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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
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large_stringlengths
1
433
reagent_smiles
large_stringclasses
634 values
catalyst_smiles
large_stringlengths
1
683
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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
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large_stringclasses
3 values
reaction_time_value
float64
0
4k
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large_stringclasses
4 values
procedure_details
large_stringlengths
1
23.6k
reference
large_stringclasses
96 values
doi
large_stringclasses
19 values
functional_groups_reactants
large_stringlengths
3
716
functional_groups_products
large_stringlengths
3
539
participating_rings_reactants
large_stringlengths
5
293
participating_rings_products
large_stringlengths
5
271
all_rings_products
large_stringlengths
5
271
byproduct_smiles
large_stringclasses
176 values
agent_smiles
large_stringlengths
1
712
temperature_c
float64
-230
30.1k
reaction_time_hours
float64
0
2.16k
reaction_smiles_with_agents
large_stringlengths
4
882
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-ae86ad57c04d47c8a8dfe28f32ee4826
CCCCCCCC/C=C\CCCCCCCCOC(=O)CCCCCCC/C=C\CCCCCCCC.CCCCCCCCCCCCCCCCOC(=O)CCCCCC(C)C>>CCCCCCCCCCCCCC(=O)OC(C)C
CCCCCCCCCCCCCCCCOC(=O)CCCCCC(C)C.CCCCCCCC/C=C\CCCCCCCCOC(=O)CCCCCCC/C=C\CCCCCCCC>>C(CCCCCCCCCCCCC)(=O)OC(C)C
CCCCCCCC/C=C\CCCCCCCCOC(=O)CCCCCCC/C=C\[CH2:8][CH2:7][CH2:6][CH2:5][CH2:4][CH2:3][CH2:2][CH3:1].CCCCCCCCCCCCCCCC[O:16][C:14]([CH2:13][CH2:12][CH2:11][CH2:10][CH2:9][CH:17]([CH3:18])[CH3:19])=[O:15]>>[CH3:1][CH2:2][CH2:3][CH2:4][CH2:5][CH2:6][CH2:7][CH2:8][CH2:9][CH2:10][CH2:11][CH2:12][CH2:13][C:14](=[O:15])[O:16][CH:1...
CCCCCCCC/C=C\CCCCCCCCOC(=O)CCCCCCC/C=C\CCCCCCCC.CCCCCCCCCCCCCCCCOC(=O)CCCCCC(C)C
CCCCCCCCCCCCCC(=O)OC(C)C
null
null
null
Heteroatom Alkylation and Arylation
OtherReaction
a88a687c4d6b7d2191008916745139c412c118bff64e3926cf21b76bd4b18ba7
af7b9f47dc4b2fc77b69f8751f8aca252642781fb348457551bd8b9e82cb1ea1
null
C-C-C-C-C-C-C-C-C-C-C-C-C-C-C-C-[O;H0;D2;+0:1]-[C:2](-[C:3])=[O;D1;H0:4].[C:5]-[C:6]-[CH2;D2;+0:7]-[CH;D3;+0:8](-[C;D1;H3:9])-[C;D1;H3:10].C-C-C-C-C-C-C-C/C=C\C-C-C-C-C-C-C-C-O-C(=O)-C-C-C-C-C-C-C/C=C\[CH2;D2;+0:11]-[C:12]-[C:13]>>[C:3]-[C:2](=[O;D1;H0:4])-[O;H0;D2;+0:1]-[CH;D3;+0:8](-[C;D1;H3:9])-[C;D1;H3:10].[C:5]-[C...
null
[]
null
null
null
null
cetearyl isononanoate--"Cetiol SN": 8.00 wt. % Conditions: See reaction.notes.procedure_details.
10.6084/m9.figshare.5104873.v1
null
Ester.Ester
Ester
null
null
null
HO-
null
null
null
CCCCCCCC/C=C\CCCCCCCCOC(=O)CCCCCCC/C=C\CCCCCCCC.CCCCCCCCCCCCCCCCOC(=O)CCCCCC(C)C>>CCCCCCCCCCCCCC(=O)OC(C)C
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-9ee6fa21344a4a619edbde84bc508fb3
O=O>>OO
C1=CC=CC=2C(C3=CC=CC=C3C(C12)=O)=O.C1=CC=C2C(=C1)C(=C3C=CC=CC3=C2O)O.O=O>>OO.C1=CC=CC=2C(C3=CC=CC=C3C(C12)=O)=O
[O:17]=[O:18]>>[OH:17][OH:18]
O=O
OO
null
null
null
Reduction
OtherReaction
481337b1920f4ce3c43b96146b16128e9761a9eff0de2ea6026c9013b690b60c
01b4766905dc763de9fb37374ca31d507f6918d1fb0d42f08e9f4930409e0a42
null
[O;H0;D1;+0:1]=[O;H0;D1;+0:2]>>[OH;D1;+0:1]-[OH;D1;+0:2]
null
[]
null
null
null
null
In all previously known anthraquinone processes, the oxidation reaction and the extraction take place in separate steps, and thus also in separate vessels. The oxidation reaction, in which anthrahydroquinone derivatives react with oxygen, forming hydrogen peroxide and anthraquinone derivatives, takes place in the oxida...
10.6084/m9.figshare.5104873.v1
null
null
Peroxide
null
null
null
null
null
null
null
O=O>>OO
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-169f88b27a294c15b3d94e8de0e682c6
CC(C)CCC[C@@H](C)[C@H]1CC[C@H]2[C@@H]3CC=C4C[C@@H](O)CC[C@]4(C)[C@H]3CC[C@]12C.O=C(Cl)OCCl>>CC(C)CCC[C@@H](C)[C@H]1CC[C@H]2[C@@H]3CC=C4C[C@](O)(C(=O)OCCl)CC[C@]4(C)[C@H]3CC[C@]12C
ClC(=O)OCCl.CC(C)CCC[C@@H](C)[C@H]1CC[C@H]2[C@@H]3CC=C4C[C@@H](O)CC[C@]4(C)[C@H]3CC[C@]12C.N1=CC=CC=C1>>ClCOC(=O)[C@]1(CC2=CC[C@H]3[C@@H]4CC[C@H]([C@@H](CCCC(C)C)C)[C@]4(CC[C@@H]3[C@]2(CC1)C)C)O
[CH3:1][CH:2]([CH3:3])[CH2:4][CH2:5][CH2:6][C@@H:7]([CH3:8])[C@H:9]1[CH2:10][CH2:11][C@H:12]2[C@@H:13]3[CH2:14][CH:15]=[C:16]4[CH2:17][C@@H:18]([OH:19])[CH2:25][CH2:26][C@:27]4([CH3:28])[C@H:29]3[CH2:30][CH2:31][C@:32]12[CH3:33].Cl[C:20](=[O:21])[O:22][CH2:23][Cl:24]>>[CH3:1][CH:2]([CH3:3])[CH2:4][CH2:5][CH2:6][C@@H:7]...
CC(C)CCC[C@@H](C)[C@H]1CC[C@H]2[C@@H]3CC=C4C[C@@H](O)CC[C@]4(C)[C@H]3CC[C@]12C.O=C(Cl)OCCl
CC(C)CCC[C@@H](C)[C@H]1CC[C@H]2[C@@H]3CC=C4C[C@](O)(C(=O)OCCl)CC[C@]4(C)[C@H]3CC[C@]12C
null
null
C(Cl)Cl
C-C Coupling
OtherReaction
aeb38539b78d1cb51ddf6ba8c84f52c066d749acbc417d09c81bbf5280e7810c
1249787e3342b915074ab435f92ce681110465e50fefb3d2a861019702951273
C1=C2CCCCC2[C@H]2CCC3CCC[C@H]3[C@@H]2C1
Cl-[C;H0;D3;+0:1](=[O;D1;H0:2])-[#8:3]-[C:4].[C:5]-[C:6]=[C:7]1-[C:8]-[C@@H;D3;+0:9](-[O;D1;H1:10])-[C:11]-[C:12]-[C:13]-1>>[C:5]-[C:6]=[C:7]1-[C:8]-[C@;H0;D4;+0:9](-[O;D1;H1:10])(-[C;H0;D3;+0:1](=[O;D1;H0:2])-[#8:3]-[C:4])-[C:11]-[C:12]-[C:13]-1
null
[]
null
null
24
HOUR
Chloromethyl chloroformate (1.96 g, 15.2 mmol) and cholesterol (5.0 g, 12.9 mmol) was dissolved in CH2Cl2 (10 ml). The solution was cooled. Pyridine (1.21 g, 15.3 mmol) was dripped into the stirred solution over 5 minutes. Heat was produced and the reaction gave a clear solution from a somewhat unclear starting solutio...
10.6084/m9.figshare.5104873.v1
null
Acyl halide.Ether.Secondary alcohol
Ester
C1=C2CCCC[C@@H]2[C@H]2CC[C@@H]3CCC[C@H]3[C@@H]2C1
C1=C2CCCC[C@@H]2[C@H]2CC[C@@H]3CCC[C@H]3[C@@H]2C1
C1=C2CCCC[C@@H]2[C@H]2CC[C@@H]3CCC[C@H]3[C@@H]2C1
HCl
C(Cl)Cl
null
24
CC(C)CCC[C@@H](C)[C@H]1CC[C@H]2[C@@H]3CC=C4C[C@@H](O)CC[C@]4(C)[C@H]3CC[C@]12C.O=C(Cl)OCCl>C(Cl)Cl>CC(C)CCC[C@@H](C)[C@H]1CC[C@H]2[C@@H]3CC=C4C[C@](O)(C(=O)OCCl)CC[C@]4(C)[C@H]3CC[C@]12C
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-c2c590b87f0c4656985c4433af338c9a
CC(O)C(=O)O.NCCN>>CC(O)C(=O)NCCNC(=O)C(C)O
C(C(O)C)(=O)O.C(CN)N>>C(CNC(C(O)C)=O)NC(C(O)C)=O
[CH3:1][CH:2]([OH:3])[C:4](=[O:5])[OH:14].[NH2:6][CH2:7][CH2:10][NH2:9]>>[CH3:1][CH:2]([OH:3])[C:4](=[O:5])[NH:6][CH2:7][CH2:8][NH:9][C:10](=[O:11])[CH:12]([CH3:13])[OH:14]
CC(O)C(=O)O.NCCN
CC(O)C(=O)NCCNC(=O)C(C)O
null
null
O
Functional Group Addition
OtherReaction
00fca04d09ae4e202c1fb99d5176ffe098e918f6bb44002a85fd613a55e3c079
cb4f7707bc4c167a5a17a3069fdab173022aff6b0194447ac4f1de103681f576
null
[C;D1;H3:1]-[C:2](-[O;D1;H1:3])-[C;H0;D3;+0:4](=[O;D1;H0:5])-[OH;D1;+0:6].[NH2;D1;+0:7]-[CH2;D2;+0:8]-[CH2;D2;+0:9]-[NH2;D1;+0:10]>>[C;D1;H3:11]-[C:12](-[OH;D1;+0:6])-[C;H0;D3;+0:9](=[O;D1;H0:13])-[NH;D2;+0:10]-[C:14]-[CH2;D2;+0:8]-[NH;D2;+0:7]-[C;H0;D3;+0:4](=[O;D1;H0:5])-[C:2](-[C;D1;H3:1])-[O;D1;H1:3]
null
[]
125
CELSIUS
null
null
Lactic acid (441 g; 4.90 moles) was placed in a reaction flask equipped with a distillation head. Under a nitrogen atmosphere, ethylene diamine (147 g; 2.45 moles) was slowly added with stirring to the reaction flask. During the course of the addition, the reaction mixture turned a deep orange and the temperature reach...
10.6084/m9.figshare.5104873.v1
null
Carboxylic acid.Primary amine.Primary amine
Secondary amide.Secondary amide.Secondary alcohol
null
null
null
Other
O
125
null
CC(O)C(=O)O.NCCN>O>CC(O)C(=O)NCCNC(=O)C(C)O
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-82348284bdb74ce681d8c47598cef413
C[C@H](O)C(=O)O>>CC(O)C(=O)O
C([C@@H](O)C)(=O)O.C(C)(=O)OC(C)=O.CCCCC(C(=O)O)O>>C(C(O)C)(=O)O.OC(C(=O)O)CCCC
[CH3:1][C@H:2]([OH:3])[C:4](=[O:5])[OH:6]>>[CH3:1][CH:2]([OH:3])[C:4](=[O:5])[OH:6]
C[C@H](O)C(=O)O
CC(O)C(=O)O
null
null
O
Miscellaneous
OtherReaction
40ba59785861b8226ce5af6bdcbb9a37f0ff50a8c7ec7d4fc4c524cf906cc65c
56ebed4a8b3cebec83c37a71d68f0c87d1e404ab05a9ce792691e4e18a2379dd
null
null
null
[]
140
CELSIUS
null
null
DL-2-Hydroxycaproic acid (1.00 g, 0.0076 moles), and L-lactic acid (4.5 g of a nominally 85% solution in water; 0.043 moles) were placed in a reaction flask equipped with a distillation head and mechanical stirrer. The flask was heated at 110° C. for 6 hours under low vacuum (aspirator) while water was removed. The tem...
10.6084/m9.figshare.5104873.v1
null
null
null
null
null
null
null
O
140
null
C[C@H](O)C(=O)O>O>CC(O)C(=O)O
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-727bc53cc8974a99824d9f77e8ab9fbc
C[C@@H]1OC(=O)[C@H](C)OC1=O>>CC(O)C(=O)O
C1(OCCCO1)=O.C(C)(=O)OC(C)=O.C[C@H]1C(=O)O[C@H](C(=O)O1)C.C1(OCCCO1)=O>>C1(OCCCO1)=O.C(C(O)C)(=O)O
C[C@H]1C(=O)[O:3][C@@H:2]([CH3:1])[C:4](=[O:5])[O:6]1>>[CH3:1][CH:2]([OH:3])[C:4](=[O:5])[OH:6]
C[C@@H]1OC(=O)[C@H](C)OC1=O
CC(O)C(=O)O
null
null
O
Reduction
Hydrolysis or Hydrogenolysis of Carboxylic Esters or Thioesters
3a489c9d1f763ca159b2b2953b45f7bfd439527fe0106b00d52bb92835ce9f92
7a1e672e57a6fb97b76aed5dc00cfd545732476349440fff57203dca5fb97d59
null
C-[C@@H]1-[O;H0;D2;+0:1]-[C:2](=[O;D1;H0:3])-[C@H;D3;+0:4](-[C;D1;H3:5])-[O;H0;D2;+0:6]-C-1=O>>[C;D1;H3:5]-[CH;D3;+0:4](-[OH;D1;+0:6])-[C:2](=[O;D1;H0:3])-[OH;D1;+0:1]
null
[]
80
CELSIUS
8
HOUR
L-Lactide (85.07 g; 0.945 moles) and water (100 mL; millipore) were placed in a 1 L 3-neck flask equipped with a mechanical stirrer, distillation head, and a thermometer. The reaction mixture was warmed to 80° C. and stirred under nitrogen overnight. The flask was then placed under vacuum (aspirator, 7 mmHg) and the te...
10.6084/m9.figshare.5104873.v1
null
Ester.Ester
Carboxylic acid.Secondary alcohol
C1COCCO1
null
null
HO-
O
80
8
C[C@@H]1OC(=O)[C@H](C)OC1=O>O>CC(O)C(=O)O
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-ec5852a39378408dbba1f53767eea48c
O=C(O)c1ccc2cc(O)ccc2c1>>O=C(O)c1ccc2c(c1)CCC(O)C2
OC=1C=C2C=CC(=CC2=CC1)C(=O)O.[H][H]>>OC1CC=2C=CC(=CC2CC1)C(=O)O
[O:1]=[C:2]([OH:3])[c:4]1[cH:5][cH:6][c:7]2[c:8]([cH:9]1)[cH:10][cH:11][c:12]([OH:13])[cH:14]2>>[O:1]=[C:2]([OH:3])[c:4]1[cH:5][cH:6][c:7]2[c:8]([cH:9]1)[CH2:10][CH2:11][CH:12]([OH:13])[CH2:14]2
O=C(O)c1ccc2cc(O)ccc2c1
O=C(O)c1ccc2c(c1)CCC(O)C2
null
[Pd]
O1CCCC1
Reduction
OtherReaction
791f5dc0669dd17ea9d12becd21433c9c87a57cda3d5cbebc67920e409dc10b6
ba6b55202ce8b357d547127b1fb6b7db62ba05b17f20b87243fcfcd8077ff42b
c1ccc2c(c1)CCCC2
[O;D1;H1:1]-[c;H0;D3;+0:2]1:[cH;D2;+0:3]:[cH;D2;+0:4]:[c:5](:[c:6]):[c:7](:[c:8]):[cH;D2;+0:9]:1>>[O;D1;H1:1]-[CH;D3;+0:2]1-[CH2;D2;+0:3]-[CH2;D2;+0:4]-[c:5](:[c:6]):[c:7](:[c:8])-[CH2;D2;+0:9]-1
null
[]
null
null
null
null
For example, 6-hydroxynaphthalene-2-carboxylic acid in a solvent such as tetrahydrofuran is reduced with hydrogen gas in the presence of a reducing catalyst such as a palladium/carbon under elevated pressure to obtain 5,6,7,8-tetrahydro-6-hydroxynaphthalene-2-carboxylic acid (1). Conditions: See reaction.notes.procedur...
10.6084/m9.figshare.5104873.v1
null
Aromatic alcohol
Secondary alcohol
c1ccc2ccccc2c1
c1ccc2c(c1)CCCC2
c1ccc2c(c1)CCCC2
null
[Pd].O1CCCC1
null
null
O=C(O)c1ccc2cc(O)ccc2c1>[Pd].O1CCCC1>O=C(O)c1ccc2c(c1)CCC(O)C2
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-eac9be152119468d80a973981c8b50e8
BrCc1ccccc1.O=C(O)C1CCc2cc(O)ccc2C1>>O=C(O)C1CCc2cc(OCc3ccccc3)ccc2C1
OC=1C=C2CCC(CC2=CC1)C(=O)O.C(C1=CC=CC=C1)Br.[OH-].[K+]>>C(C1=CC=CC=C1)OC=1C=C2CCC(CC2=CC1)C(=O)O
Br[CH2:11][c:12]1[cH:13][cH:14][cH:15][cH:16][cH:17]1.[O:1]=[C:2]([OH:3])[CH:4]1[CH2:5][CH2:6][c:7]2[cH:8][c:9]([OH:10])[cH:18][cH:19][c:20]2[CH2:21]1>>[O:1]=[C:2]([OH:3])[CH:4]1[CH2:5][CH2:6][c:7]2[cH:8][c:9]([O:10][CH2:11][c:12]3[cH:13][cH:14][cH:15][cH:16][cH:17]3)[cH:18][cH:19][c:20]2[CH2:21]1
BrCc1ccccc1.O=C(O)C1CCc2cc(O)ccc2C1
O=C(O)C1CCc2cc(OCc3ccccc3)ccc2C1
null
null
null
Heteroatom Alkylation and Arylation
Williamson Ether Synthesis
7e1040116e3a4cf0e8ec5cc7865388d9cd0efabce6d320a1c25a36e411018d8b
d5f4610d46ccc0478471c5bc0fb862644eaf764bbc5d93badb39d54f6ec8e0a5
c1ccc(COc2ccc3c(c2)CCCC3)cc1
Br-[CH2;D2;+0:1]-[c:2](:[c:3]):[c:4].[OH;D1;+0:5]-[c:6](:[c:7]):[c:8]>>[c:3]:[c:2](-[CH2;D2;+0:1]-[O;H0;D2;+0:5]-[c:6](:[c:7]):[c:8]):[c:4]
null
[]
null
null
null
null
The 1,2,3,4-tetrahydro-6-hydroxynaphthalene-2-carboxylic acid obtained in the above manner is reacted with benzyl bromide in the presence of potassium hydroxide to obtain 1,2,3,4-tetrahydro-6-benzyloxynaphthalene-2-carboxylic acid (11). Conditions: See reaction.notes.procedure_details.
10.6084/m9.figshare.5104873.v1
null
Primary halide.Aromatic alcohol
Ether
null
null
c1ccc2c(c1)CCCC2.c1ccccc1
HBr
null
null
null
BrCc1ccccc1.O=C(O)C1CCc2cc(O)ccc2C1>>O=C(O)C1CCc2cc(OCc3ccccc3)ccc2C1
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-e36c9a7b969845f3b2fcc8a9dfe44e3f
COC(=O)c1ccc2cc(C=O)ccc2c1>>COC(=O)c1ccc2ccccc2c1
[H][H].C1(=CC=CC=C1)[PH+](C1=CC=CC=C1)C1=CC=CC=C1.COC(=O)C1=CC2=CC=C(C=C2C=C1)C=O.C(Cl)Cl>>COC(=O)C1=CC2=CC=CC=C2C=C1
O=C[c:10]1[cH:9][c:8]2[cH:7][cH:6][c:5]([C:3]([O:2][CH3:1])=[O:4])[cH:14][c:13]2[cH:12][cH:11]1>>[CH3:1][O:2][C:3](=[O:4])[c:5]1[cH:6][cH:7][c:8]2[cH:9][cH:10][cH:11][cH:12][c:13]2[cH:14]1
COC(=O)c1ccc2cc(C=O)ccc2c1
COC(=O)c1ccc2ccccc2c1
null
null
O1CCCC1
Reduction
OtherReaction
e1944dcc31e48b78b2e6da09b819a00b5aec3596b56a43ea4c014a16775d2ab4
9b627af1c37cea795d25b24c8b755865edc79a56af73aa7fa1348903b24aee3f
c1ccc2ccccc2c1
O=C-[c;H0;D3;+0:1](:[c:2]:[c:3]):[c:4]:[c:5]>>[c:3]:[c:2]:[cH;D2;+0:1]:[c:4]:[c:5]
null
[]
null
null
null
null
For example, 4'-alkoxy-4-bromobiphenyl (17) is reacted with triphenylphosphin to obtain triphenylphosphonium salt of 4'-alkoxybiphenyl (21). The thus obtained triphenylphosphonium salt of 4'-alkoxybiphenyl (21) is reacted with 6-formyl-2-naphthalenecarboxylic acid methyl ester as a solution in such as methylene chlorid...
10.6084/m9.figshare.5104873.v1
null
Aldehyde
null
c1ccc2ccccc2c1
c1ccc2ccccc2c1
c1ccc2ccccc2c1
Other
O1CCCC1
null
null
COC(=O)c1ccc2cc(C=O)ccc2c1>O1CCCC1>COC(=O)c1ccc2ccccc2c1
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-bf36940ac45c47b1a49e30e635325cb5
O=C(O)c1ccc2ccccc2c1>>O=C(O)C1CCc2ccccc2C1
C1=C(C=CC2=CC=CC=C12)C(=O)O.[Na].C(C)OCCOCC>>C1C(CCC2=CC=CC=C12)C(=O)O
[O:1]=[C:2]([OH:3])[c:4]1[cH:5][cH:6][c:7]2[cH:8][cH:9][cH:10][cH:11][c:12]2[cH:13]1>>[O:1]=[C:2]([OH:3])[CH:4]1[CH2:5][CH2:6][c:7]2[cH:8][cH:9][cH:10][cH:11][c:12]2[CH2:13]1
O=C(O)c1ccc2ccccc2c1
O=C(O)C1CCc2ccccc2C1
null
null
null
Reduction
OtherReaction
4b04a19698815acedc04e64dd177c258cb21c55a1d5303acb9d39585e91e8242
312e9350dcad67590617294c0eb017edf0b9fbfe6133c06a3f393b871a889092
c1ccc2c(c1)CCCC2
[O;D1;H0:1]=[C:2](-[O;D1;H1:3])-[c;H0;D3;+0:4]1:[cH;D2;+0:5]:[c:6](:[c:7]):[c:8](:[c:9]):[cH;D2;+0:10]:[cH;D2;+0:11]:1>>[O;D1;H0:1]=[C:2](-[O;D1;H1:3])-[CH;D3;+0:4]1-[CH2;D2;+0:5]-[c:6](:[c:7]):[c:8](:[c:9])-[CH2;D2;+0:10]-[CH2;D2;+0:11]-1
null
[]
null
null
null
null
The thus obtained 6-[4'-alkoxy-4-biphenyl)ethyl]-2-naphthalenecarboxylic acid (22) is hydrogenated in the presence of metal sodium in a solvent such as 1,2-diethoxyethane to obtain 6-[4'-alkoxy-4-biphenyl)ethyl]-1,2,3,4-tetrahydro-2-naphthalenecarboxylic acid (23). Finally, the resulting 6-[4'-alkoxy-4-biphenyl)ethyl]-...
10.6084/m9.figshare.5104873.v1
null
null
null
c1ccc2ccccc2c1
c1ccc2c(c1)CCCC2
c1ccc2c(c1)CCCC2
null
null
null
null
O=C(O)c1ccc2ccccc2c1>>O=C(O)C1CCc2ccccc2C1
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-7d2c74c555f047899e0fbc54d1163d31
BrCc1ccccc1.O=C(O)C1CCc2cc(O)ccc2C1>>O=C(O)C1CCc2cc(OCc3ccccc3)ccc2C1
[OH-].[K+].OC=1C=C2CCC(CC2=CC1)C(=O)O.C(C1=CC=CC=C1)Br.[OH-].[K+].Cl>>C(C1=CC=CC=C1)OC=1C=C2CCC(CC2=CC1)C(=O)O
Br[CH2:11][c:12]1[cH:13][cH:14][cH:15][cH:16][cH:17]1.[O:1]=[C:2]([OH:3])[CH:4]1[CH2:5][CH2:6][c:7]2[cH:8][c:9]([OH:10])[cH:18][cH:19][c:20]2[CH2:21]1>>[O:1]=[C:2]([OH:3])[CH:4]1[CH2:5][CH2:6][c:7]2[cH:8][c:9]([O:10][CH2:11][c:12]3[cH:13][cH:14][cH:15][cH:16][cH:17]3)[cH:18][cH:19][c:20]2[CH2:21]1
BrCc1ccccc1.O=C(O)C1CCc2cc(O)ccc2C1
O=C(O)C1CCc2cc(OCc3ccccc3)ccc2C1
null
[I-].[Na+]
C(C)O.O
Heteroatom Alkylation and Arylation
Williamson Ether Synthesis
7e1040116e3a4cf0e8ec5cc7865388d9cd0efabce6d320a1c25a36e411018d8b
d5f4610d46ccc0478471c5bc0fb862644eaf764bbc5d93badb39d54f6ec8e0a5
c1ccc(COc2ccc3c(c2)CCCC3)cc1
Br-[CH2;D2;+0:1]-[c:2](:[c:3]):[c:4].[OH;D1;+0:5]-[c:6](:[c:7]):[c:8]>>[c:3]:[c:2](-[CH2;D2;+0:1]-[O;H0;D2;+0:5]-[c:6](:[c:7]):[c:8]):[c:4]
92.8
[{"value": 92.8, "product": "C(C1=CC=CC=C1)OC=1C=C2CCC(CC2=CC1)C(=O)O", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
100
CELSIUS
null
null
A mixture of 10.60 g (50 mmol) of 1,2,3,4-tetrahydro-6-hydroxynaphthalene-2-carboxylic acid, 12.85 g (75 mmol) of benzyl bromide, 6.6 g (100 mmol) of 85% potassium hydroxide, 0.525 g (3.5 mmol) of sodium iodide, 200 ml of ethanol and 25 ml of distilled water was heated under reflux at 100° C. for 12 hours. To this reac...
10.6084/m9.figshare.5104873.v1
null
Primary halide.Aromatic alcohol
Ether
null
null
c1ccc2c(c1)CCCC2.c1ccccc1
HBr
[I-].[Na+].C(C)O.O
100
null
BrCc1ccccc1.O=C(O)C1CCc2cc(O)ccc2C1>[I-].[Na+].C(C)O.O>O=C(O)C1CCc2cc(OCc3ccccc3)ccc2C1
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-ccd7d3bc80234865b14e3c2556c0baf6
CCCCCCCCCCOc1ccc(C(=O)OC2CCc3cc(C(=O)OCc4ccccc4)ccc3C2)cc1>>CCCCCCCCCCOc1ccc(C(=O)OC2CCc3cc(C(=O)O)ccc3C2)cc1
[H][H].C(C1=CC=CC=C1)OC(=O)C1=CC=2CCC(CC2C=C1)OC(C1=CC=C(C=C1)OCCCCCCCCCC)=O>>C(CCCCCCCCC)OC1=CC=C(C(=O)OC2CC=3C=CC(=CC3CC2)C(=O)O)C=C1
c1ccc(C[O:27][C:25]([c:24]2[cH:23][c:22]3[c:30]([cH:29][cH:28]2)[CH2:31][CH:19]([O:18][C:16]([c:15]2[cH:14][cH:13][c:12]([O:11][CH2:10][CH2:9][CH2:8][CH2:7][CH2:6][CH2:5][CH2:4][CH2:3][CH2:2][CH3:1])[cH:33][cH:32]2)=[O:17])[CH2:20][CH2:21]3)=[O:26])cc1>>[CH3:1][CH2:2][CH2:3][CH2:4][CH2:5][CH2:6][CH2:7][CH2:8][CH2:9][CH...
CCCCCCCCCCOc1ccc(C(=O)OC2CCc3cc(C(=O)OCc4ccccc4)ccc3C2)cc1
CCCCCCCCCCOc1ccc(C(=O)OC2CCc3cc(C(=O)O)ccc3C2)cc1
null
[Pd]
O1CCCC1
Deprotection
Ester saponification (alkyl deprotection)
86a971d3e4f88009ab4c98512e9f1deb51b2f0ce5cbd068cc61ae878c1e58e2a
38ae1ee78433b9acfb0390501446149c80f88f23ac2d84c60b3369bdab75cec9
O=C(OC1CCc2ccccc2C1)c1ccccc1
[O;D1;H0:1]=[C:2](-[c:3])-[O;H0;D2;+0:4]-C-c1:c:c:c:c:c:1>>[O;D1;H0:1]=[C:2](-[OH;D1;+0:4])-[c:3]
93
[{"value": 93.0, "product": "C(CCCCCCCCC)OC1=CC=C(C(=O)OC2CC=3C=CC(=CC3CC2)C(=O)O)C=C1", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
15
HOUR
Hydrogen gas was blown into a mixture of 0.53 g (1.0 mmol) of 6-(4'-decyloxybenzoyloxy)-5,6,7,8-tetrahydronaphthalene-2-carboxylic acid benzyl ester, 0.11 g of 5% palladium/carbon and 10 ml of tetrahydrofuran with stirring at room temperature and ordinary pressure for 15 hours. The reaction mixture was filtered using C...
10.6084/m9.figshare.5104873.v1
null
Ester
Carboxylic acid
c1ccccc1
null
c1ccccc1.c1ccc2c(c1)CCCC2
Other
[Pd].O1CCCC1
null
15
CCCCCCCCCCOc1ccc(C(=O)OC2CCc3cc(C(=O)OCc4ccccc4)ccc3C2)cc1>[Pd].O1CCCC1>CCCCCCCCCCOc1ccc(C(=O)OC2CCc3cc(C(=O)O)ccc3C2)cc1
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-528cd02b7f3644e7b8e580a1f266c8a1
CCCCCCCCCCOc1ccc2cc(C(=O)O)ccc2c1>>O=C(O)C1CCc2cc(O)ccc2C1
C(CCCCCCCCC)OC=1C=C2C=CC(=CC2=CC1)C(=O)O.Br>>OC=1C=C2CCC(CC2=CC1)C(=O)O
CCCCCCCCCC[O:10][c:9]1[cH:8][c:7]2[cH:6][cH:5][c:4]([C:2](=[O:1])[OH:3])[cH:14][c:13]2[cH:12][cH:11]1>>[O:1]=[C:2]([OH:3])[CH:4]1[CH2:5][CH2:6][c:7]2[cH:8][c:9]([OH:10])[cH:11][cH:12][c:13]2[CH2:14]1
CCCCCCCCCCOc1ccc2cc(C(=O)O)ccc2c1
O=C(O)C1CCc2cc(O)ccc2C1
null
null
C(C)(=O)O
Deprotection
OtherReaction
9479f30b52fd035c72fa7a3953555c10329ae405ac42eb806833d1ea5b6b2ffe
26a36596df80ec137b0e8087297418351c93c32819177f680675220622f215d4
c1ccc2c(c1)CCCC2
C-C-C-C-C-C-C-C-C-C-[O;H0;D2;+0:1]-[c:2]1:[c:3]:[c:4]:[c:5]2:[cH;D2;+0:6]:[c;H0;D3;+0:7](-[C:8](=[O;D1;H0:9])-[O;D1;H1:10]):[cH;D2;+0:11]:[cH;D2;+0:12]:[c:13]:2:[c:14]:1>>[O;D1;H0:9]=[C:8](-[O;D1;H1:10])-[CH;D3;+0:7]1-[CH2;D2;+0:6]-[c:5]2:[c:4]:[c:3]:[c:2](-[OH;D1;+0:1]):[c:14]:[c:13]:2-[CH2;D2;+0:12]-[CH2;D2;+0:11]-1
100
[{"value": 100.0, "product": "OC=1C=C2CCC(CC2=CC1)C(=O)O", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
null
null
16.6 g (50 mmol) of the 6-decyloxynaphthalene-2-carboxylic acid obtained in the first stage was heated under reflux at 130° C. for 7 hours in the presence of 250 cc of acetic acid and 86.5 g (0.5 mol) of 47% hydrobromic acid. To the reaction mixture was added distilled water, and then the resulting mixture was concentr...
10.6084/m9.figshare.5104873.v1
null
Ether
Aromatic alcohol
c1ccc2ccccc2c1
c1ccc2c(c1)CCCC2
c1ccc2c(c1)CCCC2
Other
C(C)(=O)O
null
null
CCCCCCCCCCOc1ccc2cc(C(=O)O)ccc2c1>C(C)(=O)O>O=C(O)C1CCc2cc(O)ccc2C1
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-0396fca3395e4ebeb8f2c15f2dea83c8
CCCCCCCCCCBr.O=C(O)c1ccc(-c2ccc(O)cc2)cc1>>CCCCCCCCCCOc1ccc(-c2ccc(C(=O)O)cc2)cc1
Cl.OC1=CC=C(C=C1)C1=CC=C(C=C1)C(=O)O.C(CCCCCCCCC)Br.[OH-].[K+].[I-].[Na+].[OH-].[K+]>>C(CCCCCCCCC)OC1=CC=C(C=C1)C1=CC=C(C=C1)C(=O)O
Br[CH2:10][CH2:9][CH2:8][CH2:7][CH2:6][CH2:5][CH2:4][CH2:3][CH2:2][CH3:1].[OH:11][c:12]1[cH:13][cH:14][c:15](-[c:16]2[cH:17][cH:18][c:19]([C:20](=[O:21])[OH:22])[cH:23][cH:24]2)[cH:25][cH:26]1>>[CH3:1][CH2:2][CH2:3][CH2:4][CH2:5][CH2:6][CH2:7][CH2:8][CH2:9][CH2:10][O:11][c:12]1[cH:13][cH:14][c:15](-[c:16]2[cH:17][cH:18...
CCCCCCCCCCBr.O=C(O)c1ccc(-c2ccc(O)cc2)cc1
CCCCCCCCCCOc1ccc(-c2ccc(C(=O)O)cc2)cc1
null
null
C(C)O.O
Heteroatom Alkylation and Arylation
Williamson Ether Synthesis
7e1040116e3a4cf0e8ec5cc7865388d9cd0efabce6d320a1c25a36e411018d8b
d5f4610d46ccc0478471c5bc0fb862644eaf764bbc5d93badb39d54f6ec8e0a5
c1ccc(-c2ccccc2)cc1
Br-[CH2;D2;+0:1]-[C:2]-[C:3].[OH;D1;+0:4]-[c:5](:[c:6]):[c:7]>>[C:3]-[C:2]-[CH2;D2;+0:1]-[O;H0;D2;+0:4]-[c:5](:[c:6]):[c:7]
6
[{"value": 6.0, "product": "C(CCCCCCCCC)OC1=CC=C(C=C1)C1=CC=C(C=C1)C(=O)O", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
100
CELSIUS
null
null
A mixture of 21.4 g (0.1 mol) of 4'-hydroxybiphenyl-4-carboxylic acid, 33.15 g (0.15 mol) of n-decyl bromide, 13.20 g (0.2 mol) of 85% potassium hydroxide, 1.05 g (7 mmol) of sodium iodide, 500 ml of ethanol and 100 ml of distilled water was heated under reflux at 100° C. for 12 hours. After 40 ml of 25% potassium hydr...
10.6084/m9.figshare.5104873.v1
null
Primary halide.Aromatic alcohol
Ether
null
null
c1ccccc1.c1ccccc1
HBr
C(C)O.O
100
null
CCCCCCCCCCBr.O=C(O)c1ccc(-c2ccc(O)cc2)cc1>C(C)O.O>CCCCCCCCCCOc1ccc(-c2ccc(C(=O)O)cc2)cc1
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-1973f4fcc3e34d7aab97de56c9a9b263
CCCCCC[C@@H](OC(=O)C1CCc2cc(OCc3ccccc3)ccc2C1)C(F)(F)F>>CCCCCC[C@@H](OC(=O)C1CCc2cc(O)ccc2C1)C(F)(F)F
[H][H].FC([C@@H](CCCCCC)OC(=O)C1CC2=CC=C(C=C2CC1)OCC1=CC=CC=C1)(F)F>>FC([C@@H](CCCCCC)OC(=O)C1CC2=CC=C(C=C2CC1)O)(F)F
c1ccc(C[O:17][c:16]2[cH:15][c:14]3[c:20]([cH:19][cH:18]2)[CH2:21][CH:11]([C:9]([O:8][C@H:7]([CH2:6][CH2:5][CH2:4][CH2:3][CH2:2][CH3:1])[C:22]([F:23])([F:24])[F:25])=[O:10])[CH2:12][CH2:13]3)cc1>>[CH3:1][CH2:2][CH2:3][CH2:4][CH2:5][CH2:6][C@@H:7]([O:8][C:9](=[O:10])[CH:11]1[CH2:12][CH2:13][c:14]2[cH:15][c:16]([OH:17])[c...
