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

作　　者：雷容超 兰文捷 李梦竹 傅滨[1] Lei Rongchao;Lan Wenjie;Li Mengzhu;Fu Bin(College of Science,China Agricultural University,Beijing 100193)

机构地区：[1]中国农业大学理学院,北京100193

出　　处：《有机化学》2023年第7期2553-2560,共8页Chinese Journal of Organic Chemistry

基　　金：国家重点研发计划(No.2017YFD0200301)资助项目.

摘　　要：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.

关 键 词：吡唑 苯并磺内酰胺 曼尼希加成 吡唑啉酮 碱催化 

分 类 号：TQ460.1[化学工程—制药化工] O626[理学—有机化学]