Sulfonamides are pervasive in drugs and agrochemicals,
yet are typically considered as terminal functional groups rather than
synthetic handles. To enable the general late-stage functionalization of
secondary sulfonamides, we have developed a mild and general method to
reductively cleave the N-S bonds of sulfonamides to generate sulfinates and
amines, components which can further react <i>in-situ</i>
to access a variety of other medicinally relevant functional groups. The
utility of this platform is highlighted by the selective manipulation of
several complex bioactive molecules.