Postsynthetic modification of peptides: Chemoselective C-arylation of tryptophan residues

Abstract

Born to be mild : The general, direct and selective C2 arylation of native Trp-containing peptides can be achieved by palladium-catalyzed C-H activation with aryl iodides in water, under microwave irradiation for a short time (see scheme). Under these mild conditions, the structural and stereochemical integrity of peptides is preserved. © 2010 Wiley-VCH Verlag GmbH & Co. KGaA.