期刊
ORGANIC LETTERS
卷 9, 期 8, 页码 1605-1607出版社
AMER CHEMICAL SOC
DOI: 10.1021/ol070415q
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资金
- NCI NIH HHS [CA78039] Funding Source: Medline
[GRAPHICS] The N-14-desacetoxy analogue of tubulysin H was prepared in 20 steps and 2.1% overall yield. Our strategy features a thiazole anion addition to assemble the tubuvaline residue at the C(10)-C(11) bond, as well as acylations at N-5, N-14, and N-17. This iterative coupling approach, as well as the removal of the labile N,O-acetal at N-14, enables the synthesis of analogues for detailed studies of structure-activity relationships in this family of potent tubulin disrupters.
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