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1. 发明申请

US20050080278A1 Production methods of citalopram and intermediates therefor 审中-公开
标题翻译：西酞普兰及其中间体的生产方法
公开(公告)号：US20050080278A1
公开(公告)日：2005-04-14
申请号：US10650875
申请日：2003-08-28
申请人： Tetsuya Ikemoto , Masami Igi
发明人： Tetsuya Ikemoto , Masami Igi
IPC分类号： C07C27/02 , C07C29/09 , C07C33/46 , C07C41/06 , C07C41/16 , C07C43/174 , C07C43/303 , C07C43/313 , C07C67/287 , C07C69/63 , C07D307/79 , C07D307/87 , C07C33/26
CPC分类号： C07D307/79 , C07C29/095 , C07C33/46 , C07C43/313 , C07C69/63 , C07C2601/16 , C07D307/87
摘要： The present invention provides a production method of citalopram and intermediates therefor.
摘要翻译：本发明提供西酞普兰及其中间体的制备方法。

2. 发明申请

US20020035255A1 Process for preparing pyridinemethanol compounds 失效
标题翻译：制备吡啶甲醇化合物的方法
公开(公告)号：US20020035255A1
公开(公告)日：2002-03-21
申请号：US09981919
申请日：2001-10-19
申请人： Sumika Fine Chemicals Co., Ltd.
发明人： Eiichi Iishi , Kanami Yoshikawa
IPC分类号： C07D43/04
CPC分类号： C07D401/04
摘要： A pyridinemethanol compound is an important intermediate for a mirtazapine which is useful as an antidepressant. The pyridinemethanol compound is obtained by reducing potassium pyridinecarboxylate represented by the formula (I): 1 with a metal hydride.
摘要翻译：吡啶甲醇化合物是可用作抗抑郁药的米氮平的重要中间体。吡啶甲醇化合物是通过用金属氢化物还原由式（I）表示的吡啶羧酸钾得到的。

3. 发明授权

US06096894A Production method of 2-(p-alkylphenyl)pyridine compound 失效
标题翻译： 2-（对 - 烷基苯基）吡啶化合物的制备方法
公开(公告)号：US06096894A
公开(公告)日：2000-08-01
申请号：US361749
申请日：1999-07-27
申请人： Kozo Matsui , Yoshihide Umemoto , Kiyoshi Sugi , Tetsuya Shintaku , Nobushige Itaya
发明人： Kozo Matsui , Yoshihide Umemoto , Kiyoshi Sugi , Tetsuya Shintaku , Nobushige Itaya
IPC分类号： C07D213/06 , C07D213/127 , C07D213/16
CPC分类号： C07D213/06 , C07D213/16
摘要： A method of producing a 2-(p-alkylphenyl)pyridine compound economically, easily and industrially, which comprises adding manganese dioxide and trimethylchlorosilane, or adding manganese chloride to an organic ether solvent, and reacting p-alkylphenylmagnesium halide and 2-halopyridine in the obtained organic ether solvent.
摘要翻译：经济地，容易地和在工业上生产2-（对烷基苯基）吡啶化合物的方法，其包括加入二氧化锰和三甲基氯硅烷，或向有机醚溶剂中加入氯化锰，并将对 - 烷基苯基卤化镁和2-卤代吡啶在得到有机醚溶剂。

4. 发明授权

US6090940A Method for producing potassium oxonate 有权
标题翻译：生产氧化钾的方法
公开(公告)号：US6090940A
公开(公告)日：2000-07-18
申请号：US307179
申请日：1999-05-07
申请人： Mitsuyo Sugi , Masami Igi
发明人： Mitsuyo Sugi , Masami Igi
IPC分类号： C07D233/96 , B01J27/08 , C07B61/00 , C07D251/10 , C07D251/20 , C07D251/30
CPC分类号： C07D251/20
摘要： A method for producing potassium oxonate which comprises dissolving allantoin in an aqueous potassium hydroxide solution or an aqueous potassium carbonate solution, and oxidizing said allantoin with an alkali metal hypohalogenite in the presence of potassium iodide is provided and, according to the method, potassium oxonate can be efficiently produced without requiring a manganese compound which may entail environmental pollution.
摘要翻译：提供了一种生产氧化钾的方法，其包括将尿囊素溶解在氢氧化钾水溶液或碳酸钾水溶液中，并在碘化钾存在下用碱金属二卤化物氧化所述尿囊素，根据该方法，有效地生产而不需要可能引起环境污染的锰化合物。

