Authors: Federico Luzi, Antony Gee, Salvatore Bongarzone
King’s College London
Background
Formamides are common motifs of biologically-active compounds (e.g. formoterol, octotiamine, fursaltiamine etc)1 and are frequently employed as intermediates to yield, for example, benzimidazoles.2
A rapid, simple and reliable route to [carbonyl-11C]formamides would enable access to this important class of compounds as in vivo PET imaging agents.
Aims
We report the rapid, one-pot 11C-formylation of amines via the reduction of [11C]isocyanate intermediates formed directly from cyclotron-produced [11C]CO2.
The method was applied to the radiolabelling of a small library of formamides and the chemotactic molecule formyl methionine.