Solid-phase synthesis of symmetrical and unsymmetrical polyamine analoguesof philanthotoxins using a Dde-linker

The efficient construction of symmetrical & unsymmetrical polyamine analogu es of philanthotoxins has been accomplished using the new Dde based linker. The linker allows the selective attachment of primary amines and the resul ting linkage displays excellent stability towards the conditions required f or the removal of Fmoc and Boc groups as well as the reductive alkylation c onditions used for the elaboration of polyamines. The final cleavage of the polyamine or a derivative thereof from the solid support is readily achiev ed via transamination using a volatile primary amine with the regeneration of the linker. (C) 2000 Elsevier Science Ltd. All rights reserved.