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1. 发明专利

JP2005154377A Method for producing epoxytriazole compound and its intermediate 有权
标题翻译：生产环氧化合物及其中间体的方法
公开(公告)号：JP2005154377A
公开(公告)日：2005-06-16
申请号：JP2003398252
申请日：2003-11-27
申请人： Sumitomo Chemical Co Ltd , 住友化学株式会社
发明人： O IKI , IKEMOTO TETSUYA
IPC分类号： C07C45/00 , C07C45/64 , C07C49/84 , C07D249/08 , C07D303/22 , C07D405/06
CPC分类号： C07D249/08 , C07C49/84 , C07D303/22 , Y02P20/55
摘要： PROBLEM TO BE SOLVED: To provide a method for producing an epoxytriazole compound (VII) as a synthetic intermediate for pharmaceuticals under a proper quality control. SOLUTION: The epoxytriazole compound (VII) is produced by epoxidizing a compound (I) to obtain a compound (II), deprotecting the compound, reacting the obtained compound (IV) with a compound (V) to form a compound (VI) and reacting the compound with 1,2,4-triazole. The compound (I) used as a starting raw material is purifiable by recrystallization to facilitate the quality control. In the formulas, Ar is phenyl group wherein two hydrogen atoms are substituted with fluorine atoms; and R is a lower alkyl or the like. COPYRIGHT: (C)2005,JPO&NCIPI
摘要翻译：待解决的问题：提供一种在适当的质量控制下制备作为药物的合成中间体的环氧三唑化合物（VII）的方法。环氧三唑化合物（VII）通过环氧化化合物（I）得到化合物（II），使化合物脱保护，使所得化合物（Ⅳ）与化合物（Ⅴ）反应形成化合物 VI）并使化合物与1,2,4-三唑反应。用作起始原料的化合物（I）可通过重结晶进行纯化，以方便质量控制。在该式中，Ar是其中两个氢原子被氟原子取代的苯基; 并且R是低级烷基等。版权所有（C）2005，JPO＆NCIPI

2. 发明专利

JP2005145833A Method for producing syn-1,3-diol compound 审中-公开
标题翻译：生产SYN-1,3-二醇化合物的方法
公开(公告)号：JP2005145833A
公开(公告)日：2005-06-09
申请号：JP2003381816
申请日：2003-11-11
申请人： Sumitomo Chemical Co Ltd , 住友化学株式会社
发明人： O IKI , IKEMOTO TETSUYA
IPC分类号： C07D239/42 , C07B53/00 , C07D207/34 , C07D209/24 , C07D215/14 , C07D405/06
摘要： PROBLEM TO BE SOLVED: To provide a method which can industrially advantageously produce a Syn-1,3-diol compound.
SOLUTION: A compound (III) (wherein X is -CH=CH- or the like; R is an inert group under reducing conditions; and R
1 and R
2 are each a lower alkyl group or the like) is reacted with a mixture containing a borane compound (IIa) (wherein R
3 and R
4 are each a lower alkyl group or the like) or a borane compound (IIb) (wherein R
5 is a lower alkyl or the like) and sodium boron hydride in a mixed solvent containing a lower alcohol and tetrahydrofuran to obtain the Syn-1,3-diol compound (I) (wherein one of Y
1 and Y
2 is oxygen and the other is a hydroxy group: and --- is a double bond when Y
1 and Y
2 bonded are oxygens and is a single bond when Y
1 and Y
2 bonded are hydroxy groups; X, R, R
1 and R
2 are the same as defined above).
COPYRIGHT: (C)2005,JPO&NCIPI
摘要翻译：待解决的问题：提供一种在工业上有利地产生Syn-1,3-二醇化合物的方法。解决方案：化合物（III）（其中X是-CH = CH-等; R是还原条件下的惰性基团; R 1和R 2都是惰性基团; 与其中含有硼烷化合物（IIa）（其中R 3和R 4各自为低级烷基）的混合物反应，基团等）或硼烷化合物（IIb）（其中R 5是低级烷基等）和硼氢化钠在含有低级醇和四氢呋喃的混合溶剂中，得到Syn- 1,3-二醇化合物（I）（其中Y 1 和Y 2 中的一个是氧而另一个是羟基：和---是双键当Y 1 和Y 2 键合时为氧，当Y 1 和Y 2 键合时为单键羟基; X，R，R SP 1和/或SP 2与上述定义相同）。版权所有（C）2005，JPO＆NCIPI

