- Enthalpies of combustion of the three hydroxy-pyridines and the four hydroxy-2-methylpyridines
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The enthalpies of combustion in oxygen at 298.15 K were measured in a static-bomb calorimeter and the enthalpies of sublimation at 298.15 K were measured by microcalorimetry for the following crystalline compounds: .The derived enthalpies of formation of the gaseous compounds are compared with theoretically predicted values for certain of these compounds.
- Suradi, S.,Saiad, Nabila el,Pilcher, G.,Skinner, H. A.
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Read Online
- 2-methyl-4-bromopyridine preparation method
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The invention belongs to the field of organic synthesis, and particularly relates to a 2-methyl-4-bromopyridine preparation method, which comprises: (1) carrying out a reaction on diethyl malonate andan alkali metal to generate a salt, adding a toluene solution of 2-chloro-4-nitropyridine in a dropwise manner, carrying out a condensation reaction, and decarboxylating under acidic conditions to obtain 2-methyl-4-nitropyridine; (2) carrying out hydrogenation reduction on the 2-methyl-4-nitropyridine under the catalysis of Pd/C by using methanol as a solvent, carrying out suction filtration, andconcentrating the filtrate to obtain 2-methyl-4-aminopyridine; and (3) carrying out a reaction on the 2-methyl-4-aminopyridine and an acid to generate a salt, cooling to -10-0 DEG C, adding bromine in a dropwise manner, adding a sodium nitrite aqueous solution in a dropwise manner, adjusting the pH value of the solution to achieve an alkaline state after the adding, extracting, drying, and concentrating to obtain 2-methyl-4-bromopyridine. According to the invention, the method has beneficial effects of mild reaction conditions, easy operation, simple post-treatment, easy scale-up production,good catalytic effect, high yield, inexpensive raw materials and low production cost, and is suitable for industrial production;.
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Paragraph 0015; 0018; 0020; 0022; 0024; 0026; 0028
(2020/02/06)
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- A 2 - methyl -4 - bromo pyridine preparation method
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The invention belongs to the field of organic synthesis, in particular relates to a 2 - methyl - 4 - bromo pyridine method, comprises the following steps: (1) malonic acid diethyl ester and alkali metal reaction to produce salt, then dropwise 2 - chloro - 4 - nitro pyridine to a toluene solution of a condensation reaction, after decarboxylation under acidic conditions shall be 2 - methyl - 4 nitro pyridine; (2) 2 - methyl - 4 - nitro-pyridine in under the catalysis of the Pd/C, methanol as the solvent, hydrogen reduction, filtered, the filtrate is concentrated, shall be 2 - methyl - 4 - aminopyridine; (3) 2 - methyl - 4 - aminopyridine first with an acid generating salt, cooled to - 10 °C - 0 °C, [...], drops the instillment sodium nitrite aqueous solution, pH adjusting solution is dropped is alkaline, and then extracted, drying, concentration, shall be 2 - methyl - 4 - bromo pyridine. The beneficial effect of the invention is: mild reaction conditions, is easy to operate, after treatment is simple, and easy to enlarge production, is extremely suitable for industrial production; good catalytic effect, high yield; low prices of raw materials, the production cost is low.
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Paragraph 0018; 0020; 0022; 0024; 0026; 0028
(2019/05/28)
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- AN IMPROVED PROCESS FOR PRODUCING AMINOPYRIDINES
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Disclosed herein is an improved process for producing aminopyridine compounds analogs, substituted forms, derivatives, or the pharmaceutically acceptable salts, esters, amides and prodrugs thereof with high purity and yield at industrial scale.
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Page/Page column 10
(2012/07/28)
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- The synthesis of 6-deazaformycin A
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The synthesis of the new C-nucleoside 6-deazaformycin A was achieved through the condensation of a suitably substituted lithiated 2-picoline with 2,3,5-tri-O-benzyl-d-ribonolactone, borohydride reduction of the resulting hemiacetals, followed by intramolecular Mitsunobu cyclization of the carbinols, manipulation of the protecting groups, and subsequent ring closure to result in the formation of 7-amino-3-(β-d-ribofuranosyl)pyrazolo[4,3-b]pyridine. Georg Thieme Verlag Stuttgart.
- Tite, Tony,Lougiakis, Nikolaos,Marakos, Panagiotis,Pouli, Nicole
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scheme or table
p. 2927 - 2930
(2010/02/28)
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- SMALL ORGANIC MOLECULE REGULATORS OF CELL PROLIFERATION
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The present invention makes available methods and reagents for modulating proliferation or differentiation in a cell or tissue comprising contacting the cell with a compound. In certain embodiments, the methods and reagents may be employed to correct or inhibit an aberrant or unwanted growth state, e.g., by antagonizing a normal patched pathway or agonizing smoothened or hedgehog activity.
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Page/Page column 292
(2008/12/05)
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- SMALL ORGANIC MOLECULE REGULATORS OF CELL PROLIFERATION
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The present invention makes available methods and reagents for modulating proliferation or differentiation in a cell or tissue comprising contacting the cell with a compound. In certain embodiments, the methods and reagents may be employed to correct or inhibit an aberrant or unwanted growth state, e.g., by antagonizing a normal patched pathway or agonizing smoothened orhedgehog activity.
