Tag: 100-200

The author of 《Design and Activity of Novel Oxadiazole Based Compounds That Target Poly(ADP-ribose) Polymerase》 were Vishwanath, Divakar; Girimanchanaika, Swamy S.; Dukanya, Dukanya; Rangappa, Shobith; Yang, Ji-Rui; Pandey, Vijay; Lobie, Peter E.; Basappa, Basappa. And the article was published in Molecules in 2022. Name: (6-Chloro-5-methylpyridin-3-yl)boronic acid The author mentioned the following in the article:

Novel PARP inhibitors with selective mode-of-action have been approved for clin. use. Herein, oxadiazole based ligands that are predicted to target PARP-1 have been synthesized and screened for the loss of cell viability in mammary carcinoma cells, wherein seven compounds were observed to possess significant IC50 values in the range of 1.4 to 25 μM. Furthermore, compound 5u, inhibited the viability of MCF-7 cells with an IC50 value of 1.4μM, when compared to Olaparib (IC50 = 3.2 μM). Compound 5s also decreased cell viability in MCF-7 and MDA-MB-231 cells with IC50 values of 15.3 and 19.2 μM, resp. Treatment of MCF-7 cells with compounds 5u and 5s produced PARP cleavage, H2AX phosphorylation and CASPASE-3 activation comparable to that observed with Olaparib. Compounds 5u and 5s also decreased foci-formation and 3D Matrigel growth of MCF-7 cells equivalent to or greater than that observed with Olaparib. Finally, in silico anal. demonstrated binding of compound 5s towardsthe catalytic site of PARP-1, indicating that these novel oxadiazoles synthesized herein may serve as exemplars for the development of new therapeutics in cancer. In the part of experimental materials, we found many familiar compounds, such as (6-Chloro-5-methylpyridin-3-yl)boronic acid(cas: 1003043-40-0Name: (6-Chloro-5-methylpyridin-3-yl)boronic acid)

(6-Chloro-5-methylpyridin-3-yl)boronic acid(cas: 1003043-40-0) belongs to pyridine. Pyridine, its benzo and pyridine-based compounds play diverse roles in organic chemistry. As ligands, solvents, and catalysts they facilitate reactions; thus descriptions of these new ligands and their applications abound each year.Name: (6-Chloro-5-methylpyridin-3-yl)boronic acid

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

In 2017,Li, Zhao; Gelbaum, Carol; Campbell, Zachary S.; Gould, Paul C.; Fisk, Jason S.; Holden, Bruce; Jaganathan, Arvind; Whiteker, Gregory T.; Pollet, Pamela; Liotta, Charles L. published 《Pd-Catalyzed Suzuki coupling reactions of aryl halides containing basic nitrogen centers with arylboronic acids in water in the absence of added base》.New Journal of Chemistry published the findings.Synthetic Route of C5H5BrN2 The information in the text is summarized as follows:

The Pd-catalyzed Suzuki coupling reactions of a series of aryl chlorides and aryl bromides containing basic nitrogen centers with arylboronic acids in water in the absence of added base were reported. The reactions proceeded either partially or entirely under acidic conditions. After surveying twenty-two phosphorus ligands, high yields of products were obtained with aryl chlorides only when a bulky ligand, 2-(di-tert-butyl-phosphino)-1-phenyl-1H-pyrrole (cataCXiumPtB) was used. In contrast, aryl bromides produced high yields of products in the absence of both added base and added ligand. In order to explore the Suzuki coupling process entirely under acidic conditions, a series of reactions were conducted in buffered acidic media using several model substrates. 4-Chlorobenzylamine, in the presence of cataCXiumPtB, produced high yields of product at buffered pH 6.0; the yields dropped off precipitously at buffered pH 5.0 and lower. The fall-off in yield was attributed to the decomposition of the Pd-ligand complex due to the protonation of the ligand in the more acidic aqueous media. In contrast, in the absence of an added ligand, 4-amino-2-chloropyridine produced quant. yields at buffered pH 3.5 and 4.5 while 4-amino-2-bromopyridine produced quant. yields in a series of buffered media ranging from pH 4.5 to 1.5. These substrates were only partially protonated in acidic media and could behave as active Pd ligands in the Suzuki catalytic cycle.6-Bromopyridin-3-amine(cas: 13534-97-9Synthetic Route of C5H5BrN2) was used in this study.

