Discovery of a herbicidal lead using polymer-bound activated esters in generating a combinatorial library of amides and esters.

Mol Divers

Ceregen Division of Monsanto Company-U2D, St. Louis, MO 63167, USA.

Published: August 1996

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 provided N-(3-benzoylphenyl)-3-(1,1-dimethylethyl)-1-methyl)-1 H-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.

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http://dx.doi.org/10.1007/BF01715531DOI Listing

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