Intermediate compound for preparing dextro cadotril and its preparation process and use

A kind of compound, halogenation reaction technology, applied in the field of synthetic drug dexcadotril
CN100537522CActive Publication Date: 2009-09-09SHANGHAI SHYNDEC PHARMA CO LTD +1
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Patent Information

Authority / Receiving Office
CN · China
Patent Type
Patents(China)
Current Assignee / Owner
SHANGHAI SHYNDEC PHARMA CO LTD
Publication Date
2009-09-09

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Abstract

The invention discloses a novel intermediate compound for preparing dexcadotril with the general formula (1), wherein X represents Cl, Br, I and the like. The invention also discloses the preparation method of the intermediate compound and the application of the intermediate compound in the preparation of dexcadotril.
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Description

technical field

[0001] The invention relates to the field of medicinal chemistry, in particular to an intermediate compound for preparing dexcadotril, a preparation method thereof and a method for synthesizing drug dexecadotril (dexecadotril4) with the intermediate compound. Background technique

[0002] Dexecadotril (dexecadotril 4), the chemical name is N-[(2R)-2-acetylthiomethyl-1-oxo-3-phenylpropyl]glycine benzyl ester, the drug is before registration, Mainly used for the treatment of gastrointestinal disorders.

[0003]

[0004] Literature (synth.commun., 2001, 31 (2), 211-218) reported that dimethyl benzylmalonate was reduced by tetrahydrolithium aluminum, and then hydrolyzed by lipase to obtain a single isomer, and then chromium was used to obtain a single isomer. Reagent oxidation, thioacetic acid substitution, amidation to obtain dexcadotril:

[0005]

[0006] Because the reaction system has a greater impact on the activity of biological enzymes, the enzyme ...

Claims

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