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1. (WO2017151910) SELECTIVE METAL-MEDIATED ARYLATION OF DICHALCOGENIDES IN BIOMOLECULES

Pub. No.:    WO/2017/151910    International Application No.:    PCT/US2017/020438
Publication Date: Sat Sep 09 01:59:59 CEST 2017 International Filing Date: Fri Mar 03 00:59:59 CET 2017
IPC: A61K 38/14
Applicants: MASSACHUSETTS INSTITUTE OF TECHNOLOGY
Inventors: BUCHWALD, Stephen, L.
PENTELUTE, Bradley, L.
ZHANG, Chi
Title: SELECTIVE METAL-MEDIATED ARYLATION OF DICHALCOGENIDES IN BIOMOLECULES
Abstract:
Disclosed are methods of selective cysteine and seienocysteine modification on peptide/protein molecules under physiologically relevant conditions. The methods feature several advantages over existing methods of peptide modification, such as specificity towards thiols and selenols over other nucleophiles (e.g., amines, hydroxy Is), excellent fijnctional group tolerance, and mild reaction conditions, including completely aqueous reaction conditions. Also disclosed are methods of preparing palladium complexes in the presence of oxygen.