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New method for preparing alverine citrate

A technology of alverine citrate and phenylpropanol, which is applied in the preparation of amino-substituted functional groups, the preparation of amino compounds from amines, organic chemistry, etc., can solve problems such as toxicity and difficult reaction conditions, and achieve mild reaction conditions and easy operation. Ease of the process

Inactive Publication Date: 2010-09-22
重庆北碚现代应用药物研究所
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Problems solved by technology

The methods used in this process route are all classic reactions, but the reaction conditions are difficult to achieve in large-scale production. For example, the reaction of reducing carbonyl in the Huang Minglong reaction needs to be carried out under high temperature conditions, and the hydrazine reagent used is harmful to the environment and people. certain toxicity

Method used

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  • New method for preparing alverine citrate
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Examples

Experimental program
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Effect test

Embodiment

[0012] Embodiment: the preparation of alverine citrate

[0013] The first step: the preparation of 3-phenylbromopropane

[0014] Add 50ml of water into a 250ml flask, carefully add 70ml of concentrated sulfuric acid, mix well, cool to room temperature, then add 68g of phenylpropanol and 75g of sodium bromide in turn, heat to reflux, the reaction is over, separate the organic layer, and the organic layer in turn Use 100ml of water, 5ml of concentrated sulfuric acid, 100ml of water, and 100ml of saturated sodium bicarbonate solution. Then washed three times with 100 ml of water each time to obtain 80 g of orange-red oily liquid with a yield of 80%, and no further purification was required.

[0015] Step 2: Preparation of Bethamphetamine

[0016] Add 0.05mol (9.9g) of 3-phenylbromopropane dropwise to a 250ml flask filled with 100ml of ethylamine solution under ice bath conditions, react for 4h under ice bath, and then continue to react at room temperature, followed by TLC, the ...

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Abstract

The invention discloses a new method for synthesizing alverine citrate. The method comprises the following steps of: performing bromination on phenylpropanol to prepare 3-phenyl bromopropane by taking phenylpropanol as an initiative raw material; reacting the 3-phenyl bromopropane with ethylamine solution to prepare ethylamphetamine; reacting ethylamphetamine with 3-phenyl bromopropane under the alkaline condition to prepare diphenyl propyl ethylamine; and finally reacting the diphenyl propyl ethylamine with citric acid to prepare the alverine citrate serving as the final product. The process flow has the advantage of readily available raw material, simple operation, safe reaction and economy and practicability.

Description

technical field [0001] The invention belongs to chemicals containing organic active ingredients, and in particular relates to a new preparation method of alverine citrate. Alverine citrate is a commonly used antispasmodic drug in clinical practice. Background technique [0002] Alverine citrate (Alverine, molecular formula: C 20 h 27 N·C 6 h 8 o 7 , Molecular weight: 473.6), is a synthetic papaverine derivative, listed in Western countries in 1996, it directly acts on smooth muscle, and can selectively act on the smooth muscle of the gastrointestinal tract, uterus and genitourinary organs, and has antispasmodic effect . [0003] The reported synthesis process uses benzyl chloride as the raw material to obtain the product through four steps of Grignard reaction, halogenation, amination and salt formation. [0004] Mao Xiantong et al. reported that for the pollution problem in the above-mentioned process route, the technical route was changed, and the Grignard reaction ...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07C211/27C07C209/68C07C209/08C07C59/265
Inventor 张玉斌吉庆刚王兰周
Owner 重庆北碚现代应用药物研究所
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