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Preparation method of chlorpheniramine maleate

A technology of chlorpheniramine and chlorophenylacetonitrile, which is applied in the field of drug synthesis and can solve the problems of high equipment requirements and harsh conditions

Active Publication Date: 2020-10-09
CHENGDU JIANJIANG PHARMA FACTORY
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0006] However, the synthesis needs to be carried out under high temperature and high pressure, the conditions are relatively harsh, and the requirements for equipment are high

Method used

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  • Preparation method of chlorpheniramine maleate
  • Preparation method of chlorpheniramine maleate

Examples

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Embodiment 1

[0033] Example 1. Method for synthesizing chlorpheniramine and chlorpheniramine maleate of the present invention

[0034] According to the following synthetic route, chlorpheniramine and chlorpheniramine maleate were prepared.

[0035]

[0036] (1) Preparation of Intermediate 1

[0037] Add 200 g of p-chlorobenzeneacetonitrile, 100 g of 2-chloropyridine, and 600 ml of toluene into the reaction flask, cool with ice water to 15° C., add 51.5 g of sodium amide, and react at room temperature for 2 to 5 hours after the addition. TLC monitors that the reaction is complete.

[0038] The reaction was quenched by adding water to the reaction solution, the aqueous layer was separated, the organic layer was washed with 200 ml of brine, and the organic phase was concentrated to obtain 190 g of intermediate 1 oil with a yield of 95%.

[0039] (2) Preparation of Intermediate 2

[0040] 2.1 Preparation of dimethylamino chloroethane solution:

[0041] Weigh 95g of 2-dimethylaminochloroethane hydrochlorid...

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Abstract

The invention provides a chlorpheniramine preparation method, which comprises: (1) reacting p-chlorophenylacetonitrile and 2-chloropyridine to obtain an intermediate 1; (2) reacting the intermediate 1with 2-dimethylaminochloroethane to obtain an intermediate 2; and (3) reacting the intermediate 2 with an alkali to obtain chlorpheniramine. The invention further provides a preparation method of chlorpheniramine maleate. The methods are short in synthetic route, easily available in raw materials and low in cost; the total yield is high, and the product quality is controllable; reaction conditions are mild, requirements on equipment are low, and industrial production is facilitated.

Description

Technical field [0001] The invention belongs to the technical field of drug synthesis, and specifically relates to a preparation method of chlorpheniramine and chlorpheniramine maleate. Background technique [0002] Chlorphenamine maleate, English name: Chlorphenamine maleate, chemical name: 2-[p-chloro-a-[2-(dimethylamino)ethyl]phenyl]pyridine maleate Molecular formula: C16H19ClN2. C4H4O4, molecular weight: 390.87, CAS number: 113-92-8. [0003] Chlorpheniramine maleate preparations include tablets and injections, also known as chlorpheniramine, an antihistamine drug. This product has an anti-allergic effect by antagonizing H1 receptors. Mainly used for rhinitis, skin and mucous membrane allergies and relieve cold symptoms such as tearing, sneezing and runny nose. Indications: It is used for colds and skin and mucous membrane allergic diseases. It has the function of treating urticaria, eczema, dermatitis, drug eruption, skin pruritus, neurodermatitis, insect bites, solar dermat...

Claims

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Application Information

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IPC IPC(8): C07D213/38C07D213/57C07C57/145C07C51/41
CPCC07D213/38C07D213/57C07C51/412C07C57/145Y02P20/584
Inventor 张强黄忠超雷凯但小梅吴金伟
Owner CHENGDU JIANJIANG PHARMA FACTORY
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