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抗血吸虫药物吡喹酮的合成研究

林楚焱 汪坤坤 张坤 李玫桦 张韵

遵义医科大学学报2025,Vol.48Issue(4):380-385,6.
遵义医科大学学报2025,Vol.48Issue(4):380-385,6.

抗血吸虫药物吡喹酮的合成研究

Study on the synthesis of schistosomiasis drug praziquantel

林楚焱 1汪坤坤 1张坤 2李玫桦 2张韵3

作者信息

  • 1. 遵义医科大学 药学院,贵州 遵义 563006||遵义医科大学 第一临床学院,贵州 遵义 563006
  • 2. 遵义医科大学 药学院,贵州 遵义 563006
  • 3. 遵义医科大学 药学院,贵州 遵义 563006||遵义医科大学 贵州省化学药物创制全省重点实验室,贵州 遵义 563006
  • 折叠

摘要

Abstract

Objective To study the synthetic method of schistosomiasis drug praziquantel.Methods Praziquan-tel was synthesized via oxidation,three-component reaction based on imine acylation,reduction,acylation,deprotection,acylation and cyclization reaction by using tetrahydroisoquinoline as starting material.Results The total yield of the praziquantel synthesis was 52%.The structures of praziquantel and intermediates in the process were confirmed by 1 H-NMR,13 C-NMR and HR-MS.Conclusion This method effectively avoids the use of harsh reaction conditions such as concentrated sulfuric acid,highly toxic potassium cyanide,high temperature and high pressure.This method ensures the mild reaction conditions,convenience and cost-effectiveness of the entire syn-thesis route,and shows certain industrial application potential.

关键词

吡喹酮/血吸虫药物/三组分反应/合成/新工艺

Key words

praziquantel/schistosomiasis drug/three-component reaction/synthesis/new process

分类

临床医学

引用本文复制引用

林楚焱,汪坤坤,张坤,李玫桦,张韵..抗血吸虫药物吡喹酮的合成研究[J].遵义医科大学学报,2025,48(4):380-385,6.

基金项目

贵州省科技计划项目[NO:黔科合基础-ZK(2022)一般621] (2022)

遵义医科大学大学生创新创业训练计划项目(NO:S202310661152). (NO:S202310661152)

遵义医科大学学报

2096-8159

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