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1. 发明授权

US5587474A Method for removing the protecting group for carboxyl group 失效
标题翻译：去除羧基保护基的方法
公开(公告)号：US5587474A
公开(公告)日：1996-12-24
申请号：US77383
申请日：1993-06-17
申请人： Kazuhiko Kondo , Hiroshi Horikawa , Tameo Iwasaki
发明人： Kazuhiko Kondo , Hiroshi Horikawa , Tameo Iwasaki
IPC分类号： C07D463/00 , C07D477/08 , C07D499/88 , C07D501/00 , C07D503/00 , C07D505/00 , C07D403/12
CPC分类号： C07D501/00 , C07D463/06 , C07D477/08 , C07D499/88 , C07D503/00 , C07D505/00 , Y02P20/55
摘要： A method for removing substituted or unsubstituted allyl group from .beta.-lactam compound having substituted or unsubstituted allyl group-protecting carboxyl group, which comprises treating said .beta.-lactam compound with palladium catalyst in the presence of allyl-scavenger in aqueous organic solvent, by which the substituted or unsubstituted group can be easily and effectively removed under moderate conditions so that the desired compound can be obtained in high yield at low cost.
摘要翻译：一种从具有取代或未取代的烯丙基保护羧基的β-内酰胺化合物中除去取代或未取代的烯丙基的方法，该方法包括在含有机溶剂的烯丙基清除剂存在下用钯催化剂处理所述β-内酰胺化合物，取代或未取代的基团可以在中等条件下容易且有效地除去，从而可以低成本高收率地获得所需化合物。

2. 发明授权

US5153187A 1-Methylcarbapenem derivatives and process for preparation thereof 失效
标题翻译： 1-甲基胆碱衍生物及其制备方法
公开(公告)号：US5153187A
公开(公告)日：1992-10-06
申请号：US755884
申请日：1991-09-06
申请人： Tameo Iwasaki , Kazuhiko Kondo , Hiroshi Horikawa , Totaro Yamaguchi , Tadahiro Matsushita
发明人： Tameo Iwasaki , Kazuhiko Kondo , Hiroshi Horikawa , Totaro Yamaguchi , Tadahiro Matsushita
IPC分类号： A61K31/40 , A61K31/397 , A61P31/04 , C07D207/24 , C07D477/00 , C07D477/20
CPC分类号： C07D477/20 , Y02P20/55
摘要： 1-Methylcarbapenem derivatives of the formula: ##STR1## wherein R.sup.1 is hydrogen atom or a hydroxy-protecting group, R.sup.2 is hydrogen atom or an ester residue, R.sup.3 is hydrogen atom or a lower alkyl group, or salts thereof, which have excellent antimicrobial activities and are useful as an antimicrobial drug.

3. 发明授权

US5414081A Process for preparing .beta.-lactam derivative and synthetic intermediate thereof 失效
标题翻译：制备β-内酰胺衍生物及其合成中间体的方法
公开(公告)号：US5414081A
公开(公告)日：1995-05-09
申请号：US18407
申请日：1993-02-17
申请人： Hiroshi Horikawa , Kazuhiko Kondo , Tameo Iwasaki
发明人： Hiroshi Horikawa , Kazuhiko Kondo , Tameo Iwasaki
IPC分类号： C07D463/00 , C07D477/00 , C07D477/02 , C07D477/04 , C07D499/06 , C07D499/88 , C07D499/893 , C07D499/897 , C07D501/16 , C07D501/18 , C07D503/04 , C07D505/00 , C07D513/04 , C07D515/04 , C07D487/04
CPC分类号： C07D513/04 , C07D477/02 , C07D477/04 , C07D515/04
摘要： Disclosed is a process for preparing a .beta.-lactam compound represented by the formula: ##STR1## wherein R.sup.1 represents a hydroxy-substituted lower alkyl group or an amino group each of which may be protected; R.sup.2 represents hydrogen atom or an ester residue; X represents a methylene group which may be substituted by a lower alkyl group, sulfur atom or a group represented by the formula: --A--CH.sub.2 -- where A represents sulfur atom, oxygen atom or methylene group; and W represents an active ester residue of hydroxyl group, or a salt thereof, which comprises the steps of treating a 1-aza-3-thia-bicycloalkane compound represented by the formula: ##STR2## wherein R.sup.1, R.sup.2 and X have the same meanings as defined above, or a salt thereof with a base in the presence of a desulfurizing agent and then reacting the resulting compound with an active esterifying agent of hydroxyl group.
摘要翻译：公开了一种制备由下式表示的β-内酰胺化合物的方法：低级烷基或各自可被保护的氨基; R2表示氢原子或酯残基; X表示可以被低级烷基，硫原子或由下式表示的基团取代的亚甲基：-A-CH2-，其中A表示硫原子，氧原子或亚甲基; W表示羟基的活性酯残基或其盐，其包括如下步骤：处理由下式表示的1-氮杂-3-硫杂 - 双环烷烃化合物：其中R1，R2和X 具有与上述相同的含义，或其盐与脱碱剂存在下的碱，然后使所得化合物与羟基的活性酯化剂反应。

