Day: November 10, 2022

Silveira, Flavia F. published the artcileComparative study between the anti-P. falciparum activity of triazolopyrimidine, pyrazolopyrimidine and quinoline derivatives and the identification of new PfDHODH inhibitors, Recommanded Product: 7-Chloro-5-methyl-[1,2,4]triazolo[1,5-a]pyrimidine, the main research area is triazolopyrimidine derivative preparation antimalarial PfDHODH inhibitor; pyrazolopyrimidine derivative preparation antimalarial PfDHODH inhibitor; quinoline derivative preparation antimalarial PfDHODH inhibitor; Malaria; P. falciparum; PfDHODH; Pyrazolopyrimidine; Quinoline; Triazolopyrimidine.

Three series of triazolopyrimidine I [R = H, Me, CF3; R1 = Ph, 4-MeC6H4, 4-ClC6H4, etc.], pyrazolopyrimidine II [R2 = Ph, 4-MeOC6H4, 4-FC6H4, etc.] and quinoline derivatives III [R3 = Ph, 2-naphthyl, 4-ClC6H4, etc.] as P. falciparum inhibitors (3D7 strain) was reported. Some of the compounds of I, II and III exhibited anti-P. falciparum activity, with IC50 values ranging from 0.030 to 9.1μM. Compounds I were more potent than the compounds II and III. Compounds I [R = CF3; R1 = 2-naphthyl, 4-MeC6H4, 4-FC6H4, 4-F3CC6H4] were the most potent inhibitors, with IC50 values in the range of 0.030-0.086μM and were equipotent to chloroquine. In addition, the compounds were selective, showed no cytotoxic activity against the human hepatoma cell line HepG2. All compounds I inhibited PfDHODH activity in the low micromolar to low nanomolar range (IC50 values of 0.08-1.3μM) and did not show significant inhibition against the HsDHODH homolog (0-30% at 50μM). Mol. docking studies indicated the binding mode of compounds I to PfDHODH and the highest interaction affinities for the PfDHODH enzyme were in agreement with the in vitro exptl. evaluation. Thus, the most active compounds against P. falciparum parasites I [R = CF3; R1 = 4-MeC6H4, 4-FC6H4, 4-F3CC6H4, 2-naphthyl] (IC50 = 0.086μM, 0.032μM, 0.030μM, 0.050μM, resp.) and the most active inhibitor against PfDHODH I [R = CF3; R1 = 4-ClC6H4] (IC50 = 0.08μM – PfDHODH) stood out as new lead compounds for antimalarial drug discovery. Their potent in vitro activity against P. falciparum and the selective inhibition of the PfDHODH enzyme strongly suggested that this was the mechanism of action underlying this series of compounds I.

European Journal of Medicinal Chemistry published new progress about Acids Role: RCT (Reactant), RACT (Reactant or Reagent). 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, Recommanded Product: 7-Chloro-5-methyl-[1,2,4]triazolo[1,5-a]pyrimidine.

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

Himaja, M. published the artcileSynthesis, antibacterial and insecticidal activities of a new series of 4-(5-methyl-1,2,4-triazolo[1,5-a]pyrimidin-7-ylamino)-N-(aryl)benzamides, COA of Formula: C6H5ClN4, the main research area is chlorotriazolopyrimidine aminobenzoic acid amination; triazolopyrimidinylaminobenzoic acid preparation amidation HATU coupling reagent; aryl triazolopyrimidinylaminobenzamide preparation antibacterial insecticidal.

A new series of 4-(5-methyl-1,2,4-triazolo[1,5-a]pyrimidin-7-ylamino)-N-(aryl)benzamides were synthesized by coupling 4-(5-methyl-1,2,4-triazolo[1,5-a]pyrimidin-7-ylamino)benzoic acid with different substituted amines using O-(7-azabenzotriazol-1-yl)-1,1,3,3-tetramethyluronium hexafluorophosphate (HATU) as coupling reagent. The key intermediate 4-(5-methyl-1,2,4-triazolo[1,5-a]pyrimidin-7-ylamino)benzoic acid was synthesized by the reaction of 7-chloro-5-methyl-1,2,4-triazolo[1,5-a]pyrimidine with p-aminobenzoic acid in ethanol. The structure of the newly synthesized compounds were confirmed by FT-IR, 1H NMR, 13C NMR and Mass spectral anal. and were evaluated for their antimicrobial and insecticidal activities. Some of the synthesized compounds exhibited potent insecticidal activity and significant antibacterial activity with respect to the standard drugs.

Indian Journal of Heterocyclic Chemistry published new progress about Amines Role: RCT (Reactant), RACT (Reactant or Reagent). 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, COA of Formula: C6H5ClN4.

