Category: 123148-78-7

Reference of 123148-78-7 ,Some common heterocyclic compound, 123148-78-7, molecular formula is C6H3ClIN3, its traditional synthetic route has been very mature, but the traditional synthetic route has various shortcomings, such as complicated route, low yield, poor purity, etc., below Introduce a new synthetic route.

Example 49; 4-Chloro-5-iodo-7-(2-trimethylsilanyl-ethoxymethyl)-7H-pyrrolo[2,3-d]pyrimidine (49.1); To a suspension of sodium hydride (60% in mineral oil, 78.8 g, 1.97 mmol) in dry THF (15 ml_), is added a solution of intermediate 38.2 (0.50 g, 1.79 mmol) in THF (5 ml.) dropwise and the resulting mixture is stirred for 15 min. It is then cooled to O0C and SEM chloride (0.33 ml_, 1.881 mmol) is added and the reaction mixture is stirred overnight. The reaction is quenched by carefully adding aqueous NH4CI and then extracted with EtOAc. The combined organic layer is successively washed with water, brine, dried over anhydrous Na2SO4 and concentrated in vacuo. Purification of the crude residue by column chromatography (silica 100-200 mesh, hexane : ethyl acetate = 92 : 8) gives intermediate 49.1 as a white solid, m p 108-1100C. 1H NMR (400 MHz, DMSOd6): delta 8.64 (s, 1 H), 7.53 (s, 1 H), 5.61 (s, 1 H), 3.53 (d, J = 8.29 Hz, 1 H); 0.92 (d, J = 8.29 Hz, 1 H); -0.03 (s, 9H). ESI-MS: calcd. for Ci2H17CIIN3OSi (409.73); found: 410 [M+H+].

These compound has a wide range of applications. It is believed that with the continuous development of the source of the synthetic route,123148-78-7, its application will become more common.

Reference:
Patent; NOVARTIS AG; CHEN, Yen-Liang; DURAISWAMY, Jeyaraj; KONDREDDI, Ravinder Reddy; YIN, Zheng; WO2010/15637; (2010); A1;,
Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia

Each compound has different characteristics, and only by selecting the characteristics of the compound suitable for a specific situation can the compound be applied on a large scale. 123148-78-7, name is 4-Chloro-5-iodo-7H-pyrrolo[2,3-d]pyrimidine. This compound has unique chemical properties. The synthetic route is as follows. Recommanded Product: 123148-78-7

DMF (66mL) was added to a mixture of compound 12 1 (2.00g, 7.15mmol) and 59 sodium hydride (243mg, 10.1mmol) under nitrogen atmosphere. The reaction mixture was cooled to 0C and stirred for 30min. 60 2-(Trimethylsilyl)-ethoxymethyl chloride (1.70mL, 9.58mmol) was added dropwise over 45min and stirred at 22C for 1.5h. 61 Water (150mL) and 62 EtOAc (150mL) was added to the reaction mixture, the phases were separated, and the water phase was extracted with more EtOAc (2¡Á150mL). The combined organic phases were dried over Na2SO4, filtered, and concentrated in vacuo. The product was purified by silica-gel column chromatography (n-pentane/EtOAc, 1/1, Rf=0.78) to give 2.74g (10.0mmol, 86%) of a pale yellow 63 powder; mp. 98-104C; 1H NMR (400MHz, DMSO-d6): 8.69 (s, 1H), 8.13 (s, 1H), 5.60 (s, 2H), 3.51 (t, J=8.1, 2H), 0.82 (t, J=8.1, 2H),-0.10 (s, 9H). The spectroscopic data corresponded with that reported previously [40].

If you are interested in these compounds, you can also browse my other articles.Thank you for taking the time to read this article. I hope you enjoyed it, 123148-78-7, 4-Chloro-5-iodo-7H-pyrrolo[2,3-d]pyrimidine.

Reference:
Article; Reiers¡ãlmoen, Ann Christin; Han, Jin; Sundby, Eirik; Hoff, Bard Helge; European Journal of Medicinal Chemistry; vol. 155; (2018); p. 562 – 578;,
Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia

The reaction rate of a catalyzed reaction is faster than the reaction rate of the uncatalyzed reaction at the same temperature. 123148-78-7, Name is 4-Chloro-5-iodo-7H-pyrrolo[2,3-d]pyrimidine, SMILES is ClC1=NC=NC2=C1C(=C[NH]2)I, in an article , author is Fang, Hui-Lin, once mentioned of 123148-78-7, Name: 4-Chloro-5-iodo-7H-pyrrolo[2,3-d]pyrimidine.

