Hoffmann Judith, Gorges Jan, Junk Lukas, Kazmaier Uli
Institute of Organic Chemistry, Saarland University, P.O. Box 151150, 66041 Saarbrücken, Germany.
Org Biomol Chem. 2015 Jun 7;13(21):6010-20. doi: 10.1039/c5ob00587f.
The Ugi reaction is found to be a very powerful tool for the synthesis of (pre)tubulysin derivatives, allowing the introduction of various functionalized side chains in only one step. While polar groups such as amides are not well tolerated, unpolar side chains such as allyl or propargyl ether are well accepted. These functionalities also allow subsequent modifications in the side chain, e.g. via ring closing metathesis or Click reaction.
人们发现乌吉反应是合成（前）微管溶素衍生物的一种非常强大的工具，它能在一步反应中引入各种官能化侧链。虽然酰胺等极性基团不太容易被接受，但烯丙基或炔丙基醚等非极性侧链却很容易被接受。这些官能团还允许对侧链进行后续修饰，例如通过闭环复分解反应或点击反应。
