH]cn1
null
null
CO
Functional Group Interconversion
Ester saponification (methyl deprotection)
b78ecd40845eb2270e6550c75ea2630cb164c9b25eda3fae0a944391d7396a3c
6621c5a39698b382c2c29eacd30adc11ac3552c724c517b0f319c6099a4467de
c1ccc(NCc2c[nH]cn2)cc1
C-[O;H0;D2;+0:1]-[C:2](=[O;D1;H0:3])/[C:4]=[C:5]/[c:6]>>[O;D1;H0:3]=[C:2](-[OH;D1;+0:1])/[C:4]=[C:5]/[c:6]
null
[]
null
null
20
HOUR
To a solution of methyl (E)-3-[2-(4-imidazolylmethylamino)phenyl]propenoate (0.7 g) in methanol (7 ml) was added 1N sodium hydroxide aqueous solution (3 ml) and the mixture was stirred for 20 hours. After removal of methanol from the reaction mixture, water was added to the residue. The mixture was adjusted to pH 6 wit...
10.6084/m9.figshare.5104873.v1
null
Ester
Carboxylic acid
null
null
c1ccccc1.c1c[nH]cn1
null
CO
null
20
COC(=O)/C=C/c1ccccc1NCc1c[nH]cn1>CO>Cl.O=C(O)/C=C/c1ccccc1NCc1c[nH]cn1
ord_dataset-02ee2261663048188cf6d85d2cc96e3f
ord-d66b4eef54b0430690c4005529ed7d6e
CN(C)c1cccc2c(S(=O)(=O)Cl)cccc12.N[C@@H](CCCNC(=O)OCc1ccccc1)C(=O)O>>CN(C)c1cccc2c(S(=O)(=O)NC(CCCNC(=O)OCc3ccccc3)C(=O)O)cccc12
C(=O)(OCC1=CC=CC=C1)NCCC[C@H](N)C(=O)O.S(=O)(=O)(C1=CC=CC=2C(N(C)C)=CC=CC12)Cl.Cl>>CN(C1=C2C=CC=C(C2=CC=C1)S(=O)(=O)NC(C(=O)O)CCCNC(=O)OCC1=CC=CC=C1)C
Cl[S:10]([c:9]1[c:8]2[cH:7][cH:6][cH:5][c:4]([N:2]([CH3:1])[CH3:3])[c:35]2[cH:34][cH:33][cH:32]1)(=[O:11])=[O:12].[NH2:13][C@@H:14]([CH2:15][CH2:16][CH2:17][NH:18][C:19](=[O:20])[O:21][CH2:22][c:23]1[cH:24][cH:25][cH:26][cH:27][cH:28]1)[C:29](=[O:30])[OH:31]>>[CH3:1][N:2]([CH3:3])[c:4]1[cH:5][cH:6][cH:7][c:8]2[c:9]([S:...
CN(C)c1cccc2c(S(=O)(=O)Cl)cccc12.N[C@@H](CCCNC(=O)OCc1ccccc1)C(=O)O
CN(C)c1cccc2c(S(=O)(=O)NC(CCCNC(=O)OCc3ccccc3)C(=O)O)cccc12
null
null
[OH-].[Na+].O1CCCC1
Acylation
Sulfonamide synthesis (Schotten-Baumann) primary amine
4c44ef6d7646f6ef25dd125d2c32c713d8dcae7c603407faa5f0fb810631670e
8fce8115d8a725afa92eb3910ded29d4c852e5133eba78a425054f41f7142603
O=C(NCCCCNS(=O)(=O)c1cccc2ccccc12)OCc1ccccc1
Cl-[S;H0;D4;+0:1](=[O;D1;H0:2])(=[O;D1;H0:3])-[c:4](:[c:5]):[c:6].[C:7]-[C:8]-[C@H;D3;+0:9](-[NH2;D1;+0:10])-[C:11](=[O;D1;H0:12])-[O;D1;H1:13]>>[C:7]-[C:8]-[CH;D3;+0:9](-[NH;D2;+0:10]-[S;H0;D4;+0:1](=[O;D1;H0:2])(=[O;D1;H0:3])-[c:4](:[c:5]):[c:6])-[C:11](=[O;D1;H0:12])-[O;D1;H1:13]
null
[]
0
CELSIUS
15
MINUTE
Nδ -Carbobenzyloxy-L-ornithine (39.6 g, 0.149 mol) was dissolved in a solution of 2N NaOH (90 mL) and tetrahydrofuran (200 mL) under nitrogen. After about 15 minutes at ambient temperature, the mixture was cooled to about 0° C. and subsequently treated with additional 2N NaOH (85 mL) and dansyl chloride (45.0 g, 0.167 ...
10.6084/m9.figshare.5104873.v1
null
Primary amine.Sulfonyl halide
Sulfonamide
null
null
c1ccccc1.c1ccc2ccccc2c1
HCl
[OH-].[Na+].O1CCCC1
0
0.25
CN(C)c1cccc2c(S(=O)(=O)Cl)cccc12.N[C@@H](CCCNC(=O)OCc1ccccc1)C(=O)O>[OH-].[Na+].O1CCCC1>CN(C)c1cccc2c(S(=O)(=O)NC(CCCNC(=O)OCc3ccccc3)C(=O)O)cccc12
ord_dataset-02ee2261663048188cf6d85d2cc96e3f
ord-2d1677a7d55446d6936250ae86c5bfcb
CCC1CCNCC1.CN(C)c1cccc2c(S(=O)(=O)NC(CCCNC(=O)OCc3ccccc3)C(=O)O)cccc12>>CCC1CCN(C(=O)C(CCCNC(=O)OCc2ccccc2)NS(=O)(=O)c2cccc3c(N(C)C)cccc23)CC1
C1(=CC=CC=C1)P(=O)(C1=CC=CC=C1)N=[N+]=[N-].CN(C1=C2C=CC=C(C2=CC=C1)S(=O)(=O)NC(C(=O)O)CCCNC(=O)OCC1=CC=CC=C1)C.C(C)N(CC)CC.C(C)C1CCNCC1>>CN(C1=C2C=CC=C(C2=CC=C1)S(=O)(=O)NC(CCCNC(OCC1=CC=CC=C1)=O)C(=O)N1CCC(CC1)CC)C
[CH3:1][CH2:2][CH:3]1[CH2:4][CH2:5][NH:6][CH2:41][CH2:42]1.O[C:7](=[O:8])[CH:9]([CH2:10][CH2:11][CH2:12][NH:13][C:14](=[O:15])[O:16][CH2:17][c:18]1[cH:19][cH:20][cH:21][cH:22][cH:23]1)[NH:24][S:25](=[O:26])(=[O:27])[c:28]1[cH:29][cH:30][cH:31][c:32]2[c:33]([N:34]([CH3:35])[CH3:36])[cH:37][cH:38][cH:39][c:40]12>>[CH3:1]...
CCC1CCNCC1.CN(C)c1cccc2c(S(=O)(=O)NC(CCCNC(=O)OCc3ccccc3)C(=O)O)cccc12
CCC1CCN(C(=O)C(CCCNC(=O)OCc2ccccc2)NS(=O)(=O)c2cccc3c(N(C)C)cccc23)CC1
null
null
CN(C=O)C
Acylation
Acylation of Nitrogen Nucleophiles by Carboxylic Acids
fbfce93ec1ece674255bb96c5cec09ad611382b41cf117dfe580015e21744a71
c5e4172490b2731ba9322b68af56376edadc31ce0bb9a3dfdea23a1817a852fd
O=C(NCCCC(NS(=O)(=O)c1cccc2ccccc12)C(=O)N1CCCCC1)OCc1ccccc1
O-[C;H0;D3;+0:1](=[O;D1;H0:2])-[C:3](-[#7:4])-[C:5].[C:6]-[C:7]-[NH;D2;+0:8]-[C:9]-[C:10]>>[#7:4]-[C:3](-[C:5])-[C;H0;D3;+0:1](=[O;D1;H0:2])-[N;H0;D3;+0:8](-[C:7]-[C:6])-[C:9]-[C:10]
91.1
[{"value": 45.0, "product": "CN(C1=C2C=CC=C(C2=CC=C1)S(=O)(=O)NC(CCCNC(OCC1=CC=CC=C1)=O)C(=O)N1CCC(CC1)CC)C", "details": "PERCENTYIELD", "is_desired": false}, {"value": 91.1, "product": "CN(C1=C2C=CC=C(C2=CC=C1)S(=O)(=O)NC(CCCNC(OCC1=CC=CC=C1)=O)C(=O)N1CCC(CC1)CC)C", "details": "CALCULATEDPERCENTYIELD", "is_desired": f...
0
CELSIUS
2
HOUR
To a cold (0° C.), nitrogen-blanketed mixture of 2d (48.90 g, 0.098 mol), triethylamine (25.0 mL, 0.18 mol) and 4-ethylpiperidine (20.0 g, 0.18 mol) in anhydrous dimethylformamide (160 mL) was added dropwise diphenylphosphoryl azide (21.1 mL, 0.098 mol). The mixture was stirred at about 0° C. for about 1 hour and at am...
10.6084/m9.figshare.5104873.v1
null
Carboxylic acid.Secondary amine
Tertiary amide
C1CCNCC1
C1CC[NH]CC1
C1CC[NH]CC1.c1ccccc1.c1ccc2ccccc2c1
HO-
CN(C=O)C
0
2
CCC1CCNCC1.CN(C)c1cccc2c(S(=O)(=O)NC(CCCNC(=O)OCc3ccccc3)C(=O)O)cccc12>CN(C=O)C>CCC1CCN(C(=O)C(CCCNC(=O)OCc2ccccc2)NS(=O)(=O)c2cccc3c(N(C)C)cccc23)CC1
ord_dataset-02ee2261663048188cf6d85d2cc96e3f
ord-379118b96b384749848f4c9aace367b8
Cc1ccc(S(=O)(=O)Cl)cc1.N[C@@H](CCCCNC(=O)OCc1ccccc1)C(=O)O>>Cc1ccc(S(=O)(=O)NC(CCCCNC(=O)OCc2ccccc2)C(=O)O)cc1
C(=O)(OCC1=CC=CC=C1)NCCCC[C@H](N)C(=O)O.C1(=CC=C(C=C1)S(=O)(=O)Cl)C.Cl>>CC1=CC=C(C=C1)S(=O)(=O)NC(C(=O)O)CCCCNC(=O)OCC1=CC=CC=C1
Cl[S:6]([c:5]1[cH:4][cH:3][c:2]([CH3:1])[cH:30][cH:29]1)(=[O:7])=[O:8].[NH2:9][C@@H:10]([CH2:11][CH2:12][CH2:13][CH2:14][NH:15][C:16](=[O:17])[O:18][CH2:19][c:20]1[cH:21][cH:22][cH:23][cH:24][cH:25]1)[C:26](=[O:27])[OH:28]>>[CH3:1][c:2]1[cH:3][cH:4][c:5]([S:6](=[O:7])(=[O:8])[NH:9][CH:10]([CH2:11][CH2:12][CH2:13][CH2:1...
Cc1ccc(S(=O)(=O)Cl)cc1.N[C@@H](CCCCNC(=O)OCc1ccccc1)C(=O)O
Cc1ccc(S(=O)(=O)NC(CCCCNC(=O)OCc2ccccc2)C(=O)O)cc1
null
null
[OH-].[Na+].C(C)(=O)OCC.O1CCOCC1
Acylation
Sulfonamide synthesis (Schotten-Baumann) primary amine
84f0a2c480e4021adb28613388cdf35ca03a8bd65bbdad356e160a1b94684976
2988afdf4a13d931f021994343ac8648c6e63ca3a4c0ba598a4b99bbffc001c8
O=C(NCCCCCNS(=O)(=O)c1ccccc1)OCc1ccccc1
Cl-[S;H0;D4;+0:1](=[O;D1;H0:2])(=[O;D1;H0:3])-[c:4](:[c:5]):[c:6].[C:7]-[C:8]-[C@H;D3;+0:9](-[NH2;D1;+0:10])-[C:11](=[O;D1;H0:12])-[O;D1;H1:13]>>[C:7]-[C:8]-[CH;D3;+0:9](-[NH;D2;+0:10]-[S;H0;D4;+0:1](=[O;D1;H0:2])(=[O;D1;H0:3])-[c:4](:[c:5]):[c:6])-[C:11](=[O;D1;H0:12])-[O;D1;H1:13]
81,024.5
[{"value": 81.0, "product": "CC1=CC=C(C=C1)S(=O)(=O)NC(C(=O)O)CCCCNC(=O)OCC1=CC=CC=C1", "details": "PERCENTYIELD", "is_desired": false}, {"value": 81024.5, "product": "CC1=CC=C(C=C1)S(=O)(=O)NC(C(=O)O)CCCCNC(=O)OCC1=CC=CC=C1", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
0
CELSIUS
15
MINUTE
Nε -Carbobenzyloxy-L-lysine (30.0 g, 0.107 mmol) was dissolved in a solution of 2N NaOH (60 mL) and dioxane (150 mL) under nitrogen. After about 15 minutes at room temperature, the mixture was cooled to about 0° C. and subsequently treated with additional 2N NaOH (60 mL) and p-toluenesulfonyl chloride (20.4 g, 0.107 mm...
10.6084/m9.figshare.5104873.v1
null
Tosylate.Primary amine.Sulfonyl halide
Sulfonamide
null
null
c1ccccc1.c1ccccc1
HCl
[OH-].[Na+].C(C)(=O)OCC.O1CCOCC1
0
0.25
Cc1ccc(S(=O)(=O)Cl)cc1.N[C@@H](CCCCNC(=O)OCc1ccccc1)C(=O)O>[OH-].[Na+].C(C)(=O)OCC.O1CCOCC1>Cc1ccc(S(=O)(=O)NC(CCCCNC(=O)OCc2ccccc2)C(=O)O)cc1
ord_dataset-02ee2261663048188cf6d85d2cc96e3f
ord-2e91d8d7e54a4b55a7abb98099f7788c
C1CCNCC1.Cc1ccc(S(=O)(=O)NC(CCCCNC(=O)OCc2ccccc2)C(=O)O)cc1>>Cc1ccc(S(=O)(=O)NC(CCCCNC(=O)OCc2ccccc2)C(=O)N2CCCCC2)cc1
C1(=CC=CC=C1)P(=O)(C1=CC=CC=C1)N=[N+]=[N-].CC1=CC=C(C=C1)S(=O)(=O)NC(C(=O)O)CCCCNC(=O)OCC1=CC=CC=C1.C(C)N(CC)CC.N1CCCCC1>>N1(CCCCC1)C(C(CCCCNC(OCC1=CC=CC=C1)=O)NS(=O)(=O)C1=CC=C(C=C1)C)=O
[NH:28]1[CH2:29][CH2:30][CH2:31][CH2:32][CH2:33]1.O[C:26]([CH:10]([NH:9][S:6]([c:5]1[cH:4][cH:3][c:2]([CH3:1])[cH:35][cH:34]1)(=[O:7])=[O:8])[CH2:11][CH2:12][CH2:13][CH2:14][NH:15][C:16](=[O:17])[O:18][CH2:19][c:20]1[cH:21][cH:22][cH:23][cH:24][cH:25]1)=[O:27]>>[CH3:1][c:2]1[cH:3][cH:4][c:5]([S:6](=[O:7])(=[O:8])[NH:9]...
C1CCNCC1.Cc1ccc(S(=O)(=O)NC(CCCCNC(=O)OCc2ccccc2)C(=O)O)cc1
Cc1ccc(S(=O)(=O)NC(CCCCNC(=O)OCc2ccccc2)C(=O)N2CCCCC2)cc1
null
null
CN(C=O)C
Acylation
Acylation of Nitrogen Nucleophiles by Carboxylic Acids
fbfce93ec1ece674255bb96c5cec09ad611382b41cf117dfe580015e21744a71
c5e4172490b2731ba9322b68af56376edadc31ce0bb9a3dfdea23a1817a852fd
O=C(NCCCCC(NS(=O)(=O)c1ccccc1)C(=O)N1CCCCC1)OCc1ccccc1
O-[C;H0;D3;+0:1](=[O;D1;H0:2])-[C:3](-[#7:4])-[C:5].[C:6]-[C:7]-[NH;D2;+0:8]-[C:9]-[C:10]>>[#7:4]-[C:3](-[C:5])-[C;H0;D3;+0:1](=[O;D1;H0:2])-[N;H0;D3;+0:8](-[C:7]-[C:6])-[C:9]-[C:10]
100.6
[{"value": 100.0, "product": "N1(CCCCC1)C(C(CCCCNC(OCC1=CC=CC=C1)=O)NS(=O)(=O)C1=CC=C(C=C1)C)=O", "details": "PERCENTYIELD", "is_desired": false}, {"value": 100.6, "product": "N1(CCCCC1)C(C(CCCCNC(OCC1=CC=CC=C1)=O)NS(=O)(=O)C1=CC=C(C=C1)C)=O", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
0
CELSIUS
2
HOUR
To a cold (0° C.), nitrogen-blanketed mixture of 2-[[(4-methylphenyl]sulfonyl]amino]-6-[[(phenylmethoxy)carbonyl]amino]hexanoic acid (18.00 g, 44.43 mmol), triethylamine (5.80 mL, 41.43 mmol) and piperidine (4.10 mL, 41.43 mmol) in anhydrous dimethylformamide (80 mL) was added dropwise diphenylphosphoryl azide (8.90 mL...
10.6084/m9.figshare.5104873.v1
null
Carboxylic acid.Secondary amine
Tertiary amide
C1CCNCC1
C1CC[NH]CC1
c1ccccc1.c1ccccc1.C1CC[NH]CC1
HO-
CN(C=O)C
0
2
C1CCNCC1.Cc1ccc(S(=O)(=O)NC(CCCCNC(=O)OCc2ccccc2)C(=O)O)cc1>CN(C=O)C>Cc1ccc(S(=O)(=O)NC(CCCCNC(=O)OCc2ccccc2)C(=O)N2CCCCC2)cc1
ord_dataset-02ee2261663048188cf6d85d2cc96e3f
ord-6b1f0e71dd3a42bb9faf589b927dc731
NCCc1ccc(O)c(O)c1.O=S(=O)(O)CCN1CCN(CCO)CC1.O=S(=O)(O)CCN1CCN(CCO)CC1>>CN1CCC[C@H]1c1cccnc1
C1CN(CCN1CCO)CCS(=O)(=O)O.NCCC1=CC(O)=C(O)C=C1.C1CN(CCN1CCO)CCS(=O)(=O)O.NCCC1=CC(O)=C(O)C=C1>>N1=CC=CC(=C1)[C@H]1N(C)CCC1
N[CH2:5][CH2:6][c:7]1[cH:8][cH:9][c:10](O)c(O)[cH:12]1.O=S(=O)(O)CCN1CC[N:11](CCO)CC1.O=S(=O)(O)CCN1CC[N:2]([CH2:1]CO)[CH2:3][CH2:4]1>>[CH3:1][N:2]1[CH2:3][CH2:4][CH2:5][C@H:6]1[c:7]1[cH:8][cH:9][cH:10][n:11][cH:12]1
NCCc1ccc(O)c(O)c1.O=S(=O)(O)CCN1CCN(CCO)CC1.O=S(=O)(O)CCN1CCN(CCO)CC1
CN1CCC[C@H]1c1cccnc1
null
null
C([C@@H]1[C@H]([C@@H]([C@H]([C@H](O1)O[C@]2([C@H]([C@@H]([C@H](O2)CO)O)O)CO)O)O)O)O
Heteroatom Alkylation and Arylation
OtherReaction
19fc9a872b549396d811b42e2ef2bc61edfc6ad753a9b784038fcb2d26d8bd1b
22424af31acac19f7bdb5717c7b71b423c8772246143962540fd1af6bf911444
c1cncc([C@@H]2CCCN2)c1
N-[CH2;D2;+0:1]-[CH2;D2;+0:2]-[c:3]1:[c:4]:[c:5]:[c;H0;D3;+0:6](-O):c(-O):[cH;D2;+0:7]:1.O-C-C-[N;H0;D3;+0:8]1-C-C-N(-C-C-S(-O)(=O)=O)-C-C-1.O-C-[CH2;D2;+0:9]-[N;H0;D3;+0:10]1-C-C-N(-C-C-S(-O)(=O)=O)-[CH2;D2;+0:11]-[C:12]-1>>[CH3;D1;+0:9]-[N;H0;D3;+0:10]1-[C:12]-[CH2;D2;+0:11]-[CH2;D2;+0:1]-[C@H;D3;+0:2]-1-[c:3]1:[c:4]...
null
[]
null
null
10
MINUTE
Dopamine release was measured by preparing synaptosomes from the striatal area of rat brain obtained from Sprague-Dawley rats generally according to the procedures set forth by Nagy, et al., J. Neurochem., Vol. 43, pp. 1114-1123 (1984). Striata from 4 rats were homogenized in 2 ml of 0.32M sucrose buffered with 5 mM HE...
10.6084/m9.figshare.5104873.v1
null
Primary alcohol.Primary alcohol.Aromatic alcohol.Aromatic alcohol.Primary amine.Tertiary amine.Tertiary amine.Tertiary amine.Tertiary amine.Sulfonic acid.Sulfonic acid
Tertiary amine
c1ccccc1.C1CNCC[NH]1.C1CNCC[NH]1
C1CC[NH]C1.c1ccncc1
C1CC[NH]C1.c1ccncc1
HO-
C([C@@H]1[C@H]([C@@H]([C@H]([C@H](O1)O[C@]2([C@H]([C@@H]([C@H](O2)CO)O)O)CO)O)O)O)O
null
0.166667
NCCc1ccc(O)c(O)c1.O=S(=O)(O)CCN1CCN(CCO)CC1.O=S(=O)(O)CCN1CCN(CCO)CC1>C([C@@H]1[C@H]([C@@H]([C@H]([C@H](O1)O[C@]2([C@H]([C@@H]([C@H](O2)CO)O)O)CO)O)O)O)O>CN1CCC[C@H]1c1cccnc1
ord_dataset-02ee2261663048188cf6d85d2cc96e3f
ord-8e62ba77ab194d9c9cc5595ca51f8d17
COc1ccc(OCc2ccccc2)cc1C(=O)CBr.Oc1cccnc1>>COc1ccc(OCc2ccccc2)cc1C(=O)COc1cccnc1
C(C1=CC=CC=C1)OC=1C=CC(=C(C(CBr)=O)C1)OC.OC=1C=NC=CC1.O.[H-].[Na+]>>N1=CC(=CC=C1)OCC(=O)C1=C(C=CC(=C1)OCC1=CC=CC=C1)OC
Br[CH2:19][C:17]([c:16]1[c:3]([O:2][CH3:1])[cH:4][cH:5][c:6]([O:7][CH2:8][c:9]2[cH:10][cH:11][cH:12][cH:13][cH:14]2)[cH:15]1)=[O:18].[OH:20][c:21]1[cH:22][cH:23][cH:24][n:25][cH:26]1>>[CH3:1][O:2][c:3]1[cH:4][cH:5][c:6]([O:7][CH2:8][c:9]2[cH:10][cH:11][cH:12][cH:13][cH:14]2)[cH:15][c:16]1[C:17](=[O:18])[CH2:19][O:20][c...
