Month: April 2022

Synthetic Route of C5H5FN2. The reaction of aromatic heterocyclic molecules with protons is called protonation. Aromatic heterocycles are more basic than benzene due to the participation of heteroatoms. Compound: 5-Amino-2-fluoropyridine, is researched, Molecular C5H5FN2, CAS is 1827-27-6, about 2-Aminoadipic Acid-C(O)-Glutamate Based Prostate-Specific Membrane Antigen Ligands for Potential Use as Theranostics. Author is Nakajima, Ryo; Novakova, Zora; Tueckmantel, Werner; Motlova, Lucia; Barinka, Cyril; Kozikowski, Alan P..

The design and synthesis of prostate specific membrane antigen (PSMA) ligands derived from 2-aminoadipic acid, a building block that has not previously been used to construct PSMA ligands, are reported. The effects of both the linker length and of an N-substituent of our PSMA ligands were probed, and X-ray structures of five of these ligands bound to PSMA were obtained. Among the ligands disclosed herein, I showed the highest inhibitory activity for PSMA. As ligand I can readily be radiolabeled since its fluorine atom is adjacent to the nitrogen atom of its pyridine ring, the use of this and related compounds as theranostics can be pursued.

After consulting a lot of data, we found that this compound(1827-27-6)Synthetic Route of C5H5FN2 can be used in many types of reactions. And in most cases, this compound has more advantages.

Reference:
Pyrazine – Wikipedia,
Pyrazine | C4H4N2 – PubChem

The chemical properties of alicyclic heterocycles are similar to those of the corresponding chain compounds. Compound: 4-Aminopyrimidine, is researched, Molecular C4H5N3, CAS is 591-54-8, about Synthesis of novel structural hybrids between aza-heterocycles and azelaic acid moiety with a specific activity on osteosarcoma cells, the main research direction is azelaic acid oxononanoate anticancer agent HDAC mol docking osteosarcoma; 9-hydroxystearic acid; azelaic acid; cancer; molecular docking; osteosarcoma; pyridine; pyrimidine.COA of Formula: C4H5N3.

Nine compounds bearing pyridinyl (or piperidinyl, benzimidazolyl, benzotriazolyl) groups bound to an azelayl moiety through an amide bond were synthesized. The structural analogy with some histone deacetylase inhibitors inspired their syntheses, seeking new selective histone deacetylase inhibitors (HDACi). The azelayl moiety recalls part of 9-hydroxystearic acid, a cellular lipid showing antiproliferative activity toward cancer cells with HDAC as a mol. target. Azelayl derivatives bound to a benzothiazolyl moiety further proved to be active as HDACi. The novel compounds were tested on a panel of both normal and tumor cell lines. Non-specific induction of cytotoxicity was observed in the normal cell line, while three of them induced a biol. effect only on the osteosarcoma (U2OS) cell line. One of them induced a change in nuclear shape and size. Cell-cycle alterations are associated with post-transcriptional modification of both H2/H3 and H4 histones. In line with recent studies, revealing unexpected HDAC7 function in osteoclasts, mol. docking studies on the active mols. predicted their proneness to interact with HDAC7. By reducing side effects associated with the action of the first-generation inhibitors, the herein reported compounds, thus, sound promising as selective HDACi.

After consulting a lot of data, we found that this compound(591-54-8)COA of Formula: C4H5N3 can be used in many types of reactions. And in most cases, this compound has more advantages.

Reference:
Pyrazine – Wikipedia,
Pyrazine | C4H4N2 – PubChem

Kimura, Hiroyuki; Okuda, Haruka; Ishiguro, Masumi; Arimitsu, Kenji; Makino, Akira; Nishii, Ryuichi; Miyazaki, Anna; Yagi, Yusuke; Watanabe, Hiroyuki; Kawasaki, Ikuo; Ono, Masahiro; Saji, Hideo published an article about the compound: 5-Amino-2-fluoropyridine( cas:1827-27-6,SMILESS:NC1=CN=C(C=C1)F ).Safety of 5-Amino-2-fluoropyridine. Aromatic heterocyclic compounds can be classified according to the number of heteroatoms or the size of the ring. The authors also want to convey more information about this compound (cas:1827-27-6) through the article.

