A brief historical review of the Ramberg-Backlund rearrangement is presente
d along with a summary of its applications to the synthesis of bioactive ta
rget molecules. Recent developments in this area originating from the autho
r's laboratories, mostly from the past five years, are reviewed. These incl
ude: (i) the isolation of episulfones from the Ramberg-Backlund rearrangeme
nt, (ii) the preparation of episulfones by the oxidation of episulfides, (i
ii) the generation and synthetic applications of episulfone alpha-anions, (
iv) the epoxy-Ramberg-Backlund rearrangement, (v) the tandem conjugate addi
tion-Ramberg-Backlund rearrangement, and (vi) utilisation of the Ramberg-Ba
cklund rearrangement in natural product synthesis and related areas, includ
ing recent applications for the synthesis of C-glycosides.