奥贝胆酸及其有关物质的合成  

Synthesis of Obeticholic Acid and Its Related Substances

作　　者：邱玥珩 曹忠诚[1] 强晓明[1] 武梅[1] 邓勇[1] 

机构地区：[1]四川大学华西药学院药物化学系,四川成都610041

出　　处：《中国医药工业杂志》2016年第4期376-379,共4页Chinese Journal of Pharmaceuticals

摘　　要：3?-羟基-7-酮-5?-胆甾烷-24-酸经甲酯化,与乙醛缩合得到3?-羟基-6-亚乙基-7-酮-5?-胆甾烷-24-甲酯,再经氢化还原,水解,选择性还原反应制得奥贝胆酸,总收率为31.9%。并合成了工艺中可能存在的2个有关物质,6?-乙基熊去氧胆酸和6?-乙基鹅去氧胆酸。Obeticholic acid was synthesized from 3α-hydroxy-7-keto-5β-cholan-24-oic acid via methyl esterifi cation, condensation with acetaldehyde to give methyl 3α-hydroxy-6-ethylidene-7-keto-5b-cholan-24-oate, which was subjected to hydrogenation, hydrolysis and selective reduction with an overall yield of 31.9%. Two substances including 6β-ethylursodeoxycholic acid and 6？-ethylchenodeoxy-cholic acid were successfully synthesized.

关 键 词：奥贝胆酸 鹅去氧胆酸 慢性肝炎 有关物质 合成 

分 类 号：R975.5[医药卫生—药品]