草酸依地普仑的合成

Synthesis of Escitalopram Oxadate

以5-氰基苯酞为起始原料,经亲核加成、水解、手性拆分、环化和成盐等反应制得抗抑郁药草酸依地普仑,以5-氰基苯酞计,总收率为19%。该方法工艺简单,条件温和,收率较高,适合工业化生产。

5-cyanophthalide as the starting material,escitalopram oxalate was prepared via several steps including nucleophilic addition,hydrolysis,chiral separation,cyclization and salt formation.A total yield of escitalopram oxalate was 19%.This synthetic process had milder reactive conditions,with simple procedure and high total yield.The route was suitable for industrial production.