Tag: 100-200

In 2015,Maity, Pintu; Kundu, Debasish; Ranu, Brindaban C. published 《Visible-Light-Photocatalyzed Metal-Free C-H Heteroarylation of Heteroarenes at Room Temperature: A Sustainable Synthesis of Biheteroaryls》.European Journal of Organic Chemistry published the findings.Application In Synthesis of 6-Bromopyridin-3-amine The information in the text is summarized as follows:

An efficient C-H heteroarylation of heteroarenes is achieved through visible-light photoredox-catalyzed diazotization of heteroarylamines in situ by tBuONO at room temperature A library of functionalized biheteroaryls is obtained by using this protocol. The reaction avoids the use of transition-metal catalysts, additives, and acidic reaction medium. In addition to this study using 6-Bromopyridin-3-amine, there are many other studies that have used 6-Bromopyridin-3-amine(cas: 13534-97-9Application In Synthesis of 6-Bromopyridin-3-amine) was used in this study.

6-Bromopyridin-3-amine(cas: 13534-97-9) belongs to anime. Amines can be classified according to the nature and number of substituents on nitrogen. Aliphatic amines contain only H and alkyl substituents. Aromatic amines have the nitrogen atom connected to an aromatic ring.Important amines include amino acids, biogenic amines, trimethylamine, and aniline. Inorganic derivatives of ammonia are also called amines, such as monochloramine (NClH2).Application In Synthesis of 6-Bromopyridin-3-amine

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

In 2014,Flanagan, Jack U.; Atwell, Graham J.; Heinrich, Daniel M.; Brooke, Darby G.; Silva, Shevan; Rigoreau, Laurent J. M.; Trivier, Elisabeth; Turnbull, Andrew P.; Raynham, Tony; Jamieson, Stephen M. F.; Denny, William A. published 《Morpholylureas as a new class of potent and selective inhibitors of the type 5 17-β-hydroxysteroid dehydrogenase (AKR1C3)》.Bioorganic & Medicinal Chemistry published the findings.Computed Properties of C5H3BrClN The information in the text is summarized as follows:

Inhibitors of the aldo-keto reductase enzyme AKR1C3 are of interest as potential drugs for leukemia and hormone-related cancers. A series of non-carboxylate morpholino(phenylpiperazin-1-yl)methanones were prepared by palladium-catalyzed coupling of substituted Ph or pyridyl bromides with the known morpholino(piperazin-1-yl)methanone, and shown to be potent (IC50 ∼ 100 nM) and very isoform-selective inhibitors of AKR1C3. Lipophilic electron-withdrawing substituents on the Ph ring were pos. for activity, as was an H-bond acceptor on the other terminal ring, and the ketone moiety (as a urea) was essential. These structure-activity relationships are consistent with an X-ray structure of a representative compound bound in the AKR1C3 active site, which showed H-bonding between the carbonyl oxygen of the drug and Tyr55 and His117 in the ‘oxyanion hole’ of the enzyme, with the piperazine bridging unit providing the correct twist to allow the terminal benzene ring to occupy the lipophilic pocket and align with Phe311.5-Bromo-2-chloropyridine(cas: 53939-30-3Computed Properties of C5H3BrClN) was used in this study.

5-Bromo-2-chloropyridine(cas: 53939-30-3) belongs to pyridine. When pyridine is adsorbed on oxide surfaces or in porous materials, the following species are commonly observed: (i) pyridine coordinated to Lewis acid sites, (ii) pyridine H-bonded to weakly acidic hydroxyls, and (iii) protonated pyridine. At high coverage, physisorbed pyridine and protonated dimers can also be observed.Computed Properties of C5H3BrClN

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

In 2013,Zhang, Yuanyuan; Yang, Weiqing; Xu, Keping; Ma, Menglin; Wang, Yuliang published 《Synthesis and antibacterial activities of pleuromutilin derivatives containing aryl urea groups》.Letters in Drug Design & Discovery published the findings.Safety of 6-Bromopyridin-3-amine The information in the text is summarized as follows:

