Water → HCID 86721473, compound

Participants

Reaction Conditions

Reaction Steps

[step 5] (E)-2-{3-fluoro-8-[(7-bromo-2-methylimidazo[1,2-a]pyridin-3-yl)methyl]dibenzo[b,e]oxepin-11(6H)-ylidene}propanenitrile (350 mg, 0.72 mmol) obtained in step 4 was dissolved in toluene (4.0 mL), cyclopropylboronic acid (123 mg, 1.4 mmol), tricyclohexylphosphine (80 mg, 0.29 mmol), palladium acetate (32 mg, 0.14 mmol), potassium phosphate (532 mg, 2.5 mmol) and water (13 mg, 0.72 mmol) were added, and the mixture was stirred with heating at 100° C. for 3 hr. The reaction mixture was filtered through celite, and the filtrate was concentrated under reduced pressure. The obtained residue was purified by silica gel column chromatography (chloroform/methanol=19/1 v/v) to give the title compound (280 mg, 87%).

Provenance & Evidence