申请人:SHIONOGI SEIYAKU KABUSHIKI KAISHA
公开号:EP0336143A1
公开(公告)日:1989-10-11
A novel intermediate for synthesizing 1β-alkyl-1-carbapenem, i.e., 4β-(1β-alkyl-2-carboxyprop-2-enyl)-azetidin-2-one ( II ), is prepared stereoselectively by treating 4-(leaving group substituted)azetidin-2-one ( I ) with trans-2-(leaving group substituted)methyl-3-alkylacrylic acid ( III ) and a reducing metal.
wherein, R1 is hydrogen, alkyl, or substituted alkyl;
R2 is optionally substituted alkyl;
R3 is hydrogen or a carboxy-protecting group; and
R4 and R5 each is a leaving group.
一种合成 1β-烷基-1-碳青霉烯的新型中间体,即 4β-(1β-烷基-2-羧基丙-2-烯基)-氮杂环丁烷-2-酮 ( II ),是通过将 4-(离去基团取代)氮杂环丁烷-2-酮 ( I )与反式-2-(离去基团取代)甲基-3-烷基丙烯酸 ( III )和还原性金属进行立体选择性处理而制备的。
其中,R1 是氢、烷基或取代的烷基;
R2 是任选取代的烷基
R3 是氢或羧基保护基团;以及
R4 和 R5 各为离去基团。