盐酸阿苯达唑亚砜的合成

Synthesis of Albendazole Sulfoxide Hydrochloride

以阿苯达唑为原料,采用一锅合成法,通过氧化、酸化反应得到目标产物盐酸阿苯达唑亚砜。以丙酮为反应溶剂,当阿苯达唑和盐酸的投料比为30 g∶13 mL,阿苯达唑和双氧水的投料比为1∶1.01(n∶n),反应时间为30 min时,制备的盐酸阿苯达唑亚砜的收率为95.78%,通过IR、1H-NMR1、3C-NMR和ESI-MS分析对其产物结构进行了确证。

Albendazole sulfoxide hydrochloride was synthesized with albendazole as raw materials by oxidation and acidification adopting one - step synthesis method. The yield of albendazole sulfoxide hydrochloride was 95.78% when the feed ratio of albendazole to hydrochloride was 30 g ： 13 mL, the feed ratio of albendazole to hydrogen peroxide was 1 ： 1.01, the reaction time was 30 rain. The structure of target substance was determined by IR, ^1H - NMR, ^13C - NMR and ESI - MS.