CN Patent

CN105732490A — 一种贝曲西班的制备方法

Assigned to Chongqing Medical University · Expires 2016-07-06 · 10y expired

What this patent protects

本发明提供了一种制备贝曲西班的方法，以5甲氧基靛红酸酐为原料，其与2氨基5氯吡啶在叔丁醇钾的条件下经亲核加成消除制得N(5氯2吡啶基)5甲氧基2氨基苯甲酰胺，化合物4与对氰基苯甲酰氯反应制得N(5氯2吡啶基)2[(4氰基苯甲酰基)氨基]5甲氧基苯甲酰胺盐酸盐，最后与二甲胺亲核加成共3步反应得制得目标产物贝曲西班，总收率57.8％。本发明原料价廉易得，反应条件温和，反应可控性高，具有良好的工业化应用前景。

USPTO Abstract

本发明提供了一种制备贝曲西班的方法，以5甲氧基靛红酸酐为原料，其与2氨基5氯吡啶在叔丁醇钾的条件下经亲核加成消除制得N(5氯2吡啶基)5甲氧基2氨基苯甲酰胺，化合物4与对氰基苯甲酰氯反应制得N(5氯2吡啶基)2[(4氰基苯甲酰基)氨基]5甲氧基苯甲酰胺盐酸盐，最后与二甲胺亲核加成共3步反应得制得目标产物贝曲西班，总收率57.8％。本发明原料价廉易得，反应条件温和，反应可控性高，具有良好的工业化应用前景。

Drugs covered by this patent

Patent Metadata

Patent number
CN105732490A
Jurisdiction
CN
Classification
—
Expires
2016-07-06
Drug substance claim
No
Drug product claim
No
Assignee
Chongqing Medical University
Source
FDA Orange Book + USPTO grounding via Google Patents

Bibliographic data sourced from FDA Orange Book + USPTO public records. Plain-English summary generated by AI grounded in source text. Patent term extensions (PTR, SPC, pediatric) may shift the effective expiry. Not legal advice.

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