A practical method for the amidation of aldehydes with economic ammonium chloride or amine hydrochloride salts has been developed for the synthesis of a wide variety of amides by using inexpensive copper sulfate or copper(I) oxide as a catalyst and aqueous tert-butyl hydroperoxide as an oxidant. This amidation reaction is operationally straightforward and provides primary, secondary, and tertiary amides in good to excellent yields for most cases utilizing inexpensive and readily available reagents under mild conditions. In situ formation of amine salts from free amines extends the substrate scope of the reaction. Chiral amides are also synthesized from their corresponding chiral amines without detectable racemization. The practicality of this amide formation reaction has been demonstrated in an efficient synthesis of the antiarrhythmic drug N-acetylprocainamide.
Pd
nanoparticles supported on ZIF-8 (PdNPs/ZIF-8) are described as an
efficient heterogeneous catalyst for the aminocarbonylation of bromoarenes
in the presence of phosphines and iodoarenes under phosphine-free
conditions. The catalyst can be readily prepared and is air-stable.
The palladium loading can be as low as 1 wt %, and the catalyst was
recycled four times with negligible change in catalytic performance.
A variety of pharmaceutically important amides was readily synthesized.
A TON of 2540 was easily achieved in a batch reaction by scaling up
to a gram scale. The catalyst reported can also be applied to the
synthesis of cyclic and primary amides as well as an alkoxycarbonylation
reaction to form an ester.
A practical and efficient method for the synthesis of amides has been developed by iron‐catalysed oxidative amidation of aldehydes with amine hydrochloride salts. A wide range of amides have been obtained in good to excellent yields under mild conditions. The application of this novel amide formation reaction to the synthesis of pharmaceutical compounds has been successfully demonstrated.
Mesoporous niobium oxide spheres (MNOS), conveniently prepared by a novel antisolvent precipitation approach, have been shown to be an effective catalyst for the transamidation of primary amides with amines. This novel transamidation can be efficiently carried out under solvent-free conditions and is applicable to a wide range of primary amides and amines to provide N-alkyl amides in good to excellent yields. The catalyst is highly stable and reusable. The application of this transamidation reaction has been demonstrated in the synthesis of antidepressant drug moclobemide and other druglike compounds.
scite is a Brooklyn-based organization that helps researchers better discover and understand research articles through Smart Citations–citations that display the context of the citation and describe whether the article provides supporting or contrasting evidence. scite is used by students and researchers from around the world and is funded in part by the National Science Foundation and the National Institute on Drug Abuse of the National Institutes of Health.