The present invention relates to the compound of dialkyl(2-alkoxy-6-aminophenyl)phosphine and the preparation method thereof and the application in the palladium catalyzed coupling reactions of aryl chloride and ketone. The dialkyl(2-alkoxy-6-aminophenyl)phosphine of the present invention could coordinate with the palladium catalyst to highly selectively activate the inert carbon-chlorine bond, and to catalyze direct arylation reaction in the α-position of ketones to produce corresponding coupling compounds. The preparation method of the present invention is a simple one-step method which produces the air-stable dialkyl(2-alkoxy-6-aminophenyl)phosphine. Compared with the synthetic routes of ligands to be used in the activation of carbon-chlorine bonds in the prior arts, the preparation method of the present invention has the advantages of short route and easy operation.
本发明涉及二烷基(2-烷氧基-6-
氨基苯基)膦化合物及其制备方法,以及在
钯催化芳基
氯化物和酮的偶联反应中的应用。本发明的二烷基(2-烷氧基-6-
氨基苯基)膦化合物能够与
钯催化剂配位,高度选择性地活化惰性碳-
氯键,并催化酮的α位直接芳基化反应,生成相应的偶联化合物。本发明的制备方法是一种简单的一步法,可制备出稳定于空气中的二烷基(2-烷氧基-6-
氨基苯基)膦化合物。与先前用于活化碳-
氯键的
配体的合成路线相比,本发明的制备方法具有路线短、操作简便的优点。