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-01dbb772c5e249108f0b191ed17a2c0c
ord-5c78bd6caf8a486a9043ac61fe6070d4
COC(=O)c1cc(N=Nc2ccc(O)c(CC(=O)O)c2)cc(C(=O)OC)c1>>O=C(O)Cc1cc(N=Nc2cc(C(=O)O)cc(C(=O)O)c2)ccc1O
Cl.COC(=O)C=1C=C(C=C(C1)C(=O)OC)N=NC=1C=CC(=C(C1)CC(=O)O)O.[OH-].[Na+].C(C)O>>C(=O)(O)C=1C=C(C=C(C1)C(=O)O)N=NC=1C=CC(=C(C1)CC(=O)O)O
C[O:15][C:13]([c:12]1[cH:11][c:10]([N:9]=[N:8][c:7]2[cH:6][c:5]([CH2:4][C:2](=[O:1])[OH:3])[c:24]([OH:25])[cH:23][cH:22]2)[cH:21][c:17]([C:18](=[O:19])[O:20]C)[cH:16]1)=[O:14]>>[O:1]=[C:2]([OH:3])[CH2:4][c:5]1[cH:6][c:7]([N:8]=[N:9][c:10]2[cH:11][c:12]([C:13](=[O:14])[OH:15])[cH:16][c:17]([C:18](=[O:19])[OH:20])[cH:21]...
COC(=O)c1cc(N=Nc2ccc(O)c(CC(=O)O)c2)cc(C(=O)OC)c1
O=C(O)Cc1cc(N=Nc2cc(C(=O)O)cc(C(=O)O)c2)ccc1O
null
null
O
Deprotection
OtherReaction
6e62db7aac546f574bcfb83067ba8906c30fcbfedfc37aa16b5eaad33833f45a
ed5fed81ba501ef41c88831ec6b9463b899bfdd0815c4145ae51c79addb226d0
c1ccc(N=Nc2ccccc2)cc1
C-[O;H0;D2;+0:1]-[C:2](=[O;D1;H0:3])-[c:4].C-[O;H0;D2;+0:5]-[C:6](=[O;D1;H0:7])-[c:8]>>[O;D1;H0:3]=[C:2](-[OH;D1;+0:1])-[c:4].[O;D1;H0:7]=[C:6](-[OH;D1;+0:5])-[c:8]
null
[]
null
null
null
null
12 g of 5-(3,5-bis-(methoxycarbonyl)-phenylazo)-2-hydroxyphenylacetic acid, 350 ml of water and 7 g of sodium hydroxide were boiled for 1 hour. 50 ml of ethanol was added, and the solution was diluted with water to 500 ml. The hot solution was acidified with hydrochloric acid to pH 2 and cooled. The crystals were filte...
10.6084/m9.figshare.5104873.v1
null
Ester.Ester
Carboxylic acid.Carboxylic acid
null
null
c1ccccc1.c1ccccc1
Other
O
null
null
COC(=O)c1cc(N=Nc2ccc(O)c(CC(=O)O)c2)cc(C(=O)OC)c1>O>O=C(O)Cc1cc(N=Nc2cc(C(=O)O)cc(C(=O)O)c2)ccc1O
ord_dataset-01dbb772c5e249108f0b191ed17a2c0c
ord-9c82aae6872744659c78caf24f2a0ad6
CCCCCCCCCCCCCCCCCC(=O)Cl.COC(=O)[C@@H](CCC(=O)O)NC(=O)[C@H](C)NC(=O)OC(C)(C)C.C[Si](C)(C)C(C(N)=O)[Si](C)(C)C>>CCCCCCCCCCCCCCCCCC(=O)N[C@@H](C)C(=O)N[C@H](CCC(=O)O)C(=O)OCc1ccccc1
O.N([C@@H](C)C(=O)N[C@H](CCC(O)=O)C(=O)OC)C(=O)OC(C)(C)C.C[Si](C)(C)C(C(=O)N)[Si](C)(C)C.C(CCCCCCCCCCCCCCCCC)(=O)Cl>>N([C@@H](C)C(=O)N[C@H](CCC(O)=O)C(=O)OCC1=CC=CC=C1)C(=O)CCCCCCCCCCCCCCCCC
Cl[C:18]([CH2:17][CH2:16][CH2:15][CH2:14][CH2:13][CH2:12][CH2:11][CH2:10][CH2:9][CH2:8][CH2:7][CH2:6][CH2:5][CH2:4][CH2:3][CH2:2][CH3:1])=[O:19].O=C(O[C:39]([CH3:36])([CH3:38])[CH3:40])[NH:20][C@@H:21]([CH3:22])[C:23](=[O:24])[NH:25][C@H:26]([CH2:27][CH2:28][C:29](=[O:30])[OH:31])[C:32](=[O:33])[O:34][CH3:35].C[Si](C)(...
CCCCCCCCCCCCCCCCCC(=O)Cl.COC(=O)[C@@H](CCC(=O)O)NC(=O)[C@H](C)NC(=O)OC(C)(C)C.C[Si](C)(C)C(C(N)=O)[Si](C)(C)C
CCCCCCCCCCCCCCCCCC(=O)N[C@@H](C)C(=O)N[C@H](CCC(=O)O)C(=O)OCc1ccccc1
null
null
C(Cl)Cl
Aromatic Heterocycle Formation
OtherReaction
79687e5242406d951d7886a91bed1f19dbc2bca5d0e30d5496a256a9346dedfe
fcaa19b137429f92b8346d5f48791a190e230bf573cce3aba467a16e8d190d3f
c1ccccc1
C-[Si](-C)(-[CH3;D1;+0:1])-C(-C(-N)=O)-[Si](-C)(-C)-[CH3;D1;+0:2].Cl-[C;H0;D3;+0:3](=[O;D1;H0:4])-[C:5]-[C:6].O=C(-O-[C;H0;D4;+0:7](-[CH3;D1;+0:8])(-[CH3;D1;+0:9])-[CH3;D1;+0:10])-[NH;D2;+0:11]-[C:12](-[C;D1;H3:13])-[C:14](=[O;D1;H0:15])-[#7:16]-[C:17]-[C:18](=[O;D1;H0:19])-[#8:20]-[CH3;D1;+0:21]>>[C:6]-[C:5]-[C;H0;D3;...
196.4
[{"value": 196.4, "product": "N([C@@H](C)C(=O)N[C@H](CCC(O)=O)C(=O)OCC1=CC=CC=C1)C(=O)CCCCCCCCCCCCCCCCC", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
null
null
L-Ala-D-Glu(OH)OBzl (1) (942 mg) was suspended in methylene chloride (40 ml), and bis(trimethylsilyl)acetamide (1.20 g) was added to the suspension under stirring. The resulting solution was treated with stearoyl chloride (900 mg) at ambient temperature and left for an hour. Evaporation of the solvent gave an oily resi...
10.6084/m9.figshare.5104873.v1
null
Acyl halide.Carbamic ester.Ester.Ether.Primary amide.Silyl protective group.Silyl protective group.Boc
Ester.Secondary amide
null
c1ccccc1
c1ccccc1
HCl
C(Cl)Cl
null
null
CCCCCCCCCCCCCCCCCC(=O)Cl.COC(=O)[C@@H](CCC(=O)O)NC(=O)[C@H](C)NC(=O)OC(C)(C)C.C[Si](C)(C)C(C(N)=O)[Si](C)(C)C>C(Cl)Cl>CCCCCCCCCCCCCCCCCC(=O)N[C@@H](C)C(=O)N[C@H](CCC(=O)O)C(=O)OCc1ccccc1
ord_dataset-01dbb772c5e249108f0b191ed17a2c0c
ord-cb80480d56a947c299041233295b2f80
CCN(CC)CC.CCOC(C)=O.COC(=O)[C@@H](CCC(=O)O)NC(=O)[C@H](C)NC(=O)OC(C)(C)C.N#CC(=NOC(=O)OCc1ccccc1)c1ccccc1>>CCCCCCCCCCCCCCCCCC(=O)N[C@@H](C)C(=O)N[C@H](CCC(=O)O)C(=O)OCc1ccccc1
C(C1=CC=CC=C1)OC(=O)ON=C(C#N)C1=CC=CC=C1.CC(=O)C.N([C@@H](C)C(=O)N[C@H](CCC(O)=O)C(=O)OC)C(=O)OC(C)(C)C.C(C)N(CC)CC.C(C)(=O)OCC.CC(=O)C>>N([C@@H](C)C(=O)N[C@H](CCC(O)=O)C(=O)OCC1=CC=CC=C1)C(=O)CCCCCCCCCCCCCCCCC
N([CH2:5][CH3:6])([CH2:8][CH3:7])[CH2:9][CH3:10].CC(=O)O[CH2:2][CH3:1].CO[C:32]([C@H:26]([NH:25][C:23]([C@@H:21]([NH:20][C:18](OC(C)([CH3:3])[CH3:4])=[O:19])[CH3:22])=[O:24])[CH2:27][CH2:28][C:29](=[O:30])[OH:31])=[O:33].N#C[C:17](=NOC(=O)[O:34][CH2:35][c:36]1[cH:37][cH:38][cH:39][cH:40][cH:41]1)[c:16]1[cH:11][cH:12][c...
CCN(CC)CC.CCOC(C)=O.COC(=O)[C@@H](CCC(=O)O)NC(=O)[C@H](C)NC(=O)OC(C)(C)C.N#CC(=NOC(=O)OCc1ccccc1)c1ccccc1
CCCCCCCCCCCCCCCCCC(=O)N[C@@H](C)C(=O)N[C@H](CCC(=O)O)C(=O)OCc1ccccc1
null
null
O
C-C Coupling
OtherReaction
4a9b44a97d0825ad133e04f968f43e586a6a2f1aedc9a93b20947f82d74efb97
b5d0b90a6f4148262c9e5836e06b3e8e6957025f553178e7c59f86821fe08133
c1ccccc1
C-C(=O)-O-[CH2;D2;+0:1]-[C;D1;H3:2].C-O-[C;H0;D3;+0:3](=[O;D1;H0:4])-[C:5](-[C:6])-[#7:7]-[C:8](=[O;D1;H0:9])-[C:10]-[#7:11]-[C;H0;D3;+0:12](=[O;D1;H0:13])-O-C(-C)(-[CH3;D1;+0:14])-[CH3;D1;+0:15].N#C-[C;H0;D3;+0:16](=N-O-C(=O)-[O;H0;D2;+0:17]-[C:18]-[c:19])-[c;H0;D3;+0:20]1:[cH;D2;+0:21]:[cH;D2;+0:22]:[cH;D2;+0:23]:[cH...
94.7
[{"value": 94.7, "product": "N([C@@H](C)C(=O)N[C@H](CCC(O)=O)C(=O)OCC1=CC=CC=C1)C(=O)CCCCCCCCCCCCCCCCC", "details": "PERCENTYIELD", "is_desired": false}]
null
null
null
null
To a solution of D-Lac-L-Ala-γ-D-Glu(α-OH)-(L)-mesoDAP-(L)-GlyOH (1) (1.2 g) in water (5 ml) was added triethylamine (0.96 g) and a solution of benzyloxycarbonyloxyimino-2-phenylacetonitrile (0.69 g) in acetone (5 ml) at 0° C. with stirring and the mixture was stirring over night at room temperature. After evapolation ...
10.6084/m9.figshare.5104873.v1
null
Carbamic ester.Ester.Ester.Ether.Ether.Nitrile.Tertiary amine.Boc
Ester.Secondary amide
c1ccccc1
null
c1ccccc1
HO-
O
null
null
CCN(CC)CC.CCOC(C)=O.COC(=O)[C@@H](CCC(=O)O)NC(=O)[C@H](C)NC(=O)OC(C)(C)C.N#CC(=NOC(=O)OCc1ccccc1)c1ccccc1>O>CCCCCCCCCCCCCCCCCC(=O)N[C@@H](C)C(=O)N[C@H](CCC(=O)O)C(=O)OCc1ccccc1
ord_dataset-01dbb772c5e249108f0b191ed17a2c0c
ord-34b5a02bca8a409287c4f086e8e5d348
CCCCCCCCCCCCCCCC(=O)N[C@@H](C)C(=O)N[C@H](CCC(=O)O)C(=O)OCc1ccccc1.O=C1CCC(=O)N1O>>CCCCCCCCCCCCCCCC(=O)N[C@@H](C)C(=O)N[C@H](CCC(=O)ON1C(=O)CCC1=O)C(=O)OCc1ccccc1
N([C@@H](C)C(=O)N[C@H](CCC(O)=O)C(=O)OCC1=CC=CC=C1)C(=O)CCCCCCCCCCCCCCC.ON1C(CCC1=O)=O.C1(CCCCC1)N=C=NC1CCCCC1>>N([C@@H](C)C(=O)N[C@H](CCC(ON1C(=O)CCC1=O)=O)C(=O)OCC1=CC=CC=C1)C(=O)CCCCCCCCCCCCCCC
O[C:27]([CH2:26][CH2:25][C@@H:24]([NH:23][C:21]([C@@H:19]([NH:18][C:16]([CH2:15][CH2:14][CH2:13][CH2:12][CH2:11][CH2:10][CH2:9][CH2:8][CH2:7][CH2:6][CH2:5][CH2:4][CH2:3][CH2:2][CH3:1])=[O:17])[CH3:20])=[O:22])[C:37](=[O:38])[O:39][CH2:40][c:41]1[cH:42][cH:43][cH:44][cH:45][cH:46]1)=[O:28].[OH:29][N:30]1[C:31](=[O:32])[...
CCCCCCCCCCCCCCCC(=O)N[C@@H](C)C(=O)N[C@H](CCC(=O)O)C(=O)OCc1ccccc1.O=C1CCC(=O)N1O
CCCCCCCCCCCCCCCC(=O)N[C@@H](C)C(=O)N[C@H](CCC(=O)ON1C(=O)CCC1=O)C(=O)OCc1ccccc1
null
null
C(Cl)(Cl)Cl.O1CCCC1
Protection
OtherReaction
a1b3ee4184fc00a0730e4c14eca3a5fbe87fccb44744074c13ef1bfbfabde8ad
e66168e1cfeb6611d93ee4c49193aae81e56c700a9fe46743dc42eed291ed0f9
O=C(CCCC(=O)ON1C(=O)CCC1=O)OCc1ccccc1
O-[C;H0;D3;+0:1](=[O;D1;H0:2])-[C:3]-[C:4].[O;D1;H0:5]=[C:6]1-[C:7]-[C:8]-[C:9](=[O;D1;H0:10])-[#7:11]-1-[OH;D1;+0:12]>>[C:4]-[C:3]-[C;H0;D3;+0:1](=[O;D1;H0:2])-[O;H0;D2;+0:12]-[#7:11]1-[C:6](=[O;D1;H0:5])-[C:7]-[C:8]-[C:9]-1=[O;D1;H0:10]
7,846.1
[{"value": 7846.1, "product": "N([C@@H](C)C(=O)N[C@H](CCC(ON1C(=O)CCC1=O)=O)C(=O)OCC1=CC=CC=C1)C(=O)CCCCCCCCCCCCCCC", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
18
HOUR
To a solution of palmitoyl-L-Ala-D-Glu(OH)OBzl (1)(1.84 g) in a mixture of tetrahydrofuran (20 ml) and chloroform (30 ml) were added N-hydroxysuccinimide (425 mg) and dicyclohexylcarbodiimide (728 mg). The reaction mixture was kept for 18 hours at room temperature and the precipitate was filtered off and washed with ch...
10.6084/m9.figshare.5104873.v1
null
Carboxylic acid
null
null
null
C1CC[NH]C1.c1ccccc1
HO-
C(Cl)(Cl)Cl.O1CCCC1
null
18
CCCCCCCCCCCCCCCC(=O)N[C@@H](C)C(=O)N[C@H](CCC(=O)O)C(=O)OCc1ccccc1.O=C1CCC(=O)N1O>C(Cl)(Cl)Cl.O1CCCC1>CCCCCCCCCCCCCCCC(=O)N[C@@H](C)C(=O)N[C@H](CCC(=O)ON1C(=O)CCC1=O)C(=O)OCc1ccccc1
ord_dataset-01dbb772c5e249108f0b191ed17a2c0c
ord-d88a184952ed4e1682e3d74fe14b493c
CCCCCCCCCCCCCCCC(=O)N[C@@H](C)C(=O)N[C@H](CCC(=O)O)C(=O)OCc1ccccc1.O=C(O)C(F)(F)F>>CCCCCCCCCCCCCCCC(=O)N[C@@H](C)C(=O)N[C@H](CCC(=O)ON1C(=O)CCC1=O)C(=O)OCc1ccccc1
FC(C(=O)O)(F)F.N([C@@H](C)C(=O)N[C@H](CCC(O)=O)C(=O)OCC1=CC=CC=C1)C(=O)CCCCCCCCCCCCCCC>>N([C@@H](C)C(=O)N[C@H](CCC(ON1C(=O)CCC1=O)=O)C(=O)OCC1=CC=CC=C1)C(=O)CCCCCCCCCCCCCCC
[CH3:1][CH2:2][CH2:3][CH2:4][CH2:5][CH2:6][CH2:7][CH2:8][CH2:9][CH2:10][CH2:11][CH2:12][CH2:13][CH2:14][CH2:15][C:16](=[O:17])[NH:18][C@@H:19]([CH3:20])[C:21](=[O:22])[NH:23][C@H:24]([CH2:25][CH2:26][C:27](=[O:28])[OH:29])[C:37](=[O:38])[O:39][CH2:40][c:41]1[cH:42][cH:43][cH:44][cH:45][cH:46]1.F[C:33](F)(F)[C:31](=[O:3...
CCCCCCCCCCCCCCCC(=O)N[C@@H](C)C(=O)N[C@H](CCC(=O)O)C(=O)OCc1ccccc1.O=C(O)C(F)(F)F
CCCCCCCCCCCCCCCC(=O)N[C@@H](C)C(=O)N[C@H](CCC(=O)ON1C(=O)CCC1=O)C(=O)OCc1ccccc1
null
null
null
C-C Coupling
OtherReaction
9d3882c6f12a0d957247cb9225c824b01f6b123c7e5aaf01a4ad60230ac408bf
36f812227431b4b24986bca594ef04a41a9f0a5ee5ecfdc1ed90862121d89990
O=C(CCCC(=O)ON1C(=O)CCC1=O)OCc1ccccc1
F-[C;H0;D4;+0:1](-F)(-F)-[C;H0;D3;+0:2](=[O;D1;H0:3])-[OH;D1;+0:4].[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]-[#7:9]1-[C:10](=[O;H0;D1;+0:4])-[C:11]-[CH2;D2;+0:1]-[C;H0;D3;+0:2]-1=[O;D1;H0:3]
null
[]
null
null
20
MINUTE
Trifluoroacetic acid (15 ml) was added to Boc-L-Ala-D-Glu-(OH)OBzl (1)(3.26 g) and the mixture was stirred for 20 minutes at room temperature, concentrated in vacuo and washed with diisopropylether. The oil was dissolved in a mixture of water (15 ml) and sodium bicarbonate was added until the pH of the solution became ...
10.6084/m9.figshare.5104873.v1
null
Trifluoro group.Carboxylic acid.Carboxylic acid
Tertiary amide.Tertiary amide
null
C1CC[NH]C1
C1CC[NH]C1.c1ccccc1
null
null
null
0.333333
CCCCCCCCCCCCCCCC(=O)N[C@@H](C)C(=O)N[C@H](CCC(=O)O)C(=O)OCc1ccccc1.O=C(O)C(F)(F)F>>CCCCCCCCCCCCCCCC(=O)N[C@@H](C)C(=O)N[C@H](CCC(=O)ON1C(=O)CCC1=O)C(=O)OCc1ccccc1
ord_dataset-01dbb772c5e249108f0b191ed17a2c0c
ord-eb26a125028f488199001eac7c1803da
CC(C)(C)O.CC(Cl)OC(=O)Cl>>CC(Cl)OC(=O)OC(C)(C)C
C(C)(C)(C)O.ClC(=O)OC(C)Cl.N1=CC=CC=C1>>C(OC(C)Cl)(OC(C)(C)C)=O
[OH:7][C:8]([CH3:9])([CH3:10])[CH3:11].Cl[C:5]([O:4][CH:2]([CH3:1])[Cl:3])=[O:6]>>[CH3:1][CH:2]([Cl:3])[O:4][C:5](=[O:6])[O:7][C:8]([CH3:9])([CH3:10])[CH3:11]
CC(C)(C)O.CC(Cl)OC(=O)Cl
CC(Cl)OC(=O)OC(C)(C)C
null
null
ClCCl
Acylation
Schotten-Baumann to ester
eac78f0277d3f2b491018dfae1981b579de8768cdcc1514a8c4792e129567220
85f668b80fab38c365fc662c1a9c233064a6757d7f126fae63f41481cb03e343
null
Cl-[C;H0;D3;+0:1](=[O;D1;H0:2])-[#8:3]-[C:4].[C;D1;H3:5]-[C:6](-[C;D1;H3:7])(-[C;D1;H3:8])-[OH;D1;+0:9]>>[C:4]-[#8:3]-[C;H0;D3;+0:1](=[O;D1;H0:2])-[O;H0;D2;+0:9]-[C:6](-[C;D1;H3:5])(-[C;D1;H3:7])-[C;D1;H3:8]
null
[]
null
null
null
null
In a reactor cooled to +5° C., there are introduced 600 ml of dicloromethane, 43.7 g (0.59 mole) of tert-butanol and 94.7 g (0.66 mole) of α-chloroethyl chloroformate. 57 g (0.72 mole) of pyridine are then added dropwise and with stirring while the temperature is maintained at between 10° and 20° C. The mixture is stir...
10.6084/m9.figshare.5104873.v1
null
Acyl halide.Ether.Tertiary alcohol
Carbonic Ester
null
null
null
HCl
ClCCl
null
null
CC(C)(C)O.CC(Cl)OC(=O)Cl>ClCCl>CC(Cl)OC(=O)OC(C)(C)C
ord_dataset-01dbb772c5e249108f0b191ed17a2c0c
ord-c4542c72534e465fbfebfb91c898577a
C1CCNCC1.CC(Cl)OC(=O)OC(C)(C)C>>CC(C)(C)OC(=O)N1CCCCC1
N1CCCCC1.C(=O)([O-])[O-].[K+].[K+].C(OC(C)Cl)(OC(C)(C)C)=O>>C(C)(C)(C)OC(=O)N1CCCCC1
[NH:8]1[CH2:9][CH2:10][CH2:11][CH2:12][CH2:13]1.CC(Cl)O[C:6]([O:5][C:2]([CH3:1])([CH3:3])[CH3:4])=[O:7]>>[CH3:1][C:2]([CH3:3])([CH3:4])[O:5][C:6](=[O:7])[N:8]1[CH2:9][CH2:10][CH2:11][CH2:12][CH2:13]1
C1CCNCC1.CC(Cl)OC(=O)OC(C)(C)C
CC(C)(C)OC(=O)N1CCCCC1
null
null
C1CCOC1
Protection
Boc amine protection of secondary amine
75e102b122a4a7a02da3ae4e2dcc8358b69efe231b6c70fd0fe46094e3f46d25
bdffcbfd2f9dfa9a6777281c9c0c2e6d7c7d67c4aae26b320b5d0a73afda621c
C1CCNCC1
C-C(-Cl)-O-[C;H0;D3;+0:1](=[O;D1;H0:2])-[#8:3]-[C:4](-[C;D1;H3:5])(-[C;D1;H3:6])-[C;D1;H3:7].[C:8]-[C:9]-[NH;D2;+0:10]-[C:11]-[C:12]>>[C:8]-[C:9]-[N;H0;D3;+0:10](-[C;H0;D3;+0:1](=[O;D1;H0:2])-[#8:3]-[C:4](-[C;D1;H3:5])(-[C;D1;H3:6])-[C;D1;H3:7])-[C:11]-[C:12]
null
[]
null
null
null
null
The procedure is as in Example 7, but with 8.5 g (0.1 mole) of piperidine, 60 ml of THF, 20 ml of saturated aqueous K2CO3 solution and 0.11 mole of α-chloroethyl tert-butyl carbonate. Conditions: See reaction.notes.procedure_details.
10.6084/m9.figshare.5104873.v1
null
Secondary halide.Carbonic Ester.Secondary amine.Boc
Carbamic ester
C1CCNCC1
C1CC[NH]CC1
C1CC[NH]CC1
HCl
C1CCOC1
null
null
C1CCNCC1.CC(Cl)OC(=O)OC(C)(C)C>C1CCOC1>CC(C)(C)OC(=O)N1CCCCC1
ord_dataset-01dbb772c5e249108f0b191ed17a2c0c
ord-18ed9719ba5540d59af2fe55eab3dddb
CC(C)(C)OC(=O)OC(Cl)C(Cl)(Cl)Cl.c1c[nH]cn1>>CC(C)(C)OC(=O)c1ncc[nH]1
C(OC(C)(C)C)(OC(C(Cl)(Cl)Cl)Cl)=O.N1C=NC=C1.C([O-])([O-])=O.[K+].[K+]>>C(C)(C)(C)OC(=O)C=1NC=CN1
ClC(O[C:6]([O:5][C:2]([CH3:1])([CH3:3])[CH3:4])=[O:7])C(Cl)(Cl)Cl.[cH:8]1[n:9][cH:10][cH:11][nH:12]1>>[CH3:1][C:2]([CH3:3])([CH3:4])[O:5][C:6](=[O:7])[c:8]1[n:9][cH:10][cH:11][nH:12]1
CC(C)(C)OC(=O)OC(Cl)C(Cl)(Cl)Cl.c1c[nH]cn1
CC(C)(C)OC(=O)c1ncc[nH]1
null
null
C1CCOC1
C-C Coupling
Friedel-Crafts acylation
816926b19e95b508018b448b7a2db217b2d160cb2dbf98aa6d7bdd10b1c1e54d
f06009d448893fe81afd5b89761f51e5f5ed2dc0f5de3026d91db5775be0da30
c1c[nH]cn1
Cl-C(-O-[C;H0;D3;+0:1](=[O;D1;H0:2])-[#8:3]-[C:4](-[C;D1;H3:5])(-[C;D1;H3:6])-[C;D1;H3:7])-C(-Cl)(-Cl)-Cl.[#7;a:8]1:[c:9]:[c:10]:[#7;a:11]:[cH;D2;+0:12]:1>>[C;D1;H3:5]-[C:4](-[C;D1;H3:6])(-[C;D1;H3:7])-[#8:3]-[C;H0;D3;+0:1](=[O;D1;H0:2])-[c;H0;D3;+0:12]1:[#7;a:8]:[c:9]:[c:10]:[#7;a:11]:1
null
[]
20
CELSIUS
1
HOUR
5 g (17.5 mmol) of tert-butyl 1,2,2,2-tetrachloroethyl carbonate dissolved in 10 ml of THF are added at 0° C. to a solution of imidazole (1.2 g; 17.6 mmol) in THF (20 ml) in the presence of 5M aqueous potassium carbonate solution (5 ml). The mixture is stirred for 1 hour at 20° C., and the organic phase is decanted and...
10.6084/m9.figshare.5104873.v1
null
Trichloro group.Secondary halide.Carbonic Ester.Boc
Ester
c1c[nH]cn1
c1c[nH]cn1
c1c[nH]cn1
HCl
C1CCOC1
20
1
CC(C)(C)OC(=O)OC(Cl)C(Cl)(Cl)Cl.c1c[nH]cn1>C1CCOC1>CC(C)(C)OC(=O)c1ncc[nH]1
ord_dataset-01dbb772c5e249108f0b191ed17a2c0c
ord-3c480d95de8546edb218b0eba0488c82
CC(Cl)OC(=O)Cl.CC1(C)Cc2cccc(O)c2O1>>CC(Cl)OC(=O)Oc1cccc2c1OC(C)(C)C2
ClC(C)OC(=O)Cl.CC1(OC2=C(C1)C=CC=C2O)C.N1=CC=CC=C1>>C(OC(C)Cl)(OC1=CC=CC=2CC(OC21)(C)C)=O
Cl[C:5]([O:4][CH:2]([CH3:1])[Cl:3])=[O:6].[OH:7][c:8]1[cH:9][cH:10][cH:11][c:12]2[c:13]1[O:14][C:15]([CH3:16])([CH3:17])[CH2:18]2>>[CH3:1][CH:2]([Cl:3])[O:4][C:5](=[O:6])[O:7][c:8]1[cH:9][cH:10][cH:11][c:12]2[c:13]1[O:14][C:15]([CH3:16])([CH3:17])[CH2:18]2
CC(Cl)OC(=O)Cl.CC1(C)Cc2cccc(O)c2O1
CC(Cl)OC(=O)Oc1cccc2c1OC(C)(C)C2
null
null
ClCCl
Acylation
Schotten-Baumann to ester
18e63da6830cc445f43af5e9dc21618a6276c35c0e735b25c948aaaf35c35656
9d4bf8407389b23766af8e91d21ef1aae6a051b3a051fef2f77a7ae83951845d
c1ccc2c(c1)CCO2
Cl-[C;H0;D3;+0:1](=[O;D1;H0:2])-[#8:3]-[C:4].[#8:5]-[c:6]:[c:7](-[OH;D1;+0:8]):[c:9]>>[#8:5]-[c:6]:[c:7](-[O;H0;D2;+0:8]-[C;H0;D3;+0:1](=[O;D1;H0:2])-[#8:3]-[C:4]):[c:9]
84
[{"value": 84.0, "product": "C(OC(C)Cl)(OC1=CC=CC=2CC(OC21)(C)C)=O", "details": "PERCENTYIELD", "is_desired": false}]
20
CELSIUS
3
HOUR
21.5 g (0.15 mole) of 1-chloroethylchloroformate are added in a single portion to a solution of 2,3-dihydro-2,2-dimethyl-7-benzofuranol (24.6 g; 0.15 mole) in dichloromethane (150 ml). The mixture is cooled to between 0° and 5° C., and 12 g (0.15 mole) of pyridine are added dropwise. The mixture is stirred for 3 hours ...
10.6084/m9.figshare.5104873.v1
null
Acyl halide.Ether.Aromatic alcohol
Ether.Ether
null
null
c1ccc2c(c1)CCO2
HCl
ClCCl
20
3
CC(Cl)OC(=O)Cl.CC1(C)Cc2cccc(O)c2O1>ClCCl>CC(Cl)OC(=O)Oc1cccc2c1OC(C)(C)C2
ord_dataset-01dbb772c5e249108f0b191ed17a2c0c
ord-d4106ac42a79474482487a508c64ea90
CC(Cl)OC(=O)Oc1cccc2c1OC(C)(C)C2.CN(C)c1ccccc1>>CNC(=O)Oc1cccc2c1OC(C)(C)C2
C(OC(C)Cl)(OC1=CC=CC=2CC(OC21)(C)C)=O.CN(C1=CC=CC=C1)C>>CNC(OC1=CC=CC=2CC(OC21)(C)C)=O
CC(Cl)O[C:3](=[O:4])[O:5][c:6]1[cH:7][cH:8][cH:9][c:10]2[c:11]1[O:12][C:13]([CH3:14])([CH3:15])[CH2:16]2.C[N:2](c1ccccc1)[CH3:1]>>[CH3:1][NH:2][C:3](=[O:4])[O:5][c:6]1[cH:7][cH:8][cH:9][c:10]2[c:11]1[O:12][C:13]([CH3:14])([CH3:15])[CH2:16]2
CC(Cl)OC(=O)Oc1cccc2c1OC(C)(C)C2.CN(C)c1ccccc1
CNC(=O)Oc1cccc2c1OC(C)(C)C2
null
null
N1=CC=CC=C1
Protection
OtherReaction
56c67ed9f08d552b4f5ab0709744a6a0554bc94205da239257b331d0aa710c25
1febf5cbaa5b41f12a569b80f68c4e08babe232eeb75eb42efb69ed3b6bc21f1
c1ccc2c(c1)CCO2
C-C(-Cl)-O-[C;H0;D3;+0:1](=[O;D1;H0:2])-[#8:3]-[c:4].C-[N;H0;D3;+0:5](-[C;D1;H3:6])-c1:c:c:c:c:c:1>>[C;D1;H3:6]-[NH;D2;+0:5]-[C;H0;D3;+0:1](=[O;D1;H0:2])-[#8:3]-[c:4]
null
[]
null
null
null
null
The procedure is as in (a) followed by (b), but pyridine is replaced by N,N-dimethylaniline and the intermediate carbonate is not distilled. Starting with 16.4 g of 2,3-dihydro-2,2-dimethyl-7-benzofuranol, 16.8 g (76%) of CARBOFURAN are then obtained, M.p. 147° C. Conditions: See reaction.notes.procedure_details. Worku...
10.6084/m9.figshare.5104873.v1
null
Secondary halide.Ether.Ether.Tertiary amine
Carbamic ester
c1ccccc1
null
c1ccc2c(c1)CCO2
HCl
N1=CC=CC=C1
null
null
CC(Cl)OC(=O)Oc1cccc2c1OC(C)(C)C2.CN(C)c1ccccc1>N1=CC=CC=C1>CNC(=O)Oc1cccc2c1OC(C)(C)C2
ord_dataset-01dbb772c5e249108f0b191ed17a2c0c
ord-15c439ed99fb49c6bfd27dedef4a3286
CN.O=C(Cl)OC(Cl)C(Cl)(Cl)Cl>>CNC(=O)OC(Cl)C(Cl)(Cl)Cl
CN.ClC(=O)OC(C(Cl)(Cl)Cl)Cl>>CNC(OC(C(Cl)(Cl)Cl)Cl)=O
[CH3:1][NH2:2].Cl[C:3](=[O:4])[O:5][CH:6]([Cl:7])[C:8]([Cl:9])([Cl:10])[Cl:11]>>[CH3:1][NH:2][C:3](=[O:4])[O:5][CH:6]([Cl:7])[C:8]([Cl:9])([Cl:10])[Cl:11]
CN.O=C(Cl)OC(Cl)C(Cl)(Cl)Cl
CNC(=O)OC(Cl)C(Cl)(Cl)Cl
null
null
ClCCl
Protection
Acylation of Nitrogen Nucleophiles by Acyl/Thioacyl/Carbamoyl Halides and Analogs_OS
038720aa61a7efa0f2a9ee6f2e0adf63a9ffdc2be4697c11a6215baef34f97b2
205f353513ce9506ab61831799da8fb73ec2ef5cfa927664496d3ce72c438860
null
Cl-[C;H0;D3;+0:1](=[O;D1;H0:2])-[#8:3]-[C:4].[C;D1;H3:5]-[NH2;D1;+0:6]>>[C:4]-[#8:3]-[C;H0;D3;+0:1](=[O;D1;H0:2])-[NH;D2;+0:6]-[C;D1;H3:5]
null
[]
null
null
2
HOUR
34.7 ml (0.4 mmol) of methylamine (in 40% strength aqueous solution) are added dropwise to a solution maintained at 0° C. of 49.4 g (0.2 mole) of 1,2,2,2-tetrachloroethyl chloroformate in dichloromethane (150 ml). The mixture is then stirred for 2 hours at room temperature. The organic phase is washed with 2×100 ml of ...
10.6084/m9.figshare.5104873.v1
null
Acyl halide.Ether.Primary amine
Carbamic ester
null
null
null
HCl
ClCCl
null
2
CN.O=C(Cl)OC(Cl)C(Cl)(Cl)Cl>ClCCl>CNC(=O)OC(Cl)C(Cl)(Cl)Cl
ord_dataset-01dbb772c5e249108f0b191ed17a2c0c
ord-a75633828b0a48b69e9a6ab1c8a89eba
O=C(Cl)OCCCl.c1c[nH]cn1>>CC(Cl)OC(=O)c1ncc[nH]1
ClC(=O)OCCCl.N1C=NC=C1.ClCCl.O>>ClC(C)OC(=O)C=1NC=CN1
Cl[C:5]([O:4][CH2:2][CH2:1][Cl:3])=[O:6].[cH:7]1[n:8][cH:9][cH:10][nH:11]1>>[CH3:1][CH:2]([Cl:3])[O:4][C:5](=[O:6])[c:7]1[n:8][cH:9][cH:10][nH:11]1
O=C(Cl)OCCCl.c1c[nH]cn1
CC(Cl)OC(=O)c1ncc[nH]1
null
null
null
Functional Group Interconversion
OtherReaction
7a66bfe59b3e87f9ced1393a7eb8c64227e0adcdc77dc061f59255ab9be37ce7
2079e2b380c74a553dd6ae396541b903f289ebf8d747377df9f4c7bff95f3907
c1c[nH]cn1
Cl-[C;H0;D3;+0:1](=[O;D1;H0:2])-[#8:3]-[CH2;D2;+0:4]-[CH2;D2;+0:5]-[Cl;H0;D1;+0:6].[#7;a:7]1:[c:8]:[c:9]:[#7;a:10]:[cH;D2;+0:11]:1>>[CH3;D1;+0:5]-[CH;D3;+0:4](-[Cl;H0;D1;+0:6])-[#8:3]-[C;H0;D3;+0:1](=[O;D1;H0:2])-[c;H0;D3;+0:11]1:[#7;a:7]:[c:8]:[c:9]:[#7;a:10]:1
null
[]
null
null
4
HOUR
28.6 g (0.2 mole) of chloroethyl chloroformate are added dropwise to a solution of 27.2 g (0.4 mole) of imidazole in 200 ml of dichloromethane cooled in a water bath. The mixture is stirred at room temperature for 4 hours, and 50 ml of iced water are then added. The organic phase is washed with 2×50 ml of water and the...
