新型LXRs配体——环氧胆烷酸甲酯一类物的化学合成  

Chemical synthesis of methyl epoxycholanate analogues: novel ligands for liver X receptors

作　　者：郑辉[1] 徐长荣[1] 周向东[1] 

机构地区：[1]第三军医大学基础医学部化学教研室,重庆400038

出　　处：《第三军医大学学报》2001年第9期1091-1093,共3页Journal of Third Military Medical University

基　　金：中国科学院生命有机化学国家重点实验室基金资助项目 (2 0 0 0 - 0 8);中国科学院上海有机化学研究所生命有机化学国家重点实验室基金资助

摘　　要：目的　合成两个新设计的具有环氧胆烷酸甲酯结构的化合物 :3β 羟基 5α ,6α 环氧胆烷酸甲酯、3β 羟基 5 β ,6 β 环氧胆烷酸甲酯 ,以期从中发现新的LXRs亚型选择性配体。方法　用我国丰富的甾体资源———猪去氧胆酸为原料 ,分别经三步和四步化学反应合成。结果　以 76 %和 42 %的总收率合成了两个目标化合物 ,并经波谱分析证实。结论　用高立体选择性高收率地成功合成了目标化合物。为研制治疗动脉粥样硬化等心脑血管疾病的新药打下了基础。s: Objective To synthesize two compounds with epoxycholanate structure: methyl 3β hydroxy 5β, 6β epoxycholanate and methyl 3β hydroxy 5β, 6β epoxycholanate for getting new ligands of liver X receptors (LXRs). Methods The compounds were synthesized from hyodeoxycholic acid in 3 and 4 steps and analyzed with spectroscopy. Results The compounds were synthesized in total yields of 76% and 43%, respectively, and confirmted with spectroscopy. Conclusion The compounds are synthesized with epoxycholanate structure stereocontrolledly and successfully, which founds a basis for new drug synthesis in the treatment of cardiovascular diseases, like atherosclerosis etc.

关 键 词：LXRs配体 猪去氧胆酸 3β-羟基-5α 6α-环氧胆酸甲酯 3β-羟基-5β 6β-环氧胆酸甲酯 合成 环氧胆烷酸甲酯类 

分 类 号：TQ463.3[化学工程—制药化工]