7α-Hydroxyacetyl and 7α-Hydroperoxyacetyl-substituted steroid compounds
View Patent ↗The present invention involves intermediates, including a 7α-substituted steroid (II), and processes which are used to prepare eplerenone, a useful pharmaceutical agent.
1. A compound having the structure:
wherein:
R b is selected from the group consisting of —H, C 1 -C 4 alkyl, and phenyl optionally substituted with one or two C 1 -C 4 alkyl or C 1 -C 4 alkoxy; and
R 7-2 is selected from the group consisting of —H and C 1 -C 4 alkyl optionally substituted with one or two —OH.
2. The compound of claim 1 wherein R b is —H.
3. The compound of claim 1 wherein R 7-2 is —H.
4. The compound of claim 1 wherein R 7-2 is methyl.
5. The compound of claim 1 wherein R 7-2 is isopropyl.
6. The compound of claim 1 having the structure:
7. The compound of claim 1 having the structure
8. A compound having the structure:
wherein:
R b is selected from the group consisting of —H, C 1 -C 4 alkyl, and phenyl optionally substituted with one or two C 1 -C 4 alkyl or C 1 -C 4 alkoxy; and
R 7-2 is selected from the group consisting of —H and C 1 -C 4 alkyl optionally substituted with one or two —OH.
9. The compound of claim 8 wherein R b is —H.
10. The compound of claim 8 wherein R 7-2 is —H.
11. The compound of claim 8 wherein R 7-2 is methyl.
12. The compound of claim 8 wherein R 7-2 is isopropyl.
13. The compound of claim 8 having the structure:
14. A compound having the structure:
wherein:
R b is selected from the group consisting of —H, C 1 -C 4 alkyl, and phenyl optionally substituted with one or two C 1 -C 4 alkyl or C 1 -C 4 alkoxy; and
R 7-2 is selected from the group consisting of —H and C 1 -C 4 alkyl optionally substituted with one or two —OH.
15. The compound of claim 14 wherein R b is —H.
16. The compound of claim 14 wherein R 7-2 is —H.
17. The compound of claim 14 wherein R 7-2 is methyl.
18. The compound of claim 14 wherein R 7-2 is isopropyl.
19. The compound of claim 14 having the structure: