(4-Methoxyphenyl)boronic acid → 1-[(4-Chloro-2-fluorophenyl)methyl]-5-(4-methoxyphenyl)-2(1H)-pyridinone

Participants

Reaction Steps

According to Scheme 3 Method A: The title compound was prepared from 1-(4-chloro-2-fluorobenzyl)-5-bromopyridin-2(1H)-one (1 eq, 16.4 mmol, 5.20 g, Example 1 Step 2) and 4-methoxyphenylboronic acid (1.5 eq, 25.0 mmol, 3.80 g) according to the procedure described for Example 1 Step 3. The crude product was purified by flash chromatography over silica gel using CH2Cl2/AcOEt 95/5 to 80/20 as eluent to afford 1-(2-fluoro-4-chlorobenzyl)-5-(4-methoxyphenyl)pyridin-2(1H)-one (16.4 mmol, 5.64 g, 100%) as a white solid.

Provenance & Evidence