- Method for synthesizing arbidol hydrochloride intermediate
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The invention discloses a method for synthesizing an arbidol hydrochloride intermediate, and belongs to the technical field of medical intermediates. According to the method, 5-hydroxy-1, 2-dimethylindole-3-carboxylic acid ethyl ester is used as a raw material, and esterification, bromination, thiophenol and deprotection, Mannich reaction and salification are performed to obtain arbidol hydrochloride. In the process of generating the most important intermediate 5-acetoxy-6-bromo-2-bromomethyl-1-methylindole-3-carboxylic acid through bromination reaction, (p-methyl isopropyl benzene)-rutheniumdichloride dimer is used as a catalyst, NBS serves as a bromination reagent, DMA serves as a solvent to replace a traditional bromine bromination reagent, reaction conditions are mild, reaction selectivity is high, raw material sources are convenient, pollution of bromine to the environment can be avoided, and the catalytic activity of the novel catalyst is not reduced due to the influence of thereaction environment. Therefore, the method has the advantages of few byproducts, high yield, low production cost, high safety, energy conservation and the like, and meets the modern chemical production requirements of green reaction.
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Paragraph 0016
(2020/08/25)
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- Preparation method of arbidol hydrochloride
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The invention discloses a preparation method of arbidol hydrochloride. P-nitrophenol which is cheap and easy to obtain is innovatively adopted as the raw material, and through acetylation, nitroreduction, an indole ring reaction, a methylation reaction, bromination, a reaction with thiophenol and deprotection, a Mannich reaction and salification, arbidol hydrochloride is obtained. Reaction conditions of the whole synthesis process are mild, the raw material can be conveniently obtained, the character of the product is good, the yield is high, few by-products are generated, reaction selectivity and purity are high, environmental friendliness is achieved, production cost is low, and the method is suitable for industrial production; the defects that in the prior art, selectivity is low, many by-products are generated, the yield is low, precious catalysts are used, and serious environmental pollution is caused are overcome.
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