Category: pyrimidines

Ferris, J. P.; Joshi, P. C.; Lawless, J. G. published the artcile< Chemical evolution. XXIX. Pyrimidines from hydrogen cyanide>, Related Products of 15837-41-9, the main research area is pyrimidine formation prebiosis; hydrogen cyanide pyrimidine formation.

Dilute (0.1M) solutions of HCN condensed to oligomers at pH 8-9. Hydrolysis of these oligomers at pH 8.5 or with 6N HCl yielded 4,5-dihydroxypyrimidine as the most abundant pyrimidine product along with orotic acid and 5-hydroxyuracil. Thus, the 3 major N-containing classes of biomols. could have originated from HCN on the primitive earth. The observation of the formation of orotic acid and 4-aminoimidazole-5-carboxamide by the hydrolysis of the HCN oligomers suggested that once the initially formed pyrimidines and purines were consumed, those life forms persisted which evolved enzymes for the conversion of these intermediates to the pyrimidines and purines present in contemporary RNA.

BioSystems published new progress about Molecular evolution. 15837-41-9 belongs to class pyrimidines, and the molecular formula is C4H4N2O2, Related Products of 15837-41-9.

Referemce:
Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia

Kang, Dongwei; Feng, Da; Sun, Yanying; Fang, Zengjun; Wei, Fenju; De Clercq, Erik; Pannecouque, Christophe; Liu, Xinyong; Zhan, Peng published the artcile< Structure-Based Bioisosterism Yields HIV-1 NNRTIs with Improved Drug-Resistance Profiles and Favorable Pharmacokinetic Properties>, Related Products of 18740-39-1, the main research area is thiophenepyrimidine piperidine substituted preparation antiHIV activity.

The development of efficacious NNRTIs for AIDS therapy commonly encountered the rapid generation of drug-resistant mutations, which becomes a major impediment to effective anti-HIV treatment. Using a structure-based bioisosterism strategy, a series of piperidine-substituted thiophene[2,3-d]pyrimidine derivatives were designed and synthesized. Compound I yielded the greatest potency, exhibiting significantly better anti-HIV-1 activity than ETR against all of the tested NNRTI-resistant HIV-1 strains. In addition, the phenotypic (cross)resistance of I and other NRTIs to the different selected HIV-1 strains was evaluated. As expected, no phenotypic cross-resistance against the NRTIs (AZT and PMPA) was observed with the mutant Ires strain. Furthermore, I was identified with improved solubility, lower CYP liability, and hERG inhibition. Remarkably, I exhibited optimal pharmacokinetic properties in rats (F = 37.06%) and safety in mice (LD50 > 2000 mg/kg), which highlights I as a promising anti-HIV-1 drug candidate.

Journal of Medicinal Chemistry published new progress about Anti-HIV agents. 18740-39-1 belongs to class pyrimidines, and the molecular formula is C6H2Cl2N2S, Related Products of 18740-39-1.

Referemce:
Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia

Pithova, P.; Sorm, F. published the artcile< Influence of some derivatives and structural analogs of pyrimidine and purine bases on the degradation of uracil>, Safety of 6-Bromo-1,2,4-triazine-3,5(2H,4H)-dione, the main research area is .

The enzymic degradation of uracil (I) by rat liver Me2CO powder is inhibited by compounds possessing the NHCONH grouping in a 6-membered ring. Their activity, however, disappears on methylation of N. Xanthine, uric acid, orotie acid, 2-pyridone, and 5-bromo-6-azauracil inhibit the 1st stage of I degradation, viz., its reduction to dihydrouraeil (II). The inhibitory action of 5-substituted I derivatives is apparently of competitive character. None of the above compounds, however, inhibits the degradation of II and no accumulation of β-ureidopropionie acid and β-alanine was detected in the reaction mixture

Collection of Czechoslovak Chemical Communications published new progress about 4956-05-2. 4956-05-2 belongs to class pyrimidines, and the molecular formula is C3H2BrN3O2, Safety of 6-Bromo-1,2,4-triazine-3,5(2H,4H)-dione.

Referemce:
Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia

Zasosov, V. A.; Nikulina, T. N.; Blinova, L. S.; Onoprienko, V. S.; Sycheva, V. N.; Sokolova, G. N.; Borodina, K. S.; Denisova, K. V. published the artcile< Synthesis of 4-(p-aminobenzenesulfonamido)-5,6-dimethoxypyrimidine>, Synthetic Route of 5018-38-2, the main research area is amino benzenesulfonamido methoxy pyrimidine; sulfamide pyrimidyl.

