School of Pharmaceutical Sciences, Zhengzhou University, Zhengzhou, 450001, China.
College of Chemistry and Molecular Engineering, Zhengzhou University, Zhengzhou, 450001, China.
Top Curr Chem (Cham). 2020 Feb 17;378(2):23. doi: 10.1007/s41061-020-0285-9.
Biaryl scaffolds are prevalent in natural products and drug molecules, and biaryl-containing compounds have been shown to exhibit diverse and interesting biological activities. To date, numerous synthetic methods, particularly direct C-H bond activation, have been developed for the construction of such scaffolds, due to their interesting structural features and biological profiles. We highlight herein recent advances in the construction of biologically important biaryl fragments through direct C-H bond activation and also demonstrate the application of direct C-H arylation in the total synthesis of biaryl-containing natural products and drug molecules. Selected biaryl-containing compounds.
联苯骨架在天然产物和药物分子中很常见，含联苯的化合物表现出多种多样的有趣的生物活性。迄今为止，由于其有趣的结构特征和生物特性，已经开发出许多合成方法，特别是直接 C-H 键活化方法，用于构建此类支架。我们在此重点介绍了通过直接 C-H 键活化构建生物重要的联苯片段的最新进展，并展示了直接 C-H 芳基化在含有联苯的天然产物和药物分子的全合成中的应用。
