PALLADIUM-CATALYZED AMINOCARBONYLATION OF NITROGEN-CONTAINING ARYL HALIDES USING [~11C]BH_3CO AS SOURCE OF CARBON MONOXIDE

摘要

Recent developmental work in PET radiochemistry has demonstrated the utility of [~11C]carbon monoxide as a building block for the synthesis of [~11C]carbonyl compounds despite reactivity and methodological limitations (1). An ongoing project focussed on new techniques to trap and react this versatile building block has established [~11C]BH_3CO as a good alternative to autoclaving methods with [~11C]CO for palladium-catalysed carbonylation reactions (2,3). Further developmental work has been performed in order to optimize the radiochemical yields and to show that iV-containing heterocycles commonly used in medicinal chemistry programmes can be labelled using this method (scheme 1).