Fig. 1. Introduction to scaffold hopping and single-atom skeletal editing.
(A) Schematic representation of the disconnect between design and synthesis in molecular optimization. (B) Selected examples of scaffold hopping in medicinal chemistry. HMG-CoA, 3-hydroxy-3-methylglutaryl coenzyme A; Me, methyl group; COX-2, cyclooxygenase-2. (C) Single-atom skeletal editing for heterocycle interconversion. (D) Carbon deletion of azaarenes delineated in this work.