硝唑尼特合成工艺的研究

Research on synthesis of nitazoxanide

由乙酰水杨酸和2-氨基-5-硝基噻唑为原料,选用N,N-二甲基甲酰胺和三乙胺分别作为催化剂和缚酸剂,经酰胺化反应生成一种抗寄生虫新药—硝唑尼特,其较佳的工艺条件:酰氯化反应温度70℃,氯化亚砜与乙酰水杨酸的摩尔比为1.3∶1,乙酰水杨酸与2-氨基-5-硝基噻唑的摩尔比为1.4∶1,酰胺化反应时间2.5 h,收率达76.8%。该工艺简单,收率高,具有较好的应用价值。

A new-type antiparasitic drug,nitazoxanide,was synthesized through amidation from acetylsalicylic acid and 2-amino-5-nitrothiazole in the presence of N,N-dimethylform amide as catalyst and triethylamine as acid acceptor.The optimal conditions were as follows： the temperature of acyl chloride is 70 ℃,the molar ratio of SOCl2 to acetylsalicylic acid is 1.3∶1,the molar ratio of acetylsalicylic acid to 2-amino-5-nitrothiazole is 1.4∶1,the reaction time of amidation is 2.5 h.Under such optimal reaction conditions,the conversion can reach 76.8%.Owning to its simple process and high yield,the development of nitazoxanide synthesis has an excellent prospect.