Synthesis of verubecestat as a BACE inhibitor
RAO Yan
GUO Ya-jun
ZHU Xue-yan
LIU Xiang-kui
Abstract：Objective:To synthesize verubecestat,and optimize its process.Methods:Using p-methoxybenzaLdehyde as starting material,N-{ 3-[(5R)-2H-3-amino-5,6-dihydro-1,1-dioxido-1,2,4-thiadiazin-5-yL]-4-fluorophenyl｝-5-fluoro-2-pyridinecarboxamide,an important small molecular BACE inhibitor,verubecestat has been synthesized through 10 steps in this article.Results:The structure of verubecestat has been verified by 1H-NMR and ESI-MS.Conclusion:The improved process has mild reaction condition,which is very suitable for the lab-scale production.
Keywords：BACE inhibitorsverubecestatsynthesis
Publication Date：2017-01-01
Online Publishing Date：2026-08-14(First online date of this platform, not the publication date of the document)
Pages：6( 2834-2839 )