We report a simple, fast, and eco-friendly solvent-free protocol for the synthesis of 2-aminothiazoles and 2-amino-1,3-selenazoles (16 examples) through Hantzsch condensation without the use of a catalyst. It is noteworthy that this type of procedure is unprecedented for the synthesis of 1,3-selenazoles. Reactions proceed to completion in a few seconds and products are obtained in moderate to excellent yields after easy workup. Moreover, the synthesis of 4-(2-amino-1,3selenazol-4-yl)benzonitrile hydrobromide is reported for the first time.

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A very fast method for the synthesis of the title thiazoles and selenazoles through Hantzsch cyclization starting from thiourea and selenurea, resp., is developed.

Tuberculosis (TB), remains a global health challenge, despite the many efforts and recent advances in medicine and pharmacology. The World Health Organization estimates that 1.5 million people worldwide died due to TB infection in 2018. In this context, the search for novel molecules that can offer higher potency, shorter treatment times, and fewer side effects is urgent. This work describes the synthesis of eight new benzylpiperazines containing the pyrazine moiety, with potential activity against TB. The structures were rationally planned using the molecular hybridization technique, from the drug pyrazinamide and the benzylpiperazine core. All proposed substances were obtained from a simple and reproductible synthetic process, in low yields.

NERY, A. C. S.; AVELLAR, M. M.; GOMES, C. R. B.; DE SOUZA, M. V. N.; VASCONCELOS, T. R. A.; Curr. Org. Synth. 12 (2015) 2, 140-149, http://dx.doi.org/10.2174/1570179411666141201201009 ; Inst. Tecnol. Farm.-Far Manguinhos, FioCruz-Fundacao Oswaldo Cruz, 21041 Rio de Janeiro, Brazil; Eng.) -S. Adam 30-287

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