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Synthesis of 2-Amino-5-acylthiazoles by a Tertiary Amine-Promoted One-Pot Three-Component Cascade Cyclization Using Elemental Sulfur as a Sulfur Source

Rong-Geng Fu*, Yong Wang, Fei Xia, Hao-Lin Zhang, Yuan Sun, Duo-Wen Yang, Ye-Wei Wang and Peng Yin

*School of Pharmacy, Hunan University of Chinese Medicine, Changsha 410208, People's Republic of China, Email: furonggenghnucm.edu.cn

R.-G. Fu, Y. Wang, F. Xia, H.-L. Zhang, Y. Sun, D.-W. Yang, Y.-W. Wang, P. Yin, J. Org. Chem., 2019, 84, 12237-12245.

DOI: 10.1021/acs.joc.9b02032



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Abstract

A one-pot three-component cascade cyclization of enaminones, cyanamide, and elemental sulfur provides 2-amino-5-acylthiazoles in good yields with good functional group tolerance. This method offers an effective way for accessing valuable and potentially bioactive 2-amino-5-acylthiazole derivatives.

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Key Words

thiazoles, multicomponent reactions


ID: J42-Y2019