反应详情

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0 °C

4-(2-hydroxy-ethyl)-N-(4-methoxy-benzyl)-nicotinamide (2.2 g, 7.683 mmol) and triphenylphosphine (4.03 g, 15.37 mmol) were dissolved in 50 mL of anhydrous THF. The mixture, while being stirred at 0° C. under the nitrogen atmosphere, dropwisely added with diethyl azocarboxylate (1.4 mL, 9.220 mmol) and stirred for about 1 hour at room temperature. The mixture was then concentrated under reduced pressure and a silica gel column chromatography (3% MeOH/MC) was performed on the resulting residue and obtained 1.88 g (91%) of 2-(4-methoxy-benzyl)-3,4-dihydro-2H-[2,7]naphtyridine-1-on in white solid.

1. stirringstirred for about 1 hour at room temperature
2. concentrationThe mixture was then concentrated under reduced pressure