In non-small-cell lung carcinoma patients, L858R mutation of epidermal growth factor receptor (EGFR) are often found and mol. target therapy using EGFR tyrosine kinase inhibitors is effective for the patients. However, the treatment frequently develops drug resistance by secondary mutation, of which approx. 50% is a T790M mutation. Thus, the ability to predict whether EGFR will undergo secondary mutation is extremely important. We synthesized a novel radiofluorinated 4-(anilino)pyrido[3,4-d]pyrimidine derivative ([18F]APP-1) and evaluated its potential as a positron emission tomog. (PET) imaging probe to discriminate different tumor of mutation. EGFR inhibition assay, cell-uptake and biodistribution study showed that [18F]APP-1 binds specifically to the L858R mutant EGFR but not to the L858R/T790M mutant. Finally, PET imaging study using [18F]APP-1 with tumor-bearing mice, the H3255 tumor (L858R mutant) was more clearly visualized than the H1975 tumor (L858R/T790M mutant).

After consulting a lot of data, we found that this compound(1827-27-6)Safety of 5-Amino-2-fluoropyridine can be used in many types of reactions. And in most cases, this compound has more advantages.

Reference:
Pyrazine – Wikipedia,
Pyrazine | C4H4N2 – PubChem

Epoxy compounds usually have stronger nucleophilic ability, because the alkyl group on the oxygen atom makes the bond angle smaller, which makes the lone pair of electrons react more dissimilarly with the electron-deficient system. Compound: 2-Amino-4,5-dihydrothiazole-4-carboxylic acid, is researched, Molecular C4H6N2O2S, CAS is 2150-55-2, about Metabolic control analysis of L-cysteine producing strain TS1138 of Pseudomonas sp.Recommanded Product: 2150-55-2.

A kinetic model describing the biosynthesis of L-cysteine by Pseudomonas sp. TS1138 has been developed. The two enzymes catalyzing this pathway, L-cysteine synthetase (CS) and L-cysteine desulfhydrase (CD), follow Michaelis-Menten kinetics with noncompetitive inhibition of CS by L-cysteine. From measurements of intermediates and end products that were made during L-cysteine enzymic synthesis, metabolic control anal. of the pathway was carried out using the kinetic model. The elasticity coefficients and the flux control coefficients were calculated, and the anal. revealed a shift in the flux control from CS to CD during the reaction. The findings further implicate potential targets and strategies for increasing L-cysteine production; for example, the strain TS1138 could be manipulated by site-directed mutagenesis to reduce CD activity.

After consulting a lot of data, we found that this compound(2150-55-2)Recommanded Product: 2150-55-2 can be used in many types of reactions. And in most cases, this compound has more advantages.

Reference:
Pyrazine – Wikipedia,
Pyrazine | C4H4N2 – PubChem

Application In Synthesis of 5-Amino-2-fluoropyridine. The mechanism of aromatic electrophilic substitution of aromatic heterocycles is consistent with that of benzene. Compound: 5-Amino-2-fluoropyridine, is researched, Molecular C5H5FN2, CAS is 1827-27-6, about Divergent Aminocarbonylations of Alkynes Enabled by Photoredox/Nickel Dual Catalysis. Author is Zhao, Xian; Feng, Xiaoliang; Chen, Fan; Zhu, Shengqing; Qing, Feng-Ling; Chu, Lingling.

A metallaphotoredox-catalyzed strategy for the selective and divergent aminocarbonylation of alkynes with amines and 1 atm of CO was reported. This synergistic protocol not only enables the Markovnikov-selective hydroaminocarbonylation of alkynes to afford α,β-unsaturated amides, but also facilitated a sequential four-component hydroaminocarbonylation/radical alkylation in the presence of tertiary and secondary alkyl boronate esters, which allowed for straightforward conversion of alkynes into corresponding amides. Preliminary mechanistic studied disclose that a photoinduced oxidative insertion of aniline and CO into nickel followed by a migratory insertion of (carbamoyl)nickel species was involved.

After consulting a lot of data, we found that this compound(1827-27-6)Application In Synthesis of 5-Amino-2-fluoropyridine can be used in many types of reactions. And in most cases, this compound has more advantages.

Reference:
Pyrazine – Wikipedia,
Pyrazine | C4H4N2 – PubChem

In general, if the atoms that make up the ring contain heteroatoms, such rings become heterocycles, and organic compounds containing heterocycles are called heterocyclic compounds. An article called A Bulky and Electron-Rich N-Heterocyclic Carbene Palladium Complex (SIPr)Ph2Pd(cin)Cl: Highly Efficient and Versatile for Buchwald-Hartwig Amination of (Hetero)aryl Chlorides with (Hetero)aryl Amines at Room Temperature, published in 2021-08-06, which mentions a compound: 1827-27-6, Name is 5-Amino-2-fluoropyridine, Molecular C5H5FN2, Computed Properties of C5H5FN2.

