Anticholinesterase activity of carboranyl containing thio- and selenoesters of pentavalent phosphorus acids has been studied. Insertion of the carboranyl substituents in the thioester group of phosphororganic compounds was found to increase the anticholinesterase activity as compared with the thioalkyl analogues. The compounds with B-carboranyl group are less active inhibitors of cholinesterase than their isomers with C-carboranyl group.
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J Org Chem
June 2023
CAS Key Laboratory of Receptor Research, State Key Laboratory of Drug Research, Shanghai Institute of Materia Medica, Chinese Academy of Sciences, Shanghai 201203, China.
We report herein the synthesis of exo-chalcogenated methylene chroman-3-ones via palladium-catalyzed intramolecular acyl-chalcogenation of alkyne with thio- and selenoesters. Chalcogen containing tetrasubstituted alkenes are obtained stereoselectively. This protocol tolerates various functional groups and heterocycles, affording the chroman-3-one products in moderate-to-good yields.
View Article and Find Full Text PDFInorg Chem
February 1999
Department of Chemistry, Faculty of Engineering, Gifu University, 1-1 Yanagido, Gifu 501-1193, Japan.
The first synthesis and characterization of sodium and potassium tellurocarboxylates were achieved by the reaction of acyl chlorides with the corresponding alkali metal tellurides. The salts are yellow to red solids or oils. The aliphatic derivatives are very sensitive toward oxygen and very thermally sensitive.
View Article and Find Full Text PDFJ Org Chem
October 1996
Université Claude Bernard-Lyon I, Laboratoire de Chimie Organique 3, associé au CNRS, 43 Bd du 11 Novembre 1918, 69622 Villeurbanne, France.
Alkyl and aryl trifluoromethanethiosulfonates(1) (or selenosulfonates) were prepared in one step either from alkyl and aryl sulfenyl (or selenenyl) chlorides and sodium trifluoromethanesulfinate (3) or, more generally, from disulfides (or diselenides), 3, and bromine. The second method involved trifluoromethanesulfonyl bromide as key intermediate. Benzenethiosulfonates were obtained in a similar way from disulfides, benzenesulfinate, and bromine but benzeneselenosulfonates could not be obtained by the same method from diselenides.
View Article and Find Full Text PDFAnticholinesterase activity of carboranyl containing thio- and selenoesters of pentavalent phosphorus acids has been studied. Insertion of the carboranyl substituents in the thioester group of phosphororganic compounds was found to increase the anticholinesterase activity as compared with the thioalkyl analogues. The compounds with B-carboranyl group are less active inhibitors of cholinesterase than their isomers with C-carboranyl group.
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