Syntheses of oxysterol receptors'(LXRs) ligands

作     者：ZHOU Xiangdong ZHEN Hui ZHOU Weishan 

作者机构：Department of PharnmcyThe Third Millitary Medical UniversityChongqing 400038China Shanghai Institute of Organic ChemistryChinese Academy of SciellcesShanghai 200032China 

出 版 物：《Chinese Science Bulletin》 (CHINESE SCIENCE BULLETIN)

年 卷 期：2003年第48卷第3期

页      面：247-254页

核心收录：

学科分类：1007[医学-药学(可授医学、理学学位)] 100701[医学-药物化学] 10[医学] 

基　　金：supported by the National Natural Science Foundation of China(Grant No.20072047) the State Key Laboratory of Biological Organic Chemistry in Shanghai Institute of Organic Chemistry,Chongqing Science and Technology Committee(Grant No.6617) the Third Military Medical University 

主　　题：methyl hyodeoxycholanate desmosterol acetate 24S 25-epoxycholesterol sharpless catalytic asymmetric dihydoxylation LXRs'agonists. 

摘      要：The LXRs?agonist, 24S,25-epoxycholesterol 1,was synthesized stereoselectively (100% d.e.) in 56% overall yield from methyl hyodeoxycholanate 4 in 9 steps with des-mosterol acetate 11 as the key intermediate and the modified Sharpless asymmetric dihydroxylation as the key step. TheLXRa subtype selective agonist 5a,6a:24S,25-diepoxycho-lesterol 2 and the novel LXRs?ligand 5b,6b:24S,25-diepo-xycholesterol 3 were also synthesized from 1.