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1. 发明授权

US06214604B1 Biotechnical production process of piperazine R-&agr;-carboxylic acids and piperazine S-&agr;-carboxylic acid amide 失效
标题翻译：哌嗪R-α-羧酸和哌嗪S-α-羧酸酰胺的生物工艺制备方法
公开(公告)号：US06214604B1
公开(公告)日：2001-04-10
申请号：US08952295
申请日：1997-11-10
申请人： Andreas Kiener , Jean-Paul Roduit , Klaus Heinzmann
发明人： Andreas Kiener , Jean-Paul Roduit , Klaus Heinzmann
IPC分类号： C12N120
CPC分类号： C12R1/38 , C12P17/12 , C12P41/006
摘要： A biologically pure culture of microorganisms capable of converting RS-&agr;-piperazinecarboxamides into the corresponding R-&agr;-piperazinecarboxylic acid. R-&agr;-piperazinecarboxamides is the only nitrogen source.
摘要翻译：能够将RS-α-哌嗪甲酰胺转化为相应的R-α-哌嗪甲酸的生物学纯的微生物培养物。 R-α-哌嗪甲酰胺是唯一的氮源。

2. 发明授权

US5766893A Biotechnological process for the preparation of cyclic s-alpha-imino carboxylic acids and r-alpha-imino carboxamides 失效
标题翻译：用于制备环状α-α-亚氨基羧酸和r-α-亚氨基甲酰胺的生物技术方法
公开(公告)号：US5766893A
公开(公告)日：1998-06-16
申请号：US614345
申请日：1996-03-12
申请人： Andreas Kiener , Jean-Paul Roduit , Jorg Kohr , Nicholas Shaw
发明人： Andreas Kiener , Jean-Paul Roduit , Jorg Kohr , Nicholas Shaw
IPC分类号： C12N1/20 , C12P17/00 , C12P17/10 , C12P17/12 , C12P41/00 , C12R1/22 , C12R1/38 , C12R1/39 , C12R1/40 , C12P13/00
CPC分类号： C12R1/22 , C12P17/10 , C12P17/12 , C12P41/006 , C12R1/39 , C12R1/40 , Y10S435/852 , Y10S435/874 , Y10S435/876 , Y10S435/877 , Y10S435/878
摘要： Microorganisms of interest are capable of utilizing .alpha.-imino carboxamides, in the form of the racemate or of its optically active isomers, of the general formula ##STR1## wherein A together with --NH-- and --CH-- is an optionally substituted 5- or 6-membered saturated heterocyclic ring, as sole nitrogen source, and converting (RS)-.alpha.-imino carboxamides of Formula I into an S-.alpha.-imino carboxylic acid of the general formula ##STR2## These microorganisms are useful also for biconversion of an (RS)-.alpha.-imino carboxamide of Formula I into an S-.alpha.-imino carboxylic acid.
摘要翻译：感兴趣的微生物能够利用具有通式I的外消旋体或其旋光异构体形式的α-亚氨基甲酰胺，其中A与-NH-和-CH-是任选取代的5- 或6元饱和杂环作为唯一的氮源，并将式I的（RS）-α-亚氨基甲酰胺转化为通式为II的S-α-亚氨基羧酸。这些微生物也用于双转录的式（I）的（RS）-α-亚氨基甲酰胺加入到S-亚氨基羧酸中。

