Method of Preparing a Production Intermediate for HIV Protease Inhibitors
Description of Invention:
The invention describes a novel process amenable for the large-scale practical synthesis of cis-tetrahydro-furo[2,3-b]furan-3-one. This compound is useful as a key intermediate for the synthesis of highly potent and resistance-repellent HIV protease inhibitors that share a common component called bis-tetrahydrofuran (bis-THF). Specifically, the invention provides a method of preparing these precursors by modification of reaction temperatures, conditions and reagents leading to increased yields and purity of the desired intermediates. Such modifications would be useful in the large-scale preparation of highly potent and resistance-repellent HIV protease inhibitors currently under development as antiviral agents useful in treating AIDS.
Inventors:
Guangyang Wang Michael A. Eissenstat and Tatiana Guerassina (NCI)
Patent Status:
DHHS Reference No. E-188-00/0 filed 24 Jan 2000
For Additional Information Please Contact: Sally Hu PhD MBA
NIH Office of Technology Transfer
6011 Executive Blvd, Suite 325
Rockville, MD 20852-3804
Phone: (301) 435-5606
Email: hus@mail.nih.gov
Fax: (301) 402-0220
