International Journal For Multidisciplinary Research

E-ISSN: 2582-2160   •   Impact Factor: 9.24

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Microwave promoted halogenation of quinines, heteroarenes,natural products and drugs using aqueous halogen donors and NCS.

Author(s) Prof. Dr. Balaji Digambar Kokane
Country India
Abstract Late-stage C–H chlorination and bromination of bioactive scaffolds is significant for drug discovery, as carbon–halogen bonds can effectively modulate biological activity, metabolic stability, and physicochemical profiles. Here, we develop an atom-economical, radical-mediated protocol that synthesizes high-value chlorinated or brominated quinones and (hetero)arenes. The system employs inexpensive, low-molecular-weight HCl or HBr as the halogen source, commercially available NCS in ionic liquid as ethyl ammonium nitrate, without any photocatalyst or metal catalyst. The mild reaction conditions, ready availability of reagents, excellent functional-group tolerance, high regioselectivity, and facile scalability under continuous-flow operation collectively render this approach a practical and efficient protocol for the late-stage aromatic C(sp²)–H chlorination and bromination of complex drugs and natural products. Mechanistic investigations reveal that nitrosyl halides, generated in situ by reaction of NCS and aqueous HCl or HBr, undergo homolysis to produce the corresponding halogen radicals that selectively initiate the radical halogenation of quinones and (hetero) arenes and natural products and drugs.
Keywords Ionic liquid, N-chlorosuccinsimide, aq.HCl/ HBr, Neproxen.
Field Chemistry
Published In Volume 8, Issue 1, January-February 2026
Published On 2026-01-23
DOI https://doi.org/10.36948/ijfmr.2026.v08i01.65837
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