CO2H)2 was esterified with MeOH and then treated with MeOCH2CO2CO2Me(from ClCH2CO2Me and NaOMe) to give MeO2CCH(OMe)COCO2Me, which was decarbonylated at 210° to give MeOCH(CO2Me)2. The latter reacted with NH3 and then HCONH2 in the presence of NaOEt to form the di-Na salt of 4,6-dihydroxy-5-methoxypyrimidine, which was converted to the 4,6-dichloro derivative (I) with POCl3 and PhNMe2. I reacted with NH3 in DMF to form the 4-amino derivative, which yielded 4-amino-5,6-dimethoxypyrimidine with NaOH in MeOH. The latter was converted to the title compound (II) by treatment with 4-MeO2CNHC6H4SO2Cl in pyridine, followed by hydrolysis with concentrated HCl.

Khimiko-Farmatsevticheskii Zhurnal published new progress about 5018-38-2. 5018-38-2 belongs to class pyrimidines, and the molecular formula is C5H4Cl2N2O, Synthetic Route of 5018-38-2.

Referemce:
Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia

O’Brien, Darrell E.; Weinstock, Louis T.; Springer, Robert H.; Cheng, Chia-Chung published the artcile< Pyrimidines. XIX. Pyrimidol[4,5 - e]dihydro - 1,3-oxazines and related compounds>, Category: pyrimidines, the main research area is PYRIMIDO DIHYDRO OXAZINES; OXAZINES PYRIMIDO DIHYDRO.

A number of 2-substituted 4,5-dihydroxy-6-(substituted aminomethyl)pyridimines (I) were prepared from the corresponding 2-substituted 4,5-dihydroxypyrimidines by a new pyrimidine Mannich reaction. The structure of I was proved by an independent synthesis. Further study of this reaction led to the synthesis of pyrimido[4,5-e]dihydro-1,3-oxazines (II). 24 references.

Journal of Heterocyclic Chemistry published new progress about Mannich reaction. 15837-41-9 belongs to class pyrimidines, and the molecular formula is C4H4N2O2, Category: pyrimidines.

Referemce:
Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia

Raubo, Piotr; Carbajo, Rodrigo J.; McCoull, William; Raubo, Joanna; Thomas, Morgan published the artcile< Diversity-orientated synthesis of macrocyclic heterocycles using a double SNAr approach>, Reference of 18740-39-1, the main research area is macrocyclic heterocycle preparation enantioselective diastereoselective regioselective antitumor activity microwave.

An efficient macrocyclization approach based on the double aromatic nucleophilic substitution (SNACK) was developed. This methodol. allows a facile incorporation of heterocyclic motifs into macrocyclic rings and rapid synthesis of a significant number of structurally diverse macrocycles e.g., I. SNACK macrocyclization enables preparation of stable diastereoisomers of conformationally restricted macrocycles (atropisomers) e.g., II and e.g., III. Practical application of SNACK macrocyclization in a drug discovery project was exemplified by the identification of high affinity macrocyclic binders of B-cell lymphoma 6 (BCL6).

Organic & Biomolecular Chemistry published new progress about Antitumor agents. 18740-39-1 belongs to class pyrimidines, and the molecular formula is C6H2Cl2N2S, Reference of 18740-39-1.

Referemce:
Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia

Rao, T. Sudhakar; Revankar, Ganapathi R. published the artcile< Synthesis of certain alkenyl purines and purine analogs>, Product Details of C7H8N4O, the main research area is alkenyl purine analog.

Synthesis of alkenyl derivatives of certain purines and purine analogs is described. Direct alkylation of the sodium salt of 6-chloropurine with 1-bromo-2-pentene or 4-bromo-2-methyl-2-butene in N,N-dimethylformamide furnished N-7, and N-9 alkenyl derivatives Similar alkylation of 2-amino-6-chloropurine provided the corresponding N-7, and N-9 alkenyl derivatives Acid hydrolysis of these chloro derivatives furnished the corresponding alkenyl hypoxanthines or alkenyl guanines. The direct alkylation of pyrrolo[2,3-d]pyrimidin-4(3H)-one gave N-3 alkenyl derivatives; the N-7 alkenyl derivatives were prepared starting from the 4-chloro derivatives Synthesis of 2-amino-7-(2-penten-1-yl)pyrrolo[2,3-d]pyrimidin-4(3H)-one was accomplished starting from 2-amino-4-methoxypyrrolo[2,3-d]pyrimidine. These alkenyl derivatives were found to be devoid of anti-HCMV activity in vitro.

