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1. 发明申请

WO2007011065A3 INTERMEDIATE COMPOUND FOR SYNTHESIZING PHARMACEUTICAL AGENT AND PRODUCTION METHOD THEREOF 审中-公开
标题翻译：用于合成药物的中间体化合物及其生产方法
公开(公告)号：WO2007011065A3
公开(公告)日：2007-08-16
申请号：PCT/JP2006314932
申请日：2006-07-21
申请人： MITSUBISHI PHARMA CORP , SANOFI AVENTIS , OKUYAMA MASAHIRO , UEHARA FUMIAKI , IWAMURA HIROSHI , WATANABE KAZUTOSHI
发明人： OKUYAMA MASAHIRO , UEHARA FUMIAKI , IWAMURA HIROSHI , WATANABE KAZUTOSHI
IPC分类号： C07D265/30 , C07D265/32
CPC分类号： C07D265/30 , C07D265/32
摘要： The present invention relates to a production method of an optically active morpholine compound represented by the formula 10, which includes the following steps: wherein each symbol is as defined in the specification. The present invention also relates to a production method of an compound represented by the formula 55, which includes the following steps: wherein each symbol is as defined in the specification. According to the production method of the present invention, an optically active 2-aryl-substituted morpholine compound and 3-oxo-3-(pyrimidin-4-yl)propionate, which are important as starting materials for synthesizing 2-(2-arylmorpholin-4-yl)-1-methyl-1H-[4,4']bipyrimidinyl-6-one having a tau protein kinase 1 inhibitory activity and useful as a therapeutic drug for Alzheimer's disease and the like, can be produced in a high yield by an industrially advantageous method.
摘要翻译：本发明涉及由式10表示的光学活性吗啉化合物的制备方法，其包括以下步骤：其中各符号如说明书中所定义。本发明还涉及由式55表示的化合物的制备方法，其包括以下步骤：其中每个符号如说明书中所定义。根据本发明的制备方法，可以使用作为2-（2-芳基吗啉）合成原料的重要的光学活性2-芳基取代的吗啉化合物和3-氧代-3-（嘧啶-4-基）丙酸酯 -4-基）-1-甲基-1H- [4,4']联嘧啶基-6-酮，可用作阿尔茨海默病等的治疗药物，具有τ蛋白激酶1抑制活性，通过工业上有利的方法获得产量。

2. 发明申请

WO2010104193A3 INTERMEDIATE COMPOUND FOR SYNTHESIZING PHARMACEUTICAL AGENT AND PRODUCTION METHOD THEREOF 审中-公开
标题翻译：用于合成药物的中间体化合物及其生产方法
公开(公告)号：WO2010104193A3
公开(公告)日：2010-11-18
申请号：PCT/JP2010054285
申请日：2010-03-09
申请人： MITSUBISHI TANABE PHARMA CORP , SANOFI AVENTIS , FURUYA RIKIZOU , OZAWA HIROKI , TOYOFUKU EIJI , KUSAKA SHINICHI , IWAMURA HIROSHI , SAKAI DAIKI , NAKAYAMA KAZUKI , WATANABE KAZUTOSHI
发明人： FURUYA RIKIZOU , OZAWA HIROKI , TOYOFUKU EIJI , KUSAKA SHINICHI , IWAMURA HIROSHI , SAKAI DAIKI , NAKAYAMA KAZUKI , WATANABE KAZUTOSHI
IPC分类号： C07D413/10 , C07D413/14
CPC分类号： C07D413/10 , C07D413/14
摘要： A production method of an optically active 2-{4-(5-substituted-oxadiazolyl) phenyl}morpholine which is useful as an intermediate for synthesizing a pharmaceutical agent is provided and the method comprises the following steps 1) to 4): 1) reacting a bromophenylmorpholine with a hexacyanoferrate(II) or a hydrate thereof at a temperature of from 110°C to 140°C in a reaction mixture comprising a Na2CO3, an organophosphorus compound, and a palladium catalyst in a polar aprotic solvent alone or combination of a polar aprotic solvent and other polar aprotic solvent or hydrocarbon solvent to give a cyanophenylmorpholine; 2) reacting the cyanophenylmorpholine with hydroxylamine or hydroxylamine hydrochloride at a temperature of from 10°C to 40°C in an aprotic polar solvent to give a hydroxylamine derivative; 3) reacting the hydroxylamine derivative with an acylation reagent selected from the group consisting of aliphatic acyl halides, aromatic acyl halides, aliphatic acyl anhydrides and aromatic acyl anhydrides; and 4) keeping the mixture obtained after step 3) at a temperature of from 60°C to 140°C to give a 2-{4-(5-substituted-oxadiazolyl) phenyl}morpholine.
摘要翻译：提供了一种可用作药物合成中间体的光学活性2- {4-（5-取代 - 恶二唑基）苯基}吗啉的生产方法，该方法包括以下步骤1）至4）：1）使溴苯基吗啉与六氰基高铁酸盐（II）或其水合物在110℃至140℃的温度下在包含Na 2 CO 3，有机磷化合物和钯催化剂的反应混合物中，在单独的极性非质子溶剂中或其组合极性非质子溶剂和其他极性非质子溶剂或烃溶剂反应，得到氰基苯基吗啉; 2）使氰基苯基吗啉与羟胺或羟胺盐酸盐在10℃至40℃的温度下在非质子传递极性溶剂中反应，得到羟胺衍生物; 3）使羟胺衍生物与选自脂族酰卤，芳族酰卤，脂族酰基酸酐和芳族酰基酸酐的酰化试剂反应; 和4）将步骤3）后获得的混合物保持在60℃至140℃的温度下，得到2- {4-（5-取代的 - 恶二唑基）苯基}吗啉。

