Rapid parallel synthesis of combinatorial libraries of substituted 3-thio-1,2,4-triazoles and 2-thioimidazoles.

Autor: Theoclitou ME; Bristol-Myers Squibb, Pharma Research Laboratories, 4570 Executive Drive, San Diego, California 92121, USA. Maria-Elena.Thouclitou@dupontpharma, Delaet NG, Robinson LA
Jazyk: angličtina
Zdroj: Journal of combinatorial chemistry [J Comb Chem] 2002 Jul-Aug; Vol. 4 (4), pp. 315-9.
DOI: 10.1021/cc010094o
Abstrakt: 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.
Databáze: MEDLINE