10.6084/m9.figshare.5104873.v1
null
Acyl halide.Primary halide.Ether
Secondary halide.Ester
c1c[nH]cn1
c1c[nH]cn1
c1c[nH]cn1
HCl
null
null
4
O=C(Cl)OCCCl.c1c[nH]cn1>>CC(Cl)OC(=O)c1ncc[nH]1
ord_dataset-01dbb772c5e249108f0b191ed17a2c0c
ord-0c0661338a584907b09ee85e49489e40
CC(C)(C)OC(=O)OC(Cl)C(Cl)(Cl)Cl.N[C@@H](CC(=O)O)C(=O)O>>CC(C)(C)OC(=O)N[C@@H](CC(=O)O)C(=O)O
N[C@@H](CC(=O)O)C(=O)O.O1CCOCC1.O.C(C)N(CC)CC.C(OC(C)(C)C)(OC(C(Cl)(Cl)Cl)Cl)=O>>C(C)(C)(C)OC(=O)N[C@@H](CC(=O)O)C(=O)O
ClC(O[C:6]([O:5][C:2]([CH3:1])([CH3:3])[CH3:4])=[O:7])C(Cl)(Cl)Cl.[NH2:8][C@@H:9]([CH2:10][C:11](=[O:12])[OH:13])[C:14](=[O:15])[OH:16]>>[CH3:1][C:2]([CH3:3])([CH3:4])[O:5][C:6](=[O:7])[NH:8][C@@H:9]([CH2:10][C:11](=[O:12])[OH:13])[C:14](=[O:15])[OH:16]
CC(C)(C)OC(=O)OC(Cl)C(Cl)(Cl)Cl.N[C@@H](CC(=O)O)C(=O)O
CC(C)(C)OC(=O)N[C@@H](CC(=O)O)C(=O)O
null
null
O
Protection
Boc amine protection of primary amine
37e16d190b68c39ece6a89d1e9e4bc58f5dd27899c2544e0166ffa6b73bc7e8b
9b9f365a0cb67affe811fedbc86b1fc402c859f95b93eed7848b69aa4ee65fbd
null
Cl-C(-O-[C;H0;D3;+0:1](=[O;D1;H0:2])-[#8:3]-[C:4](-[C;D1;H3:5])(-[C;D1;H3:6])-[C;D1;H3:7])-C(-Cl)(-Cl)-Cl.[NH2;D1;+0:8]-[C:9](-[C:10]-[C:11](=[O;D1;H0:12])-[O;D1;H1:13])-[C:14](=[O;D1;H0:15])-[O;D1;H1:16]>>[C;D1;H3:5]-[C:4](-[C;D1;H3:6])(-[C;D1;H3:7])-[#8:3]-[C;H0;D3;+0:1](=[O;D1;H0:2])-[NH;D2;+0:8]-[C:9](-[C:10]-[C:11...
60
[{"value": 60.0, "product": "C(C)(C)(C)OC(=O)N[C@@H](CC(=O)O)C(=O)O", "details": "PERCENTYIELD", "is_desired": false}, {"value": 60.0, "product": "C(C)(C)(C)OC(=O)N[C@@H](CC(=O)O)C(=O)O", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
null
null
To a solution of 1.33 g (10 mmol) of L-aspartic acid in a dioxane/water (1:1) mixture (30 ml), 4.2 ml (30 mmol) of triethylamine are added, and the mixture is stirred until solution is complete (approximately 10 min). 2.85 g (10 mmol) of tert-butyl 1,2,2,2-tetrachloroethyl carbonate are then added and the mixture is st...
10.6084/m9.figshare.5104873.v1
null
Trichloro group.Secondary halide.Carbonic Ester.Primary amine
Carbamic ester
null
null
null
HCl
O
null
null
CC(C)(C)OC(=O)OC(Cl)C(Cl)(Cl)Cl.N[C@@H](CC(=O)O)C(=O)O>O>CC(C)(C)OC(=O)N[C@@H](CC(=O)O)C(=O)O
ord_dataset-01dbb772c5e249108f0b191ed17a2c0c
ord-9b0ce90354764aed88d683b8b0a391d1
CC(Cl)OC(=O)OCc1ccco1.CCOC(=O)CN>>CCOC(=O)CNC(=O)OCc1ccco1
C(OC(C)Cl)(OCC1=CC=CO1)=O.NCC(=O)OCC.O.[Na+].[Cl-]>>C(C1=CC=CO1)OC(=O)NCC(=O)OCC
CC(Cl)O[C:8](=[O:9])[O:10][CH2:11][c:12]1[cH:13][cH:14][cH:15][o:16]1.[CH3:1][CH2:2][O:3][C:4](=[O:5])[CH2:6][NH2:7]>>[CH3:1][CH2:2][O:3][C:4](=[O:5])[CH2:6][NH:7][C:8](=[O:9])[O:10][CH2:11][c:12]1[cH:13][cH:14][cH:15][o:16]1
CC(Cl)OC(=O)OCc1ccco1.CCOC(=O)CN
CCOC(=O)CNC(=O)OCc1ccco1
null
null
C([O-])([O-])=O.[K+].[K+].C1CCOC1
Protection
OtherReaction
1723d7f7b61a78407ccc5d039d02c2aeebdda75282911635d78cfcb3c9298d34
1c0a2d114da0b035f9f98045bd1694b901b7743334178af36300fbe86a79443c
c1ccoc1
C-C(-Cl)-O-[C;H0;D3;+0:1](=[O;D1;H0:2])-[#8:3]-[C:4].[C:5]-[#8:6]-[C:7](=[O;D1;H0:8])-[C:9]-[NH2;D1;+0:10]>>[C:4]-[#8:3]-[C;H0;D3;+0:1](=[O;D1;H0:2])-[NH;D2;+0:10]-[C:9]-[C:7](=[O;D1;H0:8])-[#8:6]-[C:5]
66
[{"value": 66.0, "product": "C(C1=CC=CO1)OC(=O)NCC(=O)OCC", "details": "PERCENTYIELD", "is_desired": false}, {"value": 66.0, "product": "C(C1=CC=CO1)OC(=O)NCC(=O)OCC", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
18
HOUR
2.05 g (10 mmol) of α-chloroethyl furfuryl carbonate are added to a solution of 1.03 g (10 mmol) of ethyl glycinate in 6 ml of THF and 4 ml of 0.5M potassium carbonate solution maintained at between 5° and 10° C. The mixture is allowed to come to room temperature and is stirred for 18 hours. 50 ml of water saturated wi...
10.6084/m9.figshare.5104873.v1
null
Secondary halide.Carbonic Ester.Primary amine
Carbamic ester
null
null
c1ccoc1
HCl
C([O-])([O-])=O.[K+].[K+].C1CCOC1
null
18
CC(Cl)OC(=O)OCc1ccco1.CCOC(=O)CN>C([O-])([O-])=O.[K+].[K+].C1CCOC1>CCOC(=O)CNC(=O)OCc1ccco1
ord_dataset-01dbb772c5e249108f0b191ed17a2c0c
ord-0390e1237c0d4ce1b863fbe6e79e9218
CCOCCSC(SC(C)=O)=C(C(=O)OCc1ccc([N+](=O)[O-])cc1)N1C(=O)CC1SCC.O=C(OO)c1cccc(Cl)c1>>CCOCCSC(SC(C)=O)=C(C(=O)OCc1ccc([N+](=O)[O-])cc1)N1C(=O)CC1S(=O)CC
C(C)SC1CC(N1C(C(=O)OCC1=CC=C(C=C1)[N+](=O)[O-])=C(SCCOCC)SC(C)=O)=O.ClC1=CC(=CC=C1)C(=O)OO>>C(C)S(=O)C1CC(N1C(C(=O)OCC1=CC=C(C=C1)[N+](=O)[O-])=C(SCCOCC)SC(C)=O)=O
[CH3:1][CH2:2][O:3][CH2:4][CH2:5][S:6][C:7]([S:8][C:9]([CH3:10])=[O:11])=[C:12]([C:13](=[O:14])[O:15][CH2:16][c:17]1[cH:18][cH:19][c:20]([N+:21](=[O:22])[O-:23])[cH:24][cH:25]1)[N:26]1[C:27](=[O:28])[CH2:29][CH:30]1[S:31][CH2:33][CH3:34].O=C(O[OH:32])c1cccc(Cl)c1>>[CH3:1][CH2:2][O:3][CH2:4][CH2:5][S:6][C:7]([S:8][C:9](...
CCOCCSC(SC(C)=O)=C(C(=O)OCc1ccc([N+](=O)[O-])cc1)N1C(=O)CC1SCC.O=C(OO)c1cccc(Cl)c1
CCOCCSC(SC(C)=O)=C(C(=O)OCc1ccc([N+](=O)[O-])cc1)N1C(=O)CC1S(=O)CC
null
null
C(Cl)Cl
Oxidation
Sulfanyl to sulfinyl_peroxide
95b5106b07a173d8eafc1c9c8a6c938befe131c3d1caaf5886529b7aee55ea9d
7652b53bb02130dccfe4b1e8905d7f3db7f05ff3a95a0003c1bab09b1ad4083e
C=C(C(=O)OCc1ccccc1)N1CCC1=O
Cl-c1:c:c:c:c(-C(=O)-O-[OH;D1;+0:1]):c:1.[#8:2]-[C:3](=[O;D1;H0:4])-[C:5](=[C:6])-[#7:7]1-[C:8](=[O;D1;H0:9])-[C:10]-[C:11]-1-[S;H0;D2;+0:12]-[C:13]-[C;D1;H3:14]>>[#8:2]-[C:3](=[O;D1;H0:4])-[C:5](=[C:6])-[#7:7]1-[C:8](=[O;D1;H0:9])-[C:10]-[C:11]-1-[S;H0;D3;+0:12](=[O;H0;D1;+0:1])-[C:13]-[C;D1;H3:14]
null
[]
0
CELSIUS
1
HOUR
A solution of 1.4 g p-nitrobenzyl 2-(4-ethylthio-2-oxo-1-azetidinyl)-3-acetylthio-3-(2-ethoxyethylthio)-acrylate in 75 ml. methylene chloride was cooled to 0° C. under a nitrogen atmosphere. A solution of 0.551 g m-chloroperbenzoic acid in 25 ml methylene chloride was added dropwise, then the reaction mixture was stirr...
10.6084/m9.figshare.5104873.v1
null
Aromatic halide.Peroxide.Monosulfide
Sulfoxide
c1ccccc1
null
c1ccccc1.C1C[NH]C1
HCl
C(Cl)Cl
0
1
CCOCCSC(SC(C)=O)=C(C(=O)OCc1ccc([N+](=O)[O-])cc1)N1C(=O)CC1SCC.O=C(OO)c1cccc(Cl)c1>C(Cl)Cl>CCOCCSC(SC(C)=O)=C(C(=O)OCc1ccc([N+](=O)[O-])cc1)N1C(=O)CC1S(=O)CC
ord_dataset-01dbb772c5e249108f0b191ed17a2c0c
ord-869be1612db248ec8bde7c16dc757fd7
CCOCCSC(SC(C)=O)=C(C(=O)OCc1ccc([N+](=O)[O-])cc1)N1C(=O)CC1S(=O)CC.O=C(Cl)C(=O)Cl>>CCOCCSC(SC(C)=O)=C(C(=O)OCc1ccc([N+](=O)[O-])cc1)N1C(=O)CC1Cl
C(C)S(=O)C1CC(N1C(C(=O)OCC1=CC=C(C=C1)[N+](=O)[O-])=C(SCCOCC)SC(C)=O)=O.C(C(=O)Cl)(=O)Cl>>ClC1CC(N1C(C(=O)OCC1=CC=C(C=C1)[N+](=O)[O-])=C(SCCOCC)SC(C)=O)=O
CCS(=O)[CH:30]1[N:26]([C:12](=[C:7]([S:6][CH2:5][CH2:4][O:3][CH2:2][CH3:1])[S:8][C:9]([CH3:10])=[O:11])[C:13](=[O:14])[O:15][CH2:16][c:17]2[cH:18][cH:19][c:20]([N+:21](=[O:22])[O-:23])[cH:24][cH:25]2)[C:27](=[O:28])[CH2:29]1.O=C(Cl)C(=O)[Cl:31]>>[CH3:1][CH2:2][O:3][CH2:4][CH2:5][S:6][C:7]([S:8][C:9]([CH3:10])=[O:11])=[...
CCOCCSC(SC(C)=O)=C(C(=O)OCc1ccc([N+](=O)[O-])cc1)N1C(=O)CC1S(=O)CC.O=C(Cl)C(=O)Cl
CCOCCSC(SC(C)=O)=C(C(=O)OCc1ccc([N+](=O)[O-])cc1)N1C(=O)CC1Cl
null
null
C(Cl)Cl
Functional Group Interconversion
OtherReaction
7248405afe644c1a2ee565511a16c79f1d77d1fea282d76d510569ecda874877
48879576de8a8b2fa13623a529cb30f8c6008d5356f01cd965e9e2a3019acb11
C=C(C(=O)OCc1ccccc1)N1CCC1=O
C-C-S(=O)-[CH;D3;+0:1]1-[C:2]-[C:3](=[O;D1;H0:4])-[#7:5]-1-[C:6](-[C:7](-[#8:8])=[O;D1;H0:9])=[C:10](-[#16:11])-[#16:12]-[C:13](-[C;D1;H3:14])=[O;D1;H0:15].Cl-C(=O)-C(=O)-[Cl;H0;D1;+0:16]>>[#16:11]-[C:10](-[#16:12]-[C:13](-[C;D1;H3:14])=[O;D1;H0:15])=[C:6](-[#7:5]1-[C:3](=[O;D1;H0:4])-[C:2]-[CH;D3;+0:1]-1-[Cl;H0;D1;+0:...
null
[]
null
null
null
null
A solution of 1.2 g p-nitrobenzyl 2-(4-ethylsulfinyl-2-oxo-1-azetidinyl)-3-acetylthio-3-(2-ethoxyethylthio)-acrylate in 50 ml methylene chloride was cooled to -50° C. under a nitrogen atmosphere. Oxalyl chloride (0.196 ml) was added dropwise at -50° C., then the reaction mixture was allowed to warm to -15°. After 1 hou...
10.6084/m9.figshare.5104873.v1
null
Acyl halide.Acyl halide.Sulfoxide
Secondary halide
C1C[NH]C1
C1C[NH]C1
c1ccccc1.C1C[NH]C1
HCl
C(Cl)Cl
null
null
CCOCCSC(SC(C)=O)=C(C(=O)OCc1ccc([N+](=O)[O-])cc1)N1C(=O)CC1S(=O)CC.O=C(Cl)C(=O)Cl>C(Cl)Cl>CCOCCSC(SC(C)=O)=C(C(=O)OCc1ccc([N+](=O)[O-])cc1)N1C(=O)CC1Cl
ord_dataset-01dbb772c5e249108f0b191ed17a2c0c
ord-5cd096596a2f40b4833d1c38618339f5
CCOCCSC(=S)[S-].CCSC1CC(=O)N1C(Cl)C(=O)OCc1ccc([N+](=O)[O-])cc1>>CCOCCSC(=S)SC(C(=O)OCc1ccc([N+](=O)[O-])cc1)N1C(=O)CC1SCC
C(SCCOCC)([S-])=S.[K+].C(C)SC1CC(N1C(C(=O)OCC1=CC=C(C=C1)[N+](=O)[O-])Cl)=O>>C(C)SC1CC(N1C(C(=O)OCC1=CC=C(C=C1)[N+](=O)[O-])SC(=S)SCCOCC)=O
[CH3:1][CH2:2][O:3][CH2:4][CH2:5][S:6][C:7](=[S:8])[S-:9].Cl[CH:10]([C:11](=[O:12])[O:13][CH2:14][c:15]1[cH:16][cH:17][c:18]([N+:19](=[O:20])[O-:21])[cH:22][cH:23]1)[N:24]1[C:25](=[O:26])[CH2:27][CH:28]1[S:29][CH2:30][CH3:31]>>[CH3:1][CH2:2][O:3][CH2:4][CH2:5][S:6][C:7](=[S:8])[S:9][CH:10]([C:11](=[O:12])[O:13][CH2:14]...
CCOCCSC(=S)[S-].CCSC1CC(=O)N1C(Cl)C(=O)OCc1ccc([N+](=O)[O-])cc1
CCOCCSC(=S)SC(C(=O)OCc1ccc([N+](=O)[O-])cc1)N1C(=O)CC1SCC
null
[Cl-].C(C1=CC=CC=C1)[N+](CC)(CC)CC
C(Cl)Cl
Heteroatom Alkylation and Arylation
OtherReaction
38b34234eb49e03ae7a1fdde3465828940ad611ca2c7820b3bbcd591b148f6ec
745f2b0be08dc7d77c5c1355128858f853bce6044c19247ba807d27934f437f4
O=C(CN1CCC1=O)OCc1ccccc1
Cl-[CH;D3;+0:1](-[#7:2]1-[C:3]-[C:4]-[C:5]-1=[O;D1;H0:6])-[C:7](=[O;D1;H0:8])-[#8:9]-[C:10].[#16:11]-[C:12](-[S-;H0;D1:13])=[S;D1;H0:14]>>[#16:11]-[C:12](=[S;D1;H0:14])-[S;H0;D2;+0:13]-[CH;D3;+0:1](-[#7:2]1-[C:3]-[C:4]-[C:5]-1=[O;D1;H0:6])-[C:7](=[O;D1;H0:8])-[#8:9]-[C:10]
30.9
[{"value": 30.9, "product": "C(C)SC1CC(N1C(C(=O)OCC1=CC=C(C=C1)[N+](=O)[O-])SC(=S)SCCOCC)=O", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
1
HOUR
A solution of 3.58 g potassium 2-ethoxyethyl trithiocarbonate and 3.7 g benzyltriethylammonium chloride in 100 ml methylene chloride was cooled to 0° C. under a nitrogen atmosphere and a solution of 5.3 g of p-nitrobenzyl 2-(4-ethylthio-2-oxo-1-azetidinyl)-2-chloroacetate in 50 ml methylene chloride was added dropwise....
10.6084/m9.figshare.5104873.v1
null
Secondary halide.Ester.Thiocarbonyl
Ester.Thiocarbonyl
null
null
c1ccccc1.C1C[NH]C1
Other
[Cl-].C(C1=CC=CC=C1)[N+](CC)(CC)CC.C(Cl)Cl
null
1
CCOCCSC(=S)[S-].CCSC1CC(=O)N1C(Cl)C(=O)OCc1ccc([N+](=O)[O-])cc1>[Cl-].C(C1=CC=CC=C1)[N+](CC)(CC)CC.C(Cl)Cl>CCOCCSC(=S)SC(C(=O)OCc1ccc([N+](=O)[O-])cc1)N1C(=O)CC1SCC
ord_dataset-01dbb772c5e249108f0b191ed17a2c0c
ord-e72d089519f840f3b1c92dc784c5a6a9
CCSC1CC(=O)N1C(O)C(=O)OCc1ccc([N+](=O)[O-])cc1.O=S(Cl)Cl>>CCSC1CC(=O)N1C(Cl)C(=O)OCc1ccc([N+](=O)[O-])cc1
S(=O)(Cl)Cl.C(C)SC1CC(N1C(C(=O)OCC1=CC=C(C=C1)[N+](=O)[O-])O)=O.CC1=NC(=CC=C1)C>>C(C)SC1CC(N1C(C(=O)OCC1=CC=C(C=C1)[N+](=O)[O-])Cl)=O
O[CH:9]([N:8]1[CH:4]([S:3][CH2:2][CH3:1])[CH2:5][C:6]1=[O:7])[C:11](=[O:12])[O:13][CH2:14][c:15]1[cH:16][cH:17][c:18]([N+:19](=[O:20])[O-:21])[cH:22][cH:23]1.O=S(Cl)[Cl:10]>>[CH3:1][CH2:2][S:3][CH:4]1[CH2:5][C:6](=[O:7])[N:8]1[CH:9]([Cl:10])[C:11](=[O:12])[O:13][CH2:14][c:15]1[cH:16][cH:17][c:18]([N+:19](=[O:20])[O-:21...
CCSC1CC(=O)N1C(O)C(=O)OCc1ccc([N+](=O)[O-])cc1.O=S(Cl)Cl
CCSC1CC(=O)N1C(Cl)C(=O)OCc1ccc([N+](=O)[O-])cc1
null
null
O1CCCC1
Functional Group Interconversion
Alcohol to chloride_SOCl2
120bceabcea6bdd11eaba1f0010d1a819949b303a9b0a1a6f1466a187cd61a7d
5eacb98c50d3e231ab89acc1b6d4d18d9e568f456953b3682de2c7e4e6b85c60
O=C(CN1CCC1=O)OCc1ccccc1
Cl-S(=O)-[Cl;H0;D1;+0:1].O-[CH;D3;+0:2](-[#7:3]1-[C:4]-[C:5]-[C:6]-1=[O;D1;H0:7])-[C:8](=[O;D1;H0:9])-[#8:10]-[C:11]>>[C:11]-[#8:10]-[C:8](=[O;D1;H0:9])-[CH;D3;+0:2](-[Cl;H0;D1;+0:1])-[#7:3]1-[C:4]-[C:5]-[C:6]-1=[O;D1;H0:7]
null
[]
null
null
15
MINUTE
To a stirred solution of 6.8 g. of p-nitrobenzyl 2-(4-ethylthio-2-oxo-1-azetidinyl)-2-hydroxyacetate in 200 ml. of tetrahydrofuran at 0°-5° C. was added 2.98 ml. of 2,6-dimethylpyridine. This was followed by dropwise addition of a solution of 1.73 ml. of thionyl chloride in 20 ml. of tetrahydrofuran, over a 5-minute pe...
10.6084/m9.figshare.5104873.v1
null
Ester.Secondary alcohol
Secondary halide
null
null
C1C[NH]C1.c1ccccc1
HCl
O1CCCC1
null
0.25
CCSC1CC(=O)N1C(O)C(=O)OCc1ccc([N+](=O)[O-])cc1.O=S(Cl)Cl>O1CCCC1>CCSC1CC(=O)N1C(Cl)C(=O)OCc1ccc([N+](=O)[O-])cc1
ord_dataset-01dbb772c5e249108f0b191ed17a2c0c
ord-19f79d6d3da9450dae07f2e0f2b882be
CCOCCS.S=C=S>>CCOCCSC(=S)[S-]
CC(C)([O-])C.[K+].C(C)OCCS.C(=S)=S>>C(SCCOCC)([S-])=S.[K+]
[CH3:1][CH2:2][O:3][CH2:4][CH2:5][SH:6].[C:7](=[S:8])=[S:9]>>[CH3:1][CH2:2][O:3][CH2:4][CH2:5][S:6][C:7](=[S:8])[S-:9]
CCOCCS.S=C=S
CCOCCSC(=S)[S-]
null
null
O1CCCC1
Functional Group Addition
OtherReaction
5f4f81b7522510854c92122b358f666f31255d660e00e3337608c3c2cc3fe429
0fb8dc55a0761aaea061c344d8eb684ac3fd7c35d8be8b5acd462a6820bdca01
null
[C:1]-[C:2]-[SH;D1;+0:3].[S;D1;H0:4]=[C;H0;D2;+0:5]=[S;H0;D1;+0:6]>>[C:1]-[C:2]-[S;H0;D2;+0:3]-[C;H0;D3;+0:5](-[S-;H0;D1:6])=[S;D1;H0:4]
null
[]
25
CELSIUS
1
HOUR
To a solution of 6.79 g potassium t-butoxide in 300 ml of anhydrous tetrahydrofuran cooled to 0° C. under a nitrogen atmosphere was added 6.42 g of 2-mercaptoethyl ethyl ether. The resulting slurry was stirred at 25° C. for 1 hour, then 4.4 ml. of carbon disulfide was added dropwise at 0° C. The resulting solution was ...
10.6084/m9.figshare.5104873.v1
null
Aliphatic thiol
Thiocarbonyl
null
null
null
null
O1CCCC1
25
1
CCOCCS.S=C=S>O1CCCC1>CCOCCSC(=S)[S-]
ord_dataset-01dbb772c5e249108f0b191ed17a2c0c
ord-00472b5c1cba4539a1ade37a830760de
CC(=O)O.O=C1c2ccccc2C(=O)N1c1ncc(C(Cl)Cl)nc1CCl>>CC(=O)OCc1nc(C(Cl)Cl)cnc1N1C(=O)c2ccccc2C1=O
C(C)(=O)O.C(C)(=O)[O-].[K+].ClCC=1C(=NC=C(N1)C(Cl)Cl)N1C(C=2C(C1=O)=CC=CC2)=O.ClCCl>>C(C)(=O)OCC=1C(=NC=C(N1)C(Cl)Cl)N1C(C=2C(C1=O)=CC=CC2)=O
[CH3:1][C:2](=[O:3])[OH:4].Cl[CH2:5][c:6]1[n:7][c:8]([CH:9]([Cl:10])[Cl:11])[cH:12][n:13][c:14]1[N:15]1[C:16](=[O:17])[c:18]2[cH:19][cH:20][cH:21][cH:22][c:23]2[C:24]1=[O:25]>>[CH3:1][C:2](=[O:3])[O:4][CH2:5][c:6]1[n:7][c:8]([CH:9]([Cl:10])[Cl:11])[cH:12][n:13][c:14]1[N:15]1[C:16](=[O:17])[c:18]2[cH:19][cH:20][cH:21][c...
CC(=O)O.O=C1c2ccccc2C(=O)N1c1ncc(C(Cl)Cl)nc1CCl
CC(=O)OCc1nc(C(Cl)Cl)cnc1N1C(=O)c2ccccc2C1=O
null
null
CS(=O)C
Heteroatom Alkylation and Arylation
Williamson Ether Synthesis
06c4f868ad4646eea8208ecb83f54ca035dd62d04f0d8101641a4f487f2c695c
8446834f0edd1e71a2dcaffc09b80c7367abf3407263a8998354a2d20c1766bb
O=C1c2ccccc2C(=O)N1c1cnccn1
Cl-[CH2;D2;+0:1]-[c:2]1:[#7;a:3]:[c:4]:[c:5]:[#7;a:6]:[c:7]:1-[#7:8](-[C:9]=[O;D1;H0:10])-[C:11]=[O;D1;H0:12].[C;D1;H3:13]-[C:14](=[O;D1;H0:15])-[OH;D1;+0:16]>>[C;D1;H3:13]-[C:14](=[O;D1;H0:15])-[O;H0;D2;+0:16]-[CH2;D2;+0:1]-[c:2]1:[#7;a:3]:[c:4]:[c:5]:[#7;a:6]:[c:7]:1-[#7:8](-[C:9]=[O;D1;H0:10])-[C:11]=[O;D1;H0:12]
77
[{"value": 77.0, "product": "C(C)(=O)OCC=1C(=NC=C(N1)C(Cl)Cl)N1C(C=2C(C1=O)=CC=CC2)=O", "details": "PERCENTYIELD", "is_desired": false}]
null
null
3
DAY
50 ml of absolute glacial acetic acid and 35 g of potassium acetate were added to a solution of 57.7 g (0.16 mole) of 65% strength 3-chloromethyl-5-dichloromethyl-2-phthalimidopyrazine in 1,000 ml of dimethyl sulfoxide, and the mixture was then stirred for three days at room temperature. Thereafter, 1,000 ml of dichlor...
10.6084/m9.figshare.5104873.v1
null
Primary halide.Carboxylic acid
Ester
null
null
c1cnccn1.c1ccc2c(c1)C[NH]C2
HCl
CS(=O)C
null
72
CC(=O)O.O=C1c2ccccc2C(=O)N1c1ncc(C(Cl)Cl)nc1CCl>CS(=O)C>CC(=O)OCc1nc(C(Cl)Cl)cnc1N1C(=O)c2ccccc2C1=O
ord_dataset-01dbb772c5e249108f0b191ed17a2c0c
ord-25cf147f10cf48b9989fcb580416b649
CC(=O)OCc1nc(C(Cl)Cl)cnc1N1C(=O)c2ccccc2C1=O>>O=C1c2ccccc2C(=O)N1c1ncc(C(Cl)Cl)nc1CO
C(C)(=O)OC.C(C)(=O)OCC=1C(=NC=C(N1)C(Cl)Cl)N1C(C=2C(C1=O)=CC=CC2)=O.C1(=CC=C(C=C1)S(=O)(=O)O)C>>ClC(C=1N=C(C(=NC1)N1C(C=2C(C1=O)=CC=CC2)=O)CO)Cl
CC(=O)[O:22][CH2:21][c:20]1[c:12]([N:11]2[C:2](=[O:1])[c:3]3[cH:4][cH:5][cH:6][cH:7][c:8]3[C:9]2=[O:10])[n:13][cH:14][c:15]([CH:16]([Cl:17])[Cl:18])[n:19]1>>[O:1]=[C:2]1[c:3]2[cH:4][cH:5][cH:6][cH:7][c:8]2[C:9](=[O:10])[N:11]1[c:12]1[n:13][cH:14][c:15]([CH:16]([Cl:17])[Cl:18])[n:19][c:20]1[CH2:21][OH:22]
CC(=O)OCc1nc(C(Cl)Cl)cnc1N1C(=O)c2ccccc2C1=O
O=C1c2ccccc2C(=O)N1c1ncc(C(Cl)Cl)nc1CO
null
null
CO
Reduction
Hydrolysis or Hydrogenolysis of Carboxylic Esters or Thioesters
21d61543c6ec8a8cebe1b3ef55ef3dd20acbf79a4f1c12a7fb51e32be7a3248a
1fbcd628a0426673c5d10aa49a977cd2d1ae02a8cdf57bbb10d94aa03a94e937
O=C1c2ccccc2C(=O)N1c1cnccn1
C-C(=O)-[O;H0;D2;+0:1]-[C:2]-[c:3](:[#7;a:4]):[c:5]:[#7;a:6]>>[#7;a:6]:[c:5]:[c:3](-[C:2]-[OH;D1;+0:1]):[#7;a:4]
54
[{"value": 54.0, "product": "ClC(C=1N=C(C(=NC1)N1C(C=2C(C1=O)=CC=CC2)=O)CO)Cl", "details": "PERCENTYIELD", "is_desired": false}, {"value": 53.1, "product": "ClC(C=1N=C(C(=NC1)N1C(C=2C(C1=O)=CC=CC2)=O)CO)Cl", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
null
null
A mixture of 15 g (0.04 mole) of 3-acetoxymethyl-5-dichloromethyl-2-phthalimidopyrazine, 150 ml of methanol and 0.15 g of p-toluenesulfonic acid was heated to the boil, and a mixture of methanol and methyl acetate was slowly distilled off in the course of 5 hours. The mixture was then evaporated down to one-third of it...
10.6084/m9.figshare.5104873.v1
null
Ester
Primary alcohol
null
null
c1ccc2c(c1)C[NH]C2.c1cnccn1
HO-
CO
null
null
CC(=O)OCc1nc(C(Cl)Cl)cnc1N1C(=O)c2ccccc2C1=O>CO>O=C1c2ccccc2C(=O)N1c1ncc(C(Cl)Cl)nc1CO
ord_dataset-01dbb772c5e249108f0b191ed17a2c0c
ord-0e6c16dd3649420f8ec300810a013520
O=C1c2ccccc2C(=O)N1c1ncc(C(Cl)Cl)nc1CO>>O=Cc1nc(C(Cl)Cl)cnc1N1C(=O)c2ccccc2C1=O
[Cr](=O)(=O)([O-])Cl.[NH+]1=CC=CC=C1.OCC=1C(=NC=C(N1)C(Cl)Cl)N1C(C=2C(C1=O)=CC=CC2)=O>>C(=O)C=1C(=NC=C(N1)C(Cl)Cl)N1C(C=2C(C1=O)=CC=CC2)=O
[OH:1][CH2:2][c:3]1[n:4][c:5]([CH:6]([Cl:7])[Cl:8])[cH:9][n:10][c:11]1[N:12]1[C:13](=[O:14])[c:15]2[cH:16][cH:17][cH:18][cH:19][c:20]2[C:21]1=[O:22]>>[O:1]=[CH:2][c:3]1[n:4][c:5]([CH:6]([Cl:7])[Cl:8])[cH:9][n:10][c:11]1[N:12]1[C:13](=[O:14])[c:15]2[cH:16][cH:17][cH:18][cH:19][c:20]2[C:21]1=[O:22]
O=C1c2ccccc2C(=O)N1c1ncc(C(Cl)Cl)nc1CO
O=Cc1nc(C(Cl)Cl)cnc1N1C(=O)c2ccccc2C1=O
null
null
ClCCl
Oxidation
Oxidation or Dehydrogenation of Alcohols to Aldehydes and Ketones
41bfa9deea81b465c88ad21fdfb64a2e1ba29490558cf430df132cb98b4a538b
0a03c6724c1862e8f86d4a463afda55b8e067dc6cb42597b472eb7cabc03eda3
O=C1c2ccccc2C(=O)N1c1cnccn1
[O;D1;H0:1]=[C:2]-[#7:3](-[c:4]1:[#7;a:5]:[c:6]:[c:7]:[#7;a:8]:[c:9]:1-[CH2;D2;+0:10]-[OH;D1;+0:11])-[C:12]=[O;D1;H0:13]>>[O;D1;H0:1]=[C:2]-[#7:3](-[c:4]1:[#7;a:5]:[c:6]:[c:7]:[#7;a:8]:[c:9]:1-[CH;D2;+0:10]=[O;H0;D1;+0:11])-[C:12]=[O;D1;H0:13]
78
[{"value": 76.0, "product": "C(=O)C=1C(=NC=C(N1)C(Cl)Cl)N1C(C=2C(C1=O)=CC=CC2)=O", "details": "PERCENTYIELD", "is_desired": false}, {"value": 78.0, "product": "C(=O)C=1C(=NC=C(N1)C(Cl)Cl)N1C(C=2C(C1=O)=CC=CC2)=O", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
40
MINUTE
5.1 g of pyridinium chlorochromate were added a little at a time to a solution of 4 g of 3-hydroxymethyl-5-dichloromethyl-2-phthalimidopyrazine in 80 ml of dichloromethane at 35° C., after which the mixture was stirred for 40 minutes and filtered over silica gel, and the filtrate was evaporated down. 3.1 g (76%) of col...
10.6084/m9.figshare.5104873.v1
null
Primary alcohol
Aldehyde
null
null
c1cnccn1.c1ccc2c(c1)C[NH]C2
null
ClCCl
null
0.666667
O=C1c2ccccc2C(=O)N1c1ncc(C(Cl)Cl)nc1CO>ClCCl>O=Cc1nc(C(Cl)Cl)cnc1N1C(=O)c2ccccc2C1=O
ord_dataset-01dbb772c5e249108f0b191ed17a2c0c
ord-e962f65fda1a436697d07c873020f372
NO.O=Cc1nc(C(Cl)Cl)cnc1N1C(=O)c2ccccc2C1=O>>O=C1c2ccccc2C(=O)N1C1N=CC(C(Cl)Cl)=NC1=NO
C(=O)C=1C(=NC=C(N1)C(Cl)Cl)N1C(C=2C(C1=O)=CC=CC2)=O.Cl.NO.O>>N(O)=C1C(N=CC(=N1)C(Cl)Cl)N1C(C=2C(C1=O)=CC=CC2)=O
[NH2:21][OH:22].O=C[c:20]1[c:12]([N:11]2[C:2](=[O:1])[c:3]3[cH:4][cH:5][cH:6][cH:7][c:8]3[C:9]2=[O:10])[n:13][cH:14][c:15]([CH:16]([Cl:17])[Cl:18])[n:19]1>>[O:1]=[C:2]1[c:3]2[cH:4][cH:5][cH:6][cH:7][c:8]2[C:9](=[O:10])[N:11]1[CH:12]1[N:13]=[CH:14][C:15]([CH:16]([Cl:17])[Cl:18])=[N:19][C:20]1=[N:21][OH:22]
NO.O=Cc1nc(C(Cl)Cl)cnc1N1C(=O)c2ccccc2C1=O
O=C1c2ccccc2C(=O)N1C1N=CC(C(Cl)Cl)=NC1=NO
null
null
CS(=O)C
Heteroatom Alkylation and Arylation
OtherReaction
6b3f184e4728d25b133818806556fb16066cbca25a6ba9e791fb15e323a0f1ad
39209ce76115b920d674ca536c6ba4e72d7a2b3dfb7f42642512f35ff765fe85
N=C1N=CC=NC1N1C(=O)c2ccccc2C1=O
O=C-[c;H0;D3;+0:1]1:[n;H0;D2;+0:2]:[c;H0;D3;+0:3](-[C:4](-[Cl;D1;H0:5])-[Cl;D1;H0:6]):[cH;D2;+0:7]:[n;H0;D2;+0:8]:[c;H0;D3;+0:9]:1-[#7:10]1-[C:11](=[O;D1;H0:12])-[c:13]:[c:14]-[C:15]-1=[O;D1;H0:16].[NH2;D1;+0:17]-[O;D1;H1:18]>>[Cl;D1;H0:5]-[C:4](-[Cl;D1;H0:6])-[C;H0;D3;+0:3]1=[N;H0;D2;+0:2]-[C;H0;D3;+0:1](=[N;H0;D2;+0:...
67.4
[{"value": 65.0, "product": "N(O)=C1C(N=CC(=N1)C(Cl)Cl)N1C(C=2C(C1=O)=CC=CC2)=O", "details": "PERCENTYIELD", "is_desired": false}, {"value": 67.4, "product": "N(O)=C1C(N=CC(=N1)C(Cl)Cl)N1C(C=2C(C1=O)=CC=CC2)=O", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
70
CELSIUS
15
MINUTE
A solution of 10 g of 3-formyl-5-dichloromethyl-2-phthalimidopyrazine in 50 ml of dimethyl sulfoxide was heated at 50° C., 7 g of hydroxylamine hydrochloride were added, and the mixture was stirred for 15 minutes at 70° C. Thereafter, 700 ml of water were added to the reaction solution, the mixture was filtered and the...
