Day: February 9, 2023

Tetracyclic spirooxindole blockers of hNa_V1.7: activity in vitro and in CFA-induced inflammatory pain model was written by Chowdhury, Sultan;Liu, Shifeng;Cadieux, Jay A.;Hsieh, Tom;Chafeev, Mikhail;Sun, Shaoyi;Jia, Qi;Sun, Jianyu;Wood, Mark;Langille, Jonathan;Sviridov, Serguei;Fu, Jianmin;Zhang, Zaihui;Chui, Ray;Wang, Audrey;Cheng, Xing;Zhong, Jing;Hossain, Sazzad;Khakh, Kuldip;Rajlic, Ivana;Verschoof, Henry;Kwan, Rainbow;Young, Wendy. And the article was included in Medicinal Chemistry Research in 2013.Recommanded Product: 5-Hydroxy-2-methoxylpyridine This article mentions the following:

The structure-activity relationship of a new series of tetracyclic spirooxindoles led to the discovery of compound 25a, a potent hNa_V1.7 blocker with improved ADME properties and in vivo efficacy in the CFA-induced inflammatory pain model. In the experiment, the researchers used many compounds, for example, 5-Hydroxy-2-methoxylpyridine (cas: 51834-97-0Recommanded Product: 5-Hydroxy-2-methoxylpyridine).

5-Hydroxy-2-methoxylpyridine (cas: 51834-97-0) belongs to pyridine derivatives. Pyridine’s the lone pair does not contribute to the aromatic system but importantly influences the chemical properties of pyridine, as it easily supports bond formation via an electrophilic attack. Reduced pyridines, namely tetrahydropyridines, dihydropyridines and piperidines, are found in numerous natural and synthetic compounds. The synthesis and reactivity of these compounds have often been driven by the fact many of these compounds have interesting and unique pharmacological properties. Recommanded Product: 5-Hydroxy-2-methoxylpyridine

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

Scandium(III) Triflate Catalyzed Direct Synthesis of N-Unprotected Ketimines was written by Kondo, Yuta;Kadota, Tetsuya;Hirazawa, Yoshinobu;Morisaki, Kazuhiro;Morimoto, Hiroyuki;Ohshima, Takashi. And the article was included in Organic Letters in 2020.Product Details of 91-02-1 This article mentions the following:

N-Unprotected ketimines are useful substrates and intermediates for synthesizing valuable nitrogen-containing compounds, but their potential applicability is limited by the available synthetic methods. To address this issue, we report a scandium(III) triflate catalyzed direct synthesis of N-unprotected ketimines. Using com. available reagents and Lewis acid catalysts, ketones were directly transformed into the corresponding N-unprotected ketimines in high yields with broad functional group tolerance, even in multigram scales. The reactions were readily applicable for one-pot synthesis of important compounds such as a glycine Schiff base without isolation of N-unprotected ketimine intermediates. Preliminary mechanistic studies to clarify the reaction mechanism are also described. In the experiment, the researchers used many compounds, for example, Phenyl(pyridin-2-yl)methanone (cas: 91-02-1Product Details of 91-02-1).

Phenyl(pyridin-2-yl)methanone (cas: 91-02-1) belongs to pyridine derivatives. The ring atoms in the pyridine molecule are sp2-hybridized. The nitrogen is involved in the π-bonding aromatic system using its unhybridized p orbital. The lone pair is in an sp2 orbital, projecting outward from the ring in the same plane as the σ bonds. Pyridine, its benzo and pyridine-based compounds play diverse roles in organic chemistry. Pyridine-based materials are valued for their optical and physical properties as well as their medical potential. Product Details of 91-02-1

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

Novel diversely substituted 1-heteroaryl-2-imidazolines for fragment-based drug discovery was written by Krasavin, Mikhail. And the article was included in Tetrahedron Letters in 2012.Related Products of 54151-74-5 This article mentions the following:

A palladium-catalyzed Buchwald-Hartwig arylation protocol has been applied to achieve high-yielding N-heteroarylation of a diverse set of privileged 2-imidazolines, e.g. I. The resulting compounds are of interest as a novel type of mol. tool for fragment-based drug discovery. The potential for combining two 2-imidazoline moieties in a heteroarene-linked dimer via sequential Pd-catalyzed arylation has been demonstrated. In the experiment, the researchers used many compounds, for example, 2-Bromo-4-phenylpyridine (cas: 54151-74-5Related Products of 54151-74-5).

