反应详情

Using procedures analogous to Example C2 and Example A2, ethyl 4-chloro-2-(methylthio)pyrimidine-5-carboxylate, cyclopropyl amine, ethyl 2-(3-amino-4-fluorophenyl)acetate (prepared by the method of Kuse et al. Tetrahedron (2005), 67, 5754-5762) and 0.5 M ammonia in dioxane (2 ml) were combined to afford 2-amino-6-(3-amino-4-fluorophenyl)-8-cyclopropylpyrido[2,3-d]pyrimidin-7(8H)-one as an off-white solid (67 mg). 1H NMR (400 MHz, DMSO-d6): δ 8.57 (s, 1H), 7.73 (s, 1H), 7.15 (brs, 1H), 7.06 (dd, J=9.2 Hz, 2.4 Hz, 1H), 6.99 (dd, J=11.2 Hz, 11.6 Hz, 1H), 6.75-6.71 (m, 1H), 2.88-2.82 (m, 1H), 1.18-1.13 (m, 2H), 0.83-0.78 (m, 2H); MS (ESI) m/z: 312.0 (M+H+).