公开(公告)号：US5288860A

公开(公告)日：1994-02-22

申请号：US3024

申请日：1993-01-11

申请人： Sigeru Torii ,  Hideo Tanaka ,  Masatoshi Taniguchi ,  Michio Sasaoka ,  Takashi Shiroi ,  Yutaka Kameyama

发明人： Sigeru Torii ,  Hideo Tanaka ,  Masatoshi Taniguchi ,  Michio Sasaoka ,  Takashi Shiroi ,  Yutaka Kameyama

IPC分类号： C07D499/00 ,  C07D499/04 ,  C07D499/12 ,  C07D499/87 ,  C07D513/04

CPC分类号： C07D513/04 ,  C07D499/00 ,  Y02P20/55

摘要： The present invention provides a thiazolinoazetidinone derivative represented by the formula ##STR1## wherein R.sup.1 is phenyl having or not having substituent(s), methyl having or not having substituent(s) or ##STR2## group, R.sup.3 being phenyl having or not having substituent(s), and R.sup.2 is a hydrogen atom or carboxylic acid protective group, and a process for preparing the same.The present invention further provides a process for preparing a 2-exo-methylenepenam derivative characterized by hydrolyzing the thiazoline ring of a thiazolinoazetidinone derivative of the above formula (1) to effect recyclization and obtain a 2-exo-methylenepenam derivative represented by the formula ##STR3## wherein R.sup.1 and R.sup.2 are as defined above.

摘要翻译： 本发明提供由式（1）表示的噻唑并氮杂环丁酮衍生物，其中R 1是具有或不具有取代基的苯基，具有或不具有取代基的甲基或基团，R3是具有或不具有取代基的苯基， 不具有取代基，R2为氢原子或羧酸保护基，及其制备方法。 本发明进一步提供了制备2-异亚甲基台内叶酸衍生物的方法，其特征在于水解上述式（1）的噻唑并氮杂环丁酮衍生物的噻唑啉环以进行再循环，得到式（1）所示的2-外 - 亚甲基山梨醇衍生物， 图像（3）其中R1和R2如上所定义。

公开(公告)号：US4958018A

公开(公告)日：1990-09-18

申请号：US347319

申请日：1989-05-04

申请人： Sigeru Torii ,  Hideo Tanaka ,  Masatoshi Taniguchi ,  Michio Sasaoka ,  Norio Saito ,  Takashi Shiroi ,  Shigemitsu Nagao ,  Ryo Kikuchi ,  Yutaka Kameyama

发明人： Sigeru Torii ,  Hideo Tanaka ,  Masatoshi Taniguchi ,  Michio Sasaoka ,  Norio Saito ,  Takashi Shiroi ,  Shigemitsu Nagao ,  Ryo Kikuchi ,  Yutaka Kameyama

IPC分类号： B01J23/14 ,  C07B61/00 ,  C07D501/04 ,  C07D501/22

CPC分类号： C07D501/04 ,  Y02P20/55

摘要： Disclosed is a method of producing a 3-exomethylenecepham of the formula ##STR1## wherein R.sup.1 is amino or substituted amino and R.sup.2 is a carboxy-protecting group comprising reacting a cephem of the formula ##STR2## wherein R.sup.1 and R.sup.2 are as defined above and X is halogen with lead metal while maintaining the pH of the reaction system at about 0.1 to 8. The cephem (I) may be reacted with a catalytic amount of lead metal or a lead compound in the presence of a metal having a greater ionization tendency than lead.

公开(公告)号：US4689411A

公开(公告)日：1987-08-25

申请号：US865651

申请日：1986-05-15

申请人： Sigeru Torii ,  Kenji Uneyama ,  Hideo Tanaka ,  Junzo Nokami ,  Michio Sasaoka ,  Norio Saito ,  Takashi Shiroi

发明人： Sigeru Torii ,  Kenji Uneyama ,  Hideo Tanaka ,  Junzo Nokami ,  Michio Sasaoka ,  Norio Saito ,  Takashi Shiroi

IPC分类号： C07D205/095 ,  C07D403/12 ,  C07D501/02 ,  C07D501/08 ,  C07F9/568 ,  C07D205/08 ,  C07F9/65

CPC分类号： C07D403/12 ,  C07D205/095 ,  C07F9/568

摘要： This invention provides azetidinone derivatives represented by the formula ##STR1## and processes for preparing the same. The azetidinone derivatives are used as the intermediates for producing cephalosporin compounds useful as antibiotic agents.

