60425-49-2

Upstream product

• 67-56-1 methanol 
• 127605-44-1 (S)-homophenylalanine hydrobromide 
• 103-63-9 1-phenyl-2-bromoethane 
• 100-39-0 benzyl bromide 
• 106860-17-7 methyl 2S-2-amino-4-phenylbutanoate 
• 82732-07-8 Boc-L-homophenylalanine 
• 82795-51-5 D-homophenylalanine 
• 943-73-7 D-homophenylalanine 
• 127605-53-2 t-butyl N-Z-(S)-homophenylalanine 
• 123975-52-0 t-butyl 2-benzyloxycarbonylamino-3-carbomethoxy-4-phenyl-(2S)-butanoate 
• 80887-22-5 2-Acetylamino-2-phenethyl-malonic acid monoethyl ester 
• 141289-30-7 N-acetyl-DL-homophenylalanine ethyl ester 
• 96613-91-1 (R)-2-Acetamido-4-phenylbutansaeure 
• 5463-92-3 2-acetylamino-2-phenylethylmalonic acid diethyl ester 

Downstream Products

• 27038-09-1 (2S)-2-amino-4-phenyl-1-butanol 
• 885503-30-0 (2R,3R,5S)-2-(dimethoxyphosphoryl)-3-[2-(1,3-dioxo-1H,3H-benzo[de]isoquinolin-2-yl)ethyl]-5-[(1S)-methoxycarbonyl-3-phenylpropylcarbamoyl]pyrrolidine-1-carboxylic acid tert-butyl ester 
• 885503-52-6 (2R,3R,4R,5R)-5-(dimethoxyphosphoryl)-4-[2-(1,3-dioxo-1H,3H-benzo[de]isoquinolin-2-yl)ethyl]-2-[(1S)-methoxycarbonyl-3-phenylpropylcarbamoyl]-3-isobutylpyrrolidine-1-carboxylic acid tert-butyl ester 
• 116129-73-8 (4-morpholinylcarbonyl)-L-homophenylalanine 
• 116129-76-1 Morpholine-4-carboxylic acid {(S)-1-[(S)-1-((1S,2R,3S)-1-cyclohexylmethyl-2,3-dihydroxy-5-methyl-hexylcarbamoyl)-2-(1H-imidazol-4-yl)-ethylcarbamoyl]-3-phenyl-propyl}-amide 
• 245487-53-0 (S)-2-amino-N-methyl-4-phenylbutanamide 
• 1131010-46-2 N-(homophenylalanine methyl ester)-1-(2,4-dichloropheny)-5-(4-chlorophenyl)-4-methyl-1H-pyrazole-3-carboxamide 
• 1131444-48-8 methyl (2-ethoxy-2-oxoacetyl)-L-phenylalaninate 

Relevant academic research and scientific papers

Ribose conversion with amino acids into pyrraline platform chemicals-expeditious synthesis of diverse pyrrole-fused alkaloid compounds

One-pot conversion of sustainable d-ribose with l-amino acid, methyl esters produced pyrrole-2-carbaldehydes 5 in reasonable yields (32-63%) under pressurized conditions of 2.5 atm at 80 °C. The value-added pyrraline compounds 5 as platform chemicals were utilized for quick installation of poly-heterocyclic cores for the development of pyrrole-motif natural and artificial therapeutic agents. A pyrrole-fused piperazin-2-one scaffold 6 was prepared by reductive amination of pyrralines 5 with benzylamine. While further cyclization of pyrralines 5 with ethane-1,2-diamine produced pyrrolo-piperazin-2-ones 7 with an extra imidazolidine ring, the reaction with 2-amino alcohols derived from natural l-amino acids, alanine, valine, and phenylalanine, respectively provided pyrrolo-piperazin-2-ones 8, 9, and 10 with oxazolidine as the third structural core. Cell viability and an anti-inflammatory effect of the synthesized compounds were briefly tested by the MTT method and the Griess assay, among which 8h and 10g exhibited significant anti-inflammatory effects with negligible cell toxicity.

Rhodium-Catalyzed Enantioselective Synthesis of Oxazinones via an Asymmetric Ring Opening-Lactonization Cascade of Oxabicyclic Alkenes

The rhodium-catalyzed asymmetric ring opening reaction of oxabicyclic alkenes is shown to be an efficient method for synthesizing chiral heterocycles. We demonstrate that the pairwise combination of chiral catalyst with chiral amino-acid-derived pronucleophiles results in a stereodivergent synthesis of diastereomeric hydroxyesters. A favorable conformational preference induces the subsequent lactonization of one diastereomer leading to the highly enantioselective synthesis of oxazinones.

Substituted Dihydroisoquinolinones by Iodide-Promoted Cyclocarbonylation of Aromatic α-Amino Acids

Imidazolidinone derivatives of a range of aromatic α-amino acids, on treatment with phosgene and potassium iodide, undergo a mild Bischler-Napieralski-style cyclocarbonylation reaction that generates a tricyclic lactam by insertion of a C=O group between amino acid nitrogen and the ortho position of the aryl substituent. Regio- and diastereoselective functionalization of the lactam generates a library of substituted dihydroisoquinolinones and their congeners in enantioenriched form.

Distal Stereocontrol Using Guanidinylated Peptides as Multifunctional Ligands: Desymmetrization of Diarylmethanes via Ullman Cross-Coupling

We report the development of a new class of guanidine-containing peptides as multifunctional ligands for transition-metal catalysis and its application in the remote desymmetrization of diarylmethanes via copper-catalyzed Ullman cross-coupling. Through design of these peptides, high levels of enantioinduction and good isolated yields were achieved in the long-range asymmetric cross-coupling (up to 93:7 er and 76% yield) between aryl bromides and malonates. Our mechanistic studies suggest that distal stereocontrol is achieved through a Cs-bridged interaction between the Lewis-basic C-terminal carboxylate of the peptides with the distal arene of the substrate.

CANNABINOID RECEPTOR ANTAGONISTS/INVERSE AGONISTS USEFUL FOR TREATING OBESITY

The present invention provides novel pyrazoles that are useful as cannabinoid receptor antagonists and pharmaceutical compositions thereof and methods of using the same for treating obesity, diabetes, and/or cardiometabolic disorders.

UREA DERIVATIVES AND THEIR THERAPEUTIC USE

A compound of formula (I) wherein R1 is C1-6 alkyl optionally substituted by OH, C1-4 alkyl, SH, C1-4 alkylthio, phenyl or indol-3-yl, wherein C1-4 alkyl and C1-4 alkylthio are optionally s

USE OF AN AUREOLYSIN INHIBITOR FOR THE TREATMENT OF INFLAMMATORY SKIN CONDITIONS CHARACTERISED BY COLONISATION WITH STAPHYLOCOCCUS AUREUS

There is provided, inter alia, a method for the treatment or prevention of an inflammatory skin condition which is characterised by colonisation with Staphylococcus aureus, comprising the topical administration of an aureolysin inhibitor.

Novel method of treatment of inflammatory skin conditions

There is provided, inter alia, a method for the treatment or prevention of an inflammatory skin condition which is characterised by colonisation with Staphylococcus aureus, comprising the topical administration of an aureolysin inhibitor.

Discovery of a Potent and Novel Motilin Agonist

A novel series of dihydro- and tetrahydrotriazolopyridazine-1, 3-dione-based amino acid derivatives were identified as very potent motilin receptor agonists. Incorporating one additional phenylethyl glycinamide subunit to 1 (EC50 = 660 nM) was