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吡美莫司的合成和纯化工艺的研究

Studies on the Synthesis and Purification of Pimecrolimus
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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
作者 庄鸿 黄楷 乐占线 张祝兰 郑卫
机构地区 福建省微生物研究所
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)
关键词 吡美莫司 子囊霉素 一锅法合成 反相填料柱 Pimecrolimus Ascomycin One pot synthesis Reversed packing column
分类号 R914.3 [医药卫生—药物化学]
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参考文献9

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二级参考文献13

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海峡药学
2016年 第8期

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