An efficient and flexible route to novel triazolopiperazine scaffolds

Abstract

In this work we describe the preparation of novel fused, spirocyclic and chiral triazolopiperazines. We have developed a practical, rapid and robust synthetic route to these scaffolds that allows control of regio- and stereochemistry. This method utilises mild conditions and uses widely available and diverse amino acids and amidines as starting materials. These complex unprecedented 5,6,7,8-tetrahydro-[1–2,4]triazolo[1,5-a]pyrazines represent attractive building blocks for drug discovery.