摘要/Abstract

苯并稠杂环化合物具有广泛且重要的药理及生物活性, 在药物合成与研发领域有着重要的应用价值, 因而其合成方法倍受关注. 由于存在多个官能团和反应位点, 以2-卤代苯甲酰胺为重要合成子合成喹唑啉酮、异喹啉酮、异吲哚酮和苯并异噻唑酮等苯并杂环化合物取得了巨大进展. 鉴于此, 根据产物结构的不同, 概述近10年来以2-卤苯甲酰胺为起始原料合成苯并杂环化合物的研究进展, 并对相关的反应机理进行了阐述.
关键词: 2-卤苯甲酰胺, 金属催化, 串联反应, 环化反应, 苯并杂环化合物, 反应机理
Owing to important pharmacological and biological activities of benzoheterocyclic compounds, their exploration for efficient synthesis methods in drug field is of great value and wide application. Due to the existence of multiple functional groups and reaction sites, great progress has been made in the synthesis of quinazolinones, isoquinolinones, isoindolinones, benzisothiazolones and other benzoheterocyclic compounds using 2-halobenzamides as important synthons. In view of this, according to the different structures of the products, the research progress in the synthesis of benzoheterocyclic compounds with 2-halobenzamides as the starting material in recent 10 years is summarized, and the related reaction mechanism is expounded.
Key words: 2-halobenzamide, metal catalysis, domino reaction, cyclization reaction, benzoheterocyclic compound, reaction mechanism


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