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1. 发明授权

US6057480A Process for preparing fluoroaryl magnesium derivative and process for preparing (fluoroaryl) borane compound 失效
标题翻译：制备氟芳基镁衍生物的方法和制备（氟化芳基）硼烷化合物的方法
公开(公告)号：US6057480A
公开(公告)日：2000-05-02
申请号：US930708
申请日：1997-10-16
申请人： Tsunemasa Ueno , Ikuyo Katsumi , Naoko Yamamoto , Hitoshi Mitsui
发明人： Tsunemasa Ueno , Ikuyo Katsumi , Naoko Yamamoto , Hitoshi Mitsui
IPC分类号： C07F3/02 , C07F5/02
CPC分类号： C07F3/02 , C07F5/027
摘要： A fluoroaryl magnesium derivative is produced by reacting aryl fluoride, hydrocarbon halide, and magnesium with one another in an ether solvent or a mixed solvent of the ether solvent and a hydrocarbon solvent. Also, a (fluoroaryl)borane compound is produced by mixing both a solution prepared by dissolving the fluoroaryl magnesium derivative into the ether solvent and another solvent prepared by dissolving the boron halide in the ether solvent with a hydrocarbon solvent having a higher boiling point than the ether solvent, so that the fluoroaryl magnesium derivative and boron halide react with each other while the ether solvent is being distilled out.
摘要翻译： PCT No.PCT / JP97 / 00391 Sec。 371日期：1997年10月16日 102（e）日期1997年10月16日PCT 1997年2月12日提交PCT公布。公开号WO97 / 31924 PCT 日期1997年9月4日氟芳基镁衍生物通过芳基氟化物，烃卤化物和镁在醚溶剂或醚溶剂和烃溶剂的混合溶剂中彼此反应来制备。此外，（氟化芳基）硼烷化合物是通过将通过将氟化芳基镁衍生物溶解在醚溶剂中制备的溶液和通过将卤化硼溶解在醚溶剂中制备的另一种溶剂与沸点高于醚溶剂，使得氟化芳基镁衍生物和卤化硼在蒸出醚溶剂的同时彼此反应。

2. 发明授权

US06291452B1 1,4-benzodiazepinones and their uses as CCK antagonists 失效
标题翻译： 1,4-苯并二氮杂酮及其用作CCK拮抗剂
公开(公告)号：US06291452B1
公开(公告)日：2001-09-18
申请号：US09269752
申请日：1999-04-30
申请人： Yoshinari Sato , Seiichiro Tabuchi , Hitoshi Mitsui , Ikuyo Katsumi , Naoko Yamamoto
发明人： Yoshinari Sato , Seiichiro Tabuchi , Hitoshi Mitsui , Ikuyo Katsumi , Naoko Yamamoto
IPC分类号： A61K315513
CPC分类号： C07K5/0821 , A61K38/00 , C07D243/14 , C07D243/18 , C07K5/0205 , C07K5/06139
摘要： Benzodiazepine derivatives of the formula: wherein R2 is alkyl or cycloalkyl-alkyl when R4 is hydrogen, or R2 is a variety of specified groups when R4 is alkyl, halogen or dialkylamino, are useful as cholecystokinin antagonists.
摘要翻译：下式的苯并二氮杂衍生物：当R 4为氢时，R 2为烷基或环烷基 - 烷基，或者当R 4为烷基，卤素或二烷基氨基时，R 2为多种规定基团，可用作缩胆囊素拮抗剂。