CCCCCC[C@@H](OC(=O)C1CCc2cc(OCc3ccccc3)ccc2C1)C(F)(F)F
CCCCCC[C@@H](OC(=O)C1CCc2cc(O)ccc2C1)C(F)(F)F
null
[Pd]
O1CCCC1
Deprotection
Hydroxyl benzyl deprotection
36869d1fe85185a14d9eb30bf05178c600a9b6eca277ffaf3803578c30e0bf5d
26a36596df80ec137b0e8087297418351c93c32819177f680675220622f215d4
c1ccc2c(c1)CCCC2
[c:1]:[c:2](-[O;H0;D2;+0:3]-C-c1:c:c:c:c:c:1):[c:4]>>[OH;D1;+0:3]-[c:2](:[c:1]):[c:4]
100
[{"value": 100.0, "product": "FC([C@@H](CCCCCC)OC(=O)C1CC2=CC=C(C=C2CC1)O)(F)F", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
24
HOUR
Hydrogen gas was blown into a mixture of 8.19 g (18.3 mmol) of the 1,2,3,4-tetrahydro-6-benzyloxynaphthalene-2-carboxylic acid (R)-1-trifluoromethylheptyl ester obtained in the fourth stage, 3.6 g of 5% palladium/carbon as a catalyst and 50 ml of tetrahydrofuran with stirring at room temperature and ordinary pressure f...
10.6084/m9.figshare.5104873.v1
null
Ether
Aromatic alcohol
c1ccccc1
null
c1ccc2c(c1)CCCC2
Other
[Pd].O1CCCC1
null
24
CCCCCC[C@@H](OC(=O)C1CCc2cc(OCc3ccccc3)ccc2C1)C(F)(F)F>[Pd].O1CCCC1>CCCCCC[C@@H](OC(=O)C1CCc2cc(O)ccc2C1)C(F)(F)F
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-a8ec9300a50c487a97fd5c9549637998
CCCCCCCCc1ccc(-c2ccc(C(=O)O)cc2)cc1.CCCCCC[C@@H](C)OC(=O)C1CCc2cc(O)ccc2C1>>CCCCCCCCc1ccc(-c2ccccc2C(=O)Oc2ccc3c(c2)CCC(C(=O)O[C@H](C)CCCCCC)C3)cc1
C[C@H](CCCCCC)OC(=O)C1CC2=CC=C(C=C2CC1)O.C1(CCCCC1)N=C=NC1CCCCC1.C(CCCCCCC)C1=CC=C(C=C1)C1=CC=C(C=C1)C(=O)O.FC([C@@H](CCCCCC)O)(F)F>>C[C@H](CCCCCC)OC(=O)C1CC2=CC=C(C=C2CC1)OC(=O)C=1C(=CC=CC1)C1=CC=C(C=C1)CCCCCCCC
O[C:19]([c:18]1[cH:15][cH:14][c:13](-[c:12]2[cH:11][cH:10][c:9]([CH2:8][CH2:7][CH2:6][CH2:5][CH2:4][CH2:3][CH2:2][CH3:1])[cH:44][cH:43]2)[cH:16][cH:17]1)=[O:20].[OH:21][c:22]1[cH:23][cH:24][c:25]2[c:26]([cH:27]1)[CH2:28][CH2:29][CH:30]([C:31](=[O:32])[O:33][C@H:34]([CH3:35])[CH2:36][CH2:37][CH2:38][CH2:39][CH2:40][CH3:...
CCCCCCCCc1ccc(-c2ccc(C(=O)O)cc2)cc1.CCCCCC[C@@H](C)OC(=O)C1CCc2cc(O)ccc2C1
CCCCCCCCc1ccc(-c2ccccc2C(=O)Oc2ccc3c(c2)CCC(C(=O)O[C@H](C)CCCCCC)C3)cc1
null
null
C(Cl)Cl
Acylation
OtherReaction
a6f963d149e8dd87f63c5bb958cffa4c95c2af472825d9145489a37ba75220bb
1489fe0065c6531b60fda87a3857d7da1cd21873868856f058c20706f927fa08
O=C(Oc1ccc2c(c1)CCCC2)c1ccccc1-c1ccccc1
O-[C;H0;D3;+0:1](=[O;D1;H0:2])-[c;H0;D3;+0:3]1:[c:4]:[cH;D2;+0:5]:[c;H0;D3;+0:6](-[c:7](:[c:8]):[c:9]):[c:10]:[cH;D2;+0:11]:1.[OH;D1;+0:12]-[c:13](:[c:14]):[c:15]>>[O;D1;H0:2]=[C;H0;D3;+0:1](-[O;H0;D2;+0:12]-[c:13](:[c:14]):[c:15])-[c;H0;D3;+0:3]1:[c:4]:[cH;D2;+0:5]:[cH;D2;+0:11]:[c:10]:[c;H0;D3;+0:6]:1-[c:7](:[c:8]):[...
null
[]
null
null
3
HOUR
To a mixture of 0.31 g (1 mmol) of 1,2,3,4-tetrahydro-6-hydroxynaphthalene-2-carboxylic acid (R)-1-methylheptyl ester obtained as in the fourth stage of Example 23 where R-1-methyl heputanol was used in stead of (R)-1-trifluoromethylheptanol, 0.31 g (1 mmol) of 4'-octylbiphenyl-4-carboxylic acid (FK-1124-8 from Teikoku...
10.6084/m9.figshare.5104873.v1
null
Carboxylic acid.Aromatic alcohol
Ester
c1ccccc1
c1ccccc1
c1ccccc1.c1ccccc1.c1ccc2c(c1)CCCC2
HO-
C(Cl)Cl
null
3
CCCCCCCCc1ccc(-c2ccc(C(=O)O)cc2)cc1.CCCCCC[C@@H](C)OC(=O)C1CCc2cc(O)ccc2C1>C(Cl)Cl>CCCCCCCCc1ccc(-c2ccccc2C(=O)Oc2ccc3c(c2)CCC(C(=O)O[C@H](C)CCCCCC)C3)cc1
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-184fb5dc82c740e2b4c51bcf3ae69124
CCCCCCCCCCc1ccc(-c2ccc(C(=O)O)cc2)cc1.CCCCCC[C@@H](C)OC(=O)C1CCc2cc(O)ccc2C1>>CCCCCCCCCCc1ccc(-c2ccccc2C(=O)Oc2ccc3c(c2)CCC(C(=O)O[C@H](C)CCCCCC)C3)cc1
C[C@H](CCCCCC)OC(=O)C1CC2=CC=C(C=C2CC1)O.C1(CCCCC1)N=C=NC1CCCCC1.C(CCCCCCCCC)C1=CC=C(C=C1)C1=CC=C(C=C1)C(=O)O.FC([C@@H](CCCCCC)O)(F)F>>C[C@H](CCCCCC)OC(=O)C1CC2=CC=C(C=C2CC1)OC(=O)C=1C(=CC=CC1)C1=CC=C(C=C1)CCCCCCCCCC
O[C:21]([c:20]1[cH:17][cH:16][c:15](-[c:14]2[cH:13][cH:12][c:11]([CH2:10][CH2:9][CH2:8][CH2:7][CH2:6][CH2:5][CH2:4][CH2:3][CH2:2][CH3:1])[cH:46][cH:45]2)[cH:18][cH:19]1)=[O:22].[OH:23][c:24]1[cH:25][cH:26][c:27]2[c:28]([cH:29]1)[CH2:30][CH2:31][CH:32]([C:33](=[O:34])[O:35][C@H:36]([CH3:37])[CH2:38][CH2:39][CH2:40][CH2:...
CCCCCCCCCCc1ccc(-c2ccc(C(=O)O)cc2)cc1.CCCCCC[C@@H](C)OC(=O)C1CCc2cc(O)ccc2C1
CCCCCCCCCCc1ccc(-c2ccccc2C(=O)Oc2ccc3c(c2)CCC(C(=O)O[C@H](C)CCCCCC)C3)cc1
null
null
C(Cl)Cl
Acylation
OtherReaction
a6f963d149e8dd87f63c5bb958cffa4c95c2af472825d9145489a37ba75220bb
1489fe0065c6531b60fda87a3857d7da1cd21873868856f058c20706f927fa08
O=C(Oc1ccc2c(c1)CCCC2)c1ccccc1-c1ccccc1
O-[C;H0;D3;+0:1](=[O;D1;H0:2])-[c;H0;D3;+0:3]1:[c:4]:[cH;D2;+0:5]:[c;H0;D3;+0:6](-[c:7](:[c:8]):[c:9]):[c:10]:[cH;D2;+0:11]:1.[OH;D1;+0:12]-[c:13](:[c:14]):[c:15]>>[O;D1;H0:2]=[C;H0;D3;+0:1](-[O;H0;D2;+0:12]-[c:13](:[c:14]):[c:15])-[c;H0;D3;+0:3]1:[c:4]:[cH;D2;+0:5]:[cH;D2;+0:11]:[c:10]:[c;H0;D3;+0:6]:1-[c:7](:[c:8]):[...
null
[]
null
null
2.5
HOUR
To a mixture of 0.37 g (1.1 mmol) of 1,2,3,4-tetrahydro-6-hydroxynaphthalene-2-carboxylic acid (R)-1-methylheptyl ester obtained as in the fourth stage of Example 23 where (R)-1-methyl heputanol was used in stead of (R)-1-trifluoromethylheptanol, 0.33 g (1.1 mmol) of 4'-decylbiphenyl-4-carboxylic acid (FK-1124-10 from ...
10.6084/m9.figshare.5104873.v1
null
Carboxylic acid.Aromatic alcohol
Ester
c1ccccc1
c1ccccc1
c1ccccc1.c1ccccc1.c1ccc2c(c1)CCCC2
HO-
C(Cl)Cl
null
2.5
CCCCCCCCCCc1ccc(-c2ccc(C(=O)O)cc2)cc1.CCCCCC[C@@H](C)OC(=O)C1CCc2cc(O)ccc2C1>C(Cl)Cl>CCCCCCCCCCc1ccc(-c2ccccc2C(=O)Oc2ccc3c(c2)CCC(C(=O)O[C@H](C)CCCCCC)C3)cc1
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-cac03ebf9c0047c583eb8f2217093891
Cc1ccc(C(=O)O)cc1.O=C1CCC(=O)N1Br>>O=C(O)c1ccc(CBr)cc1
CC1=CC=C(C=C1)C(=O)O.BrN1C(CCC1=O)=O>>BrCC1=CC=C(C(=O)O)C=C1
[O:1]=[C:2]([OH:3])[c:4]1[cH:5][cH:6][c:7]([CH3:8])[cH:10][cH:11]1.O=C1CCC(=O)N1[Br:9]>>[O:1]=[C:2]([OH:3])[c:4]1[cH:5][cH:6][c:7]([CH2:8][Br:9])[cH:10][cH:11]1
Cc1ccc(C(=O)O)cc1.O=C1CCC(=O)N1Br
O=C(O)c1ccc(CBr)cc1
null
C(C1=CC=CC=C1)(=O)OOC(C1=CC=CC=C1)=O
C(Cl)(Cl)(Cl)Cl
Functional Group Interconversion
Wohl-Ziegler bromination benzyl primary
45c0aca0d63a96f0092e6dded9c888827eaf6379dac179e1cefc99293896300a
08f5e7e34d3f321cce3e85421b38226d6240cca0939494ae61032d4f8405cf22
c1ccccc1
O=C1-C-C-C(=O)-N-1-[Br;H0;D1;+0:1].[CH3;D1;+0:2]-[c:3](:[c:4]):[c:5]>>[Br;H0;D1;+0:1]-[CH2;D2;+0:2]-[c:3](:[c:4]):[c:5]
65.3
[{"value": 65.0, "product": "BrCC1=CC=C(C(=O)O)C=C1", "details": "PERCENTYIELD", "is_desired": false}, {"value": 65.3, "product": "BrCC1=CC=C(C(=O)O)C=C1", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
null
null
39.7 g (287 mmol) of p-toluylic acid, 51.2 g (287 mmol) of N-bromosuccinimide and 2.8 g (11.5 mmol) of dibenzoyl peroxide were suspended in 350 ml of carbon tetrachloride. Then, the resultant mixture was heated with vigorously stirring to perform a reaction under reflux for 2 hours. After completion of the reaction, th...
10.6084/m9.figshare.5104873.v1
null
Tertiary amide.Tertiary amide
Primary halide
C1CCNC1
null
c1ccccc1
HO-
C(C1=CC=CC=C1)(=O)OOC(C1=CC=CC=C1)=O.C(Cl)(Cl)(Cl)Cl
null
null
Cc1ccc(C(=O)O)cc1.O=C1CCC(=O)N1Br>C(C1=CC=CC=C1)(=O)OOC(C1=CC=CC=C1)=O.C(Cl)(Cl)(Cl)Cl>O=C(O)c1ccc(CBr)cc1
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-4f7cf5895f954e1fa345200adbbaaa61
CCCCCCCCCCOc1ccc2cc(C(=O)Oc3ccc(C(=O)OCc4ccccc4)cc3)ccc2c1>>CCCCCCCCCCOc1ccc2cc(C(=O)Oc3ccc(C(=O)O)cc3)ccc2c1
C(C1=CC=CC=C1)OC(C1=CC=C(C=C1)OC(=O)C1=CC2=CC=C(C=C2C=C1)OCCCCCCCCCC)=O.[H][H]>>C(CCCCCCCCC)OC=1C=C2C=CC(=CC2=CC1)C(=O)OC1=CC=C(C(=O)O)C=C1
c1ccc(C[O:27][C:25]([c:24]2[cH:23][cH:22][c:21]([O:20][C:18]([c:17]3[cH:16][c:15]4[cH:14][cH:13][c:12]([O:11][CH2:10][CH2:9][CH2:8][CH2:7][CH2:6][CH2:5][CH2:4][CH2:3][CH2:2][CH3:1])[cH:33][c:32]4[cH:31][cH:30]3)=[O:19])[cH:29][cH:28]2)=[O:26])cc1>>[CH3:1][CH2:2][CH2:3][CH2:4][CH2:5][CH2:6][CH2:7][CH2:8][CH2:9][CH2:10][...
CCCCCCCCCCOc1ccc2cc(C(=O)Oc3ccc(C(=O)OCc4ccccc4)cc3)ccc2c1
CCCCCCCCCCOc1ccc2cc(C(=O)Oc3ccc(C(=O)O)cc3)ccc2c1
null
[Pd]
C1CCOC1
Deprotection
Ester saponification (alkyl deprotection)
86a971d3e4f88009ab4c98512e9f1deb51b2f0ce5cbd068cc61ae878c1e58e2a
38ae1ee78433b9acfb0390501446149c80f88f23ac2d84c60b3369bdab75cec9
O=C(Oc1ccccc1)c1ccc2ccccc2c1
[O;D1;H0:1]=[C:2](-[c:3])-[O;H0;D2;+0:4]-C-c1:c:c:c:c:c:1>>[O;D1;H0:1]=[C:2](-[OH;D1;+0:4])-[c:3]
97.5
[{"value": 97.5, "product": "C(CCCCCCCCC)OC=1C=C2C=CC(=CC2=CC1)C(=O)OC1=CC=C(C(=O)O)C=C1", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
null
null
To 37.6 g (0.07 mol) of the 4-(6-decyloxy-2-naphthoyloxy)benzoic acid benzyl ester obtained in the first stage was added 3.76 g of 5% palladium/carbon, and further added 188 g of THF. Then, hydrogen gas was blown into the mixture. The resultant mixture was stirred overnight and filtered to obtain 30.6 g of 4-(6-decylox...
10.6084/m9.figshare.5104873.v1
null
Ester
Carboxylic acid
c1ccccc1
null
c1ccc2ccccc2c1.c1ccccc1
Other
[Pd].C1CCOC1
null
null
CCCCCCCCCCOc1ccc2cc(C(=O)Oc3ccc(C(=O)OCc4ccccc4)cc3)ccc2c1>[Pd].C1CCOC1>CCCCCCCCCCOc1ccc2cc(C(=O)Oc3ccc(C(=O)O)cc3)ccc2c1
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-436174135cd54d56bccd8e2f39d9c63d
CCCCCCCCCCOc1ccc(OC(=O)C2CCc3cc(OCc4ccccc4)ccc3C2)cc1>>CCCCCCCCCCOc1ccc(OC(=O)C2CCc3cc(O)ccc3C2)cc1
C(CCCCCCCCC)OC1=CC=C(C=C1)OC(=O)C1CC2=CC=C(C=C2CC1)OCC1=CC=CC=C1.[H][H]>>C(CCCCCCCCC)OC1=CC=C(C=C1)OC(=O)C1CC2=CC=C(C=C2CC1)O
c1ccc(C[O:25][c:24]2[cH:23][c:22]3[c:28]([cH:27][cH:26]2)[CH2:29][CH:19]([C:17]([O:16][c:15]2[cH:14][cH:13][c:12]([O:11][CH2:10][CH2:9][CH2:8][CH2:7][CH2:6][CH2:5][CH2:4][CH2:3][CH2:2][CH3:1])[cH:31][cH:30]2)=[O:18])[CH2:20][CH2:21]3)cc1>>[CH3:1][CH2:2][CH2:3][CH2:4][CH2:5][CH2:6][CH2:7][CH2:8][CH2:9][CH2:10][O:11][c:1...
CCCCCCCCCCOc1ccc(OC(=O)C2CCc3cc(OCc4ccccc4)ccc3C2)cc1
CCCCCCCCCCOc1ccc(OC(=O)C2CCc3cc(O)ccc3C2)cc1
null
[Pd]
O1CCCC1
Deprotection
Hydroxyl benzyl deprotection
36869d1fe85185a14d9eb30bf05178c600a9b6eca277ffaf3803578c30e0bf5d
26a36596df80ec137b0e8087297418351c93c32819177f680675220622f215d4
O=C(Oc1ccccc1)C1CCc2ccccc2C1
[c:1]:[c:2](-[O;H0;D2;+0:3]-C-c1:c:c:c:c:c:1):[c:4]>>[OH;D1;+0:3]-[c:2](:[c:1]):[c:4]
97.7
[{"value": 97.0, "product": "C(CCCCCCCCC)OC1=CC=C(C=C1)OC(=O)C1CC2=CC=C(C=C2CC1)O", "details": "PERCENTYIELD", "is_desired": false}, {"value": 97.7, "product": "C(CCCCCCCCC)OC1=CC=C(C=C1)OC(=O)C1CC2=CC=C(C=C2CC1)O", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
null
null
Then, 0.04 g of 5% palladium/carbon and 10 ml of a tetrahydrofuran solution containing 0.36 g of 2-(4-decyloxyphenyloxycarbonyl)-1,2,3,4-tetrahydro-6-benzyloxynaphthalene were stirred overnight at room temperature in a stream of hydrogen to decompose a benzyl protective group by hydrogenation. 5% palladium/carbon was r...
10.6084/m9.figshare.5104873.v1
null
Ether
Aromatic alcohol
c1ccccc1
null
c1ccccc1.c1ccc2c(c1)CCCC2
Other
[Pd].O1CCCC1
null
null
CCCCCCCCCCOc1ccc(OC(=O)C2CCc3cc(OCc4ccccc4)ccc3C2)cc1>[Pd].O1CCCC1>CCCCCCCCCCOc1ccc(OC(=O)C2CCc3cc(O)ccc3C2)cc1
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-3241ab6c22d447b498b7ce647cbfc9d9
CC(=O)O.O=Cc1ccc(C(=O)OCc2ccccc2)cc1>>O=C(O)c1ccc(C(=O)OCc2ccccc2)cc1
C(C)(=O)O.C(C)(=O)O.C(C1=CC=CC=C1)OC(C1=CC=C(C=C1)C=O)=O>>C(C1=CC=CC=C1)OC(=O)C1=CC=C(C(=O)O)C=C1
CC(=O)[OH:3].[O:1]=[CH:2][c:4]1[cH:5][cH:6][c:7]([C:8](=[O:9])[O:10][CH2:11][c:12]2[cH:13][cH:14][cH:15][cH:16][cH:17]2)[cH:18][cH:19]1>>[O:1]=[C:2]([OH:3])[c:4]1[cH:5][cH:6][c:7]([C:8](=[O:9])[O:10][CH2:11][c:12]2[cH:13][cH:14][cH:15][cH:16][cH:17]2)[cH:18][cH:19]1
CC(=O)O.O=Cc1ccc(C(=O)OCc2ccccc2)cc1
O=C(O)c1ccc(C(=O)OCc2ccccc2)cc1
null
null
O
Acylation
OtherReaction
d5040721921addb6bab9ff19b117684a5fd543f11d3d76c396d17c6075d19e99
300ca3c6bc6ac7a77293ad6cd69ffcaf96f2c9254b40f6adf6415af60ae8f700
O=C(OCc1ccccc1)c1ccccc1
C-C(=O)-[OH;D1;+0:1].[O;D1;H0:2]=[CH;D2;+0:3]-[c:4](:[c:5]):[c:6]>>[O;D1;H0:2]=[C;H0;D3;+0:3](-[OH;D1;+0:1])-[c:4](:[c:5]):[c:6]
49
[{"value": 49.0, "product": "C(C1=CC=CC=C1)OC(=O)C1=CC=C(C(=O)O)C=C1", "details": "PERCENTYIELD", "is_desired": false}]
null
null
2
HOUR
To 50 ml of an acetic acid solution containing 7.34 g (30.5 mmol) of 4-formylbenzoic acid benzyl ester were dropwise added 4.53 g (4.35 mmol) of chromic acid anhydride, 40 ml of acetic acid and 1.3 ml of water with stirring at room temperature for a period of 2 hours. The oxidation of a formyl group was further carried...
10.6084/m9.figshare.5104873.v1
null
Aldehyde.Carboxylic acid
Carboxylic acid
null
null
c1ccccc1.c1ccccc1
HO-
O
null
2
CC(=O)O.O=Cc1ccc(C(=O)OCc2ccccc2)cc1>O>O=C(O)c1ccc(C(=O)OCc2ccccc2)cc1
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-679c764250d94da2b08939ad59ce9559
CCCCCC[C@@H](OC(=O)c1ccc(C(=O)OCc2ccccc2)cc1)C(F)(F)F>>CCCCCC[C@@H](OC(=O)c1ccc(C(=O)O)cc1)C(F)(F)F
C(C1=CC=CC=C1)OC(C1=CC=C(C=C1)C(=O)O[C@H](CCCCCC)C(F)(F)F)=O.[H][H]>>FC([C@@H](CCCCCC)OC(=O)C1=CC=C(C(=O)O)C=C1)(F)F
c1ccc(C[O:17][C:15]([c:14]2[cH:13][cH:12][c:11]([C:9]([O:8][C@H:7]([CH2:6][CH2:5][CH2:4][CH2:3][CH2:2][CH3:1])[C:20]([F:21])([F:22])[F:23])=[O:10])[cH:19][cH:18]2)=[O:16])cc1>>[CH3:1][CH2:2][CH2:3][CH2:4][CH2:5][CH2:6][C@@H:7]([O:8][C:9](=[O:10])[c:11]1[cH:12][cH:13][c:14]([C:15](=[O:16])[OH:17])[cH:18][cH:19]1)[C:20](...
CCCCCC[C@@H](OC(=O)c1ccc(C(=O)OCc2ccccc2)cc1)C(F)(F)F
CCCCCC[C@@H](OC(=O)c1ccc(C(=O)O)cc1)C(F)(F)F
null
[Pd]
O1CCCC1
Deprotection
Ester saponification (alkyl deprotection)
86a971d3e4f88009ab4c98512e9f1deb51b2f0ce5cbd068cc61ae878c1e58e2a
38ae1ee78433b9acfb0390501446149c80f88f23ac2d84c60b3369bdab75cec9
c1ccccc1
[O;D1;H0:1]=[C:2](-[c:3])-[O;H0;D2;+0:4]-C-c1:c:c:c:c:c:1>>[O;D1;H0:1]=[C:2](-[OH;D1;+0:4])-[c:3]
98.9
[{"value": 98.0, "product": "FC([C@@H](CCCCCC)OC(=O)C1=CC=C(C(=O)O)C=C1)(F)F", "details": "PERCENTYIELD", "is_desired": false}, {"value": 98.9, "product": "FC([C@@H](CCCCCC)OC(=O)C1=CC=C(C(=O)O)C=C1)(F)F", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
null
null
Then, 0.07 g of 5% palladium/carbon and 10 ml of a tetrahydrofuran solution containing 0.63 g of 4-((R)-1-trifluoromethylheptyloxycarbonyl)benzoic acid benzyl ester were stirred overnight at room temperature in a stream of hydrogen to decompose a benzyl protective group by hydrogenation. 5% palladium/carbon was removed...
10.6084/m9.figshare.5104873.v1
null
Ester
Carboxylic acid
c1ccccc1
null
c1ccccc1
Other
[Pd].O1CCCC1
null
null
CCCCCC[C@@H](OC(=O)c1ccc(C(=O)OCc2ccccc2)cc1)C(F)(F)F>[Pd].O1CCCC1>CCCCCC[C@@H](OC(=O)c1ccc(C(=O)O)cc1)C(F)(F)F
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-788333422f5e4a87925a5f9214f163ee
CCCCCC[C@@H](C)OC(=O)c1ccc(C(=O)OCc2ccccc2)cc1>>CCCCCC[C@@H](C)OC(=O)c1ccc(C(=O)O)cc1
C(C1=CC=CC=C1)OC(C1=CC=C(C=C1)C(=O)O[C@@H](CCCCCC)C)=O.[H][H]>>C[C@H](CCCCCC)OC(=O)C1=CC=C(C(=O)O)C=C1
c1ccc(C[O:18][C:16]([c:15]2[cH:14][cH:13][c:12]([C:10]([O:9][C@@H:7]([CH2:6][CH2:5][CH2:4][CH2:3][CH2:2][CH3:1])[CH3:8])=[O:11])[cH:20][cH:19]2)=[O:17])cc1>>[CH3:1][CH2:2][CH2:3][CH2:4][CH2:5][CH2:6][C@@H:7]([CH3:8])[O:9][C:10](=[O:11])[c:12]1[cH:13][cH:14][c:15]([C:16](=[O:17])[OH:18])[cH:19][cH:20]1
CCCCCC[C@@H](C)OC(=O)c1ccc(C(=O)OCc2ccccc2)cc1
CCCCCC[C@@H](C)OC(=O)c1ccc(C(=O)O)cc1
null
[Pd]
O1CCCC1
Deprotection
Ester saponification (alkyl deprotection)
86a971d3e4f88009ab4c98512e9f1deb51b2f0ce5cbd068cc61ae878c1e58e2a
38ae1ee78433b9acfb0390501446149c80f88f23ac2d84c60b3369bdab75cec9
c1ccccc1
[O;D1;H0:1]=[C:2](-[c:3])-[O;H0;D2;+0:4]-C-c1:c:c:c:c:c:1>>[O;D1;H0:1]=[C:2](-[OH;D1;+0:4])-[c:3]
99.6
[{"value": 99.0, "product": "C[C@H](CCCCCC)OC(=O)C1=CC=C(C(=O)O)C=C1", "details": "PERCENTYIELD", "is_desired": false}, {"value": 99.6, "product": "C[C@H](CCCCCC)OC(=O)C1=CC=C(C(=O)O)C=C1", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
null
null
Then, 0.12 g of 5% palladium/carbon and 30 ml of a tetrahydrofuran solution containing 1.21 g of 4-((R)-1-methylheptyloxycarbonyl)benzoic acid benzyl ester were stirred overnight at room temperature in a stream of hydrogen to decompose a benzyl protective group by hydrogenation. 5% palladium/carbon was removed using Ce...
10.6084/m9.figshare.5104873.v1
null
Ester
Carboxylic acid
c1ccccc1
null
c1ccccc1
Other
[Pd].O1CCCC1
null
null
CCCCCC[C@@H](C)OC(=O)c1ccc(C(=O)OCc2ccccc2)cc1>[Pd].O1CCCC1>CCCCCC[C@@H](C)OC(=O)c1ccc(C(=O)O)cc1
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-c8e403a545964087ba37eaf4049bc15b
CCCCCCCCCCOc1ccc(-c2ccc(C(=O)O)cc2)cc1>>CCCCCCCCCCOc1ccc(-c2ccc(CO)cc2)cc1
[H-].[H-].[H-].[H-].[Li+].[Al+3].C(CCCCCCCCC)OC1=CC=C(C=C1)C1=CC=C(C=C1)C(=O)O>>OCC1=CC=C(C=C1)C1=CC=C(C=C1)OCCCCCCCCCC
O=[C:20]([c:19]1[cH:18][cH:17][c:16](-[c:15]2[cH:14][cH:13][c:12]([O:11][CH2:10][CH2:9][CH2:8][CH2:7][CH2:6][CH2:5][CH2:4][CH2:3][CH2:2][CH3:1])[cH:25][cH:24]2)[cH:23][cH:22]1)[OH:21]>>[CH3:1][CH2:2][CH2:3][CH2:4][CH2:5][CH2:6][CH2:7][CH2:8][CH2:9][CH2:10][O:11][c:12]1[cH:13][cH:14][c:15](-[c:16]2[cH:17][cH:18][c:19]([...
CCCCCCCCCCOc1ccc(-c2ccc(C(=O)O)cc2)cc1
CCCCCCCCCCOc1ccc(-c2ccc(CO)cc2)cc1
null
null
C(C)OCC
Reduction
Reduction of carboxylic acid to primary alcohol
0db83a5ebe1e318b78b55461cf7eb8f7c004eef0f9e3b6666d3df4c96b5f665e
93b4621647b04d2ad2f2825215b1567f171ba61fe10d136b5db6ea0470aa4932
c1ccc(-c2ccccc2)cc1
O=[C;H0;D3;+0:1](-[O;D1;H1:2])-[c:3](:[c:4]):[c:5]>>[O;D1;H1:2]-[CH2;D2;+0:1]-[c:3](:[c:4]):[c:5]
null
[]
null
null
null
null
0.81 g (21.34 mmol) of LiAlH4 was introduced into 40 ml of diethyl ether and stirred. To the mixture was dropwise added a solution, prepared by introducing 1.71 g (5.06 mmol) of 4'-decyloxy-4-biphenylcarboxylic acid obtained in the first stage of Example 11 into 30 ml of diethyl ether, at room temperature over a period...
10.6084/m9.figshare.5104873.v1
null
Carboxylic acid
Primary alcohol
null
null
c1ccccc1.c1ccccc1
Other
C(C)OCC
null
null
CCCCCCCCCCOc1ccc(-c2ccc(C(=O)O)cc2)cc1>C(C)OCC>CCCCCCCCCCOc1ccc(-c2ccc(CO)cc2)cc1
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-3104bd09c2f7414fbbfc325719b77c64
Br.CCCCCCCCCCOc1ccc(-c2ccc(CO)cc2)cc1>>CCCCCCCCCCOc1ccc(-c2ccc(CBr)cc2)cc1
OCC1=CC=C(C=C1)C1=CC=C(C=C1)OCCCCCCCCCC.Br>>BrCC1=CC=C(C=C1)C1=CC=C(C=C1)OCCCCCCCCCC
[BrH:21].O[CH2:20][c:19]1[cH:18][cH:17][c:16](-[c:15]2[cH:14][cH:13][c:12]([O:11][CH2:10][CH2:9][CH2:8][CH2:7][CH2:6][CH2:5][CH2:4][CH2:3][CH2:2][CH3:1])[cH:25][cH:24]2)[cH:23][cH:22]1>>[CH3:1][CH2:2][CH2:3][CH2:4][CH2:5][CH2:6][CH2:7][CH2:8][CH2:9][CH2:10][O:11][c:12]1[cH:13][cH:14][c:15](-[c:16]2[cH:17][cH:18][c:19](...
Br.CCCCCCCCCCOc1ccc(-c2ccc(CO)cc2)cc1
CCCCCCCCCCOc1ccc(-c2ccc(CBr)cc2)cc1
null
null
null
Miscellaneous
OtherReaction
cd3478bc4d4e901afd9352e983cdb4ff4c2fc601772cf0af2f0553c983f9121c
9b4091cd4cf205a0767d592c748f58d9aed076d9567056ed2bfdc4af71bd7267
c1ccc(-c2ccccc2)cc1
O-[CH2;D2;+0:1]-[c:2](:[c:3]):[c:4].[BrH;D0;+0:5]>>[Br;H0;D1;+0:5]-[CH2;D2;+0:1]-[c:2](:[c:3]):[c:4]
null
[]
null
null
3
HOUR
To 0.81 g (2.51 mmol) of 4-hydroxymethyl-4'-decyloxybiphenyl was added 15 ml of an aqueous solution containing 47% HBr, and then healed at 115° C. for 3 hours. After completion of the reaction, the resultant mixture was extracted with ether and washed with water, which was further washed with an aqueous solution contai...
10.6084/m9.figshare.5104873.v1
null
Primary alcohol
Primary halide
null
null
c1ccccc1.c1ccccc1
HO-
null
null
3
Br.CCCCCCCCCCOc1ccc(-c2ccc(CO)cc2)cc1>>CCCCCCCCCCOc1ccc(-c2ccc(CBr)cc2)cc1
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-3bb66da6f37b43aebd4a5504e234b1f4
CC(C)[C@H](N)C(=O)O.CC1(C)S[C@@H]2[C@H](NC(=O)Cc3ccccc3)C(=O)N2[C@H]1C(=O)[O-]>>CC1(C)S[C@@H]2[C@H](NC(=O)CCC[C@H](N)C(=O)O)C(=O)N2[C@H]1C(=O)O
N[C@@H](CS)C(=O)O.N[C@@H](C(C)C)C(=O)O.CC1([C@@H](N2[C@H](S1)[C@@H](C2=O)NC(=O)CC=3C=CC=CC3)C(=O)[O-])C.[K+]>>CC1([C@@H](N2[C@H](S1)[C@@H](C2=O)NC(=O)CCC[C@@H](C(=O)O)N)C(=O)O)C
C[CH:12]([CH3:11])[C@H:13]([NH2:14])[C:15](=[O:16])[OH:17].c1ccc([CH2:10][C:8]([NH:7][C@H:6]2[C@H:5]3[S:4][C:2]([CH3:1])([CH3:3])[C@H:21]([C:22](=[O:23])[O-:24])[N:20]3[C:18]2=[O:19])=[O:9])cc1>>[CH3:1][C:2]1([CH3:3])[S:4][C@@H:5]2[C@H:6]([NH:7][C:8](=[O:9])[CH2:10][CH2:11][CH2:12][C@H:13]([NH2:14])[C:15](=[O:16])[OH:1...
CC(C)[C@H](N)C(=O)O.CC1(C)S[C@@H]2[C@H](NC(=O)Cc3ccccc3)C(=O)N2[C@H]1C(=O)[O-]
CC1(C)S[C@@H]2[C@H](NC(=O)CCC[C@H](N)C(=O)O)C(=O)N2[C@H]1C(=O)O
null
null
null
C-C Coupling
OtherReaction
b1c5a75836252e474a37fcf494cff25f4048b2f6fdb0bbc647b8a649fa439615
0a3570e04fbe6a3b2ffc12a820c50434dd728efb01bf353938ae9117a6d26a85
O=C1C[C@H]2SCCN12
C-[CH;D3;+0:1](-[CH3;D1;+0:2])-[C:3](-[N;D1;H2:4])-[C:5](=[O;D1;H0:6])-[O;D1;H1:7].[O-;H0;D1:8]-[C:9](=[O;D1;H0:10])-[C:11]-[#7:12]-[C:13](=[O;D1;H0:14])-[C:15]-[#7:16]-[C:17](=[O;D1;H0:18])-[CH2;D2;+0:19]-c1:c:c:c:c:c:1>>[N;D1;H2:4]-[C:3](-[CH2;D2;+0:1]-[CH2;D2;+0:2]-[CH2;D2;+0:19]-[C:17](=[O;D1;H0:18])-[#7:16]-[C:15]...
null
[]
null
null
null
null
The first two steps in the biosynthesis of penicillin in P. chrysogenum are the condensation of the three amino acids L-5-amino-5-carboxypentanoic acid (L-α-aminoadipic acid) (A), L-cysteine (C) and L-valine (V) into the tripeptide LLD-ACV, followed by cyclization of this tripeptide to form isopenicillin N. This compou...
