MUMBAI, India, Sept. 28 -- Intellectual Property India has published a patent application (202511022504 A) filed by National Institute Of Pharmaceutical Education And Research Niper on March 12, 2025, for Heterocyclic Derivatives Of Histidine, Histamine And De-Amino Histidine And Method For Synthesizing The Same Thereof.
Inventors include Rahul Jain; and Kamya Rao.
The application for the patent was published on September 25, 2026, under issue no. 39/2026.
Abstract: The present disclosure relates to a process for the synthesis of fused heterocyclic derivatives of histidine, histamine, and de-amino histidine via palladium-catalyzed intramolecular C–H (hetero)arylation. The method involves protected N1-(ortho-halobenzyl) imidazole-based amino acid substrates undergoing regioselective annulation at the C-5 position of the imidazole ring under microwave irradiation. The reaction is performed using tetrakis(triphenylphosphine)palladium(0) as a catalyst and potassium acetate as an oxidant in an organic solvent at 120–140 °C for 45 to 60 minutes, affording fused imidazoisoindole derivatives in 70–90% yield. The process is base-free, stereoconservative, and applicable to structurally diverse substrates including aryl and heteroaryl benzyl variants. The resulting compounds are purified using silica gel chromatography and characterized by NMR and mass spectrometry. The method is operationally simple, scalable, and offers significant advantages over conventional thermal processes in terms of efficiency, selectivity, and environmental compatibility. The products have potential applications in pharmaceuticals, peptide design, and medicinal chemistry.
Disclaimer: Curated by HT Syndication.
