Day: October 13, 2022

Al-Masoudi, Najim A.; Pfleiderer, Wolfgang; Lazrek, Hassan B. published the artcile< Synthesis of some novel 1-(5-thio-β-D-glucopyranosyl)-6-azauracil derivatives. Thio sugar nucleosides>, Quality Control of 4956-05-2, the main research area is thio sugar azauracil nucleoside; thioglucopyranosyl azauracil; glycosidation thioglucopyranose azauracil.

Title compounds I (R = H, Br, SBn, NHBn) were prepared via glycosidation of azauracil with thioglucopyranose derivatives

Nucleosides & Nucleotides published new progress about 4956-05-2. 4956-05-2 belongs to class pyrimidines, and the molecular formula is C3H2BrN3O2, Quality Control of 4956-05-2.

Referemce:
Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia

Schweizer, Stefan A.; Bach, Thorsten published the artcile< Regioselective Pd(0)-catalyzed Hiyama cross-coupling reactions at dihalo-substituted heterocycles>, Product Details of C4H2Br2N2, the main research area is haloheterocycle regioselective Hiyama cross coupling alkyl fluorosilane palladium catalyst.

The regioselectivity of the Hiyama cross-coupling reaction at various dihalo-substituted heterocycles was studied. Me 2,3-dibromo-5-furancarboxylate and n-octyltrifluorosilane were employed to find optimum reaction conditions [CsF; Pd2dba3/P(2-furyl)3 as catalyst, 80-150 °C in toluene or benzene] for the desired transformation. Subsequent experiments with the title compounds and with different primary alkyltrifluorosilanes illustrate the generality of this regiochem. process.

Synlett published new progress about Haloalkyl silanes, fluoroalkyl Role: RCT (Reactant), RACT (Reactant or Reagent). 3921-01-5 belongs to class pyrimidines, and the molecular formula is C4H2Br2N2, Product Details of C4H2Br2N2.

Referemce:
Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia

Wu, Xiao-qiong published the artcile< New method for synthesis of 4,6-dichloro-5-methoxypyrimidine>, Category: pyrimidines, the main research area is dichloro methoxypyrimidine aminolysis cyclization chlorination.

The research aimed to improve the synthesis method of 4,6-dichloro-5-methoxypyrimidine. 2-Methoxy di-Me malonate was used to prepare 4,6-dichloro-5- methoxypyrimidine by aminolysis, cyclization and chlorination. Results showed that the synthetic product was analyzed by IR spectrum, hydrogen NMR and mass spectrometry. The overall yield was 42%. It was concluded that the synthesis method was suitable for industrial production, because of its warm condition and higher yield.

Anhui Nongye Kexue published new progress about Aminolysis. 5018-38-2 belongs to class pyrimidines, and the molecular formula is C5H4Cl2N2O, Category: pyrimidines.

Referemce:
Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia

Miyakawa, Shin; Cleaves, H. James; Miller, Stanley L. published the artcile< The Cold Origin of Life: B. Implications Based on Pyrimidines and Purines Produced From Frozen Ammonium Cyanide Solutions>, Application In Synthesis of 15837-41-9, the main research area is ammonium cyanide purine pyrimidine life origin.

A wide variety of pyrimidines and purines were identified as products of a dilute frozen ammonium cyanide solution that had been held at -78° for 27 yr. This demonstrates that both pyrimidines and purines could have been produced on the primitive earth in a short time by eutectic concentration of HCN, even though the concentration of HCN in the primitive ocean may have been low. We suggest that eutectic freezing is the most plausible demonstrated mechanism by which HCN polymerizations could have produced biol. important prebiotic compounds

Origins of Life and Evolution of the Biosphere published new progress about Freezing (eutectic). 15837-41-9 belongs to class pyrimidines, and the molecular formula is C4H4N2O2, Application In Synthesis of 15837-41-9.

Referemce:
Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia

Crocker, Leander; Koehler, Philipp; Bernhard, Patrick; Kerbs, Antonina; Euser, Tijmen; Fruk, Ljiljana published the artcile< Enzyme-inspired flavin-polydopamine as a biocompatible nanoparticle photocatalyst>, Category: pyrimidines, the main research area is flavin polydopamine biocompatibility nanoparticle photocatalyst.

