Potassium Phosphate, Tribasic → 2-(4-methylpyridin-3-yl)-3,4-dihydro-2,7-naphthyridin-1(2H)-one

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Reaction Steps

3,4-Dihydro-2,7-naphthyridin-1(2H)-one (I-65f: 80 mg, 0.5399 mmol) was reacted with 3-iodo-4-methylpyridine (177 mg, 0.8099 mmol), copper iodide (8 mg, 10% w/w), trans-N,N′-dimethyl-cyclohexyl-1,2-diamine (16 mg, 20% w/w) and potassium phosphate (287 mg, 1.3498 mmol) in 1,4-dioxane (5 mL) to afford the crude product. Purification by column chromatography on silica gel (3% methanol in CHCl3), followed by preparative HPLC afforded 16 mg of the product (12.4% yield).

Provenance & Evidence