Pd(II)-Catalyzed Enantioselective C(sp<sup>3</sup>)–H Arylation toward <i>P</i>-Stereogenic Dialkylphosphinamides
Chen-Yue Wang, Tao Zhou, Bing‐Feng Shi
Abstract
Transition-metal-catalyzed enantioselective C–H functionalization has emerged as a promising method for the synthesis of P -stereogenic phosphorus compounds. However, previous reports are limited to the enantioselective functionalization of C(sp 2 )–H bonds of aryl phosphine derivatives. Herein, Pd(II)-catalyzed enantioselective arylation of more challenging C(sp 3 )–H bonds toward P -stereogenic dialkylphosphinamides is achieved through the desymmetrization of gem -diethyl groups. Various P -stereogenic dialkylphosphinamides are obtained with high enantioselectivities using 3,3′-CN 2 -H 8 -BINOL as the chiral ligand. The synthetic potential of this methodology is highlighted by gram-scale preparation and further derivatizations.