4. 发明授权

US5359059A Process for preparing carbapenem derivatives 失效
标题翻译：碳青霉烯衍生物的制备方法
公开(公告)号：US5359059A
公开(公告)日：1994-10-25
申请号：US100460
申请日：1993-08-02
申请人： Tameo Iwasaki , Kazuhiko Kondo , Hiroshi Horikawa
发明人： Tameo Iwasaki , Kazuhiko Kondo , Hiroshi Horikawa
IPC分类号： C07D477/00 , C07D477/04 , C07D487/04 , C07D499/00
CPC分类号： C07D477/04
摘要： Process for preparing carbapenem derivative of the formula [I], which comprises subjecting azetidinone compound of the formula [II] to intramolecular cyclization reaction together with elimination reaction of the group of --SR.sup.4, followed by re-adding said group of --SR.sup.4 to the 2-position of the carbapenem skeleton of the intramolecularly cyclized compound, which is industrially useful as process for preparing carbapenem antimicrobials or synthetic intermediate therefor. ##STR1## wherein R.sup.1 is protected or unprotected hydroxy-substituted lower alkyl group, R.sup.2 is hydrogen atom or ester residue, R.sup.3 is hydrogen atom or lower alkyl group, and the group of --SR.sup.4 is group which can be used as substituent at 2-position of the carbapenem antimicrobials.
摘要翻译：制备式[I]的碳青霉烯衍生物的方法，其包括将式[II]的氮杂环丁酮化合物与-SR 4基团的消除反应一起分子内环化反应，然后将所述-SR 4基团重新加入到分子内环化化合物的碳青霉烯骨架的2-位，其在工业上可用作制备碳青霉烯类抗微生物剂或其合成中间体的方法。其中R 1为被保护或未被保护的羟基取代的低级烷基，R 2为氢原子或酯残基，R 3为氢原子或低级烷基，-SR 4为基团其可用作碳青霉烯类抗微生物剂的2-位上的取代基。

5. 发明授权

US5208348A Mercaptan compound 失效
标题翻译：硫醇化合物
公开(公告)号：US5208348A
公开(公告)日：1993-05-04
申请号：US913506
申请日：1992-07-14
申请人： Tameo Iwasaki , Kazuhiko Kondo , Hiroshi Horikawa , Totaro Yamaguchi , Tadahiro Matsushita
发明人： Tameo Iwasaki , Kazuhiko Kondo , Hiroshi Horikawa , Totaro Yamaguchi , Tadahiro Matsushita
IPC分类号： C07D477/20
CPC分类号： C07D477/20
摘要： A mercaptan compound of the formula ##STR1## wherein R.sup.3 is a hydrogen atom or a lower alkyl group, or a salt thereof.
摘要翻译：其中R3是氢原子或低级烷基的式“IMAGE”的硫醇化合物或其盐。

6. 发明授权

US5260438A Method for removing the protecting group for hydroxy group 失效
标题翻译：去除羟基保护基的方法
公开(公告)号：US5260438A
公开(公告)日：1993-11-09
申请号：US52680
申请日：1993-04-27
申请人： Hiroshi Horikawa , Kazuhiko Kondo , Tameo Iwasaki
发明人： Hiroshi Horikawa , Kazuhiko Kondo , Tameo Iwasaki
IPC分类号： C07D205/08 , C07D463/00 , C07D477/02 , C07D499/88 , C07D501/00 , C07D503/00 , C07D505/00 , C07D487/00 , C07D487/04 , C07D487/08 , C07D499/00
CPC分类号： C07D503/00 , C07D205/08 , C07D463/06 , C07D477/02 , C07D499/88 , C07D501/00 , C07D505/00 , Y02P20/55
摘要： A method for removing tri-substituted silyl group from .beta.-lactam compound having a tri-substituted silyl group-protecting hydroxy group, which comprises treating with an acid and a fluoride selected from alkali metal fluoride, alkaline earth metal fluoride and hydrogenfluoride of organic or inorganic amine, by which the tri-substituted silyl group can be easily and effectively removed under moderate conditions so that the desired compound can be obtained in high yield at low cost.
摘要翻译：一种从具有三取代甲硅烷基保护羟基的β-内酰胺化合物中除去三取代甲硅烷基的方法，该方法包括用酸和选自碱金属氟化物，碱土金属氟化物和有机氟化氢的氟化物无机胺，通过其可以在中等条件下容易且有效地除去三取代甲硅烷基，从而可以低成本高收率地获得所需化合物。

