Iodine(III)-mediated ring expansion: an efficient and green pathway in the synthesis of a key precursor for the design of aminopeptidase (APN or CD13) inhibitors

Iodine(III)-mediated ring expansion of a methylidenebenzocyclohexane derivative into the corresponding benzosuberone was used as a key reaction for the obtention of an important precursor for the design of aminopeptidase (APN or CD13) inhibitors. It represents the first application of this environmentally friendly rearrangement to medicinal chemistry.