COc1ccc(OCc2ccccc2)cc1C(=O)CBr.Oc1cccnc1
COc1ccc(OCc2ccccc2)cc1C(=O)COc1cccnc1
null
null
CN(C=O)C
Heteroatom Alkylation and Arylation
Williamson Ether Synthesis
8060b8e1565497a5ddf79be1adfe74f552b31798797b8841753247b06bdd2051
8749b179916f131d393264a24309227dc6177f560726bed2d1f4567dc2ac63f5
O=C(COc1cccnc1)c1cccc(OCc2ccccc2)c1
Br-[CH2;D2;+0:1]-[C:2](=[O;D1;H0:3])-[c:4].[OH;D1;+0:5]-[c:6](:[c:7]):[c:8]:[#7;a:9]:[c:10]>>[O;D1;H0:3]=[C:2](-[c:4])-[CH2;D2;+0:1]-[O;H0;D2;+0:5]-[c:6](:[c:7]):[c:8]:[#7;a:9]:[c:10]
25.7
[{"value": 25.7, "product": "N1=CC(=CC=C1)OCC(=O)C1=C(C=CC(=C1)OCC1=CC=CC=C1)OC", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
18
HOUR
To 5-benzyloxy-2-methoxyphenacyl bromide (4.0 g, 0.0119 mol) in 80 ml of dry dimethylformamide was added 3-hydroxypyridine (1.24 g, 0.013 mol, 1.1 equiv) followed by NaH (50% in oil, 0.604 g, 1.1 equiv). After stirring for 18 hours under N2, the mixture was poured into 500 ml of ice and water, and extracted 2×500 ml et...
10.6084/m9.figshare.5104873.v1
null
Primary halide.Ketone.Aromatic alcohol
Ketone.Ether
null
null
c1ccccc1.c1ccccc1.c1ccncc1
HBr
CN(C=O)C
null
18
COc1ccc(OCc2ccccc2)cc1C(=O)CBr.Oc1cccnc1>CN(C=O)C>COc1ccc(OCc2ccccc2)cc1C(=O)COc1cccnc1
ord_dataset-02ee2261663048188cf6d85d2cc96e3f
ord-d914eb82cf014fdb8c3669a45bdd545d
COc1ccc(OCc2ccccc2)cc1C(=O)CBr.COc1cccc(O)c1>>COc1cccc(OCC(=O)c2cc(OCc3ccccc3)ccc2OC)c1
COC=1C=C(C=CC1)O.OC=1C=NC=CC1.C(C1=CC=CC=C1)OC=1C=CC(=C(C(CBr)=O)C1)OC>>COC=1C=C(C=CC1)OCC(=O)C1=C(C=CC(=C1)OCC1=CC=CC=C1)OC
Br[CH2:9][C:10](=[O:11])[c:12]1[cH:13][c:14]([O:15][CH2:16][c:17]2[cH:18][cH:19][cH:20][cH:21][cH:22]2)[cH:23][cH:24][c:25]1[O:26][CH3:27].[CH3:1][O:2][c:3]1[cH:4][cH:5][cH:6][c:7]([OH:8])[cH:28]1>>[CH3:1][O:2][c:3]1[cH:4][cH:5][cH:6][c:7]([O:8][CH2:9][C:10](=[O:11])[c:12]2[cH:13][c:14]([O:15][CH2:16][c:17]3[cH:18][cH:...
COc1ccc(OCc2ccccc2)cc1C(=O)CBr.COc1cccc(O)c1
COc1cccc(OCC(=O)c2cc(OCc3ccccc3)ccc2OC)c1
null
null
null
Heteroatom Alkylation and Arylation
Williamson Ether Synthesis
8060b8e1565497a5ddf79be1adfe74f552b31798797b8841753247b06bdd2051
8749b179916f131d393264a24309227dc6177f560726bed2d1f4567dc2ac63f5
O=C(COc1ccccc1)c1cccc(OCc2ccccc2)c1
Br-[CH2;D2;+0:1]-[C:2](=[O;D1;H0:3])-[c:4].[OH;D1;+0:5]-[c:6](:[c:7]):[c:8]>>[O;D1;H0:3]=[C:2](-[c:4])-[CH2;D2;+0:1]-[O;H0;D2;+0:5]-[c:6](:[c:7]):[c:8]
null
[]
null
null
null
null
By the method of Example 1, substituting a molar equivalent of 3-methoxyphenol for 3-hydroxypyridine, 5-benzyloxy-2-methoxyphenacyl bromide was converted to present title product; mp 76°-77° C.; IR (KBr) 1680 cm-1 ; MS 378 (M+); Anal. C 73.05, H 5.74, calcd. C 73.00, H 5.86. Conditions: See reaction.notes.procedure_det...
10.6084/m9.figshare.5104873.v1
null
Primary halide.Ketone.Aromatic alcohol
Ketone.Ether
null
null
c1ccccc1.c1ccccc1.c1ccccc1
HBr
null
null
null
COc1ccc(OCc2ccccc2)cc1C(=O)CBr.COc1cccc(O)c1>>COc1cccc(OCC(=O)c2cc(OCc3ccccc3)ccc2OC)c1
ord_dataset-02ee2261663048188cf6d85d2cc96e3f
ord-b5deb4b9277448c289c6682e2181b440
CC(=O)c1cccc(OCc2ccccc2)c1.O=Cc1cccnc1>>O=C(C=Cc1cccnc1)c1ccccc1OCc1ccccc1
N1=CC(=CC=C1)C=O.CC(=O)C1=CC(=CC=C1)OCC2=CC=CC=C2.[OH-].[Na+].C(C)O>>C(C1=CC=CC=C1)OC1=C(C=CC=C1)C(C=CC=1C=NC=CC1)=O
[O:1]=[C:2]([CH3:3])[c:11]1[cH:12][cH:13][cH:14][c:16]([O:17][CH2:18][c:19]2[cH:20][cH:21][cH:22][cH:23][cH:24]2)[cH:15]1.O=[CH:4][c:5]1[cH:6][cH:7][cH:8][n:9][cH:10]1>>[O:1]=[C:2]([CH:3]=[CH:4][c:5]1[cH:6][cH:7][cH:8][n:9][cH:10]1)[c:11]1[cH:12][cH:13][cH:14][cH:15][c:16]1[O:17][CH2:18][c:19]1[cH:20][cH:21][cH:22][cH:...
CC(=O)c1cccc(OCc2ccccc2)c1.O=Cc1cccnc1
O=C(C=Cc1cccnc1)c1ccccc1OCc1ccccc1
null
null
O
C-C Coupling
OtherReaction
9fff1ed552b676da41a76495351538077f3ef1283fc0ddc29dc8ab32ab8f15a5
21d425db6b546152ab81006f738d4037a554ffa9ba484cf666f8f3284e58e404
O=C(C=Cc1cccnc1)c1ccccc1OCc1ccccc1
O=[CH;D2;+0:1]-[c:2](:[c:3]):[c:4]:[#7;a:5]:[c:6].[C:7]-[#8:8]-[c;H0;D3;+0:9]1:[cH;D2;+0:10]:[c:11]:[c:12]:[c;H0;D3;+0:13](-[C:14](-[CH3;D1;+0:15])=[O;D1;H0:16]):[cH;D2;+0:17]:1>>[C:7]-[#8:8]-[c;H0;D3;+0:9]1:[cH;D2;+0:17]:[cH;D2;+0:10]:[c:11]:[c:12]:[c;H0;D3;+0:13]:1-[C:14](=[O;D1;H0:16])-[CH;D2;+0:15]=[CH;D2;+0:1]-[c:...
null
[]
null
null
18
HOUR
To a solution of NaOH (0.488 g) in 10 ml of H2O was added 5 ml of 95% ethanol, followed by 3-benzyloxyacetophenone (2.5 g). The resulting solution was cooled to 0°-5° C. and pyridine-3-carbaldehyde (0.903 ml) added. After standing at 0°-5° C. for 18 hours, present title product was recovered by filtration and purified ...
10.6084/m9.figshare.5104873.v1
null
Aldehyde.Ketone.Ether
Ketone.Ether
c1ccccc1
c1ccccc1
c1ccncc1.c1ccccc1.c1ccccc1
HO-
O
null
18
CC(=O)c1cccc(OCc2ccccc2)c1.O=Cc1cccnc1>O>O=C(C=Cc1cccnc1)c1ccccc1OCc1ccccc1
ord_dataset-02ee2261663048188cf6d85d2cc96e3f
ord-02e63018c7f6403a9ad3b2d6de31b313
CC(=O)c1cccc(OCc2ccccc2)c1.COC(=O)c1cccc(C=O)c1>>COC(=O)c1cccc(C=CC(=O)c2cccc(OCc3ccccc3)c2)c1
C(C)(=O)O.CC(=O)C1=CC(=CC=C1)OCC2=CC=CC=C2.C(=O)C=1C=C(C(=O)OC)C=CC1.CO[Na]>>C(C1=CC=CC=C1)OC=1C=C(C=CC1)C(C=CC1=CC(=CC=C1)C(=O)OC)=O
[CH3:11][C:12](=[O:13])[c:14]1[cH:15][cH:16][cH:17][c:18]([O:19][CH2:20][c:21]2[cH:22][cH:23][cH:24][cH:25][cH:26]2)[cH:27]1.O=[CH:10][c:9]1[cH:8][cH:7][cH:6][c:5]([C:3]([O:2][CH3:1])=[O:4])[cH:28]1>>[CH3:1][O:2][C:3](=[O:4])[c:5]1[cH:6][cH:7][cH:8][c:9]([CH:10]=[CH:11][C:12](=[O:13])[c:14]2[cH:15][cH:16][cH:17][c:18](...
CC(=O)c1cccc(OCc2ccccc2)c1.COC(=O)c1cccc(C=O)c1
COC(=O)c1cccc(C=CC(=O)c2cccc(OCc3ccccc3)c2)c1
null
null
CO.O
C-C Coupling
Aldehyde and ketone to alpha,beta-unsaturated carbonyl
df1bdbab1a06af9561d74fe6bc94ee8bda1d14faad9db1ada3a214bd64a24cf8
c93e93ada40f7f922a54fe24d38f540ecf5ff25d55d497f79f5f400f75d0c7ae
O=C(C=Cc1ccccc1)c1cccc(OCc2ccccc2)c1
O=[CH;D2;+0:1]-[c:2](:[c:3]):[c:4].[CH3;D1;+0:5]-[C:6](=[O;D1;H0:7])-[c:8]>>[O;D1;H0:7]=[C:6](-[c:8])-[CH;D2;+0:5]=[CH;D2;+0:1]-[c:2](:[c:3]):[c:4]
null
[]
null
null
18
HOUR
To CH3ONa (0.45 g, 0.0082 mol) stirring in 20 ml of dry CH3OH at 10° C. was added 3-benzyloxyacetophenone (5.0 g, 0.019 mol) and methyl 3-formylbenzoate (3.12 g, 0.019 mol). A heavy precipitate formed almost immediately, and the mixture was diluted with 20 ml CH3OH, warmed to room temperature and stirred for 18 hours. ...
10.6084/m9.figshare.5104873.v1
null
Aldehyde.Ketone
Ketone
null
null
c1ccccc1.c1ccccc1.c1ccccc1
HO-
CO.O
null
18
CC(=O)c1cccc(OCc2ccccc2)c1.COC(=O)c1cccc(C=O)c1>CO.O>COC(=O)c1cccc(C=CC(=O)c2cccc(OCc3ccccc3)c2)c1
ord_dataset-02ee2261663048188cf6d85d2cc96e3f
ord-cb967cd9eaa84622bff0d06681a8f931
CCOC(=O)c1cc2cc(N)ccc2s1.O=C(O)c1cc2cc([N+](=O)[O-])ccc2o1>>CCOC(=O)c1cc2cc(N)ccc2o1
[N+](=O)([O-])C=1C=CC2=C(C=C(O2)C(=O)O)C1.NC=1C=CC2=C(C=C(S2)C(=O)OCC)C1>>NC=1C=CC2=C(C=C(O2)C(=O)OCC)C1
Nc1ccc2sc([C:4]([O:3][CH2:2][CH3:1])=[O:5])cc2c1.O=C(O)[c:6]1[cH:7][c:8]2[cH:9][c:10]([N+:11](=O)[O-])[cH:12][cH:13][c:14]2[o:15]1>>[CH3:1][CH2:2][O:3][C:4](=[O:5])[c:6]1[cH:7][c:8]2[cH:9][c:10]([NH2:11])[cH:12][cH:13][c:14]2[o:15]1
CCOC(=O)c1cc2cc(N)ccc2s1.O=C(O)c1cc2cc([N+](=O)[O-])ccc2o1
CCOC(=O)c1cc2cc(N)ccc2o1
null
null
null
Functional Group Interconversion
OtherReaction
6730e883247c168fcd3cda868e87253b047ed8e691a4c4fd4ce9586e7a554631
72229b1116248466325a77b051119920514293961507228730ef3aee179224a8
c1ccc2occc2c1
N-c1:c:c:c2:s:c(-[C;H0;D3;+0:1](=[O;D1;H0:2])-[#8:3]-[C:4]):c:c:2:c:1.O-C(=O)-[c;H0;D3;+0:5]1:[#8;a:6]:[c:7]:[c:8](:[c:9]:1):[c:10]:[c:11](-[N+;H0;D3:12](=O)-[O-]):[c:13]>>[C:4]-[#8:3]-[C;H0;D3;+0:1](=[O;D1;H0:2])-[c;H0;D3;+0:5]1:[#8;a:6]:[c:7]:[c:8](:[c:9]:1):[c:10]:[c:11](-[NH2;D1;+0:12]):[c:13]
null
[]
null
null
null
null
The appropriate arylcarboxylic acid is synthesized by the coupling of indole-2-carboxylic acid, benzofuran-2-carboxylic acid or benzothiophene-2-carboxylic acid with ethyl 5-amino-aryl-2-carboxylate in DMF with EDCI, and saponification of the ester. Ethyl 5-aminoindole-2-carboxylate is formed by catalytic hydrogenation...
10.6084/m9.figshare.5104873.v1
null
Carboxylic acid.Ester.Nitro group.Primary amine
Ester.Primary amine
c1ccc2sccc2c1.c1ccc2occc2c1
c1ccc2occc2c1
c1ccc2occc2c1
Other
null
null
null
CCOC(=O)c1cc2cc(N)ccc2s1.O=C(O)c1cc2cc([N+](=O)[O-])ccc2o1>>CCOC(=O)c1cc2cc(N)ccc2o1
ord_dataset-02ee2261663048188cf6d85d2cc96e3f
ord-3aa3f09df1fc4b0da83e26f362069cf6
ClCCl>>Cl
[OH-].[Na+].C(Cl)Cl.O.CN[C@H]1CC[C@H](C2=C1C=CC=C2)C=3C=CC(=C(C3)Cl)Cl.C(C(O)C1=CC=CC=C1)(=O)[O-]>>CN[C@H]1CC[C@H](C2=C1C=CC=C2)C=3C=CC(=C(C3)Cl)Cl.Cl
ClC[Cl:21]>>[ClH:21]
ClCCl
Cl
null
null
C(C)(C)O
Miscellaneous
OtherReaction
64e2f1d14467658fcb89f1934b11f73bcbe5aab8b019240f858e5d4d92949b50
65e22ac5ac73e4dc94c17b99f93076354fa5a281d80003bd5a6c5af277cafff7
null
Cl-C-[Cl;H0;D1;+0:1]>>[ClH;D0;+0:1]
null
[]
50
CELSIUS
3
HOUR
To a 12 liter, 3 neck round-bottom flask equipped with mechanical stirrer, 4287ml of methylene chloride, 2553ml water and 638.3gms sertraline mandelate were combined. A 10% sodium hydroxide solution, 383ml, was then added and the resulting two clear layers were separated. The aqueous layer was further extracted with 2×...
10.6084/m9.figshare.5104873.v1
null
Primary halide.Primary halide
null
null
null
null
HCl
C(C)(C)O
50
3
ClCCl>C(C)(C)O>Cl
ord_dataset-02ee2261663048188cf6d85d2cc96e3f
ord-f88643d947a34b82bf524f131968accd
C#CCCCOC.NS(=O)(=O)c1ccccc1I>>COCCCC#Cc1ccccc1S(N)(=O)=O
IC1=C(C=CC=C1)S(=O)(=O)N.C(CCC#C)OC.CN(C=O)C>>COCCCC#CC1=C(C=CC=C1)S(=O)(=O)N
[CH3:1][O:2][CH2:3][CH2:4][CH2:5][C:6]#[CH:7].I[c:8]1[cH:9][cH:10][cH:11][cH:12][c:13]1[S:14]([NH2:15])(=[O:16])=[O:17]>>[CH3:1][O:2][CH2:3][CH2:4][CH2:5][C:6]#[C:7][c:8]1[cH:9][cH:10][cH:11][cH:12][c:13]1[S:14]([NH2:15])(=[O:16])=[O:17]
C#CCCCOC.NS(=O)(=O)c1ccccc1I
COCCCC#Cc1ccccc1S(N)(=O)=O
null
[Cu]I.Cl[Pd]([P](C1=CC=CC=C1)(C2=CC=CC=C2)C3=CC=CC=C3)([P](C4=CC=CC=C4)(C5=CC=CC=C5)C6=CC=CC=C6)Cl
C(C)N(CC)CC
C-C Coupling
Sonogashira alkyne_aryl halide
15c08902746c61a960c314898ce6bb5fcc5e189f9e057388c59dba9ec9d0c81c
305eca0fd2975da49e7f69e4edfb9dc1cbce82513954bc5a73be3289e70e5f76
c1ccccc1
I-[c;H0;D3;+0:1](:[c:2]:[c:3]):[c:4](-[#16:5]):[c:6].[C:7]-[C:8]#[CH;D1;+0:9]>>[#16:5]-[c:4](:[c:6]):[c;H0;D3;+0:1](-[C;H0;D2;+0:9]#[C:8]-[C:7]):[c:2]:[c:3]
null
[]
null
null
22
HOUR
135 ml of N,N-dimethylformamide and 22 ml of triethylamine are taken and 7.5 g of 2-iodobenzenesulfonamide, 2.6 g of pent-4-yn-1-yl-methyl ether as well as 0.067 g of copper(I) iodide and 0.144 g of bis(triphenylphosphine)palladium(II) dichloride are added. The reaction mixture is heated to 65° and stirred for 22 hours...
10.6084/m9.figshare.5104873.v1
null
Aromatic halide.Alkyne
Alkyne
c1ccccc1
c1ccccc1
c1ccccc1
HI
[Cu]I.Cl[Pd]([P](C1=CC=CC=C1)(C2=CC=CC=C2)C3=CC=CC=C3)([P](C4=CC=CC=C4)(C5=CC=CC=C5)C6=CC=CC=C6)Cl.C(C)N(CC)CC
null
22
C#CCCCOC.NS(=O)(=O)c1ccccc1I>[Cu]I.Cl[Pd]([P](C1=CC=CC=C1)(C2=CC=CC=C2)C3=CC=CC=C3)([P](C4=CC=CC=C4)(C5=CC=CC=C5)C6=CC=CC=C6)Cl.C(C)N(CC)CC>COCCCC#Cc1ccccc1S(N)(=O)=O
ord_dataset-02ee2261663048188cf6d85d2cc96e3f
ord-c34b896f8df643aab6bb098bc5e91b2c
C#CCC.NS(=O)(=O)c1ccccc1I>>CCC#Cc1ccccc1S(N)(=O)=O
IC1=C(C=CC=C1)S(=O)(=O)N.C(C)N(CC)CC.IC1=C(C=CC=C1)S(=O)(=O)N.C#CCC>>C(#CCC)C1=C(C=CC=C1)S(=O)(=O)N
[CH3:1][CH2:2][C:3]#[CH:4].I[c:5]1[cH:6][cH:7][cH:8][cH:9][c:10]1[S:11]([NH2:12])(=[O:13])=[O:14]>>[CH3:1][CH2:2][C:3]#[C:4][c:5]1[cH:6][cH:7][cH:8][cH:9][c:10]1[S:11]([NH2:12])(=[O:13])=[O:14]
C#CCC.NS(=O)(=O)c1ccccc1I
CCC#Cc1ccccc1S(N)(=O)=O
null
Cl[Pd]([P](C1=CC=CC=C1)(C2=CC=CC=C2)C3=CC=CC=C3)([P](C4=CC=CC=C4)(C5=CC=CC=C5)C6=CC=CC=C6)Cl.[Cu](I)I
CN(C=O)C
C-C Coupling
Sonogashira alkyne_aryl halide
15c08902746c61a960c314898ce6bb5fcc5e189f9e057388c59dba9ec9d0c81c
305eca0fd2975da49e7f69e4edfb9dc1cbce82513954bc5a73be3289e70e5f76
c1ccccc1
I-[c;H0;D3;+0:1](:[c:2]:[c:3]):[c:4](-[#16:5]):[c:6].[C:7]-[C:8]#[CH;D1;+0:9]>>[#16:5]-[c:4](:[c:6]):[c;H0;D3;+0:1](-[C;H0;D2;+0:9]#[C:8]-[C:7]):[c:2]:[c:3]
null
[]
null
null
18
HOUR
0.1 g of bis(triphenylphosphine)palladium(II) chloride, 0.05 g of copper iodide and 18.5 ml of triethylamine are added to a solution of 5 g of 2-iodobenzenesulfonamide in 70 ml of N,N-dimethylformamide. At room temperature, argon and 1-butyne are slowly introduced. After 18 hours the thin-layer chromatogram no longer s...
10.6084/m9.figshare.5104873.v1
null
Aromatic halide.Alkyne
Alkyne
c1ccccc1
c1ccccc1
c1ccccc1
HI
Cl[Pd]([P](C1=CC=CC=C1)(C2=CC=CC=C2)C3=CC=CC=C3)([P](C4=CC=CC=C4)(C5=CC=CC=C5)C6=CC=CC=C6)Cl.[Cu](I)I.CN(C=O)C
null
18
C#CCC.NS(=O)(=O)c1ccccc1I>Cl[Pd]([P](C1=CC=CC=C1)(C2=CC=CC=C2)C3=CC=CC=C3)([P](C4=CC=CC=C4)(C5=CC=CC=C5)C6=CC=CC=C6)Cl.[Cu](I)I.CN(C=O)C>CCC#Cc1ccccc1S(N)(=O)=O
ord_dataset-02ee2261663048188cf6d85d2cc96e3f
ord-e6a9ee111b684577b5ee1b441df9ca2a
CC(=O)Cl.NS(=O)(=O)c1ccccc1C#CCCCO>>CC(=O)OCCCC#Cc1ccccc1S(N)(=O)=O
OCCCC#CC1=C(C=CC=C1)S(=O)(=O)N.N1=CC=CC=C1.C(C)(=O)Cl.C(C)N(CC)CC>>C(C)(=O)OCCCC#CC1=C(C=CC=C1)S(=O)(=O)N
Cl[C:2]([CH3:1])=[O:3].[OH:4][CH2:5][CH2:6][CH2:7][C:8]#[C:9][c:10]1[cH:11][cH:12][cH:13][cH:14][c:15]1[S:16]([NH2:17])(=[O:18])=[O:19]>>[CH3:1][C:2](=[O:3])[O:4][CH2:5][CH2:6][CH2:7][C:8]#[C:9][c:10]1[cH:11][cH:12][cH:13][cH:14][c:15]1[S:16]([NH2:17])(=[O:18])=[O:19]
CC(=O)Cl.NS(=O)(=O)c1ccccc1C#CCCCO
CC(=O)OCCCC#Cc1ccccc1S(N)(=O)=O
null
null
C1=CC=CC=C1
Acylation
Schotten-Baumann to ester
6cefe709828c5bd4655f254e75d5dff9e8876e192e7dd47256c1bc0067bc5291
d8a7643b81ed07a6f633aa99465180dfa0565e61ae25aef36338ebb9837c9cef
c1ccccc1
Cl-[C;H0;D3;+0:1](-[C;D1;H3:2])=[O;D1;H0:3].[C:4]-[C:5]-[OH;D1;+0:6]>>[C:4]-[C:5]-[O;H0;D2;+0:6]-[C;H0;D3;+0:1](-[C;D1;H3:2])=[O;D1;H0:3]
null
[]
null
null
1
HOUR
The starting material and analogous starting material may be prepared as follows: 3.0 g of 2-(5-hydroxypent-1-yn-1-yl)-benzenesulfonamide and 4.7 ml of pyridine are dissolved at 45° in 200 ml of benzene. The solution is cooled to room temperature and 1.23 ml of acetyl chloride and 3.2 ml of triethylamine are added. The...
