反应详情

To a stirred solution of {trans-4-[4-(4-amino-5-oxo-7,8-dihydropyrimido[5,4-f][1,4]oxazepin-6(5H)-yl)phenyl]cyclohexyl}acetic acid (50 mg, 0.13 mmol), from Example 2, N-methylsulfonamide (30 mg, 0.32 mmol) were added HOBT (29 mg, 0.19 mmol), EDCl (30 mg, 0.32 mmol) and TEA (19.1 mg, 0.19 mmol). After 18 hours, the reaction mixture was diluted into EtOAc, washed with water, dried over sodium sulfate and concentrated in vacuo. Reverse-phase chromatography afforded the desired product as a white solid, 5.3 mg. 1H NMR (400 MHz, DMSO-d6): δ 8.17 (s, 1H), 7.64 (br s, 2H) 7.20 (s, 4H), 4.58 (m, 2H), 3.92 (m, 2H), 3.20 (s, 3H), 2.42 (m, 1H), 2.17 (m, 2H), 1.73 (m, 5H), 1.40 (m, 2H), 1.05 m, 2H). m/z=474.4 (M+1). IC50 44.5 nM (range 34.2-75.0 nM).

1. washwashed with water
2. dry with materialdried over sodium sulfate
3. concentrationconcentrated in vacuo