公开(公告)号：EP0507124A3

公开(公告)日：1992-12-09

申请号：EP92104202.4

申请日：1992-03-11

申请人： OTSUKA KAGAKU KABUSHIKI KAISHA

发明人： Torii, Sigeru ,  Tanaka, Hideo ,  Taniguchi, Masatoshi, c/o Otsuka Kagaku K.K. ,  Sasaoka, Michio, c/o Otsuka Kagaku K.K. ,  Shiroi, Takashi, c/o Otsuka Kagaku K.K. ,  Kameyama, Yutaka, c/o Otsuka Kagaku K.K.

IPC分类号： C07D501/02 ,  C07D501/59 ,  C07D205/095

CPC分类号： C07D501/00 ,  Y02P20/55

摘要： The present invention provides a process for preparing a cephem derivative characterized in that an allenyl β -lactam compound represented by the formula (1)

wherein R 1 is amino or protected amino, R 2 is a hydrogen atom or lower alkoxyl, R 3 is a hydrogen atom or carboxylic acid protecting group and X is the group -S0 2 R 4 or -SR 4 , R 4 being substituted or unsubstituted aryl or substituted or unsubstituted nitrogen-containing aromatic heterocyclic group is reacted with a nucleophilic agent to obtain the derivative, the cephem derivative being represented by the formula (2)
wherein R 1 , R 2 and R 3 are as defined above, and Y is the residue of the nucleophilic agent.

公开(公告)号：EP0503604A3

公开(公告)日：1992-12-02

申请号：EP92104201.6

申请日：1992-03-11

申请人： OTSUKA KAGAKU KABUSHIKI KAISHA

发明人： Torii, Sigeru ,  Tanaka, Hideo ,  Taniguchi, Masatoshi, c/o Otsuka Kagaku K.K. ,  Sasaoka, Michio, c/o Otsuka Kagaku K.K. ,  Shiroi, Takashi, c/o Otsuka Kagaku K.K. ,  Kameyama, Yutaka, c/o Otsuka Kagaku K.K.

IPC分类号： C07D205/095 ,  C07D205/09

CPC分类号： C07D205/095 ,  C07D205/09 ,  Y02P20/55

摘要： The present invention provides an allenyl β -lactam compound represented by the formula (1)

wherein R¹ is a hydrogen atom, halogen atom, amino or protected amino, R² is a hydrogen atom, halogen atom, lower alkoxyl, lower acyl, lower alkyl, lower alkyl substituted with hydroxyl or protected hydroxyl, hydroxyl or protected hydroxyl, R¹ and R² representing =O when taken together, R³ is a hydrogen atom or carboxylic acid protecting group, and X is the group -SO₂R⁴ or the group -SR⁴, R⁴ being substituted or unsubstituted aryl or substituted or unsubstituted nitrogen-containing aromatic heterocyclic group.

公开(公告)号：EP0503604B1

公开(公告)日：1996-12-27

申请号：EP92104201.6

申请日：1992-03-11

申请人： OTSUKA KAGAKU KABUSHIKI KAISHA

发明人： Torii, Sigeru ,  Tanaka, Hideo ,  Taniguchi, Masatoshi, c/o Otsuka Kagaku K.K. ,  Sasaoka, Michio, c/o Otsuka Kagaku K.K. ,  Shiroi, Takashi, c/o Otsuka Kagaku K.K. ,  Kameyama, Yutaka, c/o Otsuka Kagaku K.K.

IPC分类号： C07D205/095 ,  C07D205/09

CPC分类号： C07D205/095 ,  C07D205/09 ,  Y02P20/55

公开(公告)号：EP0503604A2

公开(公告)日：1992-09-16

申请号：EP92104201.6

申请日：1992-03-11

申请人： OTSUKA KAGAKU KABUSHIKI KAISHA

发明人： Torii, Sigeru ,  Tanaka, Hideo ,  Taniguchi, Masatoshi, c/o Otsuka Kagaku K.K. ,  Sasaoka, Michio, c/o Otsuka Kagaku K.K. ,  Shiroi, Takashi, c/o Otsuka Kagaku K.K. ,  Kameyama, Yutaka, c/o Otsuka Kagaku K.K.

