Phosphorus oxychloride → 7-Chloro-1-methyl-2,3-dihydroimidazo[1,2-C]pyrimidin-5(1H)-one

Participants

Reaction Conditions

Reaction Steps

A suspension of 1-methyl-2,3-dihydroimidazo[1,2-c]pyrimidine-5,7(1H,6H)-dione (0.41 g, 2.45 mmol) in POCl3 (15 mL, 161 mmol) was stirred at 90° C. for 6 h. The suspension was concentrated in vacuo to remove all of POCl3. Cold water was added to the resultant residue, and then solid NaOH was added dropwise to adjust pH to ˜12. The solution was stirred at rt for 2 h. Aqueous HCl was added to adjust pH to ˜7. Purification via Mass Directed AutoPrep (MDAP) afforded the title compound as a white solid (0.42 g, 93% yield).

Provenance & Evidence