2385-27-5

Upstream product

• 93-98-1 N-phenyl benzoyl amide 
• 53548-19-9 α-(o-nitrophenyl)-N-phenylnitrone 
• 75-36-5 acetyl chloride 
• 71-43-2 benzene 
• 552-16-9 ortho-nitrobenzoic acid 
• 62-53-3 aniline 
• 610-14-0 2-nitrobenzyl chloride 
• 694-59-7 pyridine N-oxide 
• 57761-80-5 N-Phenyl-o-nitrobenzimidoyl chloride 
• 4530-20-5 BOC-glycine 
• 7697-37-2 nitric acid 
• 67-64-1 acetone 
• 15761-38-3 L-N-Boc-Ala 
• 97839-44-6 2-Nitro-thiobenzoesaeure-S-phenylester 

Downstream Products

• 17761-73-8 N-phenyl-2-ethylaminobenzamide 
• 99420-23-2 N-(2-nitrobenzoyl)-2,4-dinitroaniline 
• 57761-80-5 N-Phenyl-o-nitrobenzimidoyl chloride 
• 4424-17-3 2-aminobenzanilide 
• 35092-97-8 N-acetyl-N-(2-nitro-benzoyl)-aniline 
• 855245-86-2 2-(benzylamino)-N-phenylbenzamide 
• 57761-69-0 5-(2-nitrophenyl)-1-phenyltetrazole 
• 17049-65-9 2-phenyl-1,2-dihydro-3H-indazol-3-one 
• 35118-30-0 N-phenyl-N-cyanomethyl-2-nitrobenzamide 
• 16347-60-7 3-phenyl-4(3H)-quinazolinone 
• 20887-41-6 2,2-dimethyl-3-phenyl-2,3-dihydro-1H-quinazolin-4-one 
• 612-25-9 2-Nitrobenzyl alcohol 
• 33331-19-0 N-(2-nitrobenzyl)aniline 
• 62-53-3 aniline 

Relevant academic research and scientific papers

One-Pot Synthesis of Seven-Membered Heterocyclic Derivatives of Diazepines Involving Copper-Catalyzed Rearrangement Cascade Allyl-Amination

A novel and efficient method has been proposed for the synthesis of 1,4-benzodiazepine-5-ones from o-nitrobenzoic N-allylamides by using molybdenyl acetylacetonate and copper(II) trifluoromethanesulfonate as catalysts in the presence of triphenylphosphine. This synthesis process involves nitrene formation, C-H bond insertion, C≠C bond rearrangement, and C-N bond formation cascade reactions via copper- and molybdenum-catalyzed mediation. The method features a wide substrate scope and a moderate to high yield (up to 90%), exhibiting the possibility for practical applications.

A B2(OH)4-Mediated Synthesis of 2-Substituted Indazolone and Its Application in a DNA-Encoded Library

Indazolone cores are among the most common structural components in medicinal chemistry and can be found in many biologically active molecules. In this report, a mild and efficient approach to 2-substituted indazolones via B2(OH)4-mediated reductive N-N b

2-(2-chloro-4-methylphenyl) quinazoline-4 (3H)-one compound and medical application thereof

The invention discloses a 2-(2-chloro-4-methylphenyl) quinazoline-4 (3H)-one compound shown as formula (I) and a preparation method thereof and medical application thereof in sedative hypnotic, anticonvulsant, antidepressant, anxiolytic and other drugs.

Anthranilic amide and imidazobenzothiadiazole compounds disrupt: Mycobacterium tuberculosis membrane potential

A family of compounds typified by an anthranilic amide 1 was identified from a whole-cell screening effort targeted at identifying compounds that disrupt pH homeostasis in Mycobacterium tuberculosis. 1 demonstrated bactericidal activity against non-replicating M. tuberculosis in pH 4.5 buffer (MBC4.5 = 6.3 μM). Exploration of the structure-activity relations failed to simplify the scaffold. The antitubercular activity proved dependent on the lipophilicity and planarity of the molecule and directly correlated with mammalian cytotoxicity. Further studies revealed a pH-dependent correlation between the family's disruption of M. tuberculosis membrane potential and antitubercular activity, with active compounds causing a drop in membrane potential at concentrations below their MBC4.5. A second compound family, identified in the same screening effort and typified by imidazo(4,5-e)(2,1,3)benzothiadiazole 2, provided a contrasting profile. As with 1, structure-activity profiling of 2 (MBC4.5 = 25 μM) failed to minimize the initial scaffold, mammalian cytotoxicity was observed for a majority of the active compounds, and many of the active compounds disrupted M. tuberculosis membrane potential. However, unlike the anthranilic amide compounds, the benzothiadiazole compounds disrupted M. tuberculosis membrane potential primarily at concentrations above the MBC4.5 in a pH-independent fashion. These differences suggest an alternative mechanism of action for the benzothiadiazole compounds. As a result, while the cytotoxicity of the anthranilic amides limits their utility to tool compounds, benzothiadiazole 2 presents an attractive target for more focused SAR exploration.

