HRID1443313

反应详情

EQUATION

反应方程式

REACTANTS

反应物

HCID8471

Triethylamine

C6H15N

HCID61186

Valeryl chloride

C5H9ClO

结构：COC(=O)[C@@H](NCc1ccc(-c2ccccc2C#N)cc1)C(C)C

HCID16744794

Methyl N-[(2'-cyano[1,1'-biphenyl]-4-yl)methyl]-L-valinate

C20H22N2O2

结构：CCCCC(=O)N(Cc1ccc(-c2ccccc2-c2nnn[nH]2)cc1)[C@H](C(=O)O)C(C)C

HCID178447302

未命名化合物

PRODUCTS

生成物

结构：CCCCC(=O)N(Cc1ccc(-c2ccccc2C#N)cc1)[C@H](C(=O)OC)C(C)C

HCID16744795

N-[(2′-Cyano[1,1′-biphenyl]-4-yl)methyl]-N-(1-oxopentyl)-L-valine methyl ester

C25H30N2O3

AUXILIARIES

试剂、催化剂与溶剂

溶剂HCID6344

Dichloromethane

CH2Cl2

PROCEDURE

实验过程

Briefly, the process for the preparation of valsartan comprises of the condensation of N-[(2′-cyanobiphenyl-4-yl)methyl]-(L)-valine methyl ester of Formula II with valeryl chloride of Formula III in the presence of triethylamine and dichloromethane, followed by flash chromatography, to give the compound N-[(2′-cyanobiphenyl-4-yl)methyl]-N-valeryl-(L)-valine methyl ester of Formula IV. The compound of Formula IV on tetrazole formation using tributyltin azide and subsequent hydrolysis using sodium hydroxide, followed by flash chromatography, gives valsartan of Formula I.