首页> 外国专利> 1ALPHA-HYDROXY-6(1,3-BENZODITHIOL-2-YL)OXY-3,5-CYCLOVITAMIN D3

1ALPHA-HYDROXY-6(1,3-BENZODITHIOL-2-YL)OXY-3,5-CYCLOVITAMIN D3

机译:1ALPHA-HYDROXY-6(1,3-BENZODITHIOL-2-YL)OXY-3,5-CYCLOVITAMIN D3

摘要

NEW MATERIAL:1alpha-Hydroxy-6-(1,3-benzodithiol-2-yl)oxy-3,5-cyclovitamin D3 expressed by formula I. USE:Useful as a synthetic intermediate for alfacalcidol (a drug, having action of increasing calcium in blood by absorption of calcium from the outside and mobilization of calcium from bones and useful for improving symptoms accompanied by vitamin D dysbolism). The alfacalcidol, i.e., 1alpha-hydroxyvitamin D3 is synthesized by solvolyzing the compound expressed by formula I in the presence of a beteropoly-acid. PREPARATION:For example, a compound expressed by formula II is reacted with 1,3-benzodithiolium tetrafluoroborate in the presence of a base, such as pyridine, in a solvent, such as dichloromethane, while being cooled with ice to afford a novel compound expressed by formula III, which is then subjected to allylic oxidation to provide the compound expressed by formula I.
机译:新材料:由式I表示的1α-羟基-6-(1,3-苯并二硫醇-2-基)氧基-3,5-环维生素D3。用途:用作阿法骨化醇(一种具有增强作用的药物)的合成中间体通过从外界吸收钙和从骨骼中吸收钙来吸收血液中的钙,可用于改善伴随维生素D代谢不良的症状。通过在杂多酸存在下溶剂化由式I表示的化合物来合成阿法骨化醇,即1α-羟基维生素D 3。制备:例如,使式II表示的化合物与1,3-苯并二硫鎓四氟硼酸酯在碱(例如吡啶)存在下,在溶剂(例如二氯甲烷)中反应,同时用冰冷却,得到表示的新化合物式III的化合物,然后对其进行烯丙基氧化以提供式I表示的化合物。

著录项

  • 公开/公告号JPH0544947B2

    专利类型

  • 公开/公告日1993-07-07

    原文格式PDF

  • 申请/专利权人 TEIKOKU HORMONE MFG CO LTD;

    申请/专利号JP19880072813

  • 发明设计人 TAKAHASHI MINOKAZU;KONO TAKASHI;

    申请日1988-03-25

  • 分类号C07D339/06;C07C401/00;

  • 国家 JP

  • 入库时间 2022-08-22 05:20:55

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