Dialkyl(2-alkoxy-6-aminophenyl)phosphine, the preparation method and use thereof

摘要

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.

主权项

1. A dialkyl(2-alkoxyl-6-aminophenyl)phosphine compound of the formula: wherein each of R1 and R2 is independently selected from the group consisting of isopropyl, tertbutyl, cyclopentyl, or cyclohexyl; R3 is either alkyl or aryl; each of R4 and R5 is independently selected from alkyl or aryl; R6 is selected from substituted alkyl, alkoxyl, aryl, amino, thiol, carbonyl or cyano, with unfixed substituent position, the number is 0-3.