- Efficient production method of bromhexine hydrochloride
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The invention belongs to the technical field of biological medicines, and particularly relates to an efficient production method of bromhexine hydrochloride. The production method of bromhexine hydrochloride comprises the following steps: (1) reducing 3,5-dibromo-2-aminobenzaldehyde by a reducing agent to obtain an intermediate 3,5-dibromo-2-aminobenzyl alcohol; (2) reacting the intermediate 3,5-dibromo-2-aminobenzyl alcohol with N-methylcyclohexylamine, and then carrying out salt forming reaction to obtain a bromhexine hydrochloride crude product; and (3) purifying the bromhexine hydrochloride crude product to obtain the bromhexine hydrochloride.
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Paragraph 0081-0087; 0099-0102; 0110-0113; 0121-0123
(2021/01/28)
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- Preparation method of bromhexine hydrochloride
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The invention belongs to the field of pharmaceutical chemicals, and particularly relates to a bromhexine hydrochloride synthesis method. The synthesis method comprises following steps: step A, carrying out a reduction reaction between 2-amino-3,5-dibromobenzaldehyde and a reducing agent to generate 2-amino-3,5-dibromobenzyl alcohol; step B, reacting 2-amino-3,5-dibromobenzyl alcohol obtained in the step A with thionyl chloride to generate 2,4-bromo-6-chloromethyl aniline; and step C, carrying out an amination reaction between 2, 4-bromo-6-chloromethyl aniline obtained in the step B and N-methyl cyclohexyl amine, and then carrying out a salt forming reaction with an HCl salifying reagent to obtain bromhexine hydrochloride. According to the preparation method, thionyl chloride is only used as a reactant; in addition, the steps are simple, the intermediates obtained in the steps A and B do not need to be purified and directly used for the next step of reactions, therefore, the working hours required by the whole production route are remarkably shortened, the final yield is increased by 5% or above, and the method is particularly suitable for large-scale production.
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Paragraph 0066-0079; 0083-0084
(2020/08/09)
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- A preparation method of bromhexine hydrochloride (by machine translation)
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The invention belongs to the field of organic synthesis, provides a bromhexine hydrochloride of the preparation method. The invention relates to 2 - aminobenzoic acid ester compound as a raw material, by the bromo reaction, reduction reaction, condensatio
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- Preparation method and application of 2-amino-3,5-bibromobenzyl intermediate compound
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The invention provides a preparation method of a 2-amino-3,5-bibromobenzyl intermediate compound and further discloses an application of the 2-amino-3,5-bibromobenzyl intermediate compound in preparation of bromhexine and ambroxol. A cheap and available raw material 2-amino-3,5-dibromobenzaldehyde is adopted, 2-amino-3,5-dibromobenzyl alcohol is obtained through reduction, and the reaction condition is milder; N'N-carbonyldiimidazole is used for activating hydroxyl of 2-amino-3,5-dibromobenzyl alcohol to produce active ester, and the active ester is subjected to a condensation reaction with N-methylcyclohexylamine and trans-p-aminocyclohexanol to produce corresponding products respectively. The preparation method has the advantages that the reproducibility is good, the process is simple, the product purity is high and potential gene poison impurities can be avoided, and the medication safety of the 2-amino-3,5-bibromobenzyl intermediate compound can be further improved.
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Paragraph 0040; 0075; 0076; 0077
(2019/01/14)
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- A preparation method of bromhexine hydrochloride
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The invention provides a preparation method of bromhexine hydrochloride. 2-amino-3,5-dibromo benzaldehyde is taken as a raw material, and reduction, amination and salifying are carried out, so that the bromhexine hydrochloride is obtained, wherein amination and salifying are completed in one step, and an intermediate product is not needed to be separated. The preparation method of the bromhexine hydrochloride has the advantages that reaction steps are reduced, and yield and purity of the bromhexine hydrochloride product are improved.
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Paragraph 0028; 0029; 0030
(2017/05/20)
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- Sunlight-Driven Forging of Amide/Ester Bonds from Three Independent Components: An Approach to Carbamates
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A photoredox catalytic route to carbamates enabled by visible irradiation (or simply sunlight) has been developed. This process leads to a novel approach to the construction of heterocyclic rings wherein the amide or ester motifs of carbamates were assembled from three isolated components. Large-scale experiments were realized by employing continuous flow techniques, and reuse of photocatalyst demonstrated the green and sustainable aspects of this method.
- Zhao, Yating,Huang, Binbin,Yang, Chao,Chen, Qingqing,Xia, Wujiong
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supporting information
p. 5572 - 5575
(2016/11/17)
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