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1. 发明授权

US06887992B2 3-cephem derivative crystal 失效
标题翻译： 3-头孢烯衍生物晶体
公开(公告)号：US06887992B2
公开(公告)日：2005-05-03
申请号：US10679451
申请日：2003-10-07
申请人： Takashi Moriyoshi , Yasuhiro Uosaki , Yutaka Kameyama , Daisuke Suzuki , Yoshiko Seo
发明人： Takashi Moriyoshi , Yasuhiro Uosaki , Yutaka Kameyama , Daisuke Suzuki , Yoshiko Seo
IPC分类号： C07D501/00 , C07D501/12 , C07D501/24 , C07D501/30
CPC分类号： C07D501/00 , Y02P20/544
摘要： A 3-cephem derivative crystal which is a clathrate compound comprising p-methoxybenzyl ester of 7-phenylacetamide-3-formyl-3-cephem-4-carboxylic acid and dimethylformamide and a process for preparing the 3-cephem derivative crystal.
摘要翻译：作为包含7-苯基乙酰胺-3-甲酰基-3-头孢烯-4-羧酸和二甲基甲酰胺的对甲氧基苄基酯的包合物化合物的3-头孢烯衍生物结晶和制备3-头孢烯衍生物结晶的方法。

2. 发明授权

US6011151A Process for preparing .beta.-lactam halide compound 失效
标题翻译：制备β-内酰胺卤化物的方法
公开(公告)号：US6011151A
公开(公告)日：2000-01-04
申请号：US732444
申请日：1996-11-06
申请人： Sigeru Torii , Hideo Tanaka , Michio Sasaoka , Yutaka Kameyama , Daisuke Suzuki
发明人： Sigeru Torii , Hideo Tanaka , Michio Sasaoka , Yutaka Kameyama , Daisuke Suzuki
IPC分类号： C07D205/08 , C07D205/085 , C07D205/09 , C07D205/095
CPC分类号： C07D205/08 , C07D205/085 , C07D205/09 , C07D205/095 , Y02P20/55
摘要： A process for preparing a .beta.-lactam halide compound represented by the formula (2) characterized by halogenating the allenyl group of an allenyl .beta.-lactam compound represented by the formula (1) with a cupric halide and a metal halide to obtain the .beta.-lactam halide compound ##STR1## wherein R.sup.1 is a hydrogen atom or amino or protected amino, R.sup.2 is a hydrogen atom, halogen atom, lower alkoxyl, lower acyl, or lower alkyl having a hydroxyl group or protected hydroxyl group as a substituent, R.sup.3 is a hydrogen atom or carboxylic acid protecting group, and R.sup.4 is a hydrocarbon group which may have a substituent, or the group --S--S(O)n-Ar, n being 0 to 2, Ar being aryl which may have a substituent ##STR2## wherein R.sup.1, R.sup.2, R.sup.3 and R.sup.4 are the same as defined above, X and Y are each halogen atom.
摘要翻译： PCT No.PCT / JP96 / 00489 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1日PCT公布。 WO96 / 28421 PCT出版物日本1996年9月19日制备式（2）表示的β-内酰胺化合物化合物的制备方法，其特征在于用卤化铜和金属卤化物卤化由式（1）表示的烯丙基β-内酰胺化合物的全烯基得到其中R1为氢原子或氨基或被保护的氨基，R2为氢原子，卤素原子，低级烷氧基，低级酰基或具有羟基或被保护的羟基作为取代基的低级烷基的β-内酰胺化合物， R3为氢原子或羧酸保护基，R4为可具有取代基的烃基，或-SS（O）n-Ar，n为0〜2，Ar为可具有取代基的芳基， R1，R2，R3和R4与上述定义相同，X和Y各自为卤素原子。

