401930-07-2

5382-16-1

33034-67-2

401930-07-2

Using 4-hydroxypiperidine (1.65 g, 16.3 mmol) and 2-chloro-4-trifluoromethylpyrimidine (2.98 g, 16.3 mmol) as the raw material, triethylamine (4.5 mL, 32.7 mmol) was added to isopropanol (60 mL) and the mixture was heated and refluxed for 5 hours. Upon completion of the reaction, it was cooled to room temperature and diluted with hexane and white precipitate formation was observed. The solids were removed by filtration and the filtrate was subsequently purified by passing it through a silica plug and washed sequentially with a 1:1 solvent mixture of EtOAc/hexane and pure EtOAc. The collected filtrate and washings were combined and concentrated to dryness to afford the target product 1-[4-(trifluoromethyl)-2-pyrimidinyl]-4-piperidinol (3.89 g). The exact mass calculated value of the product (C10H11F3N2O) was 247.09 and the measured LCMS value was 248.2 [M+H]+.