Synthesis 2019; 51(07): 1643-1648
DOI: 10.1055/s-0037-1610674
paper
© Georg Thieme Verlag Stuttgart · New York

Morpholin-2-one Derivatives via Intramolecular Acid-Catalyzed Hydroamination

,
David W. Knight*
School of Chemistry, Cardiff University, Park Place, Cardiff, CF10 3AT, UK   Email: knightdw@cf.ac.uk   Email: wirth@cf.ac.uk
,
School of Chemistry, Cardiff University, Park Place, Cardiff, CF10 3AT, UK   Email: knightdw@cf.ac.uk   Email: wirth@cf.ac.uk
› Author Affiliations
Further Information

Publication History

Received: 06 September 2018

Accepted after revision: 06 November 2018

Publication Date:
07 January 2019 (online)


Abstract

Substituted morpholin-2-one derivatives were readily obtained in two steps starting from commercially available N-protected amino acids. In a metal-free and practical method, a catalytic amount of trifluoromethanesulfonic acid was sufficient to generate morpholinones under mild reaction conditions in an intramolecular hydroamination reaction in good to excellent yields.

Supporting Information