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1. 发明授权

EP1947083B1 PROCESS FOR PRODUCTION OF ARALKYLOXYPYRROLIDINE DERIVATIVE 有权转让
标题翻译：生产脂酰氧基吡咯烷衍生物的方法
公开(公告)号：EP1947083B1
公开(公告)日：2010-11-10
申请号：EP06796649.9
申请日：2006-08-22
申请人： Kaneka Corporation
发明人： TAKEDA, Toshihiro , OHNUKI, Masatoshi , KISHIMOTO, Narumi
IPC分类号： C07D207/12
CPC分类号： C07D207/12 , Y02P20/55
摘要： Disclosed is a process for production of an aralkyloxypyrrolidine derivative which is important for the production of a pharmaceutical or the like. A 3-aralkyloxypyrrolidine derivative can be produced in the form of a crystal by a process comprising reacting an N-protected-3-hydroxypyrrolidine with a halogenated aralkyl in the presence of a base and a metal halide and/or a phase transfer catalyst to give an N-protected-3-aralkyloxypyrrolidine, performing the deprotection of the N-protecting group in the product to give a 3-aralkyloxypyrrolidine derivative, and treating the product in a solvent containing a polar solvent. The process can produce a highly pure 3-aralkyloxypyrrolidine derivative in a simple manner, with good efficiency, and in an industrial scale.
摘要翻译：公开了一种生产药物等重要的芳烷氧基吡咯烷衍生物的方法。 3-芳烷氧基吡咯烷衍生物可以通过包括在碱和金属卤化物和/或相转移催化剂存在下使N-保护的-3-羟基吡咯烷与卤代芳烷基反应得到晶体形式，得到 N-保护的-3-芳烷氧基吡咯烷，对产物中的N-保护基进行脱保护得到3-芳烷氧基吡咯烷衍生物，并在含有极性溶剂的溶剂中处理产物。该方法可以以简单的方式高效纯化并以工业规模生产高纯度的3-芳烷氧基吡咯烷衍生物。

2. 发明授权

EP2423211B1 PROCESSES FOR PRODUCING (1S,6S)- OR (1R,6R)-CIS-2,8-DIAZABICYCLO[4.3.0]NONANE AND INTERMEDIATE THEREOF 有权
标题翻译：用于生产（1S，6S） - 或（1R，6R）CIS-2,8-二氮杂双环[4.3.0]壬烷和中间体
公开(公告)号：EP2423211B1
公开(公告)日：2014-04-16
申请号：EP10766836.0
申请日：2010-04-20
申请人： KANEKA CORPORATION
发明人： OHNUKI, Masatoshi , NISHIYAMA, Akira
IPC分类号： C07D471/04
CPC分类号： C07D471/04

3. 发明公开

EP2119709A1 METHOD FOR PRODUCING OPTICALLY ACTIVE 2-ARYLPIPERAZINE DERIVATIVE 审中-公开
标题翻译： VERFAHREN ZUR HERSTELLUNG EINES OPTISCH AKTIVEN 2-ARYLPIPERAZINDERIVATS
公开(公告)号：EP2119709A1
公开(公告)日：2009-11-18
申请号：EP08710788.4
申请日：2008-02-05
申请人： Kaneka Corporation
发明人： OHNUKI, Masatoshi , NISHIYAMA, Akira , MITSUDA, Masaru
IPC分类号： C07D241/04 , C07B53/00
CPC分类号： C07B53/00 , C07D241/04
摘要： The objective of the present invention is to produce an optically active 2-arylpiperazine derivative useful as a synthetic intermediate for pharmaceutical products and agricultural chemicals from inexpensive and readily available starting material by an industrially practicable method. The objective can be accomplished by treating an optically active substituted aminodiol derivative produced from an optically active styrene oxide derivative with a sulfonating agent in the presence of a base, and then reacting an amine compound to obtain the 2-arylpiperazine derivative. Especially, an optically active 1-unsubstituted-2-arylpiperazine derivative can be produced by treating an optically active 1-allyl-2-arylpiperazine derivative with water in the presence of a transition metal catalyst for deallylation.
摘要翻译：本发明的目的是通过工业上可行的方法从便宜且容易获得的原料制备用作药物产品和农药的合成中间体的光学活性2-芳基哌嗪衍生物。该目的可以通过在碱的存在下用磺化剂处理由光学活性苯乙烯氧化物衍生物制备的光学活性取代的氨基二醇衍生物，然后使胺化合物反应得到2-芳基哌嗪衍生物。特别地，光学活性的1-未取代-2-芳基哌嗪衍生物可以通过在过渡金属催化剂的存在下用水处理光学活性的1-烯丙基-2-芳基哌嗪衍生物来进行脱气。