A series of novel pleuromutilin derivatives containing aryl urea groups was synthesized and their antibacterial activity was evaluated in vitro against Staphylococcus aureus ATCC 26113, Staphylococcus aureus SC, Staphylococcus albus ATCC 8799 and Pseudomonas aeruginosa ATCC 27853. Most of compounds exhibited more potent activities than reference drug Tiamulin against Staphylococcus aureus ATCC 26113 and Saphylococcus aureus SC. Several compounds containing a pyridine urea group and a compound with a quinoline urea group showed excellent activity with the MIC value less than 0.001 μg/mL against Staphylococcus aureus SC. The title compounds thus formed included a thioether urea pyridine derivative (I) and related substances. The synthesis of the target compounds was achieved by a reaction of 2-[(2-amino-1,1-dimethylethyl)thio]acetic acid 6-ethenyldecahydro-5-hydroxy-4,6,9,10-tetramethyl-1-oxo-3a,9-propano-3aH-cyclopentacycloocten-8-yl ester with 2,2,2-trichloro-N-phenylacetamide derivatives and analogs. In the experiment, the researchers used 6-Bromopyridin-3-amine(cas: 13534-97-9Safety of 6-Bromopyridin-3-amine)

6-Bromopyridin-3-amine(cas: 13534-97-9) 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.Safety of 6-Bromopyridin-3-amine

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

Related Products of 18437-58-6On October 17, 2020 ,《Zinc-Catalyzed N-Alkylation of Aromatic Amines with Alcohols: A Ligand-Free Approach》 was published in Advanced Synthesis & Catalysis. The article was written by Sankar, Velayudham; Kathiresan, Murugavel; Sivakumar, Bitragunta; Mannathan, Subramaniyan. The article contains the following contents:

An efficient zinc-catalyzed N-alkylation reaction of aromatic amines was achieved using aliphatic, aromatic and heteroaromatic alcs. as the alkylating reagent. A variety of aniline derivatives, including heteroaromatic amines, underwent the N-alkylation reaction and furnished N-alkyl amines in good to excellent yields. The application of reaction was also further demonstrated by the synthesis of 2-phenylquinoline from acetophenone and 2-aminobenzyl alc. Deuterium labeling experiments showed that the reaction proceeded via a borrowing hydrogen process. The experimental part of the paper was very detailed, including the reaction process of 4-Amino-2-picoline(cas: 18437-58-6Related Products of 18437-58-6)

4-Amino-2-picoline(cas: 18437-58-6) belongs to anime. The methylamines occur in small amounts in some plants. Many polyfunctional amines (i.e., those having other functional groups in the molecule) occur as alkaloids in plants—for example, mescaline, 2-(3,4,5-trimethoxyphenyl)ethylamine; the cyclic amines nicotine, atropine, morphine, and cocaine; and the quaternary salt choline, N-(2-hydroxyethyl)trimethylammonium chloride, which is present in nerve synapses and in plant and animal cells.Related Products of 18437-58-6

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

Recommanded Product: 1206978-15-5On November 30, 2017 ,《Tri- and difluoromethoxylated N-based heterocycles – Synthesis and insecticidal activity of novel F3CO- and F2HCO-analogues of Imidacloprid and Thiacloprid》 appeared in Journal of Fluorine Chemistry. The author of the article were Landelle, Gregory; Schmitt, Etienne; Panossian, Armen; Vors, Jean-Pierre; Pazenok, Sergiy; Jeschke, Peter; Gutbrod, Oliver; Leroux, Frederic R.. The article conveys some information:

