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Novel dopamine salt and application thereof

A technology of dopamine and sodium salt, applied in the salt and preparation of dopamine and its preparation, application in the manufacture of drugs, preparation of the above salt and its preparation, dopamine sodium salt and potassium salt field, can solve human hyperchloremia, Low safety, large drug side effects and other problems, to achieve high safety performance, avoid hyperchloremia, and improve the effect of microcirculation

Inactive Publication Date: 2018-08-14
SHANGHAI DINGYA PHARM CHEM CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0006] The technical problem to be solved by the present invention is: dopamine hydrochloride commonly used in the prior art is likely to cause hyperchloremia in human body, resulting in large side effects and low safety

Method used

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  • Novel dopamine salt and application thereof
  • Novel dopamine salt and application thereof

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Experimental program
Comparison scheme
Effect test

Embodiment 1

[0045] (1) Preparation of 1-methoxy-2-hydroxybenzaldehyde (compound 3)

[0046] Under the action of catalyst, p-hydroxybenzaldehyde (compound 1) is substituted with bromine to obtain 1-bromo-2-hydroxybenzaldehyde (compound 2); 1-bromo-2-hydroxybenzaldehyde (compound 2) is under alkaline conditions Under the substitution reaction with methanol, 1-methoxy-2-hydroxybenzaldehyde (compound 3) was obtained;

[0047] (2) Preparation of dopamine

[0048] 1-methoxy-2-hydroxybenzaldehyde (compound 3) undergoes Henry reaction under the condition of glacial acetic acid to obtain compound 4; compound 4 undergoes reduction reaction under the action of catalyst to obtain compound 5; compound 5 is prepared by heating in dilute sulfuric acid dopamine.

Embodiment 2

[0050]

[0051] Weigh the prescribed amount of water for injection, and inject carbon dioxide into the water for injection for 25 minutes to saturation; then weigh dopamine disodium salt with a mass volume ratio of 64.6 mg / mL, sodium sulfite with a mass volume ratio of 50 mg / 100 mL, and sodium sulfite with a mass volume ratio of 64.6 mg / mL. Add 5g / 100mL of D-glucose monowater into the above-mentioned saturated water with carbon dioxide, stir and dissolve; add appropriate amount of lactic acid to the above solution to adjust the pH of the solution to 3.2~4.3, then add water for injection to the full amount and stir evenly; add Filter and sterilize with activated carbon at 15-35°C, fill the filtrate after passing the inspection, and sterilize at 121°C for 15 minutes.

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Abstract

The invention belongs to the technical fields of a chemical medicine and a preparation. The invention relates to novel dopamine salt and a preparation and a preparation method and an application thereof. The dopamine salt having pharmacological activity is dopamine sodium and sylvite. The application of dopamine sodium and sylvite has the important value for preparing medicines for treating chronic intractable heart failure, occlusive vascular disease and / or extreme case. The technical problems that the common dopamine hydrochloride easily generates human hyperchloremia, the side effect of themedicine is large, and safety is low in the prior art can be solved. The invention provides dopamine sodium and sylvite injections and a preparation method thereof. The injections have the advantagesof better treatment effect and higher safety performance.

Description

technical field [0001] The invention belongs to the technical field of chemical medicines and their preparations, and relates to new dopamine salts and preparations as well as their preparation methods and applications. More specifically, the present invention relates to dopamine sodium salt and potassium salt with pharmacological activity, especially the application in the manufacture of medicine, and the present invention also relates to the preparation of the above-mentioned salt and its preparation. Background technique [0002] Dopamine hydrochloride is a well-known dopamine receptor agonist. It is suitable for shock syndrome caused by myocardial infarction, trauma, endotoxin sepsis, cardiac surgery, renal failure, congestive heart failure, etc.; It is especially suitable for shock patients with decreased urine output and supplemented blood volume, so its importance is self-evident. [0003] Dopamine hydrochloride is an endogenous catecholamine and the precursor of adr...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/137A61P9/04A61P9/00A61P9/12A61P11/06A61P15/06C07C215/52C07C213/02A61K9/08A61K47/26
CPCA61K9/0014A61K9/08A61K47/26C07C215/52
Inventor 阮诗文于楠徐丽萍于梦轩
Owner SHANGHAI DINGYA PHARM CHEM CO LTD
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