Heterocyclic compounds containing an alkoxycarbonyl and a substituted
methyl group
    2.
    发明授权
    Heterocyclic compounds containing an alkoxycarbonyl and a substituted methyl group 失效
    含有烷氧羰基和取代甲基的杂环化合物

    公开(公告)号:US4435322A

    公开(公告)日:1984-03-06

    申请号:US301191

    申请日:1981-09-11

    IPC分类号: C07D205/08 C07D487/04

    CPC分类号: C07D205/08

    摘要: The invention relates to new heterocyclic compound containing an alkoxycarbonyl and a substituted methyl group a process for the preparation of these and analogeous compound and pharmaceutical compositions containing them.More particularly, the invention concerns compounds of the general formula (IVa) ##STR1## wherein R' is hydrogen, 2-ethoxycarbonylethyl, aryl or a group suitable for a temporary protection of amides andY' represents a group of the formula --COOZ or --CH.sub.2 M, in whichZ is lower alkyl andM is hydroxyl, halogen, cyano or a group of the formula --O--SO.sub.2 R.sup.2, in whichR.sup.2 is lower alkyl or aryl,with the proviso that if R' is phenyl, Y' cannot stand for the group --COOC.sub.2 H.sub.5.The invention further relates to a process for the preparation of compounds of the general formula (IV) ##STR2## in which R and Y are identical with R' and Y', respectively, except the proviso.According to a further aspect of the invention there are provided pharmaceutical compositions, first of all with antihypoxic activity, comprising compounds of the general formula (IVa) as active ingredient.

    摘要翻译: 本发明涉及含有烷氧基羰基和取代的甲基的新的杂环化合物,其制备这些和分解化合物的方法和含有它们的药物组合物。 更具体地说,本发明涉及通式(IVa)(IVa)的化合物,其中R'是氢,2-乙氧基羰基乙基,芳基或适于临时保护酰胺的基团,Y'代表式 -COOZ或-CH2M,其中Z是低级烷基,M是羟基,卤素,氰基或式-O-SO2R2的基团,其中R2是低级烷基或芳基,条件是如果R'是苯基, Y'不能代表组-COOC2H5。 本发明还涉及制备通式(IV)的化合物(IV)的方法,其中R和Y分别与R'和Y'相同,但条件是。 根据本发明的另一方面,提供首先具有抗缺氧活性的药物组合物,其包含通式(IVa)的化合物作为活性成分。

    Process for the preparation of aminolactone carboxylic acid
    6.
    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。

    Azetidinone acetic acid derivatives and process for the preparation
thereof
    7.
    发明授权
    Azetidinone acetic acid derivatives and process for the preparation thereof 失效
    氮杂环丁酮乙酸衍生物及其制备方法

    公开(公告)号:US4587049A

    公开(公告)日:1986-05-06

    申请号:US549681

    申请日:1983-11-07

    IPC分类号: C07D205/08

    CPC分类号: C07D205/08

    摘要: The invention relates to compounds of the general formula (X) ##STR1## wherein R is as a removable protecting substituent of the amido group a phenyl group or a benzyl group substituted by one or more alkoxy group(s) having 1-4 carbon atoms andR.sup.1 stands for a hydrogen atom or an alkyl group having 1-4 carbon atoms and a process for the preparation thereof.The compounds of the general formula (X) can be prepared from the starting materials of the general formula (V), wherein R and R.sup.1 are as stated above and Z is an alkyl group having 1-4 carbon atoms.The compounds of the general formula (X) are useful pharmaceutical intermediates which can be used in the preparation of known antibiotics (e.g. Thienamycin and PS-5).

    摘要翻译: 本发明涉及通式(X)的化合物(X)其中R为酰氨基的可除去保护取代基,苯基或被一个或多个具有1-羟基的烷氧基取代的苄基, 4个碳原子,R1代表氢原子或具有1-4个碳原子的烷基及其制备方法。 通式(X)的化合物可以由通式(V)的起始原料制备,其中R和R 1如上所述,Z是具有1-4个碳原子的烷基。 通式(X)的化合物是可用于制备已知抗生素(例如硫霉素和PS-5)的有用的药物中间体。

    2-(substituted imino)-thiazolidines and process for the preparation
thereof
    8.
    发明授权
    2-(substituted imino)-thiazolidines and process for the preparation thereof 失效
    2-(取代的亚氨基) - 噻唑啉及其制备方法

    公开(公告)号:US5240918A

    公开(公告)日:1993-08-31

    申请号:US857067

    申请日:1992-03-24

    IPC分类号: C07D277/18

    CPC分类号: C07D277/18

    摘要: The invention relates to new 2-(substituted imino)-thiazolidines, a process for the preparation thereof, pharmaceutical compositions comprising the same, the use of the said 2-(substituted imino)thiazolidines for the treatment of diseases and for the preparation of pharmaceutical compositions suitable for the treatment of diseases.The new 2-(substituted imino)-thiazolidine derivatives provided by the present invention correspond to the general formula (I), ##STR1## wherein R.sup.1 and R.sup.2 each represent halogen, nitro, C.sub.1-4 alkoxy or C.sub.1-4 alkyl, which latter may optionally carry one or more halogen substituent(s),R.sup.3 and R.sup.4 each represent hydrogen or C.sub.1-4 alkyl,Z denotes oxygen, sulfur or imino, which latter is substituted by a C.sub.1-6 alkyl or a C.sub.1-6 alkenyl group,R.sup.5 stands for hydrogen, C.sub.1-4 alkyl, C.sub.1-4 alkylthio or a group or the formula --NH--R, wherein R represents C.sub.1-6 alkyl, aryl, aralkyl or C.sub.1-6 alkenyl optionally carrying a halogen or a di-(C.sub.1-4 alkyl)-amino substituent; orZ and R.sup.5 together stand for a trivalent nitrogen atom, with the proviso that if Z denotes a substituted imino group, R.sup.5 stands for C.sub.1-4 alkylthio, and if R.sup.5 is C.sub.1-4 alkylthio, Z represents a substituted imino, and with the further proviso that if Z denotes sulfur, R.sup.5 is other than hydrogen or C.sub.1-4 alkyl,and possess valuable antianginal and analgesic properties.

    摘要翻译: 本发明涉及新的2-(取代的亚氨基) - 噻唑烷,其制备方法,包含该方法的药物组合物,所述2-(取代的亚氨基)噻唑烷用于治疗疾病和用于制备药物 适用于治疗疾病的组合物。 本发明提供的新的2-(取代亚氨基) - 噻唑烷衍生物对应于通式(I),其中R 1和R 2各自表示卤素,硝基,C 1-4烷氧基或C 1-4烷基 ,其可以任选地带有一个或多个卤素取代基,R 3和R 4各自表示氢或C 1-4烷基,Z表示氧,硫或亚氨基,后者被C 1-6烷基或C 1-6 烯基,R5代表氢,C1-4烷基,C1-4烷硫基或基团-NH-R,其中R表示C1-6烷基,芳基,芳烷基或任选携带卤素或 二(C 1-4烷基) - 氨基取代基; 或Z和R5一起代表三价氮原子,条件是如果Z表示取代的亚氨基,则R5表示C1-4烷硫基,如果R5是C1-4烷硫基,则Z表示取代的亚氨基,并且与 进一步的条件是,如果Z表示硫,R5不是氢或C1-4烷基,并且具有有价值的抗心绞痛和止痛特性。