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1. 发明授权

US5610312A Asymmetric hydrogenation of dihydrofuroimidazole derivatives 失效
标题翻译：二氢呋喃咪唑衍生物的不对称氢化
公开(公告)号：US5610312A
公开(公告)日：1997-03-11
申请号：US502267
申请日：1995-07-13
申请人： Martin Eyer , Rudolf Fuchs , John McGarrity
发明人： Martin Eyer , Rudolf Fuchs , John McGarrity
IPC分类号： B01J31/24 , C07D491/04 , C07D491/048 , C07F9/50 , C07F15/00 , C07D235/02 , C07D403/02 , C07D495/04 , B01J27/105
CPC分类号： C07D491/04 , Y02P20/55
摘要： A process for the asymmetric hydrogenation of the furoimidazole derivatives of the general formula: ##STR1## wherein R.sub.1 is a protective group, which is cleavable in a known way, and R.sub.2 is hydrogen or a protective group, which is cleavable in a known way, with hydrogen in the presence of a homogeneous catalyst to the corresponding diastereomeric tetrahydrofuroimidazole derivatives of the general formula: ##STR2## The tetrahydrofuroimidazole derivatives of the general formula II are intermediate products for the production of vitamin (+) biotin.
摘要翻译：用于以下通式的呋喃咪唑衍生物的不对称氢化的方法：其以已知的方式可切割，并且R 2是氢或保护基团，其可以以已知方式与氢气在均相催化剂存在下裂解通式Ⅱ的相应的非对映异构体四氢呋喃咪唑衍生物：通式Ⅱ的四氢呋喃并咪唑衍生物是用于生产维生素（+）生物素的中间产物。

2. 发明授权

US5087760A Process for the production of 1,3-cyclopentanedione 失效
标题翻译：生产1,3-环戊二烯的方法
公开(公告)号：US5087760A
公开(公告)日：1992-02-11
申请号：US460658
申请日：1990-01-03
申请人： Rudolf Fuchs , John McGarrity
发明人： Rudolf Fuchs , John McGarrity
IPC分类号： C07C45/54 , C07C45/51 , C07C45/67 , C07C49/395 , C07C49/597 , C07C69/734
CPC分类号： C07C45/673
摘要： A process for the production of 1,3-cyclopentanedione, which is a versatile intermediate product for numerous active ingredient syntheses. For this purpose, a malonic acid ester is reacted with a haloalkoxybutenoic acid ester, the resultant bis-(alkoxycarbonyl) alkoxypentenoic acid ester is cyclized to alkoxycarbonyl alkoxycyclopentenone, the ester function is saponified, and finally the intermediate is decarboxylated to the end product.
摘要翻译：一种生产1,3-环戊二酮的方法，它是多种活性成分合成的通用中间产物。为此，将丙二酸酯与卤代烷氧基丁烯酸酯反应，得到的双（烷氧基羰基）烷氧基戊烯酸酯环化为烷氧基羰基烷氧基环戊烯酮，酯官能团皂化，最后将中间体脱羧至终产物。

3. 发明授权

US5756756A Asymmetric hydrogenation of dihyrofuroimidazole derivatives 失效
标题翻译：二氟呋喃咪唑衍生物的不对称氢化
公开(公告)号：US5756756A
公开(公告)日：1998-05-26
申请号：US898119
申请日：1997-07-22
申请人： Martin Eyer , Rudolf Fuchs , John McGarrity
发明人： Martin Eyer , Rudolf Fuchs , John McGarrity
IPC分类号： B01J31/24 , C07D491/04 , C07D491/048 , C07F9/50 , C07F15/00
CPC分类号： C07D491/04 , Y02P20/55
摘要： A process for the asymmetric hydrogenation of the furoimidazole derivatives of the general formula: ##STR1## wherein R.sub.1 is a protective group, which is cleavable in a known way, and R.sub.2 is hydrogen or a protective group, which is cleavable in a known way, with hydrogen in the presence of a homogeneous catalyst to the corresponding diastereomeric tetrahydrofuroimidazole derivatives of the general formula: ##STR2## The tetrahydrofuroimidazole derivatives of the general formula II are intermediate products for the production of vitamin (+) biotin.
摘要翻译：用于以下通式的呋喃咪唑衍生物的不对称氢化的方法：其以已知的方式可切割，并且R 2是氢或保护基团，其可以以已知方式与氢气在均相催化剂存在下裂解相应的具有以下通式的非对映异构体四氢呋喃咪唑衍生物：通式II的四氢呋喃并咪唑衍生物是用于生产维生素（+）生物素的中间产物。

