反应详情

A stirred solution of (R)-1-(3-(4-fluorophenyl)-1,2,4-oxadiazol-5-yl)-2-(7-methyl-2-((2-(trimethylsilyl)ethoxy)methyl)-2H-indazol-5-yl)ethyl 4-(2-oxo-1,2-dihydroquinolin-3-yl)piperidine-1-carboxylate (16.2 mg, 0.0224 mmol) in 1:1 trifluoroacetic acid/methylene chloride 91 mL) was stirred at room temperature for 2 h. Removal of the solvents in vacuo followed by purification using preparative HPLC afforded a tan gum (8.6 mg, 65%). 1H-NMR (CDCl3, 400 MHz) δ 8.22 (s, 1H), 8.12-8.01 (m,2H), 7.80 (s, 1H), 7.76-7.45 (m, 5H), 7.35-7.45 (m, 2H), 7.30 (s,1H), 7.20-7.07 (m,2H), 6.28-6.15 (m,1H), 4.42-4.25 (m,2H), 3.57-3.45 (m,2H) 3.31-2.85 (m, 4H), 2.60 (s,3H), 2.09-1.88 (m,2H), 1.70-1.53 (m,2H). Mass spec. 593.28 (MH+).

1. customRemoval of the solvents in vacuo
2. customfollowed by purification