氟康唑合成新工艺研究

Study on the new preparation of fluconazole

摘要: 目的改进氟康唑(fluconzole1)的合成工艺。方法用间二氟苯为起始原料,用4-氨基-1H-1,2,4-三氮唑代替1H-1,2,4-三氮唑,分别采用相转移催化和超声波方法,经三步反应制得氟康唑。结果得氟康唑(1),mp137～141℃,总收率50%。结论符合中国药典2000年版二部的标准,工艺可靠,质量稳定。

Abstract: OBJECTIVE To improve the synthesis technology of fluconazole.METHODS Fluconazole was prepared after three steps reaction with m-difluorobenzenes as starting material and 1H-1,2,4-triazole was replaced by 4-amino-1H-1,2,4-triazole.The phase transfer cataly