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Updated: Aug 11, 2025

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Published on: January 3, 2018
Synthesis of 2-iminothiazolidin-4-ones via copper-catalyzed [2 + 1 + 2] tandem annulation
Mingming Zhao1,2, Yiming Guo1,2, Qi Wang1,2
1Guangzhou Institutes of Biomedicine and Health, Chinese Academy of Sciences Guangzhou 510530 P. R. China wu_linping@gibh.ac.cn qiu_fayang@gibh.ac.cn.
Abstract:
In this paper, an efficient synthesis of 2-iminothiazolidin-4-ones through a copper-catalyzed tandem annulation reaction of alkyl amines, isothiocyanates and diazo acetates is presented. Notable advantages of this [2 + 1 + 2] cyclization methodology include readily accessible starting materials, simple operation, mild reaction conditions, high yields, step-economy and diverse functional group tolerance. In addition, the reaction is applicable to the gram scale synthesis and the preparation of bioactive molecules.
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