泰地罗新生产工艺的改进

Improvement the production process of Tildipirosin

关键词:  泰地罗新  泰乐菌素  合成  氧化

Key words:  Tildipirosin  Tylosin  Synthesis  Oxide

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。

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.