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。
Abstract
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-cholanic-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 regioselectively deprotected. 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
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Key words
treating disordered lipid metabolism /
fatty acid bile acid conjugate /
aramchol /
synthesis
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中图分类号：
R914.5
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参考文献
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