Process for preparing hydroxychomanones and cis-aminochromanols
US6531617B2 · kind B2 · utility
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25Claims
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Key dates
| Filing date | Oct 24, 2001 |
| Grant date | Mar 11, 2003 |
| Priority date | — |
| Expiry date | Dec 15, 2021 |
Classification
- Technology area (CPC C)Chemistry; Metallurgy
- CPC primaryC07D311/22
- WIPO fieldOrganic fine chemistry
- WIPO sectorChemistry
Abstract
Enantiomerically enriched hydroxychromanones are obtained by the AlCl3-catalyzed intramolecular Friedel-Crafts acylation of the corresponding 3-phenoxy-2-alkylcarbonyloxy-propionic acid followed by cleavage of the carboxylate in the presence of an alkali metal peroxide or hydroperoxide. Enantiomerically enriched cis-aminochromanols can then be prepared by treating the hydroxychromanones with a hydroxylamine and hydrogenating the resulting oxime. The cis-aminochromanols can be employed as intermediates in the production of HIV protease inhibitors which are useful for treating HIV infection and AIDS.
Source: USPTO / EPO open patent data. Objective bibliographic and citation counts.