Trifluoroacetic acid → HCID 71273947, compound

Participants

Reaction Steps

A solution of 5-cyano-3-methyl-pyridine-2-carboxylic acid {6-[(R)-2-{[bis-(4-methoxy-phenyl)-phenyl-methyl]amino}-5,5-difluoro-4-(2-methoxy-ethyl)-5,6-dihydro-4H-[1,3]oxazin-4-yl]-5-fluoro-pyridin-2-yl}-amide (146 mg, 0.194 mmol), TFA (0.989 ml, 12.83 mmol) and triethylsilane (0.093 ml, 0.583 mmol) in dichloromethane (1.9 ml) was stirred at it for 18 hours. The reaction mixture was evaporated and the residue diluted with ethyl acetate, washed with sat. aqueous sodium bicarbonate solution, water and brine, dried over sodium sulfate, filtered and evaporated. 142 mg colourless resin. The product was chromatographed over a preparative silica gel plate (2 mm, 20×20 cm, Merck, dichloromethane/methanol 95:5) to give the title compound as a colourless foam. 74 mg (85% yield).

Provenance & Evidence