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1. 发明授权

EP2050738B1 NOVEL IMIDAZOLIDINONE DERIVATIVE, METHOD OF PRODUCING THE SAME AND METHOD OF PRODUCING OPTICALLY ACTIVE AMINO ACID 有权转让
标题翻译： NEW咪唑啉酮衍生物，的制造方法及其制造方法的光学活性氨基
公开(公告)号：EP2050738B1
公开(公告)日：2013-07-10
申请号：EP07743261.5
申请日：2007-05-14
申请人： Kaneka Corporation
发明人： SAKA, Yasuhiro , FUJII, Akio , OKURO, Kazumi , MITSUDA, Masaru
IPC分类号： C07D233/32 , C07C227/22 , C07C229/08 , C07C229/22 , C07C229/36 , C07B61/00
CPC分类号： C07D233/32 , C07C227/22 , C07C231/10 , C07C229/14 , C07C229/22 , C07C229/36 , C07C237/06

2. 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。

3. 发明公开

EP1153919A1 SUBSTITUTED ACETYLPYRIDINE DERIVATIVES AND PROCESS FOR THE PREPARATION OF INTERMEDIATES FOR OPTICALLY ACTIVE BETA3 AGONIST BY THE USE OF THE SAME 审中-公开
标题翻译：取代的乙酰基衍生物及其生产光学中间体，用于采用主动BETA3 AGONSITENMITTELS过程
公开(公告)号：EP1153919A1
公开(公告)日：2001-11-14
申请号：EP00903975.1
申请日：2000-02-16
申请人： KANEKA CORPORATION
发明人： AMANO, Susumu , TAOKA, Naoaki , MITSUDA, Masaru , INOUE, Kenji
IPC分类号： C07D213/50 , C07D213/64 , C07D213/72 , C07D213/75 , C07D405/04
CPC分类号： C07D213/30 , C07D213/50 , C07D213/74 , C07D213/75 , C07D405/04
摘要： It is an objective to produce intermediates of optically active beta-3 adrenaline receptor agonists from readily available raw materials in a safe, efficient and industrially advantageous manner. A substituted acetylpyridine derivative represented by the general formula (9) is reduced by enantioselective reduction to produce an optically active hydroxyethylpyridine derivative represented by the general formula (10) (wherein * represents an asymmetric carbon atom), and it is further derivatized to an intermediate of an optically active beta-3 adrenaline receptor agonist, such as an optically active dihydroxyethylpyridine derivative represented by the general formula (14) or an optically active oxirane derivative represented by the general formula (16) .
摘要翻译：它是在一个安全，有效和工业上有利的方式生产光学活性的β-3肾上腺素受体激动剂的中间体从原料易得的目标。甲substituiertem acetylpyridines衍生物由通式（9）表示由对映选择性还原还原以产生由通式（10）（worin * darstellt不对称碳原子。）表示的光学活性hydroxyethylpyridine衍生物，和它在中间体进一步衍生化，以激动剂光学活性的β-肾上腺素3受体，如在光学活性衍生物dihydroxyethylpyridine测试通过或由通式（16）表示的光学活性环氧乙烷衍生物的通式（14）表示。

4. 发明公开

EP0657415A1 OPTICALLY ACTIVE AMINO ALCOHOL DERIVATIVE AND PROCESS FOR PRODUCING THE SAME 失效
标题翻译：光学活性氨基醇衍生物及其制备方法
公开(公告)号：EP0657415A1
公开(公告)日：1995-06-14
申请号：EP94919815.4
申请日：1994-06-29
申请人： KANEKA CORPORATION
发明人： MITSUDA, Masaru , HAYASHI, Shigeo , HASEGAWA, Junzo , UEYAMA, Noboru , OHASHI, Takehisa , SHIBASAKI, Masakatsu
IPC分类号： C07C215/28 , C07C213/00 , C07C229/34 , C07C227/02 , C07C271/16 , C07D209/48
CPC分类号： C07C269/02 , C07C213/02 , C07C215/28 , C07C227/02 , C07C229/34 , C07C271/16 , Y02P20/55
摘要： A process for producing a 3-amino-1-nitro-4-phenyl-2-butanol derivative represented by general formula (1) and a 3-amino-2-hydroxy-4-phenyl-butyric acid derivative derived therefrom. In said formula, R¹ and R² represent each independently hydrogen or an amino-protecting group. The process can industrially provide an optically active amino alcohol derivative as an intermediate for synthesizing medicines such as an immunopotentiating carcinostatic bestatin in a high yield safely, readily and highly selectively.
摘要翻译：由通式（1）表示的3-氨基-1-硝基-4-苯基-2-丁醇衍生物和由其衍生的3-氨基-2-羟基-4-苯基丁酸衍生物的制备方法。在所述式中，R 1和R 2分别独立地代表氢或氨基保护基。该方法可以安全，容易且高度选择性地工业上提供光学活性氨基醇衍生物作为高产率合成药物如免疫强化制癌素贝他汀的中间体。

