Reimagining synthetic strategy with skeletal editing ticks box on chemists’ wish list

A strategic atom swap solves a longstanding selectivity problem in the synthesis of complex pyrazoles and is something that has been on the wish list of medicinal chemists for some time. The formal sulfur–nitrogen exchange leveraged asymmetry in the starting material to regioselectively install functionality on one of two resonance-related nitrogen atoms. The team believes this broad conceptual approach, reimagining skeletal editing as a tool to solve early-stage selectivity challenges, could be applied to other substrate classes and heteroatom systems.