Trimethyl borate → (2-Fluoro-5-methoxy-4-methylphenyl)boronic acid

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Reaction Steps

To 122D (750 mg, 2.8 mmol) in THF (10 mL) was added n-BuLi (1.6M in hexane, 2.3 mL) at −78° C. After stirring for 10 min, trimethyl borate (0.63 mL) was introduced. The mixture was stirred from −78° C. to rt for 3 h before it was quenched by 1N HCl and extracted with ethyl acetate. The organic extracts were washed with saturated Na2S2O3, brine and dried over MgSO4. Evaporation of the solvent gave product 122E (356 mg, 69% yield) as a solid. 1H NMR (400 MHz, CDCl3) δ ppm 2.18 (s, 3H) 3.80 (s, 3H) 6.80-6.86 (m, 2H).

Provenance & Evidence