他氟前列素的合成

Synthesis of tafluprost

目的:对他氟前列素合成工艺进行研究。方法:以科立内酯为起始原料,经过tempo氧化反应、Hormer-Wadsworth-Emmons反应、氟代、水解/还原、Wittig反应、酯化等反应合成目标化合物。结果:目标产物结构经1H-NMR和ESI-MS确证。结论:该工艺缩短了合成步骤,优化了反应条件,简化了操作,提高了产品收率。

Objective： To study the synthetic technology of tafluprost. Methods： The target compound was synthesized through TEMPO oxidation,Hormer-Wadsworth-Emmons reaction,fluorination,hydrolysis reduction,Wittig reaction,and esterification from corey lactone. Results： The structure of tafluprost was verified by^1H-NMR and ESI-MS. Conclusion： The established synthetic process has several advantages,such as reduced reaction steps,convenient operation,mild reaction condition,and higher yield.