dataset_id
large_stringclasses
414 values
reaction_id
large_stringlengths
36
36
reaction_smiles
large_stringlengths
4
873
rxn_insight_reaction
large_stringlengths
19
1.07k
mapped_reaction_smiles
large_stringlengths
14
3.37k
reactant_smiles
large_stringlengths
1
581
product_smiles
large_stringlengths
1
433
reagent_smiles
large_stringclasses
634 values
catalyst_smiles
large_stringlengths
1
683
solvent_smiles
large_stringlengths
1
245
rxn_insight_class
large_stringclasses
11 values
rxn_insight_name
large_stringclasses
346 values
rxn_insight_tag
large_stringlengths
64
64
rxn_insight_tag2
large_stringlengths
64
64
rxn_insight_scaffold
large_stringlengths
5
288
rxn_insight_template
large_stringlengths
24
2.64k
yield_percent
float64
-0.8
90,205,160,000B
yield_measurements
large_stringlengths
2
864
temperature_value
float64
-230
30.1k
temperature_units
large_stringclasses
3 values
reaction_time_value
float64
0
4k
time_units
large_stringclasses
4 values
procedure_details
large_stringlengths
1
23.6k
reference
large_stringclasses
96 values
doi
large_stringclasses
19 values
functional_groups_reactants
large_stringlengths
3
716
functional_groups_products
large_stringlengths
3
539
participating_rings_reactants
large_stringlengths
5
293
participating_rings_products
large_stringlengths
5
271
all_rings_products
large_stringlengths
5
271
byproduct_smiles
large_stringclasses
176 values
agent_smiles
large_stringlengths
1
712
temperature_c
float64
-230
30.1k
reaction_time_hours
float64
0
2.16k
reaction_smiles_with_agents
large_stringlengths
4
882
ord_dataset-03ba810b7f464a06b5d8787af2e8b64e
ord-a881f7fabe29446d94622d478d282695
CC(C)N1CCN(C(=O)c2cnc(Cl)n2C)CC1.Cc1ccccc1B(O)O>>Cc1ccccc1-c1ncc(C(=O)N2CCN(C(C)C)CC2)n1C
[O-]P(=O)([O-])[O-].[K+].[K+].[K+].C1(=C(C=CC=C1)B(O)O)C.ClC1=NC=C(N1C)C(=O)N1CCN(CC1)C(C)C>>C(C)(C)N1CCN(CC1)C(=O)C=1N(C(=NC1)C1=C(C=CC=C1)C)C
Cl[c:8]1[n:9][cH:10][c:11]([C:12](=[O:13])[N:14]2[CH2:15][CH2:16][N:17]([CH:18]([CH3:19])[CH3:20])[CH2:21][CH2:22]2)[n:23]1[CH3:24].OB(O)[c:7]1[c:2]([CH3:1])[cH:3][cH:4][cH:5][cH:6]1>>[CH3:1][c:2]1[cH:3][cH:4][cH:5][cH:6][c:7]1-[c:8]1[n:9][cH:10][c:11]([C:12](=[O:13])[N:14]2[CH2:15][CH2:16][N:17]([CH:18]([CH3:19])[CH3:...
CC(C)N1CCN(C(=O)c2cnc(Cl)n2C)CC1.Cc1ccccc1B(O)O
Cc1ccccc1-c1ncc(C(=O)N2CCN(C(C)C)CC2)n1C
null
C=1C=CC(=CC1)/C=C/C(=O)/C=C/C2=CC=CC=C2.C=1C=CC(=CC1)/C=C/C(=O)/C=C/C2=CC=CC=C2.C=1C=CC(=CC1)/C=C/C(=O)/C=C/C2=CC=CC=C2.[Pd].[Pd]
C1(=CC=CC=C1)C
C-C Coupling
Suzuki coupling with boronic acids
ce1cab4967c1a0f6f99d4e333791783eedefe86bb34f4a4690c2f95ed6598bd8
08d2969413ef1a2cd5b43667268ba178160c7b55545bf48018e31f2b019632ec
O=C(c1cnc(-c2ccccc2)[nH]1)N1CCNCC1
Cl-[c;H0;D3;+0:1]1:[#7;a:2]:[c:3]:[c:4](-[C:5](-[#7:6])=[O;D1;H0:7]):[#7;a:8]:1-[C;D1;H3:9].O-B(-O)-[c;H0;D3;+0:10](:[c:11]:[c:12]):[c:13](-[C;D1;H3:14]):[c:15]>>[#7:6]-[C:5](=[O;D1;H0:7])-[c:4]1:[c:3]:[#7;a:2]:[c;H0;D3;+0:1](-[c;H0;D3;+0:10](:[c:11]:[c:12]):[c:13](-[C;D1;H3:14]):[c:15]):[#7;a:8]:1-[C;D1;H3:9]
null
[]
100
CELSIUS
16
HOUR
A reaction vessel is charged with Pd2(dba)3 (0.0183 g, 0.02 mmol), P(t-Bu)3HBF4 (0.0116 g, 0.04 mmol), K3PO4 (0.127 g, 0.60 mmol), o-tolylboronic acid (0.0408 g, 0.30 mmol) and (2-chloro-3-methyl-3H-imidazol-4-yl)-(4-isopropyl-piperazin-1-yl)-methanone (0.0542 g, 0.20 mmol). Toluene (2.4 mL, anhydrous) is added and the...
10.6084/m9.figshare.5104873.v1
null
Aromatic halide.Boronic acid
null
c1c[nH]cn1.c1ccccc1
c1ccccc1.c1c[nH]cn1
c1ccccc1.c1c[nH]cn1.C1C[NH]CC[NH]1
HCl.B
C=1C=CC(=CC1)/C=C/C(=O)/C=C/C2=CC=CC=C2.C=1C=CC(=CC1)/C=C/C(=O)/C=C/C2=CC=CC=C2.C=1C=CC(=CC1)/C=C/C(=O)/C=C/C2=CC=CC=C2.[Pd].[Pd].C1(=CC=CC=C1)C
100
16
CC(C)N1CCN(C(=O)c2cnc(Cl)n2C)CC1.Cc1ccccc1B(O)O>C=1C=CC(=CC1)/C=C/C(=O)/C=C/C2=CC=CC=C2.C=1C=CC(=CC1)/C=C/C(=O)/C=C/C2=CC=CC=C2.C=1C=CC(=CC1)/C=C/C(=O)/C=C/C2=CC=CC=C2.[Pd].[Pd].C1(=CC=CC=C1)C>Cc1ccccc1-c1ncc(C(=O)N2CCN(C(C)C)CC2)n1C
ord_dataset-03ba810b7f464a06b5d8787af2e8b64e
ord-8b22fd99aea743d896a2430827fb4c7c
CC(C)N1CCCNCC1.OCc1cnc(-c2ccccc2F)[nH]1>>CC(C)N1CCCN(Cc2cnc(-c3ccccc3F)[nH]2)CC1
FC1=C(C=CC=C1)C=1NC(=CN1)CO.C(C)(C)N1CCNCCC1>>FC1=C(C=CC=C1)C=1NC(=CN1)CN1CCN(CCC1)C(C)C
[CH3:1][CH:2]([CH3:3])[N:4]1[CH2:5][CH2:6][CH2:7][NH:8][CH2:22][CH2:23]1.O[CH2:9][c:10]1[cH:11][n:12][c:13](-[c:14]2[cH:15][cH:16][cH:17][cH:18][c:19]2[F:20])[nH:21]1>>[CH3:1][CH:2]([CH3:3])[N:4]1[CH2:5][CH2:6][CH2:7][N:8]([CH2:9][c:10]2[cH:11][n:12][c:13](-[c:14]3[cH:15][cH:16][cH:17][cH:18][c:19]3[F:20])[nH:21]2)[CH2...
CC(C)N1CCCNCC1.OCc1cnc(-c2ccccc2F)[nH]1
CC(C)N1CCCN(Cc2cnc(-c3ccccc3F)[nH]2)CC1
null
null
O=S(Cl)Cl
Heteroatom Alkylation and Arylation
OtherReaction
a7ea0b0d55fb0c7c14cafdf733d29854813a33bc3c453bf4a4c1ad47653fab35
87693a475e46c41583976158ec46dcaf8be8cc05c5635654a6a68033770f8d5c
c1ccc(-c2ncc(CN3CCCNCC3)[nH]2)cc1
O-[CH2;D2;+0:1]-[c:2]1:[#7;a:3]:[c:4]:[#7;a:5]:[c:6]:1.[#7:7]-[C:8]-[C:9]-[NH;D2;+0:10]-[C:11]-[C:12]>>[#7:7]-[C:8]-[C:9]-[N;H0;D3;+0:10](-[CH2;D2;+0:1]-[c:2]1:[#7;a:3]:[c:4]:[#7;a:5]:[c:6]:1)-[C:11]-[C:12]
null
[]
65
CELSIUS
1
HOUR
[2-(2-Fluorophenyl)-1H-imidazol-5-yl]methyl alcohol (69 mg, 0.36 mmol, prepared essentially as described in PCT International Publication No. WO 96/16040) is dissolved in SOCl2 (4 mL) and stirred at 65° C. for 1 hr. The reaction mixture is cooled to rt then concentrated in vacuo. The residue is dissolved in toluene, an...
10.6084/m9.figshare.5104873.v1
null
Primary alcohol.Secondary amine
Tertiary amine
C1C[NH]CCNC1
C1C[NH]CC[NH]C1
C1C[NH]CC[NH]C1.c1c[nH]cn1.c1ccccc1
HO-
O=S(Cl)Cl
65
1
CC(C)N1CCCNCC1.OCc1cnc(-c2ccccc2F)[nH]1>O=S(Cl)Cl>CC(C)N1CCCN(Cc2cnc(-c3ccccc3F)[nH]2)CC1
ord_dataset-03ba810b7f464a06b5d8787af2e8b64e
ord-84ab61881c3f4d459047f990649b7d88
CCOC(=O)c1nc(C)cs1.O=C1CCC(=O)N1Br>>CCOC(=O)c1nc(C)c(Br)s1
C1CC(=O)N(C1=O)Br.C(C)OC(=O)C=1SC=C(N1)C.C1CC(=O)N(C1=O)Br>>C(C)OC(=O)C=1SC(=C(N1)C)Br
[CH3:1][CH2:2][O:3][C:4](=[O:5])[c:6]1[n:7][c:8]([CH3:9])[cH:10][s:12]1.O=C1CCC(=O)N1[Br:11]>>[CH3:1][CH2:2][O:3][C:4](=[O:5])[c:6]1[n:7][c:8]([CH3:9])[c:10]([Br:11])[s:12]1
CCOC(=O)c1nc(C)cs1.O=C1CCC(=O)N1Br
CCOC(=O)c1nc(C)c(Br)s1
null
null
C(C)#N
Functional Group Interconversion
Bromination
3505c5a135ac37e3769ac5551611b02e62ded9217a3618731c0104022c0bad49
0e444576b73669992a4073cc3f7b10ed52cb9df09f9f8e4042e39e6a602aa390
c1cscn1
O=C1-C-C-C(=O)-N-1-[Br;H0;D1;+0:1].[#8:2]-[C:3](=[O;D1;H0:4])-[c:5]1:[#16;a:6]:[cH;D2;+0:7]:[c:8](-[C;D1;H3:9]):[#7;a:10]:1>>[#8:2]-[C:3](=[O;D1;H0:4])-[c:5]1:[#16;a:6]:[c;H0;D3;+0:7](-[Br;H0;D1;+0:1]):[c:8](-[C;D1;H3:9]):[#7;a:10]:1
null
[]
null
null
2
HOUR
To a solution of 4-methyl-thiazole-2-carboxylic acid ethyl ester (171 mg, 1.0 mmol) in acetonitrile (5 ml) is added NBS (180 mg, 1.0 mmol). The reaction mixture is stirred at rt for 2 hr followed by the addition of a second portion of NBS (180 mg, 1.0 mmol). After stirring at rt for 3 hr, the solvent is removed. The re...
10.6084/m9.figshare.5104873.v1
null
Tertiary amide.Tertiary amide
Aromatic halide
c1cscn1.C1CCNC1
c1cscn1
c1cscn1
HO-
C(C)#N
null
2
CCOC(=O)c1nc(C)cs1.O=C1CCC(=O)N1Br>C(C)#N>CCOC(=O)c1nc(C)c(Br)s1
ord_dataset-03ba810b7f464a06b5d8787af2e8b64e
ord-9f1c3eae5e914686a5941e976dd60d69
CCOC(=O)c1nc(C)c(Br)s1.OB(O)c1cccc2ccccc12>>CCOC(=O)c1nc(C)c(-c2cccc3ccccc23)s1
C(C)OC(=O)C=1SC(=C(N1)C)Br.C1(=CC=CC2=CC=CC=C12)B(O)O.C([O-])([O-])=O.[Cs+].[Cs+]>>C(C)OC(=O)C=1SC(=C(N1)C)C1=CC=CC2=CC=CC=C12
Br[c:10]1[c:8]([CH3:9])[n:7][c:6]([C:4]([O:3][CH2:2][CH3:1])=[O:5])[s:21]1.OB(O)[c:11]1[cH:12][cH:13][cH:14][c:15]2[cH:16][cH:17][cH:18][cH:19][c:20]12>>[CH3:1][CH2:2][O:3][C:4](=[O:5])[c:6]1[n:7][c:8]([CH3:9])[c:10](-[c:11]2[cH:12][cH:13][cH:14][c:15]3[cH:16][cH:17][cH:18][cH:19][c:20]23)[s:21]1
CCOC(=O)c1nc(C)c(Br)s1.OB(O)c1cccc2ccccc12
CCOC(=O)c1nc(C)c(-c2cccc3ccccc23)s1
null
C=1C=CC(=CC1)[P](C=2C=CC=CC2)(C=3C=CC=CC3)[Pd]([P](C=4C=CC=CC4)(C=5C=CC=CC5)C=6C=CC=CC6)([P](C=7C=CC=CC7)(C=8C=CC=CC8)C=9C=CC=CC9)[P](C=1C=CC=CC1)(C=1C=CC=CC1)C=1C=CC=CC1
O1CCOCC1
C-C Coupling
OtherReaction
38230c1273a69eec205027790ccd7ed227c21bd62e48400f1fb43e23d949bdb1
08d2969413ef1a2cd5b43667268ba178160c7b55545bf48018e31f2b019632ec
c1ccc2c(-c3cncs3)cccc2c1
Br-[c;H0;D3;+0:1]1:[#16;a:2]:[c:3](-[C:4](-[#8:5])=[O;D1;H0:6]):[#7;a:7]:[c:8]:1-[C;D1;H3:9].O-B(-O)-[c;H0;D3;+0:10](:[c:11]:[c:12]):[c:13](:[c:14]):[c:15]>>[#8:5]-[C:4](=[O;D1;H0:6])-[c:3]1:[#16;a:2]:[c;H0;D3;+0:1](-[c;H0;D3;+0:10](:[c:11]:[c:12]):[c:13](:[c:14]):[c:15]):[c:8](-[C;D1;H3:9]):[#7;a:7]:1
null
[]
110
CELSIUS
8
HOUR
To a solution of 5-bromo-4-methyl-thiazole-2-carboxylic acid ethyl ester (60 mg, 0.24 mmol) in 1,4-dioxane (2 ml) is added 1-naphthaleneboronic acid (50 mg, 0.29 mmol), cesium carbonate (187 mg, 0.58 mmol) and Pd(PPh3)4 (28 mg, 0.024 mmol). The reaction mixture is stirred in a sealed tube at 110° C. overnight. After co...
10.6084/m9.figshare.5104873.v1
null
Aromatic halide.Boronic acid
null
c1cscn1.c1ccc2ccccc2c1
c1cscn1.c1ccc2ccccc2c1
c1cscn1.c1ccc2ccccc2c1
HBr.B
C=1C=CC(=CC1)[P](C=2C=CC=CC2)(C=3C=CC=CC3)[Pd]([P](C=4C=CC=CC4)(C=5C=CC=CC5)C=6C=CC=CC6)([P](C=7C=CC=CC7)(C=8C=CC=CC8)C=9C=CC=CC9)[P](C=1C=CC=CC1)(C=1C=CC=CC1)C=1C=CC=CC1.O1CCOCC1
110
8
CCOC(=O)c1nc(C)c(Br)s1.OB(O)c1cccc2ccccc12>C=1C=CC(=CC1)[P](C=2C=CC=CC2)(C=3C=CC=CC3)[Pd]([P](C=4C=CC=CC4)(C=5C=CC=CC5)C=6C=CC=CC6)([P](C=7C=CC=CC7)(C=8C=CC=CC8)C=9C=CC=CC9)[P](C=1C=CC=CC1)(C=1C=CC=CC1)C=1C=CC=CC1.O1CCOCC1>CCOC(=O)c1nc(C)c(-c2cccc3ccccc23)s1
ord_dataset-03ba810b7f464a06b5d8787af2e8b64e
ord-a99f6adcd06645219a6b3df332299ba2
CCOC(=O)c1nc(C)c(-c2cccc3ccccc23)s1>>Cc1nc(C(=O)O)sc1-c1cccc2ccccc12
C(C)OC(=O)C=1SC(=C(N1)C)C1=CC=CC2=CC=CC=C12.[OH-].[Na+]>>CC=1N=C(SC1C1=CC=CC2=CC=CC=C12)C(=O)O
CC[O:7][C:5]([c:4]1[n:3][c:2]([CH3:1])[c:9](-[c:10]2[cH:11][cH:12][cH:13][c:14]3[cH:15][cH:16][cH:17][cH:18][c:19]23)[s:8]1)=[O:6]>>[CH3:1][c:2]1[n:3][c:4]([C:5](=[O:6])[OH:7])[s:8][c:9]1-[c:10]1[cH:11][cH:12][cH:13][c:14]2[cH:15][cH:16][cH:17][cH:18][c:19]12
CCOC(=O)c1nc(C)c(-c2cccc3ccccc23)s1
Cc1nc(C(=O)O)sc1-c1cccc2ccccc12
null
null
C1CCOC1.O
Deprotection
Ester saponification (alkyl deprotection)
d872e08ad5c85a4add6cd04e6e987e73fead5f79b3f30ba61a81ba5029b29894
38ae1ee78433b9acfb0390501446149c80f88f23ac2d84c60b3369bdab75cec9
c1ccc2c(-c3cncs3)cccc2c1
C-C-[O;H0;D2;+0:1]-[C:2](=[O;D1;H0:3])-[c:4](:[#16;a:5]):[#7;a:6]>>[#16;a:5]:[c:4](-[C:2](=[O;D1;H0:3])-[OH;D1;+0:1]):[#7;a:6]
null
[]
null
null
1
HOUR
To a solution of 4-methyl-5-naphthalen-1-yl-thiazole-2-carboxylic acid ethyl ester (30 mg, 0.10 mmol) in water (1 ml) and THF (1 ml) is added sodium hydroxide (0.2 mL, 1M, 0.20 mmol). The reaction mixture is stirred at rt for 1 hr, and then extracted with ethyl ether (30 mL). The aqueous layer is acidified to pH<7.0 by...
10.6084/m9.figshare.5104873.v1
null
Ester
Carboxylic acid
null
null
c1cscn1.c1ccc2ccccc2c1
Other
C1CCOC1.O
null
1
CCOC(=O)c1nc(C)c(-c2cccc3ccccc23)s1>C1CCOC1.O>Cc1nc(C(=O)O)sc1-c1cccc2ccccc12
ord_dataset-03ba810b7f464a06b5d8787af2e8b64e
ord-1fd45a014550457f9029f2a892cfb77e
CC(C)N1CCNCC1.Cc1nc(C(=O)O)sc1-c1cccc2ccccc12>>Cc1nc(C(=O)N2CCN(C(C)C)CC2)sc1-c1cccc2ccccc12
CC=1N=C(SC1C1=CC=CC2=CC=CC=C12)C(=O)O.F[P-](F)(F)(F)(F)F.N1(N=NC2=C1C=CC=C2)O[P+](N(C)C)(N(C)C)N(C)C.C(C)(C)N1CCNCC1.CCN(CC)CC>>C(C)(C)N1CCN(CC1)C(=O)C=1SC(=C(N1)C)C1=CC=CC2=CC=CC=C12
[NH:7]1[CH2:8][CH2:9][N:10]([CH:11]([CH3:12])[CH3:13])[CH2:14][CH2:15]1.O[C:5]([c:4]1[n:3][c:2]([CH3:1])[c:17](-[c:18]2[cH:19][cH:20][cH:21][c:22]3[cH:23][cH:24][cH:25][cH:26][c:27]23)[s:16]1)=[O:6]>>[CH3:1][c:2]1[n:3][c:4]([C:5](=[O:6])[N:7]2[CH2:8][CH2:9][N:10]([CH:11]([CH3:12])[CH3:13])[CH2:14][CH2:15]2)[s:16][c:17]...
CC(C)N1CCNCC1.Cc1nc(C(=O)O)sc1-c1cccc2ccccc12
Cc1nc(C(=O)N2CCN(C(C)C)CC2)sc1-c1cccc2ccccc12
null
null
C(Cl)Cl
Acylation
Acylation of Nitrogen Nucleophiles by Carboxylic Acids
ed26ef5eea92a0cc433b3f89a34f4c61724425fa15a9d0ec83a0f7a903eec831
c5e4172490b2731ba9322b68af56376edadc31ce0bb9a3dfdea23a1817a852fd
O=C(c1ncc(-c2cccc3ccccc23)s1)N1CCNCC1
O-[C;H0;D3;+0:1](=[O;D1;H0:2])-[c:3]1:[#16;a:4]:[c:5]:[c:6]:[#7;a:7]:1.[#7:8]1-[C:9]-[C:10]-[NH;D2;+0:11]-[C:12]-[C:13]-1>>[O;D1;H0:2]=[C;H0;D3;+0:1](-[N;H0;D3;+0:11]1-[C:10]-[C:9]-[#7:8]-[C:13]-[C:12]-1)-[c:3]1:[#16;a:4]:[c:5]:[c:6]:[#7;a:7]:1
null
[]
null
null
2
HOUR
To a solution of 4-methyl-5-naphthalen-1-yl-thiazole-2-carboxylic acid in methylene chloride (2 ml) is added BOP (44 mg, 0.10 mmol), isopropylpiperazine (13 mg, 0.10 mmol) and Et3N (20 mg, 0.20 mmol). The reaction mixture is stirred at rt for 2 hr. Solvent is removed and the resulting mixture is purified by PTLC to giv...
10.6084/m9.figshare.5104873.v1
null
Carboxylic acid.Secondary amine
Tertiary amide
C1CNCC[NH]1
C1C[NH]CC[NH]1
c1cscn1.C1C[NH]CC[NH]1.c1ccc2ccccc2c1
HO-
C(Cl)Cl
null
2
CC(C)N1CCNCC1.Cc1nc(C(=O)O)sc1-c1cccc2ccccc12>C(Cl)Cl>Cc1nc(C(=O)N2CCN(C(C)C)CC2)sc1-c1cccc2ccccc12
ord_dataset-03ba810b7f464a06b5d8787af2e8b64e
ord-46dcf18ec7cf41598714200c3bd40942
Brc1nc(Br)c(Br)[nH]1.CCI>>CCn1c(Br)nc(Br)c1Br
[H-].[Na+].BrC=1NC(=C(N1)Br)Br.ICC>>BrC=1N(C(=C(N1)Br)Br)CC
[nH:3]1[c:4]([Br:5])[n:6][c:7]([Br:8])[c:9]1[Br:10].I[CH2:2][CH3:1]>>[CH3:1][CH2:2][n:3]1[c:4]([Br:5])[n:6][c:7]([Br:8])[c:9]1[Br:10]
Brc1nc(Br)c(Br)[nH]1.CCI
CCn1c(Br)nc(Br)c1Br
null
null
CN(C)C=O
Heteroatom Alkylation and Arylation
N-alkylation of secondary amines with alkyl halides
b9d84e1ee028da6e8c5d8924d45fbf8f3755d9adc2caf0035bd5ed7f30f5ee03
2e1e5fd9557b69cb528f6b2ffd179c67ef24ecb1a2c3994e1cdf0efe7ae19e9c
c1c[nH]cn1
I-[CH2;D2;+0:1]-[C;D1;H3:2].[Br;D1;H0:3]-[c:4]1:[nH;D2;+0:5]:[c:6](-[Br;D1;H0:7]):[#7;a:8]:[c:9]:1-[Br;D1;H0:10]>>[Br;D1;H0:3]-[c:4]1:[c:9](-[Br;D1;H0:10]):[#7;a:8]:[c:6](-[Br;D1;H0:7]):[n;H0;D3;+0:5]:1-[CH2;D2;+0:1]-[C;D1;H3:2]
null
[]
50
CELSIUS
1
HOUR
To a suspension of sodium hydride (2.40 g, 60% mineral oil suspension, 60 mmol) in anhydrous DMF (50 ml) is added a solution of 2,4,5-tribromoimidazole (15.09 g, 50 mmol) in DMF (30 ml) at rt. The resulting mixture is stirred at 50° C. for 1 hr, and then cooled to 0° C., followed by the dropwise addition of iodoethane ...
10.6084/m9.figshare.5104873.v1
null
Primary halide
null
c1c[nH]cn1
c1c[nH]cn1
c1c[nH]cn1
HI
CN(C)C=O
50
1
Brc1nc(Br)c(Br)[nH]1.CCI>CN(C)C=O>CCn1c(Br)nc(Br)c1Br
ord_dataset-03ba810b7f464a06b5d8787af2e8b64e
ord-707e734d43db4ad18a4482477ac34ea0
CCn1c(Br)nc(Br)c1Br.OB(Oc1cccc2ccccc12)c1ccccc1>>CCn1c(-c2cccc3ccccc23)nc(Br)c1Br
BrC=1N(C(=C(N1)Br)Br)CC.C1(=CC=CC2=CC=CC=C12)OB(O)C1=CC=CC=C1.C([O-])([O-])=O.[K+].[K+]>>BrC=1N=C(N(C1Br)CC)C1=CC=CC2=CC=CC=C12
Br[c:4]1[n:3]([CH2:2][CH3:1])[c:18]([Br:19])[c:16]([Br:17])[n:15]1.OB(O[c:5]1[cH:6][cH:7][cH:8][c:9]2[cH:10][cH:11][cH:12][cH:13][c:14]12)c1ccccc1>>[CH3:1][CH2:2][n:3]1[c:4](-[c:5]2[cH:6][cH:7][cH:8][c:9]3[cH:10][cH:11][cH:12][cH:13][c:14]23)[n:15][c:16]([Br:17])[c:18]1[Br:19]
CCn1c(Br)nc(Br)c1Br.OB(Oc1cccc2ccccc12)c1ccccc1
CCn1c(-c2cccc3ccccc23)nc(Br)c1Br
null
C=1C=CC(=CC1)[P](C=2C=CC=CC2)(C=3C=CC=CC3)[Pd]([P](C=4C=CC=CC4)(C=5C=CC=CC5)C=6C=CC=CC6)([P](C=7C=CC=CC7)(C=8C=CC=CC8)C=9C=CC=CC9)[P](C=1C=CC=CC1)(C=1C=CC=CC1)C=1C=CC=CC1
C1(=CC=CC=C1)C
C-C Coupling
OtherReaction
1e4b1876d7dd5c6837ce8a1dd3cb5cd6aa9f3a18e5846c4c841270b23816f12e
48892094855745f5c51f8910c27ce7c101e08ad3f9da2a58d5512e3d9c1b432f
c1ccc2c(-c3ncc[nH]3)cccc2c1
Br-[c;H0;D3;+0:1]1:[#7;a:2]:[c:3]:[c:4]:[#7;a:5]:1-[C:6].O-B(-O-[c;H0;D3;+0:7](:[c:8]:[c:9]):[c:10](:[c:11]):[c:12])-c1:c:c:c:c:c:1>>[C:6]-[#7;a:5]1:[c:4]:[c:3]:[#7;a:2]:[c;H0;D3;+0:1]:1-[c;H0;D3;+0:7](:[c:8]:[c:9]):[c:10](:[c:11]):[c:12]
null
[]
90
CELSIUS
16
HOUR
To a solution of 2,4,5-tribromo-1-ethyl-1H-imidazole (13.19 g, 40 mmol) and 1-naphthylphenylboronic acid (6.88 g, 40 mmol, 1.0 eq.) in toluene (100 ml) is added aqueous potassium carbonate solution (2.0 N, 40 ml, 2.0 eq.), followed by the addition of Pd(PPh3)4 (1.154 g, 1 mmol, 0.025 eq.). The resulting mixture is dega...
10.6084/m9.figshare.5104873.v1
null
Aromatic halide
null
c1c[nH]cn1.c1ccc2ccccc2c1.c1ccccc1
c1c[nH]cn1.c1ccc2ccccc2c1
c1c[nH]cn1.c1ccc2ccccc2c1
HBr.B
C=1C=CC(=CC1)[P](C=2C=CC=CC2)(C=3C=CC=CC3)[Pd]([P](C=4C=CC=CC4)(C=5C=CC=CC5)C=6C=CC=CC6)([P](C=7C=CC=CC7)(C=8C=CC=CC8)C=9C=CC=CC9)[P](C=1C=CC=CC1)(C=1C=CC=CC1)C=1C=CC=CC1.C1(=CC=CC=C1)C
90
16
CCn1c(Br)nc(Br)c1Br.OB(Oc1cccc2ccccc12)c1ccccc1>C=1C=CC(=CC1)[P](C=2C=CC=CC2)(C=3C=CC=CC3)[Pd]([P](C=4C=CC=CC4)(C=5C=CC=CC5)C=6C=CC=CC6)([P](C=7C=CC=CC7)(C=8C=CC=CC8)C=9C=CC=CC9)[P](C=1C=CC=CC1)(C=1C=CC=CC1)C=1C=CC=CC1.C1(=CC=CC=C1)C>CCn1c(-c2cccc3ccccc23)nc(Br)c1Br
ord_dataset-03ba810b7f464a06b5d8787af2e8b64e
ord-a8f3af09900c4770b3608276e00844f6
CCn1c(-c2cccc3ccccc23)nc(Br)c1Br.CN(C)C=O>>CCn1cc(C=O)nc1-c1cccc2ccccc12
C[Si](C)(C)Cl.CN(C)C=O.BrC=1N=C(N(C1Br)CC)C1=CC=CC2=CC=CC=C12.[Li]CCCC.CCCCCC.[Li]CCCC.CCCCCC>>C(C)N1C(=NC(=C1)C=O)C1=CC=CC2=CC=CC=C12
Br[c:4]1[n:3]([CH2:2][CH3:1])[c:9](-[c:10]2[cH:11][cH:12][cH:13][c:14]3[cH:15][cH:16][cH:17][cH:18][c:19]23)[n:8][c:5]1Br.CN(C)[CH:6]=[O:7]>>[CH3:1][CH2:2][n:3]1[cH:4][c:5]([CH:6]=[O:7])[n:8][c:9]1-[c:10]1[cH:11][cH:12][cH:13][c:14]2[cH:15][cH:16][cH:17][cH:18][c:19]12
CCn1c(-c2cccc3ccccc23)nc(Br)c1Br.CN(C)C=O
CCn1cc(C=O)nc1-c1cccc2ccccc12
null
null
CO.C1CCOC1.O
C-C Coupling
OtherReaction
9af6f9293276ec09762e7d33d47452238683ac4d42196c8b23ccaf7c6c11e003
d9c4461141b547f59eb6421e79e298156f74861075f2c22966c0a28a10b10c96
c1ccc2c(-c3ncc[nH]3)cccc2c1
Br-[c;H0;D3;+0:1]1:[#7;a:2](-[C:3]):[c:4](-[c:5]):[#7;a:6]:[c;H0;D3;+0:7]:1-Br.C-N(-C)-[CH;D2;+0:8]=[O;D1;H0:9]>>[C:3]-[#7;a:2]1:[cH;D2;+0:1]:[c;H0;D3;+0:7](-[CH;D2;+0:8]=[O;D1;H0:9]):[#7;a:6]:[c:4]:1-[c:5]
null
[]
-78
CELSIUS
1
HOUR
To a solution of 4,5-dibromo-1-ethyl-2-naphthalen-1-yl-1H-imidazole (3.80 g, 10 mmol) in anhydrous THF (60 ml) at −78° C. under nitrogen is added a solution of n-BuLi in hexane (1.6 M, 6.88 ml, 11 mmol, 1.1 eq.) dropwise. The resulting mixture is stirred at −78° C. for 1 hr, followed by dropwise addition of TMSCl (1.18...
10.6084/m9.figshare.5104873.v1
null
Aromatic halide.Aromatic halide.Tertiary amide
Aldehyde
c1c[nH]cn1
c1c[nH]cn1
c1c[nH]cn1.c1ccc2ccccc2c1
HBr
CO.C1CCOC1.O
-78
1
CCn1c(-c2cccc3ccccc23)nc(Br)c1Br.CN(C)C=O>CO.C1CCOC1.O>CCn1cc(C=O)nc1-c1cccc2ccccc12
ord_dataset-03ba810b7f464a06b5d8787af2e8b64e
ord-8d1cd2d6e27b4b369888a3d951b36078
CCOc1ccc2ccccc2c1-c1ncc(C=O)n1COC>>CCOc1ccc2ccccc2c1-c1ncc(C=O)[nH]1
C(C)OC1=C(C2=CC=CC=C2C=C1)C1=NC=C(N1COC)C=O.Cl>>C(C)OC1=C(C2=CC=CC=C2C=C1)C1=NC=C(N1)C=O
COC[n:20]1[c:14](-[c:13]2[c:4]([O:3][CH2:2][CH3:1])[cH:5][cH:6][c:7]3[cH:8][cH:9][cH:10][cH:11][c:12]32)[n:15][cH:16][c:17]1[CH:18]=[O:19]>>[CH3:1][CH2:2][O:3][c:4]1[cH:5][cH:6][c:7]2[cH:8][cH:9][cH:10][cH:11][c:12]2[c:13]1-[c:14]1[n:15][cH:16][c:17]([CH:18]=[O:19])[nH:20]1
CCOc1ccc2ccccc2c1-c1ncc(C=O)n1COC
CCOc1ccc2ccccc2c1-c1ncc(C=O)[nH]1
null
null
O1CCOCC1
Reduction
OtherReaction
c2dcbe9d831e37c9851593e99e077458c2c2bd822601c7bc7ae4afe468a8014c
84394d34c591024a84d9393eb3e8adb8ada5a6225c3abafc4dae9aedd4568be4
c1ccc2c(-c3ncc[nH]3)cccc2c1
C-O-C-[n;H0;D3;+0:1]1:[c:2](-[c:3]):[#7;a:4]:[c:5]:[c:6]:1-[C:7]=[O;D1;H0:8]>>[O;D1;H0:8]=[C:7]-[c:6]1:[c:5]:[#7;a:4]:[c:2](-[c:3]):[nH;D2;+0:1]:1
null
[]
80
CELSIUS
3
HOUR
To a solution of 2-(2-ethoxy-naphthalen-1-yl)-3-methoxymethyl-3H-imidazole-4-carbaldehyde (prepared as described for 1-ethyl-2-naphthalen-1-yl-1H-imidazole-4-carbaldehyde illustrated in example 2.F) (2.4 g, 7.4 mmol) in dioxane (30 ml) is added 6.0 N hydrochloric acid (10 ml). The resulting mixture is stirred at 80° C....
10.6084/m9.figshare.5104873.v1
null
Ether
null
c1cnc[nH]1
c1c[nH]cn1
c1ccc2ccccc2c1.c1c[nH]cn1
HO-
O1CCOCC1
80
3
CCOc1ccc2ccccc2c1-c1ncc(C=O)n1COC>O1CCOCC1>CCOc1ccc2ccccc2c1-c1ncc(C=O)[nH]1
ord_dataset-03ba810b7f464a06b5d8787af2e8b64e
ord-2b9f425e2c714e618d94b5bb6d3af4c4
CCOC(=O)OCC.CCn1c(-c2cccc3ccccc23)nc(Br)c1Br>>CCOC(=O)c1cn(CC)c(-c2cccc3ccccc23)n1
BrC=1N=C(N(C1Br)CC)C1=CC=CC2=CC=CC=C12.[Li]CCCC.CCCCCC.[Li]CCCC.CCCCCC.Cl[Si](C)(C)C.C(OCC)(OCC)=O.[F-].C(CCC)[N+](CCCC)(CCCC)CCCC>>C(C)OC(=O)C=1N=C(N(C1)CC)C1=CC=CC2=CC=CC=C12
CCO[C:4]([O:3][CH2:2][CH3:1])=[O:5].Br[c:6]1[c:7](Br)[n:8]([CH2:9][CH3:10])[c:11](-[c:12]2[cH:13][cH:14][cH:15][c:16]3[cH:17][cH:18][cH:19][cH:20][c:21]23)[n:22]1>>[CH3:1][CH2:2][O:3][C:4](=[O:5])[c:6]1[cH:7][n:8]([CH2:9][CH3:10])[c:11](-[c:12]2[cH:13][cH:14][cH:15][c:16]3[cH:17][cH:18][cH:19][cH:20][c:21]23)[n:22]1
CCOC(=O)OCC.CCn1c(-c2cccc3ccccc23)nc(Br)c1Br
CCOC(=O)c1cn(CC)c(-c2cccc3ccccc23)n1
null
null
C1CCOC1.O
C-C Coupling
OtherReaction
1884e22398b71b80056168b5b49cb39632cc01fe6aef2cf776dc7828546cc3c4
850228b587f13401a2131f8a953feaad6e5b5201ccc2bd72a0da57c6c2c84ed9
c1ccc2c(-c3ncc[nH]3)cccc2c1
Br-[c;H0;D3;+0:1]1:[#7;a:2]:[c:3](-[c:4]):[#7;a:5](-[C:6]):[c;H0;D3;+0:7]:1-Br.C-C-O-[C;H0;D3;+0:8](=[O;D1;H0:9])-[#8:10]-[C:11]>>[C:11]-[#8:10]-[C;H0;D3;+0:8](=[O;D1;H0:9])-[c;H0;D3;+0:1]1:[#7;a:2]:[c:3](-[c:4]):[#7;a:5](-[C:6]):[cH;D2;+0:7]:1
null
[]
-78
CELSIUS
1
HOUR
To a solution of 4,5-dibromo-1-ethyl-2-naphthalen-1-yl-1H-imidazole (3.80 g, 10 mmol) in anhydrous THF (60 ml) at −78° C. under nitrogen is added a solution of n-BuLi in hexane (1.6 M, 6.88 ml, 11 mmol, 1.1 eq.) dropwise. The resulting mixture is stirred at −78° C. for 1 hr, after which chlorotrimethylsilane (1.188 g, ...
