1-Chloro-4-isocyanato-2-(trifluoromethyl) benzene → 1-(4-chloro-3-trifluoromethyl-phenyl)-3-[3-(3-pyridin-4-yl-6,7-dihydro-5H-pyrazolo[5,1-b][1,3]thiazin-2-yl)-phenyl]-urea

関与物質

反応手順

3-(3-Pyridin-4-yl-6,7-dihydro-5H-pyrazolo[5,1-b][1,3]thiazin-2-yl)-phenylamine (50 mg, 0.162 mmol) was dissolved in dry DCM under nitrogen atmosphere. 4-chloro-3-trifluoromethylphenylisocyanate (43 mg, 0.195 mmol, 1.2 eq) was added, the mixture was stirred at room temperature for 2 hours and then concentrated under reduced pressure. The crude product was purified by silica gel chromatography (eluant: 100% ethyl acetate) to give 64 mg (75%) of 1-(4-chloro-3-trifluoromethyl-phenyl)-3-[3-(3-pyridin-4-yl-6,7-dihydro-5H-pyrazolo[5,1-b][1,3]thiazin-2-yl)-phenyl]-urea as white powder.

情報源と証拠