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正交设计法优化新型氮唑类抗真菌化合物关键中间体的合成工艺
引用本文:吴俊琪,叶小飞,黄蕾,柴晓云,金永生,俞世冲. 正交设计法优化新型氮唑类抗真菌化合物关键中间体的合成工艺[J]. 药学实践杂志, 2016, 34(2): 171-173
作者姓名:吴俊琪  叶小飞  黄蕾  柴晓云  金永生  俞世冲
作者单位:第二军医大学药学院有机化学教研室, 上海 200433,第二军医大学卫勤系卫生统计学教研室, 上海 200433,第二军医大学药学院有机化学教研室, 上海 200433,第二军医大学药学院有机化学教研室, 上海 200433,第二军医大学药学院有机化学教研室, 上海 200433,第二军医大学药学院有机化学教研室, 上海 200433
基金项目:第二军医大学本科学员创新实践能力孵化基地项目(2015YJ-06)
摘    要:
目的 优化新型氮唑类抗真菌化合物关键中间体的合成工艺。方法 采用正交设计法,重点考察反应温度、投料比、反应时间及溶剂4个因素对收率的影响。结果 反应温度对反应收率的影响最为显著,其次是反应时间;投料比及溶剂对收率影响不明显。结论 新工艺的收率可达50%左右,反应杂质少,后处理简便。

关 键 词:正交设计  氮唑类  抗真菌  合成
收稿时间:2015-11-20
修稿时间:2015-12-30

Orthogonal design optimization in synthesis of novel triazole antifungal compounds as key intermediates
WU Junqi,YE Xiaofei,HUANG Lei,CHAI Xiaoyun,JIN Yongsheng and YU Shichong. Orthogonal design optimization in synthesis of novel triazole antifungal compounds as key intermediates[J]. The Journal of Pharmaceutical Practice, 2016, 34(2): 171-173
Authors:WU Junqi  YE Xiaofei  HUANG Lei  CHAI Xiaoyun  JIN Yongsheng  YU Shichong
Affiliation:Department of Organic Chemistry, School of Pharmacy, Second Military Medical University, Shanghai 200433, China,Department of Medical Statistics, Faculty of Health Service, Second Military Medical University, Shanghai 200433, China,Department of Organic Chemistry, School of Pharmacy, Second Military Medical University, Shanghai 200433, China,Department of Organic Chemistry, School of Pharmacy, Second Military Medical University, Shanghai 200433, China,Department of Organic Chemistry, School of Pharmacy, Second Military Medical University, Shanghai 200433, China and Department of Organic Chemistry, School of Pharmacy, Second Military Medical University, Shanghai 200433, China
Abstract:
Objective To optimize novel triazole antifungal compounds synthesis of key intermediates. Methods The orthogonal experimental design is used, emphasizing on four factors including the reaction temperature, the weight ratio of material, reaction time and solvent on the yield. Results The effect of reaction temperature on the reaction yield is the most significant, followed by reaction time; the weight ratio of material and solvent on the yield impact is not obvious. Conclusion The new technology has several advantages and yields up to about 50%, less reactive impurities, easy post processing.
Keywords:orthogonal experimental design  triazole compounds  antifungal  synthesis
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