H-Tyr(Bzl)-OMe → HCID 86597132、化合物

HRID 1984823ノート

反応式

HRID 1984823 の反応式
[C:1]([C:5]1[CH:24]=[CH:23][C:8]([O:9][C:10]2[CH:11]=[C:12]3[C:17](=[CH:18][CH:19]=2)[CH:16]=[N:15][C:14]([C:20](O)=[O:21])=[CH:13]3)=[CH:7][CH:6]=1)([CH3:4])([CH3:3])[CH3:2].[CH3:25][O:26][C:27](=[O:45])[C@@H:28]([NH2:44])[CH2:29][C:30]1[CH:35]=[CH:34][C:33]([O:36][CH2:37][C:38]2[CH:43]=[CH:42][CH:41]=[CH:40][CH:39]=2)=[CH:32][CH:31]=1>>[CH3:25][O:26][C:27](=[O:45])[CH:28]([NH:44][C:20]([C:14]1[N:15]=[CH:16][C:17]2[C:12]([CH:13]=1)=[CH:11][C:10]([O:9][C:8]1[CH:23]=[CH:24][C:5]([C:1]([CH3:4])([CH3:3])[CH3:2])=[CH:6][CH:7]=1)=[CH:19][CH:18]=2)=[O:21])[CH2:29][C:30]1[CH:35]=[CH:34][C:33]([O:36][CH2:37][C:38]2[CH:43]=[CH:42][CH:41]=[CH:40][CH:39]=2)=[CH:32][CH:31]=1

参加物

3

反応物 2

HCID 6999558H-Tyr(Bzl)-OMeHCID 577181086-(4-Tert-butyl-phenoxy)-isoquinoline-3-carboxylic acid

生成物 1

HCID 86597132HCID 86597132、化合物収率 75.5%

実験手順

870 mg (2.71 mmol) of 6-(4-tert-butylphenoxy)-isoquinoline-3-carboxylic acid (example 295) was reacted with 871 mg (2.71 mmol) of (2S)-amino-3-(4-benzyloxy-phenyl)-propionic acid methyl ester as described in general procedure A. The crude product was purified by flash column chromatography on silica using 3:2 hexane/ethyl acetate as eluent to afford 1.205 g of 3-(4-benzyloxy-phenyl)-2-{[6-(4-tert-butyl-phenoxy)-isoquinoline-3-carbonyl]-amino}-propionic acid methyl-ester as a white solid. LCMS 590 (M+1)+.

後処理

  1. customThe crude product was purified by flash column chromatography on silica using 3:2 hexane/ethyl acetate as eluent

出典と根拠

ORDレコード
ord-30b805c175984ab095e1c3bdd1944ab6
出典データセット
uspto-grants-2009_06
特許番号
US07544699B2

反応ノート

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