Tag: M.W=100-150

Chae, Eunhee published the artcileDiscovery of biological evaluation of pyrazole/imidazole amides as mGlu5 receptor negative allosteric modulators, Application In Synthesis of 18437-58-6, the publication is Bioorganic & Medicinal Chemistry Letters (2013), 23(7), 2134-2139, database is CAplus and MEDLINE.

Development of SAR in a 5-aryl-3-acylpyridinyl-pyrazoles and 1-aryl-4-acylpyridinyl imidazoles series of mGlu5 receptor neg. allosteric modulators (mGluR5 NAMs) using a functional cell-based assay is described in this Letter. Anal. of the Ligand-lipophilic efficiency (LipE) of compounds provided new insight for the design of potent mGluR5 neg. allosteric modulators with anti-depressant activities.

Bioorganic & Medicinal Chemistry Letters published new progress about 18437-58-6. 18437-58-6 belongs to pyridine-derivatives, auxiliary class Pyridine,Amine, name is 4-Amino-2-picoline, and the molecular formula is C6H8N2, Application In Synthesis of 18437-58-6.

Referemce:
https://en.wikipedia.org/wiki/Pyridine,
Pyridine | C5H5N – PubChem

Dabholkar, Vijay V. published the artcileChemistry of novel biphenyl cyclic 3,5-disubstituted 1,2,4-oxadiazole derivatives – their synthesis and microbial evaluation, COA of Formula: C6H8N2, the publication is Heterocyclic Letters (2013), 3(4), 525-531, database is CAplus.

2′-Cyano-4-bromomethyl biphenyl was reacted with hydroxylamine hydrochloride in the presence of sodium carbonate and on further treatment with 2-methyl-4-aminopyridine yielded 3,5-disubstituted 1,2,4-oxadiazole I. 3,5-Di(4-bromomethyl-biphenyl-6′,6”-yl)-1,2,4-oxadiazole was condensed with L-valine Me ester and further cyclized with aliphatic dibromo alkanes Br₂(CH₂)_n to yield the resp. cyclic 3,5-disubstituted 1,2,4-oxadiazoles II [n = 2, 3, 4]. Compounds I and II were evaluated for their antimicrobial activity against Gram pos. and Gram neg. bacteria.

Heterocyclic Letters published new progress about 18437-58-6. 18437-58-6 belongs to pyridine-derivatives, auxiliary class Pyridine,Amine, name is 4-Amino-2-picoline, and the molecular formula is C6H8N2, COA of Formula: C6H8N2.

Referemce:
https://en.wikipedia.org/wiki/Pyridine,
Pyridine | C5H5N – PubChem

Yamada, Makito published the artcileLigand-free Suzuki-Miyaura coupling reaction of aryl chlorides using a continuous irradiation type microwave and a palladium nanoparticle catalyst: effect of a co-existing solid, Category: pyridine-derivatives, the publication is Green Chemistry (2019), 21(16), 4541-4549, database is CAplus.

The effect of a co-existing metal in the ligand-free Suzuki-Miyaura coupling reaction of aryl chlorides ArCl (Ar = Ph, pyridin-2-yl, naphthalen-1-yl, etc.) is promoted by a ”continuous irradiation type microwave” and a ”palladium nanoparticle catalyst”, and it is found that the co-existing metal affects this reaction due to its absorption ability of microwave energy in the reaction system. It is also observed that spiking occurred more frequently in the presence of a co-existing metal.

Green Chemistry published new progress about 197958-29-5. 197958-29-5 belongs to pyridine-derivatives, auxiliary class Pyridine,Boronic acid and ester, name is 2-Pyridinylboronic acid, and the molecular formula is C17H19N3O7S, Category: pyridine-derivatives.

Referemce:
https://en.wikipedia.org/wiki/Pyridine,
Pyridine | C5H5N – PubChem

Cumper, C. W. N. published the artcileThe ultraviolet spectra of aniline, 2-, 3-, and 4-aminopyridines, and of some of their derivatives in n-hexane, 1,4-dioxane, ethanol, and water solutions, Category: pyridine-derivatives, the publication is Journal of the Chemical Society [Section] B: Physical Organic (1968), 649-51, database is CAplus.

The uv spectra of aniline, 2-, 3-, and 4-aminopyridines, and certain of their derivatives have been determined in hexane, 1,4-dioxane, EtOH, and water solutions N-Methylation of the amino group increases its electron-donating ability and the introduction of a Me group or halogen atom into the Ph or pyridyl ring also produces a bathochromic shift. In dioxane and EtOH solutions the amine forms H bonds to the solvent; this also occurs with 4-aminopyridines in water; with the other solutes H bonding by the water predominates.

