6-三氟甲基烟酸的合成研究  

Study on the synthesis of 6-(trifluoromethyl) nicotinic acid

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)

机构地区：[1]河南师范大学化学化工学院河南省手性醇类药物工程技术研究中心,河南新乡453007

出　　处：《化学研究与应用》2019年第1期113-117,共5页Chemical Research and Application

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.

关 键 词：6-三氟甲基烟酸 氰基乙酸 三氟乙酸 

分 类 号：O623.6[理学—有机化学]