Facile Pd-catalyzed amination of imidazolin-1-yl chloroazines under microwave irradiation: Toward a new kinase-inhibitory chemotype

Abstract

The imidazolin-1-yl azine moiety, constructed using a recently developed Buchwald–Hartwig-type arylation methodology, displays excellent chemical stability under subsequent microwave-assisted Pd-catalyzed amination with a range of N-nucleophiles. This finding extends the usage of imidazolin-1-yl azines for bioactive compound library design. The latter is exemplified herein by the discovery of micromolar kinase inhibitors.