Claims
- 1. A method for the preparation of a compound having the structure:
- 2. The method of claim 1, wherein the acylating step comprises the step of acylating the destryptophan compound with an acylating compound having the structure:
- 3. The method of claim 2, wherein the acylating compound comprises the following stereochemistry:
- 4. The method of claim 2, wherein the acylating compound comprises the following stereochemistry:
- 5. The method of claim 1, wherein the acylating step comprises the steps of acylating the destryptophan compound with a first acylating compound having the structure:
- 6. The method of claim 5, wherein the first acylating compound comprises the following stereochemistry:
- 7. The method of claim 5, wherein the first acylating compound comprises the following stereochemistry:
- 8. A method for the preparation of a compound having the structure:
- 9. The method of claim 1 or claim 8, wherein R1 is 7-methylnonyl, 9-methyldecyl, 9-methylundecyl, nonyl, or decyl.
- 10. The method of claim 9, wherein R1 is n-nonyl.
- 11. The method of claim 1 or claim 8, wherein R5 is allyloxycarbonyl, carbobenzyloxycarbonyl or tert-butoxycarbonyl.
- 12. The method of claim 11, wherein R5 is allyloxycarbonyl.
- 13. The method of claim 1 or claim 8, wherein R6 is trityl.
- 14. The method of claim 8, wherein the acylating step comprises acylating the desasparagine compound with an acylating compound having the structure:
- 15. The method of claim 14, wherein the acylating compound comprises the following stereochemistry:
- 16. The method of claim 14, wherein the acylating compound comprises the following stereochemistry:
- 17. The method of claim 14, wherein the acylating compound comprises the following stereochemistry:
- 18. The method of claim 14, wherein the acylating compound comprises the following stereochemistry:
- 19. The method of claim 14, wherein the acylating compound comprises greater than about 50% of one diastereomer.
- 20. The method of claim 14, wherein the acylating compound comprises greater than about 75% of one diastereomer.
- 21. The method of claim 14, wherein the acylating compound comprises greater than about 90% of one diastereomer.
- 22. The method of claim 14, wherein the acylating compound comprises greater than about 95% of one diastereomer.
- 23. The method of claim 14, wherein the acylating compound comprises greater than about 98% of one diastereomer.
- 24. The method of claim 8, wherein the acylating step comprises the steps of: acylating the desasparagine compound with a first acylating compound having the structure:
- 25. The method of claim 8, wherein the acylating step comprises the steps of: acylating the desasparagine compound with a first acylating compound having the structure:
- 26. The method of claim 24 or claim 25, wherein the first acylating compound comprises the following stereochemistry:
- 27. The method of claim 24 or claim 25, wherein the first acylating compound comprises the following stereochemistry:
- 28. The method of claim 24 or claim 25, wherein the first acylating compound comprises greater than about 50% of one enantiomer.
- 29. The method of claim 24 or claim 25, wherein the first acylating compound comprises greater than about 75% of one enantiomer.
- 30. The method of claim 24 or claim 25, wherein the first acylating compound comprises greater than about 90% of one enantiomer.
- 31. The method of claim 24 or claim 25, wherein the first acylating compound comprises greater than about 95% of one enantiomer.
- 32. The method of claim 24 or claim 25, wherein the first acylating compound comprises greater than about 98% of one enantiomer.
- 33. The method of claim 24, wherein the second acylating compound comprises the following stereochemistry:
- 34. The method of claim 24, wherein the second acylating compound comprises the following stereochemistry:
- 35. The method of claim 25, wherein the second acylating compound comprises the following stereochemistry:
- 36. The method of claim 25, wherein the second acylating compound comprises the following stereochemistry:
- 37. The method of claim 24 or claim 25, wherein the second acylating compound comprises greater than about 50% of one enantiomer.
- 38. The method of claim 24 or claim 25, wherein the second acylating compound comprises greater than about 75% of one enantiomer.
- 39. The method of claim 24 or claim 25, wherein the second acylating compound comprises greater than about 90% of one enantiomer.
- 40. The method of claim 24 or claim 25, wherein the second acylating compound comprises greater than about 95% of one enantiomer.
- 41. The method of claim 24 or claim 25, wherein the second acylating compound comprises greater than about 98% of one enantiomer.
- 42. The method of claim 8, further comprising the step of removing an asparagine residue from a destryptophan compound having the structure:
- 43. The method of claim 1 or claim 42, further comprising the step of removing a tryptophan residue from a deacylated compound having the structure:
- 44. The method of claim 43, further comprising the step of deacylating an ornithine protected compound having the structure:
- 45. The method of claim 44, further comprising the step of protecting the ornithine amine group of a compound having the structure:
- 46. A composition comprising a compound having the following structure:
- 47. The composition of claim 46, further comprising one or more compounds having the following structure:
- 48. A composition comprising a compound having the following structure:
- 49. The composition of claim 48, further comprising one or more compounds having the following structure:
- 50. A composition comprising a compound having the following structure:
- 51. The composition of claim 50, further comprising one or more compounds having the following structure:
- 52. The composition of any one of claims 46, 47, 48, 49, 50, or 51, wherein R1 is 7-methylnonyl, 9-methyldecyl, 9-methylundecyl, nonyl, or decyl.
- 53. The composition of claim 52, wherein R1 is n-nonyl.
- 54. A composition comprising a compound having the following structure:
- 55. A composition comprising a compound having the following structure:
- 56. A composition comprising a compound having the following structure:
- 57. A composition comprising a compound having the following structure:
- 58. The composition of claim 57, wherein the compound comprises the following stereochemistry:
- 59. The composition of claim 57, wherein the compound comprises the following stereochemistry:
- 60. A composition comprising a compound having the following structure:
- 61. The composition of any one of claims 54, 55, 56, 57, 58, 59, or 60, wherein R5 is allyloxycarbonyl, carbobenzyloxycarbonyl or tert-butoxycarbonyl.
- 62. The composition of claim 61, wherein R5 is allyloxycarbonyl.
CROSS-REFERENCE TO RELATED APPLICATIONS
[0001] This application claims the benefit of U.S. Provisional Application No. 60/310,313, filed Aug. 6, 2001, which is hereby incorporated by reference in its entirety.
Provisional Applications (1)
|
Number |
Date |
Country |
|
60310313 |
Aug 2001 |
US |