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具有葡萄糖转运蛋白亲和力的脑靶向文拉法辛前药的合成

Synthesis of brain-targeting prodrug of Venlafaxine with affinity to GLUT₁

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【Author】 ZHANG Yong1,WU Xue-ying2,REN Yun1,HAI Li1(1.West China School of Pharmacy,Sichuan University,Chengdu,Sichuan,610041 P.R.China;2.College of Pharmacy,Chengdu University of Traditional Chinese Medicine,Chengdu,Sichuan,610075 P.R.China)

【机构】四川大学华西药学院；成都中医药大学药学院；

【摘要】目的为了提高抗抑郁药文拉法辛的脑靶向性,以血脑屏障上的葡萄糖转运蛋白1为靶标,设计并合成了脑靶向性的文拉法辛前药Ⅰ。方法以文拉法辛为起始原料,通过丁二酸为桥链与三甲硅基保护的葡萄糖偶联,脱去保护基,得到Ⅰ。结果和结论目标化合物Ⅰ经1HNMR、IR和MS确证结构。更多还原

【Abstract】 OBJECTIVE To design and synthesize a brain-targeting prodrug of Venlafaxine with affinity to the glucose transporter 1(GLUT1).METHODS Venlafaxine,as starting material,was conjugated with 1,2,3,4-tetra-O-trimethysilyl-D-glucopyranose by succinic acid,and then deprotected to get the target compound Ⅰ.RESULTS and CONCLUSION The target compound was confirmed by 1HNMR,IR and MS.更多还原