TY - JOUR
AU - Kletter, Kurt
AB - 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‐carbo‐ xylate; (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 © 2003 John Wiley & Sons, Ltd.
TI - Radiosynthesis of 3‐(2′‐( 18 F)fluoro)‐flumazenil (( 18 F)FFMZ)
JF - Journal of Labelled Compounds and Radiopharmaceuticals
DO - 10.1002/jlcr.783
DA - 2003-11-01
UR - https://www.deepdyve.com/lp/wiley/radiosynthesis-of-3-2-18-f-fluoro-flumazenil-18-f-ffmz-s3xvvSF06A
SP - 1229
EP - 1240
VL - 46
IS - 13
DP - DeepDyve
ER -