1022893-17-9

Upstream product

• 7170-36-7 6-(methoxycarbonyl)pyridine-2-carboxylic acid 
• 5453-67-8 2,6-bis(methoxycarbonyl)pyridine 
• 3886-69-9 (R)-1-phenyl-ethyl-amine 
• 499-83-2 Pyridine-2,6-dicarboxylic acid 

Downstream Products

• 1022892-99-4 C₃₂H₃₀N₈O₄ 

Relevant academic research and scientific papers

A light triggered optical and chiroptical switch based on a homochiral Eu2L3helicate

Optical and chiroptical photoswitches have found potential applications in advanced information technologies. Herein, a pair of chiral triple-stranded helicates [Eu2(o-LRR)3](TOf)6and [Eu2(o-LSS)3](TOf)6, which have chirality, luminescence and light stimuli-responsive properties, have been designed and synthesized. The ligands o-LRR/SSare composed of photochromic diarylethene moieties as spacers and two chiral 2,6-dipicolinic amides as coordination units. Through the comprehensive spectral characteristics in combination with semiempirical geometry optimization using the Sparkle/RM1 model, it was confirmed that (R/S)-1-phenylethanamines decorated at the terminals of ligands successfully controlled the stereoselective self-assembly of the helicates. Upon alternating UV and visible light irradiation, the diarylethene experienced a reversible change between a colorless open-ring state and a pink closed-ring state. This photochromic process caused variations in the electronic structure and ligand conformation, and led to the presence of light-responsive optical (UV and PL) and chiroptical (ECD and CPL) switching properties. The helicate may, therefore, be considered as a completely reversible +/- ECD and on/off CPL switch. Furthermore, on the basis of these light-switchable optical properties, the INHIBIT and IMPLICATION logic gates were fabricated.

Lanthanide supramolecular helical diastereoselective breaking induced by point chirality: Mixture or P-helix, M-helix

The self-assembly of lanthanide (europium or lanthanium) bimetallic triple helicates from two closely related chiral ligands resulted in a very different supramolecular phenomenon. One gave rise to significantly diastereoselective formation of a triple helicate, whereas the other led to diastereoselective breaking to generate a mixture of P and M diastereomers in ～1 : 1.1 ratio. The first X-ray crystal structure of a chiral ligand based lanthanide triple-helicate indicates that successive CH-π interactions were found to maintain the supramolecular helical structure. This journal is

NOVEL COMPOUND HAVING SECRETASE INHIBITORY ACTIVITY

A novel compound represented by the formula (1) below which has β-secretase inhibitory activity, its pharmaceutically acceptable salt or a prodrug thereof. wherein Ar is a substituted or unsubstituted 5 to 6 membered mono cyclic aromatic group; R1, R2 and R3 are hydrogen atom, substituted or unsubstituted alkyl group or the like, or R2 and R3 may be taken together with the adjacent nitrogen atom and carbon atom respectively to form a 3 to 6 membered ring; R4 is C1-6 alkyl group, C1-6 alkyl group substituted by phenyl, phenylthio, or a hetero ring, or the like; A is represented by the formula below: wherein X and Y are oxygen atom, NH or sulfur atom, Z is hydrogen atom, hydroxy group which may be substituted, amino group, thiol group, or the like; and B is hydroxy group, substituted or unsubstituted amino group, substituted or unsubstituted aliphatic or aromatic amino group, or the like.

Novel non-peptidic and small-sized BACE1 inhibitors

Recently, we reported substrate-based β-secretase (BACE1) inhibitors with a hydroxymethylcarbonyl (HMC) isostere as a substrate transition-state mimic. These inhibitors showed potent BACE1 inhibitory activities (～1.2 nM IC50). In order to improve in vivo enzymatic stability and permeability across the blood-brain barrier, these penta-peptidic inhibitors would need to be further optimized. On the other hand, non-peptidic inhibitors possessing isophthalic residue at the P2 position were reported from other research groups. We selected isophthalic-type aromatic residues at the P2 position and an HMC isostere at the P1 position as lead compounds. On the basis of the design approach focused on the conformer of docked inhibitor in BACE1, we found novel non-peptidic and small-sized BACE1 inhibitors possessing a 2,6-pyridinedicarboxylic, chelidamic or chelidonic residue at the P2 position.