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Efficient synthesis of 2‐bromo‐1‐[ 18 F]fluoroethane and its application in the automated preparation of 18 F‐fluoroethylated radiopharmaceuticals
Author(s) -
Comagic S.,
Piel M.,
Schirrmacher R.,
Höhnemann S.,
Rösch F.
Publication year - 2001
Publication title -
journal of labelled compounds and radiopharmaceuticals
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.432
H-Index - 47
eISSN - 1099-1344
pISSN - 0362-4803
DOI - 10.1002/jlcr.25804401307
Subject(s) - chemistry , cartridge , acetonitrile , distillation , fluoride , radiochemistry , chemical synthesis , chromatography , inorganic chemistry , mechanical engineering , biochemistry , engineering , in vitro
Abstract An efficient synthesis of 2‐bromo‐1‐[ 18 F]fluoroethane from commercially available 1,2‐dibromoethane and its integration into an automated preparation device was developed for the routine synthesis of 18 F‐fluoroethylated radiopharmaceuticals. The precursor 1,2‐dibromoethane was reacted with the [ 18 F]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‐[ 18 F]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 18 F‐fluoroalkylated radiopharmaceuticals.