Cesium carbonate → HCID 59596595, compound

Participants

Reaction Steps

A degassed solution of 3-amino-1-methyl-1H-pyrrolo[3,2-c]pyridine-2-carboxylic acid ethyl ester (521 mg, 2.4 mmol), 4-cyclopropyl-2-fluoro-1-iodo-benzene (810 mg, 3.09 mmol), Pd2dba3 (154 mg, 0.168 mmol), Xantphos (194 mg, 0.336 mmol) and cesium carbonate (1.95 g, 6.0 mmol) in toluene (5 ml) was heated at 110° C. for 18 hours. The reaction mixture was cooled to ambient temperature then filtered through a pad of Celite®. The filtrate was washed with water and brine, dried over magnesium sulphate and concentrated in vacuo to give a brown gum. The gum was purified by flash chromatography (Si-PPC, DCM:MeOH, 90:10) to provide the title compound as an orange oil (197 mg, 23%). LCMS (method B): RT=2.65 min, M+H+=354.

Provenance & Evidence