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51. 发明授权

US06339152B1 Process for producing exo-methylenepenam compounds 失效
标题翻译：生产外亚甲基山梨醇化合物的方法
公开(公告)号：US06339152B1
公开(公告)日：2002-01-15
申请号：US09380582
申请日：1999-09-07
申请人： Sigeru Torii , Hideo Tanaka , Yutaka Kameyama , Yoshihisa Tokumaru
发明人： Sigeru Torii , Hideo Tanaka , Yutaka Kameyama , Yoshihisa Tokumaru
IPC分类号： C07D49987
CPC分类号： C07D499/00 , Y02P20/55
摘要： The present invention is directed to a process for preparing an exo-methylenepenam compound wherein a cephem compound is reduced with a metal having a standard oxidation-reduction potential of up to −0.3 (V/SCE) in an amount of at least one mole per mole of the cephem compound and with a metal compound having a higher standard oxidation reduction potential than the metal and in an amount of 0.001 to 10 moles per mole of the cephem compound and wherein X is a halogen atom, lower alkylsulfonyloxy, trifluoromethanesulfonyloxy, trichloromethanesulfonyloxy, arylsulfonyloxy, toluenesulfonyloxy, or halogenated sulfonyloxy
摘要翻译：本发明涉及一种制备外亚甲基环戊二烯化合物的方法，其中头孢烯化合物以至少为1摩尔量的标准氧化还原电位高达-0.3（V / SCE）的金属还原和具有比金属高的标准氧化还原电位的金属化合物，并且每摩尔头孢烯化合物的量为0.001至10摩尔，其中X为卤素原子，低级烷基磺酰氧基，三氟甲磺酰氧基，三氯甲磺酰氧基，芳基磺酰氧基，甲苯磺酰氧基或卤代磺酰氧基

52. 发明授权

US4891369A 2.beta.-Substituted-methylpenicillanic acid derivatives, and salts and esters thereof 失效
标题翻译： 2β-取代 - 甲基青霉烷酸衍生物及其盐和酯
公开(公告)号：US4891369A
公开(公告)日：1990-01-02
申请号：US123631
申请日：1987-11-23
申请人： Sigeru Torii , Hideo Tanaka , Motoaki Tanaka , Shozo Yamada , Akira Nakai , Hisashi Ohbayashi , Tomoyasu Ohno
发明人： Sigeru Torii , Hideo Tanaka , Motoaki Tanaka , Shozo Yamada , Akira Nakai , Hisashi Ohbayashi , Tomoyasu Ohno
IPC分类号： C07D499/00 , C07D499/04 , C07D499/21 , C07D499/42 , C07D499/44 , C07D499/86
CPC分类号： C07D499/00 , Y02P20/55
摘要： Disclosed are 2.beta.-substituted-methylpenicillanic acid compounds of the formula ##STR1## wherein n is 0, 1 or 2; and ##STR2## is monocyclic or bicyclic heterocyclic ring group which has 2 to 4 nitrogen atoms as hetero atom in its ring structure and which may be optionally substituted with alkyl, alkoxycarbonyl, phenyl, formyl or benzyloxycarbonyl optionally having alkyl, nitro or a halogen atom on the benzene ring, with the proviso that said heterocyclic ring group is not 1,2,3-triazol-1-yl; or salts or esters thereof.These compounds are useful as .beta.-lactamase inhibitor.

53. 发明授权

US4482435A Process for preparing thiazolidine compounds 失效
标题翻译：制备噻唑烷化合物的方法
公开(公告)号：US4482435A
公开(公告)日：1984-11-13
申请号：US406518
申请日：1982-08-09
申请人： Sigeru Torii , Hideo Tanaka , Takashi Shiroi
发明人： Sigeru Torii , Hideo Tanaka , Takashi Shiroi
IPC分类号： C07D513/04 , C25B3/04 , C25B3/00
CPC分类号： C07D513/04 , C25B3/04
摘要： This invention provides a process for preparing a thiazolidine compound of the formula ##STR1## wherein R.sup.1 represents a hydrogen atom, alkyl group, aralkyl group, aryl group or aryloxymethyl group, and R.sup.2 represents a hydrogen atom or a group ##STR2## wherein R.sup.3 represents a hydrogen atom, alkyl group, halogenated alkyl group, benzyl group or silyl group, and X represents a hydrogen atom, halogen atom, hydroxy group, alkoxy group or acyloxy group, the process comprising electrolyzing a thiazoline compound represented by the formula ##STR3## wherein R.sup.1 and R.sup.2 are as defined above, in a mixture comprising a perchloric acid aqueous solution and an organic solvent.
摘要翻译：本发明提供了制备式（I）的噻唑烷化合物的方法，其中R 1表示氢原子，烷基，芳烷基，芳基或芳氧基甲基，R 2表示氢原子或基团其中R3表示氢原子，烷基，卤代烷基，苄基或甲硅烷基，X表示氢原子，卤素原子，羟基，烷氧基或酰氧基，该方法包括电解由式在其中R 1和R 2如上定义的含有高氯酸水溶液和有机溶剂的混合物中的图像（II）。

