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Beta (3,4-dihydroxyphenyl)-alpha-hydroxyisopropyl propionate and its synthesis

A technology of isopropyl hydroxypropionate and dihydroxyphenyl, which is applied in the field of new drug β--α-hydroxypropionate isopropyl for preventing and treating cardiovascular and cerebrovascular diseases and the field of synthesis thereof, and can solve the problem of inability to express at the molecular level, lack of It can study the structure of metabolites, the clinical efficacy of metabolic mechanism and other issues, so as to reduce the incidence, relieve symptoms, and strengthen the expansion of blood vessels.

Inactive Publication Date: 2005-02-23
NORTHWEST UNIV
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Problems solved by technology

At present, it is generally believed that Danshensu is the active ingredient in Danshen, but the existing literature only studies its pharmacology and efficacy from the perspective of clinical observation and animal experiments, but fails to express it at the molecular level. In terms of pharmacokinetics research It also only gives the relationship curve and parameters of its blood drug concentration, but fails to discuss the structure, metabolic mechanism and corresponding clinical efficacy of the main metabolites.

Method used

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  • Beta (3,4-dihydroxyphenyl)-alpha-hydroxyisopropyl propionate and its synthesis
  • Beta (3,4-dihydroxyphenyl)-alpha-hydroxyisopropyl propionate and its synthesis
  • Beta (3,4-dihydroxyphenyl)-alpha-hydroxyisopropyl propionate and its synthesis

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Embodiment Construction

[0016] Below in conjunction with accompanying drawing and pharmacodynamics test report the present invention is described in further detail.

[0017] Metabolites of Salvia miltiorrhiza in serum by figure 1 As shown in the flow diagram, it is first enriched and removed in the pre-column, and then recoiled into the analytical column for separation. figure 2 These two types of compounds were synthesized by the synthetic route shown, and prepared into solutions for mass spectrometry analysis to further confirm the structure of the main metabolites.

[0018] β-(3,4-dihydroxyphenyl)-alpha-hydroxypropionic acid isopropyl ester synthetic method (see image 3 ).

[0019] (1) Synthesis of acetylglycine:

[0020] Weigh 15 grams of aminoacetic acid (glycine), put it in a 400 ml beaker, add 60 ml of distilled water, stir to dissolve slightly, cool to room temperature, add 43 grams of acetic anhydride, cool to room temperature, put it in the refrigerator overnight, and filter it to obta...

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Abstract

The invention relates to effective components of root of red-rooted salvia to treat disease and its chemical structure and synthesize technique. It is used to treat heart and blood vessel of brain diseases. Filter the main metabolite-beta(-3,4- dihydric phenyl)-alpha hydric propionic acid isopropyl ester in human blood serum after taking medicine. The purity is 98.0%. The results demonstrate the medicine to have varies function in blood vessel dilatation, anti cerebral ischemia, oxidation resisting in vitro, and protect heart and brain and remission the diabetes caused miocardial infarction.

Description

technical field [0001] The invention belongs to the field of medicine and health, and relates to a medicine, in particular to a new medicine β-(3,4-dihydroxyphenyl)-α-hydroxypropionate isopropyl ester for preventing and treating cardiovascular and cerebrovascular diseases and its synthesis method . Background technique [0002] Salvia miltiorrhiza is a traditional Chinese medicine compound preparation with clear curative effect for treating cardiovascular and cerebrovascular diseases, but the active ingredients and structure that really play a therapeutic effect have not been clarified. At present, it is generally believed that Danshensu is the active ingredient in Danshen, but the existing literature only studies its pharmacology and efficacy from the perspective of clinical observation and animal experiments, but fails to express it at the molecular level. In terms of pharmacokinetics research It also only gives the relationship curve and parameters of its blood drug conc...

Claims

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Application Information

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IPC IPC(8): A61K31/216A61P9/00C07C69/732
Inventor 郑晓晖张延长王世祥赵新锋
Owner NORTHWEST UNIV
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