3. 发明授权

US06380435B2 PURIFYING PROCESS OF TETRAKIS(FLUOROARYL)BORATE.MAGNESIUM HALIDE, TETRAKIS(FLUOROARYL)BORATE·ETHER COMPLEX AND PRODUCING PROCESS OF THE SAME, AND PRODUCING PROCESS OF TETRAKIS(FLUOROARYL)BORATE DERIVATIVE 有权
标题翻译：（氟）硼酸盐，氟代硼酸盐（氟代）硼酸盐复合物的制备及其制备方法及其制备方法（氟代）硼酸盐衍生物
公开(公告)号：US06380435B2
公开(公告)日：2002-04-30
申请号：US09779673
申请日：2001-02-09
申请人： Hitoshi Mitsui , Tsunemasa Ueno , Ikuyo Ikeno , Naoko Yamamoto
发明人： Hitoshi Mitsui , Tsunemasa Ueno , Ikuyo Ikeno , Naoko Yamamoto
IPC分类号： C07F502
CPC分类号： C07F5/027
摘要： Tetrakis (fluoroaryl)borate.magnesium halide (Ar4BMgX) expressed by General Formula (1): where each of R1-R10 represents a hydrogen atom, a fluorine atom, a hydrocarbon group, or an alkoxy group, provided that at least one of R1-R5 represents a fluorine atom and at least one of R6-R10 represents a fluorine atom, X represents a chlorine atom, a bromine atom, or an iodide atom, and n represents 2 or 3, is treated with alkali metal salts of carboxylic acid and/or alkali earth metal salts of carboxylic acid. Then, a tetrakis(fluoroaryl)borate derivative (Ar4BZ) is produced by reacting treated Ar4BMgX with a compound generating monovalent cation seeds (for example, N,N-dimethylaniline.hydrochloride). Consequently, it has become possible to provide a purifying process of separating/removing impurities from Ar4BMgX readily and efficiently, and a process of producing inexpensive Ar4BX efficiently.
摘要翻译：由通式（1）表示的四（氟化芳基）硼酸镁卤化物（Ar4BMgX）：其中R1-R10各自表示氢原子，氟原子，烃基或烷氧基，条件是R1 -R5表示氟原子，R6-R10中的至少一个表示氟原子，X表示氯原子，溴原子或碘原子，n表示2或3，用羧酸的碱金属盐处理和/或羧酸的碱土金属盐。然后，通过使处理的Ar4BMgX与产生一价阳离子种子（例如N，N-二甲基苯胺盐酸盐）的化合物反应来制备四（氟化芳基）硼酸盐衍生物（Ar4BZ）。因此，可以容易且高效地提供从Ar4BMgX中分离除去杂质的净化方法，以及有效地制造廉价的Ar4BX的工序。

4. 发明授权

US06683218B1 Process for preparing a tetrakis(fluoroaryl) borate derivative 失效
标题翻译：制备四（氟化芳基）硼酸盐衍生物的方法
公开(公告)号：US06683218B1
公开(公告)日：2004-01-27
申请号：US08955854
申请日：1997-10-21
申请人： Hitoshi Mitsui , Ikuyo Katsumi , Naoko Yamamoto
发明人： Hitoshi Mitsui , Ikuyo Katsumi , Naoko Yamamoto
IPC分类号： C07F502
CPC分类号： C07F5/02
摘要： A fluoroaryl magnesium derivative expressed by General Formula (1): where each of R1-R5 represents a hydrogen atom, a fluorine atom, a hydrocarbon group, or an alkoxy group while at least one of R1-R5 representing a fluorine atom, and Xa represents a chlorine atom, a bromine atom, or an iodine atom; and boron halide expressed by General Formula (2): BXb3 (2) where Xb represents a fluorine atom, a chlorine atom, a bromine atom, or an iodine atom, are reacted with each other in a solvent (a) containing diethyl ether and/or tetrahydrofuran, after which the resulting reaction solution is added to a solvent (b) having a higher boiling point than diethyl ether and/or tetrahydrofuran while diethyl ether and/or tetrahydrofuran are distilled out. Consequently, it has become possible to obtain a (fluoroaryl)borane compound expressed by General Formula (3): where each of R1-R5, and Xb, represents the same as above, and n represents 2 or 3, from which magnesium halide produced as a by-product is separated and removed, selectively in a simple manner at a low cost.
摘要翻译：由通式（1）表示的氟化芳基镁衍生物：其中R1-R5各自表示氢原子，氟原子，烃基或烷氧基，而R1-R5中至少一个表示氟原子，Xa 表示氯原子，溴原子或碘原子; 由通式（2）表示的卤代硼：其中Xb表示氟原子，氯原子，溴原子或碘原子，在含有二乙醚和/或四氢呋喃的溶剂（a）中彼此反应，之后将所得反应溶液加入到沸点比二乙醚和/或四氢呋喃高的溶剂（b）中，同时蒸馏出乙醚和/或四氢呋喃。因此，可以获得由通式（3）表示的（氟化芳基）硼烷化合物：其中R1-R5和Xb各自表示与上述相同的含义，n表示2或3，由此产生卤化镁作为副产物以低成本以简单的方式选择性地分离和除去。

