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Palladium-Catalyzed Regio- and Diastereoselective Hydro(hetero)arylation for Rapid Construction of Quaternary Center Containing Cyclobutanes.

作者信息

Tao Furong, Li Shuaikang, Phanindrudu Mandalaparthi, Yang Haifei, Qi Yi, Luo Hui, Zheng Jia

机构信息

The Marine Biomedical Research Institute, School of Ocean and Tropical Medicine, Guangdong Medical University, Zhanjiang, Guangdong 524023, China.

The Marine Biomedical Research Institute of Guangdong Zhanjiang, Zhanjiang, Guangdong 524023, China.

出版信息

Org Lett. 2024 Aug 30;26(34):7222-7226. doi: 10.1021/acs.orglett.4c02645. Epub 2024 Aug 19.

DOI:10.1021/acs.orglett.4c02645
PMID:39158209
Abstract

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.

摘要

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