203926-74-3

Upstream product

• 2105-94-4 4-bromo-2-fluorophenol 
• 18162-48-6 tert-butyldimethylsilyl chloride 

Downstream Products

• 1234665-62-3 C₁₆H₂₅FO₂Si 

Relevant academic research and scientific papers

Utilizing PROTAC technology to address the on-target platelet toxicity associated with inhibition of BCL-X

BCL-XL, an anti-apoptotic BCL-2 family protein, plays a key role in cancer cell survival. However, the potential of BCL-XL as an anti-cancer target has been hampered by the on-target platelet toxicity because platelets depend on BCL-XL to maintain their viability. Here we report the development of a PROTAC BCL-XL degrader, XZ424, which has increased selectivity for BCL-XL-dependent MOLT-4 cells over human platelets compared with conventional BCL-XL inhibitors. This proof-of-concept study demonstrates the potential of utilizing a PROTAC approach to achieve tissue selectivity.

Development of structurally extended benzosiloxaboroles - synthesis andin vitrobiological evaluation

The synthesis of potassium 6-hydroxy-7-chloro-1,1-dimethyl-3,3-difluorobenzo-1,2,3-siloxaborolate5bfrom readily available 4-bromo-2-chlorophenol was developed. This compound proved useful in various derivatizations resulting in a wide range ofO-functionalized benzosiloxaboroles. Reactions of5bwith selected substituted benzoyl chlorides gave rise to a series of respective derivatives with 6-benzoate side groups attached to the benzosiloxaborole core. Furthermore, treatment of5bwith substituted benzenesufonyl chlorides afforded several benzosiloxaboroles bearing functionalized benzenesulfonate moieties at the 6 position. The synthesis of related chloropyridine-2-yloxy substituted benzosiloxaboroles was accomplished by a standard approach involving silylation/boronation of appropriate heterodiaryl ethers. Investigation of biological activity of obtained compounds revealed that some benzoate and most benzenesulfonate derivatives exhibit high activity against Gram-positive cocci such as methicillin-sensitiveStaphylococcus aureusATCC 6538P as well as methicillin-resistantS. aureusATCC 43300 with the MIC values in the range of 0.39-3.12 mg L?1. Some benzenesulfonate derivatives showed also potent activity againstEnterococcus faecalisATCC 29212 andE. faeciumATCC 6057 with MIC = 6.25 mg L?1. Importantly, for the most promising cocci-active benzenesulfonate derivatives the obtained MIC values were far below the cytotoxicity limit determined with respect to human normal lung fibroblasts (MRC-5). For those derivatives, the obtained IC50values were higher than 12.3 mg L?1. The results of antimicrobial activity and cytotoxicity indicate that the tested compounds can be considered as potential antibacterial agents.

THERAPEUTIC COMPOUNDS AND USES THEREOF

The present invention relates to compounds useful in the modulation of ion channel activity in cells. The invention also relates to use of these compounds in the treatment of pain, and pharmaceutical compositions containing these compounds and methods for their preparation.

COMPOUNDS THAT INDUCE DEGRADATION OF ANTI-APOPTOTIC BCL-2 FAMILY PROTEINS AND THE USES THEREOF

The present disclosure provides compositions and methods for selectively killing senescent cells, wherein the composition comprises a compound of Formula (I) or a compound of Formula (II). The selective killing of senescent cells may delay aging and/or treat age-related disorders.

PREPARING AN UNSATURATED CARBOXYLIC ACID SALT FROM AN ALKENE AND CARBON DIOXIDE USING A HETEROGENEOUS BASE

Process for preparing an α,β-ethylenically unsaturated carboxylic acid salt, comprising, reacting an alkene and carbon dioxide in the presence of a carboxylation catalyst to obtain a catalyst-coordinated carboxylated intermediate, treating the catalyst- c

2-PYRIDONE COMPOUNDS

A 2-pyridone compound represented by the formula [1]: {wherein in the formula [1], the ring represented by A represents a benzene ring or a pyridine ring, X represents any of the structures represented by the formulas [3] shown below: V represents a single bond or a lower alkylene group, and W represents a single bond, an ether bond or a lower alkylene group (wherein the lower alkylene group may contain an ether bond)}, a tautomer or stereoisomer of the compound, a pharmaceutically acceptable salt thereof, or a solvate thereof is a compound that has an excellent GK activating effect and is useful as a pharmaceutical.

Organic synthesis using a hypervalent iodine reagent: Unexpected and novel domino reaction leading to spiro cyclohexadienone lactones

The reaction of 1-(p-hydroxyaryl)cyclobutanols and phenyl iodide(iii) diacetate in hexafluoroisopropanol and water produced spiro cyclohexadienone lactones via a domino reaction.

Benzo [B] thiophene compounds, and compositions for treating bone loss, and hyperlipidemia

The invention provides benzo[b]thiophene compounds, formulations, and methods of inhibiting bone loss or bone resorption, particularly osteoporosis, and cardiovascular-related pathological conditions including hyperlipidemia and related cardiovascular pat

Benzo[B]thiophene compounds, intermediates, processes, compositions, and methods

The invention provides benzo[b]thiophene compounds, formulations, and methods of inhibiting bone loss or bone resorption, particularly osteoporosis, and cardiovascular-related pathological conditions including hyperlipidemia and related cardiovascular pat