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1. 发明授权

US06340762B2 Method for optical resolution of piperidine carboxylic acid derivative 失效
标题翻译：哌啶羧酸衍生物的光学拆分方法
公开(公告)号：US06340762B2
公开(公告)日：2002-01-22
申请号：US09802916
申请日：2001-03-12
申请人： Isao Hashiba , Masami Kozawa , Kiyotomo Seto
发明人： Isao Hashiba , Masami Kozawa , Kiyotomo Seto
IPC分类号： C07D21112
CPC分类号： C07D211/32 , Y02P20/55
摘要： A method for producing an optically active piperidine carboxylic acid derivative, which comprises subjecting a piperidine carboxylic acid derivative of the formula (1): wherein Z is a protecting group for the carboxyl group, to optical resolution by means of an optical resolution agent of the formula (2): wherein symbol * indicates that the designated carbon atom is asymmetric.
摘要翻译：一种光学活性哌啶羧酸衍生物的制备方法，其包括使式（1）的哌啶羧酸衍生物：其中Z为羧基的保护基，通过光学拆分剂式（2）：其中符号*表示指定的碳原子是不对称的。

2. 发明授权

US06140506A Oxazolidinone compounds and process for the preparation thereof 失效
标题翻译：恶唑烷酮化合物及其制备方法
公开(公告)号：US06140506A
公开(公告)日：2000-10-31
申请号：US222918
申请日：1998-12-30
申请人： Akio Baba , Kenji Suzuki , Yoshinobu Yanagawa , Yoko Ohkuni , Takashi Oda , Masao Shimada , Masami Kozawa
发明人： Akio Baba , Kenji Suzuki , Yoshinobu Yanagawa , Yoko Ohkuni , Takashi Oda , Masao Shimada , Masami Kozawa
IPC分类号： C07D263/52 , C07D263/62
CPC分类号： C07D263/52
摘要： The present invention produces novel cis-oxazolidinone compound which is racemic form or optically active form, of a formula (1) ##STR1## wherein R represents C.sub.1 -C.sub.6 alkyl group, C.sub.2 -C.sub.6 alkenyl group, C.sub.1 -C.sub.6 alkoxyl group, C.sub.1 -C.sub.6 alkylamino group, aryl group or halogen atom, and oxazolidinone ring is at cis-configuration, comprising reacting cis-1,2-indene epoxide of a formula (3) ##STR2## form, with sulfonyl isocyanate compound of a formula (4) ##STR3## in the presence of metal halide catalyst. Further, cis-1-amino-2-indanol is produced by hydrolyzing the oxazolidinone compound. The latter compound is useful as an intermediate of HIV-drug.
摘要翻译：本发明产生式（1）的外消旋形式或旋光形式的新型顺 - 恶唑烷酮化合物，其中R代表C1-C6烷基，C2-C6烯基，C1-C6烷氧基，C1-C6烷基氨基，芳基或卤素原子，恶唑烷酮环为顺式构型，包括使式（3）形式的顺式-1,2-茚环氧化物与式（4）的磺酰基异氰酸酯化合物在金属卤化物存在下反应催化剂。此外，通过水解恶唑烷酮化合物制备顺式-1-氨基-2-茚满醇。后一种化合物可用作HIV药物的中间体。

3. 发明申请

US20100311977A1 METHOD FOR PRODUCING 2-AZAADAMANTANE 有权
标题翻译：生产2-氮杂AD啶的方法
公开(公告)号：US20100311977A1
公开(公告)日：2010-12-09
申请号：US12744015
申请日：2008-11-20
申请人： Toshimasa Hamada , Noriaki Nagahama , Masami Kozawa , Yoshiharu Iwabuchi , Masatoshi Shibuya , Masaki Tomizawa , Yusuke Sasano
发明人： Toshimasa Hamada , Noriaki Nagahama , Masami Kozawa , Yoshiharu Iwabuchi , Masatoshi Shibuya , Masaki Tomizawa , Yusuke Sasano
IPC分类号： C07D451/14 , C07C271/24 , C07C211/41 , C07C61/29 , C07C247/00
CPC分类号： C07D451/14
摘要： To provide a method whereby a 2-azaadamantane can easily be obtained in good yield.A method for producing a 2-azaadamantane represented by the formula (1), which comprises cyclizing a compound represented by the following formula (2) in the presence of an acid.
摘要翻译：提供可以容易地以良好的产率获得2-氮杂金刚烷的方法。一种制备由式（1）表示的2-氮杂金刚烷的方法，其包括在酸存在下环化下式（2）表示的化合物。