10.6084/m9.figshare.5104873.v1
null
Aromatic halide.Aromatic halide.Carbonic Ester
Ester
c1c[nH]cn1
c1c[nH]cn1
c1c[nH]cn1.c1ccc2ccccc2c1
HBr
C1CCOC1.O
-78
1
CCOC(=O)OCC.CCn1c(-c2cccc3ccccc23)nc(Br)c1Br>C1CCOC1.O>CCOC(=O)c1cn(CC)c(-c2cccc3ccccc23)n1
ord_dataset-03ba810b7f464a06b5d8787af2e8b64e
ord-e1d19fefd1aa46a38ad1627104fb90fd
CCOC(=O)c1cn(CC)c(-c2cccc3ccccc23)n1>>CCn1cc(C(=O)O)nc1-c1cccc2ccccc12
C(C)OC(=O)C=1N=C(N(C1)CC)C1=CC=CC2=CC=CC=C12.[OH-].[Li+]>>C(C)N1C(=NC(=C1)C(=O)O)C1=CC=CC2=CC=CC=C12
CC[O:8][C:6]([c:5]1[cH:4][n:3]([CH2:2][CH3:1])[c:10](-[c:11]2[cH:12][cH:13][cH:14][c:15]3[cH:16][cH:17][cH:18][cH:19][c:20]23)[n:9]1)=[O:7]>>[CH3:1][CH2:2][n:3]1[cH:4][c:5]([C:6](=[O:7])[OH:8])[n:9][c:10]1-[c:11]1[cH:12][cH:13][cH:14][c:15]2[cH:16][cH:17][cH:18][cH:19][c:20]12
CCOC(=O)c1cn(CC)c(-c2cccc3ccccc23)n1
CCn1cc(C(=O)O)nc1-c1cccc2ccccc12
null
null
C1CCOC1.O
Deprotection
Ester saponification (alkyl deprotection)
d872e08ad5c85a4add6cd04e6e987e73fead5f79b3f30ba61a81ba5029b29894
38ae1ee78433b9acfb0390501446149c80f88f23ac2d84c60b3369bdab75cec9
c1ccc2c(-c3ncc[nH]3)cccc2c1
C-C-[O;H0;D2;+0:1]-[C:2](=[O;D1;H0:3])-[c:4](:[#7;a:5]):[c:6]:[#7;a:7]>>[#7;a:7]:[c:6]:[c:4](-[C:2](=[O;D1;H0:3])-[OH;D1;+0:1]):[#7;a:5]
null
[]
50
CELSIUS
null
null
1-Ethyl-2-naphthalen-1-yl-1H-imidazole-4-carboxylic acid ethyl ester (2.2 g, 7.48 mmol) is dissolved in THF (20 ml), followed by the addition of aqueous lithium hydroxide solution (2.0 N, 7.5 ml, 2.0 eq.). The mixture is heated at 50° C. overnight. THF is stripped off under reduced pressure, and the residue is diluted ...
10.6084/m9.figshare.5104873.v1
null
Ester
Carboxylic acid
null
null
c1c[nH]cn1.c1ccc2ccccc2c1
Other
C1CCOC1.O
50
null
CCOC(=O)c1cn(CC)c(-c2cccc3ccccc23)n1>C1CCOC1.O>CCn1cc(C(=O)O)nc1-c1cccc2ccccc12
ord_dataset-03ba810b7f464a06b5d8787af2e8b64e
ord-80f85a55b5bb42a9b5fddbc41a2802c1
CCI.c1ccc2c(-c3ncc[nH]3)cccc2c1>>CCn1ccnc1-c1cccc2ccccc12
[H-].[Na+].C1(=CC=CC2=CC=CC=C12)C=1NC=CN1.ICC>>C(C)N1C(=NC=C1)C1=CC=CC2=CC=CC=C12
I[CH2:2][CH3:1].[nH:3]1[cH:4][cH:5][n:6][c:7]1-[c:8]1[cH:9][cH:10][cH:11][c:12]2[cH:13][cH:14][cH:15][cH:16][c:17]12>>[CH3:1][CH2:2][n:3]1[cH:4][cH:5][n:6][c:7]1-[c:8]1[cH:9][cH:10][cH:11][c:12]2[cH:13][cH:14][cH:15][cH:16][c:17]12
CCI.c1ccc2c(-c3ncc[nH]3)cccc2c1
CCn1ccnc1-c1cccc2ccccc12
null
null
CN(C)C=O
Heteroatom Alkylation and Arylation
N-alkylation of secondary amines with alkyl halides
5118ce9eea46859cccf16d01cf8151757afd816de0c93fe6fcb74a0ee15c5a67
2e1e5fd9557b69cb528f6b2ffd179c67ef24ecb1a2c3994e1cdf0efe7ae19e9c
c1ccc2c(-c3ncc[nH]3)cccc2c1
I-[CH2;D2;+0:1]-[C;D1;H3:2].[c:3]-[c:4]1:[#7;a:5]:[c:6]:[c:7]:[nH;D2;+0:8]:1>>[C;D1;H3:2]-[CH2;D2;+0:1]-[n;H0;D3;+0:8]1:[c:7]:[c:6]:[#7;a:5]:[c:4]:1-[c:3]
null
[]
50
CELSIUS
1
HOUR
To a suspension of sodium hydride (2.40 g, 60% mineral oil suspension, 60 mmol) in anhydrous DMF (30 ml) is added a solution of 2-naphthalen-1-yl-1H-imidazole (9.70 g, 50 mmol) in DMF (70 ml) at rt. The resulting mixture is stirred at 50° C. for 1 hr, and then cooled to 0° C., after which iodoethane (8.19 g, 52.5 mmol,...
10.6084/m9.figshare.5104873.v1
null
Primary halide
null
c1c[nH]cn1
c1ncc[nH]1
c1ncc[nH]1.c1ccc2ccccc2c1
HI
CN(C)C=O
50
1
CCI.c1ccc2c(-c3ncc[nH]3)cccc2c1>CN(C)C=O>CCn1ccnc1-c1cccc2ccccc12
ord_dataset-03ba810b7f464a06b5d8787af2e8b64e
ord-2a1bb3c7e7b748988571efc43482488c
CCOC(=O)OCC.CCn1ccnc1-c1cccc2ccccc12>>CCOC(=O)c1cnc(-c2cccc3ccccc23)n1CC
C(OCC)(OCC)=O.C(C)N1C(=NC=C1)C1=CC=CC2=CC=CC=C12.[Li]CCCC.CCCCCC>>C(C)OC(=O)C=1N(C(=NC1)C1=CC=CC2=CC=CC=C12)CC
CCO[C:4]([O:3][CH2:2][CH3:1])=[O:5].[cH:6]1[cH:7][n:8][c:9](-[c:10]2[cH:11][cH:12][cH:13][c:14]3[cH:15][cH:16][cH:17][cH:18][c:19]23)[n:20]1[CH2:21][CH3:22]>>[CH3:1][CH2:2][O:3][C:4](=[O:5])[c:6]1[cH:7][n:8][c:9](-[c:10]2[cH:11][cH:12][cH:13][c:14]3[cH:15][cH:16][cH:17][cH:18][c:19]23)[n:20]1[CH2:21][CH3:22]
CCOC(=O)OCC.CCn1ccnc1-c1cccc2ccccc12
CCOC(=O)c1cnc(-c2cccc3ccccc23)n1CC
null
null
C1CCOC1.O
C-C Coupling
Friedel-Crafts acylation
81f148e084f1dd3db2054da155451057eb8681cac5b90e511cba933650fa3985
372f84de287e46e8e402e2fc0f416c45846439cb3eb957465fe2464b708bdd7f
c1ccc2c(-c3ncc[nH]3)cccc2c1
C-C-O-[C;H0;D3;+0:1](=[O;D1;H0:2])-[#8:3]-[C:4].[C:5]-[#7;a:6]1:[cH;D2;+0:7]:[c:8]:[#7;a:9]:[c:10]:1-[c:11]>>[C:5]-[#7;a:6]1:[c:10](-[c:11]):[#7;a:9]:[c:8]:[c;H0;D3;+0:7]:1-[C;H0;D3;+0:1](=[O;D1;H0:2])-[#8:3]-[C:4]
null
[]
-78
CELSIUS
1
HOUR
To a solution of 1-ethyl-2-naphthalen-1-yl-1H-imidazole (1.11 g, 5 mmol) in anhydrous THF (30 ml) at −78° C. under nitrogen is added a solution of n-BuLi in hexane (1.6 M, 3.44 ml, 5.5 mmol, 1.1 eq.) dropwise. The resulting mixture is stirred at −78° C. for 1 hr, followed by the addition of diethyl carbonate (1.77 g, 1...
10.6084/m9.figshare.5104873.v1
null
Carbonic Ester
Ester
c1ncc[nH]1
c1c[nH]cn1
c1c[nH]cn1.c1ccc2ccccc2c1
HO-
C1CCOC1.O
-78
1
CCOC(=O)OCC.CCn1ccnc1-c1cccc2ccccc12>C1CCOC1.O>CCOC(=O)c1cnc(-c2cccc3ccccc23)n1CC
ord_dataset-03ba810b7f464a06b5d8787af2e8b64e
ord-7e7002a68c61423684a943412eae5f7c
CCN(CC)CC.CCn1c(C(=O)O)cnc1-c1cccc2ccccc12.CN(C)[P+](On1nnc2ccccc21)(N(C)C)N(C)C>>CCn1c(C(=O)N2CCN(C3CCC3)CC2)cnc1-c1cccc2ccccc12
F[P-](F)(F)(F)(F)F.N1(N=NC2=C1C=CC=C2)O[P+](N(C)C)(N(C)C)N(C)C.C(C)N1C(=NC=C1C(=O)O)C1=CC=CC2=CC=CC=C12.CCN(CC)CC>>C1(CCC1)N1CCN(CC1)C(=O)C=1N(C(=NC1)C1=CC=CC2=CC=CC=C12)CC
[CH3:8][CH2:9][N:10]([CH2:11][CH3:12])[CH2:15][CH3:16].O[C:5]([c:4]1[n:3]([CH2:2][CH3:1])[c:19](-[c:20]2[cH:21][cH:22][cH:23][c:24]3[cH:25][cH:26][cH:27][cH:28][c:29]23)[n:18][cH:17]1)=[O:6].CN(C)[P+](On1n[n:7]c2cc[cH:13][cH:14]c21)(N(C)C)N(C)C>>[CH3:1][CH2:2][n:3]1[c:4]([C:5](=[O:6])[N:7]2[CH2:8][CH2:9][N:10]([CH:11]3...
CCN(CC)CC.CCn1c(C(=O)O)cnc1-c1cccc2ccccc12.CN(C)[P+](On1nnc2ccccc21)(N(C)C)N(C)C
CCn1c(C(=O)N2CCN(C3CCC3)CC2)cnc1-c1cccc2ccccc12
null
null
C(Cl)Cl
Acylation
OtherReaction
69ee77d23b05939e46a0f531d3c7c366c2e80e0a094236d12c3e891cd946cbde
76edb1f56d3da33321282224061a3172c17caed194f0edd7470584306a88361e
O=C(c1cnc(-c2cccc3ccccc23)[nH]1)N1CCN(C2CCC2)CC1
C-N(-C)-[P+](-O-n1:n:[n;H0;D2;+0:1]:c2:c:c:[cH;D2;+0:2]:[cH;D2;+0:3]:c:2:1)(-N(-C)-C)-N(-C)-C.O-[C;H0;D3;+0:4](=[O;D1;H0:5])-[c:6]1:[c:7]:[#7;a:8]:[c:9]:[#7;a:10]:1-[C:11].[CH3;D1;+0:12]-[CH2;D2;+0:13]-[#7:14](-[C:15]-[CH3;D1;+0:16])-[C:17]-[CH3;D1;+0:18]>>[C:11]-[#7;a:10]1:[c:9]:[#7;a:8]:[c:7]:[c:6]:1-[C;H0;D3;+0:4](=...
null
[]
null
null
8
HOUR
3-Ethyl-2-naphthalen-1-yl-3H-imidazole-4-carboxylic acid (105 mg, 0.394 mmol) and 1-cyclobutylpiperazine bistrifluoroacetate (145 mg, 0.394 mmol, 1.0 eq.) are dissolved in DCM (5 ml), and to the solution is added Et3N (4 eq.), followed by BOP coupling regent (183 mg, 0.433 mmol, 1.1 eq.). The resulting mixture is stirr...
10.6084/m9.figshare.5104873.v1
null
Carboxylic acid.Tertiary amine.Tertiary amine.Tertiary amine
Tertiary amide
c1ccc2[nH]nnc2c1
C1C[NH]CC[NH]1.C1CCC1
c1cnc[nH]1.C1C[NH]CC[NH]1.C1CCC1.c1ccc2ccccc2c1
HO-
C(Cl)Cl
null
8
CCN(CC)CC.CCn1c(C(=O)O)cnc1-c1cccc2ccccc12.CN(C)[P+](On1nnc2ccccc21)(N(C)C)N(C)C>C(Cl)Cl>CCn1c(C(=O)N2CCN(C3CCC3)CC2)cnc1-c1cccc2ccccc12
ord_dataset-03ba810b7f464a06b5d8787af2e8b64e
ord-712d0ca79ca34dd384a9ac7acc37c7c0
CCCCCC.CCn1c(-c2cccc3ccccc23)nc(Cl)c1Cl.COC(=O)OC>>CCOC(=O)c1c(Cl)nc(-c2cccc3ccccc23)n1CC
C(OC)(OC)=O.ClC=1N=C(N(C1Cl)CC)C1=CC=CC2=CC=CC=C12.[Li]CCCC.CCCCCC>>C(C)OC(=O)C=1N(C(=NC1Cl)C1=CC=CC2=CC=CC=C12)CC
CCCCC[CH3:1].Cl[c:6]1[c:7]([Cl:8])[n:9][c:10](-[c:11]2[cH:12][cH:13][cH:14][c:15]3[cH:16][cH:17][cH:18][cH:19][c:20]23)[n:21]1[CH2:22][CH3:23].CO[C:4]([O:3][CH3:2])=[O:5]>>[CH3:1][CH2:2][O:3][C:4](=[O:5])[c:6]1[c:7]([Cl:8])[n:9][c:10](-[c:11]2[cH:12][cH:13][cH:14][c:15]3[cH:16][cH:17][cH:18][cH:19][c:20]23)[n:21]1[CH2:...
CCCCCC.CCn1c(-c2cccc3ccccc23)nc(Cl)c1Cl.COC(=O)OC
CCOC(=O)c1c(Cl)nc(-c2cccc3ccccc23)n1CC
null
null
C1CCOC1.O
C-C Coupling
OtherReaction
5e0dcd9c0f4140fbcb925d05ab74e6631c7d9f4da048ac90751b65562fffc238
bcd3559e95d57605d0e6e7a6ba9cc016318f006dee2eacb538f0c39f9d5391eb
c1ccc2c(-c3ncc[nH]3)cccc2c1
C-C-C-C-C-[CH3;D1;+0:1].C-O-[C;H0;D3;+0:2](=[O;D1;H0:3])-[#8:4]-[CH3;D1;+0:5].Cl-[c;H0;D3;+0:6]1:[#7;a:7](-[C:8]):[c:9](-[c:10]):[#7;a:11]:[c:12]:1-[Cl;D1;H0:13]>>[C:8]-[#7;a:7]1:[c:9](-[c:10]):[#7;a:11]:[c:12](-[Cl;D1;H0:13]):[c;H0;D3;+0:6]:1-[C;H0;D3;+0:2](=[O;D1;H0:3])-[#8:4]-[CH2;D2;+0:5]-[CH3;D1;+0:1]
null
[]
-78
CELSIUS
1
HOUR
To a solution of 4,5-dichloro-1-ethyl-2-naphthalen-1-yl-1H-imidazole (2.87 g, 9.86 mmol) in anhydrous THF (60 ml) at −78° C. under nitrogen is added a solution of n-BuLi in hexane (1.6 M, 6.78 ml, 10.84 mmol, 1.1 eq.) dropwise. The resulting mixture is stirred at −78° C. for 1 hr, followed by the addition of dimethyl c...
10.6084/m9.figshare.5104873.v1
null
Aromatic halide.Carbonic Ester
Ester
c1c[nH]cn1
c1c[nH]cn1
c1c[nH]cn1.c1ccc2ccccc2c1
HCl
C1CCOC1.O
-78
1
CCCCCC.CCn1c(-c2cccc3ccccc23)nc(Cl)c1Cl.COC(=O)OC>C1CCOC1.O>CCOC(=O)c1c(Cl)nc(-c2cccc3ccccc23)n1CC
ord_dataset-03ba810b7f464a06b5d8787af2e8b64e
ord-3784c7b763394a5792a6078a91210fb0
CCOC(=O)c1c(Cl)nc(-c2cccc3ccccc23)n1CC>>CCn1c(-c2cccc3ccccc23)nc(Cl)c1C(=O)O
C1CCOC1.C(C)OC(=O)C=1N(C(=NC1Cl)C1=CC=CC2=CC=CC=C12)CC.C1CCOC1.[OH-].[Li+]>>ClC1=C(N(C(=N1)C1=CC=CC2=CC=CC=C12)CC)C(=O)O
CC[O:21][C:19]([c:18]1[n:3]([CH2:2][CH3:1])[c:4](-[c:5]2[cH:6][cH:7][cH:8][c:9]3[cH:10][cH:11][cH:12][cH:13][c:14]23)[n:15][c:16]1[Cl:17])=[O:20]>>[CH3:1][CH2:2][n:3]1[c:4](-[c:5]2[cH:6][cH:7][cH:8][c:9]3[cH:10][cH:11][cH:12][cH:13][c:14]23)[n:15][c:16]([Cl:17])[c:18]1[C:19](=[O:20])[OH:21]
CCOC(=O)c1c(Cl)nc(-c2cccc3ccccc23)n1CC
CCn1c(-c2cccc3ccccc23)nc(Cl)c1C(=O)O
null
null
O
Deprotection
Ester saponification (alkyl deprotection)
d872e08ad5c85a4add6cd04e6e987e73fead5f79b3f30ba61a81ba5029b29894
38ae1ee78433b9acfb0390501446149c80f88f23ac2d84c60b3369bdab75cec9
c1ccc2c(-c3ncc[nH]3)cccc2c1
C-C-[O;H0;D2;+0:1]-[C:2](=[O;D1;H0:3])-[c:4](:[#7;a:5]):[c:6]:[#7;a:7]>>[#7;a:7]:[c:6]:[c:4](-[C:2](=[O;D1;H0:3])-[OH;D1;+0:1]):[#7;a:5]
null
[]
50
CELSIUS
null
null
5-Chloro-3-ethyl-2-naphthalen-1-yl-3H-imidazole-4-carboxylic acid ethyl ester (62 g, 35 mmol) is dissolved in. THF (10 ml), and aqueous lithium hydroxide solution (2.0 N, 6.35 ml, 2.0 eq.) is added. The mixture is heated at 50° C. overnight. THF is stripped off under reduced pressure, and the residue is diluted with wa...
10.6084/m9.figshare.5104873.v1
null
Ester
Carboxylic acid
null
null
c1c[nH]cn1.c1ccc2ccccc2c1
Other
O
50
null
CCOC(=O)c1c(Cl)nc(-c2cccc3ccccc23)n1CC>O>CCn1c(-c2cccc3ccccc23)nc(Cl)c1C(=O)O
ord_dataset-03ba810b7f464a06b5d8787af2e8b64e
ord-063302fd527f4632a4a26455de7386ac
CCn1c(-c2cccc3ccccc23)nc(Br)c1Br.C[Si](C)(C)Cl.O=S(=O)(c1ccccc1)N(F)S(=O)(=O)c1ccccc1>>CCn1c(-c2cccc3ccccc23)nc(F)c1[Si](C)(C)C
C[Si](C)(C)Cl.C1=CC=C(C=C1)S(=O)(=O)N(F)S(=O)(=O)C2=CC=CC=C2.BrC=1N=C(N(C1Br)CC)C1=CC=CC2=CC=CC=C12.[Li]CCCC.CCCCCC.[Li]CCCC.CCCCCC>>C(C)N1C(=NC(=C1[Si](C)(C)C)F)C1=CC=CC2=CC=CC=C12
Br[c:16]1[n:15][c:4](-[c:5]2[cH:6][cH:7][cH:8][c:9]3[cH:10][cH:11][cH:12][cH:13][c:14]23)[n:3]([CH2:2][CH3:1])[c:18]1Br.Cl[Si:19]([CH3:20])([CH3:21])[CH3:22].O=S(=O)(c1ccccc1)N(S(=O)(=O)c1ccccc1)[F:17]>>[CH3:1][CH2:2][n:3]1[c:4](-[c:5]2[cH:6][cH:7][cH:8][c:9]3[cH:10][cH:11][cH:12][cH:13][c:14]23)[n:15][c:16]([F:17])[c:...
CCn1c(-c2cccc3ccccc23)nc(Br)c1Br.C[Si](C)(C)Cl.O=S(=O)(c1ccccc1)N(F)S(=O)(=O)c1ccccc1
CCn1c(-c2cccc3ccccc23)nc(F)c1[Si](C)(C)C
null
null
C1CCOC1.O
Miscellaneous
OtherReaction
56db6f3ed60a43dd039ce4d859f26cd02b3c839e21378a6dec6daf53b49464c7
7d719443a27bb0f615d6ac749cd29b4ae1c5b5ff710db8479ebd8b00984c881f
c1ccc2c(-c3ncc[nH]3)cccc2c1
Br-[c;H0;D3;+0:1]1:[#7;a:2]:[c:3](-[c:4]):[#7;a:5](-[C:6]):[c;H0;D3;+0:7]:1-Br.Cl-[Si;H0;D4;+0:8](-[C;D1;H3:9])(-[C;D1;H3:10])-[C;D1;H3:11].O=S(=O)(-N(-[F;H0;D1;+0:12])-S(=O)(=O)-c1:c:c:c:c:c:1)-c1:c:c:c:c:c:1>>[C:6]-[#7;a:5]1:[c:3](-[c:4]):[#7;a:2]:[c;H0;D3;+0:1](-[F;H0;D1;+0:12]):[c;H0;D3;+0:7]:1-[Si;H0;D4;+0:8](-[C;...
null
[]
-78
CELSIUS
1
HOUR
To a solution of 4,5-dibromo-1-ethyl-2-naphthalen-1-yl-1H-imidazole (6.55 g, 17.2 mmol) in anhydrous THF (150 ml) at −78° C. under nitrogen is added a solution of n-BuLi in hexane (1.6 M, 11.8 ml, 19 mmol, 1.1 eq.) dropwise. The resulting mixture is stirred at −78° C. for 1 hr, and TMSCl (2.05 g, 19 mmol, 1.1 eq.) is a...
10.6084/m9.figshare.5104873.v1
null
Aromatic halide.Aromatic halide.Tertiary amine.Silyl protective group
Aromatic halide.Silyl protective group
c1c[nH]cn1.c1ccccc1.c1ccccc1
c1c[nH]cn1
c1c[nH]cn1.c1ccc2ccccc2c1
HCl.Br-
C1CCOC1.O
-78
1
CCn1c(-c2cccc3ccccc23)nc(Br)c1Br.C[Si](C)(C)Cl.O=S(=O)(c1ccccc1)N(F)S(=O)(=O)c1ccccc1>C1CCOC1.O>CCn1c(-c2cccc3ccccc23)nc(F)c1[Si](C)(C)C
ord_dataset-03ba810b7f464a06b5d8787af2e8b64e
ord-a55c86c65da04b15a979060a6498a635
CCn1c(-c2cccc3ccccc23)nc(F)c1[Si](C)(C)C>>CCn1cc(F)nc1-c1cccc2ccccc12
C(C)N1C(=NC(=C1[Si](C)(C)C)F)C1=CC=CC2=CC=CC=C12.O.[F-].C(CCC)[N+](CCCC)(CCCC)CCCC>>C(C)N1C(=NC(=C1)F)C1=CC=CC2=CC=CC=C12
C[Si](C)(C)[c:4]1[n:3]([CH2:2][CH3:1])[c:8](-[c:9]2[cH:10][cH:11][cH:12][c:13]3[cH:14][cH:15][cH:16][cH:17][c:18]23)[n:7][c:5]1[F:6]>>[CH3:1][CH2:2][n:3]1[cH:4][c:5]([F:6])[n:7][c:8]1-[c:9]1[cH:10][cH:11][cH:12][c:13]2[cH:14][cH:15][cH:16][cH:17][c:18]12
CCn1c(-c2cccc3ccccc23)nc(F)c1[Si](C)(C)C
CCn1cc(F)nc1-c1cccc2ccccc12
null
null
C1CCOC1
Miscellaneous
OtherReaction
c7f462886971c9302390ac232c55147304002681edbc6aa0690a17b1d7b7af67
dc52a720480da1d65217db7d5178c684d09e72e99cbbe1f9f67cca818c9ff2e9
c1ccc2c(-c3ncc[nH]3)cccc2c1
C-[Si](-C)(-C)-[c;H0;D3;+0:1]1:[#7;a:2](-[C:3]):[c:4]:[#7;a:5]:[c:6]:1-[F;D1;H0:7]>>[C:3]-[#7;a:2]1:[c:4]:[#7;a:5]:[c:6](-[F;D1;H0:7]):[cH;D2;+0:1]:1
null
[]
null
null
4
HOUR
Crude 1-ethyl-4-fluoro-2-naphthalen-1-yl-5-trimethylsilanyl-1H-imidazole (5.49 g) is dissolved in THF (75 ml), and to the solution is added tetrabutylammonium fluoride hydrate (5.4 g, 20.6 mmol, 1.2 eq.). The resulting mixture is stirred at rt for 4 hr. The organic solvent is evaporated under reduced pressure, and the ...
10.6084/m9.figshare.5104873.v1
null
Silyl protective group
null
c1c[nH]cn1
c1c[nH]cn1
c1c[nH]cn1.c1ccc2ccccc2c1
Other
C1CCOC1
null
4
CCn1c(-c2cccc3ccccc23)nc(F)c1[Si](C)(C)C>C1CCOC1>CCn1cc(F)nc1-c1cccc2ccccc12
ord_dataset-03ba810b7f464a06b5d8787af2e8b64e
ord-3f58c3e8254649fcb1cc5fa9783b5209
CC#N.CCOC(=O)C(=O)C(C)=O.NCc1cccc2ccccc12>>CCOC(=O)c1[nH]c(-c2cccc3ccccc23)nc1C
C(C)OC(C(C(C)=O)=O)=O.C1(=CC=CC2=CC=CC=C12)CN.C(C)#N>>C(C)OC(=O)C=1NC(=NC1C)C1=CC=CC2=CC=CC=C12
CC#[N:19].O=[C:6]([C:4]([O:3][CH2:2][CH3:1])=[O:5])[C:20](=O)[CH3:21].[NH2:7][CH2:8][c:9]1[cH:10][cH:11][cH:12][c:13]2[cH:14][cH:15][cH:16][cH:17][c:18]12>>[CH3:1][CH2:2][O:3][C:4](=[O:5])[c:6]1[nH:7][c:8](-[c:9]2[cH:10][cH:11][cH:12][c:13]3[cH:14][cH:15][cH:16][cH:17][c:18]23)[n:19][c:20]1[CH3:21]
CC#N.CCOC(=O)C(=O)C(C)=O.NCc1cccc2ccccc12
CCOC(=O)c1[nH]c(-c2cccc3ccccc23)nc1C
null
null
null
Aromatic Heterocycle Formation
OtherReaction
aa158c8d7e0a34e08a94bd0c9bf6ae44273956195bd167763fe3fbf92c70be90
3ac027b3c2941a6ffc7e285e96b5051b88c786e5ee70393eaeeba59628125919
c1ccc2c(-c3ncc[nH]3)cccc2c1
C-C#[N;H0;D1;+0:1].O=[C;H0;D3;+0:2](-[C;D1;H3:3])-[C;H0;D3;+0:4](=O)-[C:5](=[O;D1;H0:6])-[#8:7]-[C:8].[NH2;D1;+0:9]-[CH2;D2;+0:10]-[c;H0;D3;+0:11](:[c:12]:[c:13]):[c:14](:[c:15]):[c:16]>>[C:8]-[#8:7]-[C:5](=[O;D1;H0:6])-[c;H0;D3;+0:4]1:[nH;D2;+0:9]:[c;H0;D3;+0:10](-[c;H0;D3;+0:11](:[c:12]:[c:13]):[c:14](:[c:15]):[c:16]...
null
[]
null
null
null
null
A solution of 2,3-dioxobutyric acid ethyl ester, (Z)-2-oxime (3 g), 1-naphthalenemethylamine (3.26 g) in acetonitrile (45 ml) is refluxed for 10 hr to give a white precipitate. The solid is then collected, washed with acetonitrile and dried to yield 5-methyl-2-naphthalen-1-yl-3H-imidazole-4-carboxylic acid ethyl ester....
10.6084/m9.figshare.5104873.v1
null
Ketone.Ketone.Ester.Nitrile.Primary amine
Ester
null
c1c[nH]cn1
c1c[nH]cn1.c1ccc2ccccc2c1
HO-
null
null
null
CC#N.CCOC(=O)C(=O)C(C)=O.NCc1cccc2ccccc12>>CCOC(=O)c1[nH]c(-c2cccc3ccccc23)nc1C
ord_dataset-03ba810b7f464a06b5d8787af2e8b64e
ord-3f60c457229c49a889b0212e15c53cb0
CCOC(=O)c1[nH]c(-c2cccc3ccccc23)nc1C>>Cc1nc(-c2cccc3ccccc23)[nH]c1CO
C(C)OC(=O)C=1NC(=NC1C)C1=CC=CC2=CC=CC=C12.CC(C)C[AlH]CC(C)C>>CC1=C(NC(=N1)C1=CC=CC2=CC=CC=C12)CO
CCO[C:17]([c:16]1[c:2]([CH3:1])[n:3][c:4](-[c:5]2[cH:6][cH:7][cH:8][c:9]3[cH:10][cH:11][cH:12][cH:13][c:14]23)[nH:15]1)=[O:18]>>[CH3:1][c:2]1[n:3][c:4](-[c:5]2[cH:6][cH:7][cH:8][c:9]3[cH:10][cH:11][cH:12][cH:13][c:14]23)[nH:15][c:16]1[CH2:17][OH:18]
CCOC(=O)c1[nH]c(-c2cccc3ccccc23)nc1C
Cc1nc(-c2cccc3ccccc23)[nH]c1CO
null
null
C1CCOC1
Reduction
Reduction of ester to primary alcohol
21d61543c6ec8a8cebe1b3ef55ef3dd20acbf79a4f1c12a7fb51e32be7a3248a
1fbcd628a0426673c5d10aa49a977cd2d1ae02a8cdf57bbb10d94aa03a94e937
c1ccc2c(-c3ncc[nH]3)cccc2c1
C-C-O-[C;H0;D3;+0:1](=[O;H0;D1;+0:2])-[c:3]1:[#7;a:4]:[c:5]:[#7;a:6]:[c:7]:1-[C;D1;H3:8]>>[C;D1;H3:8]-[c:7]1:[#7;a:6]:[c:5]:[#7;a:4]:[c:3]:1-[CH2;D2;+0:1]-[OH;D1;+0:2]
null
[]
null
null
2
HOUR
To a solution of 5-methyl-2-naphthalen-1-yl-3H-imidazole-4-carboxylic acid ethyl ester (280 mg) in THF (8 ml) is added DIBAL-H (3.3 ml, 1.5 M in toluene) at 0° C. The resulting solution is stirred at rt for 2 hr, and quenched with brine. The THF layer is separated and then evaporated. The residue is dissolved in EtOAc,...
10.6084/m9.figshare.5104873.v1
null
Ester
Primary alcohol
null
null
c1c[nH]cn1.c1ccc2ccccc2c1
HO-
C1CCOC1
null
2
CCOC(=O)c1[nH]c(-c2cccc3ccccc23)nc1C>C1CCOC1>Cc1nc(-c2cccc3ccccc23)[nH]c1CO
ord_dataset-03ba810b7f464a06b5d8787af2e8b64e
ord-ac11358a2b184d57b7b7919456a8a1dc
C1CCC(N2CCNCC2)C1.Cc1nc(-c2cccc3ccccc23)[nH]c1CO>>Cc1nc(-c2cccc3ccccc23)[nH]c1CN1CCN(C2CCCC2)CC1
CCN(CC)CC.CC1=C(NC(=N1)C1=CC=CC2=CC=CC=C12)CO.O=S(Cl)Cl.C1(CCCC1)N1CCNCC1>>C1(CCCC1)N1CCN(CC1)CC=1NC(=NC1C)C1=CC=CC2=CC=CC=C12
[NH:18]1[CH2:19][CH2:20][N:21]([CH:22]2[CH2:23][CH2:24][CH2:25][CH2:26]2)[CH2:27][CH2:28]1.O[CH2:17][c:16]1[c:2]([CH3:1])[n:3][c:4](-[c:5]2[cH:6][cH:7][cH:8][c:9]3[cH:10][cH:11][cH:12][cH:13][c:14]23)[nH:15]1>>[CH3:1][c:2]1[n:3][c:4](-[c:5]2[cH:6][cH:7][cH:8][c:9]3[cH:10][cH:11][cH:12][cH:13][c:14]23)[nH:15][c:16]1[CH2...
C1CCC(N2CCNCC2)C1.Cc1nc(-c2cccc3ccccc23)[nH]c1CO
Cc1nc(-c2cccc3ccccc23)[nH]c1CN1CCN(C2CCCC2)CC1
null
null
C(Cl)Cl
Heteroatom Alkylation and Arylation
OtherReaction
9885b3f1c049b08208f7467939360b5e493f0f916b8555f394ab4272f7b37bd7
87693a475e46c41583976158ec46dcaf8be8cc05c5635654a6a68033770f8d5c
c1ccc2c(-c3ncc(CN4CCN(C5CCCC5)CC4)[nH]3)cccc2c1
O-[CH2;D2;+0:1]-[c:2]1:[#7;a:3]:[c:4]:[#7;a:5]:[c:6]:1-[C;D1;H3:7].[#7:8]1-[C:9]-[C:10]-[NH;D2;+0:11]-[C:12]-[C:13]-1>>[C;D1;H3:7]-[c:6]1:[#7;a:5]:[c:4]:[#7;a:3]:[c:2]:1-[CH2;D2;+0:1]-[N;H0;D3;+0:11]1-[C:10]-[C:9]-[#7:8]-[C:13]-[C:12]-1
null
[]
null
null
null
null
(5-Methyl-2-naphthalen-1-yl-3H-imidazol-4-yl)-methanol (40 mg) is treated with SOCl2, followed by N-cyclopentylpiperazine (60 mg) and Et3N (0.04 ml) in CH2Cl2 (2 ml). The crude is purified by column (2% Et3N, 3% MeOH in EtOAc) to afford the title compound as a white solid. LCMS 375.5 (M+1). Conditions: See reaction.not...
10.6084/m9.figshare.5104873.v1
null
Primary alcohol.Secondary amine
Tertiary amine
C1CNCC[NH]1
C1C[NH]CC[NH]1
c1c[nH]cn1.c1ccc2ccccc2c1.C1C[NH]CC[NH]1.C1CCCC1
HO-
C(Cl)Cl
null
null
C1CCC(N2CCNCC2)C1.Cc1nc(-c2cccc3ccccc23)[nH]c1CO>C(Cl)Cl>Cc1nc(-c2cccc3ccccc23)[nH]c1CN1CCN(C2CCCC2)CC1
ord_dataset-03ba810b7f464a06b5d8787af2e8b64e
ord-6865d417dc3a4acbabe299198449a15e
CCI.CCOC(=O)c1[nH]c(-c2cccc3ccccc23)nc1C.O>>CCOC(=O)c1c(C)nc(-c2cccc3ccccc23)n1CC.CCOC(=O)c1nc(-c2cccc3ccccc23)n(CC)c1C
C(C)I.C(C)OC(=O)C=1NC(=NC1C)C1=CC=CC2=CC=CC=C12.[H-].[Na+].O>>C(C)OC(=O)C=1N(C(=NC1C)C1=CC=CC2=CC=CC=C12)CC.C(C)OC(=O)C=1N=C(N(C1C)CC)C1=CC=CC2=CC=CC=C12
I[CH2:22][CH3:23].[CH3:1][CH2:25][O:26][C:4](=[O:5])[c:6]1[c:7]([CH3:8])[n:9][c:10](-[c:11]2[cH:12][cH:13][cH:14][c:15]3[cH:16][cH:17][cH:18][cH:19][c:20]23)[nH:21]1.[OH2:3]>>[CH3:1][CH2:2][O:3][C:4](=[O:5])[c:6]1[c:7]([CH3:8])[n:9][c:10](-[c:11]2[cH:12][cH:13][cH:14][c:15]3[cH:16][cH:17][cH:18][cH:19][c:20]23)[n:21]1[...
