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
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large_stringlengths
14
3.37k
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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-81005d9a5e474ae9811ee087317133f2
C1CNCCN1.ClCCCCc1ccc(Cl)cc1>>Clc1ccc(CCCCN2CCNCC2)cc1
ClC1=CC=C(C=C1)CCCCCl.N1CCNCC1>>ClC1=CC=C(C=C1)CCCCN1CCNCC1
[NH:10]1[CH2:11][CH2:12][NH:13][CH2:14][CH2:15]1.Cl[CH2:9][CH2:8][CH2:7][CH2:6][c:5]1[cH:4][cH:3][c:2]([Cl:1])[cH:17][cH:16]1>>[Cl:1][c:2]1[cH:3][cH:4][c:5]([CH2:6][CH2:7][CH2:8][CH2:9][N:10]2[CH2:11][CH2:12][NH:13][CH2:14][CH2:15]2)[cH:16][cH:17]1
C1CNCCN1.ClCCCCc1ccc(Cl)cc1
Clc1ccc(CCCCN2CCNCC2)cc1
null
null
C(C)O
Heteroatom Alkylation and Arylation
N-alkylation of secondary amines with alkyl halides
61ec49e5207aa33ebff7094bb66b1d997d4af14524931a8b3643ef7a94219a9a
523d37155b42c8dc851abeddadebb241cdd90bdf649ba750c35e13c8c752d7b0
c1ccc(CCCCN2CCNCC2)cc1
Cl-[CH2;D2;+0:1]-[C:2]-[C:3].[#7:4]1-[C:5]-[C:6]-[NH;D2;+0:7]-[C:8]-[C:9]-1>>[C:3]-[C:2]-[CH2;D2;+0:1]-[N;H0;D3;+0:7]1-[C:6]-[C:5]-[#7:4]-[C:9]-[C:8]-1
46.3
[{"value": 46.3, "product": "ClC1=CC=C(C=C1)CCCCN1CCNCC1", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
null
null
A mixture of 26.4 g of 4-(4-chlorophenyl)butyl chloride, 86.1 g of anhydrous piperazine and 250 ml of reagent ethanol was refluxed overnight. Solvent was evaporated from the product and the residue was chromatographed twice on silica with the eluant being CH2Cl2 /CH3OH/ammonium hydroxide (45:5:1). The first chromatogra...
10.6084/m9.figshare.5104873.v1
null
Primary halide.Secondary amine
Tertiary amine
C1CNCCN1
C1C[NH]CCN1
c1ccccc1.C1C[NH]CCN1
HCl
C(C)O
null
null
C1CNCCN1.ClCCCCc1ccc(Cl)cc1>C(C)O>Clc1ccc(CCCCN2CCNCC2)cc1
ord_dataset-01dbb772c5e249108f0b191ed17a2c0c
ord-13fda9fea57447eebddeaa653b8ac3a5
CCOC(=O)C(CN1CCN(CCCN2CCN(Cc3ccc(Cl)cc3)CC2)CC1)c1ccccc1.Cl.Cl>>Cl.Cl.O=C(O)C(CN1CCN(CCCN2CCN(Cc3ccc(Cl)cc3)CC2)CC1)c1ccccc1
Cl.Cl.Cl.Cl.ClC1=CC=C(CN2CCN(CC2)CCCN2CCN(CC2)CC(C2=CC=CC=C2)C(=O)OCC)C=C1.[OH-].[Na+]>>Cl.Cl.Cl.Cl.ClC1=CC=C(CN2CCN(CC2)CCCN2CCN(CC2)CC(C2=CC=CC=C2)C(=O)O)C=C1
CC[O:7][C:6](=[O:5])[CH:8]([CH2:9][N:10]1[CH2:11][CH2:12][N:13]([CH2:14][CH2:15][CH2:16][N:17]2[CH2:18][CH2:19][N:20]([CH2:21][c:22]3[cH:23][cH:24][c:25]([Cl:26])[cH:27][cH:28]3)[CH2:29][CH2:30]2)[CH2:31][CH2:32]1)[c:33]1[cH:34][cH:35][cH:36][cH:37][cH:38]1.[ClH:2].[ClH:4]>>[ClH:2].[ClH:4].[O:5]=[C:6]([OH:7])[CH:8]([CH...
CCOC(=O)C(CN1CCN(CCCN2CCN(Cc3ccc(Cl)cc3)CC2)CC1)c1ccccc1.Cl.Cl
Cl.Cl.O=C(O)C(CN1CCN(CCCN2CCN(Cc3ccc(Cl)cc3)CC2)CC1)c1ccccc1
null
null
C(C)O
Miscellaneous
OtherReaction
16eb0e22715fadede32e44259800ac2375ae7dbc609f9ec677d59917bae07bec
b51da43dbb7140dac708518f8dbf83c5b067214819134afdb3f427285d08d6f8
c1ccc(CCN2CCN(CCCN3CCN(Cc4ccccc4)CC3)CC2)cc1
C-C-[O;H0;D2;+0:1]-[C:2](-[C:3])=[O;D1;H0:4]>>[C:3]-[C:2](=[O;D1;H0:4])-[OH;D1;+0:1]
172
[{"value": 40.0, "product": "Cl.Cl.Cl.Cl.ClC1=CC=C(CN2CCN(CC2)CCCN2CCN(CC2)CC(C2=CC=CC=C2)C(=O)O)C=C1", "details": "PERCENTYIELD", "is_desired": false}, {"value": 172.0, "product": "Cl.Cl.Cl.Cl.ClC1=CC=C(CN2CCN(CC2)CCCN2CCN(CC2)CC(C2=CC=CC=C2)C(=O)O)C=C1", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
null
null
A suspension of 340 mg of 1-[4-(4-chlorobenzyl)-1-piperazinyl]-3-[4-(2-ethoxycarbonyl-2-phenylethyl)-1-piperazinyl]propane tetrahydrochloride in 10 ml of ethanol was treated with 1 ml of aqueous 5M sodium hydroxide and heated under reflux for 1 hour. The reaction mixture was evaporated to dryness under reduced pressure...
10.6084/m9.figshare.5104873.v1
null
Ester
Carboxylic acid
null
null
C1C[NH]CC[NH]1.C1C[NH]CC[NH]1.c1ccccc1.c1ccccc1
Other
C(C)O
null
null
CCOC(=O)C(CN1CCN(CCCN2CCN(Cc3ccc(Cl)cc3)CC2)CC1)c1ccccc1.Cl.Cl>C(C)O>Cl.Cl.O=C(O)C(CN1CCN(CCCN2CCN(Cc3ccc(Cl)cc3)CC2)CC1)c1ccccc1
ord_dataset-01dbb772c5e249108f0b191ed17a2c0c
ord-6991b219f52b4e25941ed6cba7871dad
CI.COc1ccc(-c2cc(=O)[nH]c(C)n2)cc1OC>>COc1ccc(-c2cc(=O)n(C)c(C)n2)cc1OC
O.CC(C)([O-])C.[K+].CI.COC=1C=C(C=CC1OC)C1=CC(NC(=N1)C)=O>>COC=1C=C(C=CC1OC)C1=CC(N(C(=N1)C)C)=O
I[CH3:12].[CH3:1][O:2][c:3]1[cH:4][cH:5][c:6](-[c:7]2[cH:8][c:9](=[O:10])[nH:11][c:13]([CH3:14])[n:15]2)[cH:16][c:17]1[O:18][CH3:19]>>[CH3:1][O:2][c:3]1[cH:4][cH:5][c:6](-[c:7]2[cH:8][c:9](=[O:10])[n:11]([CH3:12])[c:13]([CH3:14])[n:15]2)[cH:16][c:17]1[O:18][CH3:19]
CI.COc1ccc(-c2cc(=O)[nH]c(C)n2)cc1OC
COc1ccc(-c2cc(=O)n(C)c(C)n2)cc1OC
null
null
CN(C=O)C
Heteroatom Alkylation and Arylation
N-alkylation of secondary amines with alkyl halides
8b8b604c36c54bca847ea1bd1b7840d48f065047e5c951a27f860631728323c9
7a358c636daddc97c1fb4c29f378044d7eac3f01815d9966e599841f642d631a
O=c1cc(-c2ccccc2)nc[nH]1
I-[CH3;D1;+0:1].[C;D1;H3:2]-[c:3]1:[#7;a:4]:[c:5]:[c:6]:[c:7](=[O;D1;H0:8]):[nH;D2;+0:9]:1>>[C;D1;H3:2]-[c:3]1:[#7;a:4]:[c:5]:[c:6]:[c:7](=[O;D1;H0:8]):[n;H0;D3;+0:9]:1-[CH3;D1;+0:1]
65.3
[{"value": 65.3, "product": "COC=1C=C(C=CC1OC)C1=CC(N(C(=N1)C)C)=O", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
null
null
To a suspension of 3,4-dihydro-6-(3,4 dimethoxyphenyl)-2-methylpyrimidin-4-one (2.0 g) in N,N-dimethylformamide (20 ml) were added potassium tert.butoxide (1.08 g) and methyl iodide (1.0 ml), and stirred at ambient temperature for an hour. Resulting mixture was poured into water, and extracted with ethyl acetate. The o...
10.6084/m9.figshare.5104873.v1
null
null
null
c1ccncn1
c1cncnc1
c1ccccc1.c1cncnc1
HI
CN(C=O)C
null
null
CI.COc1ccc(-c2cc(=O)[nH]c(C)n2)cc1OC>CN(C=O)C>COc1ccc(-c2cc(=O)n(C)c(C)n2)cc1OC
ord_dataset-01dbb772c5e249108f0b191ed17a2c0c
ord-6d50e5f7c65748e8bdcac9917b03d8e2
COc1ccc(-c2cc(=O)[nH]c(C)n2)cc1OC.O=P(Cl)(Cl)Cl>>COc1ccc(-c2cc(Cl)nc(C)n2)cc1OC
COC=1C=C(C=CC1OC)C1=CC(NC(=N1)C)=O.P(=O)(Cl)(Cl)Cl>>ClC1=NC(=NC(=C1)C1=CC(=C(C=C1)OC)OC)C
O=[c:9]1[cH:8][c:7](-[c:6]2[cH:5][cH:4][c:3]([O:2][CH3:1])[c:16]([O:17][CH3:18])[cH:15]2)[n:14][c:12]([CH3:13])[nH:11]1.O=P(Cl)(Cl)[Cl:10]>>[CH3:1][O:2][c:3]1[cH:4][cH:5][c:6](-[c:7]2[cH:8][c:9]([Cl:10])[n:11][c:12]([CH3:13])[n:14]2)[cH:15][c:16]1[O:17][CH3:18]
COc1ccc(-c2cc(=O)[nH]c(C)n2)cc1OC.O=P(Cl)(Cl)Cl
COc1ccc(-c2cc(Cl)nc(C)n2)cc1OC
null
null
null
Functional Group Interconversion
OtherReaction
ab990d4cf4e29f4bfc1eed19f85a157586116cba28cf7e047e67e704b97886a0
3c4065ab4a8681675e06a527dcad54d701c7bfdcac9f73f87773b05034108934
c1ccc(-c2ccncn2)cc1
Cl-P(-Cl)(=O)-[Cl;H0;D1;+0:1].O=[c;H0;D3;+0:2]1:[c:3]:[c:4](-[c:5]):[#7;a:6]:[c:7](-[C;D1;H3:8]):[nH;D2;+0:9]:1>>[C;D1;H3:8]-[c:7]1:[#7;a:6]:[c:4](-[c:5]):[c:3]:[c;H0;D3;+0:2](-[Cl;H0;D1;+0:1]):[n;H0;D2;+0:9]:1
null
[]
null
null
2
HOUR
A suspension of 3,4-dihydro-6-(3,4-dimethoxyphenyl)-2-methylpyrimidin-4-one (2.4 g) in phosphorus oxychloride (20 ml) was refluxed for 2 hours, and evaporated. To the residue were added aqueous sodium bicarbonate solution and chloroform, and stirred at ambient temperature for 2 hours. The organic layer was obtained and...
10.6084/m9.figshare.5104873.v1
null
null
Aromatic halide
c1ccncn1
c1cncnc1
c1ccccc1.c1cncnc1
HCl
null
null
2
COc1ccc(-c2cc(=O)[nH]c(C)n2)cc1OC.O=P(Cl)(Cl)Cl>>COc1ccc(-c2cc(Cl)nc(C)n2)cc1OC
ord_dataset-01dbb772c5e249108f0b191ed17a2c0c
ord-5c3a5a99c48944198bf063c01ea01967
CCOC(=O)CC(=O)c1ccc(OC)c(OC)c1.Nc1ccccn1>>COc1ccc(-c2cc(=O)n3ccccc3n2)cc1OC
C(C1=CC(OC)=C(OC)C=C1)(=O)CC(=O)OCC.NC1=NC=CC=C1>>COC=1C=C(C=CC1OC)C=1N=C2N(C(C1)=O)C=CC=C2
CCO[C:9]([CH2:8][C:7](=O)[c:6]1[cH:5][cH:4][c:3]([O:2][CH3:1])[c:19]([O:20][CH3:21])[cH:18]1)=[O:10].[n:11]1[cH:12][cH:13][cH:14][cH:15][c:16]1[NH2:17]>>[CH3:1][O:2][c:3]1[cH:4][cH:5][c:6](-[c:7]2[cH:8][c:9](=[O:10])[n:11]3[cH:12][cH:13][cH:14][cH:15][c:16]3[n:17]2)[cH:18][c:19]1[O:20][CH3:21]
CCOC(=O)CC(=O)c1ccc(OC)c(OC)c1.Nc1ccccn1
COc1ccc(-c2cc(=O)n3ccccc3n2)cc1OC
null
null
null
Aromatic Heterocycle Formation
OtherReaction
18aaa9c9f1fc97f1276b7f3d8d51ea2f879273fca2a44162cb2a6bbc6598427f
65fdd7798538976255c7563b30d8ae7cc21639206d12c4373c064ac8a6ebaebc
O=c1cc(-c2ccccc2)nc2ccccn12
C-C-O-[C;H0;D3;+0:1](=[O;D1;H0:2])-[CH2;D2;+0:3]-[C;H0;D3;+0:4](=O)-[c;H0;D3;+0:5](:[c:6]:[c:7]):[c:8]:[c:9].[NH2;D1;+0:10]-[c:11](:[c:12]):[n;H0;D2;+0:13]:[c:14]:[c:15]>>[O;D1;H0:2]=[c;H0;D3;+0:1]1:[cH;D2;+0:3]:[c;H0;D3;+0:4](-[c;H0;D3;+0:5](:[c:6]:[c:7]):[c:8]:[c:9]):[n;H0;D2;+0:10]:[c:11](:[c:12]):[n;H0;D3;+0:13]:1:...
150.8
[{"value": 150.8, "product": "COC=1C=C(C=CC1OC)C=1N=C2N(C(C1)=O)C=CC=C2", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
100
CELSIUS
3
HOUR
Ethyl veratroylacetate (4.5 g) was added dropwise under stirring at 60°-70° C. to a suspension of 2-aminopyridine (0.84 g) in polyphosphoric acid (13.7 g). The reaction mixture was stirred at 100° C. for 3 hrs and poured into ice-water (50 ml). The aqueous solution was extracted with chloroform, washed with water, drie...
10.6084/m9.figshare.5104873.v1
null
Ketone.Ester.Primary amine
null
c1ccncc1
c1ccn2ccccc2n1
c1ccccc1.c1ccn2ccccc2n1
HO-
null
100
3
CCOC(=O)CC(=O)c1ccc(OC)c(OC)c1.Nc1ccccn1>>COc1ccc(-c2cc(=O)n3ccccc3n2)cc1OC
ord_dataset-01dbb772c5e249108f0b191ed17a2c0c
ord-53723e478eea4102a066bd715aecef75
COc1ccc(-c2cc(=Nc3c(C)cc(C)cc3C)n(C)c(=O)[nH]2)cc1OC.O=P(Cl)(Cl)Cl>>COc1ccc(-c2cc(=Nc3c(C)cc(C)cc3C)n(C)c(Cl)n2)cc1OC
COC=1C=C(C=CC1OC)C1=CC(N(C(N1)=O)C)=NC1=C(C=C(C=C1C)C)C.P(=O)(Cl)(Cl)Cl>>ClC1=NC(=CC(N1C)=NC1=C(C=C(C=C1C)C)C)C1=CC(=C(C=C1)OC)OC
O=[c:22]1[n:20]([CH3:21])[c:9](=[N:10][c:11]2[c:12]([CH3:13])[cH:14][c:15]([CH3:16])[cH:17][c:18]2[CH3:19])[cH:8][c:7](-[c:6]2[cH:5][cH:4][c:3]([O:2][CH3:1])[c:26]([O:27][CH3:28])[cH:25]2)[nH:24]1.O=P(Cl)(Cl)[Cl:23]>>[CH3:1][O:2][c:3]1[cH:4][cH:5][c:6](-[c:7]2[cH:8][c:9](=[N:10][c:11]3[c:12]([CH3:13])[cH:14][c:15]([CH3...
COc1ccc(-c2cc(=Nc3c(C)cc(C)cc3C)n(C)c(=O)[nH]2)cc1OC.O=P(Cl)(Cl)Cl
COc1ccc(-c2cc(=Nc3c(C)cc(C)cc3C)n(C)c(Cl)n2)cc1OC
null
null
null
Functional Group Interconversion
OtherReaction
ab990d4cf4e29f4bfc1eed19f85a157586116cba28cf7e047e67e704b97886a0
3c4065ab4a8681675e06a527dcad54d701c7bfdcac9f73f87773b05034108934
c1ccc(N=c2cc(-c3ccccc3)nc[nH]2)cc1
Cl-P(-Cl)(=O)-[Cl;H0;D1;+0:1].O=[c;H0;D3;+0:2]1:[nH;D2;+0:3]:[c:4](-[c:5]):[c:6]:[c:7]:[#7;a:8]:1-[C;D1;H3:9]>>[C;D1;H3:9]-[#7;a:8]1:[c:7]:[c:6]:[c:4](-[c:5]):[n;H0;D2;+0:3]:[c;H0;D3;+0:2]:1-[Cl;H0;D1;+0:1]
null
[]
null
null
null
null
To 3,4-dihydro-6-(3,4-dimethoxyphenyl)-3-methyl-4-(2,4,6-trimethylphenylimino)-2-(1H)pyrimidone (5.0 g) was added phosphorus oxychloride (50 ml). The mixture was refluxed for 7 hours and evaporated under reduced pressure. The resulting syrup was triturated in a mixture of ice and water, neutralized with aqueous sodium ...
10.6084/m9.figshare.5104873.v1
null
null
Aromatic halide
c1ccncn1
c1cncnc1
c1ccccc1.c1cncnc1.c1ccccc1
HCl
null
null
null
COc1ccc(-c2cc(=Nc3c(C)cc(C)cc3C)n(C)c(=O)[nH]2)cc1OC.O=P(Cl)(Cl)Cl>>COc1ccc(-c2cc(=Nc3c(C)cc(C)cc3C)n(C)c(Cl)n2)cc1OC
ord_dataset-01dbb772c5e249108f0b191ed17a2c0c
ord-be3baba0a63e43b69785207ba89bb350
COc1ccc(-c2cc(=Nc3c(C)cc(C)cc3C)n(C)c(Cl)n2)cc1OC>>COc1ccc(-c2cc(=Nc3c(C)cc(C)cc3C)n(C)cn2)cc1OC
ClC1=NC(=CC(N1C)=NC1=C(C=C(C=C1C)C)C)C1=CC(=C(C=C1)OC)OC>>COC=1C=C(C=CC1OC)C1=CC(N(C=N1)C)=NC1=C(C=C(C=C1C)C)C
Cl[c:22]1[n:20]([CH3:21])[c:9](=[N:10][c:11]2[c:12]([CH3:13])[cH:14][c:15]([CH3:16])[cH:17][c:18]2[CH3:19])[cH:8][c:7](-[c:6]2[cH:5][cH:4][c:3]([O:2][CH3:1])[c:25]([O:26][CH3:27])[cH:24]2)[n:23]1>>[CH3:1][O:2][c:3]1[cH:4][cH:5][c:6](-[c:7]2[cH:8][c:9](=[N:10][c:11]3[c:12]([CH3:13])[cH:14][c:15]([CH3:16])[cH:17][c:18]3[...
COc1ccc(-c2cc(=Nc3c(C)cc(C)cc3C)n(C)c(Cl)n2)cc1OC
COc1ccc(-c2cc(=Nc3c(C)cc(C)cc3C)n(C)cn2)cc1OC
null
[Pd]
C(C)O
Functional Group Interconversion
Aromatic dehalogenation
76895d15d2d466b89a30aacc2ef4edbb246f8c7b092db05f2443e4acbf4f85b3
56de34d4a44cb25d9380269ee5e138b0f24b40a3a0db22c5508049dc775a861f
c1ccc(N=c2cc(-c3ccccc3)nc[nH]2)cc1
Cl-[c;H0;D3;+0:1](:[#7;a:2]:[c:3]):[#7;a:4](-[C;D1;H3:5]):[c:6]>>[C;D1;H3:5]-[#7;a:4](:[c:6]):[cH;D2;+0:1]:[#7;a:2]:[c:3]
26.3
[{"value": 26.3, "product": "COC=1C=C(C=CC1OC)C1=CC(N(C=N1)C)=NC1=C(C=C(C=C1C)C)C", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
40
MINUTE
To a suspension of 2-chloro-3,4-dihydro-6-(3,4-dimethoxyphenyl)-3-methyl-4-(2,4,6-trimethylphenylimino)pyrimidine (1.5 g) in ethanol (20 ml) was added 10%-palladium on carbon (0.8 g). The mixture was stirred under hydrogen (1 atm) for 40 minutes. After removal of the catalist by filtration, the filtrate was evaporated ...
10.6084/m9.figshare.5104873.v1
null
Aromatic halide
null
c1cncnc1
c1cncnc1
c1ccccc1.c1cncnc1.c1ccccc1
Other
[Pd].C(C)O
null
0.666667
COc1ccc(-c2cc(=Nc3c(C)cc(C)cc3C)n(C)c(Cl)n2)cc1OC>[Pd].C(C)O>COc1ccc(-c2cc(=Nc3c(C)cc(C)cc3C)n(C)cn2)cc1OC
ord_dataset-01dbb772c5e249108f0b191ed17a2c0c
ord-1bd4c3ba7a204a948c9a3d8d4191dea3
CNCc1ccccc1.COc1ccc(-c2cc(=Nc3c(C)cc(C)cc3C)n(C)c(Cl)n2)cc1OC>>COc1ccc(-c2cc(=Nc3c(C)cc(C)cc3C)n(C)c(N(C)Cc3ccccc3)n2)cc1OC
ClC1=NC(=CC(N1C)=NC1=C(C=C(C=C1C)C)C)C1=CC(=C(C=C1)OC)OC.CNCC1=CC=CC=C1>>COC=1C=C(C=CC1OC)C1=CC(N(C(=N1)N(CC1=CC=CC=C1)C)C)=NC1=C(C=C(C=C1C)C)C
[NH:23]([CH3:24])[CH2:25][c:26]1[cH:27][cH:28][cH:29][cH:30][cH:31]1.Cl[c:22]1[n:20]([CH3:21])[c:9](=[N:10][c:11]2[c:12]([CH3:13])[cH:14][c:15]([CH3:16])[cH:17][c:18]2[CH3:19])[cH:8][c:7](-[c:6]2[cH:5][cH:4][c:3]([O:2][CH3:1])[c:34]([O:35][CH3:36])[cH:33]2)[n:32]1>>[CH3:1][O:2][c:3]1[cH:4][cH:5][c:6](-[c:7]2[cH:8][c:9]...
CNCc1ccccc1.COc1ccc(-c2cc(=Nc3c(C)cc(C)cc3C)n(C)c(Cl)n2)cc1OC
COc1ccc(-c2cc(=Nc3c(C)cc(C)cc3C)n(C)c(N(C)Cc3ccccc3)n2)cc1OC
null
null
C(Cl)(Cl)Cl.C(C)O
Heteroatom Alkylation and Arylation
Ullmann-Goldberg Substitution amine
8a13b42f4b06102b68f4963e65202071bf1d0630fbad1b11bbd8e99b9f9c8f34
b6b8e2cdb45054a35f5e8157d624f852c0601a09401556706e166b19536eb7a7
c1ccc(CNc2nc(-c3ccccc3)cc(=Nc3ccccc3)[nH]2)cc1
Cl-[c;H0;D3;+0:1](:[#7;a:2]:[c:3]):[#7;a:4](-[C;D1;H3:5]):[c:6].[C;D1;H3:7]-[NH;D2;+0:8]-[C:9]-[c:10]>>[C;D1;H3:5]-[#7;a:4](:[c:6]):[c;H0;D3;+0:1](-[N;H0;D3;+0:8](-[C;D1;H3:7])-[C:9]-[c:10]):[#7;a:2]:[c:3]
null
[]
null
null
null
null
To a suspension of 2-chloro-3,4-dihydro-6-(3,4-dimethoxyphenyl)-3-methyl-4-(2,4,6-trimethylphenylimino)pyrimidine (1.5 g) in ethanol (15 ml) was added N-methylbenzylamine (1.47 ml). The mixture was refluxed for 5 hours. The resulting suspension was dissolved in chloroform, washed with brine, dried over magnesium sulfat...
10.6084/m9.figshare.5104873.v1
null
Aromatic halide.Secondary amine
Tertiary amine
c1cncnc1
c1cncnc1
c1ccccc1.c1cncnc1.c1ccccc1.c1ccccc1
HCl
C(Cl)(Cl)Cl.C(C)O
null
null
CNCc1ccccc1.COc1ccc(-c2cc(=Nc3c(C)cc(C)cc3C)n(C)c(Cl)n2)cc1OC>C(Cl)(Cl)Cl.C(C)O>COc1ccc(-c2cc(=Nc3c(C)cc(C)cc3C)n(C)c(N(C)Cc3ccccc3)n2)cc1OC
ord_dataset-01dbb772c5e249108f0b191ed17a2c0c
ord-dc411ea16f934b7bbc3fdf11d0029adc
C1CNCCN1.COc1ccc(-c2cc(=Nc3c(C)cc(C)cc3C)n(C)c(Cl)n2)cc1OC>>COc1ccc(-c2cc(=Nc3c(C)cc(C)cc3C)n(C)c(N3CCNCC3)n2)cc1OC
ClC1=NC(=CC(N1C)=NC1=C(C=C(C=C1C)C)C)C1=CC(=C(C=C1)OC)OC.N1CCNCC1>>COC=1C=C(C=CC1OC)C1=CC(N(C(=N1)N1CCNCC1)C)=NC1=C(C=C(C=C1C)C)C
[NH:23]1[CH2:24][CH2:25][NH:26][CH2:27][CH2:28]1.Cl[c:22]1[n:20]([CH3:21])[c:9](=[N:10][c:11]2[c:12]([CH3:13])[cH:14][c:15]([CH3:16])[cH:17][c:18]2[CH3:19])[cH:8][c:7](-[c:6]2[cH:5][cH:4][c:3]([O:2][CH3:1])[c:31]([O:32][CH3:33])[cH:30]2)[n:29]1>>[CH3:1][O:2][c:3]1[cH:4][cH:5][c:6](-[c:7]2[cH:8][c:9](=[N:10][c:11]3[c:12...
C1CNCCN1.COc1ccc(-c2cc(=Nc3c(C)cc(C)cc3C)n(C)c(Cl)n2)cc1OC
COc1ccc(-c2cc(=Nc3c(C)cc(C)cc3C)n(C)c(N3CCNCC3)n2)cc1OC
null
null
C(C)O
Heteroatom Alkylation and Arylation
Ullmann-Goldberg Substitution amine
20777ae9d5a363a48071462fee2ac360794a4b33f519e76040bff714d38f1488
b6b8e2cdb45054a35f5e8157d624f852c0601a09401556706e166b19536eb7a7
c1ccc(N=c2cc(-c3ccccc3)nc(N3CCNCC3)[nH]2)cc1
Cl-[c;H0;D3;+0:1](:[#7;a:2]:[c:3]):[#7;a:4](-[C;D1;H3:5]):[c:6].[#7:7]1-[C:8]-[C:9]-[NH;D2;+0:10]-[C:11]-[C:12]-1>>[C;D1;H3:5]-[#7;a:4](:[c:6]):[c;H0;D3;+0:1](-[N;H0;D3;+0:10]1-[C:9]-[C:8]-[#7:7]-[C:12]-[C:11]-1):[#7;a:2]:[c:3]
57.3
[{"value": 57.3, "product": "COC=1C=C(C=CC1OC)C1=CC(N(C(=N1)N1CCNCC1)C)=NC1=C(C=C(C=C1C)C)C", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
null
null
To a suspension of 2-chloro-3,4-dihydro-6-(3,4-dimethoxyphenyl)-3-methyl-4-(2,4,6-trimethylphenylimino)pyrimidine (1.07 g) in ethanol (10 ml) was added piperazine (0.70 g). The mixture was refluxed for 3 hours, cooled to ambient temperature. The mixture was evaporated, and the residue was dissolved in chloroform and wa...
10.6084/m9.figshare.5104873.v1
null
Aromatic halide.Secondary amine
Tertiary amine
C1CNCCN1.c1cncnc1
c1cncnc1.C1C[NH]CCN1
c1ccccc1.c1cncnc1.c1ccccc1.C1C[NH]CCN1
HCl
C(C)O
null
null
C1CNCCN1.COc1ccc(-c2cc(=Nc3c(C)cc(C)cc3C)n(C)c(Cl)n2)cc1OC>C(C)O>COc1ccc(-c2cc(=Nc3c(C)cc(C)cc3C)n(C)c(N3CCNCC3)n2)cc1OC
ord_dataset-01dbb772c5e249108f0b191ed17a2c0c
ord-9fe523c9c62a46dba0a4c75868ed88c4
COc1ccc(-c2cc(=Nc3c(C)cc(C)cc3C)n(C)c(Cl)n2)cc1OC.NN>>COc1ccc(-c2cc(=Nc3c(C)cc(C)cc3C)n(C)c(NN)n2)cc1OC
ClC1=NC(=CC(N1C)=NC1=C(C=C(C=C1C)C)C)C1=CC(=C(C=C1)OC)OC.O.NN>>COC=1C=C(C=CC1OC)C1=CC(N(C(=N1)NN)C)=NC1=C(C=C(C=C1C)C)C
Cl[c:22]1[n:20]([CH3:21])[c:9](=[N:10][c:11]2[c:12]([CH3:13])[cH:14][c:15]([CH3:16])[cH:17][c:18]2[CH3:19])[cH:8][c:7](-[c:6]2[cH:5][cH:4][c:3]([O:2][CH3:1])[c:27]([O:28][CH3:29])[cH:26]2)[n:25]1.[NH2:23][NH2:24]>>[CH3:1][O:2][c:3]1[cH:4][cH:5][c:6](-[c:7]2[cH:8][c:9](=[N:10][c:11]3[c:12]([CH3:13])[cH:14][c:15]([CH3:16...
COc1ccc(-c2cc(=Nc3c(C)cc(C)cc3C)n(C)c(Cl)n2)cc1OC.NN
COc1ccc(-c2cc(=Nc3c(C)cc(C)cc3C)n(C)c(NN)n2)cc1OC
null
null
C(Cl)(Cl)Cl
Heteroatom Alkylation and Arylation
OtherReaction
a2442d505c92c8b71e523800797f0037c976f9785f57388464f754ec52db04ac
61806bbf8bb8981e140ee503663af0ef0e69dc4f34f6582f974a2e4218f7da88
c1ccc(N=c2cc(-c3ccccc3)nc[nH]2)cc1
Cl-[c;H0;D3;+0:1](:[#7;a:2]:[c:3]):[#7;a:4](-[C;D1;H3:5]):[c:6].[N;D1;H2:7]-[NH2;D1;+0:8]>>[C;D1;H3:5]-[#7;a:4](:[c:6]):[c;H0;D3;+0:1](-[NH;D2;+0:8]-[N;D1;H2:7]):[#7;a:2]:[c:3]
null
[]
null
null
null
null
To a suspension of 2-chloro-3,4-dihydro-6-(3,4-dimethoxyphenyl)-3-methyl-4-(2,4,6-trimethylphenylimino)pyrimidine (10.0 g) in chloroform (100 ml) was added hydrazine hydrate (3.66 ml). The mixture was refluxed for 6 hours. The reaction mixture was evaporated in vacuo. The residue was chromatographed on silica gel using...
10.6084/m9.figshare.5104873.v1
null
Hydrazine.Aromatic halide
Hydrazine
c1cncnc1
c1cncnc1
c1ccccc1.c1cncnc1.c1ccccc1
HCl
C(Cl)(Cl)Cl
null
null
COc1ccc(-c2cc(=Nc3c(C)cc(C)cc3C)n(C)c(Cl)n2)cc1OC.NN>C(Cl)(Cl)Cl>COc1ccc(-c2cc(=Nc3c(C)cc(C)cc3C)n(C)c(NN)n2)cc1OC
ord_dataset-01dbb772c5e249108f0b191ed17a2c0c
ord-354ca21a83634760aedd88119171dfa2
COc1ccc(-c2cc(=Nc3c(C)cc(C)cc3C)n(C)c(Cl)n2)cc1OC.NNC=O>>COc1ccc(-c2cc(=Nc3c(C)cc(C)cc3C)n(C)c(NNC=O)n2)cc1OC
ClC1=NC(=CC(N1C)=NC1=C(C=C(C=C1C)C)C)C1=CC(=C(C=C1)OC)OC.C(=O)NN>>COC=1C=C(C=CC1OC)C1=CC(N(C(=N1)NNC=O)C)=NC1=C(C=C(C=C1C)C)C
Cl[c:22]1[n:20]([CH3:21])[c:9](=[N:10][c:11]2[c:12]([CH3:13])[cH:14][c:15]([CH3:16])[cH:17][c:18]2[CH3:19])[cH:8][c:7](-[c:6]2[cH:5][cH:4][c:3]([O:2][CH3:1])[c:29]([O:30][CH3:31])[cH:28]2)[n:27]1.[NH2:23][NH:24][CH:25]=[O:26]>>[CH3:1][O:2][c:3]1[cH:4][cH:5][c:6](-[c:7]2[cH:8][c:9](=[N:10][c:11]3[c:12]([CH3:13])[cH:14][...
COc1ccc(-c2cc(=Nc3c(C)cc(C)cc3C)n(C)c(Cl)n2)cc1OC.NNC=O
COc1ccc(-c2cc(=Nc3c(C)cc(C)cc3C)n(C)c(NNC=O)n2)cc1OC
null
null
C(Cl)(Cl)Cl
Heteroatom Alkylation and Arylation
OtherReaction
05c8b509fbd3209f3d5e9d92885ea58a32d461019bf8f0b9c82cd4b4f5a05883
cc5a5df08bac6de192cb68c75e5cdf4d844dc944903b8c20fd785c59a832562d
c1ccc(N=c2cc(-c3ccccc3)nc[nH]2)cc1
Cl-[c;H0;D3;+0:1](:[#7;a:2]:[c:3]):[#7;a:4](-[C;D1;H3:5]):[c:6].[NH2;D1;+0:7]-[#7:8]-[C:9]=[O;D1;H0:10]>>[C;D1;H3:5]-[#7;a:4](:[c:6]):[c;H0;D3;+0:1](-[NH;D2;+0:7]-[#7:8]-[C:9]=[O;D1;H0:10]):[#7;a:2]:[c:3]
26.4
[{"value": 26.4, "product": "COC=1C=C(C=CC1OC)C1=CC(N(C(=N1)NNC=O)C)=NC1=C(C=C(C=C1C)C)C", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
null
null
To a suspension of 2-chloro-3,4-dihydro-6-(3,4-dimethoxyphenyl)-3-methyl-4-(2,4,6-trimethylphenylimino)pyrimidine (3.0 g) in chloroform (15 ml) was added formylhydrazine (1.36 g). The mixture was refluxed for 6 hours and cooled to ambient temperature. The resulting precipitates were filtered off and the filtrate was ev...
10.6084/m9.figshare.5104873.v1
null
Acylhydrazine.Aromatic halide
Acylhydrazine
c1cncnc1
c1cncnc1
c1ccccc1.c1cncnc1.c1ccccc1
HCl
C(Cl)(Cl)Cl
null
null
COc1ccc(-c2cc(=Nc3c(C)cc(C)cc3C)n(C)c(Cl)n2)cc1OC.NNC=O>C(Cl)(Cl)Cl>COc1ccc(-c2cc(=Nc3c(C)cc(C)cc3C)n(C)c(NNC=O)n2)cc1OC
ord_dataset-01dbb772c5e249108f0b191ed17a2c0c
ord-dd36e74f535546a1be9f4ec4be1e5354
COc1ccc(-c2cc(=Nc3c(C)cc(C)cc3C)n(C)c(N3CCNCC3)n2)cc1OC.O=C(Cl)c1ccc(F)cc1>>COc1ccc(-c2cc(=Nc3c(C)cc(C)cc3C)n(C)c(N3CCN(C(=O)c4ccc(F)cc4)CC3)n2)cc1OC
COC=1C=C(C=CC1OC)C1=CC(N(C(=N1)N1CCNCC1)C)=NC1=C(C=C(C=C1C)C)C.C(C)N(CC)CC.FC1=CC=C(C(=O)Cl)C=C1>>COC=1C=C(C=CC1OC)C1=CC(N(C(=N1)N1CCN(CC1)C(C1=CC=C(C=C1)F)=O)C)=NC1=C(C=C(C=C1C)C)C
[CH3:1][O:2][c:3]1[cH:4][cH:5][c:6](-[c:7]2[cH:8][c:9](=[N:10][c:11]3[c:12]([CH3:13])[cH:14][c:15]([CH3:16])[cH:17][c:18]3[CH3:19])[n:20]([CH3:21])[c:22]([N:23]3[CH2:24][CH2:25][NH:26][CH2:36][CH2:37]3)[n:38]2)[cH:39][c:40]1[O:41][CH3:42].Cl[C:27](=[O:28])[c:29]1[cH:30][cH:31][c:32]([F:33])[cH:34][cH:35]1>>[CH3:1][O:2]...
COc1ccc(-c2cc(=Nc3c(C)cc(C)cc3C)n(C)c(N3CCNCC3)n2)cc1OC.O=C(Cl)c1ccc(F)cc1
COc1ccc(-c2cc(=Nc3c(C)cc(C)cc3C)n(C)c(N3CCN(C(=O)c4ccc(F)cc4)CC3)n2)cc1OC
null
null
O1CCCC1
Acylation
N-alkylation of secondary amines with alkyl halides
008ee4368afbd52034630a2410a1738f53049b314574435184e4e0be81b96642
96cb0a2fed10552c5770a45a2d6523b47ac3e38928b4a9c698d8577451182dcd
O=C(c1ccccc1)N1CCN(c2nc(-c3ccccc3)cc(=Nc3ccccc3)[nH]2)CC1
Cl-[C;H0;D3;+0:1](=[O;D1;H0:2])-[c:3](:[c:4]):[c:5].[#7:6]1-[C:7]-[C:8]-[NH;D2;+0:9]-[C:10]-[C:11]-1>>[O;D1;H0:2]=[C;H0;D3;+0:1](-[N;H0;D3;+0:9]1-[C:8]-[C:7]-[#7:6]-[C:11]-[C:10]-1)-[c:3](:[c:4]):[c:5]
null
[]
null
null
null
null
To a suspension of 3,4-dihydro-6-(3,4-dimethoxyphenyl)-3-methyl-2-(1-piperazinyl)-4-(2,4,6-trimethylphenylimino)pyrimidine (0.31 g) in tetrahydrofuran (10 ml) were added triethylamine (0.11 ml) and 4-fluorobenzoyl chloride (0.69 ml). The mixture was stirred at ambient temperature for an hour and the reaction was quench...
