Preparation method of vildagliptin intermediate

An intermediate, proline amide technology, applied in the field of preparation of vildagliptin intermediate -1-pyrrolidine-2-amide, can solve the problems of high solubility, low solubility, large loss, etc., and achieve excellent product quality and easy operation Simple, Gentle Effects
CN110590632AInactive Publication Date: 2019-12-20ZHEJIANG GUOBANG PHARMA
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Patent Information

Authority / Receiving Office
CN · China
Current Assignee / Owner
ZHEJIANG GUOBANG PHARMA
Publication Date
2019-12-20
Estimated Expiration
Not applicable · inactive patent

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Abstract

Belonging to the technical field of heterocyclic compounds, the invention provides a preparation method of a vildagliptin intermediate. The preparation method includes: adding prolinamide into a solvent, performing stirring and heating to dissolve prolinamide; performing cooling, adding propylene oxide as an acid-binding agent, and adding chloroacetyl chloride dropwise under stirring; carrying outcondensation reaction at the end of adding; lowering the temperature and performing heat preservation; conducting filtering, washing the filter residue, and performing drying to obtain (S)-1-(2-chloracetyl)pyrrolidine-2-amide. The method has the advantages of simple process, mild reaction conditions, high product purity and the like.
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Description

technical field

[0001] The application relates to a preparation method of vildagliptin intermediate (S)-1-(2-chloroacetyl)pyrrolidine-2-amide, which belongs to the technical field of heterocyclic compounds. Background technique

[0002] Diabetes mellitus (DM) is one of the most important non-communicable diseases currently threatening human health. In 2015, the number of patients worldwide reached 415 million. As a big country with diabetes, the prevalence of diabetes in my country continues to rise and has reached 11.6% of the total population, of which more than 90% are type 2 diabetes mellitus (T2DM). Diabetes and its complications seriously affect the quality of life of patients, and bring a heavy burden to patients, the national economy, and medical insurance. Current interventions for T2DM mainly include diet control and the use of oral and / or injectable hypoglycemic agents on the basis of exercise therapy. Dipeptidyl peptidase-4 (dipeptidyl peptidase-4, DPP-4) inhib...

Claims

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