4. 发明公开

EP2810933A1 METHOD FOR PRODUCING SOLID AMINO ACID 审中-公开
标题翻译：方法制备固体氨基
公开(公告)号：EP2810933A1
公开(公告)日：2014-12-10
申请号：EP13743938.6
申请日：2013-01-21
申请人： Kaneka Corporation
发明人： OHNUKI, Masatoshi , NISHIYAMA, Akira
IPC分类号： C07C227/42 , C07C229/06 , C07C229/08 , C07C229/12 , C07C229/32 , C07D207/16 , C07D211/60
CPC分类号： C07C227/18 , C07C227/42 , C07C2601/02 , C07D207/16 , C07D211/60 , C07C229/06 , C07C229/08 , C07C229/12 , C07C229/32 , C07C229/48
摘要： The problem to be solved by the present invention is to ea sily and efficiently produce an amino acid having 2 to 7 carbon atoms as a high-purity solid without complicated operation, whic h is useful as a synthetic intermediate for medicines or agroche micals.
The present invention is characterized in comprising a ste p of precipitating solid amino acid with high purity. In the pr esent invention, the by-produced salt composed of the sulfonic a cid and the amine was removed to the mother liquor by reacting a n amine with a sulfonic acid salt of amino acid in an aprotic pol ar solvent, or by reacting a sulfonic acid with an amine salt of amino acid in an aprotic polar solvent.
The sulfonic acid salt of amino acid, for example, may be produced by reacting a N-(tert-butoxycarbonyl) amino acid with a sulfonic acid, or by reacting an amino acid tert-butyl ester we th a sulfonic acid.

5. 发明公开

EP1947083A1 PROCESS FOR PRODUCTION OF ARALKYLOXYPYRROLIDINE DERIVATIVE 有权转让
标题翻译：生产脂酰氧基吡咯烷衍生物的方法
公开(公告)号：EP1947083A1
公开(公告)日：2008-07-23
申请号：EP06796649.9
申请日：2006-08-22
申请人： Kaneka Corporation
发明人： TAKEDA, Toshihiro , OHNUKI, Masatoshi , KISHIMOTO, Narumi
IPC分类号： C07D207/12
CPC分类号： C07D207/12 , Y02P20/55
摘要： The present invention provides a process for producing a 3-aralkyloxypyrrolidine derivative which is important for production of pharmaceutical products and the like. In the present invention, a N-protected-3-hydroxypyrrolidine is converted into a N-protected-3-aralkyloxypyrrolidine by allowing an aralkyl halide to act in the presence of a base and at least one of a metal halide and a phase-transfer catalyst followed by deprotecting a N-protecting group to convert it to a 3-aralkyloxypyrrolidine derivative and subsequently treating the derivative in a solvent containing a polar solvent, thereby obtaining the 3-aralkyloxypyrrolidine derivative as a crystal. According to the present invention, a 3-aralkyloxypyrrolidine derivative of high purity can be produced conveniently and efficiently on an industrial scale.
摘要翻译：本发明提供了一种生产药用产品等重要的3-芳烷氧基吡咯烷衍生物的方法。在本发明中，通过使芳烷基卤化物在碱的存在下和至少一种金属卤化物和相转移作用下将N-保护的-3-羟基吡咯烷转化为N-保护的-3-芳烷氧基吡咯烷然后去保护N-保护基团，将其转化为3-芳烷氧基吡咯烷衍生物，随后在含有极性溶剂的溶剂中处理衍生物，由此得到3-芳烷氧基吡咯烷衍生物的晶体。根据本发明，高纯度的3-芳烷氧基吡咯烷衍生物可以在工业规模上方便和有效地生产。

