Publication | Open Access
Amine Activation: Synthesis of <i>N</i>-(Hetero)arylamides from Isothioureas and Carboxylic Acids
43
Citations
34
References
2016
Year
Combinatorial ChemistryMedicinal ChemistryAmine ActivationClassical ProtocolsNatural SciencesDrug DiscoveryDiversity-oriented SynthesisMedicineOrganic ChemistryStereoselective SynthesisChemistryClassical Acid ActivationHeterocycle ChemistryPharmacologySynthesis MethodSynthetic ChemistryBiomolecular Engineering
A novel method for N-(hetero)arylamide synthesis based on rarely explored amine activation, rather than classical acid activation, is reported. The activated amines are easily prepared using a three-component reaction with commercial reagents. The new method shows a broad scope including challenging amides not (efficiently) accessible via classical protocols.
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