10.6084/m9.figshare.5104873.v1
null
null
Carboxylic acid
c1ccccc1
null
C1CN2CC[C@H]2S1
Other
null
null
null
CC(C)[C@H](N)C(=O)O.CC1(C)S[C@@H]2[C@H](NC(=O)Cc3ccccc3)C(=O)N2[C@H]1C(=O)[O-]>>CC1(C)S[C@@H]2[C@H](NC(=O)CCC[C@H](N)C(=O)O)C(=O)N2[C@H]1C(=O)O
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-95c128d17561404a9f727a241cd8c7d9
COC(=O)N[C@@H](Cc1ccccc1)C(=O)CCl>>COC(=O)N[C@@H](Cc1ccccc1)[C@H](O)CCl
[OH-].[Na+].ClCC([C@H](CC1=CC=CC=C1)NC(=O)OC)=O.O=C[C@H](O)[C@@H](O)[C@H](O)[C@H](O)CO.O=C[C@H](O)[C@@H](O)[C@H](O)[C@H](O)CO.ClCC([C@H](CC1=CC=CC=C1)NC(=O)OC)=O.S(O)(O)(=O)=O.O=C[C@H](O)[C@@H](O)[C@H](O)[C@H](O)CO.ClCC([C@H](CC1=CC=CC=C1)NC(=O)OC)=O>>ClC[C@H]([C@H](CC1=CC=CC=C1)NC(=O)OC)O
[CH3:1][O:2][C:3](=[O:4])[NH:5][C@@H:6]([CH2:7][c:8]1[cH:9][cH:10][cH:11][cH:12][cH:13]1)[C:14](=[O:15])[CH2:16][Cl:17]>>[CH3:1][O:2][C:3](=[O:4])[NH:5][C@@H:6]([CH2:7][c:8]1[cH:9][cH:10][cH:11][cH:12][cH:13]1)[C@H:14]([OH:15])[CH2:16][Cl:17]
COC(=O)N[C@@H](Cc1ccccc1)C(=O)CCl
COC(=O)N[C@@H](Cc1ccccc1)[C@H](O)CCl
null
null
null
Reduction
Reduction of ketone to secondary alcohol
02790ac194d8bf7ccb13d6247c59412024d87f77d2c906ef7804f021f57d5070
1bd3cd74b454139c0a0068ac0135836499926b274bff569df163210c6c944a89
c1ccccc1
[#8:1]-[C:2](=[O;D1;H0:3])-[#7:4]-[C:5](-[C:6])-[C;H0;D3;+0:7](=[O;H0;D1;+0:8])-[C:9]-[Cl;D1;H0:10]>>[#8:1]-[C:2](=[O;D1;H0:3])-[#7:4]-[C:5](-[C:6])-[C@H;D3;+0:7](-[OH;D1;+0:8])-[C:9]-[Cl;D1;H0:10]
67
[{"value": 67.0, "product": "ClC[C@H]([C@H](CC1=CC=CC=C1)NC(=O)OC)O", "details": "PERCENTYIELD", "is_desired": false}]
null
null
1
DAY
A culture was obtained by the same method as in Example 1 using Geotrichum eriense ATCC 22311 as the microorganism and then adjusted to pH 6 with an aqueous sodium hydroxide solution and an aqueous sulfuric acid solution. A 25-ml portion of this culture, 1 g of glucose and (3S)-1-chloro-3-methoxycarbonylamino-4-phenyl-...
10.6084/m9.figshare.5104873.v1
null
Ketone
Secondary alcohol
null
null
c1ccccc1
null
null
null
24
COC(=O)N[C@@H](Cc1ccccc1)C(=O)CCl>>COC(=O)N[C@@H](Cc1ccccc1)[C@H](O)CCl
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-dfb2793f61924a0a99912919753f0f33
COC(=O)N[C@@H](Cc1ccccc1)C(=O)CCl>>COC(=O)N[C@@H](Cc1ccccc1)[C@H](O)CCl
[OH-].[Na+].S(O)(O)(=O)=O.ClCC([C@H](CC1=CC=CC=C1)NC(=O)OC)=O>>ClC[C@H]([C@H](CC1=CC=CC=C1)NC(=O)OC)O
[CH3:1][O:2][C:3](=[O:4])[NH:5][C@@H:6]([CH2:7][c:8]1[cH:9][cH:10][cH:11][cH:12][cH:13]1)[C:14](=[O:15])[CH2:16][Cl:17]>>[CH3:1][O:2][C:3](=[O:4])[NH:5][C@@H:6]([CH2:7][c:8]1[cH:9][cH:10][cH:11][cH:12][cH:13]1)[C@H:14]([OH:15])[CH2:16][Cl:17]
COC(=O)N[C@@H](Cc1ccccc1)C(=O)CCl
COC(=O)N[C@@H](Cc1ccccc1)[C@H](O)CCl
null
null
null
Reduction
Reduction of ketone to secondary alcohol
02790ac194d8bf7ccb13d6247c59412024d87f77d2c906ef7804f021f57d5070
1bd3cd74b454139c0a0068ac0135836499926b274bff569df163210c6c944a89
c1ccccc1
[#8:1]-[C:2](=[O;D1;H0:3])-[#7:4]-[C:5](-[C:6])-[C;H0;D3;+0:7](=[O;H0;D1;+0:8])-[C:9]-[Cl;D1;H0:10]>>[#8:1]-[C:2](=[O;D1;H0:3])-[#7:4]-[C:5](-[C:6])-[C@H;D3;+0:7](-[OH;D1;+0:8])-[C:9]-[Cl;D1;H0:10]
61
[{"value": 61.0, "product": "ClC[C@H]([C@H](CC1=CC=CC=C1)NC(=O)OC)O", "details": "PERCENTYIELD", "is_desired": false}]
null
null
1
DAY
A culture was obtained by the same method as in Example 1 using Candida gropengiesseri IFO 0659 as the microorganism and adjusted to pH 6 with an aqueous sodium hydroxide solution and an aqueous sulfuric acid solution. A 75-ml portion of this culture was separated into a supernatant and cells by centrifugation. To the ...
10.6084/m9.figshare.5104873.v1
null
Ketone
Secondary alcohol
null
null
c1ccccc1
null
null
null
24
COC(=O)N[C@@H](Cc1ccccc1)C(=O)CCl>>COC(=O)N[C@@H](Cc1ccccc1)[C@H](O)CCl
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-b36cf4c3fce444e59afcc58bc7669a0f
O=C[C@H](O)[C@@H](O)[C@H](O)CO.O=C[C@H](O)[C@@H](O)[C@H](O)CO>>O=C[C@H](O)[C@@H](O)[C@H](O)[C@H](O)CO
C(C)O.C(C)O.O=C[C@H](O)[C@@H](O)[C@H](O)CO.O=C[C@H](O)[C@@H](O)[C@H](O)CO>>O=C[C@H](O)[C@@H](O)[C@H](O)[C@H](O)CO
[O:1]=[CH:2][C@H:3]([OH:4])[C@@H:5]([OH:6])[C@H:9]([OH:10])[CH2:11][OH:12].O=C[C@H](O)[C@@H](O)[C@@H:7](CO)[OH:8]>>[O:1]=[CH:2][C@H:3]([OH:4])[C@@H:5]([OH:6])[C@H:7]([OH:8])[C@H:9]([OH:10])[CH2:11][OH:12]
O=C[C@H](O)[C@@H](O)[C@H](O)CO.O=C[C@H](O)[C@@H](O)[C@H](O)CO
O=C[C@H](O)[C@@H](O)[C@H](O)[C@H](O)CO
null
null
null
C-C Coupling
OtherReaction
da8253d53c446f50e056a5337582998833688785c7190c36df3d409121ea7fb8
a1a0b3762b3789a70fef4edbf46bd73cf56ea18179ec70debe5450d925b63f0f
null
null
null
[]
null
null
null
null
The results presented in FIG. 2 show that in contrast to the control strain containing the shuttle vector alone (CP4[pZB 186]), the recombinant containing the added xylose isomerase, xylulokinase, transaldolase and transketolase genes demonstrated growth and ethanol production from xylose as a carbon source. The recomb...
10.6084/m9.figshare.5104873.v1
null
Aldehyde.Primary alcohol.Secondary alcohol.Secondary alcohol.Secondary alcohol.Secondary alcohol.Secondary alcohol
Secondary alcohol.Secondary alcohol.Secondary alcohol
null
null
null
HO-
null
null
null
O=C[C@H](O)[C@@H](O)[C@H](O)CO.O=C[C@H](O)[C@@H](O)[C@H](O)CO>>O=C[C@H](O)[C@@H](O)[C@H](O)[C@H](O)CO
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-a1000e40f2db412d9d636d6f712f48b1
CC(=O)c1cccs1.NNc1ccc(F)cc1>>CC(=NNc1ccc(F)cc1)c1cccs1
Cl.FC1=CC=C(C=C1)NN.C(C)(=O)C=1SC=CC1>>FC1=CC=C(C=C1)NN=C(C)C=1SC=CC1
O=[C:2]([CH3:1])[c:12]1[cH:13][cH:14][cH:15][s:16]1.[NH2:3][NH:4][c:5]1[cH:6][cH:7][c:8]([F:9])[cH:10][cH:11]1>>[CH3:1][C:2](=[N:3][NH:4][c:5]1[cH:6][cH:7][c:8]([F:9])[cH:10][cH:11]1)[c:12]1[cH:13][cH:14][cH:15][s:16]1
CC(=O)c1cccs1.NNc1ccc(F)cc1
CC(=NNc1ccc(F)cc1)c1cccs1
null
null
null
Heteroatom Alkylation and Arylation
OtherReaction
83882590079d324612170330ec542715e8ce71411b1b2946e5f0d75ea75ad4dd
16267fcabf9e555e6c245927fd3675c621f876db12f50a1b3e8576a12e06a1cf
C(=NNc1ccccc1)c1cccs1
O=[C;H0;D3;+0:1](-[C;D1;H3:2])-[c:3](:[c:4]):[#16;a:5]:[c:6].[NH2;D1;+0:7]-[#7:8]-[c:9]>>[C;D1;H3:2]-[C;H0;D3;+0:1](=[N;H0;D2;+0:7]-[#7:8]-[c:9])-[c:3](:[c:4]):[#16;a:5]:[c:6]
null
[]
null
null
null
null
This compound is prepared from commercial 4-fluorophenylhydrazine hydrochloride (Aldrich) and from commercial 2-acetylthiophene (Aldrich), according to the procedure 1. Conditions: See reaction.notes.procedure_details.
10.6084/m9.figshare.5104873.v1
null
Hydrazine.Ketone
Hydrazone
null
null
c1ccccc1.c1ccsc1
HO-
null
null
null
CC(=O)c1cccs1.NNc1ccc(F)cc1>>CC(=NNc1ccc(F)cc1)c1cccs1
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-661c1c44ce674dabb8690fdab4920af6
CC(=O)c1cccs1.NNc1cccc(F)c1>>CC(=NNc1cccc(F)c1)c1cccs1
Cl.FC=1C=C(C=CC1)NN.C(C)(=O)C=1SC=CC1>>FC=1C=C(C=CC1)NN=C(C)C=1SC=CC1
O=[C:2]([CH3:1])[c:12]1[cH:13][cH:14][cH:15][s:16]1.[NH2:3][NH:4][c:5]1[cH:6][cH:7][cH:8][c:9]([F:10])[cH:11]1>>[CH3:1][C:2](=[N:3][NH:4][c:5]1[cH:6][cH:7][cH:8][c:9]([F:10])[cH:11]1)[c:12]1[cH:13][cH:14][cH:15][s:16]1
CC(=O)c1cccs1.NNc1cccc(F)c1
CC(=NNc1cccc(F)c1)c1cccs1
null
null
null
Heteroatom Alkylation and Arylation
OtherReaction
83882590079d324612170330ec542715e8ce71411b1b2946e5f0d75ea75ad4dd
16267fcabf9e555e6c245927fd3675c621f876db12f50a1b3e8576a12e06a1cf
C(=NNc1ccccc1)c1cccs1
O=[C;H0;D3;+0:1](-[C;D1;H3:2])-[c:3](:[c:4]):[#16;a:5]:[c:6].[NH2;D1;+0:7]-[#7:8]-[c:9]>>[C;D1;H3:2]-[C;H0;D3;+0:1](=[N;H0;D2;+0:7]-[#7:8]-[c:9])-[c:3](:[c:4]):[#16;a:5]:[c:6]
null
[]
null
null
null
null
This compound is prepared from commercial 3-fluorophenylhydrazine hydrochloride (Aldrich) and from commercial 2-acetylthiophene (Aldrich), according to the procedure 1. Conditions: See reaction.notes.procedure_details.
10.6084/m9.figshare.5104873.v1
null
Hydrazine.Ketone
Hydrazone
null
null
c1ccccc1.c1ccsc1
HO-
null
null
null
CC(=O)c1cccs1.NNc1cccc(F)c1>>CC(=NNc1cccc(F)c1)c1cccs1
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-b1c4c35e4d754049b51187394fb98649
CC(=O)c1ccc[se]1.NNc1ccccc1>>CC(=NNc1ccccc1)c1ccc[se]1
Cl.C1(=CC=CC=C1)NN.C(C)(=O)C=1[Se]C=CC1>>C1(=CC=CC=C1)NN=C(C)C=1[Se]C=CC1
O=[C:2]([CH3:1])[c:11]1[cH:12][cH:13][cH:14][se:15]1.[NH2:3][NH:4][c:5]1[cH:6][cH:7][cH:8][cH:9][cH:10]1>>[CH3:1][C:2](=[N:3][NH:4][c:5]1[cH:6][cH:7][cH:8][cH:9][cH:10]1)[c:11]1[cH:12][cH:13][cH:14][se:15]1
CC(=O)c1ccc[se]1.NNc1ccccc1
CC(=NNc1ccccc1)c1ccc[se]1
null
null
null
Heteroatom Alkylation and Arylation
OtherReaction
83882590079d324612170330ec542715e8ce71411b1b2946e5f0d75ea75ad4dd
16267fcabf9e555e6c245927fd3675c621f876db12f50a1b3e8576a12e06a1cf
C(=NNc1ccccc1)c1ccc[se]1
O=[C;H0;D3;+0:1](-[C;D1;H3:2])-[c:3](:[c:4]):[#34;a:5]:[c:6].[NH2;D1;+0:7]-[#7:8]-[c:9]>>[C;D1;H3:2]-[C;H0;D3;+0:1](=[N;H0;D2;+0:7]-[#7:8]-[c:9])-[c:3](:[c:4]):[#34;a:5]:[c:6]
null
[]
null
null
null
null
This compound is prepared from commercial phenylhydrazine hydrochloride (Aldrich) and 2-acetylselenophene, which is itself obtained according to the procedure described by S. Umezawa (reference 18). Conditions: See reaction.notes.procedure_details. Workup: obtained
10.6084/m9.figshare.5104873.v1
null
Hydrazine.Ketone
Hydrazone
null
null
c1ccccc1.c1cc[se]c1
HO-
null
null
null
CC(=O)c1ccc[se]1.NNc1ccccc1>>CC(=NNc1ccccc1)c1ccc[se]1
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-c8e3bb374a104faca742086988b3b35f
CC(C)(C)NS(=O)(=O)c1sccc1Br.CCOC(=O)CF>>CC(C)(C)NS(=O)(=O)c1sccc1C(=O)CF
[Cl-].[NH4+].C(CCC)[Li].C(C)(C)(C)NS(=O)(=O)C=1SC=CC1Br.FCC(=O)OCC>>C(C)(C)(C)NS(=O)(=O)C=1SC=CC1C(CF)=O
Br[c:13]1[c:9]([S:6]([NH:5][C:2]([CH3:1])([CH3:3])[CH3:4])(=[O:7])=[O:8])[s:10][cH:11][cH:12]1.CCO[C:14](=[O:15])[CH2:16][F:17]>>[CH3:1][C:2]([CH3:3])([CH3:4])[NH:5][S:6](=[O:7])(=[O:8])[c:9]1[s:10][cH:11][cH:12][c:13]1[C:14](=[O:15])[CH2:16][F:17]
CC(C)(C)NS(=O)(=O)c1sccc1Br.CCOC(=O)CF
CC(C)(C)NS(=O)(=O)c1sccc1C(=O)CF
null
null
O1CCCC1.C(C)OC(C)=O
C-C Coupling
Ester and halide to ketone
a481c55deb0c41b36324f6d8384d9d1038aa77d83e68121861f48e3679e7d04d
7000e6fa6236297c1c515ebeaf5c7ba17704e006a4336e184f2503c0f1949baf
c1ccsc1
Br-[c;H0;D3;+0:1]1:[c:2]:[c:3]:[#16;a:4]:[c:5]:1-[#16:6].C-C-O-[C;H0;D3;+0:7](=[O;D1;H0:8])-[C:9]-[F;D1;H0:10]>>[#16:6]-[c:5]1:[#16;a:4]:[c:3]:[c:2]:[c;H0;D3;+0:1]:1-[C;H0;D3;+0:7](=[O;D1;H0:8])-[C:9]-[F;D1;H0:10]
72
[{"value": 72.0, "product": "C(C)(C)(C)NS(=O)(=O)C=1SC=CC1C(CF)=O", "details": "PERCENTYIELD", "is_desired": false}]
-78
CELSIUS
10
MINUTE
2.98 g (0.0mole) of N-t-butyl-3-bromo-2-thiophenesulfonamide was dissolved in 50mi of dry tetrahydrofuran and the mixture was cooled to -78° C. under nitrogen gas. To the reaction solution was slowly added dropwise 8.4 ml of n-butyl lithium (2.5N) and then the temperature of the mixture was raised slowly to -20° C. and...
10.6084/m9.figshare.5104873.v1
null
Aromatic halide.Ester
Ketone
c1ccsc1
c1ccsc1
c1ccsc1
HBr
O1CCCC1.C(C)OC(C)=O
-78
0.166667
CC(C)(C)NS(=O)(=O)c1sccc1Br.CCOC(=O)CF>O1CCCC1.C(C)OC(C)=O>CC(C)(C)NS(=O)(=O)c1sccc1C(=O)CF
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-79a672ca3eff441b932b12489c10964b
CC(=O)OC(CF)c1ccsc1S(=O)(=O)NC(C)(C)C>>CC(=O)OC(CF)c1ccsc1S(N)(=O)=O
C(C)(C)(C)NS(=O)(=O)C=1SC=CC1C(CF)OC(C)=O>>C(C)(=O)OC(CF)C1=C(SC=C1)S(=O)(=O)N
CC(C)(C)[NH:14][S:13]([c:12]1[c:8]([CH:5]([O:4][C:2]([CH3:1])=[O:3])[CH2:6][F:7])[cH:9][cH:10][s:11]1)(=[O:15])=[O:16]>>[CH3:1][C:2](=[O:3])[O:4][CH:5]([CH2:6][F:7])[c:8]1[cH:9][cH:10][s:11][c:12]1[S:13]([NH2:14])(=[O:15])=[O:16]
CC(=O)OC(CF)c1ccsc1S(=O)(=O)NC(C)(C)C
CC(=O)OC(CF)c1ccsc1S(N)(=O)=O
null
null
FC(C(=O)O)(F)F
Deprotection
Tert-butyl deprotection of amine
f7e1da1b4c254f1e6d5afbf8cb56733a4fabd145b80e971e3b7e31007de9e7d6
278d0fb11b582c058ac903379d7fbe11ab8c395937a204965031cf0c344845a9
c1ccsc1
C-C(-C)(-C)-[NH;D2;+0:1]-[#16:2](=[O;D1;H0:3])(=[O;D1;H0:4])-[c:5]:[#16;a:6]>>[#16;a:6]:[c:5]-[#16:2](-[NH2;D1;+0:1])(=[O;D1;H0:3])=[O;D1;H0:4]
74
[{"value": 74.0, "product": "C(C)(=O)OC(CF)C1=C(SC=C1)S(=O)(=O)N", "details": "PERCENTYIELD", "is_desired": false}, {"value": 65.3, "product": "C(C)(=O)OC(CF)C1=C(SC=C1)S(=O)(=O)N", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
12
HOUR
1.4 g (0.0043 mole) of N-t-butyl-3-(1-aceoxy-2-fluoroethyl) -2-thiophenesulfonamide synthesized in Example 2 dissolved in 5 ml of trifluoroacetic acid. The reaction solution was stirred at normal temperature for 12 hours and then concentrated under reduced pressure. The residue was dissolved in methylene chloride and w...
10.6084/m9.figshare.5104873.v1
null
Sulfonamide
Sulfonamide
null
null
c1ccsc1
Other
FC(C(=O)O)(F)F
null
12
CC(=O)OC(CF)c1ccsc1S(=O)(=O)NC(C)(C)C>FC(C(=O)O)(F)F>CC(=O)OC(CF)c1ccsc1S(N)(=O)=O
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-9db8bda42ddd42569da026335543c4dd
COc1cc(OC)nc(NC(=O)NS(=O)(=O)c2sccc2C(CF)OC(C)=O)n1>>COc1cc(OC)nc(NC(=O)NS(=O)(=O)c2sccc2C(O)CF)n1
COC1=NC(=NC(=C1)OC)NC(=O)NS(=O)(=O)C=1SC=CC1C(CF)OC(C)=O.Cl>>COC1=NC(=NC(=C1)OC)NC(=O)NS(=O)(=O)C=1SC=CC1C(CF)O
CC(=O)[O:23][CH:22]([c:21]1[c:17]([S:14]([NH:13][C:11]([NH:10][c:9]2[n:8][c:5]([O:6][CH3:7])[cH:4][c:3]([O:2][CH3:1])[n:26]2)=[O:12])(=[O:15])=[O:16])[s:18][cH:19][cH:20]1)[CH2:24][F:25]>>[CH3:1][O:2][c:3]1[cH:4][c:5]([O:6][CH3:7])[n:8][c:9]([NH:10][C:11](=[O:12])[NH:13][S:14](=[O:15])(=[O:16])[c:17]2[s:18][cH:19][cH:2...
COc1cc(OC)nc(NC(=O)NS(=O)(=O)c2sccc2C(CF)OC(C)=O)n1
COc1cc(OC)nc(NC(=O)NS(=O)(=O)c2sccc2C(O)CF)n1
null
null
[OH-].[Na+]
Reduction
Hydrolysis or Hydrogenolysis of Carboxylic Esters or Thioesters
d7acfb2397f2b5b2a83b3bebf3698d6d984dd716982297f62a944222c79ce234
19dd58e0f83625e74b4b1375d88cb4c813ee60f593d812516d14eafc4ab68dc7
O=C(Nc1ncccn1)NS(=O)(=O)c1cccs1
C-C(=O)-[O;H0;D2;+0:1]-[C:2](-[C:3])-[c:4]:[c:5]:[#16;a:6]>>[#16;a:6]:[c:5]:[c:4]-[C:2](-[C:3])-[OH;D1;+0:1]
92
[{"value": 92.0, "product": "COC1=NC(=NC(=C1)OC)NC(=O)NS(=O)(=O)C=1SC=CC1C(CF)O", "details": "PERCENTYIELD", "is_desired": false}, {"value": 88.6, "product": "COC1=NC(=NC(=C1)OC)NC(=O)NS(=O)(=O)C=1SC=CC1C(CF)O", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
1
HOUR
650 mg (0.0015 mole) of N-[(4,6-dimethoxypyrimidin-2-yl)aminocarbonyl]-3-(1-acetoxy-2-fluoroethyl)-2-thiophenesulfonamide synthesized in Example 4 was dissolved in 5 ml of aqueous sodium hydroxide solution and then stirred at normal temperature for one hour. The reaction mixture was adjusted to pH4 by adding 5% aqueous...
10.6084/m9.figshare.5104873.v1
null
Ester
Secondary alcohol
null
null
c1cncnc1.c1ccsc1
HO-
[OH-].[Na+]
null
1
COc1cc(OC)nc(NC(=O)NS(=O)(=O)c2sccc2C(CF)OC(C)=O)n1>[OH-].[Na+]>COc1cc(OC)nc(NC(=O)NS(=O)(=O)c2sccc2C(O)CF)n1
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-5c044a04ef604d88b3d7ec14794c7e4f
CC(C)(C)NS(=O)(=O)c1sccc1Br.CCOC(C)=O.[Cl-]>>CC(C)(C)NS(=O)(=O)c1sccc1C(=O)CCl
[Cl-].[NH4+].C(C)(C)(C)NS(=O)(=O)C=1SC=CC1Br.C(CCC)[Li].C(C)(=O)OCC>>C(C)(C)(C)NS(=O)(=O)C=1SC=CC1C(CCl)=O
Br[c:13]1[c:9]([S:6]([NH:5][C:2]([CH3:1])([CH3:3])[CH3:4])(=[O:7])=[O:8])[s:10][cH:11][cH:12]1.CCO[C:14](=[O:15])[CH3:16].[Cl-:17]>>[CH3:1][C:2]([CH3:3])([CH3:4])[NH:5][S:6](=[O:7])(=[O:8])[c:9]1[s:10][cH:11][cH:12][c:13]1[C:14](=[O:15])[CH2:16][Cl:17]
CC(C)(C)NS(=O)(=O)c1sccc1Br.CCOC(C)=O.[Cl-]
CC(C)(C)NS(=O)(=O)c1sccc1C(=O)CCl
null
null
null
C-C Coupling
OtherReaction
994f613feb8d69c965236a0912f4ded4253ad1b80700d1fc60d11a6088329101
b1c6261a734e53f4d91124624572b6ba9cd441d22cf9cb23410c5e92b65787c3
c1ccsc1
Br-[c;H0;D3;+0:1]1:[c:2]:[c:3]:[#16;a:4]:[c:5]:1-[#16:6].C-C-O-[C;H0;D3;+0:7](-[CH3;D1;+0:8])=[O;D1;H0:9].[Cl-;H0;D0:10]>>[#16:6]-[c:5]1:[#16;a:4]:[c:3]:[c:2]:[c;H0;D3;+0:1]:1-[C;H0;D3;+0:7](=[O;D1;H0:9])-[CH2;D2;+0:8]-[Cl;H0;D1;+0:10]
69
[{"value": 69.0, "product": "C(C)(C)(C)NS(=O)(=O)C=1SC=CC1C(CCl)=O", "details": "PERCENTYIELD", "is_desired": false}]
-78
CELSIUS
10
MINUTE
2.98 g (0.0| mole) of N-t-butyl-3-bromo-2-thiophenesulfonamide was dissolved in 50 ml of dry tetrahydrofura mixture was cooled to -78° C. under nitrogen gas. To the reaction solution was slowly added dropwise 8.4 ml of n-butyl lithium(2.5N) and then the temperature of the mixture was raised slowly to -20° C. and again ...
10.6084/m9.figshare.5104873.v1
null
Aromatic halide.Ester
Primary halide.Ketone
c1ccsc1
c1ccsc1
c1ccsc1
HBr
null
-78
0.166667
CC(C)(C)NS(=O)(=O)c1sccc1Br.CCOC(C)=O.[Cl-]>>CC(C)(C)NS(=O)(=O)c1sccc1C(=O)CCl
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-c101707cc7784ad6a6ce1b59640d7a42
CC(=O)O.CC(C)(C)NS(=O)(=O)c1sccc1C(=O)CCl>>CC(=O)OC(CCl)c1ccsc1S(=O)(=O)NC(C)(C)C
C(C)(C)(C)NS(=O)(=O)C=1SC=CC1C(CCl)=O.C(C)(=O)O.C(#N)[BH3-].[Na+]>>C(C)(C)(C)NS(=O)(=O)C=1SC=CC1C(CCl)OC(C)=O
[CH3:1][C:2](=[O:3])[OH:4].O=[C:5]([CH2:6][Cl:7])[c:8]1[cH:9][cH:10][s:11][c:12]1[S:13](=[O:14])(=[O:15])[NH:16][C:17]([CH3:18])([CH3:19])[CH3:20]>>[CH3:1][C:2](=[O:3])[O:4][CH:5]([CH2:6][Cl:7])[c:8]1[cH:9][cH:10][s:11][c:12]1[S:13](=[O:14])(=[O:15])[NH:16][C:17]([CH3:18])([CH3:19])[CH3:20]
CC(=O)O.CC(C)(C)NS(=O)(=O)c1sccc1C(=O)CCl
CC(=O)OC(CCl)c1ccsc1S(=O)(=O)NC(C)(C)C
null
null
O1CCCC1
Heteroatom Alkylation and Arylation
OtherReaction
ce3fcb13cd756b3d5007891f978a84ff044dea1b4fc6d85c30cb98a72771d8c9
1e6b32c40735d9503c42bed07f902336208e3af52b7e21f1c270af60c351b6a9
c1ccsc1
O=[C;H0;D3;+0:1](-[C:2]-[Cl;D1;H0:3])-[c:4]1:[c:5]:[c:6]:[#16;a:7]:[c:8]:1-[#16:9].[C;D1;H3:10]-[C:11](=[O;D1;H0:12])-[OH;D1;+0:13]>>[#16:9]-[c:8]1:[#16;a:7]:[c:6]:[c:5]:[c:4]:1-[CH;D3;+0:1](-[C:2]-[Cl;D1;H0:3])-[O;H0;D2;+0:13]-[C:11](-[C;D1;H3:10])=[O;D1;H0:12]
84
[{"value": 84.0, "product": "C(C)(C)(C)NS(=O)(=O)C=1SC=CC1C(CCl)OC(C)=O", "details": "PERCENTYIELD", "is_desired": false}]
null
null
30
MINUTE
1.5 g (0.005 mole) of N-t-butyl-3-(chloroacetyl)-2-thiophenesulfonamide synthesized in Example 6 was dissolved in the combined solution of 1 ml of acetic acid and 10 ml of tetrahydrofuran and then 0.31 g (0.005 mole) of sodium cyanoborohydride was added slowly thereto. The reaction solution was stirred at normal temper...
10.6084/m9.figshare.5104873.v1
null
Carboxylic acid.Ketone
Ester
null
null
c1ccsc1
Other
O1CCCC1
null
0.5
CC(=O)O.CC(C)(C)NS(=O)(=O)c1sccc1C(=O)CCl>O1CCCC1>CC(=O)OC(CCl)c1ccsc1S(=O)(=O)NC(C)(C)C
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-8f3db3635526422b993dd23dd01d5b7e
CC(=O)OC(CCl)c1ccsc1S(=O)(=O)NC(C)(C)C>>CC(=O)OC(CCl)c1ccsc1S(N)(=O)=O
C(C)(C)(C)NS(=O)(=O)C=1SC=CC1C(CCl)OC(C)=O>>C(C)(=O)OC(CCl)C1=C(SC=C1)S(=O)(=O)N
CC(C)(C)[NH:14][S:13]([c:12]1[c:8]([CH:5]([O:4][C:2]([CH3:1])=[O:3])[CH2:6][Cl:7])[cH:9][cH:10][s:11]1)(=[O:15])=[O:16]>>[CH3:1][C:2](=[O:3])[O:4][CH:5]([CH2:6][Cl:7])[c:8]1[cH:9][cH:10][s:11][c:12]1[S:13]([NH2:14])(=[O:15])=[O:16]
CC(=O)OC(CCl)c1ccsc1S(=O)(=O)NC(C)(C)C
CC(=O)OC(CCl)c1ccsc1S(N)(=O)=O
null
null
FC(C(=O)O)(F)F
Deprotection
Tert-butyl deprotection of amine
f7e1da1b4c254f1e6d5afbf8cb56733a4fabd145b80e971e3b7e31007de9e7d6
278d0fb11b582c058ac903379d7fbe11ab8c395937a204965031cf0c344845a9
c1ccsc1
C-C(-C)(-C)-[NH;D2;+0:1]-[#16:2](=[O;D1;H0:3])(=[O;D1;H0:4])-[c:5]:[#16;a:6]>>[#16;a:6]:[c:5]-[#16:2](-[NH2;D1;+0:1])(=[O;D1;H0:3])=[O;D1;H0:4]
72
[{"value": 72.0, "product": "C(C)(=O)OC(CCl)C1=C(SC=C1)S(=O)(=O)N", "details": "PERCENTYIELD", "is_desired": false}, {"value": 60.9, "product": "C(C)(=O)OC(CCl)C1=C(SC=C1)S(=O)(=O)N", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
12
HOUR
1.5 g (0.0044 mole) of N-t-butyl-3-(1-acetoxy-2-chloroethyl)-2-thiophenesulfonamide synthesized in Example 7 was dissolved in 5 ml of trifluoroacetic acid. The reaction solution was stirred at normal temperature for 12 hours and then concentrated under reduced pressure. The residue was dissolved in methylene chloride a...
10.6084/m9.figshare.5104873.v1
null
Sulfonamide
Sulfonamide
null
null
c1ccsc1
Other
FC(C(=O)O)(F)F
null
12
CC(=O)OC(CCl)c1ccsc1S(=O)(=O)NC(C)(C)C>FC(C(=O)O)(F)F>CC(=O)OC(CCl)c1ccsc1S(N)(=O)=O
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-340aa7277cd54868a6996a4b34326397
Cc1cc(OCc2ccccc2)nc(S(C)(=O)=O)n1.O>>Cc1cc(OCc2ccccc2)nc(Oc2ccccc2)n1
C(C1=CC=CC=C1)OC1=NC(=NC(=C1)C)S(=O)(=O)C.O>>C(C1=CC=CC=C1)OC1=NC(=NC(=C1)C)OC1=CC=CC=C1
O=S(=O)([CH3:9])[c:14]1[n:13][c:4]([O:5][CH2:6][c:7]2[cH:8][cH:20][cH:19][cH:18][cH:17]2)[cH:3][c:2]([CH3:1])[n:22]1.[OH2:15]>>[CH3:1][c:2]1[cH:3][c:4]([O:5][CH2:6][c:7]2[cH:8][cH:9][cH:10][cH:11][cH:12]2)[n:13][c:14]([O:15][c:16]2[cH:17][cH:18][cH:19][cH:20][cH:21]2)[n:22]1
Cc1cc(OCc2ccccc2)nc(S(C)(=O)=O)n1.O
Cc1cc(OCc2ccccc2)nc(Oc2ccccc2)n1
null
null
null
Aromatic Heterocycle Formation
OtherReaction
c689982e41cd1d37c1f084c2daae8093d19f2c277f9d78b556a3773c4e91063c
219ffa44079bee6997e244f956e9a60496f0a5398aca07eea3c14372279af105
c1ccc(COc2ccnc(Oc3ccccc3)n2)cc1
O=S(=O)(-[CH3;D1;+0:1])-[c;H0;D3;+0:2](:[#7;a:3]:[c:4]-[#8:5]-[C:6]-[c;H0;D3;+0:7]1:[cH;D2;+0:8]:[c:9]:[c:10]:[cH;D2;+0:11]:[cH;D2;+0:12]:1):[#7;a:13]:[c:14].[OH2;D0;+0:15]>>[c:14]:[#7;a:13]:[c;H0;D3;+0:2](-[O;H0;D2;+0:15]-[c:16]1:[c:17]:[cH;D2;+0:11]:[c:10]:[c:9]:[cH;D2;+0:8]:1):[#7;a:3]:[c:4]-[#8:5]-[C:6]-[c;H0;D3;+0...
null
[]
null
null
null
null
4-Benzyloxy-6-methyl-2-(methylsulfonyl)pyrimidine (Compound II-4) (0.45 g, 0.00162 mol) was added thereto and the resulting solution was allowed to react for about 2 hours at room temperature. The reaction solution was poured into water and extracted with ethyl acetate to separate an organic phase. The obtained organic...
10.6084/m9.figshare.5104873.v1
null
Sulfone
Ether
c1cncnc1.c1ccccc1
c1cncnc1.c1ccccc1.c1ccccc1
c1cncnc1.c1ccccc1.c1ccccc1
null
null
null
null
Cc1cc(OCc2ccccc2)nc(S(C)(=O)=O)n1.O>>Cc1cc(OCc2ccccc2)nc(Oc2ccccc2)n1
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-28a790364d3a4b39a6924f5c3d8fb5d8
CCOC(=O)C(CC)C(=O)OCC.N=C(N)c1ccccc1>>CCc1c(O)nc(-c2ccccc2)[nH]c1=O
O.Cl.C(C1=CC=CC=C1)(=N)N.C[O-].[Na+].C(C)C(C(=O)OCC)C(=O)OCC>>C(C)C=1C(NC(=NC1O)C1=CC=CC=C1)=O
CCO[C:4]([CH:3]([CH2:2][CH3:1])[C:15](OCC)=[O:16])=[O:5].[NH2:6][C:7]([c:8]1[cH:9][cH:10][cH:11][cH:12][cH:13]1)=[NH:14]>>[CH3:1][CH2:2][c:3]1[c:4]([OH:5])[n:6][c:7](-[c:8]2[cH:9][cH:10][cH:11][cH:12][cH:13]2)[nH:14][c:15]1=[O:16]
CCOC(=O)C(CC)C(=O)OCC.N=C(N)c1ccccc1
CCc1c(O)nc(-c2ccccc2)[nH]c1=O
null
null
CO
Aromatic Heterocycle Formation
OtherReaction
553c150cdd7dbd0db0d6f297863528c29c608f3b73363412a40d575e164d9836
b58423f9a2609746931edd2eb094cfdeeb7a95a2e60efda9d73e9e5239e8be6a
O=c1ccnc(-c2ccccc2)[nH]1
C-C-O-[C;H0;D3;+0:1](=[O;D1;H0:2])-[CH;D3;+0:3](-[C:4]-[C;D1;H3:5])-[C;H0;D3;+0:6](=[O;H0;D1;+0:7])-O-C-C.[NH2;D1;+0:8]-[C;H0;D3;+0:9](=[NH;D1;+0:10])-[c;H0;D3;+0:11](:[c:12]:[c:13]):[c:14]:[c:15]>>[C;D1;H3:5]-[C:4]-[c;H0;D3;+0:3]1:[c;H0;D3;+0:1](=[O;D1;H0:2]):[nH;D2;+0:10]:[c;H0;D3;+0:9](-[c;H0;D3;+0:11](:[c:12]:[c:13...
