56979-57-8

Upstream product

• 672-13-9 2-hydroxy-5-methoxybenzaldehyde 
• 100-44-7 benzyl chloride 
• 100-39-0 benzyl bromide 
• 150-76-5 4-methoxy-phenol 

Downstream Products

• 35485-40-6 1-Benzyloxy-4-methoxy-2-((E)-2-nitro-propenyl)-benzene 
• 29969-31-1 1-Benzyloxy-4-methoxy-2-((E)-2-nitro-vinyl)-benzene 
• 123973-80-8 2-<1-(2-benzyloxy-5-methoxyphenyl)propen-3-yl>-2-methyl-1,3-dithiane 
• 117839-00-6 2-Acetoxy-2-(2-benzyloxy-5-methoxyphenyl)acetonitrile 
• 56979-62-5 Ethyl 2-(2-benzyloxy-5-methoxyphenyl)-2-hydroxyacetate 
• 215807-45-7 1-(tert-Butoxycarbonylamino)-7-[hydroxy(2-benzyloxy-5-methoxyphenyl)methyl]-1H-benzotriazole 
• 214072-73-8 (2-(benzyloxy)-5-methoxyphenyl)methanol 
• 888710-40-5 (E)-3-(2-Benzyloxy-5-methoxy-phenyl)-propenal 
• 939985-84-9 N-(tert-butoxycarbonyl)-2-[2-(3-butynyl-1-oxy)-5-methoxyphenyl]ethylamine 
• 939985-85-0 5-{4-[2-(2-(tert-butoxycarbonylamino)ethyl)-4-methoxyphenoxy]but-1-ynyl}-5'-O-benzoyl-2',3'-didehydro-2',3'-dideoxyuridine 
• 939985-86-1 5-{4-[(2-((5-bromo-2-pyridinyl)aminothiocarbonylamino)-ethyl)-4-methoxyphenoxy]but-1-ynyl}-5'-O-benzoyl-2',3'-didehydro-2',3'-dideoxyuridine 
• 939985-82-7 N-(tert-butoxycarbonyl)-2-(2-benzyloxy-5-methoxyphenyl)ethylamine 
• 939985-83-8 tert-butyl N-[2-(2-hydroxy-5-methoxyphenyl)ethyl]-carbamate 
• 74516-59-9 2-<2-Benzyloxy-5-methoxy-phenyl>-aethylamin 

Relevant academic research and scientific papers

Chromen-based TNF-α converting enzyme (TACE) inhibitors: Design, synthesis, and biological evaluation

A series of coumarin types MMP inhibitors were designed based on gelastatin hydroxamates (1) and evaluated for TACE, cellular TNF-α, and NO inhibitory activities. Among them, compounds 9b had potent inhibitory activities in enzymatic and cellular assays a

Design, synthesis, and evaluation of dihydropyranopyrazole derivatives as novel pde2 inhibitors for the treatment of alzheimer’s disease

Phosphodiesterase 2 (PDE2) has been regarded as a novel target for the treatment of Alz-heimer’s disease (AD). In this study, we obtained (R)‐LZ77 as a hit compound with moderate PDE2 inhibitory activity (IC50 = 261.3 nM) using a high‐throughput virtual screening method based on molecular dynamics. Then, we designed and synthesized 28 dihydropyranopyrazole derivatives as PDE2 inhibitors. Among them, compound (+)‐11h was the most potent PDE2 inhibitor, with an IC50 value of 41.5 nM. The molecular docking of PDE2‐(+)‐11h reveals that the 4‐(trifluoromethyl)ben-zyl)oxyl side chain of the compound enters the H‐pocket and forms strong hydrophobic interactions with L770/L809/F862, which improves inhibitory activity. The above results may provide insight for further structural optimization of highly potent PDE2 inhibitors and may lay the foundation for their use in the treatment of AD.

4-(2,4-BIS(2-HYDROXYPHENYL)-1H-IMIDAZOL-1-YL)BENZOIC ACID DERIVATIVES AS NOVEL IRON CHELATORS

The invention relates to novel compounds of the general formula (I) pharmaceutical compositions comprising them and the use thereof as medicaments, in particular for the use as iron chelators, more particularly for the use in the prophylaxis and/or treatm

Functionalization at Will of Rim-Differentiated Pillar[5]arenes

The development of an efficient synthetic route toward rim-differentiated C5-symmetric pillar[5]arenes (P[5]s), whose two rims are decorated with different chemical functionalities, opens up successive transformations of this macrocyclic scaffo

