Day: November 10, 2022

Yin, Weiyu published the artcileHighly Practical Synthesis of Nitriles and Heterocycles from Alcohols under Mild Conditions by Aerobic Double Dehydrogenative Catalysis, HPLC of Formula: 143426-50-0, the main research area is alc aerobic double dehydrogenation ammonia nitrile synthesis; biaryl heterocycle one pot synthesis nitrile in situ heterocyclization.

A mild, aerobic, catalytic process for obtaining nitriles directly from alcs. and aqueous ammonia is described (RC6H4CH2OH + NH3 → RC6H4CN). The reaction proceeds via a dehydrogenation cascade mediated by catalytic CuI, bpy, and TEMPO in the presence of O2. The substrate scope is broad including various functionalized aromatic and aliphatic alcs. This protocol enabled the one-pot synthesis of various biaryl heterocycles directly from com. available alcs. (e.g., PhCH2OH + NH3 in first step; addition of ethylenediamine in second step → 2-phenyl-4,5-dihydro-1H-imidazole).

Organic Letters published new progress about Aliphatic alcohols Role: RCT (Reactant), RACT (Reactant or Reagent). 143426-50-0 belongs to class triazoles, name is 4-(1,2,4-Triazol-1-yl)benzyl Alcohol, and the molecular formula is C9H9N3O, HPLC of Formula: 143426-50-0.

Referemce:
1,2,3-Triazole – Wikipedia,
Triazoles – an overview | ScienceDirect Topics

Yuan, Shuo published the artcileBronsted Acid-Catalyzed Direct C(sp2)-H Heteroarylation Enabling the Synthesis of Structurally diverse Biaryl Derivatives, Related Products of triazoles, the main research area is chloro heteroarene arene hexafluoroisopropanol catalyst arylation; heterocyclic biaryl preparation.

Bronsted acid-catalyzed direct C(sp2)-H heteroarylation that enabled the synthesis of biaryl fragments in moderate to excellent yields (up to 99% yield), which was also performed at a gram scale and successfully applied to the privileged quinazoline scaffolds of the first-generation epidermal growth factor receptor (EGFR) inhibitors Gefitinib and Erlotinib, offering rapid access to a series of quinazoline-based biaryl compounds Addnl., the late-stage diversifications were performed based on the compound 5-methyl-7-(2,4,6-trimethoxyphenyl)-[1,2,4]triazolo[1,5-a]pyrimidine, generating a library of structurally diverse and complex biaryl compounds

Advanced Synthesis & Catalysis published new progress about Arylation. 24415-66-5 belongs to class triazoles, name is 7-Chloro-5-methyl-[1,2,4]triazolo[1,5-a]pyrimidine, and the molecular formula is C6H5ClN4, Related Products of triazoles.

Referemce:
1,2,3-Triazole – Wikipedia,
Triazoles – an overview | ScienceDirect Topics

Umar, Tarana published the artcileA multifunctional therapeutic approach: Synthesis, biological evaluation, crystal structure and molecular docking of diversified 1H-pyrazolo[3,4-b]pyridine derivatives against Alzheimer’s disease, Application of 7-Chloro-5-methyl-[1,2,4]triazolo[1,5-a]pyrimidine, the main research area is piperazinyl pyrazolopyridinyl acetamide preparation docking cholinesterase inhibitor amyloid aggregation; AChE inhibitors; Amyloid β aggregation inhibitors; Docking; N-(1H-pyrazolo[3,4-b]pyridin-3-yl)acetamides; Selectivity.

2-(Piperazin-1-yl)-N-(1H-pyrazolo[3,4-b]pyridin-3-yl)acetamides I [R = piperidin-1-yl, 4-methylpiperazin-1-yl, Et 4-((4-yl)piperazin-1-yl)quinoline-3-carboxylate, etc.] were described as a new class of selective and potent acetylcholinesterase (AChE) inhibitors and amyloid β aggregation inhibitors. Formation of synthesized compounds I was justified via 1H NMR, 13C NMR, mass spectra and single crystal X-Ray diffraction study. All compounds were evaluated for their acetylcholinesterase and butyrylcholinesterase inhibitory activity, inhibition of self-mediated Aβ aggregation and Cu(II)-mediated Aβ aggregation. Also, docking study was carried out in concordance with in vitro results. The most potent mol. amongst the derivatives exhibited excellent anti-AChE activity (IC50 = 4.8 nM). Kinetic study of I [R = 2-((4-yl)piperazin-1-yl)-N-(1H-pyrazolo[3,4-b]pyridin-3-yl)acetamide] suggested it to be a mixed type inhibitor. In vitro study revealed that all the compounds were capable of inhibiting self-induced β-amyloid (Aβ) aggregation with the highest inhibition percentage to be 81.65%. Potency of I [R = Et 4-((4-yl)piperazin-1-yl)quinoline-3-carboxylate, 2-((4-yl)piperazin-1-yl)-N-(1H-pyrazolo[3,4-b]pyridin-3-yl)acetamide] to inhibit self-induced Aβ1-42 aggregation was ascertained by TEM anal. Compounds were also evaluated for their Aβ disaggregation, antioxidation, metal-chelation activity.

