60798-08-5

Upstream product

• 17672-27-4 4-hydrazinobenzonitrile 
• 105-45-3 acetoacetic acid methyl ester 
• 2863-98-1 4-hydrazinobenzonitrile hydrochloride 
• 141-97-9 ethyl acetoacetate 

Downstream Products

• 948853-48-3 C₁₂H₁₁N₃O 

Relevant academic research and scientific papers

Efficient green OLEDs achieved by a terbium(III) complex with photoluminescent quantum yield close to 100%

Electroluminescence of f-f transition lanthanide complex is a traditional topic for display over decades. Here we report highly efficient organic light-emitting diodes based on a new terbium(III) complex with novel ligand CPMIP (1-(4-cyanophenyl)-3-methyl-4-isobutyryl-pyrazoline-5-one). The high triplet energy level of CPMIP (3.0 eV) and inhibited quenching effects in the solid-state lead to a nearly 100% photoluminescent quantum efficiency of Tb(CPMIP)3. The best Tb(CPMIP)3 device exhibited maximum external quantum efficiency up to 19.7%, setting a new record of OLEDs based on f-f transition lanthanide complexes. [Figure not available: see fulltext.].

Electrochemical synthesis of versatile ammonium oxides under metal catalyst-, exogenous-oxidant-, and exogenous-electrolyte-free conditions

An electrochemical oxidative cross-coupling reaction between 2.5-substituted-pyrazolin-5-ones and ammonium thiocyanate has been developed, which resulted in a series of unprecedented cross-coupling products under metal catalyst-, exogenous-oxidant-, and exogenous-electrolyte-free conditions. It is worth noting that since the resulting cross-coupling products are nearly insoluble in MeCN, the pure product could be afforded without silica gel column purification. In addition, the prepared ammonium oxides are versatile building blocks for synthesizing functionalized pyrazole derivatives.

Histone acetyltransferase P300 small molecule inhibitor and medicinal composition and application thereof

The compound capable of inhibiting histone acetyltransferase, has a significant inhibition effect p300 in inhibiting the activity, of the histone acetyltransferase, or a pharmaceutically acceptable salt (I) of; has a significant inhibitory effect on tumor cells such as the primary, representative small molecule inhibitor p300 to prostate cancer cells, malignant blood tumor cells p300 breast cancer cells, and has an effect of inhibiting the toxicity C646, of the compound by overcoming the defects, of the original, small molecule inhibitor, existing in the present invention. C646 p300. The compounds of the formula C646; are shown in, Table (I). The invention belongs to, the field of pharmaceutical chemistry.

Copper-catalyzed acylation of pyrazolones with aldehydes to afford 4-acylpyrazolones

Copper-catalyzed direct acylation of the alkenyl C-H bond in 1,2-dihydro-3H-pyrazol-3-ones has been developed, affording a series of 4-acylpyrazolones in moderate to good yields. Notably, this protocol involves readily accessible substrates and reagents, which have good functional group tolerance leading to pyrazolone derivatives under mild reaction conditions.

Structure-activity relationships of pyrazole-4-carbodithioates as antibacterials against methicillin–resistant Staphylococcus aureus

Methicillin-resistant Staphylococcus aureus (MRSA) is a major cause of serious hospital-acquired infections and is responsible for significant morbidity and mortality in residential care facilities. New agents against MRSA are needed to combat rising resistance to current antibiotics. We recently reported 5-hydroxy-3-methyl-1-phenyl-1H-pyrazole-4-carbodithioate (HMPC) as a new bacteriostatic agent against MRSA that appears to act via a novel mechanism. Here, twenty nine analogs of HMPC were synthesized, their anti-MRSA structure-activity relationships evaluated and selectivity versus human HKC-8 cells determined. Minimum inhibitory concentrations (MIC) ranged from 0.5 to 64 μg/mL and up to 16-fold selectivity was achieved. The 4-carbodithioate function was found to be essential for activity but non-specific reactivity was ruled out as a contributor to antibacterial action. The study supports further work aimed at elucidating the molecular targets of this interesting new class of anti-MRSA agents.

One-flask synthesis of pyrazolone thioethers involving catalyzed and uncatalyzed thioetherification pathways of pyrazolones

A one-flask thioetherification of pyrazolones has been demonstrated by transforming several pyrazolones to their corresponding 4-mercaptopyrazolone derivatives and employing them towards cross-coupling with various aromatic and heteroaromatic iodides by applying Pd(OAc)2/xantphos as the catalytic system. The coupling ability of these thiol intermediates with 2,3-dichloropyrazine through an aromatic SN2 pathway has also been established. This methodology provides the use of inexpensive starting materials along with a short reaction time.

Organocatalytic Asymmetric Michael/Hemiketalization/Retro-aldol Reaction of α-Nitroketones with Unsaturated Pyrazolones: Synthesis of 3-Acyloxy Pyrazoles

An organocatalytic asymmetric cascade Michael/hemiketalization/retro-aldol reaction between unsaturated pyrazolones and α-nitroketones is described. A bifunctional thiourea catalyst was found to be efficient for this reaction. With 10 mol % of catalyst, high yields as well as excellent enantioselectivities are attained for a variety of 3-acyloxy pyrazoles under mild reaction conditions.

Expeditious synthesis of functionalized tricyclic 4-spiro pyrano[2,3-c]pyrazoles in aqueous medium using dodecylbenzenesulphonic acid as a Br?nsted acid-surfactant-combined catalyst

An efficient, three-component, one-pot synthesis of highly functionalized tricyclic 4-spiro pyrano[2,3-c]pyrazoles incorporating medicinally privileged heterocyclic moieties has been developed, which also involves the tandem Knoevenagel/Michael addition reaction followed by dehydrative cyclization of pyrazolone derivatives, cyclic 1,3-diketones and cyclic ketones, catalyzed by dodecylbenzenesulphonic acid (DBSA) as a Br?nsted acid-surfactant-combined catalyst in aqueous medium. The catalyst is found to be highly competent in accelerating this reaction that results in a considerable short reaction time, alleviating the need for high thermal energy. Wide substrate scope, high to excellent product yield, operational simplicity, absence of any hazardous organic solvent, mild reaction conditions, a simple work up procedure and easily available starting materials are the salient features of this protocol.

P-Toluenesulphonic acid-promoted, I2-catalysed sulphenylation of pyrazolones with aryl sulphonyl hydrazides

Aryl pyrazolone thioethers were synthesized via the I2-catalysed cross-coupling of pyrazolones with aryl sulphonyl hydrazides in the presence of p-toluenesulphonic acid, which has been proposed to promote the reaction by facilitating the decomposition of sulphonyl hydrazides. This journal is

DRUGS COMPRISING COMBINATION OF ANTITHROMBOTIC AGENT WITH PYRAZOLONE DERIVATIVE

It is intended to provide drugs for treating and/or preventing ischemic diseases which are safe and have little side effects. Namely, drugs comprising a combination of an antithrombotic agent and a pyrazolone derivative defined in the description or its pharmaceutically acceptable salt.