Novel 2-(alpha-hydroxyl amyl) and its preparing method and use

A technology of hydroxypentyl and benzoic acid, which is applied in the field of application, can solve the problems of undisclosed preparation methods of zinc salt diethylamine salt, etc., and achieve excellent protective effect, good preventive and therapeutic effect, and low toxicity

Inactive Publication Date: 2008-10-01
北京天衡药物研究院有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

The specification discloses the preparation of potassium salt, sodium salt, lithium salt, calcium salt, and benzylamine salt, but does not disclose the specific preparation methods of zinc salt, aniline, morpholine, and diethylamine salt

Method used

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  • Novel 2-(alpha-hydroxyl amyl) and its preparing method and use
  • Novel 2-(alpha-hydroxyl amyl) and its preparing method and use
  • Novel 2-(alpha-hydroxyl amyl) and its preparing method and use

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0030] Example 1: Preparation of 2-(α-hydroxypentyl)benzoic acid N,N'-dibenzylethylenediamine salt.

[0031] 1, the preparation of 2-(alpha-hydroxy n-pentyl) benzoic acid

[0032]

[0033] operate:

[0034] Add 80g (0.348mol) of 2-(α-hydroxypentyl)sodium benzoate (prepared according to CN1382682A) and 500ml of water into a 2.5L beaker, stir and dissolve, cool to -10°C, and add cold 5% sodium benzoate in batches Hydrochloric acid, control the internal temperature at 0 to -10°C, adjust the pH to 2 to 3, extract with 500ml×3 ether, wash the ether layer with 300ml×3 water until neutral, dry the ether layer, filter off the desiccant, and depressurize Diethyl ether was removed to obtain 64 g of white solid.

[0035] 2. Preparation of 2-(α-hydroxy n-pentyl)benzoic acid N,N'-dibenzylethylenediamine salt

[0036]

[0037] operate

[0038] (1) Add 37.2 g (0.155 mol) of N, N'-dibenzylethylenediamine and 1.0 L of diethyl ether into the reaction flask, and after fully dissolving ...

Embodiment 2

[0046] Embodiment 2: Appearance character and melting point contrast of various 2-(alpha-hydroxypentyl) benzoates

[0047] Table 1 is a comparison of appearance properties and melting points of various 2-(α-hydroxypentyl)benzoates.

[0048]

[0049] * : Prepared by CN1382682A. ** : Prepared by the calcium salt method in CN1382682A *** : Prepared according to the method of Example 1

[0050] The results showed that lithium salts, sodium salts, magnesium salts, and zinc salts were all foamy or colloidal solids without obvious melting points. Morpholine and diethylamine salts are viscous liquids. None of them meet the requirements of the pharmaceutical industry. Potassium salt, calcium salt, benzylamine salt, N,N'-dibenzylethylenediamine salt, tert-butylamine salt have good physical appearance and fixed melting point. Aniline does not react at all.

Embodiment 3

[0051] Embodiment 3: Wet Stability Comparison

[0052] According to Chinese Pharmacopoeia 2000 edition two appendix XIX C " drug stability guideline " item " high humidity test method " described method test, time is 10 days. The results are shown in Table 2.

[0053] Table Dipotassium salt, calcium salt, benzylamine salt, N, N'-dibenzylethylenediamine salt, tert-butylamine salt wet stability comparison

[0054]

[0055] * The determination of the decomposition product adopts HPLC method, according to Chinese Pharmacopoeia 2000 edition two appendix VD test, C18 column, mobile phase acetonitrile:0.02M sodium dihydrogen phosphate=40:60, detection wavelength 230nm, flow rate 1ml / min.

[0056] The experimental results show that the hygroscopicity of potassium salt and benzylamine salt is more serious, and the decomposition is serious after moisture absorption, while N, N'-dibenzylethylenediamine salt and calcium salt are less hygroscopic and stable. Tert-butylamine salt has ...

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Abstract

The present invention relates to a new 2-(alpha-hydroxyamyl) benzoate and its preparation method, and medicine composition using said compound as active component, and also relates to its application for curing cardio-cerebral ischemia and cardio-cerebral arterial infarction.

Description

technical field [0001] The present invention relates to new 2-(alpha-hydroxypentyl) benzoate and its preparation method, and the pharmaceutical composition with this compound as active ingredient, also relates to this compound in the treatment of heart and brain ischemia, cardiac artery blockage etc. aspects of application. Background technique [0002] Acute ischemic stroke, coronary heart disease, and myocardial infarction are all diseases caused by atherosclerosis until thrombosis leads to ischemic injury, which brings great pain and even life-threatening to patients. At present, research on this type of drug has always been the focus and frontier of drug research and development. [0003] Chinese patent CN1382682A, application number 01109795.7, discloses 2-(alpha-hydroxypentyl) benzoate and its preparation method and application for the first time, relates to the salt of monovalent metal ion, divalent metal ion and organic base, specifically discloses Salts of potassi...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): C07C65/01C07C51/41A61K31/19A61K9/16A61K9/20A61K9/48A61P9/10C07C51/00C07C65/03
CPCA61K9/16A61K31/19C07C211/27A61P9/10
Inventor 杨文斌秦华赵兴凯马喜生
Owner 北京天衡药物研究院有限公司
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