The patent badge is an abbreviated version of the USPTO patent document. The patent badge does contain a link to the full patent document.

The patent badge is an abbreviated version of the USPTO patent document. The patent badge covers the following: Patent number, Date patent was issued, Date patent was filed, Title of the patent, Applicant, Inventor, Assignee, Attorney firm, Primary examiner, Assistant examiner, CPCs, and Abstract. The patent badge does contain a link to the full patent document (in Adobe Acrobat format, aka pdf). To download or print any patent click here.

Date of Patent:
Mar. 11, 2003

Filed:

Oct. 24, 2001
Applicant:
Inventors:

Karl Hansen, Atlantic Highlands, NJ (US);

Paul Devine, Lincroft, NJ (US);

Philippe M. Rabbat, New York, NY (US);

Assignee:

Merck & Co., Inc., Rahway, NJ (US);

Attorney:
Primary Examiner:
Int. Cl.
CPC ...
C07D / ; C07D / ;
U.S. Cl.
CPC ...
C07D / ; C07D / ;
Abstract

Enantiomerically enriched hydroxychromanones are obtained by the AlCl -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.


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