Rapid sp3-Enriched Scaffold Generation via a Selective Aziridine Amide Ring-Opening Reaction
Masahito Abe,
Jeremy S. Coleman,
Christopher C. Presley
et al.
Abstract:Sp 3 -enriched small molecules play a critical role in developing drug candidates. While designing analogues with greater sp 3 character, a methodology utilizing a less explored cyclic-aziridine amide ring-opening reaction to generate sp 3enriched scaffolds has been developed and reported. This methodology enables rapid access to substructures with higher fsp 3 values, attracting greater attention within the past few decades. The reaction exhibits a wide reaction scope, featuring a highly sterically hindered p… Show more
scite is a Brooklyn-based organization that helps researchers better discover and understand research articles through Smart Citations–citations that display the context of the citation and describe whether the article provides supporting or contrasting evidence. scite is used by students and researchers from around the world and is funded in part by the National Science Foundation and the National Institute on Drug Abuse of the National Institutes of Health.