吡美莫司的合成和纯化工艺的研究  

Studies on the Synthesis and Purification of Pimecrolimus

作　　者：庄鸿[1] 黄楷[1] 乐占线[1] 张祝兰[1] 郑卫[1] 

机构地区：[1]福建省微生物研究所,福建省新药(微生物)筛选重点实验室,福州350007

出　　处：《海峡药学》2016年第8期256-258,共3页Strait Pharmaceutical Journal

基　　金：福州市科技计划项目(编号:2014-G-56);福建省科技计划项目(编号:2015R1009-3);福建省化药技术重大研发平台(2014Y2001)

摘　　要：目的优化免疫抑制类药物吡美莫司的合成和纯化工艺。方法以子囊霉素为原料通过选择性的羟基酯化-氯化反应一锅法合成路线,再经过反相填料柱纯化后得到目标产物。结果目标产物经过红外光谱、核磁共振氢谱和质谱确认化学结构,总收率为50%,纯度为99%。结论经过该合成和纯化工艺,产品纯度高,且易于实现工业化。OBJECTIVE To optimize the synthesis and purification process pressant drug. METHODS Pimecrolimus was synthesized by using ascomycin as tively esterification and chlorination in one-pot way, and then was purified of pimecrolimus, an immunosupa starting material through selecthrough reversed packing col- umn. RESULTS Pimecrolimus was characterized by IR,1HNMR and MS. The total yield was 50% and the purity was 99%. CONCLUSION The suitable synthesis and purification process of pimecrolimus with high purity and amendable to industrialization was provided. KF：：Y WORDS ： Pimecrolimus ; Ascomyein; One pot synthesis ; Reversed packing column

关 键 词：吡美莫司 子囊霉素 一锅法合成 反相填料柱 

分 类 号：R914.3[医药卫生—药物化学]