CCI.CCOC(=O)c1[nH]c(-c2cccc3ccccc23)nc1C.O
CCOC(=O)c1c(C)nc(-c2cccc3ccccc23)n1CC.CCOC(=O)c1nc(-c2cccc3ccccc23)n(CC)c1C
null
null
CN(C)C=O
Aromatic Heterocycle Formation
OtherReaction
fc841b26e548053e0d0e23943f09005afbfa63cd82f2972d15d4541f514a0f9c
e4b1221eb59b6018d91e0913178985938131414a8c03bce5dfcc4f56490914f5
c1ccc2c(-c3ncc[nH]3)cccc2c1.c1ccc2c(-c3ncc[nH]3)cccc2c1
I-[CH2;D2;+0:1]-[C;D1;H3:2].[C;D1;H3:3]-[c:4]1:[#7;a:5]:[c:6](-[c:7]):[nH;D2;+0:8]:[c:9]:1-[C;H0;D3;+0:10](=[O;D1;H0:11])-[O;H0;D2;+0:12]-[CH2;D2;+0:13]-[CH3;D1;+0:14].[OH2;D0;+0:15]>>[C;D1;H3:16]-[CH2;D2;+0:13]-[O;H0;D2;+0:12]-[C:17](=[O;D1;H0:18])-[c:19].[C;D1;H3:2]-[CH2;D2;+0:1]-[n;H0;D3;+0:8]1:[c:6](-[c:7]):[#7;a:5...
null
[]
0
CELSIUS
30
MINUTE
To a solution of 5-methyl-2-naphthalen-1-yl-3H-imidazole-4-carboxylic acid ethyl ester (1.5 g) in DMF (30 ml) is added NaH (320 mg, 60%) at rt. The solution is stirred for 30 min, and EtI (0.6 ml) is added. After 30 min, the mixture is cooled to 0° C. and H2O is added. The mixture is then extracted with EtOAc. The extr...
10.6084/m9.figshare.5104873.v1
null
Primary halide.Ester
Ester.Ester
c1c[nH]cn1
c1c[nH]cn1.c1c[nH]cn1.c1ccc2ccccc2c1
c1c[nH]cn1.c1ccc2ccccc2c1.c1c[nH]cn1.c1ccc2ccccc2c1
I-
CN(C)C=O
0
0.5
CCI.CCOC(=O)c1[nH]c(-c2cccc3ccccc23)nc1C.O>CN(C)C=O>CCOC(=O)c1c(C)nc(-c2cccc3ccccc23)n1CC.CCOC(=O)c1nc(-c2cccc3ccccc23)n(CC)c1C
ord_dataset-03ba810b7f464a06b5d8787af2e8b64e
ord-80481d022c79468f9dd37c5cace1fcb4
CCn1c(-c2cccc3ccccc23)nc(C)c1C(=O)N1CCN(C2CCC2)CC1>>CCn1c(-c2cccc3ccccc23)nc(C)c1CN1CCN(C2CCC2)CC1
C1(CCC1)N1CCN(CC1)C(=O)C=1N(C(=NC1C)C1=CC=CC2=CC=CC=C12)CC.CC(C)C[AlH]CC(C)C>>C1(CCC1)N1CCN(CC1)CC=1N(C(=NC1C)C1=CC=CC2=CC=CC=C12)CC
O=[C:19]([c:18]1[n:3]([CH2:2][CH3:1])[c:4](-[c:5]2[cH:6][cH:7][cH:8][c:9]3[cH:10][cH:11][cH:12][cH:13][c:14]23)[n:15][c:16]1[CH3:17])[N:20]1[CH2:21][CH2:22][N:23]([CH:24]2[CH2:25][CH2:26][CH2:27]2)[CH2:28][CH2:29]1>>[CH3:1][CH2:2][n:3]1[c:4](-[c:5]2[cH:6][cH:7][cH:8][c:9]3[cH:10][cH:11][cH:12][cH:13][c:14]23)[n:15][c:1...
CCn1c(-c2cccc3ccccc23)nc(C)c1C(=O)N1CCN(C2CCC2)CC1
CCn1c(-c2cccc3ccccc23)nc(C)c1CN1CCN(C2CCC2)CC1
null
null
C1CCOC1
Reduction
Reduction of tertiary amides to amines
f74c5a050b269ec4da3871c266f01344b7447381f47cda744f8b1e9c225ae62d
c8f3c617792f7a4fae96b8a97dc0ce23461ab85d8a738fe6caacff776ef51ffa
c1ccc2c(-c3ncc(CN4CCN(C5CCC5)CC4)[nH]3)cccc2c1
O=[C;H0;D3;+0:1](-[#7:2](-[C:3])-[C:4])-[c:5]1:[#7;a:6](-[C:7]):[c:8]:[#7;a:9]:[c:10]:1-[C;D1;H3:11]>>[C:3]-[#7:2](-[CH2;D2;+0:1]-[c:5]1:[#7;a:6](-[C:7]):[c:8]:[#7;a:9]:[c:10]:1-[C;D1;H3:11])-[C:4]
null
[]
null
null
2
HOUR
To a solution of (4-cyclobutyl-piperazin-1-yl)-(3-ethyl-5-methyl-2-naphthalen-1-yl-3H-imidazol-4-yl)-methanone (40 mg) in THF (1 ml) is added DIBAL-H (0.25 ml, 1.5 M in toluene) at 0° C. The resulting solution is stirred at rt for 2 hr, and then quenched with brine. The THF layer is separated, evaporated and purified b...
10.6084/m9.figshare.5104873.v1
null
Tertiary amide
null
null
null
c1c[nH]cn1.c1ccc2ccccc2c1.C1C[NH]CC[NH]1.C1CCC1
Other
C1CCOC1
null
2
CCn1c(-c2cccc3ccccc23)nc(C)c1C(=O)N1CCN(C2CCC2)CC1>C1CCOC1>CCn1c(-c2cccc3ccccc23)nc(C)c1CN1CCN(C2CCC2)CC1
ord_dataset-03ba810b7f464a06b5d8787af2e8b64e
ord-49b7772e7ec2441798f0cd7657c64a6c
CCn1cc(C(O)C2CCNCC2)nc1-c1cccc2ccccc12.O=C1CCC1>>CCn1cc(C(O)C2CCN(C3CCC3)CC2)nc1-c1cccc2ccccc12
C(C)(=O)O.[BH-](OC(=O)C)(OC(=O)C)OC(=O)C.[Na+].C(C)N1C(=NC(=C1)C(O)C1CCNCC1)C1=CC=CC2=CC=CC=C12.C1(CCC1)=O>>C1(CCC1)N1CCC(CC1)C(O)C=1N=C(N(C1)CC)C1=CC=CC2=CC=CC=C12
[CH3:1][CH2:2][n:3]1[cH:4][c:5]([CH:6]([OH:7])[CH:8]2[CH2:9][CH2:10][NH:11][CH2:16][CH2:17]2)[n:18][c:19]1-[c:20]1[cH:21][cH:22][cH:23][c:24]2[cH:25][cH:26][cH:27][cH:28][c:29]12.O=[C:12]1[CH2:13][CH2:14][CH2:15]1>>[CH3:1][CH2:2][n:3]1[cH:4][c:5]([CH:6]([OH:7])[CH:8]2[CH2:9][CH2:10][N:11]([CH:12]3[CH2:13][CH2:14][CH2:1...
CCn1cc(C(O)C2CCNCC2)nc1-c1cccc2ccccc12.O=C1CCC1
CCn1cc(C(O)C2CCN(C3CCC3)CC2)nc1-c1cccc2ccccc12
null
null
C(Cl)Cl
Heteroatom Alkylation and Arylation
reductive amination
4beccb96faa28d88380728f020be13ff3debe8152a8220a924c88cfbe909e1b6
99acf13bfcfe579f51ccb82c65e4ca039ee7ca9b6fcd2747a3d9a292a88e564e
c1ccc2c(-c3nc(CC4CCN(C5CCC5)CC4)c[nH]3)cccc2c1
O=[C;H0;D3;+0:1]1-[C:2]-[C:3]-[C:4]-1.[C:5]-[C:6]-[NH;D2;+0:7]-[C:8]-[C:9]>>[C:5]-[C:6]-[N;H0;D3;+0:7](-[CH;D3;+0:1]1-[C:2]-[C:3]-[C:4]-1)-[C:8]-[C:9]
null
[]
null
null
8
HOUR
To a solution of (1-ethyl-2-naphthalen-1-yl-1H-imidazol-4-yl)-piperidin-4-yl-methanol (0.53 g) in CH2ClCH2Cl (12 ml) is added cyclobutanone (0.95 ml), followed by NaBH(OAc)3 and acetic acid (0.1 ml). The resulting mixture is stirred at rt overnight, diluted with CH2Cl2, washed with Na2CO3 (1M), H2O and brine, dried and...
10.6084/m9.figshare.5104873.v1
null
Ketone.Secondary amine
Tertiary amine
C1CCNCC1.C1CCC1
C1CC[NH]CC1.C1CCC1
c1c[nH]cn1.C1CC[NH]CC1.C1CCC1.c1ccc2ccccc2c1
Other
C(Cl)Cl
null
8
CCn1cc(C(O)C2CCNCC2)nc1-c1cccc2ccccc12.O=C1CCC1>C(Cl)Cl>CCn1cc(C(O)C2CCN(C3CCC3)CC2)nc1-c1cccc2ccccc12
ord_dataset-03ba810b7f464a06b5d8787af2e8b64e
ord-996368e539504cb7806c1a8a3ac7055d
CCn1cc(C(O)C2CCN(C3CCC3)CC2)nc1-c1cccc2ccccc12.CI>>CCn1cc(C(OC)C2CCN(C3CCC3)CC2)nc1-c1cccc2ccccc12
CI.C1(CCC1)N1CCC(CC1)C(O)C=1N=C(N(C1)CC)C1=CC=CC2=CC=CC=C12.[H-].[Na+]>>C1(CCC1)N1CCC(CC1)C(OC)C=1N=C(N(C1)CC)C1=CC=CC2=CC=CC=C12
[CH3:1][CH2:2][n:3]1[cH:4][c:5]([CH:6]([OH:7])[CH:9]2[CH2:10][CH2:11][N:12]([CH:13]3[CH2:14][CH2:15][CH2:16]3)[CH2:17][CH2:18]2)[n:19][c:20]1-[c:21]1[cH:22][cH:23][cH:24][c:25]2[cH:26][cH:27][cH:28][cH:29][c:30]12.I[CH3:8]>>[CH3:1][CH2:2][n:3]1[cH:4][c:5]([CH:6]([O:7][CH3:8])[CH:9]2[CH2:10][CH2:11][N:12]([CH:13]3[CH2:1...
CCn1cc(C(O)C2CCN(C3CCC3)CC2)nc1-c1cccc2ccccc12.CI
CCn1cc(C(OC)C2CCN(C3CCC3)CC2)nc1-c1cccc2ccccc12
null
null
CCOC(=O)C.CN(C)C=O
Heteroatom Alkylation and Arylation
Williamson Ether Synthesis
31ec8f945a35f4f87287620e27b68692ce42732551035fbac056df61d9acce14
08f7221cae607d413f579138dcaa6997bebcad2bbb42d2f1b3b2a2d886befb37
c1ccc2c(-c3nc(CC4CCN(C5CCC5)CC4)c[nH]3)cccc2c1
I-[CH3;D1;+0:1].[#7;a:2]:[c:3](-[C:4](-[C:5])-[OH;D1;+0:6]):[c:7]:[#7;a:8]>>[#7;a:2]:[c:3](-[C:4](-[C:5])-[O;H0;D2;+0:6]-[CH3;D1;+0:1]):[c:7]:[#7;a:8]
null
[]
null
null
30
MINUTE
To a solution of (1-cyclobutyl-piperidin-4-yl)-(1-ethyl-2-naphthalen-1-yl-1H-imidazol-4-yl)-methanol (20 mg) in DMF (2 ml) is added NaH (6 mg, 60%), followed by CH3I (15 mg). The resulting mixture is stirred at rt for 30 min, and then diluted with EtOAc, washed with water and brine, dried and solvent removed. The crude...
10.6084/m9.figshare.5104873.v1
null
Secondary alcohol
Ether
null
null
c1c[nH]cn1.C1CC[NH]CC1.C1CCC1.c1ccc2ccccc2c1
HI
CCOC(=O)C.CN(C)C=O
null
0.5
CCn1cc(C(O)C2CCN(C3CCC3)CC2)nc1-c1cccc2ccccc12.CI>CCOC(=O)C.CN(C)C=O>CCn1cc(C(OC)C2CCN(C3CCC3)CC2)nc1-c1cccc2ccccc12
ord_dataset-03ba810b7f464a06b5d8787af2e8b64e
ord-70c666ce7b4a4ede94971688eaf95325
CCI.N#CCC#N>>CCC(C#N)(C#N)CC
CC(C)(C)[O-].[K+].C(CC#N)#N.C(C)I>>C(C)C(C#N)(C#N)CC
I[CH2:2][CH3:1].[CH2:3]([C:4]#[N:5])[C:8]#[N:7]>>[CH3:1][CH2:2][C:3]([C:4]#[N:5])([C:6]#[N:7])[CH2:8][CH3:9]
CCI.N#CCC#N
CCC(C#N)(C#N)CC
null
CCCC[N+](CCCC)(CCCC)CCCC.[Br-]
null
C-C Coupling
OtherReaction
beef5228fcaf3ca6d461603efc4c90a139b5ff1639f3130cb134016aa21deb02
cfd1a6601301109b513394252983fd8657e1a8ade5f928a44f205d21f84af183
null
I-[CH2;D2;+0:1]-[C;D1;H3:2].[N;D1;H0:3]#[C:4]-[CH2;D2;+0:5]-[C;H0;D2;+0:6]#[N;H0;D1;+0:7]>>[C;D1;H3:2]-[CH2;D2;+0:1]-[C;H0;D4;+0:5](-[C:4]#[N;D1;H0:3])(-[C:8]#[N;H0;D1;+0:7])-[CH2;D2;+0:6]-[C;D1;H3:9]
null
[]
null
null
30
MINUTE
Malononitrile (15.2 g) was mixed with TBAB (3.0 g, 4 mol %) and ethyl iodide (36.8 mL, 2 equiv.). After stirring for 30 minutes at room temperature, the mixture was cooled in an ice bath, KOtBu (51.6 g, 2 equiv.) was added portionwise, the ice bath was removed, and the mixture was stirred for 30 minutes at room tempera...
10.6084/m9.figshare.5104873.v1
null
Primary halide.Nitrile
Nitrile
null
null
null
I-
CCCC[N+](CCCC)(CCCC)CCCC.[Br-]
null
0.5
CCI.N#CCC#N>CCCC[N+](CCCC)(CCCC)CCCC.[Br-]>CCC(C#N)(C#N)CC
ord_dataset-03ba810b7f464a06b5d8787af2e8b64e
ord-0f8d79ba1d9c4f4d8cc4deb72e397bf0
CCC(C#N)(C#N)CC>>CCC(CC)(CN)CN
[H-].[H-].[H-].[H-].[Li+].[Al+3].C(C)C(C#N)(C#N)CC>>C(C)C(CN)(CN)CC
[CH3:1][CH2:2][C:3]([CH2:4][CH3:5])([C:6]#[N:7])[C:8]#[N:9]>>[CH3:1][CH2:2][C:3]([CH2:4][CH3:5])([CH2:6][NH2:7])[CH2:8][NH2:9]
CCC(C#N)(C#N)CC
CCC(CC)(CN)CN
null
null
CCOCC
Reduction
OtherReaction
c2340da2c258bf397d4a8fa28e5be42ecf34d1d4e5e541c0aa9e06499bdba3ed
cb8a07357b502aa07f8272954f5a9149eabfa75b76e8c8c18ad60272c8d4f167
null
[C:1]-[C:2](-[C:3])(-[C;H0;D2;+0:4]#[N;H0;D1;+0:5])-[C;H0;D2;+0:6]#[N;H0;D1;+0:7]>>[C:1]-[C:2](-[C:3])(-[CH2;D2;+0:4]-[NH2;D1;+0:5])-[CH2;D2;+0:6]-[NH2;D1;+0:7]
null
[]
null
null
8
HOUR
A suspension of LiAlH4 (4.66 g) in dry Et2O (100 mL) was cooled in an ice bath, and a solution of 2,2-diethyl-malononitrile (5.0 g) in Et2O (50 mL) was added dropwise at such a rate that the temperature was kept below 20° C. The mixture was stirred overnight at room temperature, cooled in an ice bath, and quenched by a...
10.6084/m9.figshare.5104873.v1
null
Nitrile.Nitrile
Primary amine.Primary amine
null
null
null
null
CCOCC
null
8
CCC(C#N)(C#N)CC>CCOCC>CCC(CC)(CN)CN
ord_dataset-03ba810b7f464a06b5d8787af2e8b64e
ord-e38ddba0bf6b4ab48ea0622ffafd9638
CCC(CC)(CN)CN>>CCC1(CC)CN=NC1
C(C)C(CN)(CN)CC.OO.[O-]Cl.[Na+]>>C(C)C1(CN=NC1)CC
[CH3:1][CH2:2][C:3]([CH2:4][CH3:5])([CH2:6][NH2:7])[CH2:9][NH2:8]>>[CH3:1][CH2:2][C:3]1([CH2:4][CH3:5])[CH2:6][N:7]=[N:8][CH2:9]1
CCC(CC)(CN)CN
CCC1(CC)CN=NC1
null
null
CO.O
Oxidation
OtherReaction
da36b35276a0176b37cc03b309f4fbef7c307ef1eae406084866f9301abaa71c
ccb08cdd906ab1c43b965b3f381a9df42e8b4b6ec4217dac787b89befda7069c
C1CN=NC1
[NH2;D1;+0:1]-[C:2]-[C:3]-[C:4]-[NH2;D1;+0:5]>>[C:3]1-[C:2]-[N;H0;D2;+0:1]=[N;H0;D2;+0:5]-[C:4]-1
77
[{"value": 77.0, "product": "C(C)C1(CN=NC1)CC", "details": "PERCENTYIELD", "is_desired": false}]
null
null
2
HOUR
2,2-Diethyl-propane-1,3-diamine (5.0 g) was taken up in a mixture of H2O (40 mL) and MeOH (10 mL), and cooled in an ice bath. Simultaneously, H2O2 (24.2 mL of a 30% solution, 6 equiv.) and NaClO (54.9 mL of a 10% solution, 2.4 equiv.) were added dropwise, the ice bath was removed, and the mixture was stirred for 2 h. a...
10.6084/m9.figshare.5104873.v1
null
Primary amine.Primary amine
Diazene
null
C1CN=NC1
C1CN=NC1
null
CO.O
null
2
CCC(CC)(CN)CN>CO.O>CCC1(CC)CN=NC1
ord_dataset-03ba810b7f464a06b5d8787af2e8b64e
ord-00f2e267ad9c482b927013f0e68e637b
BrCCCCBr.N#CCC#N>>N#CC1(C#N)CCCC1
C(CC#N)#N.C1CCC2=NCCCN2CC1.BrCCCCBr>>C1(CCCC1)(C#N)C#N
Br[CH2:6][CH2:7][CH2:8][CH2:9]Br.[N:1]#[C:2][CH2:3][C:4]#[N:5]>>[N:1]#[C:2][C:3]1([C:4]#[N:5])[CH2:6][CH2:7][CH2:8][CH2:9]1
BrCCCCBr.N#CCC#N
N#CC1(C#N)CCCC1
null
null
CN(C)C=O
C-C Coupling
OtherReaction
90ff2cdd2efc3b7e3d5fddf28ea72ab16385a91dc99fbace2077f543bebdb44a
7b68950fc1047c59bb49c25e850f5a51cbe91a99bb87839c4547aec123110e4b
C1CCCC1
Br-[CH2;D2;+0:1]-[C:2]-[C:3]-[CH2;D2;+0:4]-Br.[N;D1;H0:5]#[C:6]-[CH2;D2;+0:7]-[C:8]#[N;D1;H0:9]>>[N;D1;H0:5]#[C:6]-[C;H0;D4;+0:7]1(-[C:8]#[N;D1;H0:9])-[CH2;D2;+0:1]-[C:2]-[C:3]-[CH2;D2;+0:4]-1
null
[]
80
CELSIUS
2
HOUR
Malononitrile (15.0 g) was dissolved in dry DMF (200 mL) and cooled in an ice bath. Subsequently, DBU (75 mL, 2.2. equiv.) and 1,4-dibromobutane (29.6 mL, 1.1 equiv.) were added dropwise. The ice bath was removed, an extra 100 mL of dry DMF was added, and the mixture was stirred at 80° C. for 2 h. After cooling to ambi...
10.6084/m9.figshare.5104873.v1
null
Primary halide.Primary halide
null
null
C1CCCC1
C1CCCC1
HBr
CN(C)C=O
80
2
BrCCCCBr.N#CCC#N>CN(C)C=O>N#CC1(C#N)CCCC1
ord_dataset-03ba810b7f464a06b5d8787af2e8b64e
ord-1fe459bff36d43cdb7b880e57236a9c8
N#CC1(C#N)CCCC1>>NCC1(CN)CCCC1
[H-].[H-].[H-].[H-].[Li+].[Al+3].C1(CCCC1)(C#N)C#N>>NCC1(CCCC1)CN
[N:1]#[C:2][C:3]1([C:4]#[N:5])[CH2:6][CH2:7][CH2:8][CH2:9]1>>[NH2:1][CH2:2][C:3]1([CH2:4][NH2:5])[CH2:6][CH2:7][CH2:8][CH2:9]1
N#CC1(C#N)CCCC1
NCC1(CN)CCCC1
null
null
CCOCC
Reduction
OtherReaction
c2340da2c258bf397d4a8fa28e5be42ecf34d1d4e5e541c0aa9e06499bdba3ed
cb8a07357b502aa07f8272954f5a9149eabfa75b76e8c8c18ad60272c8d4f167
C1CCCC1
[C:1]-[C:2](-[C;H0;D2;+0:3]#[N;H0;D1;+0:4])(-[C;H0;D2;+0:5]#[N;H0;D1;+0:6])-[C:7]>>[C:1]-[C:2](-[CH2;D2;+0:3]-[NH2;D1;+0:4])(-[CH2;D2;+0:5]-[NH2;D1;+0:6])-[C:7]
null
[]
null
null
8
HOUR
A suspension of LiAlH4 (4.74 g) in dry Et2O (100 mL) was cooled in an ice bath, and a solution of cyclopentane-1,1-dicarbonitrile (5.0 g) in Et2O (50 mL) was added dropwise at such a rate that the temperature was kept below 20° C. The mixture was stirred overnight at room temperature, cooled in an ice bath, and quenche...
10.6084/m9.figshare.5104873.v1
null
Nitrile.Nitrile
Primary amine.Primary amine
null
null
C1CCCC1
null
CCOCC
null
8
N#CC1(C#N)CCCC1>CCOCC>NCC1(CN)CCCC1
ord_dataset-03ba810b7f464a06b5d8787af2e8b64e
ord-950943709ef94e2cbd449c048cfa7060
NCC1(CN)CCCC1>>C1CCC2(C1)CN=NC2
NCC1(CCCC1)CN.OO.[O-]Cl.[Na+]>>C1N=NCC12CCCC2
[CH2:1]1[CH2:2][CH2:3][C:4]([CH2:6][NH2:7])([CH2:9][NH2:8])[CH2:5]1>>[CH2:1]1[CH2:2][CH2:3][C:4]2([CH2:5]1)[CH2:6][N:7]=[N:8][CH2:9]2
NCC1(CN)CCCC1
C1CCC2(C1)CN=NC2
null
null
CO.O
Oxidation
OtherReaction
090d5d4e81b866fa7ef181e233ee2a58f5345ea9d72b6baa3e51989a1d603bf5
ccb08cdd906ab1c43b965b3f381a9df42e8b4b6ec4217dac787b89befda7069c
C1CCC2(C1)CN=NC2
[NH2;D1;+0:1]-[C:2]-[C:3]-[C:4]-[NH2;D1;+0:5]>>[C:3]1-[C:2]-[N;H0;D2;+0:1]=[N;H0;D2;+0:5]-[C:4]-1
90
[{"value": 90.0, "product": "C1N=NCC12CCCC2", "details": "PERCENTYIELD", "is_desired": false}]
null
null
2
HOUR
C-(1-Aminomethyl-cyclopentyl)-methylamine (4.87 g) was taken up in a mixture of H2O (40 mL) and MeOH (10 mL), and cooled in an ice bath. Simultaneously, H2O2 (23.9 mL of a 30% solution. 6 equiv.) and NaClO (54.3 mL of a 10% solution, 2.4 equiv.) were added dropwise, the ice bath was removed, and the mixture was stirred...
10.6084/m9.figshare.5104873.v1
null
Primary amine.Primary amine
Diazene
null
C1CCC2(C1)CN=NC2
C1CCC2(C1)CN=NC2
null
CO.O
null
2
NCC1(CN)CCCC1>CO.O>C1CCC2(C1)CN=NC2
ord_dataset-03ba810b7f464a06b5d8787af2e8b64e
ord-0f24ae48faae41c7bd08e7d80696285f
BrCCCCCBr.N#CCC#N>>N#CC1(C#N)CCCCC1
C(CC#N)#N.C1CCC2=NCCCN2CC1.BrCCCCCBr>>C1(CCCCC1)(C#N)C#N
Br[CH2:6][CH2:7][CH2:8][CH2:9][CH2:10]Br.[N:1]#[C:2][CH2:3][C:4]#[N:5]>>[N:1]#[C:2][C:3]1([C:4]#[N:5])[CH2:6][CH2:7][CH2:8][CH2:9][CH2:10]1
BrCCCCCBr.N#CCC#N
N#CC1(C#N)CCCCC1
null
null
CN(C)C=O
C-C Coupling
OtherReaction
82c068fef1b7bbb44db21c6f07dae9191b2260270bca592e94309bb776f329ef
7b68950fc1047c59bb49c25e850f5a51cbe91a99bb87839c4547aec123110e4b
C1CCCCC1
Br-[CH2;D2;+0:1]-[C:2]-[C:3]-[C:4]-[CH2;D2;+0:5]-Br.[N;D1;H0:6]#[C:7]-[CH2;D2;+0:8]-[C:9]#[N;D1;H0:10]>>[N;D1;H0:6]#[C:7]-[C;H0;D4;+0:8]1(-[C:9]#[N;D1;H0:10])-[CH2;D2;+0:1]-[C:2]-[C:3]-[C:4]-[CH2;D2;+0:5]-1
null
[]
80
CELSIUS
2
HOUR
Malononitril (15.0 g) was dissolved in dry DMF (200 mL). Subsequently, DBU (75 mL) and 1,5-dibromopentane (34 mL) were added at 0° C. (ice bath). The ice bath was removed and the reaction was stirred for 2 h at 80° C. After cooling down, the reaction was poured into DCM. The organic layer was washed several times with ...
10.6084/m9.figshare.5104873.v1
null
Primary halide.Primary halide
null
null
C1CCCCC1
C1CCCCC1
HBr
CN(C)C=O
80
2
BrCCCCCBr.N#CCC#N>CN(C)C=O>N#CC1(C#N)CCCCC1
ord_dataset-03ba810b7f464a06b5d8787af2e8b64e
ord-fb00120b424c46bd9458335a138b45b6
N#CC1(C#N)CCCCC1>>NCC1(CN)CCCCC1
C1(CCCCC1)(C#N)C#N.[H-].[H-].[H-].[H-].[Li+].[Al+3]>>NCC1(CCCCC1)CN
[N:1]#[C:2][C:3]1([C:4]#[N:5])[CH2:6][CH2:7][CH2:8][CH2:9][CH2:10]1>>[NH2:1][CH2:2][C:3]1([CH2:4][NH2:5])[CH2:6][CH2:7][CH2:8][CH2:9][CH2:10]1
N#CC1(C#N)CCCCC1
NCC1(CN)CCCCC1
null
null
CCOCC
Reduction
OtherReaction
c2340da2c258bf397d4a8fa28e5be42ecf34d1d4e5e541c0aa9e06499bdba3ed
cb8a07357b502aa07f8272954f5a9149eabfa75b76e8c8c18ad60272c8d4f167
C1CCCCC1
[C:1]-[C:2](-[C;H0;D2;+0:3]#[N;H0;D1;+0:4])(-[C;H0;D2;+0:5]#[N;H0;D1;+0:6])-[C:7]>>[C:1]-[C:2](-[CH2;D2;+0:3]-[NH2;D1;+0:4])(-[CH2;D2;+0:5]-[NH2;D1;+0:6])-[C:7]
null
[]
null
null
8
HOUR
Cyclohexane-1,1-dicarbonitrile (20.0 g) was taken up in dry Et2 (70 mL). This mixture was added dropwise to a suspension of LiAlH4 (17.0 g) in dry Et2O (250 mL) cooled in an ice bath. The mixture was stirred overnight at room temperature, cooled in an ice bath, and quenched by adding H2O (17.0 mL), 2M aqueous NaOH (34....
10.6084/m9.figshare.5104873.v1
null
Nitrile.Nitrile
Primary amine.Primary amine
null
null
C1CCCCC1
null
CCOCC
null
8
N#CC1(C#N)CCCCC1>CCOCC>NCC1(CN)CCCCC1
ord_dataset-03ba810b7f464a06b5d8787af2e8b64e
ord-2504d08685a64c35a6ba654bf4472cd6
NCC1(CN)CCCCC1>>C1CCC2(CC1)CN=NC2
OO.[O-]Cl.[Na+].NCC1(CCCCC1)CN>>C1N=NCC12CCCCC2
[CH2:1]1[CH2:2][CH2:3][C:4]([CH2:7][NH2:8])([CH2:10][NH2:9])[CH2:5][CH2:6]1>>[CH2:1]1[CH2:2][CH2:3][C:4]2([CH2:5][CH2:6]1)[CH2:7][N:8]=[N:9][CH2:10]2
NCC1(CN)CCCCC1
C1CCC2(CC1)CN=NC2
null
null
CO.O
Oxidation
OtherReaction
bf22768aa26d28bfe83035a6aafeb24fa2abdfdb833ff6d3a436f3fafddf56f4
ccb08cdd906ab1c43b965b3f381a9df42e8b4b6ec4217dac787b89befda7069c
C1CCC2(CC1)CN=NC2
[NH2;D1;+0:1]-[C:2]-[C:3]-[C:4]-[NH2;D1;+0:5]>>[C:4]1-[C:3]-[C:2]-[N;H0;D2;+0:1]=[N;H0;D2;+0:5]-1
null
[]
null
null
45
MINUTE
C-(1-Aminomethyl-cyclohexyl)-methylamine (10.0 g) was taken up in a mixture of H2O (40 mL) and MeOH (10 mL), and cooled in an ice bath. Simultaneously, H2O2 (44.3 mL of a 30% solution, 6 equiv.) and NaClO (125.5 mL of a 10% solution, 2.4 equiv.) were added dropwise, the ice bath was removed, and the mixture was stirred...
10.6084/m9.figshare.5104873.v1
null
Primary amine.Primary amine
Diazene
null
C1CCC2(CC1)CN=NC2
C1CCC2(CC1)CN=NC2
null
CO.O
null
0.75
NCC1(CN)CCCCC1>CO.O>C1CCC2(CC1)CN=NC2
ord_dataset-03ba810b7f464a06b5d8787af2e8b64e
ord-65b3ead1483c4c8daf4f97d9b1eacd84
CCC(C(C)=O)C(=O)OC.Cc1ccc(S(=O)(=O)O)cc1.OCCO>>CCOC(=O)C(CC)C1(C)OCCO1
COC(C(C(=O)C)CC)=O.C(CO)O.CC=1C=CC(=CC1)S(=O)(=O)O.O>>C(C)OC(C(CC)C1(OCCO1)C)=O
[CH3:2][O:3][C:4](=[O:5])[CH:6]([CH2:7][CH3:8])[C:9]([CH3:10])=[O:11].O=S(=O)(O)c1ccc([CH3:12])cc1.O[CH2:1][CH2:13][OH:14]>>[CH3:1][CH2:2][O:3][C:4](=[O:5])[CH:6]([CH2:7][CH3:8])[C:9]1([CH3:10])[O:11][CH2:12][CH2:13][O:14]1
CCC(C(C)=O)C(=O)OC.Cc1ccc(S(=O)(=O)O)cc1.OCCO
CCOC(=O)C(CC)C1(C)OCCO1
null
null
C1(=CC=CC=C1)C
Heteroatom Alkylation and Arylation
OtherReaction
dd2b98d5fb6672d900f603c2b5596e2f1635a2b64362175d9917c11db3a04bbf
0398a9978bf1c292fba63599c8a89120980e704d65726782f860fad6206da71f
C1COCO1
O-S(=O)(=O)-c1:c:c:c(-[CH3;D1;+0:1]):c:c:1.O-[CH2;D2;+0:2]-[CH2;D2;+0:3]-[OH;D1;+0:4].[C:5]-[C:6](-[C:7](=[O;D1;H0:8])-[#8:9]-[CH3;D1;+0:10])-[C;H0;D3;+0:11](-[C;D1;H3:12])=[O;H0;D1;+0:13]>>[C:5]-[C:6](-[C:7](=[O;D1;H0:8])-[#8:9]-[CH2;D2;+0:10]-[CH3;D1;+0:2])-[C;H0;D4;+0:11]1(-[C;D1;H3:12])-[O;H0;D2;+0:13]-[CH2;D2;+0:1...
null
[]
null
null
null
null
Methyl-2-ethylacetoacetate (100 mL) was taken up in toluene (250 mL). Ethylene glycol (46.9 mL, 1.35 equiv.) and a catalytic amount of p-TsOH.H2O were added, and the mixture was refluxed overnight under Dean-Stark conditions. After cooling to ambient temperature, the mixture was washed with 5% aqueous NaHCO3 and satura...
10.6084/m9.figshare.5104873.v1
null
Tosylate.Ketone.Ester.Primary alcohol.Primary alcohol
Ester.Ether.Ether
c1ccccc1
C1COCO1
C1COCO1
TsOH.HO-
C1(=CC=CC=C1)C
null
null
CCC(C(C)=O)C(=O)OC.Cc1ccc(S(=O)(=O)O)cc1.OCCO>C1(=CC=CC=C1)C>CCOC(=O)C(CC)C1(C)OCCO1
ord_dataset-03ba810b7f464a06b5d8787af2e8b64e
ord-fcb3b7df7fec4410b638d2761073fb52
CCOC(=O)C(CC)C1(C)OCCO1>>CCC(CO)C1(C)OCCO1
C(C)OC(C(CC)C1(OCCO1)C)=O.[H-].[H-].[H-].[H-].[Li+].[Al+3]>>CC1(OCCO1)C(CO)CC
CCO[C:4]([CH:3]([CH2:2][CH3:1])[C:6]1([CH3:7])[O:8][CH2:9][CH2:10][O:11]1)=[O:5]>>[CH3:1][CH2:2][CH:3]([CH2:4][OH:5])[C:6]1([CH3:7])[O:8][CH2:9][CH2:10][O:11]1
CCOC(=O)C(CC)C1(C)OCCO1
CCC(CO)C1(C)OCCO1
null
null
CCOCC
Reduction
Reduction of ester to primary alcohol
21d61543c6ec8a8cebe1b3ef55ef3dd20acbf79a4f1c12a7fb51e32be7a3248a
1fbcd628a0426673c5d10aa49a977cd2d1ae02a8cdf57bbb10d94aa03a94e937
C1COCO1
C-C-O-[C;H0;D3;+0:1](=[O;H0;D1;+0:2])-[C:3](-[C:4])-[C:5](-[#8:6])-[#8:7]>>[#8:6]-[C:5](-[C:3](-[C:4])-[CH2;D2;+0:1]-[OH;D1;+0:2])-[#8:7]
null
[]
null
null
null
null
2-(2-Methyl-[1,3]dioxolan-2-yl)-butyric acid ethyl ester (85.5 g) was taken up in dry Et2O (50 mL). This mixture was added dropwise to a suspension of LiAlH4 (16.1 g) in dry Et2O (200 mL), cooled in an ice bath. The mixture was refluxed for 4 h., cooled in an ice bath, and quenched by adding H2O (16.1 mL), 2M aqueous N...
