477860-13-2

Upstream product

• 634192-51-1 2-fluoro-4-methoxy-1,1'-biphenyl 
• 121219-03-2 4-bromo-3-fluorophenol 
• 98-80-6 phenylboronic acid 
• 41604-19-7 1-bromo-3-fluoro-4-phenylbenzene 
• 37847-52-2 2,4-difluorobiphenyl 
• 550998-23-7 trifluoromethanesulfonic acid 2-fluoro-4-methoxyphenyl ester 
• 167683-93-4 2-fluoro-4-methoxy-phenol 
• 2105-94-4 4-bromo-2-fluorophenol 
• 122927-84-8 3-fluoro-4-iodophenol 
• 178305-99-2 (2-fluoro-[1,1'-biphenyl]-4-yl)boronic acid 

Relevant academic research and scientific papers

(4-HYDROXYPYRROLIDIN-2-YL)-HYDROXAMATE COMPOUNDS AND METHODS OF USE THEREOF

The present disclosure relates to bifunctional compounds, which can be used as modulators of targeted ubiquitination. In particular, the present disclosure is directed to compounds which contain on one end a VHL ligand moiety, which binds to the VHL E3 ubiquitin ligase, and on the other end a moiety that binds a target protein such that degradation of the target protein/polypeptide is effectuated. Also disclosed are VHL ligands.

Design, Synthesis, Structure-Activity Relationship Studies, and Three-Dimensional Quantitative Structure-Activity Relationship (3D-QSAR) Modeling of a Series of O-Biphenyl Carbamates as Dual Modulators of Dopamine D3 Receptor and Fatty Acid Amide Hydrolase

We recently reported molecules designed according to the multitarget-directed ligand paradigm to exert combined activity at human fatty acid amide hydrolase (FAAH) and dopamine receptor subtype D3 (D3R). Both targets are relevant for tackling several types of addiction (most notably nicotine addiction) and other compulsive behaviors. Here, we report an SAR exploration of a series of biphenyl-N-[4-[4-(2,3-substituted-phenyl)piperazine-1-yl]alkyl]carbamates, a novel class of molecules that had shown promising activities at the FAAH-D3R target combination in preliminary studies. We have rationalized the structural features conducive to activities at the main targets and investigated activities at two off-targets: dopamine receptor subtype D2 and endocannabinoid receptor CB1. To understand the unexpected affinity for the CB1 receptor, we devised a 3D-QSAR model, which we then prospectively validated. Compound 33 was selected for PK studies because it displayed balanced affinities for the main targets and clear selectivity over the two off-targets. 33 has good stability and oral bioavailability and can cross the blood-brain barrier.

NOVEL NUCLEOSIDE PHOSPHORAMIDATE COMPOUND AND USE THEREOF

The present invention provides a novel nucleoside phosphoramidate compound, or a stereoisomer, salt, hydrate, solvate or crystal thereof for the treatment of Flaviviridae family viral infection, especially hepatitis C viral infection. The present invention also provides the pharmaceutical composition comprising a compound of the present invention, or a stereoisomer, salt, hydrate, solvate or crystal thereof and a use of the compound or the composition of the present invention in the treatment of Flaviviridae family viral infection, especially hepatitis C viral infection. The compound of the present invention has a good anti-HCV effect.

The first general route for efficient synthesis of 18O labelled alcohols using the HOF·CH3CN complex

A mild and very efficient method for converting boronic acids to alcohols has been developed using the acetonitrile complex of hypofluorous acid HOF·CH3CN. Employing 18O-labeled water results in alcohols containing a heavy oxygen isotope. The reactions were performed at room temperature, within a few minutes and in excellent yields.

Thieme journal awardees - Where are they now? on cobalt-catalyzed biaryl coupling reactions

An operationally simple biaryl coupling reaction has been developed. The underlying domino process involves in situ Grignard formation from aryl bromides and subsequent homocoupling with catalytic CoCl2 and 1 bar synthetic air as terminal oxidant. Georg Thieme Verlag Stuttgart.

Preparation of monofluorophenols via the reaction of difluorobenzene derivatives with potassium trimethylsilanoate

An efficient synthesis of monofluorophenols via the reaction of difluorobenzene derivatives with potassium trimethylsilanoate in moderate to excellent yields is described. High regioselectivity was observed in some cases. Georg Thieme Verlag Stuttgart.

ERbeta ligands. Part 1: the discovery of ERbeta selective ligands which embrace the 4-hydroxy-biphenyl template.

The synthesis and structure-activity relationships of a series of simple biphenyls is described. Optimization of the 4-hydroxy-biphenyl template led to compounds with ERbeta selectivity on the order of 20-70-fold.