131177-53-2Relevant articles and documents
OPTICALLY-ACTIVE 2-AMINO-PHOSPHONOALKANE ACID, OPTICALLY-ACTIVE 2-AMINOPHOSPHONOALKANE ACID SALT, AND HYDRATES OF THESE
-
Paragraph 0147-0157, (2020/05/14)
A novel compound has pharmacological activities comparable to those of Nahlsgen and is storable excellently stably. The compound can be produced by a method according to the present invention for producing an optically active 2-amino-phosphonoalkanoic acid salt. In the method, a starting material DL-2-amino-phosphonoalkanoic acid represented by Formula (1) or a hydrate thereof is reacted with an optically active basic compound other than an optically active lysine, to give a diastereomeric salt mixture including a first salt (including a hydrate salt) between a D-2-amino-phosphonoalkanoic acid represented by Formula (1-1) and the optically active basic compound, and a second salt (including a hydrate salt) between an L-2-amino-phosphonoalkanoic acid represented by Formula (1-2) and the optically active basic compound. The diastereomeric salt mixture is fractionally crystallized to isolate one of the first and second diastereomeric salts.
Involucrin gene expression promoter
-
Paragraph 0102; 0106, (2019/03/28)
PROBLEM TO BE SOLVED: To provide an involucrin gene expression promoter that has high effect of promoting involucrin gene expression, and is applied to the skin, to quickly increase involucrin concentrations, and markedly improving the barrier function. SOLUTION: An involucrin gene expression promoter contains at least one selected from a compound represented by the following formula (1) [where R1 and R2 are the same or different to represent a hydrogen atom, or a substituent. n is an integer of 1 or greater], a salt thereof, and their hydrates as an active ingredient. SELECTED DRAWING: None COPYRIGHT: (C)2019,JPO&INPIT
Enantioselective synthesis of both enantiomers of 2-amino-6-phosphonohexanoic acid [(R)- and (S)-AP6], a potent and specific agonist of AMPA receptor subtype
Garcia-Barradas, Oscar,Juaristi, Eusebio
, p. 1511 - 1514 (2007/10/03)
The preparation of both enantiomers of 2-amino-6-phosphonohexanoic acid [(R)- and (S)-AP6] is described. The highly diastereoselective alkylation of imidazolidinones 4 and hydrolysis of the alkylated products [(2R,5R,1'S)-6 and (2S,5S,1'S)-6] proceeds under relatively mild conditions to give the physiologically important, enantiopure aminophosphonic acids (R)-AP6 and (S)-AP6.
Phosphorus-containing aminocarboxylic acids. VII. Asymmetric synthesis of ω-phosphono-α-aminocarboxylic acids
Andronova,Maleev,Ragulin,Il'in,Tsvetkov,Belokon'
, p. 1068 - 1071 (2007/10/03)
New asymmetric ω-phosphono-α-aminocarboxylic acids were synthesized by alkylation with ω-bromoalkylphosphonates of the glycine methylene group in the Ni(II) complex of the Schiff base derived from glycine and (S)- and (R)-2-N-(N-benzylprolyl)-o-aminobenzo
PHOSPHORUS-CONTAINING AMINOCARBOXYLIC ACIDS. COMMUNICATION IV. A CONVENIENT METHOD OF PHOSPHONIC ACIDS SYNTHESIS
Ragulin, V. V.,Bofanova, M. E.,Tsvetkov, Eugene N.
, p. 237 - 242 (2007/10/02)
The communication is concerned with the synthesis of phosphonic aminocarboxylic acids by phosphorylation of diethyl ω-halogen alkyl acetamidomalonates with tris(trimethylsilyl) phosphite, followed by alcoholysis and acid hydrolysis of the resulting intermediate esters.Key words: Phosphonic aminocarboxylic acids; tris(trimethylsilyl) phosphite; ω-halogenalkyl acetamidomalonates; phosphorylation; alcoholysis, hydrolysis
SYNTHESE D'ACIDES ω-AMINO-ω-CARBOXY-ALKYLPHOSPHONIQUES
Aboujaoude, E. Elia,Collignon, N.,Savignac, P.,Bensoam, J.
, p. 93 - 104 (2007/10/02)
ω-Amino ω-carboxyalkylphosphonic acids 1 synthesis is reviewed.For n = 4, 5, 6 a general, efficient and inexpensive synthesis is described; acetamido(ω-bromoalkyl)malonates 12 are prepared from commercial dibromoalkanes and acetamidomalonate using the phase transfer catalysis process, then condensed with triethylphosphite through an Arbuzov reaction.An acid hydrolysis followed by purification on Dowex gives aminophosphonic acids 1 (n = 4, 5, 6) with a 70percent overall yield.The lower acid 1 (n = 2) is obtained with an identical overall yield from acetamidomalonate and 2-haloethylphosphonate using also liquid-solid phase transfer catalysis.