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    • 1. 发明授权
    • Process for production of bicyclo[2.2.2]octylamine derivative
    • 二环[2.2.2]辛胺衍生物的制备方法
    • US08476470B2
    • 2013-07-02
    • US13057879
    • 2009-08-07
    • Tomohiro AkeboshiYusuke IriyamaHirotaka Kawanami
    • Tomohiro AkeboshiYusuke IriyamaHirotaka Kawanami
    • C07C62/20
    • C07C229/50C07C227/16C07C227/22C07C249/02C07C251/20C07C303/28C07C309/66C07C2602/44
    • The present invention herein provides a process for production of a bicyclo[2.2.2]octylamine derivative which may be used as an intermediate for preparation of medical and pharmaceutical products. The process is quite efficient and can produce the derivative in a large-scale while using mild reaction conditions.The process for producing a bicyclo[2.2.2]octylamine derivative comprises the steps of subjecting, to ring-formation, a compound represented by the following general formula (1): [wherein R1 represents an alkyl group having 1 to 6 carbon atoms, which may have a substituent; an arylmethyl group which may have a substituent; or an arylethyl group which may have a substituent], and a compound represented by the following general formula (2): R2—NH2  (2) [wherein R2 represents an alkyl group having 1 to 6 carbon atoms, which may have a substituent; an aralkyl group which may have a substituent; a hydroxyl group; an alkyloxy group having 1 to 6 carbon atoms, which may have a substituent; or an aralkyloxy group which may have a substituent], and then reducing the resulting product.
    • 本发明提供了可用作制备医药产品的中间体的双环[2.2.2]辛胺衍生物的制备方法。 该方法是非常有效的,并且可以在使用温和的反应条件的情况下大量产生衍生物。 制备双环[2.2.2]辛胺衍生物的方法包括以下步骤:使由下列通式(1)表示的化合物进行成环:其中R 1表示具有1至6个碳原子的烷基, 其可以具有取代基; 可以具有取代基的芳基甲基; 或可以具有取代基的芳基乙基)和由以下通式(2)表示的化合物:R2-NH2(2)[其中R2表示可以具有取代基的碳原子数1〜6的烷基] 可以具有取代基的芳烷基; 羟基; 可以具有取代基的碳原子数1〜6的烷氧基; 或可具有取代基的芳烷氧基),然后还原所得产物。