Cesium carbonate → 2,6-difluoro-N-[3-(3-{5-fluoro-2-[(3-fluorophenyl)amino]-4-pyrimidinyl}pyrazolo[1,5-a]pyridin-2-yl)phenyl]benzamide

Beteiligte Stoffe

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Reaktionsschritte

A solution 4-[2-(3-bromophenyl)pyrazolo[1,5-a]pyridin-3-yl]-5-fluoro-N-(3-fluorophenyl)-2-pyrimidinamine (40 mg, 84 mmol), Pd2(dba)3 (15.3 mg, 0.016 mmol), xantphos (14.5 mg, 0.025 mmol), Cs2CO3 (95 mg, 0.29 mmol), and 2,6-difluorobenzamide (39 mg, 0.25 mmol) in anhydrous 1,4-dioxane, that had been previously degassed with nitrogen, was heated at 160° C. in the microwave for 15 min. At this time, the crude reaction was adsorbed to silica gel and purified by LC (DCM to 5% MeOH/DCM) to afford the product (28.3 mg, 61%) as a white solid. ESIMS (M+H)+=555. 1H NMR (400 MHz, DMSO-d6) δ 6.63-6.67 (m, 1H), 7.09-7.24 (m, 4H), 7.29-7.49 (m, 3H), 7.54-7.61 (m, 1H), 7.68-7.72 (m, 1H), 7.81 (s, 1H), 7.90-7.94 (m, 1H), 8.04 (m, 1H), 8.09 (m, 1H), 8.53-8.54 (m, 1H), 8.87-8.89 (m, 1H), 9.91 (s, 1H), 10.84 (s, 1H); ESIMS (M+H)+=555.

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