Claims
- 1. A process for the production of a compound of formula (A) or a pharmaceutically acceptable salt or solvate thereof: wherein:R1 represents C1-4 alkoxy optionally substituted by one or more fluorine atoms; R2 represents H or C1-6 alkoxy optionally substituted by one or more fluorine atoms; R3 represents a 5- or 6-membered heterocyclic ring containing at least one heteroatom selected from N, O and S, the ring being optionally substituted by one or more groups selected from halogen, C1-4 alkoxy, C1-4 alkyl and CF3; R4 is a 4-, 5-, 6-, or 7-membered heterocyclic ring containing a nitrogen heteroatom, the ring being optionally fused to a benzene ring, the ring system as a whole being optionally substituted by one or more groups independently selected from OH, C1-4 alkoxy, C1-4 alkyl, halogen, CONR7R8, SO2NR7R8, (CH2)bNR7R8, and NHSO2(C1-4 alkyl); the process comprising condensing a compound of formula (B) with a compound of formula (C): whereinR1 to R3 are as defined above; R5 and R6 taken together with the N atom to which they are attached represent a 4-, 5-, 6-, or 7-membered N-containing heterocyclic ring, the ring being optionally fused to a benzene ring, the ring system as a whole being optionally substituted by one or more groups independently selected from OH, C1-4 alkoxy, C1-4 alkyl, halogen, CONR7R8, SO2NR7R8, (CH2)bNR7R8, and NHSO2(C1-4 alkyl); R7 and R8 independently represent H or C1-4 alkyl, or together with the N atom to which they are attached they may represent a 5- or 6-membered heterocyclic ring containing at least one heteroatom selected from N, O and S; and b represents 0, 1, 2 or 3; and where necessary or desired, converting the resulting compound of formula (A) into a pharmaceutically acceptable salt or solvate, or converting the resulting salt or solvate into a compound of formula (A).
- 2. A process as claimed in claim 1, wherein R1 represents methoxy.
- 3. A process as claimed in claim 1, wherein R2 represents methoxy.
- 4. A process as claimed in claim 1, wherein R3 represents an aromatic ring.
- 5. A process as claimed in claim 4, wherein R3 represents pyridinyl, pyrimidinyl, thienyl, furanyl or oxazolyl.
- 6. A process as claimed in claim 5, wherein R3 represents 2-pyridinyl or 2-pyrimidinyl.
- 7. A process as claimed in claim 1, wherein R4 represents a saturated 6-membered N-containing ring which is fused to an optionally substituted benzene ring.
- 8. A process as claimed in claim 7, wherein R4 represents a tetrahydroisoquinoline ring system.
- 9. A process as claimed in claim 8, wherein R4 is 5-methylsulfonylamino-tetrahydroisoquinoline.
- 10. A process as claimed in claim 1, wherein the reaction is carried out in a polar aprotic solvent.
- 11. A process as claimed in claim 10, wherein the polar aprotic solvent is dimethylsulfoxide.
- 12. A process as claimed in claim 1, wherein the reaction is carried out in the presence of a base.
- 13. A process as claimed in claim 12, wherein the base is an alkali metal carbonate.
- 14. A process as claimed in claim 13, wherein the base is caesium carbonate.
- 15. A process as claimed in claim 1, wherein the product is 4-amino-6,7-dimethoxy-2-(5-methanesulfonamido-1, 2, 3, 4-tetrahydoisoquinol-2-yl)-5-(2-pyridyl) quinazoline.
Priority Claims (1)
Number |
Date |
Country |
Kind |
0112061 |
May 2001 |
GB |
|
Parent Case Info
BACKGROUND OF THE INVENTION
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.
US Referenced Citations (1)
Number |
Name |
Date |
Kind |
4758568 |
Campbell et al. |
Jul 1988 |
A |
Foreign Referenced Citations (3)
Number |
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WO 9723462 |
Jul 1997 |
WO |
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Provisional Applications (1)
|
Number |
Date |
Country |
|
60/301750 |
Jun 2001 |
US |