Fonte Mélanie, Teixeira Cátia, Gomes Paula
LAQV-REQUIMTE, Departamento de Química e Bioquímica, Faculdade de Ciências Universidade do Porto Portugal
RSC Adv. 2024 Feb 19;14(9):6253-6261. doi: 10.1039/d4ra00091a. eCollection 2024 Feb 14.
Acridines are one of the most important nitrogen-containing heterocycle systems and have many applications in the therapeutic field. However, the synthesis of acridine-based scaffolds is not always straightforward. Herein, we report the optimization of two multi-step synthetic routes towards 4,9-diaminoacridines and 4-aminoacridines, which have shown promising antiplasmodial properties. The improved synthesis pathways make use of greener, simpler, and more efficient methods, with less reaction steps and increased overall yields, which were doubled in some cases. These are impactful results towards future approaches to the chemical synthesis of acridine-based compounds.
吖啶是最重要的含氮杂环体系之一，在治疗领域有许多应用。然而，基于吖啶的支架的合成并不总是简单直接的。在此，我们报告了两种多步合成路线的优化，用于合成具有良好抗疟原虫特性的4,9-二氨基吖啶和4-氨基吖啶。改进后的合成途径采用了更绿色、更简单、更高效的方法，反应步骤更少，总产率提高，在某些情况下甚至翻倍。这些结果对于基于吖啶的化合物的化学合成的未来方法具有重要意义。
