反应详情

Intermediate 42 (152 mg, 0.5 mmol) was reacted with isonicotinic acid by Method E. Flash chromatography eluted with 9:1 DCM:MeOH afforded compound 47 (204 mg, 100%) as a white solid: Mp 210-212° C. 1H NMR (500 MHz, DMSO-d6) δ 8.67 (d, J=6 Hz, 2H), 8.59 (s, 1H), 7.47 (d, J=9 Hz, 2H), 7.38 (d, J=6 Hz, 2H), 7.22 (d, J=9 Hz, 2H), 6.25 (d, J=8 Hz, 1H), 4.30 (d, J=12 Hz, 1H), 3.76 (s, 1H), 3.41 (d, J=12 Hz, 1H), 3.16 (t, J=12 Hz, 1H), 3.05 (t, J=12 Hz, 1H), 1.97-1.88 (m, 1H), 1.84-1.75 (m, 1H), 1.47-1.29 (m, 2H). Purity 92%. HRMS calculated for C19H19F3N4O3−H+ 407.1331. found (ESI(−), [M−H]) 407.1316.

1. washFlash chromatography eluted with 9:1 DCM