Process for the preparation of epothilone derivatives, new...

Details Process for the preparation of epothilone derivatives, new... Process for the preparation of epothilone derivatives, new...

2003-09-12

2008-12-30

Shiao, Rei-tsang (Department: 1626)

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

Organic compounds

Heterocyclic carbon compounds containing a hetero ring...

C549S270000

Reexamination Certificate

active

07470792

ABSTRACT:
The present invention provides a synthesis for the preparation of epothilone derivatives of formula 9wherein R1 is methyl, and R2 is an unsubstituted or substituted aryl; an unsubstituted or substituted heteroaryl; or an unsubstituted or substituted heterocyclic radical fused to a benzene nucleus; and salts thereof, and intermediates for the synthesis of a compound of formula 9.

REFERENCES:
patent: WO 98/25929 (1998-06-01), None
patent: WO 99/54330 (1999-10-01), None
patent: WO 01/07439 (2001-02-01), None
patent: WO 02/30356 (2002-04-01), None
patent: WO 2004/012735 (2004-02-01), None
Nicolaou et al., “Total Synthesis of 16-Desmethylepothilone B, Epothilone B10, Epothilone F, and Related Side Chain Modified Epothilone B Analogues”,Chem Euro J, vol. 6, No. 15, pp. 2783-2800 (2000).
Höfle, Glaser, Leibold and Sefkow, “Epothilone A-D and Their Thiazole-Modified Analogs as Novel Anticancer Agents”,Pure Appl Chem, vol. 71, No. 11, pp. 2019-2024 (1999).

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