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Base-activated latent heteroaromatic sulfinates as nucleophilic coupling partners in palladium-catalyzed cross-coupling reactions

Abstract:
Heteroaromatic sulfinates are effective nucleophilic reagents in Pd0-catalyzed cross-coupling reactions with aryl halides. However, metal sulfinate salts can be challenging to purify, solubilize in reaction media, and are not tolerant to multi-step transformations. Here we introduce base-activated, latent sulfinate reagents: β-nitrile and β-ester sulfones. We show that under the cross-coupling conditions, these species generate the sulfinate salt in situ, which then undergo efficient palladium-catalyzed desulfinative cross-coupling with (hetero)aryl bromides to deliver a broad range of biaryls. These latent sulfinate reagents have proven to be stable through multi-step substrate elaboration, and amenable to scale-up.
Publication status:
Published
Peer review status:
Peer reviewed

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Publisher copy:
10.1002/anie.202109146

Authors


Publisher:
Wiley
Journal:
Angewandte Chemie International Edition More from this journal
Volume:
60
Issue:
41
Pages:
22461-22468
Publication date:
2021-09-08
Acceptance date:
2021-07-30
DOI:
EISSN:
1521-3773
ISSN:
1433-7851
Pmid:
34342107


Language:
English
Keywords:
Pubs id:
1190410
Local pid:
pubs:1190410
Deposit date:
2021-09-07
ARK identifier:

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