Phosphorus oxychloride → 4-chloro-5H-pyrrolo[3,2-d]pyrimidine

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Reaction Steps

A mixture of 3,5-dihydropyrrolo[3,2-d]pyrimidin-4-one, (1.8 g, 13.5 mmol, 1 equiv.) and 50 mL of POCl3 was warmed at reflux for 2 hours, cooled to room temperature, and concentrated in vacuo. The residue was then diluted with 200 mL of water, made basic with solid potassium carbonate and extracted with EtOAc. The combined organic layers were dried, filtered, and concentrated in vacuo to provide 1.18 g (57%) of 4-chloro-5H-pyrrolo[3,2-d]pyrimidine as a yellow solid which was used without further purification.

Provenance & Evidence