- Electrocatalytic carboxylation of 2-amino-5-bromopyridine with CO 2 in ionic liquid 1-butyl-3-methyllimidazoliumtetrafluoborate to 6-aminonicotinic acid
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A new electrochemical procedure for the electrocatalytic carboxylation of 2-amino-5-bromopyridine with CO2 in ionic liquid, 1-butyl-3-methyllimidazolium tetrafluoborate (BMIMBF4), to 6-aminonicotinic acid was investigated for the first time. The experiments were carried out in three electrodes undivided cell under mild conditions, and the use of volatile and toxic solvents and catalysts, as well as any other additional supporting electrolytes, was avoided. The electrochemical reduction behavior of 2-amino-5-bromopyridine in BMIMBF4 had been studied by cyclic voltammetry with a reduction peak at-1.6V (vs. Ag). 6-Aminonicotinic acid was obtained in 75% yield and 100% selectivity, under the optimized condition. Moreover, the ionic liquid was successfully recycled.
- Feng, Qiuju,Huang, Kelong,Liu, Suqin,Wang, Xuanyun
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- HISTONE DEACETYLASE INHIBITORS FOR IMMUNOMODULATION IN TUMOR MICROENVIRONMENT
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Provided are compounds class I HDAC inhibitors, their production and applications. The compounds possess epigenetic immunomodulatory activities in the tumor microenvironment (TME) and thus inhibit growth of tumor cells.
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Paragraph 0103-0106
(2021/11/06)
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- COMPOUNDS AND METHODS FOR TREATING CANCER
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Substituted cinnamamide compounds and analogs, methods of making such compounds, pharmaceutical compositions and medicaments comprising such compounds, and methods of using such compounds to treat, prevent or ameliorate cancer are provided.
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Paragraph 0190; 0375
(2020/12/19)
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- Synthesis and crystallographic analysis of short pyridine-based oligoamides as DNA-targeting supramolecular binders
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In this study, the synthesis of the pyridine peptides 1-4, formed from amino-picolinic acid, and pyridine peptide 5, made from coupling of a mono-protected pyridine diamine to a mono-protected pyridine dicarboxylic acid and the X-ray crystallographic structures of 1 and 5 are discussed, along with their supramolecular interactions in the solid state. The structure of these compounds showed that they possess concave appearance which can be employed to bind to nucleic acids through multiple hydrogen bonding, which would facilitate the formation of helical-based pyridine oligoamides as novel DNA-binding molecules. This was proven by carrying out DNA denaturation studies and ethidium displacement assay on 5, but, by using MTT assays, 5 was shown to be cytotoxic against drug-resistant chronic myeloid leukaemia K562 cell-line.
- Frimannsson, Daniel O.,McCabe, Thomas,Schmitt, Wolfgang,Lawler, Mark,Gunnlaugsson, Thorfinnur
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p. 483 - 490
(2010/11/18)
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- Electroorganic synthesis of 6-aminonicotinic acid from 2-amino-5-chloropyridine
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A synthesis of 6-aminonicotinic acid by electrochemical hydrogenation of 5-chloro-2-nitropyridine and electrochemical carboxylation of 2-amino-5-chloropyridine at a cathode surface in the presence of sulphuric acid and carbon dioxide in a dimethylformamide (DMF) solution at an apparent current density of 10 mA/cm2 using an undivided cell with good yields is reported.
- Ramesh Raju,Krishna Mohan,Jayarama Reddy
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p. 4133 - 4135
(2007/10/03)
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- Composition of matter having bioactive properties
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Particles of coordinated complex comprising a basic, hydrous polymer and a capacitance adding compound, as well as methods for their production, are described. These complexes exhibit a high degree of bioactivity making them suitable for a broad range of applications through their incorporation into conventional vehicles benefiting from antimicrobial and similar properties.
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- Chichibabin aminations of pyridine bases
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Improved Chichibabin aminations of pyridine bases are described which are conducted under a pressurized gas phase containing ammonia and in the presence of a selected additive which increases the reaction rate, and also in preferred processes favorably alters the isomer ratios and product yields from the aminations while benefiting product workup and recovery as well.
