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1.发明授权INTERMEDIATES IN THE PREPARATION OF 4,5-DIFLUOROANTHRANILIC ACID 失效中间产物4,5-DIFLUOROANTHRANILSÄURE的生产。
公开(公告)号：EP0555283B1
公开(公告)日：1995-04-05
申请号：EP91918730.2
申请日：1991-07-29
申请人： PFIZER INC.
发明人： BRAISH, Tamim, F.
IPC分类号： C07C259/10 , C07C227/12 , C07C229/56 , C07D209/48
CPC分类号： C07D209/48 , C07C227/18 , C07C259/10 , C07D307/89
摘要： Compounds of formula (I), which are intermediates in the preparation of 4,5-difluoroanthranilic acid, an intermediate itself in the synthesis of quinolone antibacterials, and methods of preparing these intermediates.
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2.发明公开PROCESS FOR PREPARATION OF 1,2,4-TRIFLUOROBENZENE AND 1-CHLORO-3,4-DIFLUOROBENZENE 失效法制备1,2,4- TRIFLUOROBENZOL和1-氯-3,4-二氟苯。
公开(公告)号：EP0525019A1
公开(公告)日：1993-02-03
申请号：EP91907690.0
申请日：1991-03-22
申请人： PFIZER INC.
发明人： BRAISH, Tamim, F.
CPC分类号： C07C245/20 , C07C17/093 , C07C25/13
摘要： On prépare du 1,2,4-trifluorobenzène et du 1-chloro-3,4-difluorobenzène en faisant réagir une 2,4-difluoroaniline et une 5-chloro-2-fluoroaniline, respectivement, avec du t-butyl nitrite en présence d'un complexe d'éthérate de trifluorure de bore, après quoi on procède à la décomposition thermique des sels de diazonium obtenus 2,4-difluorophényle-diazoniumtétrafluoroborate et un fluoro-4-chloro-phényle-2-diazoniumtétrafluoroborate.
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3.发明授权PROCESS FOR PREPARING DERIVATIVES OF AZABICYCLO NAPHTHYRIDINE CARBOXYLIC ACID COMPRISING A DIPEPTIDE 失效PROCESS FOR肽衍生物的制备含AZABIZYLO萘甲酸
公开(公告)号：EP0833837B1
公开(公告)日：2002-07-31
申请号：EP96904996.4
申请日：1996-03-27
申请人： PFIZER INC.
IPC分类号： C07K1/06 , C07K5/06 , C07D471/04 , A61K31/47
CPC分类号： C07K5/06191 , Y02P20/55
摘要： A novel process for preparing a prodrug acid, viz., 7-[(1 alpha , 6 alpha , 7 alpha )-6-(L-Ala-L-Ala-amino)-3-azabicyclo[3.1.0]hex-3-yl]-6-fluoro-1-(2,4-difluorophenyl)-1,4-dihydro-4-oxo-1,8-naphthyridine-3-carboxylic acid, in the form of a pharmaceutically acceptable acid addition salt, is disclosed, which involves (1) treating an N-protected 7-[(1 alpha , 5 alpha , 6 alpha )-6-amino-3-azabicyclo[3.1.0]hex-3-yl]-6-fluoro-1-(2,4-difluorophenyl)-1,4-dihydro-4-oxo-1,8-naphthyridine-3-carboxylic acid C1-C4 alkyl ester, wherein the nitrogen-protecting group is benzyloxycarbonyl, C1-C4 alkoxycarbonyl or C1-C4 alkanoyl, with a strongly-protic acid to selectively remove the N-protecting group; (2) then condensing the resulting free amino ester compound with an N-protected L-alanyl-L-alanine dipeptide compound, wherein the N-protecting group is as previously defined, in the presence of a standard dehydrating agent to form the corresponding N-protected prodrug ester compound as the desired condensation product; and (3) thereafter hydrolyzing the intermediate N-protected prodrug ester in the presence of a pharmaceutically-acceptable strong acid to convert said N-protected prodrug ester to the desired naphthyridinone L-Ala-L-Ala prodrug acid final product, in the form of the corresponding pharmaceutically acceptable acid addition salt, indicated above. The latter prodrug acid final product is especially useful in the form of the corresponding methanesulfonic acid addition salt, which serves as a water-soluble prodrug companion to a known antibacterial agent, viz., 7-[(1 alpha , 5 alpha , 6 alpha )-6-amino-3-azabicyclo[3.1.0]hex-3-yl]-6-fluoro-1-(2,4-difluorophenyl)-1,4-dihydro-4-oxo-1-naphthyridine-3-carboxylic acid.
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4.发明公开PROCESS AND INTERMEDIATES FOR PREPARING NAPHTHYRIDONECARBOXYLIC ACID SALTS 失效过程和中间产品用于制备naphthyridonecarboxylic酸盐
公开(公告)号：EP0740667A1
公开(公告)日：1996-11-06
申请号：EP95901569.0
申请日：1994-12-12
申请人： PFIZER INC.