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

Matsuda, Yoshiro published the artcileReaction of 4-amino-1,2,4-triazolium salts with polarized olefins, Name: 4-Amino-1-methyl-4H-1,2,4-triazol-1-ium iodide, the main research area is aminotriazolium salt cyclization polarized olefin; triazolium salt amino cyclization polarized olefin; betaine mesomeric preparation; triazolopyrazole preparation.

The reaction of 4-amino-1,2,4-triazolium salts I (R = Me, CH2Ph, X = iodo, Br) with polarized olefins EtOCH:CR1CO2Et (R1 = CO2Et, NO2) and (MeS)2C:CXY (X = CO2Me, Y = cyano) in the presence of K2CO3 in EtOH or DMSO directly yielded the back-donated 1,6-cyclization products, mesomeric betaines II (R1 = CO2Et, NO2, R2 = H; R1 = cyano, R2 = SMe) via N-vinylimino ylides, while the reaction of the salts I with polarized olefins (MeS)2C:CXY (X = H, Y = NO2; X = SO2Ph, Y = cyano) gave the 1,5-dipolar cyclization products, pyrazoles III and [1,2,4]-triazolo[4,3-b]pyrazole IV.

Heterocycles published new progress about Alkenes Role: RCT (Reactant), RACT (Reactant or Reagent). 39602-93-2 belongs to class triazoles, name is 4-Amino-1-methyl-4H-1,2,4-triazol-1-ium iodide, and the molecular formula is C3H7IN4, Name: 4-Amino-1-methyl-4H-1,2,4-triazol-1-ium iodide.

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

Yuan, Shuo published the artcileBronsted acid-promoted ‘on-water’ C(sp3)-H functionalization for the synthesis of isoindolinone/[1,2,4]triazolo[1,5-a]pyrimidine derivatives targeting the SKP2-CKS1 interaction, Name: 7-Chloro-5-methyl-[1,2,4]triazolo[1,5-a]pyrimidine, the main research area is trimethoxyphenyl triazolopyrimidinyl methyl isoindolinone preparation SKP2 CKS1 inhibition SAR.

An efficient Bronsted acid-promoted C(sp3)-H functionalization approach that enabled the rapid construction of biol. important isoindolinone/[1,2,4]triazolo[1,5-a]pyrimidine hybrids from 5-methyl-7-(2,4,6-trimethoxyphenyl)-[1,2,4]triazolo[1,5-a]pyrimidine, 2-formylbenzoic acid and various anilines was reported. The title compounds were generated in high to excellent yields (up to 96%) regardless of the electronic nature and steric effects of the substituents. In this reaction, an isoindolinone scaffold, one C-C single bond and two C-N bonds were formed simultaneously with high atom economy. It was concluded that the Me group linked to the electron-deficient N-heterocycles was used as a new synthetic handle for late-state diversification and may have broad applications in the field of organic and medicinal chem. Besides, the title compounds exhibited promising activity against the SKP2-CKS1 interaction.

Chinese Chemical Letters published new progress about Anilines Role: RCT (Reactant), RACT (Reactant or Reagent). 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, Name: 7-Chloro-5-methyl-[1,2,4]triazolo[1,5-a]pyrimidine.

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

Liu, Luxiao published the artcileDeep eutectic solvent promoted one-pot synthesis of nitriles from alcohols, Category: triazoles, the main research area is aryl nitrile green preparation; alc tandem aerobic oxidation condensation deep eutectic solvent.

Various aryl nitriles RCN [R = Ph, 4-BrC6H4, 2-thienyl, etc.] were readily synthesized from aerobic oxidation of substituted benzyl alcs. in deep eutectic solvent composed of choline chloride and p-toluenesulfonic acid in the presence of 2,2,6,6-tetramethylpiperidine-1-oxyl, followed by condensation with hydroxylamine hydrochloride. High yields of corresponding nitriles had obtained under mild reactions conditions. This strategy belonged to a novel and environmentally benign transition-metal-free one-pot cascade process for the synthesis of nitriles.

Journal of Chemical Sciences (Berlin, Germany) published new progress about 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, Category: triazoles.

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

Hu, Yongke published the artcileDirect oxidative esterification of alcohols catalyzed by a nitrogen-doped carbon black-supported PdBi bimetallic catalyst under ambient conditions, SDS of cas: 143426-50-0, the main research area is PdBi bimetallic catalyzed oxidative esterification alc; aryl ester preparation PdBi bimetallic catalyzed oxidative esterification.

A highly efficient nitrogen-doped carbon black (NCB)-supported PdBi alloy nanocatalyst has been fabricated via a facile coredn. wet chem. approach. The optimal PdBi/NCB shows outstanding catalytic performance with broad substrate scope, good functional group tolerance towards direct oxidative esterification of alcs. under mild conditions in a heterogeneous catalytic system with air as the sole oxidant. A variety of benzylic and allylic alcs. were smoothly reacted with methanol and even with long-chain aliphatic alcs., providing desired esters in good to excellent yields. Moreover, the as-prepared catalyst is easily recycled and can be reused at least five times without a significant loss of catalytic activity. Superior catalytic activity is mainly attributable to the unique structure of the catalyst, including synergetic electronic effect between Pd and Bi, as well as modulated surface character by acidification and N doping for better active components’ anchoring and dispersion, as well as reactants’ adsorption. This study provides a facial, practical, eco-friendly and efficient catalytic system for oxidative esterification of alcs. and shows promising prospect in industrial production

Journal of Materials Science published new progress about 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, SDS of cas: 143426-50-0.

