Synthesis of Aminocyclopropanes by Redox‐Neutral Aminoalkylation
A redox-neutral hydroaminoalkylation strategy has been developed for the synthesis of 1,1-disubstituted aminocyclopropanes from alkenes and alkynes. Through simple solvolysis activation, the reaction of an easily accessible, bench-stable hemiaminal precursor allows excellent yields of the target products at ambient temperature. The approach presented herein has a substrate tolerance that is orthogonal to classical aminocyclopropane syntheses, and its deployment for the preparation of bioisosteres of pharmacologically active gem-α-dimethylamines resulted in improved biological properties.
Authors
- Gwyndaf A. Oliver (ORCID: https://orcid.org/0000-0002-2936-6175)
- Konstantin Günther (ORCID: https://orcid.org/0000-0002-3874-1301)
- Harald H. Sitte (ORCID: https://orcid.org/0000-0002-1339-7444)
- Nuno Maulide (ORCID: https://orcid.org/0000-0003-3643-0718)
- Sophie Woolford (ORCID: https://orcid.org/0009-0001-2762-9023)
- Chiara Sebastianelli-Schoditsch (ORCID: https://orcid.org/0009-0006-6973-9972)
- Iina Ludwig
Institutions
- Al-Ahliyya Amman University (JO)
- University of Vienna (AT)
- Austrian Academy of Sciences (AT)
- CeMM Research Center for Molecular Medicine (AT)
- Institute of Organic Chemistry (HU)
- Medical University of Vienna (AT)
Publication Details
- Journal
- Angewandte Chemie International Edition
- Published
- 2026-09-04
- DOI
- https://doi.org/10.1002/anie.8092854
- Primary Topic
- Cyclopropane Reaction Mechanisms
- Type
- article
- Field-Weighted Citation Impact
- 0.00
Funders
- European Commission
- Austrian Science Fund
- Universität Wien
- Medizinische Universität Wien
- European Research Council