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Simple and Efficient Copper-Catalyzed Approach to 2,4-Disubstituted Imidazolones

Xiaoyu Gong, Haijun Yang, Hongxia Liu, Yuyang Jiang, Yufen Zhao and Hua Fu*

*Key Laboratory of Bioorganic Phosphorus Chemistry and Chemical Biology (Ministry of Education), Department of Chemistry, Tsinghua University, Beijing 100084, P. R. China, Email: fuhuamail.tsinghua.edu.cn

X. Gong, H. Yang, H. Liu, Y. Jiang, Y. Zaho, H. Fu, Org. Lett., 2010, 12, 3128-3131.

DOI: 10.1021/ol1008813


Abstract

A simple and efficient approach to 4-arylidene-2-alkyl-4,5-dihydro-1H-imidazol-5-ones (2,4-disubstituted imidazolones) uses readily available 2-bromo-3-alkylacrylic acids and amidines as the starting materials without addition of any ligand or additive. The reaction is performed under mild conditions and will be of wide application in organic chemistry and medicinal chemistry.

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Key Words

Imidazol-5-ones


ID: J54-Y2010-1930