110623-33-1Relevant articles and documents
Kinetics for scale-up of a one-pot pathway to 5-(3-fluorophenyl)-2,4- dihydro-2,4-dimethyl-3H-1,2,4-triazole-3-thione using a hybrid model of parallel and consecutive reactions
Louks, David H.,Stolz-Dunn, Sandra K.
, p. 877 - 884 (2007)
Kinetic results are reported for the one-pot reaction of 2,4-dimethylthiosemicarbazide (1) and 3-fluorobenzoyl chloride (2) to the unisolated benzamide intermediate (3), and on to the ringclosed product, 5-(3-fluorophenyl)-2,4-dihydro-2,4-dimethyl-3H1,2,4-triazole-3-thione (4). The sensitivity of the synthetic route to competing side reactions was examined by studying the kinetics of each reaction step. A first-order kinetic Model of the hybrid consecutive and parallel reaction scheme was developed and fit to experimental data. The Model was extended to address potential mixing concerns resulting from the formation of the insoluble intermediate 3 upon scale-up where a more concentrated reaction would be used. Scale-up of the product drug substance from laboratory to 50-gal scale was successfully completed using this recently developed one-pot pathway.
3-phenyl-1,4-dialkyl-1,2,4-triazolium salts and their use as antidepressants
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, (2008/06/13)
This invention relates to the treatment of depression by administration of novel 3-(Rn -phenyl)-1,4-dialkyl-1,2,4-triazolium salts of the formula STR1 wherein R is halogen, trifluoromethyl, C1-4 lower alkyl or C1-4 lower alkoxy, n is zero, 1 or 2, and R1 and R4 independently represent C1-3 lower alkyl; and A- represents a pharmaceutically acceptable anion.
Process for the preparation of 5-aryl-2,4-dialkyl-3H-1,2,4-triazole-3-thiones
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, (2008/06/13)
The present invention relates to a a novel process for preparing 5-aryl-2,4-dialkyl-3H-1,2,4-triazole-3-thiones which have been shown to have antidepressant activity and are useful in the treatment of Wernicke-Korsakoff syndrome and Alzheimer's disease.
5-aryl-2,4-dialkyl-3H-1,2,4-triazole-3-thiones useful as antidepressants
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, (2008/06/13)
This invention relates to novel 5-(Rn -phenyl)-2,4-dialkyl-3H-1,2,4-triazole-3-thiones and to their use as antidepressants.
2,4-Dihydro-3H-1,2,4-triazole-3-thiones as Potential Antidepressant Agents
Kane, John M.,Dudley, Mark W.,Sorensen, Stephen M.,Miller, Francis P.
, p. 1253 - 1258 (2007/10/02)
A series of 5-aryl-2,4-dihydro-3H-1,2,4-triazole-3-thiones was prepared and evaluated for potential antidepressant activity.Members of this series were generally prepared by the alkaline ring closures of the corresponding 1-aroylthiosemicarbazides.Several
5-aryl-2,4-dialkyl-3H-1,2,4-triazole-3-thiones and their use as antidepressants
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, (2008/06/13)
This invention relates to novel 5-aryl-2,4-dialkyl-3H-1,2,4-triazole-3-thiones, to the intermediates and processes for their preparation, and to their use as antidepressants.
Process for the preparation of 5-aryl-2,4-dialkyl-3H-1,2,4-triazole-3-thiones
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, (2008/06/13)
This invention relates to a novel process for the preparation of 5-aryl-2,4-dialkyl-3H-1,2,4-triazole-3--thiones, useful as antidepressants, through the thionation of the corresponding 5-aryl-2,4-dialkyl-3H-1,2,4-triazol--3-ones.