- Efficient Synthesis of Nicotinic Acid Based Pseudopeptides Bearing an Amidoxime Function
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The synthesis of nicotinic acid based amino acid units bearing an amidoxime function on the pyridine ring has been developed. The starting 2-cyanonicotinic acid was efficiently coupled with methyl esters of l-α-amino acids to afford intermediate 2-cyanopyridin-3-yl-containing pseudopeptides together with the tautomeric methyl esters of (2S)-2-(7-imino-5-oxo-5,7-dihydro-6H-pyrrolo[3,4-b]pyridin-6-yl)alkanoic acids. Regioselective pyrrolidine ring opening of these esters occurred upon hydroxylamine hydrochloride treatment, giving rise to the open-chain pyridin-3-yl 2-amidoxime pseudopeptides bearing the same structure as amidoximes obtained by direct hydroxyamination of the corresponding cyano esters.
- Ovdiichuk, Olga V.,Hordiyenko, Olga V.,Medviediev, Volodymyr V.,Shishkin, Oleg V.,Arrault, Axelle
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- Cyclic acyl amidines as unexpected C4-donors for fully substituted pyridine ring formation in the base mediated reaction with malononitrile
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A new one-step, pseudo four-component approach for the synthesis of fully substituted pyridines via ring-opening of the cyclic acyl amidine of 3-amino-1H-isoindol-1-one and its aza-analogues during the reaction with malononitrile in the presence of sodium methoxide, followed by pyridine ring closure is reported. This method allows the one-step preparation of previously unknown 2-(pyridin-4-yl)(hetero)aryl carboxamides in good yields under mild reaction conditions.
- Tkachuk, Volodymyr,Merkulova, Vladyslava,Omelchenko,Arrault, Axelle,Hordiyenko, Olga
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supporting information
p. 1959 - 1963
(2019/06/27)
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- Method for synthesizing 2-aminopyridin-3-carboxylic acid
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The invention discloses a method for synthesizing 2-aminopyridin-3-carboxylic acid. The method utilizes 2, 3-pyridinedicarboxylic acid, acetic anhydride, ammonia water, hydrochloric acid, sodium hydroxide, bromine, 2-amidopyridin-3-carboxylic acid, CNTs and SnCl2.2H2O as main raw materials. Through ammonium acetate solution washing and sulfuric acid sulfonation, SnO2 of the coating layer is converted into solid super acid S-SnO2 so that the stability of the system is improved and the catalytic activity of the catalyst is improved. The method utilizes cheap and easily available raw materials, is safe in operation, realizes simple separation and purification and a high product yield and is suitable for large-scale preparation.
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Paragraph 0008; 0029
(2019/01/08)
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- Pyridazinedione compounds useful in treating neurological disorders
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The present invention relates to pyridazino[4,5-b]quinolines, and pharmaceutically useful salts thereof, which are excitatory amino acid antagonists and which are useful when such antagonism is desired such as in the treatment of neurological disorders. The invention further provides pharmaceutical compositions containing pyridazino[4,5-b]quinolines as active ingredient, and methods for the treatment of neurological disorders.
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- Preparation of substituted and unsubstituted 2-carbamoyl nicotinic and 3-quinolinecarboxylic acids
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The invention provides a process for the preparation of substituted and unsubstituted 2-carbamoyl nicotinic and 3-quinolinecarboxylic acids.
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- PREPARATION AND STRUCTURAL ASSIGNMENTS OF SOME ISOMERIC 2,3-DISUBSTITUTED PYRIDINES
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The preparation of several isomeric 2,3-disubstituted pyridine compounds are described and their spectroscopical data given.IR and NMR spectra of quinolinimide, reported by Distefano et al., are contradicted.The electron impact mass spectra are found to be useful in the differentiation between positional isomers.
- Spiessens, Luc I. M.,Anteunis, Marc J. O.
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p. 205 - 232
(2007/10/02)
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- Antisecretory 4-oxy-3-carboxy or cyano-1,2-dihydro-2-oxo-1,8-naphthyridine derivatives
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Substituted 4-oxy-3-carboxy or cyano-1,2-dihydro-2-oxo-1,8-naphthyridine derivatives as gastric antisecretory agents for use in the treatment of peptic ulcer disease.
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