440320-88-7

Upstream product

• 13033-84-6 D-phenylalanine methyl ester hydrochloride 
• 5267-64-1 (R)-2-amino-3-phenylpropanol 
• 76-83-5 trityl chloride 
• 673-06-3 D-(R)-phenylalanine 

Downstream Products

• 1226859-80-8 4-[4R-5-phenyl-4-(trityl-amino)-pent-2-enyl]-piperidine-1-carboxylic acid tert-butyl ester 
• 790223-81-3 4-[5-phenyl-4-(tritylamino)pent-2-enyl]piperidine-1-carboxylic acid tert-butyl ester 
• 484051-36-7 (2R,1'R)-N-(1'-benzyl-prop-2'-enyl)-N-[(2,4-dimethoxyphenyl)methyl]-2-benzyl-but-3-enamide 
• 484051-40-3 (3R,6R)-N-[(2,4-dimethoxyphenyl)methyl]-3,6-dibenzyl-3,6-dihydro-2-pyridone 
• 484051-32-3 (2R,1'R)-N-(1'-benzyl-prop-2'-enyl)-N-[(2,4-dimethoxyphenyl)methyl]-2-isopropyl-but-3-enamide 
• 484051-42-5 (3R,6R)-N-[(2,4-dimethoxyphenyl)methyl]-3-isopropyl-6-benzyl-3,6-dihydro-2-pyridone 
• 484051-51-6 (3R,6R)-3,6-dibenzyl-2-ethoxy-3,6-dihydropyridine 
• 214072-07-8 (3R,6R)-3,6-dibenzyl-3,6-dihydro-2-pyridone 
• 484051-53-8 (3R,6R)-3-isopropyl-6-benzyl-2-ethoxy-3,6-dihydropyridine 
• 484051-48-1 (3R,6R)-3-isopropyl-6-benzyl-3,6-dihydro-2-pyridone 
• 756462-76-7 (R)-1-benzyl-prop-2-enylamine 

Relevant academic research and scientific papers

Peptidotriazolamers Inhibit Aβ(1–42) Oligomerization and Cross a Blood-Brain-Barrier Model

In peptidotriazolamers every second peptide bond is replaced by a 1H-1,2,3-triazole. Such foldamers are expected to bridge the gap in molecular weight between small-molecule drugs and protein-based drugs. Amyloid β (Aβ) aggregates play an important role in Alzheimer's disease. We studied the impact of amide bond replacements by 1,4-disubstituted 1H-1,2,3-triazoles on the inhibitory activity of the aggregation “hot spots” K16LVFF20 and G39VVIA42 in Aβ(1–42). We found that peptidotriazolamers act as modulators of the Aβ(1–42) oligomerization. Some peptidotriazolamers are able to interfere with the formation of toxic early Aβ oligomers, depending on the position of the triazoles, which is also supported by computational studies. Preliminary in vitro results demonstrate that a highly active peptidotriazolamer is also able to cross the blood-brain-barrier.

NK-2 ANTAGONIST BASIC LINEAR COMPOUNDS AND FORMULATIONS CONTAINING THEM

The present invention describes compounds with formula (I) having linear structure basic properties useful as NK-2 antagonists; pharmaceutical compositions containing said compounds are also described and processes for their preparation.

An access to (Z)-ethylenic pseudodipeptides based on ring-closing metathesis

A new access to enantiopure (Z)-ethylenic pseudopeptides, starting from the chiral pool of amino acids and enantiopure 2-substituted-but-3-enoic acids is proposed and illustrated by the syntheses of the (Z)-ethylenic pseudopeptidic analogs of L-Phe-L-Phe, L-Phe-D-Phe, L-Phe-L-Val, L-Phe-D-Val and racemic (LL,DD) and (LD,DL) (phenyl)Gly-Phe. The key-steps of these syntheses are a ring-closing metathesis, catalysed by Grubbs' ruthenium alkykidene complexes, on diethylenic amides and the hydrolytic cleavage of the resulting dihydropyridones under mild conditions through intermediate formation of cyclic imidates.