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1. 发明专利

CA2130723C PROCESS FOR PREPARING Y-MERCAPTOCARBOXYLIC ACID DERIVATIVES 未知
公开(公告)号：CA2130723C
公开(公告)日：2006-01-31
申请号：CA2130723
申请日：1994-08-23
申请人： QUITTMANN WILHELM , MCGARRITY JOHN
发明人： QUITTMANN WILHELM , MCGARRITY JOHN
IPC分类号： C07D333/78 , C07C319/02 , C07C323/51 , C07C323/52 , C07C323/53 , C07C323/60 , C07D333/32 , C07D333/38 , C07D333/50
摘要： .gamma.-Mercaptocarboxylic acids and their derivatives, in particular esters and amides, are prepared from .gamma.- butyrolactones via the corresponding thiolactones. The thiolactones are obtained by reaction of the lactones with thiocarboxylates in polar solvents and are converted into the .gamma.-mercaptocarboxylic acid derivatives by ring opening using nucleophilic reagents such as, for example, alkali metal alkoxides. The products are intermediates, for example for the synthesis of leucotriene antagonists.

2. 发明专利

CA1322756C IMIDAZOLE DERIVATIVES AND A PROCESS FOR THEIR PRODUCTION 未知
公开(公告)号：CA1322756C
公开(公告)日：1993-10-05
申请号：CA553241
申请日：1987-12-01
申请人： MCGARRITY JOHN
发明人： MCGARRITY JOHN , TENUD LEANDER , MEUL THOMAS
IPC分类号： C07D491/04 , C07D491/048 , C07D495/04 , C07F7/10
摘要： IMIDAZOLE DERIVATIVES AND A PROCESS FOR THEIR PRODUCTION Imidazole derivatives and a process for their production. The derivatives have the formula: IX wherein R1 is an (R)- or (S)-1-phenylalkyl group, an (R)or (S)-1-alkoxycarbonyl-1-phenylmethyl group or an (R)- or (S)-1-aryloxycarbonyl-1-phenylmethyl group, R2 is hydrogen, a substituted or unsubstituted alkanoyl group, and unsubstituted or a substituted benzoyl group, a substituted or an unsubstituted benzyl group, an alkoxycarbonyl group, and aryloxycarbonyl group, an alkoxyalkyl group, a pyranyl group, a substituted or unsubstituted benzenesulfonyl group, an alkylsulfonyl group, a diarylphosphinyl group, a dialkoxyphosphinyl group or a trialkylsilyl group, and A is a sulfur or oxygen atom. The derivatives are suitable particularly as intermediate products for the production of (+) biotin.

3. 发明专利

CA2055378A1 PROCESS FOR THE PRODUCTION OF 4-HYDROXY-2-OXOPYRROLIDIN-1-YL-ACETAMIDE 未知
公开(公告)号：CA2055378A1
公开(公告)日：1993-05-14
申请号：CA2055378
申请日：1991-11-13
申请人： LAFFAN DAVID , BANZIGER MARKUS , MCGARRITY JOHN , LONZA AG
发明人： LAFFAN DAVID , BANZIGER MARKUS , MCGARRITY JOHN
IPC分类号： A61K31/40 , A61K31/4015 , A61P25/00 , B01J23/46 , C07B61/00 , C07D207/26 , C07D207/273 , C07D207/38
摘要： A process is disclosed for the production of 4hydroxy-2-oxopyrrolidin-1-yl-acetamide, which is a cerebrally active pharmaceutical agent. A 4-halo-3-alkoxy-butenoic acid ester is reacted with glycine to form a novel intermediate product of the formula: (II) wherein R represents lower alkyl. The compound II is subjected to acid hydrolysis of the alkoxy group, subsequent hydrogenation, esterification of the carboxyl function and finally conversion to the desired end product by reaction with ammonia.

