生化法合成阿托莫西汀的研究

The biochemical synthesis research of atomoxetine

药物治疗是矫正注意缺陷多动障碍(ADHD)的重要措施之一。以苯乙酮为原料经Mannich反应,微生物发酵还原、手性拆分,邻氟甲苯缩合,最终得目标产物阿托莫西汀。用生化合成法改进了中间体2的合成工艺,使其收率提高到了61.3%。该方法原料易得,操作方便,条件温和,收率较高,适于工业化生产。

Medical intervention is all important alternative for treatment of attention defecter hyperactivit disorder（ADHD）.As raw materials in order to Acetophenone by Mannich reaction,to restore the microbial fermentation and chiral separation,po-fluoride condensation,the final goal was a product of phenacetin Atomoxetine.Biological and chemical synthesis with improved synthesis of intermediate 2,to yield increased to 61.3%.The process is convenient for industrial production with high yield,available raw material and easy operation undermild condition.