LEE, CHIA-YING,李家莹,李家瑩,HUANG, SHU TING,黄淑婷,黃淑婷,WANG, HSIN-CHI,王信琦,王信琦,LIAO, YUAN-XIU,廖苑秀,廖苑秀,GUO, JIUNN-CHEH,郭俊彻,郭俊徹,KUO, LUNG-HUANG,郭隆皇,郭隆皇
申请号:
TW105135465
公开号:
TW201718562A
申请日:
2016.11.02
申请国别(地区):
TW
年份:
2017
代理人:
摘要:
The present disclosure provides processes for preparing brexpiprazole. The present disclosure also provides processes for the purification of brexpiprazole. The processes for preparing and purifying brexpiprazole of the present invention provide substantial improvements over currently known methods. In certain embodiments, the conversion of Formula XI and XII to form XIII provides increased selectivity over previously reported methods. This offers increased yield and purity. The improved process for purifying brexpiprazole disclosed herein provides brexpiprazole with superior purity and is also more suitable for industrial production.本發明提供用於製備布瑞哌唑之方法。本發明亦提供用於純化布瑞哌唑之方法。本發明之該等用於製備及純化布瑞哌唑的方法提供相較於當前已知方法之大體上改進。在某些實施例中,式XI與式XII形成式XIII之轉化提供相較於先前報導方法之增加的選擇性。此提供增加之產率與純度。本文所揭示之用於純化布瑞哌唑的改良方法提供具有優良純度之布瑞哌唑且亦更適合於工業生產。