反应详情

To a solution of 3-(5-isopentyl-6-(2-isopropylphenyl)-1-methyl-2,4-dioxo-1,2-dihydropyrido[2,3-d]pyrimidin-3(4H)-yl)propyl formate (15 mg, 0.033 mmol) in THF (4 mL) and water (4 mL) was added LiOH.H2O (2.79 mg, 0.066 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 chromatography eluted with PE/EA (10:1) to give 3-(3-hydroxypropyl)-5-isopentyl-6-(2-isopropylphenyl)-1-methylpyrido[2,3-d]pyrimidine-2,4(1H,3H)-dione (8 mg, 56.8% yield) as a white solid. 1H NMR (CDCl3) δ: 8.35 (s, 1H), 7.43-7.42 (d, J=4.0 Hz, 2H), 7.28-7.24 (m, 1H), 7.07-7.05 (m, 1H), 4.27 (m, 3H), 3.76 (s, 3H), 3.58 (s, 2H), 3.40-3.31 (m, 2H), 2.68-2.54 (m, 2H), 1.97-1.94 (m, 2H), 1.57 (m, 1H), 1.22-1.19 (m, 3H), 1.08-1.06 (m, 3H), 0.71-0.69 (m, 3H), 0.64-0.62 (d, J=8 Hz, 3H). LCMS: MH+ 424 and TR=3.546 min.

1. dry with materialThe organic layer was dried over Na2SO4
2. concentrationconcentrated to a residue which
3. customwas purified by chromatography
4. washeluted with PE/EA (10:1)