C–H Acylation as an Enabling Tool to Tag Phenolic Drugs
The site-selective functionalization of value-added compounds while implementing atom-economical C–H coupling partners represents an unmet challenge of utmost importance within organic synthesis. Herein, we report a Pd-catalyzed directed C–H acylation of a collection of relevant phenol-containing co...
| Autores: | , |
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| Tipo de recurso: | artículo |
| Fecha de publicación: | 2024 |
| País: | España |
| Institución: | Universidad del País Vasco |
| Repositorio: | Addi. Archivo Digital para la Docencia y la Investigación |
| OAI Identifier: | oai:addi.ehu.eus:10810/72266 |
| Acceso en línea: | http://hdl.handle.net/10810/72266 |
| Access Level: | acceso abierto |
| Palabra clave: | drugs acylation palladium catalysis |
| Sumario: | The site-selective functionalization of value-added compounds while implementing atom-economical C–H coupling partners represents an unmet challenge of utmost importance within organic synthesis. Herein, we report a Pd-catalyzed directed C–H acylation of a collection of relevant phenol-containing compounds with ethanol and other alcohols and aldehydes. This tagging technique is distinguished by itswater compatibility and predictable regioselectivity and features the use of ethanol as renewable feed- stock for the modification of intricate phenols, including estrogens and other top-selling pharmaceuticals. Mechanistic studies support the intermediacy of a challenging 6-membered dimeric palladacycle that undergoes the addition of nucleophilic acyl radical species |
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