Solid-phase synthesis of aryl-alkylamine derivatives using protected aminoalcohol building blocks on SynPhaseTM lanterns

A series of aryl-alkylamine carboxamide and sulfonamide derivatives were synthesized on a BAL linker using SynPhase (TM) Lanterns. All the reaction steps were performed on a solid support. The key stage was on-resin substitution of TBDPSi-protected aminoalcohols with various amines, which circumvented the multistep solution-phase synthesis of alkylamine building blocks. The chemistry applied allows building up focused libraries targeted on CNS receptors.