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1. 发明授权

US4609438A Process for preparing thiosulfonate derivatives 失效
标题翻译：硫代磺酸衍生物的制备方法
公开(公告)号：US4609438A
公开(公告)日：1986-09-02
申请号：US673309
申请日：1984-11-20
申请人： Sigeru Torii , Hideo Tanaka , Michio Sasaoka , Seiryu Uto , Yutaka Kameyama
发明人： Sigeru Torii , Hideo Tanaka , Michio Sasaoka , Seiryu Uto , Yutaka Kameyama
IPC分类号： C25B3/10 , C07D277/78 , C25B3/00
CPC分类号： C07D277/78 , C25B3/00
摘要： This invention provides a process for preparing a thiosulfonate derivative represented by the formulaR.sup.2 SO.sub.2 SR.sup.1 (III)wherein R.sup.1 is substituted or unsubstituted 2-benzothiazolyl, and R.sup.2 is substituted or unsubstituted phenyl, the process being characterized in that a compound represented by the formulaR.sup.1 SX (I)wherein R.sup.1 is as defined above, and X is hydrogen, alkali metal or SR.sup.1, and a sulfinic acid or a salt thereof represented by the formulaR.sup.2 SO.sub.2 Y (II)wherein R.sup.2 is as defined above, and Y is a hydrogen atom, alkali metal atom, alkaline earth metal atom or quaternary ammonium are subjected to an electrolytic reaction in a mixture of water and an organic solvent in the presence of a halogen salt.
摘要翻译：本发明提供一种制备由式R 2 SO 2 S R 1（III）表示的硫代磺酸酯衍生物的方法，其中R 1为取代或未取代的2-苯并噻唑基，R 2为取代或未取代的苯基，该方法的特征在于式R1SX I）其中R1如上所定义，X是氢，碱金属或SR1，以及由式R2SO2Y（Ⅱ）表示的亚磺酸或其盐，其中R2如上定义，Y是氢原子，碱金属原子，碱土金属原子或季铵在卤素盐存在下，在水和有机溶剂的混合物中进行电解反应。

2. 发明授权

US4599151A Process for preparing 2,2-bishalomethylpenam derivatives 失效
标题翻译： 2,2-二油基甲基衍生物的制备方法
公开(公告)号：US4599151A
公开(公告)日：1986-07-08
申请号：US711922
申请日：1985-03-15
申请人： Sigeru Torii , Hideo Tanaka , Michio Sasaoka , Takashi Shiroi , Seiryu Uto
发明人： Sigeru Torii , Hideo Tanaka , Michio Sasaoka , Takashi Shiroi , Seiryu Uto
IPC分类号： C25B3/04 , C07D499/00 , C07D499/06 , C07D499/44 , C25B3/00 , C25B3/06
CPC分类号： C07D499/00 , Y02P20/55
摘要： This invention provides a process for preparing a 2,2-bishalomethylpenam derivative represented by the formula ##STR1## wherein R.sup.1 represents a lower alkyl group, aryl group, arylmethyl group, arylcarbonyl group or aryloxymethyl group, R.sup.2 represents a carboxyl-protecting group, X.sup.1 and X.sup.2 are the same or different and represent a halogen atom, the process being characterized in that a disulfide represented by the formula ##STR2## wherein R.sup.1, R.sup.2 and X.sup.1 are as defined above and R.sup.3 represents an aryl group or heterocyclic group is subjected to an electrolytic reaction in a solvent in the presence of a halogen acid and/or halogen salt.
摘要翻译：本发明提供一种制备式（I）表示的2,2-二油基甲基联苯胺衍生物的方法，其中R1表示低级烷基，芳基，芳基甲基，芳基羰基或芳氧基甲基，R2表示羧基保护基基团，X1和X2相同或不同，表示卤素原子，该方法的特征在于由式（II）表示的二硫化物，其中R 1，R 2和X 1如上所定义，R 3表示芳基或杂环基在卤素酸和/或卤素盐的存在下在溶剂中进行电解反应。

