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1. 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。

2. 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。

3. 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。

4. 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。

5. 发明授权

US5760264A Process for preparing optically active metallocenyl-phosphines 失效
标题翻译：光学活性金属茂合膦的制备方法
公开(公告)号：US5760264A
公开(公告)日：1998-06-02
申请号：US836978
申请日：1997-07-09
申请人： Walter Brieden
发明人： Walter Brieden
IPC分类号： C07F9/50 , C07F17/00 , C07F17/02 , B01J31/00 , C07F15/02
CPC分类号： C07F17/02
摘要： Disclosed is a novel method of producing optically active metallocenyl phosphines of the general formula shown In the formula (Ia) (Ib), M represents iron, ruthenium or nickel; R.sup.1 and R.sup.1' both represent C.sub.1 -C.sub.4 alkyl groups; R.sup.2 and R.sup.3 each represent independently of each other either hydrogen or a C.sub.1 -C.sub.4 alkyl group, or, together with the nitrogen atom, form a five- or six member saturated heterocyclic ring which may optionally contain further heteroatoms; R.sup.4 and R.sup.5 each represent independently of each other a C.sub.1 -C.sub.4 alkyl group (for example) or an aryl group which is optionally substituted with one or more methyl or methoxy groups or with one or more fluorine atoms. These are obtained from acyl- or 1,1'-diacylmetallocenes by enantioselective reduction with borane in the presence of optically active oxazoborolidines, esterification of the metallocenyl alkanols thus obtained, nucleophilic substitution of the ester group with a secondary amine, lithiation and reaction with a phosphine halide.
摘要翻译： PCT No.PCT / EP95 / 04678 371日期1997年7月9日第 102（e）日期1997年7月9日PCT 1995年11月28日PCT PCT。公开号WO96 / 16971 日期1996年6月6日公开是制备通式（Ia）（Ib）所示通式的光学活性金属茂合膦的新方法，M代表铁，钌或镍; R1和R1'都表示C1-C4烷基; R2和R3各自独立地表示氢或C1-C4烷基，或者与氮原子一起形成五元或六元饱和的杂环，其可以任选地含有另外的杂原子; R4和R5各自独立地表示C1-C4烷基（例如）或任选被一个或多个甲基或甲氧基取代或具有一个或多个氟原子的芳基。这些通过在光学活性恶唑烷的存在下用硼烷对映选择性还原得到，由此得到的金属茂基链烷醇的酯化，酯基与仲胺的亲核取代，锂化反应和与其反应，得到酰基 - 或1,1'-二酰基茂金属膦卤化物。

6. 发明授权

US08258338B2 Process for the preparation of enantiomerically pure 1-substituted-3-aminoalcohols 有权
标题翻译：用于制备对映体纯的1-取代-3-氨基醇的方法
公开(公告)号：US08258338B2
公开(公告)日：2012-09-04
申请号：US11884542
申请日：2006-02-14
申请人： Walter Brieden , Martin Clausen , John McGarrity , Hanspeter Mettler , Colette Mettler, legal representative , Dominique Michel
发明人： Walter Brieden , Martin Clausen , John McGarrity , Hanspeter Mettler , Dominique Michel
IPC分类号： C07C33/32 , C07D333/12
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 (Ia), (Ib): 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. The process has 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, the organic solvent optionally containing water, to afford N-monosubstituted β-aminoketone sulfonates of formula (II): wherein R1, R2 and R3 are as defined above, and (b) asymmetrically hydrogenating. The sulfonates in the presence of a base and a catalyst of a transition metal and a disphosphine ligand, in a polar solvent, optionally in the presence of water.
摘要翻译：一种制备式（Ia），（Ib）的N-单取代和（bgr） - 氨基醇磺酸盐的方法：其中R1是C6-20-芳基或C4-12 - 杂芳基，各自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，并且其中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。该方法具有以下步骤：（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（任选含有水的有机溶剂）中反应，得到N-单取代的＆bgr （II）的氨基酮磺酸盐：其中R 1，R 2和R 3如上所定义，和（b）不对称氢化。在极性溶剂中，任选地在水存在下，在过渡金属和二膦配体的碱存在下和催化剂存在下的磺酸盐。

7. 发明授权

US07417153B2 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：US07417153B2
公开(公告)日：2008-08-26
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： C07D209/52 , C07D209/54 , C07D209/56 , C07D209/96 , 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) cyclopenlane-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-aza-bicyclo[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，以游离胺或二 - 或三碱性有机酸的盐形式存在，起始于2-乙酰基-2-氮杂 - 双环[2.2.1]庚-5-烯-3-酮式（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。

8. 发明授权

US07229981B2 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：US07229981B2
公开(公告)日：2007-06-12
申请号：US10695930
申请日：2003-10-29
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： 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-azabi-cyclo[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（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，得到最终化合物。

9. 发明授权

US06716981B2 Process for the preparation of N-(amino-4, 6-dihalo-pyrimidine) formamides 失效
标题翻译：制备N-（氨基-4,6-二卤代 - 嘧啶）甲酰胺的方法
公开(公告)号：US06716981B2
公开(公告)日：2004-04-06
申请号：US09867552
申请日：2001-05-31
申请人： Elie Saikali , Walter Brieden
发明人： Elie Saikali , Walter Brieden
IPC分类号： C07D23942
CPC分类号： C07D239/48
摘要： A process for the preparation of a 2,5-diamino-4,6-dihalopyrimidine of the formula: in which X is a halogen atom, comprising reacting 2,5-diamino-4,6-dihydroxypyrimidine or its salt of the formula: with a phosphorus oxyhalide and a quaternary ammonium halide or an amine in a halogenated hydrocarbon as a solvent.
摘要翻译：一种制备下式的2,5-二氨基-4,6-二卤代嘧啶的方法，其中X是卤素原子，包括使2,5-二氨基-4,6-二羟基嘧啶或其下式的盐：在卤代烃中作为溶剂使用卤氧化磷和季铵卤化物或胺。

10. 发明授权

US06271376B1 Process for the preparation of N-(amino-4,6-dihalo-pyrimidine) formamides 失效
标题翻译：制备N-（氨基-4,6-二卤代 - 嘧啶）甲酰胺的方法
公开(公告)号：US06271376B1
公开(公告)日：2001-08-07
申请号：US09461244
申请日：1999-12-16
申请人： Elie Saikali , Walter Brieden
发明人： Elie Saikali , Walter Brieden
IPC分类号： A61K31505
CPC分类号： C07D239/48
摘要： A process for the preparation of N-(amino-4,6-dihalopyrimidine)formamides of the formula: in which X is a halogen atom, starting from 2,5-diamino-4,6-dihalopyrimidine of the formula: in which X has the meaning afore-mentioned, by reaction with formic acid.
摘要翻译：制备下式的N-（氨基-4,6-二卤代嘧啶）甲酰胺的方法：其中X是卤素原子，由下式的2,5-二氨基-4,6-二卤代嘧啶开始：其中X 具有上述含义，与甲酸反应。

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