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1. 发明授权

US5688942A Process for preparing 2-isocephem derivatives 失效
标题翻译：制备2-异头孢烯衍生物的方法
公开(公告)号：US5688942A
公开(公告)日：1997-11-18
申请号：US732446
申请日：1996-11-06
申请人： Michio Sasaoka , Daisuke Suzuki , Delsoo Suh , Yoshihisa Tokumaru
发明人： Michio Sasaoka , Daisuke Suzuki , Delsoo Suh , Yoshihisa Tokumaru
IPC分类号： C07D513/04 , A61K31/54 , A61P31/04 , C07D205/08 , C07D498/04 , C07D501/00 , C07D507/08
CPC分类号： C07D205/08 , C07D501/00 , Y02P20/55
摘要： A process for preparing a 2-isocephem derivative characterized in that a thioacetic acid derivative which itself is basic or a mixture of a base and a thioacetic acid derivative is caused to act on a 2-azetidinyl-3,4-dihalogeno-2-butenoic acid compound represented by the general formula (1) in a water-containing organic solvent to obtain a 3-halomethyl-2-isocephem derivative represented by the general formula (2), and a process for preparing a 2-oxaisocephem derivative characterized in that a base is caused to act on a 2-azetidinyl-3,4-dihalogeno-2-butenoic acid compound represented by the general formula (1) in a water-containing organic solvent to obtain a 3-halomethyl-2-oxaisocephem derivative represented by the general formula (3) ##STR1## wherein R.sup.1 is a hydrogen atom, amino or protected amino, R.sup.2 is a hydrogen atom or lower alkoxyl, R.sup.1 and R.sup.2, when taken together, form a cyclic amino protecting group, R.sup.3 is a hydrogen atom or carboxylic acid protecting group, W is a leaving group, and X and Y are the same or different and are each a halogen atom ##STR2## wherein R.sup.1, R.sup.2, R.sup.3 and X are the same as above, ##STR3## wherein R.sup.1, R.sup.2, R.sup.3 and X are the same as above.
摘要翻译： PCT No.PCT / JP96 / 00538 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6日PCT公布。公开号WO96 / 28453 日期1996年9月19日制备2-异头孢烯衍生物的方法，其特征在于使本身为碱性的硫代乙酸衍生物或碱和硫代乙酸衍生物的混合物作用于2-氮杂环丁烷基-3,4- 由通式（1）表示的二卤代-2-丁烯酸化合物在含水有机溶剂中得到由通式（2）表示的3-卤代甲基-2-异头孢烯衍生物，以及制备2- 恶唑磺酸衍生物，其特征在于使碱在含水有机溶剂中作用于由通式（1）表示的2-氮杂环丁烷基-3,4-二卤代-2-丁烯酸化合物，得到3-卤代甲基 - 由通式（3）表示的2-氧代硫代衍生物无或被保护的氨基，R2是氢原子或低级烷氧基，R1和R2一起形成环状氨基保护基，R3是氢原子或羧酸保护基组，W是离职小组，X和Y是sam e或不同，各自为卤素原子，其中R1，R2，R3和X与上述相同，其中R1，R2，R3和X与上述相同。

2. 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

3. 发明授权

US07547777B2 Penam crystals and process for producing the same 失效
标题翻译： Penam晶体及其制造方法
公开(公告)号：US07547777B2
公开(公告)日：2009-06-16
申请号：US10574279
申请日：2004-10-08
申请人： Yoshihisa Tokumaru , Akihiro Shimabayashi
发明人： Yoshihisa Tokumaru , Akihiro Shimabayashi
IPC分类号： C07D499/00 , C07D499/04
CPC分类号： C07D499/86
摘要： The present invention provides novel 2α-methyl-2β-[(1,2,3-triazol-1-yl)methyl]penam-3α-carboxylic acid benzhydryl ester (TMPB)-acetone crystals for use in the production of 2α-methyl-2β-[(1,2,3-triazol-1-yl)methyl]penam-3α-carboxylic acid 1,1-dioxide benzhydryl ester (TAZB); a process for producing the TMPB-acetone crystals comprising the steps of (A) concentrating a TMPB-containing organic solvent solution, (B) dissolving the resulting concentrate in acetone, and (C) precipitating TMPB-acetone crystals from the acetone solution thus obtained; and a process for producing TAZB comprising the step of reacting the TMPB-acetone crystals with an oxidizing agent.
摘要翻译：本发明提供了用于生产2α-甲基的新的2α-甲基-2a- [（1,2,3-三唑-1-基）甲基]双 - 三羧酸二甲酯（TMPB） - 丙酮晶体 -2β-[（1,2,3-三唑-1-基）甲基] penam-3α-羧酸1,1-二氧化二苯甲酸酯（TAZB）; 制备TMPB-丙酮晶体的方法包括以下步骤：（A）浓缩含TMPB的有机溶剂溶液，（B）将所得浓缩物溶于丙酮中，和（C）从所得丙酮溶液中沉淀TMPB-丙酮晶体 ; 以及制备TAZB的方法，其包括使TMPB-丙酮晶体与氧化剂反应的步骤。

4. 发明授权

US07514553B2 Process for producing penicillanic acid compound 有权
标题翻译：生产青霉烷酸化合物的方法
公开(公告)号：US07514553B2
公开(公告)日：2009-04-07
申请号：US10569692
申请日：2004-09-02
申请人： Yoshihisa Tokumaru , Norio Saito , Makoto Akizuki
发明人： Yoshihisa Tokumaru , Norio Saito , Makoto Akizuki
IPC分类号： C07D477/06
CPC分类号： C07D499/04 , Y02P20/55
摘要： A process for preparing a penicillanic acid compound of the formula (2) comprising reacting a halogenated penicillanic acid compound of the formula (1), (a) in the presence of a metal bismuth or bismuth compound, (b) with a metal having a lower standard oxidation-reduction potential than bismuth to obtain the compound (2) (X and Y are a hydrogen atom or halogen atom, provided that X and Y are not hydrogen atoms at the same time, n is an integer of 0 to 2, R is carboxylic acid protecting group) (n and R are same as above).
摘要翻译：一种制备式（2）的青霉烷酸化合物的方法，包括使式（1）的卤代青霉烷酸化合物，（a）在金属铋或铋化合物存在下，（b）与具有比铋更低的标准氧化还原电位以获得化合物（2）（X和Y是氢原子或卤素原子，条件是X和Y不同时为氢原子，n为0-2的整数， R是羧酸保护基）（n和R与上述相同）。

5. 发明申请

US20070060559A1 Penam crystals and process for producing the same 失效
标题翻译： Penam晶体及其制造方法
公开(公告)号：US20070060559A1
公开(公告)日：2007-03-15
申请号：US10574279
申请日：2004-10-08
申请人： Yoshihisa Tokumaru , Akihiro Shimabayashi
发明人： Yoshihisa Tokumaru , Akihiro Shimabayashi
IPC分类号： A61K31/43 , C07D499/00
CPC分类号： C07D499/86
摘要： The present invention provides novel 2α-methyl-2β-[(1,2,3-triazol-1-yl)methyl]penam-3α-carboxylic acid benzhydryl ester (TMPB)-acetone crystals for use in the production of 2α-methyl-2β-[(1,2,3-triazol-1-yl)methyl]penam-3α-carboxylic acid 1,1-dioxide benzhydryl ester (TAZB); a process for producing the TMPB-acetone crystals comprising the steps of (A) concentrating a TMPB-containing organic solvent solution, (B) dissolving the resulting concentrate in acetone, and (C) precipitating TMPB-acetone crystals from the acetone solution thus obtained; and a process for producing TAZB comprising the step of reacting the TMPB-acetone crystals with an oxidizing agent.
摘要翻译：本发明提供了用于生产2α-甲基的新的2α-甲基-2a- [（1,2,3-三唑-1-基）甲基]双 - 三羧酸二甲酯（TMPB） - 丙酮晶体 -2β-[（1,2,3-三唑-1-基）甲基] penam-3α-羧酸1,1-二氧化二苯甲酸酯（TAZB）; 制备TMPB-丙酮晶体的方法包括以下步骤：（A）浓缩含TMPB的有机溶剂溶液，（B）将所得浓缩物溶于丙酮中，和（C）从所得丙酮溶液中沉淀TMPB-丙酮晶体 ; 以及制备TAZB的方法，其包括使TMPB-丙酮晶体与氧化剂反应的步骤。

