A kind of synthetic method of biphenyl diester intermediate

The technology of a kind of bifendate and synthetic method is applied in the field of synthesis of bifendate intermediate, which can solve the problems of restricting industrial production, incomplete protection, low yield, etc.
CN111004206BActive Publication Date: 2021-05-11苏州诚和医药化学有限公司
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Patent Information

Authority / Receiving Office
CN · China
Patent Type
Patents(China)
Current Assignee / Owner
苏州诚和医药化学有限公司
Publication Date
2021-05-11

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Abstract

The invention belongs to the field of chemical pharmacy, and specifically discloses a method for synthesizing a biphenyl diester intermediate. Using gallic acid as a raw material, it undergoes an esterification reaction with solid phosgene to protect the o-diphenol hydroxyl group, followed by dimethylation and deprotection. Then, the biphenyl diester intermediate is obtained through bromination and methylation. The synthesis method of the bifendate intermediate of the present invention adopts phosgene to protect the ortho-diphenol hydroxyl group, the protection is complete, the reaction condition is mild, the process is simple, and the operation is convenient. Through the exploration and optimization of conditions, the product yield and purity are high, and the waste water problem in the borax protection method is solved, without damaging the environment, and it reduces the treatment of industrial waste water in the later stage, and reduces the production cost of the overall process to the greatest extent. high application.
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Description

technical field

[0001] The invention belongs to the field of chemical pharmacy, and in particular relates to a method for synthesizing a bifendate intermediate. Background technique

[0002] Biphenyldicarboxylate (Biphenyldicarboxylate, DDB) is an intermediate product of artificial synthesis of Schisandra C, a new drug discovered in the process of researching the traditional Chinese medicine Schisandra, clinically used for chronic persistent hepatitis with elevated alanine aminotransferase (ALT), It can also be used for ALT elevation caused by chemical poisons and drugs.

[0003] CN86107486A discloses a synthetic method of biphenyl diester, the key intermediate of which is 2-bromo-3,4-methylenedioxy-5-methoxybenzoic acid methyl ester. The current industrial production process uses gallic acid as raw material , first esterify in methanol to obtain the methyl ester, then methylate under the protection of borax, and then obtain the target intermediate through bromination and c...

Claims

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