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    • 34. 发明授权
    • 1.alpha.-hydroxy vitamin D.sub.4 and novel intermediates and analogues
    • 1α-羟基维生素D4和新型中间体和类似物
    • US5488120A
    • 1996-01-30
    • US296084
    • 1994-08-24
    • Joyce C. KnutsonCharles W. BishopRobert M. Moriarty
    • Joyce C. KnutsonCharles W. BishopRobert M. Moriarty
    • A61K31/59C07C35/21C07C401/00
    • A61K31/592C07C35/21C07C401/00
    • Novel 1.alpha.-hydroxy Vitamin D.sub.4 and novel analogues, 1,25 dihydroxy Vitamin D.sub.4 and 1,24 dihydroxy Vitamin D.sub.4 which are useful for the treatment of disorders of calcium metabolism. Preparation of the novel 1.alpha.-hydroxy Vitamin D.sub.4 starts from ergosterol which is converted in six steps to 22,23-dihydroergosterol. 22,23-dihydroergosterol was irradiated to yield Vitamin D.sub.4 which was converted in four steps to 1.alpha.-hydroxy Vitamin D.sub.4 using a cyclovitamin procedure which produced the novel intermediates, Vitamin D.sub.4 tosylate, 3,5 cyclovitamin D.sub.4 and 1.alpha.-hydroxy cyclovitamin D.sub.4. 1,25 dihydroxy Vitamin D.sub.4 and 1,24 dihydroxy Vitamin D.sub.4 are isolated as biological products of the metabolism of novel 1.alpha.-hydroxy Vitamin D.sub.4 using cultured human liver cells.
    • 新型1α-羟基维生素D4和新型类似物,1,25二羟基维生素D4和1,24二羟基维生素D4,其可用于治疗钙代谢紊乱。 新型1α-羟基维生素D4的制备从麦角甾醇开始,其以六步转化为22,23-二氢麦角甾醇。 22,23-二氢麦角甾醇被照射以产生维生素D4,其使用产生新的中间体维生素D4甲苯磺酸盐,3,5环维生素D4和1α-羟基环维生素D4的环维生素程序将其四步转化为1α-羟基维生素D4 。 使用培养的人肝细胞,分离出1,25二羟基维生素D4和1,24二羟基维生素D4作为新型1α-羟基维生素D4代谢的生物学产物。