Synthese im Blickpunkt: Bioisosteres of meta‐substituted benzenes

Abstract Swapping aromatic rings with small‐ring hydrocarbon cages is a promising method for synthesising more effective drugs. Until recently, however, this tactic was restricted to the replacement of para‐substituted phenyl groups. Now, two new methods describe reliable syntheses of a motif for exchanging meta‐substituted benzene rings, ushering a new cage‐motif into the mainstream and thus opening up opportunities for medicinal chemists.