摘要
目的优化泰地罗新的合成工艺。方法以泰乐菌素为起始原料,经还原胺化、酸性水解、卤代、哌啶取代及与磷酸成盐反应得到泰地罗新及其磷酸盐。结果目标化合物经质谱和核磁共振氢谱确证化学结构,总收率31.3%,纯度99.5%(HPLC)。结论该制备过程操作简单,易于实现工业化,磷酸盐形式储存较为稳定。
Objective To improve the manufacturing process of tildpirosin.Methods Using tylosin as the starting material,reductive amination,acid hydrolysis,halogenation,piperidine substitution,and salification reaction gave tildpirosin and its phosphate.Results The chemical structure of the target compound was confirmed by ESI-MS and^1H-NMR.The total yield was 31.3%,and the purity was 99.5%(HPLC).Conclusion The preparation operation is simple,rapid,and easy to scale up industrially.Storage in a phosphate form is relatively stable.
作者
孟可
李冀
黄凯
王腾
付德才
Meng Ke;Li Ji;Huang Kai;Wang Teng;Fu De-cai(College of Chemical and Pharmaceutical Engineering,Hebei University of Science and Technology,Shijiazhuang 050018;Hebei Yuanzheng Pharmaceutical Co.,Ltd,Shijiazhuang 050041)
出处
《中国抗生素杂志》
CAS
CSCD
2020年第5期437-440,共4页
Chinese Journal of Antibiotics
关键词
泰地罗新
二溴海因
磷酸盐
合成
Tildipirosin
1
3-Dibromo-5
5-dimethyl-hydantoin
Phosphate
Synthesis