10.6084/m9.figshare.5104873.v1
null
Acyl halide.Primary alcohol
Ester
null
null
c1ccccc1
HCl
C1=CC=CC=C1
null
1
CC(=O)Cl.NS(=O)(=O)c1ccccc1C#CCCCO>C1=CC=CC=C1>CC(=O)OCCCC#Cc1ccccc1S(N)(=O)=O
ord_dataset-02ee2261663048188cf6d85d2cc96e3f
ord-855ec966bfce4a599c81dfe20ff188e7
CC(=O)OC(C)=O.CC(O)CC#Cc1ccccc1S(N)(=O)=O>>CC(=O)OC(C)CC#Cc1ccccc1S(N)(=O)=O
OC(CC#CC1=C(C=CC=C1)S(=O)(=O)N)C.C(C)(=O)OC(C)=O>>C(C)(=O)OC(CC#CC1=C(C=CC=C1)S(=O)(=O)N)C
CC(=O)O[C:2]([CH3:1])=[O:3].[OH:4][CH:5]([CH3:6])[CH2:7][C:8]#[C:9][c:10]1[cH:11][cH:12][cH:13][cH:14][c:15]1[S:16]([NH2:17])(=[O:18])=[O:19]>>[CH3:1][C:2](=[O:3])[O:4][CH:5]([CH3:6])[CH2:7][C:8]#[C:9][c:10]1[cH:11][cH:12][cH:13][cH:14][c:15]1[S:16]([NH2:17])(=[O:18])=[O:19]
CC(=O)OC(C)=O.CC(O)CC#Cc1ccccc1S(N)(=O)=O
CC(=O)OC(C)CC#Cc1ccccc1S(N)(=O)=O
null
null
N1=CC=CC=C1
Acylation
Transesterification
a7ad17dd333d7246e42d4632a0a7042db0b0d3b7f2adb7cdb2c46498a22ac4db
c98fee24664998fb42388f3a4804f79d763c5043c4f5565ea3b46913e3a86a6e
c1ccccc1
C-C(=O)-O-[C;H0;D3;+0:1](-[C;D1;H3:2])=[O;D1;H0:3].[C:4]#[C:5]-[C:6]-[C:7](-[C;D1;H3:8])-[OH;D1;+0:9]>>[C:4]#[C:5]-[C:6]-[C:7](-[C;D1;H3:8])-[O;H0;D2;+0:9]-[C;H0;D3;+0:1](-[C;D1;H3:2])=[O;D1;H0:3]
null
[]
null
null
14
HOUR
1 g of 2-(4-hydroxy-pent-1-yn-1-yl)-benzenesulfonamide is dissolved in 9 ml of pyridine and cooled to 5°, and 0.44 ml of acetic anhydride is added. The reaction mixture is stirred under argon at 5° for 14 hours and then at room temperature for a further 24 hours. The reaction mixture is then poured onto 100 ml of ice-c...
10.6084/m9.figshare.5104873.v1
null
Anhydride.Secondary alcohol
Ester
null
null
c1ccccc1
HO-
N1=CC=CC=C1
null
14
CC(=O)OC(C)=O.CC(O)CC#Cc1ccccc1S(N)(=O)=O>N1=CC=CC=C1>CC(=O)OC(C)CC#Cc1ccccc1S(N)(=O)=O
ord_dataset-02ee2261663048188cf6d85d2cc96e3f
ord-a86cb8e6d2cf4b918a68d5f5c49a6347
COc1cc(C(=O)NS(=O)(=O)c2ccccc2C#CCCCOC(C)=O)ccc1Cc1cn(C)c2ccc(NC(=O)OC3CCCC3)cc12>>COc1cc(C(=O)NS(=O)(=O)c2ccccc2C#CCCCO)ccc1Cc1cn(C)c2ccc(NC(=O)OC3CCCC3)cc12
O.[OH-].[Li+].O.C1(CCCC1)OC(=O)NC=1C=C2C(=CN(C2=CC1)C)CC1=C(C=C(C(=O)NS(=O)(=O)C2=C(C=CC=C2)C#CCCCOC(C)=O)C=C1)OC>>C1(CCCC1)OC(=O)NC=1C=C2C(=CN(C2=CC1)C)CC1=C(C=C(C(=O)NS(=O)(=O)C2=C(C=CC=C2)C#CCCCO)C=C1)OC
CC(=O)[O:23][CH2:22][CH2:21][CH2:20][C:19]#[C:18][c:17]1[c:12]([S:9]([NH:8][C:6]([c:5]2[cH:4][c:3]([O:2][CH3:1])[c:26]([CH2:27][c:28]3[cH:29][n:30]([CH3:31])[c:32]4[cH:33][cH:34][c:35]([NH:36][C:37](=[O:38])[O:39][CH:40]5[CH2:41][CH2:42][CH2:43][CH2:44]5)[cH:45][c:46]34)[cH:25][cH:24]2)=[O:7])(=[O:10])=[O:11])[cH:13][c...
COc1cc(C(=O)NS(=O)(=O)c2ccccc2C#CCCCOC(C)=O)ccc1Cc1cn(C)c2ccc(NC(=O)OC3CCCC3)cc12
COc1cc(C(=O)NS(=O)(=O)c2ccccc2C#CCCCO)ccc1Cc1cn(C)c2ccc(NC(=O)OC3CCCC3)cc12
null
null
CO.O1CCCC1
Reduction
Hydrolysis or Hydrogenolysis of Carboxylic Esters or Thioesters
21d61543c6ec8a8cebe1b3ef55ef3dd20acbf79a4f1c12a7fb51e32be7a3248a
1fbcd628a0426673c5d10aa49a977cd2d1ae02a8cdf57bbb10d94aa03a94e937
O=C(Nc1ccc2[nH]cc(Cc3ccc(C(=O)NS(=O)(=O)c4ccccc4)cc3)c2c1)OC1CCCC1
C-C(=O)-[O;H0;D2;+0:1]-[C:2]-[C:3]>>[C:3]-[C:2]-[OH;D1;+0:1]
97.7
[{"value": 97.7, "product": "C1(CCCC1)OC(=O)NC=1C=C2C(=CN(C2=CC1)C)CC1=C(C=C(C(=O)NS(=O)(=O)C2=C(C=CC=C2)C#CCCCO)C=C1)OC", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
16
HOUR
0.37 g of lithium hydroxide monohydrate and 10 ml of water are added to a solution of 1.2 g of N-[4-[5-(cyclopentyloxycarbonylamino)-1-methyl-indol-3-yl-methyl]-3-methoxybenzoyl]-2-(5-acetoxy-pent-1-yn-1-yl)-benzenesulfonamide in 40 ml of methanol/tetrahydrofuran=1/1. The mixture is stirred for 16 hours at room tempera...
10.6084/m9.figshare.5104873.v1
null
Ester
Primary alcohol
null
null
c1ccccc1.c1ccccc1.c1ccc2[nH]ccc2c1.C1CCCC1
HO-
CO.O1CCCC1
null
16
COc1cc(C(=O)NS(=O)(=O)c2ccccc2C#CCCCOC(C)=O)ccc1Cc1cn(C)c2ccc(NC(=O)OC3CCCC3)cc12>CO.O1CCCC1>COc1cc(C(=O)NS(=O)(=O)c2ccccc2C#CCCCO)ccc1Cc1cn(C)c2ccc(NC(=O)OC3CCCC3)cc12
ord_dataset-02ee2261663048188cf6d85d2cc96e3f
ord-a0f180715a4a474e864218093f7ef149
CC(=O)OC(C)=O.COc1cc(C(=O)NS(=O)(=O)c2ccccc2C#CC(C)(C)O)ccc1Cc1cn(C)c2ccc(NC(=O)OC3CCCC3)cc12>>COc1cc(C(=O)NS(=O)(=O)c2ccccc2C#CC(C)(C)OC(C)=O)ccc1Cc1cn(C)c2ccc(NC(=O)OC3CCCC3)cc12
C(C)(=O)OC(C)=O.C1(CCCC1)OC(=O)NC=1C=C2C(=CN(C2=CC1)C)CC1=C(C=C(C(=O)NS(=O)(=O)C2=C(C=CC=C2)C#CC(C)(C)O)C=C1)OC>>C1(CCCC1)OC(=O)NC=1C=C2C(=CN(C2=CC1)C)CC1=C(C=C(C(=O)NS(=O)(=O)C2=C(C=CC=C2)C#CC(C)(C)OC(C)=O)C=C1)OC
CC(=O)O[C:24]([CH3:25])=[O:26].[CH3:1][O:2][c:3]1[cH:4][c:5]([C:6](=[O:7])[NH:8][S:9](=[O:10])(=[O:11])[c:12]2[cH:13][cH:14][cH:15][cH:16][c:17]2[C:18]#[C:19][C:20]([CH3:21])([CH3:22])[OH:23])[cH:27][cH:28][c:29]1[CH2:30][c:31]1[cH:32][n:33]([CH3:34])[c:35]2[cH:36][cH:37][c:38]([NH:39][C:40](=[O:41])[O:42][CH:43]3[CH2:...
CC(=O)OC(C)=O.COc1cc(C(=O)NS(=O)(=O)c2ccccc2C#CC(C)(C)O)ccc1Cc1cn(C)c2ccc(NC(=O)OC3CCCC3)cc12
COc1cc(C(=O)NS(=O)(=O)c2ccccc2C#CC(C)(C)OC(C)=O)ccc1Cc1cn(C)c2ccc(NC(=O)OC3CCCC3)cc12
null
CN(C1=CC=NC=C1)C
N1=CC=CC=C1.C(C)(=O)OCC
Acylation
Transesterification
7845e6caeb9ebcfc4e11ccde0ca862e171727c1b0b0f5c55f250826811ed7095
aad6c0b0b2e56c19696d13bcd56b340e680e45229f4a56b765d97baaf778738e
O=C(Nc1ccc2[nH]cc(Cc3ccc(C(=O)NS(=O)(=O)c4ccccc4)cc3)c2c1)OC1CCCC1
C-C(=O)-O-[C;H0;D3;+0:1](-[C;D1;H3:2])=[O;D1;H0:3].[C;D1;H3:4]-[C:5](-[C;D1;H3:6])(-[OH;D1;+0:7])-[C:8]#[C:9]-[c:10]>>[C;D1;H3:4]-[C:5](-[C;D1;H3:6])(-[C:8]#[C:9]-[c:10])-[O;H0;D2;+0:7]-[C;H0;D3;+0:1](-[C;D1;H3:2])=[O;D1;H0:3]
null
[]
null
null
20
HOUR
0.44 g of acetic anhydride and 0.1 g of 4-dimethylaminopyridine are added to a solution of 1.0 g of N-[4-[5-(cyclopentyloxycarbonylamino)-1-methyl-indol-3-yl-methyl]-3-methoxybenzoyl]-2-(3-hydroxy-3-methyl-but-1-yn-1-yl)-benzenesulfonamide in 6 ml of pyridine. The reaction solution is stirred for 20 hours at room tempe...
10.6084/m9.figshare.5104873.v1
null
Anhydride.Tertiary alcohol
Ester
null
null
c1ccccc1.c1ccccc1.c1ccc2[nH]ccc2c1.C1CCCC1
HO-
CN(C1=CC=NC=C1)C.N1=CC=CC=C1.C(C)(=O)OCC
null
20
CC(=O)OC(C)=O.COc1cc(C(=O)NS(=O)(=O)c2ccccc2C#CC(C)(C)O)ccc1Cc1cn(C)c2ccc(NC(=O)OC3CCCC3)cc12>CN(C1=CC=NC=C1)C.N1=CC=CC=C1.C(C)(=O)OCC>COc1cc(C(=O)NS(=O)(=O)c2ccccc2C#CC(C)(C)OC(C)=O)ccc1Cc1cn(C)c2ccc(NC(=O)OC3CCCC3)cc12
ord_dataset-02ee2261663048188cf6d85d2cc96e3f
ord-6fd576943ae3459bb74deb1e7f415740
CCCC#Cc1ccccc1S(N)(=O)=O.COc1cc(C(=O)O)ccc1Cc1cn(C)c2ccc(NC(=O)OC3CCCC3)cc12>>CCCC#Cc1ccccc1S(=O)(=O)NC(=O)c1ccc(Cc2cn(C)c3ccc(NC(=O)OC4CCCC4)cc23)c(OC)c1
C(#CCCC)C1=C(C=CC=C1)S(=O)(=O)N.C1(CCCC1)OC(=O)NC=1C=C2C(=CN(C2=CC1)C)CC1=C(C=C(C(=O)O)C=C1)OC>>C1(CCCC1)OC(=O)NC=1C=C2C(=CN(C2=CC1)C)CC1=C(C=C(C(=O)NS(=O)(=O)C2=C(C=CC=C2)C#CCCC)C=C1)OC
[CH3:1][CH2:2][CH2:3][C:4]#[C:5][c:6]1[cH:7][cH:8][cH:9][cH:10][c:11]1[S:12](=[O:13])(=[O:14])[NH2:15].O[C:16](=[O:17])[c:18]1[cH:19][cH:20][c:21]([CH2:22][c:23]2[cH:24][n:25]([CH3:26])[c:27]3[cH:28][cH:29][c:30]([NH:31][C:32](=[O:33])[O:34][CH:35]4[CH2:36][CH2:37][CH2:38][CH2:39]4)[cH:40][c:41]23)[c:42]([O:43][CH3:44]...
CCCC#Cc1ccccc1S(N)(=O)=O.COc1cc(C(=O)O)ccc1Cc1cn(C)c2ccc(NC(=O)OC3CCCC3)cc12
CCCC#Cc1ccccc1S(=O)(=O)NC(=O)c1ccc(Cc2cn(C)c3ccc(NC(=O)OC4CCCC4)cc23)c(OC)c1
null
CN(C1=CC=NC=C1)C
C(Cl)Cl
Acylation
Carboxylic acid with primary amine to amide
195a412a8235704efe2985cdc18467ba661e632bab7b61944399ecc813e32a09
5e4665bad9c6f58dddd98c5f95e436c640b4c0118b04efea5cd58c7d1755401d
O=C(Nc1ccc2[nH]cc(Cc3ccc(C(=O)NS(=O)(=O)c4ccccc4)cc3)c2c1)OC1CCCC1
O-[C;H0;D3;+0:1](=[O;D1;H0:2])-[c:3](:[c:4]):[c:5].[NH2;D1;+0:6]-[#16:7](=[O;D1;H0:8])(=[O;D1;H0:9])-[c:10]>>[O;D1;H0:8]=[#16:7](=[O;D1;H0:9])(-[c:10])-[NH;D2;+0:6]-[C;H0;D3;+0:1](=[O;D1;H0:2])-[c:3](:[c:4]):[c:5]
74
[{"value": 74.0, "product": "C1(CCCC1)OC(=O)NC=1C=C2C(=CN(C2=CC1)C)CC1=C(C=C(C(=O)NS(=O)(=O)C2=C(C=CC=C2)C#CCCC)C=C1)OC", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
20
HOUR
1.07 g of 2-(pent-1-yn-1-yl)-benzenesulfonamide and 0.94 g of 3-[N-dimethylaminopropyl]-N-ethylcarbodiimide hydrochloride as well as 0.6 g of 4-dimethylaminopyridine are added to a solution of 2.0 g of 4-[5-(cyclopentyloxycarbonylamino)-1-methyl-indol-3-yl-methyl]-3-methoxy-benzoic acid in 50 ml of methylene chloride. ...
10.6084/m9.figshare.5104873.v1
null
Sulfonamide.Carboxylic acid
Sulfonamide.Secondary amide
null
null
c1ccccc1.c1ccccc1.c1ccc2[nH]ccc2c1.C1CCCC1
HO-
CN(C1=CC=NC=C1)C.C(Cl)Cl
null
20
CCCC#Cc1ccccc1S(N)(=O)=O.COc1cc(C(=O)O)ccc1Cc1cn(C)c2ccc(NC(=O)OC3CCCC3)cc12>CN(C1=CC=NC=C1)C.C(Cl)Cl>CCCC#Cc1ccccc1S(=O)(=O)NC(=O)c1ccc(Cc2cn(C)c3ccc(NC(=O)OC4CCCC4)cc23)c(OC)c1
ord_dataset-02ee2261663048188cf6d85d2cc96e3f
ord-324cff6c10c54f0e868e67759e4a7ad4
O=CCc1ccccc1.SCCCS>>c1ccc(CC2SCCCS2)cc1
[OH-].[K+].C1(=CC=CC=C1)CC=O.C(CCS)S.B(F)(F)F.CCOCC>>C1(=CC=CC=C1)CC1SCCCS1
O=[CH:6][CH2:5][c:4]1[cH:3][cH:2][cH:1][cH:13][cH:12]1.[SH:7][CH2:8][CH2:9][CH2:10][SH:11]>>[cH:1]1[cH:2][cH:3][c:4]([CH2:5][CH:6]2[S:7][CH2:8][CH2:9][CH2:10][S:11]2)[cH:12][cH:13]1
O=CCc1ccccc1.SCCCS
c1ccc(CC2SCCCS2)cc1
null
null
C(Cl)Cl
Heteroatom Alkylation and Arylation
OtherReaction
b6aa94cc288ccc335d16ebca7b7871ddfb2ace95135c953bbcca74128ef9ab0d
b33952daa52c823aed54928e18035128d6174ef232f045e0b3aec8d00e876322
c1ccc(CC2SCCCS2)cc1
O=[CH;D2;+0:1]-[C:2]-[c:3].[SH;D1;+0:4]-[C:5]-[C:6]-[C:7]-[SH;D1;+0:8]>>[c:3]-[C:2]-[CH;D3;+0:1]1-[S;H0;D2;+0:4]-[C:5]-[C:6]-[C:7]-[S;H0;D2;+0:8]-1
91
[{"value": 91.0, "product": "C1(=CC=CC=C1)CC1SCCCS1", "details": "PERCENTYIELD", "is_desired": false}, {"value": 91.0, "product": "C1(=CC=CC=C1)CC1SCCCS1", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
3
HOUR
To a solution of 33.9 g (280 mmol) of phenylacetaldehyde and 35.6 g (330 mmol) of 1,3-propanedithiol in 300 mL of methylene chloride at 0° C., was added, dropwise over a period of 30 minutes, 10 mL of boron trifluoride etherate. The reaction mixture was allowed to warm to ambient temperature and stirred for 3 h at ambi...
10.6084/m9.figshare.5104873.v1
null
Aldehyde.Aliphatic thiol.Aliphatic thiol
Monosulfide.Monosulfide
null
C1CSCSC1
c1ccccc1.C1CSCSC1
HO-
C(Cl)Cl
null
3
O=CCc1ccccc1.SCCCS>C(Cl)Cl>c1ccc(CC2SCCCS2)cc1
ord_dataset-02ee2261663048188cf6d85d2cc96e3f
ord-534cc09434c845448a5acfd9ab4503ac
COc1ccc2c(c1)CCCC2=O.[C-]#N>>COc1ccc2c(c1)CCC=C2C#N
C[Si](C)(C)C#N.COC1=CC2=C(C=C1)C(=O)CCC2.[C-]#N.[Li+]>>C(#N)C1=CCCC2=CC(=CC=C12)OC
O=[C:12]1[c:6]2[cH:5][cH:4][c:3]([O:2][CH3:1])[cH:8][c:7]2[CH2:9][CH2:10][CH2:11]1.[C-:13]#[N:14]>>[CH3:1][O:2][c:3]1[cH:4][cH:5][c:6]2[c:7]([cH:8]1)[CH2:9][CH2:10][CH:11]=[C:12]2[C:13]#[N:14]
COc1ccc2c(c1)CCCC2=O.[C-]#N
COc1ccc2c(c1)CCC=C2C#N
null
null
CN(C=O)C.O1CCCC1
C-C Coupling
OtherReaction
e01b01043bfaeb01c3e2361338f006aba25607dec206a9f74552ce86fadfe00b
38173ffb46d9f636178242326a427b3d459fe7c0171d4d0447e25702c6b09e58
C1=Cc2ccccc2CC1
O=[C;H0;D3;+0:1]1-[CH2;D2;+0:2]-[C:3]-[C:4]-[c:5]:[c:6]-1:[c:7].[C-;H0;D1:8]#[N;D1;H0:9]>>[N;D1;H0:9]#[C;H0;D2;+0:8]-[C;H0;D3;+0:1]1=[CH;D2;+0:2]-[C:3]-[C:4]-[c:5]:[c:6]-1:[c:7]
60.4
[{"value": 60.0, "product": "C(#N)C1=CCCC2=CC(=CC=C12)OC", "details": "PERCENTYIELD", "is_desired": false}, {"value": 60.4, "product": "C(#N)C1=CCCC2=CC(=CC=C12)OC", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
1.5
HOUR
Trimethylsilylcyanide (50.0 g, 510 mmol) was added to a suspension of 75.0 g (430 mmol) of 6-methoxy-α-tetralone (commercially available from Aldrich Chemical Company) in 75 mL of anhydrous tetrahydrofuran (THF) at ambient temperature. Lithium cyanide (100 mL of a 0.5M solution in N,N-dimethylformamide (DMF) was added ...
10.6084/m9.figshare.5104873.v1
null
Ketone
Nitrile
c1ccc2c(c1)CCCC2
C1=Cc2ccccc2CC1
C1=Cc2ccccc2CC1
HO-
CN(C=O)C.O1CCCC1
null
1.5
COc1ccc2c(c1)CCCC2=O.[C-]#N>CN(C=O)C.O1CCCC1>COc1ccc2c(c1)CCC=C2C#N
ord_dataset-02ee2261663048188cf6d85d2cc96e3f
ord-f0032e6d5bdc4d0cbe0c7fbec8b6a737
COc1ccc2c(c1)CCC1C2CN(C)C1Cc1ccccc1.O=C(Cl)Cc1ccccc1>>COc1ccc2c(c1)CCC1C2CN(C(=O)Cc2ccccc2)C1Cc1ccccc1
C1(=CC=CC=C1)CC(=O)Cl.O.COC1=CC2=C(C3CN(C(C3CC2)CC2=CC=CC=C2)C)C=C1.Cl.N1=CC=CC=C1>>COC1=CC2=C(C3CN(C(C3CC2)CC2=CC=CC=C2)C(=O)CC2=CC=CC=C2)C=C1
C[N:14]1[CH2:13][CH:12]2[c:6]3[cH:5][cH:4][c:3]([O:2][CH3:1])[cH:8][c:7]3[CH2:9][CH2:10][CH:11]2[CH:24]1[CH2:25][c:26]1[cH:27][cH:28][cH:29][cH:30][cH:31]1.Cl[C:15](=[O:16])[CH2:17][c:18]1[cH:19][cH:20][cH:21][cH:22][cH:23]1>>[CH3:1][O:2][c:3]1[cH:4][cH:5][c:6]2[c:7]([cH:8]1)[CH2:9][CH2:10][CH:11]1[CH:12]2[CH2:13][N:14...
