公开(公告)号：EP2123657A1

公开(公告)日：2009-11-25

申请号：EP08721477.1

申请日：2008-03-06

申请人： OTSUKA CHEMICAL COMPANY, LTD.

发明人： TANAKA, Hideo ,  KUROBOSHI, Manabu ,  TATEYAMA, Syoichi ,  YAMADA, Takae ,  KAMEYAMA, Yutaka

IPC分类号： C07D499/04 ,  C07D499/861 ,  C07D499/897

CPC分类号： C07D499/04 ,  C07D499/861 ,  C07D499/897 ,  Y02P20/55

摘要： The present invention provides a method by which a 6-hydroxyethyl penam compound represented by General Formula (2) below can be produced with a high selectivity:

wherein R represents a hydrogen atom or a protective group for carboxylic acid and X 2 represents a halogen atom;
the method including the steps of reacting a Grignard reagent with a halogeno penam compound represented by General Formula (1) below:

wherein R and X 2 are the same as above, and X 1 represents a halogen atom;
reacting the generated compound with an amine compound; and
further reacting the generated compound with acetaldehyde.

摘要翻译： 本发明提供了一种可以以高选择性制备下述通式（2）表示的6-羟乙基青霉素化合物的方法：其中R代表氢原子或羧酸保护基团，并且X 2代表卤素原子; 所述方法包括以下步骤：使格利雅试剂与由以下通式（1）表示的卤代青霉烷化合物反应：其中R和X2与上述相同，并且X1表示卤素原子; 使生成的化合物与胺化合物反应; 并进一步使生成的化合物与乙醛反应。