Chemistry Letters
Online ISSN : 1348-0715
Print ISSN : 0366-7022
Letter
Formal Synthesis of Ezetimibe Using a Proline-mediated, Asymmetric, Three-component Mannich Reaction
Yasuharu ShimasakiSeitaro KoshinoYujiro Hayashi
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2016 Volume 45 Issue 1 Pages 30-32

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Abstract

The formal total synthesis of ezetimibe was accomplished using a proline-mediated, asymmetric, three-component Mannich reaction as the key step. The two stereogenic centers on the β-lactam skeleton of ezetimibe were controlled by the syn-selective asymmetric Mannich reaction, followed by isomerization.

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© 2016 The Chemical Society of Japan
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