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11. 发明申请

WO0105759A3 PROCESS FOR THE PREPARATION OF SPIRO-[CIS-4-(BETA-HYDROXYETHYLOXY)CYCLOHEXANE-(3H) INDOL)-2'(1'H)-ONE DERIVATIVES 审中-公开
标题翻译：制备SPIRO- [CIS-4-（β-羟基乙氧基）环己基 - （3H）吲哚）-2'（1'H） - 酮衍生物的方法
公开(公告)号：WO0105759A3
公开(公告)日：2001-07-19
申请号：PCT/HU0000079
申请日：2000-07-13
申请人： SANOFI SYNTHELABO , HEJA GERGELY , CSIKOS EVA , GOENCZI CSABA , HALASZ JUDIT , HAJDU FELIX , HERMECZ ISTVAN , KIS LASZLO , NAGY LAJOS , SANTANE CSUTOR ANDREA , SIMON KALMAN , SZOMOR TIBORNE , SZVOBODA GYOERGYNE
发明人： HEJA GERGELY , CSIKOS EVA , GOENCZI CSABA , HALASZ JUDIT , HAJDU FELIX , HERMECZ ISTVAN , KIS LASZLO , NAGY LAJOS , SANTANE CSUTOR ANDREA , SIMON KALMAN , SZOMOR TIBORNE , SZVOBODA GYOERGYNE
IPC分类号： C07B61/00 , C07D209/96
CPC分类号： C07D209/96
摘要： The invention relates to a process for the preparation of spiro[ cis -4-( beta -hydroxyethyloxy) cyclohexane- [3 H ] -2'[1' H ]-one derivatives of the formula (I) wherein R and R stand independently from each other for hydrogen, C1-4alkyl, C1-4alkoxy, C1-4alkylthio, C1-4polyfluroalkyl, C1-4polyfluroalkoxy, C3-7cycloalkyloxy, C3-7cycloakylthio, phenoxy, benzyloxy or nitro group by reduction of a dispiro [(1,3- dioxolane)-2,4'- cyclohexane-1', 3"-[3 H ]indol] -2"[1" H ]- one derivative of general formula (II), wherein R and R are as defined above, which comprises carrying out the reduction (a) with sodium cyanoborohydride in the presence of a Lewis acid, or (b) with sodium borohydride in the presence of a strong acid.
摘要翻译：本发明涉及制备螺[cis 4-（β-羟基乙氧基）环己烷 - [3H] -2'[1']螺[ H] - 其中R 1和R 2彼此独立地表示氢，C 1-4烷基，C 1-4烷氧基，C 1-4烷硫基，C 1-4聚氟烷基，C 1 -C 4的式（I）的一种衍生物 4-聚氟烷氧基，C 3-7环烷氧基，C 3-7环烷硫基，苯氧基，苄氧基或硝基，通过还原一个[（1,3-二氧戊环）-2,4'-环己烷-1'，3“ - [3 H 吲哚] -2“[1”] - 通式（II）的一种衍生物，其中R 1和R 2如上所定义，其包括携带在路易斯酸存在下用氰基硼氢化钠还原（a），或（b）在强酸存在下与硼氢化钠反应。