10.6084/m9.figshare.5104873.v1
null
Ester
Primary alcohol
null
null
C1COCO1
HO-
CCOCC
null
null
CCOC(=O)C(CC)C1(C)OCCO1>CCOCC>CCC(CO)C1(C)OCCO1
ord_dataset-03ba810b7f464a06b5d8787af2e8b64e
ord-59cd7a8427e64aa59ace39ad6c78da57
CC(=O)OC(C)=O.CCC(CO)C(C)=O>>CCC(COC(C)=O)C(C)=O
C(=O)(O)[O-].[Na+].C(C)(=O)OC(C)=O.OCC(C(C)=O)CC.CO>>C(C)C(COC(C)=O)C(C)=O
CC(=O)O[C:6]([CH3:7])=[O:8].[CH3:1][CH2:2][CH:3]([CH2:4][OH:5])[C:9]([CH3:10])=[O:11]>>[CH3:1][CH2:2][CH:3]([CH2:4][O:5][C:6]([CH3:7])=[O:8])[C:9]([CH3:10])=[O:11]
CC(=O)OC(C)=O.CCC(CO)C(C)=O
CCC(COC(C)=O)C(C)=O
null
CN(C)C=1C=CN=CC1
C(Cl)(Cl)Cl
Acylation
Transesterification
f81e513b7b512b10157c16426844efd8d88e34c97987c1347c6ba8a688351205
fc27d67c790d5fb520ba5d49de1490661fa5b822b714863734ce7e3029dfa84f
null
C-C(=O)-O-[C;H0;D3;+0:1](-[C;D1;H3:2])=[O;D1;H0:3].[C;D1;H3:4]-[C:5](=[O;D1;H0:6])-[C:7]-[C:8]-[OH;D1;+0:9]>>[C;D1;H3:4]-[C:5](=[O;D1;H0:6])-[C:7]-[C:8]-[O;H0;D2;+0:9]-[C;H0;D3;+0:1](-[C;D1;H3:2])=[O;D1;H0:3]
null
[]
null
null
8
HOUR
3-Hydroxymethyl-pentan-2-one (20.7 g) was dissolved in CHCl3 (150 mL) and cooled in an ice bath. Acetic anhydride (80 mL) was added, followed by DMAP (2.18 g), and the mixture was stirred overnight at room temperature. After cooling in an ice bath, MeOH (120 mL) was added dropwise, and the mixture was poured into a sat...
10.6084/m9.figshare.5104873.v1
null
Anhydride.Primary alcohol
Ester
null
null
null
HO-
CN(C)C=1C=CN=CC1.C(Cl)(Cl)Cl
null
8
CC(=O)OC(C)=O.CCC(CO)C(C)=O>CN(C)C=1C=CN=CC1.C(Cl)(Cl)Cl>CCC(COC(C)=O)C(C)=O
ord_dataset-03ba810b7f464a06b5d8787af2e8b64e
ord-e0efabadef9048dc84919e5833e7dc29
C=O.CNC.O=C1CCCCC1>>CN(C)CC1CCCCC1=O
C1(CCCCC1)=O.C=O.Cl.CNC>>CN(C)CC1C(CCCC1)=O
O=[CH2:4].[CH3:1][NH:2][CH3:3].[CH2:5]1[CH2:6][CH2:7][CH2:8][CH2:9][C:10]1=[O:11]>>[CH3:1][N:2]([CH3:3])[CH2:4][CH:5]1[CH2:6][CH2:7][CH2:8][CH2:9][C:10]1=[O:11]
C=O.CNC.O=C1CCCCC1
CN(C)CC1CCCCC1=O
null
null
O
Heteroatom Alkylation and Arylation
OtherReaction
2bf1ede5572b12bbfdb633effec5cdb6469d6ff6fc98f249a248eade23e7c341
e8784011446fecd0a9b69948eec8f6e670a0f5952d23e21c3e86b629168fc3f8
O=C1CCCCC1
O=[CH2;D1;+0:1].[C;D1;H3:2]-[NH;D2;+0:3]-[C;D1;H3:4].[C:5]-[C:6]-[CH2;D2;+0:7]-[C:8](=[O;D1;H0:9])-[C:10]>>[C:5]-[C:6]-[CH;D3;+0:7](-[CH2;D2;+0:1]-[N;H0;D3;+0:3](-[C;D1;H3:2])-[C;D1;H3:4])-[C:8](=[O;D1;H0:9])-[C:10]
null
[]
null
null
null
null
To cyclohexanone (259 mL) was added formaldehyde (37.2 mL of a 37% aqueous solution) and dimethylamine hydrochloride (40.8 g). The stirred mixture was slowly heated and refluxed for 1 h. After cooling to ambient temperature H2O was added, and the mixture was extracted twice with Et2O. The aqueous layer was made basic b...
10.6084/m9.figshare.5104873.v1
null
Formaldehyde.Ketone.Secondary amine
Ketone.Tertiary amine
C1CCCCC1
C1CCCCC1
C1CCCCC1
HO-
O
null
null
C=O.CNC.O=C1CCCCC1>O>CN(C)CC1CCCCC1=O
ord_dataset-03ba810b7f464a06b5d8787af2e8b64e
ord-d60c876a3fb140c791fbe1953581d169
CN(C)CC1CCCCC1=O.NN>>C1CCC2CNN=C2C1
O.NN.CN(C)CC1C(CCCC1)=O>>N=1NCC2CCCCC12
C[N:6](C)[CH2:5][CH:4]1[CH2:3][CH2:2][CH2:1][CH2:9][C:8]1=O.N[NH2:7]>>[CH2:1]1[CH2:2][CH2:3][CH:4]2[CH2:5][NH:6][N:7]=[C:8]2[CH2:9]1
CN(C)CC1CCCCC1=O.NN
C1CCC2CNN=C2C1
null
null
CCCCO
Miscellaneous
OtherReaction
4fad93a6df77a16da6173b64a227379a563c7e32954554cdd404e670cc39a17d
2c24edd496ac562589e3c82864b175f91077835801e55e36f11445a79aa1b0d9
C1CCC2CNN=C2C1
C-[N;H0;D3;+0:1](-C)-[C:2]-[C:3](-[C:4])-[C;H0;D3;+0:5](=O)-[C:6]-[C:7].N-[NH2;D1;+0:8]>>[C:7]-[C:6]-[C;H0;D3;+0:5]1=[N;H0;D2;+0:8]-[NH;D2;+0:1]-[C:2]-[C:3]-1-[C:4]
null
[]
null
null
null
null
Hydrazine hydrate (28.0 mL) was dissolved in n-BuOH (200 mL) and cooled in an ice bath. A solution of 2-dimethylaminomethyl-cyclohexanone (64.0 g) in n-BuOH (50 mL) was added dropwise, the mixture was slowly warmed and refluxed for 20 hours. The solvent was evaporated under reduced pressure. Conditions: See reaction.no...
10.6084/m9.figshare.5104873.v1
null
Hydrazine.Ketone.Tertiary amine
Hydrazone
C1CCCCC1
C1CCC2CNN=C2C1
C1CCC2CNN=C2C1
HO-
CCCCO
null
null
CN(C)CC1CCCCC1=O.NN>CCCCO>C1CCC2CNN=C2C1
ord_dataset-03ba810b7f464a06b5d8787af2e8b64e
ord-47839d9892c84994b6ebb315809c5146
CC(=O)C(C)(C)CO.CS(=O)(=O)Cl>>CC(=O)C(C)(C)COS(C)(=O)=O
OCC(C(C)=O)(C)C.N1=CC=CC=C1.S(=O)(=O)(C)Cl>>CC(COS(=O)(=O)C)(C(C)=O)C
[CH3:1][C:2](=[O:3])[C:4]([CH3:5])([CH3:6])[CH2:7][OH:8].Cl[S:9]([CH3:10])(=[O:11])=[O:12]>>[CH3:1][C:2](=[O:3])[C:4]([CH3:5])([CH3:6])[CH2:7][O:8][S:9]([CH3:10])(=[O:11])=[O:12]
CC(=O)C(C)(C)CO.CS(=O)(=O)Cl
CC(=O)C(C)(C)COS(C)(=O)=O
null
null
C(Cl)Cl
Acylation
Formation of Sulfonic Esters
2fa969eb2c954bb96793348a1b2335ec63fbd290dadec6e3e02295e1768e64cf
cb77b899e4adf980b1def97230ef2861660fd7f9602260ec64747d9afd3a795a
null
Cl-[S;H0;D4;+0:1](-[C;D1;H3:2])(=[O;D1;H0:3])=[O;D1;H0:4].[C;D1;H3:5]-[C:6](=[O;D1;H0:7])-[C:8]-[C:9]-[OH;D1;+0:10]>>[C;D1;H3:2]-[S;H0;D4;+0:1](=[O;D1;H0:3])(=[O;D1;H0:4])-[O;H0;D2;+0:10]-[C:9]-[C:8]-[C:6](-[C;D1;H3:5])=[O;D1;H0:7]
null
[]
null
null
20
HOUR
23.7 g 4-Hydroxy-3,3-dimethyl-butan-2-one was dissolved in 150 mL DCM. 49.5 mL (3 eq) pyridine and 17.5 mL (1.1 eq) mesylchloride were added and the mixture was stirred at room temperature for 20 hours. The suspension was filtered and the filter cake was washed two times with DCM. The filtrate was washed with 1 M HCl a...
10.6084/m9.figshare.5104873.v1
null
Primary alcohol.Sulfonyl halide
Mesylate
null
null
null
HCl
C(Cl)Cl
null
20
CC(=O)C(C)(C)CO.CS(=O)(=O)Cl>C(Cl)Cl>CC(=O)C(C)(C)COS(C)(=O)=O
ord_dataset-03ba810b7f464a06b5d8787af2e8b64e
ord-82bf5f4e932d4b81942421c22a32c6e8
C=O.CC(=O)c1ccccc1.CNC>>CN(C)CCC(=O)c1ccccc1
Cl.C(C)(=O)C1=CC=CC=C1.C=O.Cl.CNC>>Cl.CN(CCC(=O)C1=CC=CC=C1)C
O=[CH2:4].[CH3:5][C:6](=[O:7])[c:8]1[cH:9][cH:10][cH:11][cH:12][cH:13]1.[CH3:1][NH:2][CH3:3]>>[CH3:1][N:2]([CH3:3])[CH2:4][CH2:5][C:6](=[O:7])[c:8]1[cH:9][cH:10][cH:11][cH:12][cH:13]1
C=O.CC(=O)c1ccccc1.CNC
CN(C)CCC(=O)c1ccccc1
null
null
CCO
Heteroatom Alkylation and Arylation
OtherReaction
4c2c90d9f645c3d0fa0215eb47d000c493e1508aed4accd3d32ce0636c4f4501
e8784011446fecd0a9b69948eec8f6e670a0f5952d23e21c3e86b629168fc3f8
c1ccccc1
O=[CH2;D1;+0:1].[C;D1;H3:2]-[NH;D2;+0:3]-[C;D1;H3:4].[CH3;D1;+0:5]-[C:6](=[O;D1;H0:7])-[c:8]>>[C;D1;H3:2]-[N;H0;D3;+0:3](-[C;D1;H3:4])-[CH2;D2;+0:1]-[CH2;D2;+0:5]-[C:6](=[O;D1;H0:7])-[c:8]
null
[]
null
null
null
null
To a solution of 0.5 mL concentrated aqueous HCl in 40 mL EtOH, acetophenone (30.0 g), paraformaldehyde (10.0 g) and dimethylamine hydrochloride (26.5 g) were added and the mixture was refluxed for 3 h. The mixture was cooled to room temperature, and the precipitate was filtered, washed with acetone and dried in vacuo ...
10.6084/m9.figshare.5104873.v1
null
Formaldehyde.Ketone.Secondary amine
Ketone.Tertiary amine
null
null
c1ccccc1
HO-
CCO
null
null
C=O.CC(=O)c1ccccc1.CNC>CCO>CN(C)CCC(=O)c1ccccc1
ord_dataset-03ba810b7f464a06b5d8787af2e8b64e
ord-97522613bb9a4da1bcaf9856395657d5
CN(C)CCC(=O)c1ccccc1.NN>>c1ccc(C2=NNCC2)cc1
O.NN.[OH-].[Na+].Cl.CN(CCC(=O)C1=CC=CC=C1)C>>C1(=CC=CC=C1)C1=NNCC1
CN(C)[CH2:8][CH2:9][C:5](=O)[c:4]1[cH:3][cH:2][cH:1][cH:11][cH:10]1.[NH2:6][NH2:7]>>[cH:1]1[cH:2][cH:3][c:4]([C:5]2=[N:6][NH:7][CH2:8][CH2:9]2)[cH:10][cH:11]1
CN(C)CCC(=O)c1ccccc1.NN
c1ccc(C2=NNCC2)cc1
null
null
CO
Heteroatom Alkylation and Arylation
OtherReaction
8ce4f433f4e843e34bf7c68272fb771615f9a0c93eba0d07ae65479474febfb7
75fb5ba864750cb62e4f77513eb04a2b99d0d7a6124313633b89c3d41f574e87
c1ccc(C2=NNCC2)cc1
C-N(-C)-[CH2;D2;+0:1]-[C:2]-[C;H0;D3;+0:3](=O)-[c:4](:[c:5]):[c:6].[NH2;D1;+0:7]-[NH2;D1;+0:8]>>[c:5]:[c:4](-[C;H0;D3;+0:3]1=[N;H0;D2;+0:7]-[NH;D2;+0:8]-[CH2;D2;+0:1]-[C:2]-1):[c:6]
null
[]
50
CELSIUS
null
null
Under N2 atmosphere, 3-dimethylamino-1-phenyl-propan-1-one hydrochloride (37.2 g) was dissolved in warm MeOH (75 mL), and slowly added to a solution of hydrazine hydrate (23 mL) and 50% aqueous NaOH (12 mL) in MeOH (30 mL) stirred at 50° C. The mixture was refluxed for 2 hours and evaporated under reduced pressure. Ice...
10.6084/m9.figshare.5104873.v1
null
Hydrazine.Ketone.Tertiary amine
Hydrazone
null
C1=NNCC1
c1ccccc1.C1=NNCC1
HO-
CO
50
null
CN(C)CCC(=O)c1ccccc1.NN>CO>c1ccc(C2=NNCC2)cc1
ord_dataset-03ba810b7f464a06b5d8787af2e8b64e
ord-d84e1cfa1e914306a388d7fad0ad38b1
C=O.CC(=O)c1ccc(Cl)cc1.CNC>>CN(C)CCC(=O)c1ccc(Cl)cc1
ClC1=CC=C(C=C1)C(C)=O.Cl.CNC.C=O.Cl>>Cl.ClC1=CC=C(C=C1)C(CCN(C)C)=O
O=[CH2:4].[CH3:5][C:6](=[O:7])[c:8]1[cH:9][cH:10][c:11]([Cl:12])[cH:13][cH:14]1.[CH3:1][NH:2][CH3:3]>>[CH3:1][N:2]([CH3:3])[CH2:4][CH2:5][C:6](=[O:7])[c:8]1[cH:9][cH:10][c:11]([Cl:12])[cH:13][cH:14]1
C=O.CC(=O)c1ccc(Cl)cc1.CNC
CN(C)CCC(=O)c1ccc(Cl)cc1
null
null
CCO.CC(=O)C
Heteroatom Alkylation and Arylation
OtherReaction
4c2c90d9f645c3d0fa0215eb47d000c493e1508aed4accd3d32ce0636c4f4501
e8784011446fecd0a9b69948eec8f6e670a0f5952d23e21c3e86b629168fc3f8
c1ccccc1
O=[CH2;D1;+0:1].[C;D1;H3:2]-[NH;D2;+0:3]-[C;D1;H3:4].[CH3;D1;+0:5]-[C:6](=[O;D1;H0:7])-[c:8]>>[C;D1;H3:2]-[N;H0;D3;+0:3](-[C;D1;H3:4])-[CH2;D2;+0:1]-[CH2;D2;+0:5]-[C:6](=[O;D1;H0:7])-[c:8]
112
[{"value": 112.0, "product": "Cl.ClC1=CC=C(C=C1)C(CCN(C)C)=O", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
40
CELSIUS
null
null
To EtOH (80 mL), p-chloroacetophenone (77.3 g, 0.50 mol), dimethylamine hydrochloride (52.7 g, 0.65 mol), paraformaldehyde (19.8 g, 0.66 mol) and concentrated aqueous HCl (1 mL) were added and the mixture was refluxed for 5 h. The mixture was cooled to 40° C., acetone (400 mL) was added, and under stirring the mixture ...
10.6084/m9.figshare.5104873.v1
null
Formaldehyde.Ketone.Secondary amine
Ketone.Tertiary amine
null
null
c1ccccc1
HO-
CCO.CC(=O)C
40
null
C=O.CC(=O)c1ccc(Cl)cc1.CNC>CCO.CC(=O)C>CN(C)CCC(=O)c1ccc(Cl)cc1
ord_dataset-03ba810b7f464a06b5d8787af2e8b64e
ord-46422b9f44604933bc9aea30a17a0796
CN(C)CCC(=O)c1ccc(Cl)cc1.NN>>Clc1ccc(C2=NNCC2)cc1
O.NN.[OH-].[Na+].Cl.ClC1=CC=C(C=C1)C(CCN(C)C)=O>>ClC1=CC=C(C=C1)C1=NNCC1
CN(C)[CH2:9][CH2:10][C:6](=O)[c:5]1[cH:4][cH:3][c:2]([Cl:1])[cH:12][cH:11]1.[NH2:7][NH2:8]>>[Cl:1][c:2]1[cH:3][cH:4][c:5]([C:6]2=[N:7][NH:8][CH2:9][CH2:10]2)[cH:11][cH:12]1
CN(C)CCC(=O)c1ccc(Cl)cc1.NN
Clc1ccc(C2=NNCC2)cc1
null
null
CO
Heteroatom Alkylation and Arylation
OtherReaction
8ce4f433f4e843e34bf7c68272fb771615f9a0c93eba0d07ae65479474febfb7
75fb5ba864750cb62e4f77513eb04a2b99d0d7a6124313633b89c3d41f574e87
c1ccc(C2=NNCC2)cc1
C-N(-C)-[CH2;D2;+0:1]-[C:2]-[C;H0;D3;+0:3](=O)-[c:4](:[c:5]):[c:6].[NH2;D1;+0:7]-[NH2;D1;+0:8]>>[c:5]:[c:4](-[C;H0;D3;+0:3]1=[N;H0;D2;+0:7]-[NH;D2;+0:8]-[CH2;D2;+0:1]-[C:2]-1):[c:6]
null
[]
50
CELSIUS
null
null
Under N2 atmosphere, 1-(4-chloro-phenyl)-3-dimethylamino-propan-1-one hydrochloride (37.2 g) was dissolved in warm MeOH (75 mL), and slowly added to a solution of hydrazine hydrate (23 mL) and 50% aqueous NaOH (12 mL) in MeOH (30 mL) stirred at 50° C. The mixture was refluxed for 2 hours, and evaporated under reduced p...
10.6084/m9.figshare.5104873.v1
null
Hydrazine.Ketone.Tertiary amine
Hydrazone
null
C1=NNCC1
c1ccccc1.C1=NNCC1
HO-
CO
50
null
CN(C)CCC(=O)c1ccc(Cl)cc1.NN>CO>Clc1ccc(C2=NNCC2)cc1
ord_dataset-03ba810b7f464a06b5d8787af2e8b64e
ord-7f87a3c0d5dd43838f708ff5bd85a19e
C=O.CC(=O)Cc1ccccc1>>C=C(C(C)=O)c1ccccc1
C1(=CC=CC=C1)CC(C)=O.C=O.N1CCCCC1.CC(=O)O>>C1(=CC=CC=C1)C(C(C)=O)=C
O=[CH2:1].[CH2:2]([C:3]([CH3:4])=[O:5])[c:6]1[cH:7][cH:8][cH:9][cH:10][cH:11]1>>[CH2:1]=[C:2]([C:3]([CH3:4])=[O:5])[c:6]1[cH:7][cH:8][cH:9][cH:10][cH:11]1
C=O.CC(=O)Cc1ccccc1
C=C(C(C)=O)c1ccccc1
null
null
CO
C-C Coupling
Aldol condensation
e018cde8d346e007217a7d623d56b481720581fd1c253a681b8af9a72d815368
78c3c8e8e07039066e4f5b32d7bb729f171f9f9ecd946fef585e1cde063a41ff
c1ccccc1
O=[CH2;D1;+0:1].[C;D1;H3:2]-[C:3](=[O;D1;H0:4])-[CH2;D2;+0:5]-[c:6](:[c:7]):[c:8]>>[C;D1;H3:2]-[C:3](=[O;D1;H0:4])-[C;H0;D3;+0:5](=[CH2;D1;+0:1])-[c:6](:[c:7]):[c:8]
null
[]
60
CELSIUS
3
HOUR
1-Phenyl-propan-2-one (40.8 g) was dissolved in 200 ml of MeOH. Formaline (37%) (79 mL), piperidine (4 ml) and HOAc (4 ml) where added and de reaction was stirred for 3 h at 60° C. The reaction mixture was evaporated to dryness under reduced pressure. The residue was taken up in diethyl ether, and extracted with water....
10.6084/m9.figshare.5104873.v1
null
Formaldehyde.Ketone
Ketone.Vinyl
null
null
c1ccccc1
HO-
CO
60
3
C=O.CC(=O)Cc1ccccc1>CO>C=C(C(C)=O)c1ccccc1
ord_dataset-03ba810b7f464a06b5d8787af2e8b64e
ord-cc69153d0baf4ca4ad6a0b45e3ed5cb5
NN.O=CC=Cc1ccccc1>>C1=NNC(c2ccccc2)C1
O.NN.C(C=CC1=CC=CC=C1)=O>>C1(=CC=CC=C1)C1CC=NN1
[NH2:2][NH2:3].O=[CH:1][CH:11]=[CH:4][c:5]1[cH:6][cH:7][cH:8][cH:9][cH:10]1>>[CH:1]1=[N:2][NH:3][CH:4]([c:5]2[cH:6][cH:7][cH:8][cH:9][cH:10]2)[CH2:11]1
NN.O=CC=Cc1ccccc1
C1=NNC(c2ccccc2)C1
null
null
CC(C)(C)O
Heteroatom Alkylation and Arylation
OtherReaction
e6b0a90bdf5439b0bafd80ec758c59b627b7e6dc79c973ee1b2fae667e8d9d63
c3cbc07b90655a7aa9777b584274a03a2ec0cff34c5b5edc214a16916fe29f1c
C1=NNC(c2ccccc2)C1
O=[CH;D2;+0:1]-[CH;D2;+0:2]=[CH;D2;+0:3]-[c:4](:[c:5]):[c:6].[NH2;D1;+0:7]-[NH2;D1;+0:8]>>[c:5]:[c:4](-[CH;D3;+0:3]1-[CH2;D2;+0:2]-[CH;D2;+0:1]=[N;H0;D2;+0:7]-[NH;D2;+0:8]-1):[c:6]
null
[]
null
null
null
null
Under N2 atmosphere, hydrazine hydrate (9.2 mL) was added to a solution of cinnamaldehyde (10.0 g) in t-BuOH (20 mL). The mixture was refluxed overnight, followed by concentration under reduced pressure. Water was added to the residue, and the aqueous phase was extracted twice with DCM. The combined organic layers were...
10.6084/m9.figshare.5104873.v1
null
Hydrazine.Aldehyde
Hydrazone
null
C1=NNCC1
C1=NNCC1.c1ccccc1
HO-
CC(C)(C)O
null
null
NN.O=CC=Cc1ccccc1>CC(C)(C)O>C1=NNC(c2ccccc2)C1
ord_dataset-03ba810b7f464a06b5d8787af2e8b64e
ord-b2811bb47fe647e7a75ae671606e3709
NN.O=CC=Cc1cccnc1>>C1=NNC(c2cccnc2)C1
O.NN.N1=CC(=CC=C1)C=CC=O>>N=1NC(CC1)C=1C=NC=CC1
[NH2:2][NH2:3].O=[CH:1][CH:11]=[CH:4][c:5]1[cH:6][cH:7][cH:8][n:9][cH:10]1>>[CH:1]1=[N:2][NH:3][CH:4]([c:5]2[cH:6][cH:7][cH:8][n:9][cH:10]2)[CH2:11]1
NN.O=CC=Cc1cccnc1
C1=NNC(c2cccnc2)C1
null
null
CC(C)(C)O
Heteroatom Alkylation and Arylation
OtherReaction
e6b0a90bdf5439b0bafd80ec758c59b627b7e6dc79c973ee1b2fae667e8d9d63
c3cbc07b90655a7aa9777b584274a03a2ec0cff34c5b5edc214a16916fe29f1c
C1=NNC(c2cccnc2)C1
O=[CH;D2;+0:1]-[CH;D2;+0:2]=[CH;D2;+0:3]-[c:4](:[c:5]):[c:6]:[#7;a:7]:[c:8].[NH2;D1;+0:9]-[NH2;D1;+0:10]>>[c:5]:[c:4](-[CH;D3;+0:3]1-[CH2;D2;+0:2]-[CH;D2;+0:1]=[N;H0;D2;+0:9]-[NH;D2;+0:10]-1):[c:6]:[#7;a:7]:[c:8]
null
[]
null
null
null
null
Under N2 atmosphere, hydrazine hydrate (3.65 mL, 2 equiv.) was added to a solution of 3-(3-pyridyl)acrolein (5.0 g) in t-BuOH (25 mL). The mixture was refluxed for 3 days, followed by evaporation under reduced pressure. The residue was taken up in DCM and washed with 5% aqueous NaHCO3. The organic phase was dried over ...
10.6084/m9.figshare.5104873.v1
null
Hydrazine.Aldehyde
Hydrazone
null
C1=NNCC1
C1=NNCC1.c1ccncc1
HO-
CC(C)(C)O
null
null
NN.O=CC=Cc1cccnc1>CC(C)(C)O>C1=NNC(c2cccnc2)C1
ord_dataset-03ba810b7f464a06b5d8787af2e8b64e
ord-a7d533dfc1c64b57a8781969f0672fcd
CC(C=O)=Cc1ccccc1.NN>>CC1C=NNC1c1ccccc1
O.NN.C(C)OCC.CC(C=O)=CC1=CC=CC=C1>>CC1C=NNC1C1=CC=CC=C1
O=[CH:3][C:2]([CH3:1])=[CH:6][c:7]1[cH:8][cH:9][cH:10][cH:11][cH:12]1.[NH2:4][NH2:5]>>[CH3:1][CH:2]1[CH:3]=[N:4][NH:5][CH:6]1[c:7]1[cH:8][cH:9][cH:10][cH:11][cH:12]1
CC(C=O)=Cc1ccccc1.NN
CC1C=NNC1c1ccccc1
null
null
O
Heteroatom Alkylation and Arylation
OtherReaction
e6b0a90bdf5439b0bafd80ec758c59b627b7e6dc79c973ee1b2fae667e8d9d63
c3cbc07b90655a7aa9777b584274a03a2ec0cff34c5b5edc214a16916fe29f1c
C1=NNC(c2ccccc2)C1
O=[CH;D2;+0:1]-[C;H0;D3;+0:2](-[C;D1;H3:3])=[CH;D2;+0:4]-[c:5](:[c:6]):[c:7].[NH2;D1;+0:8]-[NH2;D1;+0:9]>>[C;D1;H3:3]-[CH;D3;+0:2]1-[CH;D2;+0:1]=[N;H0;D2;+0:8]-[NH;D2;+0:9]-[CH;D3;+0:4]-1-[c:5](:[c:6]):[c:7]
null
[]
null
null
8
HOUR
5.22 ml (1 equiv.) hydrazine hydrate was added to 100 mL diethylether. The emulsion was cooled with an ice bath. 15.0 mL 2-Methyl-3-phenyl-propenal was added dropwise, and the mixture was stirred overnight at room temperature. H2O was added, the organic layer was separated and the aqueous layer was extracted with dieth...
10.6084/m9.figshare.5104873.v1
null
Hydrazine.Aldehyde
Hydrazone
null
C1=NNCC1
C1=NNCC1.c1ccccc1
HO-
O
null
8
CC(C=O)=Cc1ccccc1.NN>O>CC1C=NNC1c1ccccc1
ord_dataset-03ba810b7f464a06b5d8787af2e8b64e
ord-d24af1c2c83e4a5d85276af70c02367d
CCCC=O.O=Cc1ccccc1>>CCC(C=O)=Cc1ccccc1
Cl.[OH-].[K+].C(C1=CC=CC=C1)=O.C(CCC)=O>>C(C1=CC=CC=C1)=C(C=O)CC
[CH3:1][CH2:2][CH2:3][CH:4]=[O:5].O=[CH:6][c:7]1[cH:8][cH:9][cH:10][cH:11][cH:12]1>>[CH3:1][CH2:2][C:3]([CH:4]=[O:5])=[CH:6][c:7]1[cH:8][cH:9][cH:10][cH:11][cH:12]1
CCCC=O.O=Cc1ccccc1
CCC(C=O)=Cc1ccccc1
null
null
CCO
C-C Coupling
OtherReaction
154f038b7f5648ae5349abff8a924c982177f620bdfb6a2f53d7ca0fce37c68d
3174a51604157c488f07402e36f994f716989b8fc10687ee243713b4cfbdb11a
c1ccccc1
O=[CH;D2;+0:1]-[c:2](:[c:3]):[c:4].[C;D1;H3:5]-[C:6]-[CH2;D2;+0:7]-[C:8]=[O;D1;H0:9]>>[C;D1;H3:5]-[C:6]-[C;H0;D3;+0:7](-[C:8]=[O;D1;H0:9])=[CH;D2;+0:1]-[c:2](:[c:3]):[c:4]
70
[{"value": 70.0, "product": "C(C1=CC=CC=C1)=C(C=O)CC", "details": "PERCENTYIELD", "is_desired": false}]
null
null
3
DAY
30.0 mL Benzaldehyde was dissolved in 150 mL EtOH and cooled with an ice bath. Added was 5.01 mL 45% KOH (0.2 equiv.), followed by dropwise addition of 16.5 mL butyraldehyde. The mixture was stirred for 3 days at room temperature, acidified with 1M HCl and extracted with ether. The organic layer was dried over Na2SO4, ...
10.6084/m9.figshare.5104873.v1
null
Aldehyde.Aldehyde
Aldehyde
null
null
c1ccccc1
HO-
CCO
null
72
CCCC=O.O=Cc1ccccc1>CCO>CCC(C=O)=Cc1ccccc1
ord_dataset-03ba810b7f464a06b5d8787af2e8b64e
ord-6b9c95a31ad94f898252eaa163b5a2a7
CCC(C=O)=Cc1ccccc1.NN>>CCC1C=NNC1c1ccccc1
O.NN.C(C1=CC=CC=C1)=C(C=O)CC.O>>C(C)C1C=NNC1C1=CC=CC=C1
O=[CH:4][C:3]([CH2:2][CH3:1])=[CH:7][c:8]1[cH:9][cH:10][cH:11][cH:12][cH:13]1.[NH2:5][NH2:6]>>[CH3:1][CH2:2][CH:3]1[CH:4]=[N:5][NH:6][CH:7]1[c:8]1[cH:9][cH:10][cH:11][cH:12][cH:13]1
CCC(C=O)=Cc1ccccc1.NN
CCC1C=NNC1c1ccccc1
null
null
C(C)OCC.CCOCC
Heteroatom Alkylation and Arylation
OtherReaction
e6b0a90bdf5439b0bafd80ec758c59b627b7e6dc79c973ee1b2fae667e8d9d63
c3cbc07b90655a7aa9777b584274a03a2ec0cff34c5b5edc214a16916fe29f1c
C1=NNC(c2ccccc2)C1
O=[CH;D2;+0:1]-[C;H0;D3;+0:2](-[C:3]-[C;D1;H3:4])=[CH;D2;+0:5]-[c:6](:[c:7]):[c:8].[NH2;D1;+0:9]-[NH2;D1;+0:10]>>[C;D1;H3:4]-[C:3]-[CH;D3;+0:2]1-[CH;D2;+0:1]=[N;H0;D2;+0:9]-[NH;D2;+0:10]-[CH;D3;+0:5]-1-[c:6](:[c:7]):[c:8]
94
[{"value": 94.0, "product": "C(C)C1C=NNC1C1=CC=CC=C1", "details": "PERCENTYIELD", "is_desired": false}]
-10
CELSIUS
3
HOUR
62 ml (10 equiv.) hydrazine hydrate was added to 150 mL diethylether. The emulsion was cooled with an ice/NaCl bath to −10° C. A solution of 20.4 g 2-benzylidene-butyraldehyde in 100 mL ether was added dropwise at −10° C. and stirred at −10° C. for 3 hours. The mixture was stirred overnight (with ice bath) and allowed ...
10.6084/m9.figshare.5104873.v1
null
Hydrazine.Aldehyde
Hydrazone
null
C1=NNCC1
C1=NNCC1.c1ccccc1
HO-
C(C)OCC.CCOCC
-10
3
CCC(C=O)=Cc1ccccc1.NN>C(C)OCC.CCOCC>CCC1C=NNC1c1ccccc1
ord_dataset-03ba810b7f464a06b5d8787af2e8b64e
ord-2e554649f6b9407aa6af9dc843fd250c
COC(=O)C1=CCCN(C)C1>>CN1CCC=C(CO)C1
COC(=O)C=1CN(CCC1)C.[H-].[H-].[H-].[H-].[Li+].[Al+3].O.[OH-].[Na+].O>>CN1CC(=CCC1)CO
CO[C:7]([C:6]1=[CH:5][CH2:4][CH2:3][N:2]([CH3:1])[CH2:9]1)=[O:8]>>[CH3:1][N:2]1[CH2:3][CH2:4][CH:5]=[C:6]([CH2:7][OH:8])[CH2:9]1
COC(=O)C1=CCCN(C)C1
CN1CCC=C(CO)C1
null
null
C1CCOC1
Reduction
Reduction of ester to primary alcohol
21d61543c6ec8a8cebe1b3ef55ef3dd20acbf79a4f1c12a7fb51e32be7a3248a
1fbcd628a0426673c5d10aa49a977cd2d1ae02a8cdf57bbb10d94aa03a94e937
C1=CCNCC1
C-O-[C;H0;D3;+0:1](=[O;H0;D1;+0:2])-[C:3](=[C:4]-[C:5])-[C:6]-[#7:7]>>[#7:7]-[C:6]-[C:3](-[CH2;D2;+0:1]-[OH;D1;+0:2])=[C:4]-[C:5]
98.9
[{"value": 98.9, "product": "CN1CC(=CCC1)CO", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
3
HOUR
6.5 g of LiAlH4 (3.2 equiv.) was suspended in 100 mL dry THF and cooled with an ice bath. To this was added dropwise a solution of 8.27 g 1-Methyl-1,2,5,6-tetrahydro-pyridine-3-carboxylic acid methyl ester (free base) in 50 mL dry THF. The mixture was stirred for 3 hours at room temperature. The mixture was cooled with...
10.6084/m9.figshare.5104873.v1
null
Ester
Primary alcohol
null
null
C1=CC[NH]CC1
Other
C1CCOC1
null
3
COC(=O)C1=CCCN(C)C1>C1CCOC1>CN1CCC=C(CO)C1
ord_dataset-03ba810b7f464a06b5d8787af2e8b64e
ord-38568b8d6b4c4702808be1e41b377b58
CN1CCC=C(CO)C1>>CN1CCC=C(C=O)C1
C(C)N(CC)CC.CN1CC(=CCC1)CO.C(C(=O)Cl)(=O)Cl.CS(=O)C>>CN1CC(=CCC1)C=O
[CH3:1][N:2]1[CH2:3][CH2:4][CH:5]=[C:6]([CH2:7][OH:8])[CH2:9]1>>[CH3:1][N:2]1[CH2:3][CH2:4][CH:5]=[C:6]([CH:7]=[O:8])[CH2:9]1
CN1CCC=C(CO)C1
CN1CCC=C(C=O)C1
null
null
O.C(Cl)Cl
Oxidation
Oxidation or Dehydrogenation of Alcohols to Aldehydes and Ketones
41bfa9deea81b465c88ad21fdfb64a2e1ba29490558cf430df132cb98b4a538b
0a03c6724c1862e8f86d4a463afda55b8e067dc6cb42597b472eb7cabc03eda3
C1=CCNCC1
[#7:1]-[C:2]-[C:3](-[CH2;D2;+0:4]-[OH;D1;+0:5])=[C:6]-[C:7]>>[#7:1]-[C:2]-[C:3](-[CH;D2;+0:4]=[O;H0;D1;+0:5])=[C:6]-[C:7]
109.7
[{"value": 85.0, "product": "CN1CC(=CCC1)C=O", "details": "PERCENTYIELD", "is_desired": false}, {"value": 109.7, "product": "CN1CC(=CCC1)C=O", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
-78
CELSIUS
15
MINUTE
2.88 mL oxalyl chloride (2.4 equiv.) was dissolved in 20 mL DCM. The mixture was cooled to −78° C. and a solution of 3.37 mL DMSO (2.0 equiv.) in 10 mL DCM was added dropwise. The mixture was stirred for 15 minutes at −78° C. A solution of 3.0 g (1-Methyl-1,2,5,6-tetrahydro-pyridin-3-yl)-methanol in 10 mL DCM was added...
