Hydrochloric Acid → 1-((3R,4R)-4-methylpiperidin-3-yl)-6H-imidazo[1,5-a]pyrrolo[2,3-e]pyrazine hydrochloride

Participants

Reaction Conditions

Reaction Steps

To a solution of (3R,4R)-tert-butyl 3-(6H-imidazo[1,5-a]pyrrolo[2,3-e]pyrazin-1-yl)-4-methyl-piperidine-1-carboxylate (27.9 g, 78 mmol) in 1,4-dioxane (400 mL) was added HCl (4 N in 1,4-dioxane, 58.9 mL, 235 mmol). The resulting suspension was heated at about 60° C. for about 1 h. The reaction was allowed to cool to ambient temperature and then was filtered, washed with 1,4-dioxane (100 mL) followed by Et2O (100 mL), to give 1-((3R,4R)-4-methylpiperidin-3-yl)-6H-imidazo[1,5-a]pyrrolo[2,3-e]pyrazine hydrochloride (20.6 g, 89%) as a tan solid: LC/MS (Table 1, Method b) Rt=1.27 min; MS m/z: 256 (M+H)+.

Provenance & Evidence