Water → 3-(4-{Methoxycarbonyl-[4-methyl-2-(4-trifluoromethyl-phenyl)-thiazol-5-ylmethyl]-amino}-2-methyl-phenyl)-propionic acid methyl ester

HRID 854569ノート

反応式

HRID 854569 の反応式
[CH3:1][O:2][C:3](=[O:31])[CH2:4][CH2:5][C:6]1[CH:11]=[CH:10][C:9]([NH:12][CH2:13][C:14]2[S:18][C:17]([C:19]3[CH:24]=[CH:23][C:22]([C:25]([F:28])([F:27])[F:26])=[CH:21][CH:20]=3)=[N:16][C:15]=2[CH3:29])=[CH:8][C:7]=1[CH3:30].N1C=CC=CC=1.Cl[C:39]([O:41][CH3:42])=[O:40].O>C(Cl)Cl>[CH3:1][O:2][C:3](=[O:31])[CH2:4][CH2:5][C:6]1[CH:11]=[CH:10][C:9]([N:12]([C:39]([O:41][CH3:42])=[O:40])[CH2:13][C:14]2[S:18][C:17]([C:19]3[CH:20]=[CH:21][C:22]([C:25]([F:27])([F:28])[F:26])=[CH:23][CH:24]=3)=[N:16][C:15]=2[CH3:29])=[CH:8][C:7]=1[CH3:30]

参加物

6

反応物 4

HCID 962WaterHCID 1049PyridineHCID 6586Methyl chloroformateHCID 694694953-(2-Methyl-4-{[4-methyl-2-(4-trifluoromethyl-phenyl)-thiazol-5-ylmethyl]-amino}-phenyl)-propionic acid methyl ester

生成物 1

HCID 694759133-(4-{Methoxycarbonyl-[4-methyl-2-(4-trifluoromethyl-phenyl)-thiazol-5-ylmethyl]-amino}-2-methyl-phenyl)-propionic acid methyl ester収率 102.3%

試薬・触媒・溶媒 1

HCID 6344Dichloromethane溶媒

実験手順

To a 0° C. solution of 3-(2-Methyl-4-{[4-methyl-2-(4-trifluoromethyl-phenyl)-thiazol-5-ylmethyl]-amino}-phenyl)-propionic acid methyl ester (0.05 g, 0.11 mmol) and pyridine (0.027 mL, 0.33 mmol) in anhydrous CH2Cl2 (3 mL) is added methyl chloroformate (0.026 mL, 0.34 mmol) dropwise. The mixture is allowed to warm to RT overnight. Water is added, and the mixture is extracted with CH2Cl2. The combined organics are dried with MgSO4 and concentrated to yield the title compound (57 mg, quant.)

後処理

  1. extractionthe mixture is extracted with CH2Cl2
  2. dry with materialThe combined organics are dried with MgSO4
  3. concentrationconcentrated

出典と根拠

ORDレコード
ord-ebf1cecc7a244d2992fb017cfff6fc3f
出典データセット
uspto-grants-2007_08
特許番号
US07259175B2

反応ノート

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