107015-96-3

Upstream product

• 107015-98-5 O,O-diethyl-1-amino-2-(4-fluorophenyl)ethylphosphonate 
• 459-46-1 4-Fluorobenzyl bromide 
• 107015-98-5 (-)-O,O-diethyl-1-amino-2-(4-fluorophenyl)ethylphosphonate 
• 107015-98-5 (+)-O,O-diethyl-1-amino-2-(4-fluorophenyl)ethylphosphonate 
• 405-50-5 p-Fluorophenylacetic acid 
• 154109-03-2 {2-(4-Fluoro-phenyl)-1-[(Z)-hydroxyimino]-ethyl}-phosphonic acid diethyl ester 
• 5153-69-5 4-fluoro-β-nitrostyrene 
• 81399-34-0 1-(4-Fluorophenyl)ethylene-2-phosphonic acid diethyl ester 
• 130828-86-3 O,O-diisopropyl-1-N-benzylidenamino-2-(4-fluorophenyl)ethylphosphonate 
• 352-32-9 p-fluorotoluene 

Relevant academic research and scientific papers

Phosphonic acid analogs of fluorophenylalanines as inhibitors of human and porcine aminopeptidases N: Validation of the importance of the substitution of the aromatic ring

A library of phosphonic acid analogs of phenylalanine substituted with fluorine, chlorine and trifluoromethyl moieties on the aromatic ring was synthesized and evaluated for inhibitory activity against human (hAPN) and porcine (pAPN) aminopeptidases. Fluorogenic screening indicated that these analogs are micromolar or submicromolar inhibitors, both enzymes being more active against hAPN. In order to better understand the mode of the action of the most active compounds, molecular modeling was used. It confirmed that aminophosphonic portion of the enzyme is bound nearly identically in the case of all the studied compounds, whereas the difference in activity results from the placement of aromatic side chain of an inhibitor. Interestingly, both enantiomers of the individual compounds are usually bound quite similarly.

A (E) - 2-aryl ethylene cinnamenyl method for preparing ester derivative

The invention discloses method for preparing (E)-2-aryl vinyl phosphonate derivatives. The method comprises the specific following steps of dissolving 1-nitro-2-aryl-vinyl derivatives, a phosphorus reagent, an accelerator manganese acetate and a catalyst copper acetate in a solvent and reacting at 20-100 DEG C to obtain the (E)-2-aryl vinyl phosphonate derivatives. According to the method disclosed by the invention, the 1-nitro-2-aryl-vinyl derivatives are adopted as starting materials, the raw materials are easily available and have multiple varieties; the products obtained by the method disclosed by the invention are multiple and can be directly applied and can be also used for other further reaction; according to the method, the use of precious metal reagents and other additives is avoided; and meanwhile, the synthetic route is short, reaction conditions are mild, the reaction operation and post-treatment process are simple, the yield is high and the method is suitable for scale production.

ORGANIC PHOSPHORUS COMPOUNDS 96. RESOLUTION OF 1-AMINO-2-(4-FLUOROPHENYL)ETHYLPHOSPHONIC ACID AS WELL AS SOME DI- AND TRIPEPTIDES

Resolution of racemic 1-amino-2-(4-fluorophenyl)ethylphosphonic acid with dibenzoyltartrate is easily accomplished.In the inhibition of PAL 2b(-) is about five times as active as 2a(+).The synthesis of the dipeptides 5a and 5b, and of the tripeptides 8a a

ORGANIC PHOSPHORUS COMPOUNDS 97. SYNTHESIS AND PROPERTIES OF 1-AMINO-2-ARYL- AND 2-PYRIDYL-ETHYLPHOSPHONIC ACIDS AND DERIVATIVES

1-Amino-2-(o, m, and p-pyridyl)-ethylphosphonic acids, 5α, 5β and 5γ, have been prepared by alkylation of benzylideneaminomethylphosphonate, followed by hydrogenation and hydrolysis, whereas 1-amino-2-(o, m, and p-methoxyphenyl)-ethylphosphonic acids, 5i,

ORGANIC PHOSPHORUS COMPOUNDS 91. SYNTHESIS AND PROPERTIES OF 1-AMINO-2-ARYLETHYLPHOSPHONIC AND -PHOSPHINIC ACIDS AS WELL AS -PHOSPHINE OXIDES

The preparation, physical and spectroscopic properties of 1-amino-2-arylethylphosphonic, and -phosphinic acids as well as -phosphine oxides, the phosphorus analogues of phenylalanine are described, and the reactions of 1-amino-2-(4-fluorophenyl)ethylphosphonates with acetals, isocyanides, esters, acid anhydrides, activated aromatic nitro- and halogen compounds, and with N-protected alanine are reported.It is shown that several of the 1-amino-2-arylethylphosphonic acids are strong inhibitors of PAL and anthocyanin synthesis and also are quite active botryticides.Among the active compounds were 1-amino-2-(4-fluorophenyl)ethylphosphonic acid, 3f, and the methyl-substituted compounds 3k, 3l, and 3m.The fluoroderivative 3f was also effective as a seed-dressing agent in barley showing a 100percent protection against the fungus Fusarium nivale at 600 ppm.