Pinwen Cai; Guanyu Yang; Lanzhou Zhao; Jinqiao Wan; Jin Li; Guansai Liu
Org. Lett., 2019, 21, 17, 6633-6637
https://doi.org/10.1021/acs.orglett.9b02132

Abstract

3-Alkylated indole cores have been found in countless natural products and many biologically active compounds, including pharmaceuticals. In this report, a highly efficient approach to C3-alkylated indole derivatives on DNA via indolyl alcohol formation followed by metal-free transfer hydrogenation is developed. This on-DNA C3 alkylation approach is attractive because library compounds can be constructed from simple aldehydes or acid functionalized aldehydes, which are widely commercially available.