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51. 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。

52. 发明授权

US6147218A 2-phenylpyridine derivative and production method thereof 有权
标题翻译： 2-苯基吡啶衍生物及其制备方法
公开(公告)号：US6147218A
公开(公告)日：2000-11-14
申请号：US370636
申请日：1999-08-06
申请人： Kozo Matsui , Kiyoshi Sugi , Yoshihide Umemoto , Tetsuya Shintaku , Nobushige Itaya
发明人： Kozo Matsui , Kiyoshi Sugi , Yoshihide Umemoto , Tetsuya Shintaku , Nobushige Itaya
IPC分类号： C07D213/26 , C07D213/42 , C07D213/48 , C07D213/02
CPC分类号： C07D213/42 , C07D213/26 , C07D213/48
摘要： A series of compounds capable of deriving an intermediate for the production of a compound (A) of the following formula, ##STR1## which is an anti-HIV drug, and a production method thereof. To be specific, 4-(pyridin-2-yl)benzaldehyde hydrazone, a production method of this compound, and a production method from this compound to N-(tert-butoxycarbonyl)-N'-[4-(pyridin-2-yl)phenylmethyhidene]hydrazine. In addition, a salt of 2-(4-bromomethylphenyl)pyridine, 2-(4-dibromomethylphenyl)pyridine and a salt thereof, production methods of these compounds, and production methods to derive 4-(pyridin-2-yl)benzaldehyde which is a production intermediate for 4-(pyridin-2-yl)benzaldehyde hydrazone from these compounds.
摘要翻译：一系列能产生下式的化合物（A）的中间体的化合物，其为抗HIV药物及其制备方法。具体地说，4-（吡啶-2-基）苯甲醛腙，该化合物的制备方法，以及由该化合物制备N-（叔丁氧基羰基）-N' - [4-（吡啶-2-基）苯基亚甲基]肼。此外，2-（4-溴甲基苯基）吡啶，2-（4-二溴甲基苯基）吡啶及其盐的盐，这些化合物的制备方法和得到4-（吡啶-2-基）苯甲醛的制备方法是来自这些化合物的4-（吡啶-2-基）苯甲醛腙的生产中间体。

53. 发明授权

US3989654A Process for preparing cis-chrysanthemic acid 失效
标题翻译：顺式菊酸的制备方法
公开(公告)号：US3989654A
公开(公告)日：1976-11-02
申请号：US500018
申请日：1974-08-23
申请人： Toshiko Honda , Nobushige Itaya , Akio Higo , Fukashi Horiuchi
发明人： Toshiko Honda , Nobushige Itaya , Akio Higo , Fukashi Horiuchi
IPC分类号： C07C61/04
摘要： A novel process for preparing cis-chrysanthemic acid comprising (1) hydrolysis of trans-.delta.-halogenodihydrochrysanthemic acid or ester thereof under neutrally kept condition with an alkaline earth metal carbonate, (2) conversion of the obtained trans-.delta.-hydroxydihydrochrysanthemic acid ester into a mixture of cis-chrysanthemic acid and iso-cis-chrysanthemic acid by reacting with a strong base, and (3) separation of the cis-chrysanthemic acid from the mixture by selective conversion of the iso-cis-chrysanthemic acid with water in the presence of an acid catalyst into cis-dihydrochrysanthemolactone, followed by separation of the cis-chrysanthemic acid from the lactone with a caustic alkali and an acid.The present process is very useful for converting (-)-trans-chrysanthemic acid which is obtained, as a main remainder of racemic chrysanthemic acid prepared industrially, after (+)-trans-chrysanthemic acid was used for preparation of (+)-trans-chrysanthemic acid ester having a high insecticidal activity, into (+)-cis-chrysanthemic acid which is industrially valuable for preparation of insecticides.
摘要翻译：一种制备顺式菊酸的新方法，其包括：（1）在中性保持条件下用碱土金属碳酸盐水解反式δ-卤代二氢菊酸或其酯，（2）将所得反式δ-羟基二氢菊酸酯转化为通过与强碱反应，顺式 - 菊酸和异顺式菊酸的混合物，和（3）通过选择性地将异顺式菊酸与水分离，从而将顺式菊酸与混合物分离将酸催化剂存在于顺式二氢菊花内酯中，然后用苛性碱和酸从内酯中分离顺式菊酸。

54. 发明授权

US07632971B2 Method of crystallization of bicalutamide 失效
标题翻译：比卡鲁胺结晶方法
公开(公告)号：US07632971B2
公开(公告)日：2009-12-15
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： C07C233/05 , C07C255/50
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; 其中晶体的粒径分布为Dp10的1-10μm，Dp50为10〜25μm，Dp90为25〜100μm，并且可以通过上述方法得到结晶。和比卡鲁胺的晶体，其中晶体的粒度分布为Dp10的1-3μm，Dp50为2-5μm，Dp90为5-15μm。

55. 发明授权

US07038075B2 Production method of racemic 3-hydroxy-3-(2-phenylethyl)hexanoic acid C1-6 alkyl ester 失效
标题翻译：外消旋3-羟基-3-（2-苯基乙基）己酸C 1-6烷基酯的制备方法
公开(公告)号：US07038075B2
公开(公告)日：2006-05-02
申请号：US10727398
申请日：2003-12-04
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： C07C69/66
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。

