Ethanol → HCID 59334481, 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, pyridin-3-ylboronic acid (191 mg, 1.552 mmol), 2 M aqueous sodium carbonate solution (6 mL) and tetrakis(triphenylphosphine)palladium(0) (71.8 mg, 0.062 mmol) were added to a mixed solution of ethanol (3 mL) and toluene (3 mL), and the mixture was stirred under nitrogen atmosphere with heating at 80° C. for 16 hr. The reaction solution was diluted with ethyl acetate, washed with water and saturated brine, and dried over anhydrous sodium sulfate, and the solvent was evaporated under reduced pressure. The residue was is purified by silica gel column chromatography (methanol/ethyl acetate=0/100→20/80) to give the title compound (187 mg, yield 94%)

Provenance & Evidence