Proces for the preparation of 4-oxytetrahydropyran-2-ones
    55.
    发明申请
    Proces for the preparation of 4-oxytetrahydropyran-2-ones 失效
    处理4-氧四氢吡喃-2-酮的方法

    公开(公告)号:US20050182263A1

    公开(公告)日:2005-08-18

    申请号:US10509611

    申请日:2003-03-17

    IPC分类号: C07B51/00 C07D309/30 C07F7/08

    CPC分类号: C07D309/30

    摘要: A process for the preparation of inhibitors of HMG-CoA reductase, such as simvastatin, from 4-silyloxytetrahydropyran-2-ones with triethylamine trihydrofluoride being used as the desilylation reagent is described. The reaction is performed in organic solvents, a mixture thereof or without solvents. It is characteristic of this reaction that no additional impurities are obtained and that it takes place without the use of additional catalysts and with low excesses of the reagent.

    摘要翻译: 描述了用作为去硅烷化试剂的四乙酸三氢氟酸4-甲硅烷氧基四氢吡喃-2-酮的HMG-CoA还原酶抑制剂如辛伐他汀的制备方法。 该反应在有机溶剂,其混合物或无溶剂中进行。 该反应的特征在于没有额外的杂质获得,并且在没有使用额外的催化剂和低过量的试剂的情况下进行。

    Process for preparing a
2-(2-amino-1,6-dihydro-6-oxo-purin-9-yl)methoxy-1,3-propanediol
derivative
    59.
    发明授权
    Process for preparing a 2-(2-amino-1,6-dihydro-6-oxo-purin-9-yl)methoxy-1,3-propanediol derivative 失效
    制备2-(2-氨基-1,6-二氢-6-氧代 - 嘌呤-9-基)甲氧基-1,3-丙二醇衍生物的方法

    公开(公告)号:US6103901A

    公开(公告)日:2000-08-15

    申请号:US121446

    申请日:1998-07-23

    CPC分类号: C07D473/18 Y02P20/55

    摘要: Intermediates of Formula (III) ##STR1## wherein P.sup.1 is hydrogen or an amino-protecting group, R is lower alkyl, allyl or aralkyl, and Z is hydrogen, lower alkyl, aryl or aralkyl; and Formula (VI) ##STR2## wherein P.sup.1 is hydrogen or an amino-protecting group, P.sup.2 is an amino protecting group, and Z is hydrogen, lower alkyl, aryl or aralkyl, are useful in a novel process for preparing the mono-L-valine ester of 2-(2-amino-1,6-dihydro-6-oxo-purin-9-yl)methoxy-1,3-propanediol (ganciclovir). The mono-L-valine ester of ganciclovir and its pharmaceutically acceptable salts are of value as antiviral agents with improved absorption.

    摘要翻译: 其中P1为氢或氨基保护基的式(III)中间体,R为低级烷基,烯丙基或芳烷基,Z为氢,低级烷基,芳基或芳烷基; 和式(VI)其中P1是氢或氨基保护基,P2是氨基保护基,Z是氢,低级烷基,芳基或芳烷基,可用于制备单-L-缬氨酸酯的新方法 的2-(2-氨基-1,6-二氢-6-氧代 - 嘌呤-9-基)甲氧基-1,3-丙二醇(更昔洛韦)。 更昔洛韦的单-L-缬氨酸酯及其药学上可接受的盐具有改善吸收的抗病毒剂的价值。