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1. 发明专利

JP2015012838A 光学活性アミノ酸の製造法审中-公开
标题翻译：生产光活性氨基酸的方法
公开(公告)号：JP2015012838A
公开(公告)日：2015-01-22
申请号：JP2013141914
申请日：2013-07-05
申请人：株式会社カネカ , Kaneka Corp
发明人： NOJIRI MASUTOSHI , YOSHIDA AYA , HIRAI YOSHINORI , KAWANO SHIGERU , NISHIYAMA AKIRA , YASOHARA YOSHIHIKO
IPC分类号： C12P13/08
摘要：【課題】医薬品中間体として有用な光学活性イソバリンの高光学純度で製造する方法を提供する。【解決手段】入手容易な2-エチル-2-メチルマロン酸ジエステルから高光学純度の2-エチル-2-メチルマロン酸モノエステルに変換可能な酵素源、または2-エチル-2-メチルマロン酸ジアミドから高光学純度の2-エチル-2-メチルマロン酸モノアミドに変換可能な酵素源を取得する。各酵素源を用いた反応後、更にホフマン転位反応等により光学活性イソバリンの製造が可能となる。【選択図】なし
摘要翻译：要解决的问题：提供可用作具有高光学纯度的药物中间体的光学活性异缬氨酸的方法。溶解：从可得到的2-乙基-2-甲基丙二酸二酯转化成2-乙基-2-甲基丙二酸单酯的酶源或者从2-乙基-2-甲基丙二酸二酰胺转化成具有高光学纯度的2-乙基-2-甲基丙二酸单酰胺的酶源。通过在使用每种酶源的反应之后进一步进行霍夫曼重排反应等可以制备光学活性异缬氨酸。

2. 发明专利

JP2013046572A Method for producing optically active 2-hydroxycycloalkanecarboxylic acid ester 审中-公开
标题翻译：生产光学活性2-羟基环烷酮羧酸酯的方法
公开(公告)号：JP2013046572A
公开(公告)日：2013-03-07
申请号：JP2009278626
申请日：2009-12-08
申请人： Kaneka Corp , 株式会社カネカ
发明人： KAWANO SHIGERU , TANAKA TATSUYOSHI , NISHIYAMA AKIRA , YASOHARA YOSHIHIKO , KITA KEIKO
IPC分类号： C12P41/00 , C07B53/00 , C07C209/56 , C07C209/58 , C07C215/44 , C07C231/02 , C07C231/24 , C07C235/40 , C12N1/15 , C12N1/19 , C12N1/21 , C12N5/10 , C12N9/04 , C12N15/09 , C12P7/62
CPC分类号： C07C209/56 , C07B53/00 , C07C209/58 , C07C231/02 , C07C231/24 , C12N9/0006 , C12P7/62 , C07C235/40 , C07C215/44
摘要： PROBLEM TO BE SOLVED: To provide an efficient industrial production method of an optically active 2-hydroxycycloalkanecarboxylic acid ester useful as an intermediate for a pharmaceutical product.SOLUTION: The optically active 2-hydroxycycloalkanecarboxylic acid ester is produced by treating a 2-oxocycloalkanecarboxylic acid ester with a polypeptide, an organism that produces the polypeptide or a processed product of the organism to cause reduction. The polypeptide is derived from a microorganism selected from the group consisting of genera Candida, Rhodotorula, Devosia, Ogataea, Brevundimonas, Lactobacillus, Thermoanaerobium, Rhodococcus, Sporobolomyces and Sporidiobolus.
摘要翻译：要解决的问题：提供可用作药物产品中间体的光学活性2-羟基环烷烃羧酸酯的高效工业化生产方法。解决方案：光学活性的2-羟基环烷烃羧酸酯是通过用多肽，产生多肽的生物体或生物体的加工产物来处理2-氧代环烷烃羧酸酯来产生还原的。多肽衍生自选自念珠菌属，红酵母属，杜鹃属，Ogataea属，Brevundimonas，乳杆菌属，热厌氧菌属，红球菌属，孢子孢菌属和孢子虫属的微生物。版权所有（C）2013，JPO＆INPIT

