Phosphorus oxychloride → 2-Acetoxymethyl7-chloro-5-methoxycarbonyl-s-triazolo[1,5-a]pyrimidine

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Reaction Steps

Methyl 2-(acetoxymethyl)-4,7-dihydro-7-oxo-s-triazolo[1,5-a]pyrimidine-5-carboxylate (500 mg) (1.87 mmol) are suspended in 20 l of phosphorus oxychloride. The suspension is held under reflux for 5 hours. The mixture is concentrated in a water-jet vacuum, the residue is treated with dichloromethane and ice/water and extracted several times with dichloromethane. After drying and evaporation of the extract the product is crystallized from methanol. There are obtained 400 mg of methyl 2-(acetoxymethyl)-7-chloro-s-triazolo[1,5-a]pyrimidine-5-carboxylate.

Provenance & Evidence