5. 发明申请

US20040162340A1 Production method of hexahydrofurofuranol derivative, intermediate therefor and production method thereof 失效
标题翻译：六氢呋喃醇衍生物的制备方法及其制备方法
公开(公告)号：US20040162340A1
公开(公告)日：2004-08-19
申请号：US10744733
申请日：2003-12-23
申请人： Sumika Fine Chemicals Co., Ltd.
发明人： Tetsuya Ikemoto , Dongguo Piao
IPC分类号： A61K031/365 , C07D307/26
CPC分类号： C07C69/708 , C07D307/20 , C07D307/33 , C07D407/04 , C07D493/04 , Y02P20/55
摘要： The present invention provides a method for producing compound (XIV) useful as an intermediate for pharmaceutical agents efficiently and economically on an industrial scale without using ozone oxidation and highly toxic reagent, and an intermediate used for this method. Particularly, the present invention provides a method for producing a compound having an absolute configuration represented by the formula (XV) and an enantiomer thereof without using a technique such as optical resolution and the like, and an intermediate used for this method. (1) Compound (XIII) as a starting material is led to compound (I), and after introducing a protecting group, subjected to reduction and cyclization to give compound (XIV). Particularly, compound (XIII) as a material is led to compound (I) via compound (XX) to produce compound (XIV). Using an optically active compound (XIII) as a starting material, a compound having an absolute configuration represented by the formula (XV) and the like are produced highly stereoselectively. (2) Compound (XXI) as a starting material is stereoselectively reduced to give compound (XXII), and by introduction of a protecting group, reduction and cyclization, compound (XXVI) is obtained, and by inverting hydroxyl group, compound (XV) is produced. 1 wherein each symbol is as defined in the specification.
摘要翻译：本发明提供了在不使用臭氧氧化和高毒性试剂的情况下，以工业规模有效且经济地用作药剂中间体的化合物（XIV）的制备方法和用于该方法的中间体。特别地，本发明提供了使用具有式（XV）表示的绝对构型的化合物及其对映异构体的方法，而不使用光学拆分等技术，以及用于该方法的中间体。（1）作为原料的化合物（XIII）被引入化合物（I），引入保护基后，进行还原和环化，得到化合物（XIV）。特别地，作为材料的化合物（XIII）通过化合物（XX）导入化合物（I）以制备化合物（XIV）。使用光学活性化合物（XIII）作为原料，高度立体选择地制备具有由式（XV）表示的绝对构型的化合物等。（2）作为原料的化合物（XXI）立体选择性还原得到化合物（XXII），通过引入保护基进行还原和环化，得到化合物（XXVI），通过羟基转化，化合物（XV）生产。其中每个符号如说明书中所定义。

6. 发明申请

US20030013911A1 Production method of 2-cyclohexyl- 2-hydroxy-2-phenylacetic acid intermediate therefor and production method thereof 失效
标题翻译： 2-环己基-2-羟基-2-苯乙酸中间体的制备方法及其制备方法
公开(公告)号：US20030013911A1
公开(公告)日：2003-01-16
申请号：US09992167
申请日：2001-11-06
申请人： Sumika Fine Chemicals Co., Ltd.
发明人： Tetsuya Ikemoto , Wei-Guo Gao , Mitsuhiro Takeda , Masami Igi
IPC分类号： C07C059/54
CPC分类号： C07C69/732 , C07C51/09 , C07C51/36 , C07C67/303 , C07C67/343 , C07C59/54
摘要： The present invention relates to production of 2-cyclohexyl-2-hydroxy-2-phenylacetic acid useful as an intermediate for pharmaceutical products, by an industrial means, economically, safely in a good yield. Novel 2-(2null-cyclohexen-1null-yl)-2-hydroxy-2-phenylacetic acid ester obtained by reacting cyclohexene and benzoylformic acid ester in the presence of a Lewis acid is hydrolyzed and reduced to give 2-cyclohexyl-2-hydroxy-2-phenylacetic acid.
摘要翻译：本发明涉及通过工业方式生产可用作药物产品中间体的2-环己基-2-羟基-2-苯乙酸，经济地，安全地以良好的收率产生。在路易斯酸存在下，通过环己烯和苯甲酰甲酸酯反应得到的2-（2'-环己烯-1'-基）-2-羟基-2-苯基乙酸酯水解并还原，得到2-环己基-2 - 羟基-2-苯基乙酸。

7. 发明申请

US20020028944A1 L-tartrate of trans-(-)-4-(4-fluorophenyl)-3-hydroxymethylpiperidine compound and process for preparing the same 审中-公开
标题翻译：反式 - （ - ） - 4-（4-氟苯基）-3-羟甲基哌啶化合物的L-酒石酸盐及其制备方法
公开(公告)号：US20020028944A1
公开(公告)日：2002-03-07
申请号：US09963455
申请日：2001-09-27
申请人： Sumika Fine Chemicals Co., Ltd.
发明人： Shigeya Yamazaki , Taro Ishibashi , Yoshihiro Kawada , Hiroyuki Yumoto , Taichi Yoshikawa , Masami Igi
IPC分类号： C07D211/22
CPC分类号： C07D211/22
摘要： An L-tartrate of a trans-(null)-4-(4-fluorophenyl)-3-hydroxymethylpiperidine compound, represented by the formula (I): 1 wherein R1 is hydrogen atom, a substituted or unsubstituted, linear or branched alkyl group having 1 to 6 carbon atoms, or an aralkyl group having 7 to 12 carbon atoms. The L-tartrate of trans-(null)-4-(4-fluorophenyl)-3-hydroxymethylpiperidine compound can be suitably used as an intermediate for pharmaceuticals such as paroxetine which is useful, for example, as an antidepressant.
摘要翻译：由式（I）表示的反 - （ - ） - 4-（4-氟苯基）-3-羟甲基哌啶化合物的L-酒石酸盐：其中R1是氢原子，取代或未取代的直链或支链烷基，其具有 1至6个碳原子，或具有7至12个碳原子的芳烷基。反式 - （ - ） - 4-（4-氟苯基）-3-羟甲基哌啶化合物的L-酒石酸盐可以适当地用作药物例如帕罗西汀的中间体，其可用作例如抗抑郁药。