2-Bromo-4-phenylpyridine (cas: 54151-74-5) belongs to pyridine derivatives. The pyridine ring occurs in many important compounds, including agrochemicals, pharmaceuticals, and vitamins. One of the examples of pyridines is the well-known alkaloid lithoprimidine, which is an A3 adenosine receptor antagonist and N,N-dimethylaminopyridine (DMAP) analog, commonly used in organic synthesis.Related Products of 54151-74-5

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

Improved synthesis of 4-substituted pyridines from nitriles was written by Chelucci, Giorgio;Giacomelli, Giampaolo;Scano, Gianfranco. And the article was included in Gazzetta Chimica Italiana in 1991.Application In Synthesis of 4-Hexylpyridine This article mentions the following:

4-Substituted pyridines I ( R = n-hexyl, iso-Bu, sec-Bu, Ph) were prepared by a 4-step sequence in 23-27% overall yield starting from RCH₂CN. The synthesis involves alkylation of RCH₂CN with BrCH₂CH(OEt)₂, then with 2-iodomethyl-1,3-dioxolane, removal of the CN group and reaction of the glutaraldehyde acetals II, thus obtained, with NH₂OH.HCl in AcOH to give I. In the experiment, the researchers used many compounds, for example, 4-Hexylpyridine (cas: 27876-24-0Application In Synthesis of 4-Hexylpyridine).

4-Hexylpyridine (cas: 27876-24-0) belongs to pyridine derivatives. In contrast to benzene, Pyridine’s electron density is not evenly distributed over the ring, reflecting the negative inductive effect of the nitrogen atom. Reduced pyridines, namely tetrahydropyridines, dihydropyridines and piperidines, are found in numerous natural and synthetic compounds. The synthesis and reactivity of these compounds have often been driven by the fact many of these compounds have interesting and unique pharmacological properties. Application In Synthesis of 4-Hexylpyridine

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

Pillar[5]arene-Containing Metallacycles and Host-Guest Interaction Caused Aggregation-Induced Emission Enhancement Platforms was written by Tuo, Wei;Sun, Yan;Lu, Shuai;Li, Xiaopeng;Sun, Yao;Stang, Peter J.. And the article was included in Journal of the American Chemical Society in 2020.Related Products of 65350-59-6 This article mentions the following:

Coordination-driven Pt metallacycles have shown potential in controllable modular self-assembly, which has made a vital contribution to biomedicine, catalysis, and multiresponsive materials. Herein, pillar[5]arene units were integrated into one skeleton through coordination-driven self-assembly, resulting in the formation of a hexagonal Pt(II) metallacycle decorated with six pillar[5]arenes. The host-guest interactions of the as-prepared metallacycle (pillar[5]arenes as hosts) and 1-butyl-4-[4-(diphenylamino)styryl]pyridinium (guest) were investigated. The metallacycle was found to facilitate the coaggregation between the guests and pillar[5]arenes through a synergistic effect, thus engendering a sharp increase in fluorescence intensity. The resultant aggregate was investigated by DLS and TEM. Our studies imply that the pillar[5]arene-containing metallacycle can serve as a potential platform for realizing emission enhancement effects. In the experiment, the researchers used many compounds, for example, 1-Butyl-4-methylpyridin-1-ium bromide (cas: 65350-59-6Related Products of 65350-59-6).

1-Butyl-4-methylpyridin-1-ium bromide (cas: 65350-59-6) belongs to pyridine derivatives. Pyridine’s the lone pair does not contribute to the aromatic system but importantly influences the chemical properties of pyridine, as it easily supports bond formation via an electrophilic attack. One of the examples of pyridines is the well-known alkaloid lithoprimidine, which is an A3 adenosine receptor antagonist and N,N-dimethylaminopyridine (DMAP) analog, commonly used in organic synthesis.Related Products of 65350-59-6

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

Palladium-Catalyzed Decarboxylative Coupling of α- Oxocarboxylic Acids with C(sp²)-H of 2-Aryloxypyridines was written by Yao, Jinzhong;Feng, Ruokun;Wu, Zaihong;Liu, Zhanxiang;Zhang, Yuhong. And the article was included in Advanced Synthesis & Catalysis in 2013.Product Details of 4783-68-0 This article mentions the following:

An efficient palladium-catalyzed decarboxylative ortho-acylation of 2-aryloxypyridines with α-oxocarboxylic acids is described. In this new transformation, the aromatic C(sp²)-H bond was successfully acylated to give diverse aromatic ketones regioselectively in moderate to good yields. The pyridine group can be removed easily after the acylation to give the corresponding 2-hydroxy aromatic ketones. In the experiment, the researchers used many compounds, for example, 2-Phenoxypyridine (cas: 4783-68-0Product Details of 4783-68-0).

