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1. 发明授权

US5091530A Baron chelates of quinoline carboxylic acids 失效
标题翻译：喹啉羧酸的巴伦酸
公开(公告)号：US5091530A
公开(公告)日：1992-02-25
申请号：US290105
申请日：1988-11-23
申请人： Istvan Hermecz , Geza Kereszturi , Lelle Vasvari , Agnes Horvath , Marie Balogh , Peter Ritli , Judit Sipos , Aniko Pajor , Katalin Marmarosi
发明人： Istvan Hermecz , Geza Kereszturi , Lelle Vasvari , Agnes Horvath , Marie Balogh , Peter Ritli , Judit Sipos , Aniko Pajor , Katalin Marmarosi
IPC分类号： C07D401/04 , A61K31/4709 , A61K31/495 , A61P31/04 , C07D215/56 , C07F5/02
CPC分类号： C07D215/56
摘要： 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.
摘要翻译： 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。

2. 发明授权

US4940794A Quinoline carboxylic acid boric acid anhydrides 失效
标题翻译：喹啉羧酸硼酸酐
公开(公告)号：US4940794A
公开(公告)日：1990-07-10
申请号：US290167
申请日：1988-12-02
申请人： Istvan Hermecz , Geza Kereszturi , Lelle Vasvari , Agnes Horvath , Maria Halogh , Peter Ritli , Judit Sipos , Aniko Pajor , Katalin Marmarosi
发明人： Istvan Hermecz , Geza Kereszturi , Lelle Vasvari , Agnes Horvath , Maria Halogh , Peter Ritli , Judit Sipos , Aniko Pajor , Katalin Marmarosi
IPC分类号： C07D215/56 , A61K31/47 , A61P31/04 , C07D215/16 , C07D215/54 , C07F5/00 , C07F5/02 , C07F5/04
CPC分类号： C07F5/04
摘要： The invention relates to new quinoline-3-carboxylic acid anhydride intermediates of the Formula I ##STR1## wherein R stands for cyclopropyl, a group of the Formula --CH.sub.2 CR.sup.5 R.sup.6 R.sup.7 wherein R.sup.5, R.sup.6 and R.sup.7 stand for hydrogen or halogen, or phenyl optionally substituted by 1 or 2 halogen,R.sup.1 and R.sup.2 stand for halogen, or an aliphatic acyloxy group containing 2 to 6 carbon atoms optionally substituted by halogen, or an aromatic acyloxy group containing 7 to 11 carbon atoms,R.sup.3 stands for chlorine or fluorine andR.sup.4 stands for hydrogen or fluorine. The compounds of the Formula I are new intermediates for the preparation of known quinoline-3-carbocxylic acids showing antibacterial activity.
摘要翻译： PCT No.PCT / HU88 / 00018 Sec。 371日期：1988年12月2日 102（e）日期1988年12月2日PCT提交1988年4月8日PCT公布。出版物WO88 / 07998 日本公开号为1988年10月20日。本发明涉及式I（I）的新型喹啉-3-羧酸酐中间体，其中R代表环丙基，式-CH 2 CR 5 R 6 R 7基团，其中R5，R6和R7表示对于氢或卤素，或任选被1或2个卤素取代的苯基，R 1和R 2代表卤素，或任选被卤素取代的含2至6个碳原子的脂族酰氧基或含有7至11个碳原子的芳族酰氧基， R3代表氯或氟，R4代表氢或氟。式I化合物是制备显示抗菌活性的已知喹啉-3-羧酸的新中间体。

