Tritium labeling of a class of spirooxazaindolamines possessing analgesic properties.

In order to study the mol. action of a class of spirooxazaindolamines with promising analgesic activity, tritiated material was prepd. Efficient synthesis of 3H-labeled material allowed essential information on the mol. mechanism for this class of compds. to be obtained. Different approaches for the introduction of the 3H-label on the spirooxazaindole skeleton via 3H-methyliodide were evaluated involving lithium-mediated coupling, zinc-mediated coupling and Stille coupling. Tritiation using 3H2 (g) with a Pd-catalyst was also tested. [on SciFinder(R)]