Pd‐Catalyzed C(sp ² )−H Alkoxycarbonylation of Phenethyl‐ and Benzylamines with Chloroformates as CO Surrogates

The site-selective functionalization of C−H bonds within a complex molecule remains challenging task capital synthetic importance. Herein, an unprecedented Pd-catalyzed C(sp2)−H alkoxycarbonylation phenylalanine derivatives and other amines featuring picolinamide as the directing group (DG) is reported. This oxidative coupling distinguished by its scalability, operational simplicity, avoids use toxic carbon monoxide C1 source. Remarkably, easy cleavage DG enables efficient assembly isoindolinone compounds. Density Functional Theory calculations support PdII/PdIV catalytic cycle.