6-Bromopyridin-3-amine(cas: 13534-97-9) belongs to anime. Amines characteristically form salts with acids; a hydrogen ion, H+, adds to the nitrogen. With the strong mineral acids (e.g., H2SO4, HNO3, and HCl), the reaction is vigorous. Salt formation is instantly reversed by strong bases such as NaOH. Neutral electrophiles (compounds attracted to regions of negative charge) also react with amines; alkyl halides (R′X) and analogous alkylating agents are important examples of electrophilic reagents.Synthetic Route of C5H5BrN2

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

Dogan, Sengul Dilem; Demirpolat, Eren; Yerer Aycan, Mukerrem Betul; Balci, Metin published an article on January 14 ,2015. The article was titled 《Synthesis of new 4-aza-indoles via acyl azides》, and you may find the article in Tetrahedron.COA of Formula: C9H12N2O2 The information in the text is summarized as follows:

The authors hereby report the preparation of new azaindole derivatives starting from 2-(2-ethoxy-2-oxoethyl)nicotinic acid. Conversion of a half ester into acyl azide followed by Curtius rearrangement gave the corresponding isocyanate. Trapping of the isocyanate with different nucleophiles produced urea and urethane derivatives Intramol. cyclization reactions gave the target compounds In addition to this study using Ethyl 2-(3-aminopyridin-2-yl)acetate, there are many other studies that have used Ethyl 2-(3-aminopyridin-2-yl)acetate(cas: 295327-27-4COA of Formula: C9H12N2O2) was used in this study.

Ethyl 2-(3-aminopyridin-2-yl)acetate(cas: 295327-27-4) belongs to anime. To avoid the problem of multiple alkylation, methods have been devised for “blocking” substitution so that only one alkyl group is introduced. The Gabriel synthesis is one such method; it utilizes phthalimide, C6H4(CO)2NH, whose one acidic hydrogen atom has been removed upon the addition of a base such as KOH to form a salt.COA of Formula: C9H12N2O2

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

《Selective C-H trifluoromethoxylation of (hetero)arenes as limiting reagent》 was written by Deng, Zhijie; Zhao, Mingxin; Wang, Feng; Tang, Pingping. Reference of 4-CyanopyridineThis research focused ontrifluoromethoxylated compound preparation regioselective; arene heteroarene trifluoromethyl arylsulfonate trifluoromethoxylation. The article conveys some information:

A general late-stage C-H trifluoromethoxylation of arenes and heteroarenes RH (R = 4-methoxypyridin-2-yl, 4-t-butylphenyl, 3-acetylbenzothien-2-yl, etc.) as limiting reagent with trifluoromethoxide anion was described. The reaction is mediated by silver salts under mild reaction conditions, exhibiting broad substrate scope and wide functional-group compatibility. In addition, ortho-position selective C-H trifluoromethoxylation of pyridines is observed The method is not only applicable to the gram-scale synthesis of trifluoromethoxylated products ROCF3 but also allows efficient late-stage C-H trifluoromethoxylation of marketed small-mol. drugs, common pharmacophores and natural products. In the experimental materials used by the author, we found 4-Cyanopyridine(cas: 100-48-1Reference of 4-Cyanopyridine)

4-Cyanopyridine(cas: 100-48-1) belongs to pyridine. Pyridine-based materials are valued for their optical and physical properties as well as their medical potential. Additionally, pyridine-based natural products continue to be discovered and studied for their properties and to understand their biosynthesis.Reference of 4-Cyanopyridine

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

《Rational design, synthesis and testing of novel tricyclic topoisomerase inhibitors for the treatment of bacterial infections part 1》 was written by Kirk, R.; Ratcliffe, A.; Noonan, G.; Uosis-Martin, M.; Lyth, D.; Bardell-Cox, O.; Massam, J.; Schofield, P.; Hindley, S.; Jones, D. R.; Maclean, J.; Smith, A.; Savage, V.; Mohmed, S.; Charrier, C.; Salisbury, A-M.; Moyo, E.; Metzger, R.; Chalam-Judge, N.; Cheung, J.; Stokes, N. R.; Best, S.; Craighead, M.; Armer, R.; Huxley, A.. Recommanded Product: 6-Bromopyridin-3-amineThis research focused ontricyclic topoisomerase inhibitor bacterial infection treatment. The article conveys some information:

