Publication

Diastereoselective Synthesis of N-Heterocycle Substituted Cyclobutanes via Michael Addition onto Cyclobutenes

Jérôme Waser, Emma Gabrielle Louise Robert
2024
Journal Articles

Abstract

Herein, we present a method for the diastereoselective synthesis of N-heterocycle-substituted cyclobutanes from commercially available bromocyclobutanes. This method enables the efficient formation of various heterocyclic aminocyclobutane esters and amides using simple reagents. Notably, N-nucleophiles such as imidazoles, azoles, and nucleobase derivatives were successfully incorporated, enhancing the chemical diversity of small ring building blocks for medicinal chemistry applications.

Official source

https://infoscience.epfl.ch/entities/publication/fed7d1ef-e517-4363-9cdd-18d8e1cf603b

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