Tag: 100-200

In 2019,Organic & Biomolecular Chemistry included an article by Satpathi, Bishnupada; Dutta, Lona; Ramasastry, S. S. V.. Recommanded Product: 2-Bromonicotinaldehyde. The article was titled 《Phosphine- and water-promoted pentannulative aldol reaction》. The information in the text is summarized as follows:

An efficient metal-free intramol. aldol reaction for the synthesis of an unusual class of cyclopentanoids was described. The reaction of α-substituted dienones tethered with ketones in the presence of tributylphosphine and water provided aldols. The role of water was realized to be crucial for this transformation. Furthermore, isotopic labeling experiments provided vital information about the reaction mechanism. In the experiment, the researchers used 2-Bromonicotinaldehyde(cas: 128071-75-0Recommanded Product: 2-Bromonicotinaldehyde)

2-Bromonicotinaldehyde(cas: 128071-75-0) belongs to pyridine. Pyridine is very deactivated towards electrophilic substitution with respect to benzene. For this reason classical formylation, using methods such as the Gattermann or Vilsmeier reactions, are not generally successful. Recommanded Product: 2-Bromonicotinaldehyde

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

In 2019,Angewandte Chemie, International Edition included an article by Yang, Zhongming; Zhao, Weijia; Liu, Wei; Wei, Xing; Chen, Meng; Zhang, Xiao; Zhang, Xiaolei; Liang, Yong; Lu, Changsheng; Yan, Hong. Computed Properties of C7H9NO. The article was titled 《Metal-Free Oxidative B-N Coupling of nido-Carborane with N-Heterocycles》. The information in the text is summarized as follows:

A general method for the oxidative substitution of nido-carborane (7,8-C2B9H12-) with N-heterocycles has been developed by using 2,3-dichloro-5,6-dicyanobenzoquinone (DDQ) as an oxidant, producing 9-Het-7,8-R2-7,8-dicarbaundecaboranes(11) [Het = pyridine, (iso)quinoline, (benz)imidazole, (benzo)thiazole, oxazole, pyrazole, pyrimidine 6-azaindole; R = Ph, H, Me, tBu, RR = CH2CH:CHCH2]. This metal-free B-N coupling strategy, in both inter- and intramol. fashions, gave rise to a wide array of charge-compensated, boron-substituted nido-carboranes in high yields (up to 97%) with excellent functional-group tolerance under mild reaction conditions. The reaction mechanism was investigated by d.-functional theory (DFT) calculations A successive single-electron transfer (SET), B-H hydrogen-atom transfer (HAT), and nucleophilic attack pathway is proposed. This method provides a new approach to nitrogen-containing carboranes with potential applications in medicine and materials. In the part of experimental materials, we found many familiar compounds, such as 2-(2-Hydroxyethyl)pyridine(cas: 103-74-2Computed Properties of C7H9NO)

2-(2-Hydroxyethyl)pyridine(cas: 103-74-2) belongs to pyridine. Pyridines are often used as catalysts or reagents; particular notice has been paid recently to how pyridine coordinates to metal centers enabling a wide range of valuable reactions. Computed Properties of C7H9NO

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

In 2019,European Journal of Medicinal Chemistry included an article by Moir, Michael; Lane, Samuel; Lai, Felcia; Connor, Mark; Hibbs, David E.; Kassiou, Michael. Related Products of 128071-75-0. The article was titled 《Strategies to develop selective CB2 receptor agonists from indole carboxamide synthetic cannabinoids》. The information in the text is summarized as follows:

Activation of the CB2 receptor is an attractive therapeutic strategy for the treatment of a wide range of inflammatory diseases. However, receptor subtype selectivity is necessary in order to circumvent the psychoactive effects associated with activation of the CB1 receptor. We aimed to use potent, non-selective synthetic cannabinoids designer drugs to develop selective CB2 receptor agonists. Simple structural modifications such as moving the amide substituent of 3-amidoalkylindole synthetic cannabinoids to the 2-position and bioisosteric replacement of the indole core to the 7-azaindole scaffold are shown to be effective and general strategies to impart receptor subtype selectivity. 2-Amidoalkylindole 16 (EC50 CB1 > 10 μM, EC50 CB2 = 189 nM) and 3-amidoalkyl-7-azaindole 21 (EC50 CB1 > 10 μM, EC50 = 49 nM) were found to be potent and selective agonists with favorable physicochem. properties. Docking studies were used to elucidate the mol. basis for the observed receptor subtype selectivity for these compounds The experimental part of the paper was very detailed, including the reaction process of 2-Bromonicotinaldehyde(cas: 128071-75-0Related Products of 128071-75-0)

