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