Current Organocatalysis - Volume 10, Issue 4, 2023

Background: In the search for a new and effective synthetic approach to biologically chromene-derived compounds, a series of 2-amino-7, 7-dimethyl-5-oxo-4Htetrahydrochromene- 3-carbonitrile derivatives (4a-i) were synthesized. This synthesis involved the use of 4-(dimethylamino)pyridiniump-toluenesulfonate (DPTS) as a catalyst in an aqueous medium. Additionally, the relative stability between isomers was investigated using DFT/B3LYP calculations. Methods: The target compounds were synthesized through a multicomponent reaction of 5,5- dimethyl-1,3-cyclohexanedione (dimedone) 1, various arylaldehydes (2a-i), and malononitrile 3 in water and were recrystallized in ethanol. The reaction was promoted using DPTS, which is a lowtoxic, inexpensive, commercially available, and easy-to-handle catalyst. Results: The catalytic activity of DPTS was investigated in a condensation reaction conducted in an aqueous medium at room temperature. All synthesized compounds displayed considerable antimicrobial activities against human pathogenic bacteria and fungi. Conclusion: The developed synthetic protocol demonstrates energy efficiency, shorter reaction time, environmental friendliness, high product yields with purity, and scalability to gram-scale synthesis. DPTS proved to be a valuable contribution to the field of organocatalysis. The synthesized compounds were screened for in vitro antimicrobial activities, demonstrating varying potency against the microbial strains. Compound 4h exhibited the most potent activity with a zone of inhibition (ZOI) measuring 15 mm against E.coli. This was followed by compounds 4b, 4d, 4f, and 4g, which displayed a ZOI of 12 mm. Furthermore, the antifungal results revealed promising anticandidal activity for compounds 4b, 4e, and 4h, with a lower minimum inhibitory concentration (MIC) of 0.031 mg/ml. In addition, molecular electrostatic potential (MEP) mapping, reactivity indices such as electronegativity, electrophilic index, softness, and hardness, as well as frontier molecular orbitals (HOMO-LUMO), were used to provide further evidence regarding the stability and reactivity of the synthesized products.

Aim: The synthesis of diverse N-substituted pyrroles utilizing rice malt is identified. The reaction of hexane-2,5-dione with various primary amines develops the intriguing pyrrole scaffold in moderate to good yields. Methods: The reaction was carried out at room to ambient temperature in an extremely environmentally benign condition, without the need for any additional solvents or catalysts. Results: In the synthesis of N-derivatized pyrroles, several 1 amines, both cyclic and acyclic residue, have been accomplished. Conclusion: To the best of my knowledge, no study has been reported so far based on Paal- Knorr pyrrole synthesis utilizing rice malt as a catalyst and solvent.

Background: Globally, type 2 diabetes mellitus (T2DM) prevalence is increasing. A patient must have lifetime therapy for diabetes to manage it and prevent any complications. There are many different medications that can be used to treat Type 2 diabetes. Still, almost all of them concentrate on the declining insulin sensitivity and secretion that are associated with the onset of the illness. Methods: There is growing interest in the development of innovative anti-diabetic medications that are not insulin-reliant because treatments with such insulin-dependent mechanisms of action usually lose their effectiveness over time. One such technique is the inhibition of renal glucose reuptake. Results: Dapagliflozin, the first line of selective sodium-glucose cotransporter 2 inhibitors that reduce renal glucose reabsorption, is currently being developed as a therapy for Type 2 diabetes. Numerous analytical techniques have been developed for its detection, measurement, and regular quality control procedures. Conclusion: This review deliberates a thorough discussion on the chemistry of Dapagliflozin, all of its pharmacological actions with analytical and bioanalytical analyses, and more information on the clinical trials.

Introduction: We synthesized proline functionalized ionic liquid and further characterized it with analytical techniques. Method: After getting proper structural information on the above ionic liquid, we utilized them as a catalyst for the asymmetric Mannich-Type Reaction. Result: We synthesized 6 different types of β-amino α-cyano sulfones derivatives as Mannich adduct using various combinations of different imines and aryl sulphonyl as pre-nucleophiles. Conclusion: We obtained the corresponding chiral Mannich adduct followed by simple ether washing in excellent yield and stereoselectivity. We recycled the catalyst up to 6 runs without losing the catalytic activity.

Background: Determination of diagnostically significant components of biological materials using enzyme-free microscopic sensors is an urgent scientific task, which is being worked on by a significant number of scientific groups in the world. This is due to the fact that microscopic sensor-active tracks on inert surfaces can be obtained without preliminary manufacturing of precision templates. Methods: Laser Induced Chemical Liquid Phase Deposition (LCLD) is a laser technology that allows the deposition of microsized conductive tracks from aqueous solutions of transition metal compounds at the focus of a laser beam. These tracks can be formed by one or two metals at the same time. The possibility of obtaining complexes in solution in which two different metals interact with one common coordination sphere of the ligand is of particular interest. The structure of such complexes is still insufficiently studied. Results: The present study supplements the missing information on tartaric acid complexes, which can simultaneously coordinate two metals, for example, copper, nickel, silver, iron, and cobalt. Heterophase LCLD demonstrates high sensory activity in the electrochemical oxidation/reduction of glucose and hydrogen peroxide. Bimetallic deposits can be obtained in two ways. The first method consists of successive precipitation from a solution containing an ion of one metal, then another on top of the first. The second way is to create a solution in which two metals and one ligand are simultaneously present. Laser deposition is carried out in one stage. In practice, the possibility of the second method is not always realized. Conclusion: In the present work, the basic principles of the formation of heterophase bimetallic sensor-sensitive porous material with a highly developed surface under the action of laser radiation have been analyzed, and new reference data have been accumulated on the structure of tartrate complexes containing two metals.

Background: Catalysis has been widely applied in pharmaceutical companies in recent years. This paper reports a useful new approach for the synthesis of pyranopyrazoles. Objectives: One- pot synthesis of pyranopyrazoles using MgZrO 3@Fe 2O 3@ZnO as a novelcore- shell nanocatalyst which increases reaction rate, selectivity, ease of work-up and recyclability of the supports. Method: The present study deals with the synthesis of MgZrO 3@Fe 2O 3@ZnO core-shell catalyst using the sol-gel method. Results: The synthesized MgZrO 3@Fe 2O 3@ZnO core-shell nanoparticles were analysed using XRD, TEM and BET surface area. The nanocatalyst had an average particle size of 20 nm by TEM images and BET Surface area of 58.93 m2/g. Conclusion: Novel MgZrO 3@Fe 2O 3@ZnO core-shell nanoparticles have been used as an efficient and recoverable catalyst for one-pot synthesis of pyranopyrazoles.

Introduction: In this article, succinimidinium perchlorate as a new acidic ionic liquid catalyst was prepared and used to synthesize 5-arylidene barbituric acid and pyrano[2,3- d]pyrimidinone derivatives. Method: These two derivatives of barbituric acid have a variety of useful properties. Result: The advantages of this reagent were high yields, high efficiency, short reaction times, easy performance, easy work-up and reusability. Conclusion: Succinimidinium perchlorate, which was made for the first time in this project, was identified with different methods, including FT-IR, 1H NMR, 13C NMR and mass spectroscopic techniques derivatives of benzimidazole, which are shown in this review as a powerful scaffold.