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1. 发明授权

US5235097A Process for the preparation of 2,2-dimethyl-5-(2,5-dimethyl-phenoxy)-pentanoic acid, intermediates for preparing this compound and process for preparing the intermediates 失效
标题翻译：制备2,2-二甲基-5-（2,5-二甲基 - 苯氧基） - 戊酸的方法，制备该化合物的中间体及其制备方法
公开(公告)号：US5235097A
公开(公告)日：1993-08-10
申请号：US890781
申请日：1992-06-01
申请人： Zoltan Zubovics , Gabor Feher , Lajos Toldi , Gabor Kovacs , Antal Simay , Eva Kovacs nee Bozo , Imre Moravcsik , Ferenc Szederkenyi , Gyorgy Krasznai , Gyorgyi Vereczkey nee Donath , Kalman Nagy
发明人： Zoltan Zubovics , Gabor Feher , Lajos Toldi , Gabor Kovacs , Antal Simay , Eva Kovacs nee Bozo , Imre Moravcsik , Ferenc Szederkenyi , Gyorgy Krasznai , Gyorgyi Vereczkey nee Donath , Kalman Nagy
IPC分类号： C07C51/09 , C07C69/63 , C07C69/712
CPC分类号： C07C69/712 , C07C51/09 , C07C69/63
摘要： The invention relates to an improved process for the preparation of 2,2-dimethyl-5-(2,5-dimethylphenoxy)-pentanoic acid of Formula (I) ##STR1## which comprises reacting an ester of the general Formula (X) ##STR2## wherein X represents halogen and Z stands for a straight or branched chain C.sub.1-8 alkylene group optionally substituted by one or two 2,2-dimethyl-5-halopentanoyloxy group(s), wherein halo represents chlorine or bromine, and in which alkylene group one or two methylene group(s) may be optionally replaced either by hetero atom(s) or by a bivalent heterocyclic group--with an alkali salt of 2,5-dimethylphenol of Formula (II) ##STR3## or with an ester of the latter formed with a lower alkanoic acid, and hydrolizing the aryloxy-substituted ester of the general Formula (XI) thus obtained. ##STR4## Furthermore the invention relates to intermediate compounds of the general Formula (X), wherein X and Z are as stated above, and to a process for the preparation thereof.
摘要翻译：本发明涉及制备式（I）的（2,2-二甲基-5-（2,5-二甲基苯氧基） - 戊酸（I）的改进方法，其包括使通式（（X）其中X表示卤素，Z表示任选被一个或两个2,2-二甲基-5-卤代戊酰氧基取代的直链或支链C 1-8亚烷基，其中卤代表氯或溴，并且其中亚烷基一个或两个亚甲基可以任选地被杂原子或二价杂环基取代，与式（II）的2,5-二甲基苯酚的碱金属盐（II）或与低级链烷酸形成的酯，并使由此获得的通式（XI）的芳氧基取代的酯水解。（XI）此外，本发明涉及通式（X）的中间体化合物，其中X和Z如上所述，以及其制备方法。