Journal of Heterocyclic Chemistry published new progress about Alkenylation. 84955-32-8 belongs to class pyrimidines, and the molecular formula is C7H8N4O, Product Details of C7H8N4O.

Referemce:
Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia

Guan, Aiying; Wang, Mingan; Yang, Jinlong; Wang, Lizeng; Xie, Yong; Lan, Jie; Liu, Changling published the artcile< Discovery of a New Fungicide Candidate through Lead Optimization of Pyrimidinamine Derivatives and Its Activity against Cucumber Downy Mildew>, Formula: C5H4Cl2N2O, the main research area is fungicide pyrimidinamine derivative preparation lead optimization cucumber downy mildew; development of resistance; downy mildew; pyrimidinamine fungicide candidate; unique mode of action.

Downy mildew is one of the most highly destructive of the diseases that cause damage to fruits and vegetables. Because of the continual development of resistance, it is important to discover new fungicides with different modes of action from existing fungicides for the control of downy mildew. This study is a continuation of our previous work on the novel pyrimidinamine lead compound, (I), and includes field trials for the identification of the optimal candidate. A new compound, 5-Chloro-N-(2-(6-(4-chlorophenoxy)pyridin-3yl)ethyl)-6-(difluoromethyl)pyrimidin-4-amine, (II), was obtained from 4,5-Dichloro-6-(difluoromethyl)pyrimidine and 2-(6-(4-chlorophenoxy)pyridin-3-yl)ethanamine, which gave a lower EC50 value (0.10 mg/L) against downy mildew than lead compound I (0.19 mg/L) and the com. fungicides diflumetorim, dimethomorph, and cyazofamid (1.01-23.06 mg/L). Compound II displayed similar broad-spectrum fungicidal activity to compound I but better field efficacy than compound I, cyazofamid, and flumorph. The present work indicates that pyrimidinamine compound II is a candidate for further development as a com. fungicide for the control of downy mildew.

Journal of Agricultural and Food Chemistry published new progress about Agrochemical fungicides. 5018-38-2 belongs to class pyrimidines, and the molecular formula is C5H4Cl2N2O, Formula: C5H4Cl2N2O.

Referemce:
Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia

Reddy, L. Srikanth; Naik, B. Eswara published the artcile< Design,synthesis and structural elucidation of some novel heterocyclic molecules derived from thieno [2, 3-d] pyrimidine nucleus>, Product Details of C6H2Cl2N2S, the main research area is phenyl thienotriazolopyrimidine preparation.

Several new thieno[2,3-d]pyrimidine derivtives, 3-substituted phenyl-5-(thiophen-2- yl)thieno[3,2-e][1,2,4]triazolo[4,3-c]pyrimidines 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.

Heterocyclic Letters published new progress about Aromatic carboxylic acids Role: RCT (Reactant), RACT (Reactant or Reagent). 18740-39-1 belongs to class pyrimidines, and the molecular formula is C6H2Cl2N2S, Product Details of C6H2Cl2N2S.

Referemce:
Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia

Adriaens, E. L.; Lozet, F. published the artcile< Fermented beverages of Ruanda natives>, Computed Properties of 3921-01-5, the main research area is .

The preparation of hydromel (I), and banana (II) and sorgho (III) beers is described. I contained before and after fermentation: dry extract 365.26-115.28, inorganic matter 10.78-6.20, total N 3.15-1.93, reducing sugars in glucose 250.0-66.11, sucrose 12.45-4.29, acidity as H2SO4 1.62-5.78 g./l.; in the wort: wax and sorgho yeast 86.9 g./l.; in the I EtOH 8.6°. Corresponding data for II were: 197.12-52.63, 11.14-9.87, trace-3.15, 93.74-19.16, 80.29-2.95, 3.28-4.21 g./l. and EtOH in the end product 9.46°. “”Inkanganza”” made from II with addition of honey and sorgho yeast gave, before and after fermentation: 149.2-52.88, 10.88-5.34, 5.08-3.75, 116.54-12.45, 11.91-4.33, 4.9-3.92 g./l., EtOH 11.5°. Wort of III and the end product contained: dry extract 172.9-256.8, inorganic 5.16-6.86, N 6.08-26.56, glucose 43.02-trace, sucrose 5.57-16.06, acids 2.11-5.98 g./l., EtOH 3.75°. Uryama, a III containing about 10% honey, gave: 244.83-136.24, 7.08-7.37, 10.68-3.15, 105.17-37.43, trace-0.0, 3.92-10.15 g./l., EtOH 6.4°.

Bull. Agr. Congo Belge published new progress about Beer. 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