852227-96-4

Usage

Uses

4-(1-Piperidinyl)benzeneboronic acid pinacol ester is used as pharmaceutical intermediate.

InChI:InChI=1/C17H26BNO2/c1-16(2)17(3,4)21-18(20-16)14-8-10-15(11-9-14)19-12-6-5-7-13-19/h8-11H,5-7,12-13H2,1-4H3

Upstream product

• 76-09-5 2,3-dimethyl-2,3-butane diol 
• 4280-36-8 (4-fluorophenyl)piperidine 
• 73183-34-3 bis(pinacol)diborane 
• 22148-20-5 N-(4-bromophenyl)piperidine 

Downstream Products

• 1565835-37-1 2,5-dioxopyrrolidin-1-yl 5-(4-(piperidin-1-yl)phenyl)-thiophene-2-carboxylate 
• 1565835-39-3 2,5-dioxopyrrolidin-1-yl 5'-(4-(piperidin-1-yl)phenyl)-2,2'-bithiophene-5-carboxylate 
• 1152616-61-9 C₂₁H₁₉F₃N₄ 

Relevant academic research and scientific papers

Photo-induced thiolate catalytic activation of inert Caryl-hetero bonds for radical borylation

Substantial effort is currently being devoted to obtaining photoredox catalysts with high redox power. Yet, it remains challenging to apply the currently established methods to the activation of bonds with high bond dissociation energy and to substrates with high reduction potentials. Herein, we introduce a novel photocatalytic strategy for the activation of inert substituted arenes for aryl borylation by using thiolate as a catalyst. This catalytic system exhibits strong reducing ability and engages non-activated Caryl–F, Caryl–X, Caryl–O, Caryl–N, and Caryl–S bonds in productive radical borylation reactions, thus expanding the available aryl radical precursor scope. Despite its high reducing power, the method has a broad substrate scope and good functional-group tolerance. Spectroscopic investigations and control experiments suggest the formation of a charge-transfer complex as the key step to activate the substrates.

GLYCOLATE OXIDASE INHIBITORS FOR THE TREATMENT OF DISEASE

Described herein are compounds, methods of making such compounds, pharmaceutical compositions and medicaments containing such compounds, and methods of using such compounds to treat or prevent diseases or disorders associated with a defect in glyoxylate metabolism, for example a disease or disorder associated with the enzyme glycolate oxidase (GO) or alterations in oxalate metabolism. Such diseases or disorders include, for example, disorders of glyoxylate metabolism, including primary hyperoxaluria, that are associated with production of excessive amounts of oxalate.

GLYCOLATE OXIDASE INHIBITORS FOR THE TREATMENT OF DISEASE

Described herein are compounds, methods of making such compounds, pharmaceutical compositions and medicaments containing such compounds, and methods of using such compounds to treat or prevent diseases or disorders associated with the enzyme glycolate oxidase (GO). Such diseases or disorders include, for example, disorders of glyoxylate metabolism, including primary hyperoxaluria, that are associated with production of excessive amounts of oxalate.

Discovery, Optimization, and Target Identification of Novel Potent Broad-Spectrum Antiviral Inhibitors

Viral infections are increasing and probably long-lasting global risks. In this study, a chemical library was exploited by phenotypic screening to discover new antiviral inhibitors. After optimizations from hit to lead, a novel potent small molecule (RYL-634) was identified, showing excellent broad-spectrum inhibition activity against various pathogenic viruses, including hepatitis C virus, dengue virus, Zika virus, chikungunya virus, enterovirus 71, human immunodeficiency virus, respiratory syncytial virus, and others. The mechanism of action and potential targets of RYL-634 were further explored by the combination of activity-based protein profiling and other techniques. Finally, human dihydroorotate dehydrogenase was validated as the major target of RYL-634. We did not observe any mutant resistance under our pressure selections with RYL-634, and it had a strong synergistic effect with some Food and Drug Administration-approved drugs. Hence, there is great potential for developing new broad-spectrum antivirals based on RYL-634.

Catalytic aromatic borylation via in situ-generated borenium species

We have developed a catalytic direct borylation of arenes via in situ-generated borenium species. The choice of appropriate Lewis base was crucial to achieve the catalytic system. Electron-rich arenes were borylated in a regioselective manner.

SUBSTITUTED PYRIDOPYRAZINES AS SYK INHIBITORS

The present invention relates to pyridopyrazine compounds of formula (I), pharmaceutical compositions thereof and methods of use therefore, wherein R1, R2, R3, L, m, p and W are as defined in the specification.

Live cell cytoplasm staining and selective labeling of intracellular proteins by non-toxic cell-permeant thiophene fluorophores

A structurally correlated series of cell-permeant thiophene fluorophores, characterized by intense green or red fluorescence inside live mouse embryonic fibroblasts, was developed. The fluorophores displayed rapid internalization, excellent retention inside the cells, and high optical stability in the cytosolic environment and did not alter cell viability and reproducibility. Depending on the molecular structure, they experienced distinct fate inside the cells: from bright and lasting staining of the cytoplasm to selective tagging of a small set of globular proteins. This journal is The Royal Society of Chemistry 2014.

Kinase scaffold repurposing for neglected disease drug discovery: Discovery of an efficacious, lapatanib-derived lead compound for trypanosomiasis

Human African trypanosomiasis (HAT) is a neglected tropical disease caused by the protozoan parasite Trypanosoma brucei. Because drugs in use against HAT are toxic and require intravenous dosing, new drugs are needed. Initiating lead discovery campaigns b

5-PYRIDINONE SUBSTITUTED INDAZOLES

5-pyridinone substituted indazoles of the formula and methods of their use are presented.