反应详情

The title compound was prepared in a manner similar to EXAMPLE 2 using 2-chloro-5-(4-(methylsulfonyl)benzyl)-5,6,6a,7,9,10-hexahydro-[1,4]oxazino[3,4-h]pteridine (PREPARATION x9, 90 mg, 0.228 mmol), 7-fluoro-4-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)-1H-indole (119 mg, 0.456 mmol) and PdCl2(dppf) (8.34 mg, 0.011 mmol) in dioxane (2.5 mL) and aqueous saturated NaHCO3 (0.5 mL). 1H NMR (400 MHz, DMSO-d6) δ 3.22 (m, 3H), 3.24-3.36 (m, 2H), 3.39-3.75 (m, 3H), 3.88-4.06 (m, 2H), 4.06-4.16 (m, 1H), 4.62-4.77 (m, 2H), 7.05-7.21 (m, 2H), 7.45-7.53 (m, 1H), 7.55-7.62 (m, 1H), 7.62-7.72 (m, 3H), 7.90-7.97 (m, 2H), 11.85-12.09 (m, 1H). ESI-MS m/z [M+H]+ calc'd for C25H24FN5O3S, 494.16. found 494.5.