92122-49-1

Upstream product

• 24424-99-5 di-tert-butyl dicarbonate 
• 64-04-0 phenethylamine 
• 73096-21-6 (S)-Pyrrolidine-1,2-dicarboxylic acid 1-(4-nitro-phenyl) ester 
• 15761-39-4 1-(tert-butoxycarbonyl)-L-proline 
• 543-27-1 isobutyl chloroformate 

Downstream Products

• 123729-66-8 pyrrolidine-2-carboxylic acid phenethyl-amide 

Relevant academic research and scientific papers

Targeting the Src Homology 2 (SH2) Domain of Signal Transducer and Activator of Transcription 6 (STAT6) with Cell-Permeable, Phosphatase-Stable Phosphopeptide Mimics Potently Inhibits Tyr641 Phosphorylation and Transcriptional Activity

Signal transducer and activator of transcription 6 (STAT6) transmits signals from cytokines IL-4 and IL-13 and is activated in allergic airway disease. We are developing phosphopeptide mimetics targeting the SH2 domain of STAT6 to block recruitment to phosphotyrosine residues on IL-4 or IL-13 receptors and subsequent Tyr641 phosphorylation to inhibit the expression of genes contributing to asthma. Structure-affinity relationship studies showed that phosphopeptides based on Tyr631 from IL-4Rα bind with weak affinity to STAT6, whereas replacing the pY+3 residue with simple aryl and alkyl amides resulted in affinities in the mid to low nM range. A set of phosphatase-stable, cell-permeable prodrug analogues inhibited cytokine-stimulated STAT6 phosphorylation in both Beas-2B human airway cells and primary mouse T-lymphocytes at concentrations as low as 100 nM. IL-13-stimulated expression of CCL26 (eotaxin-3) was inhibited in a dose-dependent manner, demonstrating that targeting the SH2 domain blocks both phosphorylation and transcriptional activity of STAT6.

The phosphate-carboxylate mixed-anhydride method: A mild, efficient process for ester and amide bond construction

A highly efficient carboxylate-phosphate anhydride pathway is described for the direct, economical synthesis of esters and amides from carboxylic acids and alcohols or amines. The reaction proceeds with retention of configuration with both chiral secondary alcohols and α-amino acid derivatives allowing access to useful chiral auxiliaries, ligands, and organocatalysts. Ester and amide products can be isolated directly in high yield due to the water soluble nature of the side products.

Synthesis and catalytic activities of (S)-1-formylpyrrolidine-2-carboxylic acid derivatives for the enantioselective reductions of both a ketone and a ketimine

A series of (S)-1-formylpyrrolidine-2-carboxylic acid derivatives (6a-t) have been synthesised and examined as chiral organocatalysts in the asymmetric reduction of both ketone 2 and ketimine 3. These organic activators afforded good to moderate enantiose

2(S)-(Cycloalk-1-enecarbonyl)-1-(4-phenyl-butanoyl)pyrrolidines and 2(S)-(aroyl)-1-(4-phenylbutanoyl)pyrrolidines as prolyl oligopeptidase inhibitors

In order to replace the P2-P1 amide group, different 1-cycloalkenyls and 2-aryls were studied in the place of the P1 pyrrolidine group of a 4-phenylbutanoyl-l-Pro-pyrrolidine structure, which is a well-known prolyl oligopeptidase inhibitor SUAM-1221. The

Condensation of α-Amino Acid with Amine in the Absence of a Coupling Agent

Treatment of N-(4-nitrophenoxycarbonyl)amino acid with an equimolar amount of amine in the absence of a coupling agent gave the corresponding α-amino acid amide in high yield.

Analgesic dipeptide amides and method of use and compositions thereof

A genus of dipeptide amides including as the preferred subgenus the dipeptide amides having the structural formula R1 TyrProNR4 R5 wherein R1 is hydrogen or alkyl, R4 is phenylalkyl or substituted-phe