3. 发明授权

US5760236A Di and trisubstituted pyridines 失效
标题翻译：二取代和三取代吡啶
公开(公告)号：US5760236A
公开(公告)日：1998-06-02
申请号：US561230
申请日：1995-11-21
申请人： Andreas Kiener , Jean-Paul Roduit , Alain Wellig
发明人： Andreas Kiener , Jean-Paul Roduit , Alain Wellig
IPC分类号： C12P17/12 , C07D213/61 , C07D213/64 , C07D405/04 , C12P17/16 , C12R1/38 , C07D401/04
CPC分类号： C07D213/64 , C07D213/61 , C07D405/04
摘要： Substituted pyridines of the general formula: ##STR1## wherein R.sup.1 is hydroxyl or chlorine, and a) X is hydrogen or chlorine, R.sup.2 and R.sup.3 together are .dbd.O, R.sup.4 is a group of the formula --OR.sup.5 and R.sup.5 is hydrogen, C.sub.1 -C.sub.4 -alkyl or benzyl, or b) X is hydrogen and R.sup.2, R.sup.3 and R.sup.4 together are .dbd.N--NH--, or c) X and R.sup.2 each is hydrogen and R.sup.3 and R.sup.4 together are --O--, or d) X and R.sup.2 each is hydrogen, R.sup.3 is hydroxyl and R.sup.4 is amino or hydroxyl. The compounds are obtained by subjecting nicotine to microbiological oxidation to give 5-succinoyl-2-pyridone, followed by chemical reactions. The compounds are suitable as intermediates for the preparation of pharmaceutically active compounds.
摘要翻译：取代的具有以下通式的吡啶：其中R1是羟基或氯，以及a）X是氢或氯，R2和R3一起是= O，R4是式-OR5的基团，R5是氢，C1 C 1-4烷基或苄基，或b）X是氢，R 2，R 3和R 4一起是N-NH-，或c）X和R 2各自是氢，R 3和R 4一起是-O-，或d）X R2各自为氢，R3为羟基，R4为氨基或羟基。该化合物通过使尼古丁进行微生物氧化得到5-琥珀酰基-2-吡啶酮，然后进行化学反应。该化合物适合作为制备药物活性化合物的中间体。

4. 发明授权

US5994540A Di-and trisubstituted pyridines and their preparation 失效
标题翻译：二取代和三取代吡啶及其制备方法
公开(公告)号：US5994540A
公开(公告)日：1999-11-30
申请号：US69996
申请日：1998-04-30
申请人： Andreas Kiener , Jean-Paul Roduit , Alain Wellig
发明人： Andreas Kiener , Jean-Paul Roduit , Alain Wellig
IPC分类号： C12P17/12 , C07D213/61 , C07D213/64 , C07D405/04 , C12P17/16 , C12R1/38 , C07D401/04 , C07D403/04 , C12Q1/02
CPC分类号： C07D213/64 , C07D213/61 , C07D405/04
摘要： Substituted pyridines of the general formula: ##STR1## wherein R.sup.1 is hydroxyl or chlorine, and a) X is hydrogen or chlorine, R.sup.2 and R.sup.3 together are .dbd.O, R.sup.4 is a group of the formula --OR.sup.5 and R.sup.5 is hydrogen, C.sub.1 -C.sub.4 -alkyl or benzyl orb) X is hydrogen and R.sup.2, R.sup.3 and R.sup.4 together are .dbd.N--NH--, orc) X and R.sup.2 each is hydrogen and R.sup.3 and R.sup.4 together are --O--, ord) X and R.sup.2 each is hydrogen, R.sup.3 is hydroxyl and R.sup.4 is amino or hydroxy.The compounds are obtained by subjecting nicotine to microbiological oxidation to give 5-succinoyl-2-pyridone, followed by chemical reactions. The compounds are suitable as intermediates for the preparation of pharmaceutically active compounds.
摘要翻译：取代的具有下列通式的吡啶：其中R1是羟基或氯，以及a）X是氢或氯，R2和R3一起是= O，R4是式-OR5的基团，R5是氢，C1-C4-烷基或苄基或b）X是氢，R 2，R 3和R 4一起是N-NH-，或c）X和R 2各自是氢，R 3和R 4一起是-O-，或d）X和R 2各自是氢 R3是羟基，R4是氨基或羟基。该化合物通过使尼古丁进行微生物氧化得到5-琥珀酰基-2-吡啶酮，然后进行化学反应。该化合物适合作为制备药物活性化合物的中间体。

