反应详情

N-[5-[(2-Chloro-4-pyrimidinyl)ethynyl]-2-(methyloxy)phenyl]-2,2,2-trifluoroacetamide (1.7 g, 4.8 mmol) was subjected to cyclization with N-aminopyridinium iodide (2.1 g, 9.6 mmol) according to the procedure of Example 56, Step E to give the desired product (1.15 g, 53%). 1H NMR (400 MHz, d6-DMSO) δ 10.82 (s, 1H), 8.88 (d, J=6.8 Hz, 1H), 8.45 (d, J=5.6 Hz, 1H), 8.39 (d, J=8.4 Hz, 1H), 7.70 (d, J=2.0 Hz, 1H), 7.64-7.60 (m, 1H), 7.57 (dd, J=8.6 and 1.8 Hz, 1H), 7.28 (d, J=8.4 Hz, 1H), 7.21-7.18 (m, 1H), 7.11 (d, J=5.6 Hz, 1H), 3.90 (s, 3H) ppm.