51
[{"value": 51.0, "product": "C(C)C=1C(NC(=NC1O)C1=CC=CC=C1)=O", "details": "PERCENTYIELD", "is_desired": false}, {"value": 50.9, "product": "C(C)C=1C(NC(=NC1O)C1=CC=CC=C1)=O", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
null
null
A mixture of 45.19 g (0.29 mol) of benzamidine hydrochloride hydrate, 127.42 g (0.59 mol) of 25% sodium methoxide in methanol, 55 mL (0.29 mol) of diethyl ethylmalonate and 175 mL of methanol was heated at reflux for 25 h. The mixture was rotovapped to remove the bulk of the methanol. The residue was diluted with 300 m...
10.6084/m9.figshare.5104873.v1
null
Ester.Ester.Primary amine
Aromatic alcohol
null
c1cncnc1
c1cncnc1.c1ccccc1
HO-
CO
null
null
CCOC(=O)C(CC)C(=O)OCC.N=C(N)c1ccccc1>CO>CCc1c(O)nc(-c2ccccc2)[nH]c1=O
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-2b0378d7412b4bedb3ed0ed2242b2a38
CCOC(=O)C=C(OCC)OCC.N=C(N)c1ccccc1>>CCOc1cc(=O)[nH]c(-c2ccccc2)n1
O.Cl.C(C1=CC=CC=C1)(=N)N.C(C)(=O)[O-].[Na+].C(C)OC(=CC(=O)OCC)OCC.CS(=O)C>>C(C)OC1=CC(NC(=N1)C1=CC=CC=C1)=O
CCO[C:4]([O:3][CH2:2][CH3:1])=[CH:5][C:6](OCC)=[O:7].[NH2:8][C:9]([c:10]1[cH:11][cH:12][cH:13][cH:14][cH:15]1)=[NH:16]>>[CH3:1][CH2:2][O:3][c:4]1[cH:5][c:6](=[O:7])[nH:8][c:9](-[c:10]2[cH:11][cH:12][cH:13][cH:14][cH:15]2)[n:16]1
CCOC(=O)C=C(OCC)OCC.N=C(N)c1ccccc1
CCOc1cc(=O)[nH]c(-c2ccccc2)n1
null
null
[OH-].[Na+]
Aromatic Heterocycle Formation
OtherReaction
d82f9c458402682e7644f99b62399f0511f124c6e3c1753a992ae84d9bea89bd
82419e8808bf7ff4652f96c8cdfae6e968629b2d91d425ed75997b61827b36d9
O=c1ccnc(-c2ccccc2)[nH]1
C-C-O-[C;H0;D3;+0:1](-[#8:2]-[C:3])=[CH;D2;+0:4]-[C;H0;D3;+0:5](=[O;D1;H0:6])-O-C-C.[NH2;D1;+0:7]-[C;H0;D3;+0:8](=[NH;D1;+0:9])-[c;H0;D3;+0:10](:[c:11]:[c:12]):[c:13]:[c:14]>>[C:3]-[#8:2]-[c;H0;D3;+0:1]1:[cH;D2;+0:4]:[c;H0;D3;+0:5](=[O;D1;H0:6]):[nH;D2;+0:7]:[c;H0;D3;+0:8](-[c;H0;D3;+0:10](:[c:11]:[c:12]):[c:13]:[c:14]...
57
[{"value": 57.0, "product": "C(C)OC1=CC(NC(=N1)C1=CC=CC=C1)=O", "details": "PERCENTYIELD", "is_desired": false}, {"value": 52.7, "product": "C(C)OC1=CC(NC(=N1)C1=CC=CC=C1)=O", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
120
CELSIUS
null
null
A mixture of 3.14 g (20.0 mmol) of benzamidine hydrochloride hydrate, 1.65 g (20.1 mmol) of powdered anhydrous sodium acetate, 4.17 g (22.2 mmol) of ethyl 3,3-diethoxyacrylate and 10 mL of DMSO was heated at 120° C. for 8 h. The mixture was cooled, diluted with 50 mL of 5% aqueous NaOH and washed with two 100 mL portio...
10.6084/m9.figshare.5104873.v1
null
Ester.Ether.Ether.Primary amine
Ether
null
c1ccncn1
c1ccncn1.c1ccccc1
HO-
[OH-].[Na+]
120
null
CCOC(=O)C=C(OCC)OCC.N=C(N)c1ccccc1>[OH-].[Na+]>CCOc1cc(=O)[nH]c(-c2ccccc2)n1
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-b051943e828a4e248c90cd25b0c51782
CCc1c(Br)nc(-c2ccccc2)nc1Br.O=S(=O)(O)O>>CCc1c(Br)nc(-c2ccccc2)[nH]c1=O
S(O)(O)(=O)=O.BrC1=NC(=NC(=C1CC)Br)C1=CC=CC=C1>>BrC1=C(C(NC(=N1)C1=CC=CC=C1)=O)CC
Br[c:15]1[c:3]([CH2:2][CH3:1])[c:4]([Br:5])[n:6][c:7](-[c:8]2[cH:9][cH:10][cH:11][cH:12][cH:13]2)[n:14]1.O=S(=O)(O)[OH:16]>>[CH3:1][CH2:2][c:3]1[c:4]([Br:5])[n:6][c:7](-[c:8]2[cH:9][cH:10][cH:11][cH:12][cH:13]2)[nH:14][c:15]1=[O:16]
CCc1c(Br)nc(-c2ccccc2)nc1Br.O=S(=O)(O)O
CCc1c(Br)nc(-c2ccccc2)[nH]c1=O
null
null
O
Heteroatom Alkylation and Arylation
OtherReaction
42c44ba822f4055de2d24d5b39b754d7dda39adf52a0688a4a8eae47fd02626c
e3660767655c50df0f92afc78c794dd2af7cf646bf1430960eafd30c23bf3fa7
O=c1ccnc(-c2ccccc2)[nH]1
Br-[c;H0;D3;+0:1]1:[n;H0;D2;+0:2]:[c:3](-[c:4]):[#7;a:5]:[c:6](-[Br;D1;H0:7]):[c:8]:1-[C:9].O-S(=O)(=O)-[OH;D1;+0:10]>>[Br;D1;H0:7]-[c:6]1:[#7;a:5]:[c:3](-[c:4]):[nH;D2;+0:2]:[c;H0;D3;+0:1](=[O;H0;D1;+0:10]):[c:8]:1-[C:9]
99
[{"value": 99.0, "product": "BrC1=C(C(NC(=N1)C1=CC=CC=C1)=O)CC", "details": "PERCENTYIELD", "is_desired": false}]
null
null
18
HOUR
To 8.29 g (26.1 mmol) of crude 4,6-dibromo-5-ethyl-2-phenylpyrimidine was added a mixture of 4 mL of water and 15 mL of concentrated sulfuric acid. The mixture was stirred for 18 h and poured onto 200 g of crushed ice. After the ice had melted the precipitate was collected by filtration and dried under vacuum to afford...
10.6084/m9.figshare.5104873.v1
null
Aromatic halide
null
c1cncnc1
c1cncnc1
c1cncnc1.c1ccccc1
HBr
O
null
18
CCc1c(Br)nc(-c2ccccc2)nc1Br.O=S(=O)(O)O>O>CCc1c(Br)nc(-c2ccccc2)[nH]c1=O
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-2d447b7bc2ec4665ad48ac9de0170d06
O=C1CCC(=O)N1Br.O=c1cc(C(F)(F)F)nc(-c2ccccc2)[nH]1>>O=c1[nH]c(-c2ccccc2)nc(C(F)(F)F)c1Br
C1(=CC=CC=C1)C1=NC(=CC(N1)=O)C(F)(F)F.BrN1C(CCC1=O)=O>>BrC=1C(NC(=NC1C(F)(F)F)C1=CC=CC=C1)=O
O=C1CCC(=O)N1[Br:18].[O:1]=[c:2]1[nH:3][c:4](-[c:5]2[cH:6][cH:7][cH:8][cH:9][cH:10]2)[n:11][c:12]([C:13]([F:14])([F:15])[F:16])[cH:17]1>>[O:1]=[c:2]1[nH:3][c:4](-[c:5]2[cH:6][cH:7][cH:8][cH:9][cH:10]2)[n:11][c:12]([C:13]([F:14])([F:15])[F:16])[c:17]1[Br:18]
O=C1CCC(=O)N1Br.O=c1cc(C(F)(F)F)nc(-c2ccccc2)[nH]1
O=c1[nH]c(-c2ccccc2)nc(C(F)(F)F)c1Br
null
null
CC(=O)OCC1=C2C=CC=CC2=C(C3=CC=CC=C31)COC(=O)C
Functional Group Interconversion
Bromination
c1f267498588fdc78d70fa059a48254fc6fd3441a5bb656fda4935ce99f2babe
0e444576b73669992a4073cc3f7b10ed52cb9df09f9f8e4042e39e6a602aa390
O=c1ccnc(-c2ccccc2)[nH]1
O=C1-C-C-C(=O)-N-1-[Br;H0;D1;+0:1].[F;D1;H0:2]-[C:3](-[F;D1;H0:4])(-[F;D1;H0:5])-[c:6]1:[#7;a:7]:[c:8]:[#7;a:9]:[c:10](=[O;D1;H0:11]):[cH;D2;+0:12]:1>>[Br;H0;D1;+0:1]-[c;H0;D3;+0:12]1:[c:6](-[C:3](-[F;D1;H0:2])(-[F;D1;H0:4])-[F;D1;H0:5]):[#7;a:7]:[c:8]:[#7;a:9]:[c:10]:1=[O;D1;H0:11]
83.5
[{"value": 83.5, "product": "BrC=1C(NC(=NC1C(F)(F)F)C1=CC=CC=C1)=O", "details": "PERCENTYIELD", "is_desired": false}, {"value": 83.5, "product": "BrC=1C(NC(=NC1C(F)(F)F)C1=CC=CC=C1)=O", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
16
HOUR
To a solution of 1.0 g (3.94 mmol) of 2-phenyl-6-trifluoromethyl-4(3H)-pyrimidinone and 20 mL of glacial acetic add was added 1.0 g (5.6 mmol) N-bromosuccinimide and the mixture was left to stir at room temperature for 16 h. The reaction was poured onto ice water and vacuum filtered, washing well with water. The crude ...
10.6084/m9.figshare.5104873.v1
null
Tertiary amide.Tertiary amide
Aromatic halide
C1CCNC1.c1ccncn1
c1cncnc1
c1cncnc1.c1ccccc1
HO-
CC(=O)OCC1=C2C=CC=CC2=C(C3=CC=CC=C31)COC(=O)C
null
16
O=C1CCC(=O)N1Br.O=c1cc(C(F)(F)F)nc(-c2ccccc2)[nH]1>CC(=O)OCC1=C2C=CC=CC2=C(C3=CC=CC=C31)COC(=O)C>O=c1[nH]c(-c2ccccc2)nc(C(F)(F)F)c1Br
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-f05000905bc748e98487d679b80f953b
O=C1CCC(=O)N1Br.O=c1cc(-c2ccccc2)nc(-c2ccccc2)[nH]1>>O=c1[nH]c(-c2ccccc2)nc(-c2ccccc2)c1Br
C1(=CC=CC=C1)C1=NC(=CC(N1)=O)C1=CC=CC=C1.BrN1C(CCC1=O)=O>>BrC=1C(NC(=NC1C1=CC=CC=C1)C1=CC=CC=C1)=O
O=C1CCC(=O)N1[Br:20].[O:1]=[c:2]1[nH:3][c:4](-[c:5]2[cH:6][cH:7][cH:8][cH:9][cH:10]2)[n:11][c:12](-[c:13]2[cH:14][cH:15][cH:16][cH:17][cH:18]2)[cH:19]1>>[O:1]=[c:2]1[nH:3][c:4](-[c:5]2[cH:6][cH:7][cH:8][cH:9][cH:10]2)[n:11][c:12](-[c:13]2[cH:14][cH:15][cH:16][cH:17][cH:18]2)[c:19]1[Br:20]
O=C1CCC(=O)N1Br.O=c1cc(-c2ccccc2)nc(-c2ccccc2)[nH]1
O=c1[nH]c(-c2ccccc2)nc(-c2ccccc2)c1Br
null
null
C(C)(=O)O
Functional Group Interconversion
Bromination
c1f267498588fdc78d70fa059a48254fc6fd3441a5bb656fda4935ce99f2babe
0e444576b73669992a4073cc3f7b10ed52cb9df09f9f8e4042e39e6a602aa390
O=c1cc(-c2ccccc2)nc(-c2ccccc2)[nH]1
O=C1-C-C-C(=O)-N-1-[Br;H0;D1;+0:1].[O;D1;H0:2]=[c:3]1:[#7;a:4]:[c:5]:[#7;a:6]:[c:7](-[c:8]):[cH;D2;+0:9]:1>>[Br;H0;D1;+0:1]-[c;H0;D3;+0:9]1:[c:7](-[c:8]):[#7;a:6]:[c:5]:[#7;a:4]:[c:3]:1=[O;D1;H0:2]
48.3
[{"value": 48.0, "product": "BrC=1C(NC(=NC1C1=CC=CC=C1)C1=CC=CC=C1)=O", "details": "PERCENTYIELD", "is_desired": false}, {"value": 48.3, "product": "BrC=1C(NC(=NC1C1=CC=CC=C1)C1=CC=CC=C1)=O", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
60
HOUR
To a suspension of 13.37 g (56 mmol) of 2,6-diphenyl-4(3H)-pyrimidinone and 200 mL glacial acetic acid was added 15.1 g (84.8 mmol) of N-bromosuccinimide and the mixture was left to stir at room temperature for 60 h. The reaction was poured onto 100 g crushed ice and vacuum filtered, washing well with water, then air d...
10.6084/m9.figshare.5104873.v1
null
Tertiary amide.Tertiary amide
Aromatic halide
C1CCNC1.c1ccncn1
c1cncnc1
c1cncnc1.c1ccccc1.c1ccccc1
HO-
C(C)(=O)O
null
60
O=C1CCC(=O)N1Br.O=c1cc(-c2ccccc2)nc(-c2ccccc2)[nH]1>C(C)(=O)O>O=c1[nH]c(-c2ccccc2)nc(-c2ccccc2)c1Br
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-be4d8163d3b146d0a463a6fc363aaeaa
CCc1cc(=O)[nH]c(-c2ccccc2)n1.II>>CCc1nc(-c2ccccc2)[nH]c(=O)c1I
C(C)C1=CC(NC(=N1)C1=CC=CC=C1)=O.[OH-].[Na+].II>>C(C)C1=C(C(NC(=N1)C1=CC=CC=C1)=O)I
[CH3:1][CH2:2][c:3]1[n:4][c:5](-[c:6]2[cH:7][cH:8][cH:9][cH:10][cH:11]2)[nH:12][c:13](=[O:14])[cH:15]1.I[I:16]>>[CH3:1][CH2:2][c:3]1[n:4][c:5](-[c:6]2[cH:7][cH:8][cH:9][cH:10][cH:11]2)[nH:12][c:13](=[O:14])[c:15]1[I:16]
CCc1cc(=O)[nH]c(-c2ccccc2)n1.II
CCc1nc(-c2ccccc2)[nH]c(=O)c1I
null
null
O
Functional Group Interconversion
OtherReaction
ab990d4cf4e29f4bfc1eed19f85a157586116cba28cf7e047e67e704b97886a0
3c4065ab4a8681675e06a527dcad54d701c7bfdcac9f73f87773b05034108934
O=c1ccnc(-c2ccccc2)[nH]1
I-[I;H0;D1;+0:1].[C:2]-[c:3]1:[#7;a:4]:[c:5]:[#7;a:6]:[c:7](=[O;D1;H0:8]):[cH;D2;+0:9]:1>>[C:2]-[c:3]1:[#7;a:4]:[c:5]:[#7;a:6]:[c:7](=[O;D1;H0:8]):[c;H0;D3;+0:9]:1-[I;H0;D1;+0:1]
94.5
[{"value": 75.0, "product": "C(C)C1=C(C(NC(=N1)C1=CC=CC=C1)=O)I", "details": "PERCENTYIELD", "is_desired": false}, {"value": 94.5, "product": "C(C)C1=C(C(NC(=N1)C1=CC=CC=C1)=O)I", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
50
CELSIUS
null
null
A mixture of 8.18 g (40.9 mmol) of 6-ethyl-2-phenyl-4(3H)-pyrimidinone, 1.68 g (42.0 mmol) of sodium hydroxide, 10.42 g (41.0 mmol) of iodine and 50 mL of water was heated at 50° C. for 4 h. The mixture was cooled and filtered. The white solid collected was dried in a vacuum oven to leave 12.60 g (75%) of 6-ethyl-5-iod...
10.6084/m9.figshare.5104873.v1
null
null
Aromatic halide
c1ccncn1
c1cncnc1
c1cncnc1.c1ccccc1
HI
O
50
null
CCc1cc(=O)[nH]c(-c2ccccc2)n1.II>O>CCc1nc(-c2ccccc2)[nH]c(=O)c1I
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-475d4575be964743a02cc9754560986f
CCc1cc(=O)[nH]c(-c2ccccc2)n1.O=C1CCC(=O)N1Cl>>CCc1nc(-c2ccccc2)[nH]c(=O)c1Cl
C(C)C1=CC(NC(=N1)C1=CC=CC=C1)=O.ClN1C(CCC1=O)=O>>ClC=1C(NC(=NC1CC)C1=CC=CC=C1)=O
[CH3:1][CH2:2][c:3]1[n:4][c:5](-[c:6]2[cH:7][cH:8][cH:9][cH:10][cH:11]2)[nH:12][c:13](=[O:14])[cH:15]1.O=C1CCC(=O)N1[Cl:16]>>[CH3:1][CH2:2][c:3]1[n:4][c:5](-[c:6]2[cH:7][cH:8][cH:9][cH:10][cH:11]2)[nH:12][c:13](=[O:14])[c:15]1[Cl:16]
CCc1cc(=O)[nH]c(-c2ccccc2)n1.O=C1CCC(=O)N1Cl
CCc1nc(-c2ccccc2)[nH]c(=O)c1Cl
null
null
C(C)(=O)O
Functional Group Interconversion
Chlorination
c1f267498588fdc78d70fa059a48254fc6fd3441a5bb656fda4935ce99f2babe
0e444576b73669992a4073cc3f7b10ed52cb9df09f9f8e4042e39e6a602aa390
O=c1ccnc(-c2ccccc2)[nH]1
O=C1-C-C-C(=O)-N-1-[Cl;H0;D1;+0:1].[C:2]-[c:3]1:[#7;a:4]:[c:5]:[#7;a:6]:[c:7](=[O;D1;H0:8]):[cH;D2;+0:9]:1>>[C:2]-[c:3]1:[#7;a:4]:[c:5]:[#7;a:6]:[c:7](=[O;D1;H0:8]):[c;H0;D3;+0:9]:1-[Cl;H0;D1;+0:1]
87.1
[{"value": 87.1, "product": "ClC=1C(NC(=NC1CC)C1=CC=CC=C1)=O", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
null
null
A stirred solution of 7.81 g (39.1 mmol) of 6-ethyl-2-phenyl-4(3H)-pyrimidinone and 5.80 g (43.4 mmol) of N-chlorosuccinimide in 100 mL of glacial acetic acid was heated at 90° C. for 4 h. The mixture was cooled, poured onto crushed ice and allowed to stand until the ice had melted. The mixture was filtered and the sol...
10.6084/m9.figshare.5104873.v1
null
Tertiary amide.Tertiary amide
Aromatic halide
c1ccncn1.C1CCNC1
c1cncnc1
c1cncnc1.c1ccccc1
HO-
C(C)(=O)O
null
null
CCc1cc(=O)[nH]c(-c2ccccc2)n1.O=C1CCC(=O)N1Cl>C(C)(=O)O>CCc1nc(-c2ccccc2)[nH]c(=O)c1Cl
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-d6194f9ae43e4fbd94964245b6b3d3e4
O=c1[nH]c(-c2ccccc2)nc(Oc2ccccc2)c1I>>O=c1cc(Oc2ccccc2)nc(-c2ccccc2)[nH]1
IC=1C(NC(=NC1OC1=CC=CC=C1)C1=CC=CC=C1)=O>>O(C1=CC=CC=C1)C1=CC(NC(=N1)C1=CC=CC=C1)=O
I[c:3]1[c:2](=[O:1])[nH:20][c:13](-[c:14]2[cH:15][cH:16][cH:17][cH:18][cH:19]2)[n:12][c:4]1[O:5][c:6]1[cH:7][cH:8][cH:9][cH:10][cH:11]1>>[O:1]=[c:2]1[cH:3][c:4]([O:5][c:6]2[cH:7][cH:8][cH:9][cH:10][cH:11]2)[n:12][c:13](-[c:14]2[cH:15][cH:16][cH:17][cH:18][cH:19]2)[nH:20]1
O=c1[nH]c(-c2ccccc2)nc(Oc2ccccc2)c1I
O=c1cc(Oc2ccccc2)nc(-c2ccccc2)[nH]1
null
[Zn].[Zn].[Zn]
C(C)(=O)O
Functional Group Interconversion
Aromatic dehalogenation
895159d874869aa7a3c29ba9f3a6fce27d4e3f1b326a7f3ea2a46c97ca88bc67
56de34d4a44cb25d9380269ee5e138b0f24b40a3a0db22c5508049dc775a861f
O=c1cc(Oc2ccccc2)nc(-c2ccccc2)[nH]1
I-[c;H0;D3;+0:1]1:[c:2](=[O;D1;H0:3]):[#7;a:4]:[c:5]:[#7;a:6]:[c:7]:1-[#8:8]>>[#8:8]-[c:7]1:[#7;a:6]:[c:5]:[#7;a:4]:[c:2](=[O;D1;H0:3]):[cH;D2;+0:1]:1
125.6
[{"value": 57.0, "product": "O(C1=CC=CC=C1)C1=CC(NC(=N1)C1=CC=CC=C1)=O", "details": "PERCENTYIELD", "is_desired": false}, {"value": 125.6, "product": "O(C1=CC=CC=C1)C1=CC(NC(=N1)C1=CC=CC=C1)=O", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
null
null
A mixture of 7.07 g (18.1 mmol) of crude 5-iodo-6-phenoxy-2-phenyl-4(3H)-pyrimidinone, 2.02 g (31.1 mmol) of zinc dust and 25 mL of glacial acetic acid was heated to reflux. After 15 min an additional 2.06 g (31.7 mmol) of zinc dust was added, followed 15 min later by a further 2.04 g (31.4 mmol) of zinc dust. The mixt...
10.6084/m9.figshare.5104873.v1
null
Aromatic halide
null
c1cncnc1
c1ccncn1
c1ccncn1.c1ccccc1.c1ccccc1
I-
[Zn].[Zn].[Zn].C(C)(=O)O
null
null
O=c1[nH]c(-c2ccccc2)nc(Oc2ccccc2)c1I>[Zn].[Zn].[Zn].C(C)(=O)O>O=c1cc(Oc2ccccc2)nc(-c2ccccc2)[nH]1
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-c70bc697c73a4481b3467e71a66893b5
C#CCn1c(-c2ccccc2)nc(C(=O)OCC)c(C)c1=O>>C#CCn1c(-c2ccccc2)nc(C(=O)O)c(C)c1=O
C(C)OC(=O)C1=C(C(N(C(=N1)C1=CC=CC=C1)CC#C)=O)C.[OH-].[Na+]>>C(=O)(O)C1=C(C(N(C(=N1)C1=CC=CC=C1)CC#C)=O)C
CC[O:16][C:14]([c:13]1[n:12][c:5](-[c:6]2[cH:7][cH:8][cH:9][cH:10][cH:11]2)[n:4]([CH2:3][C:2]#[CH:1])[c:19](=[O:20])[c:17]1[CH3:18])=[O:15]>>[CH:1]#[C:2][CH2:3][n:4]1[c:5](-[c:6]2[cH:7][cH:8][cH:9][cH:10][cH:11]2)[n:12][c:13]([C:14](=[O:15])[OH:16])[c:17]([CH3:18])[c:19]1=[O:20]
C#CCn1c(-c2ccccc2)nc(C(=O)OCC)c(C)c1=O
C#CCn1c(-c2ccccc2)nc(C(=O)O)c(C)c1=O
null
null
C(C)O.C1CCOC1
Deprotection
Ester saponification (alkyl deprotection)
d872e08ad5c85a4add6cd04e6e987e73fead5f79b3f30ba61a81ba5029b29894
38ae1ee78433b9acfb0390501446149c80f88f23ac2d84c60b3369bdab75cec9
O=c1ccnc(-c2ccccc2)[nH]1
C-C-[O;H0;D2;+0:1]-[C:2](=[O;D1;H0:3])-[c:4]:[#7;a:5]>>[#7;a:5]:[c:4]-[C:2](=[O;D1;H0:3])-[OH;D1;+0:1]
53.2
[{"value": 53.0, "product": "C(=O)(O)C1=C(C(N(C(=N1)C1=CC=CC=C1)CC#C)=O)C", "details": "PERCENTYIELD", "is_desired": false}, {"value": 53.2, "product": "C(=O)(O)C1=C(C(N(C(=N1)C1=CC=CC=C1)CC#C)=O)C", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
24
HOUR
To a solution of 1.81 g (6.1 mmol) of 6-ethoxycarbonyl-5-methyl-2-phenyl-3-propargyl-4(3H)-pyrimidinone in 100 mL of ethanol and 50 mL of THF was added 50 mL of 5% aqueous sodium hydroxide. The mixture was stirred at room temperature for 24 h and rotovapped to remove the bulk of the organic solvents. The residue was di...
10.6084/m9.figshare.5104873.v1
null
Ester
Carboxylic acid
null
null
c1cncnc1.c1ccccc1
Other
C(C)O.C1CCOC1
null
24
C#CCn1c(-c2ccccc2)nc(C(=O)OCC)c(C)c1=O>C(C)O.C1CCOC1>C#CCn1c(-c2ccccc2)nc(C(=O)O)c(C)c1=O
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-21393e26ab0b4c64a67d4dbe4b4c6328
C#CCn1c(-c2ccccc2)nc(C(=O)O)c(C)c1=O.CNC>>C#CCn1c(-c2ccccc2)nc(C(=O)N(C)C)c(C)c1=O
C(=O)(O)C1=C(C(N(C(=N1)C1=CC=CC=C1)CC#C)=O)C.Cl.CNC.N1=CC=CC=C1.C1(CCCCC1)N=C=NC1CCCCC1>>CN(C(=O)C1=C(C(N(C(=N1)C1=CC=CC=C1)CC#C)=O)C)C
O[C:14]([c:13]1[n:12][c:5](-[c:6]2[cH:7][cH:8][cH:9][cH:10][cH:11]2)[n:4]([CH2:3][C:2]#[CH:1])[c:21](=[O:22])[c:19]1[CH3:20])=[O:15].[NH:16]([CH3:17])[CH3:18]>>[CH:1]#[C:2][CH2:3][n:4]1[c:5](-[c:6]2[cH:7][cH:8][cH:9][cH:10][cH:11]2)[n:12][c:13]([C:14](=[O:15])[N:16]([CH3:17])[CH3:18])[c:19]([CH3:20])[c:21]1=[O:22]
C#CCn1c(-c2ccccc2)nc(C(=O)O)c(C)c1=O.CNC
C#CCn1c(-c2ccccc2)nc(C(=O)N(C)C)c(C)c1=O
null
null
C1CCOC1
Acylation
Acylation of Nitrogen Nucleophiles by Carboxylic Acids
ac72df6259d5d7baee7abdbd4706ef4b4627f86ead9dc94f0cefcfcb37c21def
c5e4172490b2731ba9322b68af56376edadc31ce0bb9a3dfdea23a1817a852fd
O=c1ccnc(-c2ccccc2)[nH]1
O-[C;H0;D3;+0:1](=[O;D1;H0:2])-[c:3]1:[#7;a:4]:[c:5]:[#7;a:6]:[c:7]:[c:8]:1.[C;D1;H3:9]-[NH;D2;+0:10]-[C;D1;H3:11]>>[C;D1;H3:9]-[N;H0;D3;+0:10](-[C;D1;H3:11])-[C;H0;D3;+0:1](=[O;D1;H0:2])-[c:3]1:[#7;a:4]:[c:5]:[#7;a:6]:[c:7]:[c:8]:1
32
[{"value": 32.0, "product": "CN(C(=O)C1=C(C(N(C(=N1)C1=CC=CC=C1)CC#C)=O)C)C", "details": "PERCENTYIELD", "is_desired": false}, {"value": 31.7, "product": "CN(C(=O)C1=C(C(N(C(=N1)C1=CC=CC=C1)CC#C)=O)C)C", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
4
DAY
To a stirred solution of 0.87 g (3.2 mmol) of crude 6-carboxy-5-methyl-2-phenyl-3-propargyl-4(3H)-pyrimidinone, 0.32 g (3.9 mmol) of dimethylamine hydrochloride and 2 mL of pyridine in 10 mL of THF was added 0.74 g (3.6 mmol) of solid N,N'-dicyclohexylcarbodiimide. The mixture was stirred at room temperature for 4 days...
10.6084/m9.figshare.5104873.v1
null
Carboxylic acid.Secondary amine
Tertiary amide
null
null
c1cncnc1.c1ccccc1
HO-
C1CCOC1
null
96
C#CCn1c(-c2ccccc2)nc(C(=O)O)c(C)c1=O.CNC>C1CCOC1>C#CCn1c(-c2ccccc2)nc(C(=O)N(C)C)c(C)c1=O
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-c771bb9653f84a339085fb2d456f388e
C#CCn1c(-c2ccccc2)nc(Cl)c(C)c1=O.CNC>>C#CCn1c(-c2ccccc2)nc(N(C)C)c(C)c1=O
ClC1=C(C(N(C(=N1)C1=CC=CC=C1)CC#C)=O)C.CNC>>CN(C1=C(C(N(C(=N1)C1=CC=CC=C1)CC#C)=O)C)C
Cl[c:13]1[n:12][c:5](-[c:6]2[cH:7][cH:8][cH:9][cH:10][cH:11]2)[n:4]([CH2:3][C:2]#[CH:1])[c:19](=[O:20])[c:17]1[CH3:18].[NH:14]([CH3:15])[CH3:16]>>[CH:1]#[C:2][CH2:3][n:4]1[c:5](-[c:6]2[cH:7][cH:8][cH:9][cH:10][cH:11]2)[n:12][c:13]([N:14]([CH3:15])[CH3:16])[c:17]([CH3:18])[c:19]1=[O:20]
C#CCn1c(-c2ccccc2)nc(Cl)c(C)c1=O.CNC
C#CCn1c(-c2ccccc2)nc(N(C)C)c(C)c1=O
null
null
CCOCC.O1CCCC1
Heteroatom Alkylation and Arylation
Ullmann-Goldberg Substitution amine
8a13b42f4b06102b68f4963e65202071bf1d0630fbad1b11bbd8e99b9f9c8f34
b6b8e2cdb45054a35f5e8157d624f852c0601a09401556706e166b19536eb7a7
O=c1ccnc(-c2ccccc2)[nH]1
Cl-[c;H0;D3;+0:1]1:[#7;a:2]:[c:3]:[#7;a:4](-[C:5]-[C:6]#[C;D1;H1:7]):[c:8](=[O;D1;H0:9]):[c:10]:1-[C;D1;H3:11].[C;D1;H3:12]-[NH;D2;+0:13]-[C;D1;H3:14]>>[C;D1;H1:7]#[C:6]-[C:5]-[#7;a:4]1:[c:3]:[#7;a:2]:[c;H0;D3;+0:1](-[N;H0;D3;+0:13](-[C;D1;H3:12])-[C;D1;H3:14]):[c:10](-[C;D1;H3:11]):[c:8]:1=[O;D1;H0:9]
null
[]
null
null
null
null
To an ice cooled solution of 1.5 g (3.8 mmol) 6-chloro-5-methyl-2-phenyl-3-propargyl-4(3H)-pyrimidinone in 4 mL of tetrahydrofuran, was added 22 mL (99 mmol) of 4.5M dimethylamine in ether portionwise (2-4 mL) over a period of 7 days. The reaction mixture was allowed to warm and stir at room temperature after each addi...
10.6084/m9.figshare.5104873.v1
null
Aromatic halide.Secondary amine
Tertiary amine
c1cncnc1
c1cncnc1
c1cncnc1.c1ccccc1
HCl
CCOCC.O1CCCC1
null
null
C#CCn1c(-c2ccccc2)nc(Cl)c(C)c1=O.CNC>CCOCC.O1CCCC1>C#CCn1c(-c2ccccc2)nc(N(C)C)c(C)c1=O
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-1591768695574e68b20ca645245f4562
C#CCn1c(-c2ccccc2)nc(C(F)(F)F)c(CC)c1=O.[OH-]>>CCc1c(C(F)(F)F)nc(-c2ccccc2)n(CC(C)=O)c1=O
C(C)C=1C(N(C(=NC1C(F)(F)F)C1=CC=CC=C1)CC#C)=O.C(C)C=1C(N(C(=NC1C(F)(F)F)C1=CC=CC=C1)CC#C)=O.[OH-].[Na+]>>C(C)C=1C(N(C(=NC1C(F)(F)F)C1=CC=CC=C1)CC(C)=O)=O
[CH3:1][CH2:2][c:3]1[c:4]([C:5]([F:6])([F:7])[F:8])[n:9][c:10](-[c:11]2[cH:12][cH:13][cH:14][cH:15][cH:16]2)[n:17]([CH2:18][C:19]#[CH:20])[c:22]1=[O:23].[OH-:21]>>[CH3:1][CH2:2][c:3]1[c:4]([C:5]([F:6])([F:7])[F:8])[n:9][c:10](-[c:11]2[cH:12][cH:13][cH:14][cH:15][cH:16]2)[n:17]([CH2:18][C:19]([CH3:20])=[O:21])[c:22]1=[O...
C#CCn1c(-c2ccccc2)nc(C(F)(F)F)c(CC)c1=O.[OH-]
CCc1c(C(F)(F)F)nc(-c2ccccc2)n(CC(C)=O)c1=O
null
null
C1CCOC1.C(C)(=O)OCC
Heteroatom Alkylation and Arylation
OtherReaction
40bc86c3933af1a903f8329b3ea43014fcb4fcf95be97cdb9c41053869e91cb5
7f2cd7881a1a7accd4c4687f629eb04c8f2612869365019cb1ad442e2c2b003b
O=c1ccnc(-c2ccccc2)[nH]1
[#7;a:1]:[c:2]:[#7;a:3]-[C:4]-[C;H0;D2;+0:5]#[CH;D1;+0:6].[OH-;D0:7]>>[#7;a:1]:[c:2]:[#7;a:3]-[C:4]-[C;H0;D3;+0:5](-[CH3;D1;+0:6])=[O;H0;D1;+0:7]
null
[]
null
null
null
null
To a stirred solution of 4.83 g (15.8 mmol) of 5-ethyl-3-propargyl-2-phenyl-6-trifluoromethyl-4(3H)-pyrimidinone (compound 46) in 50 mL of THF was added 50 mL of 10% aq NaOH. The mixture was heated at reflux for 2 h, cooled and diluted with 150 mL of ethyl acetate. The organic layer was separated, washed with 50 mL of ...
10.6084/m9.figshare.5104873.v1
null
Alkyne
Ketone
null
null
c1cncnc1.c1ccccc1
null
C1CCOC1.C(C)(=O)OCC
null
null
C#CCn1c(-c2ccccc2)nc(C(F)(F)F)c(CC)c1=O.[OH-]>C1CCOC1.C(C)(=O)OCC>CCc1c(C(F)(F)F)nc(-c2ccccc2)n(CC(C)=O)c1=O
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-8a76bfee244c4e589316dfef7559347f
COCOC.O=c1cc(C(F)(F)F)nc(-c2ccccc2)[nH]1>>COCn1c(-c2ccccc2)nc(C(F)(F)F)cc1=O
O=P12OP3(=O)OP(=O)(O1)OP(=O)(O2)O3.C1(=CC=CC=C1)C1=NC(=CC(N1)=O)C(F)(F)F.COCOC.O=P12OP3(=O)OP(=O)(O1)OP(=O)(O2)O3.[OH-].[Na+]>>COCN1C(=NC(=CC1=O)C(F)(F)F)C1=CC=CC=C1
CO[CH2:3][O:2][CH3:1].[nH:4]1[c:5](-[c:6]2[cH:7][cH:8][cH:9][cH:10][cH:11]2)[n:12][c:13]([C:14]([F:15])([F:16])[F:17])[cH:18][c:19]1=[O:20]>>[CH3:1][O:2][CH2:3][n:4]1[c:5](-[c:6]2[cH:7][cH:8][cH:9][cH:10][cH:11]2)[n:12][c:13]([C:14]([F:15])([F:16])[F:17])[cH:18][c:19]1=[O:20]
COCOC.O=c1cc(C(F)(F)F)nc(-c2ccccc2)[nH]1
COCn1c(-c2ccccc2)nc(C(F)(F)F)cc1=O
null
null
C(Cl)(Cl)Cl.CCCCCC.C(Cl)Cl.C(C)(=O)OCC
Heteroatom Alkylation and Arylation
OtherReaction
0add32a5be4fe5174086acead6feb976d1a076dc7d68959972c5cd4b3c28c84c
ccc058ecd89f692c39a92bd6db91fb86578428d38b5955a659e0a2343eccf0fd
O=c1ccnc(-c2ccccc2)[nH]1
C-O-[CH2;D2;+0:1]-[#8:2]-[C;D1;H3:3].[O;D1;H0:4]=[c:5]1:[c:6]:[c:7]:[#7;a:8]:[c:9](-[c:10]):[nH;D2;+0:11]:1>>[C;D1;H3:3]-[#8:2]-[CH2;D2;+0:1]-[n;H0;D3;+0:11]1:[c:5](=[O;D1;H0:4]):[c:6]:[c:7]:[#7;a:8]:[c:9]:1-[c:10]
32.8
[{"value": 32.0, "product": "COCN1C(=NC(=CC1=O)C(F)(F)F)C1=CC=CC=C1", "details": "PERCENTYIELD", "is_desired": false}, {"value": 32.8, "product": "COCN1C(=NC(=CC1=O)C(F)(F)F)C1=CC=CC=C1", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
16
HOUR
To a solution of 1.5 g (5.9 mmol) of 2-phenyl-6-trifluoromethyl-4(3H)-pyrimidinone, 17.2 g (226.3 mmol) dimethoxymethane, and 35 mL of chloroform was added 2.5 g (17.6 mmol) phosphorous pentoxide, at room temperature. By TLC (25% ethyl acetate in hexane) the reaction was incomplete after 4 h and an additional 3 g (21.1...
