SYNTHESIS AND REGIOSELECTIVE SUBSTITUTION OF 6-HALO-AND 6-ALKOXY NICOTINE DERIVATIVES

Abstract

The present invention provides active compounds for modulating nicotinic acetylcholine receptors and methods of making the same. The methods of preparing the active compounds utilize different intermediate compounds.

Description

Claims

1. A method for making a compound of Formula Ia:

2. A method of making a compound of Formula III

3. A method of making a compound of Formula III

4. A method of making compounds of Formula III:

5. A method of making compounds of Formula Ia

6. A method of making a compound of Formula VI:

7. A method of making a compound of Formula VI:

8. A compound of Formula A:

9. A compound of claim 8, subject to the proviso that neither R5 nor R6 is the same as R4.

10. A composition comprising a compound of claim 8 in a pharmaceutically acceptable carrier.

11. A compound of Formula A:

12. A compound of claim 11, wherein R4 and R5 together form a fused ring.

13. A compound of claim 11, wherein R5 and R6 together form a fused ring.

14. A compound of claim 11, wherein n is 0.

15. A composition comprising a compound of claim 11 in a pharmaceutically acceptable carrier.