(E)-ethyl 4-(2-(dimethylamino)vinyl)-2-(methylthio)pyrimidine-5-carboxylate → 2-(methylsulfanyl)-5H,6H-pyrido(4,3-d)pyrimidin-5-one

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Reaction Steps

4-((E)-2-Dimethylamino-vinyl)-2-methylsulfanyl-pyrimidine-5-carboxylic acid ethyl ester 5 (13.5 g, 50.5 mmol) and NH4OAc (38.9 g, 505 mmol) were dissolved in DMF (250 mL) and stirred at reflux for about four days. Then mixture was concentrated, residue dissolved in TCM, washed with water, dried, filtered, and concentrated. The product was purified by crystallization from ethanol to obtain a colorless solid (7.60 g, 39.4 mmol, 78%).

Provenance & Evidence