1,3-Dibromo-2-(2-chloroethoxy)-5-fluorobenzene → 7-Bromo-5-fluoro-2,3-dihydro-1-benzofuran

Participants

Reaction Steps

To the compound (2.5 g, 7.4 mmol) obtained in Step 1, THF (50 mL) was added. At −78° C., a 2.6 M n-butyllithium/n-hexane solution (2.9 mL, 7.5 mmol) was added thereto and stirred for 1 hour, and then stirred at room temperature overnight. The solvent was distilled away under reduced pressure. The resulting residue was subjected to reversed-phase HPLC using ODS as a filler, and eluted with a mixture solution of water and acetonitrile, which contained trifluoroacetic acid at 0.1% (v/v). The target fraction was lyophilized to thus obtain the title compound.

Provenance & Evidence