Moran, Daniel B.’s team published research in Journal of Heterocyclic Chemistry in 1986-08-31 | CAS: 108281-78-3

Journal of Heterocyclic Chemistry published new progress about pyridinylpyridinone chlorination; chloropyridine condensation hydrazine; hydrazinopyridine orthoformate cyclization; triazolopyridine pyridinyl. 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, Recommanded Product: 6-Bromo-3-methyl-[1,2,4]triazolo[4,3-a]pyridine.

Moran, Daniel B. published the artcileSynthesis of (pyridinyl)-1,2,4-triazolo[4,3-a]pyridines, Recommanded Product: 6-Bromo-3-methyl-[1,2,4]triazolo[4,3-a]pyridine, the main research area is pyridinylpyridinone chlorination; chloropyridine condensation hydrazine; hydrazinopyridine orthoformate cyclization; triazolopyridine pyridinyl.

The principal route for the synthesis of pyridinyltriazolopyridines I (R = H, Me) was based upon the intermediate 2-chloropyridines II (R1 = Cl), which were prepared by the chlorination of pyridinylpyridinones. Direct chlorination of N-oxides III with POCl3 gave chloro-substituted mixtures, whereas rearrangement of III with Ac2O followed by chlorination gave exclusively II (R1 = Cl). Condensation of II with N2H4 gave II(R1 = NHNH2), which were cyclized with RC(OEt)3 to give I.

Journal of Heterocyclic Chemistry published new progress about pyridinylpyridinone chlorination; chloropyridine condensation hydrazine; hydrazinopyridine orthoformate cyclization; triazolopyridine pyridinyl. 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, Recommanded Product: 6-Bromo-3-methyl-[1,2,4]triazolo[4,3-a]pyridine.

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

Phelan, James P.’s team published research in Chemical Science in 2018 | CAS: 108281-78-3

Chemical Science published new progress about Addition reaction. 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, Product Details of C7H6BrN3.

Phelan, James P. published the artcileRapid access to diverse, trifluoromethyl-substituted alkenes using complementary strategies, Product Details of C7H6BrN3, the main research area is trifluoromethyl alkene preparation; silyl alc trifluoromethyl cross coupling palladium; Peterson elimination; organotrifluoroborate cross coupling palladium.

Two synergistic approaches to the facile assembly of complex α-trifluoromethyl alkenes are described. Using α-trifluoromethyl-β-silyl alcs. as masked trifluoromethyl alkenes, cross-coupling or related functionalization processes at distal electrophilic sites can be executed without inducing Peterson elimination. Subsequent Lewis acidic activation affords functionalized α-trifluoromethyl alkenes. Likewise, the development of a novel α-trifluoromethylvinyl trifluoroborate reagent complements this approach and allows a one-step cross-coupling of (hetero)aryl halides to access a broad array of complex α-trifluoromethyl alkenes.

Chemical Science published new progress about Addition reaction. 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, Product Details of C7H6BrN3.

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

Engers, Darren W.’s team published research in Bioorganic & Medicinal Chemistry Letters in 2018-08-15 | CAS: 108281-78-3

Bioorganic & Medicinal Chemistry Letters published new progress about Antiparkinsonian agents. 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, Computed Properties of 108281-78-3.

Engers, Darren W. published the artcileDiscovery and characterization of N-(1,3-dialkyl-1H-indazol-6-yl)-1H-pyrazolo[4,3-b]pyridin-3-amine scaffold as mGlu4 positive allosteric modulators that mitigate CYP1A2 induction liability, Computed Properties of 108281-78-3, the main research area is preparation dialkylindazolyl pyrazolopyridin amine derivative Parkinson’s; CYP induction; Parkinson’s disease; Positive allosteric modulator; Structure-activity relationship; mGlu4 PAM.

Previous reports from our laboratory disclosed the structure and activity of a novel 1H-pyrazolo[4,3-b]pyridine-3-amine scaffold (VU8506) which showed excellent potency, selectivity and in vivo efficacy in preclin. rodent models of Parkinson’s disease. Unfortunately, this compound suffered from significant CYP1A2 induction as measured through upstream AhR activation (125-fold) and thus was precluded from further advancement in chronic studies. Herein, we report a new scaffold developed recently which was systematically studied in order to mitigate the CYP1A2 liabilities presented in the earlier scaffolds. We have identified a novel structure that maintains the potency and selectivity of other mGlu4 PAMs, leading to 9i (hmGlu4 EC50 = 43 nM; AhR activation = 2.3-fold).

Bioorganic & Medicinal Chemistry Letters published new progress about Antiparkinsonian agents. 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, Computed Properties of 108281-78-3.

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

Temple, Kayla J.’s team published research in Bioorganic & Medicinal Chemistry Letters in 2020-02-01 | CAS: 108281-78-3

Bioorganic & Medicinal Chemistry Letters published new progress about Molecular structure-property relationship. 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, Product Details of C7H6BrN3.

Temple, Kayla J. published the artcileDiscovery of a novel 2,3-dimethylimidazo[1,2-a]pyrazine-6-carboxamide M4 positive allosteric modulator (PAM) chemotype, Product Details of C7H6BrN3, the main research area is dimethylimidazopyrazinecarboxamide preparation M4 pos allosteric modulator; M(4); Muscarinic acetylcholine receptor; Positive allosteric modulator (PAM); Structure activity relationship (SAR).

This Letter details the authors’ efforts to discover structurally unique M4 PAMs containing 5,6-heteroaryl ring systems. In an attempt to improve the DMPK profiles of the 2,3-dimethyl-2H-indazole-5-carboxamide and 1-methyl-1H-benzo[d][1,2,3]triazole-6-carboxamide cores, the authors studied a plethora of core replacements. This exercise identified a novel 2,3-dimethylimidazo[1,2-a]pyrazine-6-carboxamide core that provided improved M4 PAM activity and CNS penetration.

Bioorganic & Medicinal Chemistry Letters published new progress about Molecular structure-property relationship. 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, Product Details of C7H6BrN3.

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

Larson, Helen’s team published research in Journal of Organic Chemistry in 2019-10-18 | CAS: 108281-78-3

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.

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