دورية
Process Development of Bersacapavir, Part 1: Route Scouting Effort toward a Key Amide Intermediate
| العنوان: | Process Development of Bersacapavir, Part 1: Route Scouting Effort toward a Key Amide Intermediate |
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| المؤلفون: | Medina, Florian, Maton, William M., Weerts, Johan, Eriksson, Magnus, Bongartz, Jean-Pierre, Clemens, Kurt, Kossler, David, Peeters, Micha, Wegsteen, Koen, Maes, Tor, Keppens, Els |
| المصدر: | Organic Process Research & Development; 20240101, Issue: Preprints |
| مستخلص: | In this article, the route scouting effort toward a key secondary amide intermediate in the synthesis of bersacapavir is described. This study relies on the haloform reaction and the reactivity of trichloromethylketone. First, a more classical synthesis route was developed, based on the preparation of a carboxylic acid from the corresponding trichloromethylketone (conventional haloform reaction). The second, and preferred, approach utilized an innovative extension of the haloform reaction, allowing direct coupling between electron-poor aniline and trichloromethylketone. The desired amide intermediate was obtained in high yield and purity via a simple two-step synthesis using cheap and readily available starting materials. |
| قاعدة البيانات: | Supplemental Index |
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