Preparation method of chiral intermediate of niraparib

The invention discloses a novel synthetic method for preparing a chiral intermediate of niraparib. The method comprises the following steps: taking 4-bromophenylacetic acid and chiral substituted oxazolone as starting materials; and carrying out amide condensation, Michael addition, hydrolysis, redu...

Ausführliche Beschreibung

Gespeichert in:
Bibliographische Detailangaben
1. Verfasser: ZHONG GUIFA
Format: Patent
Sprache:chi ; eng
Schlagworte:
Online-Zugang:Volltext bestellen
Tags: Tag hinzufügen
Keine Tags, Fügen Sie den ersten Tag hinzu!
Beschreibung
Zusammenfassung:The invention discloses a novel synthetic method for preparing a chiral intermediate of niraparib. The method comprises the following steps: taking 4-bromophenylacetic acid and chiral substituted oxazolone as starting materials; and carrying out amide condensation, Michael addition, hydrolysis, reduction and intramolecular cyclization to obtain the intermediate (VII). The preparation method is low in cost, raw materials are easily obtained, the yield is high, and the synthetic method is suitable for industrialized production. 本发明公开了种新型制备尼拉帕尼的手性中间体的合成方法,该方法包括以4-溴苯乙酸与手性取代恶唑酮为起始原料,进行酰胺缩合,迈克尔加成,水解,还原,分子内成环得到中间体(VII)。本发明的制备方法成本低,原料易得,产率较高,适于工业化生产。