Category: Pyrazines

Edney, Dean; Hulcoop, David G.; Leahy, John H.; Vernon, Lois E.; Wipperman, Mark D.; Bream, Robert N.; Webb, Michael R. published an article about the compound: Ethyl oxazole-5-carboxylate( cas:118994-89-1,SMILESS:O=C(C1=CN=CO1)OCC ).Quality Control of Ethyl oxazole-5-carboxylate. 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:118994-89-1) through the article.

This paper describes the discovery and development of a flexible route to two candidate drug mols. by a common intermediate approach. Key reactions include Negishi and Suzuki couplings to form biaryl bonds. Conditions for a Miyaura borylation of heteroaryl bromides were also developed. Heteroaryl trifluoroborates and aryl chlorides were used as coupling partners in the Suzuki reaction, thereby minimizing detrimental side reactions such as protodeboronation and oxidative homocoupling. A complementary set of reaction conditions using pinacolboronates with potassium bifluoride as an additive were also developed and used to make 5 kg of drug substance for use in early-phase clin. trials.

When you point to this article, it is believed that you are also very interested in this compound(118994-89-1)Quality Control of Ethyl oxazole-5-carboxylate and due to space limitations, I can only present the most important information.

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 Recent developments of RET protein kinase inhibitors with diverse scaffolds as hinge binders, the main research direction is review RET protein kinase inhibitor nicotinonitrile imidazopyridazine pyridone; RET; RET inhibitors; RET mutation; RET-driven cancers; hinge binder; precision targeted therapy.Computed Properties of C4H5N3.

A review. RET is a proto-oncogene encoding a receptor tyrosine kinase. RET regulates key aspects of cellular proliferation, differentiation and survival. The activation of RET via gene fusions or point mutations is closely related to lung, thyroid and other cancers. This review summarizes the developments of a diversity of small mol. RET protein kinase inhibitors in the past 10 years. These RET inhibitors are classified according to their hinge binder chemotypes as: pyrimidines, including the pyrazolopyrimidines, pyrimidine oxazines, quinazolines, 4-aminopyrimidines and 4-aminopyridines; indolinones; 5-aminopyrazole-4-carboxamides; 3-trifluoromethylanilines; imidazopyridines, imidazopyridazines and pyrazopyridines; nicotinonitriles; pyridones and 1,2,4-triazoles. In each section, the biol. activities of the inhibitors, their structure-activity relationships and possible binding modes with the RET kinase are introduced.

When you point to this article, it is believed that you are also very interested in this compound(591-54-8)Computed Properties of C4H5N3 and due to space limitations, I can only present the most important information.

Reference:
Pyrazine – Wikipedia,
Pyrazine | C4H4N2 – PubChem

In organic chemistry, atoms other than carbon and hydrogen are generally referred to as heteroatoms. The most common heteroatoms are nitrogen, oxygen and sulfur. Now I present to you an article called Synthesis and hypoxia-selective cytotoxicity of a 2-nitroimidazole mustard, published in 1998-07-07, which mentions a compound: 121816-79-3, mainly applied to chloroethylaminonitroimidazole preparation hypoxia selective cytotoxicity; nitroimidazole mustard preparation hypoxia selective cytotoxicity; imidazole chloroethylaminonitro preparation hypoxia selective cytotoxicity, Product Details of 121816-79-3.

A four-step synthesis of 5-[N,N-bis(2-chloroethyl)amino]-1-methyl-2-nitroimidazole from 1-methyl-2-nitroimidazole is described. This compound showed similar hypoxia-selective cytotoxicity to the dinitrobenzamide mustard SN 23862 in UV4 cells (ca. 40-fold), and superior selectivity (>7-fold) in repair-competent AA8 cells.

In some applications, this compound(121816-79-3)Product Details of 121816-79-3 is unique.If you want to know more details about this compound, you can contact with the author or consult more relevant literature.

Reference:
Pyrazine – Wikipedia,
Pyrazine | C4H4N2 – PubChem

The reaction of an aromatic heterocycle with a proton is called a protonation. One of articles about this theory is 《Formation of 2-iminothiazolidine-4-carboxylic acid in the cyanobromination of lanthionine》. Authors are van Rensburg, N. J. J..The article about the compound:2-Amino-4,5-dihydrothiazole-4-carboxylic acidcas:2150-55-2,SMILESS:O=C(C1N=C(N)SC1)O).Related Products of 2150-55-2. Through the article, more information about this compound (cas:2150-55-2) is conveyed.

A 5 ml. solution of lanthionine in 0.1N HCl was added to 5 ml. 5% aqueous NaCN and the mixture treated with 1 ml. NCBr solution (prepared by adding 5% aqueous NaCN to a saturated solution of Br till the solution was just colorless). After 3 consecutive boilings for 30 secs. and cooling for 3 min., the thiol content estimation was interfered with by incomplete removal of NCBr. The reaction mixture was, therefore, boiled for 10 min., but the quantity of thiol formed was not consistent and reproducibility of the results was very poor. Paper chromatography of the products in sec-BuOH-HCOOH-H2O (75:15:10) system showed the presence of 2-iminothiazolidine-4-carboxylic acid (I). In these experiments, HCl was converted to HCN, which was expelled on boiling and probably the high pH led to the formation of the acid.