3. 发明专利

JP2010037206A Method for producing optically active o-methylserine or its salt 审中-公开
标题翻译：用于生产光学活性的O-甲基或其盐的方法
公开(公告)号：JP2010037206A
公开(公告)日：2010-02-18
申请号：JP2008197987
申请日：2008-07-31
申请人： Kaneka Corp , 株式会社カネカ
发明人： NISHIYAMA AKIRA
IPC分类号： C07C227/30 , C07B53/00 , C07C227/18 , C07C227/34 , C07C229/22
摘要： PROBLEM TO BE SOLVED: To provide a method for producing O-methylserine or its salt useful as an intermediate of medicines from a readily available starting material and using a low-cost reagent, which method can easily and efficiently be practiced in an industrial scale. SOLUTION: Optically active O-methylserine or its salt is prepared by subjecting a readily available optically-active N,N-dibenzylserine to O-methylation, hydrolyzing the reaction product depending on the need therefor, and further debenzylating the reaction product. Thereby, O-methylserine or its salt can efficiently be produced. COPYRIGHT: (C)2010,JPO&INPIT
摘要翻译：待解决的问题：提供一种生产O-甲基丝氨酸或其盐，其可用于从容易获得的原料中使用的药物中间体并使用低成本试剂，该方法可以容易且有效地在工业规模。解决方案：通过使易于获得的光学活性N，N-二苄基丝氨酸进行O-甲基化，根据需要水解反应产物，并进一步对反应产物进行脱苄基，制备光学活性的O-甲基丝氨酸或其盐。由此可以有效地制造O-甲基丝氨酸或其盐。版权所有（C）2010，JPO＆INPIT

4. 发明专利

JP2013173677A Method for producing (1r,2s)-1-amino-2-vinyl cyclopropane carboxylic acid ester 审中-公开
标题翻译：（1R，2S）-1-氨基-2-乙烯基环丙烷羧酸酯的制备方法
公开(公告)号：JP2013173677A
公开(公告)日：2013-09-05
申请号：JP2010136377
申请日：2010-06-15
申请人： Kaneka Corp , 株式会社カネカ
发明人： TANAKA TATSUYOSHI , NISHIYAMA AKIRA
IPC分类号： C07C227/42 , C07B57/00 , C07C229/48
CPC分类号： C07C227/34 , C07B57/00 , C07B2200/07 , C07C2601/02 , C07C229/48
摘要： PROBLEM TO BE SOLVED: To provide a method for inexpensively and efficiently producing a (1R,2S)-1-amino-2-vinyl cyclopropane carboxylic acid ester, which is useful as a pharmaceutical intermediate.SOLUTION: A (1R,2S)-1-amino-2-vinyl cyclopropane carboxylic acid ester derivative having improved optical purity is produced by forming a salt from an optically active carboxylic acid and a 1-amino-2-vinyl cyclopropane carboxylic acid ester in a racemic form or having a low optical purity, and precipitating the salt in a solid form from a solvent.
摘要翻译：要解决的问题：提供廉价有效地制备可用作药物中间体的（1R，2S）-1-氨基-2-乙烯基环丙烷羧酸酯的方法。溶液：A（1R，2S） - 具有光学纯度的改进的1-氨基-2-乙烯基环丙烷羧酸酯衍生物是由外消旋形式的光学活性羧酸和1-氨基-2-乙烯基环丙烷羧酸酯形成的盐或具有低光学性纯度，并从溶剂中沉淀出固体形式的盐。

