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Chlorpheniramine maleate crystal form preparation method

A chlorpheniramine acid crystal form and a technology for chlorpheniramine acid, which are applied in the field of pharmaceutical synthesis, can solve problems such as waste of raw materials, poor atom economy, excessive chlorpheniramine, etc., and achieve process stability and good impurity removal effect. , the effect of high purity

Pending Publication Date: 2021-12-03
NINGBO MENOVO PHARMA +1
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

From the perspective of material proportioning, this method has a relatively excessive amount of chlorpheniramine, and the atom economy of forming a salt is not good, and there is a certain waste of raw materials, which directly affects the production cost of the product.

Method used

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  • Chlorpheniramine maleate crystal form preparation method
  • Chlorpheniramine maleate crystal form preparation method
  • Chlorpheniramine maleate crystal form preparation method

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0024] Add 10g (1.0eq) of chlorpheniramine and 20mL of absolute ethanol to the three-necked flask, heat to 55°C, add 4.3g (1.02eq) of maleic acid, stir to dissolve, gradually cool down, and dropwise add 70mL of normal Heptane, after dropping, gradually cool down to 0-5°C, filter and dry to obtain 13.9g of chlorpheniramine maleate finished product. (White crystals, molar yield 98%).

[0025] Chlorpheniramine maleate finished product crystal, use Cu-Ka radiation to carry out X-ray powder diffraction to obtain such as figure 1 The XRD pattern shown, the XRD data are shown below.

[0026]

[0027]

Embodiment 2

[0029] Add 10g (1.0eq) of chlorpheniramine and 30mL of isopropanol to the three-necked flask, heat to 55°C, add 4.3g (1.02eq) of maleic acid, stir to dissolve, gradually cool down, and dropwise add 30mL of Heptane, after dropping, gradually cool down to 0-5°C, filter and dry to obtain 13.6g of chlorpheniramine maleate finished product. (White crystals, molar yield 96%).

Embodiment 3

[0031] Add 10g (1.0eq) of chlorpheniramine and 30mL of absolute ethanol to the three-necked flask, heat to 55°C, add 4.3g (1.02eq) of maleic acid, stir to dissolve, gradually cool down, and dropwise add 30mL of normal Heptane, after dropping, gradually cool down to 0-5°C, filter and dry to obtain 13.5g of chlorpheniramine maleate finished product. (White crystals, molar yield 95%).

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Abstract

The invention discloses a chlorpheniramine maleate crystal form preparation method which is different from an existing crystal form preparation method, wherein two solvents are used in the crystallization process, the impurity content in a finished product is effectively reduced, the yield and the purity are improved, the crystal form is stable, the crystal form cannot be changed due to the change of the solvent proportion, and industrial production is facilitated.

Description

technical field [0001] The invention relates to the field of medicine synthesis, in particular to a synthesis method of chlorpheniramine maleate crystal form. Background technique [0002] Chlorpheniramine maleate (English name Chlorpheniramine maleate, chemical name 1-p-chlorophenyl-1-(2-pyridyl)-3-dimethylaminopropane maleate, structural formula as shown below) The first generation of histamine (H1) receptor antagonists, which were first launched in the United States in 1978, can selectively block the action of histamine and produce antihistamine effects, thereby resisting telangiectasia caused by allergic reactions and reducing blood pressure. The permeability of capillaries can relieve the wheezing caused by the contraction of bronchial smooth muscle. It is often used for urticaria, vasodilation rhinitis, colds, asthma, rhinitis, contact dermatitis, and also for allergies and insect bites caused by drugs and food. And motion sickness etc. [0003] [0004] Chlorphen...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07D213/38C07C51/43C07C57/145
CPCC07D213/38C07C57/145C07B2200/13
Inventor 张晓霞唐雪松杨蜂李顺兴龙少波黄想亮孔叶青
Owner NINGBO MENOVO PHARMA