3. 发明授权

US07692003B2 Penicillin crystals and process for producing the same 失效
标题翻译：青霉素晶体及其生产方法
公开(公告)号：US07692003B2
公开(公告)日：2010-04-06
申请号：US10574278
申请日：2004-10-08
申请人： Isao Wada , Yutaka Kameyama
发明人： Isao Wada , Yutaka Kameyama
IPC分类号： C07D477/14
CPC分类号： C07D499/86
摘要： The present invention provides 2β-chloromethyl-2α-methylpenam-3α-carboxylic acid benzhydryl ester (CMPB) crystals of excellent stability, and a process for producing the CMPB crystals comprising the steps of (A) concentrating a solution containing CMPB; (b) subjecting the thus-obtained concentrate to column chromatography; (C) concentrating a CMPB-containing fraction; and (D) dissolving the thus-obtained CMPB-containing concentrate in an ether solvent and adding a hydrocarbon solvent to the resulting solution to precipitate CMPB crystals.
摘要翻译：本发明提供了具有优异稳定性的2'-溴甲基-2α-甲基丙烯酰胺-3α-羧酸二苯甲基酯（CMPB）晶体，以及制备CMPB晶体的方法，包括以下步骤：（A）浓缩含有CMPB的溶液; （b）将由此得到的浓缩物进行柱色谱; （C）浓缩含CMPB的级分; 和（D）将由此获得的含CMPB的浓缩物溶解在醚溶剂中并向所得溶液中加入烃溶剂以沉淀CMPB晶体。

4. 发明授权

US07183421B2 Processes for producing oxide with higher oxidation than alcohol 失效
标题翻译：生产氧化比醇高的氧化物的方法
公开(公告)号：US07183421B2
公开(公告)日：2007-02-27
申请号：US10915600
申请日：2004-08-11
申请人： Hideo Tanaka , Yutaka Kameyama
发明人： Hideo Tanaka , Yutaka Kameyama
IPC分类号： C07D309/00 , C07D407/00 , C07C67/00 , C07C51/16 , C07C45/00
CPC分类号： C25B3/02 , C07B41/00 , C07C45/29 , C07C45/294 , C07C45/30 , C07C67/40 , C07C69/716
摘要： The present invention provides a process for producing an oxide from an alcohol compound, the process comprising the steps of causing silica gel to carry the alcohol compound thereon and an oxidative catalyst thereon, and oxidizing the alcohol compound in the presence of an oxidizing agent, giving an oxide higher in oxidizing degree than the alcohol compound, and also provides a process for producing an oxide from an alcohol compound, the process comprising the steps of causing silica gel to carry the alcohol compound, and subjecting the alcohol compound to an electrolytic oxidation, giving an oxide higher in oxidizing degree than the alcohol compound.
摘要翻译：本发明提供一种由醇化合物制备氧化物的方法，该方法包括以下步骤：使硅胶在其上载有醇化合物及其上的氧化催化剂，并在氧化剂存在下氧化醇化合物，得到氧化度高于醇化合物的氧化物，还提供了由醇化合物制造氧化物的方法，该方法包括使硅胶携带醇化合物，并对醇化合物进行电解氧化，产生氧化度高于醇化合物的氧化物。

5. 发明授权

US06576761B1 Process for the preparation of cephem compounds 有权
标题翻译：头孢烯化合物的制备方法
公开(公告)号：US06576761B1
公开(公告)日：2003-06-10
申请号：US10049048
申请日：2002-02-07
申请人： Hideo Tanaka , Yutaka Kameyama
发明人： Hideo Tanaka , Yutaka Kameyama
IPC分类号： C07D50122
CPC分类号： C07D501/00 , Y02P20/55
摘要： 1. A process for preparing a 3-alkenylcephem compound or 3-norcephem compound of the formula (3) characterized in that an alkenyl halide of the formula (2), a nickel catalyst, a metal up to −0.3 (V/SCE) in standard oxidation reduction potential and a compound of a metal having a higher standard oxidation reduction potential than the metal are caused to act on a 3-cephem compound of the formula (1) in a solvent wherein R1 is a hydrogen atom or the like, R2 is a hydrogen atom or the like, R3 is a hydrogen atom or carboxylic acid protective group, and X is a halogen atom or the like, R4—Y (2) wherein R4 is 1-alkenyl having or not having a substituent, and Y is a halogen atom wherein R1, R2 and R3 are as defined above, and R5 is a hydrogen atom or 1-alkenyl having or not having a substituent.
摘要翻译： 1.一种制备式（3）的3-链烯基头孢烯化合物或3-诺卡波姆化合物的方法，其特征在于式（2）的烯基卤，镍催化剂，高达-0.3（V / SCE）在标准氧化还原电位和具有比金属更高的标准氧化还原电位的金属的化合物在R1是氢原子等的溶剂中作用于式（1）的3-头孢烯化合物时，R2 是氢原子等，R 3为氢原子或羧酸保护基，X为卤素原子等，其中，R 4为具有或不具有取代基的1-烯基，Y为卤素原子，R1， R2和R3如上定义，R5是氢原子或具有或不具有取代基的1-烯基。