2-Bromonicotinaldehyde(cas: 128071-75-0) belongs to pyridine. Pyridines are often used as catalysts or reagents; particular notice has been paid recently to how pyridine coordinates to metal centers enabling a wide range of valuable reactions. Related Products of 128071-75-0

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

In 2019,Photochemical & Photobiological Sciences included an article by Kumar, Girijesh; Guda, Ramu; Husain, Ahmad; Patra, Ranjan; Kirandeep; Kasula, Mamatha. Reference of 4-Cyanopyridine. The article was titled 《Synthesis and photophysical properties of pyridyl conjugated triazole appended naphthalenediimide derivatives》. The information in the text is summarized as follows:

A series of three substituted triazole appended naphthalenediimide (NDI)-derivatives, 2,7-bis(3,5-di(pyridin-X-yl)-4H-1,2,4-triazol-4-yl)benzo[lmn][3,8]phenanthroline-1,3,6,8(2H,7H)-tetraones (where X = 2, NDI-PyTz-1; 3, NDI-PyTz-2; and 4, NDI-PyTz-3), were designed, synthesized and well characterized using various anal. and spectroscopic techniques. All the three NDI-PyTz derivatives exhibited decent electronic properties as suggested by DFT, cyclic voltammetry and fluorescence studies. In particular, NDI-PyTz-1 demonstrated the generation of a stable anion radical [NDI-PyTz-1].-. In the part of experimental materials, we found many familiar compounds, such as 4-Cyanopyridine(cas: 100-48-1Reference of 4-Cyanopyridine)

4-Cyanopyridine(cas: 100-48-1) belongs to pyridine. Pyridine’s structure is isoelectronic with that of benzene, but its properties are quite different. Pyridine is completely miscible with water, whereas benzene is only slightly soluble. Like all hydrocarbons, benzene is neutral (in the acid–base sense), but because of its nitrogen atom, pyridine is a weak base.Reference of 4-Cyanopyridine

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

In 2017,Silvi, Mattia; Sandford, Christopher; Aggarwal, Varinder K. published 《Merging Photoredox with 1,2-Metallate Rearrangements: The Photochemical Alkylation of Vinyl Boronate Complexes》.Journal of the American Chemical Society published the findings.Electric Literature of C5H3BrClN The information in the text is summarized as follows:

Vinyl boronates react with electron-deficient alkyl iodides in the presence of visible light to give boronic esters in which two new C-C bonds were created. The reaction occurs by radical addition of an electron-deficient alkyl radical to the vinyl boronate followed by electron transfer with another mol. of alkyl iodide, continuing the chain, and triggering a 1,2-metalate rearrangement. In a number of cases, the use of a photoredox catalyst enhances yields significantly. The scope of the radical precursor includes α-iodo ketones, esters, nitriles, primary amides, α-fluorinated halo-acetates and perfluoroalkyl iodides. In the experiment, the researchers used 5-Bromo-2-chloropyridine(cas: 53939-30-3Electric Literature of C5H3BrClN)

5-Bromo-2-chloropyridine(cas: 53939-30-3) belongs to pyridine. Pyridine derivatives lend themselves to many roles in the spirited field of supramolecular chemistry – whether as the ligand backbone of metal-organic polymers or presiding over the key electronic stations of nanodevices. In biochemistry, pyridine-containing cofactors are necessary nutrients on which our lives depend. Electric Literature of C5H3BrClN

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

In 2015,Mou, Jianfeng; Park, Ann; Cai, Yu; Yuan, Junying; Yuan, Chengye published 《Structure-activity relationship study of E6 as a novel necroptosis inducer》.Bioorganic & Medicinal Chemistry Letters published the findings.Reference of 6-Bromopyridin-3-amine The information in the text is summarized as follows:

Necroptosis inducers represent a promising potential treatment for drug-resistant cancer. We herein describe the structure modification of E6, which was identified recently as a potent and selective necroptosis inducer. The studies described herein demonstrate for the first time that functionalized biphenyl derivatives possess necroptosis inducer activity. Furthermore, these studies have led to the identification of two promising compounds (I; R = 4-OMe, R = 4-OEt) that can be used for further optimization studies as well as mechanism of action investigations. The experimental process involved the reaction of 6-Bromopyridin-3-amine(cas: 13534-97-9Reference of 6-Bromopyridin-3-amine)

6-Bromopyridin-3-amine(cas: 13534-97-9) belongs to anime. The reaction of alkyl halides, R―X, where X is a halogen, or analogous reagents with ammonia (or amines) is useful with certain compounds. Not all alkyl halides are effective reagents; the reaction is sluggish with secondary alkyl groups and fails with tertiary ones. Its usefulness is largely confined to primary alkyl halides (those having two hydrogen atoms on the reacting site).Reference of 6-Bromopyridin-3-amine

