关键词: Alkaline hydrolysis Fenofibrate Sodium borohydride reduction Synthetic metabolites

来  源:   DOI:10.1016/j.rechem.2023.101282   PDF(Pubmed)

Abstract:
Synthesis and characterization of drug metabolites has emerged as an important area of research in consideration to the significant contribution of studies on metabolites in drug research. The present work comprises synthesis of 2-(4-((4-chlorophenyl)(hydroxy)methyl) phenoxy)-2-methylpropanoic acid, a metabolite of anti-hyperlipidemic drug fenofibrate. The desired compound was prepared by two different synthetic routes. The ketone group of fenofibric acid was reduced using sodium borohydride in one route whereas the hydrolysis of isopropyl ester of the reduced fenofibrate was achieved by the mild alkaline hydrolysis in the other path. Both the ways of synthesis furnished the desired compound in excellent yield and purity. The new synthetic congener was characterized by spectroscopic methods.
摘要:
考虑到药物研究中代谢物研究的重要贡献,药物代谢物的合成和表征已成为重要的研究领域。本工作包括合成2-(4-((4-氯苯基)(羟基)甲基)苯氧基)-2-甲基丙酸,抗高脂血症药物非诺贝特的代谢产物。通过两种不同的合成途径制备所需化合物。非诺贝特酸的酮基使用硼氢化钠在一条途径中还原,而还原的非诺贝特的异丙酯的水解是通过在另一条途径中的温和碱性水解实现的。两种合成方法都以优异的产率和纯度提供了所需的化合物。通过光谱方法对新的合成同源物进行了表征。
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