4. 发明授权

US5451684A Asymmetric hydrogenation of furoimidazole derivatives 失效
标题翻译：呋喃咪唑衍生物的不对称氢化
公开(公告)号：US5451684A
公开(公告)日：1995-09-19
申请号：US239588
申请日：1994-05-09
申请人： John McGarrity , Felix Spindler , Rudolf Fuchs , Martin Eyer
发明人： John McGarrity , Felix Spindler , Rudolf Fuchs , Martin Eyer
IPC分类号： B01J31/24 , C07B53/00 , C07B61/00 , C07D491/04 , C07D491/048
CPC分类号： C07D491/04 , Y02P20/55
摘要： A process for the asymmetric hydrogenation of furoimidazole derivatives of the general formula: ##STR1## wherein R.sub.1 is a protective group and R.sub.2 is hydrogen or a protective group, with hydrogen in the presence of a homogeneous catalyst to give the corresponding diastereomeric dihydrofuroimidazole derivatives of the general formula: ##STR2## The dihydrofuroimidazole derivatives of the general formula II are intermediates for the preparation of the vitamin (+)-biotin.
摘要翻译：一种通式为：其中R 1为保护基且R 2为氢或保护基的呋喃咪唑衍生物的不对称氢化方法，在均相催化剂存在下与氢气反应，得到相应的非对映异构二氢呋喃并咪唑衍生物通式II的二氢呋喃咪唑衍生物是制备维生素（+） - 生物素的中间体。

5. 发明授权

US5113012A Process for the production of 1,3-cyclopentanedione 失效
标题翻译：生产1,3-环戊二烯的方法
公开(公告)号：US5113012A
公开(公告)日：1992-05-12
申请号：US749984
申请日：1991-08-26
申请人： Rudolf Fuchs , John McGarrity
发明人： Rudolf Fuchs , John McGarrity
IPC分类号： C07C45/54 , C07C45/51 , C07C45/67 , C07C49/395 , C07C49/597 , C07C69/734
CPC分类号： C07C45/673
摘要： A process for the production of 1,3-cyclopentanedione, which is a versatile intermediate product for numerous active ingredient syntheses. For this purpose, a malonic acid ester is reacted with a haloalkoxybutenoic acid ester, the resultant bis-(alkoxycarbonyl)alkoxypentenoic acid ester is cyclized to alkoxycarbonyl alkoxycyclopentenone, the ester function is saponified, and finally the intermediate is decarboxylated to the end product.

6. 发明授权

US07973182B2 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：US07973182B2
公开(公告)日：2011-07-05
申请号：US10590140
申请日：2005-02-21
申请人： Dominique Michel , Hanspeter Mettler , John McGarrity
发明人： Dominique Michel , Hanspeter Mettler , John McGarrity
IPC分类号： C07D307/02 , C07D333/20
CPC分类号： C07C213/00 , C07B2200/07 , C07D333/22
摘要： A process for the preparation of enantiomerically pure 1-substituted-3-amino-alcohols, particularly of (S)-(−)- and (R)-(+)-3-N-methylamino-1-(2-thienyl)-1-propanol, by asymmetrically hydrogenating salts of a carboxylic acids with an aminoketone of the formula: wherein R1 is 2-thienyl, 2-furanyl or phenyl, each optionally substituted with one or more halogen atoms and/or one or more C1-4-alkyl or C1-4-alkoxy groups, and wherein R2 is C1-4-alkyl or phenyl, each optionally substituted with one or more halogen atoms and/or one or more C1-4-alkyl or C1-4-alkoxy groups. The corresponding aminoalcohols are obtained by subsequent hydrolysis of their salts. Salts of a carboxylic acid with the aminoketones and the aminoalcohols obtained by asymmetrically hydrogenating the aminoketones, respectively.
摘要翻译：制备对映体纯的1-取代-3-氨基醇，特别是（S） - （ - ） - 和（R） - （+） - 3-N-甲基氨基-1-（2-噻吩基） -1-丙醇，通过用下式的氨基酮不对称氢化羧酸盐：其中R1是2-噻吩基，2-呋喃基或苯基，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 - 烷氧基，并且其中R 2为C 1-4 - 烷基或苯基，各自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 - 烷氧基取代。相应的氨基醇通过其盐的水解得到。羧酸与通过不对称氢化氨基酮获得的氨基酮和氨基醇的羧酸盐。

