Practical and Scalable Synthetic Method for Preparation of Dolutegravir Sodium: Improvement of a Synthetic Route for Large-Scale Synthesis
| Autor: | Shoji Shinomoto, Yutaka Nishino, Naoki Miyake, Yuki Fukui, Masahiko Nagai, Tatsuro Yasukata, Takao Ooyama, Toshikazu Hakogi, Yasunori Aoyama, Yoshiyuki Taoda, Daisuke Yamada, Hiroshi Yoshida |
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| Rok vydání: | 2019 |
| Předmět: |
Materials science
Scale (ratio) 010405 organic chemistry Organic Chemistry Maltol Dolutegravir sodium 010402 general chemistry 01 natural sciences Combinatorial chemistry 0104 chemical sciences chemistry.chemical_compound chemistry Amide Scalability Moiety Oxidation process Physical and Theoretical Chemistry |
| Zdroj: | Organic Process Research & Development. 23:558-564 |
| ISSN: | 1520-586X 1083-6160 |
| Popis: | A practical and scalable synthetic method to obtain dolutegravir sodium (1) was established starting from the readily accessible material maltol (2). This synthetic method includes a scalable oxidation process of maltol and palladium-catalyzed amidation for introduction of an amide moiety, leading to a practical manufacturing method in short synthetic steps. The synthetic method demonstrated herein enables multikilogram scale manufacturing of 1 of high purity. |
| Databáze: | OpenAIRE |
| Externí odkaz: |
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