10.6084/m9.figshare.5104873.v1
null
Acyl halide.Secondary amine
Tertiary amide
C1C[NH]CCN1
C1C[NH]CC[NH]1
c1ccccc1.c1cncnc1.c1ccccc1.C1C[NH]CC[NH]1.c1ccccc1
HCl
O1CCCC1
null
null
COc1ccc(-c2cc(=Nc3c(C)cc(C)cc3C)n(C)c(N3CCNCC3)n2)cc1OC.O=C(Cl)c1ccc(F)cc1>O1CCCC1>COc1ccc(-c2cc(=Nc3c(C)cc(C)cc3C)n(C)c(N3CCN(C(=O)c4ccc(F)cc4)CC3)n2)cc1OC
ord_dataset-01dbb772c5e249108f0b191ed17a2c0c
ord-9337e50ccd674af7a4a11996c30facfa
COc1ccc(-c2cc(=Nc3c(C)cc(C)cc3C)n(C)c(NNC=O)n2)cc1OC>>COc1ccc(-c2cc(=Nc3c(C)cc(C)cc3C)n(C)c3nncn23)cc1OC
[OH-].[Na+].COC=1C=C(C=CC1OC)C1=CC(N(C(=N1)NNC=O)C)=NC1=C(C=C(C=C1C)C)C>>COC=1C=C(C=CC1OC)C1=CC(N(C=2N1C=NN2)C)=NC2=C(C=C(C=C2C)C)C
O=[CH:25][NH:24][NH:23][c:22]1[n:20]([CH3:21])[c:9](=[N:10][c:11]2[c:12]([CH3:13])[cH:14][c:15]([CH3:16])[cH:17][c:18]2[CH3:19])[cH:8][c:7](-[c:6]2[cH:5][cH:4][c:3]([O:2][CH3:1])[c:28]([O:29][CH3:30])[cH:27]2)[n:26]1>>[CH3:1][O:2][c:3]1[cH:4][cH:5][c:6](-[c:7]2[cH:8][c:9](=[N:10][c:11]3[c:12]([CH3:13])[cH:14][c:15]([CH...
COc1ccc(-c2cc(=Nc3c(C)cc(C)cc3C)n(C)c(NNC=O)n2)cc1OC
COc1ccc(-c2cc(=Nc3c(C)cc(C)cc3C)n(C)c3nncn23)cc1OC
null
null
O
Aromatic Heterocycle Formation
OtherReaction
431839368101cfcce4d54ee04001eea953337f68e32efd7aa6636f10cde15a56
3b74dccb5e8d79d411c67bfc6a766c6c6d6e4c42e46457114e1be0efa665abb5
c1ccc(N=c2cc(-c3ccccc3)n3cnnc3[nH]2)cc1
O=[CH;D2;+0:1]-[NH;D2;+0:2]-[NH;D2;+0:3]-[c:4]1:[n;H0;D2;+0:5]:[c:6](-[c:7]):[c:8]:[c:9]:[#7;a:10]:1-[C;D1;H3:11]>>[C;D1;H3:11]-[#7;a:10]1:[c:9]:[c:8]:[c:6](-[c:7]):[n;H0;D3;+0:5]2:[cH;D2;+0:1]:[n;H0;D2;+0:2]:[n;H0;D2;+0:3]:[c:4]:1:2
83.8
[{"value": 83.8, "product": "COC=1C=C(C=CC1OC)C1=CC(N(C=2N1C=NN2)C)=NC2=C(C=C(C=C2C)C)C", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
110
CELSIUS
2
HOUR
The mixture of 3,4-dihydro-6-(3,4-dimethoxyphenyl)-2-(2-formylhydrazino)-3-methyl-4-(2,4,6-trimethylphenylimino)pyrimidine (0.81 g) and polyphosphoric acid (8.2 g, 116% as phosphoric acid) was stirred at 110° C. for 2 hours and cooled to ambient temperature. The reaction mixture was poured into water and neutralized wi...
10.6084/m9.figshare.5104873.v1
null
Acylhydrazine
null
c1cncnc1
c1cnc2nncn2c1
c1ccccc1.c1ccccc1.c1cnc2nncn2c1
HO-
O
110
2
COc1ccc(-c2cc(=Nc3c(C)cc(C)cc3C)n(C)c(NNC=O)n2)cc1OC>O>COc1ccc(-c2cc(=Nc3c(C)cc(C)cc3C)n(C)c3nncn23)cc1OC
ord_dataset-01dbb772c5e249108f0b191ed17a2c0c
ord-40ed55c10e9f410d8fb8ab45b4b32b5c
COc1ccc(-c2cc(=Nc3c(C)cc(C)cc3C)n(C)c(Cl)n2)cc1OC.[N-]=[N+]=[N-]>>COc1ccc(-c2cc(=Nc3c(C)cc(C)cc3C)n(C)c3nnnn23)cc1OC
ClC1=NC(=CC(N1C)=NC1=C(C=C(C=C1C)C)C)C1=CC(=C(C=C1)OC)OC.[N-]=[N+]=[N-].[Na+]>>COC=1C=C(C=CC1OC)C1=CC(N(C=2N1N=NN2)C)=NC2=C(C=C(C=C2C)C)C
Cl[c:22]1[n:20]([CH3:21])[c:9](=[N:10][c:11]2[c:12]([CH3:13])[cH:14][c:15]([CH3:16])[cH:17][c:18]2[CH3:19])[cH:8][c:7](-[c:6]2[cH:5][cH:4][c:3]([O:2][CH3:1])[c:28]([O:29][CH3:30])[cH:27]2)[n:26]1.[N-:23]=[N+:25]=[N-:24]>>[CH3:1][O:2][c:3]1[cH:4][cH:5][c:6](-[c:7]2[cH:8][c:9](=[N:10][c:11]3[c:12]([CH3:13])[cH:14][c:15](...
COc1ccc(-c2cc(=Nc3c(C)cc(C)cc3C)n(C)c(Cl)n2)cc1OC.[N-]=[N+]=[N-]
COc1ccc(-c2cc(=Nc3c(C)cc(C)cc3C)n(C)c3nnnn23)cc1OC
null
null
CO.O
Aromatic Heterocycle Formation
OtherReaction
182b450bde9095fb43b75c5f7dae591bd7226c7b2a645b31f895fc1854549ce7
155f764f095c8454a4ad08aaa42f1abcb15d5bc1d4f122e4bcc624dd834362f2
c1ccc(N=c2cc(-c3ccccc3)n3nnnc3[nH]2)cc1
Cl-[c;H0;D3;+0:1]1:[n;H0;D2;+0:2]:[c:3](-[c:4]):[c:5]:[c:6]:[#7;a:7]:1-[C;D1;H3:8].[N-;H0;D1:9]=[N+;H0;D2:10]=[N-;H0;D1:11]>>[C;D1;H3:8]-[#7;a:7]1:[c:6]:[c:5]:[c:3](-[c:4]):[n;H0;D3;+0:2]2:[n;H0;D2;+0:10]:[n;H0;D2;+0:11]:[n;H0;D2;+0:9]:[c;H0;D3;+0:1]:1:2
78.9
[{"value": 78.9, "product": "COC=1C=C(C=CC1OC)C1=CC(N(C=2N1N=NN2)C)=NC2=C(C=C(C=C2C)C)C", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
null
null
To a suspension of 2-chloro-3,4-dihydro-6-(3,4-dimethoxyphenyl)-3-methyl-4-(2,4,6-trimethylphenylimino)pyrimidine (1.0 g) in a mixture of methanol (9 ml) and water (1.5 ml) was added sodium azide (0.163 g). The mixture was stirred at 50° to 55° C. for an hour. After removal of the solvent, the residue was washed with w...
10.6084/m9.figshare.5104873.v1
null
Aromatic halide
null
c1cncnc1
c1cnc2nnnn2c1
c1ccccc1.c1ccccc1.c1cnc2nnnn2c1
Other
CO.O
null
null
COc1ccc(-c2cc(=Nc3c(C)cc(C)cc3C)n(C)c(Cl)n2)cc1OC.[N-]=[N+]=[N-]>CO.O>COc1ccc(-c2cc(=Nc3c(C)cc(C)cc3C)n(C)c3nnnn23)cc1OC
ord_dataset-01dbb772c5e249108f0b191ed17a2c0c
ord-19fb07c87ee04a17a744052b6bbc4bb6
CI.COc1ccc(-c2cc(=Nc3c(C)cc(C)cc3C)n(C)c(N(C)Cc3ccccc3)n2)cc1OC>>COc1ccc(-c2cc(=Nc3c(C)cc(C)cc3C)n(C)c(=NCc3ccccc3)n2C)cc1OC
COC=1C=C(C=CC1OC)C1=CC(N(C(=N1)N(CC1=CC=CC=C1)C)C)=NC1=C(C=C(C=C1C)C)C.CI>>C(C1=CC=CC=C1)N=C1N(C(=CC(N1C)=NC1=C(C=C(C=C1C)C)C)C1=CC(=C(C=C1)OC)OC)C
I[CH3:32].C[N:23]([c:22]1[n:20]([CH3:21])[c:9](=[N:10][c:11]2[c:12]([CH3:13])[cH:14][c:15]([CH3:16])[cH:17][c:18]2[CH3:19])[cH:8][c:7](-[c:6]2[cH:5][cH:4][c:3]([O:2][CH3:1])[c:34]([O:35][CH3:36])[cH:33]2)[n:31]1)[CH2:24][c:25]1[cH:26][cH:27][cH:28][cH:29][cH:30]1>>[CH3:1][O:2][c:3]1[cH:4][cH:5][c:6](-[c:7]2[cH:8][c:9](...
CI.COc1ccc(-c2cc(=Nc3c(C)cc(C)cc3C)n(C)c(N(C)Cc3ccccc3)n2)cc1OC
COc1ccc(-c2cc(=Nc3c(C)cc(C)cc3C)n(C)c(=NCc3ccccc3)n2C)cc1OC
null
null
O1CCCC1
Protection
OtherReaction
bb846def72593a9f2b9f55a622fdbbce35e1d4c3fc05f325df7e2d85a38af78c
7619bfad8694b1a7e31b76c15f0caec637d52eb79098b20fc98b9e0e51bc2db0
c1ccc(CN=c2[nH]c(-c3ccccc3)cc(=Nc3ccccc3)[nH]2)cc1
C-[N;H0;D3;+0:1](-[C:2]-[c:3])-[c;H0;D3;+0:4]1:[n;H0;D2;+0:5]:[c:6](-[c:7]):[c:8]:[c:9]:[#7;a:10]:1-[C;D1;H3:11].I-[CH3;D1;+0:12]>>[C;D1;H3:11]-[#7;a:10]1:[c:9]:[c:8]:[c:6](-[c:7]):[n;H0;D3;+0:5](-[CH3;D1;+0:12]):[c;H0;D3;+0:4]:1=[N;H0;D2;+0:1]-[C:2]-[c:3]
null
[]
null
null
null
null
To a solution of 3,4-dihydro-6-(3,4-dimethoxyphenyl)-3-methyl-2-(N-methyl-N-benzylamino)-4-(2,4,6-trimethylphenylimino)pyrimidine (1.0 g) in tetrahydrofuran (20 ml) was added methyl iodide (2.58 ml). The solution was refluxed for 10 hours and cooled to ambient temperature. The reaction mixture was evaporated in vacuo a...
10.6084/m9.figshare.5104873.v1
null
Tertiary amine
null
c1cncnc1
c1cncnc1
c1ccccc1.c1cncnc1.c1ccccc1.c1ccccc1
HI
O1CCCC1
null
null
CI.COc1ccc(-c2cc(=Nc3c(C)cc(C)cc3C)n(C)c(N(C)Cc3ccccc3)n2)cc1OC>O1CCCC1>COc1ccc(-c2cc(=Nc3c(C)cc(C)cc3C)n(C)c(=NCc3ccccc3)n2C)cc1OC
ord_dataset-01dbb772c5e249108f0b191ed17a2c0c
ord-c718f36c041c43afbe95ad940fc057c9
COc1ccc(-c2cc(Cl)nc(C)n2)cc1OC.Cc1cc(C)c(N)c(C)c1>>COc1ccc(-c2cc(Nc3c(C)cc(C)cc3C)nc(C)n2)cc1OC
ClC1=NC(=NC(=C1)C1=CC(=C(C=C1)OC)OC)C.CC1=C(N)C(=CC(=C1)C)C>>COC=1C=C(C=CC1OC)C1=CC(=NC(=N1)C)NC1=C(C=C(C=C1C)C)C
Cl[c:9]1[cH:8][c:7](-[c:6]2[cH:5][cH:4][c:3]([O:2][CH3:1])[c:25]([O:26][CH3:27])[cH:24]2)[n:23][c:21]([CH3:22])[n:20]1.[NH2:10][c:11]1[c:12]([CH3:13])[cH:14][c:15]([CH3:16])[cH:17][c:18]1[CH3:19]>>[CH3:1][O:2][c:3]1[cH:4][cH:5][c:6](-[c:7]2[cH:8][c:9]([NH:10][c:11]3[c:12]([CH3:13])[cH:14][c:15]([CH3:16])[cH:17][c:18]3[...
COc1ccc(-c2cc(Cl)nc(C)n2)cc1OC.Cc1cc(C)c(N)c(C)c1
COc1ccc(-c2cc(Nc3c(C)cc(C)cc3C)nc(C)n2)cc1OC
null
null
null
Heteroatom Alkylation and Arylation
Goldberg coupling aryl amine-aryl chloride
c38b7155556ff28144ae37859ff6668b20d59da60c705d26b158542b6d8385da
71a04ae650defc5edd86a92f43c304e981a05f07ff76248da8d4155f3905a29d
c1ccc(Nc2cc(-c3ccccc3)ncn2)cc1
Cl-[c;H0;D3;+0:1]1:[#7;a:2]:[c:3](-[C;D1;H3:4]):[#7;a:5]:[c:6](-[c:7]):[c:8]:1.[NH2;D1;+0:9]-[c:10](:[c:11]):[c:12]>>[C;D1;H3:4]-[c:3]1:[#7;a:2]:[c;H0;D3;+0:1](-[NH;D2;+0:9]-[c:10](:[c:11]):[c:12]):[c:8]:[c:6](-[c:7]):[#7;a:5]:1
null
[]
120
CELSIUS
null
null
The mixture of 4-chloro-6-(3,4-dimethoxyphenyl)-2-methylpyrimidine (2.0 g) and 2,4,6-trimethylaniline (5.3 ml) was stirred at 120° C. for an hour. After cooled, the mixture was triturated with ethyl acetate. The precipitates were collected, and dissolved in chloroform. The solution was washed with aqueous sodium bicarb...
10.6084/m9.figshare.5104873.v1
null
Aromatic halide.Primary amine
Secondary amine
c1cncnc1
c1cncnc1
c1ccccc1.c1cncnc1.c1ccccc1
HCl
null
120
null
COc1ccc(-c2cc(Cl)nc(C)n2)cc1OC.Cc1cc(C)c(N)c(C)c1>>COc1ccc(-c2cc(Nc3c(C)cc(C)cc3C)nc(C)n2)cc1OC
ord_dataset-01dbb772c5e249108f0b191ed17a2c0c
ord-7a100c5c6f4546fe8ba2e190fe4324e2
CI.COc1ccc(-c2cc(Nc3c(C)cc(C)cc3C)nc(C)n2)cc1OC>>COc1ccc(-c2cc(N(C)c3c(C)cc(C)cc3C)nc(C)n2)cc1OC
COC=1C=C(C=CC1OC)C1=CC(=NC(=N1)C)NC1=C(C=C(C=C1C)C)C.CC(C)([O-])C.[K+].CI>>COC=1C=C(C=CC1OC)C1=CC(=NC(=N1)C)N(C1=C(C=C(C=C1C)C)C)C
I[CH3:11].[CH3:1][O:2][c:3]1[cH:4][cH:5][c:6](-[c:7]2[cH:8][c:9]([NH:10][c:12]3[c:13]([CH3:14])[cH:15][c:16]([CH3:17])[cH:18][c:19]3[CH3:20])[n:21][c:22]([CH3:23])[n:24]2)[cH:25][c:26]1[O:27][CH3:28]>>[CH3:1][O:2][c:3]1[cH:4][cH:5][c:6](-[c:7]2[cH:8][c:9]([N:10]([CH3:11])[c:12]3[c:13]([CH3:14])[cH:15][c:16]([CH3:17])[c...
CI.COc1ccc(-c2cc(Nc3c(C)cc(C)cc3C)nc(C)n2)cc1OC
COc1ccc(-c2cc(N(C)c3c(C)cc(C)cc3C)nc(C)n2)cc1OC
null
null
CN(C=O)C
Heteroatom Alkylation and Arylation
N-alkylation of secondary amines with alkyl halides
e1587a52a1bca6a80c6048d43276d8bccf8d3e94e692e6b210e5fd3b22494187
7cc25fba33369069673bac5bd8fc404dc064da8d6c8cf4a77f21f4df0a617fe3
c1ccc(Nc2cc(-c3ccccc3)ncn2)cc1
I-[CH3;D1;+0:1].[c:2]:[c:3](-[NH;D2;+0:4]-[c:5]1:[#7;a:6]:[c:7]:[#7;a:8]:[c:9]:[c:10]:1):[c:11]>>[CH3;D1;+0:1]-[N;H0;D3;+0:4](-[c:3](:[c:2]):[c:11])-[c:5]1:[#7;a:6]:[c:7]:[#7;a:8]:[c:9]:[c:10]:1
55.8
[{"value": 55.8, "product": "COC=1C=C(C=CC1OC)C1=CC(=NC(=N1)C)N(C1=C(C=C(C=C1C)C)C)C", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
1.5
HOUR
To a solution of 6-(3,4-dimethoxyphenyl)-2-methyl-4-(2,4,6-trimethylphenylamino)pyrimidine (1.0 g) in N,N-dimethylformamide (15 ml) were added potassium tert-butoxide (0.37 g) and methyl iodide (0.34 ml), and the mixture was stirred at ambient temperature for 1.5 hours. Then the mixture was poured into ice-water (200 m...
10.6084/m9.figshare.5104873.v1
null
Secondary amine
Tertiary amine
null
null
c1ccccc1.c1cncnc1.c1ccccc1
HI
CN(C=O)C
null
1.5
CI.COc1ccc(-c2cc(Nc3c(C)cc(C)cc3C)nc(C)n2)cc1OC>CN(C=O)C>COc1ccc(-c2cc(N(C)c3c(C)cc(C)cc3C)nc(C)n2)cc1OC
ord_dataset-01dbb772c5e249108f0b191ed17a2c0c
ord-76ac84f8bfe844fe8d9db859da230bc7
C1=CCNCC1.COc1ccc(-c2cc(=Nc3c(C)cc(C)cc3C)n(C)c(Cl)n2)cc1OC>>COc1ccc(-c2cc(=Nc3c(C)cc(C)cc3C)n(C)c(N3CC=CCC3)n2)cc1OC
ClC1=NC(=CC(N1C)=NC1=C(C=C(C=C1C)C)C)C1=CC(=C(C=C1)OC)OC.N1CCC=CC1>>COC=1C=C(C=CC1OC)C1=CC(N(C(=N1)N1CCC=CC1)C)=NC1=C(C=C(C=C1C)C)C
[NH:23]1[CH2:24][CH:25]=[CH:26][CH2:27][CH2:28]1.Cl[c:22]1[n:20]([CH3:21])[c:9](=[N:10][c:11]2[c:12]([CH3:13])[cH:14][c:15]([CH3:16])[cH:17][c:18]2[CH3:19])[cH:8][c:7](-[c:6]2[cH:5][cH:4][c:3]([O:2][CH3:1])[c:31]([O:32][CH3:33])[cH:30]2)[n:29]1>>[CH3:1][O:2][c:3]1[cH:4][cH:5][c:6](-[c:7]2[cH:8][c:9](=[N:10][c:11]3[c:12...
C1=CCNCC1.COc1ccc(-c2cc(=Nc3c(C)cc(C)cc3C)n(C)c(Cl)n2)cc1OC
COc1ccc(-c2cc(=Nc3c(C)cc(C)cc3C)n(C)c(N3CC=CCC3)n2)cc1OC
null
null
C(C)O
Heteroatom Alkylation and Arylation
Ullmann-Goldberg Substitution amine
b0012be1b87147a6e6c70481d7758c1e4cea97a075b06c4dc087fc8df8a11b0f
b6b8e2cdb45054a35f5e8157d624f852c0601a09401556706e166b19536eb7a7
C1=CCN(c2nc(-c3ccccc3)cc(=Nc3ccccc3)[nH]2)CC1
Cl-[c;H0;D3;+0:1](:[#7;a:2]:[c:3]):[#7;a:4](-[C;D1;H3:5]):[c:6].[C:7]1-[C:8]=[C:9]-[C:10]-[C:11]-[NH;D2;+0:12]-1>>[C;D1;H3:5]-[#7;a:4](:[c:6]):[c;H0;D3;+0:1](-[N;H0;D3;+0:12]1-[C:7]-[C:8]=[C:9]-[C:10]-[C:11]-1):[#7;a:2]:[c:3]
null
[]
null
null
null
null
To a suspension of 2-chloro-3,4-dihydro-6-(3,4-dimethoxyphenyl)-3-methyl-4-(2,4,6-trimethylphenylimino)pyrimidine (2.08 g) in ethanol (20 ml) was added 1,2,3,6-tetrahydropyridine (1.38 ml), and refluxed for 1.5 hours. The resulting precipitates were collected, dissolved in chloroform, washed with aqueous sodium bicarbo...
10.6084/m9.figshare.5104873.v1
null
Aromatic halide.Secondary amine
Tertiary amine
C1=CCNCC1.c1cncnc1
c1cncnc1.C1=CC[NH]CC1
c1ccccc1.c1cncnc1.c1ccccc1.C1=CC[NH]CC1
HCl
C(C)O
null
null
C1=CCNCC1.COc1ccc(-c2cc(=Nc3c(C)cc(C)cc3C)n(C)c(Cl)n2)cc1OC>C(C)O>COc1ccc(-c2cc(=Nc3c(C)cc(C)cc3C)n(C)c(N3CC=CCC3)n2)cc1OC
ord_dataset-01dbb772c5e249108f0b191ed17a2c0c
ord-49ae6795d91842138a9966c6c26eeb9a
COc1ccc(-c2cc(=Nc3c(C)cc(C)cc3C)n(C)cn2)cc1OC>>COc1ccc(C2=CC(=Nc3c(C)cc(C)cc3C)N(C)CN2)cc1OC
COC=1C=C(C=CC1OC)C1=CC(N(C=N1)C)=NC1=C(C=C(C=C1C)C)C.[BH4-].[Na+]>>COC=1C=C(C=CC1OC)C1=CC(N(CN1)C)=NC1=C(C=C(C=C1C)C)C
[CH3:1][O:2][c:3]1[cH:4][cH:5][c:6](-[c:7]2[cH:8][c:9](=[N:10][c:11]3[c:12]([CH3:13])[cH:14][c:15]([CH3:16])[cH:17][c:18]3[CH3:19])[n:20]([CH3:21])[cH:22][n:23]2)[cH:24][c:25]1[O:26][CH3:27]>>[CH3:1][O:2][c:3]1[cH:4][cH:5][c:6]([C:7]2=[CH:8][C:9](=[N:10][c:11]3[c:12]([CH3:13])[cH:14][c:15]([CH3:16])[cH:17][c:18]3[CH3:1...
COc1ccc(-c2cc(=Nc3c(C)cc(C)cc3C)n(C)cn2)cc1OC
COc1ccc(C2=CC(=Nc3c(C)cc(C)cc3C)N(C)CN2)cc1OC
null
null
C(C)O.O
Miscellaneous
OtherReaction
4f374c10be4b94bcd44017d11f58406012c0e7eb93ed620c56e1e9a043361621
ffa51f011c8cd2db0fde7a0daaa8ad62d16e443d58d706a838e147f90c7c26cf
C1=C(c2ccccc2)NCNC1=Nc1ccccc1
[C;D1;H3:1]-[n;H0;D3;+0:2]1:[cH;D2;+0:3]:[n;H0;D2;+0:4]:[c;H0;D3;+0:5](-[c;H0;D3;+0:6](:[c:7]:[c:8]):[c:9]:[c:10]):[cH;D2;+0:11]:[c;H0;D3;+0:12]:1=[#7:13]-[c:14]>>[C;D1;H3:1]-[N;H0;D3;+0:2]1-[CH2;D2;+0:3]-[NH;D2;+0:4]-[C;H0;D3;+0:5](-[c;H0;D3;+0:6](:[c:7]:[c:8]):[c:9]:[c:10])=[CH;D2;+0:11]-[C;H0;D3;+0:12]-1=[#7:13]-[c:...
58.7
[{"value": 58.7, "product": "COC=1C=C(C=CC1OC)C1=CC(N(CN1)C)=NC1=C(C=C(C=C1C)C)C", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
null
null
To a suspension of 3,4-dihydro-6-(3,4-dimethoxyphenyl)-3-methyl-4-(2,4,6-trimethylphenylimino)pyrimidine (2.0 g) in a mixture of ethanol (10 ml) and water (10 ml) was added sodium borohydride (1.04 g), and the mixture was stirred under reflux for 1.5 hours. After removal of the organic solvent, the mixture was suspende...
10.6084/m9.figshare.5104873.v1
null
null
Enamine.Tertiary amine
c1cncnc1
C1=CNC[NH]C1
c1ccccc1.C1=CNC[NH]C1.c1ccccc1
null
C(C)O.O
null
null
COc1ccc(-c2cc(=Nc3c(C)cc(C)cc3C)n(C)cn2)cc1OC>C(C)O.O>COc1ccc(C2=CC(=Nc3c(C)cc(C)cc3C)N(C)CN2)cc1OC
ord_dataset-01dbb772c5e249108f0b191ed17a2c0c
ord-3616968c1a0f4c4397905a7c8fdd4da3
CC(=O)OC(C)=O.COc1ccc(C2=CC(=Nc3c(C)cc(C)cc3C)N(C)CN2)cc1OC>>COc1ccc(C2=CC(=Nc3c(C)cc(C)cc3C)N(C)CN2C(C)=O)cc1OC
O.COC=1C=C(C=CC1OC)C1=CC(N(CN1)C)=NC1=C(C=C(C=C1C)C)C.C(C)(=O)OC(C)=O>>C(C)(=O)N1CN(C(C=C1C1=CC(=C(C=C1)OC)OC)=NC1=C(C=C(C=C1C)C)C)C
CC(=O)O[C:24]([CH3:25])=[O:26].[CH3:1][O:2][c:3]1[cH:4][cH:5][c:6]([C:7]2=[CH:8][C:9](=[N:10][c:11]3[c:12]([CH3:13])[cH:14][c:15]([CH3:16])[cH:17][c:18]3[CH3:19])[N:20]([CH3:21])[CH2:22][NH:23]2)[cH:27][c:28]1[O:29][CH3:30]>>[CH3:1][O:2][c:3]1[cH:4][cH:5][c:6]([C:7]2=[CH:8][C:9](=[N:10][c:11]3[c:12]([CH3:13])[cH:14][c:...
CC(=O)OC(C)=O.COc1ccc(C2=CC(=Nc3c(C)cc(C)cc3C)N(C)CN2)cc1OC
COc1ccc(C2=CC(=Nc3c(C)cc(C)cc3C)N(C)CN2C(C)=O)cc1OC
null
null
N1=CC=CC=C1
Acylation
Aminolysis of esters
37de4a9cab3150129c585744da39af6b1e53621ddee33eb6a0572e9cd7123509
c7805e0d43d630f03eb7041e49c61c53da3c359404af09cc4ab8902f166d026d
C1=C(c2ccccc2)NCNC1=Nc1ccccc1
C-C(=O)-O-[C;H0;D3;+0:1](-[C;D1;H3:2])=[O;D1;H0:3].[#7:4]=[C:5]1-[C:6]=[C:7](-[c:8])-[NH;D2;+0:9]-[C:10]-[#7:11]-1-[C;D1;H3:12]>>[#7:4]=[C:5]1-[C:6]=[C:7](-[c:8])-[N;H0;D3;+0:9](-[C;H0;D3;+0:1](-[C;D1;H3:2])=[O;D1;H0:3])-[C:10]-[#7:11]-1-[C;D1;H3:12]
null
[]
null
null
2.5
HOUR
To a solution of 6-(3,4-dimethoxyphenyl)-3-methyl-1,2,3,4-tetrahydro-4-(2,4,6-trimethylphenylimino)pyrimidine (0.5 g) in pyridine (5 ml) was added acetic anhydride (1.0 ml), and the mixture was stirred at ambient temperature for 2.5 hours. The mixture was poured into water (150 ml) and extracted with chloroform. The or...
10.6084/m9.figshare.5104873.v1
null
Enamine.Anhydride
Enamine.Tertiary amide
C1=CNC[NH]C1
C1=C[NH]C[NH]C1
c1ccccc1.C1=C[NH]C[NH]C1.c1ccccc1
HO-
N1=CC=CC=C1
null
2.5
CC(=O)OC(C)=O.COc1ccc(C2=CC(=Nc3c(C)cc(C)cc3C)N(C)CN2)cc1OC>N1=CC=CC=C1>COc1ccc(C2=CC(=Nc3c(C)cc(C)cc3C)N(C)CN2C(C)=O)cc1OC
ord_dataset-01dbb772c5e249108f0b191ed17a2c0c
ord-8713f1a083924a5fa46b8a31925ba557
COc1ccc(-c2cc(N3CCNCC3)nc(C)n2)cc1OC.NS(=O)(=O)c1cc(C(=O)Cl)c(Cl)cc1Cl>>COc1ccc(-c2cc(N3CCN(C(=O)c4cc(S(N)(=O)=O)c(Cl)cc4Cl)CC3)nc(C)n2)cc1OC
COC=1C=C(C=CC1OC)C1=CC(=NC(=N1)C)N1CCNCC1.C(C)N(CC)CC.ClC1=C(C(=O)Cl)C=C(C(=C1)Cl)S(N)(=O)=O>>ClC1=C(C(=O)N2CCN(CC2)C2=NC(=NC(=C2)C2=CC(=C(C=C2)OC)OC)C)C=C(C(=C1)Cl)S(N)(=O)=O
[CH3:1][O:2][c:3]1[cH:4][cH:5][c:6](-[c:7]2[cH:8][c:9]([N:10]3[CH2:11][CH2:12][NH:13][CH2:28][CH2:29]3)[n:30][c:31]([CH3:32])[n:33]2)[cH:34][c:35]1[O:36][CH3:37].Cl[C:14](=[O:15])[c:16]1[cH:17][c:18]([S:19]([NH2:20])(=[O:21])=[O:22])[c:23]([Cl:24])[cH:25][c:26]1[Cl:27]>>[CH3:1][O:2][c:3]1[cH:4][cH:5][c:6](-[c:7]2[cH:8]...
COc1ccc(-c2cc(N3CCNCC3)nc(C)n2)cc1OC.NS(=O)(=O)c1cc(C(=O)Cl)c(Cl)cc1Cl
COc1ccc(-c2cc(N3CCN(C(=O)c4cc(S(N)(=O)=O)c(Cl)cc4Cl)CC3)nc(C)n2)cc1OC
null
null
C(Cl)(Cl)Cl
Acylation
N-alkylation of secondary amines with alkyl halides
008ee4368afbd52034630a2410a1738f53049b314574435184e4e0be81b96642
96cb0a2fed10552c5770a45a2d6523b47ac3e38928b4a9c698d8577451182dcd
O=C(c1ccccc1)N1CCN(c2cc(-c3ccccc3)ncn2)CC1
Cl-[C;H0;D3;+0:1](=[O;D1;H0:2])-[c:3](:[c:4]):[c:5].[#7:6]1-[C:7]-[C:8]-[NH;D2;+0:9]-[C:10]-[C:11]-1>>[O;D1;H0:2]=[C;H0;D3;+0:1](-[N;H0;D3;+0:9]1-[C:8]-[C:7]-[#7:6]-[C:11]-[C:10]-1)-[c:3](:[c:4]):[c:5]
71.5
[{"value": 71.5, "product": "ClC1=C(C(=O)N2CCN(CC2)C2=NC(=NC(=C2)C2=CC(=C(C=C2)OC)OC)C)C=C(C(=C1)Cl)S(N)(=O)=O", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
20
HOUR
To a solution of 6-(3,4-dimethoxyphenyl)-2-methyl-4-(1-piperazinyl)pyrimidine (0.8 g) in chloroform (10 ml) were added triethylamine (0.39 ml) and 2,4-dichloro-5-sulfamoylbenzoyl chloride (0.74 g), and the mixture was stirred at ambient temperature for 20 hours. The reaction mixture was washed with water, dried over ma...
10.6084/m9.figshare.5104873.v1
null
Acyl halide.Secondary amine
Tertiary amide
C1C[NH]CCN1
C1C[NH]CC[NH]1
c1ccccc1.c1cncnc1.C1C[NH]CC[NH]1.c1ccccc1
HCl
C(Cl)(Cl)Cl
null
20
COc1ccc(-c2cc(N3CCNCC3)nc(C)n2)cc1OC.NS(=O)(=O)c1cc(C(=O)Cl)c(Cl)cc1Cl>C(Cl)(Cl)Cl>COc1ccc(-c2cc(N3CCN(C(=O)c4cc(S(N)(=O)=O)c(Cl)cc4Cl)CC3)nc(C)n2)cc1OC
ord_dataset-01dbb772c5e249108f0b191ed17a2c0c
ord-8c0e664d28f44521b67fd86394cabfa0
COc1ccc(-c2cc(Cl)nc(C)n2)cc1OC.Cc1cc(C)c(O)c(C)c1>>COc1ccc(-c2cc(Oc3c(C)cc(C)cc3C)nc(C)n2)cc1OC
O.ClC1=NC(=NC(=C1)C1=CC(=C(C=C1)OC)OC)C.CC1=C(C(=CC(=C1)C)C)O.[H-].[Na+]>>COC=1C=C(C=CC1OC)C1=CC(=NC(=N1)C)OC1=C(C=C(C=C1C)C)C
Cl[c:9]1[cH:8][c:7](-[c:6]2[cH:5][cH:4][c:3]([O:2][CH3:1])[c:25]([O:26][CH3:27])[cH:24]2)[n:23][c:21]([CH3:22])[n:20]1.[OH:10][c:11]1[c:12]([CH3:13])[cH:14][c:15]([CH3:16])[cH:17][c:18]1[CH3:19]>>[CH3:1][O:2][c:3]1[cH:4][cH:5][c:6](-[c:7]2[cH:8][c:9]([O:10][c:11]3[c:12]([CH3:13])[cH:14][c:15]([CH3:16])[cH:17][c:18]3[CH...
COc1ccc(-c2cc(Cl)nc(C)n2)cc1OC.Cc1cc(C)c(O)c(C)c1
COc1ccc(-c2cc(Oc3c(C)cc(C)cc3C)nc(C)n2)cc1OC
null
null
CN(C=O)C
Heteroatom Alkylation and Arylation
Williamson Ether Synthesis
38da1e480b17968341fc50d07104da93d31f20765e3b36e5a0790cb6b1d88a10
27e9a6bab4e3ed54aeb6be4d84cb1c0170208288795e252a46e57e44ecc064f0
c1ccc(Oc2cc(-c3ccccc3)ncn2)cc1
Cl-[c;H0;D3;+0:1]1:[#7;a:2]:[c:3](-[C;D1;H3:4]):[#7;a:5]:[c:6](-[c:7]):[c:8]:1.[OH;D1;+0:9]-[c:10](:[c:11]):[c:12]>>[C;D1;H3:4]-[c:3]1:[#7;a:2]:[c;H0;D3;+0:1](-[O;H0;D2;+0:9]-[c:10](:[c:11]):[c:12]):[c:8]:[c:6](-[c:7]):[#7;a:5]:1
71.2
[{"value": 71.2, "product": "COC=1C=C(C=CC1OC)C1=CC(=NC(=N1)C)OC1=C(C=C(C=C1C)C)C", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
5
MINUTE
To a solution of 2,4,6-trimethylphenol (1.03 g) in N,N-dimethylformamide (20 ml) was added sodium hydride (60% in oil, 0.30 g), and stirred at ambient temperature for 5 minutes. To the solution was added 4-chloro-6-(3,4-dimethoxyphenyl)-2-methylpyrimidine (2.0 g), and the mixture was stirred at ambient temperature for ...
10.6084/m9.figshare.5104873.v1
null
Aromatic halide.Aromatic alcohol
Ether
c1cncnc1
c1cncnc1
c1ccccc1.c1cncnc1.c1ccccc1
HCl
CN(C=O)C
null
0.083333
COc1ccc(-c2cc(Cl)nc(C)n2)cc1OC.Cc1cc(C)c(O)c(C)c1>CN(C=O)C>COc1ccc(-c2cc(Oc3c(C)cc(C)cc3C)nc(C)n2)cc1OC
ord_dataset-01dbb772c5e249108f0b191ed17a2c0c
ord-917a2479c3f9457d87255a214f0059bb
COc1ccc(-c2cc(Nc3ccc(N)cc3)nc(C)n2)cc1OC.CS(=O)(=O)Cl>>COc1ccc(-c2cc(Nc3ccc(NS(C)(=O)=O)cc3)nc(C)n2)cc1OC
C(Cl)(Cl)Cl.NC1=CC=C(C=C1)NC1=NC(=NC(=C1)C1=CC(=C(C=C1)OC)OC)C.CS(=O)(=O)Cl.C(C)N(CC)CC>>COC=1C=C(C=CC1OC)C1=CC(=NC(=N1)C)NC1=CC=C(C=C1)NS(=O)(=O)C
[CH3:1][O:2][c:3]1[cH:4][cH:5][c:6](-[c:7]2[cH:8][c:9]([NH:10][c:11]3[cH:12][cH:13][c:14]([NH2:15])[cH:20][cH:21]3)[n:22][c:23]([CH3:24])[n:25]2)[cH:26][c:27]1[O:28][CH3:29].Cl[S:16]([CH3:17])(=[O:18])=[O:19]>>[CH3:1][O:2][c:3]1[cH:4][cH:5][c:6](-[c:7]2[cH:8][c:9]([NH:10][c:11]3[cH:12][cH:13][c:14]([NH:15][S:16]([CH3:1...