2. 发明授权

US5155260A Process for the preparation of 2,2-dimethyl-5-(2,5-dimethyl-phenoxy)-pentanoic acid, intermediates for preparing this compound and process for preparing the intermediates 失效
标题翻译：制备2,2-二甲基-5-（2,5-二甲基 - 苯氧基） - 戊酸的方法，用于制备该化合物的中间体和制备中间体的方法
公开(公告)号：US5155260A
公开(公告)日：1992-10-13
申请号：US698081
申请日：1991-05-10
申请人： Zoltan Zubovics , Gabor Feher , Lajos Toldi , Gabor Kovacs , Antal Simay , Eva Kovacs nee Bozo , Imre Moravcsik , Ferenc Szederkenyi , Gyorgy Krasznai , Gyorgyi Vereczkey nee Donath , Kalman Nagy
发明人： Zoltan Zubovics , Gabor Feher , Lajos Toldi , Gabor Kovacs , Antal Simay , Eva Kovacs nee Bozo , Imre Moravcsik , Ferenc Szederkenyi , Gyorgy Krasznai , Gyorgyi Vereczkey nee Donath , Kalman Nagy
IPC分类号： B01J27/08 , A61K31/19 , A61K31/235 , C07B61/00 , C07C51/09 , C07C59/48 , C07C59/64 , C07C59/68 , C07C65/21 , C07C67/31 , C07C69/63 , C07C69/712 , C07C229/24 , C07D211/34
CPC分类号： C07C69/712 , C07C51/09 , C07C69/63
摘要： The invention relates to an improved process for the preparation of 2,2-dimethyl-5-(2,5-dimethylphenoxy)-pentanoic acid of Formula (I) ##STR1## which comprises reacting an ester of the general Formula (X) ##STR2## wherein X represents halogen and Z stands for a straight or branched chain C.sub.1-8 alkylene group optionally substituted by one or two 2,2-dimethyl-5-halopentanoyloxy group(s), wherein halo represents chlorine or bromine, and in which alkylene group one or two methylene group(s) may be optionally replaced either by hetero atom(s) or by a bivalent heterocyclic group--with an alkali salt of 2,5-dimethylphenol of Formula (II) ##STR3## or with an ester of the latter formed with a lower alkanoic acid, and hydrolizing the aryloxy-substituted ester of the general Formula (XI) thus obtained. Furthermore the invention relates to intermediate compounds of the general Formula (X), wherein X and Z are as stated above, and to a process for the preparation thereof.
摘要翻译：本发明涉及制备式（I）的2,2-二甲基-5-（2,5-二甲基苯氧基） - 戊酸的改进方法，其包括使通式（X）的酯与（X）其中X表示卤素，Z表示任选被一个或两个2,2-二甲基-5-卤代戊酰氧基取代的直链或支链C 1-8亚烷基，其中卤代表氯或溴，并且其中亚烷基一个或两个亚甲基可以任选被杂原子或二价杂环基取代，与式（II）的2,5-二甲基苯酚的碱金属盐（IMAGE）（ II）或与低级链烷酸形成的酯，并使由此获得的通式（XI）的芳氧基取代的酯水解。（XI）此外，本发明涉及通式（X）的中间体化合物，其中X和Z如上所述，以及其制备方法。

3. 发明授权

US4425349A Sulfur-containing isoquinoline derivatives in pharmaceutical compositions and methods of use 失效
标题翻译：含硫异喹啉衍生物在药物组合物和使用方法中的应用
公开(公告)号：US4425349A
公开(公告)日：1984-01-10
申请号：US381775
申请日：1982-05-25
申请人： Kalman Takacs , Maria H. Papp , Gabor Kovacs , Ilona K. Ajzert , Antal Simay , Peter Literati Nagy , Marian E. Puskas , Gyula Sebestyen , Istvan Stadler , Zoltan Sumeghy
发明人： Kalman Takacs , Maria H. Papp , Gabor Kovacs , Ilona K. Ajzert , Antal Simay , Peter Literati Nagy , Marian E. Puskas , Gyula Sebestyen , Istvan Stadler , Zoltan Sumeghy
IPC分类号： C07D217/14 , C07D513/04 , A61K31/47
CPC分类号： C07D513/04 , C07D217/14 , Y10S514/826 , Y10S514/869
摘要： The invention concerns new sulfur-containing isoquinoline derivatives. More particularly, the invention relates to isoquinoline derivatives of the general formula (I) ##STR1## wherein R independently represents hydrogen, hydroxyl or alkoxy having 1 to 4 carbon atoms,R.sup.1 is hydrogen, alkyl having 1 to 4 carbon atoms and optionally substituted with phenyl, phenyl optionally substituted with one or more halogen or alkoxy group, cyano or carbamoyl,R.sup.2 is phenyl optionally substituted with one or more halogen, alkoxy or carboxyl, or a group of the general formula A ##STR2## wherein R.sup.3 is hydrogen, a straight or branched chained alkyl having 1 to 4 carbon atoms or phenyl,m and n independently represent 0, 1 or 2, with the proviso that m+n is at least 1,R.sup.4 is hydrogen, phenyl, hydroxyl, acyloxy, carboxyl, alkoxycarbonyl having 1 to 6 carbon atoms, carbamoyl, carbazoyl or dialkylamino containing 1 to 6 carbon atoms in the alkyl moiety, orR.sup.2 is a straight or branched chained alkylene group having 1 to 6 carbon atoms, andthe dotted line stands for a further carbon-carbon bond or hydrogen atoms in the 3- and 4-positions of the ring,and salts and cyclic amides thereof.The new compounds possess valuable pharmaceutical activities, more particularly, are potent diuretic, antiasthmatic, hypotensive and antiinflammatory agents. Thus another aspect of the invention is a pharmaceutical composition which comprises as active ingredient a pharmaceutically effective amount of at least one compound of the general formula (I) with at least one pharmaceutically inert carrier or diluent. The invention also relates to a process for preparing these compounds.
摘要翻译：本发明涉及新的含硫异喹啉衍生物。更具体地说，本发明涉及通式（I）的异喹啉衍生物，其中R独立地表示氢，羟基或具有1至4个碳原子的烷氧基，R 1是氢，具有1至4个碳原子的烷基和任选地被苯基取代，任选被一个或多个卤素或烷氧基取代的苯基，氰基或氨基甲酰基，R 2是任选被一个或多个卤素，烷氧基或羧基取代的苯基或通式A的基团，其中R 3是氢，具有1至4个碳原子的直链或支链烷基或苯基，m和n独立地表示0,1或2，条件是m + n至少为1，R4为氢，苯基，羟基，酰氧基，羧基，具有1至6个碳原子的烷氧基羰基，在烷基部分含有1至6个碳原子的氨基甲酰基，咔唑基或二烷基氨基，或者是具有1至6个碳原子的直链或支链的亚烷基，虚线代表进一步c 环的3-和4-位的碳 - 碳键或氢原子，及其盐和环状酰胺。新化合物具有有价值的药物活性，特别是有效的利尿，止喘，降压和抗炎药。因此，本发明的另一方面是药物组合物，其包含作为活性成分的药学有效量的至少一种通式（I）的化合物与至少一种药学上惰性的载体或稀释剂。本发明还涉及制备这些化合物的方法。

