دورية أكاديمية
Development of direct C-3 difluoromethylation reaction for application in synthesis of quinoline-related drugs
العنوان: | Development of direct C-3 difluoromethylation reaction for application in synthesis of quinoline-related drugs |
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المؤلفون: | Thanh Tung Truong, John Nielsen |
المصدر: | Vietnam Journal of Science, Technology and Engineering, Vol 66, Iss 1 (2024) |
بيانات النشر: | Vietnam Ministry of Science and Technology, 2024. |
سنة النشر: | 2024 |
المجموعة: | LCC:Science |
مصطلحات موضوعية: | C-H activation, difluoromethylation, drug synthesis, quinoline, Science |
الوصف: | Fluorine holds a prominent position within the realm of drug discovery and development, substantiated by its presence in approximately 25% of drugs approved by the US Food and Drug Administration (FDA). Consequently, the advancement of new fluorination reactions stands as a pivotal area in medicinal chemistry. In particular, the monofluoro-, difluoromethyl-, and trifluoromethyl- are three groups that appear most frequently in drug structure. Quinoline, owing to its privileged structural status, plays a crucial role in drug design and synthesis. Various approaches have been documented for the direct difluoromethylation of the C-2 and C-4 positions of the quinoline ring. However, achieving direct C-3 difluoromethylation has remained an elusive objective. In this study, we introduce a novel method for effecting the direct difluoromethylation at the C-3 position of the quinoline ring. Comprehensive characterizations, including 1H-NMR, 13C-NMR, and 19F-NMR for all compounds are performed. We believe that this novel method will open a new way to access the hitherto untapped C-3-difluoromethylation active compounds. |
نوع الوثيقة: | article |
وصف الملف: | electronic resource |
اللغة: | English |
تدمد: | 2525-2461 2615-9937 |
العلاقة: | https://vietnamscience.vjst.vn/index.php/vjste/article/view/1185Test; https://doaj.org/toc/2525-2461Test; https://doaj.org/toc/2615-9937Test |
DOI: | 10.31276/VJSTE.66(1).53-58 |
الوصول الحر: | https://doaj.org/article/823fa7f23be2469c82fd529b2594f8d0Test |
رقم الانضمام: | edsdoj.823fa7f23be2469c82fd529b2594f8d0 |
قاعدة البيانات: | Directory of Open Access Journals |
تدمد: | 25252461 26159937 |
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DOI: | 10.31276/VJSTE.66(1).53-58 |