- Method for preparing amiodarone hydrochloride
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The invention discloses a method for preparing amiodarone hydrochloride, which comprises the following steps: by taking 2-butylbenzofuran and p-acetoxybenzaldehyde as raw materials, carrying out aldol reaction under Lewis acid catalysis and heating conditions, simultaneously carrying out hydroxyl oxidation, deacetylation and iodination reaction on the product in the presence of iodine and alkali, and then reacting the product with N, N-diethyl chloroethylamine, and salifying to obtain amiodarone hydrochloride. According to the method, only a catalytic amount of Lewis acid is needed, strong acidic aluminum chloride is not needed, reaction conditions are milder, byproducts are few, post-treatment is easy, and three wastes are greatly reduced; the whole route is simple to operate, the used reagents are cheap, easy to obtain and non-toxic, and the method is very suitable for industrial production.
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- Preparation method of amiodarone hydrochloride
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The invention relates to a preparation method of amiodarone hydrochloride. According to the preparation method, synthesis of intermediate 2-butylbenzofuran is realized under effect of a catalyst, a cocatalyst, and an acid binding agent, through Sonogashira coupling cyclization reaction of 2-iodo phenol and 1-acetylene in an organic solvent at a 2-iodo phenol to 1-acetylene molar ratio of 1:09-1.3,wherein reaction temperature ranges from 30 to 60 DEG C, and reaction time ranges from 12 to 38h. Compared with the prior art, the advantages are that: operation is simplified; operation convenienceand product stability are improved; controlling of the ratio of the catalyst to the materials is capable of increasing the purities and yields of intermediates; no column chromatography purifying is needed; cost is reduced; production efficiency is increased at the same time; and convenience is provided for industrial large scale production.
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- Preparation method of amiodarone hydrochloride (by machine translation)
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The invention provides a preparation method, and relates to the technical field of drug synthesis, in particular to a preparation method of amiodarone hydrochloride. The invention uses methyl hydroxybenzoate as a main raw material, and sequentially undergoes a substitution reaction, etherification reaction, hydrolysis reaction, chloro reaction, a reaction, amination reaction and acidification, and the amiodarone hydrochloride. The preparation method provided by the invention does not need the process, reduces the use, reduces the environmental pollution, greatly reduces the environmental pollution and shortens the synthesis route while chlorination of 3, 5 - diiod -4 - (2 -hydroxyethoxy) - benzoic acid by using the thionyl chloride is reduced, and the synthetic route. The preparation method provided by the invention is simple in process, low in cost, small in pollution and high in yield. (by machine translation)
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Paragraph 0097-0099
(2019/08/12)
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- Amiodarone hydrochloride preparation method
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The invention belongs to the field of medicine, and especially relates to an amiodarone hydrochloride preparation method. The method takes 2-hydroxybenzaldehyde and 2-alkyl halohexoic acid ester as the raw materials to prepare 2-butylbenzofuran, 2-butylbenzofuran is taken as the raw material, and is subjected to the steps of friedel-crafts acylation, demethylation, iodination, etherification and salt forming to obtain the amiodarone hydrochloride. By employing the method, the raw materials have the advantages of low cost and easy acquisition, the process is simple, and 2-butylbenzofuran and amiodarone hydrochloride with high purity and high yield can be obtained, the cost is low, the waste water is little, and the method is suitable for industrial production.
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