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11. 发明授权

US06903225B2 Process for producing optically active 2-[6-(hydroxymethyl)-1,3-dioxan-4-yl]acetic acid derivatives 有权
标题翻译：光学活性的2- [6-（羟甲基）-1,3-二恶烷-4-基]乙酸衍生物的制备方法
公开(公告)号：US06903225B2
公开(公告)日：2005-06-07
申请号：US10242453
申请日：2002-09-13
申请人： Noriyuki Kizaki , Yukio Yamada , Yoshihiko Yasohara , Akira Nishiyama , Makoto Miyazaki , Masaru Mitsuda , Takeshi Kondo , Noboru Ueyama , Kenji Inoue
发明人： Noriyuki Kizaki , Yukio Yamada , Yoshihiko Yasohara , Akira Nishiyama , Makoto Miyazaki , Masaru Mitsuda , Takeshi Kondo , Noboru Ueyama , Kenji Inoue
IPC分类号： C07C67/343 , C07C253/30 , C07C255/21 , C07D319/06 , C12P7/62 , C12P1/04 , C12P17/06
CPC分类号： C07D319/06 , C07B2200/07 , C07C67/343 , C07C253/30 , C12P7/62 , C07C69/716 , C07C255/21
摘要： This invention provides a process for producing optically active 2-[6-(hydroxymethyl)-1,3-dioxan-4-yl]acetic acid derivatives, which are of value as intermediates of drugs, from inexpensive starting materials without using any special equipment such as that required for super-low temperature reactions.A process for producing optically active 2-[6-(hydroxymethyl)-1,3-dioxan-4-yl]acetic acid derivatives which comprises reacting an acetic acid derivative at a temperature of not less than −30° C. with an enolate prepared by permitting either a base or a metal having a valency of 0 to act on the derivative to produce a hydroxyoxohexanoic acid derivative, reducing this compound with the aid of a strain of microorganism to provide a halomethyldioxanylacetic acid derivative, treating this compound with an acetalizing agent in the presence of an acid catalyst to provide a halomethyl-dioxanylacetic acid derivative, reacted with an acyloxylating agent to provide a acyloxymethyldioxanylacetic acid derivative, and subjecting this compound to solvolysis in the presence of a base.
摘要翻译：本发明提供了从廉价起始原料生产具有价值作为药物中间体的光学活性的2- [6-（羟甲基）-1,3-二恶烷-4-基]乙酸衍生物的方法，而不使用任何特殊设备例如超低温反应所需的。一种制备光学活性的2- [6-（羟基甲基）-1,3-二恶烷-4-基]乙酸衍生物的方法，其包括使不饱和-30℃的乙酸衍生物与烯醇化物通过使碱金属或0价金属作用于衍生物以制备羟基己酸衍生物而制备，借助于微生物菌株还原该化合物以提供卤代甲基二恶烷基乙酸衍生物，用缩醛化处理该化合物在酸催化剂存在下，提供卤代甲基 - 二恶烷基乙酸衍生物，与酰氧基化剂反应，得到酰氧基甲基二恶烷基乙酸衍生物，并在碱的存在下使其溶解。

