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1. 发明授权

US5679859A Process for producing improved crystals of 3-amino-2-hydroxyacetophenone salt 失效
标题翻译：制备3-氨基-2-羟基苯乙酮盐的改性晶体的方法
公开(公告)号：US5679859A
公开(公告)日：1997-10-21
申请号：US616082
申请日：1996-03-14
申请人： Hirokazu Murata , Hideki Ushio , Atsushi Furutani , Hiroaki Hibino , Etsuko Fukuda
发明人： Hirokazu Murata , Hideki Ushio , Atsushi Furutani , Hiroaki Hibino , Etsuko Fukuda
IPC分类号： C07C225/22 , C07C209/82
CPC分类号： C07C225/22
摘要： The present invention concerns a process for producing crystals of 3-amino-2-hydroxyacetophenone salt having a high bulk density and improved flow properties, by treating 3-amino-2-hydroxyacetophenone of formula (1) ##STR1## or hydrogen halide salt thereof with sulfuric acid, in a solvent.
摘要翻译：本发明涉及一种通过处理式（1）的3-氨基-2-羟基苯乙酮或其卤化氢盐来制备具有高堆积密度和改善流动性的3-氨基-2-羟基苯乙酮盐晶体的方法用硫酸，在溶剂中。

2. 发明授权

US5675036A Process for preparing aromatic amide compound 失效
标题翻译：制备芳香族酰胺化合物的方法
公开(公告)号：US5675036A
公开(公告)日：1997-10-07
申请号：US673441
申请日：1996-06-28
申请人： Etsuko Fukuda , Atsushi Furutani , Hideki Ushio , Hirokazu Murata
发明人： Etsuko Fukuda , Atsushi Furutani , Hideki Ushio , Hirokazu Murata
IPC分类号： C07C67/31 , C07C231/02
CPC分类号： C07C231/02 , C07C67/31
摘要： 3-�4-(4-Phenyl-1-butoxy)benzoyl!amino-2-hydroxyacetophenone is prepared by reacting a benzoate ester with a halobutylbenzene in the presence of a basic compound and an aprotic polar compound in an aromatic hydrocarbon solvent to obtain a corresponding ether, alkali hydrolyzing the ether in an aromatic hydrocarbon solvent and precipitating a hydrolysate with an acid to obtain 4-(4-phenyl-1-butoxy)benzoic acid, reacting a halogenating agent with this benzoic acid derivative in an aromatic hydrocarbon solvent to obtain an acid halide, and reacting the acid halide in an aromatic hydrocarbon solvent with a corresponding aromatic amine.
摘要翻译：通过苯甲酸酯与卤代丁基苯在碱性化合物和非质子极性化合物存在下在芳族烃溶剂中反应制备3- [4-（4-苯基-1-丁氧基）苯甲酰基]氨基-2-羟基苯乙酮，得到相应的醚，在芳族烃溶剂中碱解水解醚并用酸沉淀水解产物，得到4-（4-苯基-1-丁氧基）苯甲酸，将卤代剂与该苯甲酸衍生物在芳族烃溶剂以获得酰卤，并使芳族烃溶剂中的酰卤与相应的芳族胺反应。

3. 发明授权

US06753431B2 Production of mixed acid anhydride and amide compound 失效
标题翻译：混合酸酐和酰胺化合物的生产
公开(公告)号：US06753431B2
公开(公告)日：2004-06-22
申请号：US09870676
申请日：2001-06-01
申请人： Takashi Miki , Hideki Ushio , Isao Kurimoto
发明人： Takashi Miki , Hideki Ushio , Isao Kurimoto
IPC分类号： C07D21122
CPC分类号： C07K5/06026 , A61K38/00 , C07C269/06 , C07D277/46 , C07F9/096 , C07F9/3294 , C07C271/22
摘要： There is disclosed an advantageous mixed acid anhydride production method of formula (1): R1C(O)OY(O)n(R2)p (1) wherein R1, R2 and Y denote the same as defined below, n and p denote an integer of 1 or 2, which is characterized by adding a carboxylic acid of formula (2); R1COOH (2) wherein R1 denotes a hydrogen atom, an optionally substituted alkyl group or the like, an organic base to a solution of a carboxylic acid activating agent of formula (3); (R2)pY(O)nX (3) wherein R2 denotes an optionally substituted aliphatic hydrocarbyl group or the like, Y denotes a carbon atom, a phosphorus atom, or a sulfur atom, and X denotes a chlorine atom or the like.
摘要翻译：公开了式（1）的有利的混合酸酐的制备方法：其中R 1，R 2和Y表示与下面定义的相同，n和p表示1或2的整数，其特征在于加入式（2）的羧酸;其中R 1表示氢原子，任选取代的烷基等，式（3）的羧酸活化剂的溶液中的有机碱：其中R 1， 2>表示任选取代的脂族烃基等，Y表示碳原子，磷原子或硫原子，X表示氯原子等。