3. 发明授权

US4713452A Process for preparation of azetidinone derivatives 失效
标题翻译：氮杂环丁酮衍生物的制备方法
公开(公告)号：US4713452A
公开(公告)日：1987-12-15
申请号：US680723
申请日：1984-12-12
申请人： Sigeru Torii , Hideo Tanaka , Michio Sasaoka , Seiryu Uto , Syozo Hayase
发明人： Sigeru Torii , Hideo Tanaka , Michio Sasaoka , Seiryu Uto , Syozo Hayase
IPC分类号： C07D205/08 , A61K31/395 , A61K31/397 , A61P31/04 , C07D205/09 , C07D205/095 , C07D417/12 , C07B45/00 , C07F7/10 , C07F9/65
CPC分类号： C07D205/09 , C07D205/095
摘要： A process for preparing an azetidinone derivative represented by the formula ##STR1## wherein R.sup.1 is hydrogen, halogen or lower alkoxy, R.sup.2 is hydrogen, halogen, lower alkoxy, amino or a group ##STR2## (in which R.sup.5 is substituted or unsubstituted phenyl, substituted or unsubstituted phenylmethyl, substituted or unsubstituted phenoxymethyl, or substituted or unsubstituted benzoyl), or R.sup.1 and R.sup.2, when taken together, are carbonyl, R.sup.3 is substituted or unsubstituted phenyl, and R.sup.4 is hydrogen, optionally substituted hydrocarbon residue or acyl, silyl, sulfonyl or phosphonyl derived from inorganic acid or organic acid, the process comprising reacting a dithioazetidinone derivative represented by the formula ##STR3## wherein R.sup.1, R.sup.2 and R.sup.4 are as defined above and R.sup.9 is substituted or unsubstituted, nitrogen-containing aromatic heterocyclic residue with a compound represented by the formulaR.sup.3 SO.sub.2 CN (VII)wherein R.sup.3 is defined above.
摘要翻译：制备式（I）表示的氮杂环丁酮衍生物的方法，其中R 1是氢，卤素或低级烷氧基，R 2是氢，卤素，低级烷氧基，氨基或基团（其中R 5是取代的或未取代的苯基，取代或未取代的苯基甲基，取代或未取代的苯氧基甲基或取代或未取代的苯甲酰基），或R 1和R 2一起为羰基，R 3为取代或未取代的苯基，且R 4为氢，任选取代的烃残基或酰基，衍生自无机酸或有机酸的甲硅烷基，磺酰基或膦酰基，该方法包括使由式（VI）表示的二硫代氮杂环丁酮衍生物（其中R 1，R 2和R 4如上所定义）和R 9是取代或未取代的，含有由式R 3 SO 2 CN（Ⅶ）表示的化合物的芳族杂环残基，其中R 3如上定义。

4. 发明授权

US5905147A Process for preparing .beta.-lactam compound 失效
标题翻译： β-内酰胺化合物的制备方法
公开(公告)号：US5905147A
公开(公告)日：1999-05-18
申请号：US732443
申请日：1996-11-06
申请人： Sigeru Torii , Hideo Tanaka , Michio Sasaoka , Yutaka Kameyama
发明人： Sigeru Torii , Hideo Tanaka , Michio Sasaoka , Yutaka Kameyama
IPC分类号： C07D205/09 , C07D499/00 , C07D499/06 , C07D205/08 , C07B39/00
CPC分类号： C07D499/00 , C07D205/09
摘要： The present invention provides a process for producing a .beta.-lactam halide compound represented by the general formula (2) which process is characterized in that the hydroxyl group of a .beta.-lactam halide compound represented by the general formula (1) is substituted with a halogen atom or a leaving group. ##STR1##
摘要翻译： PCT No.PCT / JP96 / 00549 Sec。 371日期：1996年11月6日 102（e）日期1996年11月6日PCT 1996年3月7日PCT公布。公开号WO96 / 28422 日本1996年9月19日本发明提供了制备由通式（2）表示的β-内酰胺卤化物的方法，该方法的特征在于通式（1）表示的β-内酰胺卤化物的羟基）被卤素原子或离去基团取代。

5. 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。

6. 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.

