2-Methoxypyridine-3-boronic acid hydrate → Methyl 4-(4-chloro-2-methoxyphenoxy)-2-fluoro-5-(2-methoxypyridin-3-yl)benzoate

Participants

Reaction Conditions

Reaction Steps

Prepared according to Preparation 2 using methyl 5-bromo-4-(4-chloro-2-methoxyphenoxy)-2-fluorobenzoate (Preparation 17, 0.165 g, 0.423 mmol) and (2-methoxypyridin-3-yl)boronic acid mono hydrate (0.109 g, 0.637 mmol) with an extra addition of water (0.5 mL) and heating for 18 hours at 50° C. The crude product was purified by silica gel chromatography eluting with 0 to 10% EtOAc in DCM to afford the title compound as a clear gum (47.7 mg).

Provenance & Evidence