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通过串联还原胺化/内酰胺化序列高效合成γ-内酰胺

Efficient synthesis of gamma-lactams by a tandem reductive amination/lactamization sequence.

作者信息

Nöth Julica, Frankowski Kevin J, Neuenswander Benjamin, Aubé Jeffrey, Reiser Oliver

机构信息

Institut für Organische Chemie, Universität Regensburg, Universitätsstrasse 31, 93053 Regensburg, Germany.

出版信息

J Comb Chem. 2008 May-Jun;10(3):456-9. doi: 10.1021/cc700202c. Epub 2008 Mar 14.

Abstract

A three-component method for the synthesis of highly substituted gamma-lactams from readily available maleimides, aldehydes, and amines is described. A new reductive amination/intramolecular lactamization sequence provides a straightforward route to the lactam products in a single manipulation. The general utility of this method is demonstrated by the parallel synthesis of a gamma-lactam library.

摘要

本文描述了一种由易得的马来酰亚胺、醛和胺合成高度取代γ-内酰胺的三组分方法。一种新的还原胺化/分子内酰胺化序列通过单一操作提供了一条通向内酰胺产物的直接路线。γ-内酰胺库的平行合成证明了该方法的通用性。

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