IPC分类号： C07D205/095 ,  C07D205/09

CPC分类号： C07D205/095 ,  C07D205/09 ,  Y02P20/55

摘要： The present invention provides an allenyl β -lactam compound represented by the formula (1)

wherein R¹ is a hydrogen atom, halogen atom, amino or protected amino, R² is a hydrogen atom, halogen atom, lower alkoxyl, lower acyl, lower alkyl, lower alkyl substituted with hydroxyl or protected hydroxyl, hydroxyl or protected hydroxyl, R¹ and R² representing =O when taken together, R³ is a hydrogen atom or carboxylic acid protecting group, and X is the group -SO₂R⁴ or the group -SR⁴, R⁴ being substituted or unsubstituted aryl or substituted or unsubstituted nitrogen-containing aromatic heterocyclic group.

摘要翻译： 本发明提供由式（1）表示的丙烯基β-内酰胺化合物其中R 1是氢原子，卤素原子，氨基或保护的氨基，R 2是氢原子，卤素原子， 低级烷氧基，低级酰基，低级烷基，被羟基或被保护的羟基取代的低级烷基，羟基或被保护的羟基，R 1和R 2一起代表= O，R 3是氢原子或羧酸 X为-SO 2 R 4基或-SR 4基，R 4为取代或未取代的芳基或取代或未取代的含氮芳香族杂环基。

公开(公告)号：EP0507124B1

公开(公告)日：1996-12-27

申请号：EP92104202.4

申请日：1992-03-11

申请人： OTSUKA KAGAKU KABUSHIKI KAISHA

发明人： Torii, Sigeru ,  Tanaka, Hideo ,  Taniguchi, Masatoshi, c/o Otsuka Kagaku K.K. ,  Sasaoka, Michio, c/o Otsuka Kagaku K.K. ,  Shiroi, Takashi, c/o Otsuka Kagaku K.K. ,  Kameyama, Yutaka, c/o Otsuka Kagaku K.K.

IPC分类号： C07D501/02 ,  C07D501/59 ,  C07D205/095

CPC分类号： C07D501/00 ,  Y02P20/55

公开(公告)号：EP0507124A2

公开(公告)日：1992-10-07

申请号：EP92104202.4

申请日：1992-03-11

申请人： OTSUKA KAGAKU KABUSHIKI KAISHA

发明人： Torii, Sigeru ,  Tanaka, Hideo ,  Taniguchi, Masatoshi, c/o Otsuka Kagaku K.K. ,  Sasaoka, Michio, c/o Otsuka Kagaku K.K. ,  Shiroi, Takashi, c/o Otsuka Kagaku K.K. ,  Kameyama, Yutaka, c/o Otsuka Kagaku K.K.

IPC分类号： C07D501/02 ,  C07D501/59 ,  C07D205/095

CPC分类号： C07D501/00 ,  Y02P20/55

摘要： The present invention provides a process for preparing a cephem derivative characterized in that an allenyl β -lactam compound represented by the formula (1)

wherein R 1 is amino or protected amino, R 2 is a hydrogen atom or lower alkoxyl, R 3 is a hydrogen atom or carboxylic acid protecting group and X is the group -S0 2 R 4 or -SR 4 , R 4 being substituted or unsubstituted aryl or substituted or unsubstituted nitrogen-containing aromatic heterocyclic group is reacted with a nucleophilic agent to obtain the derivative, the cephem derivative being represented by the formula (2)

wherein R 1 , R 2 and R 3 are as defined above, and Y is the residue of the nucleophilic agent.

摘要翻译： 本发明提供了一种头孢衍生物的制备方法，其特征在于由式（1）表示的丙烯酰基β-内酰胺化合物其中R 1为氨基或被保护的氨基，R 2为氢原子或 低级烷氧基，R 3是氢原子或羧酸保护基，X是基团-SO 2 R 4或-SR 4，R 4是取代或未取代的芳基或取代或未取代的含氮芳族 杂环基与亲核剂反应得到衍生物，头孢烯衍生物由式（2）表示，其中R 1，R 2和R 3定义如上，Y为 亲核剂的残留物。