申请人:SANRAKU-OCEAN CO., LTD.
公开号:EP0001841A2
公开(公告)日:1979-05-16
A number of 4"-acyl derivatives of tylosin and acetyltylosin which are prepared by first protectively acylating at the 2'-hydroxyl group of tylosin or acetyitylosin, secondly at the 4'''-hydroxyl group thereof, thirdly at the 4"-hydroxyl group thereof and finally deacylating the 2'- and 4'''-acyl groups to produce new 4" acyl derivatives of tylosin or scetyltylosin which effect high blood level compared to those tylosin derivatives heretofore are disclosed.
本发明公开了一些泰乐菌素和乙酰基酪氨霉素的 4"-酰基衍生物,其制备方法是首先在泰乐菌素或乙酰基酪氨霉素的 2'-羟基上进行保护性酰化,其次在其 4''-羟基上进行保护性酰化,第三在其 4"-羟基上进行保护性酰化,最后在 2'-和 4''-酰基上进行脱酰化,从而制备出新的泰乐菌素或乙酰基酪氨霉素的 4"-酰基衍生物,与迄今为止的泰乐菌素衍生物相比,这些衍生物具有较高的血药浓度。