Potassium Carbonate → HCID 59334627, compound

Participants

Reaction Conditions

Reaction Steps

N-{[2-(5-Bromo-2-methyl-2H-indazol-4-yl)cyclopropyl]methyl}acetamide (200 mg, 0.621 mmol) obtained in Example 29, ethylboronic acid (229 mg, 3.105 mmol), dicyclohexyl(2′,4′,6′-triisopropylbiphenyl-2-yl)phosphine (30.0 mg, 0.0621 mmol), potassium carbonate (206 mg, 1.49 mmol) and tris(dibenzylideneacetone)dipalladium(0) (29.3 mg, 0.0311 mmol) were added to N,N-dimethylformamide (3.1 mL), and the mixture was stirred under nitrogen atmosphere with heating at 120° C. for 1 day. The reaction solution was diluted with ethyl acetate, and filtered through celite. The obtained filtrate was washed with water and saturated brine, and dried over anhydrous sodium sulfate, and the solvent was evaporated under reduced pressure. The residue was purified by silica gel column chromatography (NH, methanol/ethyl acetate=0/100→5/95), silica gel column chromatography (NH, methanol/ethyl acetate=0/100→20/80) and HPLC to give the title compound (31 mg, yield 18%).

Provenance & Evidence