摘要翻译： 本发明提供由式“IMAGE”表示的氮杂环丁酮衍生物及其制备方法。 氮杂环丁酮衍生物用作生产用作抗生素剂的头孢菌素化合物的中间体。

公开(公告)号：US5126447A

公开(公告)日：1992-06-30

申请号：US662605

申请日：1991-03-01

申请人： Sigeru Torii ,  Hideo Tanaka ,  Masatoshi Taniguchi ,  Michio Sasaoka ,  Takashi Shiroi ,  Ryo Kikuchi ,  Yutaka Kameyama

发明人： Sigeru Torii ,  Hideo Tanaka ,  Masatoshi Taniguchi ,  Michio Sasaoka ,  Takashi Shiroi ,  Ryo Kikuchi ,  Yutaka Kameyama

IPC分类号： B01J23/36 ,  B01J23/46 ,  C01B11/22 ,  C07B61/00 ,  C07D205/085 ,  C07D205/095 ,  C07D403/04 ,  C07D405/14 ,  C07F7/18

CPC分类号： C07D403/04 ,  C07D205/085 ,  C07D205/095 ,  C07D405/14 ,  C07F7/186 ,  Y02P20/55

摘要： A process for preparing a .beta.-lactam derivative of formula (2) and/or the corresponding enol tautomer, which includes oxidizing an alkenyl-substituted .beta.-lactam derivative of formula (1) in the presence of a ruthenium catalyst or a rhenium catalyst using a periodic acid: ##STR1## wherein R.sup.1 is a hydrogen atom, a C.sub.1-4 alkyl group or a C.sub.1-4 haloalkyl group, R.sup.2 is a hydrogen atom, a C.sub.1-4 alkyl group or a phenyl group which may have a substituent, A is a group selected from ##STR2## wherein R.sup.3 is an amino group or a protected amino group, and R.sup.4 -R.sup.8 are as defined in the application.

公开(公告)号：US4853468A

公开(公告)日：1989-08-01

申请号：US166918

申请日：1988-03-11

申请人： Sigeru Torii ,  Kenji Uneyama ,  Hideo Tanaka ,  Junzo Nokami ,  Michio Sasaoka ,  Norio Saito ,  Takashi Shiroi

发明人： Sigeru Torii ,  Kenji Uneyama ,  Hideo Tanaka ,  Junzo Nokami ,  Michio Sasaoka ,  Norio Saito ,  Takashi Shiroi

IPC分类号： C07D205/095 ,  C07D403/12 ,  C07D501/02 ,  C07D501/08 ,  C07F9/568

CPC分类号： C07D403/12 ,  C07D205/095 ,  C07F9/568

摘要： This invention provides azetidinone derivatives represented by the formula ##STR1## and processes for preparing the same. The azetidinone derivatives are used as the intermediates for producing cephalosporin compounds useful as antibiotic agents.

摘要翻译： 本发明提供由式“IMAGE”表示的氮杂环丁酮衍生物及其制备方法。 氮杂环丁酮衍生物用作生产用作抗生素剂的头孢菌素化合物的中间体。

公开(公告)号：US4784734A

公开(公告)日：1988-11-15

申请号：US71664

申请日：1987-07-09

申请人： Sigeru Torii ,  Kenji Uneyama ,  Hideo Tanaka ,  Junzo Nokami ,  Michio Sasaoka ,  Norio Saito ,  Takashi Shiroi

发明人： Sigeru Torii ,  Kenji Uneyama ,  Hideo Tanaka ,  Junzo Nokami ,  Michio Sasaoka ,  Norio Saito ,  Takashi Shiroi

IPC分类号： C07D205/095 ,  C07D403/12 ,  C07F9/568 ,  C25B3/06

CPC分类号： C07D403/12 ,  C07D205/095 ,  C07F9/568

摘要： This invention provides azetidinone derivatives represented by the formula ##STR1## and processes for preparing the same. The azetidinone derivatives are used as the intermediates for producing cephalosporin compounds useful as antibiotic agents.

摘要翻译： 本发明提供由式“IMAGE”表示的氮杂环丁酮衍生物及其制备方法。 氮杂环丁酮衍生物用作生产用作抗生素剂的头孢菌素化合物的中间体。

公开(公告)号：US5206361A

公开(公告)日：1993-04-27

申请号：US665863

申请日：1991-03-07

申请人： Sigeru Torii ,  Hideo Tanaka ,  Masatoshi Taniguchi ,  Michio Sasaoka ,  Takashi Shiroi ,  Yutaka Kameyama

发明人： Sigeru Torii ,  Hideo Tanaka ,  Masatoshi Taniguchi ,  Michio Sasaoka ,  Takashi Shiroi ,  Yutaka Kameyama

IPC分类号： C07D499/00 ,  C07D499/04 ,  C07D499/12 ,  C07D499/87 ,  C07D513/04

CPC分类号： C07D513/04 ,  C07D499/00 ,  Y02P20/55

摘要： The present invention provides a thiazolinoazetidinone derivative represented by the formula ##STR1## wherein R.sup.1 is phenyl having or not having substituent(s), methyl having or not having substituent(s) or ##STR2## group, R.sup.3 being phenyl having or not having substituent(s), and R.sup.2 is a hydrogen atom or carboxylic acid protective group, and a process for preparing the same.The present invention further provides a process for preparing a 2-exo-methylenepenam derivative characterized by hydrolyzing the thiazoline ring of a thiazolinoazetidinone derivative of the above formula (1) to effect recyclization and obtain a 2-exo-methylenepenam derivative represented by the formula ##STR3## wherein R.sup.1 and R.sup.2 are as defined above.

