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1. 发明授权

US5773626A Method for producing 1,2-benzisothiazol-3-ones 失效
标题翻译： 1,2-苯并异噻唑-3-酮的制备方法
公开(公告)号：US5773626A
公开(公告)日：1998-06-30
申请号：US718132
申请日：1996-09-18
申请人： Hirokazu Kagano , Hiroshi Goda , Katsuhiko Yoshida , Mikio Yamamoto , Shigeki Sakaue
发明人： Hirokazu Kagano , Hiroshi Goda , Katsuhiko Yoshida , Mikio Yamamoto , Shigeki Sakaue
IPC分类号： C07D275/04 , C07D275/06
CPC分类号： C07D275/04 , C07D275/06
摘要： A method for producing a 1,2-benzisothiazol-3-one, having the steps of carrying out a reaction of a 2-(alkylthio)benzaldehyde with a hydroxylamine to give a 2-(alkylthio)benzaldehyde oxime and carrying out a reaction of the 2-(alkylthio)benzaldehyde oxime with a halogenating agent; and a method for producing a 1,2-benzisothiazol-3-one, having the steps of carrying out a reaction of a 2-halobenzonitrile with an alkanethiol in a heterogeneous solvent system in the presence of a base to give a 2-(alkylthio)benzonitrile and carrying out a reaction of the 2-(alkylthio)benzonitrile with an halogenating agent in the presence of water.
摘要翻译：一种1,2-苯并异噻唑-3-酮的制备方法，其具有2-（烷硫基）苯甲醛与羟胺反应的步骤，得到2-（烷硫基）苯甲醛肟，进行 2-（烷硫基）苯甲醛肟与卤化剂; 和1,2-苯并异噻唑-3-酮的制备方法，其具有以下步骤：在非均相溶剂体系中，在碱的存在下，使2-卤代苄腈与链烷硫醇进行反应，得到2-（烷硫基）苄腈，并在水存在下进行2-（烷硫基）苄腈与卤化剂的反应。

2. 发明授权

US5508416A Method for producing alkylsulfinylbenzamides and 1,2-benzisothiazol-3-ones 失效
标题翻译：烷基亚磺酰基苯甲酰胺和1,2-苯并异噻唑-3-酮的制备方法
公开(公告)号：US5508416A
公开(公告)日：1996-04-16
申请号：US342038
申请日：1994-11-17
申请人： Hirokazu Kagano , Hiroshi Goda , Shigeki Sakaue
发明人： Hirokazu Kagano , Hiroshi Goda , Shigeki Sakaue
IPC分类号： C07C315/02 , C07C317/44 , C07C319/14 , C07C319/18 , C07C323/62 , C07D275/04
CPC分类号： C07D275/04 , C07C315/02 , C07C319/14 , C07C319/18 , C07C2101/14
摘要： A method for producing an alkylthiobenzamide by carrying out a reaction of a halobenzamide with an alkanethiol in the presence of a base in a heterogeneous solvent; a method for producing an alkylsulfinylbenzamide by carrying out a reaction of an alkylthiobenzamide with a halogen in a heterogeneous solvent; a method for producing an alkylsulfinylbenzamide by carrying out a reaction of a halobenzamide with an alkanethiol in the presence of a base in a heterogeneous solvent and a subsequent reaction with a halogen; and a method for producing a 1,2-benzisothiazol-3-one by carrying out a reaction of a 2-(alkylthio)benzamide with a halogenating agent.
摘要翻译：一种烷基硫代苯甲酰胺的制备方法，其通过在非均相溶剂中在碱存在下进行卤代苯甲酰胺与烷硫醇的反应; 通过在异质溶剂中进行烷基硫代苯甲酰胺与卤素的反应制备烷基亚磺酰基苯甲酰胺的方法; 烷基亚磺酰基苯甲酰胺的制备方法，其通过在碱存在下在非均相溶剂中进行卤代苯甲酰胺与烷硫醇的反应，随后与卤素反应; 和通过2-（烷硫基）苯甲酰胺与卤化剂的反应制备1,2-苯并异噻唑-3-酮的方法。

