4-Benzyloxy-2(1H)-pyridone → 4-Benzyloxy-1-{2-oxo-2-[3-(2,2,2-trifluoro-acetyl)-2,3,4,5-tetrahydro-1H-3-benzazepin-7-yl]-ethyl}-1H-pyridin-2-one

Participants

Reaction Steps

To 8.05 g (40.0 mmol) 4-benzyloxy-1H-pyridin-2-one in 50 mL THF is added at 0° C. subsequently 4.94 g (44.0 mmol) potassium tert-butylate, 739 mg (2.00 mmol) tert-butyl ammonium-iodide and 15.3 g (48.0 mmol) 1-[7-(2-chloro-acetyl)-1,2,4,5-tetrahydro-3-benzazepin-3-yl]-2,2,2-trifluoro-ethanone. The reaction mixture is stirred overnight at RT and poured onto 500 mL water. 100 ml tert-butylmethylether is added. The precipitate is collected and dried. The product, which contains 20% 1-[7-(2-chloro-acetyl)-1,2,4,5-tetrahydro-3-benzazepin-3-yl]-2,2,2-trifluoro-ethanone is used without further purification in the next step.

Provenance & Evidence