Trifluoroacetic acid → (4,4-Difluoro-piperidin-1-yl)-[5-(piperidin-4-yloxy)-1H-indol-2-yl]-methanone

Participants

Reaction Steps

Trifluoroacetic acid (4.13 mL, 10.0 eq.) was added to a cold (0° C.) solution of 4-[2-(4,4-difluoro-piperidine-1-carbonyl)-1H-indol-5-yloxy]-piperidine-1-carboxylic acid tert-butyl ester (example 43, step 5, 2.5 g, 1.0 eq.) in dichloromethane (20 mL). The mixture was stirred for 1 h at room temperature, evaporated to dryness and purified on silica gel, eluting with dichloromethane/methanol/ammonium hydroxide 95:5:0.25, to yield 1.7 g (86%) from the desired product as white solid. MS (m/e): 364.4 (MH+, 100%).

Provenance & Evidence