| 摘要 |
<p>A method of preparation of cholecalciferol derivatives, particularly 1α,24-dihydroxycholecalciferol of formula (1), wherein substituents R1 and R2 are hydrogen, hydroxyl, or hydroxyl protecting group, R1 and R2 being the same or different, consists in reacting phenylsulfonyl derivative of formula (2), wherein R1 and R2 denote hydrogen or hydroxyl protecting group, R1 and R2 being the same or different, with 1,2-epoxy-3-methylbutane of (S) or (R) configuration at carbon atom C-2, respectively, in the presence of an aprotic solvent and a strong organic base, and then from the resulting hydroxysulfone of (R) or (S) configuration, respectively, represented by formula (3), wherein R1 and R2 are as defined above, phenylsulfonyl group is removed by reduction to yield a compound of formula (4), from which optionally hydroxyl protecting groups are removed using the known method. The invention also provides new intermediate compounds used in the method. Cholecalciferol derivatives are active metabolites of vitamin D3.</p> |
