反应详情

温度

35 °C

A solution of tert-butyl 4-[4-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)-1H-pyrazol-1-yl]piperidine-1-carboxylate (5.02 g, 13.3 mmol) in 1,4-dioxane (40 mL) was treated with HCl (4.0 M in 1,4-dioxane, 50 mL, 200 mmol) and stirred at 35° C. for 3 h. The reaction mixture was concentrated in vacuo to a white solid, affording 5.01 g (100%) of the title compound. The material was used without additional purification. 1H NMR (400 MHz, CDCl3) δ 1.33 (s, 12H), 2.50 (br s, 4H), 3.09-3.41 (m, 2H), 3.57-3.79 (m, 2H), 4.73 (br s, 1H), 7.87 (s, 2H), 9.82 (br s, 2H); MS (ESI): 278.15 [M+H]+; HPLC tR=2.01 min.

1. concentrationThe reaction mixture was concentrated in vacuo to a white solid