3. 发明专利

JP2002194736A REINFORCING BAR EXPOSURE METHOD FOR REINFORCED CONCRETE STRUCTURE 失效
公开(公告)号：JP2002194736A
公开(公告)日：2002-07-10
申请号：JP2000404598
申请日：2000-12-26
申请人： IWAMURA HIROSHI , SATO SHIGERU
发明人： SATO SHIGERU
IPC分类号： E02D5/34 , E04G23/08
摘要： PROBLEM TO BE SOLVED: To provide a reinforcing bar exposure method for a reinforced concrete structure capable of correcting such a fact that chipping work is indispensable for the exposure of reinforcing bars filling a ready mixed concrete or the securement of a concrete joint casting surface with a prescribed strength since the conventional reinforced concerete work in the ground having ground water is so carried out that a reinforcing steel structure constituting the reinforced concrete structure and reinforcement are all rolled and embedded into a concrete structure because of a means for casting and filling the ready mixed concrete. SOLUTION: The reinforcing bar exposure method can correct the chipping work by putting a prescribed expansible tube on part of a prescribed reinforcing bar of the reinforcing steel structure, the surface of the reinforcing bar or the surrounding and the periphery, expanding the tube on which fluid pressure acts and preventing the reinforcing bar from being rolled, embedded and filled into the ready mixed concrete by separating the reinforcing bar from the casting ready mixed concrete to ensure a state of the exposed reinforcement.

4. 发明申请

WO2007011065A2 INTERMEDIATE COMPOUND FOR SYNTHESIZING PHARMACEUTICAL AGENT AND PRODUCTION METHOD THEREOF 审中-公开
标题翻译：用于合成药物代理的中间体化合物及其生产方法
公开(公告)号：WO2007011065A2
公开(公告)日：2007-01-25
申请号：PCT/JP2006/314932
申请日：2006-07-21
申请人： MITSUBISHI PHARMA CORPORATION , SANOFI-AVENTIS , OKUYAMA, Masahiro , UEHARA, Fumiaki , IWAMURA, Hiroshi , WATANABE, Kazutoshi
发明人： OKUYAMA, Masahiro , UEHARA, Fumiaki , IWAMURA, Hiroshi , WATANABE, Kazutoshi
IPC分类号： C07D265/30 , C07D265/32
CPC分类号： C07D265/30 , C07D265/32
摘要： The present invention relates to a production method of an optically active morpholine compound represented by the formula 10, which includes the following steps: wherein each symbol is as defined in the specification. The present invention also relates to a production method of an compound represented by the formula 55, which includes the following steps: wherein each symbol is as defined in the specification. According to the production method of the present invention, an optically active 2-aryl-substituted morpholine compound and 3-oxo-3-(pyrimidin-4-yl)propionate, which are important as starting materials for synthesizing 2-(2-arylmorpholin-4-yl)-1-methyl-1H-[4,4']bipyrimidinyl-6-one having a tau protein kinase 1 inhibitory activity and useful as a therapeutic drug for Alzheimer's disease and the like, can be produced in a high yield by an industrially advantageous method.
摘要翻译：本发明涉及由式10表示的光学活性吗啉化合物的制备方法，其包括以下步骤：其中每个符号如说明书中所定义。本发明还涉及由式55表示的化合物的制备方法，其包括以下步骤：其中每个符号如说明书中所定义。根据本发明的制备方法，光学活性2-芳基取代的吗啉化合物和3-氧代-3-（嘧啶-4-基）丙酸酯作为合成2-（2-芳基吗啉） -4-基）-1-甲基-1H- [4,4']二嘧啶基-6-酮，其具有tau蛋白激酶1抑制活性，可用作阿尔茨海默氏病等的治疗药物，可以以高通过工业上有利的方法得到。

