Pd-catalysed C–C macrocyclisation of a simple tripeptide: efficient total synthesis of K-13

Abstract

The cyclic tripeptide K-13 has been prepared in 11 steps from commercially available starting materials (11% overall yield); the key step is the Pd-catalysed macrocyclisation of the zinc reagent prepared by selective insertion of zinc into the aliphatic C–I bond of the linear tripeptide 3, followed by Pd-catalysed macrocyclisation.