Method for preparing (3R)-(-)-3-(2- acetamino)-5-methylhexanol

A technology of acetylamino and methylhexanoic acid, which is applied in the field of medicine, can solve the problems of excessive waste water, waste of raw materials, and long reaction time, and achieve the effects of increased yield, reduced production cost, and shortened reaction cycle
CN102898320AInactive Publication Date: 2013-01-30AURISCO PHARMACEUTICAL CO LTD
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Patent Information

Authority / Receiving Office
CN · China
Current Assignee / Owner
AURISCO PHARMACEUTICAL CO LTD
Publication Date
2013-01-30
Estimated Expiration
Not applicable · inactive patent

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Abstract

The invention provides a method for preparing an antiepileptic medicament pregabalin intermediate, i.e., (3R)-(-)-3-(2-acetamino)-5-methylhexanol. The method comprises the following steps of: salifying a (+ / -)-3-(2-acetamino)-5-methylhexanol racemic body serving as a raw material and (S)-(-)-1-phenylethylamine in a mixed solvent of alcohol and halogenated hydrocarbon, precipitating unnecessary S-shaped chiral isomer salts out, filtering, concentrating a filtrate, dissolving into water, and reacting by using an acid to obtain (3R)-(-)-3-(2- acetamino)-5-methylhexanol of which the e.e. value is 80-90 percent; and refining to obtain a (3R)-(-)-3-(2-acetamino)-5-methylhexanol product of which the e.e. value is 98-99 percent. The method has the advantages of high chiral monomer purity, wide reaction temperature range, convenience in operating and suitability for industrial production. The invention further provides a method for preparing a racemate, i.e., (+ / -)-3-(2-acetamino)-5-methylhexanol. The racemic body can be taken as a raw material for repeated use, so that the consumption of raw materials is lowered, environmental protection is promoted, and the method has high application value.
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Description

technical field

[0001] The present invention relates to medicines, in particular to the preparation of pharmaceutical intermediates, in particular to the preparation of antiepileptic drug pregabalin chiral intermediate (3R)-(-)-3-(2-acetylamino)-5-methylhexanoic acid method. Background technique

[0002] Epilepsy (commonly known as epilepsy) is a chronic disease in which the sudden abnormal discharge of brain neurons leads to transient brain dysfunction. Epileptic seizures refer to clinical phenomena caused by abnormal brain neurons and excessive hypersynchronized discharges. Depending on where in the brain the abnormally firing neurons are located, epilepsy can have a variety of manifestations, mostly motorsensory or autonomic, with or without changes in consciousness or alertness. According to relevant data, there are currently more than 50 million epilepsy patients in the world, with an average of 1 person per 100 people with epilepsy. On average, 20-70 cases of epileps...

Claims

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