Hydrogen chloride-ethyl acetate → 2-Pyrrolidinecarboxamide, 4-fluoro-, hydrochloride (1:1), (2S,4S)-

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Reaction Steps

(2S,4S)-1-(tert-Butoxycarbonyl)-2-carbamoyl-4-fluoropyrrolidine (122 g) was suspended in ethyl acetate (400 mL). While stirring this suspension under ice cooling, 4 mol/L hydrochloric acid-ethyl acetate (525 mL) was slowly added dropwise. After stirring at ice-cold temperature for 30 minutes and at room temperature for 3 hours, the precipitated crystal was collected by filtration to give the titled compound (85.9 g, white powder).

Provenance & Evidence