Microwave-Assisted C-N Coupling for the Synthesis of 2-(2H-1,2,3-Triazol-2-yl)benzoic Acid Scaffold and Novel N-Phenyl-2-(2H-1,2,3-triazol-2-yl)benzamide Derivatives

D. Pandya, Y. Naliapara
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Abstract

We report a novel methodology for the efficient and rapid synthesis of core intermediate 2-(2H-1,2,3- triazol-2-yl)benzoic acid using trans-N,N’-dimethylcyclohexane-1,2-diamine as a catalyst and copper iodide as co-catalyst under microwave irradiations and a series of novel N-phenyl-2-(2H-1,2,3-triazol- 2-yl)benzamide derivatives via acid-amine coupling reaction using DCC as a dehydrating agent and DMAP as a base. In comparison to the conventional heating procedure and performing the reaction using different combinations of catalysts and bases, the time of synthesis and efforts are significantly reduced in the present method, which also gave excellent yield. The scaffold and all novel amides were characterized by spectroscopic techniques.
微波辅助C-N偶联合成2-(2h -1,2,3-三唑-2-基)苯甲酸支架及新型n -苯基-2-(2h -1,2,3-三唑-2-基)苯酰胺衍生物
本文报道了一种以反式N,N ' -二甲基环己烷-1,2-二胺为催化剂,共吡啶为助催化剂,微波辐射下高效快速合成核心中间体2-(2h -1,2,3-三唑-2-基)苯甲酸的新方法,以及以DCC为脱水剂,dmap为碱,通过酸-胺偶联反应合成一系列新型N-苯基-2-(2h -1,2,3-三唑-2-基)苯酰胺衍生物。与传统的加热工艺和不同的催化剂和碱的组合反应相比,该方法的合成时间和工作量大大减少,产率也很好。用光谱技术对支架和所有新酰胺进行了表征。
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