COc1ccc2c(c1)CCC1C2CN(C)C1Cc1ccccc1.O=C(Cl)Cc1ccccc1
COc1ccc2c(c1)CCC1C2CN(C(=O)Cc2ccccc2)C1Cc1ccccc1
null
null
C(Cl)Cl
Acylation
OtherReaction
8e71e5d3e73017a7aac5b3eac1bfbf3e65d703de2d576d29676f344087117844
7da20c2e2c34d1dd982a91b3333ed3c480165fa1ae9d2aa385b5b9d2065f54c9
O=C(Cc1ccccc1)N1CC2c3ccccc3CCC2C1Cc1ccccc1
C-[N;H0;D3;+0:1]1-[C:2]-[C:3]-[C:4]-[C:5]-1-[C:6].Cl-[C;H0;D3;+0:7](=[O;D1;H0:8])-[C:9]-[c:10]>>[C:6]-[C:5]1-[C:4]-[C:3]-[C:2]-[N;H0;D3;+0:1]-1-[C;H0;D3;+0:7](=[O;D1;H0:8])-[C:9]-[c:10]
null
[]
0
CELSIUS
3
MINUTE
2,3,3a,4,5,9b-Hexahydro-7-methoxy-2-methyl-3-phenylmethyl-1H-benz[e]isoindole (0.80 g, 2.73 mmol), the product of Example 1, was dissolved in 10 mL of methylene chloride and approximately 5 mL of pyridine was added to the resultant solution. The solution was cooled to 0° C. and approximately 2.5 mL of phenylacetyl chlo...
10.6084/m9.figshare.5104873.v1
null
Acyl halide.Tertiary amine
Tertiary amide
c1ccc2c(c1)CCC1C[NH]CC21
c1ccc2c(c1)CCC1C[NH]CC21
c1ccc2c(c1)CCC1C[NH]CC21.c1ccccc1.c1ccccc1
HCl
C(Cl)Cl
0
0.05
COc1ccc2c(c1)CCC1C2CN(C)C1Cc1ccccc1.O=C(Cl)Cc1ccccc1>C(Cl)Cl>COc1ccc2c(c1)CCC1C2CN(C(=O)Cc2ccccc2)C1Cc1ccccc1
ord_dataset-02ee2261663048188cf6d85d2cc96e3f
ord-4393075ba1aa42428cf8d5fd71a2583e
Cc1cccc(CC(=O)C2CCc3ccccc3C2C#N)c1>>Cc1cccc(CC2NCC3c4ccccc4CCC23)c1
C(#N)C1C(CCC2=CC=CC=C12)C(=O)CC1=CC(=CC=C1)C.C(#N)C1C(CCC2=CC(=CC=C12)OC)C(=O)CC1=CC=CC=C1.C(#N)C1C(CCC2=CC(=CC=C12)OC)C(=O)CC1=CC=CC=C1.C(#N)C1C(CCC2=CC=CC=C12)C(=O)CC1=CC(=CC=C1)C>>CC=1C=C(C=CC1)CC1NCC2C3=C(CCC12)C=CC=C3
O=[C:8]([CH2:7][c:6]1[cH:5][cH:4][cH:3][c:2]([CH3:1])[cH:21]1)[CH:20]1[CH:11]([C:10]#[N:9])[c:12]2[cH:13][cH:14][cH:15][cH:16][c:17]2[CH2:18][CH2:19]1>>[CH3:1][c:2]1[cH:3][cH:4][cH:5][c:6]([CH2:7][CH:8]2[NH:9][CH2:10][CH:11]3[c:12]4[cH:13][cH:14][cH:15][cH:16][c:17]4[CH2:18][CH2:19][CH:20]23)[cH:21]1
Cc1cccc(CC(=O)C2CCc3ccccc3C2C#N)c1
Cc1cccc(CC2NCC3c4ccccc4CCC23)c1
null
null
null
Heteroatom Alkylation and Arylation
OtherReaction
2c3bf11ecf1545c8757368ea4475f8a4703f783649587bec86e10bafd8a0cc6b
cb00476b0efaa1487253fc572e1edb8b26b4ce9be61ac2320fd61511c421df80
c1ccc(CC2NCC3c4ccccc4CCC23)cc1
O=[C;H0;D3;+0:1](-[C:2]-[c:3])-[C:4](-[C:5])-[C:6](-[C;H0;D2;+0:7]#[N;H0;D1;+0:8])-[c:9]>>[C:5]-[C:4]1-[C:6](-[c:9])-[CH2;D2;+0:7]-[NH;D2;+0:8]-[CH;D3;+0:1]-1-[C:2]-[c:3]
null
[]
null
null
null
null
Following the procedures described in Step 2 of Example 6, replacing 1-cyano-6-methoxy-2-phenylmethylcarbonyl-1,2,3,4-tetrahydronaphthalene (the product of Step 1 of Example 6) with the product of Step 1 above, 1-cyano-2-(3-methylphenyl)methylcarbonyl-1,2,3,4-tetrahydronaphthalene, the title compound was prepared; MS D...
10.6084/m9.figshare.5104873.v1
null
Ketone.Nitrile
Secondary amine
null
c1ccc2c(c1)CCC1CNCC21
c1ccccc1.c1ccc2c(c1)CCC1CNCC21
Other
null
null
null
Cc1cccc(CC(=O)C2CCc3ccccc3C2C#N)c1>>Cc1cccc(CC2NCC3c4ccccc4CCC23)c1
ord_dataset-02ee2261663048188cf6d85d2cc96e3f
ord-3d8b557851dd4629afee23bc916f9121
C1CSCSC1.Fc1cccc(CBr)c1>>Fc1cccc(CC2SCCCS2)c1
C(CCC)[Li].S1CSCCC1.FC=1C=C(CBr)C=CC1>>FC=1C=C(C=CC1)CC1SCCCS1
[CH2:8]1[S:9][CH2:10][CH2:11][CH2:12][S:13]1.Br[CH2:7][c:6]1[cH:5][cH:4][cH:3][c:2]([F:1])[cH:14]1>>[F:1][c:2]1[cH:3][cH:4][cH:5][c:6]([CH2:7][CH:8]2[S:9][CH2:10][CH2:11][CH2:12][S:13]2)[cH:14]1
C1CSCSC1.Fc1cccc(CBr)c1
Fc1cccc(CC2SCCCS2)c1
null
null
CCCCCC.C1CCOC1.C(Cl)Cl
C-C Coupling
OtherReaction
ab0114b4a4cb6005c4898e16d6c0a2b288ca25c97a67a873f171ed1d3be6a47c
4efa513f567c8dda6a947e269b70f7a500c3fa9b005a8552cb1e41aa23aad50b
c1ccc(CC2SCCCS2)cc1
Br-[CH2;D2;+0:1]-[c:2](:[c:3]):[c:4].[C:5]-[#16:6]-[CH2;D2;+0:7]-[#16:8]-[C:9]>>[C:5]-[#16:6]-[CH;D3;+0:7](-[CH2;D2;+0:1]-[c:2](:[c:3]):[c:4])-[#16:8]-[C:9]
66.7
[{"value": 66.7, "product": "FC=1C=C(C=CC1)CC1SCCCS1", "details": "PERCENTYIELD", "is_desired": false}, {"value": 66.6, "product": "FC=1C=C(C=CC1)CC1SCCCS1", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
-23
CELSIUS
0.5
HOUR
1,3-Dithiane (12 g, 0.1 mol) was dissolved in 150 mL of anhydrous THF under a nitrogen atmosphere. The resultant solution was cooled to -78° C. and n-butyllithium (44 mL of a 2.5M solution of in hexane, 0.11 mol) was added. The reaction mixture was warmed to -23° C. and then stirred at -23° C. for 0.5 h. The reaction m...
10.6084/m9.figshare.5104873.v1
null
Primary halide.Monosulfide.Monosulfide
Monosulfide.Monosulfide
C1CSCSC1
C1CSCSC1
c1ccccc1.C1CSCSC1
HBr
CCCCCC.C1CCOC1.C(Cl)Cl
-23
0.5
C1CSCSC1.Fc1cccc(CBr)c1>CCCCCC.C1CCOC1.C(Cl)Cl>Fc1cccc(CC2SCCCS2)c1
ord_dataset-02ee2261663048188cf6d85d2cc96e3f
ord-e05e51d0b3d34018a312b37d4ef0a1b6
C1CSCSC1.Fc1cccc(CBr)c1>>Fc1ccc(CC2SCCCS2)cc1
C(CCC)[Li].S1CSCCC1.C1CCOC1.FC=1C=C(CBr)C=CC1>>FC1=CC=C(C=C1)CC1SCCCS1
[CH2:7]1[S:8][CH2:9][CH2:10][CH2:11][S:12]1.Br[CH2:6][c:5]1[cH:13][cH:4][cH:3][c:2]([F:1])[cH:14]1>>[F:1][c:2]1[cH:3][cH:4][c:5]([CH2:6][CH:7]2[S:8][CH2:9][CH2:10][CH2:11][S:12]2)[cH:13][cH:14]1
C1CSCSC1.Fc1cccc(CBr)c1
Fc1ccc(CC2SCCCS2)cc1
null
null
CCCCCC
C-C Coupling
OtherReaction
7eb7099aaef7a8e030bb6c6581c2bc2d7fb58e3cc95becfcad9c064e11ef082d
4efa513f567c8dda6a947e269b70f7a500c3fa9b005a8552cb1e41aa23aad50b
c1ccc(CC2SCCCS2)cc1
Br-[CH2;D2;+0:1]-[c;H0;D3;+0:2]1:[cH;D2;+0:3]:[cH;D2;+0:4]:[c:5]:[c:6](-[F;D1;H0:7]):[cH;D2;+0:8]:1.[C:9]-[#16:10]-[CH2;D2;+0:11]-[#16:12]-[C:13]>>[C:9]-[#16:10]-[CH;D3;+0:11](-[CH2;D2;+0:1]-[c;H0;D3;+0:2]1:[cH;D2;+0:3]:[cH;D2;+0:8]:[c:6](-[F;D1;H0:7]):[c:5]:[cH;D2;+0:4]:1)-[#16:12]-[C:13]
94
[{"value": 94.0, "product": "FC1=CC=C(C=C1)CC1SCCCS1", "details": "PERCENTYIELD", "is_desired": false}]
0
CELSIUS
0.5
HOUR
1,3-Dithiane (20 g, 166 mmol) was dissolved in 250 mL of anhydrous THF under a nitrogen atmosphere. The resultant solution was cooled to -78° C. and n-butyllithium (128 mL of a 1.5M solution of in hexane, 199 m mol) was added. The reaction mixture was warmed to 0° C. and then stirred at 0° C. for 0.5 h. The reaction mi...
10.6084/m9.figshare.5104873.v1
null
Primary halide.Monosulfide.Monosulfide
Monosulfide.Monosulfide
C1CSCSC1.c1ccccc1
c1ccccc1.C1CSCSC1
c1ccccc1.C1CSCSC1
HBr
CCCCCC
0
0.5
C1CSCSC1.Fc1cccc(CBr)c1>CCCCCC>Fc1ccc(CC2SCCCS2)cc1
ord_dataset-02ee2261663048188cf6d85d2cc96e3f
ord-4a42d9fa1cdc4bb59ca4fa196c120674
COC(=O)C1=CCCc2ccccc21.O=[N+]([O-])CCc1cccc([N+](=O)[O-])c1>>COC(=O)C1c2ccccc2CCC1C(Cc1cccc([N+](=O)[O-])c1)[N+](=O)[O-]
C(=O)(OC)C1=CCCC2=CC=CC=C12.[N+](=O)([O-])C=1C=C(C=CC1)CC[N+](=O)[O-].N12CCCCCC2=NCCC1>>C(=O)(OC)C1C(CCC2=CC=CC=C12)C(CC1=CC(=CC=C1)[N+](=O)[O-])[N+](=O)[O-]
[CH3:1][O:2][C:3](=[O:4])[C:5]1=[CH:14][CH2:13][CH2:12][c:11]2[c:6]1[cH:7][cH:8][cH:9][cH:10]2.[CH2:15]([CH2:16][c:17]1[cH:18][cH:19][cH:20][c:21]([N+:22](=[O:23])[O-:24])[cH:25]1)[N+:26](=[O:27])[O-:28]>>[CH3:1][O:2][C:3](=[O:4])[CH:5]1[c:6]2[cH:7][cH:8][cH:9][cH:10][c:11]2[CH2:12][CH2:13][CH:14]1[CH:15]([CH2:16][c:17...
COC(=O)C1=CCCc2ccccc21.O=[N+]([O-])CCc1cccc([N+](=O)[O-])c1
COC(=O)C1c2ccccc2CCC1C(Cc1cccc([N+](=O)[O-])c1)[N+](=O)[O-]
null
null
C(C)#N.C(C)(=O)OCC
C-C Coupling
OtherReaction
aaeb29b9af1b9b99616f9dc60e090eeceff0100c4c89fb2f957c0ec91b7320ff
6f872e1e6593abcdd0d9fb5775fd31c259676a11a338f4f9b2b3594108a0aabd
c1ccc(CCC2CCc3ccccc3C2)cc1
[C;D1;H3:1]-[#8:2]-[C:3](=[O;D1;H0:4])-[C;H0;D3;+0:5]1=[CH;D2;+0:6]-[C:7]-[C:8]-[c:9]:[c:10]-1:[c:11].[O;-;D1;H0:12]-[#7;+:13](=[O;D1;H0:14])-[CH2;D2;+0:15]-[C:16]-[c:17]>>[C;D1;H3:1]-[#8:2]-[C:3](=[O;D1;H0:4])-[CH;D3;+0:5]1-[CH;D3;+0:6](-[CH;D3;+0:15](-[C:16]-[c:17])-[#7;+:13](-[O;-;D1;H0:12])=[O;D1;H0:14])-[C:7]-[C:8...
97.2
[{"value": 97.0, "product": "C(=O)(OC)C1C(CCC2=CC=CC=C12)C(CC1=CC(=CC=C1)[N+](=O)[O-])[N+](=O)[O-]", "details": "PERCENTYIELD", "is_desired": false}, {"value": 97.2, "product": "C(=O)(OC)C1C(CCC2=CC=CC=C12)C(CC1=CC(=CC=C1)[N+](=O)[O-])[N+](=O)[O-]", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
0.5
HOUR
To a mixture of 2 g (10.6 mmol) of 1-carbomethoxy-3,4-dihydronaphthalene, from Step 1 of Example 46, and 2.08 g (10.6 mmol) of 2-(3-nitrophenyl)-1-nitroethane, from Step 2, in 1 mL of acetonitrile was added 0.2 mL of 1,8-diazabicyclo[5.4.0]undec-7-ene (DBU). The reaction mixture was stirred at ambient temperature for 0...
10.6084/m9.figshare.5104873.v1
null
Ester.Nitro group
Ester.Nitro group
C1=Cc2ccccc2CC1
c1ccc2c(c1)CCCC2
c1ccc2c(c1)CCCC2.c1ccccc1
null
C(C)#N.C(C)(=O)OCC
null
0.5
COC(=O)C1=CCCc2ccccc21.O=[N+]([O-])CCc1cccc([N+](=O)[O-])c1>C(C)#N.C(C)(=O)OCC>COC(=O)C1c2ccccc2CCC1C(Cc1cccc([N+](=O)[O-])c1)[N+](=O)[O-]
ord_dataset-02ee2261663048188cf6d85d2cc96e3f
ord-8a9dfc9e6b4442e382afa28c9f122cb5
C[N+](=O)[O-].O=Cc1cccc(Cl)c1>>O=[N+]([O-])C=Cc1cccc(Cl)c1
[OH-].[K+].ClC=1C=C(C=O)C=CC1.C(C)(=O)[O-].[NH4+].[N+](=O)([O-])C>>ClC=1C=C(C=CC1)C=C[N+](=O)[O-]
[O:1]=[N+:2]([O-:3])[CH3:4].O=[CH:5][c:6]1[cH:7][cH:8][cH:9][c:10]([Cl:11])[cH:12]1>>[O:1]=[N+:2]([O-:3])[CH:4]=[CH:5][c:6]1[cH:7][cH:8][cH:9][c:10]([Cl:11])[cH:12]1
C[N+](=O)[O-].O=Cc1cccc(Cl)c1
O=[N+]([O-])C=Cc1cccc(Cl)c1
null
null
C(C)(=O)O
C-C Coupling
OtherReaction
7ede86d40d3d69f429dde089476c8b7ffa9b74bf3050590255e6323d013c2daf
f736727903c0ad5511d468246b8e380897fd19905174c118ffa4ed4d3651f6ea
c1ccccc1
O=[CH;D2;+0:1]-[c:2](:[c:3]):[c:4].[CH3;D1;+0:5]-[#7;+:6](-[O;-;D1;H0:7])=[O;D1;H0:8]>>[O;-;D1;H0:7]-[#7;+:6](=[O;D1;H0:8])-[CH;D2;+0:5]=[CH;D2;+0:1]-[c:2](:[c:3]):[c:4]
null
[]
null
null
null
null
A mixture of 28.11 g (200 mmol) of 3-chlorobenzaldehyde, 15.4 g of ammonium acetate and 32.5 mL of nitromethane in 230 mL of glacial acetic acid was heated at reflux temperature for 3 h and then poured onto ice. The resultant aqueous mixture was made basic by the addition of 45% aqueous potassium hydroxide. The precipi...
10.6084/m9.figshare.5104873.v1
null
Aldehyde.Nitro group
Enamine
null
null
c1ccccc1
HO-
C(C)(=O)O
null
null
C[N+](=O)[O-].O=Cc1cccc(Cl)c1>C(C)(=O)O>O=[N+]([O-])C=Cc1cccc(Cl)c1
ord_dataset-02ee2261663048188cf6d85d2cc96e3f
ord-8ba885339f8d41249dc7afe4b839d218
O=[N+]([O-])C=Cc1cccc(Cl)c1>>O=[N+]([O-])CCc1cccc(Cl)c1
ClC=1C=C(C=CC1)C=C[N+](=O)[O-].[BH4-].[Na+]>>ClC=1C=C(C=CC1)CC[N+](=O)[O-]
[O:1]=[N+:2]([O-:3])[CH:4]=[CH:5][c:6]1[cH:7][cH:8][cH:9][c:10]([Cl:11])[cH:12]1>>[O:1]=[N+:2]([O-:3])[CH2:4][CH2:5][c:6]1[cH:7][cH:8][cH:9][c:10]([Cl:11])[cH:12]1
O=[N+]([O-])C=Cc1cccc(Cl)c1
O=[N+]([O-])CCc1cccc(Cl)c1
null
null
C(C)O.O1CCOCC1
Reduction
Hydrogenation (double to single)
1897ddb5557a7164dfa80083adb557accafa4233396f9576d5bfde28d2818919
92f8c31381fee05ef128b294b51ee13ebdada3b3789c3c4a7dc0a1d2ea4408c2
c1ccccc1
[O;-;D1;H0:1]-[#7;+:2](=[O;D1;H0:3])-[CH;D2;+0:4]=[CH;D2;+0:5]-[c:6](:[c:7]):[c:8]>>[O;-;D1;H0:1]-[#7;+:2](=[O;D1;H0:3])-[CH2;D2;+0:4]-[CH2;D2;+0:5]-[c:6](:[c:7]):[c:8]
48
[{"value": 48.0, "product": "ClC=1C=C(C=CC1)CC[N+](=O)[O-]", "details": "PERCENTYIELD", "is_desired": false}, {"value": 47.1, "product": "ClC=1C=C(C=CC1)CC[N+](=O)[O-]", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
2
HOUR
A solution of 13.5 g (72 mmol) of 2-(3-Chlorophenyl)-1-nitroethene, from Step 2, in 200 mL of dioxane was added dropwise to a stirred suspension of 6 g (157 mmol) of sodium borohydride in a mixture of 140 mL of dioxane and 60 mL of ethanol. The reaction mixture was stirred at ambient temperature for 2 h and then the ex...
10.6084/m9.figshare.5104873.v1
null
Enamine
Nitro group
null
null
c1ccccc1
null
C(C)O.O1CCOCC1
null
2
O=[N+]([O-])C=Cc1cccc(Cl)c1>C(C)O.O1CCOCC1>O=[N+]([O-])CCc1cccc(Cl)c1
ord_dataset-02ee2261663048188cf6d85d2cc96e3f
ord-0e9e6791f66b44a5853ffa9b8e1fcd15
CO.N#CC1=CCCc2cc(Cl)ccc21.O>>COC(=O)C1=CCCc2cc(Cl)ccc21
CO.ClC=1C=C2CCC=C(C2=CC1)C#N.O>>C(=O)(OC)C1=CCCC2=CC(=CC=C12)Cl
[CH3:1][OH:2].N#[C:3][C:5]1=[CH:6][CH2:7][CH2:8][c:9]2[cH:10][c:11]([Cl:12])[cH:13][cH:14][c:15]21.[OH2:4]>>[CH3:1][O:2][C:3](=[O:4])[C:5]1=[CH:6][CH2:7][CH2:8][c:9]2[cH:10][c:11]([Cl:12])[cH:13][cH:14][c:15]21
CO.N#CC1=CCCc2cc(Cl)ccc21.O
COC(=O)C1=CCCc2cc(Cl)ccc21
null
null
S(O)(O)(=O)=O
Acylation
OtherReaction
25b7d3e2396602529eceda3adc077f79d6fd790da73e87e4e1fbd1265f44d7b0
477d3ec3ec37df7b1359a7d22cd39dadb1daeb5d9957363442952ac99d03b083
C1=Cc2ccccc2CC1
N#[C;H0;D2;+0:1]-[C:2](=[C:3]-[C:4])-[c:5].[C;D1;H3:6]-[OH;D1;+0:7].[OH2;D0;+0:8]>>[C:4]-[C:3]=[C:2](-[C;H0;D3;+0:1](=[O;H0;D1;+0:8])-[O;H0;D2;+0:7]-[C;D1;H3:6])-[c:5]
26
[{"value": 26.0, "product": "C(=O)(OC)C1=CCCC2=CC(=CC=C12)Cl", "details": "PERCENTYIELD", "is_desired": false}]
null
null
2
DAY
6-Chloro-1-cyano-3,4-dihydronaphthalene (5 g, 263 mmol), lit ref, was dissolved in 77% sulfuric acid in methanol and the resulting solution was heated at 95°-100° C. for 2.5 h. The reaction mixture was allowed to cool to ambient temperature and 45 mL was added, followed by 5 mL of water. The reaction mixture was stirre...