6. 发明公开

EP2423211A1 PROCESSES FOR PRODUCING (1S,6S)- OR (1R,6R)-CIS-2,8-DIAZABICYCLO[4.3.0]NONANE AND INTERMEDIATE THEREOF 有权
标题翻译： VERFAHREN ZUR HERSTELLUNG VON（1S，6S） - ODER（1R，6R）-CIS-2,8-DIAZABICYCLO [4.3.0] NONAN UND ZWISCHENPRODUKT
公开(公告)号：EP2423211A1
公开(公告)日：2012-02-29
申请号：EP10766836.0
申请日：2010-04-20
申请人： Kaneka Corporation
发明人： OHNUKI, Masatoshi , NISHIYAMA, Akira
IPC分类号： C07D471/04
CPC分类号： C07D471/04
摘要： The present invention relates to a process for producing (1S,6S)- or (1R,6R)-cis-2,8-diazabicyclo[4.3,0]nonane with high optical purity by forming a salt from a (1S,6R)- or (1R,6S)-cis-7,9-dioxo-8-substituted-2,8-diazabicyclo[4.3.0]nonane derivative and an acid, precipitating the salt with high excess diastereomer ratio as a solid, reducing the solid, and removing the substituent on the nitrogen atom at 8-position. According to the present invention, it is possible to easily and effectively produce (lS,6S)- or (1R,6R)-cis-2,8-diazabicyclo[4.3.0]nonane or the salt thereof with high optical purity without troublesome procedure from inexpensive and versatile starting material. The target compound is important as a raw material for a medicine.
摘要翻译：本发明涉及一种通过从（1S，6R） - 顺式-2,8-二氮杂双环[4.3,0]壬烷制备（1S，6S） - 或（1R，6R） - 顺式-2,8-二氮杂双环[ - 或（1R，6S） - 顺式-7,9-二氧代-8-取代-2,8-二氮杂双环[4.3.0]壬烷衍生物和酸，以高过量非对映异构体比例沉淀为固体，固体，并除去8-位氮原子上的取代基。根据本发明，可以容易且有效地制备（1S，6S） - 或（1R，6R） - 顺式-2,8-二氮杂双环[4.3.0]壬烷或其具有高光学纯度的盐，无麻烦从廉价和通用的起始材料的程序。目标化合物作为药物的原料是重要的。

7. 发明公开

EP2261205A1 METHOD OF PRODUCING (S)-3-(1-CYANO-1,1-DIPHENYLMETHYL)-PYRROLIDINE 审中-公开
标题翻译： VERFAHREN ZUR HERSTELLUNG VON（S）-3-（1-氰基-1,1-二苯基甲基） - 吡咯烷
公开(公告)号：EP2261205A1
公开(公告)日：2010-12-15
申请号：EP09726472.5
申请日：2009-03-26
申请人： Kaneka Corporation
发明人： NISHIYAMA, Akira , OHNUKI, Masatoshi
IPC分类号： C07D207/09 , C07D207/12 , C07B61/00
CPC分类号： C07D207/09 , C07D207/12 , Y02P20/55
摘要： The present application relates to a method of (S)-3-(1-cyano-1,1-diphenylmethyl)-pyrrolidine by reacting an (S)-1-protected-3-(sulfonyloxy)-pyrrolidine having an easily deprotectable protecting group with diphenylacetonitrile in the presence of a base to obtain an (S)-1-protected-3-(1-cyano-1,1-diphenylmethyl)-pyrrolidine and then deprotecting the obtained compound under a mild condition. According to the method of the present invention, it is possible to efficiently produce (S)-3-(1-cyano-1,1-diphenylmethyl)-pyrrolidine, which is an important intermediate in the process of producing a muscarinic receptor antagonist such as darifenacin.
摘要翻译：本申请涉及（S）-3-（1-氰基-1,1-二苯基甲基） - 吡咯烷的方法，通过使具有容易脱保护的保护基的（S）-1-保护的3-（磺酰氧基） - 吡咯烷在碱存在下与二苯基乙腈组合，得到（S）-1-保护的3-（1-氰基-1,1-二苯基甲基） - 吡咯烷，然后在温和条件下使所得化合物脱保护。根据本发明的方法，可以有效地生产（S）-3-（1-氰基-1,1-二苯基甲基） - 吡咯烷，它是生产毒蕈碱受体拮抗剂的重要中间体作为darifenacin。

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