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Organic Photoredox-Catalyzed Site-Selective Alkylation of Glycine Derivatives and Peptides via Infrequent 1,2-Hydrogen Atom Transfer of Amidyl Radicals

Jinyu Hou, Hongying Fan, Xue Zhang, Xingyu Liu, Jian Chen, Guanghui Lv, Shiyun He, Li Hai, Zhongzhen Yang, Yong Wu

2024Organic Letters26 citationsDOI

Abstract

Herein, we disclose a visible-light-driven photoredox-catalyzed protocol for site-selective alkylation of glycine derivatives via 1,2-hydrogen atom transfer, which is distinguished by metal free and mild conditions, high chemoselectivity, and good functional group compatibility. This protocol provides a unique approach for synthesizing valuable α,β-diamino acid derivatives. Furthermore, the potential synthetic merit of this transformation is proven by a scale-up reaction and late-stage functionalization of peptides.

Topics & Concepts

ChemistryAlkylationChemoselectivityCombinatorial chemistryPhotoredox catalysisHydrogen atomCatalysisRadicalGlycineFunctional groupOrganic chemistryPhotochemistryAmino acidPhotocatalysisGroup (periodic table)PolymerBiochemistryRadical Photochemical ReactionsCatalytic C–H Functionalization MethodsSulfur-Based Synthesis Techniques