| 摘要 |
A method for making epothilones and epothilone analogs is described, as are novel compounds made by the method. Exemplary novel compounds include those according to the formula: With respect the formula, G is selected from the group consisting of R<SUB>2 </SUB>substituents independently are selected from the group consisting of H and lower alkyl groups; Z is selected from the group consisting of the halogens and -CN; M is selected from the group consisting of O and NR<SUB>3</SUB>; R<SUB>3 </SUB>is selected from the group consisting of H, lower alkyl, R<SUB>4</SUB>CO, R<SUB>4</SUB>OCO, and R<SUB>4</SUB>SO<SUB>2</SUB>; R<SUB>4 </SUB>is selected from the group consisting of H, lower alkyl, and aryl; T is selected from the group consisting of CH<SUB>2</SUB>, CO, HCOH and protected derivatives thereof; W is H or OR; and X and Y independently are selected from the group consisting of O, NH, S, CO, and C. Embodiments of the method provide convenient access to analogs of the epothilones, such as those having alternate stereochemistry and those containing an ester, amide, thioester, or alkyne moieties in the macrocycle.
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