Preparation method of optically pure 4-aryl-2-hydroxy-butyric acid

An aryl and optical technology, which is applied in the field of preparation of optically pure 4-aryl-2-hydroxy-butyric acid, can solve the problems of increased cost, cumbersome operation process, and reduced total yield, and achieves low-cost, repeatable Good sex and high selectivity
CN101941900AInactive Publication Date: 2011-01-12SHANGHAI JIAO TONG UNIV

Patent Information

Authority / Receiving Office
CN · China
Current Assignee / Owner
SHANGHAI JIAO TONG UNIV
Publication Date
2011-01-12
Estimated Expiration
Not applicable · inactive patent

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Abstract

The invention relates to a preparation method of optically pure 4-aryl-2-hydroxy-butyric acid in the technical field of chemical materials. In an organic ether or alcoholic solvent, 4-aryl-2-oxo-3-crotonic acid is catalytically hydrogenated under the coexistence of a ruthenium complex of a united aryl-axis chiral phosphine ligand and an acidic additive to prepare optically pure 4-aryl-2-hydroxy-butyric acid. Starting from the 4-aryl-2-oxo-3-crotonic acid, the invention uses the ruthenium complex of the united aryl-axis chiral phosphine ligand as a catalyst and adds the acidic additive to obtain (R)-4- aryl-2-hydroxy-butyric acid through an asymmetric catalytic hydrogenation. The invention has low cost, stable physical and chemical properties and easy purification and increases an ee value to be larger than 99 percent through a simple and convenient recrystallization method. The reaction formula is carried out as shown in the specification.
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Description

technical field The invention relates to a preparation method in the technical field of chemical materials, in particular to a preparation method of optically pure 4-aryl-2-hydroxy-butyric acid. Background technique Optically pure ethyl 4-phenyl-2-hydroxy-butyrate is an important pharmaceutical intermediate and is widely used in the fields of medicine and new materials. Among them, (R)-4-phenyl-2-hydroxy-butyric acid ethyl ester is an important intermediate for the preparation of antihypertensive drugs-pril drugs. Pulil drugs are inhibitors of angiotensin-converting enzyme (ACE), and are a class of antihypertensive drugs that are currently used in a very large amount, accounting for about one-fifth of the entire hypertension drug market. Found through the retrieval of prior art document, the method for preparing (R)-4-phenyl-2-hydroxy-butyric acid ethyl ester is a lot (Asymmetric Catalysis on Industrial Scale: Challenges, Approaches and Solutions; Wiley-VCH: Weinheim , 20...

Claims

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