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457949-09-6

Imidazo[1,2-a]pyridin-8(5H)-one, 6,7-dihydro- (9CI) synthesis

4synthesis methods
-

Yield:457949-09-6 82%

Reaction Conditions:

with potassium carbonate;sodium iodide in acetonitrile at 20 - 70; for 23 h;

Steps:

61.4 Process 4

To a solution of compound 193 (556 mg, 3.22 mmol) in acetonitrile (16 ml) were added potassium carbonate (890 mg, 6.44 mmol) and sodium iodide (480 mg, 3.20 mmol) under ice-cooling, and the mixture was stirred at room temperature for 3 hours and then it was stirred at 70 C for 20 hours. The residue obtained by evaporation was subjected to silica gel column chromatography and eluted with chloroform - methanol (9:1 v/v). The fractions containing desired compound were concentrated under reduced pressure to give compound 194 (358 mg, 82.0%) as colorless crystals. NMR (CDCl3) ?: 2.39 (2H, m), 2.77 (2H, m), 4.26 (2H, m), 7.08 (1H, s), 7.34 (1H, d, J=0.9 Hz).

References:

EP1375486,2004,A1 Location in patent:Page 142