盐酸阿扎司琼合成工艺研究

Study on the synthesis of azasteron hydrochloride

盐酸阿扎司琼(Azasetron hydrochloride)是一种高选择性,副作用低的5-HT3受体拮抗剂。本研究通过文献调研发现目前已报道的合成路线存在着工艺复杂,污染大等问题。针对这些问题,本研究报道了一条更加简便,环保,有工业化潜力的路线,通过五步反应得到目标产物,其结构经1H-NMR、13C-NMR及MS确认,总收率67.5%。

Azasetron hydrochloride is a highly specific antagonist 5-HT3 receptor antagonist with low side effects.Through literature research,it found that the complex process,high-continual pollution were the drawbacks of the reported synthetic routes.So a new method which was more convenient,environmentally friendly,and suitable for industrial production was reported.The target compound was obtained by five steps in total yield of 67.5%,the structure was confirmed by 1H-NMR,13C-NMR and MS.