10.6084/m9.figshare.5104873.v1
null
Aldehyde.Substituted dicarboximide.Primary amine
Substituted imine.Substituted imine.Substituted dicarboximide.Oxime
c1cnccn1
C1=NCCN=C1
c1ccc2c(c1)C[NH]C2.C1=NCCN=C1
HO-
CS(=O)C
70
0.25
NO.O=Cc1nc(C(Cl)Cl)cnc1N1C(=O)c2ccccc2C1=O>CS(=O)C>O=C1c2ccccc2C(=O)N1C1N=CC(C(Cl)Cl)=NC1=NO
ord_dataset-01dbb772c5e249108f0b191ed17a2c0c
ord-8989c551d2d14ccc86118bea21ea1108
COC(OC)c1cnc(N2C(=O)c3ccccc3C2=O)c(C#N)n1>>COC(OC)c1cnc(N)c(C#N)n1
O.NN.C(#N)C=1C(=NC=C(N1)C(OC)OC)N1C(C=2C(C1=O)=CC=CC2)=O>>NC1=NC=C(N=C1C#N)C(OC)OC
O=C1c2ccccc2C(=O)[N:10]1[c:9]1[n:8][cH:7][c:6]([CH:3]([O:2][CH3:1])[O:4][CH3:5])[n:14][c:11]1[C:12]#[N:13]>>[CH3:1][O:2][CH:3]([O:4][CH3:5])[c:6]1[cH:7][n:8][c:9]([NH2:10])[c:11]([C:12]#[N:13])[n:14]1
COC(OC)c1cnc(N2C(=O)c3ccccc3C2=O)c(C#N)n1
COC(OC)c1cnc(N)c(C#N)n1
null
null
CO
Reduction
Phthalimide deprotection
d9f63cee80ef758bd939ff2a10772447b3092f1576180488281833a98eb1691a
dbfe4201a9328005dfaec4c3f363ddbb4ef3c9b825f648735dc97b2b57396333
c1cnccn1
O=C1-[N;H0;D3;+0:1](-[c:2]2:[#7;a:3]:[c:4]:[c:5]:[#7;a:6]:[c:7]:2-[C:8]#[N;D1;H0:9])-C(=O)-c2:c:c:c:c:c:2-1>>[N;D1;H0:9]#[C:8]-[c:7]1:[#7;a:6]:[c:5]:[c:4]:[#7;a:3]:[c:2]:1-[NH2;D1;+0:1]
75.1
[{"value": 75.0, "product": "NC1=NC=C(N=C1C#N)C(OC)OC", "details": "PERCENTYIELD", "is_desired": false}, {"value": 75.1, "product": "NC1=NC=C(N=C1C#N)C(OC)OC", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
null
null
0.2 g of hydrazine hydrate were added dropwise to a suspension of 2 g of 3-cyano-5-dimethoxymethyl-2-phthalimidopyrazine in 40 ml of absolute methanol at 40° C. Immediately after the addition, the solution became clear, and crystals were precipitated after a few minutes. Chromatography over silica gel gave 0.9 g (75%) ...
10.6084/m9.figshare.5104873.v1
null
Substituted dicarboximide
Primary amine
c1ccc2c(c1)C[NH]C2
null
c1cnccn1
HO-
CO
null
null
COC(OC)c1cnc(N2C(=O)c3ccccc3C2=O)c(C#N)n1>CO>COC(OC)c1cnc(N)c(C#N)n1
ord_dataset-01dbb772c5e249108f0b191ed17a2c0c
ord-e68e567d6ece4a128886cf5a849df771
CC(=O)O.O=C1c2ccccc2C(=O)N1c1ncc(C(Cl)Cl)nc1CCl>>O=C1c2ccccc2C(=O)N1c1ncc(C(Cl)Cl)nc1CO
C(C)(=O)O.C(C)(=O)[O-].[K+].ClCC=1C(=NC=C(N1)C(Cl)Cl)N1C(C=2C(C1=O)=CC=CC2)=O.ClCCl>>ClC(C=1N=C(C(=NC1)N1C(C=2C(C1=O)=CC=CC2)=O)CO)Cl
CC(=O)[OH:22].Cl[CH2:21][c:20]1[c:12]([N:11]2[C:2](=[O:1])[c:3]3[cH:4][cH:5][cH:6][cH:7][c:8]3[C:9]2=[O:10])[n:13][cH:14][c:15]([CH:16]([Cl:17])[Cl:18])[n:19]1>>[O:1]=[C:2]1[c:3]2[cH:4][cH:5][cH:6][cH:7][c:8]2[C:9](=[O:10])[N:11]1[c:12]1[n:13][cH:14][c:15]([CH:16]([Cl:17])[Cl:18])[n:19][c:20]1[CH2:21][OH:22]
CC(=O)O.O=C1c2ccccc2C(=O)N1c1ncc(C(Cl)Cl)nc1CCl
O=C1c2ccccc2C(=O)N1c1ncc(C(Cl)Cl)nc1CO
null
null
CS(=O)C.O
Heteroatom Alkylation and Arylation
OtherReaction
dcda08c3a2df177b88cf2633dca6c592556d271991617ee7f8f5c291332482db
73605e1c48f69a0b692de7bd8edcecdd32045375b4fa5443073a7ab513760941
O=C1c2ccccc2C(=O)N1c1cnccn1
C-C(=O)-[OH;D1;+0:1].Cl-[CH2;D2;+0:2]-[c:3]1:[#7;a:4]:[c:5]:[c:6]:[#7;a:7]:[c:8]:1-[#7:9](-[C:10]=[O;D1;H0:11])-[C:12]=[O;D1;H0:13]>>[O;D1;H0:13]=[C:12]-[#7:9](-[c:8]1:[#7;a:7]:[c:6]:[c:5]:[#7;a:4]:[c:3]:1-[CH2;D2;+0:2]-[OH;D1;+0:1])-[C:10]=[O;D1;H0:11]
47
[{"value": 47.0, "product": "ClC(C=1N=C(C(=NC1)N1C(C=2C(C1=O)=CC=CC2)=O)CO)Cl", "details": "PERCENTYIELD", "is_desired": false}]
null
null
3
DAY
50 ml of glacial acetic acid and 35 g of potassium acetate were added to a solution of 57.7 g (0.16 mole) of 65% strength 3-chloromethyl-5-dichloromethyl-2-phthalimidopyrazine in 1,000 ml of a 95:5 dimethyl sulfoxide/water mixture. The mixture was stirred for three days at room temperature, after which 1,000 ml of dich...
10.6084/m9.figshare.5104873.v1
null
Primary halide.Carboxylic acid
Primary alcohol
null
null
c1ccc2c(c1)C[NH]C2.c1cnccn1
HCl
CS(=O)C.O
null
72
CC(=O)O.O=C1c2ccccc2C(=O)N1c1ncc(C(Cl)Cl)nc1CCl>CS(=O)C.O>O=C1c2ccccc2C(=O)N1c1ncc(C(Cl)Cl)nc1CO
ord_dataset-01dbb772c5e249108f0b191ed17a2c0c
ord-ae89461366744f8aa04b8314f2a33939
CO.N=C(N)N.Nc1ccnc(N)n1>>N#Cc1cnc2nc(N)nc(N)c2c1
NC1=NC=CC(=N1)N.NC(=N)N.CO.Cl>>NC=1N=C(C2=C(N1)N=CC(=C2)C#N)N
O[CH3:2].[NH:1]=[C:8]([NH2:9])[NH2:10].N[c:14]1[cH:3][cH:4][n:5][c:6]([NH2:12])[n:7]1>>[N:1]#[C:2][c:3]1[cH:4][n:5][c:6]2[n:7][c:8]([NH2:9])[n:10][c:11]([NH2:12])[c:13]2[cH:14]1
CO.N=C(N)N.Nc1ccnc(N)n1
N#Cc1cnc2nc(N)nc(N)c2c1
null
[Pd].Cl[Pd]Cl
CCN(CC)CC.C(C)O.CN(C)C=O
Aromatic Heterocycle Formation
OtherReaction
91b4866c3b161f7a208a3bee41df2dac0d574663f05354223179b2100d22bbfa
58f037c0e173eb90165a8f54fb237e652cce581733f0de7cc15c3f4078bab34e
c1cnc2ncncc2c1
N-[c;H0;D3;+0:1]1:[cH;D2;+0:2]:[c:3]:[#7;a:4]:[c;H0;D3;+0:5](-[NH2;D1;+0:6]):[n;H0;D2;+0:7]:1.O-[CH3;D1;+0:8].[N;D1;H2:9]-[C;H0;D3;+0:10](-[NH2;D1;+0:11])=[NH;D1;+0:12]>>[N;D1;H2:9]-[c;H0;D3;+0:10]1:[n;H0;D2;+0:11]:[c:13](-[NH2;D1;+0:6]):[c:14]2:[cH;D2;+0:1]:[c;H0;D3;+0:2](-[C;H0;D2;+0:8]#[N;H0;D1;+0:12]):[c:3]:[#7;a:4...
95
[{"value": 95.0, "product": "NC=1N=C(C2=C(N1)N=CC(=C2)C#N)N", "details": "PERCENTYIELD", "is_desired": false}]
null
null
null
null
Referring now to Scheme I, compounds 3 and 4 were prepared by reported procedures, which proved to be readily adaptable to large-scale preparations. The reductive dechlorination Steps to give 5 and 6 were done in DMF--MeOH (N,N-dimethylformamide-methyl alcohol) solution containing 5% Pd on BaCO3. This method differs sl...
10.6084/m9.figshare.5104873.v1
null
Primary amine.Primary amine.Primary amine.Methanol
Nitrile.Primary amine
c1cncnc1
c1cnc2ncncc2c1
c1cnc2ncncc2c1
null
[Pd].Cl[Pd]Cl.CCN(CC)CC.C(C)O.CN(C)C=O
null
null
CO.N=C(N)N.Nc1ccnc(N)n1>[Pd].Cl[Pd]Cl.CCN(CC)CC.C(C)O.CN(C)C=O>N#Cc1cnc2nc(N)nc(N)c2c1
ord_dataset-01dbb772c5e249108f0b191ed17a2c0c
ord-f59a2889ea174bf0ac3472c52a9f95d2
N#Cc1cc(C#N)c(Cl)nc1N>>N#Cc1cnc(N)c(C#N)c1
NC1=NC(=C(C=C1C#N)C#N)Cl>>NC1=NC=C(C=C1C#N)C#N
Cl[c:4]1[n:5][c:6]([NH2:7])[c:3]([C:2]#[N:1])[cH:11][c:8]1[C:9]#[N:10]>>[N:1]#[C:2][c:3]1[cH:4][n:5][c:6]([NH2:7])[c:8]([C:9]#[N:10])[cH:11]1
N#Cc1cc(C#N)c(Cl)nc1N
N#Cc1cnc(N)c(C#N)c1
null
null
C1CCCCC1.CCOC(=O)C
Miscellaneous
Aromatic dehalogenation
7e204a847916e0c4c140c562819111cd0e4a9bc61594eac7c0805ff63a367ef2
f004e58a958e83ed69c0f163c54d2c11d46ff03ec9dbfbb5a519e7e4cb2f94a4
c1ccncc1
Cl-[c;H0;D3;+0:1]1:[#7;a:2]:[c;H0;D3;+0:3](-[N;D1;H2:4]):[c;H0;D3;+0:5](-[C:6]#[N;D1;H0:7]):[c:8]:[c;H0;D3;+0:9]:1-[C:10]#[N;D1;H0:11]>>[N;D1;H0:11]#[C:10]-[c;H0;D3;+0:9]1:[c:8]:[c;H0;D3;+0:5](-[C:6]#[N;D1;H0:7]):[cH;D2;+0:1]:[#7;a:2]:[c;H0;D3;+0:3]:1-[N;D1;H2:4]
73
[{"value": 73.0, "product": "NC1=NC=C(C=C1C#N)C#N", "details": "PERCENTYIELD", "is_desired": false}]
null
null
null
null
2-Amino-3,5-dicyanopyridine (5) was prepared from 3 using the procedure described below for the preparation of 5 except that 5 was recrystallised from MeCN [methyl cyanide; acetonitrile) (instead of EtOH). The yield was 73% (7.00 g from 12.0 g (67.2 mmol) of 3] of product homogeneous on TLC (cyclohexane-EtOAc, 1:1); mp...
10.6084/m9.figshare.5104873.v1
null
Aromatic halide
null
c1ccncc1
c1ccncc1
c1ccncc1
Other
C1CCCCC1.CCOC(=O)C
null
null
N#Cc1cc(C#N)c(Cl)nc1N>C1CCCCC1.CCOC(=O)C>N#Cc1cnc(N)c(C#N)c1
ord_dataset-01dbb772c5e249108f0b191ed17a2c0c
ord-717477a32b7f4cc0977022329f06cd51
Cc1c(C#N)c(N)nc(Cl)c1C#N>>Cc1c(C#N)cnc(N)c1C#N
NC1=NC(=C(C(=C1C#N)C)C#N)Cl.CO.C1CCCCC1.CCOC(=O)C>>NC1=NC=C(C(=C1C#N)C)C#N
Cl[c:6]1[c:3]([C:4]#[N:5])[c:2]([CH3:1])[c:10]([C:11]#[N:12])[c:8]([NH2:9])[n:7]1>>[CH3:1][c:2]1[c:3]([C:4]#[N:5])[cH:6][n:7][c:8]([NH2:9])[c:10]1[C:11]#[N:12]
Cc1c(C#N)c(N)nc(Cl)c1C#N
Cc1c(C#N)cnc(N)c1C#N
null
[Pd]
CN(C)C=O
Functional Group Interconversion
Aromatic dehalogenation
ea85ec2fde5700c76b45764563e70d433b50e38e1af4209f646f155266c8ec96
56de34d4a44cb25d9380269ee5e138b0f24b40a3a0db22c5508049dc775a861f
c1ccncc1
Cl-[c;H0;D3;+0:1](:[#7;a:2]:[c:3]):[c:4](-[C:5]#[N;D1;H0:6]):[c:7]>>[N;D1;H0:6]#[C:5]-[c:4](:[c:7]):[cH;D2;+0:1]:[#7;a:2]:[c:3]
86
[{"value": 86.0, "product": "NC1=NC=C(C(=C1C#N)C)C#N", "details": "PERCENTYIELD", "is_desired": false}]
null
null
null
null
Hydrogenolysis of 4 (10.0 g, 52.0 mmol) in DMF (150 mL)-MeOH (75 mL) containing 5% Pd on BaCO3 (10.0 g) was carried out in a Parr shaker with H2 pressure kept near 3.5 kg/cm2 (50 psi) for six hours. The mixture was then filtered (Celite mat), and evaporated to dryness (final conditions <1 mm, bath to 45° C.) The residu...
10.6084/m9.figshare.5104873.v1
null
Aromatic halide
null
c1ccncc1
c1ccncc1
c1ccncc1
Other
[Pd].CN(C)C=O
null
null
Cc1c(C#N)c(N)nc(Cl)c1C#N>[Pd].CN(C)C=O>Cc1c(C#N)cnc(N)c1C#N
ord_dataset-01dbb772c5e249108f0b191ed17a2c0c
ord-01537abe3d964860950784242d6215b3
N#Cc1cnc(N)c(C#N)c1.N=C(N)N>>N#Cc1cnc2nc(N)nc(N)c2c1
C1CCCCC1.CCOC(=O)C.NC(=N)N.Cl.C[O-].[Na+].NC1=NC=C(C=C1C#N)C#N>>NC=1N=C(C2=C(N1)N=CC(=C2)C#N)N
[N:1]#[C:2][c:3]1[cH:4][n:5][c:6]([NH2:7])[c:13]([C:11]#[N:12])[cH:14]1.N[C:8]([NH2:9])=[NH:10]>>[N:1]#[C:2][c:3]1[cH:4][n:5][c:6]2[n:7][c:8]([NH2:9])[n:10][c:11]([NH2:12])[c:13]2[cH:14]1
N#Cc1cnc(N)c(C#N)c1.N=C(N)N
N#Cc1cnc2nc(N)nc(N)c2c1
null
null
CCO
Aromatic Heterocycle Formation
OtherReaction
4a09d814c35ed57344475f361bf7e51991fe644e5fefeb06eaebd40f1ce7c451
1aa7191beb21c0c960b18631a0bd52edc8e0a5e54fb7edd4fc42913ae18d9901
c1cnc2ncncc2c1
N-[C;H0;D3;+0:1](-[N;D1;H2:2])=[NH;D1;+0:3].[N;H0;D1;+0:4]#[C;H0;D2;+0:5]-[c:6](:[c:7]):[c:8](-[NH2;D1;+0:9]):[#7;a:10]:[c:11]>>[N;D1;H2:2]-[c;H0;D3;+0:1]1:[n;H0;D2;+0:3]:[c;H0;D3;+0:5](-[NH2;D1;+0:4]):[c:6](:[c:7]):[c:8](:[#7;a:10]:[c:11]):[n;H0;D2;+0:9]:1
95
[{"value": 95.0, "product": "NC=1N=C(C2=C(N1)N=CC(=C2)C#N)N", "details": "PERCENTYIELD", "is_desired": false}, {"value": 34.0, "product": "NC=1N=C(C2=C(N1)N=CC(=C2)C#N)N", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
null
null
Guanidine·HCl (2.66 g, 27.8 mmol) was added to a solution of NaOMe (sodium methoxide) (1.50 g, 27.8 mmol) in absolute EtOH (180 mL). The mixture was stirred at 20°-23° C. for 15 minutes before 5 (2.00 g, 13.9 mmol) was added. After a 24-hour reflux period with rapid stirring, TLC (cyclohexane-EtOAc, 1:1) showed absence...
10.6084/m9.figshare.5104873.v1
null
Nitrile.Primary amine.Primary amine
Primary amine
c1ccncc1
c1cnc2ncncc2c1
c1cnc2ncncc2c1
Other
CCO
null
null
N#Cc1cnc(N)c(C#N)c1.N=C(N)N>CCO>N#Cc1cnc2nc(N)nc(N)c2c1
ord_dataset-01dbb772c5e249108f0b191ed17a2c0c
ord-97248722c0404b71aece60e2bbc0ba59
Cc1c(C=O)cnc2nc(N)nc(N)c12>>Cc1c(CO)cnc2nc(N)nc(N)c12
[BH4-].[Na+].NC=1N=C(C2=C(N1)N=CC(=C2C)C=O)N.[BH4-].[Na+].C(C)(=O)[O-].NC=1N=C(C2=C(N1)N=CC(=C2C)C=O)N>>NC=1N=C(C2=C(N1)N=CC(=C2C)CO)N
[CH3:1][c:2]1[c:3]([CH:4]=[O:5])[cH:6][n:7][c:8]2[n:9][c:10]([NH2:11])[n:12][c:13]([NH2:14])[c:15]12>>[CH3:1][c:2]1[c:3]([CH2:4][OH:5])[cH:6][n:7][c:8]2[n:9][c:10]([NH2:11])[n:12][c:13]([NH2:14])[c:15]12
Cc1c(C=O)cnc2nc(N)nc(N)c12
Cc1c(CO)cnc2nc(N)nc(N)c12
null
null
CO
Reduction
Reduction of aldehydes and ketones to alcohols
e7895795cd3f75445716c94697823c5929dcd4b5344525875fe75d36bca2f9d7
21bb81d5469aaaca71ab12c186bea4016451717fad8780cf288858a7d8fbc55a
c1cnc2ncncc2c1
[#7;a:1]:[c:2]:[#7;a:3]:[c:4]:[c:5](-[CH;D2;+0:6]=[O;H0;D1;+0:7]):[c:8]>>[#7;a:1]:[c:2]:[#7;a:3]:[c:4]:[c:5](-[CH2;D2;+0:6]-[OH;D1;+0:7]):[c:8]
null
[]
70
CELSIUS
2
HOUR
NaBH4 (500 mg, 13.2 mmol) was added in portions during a 10 minute interval to a stirred suspension of crude 13 (2.73 g), in MeOH (500 mL) at 20°-23° C. Stirring was continued for two hours, then NaBH4 (500 mg) was again added as before. After the mixture had been stirred overnight, HPLC (acetate buffer of pH 3.6-MeOH,...
10.6084/m9.figshare.5104873.v1
null
Aldehyde
Primary alcohol
null
null
c1cnc2ncncc2c1
null
CO
70
2
Cc1c(C=O)cnc2nc(N)nc(N)c12>CO>Cc1c(CO)cnc2nc(N)nc(N)c12
ord_dataset-01dbb772c5e249108f0b191ed17a2c0c
ord-ec77ee8ce6d54d51817a1b5b60ea9228
CCOC(=O)CC[C@H](NC(=O)c1ccc(N(CC)Cc2cnc3nc(N)nc(N)c3c2C)cc1)C(=O)OCC>>CCN(Cc1cnc2nc(N)nc(N)c2c1C)c1ccc(C(=O)N[C@@H](CCC(=O)O)C(=O)O)cc1
Cl.[OH-].[Na+].COC([C@@H](NC(C1=CC=C(C=C1)N(C)CC1=C(C2=C(N=C(N=C2N)N)N=C1)C)=O)CCC(=O)OC)=O.C(C)OC([C@@H](NC(C1=CC=C(C=C1)N(CC)CC1=C(C2=C(N=C(N=C2N)N)N=C1)C)=O)CCC(=O)OCC)=O>>NC=1N=C(C2=C(N1)N=CC(=C2C)CN(C2=CC=C(C(=O)N[C@@H](CCC(=O)O)C(=O)O)C=C2)CC)N
CC[O:30][C:28]([CH2:27][CH2:26][C@H:25]([NH:24][C:22]([c:21]1[cH:20][cH:19][c:18]([N:3]([CH2:2][CH3:1])[CH2:4][c:5]2[cH:6][n:7][c:8]3[n:9][c:10]([NH2:11])[n:12][c:13]([NH2:14])[c:15]3[c:16]2[CH3:17])[cH:35][cH:34]1)=[O:23])[C:31](=[O:32])[O:33]CC)=[O:29]>>[CH3:1][CH2:2][N:3]([CH2:4][c:5]1[cH:6][n:7][c:8]2[n:9][c:10]([N...
CCOC(=O)CC[C@H](NC(=O)c1ccc(N(CC)Cc2cnc3nc(N)nc(N)c3c2C)cc1)C(=O)OCC
CCN(Cc1cnc2nc(N)nc(N)c2c1C)c1ccc(C(=O)N[C@@H](CCC(=O)O)C(=O)O)cc1
null
null
null
Deprotection
OtherReaction
6e62db7aac546f574bcfb83067ba8906c30fcbfedfc37aa16b5eaad33833f45a
ed5fed81ba501ef41c88831ec6b9463b899bfdd0815c4145ae51c79addb226d0
c1ccc(NCc2cnc3ncncc3c2)cc1
C-C-[O;H0;D2;+0:1]-[C:2](-[C:3])=[O;D1;H0:4].C-C-[O;H0;D2;+0:5]-[C:6](-[C:7])=[O;D1;H0:8]>>[C:7]-[C:6](=[O;D1;H0:8])-[OH;D1;+0:5].[C:3]-[C:2](=[O;D1;H0:4])-[OH;D1;+0:1]
97
[{"value": 97.0, "product": "NC=1N=C(C2=C(N1)N=CC(=C2C)CN(C2=CC=C(C(=O)N[C@@H](CCC(=O)O)C(=O)O)C=C2)CC)N", "details": "PERCENTYIELD", "is_desired": false}]
null
null
null
null
N-[4-[[(2,4-Diamino-5-methylpyrido[2,3-d]pyrimidin-6-yl)methyl]ethylamino]benzoyl-L-glutamic acid (21, 5-Methyl-5-deaza-10-ethylaminopterin) was prepared by saponification of 19 as described for the conversion of 18 to 20; yield 97% (56 mg from 60 mg, 0.109 mmol), of 19·0.6H2O, homogeneous by HPLC. Spectral data: mass,...
10.6084/m9.figshare.5104873.v1
null
Ester.Ester
Carboxylic acid.Carboxylic acid
null
null
c1cnc2ncncc2c1.c1ccccc1
Other
null
null
null
CCOC(=O)CC[C@H](NC(=O)c1ccc(N(CC)Cc2cnc3nc(N)nc(N)c3c2C)cc1)C(=O)OCC>>CCN(Cc1cnc2nc(N)nc(N)c2c1C)c1ccc(C(=O)N[C@@H](CCC(=O)O)C(=O)O)cc1
ord_dataset-01dbb772c5e249108f0b191ed17a2c0c
ord-097ce1f06049442d8b63f92135cc032e
CCC(C)CCCCCBr.N#Cc1ccc(O)cc1>>CC[C@H](C)CCCCCOc1ccc(C#N)cc1
C(C(C)CC)O.C([O-])([O-])=O.[K+].[K+].C(#N)C1=CC=C(C=C1)O.BrCCCCCC(CC)C>>C[C@H](CCCCCOC1=CC=C(C#N)C=C1)CC
Br[CH2:9][CH2:8][CH2:7][CH2:6][CH2:5][CH:3]([CH2:2][CH3:1])[CH3:4].[OH:10][c:11]1[cH:12][cH:13][c:14]([C:15]#[N:16])[cH:17][cH:18]1>>[CH3:1][CH2:2][C@H:3]([CH3:4])[CH2:5][CH2:6][CH2:7][CH2:8][CH2:9][O:10][c:11]1[cH:12][cH:13][c:14]([C:15]#[N:16])[cH:17][cH:18]1
CCC(C)CCCCCBr.N#Cc1ccc(O)cc1
CC[C@H](C)CCCCCOc1ccc(C#N)cc1
null
null
CN(C=O)C
Heteroatom Alkylation and Arylation
Williamson Ether Synthesis
7e1040116e3a4cf0e8ec5cc7865388d9cd0efabce6d320a1c25a36e411018d8b
d5f4610d46ccc0478471c5bc0fb862644eaf764bbc5d93badb39d54f6ec8e0a5
c1ccccc1
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
Add 5.75 g of 4-cyanophenol 10 g of 1 brom-6-methyl octane synthesized of available active amyl alcohol, 6.67 g of anhydrous potassium carbonate, 30 ml of N,N-dimethyl formamide into 100 ml four-mouth flask under nitrogen atmosphere, allow to react for 8 hours at 110° C. After the reaction, filter the insoluble matter,...
10.6084/m9.figshare.5104873.v1
null
Primary halide.Aromatic alcohol
Ether
null
null
c1ccccc1
HBr
CN(C=O)C
null
null
CCC(C)CCCCCBr.N#Cc1ccc(O)cc1>CN(C=O)C>CC[C@H](C)CCCCCOc1ccc(C#N)cc1
ord_dataset-01dbb772c5e249108f0b191ed17a2c0c
ord-1ff5c11c42b04a318b57cf8f518bbb02
CCCCCCCCC(C(=O)OCC)C(=O)OCC.CC[C@H](C)CCCCCOc1ccc(C(=N)N)cc1>>CCCCCCCCc1c(O)nc(-c2ccc(OCCCCC[C@@H](C)CC)cc2)nc1O
S(O)(O)(=O)=O.[Na].C(CCCCCCC)C(C(=O)OCC)C(=O)OCC.C[O-].[Na+].Cl.C[C@H](CCCCCOC1=CC=C(C(=N)N)C=C1)CC>>C(CCCCCCC)C=1C(=NC(=NC1O)C1=CC=C(C=C1)OCCCCC[C@H](CC)C)O
CCO[C:10]([CH:9]([CH2:8][CH2:7][CH2:6][CH2:5][CH2:4][CH2:3][CH2:2][CH3:1])[C:31](OCC)=[O:32])=[O:11].[NH2:12][C:13]([c:14]1[cH:15][cH:16][c:17]([O:18][CH2:19][CH2:20][CH2:21][CH2:22][CH2:23][C@@H:24]([CH3:25])[CH2:26][CH3:27])[cH:28][cH:29]1)=[NH:30]>>[CH3:1][CH2:2][CH2:3][CH2:4][CH2:5][CH2:6][CH2:7][CH2:8][c:9]1[c:10]...
CCCCCCCCC(C(=O)OCC)C(=O)OCC.CC[C@H](C)CCCCCOc1ccc(C(=N)N)cc1
CCCCCCCCc1c(O)nc(-c2ccc(OCCCCC[C@@H](C)CC)cc2)nc1O
null
null
CO
Aromatic Heterocycle Formation
OtherReaction
d507ea5e988c6bcfe927f1b3a86f934f8a1c706f38171153cdf4dbd7aeb28e83
6504f33921726f64e36c5f3f322459b73652319c83071522ec21b8b88a33a5a7
c1ccc(-c2ncccn2)cc1
C-C-O-[C;H0;D3;+0:1](=[O;H0;D1;+0:2])-[CH;D3;+0:3](-[C:4]-[C:5])-[C;H0;D3;+0:6](=[O;H0;D1;+0:7])-O-C-C.[NH2;D1;+0:8]-[C;H0;D3;+0:9](=[NH;D1;+0:10])-[c;H0;D3;+0:11](:[c:12]:[c:13]):[c:14]:[c:15]>>[C:5]-[C:4]-[c;H0;D3;+0:3]1:[c;H0;D3;+0:1](-[OH;D1;+0:2]):[n;H0;D2;+0:8]:[c;H0;D3;+0:9](-[c;H0;D3;+0:11](:[c:12]:[c:13]):[c:1...
null
[]
null
null
null
null
Pour 1.15 g sodium metal, and 33 ml dry methanol into 100 ml four-mouth flask; add 5 g of optically active (s)-4-(6-methyloctyloxy)benzamidine hydrochloric acid salt, then pour 4.55 g of diethyl n-octylmalonate into this sodium methylate solution and then allow to react for 18 hours under heat and reflux conditions. Af...
10.6084/m9.figshare.5104873.v1
null
Ester.Ester.Primary amine
Aromatic alcohol.Aromatic alcohol
null
c1cncnc1
c1cncnc1.c1ccccc1
HO-
CO
null
null
CCCCCCCCC(C(=O)OCC)C(=O)OCC.CC[C@H](C)CCCCCOc1ccc(C(=N)N)cc1>CO>CCCCCCCCc1c(O)nc(-c2ccc(OCCCCC[C@@H](C)CC)cc2)nc1O
ord_dataset-01dbb772c5e249108f0b191ed17a2c0c
ord-e62665853a104cb08a8caeb3781bea61
CCCCCCCCc1c(Cl)nc(-c2ccc(OCCCCC[C@@H](C)CC)cc2)nc1Cl>>CCCCCCCCc1cnc(-c2ccc(OCCCCC[C@@H](C)CC)cc2)nc1
C(CCCCCCC)C=1C(=NC(=NC1Cl)C1=CC=C(C=C1)OCCCCC[C@H](CC)C)Cl.[O-2].[Mg+2].C(C)O>>C(CCCCCCC)C=1C=NC(=NC1)C1=CC=C(C=C1)OCCCCC[C@H](CC)C
Cl[c:10]1[c:9]([CH2:8][CH2:7][CH2:6][CH2:5][CH2:4][CH2:3][CH2:2][CH3:1])[c:30](Cl)[n:29][c:12](-[c:13]2[cH:14][cH:15][c:16]([O:17][CH2:18][CH2:19][CH2:20][CH2:21][CH2:22][C@@H:23]([CH3:24])[CH2:25][CH3:26])[cH:27][cH:28]2)[n:11]1>>[CH3:1][CH2:2][CH2:3][CH2:4][CH2:5][CH2:6][CH2:7][CH2:8][c:9]1[cH:10][n:11][c:12](-[c:13]...
CCCCCCCCc1c(Cl)nc(-c2ccc(OCCCCC[C@@H](C)CC)cc2)nc1Cl
CCCCCCCCc1cnc(-c2ccc(OCCCCC[C@@H](C)CC)cc2)nc1
null
[C].[Pd]
O
Reduction
OtherReaction
fcc37c9c611ca40bb9c411eab4802374f0106d75bef4c7f56886315f511a7627
0ecff68b4ffbd9fa417ba42b220387f06d93399a1e61c4d05eaeeacbdad5d93b
c1ccc(-c2ncccn2)cc1
Cl-[c;H0;D3;+0:1]1:[#7;a:2]:[c:3](-[c:4]):[#7;a:5]:[c;H0;D3;+0:6](-Cl):[c:7]:1-[C:8]>>[C:8]-[c:7]1:[cH;D2;+0:1]:[#7;a:2]:[c:3](-[c:4]):[#7;a:5]:[cH;D2;+0:6]:1
null
[]
null
null
null
null
Pour 1.88 g of optically active (s)-5-n-octyl-2-[4-(6-methyloctyloxy)phenyl]-4,6-dichloro-pyrimidine, 0.4 g of 10% palladium-carbon, 0.55 g of magnesium oxide, 60 ml of ethanol, and 45 ml of water, into a 200 ml flask, then add hydrogen under oil bath conditions at 50° C., until the logical amount of hydrogen has been ...
10.6084/m9.figshare.5104873.v1
null
Aromatic halide.Aromatic halide
null
c1cncnc1
c1cncnc1
c1cncnc1.c1ccccc1
Other
[C].[Pd].O
null
null
CCCCCCCCc1c(Cl)nc(-c2ccc(OCCCCC[C@@H](C)CC)cc2)nc1Cl>[C].[Pd].O>CCCCCCCCc1cnc(-c2ccc(OCCCCC[C@@H](C)CC)cc2)nc1
ord_dataset-01dbb772c5e249108f0b191ed17a2c0c
ord-ae7c4249e17a4e4bb669f0513f28a2f7
CCCCCCCCBr.CC[C@H](C)CCCCCc1cnc(-c2ccc(O)cc2)nc1>>CCCCCCCCOc1ccc(-c2ncc(CCCCC[C@@H](C)CC)cn2)cc1
BrCCCCCCCC.C[C@H](CCCCCC=1C=NC(=NC1)C1=CC=C(C=C1)O)CC.[H-].[Na+]>>C(CCCCCCC)OC1=CC=C(C=C1)C1=NC=C(C=N1)CCCCC[C@H](CC)C
Br[CH2:8][CH2:7][CH2:6][CH2:5][CH2:4][CH2:3][CH2:2][CH3:1].[OH:9][c:10]1[cH:11][cH:12][c:13](-[c:14]2[n:15][cH:16][c:17]([CH2:18][CH2:19][CH2:20][CH2:21][CH2:22][C@@H:23]([CH3:24])[CH2:25][CH3:26])[cH:27][n:28]2)[cH:29][cH:30]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:12][c:13](-[...
CCCCCCCCBr.CC[C@H](C)CCCCCc1cnc(-c2ccc(O)cc2)nc1
CCCCCCCCOc1ccc(-c2ncc(CCCCC[C@@H](C)CC)cn2)cc1
null
null
CN(C=O)C
Heteroatom Alkylation and Arylation
Williamson Ether Synthesis
7e1040116e3a4cf0e8ec5cc7865388d9cd0efabce6d320a1c25a36e411018d8b
d5f4610d46ccc0478471c5bc0fb862644eaf764bbc5d93badb39d54f6ec8e0a5
c1ccc(-c2ncccn2)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
Pour 0.33 g of sodium hydride (about 50% oil suspension), 3 ml of dry N,N-dimethylformamide into a 30 ml three-mouth flask equipped with a cooling tube, thermometer, dripping funnel, and calcium chloride tube. Next, slowly drip 1.71 g of optically active (s)-4-[5-(6-methyl octyl)-2-pyrimidinyl]phenol which is dissolved...
10.6084/m9.figshare.5104873.v1
null
Primary halide.Aromatic alcohol
Ether
null
null
c1ccccc1.c1cncnc1
HBr
CN(C=O)C
null
null
CCCCCCCCBr.CC[C@H](C)CCCCCc1cnc(-c2ccc(O)cc2)nc1>CN(C=O)C>CCCCCCCCOc1ccc(-c2ncc(CCCCC[C@@H](C)CC)cn2)cc1
ord_dataset-01dbb772c5e249108f0b191ed17a2c0c
ord-0f56b0f450a745bdbb47e42936a87fa7
CCC(C)C(=O)O.CCCCCCCCCCCOc1cnc(-c2ccc(O)cc2)nc1>>CCCCCCCCCCCOc1cnc(-c2ccc(OC(=O)[C@@H](C)CC)cc2)nc1
CC(C(=O)O)CC.C(CCCCCCCCCC)OC=1C=NC(=NC1)C1=CC=C(C=C1)O>>C(CCCCCCCCCC)OC=1C=NC(=NC1)C1=CC=C(C=C1)OC([C@H](CC)C)=O
O[C:22](=[O:23])[CH:24]([CH3:25])[CH2:26][CH3:27].[CH3:1][CH2:2][CH2:3][CH2:4][CH2:5][CH2:6][CH2:7][CH2:8][CH2:9][CH2:10][CH2:11][O:12][c:13]1[cH:14][n:15][c:16](-[c:17]2[cH:18][cH:19][c:20]([OH:21])[cH:28][cH:29]2)[n:30][cH:31]1>>[CH3:1][CH2:2][CH2:3][CH2:4][CH2:5][CH2:6][CH2:7][CH2:8][CH2:9][CH2:10][CH2:11][O:12][c:1...
CCC(C)C(=O)O.CCCCCCCCCCCOc1cnc(-c2ccc(O)cc2)nc1
CCCCCCCCCCCOc1cnc(-c2ccc(OC(=O)[C@@H](C)CC)cc2)nc1
null
CN(C1=CC=NC=C1)C
C(Cl)(Cl)Cl
Acylation
Mitsunobu esterification
f18451ac648b00cb7c6684a3e64bee855b0320c7eb0f62b757b29d5fb6745560
1489fe0065c6531b60fda87a3857d7da1cd21873868856f058c20706f927fa08
c1ccc(-c2ncccn2)cc1
O-[C;H0;D3;+0:1](=[O;D1;H0:2])-[CH;D3;+0:3](-[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@@H;D3;+0:3](-[C:5]-[C;D1;H3:6])-[C;H0;D3;+0:1](=[O;D1;H0:2])-[O;H0;D2;+0:7]-[c:8](:[c:9]):[c:10]
70
[{"value": 70.0, "product": "C(CCCCCCCCCC)OC=1C=NC(=NC1)C1=CC=C(C=C1)OC([C@H](CC)C)=O", "details": "PERCENTYIELD", "is_desired": false}]
null
null
null
null
Pour 0.328 g of 2-methylbutanoic acid synthesized from (s)-amylalcohol ([α]D23 -5.8° (neat)), 1.1 g of 4-(5-n-undecyloxy-2-pyrimidinyl)phenol, 8 ml of anhydrous chloroform and 0.662 g of 4-dimethylaminopyridine, S,S'-dicyclohexylcarbodimide into a 25 ml flask and allow to react for one whole day at room temperature. Af...
