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Stereoselective Synthesis of (E)-Enol Borinates via Borylation of Lithum Enolates

Date

2019-01-25

Journal Title

Journal ISSN

Volume Title

Publisher

ORCID

0000-0003-1050-423X

Type

Thesis

Degree Level

Masters

Abstract

Aldol reactions of enol borinates constitute one the most powerful and reliable methods for asymmetric synthesis. Crucial to this success is the stereoselective preparation of enol borinates and ‘soft enolization’ is by far the most popular method; however, limitations in substrate scope have been reported, particularly with sterically hindered ketones and those incompatible with the Lewis acidic reagents. Borylation of lithium enolates was found to be a general and efficient approach to enol borinates that can overcome many of the above limitations. Under appropriate conditions, the (E)-enol borinate is produced with high diastereoselectivity regardless of the starting geometry of the precursor Li enolate. The mechanism of the underlying isomerization process is unusual. The method has been implemented successfully across a range of ketone substrates and is complementary to ‘soft enolization’ with the advantages that reactivity is dependent on lithium enolate formation and stereoselectivity is independent of the geometry of lithium enolate.

Description

Keywords

Stereoselective, (E)-Enol Borinates, Borylation, Lithum Enolates

Citation

Degree

Master of Science (M.Sc.)

Department

Chemistry

Program

Chemistry

Part Of

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DOI

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