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11. 发明授权

US06777576B2 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：US06777576B2
公开(公告)日：2004-08-17
申请号：US09992167
申请日：2001-11-06
申请人： Tetsuya Ikemoto , Wei-Guo Gao , Mitsuhiro Takeda , Masami Igi
发明人： Tetsuya Ikemoto , Wei-Guo Gao , Mitsuhiro Takeda , Masami Igi
IPC分类号： C07C5940
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-(2′-cyclohexen-1′-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。

12. 发明授权

US06458975B1 Production methods of citalopram and an intermediate therefor 失效
标题翻译：西酞普兰及其中间体的生产方法
公开(公告)号：US06458975B1
公开(公告)日：2002-10-01
申请号：US09996134
申请日：2001-11-28
申请人： Tetsuya Ikemoto , Wei-Guo Gao , Nobuhiro Arai , Masami Igi
发明人： Tetsuya Ikemoto , Wei-Guo Gao , Nobuhiro Arai , Masami Igi
IPC分类号： C07D30778
CPC分类号： C07D307/87 , C07C29/40 , C07C33/46 , C07C51/265 , C07C51/373 , C07C65/34
摘要： Citalopram can be industrially and economically produced and at a high yield by reacting a compound of the following formula [VI] with 3-(dimethylamino)propyl chloride in the presence of at least one of N,N,N′,N′-tetramethylethylenediamine and 1,3-dimethyl-2-imidazolidinone and a condensing agent.
摘要翻译：通过在N，N，N'，N'-四甲基乙二胺中的至少一种的存在下使下式[Ⅵ]化合物与3-（二甲基氨基）丙基氯反应，可以工业和经济地制备，并以高收率和1,3-二甲基-2-咪唑啉酮和缩合剂。

13. 发明授权

US06433196B1 Production method of citalopram, intermediate therefor and production method of the intermediate 失效
标题翻译：西酞普兰的生产方法，中间体和中间体的生产方法
公开(公告)号：US06433196B1
公开(公告)日：2002-08-13
申请号：US09654768
申请日：2000-09-05
申请人： Tetsuya Ikemoto , Wei-Guo Gao , Nobuhiro Arai , Masami Igi
发明人： Tetsuya Ikemoto , Wei-Guo Gao , Nobuhiro Arai , Masami Igi
IPC分类号： C07D30778
CPC分类号： C07D307/87 , C07C29/40 , C07C33/46 , C07C51/265 , C07C51/373 , C07C65/34
摘要： Citalopram can be industrially and economically produced and at a high yield by reacting a compound of the following formula [VI] with 3-(dimethylamino)propyl chloride in the presence of at least one of N,N,N′,N′-tetramethylethylenediamine and 1,3-dimethyl-2-imidazolidinone and a condensing agent. The compound of the following formula [III], which is a key compound for the production of citalopram, can be easily produced by subjecting the compound of the following formula [II] to reduction and cyclization.
摘要翻译：通过在N，N，N'，N'-四甲基乙二胺中的至少一种的存在下使下式[Ⅵ]化合物与3-（二甲基氨基）丙基氯反应，可以工业和经济地制备，并以高收率和1,3-二甲基-2-咪唑啉酮和缩合剂。通过使下式[Ⅱ]的化合物还原和环化，可以容易地制备作为西酞普兰生产的关键化合物的下式[III]的化合物。

14. 发明授权

US06433168B1 Highly pure phenothiazine compound, production method thereof, production method of intermediate therefor, and hydrate and novel crystal as starting materials for the intermediate 失效
标题翻译：高纯吩噻嗪化合物，其制备方法，其中间体的制备方法，水合物和新型晶体为中间体的起始原料
公开(公告)号：US06433168B1
公开(公告)日：2002-08-13
申请号：US09621782
申请日：2000-07-21
申请人： Shigeya Yamazaki , Hiroyuki Yumoto , Masami Igi
发明人： Shigeya Yamazaki , Hiroyuki Yumoto , Masami Igi
IPC分类号： C07D41700
CPC分类号： C07D453/02
摘要： According to the method of the present invention, an alkali metal compound, dimethyl sulfoxide, trimethyloxosulfonium halide and 3-quinuclidinone are added in a specific order to give the following compound [II]. This compound is, without treatment or isolation, directly reacted with an alkali metal salt of phenothiazine to give the following compound [III], from which the following compound [I] is obtained. During the production of compound [I], a by-produced acidic gas is removed and water is added to ensure industrial, safe and efficient production of compound [I] at a constantly high yield. Inasmuch as the present invention enables production of the following highly pure compound [A] by eliminating hydrogen halide of compound [I] in glyme in the presence of at least one kind of a base selected from potassium hydroxide and potassium alkoxide, compound [A] having a high purity of not less than 85 mol % can be provided.
摘要翻译：根据本发明的方法，以特定的顺序加入碱金属化合物，二甲基亚砜，三甲基锍卤化物和3-奎宁环酮，得到下列化合物[II]。该化合物在不经处理或分离的情况下与吩噻嗪的碱金属盐直接反应，得到以下化合物[III]，由此得到下列化合物[I]。在化合物[I]的生产过程中，除去副产的酸性气体，加入水以确保化合物[I]的工业，安全和有效的生产以不断的高产率。由于本发明能够通过在至少一种选自氢氧化钾和醇钾的碱的存在下，通过除去甘醇二甲醚中的化合物[I]的卤化氢来制备下列高纯度化合物[A]，化合物[A] 可以提供不小于85mol％的高纯度。

