Hydrogen chloride-ethyl acetate → (trans)-3-Azido-4-fluoropyrrolidine

Participants

Reaction Steps

To a solution of (trans)-tert-butyl 3-azido-4-fluoropyrrolidine-1-carboxylate (25 g, 109 mmol), as prepared in step 3 of Preparation 3, in EtOAc (100 mL) was added HCl/EtOAc (50 mL) at 0-5° C. Then the mixture was stirred at rt for 4 hr. The solid was filtered and washed with petroleum ether/EtOAc (2:1, 40 mL) to give the title compound (18 g) as a gray solid, which was used directly in the next step.

Provenance & Evidence