反应详情

A mixture of 2-hydroxy-2-(6-(2,2,2-trifluoroethoxy)pyridin-3-yl)ethyl 4-methylbenzenesulfonate (1.66 g, 4.25 mmol, Step-4, single enantiomer) and potassium carbonate (1.76 g, 12.8 mmol) in methanol (43 mL) is stirred at room temperature for 2 hours. White precipitate is filtrated and filtrate is concentrated in vacuo. The residue is poured into water, extracted with ethyl acetate and dried over sodium sulfate and concentrated in vacuo to give 0.89 g (95% yield) of the title compound as colorless oil. This material is used for the next reaction (Step-6) without further purification.

1. filtrationWhite precipitate is filtrated
2. concentrationfiltrate is concentrated in vacuo
3. additionThe residue is poured into water
4. extractionextracted with ethyl acetate
5. dry with materialdried over sodium sulfate
6. concentrationconcentrated in vacuo