1001401-62-2

Usage

Uses

Used in Pharmaceutical and Agrochemical Industries:
Benzoic acid, 2-(2H-1,2,3-triazol-2-yl)is used as an intermediate in the synthesis of various pharmaceuticals and agrochemicals, contributing to the development of new drugs and pesticides.
Used in Organic Compounds Synthesis:
Benzoic acid, 2-(2H-1,2,3... is utilized as a building block in the creation of organic compounds with anti-fungal and anti-inflammatory properties, enhancing the range of treatments available for various conditions.
Used in Photoactive Materials Synthesis:
Benzoic acid, 2-(2H-1,2,3-triazol-2-yl)is employed in the synthesis of photoactive materials, which have applications in various fields such as solar energy conversion and light-emitting devices.
Used in Polymer Cross-linking:
It is used as a cross-linking agent for polymers, improving the mechanical properties and thermal stability of polymeric materials in different industries.

Upstream product

• 88-67-5 2-Iodobenzoic acid 
• 288-36-8 1 ,2,3-Triazole 
• 288-36-8 1,2,3-triazole 
• 1192847-33-8 4,5-dibromo-2-(2-nitrophenyl)-2H-1,2,3-triazole 
• 124-38-9 carbon dioxide 
• 1173462-33-3 2-(1,2,3-triazol-2-yl)-phenylamine 

Downstream Products

• 1192159-68-4 2-(2Η-1,2,3-triazol-2-yl)benzoyl chloride 
• 1001401-72-4 tert-butyl (S)-3-methyl-4-(2-(2H-1,2,3-triazol-2-yl)benzoyl)-1,4-diazepane-1-carboxylate 
• 1030377-28-6 benzyl (5R)-5-methyl-4-[2-(2H-1,2,3-triazol-2-yl)benzoyl]-1,4-diazepane-1-carboxylate 
• 1085458-32-7 3-(6-fluoroquinazolin-2-yl)-10-[2-(2H-1,2,3-triazol-2-yl)benzoyl]-8-oxa-3,10-diazabicyclo[4.3.1]decane 
• 1085458-70-3 C₁₆H₁₉N₅O₂ 
• 1085458-68-9 tert-butyl 10-[2-(2H-1,2,3-triazol-2-yl)benzoyl]-8-oxa-3,10-diazabicyclo[4.3.1]decane-3-carboxylate 
• 1410041-98-3 N-{2-[1-(tetrahydro-2H-pyran-2-yl)-1H-pyrazol-3-yl]ethyl}-2-(2H-1,2,3-triazol-2-yl)benzamide 
• 1410039-03-0 N-ethyl-N-{2-[1-(5-fluoropyridin-2-yl)-1H-pyrazol-3-yl]ethyl}-2-(2H-1,2,3-triazol-2-yl)benzamide 
• 1381971-26-1 N-ethyl-N-{2-[3-(5-fluoropyridin-2-yl)-1H-pyrazol-1-yl]ethyl}-2-(2H-1,2,3-triazol-2-yl)benzamide 
• 1431472-54-6 2-{[(3R,6R)-6-methyl-1-{[2-(2H-1,2,3-triazol-2-yl)phenyl]carbonyl}piperidin-3-yl]oxy}pyridine-4-carbonitrile 

Relevant academic research and scientific papers

Monoacylglycerol Lipase Modulators

Bridged compounds of Formula (I) and Formula (II), pharmaceutical compositions containing them, methods of making them, and methods of using them including methods for treating disease states, disorders, and conditions associated with MGL modulation, such as those associated with pain, psychiatric disorders, neurological disorders (including, but not limited to major depressive disorder, treatment resistant depression, anxious depression, bipolar disorder), cancers and eye conditions. wherein R2, R3 R4, R5 and R6 are defined herein.

Monoacylglycerol Lipase Modulators

Fused compounds of Formula (I) and Formula (II), pharmaceutical compositions containing them, methods of making them, and methods of using them including methods for treating disease states, disorders, and conditions associated with MGL modulation, such as those associated with pain, psychiatric disorders, neurological disorders (including, but not limited to major depressive disorder, treatment resistant depression, anxious depression, bipolar disorder), cancers and eye conditions. Wherein R1, R2, R2a, R3, R3a, R4, and R4a are defined herein.

From Oxadiazole to Triazole Analogues: Optimization toward a Dual Orexin Receptor Antagonist with Improved in vivo Efficacy in Dogs

The orexin system is responsible for regulating the sleep-wake cycle. Suvorexant, a dual orexin receptor antagonist (DORA) is approved by the FDA for the treatment of insomnia disorders. Herein, we report the optimization efforts toward a DORA, where our starting point was (5-methoxy-4-methyl-2-[1,2,3]triazol-2-yl-phenyl)-{(S)-2-[5-(2-trifluoromethoxy-phenyl)-[1,2,4]oxadiazol-3-yl]-pyrrolidin-1-yl}methanone (6), a compound which emerged from our in-house research program. Compound 6 was shown to be a potent, brain-penetrating DORA with in vivo efficacy similar to suvorexant in rats. However, shortcomings from low metabolic stability, high plasma protein binding (PPB), low brain free fraction (fu brain), and low aqueous solubility, were identified and hence, compound 6 was not an ideal candidate for further development. Our optimization efforts addressing the above-mentioned shortcomings resulted in the identification of (4-chloro-2-[1,2,3]triazol-2-yl-phenyl)-{(S)-2-methyl-2-[5-(2-trifluoromethoxy-phenyl)-4H-[1,2,4]triazol-3-yl]-pyrrolidin-1-yl}l-methanone (42), a DORA with improved in vivo efficacy compared to 6.