7. 发明授权

US5495012A Process for preparing optically active 4-mercapto-2-pyrrolidone derivative and intermediate therefor 失效
标题翻译：光学活性4-巯基-2-吡咯烷酮衍生物及其中间体的制备方法
公开(公告)号：US5495012A
公开(公告)日：1996-02-27
申请号：US409410
申请日：1995-03-24
申请人： Tameo Iwasaki , Kazuhiko Kondo , Tadashi Nakatani , Ryuzo Yoshioka
发明人： Tameo Iwasaki , Kazuhiko Kondo , Tadashi Nakatani , Ryuzo Yoshioka
IPC分类号： C07B57/00 , C07C309/24 , C07C319/28 , C07C323/58 , C07D207/26 , C07D207/273 , C07D477/02 , C07C309/14 , C07C323/25
CPC分类号： C07D207/273 , C07B57/00 , C07C309/24 , C07C319/28 , C07C323/58 , C07D477/02 , Y02P20/55
摘要： A process for preparing an optically active 4-mercapto-2-pyrrolidone derivative of the formula [I]: ##STR1## wherein R.sup.1 is a hydrogen atom or a protecting group and R.sup.2 is a hydrogen atom or a protecting group, which comprises subjecting racemic 4-amino-3-mercaptobutyric acid or a salt thereof to optical resolution by using 1-(trichlorophenyl)ethanesulfonic acid, followed by subjecting the product to cyclization reaction after protecting the functional groups thereof, if necessary, and further optionally removing the protecting groups therefrom. The present process is industrially advantageous than conventional processes for preparing optically active 4-mercapto-2-pyrrolidone derivatives which are useful as an intermediate for various medicines such as carbapenem antibacterial agents.
摘要翻译：制备式[I]的光学活性4-巯基-2-吡咯烷酮衍生物的方法：保护基，R 2是氢原子或保护基，其包括使外消旋的4-氨基-3-巯基丁酸或其盐通过使用1-（三氯苯基）乙磺酸进行光学拆分，随后如果需要，保护其官能团之后使产物进行环化反应，并进一步任选地从其中除去保护基。本方法在工业上比用于制备光学活性的4-巯基-2-吡咯烷酮衍生物的方法是有用的，其可用作各种药物例如碳青霉烯类抗菌剂的中间体。

8. 发明授权

US5442055A Azetidinone compound and process for preparation thereof 失效
标题翻译：氮杂环丁酮化合物及其制备方法
公开(公告)号：US5442055A
公开(公告)日：1995-08-15
申请号：US148917
申请日：1993-11-05
申请人： Tameo Iwasaki , Kazuhiko Kondo
发明人： Tameo Iwasaki , Kazuhiko Kondo
IPC分类号： C07D239/86 , A61K31/397 , A61K31/40 , A61K31/535 , A61K31/536 , A61K31/537 , A61P31/04 , C07D20060101 , C07D205/08 , C07D217/24 , C07D239/88 , C07D265/04 , C07D265/12 , C07D265/20 , C07D265/22 , C07D279/08 , C07D401/06 , C07D403/06 , C07D413/06 , C07D417/06 , C07D477/00 , C07D477/04 , C07D227/00
CPC分类号： C07D401/06 , C07D205/08 , C07D217/24 , C07D239/88 , C07D265/12 , C07D265/22 , C07D279/08 , C07D403/06 , C07D413/06 , C07D417/06 , C07D477/04
摘要： There is disclosed an azetidinone compound of the formula [I]: ##STR1## wherein Ring B is a benzene ring which may have substituent(s), R.sup.1 is a hydroxy-substituted lower alkyl group which may have substituent(s), X is oxygen atom and the like, Y is oxygen atom and the like, and Z is a methylene group which may have substituent(s), which is useful as a synthetic intermediate of the 1.beta.-methylcarbapenem-type antibacterial agent.
摘要翻译：公开了式[I]的氮杂环丁酮化合物：其中环B是可具有取代基的苯环，R 1是可具有取代基的羟基取代的低级烷基， X为氧原子等，Y为氧原子等，Z为可具有取代基的亚甲基，可用作1β-甲基碳青霉烯型抗菌剂的合成中间体。

