1,2-Dimethoxyethane → HCID 59334497, 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, cyclopropylboronic acid (80 mg, 0.931 mmol), potassium carbonate (85.8 mg, 0.621 mmol) and tetrakis(triphenylphosphine)palladium(0) (71.8 mg, 0.062 mmol) were added to a mixed solution of water (0.25 mL) and 1,2-dimethoxyethane (2.75 mL), and the mixture was stirred at 120° C. for 20 min using microwave, thereafter at 130° C. for 40 min. The reaction solution was diluted with ethyl acetate and water, and the aqueous layer was extracted with ethyl acetate. The combined organic layers were 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) and HPLC to give the title compound (68 mg, yield 39%).

Provenance & Evidence