A bulky and electron-rich N-heterocyclic carbene palladium complex (SIPr)Ph2Pd(cin)Cl was synthesized and characterized. It was found to be highly efficient and versatile for the synthesis of substituted amines via coupling of different (hetero)aryl chlorides with various (hetero)aryl amines at room temperature, especially for the challenging amination of five- or six-membered ring heteroaryl chlorides with five- or six-membered ring heteroaryl amines. It was also successfully applied to the synthesis of various com. pharmaceuticals and candidate drugs or compounds with potential pharmacol. activities in high yields. All of these demonstrate its excellent catalytic efficacy in Buchwald-Hartwig amination and broad application prospects in relevant pharmaceutical preparations DFT calculations suggest that the steric-induced electronic interaction makes the ligand more electron-donating and the steric effect effectively regulates the rotation of iPr-Ph-iPr group in the catalyzed system due to the introduction of the di-Ph skeleton. Considering the electronic effect and steric effect together, the oxidative addition activation barriers by (SIPr)Ph2 and (SIPr) ligands are close to each other. The reductive elimination was the rate-determining step of (SIPr)Ph2Pd(cin)Cl-catalyzed system in the catalytic cycle, the appropriate steric hindrance of (SIPr)Ph2 ligand greatly reduces the energy barrier of this step. The perfect combination of electron-donating and steric hindrance ability of the ligand significantly improves the catalytic activity.

After consulting a lot of data, we found that this compound(1827-27-6)Computed Properties of C5H5FN2 can be used in many types of reactions. And in most cases, this compound has more advantages.

Reference:
Pyrazine – Wikipedia,
Pyrazine | C4H4N2 – PubChem

Related Products of 1827-27-6. So far, in addition to halogen atoms, other non-metallic atoms can become part of the aromatic heterocycle, and the target ring system is still aromatic. Compound: 5-Amino-2-fluoropyridine, is researched, Molecular C5H5FN2, CAS is 1827-27-6, about Utility of MetaSite in improving metabolic stability of the neutral indomethacin amide derivative and selective cyclooxygenase-2 inhibitor 2-(1-(4-chlorobenzoyl)-5-methoxy-2-methyl-1H-indol-3-yl)-N-phenethyl-acetamide.

Prediction of the metabolic sites for new compounds, synthesized or virtual, is important in the rational design of compounds with increased resistance to metabolism The aim of the present investigation was to use rational design together with MetaSite, an in silico tool for predicting metabolic soft spots, to synthesize compounds that retain their pharmacol. effects but are metabolically more stable in the presence of cytochrome P 450 enzymes. The model compound for these studies was the phenethyl amide (1) derivative of the nonsteroidal anti-inflammatory drug (NSAID) indomethacin. Unlike the parent NSAID, 1 is a potent and selective cyclooxygenase-2 (COX-2) inhibitor and nonulcerogenic anti-inflammatory agent in the rat. This pharmacol. benefit is offset by the finding that 1 is very unstable in rat and human microsomes because of extensive P 4503 A4/2D6-mediated metabolism on the phenethyl group, exptl. observations that were accurately predicted by MetaSite. The information was used to design analogs with polar (glycinyl) and/or electron-deficient (fluorophenyl, fluoropyridinyl) amide substituents to reduce metabolism in 1. MetaSite correctly predicted the metabolic shift from oxidation on the amide substituent to O-demethylation for these compounds, whereas rat and human microsomal stability studies and pharmacokinetic assessments in the rat confirmed that the design tactics for improving pharmacokinetic attributes of 1 had worked in our favor. In addition, the fluorophenyl and pyridinyl amide derivatives retained the potent and selective COX-2 inhibition demonstrated with 1. Overall, the predictions from MetaSite gave useful information leading to the design of new compounds with improved metabolic properties.

After consulting a lot of data, we found that this compound(1827-27-6)Related Products of 1827-27-6 can be used in many types of reactions. And in most cases, this compound has more advantages.

Reference:
Pyrazine – Wikipedia,
Pyrazine | C4H4N2 – PubChem

Name: Ethyl oxazole-5-carboxylate. The reaction of aromatic heterocyclic molecules with protons is called protonation. Aromatic heterocycles are more basic than benzene due to the participation of heteroatoms. Compound: Ethyl oxazole-5-carboxylate, is researched, Molecular C6H7NO3, CAS is 118994-89-1, about Copper-catalyzed diarylation of Se with aryl iodides and heterocycles. Author is Hu, Dehua; Liu, Miaochang; Wu, Huayue; Gao, Wenxia; Wu, Ge.