Journal of the Chemical Society [Section] B: Physical Organic published new progress about 18437-58-6. 18437-58-6 belongs to pyridine-derivatives, auxiliary class Pyridine,Amine, name is 4-Amino-2-picoline, and the molecular formula is C6H8N2, Category: pyridine-derivatives.

Referemce:
https://en.wikipedia.org/wiki/Pyridine,
Pyridine | C5H5N – PubChem

Cumper, Charles W. N. published the artcileElectric dipole moments of toluidines and some aminopicolines in benzene and 1,4-dioxane solution, Formula: C6H8N2, the publication is Journal of the Chemical Society [Section] B: Physical Organic (1967), 1100-3, database is CAplus.

The elec. dipole moments of the three toluidines and seven aminopicolines were calculated from measurements of the dielec. constants, sp. volumes, and refractive indexes of their solutions in benzene and in 1,4-dioxane at 25.00°. In o-toluidine, 4-amino-3-methylpyridine, and 2-amino-3-methylpyridine there is an interaction between the adjacent substituents but this is somewhat less in 3-amino-4-methylpyridine. Mesomeric moments are present in 2- and 4-aminopyridines and in the former direct interaction occurs between the amino-group and heterocyclic N atom.

Journal of the Chemical Society [Section] B: Physical Organic published new progress about 18437-58-6. 18437-58-6 belongs to pyridine-derivatives, auxiliary class Pyridine,Amine, name is 4-Amino-2-picoline, and the molecular formula is C6H8N2, Formula: C6H8N2.

Referemce:
https://en.wikipedia.org/wiki/Pyridine,
Pyridine | C5H5N – PubChem

Terashima, Masanao published the artcilePhotoinduced reactions. XXVII. Photochemistry of the phthalimide system. XIV. Photochemical synthesis of a pyridopyrrolo[2,1-a]isoindole system by cyclization of N-methylpyridylphthalimides, HPLC of Formula: 18437-58-6, the publication is Chemical & Pharmaceutical Bulletin (1977), 25(7), 1591-5, database is CAplus.

Photochem. reactions of N-(3-methyl-2-pyridyl)-(I), N-(4-methyl-3-pyridyl)-(II), and N-(3-methyl-4-pyridyl)phthalimide (III) were investigated. Although irradiation of II in an acetone solution gave only the dihydro product, 3-hydroxy-2-(3-methyl-2-pyridyl)phthalimidine, III afforded the expected cyclized product, 10b,11-dihydro-10b-hydroxy-6H-pyrido[4′,3′:4,5]pyrrolo[2,1-a]isoindol-6-one (IV) and dihydro product, 3-hydroxy-2-(4-methyl-3-pyridyl)phthalimidine. Under similar conditions, the cyclized product, 10b,11-dihydro-10b-hydroxy-6H-pyrido[3′,4′:4,5]pyrrolo[2,1-a]isoindol-6-one was obtained from the photolysis of III and none of the reduced product was isolated.

Chemical & Pharmaceutical Bulletin published new progress about 18437-58-6. 18437-58-6 belongs to pyridine-derivatives, auxiliary class Pyridine,Amine, name is 4-Amino-2-picoline, and the molecular formula is C15H14O3, HPLC of Formula: 18437-58-6.

Referemce:
https://en.wikipedia.org/wiki/Pyridine,
Pyridine | C5H5N – PubChem

van der Born, Dion published the artcileA Universal Procedure for the [¹⁸F]Trifluoromethylation of Aryl Iodides and Aryl Boronic Acids with Highly Improved Specific Activity, Synthetic Route of 197958-29-5, the publication is Angewandte Chemie, International Edition (2014), 53(41), 11046-11050, database is CAplus and MEDLINE.

Herein, we describe a valuable method for the introduction of the [¹⁸F]CF₃ group into arenes with highly improved specific activity by the reaction of [¹⁸F]trifluoromethane with aryl iodides or aryl boronic acids. This [¹⁸F]trifluoromethylation reaction is the first to be described in which the [¹⁸F]CF₃ products are generated in actual trace amounts and can therefore effectively be used as PET tracers. The method shows broad scope with respect to possible aryl iodide and aryl boronic acid substrates, as well as good to excellent conversion. In particular, the [¹⁸F]trifluoromethylation of boronic acids was found to outperform [¹⁸F]trifluoromethylation reactions of halogenated aryl precursors with regard to conversion, reaction conditions, and kinetics.

