反应详情

A degassed solution of 3-amino-7-fluoro-1-methyl-1H-pyrrolo[3,2-c]pyridine-2-carboxylic acid ethyl ester (900 mg, 3.8 mmol), trifluoro-methanesulfonic acid 2-fluoro-4-trimethylsilanyl-phenyl ester (1.44 mg, 4.56 mmol), Pd2dba3 (174 mg, 0.19 mmol), Xantphos (220 mg, 0.38 mmol) and Cs2CO3 (2.48 g, 7.6 mmol) in toluene (10 ml) was heated at 150° C. for 20 minutes using microwave irradiation. The reaction mixture was cooled to ambient temperature then filtered through a pad of Celite® washing with ethyl acetate. The filtrate was concentrated in vacuo and the resultant residue subjected to flash chromatography (Si-PPC, gradient 0-30% ethyl acetate in cyclohexane) to provide the title compound as a yellow/orange solid (2.12 g, 69%). LCMS (method B): RT=4.15 min, M+H+ 404.

1. custommicrowave irradiation
2. filtrationthen filtered through a pad of Celite®
3. washwashing with ethyl acetate
4. concentrationThe filtrate was concentrated in vacuo