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Details for Patent: 5,539,116

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Details for Patent: 5,539,116

Title: Method and compositions for the synthesis of BCH-189 and related compounds
Abstract:The present invention relates to a method of preparing BCH-189 and various analogs of BCH-189 from inexpensive precursors with the option of introducing functionality as needed. This synthetic route allows the stereoselective preparation of the biologically active isomer of these compounds, .beta.-BCH-189 and related compounds. Furthermore, the steochemistry at the nucleoside 4' position can be controlled to produce enantiomerically-enriched .beta.-BCH-189 and its analogs.
Inventor(s): Liotta; Dennis C. (Stone Mountain, GA), Choi; Woo-Baeg (Atlanta, GA)
Assignee: Emory University (Atlanta, GA)
Filing Date:Feb 10, 1993
Application Number:08/015,992
Claims:1. The (-)-enantiomer of the .beta.-isomer of 2',3'-dideoxy-3'-thia-cytidine (BCH-189).

2. The (-)-enantiomer of the .beta.-isomer of 2',3'-dideoxy-3'-thia-cytidine (BCH-189), in substantially pure form.

3. The (-)-enantiomer of the .beta.-isomer of 2',3'-dideoxy-3'-thia-cytidine substantially free of the (+)-enantiomer of the .beta.-isomer of 2',3'-dideoxy-3'-thia-cytidine.

4. A composition consisting essentially of the (-)-enantiomer of the .beta.-isomer of 2',3'-dideoxy-3'-thia-cytidine.

5. .beta.-BCH-189 substantially in the form of one optical isomer.

6. A composition consisting essentially of one optical isomer of .beta.-BCH-189.

7. Enantiomerically enriched .beta.-BCH-189.
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