Process for preparing optically active [S]-2-acetyl-7-(2-hydroxy-3-isopropylaminopropoxy)benzofuran and salts thereof
US4515977A · kind A · utility
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Key dates
| Filing date | Mar 16, 1983 |
| Grant date | May 7, 1985 |
| Priority date | — |
| Expiry date | Mar 16, 2003 |
Classification
- Technology area (CPC C)Chemistry; Metallurgy
- CPC primaryC07D307/86
- WIPO fieldOrganic fine chemistry
- WIPO sectorChemistry
Abstract
[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-acetyl-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.
Source: USPTO / EPO open patent data. Objective bibliographic and citation counts.