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

Participants

Reaction Steps

To a solution of 5-bromo-1-methyl-1,2-dihydropyridazine-3,6-dione (300 mg, 1.485 mmol) in THF (20 mL) at 0° C. was added PPh3 (781 mg, 2.97 mmol) and ((1S,2S)-2-(1-methyl-1H-indazol-3-yl)cyclopropyl)methanol (300 mg, 1.485 mmol) followed by dropwise addition of DIAD (0.6 mL, 2.97 mmol). The reaction mixture was warmed to ambient temperature. After stirred for 2 h, the mixture was concentrated. The residue was purified by column chromatography on silica gel, eluting with PE/EA (2/1) to give the title compound as oil.

Provenance & Evidence