CPC分类号： C07D471/04
摘要： This invention relates to novel processes for preparing compounds of formula (I), wherein R1H is as defined below, which is a salt of the naphthyridone antibiotic 7-(1α,5α,6α)-(6-amino-3-azabicyclo[3.1.0]hex-3-yl)-1-(2,4-difluorophenyl)-6-fluoro-1,4-dihydro-4-oxo-1,8-naphthyridine-3-carbocylic acid and a pharmaceutically acceptable acid. The salt and antibiotics have antibacterial activity. This invention also relates to novel intermediates, and processes for their preparation, of formulae (IV), (IIIB) or (IIIA). The compounds of formulae (IIIA), (IIIB) and (IV) are useful as intermediates in the syntheses of the azabicyclo naphthyridone carboxylic acid alkanesulfonic acid salts of formula (I).
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公开(公告)号：EP0575507B1
公开(公告)日：1996-01-31
申请号：EP92908491.1
申请日：1992-02-07
申请人： PFIZER INC.
发明人： BRAISH, Tamim, F.
IPC分类号： C07C211/38 , C07C209/68
CPC分类号： C07C209/68 , C07C211/38 , C07C2602/10 , Y02P20/582
摘要： A novel process for converting trans-isomeric N-methyl-4-(3,4-dichlorophenyl)-1,2,3,4-tetrahydro-1-naphthaleneamine to cis-isomeric N-methyl-4-(3,4-dichlorophenyl)-1,2,3,4-tetrahydro-1-naphthaleneamine is disclosed. The process involves contacting trans-isomeric N-methyl-4-(3,4-dichlorophenyl)-1,2,3,4-tetrahydro-1-naphthaleneamine, or a mixture of same with up to about an equal part by weight of the corresponding cis-isomer, with a basic equilibration agent like potassium tert.-butoxide in a reaction-inert polar organic solvent to ultimately afford a cis/trans-mixture wherein the amount of cis-amine present in said mixture achieves a constant value of about 2:1 on a weight-by-weight basis. The aforesaid resultant mixture is useful as an intermediate product that ultimately leads to pure cis-(1S)(4S)-N-methyl-4-(3,4-dichlorophenyl)-1,2,3,4-tetrahydro-1-naphthaleneamine (sertraline), which is a known antidepressant agent.
摘要翻译： 将反式异构体N-甲基-4-（3,4-二氯苯基）-1,2,3,4-四氢-1-萘胺转化成顺式异构体N-甲基-4-（3,4-二氯苯基） 二氯苯基）-1,2,3,4-四氢-1-萘胺。 该方法包括将反式异构体N-甲基-4-（3,4-二氯苯基）-1,2,3,4-四氢-1-萘胺或其混合物与最多约等于重量份的 相应的顺式异构体与碱性平衡剂如叔丁醇钾在反应惰性极性有机溶剂中反应，最终得到顺式/反式混合物，其中存在于所述混合物中的顺式胺的量达到恒定值 约2：1。 上述所得混合物可用作最终导致纯的顺式 - （1S）（4S）-N-甲基-4-（3,4-二氯苯基）-1,2,3,4-四氢-1- 萘胺（舍曲林）是已知的抗抑郁药。
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公开(公告)号：EP0629189B1
公开(公告)日：1997-08-06
申请号：EP93902893.2
申请日：1993-01-07
申请人： PFIZER INC.
发明人： BRAISH, Tamim, F.
IPC分类号： C07D209/52
CPC分类号： C07D209/52
摘要： This invention relates to novel processes for preparing compounds of formulae (III) and (VII) wherein R and X defined as below. Compounds of the formulae (VII) are useful as intermediates in the syntheses of azabicyclo quinoline carboxylic acids having antibacterial activity. This invention also relates to certain novel intermediates in the syntheses such antibiotics.
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7.发明公开
公开(公告)号：EP0629189A1
公开(公告)日：1994-12-21
申请号：EP93902893.0
申请日：1993-01-07
申请人： PFIZER INC.
发明人： BRAISH, Tamim, F.
CPC分类号： C07D209/52
摘要： L'invention se rapporte à de nouveaux procédés conçus pour préparer des composés des formules (III) et (VII), dans lesquelles R et X sont tels que définis dans l'invention. Des composés de la formule (VII) sont utiles comme intermédiaires dans les synthèses d'acides carboxyliques de quinoline azabicyclo possédant une activité antibactérienne. Cette invention se rapport également à certains nouveaux intermédiaires dans les synthèses de ces antibiotiques.
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8.发明公开INTERMEDIATES IN THE PREPARATION OF 4,5-DIFLUOROANTHRANILIC ACID 失效中间产物4,5-DIFLUOROANTHRANILSÄURE的生产。
公开(公告)号：EP0555283A1
公开(公告)日：1993-08-18
申请号：EP91918730.0
申请日：1991-07-29
申请人： PFIZER INC.
发明人： BRAISH, Tamim, F.
CPC分类号： C07D209/48 , C07C227/18 , C07C259/10 , C07D307/89
摘要： Cette invention concerne des composés correspondant à la formule (I) qui sont des intermédiaires dans la préparation d'acide 4,5-difluoroanthranilique, lui-même étant un intermédiaire dans la synthèse des agents antibactériens à la quinolone, et des procédés de préparation de ces intermédiaires.