12. 发明申请

WO9722602A2 A PROCESS FOR THE STEREOSELECTIVE REDUCTION OF alpha , beta -UNSATURATED KETONES 审中-公开
标题翻译： α，β受体克隆的STERE选择性还原的方法
公开(公告)号：WO9722602A2
公开(公告)日：1997-06-26
申请号：PCT/HU9600079
申请日：1996-12-18
申请人： CHINOIN GYOGYSZER ES VEGYESZET , GALAMBOS EVA & HF , GALAMBOS ATTILA & HM , BALOGHNE KARDOS ZSUZSANNA , BENNO NANDOR , BERESNE POVARNY MAGDOLNA , DALMADI GYULA , EBINGER KATALIN , FORRO LASZLO , HAJDU FELIX , HERMECZ ISTVAN , LUKACS GEZA , MOZSOLITS KAROLY , POLIKNE SZIGETI KATALIN , SEBESTYEN JUDIT , SZABO TIBOR , SZEVERENYI ZOLTAN , VAJDA ERVIN , VANKAI GABOR , VOFELY PAL
发明人： GALAMBOS GEZA DI , BALOGHNE KARDOS ZSUZSANNA , BENNO NANDOR , BERESNE POVARNY MAGDOLNA , DALMADI GYULA , EBINGER KATALIN , FORRO LASZLO , HAJDU FELIX , HERMECZ ISTVAN , LUKACS GEZA , MOZSOLITS KAROLY , POLIKNE SZIGETI KATALIN , SEBESTYEN JUDIT , SZABO TIBOR , SZEVERENYI ZOLTAN , VAJDA ERVIN , VANKAI GABOR , VOFELY PAL
IPC分类号： C07D307/935 , C07D307/83
CPC分类号： C07D307/83
摘要： A process for the preparation of alpha , beta -unsaturated alcohols of general formula (I), wherein R means an alkyl group of 1-4 carbon atoms, or benzoyloxy group optionally substituted with a phenyl group; R means a hydrogen atom or an alkyl group of 1-4 carbon atoms; R means a hydrogen atom or an alkyl group of 1-4 carbon atoms; R means an alkyl group of 1-6 carbon atoms optionally substituted by phenyl group or cycloalkyl group of 5-7 carbon atoms; or a phenoxy group optionally substituted by a halogen atom, or a cycloalkyl group of 5-7 carbon atoms; R means a hydrogen atom or a halogen atom; characterized in that a alpha , beta -unsaturated ketone of general formula (II) wherein the meanings of R, R , R , R , and R are as given above, is diastereoselectively reduced with a borohydride type compound in an aprotic solvent, in the presence of an inorganic substance dissoluble in the reaction mixture and having particle size from 0.01 micrometer to 10000 micrometer and optionally from the resulting mixture of epimeric alpha , beta -unsaturated alcohols of general formula (I) and (III), wherein the meanings of R, R , R , R , and R are as given above, the alpha , beta -unsaturated alcohol of general formula (I) is separated by methods known per se.
摘要翻译：一种制备通式（I）的α，β-不饱和醇的方法，其中R表示1-4个碳原子的烷基或任选被苯基取代的苯甲酰氧基; R 1表示氢原子或1-4个碳原子的烷基， R 2表示氢原子或1-4个碳原子的烷基; R 3表示任选被5-7个碳原子的苯基或环烷基取代的1-6个碳原子的烷基; 或任选被卤素原子取代的苯氧基或5-7个碳原子的环烷基; R 4表示氢原子或卤素原子; 其特征在于通式（II）的α，β-不饱和酮，其中R，R 1，R 2，R 3和R 4的含义如上所述，是非对映选择性降低的在非质子传递溶剂中，在可溶于反应混合物的无机物质存在下，其粒径为0.01微米至10000微米，并且任选地由得到的通式（b）的差向异构α，β-不饱和醇的混合物 I）和（III），其中R，R 1，R 2，R 3和R 4的含义如上所定义，通式（Ⅰ）的α，β-不饱和醇）通过本身已知的方法分离。