3. 发明授权

US5300644A Process for the preparation of quinoline carboxylic acids 失效
标题翻译：制备喹啉羧酸的方法
公开(公告)号：US5300644A
公开(公告)日：1994-04-05
申请号：US756345
申请日：1991-09-06
申请人： Istvan Hermecz , Geza Kereszturi , Lelle Vasvari , Agnes Horvath , Maria Balogh , Peter Ritli , Judit Sipos , Aniko Pajor , Katalin Marmarosi
发明人： Istvan Hermecz , Geza Kereszturi , Lelle Vasvari , Agnes Horvath , Maria Balogh , Peter Ritli , Judit Sipos , Aniko Pajor , Katalin Marmarosi
IPC分类号： C07D401/04 , A61K31/4709 , A61K31/495 , A61P31/04 , C07D215/56 , C07F5/02
CPC分类号： C07D215/56
摘要： 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 III ##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.
摘要翻译：本发明涉及制备通式Ⅰ（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 - 哌嗪基及其药物上可接受的盐，其包括使通式II的化合物（II）其中R1和R2代表卤素，含2至6个碳原子的脂族酰氧基并任选被卤素取代，或含有7至11个碳原子的芳族酰氧基与通式III的哌嗪衍生物（III）其中R3代表氢，甲基或乙基或其盐，并对由此得到的通式IV的化合物（IV）进行反应，其中R 1，R 2和R 2 如上所述，在分离后或不分离时进行水解，如果需要，将由此获得的通式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。

4. 发明授权

US5380845A Process for the preparation of quinoline carboxylic acid derivatives 失效
标题翻译：制备喹啉羧酸衍生物的方法
公开(公告)号：US5380845A
公开(公告)日：1995-01-10
申请号：US149692
申请日：1993-11-09
申请人： Istvan Hermecz , Geza Kereszturi , Lelle Vasvari , Agnes Horvath , Maria Balogh , Peter Ritli , Judit Sipos , Aniko Pajor
发明人： Istvan Hermecz , Geza Kereszturi , Lelle Vasvari , Agnes Horvath , Maria Balogh , Peter Ritli , Judit Sipos , Aniko Pajor
IPC分类号： C07D215/56 , C07D401/02 , C07D401/04
CPC分类号： C07D215/56
摘要： The invention relates to a new process for the preparation of antibacterial compounds of the Formula I ##STR1## wherein R.sup.1 stands for phenyl substituted by 1 or 2 halogen atoms;R.sup.2 stands for piperazinyl or 4-methyl-piperazinyl;and pharmaceutically acceptable salts thereof which comprises using a compound of the Formula II ##STR2## wherein R stands for halogen or an aliphatic acyloxy group containing 2 to 6 carbon atoms or an aromatic acyloxy group containing 7 to 11 carbon atoms andR.sup.4 stands for fluorine or chlorine as a starting material.
摘要翻译：本发明涉及制备式I的抗菌化合物（I）的新方法，其中R1代表被1或2个卤素原子取代的苯基; R2代表哌嗪基或4-甲基 - 哌嗪基; 其包括使用式II的化合物（II）其中R代表卤素或含2至6个碳原子的脂族酰氧基或含有7至11个碳原子的芳族酰氧基，R4代表以氟或氯为原料。

5. 发明授权

US4981966A Process for the preparation of quinoline carboxylic acids 失效
标题翻译：制备喹啉羧酸的方法
公开(公告)号：US4981966A
公开(公告)日：1991-01-01
申请号：US295439
申请日：1989-01-10
申请人： Istvan Hermecz , Geza Kereszturi , Lelle Vasvari nee Debreczy , Agnes Horvath , Maria Balogh , Gabor Kovacs , Tamas Szuts , Peter Ritli , Judit Sipos , Aniko Pajor
发明人： Istvan Hermecz , Geza Kereszturi , Lelle Vasvari nee Debreczy , Agnes Horvath , Maria Balogh , Gabor Kovacs , Tamas Szuts , Peter Ritli , Judit Sipos , Aniko Pajor
IPC分类号： C07D401/10 , A61K31/47 , A61P31/04 , C07D215/56 , C07D295/067 , C07D295/155 , C07F5/02 , C07F5/04
CPC分类号： C07D215/56 , C07F5/022 , C07F5/04
摘要： The invention relates to a new process for the preparation of compounds of the Formula I ##STR1## (wherein R stands for hydrogen or methyl) and pharmaceutically acceptable salts thereof which comprises reacting a compound of the Formula V ##STR2## (wherein R.sup.1 and R.sup.2 stand for an aliphatic acyloxy group comprising 2-6 carbon atoms and optionally substituted by halogen; or for an aromatic acyloxy group comprising 7-11 carbon atoms) with an amine of the Formula VI ##STR3## (wherein R has the same meaning as stated above) or a salt thereof and subjecting the compound of the Formula VII ##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 Formula I thus obtained into a salt thereof or setting free the same from its salt.The compounds of the Formula I are known antibacterial agents.The advantage of the process of the present invention is that it makes the desired compounds of the Formula I available in a simple manner, with high yields and in a short reaction time.
摘要翻译：本发明涉及制备式I化合物（I）（其中R代表氢或甲基）及其药学上可接受的盐的新方法，其包括使式V化合物（V ）（其中R 1和R 2表示包含2-6个碳原子并且任选被卤素取代的脂族酰氧基或对于包含7-11个碳原子的芳族酰氧基）与式VI的胺VI，（其中R具有与上述相同的含义）或其盐，并且如此获得的式VII（VII）化合物（其中R，R 1和R 2如上所述）在分离之后或在不分离之前进行水解，以及如果需要将由此获得的式I的化合物转化成其盐或使其与其盐相同。式I的化合物是已知的抗菌剂。本发明方法的优点在于使得所需的式I化合物可以简单的方式得到，产率高，反应时间短。

