Radiosynthesis of a novel PET fluoronicotinamide for melanoma tumour PET imaging [18F]MEL050

[18F]6-Fluoro-N-[2-(diethylamino)ethyl]nicotinamide [18F]MEL050 is a novel nicotinamide-based radiotracer, designed to target random metastatic dissemination of melanoma tumours by targeting melanin. Preclinical studies suggest that [18F]MEL050 has an excellent potential to improve diagnosis and staging of melanoma. Here we report the radiochemical optimization conditions of [18F]MEL050 and its large scale automated synthesis using a GE FXFN automated radiosynthesis module for clinical, phase-1 investigation. [18F]MEL050 was prepared via a one-step synthesis using no-carrier added K[18F]F-Krytpofix® 222 (DMSO, 170°C, 5 min) followed by HPLC purification. Using 6-chloro-N-[2-(diethylamino)ethyl]nicotinamide as precursor, [18F]MEL050 was obtained in 40–46% radiochemical yield (non-decay corrected), in greater than 99.9% radiochemical purity and specific activity ranging from 240 to 325 GBq μmol–1. Total synthesis time including formulation was 40 min and [18F]MEL050 was stable (99.8%) in PBS for 6 h. © 2011, CSIRO Publishing

Keywords

Positron computed tomography, Metastases, Melanomas, Synthesis, Renal clearance, Therapy

Citation

Greguric, I., Taylor, S., Pham, T., Wyatt, N., Jiang, C. D., Bourdier, T., Loc'h, C., Roselt, P., Neels, O. C., & Katsifis, A. (2011). Radiosynthesis of a novel PET fluoronicotinamide for melanoma tumour PET imaging [18F]MEL050. Australian Journal of Chemistry, 64 (7), 873-879. doi:10.1071/CH11048