Benzyl chloroformate → 1-[(Benzyloxy)carbonyl]azetidine-3-carboxylic acid

Participants

Reaction Steps

To azetidine-3-carboxylic acid (0.50 g), potassium carbonate (0.82 g), dioxan (5 mL), water (10 mL) was added benzyl chloroformate (0.74 mL) at room temperature for 6 h under nitrogen. Piperazine (5 drops) was then added. After ½ h, the dioxan was removed in vacuo and the residue diluted with 2M hydrochloric acid (25 mL). After extracting with ethyl acetate (35 mL), the organic layer was washed with brine (10 mL) and dried (MgSO4). Solvent removal in vacuo gave Intermediate 13 as a colourless oil (1.07 g).

Provenance & Evidence