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

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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