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

Authors

  • Oleksandr V. Borysov Enamine Ltd., 78 Winston Churchill St., Kyiv 02094
  • Volodymyr V. Voloshchuk Enamine Ltd., 78 Winston Churchill St., Kyiv 02094
  • Maksym A. Nechayev Enamine Ltd., 78 Winston Churchill St., Kyiv 02094
  • Viacheslav A. Lysenko Institute of Organic Chemistry, National Academy of Sciences of Ukraine, 5 Akademika Kukharya St., Kyiv 02660
  • Mykola M. Nikolaychuk Enamine Ltd., 78 Winston Churchill St., Kyiv 02094
  • Anton O. Portiankin Enamine Ltd., 78 Winston Churchill St., Kyiv 02094
  • Oleksandra V. Oliinyk Enamine Ltd., 78 Winston Churchill St., Kyiv 02094
  • Dmitry A. Lega Enamine Ltd., 78 Winston Churchill St., Kyiv 02094 National University of Pharmacy, 53 Pushkinska St., Kharkiv 61002
  • Dmytro M. Volochnyuk Enamine Ltd., 78 Winston Churchill St., Kyiv 02094 Taras Shevchenko National University of Kyiv, 60 Volodymyrska St., Kyiv 01033 Institute of Organic Chemistry, National Academy of Sciences of Ukraine, 5 Akademika Kukharya St., Kyiv 02660
  • Sergey V. Ryabukhin Enamine Ltd., 78 Winston Churchill St., Kyiv 02094 Taras Shevchenko National University of Kyiv, 60 Volodymyrska St., Kyiv 01033 Institute of Organic Chemistry, National Academy of Sciences of Ukraine, 5 Akademika Kukharya St., Kyiv 02660

DOI:

https://doi.org/10.1007/7503

Keywords:

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

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.

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Published

2023-08-09

Issue

Vol. 59 No. 6/7 (2023): Ukrainian impact on heterocyclic chemistry after the three decades of independence

Section

Original Papers