Amplification Of Tetrahydroberberine And Its Derivatives From The Rhizoma Coptidis

Coptis alkaloids are alkaline compounds which it contains nitrogen with similar structure of isoquinoline.It is the main ingredients of Coptids Rhizoma and it contains berberine, coptisine and palmatine. according to the Alkaloids unified alkalescent chemical properties,This experiment extracted Coptis alkaloids from The Coptids Rhizoma, use the mechanism which formed by an acid solution can impact of the Alkaloids can melt in water and which drop of a alkaline can be precipitate. It was utilized to investigate the influence of the pH and the concentration of NaOH on the yield of alkaloids. The obtained optimum conditions:pH=10; the concentration of NaOH 30%. The optimum conditions for synthesis of tetrohydroberberine is hydrogenation,demethylene-dioxy or demethylation. The condition for synthesis of tetrohydroberberine:the concentration of ethanol 90%; weight ratio of NaBH4 to raw material 0.6:1; weight ratio of catalyst K2CO3 to raw material 3:1 molar ratio of AICl3 to raw material 6:1 and reaction time 5 h. The coptisine and palmatine were synthesized from the tetrohydroberberine by reactions:methylation, cyclization and oxidation. The condition for synthesis of tetrohydroberberine:molar ratio of CH3I to raw material 6:1, reaction temperature 80 ℃ and reaction time 8 h. The condition for synthesis of palmatine:weight ratio of catalyst CHsCOONato raw material 3:1, molar ratio of I to raw material 4:1. The condition for synthesis of coptisine:return temperature 120℃, molar ratio of CH2BrCl to raw material 6:1, molar ratio of CsF to raw material 10:1, molar ratio of I to raw material 4:1. The structures were confirmed by UV, IR,1H-NMR and ESI-MS.