RADIOSYNTHESIS OF [H-3]METHCATHINONE, AN INHIBITOR OF MONOAMINE REUPTAKE TRANSPORTERS

[H-3]Methcathinone (2-[H-3]methylamino-1-phenylpropan-1-one) an inhibi tor of monoamine reuptake transporters, was synthesized by N-methylati on of cathinone using [H-3]methyl iodide in toluene/methanol. A two-st ep purification procedure employing preparative silica gel TLC, follow ed by reverse-phase HPLC, was developed to separate [H-3]methcathinone from unreacted starting material and side products. We were able to g enerate radio- and chemically pure [H-3]methcathinone, ready for use i n pharmacological experiments, in about eight hours. Overall yield was about 4% based on [H-3]methyl iodide.