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1. 发明授权

US06350880B1 Crystalline or crystallized acid addition salt of losartan and purification method of losartan 失效
标题翻译：氯沙坦的结晶或结晶酸加成盐和氯沙坦的纯化方法
公开(公告)号：US06350880B1
公开(公告)日：2002-02-26
申请号：US09714339
申请日：2000-11-16
申请人： Tadashi Katsura , Hiroshi Shiratani , Nobushige Itaya
发明人： Tadashi Katsura , Hiroshi Shiratani , Nobushige Itaya
IPC分类号： C07D25704
CPC分类号： C07D403/10
摘要： The present invention provides a crystalline or crystallized acid addition salt of Losartan useful for obtaining highly pure 2-n-butyl-4-chloro-1-[[2′-(1H-tetrazol-5-yl)[1,1′-biphenyl]-4-yl]methyl]-1H-imidazole-5-methanol (Losartan), and a purification method of Losartan that includes production of the crystalline or crystallized acid addition salt.
摘要翻译：本发明提供了一种用于获得高纯度2-正丁基-4-氯-1 - [[2' - （1H-四唑-5-基）[1,1'- 联苯] -4-基]甲基] -1H-咪唑-5-甲醇（氯沙坦）和氯沙坦的纯化方法，包括生成结晶或结晶的酸加成盐。

2. 发明授权

US5998652A Process for preparing 2-cyanobiphenyl compound 失效
标题翻译： 2-氰基联苯化合物的制备方法
公开(公告)号：US5998652A
公开(公告)日：1999-12-07
申请号：US009823
申请日：1998-01-20
申请人： Tadashi Katsura , Hiroshi Shiratani , Kiyoshi Sugi , Nobushige Itaya
发明人： Tadashi Katsura , Hiroshi Shiratani , Kiyoshi Sugi , Nobushige Itaya
IPC分类号： C07C253/30 , C07C255/50 , C07C255/00
CPC分类号： C07C253/30
摘要： A process for preparing a 2-cyanobiphenyl compound represented by the formula (II): ##STR1## wherein R.sup.1 is an alkyl group having 1 to 6 carbon atoms, an alkoxy group having 1 to 6 carbon atoms, or hydrogen atom, from a phenylmagnesium chloride compound represented by the formula (I): ##STR2## wherein R.sup.1 is as defined above. According to the process, a 2-cyanobiphenyl compound represented by the formula (II) can be economically, simply, industrially and advantageously prepared.
摘要翻译：一种由式（II）表示的2-氰基联苯化合物的制备方法，其中R 1是具有1至6个碳原子的烷基，具有1至6个碳原子的烷氧基或氢原子，由代表的苯基氯化镁化合物由式（I）表示：其中R1如上所定义。根据该方法，由式（II）表示的2-氰基联苯化合物可以在经济上简单地在工业上有利地制备。

3. 发明授权

US5892094A Process for preparing 4'-methyl-2-cyanobiphenyl 失效
标题翻译：制备4'-甲基-2-氰基联苯的方法
公开(公告)号：US5892094A
公开(公告)日：1999-04-06
申请号：US996341
申请日：1997-12-22
申请人： Tadashi Katsura , Hiroshi Shiratani , Kiyoshi Sugi , Nobushige Itaya
发明人： Tadashi Katsura , Hiroshi Shiratani , Kiyoshi Sugi , Nobushige Itaya
IPC分类号： C07C253/30 , C07C255/50 , C07C255/00
CPC分类号： C07C253/30
摘要： Process for preparing 4'-methyl-2-cyanobiphenyl, comprising, catalytically hydrogenating at least one brominated cyanobiphenyl compound selected from 4'-dibromomethyl-2-cyanobiphenyl and 4'-bromomethyl-2-cyanobiphenyl; and process for regenerating 4'-methyl-2-cyanobiphenyl, comprising, catalytically hydrogenating at least one brominated cyanobiphenyl compound selected from 4'-dibromomethyl-2-cyanobiphenyl and 4'-bromomethyl-2-cyanobiphenyl, contained in a filtrate prepared by brominating 4'-methyl-2-cyanobiphenyl in a solvent; crystallizing 4'-bromomethyl-2-cyanobiphenyl from the resulting reaction mixture; and removing the resulting crystals from the reaction mixture by filtration. 4'-Methyl-2-cyanobiphenyl can be used as starting materials for 4'-bromomethyl-2-cyanobiphenyl.
摘要翻译：制备4'-甲基-2-氰基联苯的方法，包括催化氢化至少一种选自4'-二溴甲基-2-氰基联苯和4'-溴甲基-2-氰基联苯的溴代氰基联苯化合物; 以及用于再生4'-甲基-2-氰基联苯的方法，包括催化氢化选自4-溴 - 二溴甲基-2-氰基联苯和4'-溴甲基-2-氰基联苯中的至少一种溴化氰基联苯化合物，其包含在通过溴化制备的滤液中 4'-甲基-2-氰基联苯; 从所得反应混合物中结晶出4'-溴甲基-2-氰基联苯; 并通过过滤从反应混合物中除去所得晶体。 4'-甲基-2-氰基联苯可用作4'-溴甲基-2-氰基联苯的原料。

