1,2-Difluoro-4-(methylsulfonyl)benzene → 3,4-difluoro-2-(2-oxo-4-(1-(5-propylpyrimidin-2-yl)piperidin-4-yloxy)pyridin-1(2H)-yl)benzonitrile

Participants

Reaction Steps

Example 252 was prepared according to procedures described in Example 248 substituting 4-(1-(5-propylpyrimidin-2-yl)piperidin-4-yloxy)pyridin-2(1H)-one (prepared according to procedures described in Example 173 Step C) for 4-(1-(5-ethylpyrimidin-2-yl)piperidin-4-yloxy)pyridin-2(1H)-one and substituting 2,3,4-trifluorobenzonitrile (Oakwood) for 1,2-difluoro-4-(methylsulfonyl)benzene. 1H NMR (400 MHz, CDCl3) δ ppm 8.10 (s, 2 H), 7.43-7.60 (m, 1 H), 7.27-7.43 (m, 1 H), 7.02 (d, J=7.78 Hz, 1 H), 6.05 (dd, J=7.65, 2.64 Hz, 1 H), 5.96 (d, J=2.51 Hz, 1 H), 4.43-4.60 (m, 1 H), 4.08-4.24 (m, 2 H), 3.49-3.66 (m, 2 H), 2.34 (t, J=7.53 Hz, 2 H), 1.99-2.08 (m, 2 H), 1.71-1.88 (m, 2 H), 1.43-1.59 (m, 2 H), 0.87 (t, J=7.28 Hz, 3 H). MS (ESI) 452 (M+H).

Provenance & Evidence