5. 发明授权

US5702930A Microbiological process for the preparation of heteroaromatic carboxylic acids using Alcaligenes faecalis 失效
标题翻译：使用粪产碱菌制备杂芳族羧酸的微生物过程
公开(公告)号：US5702930A
公开(公告)日：1997-12-30
申请号：US659362
申请日：1996-06-06
申请人： Andreas Kiener , Jean-Paul Roduit , Rainer Glockler
发明人： Andreas Kiener , Jean-Paul Roduit , Rainer Glockler
IPC分类号： C12P17/10 , C07D213/79 , C07D241/24 , C12P17/12 , C12P17/14 , C12R1/05 , C12P1/04 , C12P1/20
CPC分类号： C12P17/12
摘要： A microbiological process for the preparation of a heteroaromatic carboxylic acid or one of its physiologically tolerated salts of the formulae I or II: ##STR1## wherein R.sub.1 and R.sub.2 are identical or different and each denotes a hydrogen or halogen atom, and X denotes a nitrogen atom or CH--, from a heteroaromatic nitrile of the formulae III or IV, respectively: ##STR2## First, a microorganism, Alcaligenes faecalis (DSM 6335), is cultured in the presence of an inducer, 2-cyanopyridine, and a carbon source such as a dicarboxylic acid, a tricarboxylic acid or a carbohydrate. Substrate III or IV is then reacted with the cultured microorganism. The biotransformation is carried out under anaerobic conditions for compounds of the formula I, and under aerobic conditions for compounds of the formula II.
摘要翻译：用于制备杂芳族羧酸或其式I或II的生理耐受盐之一的微生物过程：其中R 1和R 2相同或不同，并且各自表示氢或卤素原子，X分别代表式III或IV的杂芳香腈或氮原子：首先将微生物粪肠产杆菌（DSM 6335）在存在下培养，的诱导剂，2-氰基吡啶和碳源如二羧酸，三羧酸或碳水化合物。然后将底物III或IV与培养的微生物反应。生物转化在式I化合物的厌氧条件下进行，在需氧条件下进行式II化合物。

6. 发明授权

US5622846A Biotechnological process for the preparation of cyclic-s-.alpha.-imino carboxylic acids and r-.alpha.-imino carboxamides 失效
标题翻译：用于制备环状α-α-亚氨基羧酸和r-α-亚氨基甲酰胺的生物技术方法
公开(公告)号：US5622846A
公开(公告)日：1997-04-22
申请号：US478960
申请日：1995-06-07
申请人： Andreas Kiener , Jean-Paul Roduit , J org Kohr , Nicholas Shaw
发明人： Andreas Kiener , Jean-Paul Roduit , J org Kohr , Nicholas Shaw
IPC分类号： C12N1/20 , C12P17/00 , C12P17/10 , C12P17/12 , C12P41/00 , C12R1/22 , C12R1/38 , C12R1/39 , C12R1/40 , C12P13/00
CPC分类号： C12R1/22 , C12P17/10 , C12P17/12 , C12P41/006 , C12R1/39 , C12R1/40 , Y10S435/852 , Y10S435/874 , Y10S435/876 , Y10S435/877 , Y10S435/878
摘要： Microorganisms of interest are capable of utilizing .alpha.-imino carboxamides, in the form of the racemate or of its optically active isomers, of the general formula ##STR1## wherein A together with --NH-- and --CH-- is an optionally substituted 5- or 6-membered saturated heterocyclic ring, as sole nitrogen source, and converting (RS)-.alpha.-imino carboximides of Formula I into an S-.alpha.-amino carboxylic acid of the general formula ##STR2## These microorganisms are useful also for biconversion of an (RS)-.alpha.-imino carboxamide of Formula I into an S-.alpha.-amino carboxylic acid.
摘要翻译：感兴趣的微生物能够利用具有通式I的外消旋体或其旋光异构体形式的α-亚氨基甲酰胺，其中A与-NH-和-CH-是任选取代的5- 或6元饱和杂环，作为唯一的氮源，并将式I的（RS）-α-亚氨基二甲酰亚胺转化为通式为“II”的S-α-氨基羧酸。这些微生物也可用于双转录的式（I）的（RS）-α-亚氨基甲酰胺转化成S-α-氨基羧酸。

7. 发明申请

US20060211862A1 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-氯代-5-甲酰氨基-4-吡啶基） - 氨基-2-环戊烯-1-甲醇
公开(公告)号：US20060211862A1
公开(公告)日：2006-09-21
申请号：US11421266
申请日：2006-05-31
申请人： Walter Brieden , Josef Schroer , Christine Bernegger-Egli , Eva Urban , Michael Petersen , Jean-Paul Roduit , Katja Berchtold , Holger Breitbach
发明人： Walter Brieden , Josef Schroer , Christine Bernegger-Egli , Eva Urban , Michael Petersen , Jean-Paul Roduit , Katja Berchtold , Holger Breitbach
IPC分类号： C07D473/10 , C07D239/50
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（1S，4R） - 或（1R，4S）-4-（2-氨基-6-氯-9H-嘌呤-9-基）-2-环戊烯基-1-甲醇配方在后一种合成中，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，末端化合物。

