Triethylamine → (1R*,2R*,5S*,6R*)-8-Benzyl-2-{[3,5-bis(trifluoromethyl)phenyl]methoxy}-6-{2-[2-(methylsulphonylamino)ethyl]-2H-tetrazol-5-yl}-1-phenyl-8-azabicyclo[3.2.1]octane

Participants

Reaction Steps

Methanesulphonyl chloride (90 mg, 0.78 mmol) was added to a solution of (1R*,2R*,5S*6R*)-6-[2-(2-aminoethyl)-2H-tetrazol-5-yl]-8-benzyl-2-{[3,5-bis(trifluoromethyl)phenyl]methoxy}-1-phenyl-8-azabicyclo[3.2.1]octane (Example 141; 0.45 g, 0.71 mmol) and triethylamine (101 mg, 1 mmol) in dichloromethane (10 ml). The reaction mixture was stirred at room temperature for 3 hours then washed with water (×2). The organic layer was separated, dried (MgSO4), filtered and concentrated to yield the title compound (0.47 g, 94%).

Provenance & Evidence