Diversity-Oriented Synthesis of Thiazolidine-2-imines via Microwave-Assisted One-Pot, Telescopic Approach and Its Interaction with Biomacromolecules
作者:Ananya Anubhav Saikia、Ramdas Nishanth Rao、Barnali Maiti、Musuvathi Motilal Balamurali、Kaushik Chanda
DOI:10.1021/acscombsci.0c00083
日期:2020.11.9
2-aminopyridine/pyrazine/pyrimidine with substituted isothiocyanates followed by base catalyzed ring closure with 1,2-dibromoethane to obtain thiazolidine-2-imines with broad substrate scope and high functional group tolerance. The synthetic strategy merges well with the thiourea formation followed by base catalyzed ring closure reaction for the thiazolidine-2-imine synthesis in a more modular and straightforward
在这项工作中,描述了一种用于 thiazolidine-2-亚胺组合库的单锅伸缩方法。通过2-氨基吡啶/吡嗪/嘧啶与取代的异硫氰酸酯反应,然后用1,2-二溴乙烷进行碱催化闭环,合成操作顺利进行,得到具有广泛底物范围和高官能团耐受性的噻唑烷-2-亚胺。合成策略与硫脲形成很好地结合,然后以更模块化和更直接的方法合成噻唑烷-2-亚胺的碱催化闭环反应。与传统方法相比,本文报道的合成程序代表了一种更清洁的 thiazolidine-2-亚胺路线。而且,