15. 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。

16. 发明授权

US06977306B2 Citalopram hydrobromide crystal and method for crystallization thereof 失效
标题翻译：西酞普兰氢溴酸盐晶体及其结晶方法
公开(公告)号：US06977306B2
公开(公告)日：2005-12-20
申请号：US09824447
申请日：2001-04-02
申请人： Tetsuya Ikemoto , Nobuhiro Arai , Masami Igi
发明人： Tetsuya Ikemoto , Nobuhiro Arai , Masami Igi
IPC分类号： C07D307/87 , C07D307/78 , A61K31/343
CPC分类号： C07D307/87
摘要： According to the present invention, citalopram hydrobromide dissolved in a solvent containing at least one member selected from the group consisting of alcohol having 1-3 carbon atoms, water and acetone is crystallized or recrystallized while controlling the cooling rate, thereby to 1) provide an industrial method for crystallizing citalopram hydrobromide, which enables easy control of the crystal characteristics, such as particle size, particle size distribution and aspect ratio and the like of the crystal, and 2) provide citalopram hydrobromide crystal having crystal characteristics useful as a pharmaceutical bulk.
摘要翻译：根据本发明，在控制冷却速度的同时，溶解在含有选自具有1-3个碳原子的醇中的至少一种的水溶液和水和丙酮中的西酞普兰氢溴酸盐结晶或重结晶，从而1）用于结晶西酞普兰氢溴酸盐的工业方法，其能够容易地控制晶体的晶体特性，例如粒度，粒度分布和长宽比等，以及2）提供具有作为药物体积有用的晶体特性的西酞普兰氢溴酸盐晶体。

17. 发明授权

US06930211B2 Production methods of citalopram and intermediates therefor 失效
标题翻译：西酞普兰及其中间体的生产方法
公开(公告)号：US06930211B2
公开(公告)日：2005-08-16
申请号：US10650876
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 , C07C37/55
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 a compound of the formula wherein X is chlorine atom, bromine atom or iodine atom, as well as a production method of citalopram and intermediates therefor.
摘要翻译：本发明提供下式化合物的制备方法，其中X为氯原子，溴原子或碘原子，以及西酞普兰及其中间体的制备方法。

18. 发明授权

US06433195B1 Production methods of 5-phthalancarbonitrile compound and an intermediate therefor 失效
标题翻译： 5-邻苯二甲腈化合物及其中间体的制备方法
公开(公告)号：US06433195B1
公开(公告)日：2002-08-13
申请号：US09997992
申请日：2001-11-30
申请人： Tetsuya Ikemoto , Masami Igi
发明人： Tetsuya Ikemoto , Masami Igi
IPC分类号： C07D30787
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 a 5-phthalancarbonitrile compound of the formula [VI] as well as production methods of a compound of the formula [V]
摘要翻译：本发明提供式[Ⅵ]的5-邻苯二甲腈化合物的制备方法以及式[Ⅴ]化合物的制备方法，

19. 发明授权

US06395910B2 Production method of 5-phthalancarbonitrile compound, intermediate therefor and production method of the intermediate 失效
标题翻译： 5-邻苯二甲腈化合物的制备方法，其中间体和中间体的制备方法
公开(公告)号：US06395910B2
公开(公告)日：2002-05-28
申请号：US09909596
申请日：2001-07-20
申请人： Tetsuya Ikemoto , Masami Igi
发明人： Tetsuya Ikemoto , Masami Igi
IPC分类号： C07D30906
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 a 5-phthalancarbonitrile compound, which comprises the use of a novel compound of the formula [I] wherein X is chlorine atom, bromine atom or iodine atom, as a key intermediate. The method of the present invention imposes small environmental burden (without use of a reagent imposing great burden on the environment, such as heavy metal, metal cyanide, thionyl chloride and the like) and is safe. The inventive method is based on a completely new strategy which is different from conventional production methods of 5-phthalancarbonitrile compound.
摘要翻译：本发明提供了5-邻苯二甲酰腈化合物的制备方法，该方法包括使用其中X为氯原子，溴原子或碘原子的式[I]的新化合物作为关键中间体。本发明的方法施加小环境负担（不使用对重金属，金属氰化物，亚硫酰氯等环境造成重大负担的试剂），是安全的。本发明的方法是基于与5-邻苯二甲腈化合物的常规生产方法不同的全新策略。

20. 发明授权

US06316628B1 L-tartrate of trans-(-)-4-(4-fluorophenyl)-3-hydroxymethylpiperidine compound and process for preparing the same 失效
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：US06316628B1
公开(公告)日：2001-11-13
申请号：US09342149
申请日：1999-06-29
申请人： Shigeya Yamazaki , Taro Ishibashi , Yoshihiro Kawada , Hiroyuki Yumoto , Taichi Yoshikawa , Masami Igi
发明人： Shigeya Yamazaki , Taro Ishibashi , Yoshihiro Kawada , Hiroyuki Yumoto , Taichi Yoshikawa , Masami Igi
IPC分类号： C07D21122
CPC分类号： C07D211/22
摘要： An L-tartrate of a trans-(−)-4-(4-fluorophenyl)-3-hydroxymethylpiperidine compound, represented by the formula (I): 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-(−)-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。

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