12. 发明授权

US06344569B1 Process for producing 6-cyanomethyl-1,3-dioxane-4-acetic acid derivatives 失效
标题翻译： 6-氰基甲基-1,3-二恶烷-4-乙酸衍生物的制备方法
公开(公告)号：US06344569B1
公开(公告)日：2002-02-05
申请号：US09674178
申请日：2001-01-02
申请人： Masaru Mitsuda , Makoto Miyazaki , Kenji Inoue
发明人： Masaru Mitsuda , Makoto Miyazaki , Kenji Inoue
IPC分类号： C07D31906
CPC分类号： C07D319/06 , C07C253/14 , C07C255/20
摘要： The present invention provides a process which can produce an important intermediate for the production of the HMG coenzyme A reductase inhibitor atrovastatin, 6-cyanomethyl-1,3-dioxane-4-acetic acid derivatives, with ease industrially and in good yields, wherein a 3,5-dihydroxy-6-halohexanoic acid derivative is used as the starting material, and which comprises cyanation by reaction with a cyanating agent for substitution of a cyano group for the halogen atom and an acetal formation reaction of the diol moiety with an acetal forming reagent in the presence of an acid catalyst.
摘要翻译：本发明提供了一种能够在工业上以良好的产率生产HMG辅酶A还原酶抑制剂阿曲伐他汀，6-氰基甲基-1,3-二恶烷-4-乙酸衍生物的重要中间体的方法，其中a 使用3,5-二羟基-6-卤代己酸衍生物作为原料，其中包括通过与氰化剂反应以氰基取代卤素原子进行氰化和二醇部分与缩醛的缩醛形成反应在酸催化剂存在下形成试剂。

13. 发明授权

US08273883B2 Method for producing optically active 2-arylpiperazine derivative 失效
标题翻译：光学活性2-芳基哌嗪衍生物的制备方法
公开(公告)号：US08273883B2
公开(公告)日：2012-09-25
申请号：US12449460
申请日：2008-02-05
申请人： Masatoshi Ohnuki , Akira Nishiyama , Masaru Mitsuda
发明人： Masatoshi Ohnuki , Akira Nishiyama , Masaru Mitsuda
IPC分类号： C07D241/04 , C07D295/00
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产生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-芳基哌嗪衍生物来实现。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。

14. 发明授权

US08207370B2 Process for producing optically active beta-hydroxy-alpha-aminocarboxylic acid ester 失效
标题翻译：光学活性β-羟基-α-氨基羧酸酯的制备方法
公开(公告)号：US08207370B2
公开(公告)日：2012-06-26
申请号：US12311325
申请日：2007-09-26
申请人： Tatsuya Honda , Tatsuyoshi Tanaka , Masaru Mitsuda
发明人： Tatsuya Honda , Tatsuyoshi Tanaka , Masaru Mitsuda
IPC分类号： C07C209/50 , C07C209/46 , C07C209/00 , C07C229/06
CPC分类号： C07B53/00 , C07C227/16 , C07C231/12 , C07C229/22 , C07C233/18 , C07C233/47
摘要： It is an objective of the present invention to produce an anti-form of an optically active β-hydroxy-α-aminocarboxylic acid ester efficiently, simply and industrially advantageously. The objective can be accomplished by directly and selectively producing the anti-form of the optically active β-hydroxy-α-aminocarboxylic acid ester by asymmetric reduction of a β-keto-α-aminocarboxylic acid ester using an optically active amine complex as a catalyst. Further, the β-keto-α-aminocarboxylic acid ester as a raw material can be produced at a high yield by reacting a glycine derivative with a carboxylic acid derivative.
摘要翻译：本发明的目的是在工业上有效地有效地制备光学活性的α-羟基-α-氨基羧酸酯的抗反型剂。该目的可以通过使用光学活性胺络合物不对称还原反应形式的光学活性的β-羟基-α-氨基羧酸酯来直接和选择性地制备催化剂此外，可以通过使甘氨酸衍生物与羧酸衍生物反应，以高产率制备作为原料的α-酮-α-氨基羧酸酯。

