127780-65-8

Upstream product

• 127780-59-0 [1-(Benzhydrylidene-amino)-2-(4-methoxy-phenyl)-ethyl]-phosphonic acid diethyl ester 
• 104-93-8 p-methylanizole 
• 2746-25-0 p-Methoxybenzyl bromide 
• 122570-91-6 diethyl N-(diphenylmethylene) aminomethyl phosphonate 
• 79451-14-2 O,O-diethyl-4-methoxyphenylacetylphosphonate 
• 104-01-8 4-Methoxyphenylacetic acid 
• 146036-81-9 <1-Isocyanato(2(4-methoxy)phenyl)>ethylphosphonate de diethyle 
• 137619-23-9 O,O-diethyl-1-oximato-2-(4-methoxyphenyl)-ethylphosphonate 
• 130828-97-6 (2-(4-Methoxy-phenyl)-1-{[1-phenyl-meth-(E)-ylidene]-amino}-ethyl)-phosphonic acid diethyl ester 

Downstream Products

• 16656-37-4 1-amino-2-(4-hydroxyphenyl)ethylphosphonic acid 
• 66794-14-7 1-amino-2-(4-methoxyphenyl)-ethylphosphonic acid 

Relevant academic research and scientific papers

α-Aminoalkylphosphonates as a tool in experimental optimisation of P1 side chain shape of potential inhibitors in S1 pocket of leucine- and neutral aminopeptidases

The synthesis and biological activity studies of the series of structurally different α-aminoalkylphosphonates were performed in order to optimise the shape of the side chain of the potential inhibitors in S1 pocket of leucine aminopeptidase [E.C.3.4.11.1]. Analysis of a series of compounds with aromatic, aliphatic and alicyclic P1 side chains enabled to find out the structural features, optimal for that fragment of inhibitors of LAP. The most active among all investigated compounds were the phosphonic analogues of homo-tyrosine (Ki = 120:nM) and homo-phenylalanine (Ki = 140:nM), which even as racemic mixtures were better inhibitors in comparison with the best till now-phosphonic analogue of l-leucine (230 nM). Additional comparison of the inhibitory activity obtained for aminopeptidase N (APN, E.C.3.4.11.2) give insight into structural preferences of both enzymes.

SYNTHESE DE PEPTIDES MODIFIES INCORPORANT UN MOTIF PHOSPHORE N OU C TERMINAL

A general route to phosphopeptides with a 2-oxoalkylphosphonate moiety at the terminal N-amino group or with a 1-aminoalkylphosphonate moiety at the terminal C-carboxyl group is described.The method allows the preparation of various phosphopeptides with an α-alkylated carbon atom on the P-C bond from the very available dialkylpohosphonoalcanoic acids as starting products.

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.