Study On The Synthesis Technology And Industrial Design Of TUDCA

Tauroursodeoxycholic acid(TUDCA) is a kind of bile acid drugs. It has many physiological functions such as dissolved cholesterol stone and protective liver cell and so on.Based on the relevant literature and the analysis of the principle of reactions, several synthesis routes are collected and the synthesis route that is suitable for industrial production is selected. In this paper, the TUDCA was synthesized by aminolysis of sodium taurine with carboxy-carbonate mixed anhydride prepared by reacting UDCA with phenyl chloroformate at the present of triethylamine. substitution. The influences of anhydride reaction and aminolysis reaction were investigated in molar ratio, temperature, time and so on. on. Optimum reaction conditions were selectred as follows:1 equivalent UDCA dissolved in four times,in the size of the quality, tetrahydrofuran. Then joined 1.5 equivalent of triethylamine.1.5 equivalent of the chlorine acid benzene ester was droped in the solution should be keeped at 0-5℃. This solution was keeped in 10℃for 60-80min,then filter. The filtrate under 5℃droped join 2 equivalent of taurine sodium aqueous solution(1.27mol/L), then keeped in 15℃for 100-160min. The alkaline liquor was acidize by hydrochloric acid. The absolute ethyl alcohol dissolve the residue that get by moved water in reduced pressure distillation. After filter, the ethyl alcohol was moved out from filtrate in reduced pressure distillation. According to the conditions described,TUDCA yields 75%.Based on the results of experiments, the rational scheme for the renovating of the process was discussed. The technological process,operational approach material recycling etc. were designed. It provided the theoretical basis and process parameters for the industrial production of TUDCA.