The Structure Modification Study On Componenet Of Coptis And Magnolia Herb Pairs

Natural active ingredients of Chinese herbal medicine has extensive pharmacological activity, it can be used as lead compounds of chemical drug for the corresponding structure modification. Berberine and magnolol are the effective components respective from Rhizoma Coptidis and Magnolia of traditional Chinese medicine. At present, we respectively study more about the structure modification of berberine and magnolol, but less about synthesis of the two together. Therefore, the purpose of this paper is to take the berberine and magnolol as the research object and explore the structure combination process, and then to seek a new pharmacodynamic activity product.With berberine hydrochloride as starting material and heating and microwave method as demethylation reaction to get berberrubine. Afterwards, Berberrubine and1,2-Dibromoethane for substitution reaction and obtain9-(2-ethyl bromide) of berberine hydrochloride. Finally,9-(2-ethyl bromide) berberine hydrochloride and magnolol for substitution reaction to get9-(2’-((5’,5’’-diallyl-2"-hydroxy-[1’,1’’-biphenyl]-2’-yl)oxy)ethoxy)-10-methoxy-5,6-dihydro-[1,3]dioxolo[4,5-g]isoquinolino[3,2-a]isoquinolin-7-ium. The Reaction products are analyzed by HPLC, IR, NMR and MS.Each suitable reaction conditions are follows:1. Demethylating reaction of Berberine:①heating method, vacuum,190℃, heating30min;②microwave method, the microwave power520W, the reactant material quantity proportional was:n (berberine hydrochloride):n (KI)=1:5, the reaction solvent was DMF, microwave reaction time was25min.2. The substitution reaction of Berbamine hydrochloride red alkali:the reactant material quantity proportional was according to cpmputational complexity, the reaction solvent was acetonitrile, refluxing.3. The substitution reaction of9-(2-ethyl bromide) berberine hydrochloride:the reactant material volume ratio was according to computational complexity, the reaction solvent was acetonitrile, the method was refluxing.This thesis is also explore the reaction conditions of the alkalization berberine and magnolol, the responses of samples and alkalization reaction have new spots which detected by TLC; The alkalify berberine reaction of magnolol, although the reaction failed to obtain the expected product, but to obtain the purity13-methyl tetrahydroberberine by the recrystallization method.After the berberine structure was modified, and then reaction with magnolol through intermediates1,2-Dibromoethane, and last obtain the target product.