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1. 发明授权

US07052885B2 Process for preparing heterocyclic (R)- and (S)-cyanohydrins 失效
标题翻译：制备杂环（R） - 和（S） - 氰基醇的方法
公开(公告)号：US07052885B2
公开(公告)日：2006-05-30
申请号：US10325922
申请日：2002-12-23
申请人： Peter Poechlauer , Wolfgang Skranc , Herbert Mayrhofer , Irma Wirth , Rudolf Neuhofer , Herfried Griengl , Martin Fechter
发明人： Peter Poechlauer , Wolfgang Skranc , Herbert Mayrhofer , Irma Wirth , Rudolf Neuhofer , Herfried Griengl , Martin Fechter
IPC分类号： C12P17/00 , C12P17/02 , C12P17/04 , C12P17/06 , C12P17/18
CPC分类号： C12P13/004 , C12P17/00 , C12P17/04
摘要： A process for preparing enantiomer-enriched heterocyclic (R)- and (S)-cyanohydrins of the formula (I), where R1, R2, R3, R4 independently of one another are H, an unsubstituted or substituted C1–C24-alkyl, alkenyl or alkynyl radical, where one or more carbon atoms in the chain can be replaced by an oxygen atom, a nitrogen atom, a sulfur atom, an SO or an SO2 group, an unsubstituted or substituted aryl or heteroaryl radical or heterocyclic radical or halogen, hydroxyl, NR5R6, acetyl, oxo, C1–C6-carbalkoxy, C1–C6-carbalkoxyamino, COOR7, cyano, amide, benzoylamino or NO2,R5 and R6 are H, C1–C6-alkyl radical, phenyl radical, benzyl radical or COOR7, or together form a C2–C8-alkylene or heteroalkylene radical,R7 is H or C1–C6-alkyl,n is 0, 1, 2 or 3,X, Y and Z can be an unsubstituted or substituted carbon atom or a radical selected from the group consisting of N, O, S or NR5R6, where R5 and R6 are as defined above, SO or SO2, and at least one of the radicals X, Y and Z is not a carbon atom, where the compounds of the formula (I) can have one or more double bonds in the ring, with the proviso that in a 5-membered ring the double bond is not conjugated with the —C(OH)CN-group, and/or can be anellated and/or bridged,by reacting a ketone of the formula (II), where R1, R2, R3, R4, X, Y, Z and n have the meanings above, with an (R)- or (S)-hydroxynitrile lyase in an organic, aqueous or two-phase system, or in emulsion, in the presence of a cyanide group donor.
摘要翻译：制备式（I）的对映异构体富集的杂环（R） - 和（S） - 氰基醇的方法，其中R 1，R 2，R 3，R 4彼此独立地是H，未取代或取代的C 1 - 链烯基或炔基，其中链中的一个或多个碳原子可以被氧原子，氮原子，硫原子，SO或 SO 2 2基团，未取代或取代的芳基或杂芳基或杂环基或卤素，羟基，NR 5 R 6，乙酰基，氧代C 1 -C 6 - 亚烷基氧基，C 1 -C 6 - 烷氧基氨基，COOR 7，氰基，酰胺，苯甲酰氨基或NO 2，R 5和R 6是H C 1 -C 6 - 烷基，苯基，苄基或COOR 7，或一起形成C 1 -C 6 - 8亚烷基或杂亚烷基，R 7是H或C 1 -C 6 - 烷基，n是0,1,2或3，X，Y 并且Z可以是未取代或取代的碳原子或选自它的基团由N，O，S或NR5R6组成的基团，其中R 5和R 6如上定义，SO或SO 2，并且基团X，Y和Z中的至少一个不是碳原子，其中式（I）的化合物可以在环中具有一个或多个双键，条件是在5元环中双键不与-C（OH）CN-基团共轭，并且 /或可以通过使式（II）的酮（其中R 1，R 2，R 3，R 4，X，Y，Z和n具有上述含义）与（R） - 或（ S） - 羟基腈裂解酶在有机，水相或两相体系中，或在乳液中，在氰化物基团给体存在下。

