Synthesis of 2-aminothiazoles from styrene derivatives mediated by 1,3-dibromo-5,5-dimethylhydrantoin (DBH)
作者:Chunhua Ma、Yuqi Miao、Minghao Zhao、Ping Wu、Jianglu Zhou、Zhi Li、Xilei Xie、Wei Zhang
DOI:10.1016/j.tet.2018.05.021
日期:2018.7
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
据报道,通过DBH介导的苯乙烯和硫脲的氧化环化合成2-氨基噻唑的有效方法。使用DBH作为溴源和氧化剂,通过两步一锅法成功地将各种烯烃成功转化为相应的2-氨基噻唑,产率为10-81%。该方法可以容易地以克为单位进行,并且成功地用于以苯乙烯为起始原料的抗炎药fanetizole的合成。