10.6084/m9.figshare.5104873.v1
null
Nitrile.Methanol
Ester
null
null
C1=Cc2ccccc2CC1
Other
S(O)(O)(=O)=O
null
48
CO.N#CC1=CCCc2cc(Cl)ccc21.O>S(O)(O)(=O)=O>COC(=O)C1=CCCc2cc(Cl)ccc21
ord_dataset-02ee2261663048188cf6d85d2cc96e3f
ord-5be24c88fc2e4cc8b1960a9fe0a69a5d
N#CC1=CCCc2ccccc21.N#CCCc1ccccc1>>N#CC(Cc1ccccc1)C1CCc2ccccc2C1C#N
C1(=CC=CC=C1)CCC#N.C(#N)C1=CCCC2=CC=CC=C12.C(#N)C1=CCCC2=CC=CC=C12.C(C)(C)NC(C)C.C(CCC)[Li]>>C(#N)C1C(CCC2=CC=CC=C12)C(CC1=CC=CC=C1)C#N
[CH:11]1=[C:20]([C:21]#[N:22])[c:19]2[c:14]([cH:15][cH:16][cH:17][cH:18]2)[CH2:13][CH2:12]1.[N:1]#[C:2][CH2:3][CH2:4][c:5]1[cH:6][cH:7][cH:8][cH:9][cH:10]1>>[N:1]#[C:2][CH:3]([CH2:4][c:5]1[cH:6][cH:7][cH:8][cH:9][cH:10]1)[CH:11]1[CH2:12][CH2:13][c:14]2[cH:15][cH:16][cH:17][cH:18][c:19]2[CH:20]1[C:21]#[N:22]
N#CC1=CCCc2ccccc21.N#CCCc1ccccc1
N#CC(Cc1ccccc1)C1CCc2ccccc2C1C#N
null
null
C1CCOC1
C-C Coupling
OtherReaction
0129aeb1246532f294262ba021b68c7ed1f5c6b93ed3160aab4a60666db55baa
410ec9b1cc243569e4ff568c248f0b402403802e002b4018f576af3f6960507b
c1ccc(CCC2CCc3ccccc3C2)cc1
[N;D1;H0:1]#[C:2]-[C;H0;D3;+0:3]1=[CH;D2;+0:4]-[C:5]-[C:6]-[c:7]:[c:8]-1:[c:9].[N;D1;H0:10]#[C:11]-[CH2;D2;+0:12]-[C:13]-[c:14]>>[N;D1;H0:10]#[C:11]-[CH;D3;+0:12](-[C:13]-[c:14])-[CH;D3;+0:4]1-[C:5]-[C:6]-[c:7]:[c:8](:[c:9])-[CH;D3;+0:3]-1-[C:2]#[N;D1;H0:1]
99.5
[{"value": 99.5, "product": "C(#N)C1C(CCC2=CC=CC=C12)C(CC1=CC=CC=C1)C#N", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
-78
CELSIUS
0.5
HOUR
To a solution of 3.5 mL (25 mmol) of diisopropylamine in 40 mL of THF at -78° C., under a nitrogen atmosphere, was added n-butyllithium (9.5 mL of a 2.5M solution in THF, 23.7 mmol) and the resultant solution was stirred at -78° C. for 0.5 h. To the stirred solution was slowly added a solution of 2.75 g (21 mmol) of 3-...
10.6084/m9.figshare.5104873.v1
null
null
null
C1=Cc2ccccc2CC1
c1ccc2c(c1)CCCC2
c1ccccc1.c1ccc2c(c1)CCCC2
null
C1CCOC1
-78
0.5
N#CC1=CCCc2ccccc21.N#CCCc1ccccc1>C1CCOC1>N#CC(Cc1ccccc1)C1CCc2ccccc2C1C#N
ord_dataset-02ee2261663048188cf6d85d2cc96e3f
ord-2381c22df2194b6c83a6f440b9b07972
COc1ccc2c(c1)CCC=C2C#N.COc1ccc2c(c1)CCC=C2C#N>>COc1ccc2c(c1)CCC(CC#N)C2C#N
C(#N)C1=CCCC2=CC(=CC=C12)OC.C(#N)C1=CCCC2=CC(=CC=C12)OC.C(C)(C)NC(C)C.C(CCC)[Li].C(C)#N>>C(#N)C1C(CCC2=CC(=CC=C12)OC)CC#N
[CH3:1][O:2][c:3]1[cH:4][cH:5][c:6]2[c:7]([cH:8]1)[CH2:9][CH2:10][CH:11]=[C:15]2[C:16]#[N:17].COc1ccc2c(c1)CCC=[C:12]2[C:13]#[N:14]>>[CH3:1][O:2][c:3]1[cH:4][cH:5][c:6]2[c:7]([cH:8]1)[CH2:9][CH2:10][CH:11]([CH2:12][C:13]#[N:14])[CH:15]2[C:16]#[N:17]
COc1ccc2c(c1)CCC=C2C#N.COc1ccc2c(c1)CCC=C2C#N
COc1ccc2c(c1)CCC(CC#N)C2C#N
null
null
C1CCOC1
C-C Coupling
OtherReaction
9c3387d0730f2e56be401d9834ef01667c6e3c89b1208a31c2c7da5d6214475b
a5693ad0ff37ba299a3384a72fcc8b66e16e2c53e1f48e2cc3e13008b4273e5a
c1ccc2c(c1)CCCC2
C-O-c1:c:c:c2:c(:c:1)-C-C-C=[C;H0;D3;+0:1]-2-[C:2]#[N;D1;H0:3].[N;D1;H0:4]#[C:5]-[C;H0;D3;+0:6]1=[CH;D2;+0:7]-[C:8]-[C:9]-[c:10]:[c:11]-1:[c:12]>>[N;D1;H0:3]#[C:2]-[CH2;D2;+0:1]-[CH;D3;+0:7]1-[C:8]-[C:9]-[c:10]:[c:11](:[c:12])-[CH;D3;+0:6]-1-[C:5]#[N;D1;H0:4]
74.2
[{"value": 74.0, "product": "C(#N)C1C(CCC2=CC(=CC=C12)OC)CC#N", "details": "PERCENTYIELD", "is_desired": false}, {"value": 74.2, "product": "C(#N)C1C(CCC2=CC(=CC=C12)OC)CC#N", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
-78
CELSIUS
40
MINUTE
To a solution of 1.05 mL (7.5 mmol) of diisopropylamine in 10 mL of THF at -78° C., under a nitrogen atmosphere, was added n-butyllithium (2.2 mL of a 2.5M solution in THF, 5.5 mmol) and the resultant solution was stirred at -78° C. for 40 min. To the stirred solution was added, dropwise over a 25 minute period, a solu...
10.6084/m9.figshare.5104873.v1
null
Ether
null
C1=Cc2ccccc2CC1.C1=Cc2ccccc2CC1
c1ccc2c(c1)CCCC2
c1ccc2c(c1)CCCC2
HO-
C1CCOC1
-78
0.666667
COc1ccc2c(c1)CCC=C2C#N.COc1ccc2c(c1)CCC=C2C#N>C1CCOC1>COc1ccc2c(c1)CCC(CC#N)C2C#N
ord_dataset-02ee2261663048188cf6d85d2cc96e3f
ord-4f061f4471424f05a5f309faf9ef5632
COC(=O)CC(=O)Cc1ccccc1.COc1ccc2c(c1)CCC=C2C#N>>COC(=O)C(C(=O)Cc1ccccc1)C1CCc2cc(OC)ccc2C1C#N
C1CCC2=NCCCN2CC1.O=C(CC(=O)OC)CC1=CC=CC=C1.C(#N)C1=CCCC2=CC(=CC=C12)OC.C(#N)C1=CCCC2=CC(=CC=C12)OC.C1CCC2=NCCCN2CC1>>O=C(C(C(=O)OC)C1C(C2=CC=C(C=C2CC1)OC)C#N)CC1=CC=CC=C1
[CH3:1][O:2][C:3](=[O:4])[CH2:5][C:6](=[O:7])[CH2:8][c:9]1[cH:10][cH:11][cH:12][cH:13][cH:14]1.[CH:15]1=[C:26]([C:27]#[N:28])[c:25]2[c:18]([cH:19][c:20]([O:21][CH3:22])[cH:23][cH:24]2)[CH2:17][CH2:16]1>>[CH3:1][O:2][C:3](=[O:4])[CH:5]([C:6](=[O:7])[CH2:8][c:9]1[cH:10][cH:11][cH:12][cH:13][cH:14]1)[CH:15]1[CH2:16][CH2:1...
COC(=O)CC(=O)Cc1ccccc1.COc1ccc2c(c1)CCC=C2C#N
COC(=O)C(C(=O)Cc1ccccc1)C1CCc2cc(OC)ccc2C1C#N
null
null
C(C)#N
C-C Coupling
OtherReaction
06b659e430c38d7049f44cf9f81483d3fe02a4c18a09fabdaf216969690bdca0
94c7364692188ef8ef531518cf74a9fca9728a2aa5d4b3e96a01bb7b82219171
O=C(Cc1ccccc1)CC1CCc2ccccc2C1
[C:1]-[C:2](=[O;D1;H0:3])-[CH2;D2;+0:4]-[C:5](=[O;D1;H0:6])-[#8:7]-[C;D1;H3:8].[N;D1;H0:9]#[C:10]-[C;H0;D3;+0:11]1=[CH;D2;+0:12]-[C:13]-[C:14]-[c:15]:[c:16]-1:[c:17]>>[C:1]-[C:2](=[O;D1;H0:3])-[CH;D3;+0:4](-[C:5](=[O;D1;H0:6])-[#8:7]-[C;D1;H3:8])-[CH;D3;+0:12]1-[C:13]-[C:14]-[c:15]:[c:16](:[c:17])-[CH;D3;+0:11]-1-[C:10...
65
[{"value": 65.0, "product": "O=C(C(C(=O)OC)C1C(C2=CC=C(C=C2CC1)OC)C#N)CC1=CC=CC=C1", "details": "PERCENTYIELD", "is_desired": false}, {"value": 64.6, "product": "O=C(C(C(=O)OC)C1C(C2=CC=C(C=C2CC1)OC)C#N)CC1=CC=CC=C1", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
2
HOUR
Methyl 3-oxo-4-phenylbutyrate (29.33 g, 153 mmol) and 1-cyano-6-methoxy-3,4-dihydronaphthalene (25.7, 139 mmol), the product of Step 2 of Example 1, were dissolved in 25 mL of acetonitrile. DBU (1.5 mL) was added and the reaction mixture was stirred for 2 h at ambient temperature. A second aliquot of DBU (1.5 mL) was t...
10.6084/m9.figshare.5104873.v1
null
Ketone.Ester
Ketone.Ester
C1=Cc2ccccc2CC1
c1ccc2c(c1)CCCC2
c1ccccc1.c1ccc2c(c1)CCCC2
null
C(C)#N
null
2
COC(=O)CC(=O)Cc1ccccc1.COc1ccc2c(c1)CCC=C2C#N>C(C)#N>COC(=O)C(C(=O)Cc1ccccc1)C1CCc2cc(OC)ccc2C1C#N
ord_dataset-02ee2261663048188cf6d85d2cc96e3f
ord-b7636b58c9434354a2f9df4dde371baa
COC(=O)C(C(=O)Cc1ccccc1)C1CCc2cc(OC)ccc2C1C#N>>COc1ccc2c(c1)CCC(CC(=O)Cc1ccccc1)C2C#N
Cl.O=C(C(C(=O)OC)C1C(C2=CC=C(C=C2CC1)OC)C#N)CC1=CC=CC=C1.[OH-].[Li+]>>C(#N)C1C(CCC2=CC(=CC=C12)OC)CC(CC1=CC=CC=C1)=O
COC(=O)[CH:12]([CH:11]1[CH2:10][CH2:9][c:7]2[c:6]([cH:5][cH:4][c:3]([O:2][CH3:1])[cH:8]2)[CH:22]1[C:23]#[N:24])[C:13](=[O:14])[CH2:15][c:16]1[cH:17][cH:18][cH:19][cH:20][cH:21]1>>[CH3:1][O:2][c:3]1[cH:4][cH:5][c:6]2[c:7]([cH:8]1)[CH2:9][CH2:10][CH:11]([CH2:12][C:13](=[O:14])[CH2:15][c:16]1[cH:17][cH:18][cH:19][cH:20][c...
COC(=O)C(C(=O)Cc1ccccc1)C1CCc2cc(OC)ccc2C1C#N
COc1ccc2c(c1)CCC(CC(=O)Cc1ccccc1)C2C#N
null
null
CO
Reduction
Decarboxylation
fdc964bea6eaeadfb2309e01318abba99b151c57fdaf3760a2830a6479750a9b
f277909394d9f4e61cc2cdb65fef123102672ca91cfff7f8513cb0baf66138ac
O=C(Cc1ccccc1)CC1CCc2ccccc2C1
C-O-C(=O)-[CH;D3;+0:1](-[C:2](-[C:3])-[C:4])-[C:5](-[C:6])=[O;D1;H0:7]>>[C:3]-[C:2](-[CH2;D2;+0:1]-[C:5](-[C:6])=[O;D1;H0:7])-[C:4]
70
[{"value": 70.0, "product": null, "details": "PERCENTYIELD", "is_desired": false}]
null
null
8
HOUR
Methyl 3-oxo-4-phenyl-2-(1-cyano-6-methoxy-1,2,3,4-tetrahydronaphth-2-yl)-butyrate (4.63 g, 12 mmol), from Step 1, was dissolved in 100 mL of methanol and lithium hydroxide (77 mL of a 1.0M solution) was added. The reaction mixture was stirred overnight at ambient temperature and then acidified with 1N aqueous hydrochl...
10.6084/m9.figshare.5104873.v1
null
Ketone.Ester
Ketone
null
null
c1ccc2c(c1)CCCC2.c1ccccc1
HO-
CO
null
8
COC(=O)C(C(=O)Cc1ccccc1)C1CCc2cc(OC)ccc2C1C#N>CO>COc1ccc2c(c1)CCC(CC(=O)Cc1ccccc1)C2C#N
ord_dataset-02ee2261663048188cf6d85d2cc96e3f
ord-6af1fdb47b964a16a7ec980db7c96d8b
CCOC(=O)CCC1CCc2ccccc2C1=O.[C-]#N>>CCOC(=O)CCC1=C(C#N)c2ccccc2CC1
[C-]#N.[Li+].C(C)OC(=O)CCC1C(C2=CC=CC=C2CC1)=O.C(#N)P(OCC)(OCC)=O.O>>C(#N)C1=C(CCC2=CC=CC=C12)CCC(=O)OCC
O=[C:9]1[CH:8]([CH2:7][CH2:6][C:4]([O:3][CH2:2][CH3:1])=[O:5])[CH2:19][CH2:18][c:17]2[c:12]1[cH:13][cH:14][cH:15][cH:16]2.[C-:10]#[N:11]>>[CH3:1][CH2:2][O:3][C:4](=[O:5])[CH2:6][CH2:7][C:8]1=[C:9]([C:10]#[N:11])[c:12]2[cH:13][cH:14][cH:15][cH:16][c:17]2[CH2:18][CH2:19]1
CCOC(=O)CCC1CCc2ccccc2C1=O.[C-]#N
CCOC(=O)CCC1=C(C#N)c2ccccc2CC1
null
null
CN(C)C=O.C1CCOC1
C-C Coupling
OtherReaction
e01b01043bfaeb01c3e2361338f006aba25607dec206a9f74552ce86fadfe00b
38173ffb46d9f636178242326a427b3d459fe7c0171d4d0447e25702c6b09e58
C1=Cc2ccccc2CC1
O=[C;H0;D3;+0:1]1-[CH;D3;+0:2](-[C:3]-[C:4]-[C:5](-[#8:6])=[O;D1;H0:7])-[C:8]-[C:9]-[c:10]:[c:11]-1:[c:12].[C-;H0;D1:13]#[N;D1;H0:14]>>[#8:6]-[C:5](=[O;D1;H0:7])-[C:4]-[C:3]-[C;H0;D3;+0:2]1=[C;H0;D3;+0:1](-[C;H0;D2;+0:13]#[N;D1;H0:14])-[c:11](:[c:12]):[c:10]-[C:9]-[C:8]-1
64.2
[{"value": 64.2, "product": "C(#N)C1=C(CCC2=CC=CC=C12)CCC(=O)OCC", "details": "PERCENTYIELD", "is_desired": false}, {"value": 64.1, "product": "C(#N)C1=C(CCC2=CC=CC=C12)CCC(=O)OCC", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
8
HOUR
2-(2-Ethoxycarbonylethyl)-3,4-dihydro-1(2H)-naphthalenone (19.7 g, 80 mmol), from Step 1, was dissolved in 200 mL of dry THF and diethyl cyanophosphonate (23.6 mL, 160 mmol), commercially available from Aldrich Chemical Company, was added, followed by 160 mL of a 0.5M solution of lithium cyanide in DMF. The reaction mi...
10.6084/m9.figshare.5104873.v1
null
Ketone
Nitrile
c1ccc2c(c1)CCCC2
C1=Cc2ccccc2CC1
C1=Cc2ccccc2CC1
HO-
CN(C)C=O.C1CCOC1
null
8
CCOC(=O)CCC1CCc2ccccc2C1=O.[C-]#N>CN(C)C=O.C1CCOC1>CCOC(=O)CCC1=C(C#N)c2ccccc2CC1
ord_dataset-02ee2261663048188cf6d85d2cc96e3f
ord-6e03421e3f554cada4678867b24aa606
CCOC(=O)CCC1CCc2c(OC)cccc2C1=O.[C-]#N>>CCOC(=O)CCC1=C(C#N)c2cccc(OC)c2CC1
[C-]#N.[Li+].C(C)OC(=O)CCC1C(C2=CC=CC(=C2CC1)OC)=O.C(#N)P(OCC)(OCC)=O.O>>C(#N)C1=C(CCC2=C(C=CC=C12)OC)CCC(=O)OCC
O=[C:9]1[CH:8]([CH2:7][CH2:6][C:4]([O:3][CH2:2][CH3:1])=[O:5])[CH2:21][CH2:20][c:19]2[c:12]1[cH:13][cH:14][cH:15][c:16]2[O:17][CH3:18].[C-:10]#[N:11]>>[CH3:1][CH2:2][O:3][C:4](=[O:5])[CH2:6][CH2:7][C:8]1=[C:9]([C:10]#[N:11])[c:12]2[cH:13][cH:14][cH:15][c:16]([O:17][CH3:18])[c:19]2[CH2:20][CH2:21]1
CCOC(=O)CCC1CCc2c(OC)cccc2C1=O.[C-]#N
CCOC(=O)CCC1=C(C#N)c2cccc(OC)c2CC1
null
null
CN(C)C=O.C1CCOC1
C-C Coupling
OtherReaction
e01b01043bfaeb01c3e2361338f006aba25607dec206a9f74552ce86fadfe00b
38173ffb46d9f636178242326a427b3d459fe7c0171d4d0447e25702c6b09e58
C1=Cc2ccccc2CC1
O=[C;H0;D3;+0:1]1-[CH;D3;+0:2](-[C:3]-[C:4]-[C:5](-[#8:6])=[O;D1;H0:7])-[C:8]-[C:9]-[c:10]:[c:11]-1:[c:12].[C-;H0;D1:13]#[N;D1;H0:14]>>[#8:6]-[C:5](=[O;D1;H0:7])-[C:4]-[C:3]-[C;H0;D3;+0:2]1=[C;H0;D3;+0:1](-[C;H0;D2;+0:13]#[N;D1;H0:14])-[c:11](:[c:12]):[c:10]-[C:9]-[C:8]-1
70.1
[{"value": 70.0, "product": "C(#N)C1=C(CCC2=C(C=CC=C12)OC)CCC(=O)OCC", "details": "PERCENTYIELD", "is_desired": false}, {"value": 70.1, "product": "C(#N)C1=C(CCC2=C(C=CC=C12)OC)CCC(=O)OCC", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
0
CELSIUS
8
HOUR
2-(2-Ethoxycarbonylethyl)-3,4-dihydro-5-methoxy-1(2H)-naphthalenone (1.1 g, 4 mmol), from Step 1, was dissolved in 15 mL of dry THF and cooled to 0° C. Diethyl cyanophosphonate (1.18 mL, 8 mmol), commercially available from Aldrich Chemical Company, was added, followed by 8 mL of a 0.5M solution of lithium cyanide (4 m...
10.6084/m9.figshare.5104873.v1
null
Ketone
Nitrile
c1ccc2c(c1)CCCC2
C1=Cc2ccccc2CC1
C1=Cc2ccccc2CC1
HO-
CN(C)C=O.C1CCOC1
0
8
CCOC(=O)CCC1CCc2c(OC)cccc2C1=O.[C-]#N>CN(C)C=O.C1CCOC1>CCOC(=O)CCC1=C(C#N)c2cccc(OC)c2CC1
ord_dataset-02ee2261663048188cf6d85d2cc96e3f
ord-43574d7d6f5f4aa8866fdde3b5c2f0dc
BrCc1ccccc1.O=C1CC[C@@H]2CCc3ccccc3[C@@H]2CN1>>O=C1CC[C@@H]2CCc3ccccc3[C@@H]2CN1Cc1ccccc1
O.CC(C)([O-])C.[K+].O=C1CC[C@H]2[C@@H](CN1)C1=CC=CC=C1CC2.C(C1=CC=CC=C1)Br>>C(C1=CC=CC=C1)N1C[C@@H]2[C@H](CCC1=O)CCC1=CC=CC=C12
Br[CH2:17][c:18]1[cH:19][cH:20][cH:21][cH:22][cH:23]1.[O:1]=[C:2]1[CH2:3][CH2:4][C@@H:5]2[CH2:6][CH2:7][c:8]3[cH:9][cH:10][cH:11][cH:12][c:13]3[C@@H:14]2[CH2:15][NH:16]1>>[O:1]=[C:2]1[CH2:3][CH2:4][C@@H:5]2[CH2:6][CH2:7][c:8]3[cH:9][cH:10][cH:11][cH:12][c:13]3[C@@H:14]2[CH2:15][N:16]1[CH2:17][c:18]1[cH:19][cH:20][cH:21...
BrCc1ccccc1.O=C1CC[C@@H]2CCc3ccccc3[C@@H]2CN1
O=C1CC[C@@H]2CCc3ccccc3[C@@H]2CN1Cc1ccccc1
null
null
C1CCOC1
Heteroatom Alkylation and Arylation
N-alkylation of secondary amines with alkyl halides
8d8dca04155cc1bc79249673a734d568d6a2f78b16832b1110970efacca8a1e5
4a6c1e88c9e8bed487b746792f88d478ff36cc235f9a217d4632e6babdebdc9a
O=C1CC[C@@H]2CCc3ccccc3[C@@H]2CN1Cc1ccccc1
Br-[CH2;D2;+0:1]-[c:2](:[c:3]):[c:4].[C:5]-[C:6]-[NH;D2;+0:7]-[C:8](=[O;D1;H0:9])-[C:10]>>[C:5]-[C:6]-[N;H0;D3;+0:7](-[CH2;D2;+0:1]-[c:2](:[c:3]):[c:4])-[C:8](=[O;D1;H0:9])-[C:10]
79
[{"value": 79.0, "product": "C(C1=CC=CC=C1)N1C[C@@H]2[C@H](CCC1=O)CCC1=CC=CC=C12", "details": "PERCENTYIELD", "is_desired": false}, {"value": 77.5, "product": "C(C1=CC=CC=C1)N1C[C@@H]2[C@H](CCC1=O)CCC1=CC=CC=C12", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
0.5
HOUR
To a suspension of cis-1,3,4,5,5a,6,7,11b-octahydro-3-oxo-2H-naphth[1,2-c]azepine (1.0 g, 4.65 mmol), from Step 3 of Example 75, in 20 mL of dry THF, was added potassium t-butoxide (0.78 g, 6.9 mmol). The reaction mixture was stirred at ambient temperature for 0.5 h and then cooled to 0° C. and benzyl bromide (0.8 mL, ...
