反応式
C[O:2][C:3]([C:5]1[C:13]2[N:12]=[C:11]([C:14](=[O:25])[NH:15][CH:16]3[CH2:21][CH2:20][N:19]([CH:22]([CH3:24])[CH3:23])[CH2:18][CH2:17]3)[NH:10][C:9]=2[CH:8]=[CH:7][CH:6]=1)=[O:4].Br[CH2:27][C:28]1[S:32][C:31]2[CH:33]=[CH:34][C:35]([Cl:37])=[CH:36][C:30]=2[CH:29]=1.CC#N.O>C(O)=O>[Cl:37][C:35]1[CH:34]=[CH:33][C:31]2[S:32][C:28]([CH2:27][N:10]3[C:9]4[CH:8]=[CH:7][CH:6]=[C:5]([C:3]([OH:2])=[O:4])[C:13]=4[N:12]=[C:11]3[C:14](=[O:25])[NH:15][CH:16]3[CH2:21][CH2:20][N:19]([CH:22]([CH3:23])[CH3:24])[CH2:18][CH2:17]3)=[CH:29][C:30]=2[CH:36]=1.[Cl:37][C:35]1[CH:34]=[CH:33][C:31]2[S:32][C:28]([CH2:27][N:12]3[C:13]4[C:5]([C:3]([OH:2])=[O:4])=[CH:6][CH:7]=[CH:8][C:9]=4[N:10]=[C:11]3[C:14](=[O:25])[NH:15][CH:16]3[CH2:17][CH2:18][N:19]([CH:22]([CH3:24])[CH3:23])[CH2:20][CH2:21]3)=[CH:29][C:30]=2[CH:36]=1参加物
6
反応物 3
生成物 2
試薬・触媒・溶媒 1
実験手順
1-(5-Chloro-benzo[b]thiophen-2-ylmethyl)-2-(1-isopropyl-piperidin-4-ylcarbamoyl)-1H-benzoimidazole-4-carboxylic acid and 3-(5-Chloro-benzo[b]thiophen-2-ylmethyl)-2-(1-isopropyl-piperidin-4-ylcarbamoyl)-3H-benzoimidazole-4-carboxylic acid were prepared by a procedure according to example 81 starting from 200 mg (0.58 mmol) 2-(1-Isopropyl-piperidin-4-ylcarbamoyl)-1H-benzoimidazole-4-carboxylic acid methyl ester and 151.9 mg (0.58 mmol) 2-bromomethyl-5-chloro-benzo[b]thiophene. Hydrolysis of the resulting esters and purification by preparative RP-HPLC (CH3CN/H2O gradient+0.05% formic acid) gave the title compounds as their formiates in form of white amorphous solids.
出典と根拠
- ORDレコード
- ord-c32ae755381a41f3b8761c399aaf264e
- 出典データセット
- uspto-grants-2010_06
- 特許番号
- US07741341B2
関連ノート
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