Synthesis of arachidic acid-cholic acid conjugate aramchol for treating disordered lipid metabolism / 中国药学杂志

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.