3. 发明专利

JP2013010732A Method for producing proline compound 审中-公开
标题翻译：生产精制化合物的方法
公开(公告)号：JP2013010732A
公开(公告)日：2013-01-17
申请号：JP2011273342
申请日：2011-12-14
申请人： Sumitomo Chemical Co Ltd , 住友化学株式会社
发明人： O IKI , SHIMAZAKI TAIJI , IKEMOTO TETSUYA
IPC分类号： C07D209/52 , C07B61/00
CPC分类号： C07D209/52
摘要： PROBLEM TO BE SOLVED: To provide a method for producing a proline compound (1) or a salt thereof with high yield without using an enzyme.SOLUTION: The method for producing the proline compound or the salt thereof shown by Formula (1), comprises steps A to D. [Step A]: a step of reacting a pyrrolidinone compound with a reducing agent represented by the formula (M)H-mAl(OR)in the presence of a base; [step B]: a step of reacting the pyrrolidinol compound with a cyanating agent; [step C]: a step of hydrolyzing or alcoholizing the cyanopyrrolidine compound; and [step D]: a step of substituting Rin the protected proline compound by a hydrogen atom.
摘要翻译：待解决的问题：提供一种在不使用酶的情况下以高产率制备脯氨酸化合物（1）或其盐的方法。解决方案：制备式（1）所示的脯氨酸化合物或其盐的方法包括步骤A至D. [步骤A]：使吡咯烷酮化合物与式（1）表示的还原剂反应的步骤 1 / s H 4 -mAl - （OR 3 ） m [步骤B]：使吡咯烷醇化合物与氰化剂反应的步骤; [步骤C]：使氰基吡咯烷化合物水解或醇化的步骤; 和[步骤D]：用氢原子代替保护的脯氨酸化合物中的R 2 的步骤。版权所有（C）2013，JPO＆INPIT

4. 发明专利

JP2012140390A METHOD FOR PRODUCING α-AMINO-γ-BUTYROLACTONE 审中-公开
标题翻译：生产α-氨基-γ-丁氧基酮的方法
公开(公告)号：JP2012140390A
公开(公告)日：2012-07-26
申请号：JP2011001154
申请日：2011-01-06
申请人： Sumitomo Chemical Co Ltd , 住友化学株式会社
发明人： O IKI
IPC分类号： C07D307/33 , C07B53/00
CPC分类号： C07B53/00 , C07D307/33
摘要： PROBLEM TO BE SOLVED: To provide a method for industrially producing an α-amino-γ-butyrolactone or a salt thereof with a short reaction time, with high yield, and with excellent operability, especially to provide the method for industrially producing the α-amino-γ-butyrolactone or the salt thereof having high optical purity, wherein an asymmetric carbon is less likely to be isomerized in the method.SOLUTION: A method for producing the α-amino-γ-butyrolactone or the salt thereof comprises a step where methionine and a chloroacetic or bromoacetic acid are caused to react with each other in a solvent. The solvent contains 60 wt.% or more of water relative to the total weight of the solvent.
摘要翻译：待解决的问题：提供一种工业生产α-氨基-γ-丁内酯或其盐的方法，其反应时间短，产率高，操作性优异，特别是提供工业生产方法具有高光学纯度的α-氨基-γ-丁内酯或其盐，其中在该方法中不对称碳不太可能异构化。解决方案：制备α-氨基-γ-丁内酯或其盐的方法包括使甲硫氨酸和氯乙酸或溴乙酸在溶剂中彼此反应的步骤。相对于溶剂的总重量，溶剂含有60重量％以上的水。版权所有（C）2012，JPO＆INPIT