A new approach aimed at designing an enzyme-inspired photocatalyst is presented that exploits the inherent photocatalytic activity of flavin and the facile polymerization of dopamine to afford hybrid cofactor-containing nanoparticles. The flavin-polydopamine system benefits from ease of synthesis, tunability in terms of size and activity, and excellent temporal control over the catalyzed reactions. This novel, versatile photocatalyst exhibits both photooxidation and photoreduction of chromogenic enzymic substrates. In addition, the prepared hybrid nanoparticles are shown to be non-toxic, paving the way to their use in a wider range of applications beyond green catalysis, such as antioxidant adjuvants to various therapeutic approaches.

Nanoscale Horizons published new progress about Antioxidants. 2244-11-3 belongs to class pyrimidines, and the molecular formula is C4H4N2O5, Category: pyrimidines.

Referemce:
Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia

Liu, Chunjian; Lin, James; Langevine, Charles; Smith, Daniel; Li, Jianqing; Tokarski, John S.; Khan, Javed; Ruzanov, Max; Strnad, Joann; Zupa-Fernandez, Adriana; Cheng, Lihong; Gillooly, Kathleen M.; Shuster, David; Zhang, Yifan; Thankappan, Anil; McIntyre, Kim W.; Chaudhry, Charu; Elzinga, Paul A.; Chiney, Manoj; Chimalakonda, Anjaneya; Lombardo, Louis J.; Macor, John E.; Carter, Percy H.; Burke, James R.; Weinstein, David S. published the artcile< Discovery of BMS-986202: A Clinical Tyk2 Inhibitor that Binds to Tyk2 JH2>, Synthetic Route of 89793-12-4, the main research area is BMS986202 Tyk2 JH2 inhibitor antiinflammatory inflammation.

A search for structurally diversified Tyk2 JH2 ligands from 6 (BMS-986165), a pyridazine carboxamide-derived Tyk2 JH2 ligand as a clin. Tyk2 inhibitor currently in late development for the treatment of psoriasis, began with a survey of six-membered heteroaryl groups in place of the N-Me triazolyl moiety in 6. The x-ray co-crystal structure of an early lead (12) revealed a potential new binding pocket. Exploration of the new pocket resulted in two front-runners for a clin. candidate. The potential hydrogen bonding interaction with Thr599 in the pocket was achieved with a tertiary amide moiety, confirmed by the x-ray co-crystal structure of 29. When the diversity search was extended to nicotinamides, a single fluorine atom addition was found to significantly enhance the permeability, which directly led to the discovery of 7 (BMS-986202) as a clin. Tyk2 inhibitor that binds to Tyk2 JH2. The preclin. studies of 7, including efficacy studies in mouse models of IL-23-driven acanthosis, anti-CD40-induced colitis, and spontaneous lupus, will also be presented.

Journal of Medicinal Chemistry published new progress about Acanthosis. 89793-12-4 belongs to class pyrimidines, and the molecular formula is C7H7ClN2O2, Synthetic Route of 89793-12-4.

Referemce:
Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia

Rankovic, Zoran; Cai, Jiaqiang; Fradera, Xavier; Dempster, Maureen; Mistry, Ashvin; Mitchell, Ann; Long, Clive; Hamilton, Emma; King, Angela; Boucharens, Sylviane; Jamieson, Craig; Gillespie, Jonathan; Cumming, Iain; Uitdehaag, Joost; van Zeeland, Mario published the artcile< Dioxo-triazines as a novel series of cathepsin K inhibitors>, Electric Literature of 4956-05-2, the main research area is dioxo triazine preparation cathepsin K inhibitor structure.

A novel dioxo-triazine series of cathepsin K inhibitors was identified from HTS. A rapid exploratory program led to the discovery of potent and selective cathepsin K inhibitors, typified by compound 24 which displayed IC50 values of 17 nM against catK and >10,000 nM in catL, catB and catS assays.

Bioorganic & Medicinal Chemistry Letters published new progress about Antiosteoporotic agents. 4956-05-2 belongs to class pyrimidines, and the molecular formula is C3H2BrN3O2, Electric Literature of 4956-05-2.

Referemce:
Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia

Gronowitz, S.; Hoernfeldt, A. B.; Kristjansson, V.; Musil, T. published the artcile< On the synthesis of various thienyl- and selenienylpyrimidines>, Computed Properties of 3921-01-5, the main research area is halopyrimidine coupling thiopheneboronic acid; selenopheneboronic acid coupling halopyrimdine; pyrimidineboronic acid coupling bromothiophene; bromoselenophene coupling pyrimidineboronic acid; palladium coupling catalyst halopyrimidine; thienylpyrimidine; selenienylpyrimidine.

