36804-45-2

Upstream product

• 36804-44-1 N-(2-(2-methylbenzoyl)phenyl)acetamide 
• 95-46-5 2-methylphenyl bromide 
• 133776-41-7 anthranilic acid N-methoxy-N-methylamide 
• 15898-37-0 sodium 2-methylbenzenesulfinate 
• 1885-29-6 anthranilic acid nitrile 
• 118-92-3 anthranilic acid 
• 932-31-0 ortho-tolylmagnesium bromide 
• 551-93-9 2-aminoacetophenone 
• 552-89-6 2-nitro-benzaldehyde 
• 16419-60-6 2-Methylphenylboronic acid 
• 118-48-9 isatoic anhydride 
• 525-76-8 2-methyl-4-oxo-3,1-benzoxazine 

Downstream Products

• 5501-37-1 1-methylfluoren-9-one 
• 51974-19-7 (2-hydroxyphenyl)(o-tolyl)methanone 
• 102022-54-8 2-hydroxy-4-o-tolyl-quinoline-3-carboxylic acid ethyl ester 
• 3169-55-9 (2-Methyl-phenyl)-(2-amino-phenyl)-methan 
• 1730-37-6 1-methylfluorene 

Relevant academic research and scientific papers

Novel transformation of aryl 2-iodophenyl ketones into 1,3-diarylisoquinolines with (TMS)2NH, styrenes, NIS, and tBuOK

Treatment of aryl 2-iodophenyl ketones with TMS2NH in the presence of Sc(OTf)3 at warming conditions, followed by the reaction with styrenes and NIS gave N-(1-aryl-2-iodoethyl) aryl 2-iodophenyl ketimines. Further treatment of N-(1-aryl-2-iodoethyl) aryl 2-iodophenyl ketimines with tBuOK in the presence of 1,10-phenanthroline at 120 °C generated 1,3-diarylisoquinolines in moderate yields through SET from tBuOK onto the iodophenyl group to form aryl radicals, their 6-endo-trig cyclization onto the vinyl groups, and aromatization of the cyclized intermediates. The present method is a novel approach for the preparation of the isoquinoline core via two steps from aryl 2-iodophenyl ketones.

Bicyclic Bridgehead Phosphoramidite-Based Hybrid Diphosphorus Ligands: Design, Synthesis, and Application in Catalytic Asymmetric Hydrogenation

A strategy for chiral ligand design has been developed that allows for incorporation of an achiral bicyclic bridgehead phosphoramidite to generate a class of hybrid diphosphorus ligands for high activity and asymmetric control. Using this concept, a series of chiral phosphine-phosphoramidite ligands bearing the sole chirality at the ligand backbone have been prepared and successfully employed in the Rh-catalyzed asymmetric hydrogenation of 2-vinylanilides for the synthesis of optically active anilines bearing an ortho-tertiary benzylic stereocenter.

1, 4-disubstituted 3, 4-dihydro-2 (3H)-quinazolinone compound as well as synthesis method and application thereof

The invention belongs to the field of organic synthesis and medicines, and particularly relates to a 1, 4-disubstituted 3, 4-dihydro-2 (3H)-quinazolinone compound as well as a synthesis method and application thereof. R1 is hydrogen or chlorine, R2 is hydrogen, methyl, methoxyl or fluorine, R3 is nitrophenyl, (2-trifluoromethyl-5-Cl) piperidyl, phenyl, methoxyl phenyl, methyl phenyl, 2-trifluoromethyl phenyl or C2-C8 alkyl or naphthenic base, R4 is hydrogen or methyl, and X is O or S. The compound is a novel compound with a non-peptide structure, has a good inhibitory effect on cancer cells, has a broad-spectrum effect, especially has good inhibitory activity on hepatoma carcinoma cells, and has good market prospects and application prospects.

Deoxygenative Arylation of Carboxylic Acids by Aryl Migration

An unprecedented deoxygenative arylation of aromatic carboxylic acids has been achieved, allowing the construction of an enhanced library of unsymmetrical diaryl ketones. The synergistic photoredox catalysis and phosphoranyl radical chemistry allows for precise cleavage of a stronger C?O bond and formation of a weaker C?C bond by 1,5-aryl migration under mild reaction conditions. This new protocol is independent of substrate redox-potential, electronic, and substituent effects. It affords a general and promising access to 60 examples of synthetically versatile o-amino and o-hydroxy diaryl ketones under redox-neutral conditions. Furthermore, it also brings one concise route to the total synthesis of quinolone alkaloid, (±)-yaequinolone A2, and a viridicatin derivative in satisfying yields.

