Claims
- 1. A process for the preparation of a taxane epoxide and its respective isomers which comprises reacting an oxidizing reagent with a compound of formula: ##STR9## in which R represents an acetyl group or H, R.sub.1 and R.sub.2 are an alkyl group such as Me, Et, Pr, i-Pr, n-Bu or t-Bu, R.sub.3 is H; R.sub.1 and R.sub.2 and R.sub.3 are H; R.sub.1 is an alkyl group such as Me, Et, Pr, i-Pr, n-Bu or t-Bu, R.sub.2 and R.sub.3 are H; R.sub.1 and R.sub.3 are H, R.sub.2 is an alkyl group such as Me, Et, Pr, i-Pr, n-Bu or t-Bu; R.sub.1 is H, R.sub.2 and R.sub.3 are an alkyl group such as Me, Et, Pr, i-Pr, n-Bu or t-Bu; R.sub.1 and R.sub.2 and R.sub.3 are an alkyl group Me, Et, Pr, i-Pr, n-Bu or t-Bu, in an organic solvent at a temperature for a period of time sufficient to produce a product of formula: ##STR10## in which R is Ac or H, and R.sub.1 and R.sub.2 are alkyl, R.sub.3 is H; R.sub.1 and R.sub.2 and R.sub.3 are H; R.sub.1 is alkyl, R.sub.2 and R.sub.3 are H; R.sub.1 and R.sub.3 are H, R.sub.2 is alkyl; R.sub.1 is H, R.sub.2 and R.sub.3 are alkyl; R.sub.1 and R.sub.2 and R.sub.3 are alkyl.
- 2. The process of claim 1, wherein R is Ac, R.sub.1 and R.sub.2 are Me, R.sub.3 is H.
- 3. The process of claim 1, wherein R is H, R.sub.1 and R.sub.2 are Me, R.sub.3 is H.
- 4. The process of claim 1, wherein said organic solvent is methylene chloride.
- 5. The process of claim 2, wherein oxidizing reagent is used at a reaction temperature of 0.degree.-50.degree. C.
- 6. The process of claim 5, wherein said oxidizing reagent is 3-chrolorperoxybenzoic acid.
- 7. The process of claim 6, wherein said period of time is about 12-24 hours.
- 8. The process of claim 5, wherein said oxidizing reagent is monoperoxyphethalic acid magnesium salt hexahydrate.
- 9. The process of claim 8, wherein said period of time is about 72 hours.
- 10. A compound having anticancer activity of formula: ##STR11## wherein R represents an acetyl group and R.sub.1 is an alkyl group (AC) or hydrogen (H); R.sub.2 is an alkyl group or hydrogen; and R.sub.3 is an alkyl group or hydrogen.
- 11. The compound of claim 10, wherein R.sub.1 and R.sub.2 and R.sub.3 are H.
- 12. The compound of claim 10, wherein R.sub.1 is Me, and R.sub.2 and R.sub.3 are H.
- 13. The compound of claim 10, wherein R.sub.1 and R.sub.3 are H, and R.sub.2 is Me.
- 14. The compound of claim 10, wherein R.sub.1 is H, and R.sub.2 and R.sub.3 are Me.
- 15. The compound of claim 10, wherein R.sub.1 and R.sub.2 and R.sub.3 are Me.
- 16. A compound having anticancer activity of formula: ##STR12## wherein R represents hydrogen and R.sub.1 is an alkyl group (Ac) or hydrogen (H); R.sub.2 is an alkyl group or hydrogen; and R.sub.3 is an alkyl group or hydrogen.
- 17. The compound of claim 16, wherein R.sub.1 and R.sub.2 and R.sub.3 are H.
- 18. The compound of claim 16, wherein R.sub.1 is Me, and R.sub.2 and R.sub.3 are H.
- 19. The compound of claim 16, wherein R.sub.1 and R.sub.3 are H, and R.sub.2 is Me.
- 20. The compound of claim 16, wherein R.sub.1 is H, and R.sub.2 and R.sub.3 are Me.
- 21. The compound of claim 16, wherein R.sub.1 and R.sub.2 and R.sub.3 are Me.
- 22. A compound having anticancer activity of formula: ##STR13##
- 23. A compound having anticancer activity of formula: ##STR14##
Parent Case Info
This application is a continuation-in-part of application Ser. No. 08/401,711, filed Mar. 10, 1995, now abandoned.
Non-Patent Literature Citations (2)
Entry |
"Status of the NCI Preclinical Antitumor Drug Discovery Screen," Michael R. Boyd, M.D., Ph.D., Principles & Practices of Oncology vol. 3, No. 10 (Oct. 1989). |
"Data Display and Analysis Strategies for the NCI Disease-Oriented In Vitro Antitumor Drug Screen," M.R. Boyd, K.D. Paull and L.R. Rubinstein, Proceedings of the Twenty-Second Annual Cancer Symposium, Detroit Michigan, USA--Apr. 26-28, 1990, pp.11-34. |
Continuation in Parts (1)
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Number |
Date |
Country |
Parent |
401711 |
Mar 1995 |
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