65854-93-5

Upstream product

• 98-88-4 benzoyl chloride 
• 619-45-4 4-methoxycarbonyl aniline 
• 179057-17-1 N-[4-(hydroxymethyl)phenyl] benzamide 
• 87199-17-5 4-formylphenylboronic acid, 
• 19226-36-9 3-phenyl-5H-1,4,2-dioxazol-5-one 
• 619-66-9 4-Carboxybenzaldehyde 
• 65-85-0 benzoic acid 
• 61650-22-4 N-(pivaloyloxy)benzamide 
• 623-04-1 4-aminobenzenemethanol 
• 100-47-0 benzonitrile 
• 873-75-6 4-bromobenzenemethanol 
• 555-16-8 4-nitrobenzaldehdye 
• 2403-53-4 2-(4-nitrophenyl)-1,3-dioxolane 
• 19073-14-4 4-(1,3-dioxolan-2-yl)aniline 

Downstream Products

• 1024592-14-0 trans-1-[4-(benzoylamino)phenyl]-3-phenyl-1-propen-3-one 
• 1143504-67-9 C₂₈H₂₄N₂O₄ 
• 492-70-6 1,2-diphenyl-1,2-ethanediol 
• 956-05-8 3-(4-aminophenyl)-1-phenyl-2-propen-1-one 
• 220861-72-3 5-(4-benzoylamino-phenyl)-3-oxo-tetrahydro-furan-2-carboxylic acid ethyl ester 

Relevant academic research and scientific papers

Visible-Light-Promoted Iron-Catalyzed N-Arylation of Dioxazolones with Arylboronic Acids

A visible-light-promoted and simple iron salt-catalyzed N-arylation was achieved efficiently under external photosensitizer-free conditions. Arylboronic acids and bench-stable dioxazolones were used for this cross-coupling reaction. This reaction features high reactivity, wide substrate scope, good functional group tolerance, simple operation procedure, and mild reaction conditions. Preliminary mechanistic investigations were conducted to support a radical pathway. This method may contribute to shift the paradigm of iron-catalyzed C-N bond construction and nitrene transfer chemistry.

Direct conversion of carboxylic acids to various nitrogen-containing compounds in the one-pot exploiting curtius rearrangement

Herein we report, a single-pot multistep conversion of inactivated carboxylic acids to various N-containing compounds using a common synthetic methodology. The developed methodology rendered the use of carboxylic acids as a direct surrogate of primary amines, for the synthesis of primary ureas, secondary/tertiary ureas, O/S-carbamates, benzoyl ureas, amides, and N-formyls, exploiting the Curtius reaction. This approach has a potential to provide a diversified library of N-containing compounds, starting from a single carboxylic acid, based on the selection of the nucleophile.

Rhodium-catalyzed electrophilic amination of arylboronic acids with secondary hydroxylamines

A rhodium(III)-catalyzed electrophilic amination of arylboronic acids with secondary hydroxylamines has been developed. The rhodium catalysis is compatible with heteroarylboronic acids as well as acyl and alkoxycarbonyl protecting groups on the nitrogen of O-acylhydroxylamines, and the corresponding secondary anilines are obtained in good to excellent yields.

Palladium-Catalyzed Synthesis of Aryl Amides through Silanoate-Mediated Hydrolysis of Nitriles

A procedure for the formation of aryl amides through the palladium-catalyzed coupling of nitriles and aryl bromides, via the formation of intermediary silanoate derived imidate species is reported. Optimization was undertaken and examples of the process are described that furnish the products in up to 86% isolated yield.

Design and synthesis of novel benzoxazole analogs as Aurora B kinase inhibitors

A novel series of benzoxazole analogs was designed and synthesized, and their inhibitory activities against Aurora kinases were evaluated. Some of the tested compounds exhibited a promising activity with respect to the inhibition of Aurora B kinase. A structure-activity relationship study indicated that linker length, regiochemistry, and halogen substitution play important roles in kinase inhibitory potency. The binding modes between representative compounds and Aurora kinases were interpreted through a molecular docking study to explain the inhibitory activity and selectivity for Aurora A and B kinases. Compounds 13l and 13q also show an antiproliferative effect on the human tumor cell lines in a dose-dependent manner. The most potent 13q demonstrated good efficacy in the prostate cancer PC-3 tumor xenograft model.

Design and synthesis of novel 3,5-substituted indolin-2-one derivatives

In this paper, twelve novel 3,5-substituted indolin-2-one derivatives were designed and synthesized based on indolin-2-one. The structures of the new compounds have been confirmed by 1 H NMR, HR-MS and IR spectra analysis. This study provides a new method for development of indolin-2-one derivatives.

Design and synthesis of novel N-benzylidenesulfonohydrazide inhibitors of murC and murD as potential antibacterial agents

A series of novel N-benzylidenesulfonohydrazide compounds were designed and synthesized as inhibitors of UDP-N-acetylmuramic acid:L-alanine ligase (MurC) and UDP-N-acetylmuramoyl-L-alanine:D-glutamate ligase (MurD) from E. coli, involved in the biosynthes

PHARMACEUTICAL COMPOSITION COMPRISING PYRAZOLONE DERIVATIVE

The present invention relates to pharmaceutical compositions containing a compound represented by formula (I), or a pharmaceutically acceptable prodrug or salt thereof, or a hydrate or solvate thereof as an active ingredient, (wherein, R1, R2, R3, and R4 are the same as R1, R2, R3, and R4 in the description of the present invention).

New arylsulfonohydrazide inhibitors of enzymes MurC and MurD

This invention belongs to the field of pharmaceutical chemistry and relates to new arylsulfonohydrazides as inhibitors of UDP-N-acetylmuramyl:L-alanine ligaze (MurC) and UDP-N-acetylmuramyl-L-alanine:D-glutamate ligaze (MurD), to procedures for their preparation and pharmaceutical preparations containing the same. The enzymes MurC and MurD are the key enzymes involved in the synthesis of bacterial peptidoglycan, so arylsulfonohydrazide inhibitors possess antibacterial activity. Compounds of general formula I and the pharmaceutically acceptable salts are described. The appropriate substituents are clearly presented in the body of the text and in claims.

Synthesis and in vitro evaluation of a series of diketopiperazine inhibitors of plasminogen activator inhibitor-1

We have synthesized and evaluated a series of diketopiperazine-based inhibitors of PAI-1. These studies resulted in the identification of 34 which inhibited PAI-1 in vitro with an IC50 = 0.2 μM. The synthesis and SAR of these compounds are desc