4-氯-2-甲基吡啶并[3,2-d]嘧啶的合成  

Synthesis of 4-chloro-2-methylpyrido[3,2-d]pyrimidine

作　　者：肖俊丽 骆荣双 刘钊 周志旭[1,2] 赵春深 XIAO Jun-li;LUO Rong-shuang;LIU Zhao;ZHOU Zhi-xu;ZHAO Chun-shen(School of Pharmaceutical Sciences,Guizhou University,Guiyang 550025,China;Guizhou Engineering Laboratory for Synthetic Drugs,Guiyang 550025,China)

机构地区：[1]贵州大学药学院,贵州贵阳550025 [2]贵州省合成药物工程实验室,贵州贵阳550025

出　　处：《化学研究与应用》2022年第2期444-448,共5页Chemical Research and Application

基　　金：贵州省科技计划项目(黔科合基础[2020]1Y393)资助。

摘　　要：吡啶并嘧啶类衍生物具有较好的生物活性,4-氯-2-甲基吡啶并[2,3-d]嘧啶是一种重要的医药中间体,已报道的合成方法成本较高且操作繁琐,不适合工业化生产。本文以2-氯-3-硝基吡啶为起始原料,经取代、还原、环合等5步反应得到目标化合物,产物结构经^(1)H NMR,^(13)C NMR和MS确证,总收率为33%。该路线具有成本低、反应条件温和、后处理简单、副产物少、收率较高等优点,是一条适合工业化生产的合成路线。Pyridopyrimidine derivatives are considered outstanding because of their good biological activity.4-Chloro-2-methylpyrido[2,3-d]pyrimidine is an important pharmaceutical intermediate.The reported synthetic methods of target compound are high cost and cumbersome to operate,and are not suitable for industrial production.In this paper,the target compound was obtained,which was based on 2-chloro-3-nitropyridine by means of five steps of substitution,reduction and cyclization and so on.The structure of product was confirmed by ^(1)H NMR,^(13)C NMR and MS,with an overall yield was 33%.This route had the advantages of low cost,mild reaction conditions,simple post-treatment,less by-products,and high yield.Therefore,this was a suitable synthetic route for industrial production.

关 键 词：2-氯-3-硝基吡啶 4-氯-2-甲基吡啶并[3 2-d]嘧啶 合成 

分 类 号：O626.3[理学—有机化学]