反应详情

K2CO3 (118 mg, 0.855 mmol) was added to a solution of (S)-tert-butyl 2-(5-((trimethylsilyl)ethynyl)-1H-imidazol-2-yl)pyrrolidine-1-carboxylate (950 mg, 2.85 mmol) in MeOH (25 mL) and the reaction mixture was stirred at RT for 1 h and then heated at 25° C. for 3 h. The reaction was concentrated to remove the volatiles and the residue was taken into MeOH and filtered through a Strata XC MCX cartridge. The cartridge was washed with methanol and the compound was release from the cartridge by eluting with a solution of 2M of ammonia/methanol (40 mL) and concentrated to give a (S)-tert-butyl 2-(5-ethynyl-1H-imidazol-2-yl)pyrrolidine-1-carboxylate (530 mg, 1.41 mmol, 49.6% yield).

1. temperatureheated at 25° C. for 3 h
2. concentrationThe reaction was concentrated
3. customto remove the volatiles
4. filtrationfiltered through a Strata XC MCX cartridge
5. washThe cartridge was washed with methanol
6. washby eluting with a solution of 2M of ammonia/methanol (40 mL)
7. concentrationconcentrated