21434-16-2

Upstream product

• 59-88-1 phenylhydrazine hydrochloride 
• 298-12-4 Glyoxilic acid 
• 290-87-9 1,3,5-Triazine 
• 100-63-0 phenylhydrazine 
• 50705-98-1 (2E)-2-(2-phenylhydrazin-1-ylidene)acetic acid 
• 28740-63-8 5-methyl-3-phenyl-1,3,4-oxadiazol-2(3H)-one 
• 77287-34-4 formamide 
• 6000-60-8 phenylhydrazonoacetic acid 
• 622-84-4 2-formyl-1-phenylhydrazine 
• 463-72-9 carbamic chloride 
• 64-18-6 formic acid 
• 39538-93-7 2-phenylsemicarbazide 

Downstream Products

• 155431-94-0 2-[(1R,2S)-2-(2,4-difluorophenyl)-2,3-epoxy-1-methylpropyl]-4-[4-(2,2,2-trifluoroethoxy)phenyl]-3(2H,4H)-1,2,4-triazolone 

Relevant academic research and scientific papers

Cu microcrystals garnished with copper nanoparticles catalyzed one-pot facile synthesis of novel 1,2,3-triazoles via click chemistry as antifungal agents

A remarkable, efficacious, and environmental friendly one-pot procedure affianced for the synthesis of 1,2,3-triazoles by 1,3-dipolar cycloaddition of aromatic azides, terminal alkynes over Cu microcrystals (CuMCs) by click chemistry as subsequent way. The predominance of this method is green synthetic pathway, transient reaction times, facile workup, exceptional yields (87% to 90%) with excellent purity, regioselective single product formation, and eco-friendliness of the CuMCs catalyst. Docking studies manifested strong binding interactions with enzyme sterol 14-alpha-demethylase (PDB ID: 3KHM) with excellent C-score values. The antifungal screening of synthesized compounds revealed promising activity.

GPR139 RECEPTOR MODULATORS

Compounds are provided that modulate the GPR139 receptor, compositions containing the same, and to methods of their preparation and use for treatment of a malcondition wherein modulation of the GPR139 receptor is medically indicated or beneficial. Such compounds have the structure of Formula (I): or a pharmaceutically acceptable isomer, racemate, hydrate, solvate, isotope, or salt thereof, wherein R1, R4, R5, R9, R10, Q6, Q7, and Q12 are as defined herein.

Microwave assisted regioselective synthesis of quinoline appended triazoles as potent anti-tubercular and antifungal agents via copper (I) catalyzed cycloaddition

Quinolin-3-yl-methyl-1,2,3-triazolyl-1,2,4-triazol-3(4H)-ones 8j-v were synthesized by click chemistry as an ultimate tactic where [3 + 2] cycloaddition of azides with terminal alkynes has been evolved. Herein, we are inclined to divulge the implication and prevalence of CuSO4·5H2O and THF/water promoted [3 + 2] cycloaddition reactions. The foremost supremacy of this method are transitory reaction times, facile workup, excellent yields (88–92%) with exorbitant purity and regioselective single product formation both under conventional and microwave method. Docking studies illustrated strong binding interactions with enzyme InhA-D148G (PDB ID: 4DQU) by means of high C-score values. The anti-tubercular and antifungal screening of synthesized compounds proclaimed promising activity. The in vitro and in silico studies imply that these triazoles appended quinolines may acquire the ideal structural prerequisites for auxiliary expansion of novel therapeutic agents.

Click chemistry based regioselective one-pot synthesis of coumarin-3-yl-methyl-1,2,3-triazolyl-1,2,4-triazol-3(4H)-ones as newer potent antitubercular agents

Coumarin-3-yl-methyl-1,2,3-triazolyl-1,2,4-triazol-3(4H)-ones (8k-z) were synthesized via copper(I)-catalyzed azide-alkyne cycloaddition click chemistry. The synthesized hybrid molecules were characterized by spectral studies. Compounds 8k-z were screened for their in vitro anti-TB activity by using the Microplate Alamar Blue assay and for cytotoxicity using the MTT assay. Some of the compounds were found to be most potent against the tested Mycobacterium tuberculosis H37Rv strain with a MIC of 1.60 μg/ml. Further, docking the compounds into the InhA binding pocket showed strong binding interactions and effective overall docking scores were recorded. The drug-likeness and toxicity studies were computed using Molinspiration and Protox, respectively.

Design, synthesis, docking and in vitro antifungal study of 1,2,4-Triazole hybrids of 2-(aryloxy)quinolines

Substituted quinolines containing a 1,2,4-Triazole moiety were synthesized using reported methods. The molecular docking studies support the experimental results that these compounds are active against A. fumigatus and C. albicans where N-myristoyl transf

C5-Alkyl-1,3,4-Oxadiazol-2-ones Undergo Dealkylation upon Nitrogen Insertion to Form 2H-1,2,4-Triazol-3-ones: Synthesis of 1,2,4-Triazol-3-one Hybrids with Triazolothiadiazoles and Triazolothiadiazines

The present study emphasizes on the dealklylation of 3-aryl-5-alkyl-2-oxo-Δ4-1,3,4-oxadiazoles when reacted with formamide resulting in the formation of 2-aryl-2H-1,2,4-triazol-3(4H)-ones as major product. Subsequent reactions of 2-aryl-2H-1,2,

Studies on the reaction of α-chloroformylarylhydrazine hydrochloride1 with N-heterocyclic compounds

In addition to pyridines, α-chloroformylarylhydrazine hydrochloride 1 can also react with some N-heterocyclic compounds. The cycloaddition of 1 with isoquinoline was achieved to obtain 3. The production of 4, 5, 6 given by cycloaddition of 1 with pyridazine was dependent on the reaction condition. Some heterocyclic compounds bearing an X-C=N (X:S, N) group on the ring can react with 1 to gain the derivatives of 2,4-dihydro-1,2,4-triazol-3-one. 7, 8, 9 and 10 were given by reaction of 1 with 1,3,5-triazine, 1,4,5,6- tetrahydropyrimidine, 1,3-thiazole and 2-amino-1,3-thiazole, respectively. The reactions for 2-amino-1,3,4-thiadiazole and 3-amino-1,2,4-triazole had the same product 11.

1-Substituted 4-carbamoyl-1,2,4-triazol-5-one derivatives and herbicide

A 1-phenyl, naphthyl or aralkyl-4-(N,N-di-substituted carbamoyl)-1,2,4-triazol-5-one derivative represented by the general formula (I) STR1 wherein A is an unsubstituted or substituted phenyl group, 1-naphthyl group, 5,6,7,8-tetrahydro-1-naphthyl group or

A CONVENIENT SYNTHESIS OF 1-ARYL-Δ2-1,2,4-TRIAZOLIN-5-ONES FROM ARYLHYDRAZINES

1-Aryl-1,2,4-triazolin-5-ones are prepared from arylhydrazones of α-keto acids by treatment with diphenylphosphoryl azide.