The alarming reduction in drug effectiveness against bacterial infections has created an urgent need for the development of new antibacterial agents that circumvent bacterial resistance mechanisms. We report here a series of DNA gyrase and topoisomerase IV inhibitors that demonstrate potent activity against a range of Gram-pos. and selected Gram-neg. organisms, including clin.-relevant and drug-resistant strains. In part 1, we present a detailed structure activity relationship (SAR) anal. that led to the discovery of our previously disclosed compound, REDX05931, which has a min. inhibitory concentration (MIC) of 0.06 μg mL-1 against fluoroquinolone-resistant Staphylococcus aureus. Although in vitro hERG and CYP inhibition precluded further development, it validates a rational design approach to address this urgent unmet medical need and provides a scaffold for further optimization, which is presented in part 2. The experimental part of the paper was very detailed, including the reaction process of 6-Bromopyridin-3-amine(cas: 13534-97-9Recommanded Product: 6-Bromopyridin-3-amine)

6-Bromopyridin-3-amine(cas: 13534-97-9) belongs to anime. Amines characteristically form salts with acids; a hydrogen ion, H+, adds to the nitrogen. With the strong mineral acids (e.g., H2SO4, HNO3, and HCl), the reaction is vigorous. Salt formation is instantly reversed by strong bases such as NaOH. Neutral electrophiles (compounds attracted to regions of negative charge) also react with amines; alkyl halides (R′X) and analogous alkylating agents are important examples of electrophilic reagents.Recommanded Product: 6-Bromopyridin-3-amine

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

SDS of cas: 128071-75-0In 2018 ,《Zincation and Magnesiation of Functionalized Silylated Cyanohydrins Using TMP-Bases》 was published in Synthesis. The article was written by Castello-Mico, Alicia; Knochel, Paul. The article contains the following contents:

Polyfunctional silylated cyanohydrins are readily magnesiated or zincated with TMPMgCl·LiCl or TMP2Zn·2MgCl2·2LiCl leading to the corresponding metalated derivatives These Mg- or Zn-derivatives react with various electrophiles such as benzylic bromides, allylic bromides, acid chlorides, aldehydes, NCCO2Et, or MeSO2SMe. Subsequently, TBAF-deprotection provides the corresponding keto or 1,2-diketo derivatives2-Bromonicotinaldehyde(cas: 128071-75-0SDS of cas: 128071-75-0) was used in this study.

2-Bromonicotinaldehyde(cas: 128071-75-0) 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. SDS of cas: 128071-75-0

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

Category: pyridine-derivativesIn 2020 ,《Failure of 2-pyridinecarboxylic acid, an inhibitor of 1-aminocyclopropane-1-carboxylate oxidase, as a universal flower care agent to extend the vase lifeof cut carnation flowers》 appeared in Horticulture Journal. The author of the article were Satoh, Shigeru; Makino, Keiko; Shimada, Keita; Nomura, Yoshihiro. The article conveys some information:

The 2-Pyridinecarboxylic acid (2-PCA) acts as an inhibitor of ethylene biosynthesis in Arabidopsis thaliana by binding to the active site of 1-aminocyclopropane-1-carboxylate oxidase. In this study, we examined the action of 2-PCA in comparison with the action of 3-PCA, a recently discovered stimulator of flower opening, in cut flowers of the spray-type carnation cultivars, ‘Light Pink Barbara (LPB)’, ‘Carnet’, ‘Collin’, and ‘Zulia’. With ‘LPB’ flowers, 2-PCA at 0.5-5 mM did not prolong the vase life, whereas 3-PCA at 5 mM did so. With the other three cultivars, 3-PCA generally promoted flower opening of all the cultivars. On the other hand, the action of 2-PCA on flower opening and senescence varied with the carnation cultivar and time of harvest, resulting in a shortened, unchanged or lengthened vase life of the flowers. 2-PCA also caused severe bending of flower stems in all cultivars, which lowered the display value of the flowers. The present results showed that 2-PCA is not likely to be a useful flower care agent in carnation flowers. The experimental part of the paper was very detailed, including the reaction process of Picolinic acid(cas: 98-98-6Category: pyridine-derivatives)

Picolinic acid(cas: 98-98-6) is used as a chelate for alkaline earth metals. Used to prepare picolinato ligated transition metal complexes. In synthetic organic chemistry, has been used as a substrate in the Mitsunobu reaction and in the Hammick reaction.Category: pyridine-derivatives

