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FOCUSED SMALL MOLECULE LIBRARY OF 5,6,7,8-TETRAHYDRO[1,2,4]TRIAZOLO[4,3-a]PYRAZINES: A BRICK FOR THE HOUSE OF MEDICINAL CHEMISTRY

Oleksandr V. Borysov, Volodymyr V. Voloshchuk, Maksym A. Nechayev, Viacheslav A. Lysenko, Mykola M. Nikolaychuk, Anton O. Portiankin, Oleksandra V. Oliinyk, Dmitry A. Lega, Dmytro M. Volochnyuk, Sergey V. Ryabukhin
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Abstract


The article highlights the challenges and opportunities in the development of the piperazine-fused triazoles. Approaches toward medicinal chemistry relevant building blocks based on [1,2,4]triazolo[4,3-a]pyrazine platform were elaborated. The methods provide quick and multigram access to the target derivatives starting from commercially available nonexpensive reagents. The approaches were used to create a small library of the triazolopyrazines with variety of substituents in position 3. The potential of further synthetic application of the library members for medicinally oriented synthesis was shown.

Keywords


DPP-4 inhibitors; sitagliptin; [1,2,4]triazolo[4,3-a]pyrazine; heterocyclization; medicinal chemistry

Full Text: PDF Supplementary File(s): Supporting information (9MB)


 

 

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