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Genipin derivative with uric acid transport promoting activity and preparation method thereof

A technology of genipin and its derivatives, which is applied in the field of genipin derivatives with the activity of promoting uric acid transport and its preparation, which can solve the problems of high mortality, increased uric acid excretion rate, and reduced reabsorption, etc.

Active Publication Date: 2020-08-11
INST OF AGRO FOOD SCI & TECH SHANDONG ACAD OF AGRI SCI
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0003] Uric acid transporter 1 (URAT1), organic anion transporter 1 (OAT1), and glucose transporter 9 (GLUT9) are important transporters involved in uric acid excretion in the kidney Body protein, these transporters have a remarkable effect on the regulation of uric acid excretion, and are usually an important target for drug treatment of hyperuricemia. Benzbromarone, which was approved for marketing in 1976, is a derivative of benzofuran, which can effectively inhibit the excretion of uric acid. The expression level of URAT1 and GLUT9 protein, thereby reducing the reabsorption of urate and glucose, the excretion rate of uric acid in the kidney is significantly increased, and the concentration of serum uric acid in the body is significantly decreased, so it is widely used in clinical use. With the development of benzbromarone Long-term use, clinical data have found that benzbromarone can have adverse effects on the liver, especially in patients with previous liver disease or alcohol drinking history, the risk of liver toxicity is significantly increased, resulting in great mortality. Therefore, we propose a drug with Genipin derivatives promoting uric acid transport activity and preparation method thereof

Method used

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  • Genipin derivative with uric acid transport promoting activity and preparation method thereof
  • Genipin derivative with uric acid transport promoting activity and preparation method thereof
  • Genipin derivative with uric acid transport promoting activity and preparation method thereof

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Embodiment 1

[0030] refer to Figure 1-2 , a genipin derivative with uric acid transport promoting activity, comprising the following components: geniposide, sulfuric acid, methanol, dichloromethane, triethylamine and p-toluenesulfonyl chloride.

[0031] A preparation method of a genipin derivative having the activity of promoting uric acid transport, adopting the following steps:

[0032] S1, adding geniposide into a round bottom flask, dissolving sulfuric acid in methanol, adding the methanol solution of the acid into the round bottom flask to reflux for alcoholysis reaction to obtain a reaction solution, and tracking the reaction process by TLC;

[0033] S2, neutralizing the reaction solution after the reaction in step S1 to neutrality, then extracting the reaction solution, merging the organic phases, and then evaporating to dryness to obtain genipin methyl;

[0034] S3, adding genipin methyl into a round bottom flask and dissolving it with dichloromethane, and adding triethylamine an...

Embodiment 2

[0051] refer to Figure 1-2 , a genipin derivative with uric acid transport promoting activity, comprising the following components: geniposide, sulfuric acid, methanol, dichloromethane, triethylamine and p-toluenesulfonyl chloride.

[0052] A preparation method of a genipin derivative having the activity of promoting uric acid transport, adopting the following steps:

[0053] S1, adding geniposide into a round bottom flask, dissolving sulfuric acid in methanol, adding the methanol solution of the acid into the round bottom flask to reflux for alcoholysis reaction to obtain a reaction solution, and tracking the reaction process by TLC;

[0054] S2, neutralizing the reaction solution after the reaction in step S1 to neutrality, then extracting the reaction solution, merging the organic phases, and then evaporating to dryness to obtain genipin methyl;

[0055] S3, adding genipin methyl into a round bottom flask and dissolving it with dichloromethane, and adding triethylamine an...

Embodiment 3

[0072] refer to Figure 1-2 , a genipin derivative with uric acid transport promoting activity, comprising the following components: geniposide, sulfuric acid, methanol, dichloromethane, triethylamine and p-toluenesulfonyl chloride.

[0073] A preparation method of a genipin derivative having the activity of promoting uric acid transport, adopting the following steps:

[0074] S1, adding geniposide into a round bottom flask, dissolving sulfuric acid in methanol, adding the methanol solution of the acid into the round bottom flask to reflux for alcoholysis reaction to obtain a reaction solution, and tracking the reaction process by TLC;

[0075] S2, neutralizing the reaction solution after the reaction in step S1 to neutrality, then extracting the reaction solution, merging the organic phases, and then evaporating to dryness to obtain genipin methyl;

[0076] S3, adding genipin methyl into a round bottom flask and dissolving it with dichloromethane, and adding triethylamine an...

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Abstract

The invention discloses a genipin derivative with uric acid transport promoting activity and a preparation method, and belongs to the field of genipin derivative preparation. The genipin derivative with uric acid transport promoting activity comprises geniposide, sulfuric acid, methanol, dichloromethane, triethylamine and p-toluenesulfonyl chloride. According to the invention, a novel methyl genipin derivative is synthesized, has an activity effect of promoting uric acid transport, and is subjected to corresponding biological activity detection; according to the invention, the biological activity of genipin is improved by carrying out structural modification on genipin, and the invention has important practical significance for researching and developing a novel drug for promoting uric acid transport; according to the genipin derivative capable of promoting uric acid transport, geniposide is used as a raw material for related structural modification, the synthesis method is simple, theprice of the raw material is low, and the structure is novel.

Description

technical field [0001] The invention relates to the technical field of preparation of genipin derivatives, in particular to a genipin derivative with the activity of promoting uric acid transport and a preparation method. Background technique [0002] Hyperuricemia is a disease caused by the disorder of purine metabolism in the body. In recent years, the incidence has been increasing year by year, becoming the second largest metabolic disease after diabetes. Complications, such as gout, chronic kidney disease, etc., seriously threaten human health. The kidney is the most important organ for uric acid excretion, and the kidney's processing of uric acid is very complicated and precise. The excretion of uric acid in the kidney can be roughly simplified Summarized into four processes of glomerular filtration, renal tubular reabsorption, secretion and post-secretion reabsorption, in which uric acid can be completely filtered in the glomerulus, and then almost all of the uric acid...

Claims

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Application Information

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IPC IPC(8): C07D311/94A61P19/06
CPCC07D311/94A61P19/06Y02P20/55
Inventor 刘超孙金月王目旋张瑞瑞王新坤郭溆王青
Owner INST OF AGRO FOOD SCI & TECH SHANDONG ACAD OF AGRI SCI
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