6. 发明申请

US20060281917A1 Process for producing penicillanic acid compound 有权
公开(公告)号：US20060281917A1
公开(公告)日：2006-12-14
申请号：US10569692
申请日：2004-09-02
申请人： Yoshihisa Tokumaru , Norio Saito , Makoto Akizuki
发明人： Yoshihisa Tokumaru , Norio Saito , Makoto Akizuki
IPC分类号： C07D499/04
CPC分类号： C07D499/04 , Y02P20/55
摘要： A process for preparing a penicillanic acid compound of the formula (2) comprising reacting a halogenated penicillanic acid compound of the formula (1), (a) in the presence of a metal bismuth or bismuth compound, (b) with a metal having a lower standard oxidation-reduction potential than bismuth to obtain the compound (2) (X and Y are a hydrogen atom or halogen atom, provided that X and Y are not hydrogen atoms at the same time, n is an integer of 0 to 2, R is carboxylic acid protecting group) (n and R are same as above).

7. 发明授权

US07714125B2 Process for producing penam compound useful for preparing tazobactam 有权
标题翻译：制备可用于制备他唑巴坦的penam化合物的方法
公开(公告)号：US07714125B2
公开(公告)日：2010-05-11
申请号：US11665006
申请日：2005-10-25
申请人： Isao Wada , Yoshihisa Tokumaru , Akihiro Shimabayashi
发明人： Isao Wada , Yoshihisa Tokumaru , Akihiro Shimabayashi
IPC分类号： C07D499/04
CPC分类号： C07D499/00
摘要： An object of the invention is to provide an industrially advantageous process capable of remarkably suppressing the generation of an undesirable by-product cepham compound to thereby efficiently produce a desired 2α-methyl-2β-[(1,2,3-triazol-1-yl)methyl]penam-3α-carboxylic acid ester. In the present invention, a diphenylmethyl 2β-bromomethyl-2α-methylpenam-3α-carboxylate (BMPB) is reacted with 1,2,3-triazole in a halogenated hydrocarbon solvent at −5° C. or lower. The reaction in a halogenated hydrocarbon solvent at −5° C. or less can remarkably suppress the generation of an undesirable by-product cepham compound, so that the desired diphenylmethyl 2α-methyl-2β-[(1,2,3-triazol-1-yl)methyl]penam-3α-carboxylate (TMPB) can be efficiently produced.
摘要翻译：本发明的目的是提供一种工业上有利的方法，该方法能够显着抑制不期望的副产物头孢烯化合物的产生，从而有效地产生所需的2α-甲基-2' - [（1,2,3-三唑-1-基） - 基）甲基] penam-3α-羧酸酯。在本发明中，在-5℃或更低的卤代烃溶剂中使二苯基甲基2'-溴甲基-2α-甲基青蒿素-3α-羧酸酯（BMPB）与1,2,3-三唑反应。在-5℃或更低的卤代烃溶剂中的反应可以显着地抑制不期望的副产物头孢烯化合物的产生，从而使所需的二苯基甲基2α-甲基-2' - [（1,2,3-三唑） -1-基）甲基] penam-3α-羧酸酯（TMPB）。