10.6084/m9.figshare.5104873.v1
null
Carboxylic acid.Aromatic alcohol
Ester
null
null
c1cncnc1.c1ccccc1
HO-
CN(C1=CC=NC=C1)C.C(Cl)(Cl)Cl
null
null
CCC(C)C(=O)O.CCCCCCCCCCCOc1cnc(-c2ccc(O)cc2)nc1>CN(C1=CC=NC=C1)C.C(Cl)(Cl)Cl>CCCCCCCCCCCOc1cnc(-c2ccc(OC(=O)[C@@H](C)CC)cc2)nc1
ord_dataset-01dbb772c5e249108f0b191ed17a2c0c
ord-8a8737a6ccae4f179fddb28772f1de1a
O=[N+]([O-])c1ccc(F)cc1.Oc1ccc(Cl)cc1F.Oc1ccc(Cl)cc1F>>COC(=O)C(C)Oc1ccc(Oc2ccc(Cl)cc2F)cc1
ClC1=CC(=C(C=C1)O)F.ClC1=C(C(=CC=C1)F)O.ClC1=C(C(=CC=C1)F)O.FC1=CC=C(C=C1)[N+](=O)[O-].ClC1=C(C(=C(C=C1)O)F)Cl.ClC1=CC(=C(C=C1)O)F.[Na+].[Cl-].[OH-].[Na+].C([O-])([O-])=O.[K+].[K+]>>COC(C(C)OC1=CC=C(C=C1)OC1=C(C=C(C=C1)Cl)F)=O
O=[N+]([O-])[c:5]1[cH:1][cH:21][c:11](F)[cH:10][cH:6]1.F[c:22]1cc(Cl)c[cH:9][c:8]1[OH:7].[OH:12][c:13]1[cH:14][cH:15][c:16]([Cl:17])[cH:18][c:19]1[F:20]>>[CH3:1][O:2][C:3](=[O:4])[CH:5]([CH3:6])[O:7][c:8]1[cH:9][cH:10][c:11]([O:12][c:13]2[cH:14][cH:15][c:16]([Cl:17])[cH:18][c:19]2[F:20])[cH:21][cH:22]1
O=[N+]([O-])c1ccc(F)cc1.Oc1ccc(Cl)cc1F.Oc1ccc(Cl)cc1F
COC(=O)C(C)Oc1ccc(Oc2ccc(Cl)cc2F)cc1
null
null
CS(=O)C
Acylation
OtherReaction
a776a8683d28654e58f45ae675e548b46d15281896074843aa88ca157abf261f
f349f833ad04cb89796cc34133cd7b9b734057215e1d693111caa205736c1542
c1ccc(Oc2ccccc2)cc1
Cl-c1:c:[cH;D2;+0:1]:[c:2](-[OH;D1;+0:3]):[c;H0;D3;+0:4](-F):c:1.F-[c;H0;D3;+0:5]1:[cH;D2;+0:6]:[cH;D2;+0:7]:[c;H0;D3;+0:8](-[N+](=O)-[O-]):[cH;D2;+0:9]:[cH;D2;+0:10]:1.[OH;D1;+0:11]-[c:12](:[c:13]):[c:14]>>[CH3;D1;+0:9]-[#8:15]-[C:16](=[O;D1;H0:17])-[CH;D3;+0:8](-[CH3;D1;+0:7])-[O;H0;D2;+0:3]-[c:2]1:[cH;D2;+0:4]:[cH;D...
null
[]
100
CELSIUS
30
MINUTE
To a stirred mixture of potassium carbonate (25.04 g; 0.18 mol) in DMSO (200 ml) under argon atmosphere was added an 8:2 mixture (25 g; 0.171 mol) (from Step 2A) of 4-chloro-2-fluorophenol (~20 g; 0.136 mol) and 2-chloro-6-fluorophenol (~5 g; 0.034 mol). To this mixture was added 4-fluoronitrobenzene (18.05 g; 0.128 mo...
10.6084/m9.figshare.5104873.v1
null
Aromatic halide.Aromatic halide.Aromatic halide.Nitro group.Aromatic alcohol.Aromatic alcohol
Ester.Ether.Ether
c1ccccc1.c1ccccc1
c1ccccc1
c1ccccc1.c1ccccc1
Other
CS(=O)C
100
0.5
O=[N+]([O-])c1ccc(F)cc1.Oc1ccc(Cl)cc1F.Oc1ccc(Cl)cc1F>CS(=O)C>COC(=O)C(C)Oc1ccc(Oc2ccc(Cl)cc2F)cc1
ord_dataset-01dbb772c5e249108f0b191ed17a2c0c
ord-1f1e5d760a08437fbcdac96714805542
COC(=O)C(C)Br.Oc1ccc(Oc2ccc(Br)cc2F)cc1>>COC(=O)C(C)Oc1ccc(Oc2ccc(Br)cc2F)cc1
O.BrC1=CC(=C(OC2=CC=C(C=C2)O)C=C1)F.BrC(C(=O)OC)C.C([O-])([O-])=O.[K+].[K+]>>COC(C(C)OC1=CC=C(C=C1)OC1=C(C=C(C=C1)Br)F)=O
Br[CH:5]([C:3]([O:2][CH3:1])=[O:4])[CH3:6].[OH:7][c:8]1[cH:9][cH:10][c:11]([O:12][c:13]2[cH:14][cH:15][c:16]([Br:17])[cH:18][c:19]2[F:20])[cH:21][cH:22]1>>[CH3:1][O:2][C:3](=[O:4])[CH:5]([CH3:6])[O:7][c:8]1[cH:9][cH:10][c:11]([O:12][c:13]2[cH:14][cH:15][c:16]([Br:17])[cH:18][c:19]2[F:20])[cH:21][cH:22]1
COC(=O)C(C)Br.Oc1ccc(Oc2ccc(Br)cc2F)cc1
COC(=O)C(C)Oc1ccc(Oc2ccc(Br)cc2F)cc1
null
null
CS(=O)C
Heteroatom Alkylation and Arylation
Williamson Ether Synthesis
a60236748d2543bdb97e5465447a595cd9bb5fef4e3fe96ed6af652af51cd157
94a54f0a6e629a85ca32b8fd3cf243ab64283e31ecfe8705ffe0df2304c488b4
c1ccc(Oc2ccccc2)cc1
Br-[CH;D3;+0:1](-[C;D1;H3:2])-[C:3](=[O;D1;H0:4])-[#8:5]-[C;D1;H3:6].[OH;D1;+0:7]-[c:8](:[c:9]):[c:10]>>[C;D1;H3:6]-[#8:5]-[C:3](=[O;D1;H0:4])-[CH;D3;+0:1](-[C;D1;H3:2])-[O;H0;D2;+0:7]-[c:8](:[c:9]):[c:10]
null
[]
null
null
18
HOUR
A mixture of the 4-(4-bromo-2-fluorophenoxy)phenol (5.66 g, 0.02 mol) from Step V, methyl 2-bromoproprionate (3.34 g, 0.02 mol) and potassium carbonate (3.06 g, 0.22 mol) in DMSO (30 ml) was stirred, under an atmosphere of nitrogen, at room temperature for 18 hours. The mixture was poured into water (300 ml), and the r...
10.6084/m9.figshare.5104873.v1
null
Secondary halide.Ester.Aromatic alcohol
Ester.Ether
null
null
c1ccccc1.c1ccccc1
HBr
CS(=O)C
null
18
COC(=O)C(C)Br.Oc1ccc(Oc2ccc(Br)cc2F)cc1>CS(=O)C>COC(=O)C(C)Oc1ccc(Oc2ccc(Br)cc2F)cc1
ord_dataset-01dbb772c5e249108f0b191ed17a2c0c
ord-0f78ba915f35468eaf7efcfa90a652a9
COC(=O)C(C)O.Oc1ccc(Oc2ccc(Br)cc2F)cc1>>COC(=O)C(C)Oc1ccc(Oc2ccc(Br)cc2F)cc1
CS(=O)(=O)[O-].C(C(O)C)(=O)OC.C([O-])([O-])=O.[K+].[K+].BrC1=CC(=C(OC2=CC=C(C=C2)O)C=C1)F>>COC(C(C)OC1=CC=C(C=C1)OC1=C(C=C(C=C1)Br)F)=O
O[CH:5]([C:3]([O:2][CH3:1])=[O:4])[CH3:6].[OH:7][c:8]1[cH:9][cH:10][c:11]([O:12][c:13]2[cH:14][cH:15][c:16]([Br:17])[cH:18][c:19]2[F:20])[cH:21][cH:22]1>>[CH3:1][O:2][C:3](=[O:4])[CH:5]([CH3:6])[O:7][c:8]1[cH:9][cH:10][c:11]([O:12][c:13]2[cH:14][cH:15][c:16]([Br:17])[cH:18][c:19]2[F:20])[cH:21][cH:22]1
COC(=O)C(C)O.Oc1ccc(Oc2ccc(Br)cc2F)cc1
COC(=O)C(C)Oc1ccc(Oc2ccc(Br)cc2F)cc1
null
null
CS(=O)C.O
Heteroatom Alkylation and Arylation
Mitsunobu aryl ether
dcfcc873dea6ee5e165c0ecd29b721f7fe5378b92b644a66f7b493dd677cb7f9
23ac5fc1d8cc7460c5f165241138db5f1d60f846b59bf6c4b239ddd29d58ddda
c1ccc(Oc2ccccc2)cc1
O-[CH;D3;+0:1](-[C;D1;H3:2])-[C:3](=[O;D1;H0:4])-[#8:5]-[C;D1;H3:6].[OH;D1;+0:7]-[c:8](:[c:9]):[c:10]>>[C;D1;H3:6]-[#8:5]-[C:3](=[O;D1;H0:4])-[CH;D3;+0:1](-[C;D1;H3:2])-[O;H0;D2;+0:7]-[c:8](:[c:9]):[c:10]
189.6
[{"value": 189.6, "product": "COC(C(C)OC1=CC=C(C=C1)OC1=C(C=C(C=C1)Br)F)=O", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
null
null
A mixture of the 4-(4-bromo-2-fluorophenoxy)phenol (2.83 g, 0.01 mol), the methanesulfonate of S methyl lactate (18.2 g, 0.01 mol), and potassium carbonate (1.67 g, 0.012 mol) in DMSO (70 ml) was stirred at room temperature for 40 hours, then poured into water (700 ml). The mixture was extracted with ether (2×200 ml). ...
10.6084/m9.figshare.5104873.v1
null
Ester.Secondary alcohol.Aromatic alcohol
Ester.Ether
null
null
c1ccccc1.c1ccccc1
HO-
CS(=O)C.O
null
null
COC(=O)C(C)O.Oc1ccc(Oc2ccc(Br)cc2F)cc1>CS(=O)C.O>COC(=O)C(C)Oc1ccc(Oc2ccc(Br)cc2F)cc1
ord_dataset-01dbb772c5e249108f0b191ed17a2c0c
ord-127bab2712c94c40b71146c91e151657
COC(=O)C(C)Oc1ccc(O)cc1.O=[N+]([O-])c1ccc(F)c(F)c1>>COC(=O)C(C)Oc1ccc(Oc2ccc([N+](=O)[O-])cc2F)cc1
FC=1C=C(C=CC1F)[N+](=O)[O-].OC1=CC=C(OC(C(=O)OC)C)C=C1.C([O-])([O-])=O.[K+].[K+]>>FC1=C(OC2=CC=C(OC(C(=O)OC)C)C=C2)C=CC(=C1)[N+](=O)[O-]
[CH3:1][O:2][C:3](=[O:4])[CH:5]([CH3:6])[O:7][c:8]1[cH:9][cH:10][c:11]([OH:12])[cH:23][cH:24]1.F[c:13]1[cH:14][cH:15][c:16]([N+:17](=[O:18])[O-:19])[cH:20][c:21]1[F:22]>>[CH3:1][O:2][C:3](=[O:4])[CH:5]([CH3:6])[O:7][c:8]1[cH:9][cH:10][c:11]([O:12][c:13]2[cH:14][cH:15][c:16]([N+:17](=[O:18])[O-:19])[cH:20][c:21]2[F:22])...
COC(=O)C(C)Oc1ccc(O)cc1.O=[N+]([O-])c1ccc(F)c(F)c1
COC(=O)C(C)Oc1ccc(Oc2ccc([N+](=O)[O-])cc2F)cc1
null
null
CS(=O)C
Heteroatom Alkylation and Arylation
Williamson Ether Synthesis
e4ea1e38252bc3b9c5ec04486386725e6570ab3860d45e337a1d131319bbf0fc
27e9a6bab4e3ed54aeb6be4d84cb1c0170208288795e252a46e57e44ecc064f0
c1ccc(Oc2ccccc2)cc1
F-[c;H0;D3;+0:1](:[c:2]:[c:3]):[c:4](-[F;D1;H0:5]):[c:6].[OH;D1;+0:7]-[c:8](:[c:9]):[c:10]>>[F;D1;H0:5]-[c:4](:[c:6]):[c;H0;D3;+0:1](-[O;H0;D2;+0:7]-[c:8](:[c:9]):[c:10]):[c:2]:[c:3]
98.2
[{"value": 98.0, "product": "FC1=C(OC2=CC=C(OC(C(=O)OC)C)C=C2)C=CC(=C1)[N+](=O)[O-]", "details": "PERCENTYIELD", "is_desired": false}, {"value": 98.2, "product": "FC1=C(OC2=CC=C(OC(C(=O)OC)C)C=C2)C=CC(=C1)[N+](=O)[O-]", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
null
null
A stirred mixture of 3,4-difluoronitrobenzene (13.5 g, 0.85 mol), methyl 2-(4-hydroxyphenoxy)propionate (23.1 g, 0.085 mol), and potassium carbonate (12.5 g, 0.09 mol) in DMSO (200 ml) was heated in an oil bath (120° bath temperature) for one hour. After cooling the reaction mixture was poured into ice water (1000 ml) ...
10.6084/m9.figshare.5104873.v1
null
Aromatic halide.Aromatic alcohol
Ether
c1ccccc1
c1ccccc1
c1ccccc1.c1ccccc1
HF
CS(=O)C
null
null
COC(=O)C(C)Oc1ccc(O)cc1.O=[N+]([O-])c1ccc(F)c(F)c1>CS(=O)C>COC(=O)C(C)Oc1ccc(Oc2ccc([N+](=O)[O-])cc2F)cc1
ord_dataset-01dbb772c5e249108f0b191ed17a2c0c
ord-53fcb22988bf4f00ace4b323695f617b
CCOC(=O)CCC(C)Br.Oc1ccc(Oc2ccc(Cl)cc2F)cc1>>CCOC(=O)CCC(C)Oc1ccc(Oc2ccc(Cl)cc2F)cc1
C1(=CC=CC=C1)O.Cl.[Br-].C([O-])([O-])=O.ClC1=CC(=C(OC2=CC=C(C=C2)O)C=C1)F.BrC(CCC(=O)OCC)C.C([O-])([O-])=O.[K+].[K+]>>ClC1=CC(=C(OC2=CC=C(OC(CCC(=O)OCC)C)C=C2)C=C1)F
Br[CH:8]([CH2:7][CH2:6][C:4]([O:3][CH2:2][CH3:1])=[O:5])[CH3:9].[OH:10][c:11]1[cH:12][cH:13][c:14]([O:15][c:16]2[cH:17][cH:18][c:19]([Cl:20])[cH:21][c:22]2[F:23])[cH:24][cH:25]1>>[CH3:1][CH2:2][O:3][C:4](=[O:5])[CH2:6][CH2:7][CH:8]([CH3:9])[O:10][c:11]1[cH:12][cH:13][c:14]([O:15][c:16]2[cH:17][cH:18][c:19]([Cl:20])[cH:...
CCOC(=O)CCC(C)Br.Oc1ccc(Oc2ccc(Cl)cc2F)cc1
CCOC(=O)CCC(C)Oc1ccc(Oc2ccc(Cl)cc2F)cc1
null
null
CN(C)C=O
Heteroatom Alkylation and Arylation
Williamson Ether Synthesis
bff4876be49b448135c783dd3eeeb68ab3cc5bdc91beadda8a9095106cd5c747
cf768afb66ed5041aefdce1fa6d1e40995a1ab7c4b4a4ca47544fe49ee1e629f
c1ccc(Oc2ccccc2)cc1
Br-[CH;D3;+0:1](-[C;D1;H3:2])-[C:3]-[C:4]-[C:5](-[#8:6])=[O;D1;H0:7].[OH;D1;+0:8]-[c:9](:[c:10]):[c:11]>>[#8:6]-[C:5](=[O;D1;H0:7])-[C:4]-[C:3]-[CH;D3;+0:1](-[C;D1;H3:2])-[O;H0;D2;+0:8]-[c:9](:[c:10]):[c:11]
null
[]
130
CELSIUS
null
null
A stirred mixture of 4-(4-chloro-2-fluorophenoxy)phenol (2.3 g, 0.0103 mol), ethyl 4-bromopentanoate (2.01 g, 0.0103 mol), and potassium carbonate (1.46 g, 0.105 mol) in DMF (20 ml) was heated in an oil bath at 130° C. for one hour. Additional bromide (0.5 g) and carbonate (0.5 g) were added each hour for the next four...
10.6084/m9.figshare.5104873.v1
null
Secondary halide.Aromatic alcohol
Ether
null
null
c1ccccc1.c1ccccc1
HBr
CN(C)C=O
130
null
CCOC(=O)CCC(C)Br.Oc1ccc(Oc2ccc(Cl)cc2F)cc1>CN(C)C=O>CCOC(=O)CCC(C)Oc1ccc(Oc2ccc(Cl)cc2F)cc1
ord_dataset-01dbb772c5e249108f0b191ed17a2c0c
ord-b5402a5a3ee14b03bfb946e023674692
COC(=O)C=C(OC)C(C)Br.Oc1ccc(Oc2ccc(Br)cc2F)cc1>>COC(=O)C=C(OC)C(C)Oc1ccc(Oc2ccc(Br)cc2F)cc1
BrC1=CC(=C(OC2=CC=C(C=C2)O)C=C1)F.BrC(C(=CC(=O)OC)OC)C.C([O-])([O-])=O.[K+].[K+].C(C)#N>>BrC1=CC(=C(OC2=CC=C(OC(C(=CC(=O)OC)OC)C)C=C2)C=C1)F
Br[CH:9]([C:6](=[CH:5][C:3]([O:2][CH3:1])=[O:4])[O:7][CH3:8])[CH3:10].[OH:11][c:12]1[cH:13][cH:14][c:15]([O:16][c:17]2[cH:18][cH:19][c:20]([Br:21])[cH:22][c:23]2[F:24])[cH:25][cH:26]1>>[CH3:1][O:2][C:3](=[O:4])[CH:5]=[C:6]([O:7][CH3:8])[CH:9]([CH3:10])[O:11][c:12]1[cH:13][cH:14][c:15]([O:16][c:17]2[cH:18][cH:19][c:20](...
COC(=O)C=C(OC)C(C)Br.Oc1ccc(Oc2ccc(Br)cc2F)cc1
COC(=O)C=C(OC)C(C)Oc1ccc(Oc2ccc(Br)cc2F)cc1
null
null
O
Heteroatom Alkylation and Arylation
Williamson Ether Synthesis
bff4876be49b448135c783dd3eeeb68ab3cc5bdc91beadda8a9095106cd5c747
cf768afb66ed5041aefdce1fa6d1e40995a1ab7c4b4a4ca47544fe49ee1e629f
c1ccc(Oc2ccccc2)cc1
Br-[CH;D3;+0:1](-[C;D1;H3:2])-[C:3](-[#8:4])=[C:5]-[C:6](-[#8:7])=[O;D1;H0:8].[OH;D1;+0:9]-[c:10](:[c:11]):[c:12]>>[#8:7]-[C:6](=[O;D1;H0:8])-[C:5]=[C:3](-[#8:4])-[CH;D3;+0:1](-[C;D1;H3:2])-[O;H0;D2;+0:9]-[c:10](:[c:11]):[c:12]
58.2
[{"value": 58.0, "product": "BrC1=CC(=C(OC2=CC=C(OC(C(=CC(=O)OC)OC)C)C=C2)C=C1)F", "details": "PERCENTYIELD", "is_desired": false}, {"value": 58.2, "product": "BrC1=CC(=C(OC2=CC=C(OC(C(=CC(=O)OC)OC)C)C=C2)C=C1)F", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
null
null
A mixture of 12.0 g (42.4 mmol) 4-(4-bromo-2-fluorophenoxy)phenol, 9.5 g (42.4 mmol) methyl 4-bromo-3-methoxy-2-pentenoate, 6.45 g (46.6 mmol) potassium carbonate and 180 ml acetonitrile was heated at reflux for 16 hours. The mixture was poured into water and extracted with ether. The combined ether extracts were washe...
10.6084/m9.figshare.5104873.v1
null
Secondary halide.Aromatic alcohol
Ether
null
null
c1ccccc1.c1ccccc1
HBr
O
null
null
COC(=O)C=C(OC)C(C)Br.Oc1ccc(Oc2ccc(Br)cc2F)cc1>O>COC(=O)C=C(OC)C(C)Oc1ccc(Oc2ccc(Br)cc2F)cc1
ord_dataset-01dbb772c5e249108f0b191ed17a2c0c
ord-06486a43573049c0972d0737d58446eb
COC(=O)C=C(OC)C(C)Oc1ccc(Oc2ccc(Br)cc2F)cc1>>COC(=CCO)C(C)Oc1ccc(Oc2ccc(Br)cc2F)cc1
C(C)(=O)O.CC(C)C[AlH]CC(C)C.BrC1=CC(=C(OC2=CC=C(OC(C(=CC(=O)OC)OC)C)C=C2)C=C1)F.CCOCC>>BrC1=CC(=C(OC2=CC=C(OC(C(=CCO)OC)C)C=C2)C=C1)F
CO[C:5]([CH:4]=[C:3]([O:2][CH3:1])[CH:7]([CH3:8])[O:9][c:10]1[cH:11][cH:12][c:13]([O:14][c:15]2[cH:16][cH:17][c:18]([Br:19])[cH:20][c:21]2[F:22])[cH:23][cH:24]1)=[O:6]>>[CH3:1][O:2][C:3](=[CH:4][CH2:5][OH:6])[CH:7]([CH3:8])[O:9][c:10]1[cH:11][cH:12][c:13]([O:14][c:15]2[cH:16][cH:17][c:18]([Br:19])[cH:20][c:21]2[F:22])[...
COC(=O)C=C(OC)C(C)Oc1ccc(Oc2ccc(Br)cc2F)cc1
COC(=CCO)C(C)Oc1ccc(Oc2ccc(Br)cc2F)cc1
null
null
C1(=CC=CC=C1)C.O
Reduction
Reduction of ester to primary alcohol
21d61543c6ec8a8cebe1b3ef55ef3dd20acbf79a4f1c12a7fb51e32be7a3248a
1fbcd628a0426673c5d10aa49a977cd2d1ae02a8cdf57bbb10d94aa03a94e937
c1ccc(Oc2ccccc2)cc1
C-O-[C;H0;D3;+0:1](=[O;H0;D1;+0:2])-[C:3]=[C:4](-[#8:5])-[C:6]>>[#8:5]-[C:4](-[C:6])=[C:3]-[CH2;D2;+0:1]-[OH;D1;+0:2]
74
[{"value": 74.0, "product": "BrC1=CC(=C(OC2=CC=C(OC(C(=CCO)OC)C)C=C2)C=C1)F", "details": "PERCENTYIELD", "is_desired": false}, {"value": 73.6, "product": "BrC1=CC(=C(OC2=CC=C(OC(C(=CCO)OC)C)C=C2)C=C1)F", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
-78
CELSIUS
2
HOUR
To a solution of 4.5 g (10.6 mmol) 4-(4-(4-bromo-2-fluorophenoxy)phenoxy)-3-methoxy-2-pentenoic acid, methyl ester in 25 ml toluene at -78° C. was added dropwise over a period of 30 min, 16.5 ml of 1.5M DIBAL-H in toluene, keeping the temperature below -60° C. The mixture was stirred for 21/2 hours at -78° C. To the mi...
10.6084/m9.figshare.5104873.v1
null
Ester
Primary alcohol
null
null
c1ccccc1.c1ccccc1
Other
C1(=CC=CC=C1)C.O
-78
2
COC(=O)C=C(OC)C(C)Oc1ccc(Oc2ccc(Br)cc2F)cc1>C1(=CC=CC=C1)C.O>COC(=CCO)C(C)Oc1ccc(Oc2ccc(Br)cc2F)cc1
ord_dataset-01dbb772c5e249108f0b191ed17a2c0c
ord-fd27dcb7b04c492084da2155de44a546
COC(=CCO)C(C)Oc1ccc(Oc2ccc(Br)cc2F)cc1>>C=CC(=O)C(C)Oc1ccc(Oc2ccc(Br)cc2F)cc1
BrC1=CC(=C(OC2=CC=C(OC(C(=CCO)OC)C)C=C2)C=C1)F.O>>BrC1=CC(=C(OC2=CC=C(OC(C(C=C)=O)C)C=C2)C=C1)F
C[O:4][C:3](=[CH:2][CH2:1]O)[CH:5]([CH3:6])[O:7][c:8]1[cH:9][cH:10][c:11]([O:12][c:13]2[cH:14][cH:15][c:16]([Br:17])[cH:18][c:19]2[F:20])[cH:21][cH:22]1>>[CH2:1]=[CH:2][C:3](=[O:4])[CH:5]([CH3:6])[O:7][c:8]1[cH:9][cH:10][c:11]([O:12][c:13]2[cH:14][cH:15][c:16]([Br:17])[cH:18][c:19]2[F:20])[cH:21][cH:22]1
COC(=CCO)C(C)Oc1ccc(Oc2ccc(Br)cc2F)cc1
C=CC(=O)C(C)Oc1ccc(Oc2ccc(Br)cc2F)cc1
null
null
C(Cl)Cl
Miscellaneous
OtherReaction
a8d662f969f46443ee3d205eeaa2aad04bcbbc6b5518b3c0c35fba920e940fa2
95556fd158731d9953abb86a3541dbd9e9215d18e7d86c5830e4933fdf09f92c
c1ccc(Oc2ccccc2)cc1
C-[O;H0;D2;+0:1]-[C;H0;D3;+0:2](=[CH;D2;+0:3]-[CH2;D2;+0:4]-O)-[C:5](-[#8:6])-[C;D1;H3:7]>>[#8:6]-[C:5](-[C;D1;H3:7])-[C;H0;D3;+0:2](=[O;H0;D1;+0:1])-[CH;D2;+0:3]=[CH2;D1;+0:4]
69
[{"value": 69.0, "product": "BrC1=CC(=C(OC2=CC=C(OC(C(C=C)=O)C)C=C2)C=C1)F", "details": "PERCENTYIELD", "is_desired": false}, {"value": 68.9, "product": "BrC1=CC(=C(OC2=CC=C(OC(C(C=C)=O)C)C=C2)C=C1)F", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
0
CELSIUS
45
MINUTE
To a solution of 30 ml of 35% HClO4 and 15 ml CH2Cl2 at 0° C. was added 3.0 g (7.55 mmol) 4-(4-(4-bromo-2-fluorophenoxy)phenoxy)-3-methoxy-2-penten-1-ol in 15 ml CH2Cl2. The mixture was stirred at 0° C. for 45 min, then poured into water and extracted with ether. The combined ether extracts were washed with water, drie...
10.6084/m9.figshare.5104873.v1
null
Ether.Primary alcohol
Ketone.Vinyl
null
null
c1ccccc1.c1ccccc1
HO-
C(Cl)Cl
0
0.75
COC(=CCO)C(C)Oc1ccc(Oc2ccc(Br)cc2F)cc1>C(Cl)Cl>C=CC(=O)C(C)Oc1ccc(Oc2ccc(Br)cc2F)cc1
ord_dataset-01dbb772c5e249108f0b191ed17a2c0c
ord-0e96676273d2437282408c24a90f4b9f
CC(=O)CC(C)=O.CC(Oc1ccc(Oc2ccc(Br)cc2F)cc1)C(=O)Cl>>CC(=O)C(C(C)=O)C(=O)C(C)Oc1ccc(Oc2ccc(Br)cc2F)cc1
BrC1=CC(=C(OC2=CC=C(OC(C(=O)Cl)C)C=C2)C=C1)F.CC(CC(C)=O)=O.C1=CC=CC=C1.[Na]>>C(C)(=O)C(C(C)=O)C(C(C)OC1=CC=C(C=C1)OC1=C(C=C(C=C1)Br)F)=O
[CH3:1][C:2](=[O:3])[CH2:4][C:5]([CH3:6])=[O:7].Cl[C:8](=[O:9])[CH:10]([CH3:11])[O:12][c:13]1[cH:14][cH:15][c:16]([O:17][c:18]2[cH:19][cH:20][c:21]([Br:22])[cH:23][c:24]2[F:25])[cH:26][cH:27]1>>[CH3:1][C:2](=[O:3])[CH:4]([C:5]([CH3:6])=[O:7])[C:8](=[O:9])[CH:10]([CH3:11])[O:12][c:13]1[cH:14][cH:15][c:16]([O:17][c:18]2[...
CC(=O)CC(C)=O.CC(Oc1ccc(Oc2ccc(Br)cc2F)cc1)C(=O)Cl
CC(=O)C(C(C)=O)C(=O)C(C)Oc1ccc(Oc2ccc(Br)cc2F)cc1
null
null
CCOCC.O
C-C Coupling
OtherReaction
526e6fbc0e961d2a07a8bee2a7a532eb48246fde37e16e5fd7c1b5060d3c2076
d1ef8d6a572be6944eed6d1e50ba23f9d6e95602669b67dac90442aed5304e90
c1ccc(Oc2ccccc2)cc1
Cl-[C;H0;D3;+0:1](=[O;D1;H0:2])-[C:3](-[#8:4])-[C;D1;H3:5].[C;D1;H3:6]-[C:7](=[O;D1;H0:8])-[CH2;D2;+0:9]-[C:10](-[C;D1;H3:11])=[O;D1;H0:12]>>[#8:4]-[C:3](-[C;D1;H3:5])-[C;H0;D3;+0:1](=[O;D1;H0:2])-[CH;D3;+0:9](-[C:7](-[C;D1;H3:6])=[O;D1;H0:8])-[C:10](-[C;D1;H3:11])=[O;D1;H0:12]
16
[{"value": 16.0, "product": "C(C)(=O)C(C(C)=O)C(C(C)OC1=CC=C(C=C1)OC1=C(C=C(C=C1)Br)F)=O", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
8
HOUR
A mixture of 1.7 g (17 mmol) of 2,4-pentanedione, 30 ml of benzene and 0.26 g (11.3 mmol) of sodium was warmed at reflux for 3 hours. The reaction mixture was cooled to room temperature and a solution of 10 mmol of 2-(4-(4-bromo-2-fluorophenoxy)phenoxy)propanoyl chloride was added dropwise. The resulting mixture was wa...
10.6084/m9.figshare.5104873.v1
null
Acyl halide.Ketone.Ketone
Ketone.Ketone.Ketone
null
null
c1ccccc1.c1ccccc1
HCl
CCOCC.O
null
8
CC(=O)CC(C)=O.CC(Oc1ccc(Oc2ccc(Br)cc2F)cc1)C(=O)Cl>CCOCC.O>CC(=O)C(C(C)=O)C(=O)C(C)Oc1ccc(Oc2ccc(Br)cc2F)cc1
ord_dataset-01dbb772c5e249108f0b191ed17a2c0c
ord-203e66a3104e4a1aa4c270e295862ca4
CC(C=O)Oc1ccc(Oc2ccc(Br)cc2F)cc1.CCOC(C)=O>>CCOC(=O)CC(O)C(C)Oc1ccc(Oc2ccc(Br)cc2F)cc1
C(CCC)[Li].BrC1=CC(=C(OC2=CC=C(OC(C=O)C)C=C2)C=C1)F.C(C)(C)NC(C)C.C(C)(=O)OCC.[NH4+].[Cl-]>>C(C)OC(CC(C(C)OC1=CC=C(C=C1)OC1=C(C=C(C=C1)Br)F)O)=O
[CH:7](=[O:8])[CH:9]([CH3:10])[O:11][c:12]1[cH:13][cH:14][c:15]([O:16][c:17]2[cH:18][cH:19][c:20]([Br:21])[cH:22][c:23]2[F:24])[cH:25][cH:26]1.[CH3:1][CH2:2][O:3][C:4](=[O:5])[CH3:6]>>[CH3:1][CH2:2][O:3][C:4](=[O:5])[CH2:6][CH:7]([OH:8])[CH:9]([CH3:10])[O:11][c:12]1[cH:13][cH:14][c:15]([O:16][c:17]2[cH:18][cH:19][c:20]...
CC(C=O)Oc1ccc(Oc2ccc(Br)cc2F)cc1.CCOC(C)=O
CCOC(=O)CC(O)C(C)Oc1ccc(Oc2ccc(Br)cc2F)cc1
null
null
CCCCCC.CCOCC
C-C Coupling
OtherReaction
5c727118385c562f285df4622fd28beee54f2a6dc613daeca0713283cec89087
12ce375342f37362e14813852abaca485261821306a77d2d6bbedf8a6a5866f3
c1ccc(Oc2ccccc2)cc1
[#8:1]-[C:2](-[C;D1;H3:3])-[CH;D2;+0:4]=[O;H0;D1;+0:5].[C:6]-[#8:7]-[C:8](-[CH3;D1;+0:9])=[O;D1;H0:10]>>[#8:1]-[C:2](-[C;D1;H3:3])-[CH;D3;+0:4](-[OH;D1;+0:5])-[CH2;D2;+0:9]-[C:8](=[O;D1;H0:10])-[#8:7]-[C:6]
70
[{"value": 70.0, "product": "C(C)OC(CC(C(C)OC1=CC=C(C=C1)OC1=C(C=C(C=C1)Br)F)O)=O", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
15
MINUTE
A solution of 1.54 ml (11 mmol) of diisopropylamine in 20 ml of ether was cooled under N2 to -78° C. and 6.9 ml (11 mmol) of 1.6M n-butyllithium in hexane was slowly added. After 15 min of -78° C. 0.97 g (11 mmol) of ethyl acetate in 3 ml of ether was added dropwise. The resulting mixture was stirred at -78° C. for 15 ...
10.6084/m9.figshare.5104873.v1
null
Aldehyde.Ester
Ester.Secondary alcohol
null
null
c1ccccc1.c1ccccc1
null
CCCCCC.CCOCC
null
0.25
CC(C=O)Oc1ccc(Oc2ccc(Br)cc2F)cc1.CCOC(C)=O>CCCCCC.CCOCC>CCOC(=O)CC(O)C(C)Oc1ccc(Oc2ccc(Br)cc2F)cc1
ord_dataset-01dbb772c5e249108f0b191ed17a2c0c
ord-fb27c21061f54078be4fc125c2783746
O=C1Cc2c(Cl)ccc(Cl)c2N1.O=C1Cc2cccc(C3CC3)c2N1>>O=C1Cc2ccc(Cl)cc2N1
C1(CC1)C=1C=CC=C2CC(NC12)=O.FC1=C2CC(NC2=CC(=C1)F)=O.BrC=1C=CC=C2CC(NC12)=O.CC=1C=CC=C2CC(NC12)=O.ClC1=C2CC(NC2=C(C=C1)Cl)=O.FC=1C=C2CC(NC2=C(C1)F)=O.C1(CCCCC1)C=1C=CC=C2CC(NC12)=O.FC=1C=CC=C2CC(NC12)=O.C(CCC)C=1C=C2CC(NC2=C(C1)F)=O>>ClC1=CC=C2CC(NC2=C1)=O
O=C1C[c:10]2[c:4](Cl)[cH:5][cH:6][c:7]([Cl:8])[c:9]2N1.c1cc(C2CC2)c2c(c1)[CH2:3][C:2](=[O:1])[NH:11]2>>[O:1]=[C:2]1[CH2:3][c:4]2[cH:5][cH:6][c:7]([Cl:8])[cH:9][c:10]2[NH:11]1
O=C1Cc2c(Cl)ccc(Cl)c2N1.O=C1Cc2cccc(C3CC3)c2N1
O=C1Cc2ccc(Cl)cc2N1
null
null
null
Heteroatom Alkylation and Arylation
OtherReaction
38442a974c2a8dde1e00166c906a36ef22d9d4944d31152b70b4b12c04f86abf
7f6fbbbe780e833dd4ad214bddfac885434f3ca11622b2c0bf81fe85651fcf44
O=C1Cc2ccccc2N1
Cl-[c;H0;D3;+0:1]1:[c:2]:[c:3]:[c:4](-[Cl;D1;H0:5]):[c;H0;D3;+0:6]2:[c;H0;D3;+0:7]:1-C-C(=O)-N-2.[O;D1;H0:8]=[C:9]1-[CH2;D2;+0:10]-c2:c:c:c:c(-C3-C-C-3):c:2-[NH;D2;+0:11]-1>>[Cl;D1;H0:5]-[c:4]1:[c:3]:[c:2]:[c;H0;D3;+0:1]2:[c;H0;D3;+0:7](:[cH;D2;+0:6]:1)-[NH;D2;+0:11]-[C:9](=[O;D1;H0:8])-[CH2;D2;+0:10]-2
null
[]
null
null
null
null
In an analogous manner 4- and 6-fluoro- and bromooxindoles are prepared, as well as 7-fluorooxindole, 7-bromooxindole, 7-methyloxindole, 4,6-difluorooxindole, 4,7-dichlorooxindole, 5,7-difluorooxindole, 5-n-butyl-7-fluorooxindole, 7-cyclohexyloxindole and 7-cyclopropyloxindole. Conditions: See reaction.notes.procedure_...
10.6084/m9.figshare.5104873.v1
null
Aromatic halide.Secondary amide.Secondary amide
Secondary amide
c1ccc2c(c1)CCN2.C1CC1.c1ccc2c(c1)CCN2
c1ccc2c(c1)CCN2
c1ccc2c(c1)CCN2
HCl
null
null
null
O=C1Cc2c(Cl)ccc(Cl)c2N1.O=C1Cc2cccc(C3CC3)c2N1>>O=C1Cc2ccc(Cl)cc2N1
ord_dataset-01dbb772c5e249108f0b191ed17a2c0c
ord-67d46a104ad240b9a00c308bf07eb4cb
Nc1ccc(F)c(Cl)c1.O=C(Cl)CCl>>O=C(CCl)Nc1ccc(F)c(Cl)c1
ClC=1C=C(N)C=CC1F.N1=CC=CC=C1.ClCC(=O)Cl>>ClCC(=O)NC1=CC(=C(C=C1)F)Cl
[NH2:5][c:6]1[cH:7][cH:8][c:9]([F:10])[c:11]([Cl:12])[cH:13]1.Cl[C:2](=[O:1])[CH2:3][Cl:4]>>[O:1]=[C:2]([CH2:3][Cl:4])[NH:5][c:6]1[cH:7][cH:8][c:9]([F:10])[c:11]([Cl:12])[cH:13]1
Nc1ccc(F)c(Cl)c1.O=C(Cl)CCl
O=C(CCl)Nc1ccc(F)c(Cl)c1
null
null
C1(=CC=CC=C1)C
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]-[Cl;D1;H0:4].[NH2;D1;+0:5]-[c:6](:[c:7]):[c:8]>>[Cl;D1;H0:4]-[C:3]-[C;H0;D3;+0:1](=[O;D1;H0:2])-[NH;D2;+0:5]-[c:6](:[c:7]):[c:8]
88
[{"value": 88.0, "product": "ClCC(=O)NC1=CC(=C(C=C1)F)Cl", "details": "PERCENTYIELD", "is_desired": false}]
null
null
null
null
To 130 ml. of toluene was added, with stirring, 24.0 g. (0.165 mole) of 3-chloro-4-fluoroaniline and 13.5 ml. (0.166 mole) of pyridine. The resulting solution was cooled to ca 0° C. and 13.2 ml. (0.166 mole) of 2-chloroacetyl chloride was added. The reaction mixture was stirred at room temperature for 5 hours and then ...
