Category: 174456-28-1

Hoang, Van-Hai published the artcileDiscovery of Potent Human Glutaminyl Cyclase Inhibitors as Anti-Alzheimer’s Agents Based on Rational Design, Related Products of pyrimidines, the publication is Journal of Medicinal Chemistry (2017), 60(6), 2573-2590, database is CAplus and MEDLINE.

Glutaminyl cyclase (QC) has been implicated in the formation of toxic amyloid plaques by generating the N-terminal pyroglutamate of β-amyloid peptides (pGlu-Aβ) and thus may participate in the pathogenesis of Alzheimer’s disease (AD). The authors designed a library of glutamyl cyclase (QC) inhibitors based on the proposed binding mode of the preferred substrate, Aβ_3E-42. An in vitro structure-activity relationship study identified several excellent QC inhibitors demonstrating 5- to 40-fold increases in potency compared to a known QC inhibitor. When tested in mouse models of AD, compound 212 (I) significantly reduced the brain concentrations of pyroform Aβ and total Aβ and restored cognitive functions. This potent Aβ-lowering effect was achieved by incorporating an addnl. binding region into the authors’ previously established pharmacophoric model, resulting in strong interactions with the carboxylate group of Glu 327 in the QC binding site. The authors’ study offers useful insights in designing novel QC inhibitors as a potential treatment option for AD.

Journal of Medicinal Chemistry published new progress about 174456-28-1. 174456-28-1 belongs to pyrimidines, auxiliary class Pyrimidine,Alkynyl,Alcohol, name is 3-(Pyrimidin-5-yl)prop-2-yn-1-ol, and the molecular formula is C7H6N2O, Related Products of pyrimidines.

Referemce:
https://pubchem.ncbi.nlm.nih.gov/compound/Pyrimidine,
Pyrimidine – Wikipedia

Liu, Mingyu published the artcileAtom-Economical Cross-Coupling of Internal and Terminal Alkynes to Access 1,3-Enynes, Quality Control of 174456-28-1, the publication is Journal of the American Chemical Society (2021), 143(10), 3881-3888, database is CAplus and MEDLINE.

Herein, a selective and catalytic method for synthesizing 1,3-enynes (E/Z)-RCCC(R¹)=CHR² (R = tris(propan-2-yl)silyl, 4-(acetyloxy)butyl, cyclohexylmethyl, 5-(1,3-dioxo-2,3-dihydro-1H-isoindol-2-yl)pentyl, etc.; R¹ = Et, Ph, pyridin-3-yl, pyrimidin-5-yl, etc.; R² = hydroxymethyl, (phenylformamido)methyl, [(1H-indol-5-yl)carbamoyl]methyl, etc.) without prefunctionalized building blocks was described. This method is facilitated by a tailored P,N-ligand that enables regioselective dimerization and suppresses secondary E/Z-isomerization of the product. The transformation enables several classes of unactivated internal acceptor alkynes R¹CCR² to be coupled with terminal donor alkynes RCCH to deliver 1,3-enynes in a highly regio- and stereoselective manner. The scope of compatible acceptor alkynes includes propargyl alcs., (homo)propargyl amine derivatives, and (homo)propargyl carboxamides. The reaction is scalable and can operate effectively with as low as 0.5 mol% catalyst loading. The products are versatile intermediates that can participate in various downstream transformations. The preliminary mechanistic experiments that are consistent with a redox-neutral Pd(II) catalytic cycle were also presented.

Journal of the American Chemical Society published new progress about 174456-28-1. 174456-28-1 belongs to pyrimidines, auxiliary class Pyrimidine,Alkynyl,Alcohol, name is 3-(Pyrimidin-5-yl)prop-2-yn-1-ol, and the molecular formula is C7H6N2O, Quality Control of 174456-28-1.

Referemce:
https://pubchem.ncbi.nlm.nih.gov/compound/Pyrimidine,
Pyrimidine – Wikipedia

Firouzeh, Ebrahim published the artcileVisible photosensitized sonogashira-hagihara coupling through in situ prepared palladium catalyst in N,N-dimethylformamide under copper and amine-free additives, Application In Synthesis of 174456-28-1, the publication is Journal of Photochemistry and Photobiology, A: Chemistry (2022), 114002, database is CAplus.

In this study, copper and amine-free photosensitized Sonogashira-Hagihara coupling reaction using Pd(OAc)₂ and p-nitrobenzophenone in N,N-dimethylformamide(DMF) under blue LED irradiation was reported. Effect of benzophenone, p-methoxybenzophenone and p-nitrobenzophenone as photosensitizers in Sonogashira-Hagihara reaction were studied in which higher yields were achieved using p-nitrobenzophenone. In situ preparation of palladium nanoparticles and the effect of p-nitrobenzophenone were confirmed using UV-Vis and dynamic light scattering (DLS). It was proposed that the DMF affected the formation and stabilization of palladium nanoparticles. Using this catalytic system, aryl iodides and bromides were reacted efficiently with alkynes between 25 and 60°C.

Journal of Photochemistry and Photobiology, A: Chemistry published new progress about 174456-28-1. 174456-28-1 belongs to pyrimidines, auxiliary class Pyrimidine,Alkynyl,Alcohol, name is 3-(Pyrimidin-5-yl)prop-2-yn-1-ol, and the molecular formula is C7H6N2O, Application In Synthesis of 174456-28-1.

Referemce:
https://pubchem.ncbi.nlm.nih.gov/compound/Pyrimidine,
Pyrimidine – Wikipedia