药物中间体(R)-3-氨基哌啶二(三氟乙酸)盐的合成

Synthesis of( R)-3-aminopiperidine ditrifluoroacetate

以(R)-2-((苄氧羰基)氨基)-1,5-戊二醇(1)为原料,通过酯化、环合、催化氢化、成盐反应,合成了药物中间体(R)-3-氨基哌啶二(三氟乙酸)盐(5);其结构经1H NMR、13C NMR、IR和元素分析表征。该方法具有成本较低、反应条件温和、易操作等特点,有利于工业化生产。

Drug intermediates of（R）-3-aminopiperdine ditrifluoroacetate was synthesized by using（R）-2-carbobenzoxyamino-1,5-pentanediol as raw materials, through esterification, cyclization, catalytic hydrogenation and salification reaction. And the structure of（R）-3-aminopiperdine ditrifluoroacetate was characterized by 1H NMR, 13C NMR, IR and elemental analysis. The results showed that this method has low cost, mild reaction condition, easy operation and is suitable for production in industrial scale.