- Mechanochemical catalytic transfer hydrogenation of aromatic nitro derivatives
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Mechanochemical ball milling catalytic transfer hydrogenation (CTH) of aromatic nitro compounds using readily available and cheap ammonium formate as the hydrogen source is demonstrated as a simple, facile and clean approach for the synthesis of substituted anilines and selected pharmaceutically relevant compounds. The scope of mechanochemical CTH is broad, as the reduction conditions tolerate various functionalities, for example nitro, amino, hydroxy, carbonyl, amide, urea, amino acid and heterocyclic. The presented methodology was also successfully integrated with other types of chemical reactions previously carried out mechanochemically, such as amide bond formation by coupling amines with acyl chlorides or anhydrides and click-type coupling reactions between amines and iso(thio)cyanates. In this way, we showed that active pharmaceutical ingredients Procainamide and Paracetamol could be synthesized from the respective nitro-precursors on milligram and gram scale in excellent isolated yields.
- Portada, Tomislav,Margeti?, Davor,?trukil, Vjekoslav
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supporting information
(2018/12/11)
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- A catalyst-free, waste-less ethanol-based solvothermal synthesis of amides
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A green, one-pot approach based on the solvothermal amidation of carboxylic acids with amines has been developed for the synthesis of diverse aliphatic and aromatic amides. It does not require the use of catalysts or coupling reagents and it occurs in the presence of ethanol that has been proved to have a key role in the process. The proposed strategy is also extendable to biologically active amides and could represent a low-cost and waste-less alternative to the common synthetic pathways.
- Dalu, Francesca,Scorciapino, Mariano A.,Cara, Claudio,Luridiana, Alberto,Musinu, Anna,Casu, Mariano,Secci, Francesco,Cannas, Carla
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supporting information
p. 375 - 381
(2018/02/07)
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- ORGANIC REACTIONS CARRIED OUT IN AQUEOUS SOLUTION IN THE PRESENCE OF A HYDROXYALKYL(ALKYL)CELLULOSE OR AN ALKYLCELLULOSE
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The present invention relates to a method of carrying out an organic reaction in aqueous solution in the presence of a hydroxyalkyl(alkyl)cellulose or an alkylcellulose.
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- Ammonium nitrate: A biodegradable and efficient catalyst for the direct amidation of esters under solvent-free conditions
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A simple, metal-free, and environment-friendly procedure is developed for the direct conversion of esters to amides using ammonium nitrate as a catalyst under solvent-free conditions. Aryls, heteroaryls, and aliphatic esters are easily converted to the corresponding amides in excellent isolated yields (85-99%). An enantiopure ester and amine were both shown to react without racemization. The methodology has been successfully applied to preparation of procainamide.
- Ramesh, Perla,Fadnavis, Nitin W.
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p. 138 - 140
(2015/02/19)
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- Sulphuric acid immobilized on silica gel (H2SO4-SiO2) as an eco-friendly catalyst for transamidation
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A novel method of transamidation of carboxamides with amines by using catalytic amounts of H2SO4-SiO2 has been developed under solvent free conditions. The transamidation is compatible with a wide range of aromatic, heteroaromatic, aliphatic, cyclic/acyclic primary or secondary amines. The metal/solvent-free conditions represent a significant improvement over other existing methods as the reaction can be performed in open air conditions and no column purification is required. The versatility of this methodology was further demonstrated by synthesizing the commercially available drug procainamide.
- Rasheed,Rao, D. Nageswar,Reddy, A. Siva,Shankar, Ravi,Das, Parthasarathi
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p. 10567 - 10574
(2015/02/05)
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- Direct amide synthesis from equimolar amounts of carboxylic acid and amine catalyzed by mesoporous silica SBA-15
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Direct amide synthesis from equimolar amounts of carboxylic acid and amine using mesoporous silica as a versatile heterogeneous catalyst is reported.
- Tamura, Mizuki,Murase, Daisuke,Komura, Kenichi
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supporting information
p. 769 - 776
(2015/03/14)
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- An azobenzene-containing metal-organic framework as an efficient heterogeneous catalyst for direct amidation of benzoic acids: Synthesis of bioactive compounds
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An azobenzene-containing zirconium metal-organic framework was demonstrated to be an effective heterogeneous catalyst for the direct amidation of benzoic acids in tetrahydrofuran at 70°C. This finding was applied to the synthesis of several important, representative bioactive compounds.
- Hoang, Linh T. M.,Ngo, Long H.,Nguyen, Ha L.,Nguyen, Hanh T. H.,Nguyen, Chung K.,Nguyen, Binh T.,Ton, Quang T.,Nguyen, Hong K. D.,Cordova, Kyle E.,Truong, Thanh
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supporting information
p. 17132 - 17135
(2015/12/04)
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- Chemoselective reductions of nitroaromatics in water at room temperature
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A robust and green protocol for the reduction of functionalized nitroarenes to the corresponding primary amines has been developed. It relies on inexpensive zinc dust in water containing nanomicelles derived from the commercially available designer surfactant TPGS-750-M. This mild process takes place at room temperature and tolerates a wide range of functionalities. Highly selective reductions can also be achieved in the presence of common protecting groups.
- Kelly, Sean M.,Lipshutz, Bruce H.
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- PYRAZOLOPYRIMIDINES AS CELL CYCLE KINASE INHIBITORS
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This invention comprises the novel compounds of formula (I) wherein R1, R2, R3, R4, R5, R6, X1 and X2 have defined meanings, having cell cycle kinase inhibiting enzymatic activity, their preparation, compositions containing them and their use as a medicine.
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Page/Page column 42
(2008/06/13)
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- Synthesis and application of procainamide analogs for use in an immunoassay
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The present invention relates to immobilized procainamide analogs, as well as to a method of making immobilized procainamide analogs. These immobilized analogs are prepared by activating the carboxyl group on a substituted p-benzoic acid derivative toward nucleophilic attack; reacting the activated benzoic acid derivative with a polyamine to produce the benzoic acid derivative of Formula 3: and binding the benzoic acid derivative of Formula 3 to a latex polymer having functional groups that react with aliphatic amino groups. A method of conducting an immunoassay using the immobilized procainamide analog Formula 3 is described, comprising the steps of preparing a solution comprising said immobilized procainamide analog; adding a sample suspected of containing procainamide to said solution; adding an anti-procainamide antibody to said solution and observing the rate of increase in solution turbidity following antibody addition.
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- 2-Hydroxy-5-phenylazobenzoic acid derivatives and method of treating ulcerative colitis therewith
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The present invention provides a pharmaceutical composition for treating ulcerative colitis containing at least one compound of the general formula: STR1 wherein X is an --SO2 -- or --CO-- group and R is either an unsubstituted or substituted non-heterocyclic aromatic ring system or is a radical of the general formula --(CH2)n --Y, in which Y is a hydroxyl group, an unsubstituted or substituted amino group or a carboxylic or sulphonic acid group and n is a whole number of from 1 to 6 and in which one or more hydrogen atoms in the alkylene radical can be replaced by unsubstituted or substituted amino groups or alkyl radicals and in which the --(CH2)n --Y radical is either attached directly to the nitrogen atom or via a benzene ring; and/or containing at least one ester thereof and/or at least one non-toxic, pharmaceutically acceptable salt thereof, in admixture with a solid or liquid pharmaceutical diluent or carrier. Furthermore, the present invention provides a process for preparing the compounds of the above-given general formulae and also provides a method of treating ulcerative colitis.
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