Department of Chemistry, Pennsylvania State University, University Park, Pennsylvania 16802, United States.
J Am Chem Soc. 2011 Aug 17;133(32):12451-3. doi: 10.1021/ja206138d. Epub 2011 Jul 21.
A concise, diastereoselective total synthesis of (±)-cortistatin J has been completed in 20 steps from furan. Key steps include an intramolecular [4 + 3] cyclization of a disubstituted furan with a (Z)-2-(trialkylsilyloxy)-2-enal to construct the tetracyclic core and a (Z)-vinylsilane/iminium ion cyclization to form the A ring.
已完成从呋喃出发经 20 步反应、简洁、高非对映选择性的(±)-考替司他汀 J 的全合成。关键步骤包括:取代呋喃与(Z)-2-(三烷基硅氧基)-2-烯醛的分子内[4+3]环化反应,构建四环核心,以及(Z)-乙烯基硅烷/亚胺离子环化反应,构建 A 环。