专利快速检索-快速检索全球专利，免费商用专利数据库-IPRDB

1. 发明申请

US20060177919A1 Process for the preparation of (S) - or (R) -3,3,3- trifluoro-2-hydroxy-2-methylpropionic acid 失效
标题翻译：制备（S） - 或（R）-3,3,3-三氟-2-羟基-2-甲基丙酸的方法
公开(公告)号：US20060177919A1
公开(公告)日：2006-08-10
申请号：US11200182
申请日：2005-08-10
申请人： Walter Brieden , Andrew Naughton , Karen Robins , Nicholas Shaw , Andreas Tinschert , Thomas Zimmermann
发明人： Walter Brieden , Andrew Naughton , Karen Robins , Nicholas Shaw , Andreas Tinschert , Thomas Zimmermann
IPC分类号： C12N9/80 , C12N1/21
CPC分类号： C12N1/20 , C07C235/06 , C12N9/80 , C12P7/42 , C12P13/02 , C12P41/006
摘要： The present invention relates to a novel process for the preparation of (S)— or (R)-3,3,3-trifluoro-2-hydroxy-2-methylpropionic acid and to novel microorganisms capable of utilizing the propionamide of the formula in the form of the racemate or of its optically active isomers as the sole nitrogen source.
摘要翻译：本发明涉及一种制备（S） - 或（R）-3,3,3-三氟-2-羟基-2-甲基丙酸的新方法，以及能够利用下式的丙酰胺的新型微生物外消旋体或其旋光异构体的形式作为唯一的氮源。

2. 发明授权

US07074606B2 Process for the preparation of (S) - or (R) -3,3,3-trifluoro-2-hydroxy-2-methylpropionic acid 失效
公开(公告)号：US07074606B2
公开(公告)日：2006-07-11
申请号：US10086082
申请日：2002-02-28
申请人： Walter Brieden , Andrew Naughton , Karen Robins , Nicholas Shaw , Andreas Tinschert , Thomas Zimmermann
发明人： Walter Brieden , Andrew Naughton , Karen Robins , Nicholas Shaw , Andreas Tinschert , Thomas Zimmermann
IPC分类号： C12P21/06 , C12N9/00 , C12N9/80 , C07H21/04
CPC分类号： C12N1/20 , C07C235/06 , C12N9/80 , C12P7/42 , C12P13/02 , C12P41/006
摘要： The present invention relates to a novel process for the preparation of (S)- or (R)-3,3,3-trifluoro-2-hydroxy-2-methylpropionic acid and to novel microorganisms capable of utilizing the propionamide of the formula in the form of the racemate or of its optically active isomers as the sole nitrogen source.

3. 发明授权

US07553652B2 Process for the preparation of (S)- or (R)-3,3,3-trifluoro-2-hydroxy-2-methylpropionic acid 失效
标题翻译：制备（S） - 或（R）-3,3,3-三氟-2-羟基-2-甲基丙酸的方法
公开(公告)号：US07553652B2
公开(公告)日：2009-06-30
申请号：US11200182
申请日：2005-08-10
申请人： Walter Brieden , Andrew Naughton , Karen Robins , Nicholas Shaw , Andreas Tinschert , Thomas Zimmermann
发明人： Walter Brieden , Andrew Naughton , Karen Robins , Nicholas Shaw , Andreas Tinschert , Thomas Zimmermann
IPC分类号： C12N9/80
CPC分类号： C12N1/20 , C07C235/06 , C12N9/80 , C12P7/42 , C12P13/02 , C12P41/006
摘要： The present invention relates to a novel process for the preparation of (S)— or (R)-3,3,3-trifluoro-2-hydroxy-2-methylpropionic acid and to novel microorganisms capable of utilizing the propionamide of the formula in the form of the racemate or of its optically active isomers as the sole nitrogen source.
摘要翻译：本发明涉及一种制备（S） - 或（R）-3,3,3-三氟-2-羟基-2-甲基丙酸的新方法，以及能够利用下式的丙酰胺的新型微生物外消旋体或其旋光异构体的形式作为唯一的氮源。

