Triphenylphosphine → 4-bromo-2-methyl-6-(((1S,2S)-2-(5-methylpyridin-2-yl)cyclopropyl)methoxy)pyridazin-3(2H)-one

Participants

Reaction Steps

To a solution of 5-bromo-1-methyl-1,2-dihydropyridazine-3,6-dione (100 mg, 0.49 mmol) in THF (3 mL) at 0° C. was added triphenyl phosphorous (257 mg, 0.98 mmol) and ((1S,2S)-2-(5-methylpyridin-2-yl)cyclopropyl)methanol (4) (80 mg, 0.49 mmol) followed by dropwise addition of DIAD (198 mg, 0.98 mmol). The reaction mixture was warmed to ambient temperature. After stirred for 1 h, the mixture was concentrated. The residue was purified by column chromatography on silica gel, eluting with PE/EA (1/2) to give the title compound as oil.

Provenance & Evidence