Direct access to ligand-like sulfonamide libraries <i>via</i> acid-catalyzed sulfinamide crossover

We introduce sulfinamide crossover as a new dynamic covalent reaction that rapidly generates ligand-like libraries <i>via</i> reversible S-N exchange under mild acid catalysis. The resulting mixtures can be oxidatively locked into medicinally relevant sulfonamides and directly screened by LC-MS.