10.6084/m9.figshare.5104873.v1
null
Primary alcohol
Aldehyde
null
null
C1=CC[NH]CC1
null
O.C(Cl)Cl
-78
0.25
CN1CCC=C(CO)C1>O.C(Cl)Cl>CN1CCC=C(C=O)C1
ord_dataset-03ba810b7f464a06b5d8787af2e8b64e
ord-67e561b31978414c8fcba4efacbbcbe9
CN1CCC=C(C=O)C1.NN>>CN1CCC2NN=CC2C1
CN1CC(=CCC1)C=O.O.NN>>CN1CC2C(CC1)NN=C2
O=[CH:8][C:9]1=[CH:5][CH2:4][CH2:3][N:2]([CH3:1])[CH2:10]1.[NH2:6][NH2:7]>>[CH3:1][N:2]1[CH2:3][CH2:4][CH:5]2[NH:6][N:7]=[CH:8][CH:9]2[CH2:10]1
CN1CCC=C(C=O)C1.NN
CN1CCC2NN=CC2C1
null
null
CCCCO
Heteroatom Alkylation and Arylation
OtherReaction
aa23589c91b6f94ddd92d866429ce13046adef19dfcbac63f7429913b3bb475a
c3cbc07b90655a7aa9777b584274a03a2ec0cff34c5b5edc214a16916fe29f1c
C1=NNC2CCNCC12
O=[CH;D2;+0:1]-[C;H0;D3;+0:2]1=[CH;D2;+0:3]-[C:4]-[C:5]-[#7:6](-[C;D1;H3:7])-[C:8]-1.[NH2;D1;+0:9]-[NH2;D1;+0:10]>>[C;D1;H3:7]-[#7:6]1-[C:8]-[CH;D3;+0:2]2-[CH;D2;+0:1]=[N;H0;D2;+0:10]-[NH;D2;+0:9]-[CH;D3;+0:3]-2-[C:4]-[C:5]-1
null
[]
null
null
null
null
3.2 g 1-Methyl-1,2,5,6-tetrahydro-pyridine-3-carbaldehyde was dissolved in 10 mL n-BuOH. Added were 2 equiv. of hydrazine hydrate, the mixture was refluxed for 24 hours and subsequently concentrated in vacuo. The residue was taken up in DCM and extracted with 2M NaOH, and the organic phase was dried over Na2SO4, filtra...
10.6084/m9.figshare.5104873.v1
null
Hydrazine.Aldehyde
Hydrazone
C1=CC[NH]CC1
C1=NNC2CC[NH]CC12
C1=NNC2CC[NH]CC12
HO-
CCCCO
null
null
CN1CCC=C(C=O)C1.NN>CCCCO>CN1CCC2NN=CC2C1
ord_dataset-03ba810b7f464a06b5d8787af2e8b64e
ord-bb9528bd65444948971ae1d9ea7916a5
BrCc1ccccc1.ClCCNCCCl>>ClCCN(CCCl)Cc1ccccc1
Cl.ClCCNCCCl.C(=O)([O-])[O-].[K+].[K+].C(C1=CC=CC=C1)Br>>C(C1=CC=CC=C1)N(CCCl)CCCl
Br[CH2:8][c:9]1[cH:10][cH:11][cH:12][cH:13][cH:14]1.[Cl:1][CH2:2][CH2:3][NH:4][CH2:5][CH2:6][Cl:7]>>[Cl:1][CH2:2][CH2:3][N:4]([CH2:5][CH2:6][Cl:7])[CH2:8][c:9]1[cH:10][cH:11][cH:12][cH:13][cH:14]1
BrCc1ccccc1.ClCCNCCCl
ClCCN(CCCl)Cc1ccccc1
null
null
C(C)#N
Heteroatom Alkylation and Arylation
N-alkylation of secondary amines with alkyl halides
6d58cac08ccced0a33ed16fbca180bc12aa011288d6476106d98a7b2cbc3d709
523d37155b42c8dc851abeddadebb241cdd90bdf649ba750c35e13c8c752d7b0
c1ccccc1
Br-[CH2;D2;+0:1]-[c:2](:[c:3]):[c:4].[C:5]-[C:6]-[NH;D2;+0:7]-[C:8]-[C:9]>>[C:5]-[C:6]-[N;H0;D3;+0:7](-[C:8]-[C:9])-[CH2;D2;+0:1]-[c:2](:[c:3]):[c:4]
null
[]
null
null
null
null
Bis-(2-chloro-ethyl)-amine hydrochloride was suspended in 150 mL acetonitrile. Added were 34.8 g K2CO3 (3 equiv.) and 10.0 mL benzylbromide (1 equiv.). The mixture was refluxed overnight, Concentration on silica and purification with flash column chromatography (eluents PA:ether=95:5) yielded 4.11 g of a colorless oil....
10.6084/m9.figshare.5104873.v1
null
Primary halide.Secondary amine
Tertiary amine
null
null
c1ccccc1
HBr
C(C)#N
null
null
BrCc1ccccc1.ClCCNCCCl>C(C)#N>ClCCN(CCCl)Cc1ccccc1
ord_dataset-03ba810b7f464a06b5d8787af2e8b64e
ord-6be78afd8b93470f9bf3cd37eaa8369d
NCC1(CN)CCN(Cc2ccccc2)CC1>>c1ccc(CN2CCC3(CC2)CN=NC3)cc1
NCC1(CCN(CC1)CC1=CC=CC=C1)CN.CO.OO.[O-]Cl.[Na+]>>C(C1=CC=CC=C1)N1CCC2(CN=NC2)CC1
[cH:1]1[cH:2][cH:3][c:4]([CH2:5][N:6]2[CH2:7][CH2:8][C:9]([CH2:12][NH2:13])([CH2:15][NH2:14])[CH2:10][CH2:11]2)[cH:16][cH:17]1>>[cH:1]1[cH:2][cH:3][c:4]([CH2:5][N:6]2[CH2:7][CH2:8][C:9]3([CH2:10][CH2:11]2)[CH2:12][N:13]=[N:14][CH2:15]3)[cH:16][cH:17]1
NCC1(CN)CCN(Cc2ccccc2)CC1
c1ccc(CN2CCC3(CC2)CN=NC3)cc1
null
null
O
Oxidation
OtherReaction
18390025a7adc4519b7a462816c7c35329fdd2c4c87c461cd30a333c3a79b596
ccb08cdd906ab1c43b965b3f381a9df42e8b4b6ec4217dac787b89befda7069c
c1ccc(CN2CCC3(CC2)CN=NC3)cc1
[NH2;D1;+0:1]-[C:2]-[C:3]-[C:4]-[NH2;D1;+0:5]>>[C:2]1-[C:3]-[C:4]-[N;H0;D2;+0:5]=[N;H0;D2;+0:1]-1
90.3
[{"value": 90.3, "product": "C(C1=CC=CC=C1)N1CCC2(CN=NC2)CC1", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
1
HOUR
2.48 g of C-(4-Aminomethyl-1-benzyl-piperidin-4-yl)-methylamine was suspended in 40 mL H2O and 10 mL MeOH and cooled with an ice bath. Simultaneously, 6.7 mL 30% H2O2 (6 equiv.) and 15.2 mL 10% NaClO (2.4 equiv.) were added dropwise. The mixture was stirred at room temperature for 1 hour. The mixture was extracted 2 ti...
10.6084/m9.figshare.5104873.v1
null
Primary amine.Primary amine
Diazene
null
C1CC2(CC[NH]1)CN=NC2
c1ccccc1.C1CC2(CC[NH]1)CN=NC2
null
O
null
1
NCC1(CN)CCN(Cc2ccccc2)CC1>O>c1ccc(CN2CCC3(CC2)CN=NC3)cc1
ord_dataset-03ba810b7f464a06b5d8787af2e8b64e
ord-bddcae2aae8a4f21aa0a7311799b508a
CC(C#N)(C#N)COCc1ccccc1>>CC(CN)(CN)COCc1ccccc1
C(C1=CC=CC=C1)OCC(C#N)(C#N)C.[H-].[H-].[H-].[H-].[Li+].[Al+3].O.[OH-].[Na+].O>>C(C1=CC=CC=C1)OCC(CN)(CN)C
[CH3:1][C:2]([C:3]#[N:4])([C:5]#[N:6])[CH2:7][O:8][CH2:9][c:10]1[cH:11][cH:12][cH:13][cH:14][cH:15]1>>[CH3:1][C:2]([CH2:3][NH2:4])([CH2:5][NH2:6])[CH2:7][O:8][CH2:9][c:10]1[cH:11][cH:12][cH:13][cH:14][cH:15]1
CC(C#N)(C#N)COCc1ccccc1
CC(CN)(CN)COCc1ccccc1
null
null
C(C)OCC
Reduction
OtherReaction
c2340da2c258bf397d4a8fa28e5be42ecf34d1d4e5e541c0aa9e06499bdba3ed
cb8a07357b502aa07f8272954f5a9149eabfa75b76e8c8c18ad60272c8d4f167
c1ccccc1
[C:1]-[C:2](-[C;D1;H3:3])(-[C;H0;D2;+0:4]#[N;H0;D1;+0:5])-[C;H0;D2;+0:6]#[N;H0;D1;+0:7]>>[C:1]-[C:2](-[C;D1;H3:3])(-[CH2;D2;+0:4]-[NH2;D1;+0:5])-[CH2;D2;+0:6]-[NH2;D1;+0:7]
92.9
[{"value": 84.0, "product": "C(C1=CC=CC=C1)OCC(CN)(CN)C", "details": "PERCENTYIELD", "is_desired": false}, {"value": 92.9, "product": "C(C1=CC=CC=C1)OCC(CN)(CN)C", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
4
HOUR
LiAlH4 (3.22 g; 84.84 mmol; 3.0 equiv.) was suspended in 30 mL dry diethylether and cooled with an ice bath. A solution of 2-Benzyloxymethyl-2-methyl-malononitrile (5.72 g; 28.28 mmol; 1.0 equiv.) in 20 mL dry diethylether was added dropwise. The suspension was stirred at room temperature for 4 hours, and subsequently ...
10.6084/m9.figshare.5104873.v1
null
Nitrile.Nitrile
Primary amine.Primary amine
null
null
c1ccccc1
null
C(C)OCC
null
4
CC(C#N)(C#N)COCc1ccccc1>C(C)OCC>CC(CN)(CN)COCc1ccccc1
ord_dataset-03ba810b7f464a06b5d8787af2e8b64e
ord-4052a6dbde5847328dbec77949a0b930
BrCCOCCBr.N#CCC#N>>N#CC1(C#N)CCOCC1
C(CC#N)#N.BrCCOCCBr.CC(C)(C)[O-].[K+]>>O1CCC(CC1)(C#N)C#N
Br[CH2:6][CH2:7][O:8][CH2:9][CH2:10]Br.[N:1]#[C:2][CH2:3][C:4]#[N:5]>>[N:1]#[C:2][C:3]1([C:4]#[N:5])[CH2:6][CH2:7][O:8][CH2:9][CH2:10]1
BrCCOCCBr.N#CCC#N
N#CC1(C#N)CCOCC1
null
CCCC[N+](CCCC)(CCCC)CCCC.[Br-]
CS(=O)C.C(Cl)Cl
C-C Coupling
OtherReaction
7a02bf4931a2667c7a560f7e10856bd80597aeb566d8b87c38850fad3f2124c8
7b68950fc1047c59bb49c25e850f5a51cbe91a99bb87839c4547aec123110e4b
C1CCOCC1
Br-[CH2;D2;+0:1]-[C:2]-[#8:3]-[C:4]-[CH2;D2;+0:5]-Br.[N;D1;H0:6]#[C:7]-[CH2;D2;+0:8]-[C:9]#[N;D1;H0:10]>>[N;D1;H0:6]#[C:7]-[C;H0;D4;+0:8]1(-[C:9]#[N;D1;H0:10])-[CH2;D2;+0:1]-[C:2]-[#8:3]-[C:4]-[CH2;D2;+0:5]-1
24
[{"value": 24.0, "product": "O1CCC(CC1)(C#N)C#N", "details": "PERCENTYIELD", "is_desired": false}]
null
null
4
HOUR
Malononitrile (5.0 g) was dissolved in DMSO (5 mL). Subsequently, bis(2-bromoethyl)ether (9.49 mL) and TBAB (1.22 g) were added, followed by portionwise addition of KOtBu (8.49 g). The mixture was stirred for 4 h. at room temperature, taken up in DCM and extracted 3 times with 5% aqueous NaHCO3. The organic phase was d...
10.6084/m9.figshare.5104873.v1
null
Primary halide.Primary halide
null
null
C1CCOCC1
C1CCOCC1
HBr
CCCC[N+](CCCC)(CCCC)CCCC.[Br-].CS(=O)C.C(Cl)Cl
null
4
BrCCOCCBr.N#CCC#N>CCCC[N+](CCCC)(CCCC)CCCC.[Br-].CS(=O)C.C(Cl)Cl>N#CC1(C#N)CCOCC1
ord_dataset-03ba810b7f464a06b5d8787af2e8b64e
ord-b024ed43abc34f699c2cabd633dfb5f9
N#CC1(C#N)CCOCC1>>NCC1(CN)CCOCC1
B.C1CCOC1.[OH-].[Na+].Cl.O1CCC(CC1)(C#N)C#N>>NCC1(CCOCC1)CN
[N:1]#[C:2][C:3]1([C:4]#[N:5])[CH2:6][CH2:7][O:8][CH2:9][CH2:10]1>>[NH2:1][CH2:2][C:3]1([CH2:4][NH2:5])[CH2:6][CH2:7][O:8][CH2:9][CH2:10]1
N#CC1(C#N)CCOCC1
NCC1(CN)CCOCC1
null
null
C1CCOC1
Reduction
OtherReaction
c2340da2c258bf397d4a8fa28e5be42ecf34d1d4e5e541c0aa9e06499bdba3ed
cb8a07357b502aa07f8272954f5a9149eabfa75b76e8c8c18ad60272c8d4f167
C1CCOCC1
[C:1]-[C:2](-[C;H0;D2;+0:3]#[N;H0;D1;+0:4])(-[C;H0;D2;+0:5]#[N;H0;D1;+0:6])-[C:7]>>[C:1]-[C:2](-[CH2;D2;+0:3]-[NH2;D1;+0:4])(-[CH2;D2;+0:5]-[NH2;D1;+0:6])-[C:7]
62.1
[{"value": 62.0, "product": "NCC1(CCOCC1)CN", "details": "PERCENTYIELD", "is_desired": false}, {"value": 62.1, "product": "NCC1(CCOCC1)CN", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
-10
CELSIUS
6
HOUR
Tetrahydro-pyran-4,4-dicarbonitrile (1.52 g) was dissolved in dry THF (25 mL) and cooled to −10° C. To this solution, BH3.THF (56 mL of an 1M solution in THF, 5 equiv.) was added dropwise, the mixture was allowed to warm to room temperature, and subsequently stirred at 60° C. for 6 h. The mixture was cooled in an ice b...
10.6084/m9.figshare.5104873.v1
null
Nitrile.Nitrile
Primary amine.Primary amine
null
null
C1CCOCC1
null
C1CCOC1
-10
6
N#CC1(C#N)CCOCC1>C1CCOC1>NCC1(CN)CCOCC1
ord_dataset-03ba810b7f464a06b5d8787af2e8b64e
ord-f33760f47a354d128b5ea74e5ca6a297
NCC1(CN)CCOCC1>>C1CC2(CCO1)CN=NC2
NCC1(CCOCC1)CN.OO.[O-]Cl.[Na+]>>C1N=NCC12CCOCC2
[CH2:1]1[CH2:2][C:3]([CH2:7][NH2:8])([CH2:10][NH2:9])[CH2:4][CH2:5][O:6]1>>[CH2:1]1[CH2:2][C:3]2([CH2:4][CH2:5][O:6]1)[CH2:7][N:8]=[N:9][CH2:10]2
NCC1(CN)CCOCC1
C1CC2(CCO1)CN=NC2
null
null
CO.O
Oxidation
OtherReaction
b039614aa0942bb786d1e3503d67dcda1e3cab33aa92d388b060f46889f55ddf
ccb08cdd906ab1c43b965b3f381a9df42e8b4b6ec4217dac787b89befda7069c
C1CC2(CCO1)CN=NC2
[NH2;D1;+0:1]-[C:2]-[C:3]-[C:4]-[NH2;D1;+0:5]>>[C:4]1-[C:3]-[C:2]-[N;H0;D2;+0:1]=[N;H0;D2;+0:5]-1
85
[{"value": 85.0, "product": "C1N=NCC12CCOCC2", "details": "PERCENTYIELD", "is_desired": false}]
null
null
8
HOUR
C-(4-Aminomethyl-tetrahydro-pyran-4-yl)-methylamine (1.0 g) was taken up in a mixture of H2O (10 mL) and MeOH (2.5 mL), and cooled in an ice bath. Simultaneously, H2O2 (4.8 mL of a 30% solution, 6 equiv.) and NaClO (12.4 mL of a 10% solution, 2.4 equiv.) were added dropwise, the ice bath was removed, and the mixture wa...
10.6084/m9.figshare.5104873.v1
null
Primary amine.Primary amine
Diazene
null
C1CC2(CCO1)CN=NC2
C1CC2(CCO1)CN=NC2
null
CO.O
null
8
NCC1(CN)CCOCC1>CO.O>C1CC2(CCO1)CN=NC2
ord_dataset-03ba810b7f464a06b5d8787af2e8b64e
ord-a23d62bb03b44b8aa4bbb58712329041
FC(F)(F)CCI.N#CCC#N>>N#CC(C#N)(CC(F)(F)F)CC(F)(F)F
C(CC#N)#N.ICCC(F)(F)F.[H-].[Na+]>>FC(CC(C#N)(C#N)CC(F)(F)F)(F)F
I[CH2:11][CH2:6][C:7]([F:8])([F:10])[F:13].[N:1]#[C:2][CH2:3][C:4]#[N:5]>>[N:1]#[C:2][C:3]([C:4]#[N:5])([CH2:6][C:7]([F:8])([F:9])[F:10])[CH2:11][C:12]([F:13])([F:14])[F:15]
FC(F)(F)CCI.N#CCC#N
N#CC(C#N)(CC(F)(F)F)CC(F)(F)F
null
null
C1CCOC1
C-C Coupling
OtherReaction
80ce7b97e36b0c0ec774726a0bcfd7a54bd6e39c8df554aa1de887d8048dad37
7c1d2c8d4ceba55eeb3a66322d758dc06aaff7a8226b4e829e78570c406fb155
null
I-[CH2;D2;+0:1]-[CH2;D2;+0:2]-[C;H0;D4;+0:3](-[F;D1;H0:4])(-[F;D1;H0:5])-[F;H0;D1;+0:6].[N;D1;H0:7]#[C:8]-[CH2;D2;+0:9]-[C:10]#[N;D1;H0:11]>>[F;D1;H0:4]-[C;H0;D4;+0:3](-[F;D1;H0:5])(-[F;D1;H0:12])-[CH2;D2;+0:2]-[C;H0;D4;+0:9](-[C:8]#[N;D1;H0:7])(-[C:10]#[N;D1;H0:11])-[CH2;D2;+0:1]-[C:13](-[F;D1;H0:14])(-[F;D1;H0:15])-[...
16.4
[{"value": 16.4, "product": "FC(CC(C#N)(C#N)CC(F)(F)F)(F)F", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
2
HOUR
Malononitril (20.15 mmol) and 1-iodo-3,3,3-trifluoropropane (42.65 mmol) were dissolved in 30 ml dry THF, and the mixture was cooled with an ice/salt bath. 1.61 g NaH (40.3 mmol) was added portionwise, keeping the temperature below 5° C. The reaction mixture was stirred at room temperature for 2 hours and evaporated un...
10.6084/m9.figshare.5104873.v1
null
Trifluoro group.Primary halide
Trifluoro group.Trifluoro group
null
null
null
HI
C1CCOC1
null
2
FC(F)(F)CCI.N#CCC#N>C1CCOC1>N#CC(C#N)(CC(F)(F)F)CC(F)(F)F
ord_dataset-03ba810b7f464a06b5d8787af2e8b64e
ord-1ce3f963d5cc4f66ad04c748a392f7d0
N#CC(C#N)(CC(F)(F)F)CC(F)(F)F>>NCC(CN)(CC(F)(F)F)CC(F)(F)F
[H-].[H-].[H-].[H-].[Li+].[Al+3].FC(CC(C#N)(C#N)CC(F)(F)F)(F)F>>FC(CC(CN)(CN)CC(F)(F)F)(F)F
[N:1]#[C:2][C:3]([C:4]#[N:5])([CH2:6][C:7]([F:8])([F:9])[F:10])[CH2:11][C:12]([F:13])([F:14])[F:15]>>[NH2:1][CH2:2][C:3]([CH2:4][NH2:5])([CH2:6][C:7]([F:8])([F:9])[F:10])[CH2:11][C:12]([F:13])([F:14])[F:15]
N#CC(C#N)(CC(F)(F)F)CC(F)(F)F
NCC(CN)(CC(F)(F)F)CC(F)(F)F
null
null
CCOCC
Reduction
OtherReaction
c2340da2c258bf397d4a8fa28e5be42ecf34d1d4e5e541c0aa9e06499bdba3ed
cb8a07357b502aa07f8272954f5a9149eabfa75b76e8c8c18ad60272c8d4f167
null
[C:1]-[C:2](-[C:3])(-[C;H0;D2;+0:4]#[N;H0;D1;+0:5])-[C;H0;D2;+0:6]#[N;H0;D1;+0:7]>>[C:1]-[C:2](-[C:3])(-[CH2;D2;+0:4]-[NH2;D1;+0:5])-[CH2;D2;+0:6]-[NH2;D1;+0:7]
91.5
[{"value": 91.5, "product": "FC(CC(CN)(CN)CC(F)(F)F)(F)F", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
8
HOUR
340 mg LiAlH4 (8.95 mmol) was suspended in 15 ml dry Et2O and cooled in an ice bath. A solution of 760 mg 2,2-Bis-(2,2,2-trifluoro-ethyl)-malononitrile in Et2O was added dropwise at such a rate that the temperature was kept below 20° C. The mixture was stirred overnight at room temperature, cooled in an ice bath, and q...
10.6084/m9.figshare.5104873.v1
null
Nitrile.Nitrile
Primary amine.Primary amine
null
null
null
null
CCOCC
null
8
N#CC(C#N)(CC(F)(F)F)CC(F)(F)F>CCOCC>NCC(CN)(CC(F)(F)F)CC(F)(F)F
ord_dataset-03ba810b7f464a06b5d8787af2e8b64e
ord-ac56c7d916db4ddcb9163798bf19af4e
COC(=O)Cl.NS(=O)(=O)c1ccccc1Cl>>COC(=O)NS(=O)(=O)c1ccccc1Cl
ClC(=O)OC.ClC1=C(C=CC=C1)S(=O)(=O)N.C(C)N(CC)CC>>COC(NS(=O)(=O)C1=C(C=CC=C1)Cl)=O
Cl[C:3]([O:2][CH3:1])=[O:4].[NH2:5][S:6](=[O:7])(=[O:8])[c:9]1[cH:10][cH:11][cH:12][cH:13][c:14]1[Cl:15]>>[CH3:1][O:2][C:3](=[O:4])[NH:5][S:6](=[O:7])(=[O:8])[c:9]1[cH:10][cH:11][cH:12][cH:13][c:14]1[Cl:15]
COC(=O)Cl.NS(=O)(=O)c1ccccc1Cl
COC(=O)NS(=O)(=O)c1ccccc1Cl
null
null
C(C)#N
Protection
Acylation of Nitrogen Nucleophiles by Acyl/Thioacyl/Carbamoyl Halides and Analogs_OS
2f2696288009d2012d9ec2995f8be43c58fdee99389b7d218ed77c4bafda7b17
60493cac785f670383c62b059214a5eb4def232e11814f271849329f2f6b7966
c1ccccc1
Cl-[C;H0;D3;+0:1](=[O;D1;H0:2])-[#8:3]-[C;D1;H3:4].[NH2;D1;+0:5]-[#16:6](=[O;D1;H0:7])(=[O;D1;H0:8])-[c:9]>>[C;D1;H3:4]-[#8:3]-[C;H0;D3;+0:1](=[O;D1;H0:2])-[NH;D2;+0:5]-[#16:6](=[O;D1;H0:7])(=[O;D1;H0:8])-[c:9]
null
[]
null
null
8
HOUR
To 25.0 g 2-chloro-benzenesulfonamide was added 75 mL acetonitrile and 45.2 mL (2.5 eq) triethylamine. The mixture was cooled with an ice bath and 15.1 mL methyl chloroformate was slowly added dropwise. The mixture was stirred overnight at room temperature and concentrated in vacuo. Water was added and de aqueous layer...
10.6084/m9.figshare.5104873.v1
null
Acyl halide.Sulfonamide
Sulfonamide.Carbamic ester
null
null
c1ccccc1
HCl
C(C)#N
null
8
COC(=O)Cl.NS(=O)(=O)c1ccccc1Cl>C(C)#N>COC(=O)NS(=O)(=O)c1ccccc1Cl
ord_dataset-03ba810b7f464a06b5d8787af2e8b64e
ord-e6f8b38247c34282b73c14f8fb70fdee
CCC1C=NNC1.CSC(=NS(=O)(=O)c1ccccc1Cl)SC>>CCC1C=NN(SC(C)=NS(=O)(=O)c2ccccc2Cl)C1
C(C)C1C=NNC1.N1=CC=CC=C1.CSC(=NS(=O)(=O)C1=C(C=CC=C1)Cl)SC>>ClC1=C(C=CC=C1)S(=O)(=O)N=C(SN1N=CC(C1)CC)C
[CH3:1][CH2:2][CH:3]1[CH:4]=[N:5][NH:6][CH2:21]1.C[S:7][C:8](S[CH3:9])=[N:10][S:11](=[O:12])(=[O:13])[c:14]1[cH:15][cH:16][cH:17][cH:18][c:19]1[Cl:20]>>[CH3:1][CH2:2][CH:3]1[CH:4]=[N:5][N:6]([S:7][C:8]([CH3:9])=[N:10][S:11](=[O:12])(=[O:13])[c:14]2[cH:15][cH:16][cH:17][cH:18][c:19]2[Cl:20])[CH2:21]1
CCC1C=NNC1.CSC(=NS(=O)(=O)c1ccccc1Cl)SC
CCC1C=NN(SC(C)=NS(=O)(=O)c2ccccc2Cl)C1
null
null
null
C-C Coupling
OtherReaction
8d8b038879f9ae3e1763bb6b094352cbfbed836bcad13bd5634b2dfd4485a184
ba9da9a3c58c760c9d311761733b7830676bada377cf8304c7fe9c76e3ef2110
O=S(=O)(N=CSN1CCC=N1)c1ccccc1
C-[S;H0;D2;+0:1]-[C;H0;D3;+0:2](-S-[CH3;D1;+0:3])=[#7:4]-[#16:5].[#7:6]1=[C:7]-[C:8]-[C:9]-[NH;D2;+0:10]-1>>[#16:5]-[#7:4]=[C;H0;D3;+0:2](-[CH3;D1;+0:3])-[S;H0;D2;+0:1]-[N;H0;D3;+0:10]1-[#7:6]=[C:7]-[C:8]-[C:9]-1
null
[]
null
null
null
null
500 mg 4-Ethyl-4,5-dihydro-1H-pyrazole was dissolved in 10 mL pyridine. 1.51 g N-(Bis-methylsulfanyl-methylene)-2-chloro-benzenesulfonamide was added and the mixture was refluxed overnight. The mixture was concentrated in vacuo and H2O was added, followed by extraction twice with DCM. The combined organic layers were d...
10.6084/m9.figshare.5104873.v1
null
Hydrazone.Monosulfide.Monosulfide
Hydrazone.Monosulfide
C1=NNCC1
C1=N[NH]CC1
C1=N[NH]CC1.c1ccccc1
Other
null
null
null
CCC1C=NNC1.CSC(=NS(=O)(=O)c1ccccc1Cl)SC>>CCC1C=NN(SC(C)=NS(=O)(=O)c2ccccc2Cl)C1
ord_dataset-03ba810b7f464a06b5d8787af2e8b64e
ord-ee39ee2d9b114f3a936d102e63da2c71
CCNC(=N)N1CC(CC)C=N1.O=S(=O)(Cl)c1cccc2nsnc12>>CCNC(=NS(=O)(=O)c1cccc2nsnc12)N1CC(CC)C=N1
Cl.C(C)C1C=NN(C1)C(=N)NCC.CCN(C(C)C)C(C)C.N1=C2C(=NS1)C(=CC=C2)S(=O)(=O)Cl>>C(C)NC(=NS(=O)(=O)C1=CC=CC=2C1=NSN2)N2N=CC(C2)CC
[CH3:1][CH2:2][NH:3][C:4](=[NH:5])[N:18]1[CH2:19][CH:20]([CH2:21][CH3:22])[CH:23]=[N:24]1.Cl[S:6](=[O:7])(=[O:8])[c:9]1[cH:10][cH:11][cH:12][c:13]2[n:14][s:15][n:16][c:17]12>>[CH3:1][CH2:2][NH:3][C:4](=[N:5][S:6](=[O:7])(=[O:8])[c:9]1[cH:10][cH:11][cH:12][c:13]2[n:14][s:15][n:16][c:17]12)[N:18]1[CH2:19][CH:20]([CH2:21]...
CCNC(=N)N1CC(CC)C=N1.O=S(=O)(Cl)c1cccc2nsnc12
CCNC(=NS(=O)(=O)c1cccc2nsnc12)N1CC(CC)C=N1
null
null
C(Cl)Cl
Miscellaneous
OtherReaction
65bd520d46095381b97cf2b1c808b198594dded087e2637f2dbe5add6a47838a
5f0d826ff827e7d94d07bc9ee74d0a88c79bcf75bb024f05043486e1cbe294bd
O=S(=O)(N=CN1CCC=N1)c1cccc2nsnc12
Cl-[S;H0;D4;+0:1](=[O;D1;H0:2])(=[O;D1;H0:3])-[c:4](:[c:5]):[c:6]1:[#7;a:7]:[#16;a:8]:[#7;a:9]:[c:10]:1.[#7:11]-[#7:12]-[C:13](-[#7:14])=[NH;D1;+0:15]>>[#7:11]-[#7:12]-[C:13](-[#7:14])=[N;H0;D2;+0:15]-[S;H0;D4;+0:1](=[O;D1;H0:2])(=[O;D1;H0:3])-[c:4](:[c:5]):[c:6]1:[#7;a:7]:[#16;a:8]:[#7;a:9]:[c:10]:1
84.7
[{"value": 84.7, "product": "C(C)NC(=NS(=O)(=O)C1=CC=CC=2C1=NSN2)N2N=CC(C2)CC", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
8
HOUR
300 mg 4,N-Diethyl-4,5-dihydro-pyrazole-1-carboxamidine hydrochloride was suspended in 10 mL DCM. 0.53 mL DiPEA and 310 mg benzo[1,2,5]thiadiazole-4-sulfonylchloride were added and the mixture was stirred overnight at room temperature. The mixture was washed with 5% NaHCO3 and 2 M NaOH, the organic layer dried over Na2...
10.6084/m9.figshare.5104873.v1
null
Sulfonyl halide
null
null
null
c1ccc2nsnc2c1.C1=N[NH]CC1
HCl
C(Cl)Cl
null
8
CCNC(=N)N1CC(CC)C=N1.O=S(=O)(Cl)c1cccc2nsnc12>C(Cl)Cl>CCNC(=NS(=O)(=O)c1cccc2nsnc12)N1CC(CC)C=N1
ord_dataset-03ba810b7f464a06b5d8787af2e8b64e
ord-f74a5cfdc3c645d594fa518fd94b6452
CCNC(=N)N1CC(C)(C)C=N1.O=S(=O)(Cl)c1cccc(Cl)c1>>CCNC(=NS(=O)(=O)c1cccc(Cl)c1)N1CC(C)(C)C=N1
Cl.C(C)NC(=N)N1N=CC(C1)(C)C.CCN(C(C)C)C(C)C.ClC=1C=C(C=CC1)S(=O)(=O)Cl>>ClC=1C=C(C=CC1)S(=O)(=O)N=C(NCC)N1N=CC(C1)(C)C
[CH3:1][CH2:2][NH:3][C:4](=[NH:5])[N:16]1[CH2:17][C:18]([CH3:19])([CH3:20])[CH:21]=[N:22]1.Cl[S:6](=[O:7])(=[O:8])[c:9]1[cH:10][cH:11][cH:12][c:13]([Cl:14])[cH:15]1>>[CH3:1][CH2:2][NH:3][C:4](=[N:5][S:6](=[O:7])(=[O:8])[c:9]1[cH:10][cH:11][cH:12][c:13]([Cl:14])[cH:15]1)[N:16]1[CH2:17][C:18]([CH3:19])([CH3:20])[CH:21]=[...
CCNC(=N)N1CC(C)(C)C=N1.O=S(=O)(Cl)c1cccc(Cl)c1
CCNC(=NS(=O)(=O)c1cccc(Cl)c1)N1CC(C)(C)C=N1
null
null
C(Cl)Cl
Miscellaneous
OtherReaction
65bd520d46095381b97cf2b1c808b198594dded087e2637f2dbe5add6a47838a
5f0d826ff827e7d94d07bc9ee74d0a88c79bcf75bb024f05043486e1cbe294bd
O=S(=O)(N=CN1CCC=N1)c1ccccc1
Cl-[S;H0;D4;+0:1](=[O;D1;H0:2])(=[O;D1;H0:3])-[c:4](:[c:5]):[c:6].[#7:7]-[#7:8]-[C:9](-[#7:10])=[NH;D1;+0:11]>>[#7:7]-[#7:8]-[C:9](-[#7:10])=[N;H0;D2;+0:11]-[S;H0;D4;+0:1](=[O;D1;H0:2])(=[O;D1;H0:3])-[c:4](:[c:5]):[c:6]
null
[]
null
null
20
HOUR
6.39 g N-Ethyl-4,4-dimethyl-4,5-dihydro-pyrazole-1-carboxamidine hydrochloride was suspended in 65 mL DCM. 12.0 mL DIPEA and 3.96 mL 3-chloro-benzenesulfonyl chloride were added and the suspension was stirred for 20 h. at room temperature, resulting in a dark brown turbid solution. The mixture was extracted with 2M NaO...
10.6084/m9.figshare.5104873.v1
null
Sulfonyl halide
null
null
null
c1ccccc1.C1=N[NH]CC1
HCl
C(Cl)Cl
null
20
CCNC(=N)N1CC(C)(C)C=N1.O=S(=O)(Cl)c1cccc(Cl)c1>C(Cl)Cl>CCNC(=NS(=O)(=O)c1cccc(Cl)c1)N1CC(C)(C)C=N1
ord_dataset-03ba810b7f464a06b5d8787af2e8b64e
ord-ec8adad63d0041a0969484598bc2e2fd
Cc1ccc(Br)cc1.[C-]#Cc1ccccc1>>Cc1ccc(C#Cc2ccccc2)cc1
BrC1=CC=C(C=C1)C.[Li+].[C-]#CC1=CC=CC=C1.O(C(C)C)B(OC(C)C)OC(C)C>>C1(=CC=C(C=C1)C#CC1=CC=CC=C1)C
Br[c:5]1[cH:4][cH:3][c:2]([CH3:1])[cH:15][cH:14]1.[C-:6]#[C:7][c:8]1[cH:9][cH:10][cH:11][cH:12][cH:13]1>>[CH3:1][c:2]1[cH:3][cH:4][c:5]([C:6]#[C:7][c:8]2[cH:9][cH:10][cH:11][cH:12][cH:13]2)[cH:14][cH:15]1
Cc1ccc(Br)cc1.[C-]#Cc1ccccc1
Cc1ccc(C#Cc2ccccc2)cc1
null
C=1C=CC(=CC1)[P](C=2C=CC=CC2)(C=3C=CC=CC3)[Pd]([P](C=4C=CC=CC4)(C=5C=CC=CC5)C=6C=CC=CC6)([P](C=7C=CC=CC7)(C=8C=CC=CC8)C=9C=CC=CC9)[P](C=1C=CC=CC1)(C=1C=CC=CC1)C=1C=CC=CC1
COCCOC.COCCOC.C1CCOC1
C-C Coupling
OtherReaction
93ae246e7c863443a3aaaa90941d39ebe932c135fc33ecf39310e65c58a9fbd3
1e016b25438ccc05198b60acd46c3be4f5258f827b14753e63a4bafcf188d801
C(#Cc1ccccc1)c1ccccc1
Br-[c;H0;D3;+0:1](:[c:2]:[c:3]):[c:4]:[c:5].[C-;H0;D1:6]#[C:7]-[c:8]>>[c:3]:[c:2]:[c;H0;D3;+0:1](-[C;H0;D2;+0:6]#[C:7]-[c:8]):[c:4]:[c:5]
null
[]
-78
CELSIUS
1.5
HOUR
General Procedure A. To a solution of lithium phenylacetylide (15.2 ml, 15.2 mmol) in DME (20 ml) under Argon at −78° C. was added triisopropoxylborane (3.5 ml, 15.2 mmol). The mixture was stirred at −78° C. for 1.5 hours. A solution of 1-bromo-4-methylbenzene (2 g, 11.7 mmol) in DME/THF (10 ml/10 ml) was degassed with...
