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Usage

Uses

Used in Pharmaceutical Industry:
4-Quinolinecarboxaldehyde, 6-broMois used as an intermediate in the synthesis of various pharmaceuticals. Its unique reactivity and selectivity make it a valuable building block for the development of new drugs and medicinal compounds.
Used in Agrochemical Industry:
4-Quinolinecarboxaldehyde, 6-broMois also utilized as an intermediate in the synthesis of agrochemicals, contributing to the development of new pesticides and other agricultural products.
Used in Organic Synthesis:
4-Quinolinecarboxaldehyde, 6-broMoserves as a building block for the production of various heterocyclic compounds in organic synthesis, enabling the creation of a wide range of organic compounds with diverse applications.
Used in Research Laboratories:
It is commonly used in research laboratories for the synthesis and study of quinoline-based compounds, as well as for exploring new chemical reactions and applications.

Upstream product

• 106-40-1 4-bromo-aniline 
• 41037-28-9 6-bromo-4-methylquinoline 

Relevant academic research and scientific papers

Metal-Free Chemoselective Oxidation of 4-Methylquinolines into Quinoline-4-Carbaldehydes

A convenient protocol for the synthesis of quinoline-4-carbaldehydes via chemoselective oxidation of 4-methylquinolines using hypervalent iodine(III) reagents as oxidant is described. This method highlights metal-free and mild reaction conditions, nice yield, good functional group tolerance, and high chemoselectivity.

Structural optimization towards promising β-methyl-4-acrylamido quinoline derivatives as PI3K/mTOR dual inhibitors for anti-cancer therapy: The in vitro and in vivo biological evaluation

Built upon the 4-acrylamido quinoline derivative 4, a previously discovered PI3K/mTOR dual inhibitor, structural modification was undertaken in this study with the attempt to improve its oral exposure via introducing steric hindrance to the 4-acrylamido functionality. Consequently, 14d, as the representative among the synthesized compounds, exhibited IC50 values of 0.80, 0.67, 1.30, 1.30 and 5.0 nM against PI3Kα, PI3Kβ, PI3Kγ, PI3Kδ and mTOR, respectively. Besides, 14d displayed comparable anti-proliferative activity against both PC3 and U87MG cell lines to that of the positive reference GSK2126458 with respective GI50 value of 0.36 and 0.14 μM. Kinase selectivity assay showed that 14d was selective to PI3K family. In U87MG cells, 14d can strongly down-regulate PI3K/Akt/mTOR pathway via blocking both PI3K and mTOR signaling at the concentration as low as 25 nM. Importantly, following a PO dose of 5 mg/kg in male SD rats, 14d displayed favorable oral exposure (AUC0-t = 1336.16 h × ng/mL, AUC0-∞ = 1447.63 h × ng/mL) and high maximum plasma concentration (Cmax = 903.00 ng/mL). In a U87MG glioblastoma xenograft model, tumor growth inhibition of 93.5% and tumor regression were observed at PO dose of 30 and 60 mg/kg, respectively. Meanwhile, no overt loss of body weight was observed in the 14d-treated groups. Taken together, 14d, by virtue of its attractive performance, merits further development as a potential anti-tumor candidate.

1,2,4-TRIAZINE-3-AMINE DERIVATIVE, PREPARATION METHOD THEREFOR, AND USE THEREOF IN MEDICINE

The present invention relates to a 1,2,4-triazine-3-amine derivative, a preparation therefor, and use thereof in medicine. Specifically, the present invention relates to a 1,2,4-triazine-3-amine derivative as represented by general formula (I), a preparation method therefor, a pharmaceutical composition comprising the derivative, and use thereof as a therapeutic agent, in particular as an A2a receptor antagonist, and use thereof in the preparation of a medicament for treating a condition or disorder that is ameliorated by means of inhibition of the A2a receptor, each substituent in general formula (I) being same as defined in the description.

Transition-Metal-Free Oxidation of Benzylic C-H Bonds of Six-Membered N-Heteroaromatic Compounds

A novel oxidation of benzylic C-H bonds for the synthesis of diverse six-membered N-heteroaromatic aldehydes and ketones has been developed. The obvious advantages of this approach are the simple operation, mild reaction conditions, and without use of toxic reagent and transition metal. The present method should provide a useful access for the synthesis and modification of N-heterocycles.