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    • 2. 发明授权
    • Method for preparing 4-alkoxyalkyl-4-phenylaminopiperdines and
derivatives thereof
    • 4-烷氧基烷基-4-苯基氨基哌啶及其衍生物的制备方法
    • US5145967A
    • 1992-09-08
    • US608427
    • 1990-11-02
    • Bor-Sheng LinH. Kenneth SpencerJoseph W. Scheblein
    • Bor-Sheng LinH. Kenneth SpencerJoseph W. Scheblein
    • C07D211/58
    • C07D211/58
    • The present invention is directed to a method for preparing a 4-alkoxyalkyl-4-phenylaminopiperidine compound which comprises the steps of (a) reacting an N-substituted-4-piperidone compound with an aniline compound to form a Schiff base compound, (b) reacting the Schiff base compound with an anionic reagent having an anion stabilizing group to form an amine compound, and (c) reducing the amine compound in step (b) with a reducing agent to displace the anion stabilizing group.The anionic reagent in step (b) above has the general formula:X--CYM--Zwherein X is an anion stabilizing group, Y is hydrogen or lower-alkyl, Z is lower-alkoxy or phenylmethoxy, M is an alkali or alkaline earth metal, and C is a carbon atom.
    • 本发明涉及一种制备4-烷氧基烷基-4-苯基氨基哌啶化合物的方法,该方法包括以下步骤:(a)使N-取代-4-哌啶酮化合物与苯胺化合物反应形成希夫碱化合物,(b )使希夫碱化合物与具有阴离子稳定基团的阴离子试剂反应以形成胺化合物,和(c)用还原剂还原步骤(b)中的胺化合物以置换阴离子稳定基团。 上述步骤(b)中的阴离子试剂具有以下通式:X-CYM-Z其中X为阴离子稳定基团,Y为氢或低级烷基,Z为低级烷氧基或苯基甲氧基,M为碱金属或碱土金属 金属,C为碳原子。