Direct Organocatalytic Asymmetric para C-H Aminoalkylation of Aniline Derivatives Affording Diarylmethylamines

An efficient method to directly catalyze asymmetric para C-H aminoalkylation of aniline derivatives to prepare chiral diarylmethylamine system was developed. Aniline derivatives underwent an enantioselective aminoalkylation in the presence of chiral phosphoric ac-id, affording a series of optically active diarylmethylamine products in good yields and enantioselectivities (73% yield, 91% ee). Furthermore, this method could be used to prepare the key intermediate of chiral drug levocetirizine.