反应详情

Prepared analogously to Compound 1B using diethyl (4-{[4-chloro-5-(trifluoromethyl)pyrimidin-2-yl]amino}-3-methoxybenzyl)phosphonate (Compound 1 E, 282.1 mg, 0.62 mmol) and 2-amino-N,N-diethyl-5-[1-(3-hydroxypropyl)-1H-pyrazol-4-yl]benzamide (Compound 3C, 196.7 mg, 0.62 mmol) to afford 228 mg of the title compound (50%). 1H NMR (400 MHz, CD3OD) δ 8.33 (br. s., 1H), 8.18 (s, 1H), 7.97 (s, 1H), 7.77 (dd, J=2.02, 8.34 Hz, 1H), 7.59-7.67 (m, 2H), 7.57 (d, J=8.08 Hz, 1H), 6.97 (br. s., 1H), 6.57 (br. s., 1H), 4.32 (t, J=6.95 Hz, 2H), 3.99 (quin, J=7.14 Hz, 4H), 3.89 (s, 3H), 3.59 (t, J=6.06 Hz, 2H), 3.43-3.52 (m, 2H), 3.08-3.22 (m, 4H), 2.11 (quin, J=6.57 Hz, 2H), 1.22 (t, J=7.07 Hz, 6H), 1.11 (t, J=6.95 Hz, 3H), 0.97 (br. s., 3H). MS (ESI): m/z 734.85 [M+H]+. UPLC: tR=1.22 min (UPLC-SQD: analytical—2 min).