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1. 发明授权

US4936121A Condensed heterocyclic compounds, a process for preparing the same and a herbicidal composition thereof 失效
标题翻译：缩合杂环化合物，其制备方法和除草组合物
公开(公告)号：US4936121A
公开(公告)日：1990-06-26
申请号：US256487
申请日：1988-10-12
申请人： Yukihisa Goto , Hiroshi Yagihara , Kazuhisa Masamoto , Yasuo Morishima , Yukihiro Sagawa , Hirokazu Osabe
发明人： Yukihisa Goto , Hiroshi Yagihara , Kazuhisa Masamoto , Yasuo Morishima , Yukihiro Sagawa , Hirokazu Osabe
IPC分类号： A01N43/90 , C07D455/02 , C07D471/04
CPC分类号： C07D471/04 , A01N43/90 , C07D455/02
摘要： A compound of the formula (I) ##STR1## where A is an alkylene or alkenylene group, R.sub.1 is an aryl group which may be substituted, R.sub.2 is a hydrogen atom, a lower alkyl group, a lower alkenyl group, a lower alkynyl group, a halogenated lower alkyl group, a cycloalkyl group, a lower alkoxyalkyl group, a lower alkylthioalkyl group, a phenyl group which may be substituted or an aralkyl group which may be substituted, R.sub.3 is a hydrogen atom, a halogen atom, a lower alkyl group, a lower alkenyl group, a lower alkynyl group or a halogenated lower alkyl group, or R.sub.2 and R.sub.3 may be combined to form a group of --(CH.sub.2).sub.n --(n is 3 or 4), or salt thereof, which is useful as a herbicide.

2. 发明授权

US06452026B1 Process for producing optically active threo-3-amino-1,2-epoxy compounds 失效
公开(公告)号：US06452026B1
公开(公告)日：2002-09-17
申请号：US09997875
申请日：2001-11-30
申请人： Yukihiro Sagawa , Jouji Sekine , Hisao Sato
发明人： Yukihiro Sagawa , Jouji Sekine , Hisao Sato
IPC分类号： C07D30102
CPC分类号： C07C303/28 , C07D303/36 , C07C309/66
摘要： Highly pure optically active threo-3-amino-1,2-epoxy compounds appropriate for materials for manufacturing drugs and a process for producing the same on an industrial scale. An optically active threo-3-amino-1,2-diol derivative is subjected in an organic solvent in the presence of a base to alkylsufonylation or arylsulfonylation to thereby give the corresponding optically active threo-3-amino-2-hydroxy-1-sulfonyloxy compound. Next, the resultant product is subjected to epoxidation in the presence of a base to give the corresponding optically active threo-3-amino-1,2-epoxy compound. The thus obtained epoxy compound is purified by using an organic solvent and water, thus giving a highly pure epoxy compound.

3. 发明授权

US5296492A Certain chroman derivatives useful for treating symptoms caused by contraction of smooth muscles, circulatory diseases or epilepsy 失效
标题翻译：某些苯并二氢吡喃衍生物可用于治疗由平滑肌，循环系统疾病或癫痫的收缩引起的症状
公开(公告)号：US5296492A
公开(公告)日：1994-03-22
申请号：US893403
申请日：1992-06-03
申请人： Akira Shiozawa , Atsuro Inubushi , Kazuhisa Narita , Yukihiro Sagawa , Makoto Hosono , Masashi Iida
发明人： Akira Shiozawa , Atsuro Inubushi , Kazuhisa Narita , Yukihiro Sagawa , Makoto Hosono , Masashi Iida
IPC分类号： A61K31/35 , A61K31/353 , A61K31/44 , A61K31/4433 , A61P9/00 , A61P21/00 , C07D213/50 , C07D213/64 , C07D311/20 , C07D311/68 , C07D405/04 , C07F7/18 , C07D407/04 , C07F7/02 , A61K31/695
CPC分类号： C07D405/04 , C07F7/1856
摘要： A chroman derivative represented by the following general formula [1]: ##STR1## wherein R.sub.1 represents cyano group, nitro group, halogenomethyl group or --SO.sub.2 --X group (X represents lower alkyl group having 1-6 carbon atoms or aryl group); R.sub.2 represents hydrogen atom or OA group (A represents hydrogen atom, nitro group, lower acyl group having 1-6 carbon atoms, arylcarbonyl group, lower alkylsulfonyl group having 1-6 carbon atoms, arylsulfonyl group, arylalkyl group, tetrahydropyranyl group, lower alkoxycarbonyl group having 1-6 carbon atoms, arylalkoxycarbonyl group or silyl derivative group); R.sub.3 singly represents a hydrogen atom; or R.sub.3 forms a bond jointly with R.sub.2 ; and R.sub.4, R.sub.5, R.sub.6 and R.sub.7 each represent hydrogen atom, vinyl group, formyl group, --Y--(OA).sub.n group (Y represents straight or branched chain alkylene group having 1-6 carbon atoms or lower alkenyl group having 1-6 carbon atoms, A is as defined above, and n represents an integer of 1-3.The compound of this invention is expected to be effectively usable as an agent for treatment of various symptoms due to the contraction of smooth muscles, for treatment of the diseases of the circulatory system and for treatment of epilepsy.
摘要翻译：由下列通式（1）表示的苯并二氢吡喃衍生物：（*化学结构*）（1）其中R1表示氰基，硝基，卤代甲基或-SO2-X基（X表示具有1-6个碳原子的低级烷基原子或芳基）; R2表示氢原子或OA基（A表示氢原子，硝基，具有1-6个碳原子的低级酰基，芳基羰基，具有1-6个碳原子的低级烷基磺酰基，芳基磺酰基，芳基烷基，四氢吡喃基，低级烷氧基羰基具有1-6个碳原子的基团，芳基烷氧基羰基或甲硅烷基衍生物基团）; R3单独表示氢原子; 或R3与R2一起形成键; 和R 4，R 5，R 6和R 7各自表示氢原子，乙烯基，甲酰基，-Y-（OA）n基（Y表示具有1-6个碳原子的直链或支链亚烷基或具有1-6个碳原子的低级链烯基碳原子，A如上所定义，n表示1-3的整数。预期本发明化合物可有效地用作治疗由于平滑肌收缩引起的各种症状的药剂，用于治疗循环系统疾病和治疗癫痫。