7. 发明申请

US20090156833A1 Process for the Preparation of Enantiomerically Pure 1-Substituted-3-Aminoalcohols 有权
标题翻译：对映异构纯的1-取代的3-氨基醇的制备方法
公开(公告)号：US20090156833A1
公开(公告)日：2009-06-18
申请号：US11884542
申请日：2006-02-14
申请人： Walter Brieden , Martin Clausen , John McGarrity , Hanspeter Mettler , Colette Mettler , Dominique Michel
发明人： Walter Brieden , Martin Clausen , John McGarrity , Hanspeter Mettler , Colette Mettler , Dominique Michel
IPC分类号： C07D333/36
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：制备式（Ia），（Ib）的N-单取代的β-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和/ 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，每个芳基任选地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β （II）的氨基酮磺酸盐：其中R1，R2和R3如上定义，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。

8. 发明授权

US06248571B1 Method of producing dihydroxypyrimidine derivatives 失效
标题翻译：二羟基嘧啶衍生物的制备方法
公开(公告)号：US06248571B1
公开(公告)日：2001-06-19
申请号：US09029230
申请日：1998-02-25
申请人： Beat Schmidt , Andreas Kiener , John McGarrity
发明人： Beat Schmidt , Andreas Kiener , John McGarrity
IPC分类号： C12P1712
CPC分类号： C07D239/54 , C12P13/02
摘要： A process for the preparation of dihydroxypyrimidine derivatives of the general formula: in which R1 and R2 are identical or different and are a hydrogen atom, aryl group, or a C1-C4-alkyl group or an aryl group, starting from a compound of the general formula: in which R2 has the meaning mentioned above and R3 is —CN or COOR4, in which R4 is a C1-C4-alkyl group.
摘要翻译：制备以下通式的二羟基嘧啶衍生物的方法：其中R 1和R 2相同或不同，为氢原子，芳基或C 1 -C 4烷基或芳基，以通式：其中R 2具有上述含义，R 3是-CN或COOR 4，其中R 4是C 1 -C 4 - 烷基。

9. 发明授权

US5286650A Process for the production of optically-active 4-amino-3-hydroxycarboxylic acids 失效
标题翻译：用于制备光学活性4-氨基-3-羟基羧酸的方法
公开(公告)号：US5286650A
公开(公告)日：1994-02-15
申请号：US932587
申请日：1992-08-20
申请人： Markus Banziger , John McGarrity , Thomas Meul
发明人： Markus Banziger , John McGarrity , Thomas Meul
IPC分类号： C07C227/22 , C07C269/00 , C07D207/26 , C07D207/267 , C12P17/10 , C12P41/00 , C12P13/04
CPC分类号： C07D207/267 , C07C227/22 , C07C269/00 , C07D207/26 , C12P17/10 , C12P41/004 , Y02P20/55
摘要： Starting from 5-alkylidene or 5-benzylidenetetramic acid, optically-active 4-amino-3-hydroxy-carboxylic acids are produced in the (rel-3R,4R) configuration, especially statine. The synthesis process includes the O-acylation of the tetramic acid to the corresponding 4-acyloxy-3-pyrrolin-2-one, a stereoselective hydrogenation to (rel-4R,5R)-4-acyloxy-5-alkyl or 5-benzylpyrrolidin-2-one and an enantioselective enzymatic hydrolysis of the (4R,5R)-enantiomer to 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 optionally introduction of an amino protective 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 producible according to the invention are the structural elements of enzyme inhibitors.
摘要翻译：从5-亚烷基 - 或5-亚苄基四胺酸开始，制备（rel-3R，4R） - 构型中的光学活性的4-氨基-3-羟基羧酸，特别是他汀类。合成包括将四酸与相应的4-酰氧基-3-吡咯啉-2-酮的O-酰化反应，立体选择性氢化成（rel-4R，5R）-4-酰氧基-5-烷基 - 或-5 （4R，5R） - 对映体与对应的4-羟基吡咯烷-2-酮的对映选择性酶水解。通过水解裂解内酰胺环和酯官能团，并酌情将（氨基保护基）引入到（3S，4S）构型的目标化合物中，将未水解的对映异构体分离并转化。（3R，4R） - 对映体可类似地由酶水解的4-羟基吡咯烷-2-酮得到。根据本发明可制备的4-氨基-3-羟基羧酸是酶抑制剂的组分。

