罗氟司特的合成

Synthesis of Roflumilast

以3-羟基-4-二氟甲氧基苯甲醛为原料,经过四步反应得到罗氟司特,总收率76.8%,产物结构经元素分析、NMR和MS得到了确证。该方法反应条件温和,后处理简单,适合工业化生产。

The Roflumilast was synthesized used 3-hydroxy-4-difluoromethoxy benzaldehyde as the initial materials. The reaction was readily performed with good yield under mild conditions and convenient operations, The total yield is 76.8 %, The structure was characterized by Elemental analysis,NMR and MS spectrum.