Synthesis And Biological Activityof Diclofenac, Diclofenac Derivative

Non-steroidal anti-inflammatory drugs (NSAIDs, Non-steroidal anti-inflammatory drugs) mainly refers to a class of anti-inflammatory,analgesic and antipyretic effect of corticosteroid-free non-steroidal drugs,widely used in the clinical treatment of chronic inflammation, mainly forthe treatment ofinflammatory diseases such as rheumatism arthritis,rheumatoid arthritis, osteoarthritis,can relieve various pain symptoms.However, after clinical use found that most of the NSAIDs presenceserious adverse effects, leaving the use of such drugs be limited.Therefore, how to reduce adverse drug reactions, study the mechanism,the old drugs new study by scholars at home and abroad has become thefocus. Diclofenac and its derivatives are the most representative class ofnon-steroidalanti-inflammatory drugs. At present, the diclofenac sodium,its action of mechanism is that it can selective cutting the link ofcyclooxygenase role in arachidonic acid metabolism,blocking thesynthesis of prostaglandins (PGs). They have a better treatment ofinflammatory, analgesic, anti-rheumatic therapy, can replace morphineanalgesic drugs, which have distinct pharmacologically characteristicsand significantly pharmacokinetic characteristics. For the needs ofindustrial production, this the sisestablisha chemical process to synthesisdiclofenac. Aniline anddichloro phenol as starting materials, by thefollowing reactions: such as chlorine acylation, etherification,rearrangement get intermediate synthetic2,6-dichloro-diphenylamine;2,6-dichloro-diphenylamine by acylation,cyclization,hydrolysis reactionsto synthetize diclofenac sodium and diclofenac potassium. After acidifiedthe diclofenac, the reaction with the sulfate, to form the correspondingsalt of diclofenac compound.This process can be obtained by a relativelysimple method of process materials, shorter overall reaction scheme, using milder reaction conditions, safety, simple operation, low cost, moreimportantly, can be good to use for industrial production. In addition, wehave modified the structure of diclofenac get diclofenac derivative:diclofenac methyl, diclofenac ethyl anddiclofenac butyl. We studied thebiological activity of these compounds,the experiments are xylene-induced ear edema and writhing in mice. The results show that thesecompounds also have anti-inflammatory and analgesic activity.Innovation of this paper is to synthesize a series of diclofenac salt anddiclofenac derivatives, we get seven diclofenac salt compounds, what aresynthesized for the first time expect diclofenac zinc.Diclofenacderivatives of diclofenac ethyl ester and butyl ester are synthesized forthe first time. Currently, the clinical application of diclofenac sodium anddiclofenac potassium more adverse reactions, mainly to stimulate thegastrointestinal mucosa, easy to form ulcers, the purpose of this articlethe synthesis of these compounds is hoped to expand the diclofenac aciddrugs, to find adverse reactions inflammatory and analgesic good effectof alternative medicine.