Abstract
Condensation of phenylazo-β-ketoamide 4 with oxymorphone 5 afforded an m-iodophenylpyrrolomorphinan (m-IPPM) 6 mediated by elemental zinc in acetic acid/sodium acetate buffer. m-IPPM 6 is a novel opioid receptor agonist (K i = 4.53 nM for DOP) with high selectivity for DOP receptors. m-IPPM 6 was converted into the positron emitter m-[124I]PPM 8 via the stannylated intermediate 7. The final yield was 24.5 ± 1.9 % (n = 6) with a specific activity of 2.5 ± 1.2 Ci/μmol.
Original language | English (US) |
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Pages (from-to) | 165-170 |
Number of pages | 6 |
Journal | Journal of Labelled Compounds and Radiopharmaceuticals |
Volume | 50 |
Issue number | 3 |
DOIs | |
State | Published - Mar 2007 |
Keywords
- DOP receptor agonist
- Iodine-124
- Positron emission tomography
- m-IPPM