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Radiosynthesis of [ 3 H]methcathinone, an inhibitor of monoamine reuptake transporters
Author(s) -
Cozzi Nicholas V.,
Ruoho Arnold E.
Publication year - 1998
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/(sici)1099-1344(1998100)41:10<927::aid-jlcr140>3.0.co;2-a
Subject(s) - chemistry , methyl iodide , monoamine neurotransmitter , reuptake inhibitor , chromatography , nuclear chemistry , pharmacology , organic chemistry , serotonin , biochemistry , receptor , medicine
[ 3 H]Methcathinone (2‐[ 3 H]methylamino‐1‐phenylpropan‐1‐one), an inhibitor of monoamine reuptake transporters, was synthesized by N ‐methylation of cathinone using [ 3 H]methyl iodide in toluene/ methanol. A two‐step purification procedure employing preparative silica gel TLC, followed by reverse‐phase HPLC, was developed to separate [ 3 H]methcathinone from unreacted starting material and side products. We were able to generate radio‐ and chemically pure [ 3 H]methcathinone, ready for use in pharmacological experiments, in about eight hours. Overall yield was about 4% based on [ 3 H]methyl iodide.Copyright © 1998 John Wiley & Sons, Ltd.