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

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).