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A practical approach to imidazo[1,2]hetarylglyoxylates via Friedel-Crafts acylation of the parent fused imidazoles with ethyl oxalyl chloride is reported. The reaction is strongly influenced by the electron-donating properties of the starting heterocycle. The generated imidazo[1,2]hetarylglyoxylates undergo standard transformations typical of a-keto esters upon reaction with various nucleophiles. All the products contain an imidazoheterocyclic scaffold which is considered a privileged structure for drug discovery.

Imidazo[1,2]hetarylglyoxylates: Synthesis and Reactivity Toward Nucleophiles. -The title compounds are synthesized via Friedel-Crafts acylation of fused imidazoles with ethyl oxalyl chloride. The products undergo standard transformations typical for α-keto esters. -(ZAMKOVA, I. A.; CHEKOTYLO, O. O.; GERASCHENKO, O. V.; GRYGORENKO*, O. O.; MYKHAILIUK, P. K.; TOLMACHEV, A. A.; Synthesis

A New One-Step Synthesis of 1,2,4-Triazino[2,3-c]quinazolines. -Reaction of hydrazinoquinazoline (I) and α-ketocarboxylic esters (II) affords intermediate hydrazones which, in turn, undergo cyclocondensation followed by a Dimroth-type rearrangement to title compounds (III). -(KARPENKO*, O. V.; KOVALENKO, S. I.; CHEKOTYLO, O. O.; SHISHKINA, S. V.; Heterocycles 71 (2007) 3, 619-626; Dep. Pharm. Chem., Zaporizhzhia State Med. Univ., Zaporizhzhia 69035, Ukraine; Eng.) -M. Paetzel 30-140