4. 发明授权

US06773910B1 Method of preparing (S)- or (R) -3,3,3-trifluoro-2-hydroxy-2-methylpropionic acid 失效
标题翻译：制备（S） - 或（R）-3,3,3-三氟-2-羟基-2-甲基丙酸的方法
公开(公告)号：US06773910B1
公开(公告)日：2004-08-10
申请号：US09214679
申请日：1999-12-30
申请人： Walter Brieden , Andrew Naughton , Karen Robins , Nicholas Shaw , Andreas Tinschert , Thomas Zimmermann
发明人： Walter Brieden , Andrew Naughton , Karen Robins , Nicholas Shaw , Andreas Tinschert , Thomas Zimmermann
IPC分类号： C12N100
CPC分类号： C12N1/20 , C07C235/06 , C12N9/80 , C12P7/42 , C12P13/02 , C12P41/006
摘要： Described are new micro-organisms and a new enzyme capable of using as sole source of nitrogen the propionic acid amide of formula (VI), in racemate form or as optically active isomers. Described also is a method of preparing (S)- or (R)-3,3,2-trifluoro-2-hydroxy-2-methylpropionic acid of formulas (I) and (II) starting from trifluoroaceto-acetic ester. The first three process steps are chemical, the fourth process step microbiological.
摘要翻译：描述了新的微生物和能够以外消旋形式或作为光学活性异构体使用式（VI）的丙酸酰胺作为氮源的唯一来源的新酶。还描述了由三氟乙酸 - 乙酸酯制备式（I）和（II）的（S） - 或（R）-3,3,2-三氟-2-羟基-2-甲基丙酸的方法。前三个过程步骤是化学，第四个步骤微生物。

5. 发明授权

US5789596A Process for the preparation of 1-acyl-4-arylpiperidines 失效
标题翻译： 1-酰基-4-芳基哌啶的制备方法
公开(公告)号：US5789596A
公开(公告)日：1998-08-04
申请号：US933527
申请日：1997-09-18
申请人： Walter Brieden , Didier Loetscher , Andrew Naughton
发明人： Walter Brieden , Didier Loetscher , Andrew Naughton
IPC分类号： C07D211/02 , B01J27/08 , B01J31/24 , C07B61/00 , C07D211/20 , C07D211/82
CPC分类号： C07D211/20
摘要： 1-Acyl-4-arylpiperidines of the general formula: ##STR1## wherein R.sup.1 is an aryl group optionally substituted by one or more C.sub.1-6 -alkyl groups, C.sub.1-6 -alkoxy groups, benzyloxy groups or C.sub.1-6 -alkylthio groups and/or one or more fluorine atoms, and R.sup.2 is a C.sub.1-6 -alkyl group, a C.sub.1-6 -alkoxy group, an optionally substituted aryl group, alkylaryl group or a benzyloxy group optionally substituted on the phenyl radical. The 1-acyl-4-arylpiperidines of formula I are prepared by reacting an arylmagnesium halide with a 1-acylpyridinium halide, obtainable from pyridine and an acyl halide, in the presence of a copper compound to give the corresponding 1-acyl-4-aryl-1,4-dihydropyridine, and hydrogenating the latter. The 1-acyl-4-arylpiperidines are intermediates in the synthesis of pharmaceutical active ingredients, for example, neurokinin receptor antagonists.
摘要翻译：具有以下通式的1-酰基-4-芳基哌啶：其中R 1是任选被一个或多个C 1-6 - 烷基，C 1-6 - 烷氧基，苄氧基或C 1-6 - 烷硫基任选取代的芳基基团和/或一个或多个氟原子，并且R 2是任选在苯基上被取代的C 1-6 - 烷基，C 1-6 - 烷氧基，任选取代的芳基，烷基芳基或苄氧基。式I的1-酰基-4-芳基哌啶通过在铜化合物的存在下使卤化芳基镁卤化物与可从吡啶和酰基卤获得的1-酰基吡啶鎓卤化物反应来制备，得到相应的1-酰基-4- 芳基-1,4-二氢吡啶，并将其加氢。 1-酰基-4-芳基哌啶是合成药物活性成分例如神经激肽受体拮抗剂的中间体。

