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1. 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。

2. 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。

3. 发明申请

US20050080277A1 Process for preparing optically active 2-[6-(hydroxy-methyl)-1,3-dioxan-4-yl] acetic acid derivatives 失效
标题翻译：光学活性的2- [6-（羟基 - 甲基）-1,3-二恶烷-4-基]乙酸衍生物的制备方法
公开(公告)号：US20050080277A1
公开(公告)日：2005-04-14
申请号：US10048553
申请日：2001-06-05
申请人： Akira Nishiyama , Miho Horikawa , Yoshihiko Yasohara , Noboru Ueyama , Kenji Inoue
发明人： Akira Nishiyama , Miho Horikawa , Yoshihiko Yasohara , Noboru Ueyama , Kenji Inoue
IPC分类号： C07D319/06 , C12P7/42 , C12P17/06
CPC分类号： C07D319/06 , C12P7/42 , C12P17/06
摘要： The present invention is to provide a production technology by which an optically active 2-[6-(hydroxymethyl)-1,3-dioxan-4-yl]acetic acid derivative, which are of value as pharmaceutical intermediates, can be produced from inexpensive and readily available starting materials without using any extraordinary equipment such as an ultra-low-temperature reactor. The present invention is a production process of an optically active 2-[6-(hydroxymethyl)-1,3-dioxan-4-yl]acetic acid derivative which comprises reacting an enolate, prepared by permitting a base or a 0-valent metal to act on an acetic acid ester derivative with (S)-β-hydroxy-γ-butyrolactone at a temperature not lower than −30° C. to give a dihydroxyoxohexanoic acid derivative, treating the same with an acylating agent in the presence of a base to produce a dihydroxyoxohexanoic acid monoacyl derivative, reducing this compound with a microorganism to produce a trihydroxyhexanoic acid monoacyl derivative, treating this compound with an acetal-forming reagent in the presence of an acid catalyst to produce an acyloxymethyldioxanylacetic acid derivative, and finally, subjecting this compound to solvolysis in the presence of a base.
摘要翻译：本发明提供一种生产技术，通过该技术，可以以廉价的方式生产价值为医药中间体的光学活性的2- [6-（羟甲基）-1,3-二恶烷-4-基]乙酸衍生物和容易获得的起始材料，而不使用任何非常设备，例如超低温反应器。本发明是光学活性的2- [6-（羟甲基）-1,3-二恶烷-4-基]乙酸衍生物的制备方法，该方法包括使通过使碱或0价金属在不低于-30℃的温度下用（S）-β-羟基-γ-丁内酯在乙酸酯衍生物上作用，得到二羟基氧代己酸衍生物，在酰化剂存在下用酰化剂处理碱化以制备二羟基氧己基单酰基衍生物，用微生物还原该化合物以产生三羟基己酸单酰基衍生物，在酸催化剂存在下用缩醛形成试剂处理该化合物，得到酰氧基甲基二恶烷基乙酸衍生物，最后，该化合物在碱存在下溶剂解。

