反应详情

Deprotection of 6.05 g (18.3 mmol) of 4-(1-ethoxycarbonyl-1-methyl-ethylsulfanyl)-piperidine-1-carboxylic acid tert-butyl ester is achieved by treatment with 4M aqueous HCl solution (9.13 mL) in 1,4-dioxane (40 mL) at room temperature for 18 h. The reaction mixture is concentrated to afford 4.47 g of 2-methyl-2-(piperidin-4-ylsulfanyl)-propionic acid ethyl ester as its hydrochloride salt as a brown oil. Yield: 92%; ES-MS: m/z 232 [M+H]1H NMR (500 MHz, CHLOROFORM-d) δ ppm 1.21 (3 H, t, J=7.13 Hz), 1.45 (6 H, s), 1.80-1.90 (2 H, m), 2.17 (2 H, ddd, J=10.78, 7.31, 3.66 Hz), 2.96-3.05 (2 H, m), 3.07-3.15 (1 H, m), 3.18-3.30 (2 H, m), 4.09 (2 H, q, J=7.12 Hz), 9.44 (1 H, br. s.), 9.54 (1 H, br. s.)

1. concentrationThe reaction mixture is concentrated