Hydrochloric Acid → Bavisant dihydrochloride anhydrous

Participants

Reaction Conditions

Reaction Steps

A 250 mL, three-neck flask fitted with a mechanical stirrer, addition funnel, thermocouple probe, and heating mantle was charged with (4-cyclopropyl-piperazin-1-yl)-(4-morpholin-4-ylmethyl-phenyl)-methanone (11.0 g, 0.034 mol, 1.0 eq) and ethanol (75 mL). The resulting solution was heated to 60° C. Concentrated hydrochloric acid (6.1 mL, 0.074 mol, 2.2 eq) was then added dropwise over 8 min. The reaction mixture was then heated at 60° C. for a further 10 min and then slowly cooled to 20° C. over 3 hrs. The resulting solid was collected by filtration, rinsed with pentane, and dried at 50° C. for 3 hrs in a vacuum oven to yield the title compound as a white solid.

Provenance & Evidence