苯并磺内酰胺联吡唑化合物的简便合成

A Convenient Approach to Benzosultam-Linked Pyrazole Compounds

报道了一种碱调节的快速合成苯并磺内酰胺联吡唑化合物的方法.在三乙胺和乙酸酐存在下,苯并磺内酰亚胺与吡唑-5-酮能够顺利地进行Mannich反应,并以高收率得到加成产物.推测了可能的反应机理,反应放大到克级规模,同样能够以高收率获得产物.

A base-mediated rapid synthesis of benzosultam-linked pyrazole compounds was developed.The reaction of N-sulfonyl ketimine with pyrazolin-5-one proceeded smoothly to provide the desired products in high yields in the presence of Et3N and Ac2O.The possible mechanism was proposed.This reaction could be conducted on a gram-scale with maintained high yield.