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The synthesis of tritiated (R)-2-methoxy-N-n-propyl-nor-apomorphine (MNPA)

✍ Scribed by Jonas Malmquist; Susanne Olofsson; Peter Ström

Publisher
John Wiley and Sons
Year
2007
Tongue
French
Weight
104 KB
Volume
50
Category
Article
ISSN
0022-2135

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✦ Synopsis

Abstract

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.

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