【摘要】 <正> Mannioh反应是一个在合成中多方面适用的反应.但许多人认为芳胺不能作为胺组分参加这个反应.Tramontini近期的综述中提到芳胺参加Mannich反应的例子,其酸性组分均是酚类而非典型的酮类.等曾报道苯胺或其衍生物直接与酮的Mannich碱盐酸盐反应而生成β-芳胺基苯丙酮.该方法实即文献记载的胺交换方法更多还原

【Abstract】 Mannich reaction occurs readily between aromatic primary amine, formaldehyde and alkylarylketone by the following method: arylamine was condensed with formaldehyde in ethanol at room temperature to form 3 or 5. On adding a solution of alkylarylketone in ethanolic HCl, β-arylaminoketone hydrochlorides were formed in high yields. This is a new method for direct synthesis of β-arylaminoketones through Mannich reaction.By this method, β-arylaminoketones were prepared from various para substituted arylamine RC₆H₄NH₂, where R=H, Me, OMe, Br, Cl and m- or p-nitroaniline. Alkylarylketones such as acetophenone, propiophenone and p-nitroacetophenone were used in the reaction.This result substantiates the proposal in our previous work that the exchange reaction between benzimidazole N-Mannich base and arylamine proceeds by an elimination-addition mechanism.更多还原