Process for the preparation of (4-hydroxy-6-oxo-tetrahydropyran-2-yl) acetonitrile and derivatives
    5.
    发明授权
    Process for the preparation of (4-hydroxy-6-oxo-tetrahydropyran-2-yl) acetonitrile and derivatives 有权
    (4-羟基-6-氧代 - 四氢吡喃-2-基)乙腈及其衍生物的制备方法

    公开(公告)号:US07423162B2

    公开(公告)日:2008-09-09

    申请号:US10554294

    申请日:2004-04-28

    IPC分类号: C07D309/30

    CPC分类号: C07D309/30

    摘要: The invention relates to a process for the preparation of (4-hydroxy-6-oxo-tetrahydro-pyran-2-yl)-acetonitrile from 6-X-substituted-methyl-4-hydroxy-tetrahydro-pyran-2-one, wherein X stands for a leaving group, by reacting 6-X-substituted-methyl-4-hydroxy-tetrahydro-pyran-2-one with a cyanide ion in water and by subsequent lowering of the pH to a pH between 0 and 5. (4-hydroxy-6-oxo-tetrahydro-pyran-2-yl)-acetonitrile and other compounds obtainable from (4-hydroxy-6-oxo-tetrahydro-pyran-2-yl)-acetonitrile may suitably be used in the preparation of a pharmaceutical preparation, more in particular in the preparation of statins, more in particular in the preparation of Atorvastatine or a salt thereof, for instance its calcium salt. The invention also relates to (4-hydroxy-6-oxo-tetrahydro-pyran-2-yl)-acetonitrile and other compounds obtainable therefrom.

    摘要翻译: 本发明涉及从6-X取代的甲基-4-羟基 - 四氢 - 吡喃-2-酮制备(4-羟基-6-氧代 - 四氢 - 吡喃-2-基) - 乙腈的方法, 其中X代表离去基团,通过使6-X取代的甲基-4-羟基 - 四氢 - 吡喃-2-酮与氰化物离子在水中反应,随后将pH降低至0至5之间的pH。 (4-羟基-6-氧代 - 四氢 - 吡喃-2-基) - 乙腈和从(4-羟基-6-氧代 - 四氢 - 吡喃-2-基) - 乙腈获得的其它化合物可适当地用于制备 药物制剂,更特别是制备他汀类药物,更特别是制备阿托伐他汀或其盐,例如其钙盐。 本发明还涉及(4-羟基-6-氧代 - 四氢 - 吡喃-2-基) - 乙腈及其可得的其它化合物。