21405-64-1

Upstream product

• 37556-13-1 diethyl (4-chlorobenzyl)malonate 
• 17449-02-4 p-chlorobenzylidenepropane-1,3-dioic acid 
• 622-95-7 4-chlorobenzyl bromide 
• 104-88-1 4-chlorobenzaldehyde 
• 104-83-6 1-Chloro-4-(chloromethyl)benzene 
• 88466-67-5 2,2-dimethyl-5-(4-chlorophenyl)methyl-1,3-dioxane-4,6-dione 

Downstream Products

• 860375-05-9 (4-chloro-benzyl)-piperidinomethyl-malonic acid 
• 90725-45-4 acide α bromo β chlorophenylpropionique 
• 7424-00-2 DL-Phe(4Cl) 
• 77522-28-2 bis(2,4,6-trichlorophenyl) 4-chlorobenzylmalonate 
• 82983-19-5 2-(4-chlorobenzyl)-propenoic acid 
• 2019-34-3 3-(4-chlorophenyl)propanoic acid 
• 351014-57-8 vinyl 3-(4-chlorophenyl)propanoate 
• 115355-27-6 4-chloro-α-<((R,S)-acetylthio)methyl>benzenepropanoic acid 
• 115370-16-6 (R)-2-[(R)-2-Acetylsulfanylmethyl-3-(4-chloro-phenyl)-propionylamino]-3-benzylsulfanyl-propionic acid ethyl ester 
• 115370-17-7 (R)-2-[(S)-2-Acetylsulfanylmethyl-3-(4-chloro-phenyl)-propionylamino]-3-benzylsulfanyl-propionic acid ethyl ester 
• 111510-44-2 2-Benzoylsulfanylmethyl-3-(4-chloro-phenyl)-propionic acid 
• 111510-55-5 Thiobenzoic acid S-[2-chlorocarbonyl-3-(4-chloro-phenyl)-propyl] ester 
• 107673-25-6 (R)-2-[3-(4-Chloro-phenyl)-2-mercaptomethyl-propionylamino]-3-ethylsulfanyl-propionic acid 
• 111510-65-7 (R)-2-[2-Benzoylsulfanylmethyl-3-(4-chloro-phenyl)-propionylamino]-3-ethylsulfanyl-propionic acid 

Relevant academic research and scientific papers

Synthesis and insecticidal activity of mesoionic pyrido[1,2-α]pyrimidinone derivatives containing a neonicotinoid moiety

Mesoionic pyrido[1,2-α]pyrimidinone derivatives containing a neonicotinoid moiety were designed, synthesized, and evaluated for their insecticidal activity. Some of the title compounds showed remarkable insecticidal properties against Aphis craccivora. Compound I13 exhibited satisfactory insecticidal activity against A. craccivora. Meanwhile, label-free proteomics analysis of compound I13 treatment identified a total of 821 proteins. Of these, 35 proteins were up-regulated, whereas 108 proteins were down-regulated. Differential expressions of these proteins reflected a change in cellular structure and metabolism.

METHYLENE LINKED QUINOLINYL MODULATORS OF RORyt

The present invention comprises compounds of Formula I. wherein: R1, R2, R3, R4, R5, R6, R7, R8, and R9 are defined in the specification. The invention also comprises a method of treating or ameliorating a syndrome, disorder or disease, wherein said syndrome, disorder or disease is rheumatoid arthritis or psoriasis. The invention also comprises a method of modulating RORγt activity in a mammal by administration of a therapeutically effective amount of at least one compound of claim 1.

Pd(II)-catalyzed intramolecular amidoarylation of alkenes with molecular oxygen as sole oxidant

Stereoselective palladium-catalyzed synthesis of structurally versatile indoline derivatives, using molecular oxygen as the sole oxidant, is described. New C-N and C-C bonds form across an alkene in an intramolecular manner. The C-N bond-forming step proceeds via a syn-amidopalladation pathway. The moderate kinetic isotope effects (intramolecular KIE = 3.56) suggest that electrophilic aromatic substitution occurs in the arylation step.

The effect of vinyl esters on the enantioselectivity of the lipase-catalysed transesterification of alcohols

The enantioselectivity of the lipase from Pseudomonas cepacia (PCL) in the transesterification of 2-phenyl-1-propanol 1 was studied using a series of vinyl 3-arylpropanoates as acyl donors. The most enantioselective transesterification reaction of the alcohol was attained by using vinyl 3-(p-iodophenyl)- or 3-(p-trifluoromethylphenyl)propanoates, with enantiomer ratios, E, of 116 and 138, respectively. Vinyl 3-phenylpropanoate was also effective for the resolution of 1 mediated by lipases from P. fluorescens and porcine pancreas and for the PCL-catalysed transesterification of several 2-phenyl-1-alkanols. The enantiomeric resolution of 1 was practically carried out by the first enantioselective transesterification using PCL and vinyl 3-(p-iodophenyl)propanoate to afford (R)-1 and then the enantioselective hydrolysis of the resultant ester to afford (S)-1.

Mercaptoacyl amino acid inhibitors of atriopeptidase. 1. Structure- activity relationship studies of methionine and S-alkylcysteine derivatives

A broad series of N-(3-mercaptoacyl) amino acid derivatives was evaluated for their ability to inhibit atriopeptidase (neutral endopeptidase, EC 3.4.24.11) in vitro and in vivo. Structural parameters studied were (i) the substituent on the 2-position of the 3-mercaptopropionyl moiety, (ii) the amino acid component, (iii) the S-terminal derivative, and (iv) the C- terminal derivative. Optimum activity was observed for derivatives of methionine and S-alkylcysteines. N-[3-Mercapto-2(S)-[(2- methylphenyl)methyl]-1-oxopropyl]-L-methionine was identified as a highly effective inhibitor of atriopeptidase meriting evaluation as a potential cardiovascular therapeutic agent.

ENKEPHALINASE ENZYME INHIBITING COMPOUNDS

Chiral 2-(2-benzyl-3-mercaptopropionylamino)-1-alkanol derivatives and chiral 2-(2-benzyl-3-mercaptopropionylamino)-4-methylthiobutyric acids are inhibitors of enkephalinase enzyme, reflecting their clinical utility as analgesics or anticonvulsant agents, or as therapy for disorders in which endogenous enkephalin levels are below normal.

Mesoionic Xanthine Analogues: Phosphodiesterase Inhibitory and Hypotensive Activity

Several mesoionic thiazolopyrimidines and mesoionic 1,3,4-thiadiazolopyrimidines were evaluated as inhibitors of cyclic-AMP phosphodiesterase.While small alkyl substituents at the 6 position have no significant effect on activity, phenyl and benzyl substituents enhance activity.Mesoionic structures such as 1 (R2 = H; R8 = Et) possess 20 to 40 times activity of theophylline when the R6 substituent is phenyl or 4-chlorobenzyl.Methyl and ethyl substitution at the 2 position essentially abolishes activity.Although plagued by solubility problems, several of the mesoionic derivatives were found to display weak hypotensive effects in vivo.