Method for synthesizing 2,4,5-trimethoxyethylphenylketone intermediate of alpha-asarin

A technology of trimethoxybenzene and intermediates, which is applied in the field of the key intermediate 2 of the synthetic drug a-asarone, which can solve the problems of toxic organic solvents and cumbersome acetone operations, and achieve low cost, good product quality and safe operation reliable effect
CN101891604AInactive Publication Date: 2010-11-24广西中医学院
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Patent Information

Authority / Receiving Office
CN · China
Patent Type
Applications(China)
Current Assignee / Owner
广西中医学院
Publication Date
2010-11-24
Estimated Expiration
Not applicable · inactive patent

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Abstract

The invention discloses a method for synthesizing a 2,4,5-trimethoxyethylphenylketone intermediate of alpha-asarin, which is characterized by comprising the following steps of: directly reacting 2,4,5-trimethoxybenzene, which servers as a raw material, with propanoic acid or propionic anhydride under the action of polyphosphoric acid, or a mixture of phosphoric acid and phosphoric anhydride, or a mixture of the polyphosphoric acid, the phosphoric acid and the phosphoric anhydride; and performing hydrolysis to obtain the 2,4,5-trimethoxyethylphenylketone. The product can be used as the raw material or the intermediate of the alpha-asarin or the raw material for synthesizing other medicaments, and also can be used as spices. The method of the invention has the advantages of simple process, low cost, high product quality, high yield and the like and is safe and reliable in operation and suitable for industrial production. The method can effectively solve the problems of complicated operation and the like of the synthesis of the 2,4,5-trimethoxyethylphenylketone intermediate of the alpha-asarin.
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Description

technical field

[0001] The invention relates to a convenient method for synthesizing 2,4,5-trimethoxypropiophenone, a key intermediate of drug α-asarone. Background technique

[0002] 2,4,5-Trimethoxypropiophenone is a chemical component present in Piper marginatum. It is an important raw material and intermediate for the synthesis of expectorant and antiasthmatic drug a-asarone, and it can also be used as a spice .

[0003] Indian Patent Indian Pat.Appl., 2003 DE 00119, 16 Mar 2007 and Chinese Invention Patent CN 101492351, and Zhang Ling and Liu Suyun in "Preparation of α-Asarone", "Chinese Journal of Pharmaceutical Industry", 2007, 38(7) : 477-478, all proposed to use 1,2,4-trimethoxybenzene as raw material, anhydrous aluminum trichloride or anhydrous zinc chloride as catalyst, and carry out propionylation reaction to synthesize 2,4,5 through propionyl chloride - Trimethoxypropiophenone. The disadvantage of this method is that there are many side reactions, a large amo...

Claims

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