Fragment-oriented synthesis: β-elaboration of cyclic amine fragments using enecarbamates as platform intermediates.
Alexandre F TrindadeEmily L FaulknerAndrew G LeachAdam NelsonStephen P MarsdenPublished in: Chemical communications (Cambridge, England) (2020)
A strategy for the β-sp3 functionalisation of cyclic amines is described. Regioselective conversion of protected amines to enecarbamates is achieved through electrochemical oxidation; these intermediates can be derivatised by functionalised alkyl halides under photoredox catalysis. The potential of the methods is highlighted by direct growth of a DCP2B-binding fragment.