Chen Zhilong, Wang Xiaodong
Center for Integrative Chemical Biology and Drug Discovery, Division of Chemical Biology and Medicinal Chemistry, Eshelman School of Pharmacy, University of North Carolina at Chapel Hill, Chapel Hill, NC 27599, USA.
Org Biomol Chem. 2017 Jul 21;15(27):5790-5796. doi: 10.1039/c7ob01237c. Epub 2017 Jun 29.
Tricyclic biaryls are important scaffold structures in many natural products and lead compounds in drug discovery. The formation of a biaryl unit is often the key step for the synthesis of tricyclic biaryls. Despite significant progress toward the synthesis of biaryl compounds in recent years, the direct cross-coupling of two different aryl halides is still challenging and robust methods are lacking. Herein we report a direct cross-coupling of two different aryl halides in the presence of a palladium catalyst and boron ester, which provides a new and useful complementary method to synthesize tricyclic biaryls.
三环联芳基是许多天然产物中的重要骨架结构，也是药物研发中先导化合物的重要组成部分。联芳基单元的形成通常是合成三环联芳基的关键步骤。尽管近年来在联芳基化合物的合成方面取得了显著进展，但两种不同芳基卤化物的直接交叉偶联仍然具有挑战性，且缺乏稳健的方法。在此，我们报道了在钯催化剂和硼酸酯存在下两种不同芳基卤化物的直接交叉偶联反应，该反应为合成三环联芳基提供了一种新的、有用的补充方法。