4. 发明申请

US20100004464A1 Method for producing succinimide compound 失效
标题翻译：琥珀酰亚胺化合物的制备方法
公开(公告)号：US20100004464A1
公开(公告)日：2010-01-07
申请号：US12311284
申请日：2007-09-26
申请人： Masami Kozawa , Hideki Musashi
发明人： Masami Kozawa , Hideki Musashi
IPC分类号： C07D207/40
CPC分类号： C07D207/416
摘要： There is provided a method for producing a succinimide compound. The method for producing a succinimide compound of formula (3) comprises reacting an aminomalonic ester compound of formula (1) with a compound of formula (2) in a solvent in the presence of a base, wherein an alcohol is used as the solvent and an alkali metal alkoxide is used as the base. (where R1 and R4 independently represent an alkyl group having 1 to 12 carbon atom(s) which may be a straight chain, branched or cyclic, etc., R2 and R3 independently represent a hydrogen atom, etc., R5 represents an alkyl group having 1 to 12 carbon atom(s) which may be straight chain, branched or cyclic, etc.)
摘要翻译：提供了琥珀酰亚胺化合物的制造方法。制备式（3）的琥珀酰亚胺化合物的方法包括使式（1）的氨基马来酸酯化合物与式（2）的化合物在溶剂中在碱的存在下反应，其中使用醇作为溶剂，使用碱金属醇盐作为碱。（其中R 1和R 4独立地表示可以是直链，支链或环状等的具有1至12个碳原子的烷基，R 2和R 3独立地表示氢原子等，R 5表示烷基具有1至12个碳原子，其可以是直链，支链或环状等）

5. 发明授权

US07038056B2 Method for preparing a 7-quinolinyl-3,5-dihydroxyhept-6-enoate 失效
标题翻译： 7-喹啉基-3,5-二羟基庚-6-烯酸酯的制备方法
公开(公告)号：US07038056B2
公开(公告)日：2006-05-02
申请号：US10473132
申请日：2002-03-22
申请人： Kenichi Tokunaga , Masami Kozawa , Kenji Suzuki
发明人： Kenichi Tokunaga , Masami Kozawa , Kenji Suzuki
IPC分类号： C07D215/14
CPC分类号： C07D215/14
摘要： A method for preparing a 7-quinolynyl-3,5-dihydroxyhept-6-enoate useful as an intermediate for pharmaceuticals, in high yield and in high purity, is presented. It is a method for preparing a 7-quinolinyl-3,5-dihydroxyhept-6-enoate represented by the formula (IV): (wherein R represents an alkyl group or an aryl group), characterized in that a compound represented by the formula (I): (wherein R is as defined above), or a compound represented by the formula (II): (wherein R is as defined above), is reduced by sodium borohydride in the presence of a boron compound represented by the formula (III): R′OBR″2 (III) (wherein R′ and R″ represent independently an alkyl group), and then the resultant reaction mixture is treated with an aqueous solution of hydrogen peroxide.
摘要翻译：提出了以高产率和高纯度制备用作药物中间体的7-喹啉基-3,5-二羟基庚-6-烯酸酯的方法。它是制备由式（Ⅳ）表示的7-喹啉基-3,5-二羟基庚-6-烯酸酯的方法：其中R表示烷基或芳基，其特征在于，由式（I）表示的硼化合物（式中，R如上定义）或式（II）表示的化合物：（式中，R如上述定义）在硼化氢的存在下，由式（III）：<？in-line-formula description =“In-line Formulas”end =“lead”？> R'OBR“2 < “直链式”末端=“尾”→（其中R'和R“独立地表示烷基），然后将所得反应混合物用过氧化氢水溶液处理。