4. 发明授权

US4373104A Sulfur-containing isoquinoline derivatives, process for the preparation thereof and pharmaceutical compositions containing them 失效
标题翻译：含硫异喹啉衍生物，其制备方法和含有它们的药物组合物
公开(公告)号：US4373104A
公开(公告)日：1983-02-08
申请号：US164939
申请日：1980-07-01
申请人： Kalman Takacs , Maria H. Papp , Gabor Kovacs , Ilona K. Ajzert , Antal Simay , Peter L. Nagy , Marian E. Puskas , Gyula Sebestyen , Istvan Stadler , Zoltan Sumeghy
发明人： Kalman Takacs , Maria H. Papp , Gabor Kovacs , Ilona K. Ajzert , Antal Simay , Peter L. Nagy , Marian E. Puskas , Gyula Sebestyen , Istvan Stadler , Zoltan Sumeghy
IPC分类号： C07D217/00 , A61K31/47 , A61K31/472 , A61P7/08 , A61P7/10 , A61P9/12 , A61P11/00 , A61P11/06 , A61P11/08 , A61P29/00 , A61P43/00 , C07D217/14 , C07D217/16 , C07D513/04
CPC分类号： C07D513/04 , C07D217/14 , Y10S514/869
摘要： Isoquinolines are disclosed of the formula (I) ##STR1## wherein R independently represents hydrogen, hydroxyl or alkoxy having 1 to 4 carbon atoms,R.sup.1 is hydrogen, alkyl having 1 to 4 carbon atoms and optionally substituted with phenyl, phenyl optionally substituted with one or more halogen or alkoxy group, cyano or carbomoyl,R.sup.2 is phenyl optionally substituted with one or more halogen, alkoxy or carboxyl, or a group of the general formula A ##STR2## wherein R.sup.3 is hydrogen, a straight or branched chained alkyl having 1 to 4 carbon atoms or phenyl,m and n independently represent 0, 1 or 2, with the proviso that m+n is at least 1,R.sup.4 is hydrogen, phenyl, hydroxyl, acyloxy, carboxyl, alkoxycarbonyl having 1 to 6 carbon atoms, carbamoyl, carbazoyl or dialkylamino containing 1 to 6 carbon atoms in the alkyl moiety, orR.sup.2 is a straight or branched chained alkylene group having 1 to 6 carbon atoms, andthe dotted line stands for a further carbon-carbon bond or hydrogen atoms in the 3- and 4-positions of the ring,or salts thereof. The new compounds are potent diuretic agents.
摘要翻译：公开了式（I）的异喹啉（I）其中R独立地表示氢，羟基或具有1至4个碳原子的烷氧基，R 1是氢，具有1至4个碳原子的烷基，任选被苯基取代，苯基任选地被一个或多个卤素或烷氧基取代，氰基或甲酰甲酰基，R 2是任选被一个或多个卤素，烷氧基或羧基取代的苯基或通式A的基团，其中R 3是氢，直链或支链具有1至4个碳原子的烷基或苯基，m和n独立地表示0,1或2，条件是m + n至少为1，R4为氢，苯基，羟基，酰氧基，羧基，具有1至6个碳原子的烷氧基羰基碳原子，氨基甲酰基，咔唑基或在烷基部分含有1至6个碳原子的二烷基氨基，或者R2是具有1至6个碳原子的直链或支链链烯基，虚线代表另外的碳 - 碳键或氢原子在3-和环的4-位，或其盐。新化合物是有效的利尿剂。

