The synthesis of (R)- and (S)-[N-methyl-11C]beta, beta-difluoromethamphetamine for the investigation of the binding mechanism of biogenic amines in vivo.

摘要: In an attempt to elucidate the contribution of extent nitrogen protonation on in vivo binding methamphetamine brain, enantiomers [N-methyl-11C]beta, beta-difluoroamphetamine (4) were prepared for use positron emission tomography (PET) studies. Thus, beta, from trans-beta-methylstyrene, via bromination, conversion into azirine, fluorination and resolution as tartrate salts. (R)- (S)-beta, (3) then each labelled with carbon-11 (tt/2 = 20.4 min) by N-methylation corresponding homochiral [11C]methyl iodide. The products synthesised, purified formulated 35 min, starting [11C]carbon dioxide 15-16% decay-corrected radiochemical yield, a purity > 99% specific radioactivity 50-150 GBq mumol-1 at end synthesis.