10.6084/m9.figshare.5104873.v1
null
Primary halide.Secondary amide
Tertiary amide
c1ccc2c(c1)CC[C@H]1CCCNC[C@@H]21
c1ccc2c(c1)CC[C@H]1CCC[NH]C[C@@H]21
c1ccc2c(c1)CC[C@H]1CCC[NH]C[C@@H]21.c1ccccc1
HBr
C1CCOC1
null
0.5
BrCc1ccccc1.O=C1CC[C@@H]2CCc3ccccc3[C@@H]2CN1>C1CCOC1>O=C1CC[C@@H]2CCc3ccccc3[C@@H]2CN1Cc1ccccc1
ord_dataset-02ee2261663048188cf6d85d2cc96e3f
ord-f3ba761238a143e1b68d0ab2aac52f4d
C=C(C)C(=O)OCCO.CCOC(=O)C(=O)OCC>>C=C(C)C(=O)OCCOC(=O)C(=O)OCC
C(C(=C)C)(=O)OCCO.C(C(=O)OCC)(=O)OCC.C(C)O>>C(C(=C)C)(=O)OCCOC(=O)C(=O)OCC
[CH2:1]=[C:2]([CH3:3])[C:4](=[O:5])[O:6][CH2:7][CH2:8][OH:9].CCO[C:10](=[O:11])[C:12](=[O:13])[O:14][CH2:15][CH3:16]>>[CH2:1]=[C:2]([CH3:3])[C:4](=[O:5])[O:6][CH2:7][CH2:8][O:9][C:10](=[O:11])[C:12](=[O:13])[O:14][CH2:15][CH3:16]
C=C(C)C(=O)OCCO.CCOC(=O)C(=O)OCC
C=C(C)C(=O)OCCOC(=O)C(=O)OCC
null
C1(=CC=C(C=C1)S(=O)(=O)O)C.C1(O)=CC=C(O)C=C1
null
Acylation
Transesterification
78fca4eb4a1c9bfa8e423f92a9d12c264c52db88a588463b687f679a6641c521
b13152bdbecf5f32acc9bbb4c1c2e172eebaff97800b4381979bc284516946c9
null
C-C-O-[C;H0;D3;+0:1](=[O;D1;H0:2])-[C:3](=[O;D1;H0:4])-[#8:5]-[C:6].[C:7]-[C:8]-[OH;D1;+0:9]>>[C:6]-[#8:5]-[C:3](=[O;D1;H0:4])-[C;H0;D3;+0:1](=[O;D1;H0:2])-[O;H0;D2;+0:9]-[C:8]-[C:7]
76.5
[{"value": 76.5, "product": "C(C(=C)C)(=O)OCCOC(=O)C(=O)OCC", "details": "PERCENTYIELD", "is_desired": false}, {"value": 76.5, "product": "C(C(=C)C)(=O)OCCOC(=O)C(=O)OCC", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
4
HOUR
A 500 ml flask equipped with a decanter, a thermometer, a stirrer and an inlet for nitrogen gas was charged with 65.1 g (0.5 mol) of 2-hydroxyethyl methacrylate and 365.4 g (2.5 mol) of diethyl oxalate, to which 2 g (10 mmol) of p-toluenesulfonic acid (catalyst) and 4 g of hydroquinone (polymerization inhibitor) were a...
10.6084/m9.figshare.5104873.v1
null
Ester.Ester.Primary alcohol
Ester.Ester
null
null
null
HO-
C1(=CC=C(C=C1)S(=O)(=O)O)C.C1(O)=CC=C(O)C=C1
null
4
C=C(C)C(=O)OCCO.CCOC(=O)C(=O)OCC>C1(=CC=C(C=C1)S(=O)(=O)O)C.C1(O)=CC=C(O)C=C1>C=C(C)C(=O)OCCOC(=O)C(=O)OCC
ord_dataset-02ee2261663048188cf6d85d2cc96e3f
ord-5bb43bb802e74697b19c498517a29caa
C=C(C)C(=O)OCCO.CCOC(=O)C(=O)OCC>>C=C(C)C(=O)OCCOC(=O)C(=O)OCC
C(C(=C)C)(=O)OCCO.C(C(=O)OCC)(=O)OCC.C(C)O>>C(C(=C)C)(=O)OCCOC(=O)C(=O)OCC
[CH2:1]=[C:2]([CH3:3])[C:4](=[O:5])[O:6][CH2:7][CH2:8][OH:9].CCO[C:10](=[O:11])[C:12](=[O:13])[O:14][CH2:15][CH3:16]>>[CH2:1]=[C:2]([CH3:3])[C:4](=[O:5])[O:6][CH2:7][CH2:8][O:9][C:10](=[O:11])[C:12](=[O:13])[O:14][CH2:15][CH3:16]
C=C(C)C(=O)OCCO.CCOC(=O)C(=O)OCC
C=C(C)C(=O)OCCOC(=O)C(=O)OCC
null
C1(=CC=C(C=C1)S(=O)(=O)O)C.C(C)(C)(C)C1=C(O)C=CC(=C1)O
null
Acylation
Transesterification
78fca4eb4a1c9bfa8e423f92a9d12c264c52db88a588463b687f679a6641c521
b13152bdbecf5f32acc9bbb4c1c2e172eebaff97800b4381979bc284516946c9
null
C-C-O-[C;H0;D3;+0:1](=[O;D1;H0:2])-[C:3](=[O;D1;H0:4])-[#8:5]-[C:6].[C:7]-[C:8]-[OH;D1;+0:9]>>[C:6]-[#8:5]-[C:3](=[O;D1;H0:4])-[C;H0;D3;+0:1](=[O;D1;H0:2])-[O;H0;D2;+0:9]-[C:8]-[C:7]
76.5
[{"value": 76.5, "product": "C(C(=C)C)(=O)OCCOC(=O)C(=O)OCC", "details": "PERCENTYIELD", "is_desired": false}, {"value": 56.3, "product": "C(C(=C)C)(=O)OCCOC(=O)C(=O)OCC", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
3
HOUR
A 500 ml flask equipped with a decanter, a thermometer, a stirrer and an inlet for nitrogen gas was charged with 65.1 g (0.5 mol) of 2-hydroxyethyl methacrylate and 365.4 g (2.5 mol) of diethyl oxalate, to which 2 g (10 mmol) of p-toluenesulfonic acid (catalyst) and 4 g of 2-t-butylhydroquinone (polymerization inhibito...
10.6084/m9.figshare.5104873.v1
null
Ester.Ester.Primary alcohol
Ester.Ester
null
null
null
HO-
C1(=CC=C(C=C1)S(=O)(=O)O)C.C(C)(C)(C)C1=C(O)C=CC(=C1)O
null
3
C=C(C)C(=O)OCCO.CCOC(=O)C(=O)OCC>C1(=CC=C(C=C1)S(=O)(=O)O)C.C(C)(C)(C)C1=C(O)C=CC(=C1)O>C=C(C)C(=O)OCCOC(=O)C(=O)OCC
ord_dataset-02ee2261663048188cf6d85d2cc96e3f
ord-55437dbf90b64b46927be1c1700be2ac
C=C(C)C(=O)OCCO.CCOC(=O)C(=O)OCC>>C=C(C)C(=O)OCCOC(=O)C(=O)OCC
C(C(=C)C)(=O)OCCO.C(C(=O)OCC)(=O)OCC.C(C)O>>C(C(=C)C)(=O)OCCOC(=O)C(=O)OCC
[CH2:1]=[C:2]([CH3:3])[C:4](=[O:5])[O:6][CH2:7][CH2:8][OH:9].CCO[C:10](=[O:11])[C:12](=[O:13])[O:14][CH2:15][CH3:16]>>[CH2:1]=[C:2]([CH3:3])[C:4](=[O:5])[O:6][CH2:7][CH2:8][O:9][C:10](=[O:11])[C:12](=[O:13])[O:14][CH2:15][CH3:16]
C=C(C)C(=O)OCCO.CCOC(=O)C(=O)OCC
C=C(C)C(=O)OCCOC(=O)C(=O)OCC
null
C1(=CC=C(C=C1)S(=O)(=O)O)C.C(C)(C)(C)C1=C(O)C=C(C(=C1)O)C(C)(C)C
null
Acylation
Transesterification
78fca4eb4a1c9bfa8e423f92a9d12c264c52db88a588463b687f679a6641c521
b13152bdbecf5f32acc9bbb4c1c2e172eebaff97800b4381979bc284516946c9
null
C-C-O-[C;H0;D3;+0:1](=[O;D1;H0:2])-[C:3](=[O;D1;H0:4])-[#8:5]-[C:6].[C:7]-[C:8]-[OH;D1;+0:9]>>[C:6]-[#8:5]-[C:3](=[O;D1;H0:4])-[C;H0;D3;+0:1](=[O;D1;H0:2])-[O;H0;D2;+0:9]-[C:8]-[C:7]
56.3
[{"value": 52.4, "product": "C(C(=C)C)(=O)OCCOC(=O)C(=O)OCC", "details": "PERCENTYIELD", "is_desired": false}, {"value": 56.3, "product": "C(C(=C)C)(=O)OCCOC(=O)C(=O)OCC", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
3
HOUR
A 500 ml flask equipped with a decanter, a thermometer, a stirrer and an inlet for nitrogen gas was charged with 65.1 g (0.5 mol) of 2-hydroxyethyl methacrylate and 365.4 g (2.5 mol) of diethyl oxalate, to which 2 g (10 mmol) of p-toluenesulfonic acid (catalyst) and 4 g of 2,5-di-t-butylhydroquinone (polymerization inh...
10.6084/m9.figshare.5104873.v1
null
Ester.Ester.Primary alcohol
Ester.Ester
null
null
null
HO-
C1(=CC=C(C=C1)S(=O)(=O)O)C.C(C)(C)(C)C1=C(O)C=C(C(=C1)O)C(C)(C)C
null
3
C=C(C)C(=O)OCCO.CCOC(=O)C(=O)OCC>C1(=CC=C(C=C1)S(=O)(=O)O)C.C(C)(C)(C)C1=C(O)C=C(C(=C1)O)C(C)(C)C>C=C(C)C(=O)OCCOC(=O)C(=O)OCC
ord_dataset-02ee2261663048188cf6d85d2cc96e3f
ord-1e1b570bc8ce444bb33a68c096a4880b
C=C(C)C(=O)OCCO.CCOC(=O)C(=O)OCC>>C=C(C)C(=O)OCCOC(=O)C(=O)OCC
C(C(=C)C)(=O)OCCO.C(C(=O)OCC)(=O)OCC.C(C)O>>C(C(=C)C)(=O)OCCOC(=O)C(=O)OCC
[CH2:1]=[C:2]([CH3:3])[C:4](=[O:5])[O:6][CH2:7][CH2:8][OH:9].CCO[C:10](=[O:11])[C:12](=[O:13])[O:14][CH2:15][CH3:16]>>[CH2:1]=[C:2]([CH3:3])[C:4](=[O:5])[O:6][CH2:7][CH2:8][O:9][C:10](=[O:11])[C:12](=[O:13])[O:14][CH2:15][CH3:16]
C=C(C)C(=O)OCCO.CCOC(=O)C(=O)OCC
C=C(C)C(=O)OCCOC(=O)C(=O)OCC
null
C(CCCCCCCCCCC)(=O)[O-].C(CCCCCCCCCCC)(=O)[O-].C(CCC)[Sn+2]CCCC.C(C)(C)(C)C1=C(O)C=C(C(=C1)O)C(C)(C)C
null
Acylation
Transesterification
78fca4eb4a1c9bfa8e423f92a9d12c264c52db88a588463b687f679a6641c521
b13152bdbecf5f32acc9bbb4c1c2e172eebaff97800b4381979bc284516946c9
null
C-C-O-[C;H0;D3;+0:1](=[O;D1;H0:2])-[C:3](=[O;D1;H0:4])-[#8:5]-[C:6].[C:7]-[C:8]-[OH;D1;+0:9]>>[C:6]-[#8:5]-[C:3](=[O;D1;H0:4])-[C;H0;D3;+0:1](=[O;D1;H0:2])-[O;H0;D2;+0:9]-[C:8]-[C:7]
73.2
[{"value": 73.2, "product": "C(C(=C)C)(=O)OCCOC(=O)C(=O)OCC", "details": "PERCENTYIELD", "is_desired": false}, {"value": 73.1, "product": "C(C(=C)C)(=O)OCCOC(=O)C(=O)OCC", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
null
null
A 500 ml flask equipped with a decanter, a thermometer, a stirrer and an inlet for nitrogen gas was charged with 65.1 g (0.5 mol) of 2-hydroxyethyl methacrylate and 365.4 g (2.5 mol) of diethyl oxalate, to which 2 g (10 mmol) of dibutyltin dilaurate (catalyst) and 4 g of 2,5-di-t-butylhydroquinone (polymerization inhib...
10.6084/m9.figshare.5104873.v1
null
Ester.Ester.Primary alcohol
Ester.Ester
null
null
null
HO-
C(CCCCCCCCCCC)(=O)[O-].C(CCCCCCCCCCC)(=O)[O-].C(CCC)[Sn+2]CCCC.C(C)(C)(C)C1=C(O)C=C(C(=C1)O)C(C)(C)C
null
null
C=C(C)C(=O)OCCO.CCOC(=O)C(=O)OCC>C(CCCCCCCCCCC)(=O)[O-].C(CCCCCCCCCCC)(=O)[O-].C(CCC)[Sn+2]CCCC.C(C)(C)(C)C1=C(O)C=C(C(=C1)O)C(C)(C)C>C=C(C)C(=O)OCCOC(=O)C(=O)OCC
ord_dataset-02ee2261663048188cf6d85d2cc96e3f
ord-eb42087260a94c678501a68bb3d83b03
C=Cc1ccc(CCO)cc1.CCOC(=O)C(=O)Cl>>C=Cc1ccc(CCOC(=O)C(=O)OCC)cc1
C(=O)(C(=O)OCC)Cl.OCCC1=CC=C(C=C)C=C1.C(C)N(CC)CC>>C(=O)(C(=O)OCC)OCCC1=CC=C(C=C)C=C1
[CH2:1]=[CH:2][c:3]1[cH:4][cH:5][c:6]([CH2:7][CH2:8][OH:9])[cH:17][cH:18]1.Cl[C:10](=[O:11])[C:12](=[O:13])[O:14][CH2:15][CH3:16]>>[CH2:1]=[CH:2][c:3]1[cH:4][cH:5][c:6]([CH2:7][CH2:8][O:9][C:10](=[O:11])[C:12](=[O:13])[O:14][CH2:15][CH3:16])[cH:17][cH:18]1
C=Cc1ccc(CCO)cc1.CCOC(=O)C(=O)Cl
C=Cc1ccc(CCOC(=O)C(=O)OCC)cc1
null
null
C1=CC=CC=C1
Acylation
Schotten-Baumann to ester
c6e09616b6bb08f487e50f4272dd934070dd97cfdd94b0ca77f05cb1b1832016
674ca7f6a5419c8179935ec7795e4632b99c82de6c610aa384dddefb222306c5
c1ccccc1
Cl-[C;H0;D3;+0:1](=[O;D1;H0:2])-[C:3](=[O;D1;H0:4])-[#8:5]-[C:6].[C:7]-[C:8]-[OH;D1;+0:9]>>[C:6]-[#8:5]-[C:3](=[O;D1;H0:4])-[C;H0;D3;+0:1](=[O;D1;H0:2])-[O;H0;D2;+0:9]-[C:8]-[C:7]
null
[]
10
CELSIUS
2
HOUR
A 200 ml flask equipped with a stirrer, a thermometer and a dropping funnel was charged with 14.8 g (0.1 mol) of p-hydroxyethylstyrene, 150 ml of benzene and 10.1 g (0.1 mol) of triethylamine and cooled to 10° C. To the mixture was added dropwise with stirring 13.7 g (0.1 mol) of ethoxalyl chloride for one hour at 10° ...
10.6084/m9.figshare.5104873.v1
null
Acyl halide.Ester.Primary alcohol
Ester.Ester
null
null
c1ccccc1
HCl
C1=CC=CC=C1
10
2
C=Cc1ccc(CCO)cc1.CCOC(=O)C(=O)Cl>C1=CC=CC=C1>C=Cc1ccc(CCOC(=O)C(=O)OCC)cc1
ord_dataset-02ee2261663048188cf6d85d2cc96e3f
ord-52ecedb5e4fd4c16b5bdf50423b6140d
CCCCCCCCCCCCN.[N-]=C=O>>CCCCCCCCCCCCNC(N)=O
[N-]=C=O.C(C)[NH+](CC)CC.C(CCCCCCCCCCC)N>>C(CCCCCCCCCCC)NC(=O)N
[CH3:1][CH2:2][CH2:3][CH2:4][CH2:5][CH2:6][CH2:7][CH2:8][CH2:9][CH2:10][CH2:11][CH2:12][NH2:13].[C:14](=[N-:15])=[O:16]>>[CH3:1][CH2:2][CH2:3][CH2:4][CH2:5][CH2:6][CH2:7][CH2:8][CH2:9][CH2:10][CH2:11][CH2:12][NH:13][C:14]([NH2:15])=[O:16]
CCCCCCCCCCCCN.[N-]=C=O
CCCCCCCCCCCCNC(N)=O
null
null
C(Cl)(Cl)Cl
Acylation
OtherReaction
fec8ce0db817cb9adf4794b3c5ae318c150decedadcebfebfdf328f25035cc8e
4cf759e067568cc19d6858be8959598bd5316ab2ab31ad8bd54dcb75f9008a64
null
[C:1]-[C:2]-[NH2;D1;+0:3].[N-;H0;D1:4]=[C;H0;D2;+0:5]=[O;D1;H0:6]>>[C:1]-[C:2]-[NH;D2;+0:3]-[C;H0;D3;+0:5](-[NH2;D1;+0:4])=[O;D1;H0:6]
null
[]
null
null
24
HOUR
14.1 g of dodecylamine (0.076 mol) dissolved in 20 ml of chloroform were added dropwise at room temperature with stirring to 100 ml of a solution of 10 g of triethylammonium isocyanate (0.069 mol) in chloroform, prepared according to Example 1. After completion of the addition, the mixture was subsequently stirred at r...
10.6084/m9.figshare.5104873.v1
null
Primary amine
Urea
null
null
null
null
C(Cl)(Cl)Cl
null
24
CCCCCCCCCCCCN.[N-]=C=O>C(Cl)(Cl)Cl>CCCCCCCCCCCCNC(N)=O
ord_dataset-02ee2261663048188cf6d85d2cc96e3f
ord-26e9cd6443ee4b97a309ce9dc3dbdef8
CN1CCCC1=O.NCCN.[N-]=C=O>>NC(=O)NCCNC(N)=O
C(CN)N.[N-]=C=O.CN1C(CCC1)=O>>C(CNC(=O)N)NC(=O)N
C[N:9]1CCC[C:8]1=[O:10].[NH2:4][CH2:5][CH2:6][NH2:7].[N-:1]=[C:2]=[O:3]>>[NH2:1][C:2](=[O:3])[NH:4][CH2:5][CH2:6][NH:7][C:8]([NH2:9])=[O:10]
CN1CCCC1=O.NCCN.[N-]=C=O
NC(=O)NCCNC(N)=O
null
null
null
Acylation
OtherReaction
2efad4ea4a1121c37bb39638d410230c9d1a1c77ba696ac1e25eef30dd987541
8cbc7b37abe41435ec5cf68add2d69d8e3a37c171dc02737548783ea182dfec6
null
C-[N;H0;D3;+0:1]1-C-C-C-[C;H0;D3;+0:2]-1=[O;D1;H0:3].[N-;H0;D1:4]=[C;H0;D2;+0:5]=[O;D1;H0:6].[NH2;D1;+0:7]-[C:8]-[C:9]-[NH2;D1;+0:10]>>[NH2;D1;+0:4]-[C;H0;D3;+0:5](=[O;D1;H0:6])-[NH;D2;+0:7]-[C:8]-[C:9]-[NH;D2;+0:10]-[C;H0;D3;+0:2](-[NH2;D1;+0:1])=[O;D1;H0:3]
null
[]
null
null
24
HOUR
1.88 g of ethylenediamine (0.031 mol) were added dropwise at room temperature with stirring to 100 ml of a solution of 10 g of triethylammonum isocyanate (0.069 mol) in 100 ml of N-methylpyrrolidone, prepared according to the procedure described in example 1. After stirring at room temperature for 24 hours, the reactio...
10.6084/m9.figshare.5104873.v1
null
Tertiary amide.Primary amine.Primary amine
Urea.Urea
C1CC[NH]C1
null
null
Other
null
null
24
CN1CCCC1=O.NCCN.[N-]=C=O>>NC(=O)NCCNC(N)=O
ord_dataset-02ee2261663048188cf6d85d2cc96e3f
ord-708d04ef70ce40fc929d6ad0b2ca124d
CCCCCCCCCCCCCCCCCCS.CN1CCCC1=O>>CCCCCCCCCCCCCCCCCCSC(N)=O
C(CCCCCCCCCCCCCCCCC)S.CN1C(CCC1)=O>>C(N)(SCCCCCCCCCCCCCCCCCC)=O
[CH3:1][CH2:2][CH2:3][CH2:4][CH2:5][CH2:6][CH2:7][CH2:8][CH2:9][CH2:10][CH2:11][CH2:12][CH2:13][CH2:14][CH2:15][CH2:16][CH2:17][CH2:18][SH:19].C[N:21]1CCC[C:20]1=[O:22]>>[CH3:1][CH2:2][CH2:3][CH2:4][CH2:5][CH2:6][CH2:7][CH2:8][CH2:9][CH2:10][CH2:11][CH2:12][CH2:13][CH2:14][CH2:15][CH2:16][CH2:17][CH2:18][S:19][C:20]([N...
CCCCCCCCCCCCCCCCCCS.CN1CCCC1=O
CCCCCCCCCCCCCCCCCCSC(N)=O
null
null
null
Acylation
OtherReaction
a70866c63b7b54ba7c2787885997ec190749b75aa5b80e249358347801022ac5
0ab955a5e6cea8ebd0db5bdf3ed34fbfdf14dbc1d37769d97c6058ae7d4a56ac
null
C-[N;H0;D3;+0:1]1-C-C-C-[C;H0;D3;+0:2]-1=[O;D1;H0:3].[C:4]-[C:5]-[SH;D1;+0:6]>>[C:4]-[C:5]-[S;H0;D2;+0:6]-[C;H0;D3;+0:2](-[NH2;D1;+0:1])=[O;D1;H0:3]
60
[{"value": 60.0, "product": "C(N)(SCCCCCCCCCCCCCCCCCC)=O", "details": "PERCENTYIELD", "is_desired": false}]
null
null
null
null
As described in Example 17, but using 63 g of 1-octadecylmercaptan (0.22 mol) dissolved in 30 ml of N-methylpyrrolidone, S-octadecyl thiocarbamate was obtained in a yield of 60% of theory. Conditions: See reaction.notes.procedure_details.
