Tetrahedron p. 3602 - 3607 (2018)
Update date:2022-09-26
Topics:
Ma, Chunhua
Miao, Yuqi
Zhao, Minghao
Wu, Ping
Zhou, Jianglu
Li, Zhi
Xie, Xilei
Zhang, Wei
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.
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