4. 发明专利

CA2130723A1 PROCESS FOR PREPARING Y-MERCAPTOCARBOXYLIC ACID DERIVATIVES 未知
公开(公告)号：CA2130723A1
公开(公告)日：1995-03-04
申请号：CA2130723
申请日：1994-08-23
申请人： QUITTMANN WILHELM , MCGARRITY JOHN
发明人： QUITTMANN WILHELM , MCGARRITY JOHN
IPC分类号： C07C319/02 , C07C323/51 , C07C323/52 , C07C323/53 , C07C323/60 , C07D333/32 , C07D333/38 , C07D333/50 , C07D333/78
摘要： .gamma.-Mercaptocarboxylic acids and their derivatives, in particular esters and amides, are prepared from .gamma.butyrolactones via the corresponding thiolactones. The thiolactones are obtained by reaction of the lactones with thiocarboxylates in polar solvents and are converted into the .gamma.-mercaptocarboxylic acid derivatives by ring opening using nucleophilic reagents such as, for example, alkali metal alkoxides. The products are intermediates, for example for the synthesis of leucotriene antagonists.

5. 发明专利

CA2122511A1 ASYMMETRIC HYDROGENATION OF FUROIMIDAZOLE DERIVATIVES 未知
公开(公告)号：CA2122511A1
公开(公告)日：1994-11-15
申请号：CA2122511
申请日：1994-04-29
申请人： MCGARRITY JOHN , SPINDLER FELIX , FUCHS RUDOLF , EYER MARTIN
发明人： MCGARRITY JOHN , SPINDLER FELIX , FUCHS RUDOLF , EYER MARTIN
IPC分类号： B01J31/24 , C07B53/00 , C07B61/00 , C07D491/04 , C07D491/048
摘要： A novel process for the asymmetric hydrogenation of a furoimidazole derivative of the general formula: I with hydrogen in the presence of a homogeneous catalyst to produce the corresponding diastereomeric dihydrofuroimidazole derivative of the general formula: II is described. Dihydrofuroimidazole derivatives of the general formula II are intermediates for the preparation of the vitamin (+)-biotin.

6. 发明专利

CA2076580A1 PROCESS FOR THE PRODUCTION OF OPTICALLY-ACTIVE 4-AMINO-3-HYDROXYCARBOXYLIC ACIDS 未知
公开(公告)号：CA2076580A1
公开(公告)日：1993-02-23
申请号：CA2076580
申请日：1992-08-21
申请人： BANZIGER MARKUS , MCGARRITY JOHN , MEUL THOMAS
发明人： BANZIGER MARKUS , MCGARRITY JOHN , MEUL THOMAS
IPC分类号： C07D207/273 , C12P13/00 , C12P41/00
摘要： A process is disclosed for the production of optically-active 4-amino-3-hydroxy-carboxylic acids in the (rel-3R,4R) configuration, especially statine, starting from 5-alkylidene or 5-benzylidenetetramic acid. The synthesis process includes the 0-acylation of the tetramic acid to form the corresponding 4-acyloxy-3-pyrrolin-2-one, a stereoselective hydrogenation to produce (rel-4R,5R)-4-acyloxy-5-alkyl or 5-benzylpyrrolidin-2-one and an enantioselective enzymatic hydrolysis of the (4R,5R)enantiomer to form the corresponding 4-hydroxypyrrolidin-2-one. The nonhydrolyzed enantiomer is separated and converted into the target compound with (3S,4S) configuration by hydrolytic cleavage of the lactam ring and the ester function and optional introduction of an amino protecting group. Analogously, the (3R,4R)-enantiomer can be obtained from the 4-hydroxypyrrolidin-2-one from the enzymatic hydrolysis. The 4-amino-3-hydroxycarboxylic acids produced by the process of the invention are the structural elements of enzyme inhibitors.