5. 发明专利

JP2013136632A Method for producing optically active 3-aminopiperidine or salt thereof 有权
标题翻译：用于生产光学活性的3-氨基哌啶或其盐的方法
公开(公告)号：JP2013136632A
公开(公告)日：2013-07-11
申请号：JP2013060990
申请日：2013-03-22
申请人： Kaneka Corp , 株式会社カネカ
发明人： MORI KOHEI , NOJIRI MASUTOSHI , NISHIYAMA AKIRA , TAOKA NAOAKI
IPC分类号： C07D211/56 , C07D211/60 , C12P41/00
CPC分类号： C07D211/60 , C07B57/00 , C07D211/56 , C12P17/12 , C12P41/006
摘要： PROBLEM TO BE SOLVED: To provide a method which can easily produce an optically active 3-amino piperidine or a salt thereof useful as a pharmaceutical intermediate from an inexpensive and easily available starting material and is practical for industrial production thereof, and to provide the intermediate useful for producing the optically active 3-amino piperidine or the salt thereof.SOLUTION: The method for producing the optically active 3-aminopiperidine or salt thereof includes: a process of stereoselectively hydrolyzing a racemic nipecotamide to convert into an optically active nipecotamide and an optically active nipecotic acid in the presence of an enzyme source derived from microorganism; and a process of subsequently subjecting the optically active nipecotamide to aroylation, Hofmann rearrangement, protection of amino groups and deprotection, and deriving the optically active nipecotamide into the optically active aminopiperidine or the salt thereof, or subjecting the optically active nipecotamide to selective protection with BOC (t-botoxycarbonyl), Hofmann rearrangement and deprotection and, thereby, deriving the optically active nipecotamide into the optically active aminopiperidine or the salt thereof. The optically active 3-aminopiperidine or the salt thereof useful as the pharmaceutical intermediate can be produced by an easy method applicable for industrial production from easily available starting material. Further, the intermediate useful for the production method is provided.
摘要翻译：要解决的问题：提供一种可以从廉价且容易获得的原料容易地制备用作药物中间体的光学活性3-氨基哌啶或其盐的方法，并且其实用于其工业生产，并提供中间体可用于制备光学活性3-氨基哌啶或其盐。解决方案：用于制备光学活性3-氨基哌啶或其盐的方法包括：立体选择性水解外消旋哌啶甲酰胺以转化为光学活性的夹螺旋体和光学上的方法在源自微生物的酶源存在下的活性乳酸; 以及随后对光学活性的nipecotamide进行丙烯酰化，霍夫曼重排，保护氨基和去保护的步骤，以及将光学活性的nipecotamide导出到光学活性氨基哌啶或其盐中，或者使光学活性的哌啶甲酰胺与BOC （叔丁氧基羰基），霍夫曼重排和去保护，从而将光学活性的哌甲酰胺衍生成光学活性氨基哌啶或其盐。可用作药物中间体的光学活性3-氨基哌啶或其盐可以通过易于获得的起始原料通过适用于工业生产的容易的方法制备。此外，提供了可用于生产方法的中间体。

6. 发明专利

JP2013074811A Method for producing optically active 1-substituted tetrahydroisoquinoline derivative 审中-公开
标题翻译：用于生产光学活性的1-取代的四氢喹啉衍生物的方法
公开(公告)号：JP2013074811A
公开(公告)日：2013-04-25
申请号：JP2011215407
申请日：2011-09-29
申请人： Kaneka Corp , 株式会社カネカ
发明人： NISHIHACHIJO MASAKATSU , KAWANO SHIGERU , HIRAI YOSHINORI , NISHIYAMA AKIRA , MINAMI HIROMICHI , KATAYAMA TAKANE , KUMAGAI HIDEHIKO
IPC分类号： C12P17/10 , C12N9/88 , C12N15/09
CPC分类号： Y02P20/52
摘要： PROBLEM TO BE SOLVED: To provide an efficient method for producing an optically active 1-substituted tetrahydroisoquinoline derivative by enzyme reaction.SOLUTION: In the method, the optically active 1-substituted tetrahydroisoquinoline derivative is efficiently produced by stereoselective condensing reaction by allowing an enzyme to act upon aromatic aldehyde or alkylaldehyde having long alkyl side chains and a 2-(3-hydroxyphenyl) ethylamine derivative.
摘要翻译：要解决的问题：提供通过酶反应制备光学活性1-取代的四氢异喹啉衍生物的有效方法。解决方案：在该方法中，通过使酶作用于具有长烷基侧链的芳族醛或烷基醛和2-（3-羟基苯基）乙胺，通过立体选择性缩合反应有效地制备光学活性1-取代的四氢异喹啉衍生物衍生物。版权所有（C）2013，JPO＆INPIT

