Preparation of pregabalin chiral intermediate with bio-enzyme method

A chiral intermediate, pregabalin technology, applied in the field of pregabalin chiral intermediate preparation by biological enzymatic method, can solve the problems of low optical purity of pregabalin product, many reaction steps, difficult industrialization, etc., to achieve simple and more Synthesis, low cost, effect of reducing reaction steps
CN102465157AActive Publication Date: 2012-05-23瑞博(杭州)医药科技有限公司
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Patent Information

Authority / Receiving Office
CN · China
Patent Type
Applications(China)
Current Assignee / Owner
瑞博(杭州)医药科技有限公司
Publication Date
2012-05-23

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Abstract

The invention relates to the technical field of preparation of a pregabalin chiral intermediate with a bio-enzyme method, in particular to the preparation of the pregabalin chiral intermediate with the bio-enzyme method. According to a preparation method, a compound of isobutyl glutarate shown as a formula (I) is used as a raw material and used for generating a compound of (S)-3-(carbamoyl methyl)-5-methylcaproate shown as a formula (II) in an organic solvent under the action of bio-enzyme and ammonia, wherein R is preferentially direct-chain or side-chain alkyl of C1-C4.
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Description

technical field

[0001] The present invention relates to a biological enzymatic method for preparing a pregabalin chiral intermediate, in particular to a biological enzymatic method for preparing a pregabalin intermediate (S)-3-(carbamoylmethyl)-5-methylhexyl esters. Background technique

[0002] Pregabalin is also known as CI-1008 and PD-14472, and its chemical name is (3S)-3-aminomethyl-5-methylhexanoic acid.

[0003]

[0004] It is an aminobutyric acid (GABA) receptor antagonist developed by Pfizer of the United States. It was approved by the European Union in July 2004 and was first listed in the UK immediately. It is clinically used to treat neuralgia caused by diabetes and postherpetic neuralgia. , as well as the adjuvant treatment of partial incomplete epileptic seizures in adult patients, is the first drug approved by the FDA for the treatment of more than two types of neuropathic pain, with fewer administration times and less adverse reactions, and has broad mark...

Claims

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