CF_(3)SO_(2)Na为氟源“一锅法”合成四个三氟甲基吡啶化合物  

Synthesis of Four Trifluoromethyl Pyridine by “One-pot” Method with CF_(3)SO_(2)Na as Fluorine Source

作　　者：吴浩 戴洪玉 廖万鹏 吴凤 周志旭 黄筑艳[1,2,3] WU Hao;DAI Hong-yu;LIAO Wan-peng;WU Feng;ZHOU Zhi-xu;HUANG Zhu-yan(Guizhou Weimen Pharmaceutical Company Limited,Guiyang 550018,China;School of Pharmaceutical Sciences,Guizhou University,Guiyang 550025,China;Guizhou Engineering Laboratory for Synthetic Drugs,Guiyang 550025,China)

机构地区：[1]贵州威门药业股份有限公司,贵州贵阳550018 [2]贵州大学药学院,贵州贵阳550025 [3]贵州省合成药物工程实验室,贵州贵阳550025

出　　处：《广州化学》2022年第2期34-39,共6页Guangzhou Chemistry

基　　金：贵州省科技计划项目(黔科合基础[2020]1Y393)。

摘　　要：从原料价廉易得、反应条件温和、后处理简洁和产率较高的原则出发,设计了一条制备三氟甲基吡啶化合物的优化合成路线。以CF_(3)SO_(2)Na为CF_(3)源,在叔丁基过氧化氢(TBHP)作用下,在吡啶不同位点引入三氟甲基,得到了一系列目标化合物,其中化合物A1收率为68.3%,化合物A2收率为64.9%,化合物A3和A4收率分别为79.3%和78.6%,其结构经1H-NMR和MS确证。Based on the principles of cheap raw materials,mild reaction conditions,simple post-treatment and high yield,a synthetic route of trifluoromethyl pyridine compounds was designed.Using CF_(3)SO_(2)Na as CF_(3) source,a series of target compounds was synthesized by introducing CF;at different positions of Pyridine in the presence of tert-butyl peroxide (TBHP).The yield of compound A1 was 68.3%,compound A2 was 64.9%,compounds A3 and A4 were 79.3% and 78.6%,respectively.The structure was confirmed by;H-NMR and MS.

关 键 词：三氟甲基化 芳环 一锅法合成 吡啶 CF_(3)SO_(2)Na 

分 类 号：O626.3[理学—有机化学]