Phosphorus oxychloride → 4-Chloro-2-methyl-7-(trifluoromethyl)quinoline

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Reaction Steps

2-Methyl-7-(trifluoromethyl)quinolin-4-ol (1 g, 4.4 mmol) was heated in phosphoroxychloride (3 ml) for under reflux for one hour. The mixture was poured on ice and left at 4° C. overnight. The mixture was extracted with ethylacetate, the organic phase was washed with water, dried over sodium sulfate and evaporated to dryness under reduced pressure to yield 1.1 g (4.4 mmol, quantitative) which were used directly in the next step.

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