10.6084/m9.figshare.5104873.v1
null
Ether.Ether
Ether
c1ccncn1
c1cncnc1
c1cncnc1.c1ccccc1
HO-
C(Cl)(Cl)Cl.CCCCCC.C(Cl)Cl.C(C)(=O)OCC
null
16
COCOC.O=c1cc(C(F)(F)F)nc(-c2ccccc2)[nH]1>C(Cl)(Cl)Cl.CCCCCC.C(Cl)Cl.C(C)(=O)OCC>COCn1c(-c2ccccc2)nc(C(F)(F)F)cc1=O
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-cbd7be36ef084343a7a9b531a9094d81
C#CCn1c(-c2ccccc2)nc(C(F)(F)F)c(CC)c1=O.C=CI>>C=CC#CCn1c(-c2ccccc2)nc(C(F)(F)F)c(CC)c1=O
C(C)C=1C(N(C(=NC1C(F)(F)F)C1=CC=CC=C1)CC#C)=O.C(=C)I>>C(C)C=1C(N(C(=NC1C(F)(F)F)C1=CC=CC=C1)CC#CC=C)=O
[CH:3]#[C:4][CH2:5][n:6]1[c:7](-[c:8]2[cH:9][cH:10][cH:11][cH:12][cH:13]2)[n:14][c:15]([C:16]([F:17])([F:18])[F:19])[c:20]([CH2:21][CH3:22])[c:23]1=[O:24].I[CH:2]=[CH2:1]>>[CH2:1]=[CH:2][C:3]#[C:4][CH2:5][n:6]1[c:7](-[c:8]2[cH:9][cH:10][cH:11][cH:12][cH:13]2)[n:14][c:15]([C:16]([F:17])([F:18])[F:19])[c:20]([CH2:21][CH3...
C#CCn1c(-c2ccccc2)nc(C(F)(F)F)c(CC)c1=O.C=CI
C=CC#CCn1c(-c2ccccc2)nc(C(F)(F)F)c(CC)c1=O
null
[Cu]I.[Pd](Cl)Cl.C1(=CC=CC=C1)P(C1=CC=CC=C1)C1=CC=CC=C1.C1(=CC=CC=C1)P(C1=CC=CC=C1)C1=CC=CC=C1
C(C)N(CC)CC
C-C Coupling
Sonogashira alkyne_alkenyl halide
b0275c92ec48c41d276310eb23d2d5949a66cffe648b8115d867fbb00a93be00
6ee7e5b969047b3680750ebc6d5ad3b212c3653eb4f65f81d3cb77b36ae2893f
O=c1ccnc(-c2ccccc2)[nH]1
I-[CH;D2;+0:1]=[C;D1;H2:2].[C:3]-[C:4]#[CH;D1;+0:5]>>[C:3]-[C:4]#[C;H0;D2;+0:5]-[CH;D2;+0:1]=[C;D1;H2:2]
28.4
[{"value": 28.4, "product": "C(C)C=1C(N(C(=NC1C(F)(F)F)C1=CC=CC=C1)CC#CC=C)=O", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
22
HOUR
To a deoxygenated solution of 1.01 g (3.28 mmol) of 5-ethyl-2-phenyl-3-propargyl-6-trifluoromethyl-4(3H)-pyrimidinone and 0.61 g (3.96 mmol) of vinyl iodide in 25 mL of triethylamine was added a mixture of 60 mg of copper (I) iodide and 60 mg of bis(triphenylphosphine) palladium (II) chloride. The mixture was stirred a...
10.6084/m9.figshare.5104873.v1
null
Alkyne.Vinyl
Alkyne.Vinyl
null
null
c1cncnc1.c1ccccc1
HI
[Cu]I.[Pd](Cl)Cl.C1(=CC=CC=C1)P(C1=CC=CC=C1)C1=CC=CC=C1.C1(=CC=CC=C1)P(C1=CC=CC=C1)C1=CC=CC=C1.C(C)N(CC)CC
null
22
C#CCn1c(-c2ccccc2)nc(C(F)(F)F)c(CC)c1=O.C=CI>[Cu]I.[Pd](Cl)Cl.C1(=CC=CC=C1)P(C1=CC=CC=C1)C1=CC=CC=C1.C1(=CC=CC=C1)P(C1=CC=CC=C1)C1=CC=CC=C1.C(C)N(CC)CC>C=CC#CCn1c(-c2ccccc2)nc(C(F)(F)F)c(CC)c1=O
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-febb9432bc444d1b8660781f308ba31e
C#CCn1c(-c2cccc(C3OCCO3)c2)nc(CC)c(CC)c1=O>>C#CCn1c(-c2cccc(C=O)c2)nc(CC)c(CC)c1=O
CCOCC.O.C(C)C=1C(N(C(=NC1CC)C1=CC(=CC=C1)C1OCCO1)CC#C)=O.Cl>>C(C)C=1C(N(C(=NC1CC)C1=CC(=CC=C1)C=O)CC#C)=O
C1C[O:12][CH:11]([c:10]2[cH:9][cH:8][cH:7][c:6](-[c:5]3[n:4]([CH2:3][C:2]#[CH:1])[c:21](=[O:22])[c:18]([CH2:19][CH3:20])[c:15]([CH2:16][CH3:17])[n:14]3)[cH:13]2)O1>>[CH:1]#[C:2][CH2:3][n:4]1[c:5](-[c:6]2[cH:7][cH:8][cH:9][c:10]([CH:11]=[O:12])[cH:13]2)[n:14][c:15]([CH2:16][CH3:17])[c:18]([CH2:19][CH3:20])[c:21]1=[O:22]
C#CCn1c(-c2cccc(C3OCCO3)c2)nc(CC)c(CC)c1=O
C#CCn1c(-c2cccc(C=O)c2)nc(CC)c(CC)c1=O
null
null
CCCCCC.C(C)(=O)OCC
Miscellaneous
Acetal hydrolysis to aldehyde
f12636b09f9df336ccc8fe82b927db0e267bccc7cae0970f1f91c7ceed085225
84d5a69453aa750f462aa94a6bf2116fc17c5d88a9619aaa9eefb74b0c09848d
O=c1ccnc(-c2ccccc2)[nH]1
[c:1]:[c:2](-[CH;D3;+0:3]1-O-C-C-[O;H0;D2;+0:4]-1):[c:5]>>[O;H0;D1;+0:4]=[CH;D2;+0:3]-[c:2](:[c:1]):[c:5]
86.4
[{"value": 86.0, "product": "C(C)C=1C(N(C(=NC1CC)C1=CC(=CC=C1)C=O)CC#C)=O", "details": "PERCENTYIELD", "is_desired": false}, {"value": 86.4, "product": "C(C)C=1C(N(C(=NC1CC)C1=CC(=CC=C1)C=O)CC#C)=O", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
4
HOUR
To a solution of 2.3 g (6.8 mmol) of 5,6-diethyl-2-[3-(2-dioxolanyl)phenyl]-3-propargyl-4(3H)-pyrimidinone in 1 mL of ethyl acetate was added 50 mL of 6M hydrochloric acid and the mixture was stirred for 4 hours. The reaction was followed by gas chromatography and TLC(20% ethyl acetate in hexane). Upon completion of re...
10.6084/m9.figshare.5104873.v1
null
Ether.Ether
Aldehyde
C1COCO1
null
c1cncnc1.c1ccccc1
HO-
CCCCCC.C(C)(=O)OCC
null
4
C#CCn1c(-c2cccc(C3OCCO3)c2)nc(CC)c(CC)c1=O>CCCCCC.C(C)(=O)OCC>C#CCn1c(-c2cccc(C=O)c2)nc(CC)c(CC)c1=O
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-5d84c8f338a741eebe88ed5f50eec903
CCc1nc(-c2ccccc2)n(CC)c(=O)c1I.O=C([O-])C(F)(F)F>>CCc1nc(-c2ccccc2)n(CC)c(=O)c1C(F)(F)F
C(C)N1C(=NC(=C(C1=O)I)CC)C1=CC=CC=C1.FC(C(=O)[O-])(F)F.[Na+].CN1C(CCC1)=O>>C(C)N1C(=NC(=C(C1=O)C(F)(F)F)CC)C1=CC=CC=C1
I[c:17]1[c:3]([CH2:2][CH3:1])[n:4][c:5](-[c:6]2[cH:7][cH:8][cH:9][cH:10][cH:11]2)[n:12]([CH2:13][CH3:14])[c:15]1=[O:16].O=C([O-])[C:18]([F:19])([F:20])[F:21]>>[CH3:1][CH2:2][c:3]1[n:4][c:5](-[c:6]2[cH:7][cH:8][cH:9][cH:10][cH:11]2)[n:12]([CH2:13][CH3:14])[c:15](=[O:16])[c:17]1[C:18]([F:19])([F:20])[F:21]
CCc1nc(-c2ccccc2)n(CC)c(=O)c1I.O=C([O-])C(F)(F)F
CCc1nc(-c2ccccc2)n(CC)c(=O)c1C(F)(F)F
null
[Cu]I
CCOCC
C-C Coupling
OtherReaction
47cbd2b0ff20300536d0cffca6c2ea55a53280e27fccd5cfa965ded0f6858b07
e720556849b4b6d74d42c92419c2568e82bddeb43f0960aee719e65329267335
O=c1ccnc(-c2ccccc2)[nH]1
I-[c;H0;D3;+0:1]1:[c:2](=[O;D1;H0:3]):[#7;a:4](-[C:5]):[c:6]:[#7;a:7]:[c:8]:1-[C:9].O=C(-[O-])-[C;H0;D4;+0:10](-[F;D1;H0:11])(-[F;D1;H0:12])-[F;D1;H0:13]>>[C:5]-[#7;a:4]1:[c:6]:[#7;a:7]:[c:8](-[C:9]):[c;H0;D3;+0:1](-[C;H0;D4;+0:10](-[F;D1;H0:11])(-[F;D1;H0:12])-[F;D1;H0:13]):[c:2]:1=[O;D1;H0:3]
42.2
[{"value": 42.2, "product": "C(C)N1C(=NC(=C(C1=O)C(F)(F)F)CC)C1=CC=CC=C1", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
null
null
A mixture of 1.00 g (2.8 mmol) of 3,6-diethyl-5-iodo-2-phenyl-4(3H)-pyrimidinone, 1.08 g (5.7 mmol) of copper (I) iodide, 1.54 g (11.3 mmol) of sodium trifluoroacetate and 8 mL of anhydrous N-methylpyrrolidinone was heated at 175 C for 2 h. The mixture was cooled, diluted with 175 mL of ether, washed with four 50 mL po...
10.6084/m9.figshare.5104873.v1
null
Trifluoro group.Aromatic halide
Trifluoro group
c1cncnc1
c1cncnc1
c1cncnc1.c1ccccc1
I-
[Cu]I.CCOCC
null
null
CCc1nc(-c2ccccc2)n(CC)c(=O)c1I.O=C([O-])C(F)(F)F>[Cu]I.CCOCC>CCc1nc(-c2ccccc2)n(CC)c(=O)c1C(F)(F)F
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-db525fc7ca504fc7b7efbfba048e0449
C#CCn1c(-c2cccc(C=O)c2)nc(CC)c(CC)c1=O.NO>>C#CCn1c(C2=CC=CC(=NO)C2)nc(CC)c(CC)c1=O
C(C)C=1C(N(C(=NC1CC)C1=CC(=CC=C1)C=O)CC#C)=O.Cl.NO>>C(C)C=1C(N(C(=NC1CC)C=1CC(C=CC1)=NO)CC#C)=O
O=C[c:10]1[cH:9][cH:8][cH:7][c:6](-[c:5]2[n:4]([CH2:3][C:2]#[CH:1])[c:21](=[O:22])[c:18]([CH2:19][CH3:20])[c:15]([CH2:16][CH3:17])[n:14]2)[cH:13]1.[NH2:11][OH:12]>>[CH:1]#[C:2][CH2:3][n:4]1[c:5]([C:6]2=[CH:7][CH:8]=[CH:9][C:10](=[N:11][OH:12])[CH2:13]2)[n:14][c:15]([CH2:16][CH3:17])[c:18]([CH2:19][CH3:20])[c:21]1=[O:22...
C#CCn1c(-c2cccc(C=O)c2)nc(CC)c(CC)c1=O.NO
C#CCn1c(C2=CC=CC(=NO)C2)nc(CC)c(CC)c1=O
null
null
C(C)O
Heteroatom Alkylation and Arylation
OtherReaction
15e2b91d223429254e0537e29a607acdcc37e5fd3dd4313d80c7521c1966cdc2
b81c903f6c555f71b81105429c919c51c8d3cea1128467d023295f77c1491add
N=C1C=CC=C(c2nccc(=O)[nH]2)C1
O=C-[c;H0;D3;+0:1]1:[cH;D2;+0:2]:[c;H0;D3;+0:3](-[c;H0;D3;+0:4](:[#7;a:5]:[c:6]):[#7;a:7](-[C:8]-[C:9]#[C;D1;H1:10]):[c:11]):[cH;D2;+0:12]:[cH;D2;+0:13]:[cH;D2;+0:14]:1.[NH2;D1;+0:15]-[O;D1;H1:16]>>[C;D1;H1:10]#[C:9]-[C:8]-[#7;a:7](:[c:11]):[c;H0;D3;+0:4](-[C;H0;D3;+0:3]1=[CH;D2;+0:12]-[CH;D2;+0:13]=[CH;D2;+0:14]-[C;H0...
77.6
[{"value": 77.6, "product": "C(C)C=1C(N(C(=NC1CC)C=1CC(C=CC1)=NO)CC#C)=O", "details": "PERCENTYIELD", "is_desired": false}, {"value": 60.9, "product": "C(C)C=1C(N(C(=NC1CC)C=1CC(C=CC1)=NO)CC#C)=O", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
null
null
To a 100 mL RBF were charged 1.1 g (3.7 mmol) of 5,6-diethyl-2-(3-formyl-phenyl)-3-propargyl-4(3H)-pyrimidinone, 0.52 g (7.5 mmol) of hydroxylamine hydrochloride and 50 mL of ethanol. The reaction mixture was refluxed for 17 hours. The ethanol was removed in vacuo and ether and ethyl acetate were added to the residue. ...
10.6084/m9.figshare.5104873.v1
null
Aldehyde.Primary amine
Conjugated diene.Oxime
c1ccccc1
C1=CCCC=C1
c1cncnc1.C1=CCCC=C1
HO-
C(C)O
null
null
C#CCn1c(-c2cccc(C=O)c2)nc(CC)c(CC)c1=O.NO>C(C)O>C#CCn1c(C2=CC=CC(=NO)C2)nc(CC)c(CC)c1=O
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-d39e19c8619b4440b84b2d542c14fa6e
C#CCn1c(-c2ccccc2)nc(CC)c(CC(=O)OC)c1=O>>C#CCn1c(-c2ccccc2)nc(CC)c(CCO)c1=O
O.C(C)C1=C(C(N(C(=N1)C1=CC=CC=C1)CC#C)=O)CC(=O)OC.C(C)C1=C(C(N(C(=N1)C1=CC=CC=C1)CC#C)=O)CC(=O)OC.[H-].[Al+3].[Li+].[H-].[H-].[H-].[H-].[Al+3].[Li+].[H-].[H-].[H-]>>C(C)C1=C(C(N(C(=N1)C1=CC=CC=C1)CC#C)=O)CCO
CO[C:18]([CH2:17][c:16]1[c:13]([CH2:14][CH3:15])[n:12][c:5](-[c:6]2[cH:7][cH:8][cH:9][cH:10][cH:11]2)[n:4]([CH2:3][C:2]#[CH:1])[c:20]1=[O:21])=[O:19]>>[CH:1]#[C:2][CH2:3][n:4]1[c:5](-[c:6]2[cH:7][cH:8][cH:9][cH:10][cH:11]2)[n:12][c:13]([CH2:14][CH3:15])[c:16]([CH2:17][CH2:18][OH:19])[c:20]1=[O:21]
C#CCn1c(-c2ccccc2)nc(CC)c(CC(=O)OC)c1=O
C#CCn1c(-c2ccccc2)nc(CC)c(CCO)c1=O
null
null
CCOCC.C1CCOC1
Reduction
Reduction of ester to primary alcohol
21d61543c6ec8a8cebe1b3ef55ef3dd20acbf79a4f1c12a7fb51e32be7a3248a
1fbcd628a0426673c5d10aa49a977cd2d1ae02a8cdf57bbb10d94aa03a94e937
O=c1ccnc(-c2ccccc2)[nH]1
C-O-[C;H0;D3;+0:1](=[O;H0;D1;+0:2])-[C:3]-[c:4](:[c:5]:[#7;a:6]):[c:7]:[#7;a:8]>>[#7;a:6]:[c:5]:[c:4](-[C:3]-[CH2;D2;+0:1]-[OH;D1;+0:2]):[c:7]:[#7;a:8]
null
[]
null
null
3
HOUR
A stirred solution of 1.35 g (4.4 mmol) of 6-ethyl-5-methoxycarbonylmethyl-2-phenyl-3-propargyl-4(3H)-pyrimidinone (Compound 105) in 30 mL of THF was cooled in an ice bath and a slurry of 0.10 g (2.6 mmol) of lithium aluminum hydride in 10 mL of ether was added. The ice bath was allowed to melt and the reaction mixture...
10.6084/m9.figshare.5104873.v1
null
Ester
Primary alcohol
null
null
c1cncnc1.c1ccccc1
Other
CCOCC.C1CCOC1
null
3
C#CCn1c(-c2ccccc2)nc(CC)c(CC(=O)OC)c1=O>CCOCC.C1CCOC1>C#CCn1c(-c2ccccc2)nc(CC)c(CCO)c1=O
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-f44bdc8cc42c4333808efcfd30ed387a
C#CCn1c(-c2ccccc2)nc(CC)c(CC(=O)OC)c1=O.[NH4+]>>C#CCn1c(-c2ccccc2)nc(CC)c(CC(N)=O)c1=O
C(C)C1=C(C(N(C(=N1)C1=CC=CC=C1)CC#C)=O)CC(=O)OC.C(C)C1=C(C(N(C(=N1)C1=CC=CC=C1)CC#C)=O)CC(=O)OC.[NH4+].[OH-]>>NC(=O)CC=1C(N(C(=NC1CC)C1=CC=CC=C1)CC#C)=O
CO[C:18]([CH2:17][c:16]1[c:13]([CH2:14][CH3:15])[n:12][c:5](-[c:6]2[cH:7][cH:8][cH:9][cH:10][cH:11]2)[n:4]([CH2:3][C:2]#[CH:1])[c:21]1=[O:22])=[O:20].[NH4+:19]>>[CH:1]#[C:2][CH2:3][n:4]1[c:5](-[c:6]2[cH:7][cH:8][cH:9][cH:10][cH:11]2)[n:12][c:13]([CH2:14][CH3:15])[c:16]([CH2:17][C:18]([NH2:19])=[O:20])[c:21]1=[O:22]
C#CCn1c(-c2ccccc2)nc(CC)c(CC(=O)OC)c1=O.[NH4+]
C#CCn1c(-c2ccccc2)nc(CC)c(CC(N)=O)c1=O
null
null
C1CCOC1
Acylation
OtherReaction
d5b10d4f469e7a196a3b04a6a9e159a7d90514b6df5b50c1197d4b1b774c04e1
adc0ef6f6c1340dd2dbab737c85bf17fc842769181c5db1a2b4f82b391b28f9f
O=c1ccnc(-c2ccccc2)[nH]1
C-O-[C;H0;D3;+0:1](=[O;D1;H0:2])-[C:3]-[c:4](:[c:5]:[#7;a:6]):[c:7]:[#7;a:8].[NH4+;D0:9]>>[#7;a:6]:[c:5]:[c:4](-[C:3]-[C;H0;D3;+0:1](-[NH2;D1;+0:9])=[O;D1;H0:2]):[c:7]:[#7;a:8]
null
[]
null
null
null
null
To a stirred solution of 1.75 g (5.7 mmol) of 6-ethyl-5-methoxycarbonylmethyl-2-phenyl-3-propargyl-4(3H)-pyrimidinone (Compound 105) in 100 mL of THF was added 200 mL of concentrated aqueous NH4OH. The mixture was stirred for 2 weeks and the bulk of the THF was removed on the rotovap. The mixture was shaken with 100 mL...
10.6084/m9.figshare.5104873.v1
null
Ester
Primary amide
null
null
c1cncnc1.c1ccccc1
HO-
C1CCOC1
null
null
C#CCn1c(-c2ccccc2)nc(CC)c(CC(=O)OC)c1=O.[NH4+]>C1CCOC1>C#CCn1c(-c2ccccc2)nc(CC)c(CC(N)=O)c1=O
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-504c94f80cd14c1f86ab5786e3c9e054
C#CCn1c(-c2ccccc2)nc(CC)c(OC)c1=O>>C#CCn1c(-c2ccccc2)nc(CC)c(O)c1=O
C(C)C1=C(C(N(C(=N1)C1=CC=CC=C1)CC#C)=O)OC.C(C)C1=C(C(N(C(=N1)C1=CC=CC=C1)CC#C)=O)OC>>C(C)C1=C(C(N(C(=N1)C1=CC=CC=C1)CC#C)=O)O
C[O:17][c:16]1[c:13]([CH2:14][CH3:15])[n:12][c:5](-[c:6]2[cH:7][cH:8][cH:9][cH:10][cH:11]2)[n:4]([CH2:3][C:2]#[CH:1])[c:18]1=[O:19]>>[CH:1]#[C:2][CH2:3][n:4]1[c:5](-[c:6]2[cH:7][cH:8][cH:9][cH:10][cH:11]2)[n:12][c:13]([CH2:14][CH3:15])[c:16]([OH:17])[c:18]1=[O:19]
C#CCn1c(-c2ccccc2)nc(CC)c(OC)c1=O
C#CCn1c(-c2ccccc2)nc(CC)c(O)c1=O
null
null
O
Deprotection
Cleavage of methoxy ethers to alcohols
c5320c7dfa4f544d4900efcae9b3262bf0d5286bcf39c86109232351f35b23d5
26a36596df80ec137b0e8087297418351c93c32819177f680675220622f215d4
O=c1ccnc(-c2ccccc2)[nH]1
C-[O;H0;D2;+0:1]-[c:2]1:[c:3](-[C:4]):[#7;a:5]:[c:6]:[#7;a:7](-[C:8]-[C:9]#[C;D1;H1:10]):[c:11]:1=[O;D1;H0:12]>>[C:4]-[c:3]1:[#7;a:5]:[c:6]:[#7;a:7](-[C:8]-[C:9]#[C;D1;H1:10]):[c:11](=[O;D1;H0:12]):[c:2]:1-[OH;D1;+0:1]
72
[{"value": 72.0, "product": "C(C)C1=C(C(N(C(=N1)C1=CC=CC=C1)CC#C)=O)O", "details": "PERCENTYIELD", "is_desired": false}, {"value": 71.5, "product": "C(C)C1=C(C(N(C(=N1)C1=CC=CC=C1)CC#C)=O)O", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
1.5
HOUR
To an oven dried 3-neck round bottom flask, equipped with a magnetic stirrer, a thermometer, an addition funnel, a septum and a nitrogen inlet, was added 10 mL of 1M boron tribromide in methylene chloride, by syringe. The BBr3 was cooled to -65 C with a dry ice/acetone bath and 0.9 g (3.3 mmol) of 6-ethyl-5-methoxy-2-p...
10.6084/m9.figshare.5104873.v1
null
Ether
Aromatic alcohol
null
null
c1cncnc1.c1ccccc1
Other
O
null
1.5
C#CCn1c(-c2ccccc2)nc(CC)c(OC)c1=O>O>C#CCn1c(-c2ccccc2)nc(CC)c(O)c1=O
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-b5423c5215ee415abe3ef0b650a1ea4e
C#CCn1c(-c2ccccc2)nc(CC)c(CC(N)=O)c1=O.C#CCn1c(-c2ccccc2)nc(CC)c(CC(N)=O)c1=O>>C#CCN1C(=O)C(CC#N)C(CC)(CC)N=C1c1ccccc1
FC(C(=O)OC(C(F)(F)F)=O)(F)F.NC(=O)CC=1C(N(C(=NC1CC)C1=CC=CC=C1)CC#C)=O.NC(=O)CC=1C(N(C(=NC1CC)C1=CC=CC=C1)CC#C)=O.N1=CC=CC=C1>>C(C)C1(C(C(N(C(=N1)C1=CC=CC=C1)CC#C)=O)CC#N)CC
O=[C:9]([CH2:8][c:7]1[c:5](=[O:6])[n:4]([CH2:3][C:2]#[CH:1])[c:17](-[c:18]2[cH:19][cH:20][cH:21][cH:22][cH:23]2)[n:16][c:11]1[CH2:14][CH3:15])[NH2:10].C#CCn1c(-c2ccccc2)nc([CH2:12][CH3:13])c(CC(N)=O)c1=O>>[CH:1]#[C:2][CH2:3][N:4]1[C:5](=[O:6])[CH:7]([CH2:8][C:9]#[N:10])[C:11]([CH2:12][CH3:13])([CH2:14][CH3:15])[N:16]=[...
C#CCn1c(-c2ccccc2)nc(CC)c(CC(N)=O)c1=O.C#CCn1c(-c2ccccc2)nc(CC)c(CC(N)=O)c1=O
C#CCN1C(=O)C(CC#N)C(CC)(CC)N=C1c1ccccc1
null
null
CCOCC.C1CCOC1
C-C Coupling
OtherReaction
1b263c8b01f51ed84eaf98344ae82c45c59fae78da851f7370a0e942d924e48e
e3747cc44512240445b802b2047ca2b6f84ae8fab0d24a606f2e5eeb5fddc92d
O=C1CCN=C(c2ccccc2)N1
C#C-C-n1:c(-c2:c:c:c:c:c:2):n:c(-[CH2;D2;+0:1]-[C;D1;H3:2]):c(-C-C(-N)=O):c:1=O.O=[C;H0;D3;+0:3](-[NH2;D1;+0:4])-[C:5]-[c;H0;D3;+0:6]1:[c;H0;D3;+0:7](-[C:8]-[C;D1;H3:9]):[n;H0;D2;+0:10]:[c;H0;D3;+0:11](-[c;H0;D3;+0:12](:[c:13]:[c:14]):[c:15]:[c:16]):[n;H0;D3;+0:17](-[C:18]-[C:19]#[C;D1;H1:20]):[c;H0;D3;+0:21]:1=[O;D1;H...
49.8
[{"value": 49.8, "product": "C(C)C1(C(C(N(C(=N1)C1=CC=CC=C1)CC#C)=O)CC#N)CC", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
null
null
A stirred suspension of 0.25 g (0.85 mmol) of 5-aminocarbonylmethyl-6-ethyl-2-phenyl-3-propargyl-4(3H)-pyrimidinone (Compound 275) in 12 mL of THF was cooled in an icebath and 0.15 mL (1.9 mmol) of pyridine was added followed by 0.13 mL (0.92 mmol) of trifluoroacetic anhydride. The mixture was stirred in the ice bath f...
10.6084/m9.figshare.5104873.v1
null
Primary amide.Primary amide.Alkyne
Nitrile.Tertiary amide
c1cncnc1.c1cncnc1.c1ccccc1
C1=NCCC[NH]1
C1=NCCC[NH]1.c1ccccc1
HO-
CCOCC.C1CCOC1
null
null
C#CCn1c(-c2ccccc2)nc(CC)c(CC(N)=O)c1=O.C#CCn1c(-c2ccccc2)nc(CC)c(CC(N)=O)c1=O>CCOCC.C1CCOC1>C#CCN1C(=O)C(CC#N)C(CC)(CC)N=C1c1ccccc1
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-2711ddf9e8434df4b8105ee87a87cff2
CN=C=O.Nc1ccc(F)cc1F>>CNC(=O)Nc1ccc(F)cc1F
CN=C=O.FC1=C(N)C=CC(=C1)F>>FC1=C(C=CC(=C1)F)NC(=O)NC
[CH3:1][N:2]=[C:3]=[O:4].[NH2:5][c:6]1[cH:7][cH:8][c:9]([F:10])[cH:11][c:12]1[F:13]>>[CH3:1][NH:2][C:3](=[O:4])[NH:5][c:6]1[cH:7][cH:8][c:9]([F:10])[cH:11][c:12]1[F:13]
CN=C=O.Nc1ccc(F)cc1F
CNC(=O)Nc1ccc(F)cc1F
null
null
C1(=CC=CC=C1)C
Acylation
Urea synthesis via isocyanate and primary amine
d39cd7dc52a79bb265ff8ef61ef7bf9dc7f7b5fb0150fcb4881bdfb18ab9c380
a5dc801930c765d2a435a0a2973e50163c305ba8e7641d6adbcc1550b7b96de7
c1ccccc1
[C;D1;H3:1]-[N;H0;D2;+0:2]=[C;H0;D2;+0:3]=[O;D1;H0:4].[NH2;D1;+0:5]-[c:6](:[c:7]):[c:8]>>[C;D1;H3:1]-[NH;D2;+0:2]-[C;H0;D3;+0:3](=[O;D1;H0:4])-[NH;D2;+0:5]-[c:6](:[c:7]):[c:8]
null
[]
null
null
1
HOUR
Methyl isocyanate (9.6 g, 10 mL, 0.174 mol) is added to a solution of 2,4-difluoroaniline (15 g, 0.116 mol) in toluene. The reaction mixture is stirred for 1 hour and filtered to obtain a solid. The solid is washed with hexanes and air-dried to give the title product as an off-white solid, mp 182°-183° C. Conditions: S...
10.6084/m9.figshare.5104873.v1
null
Isocyanate.Primary amine
Urea
null
null
c1ccccc1
null
C1(=CC=CC=C1)C
null
1
CN=C=O.Nc1ccc(F)cc1F>C1(=CC=CC=C1)C>CNC(=O)Nc1ccc(F)cc1F
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-e4418b697e514e7891fd2f8cc0451b85
Cn1c(=O)[nH]c(=O)n(-c2ccc(F)cc2Cl)c1=O.O=[N+]([O-])O>>Cn1c(=O)[nH]c(=O)n(-c2cc([N+](=O)[O-])c(F)cc2Cl)c1=O
[N+](=O)(O)[O-].ClC1=C(C=CC(=C1)F)N1C(N(C(NC1=O)=O)C)=O>>ClC1=C(C=C(C(=C1)F)[N+](=O)[O-])N1C(N(C(NC1=O)=O)C)=O
[CH3:1][n:2]1[c:3](=[O:4])[nH:5][c:6](=[O:7])[n:8](-[c:9]2[cH:10][cH:11][c:15]([F:16])[cH:17][c:18]2[Cl:19])[c:20]1=[O:21].O[N+:12](=[O:13])[O-:14]>>[CH3:1][n:2]1[c:3](=[O:4])[nH:5][c:6](=[O:7])[n:8](-[c:9]2[cH:10][c:11]([N+:12](=[O:13])[O-:14])[c:15]([F:16])[cH:17][c:18]2[Cl:19])[c:20]1=[O:21]
Cn1c(=O)[nH]c(=O)n(-c2ccc(F)cc2Cl)c1=O.O=[N+]([O-])O
Cn1c(=O)[nH]c(=O)n(-c2cc([N+](=O)[O-])c(F)cc2Cl)c1=O
null
null
S(O)(O)(=O)=O
Functional Group Addition
Aromatic nitration with HNO3
53848b8b2bb4e867226e49db2e60519b24be9379900e3ad7c56af54fe8fde7a5
ddce49825c02b8965f10c8d99e3c841d26e1f136da6037b417c09313e6d73097
O=c1[nH]c(=O)n(-c2ccccc2)c(=O)[nH]1
O-[N+;H0;D3:1](-[O;-;D1;H0:2])=[O;D1;H0:3].[F;D1;H0:4]-[c:5](:[c:6]):[cH;D2;+0:7]:[c:8]:[c:9]>>[F;D1;H0:4]-[c:5](:[c:6]):[c;H0;D3;+0:7](-[N+;H0;D3:1](-[O;-;D1;H0:2])=[O;D1;H0:3]):[c:8]:[c:9]
75.6
[{"value": 75.6, "product": "ClC1=C(C=C(C(=C1)F)[N+](=O)[O-])N1C(N(C(NC1=O)=O)C)=O", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
30
MINUTE
Nitric acid (70% real, 8.3 mL, 0.131 mol) is added to a solution of 1-(2-chloro-4-fluorophenyl)-3-methyl-s-triazine-2,4,6(1H,3H,5H)-trione (32.4 g, 0.119 mol) in concentrated sulfuric acid while maintaining the reaction mixture temperature below 10° C. After the addition is complete, the reaction mixture is stirred at ...
10.6084/m9.figshare.5104873.v1
null
Nitrate
Nitro group
c1ccccc1
c1ccccc1
c1ncncn1.c1ccccc1
HO-
S(O)(O)(=O)=O
null
0.5
Cn1c(=O)[nH]c(=O)n(-c2ccc(F)cc2Cl)c1=O.O=[N+]([O-])O>S(O)(O)(=O)=O>Cn1c(=O)[nH]c(=O)n(-c2cc([N+](=O)[O-])c(F)cc2Cl)c1=O
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-08b8b8866d334d3cae4bec9581c21467
Cn1c(=O)[nH]c(=O)n(-c2cc([N+](=O)[O-])c(F)cc2Cl)c1=O>>CN1CN=CN(c2cc(N)c(F)cc2Cl)C1
ClC1=C(C=C(C(=C1)F)[N+](=O)[O-])N1C(N(C(NC1=O)=O)C)=O.[H][H]>>NC=1C(=CC(=C(C1)N1CN(CN=C1)C)Cl)F
O=[c:3]1[n:2]([CH3:1])[c:16](=O)[n:6](-[c:7]2[cH:8][c:9]([N+:10](=O)[O-])[c:11]([F:12])[cH:13][c:14]2[Cl:15])[c:5](=O)[nH:4]1>>[CH3:1][N:2]1[CH2:3][N:4]=[CH:5][N:6]([c:7]2[cH:8][c:9]([NH2:10])[c:11]([F:12])[cH:13][c:14]2[Cl:15])[CH2:16]1
Cn1c(=O)[nH]c(=O)n(-c2cc([N+](=O)[O-])c(F)cc2Cl)c1=O
CN1CN=CN(c2cc(N)c(F)cc2Cl)C1
null
[Pt]
C(C)(=O)OCC
Reduction
OtherReaction
a12ef5c8c6b913d30cb7c8dc2ae210db0c0600ef67a885c2006dbb9ecfbe343f
26a2c3d4c194185f138d82af968f6432e8cc58ea35d694a1df2cd162a2f92ecb
C1=NCNCN1c1ccccc1
O=[N+;H0;D3:1](-[O-])-[c:2]1:[c:3]:[c:4]:[c:5](-[Cl;D1;H0:6]):[c;H0;D3;+0:7](-[n;H0;D3;+0:8]2:[c;H0;D3;+0:9](=O):[n;H0;D3;+0:10](-[C;D1;H3:11]):[c;H0;D3;+0:12](=O):[nH;D2;+0:13]:[c;H0;D3;+0:14]:2=O):[c:15]:1>>[C;D1;H3:11]-[N;H0;D3;+0:10]1-[CH2;D2;+0:9]-[N;H0;D3;+0:8](-[c;H0;D3;+0:7]2:[c:15]:[c:2](-[NH2;D1;+0:1]):[c:3]:...
null
[]
null
null
null
null
A mixture of 1-(2-chloro-4-fluoro-5-nitrophenyl)-3-methyl-s-triazine-2,4,6(1H,3H,5H)-trione (28.5 g, 0.09 mol) and 5% platinum on activated carbon (1 g) in ethyl acetate is hydrogenated at 55 psi until hydrogen uptake is complete. The reaction mixture is then filtered and concentrated in vacuo to give the title product...