2. 发明授权

US06909011B2 Process for preparing protected, enantiomer-enriched cyanohydrins by in-situ derivatization 失效
标题翻译：通过原位衍生制备保护的富含对映异构体的氰醇的方法
公开(公告)号：US06909011B2
公开(公告)日：2005-06-21
申请号：US10325923
申请日：2002-12-23
申请人： Wolfgang Skranc , Peter Poechlauer , Irma Wirth , Rudolf Neuhofer , Herbert Mayrhofer
发明人： Wolfgang Skranc , Peter Poechlauer , Irma Wirth , Rudolf Neuhofer , Herbert Mayrhofer
IPC分类号： C12P13/00 , C12R1/91 , C07C253/16 , C12P13/16
CPC分类号： C12P13/004
摘要： A process for preparing protected, enantiomer-enriched cyanohydrins of the formula where R1 and R2 independently of one another can be an unsubstituted, monosubstituted or polysubstituted C1-C20-alkyl, C5-C20-aryl, C5-C20-heteroaryl, C5-C20-alkaryl, C5-C20-alkylheteroaryl or C5-C20-aralkyl radical or an unsubstituted, monosubstituted or polysubstituted C5-C20-heterocycle, or C5-C20-alkylheterocycle or together can be an unsubstituted or substituted C4-C20-alkylene radical, which can contain one or more heteroatoms in the chain, or one of the radicals is hydrogen, and R3 can be an unsubstituted or substituted C1-C20-alkyl, C5-C20-aryl or C5-C20-heteroaryl radical, by reacting an aldehyde or ketone of the formula where R1 and R2 are defined as above, in the presence of an (R)- or (S)-hydroxynitrile lyase in an organic, aqueous or 2-phase system or in emulsion at a temperature of −5 to +40° C. with a carbonic ester nitrile of the formula where R3 is defined as above.
摘要翻译：制备具有下式的受保护的对映异构体富含氰醇的方法其中R 1和R 2彼此独立地可以是未取代的，单取代的或多取代的C 1 -C 20 - 烷基 C 5 -C 20 - 芳基，C 5 -C 20 - 杂芳基，C 5 - C 20 -C 20 - 烷芳基，C 5 -C 20 - 烷基杂芳基或C 5 -C 或是未取代的单取代或多取代的C 5 -C 20 - 杂环或C 5 - -C 20 - 烷基杂环或一起可以是未取代或取代的C 4 -C 20 - 亚烷基，其可以含有一个或多个杂原子在链中，或者一个基团是氢，并且R 3可以是未取代或取代的C 1 -C 20 - 烷基，C 5 C 20 -C 20 - 芳基或C 5 -C 20 - 杂芳基，通过使下式的醛或酮反应其中R1和R2 在有机，水相或两相体系中的（R） - 或（S） - 羟基腈裂解酶存在下，或在-5至+ 40℃的温度下与碳酸酯腈，其中R3如上定义。

3. 发明授权

US06818423B2 Process for the preparation of chiral &agr;-hydroxycarboxylic acids 失效
标题翻译：制备手性α-羟基羧酸的方法
公开(公告)号：US06818423B2
公开(公告)日：2004-11-16
申请号：US10286892
申请日：2002-11-04
申请人： Herbert Mayrhofer , Rudolf Neuhofer , Peter Poechlauer , Wolfgang Skranc , Irma Wirth
发明人： Herbert Mayrhofer , Rudolf Neuhofer , Peter Poechlauer , Wolfgang Skranc , Irma Wirth
IPC分类号： C12P742
CPC分类号： C12P13/004 , C07B2200/07 , C07C51/377 , C07C319/18 , C07C319/20 , C07C319/28 , C07C59/01 , C07C323/22 , C07C323/60 , C07C323/52
摘要： A process for the preparation of chiral &agr;-hydroxycarboxylic acids: in which R1 is optionally halogen substituted C1-C2-alkyl and R2 is optionally halogen substituted C2-C3-alkyl from a compound: in which R′2 is optionally halogen substituted C2-C3-alkylene, m is 0 or 1 and R is optionally substituted alkyl, aryl, heteroaryl or heterocyclyl and X can be oxygen, sulfur, sulfinyl, sulfonyl, imino, C1-C6-alkylimino, xanthate, silyl, or, if m is equal to 0, halogen, which is reacted in the presence of a cyanide group donor to give the corresponding (R)- or (S)-cyanohydrin or its racemate: which then is converted by means of acidic hydrolysis into an acid: or its racemate, and by cleavage of the group: (R)m-X (V), and optional resolution, whereby the desired chiral &agr;-hydroxycarboxylic acid of the formula (I) is obtained.
摘要翻译：一种制备手性α-羟基羧酸的方法：其中R 1任选为卤素取代的C 1 -C 2 - 烷基，R 2为卤素取代的C 2 -C 3 - 烷基，其中R'2任选为卤素取代的C2- C3-亚烷基，m是0或1，R是任选取代的烷基，芳基，杂芳基或杂环基，X可以是氧，硫，亚磺酰基，磺酰基，亚氨基，C 1 -C 6烷基亚氨基，黄原酸酯，甲硅烷基，或者，如果m是等于0，卤素，其在氰化物基团供体的存在下反应，得到相应的（R） - 或（S） - 氰基氢茚或其外消旋物，然后通过酸性水解转化成酸：或其通过裂解所述基团：任选的分辨率，由此获得所需的式（I）手性α-羟基羧酸。

