反应详情

The title compound was prepared in the same manner as described for intermediate 61 using ethyl 4-[4-(methylthio)phenyl]-2,4-dioxobutanoate (851 mg, 3.20 mmol), benzene (6 mL), 1-(1-methylethyl)-1H-pyrazol-5-amine (400 mg, 3.20 mmol), and acetic acid (3 mL). The crude product was purified by column chromatography (Silica gel, eluent; 0 to 100% EtOAc/hexanes) to give 870 mg (63%) of product. LCMS E-S (M+H)=433.2. 1H NMR (400 MHz, CHLOROFORM-d) δ ppm 1.47-1.57 (m, 3 H), 1.66 (d, J=6.8 Hz, 6 H), 2.58 (s, 3 H), 4.56 (q, J=7.2 Hz, 2 H), 5.38-5.55 (m, 1 H), 7.36-7.46 (m, 2 H), 8.12-8.19 (m, 2 H), 8.22 (s, 1 H), 8.40 (s, 1 H).

1. customThe crude product was purified by column chromatography (Silica gel, eluent; 0 to 100% EtOAc/hexanes)