5-Fluoro-2-methoxyphenol is an important pesticide and pharmaceutical intermediate. It can be synthesized from methyl ether using butyllithium and trimethoxyboron in the presence of butyllithium and trimethoxyboron. It is used to synthesize alicylates, a drug for treating hypertension.
In a 500 mL four-necked flask add 150 g (0.9 mol) acetyl guaiacol, glacial acetic acid 240 mL, iodine 2.5 g (0.01 mol) at 25 C, stirring dropwise addition of liquid bromine 160 g (2 mol), dropwise addition is complete, heated to 100 C reaction for 10 h, the reaction mixture was cooled to room temperature, with 3000 mL of ethyl acetate was extracted twice, combined with ethyl acetate layer; washed with 500 mL saturated sodium sulfite, then washed with 500 mL saturated saline, recovery of ethyl acetate to obtain the crude product, light yellow colloidal 180.0 g, light yellow colloidal material. The reaction mixture was cooled to room temperature, extracted with 3000 mL of ethyl acetate twice, combined with the ethyl acetate layer, washed with 500 mL of saturated sodium sulfite, then washed with 500 mL of saturated saline, recovered ethyl acetate to obtain the crude product, light yellow colloidal 180.0 g, purity 98.3%, yield 80.2%.