Domino beta-C-H Functionalization and [3+2] Cycloaddition for Efficient Synthesis of Diverse Spiro and Polycyclic Compounds

The acetic acid catalyzed three-component reaction of pyrrolidine, aromatic aldehydes and 4-arylidene-5-methyl-2-phenylpyrazol-3-one in refluxing toluene gave functionalized 7 ‘-(E)-benzylidenespiro[pyrazole-4,1 ‘-pyrrolizines] in good yields and with high diastereoselectivity. The similar reaction with 2-arylidene-N,N’-dimethylbarbiturates resulted in mixture of Z/E-isomers of 7 ‘- arylidenespiro[pyrimidine-5,1 ‘-pyrrolizines] in good yields. However, the three-component with N-phenylmaleimides and sequential oxidation with DDQ reaction gave 8-(E)-arylidenedihydropyrrolo[3,4-a]pyrrolizines in satisfactory yields. The reaction mechanism included sequential beta-C-H functionalization of pyrrolidine, generation of conjugated azomethine ylides, and sequential [3+2] cycloaddition with active alkenes.

Interested yet? Read on for other articles about 123148-78-7, you can contact me at any time and look forward to more communication. Name: 4-Chloro-5-iodo-7H-pyrrolo[2,3-d]pyrimidine.

Reference:
Pyrimidine | C4H4N2 – PubChem,
,Pyrimidine – Wikipedia

Enzymes are biological catalysts that produce large increases in reaction rates and tend to be specific for certain reactants and products. 123148-78-7, Name is 4-Chloro-5-iodo-7H-pyrrolo[2,3-d]pyrimidine, molecular formula is C6H3ClIN3, belongs to pyrimidines compound. In a document, author is Lamichhane, Rajesh, introduce the new discover, Product Details of 123148-78-7.

Human liver-derived MAIT cells differ from blood MAIT cells in their metabolism and response to TCR-independent activation

Mucosal associated invariant T (MAIT) cells are anti-microbial innate-like T cells that are abundant in blood and liver. MAIT cells express a semi-invariant T-cell receptor (TCR) that recognizes a pyrimidine ligand, derived from microbial riboflavin synthesis, bound to MR1. Both blood and liver derived (ld)-MAIT cells can be robustly stimulated via TCR or by cytokines produced during bacterial or viral infection. In this study, we compared the functional and transcriptomic response of human blood and ld-MAIT cells to TCR signals (Escherichia coli or the pyrimidine ligand) and cytokines (IL-12 + IL-18). While the response of blood and ld-MAIT cells to TCR signals were comparable, following cytokine stimulation ld-MAIT cells were more polyfunctional than blood MAIT cells. Transcriptomic analysis demonstrated different effector programmes of ld-MAIT cells with the two modes of activation, including the enrichment of a tissue repair signature in TCR-stimulated MAIT cells. Interestingly, we observed enhancement of IL-12 signaling and fatty acid metabolism in untreated ld-MAIT cells compared with blood MAIT cells. Additionally, MAIT cells from blood and liver were modulated similarly by TCR and cytokine signals. Therefore, we report that blood and ld-MAIT cells are fundamentally different but undergo conserved changes following activation via TCR or by cytokines.

Balanced chemical reaction does not necessarily reveal either the individual elementary reactions by which a reaction occurs or its rate law. In my other articles, you can also check out more blogs about 123148-78-7. Product Details of 123148-78-7.

Reference:
Pyrimidine | C4H4N2 – PubChem,
,Pyrimidine – Wikipedia

Electric Literature of 123148-78-7, Enzymes are biological catalysts that produce large increases in reaction rates and tend to be specific for certain reactants and products. 123148-78-7, Name is 4-Chloro-5-iodo-7H-pyrrolo[2,3-d]pyrimidine, SMILES is ClC1=NC=NC2=C1C(=C[NH]2)I, belongs to pyrimidines compound. In a article, author is Li, Wei-Ya, introduce new discover of the category.

