Claims
- 1. A compound of the formula:
- 2. A polymorphic form of a compound of the formula: which is characterized by an X-ray powder diffraction pattern with key reflections at approximately: 8.45, 16.94, 18.16 and 21.41° (2 theta).
- 3. The polymorphic form of claim 2 which is further characterized by a melting point of 136° C.
- 4. A polymorphic form of a compound of the formula: which is characterized by an X-ray powder diffraction pattern with key reflections at approximately: 16.56, 18.88, 19.36 and 23.56° (2 theta).
- 5. The polymorphic form of claim 3 which is further characterized by a melting point of 134° C.
- 6. A compound of the formula:
- 7. A process for the preparation of a compound of the formula: which comprises:reacting N-benzylethanolamine of the formula: with glyoxylic acid of the formula: in a solvent to give the compound of the formula:
- 8. The process of claim 7 wherein the solvent comprises:acetone, 2-butanone, dimethylformamide, N,N-dimethylacetamide, dimethylsulfoxide, methanol, ethanol, 1-propanol, 2-propanol, N-methylpyrrolidinone, 1,4-dioxane, 1,3-dioxolane, tetrahydrofuran, acetonitrile, mixtures therof, and mixtures of these with water.
- 9. The process of claim 7 wherein the solvent comprises:tetrahydrofuran, acetonitrile, mixtures thereof, and a mixtures of these with water.
- 10. The process of claim 7 wherein the solvent comprises a mixture of tetrahydrofuran and water.
- 11. The process of claim 7 wherein the temperature of the reaction mixture is between about ambient room temperature and about 100° C.
- 12. The process of claim 7 wherein the glyoxylic acid employed is present as a solution in water.
- 13. The process of claim 7 which comprises the additional step of isolating the intermediate compound of the formula: followed by heating such compound in a solvent to give the 4-benzyl-2-hydroxy-1,4-oxazin-3-one.
- 14. A process for the preparation of 4-benzyl-2-hydroxy-1,4-oxazin-3-one which comprises:reacting N-benzylethanolamine with glyoxylic acid in a mixture of tetrahydrofuran and water at solvent reflux, to give 4-benzyl-2-hydroxy-1,4-oxazin-3-one.
Parent Case Info
This application claims benefit of U.S. Provisional application Nos. 60/200,204 and 60/210,254 both filed on Jun. 8, 2000.
Non-Patent Literature Citations (2)
Entry |
Perrone et al. Synthesis 598-600, 1976.* |
Le Rouzic-Bellevre, C. R. Hebd. Seances Acad. Sci., Ser. C, 282(6), 307-310, 1976. |
Provisional Applications (2)
|
Number |
Date |
Country |
|
60/210254 |
Jun 2000 |
US |
|
60/210204 |
Jun 2000 |
US |