Department of Chemistry, College of Sciences, Guilan University, Rasht 41335-19141, Iran.
Department of Chemistry, College of Sciences, Guilan University, Rasht 41335-19141, Iran.
Bioorg Chem. 2018 Dec;81:326-333. doi: 10.1016/j.bioorg.2018.08.026. Epub 2018 Aug 23.
An improved, forthright, and highly efficient one-pot synthesis of a wide range of pharmaceutically exciting diverse kind of functionalized 2-amino-3-cyano-4H-pyrans and especially bis-pyrans compounds is developed using piperazine as a low-cost and environmentally benign commercially available basic catalyst in aqueous media. The attractive features of this process are simple procedure, short reaction times, high yields, no column chromatographic separation and commercial availability and recyclability of the catalyst. Also, piperazine can catalyze the synthesis of the target compounds on a larger scale. Furthermore, rational mechanism was suggested via GC-Mass analysis of the trapped intermediates.
开发了一种改良的、直截了当的、高效的一锅法合成，可广泛应用于制药领域，合成各种具有不同官能团的 2-氨基-3-氰基-4H-吡喃和双吡喃化合物。该方法使用哌嗪作为低成本、环境友好的商业可得的碱性催化剂，在水相介质中进行。该方法具有以下优点：操作简单、反应时间短、产率高、无需柱色谱分离、催化剂可商业获得且可重复使用。此外，哌嗪可以在较大规模上催化目标化合物的合成。此外，通过对捕获的中间体进行 GC-Mass 分析，提出了合理的反应机理。
