Method for synthesizing doxepin hydrochloride by using benzofuranone as raw material

The invention discloses a method for synthesizing doxepin hydrochloride by taking 3-benzofuranone as a raw material, and belongs to the technical field of chemical synthesis. According to the method, cheap 3-benzofuranone is taken as a raw material, and the doxepin hydrochloride is prepared through...

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Hauptverfasser: CUI BENQIANG, SHI YANHUI, TIAN YE, CAO CHANGSHENG
Format: Patent
Sprache:chi ; eng
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Zusammenfassung:The invention discloses a method for synthesizing doxepin hydrochloride by taking 3-benzofuranone as a raw material, and belongs to the technical field of chemical synthesis. According to the method, cheap 3-benzofuranone is taken as a raw material, and the doxepin hydrochloride is prepared through trifluoromethanesulfonic acid esterification, Suzuki coupling reaction, C-O bond activation dearomatization, Mitsunobu reaction and Heck reaction. According to the invention, the synthesis steps are simplified, the reaction conditions are mild, the operation is simple, the product yield is high, and a new way is provided for synthesis of the doxepin hydrochloride compound. Compared with the prior art, the method has the advantages of no need of concentrated acid, organic lithium or Grignard reagent, mild reaction conditions, simplified reaction steps and improved reaction efficiency. 一种以3-苯并呋喃酮为原料合成盐酸多塞平的方法,属于化学合成技术领域。该方法以廉价3-苯并呋喃酮为原料,经三氟甲磺酸酯化、Suzuki偶联反应、C-O键活化去芳化、Mitsunobu反应和Heck反应制备盐酸多塞平。本发明简化合成步骤、反应条件温和、操作简单、产物收