Design&Synthesis Of Anti-influenza Drug Arbidol And It’s Derivatives

Arbidol’s chemical name is6-Bromo-4-(dimethylaminomethyl)-5-hydroxy-5-droxy-1-methyl-2-（phenylthiomethyl）-1H-indole-3-carboxylic acidethyl ester hydrochloride monohydrate．It as a non-nucleoside class of antiviral drugwas developed by Russian Chemical Pharmacy Research Institute．It not only hasbroad spectrum antiviral activity，but also has immune regulation effect and interferoninduced effect．Nawadays，it is mainly used in the treatment of influenza and it hasbeen listed in many nations．Arbidol is a novel anti-influenza drug and it has beenreceived extensive attention．Firstly， this paper summarize the influenza etiology as well as influenzaprevention and treatment．Then this paper focus on the synthesis process arbidolparticularly．Arbidol was synthesize by using acetoacetate and1,4-Benzoquinone asraw materials,and via Nenitzescu cylization reation，O-acylation，bromination，condensation and Mannich six steps of reaction with an overall yield of40.6%．TheNenitzescu reaction is the most important step reaction in synthesis of arbidol．Thispaper changes the traditional process conditions and then use the low temperaturereaction instead of heating the reaction．This paper intrduces a catalyst ZnCl2．Thissingle step yield can reach69%．In this paper,take arbidol as the lead compound,refer to a great deal of literatureas well as analyze and summarize arbidol structure-activity relationship．Then modifythe position of structure2，4，5and6．So far arbidol’s transformation has been mainlyfocused on the position1，2and4，but on6has not been enough researched．Thisarticle uses the substitusnts of nitro，amino and acetylamino instead of bromine and atthe same time changes the groups of2，4and5．The purpose is in order to prepare forthe further investigation of aibidol’s structure-activity relationship In the article21novel arbidol derivatives were designed and synthesized．The final products werecharacterized by1HNMR and MS．The target compounds’anti－influenza virusactivity experiment is being carried on．...