Pilot Scale Process Development of SL65.0102-10, an N-Diazabicyclo[2.2.2]-octylmethyl Benzamide
Sanofi-Aventis, Recherche& Développement, 13 Quai Jules Guesde, 94400 Vitry-sur-Seine, France
Org. Process Res. Dev., 2017, 21 (1), pp 18–22
DOI: 10.1021/acs.oprd.6b00262
Publication Date (Web): December 14, 2016
Copyright © 2016 American Chemical Society
*E-mail: Philippe.Lienard@sanofi.com.
Abstract
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.
Supporting Information
The Supporting Information is available free of charge on the ACS Publications website at DOI: 10.1021/acs.oprd.6b00262.
Metrics
+
More Article Metrics 
ACS News
Quebec shooting victim was a chemist
Khaled Belkacemi was doing research on green chemistry and functional foodsWatch How Researchers Unraveled the Secret of Water Striders’ Skills
Water striders’ ability to walk on water mystified researchers for generations, but now new ...Trump meets with pharmaceutical industry executives
Drug prices, the approval process, and manufacturing jobs were the focus
0 件のコメント:
コメントを投稿