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Facile One-Pot Parallel Synthesis of 3-Amino-1,2,4-triazoles

ACS Comb. Sci. 2018, 20 (7), 461-466

DOI: 10.1021/acscombsci.8b00060

Bogolyubsky A.; Savych O.; Zhemera A.; Pipko S.; Grishchenko A.; Konovets A.; Doroshchuk R.; Khomenko D.; Brovarets V.; Moroz Y.; Vybornyi M.

A 1,2,4-triazole motif is present in numerous commercialized and investigational bioactive molecules. Despite its importance for medicinal chemistry, there is a lack of convenient combinatorial approaches toward this molecular core. Herein, we present a synthetic strategy suitable for the quick preparation of a library of structurally diverse 1,2,4-triazoles in a one-pot setting. The key steps include the formation of thioureas followed by S-alkylation using 1,3-propane sultone and consecutive ring closure leading to the desired 1,2,4-triazoles. Parallel synthesis yields thousands of 1,2,4-triazoles in a cost- and time-efficient manner from commercially available chemicals.

Facile One-Pot Parallel Synthesis of 3-Amino-1,2,4-triazoles

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