A chemical enzymatic resolution preparation method of (r)-1-(1-naphthyl)ethylamine

A chemical enzyme and ethylamine technology, which is applied in the field of chemical enzyme resolution of (R)-1-(1-naphthyl)ethylamine, can solve the problems of low yield, large pollution, poor optical selectivity, etc., and achieve The effect of high catalytic efficiency and high optical purity

Inactive Publication Date: 2011-12-14
倪发根
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  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0003] The existing preparation methods of (R)-1-(1-naphthyl)ethylamine are mainly chemical synthesis and tartaric acid resolution, but this Both methods have the disadvantages of poor optical selectivity, low yield, and large pollution

Method used

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Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0014] A (R) -1- (1-萘) chemical enzyme split preparation method of ethyne. The 1- (1-萘 ethyl) ethyleine of 1- (1-萘 萘) is the raw material, and the alcohol ethyl acetateSupply, fixed Antarctic Ferrye yeast lipase is catalyst, toluene is a solvents, for dynamic splitting, the operating conditions are controlled as follows: temperature 30 ° C, the volume ratio of the raw material and solvents is 1: 25, the quality ratio of raw materials and catalysts is to the mass ratio of the catalyst is to be the mass ratio of the catalyst to1: 0.02, the Moorbi of the raw material and the alcohol ethyl acetate is 1: 1.2.After 48 hours of reaction, the conversion rate of the substrate can reach 48%, and the E.E. value of the product can reach more than 99%.

Embodiment 2

[0016] A (R) -1- (1-萘) chemical enzyme split preparation method of ethyne. The 1- (1-萘 ethyl) ethyleine of 1- (1-萘 萘) is the raw material, and the alcohol ethyl acetateSupply, fixed Antarctic fake silk yeast lipase is catalyst, toluene is a solvents, for dynamic splitting, the operating conditions are controlled as follows: temperature 40 ° C, the volume ratio of the raw material and the solvents is 1: 30, the quality ratio of raw materials and catalysts is to the mass ratio of catalysts to1: 0.025, the Moorbi of the ingredients and benzoryl ethyl acetate is 1: 2.0.After 42 hours of reaction, the conversion rate of the substrate can reach 48%, and the E.E. value of the product can reach more than 99%.

Embodiment 3

[0018] A (R) -1- (1-萘) chemical enzyme split preparation method of ethyne. The 1- (1-萘 ethyl) ethyleine of 1- (1-萘 萘) is the raw material, and the alcohol ethyl acetateSupply, fixed Antarctic Ferrye yeast lipase is catalyst, toluene is a solvents, for dynamic splitting, the operating conditions are controlled as follows: temperature 50 ° C, the volume ratio of the raw material and solvents is 1: 35, the quality ratio of raw materials and catalysts is to the mass ratio of the catalyst is1: 0.03, the Moorbi of the raw material and the alcohol ethyl acetate is 1: 3.0.After 38 hours of reaction, the conversion rate of the substrate can reach 50%, and the E.E. value of the product can reach more than 99%.

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Abstract

The invention discloses a kinetic resolution method, in particular a method for preparing chemical enzyme of (R)-1-(1-naphthyl) ethylamine by resolution, which using 1-(1-naphthyl) ethylamine as a raw material. In the method, kinetic resolution is performed by using 1-(1-naphthyl) ethylamine which is a racemic mixture as a raw material, phenylethyl acetate as an acyl donor and immobilized lipase from Candida Antarctica as a catalyst under the controlled operation conditions that: the temperature is 30 to 80 DEG C, the volume ratio of the raw material to a solvent is 1:(25-50), the mass ratio of the raw material to the catalyst is 1:(0.02-0.05), and the molar ratio of the raw material to the phenylethyl acetate is 1:(1.2-4.0). The method has the advantages of high catalytic efficiency and environment friendliness.

Description

Technical field [0001] The present invention involves a dynamic split method, especially the chemical enzyme splitting method for preparation (R) -1- (1-萘blade) to prepare (R) -1- (1-萘blade) for the method of 1- (1-pyrine)Essence Background technique [0002] (R) -1- (1-1) Aylemine is a very important drug intermediate. It is an important intermediate that synthesizes the treatment of hydrochloride hydrochloric acid that treats thyroid glandular cancer. In addition, (R)-1- (1-) is also a very important hand-alkali, which can be used to split various handic acid. [0003] The existing (R) -1- (1-萘) preparation method is based on chemical synthesis and liquor splitting method.Shortcomings. Invention content [0004] The purpose of the present invention is to provide a (R) -1- (1-Pen) chemical enzyme split preparation method for solving the above technical problems. It has the advantages of high product optical purity and high preparation efficiency. [0005] The above -mentioned t...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C12P13/00
Inventor 倪发根
Owner 倪发根
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