铜
催化作用
联轴节(管道)
过程(计算)
组合化学
化学
工艺工程
材料科学
计算机科学
有机化学
冶金
工程类
操作系统
作者
Eric M. Phillips,Mikhail Reibarkh,John Limanto,Minh Kieu,Azzeddine Lekhal,Daniel Zewge
标识
DOI:10.1021/acs.oprd.9b00192
摘要
Verubecestat is a β-site amyloid precursor protein cleaving enzyme 1 (BACE1) inhibitor which was previously evaluated for the treatment of Alzheimer's disease. The synthesis of verubecestat relies on a Cu-catalyzed carbon–nitrogen coupling. During process development, observations of impurity formation led to a more robust understanding of the catalyst. The transformation was discovered to be highly dependent on the ratio of ligand to substrate concentration during the course of the reaction. In-depth studies aimed at attaining mechanistic understanding provided an explanation of experimental findings and ultimately led to the identification of conditions that resulted in a more robust process.
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