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    • 1. 发明公开
    • 1-히드록시-19-노르시클로비타민 D 유도체의 제조방법 및 그 제조 중간체
    • 生产1-羟基-19-硝基维生素D衍生物和生产中间体的方法
    • KR1020090082257A
    • 2009-07-29
    • KR1020097010739
    • 2007-11-01
    • 메루샹가부시키가이샤
    • 토요다,아사코나가이,하즈키코누키,카나메츠키다,토시오
    • C07C401/00A61K31/59
    • C07C401/00
    • A cyclovitamin D derivative produced from 25-hydroxyvitamin D is reacted with osmium tetraoxide or a permanganic acid salt to produce a 10,19-diolcyclovitamin D derivative. The 10,19-diolcyclovitamin D derivative is reacted with a perhalogenic acid salt or lead tetraacetate to produce a 10-oxocyclovitamin D derivative. A 1-hydroxycyclovitamin D derivative is produced from the 10-oxocyclovitamin D derivative via a cyclovitamin D derivative and a 1,10-olefincyclovitamin D derivative. The 1-hydroxycyclovitamin D derivative is subjected to solvolysis, thereby producing a 1-hydroxy-19-norvitamin D derivative. Thus, provided are: a novel process for producing a 1-hydroxy-19-norvitamin D derivative which can be used as an intermediate for the synthesis of a 1-hydroxy-19-norvitamin D derivative which is useful as a pharmaceutical agent; and an intermediate for the production.
    • 由25-羟基维生素D产生的环维生素D衍生物与四氧化锇或高锰酸盐反应,生成10,19-二醇环化维生素D衍生物。 使10,19-二醇类环维生素D衍生物与全卤酸盐或四乙酸铅反应生成10-氧代环维生素D衍生物。 通过环维生素D衍生物和1,10-烯柔性维生素D衍生物从10-氧代环维生素D衍生物产生1-羟基环维生素D衍生物。 将1-羟基环维生素D衍生物进行溶剂解,由此生成1-羟基-19-去甲维生素D衍生物。 因此,提供了可用作合成可用作药剂的1-羟基-19-诺维生素D衍生物的中间体的1-羟基-19-诺维生素D衍生物的新方法。 和生产中间体。