3. 发明授权

US5672751A Method for producing alkylsulfinylbenzamides and 1,2-benzisothiazol-3-ones 失效
标题翻译：烷基亚磺酰基苯甲酰胺和1,2-苯并异噻唑-3-酮的制备方法
公开(公告)号：US5672751A
公开(公告)日：1997-09-30
申请号：US581109
申请日：1995-12-29
申请人： Hirokazu Kagano , Hiroshi Goda , Shigeki Sakaue
发明人： Hirokazu Kagano , Hiroshi Goda , Shigeki Sakaue
IPC分类号： C07C315/02 , C07C317/44 , C07C319/14 , C07C319/18 , C07C323/62 , C07D275/04 , C07C319/12
CPC分类号： C07D275/04 , C07C315/02 , C07C319/14 , C07C319/18 , C07C2101/14
摘要： A method for producing an alkylthiobenzamide by carrying out a reaction of a halobenzamide with an alkanethiol in the presence of a base in a heterogeneous solvent; a method for producing an alkylsulfinylbenzamide by carrying out a reaction of an alkylthiobenzamide with a halogen in a heterogeneous solvent; a method for producing an alkylsulfinylbenzamide by carrying out a reaction of a halobenzamide with an alkanethiol in the presence of a base in a heterogeneous solvent and a subsequent reaction with a halogen; and a method for producing a 1,2-benzisothiazol-3-one by carrying out a reaction of a 2-(alkylthio)benzamide with a halogenating agent.
摘要翻译：一种烷基硫代苯甲酰胺的制备方法，其通过在非均相溶剂中在碱存在下进行卤代苯甲酰胺与烷硫醇的反应; 通过在异质溶剂中进行烷基硫代苯甲酰胺与卤素的反应制备烷基亚磺酰基苯甲酰胺的方法; 烷基亚磺酰基苯甲酰胺的制备方法，其通过在碱存在下在非均相溶剂中进行卤代苯甲酰胺与烷硫醇的反应，随后与卤素反应; 和通过2-（烷硫基）苯甲酰胺与卤化剂的反应制备1,2-苯并异噻唑-3-酮的方法。

4. 发明授权

US5856504A Processes for producing isothiazole derivatives 失效
标题翻译：异噻唑衍生物的制备方法
公开(公告)号：US5856504A
公开(公告)日：1999-01-05
申请号：US836697
申请日：1997-05-19
申请人： Hirokazu Kagano , Hiroshi Goda , Mikio Yamamoto , Shigeki Sakaue , Miki Toudou
发明人： Hirokazu Kagano , Hiroshi Goda , Mikio Yamamoto , Shigeki Sakaue , Miki Toudou
IPC分类号： C07D275/04
CPC分类号： C07D275/04
摘要： A method for producing a 1,2-benzisothiazole characterized by treating a 2-(alkylthio)benzaldehyde oxime with a halogen compound; a method for producing a 3-halo-1,2-benzisothiazole characterized by treating a 1,2-benzisothiazole with a halogenating agent; and a method for producing a 1-(1,2-benzisothiazol-3-yl)piperazine characterized by reacting the obtained 3-halo-1,2-benzisothiazoles with a piperazine. By the method of the present invention, 1,2-benzisothiazoles and 3-halo-1,2-benzisothiazoles, which are useful as intermediates for pharmaceutical compositions such as psychotropic agents, and 1-(1,2-benzisothiazole-3-yl)piperazines synthesized therefrom can be obtained in a high yield without using expensive starting materials by shorter and simpler process than conventional methods.
摘要翻译： PCT No.PCT / JP95 / 02484第 371日期1997年5月19日 102（e）日期1997年5月19日PCT提交1995年12月4日PCT公布。第WO96 / 17834号公报日期1996年6月13日制备1,2-苯并异噻唑的方法，其特征在于用卤素化合物处理2-（烷硫基）苯甲醛肟; 其特征在于用卤化剂处理1,2-苯并异噻唑的3-卤代-1,2-苯并异噻唑的制备方法。以及1-（1,2-苯并异噻唑-3-基）哌嗪的制造方法，其特征在于使得到的3-卤代-1,2-苯并异噻唑与哌嗪反应。通过本发明的方法，1,2-苯并异噻唑和3-卤代-1,2-苯并异噻唑可用作药物组合物如精神药物的中间体和1-（1,2-苯并异噻唑-3-基）哌嗪可以通过比常规方法更短和更简单的方法以高产率获得而不使用昂贵的起始原料。