4. 发明授权

US06861243B2 Genes containing a DNA sequence coding for hydroxynitrile lyase, recombinant proteins derived therefrom and having hydroxynitrile lyase activity, and use thereof 有权
标题翻译：含有编码羟基腈裂解酶的DNA序列的基因，由其衍生并具有羟基腈裂解酶活性的重组蛋白质及其用途
公开(公告)号：US06861243B2
公开(公告)日：2005-03-01
申请号：US10046232
申请日：2002-01-16
申请人： Helmut Schwab , Anton Glieder , Christoph Kratky , Ingrid Dreveny , Peter Pöchlauer , Wolfgang Skranc , Herbert Mayrhofer , Irma Wirth , Rudolf Neuhofer , Rodolfo Bona
发明人： Helmut Schwab , Anton Glieder , Christoph Kratky , Ingrid Dreveny , Peter Pöchlauer , Wolfgang Skranc , Herbert Mayrhofer , Irma Wirth , Rudolf Neuhofer , Rodolfo Bona
IPC分类号： C12N15/09 , C07K19/00 , C12N9/04 , C12N9/88 , C12N15/52 , C12N15/60 , C12P13/00
CPC分类号： C12P13/004 , C12N9/88 , C12N15/52
摘要： New genes containing a DNA sequence coding for hydroxynitrile lyase, which genes can be prepared via a primer combination based on the DNA sequence of the 5′-region of the mdl genes from Prunus serotina and from Prunus amygdalus and/or a primer 2 based on the 3′-region of the DNA sequences of one of the hydroxynitrile lyase isoenzymes from Prunus serotina or from Prunus amygdalus, subsequent amplification with a DNA polymerase using a DNA from organisms, containing genes coding for hydroxynitrile lyase, as templates and cloning, and also recombinant proteins which can be prepared in suitable host cells by heterologous expression of the DNA sequence of said HNL genes, and proteins and fusion proteins derived therefrom and use of said proteins for preparing (R)- or (S)-cyanohydrins.
摘要翻译：含有编码羟基腈裂解酶的DNA序列的新基因，该基因可以通过引物组合基于来自黑麦白浆和来自杏仁核的md1基因的5'区域的DNA序列和/或基于其中一个羟基腈裂解酶同工酶的一个来自山梨果皮或杏仁杏仁的DNA序列的3'区域，随后用含有编码羟基腈裂解酶的基因的来自生物体的DNA的DNA聚合酶扩增作为模板和克隆，以及可以通过异源表达所述HNL基因的DNA序列以及从其衍生的蛋白质和融合蛋白质以及所述蛋白质用于制备（R） - 或（S） - 氰基氢化物的方法，在合适的宿主细胞中制备重组蛋白质。