4. 发明授权

US06376685B1 Process for producing optically active threo-3-amino-1,2-epoxy compounds 失效
标题翻译：光学活性苏氨酸-3-氨基-1,2-环氧化合物的制备方法
公开(公告)号：US06376685B1
公开(公告)日：2002-04-23
申请号：US09600215
申请日：2000-07-12
申请人： Yukihiro Sagawa , Jouji Sekine , Hisao Sato
发明人： Yukihiro Sagawa , Jouji Sekine , Hisao Sato
IPC分类号： C07D30102
CPC分类号： C07C303/28 , C07D303/36 , C07C309/66
摘要： Highly pure optically active threo-3-amino-1,2-epoxy compounds appropriate for materials for manufacturing drugs and a process for producing the same on an industrial scale. An optically active threo-3-amino-1,2-diol derivative is subjected in an organic solvent in the presence of a base to alkylsufonylation or arylsulfonylation to thereby give the corresponding optically active threo-3-amino-2-hydroxy-1-sulfonyloxy compound. Next, the resultant product is subjected to epoxidation in the presence of a base to give the corresponding optically active threo-3-amino-1,2-epoxy compound. The thus obtained epoxy compound is purified by using an organic solvent and water, thus giving a highly pure epoxy compound.
摘要翻译：适用于制造药物的材料的高纯度旋光活性苏氨酸-3-氨基-1,2-环氧化合物及其制备方法。光学活性的苏氨酸-3-氨基-1,2-二醇衍生物在碱的存在下在有机溶剂中进行烷基磺酰化或芳基磺酰化，得到相应的光学活性的苏氨酸-3-氨基-2-羟基-1- 磺酰氧基化合物。接着，将所得产物在碱的存在下进行环氧化，得到相应的光学活性的苏氨酸-3-氨基-1,2-环氧化合物。由此获得的环氧化合物通过使用有机溶剂和水进行纯化，从而得到高纯度的环氧化合物。

5. 发明授权

US5166397A Process for producing optically active cyclobutylamines 失效
标题翻译：光学活性环丁胺的制备方法
公开(公告)号：US5166397A
公开(公告)日：1992-11-24
申请号：US757312
申请日：1991-09-10
申请人： Kazuhisa Narita , Masashi Nagai , Hideo Sugimura , Yukihiro Sagawa , Akira Shiozawa
发明人： Kazuhisa Narita , Masashi Nagai , Hideo Sugimura , Yukihiro Sagawa , Akira Shiozawa
IPC分类号： C07C213/10 , C07C215/42 , C07D473/00
CPC分类号： C07D473/00 , C07C213/10 , C07C215/42 , C07C2101/04 , Y02P20/55
摘要： This invention relates to a process for producing an optically active cyclobutylamine which comprises reacting a racemic modification of cyclobuthylamine represented by the following general formula [I]: ##STR1## wherein R.sup.1 and R.sup.2 represent each a hydrogen atom or a protecting group; with an optically active N-acylphenylglycine to thereby give two corresponding diastereomeric salts, crystallizing the more difficultly soluble diastereomeric salt and isolating the corresponding optically active cyclobutylamine from the diastereomeric salt thus crystallized. The optically active substances of the compound of the above general formula [I] are useful as, for example, an intermediate in the synthesis of 9-[(1R, 2R, 3S)-2,3-bis(hydroxymethyl)-1-cyclobutyl]guanine which is expected as an antiviral agent.
摘要翻译：本发明涉及一种光学活性环丁胺的制备方法，其包括使由以下通式[I]表示的环丁胺的外消旋体：其中R 1和R 2各自表示氢原子或保护基; 与光学活性的N-酰基苯基甘氨酸反应，从而得到两个相应的非对映异构体盐，使难溶于水的非对映异构体盐结晶，并从如此结晶的非对映体盐中分离相应的光学活性环丁基胺。上述通式[I]的化合物的光学活性物质可用作例如合成9 - [（1R，2R，3S）-2,3-双（羟甲基）-1- 环丁基]鸟嘌呤，其被预期作为抗病毒剂。

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