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Synthesizing method of single-configuration rabeprazole metabolite

A technology of rabeprazole and a synthesis method, which is applied in the field of drug metabolism to achieve the effects of reasonable process design, strong operability, and great application research value

Active Publication Date: 2016-07-27
TLC NANJING PHARMA RANDD CO LTD
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  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Benefits of technology

This patented describes an improved way to make certain chemical compounds called rhenium (Re) which have specific properties such as being able to break down into different forms like hydrogen gas or metal salt. These new compositions may find use in various applications where they could improve their performance over existing ones without affecting them significantly.

Problems solved by technology

The technical problem addressed in this patents relating to improving the effectiveness of chemotherapy treatments involving ruler's disease caused by excessive stomach acid production (GARA).

Method used

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  • Synthesizing method of single-configuration rabeprazole metabolite
  • Synthesizing method of single-configuration rabeprazole metabolite
  • Synthesizing method of single-configuration rabeprazole metabolite

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Embodiment 1

[0032] The preparation of the rabeprazole metabolite of the single configuration of embodiment 1 specifically comprises the following steps:

[0033] like figure 1 Shown is the reaction flow diagram of the present invention:

[0034] (1) Take rabeprazole sulfide (I) (20g) and suspend it in hydrobromic acid (300mL) with a volume concentration of 48%, heat to 100 degrees, react for 1 hour, cool the reaction solution to room temperature, and then Under the bath, slowly add water and ethyl acetate to the reaction solution, adjust the pH to 9-10 with 25% volume concentration of ammonia water, a large amount of white solid precipitates, filter to obtain desmethyl rabeprazole sulfide (II) Crude product 20g, obtain 11g desmethyl rabeprazole sulfide (II) intermediate after column chromatography purification;

[0035]

[0036] (2) Suspend the intermediate (II) (20g) in 200mL of dichloromethane, add imidazole (12.4g) and tert-butyldimethylsilyl chloride (12g) successively, after the...

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Abstract

The invention discloses a synthesizing method of a single-configuration rabeprazole metabolite.According to the method, rabeprazole thioether serves as a starting material, and the rabeprazole metabolite is synthesized through a five-step reaction.The optimal preparation steps and reaction conditions are screened out through a large number of experiments, the whole technological design is reasonable, and the operability is high.According to the obtained single-configuration rabeprazole metabolite, the chemical purity can reach 99% or above, and the chiral purity is larger than 99.5%.The obtained single-configuration rabeprazole metabolite provides a standard substance for metabolic mechanism research of a rabeprazole drug, can be used for exploring the metabolic process of the drug in organisms and has a great application research value in clinical pharmacokinetic research.

Description

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Claims

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Application Information

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Owner TLC NANJING PHARMA RANDD CO LTD
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