Novel benzoxazino quinoline derivatives of Formula (I) and benzoxazino isoquinoline derivatives of Formula (II) are provided:Also provided is a transition-metal-free multicomponent reaction of arynes, N-heterocycles, and carbonyl compounds leading to the diastereoselective synthesis of benzoxazino quinoline derivatives of Formula (I) and benzoxazino isoquinoline derivatives of formula (II) in good yields proceeding via 1,4-zwitterionic intermediates. The compounds possess anti-malarial activity.
