Facile, diversity-orientated one-pot synthesis of ethyl 1,5-disubstituted-1H-1,2,4-triazole-3-carboxylates |
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| Authors: | Sébastien Degorce Bénédicte DelouvriéPaul RJ Davey Myriam DidelotHervé Germain Craig S Harris Christine Lambert-van der Brempt Honorine LebraudGilles Ouvry |
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| Institution: | a AstraZeneca Oncology iMed, Centre de Recherches, Z.I. la Pompelle, BP1050, 51689 Reims Cedex 2, France
b AstraZeneca Oncology iMed, Alderley Park, Cheshire SK10 4TG, UK |
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| Abstract: | Access to the 1,5-disubstituted-1H-1,2,4-triazole-3-carboxamide motif is quite laborious and requires forcing conditions to effect the cyclocondensation step. Herein, we report an efficient and mild one-pot protocol to access this substructure in good chemical yields with high regiocontrol. |
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| Keywords: | Ethyl 1 5-disubstituted-1H-1 2 4-triazole carboxylates Regioselective acylation of N-substituted hydrazines Cyclodehydration |
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