Catalyst-Free N-Arylation Using Unactivated Fluorobenzenes

摘要

N-arylation of heteroaromatic compounds is an extremely important C—N bond-forming reaction in organic synthesis, especially with N-arylated azole and indole derivatives finding important uses (Scheme 1) as inhibitors of enzymes (e.g. COX-1,COX-2,PDE3,PDE5,topoisomera-se II), inhibitors of ATP binding. agonists or antagonists of G protein-coupled and other receptors (e.g. DA D-2, 5-HT2, α1AR,CB1, Sigma σ2, GABA_A), modulators of ion-channels, as key components in LED production, and for creating organometallic catalysts. N-arylated azole and indole derivatives are also registered pharmaceuticals (e.g. celecoxib, midazolam, flumazenil, nilotinib, edar-avone, alprazolam, sertindole; Figure 1) and insecticides or fungicides (e.g. pyraclofos, pyraclostrobin).