Ammonia → Orvepitant maleate

Participants

Reaction Steps

Orvepitant Hydrochloride (1.00 G) Was Suspended In Ethyl Acetate (20 Ml) And Water (10 ml) and 25% w/w ammonia (10 ml) were added. The aqueous layer was separated and the organic layer was washed with 10% w/w sodium chloride solution (2×10 ml). The organic solution was separated, evaporated to dryness and isopropanol (20 ml) was added. The solution was evaporated to dryness. The material was diluted with isopropanol (6 ml) and a solution of maleic acid (0.174 g) in isopropanol (2.0 ml) was added. Iso-octane (a total of 8 ml) was added and the solution was stirred overnight. The solution was evaporated to an oil. Tert-butyl methyl ether (10 ml) was added and the solution was evaporated to dryness. Repeat the addition of tert-butyl methyl ether and evaporation a total of 4 times. On final evaporation, a foam forms that solidifies to give the title compound.

Provenance & Evidence