4. 发明授权

US06333430B1 Process for preparing tert-alkyl ester from carboxylic acid 有权
标题翻译：从羧酸制备叔烷基酯的方法
公开(公告)号：US06333430B1
公开(公告)日：2001-12-25
申请号：US09561993
申请日：2000-05-02
申请人： Tetsuya Shintaku , Kiyoshi Sugi , Tadashi Katsura , Nobushige Itaya
发明人： Tetsuya Shintaku , Kiyoshi Sugi , Tadashi Katsura , Nobushige Itaya
IPC分类号： C07C6704
CPC分类号： C07C253/30 , C07C67/04 , C07C69/63 , C07C255/19
摘要： A process for preparing a tert-alkyl carboxylic acid ester represented by the formula (III): wherein R1 is an organic group; and each of R2 and R3 is independently an alkyl group having 1 to 4 carbon atoms, comprising reacting a carboxylic acid represented by the formula (I): R1—COOH (I) wherein R1 is as defined above, with a vinylidene compound represented by the formula (II): wherein R2 and R3 are as defined above, in the presence of a phosphorus halide. The tert-alkyl carboxylic acid ester can be used as intermediates for pharmaceuticals such as antibiotics.
摘要翻译：一种制备由式（III）表示的叔烷基羧酸酯的方法：其中R1是有机基团; 其中R 2和R 3各自独立地为具有1至4个碳原子的烷基，包括使由式（I）表示的羧酸：其中R 1如上定义，与由式（II）表示的亚乙烯基化合物反应：其中R2和R3如上定义，在卤化磷存在下。叔烷基羧酸酯可以用作药物如抗生素的中间体。

5. 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。

6. 发明申请

US20070238900A1 Method of Crystallization of Bicalutamide 失效
标题翻译：比卡鲁胺结晶方法
公开(公告)号：US20070238900A1
公开(公告)日：2007-10-11
申请号：US11571956
申请日：2005-07-13
申请人： Tadashi Katsura , Tadashi Mizuno , Nobushige Itaya
发明人： Tadashi Katsura , Tadashi Mizuno , Nobushige Itaya
IPC分类号： C07C261/04
CPC分类号： C07C315/06 , C07C317/46
摘要： The present invention provides a method of crystallization of bicalutamide comprising adding an acetone solution containing bicalutamide to water; crystals of bicalutamide wherein particle size distribution of the crystals is 1 to 10 μm of Dp10, 10 to 25 μm of Dp50 and 25 to 100 μm of Dp90, and the crystals are obtainable by the method described above; and crystals of bicalutamide, wherein particle size distribution of the crystals is 1 to 3 μm of Dp10, 2 to 5 μm of Dp50 and 5 to 15 μm of Dp90.
摘要翻译：本发明提供了比卡鲁胺的结晶方法，包括将含有比卡鲁胺的丙酮溶液加入水中; 其中，结晶的粒径分布为Dp 10〜10μm，Dp <50> 10〜25μm，Dp <！ - SIPO 2〜5μm，Dp < SUB> 90 。

7. 发明授权

US06683207B2 Production method of (R)-3 hydroxy-3-(2-phenylethyl) hexanoic acid and intermediate thereof 失效
标题翻译：（R）-3-羟基-3-（2-苯基乙基）己酸及其中间体的制备方法
公开(公告)号：US06683207B2
公开(公告)日：2004-01-27
申请号：US10320325
申请日：2002-12-16
申请人： Masahide Tanaka , Kozo Matsui , Tadashi Katsura , Mitsuhiro Iwasaki , Hiroshi Maeda , Nobushige Itaya
发明人： Masahide Tanaka , Kozo Matsui , Tadashi Katsura , Mitsuhiro Iwasaki , Hiroshi Maeda , Nobushige Itaya
IPC分类号： C07C5948
CPC分类号： C07C45/74 , C07B2200/07 , C07C45/62 , C07C45/73 , C07C49/213 , C07C51/43 , C07C51/487 , C07C69/732 , C07C211/29 , C07C217/58 , C07C49/217 , C07C59/48
摘要： The present invention relates to a production method of (R)-3-hydroxy-3-(2-phenylethyl)hexanoic acid which comprises optical resolution of racemic 3-hydroxy-3-(2-phenylethyl)hexanoic acid with an optically active amine of the formula (VIII) wherein R2 is 3,4-dimethoxyphenyl or 2-chlorophenyl. According to the present invention, (R)-3-hydroxy-3-(2-phenylethyl)hexanoic acid useful as a starting material of a pharmaceutical agent can be efficiently produced with a high optical purity and a relatively high total yield.
摘要翻译：本发明涉及（R）-3-羟基-3-（2-苯基乙基）己酸的制备方法，该方法包括用光学活性胺将外消旋3-羟基-3-（2-苯基乙基）己酸旋光拆分的式（VIII）其中R 2是3,4-二甲氧基苯基或2-氯苯基。根据本发明，可以以高光学纯度和较高的总产率有效地制备可用作药剂原料的（R）-3-羟基-3-（2-苯基乙基）己酸。

