4-氟-α-(2-甲基-1-氧丙基)-γ-氧-N,β-二苯基-苯丁酰胺的合成

Synthesis of 4-Fluoro-α-(2-methyl-1-oxopropyl)-γ-oxo-N,β-diphenyl-benzenebutanamide

以苯乙酸为原料,4-氟苯基苯乙酮在HBr/H2O2作用下发生α-溴代,合成2-溴-1-(4-氟苯基)-苯乙酮,再与异丁酰乙酰苯胺在碱性条件下发生α-碳上的取代反应,得到阿托伐他汀钙的关键中间体4-氟-α-(2-甲基-1-氧丙基)-γ-氧-N,β-二苯基-苯丁酰胺,总收率57.3%。化合物结构经核磁、质谱得到确认。

Using phenylacetic acid as raw material,2-bromo-1-（4-fluorophenyl）-2-phenylethanone was prepared by bromination with HBr and H_2O_2 from 1-（4-fluorophenyl）-2-phenylethanone.4-Fluoroα-（2-methyl-1-oxopropyl）-γ-oxo-N,β-diphenyl-benzenebutanamide,the key intermediate of atorvastatin calcium,was synthesized by condensation of 2-bromo-1-（4-fluorophenyl）-2-phenylethanone and 4-methyl-3-oxopentanoic acid anilide.The overall yield was 57.3%.The product was characterized by（）～1H NMR and MS spectroscopy.