Microwave-Assisted Chemistry: New Synthetic Application for the Rapid Construction of 1<i>H</i>-Pyrazolo[1,2-<i>b</i>]Phthalazine-5,10-Dione Derivatives in Diisopropyl Ethyl Ammonium Acetate

In the frame of research that examines the use of task-specific ionic liquids (ILs) for developing green methodologies toward bioactive substituted 1H-pyrazolo[1,2-b]phthalazine-5,10-diones derivatives via one-pot condensation of aldehydes, malononitrile and phthalhydrazide presence of Diisopropyl Ethyl Ammonium Acetate (DIPEAc-IL) as catalyst under conventional reflux as well as microwave irradiation condition. providing the desired product in very satisfactory yields (up to 94%) and high purity after simple workup. The task-specific ILs were recycled and reused four times without a noticeable decrease in their catalytic activity. Mild conditions with excellent conversions and simple product isolation procedures are noteworthy advantages of this method. The recyclability of the ionic liquid makes this protocol environmentally benign.</p

Synthesis and Antimicrobial Activity of New Carbohydrazide Bearing Quinoline Scaffolds in Silico ADMET and Molecular Docking Studies

In search of a more potent and new series of fluorine-containing quinoline, hybrid Schiff bases (6a–o) analogues were synthesized by a facile and efficient conventional method. They were developed via condensation of quinoline-4-carbohydrazide intermediate and aromatic aldehydes in presence of ethanol. All compounds viz., 6a–o were efficiently synthesized in good yields in ranges of 76–84%, respectively. All synthesized compounds were well characterized by using various spectroscopic techniques such as FT-IR, 1H NMR, 13C NMR, Mass spectroscopy. Moreover, all newly synthesized hybrid Schiff bases (6a–o) have been screened for their antifungal and antibacterial activity. Among these compounds (6a–d) shows good antibacterial activity, while compound 6b was found to be effective against a fungal pathogen Aspergillus niger and compound 6a was found to inhibit the visible growth of Staphylococcus aureus ATCC 6538 at low concentration with MIC 340 µg/.</p

An Efficient One-Pot Green Protocol for the Synthesis of Dihydrochromeno[4,3-<i>b</i>]Pyrazolo[4,3-<i>e</i>]Pyridin-6(7<i>H</i>)-Ones Mediated by Diisopropyl Ethyl Ammonium Acetate at Room Temperature

Development of a green protocol to access pharmaceutically relevant functionalized coumarin-pyrazole molecular hybrids, dihydrochromeno[4,3-b]Pyrazolo[4,3-e]pyridin-6(7H)-ones, has been accomplished based on a three-component tandem reaction between aromatic aldehydes, 4-hydroxycoumarin and 3-aminopyrazoles in presence of Diisopropyl Ethyl Ammonium Acetate (DIPEAc) as catalyst and solvent at room temperature is reported. The remarkable features of this new procedure are high yields, short reaction times, simple experimental and work-up procedures, mild and environmentally friendly reaction conditions, and the economic availability of the catalyst. </p

Efficient Rapid Access to Biginelli for the Multicomponent Synthesis of 1,2,3,4-Tetrahydropyrimidines in Room-Temperature Diisopropyl Ethyl Ammonium Acetate

The diisopropyl ethyl ammonium acetate (DIPEAc)-promoted Biginelli protocol has been developed for the first time by a successive one-pot three-component reaction of aldehydes, ethylcyanoacetate/ethyl acetoacetate, and thiourea/urea to afford pharmacologically promising 1,2,3,4-tetrahydropyrimidines in high yields at room temperature. The key benefits of the present scheme are the capability to allow a variability of functional groups, short reaction times, easy workup, high yields, recyclability of the catalyst, and solvent-free conditions, thus providing economic and environmental advantages. In addition, a series of 4-oxo-6-aryl-2-thioxo-1,2,3,4-tetrahydropyrimidine-5-carbonitriles analogues were synthesized and selected for their in vitro antifungal and antibacterial activities