10.6084/m9.figshare.5104873.v1
null
Nitro group
Primary amine.Tertiary amine.Tertiary amine
c1ncncn1
C1=NC[NH]C[NH]1
C1=NC[NH]C[NH]1.c1ccccc1
Other
[Pt].C(C)(=O)OCC
null
null
Cn1c(=O)[nH]c(=O)n(-c2cc([N+](=O)[O-])c(F)cc2Cl)c1=O>[Pt].C(C)(=O)OCC>CN1CN=CN(c2cc(N)c(F)cc2Cl)C1
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-6bab90c4b53c475ea6ce599eec07ade5
CCOC(=O)CN.O=C=Nc1ccc(F)c([N+](=O)[O-])c1>>CCOC(=O)CNC(=O)Nc1ccc(F)c([N+](=O)[O-])c1
O.Cl.C(C)OC(CN)=O.FC1=C(C=C(C=C1)N=C=O)[N+](=O)[O-].C(C)N(CC)CC>>FC1=C(C=C(C=C1)NC(=O)NCC(=O)OCC)[N+](=O)[O-]
[CH3:1][CH2:2][O:3][C:4](=[O:5])[CH2:6][NH2:7].[C:8](=[O:9])=[N:10][c:11]1[cH:12][cH:13][c:14]([F:15])[c:16]([N+:17](=[O:18])[O-:19])[cH:20]1>>[CH3:1][CH2:2][O:3][C:4](=[O:5])[CH2:6][NH:7][C:8](=[O:9])[NH:10][c:11]1[cH:12][cH:13][c:14]([F:15])[c:16]([N+:17](=[O:18])[O-:19])[cH:20]1
CCOC(=O)CN.O=C=Nc1ccc(F)c([N+](=O)[O-])c1
CCOC(=O)CNC(=O)Nc1ccc(F)c([N+](=O)[O-])c1
null
null
O1CCCC1
Acylation
Urea synthesis via isocyanate and primary amine
d39cd7dc52a79bb265ff8ef61ef7bf9dc7f7b5fb0150fcb4881bdfb18ab9c380
a5dc801930c765d2a435a0a2973e50163c305ba8e7641d6adbcc1550b7b96de7
c1ccccc1
[C:1]-[#8:2]-[C:3](=[O;D1;H0:4])-[C:5]-[NH2;D1;+0:6].[O;D1;H0:7]=[C;H0;D2;+0:8]=[N;H0;D2;+0:9]-[c:10](:[c:11]):[c:12]>>[C:1]-[#8:2]-[C:3](=[O;D1;H0:4])-[C:5]-[NH;D2;+0:6]-[C;H0;D3;+0:8](=[O;D1;H0:7])-[NH;D2;+0:9]-[c:10](:[c:11]):[c:12]
56.1
[{"value": 56.1, "product": "FC1=C(C=C(C=C1)NC(=O)NCC(=O)OCC)[N+](=O)[O-]", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
1
HOUR
A solution of 4-fluoro-3-nitrophenyl isocyanate (10 g, 0.055 mol) in anhydrous tetrahydrofuran is cooled to 0° C., treated with glycine ethyl ester hydrochloride (7.7 g, 0.055 mol), treated with triethylamine (5.56 g, 0.055 mol) while maintaining the temperature below 10° C., stirred at room temperature for 1 hour and ...
10.6084/m9.figshare.5104873.v1
null
Isocyanate.Primary amine
Urea
null
null
c1ccccc1
null
O1CCCC1
null
1
CCOC(=O)CN.O=C=Nc1ccc(F)c([N+](=O)[O-])c1>O1CCCC1>CCOC(=O)CNC(=O)Nc1ccc(F)c([N+](=O)[O-])c1
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-c5aff79410674f0180c8c0f0b265e45b
CCOC(=O)CNC(=O)Nc1ccc(F)c([N+](=O)[O-])c1>>CCOC(=O)CNC(=O)Nc1ccc(F)c(N)c1
FC1=C(C=C(C=C1)NC(=O)NCC(=O)OCC)[N+](=O)[O-].[H][H]>>NC=1C=C(C=CC1F)NC(=O)NCC(=O)OCC
O=[N+:17]([O-])[c:16]1[c:14]([F:15])[cH:13][cH:12][c:11]([NH:10][C:8]([NH:7][CH2:6][C:4]([O:3][CH2:2][CH3:1])=[O:5])=[O:9])[cH:18]1>>[CH3:1][CH2:2][O:3][C:4](=[O:5])[CH2:6][NH:7][C:8](=[O:9])[NH:10][c:11]1[cH:12][cH:13][c:14]([F:15])[c:16]([NH2:17])[cH:18]1
CCOC(=O)CNC(=O)Nc1ccc(F)c([N+](=O)[O-])c1
CCOC(=O)CNC(=O)Nc1ccc(F)c(N)c1
null
[Pt]
C(C)(=O)OCC
Reduction
Reduction of nitro groups to amines
bbc242b150a51e69d3ad1caaa391f4422710431b398dcb880555f476706790be
7b0317532ea57a4fcedc1efc3e3c22eb5238d1c8330da53d4f9801fc2391f567
c1ccccc1
O=[N+;H0;D3:1](-[O-])-[c:2](:[c:3]):[c:4]>>[NH2;D1;+0:1]-[c:2](:[c:3]):[c:4]
60.8
[{"value": 60.8, "product": "NC=1C=C(C=CC1F)NC(=O)NCC(=O)OCC", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
null
null
A mixture of N-[(4-fluoro-3-nitrophenyl)carbamoyl]glycine, ethyl ester (8 g, 0.029 mol) and 5% platinum on activated carbon (0.5 g) in ethyl acetate is hydrogenated at 50 psi until hydrogen uptake is complete. The reaction mixture is then filtered and cooled in an ice-bath until a solid forms. The solid is collected by...
10.6084/m9.figshare.5104873.v1
null
Nitro group
Primary amine
null
null
c1ccccc1
Other
[Pt].C(C)(=O)OCC
null
null
CCOC(=O)CNC(=O)Nc1ccc(F)c([N+](=O)[O-])c1>[Pt].C(C)(=O)OCC>CCOC(=O)CNC(=O)Nc1ccc(F)c(N)c1
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-79c673a5defa413ebe1182aa02579411
CC(C)OC(=O)CBr.Cn1c(=O)[nH]c(=O)n(-c2ccc(F)cc2Cl)c1=O>>CC(C)OC(=O)Cn1c(=O)n(C)c(=O)n(-c2ccc(F)cc2Cl)c1=O
O.ClC1=C(C=CC(=C1)F)N1C(N(C(NC1=O)=O)C)=O.C([O-])([O-])=O.[K+].[K+].BrCC(=O)OC(C)C>>ClC1=C(C=CC(=C1)F)N1C(N(C(N(C1=O)C)=O)CC(=O)OC(C)C)=O
Br[CH2:7][C:5]([O:4][CH:2]([CH3:1])[CH3:3])=[O:6].[nH:8]1[c:9](=[O:10])[n:11]([CH3:12])[c:13](=[O:14])[n:15](-[c:16]2[cH:17][cH:18][c:19]([F:20])[cH:21][c:22]2[Cl:23])[c:24]1=[O:25]>>[CH3:1][CH:2]([CH3:3])[O:4][C:5](=[O:6])[CH2:7][n:8]1[c:9](=[O:10])[n:11]([CH3:12])[c:13](=[O:14])[n:15](-[c:16]2[cH:17][cH:18][c:19]([F:...
CC(C)OC(=O)CBr.Cn1c(=O)[nH]c(=O)n(-c2ccc(F)cc2Cl)c1=O
CC(C)OC(=O)Cn1c(=O)n(C)c(=O)n(-c2ccc(F)cc2Cl)c1=O
null
null
CN(C=O)C.CCOCC.C(Cl)Cl
Heteroatom Alkylation and Arylation
N-alkylation of secondary amines with alkyl halides
42369dcf6c82c4deef5c2c853244075c2d58469f08013f2ed6a1b03bbe51bb5a
6007d70cc3173f3039a472489995dad2781e8d749be1f1aa209b0bf2f190a4b4
O=c1[nH]c(=O)n(-c2ccccc2)c(=O)[nH]1
Br-[CH2;D2;+0:1]-[C:2](=[O;D1;H0:3])-[#8:4]-[C:5].[C;D1;H3:6]-[#7;a:7]1:[c:8]:[#7;a:9](-[c:10]):[c:11](=[O;D1;H0:12]):[nH;D2;+0:13]:[c:14]:1=[O;D1;H0:15]>>[C:5]-[#8:4]-[C:2](=[O;D1;H0:3])-[CH2;D2;+0:1]-[n;H0;D3;+0:13]1:[c:11](=[O;D1;H0:12]):[#7;a:9](-[c:10]):[c:8]:[#7;a:7](-[C;D1;H3:6]):[c:14]:1=[O;D1;H0:15]
92.4
[{"value": 92.4, "product": "ClC1=C(C=CC(=C1)F)N1C(N(C(N(C1=O)C)=O)CC(=O)OC(C)C)=O", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
2
HOUR
A mixture of 1-(2-chloro-4-fluorophenyl)-3-methyl-s-triazine-2,4,6(1H,3H,5H)-trione (40.9 g, 0.150 mol), potassium carbonate (31.1 g, 0.225 mol) and isopropyl bromoacetate (29.1 mL, 0.225 mol) in N,N-dimethylformamide is stirred at room temperature for 2 hours, poured into water and extracted with ethyl acetate. The or...
10.6084/m9.figshare.5104873.v1
null
Primary halide.Ester
Ester
c1ncncn1
c1ncncn1
c1ncncn1.c1ccccc1
HBr
CN(C=O)C.CCOCC.C(Cl)Cl
null
2
CC(C)OC(=O)CBr.Cn1c(=O)[nH]c(=O)n(-c2ccc(F)cc2Cl)c1=O>CN(C=O)C.CCOCC.C(Cl)Cl>CC(C)OC(=O)Cn1c(=O)n(C)c(=O)n(-c2ccc(F)cc2Cl)c1=O
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-3e822e48328449ad872c68dab16e1be0
CC(C)OC(=O)Cn1c(=O)n(C)c(=O)n(-c2ccc(F)cc2Cl)c1=O.O=[N+]([O-])O>>Cn1c(=O)n(CC(=O)O)c(=O)n(-c2cc([N+](=O)[O-])c(F)cc2Cl)c1=O
[N+](=O)(O)[O-].ClC1=C(C=CC(=C1)F)N1C(N(C(N(C1=O)C)=O)CC(=O)OC(C)C)=O.[N+](=O)(O)[O-].[N+](=O)(O)[O-].[N+](=O)(O)[O-]>>ClC1=C(C=C(C(=C1)F)[N+](=O)[O-])N1C(N(C(N(C1=O)C)=O)CC(=O)O)=O
CC(C)[O:9][C:7]([CH2:6][n:5]1[c:3](=[O:4])[n:2]([CH3:1])[c:24](=[O:25])[n:12](-[c:13]2[cH:14][cH:15][c:19]([F:20])[cH:21][c:22]2[Cl:23])[c:10]1=[O:11])=[O:8].O[N+:16](=[O:17])[O-:18]>>[CH3:1][n:2]1[c:3](=[O:4])[n:5]([CH2:6][C:7](=[O:8])[OH:9])[c:10](=[O:11])[n:12](-[c:13]2[cH:14][c:15]([N+:16](=[O:17])[O-:18])[c:19]([F...
CC(C)OC(=O)Cn1c(=O)n(C)c(=O)n(-c2ccc(F)cc2Cl)c1=O.O=[N+]([O-])O
Cn1c(=O)n(CC(=O)O)c(=O)n(-c2cc([N+](=O)[O-])c(F)cc2Cl)c1=O
null
null
S(O)(O)(=O)=O
Functional Group Addition
OtherReaction
749ba82328ac86653dcc57dc3bef14c2a0842e6e973f7cf55c9a50f90810e24e
a9f52bf538fe1f8e7ae329cb07f47e34e1583577eae763d4cc94b0decd80b1c6
O=c1[nH]c(=O)n(-c2ccccc2)c(=O)[nH]1
C-C(-C)-[O;H0;D2;+0:1]-[C:2](-[C:3])=[O;D1;H0:4].[F;D1;H0:5]-[c:6](:[c:7]):[cH;D2;+0:8]:[c:9]:[c:10].O-[N+;H0;D3:11](-[O;-;D1;H0:12])=[O;D1;H0:13]>>[C:3]-[C:2](=[O;D1;H0:4])-[OH;D1;+0:1].[F;D1;H0:5]-[c:6](:[c:7]):[c;H0;D3;+0:8](-[N+;H0;D3:11](-[O;-;D1;H0:12])=[O;D1;H0:13]):[c:9]:[c:10]
null
[]
null
null
8
HOUR
A solution of isopropyl 3-(2-chloro-4-fluorophenyl)tetrahydro-5-methyl-2,4,6-trioxo-s-triazine-1(2H)-acetate (48.7 g, 0.0508 mol) in concentrated sulfuric acid is cooled to 0° C., treated with 90% nitric acid (2.6 mL), stirred at room temperature overnight, treated with 90% nitric acid (1.0 mL), stirred for 4 hours, tr...
10.6084/m9.figshare.5104873.v1
null
Ester.Nitrate
Carboxylic acid.Nitro group
c1ccccc1
c1ccccc1
c1ncncn1.c1ccccc1
HO-
S(O)(O)(=O)=O
null
8
CC(C)OC(=O)Cn1c(=O)n(C)c(=O)n(-c2ccc(F)cc2Cl)c1=O.O=[N+]([O-])O>S(O)(O)(=O)=O>Cn1c(=O)n(CC(=O)O)c(=O)n(-c2cc([N+](=O)[O-])c(F)cc2Cl)c1=O
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-9280354c10d14447b163cc4be4526af1
CC(C)O.Cn1c(=O)n(CC(=O)O)c(=O)n(-c2cc([N+](=O)[O-])c(F)cc2Cl)c1=O>>CC(C)OC(=O)Cn1c(=O)n(C)c(=O)n(-c2cc([N+](=O)[O-])c(F)cc2Cl)c1=O
ClC1=C(C=C(C(=C1)F)[N+](=O)[O-])N1C(N(C(N(C1=O)C)=O)CC(=O)O)=O.S(O)(O)(=O)=O.CC(C)O>>ClC1=C(C=C(C(=C1)F)[N+](=O)[O-])N1C(N(C(N(C1=O)C)=O)CC(=O)OC(C)C)=O
[CH3:1][CH:2]([CH3:3])[OH:4].O[C:5](=[O:6])[CH2:7][n:8]1[c:9](=[O:10])[n:11]([CH3:12])[c:13](=[O:14])[n:15](-[c:16]2[cH:17][c:18]([N+:19](=[O:20])[O-:21])[c:22]([F:23])[cH:24][c:25]2[Cl:26])[c:27]1=[O:28]>>[CH3:1][CH:2]([CH3:3])[O:4][C:5](=[O:6])[CH2:7][n:8]1[c:9](=[O:10])[n:11]([CH3:12])[c:13](=[O:14])[n:15](-[c:16]2[...
CC(C)O.Cn1c(=O)n(CC(=O)O)c(=O)n(-c2cc([N+](=O)[O-])c(F)cc2Cl)c1=O
CC(C)OC(=O)Cn1c(=O)n(C)c(=O)n(-c2cc([N+](=O)[O-])c(F)cc2Cl)c1=O
null
null
null
Protection
Esterification of Carboxylic Acids
624bf219458ba212c982344d7c3d6088244bf818423b8912fbf03efe5373c5bf
547c73c17c71bc10d21cd3cdbafe9d7a279f866fe729eea28fdc1be18f1a2791
O=c1[nH]c(=O)n(-c2ccccc2)c(=O)[nH]1
O-[C;H0;D3;+0:1](=[O;D1;H0:2])-[C:3]-[#7;a:4].[C;D1;H3:5]-[C:6](-[C;D1;H3:7])-[OH;D1;+0:8]>>[#7;a:4]-[C:3]-[C;H0;D3;+0:1](=[O;D1;H0:2])-[O;H0;D2;+0:8]-[C:6](-[C;D1;H3:5])-[C;D1;H3:7]
null
[]
null
null
null
null
A solution of 3-(2-chloro-4-fluoro-5-nitrophenyl)-tetrahydro-5-methyl-2,4,6-trioxo-s-triazine-1(2H)-acetic acid (43.6 g, 0.105 mol) and concentrated sulfuric acid (25 mL) in 2-propanol (300 mL) is refluxed for 12 hours, cooled to room temperature and filtered to obtain a solid. The solid is dried to give the title prod...
10.6084/m9.figshare.5104873.v1
null
Carboxylic acid.Secondary alcohol
Ester
null
null
c1ncncn1.c1ccccc1
HO-
null
null
null
CC(C)O.Cn1c(=O)n(CC(=O)O)c(=O)n(-c2cc([N+](=O)[O-])c(F)cc2Cl)c1=O>>CC(C)OC(=O)Cn1c(=O)n(C)c(=O)n(-c2cc([N+](=O)[O-])c(F)cc2Cl)c1=O
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-94f05994d0a745e9988e389fe7fb1fc2
CC(C)OC(=O)Cn1c(=O)n(C)c(=O)n(-c2cc([N+](=O)[O-])c(F)cc2Cl)c1=O>>CC(C)OC(=O)Cn1c(=O)n(C)c(=O)n(-c2cc(N)c(F)cc2Cl)c1=O
[H][H].ClC1=C(C=C(C(=C1)F)[N+](=O)[O-])N1C(N(C(N(C1=O)C)=O)CC(=O)OC(C)C)=O.[H][H].CCOCC>>NC=1C(=CC(=C(C1)N1C(N(C(N(C1=O)C)=O)CC(=O)OC(C)C)=O)Cl)F
O=[N+:19]([O-])[c:18]1[cH:17][c:16](-[n:15]2[c:13](=[O:14])[n:11]([CH3:12])[c:9](=[O:10])[n:8]([CH2:7][C:5]([O:4][CH:2]([CH3:1])[CH3:3])=[O:6])[c:25]2=[O:26])[c:23]([Cl:24])[cH:22][c:20]1[F:21]>>[CH3:1][CH:2]([CH3:3])[O:4][C:5](=[O:6])[CH2:7][n:8]1[c:9](=[O:10])[n:11]([CH3:12])[c:13](=[O:14])[n:15](-[c:16]2[cH:17][c:18...
CC(C)OC(=O)Cn1c(=O)n(C)c(=O)n(-c2cc([N+](=O)[O-])c(F)cc2Cl)c1=O
CC(C)OC(=O)Cn1c(=O)n(C)c(=O)n(-c2cc(N)c(F)cc2Cl)c1=O
null
[Pt].[Pt]
C(Cl)Cl.C(C)(=O)OCC
Reduction
Reduction of nitro groups to amines
bbc242b150a51e69d3ad1caaa391f4422710431b398dcb880555f476706790be
7b0317532ea57a4fcedc1efc3e3c22eb5238d1c8330da53d4f9801fc2391f567
O=c1[nH]c(=O)n(-c2ccccc2)c(=O)[nH]1
O=[N+;H0;D3:1](-[O-])-[c:2](:[c:3]):[c:4]>>[NH2;D1;+0:1]-[c:2](:[c:3]):[c:4]
null
[]
null
null
null
null
A mixture of isopropyl 3-(2-chloro-4-fluoro-5-nitrophenyl)tetrahydro-5-methyl-2,4,6-trioxo-s-triazine-1(2H)-acetate (34.8 g, 0.0835 mol) and 5% platinum on carbon (3.48 g) in ethyl acetate is hydrogenated until about 90 psi of hydrogen is taken up. The reaction mixture is then filtered and concentrated in vacuo to obta...
10.6084/m9.figshare.5104873.v1
null
Nitro group
Primary amine
null
null
c1ncncn1.c1ccccc1
Other
[Pt].[Pt].C(Cl)Cl.C(C)(=O)OCC
null
null
CC(C)OC(=O)Cn1c(=O)n(C)c(=O)n(-c2cc([N+](=O)[O-])c(F)cc2Cl)c1=O>[Pt].[Pt].C(Cl)Cl.C(C)(=O)OCC>CC(C)OC(=O)Cn1c(=O)n(C)c(=O)n(-c2cc(N)c(F)cc2Cl)c1=O
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-0ea27041f7c3480cb095d9b064085a09
CCOC(=O)C(Br)CBr.NCCS>>CCOC(=O)C1CSCCN1
NCCS.C(C)N(CC)CC.BrC(C(=O)OCC)CBr.C(Cl)(Cl)Cl.C1(=CC=CC=C1)C>>N1C(CSCC1)C(=O)OCC
Br[CH:6]([C:4]([O:3][CH2:2][CH3:1])=[O:5])[CH2:7]Br.[SH:8][CH2:9][CH2:10][NH2:11]>>[CH3:1][CH2:2][O:3][C:4](=[O:5])[CH:6]1[CH2:7][S:8][CH2:9][CH2:10][NH:11]1
CCOC(=O)C(Br)CBr.NCCS
CCOC(=O)C1CSCCN1
null
null
C(Cl)(Cl)Cl
Heteroatom Alkylation and Arylation
OtherReaction
134ffb04ad0575590e84053a59e6706e87e197197b1d439a5da6a271d27904ca
16dd093b51b23984a6b8d17db3e4d7c993697754e7fc0e4d8a19aecb6fefa1c8
C1CSCCN1
Br-[CH2;D2;+0:1]-[CH;D3;+0:2](-Br)-[C:3](=[O;D1;H0:4])-[#8:5]-[C:6].[NH2;D1;+0:7]-[C:8]-[C:9]-[SH;D1;+0:10]>>[C:6]-[#8:5]-[C:3](=[O;D1;H0:4])-[CH;D3;+0:2]1-[CH2;D2;+0:1]-[S;H0;D2;+0:10]-[C:9]-[C:8]-[NH;D2;+0:7]-1
null
[]
null
null
2.5
HOUR
A warm solution of 2-aminoethanethiol (10.0 g, 0.130 mol) and triethylamine (36 mL, 0.260 mol) in chloroform is added over 5 minutes to a solution of ethyl 2,3-di-bromopropionate (33.9 g, 0.130 mol) in a chloroform/toluene (1:1.6) solution. The reaction mixture is stirred at room temperature for 2.5 hours, filtered and...
10.6084/m9.figshare.5104873.v1
null
Secondary halide.Primary halide.Ester.Primary amine.Aliphatic thiol
Ester.Secondary amine.Monosulfide
null
C1CSCCN1
C1CSCCN1
HBr
C(Cl)(Cl)Cl
null
2.5
CCOC(=O)C(Br)CBr.NCCS>C(Cl)(Cl)Cl>CCOC(=O)C1CSCCN1
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-9c45683f083c467ebf79ecae3d3dc9a0
CC(C)OC(=O)Cn1c(=O)n(C)c(=O)n(-c2cc(N3C(=O)C4CSCCN4C3=O)c(F)cc2Cl)c1=O.[O-][I+3]([O-])([O-])[O-]>>CC(C)OC(=O)Cn1c(=O)n(C)c(=O)n(-c2cc(N3C(=O)C4CS(=O)CCN4C3=O)c(F)cc2Cl)c1=O
ClC1=C(C=C(C(=C1)F)N1C(N2C(CSCC2)C1=O)=O)N1C(N(C(N(C1=O)C)=O)CC(=O)OC(C)C)=O.CCOCC.I(=O)(=O)(=O)[O-].[Na+]>>ClC1=C(C=C(C(=C1)F)N1C(N2C(CS(CC2)=O)C1=O)=O)N1C(N(C(N(C1=O)C)=O)CC(=O)OC(C)C)=O
[CH3:1][CH:2]([CH3:3])[O:4][C:5](=[O:6])[CH2:7][n:8]1[c:9](=[O:10])[n:11]([CH3:12])[c:13](=[O:14])[n:15](-[c:16]2[cH:17][c:18]([N:19]3[C:20](=[O:21])[CH:22]4[CH2:23][S:24][CH2:26][CH2:27][N:28]4[C:29]3=[O:30])[c:31]([F:32])[cH:33][c:34]2[Cl:35])[c:36]1=[O:37].[O-][I+3]([O-])([O-])[O-:25]>>[CH3:1][CH:2]([CH3:3])[O:4][C:...
CC(C)OC(=O)Cn1c(=O)n(C)c(=O)n(-c2cc(N3C(=O)C4CSCCN4C3=O)c(F)cc2Cl)c1=O.[O-][I+3]([O-])([O-])[O-]
CC(C)OC(=O)Cn1c(=O)n(C)c(=O)n(-c2cc(N3C(=O)C4CS(=O)CCN4C3=O)c(F)cc2Cl)c1=O
null
null
CO.C(Cl)Cl.O
Oxidation
OtherReaction
b4a0685a09bdb9688c5dc9373a81bcecf915198f73d178e3ae74b21a40965ff4
f5f6bb6ca76a2267cd589767b4d67e7a17ab1ac383eeb6143dcd5d92e00e1b6a
O=C1C2CS(=O)CCN2C(=O)N1c1cccc(-n2c(=O)[nH]c(=O)[nH]c2=O)c1
[#7:1]-[C:2](=[O;D1;H0:3])-[C:4]1-[#7:5]-[C:6]-[C:7]-[S;H0;D2;+0:8]-[C:9]-1.[O-;H0;D1:10]-[I+3](-[O-])(-[O-])-[O-]>>[#7:1]-[C:2](=[O;D1;H0:3])-[C:4]1-[#7:5]-[C:6]-[C:7]-[S;H0;D3;+0:8](=[O;H0;D1;+0:10])-[C:9]-1
60.4
[{"value": 60.4, "product": "ClC1=C(C=C(C(=C1)F)N1C(N2C(CS(CC2)=O)C1=O)=O)N1C(N(C(N(C1=O)C)=O)CC(=O)OC(C)C)=O", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
8
HOUR
A mixture of isopropyl 3-{2-chloro-4-fluoro-5-[5,6,8,8a-tetrahydro-1,3-dioxo-1H-imidazo[5,1-c][1,4]-thiazin-2(3H)-yl]phenyl}tetrahydro-5-methyl-2,4,6-trioxo-s-triazine-1(2H)-acetate (0.95 g, 1.75 mmol) in methanol (10 mL) is added over 15 minutes to a solution of sodium periodate (0.38 g, 1.78 mmol) in water (10 mL) wh...
10.6084/m9.figshare.5104873.v1
null
Monosulfide
Sulfoxide
C1CN2C[NH]CC2CS1
C1CN2C[NH]CC2CS1
c1ncncn1.c1ccccc1.C1CN2C[NH]CC2CS1
I-
CO.C(Cl)Cl.O
null
8
CC(C)OC(=O)Cn1c(=O)n(C)c(=O)n(-c2cc(N3C(=O)C4CSCCN4C3=O)c(F)cc2Cl)c1=O.[O-][I+3]([O-])([O-])[O-]>CO.C(Cl)Cl.O>CC(C)OC(=O)Cn1c(=O)n(C)c(=O)n(-c2cc(N3C(=O)C4CS(=O)CCN4C3=O)c(F)cc2Cl)c1=O
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-0c36063e545e437080a0d9f9f89c2a06
BrCCCCBr.CCOC(=O)NNC(=O)OCC>>CCOC(=O)N1CCCCN1C(=O)OCC
BrCCCCBr.C(=O)(OCC)NNC(=O)OCC.C([O-])([O-])=O.[K+].[K+]>>N1(N(CCCC1)C(=O)OCC)C(=O)OCC
Br[CH2:7][CH2:8][CH2:9][CH2:10]Br.[CH3:1][CH2:2][O:3][C:4](=[O:5])[NH:6][NH:11][C:12](=[O:13])[O:14][CH2:15][CH3:16]>>[CH3:1][CH2:2][O:3][C:4](=[O:5])[N:6]1[CH2:7][CH2:8][CH2:9][CH2:10][N:11]1[C:12](=[O:13])[O:14][CH2:15][CH3:16]
BrCCCCBr.CCOC(=O)NNC(=O)OCC
CCOC(=O)N1CCCCN1C(=O)OCC
null
null
C(C)#N
Heteroatom Alkylation and Arylation
OtherReaction
859f3f5b982cf00cd48ce4dee0b290a672abab0fa4228379433ae95e128d543b
9b2df4ffc85c3bfa472caf43fa08b1e61cbf4a7b843972afe9671fab932acf35
C1CCNNC1
Br-[CH2;D2;+0:1]-[C:2]-[C:3]-[CH2;D2;+0:4]-Br.[C:5]-[#8:6]-[C:7](=[O;D1;H0:8])-[NH;D2;+0:9]-[NH;D2;+0:10]-[C:11](=[O;D1;H0:12])-[#8:13]-[C:14]>>[C:5]-[#8:6]-[C:7](=[O;D1;H0:8])-[N;H0;D3;+0:9]1-[CH2;D2;+0:1]-[C:2]-[C:3]-[CH2;D2;+0:4]-[N;H0;D3;+0:10]-1-[C:11](=[O;D1;H0:12])-[#8:13]-[C:14]
69.4
[{"value": 69.4, "product": "N1(N(CCCC1)C(=O)OCC)C(=O)OCC", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
null
null
1,4-Dibromobutane (81.4 mL, 0.682 mol) is added over 1 hour to a mixture of 1,2-dicarbethoxyhydrazine (100 g, 0.568 mol) and potassium carbonate (158 g, 1.14 mol) in acetonitrile (600 mL). The resultant reaction mixture is refluxed for 6 hours, cooled to room temperature, and filtered. The filtrate is concentrated in v...
10.6084/m9.figshare.5104873.v1
null
Acylhydrazine.Acylhydrazine.Primary halide.Primary halide
Acylhydrazine.Acylhydrazine.Carbamic ester.Carbamic ester
null
C1CC[NH][NH]C1
C1CC[NH][NH]C1
HBr
C(C)#N
null
null
BrCCCCBr.CCOC(=O)NNC(=O)OCC>C(C)#N>CCOC(=O)N1CCCCN1C(=O)OCC
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-abde48b4f1894595a808afe5690eeb6d
CC(C)OC(=O)Cn1c(=O)n(C)c(=O)n(-c2cc(N)c(F)cc2Cl)c1=O.S=C(Cl)Cl>>CC(C)OC(=O)Cn1c(=O)n(C)c(=O)n(-c2cc(N=C=S)c(F)cc2Cl)c1=O
C(=S)(Cl)Cl.NC=1C(=CC(=C(C1)N1C(N(C(N(C1=O)C)=O)CC(=O)OC(C)C)=O)Cl)F.C(C)N(CC)CC>>ClC1=C(C=C(C(=C1)F)N=C=S)N1C(N(C(N(C1=O)C)=O)CC(=O)OC(C)C)=O
[CH3:1][CH:2]([CH3:3])[O:4][C:5](=[O:6])[CH2:7][n:8]1[c:9](=[O:10])[n:11]([CH3:12])[c:13](=[O:14])[n:15](-[c:16]2[cH:17][c:18]([NH2:19])[c:22]([F:23])[cH:24][c:25]2[Cl:26])[c:27]1=[O:28].Cl[C:20](Cl)=[S:21]>>[CH3:1][CH:2]([CH3:3])[O:4][C:5](=[O:6])[CH2:7][n:8]1[c:9](=[O:10])[n:11]([CH3:12])[c:13](=[O:14])[n:15](-[c:16]...
CC(C)OC(=O)Cn1c(=O)n(C)c(=O)n(-c2cc(N)c(F)cc2Cl)c1=O.S=C(Cl)Cl
CC(C)OC(=O)Cn1c(=O)n(C)c(=O)n(-c2cc(N=C=S)c(F)cc2Cl)c1=O
null
null
O1CCCC1
Heteroatom Alkylation and Arylation
Amine and thiophosgene to isothiocyanate
1226380c52141f79542a4f85564c11e38ca245efc80be1557b635219a638388c
e5752ca9983a57ab07a0b76a5c8a57a6667ab2cd460616b960134623ec0fce31
O=c1[nH]c(=O)n(-c2ccccc2)c(=O)[nH]1
Cl-[C;H0;D3;+0:1](-Cl)=[S;D1;H0:2].[NH2;D1;+0:3]-[c:4](:[c:5]):[c:6]>>[S;D1;H0:2]=[C;H0;D2;+0:1]=[N;H0;D2;+0:3]-[c:4](:[c:5]):[c:6]
null
[]
null
null
4
HOUR
Thiophosgene (0.50 mL, 6.5 mmol) is added over 45 minutes to a solution of isopropyl 3-(5-amino-2-chloro-4-fluorophenyl)tetrahydro-5-methyl-2,4,6-trioxo-s-triazine-1(2H)-acetate (2.5 g, 6.5 mmol), and triethylamine (1.8 mL, 13.0 mmol) in tetrahydrofuran. The reaction mixture is stirred at room temperature for 4 hours, ...
10.6084/m9.figshare.5104873.v1
null
Alkenyl halide.Alkenyl halide.Primary amine
Isothiocyanate
null
null
c1ncncn1.c1ccccc1
HCl
O1CCCC1
null
4
CC(C)OC(=O)Cn1c(=O)n(C)c(=O)n(-c2cc(N)c(F)cc2Cl)c1=O.S=C(Cl)Cl>O1CCCC1>CC(C)OC(=O)Cn1c(=O)n(C)c(=O)n(-c2cc(N=C=S)c(F)cc2Cl)c1=O
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-2e03a241be2b4b53bf88ccfacb21967f
CC(=O)Cl.Nc1ccc(Cl)cc1F>>CC(=O)Nc1ccc(Cl)cc1F
C(C)(=O)OCC.C(C)(=O)Cl.ClC1=CC(=C(N)C=C1)F.C(C)N(CC)CC>>ClC1=CC(=C(NC(C)=O)C=C1)F
Cl[C:2]([CH3:1])=[O:3].[NH2:4][c:5]1[cH:6][cH:7][c:8]([Cl:9])[cH:10][c:11]1[F:12]>>[CH3:1][C:2](=[O:3])[NH:4][c:5]1[cH:6][cH:7][c:8]([Cl:9])[cH:10][c:11]1[F:12]
CC(=O)Cl.Nc1ccc(Cl)cc1F
CC(=O)Nc1ccc(Cl)cc1F
null
null
C(C)O.O1CCCC1
Acylation
Acylation of Nitrogen Nucleophiles by Acyl/Thioacyl/Carbamoyl Halides and Analogs_OS
38143a4d536201990008fd6f2c68e6571a341d1c367481869fbbbe36cb038937
0e6ae078978e324f714e184b4f72826d4e3bf2d9ab22d6e9f73740af687be16f
c1ccccc1
Cl-[C;H0;D3;+0:1](-[C;D1;H3:2])=[O;D1;H0:3].[NH2;D1;+0:4]-[c:5](:[c:6]):[c:7]>>[C;D1;H3:2]-[C;H0;D3;+0:1](=[O;D1;H0:3])-[NH;D2;+0:4]-[c:5](:[c:6]):[c:7]
null
[]
null
null
8
HOUR
Acetyl chloride (24.2 mL, 0.34 mol) is added slowly to a solution of 4-chloro-2-fluoroaniline (49.4 g, 0.34 mol), and triethylamine (47 mL, 0.34 mol) in tetrahydrofuran while maintaining the reaction mixture temperature below 20° C. After the addition is complete, the reaction mixture is stirred overnight at room tempe...
10.6084/m9.figshare.5104873.v1
null
Acyl halide.Primary amine
Secondary amide
null
null
c1ccccc1
HCl
C(C)O.O1CCCC1
null
8
CC(=O)Cl.Nc1ccc(Cl)cc1F>C(C)O.O1CCCC1>CC(=O)Nc1ccc(Cl)cc1F
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-b4cbb9aa494e49f7b3f195512e6252b9
CC(=O)Nc1ccc(Cl)cc1F.O=[N+]([O-])O>>CC(=O)Nc1cc([N+](=O)[O-])c(Cl)cc1F
ClC1=CC(=C(NC(C)=O)C=C1)F.[N+](=O)(O)[O-]>>ClC1=CC(=C(NC(C)=O)C=C1[N+](=O)[O-])F
[CH3:1][C:2](=[O:3])[NH:4][c:5]1[cH:6][cH:7][c:11]([Cl:12])[cH:13][c:14]1[F:15].O[N+:8](=[O:9])[O-:10]>>[CH3:1][C:2](=[O:3])[NH:4][c:5]1[cH:6][c:7]([N+:8](=[O:9])[O-:10])[c:11]([Cl:12])[cH:13][c:14]1[F:15]
CC(=O)Nc1ccc(Cl)cc1F.O=[N+]([O-])O
CC(=O)Nc1cc([N+](=O)[O-])c(Cl)cc1F
null
null
S(O)(O)(=O)=O
Functional Group Addition
Aromatic nitration with HNO3
53848b8b2bb4e867226e49db2e60519b24be9379900e3ad7c56af54fe8fde7a5
ddce49825c02b8965f10c8d99e3c841d26e1f136da6037b417c09313e6d73097
c1ccccc1
O-[N+;H0;D3:1](-[O;-;D1;H0:2])=[O;D1;H0:3].[Cl;D1;H0:4]-[c:5](:[c:6]):[cH;D2;+0:7]:[c:8]:[c:9]>>[Cl;D1;H0:4]-[c:5](:[c:6]):[c;H0;D3;+0:7](-[N+;H0;D3:1](-[O;-;D1;H0:2])=[O;D1;H0:3]):[c:8]:[c:9]
null
[]
0
CELSIUS
10
MINUTE
A mixture of 4'-chloro-2'-fluoroacetanilide (51 g, 0.272 mol) in concentrated sulfuric acid (100 mL) is cooled to 0° C., treated with nitric acid (90% real, 14 mL, 0.300 mol) over 45 minutes, stirred for 10 minutes, and poured onto ice. The resultant aqueous mixture is filtered to obtain a tan solid which is washed wit...
