化学
酚类
配体(生物化学)
芳基
组合化学
基质(水族馆)
药物发现
衍生工具(金融)
有机化学
立体化学
地质学
烷基
受体
经济
海洋学
金融经济学
生物化学
作者
Peng Wang,Marcus E. Farmer,Xing Huo,Pankaj Jain,Peng‐Xiang Shen,Mette Ishoey,James E. Bradner,Steven R. Wisniewski,Martin D. Eastgate,Jin‐Quan Yu
摘要
Here we report the development of a versatile 3-acetylamino-2-hydroxypyridine class of ligands that promote meta-C–H arylation of anilines, heterocyclic aromatic amines, phenols, and 2-benzyl heterocycles using norbornene as a transient mediator. More than 120 examples are presented, demonstrating this ligand scaffold enables a wide substrate and coupling partner scope. Meta-C–H arylation with heterocyclic aryl iodides as coupling partners is also realized for the first time using this ligand. The utility for this transformation for drug discovery is showcased by allowing the meta-C–H arylation of a lenalidomide derivative. The first steps toward a silver-free protocol for this reaction are also demonstrated.
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