In some applications, this compound(2150-55-2)Related Products of 2150-55-2 is unique.If you want to know more details about this compound, you can contact with the author or consult more relevant literature.

Reference:
Pyrazine – Wikipedia,
Pyrazine | C4H4N2 – PubChem

Recommanded Product: 5-Amino-2-fluoropyridine. The protonation of heteroatoms in aromatic heterocycles can be divided into two categories: lone pairs of electrons are in the aromatic ring conjugated system; and lone pairs of electrons do not participate. Compound: 5-Amino-2-fluoropyridine, is researched, Molecular C5H5FN2, CAS is 1827-27-6, about 18F-Labeled Pyrido[3,4-d]pyrimidine as an Effective Probe for Imaging of L858R Mutant Epidermal Growth Factor Receptor. Author is Kimura, Hiroyuki; Okuda, Haruka; Ishiguro, Masumi; Arimitsu, Kenji; Makino, Akira; Nishii, Ryuichi; Miyazaki, Anna; Yagi, Yusuke; Watanabe, Hiroyuki; Kawasaki, Ikuo; Ono, Masahiro; Saji, Hideo.

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).

In some applications, this compound(1827-27-6)Recommanded Product: 5-Amino-2-fluoropyridine is unique.If you want to know more details about this compound, you can contact with the author or consult more relevant literature.

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: 5-Amino-2-fluoropyridine, is researched, Molecular C5H5FN2, CAS is 1827-27-6, about Asymmetric synthesis of heterocyclic chloroamines and aziridines by enantioselective protonation of catalytically generated enamines.Reference of 5-Amino-2-fluoropyridine.

We report a method for the synthesis of chiral vicinal chloroamines via asym. protonation of catalytically generated prochiral chloroenamines using chiral Bronsted acids. The process is highly enantioselective, with the origin of asymmetry and catalyst substituent effects elucidated by DFT calculations We show the utility of the method as an approach to the synthesis of a broad range of heterocycle-substituted aziridines by treatment of the chloroamines with base in a one-pot process, as well as the utility of the process to allow access to vicinal diamines.

In some applications, this compound(1827-27-6)Reference of 5-Amino-2-fluoropyridine is unique.If you want to know more details about this compound, you can contact with the author or consult more relevant literature.

Reference:
Pyrazine – Wikipedia,
Pyrazine | C4H4N2 – PubChem

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.Bream, Robert N.; Clark, Hugh; Edney, Dean; Harsanyi, Antal; Hayler, John; Ironmonger, Alan; Mc Cleary, Nadine; Phillips, Natalie; Priestley, Catherine; Roberts, Alastair; Rushworth, Philip; Szeto, Peter; Webb, Michael R.; Wheelhouse, Katherine researched the compound: Ethyl oxazole-5-carboxylate( cas:118994-89-1 ).COA of Formula: C6H7NO3.They published the article 《The Application of C-H Functionalization in the Development of a Concise and Convergent Route to the Phosphatidylinositol-3-kinase Delta Inhibitor Nemiralisib.》 about this compound( cas:118994-89-1 ) in Organic Process Research & Development. Keywords: Nemiralisib improved preparation. We’ll tell you more about this compound (cas:118994-89-1).

The development of an improved and scalable method for the manufacture of Nemiralisib, a phosphatidylinositol-3-kinase delta inhibitor was studied. Incorporation of three consecutive catalytic reactions, including a palladium-catalyzed C-H functionalization and an iridium-catalyzed borylation, significantly simplified and shortened the synthetic sequence. The revised route was successfully implemented in pilot plant on multikilogram scale to deliver >100 kg of product.

In some applications, this compound(118994-89-1)COA of Formula: C6H7NO3 is unique.If you want to know more details about this compound, you can contact with the author or consult more relevant literature.

Reference:
Pyrazine – Wikipedia,
Pyrazine | C4H4N2 – PubChem

In organic chemistry, atoms other than carbon and hydrogen are generally referred to as heteroatoms. The most common heteroatoms are nitrogen, oxygen and sulfur. Now I present to you an article called Determination of 2-iminothiazolidine-4-carboxylic acid, published in 1965, which mentions a compound: 2150-55-2, mainly applied to , Electric Literature of C4H6N2O2S.

Procedures are described for determination of 2-iminothiazolidine-4-carboxylic acid, using diazotized sulfanilic acid or the mercury-diphenylthiocarbazone reaction. The compound should first be separated from interfering substances such as are found in urine. Paper electrophoresis, ion displacement, or chromatography suffice for this purpose.

In some applications, this compound(2150-55-2)Electric Literature of C4H6N2O2S is unique.If you want to know more details about this compound, you can contact with the author or consult more relevant literature.

