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Published on: May 31, 2024
Rapid parallel synthesis of combinatorial libraries of substituted 3-thio-1,2,4-triazoles and 2-thioimidazoles
Maria-Elena Theoclitou1, Nancy G J Delaet, Leslie A Robinson
1Bristol-Myers Squibb, Pharma Research Laboratories, 4570 Executive Drive, San Diego, California 92121, USA. Maria-Elena.Thouclitou@dupontpharma
Abstract:
Combinatorial libraries of substituted 3-thio-1,2,4-triazoles and 2-thioimidazoles were synthesized in good yield by alkylation of the products via the reaction of isothiocyanates and carboxylic acid hydrazides or beta-aminoketones, respectively. A total of 275 3-thio-1,2,4-triazoles and 283 2-thioimidazoles were synthesized out of the attempted 288 in each case. Most the yields were between 45% and 98%, and all the compounds synthesized were purified to >85% purity. Variations in yields revealed no definitive trends and were mainly attributed to bulky alkylating agents used and the plate well location of the reaction mixtures.