10.6084/m9.figshare.5104873.v1
null
Acyl halide.Primary amine
Secondary amide
null
null
c1ccccc1
HCl
C1(=CC=CC=C1)C
null
null
Nc1ccc(F)c(Cl)c1.O=C(Cl)CCl>C1(=CC=CC=C1)C>O=C(CCl)Nc1ccc(F)c(Cl)c1
ord_dataset-01dbb772c5e249108f0b191ed17a2c0c
ord-648f109ece9742c68f0c921925e57cde
O=C(CCl)Nc1ccc(F)c(Cl)c1>>O=C1Cc2cc(F)c(Cl)cc2N1
ClCC(=O)NC1=CC(=C(C=C1)F)Cl.[Cl-].[Al+3].[Cl-].[Cl-].Cl>>ClC1=C(C=C2CC(NC2=C1)=O)F
Cl[CH2:3][C:2](=[O:1])[NH:12][c:11]1[cH:4][cH:5][c:6]([F:7])[c:8]([Cl:9])[cH:10]1>>[O:1]=[C:2]1[CH2:3][c:4]2[cH:5][c:6]([F:7])[c:8]([Cl:9])[cH:10][c:11]2[NH:12]1
O=C(CCl)Nc1ccc(F)c(Cl)c1
O=C1Cc2cc(F)c(Cl)cc2N1
null
null
null
Functional Group Interconversion
OtherReaction
6ab2dca96c05f47f8dd3d6dbe49c7d399a1afbe6dfa21b42d4808f5071f12d2d
47a659f5704a5b7ca1b92ff731f18f109c6bde1d45152a3a393eefbd10265508
O=C1Cc2ccccc2N1
Cl-[CH2;D2;+0:1]-[C:2](=[O;D1;H0:3])-[#7:4]-[c:5](:[c:6]):[cH;D2;+0:7]:[c:8]:[c:9]>>[O;D1;H0:3]=[C:2]1-[#7:4]-[c:5](:[c:6]):[c;H0;D3;+0:7](:[c:8]:[c:9])-[CH2;D2;+0:1]-1
7
[{"value": 7.0, "product": "ClC1=C(C=C2CC(NC2=C1)=O)F", "details": "PERCENTYIELD", "is_desired": false}]
null
null
30
MINUTE
A 26.63 g. sample of the N-(2-chloro)-2-chloro-4-fluoroaniline was thoroughly mixed with 64 g. of anhydrous aluminum chloride, and the mixture was heated at 210°-230° C. for 8.5 hours. The reaction mixture was then poured onto a mixture of ice an 1N hydrochloric acid, with stirring. Stirring was continued for 30 minute...
10.6084/m9.figshare.5104873.v1
null
Primary halide
null
c1ccccc1
c1ccc2c(c1)CCN2
c1ccc2c(c1)CCN2
HCl
null
null
0.5
O=C(CCl)Nc1ccc(F)c(Cl)c1>>O=C1Cc2cc(F)c(Cl)cc2N1
ord_dataset-01dbb772c5e249108f0b191ed17a2c0c
ord-348a42addcd841a49c39a0b63d7106f4
CCCCSc1ccccc1N.CCCSc1ccc(N)cc1.CSc1ccccc1N>>CCCc1ccc2c(c1)CC(=S)N2.Cc1ccc2c(c1)NC(=S)C2.Cc1cccc2c1CC(=S)N2
CSC1=C(N)C=CC=C1.C(CC)SC1=CC=C(N)C=C1.C(CCC)SC1=C(N)C=CC=C1>>CC1=C2CC(NC2=CC=C1)=S.CC1=CC=C2CC(NC2=C1)=S.C(CC)C=1C=C2CC(NC2=CC1)=S
[cH:10]1[cH:24][cH:18][c:19]([NH2:21])[c:33]([S:34][CH2:25][CH2:16][CH2:15][CH3:14])[cH:32]1.[CH3:1][CH2:2][CH2:3][S:23][c:4]1[cH:5][cH:6][c:7]([NH2:13])[cH:8][cH:9]1.[CH3:11][S:12][c:31]1[cH:26][cH:27][cH:28][cH:29][c:30]1[NH2:35]>>[CH3:1][CH2:2][CH2:3][c:4]1[cH:5][cH:6][c:7]2[c:8]([cH:9]1)[CH2:10][C:11](=[S:12])[NH:1...
CCCCSc1ccccc1N.CCCSc1ccc(N)cc1.CSc1ccccc1N
CCCc1ccc2c(c1)CC(=S)N2.Cc1ccc2c(c1)NC(=S)C2.Cc1cccc2c1CC(=S)N2
null
null
null
Aromatic Heterocycle Formation
OtherReaction
7c0dcff1756dfc92577737d78827fbdb376e698d49d0dfda48e52fca279b70f5
4ba752877779407744016dfe5be9631931f40aaab046b94ef6e460c33a3cd11d
S=C1Cc2ccccc2N1.S=C1Cc2ccccc2N1.S=C1Cc2ccccc2N1
[C;D1;H3:1]-[CH2;D2;+0:2]-[CH2;D2;+0:3]-[CH2;D2;+0:4]-[S;H0;D2;+0:5]-[c;H0;D3;+0:6]1:[cH;D2;+0:7]:[cH;D2;+0:8]:[cH;D2;+0:9]:[cH;D2;+0:10]:[c;H0;D3;+0:11]:1-[NH2;D1;+0:12].[C;D1;H3:13]-[C:14]-[CH2;D2;+0:15]-[S;H0;D2;+0:16]-[c;H0;D3;+0:17]1:[c:18]:[c:19]:[c:20](-[NH2;D1;+0:21]):[cH;D2;+0:22]:[c:23]:1.[CH3;D1;+0:24]-[S;H0...
null
[]
null
null
null
null
4-Methylthiooxindole and 6-methylthiooxindole are prepared according to the procedure of U.S. Pat. No. 4,006,161. 7-Methylthio and 7-n-butylthiooxindoles are prepared by using the same procedure starting with 2-methylthioaniline and 2-n-butylthioaniline, respectively. 5-n-Propylthiooxindole is prepared by the same synt...
10.6084/m9.figshare.5104873.v1
null
Primary amine.Primary amine.Primary amine.Monosulfide.Monosulfide.Monosulfide
Thioamide.Thioamide.Thioamide
c1ccccc1.c1ccccc1.c1ccccc1
c1ccc2c(c1)CCN2.c1ccc2c(c1)CCN2.c1ccc2c(c1)CCN2
c1ccc2c(c1)CCN2.c1ccc2c(c1)CCN2.c1ccc2c(c1)CCN2
Other
null
null
null
CCCCSc1ccccc1N.CCCSc1ccc(N)cc1.CSc1ccccc1N>>CCCc1ccc2c(c1)CC(=S)N2.Cc1ccc2c(c1)NC(=S)C2.Cc1cccc2c1CC(=S)N2
ord_dataset-01dbb772c5e249108f0b191ed17a2c0c
ord-c0dad1d0d168495ea764fd1fd6e209c1
CCOC(=O)CC(=O)OCC.O=C(c1ccccc1)c1ccc(Cl)c([N+](=O)[O-])c1>>CCOC(=O)C(C(=O)OCC)c1ccc(C(=O)c2ccccc2)cc1[N+](=O)[O-]
ClC1=C(C=C(C(=O)C2=CC=CC=C2)C=C1)[N+](=O)[O-].[Na].C(C)O.C(CC(=O)OCC)(=O)OCC>>[N+](=O)([O-])C1=C(C=CC(=C1)C(C1=CC=CC=C1)=O)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].Cl[c:12]1[cH:13][cH:14][c:15]([C:16](=[O:17])[c:18]2[cH:19][cH:20][cH:21][cH:22][cH:23]2)[cH:24][c:25]1[N+:26](=[O:27])[O-:28]>>[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][c:15]([C:16](=[O:17])[...
CCOC(=O)CC(=O)OCC.O=C(c1ccccc1)c1ccc(Cl)c([N+](=O)[O-])c1
CCOC(=O)C(C(=O)OCC)c1ccc(C(=O)c2ccccc2)cc1[N+](=O)[O-]
null
null
C(Cl)Cl
C-C Coupling
Hurtley reaction
5a1171068c2a10d196160f01101b1c97354196d6923cfc455c6b686284d6c6f2
c0fb657475d92a5e1ab643a3f03921ebe4d047c8d805f98b012a5df3f9fb1f6c
O=C(c1ccccc1)c1ccccc1
Cl-[c;H0;D3;+0:1](:[c:2]:[c:3]):[c:4](-[#7;+:5]):[c:6].[C:7]-[#8:8]-[C:9](=[O;D1;H0:10])-[CH2;D2;+0:11]-[C:12](=[O;D1;H0:13])-[#8:14]-[C:15]>>[#7;+:5]-[c:4](:[c:6]):[c;H0;D3;+0:1](-[CH;D3;+0:11](-[C:12](=[O;D1;H0:13])-[#8:14]-[C:15])-[C:9](=[O;D1;H0:10])-[#8:8]-[C:7]):[c:2]:[c:3]
null
[]
null
null
2
HOUR
To a solution of sodium ethoxide, formed by reacting 4.6 g. (0.2 mole) of sodium metal with 200 ml. of ethanol, at 0° C. was added 32 g. (0.2 mole) of diethyl malonate followed by 26.1 g. (0.1 mole) of 4-chloro-3-nitrobenzophenone. The mixture was allowed to stir at room temperature for 2 hours and was then poured into...
10.6084/m9.figshare.5104873.v1
null
Aromatic halide.Ester.Ester
Ester.Ester
c1ccccc1
c1ccccc1
c1ccccc1.c1ccccc1
HCl
C(Cl)Cl
null
2
CCOC(=O)CC(=O)OCC.O=C(c1ccccc1)c1ccc(Cl)c([N+](=O)[O-])c1>C(Cl)Cl>CCOC(=O)C(C(=O)OCC)c1ccc(C(=O)c2ccccc2)cc1[N+](=O)[O-]
ord_dataset-01dbb772c5e249108f0b191ed17a2c0c
ord-92c9585a51c84d6bac68d122a75409e7
CCOC(=O)Cl.O=C(O)Cc1ccc(C(=O)c2ccccc2)cc1[N+](=O)[O-]>>CCOC(=O)Cc1ccc(C(=O)c2ccccc2)cc1[N+](=O)[O-]
[N+](=O)([O-])C1=C(C=CC(=C1)C(C1=CC=CC=C1)=O)CC(=O)O.C(C)N(CC)CC.C(C)OC(=O)Cl.COCCOC>>[N+](=O)([O-])C1=C(C=CC(=C1)C(C1=CC=CC=C1)=O)CC(=O)OCC
O=C(Cl)O[CH2:2][CH3:1].[OH:3][C:4](=[O:5])[CH2:6][c:7]1[cH:8][cH:9][c:10]([C:11](=[O:12])[c:13]2[cH:14][cH:15][cH:16][cH:17][cH:18]2)[cH:19][c:20]1[N+:21](=[O:22])[O-:23]>>[CH3:1][CH2:2][O:3][C:4](=[O:5])[CH2:6][c:7]1[cH:8][cH:9][c:10]([C:11](=[O:12])[c:13]2[cH:14][cH:15][cH:16][cH:17][cH:18]2)[cH:19][c:20]1[N+:21](=[O...
CCOC(=O)Cl.O=C(O)Cc1ccc(C(=O)c2ccccc2)cc1[N+](=O)[O-]
CCOC(=O)Cc1ccc(C(=O)c2ccccc2)cc1[N+](=O)[O-]
null
null
C(C)O.[Cl-].[Na+].O.C(C)OCC
Heteroatom Alkylation and Arylation
Ketonization by decarboxylation of acid halides
206d5ec09ce643b803adbcf860b4078b98a030d6380c33850f0abd3ec7da7984
8388f1b1aad516c0093910cf7e0a1fba12f038b873168f29f87df716614f8df9
O=C(c1ccccc1)c1ccccc1
Cl-C(=O)-O-[CH2;D2;+0:1]-[C;D1;H3:2].[C:3]-[C:4](=[O;D1;H0:5])-[OH;D1;+0:6]>>[C:3]-[C:4](=[O;D1;H0:5])-[O;H0;D2;+0:6]-[CH2;D2;+0:1]-[C;D1;H3:2]
94
[{"value": 94.0, "product": "[N+](=O)([O-])C1=C(C=CC(=C1)C(C1=CC=CC=C1)=O)CC(=O)OCC", "details": "PERCENTYIELD", "is_desired": false}]
10
CELSIUS
5
MINUTE
To a solution of 13.8 g. (48.4 mmoles) of 2-nitro-4-benzoylphenylacetic acid in 150 ml. of 1,2-dimethoxyethane at 15° C. was added 5.87 g. (58.1 mmole) of triethylamine. After 5 minutes 5.75 g. (53.2 mmoles) of ethylchloroformate was added and the reaction mixture allowed to stir at 10° C. for 15 minutes. Ethanol (15 m...
10.6084/m9.figshare.5104873.v1
null
Acyl halide.Carboxylic acid.Ether
Ester
null
null
c1ccccc1.c1ccccc1
HCl
C(C)O.[Cl-].[Na+].O.C(C)OCC
10
0.083333
CCOC(=O)Cl.O=C(O)Cc1ccc(C(=O)c2ccccc2)cc1[N+](=O)[O-]>C(C)O.[Cl-].[Na+].O.C(C)OCC>CCOC(=O)Cc1ccc(C(=O)c2ccccc2)cc1[N+](=O)[O-]
ord_dataset-01dbb772c5e249108f0b191ed17a2c0c
ord-d6c2eca3969d4ba2a9cdbb8916d07d20
O=C1Cc2c(Cl)cc(C(=O)c3ccccc3)cc2N1.O=C1Cc2ccc(C(=O)c3cccs3)cc2N1>>O=C1Cc2ccc(C(=O)c3ccccc3)cc2N1
FC1=C2CC(NC2=CC(=C1)C(C1=CC=CS1)=O)=O.COC1=C2CC(NC2=CC(=C1)C(CCC)=O)=O.FC1=C2CC(NC2=CC(=C1)C(C)=O)=O.COC1=C2CC(NC2=CC(=C1)C(C1=CC=CC=C1)=O)=O.C1(=CC=CS1)C(=O)C1=CC=C2CC(NC2=C1)=O.C1=C(C=CS1)C(=O)C1=CC=C2CC(NC2=C1)=O.CSC1=C2CC(NC2=CC(=C1)C(C1=CSC=C1)=O)=O.ClC1=C2CC(NC2=CC(=C1)C(C1=CC=CC=C1)=O)=O.CC1=C2CC(NC2=CC(=C1)C(C1...
O=C1Cc2c(Cl)cc(C(=O)c3ccc[cH:14][cH:15]3)cc2N1.s1[c:10]([C:8]([c:7]2[cH:6][cH:5][c:4]3[c:17]([cH:16]2)[NH:18][C:2](=[O:1])[CH2:3]3)=[O:9])[cH:11][cH:12][cH:13]1>>[O:1]=[C:2]1[CH2:3][c:4]2[cH:5][cH:6][c:7]([C:8](=[O:9])[c:10]3[cH:11][cH:12][cH:13][cH:14][cH:15]3)[cH:16][c:17]2[NH:18]1
O=C1Cc2c(Cl)cc(C(=O)c3ccccc3)cc2N1.O=C1Cc2ccc(C(=O)c3cccs3)cc2N1
O=C1Cc2ccc(C(=O)c3ccccc3)cc2N1
null
null
null
Miscellaneous
OtherReaction
b450880ff2b4862bba190acb50f208aa2d2315208774d09403a40c74b6f7d837
b99847263aa84a8ee29c980928e1cf548cef4019e6c4f5aef7c5ee3f85cfd3d3
O=C1Cc2ccc(C(=O)c3ccccc3)cc2N1
Cl-c1:c:c(-C(=O)-c2:[cH;D2;+0:1]:[cH;D2;+0:2]:c:c:c:2):c:c2:c:1-C-C(=O)-N-2.[O;D1;H0:3]=[C:4](-[c:5])-[c;H0;D3;+0:6]1:[c:7]:[c:8]:[cH;D2;+0:9]:s:1>>[O;D1;H0:3]=[C:4](-[c:5])-[c;H0;D3;+0:6]1:[c:7]:[c:8]:[cH;D2;+0:9]:[cH;D2;+0:2]:[cH;D2;+0:1]:1
null
[]
null
null
null
null
In a similar manner, starting with the appropriate reagent 6-n-butyryloxindole, 4-chloro-6-benzoyloxindole, 4-fluoro-6-acetyloxindole, 4-methoxy-6-benzoyloxindole, 4-methoxy-6-butyryloxindole, 6-(2-thenoyl)oxindole, 6-(3-thenoyl)oxindole, 4-methyl-6-(2-thenoyl)oxindole, 4-methylthio-6-(3-thenoyl)oxindole and 4-fluoro-6...
10.6084/m9.figshare.5104873.v1
null
Aromatic halide.Ketone.Ketone.Secondary amide
Ketone
c1ccc2c(c1)CCN2.c1ccccc1.c1ccsc1
c1ccccc1
c1ccc2c(c1)CCN2.c1ccccc1
HCl
null
null
null
O=C1Cc2c(Cl)cc(C(=O)c3ccccc3)cc2N1.O=C1Cc2ccc(C(=O)c3cccs3)cc2N1>>O=C1Cc2ccc(C(=O)c3ccccc3)cc2N1
ord_dataset-01dbb772c5e249108f0b191ed17a2c0c
ord-5795629fb40746d085bc44f1d0c40b6a
CC#N.O.c1ccc2c(c1)CCN2>>CC(=O)c1cccc2c1NCC2
B(Br)(Br)Br.Cl.C(C)#N.[Cl-].[Al+3].[Cl-].[Cl-].O.N1CCC2=CC=CC=C12>>C(C)(=O)C=1C=CC=C2CCNC12
N#[C:2][CH3:1].[OH2:3].[cH:4]1[cH:5][cH:6][cH:7][c:8]2[c:9]1[NH:10][CH2:11][CH2:12]2>>[CH3:1][C:2](=[O:3])[c:4]1[cH:5][cH:6][cH:7][c:8]2[c:9]1[NH:10][CH2:11][CH2:12]2
CC#N.O.c1ccc2c(c1)CCN2
CC(=O)c1cccc2c1NCC2
null
null
C1(=CC=CC=C1)C
Heteroatom Alkylation and Arylation
OtherReaction
05da27235e89652fc83a66d9d2d5176bc2f28258bebd97e499937d81fc5745d5
4ee1f20c4863715b4328c7be13c49a9e284d6de1cecfc1b4e83451c8d717f675
c1ccc2c(c1)CCN2
N#[C;H0;D2;+0:1]-[C;D1;H3:2].[C:3]-[#7:4]-[c:5](:[c:6]):[cH;D2;+0:7]:[c:8]:[c:9].[OH2;D0;+0:10]>>[C:3]-[#7:4]-[c:5](:[c:6]):[c;H0;D3;+0:7](-[C;H0;D3;+0:1](-[C;D1;H3:2])=[O;H0;D1;+0:10]):[c:8]:[c:9]
null
[]
5
CELSIUS
10
MINUTE
To a solution of 47.35 g. (0.5 mole) of boron tribromide in 300 ml. of toluene at 0° C. was added dropwise a solution of 50 g. (0.42 mole) of indoline and 22.39 g. (0.546 mole) of acetonitrile in 200 ml. of toluene. After stirring for 10 minutes 67.2 g. (0.5 mole) of aluminum chloride was added in portions. The resulti...
10.6084/m9.figshare.5104873.v1
null
Nitrile
Ketone
c1ccc2c(c1)CCN2
c1ccc2c(c1)CCN2
c1ccc2c(c1)CCN2
Other
C1(=CC=CC=C1)C
5
0.166667
CC#N.O.c1ccc2c(c1)CCN2>C1(=CC=CC=C1)C>CC(=O)c1cccc2c1NCC2
ord_dataset-01dbb772c5e249108f0b191ed17a2c0c
ord-72e6c5070b794368854183d6caa959fa
CC(=O)c1cccc2c1NCC2>>CC(=O)c1cccc2cc[nH]c12
C(C)(=O)C=1C=CC=C2CCNC12>>C(C)(=O)C=1C=CC=C2C=CNC12
[CH3:1][C:2](=[O:3])[c:4]1[cH:5][cH:6][cH:7][c:8]2[c:12]1[NH:11][CH2:10][CH2:9]2>>[CH3:1][C:2](=[O:3])[c:4]1[cH:5][cH:6][cH:7][c:8]2[cH:9][cH:10][nH:11][c:12]12
CC(=O)c1cccc2c1NCC2
CC(=O)c1cccc2cc[nH]c12
null
[O-2].[O-2].[Mn+4].[O-2].[O-2].[Mn+4].[O-2].[O-2].[Mn+4]
C(Cl)Cl
Oxidation
OtherReaction
2ed5a611e54dbdb6a4872dadd5b156713986794ff33171779f2c247b824bc0a1
45f806b8e00071c3429c43b3544e10767c5f82b269d7c53bc7fada9a5eb3b8c6
c1ccc2[nH]ccc2c1
[C;D1;H3:1]-[C:2](=[O;D1;H0:3])-[c:4]:[c:5]1:[c:6](:[c:7])-[CH2;D2;+0:8]-[CH2;D2;+0:9]-[NH;D2;+0:10]-1>>[C;D1;H3:1]-[C:2](=[O;D1;H0:3])-[c:4]:[c:5]1:[nH;D2;+0:10]:[cH;D2;+0:9]:[cH;D2;+0:8]:[c:6]:1:[c:7]
76
[{"value": 76.0, "product": "C(C)(=O)C=1C=CC=C2C=CNC12", "details": "PERCENTYIELD", "is_desired": false}]
null
null
5
HOUR
To 30 g. (0.186 mole) of 7-acetylindoline in 415 ml. of methylene chloride was added 48.5 g (0.56 mole) of manganese dioxide and the mixture refluxed through a soxhlet filled with 4A molecular sieves for 22 hours. The mixture was cooled and an additional 48.5 g. of manganese dioxide was added. Fresh molecular sieves we...
10.6084/m9.figshare.5104873.v1
null
Secondary amine
null
c1ccc2c(c1)CCN2
c1ccc2[nH]ccc2c1
c1ccc2[nH]ccc2c1
null
[O-2].[O-2].[Mn+4].[O-2].[O-2].[Mn+4].[O-2].[O-2].[Mn+4].C(Cl)Cl
null
5
CC(=O)c1cccc2c1NCC2>[O-2].[O-2].[Mn+4].[O-2].[O-2].[Mn+4].[O-2].[O-2].[Mn+4].C(Cl)Cl>CC(=O)c1cccc2cc[nH]c12
ord_dataset-01dbb772c5e249108f0b191ed17a2c0c
ord-62114cd74ab5480d93d8211eeeebf13b
CSc1cc2c(c(C(C)=O)c1)NC(=O)C2>>CC(=O)c1cccc2c1NC(=O)C2
C(CC)(=O)C=1C=CC=C2CC(NC12)=O.C(C1=CC=CC=C1)(=O)C=1C=CC=C2CC(NC12)=O.C1(=CC=CS1)C(=O)C=1C=CC=C2CC(NC12)=O.C1=C(C=CS1)C(=O)C=1C=CC=C2CC(NC12)=O.CC=1C=C2CC(NC2=C(C1)C(C)=O)=O.CSC=1C=C2CC(NC2=C(C1)C(C)=O)=O.FC=1C=C2CC(NC2=C(C1)C(C1=CC=CC=C1)=O)=O.BrC=1C=C2CC(NC2=C(C1)C(C1=CC=CS1)=O)=O>>C(C)(=O)C=1C=CC=C2CC(NC12)=O
CS[c:6]1[cH:5][c:4]([C:2]([CH3:1])=[O:3])[c:9]2[c:8]([cH:7]1)[CH2:13][C:11](=[O:12])[NH:10]2>>[CH3:1][C:2](=[O:3])[c:4]1[cH:5][cH:6][cH:7][c:8]2[c:9]1[NH:10][C:11](=[O:12])[CH2:13]2
CSc1cc2c(c(C(C)=O)c1)NC(=O)C2
CC(=O)c1cccc2c1NC(=O)C2
null
null
null
Reduction
OtherReaction
d730df81388c9d85c77c0667072e73b409dd35ba5b74f30f4a9e8e7bdba1a661
32a5269109432865a866e9a2b5da238f4471b13dee7daf193dc4e8c41b091706
O=C1Cc2ccccc2N1
C-S-[c;H0;D3;+0:1](:[c:2]:[c:3]-[C:4](-[C;D1;H3:5])=[O;D1;H0:6]):[c:7]:[c:8]>>[C;D1;H3:5]-[C:4](=[O;D1;H0:6])-[c:3]:[c:2]:[cH;D2;+0:1]:[c:7]:[c:8]
null
[]
null
null
null
null
Starting with the appropriate reagents and following the procedure of Preparation K, 7-propionyloxindole, 7-benzoyloxindole, 7-(2-thenoyl)oxindole, 7-(3-thenoyl)oxindole, 5-methyl-7-acetyloxindole, 5-methylthio-7-acetyloxindole, 5-fluoro-7-benzoyloxindole and 5-bromo-7-(2-thenoyl)oxindole are prepared. Conditions: See ...
10.6084/m9.figshare.5104873.v1
null
Monosulfide
null
c1ccc2c(c1)CCN2
c1ccc2c(c1)CCN2
c1ccc2c(c1)CCN2
Other
null
null
null
CSc1cc2c(c(C(C)=O)c1)NC(=O)C2>>CC(=O)c1cccc2c1NC(=O)C2
ord_dataset-01dbb772c5e249108f0b191ed17a2c0c
ord-6162f81a014e484d9b8d5eb5cdb0fc03
Cc1cc(C(=O)c2ccccc2)cc2c1NC(=O)C2.O=C1Cc2cc(C(=O)c3ccsc3)ccc2N1>>O=C1Cc2cc(C(=O)c3ccccc3)ccc2N1
C(C)(=O)C=1C=C2CC(NC2=CC1)=O.CC1=C2CC(NC2=CC=C1C(C)=O)=O.C1(=CC=CS1)C(=O)C=1C=C2CC(NC2=CC1)=O.C1=C(C=CS1)C(=O)C=1C=C2CC(NC2=CC1)=O.ClC1=C2CC(NC2=CC=C1C(C)=O)=O.CC=1C=C(C=C2CC(NC12)=O)C(C1=CC=CC=C1)=O.C(CC)(=O)C=1C=C2CC(NC2=CC1)=O>>C(C1=CC=CC=C1)(=O)C=1C=C2CC(NC2=CC1)=O
Cc1c[c:6]([C:7](=[O:8])[c:9]2[cH:10][cH:11][cH:12][cH:13][cH:14]2)[cH:5][c:4]2[c:17]1[NH:18][C:2](=[O:1])[CH2:3]2.O=C1Cc2cc(C(=O)c3ccsc3)[cH:15][cH:16]c2N1>>[O:1]=[C:2]1[CH2:3][c:4]2[cH:5][c:6]([C:7](=[O:8])[c:9]3[cH:10][cH:11][cH:12][cH:13][cH:14]3)[cH:15][cH:16][c:17]2[NH:18]1
Cc1cc(C(=O)c2ccccc2)cc2c1NC(=O)C2.O=C1Cc2cc(C(=O)c3ccsc3)ccc2N1
O=C1Cc2cc(C(=O)c3ccccc3)ccc2N1
null
null
null
Miscellaneous
OtherReaction
68f0df1de30bfd22cb32ca4d8d801675e44a02891b26c7502e11381199a37536
5b388534c7ab75644fe3aa2eae51d8d192360a553d2464346e04a8928be3e844
O=C1Cc2cc(C(=O)c3ccccc3)ccc2N1
C-c1:c:[c;H0;D3;+0:1](-[C:2](=[O;D1;H0:3])-[c:4]):[c:5]:[c:6]2:[c;H0;D3;+0:7]:1-[#7:8]-[C:9](=[O;D1;H0:10])-[C:11]-2.O=C1-C-c2:c:c(-C(=O)-c3:c:c:s:c:3):[cH;D2;+0:12]:[cH;D2;+0:13]:c:2-N-1>>[O;D1;H0:10]=[C:9]1-[#7:8]-[c;H0;D3;+0:7]2:[cH;D2;+0:13]:[cH;D2;+0:12]:[c;H0;D3;+0:1](-[C:2](=[O;D1;H0:3])-[c:4]):[c:5]:[c:6]:2-[C:...
null
[]
null
null
null
null
Using a similar procedure and starting with the requisite reagents, 5-acetyloxindole, 5-propionyloxindole, 5-(2-thenoyl)oxindole, 5-(3-thenoyl)oxindole, 4-methyl-5-acetyloxindole, 4-chloro-5-acetyloxindole and 7-methyl-5-benzoyloxindole are prepared. Conditions: See reaction.notes.procedure_details. Workup: are prepare...
10.6084/m9.figshare.5104873.v1
null
Ketone.Ketone.Secondary amide
Ketone
c1ccc2c(c1)CCN2.c1ccc2c(c1)CCN2.c1ccsc1
c1ccc2c(c1)CCN2
c1ccc2c(c1)CCN2.c1ccccc1
Other
null
null
null
Cc1cc(C(=O)c2ccccc2)cc2c1NC(=O)C2.O=C1Cc2cc(C(=O)c3ccsc3)ccc2N1>>O=C1Cc2cc(C(=O)c3ccccc3)ccc2N1
ord_dataset-01dbb772c5e249108f0b191ed17a2c0c
ord-3ed5c8b0016f4432bfed93da605fb3ce
O=C1Cc2ccc3c(c2N1)OCO3>>c1cc2cc3c(cc2[nH]1)OCO3
C1OC2=C3CC(NC3=CC=C2O1)=O.C1OC2=CC=C3CC(NC3=C2O1)=O.C1OC=2C=C3CC(NC3=CC2O1)=O.[N+](=O)([O-])C1=C(C=C2C(=C1)OCO2)CC(=O)OC.[N+](=O)([O-])C1OC2=C(C=CC=C2O1)CC(=O)OC>>C1OC=2C=C3C=CNC3=CC2O1
O=[C:1]1[CH2:2][c:3]2[cH:4][cH:5][c:6]3[c:7]([c:8]2[NH:9]1)[O:12][CH2:11][O:10]3>>[cH:1]1[cH:2][c:3]2[cH:4][c:5]3[c:6]([cH:7][c:8]2[nH:9]1)[O:10][CH2:11][O:12]3
O=C1Cc2ccc3c(c2N1)OCO3
c1cc2cc3c(cc2[nH]1)OCO3
null
null
null
Miscellaneous
OtherReaction
6634bf7734f230901309fa4f1521432488ab3987b53bd5428876f9d5c6eb6423
57d17b7f635fad717ee8ab10e86ef20b1bbadd42835b29ebc439bf55e4b83276
c1cc2cc3c(cc2[nH]1)OCO3
O=[C;H0;D3;+0:1]1-[CH2;D2;+0:2]-[c:3]2:[c:4]:[cH;D2;+0:5]:[c:6]3:[c;H0;D3;+0:7](:[c:8]:2-[NH;D2;+0:9]-1)-[O;H0;D2;+0:10]-[C:11]-[#8:12]-3>>[#8:12]1-[C:11]-[O;H0;D2;+0:10]-[c;H0;D3;+0:5]2:[c:4]:[c:3]3:[cH;D2;+0:2]:[cH;D2;+0:1]:[nH;D2;+0:9]:[c:8]:3:[cH;D2;+0:7]:[c:6]:2-1
null
[]
null
null
null
null
5,6-Methylenedioxyoxindole can be prepared via the reduction of methyl 2-nitro-4,5-methylenedioxyphenylacetate according to the procedure of McEvoy et al., J. Org. Chem., 38, 3350 (1973). By a similar procedure, starting with the appropriate methyl 2-nitromethylenedioxyphenylacetate, 4,5-methylenedioxyoxindole and 6,7-...
10.6084/m9.figshare.5104873.v1
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Ether.Secondary amide
Ether
c1cc2c(c3c1CCN3)OCO2
c1cc2cc3c(cc2[nH]1)OCO3
c1cc2cc3c(cc2[nH]1)OCO3
Other
null
null
null
O=C1Cc2ccc3c(c2N1)OCO3>>c1cc2cc3c(cc2[nH]1)OCO3
ord_dataset-01dbb772c5e249108f0b191ed17a2c0c
ord-2dd8beb060374261b699a38de66f5256
CC(C)N=C=O.O=C1Cc2ccccc2N1>>CC(C)NC(=O)N1C(=O)Cc2ccccc21
N1C(CC2=CC=CC=C12)=O.C(C)(C)N=C=O>>C(C)(C)NC(=O)N1C(CC2=CC=CC=C12)=O
[CH3:1][CH:2]([CH3:3])[N:4]=[C:5]=[O:6].[NH:7]1[C:8](=[O:9])[CH2:10][c:11]2[cH:12][cH:13][cH:14][cH:15][c:16]21>>[CH3:1][CH:2]([CH3:3])[NH:4][C:5](=[O:6])[N:7]1[C:8](=[O:9])[CH2:10][c:11]2[cH:12][cH:13][cH:14][cH:15][c:16]21
CC(C)N=C=O.O=C1Cc2ccccc2N1
CC(C)NC(=O)N1C(=O)Cc2ccccc21
null
null
C1(=CC=CC=C1)C
Acylation
Urea synthesis via isocyanate and secondary amine
29dd27c87e6f9801dcadea6821ce358d8a4f985bbfdea32deebaa8f964d87302
d8031df9745ffb9494a0da2553ed47ba21f8143926e9537ff85149a4ef4cadb4
O=C1Cc2ccccc2N1
[C;D1;H3:1]-[C:2](-[C;D1;H3:3])-[N;H0;D2;+0:4]=[C;H0;D2;+0:5]=[O;D1;H0:6].[O;D1;H0:7]=[C:8]1-[C:9]-[c:10]:[c:11](:[c:12])-[NH;D2;+0:13]-1>>[C;D1;H3:1]-[C:2](-[C;D1;H3:3])-[NH;D2;+0:4]-[C;H0;D3;+0:5](=[O;D1;H0:6])-[N;H0;D3;+0:13]1-[C:8](=[O;D1;H0:7])-[C:9]-[c:10]:[c:11]-1:[c:12]
null
[]
null
null
8
HOUR
To a stirred suspension of 5.0 g. (37.6 mmole) of 2-oxindole in 50 ml. of toluene was added 8.0 g. (94.0 mmole) of isopropyl isocyanate, and the mixture was heated under reflux for 6 hours. The reaction mixture was allowed to cool and then it was stirred at room temperature overnight. The solvent was removed by evapora...
10.6084/m9.figshare.5104873.v1
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Isocyanate.Secondary amide
Urea
c1ccc2c(c1)CCN2
c1ccc2c(c1)CC[NH]2
c1ccc2c(c1)CC[NH]2
null
C1(=CC=CC=C1)C
null
8
CC(C)N=C=O.O=C1Cc2ccccc2N1>C1(=CC=CC=C1)C>CC(C)NC(=O)N1C(=O)Cc2ccccc21
ord_dataset-01dbb772c5e249108f0b191ed17a2c0c
ord-bbeceddc0faf432ab9c414f3a0a0c3be
COC(=O)C1C(=O)Nc2ccc(Cl)cc21.O=C=Nc1ccccc1>>COC(=O)C1C(=O)N(C(=O)Nc2ccccc2)c2ccc(Cl)cc21
ClC=1C=C2C(C(NC2=CC1)=O)C(=O)OC.C1(=CC=CC=C1)N=C=O>>C1(=CC=CC=C1)NC(=O)N1C(C(C2=CC(=CC=C12)Cl)C(=O)OC)=O
[CH3:1][O:2][C:3](=[O:4])[CH:5]1[C:6](=[O:7])[NH:8][c:18]2[cH:19][cH:20][c:21]([Cl:22])[cH:23][c:24]21.[C:9](=[O:10])=[N:11][c:12]1[cH:13][cH:14][cH:15][cH:16][cH:17]1>>[CH3:1][O:2][C:3](=[O:4])[CH:5]1[C:6](=[O:7])[N:8]([C:9](=[O:10])[NH:11][c:12]2[cH:13][cH:14][cH:15][cH:16][cH:17]2)[c:18]2[cH:19][cH:20][c:21]([Cl:22]...
COC(=O)C1C(=O)Nc2ccc(Cl)cc21.O=C=Nc1ccccc1
COC(=O)C1C(=O)N(C(=O)Nc2ccccc2)c2ccc(Cl)cc21
null
null
C1(=CC=CC=C1)C
Acylation
Urea synthesis via isocyanate and secondary amine
29dd27c87e6f9801dcadea6821ce358d8a4f985bbfdea32deebaa8f964d87302
d8031df9745ffb9494a0da2553ed47ba21f8143926e9537ff85149a4ef4cadb4
O=C1Cc2ccccc2N1C(=O)Nc1ccccc1
[#8:1]-[C:2](=[O;D1;H0:3])-[C:4]1-[c:5]:[c:6](:[c:7])-[NH;D2;+0:8]-[C:9]-1=[O;D1;H0:10].[O;D1;H0:11]=[C;H0;D2;+0:12]=[N;H0;D2;+0:13]-[c:14](:[c:15]):[c:16]>>[#8:1]-[C:2](=[O;D1;H0:3])-[C:4]1-[c:5]:[c:6](:[c:7])-[N;H0;D3;+0:8](-[C;H0;D3;+0:12](=[O;D1;H0:11])-[NH;D2;+0:13]-[c:14](:[c:15]):[c:16])-[C:9]-1=[O;D1;H0:10]
null
[]
null
null
null
null
To 6.0 g. (0.027 mole) of methyl 5-chlorooxindole-3-carboxylate in 200 ml. of toluene was added 5.25 ml. (0.048 mole) of phenylisocyanate and the resulting reaction mixture heated to reflux overnight. The reaction mixture was cooled and diluted with petroleum ether to give, after filtration and drying, 2.0 g. of the de...
