A palladium-/copper-catalyzed intermolecular C-H amination reaction of indoles has been developed. This reaction proceeds in good to excellent yields to produce a variety of 2-amino-substituted indoles and exhibits excellent regioselectivity at room temperature. Furthermore, chloroamination of indoles provides a simple method for the construction of C-N and C-Cl bonds in one step.
Modification process
申请人:THE GOODYEAR TIRE & RUBBER COMPANY
公开号:EP0312484B1
公开(公告)日:1993-11-24
Copper-Catalyzed Chloroamination of Alkynes: Highly Regio- and Stereoselective Synthesis of (E)-β-Chloro-Enesulfonamides
An efficient copper catalysis system for the chloroamination of alkynes with chlorosulfonamide at room temperature is described, providing a highly regio- and stereoselective procedure for the synthesis of (E)-β-chloro-enesulfonamides in moderate to good yields.