Photochemische und chemische Synthesen biologisch aktiver 3-Oxazoline |
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Authors: | Karl-Heinz Pfoertner François Montavon Karl Bernauer |
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Institution: | Zentrale Forschungseinheiten und Pharmazeutische Forschungsabteilung der F. Hoffmann-La Roche & Co. AG, CH–4002 Basel |
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Abstract: | Photochemical and Chemical Syntheses of Biologically Active 3-Oxazolines Using the photoreaction of 2H-azirines with carbonyl compounds, the 2,2-dimethyl-3-oxazolines 5a, 5b , and 6a have been obtained which bear a mono- or dichlorophenyl substituent at C(4) of the five-membered heterocycle and pyridyl at C(5). These compounds exhibit interesting activities against phytopathogenic fungi. Because 6a had been selected for field testing, its photochemical preparation was supplemented by a chemical synthesis. However, the overall performance of 6a in the field was inferior to some of the recently introduced agricultural fungicides of the ergosterol biosynthesis inhibitor type. Although 16 additional 3-oxazolines with varied substituents have been prepared, the fungicidal activity found with 6a could not be improved. |
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