Institute of Drug Discovery and Design, College of Pharmaceutical Sciences, Zhejiang University, 866 Yuhangtang Road, Hangzhou, 310058, Zhejiang, China.
Angew Chem Int Ed Engl. 2017 Apr 10;56(16):4565-4568. doi: 10.1002/anie.201700840. Epub 2017 Mar 22.
Multicomponent reactions are excellent tools for rapid generation of small molecules with broad chemical diversity and molecular complexity. Herein, a novel one-pot multicomponent synthesis of β-amino amides from aldehydes, anilines, carboxylic acids and ynamides has been successfully developed. This process is practical and efficient to unravel synthetic utility and scalability. Moreover, an isotope labeling reaction was conducted to elucidate a plausible reaction mechanism.
多组分反应是快速生成具有广泛化学多样性和分子复杂性的小分子的极好工具。本文成功开发了一种从醛、苯胺、羧酸和炔酰胺一锅法合成β-氨基酰胺的新方法。该过程具有实用和高效的特点,可以揭示其合成实用性和可扩展性。此外,还进行了同位素标记反应以阐明合理的反应机理。