10. 发明授权

US4851540A Process for the production of biotin precursors 失效
标题翻译：生物素前体生产工艺
公开(公告)号：US4851540A
公开(公告)日：1989-07-25
申请号：US127052
申请日：1987-12-01
申请人： John McGarrity , Leander Tenud , Thomas Meul
发明人： John McGarrity , Leander Tenud , Thomas Meul
IPC分类号： C07D491/04 , C07D491/048 , C07D495/04
CPC分类号： C07D491/04 , C07D495/04 , Y02P20/55
摘要： Process for the production of imidazole derivatives of the formula: ##STR1## wherein R.sub.1 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, R.sub.2 is hydrogen, a substituted or unsubstituted alkanoyl group, an 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. A tetronic acid of the formula: ##STR2## wherein A has the above-mentioned meaning, is reacted with a diazonium salt, converting the resultant arylazotetronic acid or the tautomeric arylhydrazone in a further step with a chiral amine into an arylazoamino compound, reducing the arylazoamino compound, converting the resultant diamine, with phosgene or a phosgene-equivalent reagent, into the corresponding imidazole and optionally introducing a protective group by reaction with a substituted or unsubstituted aliphatic or aromatic acid chloride, an aliphatic or aromatic carboxylic acid anhydride, a haloformic acid alkyl ester, a 1-alkoxyalkyl halide, an enol ether, an aromatic or aliphatic sulfonic acid halide, a diarylphosphinic acid halide, a phosphoric acid dialkyl ester halide, a trialkyl silyl halide or a trialkyl silyl acetamide. These imidazole derivatives are suitable as intermediate products for the production of (+) biotin.
摘要翻译：制备下式的咪唑衍生物的方法：其中R1是（R） - 或（S）-1-苯基烷基，（R） - 或（S）-1-烷氧基羰基-1-苯基甲基基团或（R） - 或（S）-1-芳氧基羰基-1-苯基甲基，R2是氢，取代或未取代的烷酰基，未取代或取代的苯甲酰基，取代或未取代的苄基，烷氧基羰基基团和芳氧基羰基，烷氧基烷基，吡喃基，取代或未取代的苯磺酰基，烷基磺酰基，二芳基氧膦基，二烷氧基氧膦基或三烷基甲硅烷基，A是硫或氧原子。其中A具有上述含义的特丁酸与重氮盐反应，将得到的芳基氮杂过硫酸或互变异构芳基腙用手性胺转化成芳基偶氮氨基化合物，将还原芳基偶氮基氨基化合物，将所得二胺与光气或光气当量的试剂转化成相应的咪唑，并任选地通过与取代或未取代的脂族或芳族酰氯，脂族或芳族羧酸酐反应引入保护基，卤代甲酸烷基酯，1-烷氧基烷基卤化物，烯醇醚，芳族或脂族磺酸卤化物，二芳基次膦酸卤化物，磷酸二烷基酯卤化物，三烷基甲硅烷基卤化物或三烷基甲硅烷基乙酰胺。这些咪唑衍生物适用于生产（+）生物素的中间产物。

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