脂代谢调节药物花生酸-胆酸偶合物Aramchol的合成  

Synthesis of Arachidic Acid-Cholic Acid Conjugate Aramchol for Treating Disordered Lipid Metabolism

作　　者：蓝竹[1] 樊士勇[1] 史卫国[1] 仲伯华[1] 

机构地区：[1]军事医学科学院毒物药物研究所,北京100850

出　　处：《中国药学杂志》2013年第11期920-924,共5页Chinese Pharmaceutical Journal

摘　　要：目的改进aramchol的制备工艺,合成aramchol原料药。方法以花生酸(正二十烷酸)和胆酸为起始原料,采用选择性正交保护-去保护基的策略,通过9步反应合成了肝靶向脂肪酸-胆汁酸偶合物aramchol(3β-花生酰氨基-7α,12α-二-羟基-5β-胆甾烷-24-酸)。结果目标产物产率为12.7%。结论改进后的制备工艺反应重现性好,副反应少,操作较安全,适用于实验室小规模制备。OBJECTIVE To optimize the process of synthesizing aramchol. METHODS Using arachidic acid （eicosanoic acid ） and cholic acid as the starting materials, 3β-arachidyl-amido-7α, 12α-dihydroxyl-5β-cholanie-24-acid, a fatty acid bile acid conjugate aramchol, was synthesized through a 9 step route in which the carboxyl group and hydroxyl groups of cholic acid has been orthogonally protected and regioseleetivcly deproteeted. RESULTS The yield of the target product was 12.7%. CONCLUSION With reproducibile reactions, less by-products, and mild, controllable and relatively safe conditions, the improved process is very suitable for lab-scale production.

关 键 词：脂代谢调节 脂肪酸-胆汁酸偶合物 aramchol 合成 

分 类 号：R914.5[医药卫生—药物化学]