扎来普隆的合成

Synthesis of Zaleplon

对以 3-乙酰基苯胺为原料经酰化、缩合、乙基化及环合制得扎来普隆 (Zaleplon)工艺进行了研究 ,并对此工艺的缩合、乙基化及环合后处理方法进行了改进 ,采用溶剂重结晶来替代原工艺的柱层析 ,操作简便 ,溶剂用量降低90 % ,总收率从 38.0 %提高到 5 3.4 % ,总成本降低了 4 0 % ,适合于工业化生产。

The technical process for synthesis of Zaleplon, which is got after being acylated, condensated, ethylated and cyclized by using 3-acetylphenyamine as the raw material, has been studied. Improvements for the technical methods of condensation and cyclization also have been studied. The original process of column chromatography is replaced by the re-crystallization from solvents, which is convenient to operate and suitable for industrial production. The quantity of consumed solvent is reduced 90%, the total yield is increased from 38.0% to 53.4%, and the total cost is decreased 40%.