Scaffold-based selective SHP2 inhibitors design using core hopping, molecular docking, biological evaluation and molecular simulation

PTPN11 (coding the gene of SHP2), a classic non-receptor protein tyrosine phosphatase, is implicated in multiple cell signaling pathway. Abnormal activation of SHP2 has been shown to contribute to a variety of human diseases, including Juvenile myelomonocytic leukemia (JMML), Noonan syndrome and tumors. Thus, the SHP2 inhibitors have important therapeutic value. Here, based on the compound PubChem CID 8,478,960 (IC50 = 45.01 mu M), a series of thiophene [2,3-d] pyrimidine derivatives (IC50 = 0.4-37.87 mu M) were discovered as novel and efficient inhibitors of SHP2 through powerful core hopping and CDOCKER technology. Furthermore, the SHP2-PTP phosphatase activity assay indicated that Comp#5 (IC50 = 0.4 mu M) was the most active SHP2 inhibitor. Subsequently, the effects of Comp#5 on the structure and function of SHP2 were investigated through molecular dynamics (MD) simulation and post-kinetic analysis. The result indicated that Comp#5 enhanced the interaction of residues THR357, ARG362, LYS366, PRO424, CYS459, SER460, ALA461, ILE463, ARG465, THR507 and GLN510 with the surrounding residues, improving the stability of the catalytic active region and the entrance of catalytic active region. In particular, the Comp#5 conjugated with residue ARG362, elevating the efficient and selectivity of SHP2 protein. The study here may pave the way for discovering the novel SHP2 inhibitors for suffering cancer patients.

Electric Literature of 123148-78-7, Each elementary reaction can be described in terms of its molecularity, the number of molecules that collide in that step. The slowest step in a reaction mechanism is the rate-determining step.you can also check out more blogs about 123148-78-7.

Reference:
Pyrimidine | C4H4N2 – PubChem,
,Pyrimidine – Wikipedia

Related Products of 123148-78-7, The transformation of simple hydrocarbons into more complex and valuable products via catalytic C–H bond functionalisation has revolutionised modern synthetic chemistry. 123148-78-7, Name is 4-Chloro-5-iodo-7H-pyrrolo[2,3-d]pyrimidine, SMILES is ClC1=NC=NC2=C1C(=C[NH]2)I, belongs to pyrimidines compound. In a article, author is Osakunor, Derick N. M., introduce new discover of the category.

Schistosoma haematobium infection is associated with alterations in energy and purine-related metabolism in preschool-aged children

Author summary Schistosomiasis is a parasitic disease caused by helminth worms called schistosomes, and millions of people worldwide are infected. Studies in animal models indicate that the infection can cause alterations in metabolism of the host, leading to the observed clinical manifestations of the disease. However, there are limited human studies on the impact of schistosome infection on host metabolism, and none describing the changes that occur early in infection. There are also no studies relating to the species Schistosoma haematobium, which causes disease manifested in both the urinary and genital organs. To address this, we analysed the metabolic changes in response to the first S. haematobium infection and treatment in Zimbabwean preschool-aged children. We determined for the first time, that within three months of first infection, there are significant changes in metabolite profiles related to host energy (G6P, 3-PG, AMP, ADP) and purine (AMP, ADP) metabolism. These changes were associated with infection burden and were resolved within three months, following curative treatment. Our findings provide further understanding into the early host metabolic responses to the infection, consistent with clinical manifestations such as malnutrition, poor growth and poor physical and cognitive performance observed in schistosome-infected children. This demonstrates the need for early treatment of the infection, and will inform the development of appropriate interventions such as nutraceuticals in child feeding programs, aimed at reducing disease consequences. Further mechanistic studies will contribute to more understanding of the relationship between metabolic alterations and schistosomiasis in young children. Helminths are parasitic worms that infect over a billion people worldwide. The pathological consequences from infection are due in part, to parasite-induced changes in host metabolic pathways. Here, we analyse the changes in host metabolic profiles, in response to the first Schistosoma haematobium infection and treatment in Zimbabwean children. A cohort of 83 schistosome-negative children (2-5 years old) as determined by parasitological examination, guardian interviews and examination of medical records, was recruited at baseline. Children were followed up after three months for parasitological diagnosis of their first S. haematobium infection, by detection of parasite eggs excreted in urine. Children positive for infection were treated with the antihelminthic drug praziquantel, and treatment efficacy checked three months after treatment. Blood samples were taken at each time point, and capillary electrophoresis mass spectrometry in conjunction with multivariate analysis were used to compare the change in serum metabolite profiles in schistosome-infected versus uninfected children. Following baseline at the three-month follow up, 11 children had become infected with S. haematobium (incidence = 13.3%). Our results showed that infection with S. haematobium was associated with significant increases (>2-fold) in discriminatory metabolites, linked primarily with energy (G6P, 3-PG, AMP, ADP) and purine (AMP, ADP) metabolism. These observed changes were commensurate with schistosome infection intensity, and levels of the affected metabolites were reduced following treatment, albeit not significantly. This study demonstrates that early infection with S. haematobium is associated with alterations in host energy and purine metabolism. Taken together, these changes are consistent with parasite-related clinical manifestations of malnutrition, poor growth and poor physical and cognitive performance observed in schistosome-infected children.

