反应详情

To a solution of 3-(5-(4-chlorobenzyl)-1-methyl-6-(5-methylpyridin-3-yloxy)-2,4-dioxo-1,2-dihydropyrido[2,3-d]pyrimidin-3(4H)-yl)propyl formate (56 mg, 0.113 mmol) in THF (3 mL) and water (3 mL) was added LiOH.H2O (9.5 mg, 0.226 mmol). The reaction was stirred at RT for 15 min then diluted with EA (5 mL) and water (5 mL). The organic layer was dried over Na2SO4 and concentrated to a residue which was purified by Prep HPLC to give 5-(4-chlorobenzyl)-3-(3-hydroxypropyl)-1-methyl-6-(5-methylpyridin-3-yloxy)pyrido[2,3-d]pyrimidine-2,4(1H,3H)-dione (11 mg, 21% yield) as a white solid. 1H NMR (CD3OD) δ: 8.43 (s, 1H), 8.13-7.95 (m, 2H), 7.22-7.05 (m, 4H), 6.94 (s, 1H), 4.81 (s, 2H), 4.18 (t, J=7.1 Hz, 2H), 3.72 (s, 3H), 3.65 (t, J=6.3 Hz, 2H), 2.24 (s, 3H), 1.98-1.84 (m, 2H). LCMS: MH+ 467 and TR=2.631 min.

1. dry with materialThe organic layer was dried over Na2SO4
2. concentrationconcentrated to a residue which
3. customwas purified by Prep HPLC