10.6084/m9.figshare.5104873.v1
null
Nitrate
Nitro group
c1ccccc1
c1ccccc1
c1ccccc1
HO-
S(O)(O)(=O)=O
0
0.166667
CC(=O)Nc1ccc(Cl)cc1F.O=[N+]([O-])O>S(O)(O)(=O)=O>CC(=O)Nc1cc([N+](=O)[O-])c(Cl)cc1F
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-fdb5cf4636964e228521df4be25b6c2c
CC(=O)Nc1cc([N+](=O)[O-])c(Cl)cc1F>>CC(=O)Nc1cc(N)c(Cl)cc1F
ClC1=CC(=C(NC(C)=O)C=C1[N+](=O)[O-])F.[H][H]>>NC=1C(=CC(=C(NC(C)=O)C1)F)Cl
O=[N+:8]([O-])[c:7]1[cH:6][c:5]([NH:4][C:2]([CH3:1])=[O:3])[c:12]([F:13])[cH:11][c:9]1[Cl:10]>>[CH3:1][C:2](=[O:3])[NH:4][c:5]1[cH:6][c:7]([NH2:8])[c:9]([Cl:10])[cH:11][c:12]1[F:13]
CC(=O)Nc1cc([N+](=O)[O-])c(Cl)cc1F
CC(=O)Nc1cc(N)c(Cl)cc1F
null
[Pt]
C(C)O.O1CCCC1
Reduction
Reduction of nitro groups to amines
bbc242b150a51e69d3ad1caaa391f4422710431b398dcb880555f476706790be
7b0317532ea57a4fcedc1efc3e3c22eb5238d1c8330da53d4f9801fc2391f567
c1ccccc1
O=[N+;H0;D3:1](-[O-])-[c:2](:[c:3]):[c:4]>>[NH2;D1;+0:1]-[c:2](:[c:3]):[c:4]
null
[]
null
null
null
null
A mixture of 4'-chloro-2'-fluoro-5'-nitroacetanilide (35.2 g, 151 mmol), and 5% platinum on carbon (7.0 g, 20 wt/wt %) in an ethanol/tetrahydrofuran (2:1) solution is hydrogenated until 28 psi of hydrogen is taken up. The reaction mixture is then filtered, and concentrated in vacuo to give the title product as a tan so...
10.6084/m9.figshare.5104873.v1
null
Nitro group
Primary amine
null
null
c1ccccc1
Other
[Pt].C(C)O.O1CCCC1
null
null
CC(=O)Nc1cc([N+](=O)[O-])c(Cl)cc1F>[Pt].C(C)O.O1CCCC1>CC(=O)Nc1cc(N)c(Cl)cc1F
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-5a556d937a384abda5eb0822445fcd79
C#CCN.CC(=O)Nc1cc(N)c(Cl)cc1F.O=C(Cl)Oc1ccccc1>>C#CCNC(=O)Nc1cc(NC(C)=O)c(F)cc1Cl
C(C#C)N.NC=1C(=CC(=C(NC(C)=O)C1)F)Cl.C(C)N(CC)CC.C1(=CC=CC=C1)OC(=O)Cl>>C(C)(=O)NC=1C(=CC(=C(C1)NC(=O)NCC#C)Cl)F
[CH:1]#[C:2][CH2:3][NH2:4].[NH2:7][c:8]1[cH:9][c:10]([NH:11][C:12]([CH3:13])=[O:14])[c:15]([F:16])[cH:17][c:18]1[Cl:19].Cl[C:5](Oc1ccccc1)=[O:6]>>[CH:1]#[C:2][CH2:3][NH:4][C:5](=[O:6])[NH:7][c:8]1[cH:9][c:10]([NH:11][C:12]([CH3:13])=[O:14])[c:15]([F:16])[cH:17][c:18]1[Cl:19]
C#CCN.CC(=O)Nc1cc(N)c(Cl)cc1F.O=C(Cl)Oc1ccccc1
C#CCNC(=O)Nc1cc(NC(C)=O)c(F)cc1Cl
null
null
O.C(C)(=O)OCC.O1CCCC1
Acylation
OtherReaction
8991b331000413918f835d1c1bbc39cacc8c099ebed044fdd14fbbac35025775
9e21e129777f166dc879d63e1b5cf3ebfee62ae901ede29dec0cc02d1fd57a7f
c1ccccc1
Cl-[C;H0;D3;+0:1](=[O;D1;H0:2])-O-c1:c:c:c:c:c:1.[C;D1;H1:3]#[C:4]-[C:5]-[NH2;D1;+0:6].[NH2;D1;+0:7]-[c:8](:[c:9]):[c:10]>>[C;D1;H1:3]#[C:4]-[C:5]-[NH;D2;+0:6]-[C;H0;D3;+0:1](=[O;D1;H0:2])-[NH;D2;+0:7]-[c:8](:[c:9]):[c:10]
null
[]
null
null
75
MINUTE
A solution of 5'-amino-4'-chloro-2'-fluoroacetanilide (11.25 g, 55.6 mmol), and triethylamine (7.70 mL, 55.6 mmol) in tetrahydrofuran is added dropwise to a stirred solution of phenylchloroformate (8.70 mL, 69.4 mmol) in tetrahydrofuran while maintaining the reaction mixture temperature at 25°-30° C. After the addition...
10.6084/m9.figshare.5104873.v1
null
Acyl halide.Ether.Primary amine.Primary amine
Urea
c1ccccc1
null
c1ccccc1
HCl
O.C(C)(=O)OCC.O1CCCC1
null
1.25
C#CCN.CC(=O)Nc1cc(N)c(Cl)cc1F.O=C(Cl)Oc1ccccc1>O.C(C)(=O)OCC.O1CCCC1>C#CCNC(=O)Nc1cc(NC(C)=O)c(F)cc1Cl
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-9562367f4fb64f8a9fa6a9e9643f95bb
C#CCNC(=O)Nc1cc(NC(C)=O)c(F)cc1Cl.O=C=NC(=O)Cl>>C#CCn1c(=O)[nH]c(=O)n(-c2cc(NC(C)=O)c(F)cc2Cl)c1=O
C(C)(=O)NC=1C(=CC(=C(C1)NC(=O)NCC#C)Cl)F.N1=CC=CC=C1.N1=CC=CC=C1.C(=NC(=O)Cl)=O.C(=NC(=O)Cl)=O>>ClC1=CC(=C(NC(C)=O)C=C1N1C(N(C(NC1=O)=O)CC#C)=O)F
[CH:1]#[C:2][CH2:3][NH:4][C:23]([NH:10][c:11]1[cH:12][c:13]([NH:14][C:15]([CH3:16])=[O:17])[c:18]([F:19])[cH:20][c:21]1[Cl:22])=[O:24].Cl[C:5](=[O:6])[N:7]=[C:8]=[O:9]>>[CH:1]#[C:2][CH2:3][n:4]1[c:5](=[O:6])[nH:7][c:8](=[O:9])[n:10](-[c:11]2[cH:12][c:13]([NH:14][C:15]([CH3:16])=[O:17])[c:18]([F:19])[cH:20][c:21]2[Cl:22...
C#CCNC(=O)Nc1cc(NC(C)=O)c(F)cc1Cl.O=C=NC(=O)Cl
C#CCn1c(=O)[nH]c(=O)n(-c2cc(NC(C)=O)c(F)cc2Cl)c1=O
null
null
C(Cl)Cl
Aromatic Heterocycle Formation
OtherReaction
d450124a69c05c689cc30827449dfbc10d3158a711cfc2b694f01c10cd664df3
79088c5104e3c5a05b4759d3458d7361a5024a2ee1cbcc7fd6e408b3e17df989
O=c1[nH]c(=O)n(-c2ccccc2)c(=O)[nH]1
Cl-[C;H0;D3;+0:1](=[O;D1;H0:2])-[N;H0;D2;+0:3]=[C;H0;D2;+0:4]=[O;D1;H0:5].[C;D1;H1:6]#[C:7]-[C:8]-[NH;D2;+0:9]-[C;H0;D3;+0:10](=[O;D1;H0:11])-[NH;D2;+0:12]-[c;H0;D3;+0:13](:[c:14]:[c:15]):[c:16](-[Cl;D1;H0:17]):[c:18]>>[C;D1;H1:6]#[C:7]-[C:8]-[n;H0;D3;+0:9]1:[c;H0;D3;+0:10](=[O;D1;H0:11]):[n;H0;D3;+0:12](-[c;H0;D3;+0:1...
null
[]
null
null
8
HOUR
A mixture of 1-(5-acetamido-2-chloro-4-fluorophenyl)-3-(2-propynyl)urea (4.50 g, 15.9 mmol), and pyridine (2.56 mL, 31.8 mmol) in methylene chloride is treated with N-(chlorocarbonyl) isocyanate (1.92 mL, 23.9 mmol), stirred at room temperature overnight, refluxed for 90 minutes, cooled to room temperature, treated wit...
10.6084/m9.figshare.5104873.v1
null
Acyl halide.Urea.Isocyanate
null
null
c1ncncn1
c1ncncn1.c1ccccc1
HCl
C(Cl)Cl
null
8
C#CCNC(=O)Nc1cc(NC(C)=O)c(F)cc1Cl.O=C=NC(=O)Cl>C(Cl)Cl>C#CCn1c(=O)[nH]c(=O)n(-c2cc(NC(C)=O)c(F)cc2Cl)c1=O
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-0d9d75ac841d479a9bb6bcb95675d2f3
C#CCn1c(=O)[nH]c(=O)n(-c2cc(NC(C)=O)c(F)cc2Cl)c1=O>>C#CCn1c(=O)[nH]c(=O)n(-c2cc(N)c(F)cc2Cl)c1=O
[OH-].[Na+].ClC1=CC(=C(NC(C)=O)C=C1N1C(N(C(NC1=O)=O)CC#C)=O)F.Cl.C(C)(=O)OCC>>NC=1C(=CC(=C(C1)N1C(N(C(NC1=O)=O)CC#C)=O)Cl)F
CC(=O)[NH:14][c:13]1[cH:12][c:11](-[n:10]2[c:8](=[O:9])[nH:7][c:5](=[O:6])[n:4]([CH2:3][C:2]#[CH:1])[c:20]2=[O:21])[c:18]([Cl:19])[cH:17][c:15]1[F:16]>>[CH:1]#[C:2][CH2:3][n:4]1[c:5](=[O:6])[nH:7][c:8](=[O:9])[n:10](-[c:11]2[cH:12][c:13]([NH2:14])[c:15]([F:16])[cH:17][c:18]2[Cl:19])[c:20]1=[O:21]
C#CCn1c(=O)[nH]c(=O)n(-c2cc(NC(C)=O)c(F)cc2Cl)c1=O
C#CCn1c(=O)[nH]c(=O)n(-c2cc(N)c(F)cc2Cl)c1=O
null
null
C(C)O
Reduction
Hydrogenolysis of amides/imides/carbamates
755df58c254dea764fdda078ffd678ec540bba057c83683be04c253f1270ac7b
025f7cefe51e71668ad5d09fca32df168e9b538347403e4d5c1748073e538adc
O=c1[nH]c(=O)n(-c2ccccc2)c(=O)[nH]1
C-C(=O)-[NH;D2;+0:1]-[c:2](:[c:3]):[c:4]>>[NH2;D1;+0:1]-[c:2](:[c:3]):[c:4]
82.2
[{"value": 82.2, "product": "NC=1C(=CC(=C(C1)N1C(N(C(NC1=O)=O)CC#C)=O)Cl)F", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
null
null
A mixture of 4'-chloro-2'-fluoro-5'-[hexahydro-2,4,6-trioxo-3-(2-propynyl)-s-triazin-1-yl]acetanilide (3.00 g, 8.5 mmol), and 3N hydrochloric acid (25 mL) in ethanol (50 mL) is refluxed for 3 hours, cooled to room temperature, and poured into ethyl acetate. 3N sodium hydroxide solution (25 mL) is added to the organic s...
10.6084/m9.figshare.5104873.v1
null
Secondary amide
Primary amine
null
null
c1ncncn1.c1ccccc1
HO-
C(C)O
null
null
C#CCn1c(=O)[nH]c(=O)n(-c2cc(NC(C)=O)c(F)cc2Cl)c1=O>C(C)O>C#CCn1c(=O)[nH]c(=O)n(-c2cc(N)c(F)cc2Cl)c1=O
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-9fc8235e42584d779056ec0da7bbdc76
C#CCn1c(=O)[nH]c(=O)n(-c2cc(N)c(F)cc2Cl)c1=O.O=C1OC(=O)C2=C1CCCC2>>C#CCn1c(=O)[nH]c(=O)n(-c2cc(N3C(=O)C4=C(CCCC4)C3=O)c(F)cc2Cl)c1=O
NC=1C(=CC(=C(C1)N1C(N(C(NC1=O)=O)CC#C)=O)Cl)F.C1(C2=C(C(=O)O1)CCCC2)=O.C(C)(=O)OCC>>ClC1=CC(=C(C=C1N1C(N(C(NC1=O)=O)CC#C)=O)N1C(=O)C2=C(CCCC2)C1=O)F
[CH:1]#[C:2][CH2:3][n:4]1[c:5](=[O:6])[nH:7][c:8](=[O:9])[n:10](-[c:11]2[cH:12][c:13]([NH2:14])[c:25]([F:26])[cH:27][c:28]2[Cl:29])[c:30]1=[O:31].O1[C:15](=[O:16])[C:17]2=[C:18]([CH2:19][CH2:20][CH2:21][CH2:22]2)[C:23]1=[O:24]>>[CH:1]#[C:2][CH2:3][n:4]1[c:5](=[O:6])[nH:7][c:8](=[O:9])[n:10](-[c:11]2[cH:12][c:13]([N:14]...
C#CCn1c(=O)[nH]c(=O)n(-c2cc(N)c(F)cc2Cl)c1=O.O=C1OC(=O)C2=C1CCCC2
C#CCn1c(=O)[nH]c(=O)n(-c2cc(N3C(=O)C4=C(CCCC4)C3=O)c(F)cc2Cl)c1=O
null
null
C(C)(=O)O
Acylation
OtherReaction
e8011a3b0be1a45acf4cbe99b6add2c178c54f184ca2415e1c1cb07e7aee07ff
2a4a20e639c386292668b0b265a8e1b50d707d5f0576437dc5ade3e7fd444d29
O=C1C2=C(CCCC2)C(=O)N1c1cccc(-n2c(=O)[nH]c(=O)[nH]c2=O)c1
[C:1]-[C:2]1=[C:3](-[C:4])-[C;H0;D3;+0:5](=[O;D1;H0:6])-O-[C;H0;D3;+0:7]-1=[O;D1;H0:8].[NH2;D1;+0:9]-[c:10](:[c:11]):[c:12]>>[C:1]-[C:2]1=[C:3](-[C:4])-[C;H0;D3;+0:5](=[O;D1;H0:6])-[N;H0;D3;+0:9](-[c:10](:[c:11]):[c:12])-[C;H0;D3;+0:7]-1=[O;D1;H0:8]
55.9
[{"value": 55.9, "product": "ClC1=CC(=C(C=C1N1C(N(C(NC1=O)=O)CC#C)=O)N1C(=O)C2=C(CCCC2)C1=O)F", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
null
null
A solution of 1-(5-amino-2-chloro-4-fluorophenyl)-3-(2-propynyl)-s-triazine-2,4,6-(1H,3H,5H)-trione (1.50 g, 4.83 mmol), and 3,4,5,6-tetrahydrophthalic anhydride (0.73 g, 4.83 mmol) in acetic acid (3 mL) is heated at 100° C. for 5 hours, cooled, and poured into ethyl acetate, The organic mixture is washed sequentially ...
10.6084/m9.figshare.5104873.v1
null
Anhydride.Primary amine
Substituted dicarboximide
C1CCC2=C(C1)COC2
C1CCC2=C(C1)C[NH]C2
c1ncncn1.c1ccccc1.C1CCC2=C(C1)C[NH]C2
HO-
C(C)(=O)O
null
null
C#CCn1c(=O)[nH]c(=O)n(-c2cc(N)c(F)cc2Cl)c1=O.O=C1OC(=O)C2=C1CCCC2>C(C)(=O)O>C#CCn1c(=O)[nH]c(=O)n(-c2cc(N3C(=O)C4=C(CCCC4)C3=O)c(F)cc2Cl)c1=O
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-3ce2e94879794c84802f9843f2d4155a
Nc1ccc(Cl)cc1F.O=C1OC(=O)C2=C1CCCC2>>O=C1C2=C(CCCC2)C(=O)N1c1ccc(Cl)cc1F
O.C(C)(=O)OCC.ClC1=CC(=C(N)C=C1)F.C1(C2=C(C(=O)O1)CCCC2)=O.C(C)(=O)OCC.ClC1=CC(=C(N)C=C1)F>>ClC1=CC(=C(C=C1)N1C(=O)C2=C(CCCC2)C1=O)F
[NH2:11][c:12]1[cH:13][cH:14][c:15]([Cl:16])[cH:17][c:18]1[F:19].O1[C:2](=[O:1])[C:3]2=[C:4]([CH2:5][CH2:6][CH2:7][CH2:8]2)[C:9]1=[O:10]>>[O:1]=[C:2]1[C:3]2=[C:4]([CH2:5][CH2:6][CH2:7][CH2:8]2)[C:9](=[O:10])[N:11]1[c:12]1[cH:13][cH:14][c:15]([Cl:16])[cH:17][c:18]1[F:19]
Nc1ccc(Cl)cc1F.O=C1OC(=O)C2=C1CCCC2
O=C1C2=C(CCCC2)C(=O)N1c1ccc(Cl)cc1F
null
null
C(C)(=O)O
Acylation
OtherReaction
e8011a3b0be1a45acf4cbe99b6add2c178c54f184ca2415e1c1cb07e7aee07ff
2a4a20e639c386292668b0b265a8e1b50d707d5f0576437dc5ade3e7fd444d29
O=C1C2=C(CCCC2)C(=O)N1c1ccccc1
[C:1]-[C:2]1=[C:3](-[C:4])-[C;H0;D3;+0:5](=[O;D1;H0:6])-O-[C;H0;D3;+0:7]-1=[O;D1;H0:8].[NH2;D1;+0:9]-[c:10](:[c:11]):[c:12]>>[C:1]-[C:2]1=[C:3](-[C:4])-[C;H0;D3;+0:5](=[O;D1;H0:6])-[N;H0;D3;+0:9](-[c:10](:[c:11]):[c:12])-[C;H0;D3;+0:7]-1=[O;D1;H0:8]
69.3
[{"value": 69.3, "product": "ClC1=CC(=C(C=C1)N1C(=O)C2=C(CCCC2)C1=O)F", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
8
HOUR
A mixture of 4-chloro-2-fluoroaniline (19.0 g, 130.6 mmol), and 3,4,5,6-tetrahydrophthalic anhydride (19.85 g, 130.6 mmol) in acetic acid (150 mL) is refluxed for 2 hours, treated with additional 4-chloro-2-fluoroaniline (3.0 g), refluxed for 90 minutes, stirred at room temperature overnight and poured into a water/eth...
10.6084/m9.figshare.5104873.v1
null
Anhydride.Primary amine
Substituted dicarboximide
C1CCC2=C(C1)COC2
C1CCC2=C(C1)C[NH]C2
C1CCC2=C(C1)C[NH]C2.c1ccccc1
HO-
C(C)(=O)O
null
8
Nc1ccc(Cl)cc1F.O=C1OC(=O)C2=C1CCCC2>C(C)(=O)O>O=C1C2=C(CCCC2)C(=O)N1c1ccc(Cl)cc1F
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-1b12023f2a354fce9ed4c6252aa46b2d
O=C1C2=C(CCCC2)C(=O)N1c1ccc(Cl)cc1F.O=[N+]([O-])O>>O=C1C2=C(CCCC2)C(=O)N1c1cc([N+](=O)[O-])c(Cl)cc1F
ClC1=CC(=C(C=C1)N1C(=O)C2=C(CCCC2)C1=O)F.[N+](=O)(O)[O-]>>ClC1=CC(=C(C=C1[N+](=O)[O-])N1C(=O)C2=C(CCCC2)C1=O)F
[O:1]=[C:2]1[C:3]2=[C:4]([CH2:5][CH2:6][CH2:7][CH2:8]2)[C:9](=[O:10])[N:11]1[c:12]1[cH:13][cH:14][c:18]([Cl:19])[cH:20][c:21]1[F:22].O[N+:15](=[O:16])[O-:17]>>[O:1]=[C:2]1[C:3]2=[C:4]([CH2:5][CH2:6][CH2:7][CH2:8]2)[C:9](=[O:10])[N:11]1[c:12]1[cH:13][c:14]([N+:15](=[O:16])[O-:17])[c:18]([Cl:19])[cH:20][c:21]1[F:22]
O=C1C2=C(CCCC2)C(=O)N1c1ccc(Cl)cc1F.O=[N+]([O-])O
O=C1C2=C(CCCC2)C(=O)N1c1cc([N+](=O)[O-])c(Cl)cc1F
null
null
S(O)(O)(=O)=O
Functional Group Addition
Aromatic nitration with HNO3
53848b8b2bb4e867226e49db2e60519b24be9379900e3ad7c56af54fe8fde7a5
ddce49825c02b8965f10c8d99e3c841d26e1f136da6037b417c09313e6d73097
O=C1C2=C(CCCC2)C(=O)N1c1ccccc1
O-[N+;H0;D3:1](-[O;-;D1;H0:2])=[O;D1;H0:3].[Cl;D1;H0:4]-[c:5](:[c:6]):[cH;D2;+0:7]:[c:8]:[c:9]>>[Cl;D1;H0:4]-[c:5](:[c:6]):[c;H0;D3;+0:7](-[N+;H0;D3:1](-[O;-;D1;H0:2])=[O;D1;H0:3]):[c:8]:[c:9]
101.6
[{"value": 101.6, "product": "ClC1=CC(=C(C=C1[N+](=O)[O-])N1C(=O)C2=C(CCCC2)C1=O)F", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
-3
CELSIUS
90
MINUTE
A mixture of N-(4-chloro-2-fluorophenyl)-1-cyclohexene-1,2-dicarboximide (24.4 g, 86.7 mmol) in sulfuric acid (150 mL) is cooled to -3° C., treated dropwise with nitric acid (70% real, 6.70 mL, 104 mmol) while maintaining the temperature at 0°-2° C., stirred at room temperature for 90 minutes, and poured onto ice. The ...
10.6084/m9.figshare.5104873.v1
null
Nitrate
Nitro group
c1ccccc1
c1ccccc1
C1CCC2=C(C1)C[NH]C2.c1ccccc1
HO-
S(O)(O)(=O)=O
-3
1.5
O=C1C2=C(CCCC2)C(=O)N1c1ccc(Cl)cc1F.O=[N+]([O-])O>S(O)(O)(=O)=O>O=C1C2=C(CCCC2)C(=O)N1c1cc([N+](=O)[O-])c(Cl)cc1F
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-88f06d69204e412d96ef75bebf1aaf76
O=C1C2=C(CCCC2)C(=O)N1c1cc([N+](=O)[O-])c(Cl)cc1F>>Nc1cc(N2C(=O)C3=C(CCCC3)C2=O)c(F)cc1Cl
C(C)(=O)OCC.ClC1=CC(=C(C=C1[N+](=O)[O-])N1C(=O)C2=C(CCCC2)C1=O)F>>NC=1C(=CC(=C(C1)N1C(=O)C2=C(CCCC2)C1=O)F)Cl
O=[N+:1]([O-])[c:2]1[cH:3][c:4]([N:5]2[C:6](=[O:7])[C:8]3=[C:9]([CH2:10][CH2:11][CH2:12][CH2:13]3)[C:14]2=[O:15])[c:16]([F:17])[cH:18][c:19]1[Cl:20]>>[NH2:1][c:2]1[cH:3][c:4]([N:5]2[C:6](=[O:7])[C:8]3=[C:9]([CH2:10][CH2:11][CH2:12][CH2:13]3)[C:14]2=[O:15])[c:16]([F:17])[cH:18][c:19]1[Cl:20]
O=C1C2=C(CCCC2)C(=O)N1c1cc([N+](=O)[O-])c(Cl)cc1F
Nc1cc(N2C(=O)C3=C(CCCC3)C2=O)c(F)cc1Cl
null
[Fe]
C(C)(=O)O
Reduction
Reduction of nitro groups to amines
bbc242b150a51e69d3ad1caaa391f4422710431b398dcb880555f476706790be
7b0317532ea57a4fcedc1efc3e3c22eb5238d1c8330da53d4f9801fc2391f567
O=C1C2=C(CCCC2)C(=O)N1c1ccccc1
O=[N+;H0;D3:1](-[O-])-[c:2](:[c:3]):[c:4]>>[NH2;D1;+0:1]-[c:2](:[c:3]):[c:4]
null
[]
null
null
10
MINUTE
Iron powder (7.30 g, 130.7 mmol) is added portionwise to a mixture of N-(4-chloro-2-fluoro-5-nitrophenyl)-1-cyclohexene-1,2-dicarboximide (10.6 g, 32.7 mmol) in acetic acid (100 mL) at 65° C. After the addition is complete, the reaction mixture is stirred for 10 minutes, and filtered through diatomaceous earth. The fil...
10.6084/m9.figshare.5104873.v1
null
Nitro group
Primary amine
null
null
c1ccccc1.C1CCC2=C(C1)C[NH]C2
Other
[Fe].C(C)(=O)O
null
0.166667
O=C1C2=C(CCCC2)C(=O)N1c1cc([N+](=O)[O-])c(Cl)cc1F>[Fe].C(C)(=O)O>Nc1cc(N2C(=O)C3=C(CCCC3)C2=O)c(F)cc1Cl
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-977e991e320c48a5ae6360a814f9e68c
CC(C)OC(=O)Cn1c(=O)n(C)c(=O)n(-c2cc(N)c(F)cc2Cl)c1=O.O=C1OC(=O)c2c(F)cccc21>>CC(C)OC(=O)Cn1c(=O)n(C)c(=O)n(-c2cc(N3C(=O)c4cccc(F)c4C3=O)c(F)cc2Cl)c1=O
NC=1C(=CC(=C(C1)N1C(N(C(N(C1=O)C)=O)CC(=O)OC(C)C)=O)Cl)F.FC1=C2C(C(=O)OC2=O)=CC=C1>>ClC1=C(C=C(C(=C1)F)N1C(C=2C(C1=O)=C(C=CC2)F)=O)N2C(N(C(N(C2=O)C)=O)CC(=O)OC(C)C)=O
[CH3:1][CH:2]([CH3:3])[O:4][C:5](=[O:6])[CH2:7][n:8]1[c:9](=[O:10])[n:11]([CH3:12])[c:13](=[O:14])[n:15](-[c:16]2[cH:17][c:18]([NH2:19])[c:31]([F:32])[cH:33][c:34]2[Cl:35])[c:36]1=[O:37].O1[C:20](=[O:21])[c:22]2[cH:23][cH:24][cH:25][c:26]([F:27])[c:28]2[C:29]1=[O:30]>>[CH3:1][CH:2]([CH3:3])[O:4][C:5](=[O:6])[CH2:7][n:8...
CC(C)OC(=O)Cn1c(=O)n(C)c(=O)n(-c2cc(N)c(F)cc2Cl)c1=O.O=C1OC(=O)c2c(F)cccc21
CC(C)OC(=O)Cn1c(=O)n(C)c(=O)n(-c2cc(N3C(=O)c4cccc(F)c4C3=O)c(F)cc2Cl)c1=O
null
null
C(C)(=O)O
Acylation
Phthalic anhydride to phthalimide
c3c986d6e09320348d40a4a59ca107882ce771f249842049dc55e55f334c675b
2bbbf7b24648445e31d33a2a26f8618c2067bd23957587cc459f3c45a03ed48a
O=C1c2ccccc2C(=O)N1c1cccc(-n2c(=O)[nH]c(=O)[nH]c2=O)c1
[NH2;D1;+0:1]-[c:2](:[c:3]):[c:4].[O;D1;H0:5]=[C;H0;D3;+0:6]1-O-[C;H0;D3;+0:7](=[O;D1;H0:8])-[c:9](:[c:10]):[c:11]-1:[c:12]>>[O;D1;H0:5]=[C;H0;D3;+0:6]1-[N;H0;D3;+0:1](-[c:2](:[c:3]):[c:4])-[C;H0;D3;+0:7](=[O;D1;H0:8])-[c:9](:[c:10]):[c:11]-1:[c:12]
null
[]
null
null
null
null
A solution of isopropyl 3-(5-amino-2-chloro-4-fluorophenyl)tetrahydro-5-methyl-2,4,6-trioxo-s-triazine-1(2H)-acetate (1.0 g, 2.6 mmol) and 3-fluorophthalic anhydride (0.51 g, 3.1 mmol) in acetic acid is refluxed for 6 hours, stirred at room temperature for several days and poured onto ice. The resultant aqueous mixture...
10.6084/m9.figshare.5104873.v1
null
Anhydride.Ester.Ester.Primary amine
Substituted dicarboximide
c1ccc2c(c1)COC2
c1ccc2c(c1)C[NH]C2
c1ncncn1.c1ccccc1.c1ccc2c(c1)C[NH]C2
HO-
C(C)(=O)O
null
null
CC(C)OC(=O)Cn1c(=O)n(C)c(=O)n(-c2cc(N)c(F)cc2Cl)c1=O.O=C1OC(=O)c2c(F)cccc21>C(C)(=O)O>CC(C)OC(=O)Cn1c(=O)n(C)c(=O)n(-c2cc(N3C(=O)c4cccc(F)c4C3=O)c(F)cc2Cl)c1=O
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-7a8f9c1c64f84e7eae13346d27dfc137
CC(C)OC(=O)CBr.CC(C)OC(=O)Cn1c(=O)[nH]c(=O)n(-c2cc(N=c3sc(=O)n4n3CCCC4)c(F)cc2Cl)c1=O>>CC(C)OC(=O)Cn1c(=O)n(CC(=O)OC(C)C)c(=O)n(-c2cc(N=c3sc(=O)n4n3CCCC4)c(F)cc2Cl)c1=O
ClC1=C(C=C(C(=C1)F)N=C1SC(N2N1CCCC2)=O)N2C(N(C(NC2=O)=O)CC(=O)OC(C)C)=O.C([O-])([O-])=O.[K+].[K+].BrCC(=O)OC(C)C.O>>ClC1=C(C=C(C(=C1)F)N=C1SC(N2N1CCCC2)=O)N2C(N(C(N(C2=O)CC(=O)OC(C)C)=O)CC(=O)OC(C)C)=O
Br[CH2:12][C:13](=[O:14])[O:15][CH:16]([CH3:17])[CH3:18].[CH3:1][CH:2]([CH3:3])[O:4][C:5](=[O:6])[CH2:7][n:8]1[c:9](=[O:10])[nH:11][c:19](=[O:20])[n:21](-[c:22]2[cH:23][c:24]([N:25]=[c:26]3[s:27][c:28](=[O:29])[n:30]4[n:31]3[CH2:32][CH2:33][CH2:34][CH2:35]4)[c:36]([F:37])[cH:38][c:39]2[Cl:40])[c:41]1=[O:42]>>[CH3:1][CH...
CC(C)OC(=O)CBr.CC(C)OC(=O)Cn1c(=O)[nH]c(=O)n(-c2cc(N=c3sc(=O)n4n3CCCC4)c(F)cc2Cl)c1=O
CC(C)OC(=O)Cn1c(=O)n(CC(=O)OC(C)C)c(=O)n(-c2cc(N=c3sc(=O)n4n3CCCC4)c(F)cc2Cl)c1=O
null
null
CN(C=O)C
Heteroatom Alkylation and Arylation
N-alkylation of secondary amines with alkyl halides
42369dcf6c82c4deef5c2c853244075c2d58469f08013f2ed6a1b03bbe51bb5a
6007d70cc3173f3039a472489995dad2781e8d749be1f1aa209b0bf2f190a4b4
O=c1[nH]c(=O)n(-c2cccc(N=c3sc(=O)n4n3CCCC4)c2)c(=O)[nH]1
Br-[CH2;D2;+0:1]-[C:2](=[O;D1;H0:3])-[#8:4]-[C:5].[#8:6]-[C:7](=[O;D1;H0:8])-[C:9]-[#7;a:10]1:[c:11]:[#7;a:12](-[c:13]):[c:14](=[O;D1;H0:15]):[nH;D2;+0:16]:[c:17]:1=[O;D1;H0:18]>>[#8:6]-[C:7](=[O;D1;H0:8])-[C:9]-[#7;a:10]1:[c:11]:[#7;a:12](-[c:13]):[c:14](=[O;D1;H0:15]):[n;H0;D3;+0:16](-[CH2;D2;+0:1]-[C:2](=[O;D1;H0:3]...
29.5
[{"value": 29.5, "product": "ClC1=C(C=C(C(=C1)F)N=C1SC(N2N1CCCC2)=O)N2C(N(C(N(C2=O)CC(=O)OC(C)C)=O)CC(=O)OC(C)C)=O", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
8
HOUR
A mixture of isopropyl 3-{2-chloro-4-fluoro-5-[(tetrahydro-3-oxo-1H,3H-[1,3,4]thiadiazolo[3,4-a]-pyridazin-1-ylidene)amino]phenyl}tetrahydro-2,4,6-trioxo-s-triazine-1(2H)-acetate (0.85 g, 1.62 mmol), potassium carbonate (0.27 g, 1.95 mmol) and isopropyl bromoacetate (0,353 g, 1.95 mmol)in N,N-dimethylformamide is stirr...
10.6084/m9.figshare.5104873.v1
null
Primary halide.Ester
Ester
c1ncncn1
c1ncncn1
c1ncncn1.c1ccccc1.c1scn2n1CCCC2
HBr
CN(C=O)C
null
8
CC(C)OC(=O)CBr.CC(C)OC(=O)Cn1c(=O)[nH]c(=O)n(-c2cc(N=c3sc(=O)n4n3CCCC4)c(F)cc2Cl)c1=O>CN(C=O)C>CC(C)OC(=O)Cn1c(=O)n(CC(=O)OC(C)C)c(=O)n(-c2cc(N=c3sc(=O)n4n3CCCC4)c(F)cc2Cl)c1=O
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-a7e627b3bd4d476c9aa919241c2544ff
C=CCBr.Cn1c(=O)[nH]c(=O)n(-c2cc(N=c3sc(=O)n4n3CCCC4)c(F)cc2Cl)c1=O>>C=CCn1c(=O)n(C)c(=O)n(-c2cc(N=c3sc(=O)n4n3CCCC4)c(F)cc2Cl)c1=O
O.ClC1=C(C=C(C(=C1)F)N=C1SC(N2N1CCCC2)=O)N2C(N(C(NC2=O)=O)C)=O.C([O-])([O-])=O.[K+].[K+].C(C=C)Br>>C(C=C)N1C(N(C(N(C1=O)C)=O)C1=C(C=C(C(=C1)N=C1SC(N2N1CCCC2)=O)F)Cl)=O
Br[CH2:3][CH:2]=[CH2:1].[nH:4]1[c:5](=[O:6])[n:7]([CH3:8])[c:9](=[O:10])[n:11](-[c:12]2[cH:13][c:14]([N:15]=[c:16]3[s:17][c:18](=[O:19])[n:20]4[n:21]3[CH2:22][CH2:23][CH2:24][CH2:25]4)[c:26]([F:27])[cH:28][c:29]2[Cl:30])[c:31]1=[O:32]>>[CH2:1]=[CH:2][CH2:3][n:4]1[c:5](=[O:6])[n:7]([CH3:8])[c:9](=[O:10])[n:11](-[c:12]2[...
C=CCBr.Cn1c(=O)[nH]c(=O)n(-c2cc(N=c3sc(=O)n4n3CCCC4)c(F)cc2Cl)c1=O
C=CCn1c(=O)n(C)c(=O)n(-c2cc(N=c3sc(=O)n4n3CCCC4)c(F)cc2Cl)c1=O
null
null
CC(=O)C
Heteroatom Alkylation and Arylation
N-alkylation of secondary amines with alkyl halides
84dcf5908feaa31afcb5f12444b3389dbab6d839a84b75317076d533f4c11c42
4c606dc54eac846ef90c7b3255999ceff93277747e7c2b0ddd37ccf25562b7c5
O=c1[nH]c(=O)n(-c2cccc(N=c3sc(=O)n4n3CCCC4)c2)c(=O)[nH]1
Br-[CH2;D2;+0:1]-[C:2]=[C;D1;H2:3].[C;D1;H3:4]-[#7;a:5]1:[c:6]:[#7;a:7](-[c:8]):[c:9](=[O;D1;H0:10]):[nH;D2;+0:11]:[c:12]:1=[O;D1;H0:13]>>[C;D1;H2:3]=[C:2]-[CH2;D2;+0:1]-[n;H0;D3;+0:11]1:[c:9](=[O;D1;H0:10]):[#7;a:7](-[c:8]):[c:6]:[#7;a:5](-[C;D1;H3:4]):[c:12]:1=[O;D1;H0:13]
73.3
[{"value": 73.3, "product": "C(C=C)N1C(N(C(N(C1=O)C)=O)C1=C(C=C(C(=C1)N=C1SC(N2N1CCCC2)=O)F)Cl)=O", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
40
CELSIUS
8
HOUR
A mixture of 1-{2-chloro-4-fluoro-5-[(tetrahydro-3-oxo-1H,3H-[1,3,4]thiadiazolo[3,4-a]pyridazin-1-ylidene)-amino]phenyl}-3-methyl-s-triazine-2,4,6(1H,3H,5H)-trione (1.00 g, 2.27 mmol), potassium carbonate (0.627 g, 4.54 mmol) and allyl bromide (0.329 g, 2.72 mmol) in acetone is stirred overnight at 40° C. and poured in...
