123715-56-0

Upstream product

• 28446-72-2 4-chlorocinnamonitrile 
• 65600-74-0 ethyl diethoxymethylphosphinate 
• 28446-72-2 (2E)-3-(4-chlorophenyl)acrylonitrile 
• 65600-72-8 ethyl P-(diethoxymethyl)phosphonite 

Downstream Products

• 103680-51-9 3-amino-1-(4-chlorophenyl)propylphosphonous acid 
• 103680-66-6 ethyl 3-amino-1-(4-chlorophenyl)propyl(diethoxymethyl)phosphinate 

Relevant academic research and scientific papers

Substituted propane-phosphinic acid compounds

Compounds of the formula I STR1 wherein R denotes an aliphatic, cycloaliphatic, cycloaliphatic-aliphatic or araliphatic radical having 2 or more carbon atoms, and wherein one of the groups R1, R2 and R3 represents hydrogen or an aliphatic, cycloaliphatic, araliphatic or aromatic radical, another one of R1, R2 and R3 is hydrogen or, in the case of R1 and R2, is hydroxy, and the remaining one of R1, R2 and R3 is hydrogen, and their salts have GABAB -antagonistic properties and can be used as GABAB -antagonists. They are obtained when in a compound of formula II STR2 in which R, R1, R2 and R3 have their previous significances, Z represents --NH2 and R4 denotes a hydroxy-protective group R5 or, when R1 and R3 denote hydrogen and R2 denotes hydrogen or alkyl, denotes an alkali metal or ammonium ion R6, or Z represents a protected or latent amino group Z0 and R4 deontes hydrogen or a hydroxy-protective group R5, any group R5 or R6 is replaced by hydrogen, and/or any group Z0 is converted into --NH2.

Substituted propane-phosphinic acid compounds

Compounds of the formula I STR1 wherein R denotes an aliphatic, cycloaliphatic, cycloaliphatic-aliphatic or araliphatic radical having 2 or more carbon atoms, and wherein one of the groups R1, R2 and R3 represents hydrogen or an aliphatic, cycloaliphatic, araliphatic or aromatic radical, another one of R1, R2 and R3 is hydrogen or, in the case of R1 and R2, is hydroxy, and the remaining one of R1, R2 and R3 is hydrogen, or wherein R denotes methyl, R1 denotes hydrogen or hydroxy, R2 denotes an aromatic radical and R3 represents hydrogen, and their salts have GABAB -antagonistic properties and can be used as GABAB -antagonists. They are obtained when in a compound of formula II STR2 in which R, R1, R2 and R3 have their previous significances, Z represents --NH2 and R4 denotes a hydroxy-protective group R5 or, when R1 and R3 denote hydrogen and R2 denotes hydrogen or alkyl, denotes an alkali metal or ammonium ion R6, or Z represents a protected or latent amino group Z0 and R4 denotes hydrogen or a hydroxy-protective group R5, any group R5 or R6 is replaced by hydrogen, and/or any group Z0 is converted into --NH2.

DIETHOXYMETHYLPHOSPHONITES AND PHOSPHINATES. INTERMEDIATES FOR THE SYNTHESIS OF α,β- AND γ-AMINOALKYLPHOSPHONOUS ACIDS

New building blocks for the synthesis of functional alkyl phosphonous acids are described.Diethoxymethylphosphonites and phosphinates are readily prepared and undergo reactions typical of phosphites and phosphonates.The products are stable to chemical transformations, readily handled and purified, and easily transformed to the phosphonous acids.

SYNTHESIS OF γ-AMINOPROPYLPHOSPHONOUS ACIDS USING HYPOPHOSPHOROUS ACID SYNTHONS

γ-Aminopropylphosphonous acids have heen synthesised using hypophosphorous acid synthons.

Substituted propane-phosphonous acid compounds

The compounds of the formula STR1 in which one of the groups R1, R2 and R3 represents hydrogen, C1-8 -alkyl, C3-6 -cycloalkyl, phenyl optionally substituted by halogeno, C1-4 -alkyl, C