Process for the preparation of (4-hydroxy-6-oxo-tetrahydropyran-2-yl) acetonitrile and derivatives
    6.
    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。

    Process For Esterification Of An Organic Acid
    10.
    发明申请
    Process For Esterification Of An Organic Acid 审中-公开
    有机酸酯化方法

    公开(公告)号:US20080249329A1

    公开(公告)日:2008-10-09

    申请号:US12088159

    申请日:2006-09-26

    IPC分类号: C07C229/52

    摘要: The invention relates to a sulphonic acid salt of an amino acid alkyl ester The invention further relates to a process for the esterification of an organic acid into the corresponding organic acid ester comprising bringing the organic acid into contact with a strong acid and a solution comprising dialkylcarbonate in a reaction mixture. The invention further relates to the use of a sulphonic acid salt of an amino acid alkyl ester in the synthesis of a β-lactam antibiotic.

    摘要翻译: 本发明涉及氨基酸烷基酯的磺酸盐本发明还涉及将有机酸酯化成相应的有机酸酯的方法,包括使有机酸与强酸和包含二烷基碳酸酯的溶液接触 在反应混合物中。 本发明还涉及氨基酸烷基酯的磺酸盐在β-内酰胺抗生素的合成中的用途。