公开(公告)号：EP1010701A4

公开(公告)日：2001-07-11

申请号：EP99926869

申请日：1999-06-30

申请人： OTSUKA KAGAKU KK

发明人： KAMEYAMA YUTAKA ,  YAMADA TAKAE ,  SUH DAL SOO

IPC分类号： A61K31/545 ,  A61K31/546 ,  A61P31/04 ,  C07D501/00 ,  C07D501/04 ,  C07D501/18

CPC分类号： C07D501/00

摘要： A process for the preparation of 3-cephem compounds, characterized by reacting a β-lactam compound represented by general formula (1) with a phosphorus halide compound in the presence of an organic base to form an imino-β-lactam compound represented by general formula (2), adding a phenol to the resulting reaction system to conduct alcoholysis simultaneously with the deblocking of the carboxylate ester, and thus obtaining a 3-cephem compound represented by general formula (3) or a salt thereof, wherein R1, R2, R3 and X are each as defined in the description.

公开(公告)号：EP0700916A4

公开(公告)日：1996-07-24

申请号：EP95912451

申请日：1995-03-17

申请人： OTSUKA KAGAKU KK ,  TAIHO PHARMACEUTICAL CO LTD

发明人： AKAGI HIROSHI ,  YASUI MASARU ,  YAMADA TAKAE ,  ITO MASAHIRO ,  HANAKI HIDEAKI ,  HYODO AKIO

IPC分类号： C07D501/00 ,  C07D501/24 ,  A61K31/545

CPC分类号： C07D501/00

摘要： A cephem compound represented by general formula (1), which has an excellent antibacterial effect against various pathogenic bacteria, wherein Q represents CH or N; R1 represents carboxylate, etc.; R represents group (a) or (b); R3 represents -(CH¿2?)m-Y (m being an integer of 1 to 5, and Y being quaternary ammonium), etc.; n represents an integer of 0,1 to 4; B?-¿ represents an anion; f represents 0 or 1 when R1 represents carboxylate, and 2 when R1 represents carboxyl; and ring C represents a five-membered heterocyclic group which bears four or less nitrogen atoms and may be substituted by lower alkyl.