反应详情

2-Chloro-6-iodopyridine (400 mg, 1.67 mmol), N-methylindole-2-boronic acid (292 mg, 1.67 mmol), tetrakis(triphenylphosphine)palladium (0) (154 mg, 0.13 mmol) and Na2CO3 (442 mg, 4.18 mmol) were dissolved in water (10 mL) and dioxane (10 mL) and heated using a microwave (110° C., absorption high) for 1 h. The solvents were removed in vacuo and the residue was partitioned between DCM (50 mL) and water (30 mL). The aq fraction was extracted with DCM (30 mL) and the combined organic fractions were dried (MgSO4) and concentrated in vacuo to give the crude title compound (406 mg) as a brown gum. LCMS (ES+): 243.2 [MH]+.

1. customa microwave (110° C., absorption high) for 1 h
2. customThe solvents were removed in vacuo
3. customthe residue was partitioned between DCM (50 mL) and water (30 mL)
4. extractionThe aq fraction was extracted with DCM (30 mL)
5. dry with materialthe combined organic fractions were dried (MgSO4)
6. concentrationconcentrated in vacuo