The First Kilogram Synthesis of Beclabuvir, an HCV NS5B Polymerase Inhibitor
| العنوان: | The First Kilogram Synthesis of Beclabuvir, an HCV NS5B Polymerase Inhibitor |
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| المؤلفون: | Michelle Soltani, Zhinong Gao, Hu Wenhao, Adam Littke, Anthony Tedesco, Albert J. DelMonte, Akin H. Davulcu, Dale Vanyo, Kishta Katipally, Yuping Qiu, Jeffrey T. Bien, Purushotham Vemishetti, Richard L. Schild, Maria Sandoval, Aghogho Pedro, Yi Hsiao, Kenneth J. Fraunhoffer, Robert E. Waltermire, Chao Hang |
| المصدر: | Organic Process Research & Development. 22:1393-1408 |
| بيانات النشر: | American Chemical Society (ACS), 2018. |
| سنة النشر: | 2018 |
| مصطلحات موضوعية: | Indole test, 010405 organic chemistry, Cyclopropanation, Chemistry, Stereochemistry, Organic Chemistry, Enantioselective synthesis, Convergent synthesis, Alkylation, 010402 general chemistry, Ring (chemistry), 01 natural sciences, 0104 chemical sciences, Cyclopropane, chemistry.chemical_compound, Intramolecular force, Physical and Theoretical Chemistry |
| الوصف: | The process development and kilogram-scale synthesis of beclabuvir (BMS-791325, 1) is described. The convergent synthesis features the use of asymmetric catalysis to generate a chiral cyclopropane fragment and coupling with an indole fragment via an alkylation. Subsequent palladium-catalyzed intramolecular direct arylation efficiently builds the central seven-membered ring. The target was prepared in 12 linear steps with five isolations in an overall yield of 8%. |
| تدمد: | 1520-586X 1083-6160 |
| URL الوصول: | https://explore.openaire.eu/search/publication?articleId=doi_________::bde849fdcd900b6feab0d0d189aa4666 https://doi.org/10.1021/acs.oprd.8b00214 |
| رقم الأكسشن: | edsair.doi...........bde849fdcd900b6feab0d0d189aa4666 |
| قاعدة البيانات: | OpenAIRE |
Find this issue from the American Chemical Society | تدمد: | 1520586X 10836160 |
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