10.6084/m9.figshare.5104873.v1
null
Tertiary amide.Aliphatic thiol
Primary amide.Monosulfide
C1CC[NH]C1
null
null
Other
null
null
null
CCCCCCCCCCCCCCCCCCS.CN1CCCC1=O>>CCCCCCCCCCCCCCCCCCSC(N)=O
ord_dataset-02ee2261663048188cf6d85d2cc96e3f
ord-9f8135fc2ea3458ea13011035828fec5
CC(C)N=C(O)N(Cc1ccccc1)C(C)C.C[C@H](O)C(=O)O>>CC(O)C(=O)OCc1ccccc1
C(C1=CC=CC=C1)[C@](C(=O)O)(O)C.C([C@@H](O)C)(=O)O.C(C)(C)N(C(O)=NC(C)C)CC1=CC=CC=C1>>C(C(O)C)(=O)OCC1=CC=CC=C1
CC(C)N=C(O)N(C(C)C)[CH2:7][c:8]1[cH:9][cH:10][cH:11][cH:12][cH:13]1.[CH3:1][C@H:2]([OH:3])[C:4](=[O:5])[OH:6]>>[CH3:1][CH:2]([OH:3])[C:4](=[O:5])[O:6][CH2:7][c:8]1[cH:9][cH:10][cH:11][cH:12][cH:13]1
CC(C)N=C(O)N(Cc1ccccc1)C(C)C.C[C@H](O)C(=O)O
CC(O)C(=O)OCc1ccccc1
null
null
C1CCOC1
Heteroatom Alkylation and Arylation
OtherReaction
8ba133f06c4c0df103dfa8d83a3ae1c8f954a895eb15a5679d75dae29435b369
99f5e58a6f94b05681979232ec71674baa8e98488f497e30fe94f5f9a191f8d9
c1ccccc1
C-C(-C)-N=C(-O)-N(-[CH2;D2;+0:1]-[c:2](:[c:3]):[c:4])-C(-C)-C.[C:5]-[C:6](=[O;D1;H0:7])-[OH;D1;+0:8]>>[C:5]-[C:6](=[O;D1;H0:7])-[O;H0;D2;+0:8]-[CH2;D2;+0:1]-[c:2](:[c:3]):[c:4]
95
[{"value": 95.0, "product": "C(C(O)C)(=O)OCC1=CC=CC=C1", "details": "PERCENTYIELD", "is_desired": false}]
-15
CELSIUS
10
MINUTE
Construction of Benzyl-L-lactic Acid. L-Lactic acid (9 g, 100 mmol) is added to N,N'-diisopropylbenzylisourea (23.3 g, 100 mmol) with stirring. The mixture becomes very viscous within 10 min and is stirred intermittently for 1 h. The volume is then increased to 200 mL with THF, and the mixture stirred for 48 h at room ...
10.6084/m9.figshare.5104873.v1
null
Carboxylic acid.Tertiary amine
Ester
null
null
c1ccccc1
HO-
C1CCOC1
-15
0.166667
CC(C)N=C(O)N(Cc1ccccc1)C(C)C.C[C@H](O)C(=O)O>C1CCOC1>CC(O)C(=O)OCc1ccccc1
ord_dataset-02ee2261663048188cf6d85d2cc96e3f
ord-5c317f14cf624df39c513f9852247f2b
CC(C)N=C(O)N(Cc1ccccc1)C(C)C.O=C(O)CO>>O=C(CO)OCc1ccccc1
C(C1=CC=CC=C1)C(C(=O)O)O.C(CO)(=O)O.C(C)(C)N(C(O)=NC(C)C)CC1=CC=CC=C1>>C(CO)(=O)OCC1=CC=CC=C1
CC(C)N=C(O)N(C(C)C)[CH2:6][c:7]1[cH:8][cH:9][cH:10][cH:11][cH:12]1.[O:1]=[C:2]([CH2:3][OH:4])[OH:5]>>[O:1]=[C:2]([CH2:3][OH:4])[O:5][CH2:6][c:7]1[cH:8][cH:9][cH:10][cH:11][cH:12]1
CC(C)N=C(O)N(Cc1ccccc1)C(C)C.O=C(O)CO
O=C(CO)OCc1ccccc1
null
null
C1CCOC1
Heteroatom Alkylation and Arylation
OtherReaction
8ba133f06c4c0df103dfa8d83a3ae1c8f954a895eb15a5679d75dae29435b369
99f5e58a6f94b05681979232ec71674baa8e98488f497e30fe94f5f9a191f8d9
c1ccccc1
C-C(-C)-N=C(-O)-N(-[CH2;D2;+0:1]-[c:2](:[c:3]):[c:4])-C(-C)-C.[C:5]-[C:6](=[O;D1;H0:7])-[OH;D1;+0:8]>>[C:5]-[C:6](=[O;D1;H0:7])-[O;H0;D2;+0:8]-[CH2;D2;+0:1]-[c:2](:[c:3]):[c:4]
null
[]
-15
CELSIUS
1
HOUR
Construction of Benzyl-glycolic Acid. Glycolic acid (7.69,100 mmols) is added to N,N'-diisopropylbenzylisourea (23.39,100 mmols) with stirring for 1 hour. The volume is then increased to 200 mL with THF, and the mixture stirred for 48 h at room temperature. After cooling the mixture to -15° C., the diisopropylurea is r...
10.6084/m9.figshare.5104873.v1
null
Carboxylic acid.Tertiary amine
Ester
null
null
c1ccccc1
HO-
C1CCOC1
-15
1
CC(C)N=C(O)N(Cc1ccccc1)C(C)C.O=C(O)CO>C1CCOC1>O=C(CO)OCc1ccccc1
ord_dataset-02ee2261663048188cf6d85d2cc96e3f
ord-306e2fc44682415ab97ed11fe0b4fe4d
O=C(O)c1ccc(O)cc1.O=C=Nc1ccc([N+](=O)[O-])cc1>>O=C(Nc1ccc([N+](=O)[O-])cc1)c1ccc(O)cc1
OC1=CC=C(C(=O)O)C=C1.[N+](=O)([O-])C1=CC=C(C=C1)N=C=O.[N+](=O)([O-])C1=CC=C(C=C1)N=C=O.OC1=CC=C(C(=O)O)C=C1>>OC1=CC=C(C(=O)NC2=CC=C(C=C2)[N+](=O)[O-])C=C1
O=C(O)[c:13]1[cH:14][cH:15][c:16]([OH:17])[cH:18][cH:19]1.[O:1]=[C:2]=[N:3][c:4]1[cH:5][cH:6][c:7]([N+:8](=[O:9])[O-:10])[cH:11][cH:12]1>>[O:1]=[C:2]([NH:3][c:4]1[cH:5][cH:6][c:7]([N+:8](=[O:9])[O-:10])[cH:11][cH:12]1)[c:13]1[cH:14][cH:15][c:16]([OH:17])[cH:18][cH:19]1
O=C(O)c1ccc(O)cc1.O=C=Nc1ccc([N+](=O)[O-])cc1
O=C(Nc1ccc([N+](=O)[O-])cc1)c1ccc(O)cc1
null
[O-]CC.[Na+]
O
Acylation
OtherReaction
0a4f9f839bd76ff42d7022423fd0d57ba4af4e525edf9af136996b41a6d77a9a
8cd051de7c4ef961c82855c2d4826ac655c3097ad2a955f94089daf3fea36350
O=C(Nc1ccccc1)c1ccccc1
O-C(=O)-[c;H0;D3;+0:1](:[c:2]:[c:3]):[c:4]:[c:5].[O;D1;H0:6]=[C;H0;D2;+0:7]=[N;H0;D2;+0:8]-[c:9](:[c:10]):[c:11]>>[O;D1;H0:6]=[C;H0;D3;+0:7](-[NH;D2;+0:8]-[c:9](:[c:10]):[c:11])-[c;H0;D3;+0:1](:[c:2]:[c:3]):[c:4]:[c:5]
null
[]
30
CELSIUS
24
MINUTE
p-Hydroxybenzoic acid (59.05 grams, 0.4275 mole), sodium ethoxide catalyst (0.133 gram, 0.225% wt. of the p-hydroxybenzoic acid used) and N,N'-dimethylacetamide solvent (404 grams) are added to a reactor equipped with a reflux condenser and stirred under a nitrogen atmosphere at 80° C. p-Nitrophenylisocyanate (73.85 gr...
10.6084/m9.figshare.5104873.v1
null
Carboxylic acid.Isocyanate
Secondary amide
c1ccccc1
c1ccccc1
c1ccccc1.c1ccccc1
Other
[O-]CC.[Na+].O
30
0.4
O=C(O)c1ccc(O)cc1.O=C=Nc1ccc([N+](=O)[O-])cc1>[O-]CC.[Na+].O>O=C(Nc1ccc([N+](=O)[O-])cc1)c1ccc(O)cc1
ord_dataset-02ee2261663048188cf6d85d2cc96e3f
ord-dedaac03465d424890205b49f02a8944
O=C(Nc1ccc([N+](=O)[O-])cc1)c1ccc(O)cc1>>Nc1ccc(NC(=O)c2ccc(O)cc2)cc1
OC1=CC=C(C(=O)NC2=CC=C(C=C2)[N+](=O)[O-])C=C1>>OC1=CC=C(C(=O)NC2=CC=C(C=C2)N)C=C1
O=[N+:1]([O-])[c:2]1[cH:3][cH:4][c:5]([NH:6][C:7](=[O:8])[c:9]2[cH:10][cH:11][c:12]([OH:13])[cH:14][cH:15]2)[cH:16][cH:17]1>>[NH2:1][c:2]1[cH:3][cH:4][c:5]([NH:6][C:7](=[O:8])[c:9]2[cH:10][cH:11][c:12]([OH:13])[cH:14][cH:15]2)[cH:16][cH:17]1
O=C(Nc1ccc([N+](=O)[O-])cc1)c1ccc(O)cc1
Nc1ccc(NC(=O)c2ccc(O)cc2)cc1
null
null
C(C)O
Reduction
Reduction of nitro groups to amines
bbc242b150a51e69d3ad1caaa391f4422710431b398dcb880555f476706790be
7b0317532ea57a4fcedc1efc3e3c22eb5238d1c8330da53d4f9801fc2391f567
O=C(Nc1ccccc1)c1ccccc1
O=[N+;H0;D3:1](-[O-])-[c:2](:[c:3]):[c:4]>>[NH2;D1;+0:1]-[c:2](:[c:3]):[c:4]
null
[]
25
CELSIUS
23.3
HOUR
A portion (44.1 grams, 0.1708 mole) of 4-hydroxy-4'-nitrobenzanilide from A. above and ethanol (300 milliliters) are added to a 400 milliliter heavy walled glass bottle then sparged with nitrogen. After removal of air by nitrogen sparaing, Raney nickel catalyst (5.5 grams of a 75% wt. slurry in water at pH 10) is added...
10.6084/m9.figshare.5104873.v1
null
Nitro group
Primary amine
null
null
c1ccccc1.c1ccccc1
Other
C(C)O
25
23.3
O=C(Nc1ccc([N+](=O)[O-])cc1)c1ccc(O)cc1>C(C)O>Nc1ccc(NC(=O)c2ccc(O)cc2)cc1
ord_dataset-02ee2261663048188cf6d85d2cc96e3f
ord-b470b03ef0a74e3ea56e7f31c8f25984
CC(=O)OC(C)=O.O=C(O)Cc1ccc([N+](=O)[O-])cc1.O=Cc1ccc(O)cc1>>CC(=O)Oc1ccc(C=C(C(=O)O)c2ccc([N+](=O)[O-])cc2)cc1
OC1=CC=C(C=O)C=C1.C(C)(=O)OC(C)=O.[N+](=O)([O-])C1=CC=C(C=C1)CC(=O)O.[OH-].[Na+]>>[N+](=O)([O-])C1=CC=C(C=C1)C(C(=O)O)=CC1=CC=C(C=C1)OC(C)=O
CC(=O)O[C:2]([CH3:1])=[O:3].[CH2:10]([C:11](=[O:12])[OH:13])[c:14]1[cH:15][cH:16][c:17]([N+:18](=[O:19])[O-:20])[cH:21][cH:22]1.O=[CH:9][c:8]1[cH:7][cH:6][c:5]([OH:4])[cH:24][cH:23]1>>[CH3:1][C:2](=[O:3])[O:4][c:5]1[cH:6][cH:7][c:8]([CH:9]=[C:10]([C:11](=[O:12])[OH:13])[c:14]2[cH:15][cH:16][c:17]([N+:18](=[O:19])[O-:20...
CC(=O)OC(C)=O.O=C(O)Cc1ccc([N+](=O)[O-])cc1.O=Cc1ccc(O)cc1
CC(=O)Oc1ccc(C=C(C(=O)O)c2ccc([N+](=O)[O-])cc2)cc1
null
null
C(C)O.O
C-C Coupling
OtherReaction
24a5e5e840ab45f5ac71997b75bf9c9458ee729ce4846b47c2e20c66771f0961
6c4f18f39f8669eaadd9c3cc600e61ebad6b18d43c79a6714cb972028b541e8a
C(=Cc1ccccc1)c1ccccc1
C-C(=O)-O-[C;H0;D3;+0:1](-[C;D1;H3:2])=[O;D1;H0:3].O=[CH;D2;+0:4]-[c:5]1:[c:6]:[c:7]:[c:8](-[OH;D1;+0:9]):[c:10]:[c:11]:1.[O;D1;H0:12]=[C:13](-[O;D1;H1:14])-[CH2;D2;+0:15]-[c:16](:[c:17]):[c:18]>>[C;D1;H3:2]-[C;H0;D3;+0:1](=[O;D1;H0:3])-[O;H0;D2;+0:9]-[c:8]1:[c:7]:[c:6]:[c:5](-[CH;D2;+0:4]=[C;H0;D3;+0:15](-[C:13](=[O;D...
null
[]
60
CELSIUS
null
null
p-Nitrophenylacetic acid (94.02 grams, 0.519 mole) and 1.038 N sodium hydroxide solution (500 mL) are added to a 1,000 mL beaker and heated with stirring to 60° C. The resultant solution is rotary evaporated under vacuum until final conditions of 110° C. and 1 mm Hg are achieved and maintained for 30 minutes. A portion...
10.6084/m9.figshare.5104873.v1
null
Anhydride.Aldehyde.Aromatic alcohol
Ester
null
null
c1ccccc1.c1ccccc1
HO-
C(C)O.O
60
null
CC(=O)OC(C)=O.O=C(O)Cc1ccc([N+](=O)[O-])cc1.O=Cc1ccc(O)cc1>C(C)O.O>CC(=O)Oc1ccc(C=C(C(=O)O)c2ccc([N+](=O)[O-])cc2)cc1
ord_dataset-02ee2261663048188cf6d85d2cc96e3f
ord-d00a375e72f0484ca91396b30c1a39d9
CC(=O)Oc1ccc(C=C(C(=O)O)c2ccc([N+](=O)[O-])cc2)cc1>>O=[N+]([O-])c1ccc(C=Cc2ccc(O)cc2)cc1
[N+](=O)([O-])C1=CC=C(C=C1)C(C(=O)O)=CC1=CC=C(C=C1)OC(C)=O.C(C)O.Cl>>[N+](=O)([O-])C1=CC=C(C=C1)C=CC1=CC=C(C=C1)O
CC(=O)[O:14][c:13]1[cH:12][cH:11][c:10]([CH:9]=[C:8](C(=O)O)[c:7]2[cH:6][cH:5][c:4]([N+:2](=[O:1])[O-:3])[cH:18][cH:17]2)[cH:16][cH:15]1>>[O:1]=[N+:2]([O-:3])[c:4]1[cH:5][cH:6][c:7]([CH:8]=[CH:9][c:10]2[cH:11][cH:12][c:13]([OH:14])[cH:15][cH:16]2)[cH:17][cH:18]1
CC(=O)Oc1ccc(C=C(C(=O)O)c2ccc([N+](=O)[O-])cc2)cc1
O=[N+]([O-])c1ccc(C=Cc2ccc(O)cc2)cc1
null
null
O
Reduction
OtherReaction
63d7b9aaad312e5baffeb44abd9c90e266b4780604401c57bad121dfb88a1b0f
cdacdbe1471398702b32f2e73cf8a0e6eb084eb181796c9ace64f43ec88059ea
C(=Cc1ccccc1)c1ccccc1
C-C(=O)-[O;H0;D2;+0:1]-[c:2](:[c:3]):[c:4].O-C(=O)-[C;H0;D3;+0:5](=[C:6]-[c:7])-[c:8](:[c:9]):[c:10]>>[OH;D1;+0:1]-[c:2](:[c:3]):[c:4].[c:7]-[C:6]=[CH;D2;+0:5]-[c:8](:[c:9]):[c:10]
null
[]
95
CELSIUS
null
null
A portion (36.75 grams) of a-p-nitrophenyl-p-acetoxycinnamic acid from A. above, ethanol (300 mL) and concentrated hydrochloric acid (300 mL) are added to a reactor equipped with a reflux condenser and stirred under a nitrogen atmosphere. Heating commenced and a reflux is achieved at 93° C. Refluxing continued over the...
10.6084/m9.figshare.5104873.v1
null
Carboxylic acid.Ester
Aromatic alcohol
null
null
c1ccccc1.c1ccccc1
HO-
O
95
null
CC(=O)Oc1ccc(C=C(C(=O)O)c2ccc([N+](=O)[O-])cc2)cc1>O>O=[N+]([O-])c1ccc(C=Cc2ccc(O)cc2)cc1
ord_dataset-02ee2261663048188cf6d85d2cc96e3f
ord-f8a59aa44ce44b84b554ec20435346e3
O=[N+]([O-])c1ccc(C=Cc2ccc(O)cc2)cc1>>Nc1ccc(C=Cc2ccc(O)cc2)cc1
[N+](=O)([O-])C1=CC=C(C=C1)C=CC1=CC=C(C=C1)O>>OC1=CC=C(C=C1)C=CC1=CC=C(C=C1)N
O=[N+:1]([O-])[c:2]1[cH:3][cH:4][c:5]([CH:6]=[CH:7][c:8]2[cH:9][cH:10][c:11]([OH:12])[cH:13][cH:14]2)[cH:15][cH:16]1>>[NH2:1][c:2]1[cH:3][cH:4][c:5]([CH:6]=[CH:7][c:8]2[cH:9][cH:10][c:11]([OH:12])[cH:13][cH:14]2)[cH:15][cH:16]1
O=[N+]([O-])c1ccc(C=Cc2ccc(O)cc2)cc1
Nc1ccc(C=Cc2ccc(O)cc2)cc1
null
null
C(C)O
Reduction
Reduction of nitro groups to amines
bbc242b150a51e69d3ad1caaa391f4422710431b398dcb880555f476706790be
7b0317532ea57a4fcedc1efc3e3c22eb5238d1c8330da53d4f9801fc2391f567
C(=Cc1ccccc1)c1ccccc1
O=[N+;H0;D3:1](-[O-])-[c:2](:[c:3]):[c:4]>>[NH2;D1;+0:1]-[c:2](:[c:3]):[c:4]
null
[]
25
CELSIUS
28.5
HOUR
A portion (20.9 grams, 0.0866 mole) of 4-nitro-4'-hydroxystilbene from B. above and ethanol (300 mL) are added to a 400 milliliter heavy walled glass bottle then sparged with nitrogen. After removal of air by nitrogen sparging, Raney nickel catalyst (2.5 grams of a 50% wt. slurry in water at pH 10) is washed one time w...
10.6084/m9.figshare.5104873.v1
null
Nitro group
Primary amine
null
null
c1ccccc1.c1ccccc1
Other
C(C)O
25
28.5
O=[N+]([O-])c1ccc(C=Cc2ccc(O)cc2)cc1>C(C)O>Nc1ccc(C=Cc2ccc(O)cc2)cc1
ord_dataset-02ee2261663048188cf6d85d2cc96e3f
ord-144d23a00694409eac516557c38a54b0
O=C(O)c1ccc(O)cc1.O=C=Nc1ccc([N+](=O)[O-])cc1>>O=C(Nc1ccc([N+](=O)[O-])cc1)c1ccc(O)cc1
OC1=CC=C(C(=O)O)C=C1.[N+](=O)([O-])C1=CC=C(C=C1)N=C=O.[N+](=O)([O-])C1=CC=C(C=C1)N=C=O.OC1=CC=C(C(=O)O)C=C1>>OC1=CC=C(C(=O)NC2=CC=C(C=C2)[N+](=O)[O-])C=C1
O=C(O)[c:13]1[cH:14][cH:15][c:16]([OH:17])[cH:18][cH:19]1.[O:1]=[C:2]=[N:3][c:4]1[cH:5][cH:6][c:7]([N+:8](=[O:9])[O-:10])[cH:11][cH:12]1>>[O:1]=[C:2]([NH:3][c:4]1[cH:5][cH:6][c:7]([N+:8](=[O:9])[O-:10])[cH:11][cH:12]1)[c:13]1[cH:14][cH:15][c:16]([OH:17])[cH:18][cH:19]1
O=C(O)c1ccc(O)cc1.O=C=Nc1ccc([N+](=O)[O-])cc1
O=C(Nc1ccc([N+](=O)[O-])cc1)c1ccc(O)cc1
null
[O-]CC.[Na+]
O
Acylation
OtherReaction
0a4f9f839bd76ff42d7022423fd0d57ba4af4e525edf9af136996b41a6d77a9a
8cd051de7c4ef961c82855c2d4826ac655c3097ad2a955f94089daf3fea36350
O=C(Nc1ccccc1)c1ccccc1
O-C(=O)-[c;H0;D3;+0:1](:[c:2]:[c:3]):[c:4]:[c:5].[O;D1;H0:6]=[C;H0;D2;+0:7]=[N;H0;D2;+0:8]-[c:9](:[c:10]):[c:11]>>[O;D1;H0:6]=[C;H0;D3;+0:7](-[NH;D2;+0:8]-[c:9](:[c:10]):[c:11])-[c;H0;D3;+0:1](:[c:2]:[c:3]):[c:4]:[c:5]
null
[]
30
CELSIUS
24
MINUTE
p-Hydroxybenzoic acid (59.05 grams, 0.4275 mole), sodium ethoxide catalyst (0.133 gram, 0.225% wt. of the p-hydroxybenzoic acid used) and N,N'-dimethylacetamide solvent (404 grams) are added to a reactor equipped with a reflux condenser and stirred under a nitrogen atmosphere at 80° C. p-Nitrophenylisocyanate (73.85 gr...