Oxadiazole Derivatives as Dual Orexin Receptor Antagonists: Synthesis, Structure–Activity Relationships, and Sleep-Promoting Properties in Rats

The orexin system plays an important role in the regulation of wakefulness. Suvorexant, a dual orexin receptor antagonist (DORA) is approved for the treatment of primary insomnia. Herein, we outline our optimization efforts toward a novel DORA. We started our investigation with rac-[3-(5-chloro-benzooxazol-2-ylamino)piperidin-1-yl]-(5-methyl-2-[1,2,3]triazol-2-ylphenyl)methanone (3), a structural hybrid of suvorexant and a piperidine-containing DORA. During the optimization, we resolved liabilities such as chemical instability, CYP3A4 inhibition, and low brain penetration potential. Furthermore, structural modification of the piperidine scaffold was essential to improve potency at the orexin 2 receptor. This work led to the identification of (5-methoxy-4-methyl-2-[1,2,3]triazol-2-ylphenyl)-{(S)-2-[5-(2-trifluoromethoxyphenyl)-[1,2,4]oxadiazol-3-yl]pyrrolidin-1-yl}methanone (51), a potent, brain-penetrating DORA with in vivo efficacy similar to that of suvorexant in rats.

Highly Selective Synthesis of 2-(2 H-1,2,3-Triazol-2-yl)benzoic Acids

A selective and scalable synthesis of 2-(2H-1,2,3-triazol-2-yl)benzoic acid starting from 1-fluoro-2-nitrobenzene derivatives is presented. The four-step synthesis introduces the triazole at the start via N2-arylation of 4,5-dibromo-2H-1,2,3-triazole. A sequence of consecutive functional group transformations, namely hydrogenation, Sandmeyer iodination, and Grignard carboxylation, provides the target molecules in a reliable and scalable manner. The usefulness of this method is demonstrated by the synthesis of di-or tri(2H-1,2,3-triazol-2-yl)benzene derivatives, which are difficult to produce by other methods.

Highly selective synthesis of 2-(2H-1,2,3-Triazol-2-yl)benzoic acids

A selective and scalable synthesis of 2-(2H-1,2,3-triazol-2-yl)benzoic acid starting from 1-fluoro-2-nitrobenzene derivatives is presented. The four-step synthesis introduces the triazole at the start via N2-arylation of 4,5-dibromo-2H-1,2,3- triazole. A sequence of consecutive functional group transformations, namely hydrogenation, Sandmeyer iodination, and Grignard carboxylation, provides the target molecules in a reliable and scalable manner. The usefulness of this method is demonstrated by the synthesis of di- or tri(2H-1,2,3-triazol-2-yl)benzene derivatives, which are difficult to produce by other methods.

Octahydropyrrolo[3,4-c]pyrrole derivative and application method and application thereof

The invention relates to an octahydropyrrolo[3,4-c]pyrrole derivative and an application method and application thereof. The compound and a pharmaceutical composition containing the compound are usedfor antagonizing orexin receptors. The invention also re

Octahydropyrrolo[3,4-c]pyrrole derivatives and use thereof

The invention relates to octahydropyrrolo[3,4-c]pyrrole derivatives and a use thereof. The above compounds and a medicinal composition containing the compounds are used for suppressing an orexin receptor. The invention also relates to a method for preparing the compounds and the medicinal composition, and the use of the compounds and the medicinal composition in the treatment or prevention of orexin receptor related diseases.

Heterocyclic Compound

The present invention provide a compound having an orexin receptor antagonistic activity, which is expected to be useful as medicaments such as agents for the prophylaxis or treatment of sleep disorder, depression, anxiety disorder, panic disorder, schizophrenia, drug dependence, Alzheimer's disease and the like. The present invention relates to a compound represented by the formula (I): wherein each symbol is as defined in the specification, or a salt thereof.

SUBSTITUTED QUINAZOLINE COMPOUNDS AND PREPARATION AND USES THEREOF

The present invention relates quinazolinone compounds of Formula (I), as well as their preparation and uses, and further relates pharmaceutical compositions comprising these compounds and their uses； wherein the compounds or pharmaceutical compositions disclosed herein can be used for antagonizing the orexin receptor. The present invention also relates to uses of the compounds or pharmaceutical compositions in treating or preventing neurological and psychiatric disorders and diseases of the central nervous system in mammals, especially in humans.