Dimethylformamide → 4,7-Dichloro-1-hydroxy-2-(1-methyl-1-phenylethyl)-1,2-dihydropyrrolo[3,4-c]pyridine-3-one

Participants

Reaction Steps

In a similar manner to Step 2 of Example 16, 2,5-dichloro-N-(1-methyl-1-phenylethyl)nicotinamide (400 mg, 1.29 mmol) was dissolved in THF (16 mL), and the solution was treated with n-butyllithium-hexane solution (2.71 mol/L, 1.20 mL, 3.23 mmol) and DMF (0.250 mL, 3.23 mmol), followed by purification by slurry (diisopropylether) and flash column chromatography (hexane/ethyl acetate=60/40 to 50/50) to obtain 4,7-dichloro-1-hydroxy-2-(1-methyl-1-phenylethyl)-1,2-dihydropyrrolo[3,4-c]pyridine-3-one (312 mg, yield 72%).

Provenance & Evidence