5. 发明公开

EP3060573A1 TETRAPEPTIDE COMPOUND AND METHOD FOR PRODUCING SAME 有权转让
标题翻译： TETRA肽化合物和方法及其生产
公开(公告)号：EP3060573A1
公开(公告)日：2016-08-31
申请号：EP14802957.2
申请日：2014-10-23
申请人： Kaneka Corporation , Stealth Peptides International, Inc.
发明人： HIRAI, Yoshinori , NISHIYAMA, Akira , MITSUDA, Masaru
IPC分类号： C07K5/11
CPC分类号： C07K5/1021 , A61K38/00 , C07B2200/13 , C07K5/1019
摘要： The present invention is to provide a method for the efficient production on an industrial scale of SS-31 (D-Arg-Dmt-Lys-Phe-NH2), which is an SS peptide. According to the present invention, the desired SS-31 is produced by efficiently synthesizing a tetrapeptide compound as a precursor of SS-31 and improving the tetrapeptide purity by crystallization.

6. 发明公开

EP1942103A1 METHOD FOR PRODUCING OPTICALLY ACTIVE BENZYLAMINE DERIVATIVE 审中-公开
标题翻译： VERFAHREN ZUR HERSTELLUNG EINES OPTISCH AKTIVEN BENZYLAMINDERIVATS
公开(公告)号：EP1942103A1
公开(公告)日：2008-07-09
申请号：EP06810597.2
申请日：2006-09-27
申请人： Kaneka Corporation
发明人： TANAKA, Tatsuyoshi , OKURO, Kazumi , MITSUDA, Masaru
IPC分类号： C07C303/40 , C07B53/00 , C07C209/62 , C07C211/27 , C07C311/16 , C07B61/00
CPC分类号： C07C311/16 , C07B53/00 , C07B2200/07 , C07C209/62 , C07C211/29
摘要： The present invention relates to a method for producing an optically active benzylamine derivative which is useful as an intermediate for pharmaceutical products and the like. In the present invention, an optically active benzylalcohol derivative is reacted with a sulfonylamide derivative in the presence of a phosphine derivative and an azodicarbonyl compound, to obtain an optically active benzylsulfonylamide derivative as a novel compound. Then, the thus-obtained optically active benzylsulfonylamide derivative is reacted with a thiol derivative, thereby producing an optically active benzylamine derivative. According to the present invention, the compound can be easily produced by a simple and short process without racemization.
摘要翻译：本发明涉及可用作药物等的中间体的光学活性苄胺衍生物的制造方法。在本发明中，在膦衍生物和偶氮二羰基化合物的存在下，将光学活性苄醇衍生物与磺酰胺衍生物反应，得到作为新化合物的光学活性苄基磺酰胺衍生物。然后，将由此得到的光学活性苄基磺酰胺衍生物与硫醇衍生物反应，从而制备光学活性苄胺衍生物。根据本发明，化合物可以通过简单且短的方法容易地制备而不进行外消旋化。

7. 发明授权

EP3060573B1 TETRAPEPTIDE COMPOUND AND METHOD FOR PRODUCING SAME 有权转让
公开(公告)号：EP3060573B1
公开(公告)日：2019-07-17
申请号：EP14802957.2
申请日：2014-10-23
申请人： Kaneka Corporation , Stealth BioTherapeutics Corp
发明人： HIRAI, Yoshinori , NISHIYAMA, Akira , MITSUDA, Masaru
IPC分类号： C07K5/11

