Tag: 200-300

On October 31, 2013, Ueno, Hirokazu; Yamamoto, Takashi; Takashita, Ryuta; Yokoyama, Ryohei; Sugiura, Toshihiko; Kageyama, Shunsuke; Ando, Ayatoshi; Eda, Hiroyuki; Eviryanti, Agung; Miyazawa, Tomoko; Kirihara, Aya; Tanabe, Itsuya; Nakamura, Tarou; Noguchi, Misato; Shuto, Manami; Sugiki, Masayuki; Dohi, Mizuki published a patent.Application In Synthesis of 4-Bromo-2-isopropylpyridine The title of the patent was Preparation of N-(4-sulfonamidobenzoyl)-L-phenylalanine and N-(4-sulfonamidobenzoyl)-3-(pyridin-2-yl)-L-alanine derivatives as α4-integrin inhibitors. And the patent contained the following:

There are provided L-phenylalanine and 3-(pyridin-2-yl)-L-alanine derivatives having terminal sulfonamide groups and heterocyclic groups [I; A = Q, Q1, Q2; Arm = cycloalkane or aromatic ring containing 0-4 heteroatoms selected from O, S, and N; R1, R2, R3, R11, R12, R13, R14, R21, R22, R23, R24, R25 = group A, H, lower alkylamino, lower alkylamino-lower alkyl; group A = halo, HO, each hydroxy- or halo-(un)substituted lower alkyl, alkenyl, alkynyl, or alkylthio, NO2, NH2, CO2H, lower alkyloxycarbonyl, CONH2, lower alkanoyl, aroyl, lower alkylsulfonyl, SO2NH2, ammonium group; B = (un)substituted lower alkoxy, HO, hydroxyamino; R41 = H, lower alkyl; a, b, c, d = CR31, CR32, CR33, CR34; e, f, g, h = CR35, CR36, CR37, CR38; R31-R38 = H, halo, lower alkyl, lower alkoxy, NO2; wherein one or two of a, b, c, and d = N atom; one or two of e, f, g, and h = N atom; at least one of R31-R34 = halo or lower alkyl; D = each (un)substituted Ph or heterocyclyl; E = group A, lower alkylaminoalkylene, (un)substituted 5- or 6-membered heterocyclyl, or substituted CONH2; or lower alkylcarbonyl and lower alkyloxycarbonyl in E group are linked to Ph of D group to form a ring] or pharmaceutically acceptable salts thereof. These compounds have excellent α4-integrin-inhibiting activity with high selectivity for α4β7-integrin over α4β1-integrin. They are useful for the treatment or prevention of inflammatory diseases related to α4β7 integrin-dependent adhesion process. Thus, 100 mg Me 4-(1-methyl-2,4-dioxo-1,4-dihydropyrido[3,4-d]pyrimidin-3(2H)-yl)-L-phenylalaninate and 89.0 mg 2,6-difluoro-4-[[[5-(1H-1,2,4-triazol-1-yl)pyridin-2-yl]sulfonyl]amino]benzoic acid were suspended in 2.0 mL CH2Cl2, treated with 133 mg HATU and 0.160 mL diisopropylethylamine, stirred at room temperature for 2 h, and concentrated under reduced pressure to give, after purification using reversed phase HPLC, Me N-[2,6-difluoro-4-([[5-(1H-1,2,4-triazol-1-yl)pyridin-2-yl]sulfonyl]amino)benzoyl]-4-(1-methyl-2,4-dioxo-1,4-dihydropyrido[3,4-d]pyrimidin-3(2H)-yl)-L-phenylalaninate (II; R = Me) tris(trifluoroacetate). II.3CF3CO2H (R = Me) (25.0 mg) was treated with 2.0 mL 4 N HCl/dioxane solution and 2.0 mL H2O, stirred at 80° for 1 h, and concentrated to give, after purification using reversed phase HPLC, II.3CF3CO2H (R = H). II (R = H) (free base) inhibited the binding of MAdCAM to human RPMI-8866 cells expressing α4β7 integrin and that of MAdCAM to human RPMI-8866 cells expressing α4β1 integrin with IC50 of 0.060 and nM, resp., and 220-fold inhibition selectivity for α4β7 integrin. The experimental process involved the reaction of 4-Bromo-2-isopropylpyridine(cas: 908267-63-0).Application In Synthesis of 4-Bromo-2-isopropylpyridine

