Racecadotril compound and novel preparation method thereof

A technology of racecadotril and compounds, which is applied in the field of medicine, can solve the problems of enhanced color, reduced content of active ingredients in medicines, and low yield of racecadotril, and achieves improved product quality, mild reaction conditions, and reduced toxicity. side effects

Inactive Publication Date: 2011-06-15
HAINAN MEIDA PHARMA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, the yield of racecadotril prepared by the above-mentioned method is very low, and the purity of the final product obtained is also low, which is not suitable for suitability for industrialized production
[0010] In addition, when the cadotril compound is improperly stored or stored for too long, it will lead to a decrease in the content of the active ingredients of t

Method used

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  • Racecadotril compound and novel preparation method thereof
  • Racecadotril compound and novel preparation method thereof
  • Racecadotril compound and novel preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0038] Dissolve 5 g of racecadotril (purity: 97.3%) in 100 ml of ethanol-ethyl acetate (1:5) and add it to the top of the column. The filler is ICN allumina N with a particle size of 18-32 μm and a pore size of 6 nm. permanent alumina. The length of the column is 25cm, the diameter is 5cm, and the column pressure is 0.5pa. Then, ethanol:ethyl acetate (1:5) is pumped into the column for column chromatography. , collected in sections, collected the liquid, and dried in vacuum to obtain 4.7 g of refined racecadotril, with a yield of 96.7% and a purity of 99.7%.

Embodiment 2

[0040] Dissolve 10 g of racecadotril crude product (purity: 96.2%) in 200 ml of ethanol-ethyl acetate (1:9) and add to the top of the column. The filler is ICN allumina N with a particle size of 18-32 μm and a pore size of 6 nm. Fine-pored neutral alumina. The length of the column is 25cm, the diameter is 5cm, the column pressure is 5.0pa, and then pumped into ethanol-ethyl acetate (1:9) for column chromatography, the flow rate is 2.0ml / min, the column temperature is kept at 45°C, start timing, sampling, and follow-up monitoring , collected in sections, collected the liquid, and dried in vacuum to obtain 9.2 g of refined racecadotril, with a yield of 95.6% and a purity of 99.8%.

Embodiment 3

[0042] Dissolve 15 g of racecadotril crude product (purity: 98.0%) in 200 ml of ethanol-ethyl acetate (1:1) and add to the top of the column. The filler is Baker pores with a particle size of 50-200 μm and a pore size of 6 nm permanent alumina. The length of the column is 25cm, the diameter is 5cm, the column pressure is 1.5pa, and then pumped into ethanol-ethyl acetate (1:1) for column chromatography, the flow rate is 1.5ml / min, the column temperature is kept at 40°C, start timing, sampling, and follow-up monitoring , collected in sections, collected the liquid, and dried in vacuum to obtain 14.0 g of refined racecadotril, with a yield of 95.2% and a purity of 99.7%.

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Abstract

The invention relates to a racecadotril compound and a novel preparation method thereof. In particular, neutral alumina with a specific size is taken as a fixed phase, a mixed solvent consisting of ethanol and ethyl acetate according to a certain proportion is taken as a mobile phase, and a column temperature is kept higher than the room temperature, so that racecadotril can be refined and purified efficiently, high yield and high purity are achieved, and the method is an effective method for obtaining high-purity racecadotril. By the racecadotril obtained by the method, the product quality of a preparation is enhanced, and the clinical toxic and side effects of the racecadotril compound on the preparation of antidiarrheic medicaments are reduced.

Description

technical field [0001] The invention relates to a method for refining a compound, in particular to a method for refining a racecadotril compound, and belongs to the technical field of medicines. Background technique [0002] Racecadotril (Racecadotril), which belongs to antidiarrheal medicine, was developed and created by French Bioproject Company. It was first listed in France under the trade name Tiorfan in 1993, and was listed on the international market in 1997. The chemical name is [(R, S)]-N-(2-acetylthiomethyl-1-oxo-3-phenylpropyl)glycine benzyl ester, the molecular formula is C 21 h 23 NO 4 S, the structural formula is: [0003] [0004] Currently, oral preparations for the treatment of diarrhea mainly include oral rehydration solutions and anti-peristaltic drugs. The use of oral rehydration solutions to replenish water and electrolyte depletion is the main means of antidiarrheal treatment today, but they enhance absorption without inhibiting secretion, and th...

Claims

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Application Information

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IPC IPC(8): C07C327/32A61K31/265A61P1/12
Inventor 廖爱国
Owner HAINAN MEIDA PHARMA
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