Synthesis and fungicidal activity of some 5-(2-aminoalkanoyl)-8-aryl-4(5H)-oxo-1,2,4-triazolo[4,3-b]-1,4,2, 6-dithiadiazine 6,6-dioxide derivatives.
Title compounds (5) were conveniently prepared from 5-aryl-3-mercapto-1,2,4-triazoles (1) and chloro-sulphonyl isocyanate (CSI) to give 8-aryl-4-(5H)-oxo-1,2,4-triazolo-[4,3-b]-1,4,2,6-dithiadiazine -6,6-dioxide (2). The Compound (2) and one suspension of 2-(benzyloxycarbonylamino) akanoic acid (3) in the presence of BOP reagent afforded Z-derivatives 8-aryl-5-(2-benzyloxycarbamoyl)alkanoyl-4(5H)-oxo- 1,2,4-triazolo[4,3-b]-1,4,2,6-dithiadiazine 6,6-dioxide (4). The Z-derivatives (4) gave aspected product (5) when treated with Pd-c 5% and formic acid in DMF. These compounds have been tested in vitro for their fungicidal activity against Aspergillus niger, Fusarium oxisporum and Cephalosporium saccharii and results were compared with their parent dithidiazines.
Srivastava
M K
MK
Department of Chemistry, M.G.P.G. College, Gorakhpur, India.
Khare
R K
RK
Singh
H
H
D000935:Antifungal Agents / Q000138:chemical synthesis* / Q000494:pharmacology; D005658:Fungi / Q000187:drug effects*; D008826:Microbial Sensitivity Tests; D013829:Thiadiazines / Q000138:chemical synthesis* / Q000494:pharmacology; D014230:Triazoles / Q000138:chemical synthesis* / Q000494:pharmacology
D000935:Antifungal Agents; D013829:Thiadiazines; D014230:Triazoles