15. 发明申请

US20060223152A1 Optically active 2-allylcarboxylic acid derivative and process for producing the same 失效
标题翻译：光学活性2-烯丙基羧酸衍生物及其制备方法
公开(公告)号：US20060223152A1
公开(公告)日：2006-10-05
申请号：US10553394
申请日：2004-04-16
申请人： Kazumi Okuro , Susumu Amano , Noriyuki Kizaki , Teruaki Takesue , Masaru Mitsuda , Noriyuki Ito , Yoshihiko Yasohara
发明人： Kazumi Okuro , Susumu Amano , Noriyuki Kizaki , Teruaki Takesue , Masaru Mitsuda , Noriyuki Ito , Yoshihiko Yasohara
IPC分类号： C12P13/00 , C07F3/02
CPC分类号： C07C233/18 , C07B2200/07 , C07C51/06 , C07C67/20 , C07C233/05 , C07C271/64 , C12P7/40 , C12P41/005 , C07C57/03 , C07C69/533
摘要： The present invention provides a process for producing an optically active 2-allylcarboxylic acid derivative, which is useful as a pharmaceutical intermediate, from readily available and inexpensive starting materials by the process which can be practiced on a commercial scale in a simple and easy manner, and certain 2-allylcarboxamide derivatives, which are novel and important intermediates in that process. An N-allylcarboxamide derivative undergoes rearrangement reaction diastereoselectively in the presence of a base to give a 2-allylcarboxamide derivative, the resulting derivative is subjected to a carbamation reaction and solvolysis to give an optically active 2-allylcarboxylic acid ester, and then the ester obtained is stereoselectively hydrolyzed using an enzyme to produce 2-allylcarboxylic acid having a high optical purity. In addition, the present invention provides a 2-allylcarboxamide derivative compound which is a novel intermediate in the process of the present invention.
摘要翻译：本发明提供了一种用于制备可用作药物中间体的光学活性2-烯丙基羧酸衍生物的方法，其由易于获得且廉价的原料通过可以简单和容易的方式在商业规模上实施的方法制备，和某些2-烯丙基羧酰胺衍生物，它们是该方法中新颖且重要的中间体。 N-烯丙基甲酰胺衍生物在碱存在下非对映选择性地进行重排反应，得到2-烯丙基甲酰胺衍生物，所得衍生物进行氨基甲酰化反应和溶剂解，得到光学活性2-烯丙基羧酸酯，然后得到所述酯使用酶进行立体选择性水解以产生具有高光学纯度的2-烯丙基羧酸。此外，本发明提供了在本发明的方法中是新型中间体的2-烯丙基甲酰胺衍生物化合物。

16. 发明授权

US06642387B2 Substituted acetylpyridine derivatives and process for the preparation of intermediates for optically active &bgr;3 agonist by the use of the same 失效
标题翻译：取代的乙酰基吡啶衍生物及其制备用于光学活性β3激动剂的中间体的方法
公开(公告)号：US06642387B2
公开(公告)日：2003-11-04
申请号：US10305105
申请日：2002-11-27
申请人： Susumu Amano , Naoaki Taoka , Masaru Mitsuda , Kenji Inoue
发明人： Susumu Amano , Naoaki Taoka , Masaru Mitsuda , Kenji Inoue
IPC分类号： C07D21346
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：目的是以安全，有效和工业上有利的方式从容易获得的原料生产光学活性β-3肾上腺素受体激动剂的中间体。由通式（9）表示的取代的乙酰基吡啶衍生物通过对映选择性还原反应来制备由通式（10）表示的光学活性羟乙基吡啶衍生物（其中*表示不对称碳原子），并进一步衍生为中间体的光学活性β-3肾上腺素受体激动剂，例如由通式（14）表示的光学活性二羟基乙基吡啶衍生物或由通式（16）表示的光学活性环氧乙烷衍生物，

17. 发明授权

US06472544B1 Process for the preparation of optically active 2-[6-hydroxymethyl)-1,3-dioxan-4yl]acetic acid derivatives 有权
标题翻译：制备光学活性2-Ä6-（羟甲基）-1,3-二恶烷-4-基乙酸衍生物的方法
公开(公告)号：US06472544B1
公开(公告)日：2002-10-29
申请号：US09509998
申请日：2000-08-16
申请人： Noriyuki Kizaki , Yukio Yamada , Yoshihiko Yasohara , Akira Nishiyama , Makoto Miyazaki , Masaru Mitsuda , Takeshi Kondo , Noboru Ueyama , Kenji Inoue
发明人： Noriyuki Kizaki , Yukio Yamada , Yoshihiko Yasohara , Akira Nishiyama , Makoto Miyazaki , Masaru Mitsuda , Takeshi Kondo , Noboru Ueyama , Kenji Inoue
IPC分类号： C07D31906
CPC分类号： C07D319/06 , C07B2200/07 , C07C67/343 , C07C253/30 , C12P7/62 , C07C69/716 , C07C255/21
摘要： This invention provides a process for producing optically active 2-[6-(hydroxymethyl)-1,3-dioxan-4-yl]acetic acid derivatives, which are of value as intermediates of drugs, from inexpensive starting materials without using any special equipment such as that required for super-low temperature reactions. A process for producing optically active 2-[6-(hydroxymethyl)-1,3-dioxan-4-yl]acetic acid derivatives which comprises reacting an acetic acid derivative at a temperature of not less than −30° C. with an enolate prepared by permitting either a base or a metal having a valency of 0 to act on the derivative to produce a hydroxyoxohexanoic acid derivative, reducing this compound with the aid of a strain of microorganism to provide a halomethyldioxanylacetic acid derivative, treating this compound with an acetalizing agent in the presence of an acid catalyst to provide a halomethyldioxanylacetic acid derivative, reacted with an acyloxylating agent to provide a acyloxymethyldioxanylacetic acid derivative, and subjecting this compound to solvolysis in the presence of a base.
摘要翻译：本发明提供了从廉价起始原料生产具有价值作为药物中间体的光学活性的2- [6-（羟甲基）-1,3-二恶烷-4-基]乙酸衍生物的方法，而不使用任何特殊设备例如超低温反应所需的方法。一种制备光学活性的2- [6-（羟甲基）-1,3-二恶烷-4-基]乙酸衍生物的方法，其包括在不是的温度下使乙酸衍生物反应小于-30℃，通过使碱金属或化合价为0的金属作用于衍生物以制备羟基氧代己酸衍生物而制备的烯醇化物，借助于微生物菌株还原该化合物以提供卤甲基二恶烷基乙酸衍生物，在酸催化剂存在下用缩醛化剂处理该化合物，得到卤代甲基二恶烷基乙酸衍生物，与酰氧基化剂反应，得到酰氧基甲基二恶烷基乙酸在碱的存在下，将该化合物施用于溶剂分解。

18. 发明授权

US5616726A Optically active aminoalcohol derivatives and method of producing same 失效
标题翻译：光活性氨基醇衍生物及其制备方法
公开(公告)号：US5616726A
公开(公告)日：1997-04-01
申请号：US392826
申请日：1995-06-21
申请人： Masaru Mitsuda , Shigeo Hayashi , Junzo Hasegawa , Noboru Ueyama , Takehisa Ohashi , Masakatsu Shibasaki
发明人： Masaru Mitsuda , Shigeo Hayashi , Junzo Hasegawa , Noboru Ueyama , Takehisa Ohashi , Masakatsu Shibasaki
IPC分类号： C07C213/02 , C07C215/28 , C07C227/02 , C07C229/34 , C07C269/02 , C07C271/16
CPC分类号： C07C269/02 , C07C213/02 , C07C215/28 , C07C227/02 , C07C229/34 , C07C271/16 , Y02P20/55
摘要： An object of the present invention is to provide a safe method of commercially producing optically active aminoalcohol derivatives, which serve as intermediates for the synthesis of medicinal chemicals such as the immunopotentiating anticancer agent bestatin, in a simple and easy manner in high yields and with high levels of selectivity.The present invention consists in a method of producing 3-amino-1-nitro-4-phenyl-2-butanol derivatives of the general formula (1) ##STR1## wherein R.sup.1 and R.sup.2 each independently represents a hydrogen atom or an amino group protecting group, and a method of producing 3-amino-2-hydroxy-4-phenylbutyric acid derivatives derivable therefrom.
摘要翻译： PCT No.PCT / JP94 / 01049 Sec。 371日期：1995年6月21日 102（e）1995年6月21日PCT PCT 1994年6月29日PCT公布。出版物WO95 / 01323 日本1995年1月12日本发明的目的是提供一种安全的商业生产光学活性氨基醇衍生物的方法，其用作合成药物的中间体，例如免疫增强抗癌药的美白蛋白，简单易用高产量和高选择性。本发明在于制备通式（1）的3-氨基-1-硝基-4-苯基-2-丁醇衍生物的方法，其中R1和R2各自独立地表示氢原子或氨基保护基，以及由其衍生的3-氨基-2-羟基-4-苯基丁酸衍生物的方法。

