Shah J J, Mohanraj Krishnapriya
Department of Pharmaceutical Chemistry, Bombay College of Pharmacy, Kalina, Santacruz (E), Mumbai-400 098, India.
Indian J Pharm Sci. 2014 Jan;76(1):46-53.
A green chemistry approach for organic synthesis is described here, which involves microwave exposure of reactants in presence or absence of solvents. A novel and simple method has been developed for the synthesis of some benzotriazole derivatives under microwave irradiation. In addition, these compounds were synthesised also by conventional heating procedures for comparison. All the compounds synthesised were characterised by melting point, TLC, IR and (1)H NMR spectroscopy. Comparison between conventional and microwave-assisted synthesis was done by comparing total reaction time and percentage yield. The results suggest that microwave-assisted syntheses lead to higher yields within very short reaction times. On antifungal evaluation by cup plate method, all compounds showed antifungal activity. One compound showed activity similar to and two compounds showed better activity than standard antifungal drug flucanazole.
本文描述了一种用于有机合成的绿色化学方法，该方法涉及在有或没有溶剂存在的情况下对反应物进行微波照射。已经开发出一种新颖且简单的方法，用于在微波辐射下合成一些苯并三唑衍生物。此外，还通过传统加热程序合成了这些化合物以作比较。所有合成的化合物均通过熔点、薄层色谱、红外光谱和核磁共振氢谱进行表征。通过比较总反应时间和产率百分比，对传统合成和微波辅助合成进行了比较。结果表明，微波辅助合成在非常短的反应时间内可获得更高的产率。通过杯碟法进行抗真菌评估时，所有化合物均显示出抗真菌活性。一种化合物显示出与标准抗真菌药物氟康唑相似的活性，两种化合物显示出比氟康唑更好的活性。
