Study On The Synthetic Process Of Perpentine

Perphenazine is an antipsychotic which belongs to a piperazine derivative of phenothiazine.It is often used for treatment of paranoid psychosis,reactive psychosis,symptomatic mental illness,simple and chronic schizophrenia.In this paper,the development of antipsychotic status and several types of common drugs were briefly introduced.The role of perphenazine in antipsychotic drugs was described.This paper summarizes the synthetic methods of perinitracyin reported in the previous literature,and provides an important basis for the subject.The method of selection and process improvement of perphenazine are discussed in detail.Finally,we get a suitable synthetic route.The process uses 2-chlorophenothiazine,1,3-bromochloropropane,hydroxyethyl piperazine as raw materials via two different synthesis routes.In this first route,2-chlorophenothiazine was used as starting material based on the main ring to react with 1,3-bromochloropropane,providing intermediate product 10-(3-chloropropyl)-2-chlorophenothiazine,which further reacted with 2-hydroxyethyl piperazine to prepare perphenazine.In the second route,1,3-bromochloropropane and hydroxyethyl piperazine react firstly getting side chain,and then react with the main ring.The resulting perphenazine salt is purified to give the final product.And the two routes were compared,and the content of phenothiazine impurity was reduced by changing the feed ratio,reaction temperature,reaction time and post-treatment method.The product was identified as the target compound by1 H NMR and the content of the product was above 99.5% by HPLC.The advantage of process design is that the reaction route is simple and the raw materials are cheap and easy to obtain.At the same time,the factors influencing the product yield in the experiment were analyzed and studied.And finally get the higher yield,purity of the standard process.The advantages and disadvantages of the two routes are compared.The cost of the product is reduced and the route is safer and more environmentally friendly through the optimization of the synthesis process.Recovery of solvents reduce the costs.The process for large-scale industrial production equipment is not demanding.