反应详情

2-chloro-5-(4-(3-cyclopropyl-1H-pyrazol-5-ylamino)-5-ethynylpyrimidin-2-yl) benzamide (Compound 128) (40 mg, 13%) was prepared from 2-chloro-5-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)benzamide 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)=378.9 [M+H1H NMR (400 MHz, DMSO-d6): δ 0.75-0.76 (m, 2H), 0.98-0.99 (m, 2H), 1.89-1.97 (m, 1H), 4.87 (s, 1H), 6.41 (s, 1H), 7.65 (d, J=8.4 Hz, 1H), 7.72 (s, 1H), 8.05 (s, 1H), 8.31 (d, J=8.4 Hz, 1H), 8.33 (d, J=1.6 Hz, 1H), 8.58 (s, 1H), 8.75 (s, 1H), 12.33 (s, 1H).