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1. 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。

2. 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。

3. 发明授权

US5936104A Process for producing 1,2-epoxy-3-amino-4-phenylbutane derivatives 失效
标题翻译： 1,2-环氧-3-氨基-4-苯基丁烷衍生物的制备方法
公开(公告)号：US5936104A
公开(公告)日：1999-08-10
申请号：US907461
申请日：1997-08-08
申请人： Akira Nishiyama , Tadashi Sugawa , Hajime Manabe , Kenji Inoue , Noritaka Yoshida
发明人： Akira Nishiyama , Tadashi Sugawa , Hajime Manabe , Kenji Inoue , Noritaka Yoshida
IPC分类号： C07C29/143 , C07C45/48 , C07C269/06 , C07C319/20 , C07C323/43 , C07D303/36 , C07D303/38
CPC分类号： C07D303/36 , C07C269/06 , C07C29/143 , C07C319/20 , C07C45/48
摘要： The present invention provides a process for producing 1,2-epoxy-3-amino-4-phenylbutane derivatives which comprises treating a 1-halo-2-hydroxy-3-amino-4-phenylbutane derivative with a base in an aprotic polar organic solvent or a mixed solvent composed of an aprotic polar organic solvent and water and then causing the resulting epoxide to crystallize out from a mixed solvent composed of an aprotic polar organic solvent and water.
摘要翻译：本发明提供了1,2-环氧-3-氨基-4-苯基丁烷衍生物的制备方法，其包括用非质子极性有机物中的1-卤代-2-羟基-3-氨基-4-苯基丁烷衍生物溶剂或由非质子极性有机溶剂和水组成的混合溶剂，然后使得到的环氧化物从由非质子极性有机溶剂和水组成的混合溶剂中结晶出来。

4. 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。

5. 发明授权

US06573399B1 Synthesis of &agr;-amino-&agr;′, &agr;′-dihaloketones and process for the preparation of &bgr;-amino acid derivatives by the use of the same 失效
标题翻译： α-氨基-α'，α'-二卤代酮的合成和通过使用相同的β-氨基酸衍生物的制备方法
公开(公告)号：US06573399B1
公开(公告)日：2003-06-03
申请号：US09700207
申请日：2001-02-21
申请人： Akira Nishiyama , Kenji Inoue
发明人： Akira Nishiyama , Kenji Inoue
IPC分类号： C07C2600
CPC分类号： C07C269/06 , C07C271/18 , C07C271/22
摘要： The present invention provides a commercially profitable process for producing a &bgr;-amino acid ester derivative which comprises reacting an &agr;-amino acid ester derivative with a base and a dihalomethane, reacting the same with a lithium amide and an alkyllithium in succession, and treating the reaction product with an acid in an alcohol.
摘要翻译：本发明提供了一种商业上有利可图的β-氨基酸酯衍生物的制备方法，该方法包括使α-氨基酸酯衍生物与碱和二卤甲烷反应，将其与氨基化锂和烷基锂相继反应，并进行反应产品与酒精中的酸。

6. 发明授权

US06340767B1 Processes for the preparation of 5-hydroxy-3-oxopentanoic acid derivatives 有权
标题翻译： 5-羟基-3-氧代戊酸衍生物的制备方法
公开(公告)号：US06340767B1
公开(公告)日：2002-01-22
申请号：US09762215
申请日：2001-04-05
申请人： Akira Nishiyama , Kenji Inoue
发明人： Akira Nishiyama , Kenji Inoue
IPC分类号： C07C5100
CPC分类号： C12P7/62 , C07B2200/07 , C07C67/343 , C07C253/30 , C07D319/06 , C07C69/716 , C07C255/21 , C07C69/738
摘要： This invention provides a process for producing a 5-hydroxy-3-oxopentanoic acid, a useful pharmaceutical intermediate, easily from a readily available, inexpensive starting material without using any extraordinary production equipment such as a very-low-temperature reactor. Thus, this invention provides a process for producing a 5-hydroxy-3-oxopentanoic acid which comprises permitting a lithium amide to act upon a mixture of an acetic acid ester and a 3-hydroxypropionic acid derivative at not below −20° C. Further, this invention also provides a process for producing a 5-hydroxy-3-oxopentanoic acid which comprises treating a mixture of an acetic acid ester and a 3-hydroxypropionic acid derivative with a Grignard reagent to prepare a mixture of a compound and an acetic acid ester of the above formula (I), and permitting a lithium amide to act upon the mixture at a temperature not below −20° C.
摘要翻译：本发明提供一种生产5-羟基-3-氧代戊酸的方法，该方法是一种有用的药物中间体，容易从现成的廉价起始原料中生产，而不使用任何非常低的生产设备如极低温反应器。因此，本发明提供了一种生产5-羟基-3-氧代戊酸的方法，其包括允许氨化锂在不低于-20℃下作用于乙酸酯和3-羟基丙酸衍生物的混合物。此外，本发明还提供了一种生产5-羟基-3-氧代戊酸的方法，其包括用格氏试剂处理乙酸酯和3-羟基丙酸衍生物的混合物，以制备上式的化合物和乙酸酯的混合物（I）化合物，并允许在不低于-20℃的温度下使氨基化锂作用于混合物。

