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Bench-stable transfer reagent facilitates the generation of trifluoromethyl-sulfonimidamides

Abstract:

Sulfonimidamides are an emerging bioisosteric replacement in medicinal chemistry projects, and therefore new chemistries are necessary to access this functionality. The general synthesis of CF3-sulfonimidamides from an activated bench-stable transfer reagent is described. A diverse reaction scope is demonstrated, with a wide range of nucleophilic amines being tolerated in this transformation. The CF3-sulfonimidamides obtained contain an additional diversity point, in the form a protected imin...

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Publication status:
Published
Peer review status:
Peer reviewed
Version:
Accepted Manuscript

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Publisher copy:
10.1021/acs.joc.8b01244

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Institution:
University of Oxford
Division:
Medical Sciences Division
Department:
NDM
Subgroup:
Target Discovery Institute
Role:
Author
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Institution:
University of Oxford
Division:
Medical Sciences Division
Department:
NDM
Subgroup:
Target Discovery Institute
Oxford college:
Corpus Christi College
Role:
Author
ORCID:
0000-0002-8950-7646
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Role:
Author
ORCID:
0000-0002-4225-758X
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Bayer Pharma AG More from this funder
Boehringer Ingelheim More from this funder
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Publisher:
American Chemical Society Publisher's website
Journal:
Journal of organic chemistry Journal website
Volume:
83
Issue:
16
Pages:
9510–9516
Publication date:
2018-06-22
DOI:
EISSN:
1520-6904
ISSN:
0022-3263
Pubs id:
pubs:866270
URN:
uri:c096c74e-a436-4e9c-833c-ef88627813d0
UUID:
uuid:c096c74e-a436-4e9c-833c-ef88627813d0
Local pid:
pubs:866270
Language:
English

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