Pyridinium chloride → 1,2-Benzisothiazol-6-ol

Participants

Reaction Steps

A method similar to the method described in WO 04/043904 was used. 6-Methoxybenzo[d]isothiazole (450 mg, 2.73 mmol) and pyridine hydrochloride (3.2 g, 27.27 mmol) were heated at 210° C. in a microwave oven for 20 min. The residue was partitioned between water (30 mL) and EtOAc (3×20 mL). The combined organic layers were dried (MgSO4) and concentrated in vacuo. The residue was purified by chromatography on silica gel with EtOAc:heptane (1:1, v/v) as eluent to afford benzo[d]isothiazol-6-ol as a white solid (345 mg, 83%).

Provenance & Evidence