Radiosynthesis of a Novel PET Fluoronicotinamide for Melanoma Tumour PET Imaging; [18F]MEL050
Ivan Greguric A C , Stephen Taylor A , Tien Pham A , Naomi Wyatt A , Cathy D. Jiang A , Thomas Bourdier A , Christian Loc'h A , Peter Roselt B , Oliver C. Neels B and Andrew Katsifis AA Radiopharmaceuticals Research Institute, Australian Nuclear Science and Technology Organisation, PMB 1 Menai, Sydney, NSW 2234, Australia.
B Centre for Molecular Imaging, Peter MacCallum Cancer Centre, Melbourne, Vic. 3002, Australia.
C Corresponding author. Email: ivg@ansto.gov.au
Australian Journal of Chemistry 64(7) 873-879 https://doi.org/10.1071/CH11048
Submitted: 28 January 2011 Accepted: 24 February 2011 Published: 19 July 2011
Abstract
[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.
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