天冬氨酸导向的钯催化肽的C(sp)-H芳基化反应
Palladium-Catalyzed C(sp)-H Arylation of Peptides Directed by Aspartic Acid.
作者信息
Weng Yiyi, Zhan Xuecheng, Zhang Yiyang, Lin Wen
机构信息
College of Pharmaceutical Sciences, Zhejiang University of Technology, Hangzhou 310014, P. R. China.
出版信息
J Org Chem. 2023 Feb 17;88(4):2334-2343. doi: 10.1021/acs.joc.2c02755. Epub 2023 Jan 29.
Herein, we report a palladium-catalyzed C(sp)-H di- or monoarylation of short peptides containing N-terminal benzamide groups using aspartic acid (Asp) as an endogenous directing group. This strategy has the following merits: a broad substrate scope, selective diarylation of peptides, and gram-scale synthesis. Furthermore, this strategy can be successfully utilized to synthesize peptide-peptide conjugates.
在此，我们报道了一种钯催化的以天冬氨酸（Asp）作为内源性导向基团，对含有N-末端苯甲酰胺基团的短肽进行C(sp)-H双芳基化或单芳基化反应。该策略具有以下优点：底物范围广、肽的选择性双芳基化以及克级规模合成。此外，该策略可成功用于合成肽-肽缀合物。
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