A brief historical review of the Ramberg–Bäcklund rearrangement is presented along with a summary of its applications to the synthesis of bioactive target molecules. Recent developments in this area originating from the author’s laboratories, mostly from the past five years, are reviewed. These include: (i) the isolation of episulfones from the Ramberg–Bäcklund rearrangement, (ii) the preparation of episulfones by the oxidation of episulfides, (iii) the generation and synthetic applications of episulfone α-anions, (iv) the epoxy-Ramberg–Bäcklund rearrangement, (v) the tandem conjugate addition-Ramberg–Bäcklund rearrangement, and (vi) utilisation of the Ramberg–Bäcklund rearrangement in natural product synthesis and related areas, including recent applications for the synthesis of C-glycosides.