Department of Chemistry & Pharmaceutical Sciences, Amsterdam Institute for Molecules, Medicines & Systems (AIMMS) , Vrije Universiteit Amsterdam , De Boelelaan 1108 , 1081 HZ Amsterdam , The Netherlands.
Advanced Reactor Technology, Faculty of Applied Engineering , University of Antwerp , Groenenborgerlaan 171 , 2020 Antwerpen , Belgium.
J Org Chem. 2019 Sep 20;84(18):12058-12070. doi: 10.1021/acs.joc.9b01994. Epub 2019 Sep 10.
We report the intramolecular Tsuji-Trost reaction of Ugi adducts to give spiro-diketopiperazines in high yield and with high enantioselectivity. This approach allows the catalytic asymmetric construction of a broad range of these medicinally important heterocycles under mild conditions, in two steps from cheap, commercially available starting materials.
我们报告了 Ugi 加合物的分子内 Tsuji-Trost 反应，以高产率和高对映选择性得到螺二氢吡咯烷二酮。这种方法允许在温和条件下，从廉价、商业可得的起始原料出发，通过两步反应，催化不对称地构建广泛的这类具有重要药用价值的杂环化合物。