5. 发明授权

US07202075B2 Isolated protein having hydroxynitrile lyase activity 有权
标题翻译：具有羟基腈裂解酶活性的分离的蛋白质
公开(公告)号：US07202075B2
公开(公告)日：2007-04-10
申请号：US10940954
申请日：2004-09-15
申请人： Helmut Schwab , Anton Glieder , Christoph Kratky , Ingrid Dreveny , Rodolfo Bona , Peter Pöchlauer , Wolfgang Skranc , Herbert Mayrhofer , Irma Wirth , Rudolf Neuhofer
发明人： Helmut Schwab , Anton Glieder , Christoph Kratky , Ingrid Dreveny , Rodolfo Bona , Peter Pöchlauer , Wolfgang Skranc , Herbert Mayrhofer , Irma Wirth , Rudolf Neuhofer
IPC分类号： C12N9/88 , C12P1/00 , C07K1/00 , C07H21/04 , C07C253/00
CPC分类号： C12P13/004 , C12N9/88 , C12N15/52
摘要： New genes containing a DNA sequence coding for hydroxynitrile lyase, which genes can be prepared via a primer combination based on the DNA sequence of the 5′-region of the mdl genes from the Prunus serotina and from Prunus amygdalus and/or a primer 2 based on the 3′-region of the DNA sequences of one of the hydroxynitrile lyase isoenzymes from Prunus serotina or from Prunus amygdalus, subsequent amplification with a DNA polymerase using a DNA from organisms, containing genes coding for hydroxynitrile lyase, as templates and cloning, and also recombinant proteins which can be prepared in suitable host cells by heterologous expression of the DNA sequence of said HNL genes, and proteins and fusion proteins derived therefrom and use of said proteins for preparing (R)- or (S)-cyanohydrins.
摘要翻译：含有编码羟基腈裂解酶的DNA序列的新基因，该基因可以通过引物组合基于来自白芥子和来自杏仁核的md1基因的5'区域的DNA序列和/或引物2 在其中一个羟基腈裂解酶同工酶的一个DNA序列的3'区域上，接着使用含有编码羟基腈裂解酶的基因的生物体的DNA作为模板和克隆，用DNA聚合酶扩增，以及还可以通过异源表达所述HNL基因的DNA序列，以及从其衍生的蛋白质和融合蛋白质以及所述蛋白质用于制备（R） - 或（S） - 氰基醇的方法，在合适的宿主细胞中制备重组蛋白质。

6. 发明申请

US20050064552A1 Genes containing a DNA sequence coding for hydroxynitrile lyase, recombinant proteins derived therefrom and having hydroxynitrile lyase activity, and use thereof 有权
标题翻译：含有编码羟基腈裂解酶的DNA序列的基因，由其衍生并具有羟基腈裂解酶活性的重组蛋白质及其用途
公开(公告)号：US20050064552A1
公开(公告)日：2005-03-24
申请号：US10940954
申请日：2004-09-15
申请人： Helmut Schwab , Anton Glieder , Christoph Kratky , Ingrid Dreveny , Rodolfo Bona , Peter Pochlauer , Wolfgang Skranc , Herbert Mayrhofer , Irma Wirth , Rudolf Neuhofer
发明人： Helmut Schwab , Anton Glieder , Christoph Kratky , Ingrid Dreveny , Rodolfo Bona , Peter Pochlauer , Wolfgang Skranc , Herbert Mayrhofer , Irma Wirth , Rudolf Neuhofer
IPC分类号： C12N15/09 , C07K19/00 , C12N9/04 , C12N9/88 , C12N15/52 , C12N15/60 , C12P13/00 , C07H21/04 , C12N5/04 , C12N15/82
CPC分类号： C12P13/004 , C12N9/88 , C12N15/52
摘要： New genes containing a DNA sequence coding for hydroxynitrile lyase, which genes can be prepared via a primer combination based on the DNA sequence of the 5″-region of the mdl genes from the Prunus serotina and from Prunus amygdalus and/or a primer 2 based on the 3′-region of the DNA sequences of one of the hydroxynitrile lyase isoenzymes from Prunus serotina or from Prunus amygdalus, subsequent amplification with a DNA polymerase using a DNA from organisms, containing genes coding for hydroxynitrile lyase, as templates and cloning, and also recombinant proteins which can be prepared in suitable host cells by heterologous expression of the DNA sequence of said HNL genes, and proteins and fusion proteins derived therefrom and use of said proteins for preparing (R)- or (S)-cyanohydrins.
摘要翻译：含有编码羟基腈裂解酶的DNA序列的新基因，该基因可以通过引物组合基于来自蜜梅属和来自杏仁核的md1基因的5'区域的DNA序列和/或引物2 基于来自山梨果皮或杏仁杏仁的羟基腈裂解酶同工酶之一的DNA序列的3'区域，随后使用含有编码羟基腈裂解酶的基因的生物体的DNA作为模板和克隆用DNA聚合酶进行扩增，以及可以通过异源表达所述HNL基因的DNA序列以及从其衍生的蛋白质和融合蛋白质以及所述蛋白质用于制备（R） - 或（S） - 氰基醇的方法，在合适的宿主细胞中制备的重组蛋白质。

