Abstract

A four-step, practical, and easily scalable synthesis of 3-ethyl-4-methyl-1,5-dihydro-2H-pyrrol-2-one, an important building block of the antidiabetic drug glimepiride, has been accomplished. Key features are the synthesis of 3-methyl-4-hydroxy-2-butenolide in water and triflic acid mediated N-benzyl lactam N-deprotection. The main advantages of this process are the scalable synthetic route and decreased number of reaction steps, which paves the way for the industrial-scale synthesis of 3-ethyl-4-methyl-1,5-dihydro-2H-pyrrol-2-one.

中文翻译：

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3-乙基-4-甲基-1,5-二氢-2H-吡咯-2-酮的可扩展合成：降糖药物格列美脲的重要组成部分

摘要

已经完成了四步骤，实用且易于扩展的3-乙基-4-甲基-1,5-二氢-2H-吡咯-2-酮（抗糖尿病药格列美脲的重要组成部分）的合成。关键特征是在水中合成3-甲基-4-羟基-2-丁烯内酯和三氟甲磺酸介导的N-苄基内酰胺N-脱保护。该方法的主要优点是可扩展的合成路线和减少的反应步骤数量，为工业规模合成3-乙基-4-甲基-1,5-二氢-2H-吡咯-2-酮铺平了道路。 。