公开(公告)号：US5142040A

公开(公告)日：1992-08-25

申请号：US665838

申请日：1991-03-07

申请人： Sigeru Torii ,  Hideo Tanaka ,  Masatoshi Taniguchi ,  Michio Sasaoka ,  Takashi Shiroi ,  Ryo Kikuchi ,  Yutaka Kameyama

发明人： Sigeru Torii ,  Hideo Tanaka ,  Masatoshi Taniguchi ,  Michio Sasaoka ,  Takashi Shiroi ,  Ryo Kikuchi ,  Yutaka Kameyama

IPC分类号： C07D501/00 ,  C07D501/04 ,  C07D501/24 ,  C07D501/26

CPC分类号： C07D501/00 ,  Y02P20/55

摘要： The present invention provides a process for preparing a 3-formylcephem derivative represented by the formula (2) ##STR1## which comprises oxidizing in the presence of oxygen a 3-halomethylcephem derivative represented by the formula (1) ##STR2## wherein R.sup.1 is amino group or protected amino group, R.sup.2 is hydrogen atom or a carboxylic acid protective group, X is halogen atom.

公开(公告)号：US4566996A

公开(公告)日：1986-01-28

申请号：US567736

申请日：1984-01-03

申请人： Sigeru Torii ,  Hideo Tanaka ,  Takashi Shiroi ,  Michio Sasaoka ,  Norio Saito ,  Kiyotoshi Matsumura

发明人： Sigeru Torii ,  Hideo Tanaka ,  Takashi Shiroi ,  Michio Sasaoka ,  Norio Saito ,  Kiyotoshi Matsumura

IPC分类号： C07D205/08 ,  C07D205/095 ,  C07D405/12

CPC分类号： C07D205/095 ,  Y02P20/55

摘要： A process for preparing an azetidinone derivative represented by the formula (1) ##STR1## wherein R.sup.1 represents a substituted or unsubstituted aryl group, a substituted or unsubstituted phenylmethyl group or a substituted or unsubstituted phenoxymethyl group, R.sup.2 represents a hydrogen atom or a group for protecting carboxylic acid and Ar represents a substituted or unsubstituted phenyl group, the process comprising reacting a thiazolineazetidinone derivative represented by the formula (2) ##STR2## wherein R.sup.1 and R.sup.2 are as defined above with a sulfonyl bromide represented by the formula (3)Ar--SO.sub.2 --Br (3)wherein Ar is as defined above in water-containing organic solvent.

摘要翻译： 制备由式（1）表示的氮杂环丁酮衍生物的方法其中R1表示取代或未取代的芳基，取代或未取代的苯基甲基或取代或未取代的苯氧基甲基，R2表示氢原子或 用于保护羧酸和Ar的基团代表取代或未取代的苯基，该方法包括使式（2）表示的噻唑啉氮杂环丁酮衍生物（2）其中R1和R2如上定义， 式（3）Ar-SO 2-Br（3）其中Ar如上所述在含水有机溶剂中。

公开(公告)号：US4499265A

公开(公告)日：1985-02-12

申请号：US406568

申请日：1982-08-09

申请人： Sigeru Torii ,  Hideo Tanaka ,  Junzo Nokami ,  Takashi Shiroi ,  Norio Saito ,  Michio Sasaoka

发明人： Sigeru Torii ,  Hideo Tanaka ,  Junzo Nokami ,  Takashi Shiroi ,  Norio Saito ,  Michio Sasaoka

IPC分类号： C07D501/08 ,  C07D501/14 ,  C07D513/04

CPC分类号： C07D513/04 ,  Y02P20/55

摘要： This invention provides a process for preparing a 3-exo-methylenecepham derivative represented by the formula ##STR1## wherein R.sup.1 represents an aralkyl or aryloxymethyl group both of which may be substituted on the aromatic ring, and R.sup.2 represents a carboxyl-protecting group, the process comprising subjecting a compound represented by the formula ##STR2## wherein R.sup.1 and R.sup.2 are as defined above, to a cyclization reaction in an acidic water-containing solvent.

摘要翻译： 本发明提供一种制备由式（III）表示的3-外 - 亚甲基头孢衍生物的方法，其中R 1表示可在芳环上被取代的芳烷基或芳氧基甲基，R2表示羧基保护基 该方法包括将其中R 1和R 2如上所定义的式Ⅺ（II）表示的化合物在酸性含水溶剂中进行环化反应。