An Improved Process for the Preparation of Highly Pure Solifenacin Succinate via Resolution through Diastereomeric Crystallisation

详细信息    查看全文

• 作者：Ganala Naga Trinadhachari ; Anand Gopalkrishna Kamat ; Boddu Venkata Balaji ; Koilpillai Joseph Prabahar ; Kolukuluru Mohan Naidu ; Korupolu Raghu Babu ; Paul Douglas Sanasi
• 刊名：Organic Process Research & Development
• 出版年：2014
• 出版时间：August 15, 2014
• 年：2014
• 卷：18
• 期：8
• 页码：934-940
• 全文大小：385K
• ISSN：1520-586X

文摘

An improved process for the preparation of solifenacin succinate (1) involving resolution through diastereomeric crystallization is described. (1S)-IQL derivative (5) is esterified to form (1S)-ethoxycarbonyl IQL derivative (6) which is condensed with (RS)-3-quinuclidinol (7) to form a solifenacin diastereomeric mixture (8); this is subjected to resolution through diastereomeric crystallization to produce solifenacin succinate (1), which is used for the treatment of an overactive bladder.