COc1ccc(-c2cc(Nc3ccc(N)cc3)nc(C)n2)cc1OC.CS(=O)(=O)Cl
COc1ccc(-c2cc(Nc3ccc(NS(C)(=O)=O)cc3)nc(C)n2)cc1OC
null
null
ClCCCl
Acylation
Sulfonamide synthesis (Schotten-Baumann) primary amine
4c44ef6d7646f6ef25dd125d2c32c713d8dcae7c603407faa5f0fb810631670e
8fce8115d8a725afa92eb3910ded29d4c852e5133eba78a425054f41f7142603
c1ccc(Nc2cc(-c3ccccc3)ncn2)cc1
Cl-[S;H0;D4;+0:1](-[C;D1;H3:2])(=[O;D1;H0:3])=[O;D1;H0:4].[NH2;D1;+0:5]-[c:6](:[c:7]):[c:8]>>[C;D1;H3:2]-[S;H0;D4;+0:1](=[O;D1;H0:3])(=[O;D1;H0:4])-[NH;D2;+0:5]-[c:6](:[c:7]):[c:8]
null
[]
null
null
null
null
To a solution of 4-(4-aminophenylamino)-6-(3,4-dimethoxyphenyl)-2-methylpyrimidine (1.0 g) in 1,2-dichloroethane (20 ml) were added methanesulfonyl chloride (0.28 ml) and triethylamine (0.83 ml) and the mixture was refluxed for 3 hours. After cooled, chloroform (50 ml) was added thereto, and washed with water. The solu...
10.6084/m9.figshare.5104873.v1
null
Primary amine.Sulfonyl halide
Sulfonamide
null
null
c1ccccc1.c1cncnc1.c1ccccc1
HCl
ClCCCl
null
null
COc1ccc(-c2cc(Nc3ccc(N)cc3)nc(C)n2)cc1OC.CS(=O)(=O)Cl>ClCCCl>COc1ccc(-c2cc(Nc3ccc(NS(C)(=O)=O)cc3)nc(C)n2)cc1OC
ord_dataset-01dbb772c5e249108f0b191ed17a2c0c
ord-31d1c1feda2b47efbe166c7b36ac8cab
CN=C=O.COc1ccc(C2=CC(=Nc3c(C)cc(C)cc3C)N(C)CN2)cc1OC>>CNC(=O)N1CN(C)C(=Nc2c(C)cc(C)cc2C)C=C1c1ccc(OC)c(OC)c1
O.COC=1C=C(C=CC1OC)C1=CC(N(CN1)C)=NC1=C(C=C(C=C1C)C)C.CN=C=O>>COC=1C=C(C=CC1OC)C1=CC(N(CN1C(NC)=O)C)=NC1=C(C=C(C=C1C)C)C
[CH3:1][N:2]=[C:3]=[O:4].[NH:5]1[CH2:6][N:7]([CH3:8])[C:9](=[N:10][c:11]2[c:12]([CH3:13])[cH:14][c:15]([CH3:16])[cH:17][c:18]2[CH3:19])[CH:20]=[C:21]1[c:22]1[cH:23][cH:24][c:25]([O:26][CH3:27])[c:28]([O:29][CH3:30])[cH:31]1>>[CH3:1][NH:2][C:3](=[O:4])[N:5]1[CH2:6][N:7]([CH3:8])[C:9](=[N:10][c:11]2[c:12]([CH3:13])[cH:14...
CN=C=O.COc1ccc(C2=CC(=Nc3c(C)cc(C)cc3C)N(C)CN2)cc1OC
CNC(=O)N1CN(C)C(=Nc2c(C)cc(C)cc2C)C=C1c1ccc(OC)c(OC)c1
null
null
N1=CC=CC=C1
Acylation
Urea synthesis via isocyanate and secondary amine
4bb1a24b1b3e8307677a3ae0cb932053af15b5c63dd708805b4efb2d6595c3bc
6c7af49963b743cdb3f9754761159984e3aaed1b6f471cc88ee43e1a7e18d880
C1=C(c2ccccc2)NCNC1=Nc1ccccc1
[#7:1]=[C:2]1-[C:3]=[C:4](-[c:5])-[NH;D2;+0:6]-[C:7]-[#7:8]-1-[C;D1;H3:9].[C;D1;H3:10]-[N;H0;D2;+0:11]=[C;H0;D2;+0:12]=[O;D1;H0:13]>>[#7:1]=[C:2]1-[C:3]=[C:4](-[c:5])-[N;H0;D3;+0:6](-[C;H0;D3;+0:12](=[O;D1;H0:13])-[NH;D2;+0:11]-[C;D1;H3:10])-[C:7]-[#7:8]-1-[C;D1;H3:9]
null
[]
null
null
3
HOUR
To a solution of 6-(3,4-dimethoxyphenyl)-3-methyl-1,2,3,4-tetrahydro-4-(2,4,6-trimethylphenylimino)pyrimidine (1.0 g) in pyridine (10 ml) was added methyl isocyanate (0.18 ml), and the mixture was stirred at ambient temperature for 3 hours. Then the mixture was poured into water (150 ml), and the resultant precipitates...
10.6084/m9.figshare.5104873.v1
null
Enamine.Isocyanate
Enamine.Urea
C1=CNC[NH]C1
C1=C[NH]C[NH]C1
C1=C[NH]C[NH]C1.c1ccccc1.c1ccccc1
null
N1=CC=CC=C1
null
3
CN=C=O.COc1ccc(C2=CC(=Nc3c(C)cc(C)cc3C)N(C)CN2)cc1OC>N1=CC=CC=C1>CNC(=O)N1CN(C)C(=Nc2c(C)cc(C)cc2C)C=C1c1ccc(OC)c(OC)c1
ord_dataset-01dbb772c5e249108f0b191ed17a2c0c
ord-fa8318595eb54ee98aceafd5c8548e7b
CC(=O)c1ccncc1>>O=C(CBr)c1ccncc1
Br.C(C)(=O)C1=CC=NC=C1>>Br.BrCC(=O)C1=CC=NC=C1
[O:2]=[C:3]([CH3:4])[c:6]1[cH:7][cH:8][n:9][cH:10][cH:11]1>>[O:2]=[C:3]([CH2:4][Br:5])[c:6]1[cH:7][cH:8][n:9][cH:10][cH:11]1
CC(=O)c1ccncc1
O=C(CBr)c1ccncc1
null
null
C(C)(=O)O
Functional Group Addition
Bromination
bf5c9c3636d0bb082289a8c9a57893f9c01b86491bbac098df6f08165abff331
59d1a8eb6d53c009bab8d2eda578b612565fd5477616e626d840161408a683de
c1ccncc1
[CH3;D1;+0:1]-[C:2](=[O;D1;H0:3])-[c:4]>>[Br;D1;H0:5]-[CH2;D2;+0:1]-[C:2](=[O;D1;H0:3])-[c:4]
null
[]
null
null
null
null
A twelve-liter three neck flask fitted with an efficient mechanical stirrer, 250 mL dropping funnel, and internal thermometer was charged with glacial acetic acid (5000 mL), pyridinium bromide perbromide (90%, 830 g, 2.60 mol) and 30% hydrobromic acid in acetic acid (525 mL). After stirring at room temperature for nine...
10.6084/m9.figshare.5104873.v1
null
Ketone
Primary halide
null
null
c1ccncc1
Other
C(C)(=O)O
null
null
CC(=O)c1ccncc1>C(C)(=O)O>O=C(CBr)c1ccncc1
ord_dataset-01dbb772c5e249108f0b191ed17a2c0c
ord-01fa80306865499fa787ebe5005a2c4f
CC(=O)Nc1ccccc1Cc1nc(-c2ccncc2)cs1>>Nc1ccccc1Cc1nc(-c2ccncc2)cs1
C(C)(=O)NC1=C(CC=2SC=C(N2)C2=CC=NC=C2)C=CC=C1.[OH-].[Na+]>>NC1=C(CC=2SC=C(N2)C2=CC=NC=C2)C=CC=C1
CC(=O)[NH:1][c:2]1[cH:3][cH:4][cH:5][cH:6][c:7]1[CH2:8][c:9]1[n:10][c:11](-[c:12]2[cH:13][cH:14][n:15][cH:16][cH:17]2)[cH:18][s:19]1>>[NH2:1][c:2]1[cH:3][cH:4][cH:5][cH:6][c:7]1[CH2:8][c:9]1[n:10][c:11](-[c:12]2[cH:13][cH:14][n:15][cH:16][cH:17]2)[cH:18][s:19]1
CC(=O)Nc1ccccc1Cc1nc(-c2ccncc2)cs1
Nc1ccccc1Cc1nc(-c2ccncc2)cs1
null
null
C(C)O.Cl.O.C(Cl)Cl
Reduction
Hydrogenolysis of amides/imides/carbamates
755df58c254dea764fdda078ffd678ec540bba057c83683be04c253f1270ac7b
025f7cefe51e71668ad5d09fca32df168e9b538347403e4d5c1748073e538adc
c1ccc(Cc2nc(-c3ccncc3)cs2)cc1
C-C(=O)-[NH;D2;+0:1]-[c:2](:[c:3]):[c:4]>>[NH2;D1;+0:1]-[c:2](:[c:3]):[c:4]
69.5
[{"value": 65.0, "product": "NC1=C(CC=2SC=C(N2)C2=CC=NC=C2)C=CC=C1", "details": "PERCENTYIELD", "is_desired": false}, {"value": 69.5, "product": "NC1=C(CC=2SC=C(N2)C2=CC=NC=C2)C=CC=C1", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
null
null
A solution of 2-(o-acetamidobenzyl)-4-(4-pyridyl)thiazole (2.30 g, 0.007 mol) in concentrated hydrochloric acid (2 mL) and ethanol (3 mL) was refluxed for 3 hours, allowed to cool, diluted with water (2 mL) and methylene chloride (5 mL), and basified with 2.5N sodium hydroxide. The layers were separated with the aqueou...
10.6084/m9.figshare.5104873.v1
null
Secondary amide
Primary amine
null
null
c1ccccc1.c1cscn1.c1ccncc1
HO-
C(C)O.Cl.O.C(Cl)Cl
null
null
CC(=O)Nc1ccccc1Cc1nc(-c2ccncc2)cs1>C(C)O.Cl.O.C(Cl)Cl>Nc1ccccc1Cc1nc(-c2ccncc2)cs1
ord_dataset-01dbb772c5e249108f0b191ed17a2c0c
ord-ed73af56968b4454b488f0c1be5537e4
O=[N+]([O-])O.c1ccc(Cc2nc(-c3ccncc3)cs2)cc1>>O=[N+]([O-])c1ccc(Cc2nc(-c3ccncc3)cs2)cc1
C([O-])([O-])=O.[Na+].[Na+].[N+](=O)(O)[O-].C(C1=CC=CC=C1)C=1SC=C(N1)C1=CC=NC=C1.S(O)(O)(=O)=O>>[N+](=O)([O-])C1=CC=C(CC=2SC=C(N2)C2=CC=NC=C2)C=C1
O=[N+:2]([OH:1])[O-:3].[cH:4]1[cH:5][cH:6][c:7]([CH2:8][c:9]2[n:10][c:11](-[c:12]3[cH:13][cH:14][n:15][cH:16][cH:17]3)[cH:18][s:19]2)[cH:20][cH:21]1>>[O:1]=[N+:2]([O-:3])[c:4]1[cH:5][cH:6][c:7]([CH2:8][c:9]2[n:10][c:11](-[c:12]3[cH:13][cH:14][n:15][cH:16][cH:17]3)[cH:18][s:19]2)[cH:20][cH:21]1
O=[N+]([O-])O.c1ccc(Cc2nc(-c3ccncc3)cs2)cc1
O=[N+]([O-])c1ccc(Cc2nc(-c3ccncc3)cs2)cc1
null
null
C(Cl)(Cl)Cl
Functional Group Addition
Aromatic nitration with HNO3
53848b8b2bb4e867226e49db2e60519b24be9379900e3ad7c56af54fe8fde7a5
ddce49825c02b8965f10c8d99e3c841d26e1f136da6037b417c09313e6d73097
c1ccc(Cc2nc(-c3ccncc3)cs2)cc1
O=[N+;H0;D3:1](-[O;-;D1;H0:2])-[OH;D1;+0:3].[c:4]:[c:5]:[cH;D2;+0:6]:[c:7]:[c:8]>>[O;-;D1;H0:2]-[N+;H0;D3:1](=[O;H0;D1;+0:3])-[c;H0;D3;+0:6](:[c:5]:[c:4]):[c:7]:[c:8]
85.9
[{"value": 85.9, "product": "[N+](=O)([O-])C1=CC=C(CC=2SC=C(N2)C2=CC=NC=C2)C=C1", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
10
CELSIUS
null
null
A solution of 2-benzyl-4-(4-pyridyl)thiazole (4.50 g, 0.018 mol) in chloroform (25 mL) was added dropwise to concentrated sulfuric acid (15 mL). The resulting mixture was cooled to 10° C. and fuming nitric acid (1.45 g, 0.97 mL) carefully added dropwise such that the reaction temperature did not exceed 40° C. The mixtu...
10.6084/m9.figshare.5104873.v1
null
Nitrate
Nitro group
c1ccccc1
c1ccccc1
c1ccccc1.c1cscn1.c1ccncc1
HO-
C(Cl)(Cl)Cl
10
null
O=[N+]([O-])O.c1ccc(Cc2nc(-c3ccncc3)cs2)cc1>C(Cl)(Cl)Cl>O=[N+]([O-])c1ccc(Cc2nc(-c3ccncc3)cs2)cc1
ord_dataset-01dbb772c5e249108f0b191ed17a2c0c
ord-18b8488c6d344783bff5729349d8b2e5
CCOC=O.c1ccc(Cc2nc(-c3ccncc3)cs2)cc1>>O=CC(c1ccccc1)c1nc(-c2ccncc2)cs1
C(=O)OCC.C(C1=CC=CC=C1)C=1SC=C(N1)C1=CC=NC=C1.CN(CCN(C)C)C.C(CCC)[Li]>>C1(=CC=CC=C1)C(C=O)C=1SC=C(N1)C1=CC=NC=C1
CCO[CH:2]=[O:1].[CH2:3]([c:4]1[cH:5][cH:6][cH:7][cH:8][cH:9]1)[c:10]1[n:11][c:12](-[c:13]2[cH:14][cH:15][n:16][cH:17][cH:18]2)[cH:19][s:20]1>>[O:1]=[CH:2][CH:3]([c:4]1[cH:5][cH:6][cH:7][cH:8][cH:9]1)[c:10]1[n:11][c:12](-[c:13]2[cH:14][cH:15][n:16][cH:17][cH:18]2)[cH:19][s:20]1
CCOC=O.c1ccc(Cc2nc(-c3ccncc3)cs2)cc1
O=CC(c1ccccc1)c1nc(-c2ccncc2)cs1
null
null
O1CCCC1
C-C Coupling
OtherReaction
3dc7150b54f968d08b04811ce6d9fd58ce6b1717b4fbd76dbd02e91654c50b43
2aa39a25981921b5291a5742361ce4441cd47a0f2b930c869f26329c906b19c5
c1ccc(Cc2nc(-c3ccncc3)cs2)cc1
C-C-O-[CH;D2;+0:1]=[O;D1;H0:2].[c:3]:[c:4](-[CH2;D2;+0:5]-[c:6]1:[#16;a:7]:[c:8]:[c:9]:[#7;a:10]:1):[c:11]>>[O;D1;H0:2]=[CH;D2;+0:1]-[CH;D3;+0:5](-[c:6]1:[#16;a:7]:[c:8]:[c:9]:[#7;a:10]:1)-[c:4](:[c:3]):[c:11]
39
[{"value": 39.0, "product": "C1(=CC=CC=C1)C(C=O)C=1SC=C(N1)C1=CC=NC=C1", "details": "PERCENTYIELD", "is_desired": false}]
-78
CELSIUS
15
MINUTE
To a solution of 2-benzyl-4-(4-pyridyl)thiazole (4.00 g, 0.016 mol) and tetramethylethylenediamine (2.5 mL) in dry tetrahydrofuran (35 mL) at -78° C. under nitrogen atmosphere was added dropwise n-butyl lithium (1.6M in hexane, 11.4 mL). The resulting dark mixture was allowed to stir at -78° C. for 15 minutes, warmed t...
10.6084/m9.figshare.5104873.v1
null
Ether
Aldehyde
null
null
c1ccccc1.c1cscn1.c1ccncc1
HO-
O1CCCC1
-78
0.25
CCOC=O.c1ccc(Cc2nc(-c3ccncc3)cs2)cc1>O1CCCC1>O=CC(c1ccccc1)c1nc(-c2ccncc2)cs1
ord_dataset-01dbb772c5e249108f0b191ed17a2c0c
ord-ee8a5d8d7a7843959078967aa73d7741
NC(=S)C(F)(F)c1ccccc1.O=C(CBr)c1ccncc1>>FC(F)(c1ccccc1)c1nc(-c2ccncc2)cs1
FC(C(=S)N)(C1=CC=CC=C1)F.Br.BrCC(=O)C1=CC=NC=C1>>FC(C1=CC=CC=C1)(F)C=1SC=C(N1)C1=CC=NC=C1
[F:1][C:2]([F:3])([c:4]1[cH:5][cH:6][cH:7][cH:8][cH:9]1)[C:10]([NH2:11])=[S:20].O=[C:12]([c:13]1[cH:14][cH:15][n:16][cH:17][cH:18]1)[CH2:19]Br>>[F:1][C:2]([F:3])([c:4]1[cH:5][cH:6][cH:7][cH:8][cH:9]1)[c:10]1[n:11][c:12](-[c:13]2[cH:14][cH:15][n:16][cH:17][cH:18]2)[cH:19][s:20]1
NC(=S)C(F)(F)c1ccccc1.O=C(CBr)c1ccncc1
FC(F)(c1ccccc1)c1nc(-c2ccncc2)cs1
null
null
C(C)O
Aromatic Heterocycle Formation
OtherReaction
21eb8c7cda3c7fc14309a0c556334226f1a9147c334386d33bc70341830a82ec
9f145257a80f08f1a7a6ee36c84cd4115965bd63128f36de61c7ed688ad2603c
c1ccc(Cc2nc(-c3ccncc3)cs2)cc1
Br-[CH2;D2;+0:1]-[C;H0;D3;+0:2](=O)-[c;H0;D3;+0:3]1:[c:4]:[c:5]:[#7;a:6]:[c:7]:[c:8]:1.[F;D1;H0:9]-[C:10](-[F;D1;H0:11])(-[c:12])-[C;H0;D3;+0:13](-[NH2;D1;+0:14])=[S;H0;D1;+0:15]>>[F;D1;H0:9]-[C:10](-[F;D1;H0:11])(-[c:12])-[c;H0;D3;+0:13]1:[n;H0;D2;+0:14]:[c;H0;D3;+0:2](-[c;H0;D3;+0:3]2:[c:4]:[c:5]:[#7;a:6]:[c:7]:[c:8]...
48
[{"value": 48.0, "product": "FC(C1=CC=CC=C1)(F)C=1SC=C(N1)C1=CC=NC=C1", "details": "PERCENTYIELD", "is_desired": false}, {"value": 47.9, "product": "FC(C1=CC=CC=C1)(F)C=1SC=C(N1)C1=CC=NC=C1", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
null
null
To a solution of 2,2-difluoro-2-phenylthioacetamide (1.57 g, 0.0092 mol) in 95% ethanol (20 mL) was added α-bromo-4-acetylpyridine hydrobromide (3.20 g, 0.012 mol) and the mixture warmed on a steam bath for thirty minutes. The product was isolated in the usual way and recrystallized from ethyl acetate/hexane to afford ...
10.6084/m9.figshare.5104873.v1
null
Primary halide.Ketone.Thioamide
null
null
c1cscn1
c1ccccc1.c1cscn1.c1ccncc1
HBr
C(C)O
null
null
NC(=S)C(F)(F)c1ccccc1.O=C(CBr)c1ccncc1>C(C)O>FC(F)(c1ccccc1)c1nc(-c2ccncc2)cs1
ord_dataset-01dbb772c5e249108f0b191ed17a2c0c
ord-765591272e9a4caba598731704b65f44
N#C[S-].O=C(CBr)c1ccncc1>>Oc1nc(-c2ccncc2)cs1
Br.BrCC(=O)C1=CC=NC=C1.[S-]C#N.[K+].Cl.O>>OC=1SC=C(N1)C1=CC=NC=C1
[C:2](#[N:3])[S-:12].Br[CH2:11][C:4](=[O:1])[c:5]1[cH:6][cH:7][n:8][cH:9][cH:10]1>>[OH:1][c:2]1[n:3][c:4](-[c:5]2[cH:6][cH:7][n:8][cH:9][cH:10]2)[cH:11][s:12]1
N#C[S-].O=C(CBr)c1ccncc1
Oc1nc(-c2ccncc2)cs1
null
null
C(C)O
Aromatic Heterocycle Formation
OtherReaction
2537034356e56beddc377f967150ac167f1835fe0d357c9a23a4e3ab118a5498
cd18c57be94270d5ae64f4c553960798487616fd5806e36b30d128418cd18cca
c1cc(-c2cscn2)ccn1
Br-[CH2;D2;+0:1]-[C;H0;D3;+0:2](=[O;H0;D1;+0:3])-[c;H0;D3;+0:4]1:[c:5]:[c:6]:[#7;a:7]:[c:8]:[c:9]:1.[N;H0;D1;+0:10]#[C;H0;D2;+0:11]-[S-;H0;D1:12]>>[OH;D1;+0:3]-[c;H0;D3;+0:11]1:[n;H0;D2;+0:10]:[c;H0;D3;+0:2](-[c;H0;D3;+0:4]2:[c:5]:[c:6]:[#7;a:7]:[c:8]:[c:9]:2):[cH;D2;+0:1]:[s;H0;D2;+0:12]:1
null
[]
null
null
5
HOUR
A mixture of α-bromo-4-acetylpyridine hydrobromide (140.0 g, 0.50 mol) and potassium thiocyanate (53.4 g, 0.55 mol) in absolute ethanol (1500 mL) was heated to reflux for two hours. To the resulting mixture was added concentrated hydrochloric acid (250 mL) and water (500 mL) and reflux continued for five hours. After c...
10.6084/m9.figshare.5104873.v1
null
Primary halide.Ketone.Nitrile
Aromatic alcohol
null
c1cscn1
c1cscn1.c1ccncc1
Br-
C(C)O
null
5
N#C[S-].O=C(CBr)c1ccncc1>C(C)O>Oc1nc(-c2ccncc2)cs1
ord_dataset-01dbb772c5e249108f0b191ed17a2c0c
ord-6a872e674f0846bc9fa7a078ae69e05f
O=P(Cl)(Cl)Cl.Oc1nc(-c2ccncc2)cs1>>Clc1nc(-c2ccncc2)cs1
OC=1SC=C(N1)C1=CC=NC=C1.P(=O)(Cl)(Cl)Cl>>ClC=1SC=C(N1)C1=CC=NC=C1
O=P(Cl)(Cl)[Cl:1].O[c:2]1[n:3][c:4](-[c:5]2[cH:6][cH:7][n:8][cH:9][cH:10]2)[cH:11][s:12]1>>[Cl:1][c:2]1[n:3][c:4](-[c:5]2[cH:6][cH:7][n:8][cH:9][cH:10]2)[cH:11][s:12]1
O=P(Cl)(Cl)Cl.Oc1nc(-c2ccncc2)cs1
Clc1nc(-c2ccncc2)cs1
null
null
null
Functional Group Interconversion
Alcohol to chloride_Other
c8dfa2501a169ad412b92a30a4df16525460ddbdf84a0b2da53039c0817e89c5
e71580a8ffadb7b2717ecd7d68c1d3c0ca161ba5e6a787a49dad5a1359adc993
c1cc(-c2cscn2)ccn1
Cl-P(-Cl)(=O)-[Cl;H0;D1;+0:1].O-[c;H0;D3;+0:2]1:[#16;a:3]:[c:4]:[c:5]:[#7;a:6]:1>>[Cl;H0;D1;+0:1]-[c;H0;D3;+0:2]1:[#16;a:3]:[c:4]:[c:5]:[#7;a:6]:1
29
[{"value": 29.0, "product": "ClC=1SC=C(N1)C1=CC=NC=C1", "details": "PERCENTYIELD", "is_desired": false}]
140
CELSIUS
null
null
A mixture of 2-hydroxy-4-(4-pyridyl)thiazole (17.8 g, 0.10 mol) in phosphorous oxychloride (175 mL) was heated at 140° C. for 48 hours then quenched by carefully pouring onto ice (4000 mL). The resulting mixture was basified with 50% sodium hydroxide to pH 9 and extracted with methylene chloride (5×400 mL). The combine...
10.6084/m9.figshare.5104873.v1
null
Aromatic alcohol
Aromatic halide
c1cscn1
c1cscn1
c1cscn1.c1ccncc1
HCl
null
140
null
O=P(Cl)(Cl)Cl.Oc1nc(-c2ccncc2)cs1>>Clc1nc(-c2ccncc2)cs1
ord_dataset-01dbb772c5e249108f0b191ed17a2c0c
ord-08c4d0217383477aba8f92824c438c38
Clc1nc(-c2ccncc2)cs1.N#CCc1ccccc1>>N#CC(c1ccccc1)c1nc(-c2ccncc2)cs1
ClC=1SC=C(N1)C1=CC=NC=C1.C(C1=CC=CC=C1)C#N.[NH2-].[Na+]>>C1(=CC=CC=C1)C(C#N)C=1SC=C(N1)C1=CC=NC=C1
Cl[c:10]1[n:11][c:12](-[c:13]2[cH:14][cH:15][n:16][cH:17][cH:18]2)[cH:19][s:20]1.[N:1]#[C:2][CH2:3][c:4]1[cH:5][cH:6][cH:7][cH:8][cH:9]1>>[N:1]#[C:2][CH:3]([c:4]1[cH:5][cH:6][cH:7][cH:8][cH:9]1)[c:10]1[n:11][c:12](-[c:13]2[cH:14][cH:15][n:16][cH:17][cH:18]2)[cH:19][s:20]1
Clc1nc(-c2ccncc2)cs1.N#CCc1ccccc1
N#CC(c1ccccc1)c1nc(-c2ccncc2)cs1
null
null
C1(=CC=CC=C1)C
C-C Coupling
Hurtley reaction
07198ff39bbbd3f70802b10d0f27ae5abdac590ca6368a58203c62574039710d
48892094855745f5c51f8910c27ce7c101e08ad3f9da2a58d5512e3d9c1b432f
c1ccc(Cc2nc(-c3ccncc3)cs2)cc1
Cl-[c;H0;D3;+0:1]1:[#16;a:2]:[c:3]:[c:4]:[#7;a:5]:1.[N;D1;H0:6]#[C:7]-[CH2;D2;+0:8]-[c:9](:[c:10]):[c:11]>>[N;D1;H0:6]#[C:7]-[CH;D3;+0:8](-[c:9](:[c:10]):[c:11])-[c;H0;D3;+0:1]1:[#16;a:2]:[c:3]:[c:4]:[#7;a:5]:1
8.3
[{"value": 8.0, "product": "C1(=CC=CC=C1)C(C#N)C=1SC=C(N1)C1=CC=NC=C1", "details": "PERCENTYIELD", "is_desired": false}, {"value": 8.3, "product": "C1(=CC=CC=C1)C(C#N)C=1SC=C(N1)C1=CC=NC=C1", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
100
CELSIUS
null
null
To a solution of 2-chloro-4-(4-pyridyl)thiazole (1.00 g, 0.005 mol) and benzylcyanide (1.18 g, 0.010 mol) in dry toluene (10 mL) at 5° C. was added sodamide (400 mg, 0.010 mol) and the mixture heated to 100° C. for 20 minutes. After cooling, the mixture was quenched with water, the layers separated, and the aqueous pha...
10.6084/m9.figshare.5104873.v1
null
Aromatic halide
null
c1cscn1
c1cscn1
c1ccccc1.c1cscn1.c1ccncc1
HCl
C1(=CC=CC=C1)C
100
null
Clc1nc(-c2ccncc2)cs1.N#CCc1ccccc1>C1(=CC=CC=C1)C>N#CC(c1ccccc1)c1nc(-c2ccncc2)cs1
ord_dataset-01dbb772c5e249108f0b191ed17a2c0c
ord-fdefa7a16d504159aa72430f307694ae
[O]=[Mn](=[O])(=[O])[O-].c1ccc(Cc2nc(-c3ccncc3)cs2)cc1>>O=C(c1ccccc1)c1nc(-c2ccncc2)cs1
C(C1=CC=CC=C1)C=1SC=C(N1)C1=CC=NC=C1.[Mn](=O)(=O)(=O)[O-].[K+]>>C1(=CC=CC=C1)C(=O)C=1SC=C(N1)C1=CC=NC=C1
[O]=[Mn](=[O])([O-])=[O:1].[CH2:2]([c:3]1[cH:4][cH:5][cH:6][cH:7][cH:8]1)[c:9]1[n:10][c:11](-[c:12]2[cH:13][cH:14][n:15][cH:16][cH:17]2)[cH:18][s:19]1>>[O:1]=[C:2]([c:3]1[cH:4][cH:5][cH:6][cH:7][cH:8]1)[c:9]1[n:10][c:11](-[c:12]2[cH:13][cH:14][n:15][cH:16][cH:17]2)[cH:18][s:19]1
[O]=[Mn](=[O])(=[O])[O-].c1ccc(Cc2nc(-c3ccncc3)cs2)cc1
O=C(c1ccccc1)c1nc(-c2ccncc2)cs1
null
[I-].C(CCCCC)[N+](CCCCCC)(CCCCCC)CCCCCC
C1=CC=CC=C1.O
Heteroatom Alkylation and Arylation
OtherReaction
7a0b8463d98f4c7b922b16e60aaf09698e9f90cf246a26e079db9b5cbdeab585
a196f7191876ee39420290ab9d6c2b9eeb3251b37ae345fc435efba1949a85d9
O=C(c1ccccc1)c1nc(-c2ccncc2)cs1
[O-]-[Mn](=[O;H0;D1;+0:1])(=[O])=[O].[c:2]:[c:3](-[CH2;D2;+0:4]-[c:5]1:[#16;a:6]:[c:7]:[c:8]:[#7;a:9]:1):[c:10]>>[O;H0;D1;+0:1]=[C;H0;D3;+0:4](-[c:3](:[c:2]):[c:10])-[c:5]1:[#16;a:6]:[c:7]:[c:8]:[#7;a:9]:1
18.8
[{"value": 11.0, "product": "C1(=CC=CC=C1)C(=O)C=1SC=C(N1)C1=CC=NC=C1", "details": "PERCENTYIELD", "is_desired": false}, {"value": 18.8, "product": "C1(=CC=CC=C1)C(=O)C=1SC=C(N1)C1=CC=NC=C1", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
null
null
To a mixture of 2-benzyl-4-(4-pyridyl)thiazole (3.00 g, 0.01 mol) and potassium permanganate (3.16 g, 0.02 mol) in benzene (30 mL) and water (60 mL) was added tetrahexyl ammonium iodide (0.96 g, 0.02 mol). The biphasic mixture was heated at reflux for 15 hours. After cooling the organic layer was separated and concentr...
10.6084/m9.figshare.5104873.v1
null
null
Ketone
null
null
c1ccccc1.c1cscn1.c1ccncc1
HO-
[I-].C(CCCCC)[N+](CCCCCC)(CCCCCC)CCCCCC.C1=CC=CC=C1.O
null
null
[O]=[Mn](=[O])(=[O])[O-].c1ccc(Cc2nc(-c3ccncc3)cs2)cc1>[I-].C(CCCCC)[N+](CCCCCC)(CCCCCC)CCCCCC.C1=CC=CC=C1.O>O=C(c1ccccc1)c1nc(-c2ccncc2)cs1
ord_dataset-01dbb772c5e249108f0b191ed17a2c0c
ord-e29bb60d5a354d0d869838cdbf5e9016
O=C(c1ccccc1)c1nc(-c2ccncc2)cs1>>OC(c1ccccc1)c1nc(-c2ccncc2)cs1
C1(=CC=CC=C1)C(=O)C=1SC=C(N1)C1=CC=NC=C1.[BH4-].[Na+]>>C1(=CC=CC=C1)C(O)C=1SC=C(N1)C1=CC=NC=C1
[O:1]=[C:2]([c:3]1[cH:4][cH:5][cH:6][cH:7][cH:8]1)[c:9]1[n:10][c:11](-[c:12]2[cH:13][cH:14][n:15][cH:16][cH:17]2)[cH:18][s:19]1>>[OH:1][CH:2]([c:3]1[cH:4][cH:5][cH:6][cH:7][cH:8]1)[c:9]1[n:10][c:11](-[c:12]2[cH:13][cH:14][n:15][cH:16][cH:17]2)[cH:18][s:19]1
O=C(c1ccccc1)c1nc(-c2ccncc2)cs1
OC(c1ccccc1)c1nc(-c2ccncc2)cs1
null
null
CO
Reduction
Reduction of ketone to secondary alcohol
02790ac194d8bf7ccb13d6247c59412024d87f77d2c906ef7804f021f57d5070
1bd3cd74b454139c0a0068ac0135836499926b274bff569df163210c6c944a89
c1ccc(Cc2nc(-c3ccncc3)cs2)cc1
[O;H0;D1;+0:1]=[C;H0;D3;+0:2](-[c:3](:[c:4]):[c:5])-[c:6]1:[#16;a:7]:[c:8]:[c:9]:[#7;a:10]:1>>[OH;D1;+0:1]-[CH;D3;+0:2](-[c:3](:[c:4]):[c:5])-[c:6]1:[#16;a:7]:[c:8]:[c:9]:[#7;a:10]:1
45
[{"value": 45.0, "product": "C1(=CC=CC=C1)C(O)C=1SC=C(N1)C1=CC=NC=C1", "details": "PERCENTYIELD", "is_desired": false}, {"value": 44.7, "product": "C1(=CC=CC=C1)C(O)C=1SC=C(N1)C1=CC=NC=C1", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
1
HOUR
To a solution of 1-phenyl-1-[4-(4-pyridyl)-2-thiazolyl]methanone (675 g, 0.0025 mol) in methanol (40 mL) was added sodium borohydride (300 mg, 0.0079 mol) in portions and the mixture allowed to stir at room temperature for one hour. The reaction mixture was concentrated, diluted with water, and extracted with ether (3×...
10.6084/m9.figshare.5104873.v1
null
Ketone
Secondary alcohol
null
null
c1ccccc1.c1cscn1.c1ccncc1
null
CO
null
1
O=C(c1ccccc1)c1nc(-c2ccncc2)cs1>CO>OC(c1ccccc1)c1nc(-c2ccncc2)cs1
ord_dataset-01dbb772c5e249108f0b191ed17a2c0c
ord-c6e1cc3c94154c00aca4659516630175
c1ccc(Cc2nc(-c3ccncc3)cs2)cc1>>[O-][n+]1ccc(-c2csc(Cc3ccccc3)n2)cc1
ClC1=CC(=CC=C1)C(=O)OO.C(C1=CC=CC=C1)C=1SC=C(N1)C1=CC=NC=C1.ClC1=CC(=CC=C1)C(=O)OO>>C1(=CC=CC=C1)CC=1SC=C(N1)C1=CC=[N+](C=C1)[O-]
[n:2]1[cH:3][cH:4][c:5](-[c:6]2[cH:7][s:8][c:9]([CH2:10][c:11]3[cH:12][cH:13][cH:14][cH:15][cH:16]3)[n:17]2)[cH:18][cH:19]1>>[O-:1][n+:2]1[cH:3][cH:4][c:5](-[c:6]2[cH:7][s:8][c:9]([CH2:10][c:11]3[cH:12][cH:13][cH:14][cH:15][cH:16]3)[n:17]2)[cH:18][cH:19]1
c1ccc(Cc2nc(-c3ccncc3)cs2)cc1
[O-][n+]1ccc(-c2csc(Cc3ccccc3)n2)cc1
null
null
C(Cl)Cl
Functional Group Interconversion
OtherReaction
54415aed4bb61f76efee9ed140374352608210a9fed7c372975c12eb7023cea2
f1bbf9aa3c82f5e49be9f6d53533b6bb152f359232b6d32090c168949766aa71
c1ccc(Cc2nc(-c3cc[nH+]cc3)cs2)cc1
[c:1]:[c:2]:[n;H0;D2;+0:3]:[c:4]:[c:5]>>[O;-;D1;H0:6]-[n+;H0;D3:3](:[c:2]:[c:1]):[c:4]:[c:5]
95
[{"value": 95.0, "product": "C1(=CC=CC=C1)CC=1SC=C(N1)C1=CC=[N+](C=C1)[O-]", "details": "PERCENTYIELD", "is_desired": false}, {"value": 95.0, "product": "C1(=CC=CC=C1)CC=1SC=C(N1)C1=CC=[N+](C=C1)[O-]", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
8
HOUR
To a suspension of m-chloroperbenzoic acid (14.5 g) in dry methylene chloride (150 mL) was added a solution of 2-benzyl-4-(4-pyridyl)thiazole (15.1 g, 0.06 mol) in methylene chloride (125 mL) over thirty minutes. The mixture was allowed to stir overnight at room temperature then an additional portion of m-chloroperbenz...
10.6084/m9.figshare.5104873.v1
null
null
null
c1ccncc1
C1=CC=[NH+]C=C1
C1=CC=[NH+]C=C1.c1cscn1.c1ccccc1
null
C(Cl)Cl
null
8
c1ccc(Cc2nc(-c3ccncc3)cs2)cc1>C(Cl)Cl>[O-][n+]1ccc(-c2csc(Cc3ccccc3)n2)cc1
ord_dataset-01dbb772c5e249108f0b191ed17a2c0c
ord-c9b3112c5ae24285a00f3026a4e0278d
O=P(Cl)(Cl)Cl.[O-][n+]1ccc(-c2csc(Cc3ccccc3)n2)cc1>>Clc1cc(-c2csc(Cc3ccccc3)n2)ccn1
C1(=CC=CC=C1)CC=1SC=C(N1)C1=CC=[N+](C=C1)[O-].P(=O)(Cl)(Cl)Cl>>C(C1=CC=CC=C1)C=1SC=C(N1)C1=CC(=NC=C1)Cl
O=P(Cl)(Cl)[Cl:1].[O-][n+:19]1[cH:2][cH:3][c:4](-[c:5]2[cH:6][s:7][c:8]([CH2:9][c:10]3[cH:11][cH:12][cH:13][cH:14][cH:15]3)[n:16]2)[cH:17][cH:18]1>>[Cl:1][c:2]1[cH:3][c:4](-[c:5]2[cH:6][s:7][c:8]([CH2:9][c:10]3[cH:11][cH:12][cH:13][cH:14][cH:15]3)[n:16]2)[cH:17][cH:18][n:19]1
O=P(Cl)(Cl)Cl.[O-][n+]1ccc(-c2csc(Cc3ccccc3)n2)cc1
Clc1cc(-c2csc(Cc3ccccc3)n2)ccn1
null
null
null
Miscellaneous
OtherReaction
a7e4b874c7a18ec6b4305e16cc93c9103d77bfb4ce559ead41b2d45f56dcb90f
a48150e9dff88baab32dd83daf5ab089c597626e3c583c33a5868d8e1353c1ea
c1ccc(Cc2nc(-c3ccncc3)cs2)cc1
Cl-P(-Cl)(=O)-[Cl;H0;D1;+0:1].[O-]-[n+;H0;D3:2]1:[c:3]:[c:4]:[c:5]:[c:6]:[cH;D2;+0:7]:1>>[Cl;H0;D1;+0:1]-[c;H0;D3;+0:7]1:[c:6]:[c:5]:[c:4]:[c:3]:[n;H0;D2;+0:2]:1
31
[{"value": 31.0, "product": "C(C1=CC=CC=C1)C=1SC=C(N1)C1=CC(=NC=C1)Cl", "details": "PERCENTYIELD", "is_desired": false}, {"value": 30.6, "product": "C(C1=CC=CC=C1)C=1SC=C(N1)C1=CC(=NC=C1)Cl", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
null
null
A suspension of 4-[2-(phenylmethyl)-4-thiazolyl]pyridine-1-oxide (1.00 g, 0.0037 mol) in phosphorous oxychloride (10.0 g) was warmed on a steam bath overnight. After cooling the reaction mixture was concentrated and the residue treated with an excess of aqueous sodium bicarbonate. The tan precipitate was collected, tak...
