Abstract
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 desmosterol acetate 11 as the key intermediate and the modified Sharpless asymmetric dihydroxylation as the key step. The LXRα subtype selective agonist 5α,6α:24S,25-diepoxycholesterol 2 and the novel LXRs’ ligand 5β,6β:24S,25-diepoxycholesterol 3 were also synthesized from 1.
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