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A series of 6-fluoroaryl substituted [1,2,4]triazolo[1,5-A]pyrimidines have been synthesized by using the microwave-Assisted Suzuki cross-coupling reaction from readily available 6-bromo-[1,2,4]triazolo[1,5-A]pyrimidine. The antimicrobial activity of new compounds has been evaluated in vitro against Mycobacterium tuberculosis H37Rv and gram-negative (Neisseria gonorrhoeae ATCC 49226) bacteria. © ARKAT-USA, Inc.

The Petasis reaction of 6-alkoxy adducts of 1-alkyl-2,3-dicyano-5- arylpyrazinium salts with aromatic boronic acids, such as 2-thienylboronic, 2-furanylboronic and 3-thienylboronic acids, or their benzo analogs in dichloromethane proceeds smoothly at room temperature with the formation of the corresponding 5-aryl-6-hetaryl substituted 1,6-dihydropyrazine derivatives. All dihydropyrazines were separated as pure enantiomers by chiral HPLC, and their absolute configurations for each pair of enantiomers have been determined by X-ray analysis. Individual enantiomers were screened in vitro for their antimycobacterial activities against Mycobacterium tuberculosis H37Rv, avium, terrae and extensively drug-resistant and multi-drug-resistant strains isolated from tuberculosis patients in Ural region (Russia). It has been shown that several compounds exhibit a good level of antituberculosis activity compared to the reference drugs. © ARKAT-USA, Inc.