Rh-I-Catalyzed Site-Selective Decarbonylative Alkenylation and Arylation of Quinolones under Chelation Assistance

Abstract

An efficient catalytic system for the C-2 selective C-H functionalization of 4-quinolones was developed by using a decarbonylative coupling strategy. The installation of an N-pyrimidyl group on the quinolone nitrogen atom redirected the coordination between the catalyst and the carbonyl group to promote direct C-H functionalization at the 2-position of 4-quinolones. In addition, the present protocol was successfully applied to the C-3 selective installation of a variety of aryl and vinyl groups on an isoquinolone scaffold.