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

Temperatur

80 °C

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 dicholoromethane (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.

1. temperatureAfter cooling to room temperature
2. customthe reaction was quenched with 5% aqueous sodium thiosulphate solution (20 mL)
3. customthe solvent removed in vacuo
4. extractionThe product was then extracted into dicholoromethane (3×20 mL)
5. washthe combined organics were washed with brine (40 mL)
6. dry with materialdried (MgSO4)

ORD-Eintrag

ord-04651d658a8b47e985779050a00e7dee

Quelldatensatz

uspto-grants-2013_02

DOI

10.6084/m9.figshare.5104873.v1

Patentnummer

US08383620B2