4. 发明授权

US6114543A Process for producing optically active azetidine-2-carboxylic acid 有权
标题翻译：光学活性氮杂环丁烷-2-羧酸的制备方法
公开(公告)号：US6114543A
公开(公告)日：2000-09-05
申请号：US128974
申请日：1998-08-04
申请人： Hideki Ushio , Naoyuki Takano , Yukihiro Honda , Shinzo Seko , Motoo Hazama
发明人： Hideki Ushio , Naoyuki Takano , Yukihiro Honda , Shinzo Seko , Motoo Hazama
IPC分类号： C07D205/04
CPC分类号： C07D205/04
摘要： The present invention provides a process for preparing optically active azetidine-2-carboxylic acids using readily available reagents of relatively low price in the industry. Thus, there is provided optically active azetidine-2-carboxylic acid, and a process for producing the same by subjecting optically active N-(alkylbenzyl)azetidine-2-carboxylic acid represented by the formula (1): ##STR1## to hydrogenolysis in the presence of a catalyst.
摘要翻译：本发明提供了使用工业中价格相对较低的容易获得的试剂制备光学活性氮杂环丁烷-2-羧酸的方法。因此，提供光学活性的氮杂环丁烷-2-羧酸及其制备方法，其中式（1）表示的光学活性的N-（烷基苄基）氮杂环丁烷-2-羧酸：在催化剂

5. 发明授权

US6063940A Process for preparing 1-bromoalkylbenzene derivatives and intermediates thereof 失效
标题翻译：制备1-溴烷基苯衍生物的方法及其中间体
公开(公告)号：US6063940A
公开(公告)日：2000-05-16
申请号：US800173
申请日：1997-02-13
申请人： Hiroaki Fujishima , Yasunobu Miyamoto , Masayoshi Minai , Tsutomu Matsumoto , Hideki Ushio , Takayuk Higashii
发明人： Hiroaki Fujishima , Yasunobu Miyamoto , Masayoshi Minai , Tsutomu Matsumoto , Hideki Ushio , Takayuk Higashii
IPC分类号： C07C15/44 , C07C17/08 , C07C17/087 , C07C17/26 , C07C41/22 , C07F3/02 , C07D319/14 , C07C41/00
CPC分类号： C07C17/2632 , C07C15/44 , C07C17/08 , C07C17/087 , C07C41/22 , C07F3/02
摘要： A 1-bromoalkylbenzene derivative is prepared by reacting a phenylalkene derivative with hydrogen bromide in the presence of a non-polar solvent. The phenylalkene derivative is prepared by reacting an alkenyl halide with metal magnesium to form a Grignard reagent, and then reacting the Grignard reagent with a benzyl halide derivative. An allyl Grignard reagent is prepared by reacting continuously an allyl halide derivative with metal magnesium in an organic solvent, in which the allyl halide derivative and metal magnesium are continuously added to the reaction system and the allyl Grignard reagent formed is continuously removed from the reaction system. The processes provide the intended compounds in high yields, high selectivities and high purities.
摘要翻译：通过在非极性溶剂存在下使苯基烯烃衍生物与溴化氢反应来制备1-溴烷基苯衍生物。苯基烯烃衍生物通过烯基卤化物与金属镁反应形成格氏试剂制备，然后使格利雅试剂与苄基卤衍生物反应。通过连续将烯丙基卤衍生物与金属镁在有机溶剂中连续反应制备烯丙基格氏试剂，其中将烯丙基卤衍生物和金属镁连续加入到反应体系中，形成的烯丙基格氏试剂从反应体系中连续除去。这些方法以高产率，高选择性和高纯度提供目标化合物。

