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泰地罗新生产工艺的改进

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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.
Improvement of the Production Process of Tildipirosin
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.

tildipirosintylosinsynthesisoxide

李有志、魏秀丽、马居良

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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

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

山东久隆恒信药业有限公司,山东德州 251100

泰地罗新 泰乐菌素 合成 氧化

泰山产业创新领军人才专项资助山东省科技型中小企业创新能力提升工程项目

TSCX2022110232022TSGC2549

2024

中国兽药杂志
中国兽医药品监察所

中国兽药杂志

CSTPCD
影响因子:0.49
ISSN:1002-1280
年,卷(期):2024.58(9)
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