Diastereoselective Process Leading To A Key Intermediate For The Preparation Of Fluorinated Reverse Transcriptase Inhibitors
Description of Invention:
A novel process has been developed for synthesizing a key intermediate in the preparation of fluorinated reverse transcriptase inhibitors. Recently, several fluorinated dideoxynucleotides have been found to be effective inhibitors of reverse transcriptase and, thus, offer promise for replacing or augmenting current drugs for the treatment of HIV-1 infection; however, chemically synthesizing these fluorinated dideoxynucleotides is quite expensive, making it economically difficult to produce large-scale amounts for testing. This new process allows the synthesis of a key intermediate in the production of fluorinated dideoxynucleotides at much lower costs because the reaction is diastereoselective, meaning that there are fewer side reactions and more primary product is produced.
Inventors:
VE Marquez (NCI) JS Driscoll (NCI) MA Siddiqui (NCI)
Patent Status:
DHHS Reference No. E-023-1994/0 --
U.S. Patent No. 5,498,719 issued 12 Mar 1996
For Additional Information Please Contact: Sally Hu PhD MBA
NIH Office of Technology Transfer
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Email: hus@mail.nih.gov
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