GEN-617的合成工艺优化  

Process optimization for synthesis of GEN-617

作　　者：张铁 陈文章 毛政益 ZHANG Tie;CHEN Wen-zhang;MAO Zheng-Yi(Zunyi Vocational and Technical College,Zhunyi 563000,China;Guizhou Provincial Engineering Technology Research Center for Chemical Drug R&D,Guiyang 550004,China;People’s Hospital of Wugang,Wugang 422400,China)

机构地区：[1]遵义职业技术学院,贵州遵义563000 [2]贵州省化学合成药物研发利用工程技术研究中心,贵州贵阳550004 [3]武冈市人民医院,湖南武冈422400

出　　处：《化学研究与应用》2021年第8期1622-1625,共4页Chemical Research and Application

基　　金：贵州省科技厅项目(黔科合支撑(2017)2842号)资助。

摘　　要：以便宜易得的对氟苯甲腈(2)为起始原料经亲核取代、氧化、还原得到关键中间体(5),5与咪唑并[1,2-α]吡啶-7-羧酸(6)缩合以56.4%总收率制得GEN-617。该路线原料易得、反应条件温和、操作简单,具有良好的工业化前景。Using the inexpensive and readily available 4-fluorobenzonitrile( 1 )as starting material,key intermediate 5 was synthesized by nucleophilic substitution,oxidation and reducetion.Then coupled with the intermediate imidazo[1,2- a ]pyridine-7-carboxylic acid the desired compound GEN-617 was obtained in 56.4%overall yield.With the advantages of easy availability of raw materials,easy handling,milder reaction conditiom,this route was suitable for the industrial production.

关 键 词：对氟苯乙腈 咪唑并[1 2-A]吡啶-7-羧酸 工艺优化 GEN-617 

分 类 号：O626[理学—有机化学]