Process for preparing thiazolino azetidinone and 2-exo-methylenepenam
derivative
    2.
    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

    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 cephem compounds
    4.
    发明授权
    Process for preparing cephem compounds 失效
    头孢烯化合物的制备方法

    公开(公告)号:US5656754A

    公开(公告)日:1997-08-12

    申请号:US211119

    申请日:1994-03-22

    摘要: The present invention provides a process for preparing a cephem compound represented by the general formula (3) characterized in that an allenyl-.beta.-lactam compound represented by the general formula (1) is reacted with an organotin compound represented by the general formula (2) in the presence of a monovalent copper salt ##STR1## wherein R.sup.1 is a hydrogen atom, halogen atom, amino or protected amino, R.sup.2 is a hydrogen atom, halogen atom, lower alkoxyl, lower acyl, lower alkyl, lower alkyl having hydroxyl or protected hydroxyl as a substituent, hydroxyl or protected hydroxyl, or R.sup.1 and R.sup.2 form=0 when taken together, R.sup.3 is a hydrogen atom or carboxylic acid protecting group, R.sup.4 is aryl, aryl having a substituent, nitrogen-containing aromatic heterocyclic group or nitrogen-containing aromatic heterocyclic group having a substituent, and m is 0 or 2,(R.sup.5).sub.n --Sn(R.sup.6).sub.4--n (2)wherein R.sup.5 is alkenyl, alkenyl having a substituent, aryl, aryl having a substituent, nitrogen-containing aromatic heterocyclic group or nitrogen-containing aromatic heterocyclic group having a substituent, R.sup.6 is lower alkyl, and n is 1 or 2, ##STR2## wherein R.sup.1, R.sup.2, R.sup.3 and R.sup.5 are the same as defined above.

    摘要翻译: PCT No.PCT / JP93 / 01041 Sec。 371日期:1994年3月22日 102(e)1994年3月22日PCT 1993年7月26日PCT公布。 出版物WO94 / 02490 日期:1994年2月3日本发明提供一种制备由通式(3)表示的头孢烯化合物的方法,其特征在于,将由通式(1)表示的丙烯酰基-β-内酰胺化合物与由 在一价铜盐(1)的存在下通式(2)其中R1是氢原子,卤素原子,氨基或被保护的氨基,R2是氢原子,卤素原子,低级烷氧基,低级酰基, 低级烷基,具有羟基或被保护的羟基作为取代基的低级烷基,羟基或保护的羟基,或者R 1和R 2形成= 0,当R 3是氢原子或羧酸保护基时,R 4是芳基,具有取代基的芳基, 具有取代基的含氮芳香族杂环基或含氮芳香族杂环基,m为0或2,(R5)n-Sn(R6)4-n(2)其中R5为烯基,具有取代基的烯基, ,具有取代基的芳基,氮 - 具有取代基的芳族杂环基或含氮芳族杂环基,R6是低级烷基,n是1或2,其中R1,R2,R3和R5与上述定义相同。

    Process for preparing azetidinone derivatives
    10.
    发明授权
    Process for preparing azetidinone derivatives 失效
    制备氮杂环丁酮衍生物的方法

    公开(公告)号:US4622178A

    公开(公告)日:1986-11-11

    申请号:US608695

    申请日:1984-05-01

    摘要: A process for preparing an azetidinone derivative represented by the formula ##STR1## wherein R.sup.1 represents a straight-chain or branched-chain lower alkyl group, substituted or unsubstituted aryl group, substituted or unsubstituted phenylmethyl group or substituted or unsubstituted phenyloxymethyl group, R.sup.2 represents hydrogen atom, an optionally substituted hydrocarbon residue or protective group for amino group selected from the class consisting of acyl, silyl, sulfonyl and phosphonyl derived from organic or inorganic acid, and R.sup.3 represents a substituted or unsubstituted aryl group or the residue of substituted or unsubstituted heterocyclic ring.

    摘要翻译: PCT No.PCT / JP83 / 00298 Sec。 371日期1984年5月1日 102(e)日期1984年5月1日PCT提交1983年9月6日PCT公布。 出版物WO84 / 00960 日本3月15日,1984年。一种制备式(I)表示的氮杂环丁酮衍生物的方法,其中R 1表示直链或支链的低级烷基,取代或未取代的芳基,取代或未取代的苯基甲基 或取代或未取代的苯氧基甲基,R2表示氢原子,任选取代的烃残基或选自有机或无机酸的酰基,甲硅烷基,磺酰基和膦酰基的氨基的保护基,R3表示取代或未取代的 芳基或取代或未取代的杂环的残基。