Synthesis of multi-functionalized benzofurans through the condensation of ninhydrin and phenols using SSA as a recyclable heterogeneous acid catalyst
A simple and efficient one-pot methodology has been developed for the synthesis of biologically important multi-functionalized 3-(2$$^{\prime }$$′-hydroxyaryl)-2-(2$$^{\prime }$$′-carboxyphenyl)benzofurans using silica sulfuric acid (SSA) as a heterogeneous acid catalyst in DMF medium. The significant advantages of this methodology are the use of SSA as a recyclable solid acid catalyst, operational simplicity, easy availability of the starting materials, and good yield of the products with high atom-economy.
One-pot synthesis of 2,3-disubstituted benzofurans from 2-chlorophenols using palladium–dihydroxyterphenylphosphine catalyst
Abstract 2,3-Disubstituted benzofurans possessing 2-hydroxyphenyl moiety at the C-3 position were synthesized from readily available 2-chlorophenols and terminal alkynes by hydroxy-directed ortho-Sonogashira coupling and subsequent oxypalladation/reductive elimination, using Pd-dihydroxyterphenylphosphine catalyst. The catalyst accelerates not only the Sonogashira coupling but also the introduction of 2-hydroxyphenyl group at the C-3 position of benzofuran.
Aminoalkoxybiphenylnitriles as histamine-3 receptor ligands.
Biaryl nitrile amines were prepared and found to have high affinity and selectivity for human and rat histamine H(3) receptors.