6. 发明授权

US06476278B1 Processes for the preparation of alcohols 失效
标题翻译：制备醇的方法
公开(公告)号：US06476278B1
公开(公告)日：2002-11-05
申请号：US09868169
申请日：2001-10-25
申请人： Hideyuki Ikehira , Kunihiko Murata , Eiji Katayama , Masami Kozawa , Toru Yokozawa , Takeshi Ohkuma , Takao Ikariya , Ryoji Noyori
发明人： Hideyuki Ikehira , Kunihiko Murata , Eiji Katayama , Masami Kozawa , Toru Yokozawa , Takeshi Ohkuma , Takao Ikariya , Ryoji Noyori
IPC分类号： C07C2700
CPC分类号： C07C29/145 , C07B2200/09 , C07C45/62 , C07C2601/14 , C07C33/22 , C07C35/08 , C07C33/20
摘要： Alcohols are produced in a practical and advantageous method, by the hydrogenation of a carbonyl compound under mild conditions, by reacting the carbonyl compounds with hydrogen in the presence of a bipyridyl derivative, a group VIII transition metal complex, and a base, or by reducing a carbonyl compound in the presence of a bipyridyl derivative, a group VIII transition metal complex, a base, and an alcoholic solvent.
摘要翻译：通过在温和条件下氢化羰基化合物，通过在联吡啶衍生物，VIII族过渡金属络合物和碱的存在下使羰基化合物与氢反应，或通过还原在联吡啶衍生物，VIII族过渡金属络合物，碱和醇溶剂存在下的羰基化合物。

7. 发明授权

US08669367B2 Method for producing 2-azaadamantane 有权
标题翻译： 2-氮杂金刚烷的制备方法
公开(公告)号：US08669367B2
公开(公告)日：2014-03-11
申请号：US13585592
申请日：2012-08-14
申请人： Toshimasa Hamada , Noriaki Nagahama , Masami Kozawa , Yoshiharu Iwabuchi , Masatoshi Shibuya , Masaki Tomizawa , Yusuke Sasano
发明人： Toshimasa Hamada , Noriaki Nagahama , Masami Kozawa , Yoshiharu Iwabuchi , Masatoshi Shibuya , Masaki Tomizawa , Yusuke Sasano
IPC分类号： C07D451/14 , C07C61/29 , C07C211/41 , C07C247/00 , C07C271/24
CPC分类号： C07D451/14
摘要： To provide a method whereby a 2-azaadamantane can easily be obtained in good yield.A method for producing a 2-azaadamantane represented by the formula (1), which comprises cyclizing a compound represented by the following formula (2) in the presence of an acid.
摘要翻译：提供可以容易地以良好的产率获得2-氮杂金刚烷的方法。一种制备由式（1）表示的2-氮杂金刚烷的方法，其包括在酸存在下环化下式（2）表示的化合物。