The preparation of F3CO- and F2HCO-analogs of Imidacloprid and Thiacloprid, I (R = CF3, CHF2) and II, resp., and the evaluation of their biol. activity have been performed. For this purpose, a first synthetic approach allowed the preparation of a desired F3CO-containing key intermediate, 3-(chloromethyl)-6-(trifluoromethoxy)pyridine. To allow facile access to the corresponding F2HCO-containing key intermediate, the difluoromethylation of hydroxylated N-based heterocycles has been developed using difluoromethyl triflate (a liquid non-ODS reagent) under air in aqueous conditions and with very short reaction time. The broad diversity of compatible heterocycles includes a large series of substituted hydroxy-pyridines, but also -pyrazoles, -pyrazine, -pyridazine, and -quinolines. The couplings of both key intermediates with the required 4,5-dihydro-N-nitro-1H-imidazol-2-amine and [N(Z)]-N-2-thiazolidinylidene-cyanamide were successfully achieved using literature conditions. This work enables the preparation of valuable building blocks, which could lead to the discovery of new bioactive entities. In the part of experimental materials, we found many familiar compounds, such as 2-Chloro-4-(difluoromethoxy)pyridine(cas: 1206978-15-5Recommanded Product: 1206978-15-5)

2-Chloro-4-(difluoromethoxy)pyridine(cas: 1206978-15-5) 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.Recommanded Product: 1206978-15-5

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

Related Products of 1179360-43-0On May 1, 2013 ,《Pyridinylpyrimidines selectively inhibit human methionine aminopeptidase-1》 appeared in Bioorganic & Medicinal Chemistry. The author of the article were Zhang, Pengtao; Yang, Xinye; Zhang, Feiran; Gabelli, Sandra B.; Wang, Renxiao; Zhang, Yihua; Bhat, Shridhar; Chen, Xiaochun; Furlani, Manuel; Amzel, L. Mario; Liu, Jun O.; Ma, Dawei. The article conveys some information:

Cellular protein synthesis is initiated with methionine in eukaryotes with few exceptions. Methionine aminopeptidases (MetAPs) which catalyze the process of N-terminal methionine excision are essential for all organisms. In mammals, type 2 MetAP (MetAP2) is known to be important for angiogenesis, while type 1 MetAP (MetAP1) has been shown to play a pivotal role in cell proliferation. Authors’ previous high-throughput screening of a com. compound library uncovered a novel class of inhibitors for both human MetAP1 (HsMetAP1) and human MetAP2 (HsMetAP2). This class of inhibitors contains a pyridinylpyrimidine core. To understand the structure-activity relationship (SAR) and to search for analogs of 2 with greater potency and higher HsMetAP1-selectivity, a total of 58 analogs were acquired through either com. source or by inhouse synthesis and their inhibitory activities against HsMetAP1 and HsMetAP2 were determined Through this systematic medicinal chem. anal., the authors have identified: (1) 5-chloro-6-methyl-2-pyridin-2-ylpyrimidine as the min. element for the inhibition of HsMetAP1; (2) 5′-chloro as the favored substituent on the pyridine ring for the enhanced potency against HsMetAP1; and (3) long C4 side chains as the essentials for higher HsMetAP1-selectivity. As a result of the SAR campaign, six compounds were found to be among the most selective and potent inhibitors of purified HsMetAP1 reported to date. In addition, crystallog. anal. of one representative inhibitor (I) in complex with N-terminally truncated HsMetAP1 was also performed. Map gene.3-Chloropicolinimidamide hydrochloride(cas: 1179360-43-0Related Products of 1179360-43-0) was used in this study.

