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    Enantioselective process for producing 1-beta-methylcarbapenem antibiotic intermediates
    40.
    发明公开
    Enantioselective process for producing 1-beta-methylcarbapenem antibiotic intermediates 失效
    用于生产1-甲基胆碱酯抗生素中间体的选择性方法

    公开(公告)号：EP0197432A3

    公开(公告)日：1987-01-21

    申请号：EP86104146

    申请日：1986-03-26

    申请人： MERCK & CO. INC.

    发明人： Shinkai, Ichiro ,  Salzmann, Thomas N. ,  Fuentes, Lelia M.

    IPC分类号： C07D205/08 ,  C07D413/06 ,  C07D417/06 ,  C07D263/22 ,  C07D263/26 ,  C07D277/12

    CPC分类号： C07D413/06 ,  C07D205/08 ,  C07D263/22 ,  C07D263/26 ,  C07D277/12 ,  C07D417/06 ,  Y02P20/55

    摘要： A stereo-controlled process is described for preparing a compound of the formula:
    wherein R 1 is, e.g., C 1 -C 4 alkyl, R 2 and R 9 are independently selected from hydrogen, C 1 -C 4 linear, branched or cyclic alkyl, unsubstituted or substituted with fluoro, hydroxy, or protected hydroxy, with the proviso that both R 2 and R 9 are not unsubstituted alkyl, and R 3 is H or easily removable protecting group, comprising the steps of (a) reacting the compound:
    wherein L is a leaving group, with the chiral compound:
    wherein X 1 and X 2 are independently 0 or S, R 8 is an easily removable enol protecting group, R 4 and R 5 and R 6 are independently selected from H, C 1 -C 4 alkyl, C 7 -C 10 aralkyl, C 6 -C 10 alkaryl, which can be substituted with -OH, -OR 10 , -SH,-SR 10 , where R 10 is C 1 -C 4 alkyl, with proviso that R 4 and R 5 are not identical, in the presence of an organic base and a Lewis acid catalyst to afford the compound:
    and then (b) contacting said compound in a solvent therefor, under basic hydrolysis conditions. This compound can be transformed into a carbapenem antibiotic.