他氟前列素的合成工艺改进

Improved synthesis of tafluprost

以科立内酯为起始原料,经过Swern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,总收率为47.2%,目标化合物和关键中间体结构经MS和1H NMR确证。本工艺改进提高了反应收率,减少了过柱提纯的步骤,降低了生产成本,有利于工业化生产。

The target compound was synthesized through Swern oxidation,Hormer-Wadsworth-Emmons reaction,fluorination,hydrol-ysis,reduction,Wittig reaction and esterification from corey lactone with an overall yield of 47. 2%. The target compound and the key intermediates were confirmed by MS and 1 H NMR. The improved synthesis was benefited from high yield,easy after-treatment procedure,low cost and could be readily scale-up to mass production.