Related Products of 123148-78-7, Consequently, the presence of a catalyst will permit a system to reach equilibrium more quickly, but it has no effect on the position of the equilibrium as reflected in the value of its equilibrium constant.I hope my blog about 123148-78-7 is helpful to your research.

Reference:
Pyrimidine | C4H4N2 – PubChem,
,Pyrimidine – Wikipedia

Related Products of 123148-78-7, Chemo-enzymatic cascade processes are invaluable due to their ability to rapidly construct high-value products from available feedstock chemicals in a one-pot relay manner. 123148-78-7, Name is 4-Chloro-5-iodo-7H-pyrrolo[2,3-d]pyrimidine, SMILES is ClC1=NC=NC2=C1C(=C[NH]2)I, belongs to pyrimidines compound. In a article, author is Bibi, Maria, introduce new discover of the category.

Exploring the ability of dihydropyrimidine-5-carboxamide and 5-benzyl-2,4-diaminopyrimidine-based analogues for the selective inhibition of L. major dihydrofolate reductase

To tackle leishmaniasis, search for efficient therapeutic drug targets should be pursued. Dihydrofolate reductase (DHFR) is considered as a key target for the treatment of leishmaniasis. In current study, we are interested in the design and synthesis of selective antifolates targeting DHFR from L. major. We focused on the development of new antifolates based on 3,4-dihydropyrimidine-2-one and 5-(3,5-dimethoxybenzyl)pyrimidine-2,4-diamine motif. Structure activity relationship (SAR) studies were performed on 4-phenyl ring of dihydropyrimidine (26-30) template. While for 5-(3,5-dimethoxybenzyl) pyrimidine-2,4-diamine, the impact of different amino acids (valine, tryptophan, phenylalanine, and glutamic acid) and two carbon linkers were explored (52-59). The synthesized compounds were assayed against LmDHFR. Compound 59 with the IC50 value of 0.10 mu M appeared as potent inhibitors of L. major. Selectivity for parasite DHFR over human DHFR was also determined. Derivatives 55-59 demonstrated excellent selectivity for LmDHFR. Highest selectivity for LmDHFR was shown by compounds 56 (SI = 84.5) and 58 (SI = 87.5). Compounds Antileishmanial activity against L. major and L. donovani promastigotes was also performed. To explore the interaction pattern of the synthesized compounds with biological macromolecules, the docking studies were carried out against homology modelled LmDHFR and hDHFR targets. (C) 2020 Elsevier Masson SAS. All rights reserved.

Related Products of 123148-78-7, One of the oldest and most widely used commercial enzyme inhibitors is aspirin, which selectively inhibits one of the enzymes involved in the synthesis of molecules that trigger inflammation. you can also check out more blogs about 123148-78-7.

Reference:
Pyrimidine | C4H4N2 – PubChem,
,Pyrimidine – Wikipedia

Chemistry is the science of change. But why do chemical reactions take place? Why do chemicals react with each other? The answer is in thermodynamics and kinetics, Formula: C6H3ClIN3, 123148-78-7, Name is 4-Chloro-5-iodo-7H-pyrrolo[2,3-d]pyrimidine, SMILES is ClC1=NC=NC2=C1C(=C[NH]2)I, belongs to pyrimidines compound. In a document, author is Abdallah, M., introduce the new discover.

Expired amoxicillin and cefuroxime drugs as efficient anticorrosives for Sabic iron in 1.0 M hydrochloric acid solution

The effects of two expired antibacterial drugs, amoxicillin (Amo) cefuroxime (Cef), on the corrosion behavior of Sabic iron in 1.0 M HCl solution were examined using weight loss, galvanostatic polarization (GAP), potentiodynamic anodic polarization, and electrochemical impedance spectroscopy techniques. The outcomes showed that the inhibition efficiency increased with increasing concentrations of Amo and Cef and decreased with temperature. The activity of inhibition of these compounds was elucidated by adsorption on Sabic iron surfaces. The adsorption process obeyed the Langmuir isotherm. The activation and adsorption thermodynamic parameters have been determined and clarified. GAP studies indicated that expired Amo and Cef served as mixed inhibitors. The impedance data showed capacitive loop which indicates that charge transfer governs corrosion reactions. Expired Amo and Cef drugs are good pitting inhibitors by positively shifting the pitting potential. There is a complete agreement between the inhibition efficacies obtained from the different measurements

A reaction mechanism is the microscopic path by which reactants are transformed into products. Each step is an elementary reaction. In my other articles, you can also check out more blogs about 123148-78-7. Formula: C6H3ClIN3.

