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    Process for preparing optically active 4-mercapto-2-pyrrolidone derivative and intermediate therefor
    1.
    发明授权
    Process for preparing optically active 4-mercapto-2-pyrrolidone derivative and intermediate therefor 失效
    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。

    Process for preparing optically active 4-mercapto-2-pyrrolidone derivative and intermediate therefor
    2.
    发明授权
    Process for preparing optically active 4-mercapto-2-pyrrolidone derivative and intermediate therefor 失效
    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。

    Process for preparing .beta.-lactam derivative and synthetic intermediate thereof
    7.
    发明授权
    Process for preparing .beta.-lactam derivative and synthetic intermediate thereof 失效
    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。

    Process for preparing carbapenem derivatives
    8.
    发明授权
    Process for preparing carbapenem derivatives 失效
    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。

    Biphenyl derivatives, process for preparing the same and intermediates therefor
    10.
    发明授权
    Biphenyl derivatives, process for preparing the same and intermediates therefor 失效
    联苯衍生物，其制备方法及其中间体

    公开(公告)号：US5182404A

    公开(公告)日：1993-01-26

    申请号：US821215

    申请日：1992-01-15

    申请人： Tameo Iwasaki ,  Kazuhiko Kondo ,  Yuzo Matsuoka ,  Mamoru Matsumoto ,  Masaki Sugiura

    发明人： Tameo Iwasaki ,  Kazuhiko Kondo ,  Yuzo Matsuoka ,  Mamoru Matsumoto ,  Masaki Sugiura

    IPC分类号： C07C45/51 ,  C07C65/21 ,  C07C69/94 ,  C07D317/68

    CPC分类号： C07D317/68 ,  C07C45/515 ,  C07C65/21 ,  C07C69/94

    摘要： Novel biphenyl derivatives of the formula: ##STR1## wherein R.sup.1 is a substituted or unsubstituted aminocarbonyl group, aminothiocarbonyl group, a substituted or unsubstituted lower alkoxycarbonyl group, cyano group, or a group of the formula: ##STR2## one or two of R.sup.2 to R.sup.7 are hydrogen atom, and the remaining groups are the same or different and are each a lower alkoxy group, a phenyl-(lower)alkoxy group or hydroxy group, or the adjacent two groups thereof combine to form a lower alkylenedioxy group, and Alk.sup.1 is a lower alkylene group,or a pharmaceutically acceptable salt thereof, which are useful for the prophylaxis and treatment of hepatic diseases, and processes for preparing the same, and intermediates therefor.

    摘要翻译： 下式的新型联苯衍生物：其中R1是取代或未取代的氨基羰基，氨基硫代羰基，取代或未取代的低级烷氧基羰基，氰基或下式的基团：其中R 1〜 R7是氢原子，其余基团相同或不同，各自为低级烷氧基，苯基 - （低级）烷氧基或羟基，或其相邻的两个基团组合形成低级亚烷基二氧基，Alk1 是用于预防和治疗肝脏疾病的低级亚烷基或其药学上可接受的盐及其制备方法及其中间体。