6. 发明授权

US5908935A Process for the preparation of 1-Acyl-4-arylpiperidines 失效
标题翻译： 1-酰基-4-芳基哌啶的制备方法
公开(公告)号：US5908935A
公开(公告)日：1999-06-01
申请号：US80929
申请日：1998-05-19
申请人： Walter Brieden , Didier Loetscher , Andrew Naughton
发明人： Walter Brieden , Didier Loetscher , Andrew Naughton
IPC分类号： C07D211/02 , B01J27/08 , B01J31/24 , C07B61/00 , C07D211/20 , C07D211/82
CPC分类号： C07D211/20
摘要： 1-Acyl-4-arylpiperidines of the general formula: ##STR1## wherein R.sup.1 is an aryl group optionally substituted by one or more C.sub.1-6 -alkyl groups, C.sub.1-6 -alkoxy groups, benzyloxy groups or C.sub.1-6 -alkylthio groups and/or one or more fluorine atoms, and R.sup.2 is a C.sub.1-6 -alkyl group, a C.sub.1-6 -alkoxy group, an optionally substituted aryl group, alkylaryl group or a benzyloxy group optionally substituted on the phenyl radical. The 1-acyl-4-arylpiperidines of formula I are prepared by reacting an arylmagnesium halide with a 1-acylpyridinium halide, obtainable from pyridine and an acyl halide, in the presence of a copper compound to give the corresponding 1-acyl-4-aryl-1,4-dihydropyridine, and hydrogenating the latter. The 1-acyl-4-arylpiperidines are intermediates in the synthesis of pharmaceutical active ingredients, for example, neurokinin receptor antagonists.
摘要翻译：具有以下通式的1-酰基-4-芳基哌啶：其中R 1是任选被一个或多个C 1-6 - 烷基，C 1-6 - 烷氧基，苄氧基或C 1-6 - 烷硫基取代的芳基和/或一个或多个氟原子，R 2是任选在苯基上被取代的C 1-6 - 烷基，C 1-6 - 烷氧基，任选取代的芳基，烷基芳基或苄氧基。式I的1-酰基-4-芳基哌啶通过在铜化合物的存在下使卤化芳基镁卤化物与可从吡啶和酰基卤获得的1-酰基吡啶鎓卤化物反应来制备，得到相应的1-酰基-4- 芳基-1,4-二氢吡啶，并将其加氢。 1-酰基-4-芳基哌啶是合成药物活性成分例如神经激肽受体拮抗剂的中间体。

7. 发明申请

US20120316350A1 PROCESS FOR THE PREPARATION OF ENANTIOMERICALLY PURE 1-SUBSTITUTED-3-AMINOALCOHOLS 有权
标题翻译：制备纯化1-取代的3-氨基醇的方法
公开(公告)号：US20120316350A1
公开(公告)日：2012-12-13
申请号：US13560621
申请日：2012-07-27
申请人： Walter Brieden , Martin Clausen , John McGarrity , Hanspeter Mettler , Dominique Michel
发明人： Walter Brieden , Martin Clausen , John McGarrity , Hanspeter Mettler , Dominique Michel
IPC分类号： C07D333/22 , C07C309/04
CPC分类号： C07C303/22 , C07B2200/07 , C07C213/02 , C07C221/00 , C07C309/04 , C07C309/07 , C07C309/30 , C07C215/30 , C07C225/16
摘要： A process for the preparation of N-monosubstituted β-aminoalcohol sulfonates of formula (1a), (1b): wherein R1 is C6-20-aryl or C4-12-heteroaryl, each optionally being substituted with one or more halogen atoms and/or one or more C1-4-alkyl or C1-4-alkoxy groups, R2 is C1-4-alkyl or C6-20-aryl, each aryl optionally being substituted with one or more halogen atoms and/or one or more C1-4-alkyl or C1-4-alkoxy groups, and wherein R3 is selected from the group consisting of C1-18-alkyl, C6-20-cycloalkyl, C6-20-aryl and C7-20-aralkyl residues; including 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 which can include water to provide N-monosubstituted β-aminoketone sulfonates of formula (II): wherein R1, R2 and R3 are as defined above, and b) asymmetrically hydrogenating.
摘要翻译：一种制备式（1a），（1b）的N-单取代的 - 氨基醇磺酸盐的方法：其中R1是C6-20-芳基或C4-12 - 杂芳基，每个任选被一个或多个卤素原子取代， /或一个或多个C 1-4 - 烷基或C 1-4 - 烷氧基，R 2是C 1-4 - 烷基或C 6-20 - 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，其中R 3选自C 1-18 - 烷基，C 6-20 - 环烷基，C 6-20 - 芳基和C 7-20 - 芳烷基残基; 包括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反应，所述有机溶剂可以包括水以提供具有式（I）的N-单取代和重量的氨基酮磺酸盐（II）：其中R1，R2和R3如上定义，和b）不对称氢化。