Electrochemical: N-acylation synthesis of amides under aqueous conditions

An electrochemical N-acylation of carboxylic acids with amines was reported. The sustainable TBAB electrocatalysis proceeded with excellent chemoselectivity and positional selectivity, and with ample scope, allowing electrochemical N-acylation under mild reaction conditions at room temperature in water. Moreover, the synthetic utility of the current method is demonstrated by the synthesis of melatonin.

Method for synthesizing amide compound through photocatalysis in water phase

The invention discloses a method for synthesizing an amide compound through photocatalysis in a water phase. The method comprises the following steps: putting catalysis amounts of a free radical initiator, an amine derivative, a carboxylic acid derivative, a phase transfer catalyst, an inorganic base and water into a reaction container, carrying out a reaction in a photocatalysis reaction instrument at certain power under a room temperature condition, after a certain time, carrying out extraction by using a small amount of ethyl acetate, and carrying out recrystallization, so as to obtain theamide compound, wherein the free radical initiator is eosin, methyl orange, sodium persulfate, ammonium persulfate or potassium peroxodisulfate, the phase transfer catalyst is tetrabutylammonium bromide, and the power of the photocatalytic reaction instrument is 5W. By adopting the method disclosed by the invention, toxic thionyl chloride or phosphorus oxychloride is not needed for a chlorinationreaction, water is adopted as a solvent, a novel photocatalysis method is used, and the amide compound with a high yield can be prepared through a room-temperature reaction for 2-5 hours with an incandescent light bulb of 5W, and in addition, the method is simple in aftertreatment, and low in cost and is an ideal green synthesis method of amide compounds.

INHIBITORS OF OPLOPHORUS LUCIFERASE-DERIVED BIOLUMINESCENT COMPLEXES

Compounds that may selectively inhibit Oplophorus luciferase-derived bioluminescent complexes, e.g., NanoBiT? bioluminescent complex, are disclosed as well as compositions and kits comprising the compounds, and methods of using the compounds. The compounds are of formula (I) wherein R1-R4 and p and q are as defined in the claims.

The second aryl quinazoline compound, its preparation method and medical use thereof and comprising the pharmaceutical composition (by machine translation)

The invention relates to a I shown by following a kind of quinazoline ketone compound or its pharmaceutically acceptable salt, preparation method thereof, and for preparing tumor, antibacterial, anti-HIV, sedative and hypnotic, anticonvulsant, anti-tuberculosis, anti-Parkinson's syndrome, anti-inflammatory, antipyretic, regulating cardiovascular and regulating cell enzyme active function of the use of such drugs. (by machine translation)

Identification and SAR Evaluation of Hemozoin-Inhibiting Benzamides Active against Plasmodium falciparum

Quinoline antimalarials target hemozoin formation causing a cytotoxic accumulation of ferriprotoporphyrin IX (Fe(III)PPIX). Well-developed SAR models exist for β-hematin inhibition, parasite activity, and cellular mechanisms for this compound class, but no comparably detailed investigations exist for other hemozoin inhibiting chemotypes. Here, benzamide analogues based on previous HTS hits have been purchased or synthesized. Only derivatives containing an electron deficient aromatic ring and capable of adopting flat conformations, optimal for π-π interactions with Fe(III)PPIX, inhibited β-hematin formation. The two most potent analogues showed nanomolar parasite activity, with little CQ cross-resistance, low cytotoxicity, and high in vitro microsomal stability. Selected analogues inhibited hemozoin formation in Plasmodium falciparum causing high levels of free heme. In contrast to quinolines, introduction of amine side chains did not lead to benzamide accumulation in the parasite. These data reveal complex relationships between heme binding, free heme levels, cellular accumulation, and in vitro activity of potential novel antimalarials.

Deep eutectic solvent mediated synthesis of quinazolinones and dihydroquinazolinones: Synthesis of natural products and drugs

A mild and greener protocol was developed to synthesize substituted quinazolinones and dihydroquinazolinones via deep eutectic solvent (DES) mediated cyclization with a series of aliphatic, aromatic, and heteroaromatic aldehydes in good to excellent yields. This greener strategy was further utilised to synthesize various quinazolinone natural products and drugs.