7. 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。

8. 发明授权

US06388086B1 Process for production of 3-(3-pyridyl)-1-propanol derivatives 失效
标题翻译： 3-（3-吡啶基）-1-丙醇衍生物的制备方法
公开(公告)号：US06388086B1
公开(公告)日：2002-05-14
申请号：US09631678
申请日：2000-08-02
申请人： Akira Nishiyama , Kazumi Okuro , Kenji Inoue
发明人： Akira Nishiyama , Kazumi Okuro , Kenji Inoue
IPC分类号： C07D21330
CPC分类号： C07D213/30
摘要： A process for producing a 3-(3-pyridyl)-1-propanol derivative of use as a pharmaceutical intermediate expediently with an inexpensive material is provided. The process is concerned with a 3-(3-pyridyl)-1-propanol derivative (3): in the formula, R1 represents an alkyl group of 1 to 20 carbon atoms, aryl group of 6 to 20 carbon atoms or aralkyl group of 7 to 20 carbon atoms, which may be substituted, and comprises reacting a 3-methylpyridine with a strong base to prepare a 3-methylpyridine metal (1): in the formula, M represents lithium, sodium, potassium or a magnesium halide, where the halide is chloride or bromide, and then reacting said metal salt with an epoxy compound (2):
摘要翻译：提供了以便宜的材料制备用作药物中间体的3-（3-吡啶基）-1-丙醇衍生物的方法。该方法涉及3-（3-吡啶基）-1-丙醇衍生物（3）：式中，R1表示碳原子数为1〜20的烷基，碳原子数为6〜20的芳基或芳烷基可以被取代的7至20个碳原子，并且使3-甲基吡啶与强碱反应以制备3-甲基吡啶金属（1）：在该式中，M表示锂，钠，钾或卤化镁，其中卤化物是氯化物或溴化物，然后使所述金属盐与环氧化合物（2）反应：

9. 再颁专利

USRE39333E1 Process for the preparation of 5-hydroxy-3-oxopentanoic acid derivatives 有权
公开(公告)号：USRE39333E1
公开(公告)日：2006-10-10
申请号：US10705665
申请日：2000-06-02
申请人： Akira Nishiyama , Kenji Inoue
发明人： Akira Nishiyama , Kenji Inoue
IPC分类号： C07C69/66 , C07C59/185
CPC分类号： C12P7/62 , C07B2200/07 , C07C67/343 , C07C253/30 , C07D319/06 , C07C69/716 , C07C255/21 , C07C69/738
摘要： This invention provides a process for producing a 5-hydroxy-3-oxopentanoic acid, a useful pharmaceutical intermediate, easily from a readily available, inexpensive starting material without using any extraordinary production equipment such as a very-low-temperature reactor.Thus, this invention provides a process for producing a 5-hydroxy-3-oxopentanoic acid which comprises permitting a lithium amide to act upon a mixture of an acetic acid ester and a 3-hydroxypropionic acid derivative at not below −20° C. Further, this invention also provides a process for producing a 5-hydroxy-3-oxopentanoic acid which comprises treating a mixture of an acetic acid ester and a 3-hydroxypropionic acid derivative with a Grignard reagent to prepare a mixture of a compound and an acetic acid ester of the above formula (I), and permitting a lithium amide to act upon the mixture at a temperature not below −20° C. This invention provides a process for producing a 5-hydroxy-3-oxopentanoic acid, a useful pharmaceutical intermediate, easily from a readily available, inexpensive starting material without using any extraordinary production equipment such as a very-low temperature reactor. Thus, this invention provides a process for producing a 5-hydroxy-3-oxopentanoic acid which comprises permitting a lithium amide to act upon a mixture of an acetic acid ester and a 3-hydroxypropionic acid derivative at not below −20° C. Further, this invention also provides a process for producing a 5-hydroxy-3-oxopentanoic acid which comprises treating a mixture of an acetic acid ester and a 3-hydroxypropionic acid derivative with a Grignard reagent to prepare a mixture of a compound and an acetic acid ester of the above formula (I), and permitting a lithium amide to act upon the mixture at a temperature not below −20° C.

10. 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。

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