HCID 57456316, compound → HCID 59852752, compound

Participants

Reaction Conditions

Reaction Steps

1-(3-Benzyloxy-2-fluorophenyl)-8-chloro-3-cyclobutylimidazo[1,5-a]pyrazine: Cyclobutanecarboxylic acid [(3-benzyloxy-2-fluoro-phenyl)-(3-chloro-pyrazin-2-yl)-methyl]-amide (0.850 g, 2 mmole) was dissolved in POCl3 (6 mL) and heated at 55° C. overnight. The excess POCl3 was removed in vacuo. The residue was cooled to 0° C. and charged with a saturated solution of NH3 in 2-propanol (6 mL). The mixture was left overnight at room temperature. The separated solid was then filtered and washed with methylene chloride. The filtrate was evaporated to dryness and purified by silica-gel column chromatography using hexane:ethyl acetate (60:40) as the eluant to afford the title compound (615 mg, 75%). FAB-MS: m/z 408.3 (M+H)+.

Provenance & Evidence