DISCOVERY OF A HERBICIDAL LEAD USING POLYMER-BOUND ACTIVATED ESTERS IN GENERATING A COMBINATORIAL LIBRARY OF AMIDES AND ESTERS

A combinatorial library containing mixtures of amides and esters was p repared through solid-phase chemistry. The advantages of using solid-p hase chemistry over solution-phase chemistry to prepare this library a re 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 provid ed enyl)-3-(1,1-dimethylethyl)-1-methyl)-1H-pyrazole- 5-carboxamide as a herbicidal lead with broadleaf and narrowleaf pre-emergence herbici dal activity as low as 100 g/ha on some weed species. This study repre sents the first report of an agrochemical discovered using a combinato rial approach.