摘要
6-三氟甲基烟酸是合成含氟药物关键中间体,本文以氰基乙酸和三氟乙酸为原料,经过加成-消除、Stork烷基化、缩合成环、水解等多步反应得到目标化合物。经优化反应条件,该路线的总收率达到45%。该路线原料易得、收率高、操作简单且重复性好。
6-(Trifluoromethyl)nicotinic acid is a key intermediate in the synthesis of fluorine-containing drugs.2-Isocyano acetic acid and trifluoroacetic acid were used as starting materials to obtain the target compound via multi-step reactions,includingaddition-elimination,Stork enamine alkylation,condensation-cyclization,and hydrolysis.After optimization of the reaction conditions,the total yield of this route reached 45%.The advantages of this route included easy-to-access raw materials,high yield,simple operation,and good repeatability which made it suitable for industrial-scale production.
作者
徐桂清
周应杰
毛龙飞
李伟
XU Gui-qing;ZHOU Ying-jie;MAO Long-fei;LI Wei(School of Chemistry and Chemical Engineering,Henan Engineering Research Center of Chiral Hydroxyl Pharmaceutical,Henan normal university,Xinxiang 453007,China)
出处
《化学研究与应用》
CAS
CSCD
北大核心
2019年第1期113-117,共5页
Chemical Research and Application
关键词
6-三氟甲基烟酸
氰基乙酸
三氟乙酸
6-(trifluoromethyl)nicotinic acid
2-isocyano acetic acid
trifluoroacetic acid
作者简介
毛龙飞(1988-),男,实验师,主要从事药物合成工艺研究。E-mail:longfeimao1988@163.com