5. 发明申请

WO2010104193A2 INTERMEDIATE COMPOUND FOR SYNTHESIZING PHARMACEUTICAL AGENT AND PRODUCTION METHOD THEREOF 审中-公开
标题翻译：用于合成药物代理的中间体化合物及其生产方法
公开(公告)号：WO2010104193A2
公开(公告)日：2010-09-16
申请号：PCT/JP2010/054285
申请日：2010-03-09
申请人： MITSUBISHI TANABE PHARMA CORPORATION , SANOFI-AVENTIS , FURUYA, Rikizou , OZAWA, Hiroki , TOYOFUKU, Eiji , KUSAKA, Shinichi , IWAMURA, Hiroshi , SAKAI, Daiki , NAKAYAMA, Kazuki , WATANABE, Kazutoshi
发明人： FURUYA, Rikizou , OZAWA, Hiroki , TOYOFUKU, Eiji , KUSAKA, Shinichi , IWAMURA, Hiroshi , SAKAI, Daiki , NAKAYAMA, Kazuki , WATANABE, Kazutoshi
IPC分类号： C07D413/10
CPC分类号： C07D413/10 , C07D413/14
摘要： A production method of an optically active 2-{4-(5-substituted-oxadiazolyl) phenyl}morpholine which is useful as an intermediate for synthesizing a pharmaceutical agent is provided and the method comprises the following steps 1) to 4): 1) reacting a bromophenylmorpholine with a hexacyanoferrate(II) or a hydrate thereof at a temperature of from 110°C to 140°C in a reaction mixture comprising a Na 2 CO 3 , an organophosphorus compound, and a palladium catalyst in a polar aprotic solvent alone or combination of a polar aprotic solvent and other polar aprotic solvent or hydrocarbon solvent to give a cyanophenylmorpholine; 2) reacting the cyanophenylmorpholine with hydroxylamine or hydroxylamine hydrochloride at a temperature of from 10°C to 40°C in an aprotic polar solvent to give a hydroxylamine derivative; 3) reacting the hydroxylamine derivative with an acylation reagent selected from the group consisting of aliphatic acyl halides, aromatic acyl halides, aliphatic acyl anhydrides and aromatic acyl anhydrides; and 4) keeping the mixture obtained after step 3) at a temperature of from 60°C to 140°C to give a 2-{4-(5-substituted-oxadiazolyl) phenyl}morpholine.
摘要翻译：提供了可用作合成药剂的中间体的光学活性2- {4-（5-取代 - 恶二唑基）苯基}吗啉的制备方法，该方法包括以下步骤1）至4）：1）在110℃至140℃的温度下，将溴苯基吗啉与六氰基铁酸盐（II）或其水合物在包含Na 2 CO 3，有机磷化合物和钯催化剂的反应混合物中在极性非质子溶剂中单独或组合极性非质子溶剂和其他极性非质子溶剂或烃溶剂，得到氰基苯基吗啉; 2）使氰基苯基吗啉与羟胺或盐酸羟胺在非质子极性溶剂中在10℃至40℃的温度下反应，得到羟胺衍生物; 3）使羟胺衍生物与选自脂族酰基卤，芳族酰卤，脂族酰基酸酐和芳族酰基酸酐的酰化试剂反应; 和4）将步骤3）后获得的混合物保持在60℃至140℃的温度下，得到2- {4-（5-取代 - 恶二唑基）苯基}吗啉。

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