- Synthetic method and medicinal preparation of sodium taurocholate
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The method comprises the following steps: S10, dissolving taurine and a base in water for salt formation reaction, drying the generated salt after the reaction is ended, and obtaining taurine sodium. S20, the taurine sodium and cholic acid are subjected to condensation reaction under 2 - ethoxy -1 - ethoxycarbonyl -1 and 2 - 80 - 120 °C dihydroquinoline, and a product solution containing sodium taurocholate is obtained. S30, sodium taurocholate in the product solution is separated and purified to obtain the sodium taurocholate product. To the method, taurine and a base are subjected to salt formation reaction to obtain sodium taurocholate, and condensation reaction is carried out, so that an existing 'one-pot' is changed into a two-step method. In addition, the synthetic method provided by the invention is simple to operate and low in cost.
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Paragraph 0084-0085
(2021/11/03)
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- Refining method of sodium taurocholate
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The invention discloses a refining method for sodium taurocholate. The method includes the following steps that a crude sodium taurocholate product is dissolved in alcoholic solvents, ester solvents are added while the alcoholic solvents are hot, after cooling, the temperature is reduced, and high-purity sodium taurocholate is obtained by vacuum drying. Compared with the prior art, the method hasthe advantages that the refining method is simple in operation, ester solvents with relatively higher boiling points are adopted to reduce solvent volatilization, thus use of acetone with irritating odor and the use of low-boiling-point ether are avoided, operation is safer, and industrial production is facilitated. The yield is high, the product purity is high and not less than 91%, the purity ofrefined sodium taurocholate is 100% through an area normalization method, the purity of HPLC is more than and equal to 99.00% through ELSD detection, the purity of HPLC can be up to 99.91%, the content of a single impurity A is smaller than 0.30%, the content of a single impurity B is smaller than 0.8%, the type of impurities is significantly reduced, and the refined final product are free of impurities C and D.
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Paragraph 0047-0068
(2019/06/12)
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- Continuous flow synthesis and scale-up of glycine- and taurine-conjugated bile salts
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A multi-gram scale protocol for the N-acyl amidation of bile acids with glycine and taurine has been successfully developed under continuous flow processing conditions. Selecting ursodeoxycholic acid (UDCA) as the model compound and N-ethoxycarbonyl-2-ethoxy-1,2-dihydroquinoline (EEDQ) as the condensing agent, a modular mesoreactor assisted flow set-up was employed to significantly speed up the optimization of the reaction conditions and the flow scale-up synthesis. The results in terms of yield, in line purification, analysis, and implemented flow set-up for the reaction optimization and large scale production are reported and discussed.
- Venturoni, Francesco,Gioiello, Antimo,Sardella, Roccaldo,Natalini, Benedetto,Pellicciari, Roberto
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experimental part
p. 4109 - 4115
(2012/06/15)
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