6. 发明授权

US5284950A Process for the preparation of quinoline carboxyolic acids 失效
标题翻译：喹啉羧酸的制备方法
公开(公告)号：US5284950A
公开(公告)日：1994-02-08
申请号：US691633
申请日：1991-04-25
申请人： Istvan Hermecz , Geza Kereszturi , Lelle Vasvari nee Debreczy , Agnes Horvath , Maria Balogh , Gabor Kovacs , Tamas Szuts , Peter Ritli , Judit Sipos , Aniko Pajor
发明人： Istvan Hermecz , Geza Kereszturi , Lelle Vasvari nee Debreczy , Agnes Horvath , Maria Balogh , Gabor Kovacs , Tamas Szuts , Peter Ritli , Judit Sipos , Aniko Pajor
IPC分类号： C07D215/56 , C07F5/02 , C07F5/04 , C07D403/04
CPC分类号： C07D215/56 , C07F5/022 , C07F5/04
摘要： A method of using a compound of the Formula (V) ##STR1## or a pharmaceutically acceptable salt thereof is disclosed, wherein R.sup.1 and R.sup.2 are each C.sub.1 to C.sub.6 aliphatic acyloxy, unsubstituted or substituted by halogen, or are each C.sub.7 to C.sub.11 aromatic acyloxy,for preventing amination of the 6-position when a compound of the Formula (I) ##STR2## or a pharmaceutically acceptable salt thereof is to be formed, which comprises the steps of:(a) aminating the compound of the Formula (V) or a pharmaceutically acceptable salt thereof with piperazine in an inert organic solvent to yield a compound of the Formula (VII) ##STR3## or a pharmaceutically acceptable salt thereof, and (b) hydrolyzing the compound of the Formula (VII) or a pharmaceutically acceptable salt thereof, after or without isolation, to obtain the compound of the Formula (I), and if desired, converting the compound of the Formula (I) into a pharmaceutically acceptable salt thereof, or setting free the compound of the Formula (I) from its pharmaceutically acceptable salt.
摘要翻译：公开了使用式（V）的化合物或其药学上可接受的盐的方法，其中R 1和R 2各自是未被取代或被卤素取代的C 1至C 6脂族酰氧基，或各自为C7至 C11芳族酰氧基，用于防止当式（I）化合物或其药学上可接受的盐形成时，6-位的胺化，其包括以下步骤：（a）胺化化合物（VII）化合物或其药学上可接受的盐，和（b）将式（Ⅴ）化合物或其药学上可接受的盐与哌嗪在惰性有机溶剂中反应，得到式式（VII）化合物或其药学上可接受的盐在得到式（I）化合物后，如果需要，将式（I）化合物转化为其药学上可接受的盐，或设定释放式的化合物（I）的药学上可接受的盐。

