3,5-Dibromo-1-methylpyridin-2(1H)-one → 5-Bromo-3-(1-(2-(tert-butyldimethylsilyloxy)ethyl)-1H-pyrazol-3-ylamino)-1-methylpyridin-2(1H)-one

Participants

Reaction Steps

Using the same general procedure as described for the preparation of 103l, reaction of 119b (400 mg, 1.66 mmol) with 3,5-dibromo-1-methylpyridin-2(1H)-one (441 mg, 1.66 mmol) gave a 76% yield (521 mg) of 119c as a yellow solid: mp 96-97° C.; 1H NMR (500 MHz, CDCl3) δ 7.85 (d, 1H, J=2.5 Hz), 7.42 (s, 1H), 5.31 (d, 1H, J=2.5 Hz), 6.87 (d, 1H, J=2.5 Hz), 5.84 (d, 1H, J=2.5 Hz), 4.16 (t, 2H, J=5.0 Hz), 3.96 (t, 2H, J=5.5 Hz), 3.58 (s, 3H), 0.85 (s, 9H), −0.04 (s, 6H). MS (APCI+) m/z 427.4 (M+H).

Provenance & Evidence