6941-36-2

Upstream product

• 30412-43-2 sodium diethylacetamidomalonate 
• 104-83-6 1-Chloro-4-(chloromethyl)benzene 
• 622-95-7 4-chlorobenzyl bromide 
• 1068-90-2 2-acetylaminomalonic acid diethyl ester 
• 106-43-4 para-chlorotoluene 
• 13433-00-6 diethyl aminomalonate hydrochloride 

Downstream Products

• 7424-00-2 DL-Phe(4Cl) 
• 35175-65-6 acetylamino-(4-chloro-benzyl)-malonic acid 
• 23633-07-0 2-amino-3-(4-chlorophenyl)propionic acid hydrochloride 
• 14091-10-2 N-acetyl-4-chlorophenylalanine 
• 134166-72-6 D-p-chlorophenylalanine methyl ester 
• 14173-40-1 2-amino-3-(4-chlorophenyl)propionic acid methyl ester hydrochloride 
• 52031-05-7 2-amino-3-(4-chlorophenyl)propionic acid ethyl ester hydrochloride 
• 856571-34-1 3-(4-chlorophenyl)-2-{2-[(1H-indole-2-carbonyl)amino]benzoylamino}propionic acid ethyl ester 
• 856571-15-8 2-(2-aminobenzoylamino)-3-(4-chlorophenyl)propionic acid ethyl ester 
• 131402-99-8 2-Amino-3-(4-chloro-phenyl)-propionic acid octyl ester; hydrochloride 

Relevant academic research and scientific papers

Organocatalytic Enantioselective Addition of α-Aminoalkyl Radicals to Isoquinolines

With a dual organocatalytic system involving a chiral phosphoric acid and a dicyanopyrazine-derived chromophore (DPZ) photosensitizer and under the irradiation with visible light, an enantioselective Minisci-type addition of α-amino acid-derived redox-active esters (RAEs) to isoquinolines has been developed. A variety of prochiral α-aminoalkyl radicals generated from RAEs were successfully introduced on isoquinolines, providing a range of valuable α-isoquinoline-substituted chiral secondary amines in high yields with good to excellent enantioselectivities.

Anthranilic acid based CCK1 receptor antagonists: Preliminary investigation on their second "touch point"

In this phase of structure-affinity relationship study of VL-0395, a new anthranilic acid based CCK1 selective antagonist, we propose a series of unnatural aminoacidic derivatives. The result of this work is the identification of a new CCK ligand, which possesses an affinity (IC50 = 35 nm) one order of magnitude greater than the lead and, as a general rule, it points out how the hypothesized receptorial pocket which accommodates the Phe residue allows much more structural modification than that interacting with the N-terminal group. Hence, the modification of the C-terminal pharmacophoric group of our lead VL-0395 can not only enhance the affinity of anthranilic acid derivatives but can modulate the selectivity for one CCK receptor subtype or afford mixed antagonists.

Process for production of optically active n-protected-n-methyl-phenylalanine derivative

There is provided a process for industrially and efficiently producing an optically active N-protected-N-methyl-4-halogenophenylalanine at a high purity, which is useful as an intermediate for the production of pharmaceutical agents. An optically active N-protected-N-methyl-4-halogenophenylalanine (including the free form and/or the salt form thereof) purified to a high purity is produced by way of the deposition and isolation in the form of salt (DCHA salt or the like) from an optically active N-protected-N-methyl-4-halogenophenylalanine containing at least the optical isomer thereof as an impurity. Because the intended compound at a high purity can be recovered and obtained at a high yield, the process of the present invention is very useful as a process for producing the intermediate for the production of pharmaceutical agents.

A crystallization-induced asymmetric transformation to prepare (R)-4- chlorophenylalanine methyl ester

A second order asymmetric transformation of racemic 4- chlorophenylalanine methyl ester was achieved via salt formation with (2S,3S)-(-)-tartaric acid in the presence of salicylaldehyde to afford the desired (R)-enantiomer of 4-chlorophenylalanine methyl ester in good yield and high enantiomeric purity.