8. 发明授权

US07338945B2 Process for the preparation of aminoalcohol derivatives and their further conversion to (1R, 4S)-4(2-amino-6-chloro-5-formamido-4-pyrimidinyl)-amino-2-cyclopentenyl-1-methanol 失效
标题翻译：制备氨基醇衍生物的方法及其进一步转化为（1R，4S）-4-（2-氨基-6-氯-5-甲酰氨基-4-嘧啶基） - 氨基-2-环戊烯基-1-甲醇
公开(公告)号：US07338945B2
公开(公告)日：2008-03-04
申请号：US11616088
申请日：2006-12-26
申请人： Walter Brieden , Josef Schroer , Christine Bernegger-Egli , Eva Maria Urban , Michael Petersen , Jean-Paul Roduit , Katja Berchtold , Holger Breitbach
发明人： Walter Brieden , Josef Schroer , Christine Bernegger-Egli , Eva Maria Urban , Michael Petersen , Jean-Paul Roduit , Katja Berchtold , Holger Breitbach
IPC分类号： A01N43/00
CPC分类号： C07C213/00 , C07B2200/07 , C07C213/02 , C07C213/08 , C07C213/10 , C07C215/42 , C07C233/23 , C07C271/24 , C07C2601/10 , C07D473/00 , C07D473/40 , C12P13/001 , C12P13/02 , C12P41/007 , C07C215/26
摘要： The invention relates to a novel process for the preparation of an aminoalcohol of the formula racemically or optically active, starting from 2-azabicyclo[2.2.1]hept-5-en-3-one, its further conversion to give the corresponding acyl derivative and its further conversion to (1S,4R)- or (1R,4S)-4-(2-amino-6-chloro-9-H-purine-9-yl)-2-cyclopentenyl-1-methanol of the formulae In the latter synthesis, the aminoalcohol is converted into the corresponding D- or L-tartrate, which is then reacted with N-(2-amino-4,6-dichloropyrimidin-5-yl)formamide of the formula to give (1S,4R)- or (1R,4S)-4-[(2-amino-6-chloro-5-formamido-4-pyrimidinyl)amino]-2-cyclopentenyl-1-methanol of the formulae and then cyclized to give the end compounds.
摘要翻译：本发明涉及从2-氮杂双环[2.2.1]庚-5-烯-3-酮开始制备外消旋或光学活性的氨基醇的新方法，其进一步转化得到相应的酰基衍生物并进一步转化为式（1S，4R） - 或（1R，4S）-4-（2-氨基-6-氯-9H-嘌呤-9-基）-2-环戊烯基-1-甲醇，在后一种合成中，将氨基醇转化成相应的D-或L-酒石酸盐，然后与下式的N-（2-氨基-4,6-二氯嘧啶-5-基）甲酰胺反应，得到（1S， 4R） - 或（1R，4S）-4 - [（2-氨基-6-氯-5-甲酰氨基-4-嘧啶基）氨基] -2-环戊烯基-1-甲醇，然后环化，得到结束化合物。

