Selective acetylation of small biomolecules and their derivatives catalyzed by Er(OTf)3

Abstract

It is of great significance to develop sustainable processes of catalytic reaction. We report a selective procedure for the synthesis of acetylated bioactive compounds in water. The use of 1‐acetylimidazole combined with Er(OTf)3 as a Lewis acid catalyst gives high regioselectivity and good yields for the acetylation of primary hydroxyl groups, as well as amino groups. The protection is achieved in short reaction times under microwave irradiation, and is successful even in the case of base‐sensitive substrates.