The Synthesis of Sterically Hindered Amides

Amide bond formation is one of the most important reactions due to the ubiquity of the amide functional group in pharmaceuticals and biologically active compounds. However, even the best existing methods reach their limits when it comes to the synthesis of sterically hindered amides. In th...

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Bibliographic Details
Main Authors: Gabriel Schäfer, Jeffrey W. Bode
Format: Article
Language:deu
Published: Swiss Chemical Society 2014-04-01
Series:CHIMIA
Subjects:
Online Access:https://www.chimia.ch/chimia/article/view/5553
Description
Summary:Amide bond formation is one of the most important reactions due to the ubiquity of the amide functional group in pharmaceuticals and biologically active compounds. However, even the best existing methods reach their limits when it comes to the synthesis of sterically hindered amides. In this article we summarize our research in the formation of sterically hindered amides. We show that the direct coupling of Grignard reagents to isocyanates provides a facile and robust solution to this long-standing challenge and hope that this methodology will find widespread application in the synthesis of pharmaceuticals and materials.
ISSN:0009-4293
2673-2424