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1. 发明公开

EP0867431A1 Process for the preparation of azide derivatives 失效
标题翻译： Verfahren zur Herstellung von Azid-Derivaten
公开(公告)号：EP0867431A1
公开(公告)日：1998-09-30
申请号：EP98104327.6
申请日：1998-03-11
申请人： Eisai Chemical Co., Ltd.
发明人： Mizuno, Masanori , Shioiri, Takayuki
IPC分类号： C07C247/04 , C07C247/12 , C07C247/08 , C07C247/14 , C07C247/10 , C07D277/28 , C07H5/04
CPC分类号： C07C247/10 , C07C247/04 , C07C247/08 , C07C247/12 , C07C247/14 , C07D277/28 , C07H5/04
摘要： To provide a novel and industrially advantageous process for the preparation of azide derivatives useful as drugs, perfumes or intermediates of dyes.
A process for the preparation of aside derivatives by reacting an alcohol derivative with di-p-nitrophenyl phosphorazidate in the presence of 1,8-diazabicyclo[5.4.0]-7-undecene.
摘要翻译：提供用于制备用作染料的药物，香料或中间体的叠氮衍生物的新颖和工业上有利的方法。一种通过醇衍生物与二对硝基苯基氨基磷酸酯在1,8-二氮杂双环[5.4.0-7-十一碳烯]存在下反应制备衍生物的方法。

2. 发明授权

EP0590681B1 A process for the preparation of aminothiadiazolylacetyl halide derivatives 失效
标题翻译：一种用于氨基Thiadiazolylacetylhaliden的制备方法
公开(公告)号：EP0590681B1
公开(公告)日：1997-07-09
申请号：EP93115891.9
申请日：1993-10-01
申请人： EISAI CHEMICAL CO., LTD.
发明人： Kanai, Takeo , Imai, Akio , Sato, Katsuhiko , Shinohara, Homare , Oishi, Kazumi
IPC分类号： C07D285/08
CPC分类号： C07D285/08 , Y02P20/55

3. 发明授权

EP0488209B1 Process for producing benzylphthalazinone derivatives and salts thereof 失效
标题翻译：一种用于生产benzylphthalazinone衍生物及其盐处理
公开(公告)号：EP0488209B1
公开(公告)日：1996-05-22
申请号：EP91120268.7
申请日：1991-11-27
申请人： EISAI CHEMICAL CO., LTD.
发明人： Murakami, Kazukata
IPC分类号： C07D403/04 , A61K31/50
CPC分类号： C07D403/04

4. 发明授权

EP0592962B1 Purification method of crude product 失效
标题翻译：粗的纯化方法
公开(公告)号：EP0592962B1
公开(公告)日：1997-07-16
申请号：EP93116354.7
申请日：1993-10-08
申请人： EISAI CHEMICAL CO., LTD.
发明人： Tsujii, Masahiko , Kuroda, Hirofumi , Furusawa, Yoshikazu , Hirota, Katsuhiko
IPC分类号： B01D15/08
CPC分类号： B01D15/426

5. 发明公开

EP0675116A1 Protected aminothiazolylacetic acid derivatives 失效
标题翻译： GeschützteAminothiazolylessigsäurederivate。
公开(公告)号：EP0675116A1
公开(公告)日：1995-10-04
申请号：EP95104642.4
申请日：1995-03-29
申请人： EISAI CHEMICAL CO., LTD.
发明人： Urawa, Yoshio , Shimotani, Ahihiko , Kanai, Takeo , Tsujii, Masahiko
IPC分类号： C07D277/20
CPC分类号： C07D277/587 , C07D277/20 , C07D277/42 , C07D501/00 , Y02P20/55
摘要： Described is a protected aminothiazolylacetic acid derivative represented by the following formula (I):

wherein A represents a nitrogen atom or a methine group, R¹ and R² may be the same or different and individually represent a hydrogen atom, a lower alkyl group or a substituted or unsubstituted aryl group, R³ represents a lower alkoxy group, a halogenated lower alkoxy group, a triphenylmethoxy group, a lower alkyl group or an acyloxy group, and R⁴ represents a halogen atom, a hydroxy group, a lower alkoxy group or a substituted or unsubstituted amino group; and salts thereof; as well as processes for the preparation thereof. The protected aminothaizolylacetic acid derivative according to the present invention is an useful intermediate for introducing a 2-(2-aminothiazol-4-yl)-2-alkoxyiminoacetyl group or a 2-(2-aminotiazol-4-yl)-2-alkenoyl group into a cephem skeleton.
摘要翻译：描述了由下式（I）表示的受保护的氨基噻唑乙酸衍生物：其中A表示氮原子或次甲基，R 1和R 2可以相同或不同，并且各自表示氢原子，低级烷基或取代或未取代的芳基，R 3表示低级烷氧基，卤代低级烷氧基，三苯甲氧基，低级烷基或酰氧基，R 4表示卤素原子，羟基，低级烷氧基或取代或未取代的氨基; 及其盐; 以及其制备方法。根据本发明的受保护的氨基噻唑乙酸衍生物是用于引入2-（2-氨基噻唑-4-基）-2-烷氧基亚氨基乙酰基或2-（2-氨基噻唑-4-基）-2-烯酰基组成一个头脑骨架。

