Discovery of a herbicidal lead using polymer-bound activated esters in generating a combinatorial library of amides and esters |
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Authors: | John J. Parlow Jean E. Normansell |
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Affiliation: | (1) Ceregen Division of Monsanto Company-U2D, 800 North Lindbergh Boulevard, 63167 St. Louis, MO, USA |
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Abstract: | Summary A combinatorial library containing mixtures of amides and esters was prepared through solid-phase chemistry. The advantages of using solid-phase chemistry over solution-phase chemistry to prepare this library are discussed. The library was screened through a high-throughput whole organism herbicidal assay upon which a mixture containing amides was found to have herbicidal activity. Deconvolution of the mixture providedN-(3-benzoylphenyl)-3-(1,1-dimethylethyl)-1-methyl)-1H-pyrazole-5-carboxamide as a herbicidal lead with broadleaf and narrowleaf pre-emergence herbicidal activity as low as 100 g/ha on some weed species. This study represents the first report of an agrochemical discovered using a combinatorial approach.Supplementary Material, comprising experimental procedures for the preparation of resin II and the reaction of II with nucleophiles, GC/MS and LC/MS data for the reaction ofII with morpholine, and a detailed experimental for the preparation of 2 with characterization data, is available upon request. |
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Keywords: | Amide library Ester library Polymer-bound activated esters Herbicide lead Combinatorial library |
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