10.6084/m9.figshare.5104873.v1
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Isocyanate.Secondary amide
Urea
c1ccc2c(c1)CCN2
c1ccc2c(c1)CC[NH]2
c1ccccc1.c1ccc2c(c1)CC[NH]2
null
C1(=CC=CC=C1)C
null
null
COC(=O)C1C(=O)Nc2ccc(Cl)cc21.O=C=Nc1ccccc1>C1(=CC=CC=C1)C>COC(=O)C1C(=O)N(C(=O)Nc2ccccc2)c2ccc(Cl)cc21
ord_dataset-01dbb772c5e249108f0b191ed17a2c0c
ord-dacd69f7df84455997655f6c3f309e42
O=Cc1ccccc1>>O=Cc1ccccc1
C(C1=CC=CC=C1)=O.C(C=CC1=CC=CC=C1)=O>>C(C1=CC=CC=C1)=O.C(C=CC1=CC=CC=C1)=O
[O:11]=[CH:12][c:13]1[cH:14][cH:15][cH:16][cH:17][cH:18]1>>[O:11]=[CH:12][c:13]1[cH:14][cH:15][cH:16][cH:17][cH:18]1
O=Cc1ccccc1
O=Cc1ccccc1
null
null
null
Miscellaneous
OtherReaction
40ba59785861b8226ce5af6bdcbb9a37f0ff50a8c7ec7d4fc4c524cf906cc65c
56ebed4a8b3cebec83c37a71d68f0c87d1e404ab05a9ce792691e4e18a2379dd
c1ccccc1
null
null
[]
null
null
null
null
FIG. 2 is the GC-IR spectrum for the bottoms in the distillation pot. The peak indicated by reference numeral 20 is the peak for benzaldehyde. The peak indicated by reference numeral 21 is the peak for the cinnamaldehyde. Conditions: See reaction.notes.procedure_details.
10.6084/m9.figshare.5104873.v1
null
null
null
null
null
c1ccccc1
null
null
null
null
O=Cc1ccccc1>>O=Cc1ccccc1
ord_dataset-01dbb772c5e249108f0b191ed17a2c0c
ord-a5f8cf3706fb4e88af4fdf400f66f3e5
CCCc1cnc2c(c1)C(=O)N(C(C)(C(N)=O)C(C)C)C2=O>>CCCc1cnc2c(c1)C(=O)N1C2=NC(=O)C1(C)C(C)C
[OH-].[Na+].C(CC)C=1C=C2C(=NC1)C(N(C2=O)C(C(=O)N)(C)C(C)C)=O.O>>C(C)(C)C1(C(N=C2N1C(C=1C2=NC=C(C1)CCC)=O)=O)C
O=[C:13]1[c:7]2[n:6][cH:5][c:4]([CH2:3][CH2:2][CH3:1])[cH:9][c:8]2[C:10](=[O:11])[N:12]1[C:17]([C:15]([NH2:14])=[O:16])([CH3:18])[CH:19]([CH3:20])[CH3:21]>>[CH3:1][CH2:2][CH2:3][c:4]1[cH:5][n:6][c:7]2[c:8]([cH:9]1)[C:10](=[O:11])[N:12]1[C:13]2=[N:14][C:15](=[O:16])[C:17]1([CH3:18])[CH:19]([CH3:20])[CH3:21]
CCCc1cnc2c(c1)C(=O)N(C(C)(C(N)=O)C(C)C)C2=O
CCCc1cnc2c(c1)C(=O)N1C2=NC(=O)C1(C)C(C)C
null
null
C1(=CC=CC=C1)C
Heteroatom Alkylation and Arylation
OtherReaction
852876acc5fdf94c26885bc136e0813562d82bf37ea8cb48c3ec1f45894b34a9
cbb7764ac83f445d6d83811eb9820561db36f218c9f02320a912cef153626521
O=C1CN2C(=O)c3cccnc3C2=N1
O=[C;H0;D3;+0:1]1-[#7:2](-[C:3]-[C:4](-[NH2;D1;+0:5])=[O;D1;H0:6])-[C:7](=[O;D1;H0:8])-[c:9]:[c:10]-1:[#7;a:11]:[c:12]>>[O;D1;H0:8]=[C:7]1-[c:9]:[c:10](:[#7;a:11]:[c:12])-[C;H0;D3;+0:1]2=[N;H0;D2;+0:5]-[C:4](=[O;D1;H0:6])-[C:3]-[#7:2]-1-2
null
[]
null
null
null
null
With the simultaneous addition of 0.5 g of powdered sodium hydroxide, a solution of α-[3-n-propyl-6H-pyrrolo[3,4-b]pyridine-5,7-dione-6-yl]-α-isopropyl-α-methyl-acetamide (m.p.: 82° C.) in 100 ml of toluene is heated under reflux for 2 hours in a water separator. After the reaction solution has cooled, it is filtered t...
10.6084/m9.figshare.5104873.v1
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Substituted dicarboximide.Primary amide
null
c1cnc2c(c1)C[NH]C2
c1cnc2c(c1)CN1CCN=C21
c1cnc2c(c1)CN1CCN=C21
HO-
C1(=CC=CC=C1)C
null
null
CCCc1cnc2c(c1)C(=O)N(C(C)(C(N)=O)C(C)C)C2=O>C1(=CC=CC=C1)C>CCCc1cnc2c(c1)C(=O)N1C2=NC(=O)C1(C)C(C)C
ord_dataset-01dbb772c5e249108f0b191ed17a2c0c
ord-7aa85cf980dc49f198b0ddfbeab452f7
CC(C)CCCCCCCCCCCCC(=O)O.O=S(Cl)Cl>>CC(C)CCCCCCCCCCCCC(=O)Cl
C(CCCCCCCCCCCCC(C)C)(=O)O.S(=O)(Cl)Cl>>C(CCCCCCCCCCCCC(C)C)(=O)Cl
O[C:16]([CH2:15][CH2:14][CH2:13][CH2:12][CH2:11][CH2:10][CH2:9][CH2:8][CH2:7][CH2:6][CH2:5][CH2:4][CH:2]([CH3:1])[CH3:3])=[O:17].O=S(Cl)[Cl:18]>>[CH3:1][CH:2]([CH3:3])[CH2:4][CH2:5][CH2:6][CH2:7][CH2:8][CH2:9][CH2:10][CH2:11][CH2:12][CH2:13][CH2:14][CH2:15][C:16](=[O:17])[Cl:18]
CC(C)CCCCCCCCCCCCC(=O)O.O=S(Cl)Cl
CC(C)CCCCCCCCCCCCC(=O)Cl
null
null
null
Functional Group Interconversion
Alcohol to chloride_SOCl2
c301c14a9dcd0670d52e8b77396cbe7fd8edeedd757bc43f4162ade1fc52fc93
787f545db5dc0b29dde55b5fbed7db8625b8055f49327f97ed4d83cc47c3af1d
null
Cl-S(=O)-[Cl;H0;D1;+0:1].O-[C;H0;D3;+0:2](=[O;D1;H0:3])-[C:4]-[C:5]>>[C:5]-[C:4]-[C;H0;D3;+0:2](-[Cl;H0;D1;+0:1])=[O;D1;H0:3]
null
[]
null
null
null
null
Isohexadecanoic acid (20 g, 0.078 mol) and thionyl chloride (7.2 ml, 0.0984 mol) were refluxed together gently for 1 hour to produce isohexadecanoyl chloride and the reaction was monitored by infra-red spectroscopy. Excess thionyl chloride was distilled away under rotary pump vacuum at reflux temperature. The acyl chlo...
10.6084/m9.figshare.5104873.v1
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Carboxylic acid
Acyl halide
null
null
null
HCl
null
null
null
CC(C)CCCCCCCCCCCCC(=O)O.O=S(Cl)Cl>>CC(C)CCCCCCCCCCCCC(=O)Cl
ord_dataset-01dbb772c5e249108f0b191ed17a2c0c
ord-580394b4ef7a438bb6f3a79f841eee23
COC(=O)C(C)Br.NS(=O)(=O)c1ccccc1O>>COC(=O)C(C)Oc1ccccc1S(N)(=O)=O
OC1=C(C=CC=C1)S(=O)(=O)N.C([O-])([O-])=O.[K+].[K+].BrC(C(=O)OC)C>>COC(=O)C(C)OC1=C(C=CC=C1)S(=O)(=O)N
Br[CH:5]([C:3]([O:2][CH3:1])=[O:4])[CH3:6].[OH:7][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][C:3](=[O:4])[CH:5]([CH3:6])[O:7][c:8]1[cH:9][cH:10][cH:11][cH:12][c:13]1[S:14]([NH2:15])(=[O:16])=[O:17]
COC(=O)C(C)Br.NS(=O)(=O)c1ccccc1O
COC(=O)C(C)Oc1ccccc1S(N)(=O)=O
null
null
C(C)#N
Heteroatom Alkylation and Arylation
Williamson Ether Synthesis
a60236748d2543bdb97e5465447a595cd9bb5fef4e3fe96ed6af652af51cd157
94a54f0a6e629a85ca32b8fd3cf243ab64283e31ecfe8705ffe0df2304c488b4
c1ccccc1
Br-[CH;D3;+0:1](-[C;D1;H3:2])-[C:3](=[O;D1;H0:4])-[#8:5]-[C;D1;H3:6].[OH;D1;+0:7]-[c:8](:[c:9]):[c:10]>>[C;D1;H3:6]-[#8:5]-[C:3](=[O;D1;H0:4])-[CH;D3;+0:1](-[C;D1;H3:2])-[O;H0;D2;+0:7]-[c:8](:[c:9]):[c:10]
80.7
[{"value": 80.7, "product": "COC(=O)C(C)OC1=C(C=CC=C1)S(=O)(=O)N", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
null
null
34.6 g of 2-hydroxybenzenesulfonamide and 55.3 g of potassium carbonate are added to 800 ml of acetonitrile. With efficient stirring, 33.4 g of methyl 2-bromopropionate are added dropwise over 10 minutes and the suspension is then heated for 5 hours to 45° C. After the reaction mixture has cooled, the precipitated salt...
10.6084/m9.figshare.5104873.v1
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Secondary halide.Ester.Aromatic alcohol
Ester.Ether
null
null
c1ccccc1
HBr
C(C)#N
null
null
COC(=O)C(C)Br.NS(=O)(=O)c1ccccc1O>C(C)#N>COC(=O)C(C)Oc1ccccc1S(N)(=O)=O
ord_dataset-01dbb772c5e249108f0b191ed17a2c0c
ord-256cd9153e88410d975da315b2913afe
CCCCN=C=O.COC(=O)C(C)Oc1ccccc1S(N)(=O)=O>>COC(=O)C(C)Oc1ccccc1S(=O)(=O)N=C=O
C(=O)(Cl)Cl.COC(=O)C(C)OC1=C(C=CC=C1)S(=O)(=O)N.C(CCC)N=C=O.C(=O)(Cl)Cl>>COC(=O)C(C)OC1=C(C=CC=C1)S(=O)(=O)N=C=O
CCCCN=[C:18]=[O:19].[CH3:1][O:2][C:3](=[O:4])[CH:5]([CH3:6])[O:7][c:8]1[cH:9][cH:10][cH:11][cH:12][c:13]1[S:14](=[O:15])(=[O:16])[NH2:17]>>[CH3:1][O:2][C:3](=[O:4])[CH:5]([CH3:6])[O:7][c:8]1[cH:9][cH:10][cH:11][cH:12][c:13]1[S:14](=[O:15])(=[O:16])[N:17]=[C:18]=[O:19]
CCCCN=C=O.COC(=O)C(C)Oc1ccccc1S(N)(=O)=O
COC(=O)C(C)Oc1ccccc1S(=O)(=O)N=C=O
null
N1(NCCCCCC1)C1CCCCCCC1
C=1(C(=CC=CC1)C)C
Functional Group Interconversion
OtherReaction
d6c69f89b87c5c421a628563544ee2b8b0164ec4561bcd29a2cbba0dce4075ac
5df9e857f75ada60baf9e936007533a18389016451154bd1ed26e91b5babd844
c1ccccc1
C-C-C-C-N=[C;H0;D2;+0:1]=[O;D1;H0:2].[NH2;D1;+0:3]-[#16:4](=[O;D1;H0:5])(=[O;D1;H0:6])-[c:7]>>[O;D1;H0:5]=[#16:4](=[O;D1;H0:6])(-[c:7])-[N;H0;D2;+0:3]=[C;H0;D2;+0:1]=[O;D1;H0:2]
125.5
[{"value": 125.5, "product": "COC(=O)C(C)OC1=C(C=CC=C1)S(=O)(=O)N=C=O", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
null
null
A mixture of 12.9 g of 2-(1-methoxycarbonylethoxy)-benzenesulfonamide, 4.9 g of n-butylisocyanate and 0.1 g of diazabicyclooctane and 130 ml of xylene is refluxed for 30 minutes. Then 10 g of phosgene are passed into the solution at the same temperature over 90 minutes. Excess phosgene is expelled with nitrogen and the...
10.6084/m9.figshare.5104873.v1
null
Sulfonamide.Isocyanate
null
null
null
c1ccccc1
Other
N1(NCCCCCC1)C1CCCCCCC1.C=1(C(=CC=CC1)C)C
null
null
CCCCN=C=O.COC(=O)C(C)Oc1ccccc1S(N)(=O)=O>N1(NCCCCCC1)C1CCCCCCC1.C=1(C(=CC=CC1)C)C>COC(=O)C(C)Oc1ccccc1S(=O)(=O)N=C=O
ord_dataset-01dbb772c5e249108f0b191ed17a2c0c
ord-a8b5e717444b4d86bbebb7c007f0d53f
C=CCOc1ccccc1S(N)(=O)=O.O=C(OO)c1cccc(Cl)c1>>NS(=O)(=O)c1ccccc1OCC1CO1
ClC1=CC(=CC=C1)C(=O)OO.C(C=C)OC1=C(C=CC=C1)S(=O)(=O)N>>O1C(C1)COC1=C(C=CC=C1)S(=O)(=O)N
[NH2:1][S:2](=[O:3])(=[O:4])[c:5]1[cH:6][cH:7][cH:8][cH:9][c:10]1[O:11][CH2:12][CH:13]=[CH2:14].O=C(O[OH:15])c1cccc(Cl)c1>>[NH2:1][S:2](=[O:3])(=[O:4])[c:5]1[cH:6][cH:7][cH:8][cH:9][c:10]1[O:11][CH2:12][CH:13]1[CH2:14][O:15]1
C=CCOc1ccccc1S(N)(=O)=O.O=C(OO)c1cccc(Cl)c1
NS(=O)(=O)c1ccccc1OCC1CO1
null
null
C(Cl)Cl
Heteroatom Alkylation and Arylation
OtherReaction
fa67e488c6e215faf3f8ba92b55089cf5ac738315c63f0805edf5ac603aa4c40
8f36f0953871bb4e46b1272823a9df5d866ec11318b28272136c57016b5bffba
c1ccc(OCC2CO2)cc1
Cl-c1:c:c:c:c(-C(=O)-O-[OH;D1;+0:1]):c:1.[#8:2]-[C:3]-[CH;D2;+0:4]=[CH2;D1;+0:5]>>[#8:2]-[C:3]-[CH;D3;+0:4]1-[CH2;D2;+0:5]-[O;H0;D2;+0:1]-1
78
[{"value": 78.0, "product": "O1C(C1)COC1=C(C=CC=C1)S(=O)(=O)N", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
null
null
To a mixture of 15.3 g of 3-chloroperbenzoic acid in 270 ml of absolute methylene chloride are added 14.2 g of 2-allyloxyphenylsulfonamide over 2 minutes. The solution is then heated to reflux for 3 hours, cooled, and then washed three times with saturated sodium carbonate solution and once with water. The organic phas...
10.6084/m9.figshare.5104873.v1
null
Aromatic halide.Peroxide.Allyl
Ether
c1ccccc1
C1CO1
c1ccccc1.C1CO1
HCl
C(Cl)Cl
null
null
C=CCOc1ccccc1S(N)(=O)=O.O=C(OO)c1cccc(Cl)c1>C(Cl)Cl>NS(=O)(=O)c1ccccc1OCC1CO1
ord_dataset-01dbb772c5e249108f0b191ed17a2c0c
ord-983466e81fae4be2b37209716d2579ca
CC(=O)COc1ccccc1S(N)(=O)=O.OCCO>>CC1(COc2ccccc2S(N)(=O)=O)OCCO1
C(C(C)=O)OC1=C(C=CC=C1)S(=O)(=O)N.C(CO)O.C1(=CC=C(C=C1)S(=O)(=O)O)C.C1(=CC=CC=C1)C>>CC1(OCCO1)COC1=C(C=CC=C1)S(=O)(=O)N
[CH3:1][C:2]([CH2:3][O:4][c:5]1[cH:6][cH:7][cH:8][cH:9][c:10]1[S:11]([NH2:12])(=[O:13])=[O:14])=[O:15].O[CH2:16][CH2:17][OH:18]>>[CH3:1][C:2]1([CH2:3][O:4][c:5]2[cH:6][cH:7][cH:8][cH:9][c:10]2[S:11]([NH2:12])(=[O:13])=[O:14])[O:15][CH2:16][CH2:17][O:18]1
CC(=O)COc1ccccc1S(N)(=O)=O.OCCO
CC1(COc2ccccc2S(N)(=O)=O)OCCO1
null
null
C(C)(=O)OCC
Heteroatom Alkylation and Arylation
OtherReaction
2baa95c632045e217509d8ec12cda8674252268fe3f8cb44eb2e5ebe0f27c30f
f8121a7732f8ef583111433d2b2d82886bf3a134c51dc6363d813c8cbf4e36f5
c1ccc(OCC2OCCO2)cc1
O-[CH2;D2;+0:1]-[C:2]-[OH;D1;+0:3].[#8:4]-[C:5]-[C;H0;D3;+0:6](-[C;D1;H3:7])=[O;H0;D1;+0:8]>>[#8:4]-[C:5]-[C;H0;D4;+0:6]1(-[C;D1;H3:7])-[O;H0;D2;+0:8]-[CH2;D2;+0:1]-[C:2]-[O;H0;D2;+0:3]-1
null
[]
null
null
null
null
A mixture of 4.58 g of 2-(2-propanon-1-yloxy)phenylsulfonamide, 2 ml of ethylene glycol, 0.02 g of p-toluenesulfonic acid and 30 ml of toluene is heated for 7 hours to reflux while simultaneously separating the water of reaction. The cooled solution is taken up in 80 ml of ethyl acetate and the organic phase is washed ...
10.6084/m9.figshare.5104873.v1
null
Ketone.Primary alcohol.Primary alcohol
Ether.Ether
null
C1COCO1
c1ccccc1.C1COCO1
HO-
C(C)(=O)OCC
null
null
CC(=O)COc1ccccc1S(N)(=O)=O.OCCO>C(C)(=O)OCC>CC1(COc2ccccc2S(N)(=O)=O)OCCO1
ord_dataset-01dbb772c5e249108f0b191ed17a2c0c
ord-f338593bb42141e5a94468c5d011ca54
CCCCCC(CO)C(C)O.N#Cc1ccc(C=O)cc1>>CCCCCC1COC(c2ccc(C#N)cc2)OC1C
C(#N)C1=CC=C(C=O)C=C1.OCC(C(C)O)CCCCC.C1(=CC=C(C=C1)S(=O)(=O)O)C>>C(#N)C1=CC=C(C=C1)C1OCC(C(O1)C)CCCCC
[CH3:1][CH2:2][CH2:3][CH2:4][CH2:5][CH:6]([CH2:7][OH:8])[CH:19]([OH:18])[CH3:20].O=[CH:9][c:10]1[cH:11][cH:12][c:13]([C:14]#[N:15])[cH:16][cH:17]1>>[CH3:1][CH2:2][CH2:3][CH2:4][CH2:5][CH:6]1[CH2:7][O:8][CH:9]([c:10]2[cH:11][cH:12][c:13]([C:14]#[N:15])[cH:16][cH:17]2)[O:18][CH:19]1[CH3:20]
CCCCCC(CO)C(C)O.N#Cc1ccc(C=O)cc1
CCCCCC1COC(c2ccc(C#N)cc2)OC1C
null
null
C1=CC=CC=C1
Heteroatom Alkylation and Arylation
OtherReaction
078119554865b648a6facdc6248b78db5e4dc0f883a88231fb077723ffc0df4e
232b156bc2ce8ae2305afd0f173afafd4724b8e3a40743bae5e711a1772e739c
c1ccc(C2OCCCO2)cc1
O=[CH;D2;+0:1]-[c:2](:[c:3]):[c:4].[C;D1;H3:5]-[C:6](-[OH;D1;+0:7])-[C:8]-[C:9]-[OH;D1;+0:10]>>[C;D1;H3:5]-[C:6]1-[C:8]-[C:9]-[O;H0;D2;+0:10]-[CH;D3;+0:1](-[c:2](:[c:3]):[c:4])-[O;H0;D2;+0:7]-1
null
[]
null
null
null
null
A mixture of 0.1 mol of p-cyanobenzaldehyde, 0.1 mol of 3-hydroxymethyl-2-octanol, 200 ml of benzene and 150 mg of p-toluenesulfonic acid is boiled under a water separator until the reaction is complete. Usual working-up gives 2-p-cyanophenyl-5-n-pentyl-4-methyl-1,3-dioxane. Conditions: See reaction.notes.procedure_det...
10.6084/m9.figshare.5104873.v1
null
Aldehyde.Primary alcohol.Secondary alcohol
Ether.Ether
null
C1COCOC1
C1COCOC1.c1ccccc1
HO-
C1=CC=CC=C1
null
null
CCCCCC(CO)C(C)O.N#Cc1ccc(C=O)cc1>C1=CC=CC=C1>CCCCCC1COC(c2ccc(C#N)cc2)OC1C
ord_dataset-01dbb772c5e249108f0b191ed17a2c0c
ord-42d1b3eddfb84c7aa01824183c097731
N#CN.O=C(Cl)c1ccccc1>>N#CNC(=O)c1ccccc1
C(C1=CC=CC=C1)(=O)Cl.N#CN.[Na]>>C(C1=CC=CC=C1)(=O)NC#N
[N:1]#[C:2][NH2:3].Cl[C:4](=[O:5])[c:6]1[cH:7][cH:8][cH:9][cH:10][cH:11]1>>[N:1]#[C:2][NH:3][C:4](=[O:5])[c:6]1[cH:7][cH:8][cH:9][cH:10][cH:11]1
N#CN.O=C(Cl)c1ccccc1
N#CNC(=O)c1ccccc1
null
null
CCOCC.C(C)OCC
Acylation
Acylation of Nitrogen Nucleophiles by Acyl/Thioacyl/Carbamoyl Halides and Analogs_OS
6b8795ab649e99ec7e765cbd407ce37a0b3638ad96cc9e672bdd7bec29c34cf9
bb28f60d9d2ec09482b204d99571e49e964dfcf84ef33afba181651521212242
c1ccccc1
Cl-[C;H0;D3;+0:1](=[O;D1;H0:2])-[c:3](:[c:4]):[c:5].[N;D1;H0:6]#[C:7]-[NH2;D1;+0:8]>>[N;D1;H0:6]#[C:7]-[NH;D2;+0:8]-[C;H0;D3;+0:1](=[O;D1;H0:2])-[c:3](:[c:4]):[c:5]
89.7
[{"value": 89.7, "product": "C(C1=CC=CC=C1)(=O)NC#N", "details": "PERCENTYIELD", "is_desired": false}, {"value": 89.6, "product": "C(C1=CC=CC=C1)(=O)NC#N", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
8
HOUR
Benzoylcyanamide was prepared by the addition of benzoyl chloride (6.33 g, 0.045 mol) in 100 ml of diethyl ether to a suspension of monosodium cyanamide (5.76 g, 0.090 mol) in 100 ml of ether at 4° C. The reaction was stirred overnight at room temperature and the pale yellow solid which formed was collected and dissolv...
10.6084/m9.figshare.5104873.v1
null
Acyl halide.Cyanamide
Cyanamide.Secondary amide
null
null
c1ccccc1
HCl
CCOCC.C(C)OCC
null
8
N#CN.O=C(Cl)c1ccccc1>CCOCC.C(C)OCC>N#CNC(=O)c1ccccc1
ord_dataset-01dbb772c5e249108f0b191ed17a2c0c
ord-8d2f5af8638c4353be74f64ba58b6a7f
N#CN.O=C(Cl)C12CC3CC(CC(C3)C1)C2>>N#CNC(=O)C12CC3CC(CC(C3)C1)C2
C12(CC3CC(CC(C1)C3)C2)C(=O)Cl.N#CN.[Na]>>C12(CC3CC(CC(C1)C3)C2)C(=O)NC#N
[N:1]#[C:2][NH2:3].Cl[C:4](=[O:5])[C:6]12[CH2:7][CH:8]3[CH2:9][CH:10]([CH2:11][CH:12]([CH2:13]3)[CH2:14]1)[CH2:15]2>>[N:1]#[C:2][NH:3][C:4](=[O:5])[C:6]12[CH2:7][CH:8]3[CH2:9][CH:10]([CH2:11][CH:12]([CH2:13]3)[CH2:14]1)[CH2:15]2
N#CN.O=C(Cl)C12CC3CC(CC(C3)C1)C2
N#CNC(=O)C12CC3CC(CC(C3)C1)C2
null
null
C1CCOC1
Acylation
Acylation of Nitrogen Nucleophiles by Acyl/Thioacyl/Carbamoyl Halides and Analogs_OS
6b8795ab649e99ec7e765cbd407ce37a0b3638ad96cc9e672bdd7bec29c34cf9
bb28f60d9d2ec09482b204d99571e49e964dfcf84ef33afba181651521212242
C1C2CC3CC1CC(C2)C3
Cl-[C;H0;D3;+0:1](=[O;D1;H0:2])-[C:3](-[C:4])(-[C:5])-[C:6].[N;D1;H0:7]#[C:8]-[NH2;D1;+0:9]>>[C:4]-[C:3](-[C;H0;D3;+0:1](=[O;D1;H0:2])-[NH;D2;+0:9]-[C:8]#[N;D1;H0:7])(-[C:5])-[C:6]
85.2
[{"value": 85.2, "product": "C12(CC3CC(CC(C1)C3)C2)C(=O)NC#N", "details": "PERCENTYIELD", "is_desired": false}]
null
null
15
HOUR
1-Adamantanecarbonyl chloride (1.99 g, 0.010 mol) in 50 ml of THF was added drop-wise to a suspension of sodium cyanamide (1.92 g, 0.030 mol) in 100 ml of THF with stirring at ice bath temperature. The reaction was allowed to proceed at 25° C. for 15 hours. The reaction mixture was then extracted with ethyl acetate (10...
10.6084/m9.figshare.5104873.v1
null
Acyl halide.Cyanamide
Cyanamide.Secondary amide
null
null
C1C2CC3CC1CC(C2)C3
HCl
C1CCOC1
null
15
N#CN.O=C(Cl)C12CC3CC(CC(C3)C1)C2>C1CCOC1>N#CNC(=O)C12CC3CC(CC(C3)C1)C2
ord_dataset-01dbb772c5e249108f0b191ed17a2c0c
ord-3d74b36b043e477a96a43e1e42ccd381
CCCCCCCCCCCCCCCC(=O)Cl.N#CN>>CCCCCCCCCCCCCCCC(=O)NC#N
Cl.C(CCCCCCCCCCCCCCC)(=O)Cl.C1CCOC1.N#CN.[Na]>>C(CCCCCCCCCCCCCCC)(=O)NC#N
Cl[C:16]([CH2:15][CH2:14][CH2:13][CH2:12][CH2:11][CH2:10][CH2:9][CH2:8][CH2:7][CH2:6][CH2:5][CH2:4][CH2:3][CH2:2][CH3:1])=[O:17].[NH2:18][C:19]#[N:20]>>[CH3:1][CH2:2][CH2:3][CH2:4][CH2:5][CH2:6][CH2:7][CH2:8][CH2:9][CH2:10][CH2:11][CH2:12][CH2:13][CH2:14][CH2:15][C:16](=[O:17])[NH:18][C:19]#[N:20]
CCCCCCCCCCCCCCCC(=O)Cl.N#CN
CCCCCCCCCCCCCCCC(=O)NC#N
null
null
O
Acylation
Acylation of Nitrogen Nucleophiles by Acyl/Thioacyl/Carbamoyl Halides and Analogs_OS
6b8795ab649e99ec7e765cbd407ce37a0b3638ad96cc9e672bdd7bec29c34cf9
bb28f60d9d2ec09482b204d99571e49e964dfcf84ef33afba181651521212242
null
Cl-[C;H0;D3;+0:1](=[O;D1;H0:2])-[C:3]-[C:4].[N;D1;H0:5]#[C:6]-[NH2;D1;+0:7]>>[C:4]-[C:3]-[C;H0;D3;+0:1](=[O;D1;H0:2])-[NH;D2;+0:7]-[C:6]#[N;D1;H0:5]
96.3
[{"value": 96.3, "product": "C(CCCCCCCCCCCCCCC)(=O)NC#N", "details": "PERCENTYIELD", "is_desired": false}]
null
null
43
HOUR
A solution of palmitoyl chloride (5.5 g, 0.020 mol) in 50 ml of freshly distilled dry THF was added drop-wise to a suspension of sodium cyanamide (3.84 g. 0.060 mol) in 150 ml of freshly distilled dry THF at ice bath temperature. After the addition, the ice bath was removed and the reaction was allowed to proceed at 25...
10.6084/m9.figshare.5104873.v1
null
Acyl halide.Cyanamide
Cyanamide.Secondary amide
null
null
null
HCl
O
null
43
CCCCCCCCCCCCCCCC(=O)Cl.N#CN>O>CCCCCCCCCCCCCCCC(=O)NC#N
ord_dataset-01dbb772c5e249108f0b191ed17a2c0c
ord-dc25777ecaf7489698498252fb79841d
CCCCCCCCCCCCCCCCCC(=O)Cl.N#CN>>CCCCCCCCCCCCCCCCCC(=O)NC#N
C(CCCCCCCCCCCCCCCCC)(=O)Cl.N#CN.[Na].C>>C(CCCCCCCCCCCCCCCCC)(=O)NC#N
Cl[C:18]([CH2:17][CH2:16][CH2:15][CH2:14][CH2:13][CH2:12][CH2:11][CH2:10][CH2:9][CH2:8][CH2:7][CH2:6][CH2:5][CH2:4][CH2:3][CH2:2][CH3:1])=[O:19].[NH2:20][C:21]#[N: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][C:18](=[O:19])[NH:20][C:...
CCCCCCCCCCCCCCCCCC(=O)Cl.N#CN
CCCCCCCCCCCCCCCCCC(=O)NC#N
null
null
C1CCOC1
Acylation
Acylation of Nitrogen Nucleophiles by Acyl/Thioacyl/Carbamoyl Halides and Analogs_OS
6b8795ab649e99ec7e765cbd407ce37a0b3638ad96cc9e672bdd7bec29c34cf9
bb28f60d9d2ec09482b204d99571e49e964dfcf84ef33afba181651521212242
null
Cl-[C;H0;D3;+0:1](=[O;D1;H0:2])-[C:3]-[C:4].[N;D1;H0:5]#[C:6]-[NH2;D1;+0:7]>>[C:4]-[C:3]-[C;H0;D3;+0:1](=[O;D1;H0:2])-[NH;D2;+0:7]-[C:6]#[N;D1;H0:5]
92.4
[{"value": 92.4, "product": "C(CCCCCCCCCCCCCCCCC)(=O)NC#N", "details": "PERCENTYIELD", "is_desired": false}]
null
null
63
HOUR
Stearoyl chloride (3.03 g, 0.010 mol) in 50 ml of freshly distilled dry THF was added drop-wise to a suspension of sodium cyanamide (1.92 g, 0.030 mol) in 100 ml of freshly distilled dry THF with vigorous stirring. The reaction was allowed to proceed at 25° C for 63 hours. The solids which formed were collected by filt...
10.6084/m9.figshare.5104873.v1
null
Acyl halide.Cyanamide
Cyanamide.Secondary amide
null
null
null
HCl
C1CCOC1
null
63
CCCCCCCCCCCCCCCCCC(=O)Cl.N#CN>C1CCOC1>CCCCCCCCCCCCCCCCCC(=O)NC#N
ord_dataset-01dbb772c5e249108f0b191ed17a2c0c
ord-67ec1dc910434204b9a74a71f75eb5df
N#CN.O=C(O)CNC(=O)c1ccccc1>>N#CNC(=O)CNC(=O)c1ccccc1
N#CN.[Na].C(CNC(=O)C1=CC=CC=C1)(=O)O.C1CCC(CC1)N=C=NC2CCCCC2.ON1C(CCC1=O)=O>>C(C1=CC=CC=C1)(=O)NCC(=O)NC#N
[N:1]#[C:2][NH2:3].O[C:4](=[O:5])[CH2:6][NH:7][C:8](=[O:9])[c:10]1[cH:11][cH:12][cH:13][cH:14][cH:15]1>>[N:1]#[C:2][NH:3][C:4](=[O:5])[CH2:6][NH:7][C:8](=[O:9])[c:10]1[cH:11][cH:12][cH:13][cH:14][cH:15]1
N#CN.O=C(O)CNC(=O)c1ccccc1
N#CNC(=O)CNC(=O)c1ccccc1
null
null
C(C)#N.O.CCOC(=O)C.CC(=O)O
Acylation
Carboxylic acid with primary amine to amide
1f865723370f71cf1ab7dc00831ab704a96a4326ef6e35f073cf7a866be1f70c
2e26a213e8110c6a5818ffd27f6c5189453b5abca653629394958b094b8ce114
c1ccccc1
O-[C;H0;D3;+0:1](=[O;D1;H0:2])-[C:3]-[#7:4]-[C:5]=[O;D1;H0:6].[N;D1;H0:7]#[C:8]-[NH2;D1;+0:9]>>[N;D1;H0:7]#[C:8]-[NH;D2;+0:9]-[C;H0;D3;+0:1](=[O;D1;H0:2])-[C:3]-[#7:4]-[C:5]=[O;D1;H0:6]
56.1
[{"value": 56.1, "product": "C(C1=CC=CC=C1)(=O)NCC(=O)NC#N", "details": "PERCENTYIELD", "is_desired": false}]
null
null
8
HOUR
Hippuric acid (3.58 g, 0.020 mol), DCC (4.13 g, 0.020 mol), and N-hydroxysuccinimide (2.3 g, 0.020 mol) were stirred in 100 ml of acetonitrile at ice bath temperature for 2 hours. The reaction mixture was filtered to remove the bulk of by-product DCU. The filtrate was evaporated in vacuo to dryness, the residue was red...
10.6084/m9.figshare.5104873.v1
null
Carboxylic acid.Cyanamide
Cyanamide.Secondary amide
null
null
c1ccccc1
HO-
C(C)#N.O.CCOC(=O)C.CC(=O)O
null
8
N#CN.O=C(O)CNC(=O)c1ccccc1>C(C)#N.O.CCOC(=O)C.CC(=O)O>N#CNC(=O)CNC(=O)c1ccccc1
ord_dataset-01dbb772c5e249108f0b191ed17a2c0c
ord-5d935ab7acac4024b0d5a2228ef4a134
CC(C)C[C@H](N)C(=O)O.O=C(Cl)c1ccccc1>>CC(C)C[C@H](NC(=O)c1ccccc1)C(=O)O
C(C1=CC=CC=C1)(=O)Cl.[OH-].[Na+].N[C@@H](CC(C)C)C(=O)O>>C(C1=CC=CC=C1)(=O)N[C@@H](CC(C)C)C(=O)O
[CH3:1][CH:2]([CH3:3])[CH2:4][C@H:5]([NH2:6])[C:15](=[O:16])[OH:17].Cl[C:7](=[O:8])[c:9]1[cH:10][cH:11][cH:12][cH:13][cH:14]1>>[CH3:1][CH:2]([CH3:3])[CH2:4][C@H:5]([NH:6][C:7](=[O:8])[c:9]1[cH:10][cH:11][cH:12][cH:13][cH:14]1)[C:15](=[O:16])[OH:17]
CC(C)C[C@H](N)C(=O)O.O=C(Cl)c1ccccc1
CC(C)C[C@H](NC(=O)c1ccccc1)C(=O)O
null
null
O
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:4]):[c:5].[C:6]-[C:7](-[NH2;D1;+0:8])-[C:9](=[O;D1;H0:10])-[O;D1;H1:11]>>[C:6]-[C:7](-[NH;D2;+0:8]-[C;H0;D3;+0:1](=[O;D1;H0:2])-[c:3](:[c:4]):[c:5])-[C:9](=[O;D1;H0:10])-[O;D1;H1:11]
null
[]
null
null
null
null
Benzoyl chloride (4.22 g, 0.030 mol) and 10% NaOH (12 ml, 0.030 mol) were added separately with vigorous stirring to a solution of L-leucine (3.94 g, 0.030 mol) in 150 ml of distilled water at ice bath temperature. The reaction was allowed to proceed at this temperature until the reaction mixture became clear (30 minut...
