Radiation dosimetry of para-chloro-2-[F]fluoroethyl-etomidate: a PET tracer for adrenocortical imaging.

Background: [C]metomidate, a methyl ester analogue of etomidate, is used for positron emission tomography of adrenocortical cancer, and has been tested in recent clinical trials for lateralization in primary aldosteronism (PA). However, in PA, visualization as well as uptake quantification are hampered by the tracer's rather high non-specific liver uptake, and its overall clinical usefulness is also limited by the short 20-minute half-life of carbon-11. Therefore, we evaluated para-chloro-2-[F]fluoroethyl-etomidate, [F]CETO, a fluorine-18 (T=109.

Acyl Amidines by Pd-Catalyzed Aminocarbonylation: One-Pot Cyclizations and C Labeling.

A protocol for the carbonylative synthesis of acyl amidines from aryl halides, amidines, and carbon monoxide catalyzed by Pd(0) is reported herein. Notably, carbon monoxide is generated ex situ from a solid CO source, and several productive palladium ligands were identified with complementary benefits and substrate scope. Furthermore, sequential one-pot, two-step protocols for the synthesis of 1,2,4-triazoles and 1,2,4-oxadiazoles via acyl amidine intermediates are reported.

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

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.

First-in-human evaluation of [F]CETO: a novel tracer for adrenocortical tumours.

Purpose: [C]Metomidate positron emission tomography (PET) is currently used for staging of adrenocortical carcinoma and for lateralization in primary aldosteronism (PA). Due to the short half-life of carbon-11 and a high non-specific liver uptake of [C]metomidate there is a need for improved adrenal imaging methods. In a previous pre-clinical study para-chloro-2-[F]fluoroethyletomidate has been proven to be a specific adrenal tracer.