8. 发明授权

US08329909B2 Method for producing 2-azaadamantane compound from bicyclocarbamate compound 有权
标题翻译：由双环氨基甲酸酯化合物制备2-氮杂金刚烷化合物的方法
公开(公告)号：US08329909B2
公开(公告)日：2012-12-11
申请号：US13265978
申请日：2010-04-23
申请人： Masami Kozawa , Yuki Endo
发明人： Masami Kozawa , Yuki Endo
IPC分类号： C07D215/38
CPC分类号： C07D471/08
摘要： To provide a novel method for producing a 2-azaadamantane compound from a bicyclocarbamate compound.In accordance with the following scheme: a bicyclocarbamate compound represented by the formula (1) is reacted with a halogenating agent to produce a 2-azaadamantane carbamate compound represented by the formula (2), and the 2-azaadamantane carbamate compound is subjected to hydrogenolysis to produce a 2-azaadamantane compound represented by the formula (3) (in the formulae, R1 is hydrogen or the like, each of R2 and R3 which are independent of each other, is a hydrogen atom or a C1-6 alkyl group, Ar is an aryl group which may be substituted by Ra, Ra is halogen or the like, X is a halogen atom, and Y is X or a hydrogen atom).
摘要翻译：提供从双环氨基甲酸酯化合物制备2-氮杂金刚烷化合物的新方法。按照以下方案：将由式（1）表示的双环氨基甲酸酯化合物与卤化剂反应以制备由式（2）表示的2-氮杂金刚烷氨基甲酸酯化合物，并将2-氮杂金刚烷氨基甲酸酯化合物进行氢解制备由式（3）表示的2-氮杂金刚烷化合物（式中，R 1为氢等，R 2和R 3各自独立地为氢原子或C 1-6烷基， Ar是可以被Ra取代的芳基，Ra是卤素等，X是卤素原子，Y是X或氢原子）。

9. 发明授权

US07807846B2 Method for producing succinimide compound 失效
标题翻译：琥珀酰亚胺化合物的制备方法
公开(公告)号：US07807846B2
公开(公告)日：2010-10-05
申请号：US12311284
申请日：2007-09-26
申请人： Masami Kozawa , Hideki Musashi
发明人： Masami Kozawa , Hideki Musashi
IPC分类号： C07D207/12 , C07D207/40
CPC分类号： C07D207/416
摘要： There is provided a method for producing a succinimide compound. The method for producing a succinimide compound of formula (3) comprises reacting an aminomalonic ester compound of formula (1) with a compound of formula (2) in a solvent in the presence of a base, wherein an alcohol is used as the solvent and an alkali metal alkoxide is used as the base. (where R1 and R4 independently represent an alkyl group having 1 to 12 carbon atom(s) which may be a straight chain, branched or cyclic, etc., R2 and R3 independently represent a hydrogen atom, etc., R5 represents an alkyl group having 1 to 12 carbon atom(s) which may be straight chain, branched or cyclic, etc.).
摘要翻译：提供了琥珀酰亚胺化合物的制造方法。制备式（3）的琥珀酰亚胺化合物的方法包括使式（1）的氨基马来酸酯化合物与式（2）的化合物在溶剂中在碱的存在下反应，其中使用醇作为溶剂，使用碱金属醇盐作为碱。（其中R 1和R 4独立地表示可以是直链，支链或环状等的具有1至12个碳原子的烷基，R 2和R 3独立地表示氢原子等，R 5表示烷基具有1至12个碳原子，其可以是直链，支链或环状等）。

10. 发明授权

US08273889B2 Method for producing 2-azaadamantane 有权
标题翻译： 2-氮杂金刚烷的制备方法
公开(公告)号：US08273889B2
公开(公告)日：2012-09-25
申请号：US12744015
申请日：2008-11-20
申请人： Toshimasa Hamada , Noriaki Nagahama , Masami Kozawa , Yoshiharu Iwabuchi , Masatoshi Shibuya , Masaki Tomizawa , Yusuke Sasano
发明人： Toshimasa Hamada , Noriaki Nagahama , Masami Kozawa , Yoshiharu Iwabuchi , Masatoshi Shibuya , Masaki Tomizawa , Yusuke Sasano
IPC分类号： C07D451/14 , C07C61/29 , C07C211/41 , C07C247/00 , C07C271/24
CPC分类号： C07D451/14
摘要： The invention provides a method for producing 2-azaadamantanes represented by formula (1) in good yields. The method includes cyclizing a compound represented by formula (2) in the presence of an acid.
摘要翻译：本发明提供以良好的产率制备由式（1）表示的2-氮杂金刚烷的方法。该方法包括在酸存在下环化由式（2）表示的化合物。

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