Process for the preparation of 7-amino and 7-substituted amino-desacetoxycephalosporins from the corresponding 6-substituted amino penicillin sulphoxides
申请人:GEMA S.A.
公开号:EP0169144A2
公开(公告)日:1986-01-22
An improved process is disclosed for the preparation of 7-amino and 7-substituted amino-desacetoxycephalosporins in which the corresponding 6-substituted amino penicillin sulphoxide is heated in the presence of an acidic substance which causes expansion of the penam ring in the reactant to the Δ3 cephem ring in the product in the presence of a silicon containing compound. The process comprises adding sulphamide or a silylsulphamide or a silylsulphamoyl to the reaction or utilizing a silylsulphamide or silylsulphamoyl as the silicon containing compound.
本发明公开了一种制备 7-氨基和 7-取代氨基-去乙酰氧基头孢菌素的改进工艺,在该工艺中,相应的 6-取代氨基青霉素亚砜在一种酸性物质存在下被加热,该酸性物质可使反应物中的 penam 环在含硅化合物存在下膨胀为产物中的Δ3 cephem 环。该工艺包括在反应中加入硫酰胺或甲硅烷基硫酰胺或甲硅烷基氨基甲酰基,或利用甲硅烷基硫酰胺或甲硅烷基氨基甲酰基作为含硅化合物。