Hydrochloric Acid → HCID 86596440, compound

Participants

Reaction Steps

A solution of (2R)-1-[3,5-bis(trifluoromethyl)benzoyl]-2-[(1H-indol-3-yl)methyl]-4-[3-[6-(tert-butoxycarbonylamino)pyridin-3-yl]-2-propynyl]piperazine (127 mg) prepared by a similar manner to that of Example 5-(1) and trifluoroacetic acid (5 ml) in dichloromethane (5 ml) was stirred at room temperature for 2 hours. The reaction mixture was concentrated under reduced pressure and the residue was partitioned between saturated aqueous sodium bicarbonate solution. The organic layer was separated, dried over magnesium sulfate and concentrated under reduced pressure. The syrup obtained was dissolved into ethyl acetate and treated with 4N hydrogen chloride in ethyl acetate to give (2R)-1-[3,5-bis(trifluoromethyl)benzoyl]-2-[(1H-indol-3-yl) methyl]-4-[3-(6-aminopyridin-3-yl)-2-propynyl]piperazine dihydrochloride (80 mg).

Provenance & Evidence