5. 发明专利

JP2009035528A Method for producing trans-dibenzoxenopyrrole compound and intermediate therefor 有权
标题翻译：用于生产转化二苯并恶唑化合物的方法及其中间体
公开(公告)号：JP2009035528A
公开(公告)日：2009-02-19
申请号：JP2008020889
申请日：2008-01-31
申请人： Sumitomo Chemical Co Ltd , 住友化学株式会社
发明人： O IKI , IKEMOTO TETSUYA
IPC分类号： C07D491/044 , A61K31/55 , A61P25/18 , C07D313/14
CPC分类号： C07D313/14 , C07D491/044
摘要： PROBLEM TO BE SOLVED: To provide a method for easily producing a trans-dibenzoxenopyrrole compound. SOLUTION: Provided is a method for producing a trans-dibenzoxenopyrrole compound which comprises using a compound of formula (II) as the starting material, reducing the ester group of the material to a hydroxymethyl group, converting the hydroxymethyl group to methanesulfonate, and cyclizing the methanesulfonate to a pyrrolidine ring by hydrogenation. COPYRIGHT: (C)2009,JPO&INPIT
摘要翻译：待解决的问题：提供容易制备反式二苯并恶唑并吡咯化合物的方法。解决方案：提供一种反式二苯并恶唑并吡咯化合物的制备方法，其包括使用式（II）化合物作为起始原料，将该物质的酯基还原成羟甲基，将羟甲基转化为甲磺酸酯，并通过氢化将甲磺酸酯环化成吡咯烷环。版权所有（C）2009，JPO＆INPIT

6. 发明专利

JP2009018992A Manufacturing method of optically active mirtazapine 审中-公开
标题翻译：光学活性米他芝的制备方法
公开(公告)号：JP2009018992A
公开(公告)日：2009-01-29
申请号：JP2007180645
申请日：2007-07-10
申请人： Sumitomo Chemical Co Ltd , 住友化学株式会社
发明人： O IKI , IKEMOTO TETSUYA
IPC分类号： C07D471/14 , A61K31/55 , A61P25/20 , C07B57/00 , C07B63/00
CPC分类号： C07D471/14 , C07B57/00 , C07B63/00
摘要： PROBLEM TO BE SOLVED: To provide a method for efficiently manufacturing optically active mirtazapine.
SOLUTION: The manufacturing method of optically active mirtazapine comprises optically resolving an RS mixture of mirtazapine by optically active tartaric acid in the presence of a solvent. More concretely, the manufacturing method of the optically active mirtazapine comprises bringing the RS mixture of mirtazapine into contact with optically active tartaric acid in the presence of the solvent thereby causing a salt of the optically active mirtazapine to crystallize preferentially. The solvent is preferably a mixed solvent of a water-soluble organic solvent and water, more preferably a mixed solvent of a 1-3C alcohol solvent and water.
COPYRIGHT: (C)2009,JPO&INPIT
摘要翻译：要解决的问题：提供一种有效制造光学活性米氮平的方法。光学活性米氮平的制备方法包括通过光学活性酒石酸在溶剂存在下光学拆分米氮平的RS混合物。更具体地，光学活性米氮平的制备方法包括在溶剂存在下使米氮平的RS混合物与光学活性酒石酸接触，从而使光学活性米氮平的盐优先结晶。溶剂优选为水溶性有机溶剂和水的混合溶剂，更优选为1-3℃醇溶剂和水的混合溶剂。版权所有（C）2009，JPO＆INPIT

7. 发明专利

JP2007137877A Method for producing dibenzoxepinopyrrole compound and its intermediate, and new intermediate 有权
标题翻译：生产二苯并吡喃酮化合物及其中间体的方法和新的中间体
公开(公告)号：JP2007137877A
公开(公告)日：2007-06-07
申请号：JP2006286275
申请日：2006-10-20
申请人： Sumitomo Chemical Co Ltd , 住友化学株式会社
发明人： O IKI , IKEMOTO TETSUYA
IPC分类号： C07D207/38 , C07D491/044
摘要： PROBLEM TO BE SOLVED: To provide a new method for readily producing asenapine from an easily available raw material. SOLUTION: The asenapine [VII] is produced from (2-chlorophenyl)acetic acid [1a] through the intermediate [IV] by the method shown in the figure. COPYRIGHT: (C)2007,JPO&INPIT
摘要翻译：要解决的问题：提供从容易获得的原料容易地生产阿萘那平的新方法。解决方案：通过图中所示的方法，由（2-氯苯基）乙酸[1a]通过中间体[IV]制备亚硝尿素[Ⅶ]。版权所有（C）2007，JPO＆INPIT