10.6084/m9.figshare.5104873.v1
null
Aromatic halide
Alkyne
c1ccccc1
c1ccccc1
c1ccccc1.c1ccccc1
Br-
C=1C=CC(=CC1)[P](C=2C=CC=CC2)(C=3C=CC=CC3)[Pd]([P](C=4C=CC=CC4)(C=5C=CC=CC5)C=6C=CC=CC6)([P](C=7C=CC=CC7)(C=8C=CC=CC8)C=9C=CC=CC9)[P](C=1C=CC=CC1)(C=1C=CC=CC1)C=1C=CC=CC1.COCCOC.COCCOC.C1CCOC1
-78
1.5
Cc1ccc(Br)cc1.[C-]#Cc1ccccc1>C=1C=CC(=CC1)[P](C=2C=CC=CC2)(C=3C=CC=CC3)[Pd]([P](C=4C=CC=CC4)(C=5C=CC=CC5)C=6C=CC=CC6)([P](C=7C=CC=CC7)(C=8C=CC=CC8)C=9C=CC=CC9)[P](C=1C=CC=CC1)(C=1C=CC=CC1)C=1C=CC=CC1.COCCOC.COCCOC.C1CCOC1>Cc1ccc(C#Cc2ccccc2)cc1
ord_dataset-03ba810b7f464a06b5d8787af2e8b64e
ord-407ba34a62634895800105f14ad97f06
C=CN1CCCC1.CCOC(=O)c1nnc(-c2ccccc2)c(-c2ccccc2)n1.CCOC(=O)c1nnc(-c2ccccc2)c(-c2ccccc2)n1>>CCOC(=O)c1ccc(-c2ccccc2)c(-c2ccccc2)n1
C1(=CC=CC=C1)C=1N=C(N=NC1C1=CC=CC=C1)C(=O)OCC.C1(=CC=CC=C1)C=1N=C(N=NC1C1=CC=CC=C1)C(=O)OCC.C(=C)N1CCCC1.C(=C)N1CCCC1>>C1(=CC=CC=C1)C=1C=CC(=NC1C1=CC=CC=C1)C(=O)OCC
C(N1CCCC1)=[CH2:8].CCOC(=O)[c:7]1nnc(-c2ccccc2)c(-c2ccccc2)n1.n1n[c:9](-[c:10]2[cH:11][cH:12][cH:13][cH:14][cH:15]2)[c:16](-[c:17]2[cH:18][cH:19][cH:20][cH:21][cH:22]2)[n:23][c:6]1[C:4]([O:3][CH2:2][CH3:1])=[O:5]>>[CH3:1][CH2:2][O:3][C:4](=[O:5])[c:6]1[cH:7][cH:8][c:9](-[c:10]2[cH:11][cH:12][cH:13][cH:14][cH:15]2)[c:16...
C=CN1CCCC1.CCOC(=O)c1nnc(-c2ccccc2)c(-c2ccccc2)n1.CCOC(=O)c1nnc(-c2ccccc2)c(-c2ccccc2)n1
CCOC(=O)c1ccc(-c2ccccc2)c(-c2ccccc2)n1
null
null
C(Cl)(Cl)Cl
Miscellaneous
OtherReaction
cc03cad530703fa23e2ff0c67e0b9f19978525eb16d0ce01e888c853e60d70ca
c44d9ef0146168ac01b86e0d21b2b8ec8b64b9feba9682f4fc6d6e96c9b2417f
c1ccc(-c2cccnc2-c2ccccc2)cc1
C-C-O-C(=O)-[c;H0;D3;+0:1]1:n:n:c(-c2:c:c:c:c:c:2):c(-c2:c:c:c:c:c:2):n:1.[CH2;D1;+0:2]=C-N1-C-C-C-C-1.[C:3]-[#8:4]-[C:5](=[O;D1;H0:6])-[c;H0;D3;+0:7]1:[#7;a:8]:[c:9](-[c:10]):[c;H0;D3;+0:11](-[c:12](:[c:13]):[c:14]):n:n:1>>[C:3]-[#8:4]-[C:5](=[O;D1;H0:6])-[c;H0;D3;+0:7]1:[#7;a:8]:[c:9](-[c:10]):[c;H0;D3;+0:11](-[c:12]...
null
[]
null
null
null
null
General Procedure D. Ethyl 5,6-diphenyl-1,2,4-triazine-3-carboxylate (Compound 11, 200 mg, 0.66 mmol) and crude 1-vinylpyrrolidine (Compound 38, 2 g) in CHCl3 (20 ml) was heated at 75° C. overnight under nitrogen. The solvent was removed in vacuo, and the residue was purified by silica gel column chromatography (20% et...
10.6084/m9.figshare.5104873.v1
null
Enamine.Ester.Ester
Ester
C1CCNC1.c1cnncn1.c1ccccc1.c1ccccc1.c1cnncn1
c1ccncc1
c1ccncc1.c1ccccc1.c1ccccc1
HO-
C(Cl)(Cl)Cl
null
null
C=CN1CCCC1.CCOC(=O)c1nnc(-c2ccccc2)c(-c2ccccc2)n1.CCOC(=O)c1nnc(-c2ccccc2)c(-c2ccccc2)n1>C(Cl)(Cl)Cl>CCOC(=O)c1ccc(-c2ccccc2)c(-c2ccccc2)n1
ord_dataset-03ba810b7f464a06b5d8787af2e8b64e
ord-0eef4f474e3b4844a43a01518b3416ad
C=CN1CCCC1.CCOC(=O)c1nnc(-c2ccc(C)cc2)c(-c2ccccc2)n1.CCOC(=O)c1nnc(-c2ccc(C)cc2)c(-c2ccccc2)n1>>CCOC(=O)c1ccc(-c2ccc(C)cc2)c(-c2ccccc2)n1
C(=C)N1CCCC1.C1(=CC=CC=C1)C=1N=C(N=NC1C1=CC=C(C=C1)C)C(=O)OCC.C1(=CC=CC=C1)C=1N=C(N=NC1C1=CC=C(C=C1)C)C(=O)OCC.C(=C)N1CCCC1>>C1(=CC=CC=C1)C1=C(C=CC(=N1)C(=O)OCC)C1=CC=C(C=C1)C
C(N1CCCC1)=[CH2:8].CCOC(=O)[c:7]1nnc(-c2ccc(C)cc2)c(-c2ccccc2)n1.n1n[c:9](-[c:10]2[cH:11][cH:12][c:13]([CH3:14])[cH:15][cH:16]2)[c:17](-[c:18]2[cH:19][cH:20][cH:21][cH:22][cH:23]2)[n:24][c:6]1[C:4]([O:3][CH2:2][CH3:1])=[O:5]>>[CH3:1][CH2:2][O:3][C:4](=[O:5])[c:6]1[cH:7][cH:8][c:9](-[c:10]2[cH:11][cH:12][c:13]([CH3:14])...
C=CN1CCCC1.CCOC(=O)c1nnc(-c2ccc(C)cc2)c(-c2ccccc2)n1.CCOC(=O)c1nnc(-c2ccc(C)cc2)c(-c2ccccc2)n1
CCOC(=O)c1ccc(-c2ccc(C)cc2)c(-c2ccccc2)n1
null
null
C(Cl)(Cl)Cl
Miscellaneous
OtherReaction
cc03cad530703fa23e2ff0c67e0b9f19978525eb16d0ce01e888c853e60d70ca
c44d9ef0146168ac01b86e0d21b2b8ec8b64b9feba9682f4fc6d6e96c9b2417f
c1ccc(-c2cccnc2-c2ccccc2)cc1
C-C-O-C(=O)-[c;H0;D3;+0:1]1:n:n:c(-c2:c:c:c(-C):c:c:2):c(-c2:c:c:c:c:c:2):n:1.[CH2;D1;+0:2]=C-N1-C-C-C-C-1.[C:3]-[#8:4]-[C:5](=[O;D1;H0:6])-[c;H0;D3;+0:7]1:[#7;a:8]:[c:9](-[c:10]):[c;H0;D3;+0:11](-[c:12](:[c:13]):[c:14]):n:n:1>>[C:3]-[#8:4]-[C:5](=[O;D1;H0:6])-[c;H0;D3;+0:7]1:[#7;a:8]:[c:9](-[c:10]):[c;H0;D3;+0:11](-[c...
null
[]
null
null
null
null
Following General Procedure D, ethyl 5-phenyl-6-p-tolyl-1,2,4-triazine-3-carboxylate (Compound 12, 177 mg, 0.56 mmol) and crude 1-vinylpyrrolidine (Compound 38, 730 mg) in CHCl3 (10 ml) were reacted to produce the title compound as a yellow solid. Conditions: See reaction.notes.procedure_details. Workup: were reacted
10.6084/m9.figshare.5104873.v1
null
Enamine.Ester.Ester
Ester
C1CCNC1.c1cnncn1.c1ccccc1.c1ccccc1.c1cnncn1
c1ccncc1
c1ccncc1.c1ccccc1.c1ccccc1
HO-
C(Cl)(Cl)Cl
null
null
C=CN1CCCC1.CCOC(=O)c1nnc(-c2ccc(C)cc2)c(-c2ccccc2)n1.CCOC(=O)c1nnc(-c2ccc(C)cc2)c(-c2ccccc2)n1>C(Cl)(Cl)Cl>CCOC(=O)c1ccc(-c2ccc(C)cc2)c(-c2ccccc2)n1
ord_dataset-03ba810b7f464a06b5d8787af2e8b64e
ord-ff9619e76cab447082841ad9a3fd4058
C=CN1CCCC1.CCOC(=O)c1nnc(-c2ccc(CC)cc2)c(-c2ccccc2)n1.CCOC(=O)c1nnc(-c2ccc(CC)cc2)c(-c2ccccc2)n1>>CCOC(=O)c1ccc(-c2ccc(CC)cc2)c(-c2ccccc2)n1
C(=C)N1CCCC1.C(C)C1=CC=C(C=C1)C1=C(N=C(N=N1)C(=O)OCC)C1=CC=CC=C1.C(C)C1=CC=C(C=C1)C1=C(N=C(N=N1)C(=O)OCC)C1=CC=CC=C1.C(=C)N1CCCC1>>C(C)C1=CC=C(C=C1)C=1C=CC(=NC1C1=CC=CC=C1)C(=O)OCC
C(N1CCCC1)=[CH2:8].CCOC(=O)[c:7]1nnc(-c2ccc(CC)cc2)c(-c2ccccc2)n1.n1n[c:9](-[c:10]2[cH:11][cH:12][c:13]([CH2:14][CH3:15])[cH:16][cH:17]2)[c:18](-[c:19]2[cH:20][cH:21][cH:22][cH:23][cH:24]2)[n:25][c:6]1[C:4]([O:3][CH2:2][CH3:1])=[O:5]>>[CH3:1][CH2:2][O:3][C:4](=[O:5])[c:6]1[cH:7][cH:8][c:9](-[c:10]2[cH:11][cH:12][c:13](...
C=CN1CCCC1.CCOC(=O)c1nnc(-c2ccc(CC)cc2)c(-c2ccccc2)n1.CCOC(=O)c1nnc(-c2ccc(CC)cc2)c(-c2ccccc2)n1
CCOC(=O)c1ccc(-c2ccc(CC)cc2)c(-c2ccccc2)n1
null
null
C(Cl)(Cl)Cl
Miscellaneous
OtherReaction
cc03cad530703fa23e2ff0c67e0b9f19978525eb16d0ce01e888c853e60d70ca
c44d9ef0146168ac01b86e0d21b2b8ec8b64b9feba9682f4fc6d6e96c9b2417f
c1ccc(-c2cccnc2-c2ccccc2)cc1
C-C-O-C(=O)-[c;H0;D3;+0:1]1:n:n:c(-c2:c:c:c(-C-C):c:c:2):c(-c2:c:c:c:c:c:2):n:1.[CH2;D1;+0:2]=C-N1-C-C-C-C-1.[C:3]-[#8:4]-[C:5](=[O;D1;H0:6])-[c;H0;D3;+0:7]1:[#7;a:8]:[c:9](-[c:10]):[c;H0;D3;+0:11](-[c:12](:[c:13]):[c:14]):n:n:1>>[C:3]-[#8:4]-[C:5](=[O;D1;H0:6])-[c;H0;D3;+0:7]1:[#7;a:8]:[c:9](-[c:10]):[c;H0;D3;+0:11](-...
null
[]
null
null
null
null
Following General Procedure D, ethyl 6-(4-ethyl-phenyl)-5-phenyl-1,2,4-triazine-3-carboxylate (Compound 13, 105 mg, 0.30 mmol) and crude 1-vinylpyrrolidine (Compound 38, 2 g) in CHCl3 (10 ml) were reacted to produce the title compound as a yellow solid. Conditions: See reaction.notes.procedure_details. Workup: were rea...
10.6084/m9.figshare.5104873.v1
null
Enamine.Ester.Ester
Ester
C1CCNC1.c1cnncn1.c1ccccc1.c1ccccc1.c1cnncn1
c1ccncc1
c1ccncc1.c1ccccc1.c1ccccc1
HO-
C(Cl)(Cl)Cl
null
null
C=CN1CCCC1.CCOC(=O)c1nnc(-c2ccc(CC)cc2)c(-c2ccccc2)n1.CCOC(=O)c1nnc(-c2ccc(CC)cc2)c(-c2ccccc2)n1>C(Cl)(Cl)Cl>CCOC(=O)c1ccc(-c2ccc(CC)cc2)c(-c2ccccc2)n1
ord_dataset-03ba810b7f464a06b5d8787af2e8b64e
ord-cd87c93174394e969ed9ef7c43a800f7
CCCc1ccc(-c2nnc(C(=O)OCC)nc2-c2ccccc2)cc1.CCCc1ccc(-c2nnc(C(=O)OCC)nc2-c2ccccc2)cc1>>CCCc1ccc(-c2ccc(C(=O)OCC)nc2-c2ccccc2)cc1
C(=C)N1CCCC1.C1(=CC=CC=C1)C=1N=C(N=NC1C1=CC=C(C=C1)CCC)C(=O)OCC.C1(=CC=CC=C1)C=1N=C(N=NC1C1=CC=C(C=C1)CCC)C(=O)OCC.C(=C)N1CCCC1>>C1(=CC=CC=C1)C1=C(C=CC(=N1)C(=O)OCC)C1=CC=C(C=C1)CCC
CCCc1ccc(-[c:9]2nnc(C(=O)OCC)n[c:10]2-c2ccccc2)cc1.n1n[c:11]([C:12](=[O:13])[O:14][CH2:15][CH3:16])[n:17][c:18](-[c:19]2[cH:20][cH:21][cH:22][cH:23][cH:24]2)[c:8]1-[c:7]1[cH:6][cH:5][c:4]([CH2:3][CH2:2][CH3:1])[cH:26][cH:25]1>>[CH3:1][CH2:2][CH2:3][c:4]1[cH:5][cH:6][c:7](-[c:8]2[cH:9][cH:10][c:11]([C:12](=[O:13])[O:14]...
CCCc1ccc(-c2nnc(C(=O)OCC)nc2-c2ccccc2)cc1.CCCc1ccc(-c2nnc(C(=O)OCC)nc2-c2ccccc2)cc1
CCCc1ccc(-c2ccc(C(=O)OCC)nc2-c2ccccc2)cc1
null
null
C(Cl)(Cl)Cl
Miscellaneous
OtherReaction
15307b4243fc59c3c55c0a3c2481a190773671ebbfd60320f0f5af2fc3174896
24fd1d274a00b1436d72a65f7e271c768760ea40f563c2d852f3767e29b17299
c1ccc(-c2cccnc2-c2ccccc2)cc1
C-C-C-c1:c:c:c(-[c;H0;D3;+0:1]2:n:n:c(-C(=O)-O-C-C):n:[c;H0;D3;+0:2]:2-c2:c:c:c:c:c:2):c:c:1.[C:3]-[#8:4]-[C:5](=[O;D1;H0:6])-[c;H0;D3;+0:7]1:[#7;a:8]:[c:9](-[c:10]):[c;H0;D3;+0:11](-[c:12](:[c:13]):[c:14]):n:n:1>>[C:3]-[#8:4]-[C:5](=[O;D1;H0:6])-[c;H0;D3;+0:7]1:[#7;a:8]:[c:9](-[c:10]):[c;H0;D3;+0:11](-[c:12](:[c:13]):...
null
[]
null
null
null
null
Following General Procedure D, ethyl 5-phenyl-6-(4-propyl-phenyl)-1,2,4-triazine-3-carboxylate (Compound 14), (153 mg, 0.46 mmol) and crude 1-vinylpyrrolidine (Compound 38, 2 g) in CHCl3 (10 ml) were reacted to produce the title compound as a yellow oil. Conditions: See reaction.notes.procedure_details. Workup: were re...
10.6084/m9.figshare.5104873.v1
null
Ester.Ester
Ester
c1ccccc1.c1cnncn1.c1ccccc1.c1cnncn1
c1ccncc1
c1ccccc1.c1ccncc1.c1ccccc1
HO-
C(Cl)(Cl)Cl
null
null
CCCc1ccc(-c2nnc(C(=O)OCC)nc2-c2ccccc2)cc1.CCCc1ccc(-c2nnc(C(=O)OCC)nc2-c2ccccc2)cc1>C(Cl)(Cl)Cl>CCCc1ccc(-c2ccc(C(=O)OCC)nc2-c2ccccc2)cc1
ord_dataset-03ba810b7f464a06b5d8787af2e8b64e
ord-e1ca332375e44a608fce6d0a24b1e328
C=CN1CCCC1.CCOC(=O)c1nnc(-c2ccc(C(F)(F)F)cc2)c(-c2ccccc2)n1.CCOC(=O)c1nnc(-c2ccc(C(F)(F)F)cc2)c(-c2ccccc2)n1>>CCOC(=O)c1ccc(-c2ccc(C(F)(F)F)cc2)c(-c2ccccc2)n1
C(=C)N1CCCC1.FC(C1=CC=C(C=C1)C1=C(N=C(N=N1)C(=O)OCC)C1=CC=CC=C1)(F)F.FC(C1=CC=C(C=C1)C1=C(N=C(N=N1)C(=O)OCC)C1=CC=CC=C1)(F)F.C(=C)N1CCCC1>>C1(=CC=CC=C1)C1=C(C=CC(=N1)C(=O)OCC)C1=CC=C(C=C1)C(F)(F)F
C(N1CCCC1)=[CH2:8].CCOC(=O)[c:7]1nnc(-c2ccc(C(F)(F)F)cc2)c(-c2ccccc2)n1.n1n[c:9](-[c:10]2[cH:11][cH:12][c:13]([C:14]([F:15])([F:16])[F:17])[cH:18][cH:19]2)[c:20](-[c:21]2[cH:22][cH:23][cH:24][cH:25][cH:26]2)[n:27][c:6]1[C:4]([O:3][CH2:2][CH3:1])=[O:5]>>[CH3:1][CH2:2][O:3][C:4](=[O:5])[c:6]1[cH:7][cH:8][c:9](-[c:10]2[cH...
C=CN1CCCC1.CCOC(=O)c1nnc(-c2ccc(C(F)(F)F)cc2)c(-c2ccccc2)n1.CCOC(=O)c1nnc(-c2ccc(C(F)(F)F)cc2)c(-c2ccccc2)n1
CCOC(=O)c1ccc(-c2ccc(C(F)(F)F)cc2)c(-c2ccccc2)n1
null
null
C(Cl)(Cl)Cl
Miscellaneous
OtherReaction
e9dfcd7c4eaea72cbb32ccdf8b372fa29303834ed6ac6018661ae51fed4a4375
3edf262b85949dbd66d1bedc6bc75ff796f878143fa1d6dae97be6b12e5ca0aa
c1ccc(-c2cccnc2-c2ccccc2)cc1
C-C-O-C(=O)-[c;H0;D3;+0:1]1:n:n:c(-c2:c:c:c(-C(-F)(-F)-F):c:c:2):c(-c2:c:c:c:c:c:2):n:1.[CH2;D1;+0:2]=C-N1-C-C-C-C-1.[C:3]-[#8:4]-[C:5](=[O;D1;H0:6])-[c;H0;D3;+0:7]1:[#7;a:8]:[c:9](-[c:10]):[c;H0;D3;+0:11](-[c:12](:[c:13]):[c:14]):n:n:1>>[C:3]-[#8:4]-[C:5](=[O;D1;H0:6])-[c;H0;D3;+0:7]1:[#7;a:8]:[c:9](-[c:10]):[c;H0;D3;...
null
[]
null
null
null
null
Following General Procedure D, ethyl 6-(4-trifluoromethylphenyl)-5-phenyl-1,2,4-triazine-3-carboxylate (Compound 15), (378 mg, 1.01 mmol) and crude 1-vinylpyrrolidine (Compound 38, 780 mg) in CHCl3 (10 ml) were reacted to produce the title compound as a yellow oil. Conditions: See reaction.notes.procedure_details. Work...
10.6084/m9.figshare.5104873.v1
null
Enamine.Trifluoro group.Ester.Ester
Ester
C1CCNC1.c1cnncn1.c1ccccc1.c1ccccc1.c1cnncn1
c1ccncc1
c1ccncc1.c1ccccc1.c1ccccc1
HF
C(Cl)(Cl)Cl
null
null
C=CN1CCCC1.CCOC(=O)c1nnc(-c2ccc(C(F)(F)F)cc2)c(-c2ccccc2)n1.CCOC(=O)c1nnc(-c2ccc(C(F)(F)F)cc2)c(-c2ccccc2)n1>C(Cl)(Cl)Cl>CCOC(=O)c1ccc(-c2ccc(C(F)(F)F)cc2)c(-c2ccccc2)n1
ord_dataset-03ba810b7f464a06b5d8787af2e8b64e
ord-d5e75070b7ad48b4b69add6eef67c8a6
CCOC(=O)c1nnc(-c2ccc(CC)cc2)c(-c2ccccc2)n1.CCOC(=O)c1nnc(-c2ccc(CC)cc2)c(-c2ccccc2)n1>>CCOC(=O)c1nc(-c2ccccc2)c(-c2ccc(CC)cc2)cc1C
C(=CC)N1CCCC1.C(C)C1=CC=C(C=C1)C1=C(N=C(N=N1)C(=O)OCC)C1=CC=CC=C1.C(C)C1=CC=C(C=C1)C1=C(N=C(N=N1)C(=O)OCC)C1=CC=CC=C1.C(=CC)N1CCCC1>>C(C)C1=CC=C(C=C1)C=1C=C(C(=NC1C1=CC=CC=C1)C(=O)OCC)C
n1n[c:15](-[c:16]2[cH:17][cH:18][c:19]([CH2:20][CH3:21])[cH:22][cH:23]2)[c:8](-[c:9]2[cH:10][cH:11][cH:12][cH:13][cH:14]2)[n:7][c:6]1[C:4]([O:3][CH2:2][CH3:1])=[O:5].CCO[C:26](=O)[c:25]1nnc(-c2ccc(CC)cc2)c(-c2ccccc2)n1>>[CH3:1][CH2:2][O:3][C:4](=[O:5])[c:6]1[n:7][c:8](-[c:9]2[cH:10][cH:11][cH:12][cH:13][cH:14]2)[c:15](...
CCOC(=O)c1nnc(-c2ccc(CC)cc2)c(-c2ccccc2)n1.CCOC(=O)c1nnc(-c2ccc(CC)cc2)c(-c2ccccc2)n1
CCOC(=O)c1nc(-c2ccccc2)c(-c2ccc(CC)cc2)cc1C
null
null
C(Cl)(Cl)Cl
Miscellaneous
OtherReaction
15307b4243fc59c3c55c0a3c2481a190773671ebbfd60320f0f5af2fc3174896
24fd1d274a00b1436d72a65f7e271c768760ea40f563c2d852f3767e29b17299
c1ccc(-c2cccnc2-c2ccccc2)cc1
C-C-O-[C;H0;D3;+0:1](=O)-[c;H0;D3;+0:2]1:n:n:c(-c2:c:c:c(-C-C):c:c:2):c(-c2:c:c:c:c:c:2):n:1.[C:3]-[#8:4]-[C:5](=[O;D1;H0:6])-[c;H0;D3;+0:7]1:[#7;a:8]:[c:9](-[c:10]):[c;H0;D3;+0:11](-[c:12](:[c:13]):[c:14]):n:n:1>>[C:3]-[#8:4]-[C:5](=[O;D1;H0:6])-[c;H0;D3;+0:7]1:[#7;a:8]:[c:9](-[c:10]):[c;H0;D3;+0:11](-[c:12](:[c:13]):...
null
[]
null
null
null
null
Following General Procedure D, ethyl 6-(4-ethylphenyl)-5-phenyl-1,2,4-triazine-3-carboxylate (Compound 13, 200 mg, 0.60 mmol) and crude 1-propenyl-pyrrolidine (Compound 39, 2 g) in CHCl3 (10 ml) were reacted to produce the title compound as a yellow oil. Conditions: See reaction.notes.procedure_details. Workup: were re...
10.6084/m9.figshare.5104873.v1
null
Ester.Ester
Ester
c1cnncn1.c1cnncn1.c1ccccc1.c1ccccc1
c1ccncc1
c1ccncc1.c1ccccc1.c1ccccc1
HO-
C(Cl)(Cl)Cl
null
null
CCOC(=O)c1nnc(-c2ccc(CC)cc2)c(-c2ccccc2)n1.CCOC(=O)c1nnc(-c2ccc(CC)cc2)c(-c2ccccc2)n1>C(Cl)(Cl)Cl>CCOC(=O)c1nc(-c2ccccc2)c(-c2ccc(CC)cc2)cc1C
ord_dataset-03ba810b7f464a06b5d8787af2e8b64e
ord-2411d3daac3b49a7a31ba7c021abc1c4
C=CN1CCCC1.CCOC(=O)c1nnc(-c2ccccc2)c(-c2ccc(C)cc2)n1.CCOC(=O)c1nnc(-c2ccccc2)c(-c2ccc(C)cc2)n1>>CCOC(=O)c1ccc(-c2ccccc2)c(-c2ccc(C)cc2)n1
C(=C)N1CCCC1.C1(=CC=CC=C1)C1=C(N=C(N=N1)C(=O)OCC)C1=CC=C(C=C1)C.C1(=CC=CC=C1)C1=C(N=C(N=N1)C(=O)OCC)C1=CC=C(C=C1)C.C(=C)N1CCCC1>>C1(=CC=CC=C1)C=1C=CC(=NC1C1=CC=C(C=C1)C)C(=O)OCC
C(N1CCCC1)=[CH2:8].CCOC(=O)[c:7]1nnc(-c2ccccc2)c(-c2ccc(C)cc2)n1.n1n[c:9](-[c:10]2[cH:11][cH:12][cH:13][cH:14][cH:15]2)[c:16](-[c:17]2[cH:18][cH:19][c:20]([CH3:21])[cH:22][cH:23]2)[n:24][c:6]1[C:4]([O:3][CH2:2][CH3:1])=[O:5]>>[CH3:1][CH2:2][O:3][C:4](=[O:5])[c:6]1[cH:7][cH:8][c:9](-[c:10]2[cH:11][cH:12][cH:13][cH:14][c...
C=CN1CCCC1.CCOC(=O)c1nnc(-c2ccccc2)c(-c2ccc(C)cc2)n1.CCOC(=O)c1nnc(-c2ccccc2)c(-c2ccc(C)cc2)n1
CCOC(=O)c1ccc(-c2ccccc2)c(-c2ccc(C)cc2)n1
null
null
C(Cl)(Cl)Cl
Miscellaneous
OtherReaction
cc03cad530703fa23e2ff0c67e0b9f19978525eb16d0ce01e888c853e60d70ca
c44d9ef0146168ac01b86e0d21b2b8ec8b64b9feba9682f4fc6d6e96c9b2417f
c1ccc(-c2cccnc2-c2ccccc2)cc1
C-C-O-C(=O)-[c;H0;D3;+0:1]1:n:n:c(-c2:c:c:c:c:c:2):c(-c2:c:c:c(-C):c:c:2):n:1.[CH2;D1;+0:2]=C-N1-C-C-C-C-1.[C:3]-[#8:4]-[C:5](=[O;D1;H0:6])-[c;H0;D3;+0:7]1:[#7;a:8]:[c:9](-[c:10]):[c;H0;D3;+0:11](-[c:12](:[c:13]):[c:14]):n:n:1>>[C:3]-[#8:4]-[C:5](=[O;D1;H0:6])-[c;H0;D3;+0:7]1:[#7;a:8]:[c:9](-[c:10]):[c;H0;D3;+0:11](-[c...
null
[]
null
null
null
null
Following General Procedure D, ethyl 6-phenyl-5-p-tolyl-1,2,4-triazine-3-carboxylate (Compound 17, 361 mg, 1.13 mmol) and crude 1-vinylpyrrolidine (Compound 38, 806 mg) in CHCl3 (10 ml) were reacted to produce the title compound as a yellow oil. Conditions: See reaction.notes.procedure_details. Workup: were reacted
10.6084/m9.figshare.5104873.v1
null
Enamine.Ester.Ester
Ester
C1CCNC1.c1cnncn1.c1ccccc1.c1ccccc1.c1cnncn1
c1ccncc1
c1ccncc1.c1ccccc1.c1ccccc1
HO-
C(Cl)(Cl)Cl
null
null
C=CN1CCCC1.CCOC(=O)c1nnc(-c2ccccc2)c(-c2ccc(C)cc2)n1.CCOC(=O)c1nnc(-c2ccccc2)c(-c2ccc(C)cc2)n1>C(Cl)(Cl)Cl>CCOC(=O)c1ccc(-c2ccccc2)c(-c2ccc(C)cc2)n1
ord_dataset-03ba810b7f464a06b5d8787af2e8b64e
ord-562ae536f62e4b34b4aefe73e07bb20a
C=CN1CCCC1.CCOC(=O)c1nnc(-c2ccccc2)c(-c2ccc(CC)cc2)n1.CCOC(=O)c1nnc(-c2ccccc2)c(-c2ccc(CC)cc2)n1>>CCOC(=O)c1ccc(-c2ccccc2)c(-c2ccc(CC)cc2)n1
C(=C)N1CCCC1.C(C)C1=CC=C(C=C1)C=1N=C(N=NC1C1=CC=CC=C1)C(=O)OCC.C(C)C1=CC=C(C=C1)C=1N=C(N=NC1C1=CC=CC=C1)C(=O)OCC.C(=C)N1CCCC1>>C(C)C1=CC=C(C=C1)C1=C(C=CC(=N1)C(=O)OCC)C1=CC=CC=C1
C(N1CCCC1)=[CH2:8].CCOC(=O)[c:7]1nnc(-c2ccccc2)c(-c2ccc(CC)cc2)n1.n1n[c:9](-[c:10]2[cH:11][cH:12][cH:13][cH:14][cH:15]2)[c:16](-[c:17]2[cH:18][cH:19][c:20]([CH2:21][CH3:22])[cH:23][cH:24]2)[n:25][c:6]1[C:4]([O:3][CH2:2][CH3:1])=[O:5]>>[CH3:1][CH2:2][O:3][C:4](=[O:5])[c:6]1[cH:7][cH:8][c:9](-[c:10]2[cH:11][cH:12][cH:13]...
C=CN1CCCC1.CCOC(=O)c1nnc(-c2ccccc2)c(-c2ccc(CC)cc2)n1.CCOC(=O)c1nnc(-c2ccccc2)c(-c2ccc(CC)cc2)n1
CCOC(=O)c1ccc(-c2ccccc2)c(-c2ccc(CC)cc2)n1
null
null
C(Cl)(Cl)Cl
Miscellaneous
OtherReaction
cc03cad530703fa23e2ff0c67e0b9f19978525eb16d0ce01e888c853e60d70ca
c44d9ef0146168ac01b86e0d21b2b8ec8b64b9feba9682f4fc6d6e96c9b2417f
c1ccc(-c2cccnc2-c2ccccc2)cc1
C-C-O-C(=O)-[c;H0;D3;+0:1]1:n:n:c(-c2:c:c:c:c:c:2):c(-c2:c:c:c(-C-C):c:c:2):n:1.[CH2;D1;+0:2]=C-N1-C-C-C-C-1.[C:3]-[#8:4]-[C:5](=[O;D1;H0:6])-[c;H0;D3;+0:7]1:[#7;a:8]:[c:9](-[c:10]):[c;H0;D3;+0:11](-[c:12](:[c:13]):[c:14]):n:n:1>>[C:3]-[#8:4]-[C:5](=[O;D1;H0:6])-[c;H0;D3;+0:7]1:[#7;a:8]:[c:9](-[c:10]):[c;H0;D3;+0:11](-...
null
[]
null
null
null
null
Following General Procedure D, ethyl 5-(4-ethylphenyl)-6-phenyl-1,2,4-triazine-3-carboxylate (Compound 18, 245 mg, 0.74 mmol) and crude 1-vinylpyrrolidine (Compound 38, 572 mg) in CHCl3 (10 ml) were reacted to produce the title compound as a yellow oil. Conditions: See reaction.notes.procedure_details. Workup: were rea...
10.6084/m9.figshare.5104873.v1
null
Enamine.Ester.Ester
Ester
C1CCNC1.c1cnncn1.c1ccccc1.c1ccccc1.c1cnncn1
c1ccncc1
c1ccncc1.c1ccccc1.c1ccccc1
HO-
C(Cl)(Cl)Cl
null
null
C=CN1CCCC1.CCOC(=O)c1nnc(-c2ccccc2)c(-c2ccc(CC)cc2)n1.CCOC(=O)c1nnc(-c2ccccc2)c(-c2ccc(CC)cc2)n1>C(Cl)(Cl)Cl>CCOC(=O)c1ccc(-c2ccccc2)c(-c2ccc(CC)cc2)n1
ord_dataset-03ba810b7f464a06b5d8787af2e8b64e
ord-44b6bfd75d794d3281b750bfa16d6f38
C=CN1CCCC1.CCOC(=O)c1nnc(-c2ccccc2)c(-c2ccc(C(F)(F)F)cc2)n1.CCOC(=O)c1nnc(-c2ccccc2)c(-c2ccc(C(F)(F)F)cc2)n1>>CCOC(=O)c1ccc(-c2ccccc2)c(-c2ccc(C(F)(F)F)cc2)n1
C(=C)N1CCCC1.FC(C1=CC=C(C=C1)C=1N=C(N=NC1C1=CC=CC=C1)C(=O)OCC)(F)F.FC(C1=CC=C(C=C1)C=1N=C(N=NC1C1=CC=CC=C1)C(=O)OCC)(F)F.C(=C)N1CCCC1>>C1(=CC=CC=C1)C=1C=CC(=NC1C1=CC=C(C=C1)C(F)(F)F)C(=O)OCC
C(N1CCCC1)=[CH2:8].CCOC(=O)[c:7]1nnc(-c2ccccc2)c(-c2ccc(C(F)(F)F)cc2)n1.n1n[c:9](-[c:10]2[cH:11][cH:12][cH:13][cH:14][cH:15]2)[c:16](-[c:17]2[cH:18][cH:19][c:20]([C:21]([F:22])([F:23])[F:24])[cH:25][cH:26]2)[n:27][c:6]1[C:4]([O:3][CH2:2][CH3:1])=[O:5]>>[CH3:1][CH2:2][O:3][C:4](=[O:5])[c:6]1[cH:7][cH:8][c:9](-[c:10]2[cH...
C=CN1CCCC1.CCOC(=O)c1nnc(-c2ccccc2)c(-c2ccc(C(F)(F)F)cc2)n1.CCOC(=O)c1nnc(-c2ccccc2)c(-c2ccc(C(F)(F)F)cc2)n1
CCOC(=O)c1ccc(-c2ccccc2)c(-c2ccc(C(F)(F)F)cc2)n1
null
null
C(Cl)(Cl)Cl
Miscellaneous
OtherReaction
e9dfcd7c4eaea72cbb32ccdf8b372fa29303834ed6ac6018661ae51fed4a4375
3edf262b85949dbd66d1bedc6bc75ff796f878143fa1d6dae97be6b12e5ca0aa
c1ccc(-c2cccnc2-c2ccccc2)cc1
C-C-O-C(=O)-[c;H0;D3;+0:1]1:n:n:c(-c2:c:c:c:c:c:2):c(-c2:c:c:c(-C(-F)(-F)-F):c:c:2):n:1.[CH2;D1;+0:2]=C-N1-C-C-C-C-1.[C:3]-[#8:4]-[C:5](=[O;D1;H0:6])-[c;H0;D3;+0:7]1:[#7;a:8]:[c:9](-[c:10]):[c;H0;D3;+0:11](-[c:12](:[c:13]):[c:14]):n:n:1>>[C:3]-[#8:4]-[C:5](=[O;D1;H0:6])-[c;H0;D3;+0:7]1:[#7;a:8]:[c:9](-[c:10]):[c;H0;D3;...
null
[]
null
null
null
null
Following General Procedure D, ethyl 5-(4-trifluoromethylphenyl)-6-phenyl-1,2,4-triazine-3-carboxylate (Compound 19, 1 g, 2.68 mmol) and crude 1-vinylpyrrolidine (Compound 38, 1.4 g) in CHCl3 (20 ml) were reacted to produce the title compound as a yellow oil. Conditions: See reaction.notes.procedure_details. Workup: we...
