Synthesis of derivatives of 1,3,2-diazaphospholidin-4-ones and the corresponding 2-sulfides

Aromatic-substituted derivatives of 1,3,2-diazaphospholidin-4-ones 2a-g wer e readily prepared front 1,3-diaryl glycinamides 1 by the reaction with hex aethylphosphoric triamide. Their chemical transformation was selectively ef fected with different thionation reagents to afford thionated products at t he phosphorus atom to give 3a-g and at the carbonyl group to give 4a. An ox idation reaction at phosphorus to produce 5a was effected with 10% hydrogen peroxide. Preliminary bioassays revealed that some of the title compounds, 2a-g and 3a-g, possess selective herbicidal activity against rape. (C) 200 1 John Wiley & Sons, Inc.