10.6084/m9.figshare.5104873.v1
null
null
Aromatic halide
C1=CC=[NH+]C=C1
c1ccncc1
c1ccncc1.c1cscn1.c1ccccc1
HCl
null
null
null
O=P(Cl)(Cl)Cl.[O-][n+]1ccc(-c2csc(Cc3ccccc3)n2)cc1>>Clc1cc(-c2csc(Cc3ccccc3)n2)ccn1
ord_dataset-01dbb772c5e249108f0b191ed17a2c0c
ord-4003f3bd15224084afa096bd852af473
Clc1cc(-c2csc(Cc3ccccc3)n2)ccn1>>Cl.Cl.c1ccc(Cc2nc(-c3ccnc(N4CCCCC4)c3)cs2)cc1
C(C1=CC=CC=C1)C=1SC=C(N1)C1=CC(=NC=C1)Cl>>Cl.Cl.C(C1=CC=CC=C1)C=1SC=C(N1)C1=CC(=NC=C1)N1CCCCC1
[Cl:1][c:15]1[n:14][cH:13][cH:12][c:11](-[c:10]2[n:9][c:8]([CH2:7][c:6]3[cH:21][cH:20][cH:19][cH:3][cH:25]3)[s:24][cH:23]2)[cH:22]1>>[ClH:1].[ClH:2].[cH:3]1[cH:4][cH:5][c:6]([CH2:7][c:8]2[n:9][c:10](-[c:11]3[cH:12][cH:13][n:14][c:15]([N:16]4[CH2:17][CH2:18][CH2:19][CH2:20][CH2:21]4)[cH:22]3)[cH:23][s:24]2)[cH:25][cH:26...
Clc1cc(-c2csc(Cc3ccccc3)n2)ccn1
Cl.Cl.c1ccc(Cc2nc(-c3ccnc(N4CCCCC4)c3)cs2)cc1
null
null
N1CCCCC1
Aromatic Heterocycle Formation
OtherReaction
945d16753d2aadbd12dd057f9c2c2495efb877f5d157885b895bc9d035e01a95
66db14b78ca39a2323867c26921347f43c8475b8802a3ad393c6e0a64e54f6be
c1ccc(Cc2nc(-c3ccnc(N4CCCCC4)c3)cs2)cc1
[#16;a:1]:[c:2](-[C:3]-[c;H0;D3;+0:4]1:[cH;D2;+0:5]:[cH;D2;+0:6]:[cH;D2;+0:7]:[cH;D2;+0:8]:[cH;D2;+0:9]:1):[#7;a:10].[Cl;H0;D1;+0:11]-[c;H0;D3;+0:12](:[#7;a:13]:[c:14]):[c:15]:[c:16]>>[#16;a:1]:[c:2](-[C:3]-[c;H0;D3;+0:4]1:[c:17]:[c:18]:[cH;D2;+0:8]:[c:19]:[cH;D2;+0:9]:1):[#7;a:10].[c:16]:[c:15]:[c;H0;D3;+0:12](-[#7:20...
73.5
[{"value": 49.0, "product": "Cl.Cl.C(C1=CC=CC=C1)C=1SC=C(N1)C1=CC(=NC=C1)N1CCCCC1", "details": "PERCENTYIELD", "is_desired": false}, {"value": 73.5, "product": "Cl.Cl.C(C1=CC=CC=C1)C=1SC=C(N1)C1=CC(=NC=C1)N1CCCCC1", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
null
null
A solution of 2-benzyl-4-(2-chloro-4-pyridyl)thiazole (1.00 g, 0.0035 mol) in piperidine (15 mL) was heated to reflux for 16 hours. The reaction mixture was concentrated, taken up in ether (50 mL), filtered through celite, and the filtrate washed with water (2×). The ether layer was dried and concentrated. The residue ...
10.6084/m9.figshare.5104873.v1
null
Aromatic halide
Tertiary amine
c1ccncc1.c1ccccc1
c1ccccc1.c1ccncc1.C1CC[NH]CC1
c1ccccc1.c1cscn1.c1ccncc1.C1CC[NH]CC1
Other
N1CCCCC1
null
null
Clc1cc(-c2csc(Cc3ccccc3)n2)ccn1>N1CCCCC1>Cl.Cl.c1ccc(Cc2nc(-c3ccnc(N4CCCCC4)c3)cs2)cc1
ord_dataset-01dbb772c5e249108f0b191ed17a2c0c
ord-d201dac721b14afb8e363997a5e0f3c7
COC(=O)c1ccncc1OC.COC(C)=O>>COc1cnccc1C(C)=O
COC(C1=C(C=NC=C1)OC)=O.C(C)(=O)OC.Cl.C([O-])(O)=O.[Na+].[Na].[Na]>>COC=1C=NC=CC1C(C)=O
CO[C:9]([c:8]1[c:3]([O:2][CH3:1])[cH:4][n:5][cH:6][cH:7]1)=[O:11].COC(=O)[CH3:10]>>[CH3:1][O:2][c:3]1[cH:4][n:5][cH:6][cH:7][c:8]1[C:9]([CH3:10])=[O:11]
COC(=O)c1ccncc1OC.COC(C)=O
COc1cnccc1C(C)=O
null
null
CO.O
C-C Coupling
OtherReaction
66fad61539a4377b2099bf2b4bbabe7e2e80878fd5eeb84b925f14180416e99f
53456c3e87e97f512921684f59b54573df1eee9d8c313db55cd612727f50bb31
c1ccncc1
C-O-C(=O)-[CH3;D1;+0:1].C-O-[C;H0;D3;+0:2](=[O;D1;H0:3])-[c:4]1:[c:5]:[c:6]:[#7;a:7]:[c:8]:[c:9]:1>>[CH3;D1;+0:1]-[C;H0;D3;+0:2](=[O;D1;H0:3])-[c:4]1:[c:5]:[c:6]:[#7;a:7]:[c:8]:[c:9]:1
46.3
[{"value": 46.0, "product": "COC=1C=NC=CC1C(C)=O", "details": "PERCENTYIELD", "is_desired": false}, {"value": 46.3, "product": "COC=1C=NC=CC1C(C)=O", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
null
null
A dry 50 mL three neck flask fitted with a reflux condenser and internal thermometer was charged with dry methanol (20 mL). Sodium (516 mg, 0.022 mol) was added in portions and after all the sodium had dissolved the methanol was removed by distillation. The resulting sodium methoxide was cooled and a mixture of methyl-...
10.6084/m9.figshare.5104873.v1
null
Ester.Ester
Ketone
null
null
c1ccncc1
HO-
CO.O
null
null
COC(=O)c1ccncc1OC.COC(C)=O>CO.O>COc1cnccc1C(C)=O
ord_dataset-01dbb772c5e249108f0b191ed17a2c0c
ord-2cbd4d49833e4296861b4aa4a8ba079b
Br.COc1cnccc1C(C)=O>>COc1cnccc1C(=O)CBr
Br.[NH+]1=CC=CC=C1.Br.COC=1C=NC=CC1C(C)=O>>Br.BrCC(=O)C1=C(C=NC=C1)OC
[BrH:13].[CH3:2][O:3][c:4]1[cH:5][n:6][cH:7][cH:8][c:9]1[C:10](=[O:11])[CH3:12]>>[CH3:2][O:3][c:4]1[cH:5][n:6][cH:7][cH:8][c:9]1[C:10](=[O:11])[CH2:12][Br:13]
Br.COc1cnccc1C(C)=O
COc1cnccc1C(=O)CBr
null
null
C(C)(=O)O
Functional Group Addition
Bromination
bf5c9c3636d0bb082289a8c9a57893f9c01b86491bbac098df6f08165abff331
59d1a8eb6d53c009bab8d2eda578b612565fd5477616e626d840161408a683de
c1ccncc1
[BrH;D0;+0:1].[CH3;D1;+0:2]-[C:3](=[O;D1;H0:4])-[c:5]>>[Br;H0;D1;+0:1]-[CH2;D2;+0:2]-[C:3](=[O;D1;H0:4])-[c:5]
null
[]
null
null
4
HOUR
A solution of pyridinium hydrobromide perbromide (2.33 g, 0.0073 mol) in acetic acid (20 mL) containing 31% hydrobromic acid in acetic acid (1.85 mL) was stirred at room temperature for four hours. The mixture was cooled to 17° C. and a solution of 3-methoxy-4-acetylpyridine (1.02 g, 0.0062 mol) in acetic acid (5 mL) w...
10.6084/m9.figshare.5104873.v1
null
Ketone
Primary halide
null
null
c1ccncc1
null
C(C)(=O)O
null
4
Br.COc1cnccc1C(C)=O>C(C)(=O)O>COc1cnccc1C(=O)CBr
ord_dataset-01dbb772c5e249108f0b191ed17a2c0c
ord-c74194e3c47f4eb68794e86e6dfaa233
NN1CC=CCC1.O=C(Cl)Oc1ccccc1>>O=C(NN1CC=CCC1)Oc1ccccc1
Cl.NN1CCC=CC1.C(C)N(CC)CC.ClC(=O)OC1=CC=CC=C1>>O(C1=CC=CC=C1)C(=O)NN1CCC=CC1
[NH2:3][N:4]1[CH2:5][CH:6]=[CH:7][CH2:8][CH2:9]1.Cl[C:2](=[O:1])[O:10][c:11]1[cH:12][cH:13][cH:14][cH:15][cH:16]1>>[O:1]=[C:2]([NH:3][N:4]1[CH2:5][CH:6]=[CH:7][CH2:8][CH2:9]1)[O:10][c:11]1[cH:12][cH:13][cH:14][cH:15][cH:16]1
NN1CC=CCC1.O=C(Cl)Oc1ccccc1
O=C(NN1CC=CCC1)Oc1ccccc1
null
null
C(Cl)Cl
Protection
Acylation of Nitrogen Nucleophiles by Acyl/Thioacyl/Carbamoyl Halides and Analogs_OS
5be28d87ebf4e99b19d55116b9ee6a2de77dfa39d592d5f1181884aff5e22c5f
5fd6250903fa66c378faf3ffa4e2360187bf8e16b5a0c6900f15dfbc5082c0be
O=C(NN1CC=CCC1)Oc1ccccc1
Cl-[C;H0;D3;+0:1](=[O;D1;H0:2])-[#8:3]-[c:4].[C:5]=[C:6]-[C:7]-[#7:8](-[NH2;D1;+0:9])-[C:10]>>[C:5]=[C:6]-[C:7]-[#7:8](-[NH;D2;+0:9]-[C;H0;D3;+0:1](=[O;D1;H0:2])-[#8:3]-[c:4])-[C:10]
92.1
[{"value": 92.1, "product": "O(C1=CC=CC=C1)C(=O)NN1CCC=CC1", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
5
CELSIUS
4
HOUR
To a solution of N-amino-1,2,3,6-tetrahydropyridine hydrochloride (1.346 g) and triethylami-ne (2.024 g) in methylene chloride (60 ml) was added a solution of phenyl chloroformate (1.566 g) in methylene chloride (40 ml) and the mixture was stirred for 4 hours at 5° C. Evaporation of the solvent gave a residue, which wa...
10.6084/m9.figshare.5104873.v1
null
Acyl halide.Hydrazine
Acylhydrazine
null
null
C1=CC[NH]CC1.c1ccccc1
HCl
C(Cl)Cl
5
4
NN1CC=CCC1.O=C(Cl)Oc1ccccc1>C(Cl)Cl>O=C(NN1CC=CCC1)Oc1ccccc1
ord_dataset-01dbb772c5e249108f0b191ed17a2c0c
ord-a3795389ab974dca90679ddbd9c6c680
NN1CC=CCC1.O=C=Nc1ccc(F)cc1>>O=C(Nc1ccc(F)cc1)NN1CC=CCC1
Cl.NN1CCC=CC1.FC1=CC=C(C=C1)N=C=O.[OH-].[Na+]>>FC1=CC=C(C=C1)NC(=O)NN1CCC=CC1
[NH2:11][N:12]1[CH2:13][CH:14]=[CH:15][CH2:16][CH2:17]1.[O:1]=[C:2]=[N:3][c:4]1[cH:5][cH:6][c:7]([F:8])[cH:9][cH:10]1>>[O:1]=[C:2]([NH:3][c:4]1[cH:5][cH:6][c:7]([F:8])[cH:9][cH:10]1)[NH:11][N:12]1[CH2:13][CH:14]=[CH:15][CH2:16][CH2:17]1
NN1CC=CCC1.O=C=Nc1ccc(F)cc1
O=C(Nc1ccc(F)cc1)NN1CC=CCC1
null
null
O.O1CCOCC1
Acylation
OtherReaction
4cc4a1adc9245e9f94c26bab10e9433acf819602590c48e1d2f1cb274270f2bb
ff86715ec0916d8bbede65b7f01907f953cbdc6bb1bc08ee40ccb9bbc2c92974
O=C(Nc1ccccc1)NN1CC=CCC1
[C:1]=[C:2]-[C:3]-[#7:4](-[NH2;D1;+0:5])-[C:6].[O;D1;H0:7]=[C;H0;D2;+0:8]=[N;H0;D2;+0:9]-[c:10](:[c:11]):[c:12]>>[C:1]=[C:2]-[C:3]-[#7:4](-[NH;D2;+0:5]-[C;H0;D3;+0:8](=[O;D1;H0:7])-[NH;D2;+0:9]-[c:10](:[c:11]):[c:12])-[C:6]
77.6
[{"value": 77.6, "product": "FC1=CC=C(C=C1)NC(=O)NN1CCC=CC1", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
5
CELSIUS
2
HOUR
N-Amino-1,2,3,6-tetrahydropyridine hydrochloride (3.42 g) was dissolved in a mixture of dioxane (30 ml) and water (20 ml). The solution was adjusted to pH 7.5 with 1N-aqueous sodium hydroxide and to the resultant mixture was added a solution of 4-fluorophenylisocyanate (0.548 g) in dioxane (5 ml). Then, the mixture was...
10.6084/m9.figshare.5104873.v1
null
Hydrazine.Isocyanate
Acylhydrazine.Urea
null
null
c1ccccc1.C1=CC[NH]CC1
null
O.O1CCOCC1
5
2
NN1CC=CCC1.O=C=Nc1ccc(F)cc1>O.O1CCOCC1>O=C(Nc1ccc(F)cc1)NN1CC=CCC1
ord_dataset-01dbb772c5e249108f0b191ed17a2c0c
ord-15946ac52f84452daf9d7ce6d8f8fe10
NN1CC=CCC1.O=C=Nc1cccc(F)c1>>O=C(Nc1cccc(F)c1)NN1CC=CCC1
Cl.NN1CCC=CC1.C(C)N(CC)CC.FC=1C=C(C=CC1)N=C=O>>FC=1C=C(C=CC1)NC(=O)NN1CCC=CC1
[NH2:11][N:12]1[CH2:13][CH:14]=[CH:15][CH2:16][CH2:17]1.[O:1]=[C:2]=[N:3][c:4]1[cH:5][cH:6][cH:7][c:8]([F:9])[cH:10]1>>[O:1]=[C:2]([NH:3][c:4]1[cH:5][cH:6][cH:7][c:8]([F:9])[cH:10]1)[NH:11][N:12]1[CH2:13][CH:14]=[CH:15][CH2:16][CH2:17]1
NN1CC=CCC1.O=C=Nc1cccc(F)c1
O=C(Nc1cccc(F)c1)NN1CC=CCC1
null
null
C(Cl)Cl
Acylation
OtherReaction
4cc4a1adc9245e9f94c26bab10e9433acf819602590c48e1d2f1cb274270f2bb
ff86715ec0916d8bbede65b7f01907f953cbdc6bb1bc08ee40ccb9bbc2c92974
O=C(Nc1ccccc1)NN1CC=CCC1
[C:1]=[C:2]-[C:3]-[#7:4](-[NH2;D1;+0:5])-[C:6].[O;D1;H0:7]=[C;H0;D2;+0:8]=[N;H0;D2;+0:9]-[c:10](:[c:11]):[c:12]>>[C:1]=[C:2]-[C:3]-[#7:4](-[NH;D2;+0:5]-[C;H0;D3;+0:8](=[O;D1;H0:7])-[NH;D2;+0:9]-[c:10](:[c:11]):[c:12])-[C:6]
60.8
[{"value": 60.8, "product": "FC=1C=C(C=CC1)NC(=O)NN1CCC=CC1", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
1
HOUR
To a solution of N-amino-1,2,3,6-tetrahydropyridine hydrochloride (1.346 g) and triethylamine (1.012 g) in dry methylene chloride (40 ml) was added a solution of 3-fluorophenyl isocyanate (1.37 g) in dry methylene chloride under ice-bath cooling. After stirring for one hour, the reaction mixture was evaporated to dryne...
10.6084/m9.figshare.5104873.v1
null
Hydrazine.Isocyanate
Acylhydrazine.Urea
null
null
c1ccccc1.C1=CC[NH]CC1
null
C(Cl)Cl
null
1
NN1CC=CCC1.O=C=Nc1cccc(F)c1>C(Cl)Cl>O=C(Nc1cccc(F)c1)NN1CC=CCC1
ord_dataset-01dbb772c5e249108f0b191ed17a2c0c
ord-2972a999c99c4df9bc9aa7a812034758
Fc1ccc(N=C=S)cc1.NN1CC=C(c2ccccc2)CC1>>Fc1ccc(NC(=S)NN2CC=C(c3ccccc3)CC2)cc1
Cl.NN1CCC(=CC1)C1=CC=CC=C1.[OH-].[Na+].FC1=CC=C(C=C1)N=C=S>>FC1=CC=C(C=C1)NC(=S)NN1CCC(=CC1)C1=CC=CC=C1
[F:1][c:2]1[cH:3][cH:4][c:5]([N:6]=[C:7]=[S:8])[cH:22][cH:23]1.[NH2:9][N:10]1[CH2:11][CH:12]=[C:13]([c:14]2[cH:15][cH:16][cH:17][cH:18][cH:19]2)[CH2:20][CH2:21]1>>[F:1][c:2]1[cH:3][cH:4][c:5]([NH:6][C:7](=[S:8])[NH:9][N:10]2[CH2:11][CH:12]=[C:13]([c:14]3[cH:15][cH:16][cH:17][cH:18][cH:19]3)[CH2:20][CH2:21]2)[cH:22][cH:...
Fc1ccc(N=C=S)cc1.NN1CC=C(c2ccccc2)CC1
Fc1ccc(NC(=S)NN2CC=C(c3ccccc3)CC2)cc1
null
null
O.O1CCOCC1
Heteroatom Alkylation and Arylation
OtherReaction
d20aaa746dc43df2f35648d9419db98ed96f2035bae3684b9a4378845ffa3585
f7e2fc7ab2c341a9e6af0d77ebfb73e49e2475bed2a1247a7f61366f6427f2cf
S=C(Nc1ccccc1)NN1CC=C(c2ccccc2)CC1
[C:1]=[C:2]-[C:3]-[#7:4](-[NH2;D1;+0:5])-[C:6].[S;D1;H0:7]=[C;H0;D2;+0:8]=[N;H0;D2;+0:9]-[c:10](:[c:11]):[c:12]>>[C:1]=[C:2]-[C:3]-[#7:4](-[NH;D2;+0:5]-[C;H0;D3;+0:8](=[S;D1;H0:7])-[NH;D2;+0:9]-[c:10](:[c:11]):[c:12])-[C:6]
64.4
[{"value": 64.4, "product": "FC1=CC=C(C=C1)NC(=S)NN1CCC(=CC1)C1=CC=CC=C1", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
5
HOUR
To a stirred solution of N-amino-4-phenyl-1,2,3,6-tetrahydropyridine hydrochloride (1.05 g) in a mixture of dioxane (10 ml) and water (5 ml) was added 1N sodium hydroxide solution (5 ml) under ice-bath cooling, and then a solution of 4-fluorophenyl isothiocyanate (1.15 g) in dioxane (5 ml) was added thereto. The mixtur...
10.6084/m9.figshare.5104873.v1
null
Hydrazine.Isothiocyanate
Hydrazine.Thiourea
null
null
c1ccccc1.C1=CC[NH]CC1.c1ccccc1
null
O.O1CCOCC1
null
5
Fc1ccc(N=C=S)cc1.NN1CC=C(c2ccccc2)CC1>O.O1CCOCC1>Fc1ccc(NC(=S)NN2CC=C(c3ccccc3)CC2)cc1
ord_dataset-01dbb772c5e249108f0b191ed17a2c0c
ord-cc5f2343b0b2464494f03f96f151a07a
NN1CC=CCC1.O=C(Nc1ccc(F)cc1)Oc1ccccc1>>O=C(Nc1ccc(F)cc1)NN1CC=CCC1
FC1=CC=C(NC(=O)OC2=CC=CC=C2)C=C1.Cl.NN1CCC=CC1.C(C)N(CC)CC>>FC1=CC=C(C=C1)NC(=O)NN1CCC=CC1
[NH2:11][N:12]1[CH2:13][CH:14]=[CH:15][CH2:16][CH2:17]1.c1ccc(O[C:2](=[O:1])[NH:3][c:4]2[cH:5][cH:6][c:7]([F:8])[cH:9][cH:10]2)cc1>>[O:1]=[C:2]([NH:3][c:4]1[cH:5][cH:6][c:7]([F:8])[cH:9][cH:10]1)[NH:11][N:12]1[CH2:13][CH:14]=[CH:15][CH2:16][CH2:17]1
NN1CC=CCC1.O=C(Nc1ccc(F)cc1)Oc1ccccc1
O=C(Nc1ccc(F)cc1)NN1CC=CCC1
null
null
C(Cl)(Cl)Cl
Acylation
OtherReaction
836db69d01985cc962fe5c0a07b8b8d48bdfd49ff4000059963792bc5c6f1006
0cb77777283c5722e23a892db9f638efc73d17e00759b2f46f68b450e32d1d89
O=C(Nc1ccccc1)NN1CC=CCC1
[C:1]=[C:2]-[C:3]-[#7:4](-[NH2;D1;+0:5])-[C:6].[O;D1;H0:7]=[C;H0;D3;+0:8](-O-c1:c:c:c:c:c:1)-[#7:9]-[c:10]>>[C:1]=[C:2]-[C:3]-[#7:4](-[NH;D2;+0:5]-[C;H0;D3;+0:8](=[O;D1;H0:7])-[#7:9]-[c:10])-[C:6]
45.1
[{"value": 45.1, "product": "FC1=CC=C(C=C1)NC(=O)NN1CCC=CC1", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
null
null
A solution of 4-fluoro-N-phenoxycarbonylaniline (2.29 g), N-amino-1,2,3,6-tetrahydropyridine hydrochloride (1.346 g) and triethylamine (1.02 g) in chloroform (25 ml) was refluxed for 20 hours. After evaporation of chloroform, the residue was extracted with ethyl acetate (100 ml). The extract was washed with water, drie...
10.6084/m9.figshare.5104873.v1
null
Hydrazine.Carbamic ester.Ether
Acylhydrazine
c1ccccc1
null
c1ccccc1.C1=CC[NH]CC1
HO-
C(Cl)(Cl)Cl
null
null
NN1CC=CCC1.O=C(Nc1ccc(F)cc1)Oc1ccccc1>C(Cl)(Cl)Cl>O=C(Nc1ccc(F)cc1)NN1CC=CCC1
ord_dataset-01dbb772c5e249108f0b191ed17a2c0c
ord-4dac31e8682a4872921ace479cd32233
O=C(N=[N+]1C=CC=CC1)Nc1ccccc1>>O=C(Nc1ccccc1)NN1CC=CCC1
C1(=CC=CC=C1)NC(=O)N=[N+]1CC=CC=C1.[BH4-].[Na+].Cl>>C1(=CC=CC=C1)NC(=O)NN1CCC=CC1
[O:1]=[C:2]([NH:3][c:4]1[cH:5][cH:6][cH:7][cH:8][cH:9]1)[N:10]=[N+:11]1[CH:12]=[CH:13][CH:14]=[CH:15][CH2:16]1>>[O:1]=[C:2]([NH:3][c:4]1[cH:5][cH:6][cH:7][cH:8][cH:9]1)[NH:10][N:11]1[CH2:12][CH:13]=[CH:14][CH2:15][CH2:16]1
O=C(N=[N+]1C=CC=CC1)Nc1ccccc1
O=C(Nc1ccccc1)NN1CC=CCC1
null
null
C(C)O.O
Functional Group Interconversion
OtherReaction
e9211f4eb8ad1093fdbfa79df9ebf798cf09f13d01237eea98dde61cba4e5c46
49e46cfaf3d77e98e969c0bd47c3ecbd1ec0df0bc3c38cf005eb42de5f17a73a
O=C(Nc1ccccc1)NN1CC=CCC1
[O;D1;H0:1]=[C:2](-[#7:3]-[c:4])-[N;H0;D2;+0:5]=[N+;H0;D3:6]1-[C:7]-[CH;D2;+0:8]=[CH;D2;+0:9]-[CH;D2;+0:10]=[CH;D2;+0:11]-1>>[O;D1;H0:1]=[C:2](-[#7:3]-[c:4])-[NH;D2;+0:5]-[N;H0;D3;+0:6]1-[C:7]-[CH2;D2;+0:8]-[CH;D2;+0:9]=[CH;D2;+0:10]-[CH2;D2;+0:11]-1
null
[]
null
null
4
HOUR
To a solution of N-(phenylcarbamoylimino)pyridinium ylide (0.64 g) in a mixture of ethanol (30 ml) and water (10 ml) was added sodium borohydride (0.20 g) at ambient temperature. After being stirred for 4 hours, the reaction mixture was acidified with 1N hydrochloric acid, concentrated to a volume of ca. 15 ml. The cry...
10.6084/m9.figshare.5104873.v1
null
Enamine.Conjugated diene
Acylhydrazine.Urea
C1=CC[NH+]C=C1
C1=CC[NH]CC1
c1ccccc1.C1=CC[NH]CC1
null
C(C)O.O
null
4
O=C(N=[N+]1C=CC=CC1)Nc1ccccc1>C(C)O.O>O=C(Nc1ccccc1)NN1CC=CCC1
ord_dataset-01dbb772c5e249108f0b191ed17a2c0c
ord-ba8e9518e9a14e998c41606e7292d98b
O=C(N=[N+]1C=CC=CC1)Nc1ccc(F)cc1>>O=C(Nc1ccc(F)cc1)NN1CC=CCC1
O.FC1=CC=C(C=C1)NC(=O)N=[N+]1CC=CC=C1.[BH4-].[Na+].[BH4-].[Na+]>>FC1=CC=C(C=C1)NC(=O)NN1CCC=CC1
[O:1]=[C:2]([NH:3][c:4]1[cH:5][cH:6][c:7]([F:8])[cH:9][cH:10]1)[N:11]=[N+:12]1[CH:13]=[CH:14][CH:15]=[CH:16][CH2:17]1>>[O:1]=[C:2]([NH:3][c:4]1[cH:5][cH:6][c:7]([F:8])[cH:9][cH:10]1)[NH:11][N:12]1[CH2:13][CH:14]=[CH:15][CH2:16][CH2:17]1
O=C(N=[N+]1C=CC=CC1)Nc1ccc(F)cc1
O=C(Nc1ccc(F)cc1)NN1CC=CCC1
null
null
C(C)O
Functional Group Interconversion
OtherReaction
e9211f4eb8ad1093fdbfa79df9ebf798cf09f13d01237eea98dde61cba4e5c46
49e46cfaf3d77e98e969c0bd47c3ecbd1ec0df0bc3c38cf005eb42de5f17a73a
O=C(Nc1ccccc1)NN1CC=CCC1
[O;D1;H0:1]=[C:2](-[#7:3]-[c:4])-[N;H0;D2;+0:5]=[N+;H0;D3:6]1-[C:7]-[CH;D2;+0:8]=[CH;D2;+0:9]-[CH;D2;+0:10]=[CH;D2;+0:11]-1>>[O;D1;H0:1]=[C:2](-[#7:3]-[c:4])-[NH;D2;+0:5]-[N;H0;D3;+0:6]1-[C:7]-[CH2;D2;+0:8]-[CH;D2;+0:9]=[CH;D2;+0:10]-[CH2;D2;+0:11]-1
null
[]
null
null
16
HOUR
A suspension of N-[[(4-fluorophenyl)carbamoyl]-imino]pyridinium ylide (1.04 g) and sodium borohydride (2.55 g) in ethanol (100 ml) was stirred at ambient temperature for 16 hours. Excess of sodium borohydride was decomposed with water, and the resulting mixture was evaporated. The residue was extracted with chloroform ...
10.6084/m9.figshare.5104873.v1
null
Enamine.Conjugated diene
Acylhydrazine.Urea
C1=CC[NH+]C=C1
C1=CC[NH]CC1
c1ccccc1.C1=CC[NH]CC1
null
C(C)O
null
16
O=C(N=[N+]1C=CC=CC1)Nc1ccc(F)cc1>C(C)O>O=C(Nc1ccc(F)cc1)NN1CC=CCC1
ord_dataset-01dbb772c5e249108f0b191ed17a2c0c
ord-824d03c3210447cc84bae0d08c4e9730
COC(=O)c1ccc(NC(=O)NN2CC=CCC2)cc1>>O=C(Nc1ccc(C(=O)O)cc1)NN1CC=CCC1
COC(=O)C1=CC=C(C=C1)NC(=O)NN1CCC=CC1.[OH-].[Na+]>>C(=O)(O)C1=CC=C(C=C1)NC(=O)NN1CCC=CC1
C[O:10][C:8]([c:7]1[cH:6][cH:5][c:4]([NH:3][C:2](=[O:1])[NH:13][N:14]2[CH2:15][CH:16]=[CH:17][CH2:18][CH2:19]2)[cH:12][cH:11]1)=[O:9]>>[O:1]=[C:2]([NH:3][c:4]1[cH:5][cH:6][c:7]([C:8](=[O:9])[OH:10])[cH:11][cH:12]1)[NH:13][N:14]1[CH2:15][CH:16]=[CH:17][CH2:18][CH2:19]1
COC(=O)c1ccc(NC(=O)NN2CC=CCC2)cc1
O=C(Nc1ccc(C(=O)O)cc1)NN1CC=CCC1
null
null
C(Cl)(Cl)Cl.CO
Deprotection
Ester saponification (methyl deprotection)
d872e08ad5c85a4add6cd04e6e987e73fead5f79b3f30ba61a81ba5029b29894
38ae1ee78433b9acfb0390501446149c80f88f23ac2d84c60b3369bdab75cec9
O=C(Nc1ccccc1)NN1CC=CCC1
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]
56.6
[{"value": 56.6, "product": "C(=O)(O)C1=CC=C(C=C1)NC(=O)NN1CCC=CC1", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
null
null
To a solution of N-[[(4-methoxycarbonylphenyl)-carbamoyl]amino]-1,2,3,6-tetrahydropyridine (1.21 g) in a mixture of methanol (30 ml) and chloroform (30 ml) was added. 1N sodium hydroxide (10 ml) and the mixture was stirred at ambient temperature for 18 hours. After evaporation of the solvent, the residue was extracted ...
10.6084/m9.figshare.5104873.v1
null
Ester
Carboxylic acid
null
null
c1ccccc1.C1=CC[NH]CC1
Other
C(Cl)(Cl)Cl.CO
null
null
COC(=O)c1ccc(NC(=O)NN2CC=CCC2)cc1>C(Cl)(Cl)Cl.CO>O=C(Nc1ccc(C(=O)O)cc1)NN1CC=CCC1
ord_dataset-01dbb772c5e249108f0b191ed17a2c0c
ord-10bcb14ff2a94443b04413a0a391e4dc
CCOC(=O)[C@H](CC(=O)c1ccccc1)N[C@@H](C)C(=O)N1CCC[C@H]1C(=O)OC(C)(C)C>>CCOC(=O)[C@H](C[C@@H](O)c1ccccc1)N[C@@H](C)C(=O)N1CCC[C@H]1C(=O)OC(C)(C)C
C(C)(C)(C)OC([C@H]1N(CCC1)C([C@@H](N[C@@H](CC(=O)C1=CC=CC=C1)C(=O)OCC)C)=O)=O>>C(C)(C)(C)OC([C@H]1N(CCC1)C([C@@H](N[C@@H](C[C@@H](O)C1=CC=CC=C1)C(=O)OCC)C)=O)=O
[CH3:1][CH2:2][O:3][C:4](=[O:5])[C@H:6]([CH2:7][C:8](=[O:9])[c:10]1[cH:11][cH:12][cH:13][cH:14][cH:15]1)[NH:16][C@@H:17]([CH3:18])[C:19](=[O:20])[N:21]1[CH2:22][CH2:23][CH2:24][C@H:25]1[C:26](=[O:27])[O:28][C:29]([CH3:30])([CH3:31])[CH3:32]>>[CH3:1][CH2:2][O:3][C:4](=[O:5])[C@H:6]([CH2:7][C@@H:8]([OH:9])[c:10]1[cH:11][...
CCOC(=O)[C@H](CC(=O)c1ccccc1)N[C@@H](C)C(=O)N1CCC[C@H]1C(=O)OC(C)(C)C
CCOC(=O)[C@H](C[C@@H](O)c1ccccc1)N[C@@H](C)C(=O)N1CCC[C@H]1C(=O)OC(C)(C)C
null
[Pd]
C(C)O
Reduction
Reduction of ketone to secondary alcohol
02790ac194d8bf7ccb13d6247c59412024d87f77d2c906ef7804f021f57d5070
1bd3cd74b454139c0a0068ac0135836499926b274bff569df163210c6c944a89
O=C(CNCCCc1ccccc1)N1CCCC1
[#8:1]-[C:2](=[O;D1;H0:3])-[C:4]-[C:5]-[C;H0;D3;+0:6](=[O;H0;D1;+0:7])-[c:8](:[c:9]):[c:10]>>[#8:1]-[C:2](=[O;D1;H0:3])-[C:4]-[C:5]-[C@@H;D3;+0:6](-[OH;D1;+0:7])-[c:8](:[c:9]):[c:10]
null
[]
null
null
null
null
13.4 g (30 mmoles) of N-[1-(S)-ethoxycarbonyl-3-phenyl-3-oxo-propyl]-(S)-alanyl-(S)-proline-t - butylester are dissolved in 120 ml of ethanol and hydrogenated in the presence of 1.5 g of 10% palladium-on-charcoal catalyst at room temperature. After the uptake of the theoretically needed hydrogen (720 ml), the catalyst ...
10.6084/m9.figshare.5104873.v1
null
Ketone
Secondary alcohol
null
null
c1ccccc1.C1CC[NH]C1
null
[Pd].C(C)O
null
null
CCOC(=O)[C@H](CC(=O)c1ccccc1)N[C@@H](C)C(=O)N1CCC[C@H]1C(=O)OC(C)(C)C>[Pd].C(C)O>CCOC(=O)[C@H](C[C@@H](O)c1ccccc1)N[C@@H](C)C(=O)N1CCC[C@H]1C(=O)OC(C)(C)C
ord_dataset-01dbb772c5e249108f0b191ed17a2c0c
ord-f01be8f761ca4562ae3496ae6ef3ae07
CCOC(=O)/C=C/C(=O)c1ccccc1.C[C@H](N)C(=O)N1CCC[C@H]1C(=O)OC(C)(C)C>>CCOC(=O)[C@H](CC(=O)c1ccccc1)N[C@@H](C)C(=O)N1CCC[C@H]1C(=O)OC(C)(C)C
C(C)(C)(C)OC([C@H]1N(CCC1)C([C@@H](N)C)=O)=O.C(C)OC(\C=C\C(C1=CC=CC=C1)=O)=O.C(\C=C/C(=O)O)(=O)O>>C(\C=C/C(=O)O)(=O)O.C(C)(C)(C)OC([C@H]1N(CCC1)C([C@@H](N[C@@H](CC(=O)C1=CC=CC=C1)C(=O)OCC)C)=O)=O
[CH3:1][CH2:2][O:3][C:4](=[O:5])/[CH:6]=[CH:7]/[C:8](=[O:9])[c:10]1[cH:11][cH:12][cH:13][cH:14][cH:15]1.[NH2:16][C@@H:17]([CH3:18])[C:19](=[O:20])[N:21]1[CH2:22][CH2:23][CH2:24][C@H:25]1[C:26](=[O:27])[O:28][C:29]([CH3:30])([CH3:31])[CH3:32]>>[CH3:1][CH2:2][O:3][C:4](=[O:5])[C@H:6]([CH2:7][C:8](=[O:9])[c:10]1[cH:11][cH...
CCOC(=O)/C=C/C(=O)c1ccccc1.C[C@H](N)C(=O)N1CCC[C@H]1C(=O)OC(C)(C)C
CCOC(=O)[C@H](CC(=O)c1ccccc1)N[C@@H](C)C(=O)N1CCC[C@H]1C(=O)OC(C)(C)C
null
null
C1=CC=CC=C1
Heteroatom Alkylation and Arylation
aza-Michael addition primary
f23c1d33294f7c2373748c5c22b15927f476391e752421c17b512248b86c26cb
f96ab441d5d582a398da5dd243d1e594dd5722bfce5951b92a99ef0632ea2683
O=C(CCNCC(=O)N1CCCC1)c1ccccc1
[#8:1]-[C:2](=[O;D1;H0:3])-[C:4]-[#7:5](-[C:6](=[O;D1;H0:7])-[C:8](-[C;D1;H3:9])-[NH2;D1;+0:10])-[C:11].[C:12]-[#8:13]-[C:14](=[O;D1;H0:15])/[CH;D2;+0:16]=[CH;D2;+0:17]/[C:18](=[O;D1;H0:19])-[c:20]>>[#8:1]-[C:2](=[O;D1;H0:3])-[C:4]-[#7:5](-[C:6](=[O;D1;H0:7])-[C:8](-[C;D1;H3:9])-[NH;D2;+0:10]-[C@@H;D3;+0:16](-[CH2;D2;+...
60
[{"value": 60.0, "product": "C(\\C=C/C(=O)O)(=O)O.C(C)(C)(C)OC([C@H]1N(CCC1)C([C@@H](N[C@@H](CC(=O)C1=CC=CC=C1)C(=O)OCC)C)=O)=O", "details": "PERCENTYIELD", "is_desired": false}, {"value": 59.5, "product": "C(\\C=C/C(=O)O)(=O)O.C(C)(C)(C)OC([C@H]1N(CCC1)C([C@@H](N[C@@H](CC(=O)C1=CC=CC=C1)C(=O)OCC)C)=O)=O", "details": "...
null
null
null
null
4.84 g (20 mmoles) of (S)-alanyl-(S)-proline-t-butylester are dissolved in 40 ml of dry benzene and 4.08 g (20 mmoles) of E-ethyl-3-benzoyl-acrylate are added at room temperature under stirring. After one hour stirring at room temperature the solvent is evaporated off under reduced pressure, the residue is dissolved in...