7. 发明申请

US20100305325A1 PROCESS FOR THE PREPARATION OF AN ENANTIOMERIC TRISUBSTITUTED 3,4-DIHYDRO-ISOQUINOLINE DERIVATIVE 有权
标题翻译：制备三羟甲基丙酮衍生物的方法
公开(公告)号：US20100305325A1
公开(公告)日：2010-12-02
申请号：US12810176
申请日：2008-12-23
申请人： Erhard Bappert , Andreas Hendrikus Maria De Vries , Doris Domin , Matthias Helms , Christoph Imboden , Zarghun Nazir , Wolfgang Skranc , Felix Spindler , Michael Stanek , Wilhelm Tschebull , Gerardus Karel Maria Verzijl
发明人： Erhard Bappert , Andreas Hendrikus Maria De Vries , Doris Domin , Matthias Helms , Christoph Imboden , Zarghun Nazir , Wolfgang Skranc , Felix Spindler , Michael Stanek , Wilhelm Tschebull , Gerardus Karel Maria Verzijl
IPC分类号： C07D217/20
CPC分类号： C07D217/02
摘要： The present invention relates to a process for the preparation of the compound of formula (7) which process comprises the hydrogenation of the compound of formula (4) using bis[chloro-1,5-cyclooctadiene-iridium], (S)-i-dicyclohexylphosphino-2-[(S)-α-(dimethylamino)-2-(dicyclohexylphosphino)benzyl]-ferrocene as a catalyst.
摘要翻译：本发明涉及制备式（7）化合物的方法，该方法包括使用双[氯-1,5-环辛二烯 - 铱]，（S）-i 二环己基膦基-2 - [（S）-α-（二甲基氨基）-2-（二环己基膦基）苄基] - 二茂铁作为催化剂。

8. 发明申请

US20100143981A1 WHOLE-CELL CATALYTIC SYSTEM COMPRISING A HYDANTOINASE, A RACEMASE AND A CARBAMOYLASE 审中-公开
标题翻译：包含HYDANTOINASE，RACEMASE和CARBAMOYLASE的全细胞催化体系
公开(公告)号：US20100143981A1
公开(公告)日：2010-06-10
申请号：US12517504
申请日：2007-12-04
申请人： Monika Rusnak-Müller , Oliver May , Petrus Johannes Hermsen , Henricus Martinus Maria Gerardus Straatman , Wolfgang Skranc , Wilhelmus Hubertus Joseph Boesten , Dannis Heemskerk , Ben De Lange , Georgios Sarakinos
发明人： Monika Rusnak-Müller , Oliver May , Petrus Johannes Hermsen , Henricus Martinus Maria Gerardus Straatman , Wolfgang Skranc , Wilhelmus Hubertus Joseph Boesten , Dannis Heemskerk , Ben De Lange , Georgios Sarakinos
IPC分类号： C12P13/04 , C12N1/21 , C12N15/74 , C07D233/72 , C07C205/01
CPC分类号： C12P13/04 , C07C229/30 , C07C229/32 , C07C2601/08 , C07C2601/10 , C07C2601/14 , C07C2601/16 , C07D233/74 , C07D233/78 , C12P13/22 , C12P13/222 , C12P17/10 , C12P41/00 , C12P41/009
摘要： The present invention relates to a whole cell catalytic system for the preparation of an enantiomerically enriched α-amino acid from a corresponding hydantoin wherein hydantoinase, L-carbamoylase and hydantoin racemase are coexpressed in a recombinant micro-organism wherein the genes coding for these three enzymes are located on a single replicon. The present invention further relates to the use of such a whole cell catalytic system according in the preparation of an enantiomerically enriched L-α-amino acid from a corresponding hydantoin.
摘要翻译：本发明涉及一种用于从相应的乙内酰脲制备对映异构体富集的α-氨基酸的全细胞催化体系，其中将乙内酰脲酶，L-氨基甲酰基酶和乙内酰脲消旋酶共表达于重组微生物中，其中编码这三种酶的基因位于单个复制器上。本发明还涉及根据从对应的乙内酰脲制备对映体富集的L-α-氨基酸的这种全细胞催化体系的用途。

