59082-23-4

Upstream product

• 1122-91-4 4-bromo-benzaldehyde 
• 529-34-0 3,4-dihydronaphthalene-1(2H)-one 
• 873-75-6 4-bromobenzenemethanol 

Downstream Products

• 129116-54-7 1-(4-Bromo-phenyl)-3-oxo-1,2,3,9,10,10a-hexahydro-phenanthrene-2-carboxylic acid (4-bromo-phenyl)-amide 
• 128483-27-2 2-Mercapto-4-p-bromophenyl-4H-1,2,3,4,5,6-hexahydrobenzo-quinazoline 

Relevant academic research and scientific papers

A class of 2-benzylene tetrahydronaphthalone derivatives and preparation methods and applications thereof

The present invention relates to the field of biotechnology, discloses a class of 2-benzylene tetrahydrophthalone derivatives and preparation methods and applications thereof. 2-Benzylene tetrahydronaphthalone derivative having the following structural formula, wherein R1 is selected from chlorine, bromine, iodine, alkyl, alkoxy, substituted or unsubstituted amino, alkylthio, alkyneoxy, hydroxy or hydroxymethyl group; R2, R3, R4 are hydrogen or carboxyl-containing substituents, and R2, R3, or R4 At least one of them is a carboxyl-containing substituent group. The present invention innovatively proposes a class of 2-benzylene tetrahydronaphthalone derivatives as a new skeleton of firefly luciferase inhibitors. A class of 2-benzylene tetrahydronaphthone derivatives of the present invention having a highly efficient inhibitor of nanomolar and a nanamol IC50; by competing with D- fluorescein reversibly inhibits firefly luciferase, and exhibits a high effect of firefly glowworm luciferase inhibition at the enzyme, intracellular and in vivo levels; at the same time, it is shown that it has good biocompatibility and application potential.

Copper/GanPhos-Catalyzed 1,3-Dipolar Cycloaddition of Azo?-methine Ylides: An Efficient Access to Chiral Pyrrolidine Spirocycles

A highly efficient copper/GanPhos-catalyzed 1,3-dipolar cyclo?-addition?-of azomethine ylides is reported. This viable transformation provides a series of optically active spiro[dihydronaphthalene-2,3′-pyrrolidine]s, bearing one spiro quaternary and three tertiary stereogenic centers, in good yields and with high ee values. This protocol features high diastereo- A nd enantioselectivity, broad substrate scope and mild reaction conditions.

Tetralone derivatives are MIF tautomerase inhibitors and attenuate macrophage activation and amplify the hypothermic response in endotoxemic mice

Macrophage migration inhibitory factor (MIF) is a pro-inflammatory cytokine playing crucial role in immunity. MIF exerts a unique tautomerase enzymatic activity that has relevance concerning its multiple functions and its small molecule inhibitors have been proven to block its pro-inflammatory effects. Here we demonstrate that some of the E-2-arylmethylene-1-tetralones and their heteroanalogues efficiently bind to MIF’s active site and inhibit MIF tautomeric (enolase, ketolase activity) functions. A small set of the synthesised derivatives, namely compounds (4), (23), (24), (26) and (32), reduced inflammatory macrophage activation. Two of the selected compounds (24) and (26), however, markedly inhibited ROS and nitrite production, NF-κB activation, TNF-α, IL-6 and CCL-2 cytokine expression. Pre-treatment of mice with compound (24) exaggerated the hypothermic response to high dose of bacterial endotoxin. Our experiments suggest that tetralones and their derivatives inhibit MIF’s tautomeric functions and regulate macrophage activation and thermal changes in severe forms of systemic inflammation.

Claisen-Schmidt, aza-Michael, cyclization via cascade strategy toward microwave promoted synthesis of imidazo[2,1-b]quinazolines

Imidazole blended quinazolines are having a wide run of potential applications in synthetic field. In this current investigation, we reported a modern synthesis with the help of non-conventional energy. Optimization parameters have been stabilized utilizi

Novel 1-tetralone chalcone and composition for preventing or treating inflammatory disease comprising the same as active ingredient

Novel 1 -tetralone chalcone derivatives, 1-tetralone alone alone alone alone. A composition containing 6 - amino -1 - tetralone chalcone derivatives and 6-amino-1-tetralone alone alone alone alone is provided to systematically design 32 halogenated 1 -tet

Introduction of amino moiety enhances the inhibitory potency of 1-tetralone chalcone derivatives against LPS-stimulated reactive oxygen species production in RAW 264.7 macrophages

The design and synthesis of a series of thirty-two halogenated 1-tetralone or 6-amino-1-tetralone chalcone derivatives was achieved by the Claisen-Schmidt condensation reaction and were evaluated for their inhibitory effects against ROS production in LPS-stimulated RAW 264.7 macrophages. It was observed that the introduction of amino moiety into 1-tetralone skeleton greatly increased the inhibitory potency compared to corresponding 1-tetralone chalcones. Among the synthesized compounds, compound 18 which consists of 6-amino-1-tetralone skeleton together with o-fluorobenzylidene showed the most potent ROS inhibitory effect with IC50 value of 0.25 ± 0.13 μM. SAR analysis revealed that amino moiety at the 6th position of 1-tetralone chalcones have an important role for exerting the greater ROS inhibitory potency in LPS-stimulated RAW 264.7 macrophages than those exhibited by 1-tetralone chalcones alone.

Basic Anion-Exchange Resin-Catalyzed Aldol Condensation of Aromatic Ketones with Aldehydes in Continuous Flow

A general method for the aldol condensation of aromatic ketones with aldehydes was developed under continuous-flow conditions using a commercially available, strongly basic anion-exchange resin (A26) as catalyst. This procedure, in addition to exhibiting a wide substrate scope, promoted carbon-carbon bond formation under mild conditions using a quasi-stoichiometric ratio of starting reagents with good to excellent yields, thereby forming a limited amount of waste and allowing the process to be applied to sequential-flow systems. A proof of concept was developed in the first fully heterogeneously catalyzed two-step flow synthesis of donepezil, which is a blockbuster commercial anti-Alzheimer's drug.

Manganese(I)-Catalyzed α-Alkenylation of Ketones Using Primary Alcohols

A simple protocol of manganese catalyzed selective α-alkenylation of ketones using primary alcohols is reported. The reactions proceeded well with a low loading of catalyst (0.3 mol %). The overall transformation operates through O-H bond activation of pr

Selectivity in the Aerobic Dearomatization of Phenols: Total Synthesis of Dehydronornuciferine by Chemo- and Regioselective Oxidation

We describe a selective aerobic oxidation of meta-biaryl phenols that enables rapid access to functionalized phenanthrenes. Aerobic oxidations attract interest due to their efficiency, but remain underutilized in complex molecule settings due to challenge

Synthesis, characterization, and investigations of antimicrobial activity of 6,6-dimethyl-3-aryl-3′,4′,6,7-tetrahydro-1′H,3H-spiro[benzofuran-2,2′-naphthalene]-1′,4(5H)-dione

Chalcone-like compounds 3a–l, 2-(benzylidene)-3,4-dihydronaphthalen-1(2H)-one, were synthesized from the addition of different benzaldehyde derivatives (2a–l) to 1,2,3,4-tetrahydro-1-napthalone (1) in basic medium. Mn(OAc)3-mediated addition of