Potassium Carbonate → HCID 89650147, compound

Participants

Reaction Conditions

Reaction Steps

A mixture of 2-fluoro-benzaldehyde (0.85 mL; 8.06 mmol; 1 eq.), 3-hydroxymethyl-azetidine-1-carboxylic acid tert-butyl ester (1.66 g; 8.86 mmol; 1.1 eq.) and K2CO3 (2.23 g; 16.11 mmol; 2 eq.) in DMF (20 mL) was stirred at 120° C. for 7 days. The reaction mixture was diluted with sat. aq. NaHCO3 and extracted with DCM (2×). The combined organic layer was washed with brine (2×), dried over magnesium sulfate and concentrated in vacuo. Purification by column chromatography (heptane/EA, 95/5 to 60/40) afforded the title compound (810 mg, 35%) as a white solid. HPLC (max plot) 96.2%; Rt 4.15 min.

Provenance & Evidence