三氟甲磺酸酐介导炔酰胺与吡啶加成反应的研究  

Trifluoromethyl Sulfonic Anhydride Mediated Addition of Pyridine with Ynamides

作　　者：宋昊儒 孙建婷 吕敏 刘艺雯 魏邦国 Song Haoru;Sun Jianting;LüMin;Liu Yiwen;Wei Bangguo(School of Chemistry and Chemical Engineering,Nanjing University,Nanjing,Jiangsu 210046;School of Pharmacy,Fudan University,Shanghai 200032)

机构地区：[1]南京大学化学化工学院,南京210046 [2]复旦大学药学院,上海200032

出　　处：《有机化学》2022年第8期2433-2437,共5页Chinese Journal of Organic Chemistry

基　　金：国家自然科学基金(No.21772027)资助项目。

摘　　要：基于三氟甲磺酸酐介导炔酰胺与吡啶加成反应,建立了含烯胺结构吡啶季铵盐的合成方法.经过13个底物拓展验证,采用该方法制备含烯胺结构吡啶季铵盐的收率在65%~90%之间.该方法中吡啶氮原子高区域选择性地与炔酰胺叁键的α位进行加成,且产物以Z构型为主(Z∶E>20∶1).A convenient approach to pyridine quaternary ammonium salts containing enamine fragment has been developed,which features a trifluoromethyl sulfonic anhydride mediated regioselective addition process of pyridine with ynamides.Using this method,a variety of substituted pyridine quaternary ammonium salts containing enamine fragment 3 a~3 m were prepared in moderate to excellent yields with high regioselectivities(Z∶E up to 20∶1).

关 键 词：炔酰胺 吡啶 加成反应 吡啶季铵盐 

分 类 号：O621.25[理学—有机化学]