Prepn process of chiral 4-substituent-2-oxazolidone

An oxazolidinone and chiral technology, which is applied in the field of preparation of chiral 4-substituted-2-oxazolidinone, achieves the effects of reducing the amount of solvent, shortening the time and increasing the yield
CN1931847AInactive Publication Date: 2007-03-21上海五洲药业股份有限公司 +1
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Patent Information

Authority / Receiving Office
CN · China
Patent Type
Applications(China)
Current Assignee / Owner
上海五洲药业股份有限公司
Publication Date
2007-03-21
Estimated Expiration
Not applicable · inactive patent

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Abstract

The present invention discloses the preparation process of one kind of chiral 4-substituent-2-oxazolidone. The preparation process includes the first reducing chiral amino acid into alcohol in the presence of Lewis acid and catalyst metal boron compound, the subsequent acylation with acyl chloride compound and no phosgene, and cyclization in buffering solution with strong alkali catalyst. The present invention has low cost, less reaction steps, less wastes produced, high product quality and high total yield, and is suitable for industrial production.
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Description

Technical field:

[0001] The invention relates to the technical field of medicinal chemistry. It specifically relates to a preparation method of chiral 4-substituted-2-oxazolidinone. Background technique:

[0002] Since the thalidomide incident occurred in the 1960s, the research on the chirality of drugs and chiral drugs has attracted the attention of countries all over the world. The traditional racemic resolution technology has greatly hindered the research and development of chiral drugs.

[0003] In 1964, Mitsni used chiral adjuvant for the first time to obtain the result of stereo control of asymmetric aldol condensation reaction. Although the stereoselectivity was not high (only 58%), it caused an upsurge in chiral adjuvant research. A significant improvement occurred in the decade, when Evans and Madamune introduced a series of chiral auxiliaries leading to high stereoselectivity, including the 4-substituted-2-oxazolidinone products, which induced highly enantiosele...

Claims

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