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

Product Details of 1122-54-9In 2019 ,《One-pot metal-free synthesis of 3-CF3-1,3-oxazinopyridines by reaction of pyridines with CF3CO-acetylenes》 appeared in Molecules. The author of the article were Muzalevskiy, Vasiliy M.; Sizova, Zoia A.; Belyaeva, Kseniya V.; Trofimov, Boris A.; Nenajdenko, Valentine G.. The article conveys some information:

The reaction of pyridines with trifluoroacetylated acetylenes was investigated. It was found that the reaction of various pyridines with two mols. of CF3CO-acetylenes proceeded under mild metal-free conditions. As a result, efficient stereoselective synthesis of 3-arylethynyl-3-trifluoromethyl-1,3-oxazinopyridines was elaborated. Target heterocycles were prepared in up to quant. yields. In the part of experimental materials, we found many familiar compounds, such as 4-Acetylpyridine(cas: 1122-54-9Product Details of 1122-54-9)

4-Acetylpyridine(cas: 1122-54-9) belongs to pyridine. The basicity and metallophilic high donor number of these π-deficient systems has long favored them as ligands in metal catalysis. The last decade saw pyridine assume a stronger role as functional group for directed C–H oxidation/activation.Product Details of 1122-54-9

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

Safety of 4-EthynylpyridineIn 2022 ,《Fuel Acid Drives Base Catalysis and Supramolecular Cage-to-Device Transformation under Dissipative Conditions》 appeared in Organic Letters. The author of the article were Mondal, Debabrata; Ghosh, Amit; Paul, Indrajit; Schmittel, Michael. The article conveys some information:

In State-I, a mixture comprising a DABCO-bridged tris(zinc-porphyrin) double decker and a free biped (=slider), catalysis was OFF. Acid addition (TFA or Di-Stefano fuel acid) to State-I liberated DABCO-H+ while generating a highly dynamic slider-on-deck device (State-II). The released DABCO-H+ acted as a base organocatalyst for a Knoevenagel reaction (catalysis ON). The system was reversed to State-I (catalysis OFF) by reducing the acidity in the system (by adding DBU or via the fuel-derived base). In the experiment, the researchers used 4-Ethynylpyridine(cas: 2510-22-7Safety of 4-Ethynylpyridine)

4-Ethynylpyridine(cas: 2510-22-7) 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. Safety of 4-Ethynylpyridine

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

In 2022,Tang, Jiali; Chen, Yingbi; Wang, Shixing; Kong, Desong; Zhang, Libo published an article in Environmental Research. The title of the article was 《Highly efficient metal-organic frameworks adsorbent for Pd(II) and Au(III) recovery from solutions: Experiment and mechanism》.Name: 2,6-Diaminopyridine The author mentioned the following in the article:

With the boom of modern industry, the demand for precious metals palladium (Pd) and gold (Au) is increasing. However, the discharge of Pd(II) and Au(III) wastewater has caused environmental pollution and shortage of resources. Here, a new metal-organic frameworks adsorbent (MOF-AFH) was synthesized to efficiently sep. Pd(II) and Au(III) from the water. The adsorption behavior of Pd(II) and Au(III) was explored at the same time. When gold and palladium are adsorbed sep., the adsorption capacity of gold and palladium is 389.02 mg/g and 191.27 mg/g, resp. The equilibration time is 3 h. When gold and palladium coexist, the adsorption capacities of Au(III) and Pd(II) are 238.71 and 115.02 mg/g, resp. The exptl. results show that the adsorption of Pd(II) and Au(III) on MOF-AFH is a single-layer chem. adsorption, which is an endothermic process. MOF-AFH has excellent selectivity and after MOF-AFH is repeatedly used 4 times, the removal effect can still reach more than 90%. The adsorption mechanisms include reduction reaction and chelation with N and O-containing functional groups on the adsorbent. There is also electrostatic interaction for Au(III) adsorption. The adsorbent can be used to efficiently recover gold and palladium from wastewater. In the experimental materials used by the author, we found 2,6-Diaminopyridine(cas: 141-86-6Name: 2,6-Diaminopyridine)

2,6-Diaminopyridine(cas: 141-86-6) belongs to pyridine. Pyridine and its simple derivatives are stable and relatively unreactive liquids, with strong penetrating odours that are unpleasant.Name: 2,6-Diaminopyridine

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem