Brønsted acid catalysed chemo- and ortho-selective aminomethylation of phenol.

We have developed a Bronsted acid catalysed highly ortho-selective functionalization of free phenols with readily available N,O-acetals under mild conditions, furnishing various corresponding aminomethylated phenol products in moderate to excellent yields. The salient features of this transformation include mild conditions, good substrate scope, excellent ortho-selectivity, high efficiency, and ease of further transformation.