6. 发明授权

US06420554B1 Process for preparation of 3-cephem compound 有权
标题翻译： 3-头孢烯化合物的制备方法
公开(公告)号：US06420554B1
公开(公告)日：2002-07-16
申请号：US09485712
申请日：2000-02-29
申请人： Yutaka Kameyama , Takae Yamada , Dal Soo Suh
发明人： Yutaka Kameyama , Takae Yamada , Dal Soo Suh
IPC分类号： C07D50104
CPC分类号： C07D501/00
摘要： A process for preparing a 3-cephem compound represented by the formula (3), the process comprising the steps of reacting a &bgr;-lactam compound represented by the formula (1) with a phosphorus halide compound in the presence of an organic base to give an imino-&bgr;-lactam compound represented by the formula (2), adding a phenol to the same reaction system to cause decomposition due to reaction with an alcohol and simultaneously to remove the protection of carboxylic acid ester, giving a 3-cephem compound represented by the formula (3) or a salt thereof where R1, R2, R3 and X are as defined above.
摘要翻译：一种制备由式（3）表示的3-头孢烯化合物的方法，该方法包括以下步骤：在有机碱的存在下使由式（1）表示的β-内酰胺化合物与卤化磷化合物反应，得到由式（2）表示的亚氨基-β-内酰胺化合物，在相同的反应体系中加入苯酚以引起与醇反应引起的分解，同时除去羧酸酯的保护，得到3-头孢烯化合物通式（3）表示的化合物或其盐，其中R 1，R 2，R 3和X如上所定义。

7. 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。

8. 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。

9. 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。

10. 发明授权

US07893254B2 Process for production of 3-alkenylcephem compounds 有权
标题翻译： 3-链烯基化合物的制备方法
公开(公告)号：US07893254B2
公开(公告)日：2011-02-22
申请号：US11628248
申请日：2005-06-03
申请人： Yoichi Nishioka , Masahiro Ito , Yutaka Kameyama
发明人： Yoichi Nishioka , Masahiro Ito , Yutaka Kameyama
IPC分类号： C07D501/24 , C07D501/12
CPC分类号： C07D501/00
摘要： A process for preparing 7-amino-3-[(E/Z)-2-(4-methylthiazol-5-yl)vinyl]-3-cephem-4-carboxylic acid of the formula (1) and an alkali metal salt thereof, said acid and said salt being improved in the content of 7-amino-3-[(Z)-2-(4-methylthiazol-5-yl)vinyl]-3-cephem-4-carboxylic acid of the formula (2) or an alkali metal salt thereof, the process being characterized in that an aqueous solution of an alkali metal salt of 7-amino-3-[(E/Z)-2-(4-methylthiazol-5-yl)vinyl]-3-cephem-4-carboxylic acid of the formula (1) is treated with a high porous polymer and/or active carbon as added thereto.
摘要翻译：制备式（1）的7-氨基-3 - [（E / Z）-2-（4-甲基噻唑-5-基）乙烯基] -3-头孢烯-4-羧酸和碱金属盐所述酸和所述盐的结构改善了式（7）的7-氨基-3 - [（Z）-2-（4-甲基噻唑-5-基）乙烯基] -3-头孢烯-4-羧酸的含量 2）或其碱金属盐，该方法的特征在于将7-氨基-3 - [（E / Z）-2-（4-甲基噻唑-5-基）乙烯基] 式（1）的3-头孢烯-4-羧酸用加入其中的高多孔聚合物和/或活性炭进行处理。

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