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9.发明公开PROCESS FOR PREPARING DERIVATIVES OF AZABICYCLO NAPHTHYRIDINE CARBOXYLIC ACID COMPRISING A DIPEPTIDE 失效PROCESS FOR AZABIZYLO-CHIDIN炭酸的衍生物的制备含二肽
公开(公告)号：EP0833837A1
公开(公告)日：1998-04-08
申请号：EP96904996.0
申请日：1996-03-27
申请人： PFIZER INC.
CPC分类号： C07K5/06191 , Y02P20/55
摘要： A novel process for preparing a prodrug acid, viz., 7-[(1α, 6α, 7α)-6-(L-Ala-L-Ala-amino)-3-azabicyclo[3.1.0]hex-3-yl]-6-fluoro-1-(2,4-difluorophenyl)-1,4-dihydro-4-oxo-1,8-naphthyridine-3-carboxylic acid, in the form of a pharmaceutically acceptable acid addition salt, is disclosed, which involves (1) treating an N-protected 7-[(1α, 5α, 6α)-6-amino-3-azabicyclo[3.1.0]hex-3-yl]-6-fluoro-1-(2,4-difluorophenyl)-1,4-dihydro-4-oxo-1,8-naphthyridine-3-carboxylic acid C1-C4 alkyl ester, wherein the nitrogen-protecting group is benzyloxycarbonyl, C1-C4 alkoxycarbonyl or C1-C4 alkanoyl, with a strongly-protic acid to selectively remove the N-protecting group; (2) then condensing the resulting free amino ester compound with an N-protected L-alanyl-L-alanine dipeptide compound, wherein the N-protecting group is as previously defined, in the presence of a standard dehydrating agent to form the corresponding N-protected prodrug ester compound as the desired condensation product; and (3) thereafter hydrolyzing the intermediate N-protected prodrug ester in the presence of a pharmaceutically-acceptable strong acid to convert said N-protected prodrug ester to the desired naphthyridinone L-Ala-L-Ala prodrug acid final product, in the form of the corresponding pharmaceutically acceptable acid addition salt, indicated above. The latter prodrug acid final product is especially useful in the form of the corresponding methanesulfonic acid addition salt, which serves as a water-soluble prodrug companion to a known antibacterial agent, viz., 7-[(1α, 5α, 6α)-6-amino-3-azabicyclo[3.1.0]hex-3-yl]-6-fluoro-1-(2,4-difluorophenyl)-1,4-dihydro-4-oxo-1-naphthyridine-3-carboxylic acid.
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公开(公告)号：EP0575507A1
公开(公告)日：1993-12-29
申请号：EP92908491.0
申请日：1992-02-07
申请人： PFIZER INC.
发明人： BRAISH, Tamim, F.
CPC分类号： C07C209/68 , C07C211/38 , C07C2602/10 , Y02P20/582
摘要： L'invention décrit un nouveau procédé de conversion de trans-isomère N-méthyle-4-3,4-dichlorophényle-1,2,3,4-tétrahydro-1-naphtalèneamine en cis-isomère-N-méthyle-4-3,4-dichlorophényle-1,2,3,4-tétrahydro-1-naphthalèneamine. Le procédé comprend la mise en contact de trans-isomère-N-méthyle-4-3,4-dichlorophényle-1,2,3,4-tétrahydro-1-naphtalèneamine, ou un mélange dudit composé, avec au maximum une part égale en poids du cis-isomère correspondant, avec un agent d'équilibrage basique tel qu'un tert.-butoxyde de potassium dans un solvant polaire organique inerte, afin d'obtenir un mélange cis/trans dans lequel la quantité de cis-amine présente dans ledit mélange atteint une valeur constante d'environ 2:1 selon un rapport poids sur poids. Le mélange obtenu s'utilise comme produit intermédiaire d'obtention finale d'un composé pur de cis-1S-4S-N-méthyle-4-3,4-dichlorophényle-1,2,3,4-tétrahydro-1-naphthalèneamine (sertraline) qui est un agent antidépresseur connu.
摘要翻译： 将反式异构体N-甲基-4-（3,4-二氯苯基）-1,2,3,4-四氢-1-萘胺转化成顺式异构体N-甲基-4-（3,4-二氯苯基） 二氯苯基）-1,2,3,4-四氢-1-萘胺。 该方法包括将反式异构体N-甲基-4-（3,4-二氯苯基）-1,2,3,4-四氢-1-萘胺或其混合物与最多约等于重量份的 相应的顺式异构体与碱性平衡剂如叔丁醇钾在反应惰性极性有机溶剂中反应，最终得到顺式/反式混合物，其中存在于所述混合物中的顺式胺的量达到恒定值 约2：1。 上述所得混合物可用作最终导致纯的顺式 - （1S）（4S）-N-甲基-4-（3,4-二氯苯基）-1,2,3,4-四氢-1- 萘胺（舍曲林）是已知的抗抑郁药。
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