4-Methoxy-2-pyrimidinamine → 5-Iodo-4-methoxypyrimidin-2-amine

Participants

Reaction Conditions

Reaction Steps

To a solution of 4-methoxy-pyrimidin-2-ylamine (405 mg) in acetic acid (10 mL) was added N-iodosuccinimide (950 mg) and the mixture was heated at 80° C. for 4 h. After cooling to room temperature, the reaction was quenched with 5% aqueous sodium thiosulphate solution (20 mL) and the solvent removed in vacuo. The product was then extracted into dichloromethane (3×20 mL) and the combined organics were washed with brine (40 mL), dried (MgSO4) and reduced in vacuo to give 5-iodo-4-methoxy-pyrimidin-2-ylamine as a white solid.

Provenance & Evidence