8. 发明授权

US06723868B1 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：US06723868B1
公开(公告)日：2004-04-20
申请号：US09198427
申请日：1998-11-24
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： C07C6996
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-9H-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成式（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，将氨基醇转化成相应的D-或L-酒石酸盐，然后与制备（1S，4R） - 或（1S，4R） - 的（1R，4R） - 的N-（2-氨基-4,6-二氯嘧啶-5-基）甲酰胺反应， 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

US06175011B1 Process for the preparation of arylamides of heteroaromatic carboxylic acids 失效
标题翻译：用于制备杂芳族羧酸芳基酰胺的方法
公开(公告)号：US06175011B1
公开(公告)日：2001-01-16
申请号：US09280975
申请日：1999-03-30
申请人： Jean-Paul Roduit , Georges Kalbermatten
发明人： Jean-Paul Roduit , Georges Kalbermatten
IPC分类号： C07D25112
CPC分类号： C07D241/24 , B01J31/2295 , B01J31/2409 , B01J2231/4205 , B01J2531/824 , B01J2531/842 , C07D213/81
摘要： A process for the preparation of arylamides of heteroaromatic carboxylic acids of the formula: in which each An is nitrogen or CRn (n=1-5), with the proviso that at least one of the ring members is nitrogen and that two nitrogen atoms are not bonded directly to one another; R1 to R5, if present, independently of one another are hydrogen, C1-4-alkyl or aryl, also one of the substituents R1 to R5 can be a group of the formula —OR, in which R is an optionally substituted aromatic or heteroaromatic radical; R6 is hydrogen or C1-4-alkyl; and R7 is an optionally substituted aromatic or heteroaromatic radical. The amides are obtained from the corresponding heteroaromatic halogen compounds, the corresponding aromatic amines and carbon monoxide in the presence of a palladium diphosphine complex. Compounds of this class, especially those in which one of the substituents R1 to R5 is an aryloxy group, are important herbicides.
摘要翻译：制备下式的杂芳族羧酸的芳基酰胺的方法：其中每个An是氮或CR n（n = 1-5），条件是至少一个环成员是氮并且两个氮原子是不直接相互粘合; R 1至R 5（如果存在）彼此独立地是氢，C 1-4 - 烷基或芳基，取代基R 1至R 5中的一个也可以是式-OR的基团，其中R是任选取代的芳族或杂芳族激进; R6是氢或C1-4烷基; 并且R 7是任选取代的芳族或杂芳族基团。在钯二膦配合物存在下，酰胺由相应的杂芳族卤素化合物，相应的芳族胺和一氧化碳获得。该类化合物，特别是其中一个取代基R 1至R 5为芳氧基的化合物是重要的除草剂。

10. 发明授权

US5886181A Process for the preparation of optically active piperazine-2-carboxylic acid derivatives 失效
标题翻译：制备光学活性哌嗪-2-羧酸衍生物的方法
公开(公告)号：US5886181A
公开(公告)日：1999-03-23
申请号：US651260
申请日：1996-05-23
申请人： Rudolf Fuchs , Jean-Paul Roduit
发明人： Rudolf Fuchs , Jean-Paul Roduit
IPC分类号： B01J31/22 , B01J31/28 , C07B53/00 , C07D241/04 , C07D413/06
CPC分类号： B01J31/2404 , B01J31/2291 , B01J31/2295 , B01J31/2409 , B01J31/28 , C07D241/04 , B01J2231/645 , B01J2531/0286 , B01J2531/821 , B01J2531/822 , B01J2531/827
摘要： Optically active piperazine-2-carboxylic acid derivatives of the general formula: ##STR1## wherein R.sup.1 and R.sup.2 are inter alia hydrogen, alkyl or acyl and X is alkoxy or a (substituted) amino group, are prepared by asymmetric hydrogenation of the corresponding 1,4,5,6-tetrahydropyrazines, catalyzed by optically active rhodium, ruthenium or iridium complexes. The compounds of the Formula 1 are intermediates for the preparation of pharmaceutical active ingredients, for example, HIV protease inhibitors.
摘要翻译：通式为其中R 1和R 2特别是氢，烷基或酰基，X为烷氧基或（取代的）氨基的光学活性哌嗪-2-羧酸衍生物通过相应的由光学活性铑，钌或铱络合物催化的1,4,5,6-四氢吡嗪。式1的化合物是用于制备药物活性成分的中间体，例如HIV蛋白酶抑制剂。

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