摘要
介绍了盐酸度洛西汀的特性和用途,叙述了近年来度洛西汀的13种合成方法,并评述了其优缺点。指出所有这些路线的主要区别在于调整了中间体的合成方法:将不能利用的(R)-中间体消旋,手性合成(S)-中间体,(R)-中间体制备盐酸度洛西汀。并认为应在2013年盐酸度洛西汀的物质专利到期前开发出一条有竞争力的路线,并提出了一条可能的路线。
The characteristics and use of duloxetine hydrochloride were introduced and 13 process methods of it in recent years and their advantages and disadvantages were reviewed in this paper.It was pointed out that the major difference in all the routes was the adjustment of the synthesis of intermediates,such as racemization of (r)-intemediate;asymmetric synthesis of (s)-intermediate;the preparation of duloxetine from (r)-intermediate.It was suggested to develop a new route before the expiration of the substance patent duration of duloxetine hydrochloride in 2013 and a possible route was advised.
出处
《化工生产与技术》
CAS
2009年第4期51-55,共5页
Chemical Production and Technology
