Improved Process For The Synthesis Of Quetiapine Hydrochloride

Quetiapine is becoming a novel drug for the treatment of mental illness. With sharp development of social economy, the pace of life is increasing rapidly. As a result, people have to endure more and more pressure and the incidence of this disease is rising annuallyThe paper is about processing technology of quetiapine hydrochloride. On the basis of consulting and summarizing the literatures concerned, the author selected two routes to synthesize quetiapine hydrochloride and did some processing technology optimization:(1) Choose o-aminothiophenol and o-chlorobenzoicbenzonitrile as starting material, first etherify under potassium carbonate and cyclize under sodium tert-butanol,hydrochloride, and then react with N-[2-(2-hydroxyethoxy)ethyl] piperazine to abtain quetiapine, at last, make it into quetiapine hydrochloride;(2) Choose o-iodobenzoic acid as starting material, after acyl chloride, acid amide and sulfide, protection of amino and hydroxy, cyclization, at last, deprotection of hydroxy to get quetiapine, and then make it into quetiapine hydrochloride.This paper chiefly optimized these two select routes and explored the experimental conditions such as the choice of solvent, reagent, the ratio of raw materials, reaction temperature, reaction time, addition manner and so on.Such research leads to simpler reaction operation, lower cost and higher yield which is in ex-preparation for the industrial production.