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Microwave-Assisted Sequential One-Pot Synthesis of 8-Substituted Pyrazolo[1,5-a][1,3,5]triazines
Authors:Jonathan Elie  Corinne Fruit  Thierry Besson
Institution:1.Perha Pharmaceuticals, Perharidy Peninsula, 29680 Roscoff, France; (J.E.); (C.F.);2.Normandie University, UNIROUEN, INSA Rouen, CNRS, COBRA UMR 6014, 76000 Rouen, France
Abstract:This paper reports a convenient sequential one-pot approach for the synthesis of an array of 14 pyrazolo1,5-a]1,3,5]triazines, substituted in C8 by halogen (Br), various functions (CN and CO2Et) and alkyl or (het)aryl groups. This study confirms the interest of combining the efficient heating obtained under dielectric microwave heating and the achievement of sequential one-pot reactions, avoiding the tedious work-up and purification of intermediate compounds, achieving sustainable synthesis processes. Considering usual conventional methods, this microwave protocol is featured by advantages in terms of yields, reaction times, and convenient gram scale synthesis.
Keywords:microwave-assisted chemistry  one-pot synthesis  pyrazolo[1  5-a][1  3  5]triazines  5-aza-9-deazapurines
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