Study On Palladium-catalyzed Diamination Of Alkene

Diamine compounds are widely existed in biologically active compounds and natural products, meanwhile, many drug molecules also contain diamine nitrogen heterocyclic scaffold. As a result, more and more attentions have been paied to the methods on the economical, environmental friendly, efficient and rapid construction of C-N bond to give new diamine compounds. Until now, it is the most directly, effective and simple method to synthesize diamines via transit ion-metal-catalyzed difunctional reaction of olefins. Recently,there were large progress in the diamination reaction of olefins. However, the use of highly efficient transition metal catalysts and nitrogen sources for the synthesis of new diamine compounds have a higher research value and application prospects.This study aims to research palladium-catalyzed diamination reaction of alkenes, with the conditions of Pd(OAc)2 as catalyst, 2,2'-bipyridine as ligand in tetrahydrofuran, Using the common and oxidizing N-fluorobenzenesulfonamide as the nitrogen source under 80 ?, the reaction can efficiently get diamination product in the air, and the yield is up to 90%. This reaction is widely applicated to the synthesis of o-alkyl-N-alkylbenzamide substrates with various functional groups. Meanwhile, the prominent protocol also offers an appealing alternative for the preparation of drugs containing isoindolinone skeleton. Therefore, this protocol will have wide application in pharmaceuticals industry due to its simple,easy-to-operate procedure.