721-47-1

Upstream product

• 613-90-1 benzoyl cyanide 
• 95-54-5 1,2-diamino-benzene 
• 728-90-5 N-(2-nitrophenyl)benzanilide 
• 64-19-7 acetic acid 
• 120-51-4 benzoic acid benzyl ester 
• 65-85-0 benzoic acid 
• 98-88-4 benzoyl chloride 
• 100-52-7 benzaldehyde 
• 70787-27-8 N-(2-bromophenyl)benzamide 
• 15310-02-8 o-iodobenzanilide 
• 93-97-0 benzoic acid anhydride 
• 146651-75-4 tert–butyl (2–aminophenyl)carbamate 
• 4231-62-3 1-benzoyl-1H-benzotriazole 
• 7310-83-0 2- benzoylaminoazobenzene 

Downstream Products

• 95-54-5 1,2-diamino-benzene 
• 65-85-0 benzoic acid 
• 716-79-0 2-phenyl-1H-benzoimidazole 
• 805316-09-0 2-m-tolylazo-aniline 
• 1257862-88-6 N-(2-benzamidophenyl)quinoxaline-2-carboxamide 
• 439574-25-1 (2-benzyl-1H-benzo[d]imidazol-1-yl)(phenyl)methanone 

Relevant academic research and scientific papers

Effect of a rigid sulfonamide bond on molecular folding: A case study

A disulfonamide compound with bulky aromatic side chains was prepared, and its properties as a potential building block for foldamers were evaluated. Two different solvate crystal forms of the compound were identified and compared to the structures of an

Synthesis, biological evaluation, and molecular docking analysis of novel linker-less benzamide based potent and selective HDAC3 inhibitors

A series of novel linker-less benzamides with different aryl and heteroaryl cap groups have been designed, synthesized, and screened as potent histone deacetylase (HDAC) inhibitors with promising anticancer activity. Two lead compounds 5e and 5f were foun

Insight into Fundamental Rules of Phenylenediamines Selective Monoacylation by the Comparisons of Kinetic Characteristics in Microreactor

In this paper, the kinetics of acylation reaction of o-phenylenediamine/p-phenylenediamine and benzoic anhydride were determined in microreactors, respectively. A kinetic model was established, all kinetic parameters including reaction orders, reaction rate constants, pre-exponential factors, and activation energies were acquired. Validation experiments showed experimental data fit well with calculated data at different reactant concentrations and residence times. The comparisons of the reaction rate constants and activation energies were summarized to show the difference of chemical reactivities of phenylenediamines. According to the calculation of the kinetic model, the optimized reaction conditions were listed to meet the monoacylation selectivity equal to 97.0%.

Copper-catalyzed regioselective 2-amination of o-haloanilides with aqueous ammonia

An efficient Cu(II)-vasicine catalytic system has been developed for intramolecular C[sbnd]N bond formation. In this way, regioselective 2-amination of o-haloanilides with aqueous ammonia in EtOH has been achieved. This strategy provides several advantages, such as good regioselectivity, high yields and functional group tolerance.

[Re(η6-C6H5-benzimidazole)2]+ and Derivatives as Dye Mimics; Synthesis, UV Absorption Studies and DFT Calculations

Functionalizations of highly oxidation and hydrolysis stable mono-cationic rhenium bis-arene complexes [Re(η6-C6H6)2]+ are of great interest. We directly built up structural features of the well-known Hoechst Dye on the coordinated arenes as a model for prospective DNA minor groove binding studies. Extensions of the aromatic bis-arene unit with functionalized and derivatized benzimidazole moieties resulted in a deep orange colour of the complexes, showing UV/Vis absorption spectra with multiple transition maxima. These have been assigned with support of DFT calculations to gain information about their charge transfer natures. The different transitions of the complexes, which are either intra-ligand, ligand-to-ligand or metal-to-ligand charge transitions, were additionally compared and discussed with the spectra of the corresponding free ligands.