54. 发明授权

US4120764A Process for producing a tetraalkylthiuram disulfide 失效
标题翻译：生产四烷基秋兰姆二硫化物的方法
公开(公告)号：US4120764A
公开(公告)日：1978-10-17
申请号：US869409
申请日：1978-01-16
申请人： Sigeru Torii , Hideo Tanaka , Kiyoshi Mishima
发明人： Sigeru Torii , Hideo Tanaka , Kiyoshi Mishima
IPC分类号： C25B3/02 , C07C155/10
CPC分类号： C25B3/02
摘要： A process for producing a tetraalkylthiuram disulfide which comprises electrolytically oxidizing a dialkylammonium dialkyldithiocarbamate having the formula ##STR1## wherein each R represents an alkyl group having from 1 to 4 carbon atoms, in the presence or absence of a supporting electrolyte to produce a tetraalkylthiuram disulfide, the electrolytic oxidation being carried out in one or more solvents which dissolve at least one of the starting dialkylammonium dialkyldithiocarbamate and the resulting tetraalkylthiuram disulfide.
摘要翻译：一种生产四烷基秋兰姆二硫化物的方法，其包括电解氧化具有式“IMAGE”的二烷基二烷基二硫代氨基甲酸二烷基铵，其中每个R表示具有1至4个碳原子的烷基，在存在或不存在支持电解质的情况下，产生四烷基秋兰姆二硫化物，电解氧化在一种或多种溶剂中进行，所述溶剂溶解起始二烷基二烷基二硫代氨基甲酸烷基酯和所得的四烷基秋兰姆二硫化物中的至少一种。

55. 发明授权

US4898939A Process for preparing 2.beta.-substituted-methylpenicillin derivatives 失效
标题翻译：制备2β-取代 - 甲基青霉素衍生物的方法
公开(公告)号：US4898939A
公开(公告)日：1990-02-06
申请号：US316632
申请日：1989-02-28
申请人： Sigeru Torii , Hideo Tanaka , Motoaki Tanaka , Shozo Yamada , Akira Nakai
发明人： Sigeru Torii , Hideo Tanaka , Motoaki Tanaka , Shozo Yamada , Akira Nakai
IPC分类号： C07D499/87 , C07D499/00 , C07D499/86 , C07D499/897 , C07D521/00
CPC分类号： C07D231/12 , C07D233/56 , C07D249/08 , C07D499/00 , Y02P20/55
摘要： A process for preparing a 2.beta.-substituted-methylpenicillin compound of the formula ##STR1## wherein --N Y is an optionally substituted heterocyclic group containing 2 to 4 nitrogen atoms as the hetero atom in the ring structure, and R.sub.1 is a penicillin carboxyl protecting group, the process comprising reacting an azetidinonedisulfide compound of the formula ##STR2## wherein R.sub.1 is as defined above and R is a substituted or unsubstituted heterocyclic group with a nitrogen-containing heterocyclic compound of the formula ##STR3## wherein ##STR4## is as defined above in the presence of a metal compound.

56. 发明授权

US4238615A Cyclopentanone intermediates 2-(benzothiazolyl-2) 失效
标题翻译：环戊酮中间体2-（苯并噻唑基-2）
公开(公告)号：US4238615A
公开(公告)日：1980-12-09
申请号：US884222
申请日：1978-03-07
申请人： Sigeru Torii , Hideo Tanaka , Toshihiro Kudai
发明人： Sigeru Torii , Hideo Tanaka , Toshihiro Kudai
IPC分类号： C07C45/67 , C07D277/74 , C07D277/64
CPC分类号： C07D277/74 , C07C45/673
摘要： 2-Substituted-cyclopentanone derivatives represented by the formula ##STR1## are prepared by subjecting a 2-benzothiazolylsulfenamide derivative represented by the formula ##STR2## and cyclopentanone to condensation reaction, or by reacting the resulting condensation product with a hydrocarbon halide represented by the formulaR.sub.1 X.
摘要翻译：由式“IMAGE”表示的2-取代的环戊酮衍生物是通过使由式＆lt; IMAGE＆gt;表示的2-苯并噻唑基亚磺酰胺衍生物和环戊酮进行缩合反应，或通过使所得缩合产物与由式 R1X。