8. 发明授权

US06369266B1 Process for producing tert-butyl 4′-methyl-2-biphenylcarboxlate 失效
标题翻译：制备4'-甲基-2-联苯羧酸叔丁酯的方法
公开(公告)号：US06369266B1
公开(公告)日：2002-04-09
申请号：US09530882
申请日：2000-05-08
申请人： Tetsuya Shintaku , Kiyoshi Sugi , Tadashi Katsura , Nobushige Itaya
发明人： Tetsuya Shintaku , Kiyoshi Sugi , Tadashi Katsura , Nobushige Itaya
IPC分类号： C07C6976
CPC分类号： C07C67/04 , C07C69/76
摘要： A process for preparing tert-butyl 4′-methyl-2-biphenylcarboxylate characterized in that 4′-methyl-2-biphenylcarboxylic acid is reacted with isobutene in the presence of an acid catalyst. According to the present invention, tert-butyl 4′-methyl-2-biphenylcarboxylate having high quality can be conveniently and industrially advantageously prepared in a high yield under mild reaction conditions such as ambient temperatures without complicated procedures or any hazardous solvents.
摘要翻译：一种制备4'-甲基-2-联苯羧酸叔丁酯的方法，其特征在于4'-甲基-2-联苯基羧酸与异丁烯在酸催化剂存在下反应。根据本发明，具有高质量的4'-甲基-2-联苯羧酸叔丁酯可以在温和的反应条件例如环境温度下，无需复杂的方法或任何有害溶剂，以高产率方便地和工业上有利地制备。

9. 发明授权

US07132560B2 Crystal of bicalutamide and production method thereof 有权
标题翻译：比卡鲁胺水晶及其制备方法
公开(公告)号：US07132560B2
公开(公告)日：2006-11-07
申请号：US10740140
申请日：2003-12-18
申请人： Tetsuya Shintaku , Tadashi Katsura , Nobushige Itaya
发明人： Tetsuya Shintaku , Tadashi Katsura , Nobushige Itaya
IPC分类号： C07C255/00
CPC分类号： C07C315/06 , C07B2200/13 , C07C315/02 , C07C317/46
摘要： The present invention relates to a crystal of bicalutamide having a defined form, as well as economical and industrially practical production methods of bicalutamide and a crystal thereof, which are superior in environmental benignity and safety.Accordingly, the present invention provides a production method of bicalutamide represented by the formula (I): which includes at least a step of reacting a compound represented by the formula (3): with an oxidizing agent, a production method of a crystal of bicalutamide, as well as a crystal form of bicalutamide as defined by X-ray diffraction (XRD) or solid 13C NMR measurement.
摘要翻译：本发明涉及具有规定形式的比卡鲁胺的结晶，以及环境友好性和安全性优异的经济和工业实用的比卡鲁胺及其结晶的生产方法。因此，本发明提供由式（I）表示的比卡鲁胺的制造方法：其至少包括使式（3）表示的化合物与氧化剂反应的步骤：比卡鲁胺结晶的制造方法，以及由X射线衍射（XRD）或固体13 C NMR测定所定义的比卡鲁胺的晶体形式。

10. 发明申请

US20060183934A1 Process for producing bicalutamide and method of purifying intermediate thereof 审中-公开
标题翻译：制备比卡鲁胺的方法及其中间体的纯化方法
公开(公告)号：US20060183934A1
公开(公告)日：2006-08-17
申请号：US11401262
申请日：2006-04-11
申请人： Tetsuya Shintaku , Tadashi Katsura , Kiyoshi Sugi , Nobushige Itaya
发明人： Tetsuya Shintaku , Tadashi Katsura , Kiyoshi Sugi , Nobushige Itaya
IPC分类号： C07C255/58
CPC分类号： C07C315/02 , C07C315/06 , C07C317/46
摘要： The present invention provides a process for producing bicartamide of the formula (4); which comprises Step A comprising reacting Compound (1) of the formula (1); with peroxycarboxylic acid to obtain Compound (2) of the formula (2); Step B comprising reacting said Compound (2) with 4-fluorothiophenol to obtain crude crystals of Compound (3) of the formula (3); dissolving the crude crystals in a solvent and crystallizing to obtain purified crystals of Compound (3), and Step C comprising reacting Compound (3) and percarboxylic acid to obtain bicalutamide, and also provides a method for purifying crystals of Compound (3) which comprises dissolving crude crystals of Compound (3) in a solvent and crystallizing.
摘要翻译：本发明提供了式（4）的双卡匹酰胺的制造方法。其包括使式（1）的化合物（1）反应的步骤A; 与过氧羧酸反应得到式（2）的化合物（2）; 步骤B包括使所述化合物（2）与4-氟代苯硫酚反应，得到式（3）化合物（3）的粗晶体; 将粗结晶溶解在溶剂中并结晶，得到化合物（3）的纯化晶体，步骤C包括使化合物（3）与过羧酸反应得到比卡鲁胺，并提供化合物（3）的晶体纯化方法，其中包括将化合物（3）的粗晶体溶解在溶剂中并结晶。

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