6. 发明公开

EP0627433A1 PROCESS FOR PRODUCING IMIDAZOPYRIDINE DERIVATIVE AND INTERMEDIATE 失效
标题翻译： VERFAHREN ZUR HERSTELLUNG VON IMIDAZOPYRIDINDERIVATEN UND ZWISCHENPRODUKTE。
公开(公告)号：EP0627433A1
公开(公告)日：1994-12-07
申请号：EP94901045.8
申请日：1993-12-07
申请人： Eisai Co., Ltd. , EISAI CHEMICAL CO., LTD.
发明人： URAWA, Yoshio 16-27, Konoike Ohkaryo , FURUKAWA, Ken Residence Hiro 202 , SHIMIZU, Toshikazu Konoike Ohkaryo , YAMAGISHI, Yoji , TSURUGI, Tomio 1-1044-130, Toyosatodai , ICHINO, Tomio 2333-197, Kyuchu
IPC分类号： C07D471/04 , C07D213/75 , C07D263/10 , C07D263/14 , C07D413/12 , C07F7/18 , C07C63/06 , C07C309/65 , C07C309/73 , C07C65/105 , C07C69/76
CPC分类号： C07D213/73 , C07C63/72 , C07C65/105 , C07C69/732 , C07C69/76 , C07D213/75 , C07D263/10 , C07D263/12 , C07D263/14 , C07D309/12 , C07D413/12 , C07D471/04 , Y02P20/55
摘要： The invention provides an industrially excellent process for producing a 2-alkyl-3-(biphenyl-4-yl)-methyl-3H-imidazo[4,5-b]pyridine derivative represented by general formula (II), serving as a precursor of the angiotensin II receptor antagonist useful as an antihypertensive, a biphenyl derivative serving as a precursor of the substituent of the imidazopyridine derivative, a process for producing the biphenyl derivative, and an intermediate useful for producing the biphenyl derivative. The imidazopyridine derivative (II) can be produced in a high yield according to the process of the invention by subjecting a 2-amino-5-halogeno-3-nitropyridine derivative to amidation, N-alkylation and reductive cyclization. This process is industrially excellent, because the halogen atom introduced into the 5-position as a protective group in the nitration step can be eliminated simultaneously in the subsequent step. The above biphenyl derivative is excellent in reactivity and product purity, thus being an intermediate suitable for industrial production.
摘要翻译：本发明提供了制备用作前体的通式（II）表示的2-烷基-3-（联苯-4-基） - 甲基-3H-咪唑并[4,5-b]吡啶衍生物的工业上优异的方法可用作抗高血压药的血管紧张素II受体拮抗剂，作为咪唑并吡啶衍生物的取代基的前体的联苯衍生物，联苯衍生物的制备方法和可用于制备联苯衍生物的中间体。根据本发明的方法，可以通过使2-氨基-5-卤代-3-硝基吡啶衍生物进行酰胺化，N-烷基化和还原环化，以高产率制备咪唑并吡啶衍生物（II）。该工艺在工业上是优异的，因为在后续步骤中可以同时消除在硝化步骤中作为保护基引入5位的卤素原子。上述联苯衍生物的反应性和产物纯度优异，因此是适于工业生产的中间体。

7. 发明公开

EP0590681A3 A process for the preparation of aminothiadiazolylacetyl halide derivatives 失效
标题翻译：一种制备氨基苯甲酰基乙酰卤衍生物的方法
公开(公告)号：EP0590681A3
公开(公告)日：1994-08-17
申请号：EP93115891.9
申请日：1993-10-01
申请人： EISAI CHEMICAL CO., LTD.
发明人： Kanai, Takeo , Imai, Akio , Sato, Katsuhiko , Shinohara, Homare , Oishi, Kazumi
IPC分类号： C07D285/08
CPC分类号： C07D285/08 , Y02P20/55
摘要： 57 A process is provided for the preparation of an aminothiadiazolylacetyl halide derivative represented by the following formula (II):

wherein R 1 represents a lower alkyl, cycloalkyl or halogenated lower alkyl group; and R 2 represents an amino-protecting group or a hydrogen atom, or a salt thereof, which process uses as the starting material a compound represented by the following formula (I):
wherein R 1 and R 2 have the same meanings as defined above, or a salt thereof.

