Synthesis of 18O-labelled alcohols from unlabelled alcohols.
Rhydian H BeddoeDaniel C EdwardsLouis GoodmanHelen F SneddonRoss M DentonPublished in: Chemical communications (Cambridge, England) (2020)
The synthesis of primary, secondary and tertiary 18O-enriched alcohols from readily available 16O-alcohols via a Mitsunobu esterification and hydrolysis is described. The method is further exemplified in the labelling of the active pharmaceutical ingredient, dropropizine and is shown to be tolerant of modern, separation friendly Mitsunobu reagents.