10.6084/m9.figshare.5104873.v1
null
Ketone.Ester.Primary amine
Ketone.Ester.Secondary amine
null
null
c1ccccc1.C1CC[NH]C1
null
C1=CC=CC=C1
null
null
CCOC(=O)/C=C/C(=O)c1ccccc1.C[C@H](N)C(=O)N1CCC[C@H]1C(=O)OC(C)(C)C>C1=CC=CC=C1>CCOC(=O)[C@H](CC(=O)c1ccccc1)N[C@@H](C)C(=O)N1CCC[C@H]1C(=O)OC(C)(C)C
ord_dataset-01dbb772c5e249108f0b191ed17a2c0c
ord-b8a5aa9b39d74e0b898f76e9233cf62f
CC(C)(C)OC(=O)NCCCC[C@H](N)C(=O)N1CCC[C@H]1C(=O)OC(C)(C)C.CCOC(=O)/C=C/C(=O)c1ccccc1>>CCOC(=O)[C@H](CC(=O)c1ccccc1)N[C@@H](CCCCNC(=O)OC(C)(C)C)C(=O)N1CCC[C@H]1C(=O)OC(C)(C)C
C(C)(=O)OCC.C(C)(C)(C)OC([C@H]1N(CCC1)C([C@@H](N)CCCCNC(=O)OC(C)(C)C)=O)=O.C(C)OC(\C=C\C(C1=CC=CC=C1)=O)=O>>C(C)(C)(C)OC([C@H]1N(CCC1)C([C@@H](N[C@@H](CC(=O)C1=CC=CC=C1)C(=O)OCC)CCCCNC(=O)OC(C)(C)C)=O)=O
[NH2:16][C@@H:17]([CH2:18][CH2:19][CH2:20][CH2:21][NH:22][C:23](=[O:24])[O:25][C:26]([CH3:27])([CH3:28])[CH3:29])[C:30](=[O:31])[N:32]1[CH2:33][CH2:34][CH2:35][C@H:36]1[C:37](=[O:38])[O:39][C:40]([CH3:41])([CH3:42])[CH3:43].[CH3:1][CH2:2][O:3][C:4](=[O:5])/[CH:6]=[CH:7]/[C:8](=[O:9])[c:10]1[cH:11][cH:12][cH:13][cH:14][...
CC(C)(C)OC(=O)NCCCC[C@H](N)C(=O)N1CCC[C@H]1C(=O)OC(C)(C)C.CCOC(=O)/C=C/C(=O)c1ccccc1
CCOC(=O)[C@H](CC(=O)c1ccccc1)N[C@@H](CCCCNC(=O)OC(C)(C)C)C(=O)N1CCC[C@H]1C(=O)OC(C)(C)C
null
null
CCOCC.C(C)OCC
Heteroatom Alkylation and Arylation
aza-Michael addition primary
f23c1d33294f7c2373748c5c22b15927f476391e752421c17b512248b86c26cb
f96ab441d5d582a398da5dd243d1e594dd5722bfce5951b92a99ef0632ea2683
O=C(CCNCC(=O)N1CCCC1)c1ccccc1
[#8:1]-[C:2](=[O;D1;H0:3])-[C:4]-[#7:5](-[C:6](=[O;D1;H0:7])-[C:8](-[C:9])-[NH2;D1;+0:10])-[C:11].[C:12]-[#8:13]-[C:14](=[O;D1;H0:15])/[CH;D2;+0:16]=[CH;D2;+0:17]/[C:18](=[O;D1;H0:19])-[c:20]>>[#8:1]-[C:2](=[O;D1;H0:3])-[C:4]-[#7:5](-[C:6](=[O;D1;H0:7])-[C:8](-[C:9])-[NH;D2;+0:10]-[C@@H;D3;+0:16](-[CH2;D2;+0:17]-[C:18]...
null
[]
null
null
5
HOUR
8.0 g (20 mmoles) of Nε -t-butoxycarbonyl-(S)-lysyl-(S)-proline-t-butylester are dissolved in 100 ml of diethyl ether and 4.48 g (22 mmoles) of E-ethyl-3-benzoyl-acrylate are added to the solution. The reaction mixture is stirred at room temperature for 5 hours. After evaporation of the solvent the title product is iso...
10.6084/m9.figshare.5104873.v1
null
Ketone.Ester.Primary amine
Ketone.Ester.Secondary amine
null
null
c1ccccc1.C1CC[NH]C1
null
CCOCC.C(C)OCC
null
5
CC(C)(C)OC(=O)NCCCC[C@H](N)C(=O)N1CCC[C@H]1C(=O)OC(C)(C)C.CCOC(=O)/C=C/C(=O)c1ccccc1>CCOCC.C(C)OCC>CCOC(=O)[C@H](CC(=O)c1ccccc1)N[C@@H](CCCCNC(=O)OC(C)(C)C)C(=O)N1CCC[C@H]1C(=O)OC(C)(C)C
ord_dataset-01dbb772c5e249108f0b191ed17a2c0c
ord-97da413a676c4eefa7c6d0c7176edaf1
C=C(C)C.CCCCOC(=O)CO>>CCCCOC(=O)COC(C)(C)C
CC(C)=C.C(CO)(=O)OCCCC.S(O)(O)(=O)=O>>C(C)(C)(C)OCC(=O)OCCCC
[C:10]([CH3:11])(=[CH2:12])[CH3:13].[CH3:1][CH2:2][CH2:3][CH2:4][O:5][C:6](=[O:7])[CH2:8][OH:9]>>[CH3:1][CH2:2][CH2:3][CH2:4][O:5][C:6](=[O:7])[CH2:8][O:9][C:10]([CH3:11])([CH3:12])[CH3:13]
C=C(C)C.CCCCOC(=O)CO
CCCCOC(=O)COC(C)(C)C
null
null
C(Cl)Cl
Heteroatom Alkylation and Arylation
OtherReaction
f7c7da7c78eb65b9b2c8f63d0f16c4d5887e45e01ac1a9ea608f777c535e8cd7
d7c87de309863ac8797e1e336d1d5992291f9ca863376e68ebcf1e8fd5f0e442
null
[C;D1;H3:1]-[C;H0;D3;+0:2](-[C;D1;H3:3])=[CH2;D1;+0:4].[C:5]-[#8:6]-[C:7](=[O;D1;H0:8])-[C:9]-[OH;D1;+0:10]>>[C:5]-[#8:6]-[C:7](=[O;D1;H0:8])-[C:9]-[O;H0;D2;+0:10]-[C;H0;D4;+0:2](-[C;D1;H3:1])(-[C;D1;H3:3])-[CH3;D1;+0:4]
null
[]
null
null
3
DAY
A 500-ml, thick-walled Erlenynmeyer flask equipped with a magnetic stirring bar was cooled to -78° C. (dry iece-acetone bath) and charged with isobutylene (150 ml). Then, n-butyl glycolate (20.0 g, 0.151 mol) and 50 ml of methylene chloride was added along with 1 ml of concentrated sulfuric acid. The cold bath was remo...
10.6084/m9.figshare.5104873.v1
null
Primary alcohol.Vinyl
Ether
null
null
null
null
C(Cl)Cl
null
72
C=C(C)C.CCCCOC(=O)CO>C(Cl)Cl>CCCCOC(=O)COC(C)(C)C
ord_dataset-01dbb772c5e249108f0b191ed17a2c0c
ord-683c16909174462faf1b49adbea715f3
CCCCOC(=O)COC(C)(C)C>>CC(C)(C)OCC(=O)O
C([O-])([O-])=O.[K+].[K+].C(C)(C)(C)OCC(=O)OCCCC>>C(C)(C)(C)OCC(=O)O
CCCC[O:9][C:7]([CH2:6][O:5][C:2]([CH3:1])([CH3:3])[CH3:4])=[O:8]>>[CH3:1][C:2]([CH3:3])([CH3:4])[O:5][CH2:6][C:7](=[O:8])[OH:9]
CCCCOC(=O)COC(C)(C)C
CC(C)(C)OCC(=O)O
null
null
CO.O
Deprotection
Ester saponification (alkyl deprotection)
d872e08ad5c85a4add6cd04e6e987e73fead5f79b3f30ba61a81ba5029b29894
38ae1ee78433b9acfb0390501446149c80f88f23ac2d84c60b3369bdab75cec9
null
C-C-C-C-[O;H0;D2;+0:1]-[C:2](-[C:3])=[O;D1;H0:4]>>[C:3]-[C:2](=[O;D1;H0:4])-[OH;D1;+0:1]
null
[]
0
CELSIUS
null
null
To 100 ml of a 50:50 (v/v) methanol/water solution containing 14.35 g of potassium carbonate, was added n-butyl 2-tert-butoxyacetate (6.50 g, 0.0346 mol). The mixture was heated at reflux for 17 hours and the volatiles removed on a flash evaporator. The remaining solution was cooled to approximately 0° C. and acidified...
10.6084/m9.figshare.5104873.v1
null
Ester
Carboxylic acid
null
null
null
Other
CO.O
0
null
CCCCOC(=O)COC(C)(C)C>CO.O>CC(C)(C)OCC(=O)O
ord_dataset-01dbb772c5e249108f0b191ed17a2c0c
ord-735fc3dbd8da40b9ad499f1ee9ee5a7e
ClCc1ccc2ccccc2n1.Oc1ccccc1>>c1ccc(OCc2ccc3ccccc3n2)cc1
ClCC1=NC2=CC=CC=C2C=C1.C1(=CC=CC=C1)O.C([O-])([O-])=O.[K+].[K+].C([O-])([O-])=O.[Cs+].[Cs+].[I-].[Na+]>>O(C1=CC=CC=C1)CC1=NC2=CC=CC=C2C=C1
Cl[CH2:6][c:7]1[cH:8][cH:9][c:10]2[cH:11][cH:12][cH:13][cH:14][c:15]2[n:16]1.[cH:1]1[cH:2][cH:3][c:4]([OH:5])[cH:17][cH:18]1>>[cH:1]1[cH:2][cH:3][c:4]([O:5][CH2:6][c:7]2[cH:8][cH:9][c:10]3[cH:11][cH:12][cH:13][cH:14][c:15]3[n:16]2)[cH:17][cH:18]1
ClCc1ccc2ccccc2n1.Oc1ccccc1
c1ccc(OCc2ccc3ccccc3n2)cc1
null
null
CC(=O)C
Heteroatom Alkylation and Arylation
Williamson Ether Synthesis
7e1040116e3a4cf0e8ec5cc7865388d9cd0efabce6d320a1c25a36e411018d8b
d5f4610d46ccc0478471c5bc0fb862644eaf764bbc5d93badb39d54f6ec8e0a5
c1ccc(OCc2ccc3ccccc3n2)cc1
Cl-[CH2;D2;+0:1]-[c:2](:[c:3]):[#7;a:4]:[c:5].[OH;D1;+0:6]-[c:7](:[c:8]):[c:9]>>[c:5]:[#7;a:4]:[c:2](-[CH2;D2;+0:1]-[O;H0;D2;+0:6]-[c:7](:[c:8]):[c:9]):[c:3]
null
[]
null
null
null
null
A mixture of 2-chloromethyl quinoline (0.05 mol), phenol (0.055 mol), finely powdered potassium carbonate (0.055 mol), cesium carbonate (0.005 mol) and sodium iodide (0.0025 mol) in acetone was refluxed for about 4 hours. The reaction mixture was cooled to room temperature and filtered and the filtrate was concentrated...
10.6084/m9.figshare.5104873.v1
null
Primary halide.Aromatic alcohol
Ether
null
null
c1ccccc1.c1ccc2ncccc2c1
HCl
CC(=O)C
null
null
ClCc1ccc2ccccc2n1.Oc1ccccc1>CC(=O)C>c1ccc(OCc2ccc3ccccc3n2)cc1
ord_dataset-01dbb772c5e249108f0b191ed17a2c0c
ord-69d6dd0a63e846cc9ea6cbd2d9d2af27
O=[N+]([O-])c1ccc(O)cc1.Oc1ccccc1>>O=[N+]([O-])c1ccc(OCc2ccc3ccccc3n2)cc1
C1=CC(=CC=C1[N+](=O)[O-])O.C1(=CC=CC=C1)O>>[N+](=O)([O-])C1=CC=C(OCC2=NC3=CC=CC=C3C=C2)C=C1
[O:1]=[N+:2]([O-:3])[c:4]1[cH:5][cH:6][c:7]([OH:8])[cH:20][cH:21]1.O[c:9]1[cH:11][cH:17][cH:16][cH:15][cH:14]1>>[O:1]=[N+:2]([O-:3])[c:4]1[cH:5][cH:6][c:7]([O:8][CH2:9][c:10]2[cH:11][cH:12][c:13]3[cH:14][cH:15][cH:16][cH:17][c:18]3[n:19]2)[cH:20][cH:21]1
O=[N+]([O-])c1ccc(O)cc1.Oc1ccccc1
O=[N+]([O-])c1ccc(OCc2ccc3ccccc3n2)cc1
null
null
null
Aromatic Heterocycle Formation
OtherReaction
46ea60c0a6998c6f5c81dcefe587c0e7eb13f574231f11ea0e6d1812799c5e68
055aebb1401c8b073f067057dba15f6b45e1b6d8b27a6d27ee14b797b8e2ceae
c1ccc(OCc2ccc3ccccc3n2)cc1
O-[c;H0;D3;+0:1]1:[cH;D2;+0:2]:[cH;D2;+0:3]:[c:4]:[c:5]:[cH;D2;+0:6]:1.[OH;D1;+0:7]-[c:8](:[c:9]):[c:10]>>[c:9]:[c:8](-[O;H0;D2;+0:7]-[CH2;D2;+0:1]-[c:11]1:[#7;a:12]:[c:13]2:[cH;D2;+0:3]:[c:4]:[c:5]:[cH;D2;+0:6]:[c:14]:2:[c:15]:[cH;D2;+0:2]:1):[c:10]
null
[]
null
null
null
null
This compound was prepared in an identical manner as described in Example 1, except p-nitrophenol was substituted for phenol, m.p. 142°-143° C. Conditions: See reaction.notes.procedure_details. Workup: This compound was prepared in an identical manner
10.6084/m9.figshare.5104873.v1
null
Aromatic alcohol.Aromatic alcohol
Ether
c1ccccc1
c1ccc2ncccc2c1
c1ccccc1.c1ccc2ncccc2c1
null
null
null
null
O=[N+]([O-])c1ccc(O)cc1.Oc1ccccc1>>O=[N+]([O-])c1ccc(OCc2ccc3ccccc3n2)cc1
ord_dataset-01dbb772c5e249108f0b191ed17a2c0c
ord-3b691c0f3b274492971e450bdceebda6
NNc1ccc(F)cc1.O=C1CCCC(=O)C1>>OC1=CC(=NNc2ccc(F)cc2)CCC1
C1(CC(CCC1)=O)=O.Cl.FC1=CC=C(C=C1)NN.[OH-].[Na+]>>FC1=CC=C(C=C1)NN=C1C=C(CCC1)O
[NH2:5][NH:6][c:7]1[cH:8][cH:9][c:10]([F:11])[cH:12][cH:13]1.O=[C:4]1[CH2:3][C:2](=[O:1])[CH2:16][CH2:15][CH2:14]1>>[OH:1][C:2]1=[CH:3][C:4](=[N:5][NH:6][c:7]2[cH:8][cH:9][c:10]([F:11])[cH:12][cH:13]2)[CH2:14][CH2:15][CH2:16]1
NNc1ccc(F)cc1.O=C1CCCC(=O)C1
OC1=CC(=NNc2ccc(F)cc2)CCC1
null
null
O
Acylation
OtherReaction
4588bc0ac913444b8772115fc2d17c8f8adb352d295d5f09b850098e26b0afb9
aeed7f7f446135028f4c8b0de72f1d32a303d1e6e825e26d145e859295b3da3e
C1=CC(=NNc2ccccc2)CCC1
O=[C;H0;D3;+0:1]1-[C:2]-[C:3]-[C:4]-[C;H0;D3;+0:5](=[O;H0;D1;+0:6])-[CH2;D2;+0:7]-1.[NH2;D1;+0:8]-[#7:9]-[c:10]>>[OH;D1;+0:6]-[C;H0;D3;+0:5]1=[CH;D2;+0:7]-[C;H0;D3;+0:1](=[N;H0;D2;+0:8]-[#7:9]-[c:10])-[C:2]-[C:3]-[C:4]-1
96.4
[{"value": 96.4, "product": "FC1=CC=C(C=C1)NN=C1C=C(CCC1)O", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
30
MINUTE
A suspension of 4-fluorophenylhydrazine hydrochloride (50 g) in water (500 ml) was treated with sodium hydroxide (12.3 g) in water (50 ml) and the resultant solution added to solution of cyclohexane-1,3-dione (97%, 35.6 g) in water (300 ml) over 2 h under nitrogen with stirring. After a further 30 min, the precipitate ...
10.6084/m9.figshare.5104873.v1
null
Hydrazine.Ketone.Ketone
Hydrazone.Enol
C1CCCCC1
C1=CCCCC1
C1=CCCCC1.c1ccccc1
HO-
O
null
0.5
NNc1ccc(F)cc1.O=C1CCCC(=O)C1>O>OC1=CC(=NNc2ccc(F)cc2)CCC1
ord_dataset-01dbb772c5e249108f0b191ed17a2c0c
ord-76b14a9408c64659932b886070897fcf
COS(=O)(=O)OC.O=C1CCCc2[nH]c3ccc(F)cc3c21>>Cn1c2c(c3cc(F)ccc31)C(=O)CCC2
FC=1C=C2C=3C(CCCC3NC2=CC1)=O.C([O-])([O-])=O.[K+].[K+].COS(=O)(=O)OC>>FC=1C=C2C=3C(CCCC3N(C2=CC1)C)=O
COS(=O)(=O)O[CH3:1].[nH:2]1[c:3]2[c:4]([c:5]3[cH:6][c:7]([F:8])[cH:9][cH:10][c:11]13)[C:12](=[O:13])[CH2:14][CH2:15][CH2:16]2>>[CH3:1][n:2]1[c:3]2[c:4]([c:5]3[cH:6][c:7]([F:8])[cH:9][cH:10][c:11]13)[C:12](=[O:13])[CH2:14][CH2:15][CH2:16]2
COS(=O)(=O)OC.O=C1CCCc2[nH]c3ccc(F)cc3c21
Cn1c2c(c3cc(F)ccc31)C(=O)CCC2
null
null
CC(=O)C
Heteroatom Alkylation and Arylation
N-methylation
30cbab1101db21674c61864f82b5b188234804a6cfd88c5e783305d37b85c63f
7a358c636daddc97c1fb4c29f378044d7eac3f01815d9966e599841f642d631a
O=C1CCCc2[nH]c3ccccc3c21
C-O-S(=O)(=O)-O-[CH3;D1;+0:1].[C:2]-[c:3]1:[nH;D2;+0:4]:[c:5](:[c:6]):[c:7]:[c:8]:1-[C:9]=[O;D1;H0:10]>>[C:2]-[c:3]1:[c:8](:[c:7]:[c:5](:[c:6]):[n;H0;D3;+0:4]:1-[CH3;D1;+0:1])-[C:9]=[O;D1;H0:10]
97.5
[{"value": 97.5, "product": "FC=1C=C2C=3C(CCCC3N(C2=CC1)C)=O", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
30
MINUTE
The product of Stage (ii) (7.28 g), potassium carbonate (9.90 g), acetone (70 ml), and dimethylsulphate (5.1 ml) were vigorously stirred at room temperature overnight under nitrogen. The mixture was concentrated to one half of its volume and then stirred with water (350 ml) for 30 min. The mixture was filtered off, was...
10.6084/m9.figshare.5104873.v1
null
null
null
c1ccc2c3c([nH]c2c1)CCCC3
C1CCCc2[nH]c3ccccc3c21
C1CCCc2[nH]c3ccccc3c21
HO-
CC(=O)C
null
0.5
COS(=O)(=O)OC.O=C1CCCc2[nH]c3ccc(F)cc3c21>CC(=O)C>Cn1c2c(c3cc(F)ccc31)C(=O)CCC2
ord_dataset-01dbb772c5e249108f0b191ed17a2c0c
ord-cc2dc59ce3544cd8a5c808b61203bdd1
NNc1ccc(Br)cc1.O=C1CCCC(=O)C1>>O=C1CCCC(=NNc2ccc(Br)cc2)C1
Cl.BrC1=CC=C(C=C1)NN.C1(CC(CCC1)=O)=O>>BrC1=CC=C(C=C1)NN=C1CC(CCC1)=O
[NH2:7][NH:8][c:9]1[cH:10][cH:11][c:12]([Br:13])[cH:14][cH:15]1.O=[C:6]1[CH2:5][CH2:4][CH2:3][C:2](=[O:1])[CH2:16]1>>[O:1]=[C:2]1[CH2:3][CH2:4][CH2:5][C:6](=[N:7][NH:8][c:9]2[cH:10][cH:11][c:12]([Br:13])[cH:14][cH:15]2)[CH2:16]1
NNc1ccc(Br)cc1.O=C1CCCC(=O)C1
O=C1CCCC(=NNc2ccc(Br)cc2)C1
null
null
O
Heteroatom Alkylation and Arylation
OtherReaction
8fd42c3afb34fc209a626759948c4bd78aa782c38787b900b74e01ff0893a4bd
16267fcabf9e555e6c245927fd3675c621f876db12f50a1b3e8576a12e06a1cf
O=C1CCCC(=NNc2ccccc2)C1
O=[C;H0;D3;+0:1]1-[C:2]-[C:3](=[O;D1;H0:4])-[C:5]-[C:6]-[C:7]-1.[NH2;D1;+0:8]-[#7:9]-[c:10]>>[O;D1;H0:4]=[C:3]1-[C:2]-[C;H0;D3;+0:1](=[N;H0;D2;+0:8]-[#7:9]-[c:10])-[C:7]-[C:6]-[C:5]-1
null
[]
null
null
null
null
A solution of 4-bromophenylhydrazine hydrochloride (2.24 g) and 1,3-cyclohexanedione (1.23 g) in water (60 ml) was stirred at room temperature for 1 h, giving a precipitate. The solid title compound was filtered off and dried (1.63 g). t.l.c (D), Rf 0.35 On cooling a second crop was obtained (0.395 g) Conditions: See r...
10.6084/m9.figshare.5104873.v1
null
Hydrazine.Ketone
Hydrazone
C1CCCCC1
C1CCCCC1
C1CCCCC1.c1ccccc1
HO-
O
null
null
NNc1ccc(Br)cc1.O=C1CCCC(=O)C1>O>O=C1CCCC(=NNc2ccc(Br)cc2)C1
ord_dataset-01dbb772c5e249108f0b191ed17a2c0c
ord-477e144581644ea4bec3777f5ed06716
O=C1CCCC(=NNc2ccc(Br)cc2)C1>>O=C1CCCc2[nH]c3ccc(Br)cc3c21
BrC1=CC=C(C=C1)NN=C1CC(CCC1)=O.O>>BrC=1C=C2C=3C(CCCC3NC2=CC1)=O
N([N:7]=[C:6]1[CH2:5][CH2:4][CH2:3][C:2](=[O:1])[CH2:15]1)[c:8]1[cH:9][cH:10][c:11]([Br:12])[cH:13][cH:14]1>>[O:1]=[C:2]1[CH2:3][CH2:4][CH2:5][c:6]2[nH:7][c:8]3[cH:9][cH:10][c:11]([Br:12])[cH:13][c:14]3[c:15]21
O=C1CCCC(=NNc2ccc(Br)cc2)C1
O=C1CCCc2[nH]c3ccc(Br)cc3c21
null
[Cl-].[Zn+2].[Cl-]
C(C)(=O)O
Aromatic Heterocycle Formation
OtherReaction
5e9560b6cda3347248de8b7acae96ba24659bf5628d876729bf51ef333dea93f
6158bf86826c5f774a824bd0f476ebd74135d9604cccee336f26a5f9efada43a
O=C1CCCc2[nH]c3ccccc3c21
[O;D1;H0:1]=[C:2]1-[C:3]-[C:4]-[C:5]-[C;H0;D3;+0:6](=[N;H0;D2;+0:7]-N-[c;H0;D3;+0:8]2:[c:9]:[c:10]:[c:11]:[c:12]:[cH;D2;+0:13]:2)-[CH2;D2;+0:14]-1>>[O;D1;H0:1]=[C:2]1-[C:3]-[C:4]-[C:5]-[c;H0;D3;+0:6]2:[nH;D2;+0:7]:[c;H0;D3;+0:8]3:[c:9]:[c:10]:[c:11]:[c:12]:[c;H0;D3;+0:13]:3:[c;H0;D3;+0:14]:2-1
null
[]
null
null
null
null
The product of Stage (i) (1.5 g) was heated under reflux with dry zinc chloride (16 g) in glacial acetic acid (75 ml) for 24 h. The mixture was cooled, poured into water (200 ml), and the resulting solid filtered off and dried (0.95 g). Purification by flash chromatography (E) gave the title compound as a solid (125 mg...
10.6084/m9.figshare.5104873.v1
null
Hydrazone.Ketone
Ketone
C1CCCCC1.c1ccccc1
c1ccc2c3c([nH]c2c1)CCCC3
c1ccc2c3c([nH]c2c1)CCCC3
Other
[Cl-].[Zn+2].[Cl-].C(C)(=O)O
null
null
O=C1CCCC(=NNc2ccc(Br)cc2)C1>[Cl-].[Zn+2].[Cl-].C(C)(=O)O>O=C1CCCc2[nH]c3ccc(Br)cc3c21
ord_dataset-01dbb772c5e249108f0b191ed17a2c0c
ord-a26e6327d94044e097c670375d9520d2
C=O.CNC.Cn1c2c(c3cc(Br)ccc31)C(=O)CCC2>>CN(C)CC1CCc2c(c3cc(Br)ccc3n2C)C1=O
O.C=O.Cl.CNC.BrC=1C=C2C=3C(CCCC3N(C2=CC1)C)=O>>Cl.BrC=1C=C2C=3C(C(CCC3N(C2=CC1)C)CN(C)C)=O
O=[CH2:4].[CH3:1][NH:2][CH3:3].[CH2:5]1[CH2:6][CH2:7][c:8]2[c:9]([c:10]3[cH:11][c:12]([Br:13])[cH:14][cH:15][c:16]3[n:17]2[CH3:18])[C:19]1=[O:20]>>[CH3:1][N:2]([CH3:3])[CH2:4][CH:5]1[CH2:6][CH2:7][c:8]2[c:9]([c:10]3[cH:11][c:12]([Br:13])[cH:14][cH:15][c:16]3[n:17]2[CH3:18])[C:19]1=[O:20]
C=O.CNC.Cn1c2c(c3cc(Br)ccc31)C(=O)CCC2
CN(C)CC1CCc2c(c3cc(Br)ccc3n2C)C1=O
null
null
C(C)(=O)O
Heteroatom Alkylation and Arylation
OtherReaction
c1a45b1ac40a56543412022e9be077adade507f2494f6aa3371281dd5be7791c
e8784011446fecd0a9b69948eec8f6e670a0f5952d23e21c3e86b629168fc3f8
O=C1CCCc2[nH]c3ccccc3c21
O=[CH2;D1;+0:1].[#7;a:2]:[c:3]1:[c:4]-[C:5](=[O;D1;H0:6])-[CH2;D2;+0:7]-[C:8]-[C:9]-1.[C;D1;H3:10]-[NH;D2;+0:11]-[C;D1;H3:12]>>[#7;a:2]:[c:3]1:[c:4]-[C:5](=[O;D1;H0:6])-[CH;D3;+0:7](-[CH2;D2;+0:1]-[N;H0;D3;+0:11](-[C;D1;H3:10])-[C;D1;H3:12])-[C:8]-[C:9]-1
67.3
[{"value": 67.3, "product": "Cl.BrC=1C=C2C=3C(C(CCC3N(C2=CC1)C)CN(C)C)=O", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
null
null
Paraformaldehyde (1.5 g) and dimethylamine hydrochloride (3.75 g) were added to a solution of the product of Stage (iii) (10 g) in acetic acid (70 ml) and then heated to reflux for 8 h. On cooling to ambient temperature the reaction mixture was poured into water (400 ml). The oil which separated out was triturated with...
10.6084/m9.figshare.5104873.v1
null
Formaldehyde.Ketone.Secondary amine
Ketone.Tertiary amine
C1CCCc2[nH]c3ccccc3c21
C1[CH]CCc2[nH]c3ccccc3c21
C1[CH]CCc2[nH]c3ccccc3c21
HO-
C(C)(=O)O
null
null
C=O.CNC.Cn1c2c(c3cc(Br)ccc31)C(=O)CCC2>C(C)(=O)O>CN(C)CC1CCc2c(c3cc(Br)ccc3n2C)C1=O
ord_dataset-01dbb772c5e249108f0b191ed17a2c0c
ord-313df49ceb1b4c6cb32f2cf23619645d
COc1ccc(NN)cc1.O=C1CCCC(=O)C1>>COc1ccc2[nH]c3c(c2c1)C(=O)CCC3
C1(CC(CCC1)=O)=O.Cl.COC1=CC=C(C=C1)NN>>COC=1C=C2C=3C(CCCC3NC2=CC1)=O
N[NH:7][c:6]1[cH:5][cH:4][c:3]([O:2][CH3:1])[cH:11][cH:10]1.O=[C:8]1[CH2:9][C:12](=[O:13])[CH2:14][CH2:15][CH2:16]1>>[CH3:1][O:2][c:3]1[cH:4][cH:5][c:6]2[nH:7][c:8]3[c:9]([c:10]2[cH:11]1)[C:12](=[O:13])[CH2:14][CH2:15][CH2:16]3
COc1ccc(NN)cc1.O=C1CCCC(=O)C1
COc1ccc2[nH]c3c(c2c1)C(=O)CCC3
null
null
C(C)O.O
Aromatic Heterocycle Formation
OtherReaction
216d1a60c6e7a9cb1b0c8014f08184065b33ea82af906e7694cae36b12f075b9
0b5a1886fc2038f5ee65b48e06759bc9de0979200ef7d47d3e0b760c7f7778a8
O=C1CCCc2[nH]c3ccccc3c21
N-[NH;D2;+0:1]-[c:2](:[c:3]):[cH;D2;+0:4]:[c:5]:[c:6].O=[C;H0;D3;+0:7]1-[C:8]-[C:9]-[C:10]-[C:11](=[O;D1;H0:12])-[CH2;D2;+0:13]-1>>[O;D1;H0:12]=[C:11]1-[C:10]-[C:9]-[C:8]-[c;H0;D3;+0:7]2:[nH;D2;+0:1]:[c:2](:[c:3]):[c;H0;D3;+0:4](:[c:5]:[c:6]):[c;H0;D3;+0:13]:2-1
48.7
[{"value": 48.7, "product": "COC=1C=C2C=3C(CCCC3NC2=CC1)=O", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
3
HOUR
1,3-Cyclohexanedione (8 g) was added to a solution of 4-methoxyphenylhydrazine hydrochloride (10 g) in ethanol (350 ml) and water (70 ml). The resulting solution was stirred at room temperature for 3 h and then at reflux for 14 h. On cooling to ambient temperature, the reaction mixture was poured into water (3 l) to gi...
10.6084/m9.figshare.5104873.v1
null
Hydrazine.Ketone.Ketone
Ketone
c1ccccc1.C1CCCCC1
c1ccc2c3c([nH]c2c1)CCCC3
c1ccc2c3c([nH]c2c1)CCCC3
HO-
C(C)O.O
null
3
COc1ccc(NN)cc1.O=C1CCCC(=O)C1>C(C)O.O>COc1ccc2[nH]c3c(c2c1)C(=O)CCC3
ord_dataset-01dbb772c5e249108f0b191ed17a2c0c
ord-1ac4895b46ac455b903ac181d0e5e30d
COS(=O)(=O)OC.COc1ccc2[nH]c3c(c2c1)C(=O)CCC3>>COc1ccc2c(c1)c1c(n2C)CCCC1=O
O.C([O-])([O-])=O.[K+].[K+].COC=1C=C2C=3C(CCCC3NC2=CC1)=O.S(=O)(=O)(OC)OC>>COC=1C=C2C=3C(CCCC3N(C2=CC1)C)=O
COS(=O)(=O)O[CH3:12].[CH3:1][O:2][c:3]1[cH:4][cH:5][c:6]2[c:7]([cH:8]1)[c:9]1[c:10]([nH:11]2)[CH2:13][CH2:14][CH2:15][C:16]1=[O:17]>>[CH3:1][O:2][c:3]1[cH:4][cH:5][c:6]2[c:7]([cH:8]1)[c:9]1[c:10]([n:11]2[CH3:12])[CH2:13][CH2:14][CH2:15][C:16]1=[O:17]
COS(=O)(=O)OC.COc1ccc2[nH]c3c(c2c1)C(=O)CCC3
COc1ccc2c(c1)c1c(n2C)CCCC1=O
null
null
CC(=O)C
Heteroatom Alkylation and Arylation
N-methylation
30cbab1101db21674c61864f82b5b188234804a6cfd88c5e783305d37b85c63f
7a358c636daddc97c1fb4c29f378044d7eac3f01815d9966e599841f642d631a
O=C1CCCc2[nH]c3ccccc3c21
C-O-S(=O)(=O)-O-[CH3;D1;+0:1].[C:2]-[c:3]1:[nH;D2;+0:4]:[c:5](:[c:6]):[c:7]:[c:8]:1-[C:9]=[O;D1;H0:10]>>[C:2]-[c:3]1:[c:8](:[c:7]:[c:5](:[c:6]):[n;H0;D3;+0:4]:1-[CH3;D1;+0:1])-[C:9]=[O;D1;H0:10]
78.2
[{"value": 78.2, "product": "COC=1C=C2C=3C(CCCC3N(C2=CC1)C)=O", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
30
MINUTE
Anhydrous potassium carbonate (2.24 g) was added to a solution of the product of Stage (i) (3 g) in acetone (30 ml) at room temperature and stirred for 30 min. Dimethyl sulphate (1.6 ml) was added and the mixture was heated to reflux for 4 h. The resulting solution was poured into water (150 ml) and the resulting preci...
10.6084/m9.figshare.5104873.v1
null
null
null
c1ccc2c3c([nH]c2c1)CCCC3
C1CCCc2[nH]c3ccccc3c21
C1CCCc2[nH]c3ccccc3c21
HO-
CC(=O)C
null
0.5
COS(=O)(=O)OC.COc1ccc2[nH]c3c(c2c1)C(=O)CCC3>CC(=O)C>COc1ccc2c(c1)c1c(n2C)CCCC1=O
ord_dataset-01dbb772c5e249108f0b191ed17a2c0c
ord-63297f81bc0d4054a9441052d946e9fe
Nc1ccc(OCc2ccccc2)cc1>>NNc1ccc(OCc2ccccc2)cc1
Cl.C(C1=CC=CC=C1)OC1=CC=C(N)C=C1.N(=O)[O-].[Na+]>>Cl.C1(=CC=CC=C1)COC1=CC=C(C=C1)NN
[NH2:3][c:4]1[cH:5][cH:6][c:7]([O:8][CH2:9][c:10]2[cH:11][cH:12][cH:13][cH:14][cH:15]2)[cH:16][cH:17]1>>[NH2:2][NH:3][c:4]1[cH:5][cH:6][c:7]([O:8][CH2:9][c:10]2[cH:11][cH:12][cH:13][cH:14][cH:15]2)[cH:16][cH:17]1
Nc1ccc(OCc2ccccc2)cc1
NNc1ccc(OCc2ccccc2)cc1
null
null
Cl.O
Miscellaneous
OtherReaction
c4079cd46dafde13b56adeac363106820ab4184dee8b1ca632594de2bba804bd
5c8e4e590249a630a16b10bd7a77b27600fffbea367a0b585a920dd877e5471b
c1ccc(COc2ccccc2)cc1
[NH2;D1;+0:1]-[c:2](:[c:3]):[c:4]>>[N;D1;H2:5]-[NH;D2;+0:1]-[c:2](:[c:3]):[c:4]
null
[]
null
null
1
HOUR
A solution of sodium nitrite (16.1 g) in water was added dropwise over a period of ca 0.75 h to a cold (salt-ice bath) stirred suspension of 4-benzyloxyaniline hydrochloride (50 g) in concentrated hydrochloric acid (120 ml). The temperature was kept between -6° and -12° during the addition and stirring was continued fo...
10.6084/m9.figshare.5104873.v1
null
Primary amine
Hydrazine
null
null
c1ccccc1.c1ccccc1
Other
Cl.O
null
1
Nc1ccc(OCc2ccccc2)cc1>Cl.O>NNc1ccc(OCc2ccccc2)cc1
ord_dataset-01dbb772c5e249108f0b191ed17a2c0c
ord-78fc489b6c4b4be39c7bb6d9b5564ba7
NNc1ccc(OCc2ccccc2)cc1.O=C1CCCC(=O)C1>>O=C1CCCc2[nH]c3ccc(OCc4ccccc4)cc3c21
C1(CC(CCC1)=O)=O.Cl.C1(=CC=CC=C1)COC1=CC=C(C=C1)NN>>C1(=CC=CC=C1)COC=1C=C2C=3C(CCCC3NC2=CC1)=O
N[NH:7][c:8]1[cH:9][cH:10][c:11]([O:12][CH2:13][c:14]2[cH:15][cH:16][cH:17][cH:18][cH:19]2)[cH:20][cH:21]1.O=[C:6]1[CH2:5][CH2:4][CH2:3][C:2](=[O:1])[CH2:22]1>>[O:1]=[C:2]1[CH2:3][CH2:4][CH2:5][c:6]2[nH:7][c:8]3[cH:9][cH:10][c:11]([O:12][CH2:13][c:14]4[cH:15][cH:16][cH:17][cH:18][cH:19]4)[cH:20][c:21]3[c:22]21
NNc1ccc(OCc2ccccc2)cc1.O=C1CCCC(=O)C1
O=C1CCCc2[nH]c3ccc(OCc4ccccc4)cc3c21
null
null
C(C)O.O
Aromatic Heterocycle Formation
OtherReaction
216d1a60c6e7a9cb1b0c8014f08184065b33ea82af906e7694cae36b12f075b9
0b5a1886fc2038f5ee65b48e06759bc9de0979200ef7d47d3e0b760c7f7778a8
O=C1CCCc2[nH]c3ccc(OCc4ccccc4)cc3c21
N-[NH;D2;+0:1]-[c:2](:[c:3]):[cH;D2;+0:4]:[c:5]:[c:6].O=[C;H0;D3;+0:7]1-[C:8]-[C:9]-[C:10]-[C:11](=[O;D1;H0:12])-[CH2;D2;+0:13]-1>>[O;D1;H0:12]=[C:11]1-[C:10]-[C:9]-[C:8]-[c;H0;D3;+0:7]2:[nH;D2;+0:1]:[c:2](:[c:3]):[c;H0;D3;+0:4](:[c:5]:[c:6]):[c;H0;D3;+0:13]:2-1
38.4
[{"value": 38.4, "product": "C1(=CC=CC=C1)COC=1C=C2C=3C(CCCC3NC2=CC1)=O", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
null
null
1,3-Cyclohexanedione (3.1 g) and the product of Stage (i) (5.6 g) in ethanol (196 ml) and water (39 ml) was stirred at room temperature for 3 h and then heated to reflux for 14 h. The resulting solution was allowed to cool, poured into water (500 ml) and the precipitate filtered and washed with isopropyl acetate and et...