56. 发明授权

US06730803B2 Synthetic intermediate for epothilone derivative and production method thereof 失效
标题翻译：埃坡霉素衍生物的合成中间体及其制备方法
公开(公告)号：US06730803B2
公开(公告)日：2004-05-04
申请号：US10260946
申请日：2002-09-30
申请人： Mitsuhiro Iwasaki , Kiyoshi Sugi , Hideto Miyamoto , Nobushige Itaya
发明人： Mitsuhiro Iwasaki , Kiyoshi Sugi , Hideto Miyamoto , Nobushige Itaya
IPC分类号： C07C25500
CPC分类号： C07D417/06 , C07B2200/07 , C07C253/30 , C07C255/21 , C07D319/06 , C07D493/04 , C07C255/12 , C07C255/20
摘要： The &bgr;-keto ester compound, &bgr;-hydroxy acid compound and acetonide form of a 1,3-diol derivative of the formulas (I), (V) and (VIII) wherein each symbol is as defined in the specification, are useful as a synthetic intermediate for an epothilone derivative being developed as a pharmaceutical agent having an antitumor activity.
摘要翻译：式（I），（V）和（VIII）的1,3-二醇衍生物的β-酮酯化合物，β-羟基酸化合物和丙酮化物形式，其中每个符号如说明书中所定义，可用作作为具有抗肿瘤活性的药剂开发埃坡霉素衍生物的合成中间体。

57. 发明授权

US06365745B1 Method for producing hydrazine derivative 有权
标题翻译：肼衍生物的制备方法
公开(公告)号：US06365745B1
公开(公告)日：2002-04-02
申请号：US09905442
申请日：2001-07-13
申请人： Kozo Matsui , Kiyoshi Sugi , Hiromi Suga , Nobushige Itaya
发明人： Kozo Matsui , Kiyoshi Sugi , Hiromi Suga , Nobushige Itaya
IPC分类号： C07D21304
CPC分类号： C07C281/02 , C07C241/04 , C07C243/32
摘要： The present invention provides a method for producing a hydrazine derivative of the formula [2]: wherein R1 is alkyl group having 1-12 carbon atoms and the like, R2 is alkyl group having 1-12 carbon atoms and the like, and Ar is phenylene group and the like, from a hydrazone derivative of the formula [1] wherein R1, R2 and Ar are as defined above, in the presence of at least one base selected from the group consisting of an organic base and an inorganic base, and a metal hydrogenating catalyst. By this method, reduction proceeds selectively and a hydrogenolysis reaction (side reaction) can be suppressed.
摘要翻译：本发明提供式[2]的肼衍生物的制造方法，其中R1为具有1-12个碳原子的烷基等，R2为具有1-12个碳原子的烷基等，Ar为亚苯基等，由式[1]的腙衍生物，其中R 1，R 2和Ar如上定义，在至少一种选自有机碱和无机碱的碱的存在下，和金属氢化催化剂。通过该方法，可以选择性地还原还原，可以抑制氢解反应（副反应）。

58. 发明授权

US06268503B1 2-phenylpyridine derivative and production method thereof 有权
标题翻译： 2-苯基吡啶衍生物及其制备方法
公开(公告)号：US06268503B1
公开(公告)日：2001-07-31
申请号：US09611991
申请日：2000-07-07
申请人： Kozo Matsui , Kiyoshi Sugi , Yoshihide Umemoto , Tetsuya Shintaku , Nobushige Itaya
发明人： Kozo Matsui , Kiyoshi Sugi , Yoshihide Umemoto , Tetsuya Shintaku , Nobushige Itaya
IPC分类号： C07D21326
CPC分类号： C07D213/42 , C07D213/26 , C07D213/48
摘要： A series of compounds capable of deriving an intermediate for the production of compound (A) of the following formula, which is an anti-HIV drug, and a production method thereof. To be specific, 4-(pyridin-2-yl)benzaldehyde hydrazone, a production method of this compound, and a production method from this compound to N-(tert-butoxycarbonyl)-N′-[4-(pyridin-2-yl)phenylmethylidene]hydrazine. In addition, a salt of 2-(4-bromomethylphenyl)pyridine, 2-(4-dibromomethylphenyl)pyridine and a salt thereof, production methods of these compounds, and production methods to derive 4-(pyridin-2-yl)benzaldehyde which is a production intermediate for 4-(pyridin-2-yl)benzaldehyde hydrazone from these compounds.
摘要翻译：一系列能够得到用于制备作为抗HIV药物的下式化合物（A）的中间体的化合物及其制备方法。具体地说，4-（吡啶-2-基）苯甲醛腙，该化合物的制备方法，以及由该化合物制备N-（叔丁氧基羰基）-N' - [4-（吡啶-2-基）苯基亚甲基]肼。此外，2-（4-溴甲基苯基）吡啶，2-（4-二溴甲基苯基）吡啶及其盐的盐，这些化合物的制备方法和得到4-（吡啶-2-基）苯甲醛的制备方法是来自这些化合物的4-（吡啶-2-基）苯甲醛腙的生产中间体。

59. 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。

60. 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。

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