Acid amide derivatives and process for the preparation thereof
    52.
    发明授权
    Acid amide derivatives and process for the preparation thereof 失效
    酸酰胺衍生物及其制备方法

    公开(公告)号:US5912245A

    公开(公告)日:1999-06-15

    申请号:US737273

    申请日:1997-02-14

    CPC分类号: C07D241/44

    摘要: The present invention is directed to an acid amide of the formula ##STR1## wherein R.sup.1 represents hydrogen or nitro,R.sup.2 and R.sup.3 stand for, independently from each other, hydrogen, lower alkyl or lower alkenyl each optionally carrying a substituent selected from the group consisting of halogen, hydroxy, lower alkoxy, di(lower alkyl)amino, phenyl-lower alkoxycarbonyl and a 5- to 6-membered saturated hetero-ring selected from the group consisting of piperidino, pyrrolidino, piperazino and morpholino; orR.sup.2 and R.sup.3 form, together with the adjacent nitrogen atom, a 6-membered saturated heterocyclic group selected from the group consisting of piperidino, pyrrolidino, piperazino and morpholino, said heterocyclic group optionally carrying a hydroxy or a hydroxy-lower alkyl group; or apharmaceutically acceptable salt thereof; process of making and pharmaceutical compositions and methods of treating.

    摘要翻译: PCT No.PCT / HU95 / 00015 Sec。 371日期1997年2月14日 102(e)日期1997年2月14日PCT提交1995年5月15日PCT公布。 公开号WO95 / 31443 日期:1995年11月23日本发明涉及下式的酰胺,其中R 1表示氢或硝基,R 2和R 3彼此独立地表示氢,低级烷基或低级烯基,各自任选地带有选自 由卤素,羟基,低级烷氧基,二(低级烷基)氨基,苯基 - 低级烷氧基羰基和选自哌啶子基,吡咯烷子基,哌嗪基和吗啉代的5-至6-元饱和杂环组成的基团。 或R 2和R 3与相邻的氮原子一起形成选自哌啶子基,吡咯烷子基,哌嗪子基和吗啉代的6元饱和杂环基,所述杂环基任选地带有羟基或羟基 - 低级烷基; 或其药学上可接受的盐; 制备方法和药物组合物和治疗方法。

    Process for the preparation of aminolactone carboxylic acid
    54.
    发明授权
    Process for the preparation of aminolactone carboxylic acid 失效
    制备氨基内酯羧酸的方法

    公开(公告)号:US4559406A

    公开(公告)日:1985-12-17

    申请号:US508436

    申请日:1983-06-27

    摘要: The invention relates to a process for the preparation of the compound of the formula I, ##STR1## which comprises (a.sub.1) splitting off the ethylene ketal protecting group from the azetidinone derivative of the formula IVa, ##STR2## reducing the compound of the formula III thus obtained, ##STR3## treating the resulting compound of the formula II ##STR4## with concentrated aqueous hydrogen chloride solution; or (a.sub.2) reducing the compound of the formula III, treating the compound of the formula II thus obtained with concentrated aqueous hydrogen chloride solution; or (a.sub.3) treating the compound of the formula II with concentrated aqueous hydrogen chloride solution; and isolating the compound of the formula I thus obtained from the reaction mixture. The compound of the formula I is useful as an intermediate in the production of thienamycin, a highly potent antibiotic.

    摘要翻译: 本发明涉及一种制备式I化合物的方法,其包括(a1)将亚乙基缩酮保护基从式IVa的氮杂环丁酮衍生物中分离出来, 由此获得的式III,使用浓缩的氯化氢水溶液处理所得式II的化合物; 或(a2)还原式III的化合物,用浓缩的氯化氢水溶液处理由此获得的式II化合物; 或(a3)用浓缩的氯化氢水溶液处理式II的化合物; 并从反应混合物中分离得到的式I化合物。 式I的化合物可用作生产高效抗生素的噻吩霉素的中间体。

    Pharmaceutical intermediate for synthesizing ACE inhibitors and the use thereof
    59.
    发明授权
    Pharmaceutical intermediate for synthesizing ACE inhibitors and the use thereof 有权
    用于合成ACE抑制剂的药物中间体及其用途

    公开(公告)号:US07960558B2

    公开(公告)日:2011-06-14

    申请号:US12300545

    申请日:2007-05-11

    摘要: The compounds of the general Formula (I), wherein R1 is aryl or alkyl; R2 represents alkyl; R3 represents alkyl or aralkyl, are valuable pharmaceutical intermediates, which can be prepared by reacting a compound of the general Formula (IV) (wherein the definitions of R1 and R2 are as above), with at least 2 molar equivalents of the compound of the general Formula (VI) (wherein X represents halogen or tertiary butyloxycarbonyloxy group and R3 is as defined above). The known compounds of the general Formula (II) (wherein R1 and R2 are as defined above) are prepared by reacting the compounds of the general Formula (I) with thionyl chloride. The compounds of the general Formula (I) are new intermediates useful in the synthesis of pharmaceutically active ingredients, particularly in the preparation of ACE-inhibitors, e.g. enalapril, perindopril or ramipril.

    摘要翻译: 通式(I)的化合物,其中R 1是芳基或烷基; R2代表烷基; R3表示烷基或芳烷基,是有价值的药物中间体,其可以通过使通式(IV)化合物(其中R 1和R 2的定义如上所述)与至少2摩尔当量的 通式(VI)(其中X表示卤素或叔丁氧羰基氧基,R3如上定义)。 通式(II)的已知化合物(其中R1和R2如上定义)通过使通式(I)的化合物与亚硫酰氯反应来制备。 通式(I)的化合物是可用于合成药物活性成分的新中间体,特别是在制备ACE抑制剂中。 依那普利,培哚普利或雷米普利。