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    • 2. 发明申请
    • PROCESS FOR PRODUCTION OF 1-HYDROXY-19-NORCYCLOVITAMIN D DERIVATIVE AND INTERMEDIATE FOR THE PRODUCTION
    • 生产1-羟基-19-硝基维生素D衍生物和生产中间体的方法
    • US20110319644A1
    • 2011-12-29
    • US12312209
    • 2007-11-01
    • Asako ToyodaHazuki NagaiKaname KonukiToshio Tsuchida
    • Asako ToyodaHazuki NagaiKaname KonukiToshio Tsuchida
    • C07C401/00
    • 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-hydrocyclovitamin D derivative is subjected to solvolysis, thereby producing a 1-hydroxy-19-norviatmin D derivative. Thus provided are a novel process for production of 1-hydroxy-19-norcyclovitamin D derivative that is utilizable as an intermediate in the synthesis of 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。 1-环氢维生素D衍生物进行溶剂解,由此生成1-羟基-19-诺维那敏D衍生物。 因此提供了可用作合成作为药剂的1-羟基-19-去甲维生素D衍生物的合成中间体的1-羟基-19-去甲柔比星D衍生物的新方法。 和生产中间体。