|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|
|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.