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With tetrakis(triphenylphosphine) palladium(0); sodium carbonate; In 1,4-dioxane; at 150℃; for 0.5h;Sealed tube; Inert atmosphere; Microwave irradiation;
A mixture of 7-chloro-lH-pyrrolo[3,2-b]pyridine (prepared through the procedure described in J. Med. Chem., 2014, 57 (13), 5728-5737; 50 mg, 0.33 mmol), tert-butyl 5-(4,4,5 ,5-tetramethyl- 1 ,3 ,2-dioxaborolan-2-yl)-3 ,6-dihydro-2H-pyridine- 1 -carboxylate (CAS: 1251537-34-4; 111.5 mg, 0.36 mmol) and Pd(PPh3)4 (CAS: 14221-01-3; 38 mg, 0.03 mmol) in 1,4-dioxane (1.29 mL) and Na2C03 (0.75 mL; aq. sat. soltn.) in a sealed tube and under nitrogen atmosphere was stirred at 150 °C for 30 minutes under microwave irradiation. The reaction mixture was diluted with EtOAc and washed with water. The organic layer was separated, dried (MgS04), filtered and the solvent evaporated in vacuo. The residue was purified by flash chromatography (silica, EtOAc in DCM from 0/100 to 100/0). The desired fractions were collected and concentrated in vacuo affording intermediate 42 as a pale yellow solid (82 mg, 84percent yield).
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