反应详情

2-Bromo-N-(2,4-dihydroxy-butoxy)-5-(2-fluoro-4-iodo -phenylamino)-isonicotinamide was synthesized as described in General method 3: To a solution of 2-bromo-N-{[(4R)-2,2-dimethyl-1,3-dioxolan-4-yl]methoxy}-5-[(2-fluoro-4-iodophenyl)amino]-isonicotinamide (100.0 mg, 0.18 mmol) in dichloromethane (1 ml) was added trifluoroacetic acid (1 ml) at RT. The reaction mixture was stirred at RT for 30 min, and monitored by TLC (Hex:EtOAc=1:1 and contain TEA). Upon completion, the volatiles were evaporated, and the residue was dissolved in dichloromethane, washed with 5% aq. NaHCO3 to get a precipitate. The residue was filtered, washed with water, and dried to get 53 mg (56%) of 2-Bromo-N-(2,4-dihydroxy-butoxy)-5-(2-fluoro-4-iodo-phenylamino)-isonicotinamide. LC/MS: [8.76 min, 541 (M+1)]

1. custom2-Bromo-N-(2,4-dihydroxy-butoxy)-5-(2-fluoro-4-iodo -phenylamino)-isonicotinamide was synthesized
2. customUpon completion, the volatiles were evaporated
3. dissolutionthe residue was dissolved in dichloromethane
4. washwashed with 5% aq. NaHCO3
5. customto get a precipitate
6. filtrationThe residue was filtered
7. washwashed with water
8. customdried