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Demethylative Alkylation of Methionine Residue by Employing the Sulfonium as the Key Intermediate

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journal contribution
posted on 20.10.2021, 18:45 authored by Qi-Long Hu, Jia-Tian Liu, Jian Li, Yang Ge, Zhendong Song, Albert S. C. Chan, Xiao-Feng Xiong
Methionine (Met) offers a valuable handle to achieve peptide chemical modification owing to its unique thioether functional group. In contrast with cysteine, the site-selective functionalization of the hydrophobic and redox-sensitive thioether motif on peptides is still challenging, and strategies for diversification on the Met residue are rarely disclosed. Herein we report a transition-metal-free and redox-neutral approach for Met diversification with substrate diversity, which could be applied to synthesize cyclic peptides.