钯催化的区域选择性和非对映选择性加氢（杂）芳基化用于快速构建含环丁烷的四元中心。
Palladium-Catalyzed Regio- and Diastereoselective Hydro(hetero)arylation for Rapid Construction of Quaternary Center Containing Cyclobutanes.
发表日期：2024 Aug 19
作者：
Furong Tao, Shuaikang Li, Mandalaparthi Phanindrudu, Haifei Yang, Yi Qi, Hui Luo, Jia Zheng
来源：
TROPICAL MEDICINE & INTERNATIONAL HEALTH
摘要：
在此，我们报告了 Pd 催化的失活亚烷基环丁烷的区域和非对映选择性加氢（杂）芳基化。该方案提供了一种快速、原子经济的途径来获取具有良好功能耐受性的 3-环丁基（杂）芳烃。在导向基团的帮助下，对体积较大的γ位发生亲核攻击，形成季碳中心。此外，所选产品还表现出抗肿瘤生物活性。
Herein we report a Pd-catalyzed regio- and diastereoselective hydro(hetero)arylation of inactivated alkylidenecyclobutanes. This protocol provides a rapid and atom-economical route to access 3-cyclobutyl (hetero)arenes with good functionalities toleration. With the assistance of the directing group, nucleophilic attack happened on the bulkier γ-position to form the quaternary carbon center. Furthermore, the selected products exhibited antitumor bioactivities.