8. 发明公开

EP0247513A1 Process for producing 2-methyl-1,4-naphthoquinone 失效
标题翻译： Verfahren zur Herstellung von 2-甲基-1,4-萘醌。
公开(公告)号：EP0247513A1
公开(公告)日：1987-12-02
申请号：EP87107349.0
申请日：1987-05-20
申请人： Eisai Chemical Co., Ltd.
发明人： Shinnaka, Atsushi , Narabu, Yukio
IPC分类号： C07C50/12 , C07C46/02 , B01J27/26
CPC分类号： C07C46/02 , C07C50/10
摘要： An improved process for producing 2-methyl-1,4-naphthoquinone with a high yield comprising reaction of a 1-lower-alkoxy-2-methyl naphthalene with hydrogen peroxide in the presence of a hexacyanoferric acid or a salt thereof as catalyst. This process does not employ hazardous chromium compounds unlike conventional methods.
摘要翻译：一种生产高产率2-甲基-1,4-萘醌的改进方法，包括在六氰基铁酸或其盐作催化剂存在下1-低级烷氧基-2-甲基萘与过氧化氢的反应。该方法不像常规方法那样使用危险的铬化合物。

9. 发明授权

EP0627433B1 PROCESS FOR PRODUCING IMIDAZOPYRIDINE DERIVATIVE AND INTERMEDIATE 失效
标题翻译：用于生产咪唑衍生物和中间产品
公开(公告)号：EP0627433B1
公开(公告)日：2003-03-05
申请号：EP94901045.8
申请日：1993-12-07
申请人： Eisai Co., Ltd. , EISAI CHEMICAL CO., LTD.
发明人： URAWA, Yoshio 16-27, Konoike Ohkaryo , FURUKAWA, Ken Residence Hiro 202 , SHIMIZU, Toshikazu Konoike Ohkaryo , YAMAGISHI, Yoji , TSURUGI, Tomio 1-1044-130, Toyosatodai , ICHINO, Tomio 2333-197, Kyuchu
IPC分类号： C07D471/04 , C07D213/75 , C07D263/10 , C07D263/14 , C07D413/12 , C07F7/18 , C07C63/06 , C07C309/65 , C07C309/73 , C07C65/105 , C07C69/76
CPC分类号： C07D213/73 , C07C63/72 , C07C65/105 , C07C69/732 , C07C69/76 , C07D213/75 , C07D263/10 , C07D263/12 , C07D263/14 , C07D309/12 , C07D413/12 , C07D471/04 , Y02P20/55
摘要： The invention provides an industrially excellent process for producing a 2-alkyl-3-(biphenyl-4-yl)-methyl-3H-imidazo[4.5-b]pyridine derivative represented by general formula (II), serving as a precursor of the angiotensin II receptor antagonist useful as an antihypertensive, a biphenyl derivative serving as a precursor of the substituent of the imidazopyridine derivative, a process for producing the biphenyl derivative, and an intermediate useful for producing the biphenyl derivative. The imidazopyridine derivative (II) can be produced in a high yield according to the process of the invention by subjecting a 2-amino-5-halogeno-3-nitropyridine derivative to amidation, N-alkylation and reductive cyclization. This process is industrially excellent, because the halogen atom introduced into the 5-position as a protective group in the nitration step can be eliminated simultaneously in the subsequent step. The above biphenyl derivative is excellent in reactivity and product purity, thus being an intermediate suitable for industrial production.

10. 发明授权

EP0704435B1 PROCESS FOR PRODUCING HYDROQUINONE AND BENZOQUINONE DERIVATIVE 失效
标题翻译：于制备氢醌和苯醌衍生物
公开(公告)号：EP0704435B1
公开(公告)日：1998-06-24
申请号：EP94921818.4
申请日：1994-07-26
申请人： Eisai Co., Ltd. , EISAI CHEMICAL CO., LTD.
发明人： KOMATSU, Yuuki , MINAMI, Norio , FURUKAWA, Ken , NISHIMURA, Hiroshi , YAMAGISHI, Yoji
IPC分类号： C07D213/30 , C07D213/61 , C07D417/06 , A61K31/44
CPC分类号： C07D213/30 , C07D417/06
摘要： Intermediates used in producing benzothiazole derivatives useful for preventing and treating diseases against which the activity of inhibiting leucotriene and thromboxane production is efficacious; and a process for producing the same. The process comprises condensing a hydroquinone derivative with a pyridylcarboxaldehyde derivative without protecting the hydroxyl groups of the hydroquinone and oxidizing the formed pyridylmethylhydroquinone derivative into a pyridylmethyl-1,4-benzoquinone derivative.

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