反应详情

3-Chloromethyl-5-methyl-isoxazole (1.5 eq.) was directly added to a solution of 2-[1,4]diazepan-1-yl-7-furan-2-yl-pyrazolo[1,5-a][1,3,5]triazin-4-ylamine (0.14 mmol) and Et3N (0.3 mmol) in 3 mL of CH3CN. The resulting reaction mixture was stirred at room temp for 18 hours. It was then concentrated and purified by preparative HPLC using a mixture of aqueous CH3CN that has been buffered with 0.1% TFA. 1H NMR (DMSO-d6) δ 7.90 (br s, 2 H), 7.80 (d, J=1.0 Hz, 1H), 7.05 (d, J=3.6 Hz, 1H), 6.68 (dd, J=3.6 Hz, 1.0 Hz, 1H), 6.30 (s, 1H), 3.65 (m, 2H), 3.20-2.75 (m, 10 H), 2.35 (s, 3H) ppm. MS: m/z: 395 [M+H]+.

1. customThe resulting reaction mixture
2. concentrationIt was then concentrated
3. custompurified by preparative HPLC
4. additiona mixture of aqueous CH3CN that