Of Fungicides Cyproconazole Development And Process

Cyproconazole, which was widely used in agricultural pesticide, belongs to triazolic bactericide, it has good preventive and therapeutic effect on common plant pathogenic bacteria, and also can be used with other bactericides. This article introduces a new synthetic route of cyproconazole, which was not reported in any literatures. The synthetic route have advantages of stability, low cost, and high yield.Cyclopropyl methyl ketone was used as starting material in this article to synthesize 2-cyclopropylpropanal by Darzen reaction, Then appropriate phase transfer catalyst was added to above reaction product using potassium permanganate as oxidant to synthesize 2-cyclopropylpropanoic acid, next thionyl chloride as acylation reagent was added to synthesizeα-cyclopropylpropanoyl chloride, lastly target product cyproconazole was synthesized by five step including synthesis ofα-methyl-4-chlorophenyl cyclopropyl methyl ketone by Friedel-Crafts acylation reaction.The influence to each reaction step by process parameters including reaction temperature, reaction time, catalyst, amount of acylation reagent and oxidant was majorly investigated. Process study was intensively carried out by the methods of one-factor and orthonal experiment, expectively. Optimum process was acquired, and primary mechisms of every reaction were also discussed. Intermediate products and cyproconazole were purified, and their structures were characterized by IR (infrared spectrum),HPLC(high pressure liquid chromatography), GC(gas chromatography),1H-NMR (nuclear magnetic resonance), and MS (mass spectrum).