7. 发明专利

JP2012224606A Production method of 4,4,4-trifluoro-1-butanol 审中-公开
标题翻译： 4,4,4-三氟-1-丁醇的生产方法
公开(公告)号：JP2012224606A
公开(公告)日：2012-11-15
申请号：JP2011096437
申请日：2011-04-22
申请人： Kaneka Corp , 株式会社カネカ
发明人： YOSHIDA FUMI , HIRAI YOSHINORI , NISHIYAMA AKIRA
IPC分类号： C07C29/147 , C07C31/38
摘要： PROBLEM TO BE SOLVED: To provide a method for efficiently producing 4,4,4-trifluoro-1-butanol without a complicated operation.SOLUTION: The method comprises reacting hydrogenated boron metal in 1.0 or more equivalent with 4,4,4-trifluorocrotonic acid ester (1) as a starting material in an alcohol solvent, and then hydrolyzing the reaction liquid and distilling the hydrolyzed liquid to produce 4,4,4-trifluoro-1-butanol (2). In formula (1), R represents an alkyl group having 1 to 12 carbon atoms, alkenyl group having 2 to 12 carbon atoms, aralkyl group having 7 to 12 carbon atoms or aryl group having 6 to 12 carbon atoms.
摘要翻译：待解决的问题：提供一种有效地生产4,4,4-三氟-1-丁醇的方法，而不需要复杂的操作。解决方案：该方法包括将1.0当量以上的氢化硼金属与作为原料的4,4,4-三氟巴豆酸酯（1）在醇溶剂中反应，然后水解反应液体并蒸馏出水解液得到4,4,4-三氟-1-丁醇（2）。式（1）中，R表示碳原子数1〜12的烷基，碳原子数2〜12的烯基，碳原子数7〜12的芳烷基或碳原子数6〜12的芳基。版权所有（C）2013，JPO＆INPIT

8. 发明专利

JP2011042660A Method for producing optically active 1-substituted-2-methylpyrrolidine and intermediate of the same 审中-公开
标题翻译：生产光学活性的1-取代-2-甲基吡咯烷的方法及其中间体
公开(公告)号：JP2011042660A
公开(公告)日：2011-03-03
申请号：JP2010216556
申请日：2010-09-28
申请人： Kaneka Corp , 株式会社カネカ
发明人： NISHIYAMA AKIRA , TAOKA NAOAKI , KISHIMOTO SHIGEMI , NAGASHIMA NOBUO
IPC分类号： C07C29/143 , C07C31/20 , C07C303/28 , C07C309/66 , C12N15/53 , C12P7/18 , C12P11/00 , C12P17/10
CPC分类号： C12P17/10 , C07C303/28 , C12P7/18 , C12P11/00 , C07C309/66
摘要： PROBLEM TO BE SOLVED: To provide a method for producing easily and inexpensively an optically active 1,4-pentanediol and an optically active 1-substituted 2-methylpyrrolidine useful as an intermediate for medicines or an intermediate for agricultural chemicals from an inexpensive and easily-available starting material. SOLUTION: An optically active 1,4-pentanediol is produced by asymmetrically reducing inexpensively available 5-hydroxy-2-pentanone. An optically active 1-substituted-2-methylpyrrolidine is produced by further sulfonylating the optically active 1,4-pentanediol to convert it to an optically active sulfonate compound and subsequently reacting the compound with an amine. COPYRIGHT: (C)2011,JPO&INPIT
摘要翻译：要解决的问题：提供一种容易且廉价地制备光学活性的1,4-戊二醇和用作药物中间体的光学活性1-取代的2-甲基吡咯烷或农药中间体的方法，其价格低廉和容易获得的起始材料。解决方案：通过不对称地还原廉价的5-羟基-2-戊酮来制备光学活性的1,4-戊二醇。通过进一步磺酰化光学活性的1,4-戊二醇以将其转化为光学活性的磺酸盐化合物并随后使该化合物与胺反应来制备光学活性的1-取代-2-甲基吡咯烷。版权所有（C）2011，JPO＆INPIT

