S. Dekeczer et H. Parnes, SYNTHESIS OF [4,6-H-3]-2-PYRIDONE AND [H-3] RS-91309, Journal of labelled compounds & radiopharmaceuticals, 36(8), 1995, pp. 765-772
Citations number
4
Categorie Soggetti
Chemistry Analytical","Pharmacology & Pharmacy","Biochemical Research Methods
We describe herein, a novel synthesis of the previously unreported com
pound, 4,6-dibromo-2-pyridone (3) and its use in the preparation of [H
-3]-RS-91309, a potassium channel modulator. This key intermediate, (3
), was reduced with carrier free tritium gas to furnish [4,6-H-3]-2-py
ridone (9) having a specific activity of 50 Ci/mmole. Condensation of
(9) with epoxide (10), followed by elaboration of the resulting chrome
ne methyl group of (12) gave [H-3]-RS-91309 (14) whose specific activi
ty was also 50 Ci/mmole. This chemistry, as well as the solution of se
veral microscale related stoichiometry problems is discussed.