Phosphorus oxychloride → 1-(3-Chloropyridin-2-yl)-1,2,3,6-tetrahydropyridine-4-carbonitrile

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Reaction Steps

At 0° C., phosphoryl trichloride (10 g, 68 mmol) was slowly added into a solution of 1-(3-chloropyridin-2-yl)-4-hydroxypiperidine-4-carbonitrile (compound 22) (8 g, 33 mmol) in pyridine. After stirred at RT for 30 minutes, the reaction was washed by a HCl solution, and extracted by ethyl acetate. The organic layer was evaporated to give a crude product, which was purified using column chromatography to give the product.

Provenance & Evidence