Phosphorus oxychloride → 1-(4-Chloropyrimidin-2-yl)pyrrolidin-3-ol

Participants

Reaction Conditions

Reaction Steps

To a solution of 2-(3-hydroxypyrrolidin-1-yl)pyrimidin-4-ol (4.0 g, 23 mol) in DMF (50 mL) was added POCl3 (4.2 g, 27 mmol). The reaction mixture was stirred at 50° C. for 2 hours. The reaction mixture was poured into 200 mL ice-water. The resulting solution was concentrated at 60° C. under vacuum. The residue was purified by acidic reverse phase HPLC (10-100% acetonitrile/water+0.05% TFA modifier) to afford the title compound.

Provenance & Evidence