Process for preparing optically active (S)-2-acetyl-7-(2-hydroxy-3-isopropylaminopropoxy)benzofuran and salts thereof.

摘要

(S)-(+)-2-acetyl-7-(2,3-epoxypropoxy)benzofuran (SEBF) is prepared by subjecting 2-acetyl-7-hydroxybenzofuran and [R]-glycidol to dehydration condensation in an inert organic solvent in the presence of triphenylphosphine and a dialkyl azodicarboxylate. The [S]-(+)-2-actyl-7-(2,3-epoxypropoxy) benzofuran can be easily converted into [S]-2-acetyl-7-(2-hydroxy-3-isopropylaminopropoxy) benzofuran ([S]-befunolol) or salts thereof which are useful as a beta -adrenergic blocking agent, by reacting it with isopropylamine.