96013-95-5

Upstream product

• 18162-48-6 tert-butyldimethylsilyl chloride 
• 100-83-4 meta-hydroxybenzaldehyde 
• 288-32-4 1H-imidazole 
• 41879-37-2 t-butyldimethylsilyl amine 
• 96013-69-3 tert-butyl((3-((tert-butyldimethylsilyl)oxy)benzyl)oxy)dimethylsilane 

Downstream Products

• 147594-02-3 (E)-ethyl α-<<3-<(1,1-dimethylethyl)dimethylsiloxy>phenyl>methylene>-4,5-diphenyl-2-oxazoleacetate 
• 147594-03-4 (Z)-ethyl α-<<3-<(1,1-dimethylethyl)dimethylsiloxy>phenyl>methylene>-4,5-diphenyl-2-oxazoleacetate 
• 96013-77-3 3-(tert-butyldimethylsilyloxy)benzyl alcohol 
• 174415-62-4 α-(3-((tert-butyldimethylsilyl)oxy)phenyl)-6-bromo-3-pyridinemethanol 
• 174647-43-9 (+/-)-1-hydroxy-1-<3-(tert-butyldimethylsilyloxy)phenyl>-2-phenyl-2-(1,3-dithian-2-yl)ethane 
• 566899-16-9 [3-(tert-butyl-dimethyl-silanyloxy)-phenyl]-(3-methoxy-phenyl)-methanol 
• 479495-43-7 (E)-(S)-4-[3-(tert-Butyl-dimethyl-silanyloxy)-phenyl]-2-methyl-but-3-en-1-ol 
• 149274-04-4 tert-butyldimethyl-(3-vinylphenoxy)silane 
• 441799-14-0 1-(3-((t-butyldimethylsilyl)oxy)phenyl)prop-2-yn-1-ol 
• 179381-04-5 1-[3-(tert-Butyldimethylsilanyloxy)phenyl]propan-1-ol 
• 254753-54-3 (-)-4-(3-hydroxyphenyl)-6-methyl-2-thioxo-1,2,3,4-tetrahydropyrimidine-5-carboxylic acid ethyl ester 
• 254753-54-3 (S)-monastrol 
• 945657-71-6 (Z)-3-(tert-butyldimethylsilyloxy)-4'-methoxystilbene 
• 877438-70-5 (8R,8'R)-3,3'-bis(tert-butyldimethylsilanyloxy)-7'-(propane-1,3-diyldithio)lignano-9,9'-lactone 

Relevant academic research and scientific papers

Chromium-Salen Complex/Nitroxyl Radical Cooperative Catalysis: A Combination for Aerobic Intramolecular Dearomative Coupling of Phenols

We describe an aerobic intramolecular dearomative coupling reaction of tethered phenols using a catalytic system consisting of a chromium-salen (Cr-salen) complex combined with a nitroxyl radical. This novel catalytic system enables formation of various spirocyclic dienone products including those unable to be accessed by previously reported methods efficiently under mild reaction conditions.

Synthesis process of AMPPD

The invention relates to the technical field of organic synthesis, in particular to a synthesis process of AMPPD. The synthesis process of AMPPD comprises the following steps: reacting an intermediate with molybdate in an organic solvent to form a product

ANTIVIRAL 1,3-DI-OXO-INDENE COMPOUNDS

The invention provides compounds of Formula (I): as described herein, along with pharmaceutically acceptable salts, pharmaceutical compositions containing such compounds, and methods to use these compounds, salts and compositions for treating viral infections.

Discovery and Development of S6821 and S7958 as Potent TAS2R8 Antagonists

In humans, bitter taste is mediated by 25 TAS2Rs. Many compounds, including certain active pharmaceutical ingredients, excipients, and nutraceuticals, impart their bitter taste (or in part) through TAS2R8 activation. However, effective TAS2R8 blockers that can either suppress or reduce the bitterness of these compounds have not been described. We are hereby reporting a series of novel 3-(pyrazol-4-yl) imidazolidine-2,4-diones as potent and selective TAS2R8 antagonists. In human sensory tests, S6821 and S7958, two of the most potent analogues from the series, demonstrated efficacy in blocking TAS2R8-mediated bitterness and were selected for development. Following data evaluation by expert panels of a number of national and multinational regulatory bodies, including the US, the EU, and Japan, S6821 and S7958 were approved as safe under conditions of intended use as bitter taste blockers.