13. 发明申请

WO0105760A2 NEW PROCESS FOR THE PREPARATION OF SPIRO [(4-CYCLOHEXANONE)-[3H]INDOL]-2'[1'H]-ONE DERIVATIVES 审中-公开
标题翻译：制备螺[（4-环己酮） - [3H]吲哚] -2'[1'H] - 一种衍生物的新方法
公开(公告)号：WO0105760A2
公开(公告)日：2001-01-25
申请号：PCT/HU0000081
申请日：2000-07-13
申请人： SANOFI SYNTHELABO , GOENCZI CSABA , CSIKOS EVA , HERMECZ ISTVAN , HEJA GERGELY , ILLAR ARPAD , NAGY LAJOS , SANTANE CSUTOR ANDREA , SIMON ATTILA , SIMON KALMAN , SMELKONE ESEK AGOTA , SZOMOR TIBORNE , SZVOBODA GYOERGYNE
发明人： GOENCZI CSABA , CSIKOS EVA , HERMECZ ISTVAN , HEJA GERGELY , ILLAR ARPAD , NAGY LAJOS , SANTANE CSUTOR ANDREA , SIMON ATTILA , SIMON KALMAN , SMELKONE ESEK AGOTA , SZOMOR TIBORNE , SZVOBODA GYOERGYNE
IPC分类号： C07B61/00 , C07D209/34 , C07D209/96 , C07D405/04 , C07D209/00
CPC分类号： C07D405/04 , C07D209/34 , C07D209/96 , Y02P20/55
摘要： The invention relates to a process for the preparation of spiro[(4-cyclohexanone)- [3H]indol]- 2'[1'H]- one derivatives of general formula (I) - wherein R and R independently stand for hydrogen, C1-4alkyl, C1-4alkoxy, C1-4alkylthio, C1-4 polyfluoroalkyl, C1-4 polyfluoroalkoxy, C3-7 cycloalkyloxy, C3-7cycloalkylthio, phenoxy, benzyloxy or nitro group -, characterized by reacting an indolin-2-one derivative of general formula (II) - wherein R and R are as defined above - with a compound capable for introducing a protective group, coupling the compound of general formula (III), thus obtained - wherein R and R are as defined above and A stands for a protective group - with acrylic acid C1-4ester, cyclizing the resulting compound of general formula (IV)- wherein R and R are as defined above - with a compound capable for introducing a protective group, coupling the compound of formula (III) thus obtained, - wherein R and R are as defined above and A stands for a protective group - with an acrylic acid C ester; cyclizing the resulting compound of formula (IV) - wherein R and R are as defined above R stands for C1-4alkyl and A stands for a protective group -, eliminating the -COOR group and the A protective group of the keto-ester of general formula (V) - wherein R and R are as defined above, R stands for C1-4alkyl and A stands for a protective group -, optionally without isolation of the compounds of general formulae (IV) and/or (V) and/or (VI).
摘要翻译：本发明涉及制备通式（I）的螺[（4-环己酮） - [3H]吲哚] -2'[1'H] - 酮衍生物的方法，其中R 1和R 2 独立地表示氢，C1-4烷基，C1-4烷氧基，C1-4烷硫基，C1-4多氟烷基，C1-4多氟烷氧基，C3-7环烷氧基，C3-7环烷硫基，苯氧基，苄氧基或硝基 - （II）（其中R 1和R 2如上定义）与能够引入保护基的化合物反应，将由此获得的通式（III）的化合物与通式其中R 1和R 2定义如上，A代表保护基 - 与丙烯酸C 1-4酯反应，环化得到的通式（IV）的化合物 - 其中R 1和R 2如式如上所定义的 - 与能够引入保护基团的化合物偶联，由此获得的式（III）化合物，其中R 1和R 2如上所定义，A代表保护基 - 用丙烯酸C 1-4酯; 环化得到的式（IV）化合物 - 其中R 1和R 2如上所定义，R 3代表C 1-4烷基，A代表保护基 - 除去-COOR 3基团和通式（V）的酮基的A保护基 - 其中R 1和R 2如上所定义，R 3代表C 1-4烷基，A代表保护基 - ， - 任选不分离通式（IV）和/或（V）和/或（VI）的化合物。

14. 发明申请

WO0076994A2 PROCESS FOR THE PREPARATION OF FUMAGILLIN 审中-公开
标题翻译：制备FUMAGILLIN的方法
公开(公告)号：WO0076994A2
公开(公告)日：2000-12-21
申请号：PCT/HU0000054
申请日：2000-06-06
申请人： SANOFI SYNTHELABO , FARKAS GYULA , GYOERBIRO ANDREA , HERMECZ ISTVAN , SIMON KALMAN , SZABO ANNA , VASVARI ARPADNE
发明人： FARKAS GYULA , GYOERBIRO ANDREA , HERMECZ ISTVAN , SIMON KALMAN , SZABO ANNA , VASVARI ARPADNE
IPC分类号： C07D303/22 , C07D407/00
CPC分类号： C07D303/22
摘要： The invention relates to a process for the preparation of Fumagillin by liberation from its salt characterized by reacting Fumagillin dicyclohexylamine salt with an organic acid in alcoholic medium. According to the process Fumagillin can be produced in high yield and pure condition and with higher stability than products obtained by other preparation methods.
摘要翻译：本发明涉及一种通过从其盐中释放制备烟曲霉素的方法，其特征在于使富马青霉素二环己胺盐与醇介质中的有机酸反应。根据该方法，富马林可以以高产率和纯度的条件生产，并且具有比通过其它制备方法获得的产品更高的稳定性。

