Trifluoroacetic acid → HCID 67047497, compound

Participants

Reaction Steps

Dissolve [5-(5-cyanopyridin-3-ylethynyl)-2-fluorobenzyl]carbamic acid tert-butyl ester, (prepared as described in EXAMPLE 144), (390 mg, 1.11 mmol) in dichloromethane (7.5 mL) and treat with trifluoroacetic acid (2.57 mL, 33.3 mmol). After stirring for 1.5 h, dilute with dichloromethane and wash with an aqueous saturated solution of sodium bicarbonate and an aqueous saturated solution of sodium chloride. Dry (sodium sulfate), filter, and concentrate. Purify the residue by silica gel chromatography, eluting with a gradient from 90:10 to 75:25 (98:2 dichloromethane:7 N ammonia in methanol):(9:2 acetonitrile:7 N ammonia in methanol), to give the title compound as a white crystalline solid (270 mg, 97%).

Provenance & Evidence