Centre for Nano and Material Sciences, Jain (Deemed-to-be University), Jain Global Campus, Bangalore, Karnataka, India.
Arch Pharm (Weinheim). 2023 Jun;356(6):e2300008. doi: 10.1002/ardp.202300008. Epub 2023 Mar 10.
The Biginelli reaction has received significant consideration in recent years due to its easily accessible aldehyde, urea/thiourea, and active methylene compounds. When it comes to pharmacological applications, the Biginelli reaction end-products, the 2-oxo-1,2,3,4-tetrahydropyrimidines, are vital in pharmacological applications. Due to the ease of carrying out the Biginelli reaction, it offers a number of exciting prospects in various fields. Catalysts, however, play an essential role in Biginelli's reaction. In the absence of a catalyst, it is difficult to form products with a good yield. Many catalysts have been used in search of efficientmethodologies, including biocatalysts, Brønsted/Lewis acids, heterogeneous catalysts, organocatalysts, and so on. Nanocatalysts are currently being applied in the Biginelli reaction to improve the environmental profile as well as speed up the reaction process. This review describes the catalytic role in the Biginelli reaction and pharmacological application of 2-oxo/thioxo-1,2,3,4-tetrahydropyrimidines. This study provides information that will facilitate the development of newer catalytic methods for the Biginelli reaction, by academics as well as industrialists. It also offers a broad scope for drug design strategies, which may enable the development of novel and highly effective bioactive molecules.
近年来,由于其易得的醛、脲/硫脲和活性亚甲基化合物,Biginelli 反应受到了广泛关注。在药理学应用方面,Biginelli 反应的终产物 2-氧代-1,2,3,4-四氢嘧啶在药理学应用中至关重要。由于易于进行 Biginelli 反应,它在各个领域提供了许多令人兴奋的前景。然而,催化剂在 Biginelli 反应中起着至关重要的作用。没有催化剂,很难形成具有良好收率的产物。人们一直在寻找高效的方法,包括使用生物催化剂、布朗斯台德/路易斯酸、多相催化剂、有机催化剂等,来寻找许多催化剂。纳米催化剂目前正应用于 Biginelli 反应中,以改善环境状况并加快反应进程。这篇综述描述了 2-氧代/硫代-1,2,3,4-四氢嘧啶在 Biginelli 反应中的催化作用和药理学应用。本研究为学术界和工业界开发新型 Biginelli 反应催化方法提供了信息,也为药物设计策略提供了广阔的空间,这可能会促进新型高效生物活性分子的开发。