9. 发明申请

US20070043225A1 Method for the production of 3-amino-5-(hydroxymethyl) cyclopentane-1,2-diol-derivatives 失效
标题翻译： 3-氨基-5-（羟甲基）环戊烷-1,2-二醇衍生物的制备方法
公开(公告)号：US20070043225A1
公开(公告)日：2007-02-22
申请号：US10584848
申请日：2005-01-24
申请人： Gareth-John Griffiths , Silvia Lange , Walter Brieden
发明人： Gareth-John Griffiths , Silvia Lange , Walter Brieden
IPC分类号： C07D491/02 , C07D317/44
CPC分类号： C07D317/44 , C07D209/52 , C07D419/08 , C07D491/08
摘要： A method for the production of acetals and ketals of 3-amino-5-(hydroxymethyl)cyclopentane-1,2-diols of formula (I): (and/or the enantiomer), where R1 is H, C1-6-alkyl, C3-8-cycloalkyl or benzyl and (i) R2 is methyl and R3 is ethyl, (ii) R2 is H and R3 is C1-6-alkyl or phenyl or (iii) R2 and R3 together form a group of formula —(CH2)n— with n=4 to 6, present as free amines or as salts of di- or tri-basic organic acids, starting from 2-acetyl-2-azabicyclo[2.2.1]hept-5-en-3-one of formula (II): (and/or the enantiomer). The method is equally useful, depending on the starting material, for the production of enantiomerically-pure compounds, or mixtures with arbitrary enantiomeric content.
摘要翻译：制备式（I）的3-氨基-5-（羟甲基）环戊烷-1,2-二醇的缩醛和缩酮的方法：（和/或对映异构体），其中R 1，是C 1-6烷基，C 3-8 - 环烷基或苄基，和（i）R 2是甲基， SUP> 3是乙基，（ii）R 2是H，R 3是C 1-6 - 烷基或苯基或（iii）R 2和R 3一起形成式 - （CH 2 CH 2）n - n = 4至6，作为游离胺或作为二 - 或三碱性有机酸的盐存在，起始于式（2）的2-乙酰基-2-氮杂双环[2.2.1]庚-5-烯-3-酮 II）:(和/或对映异构体）。取决于起始原料，该方法同样可用于制备对映体纯的化合物或具有任意对映体含量的混合物。

10. 发明授权

US06448402B2 Process for the preparation of aminoalcohol derivatives and their further conversion to (1R, 4S)-4-((2-amino-6-chloro-5-formamido-4-pyrimidinyl)-amino)-2-cyclopentenyl-1-methanol 失效
标题翻译：制备氨基醇衍生物的方法及其进一步转化为（1R，4S）-4 - （（2-氨基-6-氯-5-甲酰氨基-4-嘧啶基） - 氨基）-2-环戊烯基-1-甲醇
公开(公告)号：US06448402B2
公开(公告)日：2002-09-10
申请号：US09772501
申请日：2001-01-30
申请人： Walter Brieden , Josef Schröer , Christine Bernegger-Egli , Eva Maria Urban , Michael Petersen , Jean-Paul Roduit , Katja Berchtold , Holger Breitbach
发明人： Walter Brieden , Josef Schröer , Christine Bernegger-Egli , Eva Maria Urban , Michael Petersen , Jean-Paul Roduit , Katja Berchtold , Holger Breitbach
IPC分类号： C07D47340
CPC分类号： C07C213/00 , C07B2200/07 , C07C213/02 , C07C213/08 , C07C213/10 , C07C215/42 , C07C233/23 , C07C271/24 , C07C2601/10 , C07D473/00 , C07D473/40 , C12P13/001 , C12P13/02 , C12P41/007 , C07C215/26
摘要： The invention relates to a novel process for the preparation of an aminoalcohol of the formula racemically or optically active, starting from 2-azabicyclo[2.2.1]hept-5-en-3-one, its further conversion to give the corresponding acyl derivative and its further conversion to (1S,4R)— or (1R,4S)-4-(2-amino-6-chloro-9-H-purine-9-yl)-2-cyclopentenyl-1-methanol of the formulae In the latter synthesis, the aminoalcohol is converted into the corresponding D- or L-tartrate, which is then reacted with N-(2-amino-4,6-dichloropyrimidin-5-yl)formamide of the formula to give (1S,4R)— or (1R,4S)-4-[(2-amino-6-chloro-5-formamido-4-pyrimidinyl)amino]-2-cyclopentenyl-1-methanol of the formulae and then cyclized to give the end compounds.
摘要翻译：本发明涉及一种从2-氮杂双环[2.2.1]庚-5-烯-3-酮开始制备甲醛或光学活性氨基醇的新方法，其进一步转化得到相应的酰基衍生物和其进一步转化为式（1S，4R） - 或（1R，4S）-4-（2-氨基-6-氯-9H-嘌呤-9-基）-2-环戊烯基-1-甲醇在后者的合成中，将氨基醇转化为相应的D-或L-酒石酸盐，然后将其与制备（1S，4R）-4-甲氧基苯甲酸的N-（2-氨基-4,6-二氯嘧啶-5-基）甲酰胺反应，或（1R，4S）-4 - [（2-氨基-6-氯-5-甲酰氨基-4-嘧啶基）氨基] -2-环戊烯基-1-甲醇，然后环化，得到最终化合物。

你已经成功收藏专利！

检索式保存成功!

IPRDB

热门服务

关于我们

友情链接

联系方式