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    2 .beta.-substituted thiomethylpenicillin derivatives and their preparation and use
    3.
    发明授权
    2 .beta.-substituted thiomethylpenicillin derivatives and their preparation and use 失效
    2β-取代的硫代甲基青霉素衍生物及其制备和用途

    公开(公告)号：US4861768A

    公开(公告)日：1989-08-29

    申请号：US16114

    申请日：1987-02-18

    申请人： Sigeru Torii ,  Hideo Tanaka ,  Motoaki Tanaka ,  Shozo Yamada ,  Akira Nakai ,  Hisashi Ohbayashi

    发明人： Sigeru Torii ,  Hideo Tanaka ,  Motoaki Tanaka ,  Shozo Yamada ,  Akira Nakai ,  Hisashi Ohbayashi

    IPC分类号： C07D499/00 ,  C07D499/86

    CPC分类号： C07D499/00

    摘要： Disclosed is a penicillin derivative of the formula: ##STR1## wherein n is an integer of 0, 1 or 2; Y is a cyano group, a lower acyl group, a mono- or di-lower alkylthiocarbamoyl group, ##STR2## wherein R.sub.1 is a hydrogen atom, a lower alkyl group, a phenyl group, a group --(CH.sub.2).sub.m --OR.sub.2 or --(CH.sub.2).sub.m COOR.sub.2 (m is an integer of 1 to 6 and R.sub.2 is a hydrogen atom or a penicillin carboxyl ester-forming group which is commonly used for penicillin derivatives) or a phenyl group substituted by at least one member selected from the class consisting of lower alkyl group, halogen atom and lower alkoxy group; and R is a hydrogen atom or a penicillin carboxyl ester-forming group, or a salt thereof. They are useful as .beta.-lactamase inhibitors.

    摘要翻译： 公开了下式的青霉素衍生物：其中n是0,1或2的整数; Y是氰基，低级酰基，单 - 或二 - 低级烷硫基氨基甲酰基，其中R1是氢原子，低级烷基，苯基，基 - （CH2）m-OR2或 - （CH 2）m COOR 2（m为1〜6的整数，R2为氢原子或青霉素衍生物通常使用的青霉素羧酸酯形成基）或被选自上述的至少一种的苯基 由低级烷基，卤素原子和低级烷氧基组成; 和R是氢原子或青霉素羧酸酯形成基团或其盐。 它们可用作β-内酰胺酶抑制剂。

    Process for preparing thiazolino azetidinone and 2-exo-methylenepenam derivative
    8.
    发明授权
    Process for preparing thiazolino azetidinone and 2-exo-methylenepenam derivative 失效
    制备噻唑基氮杂环丁酮和2-外 - 亚甲基台am am嗪衍生物的方法

    公开(公告)号：US5288860A

    公开(公告)日：1994-02-22

    申请号：US3024

    申请日：1993-01-11

    申请人： Sigeru Torii ,  Hideo Tanaka ,  Masatoshi Taniguchi ,  Michio Sasaoka ,  Takashi Shiroi ,  Yutaka Kameyama

    发明人： Sigeru Torii ,  Hideo Tanaka ,  Masatoshi Taniguchi ,  Michio Sasaoka ,  Takashi Shiroi ,  Yutaka Kameyama

    IPC分类号： C07D499/00 ,  C07D499/04 ,  C07D499/12 ,  C07D499/87 ,  C07D513/04

    CPC分类号： C07D513/04 ,  C07D499/00 ,  Y02P20/55

    摘要： The present invention provides a thiazolinoazetidinone derivative represented by the formula ##STR1## wherein R.sup.1 is phenyl having or not having substituent(s), methyl having or not having substituent(s) or ##STR2## group, R.sup.3 being phenyl having or not having substituent(s), and R.sup.2 is a hydrogen atom or carboxylic acid protective group, and a process for preparing the same.The present invention further provides a process for preparing a 2-exo-methylenepenam derivative characterized by hydrolyzing the thiazoline ring of a thiazolinoazetidinone derivative of the above formula (1) to effect recyclization and obtain a 2-exo-methylenepenam derivative represented by the formula ##STR3## wherein R.sup.1 and R.sup.2 are as defined above.

    摘要翻译： 本发明提供由式（1）表示的噻唑并氮杂环丁酮衍生物，其中R 1是具有或不具有取代基的苯基，具有或不具有取代基的甲基或基团，R3是具有或不具有取代基的苯基， 不具有取代基，R2为氢原子或羧酸保护基，及其制备方法。 本发明进一步提供了制备2-异亚甲基台内叶酸衍生物的方法，其特征在于水解上述式（1）的噻唑并氮杂环丁酮衍生物的噻唑啉环以进行再循环，得到式（1）所示的2-外 - 亚甲基山梨醇衍生物， 图像（3）其中R1和R2如上所定义。

    Process for preparing alkoxyphenols
    10.
    发明授权
    Process for preparing alkoxyphenols 失效
    制备烷氧基酚的方法

    公开(公告)号：US4588835A

    公开(公告)日：1986-05-13

    申请号：US662542

    申请日：1984-10-19

    申请人： Sigeru Torii ,  Hideo Tanaka ,  Mitsuo Akada

    发明人： Sigeru Torii ,  Hideo Tanaka ,  Mitsuo Akada

    IPC分类号： C07C41/16 ,  C07C43/23 ,  C07C45/70 ,  C07C45/71 ,  C07C45/64 ,  C07C67/28

    CPC分类号： C07C45/70 ,  C07C41/16 ,  C07C45/71

    摘要： A process for preparing an alkoxyphenol represented by the formula: ##STR1## wherein R is hydrogen, alkyl having 1 to 4 carbon atoms, formyl, hydroxymethyl, alkoxymethyl, dialkoxymethyl, acetoxymethyl or diacetoxymethyl, R' is alkyl having 1 to 4 carbon atoms, and n is an integer of 1 to 5, characterized in that a phenol halide represented by the formula: ##STR2## wherein R and n are as defined above, and X is chlorine or bromine is reacted, in the presence of a copper salt serving as a catalyst and of a solvent, with a product prepared by heating, in the presence of a dehydrating agent, an alkali metal hydroxide and a compound of the formula R'OH wherein R' is as defined above.

    摘要翻译： 一种由下式表示的烷氧基苯酚的方法：其中R为氢，具有1至4个碳原子的烷基，甲酰基，羟甲基，烷氧基甲基，二烷氧基甲基，乙酰氧基甲基或二乙酰氧基甲基，R'为具有1至4个碳原子的烷基， n为1〜5的整数，其特征在于，在铜盐的存在下，使由式（Ⅰ）表示的酚卤化物，其中R和n如上述定义，X为氯或溴， 作为催化剂和溶剂，通过在脱水剂的存在下，碱金属氢氧化物和式R'OH的化合物加热制备的产物，其中R'如上定义。