253122-05-3

Upstream product

• 874-60-2 4-methyl-benzoyl chloride 
• 118-92-3 anthranilic acid 
• 55577-25-8 2-(4-methylphenyl)-1H-indole 
• 18600-54-9 2-(4-methylphenyl)-4H-3,1-benzoxazin-4-one 
• 108-88-3 toluene 
• 100-51-6 benzyl alcohol 
• 99-94-5 p-Toluic acid 
• 106-43-4 para-chlorotoluene 

Downstream Products

• 18600-54-9 2-(4-methylphenyl)-4H-3,1-benzoxazin-4-one 
• 67796-02-5 4-oxo-2-(p-tolyl)quinazoline-3(4H)-carbothioamide 
• 63002-95-9 3-amino-2-(4-methylphenyl)quinazolin-4(3H)-one 

Relevant academic research and scientific papers

A straightforward TBHP-mediated synthesis of 2-amidobenzoic acids from 2-arylindoles and their antimicrobial activity

A simple and highly efficient strategy has been developed for the synthesis of 2-amidobenzoic acids through the tert-butyl hydroperoxide (TBHP)-mediated oxygenation and sequential ring opening of 2-arylindoles in a one-pot fashion under metal-free aerobic conditions. The developed synthetic protocol is operationally simple, tolerates a wide range of functional groups, and is amenable to the gram-scale. Radical trapping experiments revealed that the reaction involves a radical pathway. The synthesized compounds (2a-s) were tested for in vitro antimicrobial activity. Among all screened compounds, 2d showed the maximum antibacterial activity against P. aerugunosa (ZOI = 17 mm, MIC = 32 μg mL-1) and compounds 2d and 2p showed the maximum (32 μg mL-1) antifungal activity against A. flavus and C. albicans.

Radical-Induced, Palladium-Catalyzed C–H Activation: An Approach to Functionalize 4H-Benzo[d][1,3]oxazin-4-one Derivatives by Using Toluenes, Aldehydes, and Benzyl Alcohols

Toluenes, aldehydes, and benzyl alcohols have been utilized in the radical-induced direct functionalization of 4H-benzo[d][1,3]oxazin-4-one derivatives by using a palladium-catalyzed C–H activation strategy. The stability, low toxicity, and ease of access

ANTI-ULCERATIVE COLITIS COMPOUND

Anti-ulcerative colitis compounds include quinazoline derivatives having the following structural formula: wherein R is H, OH, or OCH3, R1 is OH or OCH3, and R2 is OCH3, or a pharmaceutically acceptab

Substituent effects on hydrogen bonding of aromatic amide-carboxylate

N-(p-benzoyl)-anthranilic acid (BAA) derivatives have been synthesized with different substituents (X: Br, Cl, OCH3, CH3), and their crystal structures have been analyzed in order to understand the variations in their molecular geome

Precursor-directed combinatorial biosynthesis of cinnamoyl, dihydrocinnamoyl, and benzoyl anthranilates in saccharomyces cerevisiae

Biological synthesis of pharmaceuticals and biochemicals offers an environmentally friendly alternative to conventional chemical synthesis. These alternative methods require the design of metabolic pathways and the identification of enzymes exhibiting ade

Design and synthesis of quinazolinone tagged acridones as cytotoxic agents and their effects on EGFR tyrosine kinase

In a quest for finding potent cytotoxic molecules, we have designed and synthesized a new scaffold by tagging quinazolinones with an acridone moiety. The new acridone-4-carboximide derivatives were evaluated for their cytotoxic potentials against the MCF7 breast cancer cell line and three colon cancer cell lines (LS174T, SW1398, and WiDr). Compound 26 showed relatively potent cytotoxic activity among the derivatives, against all the cell lines tested. Mechanistic studies for the selected derivatives 7, 8, 16, 17, 25, and 26 were conducted through in vitro EGFR tyrosine kinase inhibition studies. The results indicate that compound 26 has a better EGFR tyrosine kinase inhibitory profile. The in vitro EGFR inhibition data was correlated with the cytotoxic properties, and molecular docking studies were performed with regard to the receptor autophosphorylation sites of the protein kinase domain of the EGFR.

Synthesis and characterization of quinazoline derivatives: Search for hybrid molecule as diuretic and antihypertensive agents

To explore the pharmacological and structure-activity relationship of a series of N-substituted-(4-oxo-2-substituted-phenylquinazolin-3-(4H)-yl), substituted benzene sulfonamide derivatives (1-25) were synthesized from substituted anthranilic acids derive

Substituent effects on energetics of peptide-carboxylate hydrogen bonds as studied by 1H NMR spectroscopy: Implications for enzyme catalysis

Substituent effects in N-H···O hydrogen bonds were estimated by comparing the acidities of two series of model compounds: N-benzoylanthranilic acids (A) and 4-benzoylamidobenzoic acids (B). Intramolecular N-H···O hydrogen bonds were found to be present in the A series of compounds, while B acids were used as control models. The respective pKa values for A and B acids were determined experimentally in DMSO solution using proton NMR spectroscopy. With X = H, the pKa for A and B acids were observed to be 7.6 and 11.6, respectively, a difference of 4.0 units (ΔpKa). However, with X = p-NO 2, the ΔpKa value between A and B acids increased to 4.7 units: the pKa values for A and B acids were determined as 6.7 and 11.4, respectively. The ΔpKa values between A and B acids as a function of the X substituents were studied in 10 other examples. The effects of X substituents in A acids could be predicted on the basis of the observed linear Hammett correlations, and the sensitivity of each substituent effect was found to be comparable to those observed for the ionization of substituted benzoic acids (ρ = 1.04 for A acids, and ρ = 1.00 for benzoic acids).

A new synthesis of 2-substituted 4H-3,1-benzoxazin-4-ones by cyanuric chloride cyclodehydration of N-benzoyl- and N-acylanthranilic acids

A new and a convenient method for the synthesis of aryl- and alkyl-2-substituted 4H-3,1-benzoxazin-4-ones by cyclodehydration of N-benzoyl- and N-acylanthranilic acid by cyanuric chloride is described.