Preparation method of ambroxol hydrochloride

A technology of ambroxol hydrochloride and lithium acetate, which is applied in the preparation of organic compounds, preparation of amino hydroxyl compounds, chemical instruments and methods, etc., can solve the problems of large-scale production risks, unsuitable for industrialized large-scale production, etc., and achieve easy operation, The effect of mild conditions and mature technology

Inactive Publication Date: 2012-07-11
合肥科尚医药科技有限公司
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Problems solved by technology

Due to the high-pressure hydrogenation and optical resolution that need to be used when synthesizing the key intermediate trans 4-aminocyclohexanol, there is a large production risk, so the synthetic method that is not suitable for traditional ambroxol hydrochloride is not suitable for industrialization Production

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  • Preparation method of ambroxol hydrochloride
  • Preparation method of ambroxol hydrochloride
  • Preparation method of ambroxol hydrochloride

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Embodiment Construction

[0022] In order to make the object, technical solution and advantages of the present invention clearer, the present invention will be further described in detail below in conjunction with the accompanying drawings and embodiments. It should be understood that the specific embodiments described here are only used to explain the present invention, not to limit the present invention.

[0023] Such as figure 1 Shown, the preparation method of ambroxol hydrochloride comprises the following steps.

[0024] Step 1: the compound of formula (1) adds acetic acid (HOAc-pentane) to catalyzer lithium chloride (LiCl), lithium acetate (LiOAc), palladium acetate (Pa(Oac)), p-benzoquinone (p-benzoquinone) at room temperature Down reaction obtains formula (2) compound,

[0025]

[0026] Wherein, the reaction temperature is room temperature, and the solvent is n-pentane. Raw material 1 (that is, the compound of formula (1)) and manganese dioxide are added twice to obtain a higher yield. D...

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Abstract

The invention relates to a preparation method of ambroxol hydrochloride. The preparation method comprises the steps of: directly obtaining a compound in formula (2) from simple intermediate 1,3-cyclohexadiene under the catalysis of palladium acetate, reacting with a compound in formula (3) to obtain a compound in formula (4), hydrolyzing the compound in the formula (4) in the presence of potassium carbonate, reducing by sodium borohydride, and carrying out salt forming with hydrochloric acid to obtain ambroxol hydrochloride. Therefore, synthesis of key intermediate trans-4-amino cyclohexanol in a common process is avoided and the separation of racemic products is avoided. The method is simple and feasible in operation, mild in conditions, mature in process and high in product yield and purity, and is suitable for industrialized mass production.

Description

technical field [0001] The invention relates to the technical field of chemical industry and pharmacy, in particular to the synthesis of a crude drug, and further to a new method for synthesizing ambroxol hydrochloride. Background technique [0002] Ambroxol hydrochloride is the active metabolite of bromhexine, widely used clinically in acute and chronic bronchitis, bronchial asthma, neonatal respiratory distress and lung surgery with low toxicity , The curative effect is exact and so on. At present, the synthesis of ambroxol hydrochloride basically all takes the key intermediate trans 4-aminocyclohexanol as the main raw material. Due to the high-pressure hydrogenation and optical resolution that need to be used when synthesizing the key intermediate trans 4-aminocyclohexanol, there is a large production risk, so the synthetic method that is not suitable for traditional ambroxol hydrochloride is not suitable for industrialization Production. Contents of the invention ...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07C215/44C07C213/08
Inventor 杨永亮陶玉成
Owner 合肥科尚医药科技有限公司
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