Cephalomannine epoxide, its analogues and a method for preparing

Details Cephalomannine epoxide, its analogues and a method for preparing Cephalomannine epoxide, its analogues and a method for preparing

1997-05-21

1999-04-06

Trinh, Ba K.

Organic compounds -- part of the class 532-570 series

Organic compounds

Heterocyclic carbon compounds containing a hetero ring...

549511, C07D30514

Patent

active

058920633

ABSTRACT:
An antitumor compound of formula (5) ##STR1## in which R is Ac or H, and R.sub.1, R.sub.2 is 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, R.sub.3 is 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. Me is an abbreviation for methyl, Et is ethyl, Pr is propyl, i-Pr is isopropyl, n-Bu is n-butyl, and t-Bu is tert-butyl. Also provided by the invention is a one step method of preparing a compound of formula (5) whereby a taxane having a tiglate group attached to the side chain is contacted with an oxidizing reagent resulting in the formation of an epoxide having antitumor activity.

REFERENCES:
"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.

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