Abstract

A highly efficient green protocol is described for the development of novel benzo[4,5]thiazolo[3,2-a]pyrimidine analogues through the one-pot fusion of the 2-amino-benzothiazole with different chosen aldehydes and active methylene compounds, in ethanol medium under ultrasound irradiation conditions by using ammonium acetate as a catalyst. We achieved excellent yields (94–97%) for 24 novel target products with short reaction time (10–15 min) at room temperature. We confirmed the structures of the synthesized pyrimidine analogues by NMR and HRMS spectroscopic analysis. Exceptional yields, simple workup, no column chromatography, green solvent, rapid reaction at room temperature and excellent functional group tolerance are the benefits of this protocol.

摘要

描述了一种高效的绿色方案，用于通过 2-氨基苯并噻唑与不同选择的醛和活性亚甲基化合物的一锅融合来开发新型苯并[4,5]噻唑并[3,2- a ]嘧啶类似物，以醋酸铵为催化剂，在超声辐照条件下在乙醇介质中进行研究。我们在室温下以较短的反应时间（10-15 分钟）实现了 24 种新型目标产物的优异产率（94-97%）。我们通过NMR和HRMS光谱分析证实了合成的嘧啶类似物的结构。优异的产量、简单的后处理、无柱层析、绿色溶剂、室温下快速反应和出色的官能团耐受性是该协议的优点。