Plouch Eleda V, Le Du Eliott, Deville Melanie, Bacsa John, Renata Hans, Blakey Simon B
Department of Chemistry, Emory University, 1515 Dickey Drive, Atlanta, Georgia 30322, United States.
Department of Chemistry, BioScience Research Collaborative, Rice University, Houston, Texas 77005, United States.
Org Lett. 2025 Jul 18;27(28):7627-7632. doi: 10.1021/acs.orglett.5c02198. Epub 2025 Jul 9.
Macrocyclic peptides containing C(sp)-C(sp) side chain cross-links are a rapidly growing subclass of ribosomally synthesized and post-translationally modified peptides (RiPPs), with significant potential in the development of new pharmaceuticals. This report presents a method for the efficient synthesis of derivatives of this class using a diastereoselective cross-electrophile coupling for the formation of the key β-aryl-alkyl cross-link.
含有C(sp)-C(sp)侧链交联的大环肽是核糖体合成和翻译后修饰肽(RiPPs)中一个快速发展的亚类,在新型药物开发中具有巨大潜力。本报告介绍了一种利用非对映选择性交叉亲电偶联形成关键的β-芳基-烷基交联来高效合成此类衍生物的方法。