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Primary sulfonamide synthesis using the sulfinylamine reagent N-sulfinyl-O-(tert-butyl)hydroxylamine, t-BuONSO

Abstract:
Sulfonamides have played a defining role in the history of drug development and continue to be prevalent today. In particular, primary sulfonamides are common in marketed drugs. Here we describe the direct synthesis of these valuable compounds from organometallic reagents and a novel sulfinylamine reagent, t-BuONSO. A variety of (hetero)aryl and alkyl Grignard and organolithium reagents perform well in the reaction, providing primary sulfonamides in good to excellent yields in a convenient one-step process.
Publication status:
Published
Peer review status:
Peer reviewed

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Publisher copy:
10.1021/acs.orglett.0c03505

Authors


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Role:
Author
ORCID:
0000-0003-1054-1161
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Institution:
University of Oxford
Division:
MPLS
Department:
Chemistry
Role:
Author
ORCID:
0000-0002-8916-1454
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Role:
Author
ORCID:
0000-0001-7869-6835
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Institution:
University of Oxford
Department:
CHEMISTRY
Sub department:
Organic Chemistry
Role:
Author
ORCID:
0000-0002-0636-6471


Publisher:
American Chemical Society
Journal:
Organic Letters More from this journal
Volume:
22
Issue:
24
Pages:
9495-9499
Place of publication:
United States
Publication date:
2020-11-25
Acceptance date:
2020-11-19
DOI:
EISSN:
1523-7052
ISSN:
1523-7060
Pmid:
33237777


Language:
English
Keywords:
Pubs id:
1148019
Local pid:
pubs:1148019
Deposit date:
2021-02-12

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