Dimethylformamide → 4-Chloro-1-hydroxy-6-methyl-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-chloro-6-methyl-N-(1-methyl-1-phenylethyl)nicotinamide (500 mg, 1.73 mmol) was dissolved in THF (20 mL), and the solution was treated with n-butyllithium-hexane solution (2.71 mol/L, 4.33 mL, 3.23 mmol) and DMF (0.335 mL, 4.33 mmol), followed by purification by flash column chromatography (hexane/ethyl acetate=80/20 to 75/25) to obtain 4-chloro-1-hydroxy-6-methyl-2-(1-methyl-1-phenylethyl)-1,2-dihydropyrrolo[3,4-c]pyridine-3-one (326 mg, yield 59%).

Provenance & Evidence