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The synthesis of tritiated ( R )‐2‐methoxy‐ N ‐ n ‐propyl‐nor‐apomorphine (MNPA)
Author(s) -
Malmquist Jonas,
Olofsson Susanne,
Ström Peter
Publication year - 2007
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/jlcr.1448
Subject(s) - chemistry , high performance liquid chromatography , apomorphine , column chromatography , chromatography , ascorbic acid , structural isomer , mass spectrometry , tritium , stereochemistry , biochemistry , receptor , food science , agonist , physics , nuclear physics
A method for the preparation of [ 3 H]‐MNPA (( R )‐2‐methoxy‐ N ‐ n ‐propyl‐norapomorphine) has been developed addressing the regioisomer problem as well as the oxidation problem. ( R )‐2, 10, 11‐trihydroxy‐ N ‐ n ‐propyl‐norapomorphine was protected with 10, 11‐dibenzyl or 10, 11‐acetonide. The pure precursor was then methylated using [ 3 H]‐methyliodide. The product was isolated after deprotection and high‐pressure liquid chromatography (HPLC) purification. Ascorbic acid was used as an antioxidant in the HPLC eluent and the stock solution. Characterization of the intermediates and products with 3 H‐ and 1 H‐NMR was performed. A specific activity of 3.1 TBq/mmol (83.8 Ci/mmol) and 98.9% purity was obtained. Copyright © 2007 John Wiley & Sons, Ltd.