15. 发明专利

CA1294968C QUINOLINE CARBOXYLIC ACID BORIC ACID ANHYDRIDES AND PROCESS FOR THE PREPARATION THEREOF 未知
公开(公告)号：CA1294968C
公开(公告)日：1992-01-28
申请号：CA563463
申请日：1988-04-07
申请人： HERMECZ ISTVAN
发明人： HERMECZ ISTVAN , KERESZTURI GEZA , VASVARI LELLE , HORVATH AGNES , BALOGH MARIA , RITLI PETER , SIPOS JUDIT , PAJOR ANIKO , MARMAROSI KATALIN
IPC分类号： C07D215/56 , A61K31/47 , A61P31/04 , C07D215/16 , C07D215/54 , C07F5/00 , C07F5/02 , C07F5/04
摘要： The invention relates to new quinoline-3-carboxylic acid anhydrides of the general Formula I /I/ /wherein R stands for cyclopropyl, a group of the general Formula -CH2CR5R6R7 /wherein R5, R6 and R7 stand for hydrogen or halogen/7 or phenyl optionally substituted by 1 or 2 halogen, R1 and R2 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, R3 stands for chlorine or fluorine and R4 stands for hydrogen or fluorine/ and to the process for the preparation thereof which comprises reacting a compound of the general Formula II /II/ - 2 - 23305-1126 ¢wherein R, R3 and R4 are the same as stated above, R8 stands for hydrogen or alkyl containing 1 to 4 carbon atoms! with a compound of the Formula III HBF4 ¢III! or a borone derivative of the general Formula BX3 ¢IV! ¢wherein X stands for fluorine, chlorine or bromine! or an ether complex thereof, or a triacyloxy borate derivative of the general Formula V -B(OCOR9)3 ¢V! ¢wherein R9 stands for alkyl containing 1 to 5 carbon atoms optionally substituted by halogen, or aryl containing 6 to 10 carbon atoms!. The compounds of the general Formula I are new intermediates for the preparation of known quinoline-3-carboxylic acids showing antibacterial activity.

16. 发明专利

CA1325010C PROCESS FOR THE PREPARATION OF QUINOLINE CARBOXYLIC ACID DERIVATIVES 未知
公开(公告)号：CA1325010C
公开(公告)日：1993-12-07
申请号：CA570183
申请日：1988-06-23
申请人： HERMECZ ISTVAN
发明人： HERMECZ ISTVAN , KERESZTURI GEZA , VASVARI LELLE , HORVATH AGNES , BALOGH MARIA , RITLI PETER , SIPOS JUDIT , PAJOR ANIKO
IPC分类号： C07D215/56 , C07F5/02 , C07D401/04
摘要： The invention relates to a new process for the preperation of compounds of the general Formula I (I) (wherein R1 stands for phenyl being optionally substituted by 1 or 2 halogen atoms, or a group of the general Formula CH2CR6R7R8 (wherein R6, R7 and R8 stand for hydrogen or halogen); R2 stands for piperazinyl or 4-methyl-piperazinyl; R3 stands for hydrogen or fluorine) and pharmaceutically acceptable salts thereof which comprises reacting a compound of the general Formula II (II) (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, R4 stands for fluorine or chlorine with a piperazine derivative of the general Formula III (III) (wherein R5 stands for hydrogen or methyl) or a salt thereof and subjecting the compound of the general Formula IV (IV) thus obtained (wherein R, R1, R2 and R3 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 process 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.

17. 发明专利

CA1294621C PROCESS FOR THE PREPARATION OF 1-METHYLAMINO- QUINOLINE-CARBOXYLIC ACID DERIVATIVES 未知
公开(公告)号：CA1294621C
公开(公告)日：1992-01-21
申请号：CA524727
申请日：1986-12-08
申请人： HERMECZ ISTVAN
发明人： HERMECZ ISTVAN , KERESZTURI GEZA , VASVARI LELLE , HORVATH AGNES , BALOGH MARIA , KOVACS GABOR , SZUETS TAMAS , RITLI PETER , SIPOS JUDIT , PAJOR ANIKO
IPC分类号： C07D401/02 , A61K31/47 , C07D20060101 , C07D215/00 , C07D215/56 , C07D215/58 , C07D401/00 , C07D401/04 , C07D401/10 , C07D403/04 , C07D403/10 , C07F5/02
摘要： The present invention relates to a process for the preparation of compounds of the general Formula I /I/ and pharmaceutically acceptable salts thereof (wherein R stands for piperazinyl or 4-methyl-piperazinyl) which comprises reacting a compound of the general Formula II /II/ (wherein R1 and R2 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 /III/ (wherein R3 represents hydrogen or methyl) or a salt thereof, hydrolysing the compound of the general formula IV /IV/ thus obtained (wherein R, R1 and R2 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.

