Syntheses of oxysterol receptors(LXRs) ligands
ZHOU Xiangdong1, ZHEN Hui1 & ZHOU Weishan2 1. Department of Pharmacy, The Third Millitary Medical University,Chongqing 400038, China; 2. Shanghai Institute of Organic Chemistry, Chinese Academy of Sci-ences, Shanghai 200032, China
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.
【CateGory Index】： O641