Abstract

Orthogonally protected, N-hydroxylated, linear tri- and tetra-amines were efficiently synthesised on Merrifield resin, which was modified with a phenethyl bromide linker. The polyamine frameworks were convergently prepared from the centre with reductive aminations and nucleophilic substitutions to elongate the polyamine backbone. The required N-hydroxy groups were introduced during the cleavage of the polyamine derivatives from the resin through Cope elimination.