反应详情

Prepared analogously to Compound 1B using ethyl (4-{[4-chloro-5-(trifluoromethyl)pyrimidin-2-yl]amino}-3-methoxybenzyl)methylphosphinate (Compound 61 D, 270 mg, 0.64 mmol) and 3-amino-6-bromo-N-methylpyridine-2-carboxamide (Compound 6D, 154 mg, 0.669 mmol) to afford 298 mg of the title compound (76%). 1H NMR (400 MHz, CD-3OD) δ 9.00 (br. s., 1H), 8.36 (s, 1H), 7.63-7.73 (m, 1H), 7.51-7.61 (m, 1H), 7.07 (t, J=1.9 Hz, 1H), 6.93 (td, J=2.2, 8.1 Hz, 1H), 4.04-4.16 (m, 2H), 3.89 (s, 3H), 3.33 (s, 1H), 3.29 (s, 1H), 2.93 (s, 3H), 1.51 (s, 3H), 1.33 (t, J=7.1 Hz, 3H). MS (ESI): m/z=617.06/619.06 [M+H]+. HPLC: tR=1.01 min (UPLC-TOF: polar—3 min).