3-Chloropicolinimidamide hydrochloride(cas: 1179360-43-0) belongs to anime. Hydrogen peroxide (H2O2) and peroxy acids generally add an oxygen atom to the nitrogen of amines. With primary amines, this step is normally followed by further oxidation, leading to nitroso compounds, RNO, or nitro compounds, RNO2. Secondary amines are converted to hydroxylamines, R2NOH, and tertiary amines to amine oxides, R3NO.Related Products of 1179360-43-0

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

《Synthesis and characterization of fluorescent Schiff bases and their metal complexes from 9-anthracenecarboxaldehy》 was written by Ibrahim, Inam Hassim; Hasan, Hasan A.. Formula: C5H7N3This research focused ontransition metal complex fluorescent Schiff base analysis. The article conveys some information:

Synthesis and characterization two Schiff bases[L1] (N2Z,N6Z)-N2,N6-bis(4-((E)-anthracen-9-ylmethyleneamino)-1,5-dimethyl-2-phenyl-1H-pyrazol-3(2H)-ylidene)pyridine-2,6-diamine Synthesis via reaction of 2,6-diaminopyridine, 4-aminoantipyrine and 9-anthracenecarboxaldehyde with mole ratio (1:2:2) resp. two steps. And [L2] (N1Z,N2Z)-N1,N2-bis(4-((E)-anthracen-9-ylmethyleneamino)-1,5-dimethyl-2-phenyl-1H-pyrazol-3(2H)-ylidene)-4-methylbenzene-1,2-diamine Synthesis from reaction of o-phenylendiamine, 4-aminoantipyrine and 9-anthracenecarboxaldehyde with mole ratio (1:2:2) resp. two steps. A new series of transition metal complexes of Mn(II), Co(II), Ca(II), Cd(II), Zn(II) and pd(II) were synthesized. The structural features were derived from their elemental analyses, IR, UV-visible spectroscopy, 1HNMR, 13CNMR spectroscopy, thermal gravimetric analyses spectral, magnetic susceptibility measurement, chloride content and conductivity measurements. The electronic spectral data and magnetic measurements indicate that the complexes exhibit octahedral geometry around Ca(II), Mn(II), Cd(II), Co(II), Zn(II) while Square planer geometry around Pd(II). In addition to this study using 2,6-Diaminopyridine, there are many other studies that have used 2,6-Diaminopyridine(cas: 141-86-6Formula: C5H7N3) was used in this study.

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.Formula: C5H7N3

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

《Studies on anticoccidial agents. 11. Synthesis and anticoccidial activity of nitropyridinecarboxamides and derivatives》 was published in Journal of Medicinal Chemistry in 1977. These research results belong to Morisawa, Yasuhiro; Kataoka, Mitsuru; Kitano, Noritoshi. Electric Literature of C6H4N2O4 The article mentions the following:

Of 56 title compounds prepared, optimal in vivo activity against Eimeria tenella was shown by 2-nitroisonicotinamide (I, R1 = R2 = H) [60780-17-8] and 11 derivatives (I: R1 = H, Me; R2 = Me, CH2OH, alkanoyl, aryl acyl, heterocyclic acyl). Activity was shown by 2-, 3-, 5-, and 6-nitro-, but not by 4-nitropyridinecarboxamides. Substitution on the amide N of the various positional isomers affected their activity differently. In the part of experimental materials, we found many familiar compounds, such as 3-Nitroisonicotinic acid(cas: 59290-82-3Electric Literature of C6H4N2O4)

3-Nitroisonicotinic acid(cas: 59290-82-3) 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.Electric Literature of C6H4N2O4

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

《Structure-Guided Discovery of Potent and Selective Inhibitors of ERK1/2 from a Modestly Active and Promiscuous Chemical Start Point》 was written by Ward, Richard A.; Bethel, Paul; Cook, Calum; Davies, Emma; Debreczeni, Judit E.; Fairley, Gary; Feron, Lyman; Flemington, Vikki; Graham, Mark A.; Greenwood, Ryan; Griffin, Nicola; Hanson, Lyndsey; Hopcroft, Philip; Howard, Tina D.; Hudson, Julian; James, Michael; Jones, Clifford D.; Jones, Christopher R.; Lamont, Scott; Lewis, Richard; Lindsay, Nicola; Roberts, Karen; Simpson, Iain; St-Gallay, Steve; Swallow, Steve; Tang, Jia; Tonge, Michael; Wang, Zhenhua; Zhai, Baochang. Related Products of 1365836-53-8 And the article was included in Journal of Medicinal Chemistry on April 27 ,2017. The article conveys some information:

