一种合成氮丙啶衍生物的新方法

A noval synthesis of azirdine derivatives

研究了一种高效合成氮丙啶类化合物的新方法,以2-溴烯丙胺和取代苯基异硫氰酸酯为原料,无水DMSO作为溶剂,在室温下生成相应的硫脲加成产物,继而采用"一锅法"合成技术,以碘化亚铜为催化剂,K2CO3为碱,在100℃下反应4h,以较高产率得到了相应的氮丙啶类化合物.合成的产物经1 HNMR,13CNMR和MS表征确认.该合成方法具有新颖,高效和简便等优点.

A novel and efficient synthesis of aziridine derivatives has been developed.Using 2-bromoallylamine and substituted isothiocyanatobenzenes as starting materiels,the corresponding thioureas could be readily obtained in dry DMSO at room temperature.The subsequent ＂one-pot＂ reactions of the thioureas which would offer the corresponding aziridine derivatives in moderate to good yields were catalyzed by CuI,and mediated with K2CO3at 100 ℃ for 4hrs.The structures of the products were confirmed by1HNMR,13CNMR,and MS.This method provided a novel,efficient and concise route to synthesize the aziridine compounds.