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1. 发明授权

US5599925A Penam derivatives 失效
标题翻译： Penam衍生物
公开(公告)号：US5599925A
公开(公告)日：1997-02-04
申请号：US314307
申请日：1994-09-30
申请人： Shigeru Torii , Hideo Tanaka , Masatoshi Taniguchi , Mitio Sasaoka , Takashi Shiroi , Yutaka Kameyama
发明人： Shigeru Torii , Hideo Tanaka , Masatoshi Taniguchi , Mitio Sasaoka , Takashi Shiroi , Yutaka Kameyama
IPC分类号： C07D499/00 , C07D499/86 , C07D499/87 , C07D499/897
CPC分类号： C07D499/00 , Y02P20/55
摘要： A penam derivative of the general formula ##STR1## wherein R.sup.1 means hydrogen, halogen, amino or protected amino; R.sup.2 means hydrogen, halogen, lower alkoxy, lower acyl, lower alkyl, hydroxy- or protected hydroxy-substituted lower alkyl, hydroxy or protected hydroxy, or R.sup.1 and R.sup.2 may jointly represent oxo; R.sup.3 means hydrogen or a carboxy-protecting group; R.sup.4 means hydrogen; R.sup.5 means a group of the formula --CH.sub.2 Y where Y means halogen, --N.sub.3, --ONO.sub.2, --OR.sup.6, --OCOR.sup.6, --SCSOR.sup.6, --SCSN(R.sup.6).sub.2, --SR.sup.6, --SO.sub.2 R.sup.6, --NHR.sup.6, --N(R.sup.6).sub.2 or a substituted or unsubstituted nitrogen-containing heterocyclic group having a free valence on nitrogen; R.sup.6 means a lower alkyl, aryl or heterocyclic group which is substituted or unsubstituted; or R.sup.4 and R.sup.5 may jointly represent .dbd.CH.sub.2 ; n means 0, 1 or 2; provided, however, that where R.sup.4 and R.sup.5 jointly represent .dbd.CH.sub.2, n is not equal to 0.
摘要翻译：其中R 1表示氢，卤素，氨基或被保护的氨基; R 2表示氢，卤素，低级烷氧基，低级酰基，低级烷基，羟基或保护的羟基取代的低级烷基，羟基或保护的羟基，或者R 1和R 2可以共同表示氧代; R3表示氢或羧基保护基; R4表示氢; R5表示式-CH2Y的基团，其中Y表示卤素，-N3，-ONO2，-OR6，-OCOR6，-SCSOR6，-SCSN（R6）2，-SR6，-SO2R6，-NHR6，-N（R6） 2或在氮上具有游离价的取代或未取代的含氮杂环基; R6表示取代或未取代的低级烷基，芳基或杂环基; 或者R4和R5可以共同表示= CH2; n表示0,1或2; 但是，如果R4和R5共同表示= CH2，则n不等于0。

2. 发明授权

US5288860A Process for preparing thiazolino azetidinone and 2-exo-methylenepenam derivative 失效
标题翻译：制备噻唑基氮杂环丁酮和2-外 - 亚甲基台am am嗪衍生物的方法
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。

3. 发明授权

US4958018A Method for production of 3-exomethylenecepham derivatives 失效
标题翻译： 3-甲磺酰头孢衍生物的生产方法
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.

4. 发明授权

US5126447A Process for preparation of .beta.-lactam derivative from an alkenyl substituted .beta.-lactam derivative using a ruthenium or rhenium catalyst and a periodic acid 失效
标题翻译：使用钌或铑催化剂和周期酸从碱性取代（BETA）-LACTAM衍生物衍生得到的（BETA）-LACTAM衍生物的方法
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.

5. 发明授权

US5206361A Thiazolinoazetidinone derivative 失效
标题翻译：噻唑烷酮衍生物
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.

6. 发明授权

US5142040A Process for preparing a 3-formylcephem derivative 失效
标题翻译：制备三甲酚衍生物的方法
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.

7. 发明授权

US5204458A Process for preparing cephem derivatives 失效
标题翻译：制备CEPHEM衍生物的方法
公开(公告)号：US5204458A
公开(公告)日：1993-04-20
申请号：US849160
申请日：1992-03-10
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： C07D501/00 , C07D501/08 , C07D501/59
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 .beta.-lactam compound represented by the formula (1) ##STR1## wherein R.sup.1 is amino or protected amino, R.sup.2 is a hydrogen atom or lower alkoxyl, R.sup.3 is a hydrogen atom or carboxylic acid protecting group and X is the group --SO.sub.2 R.sup.4 or --SR.sup.4, R.sup.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) ##STR2## wherein R.sup.1, R.sup.2 and R.sup.3 are as defined above, and Y is the residue of the nucleophilic agent.