The Article related to sulfonamidobenzoylhenylalanine preparation selective alpha 4 beta 7 integrin inhibitor, inflammatory disease treatment prevention sulfonamidobenzoylhenylalanine preparation, sulfonamidobenzoylpyridinylalanine preparation selective alpha 4 beta 7 integrin inhibitor and other aspects.Application In Synthesis of 4-Bromo-2-isopropylpyridine

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

On October 15, 2014, Ghaffari, Behnaz; Preshlock, Sean M.; Plattner, Donald L.; Staples, Richard J.; Maligres, Peter E.; Krska, Shane W.; Maleczka, Robert E.; Smith, Milton R. published an article.Electric Literature of 1349171-28-3 The title of the article was Silyl Phosphorus and Nitrogen Donor Chelates for Homogeneous Ortho Borylation Catalysis. And the article contained the following:

Ir catalysts supported by ortho-(diisopropylsilyl)(di-p-tolylphosphino)benzene bidentate ligand that contains P- or N-donors, effects ortho-borylations for a range of substituted aromatics E.g., reaction of C6H5CO2Me with bis(pinacolato)diboron (B2pin2) in the presence of 1.25 mol% [Ir(OMe)(cod)]2/ 2.5 mol% (p-tol)2PC6H4-2-(SiHiPr2) in THF at 80° to give 72% yield of Me 2-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)benzoate. The substrate scope is broad, and the modular ligand synthesis allows for flexible catalyst design. The experimental process involved the reaction of 2-(2-(4,4,5,5-Tetramethyl-1,3,2-dioxaborolan-2-yl)phenyl)pyridine(cas: 1349171-28-3).Electric Literature of 1349171-28-3

The Article related to ortho silylphosphinylbenzene tethered iridium cyclooctadiene preparation catalyst orthoborylation, crystal structure ortho silylphosphinylbenzene tethered iridium cyclooctadiene, mol structure ortho silylphosphinylbenzene tethered iridium cyclooctadiene and other aspects.Electric Literature of 1349171-28-3

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

On August 14, 2003, Adam, Geo; Goetschi, Erwin; Wichmann, Juergen; Woltering, Thomas Johannes published a patent.Application In Synthesis of 4-Bromo-5-ethyl-2-methylpyridine The title of the patent was Preparation of dihydrobenzodiazepin-2-ones as metabotropic glutamate receptor antagonists for the treatment of neurological disorders. And the patent contained the following:

This invention relates to dihydrobenzo[b][1,4]diazepin-2-ones (shown as I; variables defined below; e.g. 7,8-dichloro-4-[3-(pyridin-3-yl)phenyl]-1,3-dihydrobenzo[b][1,4]diazepin-2-one). The invention further relates to medicaments containing these compounds, a process for their preparation as well as their use for preparation of medicaments for the treatment or prevention of acute and/or chronic neurol. disorders, e.g. Alzheimer’s disease. Three examples of pharmaceutical compositions containing I are included. Ki values for 50 examples of I as metabotropic glutamate receptor antagonists are tabulated, e.g. 0.00135 μM for 7,8-dichloro-4-(3-pyridin-3-ylphenyl)-1,3-dihydrobenzo[b][1,4]diazepin-2-one. More than 400 example preparations of I and many example preparations of intermediates are included. For example, 7,8-dichloro-4-[3-(pyridin-3-yl)phenyl]-1,3-dihydrobenzo[b][1,4]diazepin-2-one (310 mg) was prepared from 4,5-dichlorophenylenediamine (0.97 mmol) and 3-oxo-3-[3-(pyridin-3-yl)phenyl]propionic acid tert-Bu ester (0.97 mmol) by refluxing in xylene. For I: X is a single bond or an ethynediyl group; and wherein in case X is a single bond, R1 is H, cyano, halogen, lower alkyl, lower alkoxy, fluoro-lower alkyl, fluoro-lower alkoxy, pyrrol-1-yl, or Ph, which is (un)substituted by one or two substituents halogen, lower alkyl or fluoro-lower alkyl; or in case X is an ethynediyl group, R1 is Ph, which is (un)substituted by one or two substituents halogen, lower alkyl or fluoro-lower alkyl. R2 is H, lower alkyl, lower alkenyl lower alkoxy, halogen, -NR’R”, pyrrolidin-1-yl, piperidin-1-yl, morpholin-4-yl, fluoro-lower alkyl, fluoro-lower alkoxy, or lower alkoxy(ethoxy)m; m = 1-4; R’ is H, lower alkyl or C3-C6-cycloalkyl; R” is H, lower alkyl or C3-C6-cycloalkyl; Y is -CH= or =N-; R3 is a six-membered aromatic heterocycle containing 1 to 3-N atoms or a pyridine N-oxide, which rings are (un)substituted by one or two substituents halogen, fluoro-lower alkyl, fluoro-lower alkoxy, cyano, amino, lower alkylamino, lower alkoxy-lower alkylamino, lower hydroxy-lower alkylamino, -(CH2)n-C(O)-OR”, -(CH2)n-C(O)-NR’R”, -(CH2)n-SO2-NR’R”, -(CH2)n-C(NH2):NR”, hydroxy, lower alkoxy, lower alkylthio, C3-C6-cycloalkyl and lower alkyl, which is (un)substituted by fluoro, -NR’R”, hydroxy, lower alkoxy, pyrrolidin-1-yl, azetidin-1-yl, cyano or carbamoyloxy; n = 0-4. The experimental process involved the reaction of 4-Bromo-5-ethyl-2-methylpyridine(cas: 98488-99-4).Application In Synthesis of 4-Bromo-5-ethyl-2-methylpyridine

The Article related to alzheimer disease, anti-alzheimer agents, antipsychotics, biological memory retention defect, cognition enhancers, cognitive disorders, drug delivery systems, homo sapiens, human, metabotropic glutamate receptors role: bsu (biological study, unclassified), biol (biological study) (antagonists), nervous system agents, nervous system disease, psychosis, schizophrenia and other aspects.Application In Synthesis of 4-Bromo-5-ethyl-2-methylpyridine

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

Thongpaen, Jompol; Manguin, Romane; Dorcet, Vincent; Vives, Thomas; Duhayon, Carine; Mauduit, Marc; Basle, Olivier published an article in 2019, the title of the article was Visible Light Induced Rhodium(I)-Catalyzed C-H Borylation.Recommanded Product: 1349171-28-3 And the article contains the following content:

An efficient visible light induced Rh(I)-catalyzed regioselective borylation of aromatic C-H bonds is reported. The photocatalytic system is based on a single NHC-Rh(I) complex capable of both harvesting visible light and enabling the bond breaking/forming at room temperature The chelating nature of the NHC-carboxylate ligand was critical to ensure the stability of the Rh(I) complex and to provide excellent photocatalytic activities. Exptl. mechanistic studies evidenced a photooxidative ortho C-H bond addition upon irradiation with blue LEDs, leading to a cyclometalated Rh(III)-hydride intermediate. The experimental process involved the reaction of 2-(2-(4,4,5,5-Tetramethyl-1,3,2-dioxaborolan-2-yl)phenyl)pyridine(cas: 1349171-28-3).Recommanded Product: 1349171-28-3

