Synthesis of Fluorescent, DNA-Binding Benzo[ b]indolonaphthyridinium Derivatives by a Misguided Westphal Condensation

J Org Chem. 2022 Mar 18;87(6):4010-4017. doi: 10.1021/acs.joc.1c02755. Epub 2022 Mar 3.

Abstract

A novel type of azoniahetarene, namely, benzo[b]indolonaphthyridinium, was unexpectedly formed by the reaction of N-alkylated β-carbolinium derivatives and the enolizable 1,2-cyclohexadione under typical conditions of a Westphal reaction. The products exhibit high fluorescence intensities in polar solvents (Φfl = 0.52-0.67) and bind to DNA by intercalation with high affinity (Kb = 1.5 × 106 M-1). Furthermore, under the same conditions, DNA-binding sempervirine derivatives were synthesized in a Westphal reaction from 1,2-diketones that have at least one non-enolizable α-carbon atom, which shows that the reaction pathway is determined by the substrate structure.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • DNA* / chemistry
  • Fluorescence

Substances

  • DNA