10.6084/m9.figshare.5104873.v1
null
Hydrazine.Ketone.Ketone
Ketone
c1ccccc1.C1CCCCC1
c1ccc2c3c([nH]c2c1)CCCC3
c1ccc2c3c([nH]c2c1)CCCC3.c1ccccc1
HO-
C(C)O.O
null
null
NNc1ccc(OCc2ccccc2)cc1.O=C1CCCC(=O)C1>C(C)O.O>O=C1CCCc2[nH]c3ccc(OCc4ccccc4)cc3c21
ord_dataset-01dbb772c5e249108f0b191ed17a2c0c
ord-f29eda88a35249c99e36ce3a1f68295a
COc1cccc(N)c1>>COc1cccc(NN)c1
[Sn].Cl.COC=1C=C(N)C=CC1.Cl.N(=O)[O-].[Na+]>>Cl.COC=1C=C(C=CC1)NN
[CH3:1][O:2][c:3]1[cH:4][cH:5][cH:6][c:7]([NH2:8])[cH:10]1>>[CH3:1][O:2][c:3]1[cH:4][cH:5][cH:6][c:7]([NH:8][NH2:9])[cH:10]1
COc1cccc(N)c1
COc1cccc(NN)c1
null
null
O
Miscellaneous
OtherReaction
c4079cd46dafde13b56adeac363106820ab4184dee8b1ca632594de2bba804bd
5c8e4e590249a630a16b10bd7a77b27600fffbea367a0b585a920dd877e5471b
c1ccccc1
[NH2;D1;+0:1]-[c:2](:[c:3]):[c:4]>>[N;D1;H2:5]-[NH;D2;+0:1]-[c:2](:[c:3]):[c:4]
null
[]
null
null
null
null
A suspension of 3-methoxyaniline (10 g) in concentrated hydrochloric acid (85 ml) was stirred at ca. 0° and a solution of sodium nitrite (5.75 g) in water (25 ml) was slowly added over a period of 30 min keeping the temperature of the mixture at ca. 0°. After 1 h a solution of tin II chloride dihydrate (59 g) in concen...
10.6084/m9.figshare.5104873.v1
null
Primary amine
Hydrazine
null
null
c1ccccc1
Other
O
null
null
COc1cccc(N)c1>O>COc1cccc(NN)c1
ord_dataset-01dbb772c5e249108f0b191ed17a2c0c
ord-c419ae0f44f44e4fa86eadeb58039dce
Cn1c2c(c3cc(C#N)ccc31)C(=O)CCC2.O=S(=O)(O)O>>Cn1c2c(c3cc(C(N)=O)ccc31)C(=O)CCC2
CN1C2=CC=C(C=C2C=2C(CCCC12)=O)C#N.S(O)(O)(=O)=O>>CN1C2=CC=C(C=C2C=2C(CCCC12)=O)C(=O)N
[CH3:1][n:2]1[c:3]2[c:4]([c:5]3[cH:6][c:7]([C:8]#[N:9])[cH:11][cH:12][c:13]13)[C:14](=[O:15])[CH2:16][CH2:17][CH2:18]2.O=S(=O)(O)[OH:10]>>[CH3:1][n:2]1[c:3]2[c:4]([c:5]3[cH:6][c:7]([C:8]([NH2:9])=[O:10])[cH:11][cH:12][c:13]13)[C:14](=[O:15])[CH2:16][CH2:17][CH2:18]2
Cn1c2c(c3cc(C#N)ccc31)C(=O)CCC2.O=S(=O)(O)O
Cn1c2c(c3cc(C(N)=O)ccc31)C(=O)CCC2
null
null
null
Heteroatom Alkylation and Arylation
OtherReaction
1d1793919e847ed86dcb16487e62464531560dbf4782f9a5875bfe7e0477a3ec
d6f9d146e8ef95e62f1a3ab55a7e3b4ceec8856a5f71b6dccd4ad850f945b658
O=C1CCCc2[nH]c3ccccc3c21
O-S(=O)(=O)-[OH;D1;+0:1].[N;H0;D1;+0:2]#[C;H0;D2;+0:3]-[c:4](:[c:5]):[c:6]>>[NH2;D1;+0:2]-[C;H0;D3;+0:3](=[O;H0;D1;+0:1])-[c:4](:[c:5]):[c:6]
null
[]
null
null
null
null
A solution of the product of Stage (i) cyanonitrile (2.7 g) in concentrated sulphuric acid (30 ml) was heated at 80° for 1 h. The mixture was poured onto ice (ca. 500 g) to precipitate a solid which was filtered, washed with water (3×50 ml) and dried in vacuo to leave a solid (3.1 g). This was extracted with boiling ab...
10.6084/m9.figshare.5104873.v1
null
Nitrile
Primary amide
null
null
C1CCCc2[nH]c3ccccc3c21
Other
null
null
null
Cn1c2c(c3cc(C#N)ccc31)C(=O)CCC2.O=S(=O)(O)O>>Cn1c2c(c3cc(C(N)=O)ccc31)C(=O)CCC2
ord_dataset-01dbb772c5e249108f0b191ed17a2c0c
ord-45ebea4005c547ca92a07b1f8fb6a84c
C=O.CNC.Cn1c2c(c3cc(C(N)=O)ccc31)C(=O)CCC2>>CN(C)CC1CCc2c(c3cc(C(N)=O)ccc3n2C)C1=O
N.CN1C2=CC=C(C=C2C=2C(CCCC12)=O)C(=O)N.C=O.Cl.CNC>>CN(C)CC1CCC=2N(C3=CC=C(C=C3C2C1=O)C(=O)N)C
O=[CH2:4].[CH3:1][NH:2][CH3:3].[CH2:5]1[CH2:6][CH2:7][c:8]2[c:9]([c:10]3[cH:11][c:12]([C:13]([NH2:14])=[O:15])[cH:16][cH:17][c:18]3[n:19]2[CH3:20])[C:21]1=[O:22]>>[CH3:1][N:2]([CH3:3])[CH2:4][CH:5]1[CH2:6][CH2:7][c:8]2[c:9]([c:10]3[cH:11][c:12]([C:13]([NH2:14])=[O:15])[cH:16][cH:17][c:18]3[n:19]2[CH3:20])[C:21]1=[O:22]
C=O.CNC.Cn1c2c(c3cc(C(N)=O)ccc31)C(=O)CCC2
CN(C)CC1CCc2c(c3cc(C(N)=O)ccc3n2C)C1=O
null
null
C(C)(=O)O
Heteroatom Alkylation and Arylation
OtherReaction
c1a45b1ac40a56543412022e9be077adade507f2494f6aa3371281dd5be7791c
e8784011446fecd0a9b69948eec8f6e670a0f5952d23e21c3e86b629168fc3f8
O=C1CCCc2[nH]c3ccccc3c21
O=[CH2;D1;+0:1].[#7;a:2]:[c:3]1:[c:4]-[C:5](=[O;D1;H0:6])-[CH2;D2;+0:7]-[C:8]-[C:9]-1.[C;D1;H3:10]-[NH;D2;+0:11]-[C;D1;H3:12]>>[#7;a:2]:[c:3]1:[c:4]-[C:5](=[O;D1;H0:6])-[CH;D3;+0:7](-[CH2;D2;+0:1]-[N;H0;D3;+0:11](-[C;D1;H3:10])-[C;D1;H3:12])-[C:8]-[C:9]-1
null
[]
null
null
null
null
A mixture of the product of Stage (ii) (1.8 g), paraformaldehyde (0.3 g) and dimethylamine hydrochloride (0.75 g) in acetic acid (14 ml) was heated at 80°-100° under nitrogen for 2 h. The reaction mixture was cooled (20°), evaporated in vacuo and purified by flash chromatography (L) to give a foam. A sample (0.2 g) was...
10.6084/m9.figshare.5104873.v1
null
Formaldehyde.Ketone.Secondary amine
Ketone.Tertiary amine
C1CCCc2[nH]c3ccccc3c21
C1[CH]CCc2[nH]c3ccccc3c21
C1[CH]CCc2[nH]c3ccccc3c21
HO-
C(C)(=O)O
null
null
C=O.CNC.Cn1c2c(c3cc(C(N)=O)ccc31)C(=O)CCC2>C(C)(=O)O>CN(C)CC1CCc2c(c3cc(C(N)=O)ccc3n2C)C1=O
ord_dataset-01dbb772c5e249108f0b191ed17a2c0c
ord-35e63bd3939a469295f57ada34255d08
ClCc1coc(-c2ccccc2)n1.O=C1NC(=O)C(Cc2ccc(O)cc2)S1>>O=C1NC(=O)C(Cc2ccc(OCc3coc(-c4ccccc4)n3)cc2)S1
O.OC1=CC=C(CC2C(NC(S2)=O)=O)C=C1.[H-].[Na+].ClCC=1N=C(OC1)C1=CC=CC=C1>>C1(=CC=CC=C1)C=1OC=C(N1)COC1=CC=C(CC2C(NC(S2)=O)=O)C=C1
Cl[CH2:13][c:14]1[cH:15][o:16][c:17](-[c:18]2[cH:19][cH:20][cH:21][cH:22][cH:23]2)[n:24]1.[O:1]=[C:2]1[NH:3][C:4](=[O:5])[CH:6]([CH2:7][c:8]2[cH:9][cH:10][c:11]([OH:12])[cH:25][cH:26]2)[S:27]1>>[O:1]=[C:2]1[NH:3][C:4](=[O:5])[CH:6]([CH2:7][c:8]2[cH:9][cH:10][c:11]([O:12][CH2:13][c:14]3[cH:15][o:16][c:17](-[c:18]4[cH:19...
ClCc1coc(-c2ccccc2)n1.O=C1NC(=O)C(Cc2ccc(O)cc2)S1
O=C1NC(=O)C(Cc2ccc(OCc3coc(-c4ccccc4)n3)cc2)S1
null
null
CN(C=O)C
Heteroatom Alkylation and Arylation
Williamson Ether Synthesis
7e1040116e3a4cf0e8ec5cc7865388d9cd0efabce6d320a1c25a36e411018d8b
d5f4610d46ccc0478471c5bc0fb862644eaf764bbc5d93badb39d54f6ec8e0a5
O=C1NC(=O)C(Cc2ccc(OCc3coc(-c4ccccc4)n3)cc2)S1
Cl-[CH2;D2;+0:1]-[c:2]1:[#7;a:3]:[c:4]:[#8;a:5]:[c:6]:1.[OH;D1;+0:7]-[c:8](:[c:9]):[c:10]>>[c:9]:[c:8](-[O;H0;D2;+0:7]-[CH2;D2;+0:1]-[c:2]1:[#7;a:3]:[c:4]:[#8;a:5]:[c:6]:1):[c:10]
56.8
[{"value": 47.4, "product": "C1(=CC=CC=C1)C=1OC=C(N1)COC1=CC=C(CC2C(NC(S2)=O)=O)C=C1", "details": "PERCENTYIELD", "is_desired": false}, {"value": 56.8, "product": "C1(=CC=CC=C1)C=1OC=C(N1)COC1=CC=C(CC2C(NC(S2)=O)=O)C=C1", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
30
MINUTE
To a solution of 5-(4-hydroxybenzyl)-2,4-thiazolidinedione (9.4 g) in N,N-dimethylformamide (80 ml) was added 60% sodium hydride in oil (3.4 g), and the mixture was stirred for 30 minutes. Then, a solution of 4-chloromethyl-2-phenyloxazole (9.6 g) in N,N-dimethylformamide (20 ml) was added dropwise thereto at room temp...
10.6084/m9.figshare.5104873.v1
null
Primary halide.Aromatic alcohol
Ether
null
null
C1CSCN1.c1ccccc1.c1cocn1.c1ccccc1
HCl
CN(C=O)C
null
0.5
ClCc1coc(-c2ccccc2)n1.O=C1NC(=O)C(Cc2ccc(O)cc2)S1>CN(C=O)C>O=C1NC(=O)C(Cc2ccc(OCc3coc(-c4ccccc4)n3)cc2)S1
ord_dataset-01dbb772c5e249108f0b191ed17a2c0c
ord-1600130bf31e4d3497fdf571ee839211
CC1(c2nc(CCl)co2)CCCCC1.O=C1NC(=O)C(Cc2ccc(O)cc2)S1>>CC1(c2nc(COc3ccc(CC4SC(=O)NC4=O)cc3)co2)CCCCC1
O.[H-].[Na+].OC1=CC=C(CC2C(NC(S2)=O)=O)C=C1.ClCC=1N=C(OC1)C1(CCCCC1)C>>CC1(CCCCC1)C=1OC=C(N1)COC1=CC=C(CC2C(NC(S2)=O)=O)C=C1
Cl[CH2:6][c:5]1[n:4][c:3]([C:2]2([CH3:1])[CH2:24][CH2:25][CH2:26][CH2:27][CH2:28]2)[o:23][cH:22]1.[OH:7][c:8]1[cH:9][cH:10][c:11]([CH2:12][CH:13]2[S:14][C:15](=[O:16])[NH:17][C:18]2=[O:19])[cH:20][cH:21]1>>[CH3:1][C:2]1([c:3]2[n:4][c:5]([CH2:6][O:7][c:8]3[cH:9][cH:10][c:11]([CH2:12][CH:13]4[S:14][C:15](=[O:16])[NH:17][...
CC1(c2nc(CCl)co2)CCCCC1.O=C1NC(=O)C(Cc2ccc(O)cc2)S1
CC1(c2nc(COc3ccc(CC4SC(=O)NC4=O)cc3)co2)CCCCC1
null
null
CN(C=O)C
Heteroatom Alkylation and Arylation
Williamson Ether Synthesis
7e1040116e3a4cf0e8ec5cc7865388d9cd0efabce6d320a1c25a36e411018d8b
d5f4610d46ccc0478471c5bc0fb862644eaf764bbc5d93badb39d54f6ec8e0a5
O=C1NC(=O)C(Cc2ccc(OCc3coc(C4CCCCC4)n3)cc2)S1
Cl-[CH2;D2;+0:1]-[c:2]1:[#7;a:3]:[c:4]:[#8;a:5]:[c:6]:1.[OH;D1;+0:7]-[c:8](:[c:9]):[c:10]>>[c:9]:[c:8](-[O;H0;D2;+0:7]-[CH2;D2;+0:1]-[c:2]1:[#7;a:3]:[c:4]:[#8;a:5]:[c:6]:1):[c:10]
null
[]
null
null
30
MINUTE
60% sodium hydride in oil (1.32 g) was added to solution of 5-(4-hydroxybenzyl)-2,4-thiazolidinedione (3.35 g) in N,N-dimethylformamide (30 ml), and the mixture was stirred for 30 minutes. Then, solution of 4-chloromethyl-2-(1-methylcyclohexyl)oxazole (3.85 g) in N,N-dimethylformamide (5 ml) was added dropwise thereto ...
10.6084/m9.figshare.5104873.v1
null
Primary halide.Aromatic alcohol
Ether
null
null
c1cocn1.c1ccccc1.C1CSCN1.C1CCCCC1
HCl
CN(C=O)C
null
0.5
CC1(c2nc(CCl)co2)CCCCC1.O=C1NC(=O)C(Cc2ccc(O)cc2)S1>CN(C=O)C>CC1(c2nc(COc3ccc(CC4SC(=O)NC4=O)cc3)co2)CCCCC1
ord_dataset-01dbb772c5e249108f0b191ed17a2c0c
ord-8b455a0376424e3e96c5ad5aa252a94c
CCO.Cc1oc(-c2ccccc2)nc1CCOc1ccc(CC2SC(=N)NC2=O)cc1>>Cc1oc(-c2ccccc2)nc1CCOc1ccc(CC2SC(=O)NC2=O)cc1
N=C1SC(C(N1)=O)CC1=CC=C(C=C1)OCCC=1N=C(OC1C)C1=CC=CC=C1.Cl.C(C)O>>CC1=C(N=C(O1)C1=CC=CC=C1)CCOC1=CC=C(CC2C(NC(S2)=O)=O)C=C1
CC[OH:24].N=[C:23]1[S:22][CH:21]([CH2:20][c:19]2[cH:18][cH:17][c:16]([O:15][CH2:14][CH2:13][c:12]3[c:2]([CH3:1])[o:3][c:4](-[c:5]4[cH:6][cH:7][cH:8][cH:9][cH:10]4)[n:11]3)[cH:29][cH:28]2)[C:26](=[O:27])[NH:25]1>>[CH3:1][c:2]1[o:3][c:4](-[c:5]2[cH:6][cH:7][cH:8][cH:9][cH:10]2)[n:11][c:12]1[CH2:13][CH2:14][O:15][c:16]1[c...
CCO.Cc1oc(-c2ccccc2)nc1CCOc1ccc(CC2SC(=N)NC2=O)cc1
Cc1oc(-c2ccccc2)nc1CCOc1ccc(CC2SC(=O)NC2=O)cc1
null
null
null
Heteroatom Alkylation and Arylation
OtherReaction
6aaa2f59d7c8f3f887508e59aa8a49bf81aaddba8060243fd1af782ff664b4c8
29f3038d9385b8bd5021ff923a1b65cb4a19845f3f77cbeb7ca067f6e83c9c23
O=C1NC(=O)C(Cc2ccc(OCCc3coc(-c4ccccc4)n3)cc2)S1
C-C-[OH;D1;+0:1].N=[C;H0;D3;+0:2]1-[#16:3]-[C:4]-[C:5](=[O;D1;H0:6])-[#7:7]-1>>[O;D1;H0:6]=[C:5]1-[#7:7]-[C;H0;D3;+0:2](=[O;H0;D1;+0:1])-[#16:3]-[C:4]-1
95.7
[{"value": 95.7, "product": "CC1=C(N=C(O1)C1=CC=CC=C1)CCOC1=CC=C(CC2C(NC(S2)=O)=O)C=C1", "details": "PERCENTYIELD", "is_desired": false}]
null
null
null
null
A mixture of 2-imino-5-{4-[2-(5-methyl-2-phenyl-4-oxazolyl)ethoxy]benzyl}-4-thiazolidinone (18.8 g), 2N-HCl (200 ml) and ethanol (200 ml) was heated under reflux for 12 hours. The solvent was distilled off under reduced pressure. The residue was neutralized with saturated aqueous solution of sodium hydrogen carbonate, ...
10.6084/m9.figshare.5104873.v1
null
Primary alcohol.Monosulfide
Unsubstituted dicarboximide
C1CSCN1
C1CSCN1
c1cocn1.c1ccccc1.c1ccccc1.C1CSCN1
Other
null
null
null
CCO.Cc1oc(-c2ccccc2)nc1CCOc1ccc(CC2SC(=N)NC2=O)cc1>>Cc1oc(-c2ccccc2)nc1CCOc1ccc(CC2SC(=O)NC2=O)cc1
ord_dataset-01dbb772c5e249108f0b191ed17a2c0c
ord-8b6234674c5d40d897dae8a634dc35f0
Cc1oc(-c2ccccc2)nc1COc1ccc(CC2SC(=N)NC2=O)cc1.O=S(=O)(O)O>>Cc1oc(-c2ccccc2)nc1COc1ccc(CC2SC(=O)NC2=O)cc1
N=C1SC(C(N1)=O)CC1=CC=C(C=C1)OCC=1N=C(OC1C)C1=CC=CC=C1.OS(=O)(=O)O.O1CCOCC1>>CC1=C(N=C(O1)C1=CC=CC=C1)COC1=CC=C(CC2C(NC(S2)=O)=O)C=C1
N=[C:22]1[S:21][CH:20]([CH2:19][c:18]2[cH:17][cH:16][c:15]([O:14][CH2:13][c:12]3[c:2]([CH3:1])[o:3][c:4](-[c:5]4[cH:6][cH:7][cH:8][cH:9][cH:10]4)[n:11]3)[cH:28][cH:27]2)[C:25](=[O:26])[NH:24]1.O=S(=O)(O)[OH:23]>>[CH3:1][c:2]1[o:3][c:4](-[c:5]2[cH:6][cH:7][cH:8][cH:9][cH:10]2)[n:11][c:12]1[CH2:13][O:14][c:15]1[cH:16][cH...
Cc1oc(-c2ccccc2)nc1COc1ccc(CC2SC(=N)NC2=O)cc1.O=S(=O)(O)O
Cc1oc(-c2ccccc2)nc1COc1ccc(CC2SC(=O)NC2=O)cc1
null
null
O
Heteroatom Alkylation and Arylation
OtherReaction
36e8b3343c3732c812c88deadbd6fc3bb4fcd1410389683a7b04e225d2613a26
0035211ca664bab428d64ca2082d0980841c38a6de91749d7754b70d2a7510c1
O=C1NC(=O)C(Cc2ccc(OCc3coc(-c4ccccc4)n3)cc2)S1
N=[C;H0;D3;+0:1]1-[#16:2]-[C:3]-[C:4](=[O;D1;H0:5])-[#7:6]-1.O-S(=O)(=O)-[OH;D1;+0:7]>>[O;D1;H0:5]=[C:4]1-[#7:6]-[C;H0;D3;+0:1](=[O;H0;D1;+0:7])-[#16:2]-[C:3]-1
58.8
[{"value": 58.8, "product": "CC1=C(N=C(O1)C1=CC=CC=C1)COC1=CC=C(CC2C(NC(S2)=O)=O)C=C1", "details": "PERCENTYIELD", "is_desired": false}]
null
null
null
null
A mixture of 2-imino-5-[4-(5-methyl-2-phenyl-4-oxazolylmethoxy)benzyl]-4-thiazolidinone (11.4 g), 1N.H2SO4 (100 ml) and dioxane (100 ml) was stirred at 80° C. for 5 hours, and poured in water. The aqueous mixture was extracted with chloroform. The chloroform layer was washed with water, dried (MgSO4) and concentrated. ...
10.6084/m9.figshare.5104873.v1
null
Monosulfide
Unsubstituted dicarboximide
C1CSCN1
C1CSCN1
c1cocn1.c1ccccc1.c1ccccc1.C1CSCN1
HO-
O
null
null
Cc1oc(-c2ccccc2)nc1COc1ccc(CC2SC(=N)NC2=O)cc1.O=S(=O)(O)O>O>Cc1oc(-c2ccccc2)nc1COc1ccc(CC2SC(=O)NC2=O)cc1
ord_dataset-01dbb772c5e249108f0b191ed17a2c0c
ord-7107d45708c94d15882a5699664f3c58
Cc1oc(-c2ccccc2)nc1CCOc1ccc(CC2SC(=O)NC2=O)cc1.O=C1CCC(=O)N1Br>>O=C1NC(=O)C(Cc2ccc(OCCc3nc(-c4ccccc4)oc3CBr)cc2)S1
BrN1C(CCC1=O)=O.CC1=C(N=C(O1)C1=CC=CC=C1)CCOC1=CC=C(CC2C(NC(S2)=O)=O)C=C1.N(=NC(C#N)(C)C)C(C#N)(C)C>>BrCC1=C(N=C(O1)C1=CC=CC=C1)CCOC1=CC=C(CC2C(NC(S2)=O)=O)C=C1
[O:1]=[C:2]1[NH:3][C:4](=[O:5])[CH:6]([CH2:7][c:8]2[cH:9][cH:10][c:11]([O:12][CH2:13][CH2:14][c:15]3[n:16][c:17](-[c:18]4[cH:19][cH:20][cH:21][cH:22][cH:23]4)[o:24][c:25]3[CH3:26])[cH:28][cH:29]2)[S:30]1.O=C1CCC(=O)N1[Br:27]>>[O:1]=[C:2]1[NH:3][C:4](=[O:5])[CH:6]([CH2:7][c:8]2[cH:9][cH:10][c:11]([O:12][CH2:13][CH2:14][...
Cc1oc(-c2ccccc2)nc1CCOc1ccc(CC2SC(=O)NC2=O)cc1.O=C1CCC(=O)N1Br
O=C1NC(=O)C(Cc2ccc(OCCc3nc(-c4ccccc4)oc3CBr)cc2)S1
null
null
C(Cl)(Cl)(Cl)Cl
Functional Group Interconversion
Wohl-Ziegler bromination benzyl primary
45c0aca0d63a96f0092e6dded9c888827eaf6379dac179e1cefc99293896300a
08f5e7e34d3f321cce3e85421b38226d6240cca0939494ae61032d4f8405cf22
O=C1NC(=O)C(Cc2ccc(OCCc3coc(-c4ccccc4)n3)cc2)S1
O=C1-C-C-C(=O)-N-1-[Br;H0;D1;+0:1].[C:2]-[c:3]1:[#7;a:4]:[c:5]:[#8;a:6]:[c:7]:1-[CH3;D1;+0:8]>>[Br;H0;D1;+0:1]-[CH2;D2;+0:8]-[c:7]1:[#8;a:6]:[c:5]:[#7;a:4]:[c:3]:1-[C:2]
null
[]
null
null
null
null
N-Bromosuccinimide (2.75 g) was added portionwise to a solution of 5-{4-[2-(5-methyl-2-phenyl-4-oxazolyl)ethoxy]benzyl}-2,4-thiazolidinedione (6.0 g) and α,α'-azobisisobutyronitrile (0.5 g) in carbon tetrachloride(150 ml) under reflux. After refluxing for another 10 minutes, the reaction mixture was washed with water a...
10.6084/m9.figshare.5104873.v1
null
Tertiary amide.Tertiary amide
Primary halide
C1CCNC1
null
C1CSCN1.c1ccccc1.c1cocn1.c1ccccc1
HO-
C(Cl)(Cl)(Cl)Cl
null
null
Cc1oc(-c2ccccc2)nc1CCOc1ccc(CC2SC(=O)NC2=O)cc1.O=C1CCC(=O)N1Br>C(Cl)(Cl)(Cl)Cl>O=C1NC(=O)C(Cc2ccc(OCCc3nc(-c4ccccc4)oc3CBr)cc2)S1
ord_dataset-01dbb772c5e249108f0b191ed17a2c0c
ord-d519b00c7e994e338826daf4aa407bae
Cc1nc(C(O)COc2ccc(CC3SC(=O)NC3=O)cc2)c(C)o1>>Cc1nc(C(=O)COc2ccc(CC3SC(=O)NC3=O)cc2)c(C)o1
C(C)(=O)OC(C)=O.CC=1OC(=C(N1)C(COC1=CC=C(CC2C(NC(S2)=O)=O)C=C1)O)C.O>>CC=1OC(=C(N1)C(COC1=CC=C(CC2C(NC(S2)=O)=O)C=C1)=O)C
[CH3:1][c:2]1[n:3][c:4]([CH:5]([OH:6])[CH2:7][O:8][c:9]2[cH:10][cH:11][c:12]([CH2:13][CH:14]3[S:15][C:16](=[O:17])[NH:18][C:19]3=[O:20])[cH:21][cH:22]2)[c:23]([CH3:24])[o:25]1>>[CH3:1][c:2]1[n:3][c:4]([C:5](=[O:6])[CH2:7][O:8][c:9]2[cH:10][cH:11][c:12]([CH2:13][CH:14]3[S:15][C:16](=[O:17])[NH:18][C:19]3=[O:20])[cH:21][...
Cc1nc(C(O)COc2ccc(CC3SC(=O)NC3=O)cc2)c(C)o1
Cc1nc(C(=O)COc2ccc(CC3SC(=O)NC3=O)cc2)c(C)o1
null
null
CS(=O)C
Oxidation
Oxidation or Dehydrogenation of Alcohols to Aldehydes and Ketones
c7c20d2959ac48847b03cc1265962cf99a8ec8a85900c087dabb30077298c66c
767cfd93f5821ebb9e1e72addd9cb404b20b0c821d246ae6b87a5776b74a455b
O=C1NC(=O)C(Cc2ccc(OCC(=O)c3cocn3)cc2)S1
[#8:1]-[C:2]-[CH;D3;+0:3](-[OH;D1;+0:4])-[c:5]1:[#7;a:6]:[c:7]:[#8;a:8]:[c:9]:1-[C;D1;H3:10]>>[#8:1]-[C:2]-[C;H0;D3;+0:3](=[O;H0;D1;+0:4])-[c:5]1:[#7;a:6]:[c:7]:[#8;a:8]:[c:9]:1-[C;D1;H3:10]
48.3
[{"value": 48.3, "product": "CC=1OC(=C(N1)C(COC1=CC=C(CC2C(NC(S2)=O)=O)C=C1)=O)C", "details": "PERCENTYIELD", "is_desired": false}, {"value": 48.3, "product": "CC=1OC(=C(N1)C(COC1=CC=C(CC2C(NC(S2)=O)=O)C=C1)=O)C", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
8
HOUR
Acetic anhydride (1.0 ml) was added to a solution of 5-{4-[2-(2,5-dimethyl-4-oxazolyl)-2-hydroxyethoxy]benzyl}-2,4-thiazolidinedione (0.5 g) in dimethylsulfoxide (10 ml), and the mixture was allowed to stand overnight and poured into water. The mixture was extracted with ethyl acetate. The ethyl acetate layer was washe...
10.6084/m9.figshare.5104873.v1
null
Secondary alcohol
Ketone
null
null
c1cocn1.c1ccccc1.C1CSCN1
null
CS(=O)C
null
8
Cc1nc(C(O)COc2ccc(CC3SC(=O)NC3=O)cc2)c(C)o1>CS(=O)C>Cc1nc(C(=O)COc2ccc(CC3SC(=O)NC3=O)cc2)c(C)o1
ord_dataset-01dbb772c5e249108f0b191ed17a2c0c
ord-512f61929c254761a4426dca28886965
Cc1oc(-c2ccccc2)nc1CCOc1ccc(C=O)cc1.O=C1CSC(=O)N1>>Cc1oc(-c2ccccc2)nc1CCOc1ccc(C=C2SC(=O)NC2=O)cc1
CC1=C(N=C(O1)C1=CC=CC=C1)CCOC1=CC=C(C=O)C=C1.S1C(NC(C1)=O)=O.N1CCCCC1>>CC1=C(N=C(O1)C1=CC=CC=C1)CCOC1=CC=C(C=C2C(NC(S2)=O)=O)C=C1
O=[CH:20][c:19]1[cH:18][cH:17][c:16]([O:15][CH2:14][CH2:13][c:12]2[c:2]([CH3:1])[o:3][c:4](-[c:5]3[cH:6][cH:7][cH:8][cH:9][cH:10]3)[n:11]2)[cH:29][cH:28]1.[CH2:21]1[S:22][C:23](=[O:24])[NH:25][C:26]1=[O:27]>>[CH3:1][c:2]1[o:3][c:4](-[c:5]2[cH:6][cH:7][cH:8][cH:9][cH:10]2)[n:11][c:12]1[CH2:13][CH2:14][O:15][c:16]1[cH:17...
Cc1oc(-c2ccccc2)nc1CCOc1ccc(C=O)cc1.O=C1CSC(=O)N1
Cc1oc(-c2ccccc2)nc1CCOc1ccc(C=C2SC(=O)NC2=O)cc1
null
null
C(C)O
C-C Coupling
Aldol condensation
9a823fd9b4e4348a3556e295dbe35eee5775ba89af420a0e94956549a8f5e1f0
d1104e4dc387c28c5ac408eab23aa043e968d3cfd16e99022454bf87ce31f401
O=C1NC(=O)C(=Cc2ccc(OCCc3coc(-c4ccccc4)n3)cc2)S1
O=[CH;D2;+0:1]-[c:2](:[c:3]):[c:4].[O;D1;H0:5]=[C:6]1-[#16:7]-[CH2;D2;+0:8]-[C:9](=[O;D1;H0:10])-[#7:11]-1>>[O;D1;H0:5]=[C:6]1-[#16:7]-[C;H0;D3;+0:8](=[CH;D2;+0:1]-[c:2](:[c:3]):[c:4])-[C:9](=[O;D1;H0:10])-[#7:11]-1
77.1
[{"value": 76.8, "product": "CC1=C(N=C(O1)C1=CC=CC=C1)CCOC1=CC=C(C=C2C(NC(S2)=O)=O)C=C1", "details": "PERCENTYIELD", "is_desired": false}, {"value": 77.1, "product": "CC1=C(N=C(O1)C1=CC=CC=C1)CCOC1=CC=C(C=C2C(NC(S2)=O)=O)C=C1", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
null
null
A mixture of 4-[2-(5-methyl-2-phenyl-4-oxazolyl)ethoxy]benzaldehyde (5.0 g), 2,4-thiazolidinedione (3.8 g), piperidine (0.32 ml) and ethanol (100 ml) was stirred under reflux for 5 hours. After cooling, the crystals which separated out were collected by filtration to give 5-{4-[2-(5-methyl-2-phenyl-4-oxazolyl)ethoxy]be...
10.6084/m9.figshare.5104873.v1
null
Aldehyde.Monosulfide
Monosulfide
C1CSCN1
C1CSCN1
c1cocn1.c1ccccc1.c1ccccc1.C1CSCN1
HO-
C(C)O
null
null
Cc1oc(-c2ccccc2)nc1CCOc1ccc(C=O)cc1.O=C1CSC(=O)N1>C(C)O>Cc1oc(-c2ccccc2)nc1CCOc1ccc(C=C2SC(=O)NC2=O)cc1
ord_dataset-01dbb772c5e249108f0b191ed17a2c0c
ord-59eb3a84c5114e449b61d0353ae198d1
Cc1oc(-c2ccccc2)nc1CCl.O=C1NC(=O)C(=Cc2ccc(O)cc2)S1>>Cc1oc(-c2ccccc2)nc1COc1ccc(C=C2SC(=O)NC2=O)cc1
O.[H-].[Na+].OC1=CC=C(C=C2C(NC(S2)=O)=O)C=C1.ClCC=1N=C(OC1C)C1=CC=CC=C1>>CC1=C(N=C(O1)C1=CC=CC=C1)COC1=CC=C(C=C2C(NC(S2)=O)=O)C=C1
Cl[CH2:13][c:12]1[c:2]([CH3:1])[o:3][c:4](-[c:5]2[cH:6][cH:7][cH:8][cH:9][cH:10]2)[n:11]1.[OH:14][c:15]1[cH:16][cH:17][c:18]([CH:19]=[C:20]2[S:21][C:22](=[O:23])[NH:24][C:25]2=[O:26])[cH:27][cH:28]1>>[CH3:1][c:2]1[o:3][c:4](-[c:5]2[cH:6][cH:7][cH:8][cH:9][cH:10]2)[n:11][c:12]1[CH2:13][O:14][c:15]1[cH:16][cH:17][c:18]([...
Cc1oc(-c2ccccc2)nc1CCl.O=C1NC(=O)C(=Cc2ccc(O)cc2)S1
Cc1oc(-c2ccccc2)nc1COc1ccc(C=C2SC(=O)NC2=O)cc1
null
null
CN(C=O)C.C(C)(=O)O
Heteroatom Alkylation and Arylation
Williamson Ether Synthesis
7e1040116e3a4cf0e8ec5cc7865388d9cd0efabce6d320a1c25a36e411018d8b
d5f4610d46ccc0478471c5bc0fb862644eaf764bbc5d93badb39d54f6ec8e0a5
O=C1NC(=O)C(=Cc2ccc(OCc3coc(-c4ccccc4)n3)cc2)S1
Cl-[CH2;D2;+0:1]-[c:2]1:[#7;a:3]:[c:4]:[#8;a:5]:[c:6]:1-[C;D1;H3:7].[OH;D1;+0:8]-[c:9](:[c:10]):[c:11]>>[C;D1;H3:7]-[c:6]1:[#8;a:5]:[c:4]:[#7;a:3]:[c:2]:1-[CH2;D2;+0:1]-[O;H0;D2;+0:8]-[c:9](:[c:10]):[c:11]
41.6
[{"value": 40.8, "product": "CC1=C(N=C(O1)C1=CC=CC=C1)COC1=CC=C(C=C2C(NC(S2)=O)=O)C=C1", "details": "PERCENTYIELD", "is_desired": false}, {"value": 41.6, "product": "CC1=C(N=C(O1)C1=CC=CC=C1)COC1=CC=C(C=C2C(NC(S2)=O)=O)C=C1", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
30
MINUTE
60% sodium hydride in oil (0.24 g) was added to a solution of 5-(4-hydroxybenzylidene)-2,4-thiazolidinedione (0.664 g) in N,N-dimethylformamide (20 ml), and the mixture was stirred for 30 minutes. A solution of 4-chloromethyl-5-methyl-2-phenyloxazole (0.623 g) in N,N-dimethylformamide (10 ml) was added dropwise to the ...
10.6084/m9.figshare.5104873.v1
null
Primary halide.Aromatic alcohol
Ether
null
null
c1cocn1.c1ccccc1.c1ccccc1.C1CSCN1
HCl
CN(C=O)C.C(C)(=O)O
null
0.5
Cc1oc(-c2ccccc2)nc1CCl.O=C1NC(=O)C(=Cc2ccc(O)cc2)S1>CN(C=O)C.C(C)(=O)O>Cc1oc(-c2ccccc2)nc1COc1ccc(C=C2SC(=O)NC2=O)cc1
ord_dataset-01dbb772c5e249108f0b191ed17a2c0c
ord-b11cbb3989ca4572a78c632b845a4b6a
Cc1oc(-c2ccccc2)nc1C(=O)CBr.O=C1NC(=O)C(=Cc2ccc(O)cc2)S1>>Cc1oc(-c2ccccc2)nc1C(=O)COc1ccc(C=C2SC(=O)NC2=O)cc1
C(C)(=O)O.[H-].[Na+].OC1=CC=C(C=C2C(NC(S2)=O)=O)C=C1.BrCC(=O)C=1N=C(OC1C)C1=CC=CC=C1>>CC1=C(N=C(O1)C1=CC=CC=C1)C(COC1=CC=C(C=C2C(NC(S2)=O)=O)C=C1)=O
Br[CH2:15][C:13]([c:12]1[c:2]([CH3:1])[o:3][c:4](-[c:5]2[cH:6][cH:7][cH:8][cH:9][cH:10]2)[n:11]1)=[O:14].[OH:16][c:17]1[cH:18][cH:19][c:20]([CH:21]=[C:22]2[S:23][C:24](=[O:25])[NH:26][C:27]2=[O:28])[cH:29][cH:30]1>>[CH3:1][c:2]1[o:3][c:4](-[c:5]2[cH:6][cH:7][cH:8][cH:9][cH:10]2)[n:11][c:12]1[C:13](=[O:14])[CH2:15][O:16...
