反应详情

To a solution of 4-[2-(2-chloro-pyrimidin-5-ylamino)-ethyl]-piperidine-1,4-dicarboxylic acid 1-tert-butyl ester 4-ethyl ester (188 mg, 0.46 mmol) in tetrahydrofuran (4 mL) was added 1 M solution of potassium-tert-butoxide in tetrahydrofuran (0.55 mL, 0.55 mmol). The resulting mixture was stirred for 2 hours at ambient temperature and then added NaHCO3 (aq) (20 mL), extracted with EtOAc (2×20 mL). The combined organic extracts were dried over Na2SO4, filtered and concentrated to afford a crude solid which was then purified by flash column chromatography (0 to 10% MeOH/CH2Cl2) to provide 125 mg (74% yield) of the title compound as a solid.

1. extractionadded NaHCO3 (aq) (20 mL), extracted with EtOAc (2×20 mL)
2. dry with materialThe combined organic extracts were dried over Na2SO4
3. filtrationfiltered
4. concentrationconcentrated
5. customto afford a crude solid which
6. customwas then purified by flash column chromatography (0 to 10% MeOH/CH2Cl2)