8. 发明授权

US5196530A Process for preparing 2-exo-methylenepenam derivatives 失效
标题翻译：制备2-异 - 甲基衍生物的方法
公开(公告)号：US5196530A
公开(公告)日：1993-03-23
申请号：US848939
申请日：1992-03-10
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 , C07D499/86 , C07D499/87
CPC分类号： C07D499/00
摘要： The present invention provides a process for preparing a 2-exo-methylenepenam derivative represented by the formula (2), the process being characterized by reacting an allenyl .beta.-lactum compound represented by the formula (1) with a metallic reducing agent, in which R.sup.1, R.sup.2, R.sup.3 and X are defined in the specification. ##STR1##

9. 发明授权

US4886891A Process for preparing 1,1-disubstituted ethylene derivative by reaction of lead with a carbinol derivative 失效
标题翻译：通过铅与甲醇衍生物的反应制备1,1-二取代乙烯衍生物的方法
公开(公告)号：US4886891A
公开(公告)日：1989-12-12
申请号：US134852
申请日：1987-12-18
申请人： Shigeru Torii , Masatoshi Taniguchi , Michio Sasaoka , Yoshihisa Tomotaki , Mitsuo Akada , Hideo Tanaka , Akira Suzuki , Shiro Yamashita
发明人： Shigeru Torii , Masatoshi Taniguchi , Michio Sasaoka , Yoshihisa Tomotaki , Mitsuo Akada , Hideo Tanaka , Akira Suzuki , Shiro Yamashita
IPC分类号： C07C43/225 , C07B31/00 , C07B35/02 , C07B37/06 , C07C17/00 , C07C17/35 , C07C17/363 , C07C21/04 , C07C21/19 , C07C22/02 , C07C22/04 , C07C27/00 , C07C29/00 , C07C33/40 , C07C33/42 , C07C37/00 , C07C37/50 , C07C39/373 , C07C41/00 , C07C41/24 , C07C45/00 , C07C45/65 , C07C49/463 , C07C49/687 , C07C49/80 , C07C51/00 , C07C51/09 , C07C57/52 , C07C67/00 , C07C67/317 , C07C69/618 , C07C69/743 , C07C231/00 , C07C231/12 , C07C233/03 , C07C233/11 , C07C253/00 , C07C253/30 , C07C255/10 , C07C255/31 , C07C255/35 , C07C255/54 , C07D317/52
CPC分类号： C07C255/00 , C07C17/00 , C07C17/363 , C07C29/58 , C07C37/001 , C07C37/002 , C07C41/24 , C07C45/65 , C07C49/687 , C07C49/80 , C07C51/09 , C07C67/327 , C07D317/52 , C07C2101/16 , C07C2101/18
摘要： The present invention provides a process for preparing a 1,1-disubstituted ethylene derivative of the formula ##STR1## which comprises reacting lead with a carbinol derivative of the formula ##STR2## wherein R.sup.1, R.sup.2, R.sup.3, X, Y, m and n are defined in the specification. The reaction is conducted more advantageously in the presence of a metal having higher ionization tendency than lead.

10. 发明授权

US4912213A Process for preparing penicillanic acid derivatives 失效
标题翻译：制备青霉烷酸衍生物的方法
公开(公告)号：US4912213A
公开(公告)日：1990-03-27
申请号：US241186
申请日：1988-09-07
申请人： Masatoshi Taniguchi , Michio Sasaoka , Kiyotoshi Matsumura , Ichiro Kawahara , Kenji Kase , Daisuke Suzuki , Shigeru Torii , Hideo Tanaka , Motoaki Tanaka , Akira Nakai
发明人： Masatoshi Taniguchi , Michio Sasaoka , Kiyotoshi Matsumura , Ichiro Kawahara , Kenji Kase , Daisuke Suzuki , Shigeru Torii , Hideo Tanaka , Motoaki Tanaka , Akira Nakai
IPC分类号： C07D499/87 , B01J23/14 , B01J27/135 , C07B61/00 , C07D499/00 , C07D499/86 , C07D499/897
CPC分类号： C07D499/00 , Y02P20/55
摘要： The present invention provides a process for preparing a penicillanic acid derivative of the formula ##STR1## which comprises reacting lead with a halogenated penicillanic acid derivative of the formula ##STR2## wherein X, Y, Z and R.sup.1 are as defined in the specification. The reaction is advantageously conducted in the presence of a metal having higher ionization tendency than lead such as aluminum, iron, magnesium or a mixture thereof.

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