8. 发明申请

US20020004598A1 Process for preparing 2,6-dichloropurine 失效
公开(公告)号：US20020004598A1
公开(公告)日：2002-01-10
申请号：US09895317
申请日：2001-07-02
申请人： Sumika Fine Chemicals Co., Ltd.
发明人： Taketo Hayashi , Hiroharu Kumazawa , Junichi Nishikawa
IPC分类号： C07D473/00
CPC分类号： C07D473/40
摘要： A process for preparing 2,6-dichloropurine including chlorinating 2-amino-6-chloropurine with a chlorine source in the presence of a diazotizating agent.

9. 发明授权

US5948914A Piperidine derivative and process for preparing the same 失效
标题翻译：哌啶衍生物及其制备方法
公开(公告)号：US5948914A
公开(公告)日：1999-09-07
申请号：US53653
申请日：1998-04-02
申请人： Kiyoshi Sugi , Nobushige Itaya , Tadashi Katsura , Masami Igi , Shigeya Yamazaki , Taro Ishibashi , Teiji Yamaoka , Yoshihiro Kawada , Yayoi Tagami
发明人： Kiyoshi Sugi , Nobushige Itaya , Tadashi Katsura , Masami Igi , Shigeya Yamazaki , Taro Ishibashi , Teiji Yamaoka , Yoshihiro Kawada , Yayoi Tagami
IPC分类号： C07D211/22 , C07D211/60 , C07D211/76 , C07D405/12
CPC分类号： C07D405/12 , C07D211/22 , C07D211/60 , C07D211/76
摘要： A piperidine derivative, which can be used as an intermediate for pharmaceuticals such as paroxetine useful as antidepressants, represented by the general formula (I): ##STR1## wherein R.sup.1 is hydrogen atom, benzyloxycarbonyl group or tert-butoxycarbonyl group; R.sup.2 is hydroxymethyl group, an alkylsulfonyloxymethyl group having an alkyl moiety of 1 to 2 carbon atoms, phenylsulfonyloxymethyl group which may have methyl group at the 4-position, (3,4-methylenedioxyphenyl)oxymethyl group, carboxyl group or --CO.sub.2 R.sup.7 group in which R.sup.7 is an alkyl group having 1 to 5 carbon atoms, and Z is methylene group or carbonyl group.
摘要翻译：哌啶衍生物，其可以用作药物的中间体，例如用作抗抑郁药的帕罗西汀，由通式（I）表示：其中R1是氢原子，苄氧基羰基或叔丁氧基羰基; R2是羟甲基，具有1〜2个碳原子的烷基部分的烷基磺酰氧基甲基，4-位可具有甲基的苯基磺酰氧基甲基，（3,4-亚甲二氧基苯基）氧甲基，羧基或-CO 2 R 7基，其中 R 7为碳原子数为1〜5的烷基，Z为亚甲基或羰基。

10. 发明授权

US5304677A Method for producing 2,6-dihydroxybenzoic acid 失效
标题翻译： 2,6-二羟基苯甲酸的制备方法
公开(公告)号：US5304677A
公开(公告)日：1994-04-19
申请号：US7782
申请日：1993-01-22
申请人： Toshio Nakamatsu , Yasuhiro Nishida , Norio Kometani
发明人： Toshio Nakamatsu , Yasuhiro Nishida , Norio Kometani
IPC分类号： C07C51/43 , C07C51/487 , C07C65/03 , C07C65/01
CPC分类号： C07C51/487
摘要： A method for producing 2,6-dihydroxybenzoic acid, which comprises heating an aqueous solution which contains a mixture of 2,6-dihydroxybenzoic acid and 2,4-dihydroxybenzoic acid and has a pH value of 4 or more, to selectively decompose 2,4-dihydroxybenzoic acid, and separating 2,6-dihydroxybenzoic acid from the decomposition reaction mixture.
摘要翻译：制备2,6-二羟基苯甲酸的方法，其包括加热含有2,6-二羟基苯甲酸和2,4-二羟基苯甲酸的混合物并且pH值为4以上的水溶液以选择性分解2，并从分解反应混合物中分离出2,6-二羟基苯甲酸。

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