反应详情

3-Methyl-1H-pyrazolo[3,4-b]pyridin-5-amine (0.100 g, 0.675 mmol, Example 4, Step B), 2,6-difluoro-3-(3-fluoropropylsulfonamido)benzoic acid (0.211 g, 0.709 mmol), EDCI (0.136 g, 0.709 mmol) and HOBt (0.091 g, 0.675 mmol) were dissolved in DMF (1.9 mL) and stirred at room temperature for 16 hours. The reaction mixture was purified by reverse phase HPLC to give 2,6-difluoro-3-(3-fluoropropylsulfonamido)-N-(3-methyl-1H-pyrazolo[3,4-b]pyridin-5-yl)benzamide (0.085 g, 29%) as a solid. 1H NMR (400 MHz, d6-DMSO) δ 13.22 (s, 1H), 11.05 (s, 1H), 9.93 (br s, 1H), 8.60-8.59 (m, 1H), 8.55-8.54 (m, 1H), 7.59-7.53 (m, 1H), 7.30-7.25 (m, 1H), 4.62 (t, 1H), 4.50 (t, 1H), 3.26-3.23 (m, 2H), 2.20-2.07 (m, 2H); m/z (ES-MS) 428.1 (100.0%) [M+1].

1. customThe reaction mixture was purified by reverse phase HPLC