M. W. Moon, R. Hsi
Nov 1, 1992
Citations
0
Influential Citations
10
Citations
Journal
Journal of Labelled Compounds and Radiopharmaceuticals
Abstract
(R)-5-(diallylamino)-5,6-dihydro-4H-imidazo[4,5,1-ij]quinolin-2(1H)-one (12b) was prepared in 9% overall yield from 3-aminoquinoline. Reaction of 12b in ethyl acetate with tritium gas in presence of a 5% platinum on carbon catalyst afforded a mixture of (R)-5-(di[2,3-3H2]propylamino)-5,6-dihydro-4H-imidazo[4,5,1-ij]-quinolin-2(1H)-one ([3H]U-86170, 13, 69 Ci/mmol) and (R)-5-([2,3-3H2]-propyl-amino)-5,6-dihydro-4H-imidazo-[4,5,1-ij]quinolin-2(1H)-one ([3H]U-91356, 14, 34 Ci/mmol) which was separated by preparative reverse-phase chromatography. U-86170 and U-91356 are potent dopamine D2 agonists. The labelled compounds are useful for drug disposition studies. [3H]U-86170 is also useful as a dopamine D2 agonist radioligand for receptor binding studies.