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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

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.

5. 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.

6. 发明授权

EP0675116B1 Preparation of protected aminothiazolylacetic acid derivatives 失效
标题翻译：保护的氨基噻唑乙酸衍生物的制备
公开(公告)号：EP0675116B1
公开(公告)日：1998-06-17
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

7. 发明公开

EP0832893A1 Process for the production of cephem compounds 失效
标题翻译： Verfahren zur Herstellung von Cephem-Verbindungen
公开(公告)号：EP0832893A1
公开(公告)日：1998-04-01
申请号：EP97116634.3
申请日：1997-09-24
申请人： EISAI CHEMICAL CO., LTD.
发明人： Shinohara, Homare , Kodama, Masato , Hamamura, Kimio , Kuroda, Hirofumi
IPC分类号： C07D501/06
CPC分类号： C07D501/00
摘要： An industrially excellent, novel process for producing cephem compounds which are useful as medicines, particularly, antibiotics and represented by the following general formula (III):
which comprises reacting in water a 3-cephem-4-carboxylate represented by the following general formula (I):
or a salt thereof with an acid chloride represented by the general formula (II), R 1 COCl.
摘要翻译：一种工业上优异的新颖的制备头孢烯化合物的方法，其可用作药物，特别是抗生素，由以下通式（III）表示：，其包括在水中反应由以下化合物代表的3-头孢烯-4-羧酸通式（I）：或其与通式（II）表示的酰氯的盐，R 1 COCl。

8. 发明公开

EP0714885A2 Preparation process of aminoacetamide derivative 失效
标题翻译： Verfahren zur Herstellung von Aminoacetamid Derivaten
公开(公告)号：EP0714885A2
公开(公告)日：1996-06-05
申请号：EP95118060.3
申请日：1995-11-16
申请人： EISAI CHEMICAL CO., LTD. , ANAN CORPORATION
发明人： Seki, Chiaki , Ishizawa, Shozo , Koiwa, Atsushi , Ogura, Toshimasa , Takaha, Motoshige , Uchiyama, Manabu
IPC分类号： C07C231/14 , C07C237/04
CPC分类号： C07C231/12
摘要： Disclosed herein are novel processes for preparing aminoacetamide derivatives, wherein:

(1) a secondary amine is reacted with a 2-haloacetamide in the presence or absence of at least one solvent selected from water, lower alcohols, aromatic solvents and acetic acid esters;
(2) an N-benzylideneamine derivative is reacted with dimethyl sulfate or diethyl sulfate to form a secondary amine, and this secondary amine is then reacted with a 2-haloacetamide; and
(3) a primary amine is reacted with benzaldehyde to form an N-benzylideneamine derivative, this product is then reacted with dimethyl sulfate or diethyl sulfate to form a secondary amine, and this secondary amine is further reacted with a 2-haloacetamide.

The 2-aminoacetamide derivatives are useful as intermediates for the preparation of novel antibiotics.
摘要翻译：本文公开了制备氨基乙酰胺衍生物的新方法，其中：（1）在存在或不存在选自水，低级醇，芳族溶剂和乙酸酯的至少一种溶剂的情况下，使仲胺与2-卤代乙酰胺反应; （2）将N-亚苄基胺衍生物与硫酸二甲酯或硫酸二乙酯反应形成仲胺，然后使该仲胺与2-卤代乙酰胺反应; 和（3）将伯胺与苯甲醛反应以形成N-亚苄基胺衍生物，然后将该产物与硫酸二甲酯或硫酸二乙酯反应形成仲胺，并将该仲胺进一步与2-卤代乙酰胺反应。 2-氨基乙酰胺衍生物可用作制备新型抗生素的中间体。

9. 发明公开

EP0590681A2 A process for the preparation of aminothiadiazolylacetyl halide derivatives 失效
标题翻译： Verfahren zur Herstellung von Amino-Thiadiazolylacetylhaliden。
公开(公告)号：EP0590681A2
公开(公告)日：1994-04-06
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.
摘要翻译：提供了制备由下式（II）表示的氨基噻二唑基乙酰卤衍生物的方法：其中R 1表示低级烷基，环烷基或卤代低级烷基; R 2表示下述式（I）表示的化合物作为起始原料的氨基保护基或氢原子或其盐，其中R 1和R 2， 2>具有与上述相同的含义或其盐。

10. 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

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