Focused microwave irradiation of equimolecular mixtures of 9-chloroacridines, 4-chloroquinolines
and
4-chloroquinazolines with amines in the presence of 2 equiv of phenol allows the general, fast and
high- yielding synthesis of aminated heterocycles, with a very broad scope in terms of amine
structure (aro- matic, linear primary aliphatic, a-branched primary aliphatic, secondary aliphatic
and diamines). Workup consisted of a simple washing with water and purification could be achieved by
crystallization, avoiding the use of organic solvents in extraction and chromatographic purification
steps. This protocol provides a solution to the long-standing synthetic problem of achieving a
practical and efficient method for the amination of p-deficient nitrogen heterocycles for medicinal
chemistry applications.