5. 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。

6. 发明授权

US4599327A Dibenzo[bd]pyran derivatives, process for the preparation thereof and pharmaceutical compositions containing same 失效
标题翻译：二苯并[bd]吡喃衍生物，其制备方法和含有它们的药物组合物
公开(公告)号：US4599327A
公开(公告)日：1986-07-08
申请号：US557629
申请日：1983-12-02
申请人： Mihaly Nogradi , Dezso Korbonits , Agnes Gottsegen , Sandor Antus , Zsuzsa Furst , Jozsef Knoll , Jozsef Szejtli , Agnes Stadler , Gabor Kovacs , Katalin Marmarosi
发明人： Mihaly Nogradi , Dezso Korbonits , Agnes Gottsegen , Sandor Antus , Zsuzsa Furst , Jozsef Knoll , Jozsef Szejtli , Agnes Stadler , Gabor Kovacs , Katalin Marmarosi
IPC分类号： A61K31/35 , A61K31/352 , A61K31/715 , A61P1/08 , A61P23/00 , A61P23/02 , A61P25/02 , A61P25/04 , C07C43/178 , C07C43/205 , C07C43/23 , C07C59/68 , C07D221/12 , C07D311/78 , C07D311/80 , C07D311/92 , C07D493/10 , C08B37/00 , C08B37/16 , A61K31/70
CPC分类号： C07D493/10 , C07C309/00 , C07C43/1782 , C07C43/1785 , C07C43/2055 , C07C43/23 , C07C59/68 , C07D221/12 , C07D311/78 , C07D311/80 , C08B37/0015
摘要： 2,6-di-O-methyl-beta-cyclodextrin complexes of compounds of the formula (1a) ##STR1## wherein R.sup.2' stands for C.sub.1 to C.sub.12 alkyl or a group of the formula ##STR2## in which R.sup.11 is C.sub.1 to C.sub.4 alkyl;R.sup.12 is hydrogen or C.sub.1 to C.sub.4 alkyl;n is 0 or 1;p is 1 to 4;r is 1 to 4; andR.sup.3' and R.sup.4' are each C.sub.1 to C.sub.4 alkyl, or pharmaceutically salts thereof are disclosed, having analgesic activity.
摘要翻译：式（1a）化合物的2,6-二-O-甲基-β-环糊精复合物其中R 2'代表C 1至C 12烷基或其中R 11为C 1至C 4的式烷基; R 12是氢或C 1至C 4烷基; n为0或1; p为1〜4; r为1〜4; 和R 3'和R 4'各自为C1至C4烷基，或其药学上可接受的盐，具有止痛活性。

