دورية أكاديمية
Microwave-Assisted Synthesis of a MK2 Inhibitor by Suzuki-Miyaura Coupling for Study in Werner Syndrome Cells
| العنوان: | Microwave-Assisted Synthesis of a MK2 Inhibitor by Suzuki-Miyaura Coupling for Study in Werner Syndrome Cells |
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| المؤلفون: | Mark C. Bagley, Mohammed Baashen, Irina Chuckowree, Jessica E. Dwyer, David Kipling, Terence Davis |
| المصدر: | Pharmaceuticals, Vol 8, Iss 2, Pp 257-276 (2015) |
| بيانات النشر: | MDPI AG, 2015. |
| سنة النشر: | 2015 |
| المجموعة: | LCC:Medicine LCC:Pharmacy and materia medica |
| مصطلحات موضوعية: | Suzuki-Miyaura, cross-coupling, MK2 inhibitor, Werner syndrome, cell aging, pyrazoles, heterocycles, microwave-assisted synthesis, boronic acid, Medicine, Pharmacy and materia medica, RS1-441 |
| الوصف: | Microwave-assisted Suzuki-Miyaura cross-coupling reactions have been employed towards the synthesis of three different MAPKAPK2 (MK2) inhibitors to study accelerated aging in Werner syndrome (WS) cells, including the cross-coupling of a 2-chloroquinoline with a 3-pyridinylboronic acid, the coupling of an aryl bromide with an indolylboronic acid and the reaction of a 3-amino-4-bromopyrazole with 4-carbamoylphenylboronic acid. In all of these processes, the Suzuki-Miyaura reaction was fast and relatively efficient using a palladium catalyst under microwave irradiation. The process was incorporated into a rapid 3-step microwave-assisted method for the synthesis of a MK2 inhibitor involving 3-aminopyrazole formation, pyrazole C-4 bromination using N-bromosuccinimide (NBS), and Suzuki-Miyaura cross-coupling of the pyrazolyl bromide with 4-carbamoylphenylboronic acid to give the target 4-arylpyrazole in 35% overall yield, suitable for study in WS cells. |
| نوع الوثيقة: | article |
| وصف الملف: | electronic resource |
| اللغة: | English |
| تدمد: | 1424-8247 |
| Relation: | http://www.mdpi.com/1424-8247/8/2/257; https://doaj.org/toc/1424-8247 |
| DOI: | 10.3390/ph8020257 |
| URL الوصول: | https://doaj.org/article/8ba2c9fd6e5a45848730ec8b6ddd4744 |
| رقم الأكسشن: | edsdoj.8ba2c9fd6e5a45848730ec8b6ddd4744 |
| قاعدة البيانات: | Directory of Open Access Journals |
Full Text Finder | تدمد: | 14248247 |
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| DOI: | 10.3390/ph8020257 |