Cc1oc(-c2ccccc2)nc1C(=O)CBr.O=C1NC(=O)C(=Cc2ccc(O)cc2)S1
Cc1oc(-c2ccccc2)nc1C(=O)COc1ccc(C=C2SC(=O)NC2=O)cc1
null
null
CN(C=O)C
Heteroatom Alkylation and Arylation
Williamson Ether Synthesis
8060b8e1565497a5ddf79be1adfe74f552b31798797b8841753247b06bdd2051
8749b179916f131d393264a24309227dc6177f560726bed2d1f4567dc2ac63f5
O=C1NC(=O)C(=Cc2ccc(OCC(=O)c3coc(-c4ccccc4)n3)cc2)S1
Br-[CH2;D2;+0:1]-[C:2](=[O;D1;H0:3])-[c:4](:[#7;a:5]):[c:6]:[#8;a:7].[OH;D1;+0:8]-[c:9](:[c:10]):[c:11]>>[#7;a:5]:[c:4](-[C:2](=[O;D1;H0:3])-[CH2;D2;+0:1]-[O;H0;D2;+0:8]-[c:9](:[c:10]):[c:11]):[c:6]:[#8;a:7]
33.3
[{"value": 32.3, "product": "CC1=C(N=C(O1)C1=CC=CC=C1)C(COC1=CC=C(C=C2C(NC(S2)=O)=O)C=C1)=O", "details": "PERCENTYIELD", "is_desired": false}, {"value": 33.3, "product": "CC1=C(N=C(O1)C1=CC=CC=C1)C(COC1=CC=C(C=C2C(NC(S2)=O)=O)C=C1)=O", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
30
MINUTE
60% sodium hydride in oil (0.24 g) was added to a solution of 5-(4-hydroxybenzylidene)-2,4-thiazolidinedione (0.663 g) in N,N-dimethylformamide (20 ml) and the mixture was stirred for 30 minutes. Then, a solution of 4-bromoacetyl-5-methyl-2-phenyloxazole (0.841 g) in N,N-dimethylformamide (10 ml) was added dropwise to ...
10.6084/m9.figshare.5104873.v1
null
Primary halide.Ketone.Aromatic alcohol
Ketone.Ether
null
null
c1cocn1.c1ccccc1.c1ccccc1.C1CSCN1
HBr
CN(C=O)C
null
0.5
Cc1oc(-c2ccccc2)nc1C(=O)CBr.O=C1NC(=O)C(=Cc2ccc(O)cc2)S1>CN(C=O)C>Cc1oc(-c2ccccc2)nc1C(=O)COc1ccc(C=C2SC(=O)NC2=O)cc1
ord_dataset-01dbb772c5e249108f0b191ed17a2c0c
ord-7c9f173d9c7d4c9db041ee6af88f9112
Cc1nc(C(=O)COc2ccc(C=C3SC(=O)NC3=O)cc2)c(C)o1>>Cc1nc(C(O)COc2ccc(CC3SC(=O)NC3=O)cc2)c(C)o1
C(C)(=O)O.[BH4-].[Na+].CC=1OC(=C(N1)C(COC1=CC=C(C=C2C(NC(S2)=O)=O)C=C1)=O)C>>CC=1OC(=C(N1)C(COC1=CC=C(CC2C(NC(S2)=O)=O)C=C1)O)C
[CH3:1][c:2]1[n:3][c:4]([C:5](=[O:6])[CH2:7][O:8][c:9]2[cH:10][cH:11][c:12]([CH:13]=[C:14]3[S:15][C:16](=[O:17])[NH:18][C:19]3=[O:20])[cH:21][cH:22]2)[c:23]([CH3:24])[o:25]1>>[CH3:1][c:2]1[n:3][c:4]([CH:5]([OH:6])[CH2:7][O:8][c:9]2[cH:10][cH:11][c:12]([CH2:13][CH:14]3[S:15][C:16](=[O:17])[NH:18][C:19]3=[O:20])[cH:21][c...
Cc1nc(C(=O)COc2ccc(C=C3SC(=O)NC3=O)cc2)c(C)o1
Cc1nc(C(O)COc2ccc(CC3SC(=O)NC3=O)cc2)c(C)o1
null
null
CO.CN(C=O)C
Reduction
OtherReaction
26b547225191774776c3b4b00c692cb60cf527f116fdf2c33e3fbd48d27dd217
ca6bd49afbaeacd83eda3753e609edfcce9407a02a26bc62950bcb3b22cda1d2
O=C1NC(=O)C(Cc2ccc(OCCc3cocn3)cc2)S1
[#8:1]-[C:2]-[C;H0;D3;+0:3](=[O;H0;D1;+0:4])-[c:5]1:[#7;a:6]:[c:7]:[#8;a:8]:[c:9]:1-[C;D1;H3:10].[O;D1;H0:11]=[C:12]1-[#16:13]-[C;H0;D3;+0:14](=[CH;D2;+0:15]-[c:16](:[c:17]):[c:18])-[C:19](=[O;D1;H0:20])-[#7:21]-1>>[#8:1]-[C:2]-[CH;D3;+0:3](-[OH;D1;+0:4])-[c:5]1:[#7;a:6]:[c:7]:[#8;a:8]:[c:9]:1-[C;D1;H3:10].[O;D1;H0:11]...
97.5
[{"value": 97.5, "product": "CC=1OC(=C(N1)C(COC1=CC=C(CC2C(NC(S2)=O)=O)C=C1)O)C", "details": "PERCENTYIELD", "is_desired": false}, {"value": 96.9, "product": "CC=1OC(=C(N1)C(COC1=CC=C(CC2C(NC(S2)=O)=O)C=C1)O)C", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
null
null
Sodium borohydride (0.16 g) was added to a suspension of 5-{4-[2-(2,5-dimethyl-oxazolyl)-2-oxoethoxy]benzylidene}-2,4-thiazolidinedione (1.5 g) in methanol-N,N-dimethylformamide (1:1, V.V, 40 ml) under ice-cooling. After stirring under ice-cooling for 20 minutes, the reaction solution was poured into ice-water, and the...
10.6084/m9.figshare.5104873.v1
null
Ketone.Monosulfide
Secondary alcohol.Monosulfide
C1CSCN1
C1CSCN1
c1cocn1.c1ccccc1.C1CSCN1
null
CO.CN(C=O)C
null
null
Cc1nc(C(=O)COc2ccc(C=C3SC(=O)NC3=O)cc2)c(C)o1>CO.CN(C=O)C>Cc1nc(C(O)COc2ccc(CC3SC(=O)NC3=O)cc2)c(C)o1
ord_dataset-01dbb772c5e249108f0b191ed17a2c0c
ord-f96237b352604b159d8094b573f7f1e4
Cc1oc(-c2ccccc2)nc1CCOc1ccc(C=C2SC(=O)NC2=O)cc1>>Cc1oc(-c2ccccc2)nc1CCOc1ccc(CC2SC(=O)NC2=O)cc1
CO.CC1=C(N=C(O1)C1=CC=CC=C1)CCOC1=CC=C(C=C2C(NC(S2)=O)=O)C=C1.C(C)(=O)O>>CC1=C(N=C(O1)C1=CC=CC=C1)CCOC1=CC=C(CC2C(NC(S2)=O)=O)C=C1
[CH3:1][c:2]1[o:3][c:4](-[c:5]2[cH:6][cH:7][cH:8][cH:9][cH:10]2)[n:11][c:12]1[CH2:13][CH2:14][O:15][c:16]1[cH:17][cH:18][c:19]([CH:20]=[C:21]2[S:22][C:23](=[O:24])[NH:25][C:26]2=[O:27])[cH:28][cH:29]1>>[CH3:1][c:2]1[o:3][c:4](-[c:5]2[cH:6][cH:7][cH:8][cH:9][cH:10]2)[n:11][c:12]1[CH2:13][CH2:14][O:15][c:16]1[cH:17][cH:1...
Cc1oc(-c2ccccc2)nc1CCOc1ccc(C=C2SC(=O)NC2=O)cc1
Cc1oc(-c2ccccc2)nc1CCOc1ccc(CC2SC(=O)NC2=O)cc1
null
[Pd]
C(Cl)(Cl)Cl
Reduction
Hydrogenation (double to single)
5287357a9ceae46aa07f85d3bac2070fe5bb40eaa8eb1baec18cbe42a25e8909
229264280d760663074461f898bce2a68d1dd7a993ad956085f2c6522e0edd11
O=C1NC(=O)C(Cc2ccc(OCCc3coc(-c4ccccc4)n3)cc2)S1
[O;D1;H0:1]=[C:2]1-[#16:3]-[C;H0;D3;+0:4](=[CH;D2;+0:5]-[c:6](:[c:7]):[c:8])-[C:9](=[O;D1;H0:10])-[#7:11]-1>>[O;D1;H0:1]=[C:2]1-[#16:3]-[CH;D3;+0:4](-[CH2;D2;+0:5]-[c:6](:[c:7]):[c:8])-[C:9](=[O;D1;H0:10])-[#7:11]-1
null
[]
60
CELSIUS
3
HOUR
A stirred mixture of 5-{4-[2-(5-methyl-2-phenyl-4-oxazolyl)ethoxy]benzylidene}-2,4-thiazolidinedione (500 mg), 10% Pd-C (50% wet, 1.0 g) and acetic acid (50 ml) was hydrogenated at 70° C. and at atmospheric pressure for 3 hours. Methanol (20 ml) and chloroform (20 ml) were added to the mixture and the whole was heated ...
10.6084/m9.figshare.5104873.v1
null
Monosulfide
Monosulfide
C1CSCN1
C1CSCN1
c1cocn1.c1ccccc1.c1ccccc1.C1CSCN1
null
[Pd].C(Cl)(Cl)Cl
60
3
Cc1oc(-c2ccccc2)nc1CCOc1ccc(C=C2SC(=O)NC2=O)cc1>[Pd].C(Cl)(Cl)Cl>Cc1oc(-c2ccccc2)nc1CCOc1ccc(CC2SC(=O)NC2=O)cc1
ord_dataset-01dbb772c5e249108f0b191ed17a2c0c
ord-c8eb97027f2c4870835f040d585e95f1
Cc1oc(-c2ccccc2)nc1C(=O)COc1ccc(C=C2SC(=O)NC2=O)cc1>>Cc1oc(-c2ccccc2)nc1C(=O)COc1ccc(CC2SC(=O)NC2=O)cc1
CC1=C(N=C(O1)C1=CC=CC=C1)C(COC1=CC=C(C=C2C(NC(S2)=O)=O)C=C1)=O>>CC1=C(N=C(O1)C1=CC=CC=C1)C(COC1=CC=C(CC2C(NC(S2)=O)=O)C=C1)=O
[CH3:1][c:2]1[o:3][c:4](-[c:5]2[cH:6][cH:7][cH:8][cH:9][cH:10]2)[n:11][c:12]1[C:13](=[O:14])[CH2:15][O:16][c:17]1[cH:18][cH:19][c:20]([CH:21]=[C:22]2[S:23][C:24](=[O:25])[NH:26][C:27]2=[O:28])[cH:29][cH:30]1>>[CH3:1][c:2]1[o:3][c:4](-[c:5]2[cH:6][cH:7][cH:8][cH:9][cH:10]2)[n:11][c:12]1[C:13](=[O:14])[CH2:15][O:16][c:17...
Cc1oc(-c2ccccc2)nc1C(=O)COc1ccc(C=C2SC(=O)NC2=O)cc1
Cc1oc(-c2ccccc2)nc1C(=O)COc1ccc(CC2SC(=O)NC2=O)cc1
null
[Pd].[Pd]
O1CCOCC1
Reduction
Hydrogenation (double to single)
5287357a9ceae46aa07f85d3bac2070fe5bb40eaa8eb1baec18cbe42a25e8909
229264280d760663074461f898bce2a68d1dd7a993ad956085f2c6522e0edd11
O=C1NC(=O)C(Cc2ccc(OCC(=O)c3coc(-c4ccccc4)n3)cc2)S1
[O;D1;H0:1]=[C:2]1-[#16:3]-[C;H0;D3;+0:4](=[CH;D2;+0:5]-[c:6](:[c:7]):[c:8])-[C:9](=[O;D1;H0:10])-[#7:11]-1>>[O;D1;H0:1]=[C:2]1-[#16:3]-[CH;D3;+0:4](-[CH2;D2;+0:5]-[c:6](:[c:7]):[c:8])-[C:9](=[O;D1;H0:10])-[#7:11]-1
null
[]
null
null
4
HOUR
A stirred mixture of 5-{4-[2-(5-methyl-2-phenyl-4-oxazolyl)-2-oxoethoxy]benzylidene}-2,4-thiazolidinedione (1.0 g), Pd-black (3 g) and dioxane (100 ml) was hydrogenated at 40° C. and at atmospheric pressure. After 4 hours, another Pd-black (3 g) was added and hydrogenation was continued for 4 hours. The catalyst was fi...
10.6084/m9.figshare.5104873.v1
null
Monosulfide
Monosulfide
C1CSCN1
C1CSCN1
c1cocn1.c1ccccc1.c1ccccc1.C1CSCN1
null
[Pd].[Pd].O1CCOCC1
null
4
Cc1oc(-c2ccccc2)nc1C(=O)COc1ccc(C=C2SC(=O)NC2=O)cc1>[Pd].[Pd].O1CCOCC1>Cc1oc(-c2ccccc2)nc1C(=O)COc1ccc(CC2SC(=O)NC2=O)cc1
ord_dataset-01dbb772c5e249108f0b191ed17a2c0c
ord-7d658abe348645fab4f8f7ddde1e6c72
CCCC(N)=O.O=C(CCl)CCl>>CCCc1nc(CCl)co1
C(CCC)(=O)N.ClCC(=O)CCl.C([O-])(O)=O.[Na+]>>ClCC=1N=C(OC1)CCC
[CH3:1][CH2:2][CH2:3][C:4]([NH2:5])=[O:10].O=[C:6]([CH2:7][Cl:8])[CH2:9]Cl>>[CH3:1][CH2:2][CH2:3][c:4]1[n:5][c:6]([CH2:7][Cl:8])[cH:9][o:10]1
CCCC(N)=O.O=C(CCl)CCl
CCCc1nc(CCl)co1
null
null
O
Aromatic Heterocycle Formation
OtherReaction
ab1ba96e48a7051990ce9c668ad0397fa94fe4b34eede3db2207f921e4585efd
5a724a9223d53cbf2bb1ed354a2db350dd6d10aa40058c7a1ca373081e191f17
c1cocn1
Cl-[CH2;D2;+0:1]-[C;H0;D3;+0:2](=O)-[C:3]-[Cl;D1;H0:4].[C:5]-[C:6]-[C;H0;D3;+0:7](-[NH2;D1;+0:8])=[O;H0;D1;+0:9]>>[C:5]-[C:6]-[c;H0;D3;+0:7]1:[n;H0;D2;+0:8]:[c;H0;D3;+0:2](-[C:3]-[Cl;D1;H0:4]):[cH;D2;+0:1]:[o;H0;D2;+0:9]:1
null
[]
130
CELSIUS
null
null
A mixture of butyramide (19.88 g) and 1.3-dichloroacetone (24.14 g) was heated at 130° C. for 1.5 hours. After cooling, the mixture was diluted with water, neutralized with aqueous sodium bicarbonate solution and extracted with ethyl ether. The extract was washed with water, dried (MgSO4) and concentrated. The residue ...
10.6084/m9.figshare.5104873.v1
null
Primary halide.Ketone.Primary amide
null
null
c1cocn1
c1cocn1
HCl
O
130
null
CCCC(N)=O.O=C(CCl)CCl>O>CCCc1nc(CCl)co1
ord_dataset-01dbb772c5e249108f0b191ed17a2c0c
ord-e63f4e4c221e4ca7857dee83451d2403
CCOC(=O)CC(=O)CCl.NC(=O)c1ccccc1>>CCOC(=O)Cc1coc(-c2ccccc2)n1
C(C1=CC=CC=C1)(=O)N.ClCC(CC(=O)OCC)=O.C([O-])(O)=O.[Na+]>>C1(=CC=CC=C1)C=1OC=C(N1)CC(=O)OCC
O=[C:7]([CH2:6][C:4]([O:3][CH2:2][CH3:1])=[O:5])[CH2:8]Cl.[O:9]=[C:10]([c:11]1[cH:12][cH:13][cH:14][cH:15][cH:16]1)[NH2:17]>>[CH3:1][CH2:2][O:3][C:4](=[O:5])[CH2:6][c:7]1[cH:8][o:9][c:10](-[c:11]2[cH:12][cH:13][cH:14][cH:15][cH:16]2)[n:17]1
CCOC(=O)CC(=O)CCl.NC(=O)c1ccccc1
CCOC(=O)Cc1coc(-c2ccccc2)n1
null
null
null
Aromatic Heterocycle Formation
OtherReaction
ab1ba96e48a7051990ce9c668ad0397fa94fe4b34eede3db2207f921e4585efd
5a724a9223d53cbf2bb1ed354a2db350dd6d10aa40058c7a1ca373081e191f17
c1ccc(-c2ncco2)cc1
Cl-[CH2;D2;+0:1]-[C;H0;D3;+0:2](=O)-[C:3]-[C:4](=[O;D1;H0:5])-[#8:6]-[C:7].[NH2;D1;+0:8]-[C;H0;D3;+0:9](=[O;H0;D1;+0:10])-[c;H0;D3;+0:11](:[c:12]:[c:13]):[c:14]:[c:15]>>[C:7]-[#8:6]-[C:4](=[O;D1;H0:5])-[C:3]-[c;H0;D3;+0:2]1:[cH;D2;+0:1]:[o;H0;D2;+0:10]:[c;H0;D3;+0:9](-[c;H0;D3;+0:11](:[c:12]:[c:13]):[c:14]:[c:15]):[n;H...
38
[{"value": 28.0, "product": "C1(=CC=CC=C1)C=1OC=C(N1)CC(=O)OCC", "details": "PERCENTYIELD", "is_desired": false}, {"value": 38.0, "product": "C1(=CC=CC=C1)C=1OC=C(N1)CC(=O)OCC", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
120
CELSIUS
null
null
A mixture of benzamide (60.0 g) and ethyl 4-chloroacetoacetate (49.4 g) was heated at 120° C. for 2 hours. After cooling, aqueous sodium bicarbonate solution was added thereto and the mixture was extracted with ethyl acetate. The extract was washed with water, dried (MgSO4) and concentrated. The residue was purified by...
10.6084/m9.figshare.5104873.v1
null
Primary halide.Ketone.Primary amide
null
null
c1cocn1
c1cocn1.c1ccccc1
HCl
null
120
null
CCOC(=O)CC(=O)CCl.NC(=O)c1ccccc1>>CCOC(=O)Cc1coc(-c2ccccc2)n1
ord_dataset-01dbb772c5e249108f0b191ed17a2c0c
ord-d744f03ba5db41d1bd7902f811b93a8d
CCOC(=O)CC(=O)CCl.NC(=S)C1CCCCC1>>CCOC(=O)Cc1csc(C2CCCCC2)n1
C1(CCCCC1)C(N)=S.ClCC(CC(=O)OCC)=O>>C1(CCCCC1)C=1SC=C(N1)CC(=O)OCC
O=[C:7]([CH2:6][C:4]([O:3][CH2:2][CH3:1])=[O:5])[CH2:8]Cl.[S:9]=[C:10]([CH:11]1[CH2:12][CH2:13][CH2:14][CH2:15][CH2:16]1)[NH2:17]>>[CH3:1][CH2:2][O:3][C:4](=[O:5])[CH2:6][c:7]1[cH:8][s:9][c:10]([CH:11]2[CH2:12][CH2:13][CH2:14][CH2:15][CH2:16]2)[n:17]1
CCOC(=O)CC(=O)CCl.NC(=S)C1CCCCC1
CCOC(=O)Cc1csc(C2CCCCC2)n1
null
null
C(C)O
Aromatic Heterocycle Formation
OtherReaction
21eb8c7cda3c7fc14309a0c556334226f1a9147c334386d33bc70341830a82ec
9f145257a80f08f1a7a6ee36c84cd4115965bd63128f36de61c7ed688ad2603c
c1csc(C2CCCCC2)n1
Cl-[CH2;D2;+0:1]-[C;H0;D3;+0:2](=O)-[C:3]-[C:4](=[O;D1;H0:5])-[#8:6]-[C:7].[C:8]-[C:9](-[C;H0;D3;+0:10](-[NH2;D1;+0:11])=[S;H0;D1;+0:12])-[C:13]>>[C:8]-[C:9](-[c;H0;D3;+0:10]1:[n;H0;D2;+0:11]:[c;H0;D3;+0:2](-[C:3]-[C:4](=[O;D1;H0:5])-[#8:6]-[C:7]):[cH;D2;+0:1]:[s;H0;D2;+0:12]:1)-[C:13]
71.3
[{"value": 70.9, "product": "C1(CCCCC1)C=1SC=C(N1)CC(=O)OCC", "details": "PERCENTYIELD", "is_desired": false}, {"value": 71.3, "product": "C1(CCCCC1)C=1SC=C(N1)CC(=O)OCC", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
null
null
A mixture of cyclohexanethiocarboxamide (5.0 g), ethyl 4-chloroacetoacetate (5.74 g), ethanol (50 ml) was heated under reflux for 1 hour. After dilution with water, mixture was extracted with ethyl acetate. The extract was washed with aqueous sodium bicarbonate solution and water, dried (MgSO4), and concentrated. The r...
10.6084/m9.figshare.5104873.v1
null
Primary halide.Ketone.Thioamide
null
null
c1cscn1
c1cscn1.C1CCCCC1
HCl
C(C)O
null
null
CCOC(=O)CC(=O)CCl.NC(=S)C1CCCCC1>C(C)O>CCOC(=O)Cc1csc(C2CCCCC2)n1
ord_dataset-01dbb772c5e249108f0b191ed17a2c0c
ord-55ea6960f61b4354bc71a258ea910ffe
COC(=O)Cc1nc(-c2ccccc2)oc1C>>Cc1oc(-c2ccccc2)nc1CCO
O.CC1=C(N=C(O1)C1=CC=CC=C1)CC(=O)OC.[H-].[Al+3].[Li+].[H-].[H-].[H-].C(C)(=O)OCC>>CC1=C(N=C(O1)C1=CC=CC=C1)CCO
CO[C:14]([CH2:13][c:12]1[c:2]([CH3:1])[o:3][c:4](-[c:5]2[cH:6][cH:7][cH:8][cH:9][cH:10]2)[n:11]1)=[O:15]>>[CH3:1][c:2]1[o:3][c:4](-[c:5]2[cH:6][cH:7][cH:8][cH:9][cH:10]2)[n:11][c:12]1[CH2:13][CH2:14][OH:15]
COC(=O)Cc1nc(-c2ccccc2)oc1C
Cc1oc(-c2ccccc2)nc1CCO
null
null
C(C)OCC
Reduction
Reduction of ester to primary alcohol
21d61543c6ec8a8cebe1b3ef55ef3dd20acbf79a4f1c12a7fb51e32be7a3248a
1fbcd628a0426673c5d10aa49a977cd2d1ae02a8cdf57bbb10d94aa03a94e937
c1ccc(-c2ncco2)cc1
C-O-[C;H0;D3;+0:1](=[O;H0;D1;+0:2])-[C:3]-[c:4](:[#7;a:5]):[c:6]:[#8;a:7]>>[#7;a:5]:[c:4](-[C:3]-[CH2;D2;+0:1]-[OH;D1;+0:2]):[c:6]:[#8;a:7]
96.5
[{"value": 96.2, "product": "CC1=C(N=C(O1)C1=CC=CC=C1)CCO", "details": "PERCENTYIELD", "is_desired": false}, {"value": 96.5, "product": "CC1=C(N=C(O1)C1=CC=CC=C1)CCO", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
null
null
A solution of methyl 5-methyl-2-phenyl-4-oxazoleacetate (54 g) in dry ethyl ether (150 ml) was added dropwise to a stirred, ice-cooled suspension of lithium aluminum hydride (8.8 g) in dry ethyl ether (700 ml) during 1.5 hours. Ethyl acetate (20 ml) was added dropwise thereto with ice-cooling and then water (50 ml) was...
10.6084/m9.figshare.5104873.v1
null
Ester
Primary alcohol
null
null
c1cocn1.c1ccccc1
Other
C(C)OCC
null
null
COC(=O)Cc1nc(-c2ccccc2)oc1C>C(C)OCC>Cc1oc(-c2ccccc2)nc1CCO
ord_dataset-01dbb772c5e249108f0b191ed17a2c0c
ord-2feeb981fa26423a88ce70051e08a909
Cc1nc(CCO)c(C)o1.O=[N+]([O-])c1ccc(F)cc1>>Cc1nc(CCOc2ccc([N+](=O)[O-])cc2)c(C)o1
O.CC=1OC(=C(N1)CCO)C.FC1=CC=C(C=C1)[N+](=O)[O-].[H-].[Na+]>>CC=1OC(=C(N1)CCOC1=CC=C(C=C1)[N+](=O)[O-])C
[CH3:1][c:2]1[n:3][c:4]([CH2:5][CH2:6][OH:7])[c:17]([CH3:18])[o:19]1.F[c:8]1[cH:9][cH:10][c:11]([N+:12](=[O:13])[O-:14])[cH:15][cH:16]1>>[CH3:1][c:2]1[n:3][c:4]([CH2:5][CH2:6][O:7][c:8]2[cH:9][cH:10][c:11]([N+:12](=[O:13])[O-:14])[cH:15][cH:16]2)[c:17]([CH3:18])[o:19]1
Cc1nc(CCO)c(C)o1.O=[N+]([O-])c1ccc(F)cc1
Cc1nc(CCOc2ccc([N+](=O)[O-])cc2)c(C)o1
null
null
CN(C=O)C
Heteroatom Alkylation and Arylation
Williamson Ether Synthesis
4821d6d7238522ee9ef4538c00647e855becf4de3d9c939c0cec2b01c1e5e915
a4cafa7bcd156e21cca6eaac1b32e28ec8540642a31181122e6957f3d7559631
c1ccc(OCCc2cocn2)cc1
F-[c;H0;D3;+0:1](:[c:2]:[c:3]):[c:4]:[c:5].[C:6]-[C:7]-[OH;D1;+0:8]>>[C:6]-[C:7]-[O;H0;D2;+0:8]-[c;H0;D3;+0:1](:[c:2]:[c:3]):[c:4]:[c:5]
87.1
[{"value": 87.0, "product": "CC=1OC(=C(N1)CCOC1=CC=C(C=C1)[N+](=O)[O-])C", "details": "PERCENTYIELD", "is_desired": false}, {"value": 87.1, "product": "CC=1OC(=C(N1)CCOC1=CC=C(C=C1)[N+](=O)[O-])C", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
1
HOUR
2-(2,5-Dimethyl-4-oxazolyl)ethanol (17.0 g) and 4-fluoronitrobenzene (17.0 g) were dissolved in N,N-dimethylformamide (150 ml), and 60% sodium hydride in oil (6.0 g) was added dropwise to the solution under vigorous stirring. After stirring at room temperature for 1 hour, the reaction mixture was poured into water (1 l...
10.6084/m9.figshare.5104873.v1
null
Aromatic halide.Primary alcohol
Ether
c1ccccc1
c1ccccc1
c1cocn1.c1ccccc1
HF
CN(C=O)C
null
1
Cc1nc(CCO)c(C)o1.O=[N+]([O-])c1ccc(F)cc1>CN(C=O)C>Cc1nc(CCOc2ccc([N+](=O)[O-])cc2)c(C)o1
ord_dataset-01dbb772c5e249108f0b191ed17a2c0c
ord-fa6b00b25d154a97988b043a2abfac3a
BrBr.CC(=O)c1nc(-c2ccccc2)oc1C>>Cc1oc(-c2ccccc2)nc1C(=O)CBr
C(C)(=O)C=1N=C(OC1C)C1=CC=CC=C1.BrBr.C([O-])(O)=O.[Na+]>>BrCC(=O)C=1N=C(OC1C)C1=CC=CC=C1
Br[Br:16].[CH3:1][c:2]1[o:3][c:4](-[c:5]2[cH:6][cH:7][cH:8][cH:9][cH:10]2)[n:11][c:12]1[C:13](=[O:14])[CH3:15]>>[CH3:1][c:2]1[o:3][c:4](-[c:5]2[cH:6][cH:7][cH:8][cH:9][cH:10]2)[n:11][c:12]1[C:13](=[O:14])[CH2:15][Br:16]
BrBr.CC(=O)c1nc(-c2ccccc2)oc1C
Cc1oc(-c2ccccc2)nc1C(=O)CBr
null
null
C(Cl)(Cl)Cl
Functional Group Interconversion
Bromination
97ca6720945af5a02c450d33ec56e946521050f9771c27f9cfcb85f3477593f6
cb3e14519230141aa015a4cf9c960def3e60f01997e61621f62506924bfa15de
c1ccc(-c2ncco2)cc1
Br-[Br;H0;D1;+0:1].[#7;a:2]:[c:3](-[C:4](-[CH3;D1;+0:5])=[O;D1;H0:6]):[c:7]:[#8;a:8]>>[#7;a:2]:[c:3](-[C:4](=[O;D1;H0:6])-[CH2;D2;+0:5]-[Br;H0;D1;+0:1]):[c:7]:[#8;a:8]
86.8
[{"value": 86.3, "product": "BrCC(=O)C=1N=C(OC1C)C1=CC=CC=C1", "details": "PERCENTYIELD", "is_desired": false}, {"value": 86.8, "product": "BrCC(=O)C=1N=C(OC1C)C1=CC=CC=C1", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
55
CELSIUS
null
null
To a stirred solution of 4-acetyl-5-methyl-2-phenyloxazole (12.0 g) in chloroform (100 ml) was added at 50° C. a solution of bromine (10.5 g) in chloroform (10 ml). The mixture was further heated at 55° C. for 30 minutes and poured into saturated aqueous sodium bicarbonate solution (500 ml). The chloroform layer was se...
10.6084/m9.figshare.5104873.v1
null
Ketone
Primary halide
null
null
c1cocn1.c1ccccc1
HBr
C(Cl)(Cl)Cl
55
null
BrBr.CC(=O)c1nc(-c2ccccc2)oc1C>C(Cl)(Cl)Cl>Cc1oc(-c2ccccc2)nc1C(=O)CBr
ord_dataset-01dbb772c5e249108f0b191ed17a2c0c
ord-edc4b3f2acff4e9497253a46d41f09ff
Br.C=CC(=O)OC.Cc1oc(-c2ccccc2)nc1C(O)COc1ccc(N)cc1>>COC(=O)C(Br)Cc1ccc(OCC(O)c2nc(-c3ccccc3)oc2C)cc1
N(=O)[O-].[Na+].OC(COC1=CC=C(N)C=C1)C=1N=C(OC1C)C1=CC=CC=C1.Br.C(C=C)(=O)OC>>BrC(C(=O)OC)CC1=CC=C(C=C1)OCC(C=1N=C(OC1C)C1=CC=CC=C1)O
[BrH:6].[CH3:1][O:2][C:3](=[O:4])[CH:5]=[CH2:7].N[c:8]1[cH:9][cH:10][c:11]([O:12][CH2:13][CH:14]([OH:15])[c:16]2[n:17][c:18](-[c:19]3[cH:20][cH:21][cH:22][cH:23][cH:24]3)[o:25][c:26]2[CH3:27])[cH:28][cH:29]1>>[CH3:1][O:2][C:3](=[O:4])[CH:5]([Br:6])[CH2:7][c:8]1[cH:9][cH:10][c:11]([O:12][CH2:13][CH:14]([OH:15])[c:16]2[n...
Br.C=CC(=O)OC.Cc1oc(-c2ccccc2)nc1C(O)COc1ccc(N)cc1
COC(=O)C(Br)Cc1ccc(OCC(O)c2nc(-c3ccccc3)oc2C)cc1
null
null
CO.O.CC(=O)C
C-C Coupling
OtherReaction
fa6d89a11df1d51d550d71070755be72f9bdb83552839bba404de654836fff02
50a9d170f44f15d35e3a7d8ced3592a8de4e6e68b8b82ffc0f15a38f0aee2772
c1ccc(OCCc2coc(-c3ccccc3)n2)cc1
N-[c;H0;D3;+0:1](:[c:2]:[c:3]):[c:4]:[c:5].[BrH;D0;+0:6].[C;D1;H3:7]-[#8:8]-[C:9](=[O;D1;H0:10])-[CH;D2;+0:11]=[CH2;D1;+0:12]>>[Br;H0;D1;+0:6]-[CH;D3;+0:11](-[CH2;D2;+0:12]-[c;H0;D3;+0:1](:[c:2]:[c:3]):[c:4]:[c:5])-[C:9](=[O;D1;H0:10])-[#8:8]-[C;D1;H3:7]
98.5
[{"value": 98.5, "product": null, "details": "PERCENTYIELD", "is_desired": false}]
5
CELSIUS
15
MINUTE
4-[2-Hydroxy-2-(5-methyl-2-phenyl-4-oxazolyl)ethoxy]aniline (18.5 g) was dissolved in methanol (50 ml)-acetone (150 ml), and 47% aqueous HBr (41.0 g) was added to the solution. Then, a solution of NaNO2 (4.5 g) in water (10 ml) was added dropwise to the mixture at a temperature of not higher than 5° C. The whole was st...
10.6084/m9.figshare.5104873.v1
null
Ester.Primary amine.Vinyl
Secondary halide.Ester
c1ccccc1
c1ccccc1
c1ccccc1.c1cocn1.c1ccccc1
Other
CO.O.CC(=O)C
5
0.25
Br.C=CC(=O)OC.Cc1oc(-c2ccccc2)nc1C(O)COc1ccc(N)cc1>CO.O.CC(=O)C>COC(=O)C(Br)Cc1ccc(OCC(O)c2nc(-c3ccccc3)oc2C)cc1
ord_dataset-01dbb772c5e249108f0b191ed17a2c0c
ord-4df1147214394778b695246102bc2d3e
Cc1oc(-c2ccccc2Cl)nc1CCOc1ccc([N+](=O)[O-])cc1>>Cc1oc(-c2ccccc2Cl)nc1CCOc1ccc(N)cc1
ClC1=C(C=CC=C1)C=1OC(=C(N1)CCOC1=CC=C(C=C1)[N+](=O)[O-])C.C(C)(=O)O>>ClC1=C(C=CC=C1)C=1OC(=C(N1)CCOC1=CC=C(N)C=C1)C
O=[N+:21]([O-])[c:20]1[cH:19][cH:18][c:17]([O:16][CH2:15][CH2:14][c:13]2[c:2]([CH3:1])[o:3][c:4](-[c:5]3[cH:6][cH:7][cH:8][cH:9][c:10]3[Cl:11])[n:12]2)[cH:23][cH:22]1>>[CH3:1][c:2]1[o:3][c:4](-[c:5]2[cH:6][cH:7][cH:8][cH:9][c:10]2[Cl:11])[n:12][c:13]1[CH2:14][CH2:15][O:16][c:17]1[cH:18][cH:19][c:20]([NH2:21])[cH:22][cH...
Cc1oc(-c2ccccc2Cl)nc1CCOc1ccc([N+](=O)[O-])cc1
Cc1oc(-c2ccccc2Cl)nc1CCOc1ccc(N)cc1
null
null
O
Reduction
Reduction of nitro groups to amines
bbc242b150a51e69d3ad1caaa391f4422710431b398dcb880555f476706790be
7b0317532ea57a4fcedc1efc3e3c22eb5238d1c8330da53d4f9801fc2391f567
c1ccc(OCCc2coc(-c3ccccc3)n2)cc1
O=[N+;H0;D3:1](-[O-])-[c:2](:[c:3]):[c:4]>>[NH2;D1;+0:1]-[c:2](:[c:3]):[c:4]
97.6
[{"value": 97.6, "product": null, "details": "PERCENTYIELD", "is_desired": false}]
80
CELSIUS
2
HOUR
Reduced iron (10.6 g) was added portionwise mixture of 4-{2-[2-(2-chlorophenyl)-5-methyl-4-oxazolyl]ethoxy}nitrobenzene (22.9 g), acetic acid (150 ml) and water (50 ml) at 70° C. After stirring at 80° C. for 2 hours, the insoluble matter was filtered off, and the filtrate was concentrated under reduced pressure. Water ...
10.6084/m9.figshare.5104873.v1
null
Nitro group
Primary amine
null
null
c1cocn1.c1ccccc1.c1ccccc1
Other
O
80
2
Cc1oc(-c2ccccc2Cl)nc1CCOc1ccc([N+](=O)[O-])cc1>O>Cc1oc(-c2ccccc2Cl)nc1CCOc1ccc(N)cc1
ord_dataset-01dbb772c5e249108f0b191ed17a2c0c
ord-a0c3c5e052b64fc395583abf06cf5d36
Cc1oc(-c2ccc(OCc3ccccc3)cc2)nc1CCOc1ccc([N+](=O)[O-])cc1>>Cc1oc(-c2ccc(O)cc2)nc1CCOc1ccc(N)cc1
C(C1=CC=CC=C1)OC1=CC=C(C=C1)C=1OC(=C(N1)CCOC1=CC=C(C=C1)[N+](=O)[O-])C>>OC1=CC=C(C=C1)C=1OC(=C(N1)CCOC1=CC=C(N)C=C1)C
O=[N+:21]([O-])[c:20]1[cH:19][cH:18][c:17]([O:16][CH2:15][CH2:14][c:13]2[c:2]([CH3:1])[o:3][c:4](-[c:5]3[cH:6][cH:7][c:8]([O:9]Cc4ccccc4)[cH:10][cH:11]3)[n:12]2)[cH:23][cH:22]1>>[CH3:1][c:2]1[o:3][c:4](-[c:5]2[cH:6][cH:7][c:8]([OH:9])[cH:10][cH:11]2)[n:12][c:13]1[CH2:14][CH2:15][O:16][c:17]1[cH:18][cH:19][c:20]([NH2:21...
Cc1oc(-c2ccc(OCc3ccccc3)cc2)nc1CCOc1ccc([N+](=O)[O-])cc1
Cc1oc(-c2ccc(O)cc2)nc1CCOc1ccc(N)cc1
null
[Pd]
CO
Reduction
OtherReaction
9170d0c986a4b23b0014d38a47c7fc9d4706242a2267d3f5bc0d6f66b2394435
f6fedbf3f30216a140de5c3218dc044b3cb8996afe756cfb2650e812e7cf56ad
c1ccc(OCCc2coc(-c3ccccc3)n2)cc1
O=[N+;H0;D3:1](-[O-])-[c:2](:[c:3]):[c:4].[c:5]:[c:6](-[O;H0;D2;+0:7]-C-c1:c:c:c:c:c:1):[c:8]>>[NH2;D1;+0:1]-[c:2](:[c:3]):[c:4].[OH;D1;+0:7]-[c:6](:[c:5]):[c:8]
80.9
[{"value": 78.2, "product": "OC1=CC=C(C=C1)C=1OC(=C(N1)CCOC1=CC=C(N)C=C1)C", "details": "PERCENTYIELD", "is_desired": false}, {"value": 80.9, "product": "OC1=CC=C(C=C1)C=1OC(=C(N1)CCOC1=CC=C(N)C=C1)C", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
null
null
A solution of 4-{2-[2-(4-benzyloxyphenyl)-5-methyl-4-oxazolyl]ethoxy}nitrobenzene (10.65 g) in methanol (200 ml) was subjected to a catalytic hydrogenation over 10% Pd-C (50% wet, 4.0 g). After the catalyst was filtered off, the filtrate was concentrated to give 4-{2-[2-(4-hydroxyphenyl)-5-methyl-4-oxazolyl]ethoxy}anil...
