The Ugi reaction as the green alternative towards active pharmaceutical ingredients

Eirini Fotopoulou , Paraskevi Kleio Anastasiou , Christina Tomza , Constantinos G. Neochoritis
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Abstract

Α sustainable access to therapeutics is today imperative. More than ever, synthetic organic chemistry has to embrace all aspects of green chemistry. The utility of multicomponent reactions especially the Ugi reaction is an established approach in drug discovery. Their diversity, speed and effectiveness, combined with their compatibility with the green chemistry principles, render this type of chemistry very often an alternative to the multistep linear synthetic pathways to active pharmaceutical ingredients. This critical review compares green metrics, such as E-factor (environmental factor), AE (atom economy) and PMI (process mass intensity) factors, of the industrial and MCR syntheses of six well-known commercial drugs.

Abstract Image

乌基反应是活性药物成分的绿色替代品
可持续地获得治疗药物是当今的当务之急。有机合成化学比以往任何时候都更需要绿色化学的各个方面。多组分反应,尤其是乌基反应,是药物发现的一种既定方法。多组分反应的多样性、快速性和有效性,以及与绿色化学原则的兼容性,使这类化学反应往往成为活性药物成分多步线性合成途径的替代选择。这篇评论比较了六种著名商业药物的工业合成和 MCR 合成的绿色指标,如 E-因子(环境因子)、AE(原子经济性)和 PMI(过程质量强度)因子。
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