Medicine for treating myocardial ischemia and preparation method thereof

A pharmacy and prodrug technology, applied in the field of medicine, can solve the problems of adverse reactions, uncertain curative effect, and high dependence on individual physique of patients, and achieve the effects of outstanding drug efficacy, reduction of myocardial infarction area, and high product yield.

Pending Publication Date: 2022-04-15
HEILONGJIANG UNIV OF CHINESE MEDICINE
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

There are many kinds of anti-myocardial ischemic drugs in clinical use, commonly used include nitrates, β-receptor blockers and myocardial metabolism drugs, etc., but these drugs often cause some adverse reactions in the treatment
In addition, Danshen preparation, compound ginkgo preparation, Suxiao Jiuxin pill and other Chinese patent medicines are often used to treat myocardial ischemic diseases. Although they have a certain therapeutic effect, they depend on the individual physique of the patient, and there are uncertain results in the treatment.

Method used

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  • Medicine for treating myocardial ischemia and preparation method thereof
  • Medicine for treating myocardial ischemia and preparation method thereof
  • Medicine for treating myocardial ischemia and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

preparation example Construction

[0081] In the fifth aspect of the present invention, the present invention also provides the preparation method of the compound of formula I of the present invention, which comprises the following steps:

[0082]

[0083] Step 1: the compound of formula II reacts with the compound of formula III to generate the intermediate compound of formula IV;

[0084] Step 2: the intermediate compound of formula IV reacts with the compound of formula V to generate the compound of formula I;

[0085] Among them, X a 、X b Each independently represents halogen, preferably chlorine or bromine;

[0086] X, R 1 -R 9 , L, Y are as defined herein.

[0087] Preferably, step 1 is carried out under the action of a base; preferably, the base is selected from organic bases, especially triethylamine and pyridine.

[0088] Preferably, step 2 is carried out in the presence of cuprous salts, ligands, and alkalis; preferably, the cuprous salts are selected from cuprous bromide and cuprous iodide; ...

Embodiment 1

[0091] Embodiment 1: the preparation of compound 1

[0092]

[0093] Preparation of intermediate IV-1: under nitrogen protection, compound II-1 (7.11g, 30mmol) was dissolved in toluene (120ml), triethylamine (21ml) was added, compound III-1 (3.42g, 30mmol ) dissolved in toluene (50ml); then heated to 95 ° C for 2 hours. After cooling down to normal temperature, wash the reaction solution with water for several times, evaporate the solvent under reduced pressure, add chloroform to dissolve, filter and wash with saturated saline and water for several times, dry the organic phase with anhydrous sodium sulfate, and evaporate under reduced pressure The solvent was recrystallized with ethanol / diethyl ether (volume ratio 4:1), and dried to obtain 6.12 g of intermediate IV-1 with a yield of 75.6%. ESI-MS: 271.2[M+H] + .

[0094] Preparation of compound 1: under nitrogen protection, intermediate IV-1 (4.05g, 15mmol), compound V-1 (2.38g, 15mmol), cuprous iodide (0.95g, 5mmol), ce...

Embodiment 2

[0098] Embodiment 2: the preparation of compound 2

[0099]

[0100] According to the same preparation method as in Example 1, compound II-1 was replaced by equimolar II-2, and intermediate IV-1 was replaced by equimolar IV-2 to obtain compound 2 (4.30g), HPLC purity≧98.9 %.

[0101] ESI-MS: 386.2[M+H] + .

[0102] Elemental analysis: theoretical element content (%) C 18 h 16 FN 5 o 4 : C, 56.10; H, 4.19; N, 18.17; Measured element content (%): C, 56.13; H, 4.22; N, 18.15.

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Abstract

The invention relates to a medicine for treating myocardial ischemia and a preparation method thereof, the medicine is a compound with a structure as shown in a formula I. The medicine can effectively reduce the myocardial infarction area after myocardial infarction and can also remarkably reduce the activity of serum CK, AST and LDH. The compound is easy to prepare, low in raw material cost, high in product yield, outstanding in drug effect and suitable for being applied to prevention and treatment of myocardial ischemia in the industry.

Description

technical field [0001] The invention relates to the field of medicine, in particular, the invention relates to a medicine for treating myocardial ischemia, and also relates to a preparation method of the medicine. Background technique [0002] Myocardial ischemia refers to a pathological state in which the blood perfusion of the heart is reduced, resulting in reduced oxygen supply to the heart, abnormal myocardial energy metabolism, and failure to maintain the normal work of the heart. Clinically, it is mainly characterized by chest tightness and precordial pain. feature. Causes such as coronary artery obstruction, decreased aortic blood supply, and decreased blood pressure can all directly lead to reduced cardiac blood supply; heart valve disease, changes in blood viscosity, and myocardial disease can also lead to reduced cardiac blood supply. [0003] The basic cause of myocardial ischemia is that the oxygen supply capacity of the coronary blood flow is insufficient to me...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07D413/14A61K31/536A61P9/10A61K45/06
Inventor 陈会君胡妮娜
Owner HEILONGJIANG UNIV OF CHINESE MEDICINE
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