Small Molecule Inhibitors of the BfrB-Bfd Interaction Decrease Pseudomonas aeruginosa Fitness and Potentiate Fluoroquinolone Activity

The iron storage protein bacterioferritin (BfrB) is central to bacterial iron homeostasis. The mobilization of iron from BfrB, which requires binding by a cognate ferredoxin (Bfd), is essential to the regulation of cytosolic iron levels in P. aeruginosa. This paper describes the structure-guided development of small molecule inhibitors of the BfrB-Bfd protein-protein interaction. The process was initiated by screening a fragment library and followed by obtaining the structure of a fragment hit bound to BfrB. The structural insights were used to develop a series of 4-(benzylamino)- A nd 4-((3-phenylpropyl)amino)-isoindoline-1,3-dione analogs that selectively bind BfrB at the Bfd binding site. Challenging P. aeruginosa cells with the 4-substituted isoindoline analogs revealed a dose-dependent growth phenotype. Further investigation determined that the analogs elicit a pyoverdin hyperproduction phenotype that is consistent with blockade of the BfrB-Bfd interaction and ensuing irreversible accumulation of iron in BfrB, with concomitant depletion of iron in the cytosol. The irreversible accumulation of iron in BfrB prompted by the 4-substituted isoindoline analogs was confirmed by visualization of BfrB-iron in P. aeruginosa cell lysates separated on native PAGE gels and stained for iron with Ferene S. Challenging P. aeruginosa cultures with a combination of commercial fluoroquinolone and our isoindoline analogs results in significantly lower cell survival relative to treatment with either antibiotic or analog alone. Collectively, these findings furnish proof of concept for the usefulness of small molecule probes designed to dysregulate bacterial iron homeostasis by targeting a protein-protein interaction pivotal for iron storage in the bacterial cell.

SMALL MOLECULE INHIBITORS OF THE BFRB:BFD INTERACTION

The present technology provides compounds of Formula I and related methods for treating a bacterial infection as well as methods for inhibiting interaction of a bacterioferritin and a bacterioferritin-associated ferredoxin.

INHIBITORS OF BRUTON'S TYROSINE KINASE AND METHODS OF THEIR USE

The present disclosure is directed to compounds of Formula (I) and methods of their use and preparation, as well as compositions comprising compounds of Formula (I).

INHIBITORS OF BRUTON'S TYROSINE KINASE AND METHODS OF THEIR USE

Compounds of formula (I') and methods of their use and preparation, as well as compositions comprising compounds of formula (I').

A convenient synthesis of a lymphocyte function-associated antigen-1 (LFA-1) antagonist of 'Compound 4'

The lymphocyte function-associated antigen-1 (LFA-1) antagonist of 'Compound 4' was synthesised by a convenient route using cheap, commercially available starting materials and catalysts under mild reaction conditions and by easily handled reactions. The total yield in the preparation of 'Compound 4' was more than 38% via Sonogashira coupling of an iodide and an alkyne, reduction of the alkyne catalysed by Raney nickel and later steps involving hydrolysis of an ester, condensation of an acid and an amine and a final hydrolysis of an ester.

Photocontrolled Release of Chemicals from Nano- and Microparticle Containers

A benzoin-derived diol linker was synthesized and used to generate biocompatible polyesters that can be fully decomposed on demand upon UV irradiation. Extensive structural optimization of the linker unit was performed to enable the defined encapsulation of diverse organic compounds in the polymeric structures and allow for a well-controllable polymer cleavage process. Selective tracking of the release kinetics of encapsulated model compounds from the polymeric nano- and microparticle containers was performed by confocal laser scanning microscopy in a proof-of-principle study. The physicochemical properties of the incorporated and released model compounds ranged from fully hydrophilic to fully hydrophobic. The demonstrated biocompatibility of the utilized polyesters and degradation products enables their use in advanced applications, for example, for the smart packaging of UV-sensitive pharmaceuticals, nutritional components, or even in the area of spatially selective self-healing processes.