| GLUT1介导的脑靶向去甲文拉法辛前药的设计与合成 |
| |
| 引用本文： | 石浙秦,任云,樊维,吴勇.GLUT1介导的脑靶向去甲文拉法辛前药的设计与合成[J].华西药学杂志,2012,27(2):118-120. |
| |
| 作者姓名： | 石浙秦 任云 樊维 吴勇 |
| |
| 作者单位： | 四川大学华西药学院,四川成都,610041 |
| |
| 基金项目： | 国家自然科学基金资助项目，教育部优先资助领域项目 |
| |
| 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。
|
| 关 键 词： | 脑靶向 前药 去甲文拉法辛 葡萄糖转运蛋白1 合成 |
Design and synthesis of GLUT1 mediated brain targeting prodrug of desvenlafaxine |
| |
| SHI Zhe-qin
,
REN Yun
,
FAN Wei
,
WU Yong.Design and synthesis of GLUT1 mediated brain targeting prodrug of desvenlafaxine[J].West China Journal of Pharmaceutical Sciences,2012,27(2):118-120. |
| |
| Authors: | SHI Zhe-qin REN Yun FAN Wei WU Yong |
| |
| Institution: | *(West China School of Pharmacy,Sichuan University,Chendu,Sichuan,610041 P.R.China) |
| |
| Abstract: | OBJECTIVE To synthesize a brain targeting prodrug of desvenlafaxine mediated by glucose transporter 1(GLUT1).METHODS Desvenlafaxine protected by benzyl group was coupled with mono t-butyl adipic acid to afford compound Ⅱ,which was deprotected by trifluoroacetic acid to afford acid Ⅲ.Then compound Ⅲ was coupled with 1,2,3,4-tetra-O-trimethylsilyl-α-D-glucopyranose in the presence of DCC and DMAP to get compound Ⅳ,which was deprotected by acid to obtain compound Ⅴ.Deprotection of compound Ⅴ by H2/Pd furnished the target compound Ⅵ.RESULTS and CONCLUSION The target compound was successfully synthesized.The chemical structure of the target compound and intermediates were characterized by 1HNMR and MS. |
| |
| Keywords: | Brain targeting Prodrug Desvenlafaxine GLUT1 Synthesis |
| 本文献已被 CNKI 万方数据 等数据库收录！ |
|
