Preparation of epothilone derivatives

Details Preparation of epothilone derivatives Preparation of epothilone derivatives

2007-07-03

2007-07-03

Saeed, Kamal A. (Department: 1626)

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

Organic compounds

Heterocyclic carbon compounds containing a hetero ring...

Reexamination Certificate

active

11400682

ABSTRACT:
The invention comprises a novel process for the preparation of an epothilone derivative of formula I:wherein R1and R2independently from each other represent hydrogen or protecting groups and R3is methyl or trifluoromethyl, which are useful precursors in the synthesis of the desoxyepothilone derivatives of the formula IV:wherein R3is methyl or trifluoromethyl.The desoxepothilones of formula IV inhibit the growth of tumor cells and are therefore promising candidates for novel anticancer agents.

REFERENCES:
patent: 2004/0053910 (2004-03-01), Danishefsky et al.
patent: WO 2004/018478 (2004-03-01), None
Danishefsky et al., J. Am. Chem. Soc., 125, pp. 2899-2901 (2003).
Nolan et al., Organometallics, 18, pp. 5416-5419 (1999).
Mol, J.C., Adv. Synth. Catal., 344, pp. 671-677 (2002).
Fuerstner, A. et al,J. Org. Chem., vol. 65:7, (2000) pp. 2204-2207 XP002395456.

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