Month: October 2022

Lee, Heajin; Landgraf, Ralf; Wilson, James N. published the artcile< Synthesis and photophysical properties of a fluorescent cyanoquinoline probe for profiling ERBB2 kinase inhibitor response>, Recommanded Product: 4-(4-Methyl-1-piperazinyl)phenylboronic Acid, the main research area is cyanoquinoline fluorescent probe preparation ERBB2 kinase inhibitor; EGFR; ERBB; Fluorescent probe; Kinase inhibitor; Receptor tyrosine kinase.

A fluorescent probe targeting the ERBB2 receptor tyrosine was designed, synthesized and evaluated as reporter of ERBB2 dynamics in overexpressing BT474, i.e. Her2(+), cells. Two cyanoquinoline (CQ) probes modeled after type-I (CQ1, I) or active state and type-II (CQ2, II) or inactive state inhibitors were designed and synthesized with extended π systems that impart binding-induced, turn-on fluorescence. Solution spectroscopy revealed that I exhibited attractive photophys. properties and displayed turn-on emission in the presence of purified, soluble ERBB2 kinase domain, while II was found to be non-emissive, likely due to quenching via a photoinduced electron transfer mechanism. Live cell imaging with I revealed that this probe targeted an intracellular population of ERBB2, which increased following treatment with type-I inhibitors, gefinitib and canertinib, but showed no response to type-II inhibitors. I thus provides a novel means of imaging the dynamic response of ERBB2(+) cells to kinase inhibitors.

Bioorganic & Medicinal Chemistrypublished new progress about Density functional theory. 229009-40-9 belongs to class piperazines, and the molecular formula is C11H17BN2O2, Recommanded Product: 4-(4-Methyl-1-piperazinyl)phenylboronic Acid.

Referemce:
Piperazine – Wikipedia,
Piperazines – an overview | ScienceDirect Topics

Nishizawa, Akihiro; Takahira, Tsuyoshi; Yasui, Kosuke; Fujimoto, Hayato; Iwai, Tomohiro; Sawamura, Masaya; Chatani, Naoto; Tobisu, Mamoru published the artcile< Nickel-Catalyzed Decarboxylation of Aryl Carbamates for Converting Phenols into Aromatic Amines>, Recommanded Product: 1-Boc-4-(4-Formylphenyl)piperazine, the main research area is phenol conversion aromatic amine nickel catalyzed decarboxylation carbamate; polystyrene supported phosphine ligand nickel catalyzed decarboxylation carbamate.

Herein, we describe a new catalytic approach to accessing aromatic amines from an abundant feedstock, namely phenols. The most reliable catalytic method for converting phenols to aromatic amines uses an activating group, such as a trifluoromethane sulfonyl group. However, this activating group is eliminated as a leaving group during the amination process, resulting in significant waste. Our nickel-catalyzed decarboxylation reaction of aryl carbamates forms aromatic amines with carbon dioxide as the only byproduct. As this amination proceeds in the absence of free amines, a range of functionalities, including a formyl group, are compatible. A bisphosphine ligand immobilized on a polystyrene support (PS-DPPBz) is key to the success of this reaction, generating a catalytic species that is significantly more active than simple nonsupported variants.

Journal of the American Chemical Societypublished new progress about Amination (decarboxylative amination). 197638-83-8 belongs to class piperazines, and the molecular formula is C16H22N2O3, Recommanded Product: 1-Boc-4-(4-Formylphenyl)piperazine.

Referemce:
Piperazine – Wikipedia,
Piperazines – an overview | ScienceDirect Topics

Bhattacharyya, Bhaswati; Dhara, Kaliprasanna published the artcile< Highly efficient, mild, one pot synthesis of 2-substituted benzimidazoles, benzothiazoles and pyridoimidazoles promoted by N-iodosuccinimide>, Recommanded Product: 1-Boc-4-(4-Formylphenyl)piperazine, the main research area is benzimidazole benzothiazole imidazopyridine preparation.

A common and highly efficient metal-free route for the synthesis of 2-substituted benzimidazoles, benzothiazoles and pyridoimidazoles from suitable 1,2- functionalized aromatic compounds and various aromatic and aliphatic aldehydes and ferrocenecarboxaldehyde was developed using 1-iodo-2,5-pyrrolidinedione, (N-iodosuccinimide) as the oxidizing agent. The methodol. involved very short reaction time, mild reaction procedure and easy work-up as well as excellent yields of the products. The synthesis of the target compounds was achieved by a reaction of 1,2-benzenediamine, 2-aminobenzenethiol, 2,3-pyridinediamine with aldehydes, such as benzaldehyde derivatives, 4-formylbenzonitrile, 1,3-benzodioxole-5-carboxaldehyde, citronellal, (formyl)ferrocene. The title compounds thus formed included 2-phenyl-1H-benzimidazole, 2-phenylbenzothiazole, (4-methyl-1H-benzimidazol-2-yl)ferrocene, 2-phenyl-3H-imidazo[4,5-b]pyridine derivatives

Journal of the Indian Chemical Societypublished new progress about Aliphatic aldehydes Role: RCT (Reactant), RACT (Reactant or Reagent). 197638-83-8 belongs to class piperazines, and the molecular formula is C16H22N2O3, Recommanded Product: 1-Boc-4-(4-Formylphenyl)piperazine.

Referemce:
Piperazine – Wikipedia,
Piperazines – an overview | ScienceDirect Topics

Papagni, Antonio; Del Buttero, Paola; Bertarelli, Chiara; Miozzo, Luciano; Moret, Massimo; Pryce, Mary T.; Rizzato, Silvia published the artcile< Novel fluorinated amino-stilbenes and their solid-state photodimerization>, Reference of 197638-83-8, the main research area is fluorinated aminostilbene solid state photodimerization.

We synthesized a series of polyfluoroaminostilbenes in satisfactory yields by Wittig reaction of 4-piperazinylbenzalhehydes with pentafluorobenzylidenetriphenylphosphorane and we analyzed the photochem. behavior of these stilbenes in the solid state; thanks to arene-perfluoroarene π-π interactions, some of them have shown a good propensity to give the corresponding cyclobutane photodimers in quant. yields. The photocyclization is reversible both in solution and in polymeric matrix, affording the corresponding stilbenes with different cis-trans stereoselectivity.

New Journal of Chemistrypublished new progress about [2+2] Photocycloaddition reaction. 197638-83-8 belongs to class piperazines, and the molecular formula is C16H22N2O3, Reference of 197638-83-8.

Referemce:
Piperazine – Wikipedia,
Piperazines – an overview | ScienceDirect Topics