9. 发明专利

JP2010095453A Method for producing optically active 1-aryl-3-pyrrolidinol 审中-公开
标题翻译：用于生产光学活性的1-芳基-3-吡咯烷醇的方法
公开(公告)号：JP2010095453A
公开(公告)日：2010-04-30
申请号：JP2008265326
申请日：2008-10-14
申请人： Kaneka Corp , 株式会社カネカ
发明人： ONUKI MASATOSHI , NISHIYAMA AKIRA
IPC分类号： C07D207/08 , C07B61/00 , C07D207/12 , C07D207/14
摘要： PROBLEM TO BE SOLVED: To provide a method for readily producing an optically active 1-aryl-3-pyrrolidinol or a salt thereof, useful as an intermediate of a medicine without carrying out complicated operation from an inexpensive general-purpose starting raw material. SOLUTION: The method for producing the optically active 1-aryl-3-pyrrolidinol or the salt thereof includes reacting an aniline compound and hydrogen with an easily available optically active 4-substituted-3-hydroxybutyronitrile in the presence of a metal catalyst. The optically active 1-aryl-3-substituted pyrrolidine and the optically active 3-substituted pyrrolidine can readily and efficiently be obtained from the optically active 1-aryl-3-pyrrolidinol. COPYRIGHT: (C)2010,JPO&INPIT
摘要翻译：待解决的问题：提供一种容易地制备光学活性1-芳基-3-吡咯烷醇或其盐的方法，其不用从廉价的通用起始原料进行复杂的操作用作药物的中间体材料。解决方案：制备光学活性1-芳基-3-吡咯烷醇或其盐的方法包括使苯胺化合物和氢与容易获得的光学活性4-取代-3-羟基丁腈在金属催化剂存在下反应。光学活性1-芳基-3-取代的吡咯烷和光学活性3-取代的吡咯烷可以从光学活性1-芳基-3-吡咯烷醇中容易且有效地得到。版权所有（C）2010，JPO＆INPIT

10. 发明专利

JP2013209424A Intermediate of optically active 3-amino-2-hydroxypropionic acid cyclopropylamide derivative or salt thereof 有权
标题翻译：光活性3-氨基-2-羟基丙酸酰基环丙酰胺衍生物或其盐的中间体
公开(公告)号：JP2013209424A
公开(公告)日：2013-10-10
申请号：JP2013127772
申请日：2013-06-18
申请人： Kaneka Corp , 株式会社カネカ
发明人： MORI KOHEI , NISHIYAMA AKIRA , TAOKA NAOAKI , MORIYAMA DAISUKE , NAGASHIMA NOBUO
IPC分类号： C07D263/16 , C07B53/00 , C07C67/31 , C07C69/675 , C07C237/06 , C07D303/48 , C12P41/00
CPC分类号： C07B53/00 , C07B2200/07 , C07C67/31 , C07C231/18 , C07C237/04 , C07C237/22 , C07C2601/02 , C07D263/16 , C07D301/24 , C07D303/16 , C07D303/48 , C12P7/42 , C12P13/02 , C12P41/002 , C07C69/675
摘要： PROBLEM TO BE SOLVED: To provide a practical process for industrial production of an optically active 3-amino-2-hydroxypropionic acid cyclopropylamide derivative or a salt thereof useful as an intermediate of a medicine from a low cost and easily obtainable raw material, and useful intermediates thereof.SOLUTION: At first, an optically active epoxycarboxylic acid derivative is produced by an asymmetric reduction of an easily available 2-halo-3-oxopropionic acid derivative, followed by epoxidation of the resulting substance. Then, the optically active epoxycarboxylic acid derivative is reacted with cyclopropylamine to convert it into an optically active epoxyamide derivative, which derivative is then reacted with a nitrile to produce an optically active oxazolinamide derivative. Subsequently, an optically active 3-amino-2-hydroxypropionic acid cyclopropylamide derivative or a salt thereof is produced by a selective acid solvolysis of the oxazoline skeleton.
摘要翻译：要解决的问题：提供从低成本和容易获得的原料中用作药物中间体的光学活性3-氨基-2-羟基丙酸环丙基酰胺衍生物或其盐的工业生产的实用方法，并且可用其中间体。解决方案：首先，通过不容易获得的2-卤代-3-氧代丙酸衍生物的不对称还原产生光学活性环氧羧酸衍生物，然后进行所得物质的环氧化。然后，将光学活性环氧羧酸衍生物与环丙胺反应，将其转化为光学活性环氧酰胺衍生物，然后将该衍生物与腈反应，生成光学活性的恶唑啉酰胺衍生物。随后，通过恶唑啉骨架的选择性酸溶剂解产生光学活性3-氨基-2-羟基丙酸环丙基酰胺衍生物或其盐。

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