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ChemicalBook CAS DataBase List Arbidol hydrochloride
131707-23-8

Arbidol hydrochloride synthesis

10synthesis methods

Arbidol hydrochloride is a dual-acting anti-influenza virus drug developed by the former Soviet Union's Medicinal Chemistry Research Center. The synthetic method of Arbidol hydrochloride takes p-benzoquinone and 3-aminocrotonic acid ethyl ester as starting materials, and undergoes Netzescu reaction, O-acylation, N-alkylation, bromination, benzene Thiophenol reaction, Mannich amine methylation reaction, and acidification with hydrochloric acid to obtain the final product.

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Yield:131707-23-8 113.8 kg

Reaction Conditions:

with hydrogenchloride in ethanol;water at 35 - 70;Large scale;

Steps:

1-3 Example 1:

Concretely, the present invention provides a kind of synthetic method of Arbidol hydrochloride, the method is: add water 200kg, ethanol 200kg, dimethylamine hydrochloride 33.8kg, paraformaldehyde 10kg, concentrated hydrochloric acid 6.5kg to the reactor , 100kg of ethyl 6-bromo-5-hydroxy-1-methyl-2-(phenylthiomethyl)indole-3-carboxylate, stir and dissolve after feeding, firstly control the temperature at 35-40°C for 3h, then Slowly heat up to 65-70°C and react for 6 hours. After the reaction, cool to 0-5°C and stir and crystallize for 1 hour; centrifuge, dry and rinse the filter cake with ethanol aqueous solution with a mass fraction of 50%. After drying, the product is obtained. 113.8kg of white powder.

References:

CN115232055,2022,A Location in patent:Paragraph 0023-0031

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