10.6084/m9.figshare.5104873.v1
null
Enamine.Trifluoro group.Ester.Ester
Ester
C1CCNC1.c1cnncn1.c1ccccc1.c1ccccc1.c1cnncn1
c1ccncc1
c1ccncc1.c1ccccc1.c1ccccc1
HF
C(Cl)(Cl)Cl
null
null
C=CN1CCCC1.CCOC(=O)c1nnc(-c2ccccc2)c(-c2ccc(C(F)(F)F)cc2)n1.CCOC(=O)c1nnc(-c2ccccc2)c(-c2ccc(C(F)(F)F)cc2)n1>C(Cl)(Cl)Cl>CCOC(=O)c1ccc(-c2ccccc2)c(-c2ccc(C(F)(F)F)cc2)n1
ord_dataset-03ba810b7f464a06b5d8787af2e8b64e
ord-c8ed5a439c8346ba9a574f8b0447231e
CCOC(=O)c1ccc(-c2ccccc2)c(-c2ccccc2)n1>>COC(=O)c1ccc(-c2ccccc2)c(-c2ccccc2)n1
C1(=CC=CC=C1)C=1C=CC(=NC1C1=CC=CC=C1)C(=O)OCC.C1(=CC=CC=C1)C=1C=CC(=NC1C1=CC=CC=C1)C(=O)OCC>>C1(=CC=CC=C1)C=1C=CC(=NC1C1=CC=CC=C1)C(=O)OC
C[CH2:1][O:2][C:3](=[O:4])[c:5]1[cH:6][cH:7][c:8](-[c:9]2[cH:10][cH:11][cH:12][cH:13][cH:14]2)[c:15](-[c:16]2[cH:17][cH:18][cH:19][cH:20][cH:21]2)[n:22]1>>[CH3:1][O:2][C:3](=[O:4])[c:5]1[cH:6][cH:7][c:8](-[c:9]2[cH:10][cH:11][cH:12][cH:13][cH:14]2)[c:15](-[c:16]2[cH:17][cH:18][cH:19][cH:20][cH:21]2)[n:22]1
CCOC(=O)c1ccc(-c2ccccc2)c(-c2ccccc2)n1
COC(=O)c1ccc(-c2ccccc2)c(-c2ccccc2)n1
null
OS(=O)(=O)O
CO.O
Miscellaneous
Transesterification
797948efc8975454230354c6926ef43459a60311d668503c7a6b6bcdb3eafe50
6ad95641ddc9be155108cd2297ce15bcd8cb0ca25c68bfc4fce3cbf5009a236a
c1ccc(-c2cccnc2-c2ccccc2)cc1
C-[CH2;D2;+0:1]-[#8:2]-[C:3](=[O;D1;H0:4])-[c:5]:[#7;a:6]>>[#7;a:6]:[c:5]-[C:3](=[O;D1;H0:4])-[#8:2]-[CH3;D1;+0:1]
null
[]
null
null
null
null
General Procedure E. A solution of ethyl 5,6-diphenylpyridine-2-carboxylate (Compound 21, 30 mg, 0.1 mmol) and conc. H2SO4 (3 drops) in MeOH (5 ml) was heated at 50° C. overnight. The mixture was diluted with water, and the products were extracted with ethyl acetate. The organic layer was washed with water and brine, a...
10.6084/m9.figshare.5104873.v1
null
Ester
Ester
null
null
c1ccncc1.c1ccccc1.c1ccccc1
Other
OS(=O)(=O)O.CO.O
null
null
CCOC(=O)c1ccc(-c2ccccc2)c(-c2ccccc2)n1>OS(=O)(=O)O.CO.O>COC(=O)c1ccc(-c2ccccc2)c(-c2ccccc2)n1
ord_dataset-03ba810b7f464a06b5d8787af2e8b64e
ord-3bbe9e8d5be141679a7e56b70fc93128
CCOC(=O)c1ccc(-c2ccc(C)cc2)c(-c2ccccc2)n1>>COC(=O)c1ccc(-c2ccc(C)cc2)c(-c2ccccc2)n1
C1(=CC=CC=C1)C1=C(C=CC(=N1)C(=O)OCC)C1=CC=C(C=C1)C.C1(=CC=CC=C1)C1=C(C=CC(=N1)C(=O)OCC)C1=CC=C(C=C1)C>>C1(=CC=CC=C1)C1=C(C=CC(=N1)C(=O)OC)C1=CC=C(C=C1)C
C[CH2:1][O:2][C:3](=[O:4])[c:5]1[cH:6][cH:7][c:8](-[c:9]2[cH:10][cH:11][c:12]([CH3:13])[cH:14][cH:15]2)[c:16](-[c:17]2[cH:18][cH:19][cH:20][cH:21][cH:22]2)[n:23]1>>[CH3:1][O:2][C:3](=[O:4])[c:5]1[cH:6][cH:7][c:8](-[c:9]2[cH:10][cH:11][c:12]([CH3:13])[cH:14][cH:15]2)[c:16](-[c:17]2[cH:18][cH:19][cH:20][cH:21][cH:22]2)[n...
CCOC(=O)c1ccc(-c2ccc(C)cc2)c(-c2ccccc2)n1
COC(=O)c1ccc(-c2ccc(C)cc2)c(-c2ccccc2)n1
null
OS(=O)(=O)O
CO
Miscellaneous
Transesterification
797948efc8975454230354c6926ef43459a60311d668503c7a6b6bcdb3eafe50
6ad95641ddc9be155108cd2297ce15bcd8cb0ca25c68bfc4fce3cbf5009a236a
c1ccc(-c2cccnc2-c2ccccc2)cc1
C-[CH2;D2;+0:1]-[#8:2]-[C:3](=[O;D1;H0:4])-[c:5]:[#7;a:6]>>[#7;a:6]:[c:5]-[C:3](=[O;D1;H0:4])-[#8:2]-[CH3;D1;+0:1]
null
[]
null
null
null
null
Following General Procedure E, ethyl 6-phenyl-5-p-tolyl-pyridine-2-carboxylate (Compound 22, 70 mg, 0.22 mmol) and conc. H2SO4 (3 drops) in MeOH (3 ml) were reacted to produce the title compound as a yellow solid. Conditions: See reaction.notes.procedure_details. Workup: were reacted
10.6084/m9.figshare.5104873.v1
null
Ester
Ester
null
null
c1ccncc1.c1ccccc1.c1ccccc1
Other
OS(=O)(=O)O.CO
null
null
CCOC(=O)c1ccc(-c2ccc(C)cc2)c(-c2ccccc2)n1>OS(=O)(=O)O.CO>COC(=O)c1ccc(-c2ccc(C)cc2)c(-c2ccccc2)n1
ord_dataset-03ba810b7f464a06b5d8787af2e8b64e
ord-c8f862b8d57b4ed5a6bad16f2966582d
CCOC(=O)c1ccc(-c2ccc(CC)cc2)c(-c2ccccc2)n1>>CCc1ccc(-c2ccc(C(=O)OC)nc2-c2ccccc2)cc1
C(C)C1=CC=C(C=C1)C=1C=CC(=NC1C1=CC=CC=C1)C(=O)OCC.C(C)C1=CC=C(C=C1)C=1C=CC(=NC1C1=CC=CC=C1)C(=O)OCC>>C(C)C1=CC=C(C=C1)C=1C=CC(=NC1C1=CC=CC=C1)C(=O)OC
C[CH2:14][O:13][C:11]([c:10]1[cH:9][cH:8][c:7](-[c:6]2[cH:5][cH:4][c:3]([CH2:2][CH3:1])[cH:24][cH:23]2)[c:16](-[c:17]2[cH:18][cH:19][cH:20][cH:21][cH:22]2)[n:15]1)=[O:12]>>[CH3:1][CH2:2][c:3]1[cH:4][cH:5][c:6](-[c:7]2[cH:8][cH:9][c:10]([C:11](=[O:12])[O:13][CH3:14])[n:15][c:16]2-[c:17]2[cH:18][cH:19][cH:20][cH:21][cH:2...
CCOC(=O)c1ccc(-c2ccc(CC)cc2)c(-c2ccccc2)n1
CCc1ccc(-c2ccc(C(=O)OC)nc2-c2ccccc2)cc1
null
OS(=O)(=O)O
CO
Miscellaneous
Transesterification
797948efc8975454230354c6926ef43459a60311d668503c7a6b6bcdb3eafe50
6ad95641ddc9be155108cd2297ce15bcd8cb0ca25c68bfc4fce3cbf5009a236a
c1ccc(-c2cccnc2-c2ccccc2)cc1
C-[CH2;D2;+0:1]-[#8:2]-[C:3](=[O;D1;H0:4])-[c:5]:[#7;a:6]>>[#7;a:6]:[c:5]-[C:3](=[O;D1;H0:4])-[#8:2]-[CH3;D1;+0:1]
null
[]
null
null
null
null
Following General Procedure E, ethyl 5-(4-ethylphenyl)-6-phenylpyridine-2-carboxylate (Compound 23, 45 mg, 0.15 mmol) and conc. H2SO4 (3 drops) in MeOH (3 ml) were reacted to produce title compound as a yellow solid. Conditions: See reaction.notes.procedure_details. Workup: were reacted
10.6084/m9.figshare.5104873.v1
null
Ester
Ester
null
null
c1ccccc1.c1ccncc1.c1ccccc1
Other
OS(=O)(=O)O.CO
null
null
CCOC(=O)c1ccc(-c2ccc(CC)cc2)c(-c2ccccc2)n1>OS(=O)(=O)O.CO>CCc1ccc(-c2ccc(C(=O)OC)nc2-c2ccccc2)cc1
ord_dataset-03ba810b7f464a06b5d8787af2e8b64e
ord-096060c9f0dd4d369daa7a6032a8f907
CCCc1ccc(-c2ccc(C(=O)OCC)nc2-c2ccccc2)cc1>>CCCc1ccc(-c2ccc(C(=O)OC)nc2-c2ccccc2)cc1
C1(=CC=CC=C1)C1=C(C=CC(=N1)C(=O)OCC)C1=CC=C(C=C1)CCC.C1(=CC=CC=C1)C1=C(C=CC(=N1)C(=O)OCC)C1=CC=C(C=C1)CCC>>C1(=CC=CC=C1)C1=C(C=CC(=N1)C(=O)OC)C1=CC=C(C=C1)CCC
C[CH2:15][O:14][C:12]([c:11]1[cH:10][cH:9][c:8](-[c:7]2[cH:6][cH:5][c:4]([CH2:3][CH2:2][CH3:1])[cH:25][cH:24]2)[c:17](-[c:18]2[cH:19][cH:20][cH:21][cH:22][cH:23]2)[n:16]1)=[O:13]>>[CH3:1][CH2:2][CH2:3][c:4]1[cH:5][cH:6][c:7](-[c:8]2[cH:9][cH:10][c:11]([C:12](=[O:13])[O:14][CH3:15])[n:16][c:17]2-[c:18]2[cH:19][cH:20][cH...
CCCc1ccc(-c2ccc(C(=O)OCC)nc2-c2ccccc2)cc1
CCCc1ccc(-c2ccc(C(=O)OC)nc2-c2ccccc2)cc1
null
OS(=O)(=O)O
CO
Miscellaneous
Transesterification
797948efc8975454230354c6926ef43459a60311d668503c7a6b6bcdb3eafe50
6ad95641ddc9be155108cd2297ce15bcd8cb0ca25c68bfc4fce3cbf5009a236a
c1ccc(-c2cccnc2-c2ccccc2)cc1
C-[CH2;D2;+0:1]-[#8:2]-[C:3](=[O;D1;H0:4])-[c:5]:[#7;a:6]>>[#7;a:6]:[c:5]-[C:3](=[O;D1;H0:4])-[#8:2]-[CH3;D1;+0:1]
null
[]
null
null
null
null
Following General Procedure E, ethyl 6-phenyl-5-(4-propylphenyl)-pyridine-2-carboxylate (Compound 24, 67 mg, 0.19 mmol) and conc. H2SO4 (3 drops) in MeOH (3 ml) were reacted to produce the title compound as a white solid. Conditions: See reaction.notes.procedure_details. Workup: were reacted
10.6084/m9.figshare.5104873.v1
null
Ester
Ester
null
null
c1ccccc1.c1ccncc1.c1ccccc1
Other
OS(=O)(=O)O.CO
null
null
CCCc1ccc(-c2ccc(C(=O)OCC)nc2-c2ccccc2)cc1>OS(=O)(=O)O.CO>CCCc1ccc(-c2ccc(C(=O)OC)nc2-c2ccccc2)cc1
ord_dataset-03ba810b7f464a06b5d8787af2e8b64e
ord-c1134c48fb9443239d86e6435989bfb3
CCOC(=O)c1ccc(-c2ccc(C(F)(F)F)cc2)c(-c2ccccc2)n1>>COC(=O)c1ccc(-c2ccc(C(F)(F)F)cc2)c(-c2ccccc2)n1
C1(=CC=CC=C1)C1=C(C=CC(=N1)C(=O)OCC)C1=CC=C(C=C1)C(F)(F)F.C1(=CC=CC=C1)C1=C(C=CC(=N1)C(=O)OCC)C1=CC=C(C=C1)C(F)(F)F>>C1(=CC=CC=C1)C1=C(C=CC(=N1)C(=O)OC)C1=CC=C(C=C1)C(F)(F)F
C[CH2:1][O:2][C:3](=[O:4])[c:5]1[cH:6][cH:7][c:8](-[c:9]2[cH:10][cH:11][c:12]([C:13]([F:14])([F:15])[F:16])[cH:17][cH:18]2)[c:19](-[c:20]2[cH:21][cH:22][cH:23][cH:24][cH:25]2)[n:26]1>>[CH3:1][O:2][C:3](=[O:4])[c:5]1[cH:6][cH:7][c:8](-[c:9]2[cH:10][cH:11][c:12]([C:13]([F:14])([F:15])[F:16])[cH:17][cH:18]2)[c:19](-[c:20]...
CCOC(=O)c1ccc(-c2ccc(C(F)(F)F)cc2)c(-c2ccccc2)n1
COC(=O)c1ccc(-c2ccc(C(F)(F)F)cc2)c(-c2ccccc2)n1
null
OS(=O)(=O)O
CO
Miscellaneous
Transesterification
797948efc8975454230354c6926ef43459a60311d668503c7a6b6bcdb3eafe50
6ad95641ddc9be155108cd2297ce15bcd8cb0ca25c68bfc4fce3cbf5009a236a
c1ccc(-c2cccnc2-c2ccccc2)cc1
C-[CH2;D2;+0:1]-[#8:2]-[C:3](=[O;D1;H0:4])-[c:5]:[#7;a:6]>>[#7;a:6]:[c:5]-[C:3](=[O;D1;H0:4])-[#8:2]-[CH3;D1;+0:1]
null
[]
null
null
null
null
Following General Procedure E, ethyl 6-phenyl-5-(4-trifluoromethylphenyl)-pyridine-2-carboxylate (Compound 25, 110 mg, 0.29 mmol) and conc. H2SO4 (5 drops) in MeOH (5 ml) were reacted to produce the title compound as a white solid. Conditions: See reaction.notes.procedure_details. Workup: were reacted
10.6084/m9.figshare.5104873.v1
null
Ester
Ester
null
null
c1ccncc1.c1ccccc1.c1ccccc1
Other
OS(=O)(=O)O.CO
null
null
CCOC(=O)c1ccc(-c2ccc(C(F)(F)F)cc2)c(-c2ccccc2)n1>OS(=O)(=O)O.CO>COC(=O)c1ccc(-c2ccc(C(F)(F)F)cc2)c(-c2ccccc2)n1
ord_dataset-03ba810b7f464a06b5d8787af2e8b64e
ord-3748fd020f36428fb4e075cc855cf526
CCOC(=O)c1ccc(-c2ccccc2)c(-c2ccc(C(F)(F)F)cc2)n1>>COC(=O)c1ccc(-c2ccccc2)c(-c2ccc(C(F)(F)F)cc2)n1
C1(=CC=CC=C1)C=1C=CC(=NC1C1=CC=C(C=C1)C(F)(F)F)C(=O)OCC.C1(=CC=CC=C1)C=1C=CC(=NC1C1=CC=C(C=C1)C(F)(F)F)C(=O)OCC>>C1(=CC=CC=C1)C=1C=CC(=NC1C1=CC=C(C=C1)C(F)(F)F)C(=O)OC
C[CH2:1][O:2][C:3](=[O:4])[c:5]1[cH:6][cH:7][c:8](-[c:9]2[cH:10][cH:11][cH:12][cH:13][cH:14]2)[c:15](-[c:16]2[cH:17][cH:18][c:19]([C:20]([F:21])([F:22])[F:23])[cH:24][cH:25]2)[n:26]1>>[CH3:1][O:2][C:3](=[O:4])[c:5]1[cH:6][cH:7][c:8](-[c:9]2[cH:10][cH:11][cH:12][cH:13][cH:14]2)[c:15](-[c:16]2[cH:17][cH:18][c:19]([C:20](...
CCOC(=O)c1ccc(-c2ccccc2)c(-c2ccc(C(F)(F)F)cc2)n1
COC(=O)c1ccc(-c2ccccc2)c(-c2ccc(C(F)(F)F)cc2)n1
null
OS(=O)(=O)O
CO
Miscellaneous
Transesterification
797948efc8975454230354c6926ef43459a60311d668503c7a6b6bcdb3eafe50
6ad95641ddc9be155108cd2297ce15bcd8cb0ca25c68bfc4fce3cbf5009a236a
c1ccc(-c2cccnc2-c2ccccc2)cc1
C-[CH2;D2;+0:1]-[#8:2]-[C:3](=[O;D1;H0:4])-[c:5]:[#7;a:6]>>[#7;a:6]:[c:5]-[C:3](=[O;D1;H0:4])-[#8:2]-[CH3;D1;+0:1]
null
[]
null
null
null
null
Following General Procedure E, ethyl 5-phenyl-6-(4-trifluoromethylphenyl)-pyridine-2-carboxylate (Compound 29, 103 mg, 0.28 mmol) and conc. H2SO4 (5 drops) in MeOH (5 ml) were reacted to produce the title compound as a white solid. Conditions: See reaction.notes.procedure_details. Workup: were reacted
10.6084/m9.figshare.5104873.v1
null
Ester
Ester
null
null
c1ccncc1.c1ccccc1.c1ccccc1
Other
OS(=O)(=O)O.CO
null
null
CCOC(=O)c1ccc(-c2ccccc2)c(-c2ccc(C(F)(F)F)cc2)n1>OS(=O)(=O)O.CO>COC(=O)c1ccc(-c2ccccc2)c(-c2ccc(C(F)(F)F)cc2)n1
ord_dataset-03ba810b7f464a06b5d8787af2e8b64e
ord-ad10b7d5192549c796b757eb7bdd7792
CCOC(=O)c1nc(-c2ccccc2)c(-c2ccc(CC)cc2)cc1C>>CCc1ccc(-c2cc(C)c(C(=O)OC)nc2-c2ccccc2)cc1
C(C)C1=CC=C(C=C1)C=1C=C(C(=NC1C1=CC=CC=C1)C(=O)OCC)C.C(C)C1=CC=C(C=C1)C=1C=C(C(=NC1C1=CC=CC=C1)C(=O)OCC)C>>C(C)C1=CC=C(C=C1)C=1C=C(C(=NC1C1=CC=CC=C1)C(=O)OC)C
C[CH2:15][O:14][C:12]([c:11]1[c:9]([CH3:10])[cH:8][c:7](-[c:6]2[cH:5][cH:4][c:3]([CH2:2][CH3:1])[cH:25][cH:24]2)[c:17](-[c:18]2[cH:19][cH:20][cH:21][cH:22][cH:23]2)[n:16]1)=[O:13]>>[CH3:1][CH2:2][c:3]1[cH:4][cH:5][c:6](-[c:7]2[cH:8][c:9]([CH3:10])[c:11]([C:12](=[O:13])[O:14][CH3:15])[n:16][c:17]2-[c:18]2[cH:19][cH:20][...
CCOC(=O)c1nc(-c2ccccc2)c(-c2ccc(CC)cc2)cc1C
CCc1ccc(-c2cc(C)c(C(=O)OC)nc2-c2ccccc2)cc1
null
OS(=O)(=O)O
CO
Miscellaneous
Transesterification
797948efc8975454230354c6926ef43459a60311d668503c7a6b6bcdb3eafe50
6ad95641ddc9be155108cd2297ce15bcd8cb0ca25c68bfc4fce3cbf5009a236a
c1ccc(-c2cccnc2-c2ccccc2)cc1
C-[CH2;D2;+0:1]-[#8:2]-[C:3](=[O;D1;H0:4])-[c:5]:[#7;a:6]>>[#7;a:6]:[c:5]-[C:3](=[O;D1;H0:4])-[#8:2]-[CH3;D1;+0:1]
null
[]
null
null
null
null
Following General Procedure E, ethyl 5-(4-ethylphenyl)-3-methyl-6-phenylpyridine-2-carboxylate (Compound 26, 29 mg, 0.08 mmol) and conc. H2SO4 (3 drops) in MeOH (5 ml) were reacted to produce the title compound as an oil. Conditions: See reaction.notes.procedure_details. Workup: were reacted
10.6084/m9.figshare.5104873.v1
null
Ester
Ester
null
null
c1ccccc1.c1ccncc1.c1ccccc1
Other
OS(=O)(=O)O.CO
null
null
CCOC(=O)c1nc(-c2ccccc2)c(-c2ccc(CC)cc2)cc1C>OS(=O)(=O)O.CO>CCc1ccc(-c2cc(C)c(C(=O)OC)nc2-c2ccccc2)cc1
ord_dataset-03ba810b7f464a06b5d8787af2e8b64e
ord-cf4765e907dc45d8ae8032e5ff92a776
CCc1ccc(C=CC(=O)O)cc1>>CCc1ccc(/C=C/CO)cc1
[BH4-].[Na+].ClC(=O)OCC.C(C)C1=CC=C(C=CC(=O)O)C=C1.C(C)N(CC)CC.Cl>>C(C)C1=CC=C(C=C1)/C=C/CO
O=[C:9]([CH:8]=[CH:7][c:6]1[cH:5][cH:4][c:3]([CH2:2][CH3:1])[cH:12][cH:11]1)[OH:10]>>[CH3:1][CH2:2][c:3]1[cH:4][cH:5][c:6](/[CH:7]=[CH:8]/[CH2:9][OH:10])[cH:11][cH:12]1
CCc1ccc(C=CC(=O)O)cc1
CCc1ccc(/C=C/CO)cc1
null
null
C1CCOC1.O
Reduction
Reduction of carboxylic acid to primary alcohol
0db83a5ebe1e318b78b55461cf7eb8f7c004eef0f9e3b6666d3df4c96b5f665e
93b4621647b04d2ad2f2825215b1567f171ba61fe10d136b5db6ea0470aa4932
c1ccccc1
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
30
MINUTE
General Procedure G. A solution of ethyl chloroformate (1.1 ml, 11.4 mmol) in THF (5 ml) was added to a solution of 4-ethylcinnamic acid (2 g, 11.4 mmol) and triethylamine (1.6 ml, 11.4 mmol) in THF (50 ml) at −5° C. to −10° C., and the solution was stirred for 30 min. The resulting white precipitate was filtered off, ...
10.6084/m9.figshare.5104873.v1
null
Carboxylic acid
Primary alcohol
null
null
c1ccccc1
Other
C1CCOC1.O
null
0.5
CCc1ccc(C=CC(=O)O)cc1>C1CCOC1.O>CCc1ccc(/C=C/CO)cc1
ord_dataset-03ba810b7f464a06b5d8787af2e8b64e
ord-af09d11aafed42f59438f29d90dc1f26
CCc1ccc(/C=C/CO)cc1>>CCc1ccc(/C=C/C=O)cc1
C(C)C1=CC=C(C=C1)/C=C/CO.C(C(=O)Cl)(=O)Cl.CS(=O)C.C(C)N(CC)CC.C(C)C1=CC=C(C=C1)/C=C/CO>>C(C)C1=CC=C(C=C1)/C=C/C=O
[CH3:1][CH2:2][c:3]1[cH:4][cH:5][c:6](/[CH:7]=[CH:8]/[CH2:9][OH:10])[cH:11][cH:12]1>>[CH3:1][CH2:2][c:3]1[cH:4][cH:5][c:6](/[CH:7]=[CH:8]/[CH:9]=[O:10])[cH:11][cH:12]1
CCc1ccc(/C=C/CO)cc1
CCc1ccc(/C=C/C=O)cc1
null
null
C(Cl)Cl
Oxidation
Oxidation or Dehydrogenation of Alcohols to Aldehydes and Ketones
41bfa9deea81b465c88ad21fdfb64a2e1ba29490558cf430df132cb98b4a538b
0a03c6724c1862e8f86d4a463afda55b8e067dc6cb42597b472eb7cabc03eda3
c1ccccc1
[OH;D1;+0:1]-[CH2;D2;+0:2]/[C:3]=[C:4]/[c:5](:[c:6]):[c:7]>>[O;H0;D1;+0:1]=[CH;D2;+0:2]/[C:3]=[C:4]/[c:5](:[c:6]):[c:7]
null
[]
null
null
1
HOUR
General Procedure H. To a solution of oxalyl chloride (5.9 ml, 11.8 mmol, 2 M in CH2Cl2) in CH2Cl2 (20 ml) was added a solution of DMSO (1.1 ml, 15.7 mmol) in CH2Cl2 (3 ml) dropwise at −60° C. A solution of (E)-3-(4-ethylphenyl)prop-2-en-1-ol (Compound 40, 1.3 g, 7.8 mmol) in CH2Cl2 (5 ml) was cannulated slowly into th...
10.6084/m9.figshare.5104873.v1
null
Primary alcohol
Aldehyde
null
null
c1ccccc1
null
C(Cl)Cl
null
1
CCc1ccc(/C=C/CO)cc1>C(Cl)Cl>CCc1ccc(/C=C/C=O)cc1
ord_dataset-03ba810b7f464a06b5d8787af2e8b64e
ord-ff46d30221ab41f09c751f2de95c3f11
Cc1ccc(/C=C/CO)cc1>>Cc1ccc(/C=C/C=O)cc1
CC1=CC=C(C=C1)/C=C/CO.C(C(=O)Cl)(=O)Cl.CS(=O)C.C(C)N(CC)CC.CC1=CC=C(C=C1)/C=C/CO>>CC1=CC=C(C=C1)/C=C/C=O
[CH3:1][c:2]1[cH:3][cH:4][c:5](/[CH:6]=[CH:7]/[CH2:8][OH:9])[cH:10][cH:11]1>>[CH3:1][c:2]1[cH:3][cH:4][c:5](/[CH:6]=[CH:7]/[CH:8]=[O:9])[cH:10][cH:11]1
Cc1ccc(/C=C/CO)cc1
Cc1ccc(/C=C/C=O)cc1
null
null
C(Cl)Cl
Oxidation
Oxidation or Dehydrogenation of Alcohols to Aldehydes and Ketones
41bfa9deea81b465c88ad21fdfb64a2e1ba29490558cf430df132cb98b4a538b
0a03c6724c1862e8f86d4a463afda55b8e067dc6cb42597b472eb7cabc03eda3
c1ccccc1
[OH;D1;+0:1]-[CH2;D2;+0:2]/[C:3]=[C:4]/[c:5](:[c:6]):[c:7]>>[O;H0;D1;+0:1]=[CH;D2;+0:2]/[C:3]=[C:4]/[c:5](:[c:6]):[c:7]
null
[]
null
null
null
null
Following General Procedure H, oxalyl chloride (7.1 ml, 14.2 mmol, 2 M in CH2Cl2), DMSO (1.3 ml, 18.9 mmol), (E)-3-(4-methylphenyl)prop-2-en-1-ol (Compound 41, 1.4 g, 9.5 mmol) and triethylamine (4.4 ml, 31.4 mmol) in CH2Cl2 (5 ml) were reacted to obtain the title compound as an oil. Conditions: See reaction.notes.proc...
10.6084/m9.figshare.5104873.v1
null
Primary alcohol
Aldehyde
null
null
c1ccccc1
null
C(Cl)Cl
null
null
Cc1ccc(/C=C/CO)cc1>C(Cl)Cl>Cc1ccc(/C=C/C=O)cc1
ord_dataset-03ba810b7f464a06b5d8787af2e8b64e
ord-b4766f87ad664e35965873e1b072eb02
CCOC(=O)CN=[N+]=[N-].Cc1ccc(/C=C/C=O)cc1>>CCOC(=O)/C(=C/C=C/c1ccc(C)cc1)N=[N+]=[N-]
CC[O-].[Na+].CC1=CC=C(C=C1)/C=C/C=O.CC1=CC=C(C=C1)/C=C/C=O.N(=[N+]=[N-])CC(=O)OCC>>N(=[N+]=[N-])\C(\C(=O)OCC)=C/C=C/C1=CC=C(C=C1)C
[CH3:1][CH2:2][O:3][C:4](=[O:5])[CH2:6][N:17]=[N+:18]=[N-:19].O=[CH:7]/[CH:8]=[CH:9]/[c:10]1[cH:11][cH:12][c:13]([CH3:14])[cH:15][cH:16]1>>[CH3:1][CH2:2][O:3][C:4](=[O:5])/[C:6](=[CH:7]/[CH:8]=[CH:9]/[c:10]1[cH:11][cH:12][c:13]([CH3:14])[cH:15][cH:16]1)[N:17]=[N+:18]=[N-:19]
CCOC(=O)CN=[N+]=[N-].Cc1ccc(/C=C/C=O)cc1
CCOC(=O)/C(=C/C=C/c1ccc(C)cc1)N=[N+]=[N-]
null
null
CCO.C(C)O
C-C Coupling
Aldol condensation
96b579ff44c0fff4089c750910104cf990e0a287e373b67fd8e70fc60e740467
5d53f2f0eebc91d0a27a3fff71d2085564fbedea85248d599c79f507c8d10a9e
c1ccccc1
O=[CH;D2;+0:1]/[C:2]=[C:3]/[c:4](:[c:5]):[c:6].[C:7]-[#8:8]-[C:9](=[O;D1;H0:10])-[CH2;D2;+0:11]-[#7:12]=[#7;+:13]=[N;-;D1;H0:14]>>[C:7]-[#8:8]-[C:9](=[O;D1;H0:10])/[C;H0;D3;+0:11](-[#7:12]=[#7;+:13]=[N;-;D1;H0:14])=[CH;D2;+0:1]/[C:2]=[C:3]/[c:4](:[c:5]):[c:6]
null
[]
null
null
null
null
Following General Procedure I, a 1.38 M solution of NaOEt in ethanol (30 ml), (E)-3-(4-methylphenyl)acrylaldehyde (Compound 43, 1.1 g, 7.5 mmol) and ethyl azidoacetate (12 ml, 37.5 mmol) in EtOH (20 ml) were reacted to produce the title compound as a solid. Conditions: See reaction.notes.procedure_details.
10.6084/m9.figshare.5104873.v1
null
Aldehyde.Ester
Ester.Conjugated diene
null
null
c1ccccc1
HO-
CCO.C(C)O
null
null
CCOC(=O)CN=[N+]=[N-].Cc1ccc(/C=C/C=O)cc1>CCO.C(C)O>CCOC(=O)/C(=C/C=C/c1ccc(C)cc1)N=[N+]=[N-]
ord_dataset-03ba810b7f464a06b5d8787af2e8b64e
ord-a6ee2b9eb8ae41b1997326c72ac4001b
CCOC(=O)/C(=C/C=C/c1ccc(CC)cc1)N=[N+]=[N-].c1ccc(P(c2ccccc2)c2ccccc2)cc1>>CCOC(=O)C(=CC=Cc1ccc(CC)cc1)N=P(c1ccccc1)(c1ccccc1)c1ccccc1
C1(=CC=CC=C1)P(C1=CC=CC=C1)C1=CC=CC=C1.N(=[N+]=[N-])\C(\C(=O)OCC)=C/C=C/C1=CC=C(C=C1)CC.N(=[N+]=[N-])\C(\C(=O)OCC)=C/C=C/C1=CC=C(C=C1)CC>>C(C)OC(=O)C(N=P(C1=CC=CC=C1)(C1=CC=CC=C1)C1=CC=CC=C1)=CC=CC1=CC=C(C=C1)CC
[N-]=[N+]=[N:18]/[C:6]([C:4]([O:3][CH2:2][CH3:1])=[O:5])=[CH:7]\[CH:8]=[CH:9]\[c:10]1[cH:11][cH:12][c:13]([CH2:14][CH3:15])[cH:16][cH:17]1.[P:19]([c:20]1[cH:21][cH:22][cH:23][cH:24][cH:25]1)([c:26]1[cH:27][cH:28][cH:29][cH:30][cH:31]1)[c:32]1[cH:33][cH:34][cH:35][cH:36][cH:37]1>>[CH3:1][CH2:2][O:3][C:4](=[O:5])[C:6](=[...
CCOC(=O)/C(=C/C=C/c1ccc(CC)cc1)N=[N+]=[N-].c1ccc(P(c2ccccc2)c2ccccc2)cc1
CCOC(=O)C(=CC=Cc1ccc(CC)cc1)N=P(c1ccccc1)(c1ccccc1)c1ccccc1
null
null
C(C)OCC
Miscellaneous
OtherReaction
ccc2663030541127fcaca4e5acedd9f2784c38c6800cb643e7bb4815d3139521
fbd691a01e95e68b66bf8b0666f72e0c6d7102c3827b8153721b6e3b4f7ca6d9
C(C=Cc1ccccc1)=CN=P(c1ccccc1)(c1ccccc1)c1ccccc1
[C:1]-[#8:2]-[C:3](=[O;D1;H0:4])/[C:5](=[C:6]/[C:7]=[C:8]/[c:9])-[N;H0;D2;+0:10]=[N+]=[N-].[c:11]:[c:12](-[P;H0;D3;+0:13](-[c:14](:[c:15]):[c:16])-[c:17](:[c:18]):[c:19]):[c:20]>>[C:1]-[#8:2]-[C:3](=[O;D1;H0:4])-[C:5](=[C:6]-[C:7]=[C:8]-[c:9])-[N;H0;D2;+0:10]=[P;H0;D4;+0:13](-[c:12](:[c:11]):[c:20])(-[c:14](:[c:15]):[c...
null
[]
null
null
12
HOUR
General Procedure J. A solution of triphenylphosphine (1.2 g, 4.54 mmol) in diethyl ether (10 ml) was added dropwise to a solution of ethyl (2Z,4E)-2-azido-5-(4-ethylphenyl)penta-2,4-dienoate (Compound 44, 1.2 g, 4.54 mmol) in diethyl ether (20 ml) at 0° C. The solution was stirred for 12 hours at room temperature. Eva...
10.6084/m9.figshare.5104873.v1
null
Azide
null
null
null
c1ccccc1.c1ccccc1.c1ccccc1.c1ccccc1
Other
C(C)OCC
null
12
CCOC(=O)/C(=C/C=C/c1ccc(CC)cc1)N=[N+]=[N-].c1ccc(P(c2ccccc2)c2ccccc2)cc1>C(C)OCC>CCOC(=O)C(=CC=Cc1ccc(CC)cc1)N=P(c1ccccc1)(c1ccccc1)c1ccccc1
ord_dataset-03ba810b7f464a06b5d8787af2e8b64e
ord-6b70e7d8fcb74f30a6fe09540ac7d36f
CCOC(=O)/C(=C/C=C/c1ccc(C)cc1)N=[N+]=[N-].c1ccc(P(c2ccccc2)c2ccccc2)cc1>>CCOC(=O)C(=CC=Cc1ccc(C)cc1)N=P(c1ccccc1)(c1ccccc1)c1ccccc1
C1(=CC=CC=C1)P(C1=CC=CC=C1)C1=CC=CC=C1.N(=[N+]=[N-])\C(\C(=O)OCC)=C/C=C/C1=CC=C(C=C1)C>>C(C)OC(=O)C(N=P(C1=CC=CC=C1)(C1=CC=CC=C1)C1=CC=CC=C1)=CC=CC1=CC=C(C=C1)C
[N-]=[N+]=[N:17]/[C:6]([C:4]([O:3][CH2:2][CH3:1])=[O:5])=[CH:7]\[CH:8]=[CH:9]\[c:10]1[cH:11][cH:12][c:13]([CH3:14])[cH:15][cH:16]1.[P:18]([c:19]1[cH:20][cH:21][cH:22][cH:23][cH:24]1)([c:25]1[cH:26][cH:27][cH:28][cH:29][cH:30]1)[c:31]1[cH:32][cH:33][cH:34][cH:35][cH:36]1>>[CH3:1][CH2:2][O:3][C:4](=[O:5])[C:6](=[CH:7][CH...