Angewandte Chemie, International Edition published new progress about 197958-29-5. 197958-29-5 belongs to pyridine-derivatives, auxiliary class Pyridine,Boronic acid and ester, name is 2-Pyridinylboronic acid, and the molecular formula is C21H26Br4S2, Synthetic Route of 197958-29-5.

Referemce:
https://en.wikipedia.org/wiki/Pyridine,
Pyridine | C5H5N – PubChem

Makaravage, Katarina J. published the artcileCopper(II)-Mediated [¹¹C]Cyanation of Arylboronic Acids and Arylstannanes, Related Products of pyridine-derivatives, the publication is Organic Letters (2018), 20(6), 1530-1533, database is CAplus and MEDLINE.

A copper-mediated method for the transformation of diverse arylboron compounds and arylstannanes to aryl-[¹¹C]-nitriles is reported. This method is operationally simple, uses com. available reagents, and is compatible with a wide variety of substituted aryl- and heteroaryl substrates. This method is applied to the automated synthesis of high specific activity [¹¹C]perampanel in 10% nondecay-corrected radiochem. yield (RCY).

Organic Letters published new progress about 197958-29-5. 197958-29-5 belongs to pyridine-derivatives, auxiliary class Pyridine,Boronic acid and ester, name is 2-Pyridinylboronic acid, and the molecular formula is C5H6BNO2, Related Products of pyridine-derivatives.

Referemce:
https://en.wikipedia.org/wiki/Pyridine,
Pyridine | C5H5N – PubChem

Paone, Daniel V. published the artcilePotent, Orally Bioavailable Calcitonin Gene-Related Peptide Receptor Antagonists for the Treatment of Migraine: Discovery of N-[(3R,6S)-6-(2,3-Difluorophenyl)-2-oxo-1- (2,2,2-trifluoroethyl)azepan-3-yl]-4- (2-oxo-2,3-dihydro-1H-imidazo[4,5-b]pyridin- 1-yl)piperidine-1-carboxamide (MK-0974), Recommanded Product: 2-Pyridinylboronic acid, the publication is Journal of Medicinal Chemistry (2007), 50(23), 5564-5567, database is CAplus and MEDLINE.

Calcitonin gene-related peptide (CGRP) has been implicated in the pathogenesis of migraine. Herein we describe optimization of CGRP receptor antagonists based on an earlier lead structure containing a (3R)-amino-(6S)-phenylcaprolactam core. Replacement of the phenylimidazolinone with an azabenzimidazolone gave stable derivatives with lowered serum shifts. Extensive SAR studies of the C-6 aryl moiety revealed the potency-enhancing effect of the 2,3-difluorophenyl group, and trifluoroethylation of the N-1 amide position resulted in improved oral bioavailabilities, ultimately leading to clin. candidate 38 (MK-0974).

Journal of Medicinal Chemistry published new progress about 197958-29-5. 197958-29-5 belongs to pyridine-derivatives, auxiliary class Pyridine,Boronic acid and ester, name is 2-Pyridinylboronic acid, and the molecular formula is C5H6BNO2, Recommanded Product: 2-Pyridinylboronic acid.

Referemce:
https://en.wikipedia.org/wiki/Pyridine,
Pyridine | C5H5N – PubChem

Sekimata, Katsuhiko published the artcileBis-heteroaryl pyrazoles: identification of orally bioavailable inhibitors of activin receptor-like kinase-2 (R206H), Safety of 2-Pyridinylboronic acid, the publication is Chemical & Pharmaceutical Bulletin (2019), 67(3), 224-235, database is CAplus and MEDLINE.

Mutant activin receptor-like kinase-2 (ALK2) was reported to be closely associated with the pathogenesis of fibrodysplasia ossificans progressiva (FOP) and diffuse intrinsic pontine glioma (DIPG), and therefore presents an attractive target for therapeutic intervention. Through in silico virtual screenings and structure-activity relationship studies assisted by X-ray crystallog. analyses, a novel series of bis-heteroaryl pyrazole was identified as potent inhibitors of ALK2 (R206H). Derived from in silico hit compound RK-59638 (6a), compound 18p was identified as a potent inhibitor of ALK2 (R206H) with good aqueous solubility, liver microsomal stability, and oral bioavailability.

Chemical & Pharmaceutical Bulletin published new progress about 197958-29-5. 197958-29-5 belongs to pyridine-derivatives, auxiliary class Pyridine,Boronic acid and ester, name is 2-Pyridinylboronic acid, and the molecular formula is C6H13BO3, Safety of 2-Pyridinylboronic acid.

Referemce:
https://en.wikipedia.org/wiki/Pyridine,
Pyridine | C5H5N – PubChem