7. 发明授权

US5977352A Process for preparing 3-norcephem compounds 失效
标题翻译： 3-诺司匹林化合物的制备方法
公开(公告)号：US5977352A
公开(公告)日：1999-11-02
申请号：US11041
申请日：1998-02-06
申请人： Michio Sasaoka , Sigeru Torii , Hideo Tanaka , Ryo Kikuchi , Yutaka Kameyama
发明人： Michio Sasaoka , Sigeru Torii , Hideo Tanaka , Ryo Kikuchi , Yutaka Kameyama
IPC分类号： C07D501/00 , C07D501/08 , C07D501/16 , C07D501/20 , C07D501/22
CPC分类号： C07D501/00 , Y02P20/55
摘要： The present invention provides a process for preparing 3-norcephem compound represented by the formula (2), characterized in that a hydride reagent is acted on a halogenated .beta.-lactam compound represented by the formula (1) in the presence of a cuprous compound ##STR1## wherein R.sub.1 is a hydrogen atom, amino group or protected amino group, R.sub.2 is an aryl or substituted aryl, n is 0 to 2, R.sub.3 is a hydrogen atom or carboxylic acid protective group, X is a halogen atom, and Y is a halogen atom or a leaving group ##STR2## wherein R.sub.1 and R.sub.3 are as defined above.
摘要翻译： PCT No.PCT / JP97 / 01994 Sec。 371日期1998年2月6日 102（e）1998年2月6日PCT 1997年6月9日PCT公布。出版物WO97 / 47627 日期：1997年12月18日本发明提供一种制备式（2）表示的3-去头孢烯化合物的方法，其特征在于，在式（1）表示的卤代β-内酰胺化合物的作用下，的化合物，其中R1是氢原子，氨基或保护的氨基，R2是芳基或取代的芳基，n是0-2，R3是氢原子或羧酸保护基，X是卤素原子，和 Y是卤素原子或离去基团，其中R 1和R 3如上所定义。

8. 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.

9. 发明授权

US4629542A Process for preparing 3-exomethylenecepham derivatives 失效
标题翻译： 3-甲磺酰头孢衍生物的制备方法
公开(公告)号：US4629542A
公开(公告)日：1986-12-16
申请号：US707767
申请日：1985-03-04
申请人： Sigeru Torii , Hideo Tanaka , Michio Sasaoka , Yutaka Kameyama
发明人： Sigeru Torii , Hideo Tanaka , Michio Sasaoka , Yutaka Kameyama
IPC分类号： C25B3/04 , A61K31/545 , C07D501/04 , C07D501/14 , C25B3/00
CPC分类号： C07D501/04 , A61K31/545 , C07D501/14 , C25B3/00 , Y02P20/55
摘要： This invention provides a process for preparing 3-exomethylenecepham derivatives represented by the formula ##STR1## wherein R.sup.1 is arylacetylamino, aryloxyacetylamino, heterocyclic acetylamino or imido, and R.sup.2 is a protective group for the carboxyl, the process being characterized in that a 3-halomethylcephem compound represented by the formula ##STR2## wherein R.sup.1 and R.sup.2 are as defined above, and X is a halogen atom is electrolyzed in a mixture of a hydrophilic organic solvent and water.
摘要翻译：本发明提供了一种制备由下式表示的3-甲磺酰头孢烯衍生物的方法：其中R1是芳基乙酰基氨基，芳氧基乙酰氨基，杂环乙酰氨基或亚氨基，R2是羧基的保护基，该方法的特征在于3-卤代甲基头孢烯其中R1和R2如上所定义，X是卤素原子的式“IMAGE”表示的化合物在亲水性有机溶剂和水的混合物中电解。

