SYNTHESIS OF 'C-AMIDES USING [~(11)C]BORANE CARBONYL ([~(11)C]BH_3CO) AS A CO SOURCE

摘要

Recent literature reports have described [~(11)C]carbon monoxide as a practical building block for the synthesis of radiolabelled compounds for positron emission tomography (PET). A wide range of compounds have been prepared by palladium-/selenium-promoted carbonylation reactions using dedicated automated robotic systems. Difficulties encountered with the trapping [~(11)C]CO gas in a small solvent volume were overcome using high-pressure or recirculation systems. As an alternative we have developed a new method to convert [~(11)C]CO to [~(11)C]BH_3CO and to react this boron-based carbonylating complex in palladium-mediated reactions at atmospheric pressure (Scheme 1).