The Article related to rhodium imidazolylidenecarboxylate carbene complex preparation catalyst borylation arene, crystal structure pyridylphenyl rhodium imidazolylidenecarboxylate carbene complex, mol structure pyridylphenyl rhodium imidazolylidenecarboxylate carbene complex, carbon hydrogen activation kinetics borylation arylpyridine rhodium carbene catalyst and other aspects.Recommanded Product: 1349171-28-3

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

On December 30, 1998, Ankersen, Michael; Stidsen, Carsten Enggaard; Crider, Michael Albert published a patent.Application of 199522-66-2 The title of the patent was Preparation of thioureas as somatostatin agonists and antagonists for treating diseases related to the eye. And the patent contained the following:

The title compounds [I; m = 2-6; n = 1-3; p = 1-6; R1, R2 = H, (un)substituted C1-6 alkyl; X = S, O, NH, NCOPh, N(CN); A, B, D = (un)substituted aryl, heteroaryl], somatostatin receptor ligands of nonpeptide origin which have high and/or selective affinity to the somatostatin receptor protein designated SSTR4 (no data), and are useful for the treatment of a disease associated with an adverse condition in the retina and/or iris-ciliary body of a mammal such as high intraocular pressure (IOP) and/or deep ocular infections, were prepared and formulated. The diseases which may be treated with compounds I are e.g. glaucoma, stromal keratitis, iritis, retinitis, cataract and conjunctivitis. Compounds I are effective at 0.001-50 mg/kg/day. E.g., a 5-step synthesis of II.2HCl, starting with propane-1,3-diamine and 2-bromopyridine, is described. The experimental process involved the reaction of N1-(5-Bromopyrid-2-yl)ethane-1,2-diamine(cas: 199522-66-2).Application of 199522-66-2

The Article related to thiourea preparation formulation somatostatin agonist antagonist, glaucoma thiourea preparation formulation, eye disease thiourea preparation formulation, keratitis thiourea preparation formulation, iritis thiourea preparation formulation, retinitis thiourea preparation formulation, cataract thiourea preparation formulation and other aspects.Application of 199522-66-2

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

On September 25, 2014, Schwiebert, Erik; Streiff, John; Dixon, John; Gao, Hongwu; Ritchie, Joseph P.; Seales, Eric C.; Mai, Deborah published a patent.SDS of cas: 25813-24-5 The title of the patent was Preparation of coumarin thiazolyl derivatives and methods of use in treating hyperproliferative diseases. And the patent contained the following:

Coumarin thiazolyl derivatives I [R1 is H, halogen, OH, (un)substituted alkoxyl, (un)substituted amino, (un)substituted C1-6-alkyl, (un)substituted heterocycloalkyl; R2 is H, halogen, OH, NO2, CN, N3, thiocyanato, CF3, (un)substituted alkoxyl, (un)substituted amino, (un)substituted carbonyl, or (un)substituted C1-6-alkyl; R3 is H or substituted or unsubstituted C1-6-alkyl; R4 is (un)substituted C1-6-alkyl, (un)substituted aryl or (un)substituted heteroaryl; X is S or O; and, Y is O, NH or NMe] are provided. Thus, DBM-308 (II) was prepared from 3-chlorosalicylaldehyde via cyclocondensation with Et acetoacetate in EtOH containing piperidine to give 3-acetyl-8-chlorocoumarin (III); regioselective bromination with CuBr2 in CHCl3 to give 3-(bromoacetyl)-8-chlorocoumarin (IV); and cyclocondensation with 2-MeOC6H4NHC(:S)NH2 to give II. Methods for the treatment of hyperproliferative diseases, such as cancer, polycystic kidney disease, and fibrosis of different tissues (e.g., idiopathic pulmonary fibrosis), are provided. The antiproliferative activity of II was determined [GI50 = 166 nM; TGI = 247 nM; LC50 = >4,000 nM; IC50 = 0.69 μM vs. N828 cell line (hyperproliferative PKD cells); IC50 = 0.54 μM vs. 3-8C1 cell line (hyperproliferative PKD cells)]. The methods include administering to a subject a compound as described herein. Also provided are methods for inhibiting the interaction between two or more heat shock protein chaperones in a cell. The experimental process involved the reaction of 3,5-Dibromo-4-methoxypyridine(cas: 25813-24-5).SDS of cas: 25813-24-5