9. 发明申请

US20100113778A1 PROCESS FOR PREPARING O-CHLOROMETHYLPHENYLGLYOXYLIC ESTERS, IMPROVED PROCESS FOR PREPARING (E)-2-(2-CHLOROMETHYLPHENYL)-2-ALKOXIMINOACETIC ESTERS, AND NOVEL INTERMEDIATES FOR THEIR PREPARATION 审中-公开
标题翻译：制备O-氯代苯乙酰氧基酯的方法，（E）-2-（2-氯甲基苯基）-2-烷氧基亚胺酸酯的改进方法及其制备的新型中间体
公开(公告)号：US20100113778A1
公开(公告)日：2010-05-06
申请号：US12595113
申请日：2008-04-10
申请人： John-Matthias Wiegand , Karsten Luettgen , Wolfgang Skranc
发明人： John-Matthias Wiegand , Karsten Luettgen , Wolfgang Skranc
IPC分类号： C07D265/30 , C07C229/34 , C07C69/635 , C07C237/20
CPC分类号： C07F3/003 , C07B49/00 , C07C67/307 , C07C249/12 , C07C69/736 , C07C251/48
摘要： An improved process for preparing o-chloromethylphenylglyoxylic esters of the formula which comprises converting a compound of the formula by reaction with magnesium into the corresponding Grignard reagent which is then reacted with a compound of the formula to give the compound of the formula which is then cleaved by reaction with a chloroformic ester of the formula CICOOR4 or by reaction with phosgene to give the compound of the formula (I), followed by the isolation of the compound of the formula (I), and also an improved process for preparing (E)-2-(2-chloromethylphenyl)-2-alkoximinoacetic esters of the formula and intermediates for their preparation.
摘要翻译：一种制备下式的邻氯甲基苯基乙醛酸酯的改进方法，其包括将下式化合物与镁反应转化成相应的格氏试剂，然后与下式化合物反应，得到下式的化合物，然后将其分解通过与式CICOOR4的氯甲酸酯反应或通过与光气反应得到式（I）化合物，然后分离式（I）化合物，以及制备（E）化合物的改进方法， -2-（2-氯甲基苯基）-2-肟基乙酸酯及其制备中间体。

10. 发明授权

US08642312B2 Polypeptide having esterase activity and recombinant esterase and use thereof 有权
标题翻译：具有酯酶活性的多肽和重组酯酶及其用途
公开(公告)号：US08642312B2
公开(公告)日：2014-02-04
申请号：US13417734
申请日：2012-03-12
申请人： Gerhard Steinbauer , Micheal Stanek , Peter Pojarliev , Wolfgang Skranc , Helmut Schwab , Joannes Kierkels , Marcel Wubbolts , Harald Pichler , Manuela Hermann , Christoph Zenzmaier
发明人： Gerhard Steinbauer , Micheal Stanek , Peter Pojarliev , Wolfgang Skranc , Helmut Schwab , Joannes Kierkels , Marcel Wubbolts , Harald Pichler , Manuela Hermann , Christoph Zenzmaier
IPC分类号： C12N9/18
CPC分类号： C12N9/18 , C12P7/02 , C12P41/005
摘要： Polypeptide and recombinant protein having esterase activity which exhibit the amino acid sequence SEQ. ID. No. 1 and the use thereof.
摘要翻译：多肽和具有酯酶活性的重组蛋白质，其表现出氨基酸序列SEQ。 ID。 1及其用途。

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