4-Methylmorpholine → (2-(Trifluoromethyl)pyrimidin-5-yl)methanol

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Reaction Steps

To 0.2 g of 2-trifluoromethyl-pyrimidine-5-carboxylic acid 2 mL of diethyl ether were added, and the solution was cooled in ice-water bath to 0° C. Then 0.126 mL of N-methylmorpholine were added, followed by 0.135 mL of isobutyl-chloroformate. The reaction was left stirring for one hour at room temperature. The yellow solid formed was filtered and washed with diethyl ether. To the filtrate, 0.115 g (3.12 mmol) of sodium borohydride was then added at 0° C. and left stirring at that temperature for one hour. 5 mL of a saturated aqueous solution of sodium and potassium tartrate were then added and the mixture was extracted twice with ethyl acetate, dried with magnesium sulphate, filtered and concentrated to afford 0.09 g of (2-Trifluoromethyl-pyrimidin-5-yl)-methanol as an oil, which was used without further purification.

Provenance & Evidence