The Article related to coumarin thiazolyl derivative preparation treatment hyperproliferative disease, cancer treatment coumarin thiazolyl derivative, polycystic kidney disease treatment coumarin thiazolyl derivative, tissue fibrosis treatment coumarin thiazolyl derivative, idiopathic pulmonary fibrosis treatment coumarin thiazolyl derivative and other aspects.SDS of cas: 25813-24-5

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

On February 11, 2016, Schwiebert, Erik; Streiff, John; Dixon, John; Gao, Hongwu; Ritchie, Joseph P.; Seales, Eric C.; Mai, Deborah published a patent.Electric Literature of 25813-24-5 The title of the patent was Coumarin derivatives and methods of use in treating hyperproliferative diseases. And the patent contained the following:

Coumarin derivative compounds and methods for the treatment of hyperproliferative diseases, such as cancer, polycystic kidney disease, and fibrosis of different tissues (e.g., idiopathic pulmonary fibrosis), are provided. The methods include administering to a subject a compound as described herein. Also provided are methods for inhibiting the interaction between two or more heat shock protein chaperones in a cell. The experimental process involved the reaction of 3,5-Dibromo-4-methoxypyridine(cas: 25813-24-5).Electric Literature of 25813-24-5

The Article related to coumarin thiazolyl derivative preparation treatment hyperproliferative disease, cancer treatment coumarin thiazolyl derivative, polycystic kidney disease treatment coumarin thiazolyl derivative, tissue fibrosis treatment coumarin thiazolyl derivative, idiopathic pulmonary fibrosis treatment coumarin thiazolyl derivative and other aspects.Electric Literature of 25813-24-5

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

Thongpaen, Jompol; Schmid, Thibault E.; Toupet, Loic; Dorcet, Vincent; Mauduit, Marc; Basle, Olivier published an article in 2018, the title of the article was Directed ortho C-H borylation catalyzed using Cp*Rh(III)-NHC complexes.Computed Properties of 1349171-28-3 And the article contains the following content:

Cp*Rh(NHC) complexes I(R = iBu, iPr, Me), derived from L-amino acids, with bulky chiral bidentate NHC-carboxylate ligands were efficiently synthesized and fully characterized including solid-state structures. These unprecedented rhodium(III) complexes demonstrated high selectivity in pyridine-directed ortho-C-H borylation of arenes under mild conditions. The experimental process involved the reaction of 2-(2-(4,4,5,5-Tetramethyl-1,3,2-dioxaborolan-2-yl)phenyl)pyridine(cas: 1349171-28-3).Computed Properties of 1349171-28-3

The Article related to directed borylation arylpyridine rhodium chiral nhc catalyst preparation phenol, phenol preparation pyridyl directed borylation oxidation rhodium nhc catalyst, crystal structure rhodium chiral nhc carboxylate half sandwich complex, mol structure rhodium chiral nhc carboxylate half sandwich complex and other aspects.Computed Properties of 1349171-28-3

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

Rieder, Samuel; Melendez, Camilo; Denes, Fabrice; Jangra, Harish; Mulliri, Kleni; Zipse, Hendrik; Renaud, Philippe published an article in 2021, the title of the article was Radical chain monoalkylation of pyridines.SDS of cas: 908267-63-0 And the article contains the following content:

