Institute of Chemistry, University of Campinas , 13083-970, C.P. 6154, Campinas, SP, Brasil.
Org Lett. 2015 Dec 18;17(24):6278-81. doi: 10.1021/acs.orglett.5b03352. Epub 2015 Dec 9.
The first total synthesis of (-)-marinisporolide C was performed in 25 steps (longest linear sequence) and an overall yield of 1%. Due to the high degree of convergence and robustness, the C9-C35 fragment that corresponds to the polyol portion was obtained in gram quantity. Highlights of this synthesis include five highly stereoselective aldol reactions responsible for the construction of five C-C bonds and six stereogenic centers. Additionally, a very efficient Julia-Kocieński reaction was used to install a C22-C23 double bond, and the macrocyclic ring was closed using an intramolecular Horner-Wadsworth-Emmons olefination.
(-)-海兔内酯 C 的首次全合成是通过 25 步(最长线性序列)完成的,总收率为 1%。由于高度收敛和稳健性,对应多元醇部分的 C9-C35 片段以克级规模获得。该合成的亮点包括五个高度立体选择性的醛醇反应,负责构建五个 C-C 键和六个手性中心。此外,还使用了非常有效的 Julia-Kocieński 反应来安装 C22-C23 双键,并通过分子内 Horner-Wadsworth-Emmons 烯烃化反应来闭合大环环。