Function-Oriented Synthesis toward Peloruside A Analogues

Organic Letters(2019)

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摘要
A convergent and rapid synthesis of original C2,C3-unsaturated, C11,C13-keto–enol macrocycles with a peloruside A skeleton has been developed. These original unsaturated macrocycles constitute valuable platforms to access peloruside A analogues with high diversity. The four-fragment strategy implemented features two aldol-type couplings with the central C12–C14 building block TES-diazoacetone and a late-stage ring-closing metathesis. Enantiopure analogue 18ab showed antiproliferative activity in the low micromolar range on NCI and MCF7 tumor cell lines.
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关键词
synthesis,analogues,function-oriented
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