Department of Chemistry, Purdue University, 560 Oval Drive, West Lafayette, Indiana 47907, USA.
Org Lett. 2012 Sep 21;14(18):4730-3. doi: 10.1021/ol301886g. Epub 2012 Sep 6.
An enantioselective and convergent total synthesis of pladienolide B (1) is described. Pladienolide B binds to the SF3b complex of a spliceosome and inhibits mRNA splicing activity. The synthesis features an epoxide opening reaction, an asymmetric reduction of a β-keto ester, and a cross metathesis strategy for the side chain synthesis.
本文描述了普乐地尔 B(1)的对映选择性和收敛性的全合成。普乐地尔 B 与剪接体的 SF3b 复合物结合并抑制 mRNA 剪接活性。该合成方法的特点是环氧化物开环反应、β-酮酯的不对称还原以及侧链合成的交叉复分解策略。