4,5-dihydro-1H-imidazole-2-sulfonic acid → Brimonidine

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A mixture of 6-amino-5-bromo quinoxaline (prepared using the method reported by Danielewicz U.S. Pat. No. 3,890,319) (0.224 g, 2 mmol), imidazoline-2-sulfonic acid (0.30 g, 2 mmol) and isobutanol (3 ml) was heated to 125° C. and maintained at this temperature for 16 hours. The mixture was then cooled to room temperature and concentrated in vacuo to give a brown residue which was chromatographed (silica gel, 9:1 CHCl3 /CH3OH saturated with NH3 (g)) to yield 0.177 g (a yield of 61%) of the title compound as a yellow solid, which was characterized spectroscopically.

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