Claims
- 1. A process for the production of a compound of formula (A) or a pharmaceutically acceptable salt or solvate thereof:
- 2. The process of claim 1, wherein R1 represents methoxy.
- 3. The process of claim 1, wherein R2 represents methoxy.
- 4. The process of claim 1, wherein R3 represents an aromatic heterocyclic ring.
- 5. The process of claim 4, wherein R3 represents pyridinyl, pyrimidinyl, thienyl, furanyl or oxazolyl.
- 6. The process of claim 5, wherein R3 represents 2-pyridinyl or 2-pyrimidinyl.
- 7. The process of claim 1, wherein R4 represents a saturated 6-membered N-containing ring which is fused to an optionally substituted benzene or pyridine ring.
- 8. The process of claim 7, wherein R4 represents a tetrahydroisoquinoline ring system, which is optionally substituted.
- 9. The process of claim 8, wherein R4 is 5-methylsulfonylamino-tetrahydroisoquinoline.
- 10. The process of claim 1, wherein the reaction is carried out in a polar aprotic solvent.
- 11. The process of claim 10, wherein the polar aprotic solvent is dimethylsulfoxide.
- 12. The process of claim 1, wherein the reaction is carried out in the presence of a base.
- 13. The process of claim 12, wherein the base is an alkali metal carbonate.
- 14. The process of claim 13, wherein the base is caesium carbonate.
- 15. The process of claim 1, wherein the product is 4-amino-2-(5-methane-sulfonamido-1,2,3,4-tetrahydroisoquinol-2-yl)-6,7-dimethoxy-5-(2-pyridyl)quinazoline.
- 16. The process of claim 1, wherein a compound of formula (B) is formed by reaction of a compound of formula (D):
- 17. The process of claim 16, wherein the pyridine derivative is a pyridyl boronate.
- 18. The process of claim 16, wherein the reaction is carried out in the presence of a Pd(0) catalyst.
- 19. The process of claim 16, wherein the product is 6-fluoro-3,4-dimethoxy-2-(2-pyridyl)benzonitrile.
- 20. A compound of formula (B), having the structure:
- 22. A compound of formula (C), as defined in claim 1.
Priority Claims (1)
Number |
Date |
Country |
Kind |
0112061.7 |
May 2001 |
GB |
|
Parent Case Info
[0001] The present application claims the benefit of U.S. Provisional Patent Application Serial No. 60/301,750, filed Jun. 28, 2001, the contents of which are hereby incorporated by reference.
Provisional Applications (1)
|
Number |
Date |
Country |
|
60301750 |
Jun 2001 |
US |