HCID 71466164, compound → HCID 71466234, compound

Participants

Reaction Steps

To a stirred solution of N-(4-fluoro-3-methoxybenzyl)-2-methyl-6-(5-(piperidin-4-yl)-4,5-dihydroisoxazol-3-yl)pyrimidine-4-carboxamide hydrochloride (0.20 g, 0.43 mmol Preparation #K. 1) in DCM (10 mL) was added TEA (0.13 g, 1.29 mmol, Spectrochem) and perfluorophenyl-2-(methylsulfonyl)acetate (0.196 g, 0.645 mmol, See Ref: US 20090312338). The resulting solution was stirred at RT for about 16 h. The crude reaction mixture was purified by preparative HPLC (Table 2, Method f) to afford N-(4-fluoro-3-methoxybenzyl)-2-methyl-6-(5-(1-(2-(methylsulfonyl)acetyl)piperidin-4-yl)-4,5-dihydroisoxazol-3-yl)pyrimidine-4-carboxamide 0.072 g (31.3%); LC/MS (Table 1, Method d) Rt=0.55 min; MS m/z: 548.3 (M+H)+.

Provenance & Evidence