There are a number of small-mol. inhibitors targeting the RAS/RAF/MEK/ERK signaling pathway that have either been approved or are in clin. development for oncol. across a range of disease indications. The inhibition of ERK1/2 is of significant current interest, as cell lines with acquired resistance to BRAF and MEK inhibitors have been shown to maintain sensitivity to ERK1/2 inhibition in preclin. models. This article reports on authors’ recent work to identify novel, potent, and selective reversible ERK1/2 inhibitors from a low-mol.-weight, modestly active, and highly promiscuous chem. start point, compound I. To guide and inform the evolution of this series, inhibitor binding mode information from X-ray crystal structures was critical in the rapid exploration of this template to compound II, which was active when tested in in vivo antitumor efficacy experiments After reading the article, we found that the author used (6-Methylpyridin-2-yl)methanamine hydrochloride(cas: 1365836-53-8Related Products of 1365836-53-8)

(6-Methylpyridin-2-yl)methanamine hydrochloride(cas: 1365836-53-8) belongs to anime. The methylamines occur in small amounts in some plants. Many polyfunctional amines (i.e., those having other functional groups in the molecule) occur as alkaloids in plants—for example, mescaline, 2-(3,4,5-trimethoxyphenyl)ethylamine; the cyclic amines nicotine, atropine, morphine, and cocaine; and the quaternary salt choline, N-(2-hydroxyethyl)trimethylammonium chloride, which is present in nerve synapses and in plant and animal cells.Related Products of 1365836-53-8

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

《Near-Infrared Fluorescent Theranostic Cisplatin Prodrug with Transcatheter Intra-Arterial Therapy: Application to Rabbit Hepatocellular Carcinoma》 was written by Li, Qiang; Wang, Qi; Wang, Saibo; Zhu, Shiqin; Yuan, Tianwen; Guo, Zhiqian; Cao, Jun; Tian, He; Zhu, Wei-Hong. HPLC of Formula: 103-74-2This research focused ontranscatheter intra arterial therapy cisplatin prodrug hepatocellular carcinoma. The article conveys some information:

Transcatheter intra-arterial therapy (TIT) has become valuable in the battle against primary and secondary hepatic malignancies. However, the lack of a mechanism to visualize real-time drug release and avoid fast metabolic clearance of chemotherapeutic agents is the primary barrier to TIT for hepatocellular carcinoma. Here, a specific near-IR (NIR) fluorescent prodrug platform, i.e., DSPE-mPEG/DCM-S-Pt micelles (DCM-S-Pt@PEG), to assist TIT in direct administration to large mammals like rabbits, is presented. DCM-S-Pt@PEG consists of a NIR fluorophore for tracing drug release, a nonspecific antitumor drug cisplatin for hepatocellular carcinoma treatment, a glutathione-activatable disulfide linker, and a DSPE-mPEG nano-micelle carrier for controllable drug release. DCM-S-Pt@PEGcan make the drug accumulation in tumor tissues enhance the therapeutic effect by: (i) specific delivery of prodrug to hepatic tumor tissues through the femoral artery by TIT, (ii) sustained drug-release from the biodegradable lipid DSPE-mPEG micelle to minimize metabolic clearance, and (iii) cancer biomarker-activated drug release. It provides a promising strategy to assist TIT in treating unresectable devastating hepatocellular carcinoma administration in the rabbit model, rather than common mouse model. In the experiment, the researchers used 2-(2-Hydroxyethyl)pyridine(cas: 103-74-2HPLC of Formula: 103-74-2)

2-(2-Hydroxyethyl)pyridine(cas: 103-74-2) 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.HPLC of Formula: 103-74-2

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem