4-(Trifluoromethyl)phenyl isocyanate → 1-[3-(7-Pyridin-4-yl-pyrazolo[5,1-b]thiazol-6-yl)-phenyl]-3-(4-trifluoromethyl-phenyl)-urea

関与物質

反応手順

3-(7-Pyridin-4-yl-pyrazolo[5,1-b]thiazol-6-yl)-phenylamine (50 mg, 0.171 mmol) was dissolved in dry DCM (1 mL) under nitrogen atmosphere. p-trifluoromethylphenylisocyanate (0.025 mL, 0.179 mmol, 1.05 eq) was added and the mixture was stirred at room temperature for 1 hour. The solution was evaporated to dryness and the crude product was purified by chromatography on silica gel (DCM/MeOH 96:4) to give 80 mg of an oil, which after trituration with ethylether gave 63 mg of 1-[3-(7-pyridin-4-yl-pyrazolo[5,1-b]thiazol-6-yl)-phenyl]-3-(4-trifluoro-methyl-phenyl)-urea white solid (77%).

情報源と証拠