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Synthesis method of sodium taurocholate and pharmaceutical preparation

The technology of a sodium taurocholate and a synthesis method is applied in the synthesis method of sodium taurocholate and the field of pharmaceutical preparations, and can solve the problems of low purity and strong water absorption of sodium taurocholate, and achieves easy separation and purification, low cost Low, high yield and purity effects

Active Publication Date: 2021-11-02
WUHAN POLYTECHNIC UNIVERSITY
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  • Description
  • Claims
  • Application Information

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Problems solved by technology

The specific operation is as follows: triethylamine, EEDQ, cholic acid and taurine are "cooked in one pot" in a solution of dimethylformamide as a medium, and after cumbersome separation methods, taurocholic acid with a fair yield is obtained. Sodium, but the water absorption of the by-product triethylamine taurocholate formed by this method is too strong, it is difficult to separate it from sodium taurocholate, so that the product sodium taurocholate obtained has a lower purity

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  • Synthesis method of sodium taurocholate and pharmaceutical preparation
  • Synthesis method of sodium taurocholate and pharmaceutical preparation
  • Synthesis method of sodium taurocholate and pharmaceutical preparation

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preparation example Construction

[0038] see figure 1 , in the present embodiment, the synthetic method of sodium taurocholate comprises the following steps:

[0039] Step S10, respectively dissolving taurine and alkali in water for a salt-forming reaction, and drying the generated salt after the reaction to obtain sodium taurine;

[0040] In order to make the reaction between the taurine and the base more sufficient, in this embodiment, the molar ratio of the taurine to the base is 1: (0.9-1.1). Preferably, the molar ratio of taurine to alkali is 1:1. It should be noted that the present invention does not limit the order of adding taurine and alkali, which can be dissolved in water first, taurine can be dissolved in water first, or can be added and dissolved at the same time.

[0041] Wherein, described alkali comprises any one in sodium carbonate, sodium bicarbonate and sodium hydroxide, to generate sodium taurate with described taurine reaction, present embodiment is preferably sodium hydroxide, and its r...

Embodiment 1

[0069] (1) Place 200ml of purified water in a 500ml three-necked bottle equipped with a stirrer, a condenser and a dropping funnel, start the stirrer, add 2g (0.5mol) NaOH, and then add 62.5g (0.5mol) NaOH after completely dissolving For sulfonic acid, stir and react at 40-100°C for about 30 minutes. After the reaction is complete, control the temperature below 100°C and distill to dryness at a vacuum of -0.085Mpa to obtain white sodium taurine, which is crushed for later use.

[0070] (2) Add 500ml DMF to a 1000ml three-necked flask equipped with a stirrer and a condenser, then add 204g (0.5mol) cholic acid and 140.1g (0.57mol) EEDQ, heat up to 60°C and react for 30min to obtain a mixed Solution A, then gradually add the sodium taurine salt obtained in step (1) to it, after the addition is completed, heat to 100°C and stir for 6 hours to react, wait until the sodium taurate completely enters the solution, stop the reaction, and obtain sodium taurocholate product solution.

...

Embodiment 2

[0073] (1) Place 200ml of purified water in a 500ml three-necked bottle equipped with a stirrer, a condenser and a dropping funnel, start the stirrer, add 2g (0.5mol) NaOH, and add 56.25g (0.45mol) of NaOH after completely dissolving For sulfonic acid, stir and react at 40-100°C for about 30 minutes. After the reaction is complete, control the temperature below 100°C and distill to dryness at a vacuum of -0.085Mpa to obtain white sodium taurine, which is crushed for later use.

[0074] (2) Add 500ml of DEF to a 1000ml three-necked flask equipped with a stirrer and a condenser, then add 183.6g (0.45mol) of cholic acid and 121.6g (0.495mol) of EEDQ, heat up to 80°C and react for 20min to obtain Mix solution A, then gradually add the sodium taurine salt obtained in step (1) to it, after the addition is completed, heat to 80°C and stir for 8 hours to react, wait until sodium taurate completely enters the solution, stop the reaction, and obtain taurocholic acid containing Sodium pr...

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Abstract

The invention discloses a synthesis method of sodium taurocholate, which comprises: S10, respectively dissolving taurine and alkali in water to carry out a salt forming reaction, and drying the generated salt after the reaction is completed to obtain sodium taurate; S20, carrying out a condensation reaction on the sodium taurate and cholic acid under the action of 2-ethoxy-1-ethoxycarbonyl-1, 2-dihydroquinoline at the temperature of 80 to 120 DEG C, so as to obtain a product solution with sodium taurocholate; and S30, seperating out sodium taurocholate in the product solution and purifying, and obtaining a sodium taurocholate product is obtained. According to the method, the taurine and the alkali are subjected to the salt forming reaction to obtain the sodium taurocholate, and then the condensation reaction is performed, so that the existing one-pot boiling is changed into a two-step method, the prepared target product is easy to separate and purify, and the finally obtained sodium taurocholate is relatively high in yield and purity. In addition, the synthesis method provided by the invention is simple to operate and relatively low in cost.

Description

technical field [0001] The invention relates to the technical field of pharmaceutical compounds, in particular to a method for synthesizing sodium taurocholate and pharmaceutical preparations. Background technique [0002] Sodium taurocholate (TCANa) widely exists in the bile of vertebrates such as cattle, sheep, and snakes, and it is also the main bile acid of snake gall. Sodium taurocholate is a combined bile acid formed by linking the carboxyl group of cholic acid (CA) and the amino group of taurine through an amide bond. It is extremely difficult to directly extract sodium taurocholate from bile, and it is currently mainly obtained through synthesis. [0003] The commonly used synthetic method is the EEDQ method at present, and its synthetic steps are: take triethylamine as base, and adopt taurine and cholic acid in 2-ethoxyl-1-ethoxycarbonyl-1,2-dihydroquinone Phyline (EEDQ) was used as a condensation agent to prepare sodium taurocholate. The specific operation is as...

Claims

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Application Information

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IPC IPC(8): C07J41/00A61K31/575A61P11/14A61P11/10A61P11/06A61P29/00A61P31/00
CPCC07J41/0061A61K31/575A61P11/14A61P11/10A61P11/06A61P29/00A61P31/00
Inventor 赵静国刘子源徐凌云
Owner WUHAN POLYTECHNIC UNIVERSITY
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