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微波辅助合成:药物发现中的一项新技术。

Microwave assisted synthesis: a new technology in drug discovery.

作者信息

Santagada V, Frecentese F, Perissutti E, Fiorino F, Severino B, Caliendo G

机构信息

Dipartimento di Chimica Farmaceutica e Tossicologica, Via D. Montesano, 49, 80131 Naples, Italy.

出版信息

Mini Rev Med Chem. 2009 Mar;9(3):340-58. doi: 10.2174/1389557510909030340.

Abstract

The interest in the microwave assisted organic synthesis has been growing during the recent years. It results from an increasing knowledge of fundamentals of the dielectric heating theory, availability of an equipment designed especially for the laboratory use as well as the discovery of the special techniques of the microwave syntheses. The efficiency of microwave flash-heating chemistry in dramatically reducing reaction times (reduced from days and hours to minutes and seconds) has recently been proven in several different fields of organic chemistry and this aspect is of great importance in high-speed combinatorial and medicinal chemistry. In this contribution, the current state of the art is summarized providing examples of the most recent applications in the field of microwave assisted synthesis of biologically active compounds both in heterocyclic and in peptide and peptidomimetic optimization.

摘要

近年来,对微波辅助有机合成的兴趣一直在增长。这源于对介电加热理论基础的了解不断增加、专门为实验室使用设计的设备的可用性以及微波合成特殊技术的发现。微波闪热化学在显著缩短反应时间(从数天和数小时缩短至数分钟和数秒)方面的效率最近已在有机化学的几个不同领域得到证实,这一点在高速组合化学和药物化学中非常重要。在本论文中,总结了当前的技术水平,并提供了微波辅助合成生物活性化合物领域中最新应用的实例,涉及杂环、肽以及肽模拟物优化等方面。

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