Catalytic Asymmetric Synthesis of Diketopiperazines by Intramolecular Tsuji-Trost Allylation

J Org Chem. 2019 Sep 20;84(18):12058-12070. doi: 10.1021/acs.joc.9b01994. Epub 2019 Sep 10.

Abstract

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.

Publication types

  • Research Support, Non-U.S. Gov't