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

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。...

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Bibliographic Details
Published in药学实践杂志 Vol. 34; no. 2; pp. 171 - 173
Main Author 吴俊琪 叶小飞 黄蕾 柴晓云 金永生 俞世冲
Format Journal Article
LanguageChinese
Published 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 2016
Subjects
合成
抗真菌
正交设计
氮唑类
synthesis
antifungal
合成
orthogonal experimental design
抗真菌
氮唑类
triazole compounds
正交设计
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ISSN1006-0111
DOI10.3969/j.issn.1006-0111.2016.02.018

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Summary: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。
Bibliography:31-1685/R
WU Junqi;YE Xiaofei;HUANG Lei;CHAI Xiaoyun;JIN Yongsheng;YU Shichong;Department of Organic Chemistry,School of Pharmacy,Second Military Medical University;Department of Medical Statistics,Faculty of Health Service,Second Military Medical University; Shanghai 200433, China
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.
orthogonal experimental design; triazole compounds; antifungal; synthesis
ISSN:1006-0111
DOI:10.3969/j.issn.1006-0111.2016.02.018