5-Chloro-1H-indole-2-carboxylic acid → 4-{2-(5-Chloro-1H-indole-2-carbonyl)amino-2-(2-chloro-phenyl)ethoxymethyl}piperidine-1-carboxylic acid tert-butyl ester

HRID 32402ノート

反応式

HRID 32402 の反応式
[C:1]([O:5][C:6]([N:8]1[CH2:13][CH2:12][CH:11]([CH2:14][O:15][CH2:16][CH:17]([NH2:25])[C:18]2[CH:23]=[CH:22][CH:21]=[CH:20][C:19]=2[Cl:24])[CH2:10][CH2:9]1)=[O:7])([CH3:4])([CH3:3])[CH3:2].[Cl:26][C:27]1[CH:28]=[C:29]2[C:33](=[CH:34][CH:35]=1)[NH:32][C:31]([C:36](O)=[O:37])=[CH:30]2>>[C:1]([O:5][C:6]([N:8]1[CH2:9][CH2:10][CH:11]([CH2:14][O:15][CH2:16][CH:17]([NH:25][C:36]([C:31]2[NH:32][C:33]3[C:29]([CH:30]=2)=[CH:28][C:27]([Cl:26])=[CH:35][CH:34]=3)=[O:37])[C:18]2[CH:23]=[CH:22][CH:21]=[CH:20][C:19]=2[Cl:24])[CH2:12][CH2:13]1)=[O:7])([CH3:4])([CH3:2])[CH3:3]

参加物

3

反応物 2

HCID 826935-Chloro-1H-indole-2-carboxylic acidHCID 693096454-[2-Amino-2-(2-chlorophenyl)-ethoxymethyl]piperidine-1-carboxylic acid tert-butyl ester

生成物 1

HCID 693079174-{2-(5-Chloro-1H-indole-2-carbonyl)amino-2-(2-chloro-phenyl)ethoxymethyl}piperidine-1-carboxylic acid tert-butyl ester

実験手順

Using coupling method A, 4-[2-amino-2-(2-chlorophenyl)-ethoxymethyl]piperidine-1-carboxylic acid tert-butyl ester (300 mg, 0.8 mmol) and 5-chloroindole-2-carboxylic acid (158 mg, 1.4 mmol) afforded, after purification (SiO2: 33% EtOAc in hexane), 407 mg (92%) of the title compound.

後処理

  1. customafforded
  2. customafter purification (SiO2: 33% EtOAc in hexane), 407 mg (92%) of the title compound

出典と根拠

ORDレコード
ord-0328b3ed11004a6c8a0fc59f1d80041e
出典データセット
uspto-grants-2008_09
特許番号
US07427632B2

反応ノート

読み込み中…