2-Phenoxypyridine (cas: 4783-68-0) belongs to pyridine derivatives. In contrast to benzene, Pyridine’s electron density is not evenly distributed over the ring, reflecting the negative inductive effect of the nitrogen atom. Several pyridine derivatives play important roles in biological systems. While its biosynthesis is not fully understood, nicotinic acid (vitamin B3) occurs in some bacteria, fungi, and mammals.Product Details of 4783-68-0

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

Discovery of PIPE-359, a Brain-Penetrant, Selective M₁ Receptor Antagonist with Robust Efficacy in Murine MOG-EAE was written by Schrader, Thomas O.;Xiong, Yifeng;Lorenzana, Ariana O.;Broadhead, Alexander;Stebbins, Karin J.;Poon, Michael M.;Baccei, Christopher;Lorrain, Daniel S.. And the article was included in ACS Medicinal Chemistry Letters in 2021.Product Details of 38186-85-5 This article mentions the following:

The discovery of PIPE-359, a brain-penetrant and selective antagonist of the muscarinic acetylcholine receptor subtype 1 is described. Starting from a literature-reported M₁ antagonist, linker replacement and structure-activity relationship investigations of the eastern 1-(pyridinyl)piperazine led to the identification of a novel, potent, and selective antagonist with good MDCKII-MDR1 permeability. Continued semi-iterative positional scanning facilitated improvements in the metabolic and hERG profiles, which ultimately delivered PIPE-359. This advanced drug candidate exhibited robust efficacy in mouse myelin oligodendrocyte glycoprotein (MOG)-induced exptl. autoimmune encephalitis (EAE), a preclin. model for multiple sclerosis. In the experiment, the researchers used many compounds, for example, 2-Bromo-5-fluoro-3-methylpyridine (cas: 38186-85-5Product Details of 38186-85-5).

2-Bromo-5-fluoro-3-methylpyridine (cas: 38186-85-5) belongs to pyridine derivatives. Pyridine has a conjugated system of six π electrons that are delocalized over the ring. The molecule is planar and, thus, follows the Hückel criteria for aromatic systems. Many analogues of pyridine are known where N is replaced by other heteroatoms . Substitution of one C–H in pyridine with a second N gives rise to the diazine heterocycles (C4H4N2), with the names pyridazine, pyrimidine, and pyrazine.Product Details of 38186-85-5

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

Novel 1,4-dihydropyridine calcium antagonists. I. Synthesis and hypotensive activity of 4-(substituted pyridyl)-1,4-dihydropyridine derivatives was written by Ashimori, Atsuyuki;Ono, Taizo;Uchida, Takeshi;Ohtaki, Yutaka;Fukaya, Chikara;Watanabe, Masahiro;Yokoyama, Kazumasa. And the article was included in Chemical & Pharmaceutical Bulletin in 1990.Recommanded Product: (4-Bromopyridin-2-yl)methanol This article mentions the following:

A series of 4-(substituted pyridyl)-1,4-dihydropyridine derivatives I (R = H, halo, CF₃, etc.) were synthesized and their hypotensive effects examined Several compounds have a hypotensive activity parallel to that of nicardipine; the 4-(3-trifluoromethyl-2-pyridyl) and 4-(2-trifluoromethyl-3-pyridyl) derivatives, in particular, had approx. twice the duration of nicardipine, and the 4-(4-cyano-2-pyridyl) derivative had the most potent hypotensive activity of all the derivatives synthesized. In the experiment, the researchers used many compounds, for example, (4-Bromopyridin-2-yl)methanol (cas: 131747-45-0Recommanded Product: (4-Bromopyridin-2-yl)methanol).