10.6084/m9.figshare.5104873.v1
null
Carboxylic acid.Isocyanate
Secondary amide
c1ccccc1
c1ccccc1
c1ccccc1.c1ccccc1
Other
[O-]CC.[Na+].O
30
0.4
O=C(O)c1ccc(O)cc1.O=C=Nc1ccc([N+](=O)[O-])cc1>[O-]CC.[Na+].O>O=C(Nc1ccc([N+](=O)[O-])cc1)c1ccc(O)cc1
ord_dataset-02ee2261663048188cf6d85d2cc96e3f
ord-ae4392ce52324edfb94a96dc192d5fe2
O=C(Nc1ccc([N+](=O)[O-])cc1)c1ccc(O)cc1>>Nc1ccc(NC(=O)c2ccc(O)cc2)cc1
OC1=CC=C(C(=O)NC2=CC=C(C=C2)[N+](=O)[O-])C=C1>>OC1=CC=C(C(=O)NC2=CC=C(C=C2)N)C=C1
O=[N+:1]([O-])[c:2]1[cH:3][cH:4][c:5]([NH:6][C:7](=[O:8])[c:9]2[cH:10][cH:11][c:12]([OH:13])[cH:14][cH:15]2)[cH:16][cH:17]1>>[NH2:1][c:2]1[cH:3][cH:4][c:5]([NH:6][C:7](=[O:8])[c:9]2[cH:10][cH:11][c:12]([OH:13])[cH:14][cH:15]2)[cH:16][cH:17]1
O=C(Nc1ccc([N+](=O)[O-])cc1)c1ccc(O)cc1
Nc1ccc(NC(=O)c2ccc(O)cc2)cc1
null
null
C(C)O
Reduction
Reduction of nitro groups to amines
bbc242b150a51e69d3ad1caaa391f4422710431b398dcb880555f476706790be
7b0317532ea57a4fcedc1efc3e3c22eb5238d1c8330da53d4f9801fc2391f567
O=C(Nc1ccccc1)c1ccccc1
O=[N+;H0;D3:1](-[O-])-[c:2](:[c:3]):[c:4]>>[NH2;D1;+0:1]-[c:2](:[c:3]):[c:4]
null
[]
25
CELSIUS
23.3
HOUR
A portion (44.1 grams, 0.1708 mole) of 4-hydroxy-4'-nitrobenzanilide from A. above and ethanol (300 milliliters) are added to a 400 milliliter heavy walled glass bottle then sparged with nitrogen. After removal of air by nitrogen sparaing, Raney nickel catalyst (5.5 grams of a 75% wt. slurry in water at pH 10) is added...
10.6084/m9.figshare.5104873.v1
null
Nitro group
Primary amine
null
null
c1ccccc1.c1ccccc1
Other
C(C)O
25
23.3
O=C(Nc1ccc([N+](=O)[O-])cc1)c1ccc(O)cc1>C(C)O>Nc1ccc(NC(=O)c2ccc(O)cc2)cc1
ord_dataset-02ee2261663048188cf6d85d2cc96e3f
ord-f0a6c0c7bd4543d5854a784022e9f21e
CC(=O)OC(C)=O.O=C(O)Cc1ccc([N+](=O)[O-])cc1.O=Cc1ccc(O)cc1>>CC(=O)Oc1ccc(C=C(C(=O)O)c2ccc([N+](=O)[O-])cc2)cc1
OC1=CC=C(C=O)C=C1.C(C)(=O)OC(C)=O.[N+](=O)([O-])C1=CC=C(C=C1)CC(=O)O.[OH-].[Na+]>>[N+](=O)([O-])C1=CC=C(C=C1)C(C(=O)O)=CC1=CC=C(C=C1)OC(C)=O
CC(=O)O[C:2]([CH3:1])=[O:3].[CH2:10]([C:11](=[O:12])[OH:13])[c:14]1[cH:15][cH:16][c:17]([N+:18](=[O:19])[O-:20])[cH:21][cH:22]1.O=[CH:9][c:8]1[cH:7][cH:6][c:5]([OH:4])[cH:24][cH:23]1>>[CH3:1][C:2](=[O:3])[O:4][c:5]1[cH:6][cH:7][c:8]([CH:9]=[C:10]([C:11](=[O:12])[OH:13])[c:14]2[cH:15][cH:16][c:17]([N+:18](=[O:19])[O-:20...
CC(=O)OC(C)=O.O=C(O)Cc1ccc([N+](=O)[O-])cc1.O=Cc1ccc(O)cc1
CC(=O)Oc1ccc(C=C(C(=O)O)c2ccc([N+](=O)[O-])cc2)cc1
null
null
C(C)O.O
C-C Coupling
OtherReaction
24a5e5e840ab45f5ac71997b75bf9c9458ee729ce4846b47c2e20c66771f0961
6c4f18f39f8669eaadd9c3cc600e61ebad6b18d43c79a6714cb972028b541e8a
C(=Cc1ccccc1)c1ccccc1
C-C(=O)-O-[C;H0;D3;+0:1](-[C;D1;H3:2])=[O;D1;H0:3].O=[CH;D2;+0:4]-[c:5]1:[c:6]:[c:7]:[c:8](-[OH;D1;+0:9]):[c:10]:[c:11]:1.[O;D1;H0:12]=[C:13](-[O;D1;H1:14])-[CH2;D2;+0:15]-[c:16](:[c:17]):[c:18]>>[C;D1;H3:2]-[C;H0;D3;+0:1](=[O;D1;H0:3])-[O;H0;D2;+0:9]-[c:8]1:[c:7]:[c:6]:[c:5](-[CH;D2;+0:4]=[C;H0;D3;+0:15](-[C:13](=[O;D...
null
[]
60
CELSIUS
null
null
p-Nitrophenylacetic acid (94.02 grams, 0.519 mole) and 1.038 N sodium hydroxide solution (500 mL) are added to a 1,000 mL beaker and heated with stirring to 60° C. The resultant solution is rotary evaporated under vacuum until final conditions of 110° C. and 1 mm Hg are achieved and maintained for 30 minutes. A portion...
10.6084/m9.figshare.5104873.v1
null
Anhydride.Aldehyde.Aromatic alcohol
Ester
null
null
c1ccccc1.c1ccccc1
HO-
C(C)O.O
60
null
CC(=O)OC(C)=O.O=C(O)Cc1ccc([N+](=O)[O-])cc1.O=Cc1ccc(O)cc1>C(C)O.O>CC(=O)Oc1ccc(C=C(C(=O)O)c2ccc([N+](=O)[O-])cc2)cc1
ord_dataset-02ee2261663048188cf6d85d2cc96e3f
ord-bd2f92a102804b7a9cd611e6967e0025
CC(=O)Oc1ccc(C=C(C(=O)O)c2ccc([N+](=O)[O-])cc2)cc1>>O=[N+]([O-])c1ccc(C=Cc2ccc(O)cc2)cc1
[N+](=O)([O-])C1=CC=C(C=C1)C(C(=O)O)=CC1=CC=C(C=C1)OC(C)=O.C(C)O.Cl>>[N+](=O)([O-])C1=CC=C(C=C1)C=CC1=CC=C(C=C1)O
CC(=O)[O:14][c:13]1[cH:12][cH:11][c:10]([CH:9]=[C:8](C(=O)O)[c:7]2[cH:6][cH:5][c:4]([N+:2](=[O:1])[O-:3])[cH:18][cH:17]2)[cH:16][cH:15]1>>[O:1]=[N+:2]([O-:3])[c:4]1[cH:5][cH:6][c:7]([CH:8]=[CH:9][c:10]2[cH:11][cH:12][c:13]([OH:14])[cH:15][cH:16]2)[cH:17][cH:18]1
CC(=O)Oc1ccc(C=C(C(=O)O)c2ccc([N+](=O)[O-])cc2)cc1
O=[N+]([O-])c1ccc(C=Cc2ccc(O)cc2)cc1
null
null
O
Reduction
OtherReaction
63d7b9aaad312e5baffeb44abd9c90e266b4780604401c57bad121dfb88a1b0f
cdacdbe1471398702b32f2e73cf8a0e6eb084eb181796c9ace64f43ec88059ea
C(=Cc1ccccc1)c1ccccc1
C-C(=O)-[O;H0;D2;+0:1]-[c:2](:[c:3]):[c:4].O-C(=O)-[C;H0;D3;+0:5](=[C:6]-[c:7])-[c:8](:[c:9]):[c:10]>>[OH;D1;+0:1]-[c:2](:[c:3]):[c:4].[c:7]-[C:6]=[CH;D2;+0:5]-[c:8](:[c:9]):[c:10]
null
[]
95
CELSIUS
null
null
A portion (36.75 grams) of a-p-nitrophenyl-p-acetoxycinnamic acid from A. above, ethanol (300 mL) and concentrated hydrochloric acid (300 mL) are added to a reactor equipped with a reflux condenser and stirred under a nitrogen atmosphere. Heating commenced and a reflux is achieved at 93° C. Refluxing continued over the...
10.6084/m9.figshare.5104873.v1
null
Carboxylic acid.Ester
Aromatic alcohol
null
null
c1ccccc1.c1ccccc1
HO-
O
95
null
CC(=O)Oc1ccc(C=C(C(=O)O)c2ccc([N+](=O)[O-])cc2)cc1>O>O=[N+]([O-])c1ccc(C=Cc2ccc(O)cc2)cc1
ord_dataset-02ee2261663048188cf6d85d2cc96e3f
ord-0fc77ce97dd941919665786a507204ef
O=[N+]([O-])c1ccc(C=Cc2ccc(O)cc2)cc1>>Nc1ccc(C=Cc2ccc(O)cc2)cc1
[N+](=O)([O-])C1=CC=C(C=C1)C=CC1=CC=C(C=C1)O>>OC1=CC=C(C=C1)C=CC1=CC=C(C=C1)N
O=[N+:1]([O-])[c:2]1[cH:3][cH:4][c:5]([CH:6]=[CH:7][c:8]2[cH:9][cH:10][c:11]([OH:12])[cH:13][cH:14]2)[cH:15][cH:16]1>>[NH2:1][c:2]1[cH:3][cH:4][c:5]([CH:6]=[CH:7][c:8]2[cH:9][cH:10][c:11]([OH:12])[cH:13][cH:14]2)[cH:15][cH:16]1
O=[N+]([O-])c1ccc(C=Cc2ccc(O)cc2)cc1
Nc1ccc(C=Cc2ccc(O)cc2)cc1
null
null
C(C)O
Reduction
Reduction of nitro groups to amines
bbc242b150a51e69d3ad1caaa391f4422710431b398dcb880555f476706790be
7b0317532ea57a4fcedc1efc3e3c22eb5238d1c8330da53d4f9801fc2391f567
C(=Cc1ccccc1)c1ccccc1
O=[N+;H0;D3:1](-[O-])-[c:2](:[c:3]):[c:4]>>[NH2;D1;+0:1]-[c:2](:[c:3]):[c:4]
null
[]
25
CELSIUS
28.5
HOUR
A portion (20.9 grams, 0.0866 mole) of 4-nitro-4'-hydroxystilbene from B. above and ethanol (300 mL) are added to a 400 milliliter heavy walled glass bottle then sparged with nitrogen. After removal of air by nitrogen sparging, Raney nickel catalyst (2.5 grams of a 50% wt. slurry in water at pH 10) is washed one time w...
10.6084/m9.figshare.5104873.v1
null
Nitro group
Primary amine
null
null
c1ccccc1.c1ccccc1
Other
C(C)O
25
28.5
O=[N+]([O-])c1ccc(C=Cc2ccc(O)cc2)cc1>C(C)O>Nc1ccc(C=Cc2ccc(O)cc2)cc1
ord_dataset-02ee2261663048188cf6d85d2cc96e3f
ord-e7e3a364972640cab00e95d8a664a41d
CC1(C)CC(N=C=S)CC(C)(C)N1[O]>>CC1(C)CCCC(C)(C)N1[O]
C1=CC(=CC(=C1)NC(=O)CC2=CC=C(C=C2)NC3=NC=NC4=C3N=CN4[C@H]5[C@@H]([C@@H]([C@H](O5)CO)O)O)CC(=O)NCCN.O=C[C@H](O)[C@H](O)[C@H](O)CO.CC1(CC(CC(N1[O])(C)C)N=C=S)C.O.C1=CC(=CC(=C1)NC(=O)CC2=CC=C(C=C2)NC3=NC=NC4=C3N=CN4[C@H]5[C@@H]([C@@H]([C@H](O5)CO)O)O)CC(=O)NCCN>>CC1(CCCC(N1[O])(C)C)C.C1=CC(=CC(=C1)NC(=O)CC2=CC=C(C=C2)NC3=...
S=C=N[CH:5]1[CH2:4][C:2]([CH3:1])([CH3:3])[N:10]([O:11])[C:7]([CH3:8])([CH3:9])[CH2:6]1>>[CH3:1][C:2]1([CH3:3])[CH2:4][CH2:5][CH2:6][C:7]([CH3:8])([CH3:9])[N:10]1[O:11]
CC1(C)CC(N=C=S)CC(C)(C)N1[O]
CC1(C)CCCC(C)(C)N1[O]
null
null
CN(C)C=O
Functional Group Interconversion
OtherReaction
ce96f9dbda9551d9c3bc49f7388aca1ac64720ba7c3b1632614857a0d19192b5
4e930e84ca7a4b5a1b2ffdfd0ad5173746b70455a6634f66996611a6644c2fb6
C1CCNCC1
S=C=N-[CH;D3;+0:1]1-[C:2]-[C:3]-[#7:4]-[C:5]-[C:6]-1>>[#7:4]1-[C:3]-[C:2]-[CH2;D2;+0:1]-[C:6]-[C:5]-1
null
[]
null
null
null
null
ADAC, 2 (11.8 mg, 20 umol), was suspended in 0.5 ml DMF and treated with 4-isothiocyanato-TEMPO (2,2,6,6,-tetramethyl-1-piperidinyloxy, free radical (7 mg, Aldrich). After 1 hour 1.5 ml water was added to the solution, and the precipitate was collected, washed with a minimum of MeOH and ether, and recrystallized from D...
10.6084/m9.figshare.5104873.v1
null
Isothiocyanate
null
C1CC[NH]CC1
C1CC[NH]CC1
C1CC[NH]CC1
Other
CN(C)C=O
null
null
CC1(C)CC(N=C=S)CC(C)(C)N1[O]>CN(C)C=O>CC1(C)CCCC(C)(C)N1[O]
ord_dataset-02ee2261663048188cf6d85d2cc96e3f
ord-9dd9e53838e64349bfafd944e71e35ae
CCCCC(O[SiH](c1ccccc1)c1ccccc1)[C@@H]1O[C@H](n2ccc(N)nc2=O)CS1>>Nc1ccn([C@@H]2CS[C@H](CO)O2)c(=O)n1
C(CCC)C([C@@H]1O[C@@H](CS1)N1C(=O)N=C(N)C=C1)O[SiH](C1=CC=CC=C1)C1=CC=CC=C1.[F-].C(CCC)[N+](CCCC)(CCCC)CCCC>>OC[C@@H]1O[C@@H](CS1)N1C(=O)N=C(N)C=C1
CCCC[CH:10]([C@H:9]1[S:8][CH2:7][C@@H:6]([n:5]2[cH:4][cH:3][c:2]([NH2:1])[n:15][c:13]2=[O:14])[O:12]1)[O:11][SiH](c1ccccc1)c1ccccc1>>[NH2:1][c:2]1[cH:3][cH:4][n:5]([C@@H:6]2[CH2:7][S:8][C@H:9]([CH2:10][OH:11])[O:12]2)[c:13](=[O:14])[n:15]1
CCCCC(O[SiH](c1ccccc1)c1ccccc1)[C@@H]1O[C@H](n2ccc(N)nc2=O)CS1
Nc1ccn([C@@H]2CS[C@H](CO)O2)c(=O)n1
null
null
C1CCOC1
Deprotection
OtherReaction
9aaa703a406e2dc7eac47a2e7fa8489b941730a034828339b6d1cc86fe888dda
ff9889ffd40f59bd281424811967f384d29acb01a2d54e10590c5a677f81d17a
O=c1ncccn1[C@@H]1CSCO1
C-C-C-C-[CH;D3;+0:1](-[O;H0;D2;+0:2]-[SiH](-c1:c:c:c:c:c:1)-c1:c:c:c:c:c:1)-[C:3]1-[#16:4]-[C:5]-[C:6]-[#8:7]-1>>[OH;D1;+0:2]-[CH2;D2;+0:1]-[C:3]1-[#16:4]-[C:5]-[C:6]-[#8:7]-1
75
[{"value": 75.0, "product": "OC[C@@H]1O[C@@H](CS1)N1C(=O)N=C(N)C=C1", "details": "PERCENTYIELD", "is_desired": false}, {"value": 75.0, "product": "OC[C@@H]1O[C@@H](CS1)N1C(=O)N=C(N)C=C1", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
null
null
To a solution of the β anomer 17 (0.15 g, 0.32 mmol) in THF (25 mL) was added tetrabutylammonium fluoride 1M in THF (0.35 mL, 0.35 mmol, 1.1 eq) and the reaction was allowed to stir at room temperature until TLC indicated the disappearance of starting material (30 min). The reaction mixture was concentrated under reduc...
10.6084/m9.figshare.5104873.v1
null
null
Primary alcohol
c1ccccc1.c1ccccc1
null
c1cncnc1.C1CSCO1
Other
C1CCOC1
null
null
CCCCC(O[SiH](c1ccccc1)c1ccccc1)[C@@H]1O[C@H](n2ccc(N)nc2=O)CS1>C1CCOC1>Nc1ccn([C@@H]2CS[C@H](CO)O2)c(=O)n1
ord_dataset-02ee2261663048188cf6d85d2cc96e3f
ord-6cab89fbffc94bf8aa8d99d718c666ee
CC(C)(C)C(=O)Cl.Nc1cccc(C(F)(F)F)c1>>CC(C)(C)C(=O)Nc1cccc(C(F)(F)F)c1
O.C(C(C)(C)C)(=O)Cl.FC(C=1C=C(N)C=CC1)(F)F.C(C)N(CC)CC>>CC(C(=O)NC1=CC(=CC=C1)C(F)(F)F)(C)C
Cl[C:5]([C:2]([CH3:1])([CH3:3])[CH3:4])=[O:6].[NH2:7][c:8]1[cH:9][cH:10][cH:11][c:12]([C:13]([F:14])([F:15])[F:16])[cH:17]1>>[CH3:1][C:2]([CH3:3])([CH3:4])[C:5](=[O:6])[NH:7][c:8]1[cH:9][cH:10][cH:11][c:12]([C:13]([F:14])([F:15])[F:16])[cH:17]1
CC(C)(C)C(=O)Cl.Nc1cccc(C(F)(F)F)c1
CC(C)(C)C(=O)Nc1cccc(C(F)(F)F)c1
null
null
CCOCC
Acylation
Acylation of Nitrogen Nucleophiles by Acyl/Thioacyl/Carbamoyl Halides and Analogs_OS
38143a4d536201990008fd6f2c68e6571a341d1c367481869fbbbe36cb038937
0e6ae078978e324f714e184b4f72826d4e3bf2d9ab22d6e9f73740af687be16f
c1ccccc1
Cl-[C;H0;D3;+0:1](=[O;D1;H0:2])-[C:3](-[C;D1;H3:4])(-[C;D1;H3:5])-[C;D1;H3:6].[NH2;D1;+0:7]-[c:8](:[c:9]):[c:10]>>[C;D1;H3:4]-[C:3](-[C;D1;H3:5])(-[C;D1;H3:6])-[C;H0;D3;+0:1](=[O;D1;H0:2])-[NH;D2;+0:7]-[c:8](:[c:9]):[c:10]
98.3
[{"value": 98.0, "product": "CC(C(=O)NC1=CC(=CC=C1)C(F)(F)F)(C)C", "details": "PERCENTYIELD", "is_desired": false}, {"value": 98.3, "product": "CC(C(=O)NC1=CC(=CC=C1)C(F)(F)F)(C)C", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
14
HOUR
A solution of pivaloyl chloride (3.62 g; 30 mmol) in 40 ml dry ether was added dropwise at room temperature to a mixture of 3-trifluoromethyl-aniline (4.83 g, 30 mmol) and triethylamine (4.25 ml, 30.5 mmol). This was stirred at room temperature for a period of 14 hours and then poured into 200 ml water, extracted with ...
10.6084/m9.figshare.5104873.v1
null
Acyl halide.Primary amine
Secondary amide
null
null
c1ccccc1
HCl
CCOCC
null
14
CC(C)(C)C(=O)Cl.Nc1cccc(C(F)(F)F)c1>CCOCC>CC(C)(C)C(=O)Nc1cccc(C(F)(F)F)c1
ord_dataset-02ee2261663048188cf6d85d2cc96e3f
ord-cf8bc12a322f4aaaa1ba0ed4f8b9cd14
CC(C)(C)C(=O)Nc1cccc(C(F)(F)F)c1.CI>>Cc1c(NC(=O)C(C)(C)C)cccc1C(F)(F)F
CC(C(=O)NC1=CC(=CC=C1)C(F)(F)F)(C)C.[Li]CCCC.CI>>CC(C(=O)NC1=C(C(=CC=C1)C(F)(F)F)C)(C)C
[cH:2]1[c:3]([NH:4][C:5](=[O:6])[C:7]([CH3:8])([CH3:9])[CH3:10])[cH:11][cH:12][cH:13][c:14]1[C:15]([F:16])([F:17])[F:18].I[CH3:1]>>[CH3:1][c:2]1[c:3]([NH:4][C:5](=[O:6])[C:7]([CH3:8])([CH3:9])[CH3:10])[cH:11][cH:12][cH:13][c:14]1[C:15]([F:16])([F:17])[F:18]
CC(C)(C)C(=O)Nc1cccc(C(F)(F)F)c1.CI
Cc1c(NC(=O)C(C)(C)C)cccc1C(F)(F)F
null
null
O1CCCC1
C-C Coupling
Methylation with MeI_aryl
f457d3624ba90c4fd64ed28171ff7b2f7d20adbdddcd1b7e903999d38e58575c
410ec9b1cc243569e4ff568c248f0b402403802e002b4018f576af3f6960507b
c1ccccc1
I-[CH3;D1;+0:1].[F;D1;H0:2]-[C:3](-[F;D1;H0:4])(-[F;D1;H0:5])-[c:6](:[c:7]):[cH;D2;+0:8]:[c:9](-[#7:10]-[C:11]=[O;D1;H0:12]):[c:13]>>[CH3;D1;+0:1]-[c;H0;D3;+0:8](:[c:6](-[C:3](-[F;D1;H0:2])(-[F;D1;H0:4])-[F;D1;H0:5]):[c:7]):[c:9](-[#7:10]-[C:11]=[O;D1;H0:12]):[c:13]
80
[{"value": 80.0, "product": "CC(C(=O)NC1=C(C(=CC=C1)C(F)(F)F)C)(C)C", "details": "PERCENTYIELD", "is_desired": false}]
5
CELSIUS
null
null
A solution of 2,2-dimethyl-3'-trifluoromethyl-propionanilide (6.1 g, 25 mmol) in 100 ml dry tetrahydrofuran was cooled to 0° C. under nitrogen atmosphere and a solution of n-BuLi (1.6M in hexane, 50 ml, 75 mmol) was added dropwise in such a rate that the internal temperature did not rise above 10° C. (about 20 min.) an...
10.6084/m9.figshare.5104873.v1
null
null
null
c1ccccc1
c1ccccc1
c1ccccc1
HI
O1CCCC1
5
null
CC(C)(C)C(=O)Nc1cccc(C(F)(F)F)c1.CI>O1CCCC1>Cc1c(NC(=O)C(C)(C)C)cccc1C(F)(F)F