反应详情

A mixture of Pd(dppf)Cl2.CH2Cl2 (182 mg, 0.22 mmol, 0.1 equiv.), the crude N-(2-(dimethyl amino)ethyl)-5-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)thiophene-2-sulfonamide and 2,5-dibromo-N-(5-cyclopropyl-1H-pyrazol-3-yl)pyrimidin-4-amine (700 mg, 1.95 mmol, 1.0 eq) in dioxane (20 mL) and saturated Na2CO3 aqueous (2 mL) was heated at 100° C. for 2 h under nitrogen atmosphere. The reaction mixture was cooled to room temperature, and extracted with THF. The combined organic layers were purified by silica gel chromatography to afford compound 5-(5-bromo-4-(5-cyclopropyl-1H-pyrazol-3-ylamino)pyrimidin-2-yl)-N-(2-(dimethylamino)ethyl)thiophene-2-sulfonamide (200 mg, 20% over 2 steps). LC-MS (m/z)=512.0, 514.0 [M+H]+.

1. extractionextracted with THF
2. customThe combined organic layers were purified by silica gel chromatography