8. 发明公开

EP3489215A1 PROCESS FOR PRODUCING ORGANIC COMPOUND 有权
公开(公告)号：EP3489215A1
公开(公告)日：2019-05-29
申请号：EP17830896.1
申请日：2017-07-11
申请人： Kaneka Corporation
发明人： YASUKOUCHI, Hiroaki , MITSUDA, Masaru , NISHIYAMA, Akira , FUNABASHI, Makoto
IPC分类号： C07C67/14 , C07C69/78 , C07C231/02 , C07C233/64 , C07D235/02 , C07D263/44 , C07D301/00 , C07D303/16
摘要： The present disclosure provides a reaction of a chlorine-containing compound using a flow reactor which is less restricted by a solvent to be used. In the present disclosure, an organic compound is produced by supplying a reaction substrate having at least one functional group which can react with chlorine and is selected from the group consisting of hydroxy group, a thiol group, an amino group, a carboxyl group, a thiocarboxyl group, and an acid amide group, and a chlorine-containing compound to a flow reactor together with a trialkyl amine having 9 to 40 carbon atoms and an organic solvent, and allowing the reaction substrate and the chlorine-containing compound to react with each other.

9. 发明公开

EP1553095A1 PROCESS FOR INDUSTRIALLY PRODUCING OPTICALLY ACTIVE 1,4-BENZODIOXANE DERIVATIVE 审中-公开
标题翻译： VERFAHREN ZUR GROSSTECHNISCHEN HERSTELLUNG EINES OPTISCHAKTIVEN 1,4-BENZODIOXANDERIVATS
公开(公告)号：EP1553095A1
公开(公告)日：2005-07-13
申请号：EP03771273.4
申请日：2003-07-17
申请人： KANEKA CORPORATION
发明人： TANAKA, Tatsuyoshi , MITSUDA, Masaru
IPC分类号： C07D319/20 , C07C303/28 , C07C309/66 , C07C41/03 , C07C41/16 , C07C43/23
CPC分类号： C07D319/20
摘要： A simple and safe method for producing optically active 1,4-benzodioxane derivatives useful as intermediates for pharmaceuticals and the like from inexpensive materials is provided.
An optically active triol compound (5) produced by reaction of catechol (2) and optically active 3-halogeno-1,2-propanediol (3) is sulfonylated to form optically active trisulfonate (6), followed by cyclization with a base to yield optically active 1,4-benzodioxane (1).
摘要翻译：提供了一种用于生产用作药物等的廉价材料的中间体的光学活性1,4-苯并二氧杂环戊烷衍生物的简单和安全的方法。将通过邻苯二酚（2）和光学活性3-卤代-1,2-丙二醇（3）的反应制备的光学活性三醇化合物（5）磺酰化形成光学活性三磺酸盐（6），随后环化得到光学活性1,4-苯并二恶烷（1）的碱。

10. 发明授权

EP1024139B1 PROCESS FOR THE PREPARATION OF OPTICALLY ACTIVE 2-(6-(HYDROXYMETHYL)-1,3-DIOXAN-4-YL) ACETIC ACID DERIVATIVES 有权
标题翻译：用于生产光学活性的2-（6-（羟甲基）-1,3-二恶烷-4-基） - 衍生物
公开(公告)号：EP1024139B1
公开(公告)日：2004-05-12
申请号：EP99935066.3
申请日：1999-08-05
申请人： KANEKA CORPORATION
发明人： KIZAKI, Noriyuki , YAMADA, Yukio , YASOHARA, Yoshihiko , NISHIYAMA, Akira , MIYAZAKI, Makoto , MITSUDA, Masaru , KONDO, Takeshi , UEYAMA, Noboru , INOUE, Kenji
IPC分类号： C07D319/06 , C07C67/343 , C07C67/31
CPC分类号： C07D319/06 , C07B2200/07 , C07C67/343 , C07C253/30 , C12P7/62 , C07C69/716 , C07C255/21

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