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In the search for better herbicides a series of 1-alkyl-3-(α-hydroxy-(un)substituted benzylidene)pyrrolidine-2,4-diones were prepared and their structure-activity relationships studied. All their structures have been confirmed by 1H-NMR andelemental analysis. The preliminary bioassay results indicated that some of them have highherbicidal activity against annual dicotyledonous and monocotyledonous plants.