Kinetic resolution method of chiral amine

A kinetic separation, chiral amine technology, applied in fermentation and other directions, can solve the problems of high environmental pollution, low optical purity of products, low separation yield, etc., and achieves improved performance, great application value, and mild reaction conditions. Effect
CN102766672AInactive Publication Date: 2012-11-07六安佳诺生化科技有限公司
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Patent Information

Authority / Receiving Office
CN · China
Patent Type
Applications(China)
Current Assignee / Owner
六安佳诺生化科技有限公司
Publication Date
2012-11-07
Estimated Expiration
Not applicable · inactive patent

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Abstract

The invention discloses a kinetic resolution method of chiral amine, comprising the following steps of: adding chiral amine and acyl donor at the mol ratio of 1:0.5-3 into an organic solvent reaction system, adding lipase which accounts for 10-80 wt% of the weight of chiral amine, and reacting at the reaction temperature of 30-70 DEG C for 12-48 hours to obtain amide with the conversion rate of 50% and e.e value being greater than 99%. According to the invention, resolution of chiral amine can be mildly realized under the condition of enzyme catalysis; and simultaneously, the product has good optical purity, high yield and great application values.
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Description

field of invention

[0001] The invention relates to a kinetic resolution method, in particular to a dynamic resolution method for chiral amines. Background technique

[0002] Chiral amines with a single configuration are commonly used intermediates in the synthesis of chiral drugs, and can also be used as chiral bases to resolve various chiral acids. In industry, when preparing these optically pure chiral amines, the resolution of racemates is still the most important and practical method because of its economy and feasibility. The most important resolution method for 1-(1-naphthyl)ethylamine and 1-(2-naphthyl)ethylamine is to use D-tartaric acid as the chiral resolution reagent for chemical resolution. This method has problems such as low resolution yield, low optical purity of the product, and large environmental pollution.

[0003] How to achieve high-efficiency and green separation of chiral amines while ensuring high optical purity has become our goal. Invention cont...

Claims

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