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The preparation of the four stereoisomers of propiconazole (TILT®) is described. Their inhibition of the 14α-C-demethylation of the sterol nucleus is examined and compared with the inhibition by the four stereoisomers of etaconazole (SONAX®). The quantitative structure-activity relationships (QSAR) of substituted 1,3-dioxolane-2-yl-methyltriazoles and 1,3-dioxane-2-ylmethyltriazoles on in vivo fungicidal activity are investigated.

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Summary. ;\n improved synthesis of 4-carbethoxyquinuclidinc from 1-benzyl-4-piperidone is described.

The preparation of CGA 80000 (a-[N-(3-chloro-2,6-xylyl)-2-methoxyacetamidol-y-butyrolactone) and the separation of the four optical isomers and the diastereomeric pairs of enantiomers are described. The relationships between their absolute configurations and fungicidal activities have been examined. Biological tests have proved that one of the four isomers, with the absolute configuration (as, 3R) is mainly responsible for the fungicidal activity of CGA 80000.is not a BSI/ISO approved common name.The name clozylacon has been used for this compound. This EXPERIMENTALAll new compounds have been fully characterised by NMR and elemental analysis. N M R spectra were recorded on a Bruker AM-300 instrument; chemical shifts are reported in ppm relative to internal tetramethylsilane standard (= 0 ppm). Melting points are uncorrected. Chemical synthesisThe preferred sequence for the preparation of CGA 80000 started from 2,6-dimethylaniline and involved three steps as shown in Fig. 2. 2.1.1 a-(2,6-Xylidino)-y-butyrolactone (Fig. 2 ; ZZZ) Anhydrous sodium carbonate (64 g; 0.6 mole) was suspended in a solution of 2,6-dimethylaniline (121 g; 1.0 mole) in xylene (500 ml). a-Bromo-y-butyrolactone (206 g; 1.25 mole) was added over a period of 2 h to this suspension at reflux temperature (about 140°C). After completion of the addition, the reaction mixture was stirred for 4 h at the same temperature. Water produced in the reaction was removed during the addition of the abromo-y-butyrolactone and during the subsequent stirring by means of a Dean and Stark trap. The reaction 223 Pesric. Sci.