7. 发明申请

WO2009010231A1 PROCESS FOR THE PRODUCTION OF TERTIARY ALCOHOLS 审中-公开
标题翻译：生产醇类的方法
公开(公告)号：WO2009010231A1
公开(公告)日：2009-01-22
申请号：PCT/EP2008/005638
申请日：2008-07-10
申请人： LONZA LTD , McGARRITY, John , DJOJO, Francis
发明人： McGARRITY, John , DJOJO, Francis
IPC分类号： C07B49/00 , C07C29/147 , C07D215/18 , C07C31/135 , C07C31/12
CPC分类号： C07B49/00
摘要： Tertiary alcohols are prepared by reacting carboxylic esters with Grignard reagents in ethereal solvents in the presence of lanthanum trichloride and lithium chloride. The method is particularly suitable for the production of (α S )-α-[3-[(1 E )-2-(7-chloro-2-quino- linyl)ethenyl]phenyl]-2-(1-hydroxy-1-methylethyl)benzenepropanol of formula (A) which is an intermediate in the production of montelukast.
摘要翻译：在三氯化镧和氯化锂的存在下，在醚溶剂中使羧酸酯与格氏试剂反应制备叔醇。该方法特别适用于制备（aS）-α-[3 - [（1E）-2-（7-氯-2-喹啉基）乙烯基]苯基] -2-（1-羟基-1- （A）的甲基乙基）苯丙醇，其是孟鲁司特生产中的中间体。

8. 发明申请

WO2006087166A1 PROCESS FOR THE PREPARATION OF ENANTIOMERICALLY PURE 1-SUBSTITUTED-3-AMINOALCOHOLS 审中-公开
标题翻译：制备纯化1-取代的3-氨基醇的方法
公开(公告)号：WO2006087166A1
公开(公告)日：2006-08-24
申请号：PCT/EP2006/001334
申请日：2006-02-14
申请人： LONZA AG , BRIEDEN, Walter , CLAUSEN, Martin , McGARRITY, John , METTLER, Hanspeter , MICHEL, Dominique
发明人： BRIEDEN, Walter , CLAUSEN, Martin , McGARRITY, John , METTLER, Hanspeter , MICHEL, Dominique
IPC分类号： C07C213/08 , C07C215/30 , C07C221/00 , C07C225/16 , C07C303/22 , C07C309/04 , C07C309/07 , C07C309/30 , C07D333/20
CPC分类号： C07C303/22 , C07B2200/07 , C07C213/02 , C07C221/00 , C07C309/04 , C07C309/07 , C07C309/30 , C07C215/30 , C07C225/16
摘要： Provided is a process for the preparation of N -monosubstituted β-aminoalcohol sulfonates of formula (Ia), (Ib) wherein R 1 is C 6-20 aryl or C 4-12 heteroaryl, each optionally being substituted with one or more halogen atoms and/or one or more C 1-4 alkyl or C 1-4 alkoxy groups, R 2 is C 1-4 -alkyl or C 6-20 aryl, each aryl optionally being substituted with one or more halogen atoms and/or one or more C 1-4 -alkyl or C 1-4 -alkoxy groups, and wherein R 3 is selected from the group consisting of C 1-18 alkyl, C 6-20 cycloalkyl, C 6-20 aryl and C 7-20 aralkyl residues, comprising the steps of a) reacting a methyl ketone, a primary amine, formaldehyde and a sulfonic acid, at a pressure above 1.5 bar, optionally in a organic solvent, said organic solvent optionally containing water, to afford N -monosubstituted β-aminoketone sulfonates of formula (II), wherein R 1 , R 2 and R 3 are as defined above, and b) asymmetrically hydrogenating said sulfonates in the presence of a base and a catalyst, comprising a transition metal and a diphosphine ligand, in a polar solvent, optionally in the presence of water.
摘要翻译：提供了制备式（Ia），（Ib）的N-单取代的β-氨基醇磺酸盐的方法，其中R 1为C 6-20芳基或C 1〜每个任选被一个或多个卤素原子和/或一个或多个C 1-4烷基或C 1-4烷基取代的杂芳基 >烷氧基，R 2是C 1-4 - 烷基或C 6-20-20芳基，每个芳基任选被一个或多个卤素原子和/或一个或多个C 1-4 - 烷基或C 1-4 - 烷氧基，并且其中R 3选自由C 1-18烷基，C 6-20环烷基，C 6-20芳基和C 7-20芳基组成的组中，包括以下步骤：a）使甲基酮，伯胺，甲醛和磺酸在高于1.5巴的压力下，任选地在有机溶剂中，任选地含有水的所述有机溶剂与得到形式的N-单取代的β-氨基酮磺酸盐其中R 1，R 2，R 3和R 3如上所定义，并且b）在存在下不对称地氢化所述磺酸盐的碱和催化剂，其包含过渡金属和二膦配体，在极性溶剂中，任选地在水的存在下。

