An Efficient and Regioselective Synthesis of 2,3-Disubstituted 6-Aminoquinoxaline Derivatives Using Alkoxylation and Microwave-assisted Sonogashira Coupling

摘要

The quinoxalines are a common skeleton of nitrogen-containing heterocycles with biological properties.1 Because of their good biological activities quinoxalines, which contain 2,3-di-substituents, are of particular interest in medicinal chemistry and drug discovery programs.2 We screened diverse heterocyclic chemical compounds of in-house chemical libraries3 and identified biologically active 2,3,6-trisubstituted quinoxaline derivatives,4 containing 2,3-disub-stituted 6-aminoquinoxalines 1 (see Figure 1) that inhibited the Wnt/p-catenin signaling pathway and cell proliferation as anti-cancer agents.5 Herein, the synthetic routes of 2,3-disubstituted 6-aminoquinoxalines were developed with regioselective sequent substitutions for the further biological studies.