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- Disubstituted aryl and heteroaryl imines having retinoid-like biological activity
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Compounds of the formula STR1 wherein the R 1 groups independently are hydrogen, lower alkyl, or two geminal R 1 groups jointly represent an oxo ( O) or a thio ( S) group; R 2 is hydrogen or lower alkyl, or halogen; M is or --N CR 4 -- or --R 4 C N-- where R 4 is hydrogen or lower alkyl; X is C(R 1) 2 ; Y is phenyl optionally substituted with an R 3 group which is lower alkyl or halogen; A is (CH 2) n where n is 0-5, lower branched chain alkyl, cycloalkyl, alkenyl, alkynyl; B is hydrogen, COOH or a pharmaceutically acceptable salt thereof, COOR 8, CONR 9 R 10, --CH 2 OH, CH 2OR 11, CH 2 OCOR 11, CHO, CH(OR 12) 2, CHOR 13 O, --COR 7, CR 7 (OR 12) 2, or CR 7 OR 13 O, where R 7 is an alkyl, cycloalkyl or alkenyl group containing 1 to 5 carbons, R 8 is an alkyl group of 1 to 10 carbons, or a cycloalkyl group of 5 to 10 carbons, or R 8 is phenyl or lower alkylphenyl, R 9 and R 10 independently are hydrogen, an alkyl group of 1 to 10 carbons, or a cycloalkyl group of 5-10 carbons, or phenyl or lower alkylphenyl, R 11 is lower alkyl, phenyl or lower alkylphenyl, R 12 is lower alkyl, and R 13 is divalent alkyl radical of 2-5 carbons have retinoid-like biological activity.
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- Hydrolysis of nicotinyl 6-aminonicotinate
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The degradation kinetics of nicotinyl 6-aminonicotinate in aqueous buffer solutions were studied over the pH range from 4.0 to 10.0. In all cases, pseudo-first-order kinetics were observed at constant hydronium ion concentration. The pH-rate profile indic
- Wang,Patel
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p. 204 - 207
(2007/10/02)
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- Procedure for producing 2-aminopyridines from 2-pyridine carboxylic acid-N-oxides
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Procedure for producing 2-aminopyridines having general formula: STR1 from 2-pyridine carboxylic acid-N-oxides having the formula: STR2 wherein R is H or a --COOH group or an alkyl group having C1 to C8 or an aryl group, and n is a number between 1 and 4. The 2-pyridine carboxylic acid-N-oxide is converted with a lower aliphatic carboxylic acid anhydride and a tertiary amine in the presence of a carboxylic acid nitrile. The conversion product is hydrolyzed to the 2-aminopyridine compound.
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- On derivatives of 4-oxo-3,4-dihydropyrido[2,3-d]pyrimidine (author's transl)
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A typical representative of the hypnotic and anticonvulsive 4-quinazoline group is methaqualone (1). A number of new derivatives of 4-oxo-3,4-dihydropyrido[2,3-d]pyrimidine (10) were synthetized by substituting the benzene ring in the quinazolone molecule by the pyridine ring. The synthesis was achieved by the condensation of 2-acetaminonicotinic acid (9) and a primary amine or by the reaction of 2-aminonicotinic acid (8) with acetic acid and a primary amine. These new compounds were tested on animals for antiphlogistic, analgetic and antipyretic activities and for effects on the central nervous system as well. It was tried to establish, on the basis of the results obtained, relations between the chemical constitution and the pharmacological efficacy. It was found that, depending on the nature of the substituents in the position 3; either the antiphlogistic, analgetic and antipyretic effects or the anticonvulsive action will prevail.
- Kretzschmar
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p. 253 - 256
(2007/10/02)
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- Studies on 1,3-Benzoxazines. I. Synthesis of Primary 2-Amino-pyridines via the Reaction of Imidoyl Chlorides of 1,3-Benzoxazines with Pyridine N-Oxides
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A new synthetic method for primary 2-aminopyridine derivatives is described.Treatment of the imidoyl chlorides of 1,3-benzoxazines (1a-i) with pyridine N-oxides resulted in the introduction of an oxazine moiety into the α-position of the pyridine ring through rearrangement of the initially formed reaction adduct.Acid hydrolysis of the rearrangement products afforded 2-aminopyridine derivatives in excellent yields.When methoxypyridine N-oxides were used, products of a different type (10 and 14) were obtained.
- Wachi, Kazuyuki,Terada, Atsusuke
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p. 465 - 472
(2007/10/02)
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- Treatment of psoriasis with 6-substituted nicotinamides, 2-substituted pyrazinamides and closely related compounds
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A treatment to alleviate the symptoms of psoriasis consisting of topical application of a cream, ointment or lotion containing, as the principal active ingredient, one or more 6-substituted nicotinamides and or 2-substituted pyrazinamides is disclosed. The therapeutic composition may include a single member of the above active ingredients present in a total amount of from 0.01 to 5 percent by weight of the total composition, or a plurality thereof present in a preferred concentration range of from 0.02 to 2 percent by weight of the total composition. Topical application of the therapeutic composition in a cream, ointment, or a water or alcohol solution has been found to achieve from substantial to complete remissions of psoriasis in humans.
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