9. 发明申请

WO1997008152A1 METHOD OF PRODUCING DIHYDROXYPYRIMIDINE DERIVATIVES 审中-公开
标题翻译：用于生产羟基嘧啶衍生物
公开(公告)号：WO1997008152A1
公开(公告)日：1997-03-06
申请号：PCT/EP1996003826
申请日：1996-08-30
申请人： LONZA AG , SCHMIDT, Beat , KIENER, Andreas , McGARRITY, John
发明人： LONZA AG
IPC分类号： C07D239/54
CPC分类号： C07D239/54 , C12P13/02
摘要： The invention concerns a novel method of producing dihydroxypyrimidine derivatives of general formula (I), in which R and R are identical or different and designate a hydrogen atom, a C1 - C4 alkyl group or an aryl group. In the first step, as a substrate, a compound of general formula (II), in which R has the above meaning and R designates -CN or COOR , R being a C1 - C4 alkyl group, is converted by microorganisms of the Rhodococcus species into a malonic acid derivative of general formula (III), in which R has the above meaning and R designates a C1 - C4 alkoxy group or -NH2, and this derivative is then cyclized in the second step with a carboxylic acid amide of general formula (IV), in which R has the above meaning, in the presence of a base to form an end product according to formula (I).
摘要翻译：用于制造（I）式中，R <1>和R <2>是相同的或不同的，是氢原子，C1-C4烷基或芳基进行说明通式羟基嘧啶衍生物的新方法。这里，在第一阶段中作为底物的一般式的化合物（II），其中R <2>如上且R <3>是-CN或COOR <4>，其中R <4>是一个C1-C4定义烷基，在由属的微生物的手段通式的丙二酸衍生物红球菌（III）其中R <2>如上所定义并且R <5>装置实现的C1-C4烷氧基或-NH 2，这然后在第二阶段与通式（IV）其中，R <1>具有给出的含义，在碱的存在下环化式（I），得到最终产物的羧酸酰胺。

10. 发明申请

WO2009010230A3 PROCESS AND INTERMEDIATE FOR THE PRODUCTION OF A TERTIARY ALCOHOL AS AN INTERMEDIATE IN THE SYNTHESIS OF MONTELUKAST 审中-公开
标题翻译：在MONTELUKAST合成中作为中间体生产季铵盐的方法和中间体
公开(公告)号：WO2009010230A3
公开(公告)日：2009-04-23
申请号：PCT/EP2008005637
申请日：2008-07-10
申请人： LONZA AG , MCGARRITY JOHN , DJOJO FRANCIS
发明人： MCGARRITY JOHN , DJOJO FRANCIS
IPC分类号： C07D215/18 , C07D405/10
CPC分类号： C07D405/10 , C07D215/18
摘要： The tertiary alcohol a-[3-[(1E)-2-(7-chloro-2-quinolinyl)ethenyl]phenyl]-2-(1-hydroxy- 1-methylethyl)benzenepropanol, the (aS)-enantioner of which is an intermediate in the production of montelukast, is produced by reacting the novel lactone of formula (II) with a methylmagnesium halide in an ethereal solvent in the presence of lanthanum trichloride and lithium chloride. The lactone II can be prepared by reacting a corresponding hydroxyester with a Grignard reagent in the absence of a lanthanoid compound or with a strong base.
摘要翻译：叔醇a- [3 - [（1E）-2-（7-氯-2-喹啉基）乙烯基]苯基] -2-（1-羟基-1-甲基乙基）苯丙醇，（aS） - 苯胺是制备孟鲁司特的中间体，是通过在三氯化镧和氯化锂的存在下，在醚溶剂中使式（II）的新型内酯与甲基卤化镁反应制备的。内酯II可以通过在不存在镧系元素化合物或强碱的情况下使相应的羟基酯与格氏试剂反应来制备。

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