PDF(Pubmed)
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.
摘要：
阿替洛尔,目前世界上最畅销的五大治疗心绞痛和高血压的药物之一,为了降低心脏病发作后的死亡风险，在当前的合成方法中面临挑战，以解决低效率和环境问题。这种药物的传统合成涉及产生大量废物和其他需要处理的副产品的过程。这项研究提出了一种基于一罐DES的可持续方案，用于合成阿替洛尔。使用DES可以在不需要额外的碱或催化剂的情况下进行整个过程。在短的反应时间内，在温和的条件下,避免色谱纯化。阿替洛尔的总收率为95%。成功证明了该工艺到克级生产的可扩展性，强调其在工业应用中的潜力。最后,“绿色”评价，使用FirstPassCHEM21MetricsToolkit执行，强调了原子经济方面的优势，反应质量效率，与现有方法相比，基于DES的合成的整体过程质量强度。
