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Research Paper | Chemistry | Volume 15 Issue 8, August 2026 | Pages: 433 - 438 | India
Synthesis of Amidines Via Nucleophilic Addition of Amine to Nitrile
Abstract: Amidines are important classes of nitrogenous compounds, which have been widely used as antibiotics, diuretics, antiphlogistic drugs, anthelmintics, and acaricides. They represent an important pharmacophore in modern drug discovery. Many of the top-selling pharmaceuticals feature an amidine as a key structural component. They serve as key precursors in the preparation of many nitrogenous compounds of biological interest and play an essential role in the development of enzyme inhibitors, receptor ligands, and antimicrobial drugs. It can be found in DNA and RNA binding diamidine diminazene, Acid Sensing Ion Channel (ASIC) inhibitor, muscarinic agonists for the treatment of Alzheimer?s disease, platelet aggregation inhibitors. Many research efforts have been carried out worldwide to develop efficient and sustainable synthetic approaches for the preparation of amidines. Consequently, numerous methods involving Lewis acids, transition metal catalysts have been reported for the preparation of amidines via the direct nucleophilic addition of amine to nitrile. In this paper, we summarize the general methods for the synthesis of amidine from nitrile and amine. The emphasis has been given in the use of Lewis acids and transition metal catalysts, highlighting recent advances in green synthetic strategies. The synthesis of a few amidines by the direct nucleophilic addition of amines to nitriles using NaH as a reagent has been discussed.
Keywords: Benzonitrile, Aniline, Sodium hydride, Benzamidines, Lewis acid
How to Cite?: Pradip Debnath, "Synthesis of Amidines Via Nucleophilic Addition of Amine to Nitrile", Volume 15 Issue 8, August 2026, International Journal of Science and Research (IJSR), Pages: 433-438, https://www.ijsr.net/getabstract.php?paperid=SR26806081639, DOI: https://dx.doi.org/10.21275/SR26806081639