10.6084/m9.figshare.5104873.v1
null
Ether.Nitro group
Aromatic alcohol.Primary amine
c1ccccc1
null
c1cocn1.c1ccccc1.c1ccccc1
HO-
[Pd].CO
null
null
Cc1oc(-c2ccc(OCc3ccccc3)cc2)nc1CCOc1ccc([N+](=O)[O-])cc1>[Pd].CO>Cc1oc(-c2ccc(O)cc2)nc1CCOc1ccc(N)cc1
ord_dataset-01dbb772c5e249108f0b191ed17a2c0c
ord-760057bc35304f8ba2f1de1ab245109e
Cc1oc(-c2ccccc2)nc1CCOc1ccc(/C=C2\SC(=O)NC2=O)cc1>>Cc1oc(-c2ccccc2)nc1CCOc1ccc(/C=C2/SC(=O)NC2=O)cc1
CC1=C(N=C(O1)C1=CC=CC=C1)CCOC1=CC=C(\C=C/2\C(NC(S2)=O)=O)C=C1>>CC1=C(N=C(O1)C1=CC=CC=C1)CCOC1=CC=C(\C=C\2/C(NC(S2)=O)=O)C=C1
[CH3:1][c:2]1[o:3][c:4](-[c:5]2[cH:6][cH:7][cH:8][cH:9][cH:10]2)[n:11][c:12]1[CH2:13][CH2:14][O:15][c:16]1[cH:17][cH:18][c:19](/[CH:20]=[C:21]2\[S:22][C:23](=[O:24])[NH:25][C:26]2=[O:27])[cH:28][cH:29]1>>[CH3:1][c:2]1[o:3][c:4](-[c:5]2[cH:6][cH:7][cH:8][cH:9][cH:10]2)[n:11][c:12]1[CH2:13][CH2:14][O:15][c:16]1[cH:17][cH...
Cc1oc(-c2ccccc2)nc1CCOc1ccc(/C=C2\SC(=O)NC2=O)cc1
Cc1oc(-c2ccccc2)nc1CCOc1ccc(/C=C2/SC(=O)NC2=O)cc1
null
null
C(C)#N
Miscellaneous
OtherReaction
40ba59785861b8226ce5af6bdcbb9a37f0ff50a8c7ec7d4fc4c524cf906cc65c
56ebed4a8b3cebec83c37a71d68f0c87d1e404ab05a9ce792691e4e18a2379dd
O=C1NC(=O)/C(=C\c2ccc(OCCc3coc(-c4ccccc4)n3)cc2)S1
null
20
[{"value": 20.0, "product": "CC1=C(N=C(O1)C1=CC=CC=C1)CCOC1=CC=C(\\C=C\\2/C(NC(S2)=O)=O)C=C1", "details": "PERCENTYIELD", "is_desired": false}, {"value": 20.0, "product": "CC1=C(N=C(O1)C1=CC=CC=C1)CCOC1=CC=C(\\C=C\\2/C(NC(S2)=O)=O)C=C1", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
null
null
A solution of (Z)-5-{4-[2-(5-methyl-2-phenyl-4-oxazolyl)ethoxy]benzylidene}-2,4-thiazolidinedione (200 mg) in acetonitrile (750 ml), in a quartz tube under a stream of nitrogen, was irradiated by a 300 W high-pressure mercury lamp for 3 hours. The solvent was distilled off, and the resulting crystals were chromatograph...
10.6084/m9.figshare.5104873.v1
null
null
null
null
null
c1cocn1.c1ccccc1.c1ccccc1.C1CSCN1
null
C(C)#N
null
null
Cc1oc(-c2ccccc2)nc1CCOc1ccc(/C=C2\SC(=O)NC2=O)cc1>C(C)#N>Cc1oc(-c2ccccc2)nc1CCOc1ccc(/C=C2/SC(=O)NC2=O)cc1
ord_dataset-01dbb772c5e249108f0b191ed17a2c0c
ord-ef7d7d2ba1b7436d9bffae2309e59136
Cc1oc(-c2ccccc2)nc1CCO.N#Cc1ccc(F)cc1>>Cc1oc(-c2ccccc2)nc1CCOc1ccc(C#N)cc1
CC1=C(N=C(O1)C1=CC=CC=C1)CCO.FC1=CC=C(C#N)C=C1.[H-].[Na+].C(C)(=O)O>>CC1=C(N=C(O1)C1=CC=CC=C1)CCOC1=CC=C(C#N)C=C1
[CH3:1][c:2]1[o:3][c:4](-[c:5]2[cH:6][cH:7][cH:8][cH:9][cH:10]2)[n:11][c:12]1[CH2:13][CH2:14][OH:15].F[c:16]1[cH:17][cH:18][c:19]([C:20]#[N:21])[cH:22][cH:23]1>>[CH3:1][c:2]1[o:3][c:4](-[c:5]2[cH:6][cH:7][cH:8][cH:9][cH:10]2)[n:11][c:12]1[CH2:13][CH2:14][O:15][c:16]1[cH:17][cH:18][c:19]([C:20]#[N:21])[cH:22][cH:23]1
Cc1oc(-c2ccccc2)nc1CCO.N#Cc1ccc(F)cc1
Cc1oc(-c2ccccc2)nc1CCOc1ccc(C#N)cc1
null
null
O1CCCC1
Heteroatom Alkylation and Arylation
Williamson Ether Synthesis
4821d6d7238522ee9ef4538c00647e855becf4de3d9c939c0cec2b01c1e5e915
a4cafa7bcd156e21cca6eaac1b32e28ec8540642a31181122e6957f3d7559631
c1ccc(OCCc2coc(-c3ccccc3)n2)cc1
F-[c;H0;D3;+0:1](:[c:2]:[c:3]):[c:4]:[c:5].[C:6]-[C:7]-[OH;D1;+0:8]>>[C:6]-[C:7]-[O;H0;D2;+0:8]-[c;H0;D3;+0:1](:[c:2]:[c:3]):[c:4]:[c:5]
77.9
[{"value": 77.5, "product": "CC1=C(N=C(O1)C1=CC=CC=C1)CCOC1=CC=C(C#N)C=C1", "details": "PERCENTYIELD", "is_desired": false}, {"value": 77.9, "product": "CC1=C(N=C(O1)C1=CC=CC=C1)CCOC1=CC=C(C#N)C=C1", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
18
HOUR
2-(5-Methyl-2-phenyl-4-oxazolyl)ethanol (6.0 g) and 4-fluorobenzonitrile (5.4 g) were dissolved in tetrahydrofurane (70 ml ), and 60% sodium hydride in oil (1.4 g) was added to the solution under ice-cooling with vigorous stirring. The reaction mixture was stirred at room temperature for 18 hours and poured into ice-co...
10.6084/m9.figshare.5104873.v1
null
Aromatic halide.Primary alcohol
Ether
c1ccccc1
c1ccccc1
c1cocn1.c1ccccc1.c1ccccc1
HF
O1CCCC1
null
18
Cc1oc(-c2ccccc2)nc1CCO.N#Cc1ccc(F)cc1>O1CCCC1>Cc1oc(-c2ccccc2)nc1CCOc1ccc(C#N)cc1
ord_dataset-01dbb772c5e249108f0b191ed17a2c0c
ord-02ae9b80d0de45e4bc6c27c8e8753812
Cc1oc(-c2ccccc2)nc1CCOc1ccc(C#N)cc1.O=CO>>Cc1oc(-c2ccccc2)nc1CCOc1ccc(C=O)cc1
CC1=C(N=C(O1)C1=CC=CC=C1)CCOC1=CC=C(C#N)C=C1.C(=O)O>>CC1=C(N=C(O1)C1=CC=CC=C1)CCOC1=CC=C(C=O)C=C1
N#[C:20][c:19]1[cH:18][cH:17][c:16]([O:15][CH2:14][CH2:13][c:12]2[c:2]([CH3:1])[o:3][c:4](-[c:5]3[cH:6][cH:7][cH:8][cH:9][cH:10]3)[n:11]2)[cH:23][cH:22]1.OC=[O:21]>>[CH3:1][c:2]1[o:3][c:4](-[c:5]2[cH:6][cH:7][cH:8][cH:9][cH:10]2)[n:11][c:12]1[CH2:13][CH2:14][O:15][c:16]1[cH:17][cH:18][c:19]([CH:20]=[O:21])[cH:22][cH:23...
Cc1oc(-c2ccccc2)nc1CCOc1ccc(C#N)cc1.O=CO
Cc1oc(-c2ccccc2)nc1CCOc1ccc(C=O)cc1
null
[Ni]
null
Miscellaneous
OtherReaction
dd48b99193436fbe7b6cc0a1621b6770f60b9def12aae5a3798f5538fe569c97
0897ec40f28c09937bcdbb0203ea69433f1817427a4cf5fff67c67ea215ea2af
c1ccc(OCCc2coc(-c3ccccc3)n2)cc1
N#[C;H0;D2;+0:1]-[c:2](:[c:3]):[c:4].O-C=[O;H0;D1;+0:5]>>[O;H0;D1;+0:5]=[CH;D2;+0:1]-[c:2](:[c:3]):[c:4]
78.5
[{"value": 78.5, "product": "CC1=C(N=C(O1)C1=CC=CC=C1)CCOC1=CC=C(C=O)C=C1", "details": "PERCENTYIELD", "is_desired": false}]
null
null
null
null
A mixture of 4-[2-(5-methyl-2-phenyl-4-oxazolyl)ethoxy]benzonitrile (6.5 g), Raney nickel alloy (6.5 g) and 70% formic acid (100 ml) was heated under reflux for 2 hours. The insoluble matter was filtered off, and the filtrate was concentrated under reduced pressure. Water was added to the residue, and the mixture was e...
10.6084/m9.figshare.5104873.v1
null
Carboxylic acid.Nitrile
Aldehyde
null
null
c1cocn1.c1ccccc1.c1ccccc1
HO-
[Ni]
null
null
Cc1oc(-c2ccccc2)nc1CCOc1ccc(C#N)cc1.O=CO>[Ni]>Cc1oc(-c2ccccc2)nc1CCOc1ccc(C=O)cc1
ord_dataset-01dbb772c5e249108f0b191ed17a2c0c
ord-87fabac48c9340eaa4907ce30b7c5b7e
Cc1oc(-c2ccccc2)nc1CCl.O=Cc1ccc(O)cc1>>Cc1oc(-c2ccccc2)nc1COc1ccc(C=O)cc1
ClCC=1N=C(OC1C)C1=CC=CC=C1.OC1=CC=C(C=O)C=C1.C([O-])([O-])=O.[K+].[K+]>>CC1=C(N=C(O1)C1=CC=CC=C1)COC1=CC=C(C=O)C=C1
Cl[CH2:13][c:12]1[c:2]([CH3:1])[o:3][c:4](-[c:5]2[cH:6][cH:7][cH:8][cH:9][cH:10]2)[n:11]1.[OH:14][c:15]1[cH:16][cH:17][c:18]([CH:19]=[O:20])[cH:21][cH:22]1>>[CH3:1][c:2]1[o:3][c:4](-[c:5]2[cH:6][cH:7][cH:8][cH:9][cH:10]2)[n:11][c:12]1[CH2:13][O:14][c:15]1[cH:16][cH:17][c:18]([CH:19]=[O:20])[cH:21][cH:22]1
Cc1oc(-c2ccccc2)nc1CCl.O=Cc1ccc(O)cc1
Cc1oc(-c2ccccc2)nc1COc1ccc(C=O)cc1
null
null
null
Heteroatom Alkylation and Arylation
Williamson Ether Synthesis
7e1040116e3a4cf0e8ec5cc7865388d9cd0efabce6d320a1c25a36e411018d8b
d5f4610d46ccc0478471c5bc0fb862644eaf764bbc5d93badb39d54f6ec8e0a5
c1ccc(OCc2coc(-c3ccccc3)n2)cc1
Cl-[CH2;D2;+0:1]-[c:2]1:[#7;a:3]:[c:4]:[#8;a:5]:[c:6]:1-[C;D1;H3:7].[OH;D1;+0:8]-[c:9](:[c:10]):[c:11]>>[C;D1;H3:7]-[c:6]1:[#8;a:5]:[c:4]:[#7;a:3]:[c:2]:1-[CH2;D2;+0:1]-[O;H0;D2;+0:8]-[c:9](:[c:10]):[c:11]
100.1
[{"value": 99.8, "product": "CC1=C(N=C(O1)C1=CC=CC=C1)COC1=CC=C(C=O)C=C1", "details": "PERCENTYIELD", "is_desired": false}, {"value": 100.1, "product": "CC1=C(N=C(O1)C1=CC=CC=C1)COC1=CC=C(C=O)C=C1", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
110
CELSIUS
null
null
A mixture of 4-chloromethyl-5-methyl-2-phenyloxazole (3.12 g), 4-hydroxybenzaldehyde (1.83 g), potassium carbonate (2.28 g) and dimethylformaide (40 ml) was stirred under heating at 110° C. for 1 hour. The reaction solution was poured into ice-cold water, and the crystals which separated out were collected by filtratio...
10.6084/m9.figshare.5104873.v1
null
Primary halide.Aromatic alcohol
Ether
null
null
c1cocn1.c1ccccc1.c1ccccc1
HCl
null
110
null
Cc1oc(-c2ccccc2)nc1CCl.O=Cc1ccc(O)cc1>>Cc1oc(-c2ccccc2)nc1COc1ccc(C=O)cc1
ord_dataset-01dbb772c5e249108f0b191ed17a2c0c
ord-b8196817410144b5adfdc7884be60b1f
Cc1oc(-c2ccccc2)nc1C(=O)CBr.N#Cc1ccc(O)cc1>>Cc1oc(-c2ccccc2)nc1C(=O)COc1ccc(C#N)cc1
BrCC(=O)C=1N=C(OC1C)C1=CC=CC=C1.C(#N)C1=CC=C(C=C1)O.C([O-])([O-])=O.[K+].[K+]>>CC1=C(N=C(O1)C1=CC=CC=C1)C(COC1=CC=C(C#N)C=C1)=O
Br[CH2:15][C:13]([c:12]1[c:2]([CH3:1])[o:3][c:4](-[c:5]2[cH:6][cH:7][cH:8][cH:9][cH:10]2)[n:11]1)=[O:14].[OH:16][c:17]1[cH:18][cH:19][c:20]([C:21]#[N:22])[cH:23][cH:24]1>>[CH3:1][c:2]1[o:3][c:4](-[c:5]2[cH:6][cH:7][cH:8][cH:9][cH:10]2)[n:11][c:12]1[C:13](=[O:14])[CH2:15][O:16][c:17]1[cH:18][cH:19][c:20]([C:21]#[N:22])[...
Cc1oc(-c2ccccc2)nc1C(=O)CBr.N#Cc1ccc(O)cc1
Cc1oc(-c2ccccc2)nc1C(=O)COc1ccc(C#N)cc1
null
null
C(C)C(=O)C
Heteroatom Alkylation and Arylation
Williamson Ether Synthesis
8060b8e1565497a5ddf79be1adfe74f552b31798797b8841753247b06bdd2051
8749b179916f131d393264a24309227dc6177f560726bed2d1f4567dc2ac63f5
O=C(COc1ccccc1)c1coc(-c2ccccc2)n1
Br-[CH2;D2;+0:1]-[C:2](=[O;D1;H0:3])-[c:4](:[#7;a:5]):[c:6]:[#8;a:7].[OH;D1;+0:8]-[c:9](:[c:10]):[c:11]>>[#7;a:5]:[c:4](-[C:2](=[O;D1;H0:3])-[CH2;D2;+0:1]-[O;H0;D2;+0:8]-[c:9](:[c:10]):[c:11]):[c:6]:[#8;a:7]
79.2
[{"value": 78.8, "product": "CC1=C(N=C(O1)C1=CC=CC=C1)C(COC1=CC=C(C#N)C=C1)=O", "details": "PERCENTYIELD", "is_desired": false}, {"value": 79.2, "product": "CC1=C(N=C(O1)C1=CC=CC=C1)C(COC1=CC=C(C#N)C=C1)=O", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
null
null
A mixture of 4-bromoacetyl-5-methyl-2-phenyloxazole (7.0 g), p-cyanophenol (3.0 g), potassium carbonate (6.9 g) and methyl ethyl ketone (100 ml) was heated under reflux for 2 hours. The reaction mixture was concentrated under reduced pressure, and water (100 ml)-ether (100 ml) was added to the residue. The mixture was ...
10.6084/m9.figshare.5104873.v1
null
Primary halide.Ketone.Aromatic alcohol
Ketone.Ether
null
null
c1cocn1.c1ccccc1.c1ccccc1
HBr
C(C)C(=O)C
null
null
Cc1oc(-c2ccccc2)nc1C(=O)CBr.N#Cc1ccc(O)cc1>C(C)C(=O)C>Cc1oc(-c2ccccc2)nc1C(=O)COc1ccc(C#N)cc1
ord_dataset-01dbb772c5e249108f0b191ed17a2c0c
ord-2f9a930e708d48b38d38a3a790caddee
Cc1oc(-c2ccccc2)nc1C(=O)COc1ccc(C#N)cc1>>Cc1cccc(-c2nc(C(O)COc3ccc(C#N)cc3)co2)c1
O.[BH4-].[Na+].CC1=C(N=C(O1)C1=CC=CC=C1)C(COC1=CC=C(C#N)C=C1)=O.CN(C=O)C>>OC(COC1=CC=C(C#N)C=C1)C=1N=C(OC1)C1=CC=CC(=C1)C
[CH3:1][c:22]1[c:9]([C:10](=[O:11])[CH2:12][O:13][c:14]2[cH:15][cH:16][c:17]([C:18]#[N:19])[cH:20][cH:21]2)[n:8][c:7](-[c:6]2[cH:5][cH:4][cH:3][cH:2][cH:24]2)[o:23]1>>[CH3:1][c:2]1[cH:3][cH:4][cH:5][c:6](-[c:7]2[n:8][c:9]([CH:10]([OH:11])[CH2:12][O:13][c:14]3[cH:15][cH:16][c:17]([C:18]#[N:19])[cH:20][cH:21]3)[cH:22][o:...
Cc1oc(-c2ccccc2)nc1C(=O)COc1ccc(C#N)cc1
Cc1cccc(-c2nc(C(O)COc3ccc(C#N)cc3)co2)c1
null
null
CO
Miscellaneous
OtherReaction
ec9ef35050ba6985dceafd1b0dd2e08e66adecacf64ee5cef48bcba0b8c2eb13
65c0f1e474134afe581396038c9eec1081d3cf2c66a067b33a419661521d5253
c1ccc(OCCc2coc(-c3ccccc3)n2)cc1
[#8:1]-[C:2]-[C;H0;D3;+0:3](=[O;H0;D1;+0:4])-[c:5]1:[#7;a:6]:[c:7](-[c:8]:[c:9]:[cH;D2;+0:10]:[c:11]:[c:12]):[#8;a:13]:[c;H0;D3;+0:14]:1-[CH3;D1;+0:15]>>[#8:1]-[C:2]-[CH;D3;+0:3](-[OH;D1;+0:4])-[c:5]1:[#7;a:6]:[c:7](-[c:8]:[c:9]:[c;H0;D3;+0:10](-[CH3;D1;+0:15]):[c:11]:[c:12]):[#8;a:13]:[cH;D2;+0:14]:1
92.7
[{"value": 92.7, "product": "OC(COC1=CC=C(C#N)C=C1)C=1N=C(OC1)C1=CC=CC(=C1)C", "details": "PERCENTYIELD", "is_desired": false}]
null
null
1
HOUR
Sodium borohydride (0.654 mg) was added to a suspension of 4-[2-(5-methyl-2-phenyl-4-oxazolyl)-2-oxoethoxy]benzonitrile (5.5 g) in methanol (100 ml)-N,N-dimethylformamide (50 ml), followed by stirring at room temperature for 1 hour. The reaction solution was poured into water and the crystals which separated out were c...
10.6084/m9.figshare.5104873.v1
null
Ketone
Secondary alcohol
c1cocn1.c1ccccc1
c1ccccc1.c1cocn1
c1ccccc1.c1cocn1.c1ccccc1
null
CO
null
1
Cc1oc(-c2ccccc2)nc1C(=O)COc1ccc(C#N)cc1>CO>Cc1cccc(-c2nc(C(O)COc3ccc(C#N)cc3)co2)c1
ord_dataset-01dbb772c5e249108f0b191ed17a2c0c
ord-af833aac68e84efd9b9b7fe09d4bd9be
CCOC(=S)CC/C(C)=C/Cc1c(O)c2c(c(C)c1OC)COC2=O.O=C(Cl)Cl>>CCOC(=S)CC/C(C)=C/Cc1c(OC)c(C)c2c(c1OC(N)=O)C(=O)OC2
OC1=C2C(OCC2=C(C(=C1C/C=C(/CCC(=S)OCC)\C)OC)C)=O.N1=CC=CC=C1.C(=O)(Cl)Cl>>C(N)(=O)OC1=C2C(OCC2=C(C(=C1C/C=C(/CCC(=S)OCC)\C)OC)C)=O
[CH3:1][CH2:2][O:3][C:4](=[S:5])[CH2:6][CH2:7]/[C:8]([CH3:9])=[CH:10]/[CH2:11][c:12]1[c:13]([O:14][CH3:15])[c:16]([CH3:17])[c:18]2[c:19]([c:20]1[OH:21])[C:25](=[O:26])[O:27][CH2:28]2.Cl[C:22](Cl)=[O:24]>>[CH3:1][CH2:2][O:3][C:4](=[S:5])[CH2:6][CH2:7]/[C:8]([CH3:9])=[CH:10]/[CH2:11][c:12]1[c:13]([O:14][CH3:15])[c:16]([C...
CCOC(=S)CC/C(C)=C/Cc1c(O)c2c(c(C)c1OC)COC2=O.O=C(Cl)Cl
CCOC(=S)CC/C(C)=C/Cc1c(OC)c(C)c2c(c1OC(N)=O)C(=O)OC2
null
null
C1=CC=CC=C1
Functional Group Interconversion
OtherReaction
7a500c53e0c90ddb616b1d9844a25d18752778458f7cf9b6b4d76c7f92fd6ed9
1c930fd1a8ef596a25a9e8b02e0d655be711516e36782a4da179eb27706d6367
O=C1OCc2ccccc21
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 ethyl (E)-6-(1,3-dihydro-4-hydroxy-6-methoxy-7-methyl-3-oxo-5-isobenzofuranyl)-4-methyl-4-thiohexenoate in 10 ml of benzene cooled in an ice bath was added 0.1 ml of pyridine and 6 ml of a 12.5% solution of phosgene in benzene. The solution was stirred at 25° C. overnight, the precipitate fi...
10.6084/m9.figshare.5104873.v1
null
Acyl halide.Acyl halide.Aromatic alcohol
Carbamic ester
null
null
c1ccc2c(c1)COC2
Other
C1=CC=CC=C1
25
8
CCOC(=S)CC/C(C)=C/Cc1c(O)c2c(c(C)c1OC)COC2=O.O=C(Cl)Cl>C1=CC=CC=C1>CCOC(=S)CC/C(C)=C/Cc1c(OC)c(C)c2c(c1OC(N)=O)C(=O)OC2
ord_dataset-01dbb772c5e249108f0b191ed17a2c0c
ord-06f8abb82a5a4632b3979237b8ea745a
CC(=O)Cl.CCOC(=S)CC/C(C)=C/Cc1c(O)c2c(c(C)c1OC)COC2=O>>CCOC(=S)CC/C(C)=C/Cc1c(OC)c(C)c2c(c1OC(C)=O)C(=O)OC2
Cl.C(C)(=O)Cl.OC1=C2C(OCC2=C(C(=C1C/C=C(/CCC(=S)OCC)\C)OC)C)=O.N1=CC=CC=C1>>C(C)(=O)OC1=C2C(OCC2=C(C(=C1C/C=C(/CCC(=S)OCC)\C)OC)C)=O
Cl[C:22]([CH3:23])=[O:24].[CH3:1][CH2:2][O:3][C:4](=[S:5])[CH2:6][CH2:7]/[C:8]([CH3:9])=[CH:10]/[CH2:11][c:12]1[c:13]([O:14][CH3:15])[c:16]([CH3:17])[c:18]2[c:19]([c:20]1[OH:21])[C:25](=[O:26])[O:27][CH2:28]2>>[CH3:1][CH2:2][O:3][C:4](=[S:5])[CH2:6][CH2:7]/[C:8]([CH3:9])=[CH:10]/[CH2:11][c:12]1[c:13]([O:14][CH3:15])[c:...
CC(=O)Cl.CCOC(=S)CC/C(C)=C/Cc1c(O)c2c(c(C)c1OC)COC2=O
CCOC(=S)CC/C(C)=C/Cc1c(OC)c(C)c2c(c1OC(C)=O)C(=O)OC2
null
null
C(C)#N
Acylation
Schotten-Baumann to ester
1cda078f55e64d9385e544d1067595d5e7672bbd1eff542e7a341817a2d8c4d5
6439fc27f97ee9ed7c11ef9b5032d9493d05f28a7bbb50d256a2d54d035fbfb2
O=C1OCc2ccccc21
Cl-[C;H0;D3;+0:1](-[C;D1;H3:2])=[O;D1;H0:3].[#8:4]-[C:5](=[O;D1;H0:6])-[c:7]:[c:8](-[OH;D1;+0:9]):[c:10]>>[#8:4]-[C:5](=[O;D1;H0:6])-[c:7]:[c:8](-[O;H0;D2;+0:9]-[C;H0;D3;+0:1](-[C;D1;H3:2])=[O;D1;H0:3]):[c:10]
null
[]
null
null
2
HOUR
To a solution of 1.6 g of ethyl (E)-6-(1,3-dihydro-4-hydroxy-6-methoxy-7-methyl-3-oxo-5-isobenzofuranyl)-4-methyl-4-thiohexenoate in 120 ml of acetonitrile at 0° C. was added 0.74 ml of pyridine followed by 1.0 ml of acetyl chloride. After stirring for 2 hours the reaction mixture was poured into dilute hydrochloric ac...
10.6084/m9.figshare.5104873.v1
null
Acyl halide.Aromatic alcohol
Ester
null
null
c1ccc2c(c1)COC2
HCl
C(C)#N
null
2
CC(=O)Cl.CCOC(=S)CC/C(C)=C/Cc1c(O)c2c(c(C)c1OC)COC2=O>C(C)#N>CCOC(=S)CC/C(C)=C/Cc1c(OC)c(C)c2c(c1OC(C)=O)C(=O)OC2
ord_dataset-01dbb772c5e249108f0b191ed17a2c0c
ord-12d70a69c7f449f5ae68d848a00b2a04
CCC(C)(C)N(CC(C)O)CC(C)O>>CC(O)CN(CC(C)O)C(C)(C)C
C(C)(C)(CC)N(CC(C)O)CC(C)O.CN(CC(C)O)CC(C)O.C(C)N(CCO)CCO.C1(CCCCC1)N(CCO)CCO.C(C)C(CO)(CO)CN(C)C>>C(C)(C)(C)N(CC(C)O)CC(C)O
C[CH2:12][C:10]([N:5]([CH2:4][CH:2]([CH3:1])[OH:3])[CH2:6][CH:7]([CH3:8])[OH:9])([CH3:11])[CH3:13]>>[CH3:1][CH:2]([OH:3])[CH2:4][N:5]([CH2:6][CH:7]([CH3:8])[OH:9])[C:10]([CH3:11])([CH3:12])[CH3:13]
CCC(C)(C)N(CC(C)O)CC(C)O
CC(O)CN(CC(C)O)C(C)(C)C
null
null
null
Miscellaneous
OtherReaction
40ba59785861b8226ce5af6bdcbb9a37f0ff50a8c7ec7d4fc4c524cf906cc65c
56ebed4a8b3cebec83c37a71d68f0c87d1e404ab05a9ce792691e4e18a2379dd
null
C-[CH2;D2;+0:1]-[C:2](-[#7:3])(-[C;D1;H3:4])-[C;D1;H3:5]>>[#7:3]-[C:2](-[C;D1;H3:4])(-[C;D1;H3:5])-[CH3;D1;+0:1]
null
[]
null
null
null
null
4-methyl-4-azaheptane-2,6-diol; 3-ethyl-3-azapentane-1,5-diol; 2-ethyl-2-dimethylamino methyl-propane-1,3-diol; 4-tertiary-pentyl-4-azaheptane-2,6-diol; 3-cyclohexyl-3-azapentane-1,5-diol, 3-tert-butylmethyl-3-azapentandiol-1,5, 3-tert.-pentyl-3-aza-pentandiol-1, Conditions: See reaction.notes.procedure_details.
10.6084/m9.figshare.5104873.v1
null
null
null
null
null
null
Other
null
null
null
CCC(C)(C)N(CC(C)O)CC(C)O>>CC(O)CN(CC(C)O)C(C)(C)C
ord_dataset-01dbb772c5e249108f0b191ed17a2c0c
ord-d3765d8579c44d02900e70b0d80879d8
NCC(=O)O>>N[C@@H](CO)C(=O)O
N[C@@H](C)C(=O)O.NCC(=O)O>>N[C@@H](C)C(=O)O.N[C@@H](CO)C(=O)O
[NH2:7][CH2:8][C:9]([OH:10])=[O:12]>>[NH2:7][C@@H:8]([CH2:9][OH:10])[C:11](=[O:12])[OH:13]
NCC(=O)O
N[C@@H](CO)C(=O)O
null
null
null
Miscellaneous
OtherReaction
d54900f1356837c174b3eeb6cbc2b621e135319d6041351be853c1167cd23743
1549656c215892ebd462c7613d543b17758149df09075464e8621349b5d875a1
null
[N;D1;H2:1]-[CH2;D2;+0:2]-[C;H0;D3;+0:3](-[O;D1;H1:4])=[O;H0;D1;+0:5]>>[N;D1;H2:1]-[C@@H;D3;+0:2](-[CH2;D2;+0:3]-[O;D1;H1:4])-[C:6](-[O;D1;H1:7])=[O;H0;D1;+0:5]
null
[]
null
null
null
null
The formation of Z--Ala--SerOH is obtained by the same process as that described in Example 1.a, but using 1.1 mmol of lyophilised hydrated serine in place of cysteine and 1 mmol of alanine protected by Z and activated in place of glycine. Conditions: See reaction.notes.procedure_details.
10.6084/m9.figshare.5104873.v1
null
Carboxylic acid
Carboxylic acid.Primary alcohol
null
null
null
Other
null
null
null
NCC(=O)O>>N[C@@H](CO)C(=O)O
ord_dataset-01dbb772c5e249108f0b191ed17a2c0c
ord-bf52adeae66d476a983fab8d71fb9ecb
NCC(=O)O.N[C@@H](Cc1ccccc1)C(=O)O>>N[C@@H](CO)C(=O)O.N[C@@H](Cc1ccccc1)C(=O)O
N[C@@H](CC1=CC=CC=C1)C(=O)O.NCC(=O)O>>N[C@@H](CC1=CC=CC=C1)C(=O)O.N[C@@H](CO)C(=O)O
[NH2:1][CH2:2][C:5](=[O:4])[OH:7].[cH:3]1[cH:14][cH:13][cH:12][c:11]([CH2:10][C@H:9]([NH2:8])[C:17](=[O:18])[OH:19])[cH:16]1>>[NH2:1][C@@H:2]([CH2:3][OH:4])[C:5](=[O:6])[OH:7].[NH2:8][C@@H:9]([CH2:10][c:11]1[cH:12][cH:13][cH:14][cH:15][cH:16]1)[C:17](=[O:18])[OH:19]
NCC(=O)O.N[C@@H](Cc1ccccc1)C(=O)O
N[C@@H](CO)C(=O)O.N[C@@H](Cc1ccccc1)C(=O)O
null
null
null
Functional Group Addition
OtherReaction
5a66d4356692e54cf9fcd759ba1d12014645afb8472fb23f4af88e0490fc2174
8bef335d6c9b133d83ab31f379ef16b0942b457354d7c276c44766310ad7bc65
c1ccccc1
[C:1]-[c:2]1:[c:3]:[c:4]:[cH;D2;+0:5]:[cH;D2;+0:6]:[cH;D2;+0:7]:1.[N;D1;H2:8]-[CH2;D2;+0:9]-[C;H0;D3;+0:10](-[O;D1;H1:11])=[O;H0;D1;+0:12]>>[C:1]-[c:2]1:[c:3]:[c:4]:[cH;D2;+0:5]:[c:13]:[cH;D2;+0:7]:1.[N;D1;H2:8]-[C@@H;D3;+0:9](-[CH2;D2;+0:6]-[OH;D1;+0:12])-[C;H0;D3;+0:10](=[O;D1;H0:14])-[O;D1;H1:11]
null
[]
null
null
null
null
The formation of t-Boc--Phe--SerOH is obtained by the same process, but using 1.1 mmol of lyophilised hydrated serine in place of cysteine and 1 mmol of phenylalanine protected by t-Box and activated in place of glycine. Conditions: See reaction.notes.procedure_details. Workup: The formation of t-Boc--Phe--SerOH is obt...
10.6084/m9.figshare.5104873.v1
null
Carboxylic acid
Carboxylic acid.Primary alcohol
c1ccccc1
c1ccccc1
c1ccccc1
Other
null
null
null
NCC(=O)O.N[C@@H](Cc1ccccc1)C(=O)O>>N[C@@H](CO)C(=O)O.N[C@@H](Cc1ccccc1)C(=O)O
ord_dataset-01dbb772c5e249108f0b191ed17a2c0c
ord-a1e36e97f3014b5da163378c10482c4e
CO[Si](CCl)(OC)OC.N>>CO[Si](CNC[Si](OC)(OC)OC)(OC)OC
ClC[Si](OC)(OC)OC.N>>CO[Si](OC)(OC)CNC[Si](OC)(OC)OC
Cl[CH2:4][Si:3]([O:2][CH3:1])([O:8][CH3:9])[O:10][CH3:6].[NH3:5]>>[CH3:1][O:2][Si:3]([CH2:4][NH:5][CH2:6][Si:7]([O:8][CH3:9])([O:10][CH3:11])[O:12][CH3:13])([O:14][CH3:15])[O:16][CH3:17]
CO[Si](CCl)(OC)OC.N
CO[Si](CNC[Si](OC)(OC)OC)(OC)OC
null
null
null
Heteroatom Alkylation and Arylation
OtherReaction
1335a9c1e2702a43d3ccb5f36bfc0b3138ddbb4a919a4c95f579ac993d7757c7
373af52b4c18c2e5a54f2808d22ea3932e713b2d052f1f79fd95307522b6ab74
null
Cl-[CH2;D2;+0:1]-[Si;H0;D4;+0:2](-[#8:3]-[C;D1;H3:4])(-[O;H0;D2;+0:5]-[CH3;D1;+0:6])-[O;H0;D2;+0:7]-[C;D1;H3:8].[NH3;D0;+0:9]>>[#8:10]-[#14:11](-[CH2;D2;+0:6]-[NH;D2;+0:9]-[CH2;D2;+0:1]-[Si;H0;D4;+0:2](-[#8:12]-[C;D1;H3:13])(-[#8:14]-[C;D1;H3:15])-[#8:3]-[C;D1;H3:4])(-[O;H0;D2;+0:5]-[C;D1;H3:16])-[O;H0;D2;+0:7]-[C;D1;H...
null
[]
100
CELSIUS
null
null
Chloromethyltrimethoxysilane (50.0 g., 0.29 mole) and ammonia (98.6 g., 5.80 mole) were charged to a 300 ml. stainless steel pressure vessel. The mixture was heated to 100° C. at 800 psi pressure for 8 hours and then cooled. The mixture was filtered. The crude product was distilled at 60° C. and 0.2 mm Hg pressure to p...
10.6084/m9.figshare.5104873.v1
null
Primary halide.Silyl protective group
Secondary amine.Silyl protective group.Silyl protective group
null
null
null
null
null
100
null
CO[Si](CCl)(OC)OC.N>>CO[Si](CNC[Si](OC)(OC)OC)(OC)OC
ord_dataset-01dbb772c5e249108f0b191ed17a2c0c
ord-8f9ba23024a24c68b03865b18a945605
COC(=O)c1cc(N)cc(C(=O)OC)c1.O=C(O)Cc1ccccc1O>>COC(=O)c1cc(N=Nc2ccc(O)c(CC(=O)O)c2)cc(C(=O)OC)c1
[OH-].COC(=O)C1=CC(=CC(=C1)N)C(=O)OC.N(=O)[O-].[Na+].OC1=C(C=CC=C1)CC(=O)O>>COC(=O)C=1C=C(C=C(C1)C(=O)OC)N=NC=1C=CC(=C(C1)CC(=O)O)O
[CH3:1][O:2][C:3](=[O:4])[c:5]1[cH:6][c:7]([NH2:8])[cH:21][c:22]([C:23](=[O:24])[O:25][CH3:26])[cH:27]1.[cH:10]1[cH:11][cH:12][c:13]([OH:14])[c:15]([CH2:16][C:17](=[O:18])[OH:19])[cH:20]1>>[CH3:1][O:2][C:3](=[O:4])[c:5]1[cH:6][c:7]([N:8]=[N:9][c:10]2[cH:11][cH:12][c:13]([OH:14])[c:15]([CH2:16][C:17](=[O:18])[OH:19])[cH...
COC(=O)c1cc(N)cc(C(=O)OC)c1.O=C(O)Cc1ccccc1O
COC(=O)c1cc(N=Nc2ccc(O)c(CC(=O)O)c2)cc(C(=O)OC)c1
null
null
C(C)(=O)O.[OH-].[Na+].Cl.O
Functional Group Addition
OtherReaction
4dfa1e0075917e3f76a2c771d85af2eb7328e8c1dacc2fef053ab9d7871727bb
369e32a405523c63be3b198dc14b1fa8567bb17806d598f8dc85ecca177f9307
c1ccc(N=Nc2ccccc2)cc1
[NH2;D1;+0:1]-[c:2](:[c:3]):[c:4].[c:5]:[c:6]:[cH;D2;+0:7]:[c:8]:[c:9]>>[c:5]:[c:6]:[c;H0;D3;+0:7](-[#7:10]=[N;H0;D2;+0:1]-[c:2](:[c:3]):[c:4]):[c:8]:[c:9]
null
[]
80
CELSIUS
null
null
20.9 g of dimethyl-5-amino-benzene-1,3-dicarboxylate was dissolved in 20 ml of concentrated hydrochloric acid in 200 ml of ice water. The solution was diazotized with 7 g of sodium nitrite dissolved in 30 ml of water. 30.4 g of 2-hydroxy-phenylacetic acid was dissolved in 200 ml of water and 24 g of sodium hydroxide. T...
10.6084/m9.figshare.5104873.v1
null
Primary amine
Diazene
c1ccccc1
c1ccccc1
c1ccccc1.c1ccccc1
Other
C(C)(=O)O.[OH-].[Na+].Cl.O
80
null
COC(=O)c1cc(N)cc(C(=O)OC)c1.O=C(O)Cc1ccccc1O>C(C)(=O)O.[OH-].[Na+].Cl.O>COC(=O)c1cc(N=Nc2ccc(O)c(CC(=O)O)c2)cc(C(=O)OC)c1