877399-74-1

Method 1:     To a solution of tert-butyl 4-(4-iodo-lH-pyrazol-l-yl)piperidine-l -carboxylate (1.00 g, 2.650 mmol) in DMSO (11 mL) were added 4,4,4,,4,,5,5,5,5-octamethyl-2,2**,-bi(l,3,2- dioxaborolane) (942.5 mg, 3.710 mmol) and CH3COOK (1.04 g, 10.60 mmol) sequentially. The mixture was degassed and charged with N2 several times, then Pd(PPh3)2Cl2 (93.0 mg, 0.130 mmol) was added. The resulted mixture was stirred at 80 °C for 2 hours, then cooled to rt, and filtered through a pad of celite. The filtrate was washed with brine (100 mL x 3), dried over anhydrous Na2S04, and concentrated in vacuo. The residue was purified by a silica gel column chromatography (PE/EtOAc (v/v) = 5/1) to give the title compound as a white solid (878.6 mg, 87.9percent). MS (ESI, pos. ion) m/z: 378.0 (M+l).