The monoalkylation of N-methoxypyridinium salts with alkyl radicals generated from alkenes (via hydroboration with catecholborane), alkyl iodides (via iodine atom transfer) and xanthates to afford alkylated quinoline derivatives R-R1 [R = 4-methylquinolinyl, 4-Cl-quinolinyl, 3-Br-quinolinyl, etc.; R1 = Et, iPr, cyclohexyl, etc.] and pyridine derivatives R2-R3 [R2 = 4-phenylpyridinyl, 4-tBu-pyridinyl, 4-Br-pyridinyl, etc.; R3 = iPr, 1-adamantyl, cyclohexyl, etc.] was reported. The reaction proceeded under neutral conditions since no acid was needed to activate the heterocycle and no external oxidant was required. A rate constant for the addition of a primary radical to N-methoxylepidinium >107 M-1 s-1 was exptl. determined This rate constant was more than one order of magnitude larger than the one measured for the addition of primary alkyl radicals to protonated lepidine demonstrating the remarkable reactivity of methoxypyridinium salts toward radicals. The reaction was used for the preparation of unique pyridinylated terpenoids and was extended to a three-component carbopyridinylation of electron-rich alkenes including enol esters, enol ethers and enamides. The experimental process involved the reaction of 4-Bromo-2-isopropylpyridine(cas: 908267-63-0).SDS of cas: 908267-63-0

The Article related to alkylated pyridine derivative preparation, pyridine derivative alkene monoalkylation, alkyl iodide pyridine derivative monoalkylation, xanthate pyridine derivative monoalkylation, derivative pyridine alkylated preparation, ester alkene pyridine derivative three component carbopyridinylation and other aspects.SDS of cas: 908267-63-0

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

On October 29, 2015, Basinger, Jillian; Bookser, Brett; Chen, Mi; Chung, Demichael; Gupta, Varsha; Hudson, Andrew; Kaplan, Alan; Na, James; Renick, Joel; Santora, Vincent published a patent.Related Products of 908267-63-0 The title of the patent was Preparation of substituted 2,4,5,6-tetrahydropyrrolo[3,4-c]pyrazole and 4,5,6,7-tetrahydro-2H-pyrazolo[4,3-c]pyridine compounds as GlyT1 inhibitors. And the patent contained the following:

The title compounds I [R1 = CO2H, C(O)NH2, SO2(alkyl), etc.; R2 = H, halo, alkyl, etc.; R3 = H, alkyl, haloalkyl, etc.; R4 = H, F, alkyl, etc.; R5 = alkyl, haloalkyl, alkoxy, etc.; X = (CR)1-2; R = H, alkyl], useful in a wide range of methods, including metabolic and reaction kinetic studies; detection and imaging techniques; radioactive treatments; modulating and treating disorders mediated by GlyT1 activity; treating neurol. disorders, CNS disorders, dementia, neurodegenerative diseases, and trauma-dependent losses of function; treating stroke, including cognitive and motor deficits during stroke rehabilitation; facilitating neuroprotection and neurorecovery; enhancing the efficiency of cognitive and motor training, including animal skill training; and treating other disorders, including pain and alc.-dependence, were prepared E.g., a multi-step synthesis of II, starting from tert-Bu 4,6-dihydropyrrolo[3,4-c]pyrazole-5(2H)-carboxylate and 1-fluoro-4-iodobenzene, was described. The exemplified compounds I were their GlyT1 inhibitory activity (data given). Pharmaceutical composition comprising I is disclosed. The experimental process involved the reaction of 4-Bromo-2-isopropylpyridine(cas: 908267-63-0).Related Products of 908267-63-0

The Article related to pyrrolopyrazole pyrazolopyridine preparation glyt1 inhibitor neurol disorder treatment, cns agent cognition enhancer neuroprotection pyrrolopyrazole pyrazolopyridine preparation glyt1, dementia neurodegenerative disease stroke motor deficit pyrrolopyrazole pyrazolopyridine preparation and other aspects.Related Products of 908267-63-0

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem