- Convenient synthesis and antimicrobial activity of some novel amino acid coupled triazoles
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This study describes a promising one-pot synthesis of [2-(5-benzyl-4- phenyl- 4H-[1,2,4]triazol-3-thio)-acetyl]-amino acid methyl esters 6a-h and dipeptides 10a-e, which were successfully synthesized starting from amino acid esters 5a-h, 9a-e and azides 4
- Rayes, S.M.El
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experimental part
p. 6759 - 6772
(2011/02/24)
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- Synthesis, characterization and studies of new 3-benzyl-4H-1,2,4-triazole- 5-thiol and thiazolo[3,2-b][1,2,4]triazole-5(6H)-one heterocycles
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(Chemical Equation Presented) 3-Benzyl-4-phenyl-1,2,4-triazole-5-thiol (1) was synthesized and used as starting material for preparation of 1,2,4-triazole bearing substituted thiosemicarbazides moiety (4a-d) in high yields. The thiosemicarbazides 4a-d were cyclized in basic medium to give two triazole rings linked by thiomethylene group (5a-d), while cyclization of thiosemicarbazides 4a-d with chloroacetyl chloride in the presence of CHCl3 and K 2CO3 afforded the thiazolidinone derivatives 6a-d. The reaction of thiosemicarbazides 4a-c with phenacyl bromide in the presence of EtOH and fused CH3COONa gave the corresponding thiazoline ring systems 7a-c. Condensation of the 3-benzyl-1,2,4-triazole-5(1H)-thiol (1) with chloroacetic acid and aromatic aldehydes (8a-g) in boiling acetic acid/acetic anhydride mixture in the presence of fused sodium acetate gave one single isomer only, which might be 9a-g or 10a-g. Upon application of Micheal addition reaction on compounds 9a-e with cyclic secondary amines such as piperidine or morpholine the 2-benzyl-6-(α-amino-aryl/methyl)-1,3-thiazolo[3,2-b][1,2,4] -triazol-5-ols (11a-j) were obtained in good yields The structure of all new compounds were determined using both spectral and elemental analyses.
- Sarhan, Abdelwareth A. O.,ElSherif, Hassan A. H.,Mahmoud, Abdalla M.,Habib, Osama M. A.
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p. 897 - 907
(2008/09/21)
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- THIOTRIAZOLYL DERIVATIVES
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The invention relates to KvI.5 ion channel antagonists. Novel thiotriazolyl derivative compounds represented by Formula I, and synthesis and uses thereof for treating diseases mediated directly or indirectly by KvI.5 ion channels, are disclosed. Such cond
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Page/Page column 52
(2008/06/13)
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