10.6084/m9.figshare.5104873.v1
null
Primary halide.Allyl
Allyl
c1ncncn1
c1ncncn1
c1ncncn1.c1ccccc1.c1scn2n1CCCC2
HBr
CC(=O)C
40
8
C=CCBr.Cn1c(=O)[nH]c(=O)n(-c2cc(N=c3sc(=O)n4n3CCCC4)c(F)cc2Cl)c1=O>CC(=O)C>C=CCn1c(=O)n(C)c(=O)n(-c2cc(N=c3sc(=O)n4n3CCCC4)c(F)cc2Cl)c1=O
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-cd96027b0a0d43cfb4c23e75a82d466d
NN.O=C(O)CCC(=O)c1ccc(Cl)cc1>>O=C1CCC(c2ccc(Cl)cc2)=NN1
ClC1=CC=C(C(=O)CCC(=O)O)C=C1.O.NN>>ClC1=CC=C(C=C1)C=1CCC(NN1)=O
[NH2:13][NH2:14].O=[C:5]([CH2:4][CH2:3][C:2](O)=[O:1])[c:6]1[cH:7][cH:8][c:9]([Cl:10])[cH:11][cH:12]1>>[O:1]=[C:2]1[CH2:3][CH2:4][C:5]([c:6]2[cH:7][cH:8][c:9]([Cl:10])[cH:11][cH:12]2)=[N:13][NH:14]1
NN.O=C(O)CCC(=O)c1ccc(Cl)cc1
O=C1CCC(c2ccc(Cl)cc2)=NN1
null
null
C(C)O
Acylation
OtherReaction
16e715242dd5e92f711d46176c552652cef6c6f4fed9bc9a09a311d5b0b86cea
30de68c4dde17a0553a43eee47b1b865b8390bb08557512a59e6e71e0ed0ad51
O=C1CCC(c2ccccc2)=NN1
O-[C;H0;D3;+0:1](=[O;D1;H0:2])-[C:3]-[C:4]-[C;H0;D3;+0:5](=O)-[c:6](:[c:7]):[c:8].[NH2;D1;+0:9]-[NH2;D1;+0:10]>>[O;D1;H0:2]=[C;H0;D3;+0:1]1-[C:3]-[C:4]-[C;H0;D3;+0:5](-[c:6](:[c:7]):[c:8])=[N;H0;D2;+0:9]-[NH;D2;+0:10]-1
80
[{"value": 80.0, "product": "ClC1=CC=C(C=C1)C=1CCC(NN1)=O", "details": "PERCENTYIELD", "is_desired": false}]
null
null
null
null
To a solution of 3-(4-chlorobenzoyl)propionic acid (20g) in absolute ethanol (200 ml) was added 5 g of hydrazine monohydrate. A thick solid was formed which dissolved after heating. The resulting solution was refluxed for 3 h, cooled and the solid formed filtered and dried to yield 16 g (80%) of 6-(4-chlorophenyl)-4,5-...
10.6084/m9.figshare.5104873.v1
null
Hydrazine.Carboxylic acid.Ketone
Hydrazone amide
null
C1=NNCCC1
C1=NNCCC1.c1ccccc1
HO-
C(C)O
null
null
NN.O=C(O)CCC(=O)c1ccc(Cl)cc1>C(C)O>O=C1CCC(c2ccc(Cl)cc2)=NN1
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-42bdc25833dc410b993a2671ac65a643
CC(C(=O)O)C(=O)c1ccc(Cl)cc1.CC(C)(C)NN>>CC(C)(C)N1N=C(c2ccc(Cl)cc2)CCC1=O
ClC1=CC=C(C(=O)C(C(=O)O)C)C=C1.C(C)(=O)[O-].[Na+].Cl.C(C)(C)(C)NN>>ClC1=CC=C(C=C1)C=1CCC(N(N1)C(C)(C)C)=O
O=[C:7]([c:8]1[cH:9][cH:10][c:11]([Cl:12])[cH:13][cH:14]1)[CH:15]([CH3:16])[C:17](O)=[O:18].[CH3:1][C:2]([CH3:3])([CH3:4])[NH:5][NH2:6]>>[CH3:1][C:2]([CH3:3])([CH3:4])[N:5]1[N:6]=[C:7]([c:8]2[cH:9][cH:10][c:11]([Cl:12])[cH:13][cH:14]2)[CH2:15][CH2:16][C:17]1=[O:18]
CC(C(=O)O)C(=O)c1ccc(Cl)cc1.CC(C)(C)NN
CC(C)(C)N1N=C(c2ccc(Cl)cc2)CCC1=O
null
null
C(CCC)O
Acylation
OtherReaction
4e477d09c29dc9649665c2a512a7ab66ed0db9837b745e511eba3c76a3cc18d7
30de68c4dde17a0553a43eee47b1b865b8390bb08557512a59e6e71e0ed0ad51
O=C1CCC(c2ccccc2)=NN1
O-[C;H0;D3;+0:1](=[O;D1;H0:2])-[CH;D3;+0:3](-[CH3;D1;+0:4])-[C;H0;D3;+0:5](=O)-[c:6](:[c:7]):[c:8].[C;D1;H3:9]-[C:10](-[C;D1;H3:11])(-[C;D1;H3:12])-[NH;D2;+0:13]-[NH2;D1;+0:14]>>[C;D1;H3:9]-[C:10](-[C;D1;H3:11])(-[C;D1;H3:12])-[N;H0;D3;+0:13]1-[N;H0;D2;+0:14]=[C;H0;D3;+0:5](-[c:6](:[c:7]):[c:8])-[CH2;D2;+0:3]-[CH2;D2;+...
34.4
[{"value": 34.4, "product": "ClC1=CC=C(C=C1)C=1CCC(N(N1)C(C)(C)C)=O", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
null
null
To a solution of 4-chlorobenzoylpropionic acid (4.24 g) in n-butanol (150 ml) was added anhydrous sodium acetate (1.54 g) and t-butylhydrazine hydrochloride (2.75 g) portionwise at room temperature. The resulting mixture was refluxed for 9 hours distilling off 65 ml of n-butanol during that time. The resulting mixture ...
10.6084/m9.figshare.5104873.v1
null
Hydrazine.Carboxylic acid.Ketone
Hydrazone amide
null
C1=N[NH]CCC1
C1=N[NH]CCC1.c1ccccc1
HO-
C(CCC)O
null
null
CC(C(=O)O)C(=O)c1ccc(Cl)cc1.CC(C)(C)NN>C(CCC)O>CC(C)(C)N1N=C(c2ccc(Cl)cc2)CCC1=O
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-ce064075330c45f48a8cd178fcf95efd
COC(=O)CCC(=O)OC.COC(=O)c1cccc(Cl)c1>>O=C(O)CCC(=O)c1cccc(Cl)c1
C(CCC(=O)OC)(=O)OC.[Na].C(C)O.ClC=1C=C(C(=O)OC)C=CC1.C(CCC(=O)OC)(=O)OC>>ClC=1C=C(C(=O)CCC(=O)O)C=CC1
COC(=O)[CH2:5][CH2:4][C:2](=[O:1])[O:3]C.CO[C:6](=[O:7])[c:8]1[cH:9][cH:10][cH:11][c:12]([Cl:13])[cH:14]1>>[O:1]=[C:2]([OH:3])[CH2:4][CH2:5][C:6](=[O:7])[c:8]1[cH:9][cH:10][cH:11][c:12]([Cl:13])[cH:14]1
COC(=O)CCC(=O)OC.COC(=O)c1cccc(Cl)c1
O=C(O)CCC(=O)c1cccc(Cl)c1
null
null
CCOCC
C-C Coupling
OtherReaction
6d482de2a0c1fffe47581cf2d6dc0eefca79628574252eec326be9292f335afe
1f69704fe402a3eb0e91a243a59f68f972592be61b4c787368515903d4c85726
c1ccccc1
C-O-C(=O)-[CH2;D2;+0:1]-[C:2]-[C:3](=[O;D1;H0:4])-[O;H0;D2;+0:5]-C.C-O-[C;H0;D3;+0:6](=[O;D1;H0:7])-[c:8](:[c:9]):[c:10]>>[O;D1;H0:4]=[C:3](-[OH;D1;+0:5])-[C:2]-[CH2;D2;+0:1]-[C;H0;D3;+0:6](=[O;D1;H0:7])-[c:8](:[c:9]):[c:10]
null
[]
null
null
null
null
Sodium (11 g, spheres) was added to 200 ml ethanol with stirring. When the gas evolution ceased, methyl 3-chlorobenzoate (10 g, 0.057 mole) and dimethyl succinate (9.0 g, 0.615 mole) were added rapidly and the mixture was stirred for 5 minutes at room temperature. The mixture was slowly concentrated on a rotary evapora...
10.6084/m9.figshare.5104873.v1
null
Ester.Ester.Ester
Carboxylic acid.Ketone
null
null
c1ccccc1
HO-
CCOCC
null
null
COC(=O)CCC(=O)OC.COC(=O)c1cccc(Cl)c1>CCOCC>O=C(O)CCC(=O)c1cccc(Cl)c1
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-853ac2ea43e24e448317811edbddc04c
CC(C(=O)O)C(=O)c1ccc(Cl)cc1.O=[N+]([O-])O>>CC(C(=O)O)C(=O)c1ccc(Cl)c([N+](=O)[O-])c1
ClC1=CC=C(C(=O)C(C(=O)O)C)C=C1.[N+](=O)(O)[O-]>>ClC1=C(C=C(C(=O)C(C(=O)O)C)C=C1)[N+](=O)[O-]
[CH3:1][CH:2]([C:3](=[O:4])[OH:5])[C:6](=[O:7])[c:8]1[cH:9][cH:10][c:11]([Cl:12])[cH:13][cH:17]1.O[N+:14](=[O:15])[O-:16]>>[CH3:1][CH:2]([C:3](=[O:4])[OH:5])[C:6](=[O:7])[c:8]1[cH:9][cH:10][c:11]([Cl:12])[c:13]([N+:14](=[O:15])[O-:16])[cH:17]1
CC(C(=O)O)C(=O)c1ccc(Cl)cc1.O=[N+]([O-])O
CC(C(=O)O)C(=O)c1ccc(Cl)c([N+](=O)[O-])c1
null
null
null
Functional Group Addition
Aromatic nitration with HNO3
53848b8b2bb4e867226e49db2e60519b24be9379900e3ad7c56af54fe8fde7a5
ddce49825c02b8965f10c8d99e3c841d26e1f136da6037b417c09313e6d73097
c1ccccc1
O-[N+;H0;D3:1](-[O;-;D1;H0:2])=[O;D1;H0:3].[Cl;D1;H0:4]-[c:5](:[c:6]):[cH;D2;+0:7]:[c:8]:[c:9]-[C:10]=[O;D1;H0:11]>>[Cl;D1;H0:4]-[c:5](:[c:6]):[c;H0;D3;+0:7](-[N+;H0;D3:1](-[O;-;D1;H0:2])=[O;D1;H0:3]):[c:8]:[c:9]-[C:10]=[O;D1;H0:11]
null
[]
0
CELSIUS
30
MINUTE
To fuming nitric acid (150 ml) was added p-chlorobenzoylpropionic acid (20.0 g), slowly portionwise at 0° C. After the addition was completed the resulting mixture was stirred at 0° C. for 30 minutes and the resulting white solid was suction filtered and washed with water until the pH of the washing liquids was neutral...
10.6084/m9.figshare.5104873.v1
null
Nitrate
Nitro group
c1ccccc1
c1ccccc1
c1ccccc1
HO-
null
0
0.5
CC(C(=O)O)C(=O)c1ccc(Cl)cc1.O=[N+]([O-])O>>CC(C(=O)O)C(=O)c1ccc(Cl)c([N+](=O)[O-])c1
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-df91626c72824b1cb4c0c7f9c249511e
Cc1ccc(C(=O)CCC(=O)O)cc1.ClCl>>Cc1c(Cl)cc(C(=O)CCC(=O)O)cc1Cl
CC1=CC=C(C(=O)CCC(=O)O)C=C1.[Cl-].[Al+3].[Cl-].[Cl-].ClCl>>ClC=1C=C(C(=O)CCC(=O)O)C=C(C1C)Cl
[CH3:1][c:2]1[cH:3][cH:5][c:6]([C:7](=[O:8])[CH2:9][CH2:10][C:11](=[O:12])[OH:13])[cH:14][cH:15]1.[Cl:4][Cl:16]>>[CH3:1][c:2]1[c:3]([Cl:4])[cH:5][c:6]([C:7](=[O:8])[CH2:9][CH2:10][C:11](=[O:12])[OH:13])[cH:14][c:15]1[Cl:16]
Cc1ccc(C(=O)CCC(=O)O)cc1.ClCl
Cc1c(Cl)cc(C(=O)CCC(=O)O)cc1Cl
null
null
C(Cl)Cl
Miscellaneous
OtherReaction
d2a751fe92dcfde720edd5e4971c1aa6cc149bff4a6d230cc6b5cac59ec9498c
861258def4b3bd7367f8a87cde43fe585d40dc3669ea29055dbcb9a2de101a4d
c1ccccc1
[C;D1;H3:1]-[c:2]1:[cH;D2;+0:3]:[c:4]:[c:5](-[C:6]=[O;D1;H0:7]):[c:8]:[cH;D2;+0:9]:1.[Cl;H0;D1;+0:10]-[Cl;H0;D1;+0:11]>>[C;D1;H3:1]-[c:2]1:[c;H0;D3;+0:3](-[Cl;H0;D1;+0:10]):[c:4]:[c:5](-[C:6]=[O;D1;H0:7]):[c:8]:[c;H0;D3;+0:9]:1-[Cl;H0;D1;+0:11]
44.2
[{"value": 44.2, "product": "ClC=1C=C(C(=O)CCC(=O)O)C=C(C1C)Cl", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
null
null
To a mixture of 3-(4-methylbenzoyl)propionic acid (7.5 g) and methylene chloride (250 ml) was added slowly portionwise aluminum chloride (15 g) at 0° C. After the addition was completed chlorine gas was bubbled in slowly at 0° C. After 6 hours the reaction mixture was poured into mixture of hydrochloric acid and ice an...
10.6084/m9.figshare.5104873.v1
null
null
Aromatic halide.Aromatic halide
c1ccccc1
c1ccccc1
c1ccccc1
null
C(Cl)Cl
null
null
Cc1ccc(C(=O)CCC(=O)O)cc1.ClCl>C(Cl)Cl>Cc1c(Cl)cc(C(=O)CCC(=O)O)cc1Cl
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-65c75dc89f17409bb6ee8bc64675c761
C1=COCCC1.OCC#CCO>>OCC#CCOC1CCCCO1
C(C#CCO)O.O1CCCC=C1>>O1C(CCCC1)OCC#CCO
[CH:7]1=[CH:8][CH2:9][CH2:10][CH2:11][O:12]1.[OH:1][CH2:2][C:3]#[C:4][CH2:5][OH:6]>>[OH:1][CH2:2][C:3]#[C:4][CH2:5][O:6][CH:7]1[CH2:8][CH2:9][CH2:10][CH2:11][O:12]1
C1=COCCC1.OCC#CCO
OCC#CCOC1CCCCO1
null
null
CCOCC
Heteroatom Alkylation and Arylation
oxa-Michael addition
abdcab389770d0a73be3b825aa1d56cee234da38dbdf3510fe8104d481e7cf3f
c6a3efa2acb508a32cdf9fcedfcd9635cce0ecdcf12c094b743aa576ea01fd9a
C1CCOCC1
[#8:1]1-[C:2]-[C:3]-[C:4]-[CH;D2;+0:5]=[CH;D2;+0:6]-1.[C:7]-[C:8]#[C:9]-[C:10]-[OH;D1;+0:11]>>[C:7]-[C:8]#[C:9]-[C:10]-[O;H0;D2;+0:11]-[CH;D3;+0:6]1-[#8:1]-[C:2]-[C:3]-[C:4]-[CH2;D2;+0:5]-1
68.8
[{"value": 68.8, "product": "O1C(CCCC1)OCC#CCO", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
null
null
To a mixture of 5.0 g of 2-butyne-1,4-diol and 10 milligrams of p-toluenesulfonic add and 150 ml of dry ether there was added dropwise with stirring at room temperature 4.9 g of 3,4-dihydro-2H-pyran. After stirring overnight at ambient temperature the ether was evaporated and the residue was poured into 200 ml of water...
10.6084/m9.figshare.5104873.v1
null
Ether.Primary alcohol
Ether.Ether
C1=COCCC1
C1CCOCC1
C1CCOCC1
null
CCOCC
null
null
C1=COCCC1.OCC#CCO>CCOCC>OCC#CCOC1CCCCO1
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-1df241b7ff954c60ae215c613fabf759
C#CC1CCCCC1.C=O>>OCC#CC1CCCCC1
C1(CCCCC1)C#C.C=O.C=O>>C1(CCCCC1)C#CCO
[CH:3]#[C:4][CH:5]1[CH2:6][CH2:7][CH2:8][CH2:9][CH2:10]1.[O:1]=[CH2:2]>>[OH:1][CH2:2][C:3]#[C:4][CH:5]1[CH2:6][CH2:7][CH2:8][CH2:9][CH2:10]1
C#CC1CCCCC1.C=O
OCC#CC1CCCCC1
null
null
CCOCC
C-C Coupling
OtherReaction
b068d8bba9f864ba971dd324292d9b3526f0235b4ab7e3a9ce6aa76a39c4a1e7
22ebec2cc94dd24863aea8793d450cfe0691e1036be204d1a4c79c16effe90a4
C1CCCCC1
[CH2;D1;+0:1]=[O;H0;D1;+0:2].[C:3]-[C:4]#[CH;D1;+0:5]>>[C:3]-[C:4]#[C;H0;D2;+0:5]-[CH2;D2;+0:1]-[OH;D1;+0:2]
null
[]
null
null
null
null
To a solution of ethyl magesium bromide (prepared from 2.5 g of magnesium turning and 11.3 g of bromoethane) in ether was added dropwise a solution of 10.2 g of cyclohexylacetylene in ether and the reaction mixture was refluxed for 2 hours. The reaction mixture was cooled to ambient temperature and anhydrous formaldehy...
10.6084/m9.figshare.5104873.v1
null
Formaldehyde.Alkyne
Primary alcohol.Alkyne
null
null
C1CCCCC1
null
CCOCC
null
null
C#CC1CCCCC1.C=O>CCOCC>OCC#CC1CCCCC1
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-3ad3598473f04955b043e8d47bb746e6
O=C1CCC(c2ccc(Cl)cc2)=NN1>>O=c1ccc(-c2ccc(Cl)cc2)n[nH]1
ClC1=CC=C(C=C1)C=1CCC(NN1)=O.C(C)(=O)O.BrBr>>ClC1=CC=C(C=C1)C=1C=CC(NN1)=O
[O:1]=[C:2]1[CH2:3][CH2:4][C:5]([c:6]2[cH:7][cH:8][c:9]([Cl:10])[cH:11][cH:12]2)=[N:13][NH:14]1>>[O:1]=[c:2]1[cH:3][cH:4][c:5](-[c:6]2[cH:7][cH:8][c:9]([Cl:10])[cH:11][cH:12]2)[n:13][nH:14]1
O=C1CCC(c2ccc(Cl)cc2)=NN1
O=c1ccc(-c2ccc(Cl)cc2)n[nH]1
null
null
O
Aromatic Heterocycle Formation
OtherReaction
73c80fbcc9dd7a9125aaf1059d9d4eab31b342d21fc860abf5e65fd78456864b
78b0616e5760c6d4dadfc1fac5c58c0254d0dc7b1bf102fea4bc1349928b0776
O=c1ccc(-c2ccccc2)n[nH]1
[O;D1;H0:1]=[C;H0;D3;+0:2]1-[CH2;D2;+0:3]-[CH2;D2;+0:4]-[C;H0;D3;+0:5](-[c;H0;D3;+0:6](:[c:7]:[c:8]):[c:9]:[c:10])=[N;H0;D2;+0:11]-[NH;D2;+0:12]-1>>[O;D1;H0:1]=[c;H0;D3;+0:2]1:[cH;D2;+0:3]:[cH;D2;+0:4]:[c;H0;D3;+0:5](-[c;H0;D3;+0:6](:[c:7]:[c:8]):[c:9]:[c:10]):[n;H0;D2;+0:11]:[nH;D2;+0:12]:1
93.1
[{"value": 89.0, "product": "ClC1=CC=C(C=C1)C=1C=CC(NN1)=O", "details": "PERCENTYIELD", "is_desired": false}, {"value": 93.1, "product": "ClC1=CC=C(C=C1)C=1C=CC(NN1)=O", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
null
null
To a solution of 6-(4-chlorophenyl)-4,5-dihydropyridazinone (11.75 g) and glacial acetic acid (100 ml) was added dropwise 3 ml of bromine and the mixture was heated at 60°-70° C. for 3 h. The resulting mixture was cooled and slowly poured into 400 ml of cold water. The resulting white solid was filtered and dried to yi...
10.6084/m9.figshare.5104873.v1
null
Hydrazone amide
null
C1=NNCCC1
c1cccnn1
c1cccnn1.c1ccccc1
null
O
null
null
O=C1CCC(c2ccc(Cl)cc2)=NN1>O>O=c1ccc(-c2ccc(Cl)cc2)n[nH]1
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-72814c0515e843deab3f2d0998e62084
FC1(F)CC(Cl)(Cl)C1(F)Cl>>FC1(F)C=C(Cl)C1(F)Cl
ClC1(C(C(C1)(F)F)(F)Cl)Cl.O.Cl>>ClC1(C(C=C1Cl)(F)F)F
Cl[C:5]1([Cl:6])[CH2:4][C:2]([F:1])([F:3])[C:7]1([F:8])[Cl:9]>>[F:1][C:2]1([F:3])[CH:4]=[C:5]([Cl:6])[C:7]1([F:8])[Cl:9]
FC1(F)CC(Cl)(Cl)C1(F)Cl
FC1(F)C=C(Cl)C1(F)Cl
null
null
CCOCC.C(C)N(CC)CC
Functional Group Interconversion
OtherReaction
0ca523bc88d44f4371960ac2ff9ed0bbb8882337b7061f7fba5b4787f1e02481
986b135105e7920109b424799136a4a8281fb4a0f49253ce1bf5d4426ed78637
C1=CCC1
Cl-[C;H0;D4;+0:1]1(-[Cl;D1;H0:2])-[CH2;D2;+0:3]-[C:4](-[F;D1;H0:5])(-[F;D1;H0:6])-[C:7]-1(-[Cl;D1;H0:8])-[F;D1;H0:9]>>[Cl;D1;H0:2]-[C;H0;D3;+0:1]1=[CH;D2;+0:3]-[C:4](-[F;D1;H0:5])(-[F;D1;H0:6])-[C:7]-1(-[Cl;D1;H0:8])-[F;D1;H0:9]
79
[{"value": 79.0, "product": "ClC1(C(C=C1Cl)(F)F)F", "details": "PERCENTYIELD", "is_desired": false}, {"value": 78.2, "product": "ClC1(C(C=C1Cl)(F)F)F", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
8
HOUR
To a solution of 1,1,2 trichloro-2,3,3-trifluorocyclobutane (55.5 g) in 100 ml of anhydrous ether, triethylamine (40 ml) was added dropwise over 30 min at room temperature, and the mixture was stirred overnight at ambient temperature. The mixture was then stirred with 120 ml H2O and 7.5 ml of concentrated HCl. The ethe...
10.6084/m9.figshare.5104873.v1
null
Tertiary halide.Tertiary halide
Alkenyl halide
C1CCC1
C1=CCC1
C1=CCC1
HCl
CCOCC.C(C)N(CC)CC
null
8
FC1(F)CC(Cl)(Cl)C1(F)Cl>CCOCC.C(C)N(CC)CC>FC1(F)C=C(Cl)C1(F)Cl
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-6b35315acbe8476c894bb158bdaa472f
O=C(O)C(F)(F)C(F)(Cl)C(=O)O>>O=C(O)C(F)C(F)(F)C(=O)O
ClC(C(C(=O)O)(F)F)(C(=O)O)F>>FC(C(=O)O)(C(C(=O)O)F)F
Cl[C:6]([C:4]([C:2](=[O:1])[OH:3])([F:5])[F:7])([F:8])[C:9](=[O:10])[OH:11]>>[O:1]=[C:2]([OH:3])[CH:4]([F:5])[C:6]([F:7])([F:8])[C:9](=[O:10])[OH:11]
O=C(O)C(F)(F)C(F)(Cl)C(=O)O
O=C(O)C(F)C(F)(F)C(=O)O
null
[Zn]
O1CCOCC1
Functional Group Addition
Dehalogenation
7f145230bfb0115349e969b2f2fa1359cfafe8c166e52b50a867192005e1f5bc
d6722b0df465660a9eeeaca5a8f5b3dbb2d1ebccb44917f2eca97a85bf850d06
null
Cl-[C;H0;D4;+0:1](-[F;D1;H0:2])(-[C:3](=[O;D1;H0:4])-[O;D1;H1:5])-[C;H0;D4;+0:6](-[F;D1;H0:7])(-[F;H0;D1;+0:8])-[C:9](=[O;D1;H0:10])-[O;D1;H1:11]>>[F;D1;H0:7]-[CH;D3;+0:6](-[C:9](=[O;D1;H0:10])-[O;D1;H1:11])-[C;H0;D4;+0:1](-[F;D1;H0:2])(-[F;H0;D1;+0:8])-[C:3](=[O;D1;H0:4])-[O;D1;H1:5]
40.7
[{"value": 32.0, "product": "FC(C(=O)O)(C(C(=O)O)F)F", "details": "PERCENTYIELD", "is_desired": false}, {"value": 40.7, "product": "FC(C(=O)O)(C(C(=O)O)F)F", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
10
HOUR
To a stirring solution of the chlorotrifluorosuccinic acid (part b) (24.5 g) in 200 ml dioxane was added portionwise zinc metal (85 g) and the mixture was stirred at ambient temperature for 10 hours to yield a viscous liquid which was decanted from the unreacted zinc. Most of the dioxane was evaporated in vacuo. The re...
10.6084/m9.figshare.5104873.v1
null
Tertiary halide.Tertiary halide.Tertiary halide.Tertiary halide
Tertiary halide.Tertiary halide.Secondary halide
null
null
null
Other
[Zn].O1CCOCC1
null
10
O=C(O)C(F)(F)C(F)(Cl)C(=O)O>[Zn].O1CCOCC1>O=C(O)C(F)C(F)(F)C(=O)O
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-d1ffe8aa63584752873a03df8fe427f6
O=C1CCC(=O)O1.c1ccc2ccccc2c1>>O=C(O)CCC(=O)c1cccc2ccccc12
Cl.[Cl-].[Cl-].[Cl-].[Al+3].C1=CC=CC2=CC=CC=C12.C1(CCC(=O)O1)=O>>C1(=CC=CC2=CC=CC=C12)C(=O)CCC(=O)O
[O:1]=[C:2]1[O:3][C:6](=[O:7])[CH2:5][CH2:4]1.[cH:8]1[cH:9][cH:10][cH:11][c:12]2[cH:13][cH:14][cH:15][cH:16][c:17]12>>[O:1]=[C:2]([OH:3])[CH2:4][CH2:5][C:6](=[O:7])[c:8]1[cH:9][cH:10][cH:11][c:12]2[cH:13][cH:14][cH:15][cH:16][c:17]12
O=C1CCC(=O)O1.c1ccc2ccccc2c1
O=C(O)CCC(=O)c1cccc2ccccc12
null
null
[N+](=O)([O-])C1=CC=CC=C1
C-C Coupling
OtherReaction
d1b47ca78c3ceb45955ddf79d2b2d22c1a0978cf9fa8ded4c5ee0a8331deac4e
4836357c99dfeeac9d5083fedc379181a858ae45ac77bd85eb46e7e1a9df36f0
c1ccc2ccccc2c1
[O;D1;H0:1]=[C:2]1-[C:3]-[C:4]-[C;H0;D3;+0:5](=[O;D1;H0:6])-[O;H0;D2;+0:7]-1.[c:8]:[c:9]:[cH;D2;+0:10]:[c:11](:[c:12]):[c:13]>>[O;D1;H0:1]=[C:2](-[OH;D1;+0:7])-[C:3]-[C:4]-[C;H0;D3;+0:5](=[O;D1;H0:6])-[c;H0;D3;+0:10](:[c:9]:[c:8]):[c:11](:[c:12]):[c:13]
null
[]
null
null
null
null
A mixture of naphthalene (40 g) and succinic anhydride (20 g) was added to a well stirred suspension of aluminum trichloride (55 g) in nitrobenzene (140 ml). The resulting mixture was stirred overnight at room temperature. The mixture was then poured slowly onto ice-water (600 g) and acidified with 6N-hydrochloric acid...
10.6084/m9.figshare.5104873.v1
null
Anhydride
Carboxylic acid.Ketone
C1CCOC1.c1ccc2ccccc2c1
c1ccc2ccccc2c1
c1ccc2ccccc2c1
null
[N+](=O)([O-])C1=CC=CC=C1
null
null
O=C1CCC(=O)O1.c1ccc2ccccc2c1>[N+](=O)([O-])C1=CC=CC=C1>O=C(O)CCC(=O)c1cccc2ccccc12
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-64d1801cfcd4465887e5bc7221651fa5
NN.O=C(O)CCCC(=O)c1ccccc1>>O=c1cccc(-c2ccccc2)nn1
C(C1=CC=CC=C1)(=O)CCCC(=O)O.NN.O>>C1(=CC=CC=C1)C1=CC=CC(N=N1)=O
[NH2:13][NH2:14].O=[C:6]([CH2:5][CH2:4][CH2:3][C:2](O)=[O:1])[c:7]1[cH:8][cH:9][cH:10][cH:11][cH:12]1>>[O:1]=[c:2]1[cH:3][cH:4][cH:5][c:6](-[c:7]2[cH:8][cH:9][cH:10][cH:11][cH:12]2)[n:13][n:14]1
NN.O=C(O)CCCC(=O)c1ccccc1
O=c1cccc(-c2ccccc2)nn1
null
null
C1(=CC=CC=C1)C.CCOCC
Aromatic Heterocycle Formation
OtherReaction
a31553d36b14882561a6dcdd04ef456bc0e14ea189c472490f94f02ebbe3ca3f
eadf9e657b4bde18ed656e299092aac7dd81eee1face1030775c3edd6ccba31c
O=c1cccc(-c2ccccc2)nn1
O-[C;H0;D3;+0:1](=[O;D1;H0:2])-[CH2;D2;+0:3]-[CH2;D2;+0:4]-[CH2;D2;+0:5]-[C;H0;D3;+0:6](=O)-[c;H0;D3;+0:7](:[c:8]:[c:9]):[c:10]:[c:11].[NH2;D1;+0:12]-[NH2;D1;+0:13]>>[O;D1;H0:2]=[c;H0;D3;+0:1]1:[cH;D2;+0:3]:[cH;D2;+0:4]:[cH;D2;+0:5]:[c;H0;D3;+0:6](-[c;H0;D3;+0:7](:[c:8]:[c:9]):[c:10]:[c:11]):[n;H0;D2;+0:12]:[n;H0;D2;+0...
39
[{"value": 39.0, "product": "C1(=CC=CC=C1)C1=CC=CC(N=N1)=O", "details": "PERCENTYIELD", "is_desired": false}]
null
null
null
null
To a mixture of 10 g (0.052 mole) of 4-benzoylbutyric acid in 300 ml of toluene, hydrazine was added in one portion and the reaction was heated to reflux until all water had ceased to azeotrope. The reaction mixture was cooled and the toluene was stripped off in vacuo. The residue was dissolved in 200 ml Et2O and washe...
10.6084/m9.figshare.5104873.v1
null
Hydrazine.Carboxylic acid.Ketone
null
null
c1cccc[nH]n1
c1cccc[nH]n1.c1ccccc1
HO-
C1(=CC=CC=C1)C.CCOCC
null
null
NN.O=C(O)CCCC(=O)c1ccccc1>C1(=CC=CC=C1)C.CCOCC>O=c1cccc(-c2ccccc2)nn1
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-54e336ac6c4f4117baf301a34b00c11e
COC(=O)OC.O=C1CCc2cc(Cl)ccc21>>COC(=O)C1Cc2cc(Cl)ccc2C1=O
COC(OC)=O.[H-].[Na+].ClC=1C=C2CCC(C2=CC1)=O.[H][H]>>C(=O)(OC)C1C(C2=CC=C(C=C2C1)Cl)=O
CO[C:3]([O:2][CH3:1])=[O:4].[CH2:5]1[CH2:6][c:7]2[cH:8][c:9]([Cl:10])[cH:11][cH:12][c:13]2[C:14]1=[O:15]>>[CH3:1][O:2][C:3](=[O:4])[CH:5]1[CH2:6][c:7]2[cH:8][c:9]([Cl:10])[cH:11][cH:12][c:13]2[C:14]1=[O:15]
COC(=O)OC.O=C1CCc2cc(Cl)ccc21
COC(=O)C1Cc2cc(Cl)ccc2C1=O
null
null
C(OC)COC
C-C Coupling
OtherReaction
c2c31337dfb867d8c28bc65df0ad4496f817a712a58e176523b47d7fdb6e4f91
d76b6fc9d01d8258e5777a3b2326a8d78a9d9a55717b27736ba55600205f4ed0
O=C1CCc2ccccc21
C-O-[C;H0;D3;+0:1](=[O;D1;H0:2])-[#8:3]-[C;D1;H3:4].[O;D1;H0:5]=[C:6]1-[CH2;D2;+0:7]-[C:8]-[c:9]:[c:10]-1>>[C;D1;H3:4]-[#8:3]-[C;H0;D3;+0:1](=[O;D1;H0:2])-[CH;D3;+0:7]1-[C:8]-[c:9]:[c:10]-[C:6]-1=[O;D1;H0:5]
45
[{"value": 45.0, "product": "C(=O)(OC)C1C(C2=CC=C(C=C2C1)Cl)=O", "details": "PERCENTYIELD", "is_desired": false}, {"value": 44.5, "product": "C(=O)(OC)C1C(C2=CC=C(C=C2C1)Cl)=O", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
60
CELSIUS
null
null
To a mixture of sodium hydride (2.4 g, 60% in mineral oil, 0.06 mole) and 50 ml dry dimethoxyethane, 5-chloroindanone (50 g, 0.03 mole) in 50 ml dimethoxyethane was added dropwise at room temperature. The mixture was stirred at room temperature until hydrogen evolution ceased. Then dimethylcarbonate (27 g, 0.3 mole) wa...
10.6084/m9.figshare.5104873.v1
null
Carbonic Ester.Ketone
Ketone.Ester
c1ccc2c(c1)CCC2
c1ccc2c(c1)CCC2
c1ccc2c(c1)CCC2
HO-
C(OC)COC
60
null
COC(=O)OC.O=C1CCc2cc(Cl)ccc21>C(OC)COC>COC(=O)C1Cc2cc(Cl)ccc2C1=O
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-8d9aaadeb71b457db37c796786d39ff2
CN(C)C=O.O=C(O)Cc1ccc(Cl)cc1>>CN(C)C=C(C=O)c1ccc(Cl)cc1
C([O-])([O-])=O.[K+].[K+].P(=O)(Cl)(Cl)Cl.CN(C)C=O.ClC1=CC=C(C=C1)CC(=O)O>>ClC1=CC=C(C=C1)C(C=O)=CN(C)C
O=[CH:4][N:2]([CH3:1])[CH3:3].O=[C:6]([CH2:5][c:8]1[cH:9][cH:10][c:11]([Cl:12])[cH:13][cH:14]1)[OH:7]>>[CH3:1][N:2]([CH3:3])[CH:4]=[C:5]([CH:6]=[O:7])[c:8]1[cH:9][cH:10][c:11]([Cl:12])[cH:13][cH:14]1
CN(C)C=O.O=C(O)Cc1ccc(Cl)cc1
CN(C)C=C(C=O)c1ccc(Cl)cc1
null
null
C1(=CC=CC=C1)C
Acylation
OtherReaction
cbf378fe57a2b8d8304e623fb5ce9ee6fb9f6e90d9c6f965226d56b103180e6d
a9c635686380f13b6b5c45d80d4aef36b30fdab0aef140b81f04c277f7ba737d
c1ccccc1
O=[C;H0;D3;+0:1](-[OH;D1;+0:2])-[CH2;D2;+0:3]-[c:4](:[c:5]):[c:6].O=[CH;D2;+0:7]-[#7:8](-[C;D1;H3:9])-[C;D1;H3:10]>>[C;D1;H3:9]-[#7:8](-[C;D1;H3:10])-[CH;D2;+0:7]=[C;H0;D3;+0:3](-[CH;D2;+0:1]=[O;H0;D1;+0:2])-[c:4](:[c:5]):[c:6]
null
[]
null
null
8
HOUR
Phosphorus oxychloride (92 g) was added dropwise to stirred DMF (78 ml) between 10°-15° C. To the resulting slurry was added 4-chlorophenylacetic acid (34.12 g). The resulting mixture was stirred at room temperature for one half hour and then heated to 70°-80° C. during 5.5 hours, during which time the mixture became e...
10.6084/m9.figshare.5104873.v1
null
Carboxylic acid.Tertiary amide
Enamine.Aldehyde
null
null
c1ccccc1
HO-
C1(=CC=CC=C1)C
null
8
CN(C)C=O.O=C(O)Cc1ccc(Cl)cc1>C1(=CC=CC=C1)C>CN(C)C=C(C=O)c1ccc(Cl)cc1