反应详情

A degassed solution of 3-amino-7-fluoro-1H-pyrrolo[3,2-c]pyridine-2-carboxylic acid ethyl ester (1.0 g, 4.48 mmol), trifluoro-methanesulfonic acid 2-fluoro-4-trimethylsilanyl-phenyl ester (1.6 g, 4.93 mmol), Pd2dba3 (205 mg, 0.22 mmol), Xantphos (258 mg, 0.45 mmol) and cesium carbonate (2.0 g, 6.28 mmol) in toluene (20 ml) was subjected to microwave irradiation at 150° C. for 20 minutes. The reaction mixture was cooled to ambient temperature then diluted with ethyl acetate and filtered through a pad of Celite®. The filtrate was concentrated under reduced pressure to give a residue that was purified by flash chromatography (Si-PPC, pentane:diethyl ether, gradient 100:0 to 0:100) to afford the title compound as a yellow solid (505 mg, 29%). LCMS (method B): RT=3.39 min, M+H+=390.

1. customirradiation at 150° C. for 20 minutes
2. filtrationfiltered through a pad of Celite®
3. concentrationThe filtrate was concentrated under reduced pressure
4. customto give a residue that
5. customwas purified by flash chromatography (Si-PPC, pentane:diethyl ether, gradient 100:0 to 0:100)