9. 发明授权

US5550229A Alkylation process for preparing azetidinone compound and starting compound therefor 失效
标题翻译：制备氮杂环丁酮化合物及其起始化合物的烷基化方法
公开(公告)号：US5550229A
公开(公告)日：1996-08-27
申请号：US262892
申请日：1994-06-21
申请人： Tameo Iwasaki , Kazuhiko Kondo , Hiroshi Ohmizu
发明人： Tameo Iwasaki , Kazuhiko Kondo , Hiroshi Ohmizu
IPC分类号： C07D205/08 , C07D205/085 , C07D217/24 , C07D239/90 , C07D265/14 , C07D265/22 , C07D279/14 , C07D477/02 , C07D477/04 , C07F7/18 , C07D413/06 , C07D403/06 , C07D417/06
CPC分类号： C07D205/085 , C07D205/08 , C07D217/24 , C07D239/90 , C07D265/14 , C07D265/22 , C07D279/14 , C07D477/02 , C07D477/04 , C07F7/186 , C07F7/1892
摘要： Novel process for preparing azetidinone compound of the formula [III]: ##STR1## wherein R.sup.1 is H or lower alkyl, R.sup.2 and R.sup.3 combine together with the adjacent nitrogen to form heterocyclic group, and R.sup.4 is protected or unprotected hydroxy-substituted lower alkyl, which comprises reacting an alkanamide compound of the formula [I]: ##STR2## wherein R.sup.1, R.sup.2 and R.sup.3 are the same as defined above, with a compound of the formula [II]: ##STR3## wherein L.sup.1 is a leaving group and R.sup.4 is the same as defined above, in the presence of a base, said compound [III] being useful as synthetic intermediate for 1-methylcarbapenem derivative having excellent antibacterial activity.
摘要翻译：制备式[III]的氮杂环丁酮化合物的新方法：其中R 1为H或低级烷基，R 2和R 3与相邻的氮原子一起形成杂环基，并且R 4为被保护或未被保护的羟基取代的低级烷基，其包括使上述式[I]的链烷酰胺化合物与上述式[II]化合物反应：其中L 1是离去基团，且R 4与在碱的存在下，所述化合物[III]可用作具有优异抗菌活性的1-甲基碳青霉烯衍生物的合成中间体。

10. 发明授权

US5424446A Process for preparing optically active 4-mercapto-2-pyrrolidone derivative and intermediate therefor 失效
标题翻译：光学活性4-巯基-2-吡咯烷酮衍生物及其中间体的制备方法
公开(公告)号：US5424446A
公开(公告)日：1995-06-13
申请号：US166866
申请日：1993-12-15
申请人： Tameo Iwasaki , Kazuhiko Kondo , Tadashi Nakatani , Ryuzo Yoshioka
发明人： Tameo Iwasaki , Kazuhiko Kondo , Tadashi Nakatani , Ryuzo Yoshioka
IPC分类号： C07B53/00 , C07B57/00 , C07C309/24 , C07C319/28 , C07C323/58 , C07D207/26 , C07D207/273 , C07D477/02 , C07D207/416
CPC分类号： C07D207/273 , C07B57/00 , C07C309/24 , C07C319/28 , C07C323/58 , C07D477/02 , Y02P20/55
摘要： A process for preparing an optically active 4-mercapto-2-pyrrolidone derivative of the formula: ##STR1## wherein a group of the formula: --SR.sup.1 is a protected or unprotected mercapto group, and the group of the formula: .dbd.NR.sup.2 is a protected or unprotected imino group, which comprises subjecting racemic 4-amino-3-mercaptobutyric acid or a salt thereof to optical resolution by using 1-(2,3,4-trichlorophenyl)ethanesulfonic acid, followed by subjecting the product to cyclization reaction after protecting the functional groups thereof, if necessary, and further optionally removing the protecting groups therefrom. The present process is industrially advantageous than conventional processes for preparing optically active 4-mercapto-2-pyrrolidone derivatives which are useful as an intermediate for various medicines such as carbapenem antibacterial agents.
摘要翻译：制备下式的光学活性4-巯基-2-吡咯烷酮衍生物的方法：其中式-SR的基团是被保护或未被保护的巯基，并且下式的基团= NR2是受保护或未保护的亚氨基，其包括使用1-（2,3,4-三氯苯基）乙磺酸使外消旋4-氨基-3-巯基丁酸或其盐进行光学拆分，然后使产物保护其官能团后，如果需要，并进一步任选地从其中除去保护基，进行环化反应。本方法在工业上比用于制备光学活性的4-巯基-2-吡咯烷酮衍生物的方法是有用的，其可用作各种药物例如碳青霉烯类抗菌剂的中间体。

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