Synthesis method of E/Z type erythromycin A oxime with two configurations

The invention provides a synthesis method of E-type and Z-type two-configuration erythromycin A oxime. According to the invention, hydroxylamine hydrochloride is used as a raw material, after solid alkali neutralization, weak acid is used as a catalyst to react with erythromycin A or erythromycin A...

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Bibliographische Detailangaben
Hauptverfasser: XU XIN, ZHANG MEITANG, ZHANG FENGZHI, CHEN SHANREN, DU JIALIANG, YANG XIUDONG, LI CHONGFU
Format: Patent
Sprache:chi ; eng
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Zusammenfassung:The invention provides a synthesis method of E-type and Z-type two-configuration erythromycin A oxime. According to the invention, hydroxylamine hydrochloride is used as a raw material, after solid alkali neutralization, weak acid is used as a catalyst to react with erythromycin A or erythromycin A thiocyanate to synthesize E-type erythromycin A oxime, the process is simple, and the product yield is high. The invention also provides two methods for synthesizing Z-type erythromycin A oxime, wherein the two methods comprise a two-step method and a one-pot method; particularly, the one-pot method reduces unnecessary operation, improves efficiency, reduces three wastes, improves the total yield, and is of great significance to industrial production. 本发明提供了E式和Z式两构型红霉素A肟的合成方法。本发明以盐酸羟胺为原料、固体碱中和后、以弱酸为催化剂与红霉素A或红霉素A硫氰酸盐反应合成E式红霉素A肟,其工艺简捷,产品收率高。本发明还提供了合成Z式红霉素A肟的两种方法,包括两步法和"一锅法";特别地,"一锅法"减少了非必要操作,提高了效率、减少了三废、总收率提高,对实现工业生产有重要意义。