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

In 2013,Dai, Jian-Jun; Fang, Chi; Xiao, Bin; Yi, Jun; Xu, Jun; Liu, Zhao-Jing; Lu, Xi; Liu, Lei; Fu, Yao published 《Copper-Promoted Sandmeyer Trifluoromethylation Reaction》.Journal of the American Chemical Society published the findings.Category: pyridine-derivatives The information in the text is summarized as follows:

A copper-promoted trifluoromethylation reaction of aromatic amines is described. This transformation proceeds smoothly under mild conditions and exhibits good tolerance of many synthetically relevant functional groups. It provides an alternative approach for the synthesis of trifluoromethylated arenes and heteroarenes. It also constitutes a new example of the Sandmeyer reaction. The experimental part of the paper was very detailed, including the reaction process of 6-Bromopyridin-3-amine(cas: 13534-97-9Category: pyridine-derivatives)

6-Bromopyridin-3-amine(cas: 13534-97-9) belongs to anime. The reaction of alkyl halides, R―X, where X is a halogen, or analogous reagents with ammonia (or amines) is useful with certain compounds. Not all alkyl halides are effective reagents; the reaction is sluggish with secondary alkyl groups and fails with tertiary ones. Its usefulness is largely confined to primary alkyl halides (those having two hydrogen atoms on the reacting site).Category: pyridine-derivatives

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

Wu, Zhibing; Park, Hyung-Yeon; Xie, Dewen; Yang, Jingxin; Hou, Shuaitao; Shahzad, Nasir; Kim, Chan Kyung; Yang, Song published an article on February 3 ,2021. The article was titled 《Synthesis, Biological Evaluation, and 3D-QSAR Studies of N-(Substituted pyridine-4-yl)-1-(substituted phenyl)-5-trifluoromethyl-1H-pyrazole-4-carboxamide Derivatives as Potential Succinate Dehydrogenase Inhibitors》, and you may find the article in Journal of Agricultural and Food Chemistry.Recommanded Product: 4-Amino-2-picoline The information in the text is summarized as follows:

To develop more potential succinate dehydrogenase (SDH) inhibitors, we designed and synthesized a novel series of N-(substituted pyridine-4-yl)-1-(substituted phenyl)-5-trifluoromethyl-1H-pyrazole-4-carboxamide derivatives, I [R1 = H, CH3, F, Cl; R2 = 2-pyridinyl, 4-pyridinyl, 2-CH3-4-pyridinyl, etc.]. The bioassay results demonstrated that some title compounds exhibited excellent antifungal activity against four tested phytopathogenic fungi (Gibberella zea, Fusarium oxysporum, Cytospora mandshurica, and Phytophthora infestans). The EC50 values were 1.8μg/mL for I [R1 = Cl; R2 = 4-pyridinyl] against G. zeae, 1.5 and 3.6μg/mL for I [R1 = Cl; R2 = 2-CH3-4-pyridinyl] against F. oxysporum and C. mandshurica, resp., and 6.8μg/mL for I [R1 = F; R2 = 2-CH3-4-pyridinyl] against P. infestans. The SDH enzymic activity testing revealed that the IC50 values of I [R1 = H; R2 = 4-pyridinyl], I [R1 = CH3; R2 = 4-pyridinyl], I [R1 = F; R2 = 2-CH3-4-pyridinyl], and penthiopyrad were 12.5, 135.3, 6.9, and 223.9μg/mL, resp. The mol. docking results of this series of title compounds with SDH model demonstrated that the compounds could completely locate inside of the pocket, the body fragment formed H bonds, and the Ph ring showed a π-π interaction with Arg59, suggesting that these novel 5-trifluoromethyl-pyrazole-4-carboxamide derivatives might target SDH. These results provided a benchmark for understanding the antifungal activity against the phytopathogenic fungus P. infestans and prompt us to discover more potent SDH inhibitors.4-Amino-2-picoline(cas: 18437-58-6Recommanded Product: 4-Amino-2-picoline) was used in this study.

4-Amino-2-picoline(cas: 18437-58-6) belongs to anime. Many important products require amines as part of their syntheses. Methylamine is utilized in the production of the analgesic meperidine (trade name Demerol) and the photographic developer Metol (trademark), and dimethylamine is used in the synthesis of the antihistamine diphenhydramine (trade name Benadryl), the solvent dimethylformamide (DMF), and the rocket propellant 1,1-dimethylhydrazine. The synthesis of the insect repellent N,N-diethyl-m-toluamide (DEET) incorporates diethylamine while that of the synthetic fibre Kevlar requires aromatic amines.Recommanded Product: 4-Amino-2-picoline

