Phosphorus oxychloride → 2-(4-(2-Amino-4-chloro-6-methylpyrimidin-5-ylthio)phenyl)acetonitrile

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Reaction Steps

A mixture of the product from step (iii) (2.3 g) and POCl3 (25 ml) was heated under reflux for 8 h. The mixture was evaporated under reduced pressure and ice/water added to the residue. The mixture was stirred at rt for 15 min then neutralised with aq. 2M NaOH solution and heated at 40° C. for 2 h then extracted with DCM. The organics were dried, evaporated under reduced pressure and the residue purified by column chromatography (2% MeOH/DCM), to give the subtitle compound as a solid, 530 mg.

Provenance & Evidence