- Microwave-assisted catalytic method for a green synthesis of amides directly from amines and carboxylic acids
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Amide bonds are among the most interesting and abundant molecules of life and products of the chemical pharmaceutical industry. In this work, we describe a method of the direct synthesis of amides from carboxylic acids and amines under solvent-free conditions using minute quantities of ceric ammonium nitrate (CAN) as a catalyst. The reactions are carried out in an open microwave reactor and allow the corresponding amides to be obtained in a fast and effective manner when compared to other procedures of the direct synthesis of amides from acids and amines reported so far in the literature. The amide product isolation procedure is simple, environmentally friendly, and is performed with no need for chromatographic purification of secondary amides due to high yields. In this report, primary amines were used in most examples. However, the developed procedure seems to be applicable for secondary amines as well. The methodology produces a limited amount of wastes, and a catalyst can be easily separated. This highly efficient, robust, rapid, solvent-free, and additional reagent-free method provides a major advancement in the development of an ideal green protocol for amide bond formation.
- Kolanowski, Jacek L.,Markiewicz, Wojciech T.,Zarecki, Adam P.
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supporting information
(2020/04/23)
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- DIARYL ETHERS AS OPIOID RECEPTOR ANTAGONIST
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A compound of the formula (I) wherein the variables X1 to X10, R1 to R7 including R3', E, v, y, z, A and B are as described, or a pharmaceutically acceptable salt, solvate, enantiomer, racemate, diastereomer or mixtures thereof, useful for the treatment, prevention or amelioration of obesity and Related Diseases is disclosed.
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Page/Page column 92
(2008/06/13)
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- New oxidative transformations of phenolic and indolic oxazolines: An avenue to useful azaspirocyclic building-blocks
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The oxidative cyclization of a phenolic amide to a spirolactam has long been regarded as an 'impossible' reaction, because exposure of the substrates to a variety of oxidants results in formation of spirolactones with consequent loss of the amine segment. We recently communicated that this heretofore unknown transformation may be achieved by oxidation of oxazoline analogues of phenolic and indolic amides. Herein, we provide full details of our work.
- Braun, Norbert A.,Ousmer, Malika,Bray, Jonathan D.,Bouchu, Denis,Peters, Karl,Peters, Eva-Maria,Ciufolini, Marco A.
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p. 4397 - 4408
(2007/10/03)
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- DERIVATIVES OF 3-AMINOPROPANE-1,2-DIOL
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Derivatives of 3-aminopropane-1,2-diol of the formula STR1 in which Ar represents optionally substituted aryl,n represents the number 0 or 1, andalk represents alkylene having 2 to 5 carbon atoms, the nitrogen atom and the oxygen atom, or, if n is zero, the phenyl radical, being separated from one another by at least two carbon atoms, andR 1 and R. sub.2, independently of one another, each represents hydrogen or lower alkyl, or together they represent lower alkylene, oxa-lower alkylene, thia-lower alkylene, aza-lower alkylene or N-lower alkyl-aza-lower alkylene,and salts of such compounds, processes for their manufacture, medicaments containing the new compounds and their use for the treatment of Angina pectoris and cardiac arrhythmia, and as blood pressure-reducing agents, as well as for the treatment of reactive or endogenic states of depression.
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- Derivatives of 3-aminopropane-1,2-diol
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Derivatives of 3-aminopropane-1,2-diol of the formula STR1 in which Ar represents optionally substituted aryl, n represents the number 0 or 1, and alk represents alkylene having 2 to 5 carbon atoms, the nitrogen atom and the oxygen atom, or, if n is zero, the phenyl radical, being separated from one another by at least two carbon atoms, and R1 and R2, independently of one another, each represents hydrogen or lower alkyl, or together they represent lower alkylene, oxa-lower alkylene, thia-lower alkylene, aza-lower alkylene or N-lower alkyl-aza-lower alkylene, and salts of such compounds, processes for their manufacture, medicaments containing the new compounds and their use for the treatment of Angina pectoris and cardiac arrhythmia, and as blood pressure-reducing agents, as well as for the treatment of reactive or endogenic states of depression.
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