Organocatalytic Atroposelective Friedl?nder Quinoline Heteroannulation

An atroposelective Friedl?nder heteroannulation reaction of 2-aminoaryl ketones with α-methylene carbonyl derivatives has been developed for the first time with chiral phosphoric acid as an efficient organocatalyst. The desired enantioenriched axially chi

Iron-Promoted Construction of Indoles via Intramolecular Oxidative C-N Coupling of 2-Alkenylanilines Using Persulfate

Indole scaffold synthesis relies primarily on oxidative C-H amination of N-protected alkenylanilines for C-N intramolecular cyclization reactions. Herein, for the first time, without N-protection, various readily prepared 2-alkenylanilines were transformed into the desired indole products in good yields by using K 2 S 2 O 8 as oxidant in the presence of catalytic amounts of FeF 2. The K 2 S 2 O 8 /FeF 2 system offers a direct and benign synthetic route to 3-arylindoles and it is applicable to a wide range of substituted indoles including drug intermediates.

Cascade Amination/Cyclization/Aromatization Process for the Rapid Construction of [2,3-c]Dihydrocarbazoles and [2,3-c]Carbazoles

An intramolecular cascade amination/cyclization/aromatization reaction of functionalized alkylidenecyclopropanes has been developed in the presence of silver acetate, affording a variety of [2,3-c]dihydrocarbazoles and [2,3-c]carbazoles in moderate to excellent yields. The mechanistic investigations revealed that this cascade reaction proceeds through a radical initiated process. Moreover, further transformations for the synthesis of eustifoline-D and an OLED exhibit a potential synthetic utility of this method.

Carbonyl group coordination preferences in square-planar NiII and PdII complexes of pentadentate ligands by electron-withdrawing/donating substituents

A series of chirally switchable NiII and PdII complexes were synthesized and fully characterized by X-ray crystallography and additionally by NMR. It was found that control of the stereochemical preference between (S?,S?) and (S?,R?)

BIS(FLUOROALKYL)-1,4-BENZODIAZEPINONE COMPOUNDS AND PRODRUGS THEREOF

Disclosed are compounds of Formula (I) and/or salts thereof: wherein R1 is —CH2CH2CF3; R2 is —CH2CH2CF3 or —CH2CH2CH2CF3; R3 is H, —CH3, or Rx; R4 is H or Ry; Ring A is phenyl or pyridinyl; and Rx, Ry, Ra, Rb, y, and z are defined herein. Also disclosed are methods of using such compounds to inhibit the Notch receptor, and pharmaceutical compositions comprising such compounds. These compounds are useful in treating, preventing, or slowing the progression of diseases or disorders in a variety of therapeutic areas, such as cancer; or as prodrugs of such compounds.

Palladium-catalyzed direct addition of arylboronic acids to 2-aminobenzonitrile derivatives: Synthesis, biological evaluation and in silico analysis of 2-aminobenzophenones, 7-benzoyl-2-oxoindolines, and 7-benzoylindoles

A palladium-catalyzed direct addition of arylboronic acids to unprotected 2-aminobenzonitriles has been developed, leading to a wide range of 2-aminobenzophenones with moderate to excellent yields. The transformation has broad scope and high functional group tolerance. Moreover, 2-oxoindoline-7-carbonitrile and indole-7-carbonitrile were applicable to this process for the construction of 7-benzoyl-2-oxoindolines and 7-benzoylindoles, respectively. Among the compounds examined, compound 4e possessed the most potent anticancer activity against H446 and HGC-27 in vitro, with IC50 values of 0.02 μmol L-1 and 0.09 μmol L-1, respectively, while compound 4a showed the best potent anticancer activity against SGC-7901 with an IC50 value of 0.01 μmol L-1. Furthermore, we also performed in silico molecular docking calculations to investigate the interaction mode and binding affinity between the examined compounds and their tubulin target. This journal is