4. 发明授权

US07094594B2 Process for preparing optically active 2-[6-(hydroxy-methyl)-1,3-dioxan-4-yl] acetic acid derivatives 失效
标题翻译：光学活性的2- [6-（羟基 - 甲基）-1,3-二恶烷-4-基]乙酸衍生物的制备方法
公开(公告)号：US07094594B2
公开(公告)日：2006-08-22
申请号：US10048553
申请日：2001-06-05
申请人： Akira Nishiyama , Miho Horikawa , Yoshihiko Yasohara , Noboru Ueyama , Kenji Inoue
发明人： Akira Nishiyama , Miho Horikawa , Yoshihiko Yasohara , Noboru Ueyama , Kenji Inoue
IPC分类号： C12P41/00
CPC分类号： C07D319/06 , C12P7/42 , C12P17/06
摘要： The present invention is to provide a production technology by which an optically active 2-[6-(hydroxymethyl)-1, 3-dioxan-4-yl]acetic acid derivative, which are of value as pharmaceutical intermediates, can be produced from inexpensive and readily available starting materials without using any extraordinary equipment such as an ultra-low-temperature reactor.The present invention is a production process of an optically active 2-[6-(hydroxymethyl)-1,3-dioxan-4-yl]acetic acid derivative which comprises reacting an enolate, prepared by permitting a base or a 0-valent metal to act on an acetic acid ester derivative with (S)-β-hydroxy-γ-butyrolactone at a temperature not lower than −30° C. to give a dihydroxyoxohexanoic acid derivative, treating the same with an acylating agent in the presence of a base to produce a dihydroxyoxohexanoic acid monoacyl derivative, reducing this compound with a microorganism to produce a trihydroxyhexanoic acid monoacyl derivative, treating this compound with an acetal-forming reagent in the presence of an acid catalyst to produce an acyloxymethyldioxanylacetic acid derivative, and finally, subjecting this compound to solvolysis in the presence of a base.
摘要翻译：本发明提供一种生产技术，通过该技术，可以从廉价的方式制备价值为药物中间体的光学活性的2- [6-（羟甲基）-1,3-二恶烷-4-基]乙酸衍生物和容易获得的起始材料，而不使用任何非常设备，例如超低温反应器。本发明是光学活性的2- [6-（羟甲基）-1,3-二恶烷-4-基]乙酸衍生物的制备方法，该方法包括使通过使碱或0价金属在不低于-30℃的温度下用（S）-β-羟基-γ-丁内酯在乙酸酯衍生物上作用，得到二羟基氧代己酸衍生物，在酰化剂存在下用酰化剂处理碱化以制备二羟基氧己基单酰基衍生物，用微生物还原该化合物以产生三羟基己酸单酰基衍生物，在酸催化剂存在下用缩醛形成试剂处理该化合物，得到酰氧基甲基二恶烷基乙酸衍生物，最后，该化合物在碱存在下溶剂解。

5. 发明申请

US20060246557A1 Process for preparing optically active 2-[6-(hydroxy-methyl)-1,3-dioxan-4-yl] acetic acid derivatives 审中-公开
标题翻译：光学活性的2- [6-（羟基 - 甲基）-1,3-二恶烷-4-基]乙酸衍生物的制备方法
公开(公告)号：US20060246557A1
公开(公告)日：2006-11-02
申请号：US11477322
申请日：2006-06-30
申请人： Akira Nishiyama , Miho Horikawa , Yoshihiko Yosohara , Noboru Ueyama , Kenji Inoue
发明人： Akira Nishiyama , Miho Horikawa , Yoshihiko Yosohara , Noboru Ueyama , Kenji Inoue
IPC分类号： C12P7/64 , C12P7/62 , C07C51/00
CPC分类号： C07D319/06 , C12P7/42 , C12P17/06
摘要： The present invention is to provide a production technology by which an optically active 2-[6-(hydroxymethyl)-1,3-dioxan-4-yl]acetic acid derivative, which are of value as pharmaceutical intermediates, can be produced from inexpensive and readily available starting materials without using any extraordinary equipment such as an ultra-low-temperature reactor. The present invention is a production process of an optically active 2-[6-(hydroxymethyl)-1,3-dioxan-4-yl]acetic acid derivative which comprises reacting an enolate, prepared by permitting a base or a 0-valent metal to act on an acetic acid ester derivative with (S)-β-hydroxy-γ-butyrolactone at a temperature not lower than −30° C. to give a dihydroxyoxohexanoic acid derivative, treating the same with an acylating agent in the presence of a base to produce a dihydroxyoxohexanoic acid monoacyl derivative, reducing this compound with a microorganism to produce a trihydroxyhexanoic acid monoacyl derivative, treating this compound with an acetal-forming reagent in the presence of an acid catalyst to produce an acyloxy-methyldioxanylacetic acid derivative, and finally, subjecting this compound to solvolysis in the presence of a base.
摘要翻译：本发明提供一种生产技术，通过该技术，可以以廉价的方式生产价值为医药中间体的光学活性的2- [6-（羟甲基）-1,3-二恶烷-4-基]乙酸衍生物和容易获得的起始材料，而不使用任何非常设备，例如超低温反应器。本发明是光学活性的2- [6-（羟甲基）-1,3-二恶烷-4-基]乙酸衍生物的制备方法，该方法包括使通过使碱或0价金属在不低于-30℃的温度下用（S）-β-羟基-γ-丁内酯在乙酸酯衍生物上作用，得到二羟基氧代己酸衍生物，在酰化剂存在下用酰化剂处理制备二羟基氧基己酸单酰基衍生物，用微生物还原该化合物以产生三羟基己酸单酰基衍生物，在酸催化剂存在下用缩醛形成试剂处理该化合物以产生酰氧基 - 甲基二恶烷基乙酸衍生物，最后使该化合物在碱的存在下溶剂解。

6. 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。

7. 发明申请

US20050153408A1 Process for preparation of 2-aminotetralin derivatives and intermediates thereof 审中-公开
标题翻译： 2-氨基四氢化萘衍生物的制备方法及其中间体
公开(公告)号：US20050153408A1
公开(公告)日：2005-07-14
申请号：US10496639
申请日：2002-11-28
申请人： Tatsuya Honda , Akio Fujii , Kenji Inoue , Yoshihiko Yasohara , Yoshifumi Itagaki , Katsuji Maehara , Toshihiro Takeda , Yasuyoshi Ueda
发明人： Tatsuya Honda , Akio Fujii , Kenji Inoue , Yoshihiko Yasohara , Yoshifumi Itagaki , Katsuji Maehara , Toshihiro Takeda , Yasuyoshi Ueda
IPC分类号： C07C213/02 , C07C217/74 , C07C303/28 , C07C309/66 , C07C309/73 , C12P7/42 , C12P7/62
CPC分类号： C12P7/42 , C07B2200/07 , C07C213/02 , C07C303/28 , C07C309/66 , C07C309/73 , C07C217/74
摘要： The present invention is to efficiently and simply prepare an optically active 7-substituted-2-aminotetralin with industrial advantage. In the process, a 7-substituted-2-tetralone or its bisulfite adduct is reduced with a microorganism to an optically active 7-substituted-2-tetralol. Then, a sulfonyl group is introduced to the hydroxy group to form an optically active 7-substituted-2-sulfonyloxytetralin. Then, with inversion of the configuration, a nitrogen substituent is introduced using a nitrogen nucleophile to form an optically active 2,7-substituted tetralin. Furthermore, if necessary, the nitrogen substituent is converted into a non-substituted amino group. Thus, an optically active 7-substituted-2-aminotetralin or its salt is prepared.
摘要翻译：本发明是有效且简单地制备具有工业优势的光学活性7-取代-2-氨基四氢萘酚。在此过程中，7-取代-2-四氢萘酮或其亚硫酸氢盐加合物与微生物一起还原成光学活性的7-取代-2-四氢萘酚。然后，将磺酰基引入羟基以形成光学活性的7-取代-2-磺酰氧基四氢萘酮。然后，通过配置的倒置，使用氮亲核试剂引入氮取代基以形成光学活性的2,7-取代的四氢化萘。此外，如果需要，氮取代基转化为未取代的氨基。因此，制备光学活性的7-取代-2-氨基四氢萘或其盐。

8. 发明授权

US07582781B2 Optically active halohydrin derivative and process for producing optically active epoxy alcohol derivative from the same 失效
标题翻译：光学活性卤代醇衍生物及其制备光学活性环氧醇衍生物的方法
公开(公告)号：US07582781B2
公开(公告)日：2009-09-01
申请号：US10563635
申请日：2004-07-05
申请人： Kazumi Okuro , Tatsuyoshi Tanaka , Masaru Mitsuda , Kenji Inoue
发明人： Kazumi Okuro , Tatsuyoshi Tanaka , Masaru Mitsuda , Kenji Inoue
IPC分类号： C07D301/24 , C07D301/26 , C07D405/06 , C07C33/26 , C07C69/353 , C07F7/04
CPC分类号： C07C67/29 , C07B2200/07 , C07C29/10 , C07D301/24 , C07C33/46
摘要： The present invention provides an industrially safe, easily operable process for producing an optically active epoxy alcohol derivative useful as an intermediate for pharmaceuticals from inexpensively available materials, and also provides a novel halohydrin derivative serving as an important intermediate for the epoxy alcohol derivative. Furthermore, the present invention provides a process for producing an intermediate for a triazole antifungal agent by allowing a halohydrin to react with a triazole sulfonamide, the process including a small number of steps. A process for producing an optically active epoxy alcohol derivative includes allowing an optically active α-substituted propionate derivative to react with a haloacetic acid derivative in the presence of a base to prepare an optically active haloketone derivative, allowing the resulting haloketone derivative to react with an aryl metal compound to stereoselectively prepare a halohydrin derivative, eliminating a substituent for the hydroxy group of the halohydrin derivative, and performing epoxidation with a base. Furthermore, a process for producing an intermediate for a triazole antifungal agent includes allowing a halohydrin derivative to react with a triazole sulfonamide, the process including a small number of steps.
摘要翻译：本发明提供了一种工业上安全，易于操作的方法，用于制备用作药物的廉价可得材料的中间体的光学活性环氧醇衍生物，并且还提供了作为环氧醇衍生物的重要中间体的新型卤代醇衍生物。此外，本发明提供了通过使卤代醇与三唑磺酰胺反应来制备三唑抗真菌剂的中间体的方法，该方法包括少量的步骤。制备光学活性环氧醇衍生物的方法包括使光学活性的α-取代的丙酸酯衍生物与卤代乙酸衍生物在碱的存在下反应以制备光学活性的卤代酮衍生物，使所得到的卤代酮衍生物与芳基金属化合物立体选择性地制备卤代醇衍生物，除去卤代醇衍生物的羟基的取代基，并用碱进行环氧化。此外，制备三唑抗真菌剂中间体的方法包括使卤代醇衍生物与三唑磺酰胺反应，该方法包括少量步骤。

9. 发明授权

US07094926B2 Process for producing optically active carboxylic acid substituted in 2-position 失效
公开(公告)号：US07094926B2
公开(公告)日：2006-08-22
申请号：US10182260
申请日：2001-01-25
申请人： Susumu Amano , Masaru Mitsuda , Kenji Inoue , Koichi Kinoshita , Koki Yamashita , Yasuyoshi Ueda
发明人： Susumu Amano , Masaru Mitsuda , Kenji Inoue , Koichi Kinoshita , Koki Yamashita , Yasuyoshi Ueda
IPC分类号： C07C51/58
CPC分类号： C07C327/32 , C07C51/04 , C07C51/367 , C07C51/60 , C07C59/48 , C07C57/58 , C07C57/76
摘要： A nitrous acid salt is added at a temperature of 10 to 80° C. to an aqueous solution which contains an optically active 2-aminocarboxylic acid (4) and a protonic acid, the amount of the latter acid being 1 to 3 equivalents to the former, and which has a proton concentration of 0.5 to 2 mol/kg to conduct a reaction to thereby produce an optically active 2-hydroxycarboxylic acid (1). Thionyl chloride and a basic compound are caused to act on the compound (1) to chlorinate it and simultaneously invert the configuration in the 2-position. Thus, an optically active 2-chlorocarboxylic acid chloride (5) is induced. The compound (5) is hydrolyzed to induce an optically active 2-chlorocarboxylic acid (2). The compound (2) is reacted with a thioacetic acid salt to incorporate an acetylthio group thereinto and simultaneously invert the configuration in the 2-position to thereby produce an optically active 2-acetylthiocarboxylic acid (3).

10. 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，

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