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。