57. 发明授权

US5656754A Process for preparing cephem compounds 失效
标题翻译：头孢烯化合物的制备方法
公开(公告)号：US5656754A
公开(公告)日：1997-08-12
申请号：US211119
申请日：1994-03-22
申请人： Shigeru Torii , Hideo Tanaka , Michio Sasaoka , Takashi Shiroi , Yutaka Kameyama
发明人： Shigeru Torii , Hideo Tanaka , Michio Sasaoka , Takashi Shiroi , Yutaka Kameyama
IPC分类号： B01J27/122 , C07B61/00 , C07D205/08 , C07D205/09 , C07D205/095 , C07D501/00 , C07D501/08 , C07D501/18 , C07D501/22 , C07D501/16
CPC分类号： C07D205/09 , C07D205/095 , C07D501/00 , Y02P20/55
摘要： The present invention provides a process for preparing a cephem compound represented by the general formula (3) characterized in that an allenyl-.beta.-lactam compound represented by the general formula (1) is reacted with an organotin compound represented by the general formula (2) in the presence of a monovalent copper salt ##STR1## wherein R.sup.1 is a hydrogen atom, halogen atom, amino or protected amino, R.sup.2 is a hydrogen atom, halogen atom, lower alkoxyl, lower acyl, lower alkyl, lower alkyl having hydroxyl or protected hydroxyl as a substituent, hydroxyl or protected hydroxyl, or R.sup.1 and R.sup.2 form=0 when taken together, R.sup.3 is a hydrogen atom or carboxylic acid protecting group, R.sup.4 is aryl, aryl having a substituent, nitrogen-containing aromatic heterocyclic group or nitrogen-containing aromatic heterocyclic group having a substituent, and m is 0 or 2,(R.sup.5).sub.n --Sn(R.sup.6).sub.4--n (2)wherein R.sup.5 is alkenyl, alkenyl having a substituent, aryl, aryl having a substituent, nitrogen-containing aromatic heterocyclic group or nitrogen-containing aromatic heterocyclic group having a substituent, R.sup.6 is lower alkyl, and n is 1 or 2, ##STR2## wherein R.sup.1, R.sup.2, R.sup.3 and R.sup.5 are the same as defined above.
摘要翻译： PCT No.PCT / JP93 / 01041 Sec。 371日期：1994年3月22日 102（e）1994年3月22日PCT 1993年7月26日PCT公布。出版物WO94 / 02490 日期：1994年2月3日本发明提供一种制备由通式（3）表示的头孢烯化合物的方法，其特征在于，将由通式（1）表示的丙烯酰基-β-内酰胺化合物与由在一价铜盐（1）的存在下通式（2）其中R1是氢原子，卤素原子，氨基或被保护的氨基，R2是氢原子，卤素原子，低级烷氧基，低级酰基，低级烷基，具有羟基或被保护的羟基作为取代基的低级烷基，羟基或保护的羟基，或者R 1和R 2形成= 0，当R 3是氢原子或羧酸保护基时，R 4是芳基，具有取代基的芳基，具有取代基的含氮芳香族杂环基或含氮芳香族杂环基，m为0或2，（R5）n-Sn（R6）4-n（2）其中R5为烯基，具有取代基的烯基，，具有取代基的芳基，氮 - 具有取代基的芳族杂环基或含氮芳族杂环基，R6是低级烷基，n是1或2，其中R1，R2，R3和R5与上述定义相同。

