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Synthesis, functionalization, and reactivity of vinyl sulfondiimidamides

Abstract:

Acrylamides are the dominant electrophilic warheads used in bioactive covalent inhibitors. A limitation of acrylamides, and related unsaturated sulfonamides, is the narrow scope to modulate their electrophilicity, and hence reactivity, through simple structural modification. Here, we show that vinyl sulfondiimidamides are effective electrophilic motifs for reaction with both sulfur- and nitrogenbased biologically relevant nucleophiles. We demonstrate that the electrophilicity of these new reagents can be tuned through variation of the imidic N-substituents. Vinyl sulfondiimidamides are prepared via a short sequence that features a Cope elimination as the key alkene-forming step. A broad range of N-substituents can be installed.

Publication status:
Published
Peer review status:
Peer reviewed

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Publisher copy:
10.1002/anie.9885717

Authors

More by this author
Institution:
University of Oxford
Division:
MPLS
Department:
Chemistry
Sub department:
Chemistry Research Laboratory
Role:
Author
More by this author
Institution:
University of Oxford
Division:
MPLS
Department:
Chemistry
Sub department:
Chemistry Research Laboratory
Role:
Author
More by this author
Institution:
University of Oxford
Division:
MPLS
Department:
Chemistry
Sub department:
Chemistry Research Laboratory
Role:
Author


Publisher:
Wiley
Journal:
Angewandte Chemie International Edition More from this journal
Article number:
e9885717
Publication date:
2026-03-28
Acceptance date:
2026-03-12
DOI:
EISSN:
1521-3773
ISSN:
1433-7851


Language:
English
Keywords:
Pubs id:
2388056
Local pid:
pubs:2388056
Deposit date:
2026-03-11
ARK identifier:

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