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Synthesis of 2-aminothiazoles from styrene derivatives mediated by 1,3-dibromo-5,5-dimethylhydrantoin (DBH) |
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| Authors: | Chunhua Ma Yuqi Miao Minghao Zhao Ping Wu Jianglu Zhou Zhi Li Xilei Xie Wei Zhang |
| Institution: | 1. School of Chemistry and Chemical Engineering, Henan Normal University, Collaborative Innovation Center of Henan Province for Green Manufacturing of Fine Chemicals, Henan Key Laboratory of Organic Functional Molecule and Drug Innovation, Xinxiang 453007, China;2. School of Pharmacy, Fudan University, Shanghai 201203, China;3. College of Chemistry, Chemical Engineering and Materials Science, Shandong Normal University, Jinan 250014, China |
| Abstract: | An efficient procedure for the synthesis of 2-aminothiazoles via DBH-mediated oxidative cyclization of styrenes and thioureas is reported. Various alkenes were successfully transformed to the corresponding 2-aminothiazoles in yields of 10–81% via a two-step one-pot manner using DBH as both the bromine source and oxidant. The method can be readily carried out in gram-scale and successfully applied to the synthesis of anti-inflammatory drug fanetizole using styrene as starting material. |
| Keywords: | 2-Aminothiazole 1 3-Dibromo-5 5-dimethylhydrantoin Alkenes Heterocycles Oxidative cyclization |
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