Reference:
Pyrazine – Wikipedia,
Pyrazine | C4H4N2 – PubChem

Application In Synthesis of 5-Amino-2-fluoropyridine. Aromatic heterocyclic compounds can also be classified according to the number of heteroatoms contained in the heterocycle: single heteroatom, two heteroatoms, three heteroatoms and four heteroatoms. Compound: 5-Amino-2-fluoropyridine, is researched, Molecular C5H5FN2, CAS is 1827-27-6, about HDAC4 Inhibitors with Cyclic Linker and Non-hydroxamate Zinc Binding Group: Design, Synthesis, HDAC Screening and in vitro Cytotoxicity evaluation.. Author is Tilekar, Kalpana; Hess, Jessica D.; Upadhyay, Neha; Schweipert, Markus; Flath, Felix; Gutierrez, Denisse A.; Loiodice, Fulvio; Lavecchia, Antonio; Meyer-Almes, Franz-Josef; Aguilera, Renato J.; Ramaa, C. S..

Recent evidences highlight the usefulness of small mol. (Histone deacetylase 4) HDAC4 inhibitors in the several preclin. paradigms. Major toxicity and mutagenicity issues associated with hydroxamate HDAC inhibitors, stimulated us to develop potent non-hydroxamate inhibitors. In the present work a novel series of thiazolidinedione (TZD) derivatives with pyridine as cyclic linker and TZD ring as zinc binding group was designed and screened in a panel of isoenzymes of HDACs, wherein the most potent compounds exhibiting HDAC4 IC50-values<5 μM were 5 v, 5 w, 5 y and 5 z (IC50=4.2±1 μM, 0.75±0.03 μM, 4.9±0.5 and 2.3±0.5 μM, resp.). The docking studies displayed the unique binding mode of this series of compound at active site of HDAC4, wherein TZD ring was indicated as zinc binding group. Further, 5 w and 5 y were found as the most potent antiproliferative agent in lymphoblastic leukemia (CCRF-CEM) and breast cancer MDA-MB-231 cells. Compound 5 y was found to induce the apoptosis and DNA fragmentation of CEM cells. The western blotting anal. of 5 y also showed the presence of cleaved caspases supporting their apoptotic nature. Further, Class IIa (HDAC4) selectivity of 5 y was also supported by western blotting observations, wherein 5 y caused the accumulation of acetylated H3 but not of acetylated Tubulin. Thus, our findings endorse the further investigation of this series of compounds for their potential as targeted cancer therapeutic agents. As far as I know, this compound(1827-27-6)Application In Synthesis of 5-Amino-2-fluoropyridine can be applied in many ways, which is helpful for the development of experiments. Therefore many people are doing relevant researches.

Reference:
Pyrazine – Wikipedia,
Pyrazine | C4H4N2 – PubChem

Name: 2-Amino-4,5-dihydrothiazole-4-carboxylic acid. 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: 2-Amino-4,5-dihydrothiazole-4-carboxylic acid, is researched, Molecular C4H6N2O2S, CAS is 2150-55-2, about 2-Iminothiazolidine-4-carboxylic acid produces hippocampal CA1 lesions independent of seizure excitation and glutamate receptor activation.

In this study, the ability of either 2-iminothiazolidine-4-carboxylic acid (2-ICA), glutamate, proline or NMDA (N-methyl-D-aspartate) injected i.c.v. to produce hippocampal lesions sensitive to glutamate antagonists was compared in mice. Hippocampal CA1 damage was observed 5-days following either a seizure (3.2 μmol) or subseizure (1.0 μmol) dose of 2-ICA. Glutamate (3.2 μmol) or proline (10 μmol) also produced hippocampal damage; glutamate damage was primarily to the CA1 subfield, whereas proline damaged neurons throughout the entire hippocampal formation. NMDA (3.2 nmol) caused seizure activity in all animals with a 50% lethality. No hippocampal damage was observed in surviving mice. Neither MK-801 (dizocilpine maleate) nor CNQX (6-cyano-7-nitroquinoxaline-2,3-dione) pretreatment prevented hippocampal lesions produced by 2-ICA. In contrast, MK-801 significantly reduced the frequency of mice displaying glutamate hippocampal lesions, but failed to block seizures produced by glutamate. MK-801 also protected neurons in the CA2-3 zone and the dentate gyrus, but not in the CA1 region of proline-injected mice. Finally, pretreatment with the mixed metabotropic glutamate receptor (mGluR)1/mGluR2 antagonist-agonist (S)-4-carboxy-3-hydroxyphenylglycine (CHPG) prevented hippocampal damage produced by the mGluR 1 agonist (RS)-3,5-dihydroxyphenylglycine (DHPG), but did not protect against 2-ICA hippocampal lesions. These results show that 2-ICA hippocampal CA1 damage is not mediated through ionotropic or metabotropic glutamate receptors. 2-ICA hippocampal damage may represent a neurotoxicity that is distinct from excitotoxic-mediated cell death.

As far as I know, this compound(2150-55-2)Name: 2-Amino-4,5-dihydrothiazole-4-carboxylic acid can be applied in many ways, which is helpful for the development of experiments. Therefore many people are doing relevant researches.

Reference:
Pyrazine – Wikipedia,
Pyrazine | C4H4N2 – PubChem