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Fragment-oriented synthesis: β-elaboration of cyclic amine fragments using enecarbamates as platform intermediates.

Alexandre F TrindadeEmily L FaulknerAndrew G LeachAdam NelsonStephen P Marsden
Published 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.
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