公开(公告)号：EP0989132A4

公开(公告)日：2001-11-14

申请号：EP99910811

申请日：1999-04-02

申请人： OTSUKA KAGAKU KK

发明人： SHIMABAYASHI AKIHIRO ,  KAWAHARA ICHIROU ,  YAGUCHI SHIGETOSHI ,  ASAI HIROAKI

IPC分类号： C07D499/87 ,  C07D499/00 ,  C07D499/04 ,  C07D499/10 ,  C07D499/86 ,  C07D499/865 ,  C07D499/897 ,  C07D501/00 ,  C07D501/04 ,  C07D501/16 ,  C07D501/59

CPC分类号： C07D499/00 ,  C07D501/00

摘要： A process for producing a halogenated β-lactam compound represented by general formula (4), characterized by reacting a β-lactam-derived amino compound represented by general formula (1) with nitrous acid or a nitrite in the presence of halogen molecules under acid conditions while keeping the reactants in an aqueous slurry state to obtain the target compound. In formula (1) n is an integer of 0 to 2; and A represents formula (2) or (3), wherein R?1 and R2¿ are the same or different and each is hydrogen, halogeno, C¿1-3? alkyl, C2-4 alkenyl, C2-4 alkynyl, a nucleophilic group, or CH2R?3¿, where R3 represents halogeno or a nucleophilic group. In formula (4) A is the same as the above; X1 represents hydrogen or halogeno; and X2 represents halogeno.