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DOI: 10.1055/s-2005-870020
Parallel Synthesis of a Library of Acylsemicarbazides Using a Solution-Phase One-Pot Method and Their Evaluation as Crop-Protection Agents
Publication History
Publication Date:
18 July 2005 (online)
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Abstract
A solution-phase one-pot synthesis of a 40-member acylsemicarbazide library is outlined. The acylsemicarbazides were prepared by reacting various hydrazides with N,N′-carbonyldiimidazole (CDI) to generate 1,3,4-oxadiazole-2-one intermediates, which were then opened in situ with amines. Purification in the majority of cases was accomplished through filtration of the precipitated product in generally good yields and with ³ 95% purities. An analogous synthesis of acylthiosemicarbazides was accomplished using N,N′-thiocarbonyldiimidazole (TCDI). The library was then assayed for herbicidal, insecticidal, fungicidal and plant growth regulatory behavior.
Key words
acylsemicarbazides - acylthiosemicarbazides - 1,3,4-oxadiazol-2-one - solution phase - library - crop protection
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