Preparation method for alpha-amino ketone derivative

A technology of aminoketone and derivatives, which is applied in the field of preparation of α-aminoketone derivatives, and can solve the problems of too strong oxidation of reagents, serious side reactions, and low yield
CN102584620AInactive Publication Date: 2012-07-18SHANGHAI INST OF PHARMA IND
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Patent Information

Authority / Receiving Office
CN · China
Current Assignee / Owner
SHANGHAI INST OF PHARMA IND
Publication Date
2012-07-18
Estimated Expiration
Not applicable · inactive patent

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Abstract

The invention discloses a preparation method for an alpha-amino ketone derivative as represented by formula II. The derivative is prepared by subjecting a compound as represented by formula I to a reaction in an organic solvent under the action of trichloroisocyanuric acid and an oxidation catalyst or subjecting the compound as represented by formula I to a reaction in an organic solvent with a pH value of 8 to 11 under the action of an oxidizing agent, an oxidation catalyst, a pH conditioning agent and a phase-transfer catalyst, wherein, R1, R2 and R3 are, independently, lower alkyl groups, aryl groups, aryl-substituted lower alkyl groups, lower alkoxy groups, aryl-substituted lower alkoxy groups, carboxyl-substituted lower alkyl groups or carbonyl groups connected with lower alkyl groups, and R4 is a carbonyl group connected with a lower alkyl group, a carbonyl group connected with an aryl group or a carbonyl group connected with a phenyl-substituted lower alkyl group. The preparation method provided in the invention has the advantages of cheap and easily available raw materials, mild reaction conditions, small pollution to the environment and a high conversion rate of the raw material and is beneficial for industrial large-scale production.
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Description

technical field

[0001] The present invention relates to a preparation method of α-aminoketone derivatives. Background technique

[0002] Pseudoephedrine is the main functional ingredient of various anti-cold medicines. Years of clinical practice have shown that it is a safe and effective medicine, and it is widely used at home and abroad.

[0003] In the recrystallization mother liquor of pseudoephedrine production process, only contain about 5% (1S, 2S) type pseudoephedrine, about 95% are its (1R, 2R) type isomers. How to convert unwanted (1R, 2R) isomers into useful (1S, 2S) configurations is an important issue to be solved in industrial production. The conventional transformation method is realized through a series of operation steps such as oxidation, heating racemization, reduction, hydroxyl acylation, isomerization, hydrolysis, addition of alkali, and resolution. Among them, the choice of oxidation method is the most critical part.

[0004] The reagents commonly use...

Claims

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