反应详情

3-(4-(3-Cyclopropyl-1H-pyrazol-5-ylamino)-5-ethynylpyrimidin-2-yl)-N-(2-hydroxyethyl)benzene sulfonamide (Compound 122) (100 mg, 22%) was prepared from N-(2-hydroxyethyl)-3-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)benzenesulfonamide and 2-Bromo-N-(5-cyclopropyl-1H-pyrazol-3-yl)-5-((trimethylsilyl)ethynyl) pyrimidin-4-amine using the same Pd cataliysed condition as described in Compound 110. LC-MS (m/z)=425.1 [M+H]+. 1H NMR (400 MHz, DMSO-d6): δ 0.81-0.83 (m, 2H), 0.96-0.98 (m, 2H), 1.91-1.98 (m, 1H), 2.83 (q, J=6.0 Hz, 2H), 3.37 (q, J=6.0 Hz, 2H), 4.70 (t, J=5.6 Hz, 1H), 4.91 (s, 1H), 6.46 (s, 1H), 7.71 (t, J=5.6 Hz, 1H), 7.94 (d, J=8.0 Hz, 1H), 8.52 (d, J=7.6 Hz, 1H), 8.62 (s, 1H), 8.73 (s, 1H), 8.76 (s, 1H), 12.32 (s, 1H).