反应详情

温度

100 °C

4-[(6-Bromopyridin-2-yl)methyl]morpholine (Example 45, Step 1) (340 mg, 1.32 mmol), 2-amino-5-{[tert-butyl(dimethyl)silyl]ethynyl}thiophene-3-carboxamide (445 mg, 1.59 mmol), Pd2dba3 (121 mg, 0.13 mmol), X-Phos (315 mg, 0.66 mmol), and K2CO3 (201 mg, 1.46 mmol) were combined in a vial, sealed, and evacuated/backfilled with nitrogen. Degassed t-amyl alcohol (3.3 ml), and the reaction was vigorously stirred at 100° C. overnight. The reaction mixture was then diluted with MeOH, combined with silica, and evaporated. Flash chromatography (dry load, 0-10% MeOH/EtOAc) afforded the title compound as a yellow solid.

1. customsealed
2. customevacuated/backfilled with nitrogen
3. additionThe reaction mixture was then diluted with MeOH
4. customevaporated
5. dry with materialFlash chromatography (dry load, 0-10% MeOH/EtOAc)