Efficient and Flexible Solid‐Phase Synthesis of N‐Hydroxypolyamine Derivatives

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.(© Wiley‐VCH Verlag GmbH & Co. KGaA, 69451 Weinheim, Germany, 2008)