6533b871fe1ef96bd12d1811

RESEARCH PRODUCT

Efficient synthesis of 2-bromo-1-[18F]fluoroethane and its application in the automated preparation of 18F-fluoroethylated radiopharmaceuticals

S. HöhnemannFrank RöschS. ComagicRalf SchirrmacherMarkus Piel

subject

ChemistryOrganic ChemistryBiochemistryAnalytical Chemistrylaw.inventionchemistry.chemical_compoundlawDrug DiscoveryRadiology Nuclear Medicine and imagingAcetonitrileFluorideDistillationSpectroscopyNuclear chemistry

description

An efficient synthesis of 2-bromo-1-[18F]fluoroethane from commercially available 1,2-dibromoethane and its integration into an automated preparation device was developed for the routine synthesis of 18F-fluoroethylated radiopharmaceuticals. The precursor 1,2-dibromoethane was reacted with the [18F]fluoride/Kryptofix®2.2.2./carbonate-complex in acetonitrile at 70°C for 3 minutes. The crude reaction mixture was diluted with water, loaded on a LiChrolute ®EN-cartridge, eluated with acetonitrile and passed through an Alumina ®B-cartridge. The method can provide 2-bromo-1-[18F]fluoroethane with 98% radiochemical purity completely free of 1, 2-dibromoethan within 10 min, thus avoiding a purifying distillation step. This method was easily integrated into an automated system for the routine synthesis of 18F-fluoroalkylated radiopharmaceuticals.

https://doi.org/10.1002/jlcr.25804401307