AN EXPEDITIOUS METHOD FOR THE SYNTHESIS OF N-NITROSO N -DESMETHYL NINTEDANIB

  • Unique Paper ID: 187835
  • PageNo: 7188-7197
  • Abstract:
  • Impurities of N-Nitrosoamines have become a major problem for the pharmaceutical sector. These contaminants can inadvertently occur in bulk active pharmaceutical ingredients (APIs), presenting significant health concerns and regulatory issues, even though they are necessary to synthesize in controlled laboratory environments. There are many adverse effects of nitrosamines, carcinogenic qualities are prime. When it comes to anticancer medications, carcinogenicity become most dangerous. N-Nitroso N-Desmethyl Nintedanib is a significant worry as a strong nitrosoamine carcinogenic impurity that poses additional hazards in its therapeutic usage. Nintedanib is an API used to treat pulmonary fibrosis and some types of cancer. Because of its substantial mass, this molecule is difficult for synthesis in the lab, making direct nitrosation or demethylation hard. In this work, we used a variety of intermediates and bulk API to synthesize N-Nitroso N-Desmethyl Nintedanib. Synthesis using Boc-protected piperazine substitution proved the least time-consuming and most effective method out of all those attempted.

Copyright & License

Copyright © 2026 Authors retain the copyright of this article. This article is an open access article distributed under the Creative Commons Attribution License which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited.

BibTeX

@article{187835,
        author = {Snehal R Thakar and Nitin S Bondre and Bapu A Gawade and Anil B Gawade},
        title = {AN EXPEDITIOUS METHOD FOR THE SYNTHESIS OF N-NITROSO N -DESMETHYL NINTEDANIB},
        journal = {International Journal of Innovative Research in Technology},
        year = {2025},
        volume = {12},
        number = {6},
        pages = {7188-7197},
        issn = {2349-6002},
        url = {https://ijirt.org/article?manuscript=187835},
        abstract = {Impurities of N-Nitrosoamines have become a major problem for the pharmaceutical sector. These contaminants can inadvertently occur in bulk active pharmaceutical ingredients (APIs), presenting significant health concerns and regulatory issues, even though they are necessary to synthesize in controlled laboratory environments. There are many adverse effects of nitrosamines, carcinogenic qualities are prime. When it comes to anticancer medications, carcinogenicity become most dangerous. N-Nitroso N-Desmethyl Nintedanib is a significant worry as a strong nitrosoamine carcinogenic impurity that poses additional hazards in its therapeutic usage. Nintedanib is an API used to treat pulmonary fibrosis and some types of cancer.  Because of its substantial mass, this molecule is difficult for synthesis in the lab, making direct nitrosation or demethylation hard. In this work, we used a variety of intermediates and bulk API to synthesize N-Nitroso N-Desmethyl Nintedanib. Synthesis using Boc-protected piperazine substitution proved the least time-consuming and most effective method out of all those attempted.},
        keywords = {Nintedanib, N-Nitroso N -Desmethyl Nintedanib, anticancer, pharmaceutical impurities, Nitroso, TBN etc.},
        month = {November},
        }

Cite This Article

Thakar, S. R., & Bondre, N. S., & Gawade, B. A., & Gawade, A. B. (2025). AN EXPEDITIOUS METHOD FOR THE SYNTHESIS OF N-NITROSO N -DESMETHYL NINTEDANIB. International Journal of Innovative Research in Technology (IJIRT), 12(6), 7188–7197.

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