Reference:
Pyrimidine | C4H4N2 – PubChem,
,Pyrimidine – Wikipedia

Children learn through play, and they learn more than adults might expect. Science experiments are a great way to spark their curiosity, Category: pyrimidines123148-78-7, Name is 4-Chloro-5-iodo-7H-pyrrolo[2,3-d]pyrimidine, SMILES is ClC1=NC=NC2=C1C(=C[NH]2)I, belongs to pyrimidines compound. In a article, author is Kraemer, Andreas, introduce new discover of the category.

Optimization of pyrazolo[1,5-a]pyrimidines lead to the identification of a highly selective casein kinase 2 inhibitor

Casein kinase 2 (CK2) is a constitutively expressed serine/threonine kinase that has a large diversity of cellular substrates. Thus, CK2 has been associated with a plethora of regulatory functions and dysregulation of CK2 has been linked to disease development in particular to cancer. The broad implications in disease pathology makes CK2 an attractive target. To date, the most advanced CK2 inhibitor is silmitasertib, which has been investigated in clinical trials for treatment of various cancers, albeit several off-targets for silmitasertib have been described. To ascertain the role of CK2 inhibition in cancer, other disease and normal physiology the development of a selective CK2 inhibitor would be highly desirable. In this study we explored the pyrazolo [1,5-a]pyrimidine hinge-binding moiety for the development of selective CK2 inhibitors. Optimization of this scaffold, which included macrocyclization, led to IC20 (31) a compound that displayed high in vitro potency for CK2 (K-D = 12 nM) and exclusive selectivity for CK2. Xray analysis revealed a canonical type-I binding mode for IC20 (31). However, the polar carboxylic acid moiety that is shared by many CK2 inhibitors including silmitasertib was required for potency but limits the cellular activity of IC20 (31) and the cellular IC50 dropped to the low micromolar range. In summary, IC20 (31) represents a highly selective and potent inhibitor of CK2, which can be used as a tool compound to study CK2 biology and potential new applications for the treatment of diseases. (c) 2020 Elsevier Masson SAS. All rights reserved.

Note that a catalyst decreases the activation energy for both the forward and the reverse reactions and hence accelerates both the forward and the reverse reactions. you can also check out more blogs about 123148-78-7. Category: pyrimidines.

Reference:
Pyrimidine | C4H4N2 – PubChem,
,Pyrimidine – Wikipedia

The reaction rate of a catalyzed reaction is faster than the reaction rate of the uncatalyzed reaction at the same temperature. Recommanded Product: 123148-78-7, 123148-78-7, Name is 4-Chloro-5-iodo-7H-pyrrolo[2,3-d]pyrimidine, SMILES is ClC1=NC=NC2=C1C(=C[NH]2)I, in an article , author is Mohamed, Mosselhi A. M., once mentioned of 123148-78-7.

Nucleosides 11: synthesis of new derivatives of pyrido[2,3-d]pyrimidines and their nucleosides

Reaction of 6-amino-2-methylthio-3-methyluracil with ethyl ethoxymethyleneoxaloacetate or methyl(Z)-2-acetylamino-3-dimethylaminopropenoates afforded diethyl 2-(1,6-dihydro-1-methyl-2-(methylthio)-6-oxopyrimidin-4-yl-amino)methylene malonate or (2E)-methyl 3-(1,6-dihydro-1-methyl-2-(methylthio)-6-oxopyrimidin-4-yl-amino)-2-acetamidoacrylate, respectively. Cyclization of each of the latter products by sodium ethoxide afforded new pyrido [2,3-d]pyrimidines, which were ribosylated with 1-O-acetyl-2,3,5-O-benzoyl-beta-D-ribofuranose by the silylation method yielded the protected nucleosides. The protected nucleosides were debenzoylated by sodium methoxide to afford novel pyrido[2,3-d]pyrimidine nucleosides. The structural assignmentsv for the new compounds were based on their elemental analysis and spectroscopic data.

But sometimes, even after several years of basic chemistry education, it is not easy to form a clear picture on how they govern reactivity! 123148-78-7, you can contact me at any time and look forward to more communication. Recommanded Product: 123148-78-7.

Reference:
Pyrimidine | C4H4N2 – PubChem,
,Pyrimidine – Wikipedia