A metal-free, mild, facile, and cost-effective one-pot hypervalent-iodine-mediated transformation was developed for the synthesis of pyridoquinazolinones from 2-chloropyridines at room temperature. This reported protocol can produce biologically active pyridoquinazolinones in a single step from readily available starting materials.

A mild, cost-effective, one-pot, and metal-free hypervalent iodine-mediated protocol for the production of pyridoquinazolinones from 2-aminobenzaldehydes and 2-chloropyridines at room temperature has been established. This reported procedure can easily produce biologically active pyridoquinazolinones in a one-pot manner utilizing readily available starting materials. Operational simplicity, moderate reaction conditions, high atom economy, and high yield are some key features of this protocol. The generation of AcOH and HCl as the only by-products makes this a cost-effective procedure for the production of pyridoquinazolinones.