Pilot Scale Process Development of SL65.0102-10, an N-Diazabicyclo[2.2.2]-octylmethyl Benzamide

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• 作者：Philippe LienardPhilippe Gradoz ; Hélène Greciet ; Samir Jegham ; Didier Legroux
• 刊名：Organic Process Research & Development
• 出版年：2017
• 出版时间：January 20, 2017
• 年：2017
• 卷：21
• 期：1
• 页码：18-22
• 全文大小：285K
• ISSN：1520-586X

文摘

The process development and improvements for route selection, adapted to large scale for the pilot-scale preparation of SL65.0102-10, an N-diazabicyclo[2.2.2]-octylmethyl benzamide, a 5-HT₃ and 5-HT₄ receptor active ligand for the treatment of neurological disorders such as cognition impairment, are described in this article. Notable steps and enhancements are compared to the original route, including the improvement of a chiral epoxide synthesis by shortening the number of chemical steps, the deprotection of a quaternary ammonium salt, and the redesign of the final amidification coupling to avoid chromatography.