10.6084/m9.figshare.5104873.v1
null
Acyl halide.Primary amine
Secondary amide
null
null
c1ccccc1
HCl
O
null
null
CC(C)C[C@H](N)C(=O)O.O=C(Cl)c1ccccc1>O>CC(C)C[C@H](NC(=O)c1ccccc1)C(=O)O
ord_dataset-01dbb772c5e249108f0b191ed17a2c0c
ord-fa8fe89a9b5d4711ac8986f8cc6d799b
CC(C)C[C@H](NC(=O)c1ccccc1)C(=O)O.N#CN>>CC(C)C[C@H](NC(=O)c1ccccc1)C(=O)NC#N
N#CN.[Na].C1CCC(CC1)N=C=NC2CCCCC2.ON1C(CCC1=O)=O.C(C1=CC=CC=C1)(=O)N[C@@H](CC(C)C)C(=O)O>>C(C1=CC=CC=C1)(=O)N[C@@H](CC(C)C)C(=O)NC#N
O[C:15]([C@H:5]([CH2:4][CH:2]([CH3:1])[CH3:3])[NH:6][C:7](=[O:8])[c:9]1[cH:10][cH:11][cH:12][cH:13][cH:14]1)=[O:16].[NH2:17][C:18]#[N:19]>>[CH3:1][CH:2]([CH3:3])[CH2:4][C@H:5]([NH:6][C:7](=[O:8])[c:9]1[cH:10][cH:11][cH:12][cH:13][cH:14]1)[C:15](=[O:16])[NH:17][C:18]#[N:19]
CC(C)C[C@H](NC(=O)c1ccccc1)C(=O)O.N#CN
CC(C)C[C@H](NC(=O)c1ccccc1)C(=O)NC#N
null
null
C(C)#N.C1CCOC1.O
Acylation
Carboxylic acid with primary amine to amide
1f865723370f71cf1ab7dc00831ab704a96a4326ef6e35f073cf7a866be1f70c
2e26a213e8110c6a5818ffd27f6c5189453b5abca653629394958b094b8ce114
c1ccccc1
O-[C;H0;D3;+0:1](=[O;D1;H0:2])-[C:3](-[C:4])-[#7:5]-[C:6]=[O;D1;H0:7].[N;D1;H0:8]#[C:9]-[NH2;D1;+0:10]>>[C:4]-[C:3](-[#7:5]-[C:6]=[O;D1;H0:7])-[C;H0;D3;+0:1](=[O;D1;H0:2])-[NH;D2;+0:10]-[C:9]#[N;D1;H0:8]
42.9
[{"value": 42.9, "product": "C(C1=CC=CC=C1)(=O)N[C@@H](CC(C)C)C(=O)NC#N", "details": "PERCENTYIELD", "is_desired": false}]
null
null
2
HOUR
DCC (2.41 g, 0.0117 mol) and N-hydroxysuccinimide (1.35 g, 0.0117 mol) were added to a solution of N-benzoyl-L-leucine (2.75 g, 0.0117 mol) in 100 ml of acetonitrile at ice bath temperature. The reaction was allowed to proceed at this temperature for 2 hours. The reaction mixture was filtered to remove the bulk of the ...
10.6084/m9.figshare.5104873.v1
null
Carboxylic acid.Cyanamide
Cyanamide.Secondary amide
null
null
c1ccccc1
HO-
C(C)#N.C1CCOC1.O
null
2
CC(C)C[C@H](NC(=O)c1ccccc1)C(=O)O.N#CN>C(C)#N.C1CCOC1.O>CC(C)C[C@H](NC(=O)c1ccccc1)C(=O)NC#N
ord_dataset-01dbb772c5e249108f0b191ed17a2c0c
ord-c4b5968c16f543fc8c35e4b753328296
COC(=O)[C@@H](N)Cc1ccccc1.O=C1CC[C@@H](C(=O)O)N1>>COC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H]1CCC(=O)N1
Cl.COC([C@@H](N)CC1=CC=CC=C1)=O.CN1CCOCC1.CN1CCOCC1.ClC(=O)OCC(C)C.N1[C@@H](CCC1=O)C(=O)O>>COC([C@@H](NC([C@H]1NC(CC1)=O)=O)CC1=CC=CC=C1)=O
[CH3:1][O:2][C:3](=[O:4])[C@H:5]([CH2:6][c:7]1[cH:8][cH:9][cH:10][cH:11][cH:12]1)[NH2:13].O[C:14](=[O:15])[C@@H:16]1[CH2:17][CH2:18][C:19](=[O:20])[NH:21]1>>[CH3:1][O:2][C:3](=[O:4])[C@H:5]([CH2:6][c:7]1[cH:8][cH:9][cH:10][cH:11][cH:12]1)[NH:13][C:14](=[O:15])[C@@H:16]1[CH2:17][CH2:18][C:19](=[O:20])[NH:21]1
COC(=O)[C@@H](N)Cc1ccccc1.O=C1CC[C@@H](C(=O)O)N1
COC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H]1CCC(=O)N1
null
null
CN(C)C=O.C1CCOC1.CN(C)C=O.CCOC(=O)C.CC(=O)O
Acylation
Carboxylic acid with primary amine to amide
37494d655fc476b499cf056f6435518833ae87795aab58744c3c61cc6e2d35e8
1acc31e468ee9ff2d6601bea2d2eb10c464508bb7150073479303b3753dd92b4
O=C1CC[C@@H](C(=O)NCCc2ccccc2)N1
O-[C;H0;D3;+0:1](=[O;D1;H0:2])-[C:3](-[C:4])-[#7:5]-[C:6]=[O;D1;H0:7].[C:8]-[C:9](-[NH2;D1;+0:10])-[C:11](=[O;D1;H0:12])-[#8:13]-[C;D1;H3:14]>>[C:4]-[C:3](-[C;H0;D3;+0:1](=[O;D1;H0:2])-[NH;D2;+0:10]-[C:9](-[C:8])-[C:11](=[O;D1;H0:12])-[#8:13]-[C;D1;H3:14])-[#7:5]-[C:6]=[O;D1;H0:7]
null
[]
null
null
2
MINUTE
N-Methylmorpholine (2.02 g, 0.020 mol) and isobutyl chloroformate (2.73 g, 0.020 mol) were added to a solution of L-pyroglutamic acid (2.58 g, 0.020 mol) in 100 ml of THF/DMF (6:1) at -15° C. After a 2 minute coupling period, a mixture of L-phenylalanine methyl ester hydrochloride (4.31 g, 0.020 mol) (suspension) and N...
10.6084/m9.figshare.5104873.v1
null
Carboxylic acid.Primary amine
Secondary amide
null
null
c1ccccc1.C1CCNC1
HO-
CN(C)C=O.C1CCOC1.CN(C)C=O.CCOC(=O)C.CC(=O)O
null
0.033333
COC(=O)[C@@H](N)Cc1ccccc1.O=C1CC[C@@H](C(=O)O)N1>CN(C)C=O.C1CCOC1.CN(C)C=O.CCOC(=O)C.CC(=O)O>COC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H]1CCC(=O)N1
ord_dataset-01dbb772c5e249108f0b191ed17a2c0c
ord-590ba5be6eb243c4a69123ef9edf892d
N#CN.O=C1CC[C@@H](C(=O)N[C@@H](Cc2ccccc2)C(=O)O)N1>>N#CNC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H]1CCC(=O)N1
Cl.N#CN.[Na].N1[C@@H](CCC1=O)C(=O)N[C@@H](CC1=CC=CC=C1)C(=O)O.[Cl-].[Na+].C1CCC(CC1)N=C=NC2CCCCC2.ON1C(CCC1=O)=O>>N1[C@@H](CCC1=O)C(=O)N[C@@H](CC1=CC=CC=C1)C(=O)NC#N
[N:1]#[C:2][NH2:3].O[C:4](=[O:5])[C@H:6]([CH2:7][c:8]1[cH:9][cH:10][cH:11][cH:12][cH:13]1)[NH:14][C:15](=[O:16])[C@@H:17]1[CH2:18][CH2:19][C:20](=[O:21])[NH:22]1>>[N:1]#[C:2][NH:3][C:4](=[O:5])[C@H:6]([CH2:7][c:8]1[cH:9][cH:10][cH:11][cH:12][cH:13]1)[NH:14][C:15](=[O:16])[C@@H:17]1[CH2:18][CH2:19][C:20](=[O:21])[NH:22]...
N#CN.O=C1CC[C@@H](C(=O)N[C@@H](Cc2ccccc2)C(=O)O)N1
N#CNC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H]1CCC(=O)N1
null
null
C1CCOC1.O
Acylation
Carboxylic acid with primary amine to amide
1f865723370f71cf1ab7dc00831ab704a96a4326ef6e35f073cf7a866be1f70c
2e26a213e8110c6a5818ffd27f6c5189453b5abca653629394958b094b8ce114
O=C1CC[C@@H](C(=O)NCCc2ccccc2)N1
O-[C;H0;D3;+0:1](=[O;D1;H0:2])-[C:3](-[C:4])-[#7:5]-[C:6]=[O;D1;H0:7].[N;D1;H0:8]#[C:9]-[NH2;D1;+0:10]>>[C:4]-[C:3](-[#7:5]-[C:6]=[O;D1;H0:7])-[C;H0;D3;+0:1](=[O;D1;H0:2])-[NH;D2;+0:10]-[C:9]#[N;D1;H0:8]
42.5
[{"value": 42.5, "product": "N1[C@@H](CCC1=O)C(=O)N[C@@H](CC1=CC=CC=C1)C(=O)NC#N", "details": "PERCENTYIELD", "is_desired": false}]
null
null
6
HOUR
L-Pyroglutamyl-L-phenylalanine (4.10 g, 0.0148 mol) was allowed to react with DCC (3.37 g, 0.0163 mol) and N-hydroxysuccinimide (1.88 g, 0.0163 mol) in 60 ml of THF at ice bath temperature for 3 hours, and then at room temperature overnight. The reaction mixture was filtered and the filtrate was added drop-wise to a so...
10.6084/m9.figshare.5104873.v1
null
Carboxylic acid.Cyanamide
Cyanamide.Secondary amide
null
null
c1ccccc1.C1CCNC1
HO-
C1CCOC1.O
null
6
N#CN.O=C1CC[C@@H](C(=O)N[C@@H](Cc2ccccc2)C(=O)O)N1>C1CCOC1.O>N#CNC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H]1CCC(=O)N1
ord_dataset-01dbb772c5e249108f0b191ed17a2c0c
ord-b22dfcf72698442ba39b7f791a426504
[Cl-].[Mg+2]>>[Cl-].[Mg+2]
C(C)O.[Cl-].[Mg+2].[Cl-].[Cl-].[Mg+2].[Cl-].C(C)C(CO)CCCC>>[Cl-].[Mg+2].[Cl-].C(C)C(CO)CCCC
[Cl-:10].[Mg+2:12]>>[Cl-:10].[Mg+2:12]
[Cl-].[Mg+2]
[Cl-].[Mg+2]
null
null
C(C)O
Miscellaneous
OtherReaction
40ba59785861b8226ce5af6bdcbb9a37f0ff50a8c7ec7d4fc4c524cf906cc65c
56ebed4a8b3cebec83c37a71d68f0c87d1e404ab05a9ce792691e4e18a2379dd
null
null
null
[]
null
null
null
null
To a sample (50 g, 0.134 mole) of magnesium chloride ethanol adduct prepared as in Example 2 and having an ethanol:magnesium chloride ratio of 6 was added 60 ml of 2-ethyl-1-hexanol. The solution was then distilled at 120° C. to remove ethanol and heptane. Decane (97.7 g) was added to the resulting viscous solution to ...
10.6084/m9.figshare.5104873.v1
null
null
null
null
null
null
null
C(C)O
null
null
[Cl-].[Mg+2]>C(C)O>[Cl-].[Mg+2]
ord_dataset-01dbb772c5e249108f0b191ed17a2c0c
ord-deb5187098a744fe880b2de0378ae21c
O=Cc1ccccc1>>O=Cc1ccccc1
C(C1=CC=CC=C1)=O.C(C=CC1=CC=CC=C1)=O>>C(C1=CC=CC=C1)=O.C(C=CC1=CC=CC=C1)=O
[O:11]=[CH:12][c:13]1[cH:14][cH:15][cH:16][cH:17][cH:18]1>>[O:11]=[CH:12][c:13]1[cH:14][cH:15][cH:16][cH:17][cH:18]1
O=Cc1ccccc1
O=Cc1ccccc1
null
null
null
Miscellaneous
OtherReaction
40ba59785861b8226ce5af6bdcbb9a37f0ff50a8c7ec7d4fc4c524cf906cc65c
56ebed4a8b3cebec83c37a71d68f0c87d1e404ab05a9ce792691e4e18a2379dd
c1ccccc1
null
null
[]
null
null
null
null
FIG. 2 is the GC-IR spectrum for the bottoms in the distillation pot. The peak indicated by reference numeral 20 is the peak for benzaldehyde. The peak indicated by reference numeral 21 is the peak for the cinnamaldehyde. Conditions: See reaction.notes.procedure_details.
10.6084/m9.figshare.5104873.v1
null
null
null
null
null
c1ccccc1
null
null
null
null
O=Cc1ccccc1>>O=Cc1ccccc1
ord_dataset-01dbb772c5e249108f0b191ed17a2c0c
ord-5c4074c08323446d9ace398b44e77c79
COc1c(C)c2c(c(O)c1C/C=C(\C)CCC(=O)O)C(=O)OC2.O=S(Cl)Cl>>COc1c(C)c2c(c(O)c1C/C=C(\C)CCC(=O)Cl)C(=O)OC2
OC1=C2C(OCC2=C(C(=C1C/C=C(/CCC(=O)O)\C)OC)C)=O.S(=O)(Cl)Cl.CN(C=O)C>>OC1=C2C(OCC2=C(C(=C1C/C=C(/CCC(=O)Cl)\C)OC)C)=O
O[C:17]([CH2:16][CH2:15]/[C:13](=[CH:12]/[CH2:11][c:10]1[c:3]([O:2][CH3:1])[c:4]([CH3:5])[c:6]2[c:7]([c:8]1[OH:9])[C:20](=[O:21])[O:22][CH2:23]2)[CH3:14])=[O:18].O=S(Cl)[Cl:19]>>[CH3:1][O:2][c:3]1[c:4]([CH3:5])[c:6]2[c:7]([c:8]([OH:9])[c:10]1[CH2:11]/[CH:12]=[C:13](\[CH3:14])[CH2:15][CH2:16][C:17](=[O:18])[Cl:19])[C:20...
COc1c(C)c2c(c(O)c1C/C=C(\C)CCC(=O)O)C(=O)OC2.O=S(Cl)Cl
COc1c(C)c2c(c(O)c1C/C=C(\C)CCC(=O)Cl)C(=O)OC2
null
null
ClCCl
Functional Group Interconversion
Alcohol to chloride_SOCl2
c301c14a9dcd0670d52e8b77396cbe7fd8edeedd757bc43f4162ade1fc52fc93
787f545db5dc0b29dde55b5fbed7db8625b8055f49327f97ed4d83cc47c3af1d
O=C1OCc2ccccc21
Cl-S(=O)-[Cl;H0;D1;+0:1].O-[C;H0;D3;+0:2](=[O;D1;H0:3])-[C:4]-[C:5]\[C:6]=[C:7]>>[C:7]=[C:6]/[C:5]-[C:4]-[C;H0;D3;+0:2](-[Cl;H0;D1;+0:1])=[O;D1;H0:3]
null
[]
null
null
3
HOUR
E-6-(1,3-dihydro-4-hydroxy-6-methoxy-7-methyl-3-oxo-5-isobenzofuranyl)-4-methyl-4-hexenoic acid (mycophenolic acid) (32.0 g) was dissolved in dichloromethane (250 ml), followed by the addition of thionyl chloride (25.0 ml) and dimethylformamide (0.3 ml). The reaction mixture was stirred at room temperature for 3 hours,...
10.6084/m9.figshare.5104873.v1
null
Carboxylic acid
Acyl halide
null
null
c1ccc2c(c1)COC2
HCl
ClCCl
null
3
COc1c(C)c2c(c(O)c1C/C=C(\C)CCC(=O)O)C(=O)OC2.O=S(Cl)Cl>ClCCl>COc1c(C)c2c(c(O)c1C/C=C(\C)CCC(=O)Cl)C(=O)OC2
ord_dataset-01dbb772c5e249108f0b191ed17a2c0c
ord-2f2d405188a5411ca7d093dc5156459a
COc1c(C)c2c(c(O)c1C/C=C(\C)CCC(=O)OCCN1CCOCC1)C(=O)OC2.O=C(Cl)C12CC3CC(CC(C3)C1)C2>>COc1c(C)c2c(c(OC(=O)C34CC5CC(CC(C5)C3)C4)c1C/C=C(\C)CCC(=O)OCCN1CCOCC1)C(=O)OC2
OC1=C2C(OCC2=C(C(=C1C/C=C(/CCC(=O)OCCN1CCOCC1)\C)OC)C)=O.C12(CC3CC(CC(C1)C3)C2)C(=O)Cl.O>>C12(CC3CC(CC(C1)C3)C2)C(=O)OC2=C3C(OCC3=C(C(=C2C/C=C(/CCC(=O)OCCN2CCOCC2)\C)OC)C)=O
[CH3:1][O:2][c:3]1[c:4]([CH3:5])[c:6]2[c:7]([c:8]([OH:9])[c:22]1[CH2:23]/[CH:24]=[C:25](\[CH3:26])[CH2:27][CH2:28][C:29](=[O:30])[O:31][CH2:32][CH2:33][N:34]1[CH2:35][CH2:36][O:37][CH2:38][CH2:39]1)[C:40](=[O:41])[O:42][CH2:43]2.Cl[C:10](=[O:11])[C:12]12[CH2:13][CH:14]3[CH2:15][CH:16]([CH2:17][CH:18]([CH2:19]3)[CH2:20]...
COc1c(C)c2c(c(O)c1C/C=C(\C)CCC(=O)OCCN1CCOCC1)C(=O)OC2.O=C(Cl)C12CC3CC(CC(C3)C1)C2
COc1c(C)c2c(c(OC(=O)C34CC5CC(CC(C5)C3)C4)c1C/C=C(\C)CCC(=O)OCCN1CCOCC1)C(=O)OC2
null
null
N1=CC=CC=C1
Acylation
Schotten-Baumann to ester
1cda078f55e64d9385e544d1067595d5e7672bbd1eff542e7a341817a2d8c4d5
6439fc27f97ee9ed7c11ef9b5032d9493d05f28a7bbb50d256a2d54d035fbfb2
O=C(CCC=CCc1ccc2c(c1OC(=O)C13CC4CC(CC(C4)C1)C3)C(=O)OC2)OCCN1CCOCC1
Cl-[C;H0;D3;+0:1](=[O;D1;H0:2])-[C:3](-[C:4])(-[C:5])-[C:6].[#8:7]-[C:8](=[O;D1;H0:9])-[c:10]:[c:11](-[OH;D1;+0:12]):[c:13]>>[#8:7]-[C:8](=[O;D1;H0:9])-[c:10]:[c:11](-[O;H0;D2;+0:12]-[C;H0;D3;+0:1](=[O;D1;H0:2])-[C:3](-[C:4])(-[C:5])-[C:6]):[c:13]
null
[]
null
null
90
MINUTE
Morpholinoethyl E-6-(1,3-dihydro-4-hydroxy-6-methoxy-7-methyl-3-oxo-5-isobenzofuranyl)-4-methyl-4-hexenoate (10.0 g) was dissolved in pyridine (50.0 ml) followed by the addition of 1-adamantanecarbonyl chloride (10.0 ml). The mixture was stirred at room temperature for 90 minutes, then poured into water and extracted w...
10.6084/m9.figshare.5104873.v1
null
Acyl halide.Aromatic alcohol
Ester
null
null
c1ccc2c(c1)COC2.C1COCC[NH]1.C1C2CC3CC1CC(C2)C3
HCl
N1=CC=CC=C1
null
1.5
COc1c(C)c2c(c(O)c1C/C=C(\C)CCC(=O)OCCN1CCOCC1)C(=O)OC2.O=C(Cl)C12CC3CC(CC(C3)C1)C2>N1=CC=CC=C1>COc1c(C)c2c(c(OC(=O)C34CC5CC(CC(C5)C3)C4)c1C/C=C(\C)CCC(=O)OCCN1CCOCC1)C(=O)OC2
ord_dataset-01dbb772c5e249108f0b191ed17a2c0c
ord-ce801baf663247ddbe6aa39a88d06aae
COc1c(C)c2c(c(O)c1C/C=C(\C)CCC(=O)OCCN1CCOCC1)C(=O)OC2.O=C(Cl)Cl>>COc1c(C)c2c(c(OC(N)=O)c1C/C=C(\C)CCC(=O)OCCN1CCOCC1)C(=O)OC2
OC1=C2C(OCC2=C(C(=C1C/C=C(/CCC(=O)OCCN1CCOCC1)\C)OC)C)=O.N1=CC=CC=C1.C(=O)(Cl)Cl>>C(N)(=O)OC1=C2C(OCC2=C(C(=C1C/C=C(/CCC(=O)OCCN1CCOCC1)\C)OC)C)=O
[CH3:1][O:2][c:3]1[c:4]([CH3:5])[c:6]2[c:7]([c:8]([OH:9])[c:13]1[CH2:14]/[CH:15]=[C:16](\[CH3:17])[CH2:18][CH2:19][C:20](=[O:21])[O:22][CH2:23][CH2:24][N:25]1[CH2:26][CH2:27][O:28][CH2:29][CH2:30]1)[C:31](=[O:32])[O:33][CH2:34]2.Cl[C:10](Cl)=[O:12]>>[CH3:1][O:2][c:3]1[c:4]([CH3:5])[c:6]2[c:7]([c:8]([O:9][C:10]([NH2:11]...
COc1c(C)c2c(c(O)c1C/C=C(\C)CCC(=O)OCCN1CCOCC1)C(=O)OC2.O=C(Cl)Cl
COc1c(C)c2c(c(OC(N)=O)c1C/C=C(\C)CCC(=O)OCCN1CCOCC1)C(=O)OC2
null
null
C1=CC=CC=C1
Functional Group Interconversion
OtherReaction
7a500c53e0c90ddb616b1d9844a25d18752778458f7cf9b6b4d76c7f92fd6ed9
1c930fd1a8ef596a25a9e8b02e0d655be711516e36782a4da179eb27706d6367
O=C(CCC=CCc1ccc2c(c1)C(=O)OC2)OCCN1CCOCC1
Cl-[C;H0;D3;+0:1](-Cl)=[O;D1;H0:2].[#8:3]-[C:4](=[O;D1;H0:5])-[c:6]:[c:7](-[OH;D1;+0:8]):[c:9]>>[#8:3]-[C:4](=[O;D1;H0:5])-[c:6]:[c:7](-[O;H0;D2;+0:8]-[C;H0;D3;+0:1](-[N;D1;H2:10])=[O;D1;H0:2]):[c:9]
null
[]
25
CELSIUS
8
HOUR
To a solution of 500 mgs of morpholinoethyl (E)-6-(1,3-dihydro-4-hydroxy-6-methoxy-7-methyl-3-oxo-5-isobenzofuranyl)-4-methyl-4-hexenoate in 10 ml of benzene cooled in an ice bath is added 0.1 ml of pyridine and 6 ml of a 12.5% solution of phosgene in benzene. The solution is stirred at 25° C. overnight, the precipitat...
10.6084/m9.figshare.5104873.v1
null
Acyl halide.Acyl halide.Aromatic alcohol
Carbamic ester
null
null
C1COCC[NH]1.c1ccc2c(c1)COC2
Other
C1=CC=CC=C1
25
8
COc1c(C)c2c(c(O)c1C/C=C(\C)CCC(=O)OCCN1CCOCC1)C(=O)OC2.O=C(Cl)Cl>C1=CC=CC=C1>COc1c(C)c2c(c(OC(N)=O)c1C/C=C(\C)CCC(=O)OCCN1CCOCC1)C(=O)OC2
ord_dataset-01dbb772c5e249108f0b191ed17a2c0c
ord-8099b77f8ff84220a75161afb1f5b51b
COc1c(C)c2c(c(OC(N)=O)c1C/C=C(\C)CCC(=O)O)C(=O)OC2.OCCN1CCOCC1>>COc1c(C)c2c(c(OC(N)=O)c1C/C=C(\C)CCC(=O)OCCN1CCOCC1)C(=O)OC2
C(N)(=O)OC1=C2C(OCC2=C(C(=C1C/C=C(/CCC(=O)O)\C)OC)C)=O.C1(CCCCC1)N=C=NC1CCCCC1.OCCN1CCOCC1>>C(N)(=O)OC1=C2C(OCC2=C(C(=C1C/C=C(/CCC(=O)OCCN1CCOCC1)\C)OC)C)=O
O[C:20]([CH2:19][CH2:18]/[C:16](=[CH:15]/[CH2:14][c:13]1[c:3]([O:2][CH3:1])[c:4]([CH3:5])[c:6]2[c:7]([c:8]1[O:9][C:10]([NH2:11])=[O:12])[C:31](=[O:32])[O:33][CH2:34]2)[CH3:17])=[O:21].[OH:22][CH2:23][CH2:24][N:25]1[CH2:26][CH2:27][O:28][CH2:29][CH2:30]1>>[CH3:1][O:2][c:3]1[c:4]([CH3:5])[c:6]2[c:7]([c:8]([O:9][C:10]([NH...
COc1c(C)c2c(c(OC(N)=O)c1C/C=C(\C)CCC(=O)O)C(=O)OC2.OCCN1CCOCC1
COc1c(C)c2c(c(OC(N)=O)c1C/C=C(\C)CCC(=O)OCCN1CCOCC1)C(=O)OC2
null
null
C1CCOC1
Protection
Esterification of Carboxylic Acids
070670f68a20c1021da94fabee54def4688122fb721af5f52cd5a03630845d0e
0d8a72b7375d91aa7263e766e03a3cb7c4fa91e27abcd590409ff03b98eed690
O=C(CCC=CCc1ccc2c(c1)C(=O)OC2)OCCN1CCOCC1
O-[C;H0;D3;+0:1](=[O;D1;H0:2])-[C:3]-[C:4]\[C:5]=[C:6].[C:7]-[C:8]-[OH;D1;+0:9]>>[C:6]=[C:5]/[C:4]-[C:3]-[C;H0;D3;+0:1](=[O;D1;H0:2])-[O;H0;D2;+0:9]-[C:8]-[C:7]
null
[]
null
null
6
HOUR
To 1.0 g of E-6-(1,3-dihydro-4-carbamoyloxy-6-methoxy-7-methyl-3-oxo-5-isobenzofuranyl)-4-methyl-4-hexenoic acid dissolved in 20 ml of dry THF is added 0.59 g of dicyclohexylcarbodiimide and 0.037 g of N-(2-hydroxyethyl)morpholine. The mixture is left at room temperature for 6 hours, then evaporated to dryness. The res...
10.6084/m9.figshare.5104873.v1
null
Carboxylic acid.Primary alcohol
Ester
null
null
C1COCC[NH]1.c1ccc2c(c1)COC2
HO-
C1CCOC1
null
6
COc1c(C)c2c(c(OC(N)=O)c1C/C=C(\C)CCC(=O)O)C(=O)OC2.OCCN1CCOCC1>C1CCOC1>COc1c(C)c2c(c(OC(N)=O)c1C/C=C(\C)CCC(=O)OCCN1CCOCC1)C(=O)OC2
ord_dataset-01dbb772c5e249108f0b191ed17a2c0c
ord-dbacce31933a4d398510bac67d92c6e7
CC1(C(=O)O)CCCCC1>>CC(O)C1CCCCC1
B.C1CCOC1.CC1(CCCCC1)C(=O)O.B.C1CCOC1>>CC(O)C1CCCCC1
O=[C:2]([OH:3])[C:4]1([CH3:1])[CH2:5][CH2:6][CH2:7][CH2:8][CH2:9]1>>[CH3:1][CH:2]([OH:3])[CH:4]1[CH2:5][CH2:6][CH2:7][CH2:8][CH2:9]1
CC1(C(=O)O)CCCCC1
CC(O)C1CCCCC1
null
null
C1CCOC1
Miscellaneous
OtherReaction
02693450693b5ad939656da33c0df49f70956a83b5ea223cc76f107c32825f6a
f1507539d754dbc80163ef9a22943a8dfdc34c3cb8fad36821712aaada773cb8
C1CCCCC1
O=[C;H0;D3;+0:1](-[O;D1;H1:2])-[C;H0;D4;+0:3](-[CH3;D1;+0:4])(-[C:5]-[C:6])-[C:7]-[C:8]>>[C:6]-[C:5]-[CH;D3;+0:3](-[CH;D3;+0:1](-[CH3;D1;+0:4])-[O;D1;H1:2])-[C:7]-[C:8]
null
[]
5
CELSIUS
5
MINUTE
A three liter, three necked round bottom flask was equipped with a thermometer, magnetic stirrer, argon inlet and outlet adapters and a one liter addition funnel containing 922 ml of 1.0 molar BH3.THF. 1-Methyl cyclohexanecarboxylic acid (119.2 g; 0.84 m) was added to the reaction vessel and dissolved in 100 ml of THF....
10.6084/m9.figshare.5104873.v1
null
Carboxylic acid
Secondary alcohol
C1CCCCC1
C1CCCCC1
C1CCCCC1
Other
C1CCOC1
5
0.083333
CC1(C(=O)O)CCCCC1>C1CCOC1>CC(O)C1CCCCC1
ord_dataset-01dbb772c5e249108f0b191ed17a2c0c
ord-45c157a66bd1401c8d8bebfdf83470d2
C1CCNC1.CC(C)(C)CO.ClCC1CO1>>CC(C)(C)COCC(O)CN1CCCC1
N1CCCC1.[OH-].[Na+].C(Cl)C1CO1.C(C(C)(C)C)O>>CC(COCC(CN1CCCC1)O)(C)C
[NH:11]1[CH2:12][CH2:13][CH2:14][CH2:15]1.[CH3:1][C:2]([CH3:3])([CH3:4])[CH2:5][OH:6].Cl[CH2:7][CH:8]1[O:9][CH2:10]1>>[CH3:1][C:2]([CH3:3])([CH3:4])[CH2:5][O:6][CH2:7][CH:8]([OH:9])[CH2:10][N:11]1[CH2:12][CH2:13][CH2:14][CH2:15]1
C1CCNC1.CC(C)(C)CO.ClCC1CO1
CC(C)(C)COCC(O)CN1CCCC1
null
null
null
Heteroatom Alkylation and Arylation
OtherReaction
f655b63b9e45f6ad5030684084cf6286e38e5915a3fb4f9a1c759f986198f248
f705254aa09bb51ef7de20148bd7444ecce3ca8ae0af005a4c2394ce21658de8
C1CCNC1
Cl-[CH2;D2;+0:1]-[C:2]1-[CH2;D2;+0:3]-[O;H0;D2;+0:4]-1.[C:5]-[C:6]-[OH;D1;+0:7].[C:8]1-[C:9]-[C:10]-[C:11]-[NH;D2;+0:12]-1>>[C:5]-[C:6]-[O;H0;D2;+0:7]-[CH2;D2;+0:1]-[C:2](-[OH;D1;+0:4])-[CH2;D2;+0:3]-[N;H0;D3;+0:12]1-[C:8]-[C:9]-[C:10]-[C:11]-1
84.1
[{"value": 84.1, "product": "CC(COCC(CN1CCCC1)O)(C)C", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
95
CELSIUS
null
null
To a stirred mixture of 92.53 g (1.0 m) of epichlorohydrin and 88.15 g (1.0 m) of neopentyl alcohol was added 0.26 g (0.001 m) of stannic chloride. The reaction temperature rose to about 60° C. then exothermed to about 130° C. in a few seconds. The reaction mixture was stirred until the temperature receded to about 40°...
10.6084/m9.figshare.5104873.v1
null
Primary halide.Ether.Primary alcohol.Secondary amine
Ether.Secondary alcohol.Tertiary amine
C1CCNC1.C1CO1
C1CC[NH]C1
C1CC[NH]C1
HCl
null
95
null
C1CCNC1.CC(C)(C)CO.ClCC1CO1>>CC(C)(C)COCC(O)CN1CCCC1
ord_dataset-01dbb772c5e249108f0b191ed17a2c0c
ord-a628bb901d9b42bc84a06439d0456eed
C1CCNC1.CC(C)(C)O.ClCC1CO1>>CC(C)(C)OCC(O)CN1CCCC1
C(C)(C)(C)O.C(Cl)C1CO1.[OH-].[Na+].N1CCCC1>>CC(C)(OCC(CN1CCCC1)O)C
[NH:10]1[CH2:11][CH2:12][CH2:13][CH2:14]1.[CH3:1][C:2]([CH3:3])([CH3:4])[OH:5].Cl[CH2:6][CH:7]1[O:8][CH2:9]1>>[CH3:1][C:2]([CH3:3])([CH3:4])[O:5][CH2:6][CH:7]([OH:8])[CH2:9][N:10]1[CH2:11][CH2:12][CH2:13][CH2:14]1
C1CCNC1.CC(C)(C)O.ClCC1CO1
CC(C)(C)OCC(O)CN1CCCC1
null
[Sn](Cl)(Cl)(Cl)Cl
O
Heteroatom Alkylation and Arylation
OtherReaction
cab3417d145cb649aab2859d86bc77c26251a64f18ffe518c132eaad15f036a7
eba4cd7e03ae0e735f7b27cf7de068bb9cce248c9fa86b1e9bd11f0eb4a58d43
C1CCNC1
Cl-[CH2;D2;+0:1]-[C:2]1-[CH2;D2;+0:3]-[O;H0;D2;+0:4]-1.[C;D1;H3:5]-[C:6](-[C;D1;H3:7])(-[C;D1;H3:8])-[OH;D1;+0:9].[C:10]1-[C:11]-[C:12]-[C:13]-[NH;D2;+0:14]-1>>[C;D1;H3:5]-[C:6](-[C;D1;H3:7])(-[C;D1;H3:8])-[O;H0;D2;+0:9]-[CH2;D2;+0:1]-[C:2](-[OH;D1;+0:4])-[CH2;D2;+0:3]-[N;H0;D3;+0:14]1-[C:10]-[C:11]-[C:12]-[C:13]-1
82.6
[{"value": 82.6, "product": "CC(C)(OCC(CN1CCCC1)O)C", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
50
CELSIUS
null
null
A mixture of 100.0 g (1.35 m) of tert.butyl alcohol and 51.4 g (1.35 m) of epichlorohydrin in 240 ml of xylenes was stirred and heated to 50° C. Tin (IV) chloride (3.5 g; 1.6 ml; 0.031 m) was added all at once and the reaction mixture immediately exothermed to about 100° C. The reaction mixture was stirred at about 50°...
10.6084/m9.figshare.5104873.v1
null
Primary halide.Ether.Tertiary alcohol.Secondary amine
Ether.Secondary alcohol.Tertiary amine
C1CCNC1.C1CO1
C1CC[NH]C1
C1CC[NH]C1
HCl
[Sn](Cl)(Cl)(Cl)Cl.O
50
null
C1CCNC1.CC(C)(C)O.ClCC1CO1>[Sn](Cl)(Cl)(Cl)Cl.O>CC(C)(C)OCC(O)CN1CCCC1
ord_dataset-01dbb772c5e249108f0b191ed17a2c0c
ord-241aa2d333114c3fb4a89c919eca50fd
CC(C)(C)OCC(O)CN1CCCC1.ClP(Cl)(Cl)(Cl)Cl>>CC(C)(C)OCC(Cl)CN1CCCC1
CC(C)(OCC(CN1CCCC1)O)C.Cl.P(Cl)(Cl)(Cl)(Cl)Cl>>ClC(CN1CCCC1)COC(C)(C)C
O[CH:7]([CH2:6][O:5][C:2]([CH3:1])([CH3:3])[CH3:4])[CH2:9][N:10]1[CH2:11][CH2:12][CH2:13][CH2:14]1.ClP(Cl)(Cl)(Cl)[Cl:8]>>[CH3:1][C:2]([CH3:3])([CH3:4])[O:5][CH2:6][CH:7]([Cl:8])[CH2:9][N:10]1[CH2:11][CH2:12][CH2:13][CH2:14]1
CC(C)(C)OCC(O)CN1CCCC1.ClP(Cl)(Cl)(Cl)Cl
CC(C)(C)OCC(Cl)CN1CCCC1
null
null
C1(=CC=CC=C1)C.O1CCCC1
Functional Group Interconversion
Alcohol to chloride_Other
ed0947fcf0a870fa4568d74e29e264525d0acf781c20c116470537e8cf1d911a
495868b18ac37eabad313a8861412e57f019fb3569a2b2e50afa3ee29413ec02
C1CCNC1
Cl-P(-Cl)(-Cl)(-Cl)-[Cl;H0;D1;+0:1].O-[CH;D3;+0:2](-[C:3]-[#8:4]-[C:5](-[C;D1;H3:6])(-[C;D1;H3:7])-[C;D1;H3:8])-[C:9]-[#7:10]>>[#7:10]-[C:9]-[CH;D3;+0:2](-[Cl;H0;D1;+0:1])-[C:3]-[#8:4]-[C:5](-[C;D1;H3:6])(-[C;D1;H3:7])-[C;D1;H3:8]
null
[]
null
null
1.5
HOUR
To a stirred, cooled suspension of 34.7 g (0.167 ml) of phosphorous pentachloride in 20 ml of dry toluene (argon atmosphere) was added a solution of 31.93 g (0.159 m) of 1-[3-(1,1-dimethylethoxy)-2-hydroxypropyl]pyrrolidine (the product of Example 13a) and excess hydrogen chloride (gas) in 46 ml of dry toluene and 50 m...
10.6084/m9.figshare.5104873.v1
null
Secondary alcohol
Secondary halide
null
null
C1CC[NH]C1
HCl
C1(=CC=CC=C1)C.O1CCCC1
null
1.5
CC(C)(C)OCC(O)CN1CCCC1.ClP(Cl)(Cl)(Cl)Cl>C1(=CC=CC=C1)C.O1CCCC1>CC(C)(C)OCC(Cl)CN1CCCC1
ord_dataset-01dbb772c5e249108f0b191ed17a2c0c
ord-218fc6652d2242c19817433db7fef78c
NCCCCl.c1cnc2c(c1)CCCC2>>NCCCC1CCCc2cccnc21
N1=CC=CC=2CCCCC12.[NH2-].[Na+].Cl.ClCCCN>>N1=CC=CC=2CCCC(C12)CCCN
Cl[CH2:4][CH2:3][CH2:2][NH2:1].[CH2:5]1[CH2:6][CH2:7][CH2:8][c:9]2[cH:10][cH:11][cH:12][n:13][c:14]21>>[NH2:1][CH2:2][CH2:3][CH2:4][CH:5]1[CH2:6][CH2:7][CH2:8][c:9]2[cH:10][cH:11][cH:12][n:13][c:14]21
NCCCCl.c1cnc2c(c1)CCCC2
NCCCC1CCCc2cccnc21
null
null
N
C-C Coupling
OtherReaction
b6764dd5aaa2dc3bd963b96096138e9182d18bb5e7c8dab9ac20b36892d5bd4b
f5e5e22797736d188bba28deb76a4cee8e4fee4dca04fe24f733d2ee68a23361
c1cnc2c(c1)CCCC2
Cl-[CH2;D2;+0:1]-[C:2]-[C:3].[C:4]-[C:5]-[CH2;D2;+0:6]-[c:7](:[c:8]):[#7;a:9]:[c:10]>>[C:3]-[C:2]-[CH2;D2;+0:1]-[CH;D3;+0:6](-[C:5]-[C:4])-[c:7](:[c:8]):[#7;a:9]:[c:10]
26.5
[{"value": 26.5, "product": "N1=CC=CC=2CCCC(C12)CCCN", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
2
HOUR
5,6,7,8-Tetrahydroquinoline (20 g) was added quickly to sodamide (17.6 g) in liquid ammonia (250 ml) to give a dark red coloured solution. 3-Chloropropylamine hydrochloride (28.9 g) was added in portions over four hours when loss of colour was permanent after which the reaction was stirred for a further 2 hours and the...
