From [¹¹C]CO₂ to [¹¹C]amides: a rapid one-pot synthesis via the Mitsunobu reaction

Abstract

A novel amide synthesis methodology is described using amines, CO₂ and Grignard reagents and Mitsunobu reagents. The method was applied to carbon-11 radiochemistry to label amides using cyclotron-produced [¹¹C]CO₂. The synthetic utility of the one-pot labelling methodology was demonstrated by producing [¹¹C]melatonin. The incorporation of [¹¹C]CO₂ into [¹¹C]melatonin was 36% - determined by radioHPLC 2 min post [¹¹C]CO₂ delivery.