申请人:KRKA, tovarna zdravil, d.d., Novo mesto
公开号:EP1785414A1
公开(公告)日:2007-05-16
The present invention relates to the synthesis of antibacterial compounds such as Chloramphenicol and its analogues Thiamphenicol and Florfenicol and particularly to a new reaction for the preparation of the intermediate compound aminodiolphenylsulfone. This reaction permits the introduction of modified residues to obtain modified antibiotics with an improved stability towards the action of bacterial resistant determinants. In addition, higher purities may be also obtained due to an improved procedure requiring fewer purification steps.
本发明涉及抗菌化合物的合成,如氯霉素及其类似物硫胺苯酚和氟苯胺,特别涉及一种用于制备中间体氨基二酚苯砜的新反应。该反应允许引入修饰残基,以获得对细菌耐药基因作用具有改进稳定性的修饰抗生素。此外,由于改进的程序需要更少的纯化步骤,也可以获得更高的纯度。