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去甲基阿奇霉素羟基选择性保护的研究
赵伯龙,张萍
0
(宁夏泰瑞制药股份有限公司)
摘要:
为解决去甲基阿奇霉素活性羟基的反应选择性问题,采用丙酮与邻苯二甲酸酐对去甲基阿奇霉素进行两次邻位保护的方法,得到4”-羟基具有反应活性的保护去甲基阿奇霉素,反应摩尔收率87.9%。本研究产物可直接用于泰拉霉素的合成,实现了对去甲基阿奇霉素的选择性保护。
关键词:  去甲基阿奇霉素  丙酮  邻苯二甲酸酐  泰拉霉素A
DOI:
投稿时间:2015-08-22修订日期:2015-09-30
基金项目:
Research of Selective protection for hydroxyl of Azithromycin
(Ningxia Tairui Pharmactlal Co.,Ltd)
Abstract:
In order to resolve the problem that the reaction selectivity of azithromycin demethylate’s hydroxyl, acetone and phthalic anhydride were used to double protection the adjacent hydroxyl of azithromycin demethylate, to obtain the protection azithromycin that only the 4"-OH had reactivity. The reaction yield was 87.9%. The product of research can be directly used for the synthesis of tulathromycin,Achieve azithromycin's protect of the hydroxyl's selectivity.
Key words:  Azithromycin  Acetone  phthalic anhydride  Tulathromycin

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