通过钯催化吡啶酰胺导向的分子内 C(sp^2)-H 芳基化反应构建环芳撑支撑的肽大环。
Construction of Cyclophane-Braced Peptide Macrocycles via Palladium-Catalyzed Picolinamide-Directed Intramolecular C(sp)-H Arylation.
机构信息
State Key Laboratory and Institute of Elemento-Organic Chemistry, College of Chemistry, Nankai University, Tianjin 300071, China.
出版信息
Org Lett. 2020 Sep 4;22(17):6879-6883. doi: 10.1021/acs.orglett.0c02422. Epub 2020 Aug 19.
PMID:32813530
Abstract
A versatile method for the construction of C(sp)-linked cyclophane peptide macrocycles via Pd-catalyzed picolinamide-directed intramolecular arylation of aryl and alkenyl C-H bonds of amino acid side chains with aryl iodides is developed. This method provides simple and efficient access to a variety of cyclophane-braced structures from readily accessible linear peptide precursors.
摘要
发展了一种通过钯催化的吡啶酰胺导向的氨基酸侧链芳基和烯基 C-H 键与芳基碘化物的分子内芳基化反应构建 C(sp)-连接的环芳烷肽大环的通用方法。该方法提供了一种从易得的线性肽前体简单高效地获得各种环芳烷支撑结构的方法。
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