GLUT_1介导的脑靶向去甲文拉法辛前药的设计与合成
Design and synthesis of GLUT_1 mediated brain targeting prodrug of desvenlafaxine
作者：石浙秦;任云;樊维;吴勇;
Author：
收稿日期： 年卷（期）页码：2012,27(02):-118-120
期刊名称：华西药学杂志
Journal Name：WEST CHINA JOURNAL OF PHARMACEUTICAL SCIENCES
关键字：脑靶向;前药;去甲文拉法辛;葡萄糖转运蛋白1;合成
Key words：
基金项目：国家自然科学基金资助项目(批准号:81072532);;
教育部优先资助领域项目(批准号:20110181130011)
中文摘要
目的合成一种由葡萄糖转运蛋白1(GLUT1)介导的脑靶向去甲文拉法辛前药。方法将苄基保护的去甲文拉法辛与己二酸单叔丁酯在缩合剂DCC作用下成酯Ⅱ,经三氟乙酸脱除叔丁基保护后,再与1,2,3,4-四-O-三甲硅基-α-D-吡喃葡萄糖在缩合剂DCC的作用下成酯,在酸性条件下脱除三甲硅基保护,最后催化氢化脱除苄基保护得到目标化合物。结果与结论合成了目标化合物脑靶向去甲文拉法辛前药;目标化合物及重要中间体均经1HNMR和MS确证。
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