Institut für Organische und Biomolekulare Chemie, Georg-August-Universität, Tammanstr. 2, 37077, Göttingen, Germany.
DZHK (German Center for Cardiovascular Research), Germany.
Angew Chem Int Ed Engl. 2019 Feb 4;58(6):1684-1688. doi: 10.1002/anie.201811668. Epub 2019 Jan 9.
Bioorthogonal late-stage diversification of structurally complex peptides has enormous potential for drug discovery and molecular imaging. In recent years, transition-metal-catalyzed C-H activation has emerged as an increasingly viable tool for peptide modification. Despite major accomplishments, these strategies largely rely on expensive palladium catalysts. We herein report an unprecedented cobalt(III)-catalyzed peptide C-H activation, which enables the direct C-H functionalization of structurally complex peptides, and sets the stage for a multicatalytic C-H activation/alkene metathesis/hydrogenation strategy for the assembly of novel cyclic peptides.
生物正交的复杂结构肽的晚期多样化在药物发现和分子成像方面具有巨大的潜力。近年来，过渡金属催化的 C-H 活化已成为一种越来越可行的肽修饰工具。尽管取得了重大成就，但这些策略在很大程度上依赖于昂贵的钯催化剂。在此，我们报告了一种前所未有的钴(III)催化的肽 C-H 活化，它可以实现复杂结构肽的直接 C-H 功能化，并为多催化 C-H 活化/烯烃复分解/氢化策略的组装新型环状肽奠定了基础。
