泰地罗新生产工艺的改进
Improvement of the Production Process of Tildipirosin
李有志 1魏秀丽 2马居良3
作者信息
- 1. Shandong Provincial Key Laboratory of Qμality Safety Monitoring and Risk Assessment for Animal Products,Shandong Center for Qμality Control of Feed and Veterinary Drug,Jinan 250100,China
- 2. 山东省饲料兽药质量检验中心,山东省畜产品质量安全监测与风险评估重点实验室,济南 250100
- 3. 山东久隆恒信药业有限公司,山东德州 251100
- 折叠
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 tri oxide 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.
关键词
泰地罗新/泰乐菌素/合成/氧化Key words
tildipirosin/tylosin/synthesis/oxide引用本文复制引用
基金项目
泰山产业创新领军人才专项资助(TSCX202211023)
山东省科技型中小企业创新能力提升工程项目(2022TSGC2549)
出版年
2024
国家科技期刊平台
NSTL
万方数据