Syntheses and anti-inflammatory activity of natural 1,3-diarylpropenes

First syntheses of five natural 1,3-diarylpropenes (cinnamylphenols) 2-4, 7, and 8 along with synthesis of two other natural 1,3-diarylpropenes 1 and 5 and E-isomer of mucronulastyrene (6) were achieved by Friedel- Crafts alkylation as a key step. Subsequ

A novel series of 6-substituted 3-(pyrrolidin-1-ylmethyl)chromen-2-ones as selective monoamine oxidase (MAO) A inhibitors

A series of 6-substituted 3-(pyrrolidin-1-ylmethyl)chromen-2-ones (coumarins) have been synthesized and their inhibitory activity to human monoamine oxidase A (MAO A) and B (MAO B) determined. Incorporation of a basic amino function in the C3 position together with substitution at the C6 position produced novel coumarin compounds with selectivity for the MAO A subtype. Substitution in the C6 position with small hydrophilic groups such as hydroxy (19, IC50 = 1.46 μM) or amino (18, IC50 = 3.77 μM) gave the most potent and selective compounds for MAO A. These compounds also showed excellent aqueous solubility properties. Compound 18 [6-amino-3- (pyrrolidin-1-ylmethyl)chromen-2-one] administrated in vivo induced in rat brain a neurotransmitter metabolite profile typical of MAO A inhibition: decreased 3,4-dihydroxyphenylacetic acid (DOPAC) and 5-hydroxyindoleacetic acid (5-HIAA) but increased 3-methoxytyramine (3-MT) levels.

Total synthesis of plagiochin G and derivatives as potential cancer chemopreventive agents

A new and efficient total synthesis has been developed to obtain plagiochin G (22), a macrocyclic bisbibenzyl, and four derivatives. The key 16-membered ring containing biphenyl ether and biaryl units was closed via an intramolecular SNAr reaction. All synthesized macrocyclic bisbibenzyls inhibited Epstein-Barr virus early antigen (EBV-EA) activation induced by the tumor promoter 12-O-tetradecanoylphorbol-13-acetate (TPA) in Raji cells and, thus, are potential cancer chemopreventive agents.

Development of substituted N-[3-(3-methoxylphenyl)propyl] amides as MT 2-selective melatonin agonists: Improving metabolic stability

A series of novel and selective N-[3-(6-benzyloxy-3-methoxyphenyl)propyl] amides has recently been shown to possess sub-nanomolar range binding affinity to the type 2 melatonin receptor (MT2). Pharmacokinetics studies suggested that these compounds were subject to vigorous CYP450-mediated metabolism, resulting in a series of metabolites with significantly decreased or diminished binding affinities toward MT2 receptor. The ether bonds were found to be the major positions susceptible to metabolism. In this study, the benzyl ether bond was either removed or replaced with a carbon-carbon bond in an attempt to improve metabolic stability and enhance their resistance towards phase I oxidation. The synthesis, receptor binding affinity, intrinsic potency and metabolic stability of modified structures are reported in this article. By removal or replacement of metabolic labile ether linkerage with carbon linkers, a novel compound was identified with good potency and MT 2 selectivity, and with increased metabolic stability.

Multidimensional optimization of promising antitumor xanthone derivatives

A promising antitumor xanthone derivative was optimized following a multidimensional approach that involved the synthesis of 17 analogues, the study of their lipophilicity and solubility, and the evaluation of their growth inhibitory activity on four human tumor cell lines. A new synthetic route for the hit xanthone derivative was also developed and applied for the synthesis of its analogues. Among the used cell lines, the HL-60 showed to be in general more sensitive to the compounds tested, with the most potent compound having a GI50 of 5.1 μM, lower than the hit compound. Lipophilicity was evaluated by the partition coefficient (Kp) of a solute between buffer and two membrane models, namely liposomes and micelles. The compounds showed a log Kp between 3 and 5 and the two membrane models showed a good correlation (r2 = 0.916) between each other. Studies concerning relationship between solubility and structure were developed for the hit compound and 5 of its analogues.

Synthesis of dibenzoxepine lactams via a Cu-catalyzed one-pot etherification/aldol condensation cascade reaction: Application toward the total synthesis of aristoyagonine

A general synthesis of dibenzoxepine lactams has been developed using a one-pot Cu-catalyzed etherification/aldol condensation cascade reaction. The reaction of 4-hydroxyisoindolin-1-one with a wide range of 2-bromobenzaldehydes in the presence of a copper catalyst provided various aristoyagonine derivatives in good yields.