7. 发明授权

US4806645A Boric anhydrides of 6-fluoro-7-chloro-1-methylamino-4-oxo-1,4-dihydro-quinoline-3-carboxylic acid 失效
标题翻译： 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
公开(公告)号：US4806645A
公开(公告)日：1989-02-21
申请号：US105295
申请日：1987-08-07
申请人： Istvan Hermecz , Geza Kereszturi , Lelle Vasvari , Agnes Horvath , Maria Balogh , Gabor Kovacs , Zoltan Meszaros, deceased , Peter Ritli , Judit Sipos , Aniko Pajor
发明人： Istvan Hermecz , Geza Kereszturi , Lelle Vasvari , Agnes Horvath , Maria Balogh , Gabor Kovacs , Zoltan Meszaros, deceased , Peter Ritli , Judit Sipos , Aniko Pajor
IPC分类号： C07F5/02 , C07D215/56 , C07D215/58 , C07F5/00 , C07F5/04
CPC分类号： C07F5/04
摘要： 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).
摘要翻译： 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）。

8. 发明授权

US4803274A Norfloxacin intermediate 失效
标题翻译：诺氟沙星中间体
公开(公告)号：US4803274A
公开(公告)日：1989-02-07
申请号：US105298
申请日：1987-08-07
申请人： Istvan Hermecz , Geza Kereszturi , Lelle Vasvari , Agnes Horvath , Maria Balogh , Gabor Kovacs , Zoltan Meszaros, deceased , Peter Ritli , Judit Sipos , Aniko Pajor
发明人： Istvan Hermecz , Geza Kereszturi , Lelle Vasvari , Agnes Horvath , Maria Balogh , Gabor Kovacs , Zoltan Meszaros, deceased , Peter Ritli , Judit Sipos , Aniko Pajor
IPC分类号： C07F5/02 , C07D215/56 , C07F5/00 , C07F5/04
CPC分类号： C07F5/04
摘要： The invention relates to a process for the preparation of compounds of the Formula I ##STR1## (wherein R and R.sup.1 stand for an aliphatic acyloxy group comprising 2-5 carbon atoms and optionally substituted by halogen or for an aromatic acyloxy group comprising 7-11 carbon atoms), which comprises reacting a compound of the general Formula II ##STR2## (wherein R.sup.2 stands for hydrogen or alkyl comprising 1-4 carbon atoms) with a boron derivative of the Formula III ##STR3## (wherein R.sup.3, R.sup.4 and R.sup.5 stand for an alkyl group comprising 1-4 carbon atoms and optionally substituted by halogen or for an aryl group comprising 6-10 carbon atoms).The new compounds of the general Formula I are useful pharmaceutical intermediates.
摘要翻译： PCT No.PCT / HU86 / 00068 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。第WO87 / 03595号公报日本1987年6月18日。本发明涉及制备式I化合物（I）的方法（其中R和R 1代表包含2-5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），其包括使通式II的化合物（II）（其中R 2表示氢或包含1-4个碳原子的烷基）与式式III（III）（其中R3，R4和R5代表含有1-4个碳原子的烷基，任选被卤素取代或含有6-10个碳原子的芳基）。通式I的新化合物是有用的药物中间体。