19. 发明授权

US08716439B2 Method of producing peptide 有权
标题翻译：生产肽的方法
公开(公告)号：US08716439B2
公开(公告)日：2014-05-06
申请号：US12224543
申请日：2006-07-31
申请人： Hiroshi Murao , Ken-ichiro Morio , Masaru Mitsuda
发明人： Hiroshi Murao , Ken-ichiro Morio , Masaru Mitsuda
IPC分类号： A61K38/00
CPC分类号： C07K1/061 , C07K1/02 , C07K1/14 , C07K5/06078 , C07K5/06095 , C07K5/0806 , C07K5/0808 , C07K5/101
摘要： The present invention is related to a method of producing a peptide, characterized in contacting a reaction mixture with a base after a condensation reaction to hydrolyze while a basic condition is maintained until a ratio of a remaining unreacted active ester of an acid component is decreased to 1% or less in a liquid phase peptide synthesis method. According to the invention, a target peptide of high purity can be simply and efficiently produced by a continuous liquid phase synthesis method. Further, the present invention is related to a method of producing a peptide, characterized in using an amide-type solvent immiscible with water in a liquid phase peptide synthesis method. According to the invention, various peptides can be produced by the liquid phase synthesis method without being restricted by the amino acid sequence of the target peptide.
摘要翻译：本发明涉及一种生产肽的方法，其特征在于在缩合反应之后将反应混合物与碱反应以在碱性条件保持下进行水解，直到酸组分的剩余未反应的活性酯的比例降低至在液相肽合成方法中为1％以下。根据本发明，可以通过连续液相合成法简单有效地制备高纯度的靶肽。此外，本发明涉及一种制备肽的方法，其特征在于在液相肽合成方法中使用与水不混溶的酰胺型溶剂。根据本发明，可以通过液相合成法制备各种肽，而不受目标肽的氨基酸序列的限制。

20. 发明授权

US08383833B2 Method for producing optically active amino acid derivative 有权
标题翻译：光学活性氨基酸衍生物的制造方法
公开(公告)号：US08383833B2
公开(公告)日：2013-02-26
申请号：US12993661
申请日：2009-06-02
申请人： Shohei Yamamoto , Akio Fujii , Masaru Mitsuda
发明人： Shohei Yamamoto , Akio Fujii , Masaru Mitsuda
IPC分类号： C07D295/03
CPC分类号： C07B51/00 , C07B53/00 , C07C227/18 , C07C229/08 , C07C229/28 , C07C2601/02 , C07D207/12 , C07D211/60 , C07D295/18 , C07D403/12 , C07D495/04
摘要： The present application relates to a method for producing an optically active α-amino acid derivative, comprising steps of reacting an α-haloester derivative represented by the general formula (1): of which alcohol part of the ester group is an optically active alcohol derivative, with an amine compound; then deprotecting the obtained compound; further carrying out an ester exchange reaction. According to the present invention method, it is possible to easily produce an optically active α-amino acid ester derivative which is useful as an intermediate for drugs with high selectivity.
摘要翻译：本申请涉及一种光学活性α-氨基酸衍生物的制造方法，包括使由通式（1）表示的α-卤代酯衍生物：酯基的醇部分为光学活性醇衍生物，与胺化合物; 然后使所得化合物脱保护; 进一步进行酯交换反应。根据本发明的方法，可以容易地制备可用作高选择性药物的中间体的光学活性α-氨基酸酯衍生物。

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