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Squarate desymmetrisation–ozonolysis as an approach to β-substituted-α-ketosuccinates and squalestatin synthesis

Abstract:

Silylated tertiary alcohols from 1,2-addition of alkyllithiums to dialkyl squarates undergo alkene ozonolysis to give β-substituted-α-keto-β-(silyloxy)succinates. With 3-(triethylsilyloxy)butyllithium the methodology was applied to the 2,8-dioxabicyclo[3.2.1]octane core of the squalestatins. Enantioselective 1,2-addition to di-tert-butyl squarate using butyllithium or diethylzinc/Ti(iPrO)4 in the presence of chiral ligands (such as bisoxazolines or camphorsulfonamides, respectively) gave the ...

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Publication status:
Published
Peer review status:
Peer reviewed

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Publisher copy:
10.1016/j.tet.2019.130747

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Institution:
University of Oxford
Division:
MPLS
Department:
Chemistry
Sub department:
Organic Chemistry
Oxford college:
Oriel College
Role:
Author
Publisher:
Elsevier
Journal:
Tetrahedron More from this journal
Volume:
75
Issue:
50
Article number:
130747
Publication date:
2019-11-05
Acceptance date:
2019-10-24
DOI:
EISSN:
1464-5416
ISSN:
0040-4020
Language:
English
Keywords:
Pubs id:
pubs:1077281
UUID:
uuid:da4d3ee3-b2f4-43b1-bb4b-864108faaf13
Local pid:
pubs:1077281
Source identifiers:
1077281
Deposit date:
2019-12-15

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