9. 发明授权

US4871849A 1-Methylamino-quinoline-carboxylic acid derivatives 失效
标题翻译： 1-甲基氨基 - 喹啉羧酸衍生物
公开(公告)号：US4871849A
公开(公告)日：1989-10-03
申请号：US105299
申请日：1987-06-24
申请人： Istvan Hermecz , Geza Kereszturi , Lelle Vasvavi , Agnes Horvath , Maria Balogh , Gabor Kovacs , Tamas Szuts , Peter Ritli , Judit Sipos , Aniko Pajor
发明人： Istvan Hermecz , Geza Kereszturi , Lelle Vasvavi , Agnes Horvath , Maria Balogh , Gabor Kovacs , Tamas Szuts , Peter Ritli , Judit Sipos , Aniko Pajor
IPC分类号： C07D401/02 , A61K31/47 , C07D20060101 , C07D215/00 , C07D215/56 , C07D215/58 , C07D401/04 , C07D401/10 , C07D403/04 , C07D403/10 , C07F5/02
CPC分类号： C07F5/022 , C07D215/58
摘要： The present invention relates to a process for the preparation of compounds of the general Formula I ##STR1## and pharmaceutically acceptable salts thereof (wherein R stands for piperazinyl or 4-methyl-piperazinyl) which comprises reacting a compound of the general Formula II ##STR2## (wherein R.sup.1 and R.sup.2 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) with a piperazine of the general Formula III ##STR3## (wherein R.sup.3 represent hydrogen or methyl) or a salt thereof, hydrolysing the compound of the general Formula IV ##STR4## thus obtained (wherein R, R.sup.1 and R.sup.2 are as stated above) without or after hydrolysis 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 process of the present invention is that it enables the preparation of the compounds of the general Formula I in a simple manner, with high yields and in a short reaction time.
摘要翻译： PCT No.PCT / HU86 / 00067 Sec。 371日期1987年6月24日 102（e）1987年6月24日PCT PCT日期：1986年12月9日PCT公布。公开号WO87 / 03586 日期：1987年6月18日。本发明涉及一种制备通式I的化合物及其药学上可接受的盐（其中R代表哌嗪基或4-甲基 - 哌嗪基）的方法，其包括使通式II的化合物（其中R1和R2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者包含7-11个碳原子的芳香酰氧基）与哌嗪通式III III（其中R 3表示氢或甲基）或其盐，水解由此得到的通式IV的化合物（其中R，R 1和R 2如上所述），无水解后，如果需要，将由此获得的通式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。本发明方法的优点在于它能够以高产率和短的反应时间以简单的方式制备通式I的化合物。

10. 发明授权

US5294712A Process for the preparation of quinoline carboxylic acids 失效
标题翻译：制备喹啉羧酸的方法
公开(公告)号：US5294712A
公开(公告)日：1994-03-15
申请号：US583296
申请日：1990-09-14
申请人： Istvan Hermecz , Geza Keresturi , Lelle V. Debreczy , Agnes Horvath , Maria Balogh , Gabor Kovacs , Tamas Szuts , Peter Ritli , Judit Sipos , Aniko Pajor
发明人： Istvan Hermecz , Geza Keresturi , Lelle V. Debreczy , Agnes Horvath , Maria Balogh , Gabor Kovacs , Tamas Szuts , Peter Ritli , Judit Sipos , Aniko Pajor
IPC分类号： C07D215/56 , C07F5/02 , C07D401/04
CPC分类号： C07D215/56 , C07F5/022
摘要： The invention relates to a new process for the preparation of compounds of the Formula I ##STR1## (wherein R stands for hydrogen or methyl) and pharmaceutically acceptable salts thereof which comprises reacting a compound of the Formula V ##STR2## (wherein R.sup.1 and R.sup.2 stand for an aliphatic acyloxy group comprising 2-6 carbon atoms and optionally substituted by halogen: or for an aromatic acyloxy group comprising 7-11 carbon atoms) with an amine of the Formula VI ##STR3## (wherein R has the same meaning as stated above) or a salt thereof and subjecting the compound of the Formula VII ##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 Formula I thus obtained into a salt thereof or setting free the same from its salt.The compounds of the Formula I are known antibacterial agents.
摘要翻译：本发明涉及制备式I化合物（I）（其中R代表氢或甲基）及其药学上可接受的盐的新方法，其包括使式V化合物（V ）（其中R 1和R 2表示包含2-6个碳原子并且任选被卤素取代的脂族酰氧基或用于包含7-11个碳原子的芳族酰氧基）与式VI的胺（VI）（其中R具有与上述相同的含义）或其盐，并且如此获得的式VII（VII）化合物（其中R，R 1和R 2如上所述）在分离之后或在不分离之前进行水解，以及如果需要将由此获得的式I的化合物转化成其盐或使其与其盐相同。式I的化合物是已知的抗菌剂。

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