8. 发明专利

JP2009167166A Method for producing piperazine derivative 有权
标题翻译：生产哌嗪衍生物的方法
公开(公告)号：JP2009167166A
公开(公告)日：2009-07-30
申请号：JP2008262502
申请日：2008-10-09
申请人： Sumitomo Chemical Co Ltd , 住友化学株式会社
发明人： MAEDA CHIHARU , ISEKI EIICHI , O IKI , IMAMIYA KATSUYUKI
IPC分类号： C07D401/04 , C07B61/00 , C07C209/74 , C07C211/29 , C07C213/04 , C07C215/30 , C07D213/85
CPC分类号： C07C209/74 , C07C213/04 , C07C215/30 , C07D213/85 , C07C211/29
摘要： PROBLEM TO BE SOLVED: To provide a method for industrially easily producing a piperazine derivative useful as an intermediate for producing mirtazapine, and a method for industrially easily producing 1-methyl-3-phenylpiperazine as an important intermediate for producing the piperazine derivative, with no need of any complicated operations respectively.
SOLUTION: The method for producing the piperazine derivative represented by formula (V) comprises conducting a reaction between 1-methyl-3-phenylpiperazine and 2-chloro-3-cyanopyridine in the presence of a base and an alkali metal halide in an aprotic polar organic solvent.
COPYRIGHT: (C)2009,JPO&INPIT
摘要翻译：待解决的问题：提供一种工业上容易地制备用作制备米氮平的中间体的哌嗪衍生物的方法，以及用于工业上容易地生产1-甲基-3-苯基哌嗪作为生产哌嗪衍生物的重要中间体的方法，不需要任何复杂的操作。解决方案：由式（V）表示的哌嗪衍生物的制备方法包括在碱和碱金属卤化物存在下，在1-甲基-3-苯基哌嗪与2-氯-3-氰基吡啶之间进行反应非质子极性有机溶剂。版权所有（C）2009，JPO＆INPIT

9. 发明专利

JP2009079017A Process for preparing optically active tetrahydropyranylglycine compound 有权
标题翻译：制备光学活性四氢呋喃啉化合物的方法
公开(公告)号：JP2009079017A
公开(公告)日：2009-04-16
申请号：JP2007251061
申请日：2007-09-27
申请人： Sumitomo Chemical Co Ltd , 住友化学株式会社
发明人： MATSUI KOZO , TOMOKAWA JUNICHI , O IKI , IKEMOTO TETSUYA
IPC分类号： C07D309/04 , C07B57/00
摘要： PROBLEM TO BE SOLVED: To provide a process for industrially and inexpensively producing an optically active tetrahydropyranylglycine compound. SOLUTION: The process for producing an optically active tetrahydropyranylglycine compound comprises bringing a tetrahydropyranylglycine compound represented by formula (1) (wherein R is a benzyl group or a 1-4C alkyl group) into contact with an optically active amine, to crystallize out an optically active form of the tetrahydropyranylglycine compound and a diastereomeric salt of the optically active amine, and then treating the diastereomeric salt with an acid or a base. COPYRIGHT: (C)2009,JPO&INPIT

10. 发明专利

JP2006124326A Method for producing clopidogrel 审中-公开
标题翻译：生产胶质的方法
公开(公告)号：JP2006124326A
公开(公告)日：2006-05-18
申请号：JP2004314850
申请日：2004-10-28
申请人： Sumitomo Chemical Co Ltd , 住友化学株式会社
发明人： O IKI , IKEMOTO TETSUYA , RYO TEI
IPC分类号： C07D495/04 , C07B61/00
摘要： PROBLEM TO BE SOLVED: To provide a method for producing clopidogrel, capable of industrially suitably producing the clopidogrel at a low cost in a good yield. SOLUTION: In this method, a compound expressed by formula (II) [X is a halogen or a group expressed by R'SO 3 (R' is a lower alkyl which may be halogenated or an aryl which may be substituted); and R is a substituent which has an asymmetric carbon] and a compound expressed by formula (III) are together reacted, preferably, in the presence of a phase transfer catalyst, so that a compound expressed by formula (IV) is produced, while the reaction is diastereoselectively progressed by being accompanied with epimerization of a substituent X, and further the produced compound is converted into the clopidogrel. COPYRIGHT: (C)2006,JPO&NCIPI
摘要翻译：待解决的问题：提供氯吡格雷的生产方法，能够以低成本以良好的产率工业上合适地生产氯吡格雷。解决方案：在该方法中，由式（II）表示的化合物[X是卤素或由R'SO表示的基团（R'是可以被卤化的低级烷基可被取代的芳基）; 并且R是具有不对称碳的取代基]和由式（III）表示的化合物一起反应，优选在相转移催化剂的存在下反应，从而制备由式（IV）表示的化合物，而通过伴随着取代基X的差向异构化而非对映性地进行反应，并且进一步将所产生的化合物转化为氯吡格雷。版权所有（C）2006，JPO＆NCIPI

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