Claims
- 1. A method of making a compound of the formula (V-1):
- 2. The method of claim 1, further comprising formation of the compound of the formula (VIh-1) by reacting a compound of the formula (VIIa-1)
- 3. The method of claim 2, further comprising formation of the compound of the formula (VIIa-1) by reacting a compound of the formula (VIII-1)
- 4. A method of making a compound of the formula (V-1):
- 5. The method of claim 2, wherein with the organozinc compound has the formula formula X—Zn—(C1-C6)alkyl-(C═O)—O—R, wherein X is a halogen and R is a (C1-C20)alkyl, (C3-C10)cycloalkyl, aryl, or (C2-C9)heteroaryl.
- 6. The method of claim 4, wherein with the organozinc compound has the formula formula X—Zn—(C1-C6)alkyl-(C═O)—O—R, wherein X is a halogen and R is a (C1-C20)alkyl, (C3-C10)cycloalkyl, aryl, or (C2-C9)heteroaryl.
- 7. The method of claim 2, wherein with the organozinc compound has the formula
- 8. The method of claim 4, wherein with the organozinc compound has the formula
- 9. The method of claim 2, wherein the organozinc compound has the formula
- 10. The method of claim 4, wherein the organozinc compound has the formula
- 11. The method of claim 2, wherein the racemization scavenger is a carboxylic acid anhydride or a carboxylic acid ester.
- 12. The method of claim 4, wherein the racemization scavenger is a carboxylic acid anhydride or a carboxylic acid ester.
- 13. The method of claim 2, wherein the racemization scavenger has the formula aryl-(C═O)—O—(C═O)-aryl, R—(C═O)—O-aryl, or aryl-(C═O)—O-aryl.
- 14. The method of claim 4, wherein the racemization scavenger has the formula aryl-(C═O)—O—(C═O)-aryl, R—(C═O)—O-aryl, or aryl-(C═O)—O-aryl.
- 15. The method of claim 13, wherein the racemization scavenger is phthalic anhydride, 4-nitrophenyl acetate, or 4-fluorophenyl acetate.
- 16. The method of claim 14, wherein the racemization scavenger is phthalic anhydride, 4-nitrophenyl acetate, or 4-fluorophenyl acetate.
- 17. The method of claim 1, wherein P is carbobenzyloxy, t-butoxy carbonyl or 9-fluorenyl-methylenoxycarbonyl.
- 18. The method of claim 4, wherein P is carbobenzyloxy, t-butoxy carbonyl or 9-fluorenyl-methylenoxycarbonyl.
- 19. The method of claim 1, wherein P is t-butoxy carbonyl.
- 20. The method of claim 4, wherein P is t-butoxy carbonyl.
- 21. The method of claim 1, wherein R2 is phenyl-(CH2)m— or (C2-C9)heteroaryl-(CH2)m—, wherein each of said phenyl or (C2-C9)heteroaryl moieties may be optionally substituted with one, two, or three substituents independently selected from the group consisting of hydrogen, halogen, CN, (C1-C6)alkyl, or hydroxy.
- 22. The method of claim 4, wherein R2 is phenyl-(CH2)m— or (C2-C9)heteroaryl-(CH2)m—, wherein each of said phenyl or (C2-C9)heteroaryl moieties may be optionally substituted with one, two, or three substituents independently selected from the group consisting of hydrogen, halogen, CN, (C1-C6)alkyl, or hydroxy.
- 23. The method of claim 1, wherein R2 is 3-fluoro-benzyl.
- 24. The method of claim 4, wherein R2 is 3-fluoro-benzyl.
- 25. The method of claim 2, wherein R is a (C1-C6)alkyl, aryl, or (C2-C9)heteroaryl.
- 26. The method of claim 4, wherein R is a (C1-C6)alkyl, aryl, or (C2-C9)heteroaryl.
- 27. A compound of the formula (VIh-1)
- 28. A compound of the formula (VIIa-1)
- 29. The compound of claim 27, wherein P is carbobenzyloxy, t-butoxy carbonyl or 9-fluorenyl-methylenoxycarbonyl.
- 30. The compound of claim 28, wherein P is carbobenzyloxy, t-butoxy carbonyl or 9-fluorenyl-methylenoxycarbonyl.
- 31. The compound of claim 29, wherein P is t-butoxy carbonyl.
- 32. The compound of claim 30, wherein P is t-butoxy carbonyl.
- 33. The compound of claim 27, wherein R2 is phenyl-(CH2)m— or (C2-C9)heteroaryl-(CH2)m—, wherein each of said phenyl or (C2-C9)heteroaryl moieties may be optionally substituted with one, two, or three substituents independently selected from the group consisting of hydrogen, halogen, CN, (C1-C6)alkyl, or hydroxy.
- 34. The compound of claim 28, wherein R2 is phenyl-(CH2)m— or (C2-C9)heteroaryl-(CH2)m—, wherein each of said phenyl or (C2-C9)heteroaryl moieties may be optionally substituted with one, two, or three substituents independently selected from the group consisting of hydrogen, halogen, CN, (C1-C6)alkyl, or hydroxy.
- 35. The compound of claim 33, wherein R2 is 3-fluoro-benzyl.
- 36. The compound of claim 34, wherein R2 is 3-fluoro-benzyl.
PRIORITY CLAIM
[0001] The present application claims priority to U.S. Patent Application Serial No. 60/422,737, filed Oct. 31, 2002, which is incorporated herein in its entirety.
Provisional Applications (1)
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Number |
Date |
Country |
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60422737 |
Oct 2002 |
US |