Rhodium(Ⅲ)-Catalyzed Intermolecular Unactivated Secondary C(sp3)-H Bond Amidation Assisted by 3,5-Dimethylpyrazole
作者单位：南开大学 State Key Laboratory of Elemento-Organic ChemistryCollege of ChemistryNankai University
会议名称：《中国化学会·第十六届全国有机合成化学学术研讨会》
会议日期：2019年
学科分类：07[理学] 070303[理学-有机化学] 0703[理学-化学]
关 键 词：rhodium unactivated amidation sulfonylureas
摘 要：Transition-metal-catalyzed amination of unactivated C(sp)-H bond has undergone a breakthrough in recent years. However,most of them focus on the primary C(sp)-H bond. Direct amination of intermolecular unactivated secondary C(sp)-H bond still remains highly challenge.Herein,Rh(Ⅲ)-catalyzed intermolecular unactivated secondary C(sp)-H bond amidation reactions via nitrene insertion assisted by 3,5-dimetlylpyrazole have been developed.This procedure tolerates a broad substrates scope including chain and cyclic N-alklyamides under mild conditions.Notably,the directing group 3,5-dimethylpyrazole of chain N-alkylamide substrates could be easily removed via cascade intermolecular amidation and intramolecular cyclization in one-pot affording the sulfonylureas by increasing the reaction temperature.