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Sustainable Synthesis of the Active Pharmaceutical Ingredient Atenolol in Deep Eutectic Solvents.
Procopio, Debora; Siciliano, Carlo; Perri, Assunta; Guillena, Gabriela; Ramón, Diego J; Di Gioia, Maria Luisa.
Afiliación
  • Procopio D; Department of Pharmacy, Health and Nutritional Sciences, University of Calabria, 87036 Rende, Italy.
  • Siciliano C; Department of Pharmacy, Health and Nutritional Sciences, University of Calabria, 87036 Rende, Italy.
  • Perri A; Department of Pharmacy, Health and Nutritional Sciences, University of Calabria, 87036 Rende, Italy.
  • Guillena G; Department of Organic Chemistry, Institute of Organic Synthesis (ISO), University of Alicante, 03080 Alicante, Spain.
  • Ramón DJ; Department of Organic Chemistry, Institute of Organic Synthesis (ISO), University of Alicante, 03080 Alicante, Spain.
  • Di Gioia ML; Department of Pharmacy, Health and Nutritional Sciences, University of Calabria, 87036 Rende, Italy.
Int J Mol Sci ; 25(12)2024 Jun 18.
Article en En | MEDLINE | ID: mdl-38928384
ABSTRACT
Atenolol, one of the top five best-selling drugs in the world today used to treat angina and hypertension, and to reduce the risk of death after a heart attack, faces challenges in current synthetic methods to address inefficiencies and environmental concerns. The traditional synthesis of this drug involves a process that generates a large amount of waste and other by-products that need disposal. This study presents a one-pot DES-based sustainable protocol for synthesizing atenolol. The use of the DES allowed the entire process to be conducted with no need for additional bases or catalysts, in short reaction times, under mild conditions, and avoiding chromatographic purification. The overall yield of atenolol was 95%. The scalability of the process to gram-scale production was successfully demonstrated, emphasizing its potential in industrial applications. Finally, the 'greenness' evaluation, performed using the First Pass CHEM21 Metrics Toolkit, highlighted the superiority in terms of the atom economy, the reaction mass efficiency, and the overall process mass intensity of the DES-based synthesis compared with the already existing methods.
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Texto completo: 1 Colección: 01-internacional Base de datos: MEDLINE Asunto principal: Atenolol / Disolventes Eutécticos Profundos Idioma: En Revista: Int J Mol Sci Año: 2024 Tipo del documento: Article País de afiliación: Italia Pais de publicación: Suiza

Texto completo: 1 Colección: 01-internacional Base de datos: MEDLINE Asunto principal: Atenolol / Disolventes Eutécticos Profundos Idioma: En Revista: Int J Mol Sci Año: 2024 Tipo del documento: Article País de afiliación: Italia Pais de publicación: Suiza