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Updated: Feb 11, 2026

Functionalized Spirocyclic Heterocycle Synthesis and Cytotoxicity Assay
Published on: February 9, 2021
A 2-(1-methylhydrazinyl)pyridine-directed C-H functionalization/spirocyclization cascade: facile access to
Hua Zhao1, Xiaoru Shao, Taimin Wang
1State Key Laboratory of Chemical Oncogenomics, School of Chemical Biology and Biotechnology, Shenzhen Graduate School of Peking University, Shenzhen 518055, China. zhaihb@pkusz.edu.cn.
Abstract:
A cobalt-catalyzed oxidative coupling of benzoic hydrazides with maleimides by utilizing 2-(1-methylhydrazinyl)pyridine as a bidentate directing group has been developed. This C-H functionalization/spirocyclization cascade protocol shows high efficiency and remarkable functional group tolerance, and the ubiquitous spirosuccinimides were obtained in good to excellent yields with high regioselectivity. This strategy also provides a novel and efficient access to diverse symmetric and unsymmetrical bisspirosuccinimides.
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