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Page/Page column 292
(2008/12/05)
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- SMALL ORGANIC MOLECULE REGULATORS OF CELL PROLIFERATION
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The present invention makes available methods and reagents for modulating proliferation or differentiation in a cell or tissue comprising contacting the cell with a compound. In certain embodiments, the methods and reagents may be employed to correct or inhibit an aberrant or unwanted growth state, e.g., by antagonizing a normal patched pathway or agonizing smoothened orhedgehog activity.
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Page/Page column 291-292
(2008/12/05)
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- PROCESSES FOR THE PREPARATION OF COMPOUNDS
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The present invention provides improved synthetic methods for the preparation of compounds that modulate proliferation or differentiation in a cell or tissue.
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Page/Page column 203
(2010/11/28)
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- Pyrazine-2-carboxyamide derivatives
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The present invention is concerned with novel pyrazine 2-carboxyamide derivatives of formula (I) wherein R1, R2 and R3 are as defined in the specification. These compounds are useful for the treatment of CNS disorders.
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Page/Page column 15
(2008/06/13)
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- 1,1,1-TRIFLUORO-4-PHENYL-4-METHYL-2-(1H-PYRROLO
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Compounds of Formula (IA), IB), IC), and (ID) wherein R1, R2, R3, R4, R5, and R6 are as respectively defined herein for Formula (IA), (IB), (IC), and (ID), or a tautomer, prodrug, solvate, or salt thereof; pharmaceutical compositions containing such compounds, and methods of modulating the glucocorticoid receptor function and methods of treating disease-states or conditions mediated by the glucocorticoid receptor function or characterized by inflammatory, allergic, or proliferative processes in a patient using these compounds.
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Page/Page column 166
(2010/02/11)
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- PYRIDINE DERIVATIVES AND USE THEREOF AS UROTENSIN II ANTAGONISTS
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The invention relates to novel pyridine derivatives of formula 1 and related compounds and their use as active ingredients in the preparation of pharmaceutical compositions. The invention also concerns related aspects including processes for the preparation of the compounds, pharmaceutical compositions containing one or more of those compounds and their use as neurohormonal antagonists, especially as urotensin II inhibitors.
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Page/Page column 57
(2008/06/13)
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- PHOSPHODIESTERASE 4 INHIBITORS
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PDE4 inhibition is achieved by novel compounds of the Formula (I) wherein R1 and R2 are as defined herein.
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- NOVEL BUTADIENE DERIVATIVES, PROCESS FOR PREPARATION OF THE SAME AND INTERMEDIATES FOR THE SYNTHESIS THEREOF
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A butadiene derivative having an excellent inhibitory activity on the PAI-1, which is represented by the general formula [I]: wherein R1 is a hydrogen atom or a lower alkyl group, R2 is a lower alkyl group, R3 is a lower alkoxy group, R4 is a hydrogen atom or a lower alkyl group, R5 is a lower alkyl group, or a pharmaceutically acceptable salt thereof, a process a process for preparing the same and an intermediate thereof.
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- A general and versatile synthesis of 2-alkyl-4-aminopyridines
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A versatile two-step synthesis of 2-alkyl-4-aminopyridines from commercially available cis-1-methoxy-1-buten-3-yne is described. Acylation of the yne derivative followed by amination and cyclization in ammonia produced the desired substituted pyridines in high yield.
- Hedge, Vidyadhar B.,Renga, James M.,Owen, John M.
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p. 1847 - 1850
(2007/10/03)
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- 5-SUBSTITUTED IMIDAZO[4,5-C]PYRIDINES
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The present invention relates to a class of compounds represented by the formula STR1 or a pharmaceutically acceptable salt thereof useful in the treatment of diseases or disorders mediated by platelet activating factor (PAF).
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- N-phenyl-N'-pyridinylureas as anticonvulsant agents
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A series of N-phenyl-N'-pyridinylureas was examined for anticonvulsant activity. Extensive structure/activity investigations revealed optimal activity in the N-(2,6-disubstituted-phenyl)-N'-(4-pyridinyl)urea series, with 37 exhibiting the best overall anticonvulsant profile. Compound 37 was effective against seizures induced by maximal electroshock but did not protect mice from clonic seizures produced by the convulsant pentylenetetrazol. The overall pharmacological profile suggests that 37 would be of therapeutic use in the treatment of generalized tonic-clonic and partial seizures. Compound 37 was selected for Phase 1 clinical trials.
- Pavia,Lobbestael,Taylor,Hershenson,Miskell
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p. 854 - 861
(2007/10/02)
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- Pyrido[3,4-e]-1,2,4-triazines and related heterocycles as potential antifungal agents
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The preparation and biological activities of a series of pyrido[3,4-e]-1,2,4-triazines, 1,2,4-triazino[5,6-c]quinolines, and related fused triazines are described. Methyl, amino, and acylamino substituents were placed in the pyridyl ring of the former system. Other structural modifications included various alkyl, cycloalkyl, substituted phenyl, and heterocyclic groups in the 3-position of these ring systems. In agar dilution assays, actives in this series inhibited strains of Candida, Aspergillus, Mucor, and Trychophyton species at MIC's of ≤ 16 μg/mL.
- Reich,Fabio,Lee,Kuck,Testa
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p. 2474 - 2485
(2007/10/02)
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