反应详情

温度

100 °C

A microwave vial was charged with (S)-2-amino-4-((1-(6-bromo-1-methyl-1H-pyrrolo[3,2-b]pyridin-5-yl)ethyl)amino)-6-methylpyrimidine-5-carbonitrile (0.07 g, 0.181 mmol), tert-butyl (4-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)cyclohex-3-en-1-yl)carbamate (0.076 g, 0.236 mmol), PdCl2(dppf)-CH2Cl2 adduct (0.015 g, 0.018 mmol) and sodium bicarbonate (0.030 g, 0.362 mmol) in dioxane (2 mL) and water (0.500 mL). The reaction mixture was heated to 100° C. for 40 minutes in a microwave reactor. Following reaction, the solvent was removed under a nitrogen stream and the residue was partitioned between ethyl acetate (20 mL) and water (20 mL). The organic phase was dried over anhydrous sodium sulfate and purified on a silica gel column (20-80% ethyl acetate/heptanes gradient) to give the title compound as a tan solid (79 mg, 87%). ESI-MS m/z [M+H]+ calc'd for C27H34N8O2, 503. found 503.

1. customreaction
2. customthe solvent was removed under a nitrogen stream
3. customthe residue was partitioned between ethyl acetate (20 mL) and water (20 mL)
4. dry with materialThe organic phase was dried over anhydrous sodium sulfate
5. custompurified on a silica gel column (20-80% ethyl acetate/heptanes gradient)