Palladium(II)-Catalyzed\nSite-Selective C(sp<sup>3</sup>)–H Alkenylation of Oligopeptides

An innovative palladium-catalyzed alkenylation of peptides\nand\nvinyl iodides has been developed. This method does not require the\nintroduction of a directing group and uses carboxylic acid groups\nas endogenous directing groups. It is noteworthy that two key building\nblocks for the ilamycins and CXCR7 modulators were prepared using\nour methodology. In addition, the free carboxylic acid residue can\nbe linked to a variety of other compounds, providing a novel approach\nto the synthesis of peptide drugs in the future.