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伏立康唑是是一种广谱的三唑类抗真菌药,其质量一直备受关注,本文用液相色谱法对伏立康唑合成的起始原料(2R,3S/2S,3R)-2-(2,4-二氟苯基)-3-(4-氯-5-氟嘧啶)-1-(1H-1,2,4-三唑-1-基)丁-2-醇盐酸盐中的杂质种类进行定性研究分析。结果可知其原料杂质为1-(2,4)-二氟苯基-2-(1H-1,2,4-三唑-1-基)乙酮及4-乙基-5-氟-嘧啶,它们既是伏立康唑合成中间体,又是降解产物。为确保伏立康唑合成的质量,初步制定了伏立康唑合成起始原料的质量标准,总杂质不得超过10.0%,1-(2,4)-二氟苯基-2-(1H-1,2,4-三唑-1-基)乙酮不得过1.4%,4-乙基-5-氟-嘧啶不得过1.4%。
Voriconazole is a broad-spectrum triazole antifungal drug, its quality has been of great concern. In this paper, the synthesis of voriconazole starting material (2R, 3S / 2S, 3R) -2- (2, 4-difluorophenyl) -3- (4-chloro-5-fluoropyrimidine) -1- (1H-1,2,4-triazol- 1-yl) butan-2-ol hydrochloride Types of qualitative research and analysis. The results showed that the raw material impurities were 1- (2,4) -difluorophenyl-2- (1H-1,2,4-triazol-1-yl) ethanone and 4-ethyl- , They are both voriconazole synthesis intermediates, but also degradation products. In order to ensure the quality of voriconazole synthesis, the quality standard of voriconazole synthesis starting material was preliminarily determined. The total impurities should not exceed 10.0%. The content of 1- (2,4) -difluorophenyl-2- Triazol-1-yl) ethanone did not pass 1.4%, 4-ethyl-5-fluoro-pyrimidine did not pass 1.4%.