7. 发明授权

US4450309A Process for the preparation of unsaturated geminal dihalogen compounds 失效
标题翻译：制备不饱和偕二卤化合物的方法
公开(公告)号：US4450309A
公开(公告)日：1984-05-22
申请号：US391866
申请日：1982-06-24
申请人： Rudolf Soos , Jozsef Nemes , Laszlo Vidra , Miklos Szelestei , Gabor Kovacs , Istvan Szekeley
发明人： Rudolf Soos , Jozsef Nemes , Laszlo Vidra , Miklos Szelestei , Gabor Kovacs , Istvan Szekeley
IPC分类号： C07C17/361 , B01J21/00 , B01J23/00 , B01J23/06 , B01J27/00 , C07B61/00 , C07C17/00 , C07C17/363 , C07C21/02 , C07C21/04 , C07C21/17 , C07C21/19 , C07C67/00 , C07C17/33
CPC分类号： C07C17/363
摘要： The invention relates to a new process for preparing unsaturated geminal dihalogen compounds. More particularly, the invention concerns a process for preparing compounds of the formula (I) ##STR1## wherein X is halogen,R.sup.1 is a straight or branched chained alkenyl group having 2 to 6 carbon atoms,by clearing the corresponding 1-substituted 2,2,2-trihaloethylesters.
摘要翻译：本发明涉及一种制备不饱和偕二卤化合物的新方法。更具体地，本发明涉及制备式（I）化合物的方法，其中X是卤素，R 1是具有2-6个碳原子的直链或支链链烯基，通过将相应的1-取代的2， 2,2-三卤乙基酯。

8. 发明授权

US4851416A Berban derivatives as .alpha..sub.2 -adrenergic antagonists 失效
标题翻译： Berban衍生物作为α2-肾上腺素能拮抗剂
公开(公告)号：US4851416A
公开(公告)日：1989-07-25
申请号：US867323
申请日：1986-05-23
申请人： Szilveszter Vizi , Csaba Szantai , Lajos Szabo , Istvan Toth , Gabor Kovacs , Jeno Marton , Laszlo Harsing , Gyorgy Somogyi , Jozsef Gaal
发明人： Szilveszter Vizi , Csaba Szantai , Lajos Szabo , Istvan Toth , Gabor Kovacs , Jeno Marton , Laszlo Harsing , Gyorgy Somogyi , Jozsef Gaal
IPC分类号： C07D453/00 , A61K31/47 , A61P25/02 , A61P25/24 , A61P25/26 , C07D455/03 , C07D471/04
CPC分类号： C07D455/00
摘要： The invention relates to novel racemic or optically active berban derivatives of the formula (I) ##STR1## wherein R.sup.1 and R.sup.2 represent independently from the other a hydroxyl, straight or branched chain alkoxy group 1 to 6 carbon atoms or R.sup.1 and R.sup.2 together represent a C.sub.1-3 alkylenedioxy group;R.sup.3 and R.sup.4 represent independently from the other hydrogen, straight or branched chain alkyl group, having 1 to 6 carbon atoms and optionally substituted by hydroxyl group, or a C.sub.2-6 alkoxycarbonyl or cyano group; andR.sup.5 represents hydrogen, straight or branched chain alkyl group having 1 to 6 carbon atoms, C.sub.1-7 aliphatic or aromatic acyl group or C.sub.1-7 alkylsulphonyl or arylsulphonyl group, anda salt thereof, to pharmaceutical compositions containing them, to the use as well as to process for preparing the novel compounds. The compounds of the formula (I) are selective .alpha..sub.2 -adrenergic receptor-blocking substances and thus, they may be used for the treament of depressive illnesses.
摘要翻译：本发明涉及式（I）的新型外消旋或光学活性伯类衍生物，其中R 1和R 2彼此独立地表示1至6个碳原子的羟基，直链或支链烷氧基或R1和R2 一起代表C1-3亚烷基二氧基; R3和R4独立地表示独立于具有1-6个碳原子并且任选被羟基取代的另一个氢，直链或支链烷基或C 2-6烷氧羰基或氰基; 并且R 5表示氢，具有1〜6个碳原子的直链或支链烷基，C 1-7脂族或芳族酰基或C 1-7烷基磺酰基或芳基磺酰基及其盐与含有它们的药物组合物以及用于制备新化合物的方法。式（I）化合物是选择性α2-肾上腺素能受体阻断物质，因此可用于抑郁症的治疗。

9. 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）。

10. 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。

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