6. 发明授权

US5874593A Production process and intermediate of tetrazole compound 失效
标题翻译：四唑化合物的生产工艺和中间体
公开(公告)号：US5874593A
公开(公告)日：1999-02-23
申请号：US592375
申请日：1996-02-08
申请人： Hideki Ushio , Takayuki Higashii , Masayoshi Minai , Akihiko Nakamura
发明人： Hideki Ushio , Takayuki Higashii , Masayoshi Minai , Akihiko Nakamura
IPC分类号： C07C251/86 , C07C257/18 , C07C257/22 , C07D257/04 , C07D405/04
CPC分类号： C07D257/04 , C07C251/86 , C07C257/18 , C07C257/22 , C07D405/04
摘要： There are disclosed an industrially favorable process for producing a tetrazole compound of general formula (1): ##STR1## characterized in that a nitrile of general formula (2):R.sup.1 CN (2)is reacted with hydrazine or a salt thereof in the presence of a catalyst, followed by reaction with a nitrous acid compound of general formula (3):ANO.sub.2 (3)or a nitrile of general formula (2) is reacted with hydrogen sulfide, followed by reaction with an alkyl halide of general formula (4):R.sup.4 J (4)with hydrazine or a salt thereof, and then with a nitrous acid compound of general formula (3); and an intermediate of general formula (5):R.sup.1 C(=R.sup.5)R.sup.6 (5)which is useful for the production of the tetrazole compound (in which R.sup.1 to R.sup.6, A and J in the above formulas are as defined in the specification).
摘要翻译： PCT No.PCT / JP95 / 00919 Sec。 371日期1996年2月8日 102（e）日期1996年2月8日PCT提交1995年5月15日PCT公布。出版物WO95 / 31445 日本公开了1995年11月23日的通式（1）的四唑化合物的工业上有利的方法：其中通式（2）的腈：R1CN（2）与肼或其盐在催化剂存在下反应，随后与通式（3）的亚硝酸化合物：ANO2（3）或通式（2）的腈反应与硫化氢反应，随后与通式（4）的烷基卤化物：R4J（4）与肼或其盐，然后与通式（3）的亚硝酸化合物反应; 和通式（5）的中间体：可用于制备四唑化合物的R1C（= R5）R6（5）（上述式中的R1至R6，A和J如说明书中所定义）。

7. 发明申请

US20090118519A1 Production Method of Polycyclic Lactams 审中-公开
标题翻译：多环内酰胺的生产方法
公开(公告)号：US20090118519A1
公开(公告)日：2009-05-07
申请号：US12297113
申请日：2006-06-28
申请人： Norihiko Hirata , Toshitsugi Uemura , Hideki Ushio
发明人： Norihiko Hirata , Toshitsugi Uemura , Hideki Ushio
IPC分类号： C07D209/48
CPC分类号： C07D209/48 , C07D209/52
摘要： A process for producing lactams of formula (1) below, including the step of reacting lactones of formula (2) below with imides of any of formulae (3a), (3b) and (3c) to thereby obtain corresponding carboxylic acids (step A); the step of esterifying the carboxylic acids into corresponding esters (step B); and the step of reacting the esters with amines to thereby obtain lactams of the formula (1) (step C). In the formulae (1)-(2) and (3a)-(3c), when R3 and R4 are simultaneously hydrogen atoms, R is a substituted methylene or optionally substituted polymethylene; when at least one of R3 and R4 is a substituent other than hydrogen atom, R is an optionally substituted methylene or polymethylene; each of R3, R4, R5 and R6 independently is a hydrogen atom, a halogen atom, cyano, etc.; each of A1, A2, A3, A4, A5, A6, A7, A8, A9 and A10 independently is a hydrogen atom, a halogen atom, nitro, etc.; and M is a hydrogen atom or an alkali metal atom.
摘要翻译：一种生产下式（1）的内酰胺的方法，包括使下式（2）的内酯与式（3a），（3b）和（3c）中任一式的酰亚胺反应的步骤，从而得到相应的羧酸（步骤A ）; 将羧酸酯化成相应的酯（步骤B）的步骤; 以及使酯与胺反应从而得到式（1）的内酰胺（步骤C）的步骤。在式（1） - （2）和（3a） - （3c）中，当R3和R4同时为氢原子时，R为取代的亚甲基或任选取代的聚亚甲基; 当R 3和R 4中的至少一个是除氢原子以外的取代基时，R是任选取代的亚甲基或聚亚甲基; R 3，R 4，R 5和R 6各自独立地为氢原子，卤原子，氰基等; A1，A2，A3，A4，A5，A6，A7，A8，A9和A10各自独立地为氢原子，卤素原子，硝基等; M是氢原子或碱金属原子。

8. 发明授权

US06653507B2 Process for producing optically active 3,3,3-trifluoro-2-hydroxy-2-methylpropionic acid, and salt thereof 失效
标题翻译：光学活性3,3,3-三氟-2-羟基-2-甲基丙酸的制备方法及其盐
公开(公告)号：US06653507B2
公开(公告)日：2003-11-25
申请号：US10147966
申请日：2002-05-20
申请人： Miyuki Oikawa , Hideki Ushio , Isao Kurimoto , Takayuki Higashii
发明人： Miyuki Oikawa , Hideki Ushio , Isao Kurimoto , Takayuki Higashii
IPC分类号： C07C21100
CPC分类号： C07C251/24 , C07B2200/07 , C07C51/412 , C07C51/43 , C07C59/115 , C07C211/27 , C07C211/29 , C07C217/58
摘要： There are disclosed are A diastereomer salt of formula (1): a process for producing the same, a process for producing optically active 3,3,3-trifluoro-2-hydroxy-2-methylpropionic acid of formula (2′): a novel optically active amine compound of formula (4): a novel optically active amine compound of formula (8): an imine compound of formula (7) or (11):
摘要翻译：公开了式（1）的非对映异构体盐：其制备方法，制备式（2'）的光学活性3,3,3-三氟-2-羟基-2-甲基丙酸的方法：a 式（4）的新型光学活性胺化合物：式（8）的新型光学活性胺化合物：式（7）或（11）的亚胺化合物：

9. 发明授权

US5659051A Process of producing 2-cyano-4-oxo-4H-benzopyran compounds 失效
标题翻译：制备2-氰基-4-氧代-4H-苯并吡喃化合物的方法
公开(公告)号：US5659051A
公开(公告)日：1997-08-19
申请号：US273119
申请日：1994-07-11
申请人： Takayuki Higashii , Hideki Ushio , Yukari Fujimoto , Tsutomu Matsumoto , Masayoshi Minai , Katsuichi Yasunaga , Hiroshi Sogabe , Takahiro Kotera
发明人： Takayuki Higashii , Hideki Ushio , Yukari Fujimoto , Tsutomu Matsumoto , Masayoshi Minai , Katsuichi Yasunaga , Hiroshi Sogabe , Takahiro Kotera
IPC分类号： C07D311/24
CPC分类号： C07D311/24
摘要： There is disclosed a process of producing a 2-cyano-4-oxo-4H-benzopyran compound of the general formula (2): ##STR1## wherein R.sup.1 and R.sup.2 are independently hydrogen, halogen, hydroxy, C.sub.1 -C.sub.5 alkyl, C.sub.1 -C.sub.5 alkoxy, nitro or a group of the RCONH wherein R is C.sub.1 -C.sub.20 alkyl, phenyl, phenyl-substituted (C.sub.1 -C.sub.20) alkyl, phenyl (C.sub.1 -C.sub.20)alkoxyphenyl or (C.sub.1 -C.sub.20) alkoxyphenyl. This production process is characterized in that a carboxamide of the general formula (1): ##STR2## wherein R.sup.1 and R.sup.2 are each as defined above, is reacted with a dehydrating agent in the presence of a pyridine compound of the general formula (4): ##STR3## wherein A.sup.1 and A.sup.2 are independently hydrogen or C.sub.1 -C.sub.5 alkyl. If the final product cannot be obtained as crystals having good filtration properties by ordinary treatments, a novel technique as disclosed herein can provide such crystals by dissolving the reaction product in an organic solvent insoluble or slightly soluble in water; pouring the resultant solution into water; and removing the organic solvent by distillation with stirring to effect the crystallization of the final product.
摘要翻译：公开了通式（2）的2-氰基-4-氧代-4H-苯并吡喃化合物的制备方法：其中R 1和R 2独立地是氢，卤素，羟基，C 1 -C 5烷基硝基或其中R为C 1 -C 20烷基，苯基，苯基取代的（C 1 -C 20）烷基，苯基（C 1 -C 20）烷氧基苯基或（C 1 -C 20）烷氧基苯基）的RCONH基团。该制造方法的特征在于通式（1）的羧酰胺：其中R 1和R 2各自如上所定义，与脱水剂在通式（Ⅴ）的吡啶化合物存在下反应，（4）：其中A1和A2独立地为氢或C1-C5烷基。如果通过常规处理不能获得具有良好过滤性能的结晶的最终产品，则本文公开的新技术可以通过将反应产物溶解在不溶或微溶于水的有机溶剂中来提供这种晶体; 将所得溶液倒入水中; 并在搅拌下通过蒸馏除去有机溶剂以实现最终产物的结晶。

10. 发明授权

US06894190B2 Process for producing optically active 3,3,3-trifluoro-2-hydroxy-2-methylpropionic acid, and salt thereof 失效
标题翻译：光学活性3,3,3-三氟-2-羟基-2-甲基丙酸的制备方法及其盐
公开(公告)号：US06894190B2
公开(公告)日：2005-05-17
申请号：US10603941
申请日：2003-06-26
申请人： Miyuki Oikawa , Hideki Ushio , Isao Kurimoto , Takayuki Higashii
发明人： Miyuki Oikawa , Hideki Ushio , Isao Kurimoto , Takayuki Higashii
IPC分类号： C07C51/41 , C07C51/43 , C07C59/115 , C07C211/27 , C07C211/29 , C07C217/58 , C07C251/24 , C07C211/00
CPC分类号： C07C251/24 , C07B2200/07 , C07C51/412 , C07C51/43 , C07C59/115 , C07C211/27 , C07C211/29 , C07C217/58
摘要： There are disclosed imine compounds of formula (7) and (11), and processes for preparing the same:
摘要翻译：公开了式（7）和（11）的亚胺化合物及其制备方法：

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