Trifluoroacetic acid → HCID 52914055, compound

Participants

Reaction Steps

814 mg of tert-butyl [(3-{2-[(cyclopropylsulfonyl)amino]-5-fluoro-3-[(2-fluoro-4-iodophenyl)amino]phenoxy}benzyl)sulfamoyl]carbamate (Intermediate 18A; 1.08 mmol, 1 eq.) were dissolved in 30 mL DCM and 1.67 mL TFA were added. The reaction mixture was stirred at rt overnight. The reaction mixture was partitioned between saturated aq. sodium bicarbonate solution and dichloromethane. The pH was adjusted to pH=8 with aq. 2N sodium hydroxide solution. The layers were separated and the aqueouse layer reextracted twice with dichloromethane. The combined organic layers were washed once with brine, filtered and concentrated in vacuo. The crude product was purified by preparative HPLC providing 322 mg of the desired product (46% yield).

Provenance & Evidence