Synthesis of Florbetapir aza-analogues using chemistry of pyridinium N-aminides

Abstract

Neuroimaging of β-amyloid (Aβ) plaques in brain, employing Positron Emission Tomography (PET) has enabled early diagnosis of Alzheimer’s Disease and, although different 18F radiolabeled markers as Florbetapir and Florbetaben are already in the market, new molecules with better affinity and selectivity to Aβ plaques should be explored. In this article, two aza-analogues of Florbetapir have been synthesized from Pyridinium N-aminides. The new aza-analogues were prepared following straightforward synthetic routes under mild conditions. Although the products have been obtained using stable 19F, the methods are compatible with the future use of 18F, to generate products to be tested in the development of new PET reagents.