10.6084/m9.figshare.5104873.v1
null
Primary halide
null
c1cnc2c(c1)CCCC2
c1cnc2c(c1)CCCC2
c1cnc2c(c1)CCCC2
HCl
N
null
2
NCCCCl.c1cnc2c(c1)CCCC2>N>NCCCC1CCCc2cccnc21
ord_dataset-01dbb772c5e249108f0b191ed17a2c0c
ord-9fa178249b754b389254ccf16bc7859d
Cc1ccc(Cc2c[nH]c(N[N+](=O)[O-])nc2=O)cn1.NCCCC1CCCc2cccnc21>>Cc1ccc(Cc2c[nH]c(NCCCC3CCCc4cccnc43)nc2=O)cn1
N1=CC=CC=2CCCC(C12)CCCN.[N+](=O)([O-])NC=1NC=C(C(N1)=O)CC=1C=NC(=CC1)C>>N1=CC=CC=2CCCC(C12)CCCNC=1NC=C(C(N1)=O)CC=1C=NC(=CC1)C
O=[N+]([O-])N[c:10]1[nH:9][cH:8][c:7]([CH2:6][c:5]2[cH:4][cH:3][c:2]([CH3:1])[n:29][cH:28]2)[c:26](=[O:27])[n:25]1.[NH2:11][CH2:12][CH2:13][CH2:14][CH:15]1[CH2:16][CH2:17][CH2:18][c:19]2[cH:20][cH:21][cH:22][n:23][c:24]21>>[CH3:1][c:2]1[cH:3][cH:4][c:5]([CH2:6][c:7]2[cH:8][nH:9][c:10]([NH:11][CH2:12][CH2:13][CH2:14][CH...
Cc1ccc(Cc2c[nH]c(N[N+](=O)[O-])nc2=O)cn1.NCCCC1CCCc2cccnc21
Cc1ccc(Cc2c[nH]c(NCCCC3CCCc4cccnc43)nc2=O)cn1
null
null
N1=CC=CC=C1
Functional Group Interconversion
OtherReaction
05b684912773000dd80e55082a7a1b852822633f01eaa1fe214d84d8b29bbd58
a08d030a1a70ff4a445173118d028d17232424f5644d46118c3f0ed4772c2485
O=c1nc(NCCCC2CCCc3cccnc32)[nH]cc1Cc1cccnc1
O=[N+](-[O-])-N-[c;H0;D3;+0:1](:[#7;a:2]:[c:3]):[#7;a:4]:[c:5].[C:6]-[C:7]-[NH2;D1;+0:8]>>[C:6]-[C:7]-[NH;D2;+0:8]-[c;H0;D3;+0:1](:[#7;a:2]:[c:3]):[#7;a:4]:[c:5]
26.4
[{"value": 26.4, "product": "N1=CC=CC=2CCCC(C12)CCCNC=1NC=C(C(N1)=O)CC=1C=NC(=CC1)C", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
null
null
A solution of 3-(5,6,7,8-tetrahydroquinol-8-yl)-propylamine (0.75 g, 0.0038 mole) and 2-nitroamino-5-(6-methylpyrid-3-ylmethyl)-4(1H)-pyrimidone (0.99 g, 0.0037 mole) in pyridine (1 ml) was refluxed for 8 hr and evaporated to dryness. The residue was chromatographed on silica in 10% MeOH/CHCl3 then dissolved in hot CHC...
10.6084/m9.figshare.5104873.v1
null
Hydrazine.Primary amine
Secondary amine
c1cncnc1
c1cncnc1
c1ccncc1.c1cncnc1.c1cnc2c(c1)CCCC2
HO-
N1=CC=CC=C1
null
null
Cc1ccc(Cc2c[nH]c(N[N+](=O)[O-])nc2=O)cn1.NCCCC1CCCc2cccnc21>N1=CC=CC=C1>Cc1ccc(Cc2c[nH]c(NCCCC3CCCc4cccnc43)nc2=O)cn1
ord_dataset-01dbb772c5e249108f0b191ed17a2c0c
ord-ecedeae11bc2433581aed340c21acce6
Brc1cncnc1.COC(=O)c1ccc(Cl)cc1Cl>>O=C(c1cncnc1)c1ccc(Cl)cc1Cl
C(CCC)[Li].[Cl-].[NH4+].ClC1=C(C(=O)OC)C=CC(=C1)Cl.BrC=1C=NC=NC1>>ClC1=C(C(=O)C=2C=NC=NC2)C=CC(=C1)Cl
Br[c:3]1[cH:4][n:5][cH:6][n:7][cH:8]1.CO[C:2](=[O:1])[c:9]1[cH:10][cH:11][c:12]([Cl:13])[cH:14][c:15]1[Cl:16]>>[O:1]=[C:2]([c:3]1[cH:4][n:5][cH:6][n:7][cH:8]1)[c:9]1[cH:10][cH:11][c:12]([Cl:13])[cH:14][c:15]1[Cl:16]
Brc1cncnc1.COC(=O)c1ccc(Cl)cc1Cl
O=C(c1cncnc1)c1ccc(Cl)cc1Cl
null
null
CCCCCC.O1CCCC1.C(C)OCC
C-C Coupling
Ester and halide to ketone
bb0648e8f53cb690526a8f718157b4e43d22f41b3fb2a22a100bc7b75c3830db
7000e6fa6236297c1c515ebeaf5c7ba17704e006a4336e184f2503c0f1949baf
O=C(c1ccccc1)c1cncnc1
Br-[c;H0;D3;+0:1]1:[c:2]:[#7;a:3]:[c:4]:[#7;a:5]:[c:6]:1.C-O-[C;H0;D3;+0:7](=[O;D1;H0:8])-[c:9](:[c:10]):[c:11]>>[O;D1;H0:8]=[C;H0;D3;+0:7](-[c:9](:[c:10]):[c:11])-[c;H0;D3;+0:1]1:[c:2]:[#7;a:3]:[c:4]:[#7;a:5]:[c:6]:1
null
[]
null
null
0.5
HOUR
61.8 g (0.3 mole) of methyl 2,4-dichlorobenzoate and 52.2 g (0.33 mole) of 5-bromopyrimidine are dissolved in a mixture of 400 ml of tetrahydrofuran and 200 ml of diethyl ether. After the addition of 30 g of molecular sieve, the reaction mixture is stirred for 1/2 hour at room temperature and then cooled to about -120°...
10.6084/m9.figshare.5104873.v1
null
Aromatic halide.Ester
Ketone
c1cncnc1
c1cncnc1
c1cncnc1.c1ccccc1
HBr
CCCCCC.O1CCCC1.C(C)OCC
null
0.5
Brc1cncnc1.COC(=O)c1ccc(Cl)cc1Cl>CCCCCC.O1CCCC1.C(C)OCC>O=C(c1cncnc1)c1ccc(Cl)cc1Cl
ord_dataset-01dbb772c5e249108f0b191ed17a2c0c
ord-21579b9c6dbe424cb126459426052c6c
Clc1ncc(Br)cn1.Nc1ccc(O)c(Cl)c1>>Nc1ccc(Oc2ncc(Br)cn2)c(Cl)c1
BrC=1C=NC(=NC1)Cl.NC1=CC(=C(C=C1)O)Cl.C([O-])([O-])=O.[K+].[K+].CS(=O)C>>BrC=1C=NC(=NC1)OC1=C(C=C(N)C=C1)Cl
Cl[c:7]1[n:8][cH:9][c:10]([Br:11])[cH:12][n:13]1.[NH2:1][c:2]1[cH:3][cH:4][c:5]([OH:6])[c:14]([Cl:15])[cH:16]1>>[NH2:1][c:2]1[cH:3][cH:4][c:5]([O:6][c:7]2[n:8][cH:9][c:10]([Br:11])[cH:12][n:13]2)[c:14]([Cl:15])[cH:16]1
Clc1ncc(Br)cn1.Nc1ccc(O)c(Cl)c1
Nc1ccc(Oc2ncc(Br)cn2)c(Cl)c1
null
null
O
Heteroatom Alkylation and Arylation
Williamson Ether Synthesis
38da1e480b17968341fc50d07104da93d31f20765e3b36e5a0790cb6b1d88a10
27e9a6bab4e3ed54aeb6be4d84cb1c0170208288795e252a46e57e44ecc064f0
c1ccc(Oc2ncccn2)cc1
Cl-[c;H0;D3;+0:1](:[#7;a:2]:[c:3]):[#7;a:4]:[c:5].[OH;D1;+0:6]-[c:7](:[c:8]):[c:9]>>[c:3]:[#7;a:2]:[c;H0;D3;+0:1](-[O;H0;D2;+0:6]-[c:7](:[c:8]):[c:9]):[#7;a:4]:[c:5]
62.6
[{"value": 62.6, "product": "BrC=1C=NC(=NC1)OC1=C(C=C(N)C=C1)Cl", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
null
null
Into a flask, 7.00 g of 5-bromo-2-chloropyrimidine, 5.19 g of 4-amino-2-chlorophenol, 9.98 g of potassium carbonate and 70 ml of dimethylsulfoxide were introduced, and reacted in a nitrogen atmosphere at 120° C. for 1.5 hours under stirring. After the completion of the reaction, the product was poured into water, and e...
10.6084/m9.figshare.5104873.v1
null
Aromatic halide.Aromatic alcohol
Ether
c1cncnc1
c1cncnc1
c1ccccc1.c1cncnc1
HCl
O
null
null
Clc1ncc(Br)cn1.Nc1ccc(O)c(Cl)c1>O>Nc1ccc(Oc2ncc(Br)cn2)c(Cl)c1
ord_dataset-01dbb772c5e249108f0b191ed17a2c0c
ord-5d8975024a1740ce98c9290e59b3aec3
Nc1ccc(Oc2ncc(Br)cn2)c(Cl)c1.O=C=NC(=O)c1ccccc1[N+](=O)[O-]>>O=C(NC(=O)c1ccccc1[N+](=O)[O-])Nc1ccc(Oc2ncc(Br)cn2)c(Cl)c1
CO.BrC=1C=NC(=NC1)OC1=C(C=C(N)C=C1)Cl.[N+](=O)([O-])C1=C(C(=O)N=C=O)C=CC=C1.O>>[N+](=O)([O-])C1=C(C(=O)NC(=O)NC2=CC(=C(C=C2)OC2=NC=C(C=N2)Br)Cl)C=CC=C1
[NH2:15][c:16]1[cH:17][cH:18][c:19]([O:20][c:21]2[n:22][cH:23][c:24]([Br:25])[cH:26][n:27]2)[c:28]([Cl:29])[cH:30]1.[O:1]=[C:2]=[N:3][C:4](=[O:5])[c:6]1[cH:7][cH:8][cH:9][cH:10][c:11]1[N+:12](=[O:13])[O-:14]>>[O:1]=[C:2]([NH:3][C:4](=[O:5])[c:6]1[cH:7][cH:8][cH:9][cH:10][c:11]1[N+:12](=[O:13])[O-:14])[NH:15][c:16]1[cH:...
Nc1ccc(Oc2ncc(Br)cn2)c(Cl)c1.O=C=NC(=O)c1ccccc1[N+](=O)[O-]
O=C(NC(=O)c1ccccc1[N+](=O)[O-])Nc1ccc(Oc2ncc(Br)cn2)c(Cl)c1
null
null
O1CCOCC1
Acylation
Urea synthesis via isocyanate and primary amine
d39cd7dc52a79bb265ff8ef61ef7bf9dc7f7b5fb0150fcb4881bdfb18ab9c380
a5dc801930c765d2a435a0a2973e50163c305ba8e7641d6adbcc1550b7b96de7
O=C(NC(=O)c1ccccc1)Nc1ccc(Oc2ncccn2)cc1
[NH2;D1;+0:1]-[c:2](:[c:3]):[c:4].[O;D1;H0:5]=[C;H0;D2;+0:6]=[N;H0;D2;+0:7]-[C:8](=[O;D1;H0:9])-[c:10]>>[O;D1;H0:5]=[C;H0;D3;+0:6](-[NH;D2;+0:1]-[c:2](:[c:3]):[c:4])-[NH;D2;+0:7]-[C:8](=[O;D1;H0:9])-[c:10]
84.5
[{"value": 84.5, "product": "[N+](=O)([O-])C1=C(C(=O)NC(=O)NC2=CC(=C(C=C2)OC2=NC=C(C=N2)Br)Cl)C=CC=C1", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
null
null
Into a flask, a solution obtained by dissolving 6.80 g of the above 4-(5-bromo-2-pyrimidinyloxy)-3-chloroaniline in 30 ml of dioxane, was introduced, and a solution obtained by dissolving 5.76 g of 2-nitrobenzoylisocyanate in 30 ml of dioxane, was dropwise added thereto, and then the mixture was reacted at room tempera...
10.6084/m9.figshare.5104873.v1
null
Isocyanate.Primary amine
Urea
null
null
c1ccccc1.c1ccccc1.c1cncnc1
null
O1CCOCC1
null
null
Nc1ccc(Oc2ncc(Br)cn2)c(Cl)c1.O=C=NC(=O)c1ccccc1[N+](=O)[O-]>O1CCOCC1>O=C(NC(=O)c1ccccc1[N+](=O)[O-])Nc1ccc(Oc2ncc(Br)cn2)c(Cl)c1
ord_dataset-01dbb772c5e249108f0b191ed17a2c0c
ord-9d1b517cc1984e3fb05e9d6f78f2916e
Clc1cnc(Cl)nc1.Nc1ccc(O)c(Cl)c1>>Nc1ccc(Oc2ncc(Cl)cn2)c(Cl)c1
[N+](=O)([O-])C1=C(C(=O)NC(=O)NC2=CC(=C(C=C2)OC2=NC=C(C=N2)Cl)Cl)C=CC=C1.ClC1=NC=C(C=N1)Cl.NC1=CC(=C(C=C1)O)Cl.C([O-])([O-])=O.[K+].[K+]>>ClC=1C=C(N)C=CC1OC1=NC=C(C=N1)Cl
Cl[c:7]1[n:8][cH:9][c:10]([Cl:11])[cH:12][n:13]1.[NH2:1][c:2]1[cH:3][cH:4][c:5]([OH:6])[c:14]([Cl:15])[cH:16]1>>[NH2:1][c:2]1[cH:3][cH:4][c:5]([O:6][c:7]2[n:8][cH:9][c:10]([Cl:11])[cH:12][n:13]2)[c:14]([Cl:15])[cH:16]1
Clc1cnc(Cl)nc1.Nc1ccc(O)c(Cl)c1
Nc1ccc(Oc2ncc(Cl)cn2)c(Cl)c1
null
null
CS(=O)C.O
Heteroatom Alkylation and Arylation
Williamson Ether Synthesis
38da1e480b17968341fc50d07104da93d31f20765e3b36e5a0790cb6b1d88a10
27e9a6bab4e3ed54aeb6be4d84cb1c0170208288795e252a46e57e44ecc064f0
c1ccc(Oc2ncccn2)cc1
Cl-[c;H0;D3;+0:1](:[#7;a:2]:[c:3]):[#7;a:4]:[c:5].[OH;D1;+0:6]-[c:7](:[c:8]):[c:9]>>[c:3]:[#7;a:2]:[c;H0;D3;+0:1](-[O;H0;D2;+0:6]-[c:7](:[c:8]):[c:9]):[#7;a:4]:[c:5]
null
[]
null
null
null
null
N-(2-nitrobenzoyl)-N'-[3-chloro-4-(5-chloro-2-pyrimidinyloxy)phenyl]urea (1) Into a flask, 1.50 g of 2,5-dichloropyrimidine, 1.45 g of 4-amino-2-chlorophenol, 2.76 g of potassium carbonate and 15 ml of dimethylsulfoxide, were introduced, and reacted in a nitrogen atmosphere at 100° C. for 1.5 hours under stirring. Afte...
10.6084/m9.figshare.5104873.v1
null
Aromatic halide.Aromatic alcohol
Ether
c1cncnc1
c1cncnc1
c1ccccc1.c1cncnc1
HCl
CS(=O)C.O
null
null
Clc1cnc(Cl)nc1.Nc1ccc(O)c(Cl)c1>CS(=O)C.O>Nc1ccc(Oc2ncc(Cl)cn2)c(Cl)c1
ord_dataset-01dbb772c5e249108f0b191ed17a2c0c
ord-7ff718f3b7e94c629eff1d63f4573f1b
Nc1ccc(Oc2ncc(Br)cn2)c(Cl)c1.O=C(Cl)Cl>>O=C=Nc1ccc(Oc2ncc(Br)cn2)c(Cl)c1
C(=O)(Cl)Cl.BrC=1C=NC(=NC1)OC1=C(C=C(N)C=C1)Cl>>BrC=1C=NC(=NC1)OC1=C(C=C(C=C1)N=C=O)Cl
[NH2:3][c:4]1[cH:5][cH:6][c:7]([O:8][c:9]2[n:10][cH:11][c:12]([Br:13])[cH:14][n:15]2)[c:16]([Cl:17])[cH:18]1.Cl[C:2](Cl)=[O:1]>>[O:1]=[C:2]=[N:3][c:4]1[cH:5][cH:6][c:7]([O:8][c:9]2[n:10][cH:11][c:12]([Br:13])[cH:14][n:15]2)[c:16]([Cl:17])[cH:18]1
Nc1ccc(Oc2ncc(Br)cn2)c(Cl)c1.O=C(Cl)Cl
O=C=Nc1ccc(Oc2ncc(Br)cn2)c(Cl)c1
null
null
C(C)(=O)OCC
Miscellaneous
OtherReaction
7d3fae5ca5d4875eff5b8b9cc12bb45e992207dcc8962ac035cf5aaf63f27286
5e78fe62a292da2c55590df217f7e190c26df27095ff0827e6cc86b7659890bd
c1ccc(Oc2ncccn2)cc1
Cl-[C;H0;D3;+0:1](-Cl)=[O;D1;H0:2].[NH2;D1;+0:3]-[c:4](:[c:5]):[c:6]>>[O;D1;H0:2]=[C;H0;D2;+0:1]=[N;H0;D2;+0:3]-[c:4](:[c:5]):[c:6]
95.1
[{"value": 95.1, "product": "BrC=1C=NC(=NC1)OC1=C(C=C(C=C1)N=C=O)Cl", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
null
null
Into a flask, a solution of 0.02 mol of phosgene in 30 ml of ethyl acetate was introduced. To this solution, a solution of 3 g of 4-(5-bromo-2-pyrimidinyloxy)-3-chloroaniline in 10 ml of ethyl acetate was dropwise added at room temperature. The mixture was reacted at room temperature for 3 hours under stirring and furt...
10.6084/m9.figshare.5104873.v1
null
Acyl halide.Acyl halide.Primary amine
Isocyanate
null
null
c1ccccc1.c1cncnc1
HCl
C(C)(=O)OCC
null
null
Nc1ccc(Oc2ncc(Br)cn2)c(Cl)c1.O=C(Cl)Cl>C(C)(=O)OCC>O=C=Nc1ccc(Oc2ncc(Br)cn2)c(Cl)c1
ord_dataset-01dbb772c5e249108f0b191ed17a2c0c
ord-4dcca75acd3843ae9e867d6f1684e2bb
O=C(O)CCCCC[P+](c1ccccc1)(c1ccccc1)c1ccccc1.O=C(c1ccccc1)c1cccnc1>>O=C(O)CCCC/C=C(/c1ccccc1)c1cccnc1
[Br-].C(=O)(O)CCCCC[P+](C1=CC=CC=C1)(C1=CC=CC=C1)C1=CC=CC=C1.CS(=O)C.[H-].[Na+].C(C1=CC=CC=C1)(=O)C=1C=NC=CC1>>N1=CC(=CC=C1)\C(=C/CCCCC(=O)O)\C1=CC=CC=C1
c1ccc([P+](c2ccccc2)(c2ccccc2)[CH2:8][CH2:7][CH2:6][CH2:5][CH2:4][C:2](=[O:1])[OH:3])cc1.O=[C:9]([c:10]1[cH:11][cH:12][cH:13][cH:14][cH:15]1)[c:16]1[cH:17][cH:18][cH:19][n:20][cH:21]1>>[O:1]=[C:2]([OH:3])[CH2:4][CH2:5][CH2:6][CH2:7]/[CH:8]=[C:9](/[c:10]1[cH:11][cH:12][cH:13][cH:14][cH:15]1)[c:16]1[cH:17][cH:18][cH:19][...
O=C(O)CCCCC[P+](c1ccccc1)(c1ccccc1)c1ccccc1.O=C(c1ccccc1)c1cccnc1
O=C(O)CCCC/C=C(/c1ccccc1)c1cccnc1
null
null
O.O1CCCC1
C-C Coupling
Wittig with Phosphonium
6dd0a5c38831fb7d6f247fdce547914e97c2a39af502d5696ce93cba92b782d4
06a42e352cf517302d592bf38a2fd11b220014e39071074dc7becb6ee0bee4b2
[CH]=C(c1ccccc1)c1cccnc1
O=[C;H0;D3;+0:1](-[c:2](:[c:3]):[c:4])-[c:5](:[c:6]):[c:7]:[#7;a:8]:[c:9].[C:10]-[C:11]-[CH2;D2;+0:12]-[P+](-c1:c:c:c:c:c:1)(-c1:c:c:c:c:c:1)-c1:c:c:c:c:c:1>>[C:10]-[C:11]/[CH;D2;+0:12]=[C;H0;D3;+0:1](/[c:2](:[c:3]):[c:4])-[c:5](:[c:6]):[c:7]:[#7;a:8]:[c:9]
80
[{"value": 79.0, "product": "N1=CC(=CC=C1)\\C(=C/CCCCC(=O)O)\\C1=CC=CC=C1", "details": "PERCENTYIELD", "is_desired": false}, {"value": 80.0, "product": "N1=CC(=CC=C1)\\C(=C/CCCCC(=O)O)\\C1=CC=CC=C1", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
80
CELSIUS
5
MINUTE
To dimethylsulfoxide (40 ml) was added dropwise sodium hydride (1.0 g), and the mixture was heated at 80° C. for 30 minutes. The reaction mixture was cooled to room temperature, to which was added 5-carboxypentyltriphenyl phosphonium bromide (9.5 g, 21 mmoles) and the mixture was stirred for 5 minutes. To the reaction ...
10.6084/m9.figshare.5104873.v1
null
Ketone
null
c1ccccc1.c1ccccc1.c1ccccc1
null
c1ccccc1.c1ccncc1
HO-
O.O1CCCC1
80
0.083333
O=C(O)CCCCC[P+](c1ccccc1)(c1ccccc1)c1ccccc1.O=C(c1ccccc1)c1cccnc1>O.O1CCCC1>O=C(O)CCCC/C=C(/c1ccccc1)c1cccnc1
ord_dataset-01dbb772c5e249108f0b191ed17a2c0c
ord-5655146716e448659bad88b9b85685fd
C=CC(O)(c1ccccc1)c1cccnc1.COC(=O)c1cccc(O)c1>>COC(=O)c1cccc(OCC=C(c2ccccc2)c2cccnc2)c1
P(Cl)(Cl)(Cl)(Cl)Cl.[H-].[Na+].OC=1C=C(C(=O)OC)C=CC1.C1(=CC=CC=C1)C(C=C)(O)C=1C=NC=CC1>>N1=CC(=CC=C1)C(=CCOC=1C=C(C(=O)OC)C=CC1)C1=CC=CC=C1
O[C:13]([CH:12]=[CH2:11])([c:14]1[cH:15][cH:16][cH:17][cH:18][cH:19]1)[c:20]1[cH:21][cH:22][cH:23][n:24][cH:25]1.[CH3:1][O:2][C:3](=[O:4])[c:5]1[cH:6][cH:7][cH:8][c:9]([OH:10])[cH:26]1>>[CH3:1][O:2][C:3](=[O:4])[c:5]1[cH:6][cH:7][cH:8][c:9]([O:10][CH2:11][CH:12]=[C:13]([c:14]2[cH:15][cH:16][cH:17][cH:18][cH:19]2)[c:20]...
C=CC(O)(c1ccccc1)c1cccnc1.COC(=O)c1cccc(O)c1
COC(=O)c1cccc(OCC=C(c2ccccc2)c2cccnc2)c1
null
null
ClCCl.CN(C=O)C
Heteroatom Alkylation and Arylation
OtherReaction
6dd1031b55c8988c52506353b9f12735a423d806dc625fb675a31a2e2a3f0c29
4b905ec47df6dc7f9816cc6f36157b531561efa990c5cc2eaa8ddf31db051e9d
C(COc1ccccc1)=C(c1ccccc1)c1cccnc1
O-[C;H0;D4;+0:1](-[CH;D2;+0:2]=[CH2;D1;+0:3])(-[c:4](:[c:5]):[c:6])-[c:7](:[c:8]):[c:9]:[#7;a:10]:[c:11].[OH;D1;+0:12]-[c:13](:[c:14]):[c:15]>>[c:5]:[c:4](-[C;H0;D3;+0:1](=[CH;D2;+0:2]-[CH2;D2;+0:3]-[O;H0;D2;+0:12]-[c:13](:[c:14]):[c:15])-[c:7](:[c:8]):[c:9]:[#7;a:10]:[c:11]):[c:6]
96.5
[{"value": 92.0, "product": "N1=CC(=CC=C1)C(=CCOC=1C=C(C(=O)OC)C=CC1)C1=CC=CC=C1", "details": "PERCENTYIELD", "is_desired": false}, {"value": 96.5, "product": "N1=CC(=CC=C1)C(=CCOC=1C=C(C(=O)OC)C=CC1)C1=CC=CC=C1", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
1
HOUR
Phosphorus pentachloride (3.0 g, 14.2 mmoles) was suspended in dichloromethane (4 ml). To the suspension was added dropwise a solution of 1-phenyl-1-(3-pyridyl)-2-propen-1-ol (2.0 g, 9.5 mmoles) in dichloromethane (20 ml) at 0° C., then the mixture was stirred for one hour at room temperature, followed by washing with ...
10.6084/m9.figshare.5104873.v1
null
Tertiary alcohol.Aromatic alcohol.Vinyl
Ether
null
null
c1ccccc1.c1ccccc1.c1ccncc1
HO-
ClCCl.CN(C=O)C
null
1
C=CC(O)(c1ccccc1)c1cccnc1.COC(=O)c1cccc(O)c1>ClCCl.CN(C=O)C>COC(=O)c1cccc(OCC=C(c2ccccc2)c2cccnc2)c1
ord_dataset-01dbb772c5e249108f0b191ed17a2c0c
ord-b8e8a0e44dc8447099988bc5cd8e65ec
COC(=O)c1cccc(OCC=C(c2ccccc2)c2cccnc2)c1>>O=C(O)c1cccc(OCC=C(c2ccccc2)c2cccnc2)c1
N1=CC(=CC=C1)C(=CCOC=1C=C(C(=O)OC)C=CC1)C1=CC=CC=C1.[OH-].[Na+].Cl>>N1=CC(=CC=C1)C(=CCOC=1C=C(C(=O)O)C=CC1)C1=CC=CC=C1
C[O:3][C:2](=[O:1])[c:4]1[cH:5][cH:6][cH:7][c:8]([O:9][CH2:10][CH:11]=[C:12]([c:13]2[cH:14][cH:15][cH:16][cH:17][cH:18]2)[c:19]2[cH:20][cH:21][cH:22][n:23][cH:24]2)[cH:25]1>>[O:1]=[C:2]([OH:3])[c:4]1[cH:5][cH:6][cH:7][c:8]([O:9][CH2:10][CH:11]=[C:12]([c:13]2[cH:14][cH:15][cH:16][cH:17][cH:18]2)[c:19]2[cH:20][cH:21][cH:...
COC(=O)c1cccc(OCC=C(c2ccccc2)c2cccnc2)c1
O=C(O)c1cccc(OCC=C(c2ccccc2)c2cccnc2)c1
null
null
CO.O
Deprotection
Ester saponification (methyl deprotection)
d872e08ad5c85a4add6cd04e6e987e73fead5f79b3f30ba61a81ba5029b29894
38ae1ee78433b9acfb0390501446149c80f88f23ac2d84c60b3369bdab75cec9
C(COc1ccccc1)=C(c1ccccc1)c1cccnc1
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]
80
[{"value": 80.0, "product": "N1=CC(=CC=C1)C(=CCOC=1C=C(C(=O)O)C=CC1)C1=CC=CC=C1", "details": "PERCENTYIELD", "is_desired": false}, {"value": 79.8, "product": "N1=CC(=CC=C1)C(=CCOC=1C=C(C(=O)O)C=CC1)C1=CC=CC=C1", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
60
CELSIUS
2
HOUR
Methyl 3-[3-(3-pyridyl)-3-phenyl-2-propenyloxy]benzoate (If-56, 1.5 g, 4.35 mmoles) was dissolved in a mixture of water (3 ml) and methanol (10 ml). To the solution was added sodium hydroxide (700 mg, 17.5 mmoles). The mixture was stirred for 2 hours at 60° C., which was then left standing for cooling. To the reaction ...
10.6084/m9.figshare.5104873.v1
null
Ester
Carboxylic acid
null
null
c1ccccc1.c1ccccc1.c1ccncc1
Other
CO.O
60
2
COC(=O)c1cccc(OCC=C(c2ccccc2)c2cccnc2)c1>CO.O>O=C(O)c1cccc(OCC=C(c2ccccc2)c2cccnc2)c1
ord_dataset-01dbb772c5e249108f0b191ed17a2c0c
ord-044f299de98846bab0cf25d80cf220f1
CCN(CC)CCn1nc2c3c(c(CO)ccc31)Sc1cc(Cl)ccc1-2>>Cl
N1=CC(=CC=C1)/C(=C/CCCCC(=O)O)/C1=CC=CC=C1.CCN(CC)CCN1C2=C3C(=C(C=C2)CO)SC4=C(C3=N1)C=CC(=C4)Cl>>Cl.N1=CC(=CC=C1)/C(=C/CCCCC(=O)O)/C1=CC=CC=C1
CCN(CC)CCn1nc2c3c(c(CO)ccc31)Sc1cc([Cl:1])ccc1-2>>[ClH:1]
CCN(CC)CCn1nc2c3c(c(CO)ccc31)Sc1cc(Cl)ccc1-2
Cl
null
null
Cl
Reduction
OtherReaction
7f6e9d0c2b31a05c545a6fe90c98490646ba31bf2fcf7da30c3d5d3bcae5a4b7
a8fe5a648487d7d872f64daf4ea9ebf311e852d3acc149475b7d310b975d36e4
null
C-C-N(-C-C)-C-C-n1:n:c2:c3:c(:c(-C-O):c:c:c:3:1)-S-c1:c:c(-[Cl;H0;D1;+0:1]):c:c:c:1-2>>[ClH;D0;+0:1]
null
[]
null
null
null
null
To (E)-7-(3-pyridyl)-7-phenyl-6-heptenoic acid (Ia-4, 300 mg was dissolved in 2N HCl (5 ml). The solution was concentrated under reduced pressure. Recrystallization of the resulting crystals from ethanol-isopropyl ether gave (E)-7-(3-pyridyl)-7-phenyl-6-heptenoic acid hydrochloride (Ii-75) (285 mg), m.p. 163°-165° C. P...
10.6084/m9.figshare.5104873.v1
null
Aromatic halide.Primary alcohol.Tertiary amine.Monosulfide
null
c1ccc2c(c1)Sc1cccc3[nH]nc2c13
null
null
Other
Cl
null
null
CCN(CC)CCn1nc2c3c(c(CO)ccc31)Sc1cc(Cl)ccc1-2>Cl>Cl
ord_dataset-01dbb772c5e249108f0b191ed17a2c0c
ord-f4d40c8105a54f1dabfdfe034ad81e84
O=C(O)CCCC/C=C(\c1ccccc1)c1cccnc1>>O=C([O-])CCCC/C=C(\c1ccccc1)c1cccnc1
N1=CC(=CC=C1)/C(=C/CCCCC(=O)O)/C1=CC=CC=C1.C(O)([O-])=O.[Na+]>>N1=CC(=CC=C1)/C(=C/CCCCC(=O)[O-])/C1=CC=CC=C1.[Na+]
[O:1]=[C:2]([OH:3])[CH2:4][CH2:5][CH2:6][CH2:7]/[CH:8]=[C:9](\[c:10]1[cH:11][cH:12][cH:13][cH:14][cH:15]1)[c:16]1[cH:17][cH:18][cH:19][n:20][cH:21]1>>[O:1]=[C:2]([O-:3])[CH2:4][CH2:5][CH2:6][CH2:7]/[CH:8]=[C:9](\[c:10]1[cH:11][cH:12][cH:13][cH:14][cH:15]1)[c:16]1[cH:17][cH:18][cH:19][n:20][cH:21]1
O=C(O)CCCC/C=C(\c1ccccc1)c1cccnc1
O=C([O-])CCCC/C=C(\c1ccccc1)c1cccnc1
null
null
O
Oxidation
Carboxylic acid to carboxylate
af9382a4a3fca177895c8a400271aa22025197fc08b983f9d71150044c1e6777
b3097057beeca787f1d4960a7ee432572ee7aecad541233195b0dbbc0f674e9c
[CH]=C(c1ccccc1)c1cccnc1
[C:1]-[C:2](=[O;D1;H0:3])-[OH;D1;+0:4]>>[C:1]-[C:2](-[O-;H0;D1:4])=[O;D1;H0:3]
55.7
[{"value": 55.7, "product": "N1=CC(=CC=C1)/C(=C/CCCCC(=O)[O-])/C1=CC=CC=C1.[Na+]", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
null
null
(E)-7-(3-pyridyl)-7-phenyl-6-heptenoic acid (Ia-4) (500 mg) and sodium hydrogen carbonate (160 mg) were added to water (5 ml) to make a homogeneous solution. The solution was concentrated under reduced pressure. The concentrate was pulverized by the use of ethanol-isopropylether to obtain sodium (E)-7-(3-pyridyl)-7-phe...
10.6084/m9.figshare.5104873.v1
null
Carboxylic acid
null
null
null
c1ccccc1.c1ccncc1
null
O
null
null
O=C(O)CCCC/C=C(\c1ccccc1)c1cccnc1>O>O=C([O-])CCCC/C=C(\c1ccccc1)c1cccnc1
ord_dataset-01dbb772c5e249108f0b191ed17a2c0c
ord-a74b6d8de3c74927ba4f80b2e8d86f3c
O=C(O)CCCCC[P+](c1ccccc1)(c1ccccc1)c1ccccc1.O=C(c1cccnc1)c1ccc2c(c1)OCO2>>O=C(O)CCCC/C=C(\c1cccnc1)c1ccc2c(c1)OCO2
C1OC=2C=C(C(=O)C=3C=NC=CC3)C=CC2O1.[H-].[Na+].CS(=O)C.[Br-].C(=O)(O)CCCCC[P+](C1=CC=CC=C1)(C1=CC=CC=C1)C1=CC=CC=C1>>C1OC=2C=C(C=CC2O1)/C(=C/CCCCC(=O)O)/C=1C=NC=CC1
c1ccc([P+](c2ccccc2)(c2ccccc2)[CH2:8][CH2:7][CH2:6][CH2:5][CH2:4][C:2](=[O:1])[OH:3])cc1.O=[C:9]([c:10]1[cH:11][cH:12][cH:13][n:14][cH:15]1)[c:16]1[cH:17][cH:18][c:19]2[c:20]([cH:21]1)[O:22][CH2:23][O:24]2>>[O:1]=[C:2]([OH:3])[CH2:4][CH2:5][CH2:6][CH2:7]/[CH:8]=[C:9](\[c:10]1[cH:11][cH:12][cH:13][n:14][cH:15]1)[c:16]1[...
O=C(O)CCCCC[P+](c1ccccc1)(c1ccccc1)c1ccccc1.O=C(c1cccnc1)c1ccc2c(c1)OCO2
O=C(O)CCCC/C=C(\c1cccnc1)c1ccc2c(c1)OCO2
null
null
O.O1CCCC1
C-C Coupling
Wittig with Phosphonium
6dd0a5c38831fb7d6f247fdce547914e97c2a39af502d5696ce93cba92b782d4
06a42e352cf517302d592bf38a2fd11b220014e39071074dc7becb6ee0bee4b2
[CH]=C(c1cccnc1)c1ccc2c(c1)OCO2
O=[C;H0;D3;+0:1](-[c:2](:[c:3]):[c:4]:[#7;a:5]:[c:6])-[c:7](:[c:8]):[c:9].[C:10]-[C:11]-[CH2;D2;+0:12]-[P+](-c1:c:c:c:c:c:1)(-c1:c:c:c:c:c:1)-c1:c:c:c:c:c:1>>[C:10]-[C:11]/[CH;D2;+0:12]=[C;H0;D3;+0:1](\[c:2](:[c:3]):[c:4]:[#7;a:5]:[c:6])-[c:7](:[c:8]):[c:9]
24.6
[{"value": 24.6, "product": "C1OC=2C=C(C=CC2O1)/C(=C/CCCCC(=O)O)/C=1C=NC=CC1", "details": "PERCENTYIELD", "is_desired": false}, {"value": 11.2, "product": "C1OC=2C=C(C=CC2O1)/C(=C/CCCCC(=O)O)/C=1C=NC=CC1", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
85
CELSIUS
null
null
Sodium hydride (1 g, 60% in oil) was added to dimethyl sulfoxide (25 ml) under nitrogen and the mixture was heated at 85° C. with stirring for an hour. The reaction mixture was cooled to room temperature and 5-carboxypentyltriphenylphosphonium bromide (5.2 g, 11 mmoles) was added gradually. The mixture was stirred for ...
10.6084/m9.figshare.5104873.v1
null
Ketone
null
c1ccccc1.c1ccccc1.c1ccccc1
null
c1ccncc1.c1ccc2c(c1)OCO2
HO-
O.O1CCCC1
85
null
O=C(O)CCCCC[P+](c1ccccc1)(c1ccccc1)c1ccccc1.O=C(c1cccnc1)c1ccc2c(c1)OCO2>O.O1CCCC1>O=C(O)CCCC/C=C(\c1cccnc1)c1ccc2c(c1)OCO2