“…30 This protocol is also suitable for the modification of peptides, as long as no acidic N–H-bond is present in the reacting amino acid. 31 To date, the best results have been obtained with amides of 8-aminoquinoline (AQ) 32 or 2-(methylthio)aniline (MTA), 33 with both directing groups developed by Daugulis et al 34 In general, (het)aryliodides or -bromides are employed for the functionalisation of cyclic or N -methylated amino acids at the β-position, whereas the introduction of alkyl groups is relatively rare. We were therefore inspired to determine if we could introduce a protected, highly functionalised side chain in a single step into a suitably protected alanine derivative, e.g.…”