Process for preparing optically active ¬s|-2-...

C - Chemistry – Metallurgy – 07 – D

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C07D 407/12 (2006.01) C07D 301/02 (2006.01) C07D 307/86 (2006.01)

Patent

CA 1190238

Abstract of the Disclosure [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.

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