METHOD FOR PREPARING NILUTAMIDE AND INTERMEDIATE THEREOF

Disclosed is a method for preparing nilutamide and an intermediate thereof. The method comprises the following steps: at a temperature of 25 °C to 160 °C, using 4-nitro-3-trifluoromethylaniline represented by formula (I) and a compound represented by formula (II) with an amino protecting group PG as...

Ausführliche Beschreibung

Gespeichert in:
Bibliographische Detailangaben
Hauptverfasser: LI, Linwu, YU, Sijie, LI, Chenye, SHAO, Lei, ZENG, Wanjing, SONG, Yingwei, MENG, Xiangguo, WU, Kai, WANG, Luyi, YIN, Zixin, CHANG, Renjun, WANG, Yijing, HU, Xiamin, SHI, Yuhao
Format: Patent
Sprache:chi ; eng ; fre
Schlagworte:
Online-Zugang:Volltext bestellen
Tags: Tag hinzufügen
Keine Tags, Fügen Sie den ersten Tag hinzu!
Beschreibung
Zusammenfassung:Disclosed is a method for preparing nilutamide and an intermediate thereof. The method comprises the following steps: at a temperature of 25 °C to 160 °C, using 4-nitro-3-trifluoromethylaniline represented by formula (I) and a compound represented by formula (II) with an amino protecting group PG as raw materials to conduct a condensation reaction and a ring-closing reaction to generate a compound represented by formula (III) and subjecting the compound represented by formula (III) to a direct ring closure without purification to generate nilutamide (formula IV); or subjecting the compound represented by formula (III) to a ring closure to prepare nilutamide. The present invention features short reaction steps, simple operation, high yield, and moderate reaction conditions, and uses cheap and readily available reagents, thus being suitable for both small-scale laboratory preparation and large-scale industrial production. Using the route described above, a new method for constructing a hydantoin ring is provide