反应详情

Aqueous lithium hydroxide (1M, 130 mL, 0.13 mmol) was added dropwise to a stirred solution of (R)-1-methoxy-3-(7-methyl-2-((2-(trimethylsilyl)ethoxy)methyl)-2H-indazol-5-yl)-1-oxopropan-2-yl 4-(2-oxo-1,2-dihydroquinolin-3-yl)piperidine-1-carboxylate (40 mg, 0.0646 mmol) in dioxane (2 mL) at 0° C., and the mixture was stirred for 2 h. The reaction was quenched with 1N hydrochloric acid, poured into ethyl acetate (30 mL), washed with brine (10 mL), dried over magnesium sulfate and concentrated in vacuo to afford a tan foamy solid (32 mg, 82%), which was used without further purification. 1H-NMR (CDCl3, 400 MHz) δ 8.02 (s,1H), 7.60 (s,1H), 7.52-7.32 (m, 3H), 7.29-7.13 (m, 2H), 7.05 (s,1H), 5.71 (s,2H), 5.29 (dd, J=9.0, 3.8 Hz, 1H), 4.28 (br, 2H), 3.34 (br, 2H), 3.34 (dd, J=14.1, 3.9 Hz, 2H), 3.21 (dd, J=14.4, 9.2 Hz, 2H) 3.13-2.75 (m, 4H), 2.60 (s, 3H), 1.95-1.72 (m, 4H), 0.95-1.85 (m, 2H), 0.051 (s, 9H).

1. customThe reaction was quenched with 1N hydrochloric acid
2. additionpoured into ethyl acetate (30 mL)
3. washwashed with brine (10 mL)
4. dry with materialdried over magnesium sulfate
5. concentrationconcentrated in vacuo