4-Piperidinecarboxylic acid → 5-Bromo-7-fluoro-2-(piperidin-4-yl)benzo[d]oxazole

Participants

Reaction Conditions

Reaction Steps

2-amino-4-bromo-6-fluorophenol (1.7 g, 8.24 mmol) and isonipecotic acid (1.06 g, 8.24 mmol) were dissolved in polyphosphoric acid (28 g). This mixture was heated to 195° C. for 3 h. After 3 h, reaction mixture cooled to rt and basified with aqueous NaOH solution to pH 14. Solid that obtained was filtered and dried to obtain the title compound (1.3 g) as a brown solid.

Provenance & Evidence