58. 发明授权

US5656755A Process for preparation on 3-substituted cephem compound 失效
标题翻译： 3-取代头孢烯化合物的制备方法
公开(公告)号：US5656755A
公开(公告)日：1997-08-12
申请号：US464853
申请日：1995-07-06
申请人： Shigeru Torii , Hideo Tanaka , Michio Sasaoka , Takashi Shiroi
发明人： Shigeru Torii , Hideo Tanaka , Michio Sasaoka , Takashi Shiroi
IPC分类号： B01J21/02 , B01J31/12 , C07B61/00 , C07D501/00 , C07D501/08 , C07D501/22 , C07D501/36
CPC分类号： C07D501/00 , Y02P20/55
摘要： An object of the invention is to provide a process for preparing a 3-substituted cephem compound from an allenyl-.beta.-lactam compound which can be easily produced from an inexpensive penicillin compound by a simple reaction procedure.The process of the invention comprises reacting an allenyl-.beta.-lactam compound with an organohalogen compound in the presence of a metal having a standard oxidation-reduction potential of -0.3 (V/SCE) or less in an amount at least equimolar with the allenyl-.beta.-lactam compound and 0.0001 to 0.5 mole, per mole of the allenyl-.beta.-lactam compound, of a metal compound having a higher standard oxidation-reduction potential than said metal.
摘要翻译： PCT No.PCT / JP94 / 01859 Sec。 371日期：1995年7月6日 102（e）日期1995年7月6日PCT 1994年11月4日PCT PCT。第WO95 / 13281号公报日期1995年5月18日本发明的目的是提供一种由丙烯烯基-β-内酰胺化合物制备3-取代的头孢烯化合物的方法，其可以通过简单的反应方法由便宜的青霉素化合物制备。本发明的方法包括在具有-0.3（V / SCE）或更小的标准氧化还原电位的金属的存在下，将烯丙基-β-内酰胺化合物与有机卤素化合物反应，其量与至少等摩尔的烯丙基 -β-内酰胺化合物和0.0001至0.5摩尔/摩尔的烯丙基-β-内酰胺化合物，具有比所述金属更高的标准氧化还原电位的金属化合物。

59. 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.

60. 发明授权

US5919924A Process for preparing 3-halogenated cephem derivative 失效
标题翻译： 3-卤代头孢烯衍生物的制备方法
公开(公告)号：US5919924A
公开(公告)日：1999-07-06
申请号：US849393
申请日：1997-06-03
申请人： Michio Sasaoka , Shigeru Torii , Hideo Tanaka , Ryo Kikuchi , Yutaka Kameyama , Kouichi Sorajo
发明人： Michio Sasaoka , Shigeru Torii , Hideo Tanaka , Ryo Kikuchi , Yutaka Kameyama , Kouichi Sorajo
IPC分类号： A61K31/545 , A61K31/546 , A61P31/04 , B01J27/055 , B01J27/122 , B01J31/20 , C07B61/00 , C07D501/00 , C07D501/08 , C07D501/18 , C07D501/59
CPC分类号： C07D501/00 , Y02P20/55
摘要： A process for preparing a 3-halogenated cephem derivative represented by the formula (2), characterized by causing a halogenating reagent to act on an allenyl .beta.-lactam compound represented by the formula (1) in the presence of a cuprous salt or cupric salt to obtain the 3-halogenated cephem derivative ##STR1## wherein R.sup.1 is a hydrogen atom, amino or protected amino, R.sup.2 is a hydrogen atom, halogen atom, lower alkoxyl, lower acyl, lower alkyl, lower alkyl having at least one selected from hydroxyl and protected hydroxyl as a substituent, hydroxyl or protected hydroxyl, R.sup.3 is a hydrogen atom or carboxylic acid protecting group, R.sup.4 is an aromatic compound residue which may have a substituent or nitrogen-containing aromatic heterocyclic compound residue which may have a substituent, and n is 0 to 2 ##STR2## wherein R.sup.1, R.sup.2 and R.sup.3 are as defined above, X is a halogen atom.
摘要翻译： PCT No.PCT / JP96 / 03298 Sec。 371日期：1997年6月3日 102（e）日期1997年6月3日PCT 1996年11月8日PCT公布。第WO97 / 17353号公报日期：1997年5月5日制备式（2）表示的3-卤代头孢烯衍生物的方法，其特征在于，使卤化剂作用于由式（1）表示的丙烯酰基β-内酰胺化合物，盐或铜盐，得到其中R 1为氢原子，氨基或被保护的氨基，R 2为氢原子，卤素原子，低级烷氧基，低级酰基，低级烷基，具有选自以下的至少一种的低级烷基的3-卤代头孢烯衍生物羟基和保护的羟基作为取代基，羟基或被保护的羟基，R3是氢原子或羧酸保护基，R4是可以具有取代基的芳族化合物残基或可以具有取代基的含氮芳族杂环化合物残基，以及 n为0〜2，其中R1，R2和R3如上所定义，X为卤素原子。

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