Various thienyl- and selenienylpyrimidines, including 5-substituted uracils, were prepared by the Pd(0)-catalyzed coupling between halopyrimidines I (R = H, Cl, Br, Me3CO, PhCH2O; R1 = Br, H) and thiopheneboronic acids and selenopheneboronic acids II [R2 = B(OH)2; X = S, Se, resp.]. 5-Bromouracil had to be protected as the tert-butoxy or benzyloxy derivative in order to achieve successful coupling. The compounds could also be obtained in a reversed manner, when pyrimidineboronic acids I [R = H, Me3CO; R1 = B(OH)2] were coupled with halothiophenes and haloselenophenes II (R2 = Br; X = S, Se).

Chemica Scripta published new progress about Coupling reaction. 3921-01-5 belongs to class pyrimidines, and the molecular formula is C4H2Br2N2, Computed Properties of 3921-01-5.

Referemce:
Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia

Prabhakar, Virupakshi; Kondra, Sudhakar Babu; Maddula, Srinivasula Reddy; Parandhama, G.; Latha, J. published the artcile< Synthesis, structural elucidation of novel thieno [2,3-d] pyrimidine core unit containing 1,2,4-triazoles and thiophenes as potent antimicrobial activity>, Application In Synthesis of 18740-39-1, the main research area is aryl thiophenyl thienotriazolopyrimidine preparation antibacterial antifungal activity SAR.

Several new thieno[3,2-e][1,2,4]triazolo[4,3-c]pyrimidines I [R = Ph, 4-MeC6H4, 4-MeOC6H4, etc.] were synthesized starting from thieno[2,3-d]pyrimidine-2,4-diol. The characterization of the newly synthesized compounds was established by IR, 1H NMR, 13C NMR and mass spectral anal. The final compounds I were screened for their antibacterial activity against Bacillus subtilis and Staphylococcus aureus from Gram pos. group of bacteria and Escherichia coli and Klebsiella pneumonia from Gram neg. group of bacteria and antifungal activity against Candida albicans and Aspergillus flavus. Antibacterial and antifungal activities were evaluated and compared with the standard drugs. From antibacterial and antifungal activities screening results, it was observed that compounds I [R = pyridin-3-yl, 1H-indol-2-yl, 4-F3CC6H4] possessed good activity.

Organic Chemistry: Current Research published new progress about Antibacterial agents. 18740-39-1 belongs to class pyrimidines, and the molecular formula is C6H2Cl2N2S, Application In Synthesis of 18740-39-1.

Referemce:
Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia

Riederer, Heinz; Huettermann, Juergen published the artcile< Matrix-isolation of free radicals from 5-halouracils. 3. Electron spin resonance of base oxidation in aqueous acidic glasses>, Computed Properties of 4956-05-2, the main research area is ESR irradiated nucleic acid base; uracil irradiated ESR; halouracil irradiated ESR; thymine irradiated ESR; nucleoside derivative irradiated ESR.

ESR of x-irradiated aqueous acidic glasses (5.3 M H2SO4, 7.2-14.7 M H3PO4) was used to study the base π-cations of the nucleic acid constituents uracil (U), thymine (T), and the range of 5-halouracils (FU, ClU, BU, IU) as well as their nucleoside derivatives, and to follow their secondary reactions. High solute concentrations (>50 mM) and the presence of electron scavengers (100-200 mM Na2S2O8 or H2O2) favored cation formation and stabilization and suppressed the formation of other solute radicals. Generation of the base cations resulted from transfer of a (possibly) excited solvent hole to the pyrimidine base during x-irradation at 77 K and from attack of the trapped solvent hole (SO4-: or HPO4-:) after thermal activation at 145-65 K. The base cations were either deprotonated at N1, as in most of the free bases, or added OH- at C6 in the nucleosides, where the deoxyribose moiety prevented deprotonation. This hydroxylation was suppressed in a water-deficient system (e.g., 14.7 M H3PO4) but very efficient in 5.3 M H2SO4. The structures of both the primary and secondary radicals were confirmed in most cases by a complete simulation of the exptl. ESR powder spectra. The ESR parameters obtained display a strong influence of the 5 substituent (i.e., the halogens) on the spin-d. distribution in the radicals. Characteristic for the π cations was the high spin d. in the halogen π orbital, ranging from 8% in FU to 40% in IU. Moreover, the amount of H2O in the environment exerts a considerable influence on the halogen spin densities in the charged cation.

Journal of Physical Chemistry published new progress about ESR (electron spin resonance). 4956-05-2 belongs to class pyrimidines, and the molecular formula is C3H2BrN3O2, Computed Properties of 4956-05-2.

Referemce:
Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia