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A general synthetic methodology employing heteroaryl-aryl Suzuki coupling is reviewed, by which 15 heteroaromatic ring systems of biological interest have been prepared.

Upon reaction with aqueous potassium hydroxide and aliphatic and aromatic aldehydes 2 the salts 1,2-diaminoquinolinium tosylate 4 and 1,2-diaminoisoquinolinium tosylate 9 were converted into the corresponding 2-substituted [1,2,4]triazolo[1,5-a]quinolines 8 and [1,2,4]triazolo[5,1-a]isoquinolines 13, respectively. The formation of the final products requires aerial oxidation.

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