Vilazodone intermediate synthesis method

The invention discloses a Vilazodone intermediate synthesis method. According to the Vilazodone intermediate synthesis method, 6-nitrocoumarin serves as an initial raw material, through the steps of ring opening, intramolecular cyclization, esterification, reduction, piperazine-ring preparation and...

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Hauptverfasser: DONG SHUQIU, FENG RUIMAO, ZHANG QINGJIE
Format: Patent
Sprache:chi ; eng
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Zusammenfassung:The invention discloses a Vilazodone intermediate synthesis method. According to the Vilazodone intermediate synthesis method, 6-nitrocoumarin serves as an initial raw material, through the steps of ring opening, intramolecular cyclization, esterification, reduction, piperazine-ring preparation and the like, the key Vilazodone intermediate 5-(1-piperazinyl)-2-benzofuran-2-carboxylic acid ethyl ester shown in the formula I is obtained. The Vilazodone intermediate synthesis method is simple is synthesis path, the yield of the targeted product is high, and the Vilazodone intermediate synthesis method is suitable for industrial large-scale production. 本发明涉及种维拉佐酮中间体合成方法,以6-硝基香豆素为起始原料原料,经开环、分子内关环、酯化、还原、哌嗪环制备等步骤,得到维拉佐酮关键中间体式Ⅰ化合物5-(1-哌嗪基)-2-苯并呋喃-2-羧酸乙酯。本发明合成路线简单,目标产物收率较高,适合工业化放大生产。