Metal-Free Late-Stage Alkylation of Tryptophan and Tryptophan-Containing Peptides with 1,3-Dithiane Derivatives
ORGANIC LETTERS(2023)
Abstract
Late-stage diversification of structurallycomplex peptides hasenormous potential for drug discovery and molecular imaging. We reporta simple, metal-free, late-stage reductive C2 alkylation of tryptophanand tryptophan-containing peptides using readily available 1,3-dithianes.This alkylation protocol has a wide substrate scope and an excellenttolerance for reactive functional groups.
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Key words
peptides,alkylation,metal-free,late-stage,tryptophan-containing
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