CCOC(=O)/C(=C/C=C/c1ccc(C)cc1)N=[N+]=[N-].c1ccc(P(c2ccccc2)c2ccccc2)cc1
CCOC(=O)C(=CC=Cc1ccc(C)cc1)N=P(c1ccccc1)(c1ccccc1)c1ccccc1
null
null
C(C)OCC
Miscellaneous
OtherReaction
ccc2663030541127fcaca4e5acedd9f2784c38c6800cb643e7bb4815d3139521
fbd691a01e95e68b66bf8b0666f72e0c6d7102c3827b8153721b6e3b4f7ca6d9
C(C=Cc1ccccc1)=CN=P(c1ccccc1)(c1ccccc1)c1ccccc1
[C:1]-[#8:2]-[C:3](=[O;D1;H0:4])/[C:5](=[C:6]/[C:7]=[C:8]/[c:9])-[N;H0;D2;+0:10]=[N+]=[N-].[c:11]:[c:12](-[P;H0;D3;+0:13](-[c:14](:[c:15]):[c:16])-[c:17](:[c:18]):[c:19]):[c:20]>>[C:1]-[#8:2]-[C:3](=[O;D1;H0:4])-[C:5](=[C:6]-[C:7]=[C:8]-[c:9])-[N;H0;D2;+0:10]=[P;H0;D4;+0:13](-[c:12](:[c:11]):[c:20])(-[c:14](:[c:15]):[c...
null
[]
null
null
null
null
Following General Procedure J, triphenylphosphine (1.5 g, 5.8 mmol) ethyl (2Z,4E)-2-azido-5-(4-methylphenyl)penta-2,4-dienoate (Compound 45, 1.5 g, 5.8 mmol) in diethyl ether (50 ml) were reacted to produce the title compound as a yellow solid. Conditions: See reaction.notes.procedure_details. Workup: were reacted
10.6084/m9.figshare.5104873.v1
null
Azide
null
null
null
c1ccccc1.c1ccccc1.c1ccccc1.c1ccccc1
Other
C(C)OCC
null
null
CCOC(=O)/C(=C/C=C/c1ccc(C)cc1)N=[N+]=[N-].c1ccc(P(c2ccccc2)c2ccccc2)cc1>C(C)OCC>CCOC(=O)C(=CC=Cc1ccc(C)cc1)N=P(c1ccccc1)(c1ccccc1)c1ccccc1
ord_dataset-03ba810b7f464a06b5d8787af2e8b64e
ord-12e19353160e48d3b4cc4a7e27d8621c
CCOC(=O)C(=CC=Cc1ccc(CC)cc1)N=P(c1ccccc1)(c1ccccc1)c1ccccc1.O=Cc1ccc(C(F)(F)F)cc1>>CCOC(=O)c1ccc(-c2ccc(CC)cc2)c(-c2ccc(C(F)(F)F)cc2)n1
FC(C1=CC=C(C=O)C=C1)(F)F.C(C)OC(=O)C(N=P(C1=CC=CC=C1)(C1=CC=CC=C1)C1=CC=CC=C1)=CC=CC1=CC=C(C=C1)CC.C(C)OC(=O)C(N=P(C1=CC=CC=C1)(C1=CC=CC=C1)C1=CC=CC=C1)=CC=CC1=CC=C(C=C1)CC>>C(C)C1=CC=C(C=C1)C=1C=CC(=NC1C1=CC=C(C=C1)C(F)(F)F)C(=O)OCC
c1ccc(P(c2ccccc2)(c2ccccc2)=[N:29][C:6]([C:4]([O:3][CH2:2][CH3:1])=[O:5])=[CH:7][CH:8]=[CH:9][c:10]2[cH:11][cH:12][c:13]([CH2:14][CH3:15])[cH:16][cH:17]2)cc1.O=[CH:18][c:19]1[cH:20][cH:21][c:22]([C:23]([F:24])([F:25])[F:26])[cH:27][cH:28]1>>[CH3:1][CH2:2][O:3][C:4](=[O:5])[c:6]1[cH:7][cH:8][c:9](-[c:10]2[cH:11][cH:12][...
CCOC(=O)C(=CC=Cc1ccc(CC)cc1)N=P(c1ccccc1)(c1ccccc1)c1ccccc1.O=Cc1ccc(C(F)(F)F)cc1
CCOC(=O)c1ccc(-c2ccc(CC)cc2)c(-c2ccc(C(F)(F)F)cc2)n1
null
null
C(C)#N
Miscellaneous
OtherReaction
02f0f968b0b9e802ed3422aadb999224491a6d9de2a1d809a485b6b3f5f050b2
68e49bad39abe3d5621e12b41ee11e354e282b66589572f30d80e0f4c6de6ee3
c1ccc(-c2cccnc2-c2ccccc2)cc1
O=[CH;D2;+0:1]-[c;H0;D3;+0:2](:[c:3]:[c:4]):[c:5]:[c:6].[C:7]-[#8:8]-[C:9](=[O;D1;H0:10])-[C;H0;D3;+0:11](=[CH;D2;+0:12]-[CH;D2;+0:13]=[CH;D2;+0:14]-[c;H0;D3;+0:15](:[c:16]:[c:17]):[c:18]:[c:19])-[N;H0;D2;+0:20]=P(-c1:c:c:c:c:c:1)(-c1:c:c:c:c:c:1)-c1:c:c:c:c:c:1>>[C:7]-[#8:8]-[C:9](=[O;D1;H0:10])-[c;H0;D3;+0:11]1:[cH;D...
null
[]
60
CELSIUS
null
null
General Procedure K. 4-(trifluoromethyl)benzaldehyde (153 mg, 1.88 mmol) was added to a stirred solution of 3-ethoxycarbonyl-1,1,1-triphenyl-6-(4-ethylphenyl)-2-aza-1λ5-phosphahexa-1,3,5-triene (Compound 46, 444 mg, 0.88 mmol) in dry acetonitrile (10 ml) and the solution was heated to 60° C. for 18 hours. The solution ...
10.6084/m9.figshare.5104873.v1
null
Aldehyde.Ester.Conjugated diene
Ester
c1ccccc1.c1ccccc1.c1ccccc1
c1ccncc1
c1ccncc1.c1ccccc1.c1ccccc1
HO-
C(C)#N
60
null
CCOC(=O)C(=CC=Cc1ccc(CC)cc1)N=P(c1ccccc1)(c1ccccc1)c1ccccc1.O=Cc1ccc(C(F)(F)F)cc1>C(C)#N>CCOC(=O)c1ccc(-c2ccc(CC)cc2)c(-c2ccc(C(F)(F)F)cc2)n1
ord_dataset-03ba810b7f464a06b5d8787af2e8b64e
ord-785262fa1aa54b4eaa636014f7b15a5e
CCOC(=O)C(=CC=Cc1ccc(CC)cc1)N=P(c1ccccc1)(c1ccccc1)c1ccccc1.O=Cc1ccncc1>>CCOC(=O)c1ccc(-c2ccc(CC)cc2)c(-c2ccncc2)n1
N1=CC=C(C=C1)C=O.C(C)OC(=O)C(N=P(C1=CC=CC=C1)(C1=CC=CC=C1)C1=CC=CC=C1)=CC=CC1=CC=C(C=C1)CC.C(C)OC(=O)C(N=P(C1=CC=CC=C1)(C1=CC=CC=C1)C1=CC=CC=C1)=CC=CC1=CC=C(C=C1)CC>>C(C)C1=CC=C(C=C1)C=1C(=NC(=CC1)C(=O)OCC)C1=CC=NC=C1
c1ccc(P(c2ccccc2)(c2ccccc2)=[N:25][C:6]([C:4]([O:3][CH2:2][CH3:1])=[O:5])=[CH:7][CH:8]=[CH:9][c:10]2[cH:11][cH:12][c:13]([CH2:14][CH3:15])[cH:16][cH:17]2)cc1.O=[CH:18][c:19]1[cH:20][cH:21][n:22][cH:23][cH:24]1>>[CH3:1][CH2:2][O:3][C:4](=[O:5])[c:6]1[cH:7][cH:8][c:9](-[c:10]2[cH:11][cH:12][c:13]([CH2:14][CH3:15])[cH:16]...
CCOC(=O)C(=CC=Cc1ccc(CC)cc1)N=P(c1ccccc1)(c1ccccc1)c1ccccc1.O=Cc1ccncc1
CCOC(=O)c1ccc(-c2ccc(CC)cc2)c(-c2ccncc2)n1
null
null
C(C)#N
Miscellaneous
OtherReaction
02f0f968b0b9e802ed3422aadb999224491a6d9de2a1d809a485b6b3f5f050b2
68e49bad39abe3d5621e12b41ee11e354e282b66589572f30d80e0f4c6de6ee3
c1ccc(-c2cccnc2-c2ccncc2)cc1
O=[CH;D2;+0:1]-[c;H0;D3;+0:2]1:[c:3]:[c:4]:[#7;a:5]:[c:6]:[c:7]:1.[C:8]-[#8:9]-[C:10](=[O;D1;H0:11])-[C;H0;D3;+0:12](=[CH;D2;+0:13]-[CH;D2;+0:14]=[CH;D2;+0:15]-[c;H0;D3;+0:16](:[c:17]:[c:18]):[c:19]:[c:20])-[N;H0;D2;+0:21]=P(-c1:c:c:c:c:c:1)(-c1:c:c:c:c:c:1)-c1:c:c:c:c:c:1>>[C:8]-[#8:9]-[C:10](=[O;D1;H0:11])-[c;H0;D3;+...
null
[]
null
null
null
null
Following General Procedure K, 4-pyridinecarboxaldehyde (92 mg, 0.86 mmol) and 3-ethoxycarbonyl-1,1,1-triphenyl-6-(4-ethylphenyl)-2-aza-1λ5-phosphahexa-1,3,5-triene (Compound 46, 434 mg, 0.86 mmol) in dry acetonitrile (10 ml) were reacted to produce the title compound as a yellow solid. Conditions: See reaction.notes.p...
10.6084/m9.figshare.5104873.v1
null
Aldehyde.Ester.Conjugated diene
Ester
c1ccccc1.c1ccccc1.c1ccccc1
c1ccncc1
c1ccncc1.c1ccccc1.c1ccncc1
HO-
C(C)#N
null
null
CCOC(=O)C(=CC=Cc1ccc(CC)cc1)N=P(c1ccccc1)(c1ccccc1)c1ccccc1.O=Cc1ccncc1>C(C)#N>CCOC(=O)c1ccc(-c2ccc(CC)cc2)c(-c2ccncc2)n1
ord_dataset-03ba810b7f464a06b5d8787af2e8b64e
ord-d60f8401e2e744eba24dc3965d488e26
CCOC(=O)C(=CC=Cc1ccc(CC)cc1)N=P(c1ccccc1)(c1ccccc1)c1ccccc1.O=Cc1ccccn1>>CCOC(=O)c1ccc(-c2ccc(CC)cc2)c(-c2ccccn2)n1
N1=C(C=CC=C1)C=O.C(C)OC(=O)C(N=P(C1=CC=CC=C1)(C1=CC=CC=C1)C1=CC=CC=C1)=CC=CC1=CC=C(C=C1)CC.C(C)OC(=O)C(N=P(C1=CC=CC=C1)(C1=CC=CC=C1)C1=CC=CC=C1)=CC=CC1=CC=C(C=C1)CC>>C(C)C1=CC=C(C=C1)C=1C(=NC(=CC1)C(=O)OCC)C1=NC=CC=C1
c1ccc(P(c2ccccc2)(c2ccccc2)=[N:25][C:6]([C:4]([O:3][CH2:2][CH3:1])=[O:5])=[CH:7][CH:8]=[CH:9][c:10]2[cH:11][cH:12][c:13]([CH2:14][CH3:15])[cH:16][cH:17]2)cc1.O=[CH:18][c:19]1[cH:20][cH:21][cH:22][cH:23][n:24]1>>[CH3:1][CH2:2][O:3][C:4](=[O:5])[c:6]1[cH:7][cH:8][c:9](-[c:10]2[cH:11][cH:12][c:13]([CH2:14][CH3:15])[cH:16]...
CCOC(=O)C(=CC=Cc1ccc(CC)cc1)N=P(c1ccccc1)(c1ccccc1)c1ccccc1.O=Cc1ccccn1
CCOC(=O)c1ccc(-c2ccc(CC)cc2)c(-c2ccccn2)n1
null
null
C(C)#N
Miscellaneous
OtherReaction
02f0f968b0b9e802ed3422aadb999224491a6d9de2a1d809a485b6b3f5f050b2
68e49bad39abe3d5621e12b41ee11e354e282b66589572f30d80e0f4c6de6ee3
c1ccc(-c2cccnc2-c2ccccn2)cc1
O=[CH;D2;+0:1]-[c;H0;D3;+0:2](:[#7;a:3]:[c:4]):[c:5]:[c:6].[C:7]-[#8:8]-[C:9](=[O;D1;H0:10])-[C;H0;D3;+0:11](=[CH;D2;+0:12]-[CH;D2;+0:13]=[CH;D2;+0:14]-[c;H0;D3;+0:15](:[c:16]:[c:17]):[c:18]:[c:19])-[N;H0;D2;+0:20]=P(-c1:c:c:c:c:c:1)(-c1:c:c:c:c:c:1)-c1:c:c:c:c:c:1>>[C:7]-[#8:8]-[C:9](=[O;D1;H0:10])-[c;H0;D3;+0:11]1:[c...
null
[]
null
null
null
null
Following General Procedure K, 2-pyridinecarboxaldehyde (41 mg, 0.38 mmol) and 3-ethoxycarbonyl-1,1,1-triphenyl-6-(4-ethylphenyl)-2-aza-1λ5-phosphahexa-1,3,5-triene (Compound 46, 193 mg, 0.38 mmol) in dry acetonitrile (5 ml) were reacted to produce the title compound as a yellow solid. Conditions: See reaction.notes.pr...
10.6084/m9.figshare.5104873.v1
null
Aldehyde.Ester.Conjugated diene
Ester
c1ccccc1.c1ccccc1.c1ccccc1
c1ccncc1
c1ccncc1.c1ccccc1.c1ccncc1
HO-
C(C)#N
null
null
CCOC(=O)C(=CC=Cc1ccc(CC)cc1)N=P(c1ccccc1)(c1ccccc1)c1ccccc1.O=Cc1ccccn1>C(C)#N>CCOC(=O)c1ccc(-c2ccc(CC)cc2)c(-c2ccccn2)n1
ord_dataset-03ba810b7f464a06b5d8787af2e8b64e
ord-2678073f777c403da66620f9ff443181
CCOC(=O)c1ccc(-c2ccc(CC)cc2)c(-c2ccc(C(F)(F)F)cc2)n1>>CCc1ccc(-c2ccc(C(=O)OC)nc2-c2ccc(C(F)(F)F)cc2)cc1
C(C)C1=CC=C(C=C1)C=1C=CC(=NC1C1=CC=C(C=C1)C(F)(F)F)C(=O)OCC.C(C)C1=CC=C(C=C1)C=1C=CC(=NC1C1=CC=C(C=C1)C(F)(F)F)C(=O)OCC>>C(C)C1=CC=C(C=C1)C=1C=CC(=NC1C1=CC=C(C=C1)C(F)(F)F)C(=O)OC
C[CH2:14][O:13][C:11]([c:10]1[cH:9][cH:8][c:7](-[c:6]2[cH:5][cH:4][c:3]([CH2:2][CH3:1])[cH:28][cH:27]2)[c:16](-[c:17]2[cH:18][cH:19][c:20]([C:21]([F:22])([F:23])[F:24])[cH:25][cH:26]2)[n:15]1)=[O:12]>>[CH3:1][CH2:2][c:3]1[cH:4][cH:5][c:6](-[c:7]2[cH:8][cH:9][c:10]([C:11](=[O:12])[O:13][CH3:14])[n:15][c:16]2-[c:17]2[cH:...
CCOC(=O)c1ccc(-c2ccc(CC)cc2)c(-c2ccc(C(F)(F)F)cc2)n1
CCc1ccc(-c2ccc(C(=O)OC)nc2-c2ccc(C(F)(F)F)cc2)cc1
null
OS(=O)(=O)O
CO
Miscellaneous
Transesterification
797948efc8975454230354c6926ef43459a60311d668503c7a6b6bcdb3eafe50
6ad95641ddc9be155108cd2297ce15bcd8cb0ca25c68bfc4fce3cbf5009a236a
c1ccc(-c2cccnc2-c2ccccc2)cc1
C-[CH2;D2;+0:1]-[#8:2]-[C:3](=[O;D1;H0:4])-[c:5]:[#7;a:6]>>[#7;a:6]:[c:5]-[C:3](=[O;D1;H0:4])-[#8:2]-[CH3;D1;+0:1]
null
[]
null
null
null
null
Following General Procedure E, ethyl 5-(4-ethylphenyl)-6-(4-(trifluoromethyl)phenyl)pyridine-2-carboxylate (Compound 48, 60 mg, 0.15 mmol) and conc. H2SO4 (10 drops) in methanol were reacted to produce the title compound as a light yellow solid. Conditions: See reaction.notes.procedure_details. Workup: were reacted
10.6084/m9.figshare.5104873.v1
null
Ester
Ester
null
null
c1ccccc1.c1ccncc1.c1ccccc1
Other
OS(=O)(=O)O.CO
null
null
CCOC(=O)c1ccc(-c2ccc(CC)cc2)c(-c2ccc(C(F)(F)F)cc2)n1>OS(=O)(=O)O.CO>CCc1ccc(-c2ccc(C(=O)OC)nc2-c2ccc(C(F)(F)F)cc2)cc1
ord_dataset-03ba810b7f464a06b5d8787af2e8b64e
ord-36fda2b6e6234cea9f29b13440c68cbc
CCOC(=O)c1ccc(-c2ccc(CC)cc2)c(-c2ccncc2)n1>>CCc1ccc(-c2ccc(C(=O)OC)nc2-c2ccncc2)cc1
N1=C(C=CC=C1)C(=O)[O-].C(C)C1=CC=C(C=C1)C=1C(=NC(=CC1)C(=O)OCC)C1=CC=NC=C1>>C(C)C1=CC=C(C=C1)C=1C=CC(=NC1C1=CC=NC=C1)C(=O)OC
C[CH2:14][O:13][C:11]([c:10]1[cH:9][cH:8][c:7](-[c:6]2[cH:5][cH:4][c:3]([CH2:2][CH3:1])[cH:24][cH:23]2)[c:16](-[c:17]2[cH:18][cH:19][n:20][cH:21][cH:22]2)[n:15]1)=[O:12]>>[CH3:1][CH2:2][c:3]1[cH:4][cH:5][c:6](-[c:7]2[cH:8][cH:9][c:10]([C:11](=[O:12])[O:13][CH3:14])[n:15][c:16]2-[c:17]2[cH:18][cH:19][n:20][cH:21][cH:22]...
CCOC(=O)c1ccc(-c2ccc(CC)cc2)c(-c2ccncc2)n1
CCc1ccc(-c2ccc(C(=O)OC)nc2-c2ccncc2)cc1
null
OS(=O)(=O)O
CO
Miscellaneous
Transesterification
797948efc8975454230354c6926ef43459a60311d668503c7a6b6bcdb3eafe50
6ad95641ddc9be155108cd2297ce15bcd8cb0ca25c68bfc4fce3cbf5009a236a
c1ccc(-c2cccnc2-c2ccncc2)cc1
C-[CH2;D2;+0:1]-[#8:2]-[C:3](=[O;D1;H0:4])-[c:5]:[#7;a:6]>>[#7;a:6]:[c:5]-[C:3](=[O;D1;H0:4])-[#8:2]-[CH3;D1;+0:1]
null
[]
null
null
null
null
Following General Procedure E, ethyl 5-(4-ethylphenyl)-6-(pyridine-4-yl)phenyl)pyridine-2-carboxylate (Compound 49, 48 mg, 0.14 mmol) and conc. H2SO4 (10 drops) in methanol were reacted to produce the title compound as a light yellow solid. Conditions: See reaction.notes.procedure_details. Workup: were reacted
10.6084/m9.figshare.5104873.v1
null
Ester
Ester
null
null
c1ccccc1.c1ccncc1.c1ccncc1
Other
OS(=O)(=O)O.CO
null
null
CCOC(=O)c1ccc(-c2ccc(CC)cc2)c(-c2ccncc2)n1>OS(=O)(=O)O.CO>CCc1ccc(-c2ccc(C(=O)OC)nc2-c2ccncc2)cc1
ord_dataset-03ba810b7f464a06b5d8787af2e8b64e
ord-f84eb07691ad48848f4d45b22cacaa43
CCOC(=O)c1ccc(-c2ccc(CC)cc2)c(-c2ccccn2)n1>>CCc1ccc(-c2ccc(C(=O)OC)nc2-c2ccccn2)cc1
N1=C(C=CC=C1)C(=O)[O-].C(C)C1=CC=C(C=C1)C=1C(=NC(=CC1)C(=O)OCC)C1=NC=CC=C1>>C(C)C1=CC=C(C=C1)C=1C=CC(=NC1C1=NC=CC=C1)C(=O)OC
C[CH2:14][O:13][C:11]([c:10]1[cH:9][cH:8][c:7](-[c:6]2[cH:5][cH:4][c:3]([CH2:2][CH3:1])[cH:24][cH:23]2)[c:16](-[c:17]2[cH:18][cH:19][cH:20][cH:21][n:22]2)[n:15]1)=[O:12]>>[CH3:1][CH2:2][c:3]1[cH:4][cH:5][c:6](-[c:7]2[cH:8][cH:9][c:10]([C:11](=[O:12])[O:13][CH3:14])[n:15][c:16]2-[c:17]2[cH:18][cH:19][cH:20][cH:21][n:22]...
CCOC(=O)c1ccc(-c2ccc(CC)cc2)c(-c2ccccn2)n1
CCc1ccc(-c2ccc(C(=O)OC)nc2-c2ccccn2)cc1
null
OS(=O)(=O)O
CO
Miscellaneous
Transesterification
797948efc8975454230354c6926ef43459a60311d668503c7a6b6bcdb3eafe50
6ad95641ddc9be155108cd2297ce15bcd8cb0ca25c68bfc4fce3cbf5009a236a
c1ccc(-c2cccnc2-c2ccccn2)cc1
C-[CH2;D2;+0:1]-[#8:2]-[C:3](=[O;D1;H0:4])-[c:5]:[#7;a:6]>>[#7;a:6]:[c:5]-[C:3](=[O;D1;H0:4])-[#8:2]-[CH3;D1;+0:1]
null
[]
null
null
null
null
Following General Procedure E, ethyl 5-(4-ethylphenyl)-6-(pyridine-2-yl)phenyl)pyridine-2-carboxylate (Compound 50, 16 mg, 0.05 mmol) and conc. H2SO4 (10 drops) in methanol were reacted to produce the title compound as a light yellow solid. Conditions: See reaction.notes.procedure_details. Workup: were reacted
10.6084/m9.figshare.5104873.v1
null
Ester
Ester
null
null
c1ccccc1.c1ccncc1.c1ccncc1
Other
OS(=O)(=O)O.CO
null
null
CCOC(=O)c1ccc(-c2ccc(CC)cc2)c(-c2ccccn2)n1>OS(=O)(=O)O.CO>CCc1ccc(-c2ccc(C(=O)OC)nc2-c2ccccn2)cc1
ord_dataset-03ba810b7f464a06b5d8787af2e8b64e
ord-f2ac45d32fa641e1bc045452d34d6cd4
CCOC(=O)c1ccc(-c2ccccc2)c(-c2ccccc2)n1>>O=Cc1ccc(-c2ccccc2)c(-c2ccccc2)n1
C1(=CC=CC=C1)C=1C=CC(=NC1C1=CC=CC=C1)C(=O)OCC.C1(=CC=CC=C1)C=1C=CC(=NC1C1=CC=CC=C1)C(=O)OCC.CC(C)C[AlH]CC(C)C>>C1(=CC=CC=C1)C=1C=CC(=NC1C1=CC=CC=C1)C=O
CCO[C:2](=[O:1])[c:3]1[cH:4][cH:5][c:6](-[c:7]2[cH:8][cH:9][cH:10][cH:11][cH:12]2)[c:13](-[c:14]2[cH:15][cH:16][cH:17][cH:18][cH:19]2)[n:20]1>>[O:1]=[CH:2][c:3]1[cH:4][cH:5][c:6](-[c:7]2[cH:8][cH:9][cH:10][cH:11][cH:12]2)[c:13](-[c:14]2[cH:15][cH:16][cH:17][cH:18][cH:19]2)[n:20]1
CCOC(=O)c1ccc(-c2ccccc2)c(-c2ccccc2)n1
O=Cc1ccc(-c2ccccc2)c(-c2ccccc2)n1
null
null
C(Cl)Cl
Reduction
OtherReaction
ec1c6c64dd9be73981e5a6c952ab740869d298b20e87e097e88e1179cc5bc6dc
33ddc7b9457742ba0a376f08a972e4f33779267f6f1fe15e3be786427ae9f4ec
c1ccc(-c2cccnc2-c2ccccc2)cc1
C-C-O-[C;H0;D3;+0:1](=[O;D1;H0:2])-[c:3](:[c:4]):[#7;a:5]:[c:6]>>[O;D1;H0:2]=[CH;D2;+0:1]-[c:3](:[c:4]):[#7;a:5]:[c:6]
null
[]
null
null
1
HOUR
General Procedure L. To a solution of ethyl 5,6-diphenylpyridine-2-carboxylate (Compound 21, 145 mg, 0.48 mmol) in CH2Cl2 (5 ml) at −78° C. was added DIBAL-H (0.72 ml, 0.72 mmol, 1.0 M in Toluene) and the mixture was stirred between −78° C. and −60° C. for 1 hour under argon. The reaction was quenched with aq, NH4Cl, d...
10.6084/m9.figshare.5104873.v1
null
Ester
Aldehyde
null
null
c1ccncc1.c1ccccc1.c1ccccc1
HO-
C(Cl)Cl
null
1
CCOC(=O)c1ccc(-c2ccccc2)c(-c2ccccc2)n1>C(Cl)Cl>O=Cc1ccc(-c2ccccc2)c(-c2ccccc2)n1
ord_dataset-03ba810b7f464a06b5d8787af2e8b64e
ord-25cfcf96b25d4fc6b54c9b584a00826c
CCOC(=O)c1ccc(-c2ccc(C(F)(F)F)cc2)c(-c2ccccc2)n1>>O=Cc1ccc(-c2ccc(C(F)(F)F)cc2)c(-c2ccccc2)n1
C1(=CC=CC=C1)C1=C(C=CC(=N1)C(=O)OCC)C1=CC=C(C=C1)C(F)(F)F.C1(=CC=CC=C1)C1=C(C=CC(=N1)C(=O)OCC)C1=CC=C(C=C1)C(F)(F)F.CC(C)C[AlH]CC(C)C>>FC(C1=CC=C(C=C1)C=1C=CC(=NC1C1=CC=CC=C1)C=O)(F)F
CCO[C:2](=[O:1])[c:3]1[cH:4][cH:5][c:6](-[c:7]2[cH:8][cH:9][c:10]([C:11]([F:12])([F:13])[F:14])[cH:15][cH:16]2)[c:17](-[c:18]2[cH:19][cH:20][cH:21][cH:22][cH:23]2)[n:24]1>>[O:1]=[CH:2][c:3]1[cH:4][cH:5][c:6](-[c:7]2[cH:8][cH:9][c:10]([C:11]([F:12])([F:13])[F:14])[cH:15][cH:16]2)[c:17](-[c:18]2[cH:19][cH:20][cH:21][cH:2...
CCOC(=O)c1ccc(-c2ccc(C(F)(F)F)cc2)c(-c2ccccc2)n1
O=Cc1ccc(-c2ccc(C(F)(F)F)cc2)c(-c2ccccc2)n1
null
null
C(Cl)Cl
Reduction
OtherReaction
ec1c6c64dd9be73981e5a6c952ab740869d298b20e87e097e88e1179cc5bc6dc
33ddc7b9457742ba0a376f08a972e4f33779267f6f1fe15e3be786427ae9f4ec
c1ccc(-c2cccnc2-c2ccccc2)cc1
C-C-O-[C;H0;D3;+0:1](=[O;D1;H0:2])-[c:3](:[c:4]):[#7;a:5]:[c:6]>>[O;D1;H0:2]=[CH;D2;+0:1]-[c:3](:[c:4]):[#7;a:5]:[c:6]
null
[]
null
null
null
null
Following General Procedure L, ethyl 5-(4-trifluoromethylphenyl)-6-phenylpyridine-2-carboxylate (Compound 25, 74 mg, 0.20 mmol) and DIBAL-H (0.3 ml, 0.30 mmol, 1.0 M in hexane) in CH2Cl2 (3 ml) were reacted to produce the title compound after purification by column chromatography (silica gel, 15% ethyl acetate in hexan...
10.6084/m9.figshare.5104873.v1
null
Ester
Aldehyde
null
null
c1ccncc1.c1ccccc1.c1ccccc1
HO-
C(Cl)Cl
null
null
CCOC(=O)c1ccc(-c2ccc(C(F)(F)F)cc2)c(-c2ccccc2)n1>C(Cl)Cl>O=Cc1ccc(-c2ccc(C(F)(F)F)cc2)c(-c2ccccc2)n1
ord_dataset-03ba810b7f464a06b5d8787af2e8b64e
ord-eb6ca69b6c7b4a888c638ddbdf043103
NCCCP(=O)(O)O.O=Cc1ccc(-c2ccccc2)c(-c2ccccc2)n1>>O=P(O)(O)CCCNCc1ccc(-c2ccccc2)c(-c2ccccc2)n1
C1(=CC=CC=C1)C=1C=CC(=NC1C1=CC=CC=C1)C=O.C1(=CC=CC=C1)C=1C=CC(=NC1C1=CC=CC=C1)C=O.NCCCP(O)(O)=O.[BH3-]C#N.[Na+]>>C1(=CC=CC=C1)C=1C=CC(=NC1C1=CC=CC=C1)CNCCCP(O)(O)=O
[O:1]=[P:2]([OH:3])([OH:4])[CH2:5][CH2:6][CH2:7][NH2:8].O=[CH:9][c:10]1[cH:11][cH:12][c:13](-[c:14]2[cH:15][cH:16][cH:17][cH:18][cH:19]2)[c:20](-[c:21]2[cH:22][cH:23][cH:24][cH:25][cH:26]2)[n:27]1>>[O:1]=[P:2]([OH:3])([OH:4])[CH2:5][CH2:6][CH2:7][NH:8][CH2:9][c:10]1[cH:11][cH:12][c:13](-[c:14]2[cH:15][cH:16][cH:17][cH:...
NCCCP(=O)(O)O.O=Cc1ccc(-c2ccccc2)c(-c2ccccc2)n1
O=P(O)(O)CCCNCc1ccc(-c2ccccc2)c(-c2ccccc2)n1
null
null
CO
Heteroatom Alkylation and Arylation
Reductive amination with aldehyde
422be648aea52bce28ccc8fb32ec3178aaa47bbd624f063874619362f075b5f2
7915721a3e395aed85e3c40dc4d725c571a931ac517c6a0da16f2a2b0bb5eac7
c1ccc(-c2cccnc2-c2ccccc2)cc1
O=[CH;D2;+0:1]-[c:2](:[c:3]):[#7;a:4]:[c:5].[C:6]-[C:7]-[NH2;D1;+0:8]>>[C:6]-[C:7]-[NH;D2;+0:8]-[CH2;D2;+0:1]-[c:2](:[c:3]):[#7;a:4]:[c:5]
null
[]
50
CELSIUS
30
MINUTE
General Procedure M. To a solution of 5,6-diphenylpyridine-2-carbaldehyde (Compound 54, 95 mg, 0.37 mmol) and (3-amino-propyl)-phosphonic acid (51 mg, 0.37 mmol) in MeOH (3 ml) was added Bu4NOH (0.4 ml, 0.37 mmol, 1M in MeOH) under argon. The mixture was stirred at 50° C. for 30 min. before adding NaCNBH3 (23 mg, 0.37 ...
10.6084/m9.figshare.5104873.v1
null
Aldehyde.Primary amine
Secondary amine
null
null
c1ccncc1.c1ccccc1.c1ccccc1
Other
CO
50
0.5
NCCCP(=O)(O)O.O=Cc1ccc(-c2ccccc2)c(-c2ccccc2)n1>CO>O=P(O)(O)CCCNCc1ccc(-c2ccccc2)c(-c2ccccc2)n1
ord_dataset-03ba810b7f464a06b5d8787af2e8b64e
ord-022616730b0b4007b11ba681d49f496b
Cc1ccc(-c2ccc(C=O)nc2-c2ccccc2)cc1.NCCCP(=O)(O)O>>Cc1ccc(-c2ccc(CNCCCP(=O)(O)O)nc2-c2ccccc2)cc1
[BH3-]C#N.[Na+].C1(=CC=CC=C1)C1=C(C=CC(=N1)C=O)C1=CC=C(C=C1)C.C1(=CC=CC=C1)C1=C(C=CC(=N1)C=O)C1=CC=C(C=C1)C.NCCCP(O)(O)=O>>C1(=CC=CC=C1)C1=C(C=CC(=N1)CNCCCP(O)(O)=O)C1=CC=C(C=C1)C
O=[CH:10][c:9]1[cH:8][cH:7][c:6](-[c:5]2[cH:4][cH:3][c:2]([CH3:1])[cH:28][cH:27]2)[c:20](-[c:21]2[cH:22][cH:23][cH:24][cH:25][cH:26]2)[n:19]1.[NH2:11][CH2:12][CH2:13][CH2:14][P:15](=[O:16])([OH:17])[OH:18]>>[CH3:1][c:2]1[cH:3][cH:4][c:5](-[c:6]2[cH:7][cH:8][c:9]([CH2:10][NH:11][CH2:12][CH2:13][CH2:14][P:15](=[O:16])([O...
Cc1ccc(-c2ccc(C=O)nc2-c2ccccc2)cc1.NCCCP(=O)(O)O
Cc1ccc(-c2ccc(CNCCCP(=O)(O)O)nc2-c2ccccc2)cc1
null
null
CO
Heteroatom Alkylation and Arylation
Reductive amination with aldehyde
422be648aea52bce28ccc8fb32ec3178aaa47bbd624f063874619362f075b5f2
7915721a3e395aed85e3c40dc4d725c571a931ac517c6a0da16f2a2b0bb5eac7
c1ccc(-c2cccnc2-c2ccccc2)cc1
O=[CH;D2;+0:1]-[c:2](:[c:3]):[#7;a:4]:[c:5].[C:6]-[C:7]-[NH2;D1;+0:8]>>[C:6]-[C:7]-[NH;D2;+0:8]-[CH2;D2;+0:1]-[c:2](:[c:3]):[#7;a:4]:[c:5]
null
[]
null
null
null
null
Following General Procedure M, 6-phenyl-5-p-tolylpyridine-2-carbaldehyde (Compound 55, 67 mg, 0.25 mmol), (3-aminopropyl)-phosphonic acid (34 mg, 0.25 mmol), Bu4NOH (0.2 ml, 0.25 mmol, 1 M in MeOH) and NaCNBH3 (15 mg, 0.25 mmol) in MeOH (3 ml) were reacted to produce the title compound as a white solid. Conditions: See...
10.6084/m9.figshare.5104873.v1
null
Aldehyde.Primary amine
Secondary amine
null
null
c1ccccc1.c1ccncc1.c1ccccc1
Other
CO
null
null
Cc1ccc(-c2ccc(C=O)nc2-c2ccccc2)cc1.NCCCP(=O)(O)O>CO>Cc1ccc(-c2ccc(CNCCCP(=O)(O)O)nc2-c2ccccc2)cc1
ord_dataset-03ba810b7f464a06b5d8787af2e8b64e
ord-6c223868fa6e418e812f48b461d0ad88
NCCCP(=O)(O)O.O=Cc1ccc(-c2ccc(C(F)(F)F)cc2)c(-c2ccccc2)n1>>O=P(O)(O)CCCNCc1ccc(-c2ccc(C(F)(F)F)cc2)c(-c2ccccc2)n1
[BH3-]C#N.[Na+].FC(C1=CC=C(C=C1)C=1C=CC(=NC1C1=CC=CC=C1)C=O)(F)F.FC(C1=CC=C(C=C1)C=1C=CC(=NC1C1=CC=CC=C1)C=O)(F)F.NCCCP(O)(O)=O>>C1(=CC=CC=C1)C1=C(C=CC(=N1)CNCCCP(O)(O)=O)C1=CC=C(C=C1)C(F)(F)F
[O:1]=[P:2]([OH:3])([OH:4])[CH2:5][CH2:6][CH2:7][NH2:8].O=[CH:9][c:10]1[cH:11][cH:12][c:13](-[c:14]2[cH:15][cH:16][c:17]([C:18]([F:19])([F:20])[F:21])[cH:22][cH:23]2)[c:24](-[c:25]2[cH:26][cH:27][cH:28][cH:29][cH:30]2)[n:31]1>>[O:1]=[P:2]([OH:3])([OH:4])[CH2:5][CH2:6][CH2:7][NH:8][CH2:9][c:10]1[cH:11][cH:12][c:13](-[c:...
NCCCP(=O)(O)O.O=Cc1ccc(-c2ccc(C(F)(F)F)cc2)c(-c2ccccc2)n1
O=P(O)(O)CCCNCc1ccc(-c2ccc(C(F)(F)F)cc2)c(-c2ccccc2)n1
null
null
CO
Heteroatom Alkylation and Arylation
Reductive amination with aldehyde
422be648aea52bce28ccc8fb32ec3178aaa47bbd624f063874619362f075b5f2
7915721a3e395aed85e3c40dc4d725c571a931ac517c6a0da16f2a2b0bb5eac7
c1ccc(-c2cccnc2-c2ccccc2)cc1
O=[CH;D2;+0:1]-[c:2](:[c:3]):[#7;a:4]:[c:5].[C:6]-[C:7]-[NH2;D1;+0:8]>>[C:6]-[C:7]-[NH;D2;+0:8]-[CH2;D2;+0:1]-[c:2](:[c:3]):[#7;a:4]:[c:5]
null
[]
null
null
null
null
Following General Procedure M, 5-(4-trifluoromethylphenyl)-6-phenyl-pyridine-2-carbaldehyde (Compound 57, 58 mg, 0.18 mmol), (3-amino-propyl)-phosphonic acid (25 mg, 0.18 mmol), Bu4NOH (0.18 ml, 0.18 mmol, 1 M in MeOH) and NaCNBH3 (11 mg, 0.18 mmol) in MeOH (3 ml) were reacted to produce the title compound as a white s...
10.6084/m9.figshare.5104873.v1
null
Aldehyde.Primary amine
Secondary amine
null
null
c1ccncc1.c1ccccc1.c1ccccc1
Other
CO
null
null
NCCCP(=O)(O)O.O=Cc1ccc(-c2ccc(C(F)(F)F)cc2)c(-c2ccccc2)n1>CO>O=P(O)(O)CCCNCc1ccc(-c2ccc(C(F)(F)F)cc2)c(-c2ccccc2)n1