18. 发明专利

CS238901B1 PROCESSING OF 4-OXO-4H-PYRIDO/1,2-A/PYRIMIDINE DERIVATIVES 未知
公开(公告)号：CS238901B1
公开(公告)日：1985-12-16
申请号：CS541778
申请日：1978-08-18
申请人： KNOLL JOUZSEF , MESZAROS ZOLTAN , HERMECZ ISTVAN , FUELOEP FERENC , BERNATH GABOR , VIRAG SANDOR , NAGY GABOR , SZENTMIKLOSI PETER
发明人： KNOLL JOUZSEF , MESZAROS ZOLTAN , HERMECZ ISTVAN , FUELOEP FERENC , BERNATH GABOR , VIRAG SANDOR , NAGY GABOR , SZENTMIKLOSI PETER
IPC分类号： A61K31/505 , A61K31/519 , A61P25/04 , A61P29/00 , C07D471/04
摘要： Compounds of the formula or pharmaceutically acceptable acid-addition or quaternart ammonium salts thereof wherein R is hydroxy, carboxy, lower alkoxycarbonyl, benzyloxycarbonyl, phenoxycarbonyl, carbamoyl, N-loweralkyl-carbamoyl, N,N-dilower-alkyl-carbamoyl, carboazido, carbohydrazido or cyano; R2 is C1 to C6 alkyl; R3 is C1 to C6 alkyl or benzyl; and R4 is a single electron pair, hydrogen or lower alkyl; and the dotted lines represent saturated or unsaturated bonds, are disclosed with analgesic properties.

19. 发明专利

CA1284800C ANHYDRIDES OF 1-ETHYL-6-FLUORO-7-CHLORO-4-OXO-1,4- DIHYDROQUINOLINE-3-CARBOXYLIC ACIDS AND BORIC ACIDS 未知
公开(公告)号：CA1284800C
公开(公告)日：1991-06-11
申请号：CA524725
申请日：1986-12-08
申请人： HERMECZ ISTVAN
发明人： HERMECZ ISTVAN , KERESZTURI GEZA , VASVARI LELLE , HORVATH AGNES , BALOGH MARIA , KOVACS GABOR , MESZAROS ZOLTAN , RITLI PETER , SIPOS JUDIT , PAJOR ANIKO
IPC分类号： C07F5/02 , C07D215/56 , C07F5/00 , C07F5/04
摘要： The invention relates to a process for the preparation of compounds of the general formula I /I/ (wherein R and R1 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 /II/ (wherein R2 stands for hydrogen or alkyl comprising 1-4 carbon atoms) with a borone derivative of the general Formula III /III/ (wherein R3, R4 and R5 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.

20. 发明专利

CS240351B1 METHOD OF PIRIMIDINE TRICYCLIC DERIVATIVES PRODUCTION 未知
公开(公告)号：CS240351B1
公开(公告)日：1986-02-13
申请号：CS541878
申请日：1978-08-18
申请人： HERMECZ ISTVAN , FUELOEP FERENC , MESZAROS ZOLTAN , BERNATH GABOR , KNOLL JOZSEF
发明人： HERMECZ ISTVAN , FUELOEP FERENC , MESZAROS ZOLTAN , BERNATH GABOR , KNOLL JOZSEF
IPC分类号： A61K31/505 , A61K31/517 , A61K31/55 , A61P7/02 , A61P9/10 , A61P11/00 , A61P25/04 , A61P29/00 , A61P31/04 , A61P43/00 , C07D471/04 , C07D487/04
摘要： Pharmaceutical intermediates, morphine potentiators and other compounds have the formula wherein R is hydrogen, halogen, C1-4 alkyl, hydroxy, nitro, amino, carboxy or a carboxylic acid derivate radical, R1 is hydrogen or a C1-4 alkyl, R2 is hydrogen or C1-4 alkyl, R3 is hydrogen, R4 is hydrogen or C1-4 alkyl, R5 is hydrogen R6 is hydrogen or R3 and R4 and/or R5 and R6 form a chemical bond, X is oxygen or imino, m is 1, 2, 3 or 4, n is 0, 1, 2 or 3, and if n is 1, then the dotted lines can stand for bonds, with the proviso that if m=1 and n=1 and if in the 2,3-, 6,7-, 8,9- and 1,10-positions double bonds are present, and R1 and R2 are hydrogen, then R is other than 9-hydroxy or 9-methyl; if m=2 and n=1 and R2 is hydrogen, then at least one of R and R1 is other than hydrogen; and if m=2 and n=2 and R2 is hydrogen and the molecule is a 2,3,4,6,7,8,9,10-octahydro derivative, then at least one of R and R1 is other than hydrogen or an acid-addition or quaternary salt thereof.

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