Claims
- 1. A compound of formula (I) ##STR6## or a pharmaceutically acceptable salt thereof, wherein R and R.sup.1 are independently hydrogen or fluorine.
- 2. A (+-)-(2R*,3R*,5S*) racemate according to claim 1, and pharmaceutically acceptable salts thereof.
- 3. A (2S,3S,5R) compound according to claim 1 and pharmaceutically acceptable salts thereof.
- 4. A (2R,3R,5S) compound according to claim 1, and pharmaceutically acceptable salts thereof.
- 5. (+-)-(2R*,3R*,5S*)-2-(3-Fluorophenyl)-3,5-dimethylmorpholine and pharmaceutically acceptable salts thereof.
- 6. (2S,3S,5R)-2-(3,4-Difluorophenyl)-3,5-dimethylmorpholine and pharmaceutically acceptable salts thereof.
- 7. A pharmaceutical formulation comprising a compound according to claim 1 together with an acceptable carrier therefor.
- 8. A formulation according to claim 7 adapted for oral administration.
- 9. A formulation according to claim 8 in the form of a capsule or tablet.
- 10. A process for the preparation of a compound of formula (I) ##STR7## or a pharmaceutically acceptable salt thereof, wherein R and R.sup.1 are independently hydrogen or fluorine, said process comprising cyclization of the corresponding compound of formula (II) ##STR8## wherein R and R.sup.1 are as defined in formula (I).
- 11. A method according to claim 10 for the preparation of a (+-)-(2R*,3R*,5S*) racemate of formula (I) or a pharmaceutically acceptable salt thereof.
- 12. A method according to claim 10 for the preparation of a (2S,3S,5R) compound of formula (I) or a pharmaceutically acceptable salt thereof.
- 13. A method according to claim 10 for the preparation of a (2R,3R,5S) compound of formula (I) or a pharmaceutically acceptable salt thereof.
- 14. A method according to claim 10 for the preparation of (+-)-(2R*,3R*,5S*)-2-(3-fluorophenyl)-3,5-dimethylmorpholine, or a pharmaceutically acceptable salt thereof, comprising cyclization of (1R*,2S*)-2-{�(1RS)-2-hydroxy-1-methylethyl!amino}-1-(3-fluorophenyl)propanol.
- 15. A method according to claim 10 for the preparation of (2S,3S,5R)-2-(3,4-difluorophenyl)-3,5-dimethylmorpholine, or a pharmaceutically acceptable salt thereof, comprising cyclization of (1R,2S)-1-(3,4-difluorophenyl)-2-{�(1R)-2-hydroxy-1-methylethyl!amino}propanol.
Priority Claims (1)
Number |
Date |
Country |
Kind |
9108629 |
Apr 1991 |
GBX |
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Parent Case Info
This application is a division of application Ser. No. 08/444,609 filed May 19, 1995 which application is now U.S. Pat. No. 5,648,347, which is U.S. Ser. No. 08/140,010 filed Oct. 22, 1993 now abandoned.
US Referenced Citations (1)
Number |
Name |
Date |
Kind |
5648347 |
Mehta et al. |
Jul 1997 |
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Non-Patent Literature Citations (1)
Entry |
CA 120: 323429, 1992. |
Divisions (1)
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Number |
Date |
Country |
Parent |
444609 |
May 1995 |
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Continuations (1)
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Number |
Date |
Country |
Parent |
140010 |
Oct 1993 |
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