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Triazolobenzodiazepines are frequently described in the literature and are considered to be valuable components because of their broad range of biological activity. Derivatives of this structure, the triazolodiazepines, however are fairly limited described and the known synthetic methods lead to similar substitution patterns. Therefore, a simple synthetic method, leading to substituted 5,6,7,8-4H-[1,2,3]triazolo[1,5-a][1,4]diazepines, was developed. A one pot sequential reaction that consists of the known A3-coupling, followed by azidation and cyclization was developed. It was found that a one-pot A4-coupling was not possible because of the competition between the CuAAC and the A³-coupling. Applying the optimized conditions, a library of 24 compounds was synthesized. However, the extension of the one pot sequential reaction to substrates with an additional substituent on the seven membered ring, and the synthesis of triazolodiazocines, met with little success. The generated compounds will be screened for biological activity.