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    • 1. 发明授权
    • Baron chelates of quinoline carboxylic acids
    • 喹啉羧酸的巴伦酸
    • US5091530A
    • 1992-02-25
    • US290105
    • 1988-11-23
    • Istvan HermeczGeza KereszturiLelle VasvariAgnes HorvathMarie BaloghPeter RitliJudit SiposAniko PajorKatalin Marmarosi
    • Istvan HermeczGeza KereszturiLelle VasvariAgnes HorvathMarie BaloghPeter RitliJudit SiposAniko PajorKatalin Marmarosi
    • C07D401/04A61K31/4709A61K31/495A61P31/04C07D215/56C07F5/02
    • C07D215/56
    • The invention relates to a new process for the preparation of compounds of the general Formula I ##STR1## /wherein R stands for piperazinyl, 4-methyl-piperazinyl or 4-ethyl-piperazinyl group/ and pharmaceutically acceptable salts thereof which comprises reacting a compound of the general Formula II ##STR2## /wherein R.sup.1 and R.sup.2 stand for halogen, for an aliphatic acyloxy group containing 2 to 6 carbon atoms and optionally substituted by halogen, or for an aromatic acyloxy group containing 7 to 11 carbon atoms/ with a piperazine derivative of the general Formula ##STR3## /wherein R.sup.3 stands for hydrogen, methyl or ethyl/ or a salt thereof and subjecting the compound of the general Formula IV ##STR4## thus obtained /wherein R, R.sup.1 and R.sup.2 are as stated above/ to hydrolysis after or without isolation and if desired converting the compound of the general Formula I thus obtained into a salt thereof or setting free the same from its salt.The compounds of the general Formula I are known antibacterial agents.The advantage of the present invention is that it makes the desired compounds of the general Formula I available in a simple manner, with high yields and in a short reaction time.
    • PCT No.PCT / HU88 / 00019 Sec。 371日期1988年11月23日第 102(e)日期1988年11月23日PCT提交1988年4月8日PCT公布。 公开号WO88 / 07993 1988年10月20日的日期。本发明涉及制备通式I化合物的新方法,其中R代表哌嗪基,4-甲基 - 哌嗪基或4-乙基 - 哌嗪基/ 或其药学上可接受的盐,其包括使通式II的化合物其中R 1和R 2表示卤素,含有2至6个碳原子的脂族酰氧基并且任选被卤素取代,或 含有7〜11个碳原子的芳香族酰氧基/通式为其中R 3代表氢,甲基或乙基/或其盐,并通式IV的化合物 / IV /由此获得的/其中R,R 1和R 2如上所述/在分离后或不分离下进行水解,如果需要,将所得通式I的化合物转化为其盐或使其与其盐相同。 通式I的化合物是已知的抗菌剂。 本发明的优点在于使得所需的通式Ⅰ化合物以简单的方式得到,产率高,反应时间短。
    • 7. 发明授权
    • Boric anhydrides of
6-fluoro-7-chloro-1-methylamino-4-oxo-1,4-dihydro-quinoline-3-carboxylic
acid
    • 6-氟-7-氯-1-甲基氨基-4-氧代-1,4-二氢 - 喹啉-3-羧酸的硼酸酐
    • US4806645A
    • 1989-02-21
    • US105295
    • 1987-08-07
    • Istvan HermeczGeza KereszturiLelle VasvariAgnes HorvathMaria BaloghGabor KovacsZoltan Meszaros, deceasedPeter RitliJudit SiposAniko Pajor
    • Istvan HermeczGeza KereszturiLelle VasvariAgnes HorvathMaria BaloghGabor KovacsZoltan Meszaros, deceasedPeter RitliJudit SiposAniko Pajor
    • C07F5/02C07D215/56C07D215/58C07F5/00C07F5/04
    • C07F5/04
    • The invention relates to new 6-fluoro-7-chloro-1-methylamino-4-oxo-1,4-dihydro-quinoline-3-carboxylic acid/boric acid anhydrides of the general Formula I ##STR1## (wherein R and R.sup.1 stand for halogen; an aliphatic acyloxy group comprising 2-6 carbon atoms and optionally substituted by halogen; or an aromatic acyloxy group comprising 7-11 carbon atoms).The new compounds of the general Formula I are valuable intermediates useful in the preparation of the antibacterial agent 6-fluoro-1-methylamino-7-(4-methyl-piperazino)-4-oxo-1,4-dihydro-quinoline-3- carboxylic acid.The new compounds of the general Formula I may be prepared by reacting a compound of the Formula II ##STR2## or a compound of the general Formula III ##STR3## (wherein R.sup.2 stands for alkyl comprising 1-4 carbon atoms) with hydrogen fluoro borate of the Formula IVHBF.sub.4 /IV/or a borone trihalide of the general Formula VBX.sub.3 /V/(wherein X stands for fluorine, chlorine or bromine) or a complex thereof formed with an ether or a borone derivative of the general Formula VI ##STR4## (wherein R.sup.3, R.sup.4 and R.sup.5 stand for alkyl comprising 1-5 carbon atoms and optionally substituted by halogen or aryl comprising 6-10 carbon atoms).
    • PCT No. PCT / HU86 / 00066 Sec。 371日期1987年8月7日 102(e)日期1987年8月7日PCT申请日1986年12月9日PCT公布。 公开号WO87 / 03594 日期:1987年6月18日本发明涉及通式I的新的6-氟-7-氯-1-甲基氨基-4-氧代-1,4-二氢 - 喹啉-3-羧酸/硼酸酐, 图像(I)(其中R和R1代表卤素;包含2-6个碳原子并任选被卤素取代的脂族酰氧基;或包含7-11个碳原子的芳族酰氧基)。 通式I的新化合物是可用于制备抗菌剂6-氟-1-甲基氨基-7-(4-甲基 - 哌嗪子基)-4-氧代-1,4-二氢 - 喹啉线衍生物的有价值的中间体, 3-羧酸。 通式I的新化合物可以通过使式II的化合物(II)或通式III的化合物(III)(其中R 2代表包含1-4个碳原子的烷基) 原子)与式IV的氢氟硼酸盐HBF 4 / IV /或通式V BX 3 / V /(其中X表示氟,氯或溴)的三卤化硼硼烷或其与醚或硼烷衍生物形成的络合物 通式VI(VI)(其中R 3,R 4和R 5代表包含1-5个碳原子并且任选地被卤素或包含6-10个碳原子的芳基取代的烷基)。