Palladium-Mediated Synthesis of [Carbonyl-¹¹C]acyl Amidines from Aryl Iodides and Aryl Bromides and Their One-Pot Cyclization to ¹¹C-Labeled Oxadiazoles.

ABSTRACT: Positron emission tomography (PET) is a highly valuable imaging technique with many clinical applications. The possibility to study physiological and biochemical processes in vivo also makes PET an important tool in drug discovery. Of importance is the possibility of labelling the compound of interest with a positron-emitting radionuclide, such as carbon-11. Carbonylation reactions with [¹¹C]carbon monoxide ([¹¹C]CO) has been used to label a number of molecules containing a carbonyl derivative, such as amides and esters, with carbon-11. Presented herein is the palladium-mediated carbonylative synthesis of [carbonyl-¹¹C]acyl amidines and their subsequent cyclization to ¹¹C-labeled 1,2,4-oxadiazoles. Starting from amidines, [¹¹C]CO, and

SUBMITTER: Rydfjord J 

PROVIDER: S-EPMC10127284 | biostudies-literature | 2023 Apr

REPOSITORIES: biostudies-literature