5. 发明授权

US5744609A Method for producing alkylsulfinylbenzamides and 1-2 benzisothiazol-3-ones 失效
标题翻译：烷基亚磺酰基苯甲酰胺和1-2苯并异噻唑-3-酮的制备方法
公开(公告)号：US5744609A
公开(公告)日：1998-04-28
申请号：US831533
申请日：1997-04-07
申请人： Hirokazu Kagano , Hiroshi Goda , Shigeki Sakaue
发明人： Hirokazu Kagano , Hiroshi Goda , Shigeki Sakaue
IPC分类号： C07C315/02 , C07C317/44 , C07C319/14 , C07C319/18 , C07C323/62 , C07D275/04 , C07C323/04
CPC分类号： C07D275/04 , C07C315/02 , C07C319/14 , C07C319/18 , C07C2101/14
摘要： A method for producing an alkylthiobenzamide by carrying out a reaction of a halobenzamide with an alkanethiol in the presence of a base in a heterogeneous solvent; a method for producing an alkylsulfinylbenzamide by carrying out a reaction of an alkylthiobenzamide with a halogen in a heterogeneous solvent; a method for producing an alkylsulfinylbenzamide by carrying cut a reaction of a halobenzamide with an alkanethiol in the presence of a base in a heterogeneous solvent and a subsequent reaction with a halogen; and a method for producing a 1,2-benzisothiazol-3-one by carrying out a reaction of a 2-(alkylthio)benzamide with a halogenating agent.
摘要翻译：一种烷基硫代苯甲酰胺的制备方法，其通过在非均相溶剂中在碱存在下进行卤代苯甲酰胺与烷硫醇的反应; 通过在异质溶剂中进行烷基硫代苯甲酰胺与卤素的反应制备烷基亚磺酰基苯甲酰胺的方法; 一种烷基亚磺酰基苯甲酰胺的制备方法，其通过在碱存在下在非均相溶剂中进行卤代苯甲酰胺与烷硫醇的反应，随后与卤素反应; 和通过2-（烷硫基）苯甲酰胺与卤化剂的反应制备1,2-苯并异噻唑-3-酮的方法。

6. 发明授权

US5633384A Method for producing 1,2-benzisothiazol-3-ones 失效
标题翻译： 1,2-苯并异噻唑-3-酮的制备方法
公开(公告)号：US5633384A
公开(公告)日：1997-05-27
申请号：US467829
申请日：1995-06-06
申请人： Hirokazu Kagano , Hiroshi Goda , Katsuhiko Yoshida , Mikio Yamamoto , Shigeki Sakaue
发明人： Hirokazu Kagano , Hiroshi Goda , Katsuhiko Yoshida , Mikio Yamamoto , Shigeki Sakaue
IPC分类号： C07D275/04 , C07D275/06
CPC分类号： C07D275/04 , C07D275/06
摘要： A method for producing a 1,2-benzisothiazol-3-one, having the steps of carrying out a reaction of a 2-(alkylthio)benzaldehyde with a hydroxylamine to give a 2-(alkylthio)benzaldehyde oxime and carrying out a reaction of the 2-(alkylthio)benzaldehyde oxime with a halogenating agent; and a method for producing a 1,2-benzisothiazol-3-one, having the steps of carrying out a reaction of a 2-halobenzonitrile with an alkanethiol in a heterogeneous solvent system in the presence of a base to give a 2-(alkylthio)benzonitrile and carrying out a reaction of the 2-(alkylthio)benzonitrile with an halogenating agent in the presence of water.
摘要翻译：一种1,2-苯并异噻唑-3-酮的制备方法，其具有2-（烷硫基）苯甲醛与羟胺反应的步骤，得到2-（烷硫基）苯甲醛肟，进行 2-（烷硫基）苯甲醛肟与卤化剂; 和1,2-苯并异噻唑-3-酮的制备方法，其具有以下步骤：在非均相溶剂体系中，在碱的存在下，使2-卤代苄腈与链烷硫醇进行反应，得到2-（烷硫基）苄腈，并在水存在下进行2-（烷硫基）苄腈与卤化剂的反应。

7. 发明授权

US5298630A Processes for producing 2-substituted benzo[B]thiophene 失效
标题翻译：制备2-取代苯并[b]噻吩的方法
公开(公告)号：US5298630A
公开(公告)日：1994-03-29
申请号：US945084
申请日：1992-09-15
申请人： Hirokazu Kagano , Hiroshi Goda , Katsuhiko Yoshida , Masahito Nakano
发明人： Hirokazu Kagano , Hiroshi Goda , Katsuhiko Yoshida , Masahito Nakano
IPC分类号： C07C319/14 , C07C323/22 , C07D333/56 , C07D333/70
CPC分类号： C07D333/70 , C07C319/14 , C07D333/56
摘要： A 2-alkylthiobenzaldehyde of general formula (I) is reacted with a halo compound of general formula (II) to produce a 2-substituted benzo[b]thiophene of general formula (III): ##STR1## wherein R.sup.1 means an alkyl group of 1 to 4 carbon atoms,X.sup.1 CH.sub.2 Y (II)wherein X.sup.1 means Cl or Br; Y means --CO.sub.2 H, --CO.sub.2 R.sup.2, --COR.sup.2, --CONH.sub.2 or --CN; R.sup.2 means an alkyl group of 1 to 4 carbon atoms, ##STR2## wherein Y is as defined above. The process of this invention is of great economic and industrial value, for 2-acetylbenzo[b]thiophene and 2-benzo[b]thiophenecarboxylic acid, which are important intermediates for drugs and agricultural chemicals among others, can be obtained in a simple manner, easily and in high yield.
摘要翻译：将通式（I）的2-烷硫基苯甲醛与通式（II）的卤代化合物反应，生成通式（III）的2-取代苯并（b）噻吩：（*化学结构*）（I）其中 R1表示1〜4个碳原子的烷基，X1CH2Y（Ⅱ）其中X1表示Cl或Br; Y表示-CO 2 H，-CO 2 R 2，-COR 2，-CONH 2或-CN; R2表示1〜4个碳原子的烷基，（*化学结构*）（III）其中Y如上定义。本发明的方法具有很大的经济和工业价值，可以以简单的方式获得作为药物和农药等重要中间体的2-乙酰基苯并（b）噻吩和2-苯并（b）噻吩羧酸，容易和高产量。

