352288-39-2

Upstream product

• 13329-40-3 4-Iodoacetophenone 
• 352288-23-4 ethyl (E)-3-(4-iodophenyl)but-2-enoate 

Downstream Products

• 516517-66-1 ethyl (E,E)-(S,S)-3-{4-[3-(4'-{4-(4-(2-ethoxy-2-ethoxycarbonylethyl)phenoxy)but-2-en-2-yl}biphenyl-4-yl)but-2-en-1-yloxy]phenyl}-2-ethoxypropanoate 
• 630110-17-7 ethyl (E,E)-(S)-3-{4-[3-(4'-{4-[tert-butyldimethylsilyloxy]but-2-en-2-yl}biphenyl-4-yl)but-2-en-1-yloxy]phenyl}-2-ethoxypropanoate 
• 516518-53-9 ethyl (E,E)-(S)-3-{4-[3-(4'-{4-hydroxybut-2-en-2-yl}biphenyl-4-yl)but-2-en-1-yloxy]phenyl}-2-ethoxypropanoate 

Relevant academic research and scientific papers

Ir-Catalyzed Asymmetric Allylic Alkylation of Dialkyl Malonates Enabling the Construction of Enantioenriched All-Carbon Quaternary Centers

An enantioselective iridium-catalyzed allylic alkylation of malonates with trisubstituted allylic electrophiles to form all-carbon quaternary stereocenters is reported. This reaction proceeds at ambient temperature and enables the preparation of a wide range of enantioenriched products in up to 93% yield and 97% ee. The quaternary products can be readily converted to several valuable building blocks such as vicinal quaternary products and β-quaternary acids.

Large Dimeric Ligands with Favorable Pharmacokinetic Properties and Peroxisome Proliferator-Activated Receptor Agonist Activity in Vitro and in Vivo

Two potent nonselective, but PPARα-preferring, PPAR agonists 5 and 6 were designed and synthesized in high yields. The concept of dimeric ligands in transcription factors was investigated by synthesizing and testing the corresponding dimers 7, 8a, and 8b in PPAR transactivation assays. The three dimeric ligands all showed agonist activity on all three PPAR receptor subtypes, but with different profiles compared to the monomers 5 and 6. Despite breaking all the "rule of five" criteria, the dimers had excellent oral bioavailability and pharmacokinetic properties, resulting in good in vivo efficacy in db/db mice. X-ray crystal structure and modeling experiments suggested that the dimers interacted with the AF-2 helix as well as with amino acid residues in the lipophilic pocket close to the receptor surface.

Novel compounds, their preparation and use

A novel class of dicarboxylic acid derivatives, the use of these compounds as pharmaceutical compositions, pharmaceutical compositions comprising the compounds and methods of treatment employing these compounds and compositions. The present compounds may be useful in the treatment and/or prevention of conditions mediated by Peroxisome Proliferator-Activated Receptors (PPAR).

Compounds, their preparation and use

The present invention relates to compounds of the general formula (I) The compounds are useful in the treatment and/or prevention of conditions mediated by nuclear receptors, in particular the Peroxisome Proliferator-Activated Receptors (PPAR).