[EN] PROCESS FOR MANUFACTURING ADAMANTANE DERIVATIVES WITH HIGH YIELD<br/>[FR] PROCÉDÉ POUR LA FABRICATION DE DÉRIVÉS D'ADAMANTANE AVEC UN RENDEMENT ÉLEVÉ
申请人:MERZ PHARMA GMBH & CO KGAA
公开号:WO2010015415A1
公开(公告)日:2010-02-11
The present invention pertains to process for the amidation of a substituted 1-bromo-adamantane comprising a step (0) of reacting a substituted adamantane with an excess of bromine to obtain a 1-bromo-adamantane and a step (i) of reacting said substituted 1-bromo-adamantane with an amide, wherein the substituted 1-bromo-adamantane is used in the form of a mixture comprising bromine as obtained in step (0), wherein in step (0) a bromine: substituted adamantane molar ratio of from [2.5:1] to less than [5:1] is employed.
本发明涉及一种取代的
1-溴金刚烷的酰胺化过程,包括步骤(0)反应取代
金刚烷和过量
溴化合成
1-溴金刚烷,以及步骤(i)反应所述取代的
1-溴金刚烷与酰胺反应,其中所述取代的
1-溴金刚烷以步骤(0)得到的含有
溴的混合物的形式使用,其中在步骤(0)中使用
溴:取代
金刚烷的摩尔比为[2.5:1]至少于[5:1]。