连续流氧化工艺合成丙硫菌唑

Synthesis of Prothioconazole via Continuous Flow Oxidation

丙硫菌唑是新型广谱三唑硫酮类杀菌剂,其合成过程中氧化条件苛刻,规模化生产存在很大挑战,为此开发了清洁、温和的连续流氧化工艺。在微通道反应器中,中间体2-(1-氯环丙烷-1-基)-1-(2-氯苯基)-2-羟基-3-(1,2,4-三唑烷-5-硫酮-1-基)-丙烷在氧化剂作用下,连续高效合成丙硫菌唑。在优化条件下,该中间体可以定量转化为丙硫菌唑。连续流氧化工艺条件温和,转化率高,适合工业化生产。

Prothioconazole is a new triazolinthione fungicide with broad spectrum bioactivities. A big challenge in the large scale preparation of prothioconazole is the oxidation condition. Thus a clean and mild continuous flow- oxidation process was studied. The intermediate 1-（2-（1-chlorocyclopropyl）-3-（2-chlorophenyl）-2-hydroxypropyl）-i H-1,2,4-triazole- 5 （4H）-thione was oxidized in the presence of oxidant in micro-reactor to generate prothioconazole continuously. Prothio- conazole could be synthesized efficiently under optimized condition. The continuous flow- oxidation method featured with the advantages of mild reaction condition and high total yield, and it was suitable for industrial production.