Blue-Light-Induced Stereoselective Synthesis of α-Alkylated Amino Acid Derivatives

Abstract

A photoredox-catalyzed decarboxylative C(sp³)−H alkylation of glycine derivatives, utilizing (+)/(−)-camphorsultam as a chiral auxiliary and alkyl N-hydroxyphthalimide (NHP) ester as a radical precursor, has been developed, providing an efficient approach for the stereoselective synthesis of valuable enantioenriched unnatural α-alkylated amino acid derivatives. The methodology operates under mild conditions, demonstrates broad substrate tolerance, and exhibits excellent stereoselectivity. Preliminary mechanistic investigations indicate that the reaction proceeds via a radical pathway.