Phosphorus oxychloride → Ethyl 2-chloroindolizine-1-carboxylate

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Reaction Steps

To a solution of 3.0 g of ethyl 2-hydroxypyrrolo [1,2-a]pyridine-1-carboxylate in 50 ml of acetonitrile, 2.7 g of phosphorus oxychloride is added at room temperature and stirred for 2 hours. The reaction mixture is concentrated under reduced pressure, added with water and then extracted with dichloromethane. The extract is dried on anhydrous sodium sulfate and distilled to remove dichloromethane. The residue is purified by silica gel chromatography (eluent: n-hexane-ethyl acetate) to give 2.0 g of the title compound as crystals.

Provenance & Evidence