A new synthetic method was developed for the N-arylation of pyrazoles using diaryliodonium salts. The transformation does not require any transition-metal catalyst and provides the desired N-arylpyrazoles rapidly under mild reaction condition in the presence of aqueous ammonia solution as a mild base without the use of inert atmosphere. The chemoselectivity of unsymmetric diaryliodonium salts w...

Abstarct:A simple one-pot synthesis of pyrano[ 2,3-c]pyrazoles was developed by a three-component reaction of various benzaldehydes, malononitrile and 1-phenyl or hydro-3-methyl-1H-pyrazol-5(4H)-one in the presence of N-methyl pyridinium p-toluene sulfonate (NMPyTs) as a catalyst. All of the synthesized compounds were identified by IR, 1H NMR, 13C NMR and mass spectroscopy techniques. In the me...

The five membered heterocyclic compounds pyrazolines were found as the core structure in a large variety of compounds. Pyrazoles have been the recent target of numerous methodologies, mostly due to their prevalence as scaffolds in synthesis of bioactive compounds and reactions in different media. In this review, an attempt is made to provide an up to date developments in the synthetic strategie...

Chromones, six-membered oxygen heterocycles, and pyrazoles, five-membered two-adjacent-nitrogen-containing heterocycles, represent two important classes of biologically active compounds. Certain derivatives of these scaffolds play an important role in medicinal chemistry and have been extensively used as versatile building blocks in organic synthesis. In this context, we will discuss the most r...

The vaporization enthalpies of 1-methyl-, 1-ethyl-, 1-phenyl-, and 1-benzylimidazole, 1-methyl- and 1-phenylpyrazole, and trans-azobenzene are evaluated by correlation-gas chromatography (C-GC) using a variety of azines and diazines as standards. The vaporization enthalpies obtained by C-GC when compared to literature values are approximately 14 kJ·mol(-1) smaller for the imidazoles and 6 kJ·mo...

BACKGROUND The present study was designed to investigate the insecticidal efficacy of four different classes of insecticides: pyrethroids, organophosphates, phenyl-pyrazoles and neo-nicotenoids. One representative chemical from each class was selected to compare the toxicity: deltamethrin from pyrethroids, Dichlorovinyl Dimethyl Phosphate (DDVP) from organophosphates, fipronil from phenyl-pyraz...

Abstract An efficient cycloaddition reaction of trifluoroacetohydrazonoyl bromides with nitroolefins was developed, which regioselectively produced 3‐trifluoromethyl‐4‐substituted pyrazoles. The has the advantages mild conditions, good tolerance functional groups and simple operation.

We have developed a new method of iodocyclization based on reagent-controlled oxidative aromatization. Our strategy takes advantage of the dual nature of iodine as both an iodinating and an oxidizing agent. This approach enabled "product switch" and enhanced the flexibility of the synthetic pathway toward pyrazoles and isoxazoles. In addition, the iodo moiety of the cyclized product could creat...

An efficient synthesis of pyrazoles from tosylhydrazones and nitroalkenes was developed. In comparison with the previously reported 1,3-dipolar cycloaddition reaction of diazo compounds with electron-deficient alkenes or alkynes, this methodology proceeded with a sequential Baylis-Hillman/intramolecular cyclization mechanism and a variety of reversed regioselectivity products were prepared in g...

Direct arylation of most five-membered ring heterocycles are generally easily accessible and strongly favored at the ?-position using classical palladium-catalysis. Conversely, regioselective functionalization such concurrent ?-position remains currently very challenging. Herein, we report general conditions for direct pyrazoles, while C?H is free. By aryl bromides as source a judicious choice ...