利奈唑胺合成方法的改进
An improved synthesis of Linezolid
作者：白平;桑志培;何洪光;邓勇;
Author：
收稿日期： 年卷（期）页码：2015,30(01):-7-9
期刊名称：华西药学杂志
Journal Name：WEST CHINA JOURNAL OF PHARMACEUTICAL SCIENCES
关键字：噁唑烷酮类抗菌药;利奈唑胺;3-氟-4-吗啉基苯胺;(R)-环氧氯丙烷;合成
Key words：
基金项目：
中文摘要
目的改进新型抗菌药利奈唑胺的合成方法。方法以3-氟-4-吗啉基苯胺为起始原料,在三氟甲磺酸锂催化下与(R)-环氧氯丙烷缩合,经氯甲酸甲酯酰化、氨解得(S)-3-(3-氟-4-吗啉苯基)-5-氨甲基-1,3-噁唑烷-2-酮,再经醋酐乙酰化得利奈唑胺。结果利奈唑胺的化学结构经1HNMR、ESI-MS确证,总收率为63%。结论所用方法具有反应步骤少、原料易得、条件温和、操作简便、收率高等优点。
参考文献
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