| 摘要: |
| 为优化泰地罗新合成工艺，将泰乐菌素经胺化，亲核取代，氧化，二次胺化后得到
泰地罗新成品。其中，氧化20位羟基采用了二甲亚砜-吡啶-三氧化硫氧化剂，将20位羟基氧化为醛基且经缩合反应引入哌啶基，该工艺相较于文献中报道的碘代而言，降低了生产成本，减少了副反应的发生，提高了泰地罗新的收率，使总收率在43%。该工艺制备简单，可以实现工业化生产。 |
| 关键词: 泰地罗新 泰乐菌素 合成 氧化 |
| DOI： |
| 投稿时间：2024-05-26修订日期：2024-09-11 |
| 基金项目:泰山产业创新领军人才专项资助(项目编号：TSCX202211023)；山东省科技型中小企业创新能力提升工程项目（2022TSGC2549） |
|
| Improvement the production process of Tildipirosin |
|
| (Shandong Center for Quality Control of Feed and Veterinary Drμgs) |
| Abstract: |
| In order to optimize the synthesis process of Tylosin, Tylosin was obtained by amination, nucleophilic substitution, oxidation, and secondary amination. Among them, Dimethyl sulfoxide- pyridine -sulfur trioxide oxidant was used to oxide the 20 hydroxyl group, which was oxidized to an aldehyde group and capable of adding a piperidine group. Compared with the reported iodine substitution in the literature, this process reduced production costs, reduced the occurrence of side reactions, and improved the yield of tirosin, resulting in a total yield of 43%. This process is simple to prepare and can achieve industrial production. |
| Key words: Tildipirosin Tylosin Synthesis Oxide |
