905710-81-8

Upstream product

• 94569-84-3 2-bromo-5-fluorobenzaldehyde 
• 4009-98-7 (methoxymethyl)triphenylphosphonium chloride 
• 866029-28-9 2-(2-bromo-5-fluorophenyl)ethan-1-ol 
• 1069115-12-3 methyl 2-(2-bromo-5-fluorophenyl)acetate 
• 739336-26-6 2-(2-bromo-5-fluorophenyl) acetic acid 
• 4009-98-7 (methoxymethyl)triphenylphosphonium chloride 

Downstream Products

• 866029-28-9 2-(2-bromo-5-fluorophenyl)ethan-1-ol 
• 905710-82-9 1-bromo-4-fluoro-2-[2-(methoxymethoxy)ethyl]benzene 
• 1416799-71-7 1-(2-bromo-5-fluorophenyl)-4-(2-phenoxyphenyl)but-3-yn-2-ol 
• 1373403-27-0 C₁₂H₁₂BrFO₂ 
• 1600046-05-6 C₁₁H₁₂BrFO 

Relevant academic research and scientific papers

Synthesis and inhibitory studies of phosphonic acid analogues of homophenylalanine and phenylalanine towards alanyl aminopeptidases

A library of novel phosphonic acid analogues of homophenylalanine and phenylalanine, containing fluorine and bromine atoms in the phenyl ring, have been synthesized. Their inhibitory properties against two important alanine aminopeptidases, of human (hAPN, CD13) and porcine (pAPN) origin, were evaluated. Enzymatic studies and comparison with literature data indicated the higher inhibitory potential of the homophenylalanine over phenylalanine derivatives towards both enzymes. Their inhibition constants were in the submicromolar range for hAPN and the micromolar range for pAPN, with 1-amino-3-(3-fluorophenyl) propylphosphonic acid (compound 15c) being one of the best low-molecular inhibitors of both enzymes. To the best of our knowledge, P1 homophenylalanine analogues are the most active inhibitors of the APN among phosphonic and phosphinic derivatives described in the literature. Therefore, they constitute interesting building blocks for the further design of chemically more complex inhibitors. Based on molecular modeling simulations and SAR (structure-activity relationship) analysis, the optimal architecture of enzyme-inhibitor complexes for hAPN and pAPN were determined.

Benzoxaborole-1-alcohol compound and preparation method and application thereof

The invention belongs to the field of bactericides, and particularly relates to a benzoxaborole-1-alcohol compound and a preparation method and application thereof. The benzoxaborole-1-alcohol compound has good bactericidal activity, can effectively control tomato early blight, wheat scab, rice sheath blight disease, strawberry gray mold, apple blotch, cucumber anthracnose and other crop diseases,can produce excellent antibacterial effects at low concentration, and shows good selectivity. The compound is used as a leucyl-tRNA synthetase inhibitor, the evolution difference of aminoacyl-tRNA synthetase of germs and eukaryotes is utilized, and the compound has very high safety to non-target organisms while killing the germs and can be used as a bactericide in agriculture.

Indoles synthesized from amines via copper catalysis

N-Substituted indoles are synthesized from primary amines through a tandem reaction sequence. Initial condensation of the amine with an α-(o-haloaryl)ketone or aldehyde is followed by intramolecular aryl amination catalyzed by CuI. A variety of anilines and alkyl amines, including those with significant steric demands, are converted to indoles in high yields and with varying indole substitution.

CuCN-mediated cascade cyclization of 4-(2-bromophenyl)-2-butenoates: A high-yield synthesis of substituted naphthalene amino esters

A new method of CuCN-mediated one-pot cyclization of 4-(2-bromophenyl)-2- butenoates leading to efficient synthesis of substituted naphthalene amino esters including phenanthrene aromatic structural units is described. Deuterium labeling studies establish

Asymmetric synthesis of chiral 9,10-dihydrophenanthrenes using Pd-catalyzed asymmetric intramolecular Friedel-Crafts allylic alkylation of phenols

We developed a novel asymmetric synthetic method for multisubstituted 9,10-dihydrophenanthrenes based on the Pd-catalyzed asymmetric intramolecular Friedel-Crafts allylic alkylation of phenols, which produces 10-vinyl or 10-isopropenyl chiral 9,10-dihydro

Palladium-catalyzed domino carbopalladation/C-H activation for the synthesis of tetrasubstituted alkenes bearing five- and seven-membered rings

A Pd-catalyzed domino carbopalladation/C-H-activation reaction of phenoxyphenyl-substituted propargylic alcohols was used for the synthesis of tetrasubstituted alkenes bearing either a dihydroindene or benzo[7]annulene motif. These compounds are of intere

Palladium-catalyzed domino carbopalladation/C-H activation for the synthesis of tetrasubstituted alkenes bearing five- and seven-membered rings

A Pd-catalyzed domino carbopalladation/C-H-activation reaction of phenoxyphenyl-substituted propargylic alcohols was used for the synthesis of tetrasubstituted alkenes bearing either a dihydroindene or benzo[7]annulene motif. These compounds are of intere

Hydrolytically-Resistant Boron-Containing Therapeutics And Methods Of Use

Compositions and methods of use of boron derivatives, including benzoxaboroles, benzazaboroles and benzthiaboroles, as therapeutic agents for treatment of diseases caused by fungi, yeast, bacteria or viruses are disclosed, as well as methods for synthesis of said agents and compositions thereof.

Discovery of a new boron-containing antifungal agent, 5-fluoro-1,3-dihydro- 1-hydroxy-2,1-benzoxaborole (AN2690), for the potential treatment of onychomycosis

A structure-activity relationship investigation for a more efficacious therapy to treat onychomycosis, a fungal infection of the toe and fingernails, led to the discovery of a boron-containing small molecule, 5-fluoro-1,3-dihydro- 1-hydroxy-2,1-benzoxaborole (AN2690), which is currently in clinical trials for onychomycosis topical treatment.