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

Application In Synthesis of 2-Bromopyridin-3-amineOn March 21, 2022, Salameh, Nihad; Ferlin, Francesco; Valentini, Federica; Anastasiou, Ioannis; Vaccaro, Luigi published an article in ACS Sustainable Chemistry & Engineering. The article was 《Waste-Minimized Continuous-Flow Synthesis of Oxindoles Exploiting a Polymer-Supported N Heterocyclic Palladium Carbene Complex in a CPME/Water Azeotrope》. The article mentions the following:

The development of an effective synthetic protocol for the synthesis of oxindoles in flow based on a C(sp3)-H activation process promoted by a supported N-heterocyclic carbene palladium heterogeneous catalytic system using cyclopentyl Me ether (CPME) as the reaction medium was reported. The design of the catalyst, the selection of the solvent medium, and the definition of a tailored continuous flow reactor have been all designed to establish an efficient waste-minimized process for the intramol. cyclization of N-methyl-2-halo-acetanilides. The use of CPME in its aqueous azeotropic mixture has allowed to reach high yields of products with a simplified precipitation workup that includes the downstream process separation and recycling of the solvent. An assessment of the environmental and safety hazard features has also been made in order to better clarify the implications in terms of sustainability of the newly developed process. The experimental part of the paper was very detailed, including the reaction process of 2-Bromopyridin-3-amine(cas: 39856-58-1Application In Synthesis of 2-Bromopyridin-3-amine)

2-Bromopyridin-3-amine(cas: 39856-58-1) belongs to anime. The reaction of alkyl halides, R―X, where X is a halogen, or analogous reagents with ammonia (or amines) is useful with certain compounds. Not all alkyl halides are effective reagents; the reaction is sluggish with secondary alkyl groups and fails with tertiary ones. Its usefulness is largely confined to primary alkyl halides (those having two hydrogen atoms on the reacting site).Application In Synthesis of 2-Bromopyridin-3-amine

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

Category: pyridine-derivativesIn 2020 ,《Design, Drug-Likeness, Synthesis, Characterization, Antimicrobial Activity, Molecular Docking, and MTT Assessment of 1,3-Thiazolidin-4-one Bearing Piperonal and Pyrimidine Moieties》 was published in Russian Journal of Bioorganic Chemistry. The article was written by Mohammad Arshad. The article contains the following contents:

The recent study reported the designing of substituted 3-[4-(1,3-benzodioxol-5-yl)-6-(pyridin-2-yl)pyrimidin-2-yl]-2-(pyridin-2-yl)-1,3-thiazolidin-4-one derivatives and assessed computationally to calculate the bioactivity and physicochem. properties. The substituted 3-[4-(1,3-benzodioxol-5-yl)-6-(pyridin-2-yl)pyrimidin-2-yl]-2-(pyridin-2-yl)-1,3-thiazolidin-4-one derivatives represented the bioactivity score in the zone for an active drug mol. and were in compliance with the Lipinski Rule of five. Then the synthesis, characterization, and biol. screening as antimicrobial potential and percent viability of cells were carried out for the substituted 3-[4-(1,3-benzodioxol-5-yl)-6-(pyridin-2-yl)pyrimidin-2-yl]-2-(pyridin-2-yl)-1,3-thiazolidin-4-one derivatives The zone of inhibition and min. inhibitory concentration (MIC) findings portrayed that the compounds-(IV) and compound-(V) possessed better antimicrobial activity than the reference drug ciprofloxacin, while the significant antimicrobial potential was observed by other members of the series. The mol. docking studies were performed to assist the in vitro antimicrobial results and the findings exhibited that significant H-bonding in between the substituted 3-[4-(1,3-benzodioxol-5-yl)-6-(pyridin-2-yl)pyrimidin-2-yl]-2-(pyridin-2-yl)-1,3-thiazolidin-4-one derivatives and the residues of GlcN-6-P-synthase, like ASP 474 (I-IX), SER 316 (I-VI), ASN 522 (I-IX), TRP 313 (V) with good binding affinity ranging -7.7 to -6.8 kcal/mol. The compounds represented the less toxic effects to the HepG2 cells and the percent viability of the cells ranging from 93-98%, 73-78% and 70-76% up to 3.125, 50, 100 mmol/L resp. In the part of experimental materials, we found many familiar compounds, such as 4-Acetylpyridine(cas: 1122-54-9Category: pyridine-derivatives)

4-Acetylpyridine(cas: 1122-54-9) belongs to pyridine. Pyridines, quinolines, and isoquinolines have found a function in almost all aspects of organic chemistry. Pyridine has found use as a solvent, base, ligand, functional group, and molecular scaffold. As structural elements, these moieties are potent electron-deficient groups, metal-directing functionalities, fluorophores, and medicinally important pharmacophores. Category: pyridine-derivatives

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem