反应详情

The titled compound was prepared using a procedure similar to the one described for the synthesis of Example 6 using N6-[(1S)-1-(5-fluoropyrimidin-2-yl)ethyl]-N2-(5-isopropoxy-1H-pyrazol-3-yl)-3-nitropyridine-2,6-diamine (Intermediate 20) as the starting material. The starting material (1.7 g) was dissolved into ethanol (10 mL). To the solution was added Pd—C (0.3 g, 10%). A hydrogen inlet was introduced into the reaction flask. The resulting mixture was stirred for 5 hours. Formamidine acetate (2 g) was added to the resulting mixture. The mixture was stirred at 85° C. for 4 hours. The resulting mixture was filtered, and the filtrate was concentrated. The resulting residue was separated by Silica gel column. The title compound was obtained (0.14 g) as a by-product. LCMS: 365 [M+1]. 1H NMR (400 MHz, CD3OD) δ 8.60 (s, 2H), 8.20 (s, 1H), 7.60 (d, 1H), 7.20 (s, 2H), 6.50 (d, 1H), 6.10 (br, 1H), 5.10 (s, 1H), 4.70 (m, 1H), 1.40 (d, 3H), 1.30 (d, 6H).

1. customThe titled compound was prepared
2. additionA hydrogen inlet was introduced into the reaction flask
3. stirringThe mixture was stirred at 85° C. for 4 hours
4. filtrationThe resulting mixture was filtered
5. concentrationthe filtrate was concentrated
6. customThe resulting residue was separated by Silica gel column