CIQUP/Department of Chemistry and Biochemistry, Faculty of Sciences, University of Porto, Rua do Campo Alegre, 4169-007 Porto, Portugal.
Molecules. 2019 Nov 20;24(23):4214. doi: 10.3390/molecules24234214.
6-Bromochromone-2-carboxylic acid () was synthesized by a microwave-assisted process. The optimization of the reaction was performed varying parameters, such as type of base/number of reagent equivalents, solvent, temperature and reaction time. The yield of the reaction was improved to 87%. The new synthetic route is versatile as several chromone-2-carboxylic acids (compounds -) were obtained with good yields (54-93%). Only in the case of the nitro substituent (compound ), an ester was obtained instead of the desired carboxylic acid. Following this synthetic route chromone carboxylic acids can be attained with a high degree of purity, without the need of the tedious and expensive purification processes through column chromatography. The reaction is safe, cost-effective, fast and robust, and can be used in the development of concise and diversity-oriented libraries based on chromone scaffold. The overall study can be looked as a step forward to speed-up the discovery of chromone-based multitarget-directed ligands.
6-溴色酮-2-羧酸（）通过微波辅助法合成。通过改变碱的种类/试剂当量的数量、溶剂、温度和反应时间等参数对反应进行了优化。反应收率提高到 87%。新的合成路线具有通用性，因为几种色酮-2-羧酸（化合物 -）以良好的收率（54-93%）得到。只有在硝基取代基（化合物）的情况下，得到的是酯而不是所需的羧酸。通过这种合成路线，可以获得高纯度的色酮羧酸，而无需通过繁琐且昂贵的柱色谱纯化过程。该反应安全、经济高效、快速且稳健，可用于基于色酮支架的简洁和多样化导向文库的开发。总的来说，这项研究可以看作是加快发现基于色酮的多靶点导向配体的一个步骤。
