芳香杂环甲基卤代反应  

Halogenation of Heteroaromatic Side Chain

作　　者：范柏林[1] 刘增路[1] 唐玫[1] 毛振民[1] 

机构地区：[1]上海交通大学药学院,上海200240

出　　处：《广州化学》2008年第2期67-71,共5页Guangzhou Chemistry

摘　　要：总结了五元、六元及其它芳香杂环的甲基卤代的制备方法,如甲基呋喃、甲基噁唑及甲基吡啶的溴化条件等。主要有三种方法:(1)芳香杂环甲基直接以N-溴代丁二酰亚胺(N-Bromosuccinimide,NBS)溴化。(2)以芳香杂环的羟基甲基与三苯基磷和四溴化碳反应。(3)通过预留卤代甲基来生成相应的芳香卤代甲基,如3-氯甲基-1H-吡唑-羧酸乙酯的合成。Approaches to synthesize halogenomethyl of five or six member and other heteroaromatic compounds were described. For example, bromonation conditions of the furan, oxazole and pyridine side chain were reviewed. There are three methods to prepare heteroaromatic halogenomethyl. Firstly, heteroaromatic methyl directly brominated by NBS. Secondly, heteroaromatic hydroxylmethyl was handled by triphenylphosphine and carbon tetrabromide. Thirdly, heteroaromatic halogenomethyl was prepared by the resivation of halogenomethyl, such as the preparation of methyl 3-（chloromethyl）-1H-pyrazole-4-carboxlyale.

关 键 词：卤代 杂环 合成 

分 类 号：O626[理学—有机化学]