8. 发明申请

US20090012287A1 Process for Producing Penam Compound 有权
标题翻译：生产Penam化合物的方法
公开(公告)号：US20090012287A1
公开(公告)日：2009-01-08
申请号：US11665006
申请日：2005-10-25
申请人： Isao Wada , Yoshihisa Tokumaru , Akihiro Shimabayashi
发明人： Isao Wada , Yoshihisa Tokumaru , Akihiro Shimabayashi
IPC分类号： C07D499/04
CPC分类号： C07D499/00
摘要： An object of the invention is to provide an industrially advantageous process capable of remarkably suppressing the generation of an undesirable by-product cepham compound to thereby efficiently produce a desired 2α-methyl-2β-[(1,2,3-triazol-1-yl)methyl]penam-3α-carboxylic acid ester. In the present invention, a diphenylmethyl 2β-bromomethyl-2α-methylpenam-3α-carboxylate (BMPB) is reacted with 1,2,3-triazole in a halogenated hydrocarbon solvent at −5° C. or lower. The reaction in a halogenated hydrocarbon solvent at −5° C. or less can remarkably suppress the generation of an undesirable by-product cepham compound, so that the desired diphenylmethyl 2α-methyl-2β-[(1,2,3-triazol-1-yl)methyl]penam-3α-carboxylate (TMPB) can be efficiently produced.
摘要翻译：本发明的目的是提供一种工业上有利的方法，该方法能够显着地抑制不期望的副产物头孢烯化合物的产生，从而有效地产生所需的2α-甲基-2aeta - [（1,2,3-三唑-1-基）吡啶-3-基）甲基] penam-3α-羧酸酯。在本发明中，在-5℃或更低的卤代烃溶剂中使二苯基甲基2ba-溴甲基-2α-甲基青蒿素-3α-羧酸酯（BMPB）与1,2,3-三唑反应。在-5℃或更低的卤代烃溶剂中的反应可以显着地抑制不合需要的副产物头孢烯化合物的产生，使得所需的二甲基二甲基-2α-甲基-2β-[（1,2,3-三唑-2-基）（TMPB））可以有效地制备。

9. 发明授权

US6063918A Process for preparing 2-isocephem derivatives 失效
标题翻译：制备2-异头孢烯衍生物的方法
公开(公告)号：US6063918A
公开(公告)日：2000-05-16
申请号：US889048
申请日：1997-07-07
申请人： Michio Sasaoka , Daisuke Suzuki , Delsoo Suh , Yoshihisa Tokumaru
发明人： Michio Sasaoka , Daisuke Suzuki , Delsoo Suh , Yoshihisa Tokumaru
IPC分类号： C07D513/04 , A61K31/54 , A61P31/04 , C07D205/08 , C07D498/04 , C07D501/00 , C07D507/08
CPC分类号： C07D205/08 , C07D501/00 , Y02P20/55
摘要： A process for preparing a 2-isocephem derivative characterized in that a thioacetic acid derivative which itself is basic or a mixture of a base and a thioacetic acid derivative is caused to act on a 2-azetidinyl-3,4-dihalogeno-2-butenoic acid compound represented by the general formula (1) in a water-containing organic solvent to obtain a 3-halomethyl-2-isocephem derivative represented by the general formula (2), and a process for preparing a 2-oxaisocephem derivative characterized in that a base is caused to act on a 2-azetidinyl-3,4-dihalogeno-2-butenoic acid compound represented by the general formula (1) in a water-containing organic solvent to obtain a 3-halomethyl-2-oxaisocephem derivative represented by the general formula (3) ##STR1## wherein R.sup.1 is a hydrogen atom, amino or protected amino, R.sup.2 is a hydrogen atom or lower alkoxyl, R.sup.1 and R.sup.2, when taken together, form a cyclic amino protecting group, R.sup.3 is a hydrogen atom or carboxylic acid protecting group, W is a leaving group, and X and Y are the same or different and are each a halogen atom.
摘要翻译：制备2-异头孢烯衍生物的方法，其特征在于使本身为碱性的硫代乙酸衍生物或碱和硫代乙酸衍生物的混合物作用于2-氮杂环丁烷基-3,4-二卤代-2-丁烯酸在含水有机溶剂中由通式（1）表示的酸化合物，得到由通式（2）表示的3-卤代甲基-2-异头孢烯衍生物及其制备方法，其特征在于，在含水有机溶剂中使碱作用于由通式（1）表示的2-氮杂环丁烷基-3,4-二卤代-2-丁烯酸化合物，得到3-卤代甲基-2-氧代硫代衍生物通式（3）其中R 1为氢原子，氨基或被保护的氨基，R 2为氢原子或低级烷氧基，R 1和R 2一起形成环状氨基保护基，R 3为氢原子或羧酸酸保护基，W是离去基团，X a nd Y相同或不同，各自为卤素原子。

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