4-(Trifluoromethyl)phenyl isocyanate → N-(5-{[4-fluoro-3-({[4-(trifluoromethyl)phenyl]carbamoyl}amino)phenyl]amino}[1,3]thiazolo[5,4-b]pyridin-2-yl)cyclopropanecarboxamide

Participants

Reaction Steps

N-{5-[(3-Amino-4-fluorophenyl)amino][1,3]thiazolo[5,4-b]pyridin-2-yl}cyclopropanecarboxamide (100 mg, 0.30 mmol) produced in Example 12(v) was dissolved in tetrahydrofuran (10 ml), 1-isocyanato-4-(trifluoromethyl)benzene (84 mg, 0.45 mmol) was added, and the mixture was stirred at room temperature for 1 hr. The reaction mixture was concentrated under reduced pressure, and the residue was purified by silica gel column chromatography (petroleum ether/ethyl acetate=10/1) to give the title compound (47 mg, 30%) as a yellow-brown powder.

Provenance & Evidence