反应详情

2-(4-Methoxybenzyl)-3,4-dihydro-2,6-naphthyridin-1(2H)-one (I-67g: 300 mg, 1.119 mmol) was reacted with p-toluene sulfonic acid (851 mg, 4.476 mmol) and toluene (10 mL) at 110° C. for 4 hours. The reaction mass was concentrated under reduced pressure, neutralized with 1N HCl solution to pH 7 and extracted using DCM. The organic layer was dried over anhydrous Na2SO4 and concentrated under reduced pressure to afford the crude product. Purification by column chromatography on silica gel (2% methanol in CHCl3) afforded 45 mg of the product (27.10% yield).

1. concentrationThe reaction mass was concentrated under reduced pressure
2. extractionextracted
3. dry with materialThe organic layer was dried over anhydrous Na2SO4
4. concentrationconcentrated under reduced pressure
5. customto afford the crude product
6. customPurification by column chromatography on silica gel (2% methanol in CHCl3)