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

Lou, Ji-Cong published the artcileMetal-Free Oxidation of Trichloroacetimidates to Aldehydes, HPLC of Formula: 143426-50-0, the main research area is alc trichloroacetonitrile DBU imidation; trichloroacetimidate preparation dimethylsulfoxide oxidation; carbonyl compound preparation.

A metal-free oxidation reaction of trichloroacetimidates to aldehydes or ketones with DMSO as an oxidant was reported. The reaction exhibited a broad range of functional group tolerance. Detailed mechanistic studies were performed with the aid of NMR, in-situ IR spectroscopy, GC-MS anal. and 18O-labeling experiments

Asian Journal of Organic Chemistry published new progress about 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

Jishkariani, Davit published the artcileCu(I)-Catalyzed Regioselective Synthesis of Pyrazolo[5,1-c]-1,2,4-triazoles, SDS of cas: 39602-93-2, the main research area is terminal alkyne triazolium imide regioselective cycloaddition copper; regioselective preparation; copper regioselective cycloaddition catalyst.

Cycloadditions of terminal alkynes to 1,2,4-triazolium N-imides in the presence of base and Cu(I) afford pyrazolo[5,1-c]-1,2,4-triazoles, e.g., I, regioselectively. The scope of alkynes, the influence of the electronic nature of the leaving group, and variations in the 1-alkyl substituent were examined Quantum chem. calculations were employed to explain the distinct reactivity of the propiolates.

Journal of Organic Chemistry published new progress about Alkynes, α- Role: RCT (Reactant), RACT (Reactant or Reagent). 39602-93-2 belongs to class triazoles, name is 4-Amino-1-methyl-4H-1,2,4-triazol-1-ium iodide, and the molecular formula is C3H7IN4, SDS of cas: 39602-93-2.

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

Larson, Helen published the artcileNi-Catalyzed C-H Arylation of Oxazoles and Benzoxazoles Using Pharmaceutically Relevant Aryl Chlorides and Bromides, Synthetic Route of 108281-78-3, the main research area is nickel catalyst arylation oxazole benzoxazole pharmaceutically relevant aryl halide.

This manuscript details the development of the nickel-catalyzed arylation of oxazoles and benzoxazoles with aryl halides. A series of aryl, heteroaryl, and druglike electrophiles relevant to pharmaceutical applications were surveyed. The desired arylated products were obtained in synthetically useful yields using electronically and structurally varied aryl halides. The use of microscale high-throughput experimentation was essential for both the rapid identification of optimal reaction parameters and the investigation of the aryl halide scope.

Journal of Organic Chemistry published new progress about Aryl bromides Role: RCT (Reactant), RACT (Reactant or Reagent). 108281-78-3 belongs to class triazoles, name is 6-Bromo-3-methyl-[1,2,4]triazolo[4,3-a]pyridine, and the molecular formula is C7H6BrN3, Synthetic Route of 108281-78-3.

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

Panmand, Deepak S. published the artcileSynthesis and Direct C2 Functionalization of Imidazolium and 1,2,4-Triazolium N-Imides, Recommanded Product: 4-Amino-1-methyl-4H-1,2,4-triazol-1-ium iodide, the main research area is aryl imidazolpyrazolole pyrazolotriazole imidazoliumylamide triazoliumylamide preparation fluorescence emission spectra; azoliumimide acetylene aryl iodide arylation alkynylation cyclization.

Pd-catalyzed direct C2 arylation and Cu-catalyzed direct one-pot alkynylation/intramol. cyclization of azolium N-imides are reported. Various acetylenes, aryl iodides, and 1-alkyl substituents were examined The mild protocol allows direct C2 arylation of azolium N-imides without the use of specialized reagents together with novel one-pot regioselective preparations of imidazole-pyrazolo e. g., I, and pyrazolo-1,2,4-triazole e. g., II ring systems. The electronic properties of selected examples were examined by fluorescence spectroscopy.

Journal of Organic Chemistry published new progress about Alkynes, aryl Role: RCT (Reactant), RACT (Reactant or Reagent). 39602-93-2 belongs to class triazoles, name is 4-Amino-1-methyl-4H-1,2,4-triazol-1-ium iodide, and the molecular formula is C3H7IN4, Recommanded Product: 4-Amino-1-methyl-4H-1,2,4-triazol-1-ium iodide.

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