Method for the synthesis of rasagiline
    10.
    发明授权
    Method for the synthesis of rasagiline 有权
    雷沙吉兰的合成方法

    公开(公告)号:US08901352B2

    公开(公告)日:2014-12-02

    申请号:US13979028

    申请日:2011-01-13

    摘要: We have developed a new method for the synthesis of Rasagiline (Formula 1) based on the alkylation of trifluoroacetyl protected aminoindan. This protection enabled us to carry out an alkylation of aminoindan with a high yield and purity under very mild conditions with a wide range of reaction conditions and reagent selection. Considering the ease, purity and high yields of introducing and removal of the trifluoroacetyl group, this approach is a highly practical and economical way for the synthesis of rasagiline or its pharmaceutically acceptable salts.

    摘要翻译: 我们已经开发了一种基于三氟乙酰基保护的氨基茚满烷基化合成雷沙吉兰(式1)的新方法。 这种保护使我们能够在非常温和的条件下,在广泛的反应条件和试剂选择下,以高产率和纯度进行氨基茚满烷基化。 考虑到引入和去除三氟乙酰基的容易性,纯度和高产率,该方法是合成雷沙吉兰或其药学上可接受的盐的高度实用和经济的方法。