European Journal of Medicinal Chemistry published new progress about Aggregation. 24415-66-5 belongs to class triazoles, name is 7-Chloro-5-methyl-[1,2,4]triazolo[1,5-a]pyrimidine, and the molecular formula is C6H5ClN4, Application of 7-Chloro-5-methyl-[1,2,4]triazolo[1,5-a]pyrimidine.

Referemce:
1,2,3-Triazole – Wikipedia,
Triazoles – an overview | ScienceDirect Topics

Gomez, Laurent published the artcileDesign and Synthesis of Novel and Selective Phosphodiesterase 2 (PDE2a) Inhibitors for the Treatment of Memory Disorders, Synthetic Route of 24415-66-5, the main research area is triazolopyrimidine preparation PDE2a inhibitor SAR memory disorder treatment.

A series of potent and selective [1,2,4]triazolo[1,5-a]pyrimidine PDE2a inhibitors is reported. The design and improvement of the binding properties of this series was achieved using X-ray crystal structures in conjunction with careful anal. of electronic and structural requirements for the PDE2a enzyme. One of the lead compounds, compound I (DNS-8254), was identified as a potent and highly selective PDE2a enzyme inhibitor with favorable rat pharmacokinetic properties. Interestingly, the increased potency of compound I was facilitated by the formation of a halogen bond with the oxygen of Tyr827 present in the PDE2a active site. In vivo, compound I demonstrated significant memory enhancing effects in a rat model of novel object recognition. Taken together, these data suggest that compound I may be a useful tool to explore the pharmacol. of selective PDE2a inhibition.

Journal of Medicinal Chemistry published new progress about Memory disorders. 24415-66-5 belongs to class triazoles, name is 7-Chloro-5-methyl-[1,2,4]triazolo[1,5-a]pyrimidine, and the molecular formula is C6H5ClN4, Synthetic Route of 24415-66-5.

Referemce:
1,2,3-Triazole – Wikipedia,
Triazoles – an overview | ScienceDirect Topics

Werbel, Leslie M. published the artcilePotential antimalarial substances. XIV. [[(Dialkylamino)alkyl]amino]pyrimido[1,2-a]benzimidazoles, 2,3,-dihydro-1H-cyclopenta[4,5]pyrimido[1,2-a]benzimidazoles, and s-triazolo[1,5-a]pyrimidines as potential antimalarial agents, Synthetic Route of 24415-66-5, the main research area is pyrimido benzimidazoles; benzimidazoles pyrimido; cyclopentapyrimidobenzimidazoles; triazolo pyrimidines; pyrimidines triazolo.

The structure of the product of the reaction of 2-aminobenzimidazole with ethyl acetoacetate was established by NMR spectroscopy as 2-methylpyr imido[1,2-a]benzimidazol-4-ol (I). 7(and 8)-Chloro-2-methylpyrimido[1,2-a]benzimidazol-4-ol (II and III), 2-(trifluoromethyl)pyrimido[1,2-a]benzimidazol-4-ol, 2,7,8-trimethylpyrimido[1,2-a]benzimidazol-4-ol, 2-benzyl-1,2,3,4-tetrahydropyrido-[4′,3′:4,5]pyrimido[1,2-a]benzimidazol-12-ol, 1,2,3,4-tetrahydro-benzimidazo[2,1-b]quinazolin-12-ol, and 2,3-dihydro-1H-cyclopenta[4,5]pyrimido[1,2-a]benzimidazol-11-ol (IV) were prepared in a similar manner. Chlorination of I, II, III, IV, and 5-methyl-s-triazolo[1,5-a]pyrimidin-7-ol with POCl3 afforded the corresponding chloroheterocycles, which were condensed with the appropriate N,N-dialkylalkylenediamine or Na,Na-diethyl-6-methoxytoluene-α,3-diamine to give various 4-[[(dialkylamino)-alkyl]amino]-2-methylpyrimido[1,2-a]benzimidazoles, 11-[[(dialkylamino)alkyl]amino]-2,3-dihydro-1H-cyclopenta[4,5]pyrimido[1,2-a] benzimidazoles and 7-[[(dialkylamino)alkyl]-amino]-5-methyl-s-triazolo[1,5-a]pyrimidines. None of these compounds displayed significant antimalarial activity against Plasmodium berghei in the mouse.

Journal of Heterocyclic Chemistry published new progress about Drugs. 24415-66-5 belongs to class triazoles, name is 7-Chloro-5-methyl-[1,2,4]triazolo[1,5-a]pyrimidine, and the molecular formula is C6H5ClN4, Synthetic Route of 24415-66-5.

Referemce:
1,2,3-Triazole – Wikipedia,
Triazoles – an overview | ScienceDirect Topics