Formal Synthesis of Fostriecin via Asymmetric Alcohol-Mediated Carbonyl Allylation

通过不对称醇介导的羰基烯丙基化反应正式合成福斯特里辛

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Abstract

A formal synthesis of fostriecin via convergent assembly of two fragments prepared via asymmetric alcohol-mediated C-C coupling is described. One fragment is made by the enantioselective iridium-catalyzed allylation of an allylic alcohol mediated by allyl acetate. The other fragment is made via enantioselective ruthenium-catalyzed reductive syn-(α-alkoxy)allylation of an aldehyde mediated by an alkoxyallene (where 2-propanol is the hydrogen source), representing the first use of this method in target-oriented synthesis. Metathetic fragment union enables interception of a late-stage compound that previously required a 25 step (LLS) synthesis in only 7 steps (LLS).

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