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Synthesis of enantioenriched α-chiral bicyclo[1.1.1]pentanes

Abstract:
Bicyclo[1.1.1]pentanes (BCPs), useful surrogates for para-substituted arenes, alkynes, and tert-butyl groups in medicinal chemistry, are challenging to prepare when featuring stereogenic centers adjacent to the BCP. We report the development of an efficient route to α-chiral BCPs, via highly diastereoselective asymmetric enolate functionalization. We also describe the application of this chemistry to the synthesis of BCP analogues of phenylglycine and tarenflurbil, the single enantiomer of the NSAID flurbiprofen.
Publication status:
Published
Peer review status:
Peer reviewed

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Publisher copy:
10.1021/acs.orglett.9b00691

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Institution:
University of Oxford
Division:
MPLS
Department:
Chemistry
Sub department:
Organic Chemistry
Oxford college:
Jesus College
Role:
Author
ORCID:
0000-0002-4149-0494
Publisher:
American Chemical Society Publisher's website
Journal:
Organic Letters Journal website
Volume:
21
Issue:
7
Pages:
2408-2411
Publication date:
2019-03-14
Acceptance date:
2019-03-14
DOI:
EISSN:
1523-7052
ISSN:
1523-7060
Pmid:
30869907
Language:
English
Keywords:
Pubs id:
pubs:983441
UUID:
uuid:0b13041e-08a3-4ba1-8f47-69143e87fcb5
Local pid:
pubs:983441
Source identifiers:
983441
Deposit date:
2019-05-17

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