氮杂吲哚合成  

Synthesis of Azaindoles

作　　者：王志会[1] 王晓[1] 

机构地区：[1]中国石油大学(北京)理学院,北京102249

出　　处：《化学进展》2012年第10期1974-1982,共9页Progress in Chemistry

基　　金：中国石油大学(北京)科研基金项目(No.YJRC-2011-13);中国石油大学(北京)基础学科基金项目(No.JCXK-2011-04)资助

摘　　要：氮杂吲哚是一类重要的杂环分子,在材料科学以及药物设计与合成中具有重要地位。由于氮杂吲哚在结构上区别于吲哚,所以一些经典的合成吲哚的方法并不很适用于氮杂吲哚的合成。近年来,金属有机化学的发展为氮杂吲哚的合成提供了更多的原料选择以及更有效的成环方式,从而为氮杂吲哚的合成开辟了新的方向。本文综述了氮杂吲哚有机合成方法学近年来的进展,介绍了通过Bartoli合成、Fischer吲哚合成、有机锂试剂、过渡金属促进以及其他方法来合成氮杂吲哚类化合物的研究,总结了合成各类氮杂吲哚(4-氮杂吲哚、5-氮杂吲哚、6-氮杂吲哚以及7-氮杂吲哚)的常用有机合成方法,为促进氮杂吲哚类化合物在药物合成化学以及材料科学方面的应用提供了基础。Azaindoles belong to a kind of very important heterocycles, which play a role in material science and drug design and synthesis. Since azaindoles have the different molecular structure compared to indole, many kinds of indole syntheses don＇ t work so efficiently. Recently, the development of organometallic chemistry has supported the azaindole synthesis with more kinds of starting material and more powerful ways to build up the cyclic structure of azaindoles, so it has made the new possibilities to synthesize azaindoles. We have surveyed the development of azaindole synthesis recently. Several ways for the azaindole synthesis, such as Bartoli synthesis, Fischer indole synthesis, organolithium methods, transition-metal mediated methods and so on, have been introduced. This review summarized the very useful methods to synthesize many kinds of azaindoles （4-azaindole, 5-azaindole, 6-azaindole and 7-azaindole）, that will be helpful for the application of azaindole compounds in material science and pharmaceutical synthetic chemistry.

关 键 词：氮杂吲哚 有机合成 过渡金属 

分 类 号：O621.36[理学—有机化学] O626[理学—化学]