The regioselective copper-catalyzed three-component coupling reaction of electron-deficient heterocycles, like aryl-oxadiazoles/aryloxazoles/dimethyl-purine-diones, etc. with aryl iodides in presence of Se powder so as to yield corresponding diaryl-selenated heterocycles such as arylselanyl-aryl-oxadiazoles I [R = Ph, 4-MeC6H4, 2-thienyl, etc.; R1 = Ph, 2-naphthyl, 3-thienyl, etc.] and arylselanyl-aryl-oxazoles II [R2 = Ph, 2,4,6-triMeC6H2; R3 = CO2Et, Ph, 4-MeSC6H4, etc.] was disclosed. The established methodol. provided an efficient and practical pathway to access arylselenated heterocycles via copper-catalyzed double C-Se bond formation. This transformation featured the use of elemental Se as the selenating reagent, a cost-effective catalytic system and the late-stage selenation of bioactive compounds

After consulting a lot of data, we found that this compound(118994-89-1)Name: Ethyl oxazole-5-carboxylate can be used in many types of reactions. And in most cases, this compound has more advantages.

Reference:
Pyrazine – Wikipedia,
Pyrazine | C4H4N2 – PubChem

The chemical properties of alicyclic heterocycles are similar to those of the corresponding chain compounds. Compound: 4-Aminopyrimidine, is researched, Molecular C4H5N3, CAS is 591-54-8, about Generation and on-demand initiation of acute ictal activity in rodent and human tissue, the main research direction is seizure cortex optogenetics neurotransmitters.SDS of cas: 591-54-8.

Controlling seizures remains a challenging issue for the medical community. To make progress, researchers need a way to extensively study seizure dynamics and investigate its underlying mechanisms. Acute seizure models are convenient, offer the ability to perform electrophysiol. recordings, and can generate a large volume of electrog. seizure-like (ictal) events. The promising findings from acute seizure models can then be advanced to chronic epilepsy models and clin. trials. Thus, studying seizures in acute models that faithfully replicate the electrog. and dynamical signatures of a clin. seizure will be essential for making clin. relevant findings. Studying ictal events in acute seizure models prepared from human tissue is also important for making findings that are clin. relevant. The key focus in this paper is on the cortical 4-AP model due to its versatility in generating ictal events in both in vivo and in vitro studies, as well as in both mouse and human tissue. The methods in this paper will also describe an alternative method of seizure induction using the Zero-Mg2+ model and provide a detailed overview of the advantages and limitations of the epileptiform-like activity generated in the different acute seizure models. Moreover, by taking advantage of com. available optogenetic mouse strains, a brief (30 ms) light pulse can be used to trigger an ictal event identical to those occurring spontaneously. Similarly, 30 – 100 ms puffs of neurotransmitters (Gamma-Amino Butyric Acid or glutamate) can be applied to the human tissue to trigger ictal events that are identical to those occurring spontaneously. The ability to trigger ictal events on-demand in acute seizure models offers the newfound ability to observe the exact sequence of events that underlie seizure initiation dynamics and efficiently evaluate potential anti-seizure therapies.

After consulting a lot of data, we found that this compound(591-54-8)SDS of cas: 591-54-8 can be used in many types of reactions. And in most cases, this compound has more advantages.

Reference:
Pyrazine – Wikipedia,
Pyrazine | C4H4N2 – PubChem

In general, if the atoms that make up the ring contain heteroatoms, such rings become heterocycles, and organic compounds containing heterocycles are called heterocyclic compounds. An article called Palladium-catalyzed direct C2-arylation of azoles with aromatic triazenes, published in 2019, which mentions a compound: 118994-89-1, Name is Ethyl oxazole-5-carboxylate, Molecular C6H7NO3, Application of 118994-89-1.

A highly efficient palladium-catalyzed arylation of azoles at the C2-position using 1-aryltriazenes as aryl reagents was developed for the synthesis of aryl azoles, e.g., I. Azoles including oxazoles, thiazoles, imidazoles, 1,3,4-oxadiazoles and oxazolines reacted with 1-aryltriazenes smoothly to generate the corresponding products in good to excellent yields and various substitution patterns were tolerated toward the reaction.

After consulting a lot of data, we found that this compound(118994-89-1)Application of 118994-89-1 can be used in many types of reactions. And in most cases, this compound has more advantages.

Reference:
Pyrazine – Wikipedia,
Pyrazine | C4H4N2 – PubChem