5. 发明授权

US06624329B2 PURIFYING PROCESS OF TETRAKIS (FLUOROARYL) BORATE·MAGNESIUM HALIDE, TETRAKIS (FLUOROARYL) BORATE·ETHER COMPLEX AND PRODUCING PROCESS OF THE SAME, AND PRODUCING PROCESS OF TETRAKIS (FLUOROARYL) BORATE DERIVATIVE 失效
标题翻译：（氟）硼酸盐，氟代硼酸盐（氟代）硼酸盐复合物的制备及其制备方法及其制备方法（氟代）硼酸盐衍生物
公开(公告)号：US06624329B2
公开(公告)日：2003-09-23
申请号：US10024306
申请日：2001-12-21
申请人： Hitoshi Mitsui , Tsunemasa Ueno , Ikuyo Ikeno , Naoko Yamamoto
发明人： Hitoshi Mitsui , Tsunemasa Ueno , Ikuyo Ikeno , Naoko Yamamoto
IPC分类号： C07F502
CPC分类号： C07F5/027
摘要： Tetrakis(fluoroaryl)borate•magnesium halide (Ar4BMgX) expressed by General Formula (1): where each of R1-R10 represents a hydrogen atom, a fluorine atom, a hydrocarbon group, or an alkoxy group, provided that at least one of R1-R5 represents a fluorine atom and at least one of R6-R10 represents a fluorine atom, X represents a chlorine atom, a bromine atom, or an iodide atom, and n represents 2 or 3, is treated with alkali metal salts of carboxylic acid and/or alkali earth metal salts of carboxylic acid. Then, a tetrakis(fluoroaryl)borate derivative (Ar4BZ) is produced by reacting treated Ar4BMgX with a compound generating monovalent cation seeds (for example, N,N-dimethylaniline•hydrochloride). Consequently, it has become possible to provide a purifying process of separating/removing impurities from Ar4BMgX readily and efficiently, and a process of producing inexpensive Ar4BX efficiently.
摘要翻译：由通式（1）表示的四（氟化芳基）硼酸镁卤化物（Ar4BMgX）：其中R1-R10各自表示氢原子，氟原子，烃基或烷氧基，条件是R 1 -R5表示氟原子，R6-R10中的至少一个表示氟原子，X表示氯原子，溴原子或碘原子，n表示2或3，用羧酸的碱金属盐处理和/或羧酸的碱土金属盐。然后，通过使处理的Ar4BMgX与产生一价阳离子种子（例如N，N-二甲基苯胺盐酸盐）的化合物反应来制备四（氟化芳基）硼酸盐衍生物（Ar4BZ）。因此，可以容易且高效地提供从Ar4BMgX中分离除去杂质的净化方法，以及有效地制造廉价的Ar4BX的工序。

6. 发明授权

US06215025B1 Method for purifying tetrakis (fluoroaryl) borate/magnesium halide, tetrakis (fluoroaryl) borate/ether complex and process for preparing the same, and process for preparing tetrakis (fluoroaryl) borate derivative 有权
标题翻译：四（氟化芳基）硼酸盐/卤化镁，四（氟化芳基）硼酸盐/醚络合物及其制备方法的纯化方法以及四（氟化芳基）硼酸盐衍生物的制备方法
公开(公告)号：US06215025B1
公开(公告)日：2001-04-10
申请号：US09171832
申请日：1998-10-26
申请人： Hitoshi Mitsui , Tsunemasa Ueno , Ikuyo Ikeno , Naoko Yamamoto
发明人： Hitoshi Mitsui , Tsunemasa Ueno , Ikuyo Ikeno , Naoko Yamamoto
IPC分类号： C07F502
CPC分类号： C07F5/027
摘要： Tetrakis(fluoroaryl)borate.magnesium halide (Ar4BMgX) expressed by General Formula (1): where each of R1-R10 represents a hydrogen atom, a fluorine atom, a hydrocarbon group, or an alkoxy group, provided that at least one of R1-R5 represents a fluorine atom and at least one of R6-R10 represents a fluorine atom, X represents a chlorine atom, a bromine atom, or an iodide atom, and n represents 2 or 3, is treated with alkali metal salts of carboxylic acid and/or alkali earth metal salts of carboxylic acid. Then, a tetrakis(fluoroaryl)borate derivative (Ar4BZ) is produced by reacting treated Ar4BMgX with a compound generating monovalent cation seeds (for example, N,N-dimethylaniline.hydrochloride). Consequently, it has become possible to provide a purifying process of separating/removing impurities from Ar4BMgX readily and efficiently, and a process of producing inexpensive Ar4BX efficiently.
摘要翻译：由通式（1）表示的四（氟化芳基）硼酸镁卤化物（Ar4BMgX）：其中R1-R10各自表示氢原子，氟原子，烃基或烷氧基，条件是R1 -R5表示氟原子，R6-R10中的至少一个表示氟原子，X表示氯原子，溴原子或碘原子，n表示2或3，用羧酸的碱金属盐处理和/或羧酸的碱土金属盐。然后，通过使处理的Ar4BMgX与产生一价阳离子种子（例如N，N-二甲基苯胺盐酸盐）的化合物反应来制备四（氟化芳基）硼酸盐衍生物（Ar4BZ）。因此，可以容易且高效地提供从Ar4BMgX中分离除去杂质的净化方法，以及有效地制造廉价的Ar4BX的工序。

7. 发明授权

US6118026A Stabilizer for (fluoroaryl)borane compound and methods of stabilizing and crystallizing (fluoroaryl)borane compound 失效
标题翻译：（氟化芳基）硼烷化合物的稳定剂和稳定和结晶（氟化芳基）硼烷化合物的方法
公开(公告)号：US6118026A
公开(公告)日：2000-09-12
申请号：US104042
申请日：1998-06-25
申请人： Hitoshi Mitsui , Tsunemasa Ueno , Ikuyo Ikeno , Naoko Yamamoto
发明人： Hitoshi Mitsui , Tsunemasa Ueno , Ikuyo Ikeno , Naoko Yamamoto
IPC分类号： C07F5/02 , C07C5/02
CPC分类号： C07F5/027
摘要： A (fluoroaryl)borane compound expressed by General Formula (1): ##STR1## where each of R.sub.1 -R.sub.5 represents a hydrogen atom, a fluorine atom, a hydrocarbon group, or an alkoxy group, provided that at least one of R.sub.1 -R.sub.5 represents a fluorine atom, X represents a fluorine atom, a chlorine atom, a bromine atom, or an iodine atom, and n represents 2 or 3, is stabilized by letting inorganic metal salts having a fluorine atom coexist with the (fluoroaryl)borane compound in a hydrocarbon solution. After the hydrocarbon solution is concentrated in the presence of the inorganic metal salts, the inorganic metal salts are removed and the fluoroaryl)borane compound is crystallized. Consequently, it has become possible to provide a method of stabilizing a (fluoroaryl)borane compound by suppressing the decomposition reaction while the solution is heated and concentrated, stored (preserved), or transported/transferred, and a crystallizing method of isolating highly-pure crystals (powders) of the (fluoroaryl)borane compound efficiently.
摘要翻译：由通式（1）表示的（氟化芳基）硼烷化合物：其中R 1 -R 5各自表示氢原子，氟原子，烃基或烷氧基，条件是R 1 -R 5中的至少一个表示氟原子，X表示氟原子，氯原子，溴原子或碘原子，n表示2或3，通过使具有氟原子的无机金属盐与（氟化芳基）硼烷化合物在烃中共存而稳定化解。在无机金属盐存在下将烃溶液浓缩后，除去无机金属盐，并使氟代芳基）硼烷化合物结晶。因此，可以提供一种通过在将溶液加热浓缩，储存（保存）或输送/转移的同时抑制分解反应来稳定（氟化芳基）硼烷化合物的方法，以及分离高纯度（氟化芳基）硼烷化合物的结晶（粉末）有效。

8. 发明授权

US5763437A Benzodiazepine derivatives 失效
标题翻译：苯并二氮杂衍生物
公开(公告)号：US5763437A
公开(公告)日：1998-06-09
申请号：US776196
申请日：1997-01-29
申请人： Yoshinari Sato , Kazuo Sakane , Seiichiro Tabuchi , Hitoshi Mitsui , Ikuyo Katsumi , Yuichi Satoh
发明人： Yoshinari Sato , Kazuo Sakane , Seiichiro Tabuchi , Hitoshi Mitsui , Ikuyo Katsumi , Yuichi Satoh
IPC分类号： C07D243/14 , A61K31/55 , A61K31/551 , A61P1/00 , A61P25/04 , A61P25/18 , C07D243/24 , C07D243/26 , C07D401/06 , C07D403/06 , C07D405/06 , C07D409/06 , C07D413/06 , C07D417/06 , C07D487/08
CPC分类号： C07D243/24
摘要： Benzodiazepine derivatives of formula (I) wherein R.sup.1 is aryl which may have one or more suitable substituent(s), R.sup.2 is C.sub.3 -C.sub.8 cycloalkyl which may have one or more suitable substituent(s), A is lower alkylene, R.sup.3 is a heterocyclic group selected from the group consisting of tetrahydrofuryl, dioxolanyl, filryl, thienyl, isoxazolyl, pyridyl, benzimidazolyl, benzotiazolyl, benzoxazolyl, benzopyrany, quinolyl, isoquinolyl, tetrahydroisoquinolyl, benzothienyl and benzofuryl, each of which may have one or more suitable substituent(s), or a pharmaceutically acceptable salt thereof, which are useful as a medicament.
摘要翻译： PCT No.PCT / JP95 / 01497 Sec。 371日期1997年1月29日 102（e）1997年1月29日PCT PCT 1995年7月27日PCT公布。公开号WO96 / 04254 日期：1996年2月15日，式（I）的苯并二氮杂衍生物，其中R 1为可具有一个或多个合适取代基的芳基，R 2为可具有一个或多个合适取代基的C 3 -C 8环烷基，A为低级亚烷基 R3是选自四氢呋喃基，二氧戊环基，二烯丙基，噻吩基，异恶唑基，吡啶基，苯并咪唑基，苯并噻唑基，苯并恶唑基，苯并吡喃基，喹啉基，异喹啉基，四氢异喹啉基，苯并噻吩基和苯并呋喃基的杂环基，其各自可以具有一个或多个合适的取代基或其药学上可接受的盐，其可用作药物。

9. 发明授权

US06410810B1 Handling method of (fluoroaryl) borane compound and preparing method of hydrocarbon solution 失效
标题翻译：（氟化芳基）硼烷化合物的处理方法和烃溶液的制备方法
公开(公告)号：US06410810B1
公开(公告)日：2002-06-25
申请号：US09512289
申请日：2000-02-24
申请人： Hitoshi Mitsui , Tsunemasa Ueno , Ikuyo Ikeno , Naoko Hirano
发明人： Hitoshi Mitsui , Tsunemasa Ueno , Ikuyo Ikeno , Naoko Hirano
IPC分类号： C07C720
CPC分类号： C07F5/02 , C07F5/027
摘要： A mixture of bis- and tris(fluoroaryl)borane compounds expressed by General Formula (1) below is handled in the form of a slurry made with a hydrocarbon solvent: where each of R1, R2, R3, R4 and R5 independently represents a hydrogen atom, a fluorine atom, a hydrocarbon group, or an alkoxy group provided that at least one of R1-R5 represents a fluorine atom, X represents a fluorine atom, a chlorine atom, a bromine atom, or an iodine atom, and wherein n represents 2 for the bis(fluoroaryl)borane compounds and 3 for the tris(fluoroaryl)borane compounds. Then, a hydrocarbon solution of the (fluoroaryl)borane compounds having a concentration of the tris(fluoroaryl)borane compounds in a range between 1 wt % and 1 wt % is prepared by dissolving the slurry into a hydrocarbon solvent in a virtually air-tight vessel. Consequently, it has become possible to provide a method of handling the tris(fluoroaryl)borane compounds in an industrially and economically advantageous manner, and a method of preparing the hydrocarbon solution of the tris(fluoroaryl)borane compounds readily and quickly without lowering the purity.
摘要翻译：由以下通式（1）表示的双 - 和三（氟芳基）硼烷化合物的混合物以用烃溶剂制备的浆料的形式进行处理：其中R1，R2，R3，R4和R5各自独立地表示氢原子，氟原子，烃基或烷氧基，只要R 1 -R 5中的至少一个表示氟原子，X表示氟原子，氯原子，溴原子或碘原子，并且其中n 对于双（氟芳基）硼烷化合物，代表2，三（氟芳基）硼烷化合物为3。然后，将具有1重量％至1重量％范围内的三（氟芳基）硼烷化合物浓度的（氟化芳基）硼烷化合物的烃溶液通过将该浆料实际上气密地船只。因此，可以以工业上和经济上有利的方式提供三（氟化芳基）硼烷化合物的处理方法，以及容易且快速地制备三（氟芳基）硼烷化合物的烃溶液而不降低纯度的方法。

10. 发明授权

US06812360B2 Process for preparing bis(fluoroaryl)boron derivatives 失效
标题翻译：制备双（氟化芳基）硼衍生物的方法
公开(公告)号：US06812360B2
公开(公告)日：2004-11-02
申请号：US10221029
申请日：2002-09-09
申请人： Ikuyo Ikeno , Hitoshi Mitsui , Toshiya Iida , Toshimitsu Moriguchi
发明人： Ikuyo Ikeno , Hitoshi Mitsui , Toshiya Iida , Toshimitsu Moriguchi
IPC分类号： C07F502
CPC分类号： C07F5/025 , C07F5/027
摘要： Bis(fluoroaryl)borane derivative is produced by reacting tris(fluoroaryl)borane with a compound, such as water, ethanol, ammonia and the like, in a hydrocarbon solvent at a molar ratio raging from 1:0.9 to 1:1.1. It is more preferable that the reaction is carried out while the hydrocarbon solvent is distilled off. It is more preferable that hydrocarbon solvent is substantially an aliphatic hydrocarbon solvent. With this arrangement, it is possible to provide a method for producing and isolating the bis(fluoroaryl)borane derivative of a high purity, with ease and at a low cost.

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