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One-Pot Stereoselective Synthesis of 2,3-Diglycosylindoles and Tryptophan-C-glycosides via Palladium-Catalyzed C–H Glycosylation of Indole and Tryptophan

Yanan Ding, Ning Li, Yan‐Chong Huang, Wei‐Yu Shi, Nian Zheng, Cui‐Tian Wang, Yang An, Xue‐Yuan Liu, Yong‐Min Liang

2022Organic Letters30 citationsDOI

Abstract

We described a novel palladium-catalyzed C-H glycosylation of indole or tryptophan for a one-pot stereoselective synthesis of 2,3-diglycosylindoles and tryptophan-C-glycosides. In this strategy, the use of air and base-free and ligand-free conditions provided a highly efficient route to construct C-glycosides. The method can be applied to a wide range of cost-effective and convenient glycosyl chloride donors. Mechanistic studies indicated that the indole 2,3-diglycosylation sequence was C3 and then C2.

Topics & Concepts

ChemistryIndole testStereoselectivityGlycosylationPalladiumTryptophanCatalysisCombinatorial chemistryGlycosylStereochemistryGlycosideOrganic chemistryAmino acidBiochemistryCatalytic C–H Functionalization MethodsCarbohydrate Chemistry and SynthesisSynthesis and Catalytic Reactions