| With the increasing need of food in the whole world,great importance has been put on the pesticides for protecting the plant from pets and disease.However,as a kind of chemicals,its long-term use will do harm to the environment.So the development of green,environmental-friendly,efficient,and low toxic pesticides is very attractive recently.Metconazole,as a triazole antiseptic,fits the need nicely.Until now,several methods mainly using diethyl adipate as the starting material have been reported to synthesize this compound.However,these approaches still have the problems of multiple steps and low yields.Therefore,it is highly desireable and meaningful to develop a new and efficient route for the synthesis of metconazole.In this dissertation,we have developed a simple and new approach for the preparation of metconazole from cyclopentanone and p-chlorobenzaldehyde.Every step in the route was carefully optimized.Meanwhile,the enantioselective synthesis of metconazole in optically pure form was also studied using the hydrogenation technology developed in our lab.In summary,this process has reached the industrialization production standards since the advantages of short route,high yield,convenient operability,as well as good economics and safety. |
