Ethanol → HCID 59334593, compound

Participants

Reaction Conditions

Reaction Steps

N-{[2-(5-Bromo-2-methyl-2H-indazol-4-yl)cyclopropyl]methyl}acetamide (100 mg, 0.310 mmol) obtained in Example 29, phenylboronic acid (94.6 mg, 0.776 mmol), 2 M aqueous sodium carbonate solution (3 mL) and tetrakis(triphenylphosphine)palladium(0) (35.8 mg, 0.031 mmol) were added to a mixed solution of ethanol (1.5 mL) and toluene (1.5 mL), and the mixture was stirred under nitrogen atmosphere with heating at 80° C. for 15 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 purified by silica gel column chromatography (methanol/ethyl acetate=0/100→10/90) to give the title compound (98.9 mg, yield 99%).

Provenance & Evidence