(4-Bromopyridin-2-yl)methanol (cas: 131747-45-0) belongs to pyridine derivatives. Pyridine has a dipole moment and a weaker resonant stabilization than benzene (resonance energy 117 kJ·mol−1 in pyridine vs. 150 kJ·mol−1 in benzene). Several pyridine derivatives play important roles in biological systems. While its biosynthesis is not fully understood, nicotinic acid (vitamin B3) occurs in some bacteria, fungi, and mammals.Recommanded Product: (4-Bromopyridin-2-yl)methanol

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

Scalable Rhodium(III)-Catalyzed Aryl C-H Phosphorylation Enabled by Anodic Oxidation Induced Reductive Elimination was written by Wu, Zheng-Jian;Su, Feng;Lin, Weidong;Song, Jinshuai;Wen, Ting-Bin;Zhang, Hui-Jun;Xu, Hai-Chao. And the article was included in Angewandte Chemie, International Edition in 2019.HPLC of Formula: 4783-68-0 This article mentions the following:

Transition metal catalyzed C-H phosphorylation remains an unsolved challenge. Reported methods are generally limited in scope and require stoichiometric silver salts as oxidants. Reported here is an electrochem. driven Rh^III-catalyzed aryl C-H phosphorylation reaction that proceeds through H₂ evolution, obviating the need for stoichiometric metal oxidants. The method is compatible with a variety of aryl C-H and P-H coupling partners and particularly useful for synthesizing triarylphosphine oxides from diarylphosphine oxides, which are often difficult coupling partners for transition metal catalyzed C-H phosphorylation reactions. Exptl. results suggest that the mechanism responsible for the C-P bond formation involves an oxidation-induced reductive elimination process. In the experiment, the researchers used many compounds, for example, 2-Phenoxypyridine (cas: 4783-68-0HPLC of Formula: 4783-68-0).

2-Phenoxypyridine (cas: 4783-68-0) belongs to pyridine derivatives. Pyridine’s the lone pair does not contribute to the aromatic system but importantly influences the chemical properties of pyridine, as it easily supports bond formation via an electrophilic attack. Halopyridines are particularly attractive synthetic building blocks in a variety of cross-coupling methods, including the Suzuki-Miyaura cross-coupling reaction.HPLC of Formula: 4783-68-0

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

C-5 Substituted heteroaryl 3-pyridinecarbonitriles as PKCθ inhibitors: Part I was written by Subrath, Joan;Wang, Daniel;Wu, Biqi;Niu, Chuansheng;Boschelli, Diane H.;Lee, Julie;Yang, Xiaoke;Brennan, Agnes;Chaudhary, Divya. And the article was included in Bioorganic & Medicinal Chemistry Letters in 2009.Application of 1073354-14-9 This article mentions the following:

We earlier reported that 3-pyridinecarbonitriles with a 4-methylindolyl-5-amino group at C-4 and a Ph group at C-5 were inhibitors of PKCθ. Keeping the group at C-4 of the pyridine core constant, we varied the water solubilizing group on the Ph ring at C-5 and then replaced the C-5 Ph ring with several monocyclic heteroaryl rings, including furan, thiophene and pyridine. Analog 6e (I) with a 4-methylindol-5-ylamino group at C-4 and a 5-[(4-methylpiperazin-1-yl)methyl]-2-furyl group C-5 had an IC₅₀ value of 4.5 nM for the inhibition of PKCθ. In the experiment, the researchers used many compounds, for example, 5-(4,4,5,5-Tetramethyl-1,3,2-dioxaborolan-2-yl)picolinaldehyde (cas: 1073354-14-9Application of 1073354-14-9).

5-(4,4,5,5-Tetramethyl-1,3,2-dioxaborolan-2-yl)picolinaldehyde (cas: 1073354-14-9) belongs to pyridine derivatives. The ring atoms in the pyridine molecule are sp2-hybridized. The nitrogen is involved in the π-bonding aromatic system using its unhybridized p orbital. The lone pair is in an sp2 orbital, projecting outward from the ring in the same plane as the σ bonds. Reduced pyridines, namely tetrahydropyridines, dihydropyridines and piperidines, are found in numerous natural and synthetic compounds. The synthesis and reactivity of these compounds have often been driven by the fact many of these compounds have interesting and unique pharmacological properties. Application of 1073354-14-9

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem