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Application of the Bischler–Napieralski–Pschorr radiosynthesis of (R)-(-)-[6a-14C]apomorphine, a non-selective D1/D2 dopamine receptor agonist

✍ Scribed by Sean L. Kitson; Eric Knagg

Book ID: 102367874
Publisher: John Wiley and Sons
Year: 2006
Tongue: French
Weight: 198 KB
Volume: 49
Category: Article
ISSN: 0022-2135
DOI: 10.1002/jlcr.1070

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✦ Synopsis

A method has been developed for the carbon-14 radiosynthesis of non-narcotic morphine derivative (R)-(-)-[6a-14 C]apomorphine ð1Þ from the starting material 3,4-dimethoxy-2-nitrophenyl-N-phenethyl[carboxyl-14 C]acetamide ð5Þ. The key to this synthesis was the application of the Bischler-Napieralski cyclodehydration to 1-(3,4dimethoxy-2-nitrobenzyl)dihydro[1-14 C]isoquinoline ð4Þ, followed by N-methylation and reduction to 1-(3,4-dimethoxy-2-nitrobenzyl)-2-methyl-1,2,3,4-tetrahydro[1-14 C] isoquinoline ð3Þ. A final Pschorr reductive ring closure followed by chiral separation to give (R)-(-)-[6a-14 C]apomorphine dimethyl ether ð2Þ and O-demethylation led to (R)-(-)-[6a-14 C]apomorphine ð1Þ with a specific activity of 55 mCi/mmol, radiochemical purity of >98% and chiral purity of >99%.

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