N-Acylbenzotriazole: convenient approach for protecting group-free monoacylation of symmetric diamines

Abstract: An efficient green route for monoacylation of aromatic diamines, namely o-phenylenediamine and p-phenylenediamine and aliphatic diamines ethylenediamine and piperazine using N-acylbenzotriazoles (NABs) in n-butanol was developed. The new protocol does not require prior selective protection of the diamine and comprises simple conditions, short reaction times, an easy work up as well as high isolated yields (69–94%). Moreover, the method described herein enable stepwise acylation of aliphatic diamines such as ethylenediamine and piperazine with two different N-acylbenzotriazoles affording unsymmetrical substituted diamines that can be used for construction of pharmaceutically important targets such as drugs, foldamers, and drug conjugates. Graphic abstract: [Figure not available: see fulltext.]

Azobenzene-diamides as Photopharmacological Ligands for Insect Ryanodine Receptor

Photoresponsive ligands are powerful tool compounds for studying receptor function with spatiotemporal resolution. However, to the best of our knowledge, such a ligand is not available for the ryanodine receptor (RyR). Herein, we present a photochromic ligand (PCL) for insect RyR by decorating chlorantraniliprole (CHL) with photoswitchable azobenzene (AB). We demonstrated that one potent ligand, named ABCHL13, shows light-induced reversible trans-cis isomerization and 3.5-fold insecticidal activity decrease toward oriental armyworm (Mythimna separata) after UV-light irradiation, that is, trans-ABCH13 has higher activity than the cis-ABCH13. ABCHL13 enables optical control over intracellular Ca2+ release in dorsal unpaired median (DUM) neurons of M. separata and American cockroach (Periplaneta americana) and cardiac function of P. americana. Our results provide a first photopharmacological toolkit that is applicable to light-dependent regulation of RyR and heart beating.

Synthesis of Structurally Diverse Benzotriazoles via Rapid Diazotization and Intramolecular Cyclization of 1,2-Aryldiamines

An operationally simple method has been developed for the preparation of N-unsubstituted benzotriazoles by diazotization and intramolecular cyclization of a wide range of 1,2-aryldiamines under mild conditions, using a polymer-supported nitrite reagent and p-tosic acid. The functional group tolerance of this approach was further demonstrated with effective activation and cyclization of N-alkyl, -aryl, and -acyl ortho-aminoanilines leading to the synthesis of N1-substituted benzotriazoles. The synthetic utility of this one-pot heterocyclization process was exemplified with the preparation of a number of biologically and medicinally important benzotriazole scaffolds, including an α-amino acid analogue.

A kind of sphingomyelin synthase inhibitor, its preparation method and application thereof

The invention provides general formula (I) compound of formula, its pharmaceutically acceptable salts or stereoisomers, wherein X, Y, M, Z, R and Ar respectively as defined in the specification. The invention also provides a composition comprising a therapeutically effective amount of at least one of the foregoing general formula (I) compounds of formula, its pharmaceutically acceptable salts or stereoisomers, and the above-mentioned compound, its pharmaceutically acceptable salts or stereoisomers, or the above-mentioned pharmaceutical composition in preparation for the prevention and/or treatment of sphingomyelin level abnormal increase of the disease caused by the use of the medicament. The invention of the general formula (I) compound of formula, its pharmaceutically acceptable salts or stereoisomers, can selectively inhibit sphingomyelin synthase, internal and external pharmacodynamic effects are significant, the safety is high.

Comprehensive Synthesis of Amino Acid-Derived Thiazole Peptidomimetic Analogues to Understand the Enigmatic Drug/Substrate-Binding Site of P-Glycoprotein

A novel set of 64 analogues based on our lead compound 1 was designed and synthesized with an initial objective of understanding the structural requirements of ligands binding to a highly perplexing substrate-binding site of P-glycoprotein (P-gp) and their effect on modulating the ATPase function of the efflux pump. Compound 1, a stimulator of P-gp ATPase activity, was transformed to ATPase inhibitory compounds 39, 53, and 109. The ATPase inhibition by these compounds was predominantly contributed by the presence of a cyclohexyl group in lieu of the 2-aminobenzophenone moiety of 1. The 4,4-difluorocyclohexyl analogues, 53 and 109, inhibited the photolabeling by [125I]-IAAP, with IC50 values of 0.1 and 0.76 μM, respectively. Selected compounds were shown to reverse paclitaxel resistance in HEK293 cells overexpressing P-gp and were selective toward P-gp over CYP3A4. Induced-fit docking highlighted a plausible binding pattern of inhibitory compounds in the putative-binding pocket of P-gp. The current study underscores the stringent requirement by P-gp to bind to chemically similar molecules.