Recemizing method for alpha-aminoalcohol compounds and its catalyst

Abstract

The present invention discloses a kind of alpha-amino alcohol compound racemizing method and its catalyst. The catalyst has Al2O3 carrier and active component of one or several of Co, Cr, Mo, Rh, Zn, Fe, Cu, Ni, Sr, Ca and Bioavailability, with the total active component amount is 20-40 wt% of the catalyst. In a fixed bed reactor and hydrogen atmosphere, liquid or gas phase alpha-amino alcohol compound is introduced, diluted with solvent, and reacted at material feeding space velocity of 100-20000 / hr, temperature of 100-300 deg.c and pressure of 0.5-0.8 MPa. The present invention has the advantages of simple preparing process, low cost, stable activity and long service life of catalyst, high yield of the racemized product and high racemizing effect.

Description

technical field [0001] The invention belongs to the racemization technology of pharmaceutical intermediate α-amino alcohol series compounds, specifically the racemization method and catalyst of α-amino alcohol compounds. Background technique [0002] α-Amino alcohol compounds are an important class of pharmaceutical intermediates. But for most α-aminoalcohol compounds, only one enantiomer is what we need, and the other enantiomer has no application value. For example: S-2-amino-1-butanol is an important intermediate in the synthesis of anti-tuberculosis drug ethambutol hydrochloride, but R-2-amino-1-butanol has no application value. Therefore, in order to reduce production costs, it is necessary to convert R-2-amino-1-butanol into (R, S)-2-amino-1-butanol by racemization, and then split to obtain S-2-amino-1 -butanol and be utilized. The relevant patent reports mainly include the following: US 4,096,186 reports Co, Co / Fe prepared by coprecipit...

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Problems solved by technology

The relevant patent reports mainly include the following: US 4,096,186 reports Co, Co / Fe prepared by coprecipitation 2 o 3 As a catalyst, in NH 3 and H 2 R-2-amino-1-butanol is racemized in the presence of R-2-amino-1-butanol. When the best product yield is 97.6%, the racemization rate is only 63%; when the racemization rate is 99%, the product yield is The rate is only 75.1%, that is, it cannot achieve better racemization effect and higher product yield at the same time

IN-A-162,213 reported Rh / Al 2 o 3 As a catalyst, in NH 3 and H 2 R-2-amino-1-butanol was racemized in the presence, but the racemization rate was only 42.5%

At the same time, the common disadvantages of the above two patents are: 1. NH needs to be used in the reaction 3 , making it difficult to control the production, and at the same time make it difficult to refine the product; 2. The cost of the catalyst is relatively high

US 4,990,666 reports using skeleton cobalt as a catalyst for the racemization of R-2-amino-1-butanol in a hydrogen-facing state, but it is mainly suitable for batch reactions, and the cost of the catalyst is relatively high

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