Efficient Synthesis of Heterocyclic Neurotensin Receptor Ligands by Microwave-Assisted Aminocarbonylation

Christopher Lang; Peter Gmeiner

doi:10.1055/s-0033-1338497

Synthesis, Table of Contents

Synthesis 2013; 45(17): 2474-2480
DOI: 10.1055/s-0033-1338497

paper

Efficient Synthesis of Heterocyclic Neurotensin Receptor Ligands by Microwave-Assisted Aminocarbonylation

Christopher Lang

Department of Chemistry and Pharmacy, Emil Fischer Center, Friedrich Alexander University Erlangen-Nürnberg, Schuhstr. 19, 91052 Erlangen, Germany Fax: +49(9131)8522585 Email: peter.gmeiner@fau.de

,

Peter Gmeiner*

Department of Chemistry and Pharmacy, Emil Fischer Center, Friedrich Alexander University Erlangen-Nürnberg, Schuhstr. 19, 91052 Erlangen, Germany Fax: +49(9131)8522585 Email: peter.gmeiner@fau.de

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Abstract

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Abstract

Marking the heterocyclic neurotensin receptor antagonist SR142948A as a lead compound, the development of an efficient and a practical synthetic route to heterocyclic aryl carboxamides is reported. Thus, a highly efficient and flexible access to these carboxamides was elaborated by taking advantage of microwave-assisted aminocarbonylation reaction mediated by Mo(CO)₆, Herrmann’s palladacycle, [(t-Bu)₃PH]BF₄, and DBU.

Key words

aminocarbonylation - microwave - aryl bromide - palladium catalysis - palladacycles - medicinal chemistry

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References

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