Synthesis and Biological Activity of N-Dichloroacetyl-3-methyl-2-n-propyl-l-oxa-4-aza-spiro-4,5 -decane

摘要

Herbicide safeners are the compounds which can protect crops from being injured by herbicides and enhance the tolerance of crops to herbicides. They can enlarge the application scope of herbicides. N-dichloroacetyl oxazolidine compounds, such as R-28725(N-dichloroacetyl-2,2-dimethyl-l, 3-oxazolidine), are a new series of herbicide safeners reported recently. They are good safeners for thiocarbamate and chloracetamide herbicide and can also be used to protect the crops from some sul-fonylurea or imidazolinone herbicide injury. In order to investigate the relationship between the chemical structure and the biological activity of N-dichloroacetyl oxazolidine, a series of N-dichloroacetyl oxazolidine compounds have been synthesized. The title compound is a novel N-dichloroacetyl oxazolidine compound. The present paper covers the synthesis of the title compound which was prepared from nitroethane, n-bu-tyraldehyde, cyclohexanone and dichloroacetyl chloride as the starting material outlined in Scheme 1. This procedure has a wide scope and should allow for the synthesis of a large variety of W-dichloroacetyl oxazolidines which are the potential antidotes of some herbicides. The preliminary biological activity of the title compound has also been studied.