Triphenylphosphine → 4-[1-(1H-indazol-5-ylmethyl)-6-oxo-1,6-dihydropyridazin-3-yl]-N-(3-piperidin-1-ylpropyl)benzamide

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Reaction Steps

Under a nitrogen atmosphere, 38 mg (0.11 mmol) of 4-(6-oxo-1,6-dihydropyridazin-3-yl)-N-(3-piperidin-1-ylpropyl)benzamide are suspended in 1 ml of THF, and 27 mg (0.18 mmol) of (1H-indazol-5-yl)methanol and 88 mg (0.34 mmol) of triphenyphosphine are added. 53 μl (0.34 mmol) of diethyl azodicarboxylate was added dropwise to this suspension at 2-10° C. with ice-cooling. The suspension was stirred at room temperature for 15 h. The reaction mixture was evaporated and purified by means of preparative HPLC.

Provenance & Evidence