676437-19-7Relevant academic research and scientific papers
Radiosynthesis of 3-(2′-[18F]fluoro)-flumazenil ([ 18F]FFMZ)
Wadsak, Wolfgang,Mitterhauser, Markus,Mien, Leonhard-Key,Toegel, Stefan,Keppler, Bernhard,Dudczak, Robert,Kletter, Kurt
, p. 1229 - 1240 (2003)
Recently, two fluorine-18 labelled derivatives of flumazenil were described: 5-(2′-[18F]fluoroethyl)-5-desmethylflumazenil (ethyl 8-fluoro-5-[18F]fluoroethyl-6-oxo-5, 6-dihydro-4H-benzo-[f]imidazo[1,5-a] [1,4]diazepine-3-carboxylate; [ 18F]FEFMZ) and 3-(2′-[18F]fluoro)-flumazenil (2′-[18F]fluoroethyl 8-fluoro-5-methyl-6-oxo-5, 6-dihydro-4H-benzo-[f]imidazo[1,5-a]-[1,4]diazepine-3-carboxylate; [ 18F]FFMZ). Since the biodistribution data of the latter were superior to those of the former we developed a synthetic approach for [ 18F]FFMZ starting from a commercially available precursor, thereby obviating the need to prepare a precursor by ourselves. The following two-step procedure was developed: First, [18F]fluoride was reacted with 2-bromoethyl triflate using the kryptofix/acetonitrile method to yield 2-bromo-[18F]fluoroethane ([18F]BFE). In the second step, distilled [18F]BFE was reacted with the tetrabutylammonium salt of 3-desethylflumazenil (8-fluoro-5-methyl-6-oxo-5,6-dihydro-4H-benzo-[f] imidazo[1,5-a] [1,4]diazepine-3-carboxylic acid) to yield [18F]FFMZ. The synthesis of [18F]FFMZ allows for the production of up to 7 GBq of this PET-tracer, enough to serve several patients. [18F]FFMZ synthesis was completed in less than 80 min and the radiochemical purity exceeded 98%. Copyright
