RSV抑制剂BMS-433771中间体的合成  

Synthesis of Intermediate for RSV Inhibitor BMS-433771

作　　者：刘剑伟 于雯清 周佳 余雅宁 张全升 花现 钟欣怡 LIU Jian-wei;YU Wen-qing;ZHOU Jia;YU Ya-ning;ZHANG Quan-sheng;HUA Xian;ZHONG Xin-yi(Weifang Huitao Chemical Co.,Ltd.,Weifang 261200,China;College of Science&Technology,Ningbo University,Cixi 315302,China)

机构地区：[1]潍坊汇韬化工有限公司,山东潍坊261200 [2]宁波大学科学技术学院,浙江慈溪315302

出　　处：《精细化工中间体》2023年第3期34-37,共4页Fine Chemical Intermediates

摘　　要：1-环丙基-1,3-二氢咪唑并[4,5-C]吡啶-2-酮是人类呼吸道合胞病毒(RSV)抑制剂BMS-433771的关键中间体,以此为基础可以合成一系列氮杂双咪唑酮类RSV抑制剂。以4-羟基吡啶为原料,经硝化、氯化和亲核取代反应、氢化、环化4步反应得到1-环丙基-1,3-二氢咪唑并[4,5-C]吡啶-2-酮,其结构经^(1)H NMR表征确证。该合成工艺操作简单,杂质少,具有工业化应用前景。1-Cyclopropyl-1,3-dihydroimidazolo[4,5-C]pyridinone-2-one is a key intermediate of human respirato-ry syncytial virus(RSV)inhibitor BMS-433771,on the basis of thisintermediate a series of azodimidazolidone RSV inhibitors can be synthesized.Using 4-hydroxypyridine as the raw material,1-cyclopropyl-1,3-dihydroimidazolo[4,5-C]pyridinone-2-one was obtained by nitration,one pot reaction of chlorination and nucleophilic substitution,hydrogenation and cyclization,the structure of the final product was confirmed by^(1)H NMR.The synthetic process is easy to operate with less impurities,so it is suitable for industrial production.

关 键 词：氮杂双咪唑酮 RSV抑制剂 4-羟基吡啶 BMS-433771 

分 类 号：R373[医药卫生—病原生物学]