公开(公告)号：EP0759437A4

公开(公告)日：1997-06-11

申请号：EP96905005

申请日：1996-03-06

申请人： OTSUKA KAGAKU KK

发明人： SASAOKA MICHIO ,  SUZUKI DAISUKE ,  SUH DELSOO ,  TOKUMARU Y

IPC分类号： C07D513/04 ,  A61K31/54 ,  A61P31/04 ,  C07D205/08 ,  C07D498/04 ,  C07D501/00 ,  C07D507/08

CPC分类号： C07D205/08 ,  C07D501/00 ,  Y02P20/55

摘要： A process for producing a 2-isocephem derivative which comprises treating, in a water-containing organic solvent, a 2-azetidinyl-3,4-dihalogeno-2-butenoic acid compound represented by general formula (1) with a thioacetic acid derivative showing basicity per se or a mixture of a base with a thioacetic acid derivative to thereby give a 3-halomethyl-2-isocephem derivative represented by general formula (2); and a process for producing a 2-oxaisocephem derivative which comprises treating, in a water-containing organic solvent, a 2-azetidinyl-3,4-dihalogeno-2-butenoic acid compound represented by general formula (1) with a base to thereby give a 3-halomethyl-2-oxaisocephem derivative represented by general formula (3); in formula (1), R1 represents hydrogen or optionally protected amino; R2 represents hydrogen or lower alkoxy, or R?1 and R2¿ may form together a cyclic amino protecting group; R3 represents hydrogen or a carboxyl protecting group; W represents a leaving group; and X and Y may be the same or different and each represents halogeno; in formula (2), R?1, R2, R3¿ and X are each as defined above; in formula (3), R?1, R2, R3¿ and X are each as defined above.

摘要翻译： 通过以下方法制备结构式（3）的2-氧代奥西辛衍生物，其中使碱在含水有机溶剂中作用于结构（1）的2-氮杂环丁烷基-3,4-二卤代-2-丁烯酸化合物 得到3-卤代甲基2-氧代硫代衍生物。