反应详情

A mixture of 2-(5-bromo-4-cyano-2-fluorophenylamino)-4,4,4-trifluorobutanamide (90 mg, 0.254 mmol), 5-amino-3-methylisothiazole hydrochloride (58 mg, 0.385 mmol), K2CO3 (200 mg, 1.45 mmol), BINAP (35 mg, 0.056 mmol) and Pd(OAc)2 (23 mg, 0.100 mmol) in dioxane (3 mL) was degassed with argon, then was stirred at 120 C for 18 h. Water and EtOAc were added. The organic phase was separated, dried over Na2SO4, concentrated in vacuo to give 2-(4-cyano-2-fluoro-5-(3-methylisothiazol-5-ylamino)phenylamino)-4,4,4-trifluorobutanamide (98 mg).

1. customwas degassed with argon
2. additionWater and EtOAc were added
3. customThe organic phase was separated
4. dry with materialdried over Na2SO4
5. concentrationconcentrated in vacuo