10. 发明授权

US5929233A Cyclization for preparing halo-cephems 失效
标题翻译：用于制备晕圈的环化
公开(公告)号：US5929233A
公开(公告)日：1999-07-27
申请号：US732445
申请日：1996-11-06
申请人： Sigeru Torii , Hideo Tanaka , Michio Sasaoka , Yutaka Kameyama , Isao Wada , Yasuhisa Amano
发明人： Sigeru Torii , Hideo Tanaka , Michio Sasaoka , Yutaka Kameyama , Isao Wada , Yasuhisa Amano
IPC分类号： C07D205/09 , C07D205/095 , C07D501/00 , C07D501/08 , C07D513/04
CPC分类号： C07D513/04 , C07D205/09 , C07D205/095 , C07D501/00
摘要： The invention provides a process for preparing an allenyl .beta.-lactam of formula (4), by reacting the hydroxyl group of a .beta.-lactam of formula (1) with a reactive derivative of sulfonic acid of formula (2) to convert the compound of formula (1) to a .beta.-lactam of formula (3), thereafter reacting the resulting .beta.-lactam with a basic anion exchange resin of the type having a tertiary organic base fixed to the resin and isolating the allenyl .beta.-lactam of formula (4) with stability and high purity in a high yield.The invention also provides a process for preparing an allenyl .beta.-lactam of formula (4), by reacting the hydroxyl group of a .beta.-lactam compound of formula (1) with a reactive derivative of sulfonic acid of formula (2) to convert the compound of the formula (1) to a .beta.-lactam compound of formula (3), thereafter reacting the resulting .beta.-lactam of formula (3) with a tertiary organic base to convert the compound (3) to the allenyl .beta.-lactam of formula (4), thereafter causing two kinds of ion exchange resins, i.e., an acidic cation exchange resin and a basic anion exchange resin, to alternately or simultaneously act on the lactam of formula (4) and isolating the allenyl .beta.-lactam of formula (4).Further, the invention provides a process for preparing a 3-halogenated cephem of formula (6), characterized by causing a halogenating reagent to act on an allenyl .beta.-lactam of formula (4) in the presence of a sulfinate ion or thiolate ion capturing agent to obtain the 3-halogenated cephem.
摘要翻译： PCT No.PCT / JP96 / 00575 Sec。 371日期：1996年11月6日 102（e）日期1996年11月6日PCT 1996年3月8日PCT公布。公开号WO96 / 29334 日期1996年9月26日本发明提供通过使式（1）的β-内酰胺的羟基与式（2）的磺酸的反应性衍生物反应制备式（4）的烯丙基β-内酰胺的方法，将式（1）化合物转化成式（3）的β-内酰胺，然后将所得的β-内酰胺与具有叔有机碱类型的碱式阴离子交换树脂反应固定在树脂上并分离丙烯基β 式（4）的内酰胺，其产率稳定，纯度高。本发明还提供了通过使式（1）的β-内酰胺化合物的羟基与式（2）的磺酸的反应性衍生物反应来制备式（4）的烯丙基β-内酰胺的方法，以将式（1）的化合物与式（3）的β-内酰胺化合物反应，然后使得到的式（3）的β-内酰胺与叔有机碱反应，将化合物（3）转化为式（4），然后使两种离子交换树脂，即酸性阳离子交换树脂和碱性阴离子交换树脂交替或同时作用于式（4）的内酰胺，并分离式（4）。此外，本发明提供了制备式（6）的3-卤代头孢烯的方法，其特征在于，在亚磺酸根离子或硫醇盐离子捕获的存在下，使卤化试剂作用于式（4）的烯丙基β-内酰胺代理获得3卤代头孢烯。

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