8. 发明授权

US5210291A Method for producing dichlorophenylthioglycolic acid 失效
标题翻译：生产二氯乙酰胆酸的方法
公开(公告)号：US5210291A
公开(公告)日：1993-05-11
申请号：US794906
申请日：1991-11-20
申请人： Michio Suzuki , Hiroyuki Hata , Masato Yoshikawa , Toshiyuki Ohe , Hirokazu Kagano , Hiroshi Goda , Masahito Nakano , Masaki Teramoto
发明人： Michio Suzuki , Hiroyuki Hata , Masato Yoshikawa , Toshiyuki Ohe , Hirokazu Kagano , Hiroshi Goda , Masahito Nakano , Masaki Teramoto
IPC分类号： C07C319/14 , C07C323/52
CPC分类号： C07C319/14 , C07C323/52
摘要： The present invention is directed to a method for producing dichlorophenylthioglycolic acid which comprises reacting monobromodichlorobenzene or trichlorobenzene with a thioglycolate in a ratio of 0.5 to 2.5 mols of the latter to 1 mol of the former in a polar solvent, and to a method for producing dichlorophenylthioglycolic acid comprising further reacting the reaction mixture obtained as above with a monohalogenoacetate.The method of the present invention is very useful industrially, advantageously producing dichlorophenylthioglycolic acid in high yield.

9. 发明授权

US5939548A Process for preparation of 3-piperazinylbenzisothiazoles 有权
标题翻译： 3-哌嗪基苯并异噻唑的制备方法
公开(公告)号：US5939548A
公开(公告)日：1999-08-17
申请号：US128540
申请日：1998-08-04
申请人： Hiroshi Goda , Junichi Sakamoto , Shigeki Sakaue , Sakae Kajihara , Miki Todo
发明人： Hiroshi Goda , Junichi Sakamoto , Shigeki Sakaue , Sakae Kajihara , Miki Todo
IPC分类号： C07D275/04 , C07D275/06 , C07D417/04
CPC分类号： C07D275/06
摘要： There is disclosed a process for preparing 3-piperazinylbenzisothiazoles comprising reacting the specified 3-halo-1,2-benzisothiazole or 2-cyanobenzenesulfenyl halide in the presence of an alkylene glycol derivative. The process is industrially effective, easy and economical and can provide useful intermediates for production of pharmaceutical preparations.
摘要翻译：公开了一种制备3-哌嗪基苯并异噻唑的方法，包括在亚烷基二醇衍生物存在下使指定的3-卤代-1,2-苯并异噻唑或2-氰基苯硫基卤化物反应。该方法在工业上有效，容易和经济，并且可以提供制备药物制剂的有用中间体。

10. 发明授权

US5861511A Process for preparation of 3 piperazinylbenzisothiazoles 失效
标题翻译：制备3哌嗪基苯并异噻唑的方法
公开(公告)号：US5861511A
公开(公告)日：1999-01-19
申请号：US938845
申请日：1997-09-26
申请人： Hiroshi Goda , Junichi Sakamoto , Shigeki Sakaue , Sakae Kajihara , Miki Todo
发明人： Hiroshi Goda , Junichi Sakamoto , Shigeki Sakaue , Sakae Kajihara , Miki Todo
IPC分类号： C07D275/04 , C07D275/06 , C07D417/04
CPC分类号： C07D275/06
摘要： There is disclosed a process for preparing 3-piperazinylbenzisothiazoles comprising reacting the specified 3-halo-1,2-benzisothiazole or 2-cyanobenzenesulfenyl halide in the presence of an alkylene glycol derivative. The process is industrially effective, easy and economical and can provide useful intermediates for production of pharmaceutical preparations.
摘要翻译：公开了一种制备3-哌嗪基苯并异噻唑的方法，包括在亚烷基二醇衍生物存在下使指定的3-卤代-1,2-苯并异噻唑或2-氰基苯硫基卤化物反应。该方法在工业上有效，容易和经济，并且可以提供制备药物制剂的有用中间体。

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